Plendil 5mg Astrazeneca medicine for hypertension, stable angina (30 tablets)

ATC code: C08C AD2. Felodipine (Plendil) is a selective calcium channel blocker on the circuit, used to treat hypertension and stable angina.

The active ingredient of Plendil, Felodipine, is a derivative of dihydropyridine. Felodipine is a mixture of fertilizer.

Felodipine works by reducing the impact of the peripheral circuit, especially the resistance in the arteries. The electrical activity and spasm of blood vessel muscle cells are inhibited through the effects on calcium channels in the cell membrane.

Due to the selective effect on the smooth muscle in the artery area, the felodipine at the dose of treatment does not have a negative muscle contraction effect on the heart, and also has no clinical electrophysiological effects.

Felodipin relaxes smooth muscles in the respiratory tract. Clinical experience has shown that Felodipine has little effect on the function of gastric movement. It is also not seen that felodipine has a significant clinical influence on blood lipids during long -term treatment, nor has any clinical significant effect on metabolic control (HBA1C) in patients with type II diabetes in six months of treatment. In general, Felodipine can be used for patients with left ventricular failure and treated under a regular therapy, or with asthma, diabetes, gout or hyperlipidemia.

Anti -blood pressure effect:

Felodipine reduces arterial blood pressure by reducing the barrier in the peripheral vessels. Treatment of patients with plentil hypertension will reduce blood pressure in lying, sitting and standing positions, and when resting and during exercise.

Felodipine does not cause hypotension, because there is no effect on venous muscles or a mechanism to control the sympathetic system.

Lower blood pressure can cause a temporary reflex to increase heart rate and blood emulsion in the heart at the beginning. Increasing the effect of increasing heart rate when Felodipine is used with beta receptor inhibitors. Felodipine concentration in plasma has a positive correlation for reducing peripheral and blood pressure. In a stable state, the efficiency remains on the remaining dose and gives the effect of reducing blood pressure within 24 hours.

Felodipine treatment is associated with the regression of left ventricular hypertrophy.

Felodipine has diuretic and sodium excretion effect but has no diuretic effect.

The reabsorption of sodium and water in the renal tubules is reduced, it can be explained that due to the lack of salt and body fluid in the patient. Felodipine reduces kidney blood vessel resistance and increases kidney perfusion. The glomerular filtration is unchanged. Felodipine does not affect the excretion of albumin.

In hot study (Hypertension Optimal Treatment - Optimal treatment of hypertension), including 18,790 patients with mild to moderate hypertension, treatment with Plendil, combined with transferred inhibitors, Big and/diuretic inhibitors, if needed, leading to diastolic blood pressure (DBP) ≤ 90 mmHg at 93% of patients.

In this study, the rate of cardiovascular events in patients with type II diabetes (n = 151) is significantly lower (50%) in the group where the target hypertension is ≤ 80 mmHg (11.9/1000 patients - year), compared to the groups of the target hypertension under 90 mmHg (24.4/1000 patients - year).

Plendil is one of two calcium antagonists in the Stop - 2 study in Sweden, performed in 6,614 patients with hypertension ages from 70 - 84. The study shows that the treatment of hypertension starts with calcium antagonists in the dihydropyrine group and with supplementation and/or diuretics. For the treatment of hypertension patients, Plendil can be used for monomers or in combination with other antihypertensive drugs, such as beta receptor inhibitors, diuretics or medications inhibitors.

Anti -angina effect:

Felodipine works through coronary dilatation, thereby improving perfusion and providing oxygen to the heart. Reducing the load in the heart by reducing peripheral artery resistance (post -load reduction), the result is to reduce the oxygen demand of the heart muscle. Felodipine stops coronary spasms.

Felodipin improves her ability to try and reduce the frequency of angina in patients with stable angina and angina due to effort.

When starting treatment, there is a reflex that increases the transient heart rate, this reflex will disappear if the plentil is used in combination with the beta receptor inhibitor. The onset time is two hours and the acting time is 24 hours. Plendil can be used in conjunction with beta receptor inhibitors or single therapy to treat patients with angina.

Children:

Clinical experience of using felodipine in children with hypertension is limited. In a random study, double blindness, parallel group, the hypotension effect of Felodipine once a day in children from 6 to 16 years old with primary hypertension has been studied. Children patients were treated for three weeks with 2.5 mg (n = 33), 5 mg (n = 33), 10 mg (n = 31) or placebo (n = 35). This study did not prove any anti -hypertension effect in children for 6-16 years.

Felodipine's long -term effects on growth, puberty and general development have not been studied. The long -term effect of anti -hypertension therapy is a treatment in childhood to reduce the incidence of cardiovascular disease and death in adulthood has not been established.

