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A comprehensive overview of the pharmacological treatments for substance abuse disorders, including opioid addiction, alcohol dependence, and related conditions. It covers the key details of several commonly prescribed medications, such as their indications, affected neurotransmitters, target symptoms, pharmacokinetic properties, notable side effects, and dosing considerations. The information presented is highly relevant for healthcare professionals, researchers, and students studying addiction medicine, pharmacology, or related fields. The document delves into the mechanisms of action, clinical applications, and safety profiles of drugs like buprenorphine, naltrexone, acamprosate, and disulfiram, offering valuable insights into the management of substance use disorders. By studying this document, readers can gain a deeper understanding of the pharmacological approaches to treating addiction and the factors that guide the selection and use of these medications.
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Drug Name Indica/on Neurotransmi3er(s) Affected Target Symptoms Half-life (T1/2), Metabolism (CYP 450 enzyme) Notable Side Effects (link to NT or affected brain circuit) Ini/al Dosing Considera/ons Specific lifespan considera/ons (age, pregnancy, breasPeeding) Buprenorphine (Subutex) Indica/on: Treatment of opioid addic/on and dependence Neurotransmi3ers affected: GABA, Norepinephrine, Dopamine Target symptoms: Opioid Dependence Half life: 24- hours CYP450: CYP 3A -hypotension -pruri/s -erythema -respiratory depression -liver failure -headache -cons/pa/on -nausea, vomi/ng Ini/al dosing: Day 1: 8 mg Day 2: 12-16 mg Day 3-7: increase 4 mg every increments, max dose is 32 mg Considera/ons: -cau/ous usage in elderly pa/ents and pa/ents with co- morbidi/es like cardiac issues -not recommended for pregnant women due to neonatal withdrawal or women who are breasPeeding -safety has not been ensured for usage in children and adolescents -monitor for liver toxicity, not recommended for pa/ents with liver failure
Buprenorphine/Naloxone (Suboxone, Zubsolv, Bunavail) Indica/on: Treatment of opioid addic/on and dependence Neurotransmi3ers affected: Par/al agonist at the Mu opioid receptor, antagonist at the kappa opioid receptor Target symptoms: Opioid dependence Half life: 24- hours CYP450: CYP 3A -headache -nausea -cons/pa/on -hypotension -respiratory depression -liver failure -oral hypesthesia -glossodynia Ini/al dosing: Suboxone (buprenorphine/naloxone) Day 1: 2mg/0.5 mg Day 2: 16 mg/4 mg Day 3-7: increase 4 mg in increments each /me, max dose 32 mg Considera/ons: -cau/ous usage in elderly pa/ents and cardiac pa/ents -not recommended in pregnant women or women who are breasPeeding -not safe for using in children and adolescents -pa/ents should be observed for 2 hours a_er first dose -pa/ent should be seen once a week during stabiliza/on -monitor for liver toxicity
Methadone (Dolophine, Methadose) Indica/on: Opioid abuse, dependence and withdrawal Neurotransmi3ers affected: Antagonist to NMDA receptor, binds to opiate receptors in the CNS and inhibit pain pathways to alter response to pain and lead to CNS depression Target symptoms: Opioid addic/on and withdrawal, moderate to severe pain Half life: 8-59 hours CYP450: CYP 2C19, CYP450 2B6, CYP450 2C9, CYP450 2D6, CYP450 3A -rash -swearing -loss of menstrual period -sexual dysfunc/on -arrhythmia -prolonged QT -weight gain -cons/pa/on -urinary reten/on -agita/on, hallucina/on -seizure -respiratory depression -electrolytes imbalance -pulmonary edema Ini/al dosing: -Pa/ents with no/low tolerance of opioid: 2.5-10 mg/ day -Pa/ents with lower levels of opioid tolerance: 10-20 mg/ day -Pa/ents with withdrawal symptoms and no signs of seda/on: 20-30 mg/day -Max dose is 30 mg/day Considera/ons: -not for use in pregnant women or women who are breasPeeding, can cause neonatal opioid withdrawal -pa/ent must get pregnancy test before star/ng this medica/on -adjust dosage for pa/ents with renal and liver diseases -can cause hypoxia, hypercapnia, arrhythmia, respiratory depression
Naltrexone (Revia, Vivitrol) Indica/on: Alcohol dependence, prevents opioid addic/on relapse Neurotransmi3ers affected: Blocks the Mu opioid receptors, which prevent the pleasurable results from opioids Target symptoms: Alcohol addic/on, opioid addic/on Half life: 13 hours Injec/on: 5-10 days CYP450: None -injec/on site reac/ons like itchiness, erythema, swelling -nausea, vomi/ng -poor appe/te -dizziness -anxiety -eosinophillic pneumonia -hepatocellular injury Ini/al dosing: -Alcohol: 50 mg/day orally, 380 mg IM injec/on every 4 weeks -Opioid: 25 mg/day orally, 380 mg IM injec/on every 4 weeks Considera/ons: -not recommended for elderly pa/ents, children or adolescents -not recommended for pregnant women or women who are breasPeeding Acamprosate (Campral) Indica/on: Maintenance of alcohol abs/nence, treatment of alcohol dependence Neurotransmi3ers affected: Increases GABA, decreases glutamate neurotransmi3ers, bind and blocks some glutamate receptors Target symptoms: Alcohol dependence Half life: 20- hours CYP450: none -nausea, vomi/ng -suicidal idea/on -diarrhea -anxiety -depression Ini/al dosing: 666 mg TID orally Considera/ons: -adjust dosage for elderly pa/ents due to decreased renal func/ons -not recommended for pregnant women or women who are breasPeeding -monitor pa/ents for signs of depression and suicidal idea/on -not recommended for pa/ents with renal diseases -not safe for usage in children and adolescents
Disulfiram (Antabuse) Indica/on: Maintenance of alcohol abs/nence Neurotransmi3ers affected: Inhibits aldehyde dehydrogenase and affect metabolism of alcohol Target symptoms: Alcohol dependence Half life: 60- hours CYP450: CYP 2A6, CYP450 1A2, CYP450 2B6, CYP450 2D6, CYP450 2E1, CYP450 3A -seda/on -headache -nausea, vomi/ng if alcohol is consumed -metallic taste in mouth -derma//s -liver failure -CHF -respiratory depression -tachycardia Ini/al dosing: -250/500 mg per day for 1 to 2 weeks -Maintenance dose: 250- mg/day -Only start if last alcoholic drink was more than 12 hours ago Considera/ons: -not recommended for pa/ents with renal failure, liver failure, cardiovascular diseases, or elderly pa/ents -not safe for use in children and adolescents -do not use for pa/ents who are intoxicated or last alcoholic drink was less than 12 hours ago -not recommended for pregnant women or women who are breasPeeding