Hycomine Compound Tablets (Endo Labs)

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DESCRIPTION

HYCOMINE Compound tablets contain hydrocodone (dihydrocodeinone) bitartrate, a semi-synthetic centrally-acting opioid antitussive; chlorpheniramine maleate, an antihistamine; phenylephrine hydrochloride, a sympathomimetic amine decongestant; acetaminophen, an analgesic/antipyretic; and caffeine, a centrally-acting stimulant, for oral administration.

Each HYCOMINE Compound tablet contains:

Hydrocodone Bitartrate, USP 5 mg

Chlorpheniramine Maleate, USP    2 mg

Phenylephrine Hydrochloride, USP   10 mg

Acetaminophen, USP 250 mg

Caffeine, Anhydrous, USP   30 mg

HYCOMINE Compound tablets also contain: cherry flavor, colloidal silicon dioxide, FD&C Red 40, magnesium stearate, microcrystalline cellulose, povidone and starch.

CLINICAL PHARMACOLOGY

Clinical trials have proven hydrocodone bitartrate to be an effective antitussive agent which is pharmacologically 2 to 8 times as potent as codeine. At equi-effective doses, its sedative action is greater than codeine. The precise mechanism of action of hydrocodone and other opiates is not known, however, hydrocodone is believed to act by directly depressing the cough center. In excessive doses hydrocodone, like other opium derivatives, will depress respiration. The effects of hydrocodone in therapeutic doses on the cardiovascular system is insignificant. The constipation effects of hydrocodone are much weaker than that of morphine and no stronger than that of codeine. Hydrocodone can produce miosis, euphoria, physical and psychological dependence. At therapeutic antitussive doses, it does exert analgesic effects. Following a 10 mg oral dose of hydrocodone administered to five adult male human subjects, the mean peak concentration was 23.6 ± 5.2 ng/mL. Maximum serum levels were achieved at 1.3 ± 0.3 hours and the half-life was determined to be 3.8 ± 0.3 hours. Hydrocodone exhibits a complex pattern of metabolism including O-demethylation, N-demethylation and 6-keto reduction to the corresponding 6-(alpha)- and 6-(beta)-hydroxymetabolites.

Chlorpheniramine maleate is a competitive H ₁ -receptor histamine blocking drug, thereby counteracting the effects of histamine release associated with allergic manifestations of upper respiratory tract inflammatory disorders. H ₁ -blocking drugs inhibit the actions of histamine on smooth muscle, capillary permeability, and can both stimulate and depress the central nervous system. Phenylephrine hydrochloride effects its vasoconstrictor activity by releasing noradrenaline from sympathetic nerve endings, and from direct stimulation of (alpha)-adrenoreceptors in blood vessels. Acetaminophen is an antipyretic and peripherally acting analgesic. Caffeine is a central nervous system stimulant.

INDICATIONS AND USAGE

HYCOMINE Compound is indicated for the symptomatic relief of cough, nasal congestion, and discomfort associated with upper respiratory tract infections.

CONTRAINDICATIONS

HYCOMINE Compound is contraindicated in patients hypersensitive to any component of the drug, and concurrent MAO inhibitor therapy. Patients known to be hypersensitive to other opioids, antihistamines, or sympathomimetic amines may exhibit cross sensitivity with HYCOMINE Compound. Phenylephrine is contraindicated in patients with heart disease, hypertension, diabetes or hyperthyroidism. Hydrocodone is contraindicated in the presence of an intracranial lesion associated with increased intracranial pressure, and whenever ventilatory function is depressed.

WARNINGS

May be habit forming. Hydrocodone can produce drug dependence of the morphine type and therefore has the potential for being abused. Psychic dependence, physical dependence and tolerance may develop upon repeated administration of HYCOMINE Compound and it should be prescribed and administered with the same degree of caution appropriate to the use of other opioid drugs. (See DRUG ABUSE AND DEPENDENCE ).

Respiratory Depression:    HYCOMINE Compound produces dose-related respiratory depression by directly acting on brain stem respiratory centers. If respiratory depression occurs, it may be antagonized by the use of NARCAN® (naloxone hydrochloride) and other supportive measures when indicated.

Head Injury and Increased Intracranial Pressure:    The respiratory depressant properties of opioids and their capacity to elevate cerebrospinal fluid pressure may be markedly exaggerated in the presence of head injury, other intracranial lesions or a pre-existing increase in intracranial pressure. Furthermore, opioids produce adverse reactions which may obscure the clinical course of patients with head injuries.

