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Cardiovascular II > Adrenoceptor agonists and antagonists > Flashcards

Adrenoceptor agonists and antagonists Flashcards

1
Q

Amino acid from which catecholamines are derived

A

Tyrosine

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2
Q

Metabolic precursor of noradrenaline and adrenaline

A

Dopamine

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3
Q

Enzymes that inactive norepinephrine and epinephrine

A

Monoamine oxidase (MAO)
Catecholamine-O methyltransferase (COMT)

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4
Q

Only enzyme that metabolizes norepinephrine intraneuronally

A

MAO

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5
Q

Neuronal reuptake inhibitors that potentiate effects of norepinephrine and epinephrine

A

Cocaine
TCAs

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6
Q

Vesicular reuptake inhibitor affecting catecholamine metabolism. Used to be used for HTN.

A

Reserpine

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7
Q

Agents that inhibit MAO-A, rarely used for depression.

A

Clorgyline
Moclobemide

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8
Q

Agent that inhibits MAO-B, used in Parkinson’s disease.

A

Selegiline

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9
Q

General result of activation of alpha-1 adrenergic receptors

A

Gq –> Activate phospholipase C –> IP3 and DAG –> increase Ca

Causes contraction and secretion

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10
Q

General result of activation of alpha-2 adrenergic receptors

A

Gi –> inhibit adenylyl cyclase –> decrease cAMP –> decrease NT release and cause muscle contraction

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11
Q

General affect of activation of beta-1 adrenergic receptors

A

Gs –> stimulate adenylate cyclase –> increase cAMP

Increase HR, force, and renin release

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12
Q

General affect of activation of beta-2 adrenergic receptors

A

Gs –> stimulate adenylate cyclase –> increase cAMP

Relax smooth muscle
Increase glycogenolysis, HR, and force

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13
Q

Locations of alpha-1 adrenergic receptors

A

Effector tissues
Smooth muscle
Glands

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14
Q

Locations of alpha-2 adrenergic receptors

A

Nerve endings
Some smooth muscle

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15
Q

Locations of beta-1 adrenergic receptors

A

Cardiac muscle
Juxtaglomerular apparatus

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16
Q

Locations of beta-2 adrenergic receptors

A

Smooth muscle
Liver
Heart

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17
Q

Locations of beta-3 adrenergic receptors

A

Adipose cells

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18
Q

General affect of activation of beta-3 adrenergic receptors

A

Gs –> stimulate adenylate cyclase –> increase cAMP

Increase lipolysis

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19
Q

General affect of activation of D3 adrenergic receptors

A

Gs –> stimulate adenylyl cyclase –> increase cAMP

Relax renal vascular smooth muscle

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20
Q

Location of D3 adrenergic receptors

A

Smooth muscle

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21
Q

Only adrenergic receptor present on the presynaptic region

A

Alpha-2 –> inhibitory

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22
Q

Adrenergic receptor that, when activated, inhibits the release of norepinephrine

A

Alpha-2

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23
Q

Adrenergic receptor in pancreas that decreases insulin secretion

A

Alpha-2

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24
Q

Adrenergic receptor in pancreas that increases insulin secretion

A

Beta-2

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25
Q

Direct acting sympathomimetic drug that is a selective alpha-1 agonist

A

Phenylephrine

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26
Q

Uses of phenylephrine

A

Nasal decongestant
Mydriatic
Hypotension (rare)

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27
Q

Side effect of phenylephrine

A

Reflex bradycardia 2/2 increased BP and TPR

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28
Q

Direct acting sympathomimetic drugs that are selective alpha-2 agonists

A

Clonidine
Apraclonidine
Brimonidine

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29
Q

Reason for selective, direct-acting alpha-2 agonist use in glaucoma

A

Reduce aqueous humor secretion by alpha-2 action in ciliary muscles

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30
Q

Uses of clonidine

A

Moderate HTN
Migraine prophylaxis
Management of withdrawal symptoms
Menopausal hot flashes
Control diarrhea in autonomic neuropathy 2/2 DM

