cholinoceptor blocking agents
Download
Skip this Video
Download Presentation
Cholinoceptor Blocking Agents

Loading in 2 Seconds...

play fullscreen
1 / 15

Cholinoceptor Blocking Agents - PowerPoint PPT Presentation


  • 144 Views
  • Uploaded on

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

loader
I am the owner, or an agent authorized to act on behalf of the owner, of the copyrighted work described.
capcha
Download Presentation

PowerPoint Slideshow about 'Cholinoceptor Blocking Agents' - isaura


An Image/Link below is provided (as is) to download presentation

Download Policy: Content on the Website is provided to you AS IS for your information and personal use and may not be sold / licensed / shared on other websites without getting consent from its author.While downloading, if for some reason you are not able to download a presentation, the publisher may have deleted the file from their server.


- - - - - - - - - - - - - - - - - - - - - - - - - - E N D - - - - - - - - - - - - - - - - - - - - - - - - - -
Presentation Transcript
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
slide6
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
slide7
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
ad