Felotens retard, 5 mg 30 pcs

Pharmacotherapeutic group:

Slow calcium channel blocker

ATC code: C08CA02

Indications

– Arterial hypertension (in monotherapy or in combination with other hypotensive agents, such as beta-adrenoblockers, diuretics and ACE inhibitors);

Stable angina (in monotherapy and in combination with beta-adrenoblockers).

Active ingredient

Composition

1 long-acting film-coated tablet contains:

the active ingredient:

felodipine 5 mg;

auxiliary substances:

hypromellose (hydroxypropyl methylcellulose) 70 mg,

calcium hydrophosphate dihydrate 21 mg,

silicon dioxide colloid 1.5 mg,

lactose monohydrate 72 mg,

magnesium stearate 1 mg,

sodium alginate 2 mg,

povidone K-30 7.5 mg;

composition of the film coating:

Opadray II Yellow 6 mg, including: polyvinyl alcohol 2.4 mg, macrogol (polyethylene glycol) 1.21 mg, talc 0.89 mg, titanium dioxide 1.41 mg, iron oxide yellow dye 0.09 mg.

How to take, the dosage

Ingestion, preferably with water, on an empty stomach or with a small amount of food low in fat and carbohydrates.

The tablet should not be divided, crushed or chewed.

Arterial hypertension

The dose is always determined individually. Therapy begins with a dose of 5 mg once daily. If necessary, the dose 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 elderly patients or patients with impaired liver function, the recommended starting dose is 2.5 mg once daily. The maximum daily dose is 10 mg.

Stable angina pectoris

The dose is always determined individually. Treatment begins with a dose of 5 mg once daily; if necessary, the dose can be increased to 10 mg once daily.

Phelotensis® retard may be used in combination with beta-adrenoblockers, ACE inhibitors or diuretics. Combination therapy usually increases the antihypertensive effect of the drug. It is necessary to beware of the development of arterial hypotension. In patients with impaired renal function the drug pharmacokinetics does not change significantly. Caution is necessary in patients with impaired renal function (CKD less than 30 ml/min).

Interaction

Digoxin: Felodipine increases the plasma concentration of digoxin, but there is no need to change the dose of felodipine.

CYP3A4 isoenzyme inhibitors (cimetidine, erythromycin, itraconazole, ketoconazole) slow down the metabolism of felodipine in the liver, increasing the plasma concentration of the drug.

The inducers of CYP3A4 isoenzyme (phenytoin, carbamazepine, rifampicin, barbiturates, phenobarbital, preparations of St John’s Wort) decrease AUC (area under pharmacokinetic curve “concentration-time”) of felodipine by 93 % and Cmax by
82 %. Concomitant administration should be avoided.

Non-steroidal anti-inflammatory drugs do not impair the antihypertensive effect of felodipine.

Warfarin: The high protein binding capacity of felodipine does not affect the binding capacity of the free warfarin fraction.

Beta-adrenoblockers, verapamil, tricyclic antidepressants and diuretics enhance the antihypertensive effect of felodipine.

The azole antimicrobials (ketoconazole, itraconazole) together increase AUC of felodipine by 8 times and Cmax by 6 times.

Macrolide antibiotics (erythromycin): co-administration increases AUC and Cmax of felodipine by 2.5 times.

HIV protease inhibitors also increase the blood concentration of felodipine.

Grapefruit juice increases AUC and Cmax of felodipine by 2-fold, so felodipine should not be used simultaneously with grapefruit juice.

Tacrolimus: Felodipine increases plasma concentrations of tacrolimus when used together (monitoring of plasma tacrolimus concentrations 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

Felotense® retard should be administered with caution in patients with a tendency to tachycardia and severe left ventricular dysfunction. As well as other vasodilators, in rare cases felodipine 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 pulmonary diseases, impaired renal function, diabetes, gout, hyperlipidemia, Raynaud’s syndrome, and after lung transplantation.

Phelotensis® retard has no effect on blood glucose concentration and lipid profile. Hyperglycemia has been noted only in isolated cases.

With impaired renal function there is no effect on the drug concentration in plasma, therefore no dose adjustment is required in patients with impaired renal function. However, caution should be exercised when prescribing the drug in patients with renal impairment.

