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MindMap Gallery Pharmacology-Choline receptor agonists

Pharmacology-Choline receptor agonists

Taking acetylcholine as a representative, it introduces the in vivo processes, pharmacological effects, clinical applications, adverse reactions, and contraindications of choline receptor agonists, and combines them with synthetic drugs such as methacholine, carbachol, etc. The pharmacology should be used when studying. Function is the key link, focus on combing, pay attention to compare the similarities and differences between different drugs

Edited at 2023-11-01 21:45:20

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Pharmacology-Choline receptor agonists

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Outline

choline receptor agonists

direct acting cholinomimetics

Directly stimulates choline receptors, producing M-like and N-like effects

M choline receptor agonists

Choline esters

acetylcholine

Endogenous neurotransmitters, which have no clinical value due to the presence of efficient hydrolase (acetylcholinesterase)

Pharmacological effects

M-like effect

Cardiac depression (M2)

Vagal secretion ACh

Cause vagus-like effects

Slows down myocardial contractility (negative inotropic effect)

Slow down heart rate (negative frequency effect)

Slows conduction through the atrioventricular and sinoatrial nodes (negative conduction effect)

Shorten the atrial refractory period

The vagus nerve releases acetylcholine, which acts on the M2 receptor on the atrial myocyte membrane, inhibiting the L-type calcium channel of the cardiomyocyte, reducing the influx of calcium ions, and at the same time activating the acetylcholine-dependent potassium channel, increasing the outflow of potassium ions, and shortening the plateau phase of the atrial myocytes. Effective refractory period shortened

M2 distribution density is higher in the atria than in the ventricles

Vascular (systemic) dilation (M3)

Acts on the M3 receptor of vascular endothelium, increases NO release, and causes relaxation of vascular smooth muscle

Can only cause vasodilation with intact endothelium

Smooth muscle contraction (M3)

Gastrointestinal tract: Increased contraction amplitude, tension, and peristalsis, promoting gastrointestinal secretion

Urinary tract: The bladder detrusor contracts and the bladder trigone and external sphincter relax to promote urination.

Bronchus: Smooth muscle contraction increases airway resistance

Increased glandular secretion (M3)

The most obvious increase in secretion of sweat glands, salivary glands, and tear glands

respiratory tract, bronchial glands

gastrointestinal glands

Eye(M3)

pupillary sphincter contraction, pupil constriction

Ciliary muscle contraction to regulate myopia

N-like effect (shown only in large doses)

ganglion excitement

Increased adrenal medulla secretion

skeletal muscle contraction

methacholine

Resist hydrolysis by cholinesterase and extend the action time

Selectivity: obvious effect on cardiovascular system

Clinical application

Used to treat atrial arrhythmias

Treating xerosis of oral mucosa

Contraindications

Bronchial Asthma

Bronchial smooth muscle contraction, triggering asthma

coronary ischemia

Blood vessels dilate and perfusion pressure is difficult to maintain

ulcer

Increased secretion of digestive juices, aggravating ulcers

carbachol

Not easily hydrolyzed by cholinesterase

Selectivity: It has obvious effects on the urinary tract and intestinal tract, but is not as selective as betcholine.

Clinical application: relieve postoperative abdominal distension and urinary retention, local eye drops to treat glaucoma

Mode of administration: Intravenous injection is prohibited, only for subcutaneous injection

Contraindications

Bronchial Asthma

coronary ischemia

ulcer

becholine

Not easily hydrolyzed by cholinesterase

Selectivity: obvious effect on urinary tract and intestines

Clinical application: used for postoperative abdominal distension, gastric hypotonia, and gastric retention

Contraindications

Bronchial Asthma

coronary ischemia

ulcer

alkaloids

Pilocarpine piloarpine (pilocarpine)

Pharmacological effects

Eye

anatomy of eye

Aqueous humor circulation pathway

Ciliary muscle - posterior chamber - pupil - anterior chamber - iridocorneal angle (anterior chamber angle) - scleral venous sinus - ophthalmic vein

pupillary sphincter

Innervated by the cholinergic nerve of the oculomotor nerve, the pupils contract with excitement and constriction.

pupillary dilator muscle

Innervated by noradrenergic nerves of the oculomotor nerve, excited contraction, pupil dilation

lens

Near vision, ciliary muscle contraction, suspensory ligament relaxation, and lens curvature increase

Vision of distant objects, ciliary muscle relaxation, suspensory ligament tension, lens curvature reduction

effect

miosis

Exciting M receptors, pupillary sphincter contraction

Lower intraocular pressure

The pupillary sphincter contracts, the anterior chamber angle increases, and the aqueous humor returns smoothly

Regulate spasm

Exciting the M receptor, the ciliary muscle contracts, the zonular ligament relaxes, the lens curvature increases, and the near distance is clear and the distance is blurry.

glands

Use in large doses to increase the secretion of various glands (sweat glands, salivary glands)

Clinical application

glaucoma

Low-concentration pilocarpine (less than 2%) eye drops can treat angle-closure glaucoma (congestive glaucoma)

For open-angle glaucoma (simple glaucoma), there is certain curative effect in the early stage

When used, it can compress the inner canthus of the eye to avoid central adverse reactions.

iridocyclitis

Inflammatory exudation is prone to adhesion

Use alternately with mydriasis (atropine) to prevent adhesion of the iris and lens

Taken orally to treat dry mouth

Adverse reactions

Symptoms of M receptor hyperexcitability occur after overdose, and atropine antagonism is used for treatment.

Muscarine

Not for treatment

Symptoms of poisoning

Salivation, tearing, nausea, vomiting, headache, visual disturbance, abdominal cramps, diarrhea, bronchospasm, bradycardia, drop in blood pressure, shock

N-choline receptor agonists

Nicotine

Alkaloids, highly fat-soluble and can be absorbed by the skin

No clinical value

bipolar

start to get excited

subsequent inhibition

Lobelin

Glaucoma classification

Open angle type

Hyperemia, mechanical obstruction of the anterior chamber angle by the iris

Closed angle type

Simple elevated intraocular pressure