Bupivacaine Hydrochloride Injection BP 0.375 % w / v

1. Name Of The Medicinal Product

Bupivacaine Hydrochloride Injection B.P. 0.375 % w/v

2. Qualitative And Quantitative Composition

Solution for Injection containing 0.395 % w/v Bupivacaine Hydrochloride B.P; Ph.Eur equivalent to 0.375 % w/v anhydrous bupivacaine hydrochloride.

3. Pharmaceutical Form

Clear, colourless aqueous, sterile solution in 10 ml and 20 ml translucent plastic ampoules

4. Clinical Particulars

4.1 Therapeutic Indications

Bupivacaine Hydrochloride Injection B.P. 0.375% w/v may be used for the production of local anaesthesia by peripheral nerve block(s), or by central neural block (caudal or lumbar epidural) for analgesia in labour.

4.2 Posology And Method Of Administration

Route of Administration:

Infiltration by injection Epidural Caudal

Every precaution should be taken to avoid an accidental intravascular injection; careful aspiration is essential. For epidural anaesthesia, a test dose of 3-5 ml of bupivacaine containing adrenaline is recommended, since an intravascular injection of an adrenaline-containing solution may be recognised by an increase in heart rate. Verbal contact with the patient and repeated measurements of heart rate (ECG) should be maintained following the test dose. Aspiration should be repeated prior to administration of the main dose. The main dose should be injected slowly in incremental doses of 25 to 50 mg/minute, while keeping in constant contact with the patient. If toxic symptoms or signs of an intrathecal blockade occur, the injection should be stopped immediately.

The lowest dosage required to achieve anaesthesia should be given. However, the dosage will vary and will depend on the area to be anaesthetised, the vascularity of the tissues, the number of neuronal segments to be blocked, individual tolerance and the technique of anaesthesia used.

The maximum dosage must be determined by evaluating the size and physical status of the patient and considering the usual rate of systemic absorption from a particular injection site. Experience to date indicates a single dose of up to150mg Bupivacaine Hydrochloride. Doses of up to 50mg 2-hourly may subsequently be used. A maximum dose of 2mg/kg should not be exceeded in any four hour period and the total dose over 24 hours should not exceed 400mg.

The dosages in the following table are recommended as a guide for use in the average adult. For young, elderly or debilitated patients these doses should be reduced.

Type of Block	% Conc	Each dose	Indications	Motor block
ml	mg
Lumbar epidural	0.375	6-12	22.5-45.0	Analgesia in labour	Moderate to minimal
Caudal epidural	0.375	10-20	37.5-75.0	Analgesia in labour	Moderate
Peripheral nerves	0.375	Up to 40	Up to 150	Surgical procedures and post-operative analgesia	Moderate

Children: Not recommended

4.3 Contraindications

Bupivacaine hydrochloride solutions are contra-indicated in patients with a known hypersensitivity to local anaesthetic agents of the amide group or to other components of the injectable formulation. Solutions of bupivacaine hydrochloride are contra-indicated for intravenous regional anaesthesia (Bier's block).

Epidural anaesthesia, regardless of the local anaesthetic used, has its own contra-indications which include: Active disease of the central nervous system such as meningitis, poliomyelitis, intracranial haemorrhage, subacute combined degeneration of the cord due to pernicious anaemia, and cerebral or spinal tumors. Tuberculosis of the spine. Pyogenic infection of the skin at or adjacent to the site of lumbar puncture. Cardiogenic or hypovolaemic shock. Coagulation disoders or ongoing anticoagulant therapy. Epidural and spinal anaesthesia is contra-indicated in patients with an expanding cerebral lesion, a tumor, cyst or abscess, which may, if the intracranial pressure is suddenly altered, cause obstruction to the cerebrospinal fluid or blood circulation (the pressure cone).

4.4 Special Warnings And Precautions For Use

Before any nerve block is attempted, intravenous access for resuscitation purposes should be established. Adequate resuscitative equipment (oxygen, suction, means of intubation and appropriate emergency drugs) must be available. Epidural and spinal block techniques should only be carried out by clinicians with the necessary knowledge and experience.

There have been reports of cardiac arrest with difficult resuscitation or death during the use of bupivacaine for epidural anaesthesia in obstetrical patients. Resuscitation has been difficult or impossible despite adequate preparation and appropriate management. Cardiac arrest has occurred after convulsions resulting from systemic toxicity, presumably following inadvertent intravascular injection. Regardless of the site of injection or overdosage, inadvertent intravenous injection may give rise to toxic reactions. Injection of repeated doses of bupivacaine hydrochloride may cause significant increases in blood levels with each repeated dose due to slow accumulation of the drug. Tolerance varies with the status of the patient. Debilitated, elderly or acutely ill patients should be given reduced doses commensurate with their physical status.

Only in rare cases have amide local anaesthetics been associated with allergic reactions (with anaphylactic shock developing in most severe instances). Patients allergic to ester-type local anaesthetics such as procaine have not shown cross-sensitivity to amide-type agents such as bupivacaine.

Since bupivacaine is metabolised in the liver, it should be used cautiously in patients with liver disease or with reduced liver blood flow. Local anaesthetics should be used with caution for epidural or spinal anaesthesia in the following situations: severe shock, hypovolaemia, dehydration, hypotension below 90mm systolic or a level less than 30% of their average systolic blood pressure, gross hypertension, marked obesity, senility, cerebral atheroma, myocardial degeneration, toxaemia and severe ischaemic heart disease (especially with a history of recent infarction) because of the dangers of hypotension.

Similar caution is required in cases of impaired cardiovascular conduction, such as patients with a fixed cardiac output (severe valvular stenosis, heart block, beta-blocking therapy), resulting in decreased ability to respond to dilatation of the vascular bed or to compensate for functional changes associated with the prolongation of A-V conduction produced by local anaesthetics.

Epidural and spinal anaesthesia with any local anaesthetic can cause hypotension and bradycardia which should be anticipated and appropriate precautions taken. These may include preloading the circulation with crystalloid or colloid solution. If hypotension develops, it should be treated with posture, pressor drugs e.g. ephedrine 10-15mg intravenously in divided doses, intravenous infusions, atropine or glycopyrrolate in the presence of severe bradycardia, and oxygen. Severe hypotension may result from hypovolaemia due to haemorrhage or dehydration or aorta-caval occlusion in patients with massive ascites, large abdominal tumors or late pregnancy. Marked hypotension should be avoided in patients with cardiac decompensation.

Patients with hypovolaemia due to any cause may develop sudden and severe hypotension during epidural or spinal anaesthesia.

Epidural and spinal anaesthesia, properly performed, is generally well tolerated by obese patients and by those with obstructive lung disease. However, patients with a splinted diaphragm which interferes with breathing, such as those with hydramnios, large ovarian or uterine tumors, pregnancy, ascites or omental obesity are at risk from hypoxia due to respiratory inadequacy and aortocaval compression due to tumor mass. Lateral tilt, oxygen and mechanical ventilation should be used when indicated. Dosage should be reduced in such patients. Patients who are breathless from any cause e.g. pleural effusion, may become hypoxic, especially if the level of anaesthesia is so high as to cause paralysis of the intercostal muscles.

