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DVM Pharmacology > ANS Mimetics & Lytics > Flashcards

ANS Mimetics & Lytics Flashcards

1
Q

Parasympathetic Presynaptic Receptor and Neurotransmitter

A

N - Nicotinic (Cholinergic)

ACh - Acetylcholine

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2
Q

Parasympathetic Postsynaptic Receptor and Neurotransmitter

A

M1-5 - Muscarinic (Cholinergic)

ACh - Acetylcholine

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3
Q

Direct Parasympathomimetic (1)

A

Bethanechol (PO)

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4
Q

Reversible, Indirect Parasympathomimetics (3): Acetylcholinesterase Inhibitor, Cholinesterase Inhibitor, Anticholinesterase, Cholinergic

A

Edrophonium (inj)
Neostigmine (inj, PO)
Pyridostigmine (inj, PO, ER)

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5
Q

Direct Parasympatholytics (4): Muscarinic Antagonist, Anticholinergic, Antimuscarinic

A

Atropine (inj, PO, ophth)
Glycopyrrolate (inj)
Oxybutynin (PO, ER)
Propantheline (PO, ER)

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6
Q

M3 selectivity at detrusor muscle for contraction of the bladder; also stimulates contraction of GI smooth muscle

A

Bethanechol

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7
Q

Shortest to Longest Onset and Duration of Action for Reversible, Indirect Parasympathomimetics: Edrophonium, Neostigmine, Pyridostigmine

A

Edrophonium 1min to 10min

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8
Q

__________ is used for the Tensilon Response test for canine myasthenia gravis.

A

Edrophonium

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9
Q

__________ is most commonly used to treat canine myasthenia gravis.

A

Pyridostigmine

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10
Q

_________ crisis: caused by not enough ACh/receptor interactions

A

myasthenic

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11
Q

__________ crisis: caused by too many ACh/receptor interactions

A

cholinergic

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12
Q

Carbaryl ad Propoxur are examples of Carbamate insecticides, which are __________, indirect parasympathomimetics.

A

reversible

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13
Q

Chlorpyrifos, Diazinon and Malathion are examples of Organophosphate insecticides, which are __________, indirect parasympathomimetics.

A

irreversble

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14
Q

Which is metabolized faster, carbamate or organophosphate insecticides?

A

carbamate

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15
Q

Carbamate insecticides are less selective for motor end plate nicotinic receptors than Edrophonium, Neostigmine or Pyridostigmine; but more likely to cross the blood-brain barrier leading to CNS signs such as seizure. True or False

A

True

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16
Q

Primary Signs: Muscarinic (associated with Carbamate and Organophosphate toxicity)

A 
DUMBBELS
Diarrhea
Urination
Miosis (+++ pupil constriction)
Bronchospasm
Bradycardia
Emesis (vomiting)
Lacrimation
Salivation
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17
Q

Secondary Signs: Nicotinic (associated with Carbamate and Organophosphate toxicity)

A

muscle tremors
weakness
paralysis
CNS excitement less common

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18
Q

Tertiary Signs (associated with Carbamate and Organophosphate toxicity)

A

Nicotinic Blockade

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19
Q

Treat carbamate or organophosphate toxicity with __________ for nonspecific counteraction of physiologic and muscarinic effects.

A

Atropine

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20
Q

__________ is required in early stages of onset of organophosphate toxicity in order to break the chemical bonds prior to “aging” (irreversible development of strong bond holding organophosphate to the active site of acetylcholinesterase)

A

Antidote: Pralidoxime (2-PAM)

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21
Q

Prototypical nonspecific muscarinic antagonist:

A

Atropine

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22
Q

Atropine is an __________ originally extracted from the belladonna plant.

A

alkaloid (Alkaloid, any of a class of naturally occurring organic nitrogen-containing bases. Alkaloids have diverse and important physiological effects on humans and other animals. Well-known alkaloids include morphine, strychnine, quinine, ephedrine, and nicotine.)

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23
Q

Glycopyrrolate has a slower onset of action and longer duration of action than Atropine. True or False

A

True: Glycopyrrolate onset 30min, duration 2-3h

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24
Q

CAUTION in __________ with atropine, since it decreases intestinal motility and may lead to adynamic ileus.

A

horses, equids

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25
Q

_________ is the paralysis of the ciliary muscle of the eye leading to loss of lens accommodation and blurred vision. CAUTION in _________ with atropine, since blurred vision can caused panic.

A

cycloplegia; horses

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26
Q

_________ have endogenous atropinases and thus metabolize atropine rapidly, limiting its clinical utility in this species.

