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Pharmacology and Medical Chemistry I > Exam 4 - Lecture 42-43, Adrenergic Agonists I + II > Flashcards

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

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1
Q

a1 antagonist signaling

A

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

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2
Q

a2 antagonist signaling

A

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

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3
Q

b antagonists signaling

A

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

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4
Q

a1 receptor antagonist commonly used..

A

for vascular relaxation effects, inhibit vasoconstriction and cause vasodilation

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5
Q

b receptors…

A

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

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6
Q

a antagonists used to…

A

control BP during surgery and in treatment of pheochromocytomas

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7
Q

a1 selective antagonists

A

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

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8
Q

a2 selective antagonists

A

have limited clinical usefulness; limited benefit in male ED

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9
Q

b antagonists are useful in…

A

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

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10
Q

Angina pectoris

A

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

beta blockers decrease contractility, cardiac work and oxygen demand

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11
Q

Myocardial infarction

A

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

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12
Q

Arrhythmia/Dysrhythmias

A

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

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13
Q

Congestive heart failure

A

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

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14
Q

hypertension

A

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

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15
Q

Pheochromocytoma

A

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

localized using CT scan or MRI with MIBG

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16
Q

Benign prostatic hypertrophy

A

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

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17
Q

glaucoma

A

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

Beta blockers used to decrease intraocular pressure

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18
Q

Thyrotoxicosis

A

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

nonselective beta blockers treat increase HR and tremors

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19
Q

Anxiety

A

non specific beta blockers treat symptoms

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20
Q

PTSD

A

a antagonist and B blockers clinically used to alleviate symptoms

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21
Q

Migraine prophylaxis

A

beta blockers = prophylactic treatments of migraines

22
Q

alpha non-selective

A

phenoxybenzamine

Phentolamine

23
Q

a1 selective

A

-osin’s

indoramin
urapidil

24
Q

a2 selective

A

yohimbine

25
Q

beta non selective (first gen)

A 
nadolol
penbutolol
pindolol
propranolol
timolol
sotalol
levobunolol
metipranolol
26
Q

b1 selective (second gen)

A 
acebutolol
atenolol
bisoprolol
esmolol
metoprolol

best for heart

27
Q

beta non selective (3rd gen)

A

carteolol
carvedilol
bucindolol
labetalol

28
Q

b1 selective (3rd gen)

A

betaxolol
celiprolol
nebivolol

29
Q

Phentolamine

A

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

30
Q

Prazosin

A

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

31
Q

Terazosin

A

close structural analog to prazosin, but less potent

Indications: benign prostatic hyperplasia, hypertension

Mechanism: similar to prazosin

Side effects: similar to prazosin

32
Q

Doxazosin

A

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

33
Q

tamsulosin

A

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

34
Q

Yohimbine

A

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

35
Q

Beta blockers properties

A

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

36
Q

1st gen beta is non selective

A

blocks both b1 and b2

many side effects

37
Q

2nd generation are cardiac selective

A

most affects heart but will decrease cardiac output

38
Q

3rd gen shows additional effects

A

ISA

membrane stabilizing effects

some drugs have additional mechanism of vasodilation

39
Q

ISA

A

intrinsic sympathomimetic activity

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

40
Q

Propranolol

A

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 **

41
Q

Nadolol

A

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

42
Q

Timolol

A

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

43
Q

Pindolol

A

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

44
Q

Metoprolol

A

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

45
Q

Acebutolol

A

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

46
Q

Bisoprolol

A

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

47
Q

Atenolol

A

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

48
Q

How do 3rd gen B Blockers lower BP?

A

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

49
Q

Labetalol

A

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

50
Q

Carvedilol

A

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

Pharmacology and Medical Chemistry I (30 decks)

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