ANTICHOLINERGICS
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This document summarizes information about cholinergic receptors and anticholinergic drugs. It discusses the classification of cholinergic receptors into nicotinic and muscarinic receptors. It then describes natural and semisynthetic anticholinergic drugs that act on muscarinic receptors, including atropine and hyoscine. The document outlines the mechanisms, uses and side effects of various anticholinergic drugs for conditions like COPD, peptic ulcers, overactive bladder, and Parkinson's disease. It also discusses ganglionic blockers and neuromuscular blocking drugs that act on nicotinic receptors.
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ANTICHOLINERGICS
- 1. Dr Anu Chandran FINAL YEAR PG DEPARTMENT OF PHARMACOLOGY
- 6. Cholinergic receptors Receptor ? Cholinoreceptor Nicotinic receptor Muscarinic receptor
- 10. 1. Anti muscarinic 2. Anti nicotinic
- 11. 1.NATURAL ALKALOIDS Atropine Hyoscine 1.ANTI MUSCARINIC DRUGS
- 12. Atropine Scopolamine Atropine prototype drug Source---Atropa belladona (deadly night shade) Datura stramonium NATURAL ALKALOIDS
- 13. GUESS? BELLADONNAATROPOS History Linnaeus – Atropa belladona
- 14. NATURAL ALKALOIDS Atropa belladona Hyocyamus niger Solanaceae family
- 15. ACTIONS CNS Overall stimulant action. low doses restricted entry into the brain. High dose .- •stimulates many medullary centers vagal, respiratory & vasоmotor.
- 16. •Antimotion sickness property : ↓vestib excitation •suppresses tremor & rigidity in parkinsonism. •High doses cause cortical excitation, restlessness, disorientation, hallucinations & delirium followed by resp depression & coma.
- 17. CVS Heart SA node-Block M2-Tachycardia AV node-↓refractoryperiod↑conduction PR interval shortened Blood vessel No consistent effect Cutaneous Vasodiln--Atropine flush
- 18. EYE Mydriasis Dryness ↑IOT Abolition of light reflex Photophobia Blurring of near vision
- 19. SMOOTH MUSCLE Relaxant GIT ↓ tone ,amplitude of peristaltic contraction-Constipation Mild antispasmodic-Gallbladder, bileduct Urinary tract ↓Tone , amplitude of contractions of ureter,bladder—Urinary retention
- 20. Smooth muscle--- Respiratory Broncho dilation,decrease in airway resistance Depress mucociliary clearance
- 22. Comparison- Atropine Hyoscine Source Atropa belladona Datura stromonium Hyoscyamus niger Ester of tropic acid Tropine scopine Duration long short CNS Excitation Depression
- 23. Atropine (pk) Duration of action - to 8 hours except in the eyes (72 hours or longer) Dose -0.5 mg to 1 mg Metabolism -40% liver, Excretion -60% un changed in the urineJune 16 23Dr. Med. Khaled Radaideh
- 24. USES OF ATROPINE Counteract brady cardia& partial heart block Myocardial infarction Digitalis toxicity Secific antidote in anticholineesterase poisoning,early mushroom poisoning Atropine 2mg i/v every 10 min till signs of atropinisation appear
- 26. CONTRA INDICATIONS Narrow Iridocorneal angle ppt Acute Congestive Glaucoma Elderly males with Prostatic Hypertrophy Urinary retention may occur
- 27. Belladona poisoning Consumption of seeds& berries Children more susceptible Drug overdose
- 28. Gen.exmn-dry mouth,hot flushed skin Eyes- dilated pupil,photophobia,blurring near vision CVS tachycardia,hypotension,weak pulse GIT decreased bowel sounds,constipation UT difficuilty in micturition CNS psycotic behaviour,ataxia,delirium,visual hallucn,respdepression,covulsion,coma Dry as bone,blind as bat ,red as beet,mad as hatter BELLADONA POISONING
- 29. Homatropine Atropine Methonitrate Hyoscine Butylbromide Ipratropium Br Tiotropium Br 2.SEMISYNTHETIC
- 30. Mydratics Anti sec – antispasmodics Vasicoselective Antiparkinsonian 3.SYNTHETIC
- 31. ANTISPASMODIC Intestinalcolic,Renalcolic,biliarycolic, Abdominal cramps in dysentry,diarrhoea dysmenorrhoea Dicyclomine Propantheline Oxyphenonium Pipenzolate Hyoscine butyl bromide
- 33. COPD &ASTHMA Ipratropium,Tiotropium Broncho dilation(additive with adrenergics) No impairment of muco ciliary clearance Acute attack of asthma –Ipratropium nebulised with salbutamol
- 34. ANTISECRETORY Atropine,Hyoscine,Glycopyrrolate Preanasthetic medication ↓ salivary,tracheobronchial secretions prevent laryngospasm Vasovagal attacks in anasthesia ↓ Peptic ulcer ↓ gastric secretion Atropine,Pirenzepine
- 35. VASICOSELECTIVE Oxybutynin,Tolterodine,Darifenacin Trospium,Flavoxate Relax smooth muscle of ureters &bladder Improve bladder capacity,↓involuntary voiding Decrease pain USE Neurogenic bladder Detrusor instability,urinary incompetence Nocturnal enuresis
- 36. ANTISPASMODIC Intestinalcolic,Renalcolic,biliarycolic, Abdominal cramps in dysentry,diarrhoea dysmenorrhoea Dicyclomine Propantheline Oxyphenonium Pipenzolate Hyoscine butyl bromide
- 38. Hexamethonium (3,5,6 MP) pentolinium Mecamylamine Pempidine Trimethaphan( monosulphan ) Ganglion blockers
- 39. SLOW IV Ultra short acting Uses a. hypertension (dissecting aortic aneurysm) b. hypertensive emergency c. Autonomic hyperreflexia d. Acute pulmonary oedema CI a. Asthma TRIMETHAPHAN
- 42. Opening Na channel Phase 1 - rapid ,depolarization, gradual repolarization Phase 2 – desensitization of receptors to acetyl choline, full repolarization Depolarizing blockers
- 43. Skeletal muscles - muscle weekness ,flaccid paralysis Cvs – BP falls ( sch variable) CNS – do not cross BBB Histamine release Autonomic ganglion – some blockage GIT – paralytic ileus Actions
- 44. IV Metabolized in liver Excreted kidney Sch - pseudocholinesterase PK
- 45. General anesthesia Assisted ventilation Tetanus Status epilepticus Uses
- 46. THANK YOU