Acetaminophen; Chlorpheniramine Maleate; Hydrocodone Bitartrate; Phenylephrine Hydrochloride (0036)
| Ingredients: |
Acetaminophen; Chlorpheniramine Maleate; Hydrocodone Bitartrate; Phenylephrine Hydrochloride |
| Indications: |
Congestion, nasal; Cough |
| Pregnancy Category: |
C |
| FDA Approved: |
pre- 1938 |
| Classes: |
Analgesics, non- narcotic; Antihistamines, H1; Antitussives; Decongestants, nasal |
| Brand Names: |
Hycomine Compound
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US
;
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| DEA schedules: |
Schedule III |
DESCRIPTION
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Hycomine compound tablets contain hydrocodone (dihydrocodeinone) bitartrate, a semi- synthetic centrally- acting narcotic
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*: 5 mg
- Chlorpheniramine Maleate: 2 mg
- Phenylephrine Hydrochloride: 10 mg
- Acetaminophen: 250 mg
- Caffeine, Anhydrous: 30 mg
* Warning: May be habit forming
Hycomine Compound tablets also contain: Cherry flavor, colloidal silicon dioxide, FD&C red 40, magnesium stearate, microcrystalline cellulose, povidone and starch.
Storage: Store at controlled room temperature (59- 86°F, 15- 30°C).
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CLINICAL PHARMACOLOGY
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Clinical trials have proven hydrocodone bitartrate to be an effective antitussive agent which is pharmacologically 2- 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 5 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- α- and 6- β- hydroxymetabolites.
Chlorpheniramine maleate is a competitive H1 - receptor histamine blocking drug, thereby counteracting the effects of histamine release associated with allergic manifestations
of upper respiratory tract inflammatory disorders. H1 - 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 α- adrenoreceptors in blood vessels. Acetaminophen is an antipyretic
and peripherally acting analgesic. Caffeine is a central nervous system stimulant.
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INDICATIONS AND USAGE
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Hycomine compound is indicated for the symptomatic relief of cough, nasal congestion, and discomfort associated with upper
respiratory tract infections.
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CONTRAINDICATIONS
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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.
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WARNINGS
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May be habit forming. Hydrocodone can produce drug dependence of the morphine type and therefore has the potential for being
abused. Psychic 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 narcotic drugs. (See DRUG ABUSE AND DEPENDENCE .)
Respiratory Depression
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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 naloxone HCl and other supportive measures when indicated.
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Head Injury and Increased Intracranial Pressure
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The respiratory depressant properties of narcotics 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, narcotics produce adverse reactions which may obscure the clinical course of patients with head injuries.
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Acute Abdominal Conditions
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The administration of hycomine compound or other narcotics may obscure the diagnosis or clinical course of patients with acute
abdominal conditions.
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Phenylephrine
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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.
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Chlorpheniramine
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Antihistamines may produce drowsiness or excitation, particularly in children and elderly patients.
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PRECAUTIONS
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General
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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 Patient
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Hydrocodone, like all narcotics, 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.
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Carcinogenesis, Mutagenesis, and Impairment of Fertility
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Carcinogenicity, mutagenicity and reproduction studies have not been conducted with hycomine compound.
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Pregnancy Category C
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Teratogenic Effects
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Animal reproduction studies have not been conducted with hycomine compound. It is also not known whether this drug can cause
fetal harm when administered to pregnant woman or can affect reproductive capacity. Hycomine compound should be given to a
pregnant woman only if clearly needed.
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Nonteratogenic Effects
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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 of dose. Chlorpromazine 0.7- 1.0 mg/ kg q6h, phenobarbital 2 mg/ kg q6h, and paregoric 2-
4 drops/ kg q4h, have been used to treat withdrawal symptoms in infants. The duration of therapy is 4- 28 days, with the dosages
decreased as tolerated.
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Nursing Mothers
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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.
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Pediatric Use
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Safety and effectiveness in children below the age of 2 years have not been established.
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DRUG INTERACTIONS
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Patients receiving other narcotic 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 ).
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ADVERSE REACTIONS
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- Respiratory System: Hydrocodone produces dose- related respiratory depression by acting directly on the 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.
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DRUG ABUSE AND DEPENDENCE
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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 narcotic. Psychic dependence, physical dependence, and tolerance may develop upon repeated
administration of narcotics; therefore, this drug 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 following
the administration of a narcotic 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- 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.
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OVERDOSAGE
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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
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Signs and Symptoms
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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 of N- acetylcysteine as an antidote.
In adults, hepatic toxicity has rarely been reported with acute overdoses of less than 10 g and fatalities with less than
15 g. 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- 72 hours post- ingestion.
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Treatment
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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 4 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 overdosage ingestions
for optimal results, but in any case, within 24 hours. Following recovery, there are no residual structural or functional
hepatic abnormalities.
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Hydrocodone
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Signs and Symptoms
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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.
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Treatment
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Primary attention should be given to the reestablishment of adequate respiratory exchange through a provision of a patent
airway and the institution of assisted or controlled ventilation. The narcotic antagonist naloxone HCl is a specific antidote
for respiratory depression which may result from overdosage or unusual sensitivity to narcotics including hydrocodone. Therefore
an appropriate dose of naloxone HCl should be administered, preferably by the IV route simultaneously with efforts at respiratory
resuscitation. For further information, see full prescribing information of naloxone HCl. An antagonist should not be administered
in the absence of clinically significant respiratory depression. Oxygen, IV 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.
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DOSAGE AND ADMINISTRATION
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Usual dosage, not less than 4 hours apart:
- Adults: 1 tablet 4 times a day.
- Children: 6 to 12 years: ½ tablet 4 times a day.
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PRODUCT IDENTIFICATION
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None Available |
PRODUCT LISTING - RATED THERAPEUTICALLY EQUIVALENT
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| tablet - oral - - -
|
| 100.0's |
$83.25 |
Hycomine Compound
Bristol- Myers Squibb Medical Imaging
|
00056004870 |
| 100.0's |
$117.13 |
Hycomine Compound
Endo Laboratories LLC
|
63481004870 |
| 500.0's |
$367.13 |
Hycomine Compound
Bristol- Myers Squibb Medical Imaging
|
00056004885 |
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