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53 Cards in this Set

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  • Back
Name the 3 non-selective adrenergic antagonist which are highly selective competitve inhibitors of alpha-1 receptors.
Doxazosin, terazosin, and alfuzosin
Which drug is selective for alpha-1A receptor antagonist, (which is a subtype of alpha-1 adrenergic receptors)? What does this drug target?
Tamsulosin, which targetrs prostate alpha-1 receptors.
All alpha antagonist covered in the adrenergic antagonist section bind to alpha adrenergic receptors in a?
reversible and competitive manner
Where does adrenergic antagonist bind?
They bind mostly with postsynaptic receptors and inhibit them in a reversible and competitive manner.
When the adrenergic antagonist block the adrenergic receptors, what happens?
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)
All beta antagonist covered in the adrenergic antagonist section bind to beta adrenergic receptors in a?
reversible and competitive manner
Beta adrenergic antagonist are commonly referred to as?
Beta-blockers (nearly all drugs ending in "-olol)
What is sotalol used for?
Which drug is the prototypical beta adrenergic antagonist that all others are compared with?
Name 5 non-selective beta receptor antagonist.
Propranolol, nadolol, pindolol, sotalol, and timolol
Drugs that have a chemical substituent on the para position of the aromatic ring are selective for?
They are selective for Beta-1 receptors and have less binding affinity for beta-2 receptors.
Name 6 drugs which have a chemical substituent on the para position of the aromatic ring.
Acebutolol, atenolol, betaxolol, bisoprolol, esmolol, and metaprolol
Which drug is an ester that is rapidly inactivated by plasma esterases?
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?
Name 2 non-selective adrenergic antagonist and which receptors they act on?
Labetalol and Carvedilol are antagonists at beta-1, beta-2, and alpha-1 receptors.
What effects do non-selective alpha antagonist have on the cardivascular system?
They cause postural hypotension and tachycardia, but they have little effect on resting blood pressure.
Inhibition of peripheral alpha-1 receptors in the cardiovascular system by non-selective alpha antagonists leads to?
vasodilation of the vasculature, usually resulting in a baroreceptor-mediated increase in heart rate (reflex tachycardia)
Non-selective alpha antagonist in the cardiovascular system cause inhibition of presynaptic alpha-2 receptors in the CNS leads to?
Enhancement of norepinephrine release from the CNS.
What effect do alpha-1 adrenergic antagonist have on the cardiovascular system?
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.
What effects do non-selective beta-antagonist have on the cardiovascular system (beta-1 receptors)?
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.
What effects do non-selective beta-antagonist have on the cardiovascular system (beta-2 receptors)?
This leads to a slight initial increasee in peripheral resistance due to prevention od vasodilation by endogenous catecholamine activation of beta-2 receptors.
What effects do the non-selective adrenergic antagonist have on the cardiovascular system?
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.
What are common adverse effects of nonselective alpha adrenergic antagonist and alpha-1 adrenergic antagonist?
Postural Hypotension and reflex tachycardia
What effect does alpha adrenergic receptor antagonism have on the respiratory system?
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.
What effect does the non-selective beta adrenergic antagonist have on the respiratory system?
Beta-adrenergic antagonist block endogenous catecholamines from stimulating beta-2 receptors in the bronchial tissue.
What occurs in patients with asthma or COPD when they are taking a non-selective beta adrenergic antagonist?
An increase in airway resistance and secretions may result, causing an exacerbation of disease symptoms.
What effects do alpha-1 selective adrenergic antagonist have on the genitourinary tract?
decrease in resistance to urinary flow
What is the first drug to be marketed as an alpha-1A receptor antagonist?
What effects do beta-adrenergic antagonist have on the eye?
They decrease intraocular pressure by decreasing the production of aqueous humor.
What effects do beta-adrenergic antagonist have in the endrocrine system?
They partially inhibit glycogenolysis in the liver. Also, in the pancreas, insulin secretion is blocked.
TRUE/FALSE. Beta antagonist should be used with caution in diabetic patients?
TRUE. Particulary in patients with type-1 diabetes mellitus and those that are prone to hypoglycemic episodes.
What occurs in patients who chronically use beta-adrenergic antagonistic drugs?
Leads to increased plasma concentrationd of VLDL and decreased plasma concentrations of HDL. Both of these effects has a negative impact on cardiovascular health.
What effects do beta-adrenergic antagonist have on the CNS?
Beta antagonists with significatn lipid solubility may cross the blood brain barrier, resulting in various CNS effects such as CNS depression.
Name 1 beta-adrenergic antagonist with has the greatest lipid solubility which therefore may cause significant CNS effects, both desirable and undesirable.
Which type of adrenergic antagonist are used more frequently for the treatment of hypertension?
beta-adrenergic antagonist (propranolol and metoprolol)
Which 3 beta-adrenergic antagonists are used for cardiac arrhythmias?
propranolol,sotalol, and esmolol
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.
Which 2 beta-adrenergic antagonist and 1 nonselective adrenergic antagonist drugs are used in patients with congestive heart failure?
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.
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?
Carvedilol and Labetalol
Which alpha-1 adrenergic antagonist is useful for the management of benign prostatic hypertrophy?
What are 2 common adverse effects of nonselective alpha adrenergic antagonist and alpha-1 adenergic antagonists?
Postural Hypotension and relex tachycardia
What is a common adverse effect of alpha-1 adrenergic antagonists?
First-dose syncope, in which patients lose consciousness following the first dose of medication. (terazosin and doxazosin)
What is a common adverse effect for beta-adrenergic antagonists?
May induce CHF in patients with impaired cardiac function and may exacerbate symptoms in patients with preexisting CHF.
What common adverse effect does nonselective beta-antagonist have?
They may exacerbate the symptoms in patients with preexisting airway diseases, such as asthma or COPD.
What common adverse effects do beta-adrenergic antagonists cause?
They cause a number of CNS-related adverse effects, including depression, sleep disorders, nightmares, and fatigue.
What happens if antipsychotic medications and adrenergic receptor antagonists (especially alpha-adrenergic receptor antagonist) are administered together?
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.
Which drugs may oppose the hypotensive effects of beta adrenergic antagonists?
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).
What does the use of sotalol with potassium-depleting diuretics (furosemide) cause?
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.
Name 2 nonselective antagonist.
Carvedilol and Lebatalol
Name 3 Alpha-1 selective antagonist.
Doxazosin, Terazosin, Alfuzosin
Name 1 Alpha-1A antagonist
Name 5 Nonselective beta antagonist.
Nadolol, Pindolol, Propranolol, Sotalol, Timolol
Name 5 Beta-1 selective antagonist.
Atenolol, Betaxolol, Bisoprolol, Esmolol, metoprolol