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Pharmacology > Autonomics: Adrenergic Agonists and Antagonists > Flashcards

Autonomics: Adrenergic Agonists and Antagonists Flashcards

1
Q

Alpha 1

A

Gq Transmembrane - Phospholipase C to increase DAG and IP3 to increase intracellular calcium.
Contraction of vascular smooth muscle, contracts pupil muscle causing dilation, erects hair, contracts prostate, increases force of contraction on heart, increases glycogenolysis, decreases renin release.

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2
Q

Alpha 2

A

Gi - decrease adenylyl cyclase to decrease cAMP
multiple effects on CNS, causes platelet aggregation, inhibition of neurotransmitter release in presynaptic nerve terminals, contracture of vascular smooth muscle, inhibition of lipolysis in fat cells and decreased insulin secretion.

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3
Q

Beta 1

A

Gs Increase adenylyl cyclase to increase cAMP
HEART, increase HR at SA node, and conduction velocity at AV node, increase force of contracture, conduction velocity, cardiac output, increases renin release.

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4
Q

Beta 2

A

Gs Increase adenylyl cyclase to increase cAMP
Vasodilation of blood vessels, stimulated glycogenolysis in muscles to promote contractility (Tremor), bronchiodilation, increase in glucagon secretion, and relaxation of uterus

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5
Q

Beta 3

A

Gs Increase adenylyl cyclase to increase cAMP

activates lipolysis, relaxes detrusor muscle

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6
Q

Dopamine 1

A

Gs Increase adenylyl cyclase to increase cAMP

Vasodilation in renal, mesenteric and coronary vasculature, increases GFR, renal blood flow and Na secretion.

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7
Q

Norepinephrine (levophed)

A

alpha -1 alpha -1 beta -1 beta -3
Heart: increases pacemaker, conduction, force of contraction, decreases HR by vagal response.
Arteries: Vasoconstriction
Veins: venoconstriction

Decrease in HR, MPB slightly increased, net peripheral resistance increased. Used to maintain BP in shock and hypotension

Adverse: tissue necrosis and sloughing in extravasation. anxiety, hyperglycemia, arrhythmias, and cerebral hemorrhage.

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8
Q

Epinephrine

A

alphas and betas
Heart: increase pacemaker, conduction, force of contraction, and rate.
Arteries: vasoconstriction except in most arterial beds - vasodilation in skeletal muscle.
Lungs: bronchodilation, decongestion

HR increase, MBP remains unchanged, decrease in net peripheral resistance. Used for anaphylactic shock - bronchodilator, maintain heart, beta attenuates histamine release.

Adverse: restlessness, tremor, palpitations, cerebral hemorrhage, tachycardia, arrhythmias, hyperglycemia.

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9
Q

Isoproterenol

A

betas
Heart: increase pacemaker, conduction, force and rate of contraction.
Vasodilation in arteries, bronchodilation in lungs

HR increases, MBP decrease, Net resistance decreases. Used as bronchodilator and emergency stimulant.

Adverse: Palpitation, headache, flushed skin, tachycardia, cardiac ischemia and arrhythmias.

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10
Q

Dopamine

A

dopamine-1, beta-1, alpha-1
Effects highly dependent on dose used.
Increased heart output, blood pressure, improved renal and intestinal perfusion.

HR increases, MBP increase, net resistance decrease. Used for short term cardiovascular support. Used when BP in low and able to administer drug through IV. Used during congestive heart failure, and reserves the kidneys in periods of shock.

Adverse: tachycardia, excessive vasoconstriction, can produce ischemic necrosis and sloughing, headaches, nausea, vomiting.

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11
Q

Dobutamine

A

beta-1, beta-2 > alpha-1
Increases output and stroke volume without similar increase in rate of heart, no real change in vascular resistance.
Mild alpha-1 agonist (racemic mixture).

Used for short-treatment of cardiac decompensation.
Adverse: Blood pressure and heart rate increase during rapid infusion, hypertensive patients may experience exaggerated pressor response, arrhythmias, increase oxygen demand of tissues.

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12
Q

Beta -2 Selective

A

Active bronchodilators, delay premature labor (tocolysis), minimize beta-1 stimulation on heart, vasodilators.

Increase usefulness in treatment of asthma, bronchospasm, and emphysema.
Asthma: inhalation forms are preferred, oral routes accepted. Arterial oxygen tension may fall during treatment due to vasodilation of pulmonary beds.

Adverse: tremor, underlying increase risk of cardiovascular disease, tachycardia (adverse beta-1 stimulation).

