Percocet

Generic Name: oxycodone and acetaminophen (Oral route)

a-seet-a-MIN-oh-fen, ox-i-KOE-done hye-droe-KLOR-ide

Oral route(Tablet)

Acetaminophen has been associated with cases of acute liver failure, at times resulting in liver transplant and death. Most of the cases of liver injury are associated with the use of acetaminophen at doses that exceed 4000 mg/day, and often involve more than one acetaminophen-containing product .

Commonly used brand name(s)

In the U.S.

• Endocet


• Magnacet


• Narvox


• Percocet


• Perloxx


• Primalev


• Roxicet


• Roxilox


• Tylox


• Xolox

Available Dosage Forms:

• Tablet


• Solution


• Capsule

Therapeutic Class: Opioid/Acetaminophen Combination

Chemical Class: Oxycodone

Uses For Percocet

Oxycodone and acetaminophen combination is used to relieve moderate to moderately severe pain.

Acetaminophen is used to relieve pain and reduce fever in patients. It does not become habit-forming when taken for a long time. But acetaminophen may cause other unwanted effects when taken in large doses, including liver damage.

Oxycodone belongs to the group of medicines called narcotic analgesics (pain medicines). It acts on the central nervous system (CNS) to relieve pain.

When oxycodone is used for a long time, it may become habit-forming, causing mental or physical dependence. However, people who have continuing pain should not let the fear of dependence keep them from using narcotics to relieve their pain. Mental dependence (addiction) is not likely to occur when narcotics are used for this purpose. Physical dependence may lead to withdrawal side effects if treatment is stopped suddenly. However, severe withdrawal side effects can usually be prevented by gradually reducing the dose over a period of time before treatment is stopped completely.

This medicine is available only with your doctor's prescription.

Before Using Percocet

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Appropriate studies have not been performed on the relationship of age to the effects of oxycodone and acetaminophen combination in the pediatric population. Safety and efficacy have not been established.

Geriatric

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of oxycodone and acetaminophen combination in the elderly. However, elderly patients are more likely to have age-related kidney or liver problems, which may require caution and an adjustment in the dose for patients receiving oxycodone and acetaminophen combination.

Pregnancy

	Pregnancy Category	Explanation
All Trimesters	C	Animal studies have shown an adverse effect and there are no adequate studies in pregnant women OR no animal studies have been conducted and there are no adequate studies in pregnant women.

Breast Feeding

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.

• Naltrexone

Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Acetophenazine


• Adinazolam


• Alfentanil


• Alprazolam


• Amobarbital


• Anileridine


• Aprobarbital


• Atazanavir


• Brofaromine


• Bromazepam


• Brotizolam


• Buprenorphine


• Buspirone


• Butabarbital


• Butalbital


• Butorphanol


• Carisoprodol


• Chloral Hydrate


• Chlordiazepoxide


• Chlorpromazine


• Chlorzoxazone


• Clarithromycin


• Clobazam


• Clonazepam


• Clorazepate


• Clorgyline


• Codeine


• Dantrolene


• Desflurane


• Dexmedetomidine


• Dezocine


• Diazepam


• Diphenhydramine


• Doxylamine


• Enflurane


• Erythromycin


• Escitalopram


• Estazolam


• Eszopiclone


• Ethchlorvynol


• Ethopropazine


• Fentanyl


• Flumazenil


• Flunitrazepam


• Fluphenazine


• Flurazepam


• Fluvoxamine


• Fospropofol


• Furazolidone


• Halazepam


• Halothane


• Hydrocodone


• Hydromorphone


• Hydroxyzine


• Indinavir


• Iproniazid


• Isocarboxazid


• Isoflurane


• Itraconazole


• Ketamine


• Ketazolam


• Ketoconazole


• Lazabemide


• Levorphanol


• Linezolid


• Lorazepam


• Lormetazepam


• Medazepam


• Meperidine


• Mephenesin


• Mephobarbital


• Meprobamate


• Mesoridazine


• Metaxalone


• Methdilazine


• Methocarbamol


• Methohexital


• Midazolam


• Moclobemide


• Morphine


• Morphine Sulfate Liposome


• Nalbuphine


• Nefazodone


• Nelfinavir


• Nialamide


• Nitrazepam


• Nitrous Oxide


• Nordazepam


• Opium


• Oxazepam


• Oxycodone


• Oxymorphone


• Pargyline


• Pentazocine


• Pentobarbital


• Perphenazine


• Phenelzine


• Phenobarbital


• Prazepam


• Procarbazine


• Prochlorperazine


• Promazine


• Promethazine


• Propiomazine


• Propofol


• Propoxyphene


• Quazepam


• Ramelteon


• Rasagiline


• Remifentanil


• Ritonavir


• Saquinavir


• Secobarbital


• Selegiline


• Sertraline


• Sevoflurane


• Sodium Oxybate


• Sufentanil


• Tapentadol


• Telithromycin


• Temazepam


• Thiethylperazine


• Thiopental


• Thioridazine


• Toloxatone


• Tranylcypromine


• Triazolam


• Trifluoperazine


• Triflupromazine


• Trimeprazine


• Zaleplon


• Zolpidem

Using this medicine with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Acenocoumarol


• Carbamazepine


• Isoniazid


• Miconazole


• Phenytoin


• Rifampin


• St John's Wort


• Voriconazole


• Warfarin


• Zidovudine

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following is usually not recommended, but may be unavoidable in some cases. If used together, your doctor may change the dose or how often you use this medicine, or give you special instructions about the use of food, alcohol, or tobacco.

• Ethanol

Using this medicine with any of the following may cause an increased risk of certain side effects but may be unavoidable in some cases. If used together, your doctor may change the dose or how often you use this medicine, or give you special instructions about the use of food, alcohol, or tobacco.

• Cabbage

Other Medical Problems

The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

• Addison's disease (adrenal gland problem) or


• Alcohol abuse, history of or


• Brain tumor, history of or


• Chronic obstructive pulmonary disease (COPD) or


• CNS depression or


• Cor pulmonale (serious heart condition) or


• Drug dependence, especially with narcotics, or history of or


• Enlarged prostate (BPH, prostatic hypertrophy) or


• Head injuries, history of or


• Hypothyroidism (an underactive thyroid) or


• Hypovolemia (low blood volume) or


• Kyphoscoliosis (curvature of the spine with breathing problems) or


• Mental illness or


• Problems with passing urine—Use with caution. May increase risk for more serious side effects.

• Asthma, severe or


• Hypercarbia (high carbon dioxide in the blood), severe or


• Paralytic ileus (bowels stop working and may be blocked) or


• Respiratory depression (very slow breathing)—Should not be used in patients with these conditions.

• Hypotension (low blood pressure) or


• Pancreatitis (inflammation of the pancreas) or


• Seizures, history of or


• Stomach problems—Use with caution. May make these conditions worse.

• Kidney disease or


• Liver disease—Use with caution. The effects may be increased because of slower removal of the medicine from the body.

Proper Use of oxycodone and acetaminophen

This section provides information on the proper use of a number of products that contain oxycodone and acetaminophen. It may not be specific to Percocet. Please read with care.

Take this medicine only as directed by your doctor. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered. This is especially important for elderly patients, who may be more sensitive to the effects of pain medicines. If too much of this medicine is taken for a long time, it may become habit-forming and cause mental or physical dependence. Also, large amounts of acetaminophen may cause liver damage if taken for a long time.

Measure the oral liquid using the patient cup that comes with the package.

Carefully check the labels of all other medicines you are using, because they may also contain acetaminophen. It is not safe to use more than 4 grams (4,000 milligrams) of acetaminophen in one day (24 hours).

Dosing

The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

• For moderate to moderately severe pain:
  
  • For oral dosage form (capsules):
    
    • Adults—One capsule every 6 hours as needed.
    
    
    • Children—Use and dose must be determined by your doctor.
    
    
  
  
  • For oral dosage form (solution):
    
    • Adults—5 milliliters (mL) or one teaspoonful every 6 hours as needed. However, the dose is usually not more than 60 mL (12 teaspoonfuls) per day.
    
    
    • Children—Use and dose must be determined by your doctor.
    
    
  
  
  • For oral dosage form (tablets):
    
    • Adults—One tablet every 6 hours as needed. However, the dose is usually not more than 6 to 12 tablets per day.
    
    
    • Children—Use and dose must be determined by your doctor.
    
    
  
  

Missed Dose

If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Flush any unused capsules, liquid, or tablets down the toilet.

Precautions While Using Percocet

It is very important that your doctor check your progress while you are taking this medicine. This will allow your doctor to see if the medicine is working properly and to decide if you should continue to take it.

It is against the law and dangerous for anyone else to use your medicine. Keep your unused tablets in a safe and secure place. People who are addicted to drugs might want to steal this medicine.

This medicine will add to the effects of alcohol and other CNS depressants (medicines that can make you drowsy or less alert). Some examples of CNS depressants are antihistamines or medicine for allergies or colds; sedatives, tranquilizers, or sleeping medicine; other prescription pain medicine or narcotics; medicine for seizures or barbiturates; muscle relaxants; or anesthetics, including some dental anesthetics. Also, there may be a greater risk of liver damage if you drink three or more alcoholic beverages while you are taking acetaminophen. Do not drink alcoholic beverages, and check with your doctor before taking any of these medicines while you are using this medicine.

This medicine may be habit-forming. If you feel that the medicine is not working as well, do not use more than your prescribed dose. Call your doctor for instructions.

Dizziness, lightheadedness, or fainting may occur when you get up suddenly from a lying or sitting position. Getting up slowly may help lessen this problem. Also, lying down for a while may relieve the dizziness or lightheadedness.

This medicine may make you dizzy, drowsy, or lightheaded. Make sure you know how you react to this medicine before you drive, use machines, or do anything else that could be dangerous if you are dizzy or not alert.

