Adrenergic Antagonists

Front 1

Name the 3 non-selective adrenergic antagonist which are highly selective competitve inhibitors of alpha-1 receptors.

Back 1

Doxazosin, terazosin, and alfuzosin

Front 2

Which drug is selective for alpha-1A receptor antagonist, (which is a subtype of alpha-1 adrenergic receptors)? What does this drug target?

Back 2

Tamsulosin, which targetrs prostate alpha-1 receptors.

Front 3

All alpha antagonist covered in the adrenergic antagonist section bind to alpha adrenergic receptors in a?

Back 3

reversible and competitive manner

Front 4

Where does adrenergic antagonist bind?

Back 4

They bind mostly with postsynaptic receptors and inhibit them in a reversible and competitive manner.

Front 5

When the adrenergic antagonist block the adrenergic receptors, what happens?

Back 5

1. Blockade of adrenergic receptors prevents binding and activation of these receptors by endogenous catecholamines.
2. Blockade of adrenergic receptors will usually reverse the effects of drugs that are adrenergic agonists (sympathomimetics)

Front 6

All beta antagonist covered in the adrenergic antagonist section bind to beta adrenergic receptors in a?

Back 6

reversible and competitive manner

Front 7

Beta adrenergic antagonist are commonly referred to as?

Back 7

Beta-blockers (nearly all drugs ending in "-olol)

Front 8

What is sotalol used for?

Back 8

arrhythmias

Front 9

Which drug is the prototypical beta adrenergic antagonist that all others are compared with?

Back 9

Propranolol

Front 10

Name 5 non-selective beta receptor antagonist.

Back 10

Propranolol, nadolol, pindolol, sotalol, and timolol

Front 11

Drugs that have a chemical substituent on the para position of the aromatic ring are selective for?

Back 11

They are selective for Beta-1 receptors and have less binding affinity for beta-2 receptors.

Front 12

Name 6 drugs which have a chemical substituent on the para position of the aromatic ring.

Back 12

Acebutolol, atenolol, betaxolol, bisoprolol, esmolol, and metaprolol

Front 13

Which drug is an ester that is rapidly inactivated by plasma esterases?

Back 13

Esmolol

Front 14

Which drug is a short-acting beta-1 selective antagonist and can be used as an rapid "on-off" type drug for the control of life-threatening hypertension?

Back 14

Esmolol

Front 15

Name 2 non-selective adrenergic antagonist and which receptors they act on?

Back 15

Labetalol and Carvedilol are antagonists at beta-1, beta-2, and alpha-1 receptors.

Front 16

What effects do non-selective alpha antagonist have on the cardivascular system?

Back 16

They cause postural hypotension and tachycardia, but they have little effect on resting blood pressure.

Front 17

Inhibition of peripheral alpha-1 receptors in the cardiovascular system by non-selective alpha antagonists leads to?

Back 17

vasodilation of the vasculature, usually resulting in a baroreceptor-mediated increase in heart rate (reflex tachycardia)

Front 18

Non-selective alpha antagonist in the cardiovascular system cause inhibition of presynaptic alpha-2 receptors in the CNS leads to?

Back 18

Enhancement of norepinephrine release from the CNS.

Front 19

What effect do alpha-1 adrenergic antagonist have on the cardiovascular system?

Back 19

1. They have a potent vasodilation effect on peripheral vascular tissue, resulting in a reduction of blood pressure.
2. They also cause "epinephrine reversal". When given concurrently with epinephrine, a non-selective adrenergic agonist, they block alpha-1 receptors, freeing epinephrine to have unopposed beta-2 agonist effects in the peripheral vasculature. This results in the conversion of the effect of epinephrine as a vasopressor to a vaso-depressor agent.

Front 20

What effects do non-selective beta-antagonist have on the cardiovascular system (beta-1 receptors)?

Back 20

Decrease heart rate (negative chronotrophic effect) and force of contraction (negative inotropic effect), slow AV node conduction, and increase the PR interval by antagonism of beta-1 receptors in cardiac tissue resulting in a chronic reduction of blood pressure in patients who have hypertension. Also, they block the release of renin caused by the sympathetic nervous system.

Front 21

What effects do non-selective beta-antagonist have on the cardiovascular system (beta-2 receptors)?

Back 21

This leads to a slight initial increasee in peripheral resistance due to prevention od vasodilation by endogenous catecholamine activation of beta-2 receptors.

Front 22

What effects do the non-selective adrenergic antagonist have on the cardiovascular system?

Back 22

They produce vasodilation and decrease blood pressure, but generally without reflex tachycardia that usually accompanies alpha blockade. The lack of reflex tachycardia may be explaining by the fact that they also simultaneously block beta-1 receptors in the heart.

Front 23

What are common adverse effects of nonselective alpha adrenergic antagonist and alpha-1 adrenergic antagonist?

Back 23

Postural Hypotension and reflex tachycardia

Front 24

What effect does alpha adrenergic receptor antagonism have on the respiratory system?

Back 24

May cause vasodilation in the upper respiratory tract due to blockade of stimulation of alpha-1 receptors by endogenous catecholamines. As a result, drugs with alpha-1 receptor blocking properties may cause nasal stuffiness and congestion.

Front 25

What effect does the non-selective beta adrenergic antagonist have on the respiratory system?

Back 25

Beta-adrenergic antagonist block endogenous catecholamines from stimulating beta-2 receptors in the bronchial tissue.

