Generic Name and Formulations:
Methadone HCl 5mg, 10mg; scored tabs.
Company:
Roxane Laboratories, Inc.
| 12/27/12 |
| Updated with limitations of use. |
Detoxification treatment of opioid addiction (heroin or other morphine-like drugs). For maintenance treatment of opioid addiction (heroin or other morphine-like drugs), in conjunction with appropriate social and medical services.
See literature. Particular vigilance is necessary during treatment initiation, during conversion from one opioid to another, and during dose titration. Peak respiratory depressant effects typically occur later, and persist longer than peak analgesic effects. Induction/initial dosing: 20–30mg, an additional 5–10mg may be given if withdrawal symptoms not suppressed. Total daily dose on first day of treatment: max 40mg. Adjust dose cautiously. Short-term detoxification: titrate to total daily dose of 40mg in divided doses, continue for 2–3 days, then gradually decrease dose. Maintenance treatment: titrate to dose at which opioid symptoms are prevented for 24hrs, drug hunger/craving is reduced, euphoric effects are blocked/attenuated, and patient is tolerant to sedative effects; usual range: 80–120mg/day. Medically supervised withdrawal after a period of maintenance treatment: dose reduction should be <10% of maintenance dose, 10–14 day intervals should elapse between dose reductions.
<18yrs: not established.
Opioid.
Significant respiratory depression. Acute or severe bronchial asthma (in the absence of resuscitative equipment or in unmonitored settings). Known or suspected paralytic ileus.
May only be dispensed by opioid treatment programs certified by the Substance Abuse and Mental Health Services Administration and approved by designated state authority. Deaths, cardiac and respiratory, have been reported during initiation and conversion of pain patients to methadone from other opioids. A high degree of opioid tolerance does not eliminate the possibility of overdose, iatrogenic or otherwise. Increased risk of respiratory depression with COPD, cor pulmonale, CNS depression, coma, head injury, increased intracranial pressure. Cardiac hypertrophy, concomitant diuretic use, hypokalemia, hypomagnesemia: increased risk of QT prolongation; monitor cardiovascular status. Impaired renal or hepatic function. GI obstruction. Acute pancreatitis. Biliary tract disease. Severe volume depletion. Seizure disorders. Drug abusers. Avoid abrupt cessation. Elderly. Cachectic. Debilitated. Pregnancy (Cat.C). Newborns born to mothers taking opioids regularly. Obstetric analgesia, nursing mothers: not recommended.
Increased CNS effects with concomitant CNS depressants, alcohol. Withdrawal symptoms with concomitant opioid antagonists, mixed agonist/antagonists, partial agonists (eg, naloxone, naltrexone, pentazocine, nalbuphine, butorphanol, buprenorphine). Potentiated by CYP3A4 and/or CYP2C9 inhibitors (eg, ketoconazole, itraconazole, voriconazole, clarithromycin, telithromycin, erythromycin, sertraline, fluvoxamine); monitor, adjust dose. Antagonized by abacavir, amprenavir, darunavir+ritonavir, telaprevir, saquinavir+ritonavir, tipranivir+ritonavir, efavirenz, nelfinavir, nevirapine, ritonavir, lopinavir+ritonavir, rifampin, phenytoin, St. John's Wort, phenobarbital, carbamazepine, other CYP450 inducers; monitor; adjust methadone dose. Potentiates zidovudine, desipramine. Antagonizes didanosine, stavudine. Concomitant MAOIs: perform sensitivity test with small doses of methadone; monitor. Caution with drugs that prolong the QT interval (eg, Class I and III antiarrhythmics, neuroleptics, tricyclic antidepressants, calcium channel blockers) and drugs capable of inducing electrolyte disturbances (eg, diuretics, laxatives, mineralcorticoid hormones). Increased risk of urinary retention and/or severe constipation with anticholinergics; monitor.
