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Cardiovascular II > Adrenoceptor agonists and antagonists > Flashcards

Adrenoceptor agonists and antagonists Flashcards

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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
Direct acting sympathomimetic drug that is a selective alpha-1 agonist
Phenylephrine
26
Uses of phenylephrine
Nasal decongestant Mydriatic Hypotension (rare)
27
Side effect of phenylephrine
Reflex bradycardia 2/2 increased BP and TPR
28
Direct acting sympathomimetic drugs that are selective alpha-2 agonists
Clonidine Apraclonidine Brimonidine
29
Reason for selective, direct-acting alpha-2 agonist use in glaucoma
Reduce aqueous humor secretion by alpha-2 action in ciliary muscles
30
Uses of clonidine
Moderate HTN Migraine prophylaxis Management of withdrawal symptoms Menopausal hot flashes Control diarrhea in autonomic neuropathy 2/2 DM
31
Adverse effects of clonidine
Dry mouth Sedation Nasal stuffiness Constipation Impotence
32
Centrally acting alpha-2 adrenoceptor agonist use for management of spasticity in MS
Tizanidine
33
Direct acting sympathomimetic drug that is a selective beta-1 agonist
Dobutamine
34
Effect and use of dobutamine
More selective ionotropic and chronotropic effects --> used in HF to increase CO and SV without increasing HR
35
Direct acting sympathomimetic drugs that are selective beta-2 agonists
Terbutaline Albuterol Salmeterol
36
Uses of selective beta-2 agonists
Immediate relief of asthma Arrest uncomplicated premature labor (24-34 wks)
37
Adverse effects of beta-2 agonists
Tremors in hands Palpitations Hypokalemia
38
Direct acting sympathomimetic drug that is a selective beta-3 agonist
Mirabegron
39
Use of mirabegron
Overactive bladder --> urgency and frequency
40
Direct acting sympathomimetic drug that is a non-selective alpha-1 and alpha-2 agonist
Oxymetazoline
41
Direct acting sympathomimetic drug that is a non-selective beta agonist (1, 2, and 3)
Isoproterenol
42
Effects of isoproterenol
Significant increase: HR, CO Significant decrease: DBP, bronchial muscle Increase: SBP, blood flow, blood sugar Decrease: mean BP, intestinal muscle
43
Effects of adrenaline/epinephrine
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
44
Effects of norepinephrine
Significant increase: SBP, DBP, mean BP Increase: Coronary blood flow Decrease: HR, blood flow (skin, mucus membranes, kidney), intestinal muscle
45
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.
Epinephrine
46
Overall cardiac effect of epinephrine
Increase SBP
47
Overall vascular effect of epinephrine
Decrease DBP --> decrease TPR
48
Bronchial effects of epinephrine
Bronchodilation (beta-2) Decrease bronchial secretion (alpha-1)
49
GIT affects of epinephrine
Sphincter contraction (alpha-1) Gut relaxation (alpha-2 and beta)
50
Uses of epinephrine
Anaphylactic shock Prolong duration of local anesthetic agents Control epistaxis (rare) Cardiac resuscitation
51
Adverse effects of epinephrine
CVS --> angina, palpitation, arrhythmias CNS --> anxiety, tremors, HA, cerebral hemorrhage
52
Contraindications of epinephrine
HTN Angina Hyperthyroidism (receptor upregulation) MAO use
53
Direct acting sympathomimetic drug that is a non-selective alpha-1, alpha-2, and beta-1 agonist
Norepinephrine
54
Overall cardiovascular affect of norepinephrine
Increase in SBP and DBP
55
Uses of norepinephrine
Cardiogenic shock Hypotensive states --> surgical shock and MI
56
Reason that dopamine is preferred over norepinephrine for cardiogenic shock
Does not have risk of renal failure
57
Direct acting sympathomimetic drug that is a non-selective D1, D2, and beta-1 agonist
Dopamine
58
Dosing for dopaminergic effect of dopamine and the therapeutic effect
0.5-2 mcg/kg/min Increase urine output and renal blood flow
59
Dosing for beta-1 effect of dopamine and the therapeutic effect
2-10 mcg/kg/min Increase renal blood flow, CO, HR, and cardiac contractility
60
Dosing for alpha effect of dopamine and the therapeutic effect
>10 mcg/kg/min Increase BP and stimulate vasoconstriction
61
Risk with high dose of dopamine
Tachyarrhythmia
62
Uses of dopamine
Cardiogenic shock CCF, liver, and renal failure Hypotensive states --> after hypovolemia correction
63
Adverse effects of dopamine
N/V Tachycardia HTN Ectopic beats Arrhythmias
64
Hypotension that occurs when epinephrine is given after pretreatment with what?
Alpha blocker --> Dale's vasomotor reversal
65
Accentuated hypertensive effect that occurs when epinephrine is given after pretreatment with what?
Beta-blocker --> Dale's vasomotor reversal
66
Adrenoceptor acting drugs used as pressor agents
Norepinephrine Dopamine Ephedrine
67
Adrenoceptor acting drugs used as cardiac stimulants
Epinephrine Dobutamine
68
