Cology Quiz 3

Front 1

RLS in ACh synthesis?

Back 1

Choline uptake via active transport (source mainly diet)

Front 2

Action of ACHE (acetylcholinesterase)

Back 2

Metabolizes ACh into acetate and choline

Front 3

Action of CAT (choline acetyltransferase)

Back 3

Combine choline and acetyl CoA

Front 4

What type of channel is present on the the ACh nerve?

Back 4

Voltage-dependent calcium channel

Front 5

Acetylcholinesterase (ACHE) location

Back 5

RBC, nerves, muscle, and placenta; fastest enzyme

Front 6

Butyrylcholinesterase location

Back 6

plasma, liver, skin; fastest enzyme

Front 7

Drug Mechanism: prevent release

Back 7

Botulinus toxin, metacholine, and Mg++ with anticholinergic effect

Front 8

Drug Mechanism: interfere with synthesis

Back 8

Hemicholinium which blocks choline uptake

Front 9

Drug Mechanism: enhance release

Back 9

beta-bungarotoxin and black widow venom and causes muscle contraction

Front 10

Drug Mechanism: block postsynaptic receptors

Back 10

atropine (M), d-tubocurarie (Nm), hexamethonium (Nn), and alpha-bugarotoxin with antimuscarinic paralysis

Front 11

Drug Mechanism: inhibit enzyme

Back 11

Physostigmine with enhanced cholinergic function

Front 12

Components of nicotinic receptor

Back 12

5 subunits, Na+ ion channel, requires 2 drug molecules or ACh to activate

Front 13

Nicotinic receptor

Back 13

Stimulated by nicotine, inhibited by curare and trimethaphan

Front 14

Muscle nicotinic receptor

Back 14

2 alpha, 1 beta, 1 gamma, 1 delta

Front 15

Neural nicotinic receptor

Back 15

2 alpha-3 and 3 beta-4

Front 16

Ganglia nicotinic receptor

Back 16

2 alpha-4 and 3 beta-4

Front 17

Muscarinic receptors

Back 17

G-coupled (Gi and Gq/11), 7 membrane-spanning units, activated by muscarine and inhibited by atropine

Front 18

Acetylcholine brand name?

Back 18

Miochol

Front 19

Acetylcholine: direct cholinergic agonist

Back 19

topical use to cause miosis, short acting (10 min), nicotinic and muscarinic agonist

Front 20

Nicotine: direct cholinergic agonist

Back 20

stimulate ganglia, adrenal medulla and skeletal muscle

Front 21

Therapeutic use of nicotine

Back 21

nicotine withdrawal, ulcerative colitis

Front 22

Side effects of nicotine

Back 22

tremors, convulsions, respiratory paralysis, CTZ stimulant

Front 23

Methacholine brand name?

Back 23

Provocholine

Front 24

Methacholine: direct cholinergic agonist

Back 24

test of airway responsiveness in asthmatics (to diagnose), M3 receptors

Front 25

Carbachol brand name?

Back 25

Carbastat and Carboptic

Front 26

Carbachol: direct cholinergic agonist

Back 26

nicotinic and muscarinic effects, resistant to ACHE (effective orally), stimulate GI and bladder, used in urinary retention, glaucoma, and miosis

Front 27

Bethanechol brand name?

Back 27

Urecholine

Front 28

Bethanechol: direct cholinergic agonist

Back 28

selective muscarinic, resistant to ACHE, bowel and bladder stimulant (atony), urinary stimulant

Front 29

Bethanechol side effects?

Back 29

sweating, salivation, bronchospasm, accomodation problems

Front 30

Arecholine: direct cholinergic agonist

Back 30

natural alkaloid, nicotinic and muscarinic activity, being looked at in Alzheimer's disease, no activity of ACHE

Front 31

Muscarine: direct cholinergic agonist

Back 31

amantia muscarina (mushroom), muscarinic activity, no activity of ACHE

Front 32

Pilocarpine brand name?

Back 32

Ocusert, Pilocar, and Salagen

Front 33

Pilocarpine: direct cholinergic agonist

Back 33

natural alkaloid, muscarinic actions, stimulates sweat glands, salivary glands and gastric glands, crosses BBB

Front 34

Pilocarpine uses?

Back 34

Glaucoma, GI, xerostomia, looked at in Alzheimer's disease

Front 35

General toxicity of direct cholinergic agonists

Back 35

SLUD: salivation, lacrimation, urination, and defecation as well as sweating, visual problems, miosis, bradycardia, and hyptension

Front 36

Contraindications of direct cholinergic agonists

Back 36

Asthmatics, hyperthyroid patients (atrial fibrillation), myocardial ischemia, and peptic ulcer

Front 37

Indirect acting cholinergic agonists general info

Back 37

Inhibit ACHE, increasing ACh in synapse at all locations where ACh is released; activate ACh receptors

Front 38

Indirect acting cholinergic agonists stimulation

Back 38

Stimulate muscarinic receptors on autonomic organs; stimulate then desensitize ganglia and skeletal muscle

Front 39

Reversible indirect acting cholinergic agonists

Back 39

in minutes to hours: carbamates, quaternary ammoniums

Front 40

Irreversible indirect acting cholinergic agonists

Back 40

weeks to months: organophosphates, nerve gases

Front 41

Therapeutic uses of indirect acting cholinergic agonists

Back 41

paralytic ileus, stimulate urinary bladder, glaucoma, myasthenia gravis, anticholinergic poisoning, and Alzheimer's disease

Front 42

Physostigmine brand name?

Back 42

Esereine and Antilirum

Front 43

Physostigmine: indirect acting cholinergic agonist

Back 43

natural alkaloid, orally active, only available as injection, crosses BBB

Front 44

Uses of physostigmine?