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13
Q

Albuterol

A

Short-acting beta-2 selective

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14
Q

Ipratropium

A

Short-acting beta-2 selective

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15
Q

Levalbuterol

A

short-acting beta-2 selective

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16
Q

Metaproterenol

A

short-acting beta-2 selective

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17
Q

Arformoterol

A

long-acting beta-2 selective

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18
Q

Fromoterol

A

long-acting beta-2 selective

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19
Q

Indacaterol

A

long-acting beta-2 selective

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20
Q

Salmeterol

A

long-acting beta-2 selective

Not recommended for acute treatment of asthma due to slow onset

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21
Q

Terbutaline

A

long acting beta-2 selective

Subcutaneous or intravenous for emergency asthma attack.

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22
Q

Mirabegron

A

Beta-3 selective agent
Relaxes detrusor smooth muscle of urinary bladder to increase capacity. Orally active with 50hr half life (hepatic biotransformation).

Contraindications: Bladder or urinary obstruction, pregnancy or breast feeding, renal or hepatic dysfunction, MAO-inhibitor therapy, hypertension.

Adverse effects: hypertension, sinus tachycardia or heart, gastric distress, increased UTI, headache, increased risk of respiratory infections.

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23
Q

Oxymetazoline

A

Alpha-1 selective agent

Therapeutic: Nasal decongestant, mydriasis, maintenance of blood pressure through surgery (vasoconstriction)

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24
Q

Phenylephrine

A

Alpha-1 selective agent

Therapeutic: Nasal decongestant, mydriasis, maintenance of blood pressure through surgery (vasoconstriction)

25
Q

Clonidine

A 
Alpha-2 selective agent, transdermal patch
Antihypertensive actions (dominant) 
Lower brainstem alpha-2 stimulation centrally reduces sympathetic outflow, reducing BP, postural reflexes remain intact.

Adverse: Rebound effect may occur with abrupt discontinuation of drug. Dry mouth and sedation, sexual dysfunction, marked bradycardia, contact dermatitis.

26
Q

Guanabenz

A 
Alpha-2 selective agent
Antihypertensive actions (dominant) 
Lower brainstem alpha-2 stimulation centrally reduces sympathetic outflow, reducing BP, postural reflexes remain intact.

Adverse: Rebound effect may occur with abrupt discontinuation of drug. Dry mouth and sedation, sexual dysfunction, marked bradycardia, contact dermatitis.

27
Q

Guanfacine

A 
Alpha-2 selective agent
Antihypertensive actions (dominant) 
Lower brainstem alpha-2 stimulation centrally reduces sympathetic outflow, reducing BP, postural reflexes remain intact.

Adverse: Rebound effect may occur with abrupt discontinuation of drug. Dry mouth and sedation, sexual dysfunction, marked bradycardia, contact dermatitis.

28
Q

Alpha-methyldopa (methyldopa)

A 
Alpha-2 selective agent
Indirect mechanism of action - activity away from synapse. Substrate for catecholamine synthesis pathway (end product is alpha-methyl norepinephrine) 
Antihypertensive actions (dominant) 
Lower brainstem alpha-2 stimulation centrally reduces sympathetic outflow, reducing BP, postural reflexes remain intact.

Adverse: No rebound effect, slow onset of action. Dry mouth and sedation, sexual dysfunction, marked bradycardia, contact dermatitis, hemolytic anemia, parkinson’s like effect.

29
Q

Amphetamine

A

Mixed Action Agonists
Promote release, prevent termination of action (terminal uptake inhibition and biotransformation inhibition), direct receptor stimulation.
Adverse: Drug dependance and abuse potential; psychological disorders, pulmonary hypertension, CNS stimulation.

30
Q

Methamphetamine

A

Mixed Action Agonists
Tx: Obesity, narcolepsy, attention deficit disorder, nasal decongestant.
Adverse: Drug dependance and abuse potential; psychological disorders, pulmonary hypertension, CNS stimulation.

31
Q

Methylphenidate

A

Mixed Action Agonists
Tx: Obesity, narcolepsy, attention deficit disorder, nasal decongestant.
Adverse: Drug dependance and abuse potential; psychological disorders, pulmonary hypertension, CNS stimulation.

32
Q

Ephedrine

A

Mixed Action Agonists

Tx: Obesity, narcolepsy, attention deficit disorder, nasal decongestant.

33
Q

Tyramine

A

Mixed Action Agonists
Tx: Obesity, narcolepsy, attention deficit disorder, nasal decongestant.
Naturally formed in GI tract and quickly biotransformed. In the presence of monoamine oxidase inhibitors it can increase pressor. Chronic tyramine administration results in increased conversion to octopamine (blocks norepinephrine storage in vesicles leading to reduced pressor)

34
Q

Mixed Action Agonists

A

Indirect agonist, promote release, prevent termination of action (terminal uptake inhibition and biotransformation inhibition), direct receptor stimulation.

