Felodip

Felodipine is an antihypertensive drug.

[ 1 ], [ 2 ], [ 3 ]

Indications Felodipa

It is used to eliminate the following diseases:

• angina pectoris;
• essential hypertension;
• spontaneous angina.

Release form

The medicine is released in tablets, 10 pieces per blister pack. The box contains 3 or 10 such packs.

Pharmacodynamics

According to the principle of medicinal action, it is a blocker of slow Ca channels. Its active element is a derivative of the component dihydropyridine. In addition to antihypertensive properties, the drug also has antianginal properties. A decrease in blood pressure values occurs due to a decrease in the indicators of total peripheral vascular resistance.

The intensity of the anti-ischemic effect depends on the dosage. Felodipine has the ability to protect against the development of reperfusion complications, as well as reduce myocardial volumes.

With respect to the conduction system, only a minimal effect is noted; the active element does not have a negative inotropic effect.

[ 4 ], [ 5 ], [ 6 ], [ 7 ], [ 8 ], [ 9 ], [ 10 ]

Pharmacokinetics

The active element is almost completely absorbed when it enters the gastrointestinal tract. After the first liver passage, intensive metabolic processes are observed. The drug is 99% synthesized with protein.

The active component is excreted with mother's milk during lactation, and in addition, it can pass through the BBB and placenta. Known products of drug metabolism do not have medicinal activity.

About 0.5% of the drug is excreted unchanged, another 70% is excreted as decay products through the kidneys, and the remainder is excreted through the intestines. At the α stage, the half-life is 4 hours, and at the β stage, 24 hours.

It is noted that in elderly people and people with liver diseases, the levels of felodipine in the blood are much higher than the values observed in the younger age group.

Long-term use of the drug does not cause accumulation of the active element. The only exceptions are patients with chronic renal failure, who experience accumulation of inactive metabolic products (in such cases, individual dosage adjustment is necessary).

Dosing and administration

The drug should be taken in the morning - before or after breakfast. It is forbidden to crush or chew the tablets.

Use of drugs to eliminate essential hypertension.

Antihypertensive treatment should be started with a minimum dose of 5 mg. If this dosage is ineffective, the dose should be increased to 10 mg. Felodipine is taken once a day.

If the patient suffers from liver pathologies, it is necessary to start therapy with a dose of 2.5 mg, while monitoring liver function indicators.

Therapy for stable angina.

The dosage size should be selected individually, the initial daily dose is 5 mg. The maximum daily dose is 20 mg.

If the patient is taking ACE inhibitors, β-blockers or diuretics together with the drug, dosage adjustments may be required to avoid a decrease in blood pressure.

If the patient has a disease affecting the liver, the dosage is selected individually.

[ 14 ]

Use Felodipa during pregnancy

The medicine should not be prescribed to breastfeeding mothers or pregnant women.

Contraindications

Main contraindications:

• aortic stenosis (the disease has a clinically significant expression);
• myocardial infarction (in the acute stage, up to 1 month);
• decompensated heart failure;
• marked decrease in blood pressure values;
• unstable angina;
• intolerance to the components of the drug;
• cardiogenic shock;
• children and adolescents under 18 years of age (since there is no information about the safety of the drug and the effectiveness of its use).

Caution is required when used in people with kidney and liver diseases - Felodipine should be taken with blood biochemical values monitored.

Side effects Felodipa

The use of the drug can provoke the development of such negative symptoms:

• rapid onset of fatigue;
• headaches of a pronounced nature (similar to migraine);
• redness of the skin on the face;
• increased heart rate;
• dizziness.

All the above symptoms disappear on their own after 2-3 weeks of therapy, and may reappear due to an increase in the dosage of the drug. Due to the development of precapillary vasodilation, peripheral edema may occur.

During periodontitis, swelling in the gum area is observed, which has a weak degree of expression. If oral hygiene is carefully observed, these manifestations quickly disappear.

Taking the drug often causes the following side effects: photosensitivity, skin itching, urticaria and Quincke's edema. In addition, arthralgia with myalgia, peripheral edema, gingival hyperplasia and paresthesia, as well as an increase in AST and ALT values.

[ 11 ], [ 12 ], [ 13 ]

Overdose

In case of poisoning, a decrease in blood pressure and a pronounced form of bradycardia are observed.

If such symptoms develop, the first aid is to lay the victim in a horizontal position and raise his legs. If bradycardia is observed, the patient is given 0.5-1 mg of atropine intravenously.

To increase the plasma volume, the patient should be given an infusion of dextran or glucose solution or NaCl solution. If these procedures do not produce results, the use of α-adrenergic stimulants is required.

Interactions with other drugs

Medicines that increase the levels of felodipine in the blood and inhibit its metabolism: cimetidine with erythromycin, as well as itraconazole with ketoconazole.

It was found that the combination with digoxin causes an increase in its indicators, but these changes do not require correction of the Felodipine portion sizes.

The level of the active element of the drug decreases when combined with drugs such as carbamazepine with barbiturates and phenytoin with rifampicin.

Medicines from the NSAID category do not affect the degree of expression of the antihypertensive properties of the drug. High values of the synthesis of the active element with plasma protein do not affect the process of synthesis of fractions of other drugs, including warfarin.

The antihypertensive effect is potentiated when the drug is combined with tricyclics, diuretics, β-blockers and verapamil.

Grapefruit juice contains flavonoids that can increase the bioavailability of felodipine, which is why it is strictly forbidden to take the medicine with this juice.

[ 15 ]

Storage conditions

Felodipine must be kept in standard conditions for medicinal preparations. Temperature level – within 10-25°C.

Shelf life

Felodipine is permitted to be used for 4 years from the date of release of the therapeutic agent.

Analogues

The medicine's analogues are Plendil and Felodipine.

Reviews

Felodipine is used quite infrequently compared to other MCC blockers (such as nifedipine with amlodipine, as well as lercanidipine). This is mainly due to the excessively high cost of the drug.

People who have used the drug comment on it in a positive way, noting the good tolerability of the drug and high medicinal effectiveness in the treatment of essential hypertension.

People suffering from angina pectoris, in their reviews, say that with prolonged therapy there is a noticeable improvement in the condition, angina pain sensations become less frequent and have less intensity.