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270 S1 > 6.2 Adrenergic Meds > Flashcards

6.2 Adrenergic Meds Flashcards

1
Q

What are the A1 agonists?

A

Phenylepherine

Milodrine

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2
Q

What are the indications and SA of phenylpherine?

A

selectively stimulates A1 receptor, short half life (2-3 hr) used to maintain BP
If just want vasocontriction (HR ok) use phenylephrine/neosynephrin
ALSO in nasal decongestants (OTC sudafed)- controls congestion by vasoconstriction
SA- high BP, so don’t give with HTN

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3
Q

What are the indications and SA of milodrine?

A

Prodrug, Selective to A1. Used for pt with poor autonomic fxn (eg parkinsons)
Eg orthostatic hypotension, maintains BP;
SA- Black box warning- causes supine HTN

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4
Q

What are the subcategories of A2 agonists?

A

Central acting

Peripheral acting

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5
Q

What are the indications for clonidine?

A

Lower BP
alpha-2 receptors in CNS suppress outflow of sympathetic activity  lower BP
Vasoconstriction nasal decongestant

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6
Q

What are the indications for clonidine?

A

HTN
Reducing diarrhea in DM pts w/ autonomic neuropathy
Relieve w/d sxs – narcotics, alcohol, and tobacco addiction decr craving
** 100% bioavailability PO

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7
Q

What are the side effects of clonidine?

A

Dry mouth
Sedation
Sexual dysfunction
Caution: w/d rxn follow abrupt d/c of long term therapy

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8
Q

What is brimodinine used for?

A

Alpha-2 selective reduce prod of aqueous humor

Lower intraocular pressure (i.e. open-angle glaucoma)

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9
Q

What is guanfacine used for?

A 
Alpha-2 selective (more than clonidine) -- central
Lower BP
ER formulation (Intuniv®)  -- for ADHD
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10
Q

What is guanabenz used for?

A

Centrally acting alpha-2 agonist

Extensively metabolized by liver = many DDI

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11
Q

What is methydopa used for?

A

Centrally acting antihypertensive
Metabolized to alpha-methyl-NE (in brain)  activate alpha-2 in CNS lower BP
Used with pregnanct PTs to lower BP- centrally acting HTN

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12
Q

What is tizanidine used for?

A

Central acting alpha-2 stimulator

Muscle relaxant tx muscle spasticity d/t spinal or cerebral dz

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13
Q

What subcategories of Beta agonists are there?

A

Non-selective
B1 selective
B2 selective
** Can be dose-dependent

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14
Q

What is isoproterenol used for?

Receptor?

A

Non-selective Beta agonist, relaxes all smooth muscle, esp. RESP and GI. for asthma

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15
Q

What is dobutamine used for? Receptor?

A

B1 selective

+ inotrope, increase cardiac output, with less reflex tachycardia

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16
Q

What is levalbuterol used for? Receptor?

A

B2 selective

Bronchial dilation

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17
Q

What is Terbutaline used for? Receptor?

A

Asthma

Tocolytics- prevents smooth muscle contractions, e.g. in pregnancy

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18
Q

What is metaproterenol used for? Receptor?

A

B2
Tx asthma
Less beta-2 selective than albuterol or terbutaline more prone to cardiac stimulation
Resistant to COMT

19
Q

What receptor for albuterol? Use?

A

B2

Asthma

20
Q

What is levalbuterol used for?

A

R-enantiomer of albuterol
Tx asthma, COPD
B2

21
Q

What does pirbuterol target?

A

B2

22
Q

What is formoterol used for?

Receptor?

A

Long duration Bronchial dilation may persist for 12hrs

Tx: Asthma and COPD

23
Q

What is anformoterol used for?

A

R,R) enantiomer of formoterol

Twice as potent as Formoterol

24
Q

What is levodopa used for? receptor?

A

Dopamine agonist
Treatment of Parkinson’s disease or prolactinemia
Converts to dopamine  stimulate dopamine receptors

25
Q

What is fenoldopam used for? Receptor?

A

D1 agonist  peripheral vasodilation

Treatment of severe HTN (ICU med)

26
Q

What are the 4 mechanisms of indirect-acting sympathomimetics?

A

Displace storage- Drug comes in, displaces neurotransmitter from vesicles that store them, so when signal for release comes, cause excessive release
Inhibit reuptake
MAO Inhibiter
COMT inhibitor

27
Q

What are examples of indirect sympathomimetics that displace storage?