Heroin withdrawal, lightheadedness, dizziness, sedation, nausea, vomiting, sweating; respiratory depression, systemic hypotension; QT interval prolongation, torsades de pointes (esp. with high doses).
Hepatic (CYP3A4, CYP2B6, CYP2C19; also CYP2C9 and CYP2D6).
Renal, fecal.
YES
Tabs—100
| 12/27/12 |
| Updated with limitations of use. |
Moderate to severe pain when a continuous, around-the-clock opioid analgesic is needed for an extended period of time. Not for use: as an as-needed (prn) analgesic, for pain that is mild or not expected to persist for an extended period of time, for acute pain, or for postoperative pain.
See literature. Particular vigilance is necessary during treatment initiation, during conversion from one opioid to another, and during dose titration. Peak respiratory depressant effects typically occur later, and persist longer than peak analgesic effects. Opioid non-tolerant: initially 2.5–10mg every 8–12hrs, slowly titrated to effect. Conversion from parenteral methadone to oral methadone: initially use 1:2 dose ratio. Switching to methadone from other chronic opioids: equianalgesic methadone dosing varies; dosing should not be solely based on conversion tables; individualize.
<18yrs: not established.
Opioid.
Significant respiratory depression. Acute or severe bronchial asthma (in the absence of resuscitative equipment or in unmonitored settings). Known or suspected paralytic ileus.
Deaths, cardiac and respiratory, have been reported during initiation and conversion of pain patients to methadone from other opioids. A high degree of opioid tolerance does not eliminate the possibility of overdose, iatrogenic or otherwise. Increased risk of respiratory depression with COPD, cor pulmonale, CNS depression, coma, head injury, increased intracranial pressure. Cardiac hypertrophy, concomitant diuretic use, hypokalemia, hypomagnesemia: increased risk of QT prolongation; monitor cardiovascular status. Impaired renal or hepatic function. GI obstruction. Acute pancreatitis. Biliary tract disease. Severe volume depletion. Seizure disorders. Drug abusers. Avoid abrupt cessation. Elderly. Cachectic. Debilitated. Pregnancy (Cat.C). Newborns born to mothers taking opioids regularly. Obstetric analgesia, nursing mothers: not recommended.
Increased CNS effects with concomitant CNS depressants, alcohol. Withdrawal symptoms with concomitant opioid antagonists, mixed agonist/antagonists, partial agonists (eg, naloxone, naltrexone, pentazocine, nalbuphine, butorphanol, buprenorphine). Potentiated by CYP3A4 and/or CYP2C9 inhibitors (eg, ketoconazole, itraconazole, voriconazole, clarithromycin, telithromycin, erythromycin, sertraline, fluvoxamine); monitor, adjust dose. Antagonized by abacavir, amprenavir, darunavir+ritonavir, telaprevir, saquinavir+ritonavir, tipranivir+ritonavir, efavirenz, nelfinavir, nevirapine, ritonavir, lopinavir+ritonavir, rifampin, phenytoin, St. John's Wort, phenobarbital, carbamazepine, other CYP450 inducers; monitor; adjust methadone dose. Potentiates zidovudine, desipramine. Antagonizes didanosine, stavudine. Concomitant MAOIs: perform sensitivity test with small doses of methadone; monitor. Caution with drugs that prolong the QT interval (eg, Class I and III antiarrhythmics, neuroleptics, tricyclic antidepressants, calcium channel blockers) and drugs capable of inducing electrolyte disturbances (eg, diuretics, laxatives, mineralcorticoid hormones). Increased risk of urinary retention and/or severe constipation with anticholinergics; monitor.
Lightheadedness, dizziness, sedation, nausea, vomiting, sweating; respiratory depression, systemic hypotension; QT interval prolongation, torsades de pointes (esp. with high doses).
Hepatic (CYP3A4, CYP2B6, CYP2C19; also CYP2C9 and CYP2D6).
Renal, fecal.
YES
Tabs—100