Pharm Drugs- Cholinergic Agonists and Antagonists

Question 1

Methacholine

Answer 1

• direct-acting cholinomimetic
• inhaled for dx of bronchial airway hyperreactivity in pts w/out asthma
• rarely used

Question 2

Bethanechol

Answer 2

• direct-acting cholinomimetic
• tx for urinary retention and heartburn
• selective mAChR agonist
• can cause urinary tract inf d/t retention

Question 3

Carbachol

Answer 3

• direct-acting cholinomimetic
• nonspecific
• tx glaucoma or produces miosis during surgery or exam

Question 4

Cevimeline

Answer 4

• direct-acting cholinomimetic
• PO for xerostomia in Sjogren’s syndrome pts
• urine elim

Question 5

Pilocarpine

Answer 5

• direct-acting cholinomimetic
• PO for xerostomia in Sjogren’s or head/neck Ca pts,
• topical for miosis during opth procedures and glaucoma

Question 6

Varenicline

Answer 6

• direct-acting cholinomimetic
• smoking cessation
• partial agonist to (alpha)4(beta)2 nAChRs in brain
• MC AE = nausea, SAE = suicidal ideation

Question 7

cholinesterase inhibitors

Answer 7

• ambenonium
• donepezil
• echothiophate
• galantamine
• neostigmine
• physostigmine
• pridostigmine
• rivastigmine
• tacrine

Question 8

pralidoxime

Answer 8

• cholinesterase regenerator
• must be given before aging of organophosphate
• current antidotal therapy for organophosphate exposure

Question 9

scopolamine

Answer 9

• antimuscarinic drug
• acts at mAChRs to tx motion sickness IV, PO, or transdermal
• used in opthamology

Question 10

atropine

Answer 10

• antimuscarinic drug
• tertiary amine that can act at CNS level (slower and longer on brain)
• acts selectively at mAChRs and is reversible
• tx for cholinergic poisoning, organophosphate exposure
• 2 hr T1/2
• most sensitive tissues = salivary, bronchial, sweat
• causes mydraisis
• “atropine fever” in children
• blocks vagal reflexes by surgical manipulation of organs
• first drug of choice in syptomatic brady in ACLS
• paired with opioid to create antidiarrheal drug
• tx urinary urgency in inflammatory bladder disorders
• should be avoided in pts with acid-peptic disease

Question 11

Glycopyrrolate

Answer 11

• antimuscarinic drug
• used to tx GI disorders
• quartenary amine that elicits effets in periphery
• blocks parasympathetics during release of anethesia

Question 12

Ipratroprium

Answer 12

• antimuscarinic drug
• used as first-line therapy to tx resp disorders: asthma & COPD
• quarternary amine w/ effects at periphery
• T1/2 = 2 hr

Question 13

Tiotropium

Answer 13

• used to tx resp disorders: asthma & COPD

- T1/2 = 120h, dosed QID

Question 14

Oxybutynin

Answer 14

• animuscarinic drug
• somewhat selective for M3
• used to tx urinary disorders to reduce frequency
• AEs = xerostomia, dizziness, constipation, blurred vision, dry eyes, UTIs

Question 15

Achetylcholine

Answer 15

• direct-acting cholinomimetic
• approved to IO use during surgery, causes miosis
• rarely given systemically