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PHRM 844 Exam 5 LOs > Vasoconstrictors/Vasodilators > Flashcards

Vasoconstrictors/Vasodilators Flashcards

1
Q

What receptors are the molecular basis that causes vascoconstriction?

A

GPCRs coupled to vasoconstriction: a1 adrenergic

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2
Q

what drugs are alpha1 receptor agonists?

A
  1. epinepherine
  2. phenylephrine
  3. midodrine
  4. droxidopa
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3
Q

what do we use for an adjunct to local anesthetics that can help reduce blood flow to injection site?

A

epinepherine

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4
Q

what drug do we use for homeostasis during surgery?

A

epinepherine

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5
Q

what are the direct-acting a1 receptors ?

A

phenylepherine

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6
Q

what is an indirect acting agent for a1?

A

peudoephederine

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7
Q

what are the partial agonists for a1 receptors?

A

naphazoline, oxymetazoline, tetrahydrozoline

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8
Q

why does increasing K+ channel openings relax vascular smooth muscle?

A
  1. K+ sets membrane potential
  2. longer channels open the closer to equilibrium
  3. The closer to equilibrium the harder it is to depolarize enough to open VOLTAGE_GATED Ca2+ Channels
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9
Q

what is minoxidil? What does it do?

A

K+ Channel agonist/open
- promotes hair growth (hypertrichosis)

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10
Q

what drug classes are vasodilators?

A
  1. Cyclic GMP Modulators
  2. K+ Channel agonists
  3. Endothelin receptor Agonist
  4. PGI2 analogs - IP receptor agonist
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11
Q

what is diazoxide? what is its use and moa?

A
  1. K+ channel agonist/opener
  2. inhibit release of insulin from Pancreatic B-cells
  3. orally for hypoglycemia to hyperinsulinemia
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12
Q

what is adenosine? What is it used for?

A
  1. binds to A1 (GPCR)
  2. given IV - coronary stress test
  3. also supraventricular arrhythmias
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13
Q

how does adenosine hyperpolarize vascular smooth muscle?

A

GIRK
1. Gby binds and activates GIRK–> conducts K+ and membrane hyperpolarization

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14
Q

what is the nitric oxide-cyclic GMP pathway?

A
  1. eNOs found in vascular endothelium (activated by Ca2+-CAM)
  2. NO diffuses to vascular smooth muscle
  3. guanylate cyclase is found in the vascular smooth muscle
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15
Q

what happens after NO moves to smooth muscle and how does it relax it?

A
  1. NO binds to heme iron group in guanylate cyclase
  2. activates protein kinase G (cGKI)
  3. elevated GMP reduces phosphorylation of myosin LC causing relaxation
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16
Q

how does protein kinase G relax smooth muscle?

A
  1. inhibit L-type Ca2+ channel (Cav1.2)
  2. stim Ca2+ K+ channel (BKca)
  3. decreased myosin phosphatase 1
  4. enhance Ca2+ in ER (phospholamban)
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17
Q

what do organic nitrates do?

A

breakdown to NO (bioactivation)

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18
Q

what are the PK of organic nitrates?

A
  1. given sublingual in tx of acute attacks of angina
  2. tolerance occurs with continuous admin
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19
Q

who had a tolerance to glyceryl trinitrate?

A

munitions workers

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20
Q

what is the PK for glycerol trinitrate?

A

likely accounts for the lack of efficacy of GTN in a large percentage of the Asian population

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21
Q

what is the mechanism of cell damage inititated by hyperglycemia?

A

AGE precursor methylglyoxal inhibits vasorelaxation stimulated by acetylcholine/Nitric Oxide

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22
Q

what does sodium nitroprusside do ?

A
  1. dilates veins and arterioles
  2. limits duration of treatment due to ctructure
23
Q

what is hydralazine and what does it do?

A
  1. dilates arterioles preferentially
  2. interfere with the release of Ca2+ from the ER
24
Q

what does the combo of hydralazine and ISDN do for BiDil?

A

decreased mortality in AA with CHF

25
Q

what is BNP and what does it do?

A
  1. human type B natriuretic peptide
  2. binds and activates membrane-bound guanylate cyclase
26
Q

what is sacubitril and when is it not used?

A
  1. inhibitor of neprilysin (a protease)
  2. prevents breakdown of BNP by enhancing its action
  3. not used with ACE
27
Q

what are the 2 PDE3 cAMP inhibitors? what do they do?

A

amirone and milrinone
1. inhibit the breakdown of cGMP/AMP

28
Q

what fold of difference does cGMP PDE5 have over PDE6?

A

10 fold selectivity inhibition of PDE6 in retina

29
Q

what does the inhibition of PDE6 in retina cause?

A

bluish vision

30
Q

what is the effect for sildenafil on blood flow in the penis?

A

predominent in the corpus cavernosum

31
Q

what is special about levitra compared to other PDE5s?

A
  1. shorter time to onset than viagra
  2. more selective than viagra
32
Q

what is special about cialis compared to the other PDE5?

A
  1. more selective than viagra
  2. longer duration of action than viagra or levitra
33
Q

when is a PDE5 contraindicated?

A

organic nitrates

34
Q

what are the main vasodilators used in PAH?

A

actin neutralizers

35
Q

what are the 3 vasoconstrictor antagonists?

A
  1. bosentan
  2. macitentan
  3. ambrisentan
36
Q

what does bosentan and macitentan have in common?

A
  1. both block ETa and ETb
  2. low MW receptor antagonsits
37
Q

what is special about ambrisentan?

A

blocks only ETa

38
Q

what are vasoconstircotr antagonsits approved for and contraindicated for?

A
  1. approved for pulmonary arterial HTN
  2. contraindicated in pregnancy and hepatotoxicity (bosentan only)
39
Q

what do prostacyclin analogs do? where is it produced?

A
  1. relax pulmonary vascular SM
  2. PGI2 found in endothelium
40
Q

what are the different drugs in the prostacyclin class and what is their dosage form?

A
  1. PGI2 –> IV
  2. treprostinil –> oral, IV
  3. lloprost –> inhalation
  4. selexipag –> oral (bid), IV
41
Q

what is adempas and its mechansim and metabolism?

A
  1. allosteric activator of sGC
  2. increases cGMP concentration in VSM
  3. substrate for P-gp, CYP1A1, 3A
42
Q

what drug is this?

A

minoxidil

43
Q

what drug is this?

A

diazoxide

44
Q

what drug is this?

A

SNP

45
Q

what drug is this?

A

hydralazine

46
Q

what drug is this?

A

sacubitril

47
Q

what class is this?

A

PDE3

48
Q

what drug is this?

A

tadalafil

49
Q

what drug is this?

A

sildenafil

50
Q

what drug is this?

A

vardenafil

51
Q

what drugs is this? what class?

A

vasoconstricotr antagonsit
- bosentan and macitentan

52
Q

what drug is this?

A

ambrisentan

53
Q

what drug class is this?

A

prostacyclin analogs

54
Q

what drug is this?

A

riociguat

PHRM 844 Exam 5 LOs (7 decks)

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