Buy Felodipine tabletsprolong.d-I coated 10mg N30

Felodipine pillsprolong.d-I coated 10mg N30

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Active ingredients

Famotidine

Release form

Pills

Composition

Felodipine 10 mg Excipients: lactose monohydrate, kollidon SR (polyvinyl acetate 80%, povidone 19%, sodium lauryl sulfate 0.8%, silicon dioxide 0.2%) 76 mg, colloidal silicon dioxide, sodium fumarate. The composition of the tablet shell: Opadry II - polyvinyl alcohol, partially hydrolyzed, macrogol 3350, talcg, titanium dioxide, soy lecithin, aluminum lacquer based on indigo carmine dye, aluminum varnish based on dye azorubine, aluminum lacquer based on dye crimson [Ponso 4R].

Pharmacological effect

Selective calcium channel blocker class II from the group of dihydropyridine derivatives. Like other dihydropyridine derivatives, felodipine has a significantly higher affinity for the calcium channels of arterial vascular smooth muscle cells than for the calcium channels of cardiomyocytes. By blocking calcium channels and disrupting the entry of calcium ions into the smooth muscle cells of the arterial vessels, it causes their expansion, decreases the round focal paths and lowers blood pressure. Reduces afterload on the heart. Virtually no inhibitory effect on contractility and conductivity of the myocardium, causes a moderately pronounced reflex tachycardia. Increases coronary blood flow. Reduces the flow of extracellular calcium into the cardiomyocytes and smooth muscle cells of the coronary and peripheral arteries; in high doses reduces the release of calcium ions from intracellular depots. Reduces the number of functioning channels, without affecting the time of their activation, inactivation and recovery. Separates the processes of excitation and contraction in the myocardium, mediated by tropomyosin and troponin, and in vascular smooth muscle, mediated by calmodulin. In therapeutic doses, normalizes the transmembrane current of calcium, disturbed in a number of pathological conditions, especially in hypertension. Reduces blood pressure due to vazodilatatsii, reduce OPS. Does not affect the tone of the veins and adrenergic vasomotor innervation, therefore, does not cause orthostatic hypotension. It has a dose-dependent anti-ischemic effect. Enhances coronary blood flow, improves blood supply to the ischemic zones of the myocardium without the development of the "robbery" phenomenon, activates the functioning of collaterals, protects against reperfusion complications, slightly increases the heart rate. By expanding the peripheral arteries, it reduces the afterload. Almost no effect on sinoatrial and AV nodes.Practically does not have a negative inotropic effect (a reflex increase in heart rate in response to vasodilation masks a negative inotropic effect). Enhances renal blood flow, has a moderate natriuretic and diuretic effect. The action begins after 2-5 hours and lasts for 24 hours. The effect of the effect correlates with the dose and concentration in the plasma.

Pharmacokinetics

After oral administration, felodipine is almost completely absorbed from the gastrointestinal tract and is extensively metabolized during the "first pass" through the liver. Binding to plasma proteins (mainly albumin) is about 99%. In small quantities, penetrates through the BBB and the placental barrier, excreted in breast milk. Felodipine is extensively metabolized in the liver; all its known metabolites do not possess pharmacological activity. Metabolism occurs with the participation of isoenzymes CYP3A4, CYP3A5, CYP3A7. About 70% are excreted by the kidneys as metabolites and less than 0.5% unchanged; the rest is excreted through the intestines. T1 / 2 in the α-phase is about 4 hours, in the phase - about 24 hours. In elderly patients, as well as in patients with impaired liver function, the concentration of felodipine in the blood is higher than in younger patients. Does not cumulate even with prolonged use; in chronic renal failure, cumulation of inactive metabolites is observed.

Indications

Arterial hypertension, angina (with the ineffectiveness of beta-blockers and nitrates), Raynaud's syndrome (as a symptomatic therapy).

Contraindications

Acute myocardial infarction, decompensated chronic heart failure, age up to 18 years, pregnancy, women of childbearing age with a high probability of pregnancy, hypersensitivity to felodipine.

Use during pregnancy and lactation

Contraindicated for use in pregnancy (including possible).

Dosage and administration

Apply inside mainly in the form of dosage forms, providing a constant release of the active substance - 5-10 mg 1 time / day, if necessary - 20 mg 1 time / day. The maximum daily dose is 20 mg.

Side effects

Since the cardiovascular system: flushing of the skin of the face, accompanied by flushing of the face, tachycardia,swelling in the ankle joint (as a result of precapillary vasodilation), syncope, extrasystole, severe arterial hypotension, accompanied by reflex tachycardia and worsening of angina, leukocytoclastic vasculitis. From the side of the central nervous system: headache, dizziness, fatigue, paresthesia. On the part of the digestive system: nausea, abdominal pain, vomiting, increased activity of hepatic transaminases, gingival hyperplasia, mucous membrane of the tongue, gingivitis. On the part of the musculoskeletal system: rarely - arthralgia, myalgia. Allergic reactions: skin rash, itching, urticaria, angioedema of the lips or tongue, photosensitization reaction. Other: impotence / sexual dysfunction, frequent urination, fever, hyperglycemia.

Interaction with other drugs

With simultaneous use with inhibitors of microsomal liver enzymes may increase the concentration of felodipine in the blood plasma. It is possible to decrease the concentration of felodipine in the blood plasma due to an increase in the intensity of its metabolism in the liver under the influence of carbamazepine, phenytoin and phenobarbital (which are inducers of microsomal liver enzymes) and to accelerate excretion from the body. With simultaneous use of digoxin, it is possible to increase the concentration of digoxin in the blood plasma. With simultaneous use with itraconazole, ketoconazole slows down the metabolism of felodipine in the liver, which leads to an increase in the concentration of felodipine in the blood plasma and increase the risk of side effects. With simultaneous use with erythromycin, felodipine bioavailability increases. There is a message of increased therapeutic and side effects of felodipine in a patient receiving erythromycin. Increases the bioavailability of propranolol. With simultaneous use with beta-blockers increases the risk of developing chronic heart failure. A decrease in the antihypertensive effect is observed with the simultaneous use of felodipine with NSAIDs, GCS (sodium retention and blockade of prostaglandin synthesis by the kidneys) and estrogens (sodium retention), calcium preparations; The antihypertensive effect is enhanced with simultaneous use with inhalants for anesthesia, beta-blockers, alpha-blockers, sympathomimetics and other antihypertensive drugs.Drugs that cause an increase in the duration of the QT interval, increase the negative inotropic effect and may increase the risk of significant lengthening of the QT interval.

special instructions

Use with caution in patients with heart failure, blood pressure lability, renal failure, heart failure after myocardial infarction. When used in patients with angina pectoris, it should be borne in mind that in rare cases felodipine can cause severe arterial hypotension, which leads to myocardial ischemia.

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