Chapter 10 (SAS 1) Flashcards by Liahona Velecio Que | Brainscape

Q

What are the endogenous catecholamines?

A

Norepinephrine, Epinephrine, and Dopamine

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Q

Binds to a1, a2, and b1 receptors

A

Norepinephrine

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Q

Binds to a and b receptors

A

Epinephrine

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Q

Binds to the alpha-1. alpha-2, beta-1 receptors and also dopamine receptors

A

Dopamine

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Q

Locations comprising alpha 1

A

Smooth muscles:
Vascular smooth muscles
Prostatic smooth muscles
Pupillary dilator muscles
Pilomotor smooth muscles

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Q

Response of a1: Vascular smooth muscles

A

Vasoconstriction

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Q

Response of a1: Prostatic smooth muscles

A

Contraction

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Q

Response of a1: Pupillary dilator muscle

A

Contraction

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Q

Response of a1: Pilomotor smooth muscles

A

Contraction

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Q

Locations comprising alpha-2

A

Presynaptic CNS and Postsynaptic

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Q

Response of a2: Presynaptic CNS

A

Inhibits release of NE
Consequence:
Central - Sedation and Depression
Peripheral - Vasodilation

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Q

Response of a2: Postsynaptic

A

Vasoconstriction

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Q

Location comprising b2

A

Smooth Muscle (Bronchial smooth muscle, Uterine smooth muscle, Vascular smooth muscle supplying skeletal muscles)
Skeletal Muscle
Liver

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Q

Locations comprising b3

A

Adipose tissues

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Q

Response of b2: Bronchial smooth muscle

A

Bronchodilation

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Q

Response of b2: Uterine smooth muscle

A

Relaxation (tocolysis)

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Q

Locations comprising b1

A

Heart and Juxtaglomerular cells

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Q

Locations comprising b1

A

Heart and Juxtaglomerular cells

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Q

Locations comprising b1

A

Heart and Juxtaglomerular cells

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Q

Locations comprising b1

A

Heart and Juxtaglomerular cells

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Q

Locations comprising b1

A

Heart and Juxtaglomerular cells

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Q

Response of b1: Heart

A

Increases cardiac output (positive chronotropic effect), Increases impulse conduction (positive dromotropic effect), and increases contraction (positive inotropic effect)

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Q

Response of b1: Juxtaglomerular cells

A

Increase renin release

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Q

Response of b2: Bronchial smooth muscle

A

Bronchodilation

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Q

Response of b1: Uterine smooth muscle

A

Relaxation

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Q

Response of b1: Vascular smooth muscle that supplies the skeletal system

A

Vasodilation

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Q

Response of b1: Skeletal muscle

A

Muscle contraction and Promotes potassium uptake

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Q

Response of b1: Liver

A

Activates glycogenolysis and gluconeogenesis

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Q

Response of b2: adipose tissue

A

Lipolysis

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Q

Nonselective a antagonist is used in the treatment of

A

Pheochromocytoma

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Q

What is pheochromocytoma?

A

a tumor that secretes catecholamines

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Q

Selective a1 antagonists is used in?

A

Hypertension and benign prostatic hyperplasia

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Q

Beta-receptor antagonists drugs are for?

A

Hypertension, ischemic heart disease, arrhythmias, glaucoma, and endocrinological and neurological disorders

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Q

Alpha receptor may be ____ or ____ in their mechanism of action

A

Reversible or irreversible

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Q

Reversible antagonists

A

Dissociate from the receptors wherein the block can be surmounted with sufficiently high amount of agonists

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Q

Examples of reversible antagonists

A

Phentolamine and prazosin

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Q

Irreversible antagonists

A

Do not dissociate and cannot be surmounted

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Q

Example of an irreversible antagonists

A

Phenoxybenzamine (it covalently binds to the receptors)

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Q

Cardiovascular effects of alpha receptor antagonists

A

Causes a decrease in blood pressure

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Q

Drug of choice for pheochromocytoma

A

Phenoxybenzamine

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Q

Drug of choice for the management of Raynaud’s syndrome

A

Phentolamine and Tolazoline

Q

Selective a1 antagonists

A

Prazosin, Doxazosin, Terazosin, Alfuzosin, Tamsulosin

Q

Explain orthostatic hypertension

A

It is the lowering of blood pressure that happens when you stand up from lying or sitting down

Q

Other name for orthostatic hypertension

A

Postural hypertension

Q

What receptor are expressed in the base of the bladder and the prostate?

