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SBL (Skin, Blood, Lymph) Exam 1 and 2 > Lecture 4: Adrenergic Drugs > Flashcards

Lecture 4: Adrenergic Drugs Flashcards

1
Q

What are two Alpha Agonist drugs? (PC) What receptors are they specific for?

A

phenylephrine a1 > a2

clonidine a2 > a1

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2
Q

What are two mixed Alpha/Beta Agonist drugs? (NE) What receptors do they like to bind to?

A

norephinephrine and epinephrine

NE –> a1 = a2 and B1&raquo_space; B2
E –> a1 = a2 and B1 = B2

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3
Q

What are three Beta Agonist drugs? (DIA) What receptors to they utilize?

A

dobutamine –> B1 > B2

isoproterenol –> B1 = B2

albuterol –> B2 > B1

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4
Q

What indirect adrenomimetic drug inhibits the re-uptake of dopamine and norephinephrine?

A

cocaine

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5
Q

What two indirect adrenomimetic drugs are inhibitors of MAO? (SP)

A

selegiline and phenelzine

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6
Q

What three indirect adrenomimetic drugs reverse norepinephrine and dopamine mechanisms, and increase their release? (AMT)

A

amphetamines, methylphenidate, and tyramine (not a drug)

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7
Q

What drug is a releasing agent AND a direct adrenergic receptor agonist?

A

ephedrine

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8
Q

What G protein does the alpha 1 receptor type use and what are its effects?

A
  • uses Gq

- inc. IP3 and DAG common to all

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9
Q

What G protein does the alpha 2 receptor type use and what are its effects?

A
  • uses Gi

- dec. cAMP common to all

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10
Q

What G protein does the beta receptor type use and what are its effects?

A
  • uses Gs

- inc. cAMP common to all

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11
Q

What G proteins do dopamine receptors D1 and D2 use and what are their effects?

A

D1 uses Gs = inc. cAMP

D2 uses Gi = dec. cAMP

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12
Q

What is epinephrines selectivity for receptors vs norephinephrines selectivity for receptors?

A

E –> a1 = a2 and B1 = B2

NE –> a1 = a2 and B1&raquo_space; B2

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13
Q

What is epinephrines effect on cardiac function and what receptor does it use?

A
  • uses B1

- inc. force of contraction, HR, and AV node conductivity

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14
Q

What is epinephrines effect on vascular tone and what receptors does it use?

A
  • uses B2 and a1

- inc. systolic BP, may dec. diastolic BP and TPR, mean arterial pressure stays the same

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15
Q

What receptor type, when stimulated, inc. renin release?

A

B1 (mainly found on heart and juxtaglomerular cells)

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16
Q

What do D1 and D2 receptors do when activated?

A 
D1 = dilates renal blood vessels (on SM)
D2 = modulate transmitter release from nerve endings
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17
Q

What do B3 receptors do when activated? (2)

A

on bladder (relax detrusor muscle) and on fat cells (activates lipolysis)

18
Q

What are epinephrines 2 effects on the respiratory system and what receptors does it bind to?

A
  1. relaxes bronchial muscles (B2)

2. dec. bronchial secretion/congestion (a1)

19
Q

What are the 3 locations for B2 receptors and what are their actions? (SSL)

A
  1. Resp/uterine/vascular SM - relaxation
  2. Skeletal muscle - potassium uptake
  3. Liver - glycogenolysis and gluconeogenesis
20
Q

What are the 4 locations for a1 receptors and what are their actions? (VPPH)

A
  1. most vascular SM (innervated) - contraction
  2. pupillary dilator muscle - contraction
  3. prostate - contraction
  4. heart - inc. force of contraction
21
Q

What are the 5 locations for a2 receptors and what are their actions? (NPNVF)

A
  1. Neurons - modulate transmitter release
  2. Platelets - aggregation
  3. nerve terminals - inhibit transmitter release
  4. some vascular SM - contraction
  5. fat cells - inhibit lipolysis
22
Q

What is norepinephrines effect on the heart and blood vessels?

A

potent cardiac stimulate (reduces HR –> baroreflex) and vasoconstrictor

  • inc. peripheral vascular resistance and BP
23
Q

What are the two functions of phenylephrine?

A
  • effective mydriatic (pupil dilator) and decongestant

- causes severe vasoconstriction, BP inc., and bradycardia (baroreflex in response)

24
Q

What is major function of clonidine?

A
  • central effect on presynaptic a2 receptors in lower brainstem that helps regulate NE release
  • dec. sympathetic outflow, reduce BP, cause bradycardia
  • local application = vasoconstriction
25
Q

What are the two functions of isoproterenol?

A
  • inc. cardiac output (B1)

- vasodilator and bronchodilation (B2)

26
Q

What are the functions of dobutamine and albuterol?

A

D - potent inotropic action (less prominent chronotropic effect compared to isoproterenol)
- some a1 activity (- = agonist, + = antagonist)

A - bronchodilation

27
Q

What is the importance of Tyramine?

A
  • does NOT cross BBB (hydrophilic, unlike rest of indirect drugs)
  • elevates systolic blood pressure (intravenously) and is used in pressor tests to evaluate peripheral adrenergic function
28
Q

What are common adverse effects of indirect acting lipophilic drugs on the central nervous system?

A
  • insomnia, lack of appetite, anxiety, paranoia, convulsions and hemorrhagic stroke
29
Q

What are two non-selective alpha receptor antagonists? (PP)

A

phentolamine (reversible competitive; short acting)

phenoxybenzamine
- non-competitive, irreversible; long acting

30
Q

What are 3 a1 receptor selective antagonists? (PTD)

A

prazosin, tamsulosin, doxazosin

31
Q

What are 2 mixed blocker antagonists? (LC)

A

Labetalol
Carvedilol

  • both are B and a1 antagonists
32
Q

What are 3 B1 and B2 blockers? (PNP)

A

propranolol, pindolol, nadolol

33
Q

What are 4 B1 selective blockers? (MBAA)

A

metoprolol, betaxolol, acebutolol, atenolol

34
Q

What indirect acting antiadrenergic drug blocks norepinephrine release and which one is an inhibitor of tyrosine hydroxlase?

A
  1. guanethidine

2. metyrosine

35
Q

What suffix do all direct a1 receptor antagonists end in?

A

-osin

36
Q

What 3 Beta blockers are full antagonists? (ANP)

A

atenolol, nadolol, propranolol

37
Q

What 3 Beta blockers are partial agonists? (ALP) What is there an increase in with use?

A

acebutolol, labetalol, pindolol

  • inc. in VLDL compared to HDL
38
Q

What 2 Beta blockers are inverse agonists? (BM)

A

betaxolol, metoprolol

39
Q

What two Beta Blockers are used to treat Heart Failure? (MC)

A

metoprolol, carvedilol

  • contraindicated in acute/severe congestive heart failure
40
Q

What Beta Blocker is used to treat glaucoma?

A

betaxolol (no local anesthetic activity)

  • propranolol NOT used
41
Q

What Beta Blocker is used to treat Hyperthyroidism?

A

propranolol

  • see excessive catecholamine action on the heart
42
Q

What would you switch to if a patient on beta blockers experienced either adverse cardiovascular effects or was chronically using beta blockers?

A
  • switch to partial agonist

- see an inc. in VLDL with chronic beta blocker use

SBL (Skin, Blood, Lymph) Exam 1 and 2 (22 decks)

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