Cholinergics and Anticholinergics Flashcards

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

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

A

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

24
Q

Effects of high doses of cholinergic drugs

A

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

25
Q

Adverse reactions of cholinergic drugs

A

Overstimulated effects of cholinergic system
Salivation, lacrimation, urination, defecation, gastrointestinal cramps and emesis (SLUDGE)

26
Q

Contraindications of cholinergic drugs

A

Bronchial asthma
Hyperthyroidism
GI or urinary tract obstruction
Myastenia gravis treated with neostigmine
Peptic ulcer disease
Severe cardiac disease

27
Q

Acetylcholine uses

A

Rarely given systemically
Topical 1% solution for the induction of miosis during ophthalmologic surgery

28
Q

Methacholine uses

A

Diagnosis of bronchial airway hyperactivity (long acting, so not clinically used as much)

29
Q

Carbacol (carbamylcholine) uses

A

To produce miosis in ophthalmology (after cataract surgery)
Treatment of colic and impaction of the intestinal tract
Rumen atony and impaction

30
Q

Bethanechol (carbamylmethylcholine chloride; urecholine) uses

A

Increases tone and motility fo dilated bladder and Gi tract
Treat urinary bladder atony in cats with urolithiasis
Xerostomia
Sjogren syndrome

31
Q

Pilocarpine uses

A

Treating glaucoma
Neurogenic keratoconjunctivitis sicca in dogs (lowering intraocular pressure)

32
Q

How does pilocarpine affect the body?

A

Increases secretion of digestive system, peristaltic motility of GI tract, and constriction of pupil

33
Q

Naturally occurring cholinomimetic alkaloids

A

Pilocaprine, muscarine and arecoline
Plant alkaloids that exert cholinomimetic activities with minimal activity at nicotinic sites
DON’T INHIBIT CHOLINESTERASE ENZYME

34
Q

Where are the natural cholinomimetic alkaloids found?

A

Pilocarpine (leaves)
Arecoline (seed)
Muscarine (mushroom)

35
Q

Effects of indirect acting cholinomimetics

A

Inactivate or inhibit the AChE
Prolonging lifetime of ACh
Anticholinesterase agents or cholinesterase enzyme inhibitors

36
Q

What causes mycetism or cholinergic toxicity

A

Higher consumption of wild mushrooms (culinary)
Overdose of cholinergic drugs
Ex: A. muscaria and A. phalloid

37
Q

Symptoms of cholinergic toxicity

A

Excessive sludge- excessive sweating, bronchospasm, headache, visual disturbances, abdominal colic, hypotension, shock and bradycardia

38
Q

Treatment of cholinergic toxicity

A

Atropine: 1-2 mg IM injection to reverse symptoms

39
Q

Effects of anticholingeric drugs

A

Bladder relaxation
Bronchodilation
Decrease exocrine gland secretion
Decrease gut motility
Mydriasis

40
Q

Anticholinergics/ Muscarinic antagonists

A

Atropine (main) and Scopolamine- competitive inhibitors (belladona alkaloids)

41
Q

Benztropine (anti)

A

CNS
Treats parkinsons

42
Q

Ipratopium (anti)

A

Bronchi (bronchial smooth muscles)
Bronchodialte in asthma and COPD

43
Q

Oxybutinin (anti)

A

GI
Treats transient cystitis and postoperative bladder

44
Q

Scopolamine (anti)

A

CNS
Prevents motion sickness
Small animals: antispasmodic and antisecretory (diarrhea)
Horse: relax the rectum for rectal exam

45
Q

Clinical uses of atropine

A

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
Q

Propantheline:

A

Anti-secretory and antispasmodic effects treating diarrhea
Reduce colonic peristalsis in horses

47
Q

Isopropamide

A

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
Q

Glycopyrronium

A

Adjunct to general anesthesia
Decreases acid secretion in stomach

49
Q

How do anticholineric drugs affect the CNS

A

Depending on the dose, drugs can cause stimulation or depression

50
Q

How do anticholineric drugs affect exocrine glands

A

Reduce the flow of volume of secretion in the respiratory, GI and genitourinary tracts

51
Q

How do anticholineric drugs affect smooth muscles

A

Relax smooth muscles in respiratory and GI tracts
Delay gastric emptying and decrease sophageal gastric emptying
Causes bronchial dialtion

52
Q

How do anticholineric drugs affect the eye

A

Cause mydriasis and cycloplegia

53
Q

Reversible ndirect acting cholinergic uses

A

Physostigme- atropine overdose
Neostigme/ pyridostogme- MG
Edrophonium- diagnose MG
Ecothiophate- glaucoma

54
Q

Irreversible indirect cholinergic uses

A

DFP- district pupil in glaucoma
Soman, Tabun, Sarin- nerve gases
Dichlorvos- oral anthelmintic and pesticides