Cholinergic Agonists Flashcards

1
Q

Choline Esters

A

ACh
Methacholine
Bethanechol
Carbachol

Direct-acting; Mimic ACh

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2
Q

AcetylCholine

A
  • Short duration/Rapid affect
  • Does snot penetrate BBB
  • Dec HR/CO
  • Rarely used clinically; Opthalmic surgery for Myosis
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3
Q

Methacholine

A
  • NOT hydralized by AChE
  • Inhalation
  • Bronchial challenge test -> Bronchial airway hypersensitivity
  • eye drops as a miotic
  • Contra: Stroke, MI, Severe asthma, COPD
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4
Q

Bethanechol

A
  • NOT hydrolyzed by AChE
  • Strong M2/3 agonist
  • NO Nicotinic action
  • Stimulate neurogenic bladder, GI smooth. Muscle
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5
Q

Carbachol

A
  • Also NOT hydrolyzed
  • BOTH M and N receptors
  • Cardiovascular + GI systems
  • Release of EP
  • Topically treat Open-angle Glaucoma
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6
Q

Alkaloids

A
  • Naturally occurring Cholinomimetics
  • Muscarinic
  • Pilocarpine
  • Nicotine
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7
Q

Muscarine

A
  • NOT hydrolyzed
  • Does NOT cross BBB
  • Diagnosis: history of mushroom ingestion; Cholinergic symptoms esp sweating
  • Antidote -> Atropine (competitive muscarine antagonist)
  • Administer O2 prior
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8
Q

Pilocarpine

A
  • Stable to hydrolysis
  • Primarily Muscarinic
  • Penetrates BBB; Rapid contraction ofciliary muscle
  • Strong stimulations of secretions
  • Clinical: Open + Closed angle Glaucoma; Xerostomia; Sjogren’s; Atropine Mydriasis; Iris-lens adhesion
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9
Q

Nicotine

A
  • N receptors at autonomic ganglia, NMJ, and Adrenal medulla
  • Low Dose-> Stimulant; High Dose - Reward pathway
  • INC HR/BP, GI Motility, Vasocontriction
  • Overdose: Profuse PSN, respiratory depression, tremors, and convulsions
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10
Q

Cevimeline

A
  • Synthetic; oral
  • M1/3 agonist
  • Exocrine glands -> Xerostomia

*Siponmod: selective S1P receptor modulator for oral use for MS; Risk f SEVER Bradycardia and AV Block

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11
Q

Varenicline

A
  • Direct partial agonist of Nicotinic receptor
  • Smoking cessation
  • Significant decreased craving/withdrawal symptoms
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12
Q

Major contraindications for ALL Direct cholinergic

A
  • COPD
  • Peptic Ulcer
  • Arrhythmias + CVD
  • Angle-closure glaucoma
  • Hyperthyroidism
  • Urinary Obstruction
  • Orthostatic hypotension
  • Sever Miosis
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13
Q

Reversible/Carbamates

A
  • inhibit AChE preventing degradation of ACh
  • Physostigmine
  • Neostigmine
  • Pyridostigmine
  • Tacrine, Donbepezil, Rivastigmine, Galantamine
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14
Q

Physostigmine

A
  • Tertiary amine
  • Works on both; Marked Muscarinic
  • Enter CNS; prominent Autonomic effectors
  • Clinical: USed for Atony, Severe atropine poisoning (especially CNS), acute glaucoma
  • CNS adverse effects
  • Contra: Pulmonary disease, Diabetes
  • Overdoes -> Cholinergic crisis
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15
Q

Neostigmine

A
  • Poorly absorbed; NO CNS
  • Prominent SKM
  • Clinical: Myasthenia Gravis; Reversal of nondepolarizing NM blockage; Ogilvie’s Syndrome
  • Snake bite

Adverse: NOT for atropine toxicity

Administration: Along w/ anti muscarinic glycopyrrolate or atropine

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16
Q

Pyridostigmine

A
  • Neostigmine analog
  • CHRONIC Management of MG; first line therapy
  • Pretreatment for Soman nerve gas in military
17
Q

Organophosphates/ Irreversibles

A
  • Echothiophate
  • Parathion
  • Malathion
  • Nerve Gas
18
Q

Echothiophate

A
  • Generalized cholinergic stimulation in both N/M
  • Chronic Aspen angle glaucoma
  • Adverse: Seizures, Psychosis, GII upset, Salivation, blurry vision, bradycardia
  • NM Blockage
19
Q

Parathion

A
  • Insecticide
  • Rapidly absorbed
  • NOT rapidly detoxified
  • PNS effects + Paralysis + Coma
20
Q

Malathion

A
  • organophosphate; rapidly absorbed + long duration similar to Parathion
21
Q

Nerve Agents

A
  • Organophosphates
  • High Potency, severe symptoms
  • Treatment: Oxime 2PAM - Atropine - Benzodiazepine
22
Q

2-PAM

A
  • Reactivates AChE

- Can’t penetrate CNS; In conjunctions with atropine for Nerve gas Toxicity

23
Q

Acute antiAChE Toxicity Clinical Findings

A

SLUDGE

Salivation
Lacrimation
Urinary freq
Diarrhea
GI Upset
Emesis
24
Q

Contra for AntiAChE Agents

A
  • Succinyl Choline
  • CV Disease
  • Glaucoma
  • Renal impairment
  • Respiratoruy Disease