Phenigidine, pills 10mg, 50pcs

Composition

1 tablet contains 0.01 g of phenigidine;

excipients:

potato or corn starch,

milk

sugar, refined sugar,

calcium stearate,

tween-80.

Pharmacological action

Pharmaceutical group:

blocker of “slow” calcium channels.

Pharmaceutical action:

 Selective BMCC, a 1,4-dihydropyridine derivative. It has vasodilating, antianginal and hypotensive effects. Reduces the flow of Ca2+ into cardiomyocytes and smooth muscle cells of coronary and peripheral arteries; in high doses, it suppresses the release of Ca2+ from intracellular depots. Reduces the number of functioning channels, without affecting the time of their activation, inactivation and recovery.

It separates the processes of excitation and contraction in the myocardium mediated by tropomyosin and troponin, and in vascular smooth muscles mediated by calmodulin. In therapeutic doses, it normalizes the transmembrane Ca2+ current, which is disturbed in a number of pathological conditions, primarily in arterial hypertension. It does not affect the tone of the veins. Increases coronary blood flow, improves blood supply to ischemic areas of the myocardium without the development of the phenomenon of “stealing”, activates the functioning of collaterals. By dilating the peripheral arteries, it reduces OPSS, myocardial tone, afterload, and myocardial oxygen demand, and increases the duration of LV diastolic relaxation. Practically does not affect the SA and AV nodes and has no antiarrhythmic activity. Increases renal blood flow, causes moderate natriuresis.

The negative chrono -, dromo -, and inotropic effects are overlaid by reflex activation of the sympathoadrenal system and an increase in heart rate in response to peripheral vasodilation.

Time of onset of the effect: 20 minutes – for oral use,5 minutes – for sublingual use of capsule contents; duration of the effect: 4-6 hours – for tablets and capsules,12-24 hours – for prolonged forms.

Pharmacokinetics:  

Absorption is high (more than 92-98%). Bioavailability – 40-60%. Food intake increases bioavailability. It has a “first pass” effect through the liver. Retard forms provide a gradual release of the Active ingredient into the systemic circulation. TCmax and Cmax depend on the dosage form: 1-2 h for capsules (in the case of sublingual use-0.5-1 h); 1-3 h and 65 ng / ml for 10 mg tablets; 1.6-4.2 h and 47-76 ng/ml for 20 mg retard tablets; 1.2-4 h for 30 mg retard tablets. Plasma protein binding is 90%.

When administered intravenously, T1 / 2 lasts 3.6 hours, the volume of distribution is 3.9 l / kg, plasma clearance is 900 ml / min, and Css is 17 ng / ml. Penetrates the BBB and placental barrier, is excreted in breast milk.

It is completely metabolized in the liver. CYP3A4, CYP3A5 and CYP3A7 isoenzymes are involved in drug metabolism. T1 / 2 for tablets of 10 mg, capsules-2-4 hours, for retard tablets-3.8-16.9 hours. In patients with hepatic insufficiency, total clearance decreases and T1 increases/2. It is excreted as inactive metabolites mainly by the kidneys (80%) and with bile (20%).

There is no cumulative effect. CRF, hemodialysis and peritoneal dialysis do not affect the pharmacokinetics. With prolonged use (2-3 months), tolerance to the drug develops. Plasmapheresis may increase elimination.

Indications

Prevention and treatment of angina attacks; arterial hypertension of various origins, hypertensive crisis.

Contraindications

Hypersensitivity to Phenigidine, cardiogenic shock, hypotension, tachycardia, acute period of myocardial infarction (first 8 days), heart failure, pregnancy, childhood.

Since Phenigidine is excreted in breast milk, its use during lactation should be avoided or breast-feeding should be discontinued during treatment

Side effects

Side effects occur mainly at the beginning of treatment, usually mild and temporary. More than 1% of patients may experience headache, hyperemia of the skin of the face and other parts of the body, accompanied by a burning sensation (erythema, erythromegaly), palpitations, swelling of the lower legs (associated with vasodilation), dizziness, fatigue, nausea, a feeling of heaviness in the stomach, diarrhea, constipation; less than 1% of cases may experience shortness of breath, myalgia, tremor, increased excitability, paresthesia, tachycardia, hypotension, skin rash and pruritus; less than 0.1% of patients (some elderly men, with long-term therapy) may develop gynecomastia, which completely regresses after discontinuation of the drug; with long-term treatment, gum hyperplasia may also disappear completely after discontinuation of the drug.

