Autonomic nervous system lecture 2

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Autonomic nervous system

Autonomic nervous system

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  • 1. A- CHOLIN ESTERASEA- CHOLIN ESTERASE ‫الملح‬ ‫فاضل‬ ‫محمد‬ ‫ثامر‬ ‫حسان‬‫الملح‬ ‫فاضل‬ ‫محمد‬ ‫ثامر‬ ‫حسان‬ Group – B -Group – B -
  • 2. 2- carbachol2- carbachol  PotentPotent agonist activity.agonist activity.  direct act :Nonselective (Muscarinic /direct act :Nonselective (Muscarinic / Nicotinic)Nicotinic)  ..
  • 3.  USES:USES:  1. Topically for glaucoma;1. Topically for glaucoma;  2. intraocular for miosis in surgery.2. intraocular for miosis in surgery.  3. expel gases3. expel gases  4. stimulate intestinal motility.4. stimulate intestinal motility.  5.relive urinary retention5.relive urinary retention  Side Effects:Side Effects: Corneal edema; decreased visionCorneal edema; decreased vision..
  • 4. 33--bethanecholbethanechol  ActionAction::  Potent muscarinic agonist (directlyPotent muscarinic agonist (directly stimulate Muscarinic receptors)stimulate Muscarinic receptors)  Orally effective, also administered byOrally effective, also administered by subcutaneous injection.subcutaneous injection.  Increased hydrolytic stabilityIncreased hydrolytic stability
  • 5.  Therapeutic applicationsTherapeutic applications::  For the relief of post-surgical urinaryFor the relief of post-surgical urinary retention and abdominal distention Andretention and abdominal distention And stimulate atonic bladderstimulate atonic bladder  ((Stimulant of GI tract smooth muscle andStimulant of GI tract smooth muscle and urinary bladder).urinary bladder).  Adverse effectsAdverse effects::  Low toxicity, no serious side effects.Low toxicity, no serious side effects.  Should be used with caution in asthmaticShould be used with caution in asthmatic patients.patients.
  • 6. 4-Methacholine -----4-Methacholine ----- More stable than acetylcholine.More stable than acetylcholine.  More selective action (muscarinic > nicotinic).More selective action (muscarinic > nicotinic).
  • 7. B- Natural alkaloid :B- Natural alkaloid : muscarine , arecolin ,muscarine , arecolin , pilocarpinepilocarpine
  • 8. PilocarpinePilocarpine  Natural product. Isolated from the leaves ofNatural product. Isolated from the leaves of Pilocarpus jaborandiPilocarpus jaborandi..  Actions :Actions :  decrease in IOP , miosisdecrease in IOP , miosis  stimulator of secretions.stimulator of secretions.  Available as ophthalmicAvailable as ophthalmic solution, gel, tablet .solution, gel, tablet .
  • 9.  Systemic effects:Systemic effects: include copious sweating,include copious sweating, salivation and gastric secretion.salivation and gastric secretion.  Uses:Uses:  lowering of IOP therefore Used in the treatmentlowering of IOP therefore Used in the treatment of glaucomaof glaucoma  treatment of xerostomia (dry mouth).treatment of xerostomia (dry mouth).  Adverse effects:Adverse effects:  1-blurred vision1-blurred vision  2- lacrimation2- lacrimation  3- sever sweating3- sever sweating 4-bronchospsm4-bronchospsm
  • 10. GlaucomaGlaucoma disease characterized by increase of intradisease characterized by increase of intra ocular pressure, atrophy of optic disc ,lossocular pressure, atrophy of optic disc ,loss in the field of vision.in the field of vision. Glaucoma :Glaucoma : divided into 2 typesdivided into 2 types 1-open wide angle Glaucoma (chronic)1-open wide angle Glaucoma (chronic) 2-narrow closed angle Glaucoma (acute)2-narrow closed angle Glaucoma (acute)
  • 11. Figure 14-5 Forms of primary adult glaucoma. (A) In open-angle (chronic) glaucoma, the anterior chamber angle remains open, but drainage of aqueous humor through the canal of Schlemm is impaired; (B) in closed-angle (acute) glaucoma, the angle of the iris and anterior chamber narrows, obstructing the outflow of aqueous humor.
