PRESID table. 10 mg. 30 tablets
PRESID table. 10 mg. 30 tablets
Qualitative and quantitative composition
Felodipine 2,5 mg, 5 mg or 10 mg in one tablet, extended release
PRESID 2,5 mg: Yellow, round, biconvex, coated tablets imprinted with 2,5. PRESID 5 mg: Light pink, round, biconvex, coated tablets imprinted 5.PRESID 10 mg: Reddish-brown 'round biconvex, coated tablets imprinted with 10.
Treatment of essential hypertension. Prevention of stable and vasospastic forms of stenokardiya.Lekarstveniyat product is indicated for the treatment of adult patients.
Dosage and administration
Adults (including the elderly): The dose of the product should always be determined individually. Treatment is initiated at 5 mg once daily. If necessary, the dose may be increased or added to other antihypertensive agents. The usual maintenance dose is 5-10 mg once daily. With the purpose of testing the dose is appropriate to use the tablet 2,5 mg felodipine. In older patients a starting dose of 2,5 mg once daily may be sufficient.
Adults: The dose of the product, should always be determined individually. Treatment is initiated at 5 mg once daily and if needed, the dose may be increased to 10 mg once daily. The maximum dose is 20 mg daily.
Presid medicinal product can be administered in combination with p-blockers, ACE inhibitors or 'diuretics / Combination therapy usually increases the antihypertensive effect. Hypotension should be avoided. In patients with severe hepatic impairment therapeutic dose should be reduced (we recommend a starting dose of 2,5 mg per day). The pharmacokinetics of the product is not significantly altered in patients with impaired renal function and therefore no dosage adjustment for patients.
The best way for acceptance of the product in the morning before a meal or after a snack. Coated tablets should be swallowed whole with a little water and must not be chewed, divided or crushed.
The product is contraindicated in patients with unstable angina in patients with pre-existing allergic reactions or other dihydropyridines felodipine (cross-reactivity), known hypersensitivity to any of its ingredients and pregnancy. Presid medicinal product must not be used in patients with symptomatic aortic stenosis in decompensated heart failure, over one month after the onset of myocardial infarction with marked hypotension and cardiogenic shock.
Only in rare cases the product Presid like other vasodilators can cause severe hypotension which in sensitized patients may manifest as myocardial ischemia. There is no any evidence that the product is effective for secondary prevention of myocardial infarction.
Efficacy and safety in the treatment of malignant hypertension has not been established.
Safety and efficacy in children have not been established and therefore should not be given to children.
Coadministration with agents that interact with cytochrome P-450 enzyme system may affect plasma concentrations of felodipine. Enzyme inhibitors (eg, cimetidine, ranitidine, erythromycin, itraconazole, ketoconazole, ritonavir, saquinavir, quinidine) increased plasma concentrations of felodipine and therefore applied the product Presid doses should be reduced in case of co-administration of these drugs. Enzyme inducers (eg, phenytoin, carbamazepine and barbiturates) may reduce plasma concentrations of felrdipina and the dose of the product should be Presid increased. There is no need for changing the dosage of concomitant digoxin. High binding of felodipine plasma protein does not affect other drugs highly bound to plasma proteins (eg, warfarin).
The use of grapefruit juice contains flavonoids increases in peak plasma levels and bioavailability of felodipine and grapefruit juice so should not be taken with Presid. Antihypertensive drugs prolong the hypotensive effect of felodipine while sympathomimetics reduce.
Pregnancy and lactation
Forbidden is to use the product Presid child. Felodipinat is found in breast milk, but it is not known whether there are any adverse effects on the newborn. Nursing mothers should not use the product if the effect of treatment outweighs the risk to the infant.
Effects on ability to drive and use machines
The product can Presid especially at the beginning of treatment or when dosage adjustment will affect the ability to drive a motor vehicle or operating machinery.
Like other calcium channel blockers can be observed flushing, headache, palpitations, dizziness and fatigue. These effects are usually transient and occur most frequently during initiation of treatment or after an increase in dosage of the product. It can be seen as early as the dose used, swollen ankles due to prekapilyarna vasodilation. Mild swelling of the gums may occur in patients suffering from gingivitis or periodontitis. It can be avoided by careful oral hygiene. Like other dihydropyridines in rare cases can be observed worsening symptoms of angina especially in early treatment in patients with ischemic heart disease.
In clinical studies and monitoring the product, the following adverse events grouped as follows:
Common (greater than 1%), uncommon (0.1 - 1%), rare (0.01 - 0.1%), very rare (less than 0.01%).
Central and peripheral nervous system
KozhaSadova system (extra-cardiac):
Headache Flushing Peripheral edema
Central and peripheral nervous system
Tachycardia, palpitations, dizziness, paresthesia, nausea, abdominal pain, rash and sarbezhUmor
Syncope Vomiting Pain in joints and muscles impotence, sexual dysfunction
Urticaria hyperplasia gingival
Increased levels of liver enzymes
Photosensitivity reaction, leukocytoclastic vasculitis
Hypersensitivity reactions eg. Angioedema and fever
Symptoms of overdose product occurs with significant peripheral vasodilation and symptomatic hypotension, which may sometimes be accompanied by bradikardiya.Lechenie: if there is severe hypotension should be symptomatic treatment. The patient is placed supine on your back with your feet up. If there is bradycardia and applied atropine 0.5 - 1 mg iv If these measures are not sufficient to apply fiziolgichen infusion of saline or dextran. If the clinical condition of the patient is normal apply a1-adrenergic.