A

“amphetamine-like” = “displacers”

Ex: Amphetamine, methamphetamine, phendimetrazine (bontril), and methylphenidate

28
Q

What are examples of indirect sympathomimetics that inhibit uptake?

A

NE transport inhibitor
Ex:
Atomoxitine (Strattera) – ADHD – selective for NE reuptake transporter
Sibutramine (Meridia) – weight loss – serotonin and NE reuptake inhibitor
Duloxetine – chronic pain, fibromyalgia – SNRI
Cocaine – local anesthetic – dopamine reuptake inhibitor at the “pleasure centers” in the brain – highly abuse

29
Q

What are the many applications of sympathomimetics?

A

Treatment of Acute hypotension or shock (i.e. maintaining BP)
Ex: Levophed (norepinephrine); Neo-synephrine (phenylephrine)
Chronic orthostatic hypotension
Hypertension – Centrally acting alpha-2 agents
Inducing local vasoconstriction – decongestant
Bronchial dilation
Anaphylaxis
Mydriatic agent (i.e. phenylephrine)
Tocolytics – suppress premature labor
Weight loss
Narcolepsy – i.e. amphetamine, methamphetamine
ADHD

30
Q

What is an alpha blockade? What causes it?

A

When alpha receptors stimulated, cause vasoconstriction, so when blocked, cause vasodilation in arterioles and vains
= lower BP and vascular resistance (afterload)
If BP too low with these meds, body will attemot to compensate, up HR, …. Keeps building until pt crashes

SA- reflex tachycardia- autonomic reflex kicks in, hr increases
Orthostatic HTN- causes peripheral vasculature to be less responsive to vasoconsteiction
Decreases resistance to flow of urine… promotes urinary outflow

31
Q

What is prazosin used for? Receptor?

A

Blockade of alpha1 receptors in arterioles and veins
No reflex tachycardia d/t alpha 1 selective
Good PO absorption – 70% bioavailability
95% protein bound; T1/2 = ~3hrs

32
Q

What is terazosin used for?

Receptor?

A

Less potent than prazosin
High specificity for alpha-1 receptors
>90% bioavailability; T1/2 = 12hrs
Tx: HTN, BPH

33
Q

What do -osin meds do?

A

A1 blocker

34
Q

What is yohimbine? Receptor?

A

Competitive alpha-2 blocker
Found in bark of Pausinytalia yohimbe and Rauwolfia root
Structure resemble reserpine
Enters CNS incr BP and HR (opposite to clonidine)
Also blocks 5HT
Tx: male sexual dysfunction – less conclusive than PDE5 inhibitors

35
Q

What is phenooxybenzamine?

Receptor?

A

covalent bond to receptor irreversible blockade

Treatment of pheochromocytoma (adrenal tumor secrete lots of catecholamines)

36
Q

What is phentolamine? receptor?

A

A2 blocker
Indications:
Pheochromocytoma
Extravasation necrosis from alpha agonists
HTN crises follow abrupt w/d of clonidine
Caution: in PUD enhance GI secretion d/t histamine release
SE:
Hypotension
Tachycardia
Arrhythmias
MI

37
Q

What are the general effects of Beta blockers?

A

Lower BP
Increase airway resistance
Reduce intraocular pressure
Selectivity is dose-dependent

38
Q

What are the B1 selective Beta blockers?

A

-olol

BBEAAM - We’ll have a list of drugs

39
Q

What is notable about acebulol and esmolol?

A

Acebulol- B1 blocker and partial agonist– When binds to receptor, blocks the receptor, but stiumulates it a little= won’t lower BP as much

Esmolol- T1/2 10min!! Use if need a short acting B1 antagonist

40
Q

What is propranolol used for?

A

Used off-label for panic attacks, anxiety; anti-arrythmic; migraine prophylaxis; hyperthyroid

41
Q

What is labetolol used for?

A

partial agonist and A1 selective

42
Q

What are side affects of beta blockers?

A 
Bradycardia
Mild sedation
Cold hands
Vivid dreams
Depression – rare
Nonselective agents – worsen preexisting asthma
Depressed myocardial contractility and excitability
Cautious in decompensated HF
43
Q

What happens with beta blockers and asthma? heart failure?

A

With asthma- B2 blockers cause broncho constriction asthma exascerbation

Can case/worsen heart failure if used in decompensated HF

270 S1 (19 decks)

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