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31
Q

Adverse effects of clonidine

A

Dry mouth
Sedation
Nasal stuffiness
Constipation
Impotence

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32
Q

Centrally acting alpha-2 adrenoceptor agonist use for management of spasticity in MS

A

Tizanidine

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33
Q

Direct acting sympathomimetic drug that is a selective beta-1 agonist

A

Dobutamine

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34
Q

Effect and use of dobutamine

A

More selective ionotropic and chronotropic effects –> used in HF to increase CO and SV without increasing HR

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35
Q

Direct acting sympathomimetic drugs that are selective beta-2 agonists

A

Terbutaline
Albuterol
Salmeterol

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36
Q

Uses of selective beta-2 agonists

A

Immediate relief of asthma
Arrest uncomplicated premature labor (24-34 wks)

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37
Q

Adverse effects of beta-2 agonists

A

Tremors in hands
Palpitations
Hypokalemia

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38
Q

Direct acting sympathomimetic drug that is a selective beta-3 agonist

A

Mirabegron

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39
Q

Use of mirabegron

A

Overactive bladder –> urgency and frequency

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40
Q

Direct acting sympathomimetic drug that is a non-selective alpha-1 and alpha-2 agonist

A

Oxymetazoline

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41
Q

Direct acting sympathomimetic drug that is a non-selective beta agonist (1, 2, and 3)

A

Isoproterenol

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42
Q

Effects of isoproterenol

A

Significant increase: HR, CO

Significant decrease: DBP, bronchial muscle

Increase: SBP, blood flow, blood sugar

Decrease: mean BP, intestinal muscle

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43
Q

Effects of adrenaline/epinephrine

A

Significant increase: CO, SBP, blood flow to skeletal muscle and liver, blood sugar

Significant decrease: Bronchial muscle, intestinal muscle

Increase: HR, mean BP, coronary blood flow

Decrease: Blood flow to skin, mucus membranes, kidney

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44
Q

Effects of norepinephrine

A

Significant increase: SBP, DBP, mean BP

Increase: Coronary blood flow

Decrease: HR, blood flow (skin, mucus membranes, kidney), intestinal muscle

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45
Q

Direct acting sympathomimetic drug that is a non-selective alpha-1, alpha-2, beta-1, and beta-2 agonist. May also have weak beta-3 action.

A

Epinephrine

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46
Q

Overall cardiac effect of epinephrine

A

Increase SBP

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47
Q

Overall vascular effect of epinephrine

A

Decrease DBP –> decrease TPR

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48
Q

Bronchial effects of epinephrine

A

Bronchodilation (beta-2)
Decrease bronchial secretion (alpha-1)

49
Q

GIT affects of epinephrine

A

Sphincter contraction (alpha-1)
Gut relaxation (alpha-2 and beta)

50
Q

Uses of epinephrine

A

Anaphylactic shock
Prolong duration of local anesthetic agents
Control epistaxis (rare)
Cardiac resuscitation

51
Q

Adverse effects of epinephrine

A

CVS –> angina, palpitation, arrhythmias

CNS –> anxiety, tremors, HA, cerebral hemorrhage

52
Q

Contraindications of epinephrine

A

HTN
Angina
Hyperthyroidism (receptor upregulation)
MAO use

53
Q

Direct acting sympathomimetic drug that is a non-selective alpha-1, alpha-2, and beta-1 agonist

A

Norepinephrine

54
Q

Overall cardiovascular affect of norepinephrine

A

Increase in SBP and DBP

55
Q

Uses of norepinephrine

A

Cardiogenic shock
Hypotensive states –> surgical shock and MI

56
Q

Reason that dopamine is preferred over norepinephrine for cardiogenic shock

A

Does not have risk of renal failure

57
Q

Direct acting sympathomimetic drug that is a non-selective D1, D2, and beta-1 agonist

