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Pharm for midterm > Adrenergics > Flashcards

Adrenergics Flashcards

1
Q

Tyramine

A
  • dietary amine usually metabolized by MAO in GI and liver
  • in pts w/ MAO inhibitors. tyramine absorbed in large amts. End up with too much tyramine, too much NE being made= Hypertensive crisis
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2
Q

Alpha-methyltyrosine

A

Inhibits tyrosine hydroxylase (first step in synthesis of catecholamines)
RATE LIMITING STEP

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3
Q

Reserpine

A

Blocks VMAT (a transporter of bioamines [NE, DA, 5-HT] from cytoplasm into storage vesicles).

  • at low doses: leaking of NE into cytoplasm= depletion of NE in neuron (MAO degradation)
  • at high doses: overwhelm MAO–> exit into synapticc space through NET, acting in reverse–> transient sympathiomemetic effect
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4
Q

guanethidine

A

displaces NE in storage vesicles, leading to gradual depletion of NE (if not in storage vesicles, potentially ready to be destroyed by MAO)

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5
Q

amphetamine

A

displaces endogenous NE (like tyramine)

  • weak inhibitor of MAO-
  • blocks reuptake by NET and DAT
  • little agonist action at alpha and beta receptors, marked behavioral effects
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6
Q

cocaine

A

potent inhibitor of NET. essentially eliminates catecholamine transport. used as local anesthetic.

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7
Q

imipramine

fluoxetine

A

inhibitors of NET

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8
Q

tricyclic antidepressants

A

blocks Na/K ATPase (blocks action potential rom proceeding) and blocks NET
-prevents reuptake of NE and epinephrine=increased DOA

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9
Q

Phenelzine

A

inhibits MAO-A, increasing NE and 5-HT content

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10
Q

Selegiline

A

inhibits MAO, increases DA

-low doses for treatment of parkinsons disease

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11
Q

activity of alpha-1 receptor

A

vasoconstriction, increased peripheral vascular resistance, increase BP, mydriasis, increased closure of internal sphincter of bladder

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12
Q

activity of alpha 2 receptor

A

feedback receptor. inhibit NE release resulting in decreased BP, inhibit insulin release (pretty much inhibits sympathetics)

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13
Q

activity of B1 receptor

A

tachycardia, increased myocardial contractility, increased cardiac output, increased renin release, increased lipolysis

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14
Q

activity of B2 receptor

A

Vasodilation, decreased peripheral vascular resistance, decreased BP, bronchodilation, increased glycogenolysis in liver and muscle, increased glucagon release, relax uterine smooth muscle

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15
Q

direct adrenergic agonists

A

Epi/NE

  • albuterol, pirbuterol, terbutaline
  • dobutamine, dopamine
  • isoproteranol
  • phenylephrine
  • clonidine
  • salmeterol, formoterol
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16
Q

indirect adrenergic agonists

A

amphetmine

tyramine

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17
Q

mixed adrenergic agonist

A

ephedrine

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18
Q

epinephrine

A

Emergent treatment for asthma, glaucoma. direct- interacts w/ both alpha and beta receptors. (low doses- acts on beta- vasodilation)
(high doses- acts on alpha–vasoconstriction)
CV: 1) B1= (+) ionotropic, chronotropic= increased cardiac output
2) alpha- vasoconstricts arterioles
3) B2= vasodilates vessels to liver and skeletal muscle.
Net result: increased systemic BP

Respiratory: bronchodilation of smooth muscle (b2)
Hyperglycemia: decrease insulin release (alpha2), glycogenolysis increases, increase release of glucagon (b2), lypolysis (b1)

19
Q

Ephedrine

A

mixed adrenergic agonist.
ADRs: anxiety, fear, tension, HA, tremor. increase BP, hemorrhage, arrhythmias, pulmonary edema
Interactions: 1) hyperthyroidism- exaggerated CV effects due to increased receptor production. 2) cocaine- exaggerated CV effects due to prevention of reuptake

20
Q

Norepinephrine

A

affects alpha1, beta1.
CV: vasoconstriction in periphery= increased BP. baroreceptor reflex: increased BP–> increased vagal activity stimulating baroreceptors causing bradycardia.

21
Q

Labetolol

Carvediol

A

Antagonists of A1, B1, B2 receptors.

Causes peripheral vasodilation. doesn’t alter lipid/glucose levels.

