6.2 Adrenergic Meds Flashcards

(43 cards)

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?

20
Q

What is levalbuterol used for?

A

R-enantiomer of albuterol
Tx asthma, COPD
B2

21
Q

What does pirbuterol target?

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
What is fenoldopam used for? Receptor?
D1 agonist  peripheral vasodilation | Treatment of severe HTN (ICU med)
26
What are the 4 mechanisms of indirect-acting sympathomimetics?
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
What are examples of indirect sympathomimetics that displace storage?
“amphetamine-like” = “displacers” | Ex: Amphetamine, methamphetamine, phendimetrazine (bontril), and methylphenidate
28
What are examples of indirect sympathomimetics that inhibit uptake?
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
What are the many applications of sympathomimetics?
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
What is an alpha blockade? What causes it?
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
What is prazosin used for? Receptor?
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
What is terazosin used for? | Receptor?
Less potent than prazosin High specificity for alpha-1 receptors >90% bioavailability; T1/2 = 12hrs Tx: HTN, BPH
33
What do -osin meds do?
A1 blocker
34
What is yohimbine? Receptor?
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
What is phenooxybenzamine? | Receptor?
covalent bond to receptor irreversible blockade | Treatment of pheochromocytoma (adrenal tumor secrete lots of catecholamines)
36
What is phentolamine? receptor?
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
What are the general effects of Beta blockers?
Lower BP Increase airway resistance Reduce intraocular pressure Selectivity is dose-dependent
38
What are the B1 selective Beta blockers?
-olol | BBEAAM - We'll have a list of drugs
39
What is notable about acebulol and esmolol?
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
What is propranolol used for?
Used off-label for panic attacks, anxiety; anti-arrythmic; migraine prophylaxis; hyperthyroid
41
What is labetolol used for?
partial agonist and A1 selective
42
What are side affects of beta blockers?
``` Bradycardia Mild sedation Cold hands Vivid dreams Depression – rare Nonselective agents – worsen preexisting asthma Depressed myocardial contractility and excitability Cautious in decompensated HF ```
43
What happens with beta blockers and asthma? heart failure?
With asthma- B2 blockers cause broncho constriction asthma exascerbation Can case/worsen heart failure if used in decompensated HF