Pharm 6

Front 1

ACh synthesis

Back 1

- ChAT is the enzyme and its superfast
- get actyl from mito and choline from HAChTS (transport system)

Front 2

ACh release

Back 2

- AP -> Na entry -> depol,
- opens voltage-dependent Ca channels -> fusion of vesicles w/ PM and release

Front 3

ACh metaboism

Back 3

- AChE at pre and post synaptic elements
- BtCHE - plasma cholinestrase (nonspecific)

Front 4

Muscarinic receptors

Back 4

- on all autonomic effector cells, certain autonomic ganglion cells, and in CNS
- slow relative to nicotinic
- on Cholinergic pre elements for feedback
- G-protein-linked and

Front 5

Nicotinic recetpors

Back 5

- ones of autonomic ganglion distinct from ones at NMJ
- ligand-gated ion channels - binding of ACh -> rapid net influx of Na+ and Ca2+ into the cell -> depol

Front 6

M1, M3, and M5

Back 6

stimulate PIP2

Front 7

M2, M4

Back 7

inhibit cAMP

Front 8

N1

Back 8

for skeletal muscle

Front 9

N2

Back 9

neural

Front 10

parasympathomimetic drugs

Back 10

act as direct agonists at cholinergic receptors

Front 11

Methacholine

Back 11

- direct parasympathomimetic
- B-methyl sub makes it a muscarinic agonist
- longer duration than Ach b/c is hydrolysis at 1/3 the rate as ACh
- used to test for bronchial hyperactivity and asthmaha
- SE after s.c. injection are hypotension, NandV, asthma attacks, heart block, SLUDS

Front 12

Carbachol

Back 12

- direct parasympathomimetic
- a carbamate sub that protects is, so long duration
- not selective
- gets muscarinic of ciliary to cause miosis and open canals
- so topically for glaucoma

Front 13

Bethanechol

Back 13

- direct parasympathomimetic
- like methacholine and carbachol w/ a 13-methyl sub and a carbamate sub
- long (2-3 hour) duration
- selective for muscarinic
– orally or s.c., it exerts only mild CV - gets mainly the GI and bladder
– used to increase tone and contractions of pts intestine and bladder

Front 14

Pilocarpine

Back 14

- direct parasympathomimetic
- plant alkaloid
- selective for muscarinic
- not a choline ester, sp ChEs dont work
- 2-3 hour duration
- topically like carbachol for glaucoma
- systematically, you get usual side effects

Front 15

Atropine

Back 15

will block or reverse the adverse effects of parasympathomimetics

Front 16

edrophonium

Back 16

- Reversible ChE Inhibitor
- short duration
– used as MG diagnostic test as IV will reverse muscle weakness

Front 17

neostigmine

Back 17

- Reversible ChE Inhibitor
- quaternary amine
– wont cross BBB, so good for peripheral disorders
– stimulates GI contractions and secretions, contractions of bladder, and improves neurotransmission at somatic nerves and SkM
– used for intestinal and bladder atony and for MG
- pyridostigmine and ambenonium replacing b/c they last longer

Front 18

physostigmine

Back 18

- Reversible ChE Inhibitor
- tertiary amine from plant
- can penetrate into CNS
- topically for glaucoma

Front 19

Reversible cholinesterase inhibitors

Back 19

- carbamyl esters that hydrolyze the ester linkage
– E site more resistant than A site, which slows the hydrolysis of Ach
– the free site can regenerate so its reversible

Front 20

Irreversible cholinesterase inhibitors

Back 20

- aka organophosphate ChEs
- inhibit AChE and plasma ChE
- when it interacts, its hydrolzed, but the Pd E site is not
- the free active site regenerates slowly or not at all
- recovery depends on the synthesis of new enzyme

Front 21

DFP

Back 21

- irreversalbe ChE inhibitor
– topically for glaucoma
- long duration, should
- overuse can lead to SLUD

Front 22

Pralidoxime

Back 22

- use to treat an overdose of irreversible ChE inhibitors
- if used prior to aging (alkyl group more tightly bound to E site), frees enzyme to an active unit
- most striking effect occurs at the NMJ
- does not penetrate BBB

Front 23

methacholine trade name

Back 23

(Provocholine)

Front 24

carbachol trade name

Back 24

(Carbastat; Isopto Carbachol)

Front 25

bethanechol trade name

Back 25

(Urecholine; Duvoid)

Front 26

pilocarpine trade name

Back 26

(Pilocar; Isopto Carpine)

Front 27

edrophonium trade name

Back 27

(Enlon; Reversol; Tensilon)

Front 28

neostigmine trade name

Back 28

(Prostigmin)

Front 29

physostigmine trade name

Back 29

(Antilirium; Isopto Eserine; Synapton)

Front 30

DFP trade name

Back 30

(Floropryl)

Front 31

pralidoxime trade name

Back 31

(Protopam)