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Pharm - Sam > pharm: adrenergic receptors > Flashcards

pharm: adrenergic receptors Flashcards

1
Q

what are some examples of adrenergic direct acting agonists? give 2 overarching types

A
  1. Catecholamines
  2. Non-catecholamines
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2
Q

what are examples of catecholamines that are direct acting adrenergic agonists?

A

epinephrine

norepinephrine

isoproterenol

dopamine

dobutamine

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3
Q

why do catecholamines need to be given parenterally (taken by a route other than through the mouth ie. IM or IV)?

what affects a catecholamines efficiency?

A

catecholamines are rapidly metabolized in the gut, liver, and other tissues by monoamine oxidase (MAO) and catechol-O-methyltransferase (COMT)

Catecholamines effects depend on affinity and specificity for type of Adrenergic receptor

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4
Q

Epinephrine (direct adrenergic agonist)

  • effects on body (in various receptors)
  • when is it used?
A

can bind to ALL the adrenergic receptors

vasoconstriction & increase BP (ALPHA 1)

cardiac stimulation (BETA 1)

bronchodilation & skeletal muscle vasodilation (BETA 2)

used in anaphylactic shock and cardiac arrest

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5
Q

Norepinephrine (direct adrenergic agonist)

  • effect on body (various receptors)?
  • when is it used?
A

vasoconstriction & increase BP (A1)

cardiac stimulation (B1)

used in hypotension and shock

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6
Q

Isoproterenol (direct adrenergic agonist)

  • effect on body?
  • when is it used?
A

cardiac stimulation (B1)

bronchodilation (B2)

used to tx. asthma, AV block, and bradycardia

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7
Q

Dopamine (direct adrenergic agonist)

*what is it a precursor to?

  • effect on body?
  • what is it used for?
A

*precursor to epi, NE

  • renal vasodilation (D1)
  • cardiac stimulation (B1)
  • increase BP (A1)
  • used to tx. cardiogenic shock, septic shock, heart failure, and adjunct to fluid administration in hypovolemic shock
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8
Q

Dobutamine (direct adrenergic agonist)

  • affinity for what receptor?
  • what is it used for?
A
  • highest affinity for B1 receptor
  • less activity at A1 receptor
  • used to tx. cardiogenic shock, cardiac arrest, and heart failure
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9
Q

what are examples of non-catecholamines that are direct acting adrenergic agonists?

A

phenylephrine

albuterol

clonidine

terbutaline

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10
Q

Phenylephrine (direct adrenergic agonist)

  • effect on body?
  • what is it used for?
A

(A1) effects:

  • vasoconstriction
  • increase BP
  • mydriasis
  • used as nasal decongestant, ocular decongestant, and maintenance of BP during surgery
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11
Q

Albuterol (direct adrenergic agonist)

  • effect on body?
  • what is it used for?
A

Bronchodilation (B2)

used in asthma

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12
Q

Clonidine (direct adrenergic agonist)

  • effect on body?
  • what is it used for?
A
  • inhibits NE release from nerve terminal of postganglionic neuron (feedback inhibition - A2)
  • can have effects in CNS (sedation)
  • used to treat chronic hypertension
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13
Q

Terbutaline (direct adrenergic agonist)

  • effect on body?
  • what is it used for?
A
  • Bronchodilation and uterine relaxation (B2)
  • used to tx. asthma and premature labor (tocolytic)

SIDE NOTE – tocolytic = anti-contraction med used to prevent premature labor

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14
Q

what are some examples of adrenergic indirect acting agonists? (3)

A

amphetamine

cocaine

tyramine

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15
Q

Amphetamine (indirect adrenergic agonist)

(THINK ADDERALL)

A
  • increase release of NE & DA from sympathetic NS neurons
  • vasoconstriction
  • cardiac stimulation
  • increase BP
  • penetrates CNS – CNS stimulation (increases mood and alertness, but decreases appetite)
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16
Q

Cocaine (indirect adrenergic agonist)

A
  • local anesthetic
  • stimulates sympathetic NS by blocking reuptake of NE & DA in the parasymp & symp NS –> similar effects as ampetamine
17
Q

Tyramine (indirect adrenergic agonist)

A
  • normal by-product of tyrosine metabolism in body
  • found in high conc. in fermented foods (cheese, beer, red wine, cured meats - salami & pepperoni)
  • indirect sympathomimetric b/c it causes the release of stored catecholamines
  • (SIDE NOTE: SYMPATHOMIMETRIC means: mimic the effects of transmitter substances of the sympathetic nervous system such as catecholamines)*
  • normally metabolized by MAO –> so if taking MAO inhibitor must avoid tyramine-containing food
18
Q

what is a mixed acting adrenergic agonist?

give an example of one

A
  • works both directly and indirectly
  • causes vasoconstriction by binding to A1
  • increases release of NE from sympathetic neurons
  • EX: pseudoephrine – nasal decongestant
19
Q

what are the types of adrenergic antagonists?

A

alpha adrenergic receptor antagonists (a-blockers)

beta adrenergic receptor antagonists (b-blockers)

-can be nonselective and selective

20
Q

what are nonselective a-blockers?

A

block both a1 and a2 receptors (hence nonselective)

21
Q

what are 2 examples of non-selective alpha-blockers?

A

phenoxybenzamine

phentolamine

22
Q

Phenoxybenzamine (non-selective a-blocker)

A
  • noncompetitive, irreversible
  • tx: hypertensive episodes associated w/ pheochromocytoma

(tumor in adrenal gland that secretes catecholamines)

23
Q

Phentolamine (non-selective a-blocker)

A
  • competitive, reversible
  • Dx and tx hypertensive episodes from pheochromocytoma
  • tx. necrosis and ischemia from extravasations (leakage) of epinephrine
24
Q

what are selective a1-blockers?

how do they work/ what are they used for?

A

“azosin”

  • relax vascular smooth muscle and smooth muscle in bladder and prostate
  • produce vasodilation and decrease BP
  • used to tx hypertension and urinary retention due to benign prostatic hyperplasia (BPH)
25
Q

examples of selective-A1 blockers?

A

doxazoin

prazosin

terazosin

tamsulosin, alfuzosin – only for BPH not for hypertension

26
Q

what are non-selective b- blockers?

  • what they do?
  • what are they used for?
A
  • “olol”
  • block b1 receptors in heart and b2 in smooth muscle, liver, and other tissues
  • B1 blockade: decreases BP, CO, renin release, and aqueous humor selection

-B2 blockade: bronchoconstriction, decreases glycogenolysis, mask signs of hypoglycemia

tx: hypertension, angina, arrythmias, MI, migraine, glaucoma

27
Q

examples of non-selective b-blockers?

A

“olol”

propanolol

nadolol

timolol

28
Q

what are selective B1 blockers?

A
  • selective for B1 receptors (primarily in cardiac tissue)
  • AKA - “cardioselective B-blockers”
  • produce less bronchoconstriction and other B2 receptor mediated effects

Tx: hypertension, angina, MI

29
Q

examples of selective B1 blockers?

A

Atenolol

Metaprolol (Lopressor)

30
Q

what are mixed alpha and beta adrenergic receptor antagonists?

A

block both a- and b- receptors

31
Q

examples of mixed alpha and beta receptor agonists?

A

Carvedilol – tx: hypertension and CHF

Labetalol – tx: hypertension

Pharm - Sam (3 decks)

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