Sedatives-Anxiolytics Win-2020 post.pptx - Integrated Medicinal Chemistry and Pharmacology II PSC 6311 NeuroPharmacology Sedatives Hypnotics Anxiolytics

Sedatives-Anxiolytics Win-2020 post.pptx - Integrated...

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NeuroPharmacology: Sedatives, Hypnotics, Anxiolytics and Sleep Aids Integrated Medicinal Chemistry and Pharmacology II PSC 6311 Karen S. Mark , Ph.D. ; Associate Professor Pharmaceutical Sciences Office: Room 275 email: [email protected] ph: 865-288-5839 Katzung, Basic and Clinical Pharmacology , 14 th ed.; Chapter 22 Foye’s, Principles of Medicinal Chemistry , 8 th ed.; Chapters 11 and 12 Foye’s, Principles of Medicinal Chemistry , 7 th ed.; Chapter 15 Goodman & Gilman’s The Pharmacological Basis of Therapeutics , 13 th ed.; Chapters 15 and 17
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Lecture Objectives Describe GABA-A receptor and role in neurotransmission Compare and contrast binding sites for different classes of drugs that act at GABA receptor Explain the MOA for BDZ, Barbs, and Z-drugs Explain key structural aspects of SAR for BDZs and Barbs Explain how drug classes differ from each other in regulating the GABA- A receptor, metabolism, safety profile, and DDIs BDZ / Barbs: know up to 3 with short / intermed / long (t 1/2 ) Describe MOA, PK, ADE for suvorexant, ramelteon, and buspirone Explain the use(s) for flumazenil
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Drugs Covered in this Section chlordiazepoxide chlorazepate* clonazepam diazepam flurazepam lorazepam nitrazepam oxazepam quazepam temazepam amobarbital butabarbital methohexital pentobarbital phenobarbital secobarbital zolpidem zaleplon eszopiclone ramelteon tasimelteon lemborexant suvorexant buspirone flumazenil alprazolam estazolam midazolam triazolam
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Clinical Uses Insomnia ( sleep aids ) Relief of anxiety / performance anxiety Chronic alcoholism ( withdrawal relief ) Medical / surgical procedures Sedation and/or amnesia Trauma-induced coma Cancer associated sedation Patient with epilepsy / seizures Psychiatric treatment Major Depressive Disorder
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Sedation vs. Hynotic Sedative drugs reduces moderates excitement (anxiolytic activity) calms the recipient decreases activity combination of sedative agents can lead to respiratory and CNS depression Hypnotic drugs produces drowsiness facilitates the onset / maintenance of a sleep-state where the individual can be easily aroused
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Organ Level Effects Central Nervous System CNS depression = inhibits neurotransmission beneficial for: inducing sleep, preventing epilepsy, sedation during surgery, reducing anxiety low doses anxiolytic effects higher doses depressed psychomotor / cognitive function Hypnotics : Induce sleep with adequate dosing: all have this in common Tolerance develops when used for > 2wks Effect on sleep architecture depends on: Drug, dose, and frequency All of these drugs latency to sleep onset Effects on REM and NREM differ Respiratory (Pulmonary) System Cardiovascular System
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Organ Level Effects Respiration effects are dose related Hypnotic doses Healthy person normal respiration Pulmonary disease respiratory depression High-dose, accumulation, over-dose Medullary depression of respiration Coma and death Cardiovascular system Hypnotic doses Healthy person no cardiovascular effects
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