INDICATIONS     CONTRA-INDICATIONS     DOSAGE     SIDE-EFFECTS     PREGNANCY     OVERDOSE     IDENTIFICATION     PATIENT INFORMATION

Logo EQUANIL® Tablets
EQUANIL® L.A. Tablets

SCHEDULING STATUS:
S5

PROPRIETARY NAME
(and dosage form):

EQUANIL® Tablets
EQUANIL® L.A. Tablets

COMPOSITION:
Each EQUANIL tablet contains
meprobamate 400 mg.
Each EQUANIL L.A. tablet contains meprobamate 400 mg as a slow release tablet.

Chemically, meprobamate is
2,2-di-(carbamoyl-oxymethyl)-pentane
EQUANIL L.A. tablets contain TARTRAZINE.

PHARMACOLOGICAL CLASSIFICATION:
Category A, 2.6 Tranquillizers

PHARMACOLOGICAL ACTION:
EQUANIL (meprobamate) is a carbamate derivative which has been shown to have effects at multiple sites in the central nervous system including the thalamus and limbic system.

Pharmacokinetics:
Meprobamate is well absorbed from the gastrointestinal tract. The drug is widely distributed in the body; there is little binding to plasma protein. Meprobamate undergoes extensive metabolism in the liver with 10 to 20% of the drug eliminated unchanged via the kidneys; the remainder is excreted as hydroxymeprobamate and as the glucoronide. Meprobamate can induce some hepatic microsomal enzymes, but is not clear whether the drug induces the enzymes responsible for its own metabolism.

INDICATIONS:
For the relief of anxiety and tension; as an adjunct in the treatment of various disease states in which anxiety and tension are manifested.
The effectiveness of EQUANIL and EQUANIL L.A. in long-term use, that is, more than 4 months, has not been assessed by systematic clinical studies.
The physician should reassess periodically the usefulness of the drug for the individual patient.

CONTRA-INDICATIONS:
Acute intermittent porphyria and allergic or idiosyncratic reactions to meprobamate or related compounds, such as carisoprodol, mebutamate or carbromal.

WARNINGS:
Addiction potential:
Physical dependence, psychological dependence, and abuse have occurred. Chronic intoxication from prolonged ingestion of, usually, greater than recommended doses is manifested by ataxia, slurred speech, and vertigo. Therefore, careful supervision of dose and amounts prescribed is advised, as well as avoidance of prolonged administration, especially for alcoholics and other patients with a known propensity for taking excessive quantities of drugs.
Sudden withdrawal of the drug after prolonged and excessive use may precipitate recurrence of pre-existing symptoms such as anxiety, anorexia, or insomnia, or withdrawal reactions such as vomiting, ataxia, tremors, muscle twitching, confusional states, hallucinosis, and rarely, convulsive seizures. Such seizures are more likely to occur in persons with central nervous system damage or pre-existent or latent convulsive disorders. Onset of withdrawal symptoms occurs usually within 12 to 48 hours after discontinuation of meprobamate; symptoms usually cease within the next 12 to 48 hour period. To avoid withdrawal symptoms, it is recommended that meprobamate not be abruptly discontinued in these situations; rather, a gradual tapering of the dose be attempted. Alternatively, a short-acting barbiturate may be substituted then gradually withdrawn.

Usage in Pregnancy and Lactation:
An increased risk of congenital malformations associated with the use of minor tranquillizers (meprobamate, chlordiazepoxide, and diazepam) during the first trimester of pregnancy has been suggested in several studies. Because use of these drugs is rarely a matter of urgency, their use during this period should almost always be avoided. The possibility that a woman of childbearing potential may be pregnant at the time of institution of therapy should be considered. Patients should be advised that if they become pregnant during therapy or intend to become pregnant they should communicate with their physicians about the desirability of discontinuing the drug. Meprobamate passes the placental barrier. It is present both in umbilical-cord blood at or near maternal plasma levels and in breast milk of lactating mothers at concentrations two to four times that of maternal plasma. When use of meprobamate is contemplated in breastfeeding patients, the drug’s higher concentration in breast milk as compared to maternal plasma levels should be considered.

Usage in Children:
Meprobamate should not be administered to children under 6 years of age since there is a lack of documented evidence of safety and effectiveness.
EQUANIL L.A. tablets contains F D and C Yellow No. 5 (tartrazine) which may cause allergic-type reactions (including bronchial asthma) in certain susceptible individuals. Although the overall incidence of tartrazine sensitivity in the general population is currently thought to be low, it is frequently seen in patients who have aspirin sensitivity.

DOSAGE AND DIRECTIONS FOR USE:
EQUANIL tablets: Usual adult dose is 1 200-1 600 mg/day in divided doses. Doses greater than 2 400 mg/day are not recommended. The usual dose of children ages 6-12 years is 100-200 mg two to three times daily. Not recommended for children under 6 years.

EQUANIL L.A. tablets: Usual adult dose is 1 tablet twice daily.

