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M2 Pharmacology Jen > Cholinergic > Flashcards

Cholinergic Flashcards

1
Q

Acetylcholine: class

A

the original cholinergic agonist, naturally-occuring

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2
Q

Cholinergics: aka what?

A

parasympathomimetics. bind directly to cholinoceptors.

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3
Q

Acetylcholine: indication

A

glaucoma

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4
Q

Acetylcholine: why not widely used as therapy?

A

many actions, leads to diffuse effects, rapid inactivation by cholinestases

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5
Q

Carbachol: class

A

Cholinergic agonist

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6
Q

Carbachol: indication

A

Glaucoma

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7
Q

Carbachol: action

A

locally instilled in the eye, it mimics the effects of ACh, causing miosis and accomodation (ciliary muscle in a state of contraction).

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8
Q

Bethanechol: class

A

Muscurinic agonist

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9
Q

Bethanechol: indication

A

Neurogenic illeus

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10
Q

Bethanechol: PD

A

binds to muscarinic cholinergic receptors and causes contraction of smooth muscle

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11
Q

Bethanechol: tox

A

reflex tachycardia (due to vasodilation), bronchoconstriction, increased secretory activity (sweat, GI/respiratory secretions)

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12
Q

Bethanechol: special

A

has been replaced by newer drugs that act upstream on the neurons that release ACh (increase the release of ACh)

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13
Q

Methacholine: class

A

Muscurinic agonist

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14
Q

Methacholine: indication

A

Asthma dx: aerosolized form used to challenge pts during diagnostic testing for asthma

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15
Q

Methacholine: PD

A

binds to muscarinic cholintergic receptors in airway and causes bronchoconstriction; asthmatics with hyperreactive airways respond to lower concentrations

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16
Q

Methacholine: tox

A

bronchoconstriction, increased secretory activity (sweat, GI/respiratory secretions)

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17
Q

Pilocarpine: class

A

Muscurinic agonist

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18
Q

Pilocarpine: indication

A

glaucoma

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19
Q

Pilocarpine: PD

A

activates muscarinic receptors on the pupillary sphincter muscle, causing the muscle to stay relatively constricted (this prevents the muscles of the iris from blocking the already narrow angle between the sclera and the iris, and thus allows the aqueous humor to drain better)

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20
Q

Pilocarpine: tox

A

increased secretory activity (lacrimation)

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21
Q

Pilocarpine: route

A

topical

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22
Q

Nicotine: class

A

Nicotinic agonist

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23
Q

Nicotine: indication

A

smoking cessation

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24
Q

Nicotine: PD

A

binds to nicotinic receptors; slower action than the nicotine found in cigarettes

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25
Q

Nicotine: tox

A

CNS stimulation (drug is lipid soluble), neuromuscular junction depolarization leading to spasms and then paralysis (if given high dose); can cause increased sympathetic activity (since nicotinic receptors are in ganglia), leading to toxicity related to increased secretions from the adrenal glands

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26
Q

Varenicline: class

A

very selective partial agonist of a2-b4 nicotinic receptors (so nicotine can’t access)

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27
Q

Varenicline: indication

A

smoking cess

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28
Q

Varenicline: PD

A

CNS mesolimbic dopamine, partial a4-b2 stimulation prevents low dopamine and cravings; also prevents nicotine from creating dopamine surges, No chemical reward

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29
Q

Varenicline: PK

A

well absorbed; peak 4 h, t1/2 = 24 h; excreted primarily in urine as unchanged drug

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30
Q

Varenicline: special

A

Reports of suicidal thoughts and aggressive and erratic behavior → patients and caregivers should be instructed about the importance of monitoring for neuropsychiatric symptoms, and to communicate immediately with the prescriber the emergence of agitation, depression, unusual changes in behavior, or suicidality. Psychiatric patients – use extreme caution. Contraindicated in pregnancy/lactation. Causes drowsiness, caution operating machinery

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31
Q

Varenicline: monitor

A

neuropsychiatric symptoms

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32
Q

Edrophonium: class

A

Short acting AChE inhibitor

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33
Q

Edrophonium: indication

A

Myesthenia Gravis Dx

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34
Q

Edrophonium: PD

A

blocks action of cholinesterases, thereby increasing the action of ACh; an alcohol; does NOT form a covalent bond with esteratic site on ChE’s

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35
Q

Edrophonium: PK

A

very short acting

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36
Q

Edrophonium: special

A

charged so does not cross BBB

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37
Q

Neostigmine: class

A

Intermediate acting AChE inhibitor

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38
Q

Neostigmine: indication

A

Myesthenia Gravis Rx

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39
Q

Neostigmine: PD

A

blocks cholinesterases, thereby increasing the effect of ACh (restores neuromuscular transmission in MG patients); bind covalently to esteratic site of cholinesterase and leave behind a carbamoyl residue (blocks enzyme) that is released slowly over hours

