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Pharmacology > Unit 2. Autonomics > Flashcards

Unit 2. Autonomics Flashcards

1
Q

Bethanechol

A

Class: Direct acting cholinomimetic, carbamic ester derivative
MOA: direct acting on muscarinic ACh receptors
Uses: Ileus (post op, neurogenic), urinary retention
Tox: SLUDGE

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2
Q

Meaning of SLUDGE

A

Toxic effects of direct cholinomimetics (muscarinic): salivation, lacrimation, urination, defecation, GI distress, emesis

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3
Q

Muscarine

A

Class: Direct acting cholinomimetic (musc), non-ester alkaloid
MOA: direct acting on musc Ach receptors
Uses: none give
Tox: SLUDGE

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4
Q

Cevimeline

A

Class: Direct acting musc cholinomimetic, non-ester alkaloid
MOA: direct acting on musc ACh receptors
Uses: dry mouth (xerostomia)– can be post-radiation, Sjogrens
Tox: SLUDGE

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5
Q

Nicotine

A

Class: Direct acting nicotinic cholinomimetic, non-ester alkaloid
MOA: direct acting on nicotinic ACh receptors
Uses: smoking cessation (reduces cravings)
Tox: none given

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6
Q

Neostigmine

A 
Class: Indirect acting cholinomimetic
MOA: AChE inhibitor
Uses: ileus (post-op, neurogenic), urinary retention, myasthenia gravis, reversal of neuromuscular blockade (non-depolarizing)
Tox: SLUDGE + paralysis, resp distress
Note: short-acting (lasts .5-2 hrs)
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7
Q

Physostigmine

A 
Class: Indirect acting cholinomimetic, Carbamate ester
MOA: AChE inhibitor
Uses: glaucoma
Tox: SLUDGE + paralysis, resp distress
Note: short-acting (lasts .5-2 hrs)
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8
Q

Pilocarpine

A

Class: Direct acting cholinomimetic, non-ester alkaloid
MOA: direct muscarinic activation
Uses: glaucoma (ciliary muscle contration)
TOX: SLUDGE

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9
Q

Donepezil

A

Class: Indirect cholinomimetic, non-ester
MOA: AChE inhibitor
Uses: Alzheimers (amplifies endogenous ACh in CNS)
Tox: SLUDGE + paralysis, resp distress

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10
Q

Edrophonium

A

Class: Indirect cholinomimetic, non-ester
MOA: AChE inhibitor
Uses: Myasthenia gravis (differentiate b/n deficiency and overload), ileus
Tox: SLUDGE + paralysis, resp distress
Note: v short acting (lasts 5-15 mins)

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11
Q

Echothiophate

A

Class: Indirect cholinomimetic, organophosphate
MOA: AChE inhibitor via phosphorylation (can be irreversible)
Uses: glaucoma
Tox: SLUDGE + paralysis, resp distress
Note: LONG acting (>100 hrs)

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12
Q

Pralidoxime (2-PAM)

A

Class: strong nucleophile
MOA: regenerates phosphorylated AChE
Uses: antidote for poisoning w nerve gas (Sarin), insecticides
Note: give quickly before enzyme “ages”

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13
Q

Atropine

A

Class: Tertiary amine antimuscarinic
MOA: blocks musc receptors
Uses: mydriasis, cycloplegia; to save from AchEi
Tox: musc block (dry as a bone, blind as a bat, red as a beet, mad as a hatter) + atropine fever + tachycardia (after initial brady)

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14
Q

Scopolamine

A

Class: Tertiary amine antimuscarinic
MOA: blocks musc receptors
Uses: prevent/reduce motion sickness
Tox: musc block (dry as a bone, blind as a bat, red as a beet, mad as a hatter) + atropine fever + tachycardia (after initial brady)

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15
Q

Dicyclomine

A

Class: Tertiary amine antimuscarinic
MOA: blocks musc receptors
Uses: reduce transient GI hypermotility
Tox: musc block (dry as a bone, blind as a bat, red as a beet, mad as a hatter) + atropine fever + tachycardia (after initial brady)

