Antimuscarinic Agents 2 Power Point Presentation

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Antimuscarinic Agents 2 Power Point Presentation

  1. 1. Comparison between Atropine & Hyoscine Hyoscyamys niger Depressant (amnesia, fatigue, drowsiness, N-REM sleep) Excitation More potent on eye & secretory glands Shorter +++ Atropa belladonna Excitatory Excitation (mild) Excitation (strong) More potent on heart, bronchial muscle & intestines Longer ++ <ul><li>Chief source </li></ul><ul><li>CNS effect </li></ul><ul><li>low dose </li></ul><ul><li>high dose </li></ul><ul><li>3. Anticholinergic property </li></ul><ul><li>4. D.o.A </li></ul><ul><li>5. Antimotion sickness </li></ul>Hyoscine Atropine
  2. 2. <ul><li>Quaternary compounds </li></ul><ul><li>They have some common features:- </li></ul><ul><li>Oral absorption is incomplete. </li></ul><ul><li>Do not penetrate brain & eye – central & ocular effects are not seen after parenteral/oral administration. </li></ul><ul><li>Slow elimination & most of them are longer acting than atropine. </li></ul><ul><li>They have higher nicotinic blocking property. </li></ul><ul><li>At clinical doses, ganglionic blockade may occur – postural hypotension, impotence are additional s/e. </li></ul><ul><li>At high doses NMB (neuromuscular blocking) may also occur. </li></ul>
  3. 3. <ul><li>Hyoscine butylbromide </li></ul><ul><li>20- 40mg oral, i.m, s.c, i.v </li></ul><ul><li>It is less potent & longer acting than atropine. </li></ul><ul><li>Used for esophageal & G.I spastic conditions. </li></ul><ul><li>Ipratropium bromide </li></ul><ul><li>40-80 μ g by inhalation. </li></ul><ul><li>It acts selectively on bronchial muscle without altering volume or consistency of respiratory secretions. </li></ul><ul><li>It doesn’t depress mucociliary clearance by bronchial epithelium (atropine does it) </li></ul>
  4. 4. <ul><li>It has a gradual onset and late peak (at 60-90min) of bronchodilatory effect in comparison to inhaled sympathomimetics – more suitable for regular prophylactic use. </li></ul><ul><li>Action lasts 4-6hrs. </li></ul><ul><li>It acts on receptors located mainly in the larger central airways. (primary site of action for sympathomimetics are peripheral bronchioles) </li></ul><ul><li>It is more effective in COPD. </li></ul>
  5. 5. <ul><li>s/e (local) </li></ul><ul><li>Dryness of mouth </li></ul><ul><li>Scratching in trachea </li></ul><ul><li>Cough </li></ul><ul><li>Bad taste </li></ul><ul><li>Nervousness </li></ul><ul><li>Propantheline </li></ul><ul><li>15-30mg oral </li></ul><ul><li>Most popular anticholinergic were used for peptic ulcer and gastritis. </li></ul><ul><li>Higher ganglion blocking activity is believed to aid antisecretory effects. </li></ul><ul><li>It also delays gastric emptying. </li></ul><ul><li>Action lasts 6-8hrs. </li></ul>
  6. 6. <ul><li>Oxyphenonium </li></ul><ul><li>5-10mg (children3-5mg) oral </li></ul><ul><li>Similar to Propantheline </li></ul><ul><li>For peptic ulcer and g.i hypermotility. </li></ul><ul><li>Clidinium </li></ul><ul><li>2.5-5mg oral </li></ul><ul><li>It is used in combination with Benzodiazepines for nervous dyspepsia, gastritis, irritable colon. </li></ul>
  7. 7. <ul><li>Pipenzolate methylbromide </li></ul><ul><li>5-10mg (children 2-3mg) oral </li></ul><ul><li>For flatulent dyspepsia, infantile colics and other g.i spasm. </li></ul><ul><li>Isopropamide </li></ul><ul><li>5mg oral </li></ul><ul><li>For hyper acidity, nervous dyspepsia, irritable bowel and other g.i problems, specially when associate with emotional/mental disorders. </li></ul>