Septicaemia can increase the risk of intraspinal abscess formation in the postoperative period.

Paracervical block may have a greater adverse effect on the foetus that other nerve blocks used in obstetrics. Due to the systemic toxicity of bupivacaine, special care should be taken when using bupivacaine for paracervical block.

Small doses of local anaesthetics injected into the head and neck, including retrobulbar, dental and stellate ganglion blocks, may produce systemic toxicity due to inadvertent intra-arterial injection. Clinicians who perform retrobulbar blocks should be aware that there have been reports of respiratory arrest following local anaesthetic injection. Prior to retrobulbar block, necessary equipment, drugs and personnel should be immediately available as with all other regional procedures.

4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction

Bupivacaine should be used with care in patients receiving anti-arrhythmic drugs with local anaesthetic activity e.g. lignocaine, tocainide or beta-blocking drugs, since their toxic effects may be additive.

4.6 Pregnancy And Lactation

Bupivacaine enters the mother's milk, but in such small quantities that there is no risk of affecting the child at therapeutic dose levels.

There is no evidence of untoward effects in human pregnancy. In large doses there is evidence of decreased pup survival in rats and embryological effect in rabbits if bupivacaine is administered in pregnancy. Bupivacaine should not therefore be given in early pregnancy unless the benefits are considered to outweigh the risks.

Foetal bradycardia may occur following paracervical nerve block. Labour may be prolonged leading to the need for caesarean section.

4.7 Effects On Ability To Drive And Use Machines

In general, it is sufficient to allow 2-4 hours post nerve block or until full functions have returned following regional nerve block. In many situations, patients receive a sedative or other C.N.S. depressant drug e.g. diazepam, midazolam to allow the block to be performed. One must allow adequate time for the effects of these drugs to clear. Depending on dosage, local anaesthetics may have a very mild effect on mental function and co-ordination even in the absence of overt CNS toxicity and may temporarily impair locomotion and alertness.

4.8 Undesirable Effects

Serious systemic adverse reactions are rare, but may occur in connection with overdosage or unintentional intravascular injection.

Allergic skin and systemic reactions are very rare but have been reported. They include e.g. urticaria, face oedema, and brochospasm. Life threatening anaphylactic reactions have also been documented.

Bupivacaine causes systemic toxicity similar to that observed with other local anaesthetic agents. It is caused by high plasma concentration as a result of excessive dosage, rapid absorption or most commonly, inadvertent intravascular injection. Pronounced acidosis or hypoxia may increase the risk and severity of toxic reactions. Such reactions involve the central nervous system and the cardiovascular system. CNS reactions are characterised by numbness of the tongue, light-headedness, dizziness, blurred vision and muscle twitch, followed by drowsiness, convulsions, unconsciousness and possibly respiratory arrest.

Cardiovascular reactions are related to depression of the conduction system of the heart and myocardium leading to decreased cardiac output, heart block, hypotension, bradycardia and sometimes ventricular arrhythmias, including ventricular tachycardia, ventricular fibrillation and cardiac arrest. Usually these will be preceded or accompanied by major CNS toxicity, i.e. convulsions, but in rare cases cardiac arrest has occurred without prodromal CNS effects.

Epidural anaesthesia itself can cause adverse reactions regardless of the local anaesthetic agent used. These include hypotension and bradycardia due to sympathetic blockade and/or vasovagal fainting.

In severe cases cardiac arrest may occur. Accidental subarachnoid injection can lead to very high spinal anaesthesia possibly with apnoea and severe hypotension.

Neurological damage is a rare but well recognised consequence of regional and particularly epidural and spinal anaesthesia. It may be due to several causes, e.g. direct injury to the spinal cord or spinal nerves, anterior spinal artery syndrome, injection of an irritant substance, or an injection of a non-sterile solution. These may result in localised areas of paraesthesia or anaesthesia, motor weakness, loss of sphincter control and paraplegia. Occasionally these are permanent.

Hepatic dysfunction, with reversible increases of SGOT, SGPT, alkaline phosphatase and bilirubin has been observed following repeated injections or infusions of bupivacaine. If signs of hepatic dysfunction are observed during treatment with bupivacaine, the drug should be discontinued.

4.9 Overdose

Acute systemic toxicity

With accidental intravascular injection, the toxic effect will be obvious within <0.5-3 min., while with overdosage, peak plasma concentrations may not be reached for 20-30 min, and signs of toxicity are therefore delayed. Toxic reactions originate mainly in the central nervous and the cardiovascular systems.

Central nervous system toxicity is a graded response with symptoms and signs of escalating severity. The first symptoms are circumoral paraesthesia, numbness of the tongue, light-headedness, hyperacusis and tinnitus. Visual disturbance and muscular tremors are more serious and precede the onset of generalized convulsions. These signs must not be mistaken for a neurotic behaviour. Unconsciousness and grand mal convulsions may follow and can last from a few seconds to several minutes. Hypoxia and hypercarbia occur rapidly following convulsions due to the increased muscular activity together with the interference with normal respiration and loss of the airway. In severe cases, apnoea may occur. Acidosis increases the toxic effects of local anaesthetics.

Recovery is due to redistribution of the local anaesthetic drug from the central nervous system and metabolism. Recovery may be rapid unless large amounts of the drug have been injected.

Cardiovascular effects are only seen in patients with high systemic concentrations. Severe hypotension, bradycardia, arrhythmia and cardiovascular collapse may be the result in such cases.

Generally cardiovascular toxic effects are preceded by signs of toxicity in the central nervous system, unless the patient is receiving a general anaesthetic or is heavily sedated with drugs such as benzodiazepine or barbiturate.

Treatment of acute toxicity

Treatment of acute toxicity should be instituted at the latest when twitches occur. Necessary drugs and equipment should be immediately available. The objectives of treatment are to maintain oxygenation, stop the convulsions and to support the circulation.

Oxygen must be given and assisted ventilation if necessary (mask and bag). An anticonvulsant should be given i.v. if the convulsions do not stop spontaneously in 15-20 seconds. Thiopental 100-150mg i.v. will abort the convulsions rapidly. Alternatively diazepam 5-10mg i.v. may be used but its action is slower. Suxamethonium will stop the muscle convulsions rapidly, but will require tracheal intubation and controlled ventilation, and should be used by those familiar with these procedures.

If cardiovascular depression is evident (hypotension, bradycardia), ephedrine 5-10mg i.v. should be given and may be repeated if necessary after 2-3 min.

Should cardiac arrest occur, immediate cardiopulmonary resuscitation should be instituted. Optimal oxygenation and ventilation and circulatory support as well as treatment of acidosis are of vital importance, since hypoxia and acidosis will increase the systemic toxicity of local anaesthetics. Adrenaline should be given intravenously as soon as possible and repeated if necessary.

