Exam 4 - Lecture 42-43, Adrenergic Agonists I + II

Question 1

a1 antagonist signaling

Answer 1

block Gaq -> no Ca increase -> smooth muscle dilation

Question 2

a2 antagonist signaling

Answer 2

blocks Gai -> increase Ca2 + cAMP production -> increase transmitter release and smooth muscle relaxation

Question 3

b antagonists signaling

Answer 3

blocks Gas -> no increase cAMP -> decrease heart muscle contraction, decrease renin secretion

Question 4

a1 receptor antagonist commonly used..

Answer 4

for vascular relaxation effects, inhibit vasoconstriction and cause vasodilation

Question 5

b receptors…

Answer 5

decrease HR contractility, conductor velocity and relaxation rate

little vascular effect, but can have small degree of vasoconstriction

contraindicated in patients with sinus sickness

cause inhibition of renin release form kidneys

Question 6

a antagonists used to…

Answer 6

control BP during surgery and in treatment of pheochromocytomas

Question 7

a1 selective antagonists

Answer 7

are used in primary hypertension and BPH major depressive disorder, PTSD

Question 8

a2 selective antagonists

Answer 8

have limited clinical usefulness; limited benefit in male ED

Question 9

b antagonists are useful in…

Answer 9

variety of clinical conditions and are firmly established in treatment of hypertension, ischemic heart disease, arrhythmias, endocrinology and neurologic disorders, glaucoma, and other conditions

Question 10

Angina pectoris

Answer 10

severe pain in chest, due to inadequate blood supply to heart.

beta blockers decrease contractility, cardiac work and oxygen demand

Question 11

Myocardial infarction

Answer 11

beta blockers used as secondary prevention, reducing infarct size, risk of ventricular fibrillation and decrease overall risk of death

beta blocker reduce HR,BP and contractility

Question 12

Arrhythmia/Dysrhythmias

Answer 12

abnormalities in cardiac muscle contractions or normal rhythm of the rate of rate heart beat.

Beta blockers may stop the dysrhythmia, primarily used to slow down heart rate during dysrhythmia.

beta blocker reduce HR,BP and contractility

Question 13

Congestive heart failure

Answer 13

cardiac output is insufficient to meet metabolic demand leading to fluid build up around the heart.

Beta blockers block harmful activation of the SNS or renin-angiotensin system

beta blocker reduce HR,BP and contractility

Question 14

hypertension

Answer 14

treatment with beta blockers useful for reducing cardiac output, reduction of renin release form kidney, and decrease of sympathetic activity

beta blocker reduce HR,BP and contractility

Question 15

Pheochromocytoma

Answer 15

tumor in medulla of adrenal gland which produces large amounts of catecholamines

localized using CT scan or MRI with MIBG

Question 16

Benign prostatic hypertrophy

Answer 16

enlarged prostate gland leading to decreased urine output

a antagonist used to relax prostate and bladder smooth muscle, but do not decrease the size of prostate

Question 17

glaucoma

Answer 17

disease of optic nerve causing cupping of optic disc leading to loss of vision

Beta blockers used to decrease intraocular pressure

Question 18

Thyrotoxicosis

Answer 18

“thyroid storm” increased thyroid hormone production and secretions resulting in increased heart rate, tremors, and nervousness

nonselective beta blockers treat increase HR and tremors

Question 19

Anxiety

Answer 19

non specific beta blockers treat symptoms

Question 20

PTSD

Answer 20

a antagonist and B blockers clinically used to alleviate symptoms

Question 21

Migraine prophylaxis

Answer 21

beta blockers = prophylactic treatments of migraines

Question 22

alpha non-selective

Answer 22

phenoxybenzamine

Phentolamine

Question 23

a1 selective

Answer 23

-osin’s

indoramin
urapidil

Question 24

a2 selective

Answer 24

yohimbine

Question 25

beta non selective (first gen)

Answer 25

``` nadolol penbutolol pindolol propranolol timolol sotalol levobunolol metipranolol ```

Question 26

b1 selective (second gen)

Answer 26

``` acebutolol atenolol bisoprolol esmolol metoprolol ``` best for heart

Question 27

beta non selective (3rd gen)

Answer 27

carteolol carvedilol bucindolol labetalol

Question 28

b1 selective (3rd gen)

Answer 28

betaxolol celiprolol nebivolol

Question 29

Phentolamine

Answer 29

Non-selective Alpha antagonist Indications: Hypertensive emergency; treat and diagnose pheochromocytoma; reversal of anesthesia Side effect: hypotension, orthostatic hypotension, reflex tachycardia, priapism; nasal congestion Contraindications: angina/coronary artery disease, MI, hypotension

Question 30

Prazosin

Answer 30

Prototypic for a1 antagonists Indications: Monotherapy for mild hypertension or with other drugs for moderate to severe hypertension BPH side effects: slight risk of pancreatitis, dizziness, headache, lethargy, 1st dose can cause sever hypotension Pregnancy category: C but avoided

Question 31

Terazosin

Answer 31

close structural analog to prazosin, but less potent Indications: benign prostatic hyperplasia, hypertension Mechanism: similar to prazosin Side effects: similar to prazosin

Question 32

Doxazosin

Answer 32

close analog to prazosin Indications: Benign prostatic hyperplasia; ureteric stone; neurogenic bladder and ED diagnosis Mechanism: non-subtype-selective a1 antagonist side effects: nausea, cardiovascular edema, priapism may occur leading to permanent impotence Contraindications: Do not use with PDE5 inhibitor for risks of hypotension

