Brand Name: AMLOTEK®
Generic name: Amlodipin
Pharmaceutical category: Calcium channel blockers
AMLOTEK® is used with or without other medications to treat high blood pressure. Lowering high blood pressure helps prevent strokes, heart attacks, and kidney problems. AMLOTEK® belongs to a class of drugs known as calcium channel blockers. It works by relaxing blood vessels so blood can flow more easily.
AMLOTEK® is also used to prevent certain types of chest pain (angina). It may help to increase your ability to exercise and decrease the frequency of angina attacks. It should not be used to treat attacks of chest pain when they occur. Use other medications (such as sublingual nitroglycerin) to relieve attacks of chest pain as directed by your doctor.
Mechanism of action:
AMLOTEK® is an angioselective calcium channel blocker and inhibits the movement of calcium ions into vascular smooth muscle cells and cardiac muscle cells which inhibits the contraction of cardiac muscle and vascular smooth muscle cells. AMLOTEK® inhibits calcium ion influx across cell membranes, with a greater effect on vascular smooth muscle cells. This causes vasodilation and a reduction in peripheral vascular resistance, thus lowering blood pressure. Its effects on cardiac muscle also prevent excessive constriction in the coronary arteries.
Negative inotropic effects can be detected in vitro, but such effects have not been seen in intact animals at therapeutic doses. Among the two stereoisomers [R (+), S (–)], the (–) isomer has been reported to be more active than the (+) isomer. Serum calcium concentration is not affected by AMLOTEK®. And it specifically inhibits the currents of L-type Cav1.3 channels in the zona glomerulosa of the adrenal gland.
AMLOTEK® has been studied in healthy volunteers following oral administration of 14C-labelled drug. AMLOTEK® is well absorbed by the oral route with a mean oral bioavailability around 60%; the half-life of AMLOTEK® is about 30 h to 50 h, and steady-state plasma concentrations are achieved after 7 to 8 days of daily dosing. In the blood it has high plasma protein binding of 97.5%. Its long half-life and high bioavailability are largely in part of its high pKa (8.6); it is ionized at physiological pH, and thus can strongly attract proteins. It is slowly metabolized in the liver by CYP3A4, with its amine group being oxidized and its side ester chain being hydrolyzed, resulting in an inactive pyridine metabolite. Renal elimination is the major route of excretion with about 60% of an administered dose recovered in urine, largely as inactive pyridine metabolites. However, renal impairment does not significantly influence AMLOTEK® elimination. 20-25% of the drug is excreted in the faeces.
AMLOTEK® is contraindicated in dihydropyridine hypersensitivity. It can couse liver damage.
Several drugs interact with AMLOTEK® to increase its levels in the body. CYP3A inhibitors, by nature of inhibiting the enzyme that metabolizes AMLOTEK®, CYP3A4, are one such class of drugs. Others include the calcium-channel blocker diltiazem, the antibiotic clarithromycin, and possibly some antifungals. AMLOTEK® causes several drugs to increase in levels, including cyclosporine, simvastatin, and tacrolimus (the increase in the last one being more likely in people with CYP3A5*3 genetic polymorphisms). When more than 20 mg of simvastatin, a lipid-lowering agent, are given with AMLOTEK®, the risk of myopathy increases. Giving AMLOTEK® with Viagra increases the risk of hypotension.
AMLOTEK® can cause a severe allergic reaction. Symptoms include:
– Trouble breathing
– Swelling of your throat or tongue
In many cases, the most common side effects of AMLOTEK® happen because the medicine is working too well. Rather than having high blood pressure, it may cause low blood pressure (hypotension). Symptoms of low blood pressure include:
– Flushing (this is very common at first but usually resolves within the first two weeks of taking AMLOTEK®)
– Swollen ankles (especially in warmer weather)
The common side effects listed above happen in more than 1 in 100 people, and are usually mild and short-term. If they last longer than a few days, speak to your GP or pharmacist.
AMLOTEK® is available as 5mg tablets. The usual starting dose is 5mg, although this may be increased to 10mg if the symptoms of your high blood pressure or angina are not abating. The higher the dose of AMLOTEK®, the lower the blood pressure will be.
The dose you receive will depend on your blood pressure and whether or not you are experiencing any symptoms. Your GP will keep tabs on your blood pressure throughout treatment and may adjust the dose accordingly.
Drug forms and strengths:
Form: oral tablet
Strengths: 5 mg
AMLOTEK® in the dosage of 5 mg in the pharmaceutical basket of Pars pharmed company can be presented to the market. Providing all documents related to the manufacture and analysis of this product to the Food and Drug Agency, the license and the export license was issued.