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1. Pharmacology > Cholinergics and Anticholinergics > Flashcards

Cholinergics and Anticholinergics Flashcards

(54 cards)

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1
Q

What aids in the release and Acetycholine?

A

ChAT- choline acetyltranferase
VAMP- vescicle- associated membrane proteins
SNAP- synaptasome-associated proteins
AchE- Acetylcholinesterase

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2
Q

Cholinergic agents

A

AKA cholinergic agonists, parasympathomimetics, cholinomimetics
Mimics Acetylecholine (ACh)

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3
Q

Cholinoceptors

A

Mediates the parasympathetic activity
Muscarinic and nicotonic receptors

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4
Q

M1 receptor

A

Nerves, CNS, ENS
Pirenzepine and telezepine

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5
Q

Pirenzepine

A

Inhibits gastric acid secretion and reduces muscle spasm
Treatment of peptic ulcers
Chronic obstructive pulmonary disease

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6
Q

Telezepine

A

More potent inhibitor of gastric acid than pirenzepine
Treating peptic ulcers in humans

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7
Q

M2 receptor

A

Heart, nerves, smooth muscle (cardiac M2)
Tripitramine and methoctramine

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8
Q

Tripitramine

A

Selective antagonist for M2 receptors
Blocks cholinergic bradycardia

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9
Q

Methoctramine

A

Cardiac M2 muscarinic receptor antagonist

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10
Q

M3 receptor

A

Other visceral organs: bladder constriction, bronchoconstriction, increases exocrine gland secretion, increases gut motility, miosis via pupillary sphincter
Darifenacin and solifenacin

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11
Q

Darifenacin

A

Selective antagonist of M3 receptor
Treatment of overactive bladder

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12
Q

Solifenacin

A

Selective M3 receptor antagonist
Urinary antispasmodic, treatment of overactive bladder

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13
Q

Direct acting cholingeric stimulants

A

Acts directly on cholinergic receptors
Cholingeric (muscaneric) agonists
Includes cholinesters (acetylcholine, methacholine, bethanechol, carbachol) and alkaloids (muscarine and pilocarpine)

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14
Q

Indirect acting cholinergic stimulants

A

Inhibits the breakdown of AcH by inhibiting cholinesterase
Includes carbamates (reversible) and phosphates (irreversible)

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15
Q

Why is ACh administration difficult in clinics?

A

Non selective (acts everywhere)
Rapidly deactivated (AChE and short half-life)

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16
Q

Cholinesters and natural alkaloids

A

Absorption: polarity dependent, IV IM and SQ for local effects
Metabolism: AChE dependent

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17
Q

Therapeutic uses for muscarinic agonists

A

Treatment of urinary bladder disorders, xerostomia (dry mouth), diagnosis of bronchial hyperreactivity, opthalmology , glaucoma treatment

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18
Q

Pharmacological effects that AcH has on the cardiovascular system

A

Inhibitory effects:
Vasodilation
Decrease in HR, conduction velocity in AV node and force of cardiac contraction

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19
Q

Pharmacological effects that AcH/ cholinergic drugs has on the GI tract

A

Excite the smooth muscles of the GI tract
Increased activity, motility, secretion and urinary frequency

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20
Q

Pharmacological effects that AcH/ cholinergic drugs has on the eye

A

Miosis (constriction) and decreased intraocular pressure

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21
Q

What overall effects does does AcH/ cholinergic drugs have on the body

A

Increased secretion from every body system
Increased salivation and sweating

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22
Q

Pharmacological effects that AcH/ cholinergic drugs has on the respiratory tract

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A

Increases parasympathetic activity (bronchocontriction)
Increased tracheobronchial secretion and stimulation of the chemoreceptors of the carotid and aortic bodies

23
Q

Effects of recommended doses of cholinergic drugs

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A

Affects muscarinic receptors
Desired effects are primarily due to muscarinic receptor stimulation

24
Q

Effects of high doses of cholinergic drugs

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A

Stimulates the nicotonic receptors
Undesirable effects due to stimulation of nicotinic receptors (toxic)

