MindMap Gallery Pharmacology Chapter 6 and 7 Choline receptor agonists, anticholinesterase drugs and cholinesterase reactivating drugs
This is a mind map about pharmacology chapters 6 and 7. The main content includes: anticholinesterase drugs, cholinesterase reactivating drugs, and choline receptor agonists.
Edited at 2024-03-13 19:56:34This 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.
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.
choline receptor agonists
M choline receptor agonists
Choline esters
AcetylcholineACH
Widely used, no clinical value
Pharmacological effects
Cardiovascular System
Relax blood vessels throughout the body
Stimulates the M3 choline receptor subtype of vascular endothelial cells, resulting in the release of endothelium-dependent relaxing factor nitric oxide, thereby causing relaxation of adjacent smooth muscle cells
Stimulates M receptors in the presynaptic membrane of noradrenergic nerve terminals, inhibits the release of NA, and produces vasodilation.
to the heart
weaken myocardial contractility
The ventricle has less cholinergic innervation, so the direct effect of ACh on the heart is mainly in the atrium
The effect on the ventricle is mainly caused indirectly by affecting noradrenergic nerve activity.
Slow down heart rate: negative frequency effect
Slows down atrioventricular node and Purkinje fiber conduction
Shorten the atrial refractory period
Exciting gastrointestinal tract, detrusor, bronchi
Promote abdominal secretion of glands
carbachol
Topical eye drops to treat glaucoma
methacholine
becholine
Alkaloids
Pilocarpine
Pharmacological effects
Eye to eye
miosis
Activates pupillary sphincter M choline receptors
Reduce intraocular pressure
Through the miotic effect, the iris is pulled toward the center, which expands the anterior chamber angle gap around the iris, promotes the reflux of aqueous humor, and reduces intraocular pressure.
Regulate spasm
The ciliary muscle contracts, the suspensory ligament relaxes, and the lens becomes convex, making it possible to see near objects but difficult to see distant objects.
Increase the secretion of sweat and salivary glands
Clinical application
Treat glaucoma
iridocyclitis
Muscarine
N receptor agonists
There are two subtypes of N-choline receptors, NM and NN: NM receptors are distributed in skeletal muscles, and NN receptors are distributed in the brachyonode and adrenal medulla.
Nicotine: has biphasic properties: transient stimulation of NN receptors followed by sustained inhibition of the receptors
Anticholinesterase drugs and cholinesterase reactivating drugs
anticholinesterase drugs
Reversibility
Pharmacological effects
Eye
Causes pupil constriction and ciliary muscle accommodation spasm, causing vision to adjust to a myopic state
Can promote aqueous humor reflux, thereby increasing intraocular pressure
Exciting gastrointestinal tract
Clinical application
myasthenia gravis
Bloating and urinary retention
glaucoma
Commonly used medicines
neostigmine
Oral absorption is small and irregular
Not easily accessible to the central nervous system.
Inhibit AChE
It can directly stimulate N receptors on the motor end plates of skeletal muscles and has a strong excitatory effect on skeletal muscles. Exciting gastrointestinal smooth muscle, followed by
treat
Treating myasthenia gravis
Intestinal paralysis after abdominal surgery
Paroxysmal supraventricular tachycardia and toxic effects in overdose with countercompetitive neuromuscular blocking drugs
Irreversibility-organophosphates
Covalently binds to AChE
acute poisoning
M-like
Nausea, vomiting, abdominal pain, incontinence, salivation, increased bronchial secretion, dyspnea, sweating, miosis, slowed heart rate and decreased blood pressure, etc.
N kinds
neuromuscular junction
Muscle weakness, involuntary muscle fasciculations, tremors
Central Nervous System
Convulsions, restlessness, etc.
chronic poisoning
Diagnosis and treatment of poisoning
eliminate poison
Remove patient from site and remove contaminated clothing
If the skin is affected, wash the skin with warm water and soap.
For patients with oral poisoning, gastric juice and poisons should be extracted first, and gastric lavage should be performed repeatedly with lukewarm 2% sodium bicarbonate solution or 1% saline until the eluate does not contain the smell of pesticides, and then magnesium sulfate should be given for catharsis.
If the eyes are exposed to poison, they can be rinsed with 2% sodium bicarbonate solution or 0.9% sodium chloride solution for several minutes.
Antidote
atropine
Atropine can quickly antagonize the M-like effects of ACh in the body, which manifests as relaxing various smooth muscles, inhibiting the secretion of various glands, increasing heart rate, and dilating pupils, etc.
Until the symptoms of M bile receptor excitement disappear or symptoms of mild atropine poisoning appear, that is, atropinization
AChE resurrection drug
Application principles of detoxification drugs
Combination medication
Take medication as early as possible
Take adequate medication
Repeat medication
Symptomatic treatment
Maintain the patient's airway unobstructed, including endobronchial suction, artificial respiration, and oxygen supply.
Use diazepam (5~10mg, intravenous injection) to control persistent convulsions.
Anti-shock.
cholinesterase reactivating drugs
pralidoxime chloride
Restore AChE activity
.Direct detoxification effect
It directly combines with free organic phosphates in the body to become non-toxic phosphorylated pralidoxime chloride and is excreted in the urine.
【Clinical application】
Treatment of organophosphorus poisoning. It can significantly reduce N-like symptoms, has the most obvious inhibitory effect on skeletal muscle spasm, and can quickly inhibit fasciculations; it also has a certain improvement effect on the symptoms of poisoning in the central nervous system.
; but has less effect on M-like symptoms. Therefore, it should be combined with atropine to control symptoms.
pralidoxime iodide