  • 12. Parasymathomimetic drug:Parasymathomimetic drug: 1- direct acting cholinergic1- direct acting cholinergic agent (Natural and cholineagent (Natural and choline esterase )esterase ) 2- Indirect acting cholinergic2- Indirect acting cholinergic agent:agent: Divided intoDivided into reversible & irreversiblereversible & irreversible
  • 13. 2- Indirect acting cholinergic2- Indirect acting cholinergic agent:agent: Divided intoDivided into reversible & irreversiblereversible & irreversible
  • 14. reversiblereversible  Acetylcholinesterase Inhibitors (AChEI)Acetylcholinesterase Inhibitors (AChEI) (cholinesterase enzyme inhibitors (ChEI)(cholinesterase enzyme inhibitors (ChEI)  Inhibition of acetylcholinesterase (AChE)Inhibition of acetylcholinesterase (AChE) lead to increases the concentration oflead to increases the concentration of acetylcholine (ACh) in the synapse.acetylcholine (ACh) in the synapse.  This results inThis results in prolonging the actionprolonging the action ofof ACh, producing both muscarinic andACh, producing both muscarinic and nicotinic responses.nicotinic responses.
  • 15. AnticholinestrasesAnticholinestrases (reversible(reversible)) Acetylcholinestrase is an enzyme thatAcetylcholinestrase is an enzyme that cleavescleaves Ach toAch to acetate and choline.acetate and choline. Drugs thatDrugs that inhibit this enzymeinhibit this enzyme provideprovide cholinergic action.cholinergic action.
  • 16. AGENTS AFFECTINGAGENTS AFFECTING CHOLINERGIC TRANSMISSIONCHOLINERGIC TRANSMISSION HemicholiniumHemicholinium LatrotoxinLatrotoxin VesamicolVesamicol Botulinus toxinBotulinus toxin CalciumCalcium PhysostigminePhysostigmine AtropineAtropine d-Tubocurarined-Tubocurarine
  • 17. 11--physostigminephysostigmine  Natural product, isolated from the seeds ofNatural product, isolated from the seeds of Physostigma venenosumPhysostigma venenosum  Physostigmine : Sensitive to heat, light,Physostigmine : Sensitive to heat, light, moisture etc.moisture etc.  Diffuses into the CNSDiffuses into the CNS
  • 18. physostigminephysostigmine Actions:Actions:  Stimulate Muscarinic & Nicotinic sits .Stimulate Muscarinic & Nicotinic sits .  StimulateStimulate NicotinicNicotinic receptors ofreceptors of neuromuscular junctions.neuromuscular junctions.  Duration of action about 2-3 hr.Duration of action about 2-3 hr.  Stimulate CNSStimulate CNS
  • 19. physostigminephysostigmine Therapeutics uses:Therapeutics uses:  Topically in eye.Topically in eye.  Anti doteAnti dote forfor atropine (atropine (treat over dose oftreat over dose of anticholinergic drugs.anticholinergic drugs.  Treatment of myasthenia gravies.Treatment of myasthenia gravies.  increase intestinal & bladder motilityincrease intestinal & bladder motility  Terminate the effect ofTerminate the effect of tubocurarine.tubocurarine.  Topical application in the treatment ofTopical application in the treatment of glaucomaglaucoma
  • 20. physostigminephysostigmine Adverse effects:Adverse effects: -convulsions-convulsions -Bradycardia-Bradycardia -paralysis of skeletal muscles-paralysis of skeletal muscles
  • 21. 22--neostigmineneostigmine  Chemically more stable than physostigmineChemically more stable than physostigmine  Longer duration of action (2-4 hr)Longer duration of action (2-4 hr)  Neostigmine administered orally or ivNeostigmine administered orally or iv *adverse effects:*adverse effects: generalized cholinergic stimulation.generalized cholinergic stimulation.
  • 22. **Therapeutics uses:Therapeutics uses: 1-1- stimulate bladder & GIT.stimulate bladder & GIT. 2- antidote of tubocurarine.2- antidote of tubocurarine. 3- treat of myasthenia gravis.3- treat of myasthenia gravis. 4-4- The most frequent use of neostigmine isThe most frequent use of neostigmine is to prevent atony of the intestinal, skeletal,to prevent atony of the intestinal, skeletal, and bladder musculature.and bladder musculature.  5- Also used as urinary stimulant.5- Also used as urinary stimulant.
