CHAPTER 6 Cholinoceptor

Blocking Agents ( I )
--M Receptor Blockers

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 Atropine
Atropine is one of M receptor blockers , which inhibits the
actions of acetylcholine and cholinomimetic drugs at
muscarinic receptors in smooth muscles, heart, and
exocrine glands. In addition to these peripheral effects,
atropine by blocking the acetylcholine receptor sites in the
CNS, produces CNS effects in large dose. Atropine also
blocks the ganglionic Nl receptor in very large dose or
toxic dose. The pharmacological effects of atropine in
general are dose dependent. With the increase of dose the
following phenomena appear in turn: gland secretion
decrease, mydriasis and cycloplegia, smooth muscle of
gastrointestinal tract and urinary bladder relaxation, heart
rate increase, and CNS action. 2
Effects,uses and side reactions

1. Effects on involuntary muscles

1)Gastrointestinal tract
Effects: It decreases the amplitude and frequency
of peristaltic contractions and reduces the tone of
stomach, small intestine, colon and biliary tract
Uses: It is used for the relief of gastrospasm and
abdominal colic; combined with an opioid, it is can
used for the treatment of biliary colic.
side reaction: constipation and aerenterectasia
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Effects,uses and side reactions
2) Urinary bladder and urethra
Effects: The tone of urinary bladder and ureter
decreased, whereas vesicle sphincter tone is
increased.
Uses: It is used for the treatment of renal colic and
irritation sign of bladder.
Side reaction: retention.
3) Smooth muscle of airway
It produces slight bronchodilatation. Some
antimuscarinic agents (ipratropine) are valuable in
some patients with asthma , but not as useful as the β-
adrenergic stimulants.
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2. Effects on secretions
1) Sweat gland and salivary secretions are greatly
reduced.
Side reaction
┌Sweat secretions↓→body temperature↑
│ → flushed skin.
└Salivary secretions↓→dry mouth
2) Its ability to reduce bronchial secretion makes it
useful as a pre-anesthetic agent.
3) There is a reduction in gastric secretion and total
acid content, especially at doses greater than 1 mg.
3. Effects on the eye
1) M receptor↓→pupillary constrictor muscle↓→
mydriasis. → intraocular pressure ↑
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2)Uses:
①Treatment of iritis (alternative using pilocarpine).
②Used for funduscopic examination.
(Theαadrenergic stimulants, eg, phenylephrine,
produce a short-lasting mydriasis that is usually
more sufficient for the examination of retina.
3)Side reaction: mydriasis→narrow anterior chamber
→ induction or exacerbation of glaucoma.
Intraocular pressure rise
Cycloplagia side effects
Far vision
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4. Effects on the heart
M receptor↓→the heart↑
┌heart rate↑
│atrioventricular conduction↑
│ (shortening of P-R intreval)
└cardiac output↑
Heart rate slows initially with lower dose because of
stimulation of cardioinhibitory center. Tackycardia
then follows because of M receptor block. Higher
doses cause only tachycardia.
Uses: ①Treatment of sinus node bradycardia;
②Treatment of a high-grade atrioventricular
block
Side reaction: Rapid pulse 7
5. Effects on blood vessels
┌direct vasodilating effect
└sweat secretions↓→body temperature↑→
indirect vasodilation→flushed skin.
Atropine has little effects on blood pressure
because of both the increase in output and decrease
of total peripheral resistance
Uses: Treatment of infective shock in large doses
for relieve vasospasm of small blood vessels.

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6. Effects on the CNS
1) Large doses can produce restlessness, confusion,
disorientation, halluciation and coma
2)Central M receptor↓→antitremor activity.

Some antimuscarinic agents (benzhexol,

scopolamine) are valuable in some patients with
parkinson disease and parkinsonian syndrome.
Other antimuscarinic agents
1. Scopolamine
[Pharmacologic effects]
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1)It is more potent than atropine in: decreasing gland
secretions (bronchial, salivary and sweat); producing
mydriasis and cycloplegia.
2) It is less potent than atropine in its effects on: heart,
bronchial muscles and intestines.
3) It has a shorter duration of action, and has depre-
ssive effects on CNS and vestibular nerve.

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【 Therapeutic uses and adverse effects 】
1)Its uses and side reactions are similar to those of atropine.
2) It is more excellent for treatment of motion sickness and
Barkinson disease, and is more useful as a preanesthetic
agent.
┌ more potent in secretions──┐
│ 　　　　　 ├ as preanesthetic agent
┤ depression on CNS──── ┤
│ 　　　　　 ├ motion sickness↓
│ depression on vestibular nerve ┘
└ central antimuscarinic effects─Barkinson disorders↓

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2. Homatropine and Eucatropine
They are rapidly acting agents used to produce cycloplegia
and mydriasis for ophthalmologic examination
3. Propantheline
M↓: It is more potent and longer effects on smooth muscle
and gastric secretion, used for the relief of gastrospasm of
enuresis
N↓:N1↓→α↓,β↓→Bp↓ pamyoparalysis adverse

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• How many effects atropine has?
• How many side effects atropine has?
• Why will the rapid pulse appear when we
treatment of sinus node bradycardia?

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