· Pharmacologic classification: piperidine-dione derivative.
· Therapeutic classification: sedative-hypnotic.
· Controlled substance schedule III.
· Pregnancy risk category B.
Available by prescription only
Tablets: 50 mg, 200 mg
Capsules: 300 mg
Indications, route and dosage
Adults: 200 to 400 mg P.O. 15 minutes before bedtime.
Children over age 12: 50 mg P.O. h.s., increased to 200 mg, if necessary. Maximum dosage is 400 mg/day.
Contraindications and precautions
Methyprylon is contraindicated in patients with known hypersensitivity to the drug. Drug should be used cautiously in patients with hepatic or renal failure, which may result in impaired elimination.
Use caution when long-term therapy is being considered in patients with low platelet or white blood cell counts, because drug may cause further depressions of blood count.
Use cautiously in patients with a history of mental depression, suicidal ideation or drug abuse.
Methyprylon may add to or potentiate the effects of alcohol, barbiturates, antihistamines, tranquilizers, narcotics, benzodiazepines and other CNS depressants.
· CNS: morning drowsiness, dizziness, vertigo, ataxia, pyrexia, headache, paradoxical excitation, nightmares, depression, confusion.
· CV: hypotension, syncope.
· DERM: rash, pruritus.
· EENT: diplopia, blurred vision.
· Gl: esophagitis, vomiting, nausea, diarrhea, constipation.
· HEMA: aplastic anemia, thrombocytopenic purpura, neutropenia.
· Other: cholestatic jaundice.
Note: Drug should be discontinued if hypersensitivity, paradoxical excitation, or acute organic brain syndrome occur or if platelet or neutrophil counts decline.
Overdose and treatment
Clinical manifestations of overdose include somnolence, confusion, coma, hypotension, shock, tachycardia, constricted pupils, edema, and respiratory depression.
Support respiration and cardiovascular function; empty stomach by emesis or lavage if ingestion was recent. Hemodialysis removes methyprylon. Excitation, seizures, delirium, and hallucinations may be seen upon recovery. Use barbiturates cautiously for control.
u Special considerations
· Methyprylon is not a first-line drug because of its potential for adverse reactions and toxicity.
· Like many other hypnotic agents, this drug is associated with diminished effectiveness during prolonged use. It is not recommended for use longer than 7 days.
· Periodic blood counts are advisable during long-term treatment to prevent possible adverse effects.
· Institute safely measures: supervised walking and raised bed rails, especially for elderly patients.
· Take precautions to prevent drug hoarding or selfdosing by patients who are depressed or suicidal or who have a history of drug abuse or addiction.
· Abrupt discontinuation may cause withdrawal symptoms; discontinue by reducing dose gradually.Continued use for long periods may cause addiction.
· Store in a cool, dry place.
Information for the patient
· Tell the patient to avoid the use of other CNS depressants unless prescribed. Warn the patient about the dangers of combining this drug with alcohol. An excessive depressant effect is possible even if the drug is taken the evening before ingestion of alcohol.
· Warn the patient not to increase dose or frequency unless prescribed, and not to abruptly stop taking the drug if he has been taking it for a prolonged period, because withdrawal symptoms may occur.
· Advise the patient not to attempt tasks that require mental alertness or physical coordination until the drug’s CNS effects are known.
· Advise the patient of potential for psychological or physical dependence with chronic use.
Elderly patients, especially those with hepatic or renal disease, may experience greater CNS depression. Use lowest effective dose.
Safe use in clildren under age 12 has not been established.
Safe use of methyprylon in breast-feeding women has not been established.