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16
Q

Tropicamide

A

Class: Tertiary amine antimuscarinic
MOA: blocks musc receptors
Uses: mydriasis, cycloplegia (very rapidly metabolized; short acting)
Tox: musc block (dry as a bone, blind as a bat, red as a beet, mad as a hatter) + atropine fever + tachycardia (after initial brady)

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17
Q

Tolterodine

A

Class: Tertiary amine antimuscarinic
MOA: blocks musc receptors
Uses: treat transient cystitis, post-op bladder spasms, incontinence
Tox: musc block (dry as a bone, blind as a bat, red as a beet, mad as a hatter) + atropine fever + tachycardia (after initial brady)

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18
Q

Benztropine

A

Class: Tertiary amine antimuscarinic
MOA: blocks musc receptors
Uses: Parkinsons (crosses BBB)
Tox: musc block (dry as a bone, blind as a bat, red as a beet, mad as a hatter) + atropine fever + tachycardia (after initial brady)

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19
Q

Ipatropium

A

Class: Quarternary amine antimuscarinic
MOA: blocks musc receptors
Uses: asthma, COPD (bronchodilation); short acting
Tox: musc block (dry as a bone, blind as a bat, red as a beet, mad as a hatter) + atropine fever + tachycardia (after initial brady)

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20
Q

Tiotropium

A

Class: Quarternary amine antimuscarinic
MOA: blocks musc receptors
Uses: asthma, COPD (bronchodilation); long acting
Tox: musc block (dry as a bone, blind as a bat, red as a beet, mad as a hatter) + atropine fever + tachycardia (after initial brady)

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21
Q

Hexamethonium

A

Class: Ganglionic blocker, quarternary amine
MOA: blocks nicotinic-N receptors
Uses: HTN crisis, “bloodless” field surgery (decreasing symp tone)

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22
Q

Succinylcholine

A

Class: depolarizing NMJ blocker
MOA: super agonist; overstimulation of nicotinic receptors –> desensitization of muscle unit
Tox: resp paralysis, disturbance of autonomic fxn (can interact a bit with nicotinic-N)
Notes: block in UNAFFECTED (maybe increased) by AChE inhibitors; very quick acting

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23
Q

Tubocurarine

A

Class: non-depolarizing NMJ blocker
MOA: competitive inhib at nicotinic-M receptor
Uses: MM relaxant for surgery w/o deep anesth
Tox: resp paralysis, disturbance of autonomic fxn (can interact a bit with nicotinic-N)
Notes: lasts 30-60 mins; block IS decreased by AChE inhibitor

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24
Q

Mivacurium

A

Class: non-depolarizing NMJ blocker
MOA: competitive inhib at nicotinic-M receptor
Uses: MM relaxant for surgery w/o deep anesth
Tox: resp paralysis, disturbance of autonomic fxn (can interact a bit with nicotinic-N)
Notes: shorter acting than tubocurarine; block IS decreased by AChE inhibitor

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25
Q

Botulin toxin A

A

Class: local paralytic
MOA: degrades SNAP-25 –> blocks ACh vesicle fusion and release (pre-synaptic)
Uses: reduce wrinkles, achalasia, strabismus, oromandibular dystonia

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26
Q

Norepinephrine

A

Class: non-selective sympathomimetic
MOA: agonist @ a1, a2, b1
Uses: hypotension
Tox: HTN, arrhythmias, headache

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27
Q

Epinephrine

A

Class: non-selective sympathomimetic
MOA: agonist @ a1, a2, b1, b2
Uses: anaphylactic shock, to contain local anesthetics, glaucoma, control hemorr in superficial surgery
Tox- palpitations, arhythmias, headache, tremor

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28
Q

Amphetamine

A

Class: indirect sympathomimetic
MOA: increases release of NE from cytoplasmic pool (no Ca necessary)
Uses: ADHD, narcolepsy, recreational
Tox: HTN, insomnia, anxiety, arrhythmias