Check with your doctor right away if you have pain or tenderness in the upper stomach; pale stools; dark urine; loss of appetite; nausea; unusual tiredness or weakness; or yellow eyes or skin. These could be symptoms of a serious liver problem.

This medicine may cause a serious type of allergic reaction called anaphylaxis. Anaphylaxis can be life-threatening and requires immediate medical attention. Stop using this medicine and call your doctor right away if you have a rash; itching; hoarseness; trouble breathing; trouble swallowing; or any swelling of your hands, face, or mouth while you are using this medicine.

Using narcotics for a long time can cause severe constipation. To prevent this, your doctor may direct you to take laxatives, drink a lot of fluids, or increase the amount of fiber in your diet. Be sure to follow the directions carefully, because continuing constipation can lead to more serious problems.

If you have been using this medicine regularly for several weeks or longer, do not change your dose or suddenly stop using it without checking with your doctor. Your doctor may want you to gradually reduce the amount you are using before stopping it completely. This may help prevent worsening of your condition and reduce the possibility of withdrawal symptoms, such as abdominal or stomach cramps, anxiety, fever, irritability, nausea, restlessness, runny nose, sweating, tremors, or trouble with sleeping.

Using this medicine while you are pregnant may cause serious unwanted effects in your newborn baby. Tell your doctor right away if you think you are pregnant or if you plan to become pregnant while using this medicine.

Before you have any medical tests, tell the medical doctor in charge that you are taking this medicine. The results of some tests may be affected by this medicine.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines, especially those containing acetaminophen (Tylenol (R)), and herbal or vitamin supplements.

Percocet Side Effects

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

More common

• Abdominal or stomach pain


• black, tarry stools


• chills


• dark urine


• dizziness


• fever


• headache


• itching


• light-colored stools


• loss of appetite


• nausea


• rash


• unpleasant breath odor


• unusual tiredness or weakness


• vomiting of blood


• yellow eyes or skin

Rare

• Cough or hoarseness


• fever with or without chills


• general feeling of tiredness or weakness


• lower back or side pain


• painful or difficult urination


• sore throat


• sores, ulcers, or white spots on the lips or in the mouth


• unusual bleeding or bruising

Incidence not known

• Back, leg, or stomach pains


• bleeding gums


• bloating


• blood in the urine or stools


• blue lips and fingernails


• blurred vision


• burning, crawling, itching, numbness, prickling, "pins and needles", or tingling feelings


• chest pain or discomfort


• clay-colored stools


• cloudy urine


• clumsiness


• confusion


• constipation


• coughing that sometimes produces a pink frothy sputum


• decrease in the frequency of urination


• decrease in urine volume


• decreased awareness or responsiveness


• decreased frequency or amount of urine


• decreased urination


• difficult or labored breathing


• difficult or painful urination


• difficult, fast, noisy breathing, sometimes with wheezing


• difficulty in passing urine (dribbling)


• difficulty with swallowing


• dizziness, faintness, or lightheadedness when getting up suddenly from a lying or sitting position


• drowsiness


• dry mouth


• extremely shallow or slow breathing


• fainting


• fast or deep breathing


• fast, slow, irregular, pounding, or racing heartbeat or pulse


• feeling of warmth


• general body swelling


• greatly decreased frequency of urination or amount of urine


• hives or welts


• increase in heart rate


• increased blood pressure


• increased sweating


• increased thirst


• indigestion


• large, hive-like swelling on the face, eyelids, lips, tongue, throat, hands, legs, feet, or sex organs


• lightheadedness


• low body temperature


• muscle aches


• muscle tremors


• muscle weakness


• nervousness


• noisy breathing


• nosebleeds


• numbness or tingling in the hands, feet, or lips


• pains in the stomach, side, or abdomen, possibly radiating to the back


• pale skin


• pinpoint red spots on the skin


• pounding in the ears


• puffiness or swelling of the eyelids or around the eyes, face, lips, or tongue


• rapid, deep breathing


• rapid, shallow breathing


• redness of the face, neck, arms, and occasionally, upper chest


• redness of the skin


• restlessness


• seizures


• severe constipation


• severe sleepiness


• severe vomiting


• shivering


• shortness of breath


• skin blisters


• skin rash


• sleepiness


• slow or irregular breathing


• sore throat


• stomach cramps


• stomach pain, continuing


• sudden decrease in the amount of urine


• sunken eyes


• sweating


• swelling in the legs and ankles


• swelling of the face, fingers, or lower legs


• thirst


• tightness in the chest


• tiredness


• troubled breathing


• unpleasant breath odor


• upper right abdominal or stomach pain


• vomiting


• vomiting of blood


• weak or feeble pulse


• weakness or heaviness of the legs


• weight gain


• wheezing


• wrinkled skin

Get emergency help immediately if any of the following symptoms of overdose occur:

Symptoms of overdose

• Bluish lips or skin


• change in consciousness


• cold, clammy skin


• extreme sleepiness


• general feeling of discomfort or illness


• loss of consciousness


• no blood pressure or pulse


• not breathing


• stopping of heart


• unconsciousness

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

• Relaxed and calm

Incidence not known

• Acid or sour stomach


• agitation


• anxiety


• bad or unusual or unpleasant (after) taste


• belching


• change in taste


• cold sweats


• constricted, pinpoint, or small pupils (black part of the eye)


• continuing ringing or buzzing or other unexplained noise in the ears


• cool, pale skin


• depression


• diarrhea


• difficulty with moving


• disturbed color perception


• double vision


• excess air or gas in the stomach or intestines


• false or unusual sense of well-being


• flushed, dry skin


• fruit-like breath odor


• full feeling


• general feeling of discomfort or illness


• halos around lights


• hearing loss


• heartburn


• increased hunger


• increased thirst


• increased urination


• indigestion


• joint pain


• lack or loss of strength


• muscle cramps or spasms


• muscle pain or stiffness


• nervousness


• night blindness


• nightmares


• overbright appearance of lights


• passing gas


• rash


• red eye


• seeing, hearing, or feeling things that are not there


• seizures


• severe sleepiness


• shakiness


• sleepiness or unusual drowsiness


• sleeplessness


• slurred speech


• stomach discomfort, upset, or pain


• stomach fullness


• sweating


• swollen joints


• thirst


• trouble sleeping


• troubled breathing


• tunnel vision


• unable to sleep


• unexplained weight loss


• unusual drowsiness, dullness, tiredness, weakness, or feeling of sluggishness

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

See also: Percocet side effects (in more detail)

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More Percocet resources

• Percocet Side Effects (in more detail)
• Percocet Use in Pregnancy & Breastfeeding
• Drug Images
• Percocet Drug Interactions
• Percocet Support Group
• 122 Reviews for Percocet - Add your own review/rating

Compare Percocet with other medications

• Pain

Fortesta Gel

Pronunciation: tes-TOS-ter-one
Generic Name: Testosterone
Brand Name: Fortesta

Children who have been exposed to Fortesta Gel have developed symptoms such as enlarged genitals; increased pubic hair, erections, or sex drive; aggressive behavior; and increased bone age. Contact the child's doctor right away if any of these symptoms occur. Children should avoid contact with unwashed or unclothed application sites in men who use Fortesta Gel.

Closely follow the recommended instructions for use of Fortesta Gel.

Fortesta Gel is used for:

Treating symptoms of low testosterone in adult men when the body does not make any testosterone or not enough testosterone (hypogonadism). It may also be used for other conditions as determined by your doctor.

Fortesta Gel is an androgen hormone. It works by replacing or supplementing the testosterone that is naturally made in the body.

Do NOT use Fortesta Gel if:

• you are allergic to any ingredient in Fortesta Gel


• you are pregnant, may become pregnant, or are breast-feeding


• you have known or suspected breast or prostate cancer

Contact your doctor or health care provider right away if any of these apply to you.

Before using Fortesta Gel:

Some medical conditions may interact with Fortesta Gel. Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:

• if you are pregnant, planning to become pregnant, or are breast-feeding


• if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement


• if you have allergies to medicines, foods, or other substances


• if you have heart problems (eg, congestive heart failure), high cholesterol levels, swelling or fluid buildup (edema), lung problems, or sleep apnea (long pauses in breathing while you sleep)


• if you have cancer, diabetes, an enlarged prostate, benign prostatic hypertrophy (BPH), kidney or liver problems, high blood calcium levels, or you are overweight


• if you are using insulin

Some MEDICINES MAY INTERACT with Fortesta Gel. Tell your health care provider if you are taking any other medicines, especially any of the following:

• Corticosteroids (eg, prednisone) or corticotropin (ACTH) because they may increase the risk of Fortesta Gel's side effects


• Anticoagulants (eg, warfarin) because the risk of their side effects may be increased by Fortesta Gel

This may not be a complete list of all interactions that may occur. Ask your health care provider if Fortesta Gel may interact with other medicines that you take. Check with your health care provider before you start, stop, or change the dose of any medicine.

How to use Fortesta Gel:

Use Fortesta Gel as directed by your doctor. Check the label on the medicine for exact dosing instructions.

• Fortesta Gel comes with an extra patient information sheet called a Medication Guide. Read it carefully. Read it again each time you get Fortesta Gel refilled.


• You will need to prime this product before the first use. To prime it, with the canister in the upright position, depress the pump 8 times and appropriately discard the gel that is pumped out.


• Apply Fortesta Gel with one finger and gently rub it evenly onto clean, dry skin of the front and inner thighs. Make sure that your shorts or pants will be able to cover the application site.


• Do not apply Fortesta Gel to the genitals or other parts of the body. Avoid applying Fortesta Gel to the thigh adjacent to the scrotum. Do not apply it over open sores, wounds, or irritated skin.


