dolophine


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Related to dolophine: Methadose

methadone hydrochloride eptadone (UK)

Dolophine, Metadol, Methadone HCl Intensol, Methadose, Physeptone (UK), Synastone (UK)

Pharmacologic class: Opioid agonist

Therapeutic class: Analgesic, opioid detoxification adjunct

Controlled substance schedule II

Pregnancy risk category C

FDA Box Warning

• Deaths have occurred during drug initiation for opioid dependence. In some cases, deaths apparently resulted from respiratory or cardiac effects of methadone and too-rapid titration without considering drug accumulation. Make sure you understand drug's pharmacokinetics, and be vigilant during treatment initiation and dosage titration. Caution patients against self-medicating with CNS depressants at start of therapy.

• Prolonged QT intervals and serious arrhythmia (torsades de pointes) have occurred. Most cases involved patients being treated for pain with large, multiple daily doses.

• Federal law requires that when drug is used to treat opioid addiction in detoxification or maintenance programs, it can be dispensed only by treatment programs certified by the Substance Abuse and Mental Health Services Administration and approved by designated state authority. Certified treatment programs must dispense and use drug in oral form only and according to treatment requirements stipulated in Federal Opioid Treatment Standards. Failure to abide by regulations may lead to criminal prosecution, drug seizure, revocation of program approval, and injunction precluding program operation.

Action

Binds to and depresses opiate receptors in spinal cord and CNS, altering perception of and response to pain

Availability

Injection: 10 mg/ml

Oral solution: 5 mg/5 ml, 10 mg/5 ml, 10 mg/ml (concentrate)

Tablets: 5 mg, 10 mg

Tablets (dispersible diskettes): 40 mg

Indications and dosages

Opioid detoxification

Adults: Initially, 15 to 20 mg/day P.O. to suppress withdrawal. Additional doses may be necessary if symptoms aren't suppressed or if they reappear. Most patients are adequately stabilized on total daily dosage of 40 mg given in single or divided doses; however, some may need higher dosages. When patient is stable for 2 to 3 days, decrease dosage gradually at 2-day intervals. If patient can't tolerate oral doses, give I.M. or subcutaneously (usually at about 25% of total daily P.O. dosage) in two injections.

To maintain opioid abstinence

Adults: Oral dosage highly individualized based on control of abstinence symptoms without respiratory depression or marked sedation. If patient can't tolerate oral doses, give I.M. or subcutaneously (usually at about 25% of total daily P.O. dosage) in two injections.

Chronic and severe pain

Adults: For chronic pain, 2.5 to 10 mg P.O., I.M., or subcutaneously q 3 to 4 hours as needed; adjust dosage and dosing interval as needed. For severe chronic pain (as in terminal illness), 5 to 20 mg P.O. q 6 to 8 hours.

Children: Dosage individualized.

Contraindications

• Hypersensitivity to drug or other opioid agonists

Precautions

Use cautiously in:
• head trauma; severe renal, hepatic, or pulmonary disease; hypothyroidism; adrenal insufficiency; undiagnosed abdominal pain; prostatic hypertrophy; urethral stricture; toxic psychosis; Addison's disease; cor pulmonale; increased intracranial pressure; severe inflammatory bowel disease; severe CNS depression; hypercapnia; seizures; fever; alcoholism
• recent renal or hepatic surgery
• elderly or debilitated patients
• pregnant patients, patients in labor, or breastfeeding patients.

Administration

• Mix dispersible tablets with 120 ml of water or orange juice, citrus Tang, or other acidic fruit beverage.
• Dilute 10 mg/ml of oral solution with water or other liquid to at least 30 ml. In detoxification and maintenance of opioid withdrawal, dilute solution in at least 90 ml of fluid.
• When used parenterally, I.M. route is preferred. Rotate injection sites.
• For detoxification and maintenance, give oral solution only, to reduce potential for parenteral abuse, hoarding, and accidental ingestion.
• Know that patients who can't take oral drugs because of nausea or vomiting during detoxification or maintenance should be hospitalized and given methadone parenterally.