Peripheral - increase vascular resistance and BP, mild bronchodilation, cardiac stimulation and arrhythmias, decreased nasal congestion.
Central - Increased respiration, alertness/confidence, psychogenetic effects, appetite suppressant.

Tx: Obesity, narcolepsy, attention deficit disorder, nasal decongestant.
Adverse: Drug dependance and abuse potential; psychological disorders, pulmonary hypertension, CNS stimulation.

35
Q

Phenoxybenzamine

A

Non-selective alpha antagonist
Irreversible binding - long duration of action
Intravenous/oral route
Tx: benign prostatic hypertrophy, acute control of hypertension, treatment of hypertension related to phenochromocytoma

Cardiovascular: vasodilation, hypotension, tachycardia, venous pooling.
Anticholinergic
Antihistamine and anti-serotonin effects

Adverse: Severe postural hypotension (only beta left - relaxation), nasal stuffiness, marked tachycardia, anticholinergic effects, sexual dysfunction.

36
Q

Phentolamine

A

Non-selective alpha antagonist - intravenous
Reversible antagonist
Releases histamine from mast cells, cholinomimetic actions.
Tx: treatment of hypertension related to phenochromocytoma, clonidine withdrawal hypertension, reversal of local vasoconstriction, pulmonary hypertension in newborns.

Cardiovascular: reduced vascular resistance, venous pooling, marked hypotension and tachycardia. Stimulation of GI motility and acid secretion.

37
Q

Prazosin

A

Short acting selective alpha-1 antagonist
Reversible blocker
Tx: General treatment of hypertension and benign prostatic hypertrophy

38
Q

Terazosin

A

selective alpha-1 antagonist
Reversible blocker
Tx: General treatment of hypertension and benign prostatic hypertrophy

39
Q

Doxazosin

A

long acting selective alpha-1 antagonist
Reversible blocker
Tx: General treatment of hypertension and benign prostatic hypertrophy

Adverse: First dose effect, fluid retention, tachycardia, nasal stuffiness.

40
Q

Tamsulosin

A

selective alpha-1 antagonist
Reversible blocker
Tx: General treatment of hypertension and benign prostatic hypertrophy

Adverse: First dose effect, fluid retention, tachycardia, nasal stuffiness.

41
Q

Alfuzosin

A

Selective alpha-1 antagonist
Reversible blocker
Tx: General treatment of hypertension and benign prostatic hypertrophy

Adverse: First dose effect, fluid retention, tachycardia, nasal stuffiness.

42
Q

Selective Alpha-1 antagonists

A

Cardiovascular effects less than non-selective alpha blockers.
Reduced vascular resistance, lower incidence of postural hypotension (veins less sensitive/first dose still a problem), lower incidence of tachycardia

Adverse: First dose effect, fluid retention, tachycardia, nasal stuffiness.

43
Q

3 Generations of Beta Blockers

A

Classical non-selective beta blockers – 1st generation

Beta1-selective beta blockers – 2nd generation

Non-selective beta blockers with additional actions
& Beta1-selective beta blockers with additional actions – 3rd generation

44
Q

Nadolol

A

Classical non-selective beta blockers – 1st generation
Tx: Hypertension, angina (chronic/stable), arrhythmias, heart failure, hyperthyroidism, glaucoma, tremor (essential), migraine prophylaxis

Must be used with care for patients with asthma, diabetes (mask the tremor, racing of heart and sweating – important signs of hypoglycemia), or peripheral artery disease (make the issue worse)

Adverse: withdrawal with abrupt stoppage of drug, acute heart failure and conduction problems, bradycardia, bronchospasm, peripheral vascular disease, hypersensitivity.

45
Q

Penbutolol

A

Classical non-selective beta blockers – 1st generation

Tx:Hypertension, angina (chronic/stable), arrhythmias, heart failure, hyperthyroidism, glaucoma, tremor (essential), migraine prophylaxis

Must be used with care for patients with asthma, diabetes (mask the tremor, racing of heart and sweating – important signs of hypoglycemia), or peripheral artery disease (make the issue worse)

Adverse: withdrawal with abrupt stoppage of drug, acute heart failure and conduction problems, bradycardia, bronchospasm, peripheral vascular disease, hypersensitivity.

46
Q

Pindolol

A

Classical non-selective beta blockers – 1st generation (beta blocker with Intrinsic sympathomimetic activity)
Tx: Use in patients with a low resting heart rate. Hypertension, angina (chronic/stable), arrhythmias, heart failure, hyperthyroidism, glaucoma, tremor (essential), migraine prophylaxis

Must be used with care for patients with asthma, diabetes (mask the tremor, racing of heart and sweating – important signs of hypoglycemia), or peripheral artery disease (make the issue worse)

Adverse: withdrawal with abrupt stoppage of drug, acute heart failure and conduction problems, bradycardia, bronchospasm, peripheral vascular disease, hypersensitivity.

