High Yields: Anxiolytics, Hypnotics and Barbiturates PDF
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Universidad Autónoma de Guadalajara
Sonia Guadalupe Barreno Rocha
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These medical notes cover the topics of anxiolytics, hypnotics, and barbiturates. They detail their mechanisms of action, clinical uses, adverse effects, and contraindications. The document is presented in a lecture format.
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High Yields: ANXIOLYTICS, HYPNOTICS AND BARBITURATES Sonia Guadalupe Barreno Rocha MD, PhD [email protected] WE MAKE DOCTORS Benzodiazepines Family...
High Yields: ANXIOLYTICS, HYPNOTICS AND BARBITURATES Sonia Guadalupe Barreno Rocha MD, PhD [email protected] WE MAKE DOCTORS Benzodiazepines Family Adverse MoA Clinical Use effects Diazepam, lorazepam, triazolam, Dependence, additive CNS temazepam, Facilitate GABAA depression effects with oxazepam, action by ↑ Anxiety, panic disorder, alcohol and barbiturates. midazolam, frequency of Cl– spasticity, status Less risk of respiratory channel opening depression and coma than chlordiazepoxi epilepticus (lorazepam, with barbiturates. Can de, alprazolam (“frenzodiazepines” diazepam, midazolam), eclampsia, medically precipitate seizures by ↑ frequency). ↓ REM causing acute sleep supervised withdrawal (eg, alcohol/DTs; long- benzodiazepine acting withdrawal. Treat overdose with chlordiazepoxide and flumazenil (competitive antagonist diazepam are preferred), night at GABA benzodiazepine receptor) terrors, sleepwalking, general anesthetic (amnesia, muscle relaxation), hypnotic (insomnia). Barbiturates Family MoA Clinical Use Adverse effects Contraindications Phenobarbital, Respiratory and pentobarbital Sedative for anxiety, cardiovascular Facilitate GABAA seizures, insomnia depression (can action by ↑ time be fatal); CNS of Cl– channel depression (can opening, thus ↓ be exacerbated by Porphyria alcohol use); neuron firing dependence; drug interactions (induces cytochrome P- 450) Buspirone MoA Clinical Use Disadvantages Generalized anxiety disorder. Does not cause I take buspirone. sedation, addiction, or tolerance. Begins to take effect after 1–2 weeks. Does not interact with alcohol (vs Partial 5-HT1A barbiturates, benzodiazepines). The anxiolytic effects receptor agonist. may take 3–4 weeks to become established; less effective in panic disorders. Insomnia Therapy Agent Mechanism Adverse Effects Notes Non- Examples: Zolpidem, Ataxia, headaches, These ZZZs put you to sleep benzodiazepine Zaleplon, esZopiclone confusion Short duration due to rapid Hypnotics Cause only modest day-after metabolism by liver enzymes; Act via the BZ1 subtype psychomotor depression effects reversed by of and few amnestic effects (vs flumazenil, less dependency GABA receptor older risk and less sleep cycle sedative-hypnotics) disturbance (vs benzodiazepine hypnotics) Suvorexant Orexin (hypocretin) CNS depression Contraindications: receptor antagonist (somnolence), Narcolepsy, combination headache, abnormal sleep- with strong CYP3A4 related activities inhibitors Not recommended in patients with liver disease Limited risk of dependency Ramelteon Melatonin receptor Dizziness, nausea, fatigue, No known risk of dependency agonist: binds MT1 and headache MT2 in suprachiasmatic nucleus References Le T, Bhushan V, Qiu C, Chalise A, Kaparaliotis P, Coleman C, Kallianos K. First Aid for USMLE Step 1 2023. 1st edition. USA: McGrawHill; 2023. Vanderah TW. Sedative-Hypnotic Drugs. In: Vanderah TW. eds. Katzung’s Basic & Clinical Pharmacology, 16th Edition. McGraw- Hill; 2024. Chapter 22. https://bibliodig.uag.mx:2091/content.aspx?bookid=3382§ioni d=281750253