• It is best to apply Fortesta Gel at the same time every day in the morning after showering or bathing, unless directed otherwise by your doctor.


• Do not allow another person to apply Fortesta Gel for you.


• Wash your hands with soap and water immediately after using Fortesta Gel.


• Allow Fortesta Gel to dry for a few minutes before dressing.


• After Fortesta Gel has dried, cover the application site (eg, with shorts or pants) to prevent others from coming into contact with Fortesta Gel. If direct skin-to-skin contact with another person is expected, wash the application site well with soap and water to remove the medicine.


• For best results, wait at least 2 hours after applying Fortesta Gel before you shower or swim. Showering or swimming just 1 hour after applying Fortesta Gel may be permitted if done very infrequently.


• If you miss a dose of Fortesta Gel, use it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not use 2 doses at once.

Ask your health care provider any questions you may have about how to use Fortesta Gel.

Important safety information:

• Fortesta Gel may cause dizziness. This effect may be worse if you take it with alcohol or certain medicines. Use Fortesta Gel with caution. Do not drive or perform other possibly unsafe tasks until you know how you react to it.


• Do NOT change your dose or use more than the recommended dose without checking with your doctor.


• Patients who use androgens (such as testosterone) may have an increased risk of prostate cancer. Check with your doctor if you have questions about your risk of prostate cancer while you use Fortesta Gel.


• Do not allow others, especially children and women, to come into contact with the medicine, the application site, or any unwashed clothing that may have touched the application site. If someone else comes into contact with Fortesta Gel, have them wash the area with soap and water right away.


• Contact your doctor right away if a child you are in close contact with develops enlarged genitals, pubic hair, or increased sex drive, or if your female partner develops a change in hair distribution, an increase in acne, or any masculine signs.


• Fortesta Gel is flammable. Avoid fire, an open flame, or smoking after application until Fortesta Gel has dried.


• Do not switch between other topical testosterone products and Fortesta Gel without talking to your doctor.


• Tell your doctor or dentist that you take Fortesta Gel before you receive any medical or dental care, emergency care, or surgery.


• Fortesta Gel may interfere with certain lab tests. Be sure your doctor and lab personnel know you are using Fortesta Gel.


• Diabetes patients - Fortesta Gel may affect your blood sugar. Check blood sugar levels closely. Ask your doctor before you change the dose of your diabetes medicine.


• Large doses of Fortesta Gel may lower your sperm count. Discuss any questions or concerns with your doctor.


• Lab tests, including liver function, hematocrit, blood cholesterol, prostate-specific antigen (PSA), and blood testosterone, may be performed while you use Fortesta Gel. These tests may be used to monitor your condition or check for side effects. Be sure to keep all doctor and lab appointments.


• Use Fortesta Gel with caution in the ELDERLY; they may be more sensitive to its effects, especially an enlarged prostate or prostate cancer.


• Fortesta Gel should be used with extreme caution in CHILDREN younger than 18 years old; safety and effectiveness in these children have not been confirmed.


• PREGNANCY and BREAST-FEEDING: Fortesta Gel is not approved for use in women. Fortesta Gel may cause harm to the fetus. Do not use Fortesta Gel if you are pregnant. If you think you may be pregnant, contact your doctor right away. It is not known if Fortesta Gel is found in breast milk. Do not breast-feed while using Fortesta Gel.

Possible side effects of Fortesta Gel:

All medicines may cause side effects, but many people have no, or minor, side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome:

Abnormal dreams; acne; change in sex drive; dizziness; headache; skin redness or irritation at the application site.

Seek medical attention right away if any of these SEVERE side effects occur:

Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); breast tenderness or enlargement; calf pain, swelling, or redness; change in the size or shape of the testicles; dark urine; excessive daytime sleepiness; frequent, prolonged, or painful erections; interrupted breathing while sleeping; loss of appetite; memory problems; migraine; mood or mental changes (eg, anxiety, depression, hostility, suicidal thoughts); nausea; new or worsening urination problems (eg, frequent urination, inability to urinate, weak urine stream); pale stools; severe headache; shortness of breath; skin discoloration; stomach pain; swelling of the hands, ankles, or legs; trouble sleeping or other sleep changes; unexplained or unusual weight gain; unusual tiredness or weakness; vomiting; yellowing of the skin or eyes.

This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider. Call your doctor for medical advice about side effects. To report side effects to the appropriate agency, please read the Guide to Reporting Problems to FDA.

See also: Fortesta side effects (in more detail)

If OVERDOSE is suspected:

Contact 1-800-222-1222 (the American Association of Poison Control Centers), your local poison control center, or emergency room immediately. Symptoms may include confusion; one-sided weakness; slurred speech; vision changes.

Proper storage of Fortesta Gel:

Store Fortesta Gel between 68 and 77 degrees F (20 and 25 degrees C). Brief storage at temperatures between 59 and 86 degrees F (15 and 30 degrees C) is permitted. Do not freeze. Store away from heat, moisture, and light. Keep Fortesta Gel out of the reach of children and away from pets.

General information:

• If you have any questions about Fortesta Gel, please talk with your doctor, pharmacist, or other health care provider.


• Fortesta Gel is to be used only by the patient for whom it is prescribed. Do not share it with other people.


• If your symptoms do not improve or if they become worse, check with your doctor.


• Check with your pharmacist about how to dispose of unused medicine.

This information is a summary only. It does not contain all information about Fortesta Gel. If you have questions about the medicine you are taking or would like more information, check with your doctor, pharmacist, or other health care provider.

Issue Date: February 1, 2012

Database Edition 12.1.1.002

Copyright © 2012 Wolters Kluwer Health, Inc.

More Fortesta resources

• Fortesta Side Effects (in more detail)
• Fortesta Use in Pregnancy & Breastfeeding
• Fortesta Drug Interactions
• Fortesta Support Group
• 2 Reviews for Fortesta - Add your own review/rating

Compare Fortesta with other medications

• Hypogonadism, Male

Antidepressants

Antidepressants are drugs that treat depression and improve the symptoms. The main types of antidepressants are tricyclic antidepressants, selective serotonin reuptake inhibitors, monoamine oxidase inhibitors and other atypical antidepressants. All types of antidepressant drugs may take more than two weeks to show any benefits, although their pharmacological effects are produced immediately.

See also

• miscellaneous antidepressants
• monoamine oxidase inhibitors
• phenylpiperazine antidepressants
• selective serotonin reuptake inhibitors
• serotonin-norepinephrine reuptake inhibitors
• tetracyclic antidepressants
• tricyclic antidepressants

Drug List:

Hydrocortisone Butyrate Solution

Dosage Form: topical solution
Hydrocortisone Butyrate Solution, 0.1%



For Dermatological Use Only

DESCRIPTION

Hydrocortisone Butyrate Solution, 0.1% contains the topical corticosteroid hydrocortisone butyrate, a non-fluorinated hydrocortisone ester. It has the chemical name: pregn-4-ene-3,20-dione, 11,21 - dihydroxy-17-[(1-oxobutyl)oxy]-, (11β-;

the molecular formula: C25H36O6;

the molecular weight: 432.54;

and the CAS registry number: 13609-67-1.

Its structural formula is:

Each mL of Hydrocortisone Butyrate Solution, 0.1% contains 1.0 mg of hydrocortisone butyrate in a vehicle consisting of isopropyl alcohol (50%), glycerin, povidone, citric acid, sodium citrate and purified water.

CLINICAL PHARMACOLOGY

Topical corticosteroids share anti-inflammatory, anti-pruritic and vasoconstrictive actions. The mechanism of anti-inflammatory activity of the topical corticosteroids is unclear. Various laboratory methods, including vasoconstrictor assays, are used to compare and predict potencies and/or clinical efficacies of the topical corticosteroids. There is some evidence to suggest that a recognizable correlation exists between vasoconstrictor potency and therapeutic efficacy in man.

PHARMACOKINETICS

The extent of percutaneous absorption of topical corticosteroids is determined by many factors including the vehicle, the integrity of the epidermal barrier, and the use of occlusive dressings.

Topical corticosteroids can be absorbed from normal intact skin. Inflammation and/or other disease processes in the skin increase percutaneous absorption. Occlusive dressings substantially increase the percutaneous absorption of topical corticosteroids.

Once absorbed through the skin, topical corticosteroids are handled through pharmacokinetic pathways similar to systemically administered corticosteroids. Corticosteroids are bound to plasma proteins in varying degrees. Corticosteroids are metabolized primarily in the liver and are then excreted by the kidneys. Some of the topical corticosteroids and their metabolites are also excreted into the bile.

INDICATIONS AND USAGE

Hydrocortisone Butyrate Solution, 0.1% is indicated for the relief of the inflammatory and pruritic manifestations of seborrheic dermatoses.

CONTRAINDICATIONS

Topical corticosteroids are contraindicated in those patients with a history of hypersensitivity to any of the components of the preparation.

PRECAUTIONS

General

Systemic absorption of topical corticosteroids has produced reversible hypothalamic-pituitary-adrenal (HPA) axis suppression, manifestations of Cushing's syndrome, hyperglycemia, and glucosuria in some patients. Conditions which augment systemic absorption include the application of the more potent steroids, use over large surface areas, prolonged use, and the addition of occlusive dressings.

Therefore, patients receiving a large dose of a potent topical steroid applied to a large surface area or under an occlusive dressing should be evaluated periodically for evidence of HPA axis suppression by using the urinary free cortisol and ACTH stimulation tests.

If HPA axis suppression is noted, an attempt should be made to withdraw the drug, to reduce the frequency of application, or to substitute a less potent steroid.

Recovery of HPA axis function is generally prompt and complete upon discontinuation of the drug.

Infrequently, signs and symptoms of steroid withdrawal may occur, requiring supplemental systemic corticosteroids.

