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Renal 2 Final - Pharm > Kruse - Vasodilators > Flashcards

Kruse - Vasodilators Flashcards

1
Q

Dihydropyridines (DHPs) are _____ blockers

A

Calcium channel

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2
Q

Name the DHPs = 7 of them
What do they end in?
ANC FINN

A 
Amlodipine*
Nifedipine*
Clevidipine
Felodipine
Isradipine
Nicardipine
Nisoldipine
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3
Q

Non-DHPs = 2 of them

A

Diltiazem

Verapamil

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4
Q

Potassium Channel Openers = 2 of them

A

Diazoxide

Minoxidil

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5
Q

Dopamine Agonists = 1

A

Fenoldopam

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6
Q

Nitric Oxide Modulators = 3 of them

A

Hydralazine
Nitroprusside
Organic Nitrates - Nitroglycerin + Isorbide dinitrate

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7
Q

DHP MOA?

A

Nifedipine, Amlodipine = prototypes

  • block L-type Ca+ channels in vasculature > cardiac channels
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8
Q

Non DHP MOA?

A

Prototype = verapamil + Diltiazem

MOA: nonselective block of vascular + cardiac L-type calcium channels

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9
Q

Calcium channel blockers (CCB)

A
  • dihydropyridines (DHPs) + non DHPs
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10
Q

Do DHP and non-DHP bind to same or different sites on the L-type channel proteins? What is the effect?

A

Different

Causes differences in effects on vascular vs. cardiac tissue responses + different kinetics of action at the receptor

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11
Q

CCBs bind effectively to what kind of channels? What does it do?

A
  • Open and inactivated channels

- reduces the frequency of opening in response to depolarization

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12
Q

Effect of CCB on smooth muscle?

A

Cause vasodilation = decrease peripheral resistance

  • arterioles = more sensitive than veins
  • relaxed arteriolar smooth m. = decreased O2 demand by heart
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13
Q

Effect of CCB on cardiac m.

A
  • reduced contractility in heart
  • decrease in SA node pacemaker rate
  • decreased conduction velocity

Note:

  • non DHP have MORE cardiac effect than DHPs
  • DHPs block cardiac channels in smooth muscle at lower concentrations, so cardiac effect is negligible
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14
Q

CCB Metabolism (pharmacokinetics)

Are they active when taken orally?

A

Yes

  • high first pass metabolism
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15
Q

Which CCBs are also taken via IV = 4 of them

A

Nifedipine
Clevidipine
Verapamil
Diltiazem

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16
Q

Which CCB has a long half life?

A

Amlodipine = 35-50 hours

Other CCBs have 2-12 hours half life

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17
Q

Drug interaction between non-DHP CCBs and ______ is dangerous.

A

B-blockers

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18
Q

Are CCBs well tolerated?

A

Yes

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19
Q

Side Effects of DHPs?

A 
Hypotension
Dizziness
Headache
Peripheral edema
Flushing
Tachycardia
Rash
Gingival hyperplasia
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20
Q

Short acting or long acting DHPs should NOT be used for chronic HTN?

A

Short acting - do not use!

  • preferred = long acting + slow release DHPs
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21
Q

Side effects for Non-DHPs

A 
Dizziness
Headache
Peripheral edema
Constipation* --- especially verapamil!!
AV block
Bradycardia
HF
Lupus-like rash -- with diltiazem
Pulmonary edema
Coughing 
Wheezing

** verapamil > diltiazem = slow HR, slow AV conduction, cause heart block

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22
Q

Non DHPs are contraindicated in?

IMPORTANT!

A

Ppl taking b-blockers

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23
Q

Which DHP does NOT decrease AV conduction

A

Nifedepine

  • can be used safely than non-DHPs in presence of AV conduction abnormalities
24
Q

CCBs are not indicated for ____. But which 2 drugs can b used for another indication, such as ANGINA or HTN?

A

Use in heart failure pts

Can use amlodipine or felodipine

25
Q

Verapamil (non DHP) can increase _____ blood level

A

Digoxin

26
Q

A. DHP is an additive with ______

B. Non DHP is an additive with _____

A

A. Vasodilators

B. Cardiac depressants + HTN drugs

27
Q

Potassium channel openers = 2 of them

A

Diazoxide

Minoxidil

28
Q

MOA for Diazoxide + Minoxidil

A

Opens potassium channel in smooth muscle

29
Q

Diazoxide

Increased potassium permeability ________ smooth muscle membrane?

A

Hyperpolarizes

30
Q

Diazoxide (Potassium channel opener)

How long acting?
How is it usually administered?

A

Long acting = 4-12 hours after injection

  • 3-4 injections, 5-15 minutes apart as needed
  • sometimes via IV
31
Q

Diazoxide

Adverse effects?

Hypotensive effects greater in? How to avoid these problems?