Cardiac arrest due to bupivacaine can be resistant to electrical defibrillation and resuscitation should be continued for a prolonged period.

5. Pharmacological Properties

5.1 Pharmacodynamic Properties

Bupivacaine Hydrochloride is a long acting local anaesthetic of the amide type. It prevents the generation and conduction of the nerve impulse by decreasing the permeability of the nerve cell membrane to sodium ions. As well as blocking conduction in nerve axons in the peripheral nervous system, local anaesthetics interfere with the function of all organs in which conduction or transmission of impulses occur. Following absorption, bupivacaine may cause stimulation of the CNS followed by depression and, in the cardiovascular system, it acts primarily on the myocardium where it may decrease electrical excitability, conduction rate and force of contraction.

5.2 Pharmacokinetic Properties

Like other local anaesthetics, the rate of systemic absorption of bupivacaine is dependent upon the total dose and concentration administered, the route of administration and the vascularity of the tissue locally. Bupivacaine is about 95% bound to plasma proteins, mainly to alpha-1-acid glycoprotein at low concentrations and to albumin at high concentrations. It has a half-life of 1.5 to 5 hours in adults and about 8 hours in neonates. Local anaesthetics are distributed to some extent to all body tissues, with higher concentrations found in highly perfused organs such as liver, heart and brain.

Bupivacaine is metabolised in the liver and is excreted in the urine mainly as metabolites, with only 5 to 6% as unchanged drug. The drug crosses the placenta.

5.3 Preclinical Safety Data

No further relevant information other than which is included in other sections of the Summary of Product Characteristics

6. Pharmaceutical Particulars

6.1 List Of Excipients

Sodium Chloride

Sodium Hydroxide

Water for Injection

6.2 Incompatibilities

Bupivacaine Hydrochloride Injection should not be mixed with other drugs. The solution must not be stored in contact with metal e.g. needles or metal parts of syringes as dissolved metal ions may cause swelling at site of the injection.

6.3 Shelf Life

3years

6.4 Special Precautions For Storage

Protect from light

Store at 25^oC.

6.5 Nature And Contents Of Container

Translucent plastic ampoule, the plastic is manufactured from polypropylene Ph.Eur. The ampoules are packed in individual thermoformed sterile polypropylene lidded trays, which are then packed in cardboard cartons.

Pack sizes: 10, 20, 50 and 100 x 10ml sterile wrapped ampoules

10, 20, 50 and 100 x 20ml sterile wrapped ampoules

6.6 Special Precautions For Disposal And Other Handling

Use as directed by the physician.

Keep out of reach of children.

If only part used, discard the remaining solution.

ADMINSTRATIVE DATA

7. Marketing Authorisation Holder

Antigen International Ltd.

Roscrea

Co.Tipperary

Ireland

8. Marketing Authorisation Number(S)

PL 02848/0183.

9. Date Of First Authorisation/Renewal Of The Authorisation

19 May 1997.

10. Date Of Revision Of The Text

November 2002.

Zolene HC otic

Generic Name: chloroxylenol, hydrocortisone, and pramoxine (otic) (KLOR oh ZYE nol, HYE droe KOR ti sone, pra MOX een)

Brand Names: Aero Otic HC, Cortamox, Cortane-B, Cortane-B Aqueous, Cortane-B Otic, Cortic-ND, Cyotic, Exotic-HC, Hydro Ear, IvDerm, Otirx, Oto-End, Otomar HC, Tri-Otic, Zolene HC, Zoto-HC Drops

What is Zolene HC (chloroxylenol, hydrocortisone, and pramoxine (otic))?

Chloroxylenol is an antibiotic that fights bacteria.

Pramoxine is a topical anesthetic. It works by interfering with pain signals sent from the nerves to the brain.

Hydrocortisone is a steroid. It reduces the actions of chemicals in the body that cause inflammation, redness, and swelling.

The combination of chloroxylenol, hydrocortisone, and pramoxine otic (for the ear) are used to treat pain, and swelling caused by ear infections.

Chloroxylenol, hydrocortisone, and pramoxine otic may also be used for other purposes not listed in this medication guide.

What is the most important information I should know about Zolene HC (chloroxylenol, hydrocortisone, and pramoxine (otic))?

Do not use this medication if you have a ruptured (torn) ear drum, or the medication could leak into the inner ear. A ruptured ear drum usually causes moderate to severe ear pain, with or without a decrease in hearing. Call your doctor if you think you have a ruptured ear drum. Your doctor will use a special scope to see any tear in your ear drum.

Before using chloroxylenol, hydrocortisone, and pramoxine, tell your doctor if you are allergic to any drugs, or if you have any type of illness or infection (other than an ear infection).

Chloroxylenol, hydrocortisone, and pramoxine otic is for use only in your ear. Avoid getting this medication in your mouth or eyes. If it does get into any of these areas, rinse with water. Ear infections may sometimes cause dizziness or a loss of balance. Be careful if you drive, operate machinery, or do anything else hazardous if you feel dizzy or off balance. Stop using this medication and call your doctor at once if you have ear drainage or discharge, severe burning or itching in your ear, or worsening pain, irritation, or rash.

Less serious side effects are more likely, and you may have none at all.

What should I discuss with my healthcare provider before using Zolene HC (chloroxylenol, hydrocortisone, and pramoxine (otic))?

You should not use this medication if you are allergic to chloroxylenol, hydrocortisone, or pramoxine.

Do not use this medication if you have a ruptured (torn) ear drum, or the medication could leak into the inner ear. A ruptured ear drum usually causes moderate to severe ear pain, with or without a decrease in hearing. Call your doctor if you think you have a ruptured ear drum. Your doctor will use a special scope to see any tear in your ear drum.

Before using chloroxylenol, hydrocortisone, and pramoxine, tell your doctor if you are allergic to any drugs, or if you have any type of illness or infection (other than an ear infection).

FDA pregnancy category C. This medication may be harmful to an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant during treatment. It is not known whether chloroxylenol, hydrocortisone, and pramoxine otic passes into breast milk or if it could harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby.

How should I use my Zolene HC (chloroxylenol, hydrocortisone, and pramoxine (otic))?

Use this medication exactly as it was prescribed for you. Do not use the medication in larger amounts, or use it for longer than recommended by your doctor.

Do not use the medication in your eyes or take it by mouth. Chloroxylenol, hydrocortisone, and pramoxine otic is for use in the ears only.

For best results, remove any ear wax or other debris before using the ear drops. Ask your doctor about safe methods of ear wax removal.

To use the ear drops, first remove the cap from the dropper bottle. Lie down or tilt your head with your ear facing upward. Pull back on your ear gently to open up the ear canal. Hold the dropper upside down over your ear canal and place enough drops of the medicine in your ear to fill the ear canal.