SIDE-EFFECTS AND SPECIAL PRECAUTIONS:
SIDE-EFFECTS:
Central nervous system:
Drowsiness, ataxia, dizziness, slurred speech, headache, vertigo, weakness, paresthesias, impairment of visual accommodation, euphoria, overstimulation, paradoxical excitement, fast EEG activity.

Gastrointestinal:
Nausea, vomiting, diarrhoea.

Cardiovascular:
Palpitation, tachycardia, various forms of arrhythmia, transient ECG changes, syncope, hypotensive crises.

Allergic or Idiosyncratic:
Milder reactions are characterized by an itchy, urticarial, or erythematous maculopapular rash which may be generalized or confined to the groin. Other reactions have included leukopaenia, acute nonthrombocytopaenic purpura, petechiae, ecchymoses, eosinophilia, peripheral oedema, adenopathy, fever, fixed drug eruption with cross reaction to carisoprodol, and cross sensitivity between meprobamate/mebutamate and meprobamate/carbromal.
More severe hypersensitivity reactions, rarely reported, include hyperpyrexia, chills, angioneurotic oedema, bronchospasm, oliguria, and anuria. Also, anaphylaxis, exfoliative dermatitis, stomatitis and proctitis. Stevens-Johnson syndrome and bullous dermatitis have occurred.

Haematologic (See also “Allergic or Idiosyncratic”):
Agranulocytosis, aplastic anaemia have been reported, although no casual relationship has been established, and thrombocytopaenic purpura.

Other:
Exacerbation of porphyric symptoms.

SPECIAL PRECAUTIONS:
The least effective dose should be administered, particularly to elderly and/or debilitated patients in order to preclude oversedation.
Meprobamate is metabolized in the liver and excreted by the kidney; to avoid its excess accumulation, caution should be exercised in the administration to patients with compromised liver or kidney function.
Meprobamate occasionally may precipitate seizures in epileptic patients. The drug should be prescribed cautiously and in small quantities to patients with suicidal tendencies.

Potentially Hazardous Tasks:
Patients should be warned that meprobamate may impair the mental or physical abilities required for performance of potentially hazardous tasks such as driving or operating machinery.

Additive Effects:
Since CNS-suppressant effects of meprobamate and alcohol or meprobamate and other psychotropic drugs may be additive, appropriate caution should be exercised with patients who take more than one of these agents simultaneously.

Medicine Interactions:
The enzyme-inducing effect of meprobamate may decrease the activity of some drugs which are metabolized by the liver, including digitoxin and endogenous and exogenous estrogens. The risk of breakthrough bleeding, spotting, or pregnancy in women taking oral contraceptives, is therefore increased when such women are also taking meprobamate.

Laboratory Test Interactions:
Meprobamate may cause falsely high urinary 17-ketosteroid and 17-ketogenic steroid levels in the Zimmerman reaction and 17-hydroxycorticosteroid levels in the modified Glenn-Nelson technique.

Addiction potential: See “WARNINGS”.

Usage in Pregnancy and Lactation: See “WARNINGS”.

Usage in children: See “WARNINGS”.

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT:
Suicidal attempts with meprobamate have resulted in drowsiness, lethargy, stupor, ataxia, coma, shock, vasomotor, and respiratory collapse.
Some suicidal attempts have been fatal.
General supportive measures should be employed along with gastric lavage, I.V. fluids should be administered, and an adequate airway maintained.
Diuresis, osmotic (mannitol) diuresis, peritoneal dialysis, and haemodialysis have been used successfully. Careful monitoring of urinary output is necessary and caution should be taken to avoid overhydration. Relapse and death, after initial recovery, have been attributed to incomplete gastric emptying and delayed absorption.

IDENTIFICATION:
EQUANIL tablets are white, flat tablets with bevelled edges containing not more than a slight characteristic odour, having the word “WYETH’ impressed on both halves of the scored face and the letter “W”within a shield impressed on the other face.

EQUANIL L.A. tablets are yellow with the letter “W’within a shield imprinted on both sides.

PRESENTATION:
EQUANIL tablets: Bottles of 100 and 250 tablets.
EQUANIL L.A. tablets: Bottles of 25 tablets.

STORAGE DIRECTIONS:
Store in a cool (below 25 °C), dry place.
Keep out of reach of children.

REFERENCE NUMBERS:
EQUANIL tablets B1340 (Act 101/1965)
EQUANIL L.A. tablets B1341 (Act 101/1965)

NAME AND BUSINESS ADDRESS OF APPLICANT:
AKROMED PRODUCTS
Electron Avenue ISANDO 1600

Trademark and product,
under licence from
WYETH-AYERST LABORATORIES. U.S.A.

DATE OF PUBLICATION OF THIS PACKAGE INSERT:
6 December 1984
        24460 IG608
        Davbar Dbn.

SAEPI HOME PAGE      TRADE NAME INDEX      GENERIC NAME INDEX      FEEDBACK
Information presented by Malahyde Information Systems © Copyright 1996-2000