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Amlozek is a calcium channel blocker. It is used to treat high blood pressure, which affects more and more people around the world. Read about the mechanism of action of Amlozek and how to dose it.
Amlozek – characteristics
Amlodipine contains the active substance amlodipine, which belongs to a group of medicines called calcium channel blockers. Amlozek is used to treat high blood pressure (hypertension) or a chest pain called angina, a rare form of which is Prinzmetal’s angina (vasospastic angina).
In people with high blood pressure, this medicine widens the blood vessels, making it easier for the blood to flow through them. In people with coronary heart disease, Amlozek helps blood flow to the heart muscle by increasing the amount of oxygen supplied, which in turn prevents chest pain. This medicine does not provide immediate relief of chest pain caused by angina.
See: Angina pectoris increases the risk of coronary heart disease in women
Amlozek – mechanism of action
Amlodipine is a calcium ion influx antagonist of the dihydropyridine group (slow calcium channel inhibitor or calcium ion antagonist) and inhibits the transmembrane influx of calcium ions into cardiac and vascular muscular cells.
The mechanism of the antihypertensive effect of amlodipine is due to a direct relaxant effect on vascular smooth muscle. The exact mechanism by which amlodipine relieves symptoms of angina is not fully understood, but amlodipine reduces heart hypoxia through the following two types of action:
- amlodipine dilates the precapillary arterioles and thus reduces the total peripheral resistance (afterload) that the heart has to overcome. As the heart rate remains unchanged, this action reduces the energy consumption and oxygen demand of the heart muscle.
- The mechanism of action of amlodipine probably also involves the expansion of large coronary arteries and arterioles, both in unchanged and ischemic areas. This increases the heart’s oxygen supply in patients with spasms of the coronary arteries (Prinzmetal’s angina).
In hypertensive subjects, once daily dosing produces clinically significant reductions in blood pressure in both the supine and standing positions for 24 hours. Due to the slow onset of action, no rapid fall in blood pressure is observed following administration of amlodipine.
In patients with angina, the administration of a single daily dose of amlodipine increases the time to exercise, the time to angina, and the time to 1 mm ST segment depression, and reduces both the frequency of angina attacks and the need for glyceryl trinitrate.
Also read: Primary arterial hypertension – causes, symptoms and treatment
Amlozek – indications
Amlozek is used as first line treatment in the treatment of high blood pressure, ischemic heart disease caused by vasoconstriction (stable angina) and / or vasospasm (Prinzmetal’s angina).
Used alone to normalize blood pressure in most patients. It can be administered in combination with thiazide diuretics, alpha blockers, beta blockers, and angiotensin converting enzyme (ACE) inhibitors.
See: Pulmonary arterial hypertension – symptoms and treatment. What is life like with TNP?
Amlozek – contraindications
Amlodipine, and its active substance, i.e. amlodipine, is contraindicated in people:
- with hypersensitivity to dihydropyridine derivatives, amlodipine or any of the excipients,
- with severe hypotension – in shock (including cardiogenic shock),
- obstruction in the outflow tract of the left ventricle (e.g. high-grade aortic stenosis)
- with haemodymic unstable heart failure after acute myocardial infarction.
Amlozek – dosage
Dosage of Amlozek in adults: For the treatment of both high blood pressure and angina, the usual starting dose is 5 mg once a day. The dose may be increased to a maximum of 10 mg daily, depending on the patient’s individual response to treatment.
Dosage of Amlozek in children and adolescents with hypertension aged 6 to 17 years: the recommended oral starting dose for children and adolescents 6 to 17 years of age is 2,5 mg once a day. The dose may be increased to 5 mg once a day if desired blood pressure has not been obtained after 4 weeks of use. Doses greater than 5 mg daily have not been studied in children and adolescents.
The editorial board recommends: Poor sleep promotes resistant arterial hypertension
Amlozek – precautions
Amlozek should be dosed with caution in people with heart failure, as it increases the risk of pulmonary edema, as well as in liver dysfunction.
In some situations it may be necessary to carry out certain check-ups. In some cases, side effects that may disrupt your reaction time – dizziness or visual disturbances – may affect your ability to drive or use machines.
Amlozek – side effects
Amlozek can cause various side effects. They only occur in a certain group of patients. They suffer from drowsiness, fatigue, headaches and dizziness, abdominal pain, nausea, palpitations, flushing, hot flushes and malaise.
Less often than mentioned, weakness and fainting, paresthesia, mood changes, visual disturbances, tinnitus, chest pain, taste disturbances, stomach problems (diarrhea, constipation, indigestion), sweating, alopecia, rash and skin discoloration are also possible, itching, hypotension, dyspnoea, rhinitis, profuse sweating.
Very rarely, severe skin reactions, peripheral neuropathy, jaundice, hepatitis, cough, inflammation of blood vessels, increased blood glucose, decreased white blood cells, swelling of the face, lips, tongue, throat, inflammation of the stomach, inflammation of the pancreas.
Amlozek and pregnancy and breastfeeding
The safety of amlodipine in human pregnancy has not been established. Animal studies have shown reproductive toxicity at high doses. The use of amlodipine during pregnancy is possible only when there is no other, safer product and when the disease poses a greater risk to the mother and the fetus.
Amlodipine is excreted in human milk. It has been estimated that the proportion of the dose that the infant receives from the breastfeeding mother is in an interquartile range of 3% to 7%, with a maximum of 15%. The effect of amlodipine on infants is unknown.
A decision whether to continue or discontinue breast-feeding or to continue or discontinue amlodipine administration should be made taking into account the benefit of breast-feeding to the child and the benefit of amlodipine therapy to the mother.
See: The world’s oldest mothers. “If you have a child, you have no death”
Amlozek – overdose
Available data indicate that large overdose may lead to profound peripheral vasodilation and possible reflex tachycardia. Substantial and possibly prolonged hypotension, leading to shock, including fatal shock, has been reported.
Clinically significant hypotension due to amlodipine overdose requires active support of the cardiovascular system, including monitoring of cardiac and respiratory function, elevation of the limbs, and control of circulating fluid volume and urine output.
Read also: Normal blood pressure – norms, measuring pressure, hypertension. Normal pressure in pregnancy
Amlozek – interactions with other drugs
Tell your doctor about all the medications you are taking or have recently taken, and about any medications you plan to use. Amlozek may interact with other medications, and other medicines may interact with Amlozek. These are:
- ketoconazole, itraconazole (antifungals)
- ritonavir, indinavir, nelfinavir (so called protease inhibitors used to treat HIV),
- rifampicin, erythromycin, clarithromycin (antibiotics)
- St. John’s wort,
- verapamil, diltiazem (medicines for heart conditions)
- dantrolene (used as an infusion for severe abnormal body temperature)
- tacrolimus, sirolimus, temsirolimus and everolimus (medicines that suppress your immune system),
- simvastatin (cholesterol lowering medicine),
- cyclosporine (an immunosuppressive drug).
Amlozek may lower your blood pressure to a greater extent if you are taking other medicines for hypertension.
Amlozek – price
The price for Amlozek depends on the amount of tablet weight in the package. A package containing 30 tablets of 5 mg will cost approximately PLN 13, and 30 tablets of 10 mg will cost approximately PLN 19.