Adrenergic Drugs Flashcards by Walker Short

What neurotransmitters are catecholamines?

Dopamine
Norepinephrine
Epinephrine

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What are drugs that are directly acting adrenergic drugs?

-they are drugs/neurotransmitters that produce responses by interacting with the adrenoreceptors on target cells (alpha or beta)

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What are drugs that indirectly acting adrenergic drugs?

-Drugs that cause the release of norepinephrine

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What kind of receptors are adrenergic receptors?

-G protein coupled receptors

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What adrenergic receptors does Isoproterenol work on?

-B 1, 2, & 3

**only Beta receptors

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Does dopamine act on adrenergic receptors?

Yes, only at high concentrations
B1 first, then a1
not B2

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What happens as the group on the amine of a catecholamine gets larger?

That catecholamine has a higher affinity for beta receptors and a lower affinity for alpha receptors

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Local anesthetics contain epinephrine.
What receptors are the target?
Why include epinephrine?

-alpha 1 receptors

to achieve local vasoconstriction, which keeps the anesthetic locally for a longer duration

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What vascular receptors does epinephrine activate at low vs high doses?

Low dose:
-B2 receptors = vasodilation

High dose:
-a1 receptors = vasoconstriction

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What is the effect of Isoproterenol on mean arterial pressure? Why?

-decrease slightly

Because it will stimulate B receptors in heart which will strongly increase cardiac force and rate = slightly increased systolic pressure
however, lots of vasodilation, causing diastolic pressure to drop a lot, so MAP will drop a bit

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A patient upon arrival at Ben Taub emergency room with very high blood pressure 220 / 160. He was treated with clonidine.
Clonidine is an emergency anti-hypertensive.

What is the effect of clonidine (alpha-2 agonist) on release of norepinephrine from
adrenergic nerve terminals?

A. Increase

B. Decrease

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Describe adrenergic presynaptic autoreceptors.

Mostly a2

- NE release will stimulate post synaptic cell, but also activate a2 autoreceptor, thus decreasing vesicular release

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What receptors does norepinephrine work on?

B1 & alphas

**NOT B2

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What receptors does epinephrine work on?

All alpha and beta receptors

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List Isoproterenol, Norepinephrine, and epinephrine in order of increasing size of their amine group.

Norepinephrine –> Epinephrine –> Isoproterenol

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What is the effect of epinephrine on the immune system?

A. Up regulates immune system
B. Down regulates immune system

B. Down regulates immune system

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Cardiovascular effects of dopamine are due to:

1) agonist at dopamine receptors
2) releasing more NE from nerve terminals
3) agonist at B1 and a1 receptors (at higher conc.)

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What is the cardiovascular effect of low dose dopamine?

Vasodilation in renal, mesenteric, coronary, and cerebral vascular beds

**only acting on D1 receptors

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What are the uses of high doses of dopamine?

preserve renal blood flow
protect vital organs
treat cardiogenic shock
Increased force of heart contraction

**acts on D1, B1, and a1 receptors

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Why is it good that moderate doses of dopamine will increase heart contractility much more than heart rate?

-oxygen demand on the heart does not increase significantly

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Where is epinephrine made?

Adrenal medulla

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Which receptor does Phenylephrine act on? Is it an agonist or antagonist?

a1 agonist

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Which receptor does Clonidine act on? Is it an agonist or antagonist?

a2 agonist

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Which receptor does Dobutamine act on? Is it an agonist or antagonist?

B1 agonist

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Which receptor does albuterol act on? Is it an agonist or antagonist?

B2 agonist *fast acting

Which receptor does salmeterol act on? Is it an agonist or antagonist?

B2 agonist *long acting

Which receptor does Ritodrine act on? Is it an agonist or antagonist?

B2 agonist

You have a trauma patient and your goal is to improve blood flow to kidneys with out increasing work load on the heart. Best drug (via IV drip) will be: ``` A. Albuterol (b2 agonist) B. Low dose Dopamine (Intropin) C. Epinephrine (Adrenalin) D. Dobutamine (b1 agonist) E. Norepinephrine (Levophed) ```

B. Low dose Dopamine (Intropin)

When is Phenylephrine used?

- during surgery to raise BP - Nasal decongestant (a1 agonist)

When is clonidine used?

- reduces sympathetic outflow from CNS - emergency antihypertensive, used in emergency only (a2 agonist)

What is a-methyldopa used for?

- anti-hypertensive in pregnant women - prodrug (a2 agonist)

What is priapism and what is its treatment?

- medical condition in which the erect penis does not return to its flaccid state - inject cavernosum with Phenylephrine (a1 agonist)

When is Dobutamine used?

-cardiogenic and septic shock to increase cardiac output | B1 specific agonist

When is Ritodrine used?

-relaxes uterus, prevents premature deliveries | B2 selective agonist

Which one of the following drugs is used for Cardiac stress test? ``` A. Dobutamine B. Low dose dopamine C. Clonidine D. Phenylephrine E. Methamphetamine ```

A. Dobutamine

What is Ephedrine used for? And what is its MoA?

