BY
SYED FAYYAZUDDIN
1/30/2015 1
CONTENTS
 INTRODUCTION
 CLASSIFICATION
 PHARMACOLOGICAL ACTIONS
 DRUGS
 USES
1/30/2015 2
INRODUCTION
 Acetylcholine.
1/30/2015 3
Receptor Location
M1 CNS, Postganglionic neurons.
M2 Myocardium, Smooth muscles.
M3 Exocrine glands, Smooth muscles.
M4 CN...
1/30/2015 5
1/30/2015 6
MECHANISM OF ACTION
IP3 DAG cAMP Na+/K+
1/30/2015 7
 Blocks action of Ach on autonomic effectors through
muscarinic receptors.
 Competitive antagonists.
 Prototype Atropin...
Classification
 1. Natural alkaloids:
 Atropine
 Hyoscine
 2. Semisynthetic derivatives:
 Homatropine
 Hyoscine buty...
 3. Synthetic compounds:
A.Mydriatics:
 Tropicamide
B.Antisecretory-antispasmodic:
 Dicyclomine.
 Propanthaline.
 Bip...
 GANGLIONIC BLOCKING AGENTS.
 COMPETATIVE BLOCKERS
 Hexamethonium
 Mecamylamine
 PERSISTANT DEPOLARISING BLOCKERS
 N...
PHARMACOLOGICAL ACTIONS
 CNS
 Stimulates many medullary centres.
 Vagal, respiratory and vasomotor.
 Anti-motion sickn...
 CVS
 primarily in modifications of the heart rate:
 very low dose, it can give a slight cardiac slowing
 therapeutic ...
PHARMACOLOGICAL ACTIONS
 EYS
 Mydriasis
 Cycloplegia
 Photophobia.
 SMOOTH MUSCLES
 Relaxation
 M3 Blokade
 Tone i...
PHARMACOLOGICAL ACTIONS
 GLANDS
 Sweat
 Bronchial secretions
 Lacrinal secretions.
 Acid, pepsin and mucus in stomach...
Sensitivity
Gastric
glands and
smooth
muscle.
Smooth
muscle
intestine and
bladder.
Eye,
bronchial
muscle and
heart.
Saliva...
TROPICAMIDE
 Blocks the response of sphincter muscle of iris and ciliary
muscles to cholinergic stimulation thus causing ...
 ADVERSE REACTIONS:
 Blurred vision
 Photo phobia
 Increased intraocular pressure
 Dry mouth
 Tachycardia
 Headache...
DICYCLOMINE
 It is a smooth muscle relaxant.
 Irritable Bowel Syndrome (also known as spastic colon).
 It relieves musc...
ADVERSE REACTIONS:
 Dry mouth
 Tachycardia
 Headache
 Allergic reactions
 Nausea
 Vomiting
 confusion
 agitation
HEXAMETHONIUM
 Ganglionic blocker
 N receptor antagonist, acts in autonomic ganglia.
 Does not have any effect on musca...
 ADVERSE EFFECTS :
 Constipation
 Urinary retention
 Glaucoma
 Blurry vision
 Decreased lacrymal secretion
 Dry mou...
USES
 Antisecretory
 Preanaesthtic
 The main reasons for using anticholinergic drugs were
drying of secretions and prot...
 Antispasmodic
 Spactic constipation
 Nervous and drug induced diarrhoea.
 Asthama, COPD
 Cardiac vagolytic
 Bradyca...
References
 Tripathi KD. Anticholinergic drugs.In Essentials of medical
Pharmacology. 5th ed. JP Brothers Medical publish...
