Universal reference book for medicines
Product name: FELODIPINE-SZ (FELODIPINE-SZ)

Active substance: felodipine

Type: Calcium channel blocker

Manufacturer: СЕВЕРНАЯ ЗВЕЗДА (Russia)
Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..

PHARMACHOLOGIC EFFECT
Selective blocker of calcium channels of II class from the group of dihydropyridine derivatives.
Like other dihydropyridine derivatives, felodipine has a significantly higher affinity for the calcium channels of the smooth muscle cells of the arterial vessels than for the calcium channels of the cardiomyocytes. Blocking the calcium channels and disrupting the entry of calcium ions into the smooth muscle cells of the arterial vessels, causes their expansion, reduces the OPSS and lowers blood pressure. Decreases the afterload on the heart.
Virtually does not have an inhibitory effect on contractility and conductivity of the myocardium, causes a mild reflex tachycardia.
Increases coronary blood flow.
Reduces the flow of extracellular calcium into cardiomyocytes and smooth muscle cells of the coronary and peripheral arteries;
in high doses reduces the release of calcium ions from the intracellular depot. 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 smooth muscles of vessels, mediated by calmodulin.
In therapeutic doses normalizes the transmembrane current of calcium, disrupted in a number of pathological conditions, especially in hypertension.
Reduces blood pressure due to vasodilation, a decrease in OPSS. Does not affect the tone of the veins and adrenergic vasomotor innervation, so it does not cause orthostatic hypotension.
Has a dose-dependent anti-ischemic effect.
Strengthens the coronary blood flow, improves the blood supply of the ischemic zones of the myocardium without the development of the phenomenon of "stealing," activates the functioning of collaterals, protects against complications of reperfusion, slightly increases heart rate.Expanding the peripheral arteries, reduces afterload.
Almost does not affect the sinoatrial and AV-nodes.
Virtually does not have a negative inotropic effect (a reflex increase in heart rate in response to vasodilation disguises a negative inotropic effect).
It enhances kidney blood flow, has a moderate natriuretic and diuretic effect.

The effect begins in 2-5 hours and lasts for 24 hours. The severity of the effect correlates with the dose and concentration in the plasma.

PHARMACOKINETICS
After ingestion, felodipine is almost completely absorbed from the digestive tract and is subjected to intensive metabolism during the "first passage" through the liver.Binding to plasma proteins (mainly with albumins) is about 99%.
In small amounts, it penetrates the GEB and the placental barrier, excreted in breast milk. Felodipine is extensively metabolized in the liver, all its known metabolites do not have pharmacological activity. Metabolism occurs with the participation of isoenzymes CYP3A4, CYP3A5, CYP3A7.
About 70% is excreted by the kidneys in the form of metabolites and less than 0.5% unchanged;
the remainder is excreted through the intestine. T 1/2 in the? -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.

Do not cumulate even with prolonged use;
In chronic renal failure, cumulation of inactive metabolites is observed.
INDICATIONS
Arterial hypertension, angina pectoris (with ineffectiveness of beta-adrenoblockers and nitrates), Reynaud's syndrome (as symptomatic therapy).

DOSING MODE
Used 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 EFFECT
From the side of the cardiovascular system: flushing of the skin to the skin of the face, accompanied by hyperemia of the face, tachycardia, swelling in the ankle (as a consequence of precapillary vasodilation), fainting, extrasystole, severe arterial hypotension accompanied by reflex tachycardia and worsening of angina pectoris, leukocytoclastic vasculitis.

From the side of the central nervous system: headache, dizziness, a sense of fatigue, paresthesia.

From the digestive system: nausea, abdominal pain, vomiting, increased activity of hepatic transaminases, gingival hyperplasia, tongue mucosa, and gingivitis.

From the musculoskeletal system: rarely - arthralgia, myalgia.

Allergic reactions: skin rash, itching, hives, angioedema, swelling of the lips or tongue, photosensitivity reaction.

Other: impotence / sexual dysfunction, frequent urination, fever, hyperglycemia.

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

PREGNANCY AND LACTATION
Contraindicated in pregnancy (including possible).

APPLICATION FOR FUNCTIONS OF THE LIVER
Use with caution in patients with renal failure.

APPLICATION FOR CHILDREN
Contraindicated at the age of 18 years.

SPECIAL INSTRUCTIONS
Use with caution in patients with heart failure, lability of AD, with renal failure, heart failure after myocardial infarction.

When used in patients with angina pectoris, it should be noted that in rare cases, felodipine can cause severe arterial hypotension, which leads to myocardial ischemia.

DRUG INTERACTION
With simultaneous use with inhibitors of microsomal liver enzymes, an increase in the concentration of felodipine in the blood plasma is possible.

It is possible to reduce the concentration of felodipine in the blood plasma due to increased intensity of its metabolism in the liver under the influence of carbamazepine, phenytoin and phenobarbital (which are inducers of microsomal liver enzymes) and acceleration of excretion from the body.

With simultaneous use with digoxin, an increase in the concentration of digoxin in the blood plasma is possible.

With simultaneous use with itraconazole, ketoconazole, the metabolism of felodipine in the liver slows down, which leads to an increase in the concentration of felodipine in the blood plasma and an increased risk of side effects.

With simultaneous use with erythromycin, the bioavailability of felodipine increases.
There is a reported increase in the therapeutic and side effects of felodipine in a patient receiving erythromycin.
Increases the bioavailability of propranolol.
With simultaneous use with beta-blockers, the risk of developing chronic heart failure increases.
Reduction of 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 intensification of antihypertensive action occurs with simultaneous application with inhalation means for anesthesia, beta-adrenoblockers, alpha-adrenoblockers, sympathomimetics and other antihypertensive drugs.
Drugs that increase the duration of the QT interval increase the negative inotropic effect and may increase the risk of a significant prolongation of the QT interval.

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