A

Dopamine

58
Q

Dosing for dopaminergic effect of dopamine and the therapeutic effect

A

0.5-2 mcg/kg/min

Increase urine output and renal blood flow

59
Q

Dosing for beta-1 effect of dopamine and the therapeutic effect

A

2-10 mcg/kg/min

Increase renal blood flow, CO, HR, and cardiac contractility

60
Q

Dosing for alpha effect of dopamine and the therapeutic effect

A

> 10 mcg/kg/min

Increase BP and stimulate vasoconstriction

61
Q

Risk with high dose of dopamine

A

Tachyarrhythmia

62
Q

Uses of dopamine

A

Cardiogenic shock
CCF, liver, and renal failure
Hypotensive states –> after hypovolemia correction

63
Q

Adverse effects of dopamine

A

N/V
Tachycardia
HTN
Ectopic beats
Arrhythmias

64
Q

Hypotension that occurs when epinephrine is given after pretreatment with what?

A

Alpha blocker –> Dale’s vasomotor reversal

65
Q

Accentuated hypertensive effect that occurs when epinephrine is given after pretreatment with what?

A

Beta-blocker –> Dale’s vasomotor reversal

66
Q

Adrenoceptor acting drugs used as pressor agents

A

Norepinephrine
Dopamine
Ephedrine

67
Q

Adrenoceptor acting drugs used as cardiac stimulants

A

Epinephrine
Dobutamine

68
Q

Adrenoceptor acting drugs used as bronchodilators

A

Albuterol
Terbutaline
Salmeterol

69
Q

Adrenoceptor acting drugs used as nasal decongestants

A

Phenylephrine
Oxymetazoline
Pseudoephedrine

70
Q

Adrenoceptor acting drugs used as CNS stimulants

A

Amphetamine
Methamphetamine

71
Q

Adrenoceptor acting drug that were used as anorectics

A

Fenfluramine (obsolete)
Sibutramine (discontinued)

72
Q

Adrenoceptor acting drugs used as uterine relaxants

A

Terbutaline
Albuterol
Mirabegron

73
Q

Indirect-acting adrenoceptor agonists that work by releasing norepinephrine from vesicles

A

Amphetamine
Tyramine

74
Q

Indirect-acting adrenoceptor agonist that works by inhibiting uptake of norepinephrine from the synaptic cleft

A

Cocaine

75
Q

Indirect-acting adrenoceptor agonist that works by inhibiting MAO

A

Selegiline

76
Q

Indirect-acting adrenoceptor agonist that works by inhibiting COMT

A

Entacapone

77
Q

Uses of amphetamine

A

Narcolepsy
ADHD

78
Q

Therapeutic effects of amphetamine

A

Wakefulness and alertness
Decrease fatigue
Improve physical performance
Appetite suppression
Improves task performance, but also increases errors

79
Q

Contraindication of tyramine

A

Hypertensive crisis with MAO inhibitor

80
Q

Foods that contain tyramine

A

Cheese
Beef
Wine
Beer
Yogurt
Yeast

81
Q

Adrenergic agonists that are non-selective for alpha receptors

A

Phenoxybenzamine
Phentolamine

82
Q

Irreversible nonselective antagonist of alpha-1 and alpha-2

A

Phenoxybenzamine

83
Q

Therapeutic effects of phenoxybenzamine

A

Vasodilation
Hypotension
Reflex tachycardia

84
Q

Uses of phenoxybenzamine

A

Pheochromocytoma
Raynaud’s syndrome
Frostbite

85
Q

Adverse effects of phenocybenzamine

A

Marked postural hypotension
Inhibition of ejaculation
Sedation

86
Q

Competitive, reversible, non-selective agonist of alpha-1 and alpha-2

A

Phentolamine

87
Q

Therapeutic effects of phentolamine

A

Vasodilation
Hypotension
Reflex tachycardia

88
Q

Uses of phentolamine

A

Pheochromocytoma
Peripheral vascular disease
Hypertensive crisis

89
Q

Selective alpha-1 antagonists

A

Prazosin
Terazosin
Doxazosin
Alfuzosin
Tamsulosin
Silodosin

90
Q

Therapeutic effects of prazosin

A

Peripheral vasodilation
Phosphodiesterase inhibition –> vasodilates
Improved urine outflow in BPH

