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sedative and hypnotics Group 6.pptx

NURSE um DAYSTAR UNIVERSITY-KENYA, ATHI-RIVER MACHAKOS
24. Mar 2023
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sedative and hypnotics Group 6.pptx

  1. GROUP 6 Clinical Pharmacology 2
  2. Members i. CALEB WANYONYI 21-2220 ii. AKAL MORRIS 21-2668 iii. TONY BARAKA 21-2114 iv. ASNATH MAKORI 21-2853 v. SOFIA MURIUNGI 21-2755 vi. NEDDY CHELANGAT 21-2315 vii.VINCENT KIBUNGEI 21-2435 viii.TRACY MURANDE 22-0173 ix. DAVID MACHUKA. 21-2325 x. HADEN CHWEYA 21-2340
  3. Stages of sleep Stage 1 (2-5%) REM (Ø &αwaves) Stage 2 Non REM (67-75 STAGE 3 DEEP SLEEP STAGE 4 DEEP SLEEP
  4. Pharmacokinetics Route: oral Absorption: lipid-soluble and are absorbed well from the gastrointestinal tract Distribution: wide and crosses BBB Metabolism: liver Elimination: urine
  5. Pharmacodynamics The CNS effects of most sedative-hypnotics depend on dose. These effects range from sedation and relief of anxiety (anxiolysis), through hypnosis (facilitation of sleep), to anesthesia and coma. Depressant effects are additive when 2 or more drugs are given together. The steepness of the dose–response curve varies among drug groups; those with flatter curves, such as benzodiazepines and the newer hypnotics (eg, zolpidem), are safer for clinical use.
  6. Mode of Action Barbiturates Bind to the GABA-A receptor and increase the duration of chloride ion channel opening, leading to neuronal inhibition. Benzodiazepines Benzodiazepines bind to a specific site on the GABA-A receptor and enhance the affinity of GABA for the receptor, leading to increased chloride ion channel opening and neuronal inhibition. Non-benzodiazepine hypnotics also enhance the activity of the GABA receptor, but through a different mechanism.
  7. Long-acting and sshort-acting benzodiazepines a) Short-acting benzodiazepines Short-acting benzodiazepines have a shorter half-life. This means that the drugs are processed and leave the body more quickly. Short-acting drugs have a higher risk of withdrawal symptoms. This is because the body has less time to adapt to working without the drug once you stop taking it. b) Long-acting benzodiazepines They have a longer half-life. This means that the drugs are processed by the body more slowly and take longer to leave the body.
  8. Classification of benzodiazepines Short acting (3-5hours)  Triazolam Intermediate (6-24hrs)  Alprazolam  Lorazepam  Estazolam  Oxazepam  Temazepam Long acting (24-72hrs) Chlorazepate Chlordiazepoxide Diazepam Flurazepam Quazepam Prazepam Nitrazepam
  9. MoA (benzodiazepines) GABA is the transmitter most associated with inhibition in the CNS and the GABA receptor mediates this effect. Receptors for benzodiazepines are located on the GABAA receptor molecule and thus are present in many brain regions, including the thalamus, limbic structures, and the cerebral cortex The drug binds to GABA-A (gamma-aminobutric Acid) receptors and increase frequency of Chloride channel opening. Increasing chloride flow into neurons hence hyperplorasation therefore inhibiting propagation of AP
  10. Pharmacokinetics Route: oral, IM (SLOW) Absorption: Via GIT Distribution: Wide Metabolism: liver as they bind to plasma protein Excretion: Kidney
  11. Indications
  12. Adverse Effects •Ataxia •Hangover •Tolerance •Physical and psychological dependence •Withdrawal Symptoms (insomnia, anorexia, agitation, tremors, Convulsions) •Drowsiness & Dizziness (common)
  13. Drug Interaction •Synergistic effects with CNS depressant •Enzyme modulators : Rifampicin (decrease ½ life) Cimetidine (increase ½ life) *N/B These drugs are Pregnancy risk category D (studies in pregnant women have demonstrated a risk to the fetus; potential benefits of the drug may outweigh the risks)
  14. 2. Barbiturates •Derivatives of barbutric acid thus the name CLASSIFICATION Long acting (6-12hours) Mephobarbitone Phenobarbitone Intermediate acting (3-6hrs) Amobarbitone Aprobarbitone Butabarbitone Short acting <3hrs Hexabarbitone Pentobarbitone Secobarbitone Ultra-Sound Acting<15-20mins Thiopentone Methohexitone
  15. MoA Act to GABA but does not bind to BZD (α and ϒ) but binds to another site (α and β ) on the same macromolecular complex to exert GABA facilitatory action. They also enhance BZD binding to their site. At high conc they increase chloride ions conductance and inhibit Calcium ions dependent release of neurotransmitter They depress glutamate induced neuronal depolarization thr AMPA receptors.
