Cholinoceptor blocking agents
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Cholinoceptor Blocking Agents. Pawitra Pulbutr M.Sc. In Pharm (Pharmacology). Objectives. นิสิตมีความรู้ความเข้าใจถึงเภสัชวิทยา กลไกการออกฤทธิ์ เภสัชจลนศาสตร์ การใช้ประโยชน์ทางคลินิก อาการไม่พึงประสงค์ ข้อควรระวังการใช้ยาของที่ออกฤทธิ์ต้านโคลิโนเซปเตอร์. Cholinoceptor Blocking Agents.

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Cholinoceptor Blocking Agents

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Cholinoceptor blocking agents

Cholinoceptor Blocking Agents

Pawitra Pulbutr

M.Sc. In Pharm (Pharmacology)


Objectives

Objectives

  • นิสิตมีความรู้ความเข้าใจถึงเภสัชวิทยา กลไกการออกฤทธิ์ เภสัชจลนศาสตร์ การใช้ประโยชน์ทางคลินิก อาการไม่พึงประสงค์ ข้อควรระวังการใช้ยาของที่ออกฤทธิ์ต้านโคลิโนเซปเตอร์


Cholinoceptor blocking agents1

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


Basic pharmacology of muscarinic blocker

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


Organ system effects

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 Parkinson’s disease

      • Overcholinergic activity… Too much ACh

      • Lack of dopaminergic activity in brain

      • Antimuscarinic agent + Dopamine precursor

    • Motion sickness … Vestibular disturbance

      • Scopolamine


Cholinoceptor blocking agents

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


Cholinoceptor blocking agents

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

      • >>> Modest effect in normal hemodynamic

      • Tachycardia

      • Less effect on BP


Respiratory system

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


Gi tract

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


Genitourinary tract

Genitourinary tract

  • Relaxation of ureter & bladder

  • Decrease voiding

  • Use …urinary tract spasm… inflammation

  • Caution in elderly male … BPH>>> urinary retention

  • No effect on uterus


Sweat gland

Sweat gland

  • Inhibit thermoregulatory sweating

  • Inhibit eccrine gland secretion

  • Controlled by cholinergic sympathetic nerve

  • May cause …Atropine fever


Clinical pharmacology

Clinical Pharmacology

  • Parkinson’s 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


Adrs of anticholinoceptor

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


Contraindication of atropine

Contraindication of Atropine

  • Glaucoma

    • Angle closure glaucoma

  • Elderly male

    • BPH

  • Peptic ulcer

    • Decrease gastric emptying


Cholinoceptor blocking agents

Q & A


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