Do not place the dropper tip into your ear, or allow the tip to touch any surface. It may become contaminated.

After using the ear drops, keep the ear tilted upward for about 5 minutes. You may also be able to soak a small cotton wick with the medication and leave it in place. Ask your doctor of pharmacist for instructions on using a cotton wick.

Wipe the dropper tip with a clean tissue. Do not wash the tip with water or soap.

Use this medication for the full prescribed length of time. Your symptoms may improve before the infection is completely cleared. Talk with your doctor if your symptoms do not improve after using this medication.

Store the ear drops at room temperature away from moisture and heat. Keep the bottle properly capped.

What happens if I miss a dose?

Use the missed dose as soon as you remember. If it is almost time for your next dose, wait until then to use the medicine and skip the missed dose. Do not use extra medicine to make up the missed dose.

What happens if I overdose?

Seek emergency medical attention if you think you have used too much of this medicine.

An overdose of chloroxylenol, hydrocortisone, and pramoxine applied into the ear is not likely to cause life-threatening symptoms.

What should I avoid while using this medication?

Do not use other ear drops during treatment with chloroxylenol, hydrocortisone, and pramoxine otic without first talking to your doctor. Ear infections may sometimes cause dizziness or a loss of balance. Be careful if you drive, operate machinery, or do anything else hazardous if you feel dizzy or off balance. Chloroxylenol, hydrocortisone, and pramoxine otic is for use only in your ear. Avoid getting this medication in your mouth or eyes. If it does get into any of these areas, rinse with water.

Zolene HC (chloroxylenol, hydrocortisone, and pramoxine (otic)) side effects

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. Stop using this medication and call your doctor at once if you have any of these serious side effects:

• 
  

  ear drainage or discharge;

  
  


• 
  

  severe burning or itching in your ear; or

  
  


• 
  

  worsening pain, irritation, or rash.

  
  

Less serious side effects are more likely, and you may have none at all.

This is not a complete list of side effects and others may occur. Tell your doctor about any unusual or bothersome side effect. You may report side effects to FDA at 1-800-FDA-1088.

What other drugs will affect my Zolene HC (chloroxylenol, hydrocortisone, and pramoxine (otic))?

It is not likely that other drugs you take orally or inject will have an effect on chloroxylenol, hydrocortisone, and hydrocortisone otic. But many drugs can interact with each other. Tell your doctor about all your prescription and over-the-counter medications, vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start a new medication without telling your doctor.

More Zolene HC resources

• Zolene HC Use in Pregnancy & Breastfeeding
• Zolene HC Support Group
• 0 Reviews for Zolene HC - Add your own review/rating

Compare Zolene HC with other medications

• Acute Otitis Externa
• Ear Conditions
• Otitis Externa

Where can I get more information?

• Your pharmacist can provide more information about chloroxylenol, hydrocortisone, and pramoxine otic.

Fluocinonide Solution

FLUOCINONIDE TOPICAL SOLUTION USP, 0.05%

For External Use Only

Rx only

Not for Ophthalmic Use

Fluocinonide Solution Description

The topical corticosteroids constitute a class of primarily synthetic steroids used as anti-inflammatory and antipruritic agents. Fluocinonide Topical Solution contains Fluocinonide USP (Pregna-1,4-diene-3,20-dione, 21-(acetyloxy)-6,9-difluoro-11-hydroxy-16,17-[(1-methylethylidene)bis(oxy)]-, (6α,11β,16α)-). It has a molecular formula of C26H32F2O7 and a molecular weight of 494.53. It has the following structural formula:

Each mL of the 0.05% solution contains: fluocinonide 0.5 mg in a solution of alcohol (35%), diisopropyl adipate, citric acid and propylene glycol. In this formulation, the active ingredient is totally in solution.

Fluocinonide Solution - Clinical Pharmacology

Topical corticosteroids share anti-inflammatory, antipruritic 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. A significantly greater amount of fluocinonide is absorbed from the solution than from cream or gel formulations. Topical corticosteroids can be absorbed from normal intact skin. Inflammation and/or other disease processes in the skin increase the percutaneous absorption. Occlusive dressings substantially increase the percutaneous absorption of topical corticosteroids. Thus, occlusive dressings may be a valuable therapeutic adjunct for treatment of resistant dermatoses (See DOSAGE AND ADMINISTRATION).

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 for Fluocinonide Solution

Fluocinonide Topical Solution is indicated for the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses.

Contraindications

Fluocinonide Topical Solution is 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, the addition of occlusive dressings and dosage form. 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).

Not for ophthalmic use. Severe irritation is possible if fluocinonide topical solution contacts the eye. If that should occur, immediate flushing of the eye with a large volume of water is recommended. If irritation develops, topical corticosteroids should be discontinued and appropriate therapy instituted.

As with any topical corticosteroid product, prolonged use may produce atrophy of the skin and subcutaneous tissues. When used on intertriginous or flexor areas, or on the face, this may occur even with short term use.

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 Patients: 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. If there is contact with the eye(s) and severe irritation occurs, immediately flush with large volume of water.


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 dressings.


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:Teratogenic Effects: 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 and miliaria.

Overdosage

Topically applied corticosteroids can be absorbed in sufficient amounts to produce systemic effects

(See PRECAUTIONS).

Fluocinonide Solution Dosage and Administration

Apply a thin film to the affected area two to four times daily depending on the severity of the condition. Occlusive dressings may be used for the management of psoriasis or recalcitrant conditions. If an infection develops, the use of occlusive dressings should be discontinued and appropriate antimicrobial therapy instituted.

How is Fluocinonide Solution Supplied

Fluocinonide Topical Solution USP, 0.05% in:

      60 mL bottles          NDC 0168-0134-60.

Store at controlled room temperature 15°-30°C (59°-86°F).

Avoid excessive heat above 40°C (104°F).

E. FOUGERA & CO.

A division of

Fougera

PHARMACEUTICALS INC.

Melville, New York 11747

I2134C

R10/11

#49

PACKAGE LABEL – PRINCIPAL DISPLAY PANEL – 60mL CONTAINER

NDC 0168-0134-60

FOUGERA®

FLUOCINONIDE

TOPICAL SOLUTION

USP, 0.05%

60mL

FOR EXTERNAL USE ONLY

NOT FOR OPHTHALMIC USE

Rx only

E. FOUGERA & CO.

A division of Fougera Pharmaceuticals Inc.

Melville, New York 11747

PACKAGE LABEL – PRINCIPAL DISPLAY PANEL – 60mL CARTON

NDC 0168-0134-60

FOUGERA®

FLUOCINONIDE

TOPICAL

SOLUTION

USP, 0.05%

60 mL

EACH mL CONTAINS: fluocinonide

0.5 mg in a solution of alcohol

(35%), diisopropyl adipate, citric

acid, and propylene glycol.