  16. Pharmacokinetics Route: Oral Absorption: via GIT Distribution: wide ( from CNS to Skeletal muscles) Metabolism: Liver by oxidation, conjugation, dealkylation Excretion: Kidney
  17. Indications Epilepsy except for phenobarbitone and anesthesia thiopentone Adjuvant in psychosomatic disorders
  18. Adverse effects Hangover Tolerance Idiosyncrasy (untoward reactions to drugs that occur in a small fraction of patients and have no obvious relationship to dose or duration of therapy) Hypersensitivity Mental Confusion *It has no specific antidote
  19. INDICATIONS (generally) Sedatives i. Sedatives are used for a variety of indications, including anxiety, insomnia, and seizure disorders. Barbiturates are used primarily for anesthesia induction and maintenance, but are also used as anticonvulsants. Benzodiazepines are used for anxiety, insomnia, seizure disorders, and muscle relaxation. Non-benzodiazepine hypnotics are used primarily for insomnia. Hypnotics i. Hypnotics are primarily used to treat insomnia, sleep disturbances, and other sleep disorders. They are also used in certain medical procedures that require sedation or anesthesia.
  20. Toxicity i. Psychomotor dysfunction ii. Additive CNS depression iii.Overdose
  21. Drug interaction diazepam, flurazepam + benzodiazepines= Excessive Sedation
  22. ATYPICAL SEDATIVE-HYPNOTICS Buspirone MoA •The drug interacts with the 5-HT1A subclass of brain serotonin receptors as a partial agonist, but the precise mechanism of its anxiolytic effect is unknown •Pharmacokinetics •metabolized by CYP3A4, and its plasma levels are markedly increased by drugs such as erythromycin and ketoconazole •Adverse effects; tachycardia, paresthesias, pupillary constriction, and gastrointestinal distress  Buspirone is safe in pregnancy
  23. Orexin Antagonists •Orexin is a peptide found in the hypothalamus and is involved in wakefulness •Suvorexant, an antagonist at OX1R and OX2R orexin receptors, has hypnotic properties and is approved for the treatment of insomnia.
  24. Miscellaneous (Non-benzodiazepines hypnotics) 1. Zopiclone Agonist subtype of BZD receptors involved in hypnotics action. Used for insomnia (<2weeks) Side effects: metallic taste, dry mouth, mild dependence, impaired judgement
  25. 2. paraldehyde It is colourless, transparent, pungent and inflammable liquid. Given Rectally, IV, IM,Orally Used in epilepsy in children *Others Melatonin- hormone from pineal gland that improve quality of sleep. *Ramelteon-melatonin agonist
  26. THANK YOU FOR YOUR ATTENTION The good physician treats the disease; the great physician treats the patient who has the disease. William Osler
  27. References 1. Kartzung, B. G. & Trevor, A. (2015). Basic and Clinical Pharmacology. McGraw-Hill; (13thed.) ISBN: 13-9780071825054; 10: 0071825053
  28. QUESTIONS???? 💊 💊 😉😂👋 Prepared by: Akal Lobenyo Morris
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