Children may absorb proportionally larger amounts of topical corticosteroids and thus be more susceptible to systemic toxicity.

(See PRECAUTIONS - PEDIATRIC USE).

If irritation develops, topical corticosteroids should be discontinued and appropriate therapy instituted.

In the presence of dermatological infections, the use of an appropriate antifungal or antibacterial agent should be instituted. If a favorable response does not occur promptly, the corticosteroid should be discontinued until the infection has been adequately controlled.

Information for the Patient

Patients using topical corticosteroids should receive the following information and instructions:

1. This medication is to be used as directed by the physician. It is for external use only. Avoid contact with the eyes.

2. Patients should be advised not to use this medication for any disorder other than for which it was prescribed.

3. The treated skin area should not be bandaged or otherwise covered or wrapped as to be occlusive unless directed by the physician.

4. Patients should report any signs of local adverse reactions especially under occlusive dressing.

5. Parents of pediatric patients should be advised not to use tight-fitting diapers or plastic pants on a child being treated in the diaper area, as these garments may constitute occlusive dressings.

Laboratory Tests

The following tests may be helpful in evaluating the HPA axis suppression:

Urinary free cortisol test

ACTH stimulation test

Carcinogenesis, Mutagenesis, and Impairment of Fertility

Long-term animal studies have not been performed to evaluate the carcinogenic potential or the effect on fertility of topical corticosteroids.

Studies to determine mutagenicity with prednisolone and hydrocortisone have revealed negative results.

Pregnancy Category C

Corticosteroids are generally teratogenic in laboratory animals when administered systemically at relatively low dosage levels. The more potent corticosteroids have been shown to be teratogenic after dermal application in laboratory animals. There are no adequate and well-controlled studies in pregnant women on teratogenic effects from topically applied corticosteroids. Therefore, topical corticosteroids should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Drugs of this class should not be used extensively on pregnant patients, in large amounts, or for prolonged periods of time.

Nursing Mothers

It is not known whether topical administration of corticosteroids could result in sufficient systemic absorption to produce detectable quantities in breast milk. Systemically administered corticosteroids are secreted into breast milk, in quantities not likely to have a deleterious effect on the infant. Nevertheless, caution should be exercised when topical corticosteroids are administered to a nursing woman.

Pediatric Use

Pediatric patients may demonstrate greater susceptibility to topical corticosteroid-induced HPA axis suppression and Cushing's syndrome than mature patients because of a larger skin surface area to body weight ratio.

Hypothalamic-pituitary-adrenal (HPA) axis suppression, Cushing's syndrome, and intracranial hypertension have been reported in children receiving topical corticosteroids.

Manifestations of adrenal suppression in children include linear growth retardation, delayed weight gain, low plasma cortisol levels, and absence of response to ACTH stimulation. Manifestations of intracranial hypertension include bulging fontanelles, headaches, and bilateral papilledema.

Administration of topical corticosteroids to children should be limited to the least amount compatible with an effective therapeutic regimen. Chronic corticosteroid therapy may interfere with the growth and development of children.

ADVERSE REACTIONS

The following local adverse reactions are reported infrequently with topical corticosteroids but may occur more frequently with the use of occlusive dressings. These reactions are listed in an approximate decreasing order of occurrence: burning, itching, irritation, dryness, folliculitis, hypertrichosis, acneiform eruptions, hypopigmentation, perioral dermatitis, allergic contact dermatitis, maceration of the skin, secondary infection, skin atrophy, striae, miliaria.

OVERDOSAGE

Topically applied corticosteroids can be absorbed in sufficient amounts to produce systemic effects. (See PRECAUTIONS.)

DOSAGE AND ADMINISTRATION

Hydrocortisone Butyrate Solution, 0.1% should be applied to the affected area as a thin film two or three times daily depending on the severity of the condition.

HOW SUPPLIED

Hydrocortisone Butyrate Solution, 0.1% is supplied in tubes containing:

60 mL          NDC 43478-273-61

STORAGE

Store at controlled temperature between 41° - 77°F (5° - 25°C).

Manufactured for Rouses Point Pharmaceuticals, LLC

Cranford, NJ 07016

By Ferndale Laboratories, Inc.

Ferndale, MI 48220

PRINCIPAL DISPLAY PANEL

NDC 43478-273-61

HYDROCORTISONE BUTYRATE  hydrocortisone butyrate  solution

Product Information Product Type HUMAN PRESCRIPTION DRUG NDC Product Code (Source) 43478-273 Route of Administration TOPICAL DEA Schedule

Active Ingredient/Active Moiety Ingredient Name Basis of Strength Strength HYDROCORTISONE BUTYRATE (HYDROCORTISONE) HYDROCORTISONE BUTYRATE 1 mg  in 1 mL

Inactive Ingredients Ingredient Name Strength ISOPROPYL ALCOHOL   ANHYDROUS CITRIC ACID   SODIUM CITRATE   GLYCERIN   POVIDONE   WATER

Product Characteristics Color      Score      Shape Size Flavor Imprint Code Contains

Packaging # NDC Package Description Multilevel Packaging 1 43478-273-61 1 BOTTLE In 1 CARTON contains a BOTTLE 1 60 mL In 1 BOTTLE This package is contained within the CARTON (43478-273-61)

Marketing Information
Marketing Category	Application Number or Monograph Citation	Marketing Start Date	Marketing End Date
NDA	NDA019116	02/24/2010

Labeler - Rouses Point Pharm (849346924)

Registrant - Triax Pharmaceuticals, LLC (194481409)

Establishment
Name	Address	ID/FEI	Operations
Ferndale Laboratories, Inc.		005320536	MANUFACTURE, ANALYSIS

Establishment
Name	Address	ID/FEI	Operations
Pharmacia & Upjohn Co., Inc.		007702681	API MANUFACTURE

Revised: 03/2010Rouses Point Pharm

More Hydrocortisone Butyrate Solution resources

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• Hydrocortisone Butyrate Solution Drug Interactions
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• 15 Reviews for Hydrocortisone Butyrate - Add your own review/rating

Compare Hydrocortisone Butyrate Solution with other medications

• Anal Itching
• Aphthous Stomatitis, Recurrent
• Atopic Dermatitis
• Dermatitis
• Eczema
• Gingivitis
• Hemorrhoids
• Proctitis
• Pruritus
• Psoriasis
• Seborrheic Dermatitis
• Skin Rash
• Ulcerative Colitis, Active

Salflex

Generic Name: salicylate (Oral route, Rectal route)

Commonly used brand name(s)

In the U.S.

• Amigesic


• Asacol


• Azulfidine


• Azulfidine Entabs


• Bayer


• Canasa


• Colazal


• Dipentum


• Doan's Extra Strength


• Doan's Regular


• Dolobid


• Ecotrin


• Kaopectate


• Pepto Bismol


• Salflex


• Tricosal


• Trilisate

In Canada

• Alti-Sulfasalazine


• Arthropan


• Asacol 800


• Bismuth Extra Strength


• Bismuth Original Formula


• Mesasal


• Pentasa


• Pepto-Bismol


• Pms-Asa Suppository Adult


• Pms-Asa Suppository Children


• Salazopyrin


• Salofalk

Available Dosage Forms:

• Tablet, Enteric Coated


• Tablet, Extended Release


• Suppository


• Tablet


• Capsule


• Tablet, Chewable


• Tablet, Effervescent


• Capsule, Delayed Release


• Gum


• Tablet, Delayed Release


• Enema


• Capsule, Extended Release


• Liquid


• Solution


• Suspension

Uses For Salflex

Aspirin may also be used to lessen the chance of heart attack, stroke, or other problems that may occur when a blood vessel is blocked by blood clots. Aspirin helps prevent dangerous blood clots from forming. However, this effect of aspirin may increase the chance of serious bleeding in some people. Therefore, aspirin should be used for this purpose only when your doctor decides, after studying your medical condition and history, that the danger of blood clots is greater than the risk of bleeding. Do not take aspirin to prevent blood clots or a heart attack unless it has been ordered by your doctor.

Salicylates may also be used for other conditions as determined by your doctor.

The caffeine present in some of these products may provide additional relief of headache pain or faster pain relief.

Some salicylates are available only with your medical doctor's or dentist's prescription. Others are available without a prescription; however, your medical doctor or dentist may have special instructions on the proper dose of these medicines for your medical condition.

Importance of Diet

Make certain your health care professional knows if you are on a low-sodium diet. Regular use of large amounts of sodium salicylate (as for arthritis) can add a large amount of sodium to your diet. Sodium salicylate contains 46 mg of sodium in each 325-mg tablet and 92 mg of sodium in each 650-mg tablet.

Before Using Salflex

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to medicines in this group or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Do not give aspirin or other salicylates to a child or a teenager with a fever or other symptoms of a virus infection, especially flu or chickenpox, without first discussing its use with your child's doctor. This is very important because salicylates may cause a serious illness called Reye's syndrome in children and teenagers with fever caused by a virus infection, especially flu or chickenpox.

Some children may need to take aspirin or another salicylate regularly (as for arthritis). However, your child's doctor may want to stop the medicine for a while if a fever or other symptoms of a virus infection occur. Discuss this with your child's doctor, so that you will know ahead of time what to do if your child gets sick.

Children who do not have a virus infection may also be more sensitive to the effects of salicylates, especially if they have a fever or have lost large amounts of body fluid because of vomiting, diarrhea, or sweating. This may increase the chance of side effects during treatment.

Geriatric

Elderly people are especially sensitive to the effects of salicylates. This may increase the chance of side effects during treatment.

Pregnancy

Salicylates have not been shown to cause birth defects in humans. Studies on birth defects in humans have been done with aspirin but not with other salicylates. However, salicylates caused birth defects in animal studies.