Pharmacotherapeutic group: vasodilator antihypertensives
Felodipine is a calcium antagonist vazoselektiven high with predominant vascular effect of the dihydropyridine type, which lowers blood pressure by reducing peripheral vascular resistance. At therapeutic doses it selectively affects the smooth muscle of arterioles and does not directly affect myocardial contractility and impulse conduction in the conduction system of the heart. "It does not affect the smooth muscle of the veins or adrenergic vasomotor mechanisms and therefore the application of felodipine is not associated with symptoms of orthostatic hypotension. felodipine has a mild diuretic and natriuretic effect and no fluid in the body.
Presid product can be used alone or in combination with other antihypertensive agents, eg. beta-blockers, diuretics or ACE inhibitors in order to achieve an increased antihypertensive effect. Felodipine reduced systolic and diastolic blood pressure and can be used in patients with isolated systolic hypertension. Felodipine antihipetenzivnata retains its effectiveness even when combined with nonsteroidal anti-inflammatory drugs (NSAID).
Felodipine has antianginal and anti-ischemic effects due to its ability to improve the balance between consumption and oxygen supply to the myocardium. Felodipinat decreases coronary vascular resistance. Blood flow through the coronary veins and supply the myocardium with oxygen is also increased as a result of dilatation of arteries and arterioles of the epicardium. Felodipinat effectively prevents the development of coronary artery spasm. The decrease in systemic blood pressure Felodipine decreases the afterload of the left ventricle and reduced oxygen requirements of the myocardium.
Felodipine improves tolerability load and reduces angina attacks in patients with stable exertional angina caused. In patients with vasospastic angina by type, it reduces the manifestations of ischemic heart disease.
Felodipinat is effective and well tolerated in elderly patients and in patients suffering from co-morbidities such. asthma and other obstructive lung diseases, renal dysfunction, diabetes mellitus, gout, hyperlipemia, Raynaud's phenomenon in patients after renal transplantation. Felodipinat not affect glucose and lipid profil.Myasto mechanism of action in their pharmacodynamic characteristics felodipine has a high selectivity for blood 'vessels. Resistant smooth muscle in arterioles is extremely sensitive to the effects of felodipine. Felodipinat inhibits electrical and contractile activity of vascular smooth muscle through effects on calcium channels in the cell membrane. hemodynamic effects, the main hemodynamic effect of felodipine is a reduction in total peripheral vascular resistance, leading to a drop in blood pressure, the effect is dose dependent. Usually blood pressure is monitored for 2 hours after a single application and prodazhava least 24 hours. ratio T / P is significantly higher than 50%. exists a positive correlation between plasma drug concentration, the rate of decrease in peripheral vascular resistance and the degree of reduction in blood pressure.
Electrophysiological and other cardiac effects: In tepapevtichni dozifelodipinat no effect on myocardial contractility, AV conduction and refractory phase of AV vazel.Babrechni effects: Felodipinat has natriuretic and diuretic effect by reducing the Na + reabsorption in the renal tubules. Once administered in some other vasodilators observed retention of water and sodium. Following administration of felodipine renal vascular resistance and decreased glomerular filtration rate did not change. In patients with impaired renal function glomerular filtration rate may increase during the implementation of felodipin.Patsientite after renal transplantation felodipine well tolerated.
Absorption and distribution:
Following oral administration, felodipine wrapped prolonged release is completely absorbed from the gastrointestinal tract. The systemic bioavailability of Felodipine is about 15% in humans and is independent of the dose used in the therapeutic dose range. Felodipine is bound to plasma proteins, particularly albumin approximately 99%. Felodipine in the form of coated prolonged-release tablets leads to the extension phase of absorption and plasma concentration over 24 hours.
Metabolism and Elimination:
Felodipine is extensively metabolised in the liver and all its metabolites are inactive. The half-life is 25 hours. With continued application of the active substance is not accumulation. Older patients and patients with impaired babrechna.funktsiya have higher plasma concentrations of felodipine, than younger patients. The pharmacokinetics of felodipine are not altered in patients with renal impairment, including patients on hemodialysis, approximately 70% of the administered dose was excreted in urine and faeces as metabolites. Less than 0.5% of the administered dose is excreted unchanged in the urine. No significant accumulation of product during prolonged therapy. Felodipine is extensively metabolised in the liver to inactive metabolites. About 70% of the dose is excreted as metabolites in the urine and the remainder is excreted in faeces. Less than 0.5% of the dose is excreted unchanged in the urine.
Preclinical safety data
In a study on fertility and reproductive behavior in rats treated with felodipine in the groups treated with higher doses of felodipine during the birth was longer and incidence of mortality during childbirth and the postnatal period were higher. There were no violations of fertility in rats using felodipine in therapeutic doses. Reproduction studies in rabbits showed reversible enlargement of the mammary glands of females and abnormal fetal limbs depending on the doses used. Anomalies were found in fetuses when felodipine was used in the early stages of fetal development. Mutagenicity: Mutagenicity study using four different test did not show any mutagenic properties of felodipine.
The studies were conducted in mice and rats. Tumors were observed in interstitial cells of the testes of rats. This specific effect is due to the effects of felodipine on the endocrine system of rats and was not seen in humans.
List of excipients (qualitative)
Lactose monohydrate, Cellulose microcrystalline, Hypromellose 2910/50, HypromeJIose 2910/6, Povidone 25, Propyl gallate, Silica colloidal anhydrous, Magnesium stearate. Ferric oxide yellow. Ferric oxide red (Presid tablets in 5 mg and 10 mg), Titanium dioxide, Talc, Propylene glycol.
He is known.
At temperatures below 30 ° C.
PVC / PE / PVDC aluminum blister package leaflet and carton. Pack sizes: 30 or 100 coated prolonged-release tablets.