22
Q

Carvediol

A

Antagonist of A1, B1, B2 receptors.

decreases lipid peroxidation and vascular thickening–benefits CHF

23
Q

Labetolol

A

Antagonist of A1, B1, B2 receptors

for HTN, CHF, PIH, HTN emergencies leads to decreased BP

24
Q

Pindolol

Acebutolol

A

Antagonists w/ partial agonist activity. (Blocks natural transmitter, but elicits small response itself)
Weakly stimulates B1 and B2 (but unable to respond to more potent catecholamine= decreased cellular effects)
activity: minimize lipid and CHO metabolism.
Used: HTN

25
Q

acebutolol
atenolol
metoprolol
esmolol

A

Selective B1 receptor blockers (cardioselective)

  • Eliminates unwanted broncoconstriction (so can be used in asthmatics and diabetic patients)
  • Little efect on CHO metabolism or PVR
  • useful in hypertensive DM pts receiving insulin or oral hypoglycemics
26
Q

timolol

nadolol

A

non-selective beta blockers

Uses: glaucoma and HTN

27
Q

propranolol

A

non-selective beta blocker (decreases HR, causes broncoconstriction)

  • uses: decrease BP, treat angina, arrhythmias, MI, glaucoma, prophylaxis for migraines
  • effects: decrease cardiac output (B1), decrease rate and force of HR. (but B2 effects are bad. not drug of choice for patients like asthmatics/diabetics)
28
Q

Tamsulosin

A

Treatment for benign prostate hyperplasia (BPH)
-inhibits alpha-1A receptor (specific for prostate): on smooth tissue of prostate, decreases tone of bladder neck and prostate, improves urine flow.

29
Q

Prazosin
Doxazosin
Terazosin

A

selective alpha1 blacker (so it vasodilates)

Treats HTN, BPH, CHF. relaxesarterial and venous smooth muscle—decreased PVR

30
Q

Phentolamine

A

competitive non-selective alpha-blocker (adrenergic antagonist)
blocks alpha1

31
Q

adrenergic antagonists (alpha blockers)

A

-phenotolamine (non-selective)
-prazosin, doxazosin, terazosin (alpha1-selective)
-tamsulosin
all reverse vasoconstrictive effects of epi
sd effects: orthostatic hypotension, reflex tachycardia, vertigo, sexual dysfunction

32
Q

dopamine

A

acts at renal mesentery
(at low doses, acts on D1 receptors in renal, mesenteric, and coronary vascular beds (vasodilators)
(at higher doses +ionotrope at B1 receptor)
(at really high doses, vasoconstricts via A1 receptor
DOC for shock; at appropriate doses is useful in management of decreased CO associated w/ compromised renal function like severe CHF

33
Q

phenylephrine

A

alpha-1 selective agonist. topical, constricts vascular smooth muscle in relief of nasal congestion.

  • not a catechol derivative so not substrate for COMT (loses potential metabolizers)
  • induces reflex bradycardia (bc it vasoconstricts) when given parenterally; increases BP
34
Q

Oxymetazoline

A

alpha-1 selective.

Topical, constricts vascular smooth muscle in relief of opthalmic hyperemia

35
Q

clonidine

A

decreases BP by suppressing sympathetic outflow

  • adverse effects: dry mouth, sedation (antimuscarinic)
  • alpha2 agonist
36
Q

Alpha-methyldopa

A

metabolized to alpha-methylnorepinephrine

  • alpha 2 agonist
  • THIS IS A PRO-DRUG. decreases sympathetic outflow
37
Q

guanfacine

A

alpha2 agonist in CNS to decrease sympathetic outflow.

adverse effects: dry mouth, sedation.

38
Q

isoproterenol

A

beta-nonselective agonist (designed to work better than epi, NE)
CV: +ionotropic, +chronotropic (B1); vasodilates arterioles of skeletal muscle (B2)
Pulmonary: bronchodilation
Used: stimulates cardiac emergencies

39
Q

dobutamine

A

B1-selective

  • increases CO and rate- more +ionotropic effects
  • treats increased CO in CHF
  • racemic mix cancels out alpha (not as strong as isoproterenol)
40
Q

albuterol
perbuterol
terbutaline

A

Beta2 short-acting bronchodilators

41
Q

Salmeterol

Formoterol

A

Beta2 long-acting bronchodilators

42
Q

therapeutic uses of adrenergic agonists

A

shock, hypotension, cardiac arrest, local vasoconstriction, narcolepsy, weight reduction, ADHD

43
Q

What are the 2 exceptions of sympathetic innervation? (hint: sweat glands and renal)

A

Exception: Sympathetic innervation of sweat glands is cholinergic

Exception : Sympathetic innervation of renal vasculature is dopaminergic (dopamine)

44
Q

Define sympathomimetic

A

Adrenergic drug which acts directly on adrenergic receptor (alpha, beta), activating it
Another term to describe adrenergic agonists

Pharm for midterm (5 decks)

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