  8. 8. <ul><li>Glycopyrrolate </li></ul><ul><li>0.1-0.3mg i.m, 1-2mg oral </li></ul><ul><li>It is a potent and rapidly acting antimuscarinic agent. </li></ul><ul><li>No central effects. </li></ul><ul><li>Used for preanesthetic medication and during anesthesia. </li></ul>
  9. 9. <ul><li>Tertiary amines </li></ul><ul><li>Dicyclomine </li></ul><ul><li>20mg oral </li></ul><ul><li>Weak anticholinergic property </li></ul><ul><li>It has direct smooth muscle relaxant action (antispasmodic). </li></ul><ul><li>It also has antiemetic property. </li></ul><ul><li>Used in motion sickness, morning sickness, dysmenorrhoea and irritable bowel </li></ul><ul><li>Dicyclomine shows less s/e. </li></ul>
  10. 10. <ul><li>Oxybutynin </li></ul><ul><li>5mg BD/TDS oral, children above 5yr 2.5mg BD. </li></ul><ul><li>It has high affinity for receptors in urinary bladder & salivary glands (selective M 1 /M 3 subtypes). </li></ul><ul><li>It has additional smooth muscle relaxant and local anesthetic property. </li></ul><ul><li>Used in neurogenic bladder, spina bifida and nocturnal enuresis. </li></ul><ul><li>Flavoxate </li></ul><ul><li>Its properties and uses are similar to Oxybutynin </li></ul>
  11. 11. <ul><li>Drotaverine </li></ul><ul><li>40-80mg TDS </li></ul><ul><li>Non-anticholinergic smooth muscle antispasmodic. </li></ul><ul><li>M/A </li></ul><ul><li>This leads to elevation of intracellular cAMP/cGMP causes smooth muscle relaxation. </li></ul><ul><li>For intestinal, biliary and renal colics, irritable bowel syndrome, uterine spasms etc. </li></ul><ul><li>It can be administered orally as well as parenterally. </li></ul>5 `AMP/5`GMP Phosphodiesterase-4 Drotaverine inhibition cAMP/cGMP
  12. 12. <ul><li>s/e </li></ul><ul><li>Headache </li></ul><ul><li>Dizziness </li></ul><ul><li>Constipation </li></ul><ul><li>Flushing </li></ul><ul><li>Fall in B.P on i.v inj </li></ul>
  13. 13. <ul><li>Mydriatics </li></ul><ul><li>Mydriasis occurs either due to the contraction of dilator pupillae (e.g.:- α 1 adrenergic agonists) or by the relaxation of sphincter pupillae of eye (e.g.:- antimuscarinics) </li></ul><ul><li>Homatropine </li></ul><ul><li>1%, 2% eye drops. </li></ul><ul><li>It is 10 times less potent than atropine. </li></ul><ul><li>Instilled in eye, it acts in 45-60min </li></ul><ul><li>Mydriasis lasts 1-3days, while accommodation reverse in 1-2 days. </li></ul><ul><li>It is used in adults. Children has high ciliary muscle tone hence it produces unsatisfactory cycloplegia. </li></ul>
  14. 14. <ul><li>Cyclopentolate </li></ul><ul><li>0.5%, 1% eye drops. </li></ul><ul><li>It is potent & rapidly acting agent. </li></ul><ul><li>Mydriasis & cycloplegia occur in 30-60min and last about a day. </li></ul><ul><li>It is preferred for cycloplegic refraction. </li></ul><ul><li>Children may show transient behavioral abnormalities due to absorption of the drug after passage into the nasolacrymal duct. </li></ul><ul><li>It is used in iritis & uveitis. </li></ul>
  15. 15. <ul><li>Tropicamide </li></ul><ul><li>0.5%, 1% eye drops. </li></ul><ul><li>It has the quickest (20-40min) and briefest (3-6hrs) action. </li></ul><ul><li>It is used for refraction testing in adults and as a short acting mydriatic for fundoscopy. </li></ul>

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