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ANTICHOLINERGIC DRUGS. Anticholinergic drugs. What students should know: Student should be able to : Describe Kinetics of muscarinic antagonists The effects of atropine on the major organ systems. To list the clinical uses of muscarinic antagonists .

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ANTICHOLINERGIC DRUGS


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slide2

Anticholinergic drugs

  • What students should know:
  • Student should be able to :
  • Describe Kinetics of muscarinic antagonists
  • The effects of atropine on the major organ systems.
  • To list the clinical uses of muscarinic antagonists.
  • To know adverse effects& contraindications of anticholinergic
  • drugs.
  • To identify at least one antimuscarinic agent for each of the
  • following special uses:mydriasis, cyclopedia, peptic ulcer &
  • parkinsonism.
slide3

Anticholinergic drugs

are drugs that block cholinergic receptors.

slide4

Anticholinergic drugs

Antimuscarinics

(Parasympatholytics)

Antinicotinics

Ganglionic

blockers

Neuromuscular blockers

Naturally occurring alkaloids

synthetic atropine substitutes

slide5

Antimuscarinics

Antimuscarinics

Naturally occurring alkaloids

synthetic atropine substitutes

slide6

Antimuscarinics

Muscarinic antagonists

  • Natural alkaloids
  • Drugs as : Atropine - Hyoscine
  • Esters of tropic acid and tertiary amines
  • Lipid soluble
  • Good oral absorption
  • Good distribution
  • Cross blood brain barrier (have CNS actions)
slide7

Antimuscarinics

Muscarinic antagonists

Synthetic atropine substitutes

Benztropine

Homatropine

Tropicamaide

Pirenzepine

Ipratropium

Glycopyrrolate

Oxybutynin

slide8

Antimuscarinic drugs

Mechanism of action

  • Reversible competitive blockade of muscarinic receptors.
  • Atropine can block all muscarinic receptors.
slide9

Pharmacological effects of

atropine

CNS

  • Sedation
  • Antiemetic effect (block vomiting center)
  • antiparkinsonian effect (block basal ganglia).
  • Toxic dose:

Hyperthermia - excitement-hallucination.

slide10
Cardiovascular system (CVS)
  • Tachycardia (increase in heart rate)
  •  AV conduction ( + ve dromotropic effect)
  • Therapeutic dose:  Vasodilatation induced by cholinomimetics.
  • Toxic dose: Cutaneous vasodilatation  (atropine flush).

Respiratory system

  • Relaxation of bronchial muscles (bronchodilator)
  •  Bronchial secretion  viscosity
slide11
Eye
  • Passive mydriasis

due to paralysis of circular muscle

  • Cycloplegia (loss of near accommodation)

due to paralysis of ciliary muscle.

  • Loss of light reflex.
  • increase I.O.P # glaucoma.
  •  Lacrimal secretion  sandy eye
slide12
Secretions

Salivary secretion  ( Dry mouth ).

 Sweating  Dry skin  Fever in infants and children.

 Bronchial secretion   Viscosity

Lacrimal secretion  Sandy eye

slide13
GIT
  • Relaxation of smooth muscles.
  •  GIT motility Antispasmodic effect.
  •  Sphincter contractions
  • Constipation

Urinary Tract

  • Relaxation of smooth muscles of urinary bladder.
  • Sphincter contraction.
  • Urinary retention.
slide14
Hyoscine (SCOPOLAMINE)

What is difference between atropine and hyoscine?

Hyoscine has

Shorter duration of action

More CNS depressant action

Antiemetics action in motion sickness

Can produce amnesia.

Less CVS effect

slide18
Adverse effects

Eye: Blurred vision – Mydriasis

CVS: Tachycardia - Atropine flush

GUT:Urinary retention

GIT: Constipation, paralytic ileus

Secretions: Dryness of mouth , Sandy eye

Increased body temperature.

CNS: sedation, hallucination, excitation (Toxic dose).

Treatment

  • Gastric lavage.
  • Anticonvulsant.
  • Cooling blanket.

Antidote: Physostigmine ( IV slowly).

slide19
Contraindications
  • Glaucoma (angle closure glaucoma)
  • Tachycardia
  • Prostate hypertrophy in old patients.
  • Constipation, paralytic ileus, intestinal obstruction.
  • Children in case of atropine
slide20

Can antimuscarinic drugs reverse the action

of neostigmine on skeletal muscles?

slide21
SUMMARY
  • Antimuscarinics reverse action of cholinomimetics on muscarinic receptors.
  • Are useful in many applications including intestinal spasm, constipation, urinary retention, vomiting, parkinsonism, asthma and peptic ulcer.
  • Are contraindicated in constipation, Prostate hypertrophy, tachycardia and glaucoma.