Some reports have suggested that too much use of aspirin late in pregnancy may cause a decrease in the newborn's weight and possible death of the fetus or newborn infant. However, the mothers in these reports had been taking much larger amounts of aspirin than are usually recommended. Studies of mothers taking aspirin in the doses that are usually recommended did not show these unwanted effects. However, there is a chance that regular use of salicylates late in pregnancy may cause unwanted effects on the heart or blood flow in the fetus or in the newborn infant.

Use of salicylates, especially aspirin, during the last 2 weeks of pregnancy may cause bleeding problems in the fetus before or during delivery or in the newborn infant. Also, too much use of salicylates during the last 3 months of pregnancy may increase the length of pregnancy, prolong labor, cause other problems during delivery, or cause severe bleeding in the mother before, during, or after delivery. Do not take aspirin during the last 3 months of pregnancy unless it has been ordered by your doctor.

Studies in humans have not shown that caffeine (present in some aspirin products) causes birth defects. However, studies in animals have shown that caffeine causes birth defects when given in very large doses (amounts equal to those present in 12 to 24 cups of coffee a day).

Breast Feeding

Salicylates pass into the breast milk. Although salicylates have not been reported to cause problems in nursing babies, it is possible that problems may occur if large amounts are taken regularly, as for arthritis (rheumatism).

Caffeine passes into the breast milk in small amounts.

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking any of these medicines, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using medicines in this class with any of the following medicines is not recommended. Your doctor may decide not to treat you with a medication in this class or change some of the other medicines you take.

• Influenza Virus Vaccine, Live


• Ketorolac


• Pentoxifylline

Using medicines in this class with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Abciximab


• Acenocoumarol


• Alteplase, Recombinant


• Anisindione


• Ardeparin


• Argatroban


• Beta Glucan


• Bivalirudin


• Certoparin


• Cilostazol


• Citalopram


• Clopidogrel


• Clovoxamine


• Dabigatran Etexilate


• Dalteparin


• Danaparoid


• Desirudin


• Desvenlafaxine


• Dicumarol


• Dipyridamole


• Duloxetine


• Enoxaparin


• Eptifibatide


• Escitalopram


• Femoxetine


• Flesinoxan


• Fluoxetine


• Fluvoxamine


• Fondaparinux


• Ginkgo


• Heparin


• Ketoprofen


• Lepirudin


• Methotrexate


• Milnacipran


• Nadroparin


• Naproxen


• Nefazodone


• Parnaparin


• Paroxetine


• Pemetrexed


• Phenindione


• Phenprocoumon


• Protein C


• Reteplase, Recombinant


• Reviparin


• Riluzole


• Rivaroxaban


• Sertraline


• Sibutramine


• Tacrolimus


• Ticlopidine


• Tinzaparin


• Tirofiban


• Varicella Virus Vaccine


• Venlafaxine


• Vilazodone


• Warfarin


• Zimeldine

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Other Medical Problems

The presence of other medical problems may affect the use of medicines in this class. Make sure you tell your doctor if you have any other medical problems, especially:

• Anemia or


• Overactive thyroid or


• Stomach ulcer or other stomach problems—Salicylates may make your condition worse.

• Asthma, allergies, and nasal polyps (history of) or


• Glucose-6-phosphate dehydrogenase (G6PD) deficiency or


• High blood pressure (hypertension) or


• Kidney disease or


• Liver disease—The chance of side effects may be increased.

• Gout—Salicylates can make this condition worse and can also lessen the effects of some medicines used to treat gout.

• Heart disease—The chance of some side effects may be increased. Also, the caffeine present in some aspirin products can make some kinds of heart disease worse.

• Hemophilia or other bleeding problems—The chance of bleeding may be increased, especially with aspirin.

Proper Use of salicylate

This section provides information on the proper use of a number of products that contain salicylate. It may not be specific to Salflex. Please read with care.

Take this medicine after meals or with food (except for enteric-coated capsules or tablets and aspirin suppositories) to lessen stomach irritation.

Take tablet or capsule forms of this medicine with a full glass (8 ounces) of water. Also, do not lie down for about 15 to 30 minutes after swallowing the medicine. This helps to prevent irritation that may lead to trouble in swallowing.

For patients taking aspirin (including buffered aspirin and/or products containing caffeine):

• Do not use any product that contains aspirin if it has a strong, vinegar-like odor. This odor means the medicine is breaking down. If you have any questions about this, check with your health care professional.


• If you are to take any medicine that contains aspirin within 7 days after having your tonsils removed, a tooth pulled, or other dental or mouth surgery, be sure to swallow the aspirin whole. Do not chew aspirin during this time.


• Do not place any medicine that contains aspirin directly on a tooth or gum surface. This may cause a burn.


• There are several different forms of aspirin or buffered aspirin tablets. If you are using:
  
  • chewable aspirin tablets, they may be chewed, dissolved in liquid, crushed, or swallowed whole.
  
  
  • delayed-release (enteric-coated) aspirin tablets, they must be swallowed whole. Do not crush them or break them up before taking.
  
  
  • extended-release (long-acting) aspirin tablets, check with your pharmacist as to how they should be taken. Some may be broken up (but must not be crushed) before swallowing if you cannot swallow them whole. Others should not be broken up and must be swallowed whole.
  
  

To use aspirin suppositories:

• If the suppository is too soft to insert, chill it in the refrigerator for 30 minutes or run cold water over it before removing the foil wrapper.


• To insert the suppository: First remove the foil wrapper and moisten the suppository with cold water. Lie down on your side and use your finger to push the suppository well up into the rectum.

To take choline and magnesium salicylates (e.g., Trilisate) oral solution:

• The liquid may be mixed with fruit juice just before taking.


• Drink a full glass (8 ounces) of water after taking the medicine.

To take enteric-coated sodium salicylate tablets:

• The tablets must be swallowed whole. Do not crush them or break them up before taking.

Unless otherwise directed by your medical doctor or dentist:

• Do not take more of this medicine than recommended on the label, to lessen the chance of side effects.


• Children up to 12 years of age should not take this medicine more than 5 times a day.

When used for arthritis (rheumatism), this medicine must be taken regularly as ordered by your doctor in order for it to help you. Up to 2 to 3 weeks or longer may pass before you feel the full effects of this medicine.

Dosing

The dose medicines in this class will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of these medicines. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

• For aspirin


• For oral dosage forms (short-acting tablets, chewable tablets, and delayed-release [enteric-coated] tablets):
  
  • For pain or fever:
    
    • Adults and teenagers—325 to 500 milligrams (mg) every three or four hours, 650 mg every four to six hours, or 1000 mg every six hours as needed.
    
    
    • Children 11 to 12 years of age—320 to 480 mg every four hours as needed.
    
    
    • Children 9 to 11 years of age—320 to 400 mg every four hours as needed.
    
    
    • Children 6 to 9 years of age—320 to 325 mg every four hours as needed.
    
    
    • Children 4 to 6 years of age—240 mg every four hours as needed.
    
    
    • Children 2 to 4 years of age—160 mg every four hours as needed.
    
    
    • Children up to 2 years of age—Dose must be determined by your doctor.
    
    
  
  
  • For arthritis:
    
    • Adults and teenagers—A total of 3600 to 5400 mg a day, divided into several smaller doses.
    
    
    • Children—A total of 80 to 100 mg per kilogram (kg) (32 to 40 mg per pound) of body weight a day, divided into several smaller doses.
    
    
  
  
  • For preventing a heart attack, stroke, or other problems caused by blood clots:
    
    • Adults—Most people will take 81, 162.5, or 325 mg a day or 325 mg every other day. Some people taking aspirin to prevent a stroke may need as much as 1000 mg a day.
    
    
    • Children—Use and dose must be determined by your doctor.
    
    
  
  


• For oral dosage form (chewing gum):
  
  • For pain:
    
    • Adults and teenagers—2 tablets every four hours as needed.
    
    
    • Children 6 to 12 years of age—1 or 2 tablets (227 mg each) up to four times a day.
    
    
    • Children 3 to 6 years of age—1 tablet (227 mg) up to three times a day.
    
    
    • Children up to 3 years of age—Dose must be determined by your doctor.
    
    
  
  


• For long-acting oral dosage form (extended-release tablets):
  
  • For pain:
    
    • Adults and teenagers—1 or 2 tablets twice a day.
    
    
    • Children—The long-acting aspirin tablets are too strong for use in children.
    
    
  
  
  • For arthritis:
    
    • Adults and teenagers—1 or 2 tablets twice a day, at first. Your doctor will then adjust your dose as needed.
    
    
    • Children—The long-acting aspirin tablets are too strong for use in children.
    
    
  
  


• For rectal dosage form (suppositories):
  
  • For pain or fever:
    
    • Adults and teenagers—325 to 650 mg every four hours as needed.
    
    
    • Children 11 to 12 years of age—325 to 480 mg every four hours as needed.
    
    
    • Children 9 to 11 years of age—325 to 400 mg every four hours as needed.
    
    
    • Children 6 to 9 years of age—325 mg every four hours as needed.
    
    
    • Children 4 to 6 years of age—240 mg every four hours as needed.
    
    
    • Children 2 to 4 years of age—160 mg every four hours as needed.
    
    
    • Children up to 2 years of age—Dose must be determined by your doctor.
    
    
  
  
  • For arthritis:
    
    • Adults and teenagers—A total of 3600 to 5400 mg a day, divided into several smaller doses.
    
    
    • Children—A total of 80 to 100 mg per kilogram (kg) (32 to 40 mg per pound) of body weight a day, divided into several smaller doses.
    
    
  
  

• For aspirin and caffeine


• For oral dosage forms (capsule):
  
  • For pain or fever:
    
    • Adults and teenagers—325 to 500 milligrams (mg) of aspirin every three or four hours, 650 mg of aspirin every four to six hours, or 1000 mg of aspirin every six hours as needed.
    
