Felodip, sustained release pills 2.5mg 30pcs

Composition

1 tablet of prolonged action, film-coated, contains:

Active ingredient:

felodipine 2.5 mg

. excipients:

lactose monohydrate,

microcrystalline cellulose,

hypromellose,

povidone,

propyl gallate,

magnesium stearate,

colloidal anhydrous silicon,

iron oxide yellow,

iron oxide red,

titanium dioxide,

talc,

propylene glycol.

Pharmacological action

Pharmacodynamics

Felodip belongs to the “slow” calcium channel blockers of the dihydropyridine series. It has a hypotensive, antianginal effect.

Reduces blood pressure (BP) by reducing peripheral vascular resistance. It has a dose-dependent anti-ischemic effect. Reduces the size of myocardial infarction, protects against reperfusion complications. Practically does not have a negative inotropic effect, has a minimal effect on the conducting system of the heart.

Pharmacokinetics

Absorption and distribution

The delayed release of felodipine from coated tablets leads to an elongation of the absorption phase of the drug and ensures a uniform concentration of felodipine in the blood plasma for 24 hours. Felodipine is almost completely absorbed in the gastrointestinal tract. Bioavailability is independent of the dose within the therapeutic interval and is approximately 15%.99% of felodipine binds to blood proteins, primarily albumins.

Felodipine is completely metabolized in the liver, and all its metabolites are inactive. The elimination half-life of felodipine is 25 hours. With prolonged use, felodipine accumulation does not occur.

Pharmacokinetics in special groups of patents

In elderly patients and in cases of impaired liver function, the concentration of felodipine in blood plasma is higher than in young patients. The pharmacokinetic parameters of felodipine do not change in patients with impaired renal function, including during hemodialysis. About 70% of the dose taken is excreted in the urine, and the rest is excreted in the feces in the form of metabolites. Less than 0.5% of the dose is excreted unchanged in the urine. Felodipine passes through the blood-placental barrier into the placenta and is excreted in breast milk.

Indications

Arterial hypertension, stable angina pectoris (including Prinzmetal angina pectoris)

Contraindications

• Hypersensitivity to felodipine and other dihydropyridine derivatives
• Unstable angina pectoris
• Acute myocardial infarction and within one month after the previous myocardial infarction
• Cardiogenic shock
• Clinically significant aortic stenosis
• Pregnancy and lactation
• Chronic heart failure in the stage of decompensation
• Severe arterial hypotension
• Age up to 18 years (efficacy and safety have not been established)

With caution, hepatic and / or renal failure, aortic stenosis, lability of blood pressure and heart failure after myocardial infarction

Side effects

As with other slow-acting calcium channel blockers, the drug can cause facial flushing, headache, palpitations, dizziness, and increased fatigue.

These reactions are reversible and most often occur at the beginning of treatment or with an increase in the dose of the drug. Also, depending on the dose, peripheral edema may appear, which are a consequence of precapillary vasodilation. Patients with gum disease or periodontitis may experience mild swelling of the gums. This can be prevented by careful oral hygiene.

The frequency of side effects is determined by the following definitions: common (1/100 or more), less common (1/1000-1/100) rare (1/10000-1/1000), very rare (less than 1/10000).

From the cardiovascular system: often – “hot flashes” of blood to the skin of the face, accompanied by facial hyperemia, swelling of the ankles; less often – tachycardia, palpitation; rarely – fainting; very rarely – extrasystole, a pronounced decrease in blood pressure, accompanied by reflex tachycardia and worsening of angina, leukocytoclastic vasculitis.

From the nervous system: often-headache; less often-paresthesia, dizziness.

From the digestive system: less often-nausea, abdominal pain; rarely-vomiting; very rarely-increased activity of “liver” transaminases; rarely – hyperplasia of the gums, tongue mucosa, gingivitis.

Musculoskeletal disorders: rarely-arthralgia, myalgia.

Allergic reactions: less often-skin rash, pruritus; rarely-urticaria; very rarely-angioedema of the lips or tongue, photosensitization reaction.

From the urinary system: very rarely-frequent urination.

Others: less often – fatigue; rarely-impotence/sexual dysfunction; very rarely-fever, hyperglycemia.

From the skin: rarely-urticaria and pruritus. In isolated cases – photosensitization reactions.

No causal relationship has been established: chest pain, facial edema, flu-like syndrome, decreased blood pressure, myocardial infarction, syncope, angina pectoris, arrhythmia, extrasystole, diarrhea, dry mouth, flatulence, gynecomastia, anemia, arthralgia, back pain, myalgia, upper and lower limb pain, depression, insomnia, anxiety, nervousness, drowsiness, irritability, pharyngitis, shortness of breath, bronchitis, flu, sinusitis, nosebleeds, erythema, bruising, leukocytoclastic vasculitis, visual impairment, polyuria, dysuria.

