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| Medication | Dosage form | Mechanism of action | DEA schedule | Application in primary care |
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| Methadone | Tablet: 5 mg, 10 mg
Tablet for suspension: 40 mg
Oral concentrate: 10 mg/mL
Oral solution: 5 mg/5 mL, 10 mg/5 mL
Injection: 10 mg/mL | Mu agonist at the mu opioid receptor and also possible antagonist at the N-methyl-D-aspartate receptor | CII | Based on federal regulations primary care integration into/or linkage with Opioid Treatment Programs is required |
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| Buprenorphine-naloxone | Sublingual film: buprenorphine/naloxone 2 mg/0.5 mg, 4 mg/1 mg, 8 mg/2 mg, and 12 mg/3 mg
Sublingual tablet: buprenorphine/naloxone 1.4 mg/0.36 mg, 2 mg/0.5 mg, 5.7 mg/1.4 mg, and 8 mg/2 mg | Buprenorphine: Partial mu agonist at the mu opioid receptor and an antagonist at the kappa opioid receptor
Naloxone: antagonist at mu opioid receptor and produces withdrawal signs/symptoms | CIII | To prescribe buprenorphine in a primary care setting, a physician must obtain a waiver from
SAMHSA and be issued an additional registration number by the DEA (see http://www.dpt.samhsa.gov/ for details) |
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| Buprenorphine | | Partial mu agonist at the mu opioid receptor and an antagonist at the kappa opioid receptor | CIII | Buprenorphine without naloxone products are indicated only for patients with documented hypersensitivity to naloxone |
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| Naltrexone | Tablets: 25 mg, 50 mg, and 100 mg
Extended-release injectable suspension: 380 mg/vial | Opioid antagonist with highest affinity for the mu opioid receptor Little or no opioid agonist activity
Produces some pupillary constriction by an unknown mechanism | n/a | Provided by prescription; naltrexone provides a blockade of opioid receptors, reduces cravings, and diminishes the rewarding effects of alcohol and opioids
Extended-release injectable naltrexone is indicated for the prevention of relapse to opioids or alcohol |
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| Acamprosate | Delayed-release tablet: 333 mg | Mechanism not completely understood; studies suggest that acamprosate may interact with glutamate and GABA neurotransmitter systems centrally | n/a | Provided by prescription; acamprosate reduces symptoms of protracted abstinence associated with chronic alcohol exposure and alcohol withdrawal |
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| Disulfiram | Tablet: 250 mg, 500 mg | Blocks oxidation of alcohol at the acetaldehyde stage | n/a | When taken in combination with alcohol, disulfiram causes severe physical reactions, including nausea, flushing, and heart palpitations
The knowledge that such a reaction is likely if alcohol is consumed acts as a deterrent to drinking |
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| Naloxone | Injection: 0.4 mg/mL, 1 mg/mL, and 0.4 mg/0.4 mg | Opioid antagonist;
in vitro studies suggest that it antagonizes opioid effects by competing for the mu, kappa, and sigma opiate receptor sites in the CNS, with the greatest affinity for the mu receptor | n/a | Naloxone is the antidote to opioid toxicity
It reverses the respiratory depression induced by opioids
It has no psychoactive properties and no abuse potential
To be effective naloxone should be administered as soon as possible when opioid overdose is suspected, usually prior to transport to an emergency department Because of this naloxone should be prescribed to persons at risk of opioid overdose for emergency administration
Education and training should be provided to the patient and family members on how to reduce risk, recognize, and respond to overdose appropriately Naloxone is typically dispensed in an injectable form and may require prescription of syringes |
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