Acute Abdominal Conditions:    The administration ofHYCOMINE Compound or other opioids may obscure the diagnosis or clinical course of patients with acute abdominal conditions.

Phenylephrine:    Hypertensive crises can occur with concurrent use of phenylephrine and monoamine oxidase (MAO) inhibitors, indomethacin or with beta-blockers and methyldopa.

If a hypertensive crisis occurs these drugs should be discontinued immediately and therapy to lower blood pressure should be instituted immediately. Fever should be managed by means of external cooling.

Chlorpheniramine:    Antihistamines may produce drowsiness or excitation, particularly in children and elderly patients.

PRECAUTIONS

Before prescribing medication to suppress or modify cough, it is important to ascertain that the underlying cause of cough is identified, that modification of cough does not increase the risk of clinical or physiologic complications, and that appropriate therapy for the primary disease is provided.

Usage in Ambulatory Patients:    Hydrocodone, like all opioids, and antihistamines such as chlorpheniramine maleate, may impair the mental and/or physical abilities required for the performance of potentially hazardous tasks such as driving a car or operating machinery; phenylephrine may produce a rapid pulse, dizziness or palpitations; patients should be cautioned accordingly.

Drug Interactions:    Patients receiving other opioid analgesics, general anesthetics, phenothiazines, other tranquilizers, sedative-hypnotics or other CNS depressants (including alcohol) concomitantly with hydrocodone may exhibit an additive CNS depression. When such combined therapy is contemplated, the dose of one or both agents should be reduced. The use of phenylephrine with other sympathomimetic amines and MAO inhibitors may produce an additive elevation of blood pressure. MAO inhibitors may prolong the anticholinergic effects of antihistamines. (See WARNINGS ).

Carcinogenesis, Mutagenesis, Impairment of Fertility: Carcinogenicity, mutagenicity, and reproduction studies have not been conducted with HYCOMINE Compound.

Usage in Pregnancy:    Pregnancy Category C. Animal reproduction studies have not been conducted withHYCOMINE Compound. It is also not known whetherHYCOMINE Compound can cause fetal harm when administered to a pregnant woman or can affect reproductive capacity. HYCOMINE Compound should be given to a pregnant woman only if clearly needed.

Nonteratogenic Effects:    Babies born to mothers who have been taking opioids regularly prior to delivery will be physically dependent. The withdrawal signs include irritability and excessive crying, tremors, hyperactive reflexes, increased respiratory rate, increased stools, sneezing, yawning, vomiting and fever. The intensity of the syndrome does not always correlate with the duration of maternal opioid use or dose. Chlorpromazine 0.7-1.0 mg/kg q 6 h, phenobarbital 2 mg/kg q 6 h, and paregoric 2-4 drops/kg q 4 h, have been used to treat withdrawal symptoms in infants. The duration of therapy is 4 to 28 days, with dosages decreased as tolerated.

Nursing Mothers:    It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from HYCOMINE Compound, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.

Pediatric Use:    Safety and effectiveness in pediatric patients below the age of 2 years have not been established.

ADVERSE REACTIONS

Respiratory System:    Hydrocodone produces dose-related respiratory depression by acting directly on brain stem respiratory centers.

Cardiovascular System:    Hypertension, postural hypotension, tachycardia and palpitations.

Genitourinary System:    Ureteral spasm, spasm of vesical sphincters and urinary retention have been reported with opiates.

Central Nervous System:    Sedation, drowsiness, mental clouding, lethargy, impairment of mental and physical performance, anxiety, fear, dysphoria, dizziness, psychic dependence, mood changes, and blurred vision.

Gastrointestinal System:    Nausea and vomiting occur more frequently in ambulatory than in recumbent patients.

DRUG ABUSE AND DEPENDENCE

Special care should be exercised in prescribing hydrocodone for emotionally unstable patients and for those with a history of drug misuse. Such patients should be closely supervised when long-term therapy is contemplated.

HYCOMINE Compound is a Schedule III opioid. Psychic dependence, physical dependence, and tolerance may develop upon repeated administration of opioids; therefore,HYCOMINE Compound should always be prescribed and administered with caution. Physical dependence is the condition in which continued administration of the drug is required to prevent the appearance of a withdrawal syndrome.

Patients physically dependent on opioids will develop an abstinence syndrome upon abrupt discontinuation of the opioid or following the administration of a opioid antagonist. The character and severity of the withdrawal symptoms are related to the degree of physical dependence. Manifestations of opioid withdrawal are similar to but milder than that of morphine and include lacrimation, rhinorrhea, yawning, sweating, restlessness, dilated pupils, anorexia, gooseflesh, irritability and tremor. In more severe forms, nausea, vomiting, intestinal spasm and diarrhea, increased heart rate and blood pressure, chills, and pains in bones and muscles of the back and extremities may occur. Peak effects will usually be apparent at 48 to 72 hours.