91
Q

Reason for lesser reflex tachycardia of prazosin compared to phentolamine and phenoxybenzamine

A

No alpha-2 blocking, no promotion of norepinephrine release

92
Q

Uses of prazosin

A

Hypertension
BPH
Raynaud’s –> rare, CCB prefered

93
Q

Adverse effect of prazosin

A

Postural hypotension

94
Q

Alpha-1A antagonists, specific for smooth muscles in bladder neck and urethra

A

Tamsulosin
Silodosin

95
Q

Adverse effects of tamsulosin and silodosin

A

Abnormal ejaculation
Floppy iris syndrome

96
Q

Selective alpha-2 agonist

A

Yohimbine

97
Q

Uses of yohimbine

A

Generally unestablished

Male sexual dysfunction
Diabetic neuropathy

98
Q

Non-selective beta antagonists

A

Propranolol
Timolol
Sotalol
Pindolol

99
Q

Cardiovascular effects of propranolol

A

Decrease HR, contractility, conduction, and CO –> reduced myocardial oxygen demand

Decreased renin secretion

Increased TPR

100
Q

Respiratory effect of propranolol

A

Bronchoconstriction in asthma

101
Q

Metabolic effects of propranolol

A

Increase LDL and triglyceride
Decrease HDL

Hypoglycemia masking in diabetics

102
Q

CNS effects of propranolol

A

Sedation
Lethargy
Sleep disturbance
Suppress performance anxiety

103
Q

Miscellaneous effects of propranolol

A

Decrease formation of aqueous humor
Reduce portal venous pressure in cirrhosis

104
Q

Uses of propranolol

A

CHF
Stable angina pectoris
Arrhythmias
MI
Migraine prophylaxis
Peripheral manifestation of anxiety
Hyperthyroidism
Pheochromocytoma –> with alpha blocker
Alcohol withdrawal
Esophageal varices and portal HTN

105
Q

Contraindication of propranolol

A

Prinzmetal’s angina

106
Q

Adverse effects of propranolol

A

Bronchoconstriction
Bradycardia
Cold extremities
Hypoglycemia
Fatigue
Sleep disturbance
Rebound HTN
Adverse lipid profile

107
Q

Treatment of propranolol toxicity

A

Maintain ABCs
IV fluid and atropine
Glucagon

108
Q

Non-selective beta blocker used as eye drop for open angle glaucoma

A

Timolol

109
Q

Reason sotalol is also a class II anti-arrhythmic drug

A

Additional K blocking property

110
Q

Selective beta-1 antagonists

A

Atenolol
Esmolol
Metoprolol

111
Q

Advantages of selective beta-1 antagonists

A

Safer in asthma
Safer in diabetics
Safer in PVE
Less effect on lipids

112
Q

Prominent beta-1 and beta-2 antagonist with a lesser alpha-1 antagonistic effect

A

Carvedilol

113
Q

Actions of carvedilol

A

Inhibits free radical induced lipid peroxidation
Inhibits smooth muscle mitogenesis
Blocks L-type voltage gated Ca channels

114
Q

Uses of carvedilol

A

CHF
HTN
Angina

115
Q

Selective alpha-1 and beta-1 antagonist with partial agonistic action on beta-2

A

Labetalol

116
Q

Therapeutic effects of labetalol

A

Decrease BP
Peripheral vasodilation
Bronchodilation

117
Q

Uses of labetalol

A

HTN in pregnancy
Pheochromocytoma
Rebound HTN from clonidine

118
Q

Adverse effects of labetalol

A

Postural hypotension
Hepatotoxicity

119
Q
A

Cardiovascular II (29 decks)

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