A

Excessive hypotension can cause stroke + MI
Hypoglycemia in pts with renal sufficiency
Cause Na + H20 retention (not a problem b/c short duration of use)

  • hypotensive effects greater in patients with renal failure (b/c less protein binding) And pts taking b-blockers to prevent reflex tachycardia
  • avoided in pts with ischemic heart disease –> risk for angina, ischemia, Cardiac failure
  • should give smaller doses
32
Q

Minoxidil effect on smooth muscle membrane ?

A

Increases potassium permeability = hyperpolarization of smooth muscle = reduced probablity of contraction

Dilation of arterioles, but NOT VEINS
- more efficent than hydralazine (a NO modulating drug)

33
Q

Side Effects of Minoxidil

A

Headache
Sweating
Hypertrichosis (abnormal hair growth)

Effects more than with hydralazine (NO modulator)

  • *associated with reflex sympathetic stimulation
    • increased Na + H20 retention causes:
  • tachycardia
  • palpitations
  • angina
  • edema
34
Q

How to avoid the following effects of Minoxidil?

Effects more than with hydralazine (NO modulator)

  • *associated with reflex sympathetic stimulation
    • increased Na + H20 retention causes:
  • tachycardia
  • palpitations
  • angina
  • edema
A

Use in combination with a b-blocker and loop diuretic

35
Q

Clinical uses of Minoxidil (potassium channel opener)

A
  • LT outpatient therapy of severe HTN

** use to stimulate hair growth (ex. Rogaine)

36
Q

Fenoldopam (Dopamine agonist) MOA

A

Agonist for dopamine D1 receptors

37
Q

Adverse effects of Fenoldopam

A

Tachycardia
Headache
Flushing

38
Q

Fenoldopam contraindications

A

Avoid in patients with glaucoma — increases intraocular pressure

39
Q

Clinical use of fenoldopam

A

HTN emergencies

Peri- + postoperative HTN

40
Q

Nitric Oxide modulators = 3 of them

A

Hydralazine
Sodium Nitroprusside
Organic Nitrates

41
Q

MOA for Hydralazine? Effects?

A

Stimulate release of NO from endothelium = increased cGMP

- cause dilation of arterioles, but NOT VEINS + reflex tachycardia

42
Q

Side Effects of Hydralazine

A 
Headache
Nausea
Anorexia
Palpitations
Sweating
Flushing

Rare peripheral neuropathy + drug fever

43
Q

Contraindications for Hydralazine

A

Dont use in pts with ischemia Heart disease, reflex tachycardia

  • sympathetic stimulation can cause angina + ischemic arhythmias
44
Q

Clinical uses for hydralazine

A
  • LT outpatient therapy of HTN + HTN emergencies
  • combination with nitrates = effective in heart failure
  • used for HTN in pregnancy (with methyldopa)
45
Q

Sodium Nitroprusside MOA and effects

A

Release NO = increased cGMP

  • cause dilation of arterial + venous vessels
  • decrease peripheral vasc. Resistance + venous return
  • in absence of heart failure, bp decreases, but CO does NOT change
  • when CO = low due to HF, CO increases due to afterload reduction
46
Q

How is Sodium nitroprusside administered?

A

Rapid metabolsim = short duration of effect
Given via IV
should Monitor bp!

47
Q

Side Effects of Sodium Nitroprusside

A

hypotension
Cyanide + thiocyanate released during metabolism
– no problem if drug used for short time

Long term use (few days) = metabolic acidosis, arrhythmias, excessive hypotension, death

48
Q

Clinical use of Sodium nitroprusside

A

HTN emergecy

Acute decompensated heart failure

49
Q

Organic Nitrates - two types

A

Nitroglycerin + isosorbide dinitrate

50
Q

MOA for organic nitrates and Effect

A

Release NO via enzymatic metabolism

Effect

  • relax smooth muscles (veins > arteries)
  • no effect on cardiac or skeletal muscle
  • decrease heart size
  • CO reduced if no HF
  • decrease platelet aggregation
51
Q

Metabolism of Organic nitrates

A
  • High first pass effect = low bioavailability
  • given sublingually to avoid first-pass
  • blood level reached in 15-30 min
  • if want longer duration of action —> taken orally, transdermallly, and buccally
52
Q

How to get tolerance to organic nitrates

Compensatory response to get tolerance?
How to avoid?

A

Via continuous exposure

Compensatory responses

  • tachycardia
  • increased cardiac contractility
  • rentension of Na + H20
  • best to use after 8 hours to avoid tolerance
53
Q

Side effects of organic nitrate usage?

A

Orthostatic hypotension
Syncope
Throbbing headache

Due to

  • decreased NO release
  • decreased availabilty of sulfhydryl donors
  • increased Oxygen free radicals
  • Decreased calcitonin gene related peptide (CGRP) availability
54
Q

Contraindications for nitrogen oxide

A

Increased intracranial pressure

Remove transdermal patches if using external defibrillators

55
Q

Drug-drug interactions btw organic nitrates and ____

A

Synergistic hypotension if use PDE5 inhibitors (sildenafil, tadalafil, vardenafil)

Renal 2 Final - Pharm (4 decks)

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