Careful oral hygiene is necessary because of possible development of gum hyperplasia and gingivitis.

Impact on ability to drive vehicles and machines Patients who have dizziness or weakness during treatment with Felotens®retard should avoid driving motor transport and work requiring increased concentration and rapid psychomotor reaction.

Contraindications

– hypersensitivity to felodipine and other dihydropyridine-type derivatives;

– unstable angina pectoris;

– acute myocardial infarction and within one month of myocardial infarction;

– cardiogenic shock;

Hemodynamically significant aortic and mitral stenosis;

– hypertrophic obstructive cardiomyopathy;

– pregnancy and lactation;

– decompensated chronic heart failure;

– Severe arterial hypotension;

– lactase deficiency, lactose intolerance, glucose-galactose malabsorption;

– Age less than 18 years (effectiveness and safety not established).

With caution

Hepatic impairment, severe renal failure (creatinine clearance (CK) less than 30 ml/min), aortic and mitral stenosis, BP lability and heart failure after myocardial infarction, advanced age.

Side effects

As with other slow calcium channel blockers, the drug may cause facial redness, headache, palpitations, dizziness and increased fatigue. These reactions are reversible and most often occur at the beginning of treatment or when the drug dose is increased. Also, depending on the dose, peripheral edema may appear, which is a consequence of precapillary vasodilation. Mild swelling of the gums may occur in patients with gum inflammation or periodontitis. This can be counteracted by good oral hygiene practices.

WHO (World Health Organization) classification for the incidence of side effects:

often, ≥1/100 to < 1/10 appointments (>1% and < 10%);

infrequent, ≥1/1000 to < 1/100 appointments (>0.1% and < 1%);

rarely, ≥1/10000 to < 1/1000 appointments (>0.01% and < 0.1%);

very rarely, < 1/10000 appointments (< 0.01%).

Cardiovascular system disorders

often – “flushes” of blood to the skin of the face accompanied by facial hyperemia, swelling of ankles;

infrequent – tachycardia, palpitations, marked BP decrease accompanied by reflex tachycardia and worsening of the course of angina pectoris;

very rarely – extrasystole, leukocytoclastic vasculitis.

Nervous system disorders

often – headache;

infrequently – paresthesia, dizziness;

rarely – syncope.

Digestive system disorders

infrequent – nausea, abdominal pain;

rarely – vomiting;

Overdose

Symptoms: In overdose, symptoms of intoxication appear 12-16 hours after taking the drug, sometimes symptoms may occur several days after taking the drug. The following symptoms may be noted: pronounced BP decrease, bradycardia, AV (atrioventricular) block of degree I-III, ventricular extrasystole, atrial-ventricular dissociation, asystole, ventricular fibrillation; headache, dizziness, impaired consciousness (or coma), seizures; dyspnea, pulmonary edema (non-cardiac) and apnea; in adults, respiratory distress syndrome may develop; acidosis, hypokalemia, hyperglycemia, hypocalcemia; flushed face, hypothermia; nausea, vomiting.

Treatment: Gastric lavage, administration of activated charcoal, in some cases effective even in the late stage of intoxication. Specific antidote – calcium preparations. With a pronounced decrease in BP, the patient should be given a horizontal position, legs elevated. If bradycardia develops, an IV injection of atropine at a dose of 0.25-0.5 mg is indicated and should be administered before gastric lavage, due to the risk of vagus nerve stimulation. ECG monitoring. Provide airway patency and adequate ventilation if necessary. Correction of acid-base status and serum electrolytes is indicated. In case of bradycardia and AV block, administer atropine 0.5-1.0 mg v/v, repeat administration if necessary, or initially administer isoprenaline 0.05-0.1 µg/kg/min. In early acute intoxication, an artificial pacemaker may be necessary. BP decrease is corrected by IV fluid administration (dextrose solution, 0.9% sodium chloride solution, dextran). Adults are given calcium gluconate solution 20-30 ml by IV for
5 min, and the same dose is repeated if necessary. If necessary, norepinephrine (adrenaline) or dopamine is administered by infusion. Glucagon may be administered in acute intoxication. Diazepam is prescribed for convulsions.

Similarities