- nasal decongestant - raise blood pressure during surgery -a and B indirect agonist

Priapism is erections lasting for hours. Pharmacological treatment is: ``` A. Albuterol B. Clonidine C. Dobutamine D. Phenylephrine E. Amphetamine ```

D. Phenylephrine

A. Which of the following is a bronchodilator? B. Which one is a choice antihypertensive in pregnant women? C. Which of the following raises BP by vasoconstriction? ``` A. Dobutamine B. Clonidine C. Phenylephrine D. Salmeterol E. Alpha-methyldopa ```

A= D. Salmeterol

What receptors does dopamine act on at low, moderate, and high doses?

Low: D1 Moderate: D1 & B1 High: D1, B1, & a1

Which receptor does Formoterol act on? Is it an agonist or antagonist?

B2 agonist *long acting

What is epinephrine's effect on Mast cells? What receptor?

- inhibits degranulation (think anaphylaxis) | - B2 agonist

What is the first line treatment for Parkinson’s disease? ``` A. SSRIs B. L-Dopa C. Dopamine blockers D. Serotonin blockers E. Acetylcholinesterase inhibitors F. Methylphenidate (Ritalin) ```

B. L-Dopa

Why don't we use selective B2 blockers?

-you will suffocate your patient

What is a Sympathomimetic?

-a drug that mimics nor/epinephrine

What type of side effects do SSRIs have?

-Adrenergic sid1e effects

What are B1 blockers used to treat?

- Hypertension - CHF - Post-MI - Angina pain - Glaucoma - migraine, hyperthyroidism, performance anxiety

What is the suffix of all beta blockers?

-olol

Why don't we stop B blocker use abruptly?

- the # of B receptors will have been upregulated | - stopping immediately can cause arrhythmias

What is Labetalol?

- Used to treat Hypertension | - Mixed alpha 1 and Beta blocker

What is Carvedilol?

- Used to treat Hypertension | - Mixed alpha 1 and Beta blocker

Why is a thiazide sometimes used in conjunction with a B blocker?

- to downregulate the RAAAs system | - Decrease plasma volume

What are cardio-selective B blockers?

- selective to B1 - less bronchoconstriction - More expensive

How can a partial B agonist treat hypertension?

- competing with full agonist epinephrine for B receptors | - wont activated as much as epinephrine, so net effect is decreased cardiac output

Out of the following receptors, which receptors predominate (abundant) on smooth muscle around veins? ``` A. Beta 2 B. Alpha 1 C. Alpha 2 D. Beta 1 E. Beta 3 ```

B. Alpha 1

What are alpha (1) blockers used to treat?

- antihypertensive - treat BPH **Alpha 2 blockers have little clinical use

``` Vascular tone (peripheral vascular resistance) is maintained by activation of : ``` ``` A. Beta-1 receptors B. Nicotinic receptors C. Beta-2 receptors D. Alpha-1 receptors E. Alpha-2 receptors ```

D. Alpha-1 receptors

What is Tamsulosin?

=Flomax - Alpha 1 blocker - treats BPH

What is Phenoxybenzamine?

-irreversible alpha 1 blocker -used to treat pheochromocytoma (epinephrine secreting adrenal medulla tumor) -antihypertensive used during surgery to remove tumor

What is Yohimbine

- Alpha 2 blocker - Might treat erectile dysfunction? probs not, must be locally injected. - Adverse effect: increase HR and BP

What is Terazosin?

- Alpha 1 bocker | - Treats hypertension

What do parasympathetic presynaptic alpha 2 receptors do?

-inhibit release of NT

What are the most significant adverse effects of alpha 1 blockers?

- postural/orthostatic hypotension | - reflex tachycardia

Why are combined a and B blockers useful? (labetalol, carvedilol)

a1 blocker dilates blood vessels; results in reflex tachycardia; b1-blocker prevents increase in heart rate. Drugs with multiple activities are some times very useful. Bottom line: Decrease PVR and Blood Pressure, No change in Heart Rate & Cardiac Output

A patient was given a bolus dose of terazosin (Hytrin). Question A. Terazosin belongs to what class of drug? ``` A. Alpha-1 agonist B. Alpha-1 blocker C. Beta blocker D. Alpha-2 blocker E. Beta-1 agonist ```

B. Alpha-1 blocker ***ZOSIN

A patient on spinal anesthesia goes into severe hypotension. The drug of choice to correct this hypotension is: ``` A. Propranolol B. Isoproterenol C. Phenylephrine D. Clonidine E. Albuterol ```

C. Phenylephrine

What is the drug of choice to treat BPH (Benign Prostatic Hypertrophy) resulting in urinary retention? ``` A. Tamsulosin B. Phenylephrine C. Nitroglycerin D. Bethanechol E. Propranolol F. Terazosin ```

A. Tamsulosin

What causes schizophrenia?

-high dopamine (D2) in the limbic system