- inhibits the release of acetylcholine - cleaves SNARE proteins including synaptobrevin

- desensitization of adrenergic receptors

- sensitization of adrenergic receptors

- autoimmune disease - Abs attacks thyroid

Muscarinic Agonist Flashcards by Ayden Zarkhah

Diabetic autonomic neuropathy

metabolic insult to nerve fibers
neurovascular insufficiency
autoimmune damage
neurohormonal growth factor deficiency

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Cardiovascular autonomic neuropathy

clinically most important form

- increased risk of silent myocardial ischemia/mortality

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Autonomic dysfunction with alcoholism + chronic liver disease

autonomic, mainly vagal, nerve dysfunction is common with these two conditions
advanced chronic liver disease characterized by peripheral arterial vasodilation + increased plasma [catecholamine].

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Organism responsible for botulism poisoning

Clostridium botulinum, present in soil and water

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Source of botulism poisoning

foodborne, wound borne

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Action of botulism

inhibits the release of acetylcholine

- cleaves SNARE proteins including synaptobrevin

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Symptoms of botulism

weakness, trouble seeing, fatigue, trouble speaking

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Graves disease description

autoimmune disease
thyroid stimulating Ig
stimulate secretion of Thyroxine(T4) and Triiodothyronine(T3)

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Symptoms of Grave’s disease

mimic hyperadrenergic state
feeling hot
excessive sweating
irregular heartbeat/tachycardia
diarrhea/hyperdefecation
dry eyes
weight loss
hypertension

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Treatment of Grave’s disease

treatment with Beta-blocker

- contraindication for use of muscarinic agonists

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Relationship between thyroid and adrenal

adrenal gland activation(stress) => glucocorticoids inhibit enzyme that converts T4 to T3.
interaction between PANS, SANS, and Thyroid function

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Reduced body weight and its action on thyroid and adrenal

T3 decrease
SANS decrease
PANS increase

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Elevated body weight and its action on thyroid and adrenal

T3 increase

- SANS increase

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Hypothyroidism

desensitization of adrenergic receptors

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Hyperthyroidism

sensitization of adrenergic receptors

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Undiagnosed hypothyroidism

iodine deficiency

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Hashimoto’s disease

autoimmune disease

- Abs attacks thyroid

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Symptoms of hypothyroidism

cold
dry skin
constipation
slowed heart rate
weight increase
hair loss

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Cholinergic stimulation on Urinary tract

increase ureteral peristalsis
decrease bladder capacity
increase voiding pressure

Cholinergic stimulation on Blood pressure

increase blood pressure

Cholinergic stimulation on GI

increase GI tone
contractility
increased secretory activity

Cholinergic stimulation on Respiratory

bronchoconstriction
mucus secretion
increase secretion from all glands including salivation, sweat, lacrimal, digestive, tracheobronchial

Cholinergic stimulation on Eye

miosis

- drainage of anterior chamber

Cholinergic stimulation basic two drugs

acetylcholinesterase inhibitors

- muscarinic agonists

Muscarine and muscarinic receptors

- aminita muscaria : kills flies - contains alkaloid muscarine - first parasympathomimetic - can cross BBB and cause convulsions

Direct acting cholinergic receptor agonists are?

Esters

Molecular description of cholinergic receptor agonist

- polarity(quartanary ammonium) | - limited CNS distribution, and GI absorption

4 drugs of the direct acting cholinergic receptor agonist

``` acetylcholine carbachol methacoline(provocholine) bethanechol(urecholine) muscarine pilocarpine ```

Cholinergic agonist OD risk by acting on nicotinic receptors

acetylcholine carbachol methacholine

Short acting cholinergic agonist

acetylcholine | methacholine

Methacholine and Asthma/COPD diagnosis

- use to diagnose bronchial hyperreactivity - bronchial challenge test - respond to lower drug dose

Open/narrow angle glaucoma

- clogged trabecular meshwork | - slow progression

Closed-angle glaucoma

- iris and ciliary body block the canal of schemm and trabecular network - fast progression

Treatment for open/narrow angle glaucoma

Tinolol (Beta-blocker) | -stretch open meshwork

Action on closed angle glaucoma

M3 contraction to pull ciliary body away

Muscarinic agonists for treatment of glaucoma

Carbachol | Pilocarpine

Carbachol description

- primarily used for glaucoma - 2 to 5min onset, 4-8hr duration - longer acting than pilocarpine

Pilocarpine description

- relieves block of canal of schlemm | - partial agonist (less headache)

Adverse effects of pilocarpine

- sweating, salivation, diarrhea, bronchial mucus secretion - bronchospasm, bradycardia, vasodilation - miosis; blurred vision, impaired night vision - reduced BBB function; epilepsy

Bethanechol description

- muscarinic selective | - orally or subQ

Contraindications of Bethanechol

- urinary retention; avoid use in bladder outlet obstruction(bladder stone, prostate hyper. tumor) - post operative ileus(GI atony)

Cevimeline and pilocarpine description

- xerostomia(dryness of mouth) - following head/neck irradiation - sjogren's disease/syndrome

Nicotine description

- full agonist - protonated at acidic pH - absorbed in mouth and lung

Side effects of nicotine

- irritation at site - fast/irregular heart beat - difficulty breathing

Contraindication of nicotine

cardiovascular disease

Varenicline(chantix) description

- alpha4beta2 nicotinic receptor partial agonist - activates nicotine receptor much less than nicotine - blocks nicotine from binding - well tolerated

Side effects of varenicline

- GI related - nausea, constipation, gas, vomiting - altered dreams