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Cholinoceptor Blocking Agents

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Cholinoceptor Blocking Agents Pawitra Pulbutr M.Sc. In Pharm (Pharmacology) Objectives ... – PowerPoint PPT presentation

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Title: Cholinoceptor Blocking Agents


1
Cholinoceptor Blocking Agents
  • Pawitra Pulbutr
  • M.Sc. In Pharm (Pharmacology)

2
Objectives
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3
Cholinoceptor Blocking Agents
  • Inhibit binding of ACh or cholinoceptor agonist
    to cholinoceptor
  • Cholinoceptor antagonist/ blocker
  • Parasympatholytic Not appropriate
  • Antimuscarinic receptor
  • Antinicotinic receptor
  • Ganglionic blocker
  • Neuromuscular blocker

4
Basic Pharmacology of Muscarinic blocker
  • Prototype Atropine
  • Tertiary amine derivative
  • Quaternary amine derivative increase peripheral
    effect
  • Atropine (Hyoscyamine)
  • Atropa belladonna (deadly nightshade)
  • Datura stramonium (jimsonweed or thorn apple)
  • L (-) hyoscyamine natural occur
  • d,l- hyoscyamine commercial available
  • Scopolamine (Hyoscine)
  • Hyoscyamus niger
  • L (-) hyoscine natural occur
  • L-isomer is more active than d-isomer

5
Organ System Effects
  • CNS
  • Atropine
  • CNS stimulation also sedative effect
  • Scopolamine More CNS effect
  • Drowsiness, amnesia
  • Toxic dose excitement, agitation,
    hallucination, coma
  • Use
  • Tremor in Parkinsons disease
  • Overcholinergic activity Too much ACh
  • Lack of dopaminergic activity in brain
  • Antimuscarinic agent Dopamine precursor
  • Motion sickness Vestibular disturbance
  • Scopolamine

6
Eyes
  • Cholinoceptor Control pupillary contractor
    muscle ciliary muscle
  • Anticholinoceptor
  • Mydriasis
  • Inhibit ciliary muscle contraction
  • Cycloplegia
  • Focus defect
  • Use in ophthalmology
  • Caution in glaucoma increase intraocular
    pressure
  • Decrease lacrimal secretion, sandy eyes

7
CVS
  • Atropine at heart
  • Low dose Inhibit presynaptic cholinoceptor
    first increase ACh release bradycardia
  • Moderate to high dose Relative tachycardia
  • AV node
  • () dromotropic Shorten PR interval
  • Less effect on ventricle
  • Total effect of Atropine
  • gtgtgt Modest effect in normal hemodynamic
  • Tachycardia
  • Less effect on BP

8
Respiratory system
  • Vagal innervation Smooth muscle secretory
    gland
  • Atropine
  • Bronchodilation
  • Decrease secretion
  • Use
  • Asthma less effective than ?2-agonist
  • Chronic Obstruction Pulmonary Disease (COPD)
  • Premedication of inhalant anesthetic agent
    decrease secretion laryngospasm

9
GI tract
  • Decrease GI motility secretion
  • Prolong gastric emptying time intestinal
    transit time
  • Partially effect ENS controlled by local
    hormone other noncholinergic neuron
  • Decrease saliva dry mouth
  • Less effect on gastric secretion
  • Mostly on basal secretion
  • Pirenzepine, Telezepine decrease gastric acid
    secretion
  • No effect on pancreatic intestinal secretion
    under hormonal control
  • Use
  • Peptic ulcer Not use recently
  • Control diarrhea from parasympathetic system
    overactive
  • Spasmolytic action

10
Genitourinary tract
  • Relaxation of ureter bladder
  • Decrease voiding
  • Use urinary tract spasm inflammation
  • Caution in elderly male BPHgtgtgt urinary
    retention
  • No effect on uterus

11
Sweat gland
  • Inhibit thermoregulatory sweating
  • Inhibit eccrine gland secretion
  • Controlled by cholinergic sympathetic nerve
  • May cause Atropine fever

12
Clinical Pharmacology
  • Parkinsons disease
  • Motion sickness
  • Mydriasis
  • Adjunct to general anesthesia
  • Asthma/ COPD
  • Hyperactive carotid sinus reflex fainting
  • Antispasmodic, traveller diarrhea, peptic ulcer
  • Urinary urgency
  • Urolithiasis
  • Cholinergic poisoning

13
ADRs of anticholinoceptor
  • Depends on desired effect
  • Cholinoceptor blocking effect
  • Dry mouth, mydriasis, tachycardia, hot flush,
    agitation, delirium, increase body temperature
    (esp infant)
  • Reversal of atropine overdosage
  • Symptomatic
  • ACh E inhibitor physostigmine ADRs

14
Contraindication of Atropine
  • Glaucoma
  • Angle closure glaucoma
  • Elderly male
  • BPH
  • Peptic ulcer
  • Decrease gastric emptying

15
Q A
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