Syed parasympatholytics
Syed parasympatholytics
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Syed parasympatholytics

  1. 1. BY SYED FAYYAZUDDIN 1/30/2015 1
  2. 2. CONTENTS  INTRODUCTION  CLASSIFICATION  PHARMACOLOGICAL ACTIONS  DRUGS  USES 1/30/2015 2
  3. 3. INRODUCTION  Acetylcholine. 1/30/2015 3
  4. 4. Receptor Location M1 CNS, Postganglionic neurons. M2 Myocardium, Smooth muscles. M3 Exocrine glands, Smooth muscles. M4 CNS M5 CNS M6 CNS M7 CNS M8 CNS M9 CNS M10 HEART M11 BRONCHI M12 BRONCHI M13 CNS NN Postganglionic neurons. NM Skeletal muscles. 1/30/2015 4
  5. 5. 1/30/2015 5
  6. 6. 1/30/2015 6
  7. 7. MECHANISM OF ACTION IP3 DAG cAMP Na+/K+ 1/30/2015 7
  8. 8.  Blocks action of Ach on autonomic effectors through muscarinic receptors.  Competitive antagonists.  Prototype Atropine. 1/30/2015 8
  9. 9. Classification  1. Natural alkaloids:  Atropine  Hyoscine  2. Semisynthetic derivatives:  Homatropine  Hyoscine butyl bromide  Atropine methonitrate. 1/30/2015 9
  10. 10.  3. Synthetic compounds: A.Mydriatics:  Tropicamide B.Antisecretory-antispasmodic:  Dicyclomine.  Propanthaline.  Biperden. C.Antiparkinsonian:  Tryhexyl phenidyl. 1/30/2015 10
  11. 11.  GANGLIONIC BLOCKING AGENTS.  COMPETATIVE BLOCKERS  Hexamethonium  Mecamylamine  PERSISTANT DEPOLARISING BLOCKERS  Nicotine  Anticholinesterases 1/30/2015 11
  12. 12. PHARMACOLOGICAL ACTIONS  CNS  Stimulates many medullary centres.  Vagal, respiratory and vasomotor.  Anti-motion sickness property.  High dose cause  Restlessness  Disorientation  Hallucinations  Respiratory depression  Coma. 1/30/2015 12
  13. 13.  CVS  primarily in modifications of the heart rate:  very low dose, it can give a slight cardiac slowing  therapeutic dose there is generally cardiac acceleration  It does not have vascular effects since there is no parasympathetic tonus on the vessels but it inhibits vasodilatation caused by an intravenous injection of acetylcholine.  It does not induce modifications of arterial pressure in spite of increased cardiac rate.  in very high or toxic dose, it induces a fall of the arterial pressure by depression of the vasomotor centers 1/30/2015 13
  14. 14. PHARMACOLOGICAL ACTIONS  EYS  Mydriasis  Cycloplegia  Photophobia.  SMOOTH MUSCLES  Relaxation  M3 Blokade  Tone is reduced  Constipation  Bronchodilation (asthma) 1/30/2015 14
  15. 15. PHARMACOLOGICAL ACTIONS  GLANDS  Sweat  Bronchial secretions  Lacrinal secretions.  Acid, pepsin and mucus in stomach.  BODY TEMPERATURE  Inhibition of sweating  Temperature regulatory centre in hypothalamus  Atropine fever 1/30/2015 15
  16. 16. Sensitivity Gastric glands and smooth muscle. Smooth muscle intestine and bladder. Eye, bronchial muscle and heart. Saliva , sweat, bronchial secretions. 1/30/2015 16
  17. 17. TROPICAMIDE  Blocks the response of sphincter muscle of iris and ciliary muscles to cholinergic stimulation thus causing mydriasis.  Stronger preparation also paralyzes accommodation.  Acts within 15-30 m and duration is 3-8 h.  typically used during eye examinations such as the dilated fundus examination, but it may also be used before or after eye surgery.
  18. 18.  ADVERSE REACTIONS:  Blurred vision  Photo phobia  Increased intraocular pressure  Dry mouth  Tachycardia  Headache  Allergic reactions  Nausea  Vomiting
  19. 19. DICYCLOMINE  It is a smooth muscle relaxant.  Irritable Bowel Syndrome (also known as spastic colon).  It relieves muscle spasms and cramping in the gastrointestinal tract by blocking the activity of acetylcholine on cholinergic (muscarinic) receptors on the surface of muscle cells.
  20. 20. ADVERSE REACTIONS:  Dry mouth  Tachycardia  Headache  Allergic reactions  Nausea  Vomiting  confusion  agitation
  21. 21. HEXAMETHONIUM  Ganglionic blocker  N receptor antagonist, acts in autonomic ganglia.  Does not have any effect on muscarinic Ach receptors.  Acts at receptors at neuromuscular junction responsible for skeletal muscle motor response.
  22. 22.  ADVERSE EFFECTS :  Constipation  Urinary retention  Glaucoma  Blurry vision  Decreased lacrymal secretion  Dry mouth (xerostomia)
  23. 23. USES  Antisecretory  Preanaesthtic  The main reasons for using anticholinergic drugs were drying of secretions and protection against vagal over activity.  Blocks responses to vegal refluxes induced by sergical manipulations of visceral organs.  Peptic ulcer  Pulmonary embolism 1/30/2015 24
  24. 24.  Antispasmodic  Spactic constipation  Nervous and drug induced diarrhoea.  Asthama, COPD  Cardiac vagolytic  Bradycardia  Central actions  Parkinsonism  Motion sickness 1/30/2015 25
  25. 25. References  Tripathi KD. Anticholinergic drugs.In Essentials of medical Pharmacology. 5th ed. JP Brothers Medical publishers (P) Ltd: New Delhi; 2003. pp. 93-102.  Katzung, Bertram.G, Basic and clinical pharmacology.10th ed. Mc Graw Hill. USA(NY); 2006. pp. 482-9.  Goodman & Gilman’s, The Pharmacological Basis Of Therapeutics. 11th ed. Mc Graw Hill. USA(NY); 2006. pp. 121- 9. 1/30/2015 26
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