Interaction

Felodipine increases the concentration of digoxin in blood plasma, but changes in the dosage of felodipine are not required. Cytochrome p450 inhibitors (for example, cimetidine, erythromycin, itraconazole, ketoconazole) slow down the metabolism of felodipine in the liver, increasing the concentration of the drug in blood plasma.

Inducers of microsomal enzymes (phenytoin, carbamazepine, rifampicin, barbiturates) reduce the concentration of felodipine in blood plasma. Nonsteroidal anti-inflammatory drugs do not weaken the hypotensive effect of felodipine.

The high degree of protein binding of felodipine does not affect the binding of the free fraction of other drugs (for example, warfarin). Do not use felodipine at the same time as grapefruit juice. Beta-blockers, verapamil, tricyclic antidepressants and diuretics enhance the hypotensive effect of felodipine.

Cytochrome P 450 inhibitors (cimetidine, erythromycin, ketoconazole, itraconazole, HIV protease inhibitors, grapefruit juice), slowing down the metabolism of the drug in the liver, increase its concentration in plasma: with itraconazole, the AUC of felodipine increases by 8 times, Cmax-by 6 times, with erythromycin – AUC and Cmax by 2.5 times, with grapefruit juice-by 2 times, respectively.

Inducers of microsomal oxidation-phenytoin, carbamazepine, phenobarbital, rifampicin, tincture of St. John’s wort-reduce the AUC of felodipine by 93% and Cmax-by 82%.

Increases the concentration of tacrolimus in blood plasma when used together (it is recommended to monitor the concentration of tacrolimus in blood plasma and possible dose adjustment).

Cyclosporine increases the Cmax of felodipine by 150%, AUC by 60% (the effect of felodipine on the pharmacokinetic parameters of cyclosporine is minimal). Cimetidine increases the Cmax and AUC of felodipine by 55%.

How to take, course of use and dosage

The drug is best taken orally in the morning, before meals or after a light breakfast. Coated tablets should not be chewed, divided, or crushed.

Arterial hypertension

Adults (including the elderly): The dosage is always determined individually. Therapy begins with a dose of 5 mg once a day. If necessary, the dosage can be increased; usually the maintenance dose is 5-10 mg once a day. To determine the individual dose, it is best to use tablets containing 2.5 mg of felodipine. In the elderly or patients with impaired liver function, the recommended initial dosage is 2.5 mg once a day.

Stable angina pectoris

Adults: The dosage is always determined individually. Treatment begins with a dose of 5 mg once a day, if necessary, you can increase the dose to 10 mg once a day. The maximum daily dose is 20 mg once a day.

Felodip may be used in combination with beta-blockers, angiotensin converting enzyme (ACE) inhibitors, or diuretics.

Combination therapy usually increases the antihypertensive effect of the drug.

It is necessary to avoid the development of arterial hypotension. In patients with severe hepatic impairment, the therapeutic dose should be reduced.

In patients with impaired renal function, the pharmacokinetics of the drug does not change significantly.

Overdose

Symptoms: marked decrease in blood pressure, bradycardia.

Treatment: perform symptomatic therapy. With a pronounced decrease in blood pressure, the patient should be given a horizontal position, raise his legs. With the development of bradycardia, intravenous use of atropine at a dose of 0.5-1.0 mg is indicated.

If this is not enough, it is necessary to increase the volume of blood plasma by infusion of a solution of dextrose (glucose), sodium chloride or dextran. If the above measures are ineffective, symptomatic drugs with a predominant effect on alpha-adrenergic receptors are prescribed.

Special instructions

The drug felodip, as well as other vasodilators, in rare cases can cause significant arterial hypotension, which in a number of predisposed patients can lead to the development of myocardial ischemia. Currently, there are no data on the feasibility of using the drug as a secondary prevention of myocardial infarction.

Felodipine is effective and well tolerated by patients regardless of gender and age, as well as patients with concomitant diseases such as bronchial asthma and other lung diseases; impaired renal function; diabetes mellitus; gout; hyperlipidemia; Raynaud’s syndrome, as well as after lung transplantation.

Felodipine has no effect on blood glucose concentration and lipid profile.

Influence on the ability to drive motor vehicles and manage mechanisms:

patients who experience weakness or dizziness during treatment with felodipine should refrain from driving vehicles and work that requires increased attention and concentration.

Form of production

Film-coated long-acting tablets

Storage conditions

Store in a dry place protected from light at a temperature not exceeding 25°C. Keep out of reach of children.

Shelf

life is 4 years.

Active ingredient

Felodipine

Conditions of release from pharmacies

By prescription

Dosage form

long-acting tablets

Purpose

For adults as directed by your doctor

Indications

Angina, Hypertension