Adrenoceptor acting drugs used as bronchodilators
Albuterol Terbutaline Salmeterol
69
Adrenoceptor acting drugs used as nasal decongestants
Phenylephrine Oxymetazoline Pseudoephedrine
70
Adrenoceptor acting drugs used as CNS stimulants
Amphetamine Methamphetamine
71
Adrenoceptor acting drug that were used as anorectics
Fenfluramine (obsolete) Sibutramine (discontinued)
72
Adrenoceptor acting drugs used as uterine relaxants
Terbutaline Albuterol Mirabegron
73
Indirect-acting adrenoceptor agonists that work by releasing norepinephrine from vesicles
Amphetamine Tyramine
74
Indirect-acting adrenoceptor agonist that works by inhibiting uptake of norepinephrine from the synaptic cleft
Cocaine
75
Indirect-acting adrenoceptor agonist that works by inhibiting MAO
Selegiline
76
Indirect-acting adrenoceptor agonist that works by inhibiting COMT
Entacapone
77
Uses of amphetamine
Narcolepsy ADHD
78
Therapeutic effects of amphetamine
Wakefulness and alertness Decrease fatigue Improve physical performance Appetite suppression Improves task performance, but also increases errors
79
Contraindication of tyramine
Hypertensive crisis with MAO inhibitor
80
Foods that contain tyramine
Cheese Beef Wine Beer Yogurt Yeast
81
Adrenergic agonists that are non-selective for alpha receptors
Phenoxybenzamine Phentolamine
82
Irreversible nonselective antagonist of alpha-1 and alpha-2
Phenoxybenzamine
83
Therapeutic effects of phenoxybenzamine
Vasodilation Hypotension Reflex tachycardia
84
Uses of phenoxybenzamine
Pheochromocytoma Raynaud's syndrome Frostbite
85
Adverse effects of phenocybenzamine
Marked postural hypotension Inhibition of ejaculation Sedation
86
Competitive, reversible, non-selective agonist of alpha-1 and alpha-2
Phentolamine
87
Therapeutic effects of phentolamine
Vasodilation Hypotension Reflex tachycardia
88
Uses of phentolamine
Pheochromocytoma Peripheral vascular disease Hypertensive crisis
89
Selective alpha-1 antagonists
Prazosin Terazosin Doxazosin Alfuzosin Tamsulosin Silodosin
90
Therapeutic effects of prazosin
Peripheral vasodilation Phosphodiesterase inhibition --> vasodilates Improved urine outflow in BPH
91
Reason for lesser reflex tachycardia of prazosin compared to phentolamine and phenoxybenzamine
No alpha-2 blocking, no promotion of norepinephrine release
92
Uses of prazosin
Hypertension BPH Raynaud's --> rare, CCB prefered
93
Adverse effect of prazosin
Postural hypotension
94
Alpha-1A antagonists, specific for smooth muscles in bladder neck and urethra
Tamsulosin Silodosin
95
Adverse effects of tamsulosin and silodosin
Abnormal ejaculation Floppy iris syndrome
96
Selective alpha-2 agonist
Yohimbine
97
Uses of yohimbine
Generally unestablished Male sexual dysfunction Diabetic neuropathy
98
Non-selective beta antagonists
Propranolol Timolol Sotalol Pindolol
99
Cardiovascular effects of propranolol
Decrease HR, contractility, conduction, and CO --> reduced myocardial oxygen demand Decreased renin secretion Increased TPR
100
Respiratory effect of propranolol
Bronchoconstriction in asthma
101
Metabolic effects of propranolol
Increase LDL and triglyceride Decrease HDL Hypoglycemia masking in diabetics
102
CNS effects of propranolol
Sedation Lethargy Sleep disturbance Suppress performance anxiety
103
Miscellaneous effects of propranolol
Decrease formation of aqueous humor Reduce portal venous pressure in cirrhosis
104
Uses of propranolol
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
Contraindication of propranolol
Prinzmetal's angina
106
Adverse effects of propranolol
Bronchoconstriction Bradycardia Cold extremities Hypoglycemia Fatigue Sleep disturbance Rebound HTN Adverse lipid profile
107
Treatment of propranolol toxicity
Maintain ABCs IV fluid and atropine Glucagon
108
Non-selective beta blocker used as eye drop for open angle glaucoma
Timolol
109
Reason sotalol is also a class II anti-arrhythmic drug
Additional K blocking property
110
Selective beta-1 antagonists
Atenolol Esmolol Metoprolol
111
Advantages of selective beta-1 antagonists
Safer in asthma Safer in diabetics Safer in PVE Less effect on lipids
112
Prominent beta-1 and beta-2 antagonist with a lesser alpha-1 antagonistic effect
Carvedilol
113
Actions of carvedilol
Inhibits free radical induced lipid peroxidation Inhibits smooth muscle mitogenesis Blocks L-type voltage gated Ca channels
114
Uses of carvedilol
CHF HTN Angina
115
Selective alpha-1 and beta-1 antagonist with partial agonistic action on beta-2
Labetalol
116
Therapeutic effects of labetalol
Decrease BP Peripheral vasodilation Bronchodilation
117
Uses of labetalol
HTN in pregnancy Pheochromocytoma Rebound HTN from clonidine
118
Adverse effects of labetalol
Postural hypotension Hepatotoxicity
119

Cardiovascular II (29 decks)

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