Cholinergic Drugs

Front 1

Direct acting cholinergic drugs

Back 1

Bethanechol, Carbachol, Methacholine, Pilocarpine

Front 2

Derivation of Bethanechol

Back 2

Carbamoyl ester of Ach

Front 3

Anatomical function of Bethanechol

Back 3

1. Increase intestinal motility

Front 4

Receptor affinity of Bethanechol

Back 4

Direct muscarinic receptor stimulant (No nicotinic action)

Front 5

Degradation of Bethanechol

Back 5

Not hydrolyzed by AchE (Compound is NH2 / Ach is NH3)

Front 6

Clinical use(s) of Bethanechol

Back 6

1. Treat urinary atony in cats after urolith ***Must have Patent Urethra***

Front 7

Side effects of Bethanechol

Back 7

Salivation, Sweating (diaphoresis), hypotension, colic, nausea, bronchospasm, miosis, urinary urgency, diarrhea

Front 8

Derivation of Carbachol

Back 8

Ester of Carbamic Acid (Similar to Bethanechol without CH3 group)

Front 9

Receptor affinity of Carbachol

Back 9

Stimulates Nicotinic and Muscarinic -> Initially stimulatory effect of cardio & digestive, then nicotinic effect on adrenal medulla

Front 10

Clinical use(s) of Carbachol

Back 10

1. Rumen atony after impaction - use stool softener first

Front 11

Derivation of Methacholine

Back 11

Synthetic choline ester

Front 12

Receptor affinity of Methacholine

Back 12

Mostly muscarinic

Front 13

Clinical use(s) of Methacholine

Back 13

Treat ergot poisoning in goats (vasodilation)

Front 14

Derivation of Pilocarpine

Back 14

Alkaloid of leaves. P. Mircoflexis

Front 15

Receptor affinity of Pilocarpine

Back 15

Stimulate direct muscarinic receptor

Front 16

Degradation of Pilocarpine

Back 16

Stable to AchE

Front 17

Clinical use(s) of Pilocarpine

Back 17

1. Pupil miosis if used topically

Front 18

Indirect reversible cholineric drugs

Back 18

Physostigmine, Neostigmine, Edrophonium

Front 19

Derivation of Physostigmine

Back 19

Alkaloid from seeds of Physostigma Venenosum "Calabar Bean"

Front 20

Receptor affinity of Physostigmine

Back 20

Stimulates nicotinic and muscarinic

Front 21

Degradation of Physostigmine

Back 21

Capture enzyme - reduce hydrolysis of Ach by AchE

Front 22

Clinical use(s) of Physostigmine

Back 22

1. Cross BBB

Front 23

Derivation of Neostigmine

Back 23

Synthetic - related to Physostigmine

Front 24

Clinical use(s) of Neostigmine

Back 24

1. Treat Myastenia Gravis (antibody against Ach receptor)

Front 25

Derivation of Edrophonium

Back 25

Similar to neostigmine (synthetic - related to Physostigmine)

Front 26

Degradation of Edrophonium

Back 26

Short action 10-20 minutes

Front 27

Clinical use(s) of Edrophonium

Back 27

1. Used to diagnose Myasthenia Gravis -> if true MG then immediate increase in muscle strength when administered via IV

Front 28

Parasympathetic Drugs (Anticholinergic)

Back 28

Atropine, Scopolamine, Glycopyrrolate, Homatropine, Ipratropine, Daritenacin

Front 29

Derivation of Atropine

Back 29

Belladonna plant

Front 30

Anatomical function(s) of Atropine

Back 30

1. Bronchodilation

Front 31

Receptor affinity of Atropine

Back 31

Competitively binds to muscarinic receptor to prevent Ach binding

Front 32

Side effect(s) of Atropine

Back 32

Blurred vision, mydriasis, urinary retention, dry mouth, CNS (confusion, delirium) = use Physostigmine as antidote!!!

Front 33

Clinical uses(s) of Atropine

Back 33

1. Cross BBB

Front 34

Derivation of Scopolamine

Back 34

Alkaloid, similar to Atropine

Front 35

Side effect(s) of Scopolamine

Back 35

1. Loss of short term memory

Front 36

Clinical use(s) of Scopolamine

Back 36

1. Prevent motion sickness

Front 37

Derivation of Glycopyrrolate

Back 37

Synthetic, similar to Atropine

Front 38

Clinical use(s) of Glycopyrrolate

Back 38

1. Use as preanesthetic -> less tachycardia, decrease acid in stomach and IV, IM, SC is fast action

Front 39

Direct acting cholinergic drugs

Back 39

Bethanechol, Carbachol, Methacholine, Pilocarpine
Derivation of Bethanechol

Front 40

2. Stimulate detrusor muscle - relax trigone and sphincter = urination
Receptor affinity of Bethanechol

Back 40

Direct muscarinic receptor stimulant (No nicotinic action)
Degradation of Bethanechol

Front 41

2. Bladder atony treatment in humans postpartum
Side effects of Bethanechol

Back 41

Salivation, Sweating (diaphoresis), hypotension, colic, nausea, bronchospasm, miosis, urinary urgency, diarrhea
Derivation of Carbachol

Front 42

2. Colic in horses
Derivation of Methacholine

Back 42

Synthetic choline ester
Receptor affinity of Methacholine

Front 43

2. Treat glaucoma due to blockage of canal of schlem (act on ciliary m to decrease fluid pressure)
Indirect reversible cholineric drugs

Back 43

Physostigmine, Neostigmine, Edrophonium
Derivation of Physostigmine

Front 44

2-4 hour duration
Clinical use(s) of Physostigmine

Back 44

1. Cross BBB

Front 45

4. Reverse curarae-like effects
Derivation of Neostigmine

Back 45

Synthetic - related to Physostigmine
Clinical use(s) of Neostigmine

Front 46

2. Does not cross BBB!
Derivation of Edrophonium

Back 46

Similar to neostigmine (synthetic - related to Physostigmine)
Degradation of Edrophonium

Front 47

2. Reverse curarae-like effect
Parasympathetic Drugs (Anticholinergic)

Back 47

Atropine, Scopolamine, Glycopyrrolate, Homatropine, Ipratropine, Daritenacin
Derivation of Atropine

Front 48

8. High therapeutic dose = tachycardia -> stops vagus innervation on heart
Receptor affinity of Atropine

Back 48

Competitively binds to muscarinic receptor to prevent Ach binding
Side effect(s) of Atropine

Front 49

6. Antidote for shroom poisoning
Derivation of Scopolamine

Back 49

Alkaloid, similar to Atropine
Side effect(s) of Scopolamine

Front 50

2. More effective centrally
Derivation of Glycopyrrolate

Back 50

Synthetic, similar to Atropine
Clinical use(s) of Glycopyrrolate