25
Adverse reactions of cholinergic drugs
Overstimulated effects of cholinergic system Salivation, lacrimation, urination, defecation, gastrointestinal cramps and emesis (SLUDGE)
26
Contraindications of cholinergic drugs
Bronchial asthma Hyperthyroidism GI or urinary tract obstruction Myastenia gravis treated with neostigmine Peptic ulcer disease Severe cardiac disease
27
Acetylcholine uses
Rarely given systemically Topical 1% solution for the induction of miosis during ophthalmologic surgery
28
Methacholine uses
Diagnosis of bronchial airway hyperactivity (long acting, so not clinically used as much)
29
Carbacol (carbamylcholine) uses
To produce miosis in ophthalmology (after cataract surgery) Treatment of colic and impaction of the intestinal tract Rumen atony and impaction
30
Bethanechol (carbamylmethylcholine chloride; urecholine) uses
Increases tone and motility fo dilated bladder and Gi tract Treat urinary bladder atony in cats with urolithiasis Xerostomia Sjogren syndrome
31
Pilocarpine uses
Treating glaucoma Neurogenic keratoconjunctivitis sicca in dogs (lowering intraocular pressure)
32
How does pilocarpine affect the body?
Increases secretion of digestive system, peristaltic motility of GI tract, and constriction of pupil
33
Naturally occurring cholinomimetic alkaloids
Pilocaprine, muscarine and arecoline Plant alkaloids that exert cholinomimetic activities with minimal activity at nicotinic sites DON'T INHIBIT CHOLINESTERASE ENZYME
34
Where are the natural cholinomimetic alkaloids found?
Pilocarpine (leaves) Arecoline (seed) Muscarine (mushroom)
35
Effects of indirect acting cholinomimetics
Inactivate or inhibit the AChE Prolonging lifetime of ACh Anticholinesterase agents or cholinesterase enzyme inhibitors
36
What causes mycetism or cholinergic toxicity
Higher consumption of wild mushrooms (culinary) Overdose of cholinergic drugs Ex: A. muscaria and A. phalloid
37
Symptoms of cholinergic toxicity
Excessive sludge- excessive sweating, bronchospasm, headache, visual disturbances, abdominal colic, hypotension, shock and bradycardia
38
Treatment of cholinergic toxicity
Atropine: 1-2 mg IM injection to reverse symptoms
39
Effects of anticholingeric drugs
Bladder relaxation Bronchodilation Decrease exocrine gland secretion Decrease gut motility Mydriasis
40
Anticholinergics/ Muscarinic antagonists
Atropine (main) and Scopolamine- competitive inhibitors (belladona alkaloids)
41
Benztropine (anti)
CNS Treats parkinsons
42
Ipratopium (anti)
Bronchi (bronchial smooth muscles) Bronchodialte in asthma and COPD
43
Oxybutinin (anti)
GI Treats transient cystitis and postoperative bladder
44
Scopolamine (anti)
CNS Prevents motion sickness Small animals: antispasmodic and antisecretory (diarrhea) Horse: relax the rectum for rectal exam
45
Clinical uses of atropine
Pre-aesthetic to prevent/ reduce secretions Antispasmodic of intestinal, urinary or biliary duct Bronchodilator Cardiac stimulant Antidote to anticholinesterase agents Mydriatic Control of pain Relief of heaves in horses
46
Propantheline:
Anti-secretory and antispasmodic effects treating diarrhea Reduce colonic peristalsis in horses
47
Isopropamide
Provides long duration, treatment of peptic ulcers and other GI disorders involving hyperacidity Used for antiemetic, antidiarrheal, anticholinergic and antiarrhythmic effects Used with prochlorperazine
48
Glycopyrronium
Adjunct to general anesthesia Decreases acid secretion in stomach
49
How do anticholineric drugs affect the CNS
Depending on the dose, drugs can cause stimulation or depression
50
How do anticholineric drugs affect exocrine glands
Reduce the flow of volume of secretion in the respiratory, GI and genitourinary tracts
51
How do anticholineric drugs affect smooth muscles
Relax smooth muscles in respiratory and GI tracts Delay gastric emptying and decrease sophageal gastric emptying Causes bronchial dialtion
52
How do anticholineric drugs affect the eye
Cause mydriasis and cycloplegia
53
Reversible ndirect acting cholinergic uses
Physostigme- atropine overdose Neostigme/ pyridostogme- MG Edrophonium- diagnose MG Ecothiophate- glaucoma
54
Irreversible indirect cholinergic uses
DFP- district pupil in glaucoma Soman, Tabun, Sarin- nerve gases Dichlorvos- oral anthelmintic and pesticides

1. Pharmacology (29 decks)

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