    
    • Children 9 to 12 years of age—325 to 400 mg every four hours as needed.
    
    
    • Children 6 to 9 years of age—325 mg every four hours as needed.
    
    
    • Children up to 6 years of age—Aspirin and caffeine capsules are too strong for use in children up to 6 years of age
    
    
  
  
  • For preventing a heart attack, stroke, or other problems caused by blood clots:
    
    • Adults—325 mg a day or every other day. People who take smaller doses of aspirin will have to use a different product. Some people taking aspirin to prevent a stroke may need as much as 1000 mg a day.
    
    
    • Children—Use and dose must be determined by your doctor.
    
    
  
  


• For oral dosage form (tablets):
  
  • For pain or fever:
    
    • Adults and teenagers—325 to 500 mg of aspirin every three or four hours, 650 mg of aspirin every four to six hours, or 1000 mg of aspirin every six hours as needed.
    
    
    • Children 9 to 12 years of age—325 to 400 mg every four hours as needed.
    
    
    • Children up to 9 years of age—Aspirin and caffeine tablets are too strong for use in children up to 9 years of age.
    
    
  
  
  • For arthritis:
    
    • Adults and teenagers—A total of 3600 to 5400 mg of aspirin a day, divided into several smaller doses.
    
    
    • Children—A total of 80 to 100 mg per kg (32 to 40 mg per pound) of body weight a day, divided into several smaller doses.
    
    
  
  
  • For preventing a heart attack, stroke, or other problems caused by blood clots:
    
    • Adults—325 mg a day or every other day. People who take smaller doses of aspirin will have to use a different product. Some people taking aspirin to prevent a stroke may need as much as 1000 mg a day.
    
    
    • Children—Use and dose must be determined by your doctor.
    
    
  
  

• For buffered aspirin


• For oral dosage forms (tablets):
  
  • For pain or fever:
    
    • Adults and teenagers—325 to 500 milligrams (mg) of aspirin every three or four hours, 650 mg of aspirin every four to six hours, or 1000 mg of aspirin every six hours as needed.
    
    
    • Children 11 to 12 years of age—One or one and one-half 325-mg tablets every four hours as needed.
    
    
    • Children 9 to 11 years of age—One or one and one-fourth 325-mg tablets every four hours as needed.
    
    
    • Children 6 to 9 years of age—One 325-mg tablet every four hours as needed.
    
    
    • Children 4 to 6 years of age—Three-fourths of a 325-mg tablet every four hours as needed.
    
    
    • Children 2 to 4 years of age—One-half of a 325-mg tablet every four hours as needed.
    
    
    • Children up to 2 years of age—Dose must be determined by your doctor.
    
    
  
  
  • For arthritis:
    
    • Adults and teenagers—A total of 3600 to 5400 mg of aspirin a day, divided into several smaller doses.
    
    
    • Children—A total of 80 to 100 mg per kilogram (kg) (32 to 40 mg per pound) of body weight a day, divided into several smaller doses.
    
    
  
  
  • For preventing a heart attack, stroke, or other problems caused by blood clots:
    
    • Adults—325 mg a day or every other day. People who take smaller doses of aspirin will have to use a different product. Some people taking aspirin to prevent a stroke may need as much as 1000 mg a day.
    
    
    • Children—Use and dose must be determined by your doctor.
    
    
  
  

• For buffered aspirin and caffeine


• For oral dosage form (tablets):
  
  • For pain or fever:
    
    • Adults and teenagers—325 or 421 milligrams (mg) of aspirin every three or four hours, 650 mg of aspirin every four to six hours, or 842 mg of aspirin every six hours as needed.
    
    
    • Children 11 to 12 years of age—One or one and one-half 325-mg tablets, or one 421-mg tablet, every four hours as needed.
    
    
    • Children 9 to 11 years of age—One or one and one-fourth 325-mg tablets every four hours as needed.
    
    
    • Children 6 to 9 years of age—One 325-mg or 421-mg tablet every four hours as needed.
    
    
    • Children 4 to 6 years of age—Three-fourths of a 325-mg tablet every four hours as needed.
    
    
    • Children 2 to 4 years of age—One-half of a 325-mg tablet every four hours as needed.
    
    
    • Children up to 2 years of age—Dose must be determined by your doctor.
    
    
  
  
  • For arthritis:
    
    • Adults and teenagers—A total of 3600 to 5400 mg of aspirin a day, divided into several smaller doses.
    
    
    • Children—A total of 80 to 100 mg per kilogram (kg) (32 to 40 mg per pound) of body weight a day, divided into several smaller doses.
    
    
  
  
  • For preventing a heart attack, stroke, or other problems caused by blood clots:
    
    • Adults—162.5 or 325 mg (one-half or one 325-mg tablet) a day or 325 mg every other day. People who need smaller doses of aspirin will have to use a different product. Some people taking aspirin to prevent a stroke may need as much as 1000 mg a day.
    
    
    • Children—Use and dose must be determined by your doctor.
    
    
  
  

• For choline salicylate


• For oral dosage form (oral solution):
  
  • For pain or fever:
    
    • Adults and teenagers—One-half or three-fourths of a teaspoonful every three hours, one-half or one teaspoonful every four hours, or one or one and one-half teaspoonfuls every six hours as needed.
    
    
    • Children 11 to 12 years of age—2.5 to 3.75 mL (one-half to three-fourths of a teaspoonful) every four hours as needed. This amount should be measured by a special measuring spoon.
    
    
    • Children 6 to 11 years of age—2.5 mL (one-half of a teaspoonful) every four hours as needed. This amount should be measured by a special measuring spoon.
    
    
    • Children 4 to 6 years of age—1.66 mL every four hours as needed. This amount should be measured by a special dropper or measuring spoon.
    
    
    • Children 2 to 4 years of age—1.25 milliliters (mL) (one-fourth of a teaspoonful) every four hours as needed. This amount should be measured by a special dropper or measuring spoon.
    
    
    • Children up to 2 years of age—Dose must be determined by your doctor.
    
    
  
  
  • For arthritis:
    
    • Adults—A total of five and one-half to eight teaspoonfuls a day, divided into several smaller doses.
    
    
    • Children—A total of 0.6 to 0.7 mL per kilogram (kg) (0.25 to 0.28 mL per pound) of body weight a day, divided into several smaller doses.
    
    
  
  

• For choline and magnesium salicylates


• For oral dosage forms (oral solution or tablets):
  
  • For pain or fever:
    
    • Adults and teenagers—A total of 2000 to 3000 milligrams (mg) a day, divided into two or three doses.
    
    
    • Children weighing more than 37 kg (90 pounds or more)—2200 mg a day, divided into two doses.
    
    
    • Children weighing up to 37 kilograms (kg) (about 89 pounds)—A total of 50 mg per kg (20 mg per pound) of body weight a day, divided into two doses.
    
    
  
  

• For magnesium salicylate


• For oral dosage form (tablets):
  
  • For pain:
    
    • Adults and teenagers—2 regular-strength tablets every four hours, up to a maximum of 12 tablets a day, or 2 extra-strength tablets every eight hours, up to a maximum of 8 tablets a day.
    
    
    • Children—Dose must be determined by your doctor.
    
    
  
  

• For salsalate


• For oral dosage forms (capsules or tablets):
  
  • For arthritis:
    
    • Adults and teenagers—500 to 1000 milligrams (mg) two or three times a day, to start. Your doctor will then adjust your dose as needed.
    
    
    • Children—Dose must be determined by your doctor.
    
    
  
  

• For sodium salicylate


• For oral dosage forms (tablets or delayed-release [enteric-coated] tablets):
  
  • For pain or fever:
    
    • Adults and teenagers—325 or 650 milligrams (mg) every four hours as needed.
    
    
    • Children 6 years of age and older—325 mg every four hours as needed.
    
    
    • Children up to 6 years of age—This medicine is too strong for use in children younger than 6 years of age.
    
    
  
  
  • For arthritis:
    
    • Adults and teenagers—A total of 3600 to 5400 mg a day, divided into several smaller doses.
    
    
    • Children—A total of 80 to 100 mg per kilogram (kg) (32 to 40 mg per pound) of body weight a day, divided into several smaller doses.
    
    
  
  

Missed Dose

If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage

Keep out of the reach of children.

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Do not keep outdated medicine or medicine no longer needed.

Precautions While Using Salflex

Check the labels of all nonprescription (over-the-counter [OTC]) and prescription medicines you now take. If any contain aspirin or other salicylates (including bismuth subsalicylate [e.g., Pepto-Bismol] or any shampoo or skin medicine that contains salicylic acid or any other salicylate), check with your health care professional. Taking or using them together with this medicine may cause an overdose.

If you will be taking salicylates for a long time (more than 5 days in a row for children or 10 days in a row for adults) or in large amounts, your doctor should check your progress at regular visits.

Serious side effects can occur during treatment with this medicine. Sometimes serious side effects can occur without any warning. However, possible warning signs often occur, including swelling of the face, fingers, feet, and/or lower legs; severe stomach pain, black, tarry stools, and/or vomiting of blood or material that looks like coffee grounds; unusual weight gain; and/or skin rash. Also, signs of serious heart problems could occur such as chest pain, tightness in chest, fast or irregular heartbeat, or unusual flushing or warmth of skin. Stop taking this medicine and check with your doctor immediately if you notice any of these warning signs.

Check with your medical doctor or dentist:

• If you are taking this medicine to relieve pain and the pain lasts for more than 10 days (5 days for children) or if the pain gets worse, if new symptoms occur, or if redness or swelling is present. These could be signs of a serious condition that needs medical or dental treatment.


• If you are taking this medicine to bring down a fever, and the fever lasts for more than 3 days or returns, if the fever gets worse, if new symptoms occur, or if redness or swelling is present. These could be signs of a serious condition that needs treatment.


