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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
Verapamil (non DHP) can increase _____ blood level
Digoxin
26
A. DHP is an additive with ______ B. Non DHP is an additive with _____
A. Vasodilators B. Cardiac depressants + HTN drugs
27
Potassium channel openers = 2 of them
Diazoxide | Minoxidil
28
MOA for Diazoxide + Minoxidil
Opens potassium channel in smooth muscle
29
Diazoxide Increased potassium permeability ________ smooth muscle membrane?
Hyperpolarizes
30
Diazoxide (Potassium channel opener) How long acting? How is it usually administered?
Long acting = 4-12 hours after injection - 3-4 injections, 5-15 minutes apart as needed - sometimes via IV
31
Diazoxide Adverse effects? Hypotensive effects greater in? How to avoid these problems?
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
Minoxidil effect on smooth muscle membrane ?
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
Side Effects of Minoxidil
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
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
Use in combination with a b-blocker and loop diuretic
35
Clinical uses of Minoxidil (potassium channel opener)
- LT outpatient therapy of severe HTN **** use to stimulate hair growth (ex. Rogaine)
36
Fenoldopam (Dopamine agonist) MOA
Agonist for dopamine D1 receptors
37
Adverse effects of Fenoldopam
Tachycardia Headache Flushing
38
Fenoldopam contraindications
Avoid in patients with glaucoma --- increases intraocular pressure
39
Clinical use of fenoldopam
HTN emergencies | Peri- + postoperative HTN
40
Nitric Oxide modulators = 3 of them
Hydralazine Sodium Nitroprusside Organic Nitrates
41
MOA for Hydralazine? Effects?
Stimulate release of NO from endothelium = increased cGMP | - cause dilation of arterioles, but NOT VEINS + reflex tachycardia
42
Side Effects of Hydralazine
``` Headache Nausea Anorexia Palpitations Sweating Flushing ``` Rare peripheral neuropathy + drug fever
43
Contraindications for Hydralazine
Dont use in pts with ischemia Heart disease, reflex tachycardia - sympathetic stimulation can cause angina + ischemic arhythmias
44
Clinical uses for hydralazine
- LT outpatient therapy of HTN + HTN emergencies - combination with nitrates = effective in heart failure - used for HTN in pregnancy (with methyldopa)
45
Sodium Nitroprusside MOA and effects
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
How is Sodium nitroprusside administered?
Rapid metabolsim = short duration of effect Given via IV should Monitor bp!
47
Side Effects of Sodium Nitroprusside
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
Clinical use of Sodium nitroprusside
HTN emergecy | Acute decompensated heart failure
49
Organic Nitrates - two types
Nitroglycerin + isosorbide dinitrate
50
MOA for organic nitrates and Effect
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
Metabolism of Organic nitrates
- 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
How to get tolerance to organic nitrates Compensatory response to get tolerance? How to avoid?
Via continuous exposure Compensatory responses - tachycardia - increased cardiac contractility - rentension of Na + H20 - best to use after 8 hours to avoid tolerance
53
Side effects of organic nitrate usage?
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
Contraindications for nitrogen oxide
Increased intracranial pressure | Remove transdermal patches if using external defibrillators
55
Drug-drug interactions btw organic nitrates and ____
Synergistic hypotension if use PDE5 inhibitors (sildenafil, tadalafil, vardenafil)

Renal 2 Final - Pharm (4 decks)

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