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Flashcards in Adrenergic Deck (46)
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1

alpha agonist activity

Stimulation of a1
Induce contraction of smooth muscle
Primary effect- vasoconstriction of most vascular smooth muscle

2

alpha 1 selective agonist clinical use

Decongestant
Pressor (BV constriction)

3

Phenylephrine important pharmokinetics

Longer duration of action than catecholamines

4

Phenylephrine (a1 agonist) adverse effects

Angina, anxiety, bradycardia, hypertension, tissue necrosis

5

alpha 1 and beta 1&2 agonists

sympathomimetics

6

alpha 1 and beta 1 &2 antagonists

sympatholytic

7

olol

beta blocker

8

lol

funny beta blocker

9

Phenylephrine interaction

MAO inhibitors (MAO breaks down phenylephrine)

10

Methyldopa is a

prodrug

11

a2 agonist action

Stimulation of a2 receptors in the medulla has sympatholytic effects
No reflex tachycardia
Decrease overall NE release thru stimulation of pre-synaptic receptors

Net Effect:
Hypotension
Bradycardia
Decreased cardiac output

12

a2 agonist clinical use

Hypertension
Clonidine more potent and used more often than methyldopa but pregnancy category C

Clonidine: Several CNS disorders including ADHD, mitigate drug withdrawal, severe pain

13

Methyldopa (a2 agonist) first-line therapy

for hypertension during pregnancy

14

a2 agonist adverse effects

orthostatic hypotension, tolerance, sudden withdrawal precipitates hypertensive crisis

15

Clonidine is effective both in the periphery and in the brain. Alpha-methyldopa is effective only in the

brain. It readily enters the brain where it is metabolized to the active compound a-methyl-norepinephrine (a2 agonist).

16

B1 effects in

heart, glomeruli cells in kidney

17

B2 effects in

lung (dialation), skeletal muscle vasculature (promotes blood flow)

18

Isoproterenol (nonselective B agonist) clinical use

cardiac arrest, AV block, bradycardia

19

Dobutamine

selective B1 agonist; activates a1 receptors at high doses; increases force of contraction of heart

20

B2 mech of action

(albuterol)
Relaxation of vascular smooth muscle.
Particularly in skeletal muscle vasculature
Relaxation of bronchial smooth muscle.
Stimulation of glycogenolysis
May lead to hyperglycemia.
Relaxation of uterine smooth muscle.

21

B2 agonist clinical use

Asthma
Acute bronchospasm
Bronchospasm prophylaxis
Premature Labor - Ritodrine (Yutopar®)

22

B2 agonist adverse effects

Tremors
Stimulation (CNS)
Palpitations
Tachycardia (direct and reflex) (some B1 effects)

23

a1 receptor location

blood vessels

24

a antagonists action

Block a1 or both a1 and a2 receptors
Decrease peripheral vascular resistance
Vasodilation triggers increased heart rate
HR increase more pronounced with mixed a1/a2 antagonists because of diminished a2 feedback in heart (remember a2 in presynaptic nerve termini).

25

Non-selective a antagonist clinical use

Pheochromocytoma
(tumor of adrenal gland)

26

a1 antagonist use

Hypertension*(not first line)
Benign prostatic hyperplasia (BPH)

27

Phentolamine route of admin

IV or IM route of admin

28

Prazosin

short half life (not good anti-hypertensive)

29

a antagonists adverse effects

Dizziness
Hypotension
Postural hypotension
Reflex tachycardia
Nasal stuffiness
Inhibition of ejaculation
Tolerance†
Na/H2O retention when used alone for HTN

30

a antagonists contraindication

Angina, MI

31

B antagonist actions

Block b1 or both b1 and b2 receptors
Cardiovascular
Have negative inotropic, dromotropic and chronotropic effects
Decrease renin release
Block of b2 may increase peripheral resistance
CNS
Anxiolytic
CNS effects may contribute to decrease HTN
Eye
Decreased aqueous humor production
Lungs
Bronchoconstriction
More prominent in b1/ b2 than b1-selective
Metabolic
Lipolysis and glycogenolysis are inhibited
Insulin release is inhibited
Inhibit recovery from hypoglycemia
More prominent in b1/ b2 than b1-selective

32

Non-selective b Antagonists: Clinical Use

angina, cardiac arrhythmias, hypertension, myocardial infarction prophylaxis, pheochromocytoma, post-myocardial infarction, thyrotoxicosis, tremor

33

B blockers shouldn't be used as 1st line treatment for

hypertension

34

When are b blockers first-line therapy for hypertension?

Ischemic Heart Disease
Recent STEMI or non-STEMI
Left Ventricular Systolic Dysfunction
Some Arrhythmias
(decrease BP and decrease heart remodeling)

35

Propanolol's half life is

long, which makes it a good treatment for hypertension

36

Propanolol (b blocker) adverse effects

Dizziness, fatigue, lethargy, sinus bradycardia and hypotension, exacerbation of asthma, dyspnea, or diabetes mellitus

37

Propanolol Contraindications

Diabetes mellitus, hyperthyroidism
Pregnancy category C*
Asthma, AV block, bradycardia, cardiogenic shock, sick sinus syndrome

38

Withdrawal Syndrome

Rebound hypertension, MI, cardiac arrhythmias and panic attacks can result from sudden withdrawal from B antagonists

39

B1 antagonist actions

Similar cardiovascular actions as the non-selective antagonists
Since they have no b2 activity, they are preferred in patients with bronchospasm, diabetes and peripheral vascular disease

40

B1 antagonist clinical use

acute MI, angina, cardiac arrhythmias, hypertension, myocardial infarction prophylaxis, postmyocardial infarction; metoprolol-heart failure

41

Metoprolol has a ________ half life than Atenolol, making it

longer; better treatment (less escape into disease progression)

42

b1 Antagonists : Adverse Effects Adverse Effects, Contraindications

Similar to the non-selective b antagonists
Asthma and bronchospasms are no longer absolute contraindication, but b1 antagonists should be used with great caution in these individuals.
Atenolol-Pregnancy category D

43

Mixed a1/b-Adrenoceptor Antagonist: Mechanisms of Action

Block a1 and both b1 and b2 receptors
Cardiovascular
Mixture of both a1 antagonists and b blockers

44

Mixed a1/b-Adrenoceptor Antagonist: clinical use

acute MI, angina, cardiomyopathy, heart failure (1 of 3 recommended), hypertension, myocardial infarction prophylaxis, postmyocardial infarction

45

Labetalol has a ________ half life than Carvedilol, but

shorter; but it is a good drug for hypertensive pregnant women

46

Mixed a1/b-Adrenoceptor Antagonist Adverse effects

Similar to the non-selective b blockers (i.e. bronchospasms) and a1 antagonists (postural hypotension)
Less reflex tachycardia than a1 antagonists, less peripheral vasoconstriction than with b blockers
Carvedilol contraindicated in hepatic disease