DOLOPHINE CII

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DOLOPHINE

Addiction/dependence
Narcotic analgesics
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Generic Name and Formulations:

Methadone HCl 5mg, 10mg; scored tabs.

Select therapeutic use:

Indications for DOLOPHINE:

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.

Adult:

See full labeling. 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 withdrawal 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. Pregnancy: may need dose increase. Concomitant use or discontinuation of CYP3A4, CYP2B6, CYP2C19, CYP2C9, and CYP2D6 inhibitors or inducers: monitor closely and consider dose adjustments (see full labeling).

Children:

<18yrs: not established.

Contraindications:

Significant respiratory depression. Acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment. Known or suspected GI obstruction, including paralytic ileus.

Warnings/Precautions:

May only be dispensed by opioid treatment programs certified by the Substance Abuse and Mental Health Services Administration and approved by designated state authority. Life-threatening respiratory depression; monitor within first 24–72hrs of initiating therapy and following dose increases. Accidental exposure may cause fatal overdose (esp. in children). COPD, cor pulmonale, decreased respiratory reserve, hypoxia, hypercapnia, or pre-existing respiratory depression; monitor and consider non-opioid analgesics. Abuse potential (monitor). Life-threatening QT prolongation and serious arrhythmia; monitor for cardiac rhythm changes in high-risk patients (eg. cardiac hypertrophy, concomitant diuretic use, hypokalemia, hypomagnesemia), history of cardiac conduction abnormalities, and those taking drugs affecting cardiac conduction. Adrenal insufficiency. Head injury. Increased intracranial pressure, brain tumors; monitor. Seizure disorders. CNS depression. Impaired consciousness, coma, shock; avoid. Biliary tract disease. Acute pancreatitis. Drug abusers. Renal or severe hepatic impairment. Reevaluate periodically. Avoid abrupt cessation. Elderly. Cachectic. Debilitated. Labor & delivery: not recommended. Pregnancy; potential neonatal opioid withdrawal syndrome during prolonged use. Nursing mothers: monitor infants.

Interactions:

Increased risk of hypotension, respiratory depression, sedation with benzodiazepines or other CNS depressants (eg, non-benzodiazepine sedatives/hypnotics, anxiolytics, general anesthetics, phenothiazines, tranquilizers, muscle relaxants, antipsychotics, alcohol, other opioids); reserve concomitant use in those for whom alternative options are inadequate; limit dosages/durations to minimum required; monitor. During or within 14 days of MAOIs: not recommended. Risk of serotonin syndrome with serotonergic drugs (eg, SSRIs, SNRIs, TCAs, triptans, 5-HT3 antagonists, mirtazapine, trazodone, tramadol, MAOIs, linezolid, IV methylene blue); monitor and discontinue if suspected. Avoid concomitant mixed agonist/antagonist opioids (eg, butorphanol, nalbuphine, pentazocine) or partial agonist (eg, buprenorphine); may reduce effects and precipitate withdrawal symptoms. Potentiated by macrolides, azole antifungals, protease inhibitors, fluvoxamine, sertraline, and other CYP3A4, CYP2B6, CYP2C19, CYP2C9, or CYP2D6 inhibitors. Antagonized by rifampin, carbamazepine, phenytoin, St. John's Wort, phenobarbital, abacavir, amprenavir, darunavir+ritonavir, efavirenz, nelfinavir, nevirapine, ritonavir, telaprevir, lopinavir+ritonavir, saquinavir+ritonavir, tipranivir+ritonavir, and other CYP3A4, CYP2B6, CYP2C19, or CYP2C9 inducers. Caution with drugs that prolong the QT interval (eg, Class I and III antiarrhythmics, neuroleptics, TCAs, CCBs) and drugs capable of inducing electrolyte disturbances (eg, diuretics, laxatives, mineralcorticoid hormones). May potentiate zidovudine, desipramine. May antagonize diuretics, didanosine, stavudine; monitor. Paralytic ileus may occur with anticholinergics. Diphenhydramine, doxylamine, clomipramine, chlorpromazine, thioridazine, quetiapine, verapamil may cause false (+) methadone drug screens.

Pharmacological Class:

Opioid agonist.

Adverse Reactions:

Lightheadedness, dizziness, sedation, nausea, vomiting, sweating; respiratory depression, severe hypotension, syncope, QT prolongation.

Metabolism:

Hepatic (CYP3A4, CYP2B6, CYP2C19; also CYP2C9 and CYP2D6).

Elimination:

Renal, fecal.

REMS:

YES

Generic Availability:

YES

How Supplied:

Tabs—100

DOLOPHINE 10mg tablets (Qty:120)

appx. price $81.00

Indications for DOLOPHINE:

Management of pain severe enough to require daily, around-the-clock, long-term opioid treatment and for which alternative treatments are inadequate.