Very rarely, initial hyperglycemia, transient visual disturbances, increased daily diuresis (may be considered a positive effect with elevated blood pressure), impaired liver function (increased transaminases, intrahepatic cholestasis), exfoliative dermatitis, photosensitization, systemic allergic reactions, thrombocytopenic purpura, agranulocytosis are observed; these phenomena disappear after discontinuation of the drug. As a result of a decrease in blood pressure, a collapse may develop.

A sharp decrease in blood pressure due to vasodilation is possible in patients on dialysis, with malignant arterial hypertension and hypovolemia. When treating patients with stable angina pectoris within 1 hour after taking Phenigidine, pain behind the sternum may appear in the type of angina pectoris.

In some patients, usually at the beginning of treatment, it is possible to increase the frequency, duration and severity of angina attacks, which requires discontinuation of the drug.

Interaction

The antihypertensive effect of Phenigidine may be enhanced by concomitant use of other antihypertensive agents. Cimetidine increases the plasma level of nifedipine and may enhance the antihypertensive effect of Phenigidine.

When combined with adrenergic blockers, hypotension and heart failure may develop. Phenigidine reduces the clearance of digoxin and increases its concentration in the blood serum; regular monitoring and, if necessary, reducing the dose of digoxin is necessary.

With simultaneous use of Phenigidine and quinidine, in some cases, a decrease was observed, and after the withdrawal of Phenigidine, a significant increase in quinidine in blood plasma was observed.

When prescribing or discontinuing the drug against the background of quinidine therapy, it is recommended to monitor the level of quinidine and, if necessary, adjust its doses. The use of Phenigidine in combination with rifampicin is contraindicated (due to the inducing effect on liver enzymes, rifampicin accelerates the metabolism of Phenigidine and may weaken its therapeutic effect).

Diltiazem reduces the clearance of Phenigidine; both drugs should be administered simultaneously with caution, if necessary, reduce the dose of Phenigidine. Incompatibility with radiopaque agents was not noted.

How to take, course of use and dosage

The drug is taken orally, without chewing, with a small amount of liquid, regardless of food intake. Simultaneous food intake slows down, but does not reduce the degree of absorption of the drug (some foods affect the bioavailability of the drug). The dose is set individually.

The initial dose for adults is 10 mg (1 tablet),3-4 times a day. If necessary, the dose is gradually increased to 20 mg,3-4 times a day. The maximum daily dose is 120 mg.

To stop an attack of angina pectoris or hypertensive crisis, the drug is used sublingually: 1 tablet of 0.01 g is chewed and placed under the tongue; after a while (5-10 minutes), you can swallow the drug with a small amount of water, while it is recommended to be in a supine position for 30-60 minutes. The duration of treatment is determined by the doctor.

Overdose

Symptoms: headache, hyperemia of the facial skin, prolonged systemic hypotension, bradycardia, bradiarrhythmia.

With severe poisoning, collapse, sinus node depression is possible.

Treatment: use of norepinephrine, intravenous use of calcium chloride or calcium gluconate in atropine solution.

Special instructions

Special care should be taken when prescribing the drug to patients with significantly reduced blood pressure (systolic pressure below 90 mm Hg), with severe heart failure or aortic stenosis. If liver function is impaired, patients should be carefully monitored, and if necessary, the dose of Phenigidine should be reduced.

The drug can affect the psychophysical abilities of the body, weakening attention and slowing down responses, especially when drinking alcohol at the same time.

The use of grapefruit juice during treatment with Phenigidine may lead to an increase in the concentration of the drug in the blood plasma and increase its hypotensive effect.

Taking Phenigidine may cause a false increase in the level of vanillyl-mandelic acid in the urine during spectrophotometric examination; the results of determining this indicator by high-pressure liquid chromatography are not distorted.

Form of production

Pills.

Storage conditions

Keep out of the reach of children, dry, protected from light, at a temperature of 8 ° C to 15 ° C.

Shelf

life is 3 years.

Active ingredient

Nifedipine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Hypertension, Angina