MindMap Gallery Pharmacology 9th Edition Chapter 8 Choline Receptor Blocking Drugs (I) - M Choline Receptor Blocking Drugs
This is a mind map about pharmacology-M choline receptor blocking drugs, including atropine and its similar alkaloids, Atropine versus synthetic substitutes, etc.
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This is a mind map about bacteria, and its main contents include: overview, morphology, types, structure, reproduction, distribution, application, and expansion. The summary is comprehensive and meticulous, suitable as review materials.
This is a mind map about plant asexual reproduction, and its main contents include: concept, spore reproduction, vegetative reproduction, tissue culture, and buds. The summary is comprehensive and meticulous, suitable as review materials.
This is a mind map about the reproductive development of animals, and its main contents include: insects, frogs, birds, sexual reproduction, and asexual reproduction. The summary is comprehensive and meticulous, suitable as review materials.
Chapter 8 Choline Receptor Blocking Drugs (I)—M Choline Receptor Blocking Drugs
Section 1 Atropine and its similar alkaloids
atropine
Pharmacological effects and mechanisms
Atropine has high selectivity for M receptors, but low selectivity for each subtype of M receptors. High-dose atropine also has a blocking effect on ganglion N receptors
Tip: The antagonistic effect of atropine on exogenous choline esters is much stronger than that of endogenous ACh.
1. Glands: inhibitory effect. The most obvious effect on salivary glands (M3) and sweat glands
2. Eyes: dilation of pupils, increase in intraocular pressure, and accommodation paralysis (opposite to pilocarpine)
(1) Pupil dilation: blocks the M receptor on the pupillary sphincter, causing the pupillary sphincter to relax
(2) Increased intraocular pressure: Due to the dilation of the pupil, the iris retreats to the edge, narrowing the anterior chamber angle gap and hindering the reflux of aqueous humor. Therefore, it is contraindicated for patients with glaucoma.
(3) Accommodative paralysis: clear vision of distant objects. (As opposed to pilocarpine, which “regulates spasms”)
3. Smooth muscle: It has a relaxing effect on a variety of visceral smooth muscles innervated by cholinergic nerves. Gastrointestinal tract > Bladder > Ureter, bile duct, bronchi > Uterus
4. Cardiovascular system
(1) Heart: A therapeutic dose of atropine can temporarily and slightly slow down the heart rate; a larger dose of atropine can block the M2 receptors in the sinoatrial node, relieve the inhibitory effect of the vagus nerve on it, and accelerate the heart rate.
(2) Blood vessels: dilate blood vessels and improve microcirculation (small blood vessels in the periphery and internal organs)
5. Excitement center
Clinical application
1. Relieve smooth muscle spasm
Effective for gastrointestinal colic, bladder irritation and enuresis
For renal and biliary colic, it needs to be combined with analgesics (Meperidine)
2. Inhibit gland secretion: used for administration before general anesthesia to reduce the secretion of respiratory glands and salivary glands to prevent secretions from blocking the respiratory tract and the occurrence of aspiration pneumonia.
3. Ophthalmology
Iridocyclitis: Atropine can relax the iris pupillary sphincter and ciliary muscles, allowing them to fully rest, which is beneficial to the resolution of inflammation. It can also be used in combination with miotic drugs (pilocarpine) to prevent adhesion between the iris and the lens.
Optometry, fundus examination: pupil dilation
4. Bradyarrhythmia: Atropine can relieve the inhibitory effect of the vagus nerve on the heart For sinus bradycardia caused by vagus nerve overexcitation.
5. Anti-shock
6. Rescue organophosphate poisoning
Adverse reactions: dry mouth, blurred vision, accelerated heart rate, dilated pupils and flushed skin, etc.
Atropine poisoning Central symptoms - physostigmine Peripheral symptoms—pilocarpine
Contraindications: Glaucoma and prostatic hypertrophy (may aggravate urination difficulty)
Scopolamine
Functional characteristics
1. Strong effect on glands and eyes, weak effect on cardiovascular and smooth muscles
2. Has an inhibitory effect on the CNS
3. Anti-motion sickness and anti-vomiting
4. Anti-Parkinson’s disease
5. Euphoric effect
Anisodamine
Characteristics of action: Its cardiovascular effects are equivalent to those of atropine, while others are weaker than atropine. High selectivity and few side effects
Usage: Gastrointestinal colic, infection, toxic shock
Section 2 Atropine versus synthetic substitutes
1. Synthetic mydriatic drugs: such as homatropine and trocaramide. The duration of its pupil dilating effect is significantly shortened
2. Synthetic antispasmodics
(1) Quaternary ammonium antispasmodic drugs: propantheline bromide (probenthene). For gastric and duodenal ulcers
(2) Tertiary amine antispasmodic drugs: Benatezin (Weifukang). It can relieve smooth muscle spasm, inhibit gastric acid secretion, and has a central sedative effect. Suitable for ulcer patients with anxiety disorder
3. Selective M receptor blockers: pirenzepine, selective M1 receptor blockers