29
Q

Tyramine

A

Class: indirect sympathomimetic
MOA: increases release of NE from cytoplasmic pool via exchange transporter (no Ca necessary)
Uses:
Note: tachyphylaxis = acute tolerance (pool used up); source = fermented foods

30
Q

Isoproteronol

A

Class: non-selective B agonist
MOA: agonist @ b1, b2
Uses: bronchodilation (asthma), shock, heart block
Tox: palpitation, tachyarrhythmias, headache

31
Q

Dobutamine

A

Class: B1 selective agonist
MOA: agonist @ b1
Uses: cardiac decompensation, shock, heart block; use for “chemical cardiac stress test”
Tox: tachyarrhythmias, HTN

32
Q

Albuterol

A

Class: B2 selective agonist
MOA: agonist @ b2
Uses: prevent/reverse exercise-induced bronchospasm, mild asthma, COPD
Tox: tachycardia (reflex), MM temor; can mask progressively sever inflammation

33
Q

Terbutaline

A

Class: B2 selective agonist
MOA: agonist @ b2
Uses: prevent/reverse exercise-induced bronchospasm, mild asthma, COPD + early labor
Tox: tachycardia (reflex), MM temor; can mask progressively sever inflammation

34
Q

Phenylephrine

A

Class: a1 selective agonist
MOA: agonist @ a1
Uses: nasal congestions, postural hypotension
Tox: HTN, reflex bradycardia

35
Q

Clonidine

A

Class: a2 selective agonist
MOA: agonist @ a2 (inhib autoreceptor) –> decrease symp output from CNS
Uses: HTN, shock, withdrawl from drug dependence (cross BBB)
Tox: sedation

36
Q

a-methyldopa

A

Class: a2 selective agonist
MOA: prodrug that decreases synthesis of NE (goes through pathway instead of dopa) + end product (a-methylNE) activates a2 receptors
Uses: HTN, shock, withdrawl from drug dependence (cross BBB)
Tox: sedation

37
Q

Fenoldopam

A

Class: selective D1 agonist
MOA: agonist @ D1 –> vasodilation @ renal, coronary, mesentaric
Uses: to incr blood flow @ these areas; hypertensive emergency; anuria
Tox: postural hypotension

38
Q

Dopamine

A

Class: mixed acting agonist (direct/indirect)
MOA: agonist @ D1, b1, a1 (as dose increases, in that order); also increases NE release
Uses: shock, renal failure, hypotension
Tox- vasoconstriction @ high doses

39
Q

Phentolamine

A

Class: non-selective a antagonist
MOA: comp antag @ a1, a2 (–>vasodilation)
Uses: pheochromocytoma (w b blocker), Raynauds, frostbite, shock
Tox: postural hypotension, inhibition of ejaculation, reflex tachy

40
Q

Phenoxybenzamine

A

Class: non-selective a antagonist
MOA: non-comp antag @ a1, a2 (covalent bond)
Uses: pheochromocytoma (w b blocker), Raynauds, frostbite, shock
Tox: postural hypotension, inhibition of ejaculation, reflex tachy

41
Q

Prazosin

A

Class: a1 selective antagonist
MOA: comp antag @ a1–> vasodilation
Uses: primary HTN, BPH
Tox: postural hypotension (usually 1st dose)
Note: less tachy than phentolamine, phenoxybenzamine because a2 autoreceptor is open for NE to bind –>less NE release on B1 receptors (–>less tachy)

42
Q

Propanolol

A

Class: 1st gen b blocker (non-selective)
MOA: antag @ B1, B2
Uses: angina, HTN, arrhythmias
Tox: bradycardia, bronchoconstriction, sexual dysfunction

43
Q

Timolol

A

Class: 1st gen b blocker (non-selective)
MOA: antag @ B1, B2
Uses: angina, HTN, arrhythmias, glaucoma
Tox: bradycardia, bronchoconstriction, sexual dysfunction

44
Q

Metoprolol

A

Class: 2nd gen b blocker (b1 selective)
MOA: antag @ B1
Uses: angina, HTN, arrythmias, CHF
Tox: bradycardia, sexual dysfxn