47
Q

Propranolol

A

Classical non-selective beta blockers – 1st generation
Tx: Hypertension, angina (chronic/stable), arrhythmias, heart failure, hyperthyroidism, glaucoma, tremor (essential), migraine prophylaxis

Must be used with care for patients with asthma, diabetes (mask the tremor, racing of heart and sweating – important signs of hypoglycemia), or peripheral artery disease (make the issue worse)

Adverse: withdrawal with abrupt stoppage of drug, acute heart failure and conduction problems, bradycardia, bronchospasm, peripheral vascular disease, hypersensitivity.

48
Q

Timolol

A

Classical non-selective beta blockers – 1st generation
Tx: Hypertension, angina (chronic/stable), arrhythmias, heart failure, hyperthyroidism, glaucoma, tremor (essential), migraine prophylaxis

Must be used with care for patients with asthma, diabetes (mask the tremor, racing of heart and sweating – important signs of hypoglycemia), or peripheral artery disease (make the issue worse)

Adverse: withdrawal with abrupt stoppage of drug, acute heart failure and conduction problems, bradycardia, bronchospasm, peripheral vascular disease, hypersensitivity.

49
Q

Acebutolol

A

Beta1-selective beta blockers – 2nd generation
(beta blocker with Intrinsic sympathomimetic activity)
Tx: Use in patients with a low resting heart rate. Hypertension, angina (chronic/stable), arrhythmias, heart failure, hyperthyroidism, glaucoma, tremor (essential), migraine prophylaxis

50
Q

Atenolol

A

Beta1-selective beta blockers – 2nd generation
Tx: Hypertension, angina (chronic/stable), arrhythmias, heart failure, hyperthyroidism, glaucoma, tremor (essential), migraine prophylaxis

51
Q

Bisoprolol

A

Beta1-selective beta blockers – 2nd generation
Tx: Hypertension, angina (chronic/stable), arrhythmias, heart failure, hyperthyroidism, glaucoma, tremor (essential), migraine prophylaxis

52
Q

Esmolol

A

Beta1-selective beta blockers – 2nd generation
Tx: Hypertension, angina (chronic/stable), arrhythmias, heart failure, hyperthyroidism, glaucoma, tremor (essential), migraine prophylaxis

53
Q

Metoprolol

A

Beta1-selective beta blockers – 2nd generation
Tx: Hypertension, angina (chronic/stable), arrhythmias, heart failure, hyperthyroidism, glaucoma, tremor (essential), migraine prophylaxis

54
Q

Carvedilol

A

Non-selective beta blockers with additional actions – 3rd generation
Indication: hypertension, congestive heart failure (stable, cardiovascular event prevention)

also alpha-1 blockers (primary) and membrane stabilizing (secondary effect through mainly calcium entry blockade) -These would be a good drug of choice for treating amphetamine (sympathetic activation) hypertension. Because they block both alpha and beta.

55
Q

Labetalol

A

Non-selective beta blockers with additional actions – 3rd generation

Primary Indications are hypertension and hypertensive emergency

also alpha-1 blockers (primary) and membrane stabilizing (secondary effect through mainly calcium entry blockade) -These would be a good drug of choice for treating amphetamine (sympathetic activation) hypertension. Because they block both alpha and beta.

56
Q

Betaxolol

A

Beta1-selective beta blockers with additional actions – 3rd generation
Indication for hypertension, also membrane stabilizing through calcium entry blockade

57
Q

Celiprolol

A

Beta1-selective beta blockers with additional actions – 3rd generation

58
Q

Nebivolol

A

Beta1-selective beta blockers with additional actions – 3rd generation
Bystolic, primary indication is for hypertension. Also provides vascular relaxation by enhanced nitric oxide production.

59
Q

Beta-1 antagonists

A

Selectivity lost at high doses
Tx: Hypertension, angina (chronic/stable), arrhythmias, heart failure, hyperthyroidism, glaucoma, tremor (essential), migraine prophylaxis

Must be used with care for patients with asthma, diabetes (mask the tremor, racing of heart and sweating – important signs of hypoglycemia), or peripheral artery disease (make the issue worse)

Adverse: withdrawal with abrupt stoppage of drug, acute heart failure and conduction problems, bradycardia, bronchospasm, peripheral vascular disease, hypersensitivity, sexual dysfunction

Pharmacology (7 decks)

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