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Action/Kinetics:
Produces only mild euphoria, which is the reason it is used as a heroin withdrawal substitute and for maintenance programs. Produces physical dependence; withdrawal symptoms develop more slowly and are less intense but more prolonged than those associated with morphine. Does not produce sedation or narcosis. Not effective for preoperative or obstetric anesthesia. Only one-half as potent PO as when given parenterally.
Onset: 30-60 min.
Peak effects: 30-60 min.
Duration: 4-6 hr.
t
1/2: 15-30 hr. Both the duration and half-life increase with repeated use due to cumulative effects.
Uses:
Severe pain. Detoxification and maintenance of narcotic dependence.
Additional Contraindications:
IV use, liver disease, during pregnancy, in children, or in obstetrics (due to long duration of action and chance of respiratory depression in the neonate).
Special Concerns:
Use with caution during lactation.
Additional Side Effects:
Marked constipation, excessive sweating, pulmonary edema, choreic movements.
Laboratory Test Alterations:
Immunoglobulin G.
Drug Interactions:
[o]
Additional Drug Interactions:
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Cimetidine /
Respiratory and CNS depression
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Desipramine /
Desipramine blood levels
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Phenytoin /
Methadone effect R/T
liver metabolism
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Protease inhibitors /
Respiratory and CNS depression
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Rifampin /
Methadone effect R/T
liver metabolism; may precipitate withdrawal
How Supplied:
Injection: 10 mg/mL;
Oral Concentrate: 10 mg/mL;
Oral Solution: 5 mg/5 mL, 10 mg/5 mL;
Tablet: 5 mg, 10 mg, 40 mg
Dosage
?Tablets, Oral Solution, Oral Concentrate, Injection
Analgesia.
Adults, individualized: 2.5-10 mg q 3-4 hr, although higher doses may be necessary for severe pain or due to development of tolerance.
Narcotic withdrawal.
Initial: 15-20 mg/day PO (some may require 40 mg/day);
then, depending on need of the client, slowly decrease dosage.
Maintenance following narcotic withdrawal.
Adults, individualized, initial: 20-40 mg PO 4-8 hr after heroin is stopped;
then, adjust dosage as required up to 120 mg/day.