FOR EXTERNAL USE ONLY

NOT FOR OPHTHALMIC USE

Rx only

E. FOUGERA & CO.

A division of

Fougera Pharmaceuticals Inc.

Melville, New York 11747

FLUOCINONIDE  fluocinonide  solution

Product Information Product Type HUMAN PRESCRIPTION DRUG NDC Product Code (Source) 0168-0134 Route of Administration TOPICAL DEA Schedule

Active Ingredient/Active Moiety Ingredient Name Basis of Strength Strength fluocinonide (fluocinonide) fluocinonide 0.5 mg  in 1 mL

Inactive Ingredients Ingredient Name Strength alcohol   diisopropyl adipate   citric acid monohydrate   propylene glycol

Product Characteristics Color      Score      Shape Size Flavor Imprint Code Contains

Packaging # NDC Package Description Multilevel Packaging 1 0168-0134-60 1 BOTTLE In 1 CARTON contains a BOTTLE 1 60 mL In 1 BOTTLE This package is contained within the CARTON (0168-0134-60)

Marketing Information
Marketing Category	Application Number or Monograph Citation	Marketing Start Date	Marketing End Date
ANDA	ANDA072934	02/27/1995

Labeler - E. FOUGERA & CO. A division of Fougera Pharmaceuticals Inc. (043838424)

Establishment
Name	Address	ID/FEI	Operations
Fougera Pharmaceuticals Inc.		043838424	ANALYSIS

Establishment
Name	Address	ID/FEI	Operations
Fougera Pharmaceuticals Inc.		174491316	MANUFACTURE

Revised: 01/2012E. FOUGERA & CO. A division of Fougera Pharmaceuticals Inc.

Program 6 Month Injectable

Dosage Form: FOR ANIMAL USE ONLY
Program 6 Month Injectable for Cats

6 Month Injectable for Cats

The six-month injection that controls flea populations in cats.

Caution

U.S. Federal law restricts this drug to use by or on the order of a licensed veterinarian.

Description

PROGRAM® (lufenuron) 6 Month Injectable for Cats is available in two syringe sizes for subcutaneous administration to cats and kittens according to their weight (See Dosage). Each preloaded syringe is formulated to provide 4.54 mg/pound (10 mg/kg) body weight of lufenuron. The active ingredient of Program 6 Month Injectable for Cats is lufenuron, a benzoylphenyl-urea derivative with the following chemical composition: N-[2,5-dichloro-4-(1,1,2,3,3,3,-hexafluoropropoxy)-phenylaminocarbonyl]-2,6-difluorobenzamide. Benzoylphenyl-urea compounds, including lufenuron, are classified as insect development inhibitors (IDIs).

Mode of Action

Lufenuron, the active ingredient of Program 6 Month Injectable for Cats, is an insect development inhibitor which breaks the flea life cycle by inhibiting egg development. Lufenuron’s mode of action is interference with chitin synthesis, polymerization and deposition. Lufenuron has no effect on adult fleas.

After biting a lufenuron-treated cat, the female flea ingests a blood meal containing lufenuron which is subsequently deposited in her eggs. Lufenuron prevents flea eggs from hatching and developing into adults and thus controls flea populations by breaking the life cycle. (See Efficacy.)

Indications

Program 6 Month Injectable for Cats is indicated for use in cats, six weeks of age and older, for the control of flea populations.

Lufenuron controls flea populations by preventing the development of flea eggs and does not kill adult fleas. Concurrent use of insecticides may be necessary for adequate control of adult fleas.

Warning

Do not use in dogs. A severe local reaction may occur in dogs that is not seen in cats.

Precautions

The safety of Program 6 Month Injectable for Cats in reproducing animals has not been established.

Program 6 Month Injectable for Cats breaks the flea life cycle by inhibiting egg development. However, pre-existing flea populations may continue to develop and emerge after treatment with Program 6 Month Injectable for Cats. Based on results of clinical studies, this emergence generally occurs during the first 30-60 days. Therefore, noticeable control may not be observed until several weeks after dosing when a pre-existing infestation is present. Cooler geographic areas may have longer lag periods due to a prolonged flea life cycle. Insecticides may be used concurrently depending on the severity of the infestation.

Efficacy

Laboratory and clinical trials have shown that Program 6 Month Injectable for Cats is a safe, effective and convenient method to control flea populations. A single dose provides long-lasting control for a full 6 months.

In laboratory studies, Program 6 Month Injectable for Cats provided a cumulative percent control of egg development of 94.8% and 97.7% beginning 14 days post-treatment through six months post-treatment in the dose titration and dose confirmation studies, respectively. There was a 2-3 week “induction phase” in these studies before significant effects on flea reproduction were seen.

Program 6 Month Injectable for Cats was effective in controlling flea populations when administered to 183 pet cats in a clinical setting. At study initiation, treated cats averaged 43 fleas per cat. Six months post-injection these cats averaged 11 fleas per cat.

Safety

Program 6 Month Injectable for Cats has been used and tested safely in over sixteen breeds of cats, including females, males and kittens. In well-controlled clinical trials, 294 cats were treated with lufenuron. Program 6 Month Injectable for Cats has also been safely used in cats receiving frequently used veterinary products such as vaccines, anthelmintics, antibiotics, steroids and insecticides.

The acute toxicity of injectable lufenuron was evaluated by administering 100 mg/kg bw, 10x the recommended 10 mg/kg bw dose rate, to adult cats. The potential cumulative toxicity of 1x and 3x the 10 mg/kg six month use rate of lufenuron injectable in 2 week old kittens was evaluated over a two month period. Other than injection site reactions (see below), no clinical signs of toxicity were reported in these studies.

Cumulative toxicity of injectable lufenuron in 2 month old cats was evaluated by administering 1, 3, or 5x the six-month dose three times during the 6 month study. This equates to cumulative doses of 3X, 9X, and 15X, respectively. Other than injection site reactions (see below), no clinical signs of toxicity were reported in these studies. Heinz body inclusions were present in all the control and treated cats, however, erythrocytes in the 50 mg/kg (15x cumulative dose) group had slightly elevated levels of Heinz bodies at 3-6 months.

The following injection site reactions were noted in these laboratory studies. Transient, minor discomfort was noted in some kittens and cats upon injection. Small raised areas at the injection sites, presumed to be deposits of lufenuron, were seen immediately after administration and persisted in some cases for the duration of the studies.This response at the injection site correlated microscopically with acute to granulomatous inflammation and fibrosis. Older injection sites showed less inflammation which indicates these effects may resolve with time. No neoplastic transformations were found. (See Adverse Reactions.)

Dosage

Program 6 Month Injectable for Cats is injected subcutaneously once every six months at the recommended minimum dosage of 4.54 mg lufenuron per pound (10 mg/kg) of body weight. 

