Cholinergic Agonists Flashcards
1
Q
Choline Esters
A
ACh
Methacholine
Bethanechol
Carbachol
Direct-acting; Mimic ACh
2
Q
AcetylCholine
A
- Short duration/Rapid affect
- Does snot penetrate BBB
- Dec HR/CO
- Rarely used clinically; Opthalmic surgery for Myosis
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
4
Q
Bethanechol
A
- NOT hydrolyzed by AChE
- Strong M2/3 agonist
- NO Nicotinic action
- Stimulate neurogenic bladder, GI smooth. Muscle
5
Q
Carbachol
A
- Also NOT hydrolyzed
- BOTH M and N receptors
- Cardiovascular + GI systems
- Release of EP
- Topically treat Open-angle Glaucoma
6
Q
Alkaloids
A
- Naturally occurring Cholinomimetics
- Muscarinic
- Pilocarpine
- Nicotine
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
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
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
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
11
Q
Varenicline
A
- Direct partial agonist of Nicotinic receptor
- Smoking cessation
- Significant decreased craving/withdrawal symptoms
12
Q
Major contraindications for ALL Direct cholinergic
A
- COPD
- Peptic Ulcer
- Arrhythmias + CVD
- Angle-closure glaucoma
- Hyperthyroidism
- Urinary Obstruction
- Orthostatic hypotension
- Sever Miosis
13
Q
Reversible/Carbamates
A
- inhibit AChE preventing degradation of ACh
- Physostigmine
- Neostigmine
- Pyridostigmine
- Tacrine, Donbepezil, Rivastigmine, Galantamine
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
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
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
