Pharmaco kinetics Reach peak level within 30 min to 6 8 hr metabolized in liver

Pharmaco kinetics reach peak level within 30 min to 6

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Pharmaco -kinetics Reach peak level within 30 min to 6-8 hr; metabolized in liver and biotransformed by oxidation or by conjugation (better response in liver impairment) Peak in 0.7 to 1.5 hr, slow onset of action (up to 6 wks) needs multiple dosing during day; anxiolytic effect in 1-2 wks; max benefit takes 3-6wks Few drug interactions d/t not inhibited by CYP 450 Pharmaco -therapeu tics Xanax & Ativan high risk of dependence d/t high potency and rapid, short term action but Klonopin is less d/t long action Withdrawal Sx occurs 1-2 days after last dosing of short-acting; 5-1 days in long-acting Contraindication in panic attack; liver, renal dz Pregnancy B
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Contraindication in pregnancy, lactation, liver & renal dz Clinical use & dosing Insomnia: Flurazepam (Dalmane), Temazepam (Restoril) depressive Sx worsens, Diazepam: used for acute stage of alcohol withdrawal no longer than 4-6 wks d/t dependency Clonazepam can be used for long-term treatment of anxiety but Buspirone or SSRs are the first line choice Low risk of dependence and side effects Frequently used adjunctively w/ SSRIs in treatment- resistant depression (first line) ADRs Physical & psychological dependence; Most common: drowsiness & confusion; Major ADRs CNS depression; excessive sedation, cardiac & resp depression; narrow-angle glaucoma; older adults cautiously use BZD d/t increase sensitivity, risk of falls, delirium, cognitive impairment, MVA, FX Few ADRs, most common: light- headedness, Ha, insomnia, nervousness, dry mouth; rare serotonin syndrome Monitorin g Increase TCAs, digitalis levels in concurrent use of benzo; long-term use periodic assessment of LFT and CBC Barbiturates & Hypnotics Barbiturates Sedative Hypnotics Short-acting (30min – 4hr): Pentobarbital (Nembutal), Secobarbital (Seconal) Intermediate-acting (6-8): Amobarbital (Amytal), Aprobarbital (Alurate), Butabarbital sodium (Butisol) Long-acting (10-12): Mephobarbital (Mebaral), Phenobarbital (Luminal) Nonbenzo Benzo Zolpidem (Ambien), Zaleplon (Sonata), Eszopiclone (Lunesta) Melatonin receptor agonist: Ramelteon (Rozerem) Orexin receptor antagonist: Suvorexant (Belsorma) Rapid onset, slow- acting: Triazolam (Halcion) Delayed onset, intermediate- acting: Temazepam (Restoril), Estazolam (Prosom) Rapid onset, long acting: flurazepam (Dalmane), Quazepam (Doral) Pharmaco- dynamics CNS depression—reduced motor stimulation & increased sleep Indication: pheno & mephobarbital effective in tonic-clonic, simple partial complex partial sz (not first line in emergency); preanesthetic sedation, short- term tx of insomnia (last resort) For sedation during episodes of insomnia Take within 30 min of bedtime Pharmaco- kinetics Metabolized in live by CYP 450 (auto-induced metabolism increase rate of metabolism & potential for tolerance) and excreted in urine Pregnancy D Zolpidem, Zalepion, Eszopiclone extensively metablized by aldehydre oxidase & CYP 450 and excreted in urine Pregnancy C
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Pharmaco- therapeuti cs W/ alcohol causes death d/t additive depressive effect; withdrawal (sx occurs 8-12hr after last dose) & detoxification —potentially fatal, gradual approach needed Worsening depression;
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  • Spring '14
  • Henrikson,J
  • Major depressive disorder

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