Cholinergic Drugs

Front 1

Acetylcholine
-Class
-Therapeutic use
-Adverse effects

Back 1

-Muscarinic agonist, choline ester, (really sensitive to cholinesterases)
-topical administration on conjunctiva (increases aqueous humor outflow)
-visual difficulty with far sight, reddening, stinging, cataracts and retinal detachment with long term use, postoperative iritis

Front 2

Carbachol
-Class
-Therapeutic use
-Adverse effects

Back 2

-Muscarinic agonist, choline ester, (negligible sensitivity to cholinesterases)
-topical administration on conjunctiva= glaucoma (increases aqueous humor outflow)
-visual difficulty with far sight, reddening, stinging, cataracts and retinal detachment with long term use, postoperative iritis

Front 3

Bethenechol
-Class
-Therapeutic use
-Adverse effects

Back 3

-Muscarinic agonist, choline ester, (negligible sensitivity to cholinesterases)- (no effects on nicotinic receptors)
-PO or SC administration (avoid IV or IM), xerostomia, postop nonobstructive ileus, urinary retention, neurogenic bladder
-nausea/vomiting (due to inc GI activity), abdominal pain, diarrhea, bronchospasm, sweating, hypotension, urinary urgency, skin flushing {CONTRA: peptic ulcer dz, IBD, hyperthyroidism, coronary artery dz, hypotension}

Front 4

Pilocarpine
-Class
-Therapeutic use
-Adverse effects

Back 4

-Muscarinic agonist, natural alkaloid (DO NOT activate nicotinic receptors)
-Can cross BBB, prominent salivation and sweating, locally in open angle glaucoma, sometimes orally for xerostomia from radiation or sjorgens syndrome
-hyperparasympatheic symptoms can result, convulsions, coma (no affect on skeletal muscle tone bc no effect on nicotinic receptors)

Front 5

Muscarine
-Class
-Therapeutic use
-Adverse effects

Back 5

-Muscarinic agonist, natural alkaloid (DO NOT activate nicotinic receptors)
- (no uses) Can cross BBB, prominent salivation and sweating
-from mushrooms (poisoning= mycetism), symptoms develop within 30-60min: salivation, visual disturbance, sweating, colic, bradycardia, hypotension, tremors, convulsions, coma

Front 6

Edrophonium (alcohol)
-Class
-Therapeutic use
-Adverse effects

Back 6

-Cholinesterase reversible inhibitor (short lived 2-10min), low oral bioavailability, only distributes to peripheral tissue
-through IV to test if pt has cholinergic crisis (decrease in muscle strength) or myasthenia crisis (increase in muscle strength)

Front 7

Physostigmine (carbamate)
-Class
-Therapeutic use
-Adverse effects

Back 7

-Cholinesterase reversible inhibitor (prolonged 1-6hrs); tertiary amine (good oral bioavailability), can enter CNS, hydrolyzed by plasma esterase
-open angle glaucoma

Front 8

Neostigmine (carbamate)
-Class
-Therapeutic use
-Adverse effects

Back 8

-Cholinesterase reversible inhibitor (prolonged 1-6hrs)
[can directly activate nicotinic receptors at the NMJ], low oral bioavailability, only distributes to peripheral tissue, hydrolyzed by plasma esterase
-myasthenia gravis pts,post-op nonobstructive ileus, urinary retention, neurogenic bladder

Front 9

Donepezil
-Class
-Therapeutic use
-Adverse effects

Back 9

-Cholinesterase reversible inhibitor, selective acetylcholinesterase inhibitor in the brain
-can improve performance in Alzheimer's dz (early stages)

Front 10

Parathione (and other organophosphates)
-Class
-Therapeutic use
-Adverse effects

Back 10

-Cholinesterase irreversible inhibitor, very good oral bioavailability, gets hydrolyzed by paraoxonases (enzymes in plasma and liver)

Front 11

Pralidoxime
-Class
-Therapeutic use
-Adverse effects

Back 11

-Cholinesterase reactivator, doesn't cross BBB
-poisoning by organophosphate insecticides (regenerates acetylcholinesterase enzyme) - action most pronounced at NMJ sites (not really autonomic or CNS sites)
-{CONTRA: GI disorders, IBD, cholinergic crisis in myasthenic pt, asthma, hypotension, coronary artery dz, hyperthyroidism, parkinsons, seizure disorders