A

Alpha1 receptor

Q

Blockade of alpha1 receptor results to?

A

Decreased flow of urine

Q

Using alpha1 receptor antagonists in the bladder or in the prostate results to?

A

treat urinary retention due to prostatic hyperplasia

Q

Inhibits reuptake of released norepinephrine

A

Phenoxybenzamine

Q

Adverse effects of phenoxybenzamine

A

Orthostatic hypotension, tachycardia, nasal stuffiness, inhibition of ejaculation, fatigue, sedation, and nausea

Q

Potent competitive antagonist at both a1 and a2 receptors

A

Phentolamine

Q

Reduces peripheral resistance through blockade of a1 receptors

A

Phentolamine

Q

Effective in the management of hypertension; highly selective for a1 receptors; relaxes both peripheral and vascular smooth muscle as well as the smooth muscles in the prostate

A

Prazosin

Q

Another reversible a1-selective antagonist used in the treatment for hypertension; approved for use of men with BPH; has high bioavailability but is extensively metabolized; only a small fraction of unchanged drug is excreted in the urine

A

Terazosin

Q

Also used for hypertension and BPH; differs in such a way that it has a long half-life; moderate bioavailability, and very little parent drug is excreted in the urine

A

Doxazosin

Q

Competitive a1 antagonist; has a high affinity for a1A and a1D receptors; greater potency in inhibiting contraction in the prostate muscle

A

Tamsulosin

Q

a1 selective quinazoline derivative that is approved for BPH; increased risk of QT prolongation in susceptible individuals

A

Alfuzosin

Q

Resembles tamsulosin in blocking the a1A receptor and is used for BPH

A

Silodosin

Q

Another a1 selective antagonist that has efficacy as antihypertensive

A

Indoramin

Q

a1 antagonist that has a weak a2 agonist, and is also used in Europe for hypertension and BPH

A

Urapidil

Q

both a1 selective and beta antagonist

A

Carvedilol and Labetalol

Q

neuroleptic drugs; potent dopamine receptors but are also antagonists at a receptors

A

Chlorpromazine and haloperidol

Q

antidepressant and has the capacity to block a1 receptors

A

Trazodone

Q

ergot derivatives that causes a reversible alpha receptor blockade via a partial agonist action

A

Ergotamine and Dihydroergotamine

Q

a2 selective antagonist and is used in the treatment of orthostatic hypotension because it inhibits the release of norepinephrine through its blockade; once widely used for erectile dysfunction; and reverses the hypertensive effect caused by a2-adrenoceptor agonists

A

Yohimbine

Q

A tumor of the adrenal medulla or sympathetic ganglion cells

A

Pheochromocytoma

Q

Are most useful in the preoperative management of pheochromocytoma

A

Alpha-receptor antagonists

Q

a-adrenoceptor drugs have limited application in the management of hypertensive emergencies, but _____ has been used in this setting

A

Labetalol

Q

Individuals with Raynaud’s syndrome or excessive reversible vasopasm in the peripheral circulation do benefit from prazosin and phenoxybenzamine. However, _____ are preferable for most patients

A

Calcium channel blockers

Q

Mechanism of action in improving urine flow

A

Partial reversal of smooth muscle contraction in the enlarged prostate and the bladder base

Q

Has relatively little clinical usefulness and prescription drugs with this mechanisms are no longer available although the bark of yohimbine is used for erectile dysfunction (though the effectiveness is questionable)

A

Alpha2 receptor antagonist

Q

What do beta-receptors antagonists have in common?

