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
