Addiction_Medication_table_s

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Chamberlain College of Nursing *

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NR 546 ADV

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Biology

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Oct 30, 2023

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docx

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Drug Name Indication Neurotransmitter(s) Affected Target Symptoms Half-life (T1/2), Metabolism (CYP 450 enzyme) Notable Side Effects (link to NT or affected brain circuit) Initial Dosing Considerations Specific lifespan considerations (age, pregnancy, breastfeeding) Buprenorphine (Subutex) mu opioid receptor partial agonist Maintenance treatment of opioid dependence • Metabolized by CYP450 3A4 • Elimination half- life of sublingual buprenorphine is 24–42 hours • Elimination half- life of naloxone is 2–12 hours • Headache, constipation, nausea • Oral hypoesthesia, glossodynia • Orthostatic hypotension • Implant specifi c: insertion site pain, pruritis, erythema Binding at mu opioid receptors causes side effects. • Sublingual: 8–32 mg/day • Implant: 4 implants intended to be in place for 6 months -use with caution in elderly patients -not recommended in breast feeding mothers -may be preferable to methadone in pregnant women Buprenorphine/Naloxone (Suboxone, Zubsolv, Bunavail) mu opioid receptor partial agonist Maintenance treatment of opioid dependence • Metabolized by CYP450 3A4 • Elimination half- life of sublingual buprenorphine is 24–42 hours • Elimination half- life of naloxone is 2–12 hours • Headache, constipation, nausea • Oral hypoesthesia, glossodynia • Orthostatic hypotension • Implant specifi c: insertion site pain, pruritis, erythema Binding at mu opioid receptors causes side effects. -Naloxone has no bio availability when • Sublingual: 8–32 mg/day -use with caution in elderly patients -not recommended in breast feeding mothers -may be preferable to methadone in pregnant women

administered sublingually. However, if suboxone is injected, naloxone will block intended euphoric effect. Naloxone acts as a deterrent against injection of the drug. Methadone (Dolophine, Methadose) full µ-opioid receptor (MOR) agonist and N- methyl-d-aspartate (NMDA) receptor antagonist Maintenance treatment of opioid dependence Cytochrome P450 enzymes, primarily CYP3A4, CYP2B6, and CYP2C19 and to a lesser extent CYP2C9, CYP2C8, and CYP2D6, are responsible for conversion of methadone to EDDP Due to interindividual differences in pharmacokinetics, estimates of methadone's half- life have ranged from 15–207 hours with official monographs listing it between 7-59 hours  Restlessness  Upset stomach or vomiting  Slow breathing  Itchy skin  Constipation  Sexual problems  Weight gain  Sleep changes  Appetite changes  Headache  Stomach pain  Dry mouth  Flushing  Mood changes  Vision problems -For opioid addiction 20-30 mg daily -dose is titrated up as tolerated, it is possible to be on 150-200 mg of methadone -Not recommended in breast feeding moms - has not been studied in pregnant patients -use with caution in elderly patients

Naltrexone (Revia, Vivitrol) opioid receptor antagonist • Alcohol dependence • Blockade of effects of exogenously administered opioids (oral) Prevention of relapse to opioid dependence (injection) Elimination half-life of oral naltrexone is approximately 13 hours Elimination half-life of naltrexone via injection is 5–10 days -independent of CYP450 enzymes Nausea, vomiting, decreased appetite Dizziness, dysphoria, anxiety Injection site reactions (pain, tenderness, pruritis, induration, swelling, erythema, or bruising); in some cases injection site reactions may be very severe -causes side effects by blockade of mu opioid receptors Oral: 50 mg/day or 100 mg on Mon and Wed and 150 mg on Fri Injection: 380 mg every 4 weeks -some elderly patients may tolerate lower doses, use with caution. -not recommended in pregnant women. Pregnant women who need to stop drinking may consider behavioral therapy before pharmacotherapy Acamprosate (Campral) glutamate multi- modal (Glu-MM • Maintenance of alcohol abstinence Terminal half-life 20– 33 hours Excreted unchanged via the kidneys Diarrhea, nausea Anxiety, depression Theoretically, behavioral side effects due to changes in neurotransmitter concentrations at receptors in parts of the brain and body other than those that cause therapeutic 666 mg three times daily (>60 kg) • 666 mg two times daily (<60 kg) -elderly patients may tolerate lower doses, consider monitoring renal function - Unknown if acamprosate is secreted in human breast milk, but all psychotropics assumed to be secreted in breast milk

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actions Gastrointestinal side effects may be related to large doses of a drug that is an amino acid derivative, increasing osmotic absorption in the gastrointestinal tract Disulfiram (Antabuse) Alcohol dependence treatment Irreversibly inhibits aldehyde dehydrogenase, the enzyme involved in second-stage metabolism of alcohol If alcohol is consumed by a patient taking disulfiram, toxic levels of acetaldehyde Build-up, causing unpleasant side effects • Half-life of parent drug is 60–120 hours • Half-life of metabolites is 13.9 hours (diethyldithiocarba mate) and 8.9 hours (carbon disulfide) • Metallic taste, dermatitis, sedation • Flushing, headache, tachycardia, nausea, vomiting (if alcohol is consumed) When alcohol is consumed by a patient taking disulfiram, levels of acetaldehyde Build-up, causing side effects of alcohol toxicity • One of disulfiram’s metabolites is carbon disulfide, which may be excreted through the lungs; this could • 250–500 mg/day; 1-year duration • Not generally recommended for patients older than age 60 • Some elderly patients may tolerate lower doses better -Pregnant women needing to stop drinking may consider behavioral therapy before Pharmacotherapy Not recommended in breast feeding mothers

account for the side effect of metallic taste