Exam #02 - Adrenergic Agonists and Antagonists and Anti-hypertensive Agents Flashcards

1
Q

Phenylephrine

A

Type: Direct-acting Adrenergic agonist

Selectivity: Alpha-1 selective

MOA:
powerful post-synaptic alpha-receptor agonist producing vasoconstriction

Major Therapeutic Use:
nasal decongestant
ophthalmic solutions for mydriasis

AE:
high doses can cause hypertensive HA and heart irregularities

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2
Q

Clonidine

A

Brand Name: Catapres

Type: Direct-acting Adrenergic agonist

Selectivity: Alpha-2 selective

Major Therapeutic Use:
hypertension

MOA: stimulates alpha-2 adrenergic receptors in the brain resulting in reduced sympathetic outflow from the CNS and decreased peripheral resistance, renal vascular resistance, HR, and BP

Notes:
2 similar drugs: Guanabenz & Guanfacine

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3
Q

Dobutamine

A

Type: Direct-acting Adrenergic agonist

Selectivity: Beta-1 selective

MOA:
stimulates beta-1 receptors in heart

Major Therapeutic Use:
increase CO and cardiac contractility to treat CHF

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4
Q

Terbutaline

A

Type: Direct-acting Adrenergic agonist
Selectivity: Beta-2 selective

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5
Q

Isoproterenol

A

Type: Direct-acting Adrenergic agonist

Selectivity: Non-selective Beta agonist

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6
Q

Epinephrine

A

Type: Direct-acting Adrenergic agonist

Selectivity: Non-selective agonist

MOA:
activates both alpha and beta receptors

Major Therapeutic Use:
anaphylaxis, asthma, cardiac arrest, glaucoma,
cardiac stimulant (inotropic & chronotropic), potent vasoconstrictor, increase duration of LA for nerve block (give LA with epi constricts adjacent vessels and forms pocket), control of local bleeding (esp for facial surgery)

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7
Q

NE

A

Type: Direct-acting Adrenergic agonist

Selectivity: Non-selective agonist (hits all but beta-2)

MOA:
a sympathomimetic amine alpha activity results in peripheral vasoconstriction and beta activity leading to inotropic stimulation of the heart and coronary artery vasodilation

Major Therapeutic Use:
hypotension
cardiac arrest

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8
Q

Ephedrine

A

Type: Indirect/Mixed adrenergic agonist

Selectivity: Non-selective agonist

MOA: releases stored catecholamines (namely NE) increasing activity on adrenergic receptors

Major Therapeutic Use:
nasal decongestant, weight loss products

Notes:
found in Ma Huang plant
can cross BBB

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9
Q

Amphetamine

A

Type: Indirect Adrenergic agonist

MOA: stimulates release of NE, DA, and serotonin by impairing VMAT - more DA gets released into cytosol and gets pushed out into the synapse (some gets metabolized in cytoplasm before it’s released)
appetite suppressant and CNS stimulant

Major Therapeutic Use:
derivatives of amphetamine are used to treat ADHD and narcolepsy

AE:
toxicity due to excess beta receptor stimulation of the heart

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10
Q

Tyramine

A

Type: Indirect Adrenergic agonist

MOA:
stimulates the release of catecholamine (namely NE)

AE:
Tyramine is found in fermented foods (cheese, sausage, pickled fish, wine). If patient ingests these foods and is also taking a MAO inhibitor, there will be an increase in [NE] which can lead to a hypertensive crisis

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11
Q

Cocaine

A

Type: Indirect-acting Adrenergic agonist

Therapeutic Use: LA, vasoconstriction, peripheral sympathomimetic actions

MOA: inhibits reuptake of NE, DA, and serotonin by working at the DAT and NET

AE:
toxicity due to beta-receptor stimulation of heart
abuse mainly related to inhibition of DA reuptake

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12
Q

Reserpine

A

MOA: Irreversibly binds to VMAT stopping the packing of NE and DA into vesicles. Reduces sympathetic output, decreases HR and arterial BP

Major Therapeutic Use:
hypertension
psychotic disorder

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13
Q

Would direct acting adrenergic agonists be impacted by prior treatment with reserpine?

A

No, responses may actually be potentiated by reserpine (and cocaine)

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14
Q

Would mixed acting adrenergic agonists be impacted by prior treatment with reserpine?

A

Yes, b/c ephedrine is still acting on post-synaptic receptors, the response would be reduced

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15
Q

Would indirect acting adrenergic agonists be impacted by prior treatment with reserpine?

A

Yes, responses are abolished b/c stores of NE and DA have been depleted

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16
Q

Dopamine (DA)

A

Brand Name: Intropin

Selectivity: dopaminergic and adrenergic agonist

MOA:
produces positive inotropic and chronotropic effects on myocardium by activating beta1-receptors on heart and releases NE from storage sites thus increasing heart rate and contractility. Also stimulates alpha-adrenoreceptor activity resulting in vasoconstriction increasing peripheral resistance and a rise in BP

Major Therapeutic Use:
raises BP (vasopressor)
useful in treating CHF
at low doses, good for treating shock situations

Notes: Dose dependent; at low doses PR can decrease, at higher doses activates alpha-1 receptors leading to vasoconstriction

17
Q

Salmeterol

&

Formoterol (Foradil)

A

Brand name: Serevent

Selectivity: beta-2 agonist

MOA:
activation of beta-2 receptors in lungs
long acting due to high lipid solubility

Major Therapeutic Use:
Chronic asthma and COPD
DOC for long lasting effects
Used as asthma prophylaxis

AE: tremor, tachycardia (from effects way down the line on beta-1 receptor)

18
Q

Albuterol

&

Metaproterenol

&

Pirbuterol (Maxair)