• If you are taking this medicine for a sore throat, and the sore throat is very painful, lasts for more than 2 days, or occurs together with or is followed by fever, headache, skin rash, nausea, or vomiting.


• If you are taking this medicine regularly, as for arthritis (rheumatism), and you notice a ringing or buzzing in your ears or severe or continuing headaches. These are often the first signs that too much salicylate is being taken. Your doctor may want to change the amount of medicine you are taking every day.

For patients taking aspirin to lessen the chance of heart attack, stroke, or other problems caused by blood clots:

• Take only the amount of aspirin ordered by your doctor. If you need a medicine to relieve pain, a fever, or arthritis, your doctor may not want you to take extra aspirin. It is a good idea to discuss this with your doctor, so that you will know ahead of time what medicine to take.


• Do not stop taking this medicine for any reason without first checking with the doctor who directed you to take it.

Taking certain other medicines together with a salicylate may increase the chance of unwanted effects. The risk will depend on how much of each medicine you take every day, and on how long you take the medicines together. If your doctor directs you to take these medicines together on a regular basis, follow his or her directions carefully. However, do not take any of the following medicines together with a salicylate for more than a few days, unless your doctor has directed you to do so and is following your progress:

• Acetaminophen (e.g., Tylenol)


• Diclofenac (e.g., Voltaren)


• Diflunisal (e.g., Dolobid)


• Etodolac (e.g., Lodine)


• Fenoprofen (e.g., Nalfon)


• Floctafenine (e.g., Idarac)


• Flurbiprofen, oral (e.g., Ansaid)


• Ibuprofen (e.g., Motrin)


• Indomethacin (e.g., Indocin)


• Ketoprofen (e.g., Orudis)


• Ketorolac (e.g., Toradol)


• Meclofenamate (e.g., Meclomen)


• Mefenamic acid (e.g., Ponstel)


• Nabumetone (e.g., Relafen)


• Naproxen (e.g., Naprosyn)


• Oxaprozin (e.g., Daypro)


• Phenylbutazone (e.g., Butazolidin)


• Piroxicam (e.g., Feldene)


• Sulindac (e.g., Clinoril)


• Tenoxicam (e.g., Mobiflex)


• Tiaprofenic acid (e.g., Surgam)


• Tolmetin (e.g., Tolectin)

For diabetic patients:

• False urine sugar test results may occur if you are regularly taking large amounts of salicylates, such as:
  
  • Aspirin: 8 or more 325-mg (5-grain), or 4 or more 500-mg or 650-mg (10-grain), or 3 or more 800-mg (or higher strength), doses a day.
  
  
  • Buffered aspirin or
  
  
  • Sodium salicylate: 8 or more 325-mg (5-grain), or 4 or more 500-mg or 650-mg (10-grain), doses a day.
  
  
  • Choline salicylate: 4 or more teaspoonfuls (each teaspoonful containing 870 mg) a day.
  
  
  • Choline and magnesium salicylates: 5 or more 500-mg tablets or teaspoonfuls, 4 or more 750-mg tablets, or 2 or more 1000-mg tablets, a day.
  
  
  • Magnesium salicylate: 7 or more regular-strength, or 4 or more extra-strength, tablets a day.
  
  
  • Salsalate: 4 or more 500-mg doses, or 3 or more 750-mg doses, a day.
  
  


• Smaller doses or occasional use of salicylates usually will not affect urine sugar tests. However, check with your health care professional (especially if your diabetes is not well-controlled) if:
  
  • you are not sure how much salicylate you are taking every day.
  
  
  • you notice any change in your urine sugar test results.
  
  
  • you have any other questions about this possible problem.
  
  

Do not take aspirin for 5 days before any surgery, including dental surgery, unless otherwise directed by your medical doctor or dentist. Taking aspirin during this time may cause bleeding problems.

For patients taking buffered aspirin, choline and magnesium salicylates (e.g., Trilisate), or magnesium salicylate (e.g., Doan's):

• Buffered aspirin, choline and magnesium salicylates, or magnesium salicylate can keep many other medicines, especially some medicines used to treat infections, from working properly. This problem can be prevented by not taking the 2 medicines too close together. Ask your health care professional how long you should wait between taking a medicine for infection and taking buffered aspirin, choline and magnesium salicylates, or magnesium salicylate.

If you are taking a laxative containing cellulose, take the salicylate at least 2 hours before or after you take the laxative. Taking these medicines too close together may lessen the effects of the salicylate.

For patients taking this medicine by mouth:

• Stomach problems may be more likely to occur if you drink alcoholic beverages while being treated with this medicine, especially if you are taking it in high doses or for a long time. Check with your doctor if you have any questions about this.

For patients using aspirin suppositories:

• Aspirin suppositories may cause irritation of the rectum. Check with your doctor if this occurs.

Salicylates may interfere with the results of some medical tests. Before you have any medical tests, tell the doctor in charge if you have taken any of these medicines within the past week. If possible, it is best to check with the doctor first, to find out whether the medicine may be taken during the week before the test.

For patients taking one of the products that contain caffeine:

• Caffeine may interfere with the result of a test that uses adenosine (e.g., Adenocard) or dipyridamole (e.g., Persantine) to help find out how well your blood is flowing through certain blood vessels. Therefore, you should not have any caffeine for at least 8 to 12 hours before the test.

If you think that you or anyone else may have taken an overdose, get emergency help at once. Taking an overdose of these medicines may cause unconsciousness or death. Signs of overdose include convulsions (seizures), hearing loss, confusion, ringing or buzzing in the ears, severe drowsiness or tiredness, severe excitement or nervousness, and fast or deep breathing.

Salflex Side Effects

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Get emergency help immediately if any of the following side effects occur:

Symptoms of overdose in children

• Changes in behavior


• drowsiness or tiredness (severe)


• fast or deep breathing

• Any loss of hearing


• bloody urine


• confusion


• convulsions (seizures)


• diarrhea (severe or continuing)


• difficulty in swallowing


• dizziness, lightheadedness, or feeling faint (severe)


• drowsiness (severe)


• excitement or nervousness (severe)


• fast or deep breathing


• flushing, redness, or other change in skin color


• hallucinations (seeing, hearing, or feeling things that are not there)


• increased sweating


• increased thirst


• nausea or vomiting (severe or continuing)


• shortness of breath, troubled breathing, tightness in chest, or wheezing


• stomach pain (severe or continuing)


• swelling of eyelids, face, or lips


• unexplained fever


• uncontrollable flapping movements of the hands (especially in elderly patients)


• vision problems

Check with your doctor as soon as possible if any of the following side effects occur:

Less common or rare

• Abdominal or stomach pain, cramping, or burning (severe)


• bloody or black, tarry stools


• headache (severe or continuing)


• ringing or buzzing in ears (continuing)


• skin rash, hives, or itching


• unusual tiredness or weakness


• vomiting of blood or material that looks like coffee grounds

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

• Abdominal or stomach cramps, pain, or discomfort (mild to moderate)


• heartburn or indigestion


• nausea or vomiting

Less common

• Trouble in sleeping, nervousness, or jitters (only for products containing caffeine)

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

The information contained in the Thomson Reuters Micromedex products as delivered by Drugs.com is intended as an educational aid only. It is not intended as medical advice for individual conditions or treatment. It is not a substitute for a medical exam, nor does it replace the need for services provided by medical professionals. Talk to your doctor, nurse or pharmacist before taking any prescription or over the counter drugs (including any herbal medicines or supplements) or following any treatment or regimen. Only your doctor, nurse, or pharmacist can provide you with advice on what is safe and effective for you.

The use of the Thomson Reuters Healthcare products is at your sole risk. These products are provided "AS IS" and "as available" for use, without warranties of any kind, either express or implied. Thomson Reuters Healthcare and Drugs.com make no representation or warranty as to the accuracy, reliability, timeliness, usefulness or completeness of any of the information contained in the products. Additionally, THOMSON REUTERS HEALTHCARE MAKES NO REPRESENTATION OR WARRANTIES AS TO THE OPINIONS OR OTHER SERVICE OR DATA YOU MAY ACCESS, DOWNLOAD OR USE AS A RESULT OF USE OF THE THOMSON REUTERS HEALTHCARE PRODUCTS. ALL IMPLIED WARRANTIES OF MERCHANTABILITY AND FITNESS FOR A PARTICULAR PURPOSE OR USE ARE HEREBY EXCLUDED. Thomson Reuters Healthcare does not assume any responsibility or risk for your use of the Thomson Reuters Healthcare products.

Febuxostat

Class: Antigout Agents
VA Class: MS400
Chemical Name: 2-[3-cyano-4-(2-methylpropoxy) phenyl]-4-methylthiazole-5-carboxylic acid
Molecular Formula: C₁₆H₁₆N₂O₃S
CAS Number: 144060-53-7
Brands: Uloric

Introduction

Xanthine oxidase inhibitor.^{1 2 3 4 5 6 8}

Uses for Febuxostat

Gout

Long-term management of hyperuricemia in patients with gout.^{1 2 3 4 5 6 7}

Goal in management of gout is reduction in serum urate concentrations to levels below the limit of urate solubility (about 6.8 mg/dL).^{2 4}

Not recommended for the management of asymptomatic hyperuricemia.¹

Febuxostat Dosage and Administration

General

• 
  

  Acute gout attacks (gout flare) may occur after initiation of febuxostat.¹ Consider gout flare prophylaxis with an NSAIA or colchicine; start these agents when febuxostat therapy is initiated.¹ Gout flare prophylaxis may be beneficial for up to 6 months.¹ During these acute attacks, continue febuxostat and manage the gout flare as appropriate.¹

  
  


• 
  

  Testing for target serum urate concentrations can be performed after 2 weeks of febuxostat therapy.¹

  
  

Administration

Oral Administration

Administered orally without regard to meals or antacids.^{1 10}

Dosage

Adults

Gout

Oral

Initial dosage is 40 mg once daily.¹ Increase dosage to 80 mg once daily in patients who do not achieve serum urate concentrations of <6 mg/dL after 2 weeks of therapy with febuxostat 40 mg once daily.¹

Special Populations

Dosage adjustment is not needed in patients with mild to moderate renal or hepatic impairment.^{1 8}

Cautions for Febuxostat

Contraindications

• 
  

  Concomitant therapy with azathioprine, mercaptopurine, or theophylline.¹ (See Interactions.)