Recommended Dosage Schedule                       

Body Weight	Syringe Size	Lufenuron Dose
Up to 8.8 lbs. (4.0 kg)	Small (0.4 ml)	40 mg
8.9 lbs. to 17.6 lbs. (4.1 to 8.0 kg)	Large (0.8 ml)	80 mg

Administration

Administer Program 6 Month Injectable for Cats subcutaneously using standard injection technique. Before administration, shake well to thoroughly mix the sterile suspension. Remove the needle guard and subcutaneously inject the entire contents of the syringe. Do not inject intramuscularly. The empty syringe should be disposed of in an approved manner.

To ensure the greatest benefits from the use of Program 6 Month Injectable for Cats, it is important to treat all cats within a household. All dogs within the household should be treated with lufenuron tablets. Untreated dogs and cats may develop infestations which could reduce the overall flea control within a household.

Do not administer this product to dogs.

Adverse Reactions

The following adverse reactions were observed in clinical field trials with Program 6 Month Injectable for Cats: pain on injection, injection site lumps/granulomas, vomiting, listlessness/lethargy and anorexia.

Histologic examination of one cat’s injection site lump showed evidence of inflammation surrounding an area of necrosis with marked proliferation of fibrous connective tissue. In another cat, granulamatous inflammation was noted which included non-pleomorphic fibrocytes and fibroplasia.

How Supplied

Program 6 Month Injectable for Cats is available in 0.4 ml and 0.8 ml unit dose syringes, formulated according to the weight of the cat. Unit dose packs are available in packages of 10 syringes per carton.

Storage Conditions

Program 6 Month Injectable for Cats should be stored at room temperature between 59° and 86 °F (15-30 °C).

NADA# 141-105, Approved by FDA

Manufactured for:

Novartis Animal Health US, Inc.,

Greensboro, NC 27404

© 1998 Novartis

NAH/PRO-FI/VI/1 

2/98

PRINCIPAL DISPLAY PANEL

Package Label – 40 mg

FOR CAT

TREATMENT ONLY

NOVARTIS

PROGRAM® (LUFENURON) 6 MONTH INJECTABLE FOR CATS 

40 mg.

up to 8.8 lbs.

Net Contents: Each syringe contains

40 mg LUFENURON in 0.4 mL

Contents: 10 syringes

Product #50911

NADA# 141-105, Approved by FDA

Caution: Federal (USA) law restricts this drug

to be used by the order of a licensed veterinarian.

Keep this and all drugs out

of the reach of children

PRINCIPAL DISPLAY PANEL

Package Label – 80 mg

FOR CAT

TREATMENT ONLY

NOVARTIS

PROGRAM® (LUFENURON) 6 MONTH INJECTABLE FOR CATS 

80 mg.

8.9 to 17.6 lbs.

Net Contents: Each syringe contains

80 mg LUFENURON in 0.8 mL

Contents: 10 syringes

Product #50921

NADA# 141-105, Approved by FDA

Caution: Federal (USA) law restricts this drug

to be used by the order of a licensed veterinarian.

Keep this and all drugs out

of the reach of children

Program 6 Month Injectable FOR CATS  lufenuron  injection, suspension

Product Information Product Type PRESCRIPTION ANIMAL DRUG NDC Product Code (Source) 58198-5091 Route of Administration SUBCUTANEOUS DEA Schedule

Active Ingredient/Active Moiety Ingredient Name Basis of Strength Strength LUFENURON (LUFENURON) LUFENURON 100 mg  in 1 mL

Inactive Ingredients Ingredient Name Strength No Inactive Ingredients Found

Product Characteristics Color      Score      Shape Size Flavor Imprint Code Contains

Packaging # NDC Package Description Multilevel Packaging 1 58198-5091-1 10 SYRINGE In 1 CARTON contains a SYRINGE, PLASTIC 1 0.4 mL In 1 SYRINGE, PLASTIC This package is contained within the CARTON (58198-5091-1)

Marketing Information
Marketing Category	Application Number or Monograph Citation	Marketing Start Date	Marketing End Date
NADA	NADA141105	03/13/1998

Program 6 Month Injectable FOR CATS  lufenuron  injection, suspension

Product Information Product Type PRESCRIPTION ANIMAL DRUG NDC Product Code (Source) 58198-5092 Route of Administration SUBCUTANEOUS DEA Schedule

Active Ingredient/Active Moiety Ingredient Name Basis of Strength Strength LUFENURON (LUFENURON) LUFENURON 100 mg  in 1 mL

Inactive Ingredients Ingredient Name Strength No Inactive Ingredients Found

Product Characteristics Color      Score      Shape Size Flavor Imprint Code Contains

Packaging # NDC Package Description Multilevel Packaging 1 58198-5092-1 10 SYRINGE In 1 CARTON contains a SYRINGE, PLASTIC 1 0.8 mL In 1 SYRINGE, PLASTIC This package is contained within the CARTON (58198-5092-1)

Marketing Information
Marketing Category	Application Number or Monograph Citation	Marketing Start Date	Marketing End Date
NADA	NADA141105	03/13/1998

Labeler - Novartis Animal Health US, Inc. (966985624)

Revised: 03/1998Novartis Animal Health US, Inc.

Maxitrol Drops

Pronunciation: DEX-a-METH-a-sone/NEE-oh-MYE-sin/POL-ee-MIX-in
Generic Name: Dexamethasone/Neomycin/Polymyxin B
Brand Name: Examples include Maxitrol and Poly-Dex

Maxitrol Drops are used for:

Treating eye infections and associated symptoms, including redness, irritation, and discomfort, caused by certain bacteria. It may also be used for other conditions as determined by your doctor.

Maxitrol Drops are a combination of 2 antibiotics and a corticosteroid (dexamethasone). The antibiotics work by slowing the growth of, or killing, sensitive bacteria on the eye. The corticosteroid reduces inflammation.

Do NOT use Maxitrol Drops if:

• you are allergic to any ingredient in Maxitrol Drops


• you have a fungal, viral (eg, herpes simplex, chickenpox, shingles), or mycobacterial infection of the eye

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

Before using Maxitrol Drops:

Some medical conditions may interact with Maxitrol Drops. 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 diabetes, glaucoma, or thinning of the cornea or white of the eye

Some MEDICINES MAY INTERACT with Maxitrol Drops. Because little, if any, of Maxitrol Drops are absorbed into the blood, the risk of it interacting with another medicine is low.

Ask your health care provider if Maxitrol Drops 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 Maxitrol Drops:

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

• Maxitrol Drops are only for the eye. Do not get it in your nose or mouth.


• To prevent reinfection, wash your hands before and after using Maxitrol Drops.


• Shake well before each use.


• To use Maxitrol Drops in the eye, first, wash your hands. Tilt your head back. Using your index finger, pull the lower eyelid away from the eye to form a pouch. Drop the medicine into the pouch and gently close your eyes. Immediately use your finger to apply pressure to the inside corner of the eyelid for 1 to 2 minutes. Do not blink. Remove excess medicine around your eye with a clean, dry tissue, being careful not to touch your eye. Wash your hands to remove any medicine that may be on them.