Question 33

tamsulosin

Answer 33

Indications: BPH; ureteric stone; neurogenic bladder Mechanism: selective a1 receptor antagonist Side effects: failure to jizz; orthostatic hypertension; dizziness, vertigo, somnolence; maybe back pain, rhinitis, or pharyngitis Contraindications hepatic or renal impairment; advise surgeons before cataract surgey

Question 34

Yohimbine

Answer 34

a2 antagonists, mainly used in research Indications: no FDA approved; natural product for impotence in males Contraindications: psych patients, history of ulcers, renal or liver disease, tyramine contains foods, pregnancy, antidepressant, chronic inflammation of sex organs of prostate gland Pregnancy Category X

Question 35

Beta blockers properties

Answer 35

little effect on heart when person at rest, but big effect when sympathetic control of heart is dominant (exercise or stress) block chronotropic and inotropic actions of catecholamines block exercise-induced increases in HR and contractility, but cardiac output is less effected due to an increased stroke volume

Question 36

1st gen beta is non selective

Answer 36

blocks both b1 and b2 many side effects

Question 37

2nd generation are cardiac selective

Answer 37

most affects heart but will decrease cardiac output

Question 38

3rd gen shows additional effects

Answer 38

ISA membrane stabilizing effects some drugs have additional mechanism of vasodilation

Question 39

ISA

Answer 39

intrinsic sympathomimetic activity mimic effects of E and NE causing very slight increase in BP and HR

Question 40

Propranolol

Answer 40

prototypic B receptor antagonist Indications: Hypertension, angina, essential tremors, prevention of MI, migraine prophylaxis Lacks: ISA Side effects: cold extremities, anorexia, nausea, vomiting, insomnia, wheezing Monitor: asthma symptoms and blood glucose Contraindications: low blood pressure (<50/30), sinus bradycardia w/o pacemaker *** Highly Lipophilic, crosses BBB ***

Question 41

Nadolol

Answer 41

Indications: angina, hypertension, ff label migraine prophylaxis and parkinsonian tremors Use caution/adjust doses in patients with renal failure Long acting antagonist with B1=B2 affinities

Question 42

Timolol

Answer 42

Indications: Intraocular hypertension and glaucoma Contraindications: OU admin can lead to systemic effects in patients with asthma or CHF, use caution with cimetidine due to increase plasma levels of timolol Pregnancy category C, can cross placenta resulting in bradycardia and cardiac arrhythmia

Question 43

Pindolol

Answer 43

Indications: angina, hypertension Mechanism: nonselective b antagonist, with ISA with membrane stabilizing activity and low lipid solubility Use caution in patients with renal failure, excreted from kidney Side effects: decreased sex drive, sleep problems, tired feeling, anxiety, nervousness, dizziness, drowsiness Pregnancy category B - no proven risk humans

Question 44

Metoprolol

Answer 44

Indications: angina, CHF, hypertension Mechanism: b1 selective antagonist, devoid of ISA and membrane stabilizing activity Contraindications: acute MI in patients with HR <45bpm, systolic BP <100 mmHG or in moderate to sever HF, severe bradycardia or sick sinus syndrome Side effects: diarrhea, fatigue, headache or depression; **drug may mask symptoms of hypoglycemia** Pregnancy category C, safe breast feeding

Question 45

Acebutolol

Answer 45

Indications: Hypertension, ventricular arrhythmias Mechanism: B1 selective antagonis 2nd gen, ISA and membrane-stabilizing activity Side effect: dizziness, headache, fatigue...monitor asthma and blood glucose contraindications: cardiogenic shock, overt cardiac failure, sever bradycardia, 2nd/3rd degree heart block Pregnancy class: B

Question 46

Bisoprolol

Answer 46

Indications: hypertension b1 selective antagonist 2nd gen), lacks both ISA and membrane stabilizing activity Side effect: dizziness, bradycardia, hypotension and fatigue....monitor: asthma and blood glucose Contraindications: cardiogenic shock, overeat cardiac failure; severe bradycardia, 2nd/3rd degree hear block Pregnancy Class: C

Question 47

Atenolol

Answer 47

Indications: Hypertension, coronary heart disease, arrhythmias, angina Mechanism: B1 selective antagonist that is devoid of ISA and membrane stabilizing activity contraindications: cardiogenic shock, overt cardiac failure; severe bradycardia, 2nd/3rd degree hear block Pregnancy class: D

Question 48

How do 3rd gen B Blockers lower BP?

Answer 48

through peripheral vasodilation, enhancing hypotension, increasing peripheral blood flow and/or decreasing after load

Question 49

Labetalol

Answer 49

Indications: hypertension Mechanism: mixed a1 and non-selective b antagonist....membrane stabilizing effects and ISA effects Side effects: orthostatic hypotension, tingling of skin, dizziness, nasal congestion, bronchospasm Contraindications: bronchial asthma, overt cardiac failure; COPD; hypotension Pregnancy class: C

Question 50

Carvedilol

Answer 50

Indications: hypertension; HF, impaired left ventricular function Mechanism: mixed a1 and non-selective B antagonist; has antioxidant and antiflammatory effects, at high dose Ca channel-blocking activity. No ISA but has membrane stabilizing activity. Reno-protective, favorable effects in patients with diabetes or metabolic syndrome Side effects: weight gain, diarrhea, dizziness, ED Contraindications: use caution with drugs that affect liver oxidation; similar to metoprolol Pregnancy class: not assigned, considered safe but conflicting data