45
Q

Atenolol

A

Class: 2nd gen b blocker (b1 selective)
MOA: antag @ B1
Uses: angina, HTN, arrythmias, CHF
Tox: bradycardia, sexual dysfxn

46
Q

Bisoprolol

A

Class: 2nd gen b blocker (b1 selective)
MOA: antag @ B1
Uses: angina, HTN, arrythmias, CHF
Tox: bradycardia, sexual dysfxn

47
Q

Carvedilol

A

Class: 3rd gen “A” b-blocker
MOA: antag @ B1, B2, + “additional action” @ a1
Uses: CHF, HTN
Tox: bradycardia, fatigue

48
Q

Labetalol

A

Class: 3rd gen “A” b-blocker
MOA: antag @ B1, B2, + “additional action” @ a1
Uses: CHF, HTN
Tox: bradycardia, fatigue

49
Q

Betaxolol

A

Class: 3rd gen “B” b-blocker (b1 selective)
MOA: antag @ B1 + “additional action” of blocking Ca2+ channel
Uses: CHF, HTN
Tox: bradycardia

50
Q

Cocaine

A

Class: indirect acting adrenergic
MOA: prevents NE uptake; crosses BBB

51
Q

Guanethidine

A

Class: indirect acting adrenergic antagonist
MOA: false NT (vesicles get filled w this instead of NE)
Uses: HTN; not used in US; does not cross BBB
Tox: many and serious

52
Q

Reserpine

A

Class: Indirect acting adrenergic antag
MOA: release of empty vesicles (binds uptake transporter so NE is not taken up into vesicle)
Uses: older antihypertensive
Tox: many, serious (incl depression, suicide)
Note: cheap, still used abroad

53
Q

a-methyl-tyrosine

A

Class: indirect adrenergic antag
MOA: inhibits tyrosine hydroxylase (rate-limiting step) –> decr NE synth
Uses: pheochromocytoma
Tox: many, serious

54
Q

Ephedrine

A

Class: mixed indirect/direct acting adrenergic
Uses: nasal decongestant, anorexic

55
Q

Direct cholinomimetics

A

Bethanechol, muscarine, pilocarpine, cevimeline, nicotine

56
Q

Indirect cholinomimetics

A

Neostigmine, physostigmine, donepezil, edrophonium, echothiophate

57
Q

Anti-muscarinics: types + drugs

A

tertiary amines: atropine, scopolomine, dicyclomine, tropicamide, tolterodine, benztropine
quart amines: ipatropium, tiotropium

58
Q

Ganglionic blockers

A

Hexamethonium

59
Q

NMJ blockers- types + drugs

A

depolarizing: succinylcholine

non-depol: tubocurarine, mivacurium

60
Q

Non-selective adrenergic agonists (+targets)

A

norepi (a1, a2, b1), epi (a1, a2, b1, b2), isoproterenol (b1, b2)
ergot alkaloids: ergonovine (a), ergotamine (a), bromocriptine (d1, d2)

61
Q

Indirect acting adrenergic agonists

A

amphetamine, tyramine, ephedrine (mixed), dopamine (mixed), cocaine

62
Q

Selective b agonists

A

b1: dobutamine
b2: albuteral, terbutamine

63
Q

Selective a agonist

A

a1: phenylephrine
a2: clonidine, a-methyl-dopa

64
Q

D1 agonists

A

dopamine (non-selective; also b1, a1 + indirect NE release)

fenoldopam (d1-selective)

65
Q

a-blockers (non-selective + selective)

A

non-sel: phentolamine, phenoxybenzamine

a1-sel: prazosin

66
Q

non-selective b-blockers

A

1st gen: propanolol, timolol

3rd gen “A”: carvedilol, labetalol (+a1 block)

67
Q

selective b-blockers

A

2nd gen: metoprolol, atenolol, bisoprolol (b1)

3rd gen “B”: betaxolol (+Ca channel block)

68
Q

Indirect acting adrenergic antagonists

A

Guanethidine, reserpine, a-methyl-tyrosine

Pharmacology (5 decks)

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