  
  

Warnings/Precautions

Acute Gout

Febuxostat initiation may increase frequency of acute gout attacks (gout flare).¹ Consider gout flare prophylaxis with an NSAIA or colchicine; start these agents when febuxostat therapy is initiated.¹

Cardiovascular Events

Higher rate of cardiovascular thromboembolic events (cardiovascular deaths, nonfatal MI, nonfatal stroke) in patients receiving febuxostat than in patients receiving allopurinol.¹ Causal relationship not established.¹ Monitor for signs and symptoms of MI and stroke.¹

Hepatic Effects

Elevations of serum transaminase concentrations reported.¹ Perform liver function tests during therapy (e.g., at month 2 and 4 of therapy and then periodically).¹

Specific Populations

Pregnancy

Category C.¹

Lactation

Distributed into milk in rats; not known whether distributed into human milk.¹ Use with caution in nursing women.¹

Pediatric Use

Safety and efficacy have not been established in pediatric patients <18 years of age.¹

Geriatric Use

No substantial differences in safety and efficacy relative to younger adults, but increased sensitivity of some older patients cannot be ruled out.¹

Dosage adjustment based on age not needed.^{1 3}

Hepatic Impairment

Not studied in patients with severe hepatic impairment (Child-Pugh class C); caution if used in these individuals.¹ Dosage adjustment not needed in patients with mild to moderate hepatic impairment (Child-Pugh class A or B).^{1 8}

Renal Impairment

Insufficient date in patients with severe renal impairment (Cl_cr <30 mL/minute); caution if used in these individuals.¹ Dosage adjustment not needed in patients with mild to moderate renal impairment (Cl_cr 30–89 mL/minute).¹

Not studied in individuals with end-stage renal disease who are undergoing dialysis.¹

Secondary Hyperuricemia

Not evaluated in patients with secondary hyperuricemia.¹ Not recommended in patients whose rate of urate formation is greatly increased.¹

Common Adverse Effects

Liver function abnormalities, nausea, arthralgia, rash.¹

Interactions for Febuxostat

Febuxostat does not inhibit cytochrome P-450 (CYP) isoenzymes 1A2, 2C9, 2C19, or 3A4; febuxostat is a weak inhibitor of CYP2D6.¹ Febuxostat does not induce CYP1A2, 2B6, 2C9, 2C19, 3A4.¹

Febuxostat is metabolized by conjugation by glucuronosyltransferase (uridine diphosphoglucuronosyltransferase, UDP-glucuronate β-D-glucuronosyltransferase [acceptor-unspecific], UGT) enzymes, including UGT1A1, UGT1A3, UGT1A9, and UGT2B7, as well as by oxidation by CYP isoenzymes, including CYP1A2, 2C8, and 2C9, and non-CYP enzymes.¹ Relative contribution of each enzyme isoform to the drug's metabolism is not clear.¹

Drugs Affecting Hepatic Microsomal or Other Enzymes

Drug interactions generally are not expected between febuxostat and inhibitors or inducers of particular enzyme isoforms.¹

Drugs Metabolized by Hepatic Microsomal Enzymes

Pharmacokinetic interactions are unlikely between febuxostat and substrates of these isoenzymes.¹

Drugs Metabolized by Xanthine Oxidase

Inhibition of xanthine oxidase by febuxostat may increase plasma concentrations of drugs metabolized by the enzyme if administered concomitantly, resulting in toxicity.¹ (See Contraindications.)

Specific Drugs

Drug	Interaction	Comments
Antacids	Pharmacokinetic interaction unlikely1 10
Antineoplastic agents	Not evaluated1 Mercaptopurine: Inhibition of mercaptopurine metabolism; possible increase in toxic effects1	No information on safety of concomitant use1 Mercaptopurine: Concomitant use contraindicated1
Azathioprine	Inhibition of azathioprine metabolism; possible increase in toxic effects1	Concomitant use contraindicated1
Colchicine	Clinically important pharmacokinetic interaction unlikely1	Dosage adjustment not needed
Desipramine	Pharmacokinetic interaction not considered clinically important1	Dosage adjustment not expected to be necessary1
Hydrochlorothiazide	Clinically important pharmacokinetic interaction unlikely1	Dosage adjustment not needed
Indomethacin	Clinically important pharmacokinetic interaction unlikely1	Dosage adjustment not needed
Naproxen	Clinically important pharmacokinetic interaction unlikely1	Dosage adjustment not needed
Theophylline	Inhibition of theophylline metabolism; possible increase in toxic effects1	Concomitant use contraindicated1
Warfarin	Pharmacokinetic interaction unlikely1	Dosage adjustment not needed

Febuxostat Pharmacokinetics

Absorption

Bioavailability

Peak plasma concentrations of febuxostat are reached in 1–1.5 hours.^{1 3}

Food

Administration with food decreases the rate and extent of absorption of febuxostat; not considered clinically important.^{1 10}

Distribution

Plasma Protein Binding

99.2%.¹

Elimination

Metabolism

Febuxostat is metabolized by uridine diphosphate-glucuronosyltransferase (UGT) 1A1, 1A3, 1A9, 2B7, CYP 1A2, 2C8, 2C9, and other enzymes.¹

Elimination Route

Excreted in urine (49%) and feces (45%), principally as metabolites.¹

Half-life

5–8 hours.¹

Special Populations

Pharmacokinetic values in geriatric adults similar to those in younger adults.^{1 3}

Extent of absorption and half-life increased in individuals with renal impairment; not considered clinically important.¹

Extent of absorption increased in individuals with mild to moderate hepatic impairment; not considered clinically important.^{1 8}

Stability

Storage

Oral

Tablets

25°C (may be exposed to 15–30°C).¹

ActionsActions

• 
  

  Febuxostat inhibits xanthine oxidase, the enzyme that catalyzes the conversion of hypoxanthine to xanthine and xanthine to uric acid.^{1 3} By blocking uric acid production, febuxostat decreases serum concentrations of uric acid.^{1 2 3}

  
  


• 
  

  Febuxostat has minimal effects on other enzymes involved in purine and pyrimidine synthesis and metabolism.^{1 2}

  
  

Advice to Patients

• 
  

  Possibility of gout flares, liver function abnormalities, and cardiovascular events.¹

  
  


• 
  

  Importance of informing clinician of rash, chest pain, shortness of breath, or symptoms suggestive of stroke.¹

  
  


• 
  

  Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs and herbal products and any concomitant illnesses.¹

  
  


• 
  

  Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.¹

  
  


• 
  

  Importance of advising patients of other important precautionary information.¹ (See Cautions.)

  
  

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Febuxostat

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Oral	Tablets	40 mg	Uloric	Takeda
		80 mg	Uloric	Takeda

Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.

The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions February 2010. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

1. Takeda Pharmaceuticals America. Uloric (febuxostat) tablets prescribing information. Deerfield, Il; 2009 Feb.

2. Becker MA, Schumacher HR, Wortmann RL et al. Febuxostat compared with allopurinol in patients with hyperuricemia and gout. N Engl J Med. 2005; 353:2450-61. [PubMed 16339094]

3. Khosravan R, Kukulka MJ, Wu J-T et al. The effect of age and gender on pharmacokinetics, pharmacodynamics, and safety of febuxostat, a novel nonpurine selective inhibitor of xanthine oxidase. J Clin Pharmacol. 2008; 48:1014-24. [PubMed 18635756]

4. Schumacher HR, Becker MA, Wortmann RL et al. Effects of febuxostat versus allopurinol and placebo in reducing serum urate in subjects with hyperuricemia and gout: a 28-week, phase III, randomized, double-blind, parallel-group trial. Arthritis Rheum. 2008; 59:1540-8. [PubMed 18975369]

5. Becker MA, Schumacher HR, MacDonald PA et al. Clinical efficacy and safety of successful longterm urate lowering with febuxostat or allopurinol in subjects with gout. J Rheumatol. 2009; 36:1273-82. [PubMed 19286847]

6. Anon. Febuxostat (Uloric) for chronic treatment of gout. Med Lett Drugs Ther. 2009; 51:37-8.

7. Becker M, Schumacher HR, Espinoza L et al. A phase 3 randomized, controlled, multicenter, double-blind trial (RCT) comparing efficacy and safety of daily febuxostat (FEB) and allopurinol (ALLO) in subjects with gout. 2008 annual meeting American College of Rheumatology, San Francisco.

8. Khosravan R, Grabowski BA, Mayer MD et al. The effect of mild and moderate hepatic impairment on pharmacokinetics, pharmacodynamics, and safety of febuxostat, a novel nonpurine selective inhibitor of xanthine oxidase. J Clin Pharmacol. 2006; 46:88-102. [PubMed 16397288]

9. Khosravan R, Wu J-T, Joseph-Ridge N et al. Pharmacokinetic interactions of concomitant administration of febuxostat and NSAIDs. J Clin Pharmacol. 2006; 46:855-66. [PubMed 16855070]

10. Khosravan R, Grabowski B, Wu J-T et al. Effect of food or antacid on pharmacokinetics and pharmacodynamics of febuxostat in healthy subjects. Br J Clin Pharmacol. 2007; 65:355-63. [PubMed 17953718]

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