  • 23. Myasthenia gravisMyasthenia gravis Autoimmune diseaseAutoimmune disease Ab againstAb against Ach receptorsAch receptors at neuromuscular junctionat neuromuscular junction Weakness of skeletal musclesWeakness of skeletal muscles Edrophonium used for diagnosisEdrophonium used for diagnosis Neostigmine , pyridostigmine used for treatmentNeostigmine , pyridostigmine used for treatment
  • 24. 33--pyridostigminepyridostigmine ** treatment of myasthenia gravis** treatment of myasthenia gravis **duration of action 3-6hr.**duration of action 3-6hr.  PyridostigminePyridostigmine is the most widelyis the most widely used for the treatment of myastheniaused for the treatment of myasthenia gravisgravis
  • 25. 44--EdrophoniumEdrophonium  Administered parenterallyAdministered parenterally  Rapid onsetRapid onset  short duration of actionshort duration of action 10-20 min( short10-20 min( short acting )acting )  Also exhibits direct cholinomimetic effect onAlso exhibits direct cholinomimetic effect on skeletal muscleskeletal muscle  Used in the Diagnosis of myasthenia gravis.Used in the Diagnosis of myasthenia gravis.  Over dose cause cholinergic crisisOver dose cause cholinergic crisis  Atropine is the antidoteAtropine is the antidote
  • 26. Irreversible cholinestraseIrreversible cholinestrase inhibitorsinhibitors 1- organophosphorus ;;1- organophosphorus ;; ((malathion & parathionmalathion & parathion)) :used in:used in insecticideinsecticide 2- Tabun & Sarin : nerve gas (chemical war2- Tabun & Sarin : nerve gas (chemical war agent )agent )
  • 27.  Irreversible InhibitorsIrreversible Inhibitors  Compounds containingCompounds containing phosphoryl orphosphoryl or phosphonic groupphosphonic group that can react with ChEthat can react with ChE to form ChE-phosphate complexes stable toto form ChE-phosphate complexes stable to hydrolytic cleavage.hydrolytic cleavage.  Mainly used as agricultural insecticides andMainly used as agricultural insecticides and nerve gas agents.nerve gas agents.
  • 28. Mechanism of actionMechanism of action  Combined of o.p.c with choline esteraseCombined of o.p.c with choline esterase enzyme irreversible & formation anewenzyme irreversible & formation anew compoundcompound  O.p.c + chE -------------- o.pO.p.c + chE -------------- o.p——chEchE  O.p.c highly lipid solubleO.p.c highly lipid soluble
  • 29. Adverse effects ofAdverse effects of organophosphate compoundsorganophosphate compounds::  Miosis , RhinorrheaMiosis , Rhinorrhea  Frontal headache , BronchoconstrictionFrontal headache , Bronchoconstriction  Laryngospasm , SalivationLaryngospasm , Salivation  GIT disturbances , BradycardiaGIT disturbances , Bradycardia  Sweating , LacrimationSweating , Lacrimation  Involuntary micturition , Muscle weaknessInvoluntary micturition , Muscle weakness  Ataxia, confusion ,Ataxia, confusion ,  DeathDeath
  • 30. treatmenttreatment  1- stop exposure1- stop exposure  2-wash skin2-wash skin  3-oxygen supply .3-oxygen supply .  4 replace fluid .4 replace fluid .  5-atropine5-atropine  6- 2-PAM(Pralidoxime)6- 2-PAM(Pralidoxime)
  • 31. Reactivation of acetylecholinestraseReactivation of acetylecholinestrase  PralidoximePralidoxime synthetic compound that cansynthetic compound that can reactivatereactivate thethe acetylcholinestrase if its given beforeacetylcholinestrase if its given before agingaging ofof enzyme ((aging mean: loss of an alkyl gp fromenzyme ((aging mean: loss of an alkyl gp from the structure of enzyme)).the structure of enzyme)). PralidoximePralidoxime :Effective antidote for poisoning:Effective antidote for poisoning byby parathion and related pesticidesparathion and related pesticides •• Most effective by intramuscular, intravenous, orMost effective by intramuscular, intravenous, or subcutaneous administrationsubcutaneous administration •• Treatment is effective if initiated within fewTreatment is effective if initiated within few hourshours