A

rabbits

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27
Q

Atropine is indicated for __________ crisis.

A

cholinergic

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28
Q

Shortest to Longest Onset and Duration of Action for Parasympatholytics: Atropine, Glycopyrrolate

A

Atropine

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29
Q

Which is more arrhythmogenic, Atropine or Glycopyrrolate?

A

Atropine

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30
Q

Glycopyrrolate is a quaternary ammonium compound; it does not cross the blood-brain barrier and is therefore less likely to cause CNS effects. True or False

A

True

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31
Q

Glycopyrrolate is perferred over Atropine in rabbits. True or False

A

True

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32
Q

Pharmacokinetics and Indications for Oxybutynin are congruent with those of Propantheline; EXCEPT Oxybutynin is widely distributed whereas Propantheline does not cross the blood-brain barrier. True or False

A

True

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33
Q

At normal doses of Oxybutynin and Propantheline, the __________ and __________ appear to be the most affected.

A

bladder, intestinal tract (large intestine***)

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34
Q

Antispasmodic indicated for the GI tract:

A

Aminopentamide

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35
Q

Antispasmodic indicated for colic in equids and also used to treat bradycardia:

A

Buscopan (N-Butylscopolammonium Bromide)

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36
Q

Parasympathetic Effects: EYE (2)

A

1) contraction of ciliary muscle: lens accommodation for myopia (short/near-sightedness)
2) contraction of iris sphincter muscle for miosis (constriction)

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37
Q

Sympathetic Effects: EYE (3)

A

1) relaxation of ciliary muscle: lens accommodation for hypermetropia (long/far-sightedness)
2) contraction of iris radial muscle for mydriasis (dilation)
3) decrease aqueous humor production

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38
Q

Parasympathetic Effects: HEART (3)

A

1) decreased heart rate: bradycardia
2) decreased contractility: -ve inotropy
3) decreased AV node conduction

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39
Q

Sympathetic Effects: Beta 1: HEART (3)

A

1) increased heart rate: tachycardia
2) increased contractility: +ve inotropy
3) increased automaticity and increased AV node conduction

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40
Q

Parasympathetic Effects: VASCULATURE (1)

A

1) indirect vasodilation through release of endogenous nitrous oxide (NO) from endothelium

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41
Q

Sympathetic Effects: VASCULATURE (3)

A

1) Alpha 1 - vasoconstriction
2) Beta 2 - vasodilation
3) Alpha 2 - various (vasoconstriction/dilation)

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42
Q

Parasympathetic Effects: LUNG (2)

A

1) bronchoconstriction

2) increase respiratory secretions

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43
Q

Sympathetic Effects: Beta 2: LUNG (1)

A

Bronchodilation

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44
Q

Parasympathetic Effects: GI TRACT (3)

A

1) increase motility
2) relax sphincters
3) stimulate secretion

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45
Q

Sympathetic Effects: Alpha 1, Beta 1, Beta 2: GI TRACT (3)

A

1) decrease motility
2) contract sphincters
3) inhibit secretion

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46
Q

Parasympathetic Effects: URINARY BLADDER (2)

A

1) contract detrusor

2) relax sphincter

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47
Q

Sympathetic Effects: Alpha 1, Beta 2: URINARY BLADDER (2)

A

1) Alpha 1: contract sphincter

2) Beta 2: relax detrusor muscle

48
Q

DRUG + ACTION @ urinary bladder: contract detrusor muscle

A

Bethanechol: Direct Parasympathomimetic (M3+++)

49
Q

DRUG + ACTION @ urinary bladder: contract internal sphincter

A

Phenylopropanolamine, Estrogens: Mixed Sympathomimetic

50
Q

DRUG + ACTION @ urinary bladder: relax detrusor muscle

A

Oxybutynin or Propantheline: Direct Parasympatholytics

51
Q

DRUG + ACTION @ urinary bladder: relax internal sphincter

A

Phenoxybenzamine (Alpha nonselctive) or Prazosin (Alpha 1): Direct Sympatholytics

52
Q

Cholinergic Receptors (2)

A

Nicotinic + Muscarinic

53
Q

Nicotinic receptors are ________ receptors.

A

ionotropic

54
Q

Muscarinic receptors are ________ receptors.

