Sedative-Hypnotics Drugs

Introduction to Sedative-Hypnotics Drugs
Sleep, Introduction to Sedatives -hypnotics, Sedative-hypnotic drug classification, Pharmacology of sedative-hypnotic drugs, Overview, New inventions
Presented by
AGGIM SUMASHREE
Department of Pharmacology

1. Sedative-Hypnotics Drugs   A Seminar as a part of curricular requirement for M . Pharmacy I year I Semester Presented by AGGIM SUMASHREE (20L81S0102) Pharmacology Under the guidance of A . Sudheer Kumar M.Pharm , ( Ph.D ) Assistant Professor

2. Contents : Sleep Introduction to Sedatives -hypnotics Sedative-hypnotic drug classification Pharmacology of sedative-hypnotic drugs Overview New inventions References 2

3. Sleep: Normal sleep cyclic and repetitive, consists of distinct stages based on three physiological measures: the electroencephalogram, the electromyogram and the electronystagmogram . Non rapid eye movement (NERM)sleep 70%-75% stage 1,2 stage 3,4:slow wave sleep,sws Rapid eye movement(REM) sleep 3

4. A normal sleep cycle

5. An effective sedative agent should reduce anxiety and exert a calming effect with little or no effect on motor or mental functions. A hypnotic drug produce drowsiness and encourage the onset and maintenance of a state of sleep that as far as possible resembles the natural sleep state. Hypnotics effects involve more pronounced depression. Graded dose-dependent depression of CNS function is a characteristic of sedative-hypnotics. Sedatives-hypnotics:

6. Classification : Benzodiazepines: 1.Short acting : Triazolam , Temazepam 2.Intermediate acting: Alprazolam , Lorazepam 3.Long acting: Diazepam Barbiturtes : 1.long acting: Phenobarbitone 2.Short acting: Butobarbitone , Pentobarbitone 3.Ultra-short acting: Thiopentone , Methohexitone Miscellaneous agents: Buspirone , Zaleplon , Zolpidem , cholarhydrate . 6

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8. Pharmacology of drugs: Pharmacology includes Mechanism of action Pharmacokinetics Adverse effects Therapeutic uses 8

9. Mechanism of action: Sedatives-hypnotics Bind to GABA receptor at different allosteric sites Facilitates GABA action Barbiturates increase duration and benodiazepines increase frequency of opening of cl channel Membrane hyperpolarization CNS depression 9

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11. Pharmacokinetics: Benzodiazipines : Absorption: orally/I.M/I.V distribution: pass BBB and Placenta, secreted into breast milk Metabolism: in liver by microsomal enzyme Half-life: long acting-1-3days short acting-3-8hrs Intermediate acting-10-20hrs Excretion: excreted as glucoronide conjugates in urine. 11

12. Barbiturates : Absorption: oral/I.V/I.M Distribution: to all body Metabolism: Liver Excretion: alkalinization of the urine expedites the excretion of barbiturates. 12

13. Adverse effects : Cross placental barrier Depression of neonatal vital function Detectable in breast milk Cvs depression Dependence Drug-drug interaction Pophyria Paradoxical excitement in children 13

14. Therapeutic uses Epilepsy in emergency Short-term use of sedative-hypnotics for treating anxiety Premedication prior to surgery Panic and Agoraphobia Reduces anxiety and aggression Sleep disorder, insomnia Treatment of muscle plasticity in cerebral plasy and tetanus 14

15. New inventions: ROZEREM- Ramelteon It appears to be a promising novel hypnotic, provided its efficacy is established. It is a MT1 and MT2 Melatonin receptor agonist introduced in USA and now approved in India. Meloset , Zytonin , Externex are some of the marketed melatonin receptor agonist drugs. 15

16. Overview : 16

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19. References : JAMES M. RITTER et,al . “RANG AND DALE’S Textbook of Pharmacology” 9 TH edition 2018 p.577 KD TRIPATHI “Essentials of Medical Pharmacology Textbook of pharmacology 7 th edition 2013 p.397. LUCIA SUKYS-CLAUDINO et al. Braz J Psychiatry Article in Portuguese 2010 sep- PubMed,gov 19

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