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40
Q

Neostigmine: PK

A

longer acting than edrophonium but not as long as organophosphate ChE inhibitors

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41
Q

Neostigmine: tox

A

overdose results in increased muscarinic effects (cholinergic crisis)

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42
Q

Neostigmine: special

A

does not cross BBB

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43
Q

Physostigmine: class

A

Intermediate acting AChE inhibitor

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44
Q

Physostigmine: indication

A

Rx CNS side effects of muscarinic agonists

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45
Q

Physostigmine: PD

A

blocks cholinesterases, thereby increasing the effect of ACh (restores neuromuscular transmission in MG patients); bind covalently to esteratic site of cholinesterase and leave behind a carbamoyl residue (blocks enzyme) that is released slowly over hours

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46
Q

Physostigmine: PK

A

longer acting than edrophonium but not as long as organophosphate ChE inhibitors

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47
Q

Physostigmine: tox

A

overdose results in increased muscarinic effects (cholinergic crisis); enters the brain, and ChE inhibitors in CNS can have dangerous effects

48
Q

Physostigmine: special

A

crosses the BBB (uncharged and lipid soluble)

49
Q

Organophosphates: what fits in this category?

A

Sarin, soman, parathion, malathion

50
Q

Organiphosphates: class

A

Long acting AChE inhibitor

51
Q

Organiphosphates: indication

A

insecticides, nerve gasses, WMD. not really used medically

52
Q

Organiphosphates: PD

A

blocks cholinesterases, thereby increasing the effect of ACh (restores neuromuscular transmission in MG patients); bind covalently to esteratic site of cholinesterase and leave behind a phosphate residue (blocks enzyme) that is released slowly over days to weeks

53
Q

Organophosphates: PK

A

MUCH longer acting than the other two types of ChE inhibitors (carbamates and edrophonium)

54
Q

Ectothiophate: class

A

Long acting AChE inhibitor

55
Q

Ectothiophate: indication

A

glaucoma

56
Q

Ectothiophate: PD

A

blocks cholinesterases, thereby increasing the effect of ACh (restores neuromuscular transmission in MG patients); bind covalently to esteratic site of cholinesterase and leave behind a phosphate residue (blocks enzyme) that is released slowly over days to weeks

57
Q

Ectothiophate: PK

A

MUCH longer acting than the other two types of ChE inhibitors (carbamates and edrophonium)

58
Q

Pralidoxime: class

A

cholinesterase regenerator (rescue drug - action opposes that of organophsphate ChE inhibitors)

59
Q

Pralidoxime: indication

A

accidental exposure to insecticides or nerve gases that contain organophosphate ChE inhibitors

60
Q

Pralidoxime: PD

A

has high affinity for phosphate group that is bound to esteratic site of ChE (from organophosphate); binds phosphate group, which frees cholinesterase

61
Q

Pralidoxime: special

A

Give soon after exposure

62
Q

Metoclopramide: class

A

Indirect cholinergic, stimulates ACh release

63
Q

Metoclopramide: indication

A

Neurogenic illeus, nausea

64
Q

Atropine: class

A

non-selective muscarinic blocker

65
Q

Atropine: indication

A

to dilate pupils, bradycardia (raises HR), to decrease secretions, organophosphate poisoning (insecticide, etc – blocks action of ACh; given with Pralidoxime)

66
Q

Atropine: PD

A

lowers the parasympathetic activity of all muscles and glands regulated by the parasympathetic nervous system (dilates eye, increases HR, reduces airway secretions, etc)

67
Q

Atropine: PK

A

effect lasts 4-8 hours (except in eye, where they can last up to 72 hrs)

68
Q

Atropine: tox

A

Atropine poisoning (intensification of sympathetic effects in same end organs):
Mad as a hatter: delirium, hallucinations
Blind as a bat: mydriasis, photophobia, blurred vision (cycloplegia)
Dry as a bone: block of secretions (salivary, sweat)
Red as a beet: prostaglandins?, fever, anhidrosis (inability to sweat), dilation of vessels
Hot as a hare: hyperthermia resulting from anhidrosis; can be lethal in infants
Other side effects of atropine include:
urinary retention (block of detrusor muscle)
bronchodilation
constipation
tachycardia

69
Q

Atropine: excr

A

by both liver and kidney

70
Q

Atropine: special

A

lipid soluble (can cross BBB); use with caution in infants because of risk of hyperthermia; don’t use in men with prostatic hyperplasia

71
Q

Scopolamine: class

A

Muscurinic blocker

72
Q

Scopolamine: indication

A

Motion sickness, pupil dilation

73
Q

Scopolamine: PD

A

lowers the parasympathetic activity of all muscles and glands regulated by the parasympathetic nervous system (dilates eye, increases HR, reduces airway secretions, etc)

