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Cholinoceptor Blocking Drugs

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Cholinoceptor Blocking Drugs Classification Base on specific receptor affinities Antimuscarinic agents Antinicotinic agents( consist of ganglion-blockers and ... – PowerPoint PPT presentation

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Title: Cholinoceptor Blocking Drugs


1
Cholinoceptor Blocking
Drugs
2
Classification
  • Base on specific receptor affinities
  • Antimuscarinic agents
  • Antinicotinic agents( consist of
    ganglion-blockers and neuromuscular junction
    blockers)

3
Atropine and its alkaloids
  • Atropine
  • Anisodamine
  • Acopolamine

4
chemistry and pharmacokinetics
  • Tertiary amine alkaloid esters of tropic acid
  • Well absorbed from the gut and across the
    conjunctival membrane
  • Widely distributed
  • Metabolism and excretion

5
Pharmacological Effects
  • Glands
  • Sweat, salivary gland secretion are greatly
    reduced
  • Bronchial secretion decreased
  • Reduction in gastric secretion and total acid
    content, especially at doses greater than 1 mg

6
Pharmacological Effects
  • Eye
  • Mydriasis
  • ocular pressure increase
  • cycloplegia

7
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10
Pharmacological Effects
  • Smooth muscle
  • Gastrointestinal tract relax
  • Genitourinary tract relax, void slowly

11
Pharmacological Effects
  • Cardiovascular system
  • Heart rateLower doses Presynaptic receptor
    blocked bradycardia
  • At moderate to high therapeutic doses
    tachycardia
  • Atrioventricular conduction
  • In toxic concentrations intraventricular
    conduction block

12
Pharmacological Effects
  • blood vessel and pressure
  • Vasodilation and hypopiesis caused by
    cholinnergic nerve can be blocked
  • At toxic doses, cutaneous vasodilation

13
Pharmacological Effects
  • CNS
  • At normal doses, minimal stimulant effect
  • In toxic doses, excitement, agitation,
    hallucinations and coma

14
Clinical uses
  • Relieve hyperkinesia
  • Inhibit secretion
  • Ophthalmology iritis, optometry
  • Arrhythmia
  • shock
  • Cholinergic poisoning

15
Clinical uses
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16
Adverse effects
  • Dry mouth, mydriasis, tachycardia, hot and
    flushed skin, agitation and delirium
  • Hyperthermic effects dangerous when overdose in
    infants/children
  • CNS hallucinations, coma

17
Rescue
  • Catharsis
  • Physostigmine
  • CNS diazepam

18
Anisodamine
  • Pharmacodynamics similar to atropine
  • Clinical uses shock

19
Scopolamine
  • CNS inhibited
  • Take before anaesthesia
  • motion sickness
  • Parkinsons disease

20

mydriatic

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21
  • Quaternary antimuscarinic drug propantheline
    bromide
  • Triple antimuscarinic drug
  • Pakinsons disease
  • benactyzine

22
  • Pirenzepin
  • Block M1, M4 receptor selectively
  • Ulcer, chronic bronchitis

23
NN Cholinoceptor Blocking Drugs
  • ganglionic blocking drugs
  • Mecamylamine, trimetaphan camsilate

24
pharmacodynamics
  • Block N1-receptors in ganglion competitively,
    decrease blood pressure
  • Small artery Relax, decrease blood vessle
    resistance
  • Venulae relax, decrease blood volume returing to
    heart

25
Clinical use
  • Decompression in anesthesia and operation of
    aortic aneurysm

26
Adverse response
  • Much and severe adverse responsespostural
    hypotension, retention of urine, etc.

27
N2 Cholinoceptor Blocking Drugs
  • Skeletal muscle relaxants
  • It combines with N2-receptor of motor end-plate
    on postsynaptic membrane, the transmission of
    nerve impulse is blocked, leading to skeletal
    muscle relaxation.

28
  • divide into two classes on the basis of their
    mechanism of action
  • Depolarizing muscular relaxants succinylcholine
  • Nondepolarizing muscular relaxants
    d-tubercurarine

29
Depolarizing muscular relaxants
  • Mechnism
  • Binds to Nm receptor
  • Depolarize longer than Ach
  • Depolarization nondepolarization

30
Depolarizing muscular relaxants
  • Quiver before relaxation
  • Acute tolerance
  • Cholinesterase inhibitors can strength its
    effects
  • Can not block NN-receptors in ganglion

31
Succinylcholine
  • Clinical uses
  • Guttural muscle are more sensitive to
    succinylcholine
  • Bronchoscope examination, esophagoscope
    examination

32
Adverse responses
  • Asphyxia
  • Fascicle quiver
  • blood plasma
  • Idiosyncratic reaction

33
Nondepolarizing muscular relaxants
  • d-tubercurarine
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