Limitations Of use:

Not for use as an as-needed (prn) analgesic. Use only if alternative treatment options (eg, non-opioid analgesics, immediate-release opioids) are ineffective, not tolerated, or otherwise inadequate to provide sufficient management of pain.

Adult:

See full labeling. Use lowest effective dose for shortest duration. 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. Individualize. Opioid-naive: initially 2.5mg every 8–12hrs. May increase dose every 3–5 days; titrate slowly. Conversion from other oral opioids: discontinue all other around-the-clock opioids when Dolophine is initiated; deaths have occurred in opioid-tolerant patients during conversion (see full labeling). Conversion from parenteral methadone: use a 1:2 mg for parenteral to oral methadone ratio. Pregnancy: may need dose increase. Concomitant use or discontinuation of CYP3A4, CYP2B6, CYP2C19, CYP2C9, and CYP2D6 inhibitors or inducers: monitor closely and consider dose adjustments (see full labeling). Withdraw gradually by 15–50% every 2–4 days.

Children:

<18yrs: not established.

Contraindications:

Significant respiratory depression. Acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment. Known or suspected GI obstruction, including paralytic ileus.

Warnings/Precautions:

Life-threatening respiratory depression; monitor within first 24–72hrs of initiating therapy and following dose increases. Accidental exposure may cause fatal overdose (esp. in children). COPD, cor pulmonale, decreased respiratory reserve, hypoxia, hypercapnia, or pre-existing respiratory depression; monitor and consider non-opioid analgesics. Abuse potential (monitor). Life-threatening QT prolongation and serious arrhythmia; monitor for cardiac rhythm changes in high-risk patients (eg. cardiac hypertrophy, concomitant diuretic use, hypokalemia, hypomagnesemia), history of cardiac conduction abnormalities, and those taking drugs affecting cardiac conduction. Adrenal insufficiency. Head injury. Increased intracranial pressure, brain tumors; monitor. Seizure disorders. CNS depression. Impaired consciousness, coma, shock; avoid. Biliary tract disease. Acute pancreatitis. Drug abusers. Renal or severe hepatic impairment. Reevaluate periodically. Avoid abrupt cessation. Elderly. Cachectic. Debilitated. Labor & delivery: not recommended. Pregnancy; potential neonatal opioid withdrawal syndrome during prolonged use. Nursing mothers: monitor infants.

Interactions:

Increased risk of hypotension, respiratory depression, sedation with benzodiazepines or other CNS depressants (eg, non-benzodiazepine sedatives/hypnotics, anxiolytics, general anesthetics, phenothiazines, tranquilizers, muscle relaxants, antipsychotics, alcohol, other opioids); reserve concomitant use in those for whom alternative options are inadequate; limit dosages/durations to minimum required; monitor. During or within 14 days of MAOIs: not recommended. Risk of serotonin syndrome with serotonergic drugs (eg, SSRIs, SNRIs, TCAs, triptans, 5-HT3 antagonists, mirtazapine, trazodone, tramadol, MAOIs, linezolid, IV methylene blue); monitor and discontinue if suspected. Avoid concomitant mixed agonist/antagonist opioids (eg, butorphanol, nalbuphine, pentazocine) or partial agonist (eg, buprenorphine); may reduce effects and precipitate withdrawal symptoms. Potentiated by macrolides, azole antifungals, protease inhibitors, fluvoxamine, sertraline, and other CYP3A4, CYP2B6, CYP2C19, CYP2C9, or CYP2D6 inhibitors. Antagonized by rifampin, carbamazepine, phenytoin, St. John's Wort, phenobarbital, abacavir, amprenavir, darunavir+ritonavir, efavirenz, nelfinavir, nevirapine, ritonavir, telaprevir, lopinavir+ritonavir, saquinavir+ritonavir, tipranivir+ritonavir, and other CYP3A4, CYP2B6, CYP2C19, or CYP2C9 inducers. Caution with drugs that prolong the QT interval (eg, Class I and III antiarrhythmics, neuroleptics, TCAs, CCBs) and drugs capable of inducing electrolyte disturbances (eg, diuretics, laxatives, mineralcorticoid hormones). May potentiate zidovudine, desipramine. May antagonize diuretics, didanosine, stavudine; monitor. Paralytic ileus may occur with anticholinergics. Diphenhydramine, doxylamine, clomipramine, chlorpromazine, thioridazine, quetiapine, verapamil may cause false (+) methadone drug screens.

Pharmacological Class:

Opioid agonist.

Adverse Reactions:

Lightheadedness, dizziness, sedation, nausea, vomiting, sweating; respiratory depression, severe hypotension, syncope, QT prolongation.

Metabolism:

Hepatic (CYP3A4, CYP2B6, CYP2C19; also CYP2C9 and CYP2D6).

Elimination:

Renal, fecal.

REMS:

YES

Generic Availability:

YES

How Supplied:

Tabs—100

DOLOPHINE 10mg tablets (Qty:120)

appx. price $81.00