A

Antagonizing the effects of catecholamines

Q

Differentiate pure antagonist, partial agonists, and inverse agonists

A

Pure antagonist is the occupancy of the b-receptor but causes no activation of the receptor. Partial agonist causes partial activation of the receptor. Inverse agonists stabilize the conformation of beta receptors reducing the proportion of active receptors.

Q

The beta receptor antagonists differs in their ______ for b1 and b2 receptors.

A

Relative affinities

Q

None of the clinically available beta receptors are B1-selective. Thus, the selectivity is ______, as it tends to diminish at higher drug concentration.

A

Dose-related

Q

Most of the drugs in this class are well-absorbed after oral administration where peak concentrations occur after 1-3 hours of ingestion

A

Beta-receptor antagonists

Q

What beta blocker undergoes extensive hepatic metabolism and its bioavailability is relatively low

A

Propranolol

Q

____ and ___ are quite lipophilic and readily cross the BBB

A

Propranolol and Penbutolol

Q

Major exception in beta-receptor antagonists with a half-life of approximately 10 minutes.

A

Esmolol

Q

Excreted unchanged in the urine and has the longest half-life of any available beta-receptor antagonists

A

Nadolol

Q

Effects of beta-receptor antagonist on the CV system

A

Lower blood pressure, do not cause hypotension in healthy individuals, and have prominent effects in the heart especially in the treatment of angina and chronic heart failure

Q

What should the patient if she has asthma and needs to take a beta-receptor antagonist to treat her heart condition?

A

Beta-1 receptor antagonist

Q

The mechanism of beta-receptor antagonists in reducing intraocular pressure in the eye especially in glaucoma

A

Decreasing aqueous humor

Q

Coronary artery disease is less likely to occur if the beta blockers are ____.

A

Partial agonists

Q

Local anesthetic action is also known as

A

Membrane-stabilizing action

Q

Prominent effect of several B-blockers

A

Local anesthetic action

Q

Membrane-stabilizing B blockers are not used topically in the ____.

A

Eye

Q

Nonselective b-blocker that lacks local action but has marked class III antiarrhythmic effect

A

Sotalol

Q

Prototypical B-blocking drug

A

Propranolol

Q

Safer in patients who experience bronchoconstriction in response to propranolol

A

Metoprolol, Atenolol

Q

may be preferable to patient with diabetes and peripheral vascular disease when therapy with B-blocker is required

A

Beta-1 selective antagonist

Q

is a beta-1 selective antagonist with modest capacity to activate b2 receptors

A

Celiprolol

Q

Ultra-short-acting b1 selective adrenoceptor antagonist that is useful in controlling supraventricular arrhythmias and etc.

A

Esmolol

Q

Partial B agonist activity and is less likely to cause bradycardia and abnormalities in plasma lipids

A

Pindolol, Acebutolol, Penbutolol,
Carteolol, Oxprenolol, and Celiprolol

Q

Most highly selective b1-blocker by promoting endothelial nitric oxide production

A

Nebivolol

Q

Is a reversible adrenoceptor blocker that is available as a racemic mixture of two pairs of chiral isomers

A

Labetalol

Q

In labetalol, the S,R isomer si _____

A

Potent a blocker

Q

In labetalol, the R,R, isomer is ___

A

Potent b blocker

Q

Nonselective B-blockers with the capacity to block a1-adrenergic receptors

A

Carvedilol, Medroxalol, Bucindolol

Q

Nonselective B-blocker without local therapeutic activity which is advantageous when treating glaucoma topically

A

Timolol

Q

A beta-blocker that is noteworthy because of its very long duration of action

A

Nadolol

Q

____ and ___ are also used for topical ophthalmic application in glaucoma

A

Levobunolol and Betaxolol

Q

Selective b2-blocking drug used in research

A

Butoxamine