A

metabotropic (g protein coupled)

55
Q

Nicotinic: Nm subtype represents

A

Nm are nicotinic receptors found at the neuromuscular junction (NMJ)

56
Q

Nicotinic: Nn subtype represents

A

Nn are nicotinic receptors found at CNS and autonomic ganglia

57
Q

There are _____ subtypes of muscarinic receptors:

A

5

58
Q

M 1, 3, 5 are ________

A

stimulatory

59
Q

M 2, 4 are ________

A

inhibitory

60
Q

Adrenergic Receptors (2)

A

Alpha + Beta

61
Q

Both Alpha and Beta receptors are ________ receptors.

A

metabotropic (g protein coupled)

62
Q

There are _____ subtypes of alpha receptors:

A

2

63
Q

There are _____ subtypes of beta receptors:

A

3

64
Q

Parasympathetic signs are observed with the use of ________ and ________ drugs.

A

Parasympathomimetic and Sympatholytic

65
Q

Sympathetic signs are observed with the use of ________ and ________ drugs.

A

Sympathomimetic and Parasympatholytic

66
Q

Both endogenous and synthetic catecholamines have ___ oral bioavailability but are readily absorbed from the respiratory tract (inhalation or nebulisation).

A

low

67
Q

Direct Sympathomimetics: Endogenous Catecholamines (3)

A

Epinephrine (inj)
Norepinephrine (inj)
Dopamine (inj)

68
Q

Direct Sympathomimetics: Synthetic Catecholamines (4)

A

Dobutamine (inj)
Isoproterenol (inj)
Phenylephrine (inj, PO, intranasal, ophth)
Ractopamine/Zilpaterol

BUT PHENYLEPHRINE AND RACTOPAMINE IS NOT TECHNICALLY A CATECHOLAMINE

69
Q

Epinephrine, an adrenergic agonist, activates 5 receptors:

A

1) Alpha 1
2) Alpha 2
3) Beta 1
4) Beta 2
5) Beta 3

70
Q

Epinephrine @ Alpha 1:

A

vasoconstriction (at high doses)

71
Q

Epinephrine @ Beta 2:

A

bronchodilation, vasodilation (at low doses)

72
Q

Epinephrine @ Beta 1:

A

cardiac contraction

73
Q

Epinephrine indications (3):

A

1) cardiac arrest
2) anaphylaxis
3) vasopressor effect

74
Q

Norepinephrine, an adrenergic agonist, activates 3 receptors:

A

1) Alpha 1*
2) Alpha 2*
3) Beta 1

75
Q

Which is the stronger vasocontrictor, Epi or Norepi; leading to strong baroreceptor response and decrease in heart rate and contractility in spite of Beta 1 effects?

A

NE (reflex vagal bradycardia as a result of baroreceptor response is therefore more common with no repinephrine)

76
Q

Avoid extravasation with ________ and ________.

A

Norepinephrine and Dopamine

77
Q

Dopamine and Dobutamine have a very _____ half life.

A

short (minutes)

78
Q

Dopamine action @ low to medium dose

A

peripheral dopamine receptor agonist: dilation of vascular beds (renal, mesenteric, coronary, intercerebral)

79
Q

Dopamine action @ medium to high dose

A

Beta 1 agonist (+ve inotrope, +ve chronotrope)

80
Q

Dopamine action @ high dose

A

Alpha 1 agonist (vasoconstriction with NE release), Beta 1 agonist (+ve inotrope, +ve chronotrope)

81
Q

Dobutamine, a synthetic catecholamine that act as direct sympathomimetics, acts primarily at ______ receptors, with minor action at ______ and ______ receptors.

A

Primary: Beta 1
Minor: Alpha 1, Beta 2

82
Q

Isoproterenol, a synthetic catecholamine that act as direct sympathomimetics, acts primarily at ______ and ______ receptors.

A

Beta 1 + Beta 2

83
Q

Phenylephrine is a synthetic catecholamine that acts as a direct sympathomimetic at _____ receptors, indicated for treatment of hypotension and shock.

A

Alpha 1

84
Q

Direct Sympathomimetics: Selective Beta 2 Agonists (4)

A

Albuterol
Clenbuterol
Terbutaline
Isoxuprine

85
Q

Albuterol, Clenbuterol, Terbutaline and Isoxuprine are agonists at _____ and minor agonists at ______ receptors.

A

Primary Agonist: Beta 2

Minor Agonist: Beta 1

86
Q

Nonspecific alpha adrenergic antagonist or alpha blocker, direct sympatholytic, indicated for the treatment of a hypertonic urethral sphincter (drug will relax sphincter) and pheochromocytoma

A

Phenoxybenzamine

87
Q

Specific Alpha 1 antagonist or Alpha 1 blocker, direct sympatholytic, indicated for the treatment of a hypertonic urethral sphincter (drug will relax sphincter)

A

Prazosin

88
Q

Class II antiarrhythmics indicated for the treatment of tachycardia:

A

beta adrenergic antagonists or beta blockers

89
Q

Nonselective beta blocker may also be considered an inverse agonist.