• To prevent germs from contaminating your medicine, do not touch the applicator tip to any surface, including the eye. Keep the container tightly closed.


• Do not wear contact lenses while you are using Maxitrol Drops. Take care of your contact lenses as directed by the manufacturer. Check with your doctor before you use them.


• To clear up your infection completely, use Maxitrol Drops for the full course of treatment. Keep using it even if you feel better in a few days.


• If you miss a dose of Maxitrol Drops, 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 Maxitrol Drops.

Important safety information:

• Maxitrol Drops only works against bacteria; it does not treat viral infections (eg, the common cold).


• Be sure to use Maxitrol Drops for the full course of treatment. If you do not, the medicine may not clear up your infection completely. The bacteria could also become less sensitive to this or other medicines. This could make the infection harder to treat in the future.


• Long-term or repeated use of Maxitrol Drops may cause a second infection. Tell your doctor if signs of a second infection occur. Your medicine may need to be changed to treat this.


• Long-term use of Maxitrol Drops may cause an increase in the pressure in your eyes. Do NOT take more than the recommended dose or use for longer than 10 days without checking with your doctor.


• Maxitrol Drops should be used with extreme caution in CHILDREN; safety and effectiveness in children have not been confirmed.


• PREGNANCY and BREAST-FEEDING: If you become pregnant, contact your doctor. You will need to discuss the benefits and risks of using Maxitrol Drops while you are pregnant. It is not known if Maxitrol Drops are found in breast milk after topical use. If you are or will be breast-feeding while you use Maxitrol Drops, check with your doctor. Discuss any possible risks to your baby.

Possible side effects of Maxitrol Drops:

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:

Burning or stinging when you first put the medicine in your eye; dry, flaky skin; irritation; itching; redness; swelling.

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); changes in vision; continued burning or itching; eye pain.

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: Maxitrol 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.

Proper storage of Maxitrol Drops:

Store Maxitrol Drops between 46 and 80 degrees F (8 and 27 degrees C). Store away from heat, moisture, and light. Keep the container tightly closed. Keep Maxitrol Drops out of the reach of children and away from pets.

General information:

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


• Maxitrol Drops are 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 Maxitrol Drops. 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 Maxitrol resources

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

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selegiline Transdermal

se-LE-ji-leen

Transdermal route(Patch, Extended Release)

Antidepressants increased the risk of suicidal thinking and behavior in children, adolescents, and young adults in short-term studies with major depressive disorder (MDD) and other psychiatric disorders. Short term studies did not show an increase in the risk of suicidality with antidepressants compared to placebo in adults beyond age 24, and there was a reduction in risk with antidepressants compared to placebo in adults aged 65 and older. This risk must be balanced with the clinical need. Monitor patients closely for clinical worsening, suicidality, or unusual changes in behavior. Families and caregivers should be advised of the need for close observation and communication with the prescriber. The transdermal patch should not be used in pediatric patients under the age of 12, at any dose, even with dietary modifications .

Commonly used brand name(s)

In the U.S.

• Emsam

Available Dosage Forms:

• Patch, Extended Release

Therapeutic Class: Antidepressant

Pharmacologic Class: Monoamine Oxidase Inhibitor, Type B

Uses For selegiline

Selegiline transdermal is used to treat mental depression. selegiline is a monoamine oxidase (MAO) inhibitor .

selegiline is available only with your doctor's prescription .

Before Using selegiline

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 selegiline, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to selegiline 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 performed to date have not demonstrated any benefit to using selegiline transdermal in children with depression. Studies have shown that some children, teenagers, and young adults think about suicide or attempt suicide when taking selegiline. Because of this toxicity, use in children is not recommended .

Selegiline transdermal should not be used in children below 12 years of age .

Geriatric

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of selegiline transdermal in the elderly .

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 selegiline, 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 selegiline 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.

• Amitriptyline


• Amoxapine


• Amphetamine


• Apraclonidine


• Atomoxetine


• Benzphetamine


• Brimonidine


• Bupropion


• Carbamazepine


• Citalopram


• Clomipramine


• Cyclobenzaprine


• Cyproheptadine


• Desipramine


• Desvenlafaxine


• Dexfenfluramine


• Dexmethylphenidate


• Dextroamphetamine


• Dextromethorphan


• Diethylpropion


• Duloxetine


• Ephedrine


• Escitalopram


• Fenfluramine


• Fluoxetine


• Guanadrel


• Guanethidine


• Imipramine


• Isocarboxazid


• Isometheptene


• Levodopa


• Levomethadyl


• Linezolid


• Lisdexamfetamine


• Maprotiline


• Mazindol


• Meperidine


• Methadone


• Methamphetamine


• Methotrimeprazine


• Methyldopa


• Methylene Blue


• Methylphenidate


• Milnacipran


• Mirtazapine


• Morphine


• Morphine Sulfate Liposome


• Nefopam


• Nortriptyline


• Opipramol


• Oxcarbazepine


• Paroxetine


• Phendimetrazine


• Phenelzine


• Phenmetrazine


• Phentermine


• Phenylalanine


• Phenylephrine


• Phenylpropanolamine


• Procarbazine


• Propoxyphene


• Protriptyline


• Pseudoephedrine


• Rasagiline


• Reserpine


• Selegiline


• Sertraline


• Sibutramine


• St John's Wort


• Tapentadol


• Tetrabenazine


• Tramadol


• Tranylcypromine


• Trimipramine


• Venlafaxine


• Vilazodone

Using selegiline 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.

• Albuterol


• Altretamine


• Arformoterol


• Avocado


• Bambuterol


• Bitolterol


• Bitter Orange


• Broxaterol


• Buspirone


• Clenbuterol


• Clovoxamine


• Difenoxin


• Diphenoxylate


• Dothiepin


• Doxepin


• Droperidol


• Ethchlorvynol


• Femoxetine


• Fenoterol


• Fentanyl


• Fluvoxamine


• Formoterol


• Guarana


• Hexoprenaline


• Hydromorphone


• Indacaterol


• Isoetharine


• Kava


• Levalbuterol


• Licorice


• Lofepramine


• Ma Huang


• Mate


• Mephentermine


• Metaraminol


• Metoclopramide


• Nefazodone


• Oxycodone


• Pentazocine


• Pirbuterol


• Procaterol


• Reboxetine


• Rimiterol


• Ritodrine


• Salmeterol


• St John's Wort


• Terbutaline


• Tryptophan


• Tulobuterol


• Tyrosine

Using selegiline 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.

• Acarbose


• Acetohexamide


• Benfluorex


• Chlorpropamide


• Dopamine


• Ginseng


• Gliclazide


• Glimepiride


• Glipizide


• Gliquidone


• Glyburide


• Guar Gum


• Insulin


• Insulin Aspart, Recombinant


• Insulin Glulisine


• Insulin Lispro, Recombinant


• Metformin


• Miglitol


• Repaglinide


• Tolazamide


• Tolbutamide


• Troglitazone

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 selegiline 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 selegiline, or give you special instructions about the use of food, alcohol, or tobacco.