74
Q

Scopolamine: special

A

crosses BBB (effect on motion sickness via CNS)

75
Q

Benztropine: class

A

Muscurinic blocker

76
Q

Benztropine: indications

A

reduce symptoms of Parkinson’s and parkinsonism (decreases tremors)

77
Q

Benztropine: PD

A

lowers the parasympathetic activity of all muscles and glands regulated by the parasympathetic nervous system (dilates eye, increases HR, reduces airway secretions, etc)

78
Q

Succinylcholine: class

A

Depolarizing nicotinic blocker

79
Q

Succinylcholine: indication

A

Surgical paralysis

80
Q

Succinylcholine: PD

A

persistently depolarizes neuromuscular end plate, which causes flaccid skeletal muscle paralysis to develop desensitization; functions like ACh at NMJ; does NOT get to ganglia

81
Q

Succinylcholine: PK

A

short acting (effects of bolus last 5-7 min)

82
Q

Succinylcholine: excretion

A

cleared by plasma ChE

83
Q

Succinylcholine: interaction

A

Anesthetic gases and aminoglycoside antibiotics synergize with succinylcholine

84
Q

Succinylcholine: special

A

only NMJ depolarizing blocker in clinical use; do NOT give to patients lacking ChE (causes prolonged paralysis)

85
Q

Tubocurarine: class

A

Non-depolarizing nicotinic blocker

86
Q

Tubocurarine: indication

A

Surgical paralysis

87
Q

Tubocurarine: PD

A

directly blocks receptors on nicotinic end plate, thereby causing flaccid skeletal muscle paralysis

88
Q

Tubocurarine: PK

A

lasts 30-60 min (longer than succinylcholine)

89
Q

Tubocurarine: special

A

Throughout paralysis, consciousness and sensorium is intact  never give these types of drugs to an unanesthetized patient, and never let a patient emerge from anesthesia before reversing the paralysis with neostigmine

90
Q

Rocuronium: class

A

Non-depolarizing nicotinic blocker

91
Q

Rocuronium: indication

A

Surgical paralysis

92
Q

Rocuronium: PD

A

directly blocks receptors on nicotinic end plate, thereby causing flaccid skeletal muscle paralysis

93
Q

Rocuronium: PK

A

shorter acting than d-tubocurarine

94
Q

Rocuronium: excr

A

liver

95
Q

Rocuronium: special

A

don’t give to pts with liver disfunction

96
Q

Botulinum toxin: class

A

bacterial exotoxin

97
Q

Botulinum toxin: indication

A

facial wrinkles!

98
Q

Botulinium toxin: PD

A

blocks neuronal release of ACh; causes botulism; Interferes with docking proteins on the interior of the nerve membrane (vesicles containing ACh cannot dock properly and therefore cannot release ACh)  leads to flaccid paralysis; symptoms similar to atropine poisoning except for the CNS effects

99
Q

Cisatracurium: class

A

Non-depolarizing nicotinic blocker

100
Q

Cisatracurium: indication

A

Surgical paralysis

101
Q

Cisatracurium: PD

A

directly blocks receptors on nicotinic end plate, thereby causing flaccid skeletal muscle paralysis

102
Q

Cisatracurium: PK

A

shorter acting than d-tubocurarine

103
Q

Cisatracurium: excr

A

cleared by liver and plasma esterases

104
Q

Trimethaphan: class

A

NN (ganglionic) blocker

105
Q

Trimethaphan: indication

A

HTN: only to treat HTN crisis, or for controlled hypotension during surgery

106
Q

Trimethaphan: PD

A

blocks nicotinic transmission with both sympathetic and parasympathetic ganglia (NN receptors); produces veno- and vaso-dilatation

107
Q

Trimethaphan: PK

A

useful only when given iv; produces fall in BP within minutes; partly metabolized, and partly excreted by kidneys

108
Q

Trimethaphan: tox

A

watch out for sudden, severe drop in BP; also fall in HR; also, reduction in just about any sympathetic or parasympathetic response

109
Q

Trimethaphan: interactions

A

additive effects with most other antihypertensives;

110
Q

Trimethaphan: special

A

patients are quite miserable, hence only used during general anesthesia; also, helps to tilt patient to help control BP

111
Q

Trimethaphan: monitor

A

minute to minute monitoring of BP (and HR)

112
Q

Oxybutynin: class

A

Muscurinic blocker

113
Q

Oxybutynin: indication

A

Urgency and bladder spasms

114
Q

Glycopyrrolate: class

A

Muscurinic blocker

115
Q

Glycopyrrolate: indication

A

Urgency and bladder spasms

M2 Pharmacology Jen (11 decks)

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