A

Propanolol

90
Q

Selective Beta 1 blocker

A

Atenolol, Esmolol

91
Q

Oral bioavailability of propanolol is ___ to ___% due to significant first-pass metabolic effect; thus the oral dose is significantly greater than the injectable on a mg/kg basis.

A

2 to 27%

92
Q

Propanolol is indicated for its beta 2 blockade effects: (3)

A

bradycardia, bronchospasm, hypotension; bradycardia by decreasing SA and AV node conduction and by decreasing cardiac output and myocardial oxygen demand

93
Q

Propanolol is indicated in the treatment of: (3)

A

supraventricular tachyarrhythmias subsequent to feline hyperthyroidism and methylxanthine/chocolate toxicosis

94
Q

Propanolol is mostly secreted as metabolites in

A

urine

95
Q

Propanolol readily crosses the blood-brain barrier. True or False

A

True

96
Q

The half life for propanolol is ____

A

1-2h

97
Q

Degree of passing the blood-brain barrier among beta blockers:

A

Propanolol (readily crosses) > Atenolol > Esmolol (does not cross)

98
Q

Half life among beta blockers:

A

Atenolol (2h) > Propanolol > Esmolol (20min)

99
Q

Propanolol has membrane stabilizing effects where as Esmolol lacks these effects.

A

True

100
Q

Atenolol requires minimal liver metabolism (___% excreted in the urine and ___% excreted in the feces.)

A

50/50

101
Q

Atenolol is a better choice for patients with respiratory disease due to Beta 1 selectivity with lack of Beta 2 effects that Propanolol antagonises. True or False

A

True

102
Q

Indirect Sympatholytic, blocks vesicular monoamine transporters thus reducing norepinephrine uptake into vesicles, leading to reduced NE storage and mediator depletion: used as a calming agent for equines in situations such as long term stall rest

A

Reserpine

103
Q

______ ______ ______ are indicated primarily for treatment of asthma (feline) and COPD (equine).

A

Selective Beta 2 Agonists (Direct Sympathomimetics): Albuterol, Clenbuterol, Terbutaline

104
Q

Selective Beta 2 Agonist, Direct Sympathomimetic, indicated as a peripheral vasodilator and tocolytic (uterine relaxation).

A

Isoxuprine

105
Q

Nonselective Beta Agonist: activation of Beta 1+2+3: indicated as a partitioning agent for increase of muscle deposition in late finishing food production animals

A

Ractopamine/Zilpaterol

106
Q

Indirect Sympathomimetics: 3 Groups

A

1) Tricyclic Antidepressants
2) Monoamine Oxidase Inhibitors (MAOIs)
3) Illicit Drugs

107
Q

Illicity Drugs as Indirect Sympathomimetics:

A

Amphetamine + Cocaine

108
Q

Amphetamine MOA

A

blocks NE release

109
Q

Cocaine MOA

A

blocks NE re-uptake

110
Q

Monoamine Oxidase Inhibitor MOA

A

inhibit MAO-B thus inhibiting the breakdown of dopamine; at high doses can also inhibit MAO-A thus inhibiting the breakdown of norepinephrine; also metabolises amphetamine to methamphetamine

111
Q

Mixed Sympathomimetics indicated for indirect increase in release of Norepi

A

Phenylpropanolamine + Ephedrine/Pseudoephedrine

112
Q

Phenylpropanolamine (PPA) acts primarily to increase norephinephrine release at ___________: Mixed Sympathomimetic

A

the neck of the bladder (urethral sphincter)

113
Q

Ephedrine is indicated for use as a CRI to maintain ___________ under anaesthesia.

A

blood pressure

114
Q

Ephedrine can be a component of some Chinese Herbal Therapies such as _____ ________.

A

Ma Huang

115
Q

________ to PPA is seen in human patients but not veterinary patients.

A

tachyphylaxis

116
Q

________ increase expression of Alpha 1 receptors in the internal urinary sphincter; synergism is observed when PPA is used in conjunction with hormonal therapies.

A

Estrogens (Diethylstilbestrol, Estriol)

117
Q

PPA MOI

A

treatment of urinary incontinence due to urethral sphincter hypotonus

DVM Pharmacology (2 decks)

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