Antianginals Flashcards
Nitrates– effects low vs high dose
Low dose: increase venous capacitance, reduce preload
High dose: Arterial dilation, decrease PVR and BP (afterload). Dilates epicardial coronary vessels
Nitrates indication
All Type of Angina
Acute Angina Attack & Prophylaxis
Nitrates MOA
Biotransformation NO
*in mitochondria
Activation of Guanylate Cyclase [cGMP] Activation of MLC Phosphatase Smooth Muscle Relaxation
Nitrates metabolism?
Isosorbide Mono/Dinitrate are prodrugs, activated by 1st pass
Avoid continuous exposure, must not use 10-14 hrs/day
Nitrates should be given as (A) due to extensive (B)
A- sublingual/spray
B- 1st pass metabolism
Nitrates are activated by (A) therefore they are less effective in which population (B)?
A- ALDH2 and P450 dehydrogenase
B- Asians with SNP in ALDH2– those who get asian flush
Nitrates should not be taken with (A) due to (B)
A- Sildenafil (viagra)
B- risk for critical hypotension
BBlockers are indicated for…
Stable or Unstable Angina
NOT variant Angina
Selective BB? Non selective BB?
Nonselective:
Propranolol
Nadolol
Timolol
Selective: Acebutolol Atenolol Metoprolol Labetalol Pindolol Carvedilol Nebivolol
Effects of BBlockers
decrease HR /BP
decrease Exercise-induced increase in HR & Contractility
Block Sympathetics
Prevent Reflex Tachycardia from Nitrates
Nitrates can cause reflex (A), which can be prevented with (B)
A- tachycardia
B- BBlockers
Lipid soluble BBlockers are eliminated by…
liver
propanolol
metoprolol
Hydrophilic BBlockers are eliminated by …
kidneys
nadolol
atenolol
Beta 3 agonist and Beta 1 antagonist?
Nebevolol
renal elimination
Beta 3 agonist and Beta 1 antagonist?
Nebevolol
renal elimination
nonselective BBlocker/a Blocker
Labetolol/carvedilol
decrease IP3, decrease Ca release to cause vasodilation
Indications for Ca Channel blockers
Stable or Variant Angina
“-pine” = dyhydropyridine
Ca channels are different splice variants b/w vascular smooth muscle and heart
Examples of Ca channel blockers
Dilitazem
Verapamil
-PINE = dihydropyridines amiodipine nicardipine nifedipine nimodipine
MOA of Diltiazam and Verampamil?
Selective Antagonist for Heart:
Activity of Voltage Dependent Ca++ Channel Activity
(L-type channels)
Decrease HR
Ca Channel blockers are metabolized by …
CYP3A4- many interactions!
Ca channel blockers AE
Diltiazem
Verampamil
Bradycardia, AV Node conduction, - inotropy, Edema/Headache, Constipation
Nicardipine is an example of a (A) which is a (B) antagonist for (C) and acts on (D) to cause (E)
A- Ca Channel blocker/ dihydropyridine
B- selective
C- arterioles
D- Ca Ltype channels
E- vasodilation
Dihydropyridines systemic effects
decrease PVR and BP, Decrease afterload
Dihydropyridines AE
Could Cause Reflexive Tachycardia, in reponse to BP
Fewer adverse effects with Long Acting (Amlodipine) or Sustained Release (Nifedipine)
*Long-acting: Peripheral Edema, Headache
*Short-acting: Hypotension, Reflex tachycardia, MI risk, & peripheral edema, headache
