Methadose and generics; previously available as Dolophine
Narcotic, analgesic

C	2	Yes	Yes	No
Key

• Tabs: 5, 10 mg
• Tabs, dispersible (Methadose and generics): 40 mg
• Oral solution: 5 mg/5 mL (500 mL), 10 mg/5 mL (500 mL); contains 8% alcohol
• Concentrated oral solution (Methadose and generics): 10 mg/mL (30 mL); may contain propylene glycol and parabens and may be sugar free
• Injection: 10 mg/mL (20 mL), contains 0.5% chlorobutanol

Dosing

• Analgesia (initial doses; see remarks):
  • Child: 0.7 mg/kg/24 hr ÷ Q4–6 hr PO, SC, IM, or IV PRN pain; max. dose: 10 mg/dose
  • Adult: 2.5–10 mg/dose Q8–12 hr PO, SC, IM, or IV PRN pain
• Detoxification or maintenance: See package insert.

Notes

• Unintentional overdoses have resulted in fatalities and severe adverse events such as respiratory depression and cardiac arrhythmias. Use with caution in hepatic ( avoid in severe cases) and biliary tract impairment. May cause respiratory depression, sedation, increased intracranial pressure, hypotension, and bradycardia. Cardiac QT interval prolongation and serious arrhythmias have occurred mostly with higher doses; avoid use with other medications that may prolong QT interval. Nystagmus, strabismus, hypoglycemia, hypokalemia, hypomagnesemia, and weight gain have been reported.
• Average T_1/2: Children 19 hr, and adults 35 hr. Duration of action PO is 6–8 hr initially and 22–48 hr after repeated doses. Respiratory effects last longer than analgesia. Accumulation may occur with continuous use, making it necessary to adjust dose.
• Nevirapine may decrease serum levels of methadone. Fatalities have been reported with abuse in combination with benzodiazepines. Serotonin syndrome has been reported with use with selective serotonin reuptake inhibitors (SSRIs), serotonin norepinephrine reuptake inhibitor (SNRIs), TCAs, 5-HT3 antagonists, MAO inhibitors, and drugs that affect the serotonergic neurotransmitter system (e.g., trazodone, tramadol). Methadone is a substrate for CYP 450 3A3/4, 2D6, and 1A2 and inhibitor of 2D6.
• See Chapter 6 for equianalgesic dosing and onset of action. Adjust dose in renal failure (see Chapter 31 ) .
• A Risk Evaluation and Mitigation Strategy (REMS) is required for healthcare providers to ensure the benefits outweigh the risks of addiction, abuse, and misuse. See www.fda.gov/OpioidAnalgesicREMSBlueprint or call 1-800-503-0784.