Pharm 21 Vascular Tone Flashcards
MOA:
Donates NO–>activates guanylyl cyclase and increases dephosphorylation of myosin light chain in vascular smooth muscle= vasodilation
Nitrates, Inhaled NO, Sodium Nitroprusside
Tx: short acting (sublingual), long acting (oral) angina
Isosorbide dinitrate
Consideration:
venous dilation greater than arteriolar
isosorbide dinitrate
Organic Nitrates (5)
isosorbide dinitrate, isosorbide 5-mononitrate, nitroglycerin, sodium nitroprusside, inhaled NO gas
Tx:
prophylaxis angina, chronic IHD
isosorbide 5-mononitrate
consideration:
100% bioavailable orally
Isosorbide 5-mononitrate
Tx:
Agnina attacks, chronic IHD, acute heart failure
Nitroglycerin (NTG)
Consideration: Ergotamine may oppose coronary vasodilation of nitrates
NTG
Tx:
HTN emergency, severe cardiac failure, Ergot alkaloid toxicity
Sodium nitroprusside
Consideration: cyanide toxicity (thiocyanate toxicity)
sodium nitroprusside
Tx:
Neonatal respiratory failure
inhaled NO gas
Consideration:
selectively dilates pulmonary vasculature
inhaled NO gas
Phosphodiesterase Type V (PDE5) Inhibitors (3)
Sildenafil, Vardenafil, Tadalafil
MOA: Inhibit PDE5 (enzyme for converting cGMP to GMP) cGMP normally relaxes vessels= dilation (PDE5 inactivate cGMP-->GMP)
Phosphodiesterase Type 5 (PDE5) Inhibitors
Tx:
Erectile dysfunction
PDE5 inhibitors
consideration:
concomitant use of organic nitrate vasodilators= Hypotension
PDE5 inhibitors
Calcium channel blockers (CCB)
Dihydropyridines: Nidfedipine, amlodipine, felodipine, clevidipine; Benzothiazepine: Diltiazem; Phenylalkylamine: Verapamil
MOA:
Block influx of calcium (L-type channels)= no actin myosin cross bridge formation= no contraction= dilation
Calcium channel blockers
Tx:
Angina, HTN, Raynaud’s phenomenon, Pre-eclampsia
Dihydropyridines (CCB)
Considerations:
Amlodipine has higher bioavailability, longer peak time, slower metabolism
Dihydropyridines (CCB)
Tx Same as Phenylalkylamine):
Prinzmetal angina, HTN, A-fib, Paroxysmal SVT
Benzothiazepine: Diltiazem
Benzothiazepine medication name
Diltiazem
Dihydropyridine medications name (4)
Nidfedipine, Amlodipine, Felodipine, Clevidipine
Tx (same as Dihydropyridines):
Prinzmetal angina, HTN, A-fib, Paroxysmal SVT
Phenylalkylamine
Consideration:
concomitent alcohol use will increase alcohol concentration
Phenylalkylamine
Phenylalkylamine medication name
Verapamil
MOA:
Open ATP modulated K+ channels to hyperpolarize membrane= decreased influx of calcium= dilation
K+ channel openers
K+ channel opener medications (4)
minoxidil, pinacidil, nicorandil, cromakalim
Tx:
Severe/refractory HTN; male alopecia (topical minoxidil)
K+ channel openers
Considerations:
typically used with B-blockers and diuretic
K+ channel openers
MOA:
Block avtivation of endothelin receptors (ETa,b)
Endothelin Receptor Antagonists
Tx:
Pulmonary HTN
Endothelin Receptor Antagonists
Considerations:
hepatotoxicity (monthly monitoring), No pregnancy use
Endothelin Receptor Antagonists
Endothelin Receptor Antagonist medications (2)
Bosentan, Ambrisentan
MOA:
Arteriolar vasodilator
Hydralyzine
Tx:
Severe HTN, Severe Heart failure
Hydralyzine
considerations:
cause reversible SLE, Usually used with Isosorbide dinitrate; morbity/mortality benefits for blacks wtih advanced heart failure
Hydralyzine
a-1 Adrenergic Antagonist medications (3)
Prazosin, Doxazosin, Terazosin
B-Adrenergic Antagonist medications (3)
Propanolol (nonselective), Atenolol, Metoprolol (B1-selective)
ACE Inhibitor medications (3)
Captopril, Lisinopril, Enalopril
AT1 REceptor Antagonist medications (2)
Losartan, Valsartan
MOA:
Inhibit cleavage of Angiotensin (AT) I to ATII by ACE; Inhibit defradation of bradykinin by kininase II
ACE Inhibitors