Autonomic Agents Drug Chart

Direct-acting cholinomimetic agents

acetylcholine, carbachol, pilocarpine, cevimeline, bethanechol, nicotine, varenicline

Direct-acting cholinomimetic MOA

bind to and activate muscarinic or nicotinic receptors

Acetylcholine and carbachol indication

rapid miosis

ACh/carbachol DOA length

short

Common side effects of ACh/carbachol

corneal edema, clouding

Serious side effects of ACh/carbachol

retinal detachment, minimal risk of systemic effects

Pilocarpine/cevimeline indication (opth)

lowers IOP (can lead to miosis induction)

Pilocarpine/cevimeline indication (PO)

dry mouth, sjogren’s syndrome

Pilocarpine DOA

longer DOA than other agents

In which way is cevimeline selective?

M3 selective (fewer undesirable side effects)

CIs with pilocarpine/cevimeline

narrow-angle glaucoma, uncontrolled asthma

Precautions with pilocarpine/cevimeline

PO: cardiovascular, pulmonary

Common side effects of pilocarpine/cevimeline (opth)

decreased accommodation to low light

Common side effects of pilocarpine/cevimeline (PO)

sweating, GI overactivity

Serious side effects of pilocarpine/cevimeline

cholinergic side effects related to the extension of the MOA is seen with PO formulation

Bethanechol indication

urinary retention

How does bethanechol work?

relaxes parasympathetic sphincter

Common side effects of bethanechol

urinary urgency

Direct-acting cholinomimetic systemic cholinergic side effects

bradycardia, hypotension, breathing difficulties, flushing/sweating, epigastric distress, abdominal cramps, diarrhea, urinary urgency

Where do nicotinic receptors act?

autonomic ganglia and skeletal muscle (some CNS) via transmembrane polypeptide ion channel

Where do muscarinic receptors act?

effector tissues (smooth muscle, heart, exocrine glands)

Nicotine brand

nicorette, nicoderm

Nicotine indication

smoking cessation

How does nicotine work?

agonist at Nn/Nm; crosses bbb

Precaution with nicotine

dependence

Common side effect of nicotine

withdrawal

Nicotine polacrilex brand

nicorette

Nicorette formulation

gum/lozenge

Nicotine nasal

nicotrol

Varenicline brand

chantix

Varenicline indication

smoking cessation

Varenicline MOA

partial neuronal alpha-4-beta-2 nicotinic receptor agonist; prevents nicotine stimulation

Which is dose adjustment necessary with varenicline?

renal elimination

Varenicline BBW

serious neuropsychiatric events

Precaution with varenicline

psychiatric history

Common side effects of varenicline

nausea (titrate dose), bizarre dreams, insomnia

What is required with varenicline?

REMS medication guide required; titrate dose upon initiation to decrease GI side effects