Dynamic pharmacokinetics

The active ingredient in prolonged release tablets is felodipine attached to a polymer that forms a gel layer when exposed to water, from which Felodipine is released continuously, leading to slow onset.

Felodipine's bioavailability is about 15% and does not depend on the absorption of food at the same time. However, the absorption rate - although it is not the level of absorption - is affected by the absorption of food at the same time, and the maximum concentration in plasma thereby increases about 65%.

Maximum concentration in plasma is achieved after 3-5 hours. The level of cohesion with plasma protein is about 99%. The distribution volume in a stable state is 12 l/kg. Felodipine's disposal time in the excretion period is about 25 hours and stable state achieved after 5 days. There is no risk of accumulation during long -term treatment.

The average clearance is 1200 ml/min. Reducing clearance in older patients and patients with liver function failure leading to higher plasma felodipine levels. However, age only partly explains the change in plasma concentrations between individuals.

Felodipine is metabolized in the liver by Cytochrome P450 3A4 and no identification metabolites have the effect of vasodilation. About 70% of the dose is eliminated in the form of metabolites in urine and the rest is eliminated through feces. Less than 0.5% of the dose is excreted in the form of unchanged urine.

Be cautious when using

need to be very careful when taking the drug for patients in the following cases:

The efficiency and safety of felodipine in the treatment of emergency hypertension has not been set.

Felodipine may lower blood pressure with tachycardia later. This can lead to myocardial anemia in sensitive patients.

Felodipine is eliminated through the liver. Therefore, it may be expected that the concentration of treatment is higher and the drug response occurs in patients with impaired liver function (see the dose and usage).

Concomitance the use of stimulants or strong inhibits CYP3A4 enzymes leads to a significant reduction in felodipine levels in plasma. Therefore it is necessary to avoid these combinations. (See the interaction with other drugs and other types of interactions).

Plendil contains lactose. Patients with rare genetic problems about galactose tolerance or malposure-galactose should not take this medication.

Plendil contains castor oil, so it can cause stomach pain and diarrhea.

The effect of the drug on the ability to drive and operate machinery

because dizziness and fatigue may occur related to treatment with Plendil, this should be considered when there is a high concentration, for example, when driving or operating machinery.

Use drugs for women during pregnancy and lactation

Pregnant women:

There is no adequate data on the use of Plendil in pregnant women. Contraindicated use of Plendil during pregnancy, there has been observed the teratogenic effect in animal studies (see clinical safety data section). The possibility of pregnancy must be excluded before the beginning of treatment with Plendil.

Calcium antagonists may inhibit premature contractions in the uterus, but there is no clear evidence of delayed birth during pregnancy. There is a risk of fetal deficiency in the fetus when the mother has hypotension and reduces uterine perfusion due to the distribution of blood flow through peripheral vascular dilatation.

breastfeeding women:

Felodipin is excreted through breast milk. If women who are breastfeeding have felodipine treatments, only a very small dose is transmitted through breast milk to the baby. There is no enough experience in treating felodipine during breastfeeding to assess risks for children. Therefore, plentil should not be used during breastfeeding. In the case of medical treatment benefits is considered to be more important, safety measures should be stopped breastfeeding.

Drug interaction

Felodipine is metabolized in the liver by cytochrome P450 3A4 (CYP3A4). Concentrated use with inhibitors or CYP3A4 inhibitors may affect felodipine levels in plasma.

CYP3A4 induction drugs

The drug increases the metabolism of Felodipine by touch P450, such as: Carbamazepine, Phenytoin, Barbiturate drugs such as Phenobarbital, Rifampicin, Efavirenz, Nevirapine, as well as St. John (Hypericum Perforatum). When used with carbamazepine, phenytoin and phenobarbital, the concentration below the AUC curve of Felodipine has decreased by 93% and CMAX decreased by 82%. Should avoid coordination with CYP3A4 induction drugs.

CYP3A4 inhibitors

Strong CYP3A4 inhibitors such as Azole antifungal drugs (iTraconazole, ketoconazole) and macrolid antibiotics (erythromycin) and enamel inhibitors of HIV virus. Simultaneous use with iTraconazole as Felodipine's CMAX increased eight times and the AUC increased six times. Simultaneous use with erythromycin leads to cmax and auc of felodipine about 2.5 times. Should avoid coordination with strong CYP3A4 inhibitors.

Grapefruit juice inhibits CYP3A4. Using Felodipine along with grapefruit juice, the cmax and auc of Felodipine increases about twice. Should avoid taking medicine with grapefruit juice.

cimetidine

Simultaneous use of felodipine with cimetidine increases cmax and auc of felodipine about 55%.

Other interactions