Felodip, 2,5mg 30 pcs.

Pharmacodynamics

Phelodip refers to “slow” calcium channel blockers of the dihydropyridine series. It has hypotensive, antianginal action.

Limits 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. It has practically no negative inotropic effect and has minimal effect on the cardiac conduction system.

Pharmacokinetics

Absorption and distribution

Delayed release of felodipine from coated tablets results in a prolonged absorption phase of the drug and provides uniform plasma concentrations of felodipine 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 is bound to blood proteins, especially to albumin.

Metabolism and excretion

Felodipine is completely metabolized in the liver, and all its metabolites are inactive.
The elimination half-life of felodipine is 25 hours. There is no cumulation of felodipine with prolonged use.

Pharmacokinetics in special groups:

In elderly patients and in cases of hepatic dysfunction, plasma felodipine concentrations are higher than in younger patients. Pharmacokinetic parameters of felodipine do not change in patients with impaired renal function, including those under hemodialysis. About 70% of the administered dose is excreted with urine, and the rest with feces in the form of metabolites. Less than 0.5% of the administered dose is excreted unchanged in the urine. Felodipine penetrates through the blood-placental barrier to the placenta and is excreted with breast milk.

Indications

Arterial hypertension, stable angina pectoris (including Prinzmetal angina)

Active ingredient

Composition

1 film-coated sustained release tablet contains:

the active ingredient:

felodipine 2.5 mg.

Auxiliary substances:

Lactose monohydrate,

Microcrystalline cellulose,

How to take, the dosage

The drug is best taken in the morning orally, before meals or after a light breakfast.
Coated tablets should not be crushed, split 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, a starting dose of 2.5 mg once daily is recommended.

Stable angina pectoris

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

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

Combination therapy usually increases the hypotensive effect of the drug.

The development of arterial hypotension should be cautioned. In patients with significant hepatic impairment, the therapeutic dose should be decreased.

In patients with impaired renal function there is no significant change in pharmacokinetics of the drug.

Interaction

Cytochrome P450 inhibitors (e.g., cimetidine, erythromycin, itraconazole, ketoconazole) slow down the metabolism of felodipine in the liver, increasing the drug plasma concentration.

Microsomal enzyme inducers (phenytoin, carbamazepine, rifampicin, barbiturates) decrease the plasma concentration of felodipine. Nonsteroidal anti-inflammatory drugs do not weaken the hypotensive effect of felodipine.

The high degree of binding of felodipine to proteins does not affect the binding of the free fraction of other drugs (e.g., warfarin). Felodipine should not be used simultaneously with grapefruit juice. Beta-adrenoblockers, verapamil, tricyclic antidepressants and diuretics increase the hypotensive effect of felodipine.

Cytochrome P450 inhibitors (cimetidine, erythromycin, ketoconazole, itraconazole, HIV protease inhibitors, grapefruit juice), slowing the metabolism of the drug in the liver, increase its plasma concentration: with itraconazole – AUC of felodipine increases 8-fold, Cmax – 6-fold, with erythromycin – AUC and Cmax – 2.5 times, with grapefruit juice – 2 times, respectively.

Microsomal oxidation inducers – phenytoin, carbamazepine, phenobarbital, rifampicin, tincture of Saint John’s wort – decrease AUC of felodipine by 93% and Cmax – by 82%.

Induces plasma concentrations of tacrolimus when used together (monitoring of plasma concentrations of tacrolimus and possible dose adjustment is recommended).

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

Special Instructions

Felodip, as well as other vasodilators, in rare cases may cause significant arterial hypotension, which in some predisposed patients may 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 by patients with comorbidities such as bronchial asthma and other lung diseases; impaired renal function; diabetes; gout; hyperlipidemia; Raynaud’s syndrome; and after lung transplantation.

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

Impact on the ability to drive and operate machinery:

Patients who experience weakness and dizziness during treatment with felodipine should avoid driving and work requiring increased attention and concentration.

Contraindications

Side effects

As with other slow calcium channel blockers, the drug may cause redness of the face, headache, palpitations, dizziness and increased fatigue.

These reactions are reversible and most often occur at the beginning of treatment or when increasing the dose of the drug. Also, depending on the dose, peripheral edema may occur, which is a consequence of precapillary vasodilation. Mild swelling of the gums may occur in patients with gum inflammation or periodontitis. This may be counteracted by good oral hygiene practices.

The frequency of side effects is according to the following definitions: frequently (1/100 or more), less frequently (1/1000-1/100) rarely (1/10000-1/1000), very rarely (less than 1/10000).

In the cardiovascular system: frequently – “flushes” of blood to the skin of the face, accompanied by facial hyperemia, swelling of the ankles; less frequently – tachycardia, palpitation; rarely – syncope; very rarely – extrasystole, marked BP decrease, accompanied by reflex tachycardia and worsening of angina pectoris, leukocytoclastic vasculitis.

Nervous system disorders: frequently – headache; less frequently – paresthesia, dizziness.

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

Musculoskeletal system: rare – arthralgia, myalgia.

Allergic reactions: less frequently – skin rash, itching; rarely – urticaria; very rarely – angioedema of the lips or tongue, photosensitization reaction.

The urinary system: very rare – frequent urination.

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

Skin disorders: rare- urticaria and itching. In isolated cases – photosensitization reactions;

The cause-and-effect relationship has not been established: chest pain, facial edema, flu-like syndrome, decreased BP, myocardial infarction, syncope, angina pectoris, arrhythmia, extrasystole, diarrhea, dry mouth, flatulence, gynecomastia, anemia, arthralgia, back pain, myalgia, pain in the upper and lower extremities, depression, insomnia, anxiety, nervousness, drowsiness, irritability, pharyngitis, shortness of breath, bronchitis, flu, sinusitis, nasal bleeding, erythema, bruising, leukocytoclastic vasculitis, visual disturbances, polyuria, dysuria.

Overdose

Symptoms: marked BP decrease, bradycardia.

Treatment: symptomatic therapy is carried out. In marked BP decrease the patient should be given a horizontal position, legs should be elevated. If bradycardia develops, intravenous injection of atropine in a dose of 0.5-1.0 mg is indicated.

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

Similarities