Back 44

mitotic in glaucoma, atropine toxicity (with muscarinic side effects)

Front 45

Neostigmine brand name?

Back 45

Prostigmine

Front 46

Neostigmine: indirect acting cholinergic agonist

Back 46

doesn't enter CNS, oral and injection, uses: paralytic ileus, urinary retention, myasthenia gravis, and reverse neuromuscular blockade

Front 47

Pyridostigmine brand name?

Back 47

Mestinon and Regonol

Front 48

Pyridostigmine: indirect acting cholinergic agonist

Back 48

similar to neostigmine, slower onset, longer duration of action, orally and injection

Front 49

Uses of pyridostigmine?

Back 49

myasthenia gravis, prophylactic for nerve gases, and reverse neuromuscular blockade

Front 50

Edrophonium brand name?

Back 50

Tensilon, Reversol, and Enlon

Front 51

Edrophonium: indirect acting cholinergic agonist

Back 51

lacks carbamoyl group, blocks anionic site, very short duration of action (10 min), injection, for DIAGNOSIS of myasthenia gravis

Front 52

Tacrine brand name?

Back 52

Cognex

Front 53

Tacrine: indirect acting cholinergic agonist

Back 53

CNS selective-no carbamoyl group, reversible inhibitor

Front 54

Uses of Tacrine?

Back 54

Alzheimer's disease (modest effects, 15-30% of patients), does not slow disease, 4 times daily, and hepatotoxicity (30%, reversible)

Front 55

Donepezil brand name?

Back 55

Aricept

Front 56

Donepezil: indirect acting cholinergic agonist

Back 56

Alzheimer's disease, once daily dosing, no liver disease, effective in up to 80%, may slightly slow progression (~6 months), doesn't alter underlying disease, muscarinic side effects

Front 57

Galantamine brand name?

Back 57

Reminyl

Front 58

Galantamine: indirect acting cholinergic agonist

Back 58

Alzheimer's disease, oral, 2 times daily, natural alkaloid, reversible inhibitor

Front 59

Side effects of Galantamine?

Back 59

liver, GI tract, bronchoconstriction, drowsiness

Front 60

Rivastigmine brand name?

Back 60

Exelon

Front 61

Rivastigmine: indirect acting cholinergic agonist

Back 61

newest inhibitor for Alzheimer's diesease, long lasting inhibition, 10 hrs, oral, 2 times daily, MAY SLOW PROGRESSION, selective for G1 isoform found mainly in brain, slowly dissociates

Front 62

Side effects of Rivastigmine?

Back 62

muscarinic, hallucinations

Front 63

Irreversible inhibitors (organophosphates)

Back 63

high lipid solubility, low molecular weight, transdermal absorption, CNS penetration (uses: insecticides and nerve gases)

Front 64

Insecticide antidote?

Back 64

2-PAM

Front 65

Nicotinic antagonists

Back 65

neuronal type-ganglionic blockers
muscle type-neuromuscular blockers

Front 66

Muscarinic antagonists

Back 66

M1-neurons and GI tract
M2-heart
M3-smooth muscle, glands

Front 67

Atropine brand name?

Back 67

Atripisol, Ocu-tropin, Sal-tropin

Front 68

Atropine: cholinergic antagonist

Back 68

belladonna alkaloid, non-selective muscarinic blockade

Front 69

Uses of atropine?

Back 69

mydriasis, bradycardia, GI hyperactivity, bronchodilation (Homatropine with -OH, shorter duration)

Front 70

Atropine overdose effects?

Back 70

Dry as bone
Red as a beet
Blind as a bat
Mad as a hatter
Atropine fever (especially in children)
Antidote: physostigmine

Front 71

Scopolamine brand name?

Back 71

Scopace, Isopto-Hyoscine, Transderm Scop

Front 72

Scopolamine: cholinergic antagonist

Back 72

natural alkaloid, effective prophylaxis of motion sickness, mydriasis, amnesia, CNS depression, "twilight sleep" (opiate + scopolamine)

Front 73

Ipratropium brand name?
Tiotropium brand name?

Back 73

Atrovent
Spiriva

Front 74

Ipratropium and Tiotropium: cholinergic antagonists

Back 74

quaternary ammonium, doesn't cross BBB, inhalation, developed for bronchial relaxation, less paralytic effect than atropine on cilia, Tiotropium > duration of action
Ipratropium=M1-M3
Tiotropium=M1 and M3
Used in COPD and asthma

Front 75

Tolterodine brand name?

Back 75

Detrol

Front 76

Tolterodine: cholinergic antagonist

Back 76

selective for bladder, overactive bladder, dry mouth in 40% of patients

Front 77

Oxybutynin brand name?

Back 77

Ditropan

Front 78

Oxybutynin: cholinergic antagonist

Back 78

urinary incontinence, SE of dry mouth and dry eyes (Oxytrol=transdermal formulation)

Front 79

Solifenacin brand name?
Darifenacin brand name?

Back 79

Vesicare
Enablex

Front 80

Solifenacin and Darifenacin: cholinergic antagonists

Back 80

selective M3 antagonists, slightly more selective for bladder, less dry mouth and eye interactions, drug interactions (solifenacin-CYP3A4 and darifenacin-CYP3A4 and CYP2D6)

Front 81

Benztropin brand name?
Trihexyphenidyl brand name?

Back 81

Cogentin
Artane

Front 82

Benztropin and Trihexyphenidyl: cholinergic antagonists

Back 82

tremor in Parkinson's disease, balance DA release, doesn't stop progression of disease, CNS excitation

Front 83

Pirenzipine brand name?

Back 83

Gastrozepin

Front 84

Pirenzipine: cholinergic antagonist

Back 84

M1 selective, eliminate cholinergic histamine release (still have M3 activation available)