Treatment of withdrawal is usually managed by providing sufficient quantities of an opioid to suppress severe withdrawal symptoms and then gradually reducing the dose of opioid over a period of several days.

OVERDOSAGE

The signs and symptoms of overdosage of the individual components of HYCOMINE Compound may be modified in varying degrees by the presence of other active ingredients. Overdosage with phenylephrine alone may result in tremor, restlessness, increased motor activity, agitation and hallucinations.

Acetaminophen

Signs and Symptoms:    In acute acetaminophen overdosage, dose-dependent, potentially fatal hepatic necrosis is the most serious adverse effect. Renal tubular necrosis, hypoglycemic coma and thrombocytopenia may also occur.

Acetaminophen in massive overdosage may cause hepatic toxicity in some patients. In cases of suspected overdose, you may wish to call your regional poison center for assistance in diagnosis and for directions in the use ofN-acetylcysteine as an antidote.

In adults, hepatic toxicity has rarely been reported with acute overdoses of less than 10 grams and fatalities with less than 15 grams. Importantly, young children seem to be more resistant than adults to the hepatotoxic effect of an acetaminophen overdose. Despite this, the measures outlined below should be initiated in any adult or child suspected of having ingested an acetaminophen overdose.

Early symptoms following a potentially hepatotoxic overdose may include nausea, vomiting, diaphoresis and general malaise. Clinical and laboratory evidence of hepatic toxicity may not be apparent until 48 to 72 hours post-ingestion.

Treatment:    The stomach should be emptied promptly by lavage or by induction of emesis with syrup of ipecac. Patient's estimates of the quantity of a drug ingested are notoriously unreliable. Therefore, if an acetaminophen overdose is suspected, a serum acetaminophen assay should be obtained as early as possible, but no sooner than four hours following ingestion. Liver function studies should be obtained initially and repeated at 24-hour intervals.

The antidote, N-acetylcysteine should be administered as early as possible, preferably within 16 hours of the overdose ingestions for optimal results, but in any case, within 24 hours. Following recovery, there are no residual structural or functional hepatic abnormalities.

Hydrocodone

Signs and Symptoms:    Serious overdosage with hydrocodone is characterized by respiratory depression (a decrease in respiratory rate and/or tidal volume, Cheyne-Stokes respiration, cyanosis), extreme somnolence progressing to stupor or coma, skeletal muscle flaccidity, cold and clammy skin, and sometimes bradycardia and hypotension. In severe overdosage, apnea, circulatory collapse, cardiac arrest and death may occur.

Treatment:    Primary attention should be given to the reestablishment of adequate respiratory exchange through provision of a patent airway and the institution of assisted or controlled ventilation. The opioid antagonist naloxone hydrochloride is a specific antidote for respiratory depression which may result from overdosage or unusual sensitivity to opioids including hydrocodone. Therefore, an appropriate dose of naloxone hydrochloride should be administered, preferably by the intravenous route, simultaneously with efforts at respiratory resuscitation. For further information, see full prescribing information for naloxone hydrochloride. An antagonist should not be administered in the absence of clinically significant respiratory depression. Oxygen, intravenous fluids, vasopressors and other supportive measures should be employed as indicated. Gastric emptying may be useful in removing unabsorbed drug. Activated charcoal may be of benefit.

DOSAGE AND ADMINISTRATION

Usual dosage, not less than 4 hours apart:

Adults: 1 tablet 4 times a day

Children: 6 to 12 years: 1/2 tablet 4 times a day

The total daily consumption of acetaminophen should not exceed 4 grams.

HOW SUPPLIED

HYCOMINE® Compound is available as a coral pink, round tablet scored and debossed with "HYCOMINE" on one side and plain on the other, supplied in bottles as follows:

Bottles of 100    NDC 63481-048-70

Bottles of 500    NDC 63481-048-85

Oral prescription where permitted by State law.

Store at 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F). [See USP Controlled Room Temperature.] Dispense in a tight, light-resistant container as defined in the USP, with a child-resistant closure (as required).

HYCOMINE® is a Registered Trademark of Endo Pharmaceuticals Inc.

NARCAN® is a Registered Trademark of Endo Pharmaceuticals Inc.

Copyright © Endo Pharmaceuticals Inc. 2003

6491-03/May, 2003

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