Ch.

11 anticholinergic drugs

R1
 The pharmacology of drugs that block
muscarinic receptors
cf)nondepol.NM blocking agent-nicotinic Rc.
Antimuscarinic
the mechanism of action and clinical
pharmacology
-atropine
-scopolamine
-glycopyrrolate
 <Mechanisms of action>
Anticholinergics are esters of an aromatic
acid an combined with an organic base
The ester linkage competitively blocks
binding by Ach. and prevent Rc.activation
Receptors subgroups
-M1(neuronal)
-M2(cardiac)
-M3(glandular)
 <clinical pharmacology>
In clinical doses, only muscarinic Rc.are blocked
The anticholinergic effects depends on the degree of
baseline vagal tone.
Cardiovascular
-tachycardia; useful in reversing bradycardia d/t
vagal reflexes (baroreceptor reflex, peritoneal
stimulation,
or oculocardiac reflex)
-AV node conduction->PR interval
-little effects on ventricular function or
pph.vasculature
-modestly enhance sympathetic activity
-large doses cutaneous blood vessel
dilatation(atropine flush)
 Respiratory
-inhibit secretion of the respiratory tract
mucosa, from nose to bronchi
-relaxation of the bronchial smooth
musculature reduces airway resistence and
anatomic dead space(esp. in COPD and
asthma)
 Cerebral
-ranging from stimulation to depression
depending on drug choice and dosage
-stimulation as excitation, restlessness, or
hallucinations
-depression as sedation and amnesia
-physostigmine(BBB) reverses these
action
 Gastrointestinal
-salivary secretion
-decreased intestinal motility and peristalsis-
>gastric emptying
-lower esophageal sphincter tone
->aspiration pneumonia
 Ophthalmic
-mydriasis and cycloplegia
Genitourinary
-urinary retention
Thermoregulation
-sweat gland
(atropine fever)
Immune mediated hypersensitivity
-little efficacy
 <specific anticholinergic drugs>
Atropine
Physical structure

Dosage and packaging

-premedication : 0.01-0.02mg/kg(up to 0.4-0.6mg/adult dose) IV,
or IM
-severe bradycardia 2mg
-cholinesterase inhibitors side effect
reverse
 Clinical considerations
1) Bronchial smooth muscle heart
-> bradyarrhythmia
2) Coronary artery dis. atropine
tachycardia


3) ipratropium bromide : Atropine
bronchospasm
acute COPD
4) CNS
(1) BBB
(2) Postop. Memory deficit
(3) toxic dose : excitatory reaction
5) 0.01-0.02 mg/kg intramuscular dose
antisialagogue effect
6) Cautious Use
(1) narrow-angle glaucoma
(2) prostatic hypertrophy
(3) bladder-neck obx.
Scopolamine
Physical structure

dosage and packaging

-Premedication : 0.01-0.02mg/kg(up to 0.4-
0.6mg/adult dose) IV, or IM -Atropine
 Clinical consideration
-atopine antisialagogue
- CNS effect
-Clinical dose : drowsiness, amnesia
(restlessness, delirium )
-(motion sickness)
-Closed angle glaucoma (best
avoided)
Glycopyrrolate
Physical structure

Dosage and packaging

dose : atropine 1/2
premedication dose : 0.005-0.01mg/kg (up to 0.2-
0.3 mg in adult )
 Clinical consideration
BBB
CNS ophthalmic activity
Salivary gland respiratory tract secretion
IV HR ( IM )
Longer duration (2-4h vs atropine 30min)