What is the mechanism of action of amlodipine?
Mechanism of Action Amlodipine is a dihydropyridine calcium antagonist (calcium ion antagonist or slow-channel blocker) that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle.
How is amlodipine metabolized?
Amlodipine is extensively metabolized by the liver to inactive metabolites with 10% of the parent compound. The plasma elimination half-life is about 35-50 hours and is consistent with once daily dosing. 60% of metabolites are excreted in the urine.
How does amlodipine work for hypertension?
Amlodipine is a type of medicine called a calcium channel blocker. Like other calcium channel blockers, amlodipine works in high blood pressure by relaxing and widening blood vessels. This lowers your blood pressure and makes it easier for your heart to pump blood around your body.
What is the route for amlodipine?
Amlodipine (Oral Route)
Does amlodipine cause vasodilation?
Dihydropyridines — The dihydropyridines, including nifedipine, isradipine, felodipine, nicardipine, nisoldipine, lacidipine, amlodipine, and levamlodipine are potent vasodilators that have little or no negative effect clinically upon cardiac contractility or conduction.
How does Norvasc work?
How does NORVASC work? NORVASC relaxes your blood vessels, which lets your blood flow more easily and helps lower your blood pressure. Lowering your blood pressure is important because it lowers your risk of having a stroke or heart attack.
Where does amlodipine metabolize?
the liver
Amlodipine is extensively metabolised in the liver (but there is no significant presystemic or first-pass metabolism) and is slowly cleared with a terminal elimination half-life of 40 to 50h. Volume of distribution is large (21 L/kg) and there is a high degree of protein binding (98%).
Is amlodipine metabolized in the liver?
Amlodipine is slowly absorbed, its absolute bioavailability is high, and it is extensively metabolized in the liver.
How long before amlodipine leaves your system?
In other words, it takes about 30 to 50 hours for your body to get rid of half of a dose of amlodipine. It usually takes about five half-lives for a drug to leave your system entirely. For amlodipine, this means the drug will stay in your system for about 10 days after your last dose.
Why is amlodipine given at night?
New research suggests that taking your blood pressure medication at bedtime may more effectively reduce your risk of illness or death due to heart and blood vessel disease. Timing of medication is important because blood pressure follows a daily rhythm. It rises higher during the day and falls at night when we sleep.
Can amlodipine be given IV?
This is the first clinical study demonstrating that the IV administration of amlodipine produces a powerful coronary vasodilatation in subjects with angiographically normal coronary arteries and normal ventricular function, besides its known systemic vasodilating effects.
Is amlodipine a diuretic?
Amlodipine is a calcium channel blocker that relaxes (widens) blood vessels and improves blood flow. Hydrochlorothiazide is a thiazide diuretic (water pill) that helps prevent your body from absorbing too much salt, which can cause fluid retention.
Which is the route of elimination for amlodipine?
Route of Elimination. Amlodipine is extensively metabolized in the liver (but there is no significant presystemic or first-pass metabolism) and is slowly cleared with a terminal elimination half-life of 40 to 50 hr. Volume of distribution is large (21 L/kg) and there is a high degree of protein binding (98%).
How is amlodipine besylate used to treat angina pectoris?
This agent may also modulate multi-drug resistance (MDR) activity through inhibition of the p-glycoprotein efflux pump. Amlodipine besylate is a second generation calcium channel blocker that is used in the therapy of hypertension and angina pectoris.
How does the besylate salt of amlodipine work?
Amlodipine Besylate is the besylate salt of amlodipine, a synthetic dihydropyridine with antihypertensive and antianginal effects. Amlodipine inhibits the influx of extracellular calcium ions into myocardial and peripheral vascular smooth muscle cells, thereby preventing vascular and myocardial contraction.
Are there any pharmacokinetic interactions with amlodipine?
There is no evidence of pharmacokinetic drug interactions. Amlodipine shows linear dose-related pharmacokinetic characteristics and, at steady-state, there are relatively small fluctuations in plasma concentrations across a dosage interval.