Autonomics

Front 1

Mechanism of action/use of bethanechol?

Back 1

choline ester that acts as a muscarinic receptor agonist by directly binding to and activating the receptors
--consequently induces parasympathetic effects (reduces HR, stimulates gland secretion, induces bronchoconstriction, etc.)
-quaternary ammonium functional group renders it relatively resistant to hydrolysis and therefore relatively stable. This group also makes it relatively insoluble in lipids, poorly absorbed, and unable to enter CNS!
-treats postoperative and neurogenic bowel obstruction and urinary retention by activating bowel and bladder smooth muscle

Front 2

Mechanism of action/use of muscarine?

Back 2

-Non-ester cholinomimetic (alkaloid) agent that directly agonizes muscarinic receptors by binding to and activating them

Front 3

Mechanism of action/use of pilocarpine?

Back 3

-Non-ester cholinomimetic (alkaloid) agent that directly agonizes muscarinic receptors by binding to and activating them
-treats glaucoma by activating the papillary sphincter and ciliary muscles of the eye

Front 4

Mechanism of action/use of cevimeline?

Back 4

-Non-ester cholinomimetic (alkaloid) agent that directly agonizes muscarinic receptors by binding to and activating them
-specific for M3 receptors (therefore increases salvation)
-used to treat dry mouth in disorders such as Sjogren's syndrome and post-radiation therapy

Front 5

Mechanism of action/use of nicotine (NRT)?

Back 5

-non-ester cholinomimetic alkaloid that directly agonizes nicotinic receptors by binding to and activating them
-used to help smokers quit by reducing cravings

Front 6

Mechanism of action/use of neostigmine?

Back 6

-Cholinomimetic agent that indirectly activates cholinergic receptors by inhibiting cholinesterase.
-composed of a carbamate ester and a phenol with a quaternary ammonium compound
--carbamate ester group binds to acetylcholinesterase active site
-treats postoperative and neurogenic bowel obstruction and urinary retention by amplifying endogenous acetylcholine
-treats Myasthenia Gravis and reverses neuromuscular blockade by amplifying endogenous acetylcholine and increasing skeletal muscle strength

Front 7

Mechanism of action/use of physostigmine?

Back 7

-Cholinomimetic agent that indirectly activates cholinergic receptors by inhibiting cholinesterase (and thereby increasing endogenous Ach)
-treats glaucoma by amplifying the effects of Ach (causes cillary muscle contraction and reduced intraocular pressure)

Front 8

Mechanism of action/use of donepezil?

Back 8

-Cholinomimetic agent that indirectly activates cholinergic receptors by inhibiting cholinesterase (and thereby increasing endogenous Ach)
--binds to acetylcholinesterase, but not covalently, so the duration of inhibition depends upon metabolism
-hydrophobic and readily crosses BBB (therefore exerts CNS effects)
-treats Alzheimer's by amplifying endogenous Ach in the brain

Front 9

Mechanism of action/use of edrophonium?

Back 9

-Cholinomimetic agent that indirectly activates cholinergic receptors by inhibiting cholinesterase (and thereby increasing endogenous Ach)
--binds to acetylcholinesterase, but not covalently, so the duration of inhibition depends upon metabolism
-treats myasthenia gravis and reverses a neuromuscular blockade by amplifying endogenous acetylcholine and increasing skeletal muscle strength

Front 10

Mechanism of action/use of pralidozime?

Back 10

-reverses inhibition of acetylcholinesterase by organophosphates and cholinomimetic agents
--strong neucleophile that regenerates enzyme that has been phosphorylated
--will only work before the acetylcholine-inhibitor complex has undergone aging, a process that renders the enzyme irreversibly inhibited