Adverse reactions

CNS: amnesia, anxiety, confusion, poor concentration, delirium, delusions, depression, dizziness, drowsiness, euphoria, fever, hallucinations, headache, insomnia, lethargy, light-headedness, malaise, psychosis, restlessness, sedation, clouded sensorium, syncope, tremor, seizures, coma

CV: hypotension, palpitations, edema, bradycardia, shock, cardiac arrest

EENT: visual disturbances

GI: nausea, vomiting, constipation, ileus, biliary tract spasm, gastroesophageal reflux, indigestion, dysphagia, dry mouth, anorexia

GU: urinary hesitancy, urinary retention, prolonged labor, difficult ejaculation, erectile dysfunction

Hematologic: anemia, leukopenia, thrombocytopenia

Musculoskeletal: joint pain

Respiratory: depressed cough reflex, hypoventilation, wheezing, asthma exacerbation, atelectasis, pulmonary edema, bronchospasm, respiratory depression or arrest, apnea

Skin: urticaria, pruritus, flushing, pallor, diaphoresis

Other: allergic reaction, hiccups, facial or injection site edema, pain, physical or psychological drug dependence, withdrawal symptoms

Interactions

Drug-drug.Amitriptyline, antihistamines, chloral hydrate, clomipramine, glutethimide, methocarbamol, MAO inhibitors, nortriptyline: increased CNS and respiratory depression

Anticholinergics: increased risk of severe constipation leading to ileus

Antiemetics, general anesthetics, phenothiazines, sedative-hypnotics, tranquilizers: coma, hypotension, respiratory depression, severe sedation

Ascorbic acid, phenytoin, phosphate, potassium, rifampin: decreased methadone blood level

Cimetidine, fluvoxamine, protease inhibitors: increased analgesia, CNS and respiratory depression

Diuretics: increased diuresis

Hydroxyzine: increased analgesia, CNS depression, and hypotension

Paregoric, loperamide: increased CNS depression, severe constipation

Naloxone: antagonism of methadone's analgesic, CNS, and respiratory effects

Naltrexone: induction or worsening of withdrawal symptoms (when given within 7 days of methadone)

Neuromuscular blockers: increased or prolonged respiratory depression

Drug-diagnostic tests.Amylase, liver function tests: increased levels

Drug-behaviors.Alcohol use: increased CNS and respiratory depression

Patient monitoring

• Assess patient for relief of severe, chronic pain requiring around-the-clock dosing. Tailor dosage to patient's pain level and drug tolerance.
• Monitor CNS, respiratory, and cardiovascular status.
• Watch for deepening sedation, which may increase with successive doses.
• Evaluate bowel and bladder function. Give laxatives if appropriate.
• Monitor detoxification treatment closely. Short-term detoxification shouldn't exceed 30 days; long-term detoxification, 180 days.
• Assess patient on maintenance therapy for successful rehabilitation. Know that maintenance therapy should be part of comprehensive treatment plan that includes medical, vocational rehabilitative, employment, educational, and counseling services.

Patient teaching

Instruct patient to promptly report severe adverse reactions.
• Tell patient he may take drug with food if GI upset occurs.
• Tell ambulatory patient to change positions slowly to avoid orthostatic hypotension.

Caution patient not to discontinue drug abruptly.
• Advise patient to avoid driving and other hazardous activities, because drug may cause drowsiness or dizziness.
• Tell female patient to inform prescriber if she's pregnant or breastfeeding.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and behaviors mentioned above.

methadone

A synthetic, relatively long-acting oral opioid analgesic used primarily for narcotic detoxification and controlled maintenance of heroin addiction.

Uses
Severe pain; antitussive.
 
Adverse effects
Lightheadedness, dizziness, anorexia, nausea and vomiting, dry mouth, sweating, drowsiness, hypotension, decreased intestinal motility, respiratory depression.

Inducers of methadone metabolism
Phenytoin, carbamazepine, rifampicin, fluconazole, some protease inhibitors—all via CYP3A4 induction.

Overdose effects
Respiratory depression, stupor, coma, loss of short-term memory.
 
Methadone overdose, autopsy findings
Airway obstruction, pulmonary oedema, aspiration of vomit, bronchopneumonia, cardiac arrest/failure.

Street terms
Amidone, dollies, dolls, done, fixer, fizzies, juice, juicer, medecina, meth-a-done, pixie, synthetic heroin, wafers.

Dolophine®

Methadone, see there.

dolophine

References in periodicals archive ?
The FDA also recommends that health care professionals who prescribe methadone carefully read and follow the prescribing information for Dolophine, the marketed methadone product, which was revised and approved on Nov.
Until 2004, only two drugs (disulfiram (Odyssey Pharmaceuticals' Antabuse) and naltrexone (Barr Pharmaceuticals' ReVia, generics)) were approved in the United States for treatment of alcohol dependence, and until 2002, only three drugs (methadone (Roxane Laboratories' Dolophine, generics), naltrexone, and levomethadyl (Roxane Laboratories' Orlaam)) were approved for treatment of opioid dependence; levomethadyl has since been pulled from the market.