• Tyramine Containing Food

Other Medical Problems

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

• Heart attack, recent or


• Heart problems or


• Low blood pressure or


• Seizures—Use with caution. selegiline may worsen these conditions .

• Mania or hypomania (history of)—Use of selegiline transdermal may activate these conditions .

• Pheochromocytoma (a tumor of the adrenal gland)—Should not be used in patients with this condition .

Proper Use of selegiline

selegiline comes with a Medication Guide. Read and follow these instructions carefully. Ask your doctor or pharmacist if you have any questions .

To use the skin patch:

• Apply the patch right away after removing it from the protective pouch. Do not cut it into smaller pieces and do not touch the sticky surface of the patch. Wear only one patch at a time.


• Apply the patch to a dry, smooth skin area on your upper chest or back (below the neck and above the waist), upper thigh, or to the outer surface of the upper arm. Do not put the patch over hairy, oily, irritated, broken, scarred, or calloused skin. Avoid putting the patch on areas where it could be rubbed off by tight clothing.


• Press the patch firmly in place with your fingertips to make sure that the edges of the patch stick well.


• Put on a new patch if the old one has fallen off and cannot be reapplied.


• After 24 hours, remove the patch. Choose a different place on your skin to apply the new patch. Do not put the new patch on the same place you wore the last one. Try to change the patch at the same time each day.


• After removing a used patch, fold the patch in half with the sticky sides together. Make sure to dispose of it out of the reach of children and pets.


• Wash the area of skin where you will apply the patch gently with soap and warm water. Rinse completely and dry with a clean dry towel.


• Do not expose the patch to direct sources of heat, such as heating pads, electric blankets, heat lamps, saunas, hot tubs, heated water beds, or direct sunlight for long periods of time.


• Wash your hands with soap and water before and after applying a patch. Do not touch your eyes until after you have washed your hands .

Do not stop using selegiline without asking your doctor. If you have not used your medicine for several days in a row, do not start using it again without talking to your doctor first .

Dosing

The dose of selegiline 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 selegiline. 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 transdermal dosage form (patch):
  
  • For mental depression:
    
    • Adults—At first, one 6 milligram (mg) patch once a day. Your doctor may increase your dose if needed.
    
    
    • Children 12 years of age and older—Use and dose must be determined by your doctor.
    
    
    • Children below 12 years of age—Use is not recommended .
    
    
  
  

Missed Dose

If you forget to wear or change a patch, put one on as soon as you can. If it is almost time to put on your next patch, wait until then to apply a new patch and skip the one you missed. Do not apply extra patches to make up for a missed dose.

Storage

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

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.

Precautions While Using selegiline

It is very important that your doctor check your progress at regular visits to make sure selegiline is working properly and to check for unwanted effects .

Selegiline transdermal may cause some people to be agitated, irritable, or display other abnormal behaviors. It may also cause some people to have suicidal thoughts and tendencies or to become more depressed. If you, your child, or your caregiver notice any of these side effects, tell your doctor or your child's doctor right away .

When selegiline transdermal is used at low doses, there are no restrictions on food or beverages you eat or drink. However, the chance exists that dangerous reactions, such as sudden high blood pressure, may occur if higher doses are used with certain foods or beverages. These foods or beverages include foods that have a high tyramine content (most common in foods that are aged or fermented to increase their flavor), such as cheeses; fava or broad bean pods; yeast or meat extracts; smoked or pickled meat, poultry, or fish; fermented sausage (bologna, pepperoni, salami, summer sausage) or other fermented meat; sauerkraut; any spoiled or improperly stored meat, poultry, fish, or animal livers; or any overripe fruit. These may also include alcoholic beverages or alcohol-free or reduced-alcohol beer and wine. Also, for at least 2 weeks after you stop using selegiline, these foods or beverages may continue to react with selegiline transdermal. If a list of these foods and beverages is not given to you, ask your health care professional to provide one .

Check with your doctor or hospital emergency room immediately if severe headache, stiff neck, chest pains, fast heartbeat, or nausea and vomiting occur while you are using selegiline. These may be symptoms of a serious side effect that should have a doctor's attention .

You should not use selegiline if you are taking other medicines to treat depression (such as amitriptyline, bupropion, doxepin, duloxetine, fluoxetine, imipramine, mirtazapine, nortriptyline, paroxetine, sertraline, venlafaxine, Celexa®, Cymbalta®, Effexor®, Elavil®, Lexapro™, Paxil®, Prozac®, Tofranil®, Wellbutrin®, or Zoloft®), anxiety medicine (such as buspirone or BuSpar®), MAO inhibitors (MAOI) (such as Eldepryl®, Marplan®, Nardil®, or Parnate®), St. John's wort, or pain medicines (such as meperidine, methadone, propoxyphene, tramadol, Darvon®, Demerol®, Dolophine®, or Ultram®). Do not use selegiline if you are taking seizure medicines (such as carbamazepine, oxcarbazepine, Tegretol®, or Trileptal®), cough medicines (such as dextromethorphan or Benylin®), medicine to treat muscle spasms (such as cyclobenzaprine or Flexeril®), over-the-counter diet pills, herbal weight-loss products, cold medicines (such as ephedrine, phenylephrine, phenylpropanolamine, pseudoephedrine, Neo-Synephrine®, Novafed®, or Sudafed®), any herbal or dietary supplement that contains tyramine, or medicines called amphetamines (also called stimulants or "uppers"). Do not use selegiline if you take selegiline capsules or tablets .

Before you have any kind of surgery, tell the medical doctor in charge that you are taking selegiline. Using selegiline together with medicines that are sometimes used during surgery may increase the effects of these medicines .

Dizziness, lightheadedness, or fainting may occur, especially when you get up from a lying or sitting position. Getting up slowly may help. If the problem continues or gets worse, check with your doctor .

selegiline 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

• Chills


• cold sweats


• confusion


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


• headache


• sleeplessness


• trouble sleeping


• unable to sleep

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

• Burning, itching, redness, skin rash, swelling, or soreness at site


• diarrhea


• dry mouth

Less common

• Acid or sour stomach


• belching


• body aches or pain


• change or problem with discharge of semen


• congestion


• cough


• dryness or soreness of throat


• fever


• heartburn


• hoarseness


• indigestion


• pain or tenderness around eyes and cheekbones


• rash


• runny nose


• shortness of breath or troubled breathing


• stomach discomfort, upset, or pain


• stuffy or runny nose


• tender, swollen glands in neck


• tightness of chest or wheezing


• trouble in swallowing


• voice changes


• weight changes

Rare

• Decreased interest in sexual intercourse


• inability to have or keep an erection


• loss in sexual ability, desire, drive, or performance


• not able to have an orgasm

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: selegiline Transdermal side effects (in more detail)

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