Front 26

What occurs in patients with asthma or COPD when they are taking a non-selective beta adrenergic antagonist?

Back 26

An increase in airway resistance and secretions may result, causing an exacerbation of disease symptoms.

Front 27

What effects do alpha-1 selective adrenergic antagonist have on the genitourinary tract?

Back 27

decrease in resistance to urinary flow

Front 28

What is the first drug to be marketed as an alpha-1A receptor antagonist?

Back 28

Tamsulosin

Front 29

What effects do beta-adrenergic antagonist have on the eye?

Back 29

They decrease intraocular pressure by decreasing the production of aqueous humor.

Front 30

What effects do beta-adrenergic antagonist have in the endrocrine system?

Back 30

They partially inhibit glycogenolysis in the liver. Also, in the pancreas, insulin secretion is blocked.

Front 31

TRUE/FALSE. Beta antagonist should be used with caution in diabetic patients?

Back 31

TRUE. Particulary in patients with type-1 diabetes mellitus and those that are prone to hypoglycemic episodes.

Front 32

What occurs in patients who chronically use beta-adrenergic antagonistic drugs?

Back 32

Leads to increased plasma concentrationd of VLDL and decreased plasma concentrations of HDL. Both of these effects has a negative impact on cardiovascular health.

Front 33

What effects do beta-adrenergic antagonist have on the CNS?

Back 33

Beta antagonists with significatn lipid solubility may cross the blood brain barrier, resulting in various CNS effects such as CNS depression.

Front 34

Name 1 beta-adrenergic antagonist with has the greatest lipid solubility which therefore may cause significant CNS effects, both desirable and undesirable.

Back 34

Propranolol

Front 35

Which type of adrenergic antagonist are used more frequently for the treatment of hypertension?

Back 35

beta-adrenergic antagonist (propranolol and metoprolol)

Front 36

Which 3 beta-adrenergic antagonists are used for cardiac arrhythmias?

Back 36

propranolol,sotalol, and esmolol

Front 37

Esmolol

Back 37

Useful as a very short-acting intravenous antihypertensive agent for certain cardiac conditions such as controlling the heart rate in supraventricular tachycardias. It is given as a continuous IV infusion to allow for careful control of pharmacodynamic effect.

Front 38

Which 2 beta-adrenergic antagonist and 1 nonselective adrenergic antagonist drugs are used in patients with congestive heart failure?

Back 38

2 beta-adrenergic antagonist: Bisoprolol and metoprolol
1 nonselective adrenergic antagonist: carvedilol. The selected beta-adrenergic antagonist are useful for decreasing mortality in patients with CHF.

Front 39

Which 2 nonselective adrenergic antagonist with both alpha-1 and beta antagonist properties are useful for the management of several cardiovascular disorders such as hypertension and congestive heart failure?

Back 39

Carvedilol and Labetalol

Front 40

Which alpha-1 adrenergic antagonist is useful for the management of benign prostatic hypertrophy?

Back 40

Terazosin

Front 41

What are 2 common adverse effects of nonselective alpha adrenergic antagonist and alpha-1 adenergic antagonists?

Back 41

Postural Hypotension and relex tachycardia

Front 42

What is a common adverse effect of alpha-1 adrenergic antagonists?

Back 42

First-dose syncope, in which patients lose consciousness following the first dose of medication. (terazosin and doxazosin)

Front 43

What is a common adverse effect for beta-adrenergic antagonists?

Back 43

May induce CHF in patients with impaired cardiac function and may exacerbate symptoms in patients with preexisting CHF.

Front 44

What common adverse effect does nonselective beta-antagonist have?

Back 44

They may exacerbate the symptoms in patients with preexisting airway diseases, such as asthma or COPD.

Front 45

What common adverse effects do beta-adrenergic antagonists cause?

Back 45

They cause a number of CNS-related adverse effects, including depression, sleep disorders, nightmares, and fatigue.

Front 46

What happens if antipsychotic medications and adrenergic receptor antagonists (especially alpha-adrenergic receptor antagonist) are administered together?

Back 46

Several conventional antipsychotic medications, particularily the high-dose phenothiazines (chlorpromazine) and certain atypical antipsychotic agents (clozapine) may cause postural hypotension due to alpha adrenergic receptor blockade. This effects may be increased if these antipsychotics are administered with an adrenergic receptor antagonists.

Front 47

Which drugs may oppose the hypotensive effects of beta adrenergic antagonists?

Back 47

Indomethacin and other NSAIDs. This maybe due to NSAID inhibition of prostaglandin A and prostaglandin E from the renal medulla (these two prostaglandins have potent vasodilatory effects).

Front 48

What does the use of sotalol with potassium-depleting diuretics (furosemide) cause?

Back 48

Torsades de pointes, a life-threatening ventricular arrythmia. This is a direct result of the antiarrthymia effect of sotalol being amplified due to a rapid fall in potassium levels.

Front 49

Name 2 nonselective antagonist.

Back 49

Carvedilol and Lebatalol

Front 50

Name 3 Alpha-1 selective antagonist.

Back 50

Doxazosin, Terazosin, Alfuzosin

Front 51

Name 1 Alpha-1A antagonist

Back 51

Tamsulosin

Front 52

Name 5 Nonselective beta antagonist.

Back 52

Nadolol, Pindolol, Propranolol, Sotalol, Timolol

Front 53

Name 5 Beta-1 selective antagonist.

Back 53

Atenolol, Betaxolol, Bisoprolol, Esmolol, metoprolol