A

Brand name: Proventil

Selectivity: beta-2 agonist

MOA:
activation of beta-2 receptors in lungs
max effects within 15-30 min, lasts 3-4 hours

Major Therapeutic Use:
acute bronchospasm
useful in treating exercise induced asthma

AE:
use with caution in patients with cardiac arrythmias and uncontrolled hypertension
tremor, tachycardia

19
Q

Pseudoephedrine

A

Type: Indirect/Mixed adrenergic agonist

Selectivity: Non-selective agonist

MOA: releases stored catecholamines (namely NE) increasing activity on adrenergic receptors

Major Therapeutic Use:
OTC nasal/sinus decongestant

Notes:
found in Ma Huang plant
can cross BBB

20
Q

Phentolamine

A

Type: non-selective alpha antagonist (competitive, surmountable)

MOA:
Reversibly binds and blocks alpha-1 and alpha-2 receptors. Decreases peripheral resistance (alpha-1) and increase CO (blocking alpha-2 receptors increase sympathetic outflow)

Major Therapeutic Use:
pheochromocytoma (tumor in adrenal medulla releasing excess Epi and NE)
shorter duration of action than Phenoxybenzamine

AE:
postural hypotension
tachycardia

21
Q

Phenoxybenzamine

A

Type: non-selective alpha antagonist (non-competitive, non-surmountable)

MOA: irreversibly binds and blocks alpha-1 and alpha-2 receptors. Decreases peripheral resistance (alpha-1) and increase CO (blocking alpha-2 receptors increase sympathetic outflow)

Major Therapeutic Use:
pheochromocytoma (tumor in adrenal medulla releasing excess Epi and NE)
long duration of action

AE:
postural hypotension
tachycardia

22
Q
Prazosin
&
Terazosin
&
Doxazosin
A

Type: alpha-1 selective antagonist

MOA:
blocks alpha-1 receptors which decreases peripheral resistance

Major Therapeutic Use:
moderate to mild hypertension
BPH

AE:
vertigo
reflex tachycardia
postural hypotension

23
Q

Tamsulosin

A

Type: alpha-1 selective antagonist (selective for receptors in prostate)

MOA:
blocks alpha-1 receptors (mostly) in prostate

Major Therapeutic Use:
only used to treat BPH since it’s very selective for alpha-1 receptors in the prostate

24
Q

Yohimbine

A

Type: alpha-2 selective antagonist

No present clinical role

25
Q

Propanolol

A

Type: non-selective beta blocker

MOA:
blocks beta-1 and beta-2 receptors, decreasing HR, myocardial contractility, BP, and O2 demand (from heart slowing down)

Major Therapeutic Use:
hypertension
angina
arrythmias and tachycardia
migraine prophylaxis

AE:
use with caution in asthma patients, since this is a non-selective beta blocker (blocking beta-2 receptor would result in increased bronchoconstriction

26
Q
Acebutolol
& 
Atenolol
&
Metoprolol
A

Type: Beta-1 selective blocker (competitive, surmountable)

MOA:
blocks beta-1 receptors resulting in decreased HR, CO, BP

Major Therapeutic Use:
hypertension (especially in patients with asthma)
supraventricular and ventricular arrythmias
ischemic heart disease

27
Q

Esmolol

A

Type: Beta-1 selective blocker (competitive, surmountable)

MOA:
blocks beta-1 receptors resulting in decreased HR, CO, BP. rapid onset, short acting drug (10 min)

Major Therapeutic Use:
Useful in treating critically ill patients with arrhythmias via IV in hospital setting only.

28
Q

Timolol

A

Type: non-selective beta blocker

Major Therapeutic Use:
treats open angle glaucoma

NO LA effect so safe for glaucoma (you wouldn’t want to numb the eye to treat glaucoma)

29
Q

Nadolol

A

Type: non-selective beta blocker

Major Therapeutic Use:
hypertension
LONG ACTING (14-24 hours)

30
Q

Labetalol

A

Type: non-selective alpha & beta blocker

Major Therapeutic Use:
hypertension
heart failure
arrythmias, angina

AE:
use caution in asthma patients

Notes:
NOT useful in treating glaucoma b/c it has LA effect

31
Q

Carvedilol

A

Type: non-selective alpha & beta blocker

MOA: non-selective blocker, plus Ca+2 channel blocker, antioxidant activity

Major Therapeutic Use:
useful in treating patients with CHF b/c it’s slightly more beta selective
hypertension

AE:
use caution in asthma patients

Note:
metabolite of carvedilol has amazing anti-oxidant properties

32
Q

Nebivolol

A

Type: beta-1 selective blocker

MOA:
blocks beta-1 receptors AND increases NO production (contributes to vasodilation)
Long acting (11-30 hours)

Major Therapeutic Use:
hypertension

33
Q

Carteolol

A

Type: non-selective beta blocker

MOA:
blocks beta-1 receptors AND increases NO production AND has partial agonism on beta-2 receptors (all contributing to vasodilation)

Major Therapeutic Use:
hypertension

34
Q

Betaxolol

A

Type: beta-1 selective blocker

MOA: blocks beta-1 receptors AND Ca+2 channel blocker (contributes to vasodilation)

Major Therapeutic Use:
hypertension
glaucoma

35
Q

Methyldopa

A

Type: alpha-2 selective agonist

MOA:
methyldopa injected, rapidly enters brain, converted into methylnorepinephrine which activates alpha-2 receptors and leads to reduction in sympathetic outflow lowering CO, peripheral resistance, and BP

Major Therapeutic Use:
hypertension in pregnant women

Notes:
much longer duration of action compared to Clonidine (the other alpha-2 agonist)