Pharmadipin oral drops 2% 5ml — Made in Ukraine — Free Delivery

Pharmacological properties

Pharmacodynamics. Pharmadipin exhibits antianginal and antihypertensive effects. blocks the entry of calcium ions into cardiomyocytes and smooth muscle cells of coronary and peripheral arteries through slow voltage-gated calcium channels of cell membranes. relaxes vascular smooth muscles, eliminates spasms and expands coronary and peripheral arteries, reducing the opsis, blood pressure, afterload and myocardial oxygen demand; slightly reduces myocardial contractility, somewhat reduces platelet aggregation.

Pharmacokinetics. When taken orally, it is well absorbed in the digestive tract, bioavailability is 40-60%. The effect develops especially quickly (after 5-10 minutes) with sublingual administration. Typically, the maximum action is recorded in 30-40 minutes. Food intake does not significantly affect the rate of absorption of the preparation. The hemodynamic effect persists for 4-6 hours. Up to 90% of nifedipine binds to plasma proteins. It is metabolized in the liver and excreted from the body mainly in the form of inactive metabolites. The total clearance of nifedipine is 0.4–0.6 l / kg / h. T½ is 2–4 hours. In the elderly and patients with cirrhosis of the liver, the metabolism of nifedipine slows down, so their T½ of the preparation can be lengthened by almost 2 times, which requires a dose reduction and an increase in the intervals between doses of the preparation. In the body, nifedipine does not accumulate. In small amounts, it penetrates the BBB and the placental barrier, excreted in breast milk.

Indications

Ag (for the treatment of hypertensive crises).

Application

Pharmadipin is used for the treatment of hypertensive crisis as an emergency preparation. it is not recommended to use the preparation in this dosage form for course administration.

If it is necessary to conduct a course of antihypertensive therapy, the preparation and the dosage form are selected by the doctor.

With a sudden and significant increase in blood pressure, the initial single dose for adults is 3-5 drops (2-3.35 mg), for the elderly - no more than 3 drops (2 mg) under the tongue or drip on a piece of bread or sugar, as possible holding in the mouth longer. In case of insufficient effectiveness, the dose can be gradually increased to a clinically significant effect. In the future, in cases of increased blood pressure, it is necessary to focus on this dose. If necessary (increase in blood pressure to 190/100–220/110 mm Hg), a single dose can be gradually increased in some cases to 10–15 drops (6.7–10 mg), taking into account individual changes in the patient's blood pressure.

It is necessary to take into account the individual sensitivity of individual patients to Pharmadipin. In such cases, the dose is selected individually, starting with 3 drops, and gradually increased by 2-3 drops (1.34-2 mg) until a clinical effect is achieved.

Exceeding the initial dose of the preparation can lead to a sharp decrease in blood pressure!

Contraindications

Acute myocardial infarction (first 4 weeks); cardiogenic shock; severe aortic and mitral stenosis; unstable angina; do not use for the treatment of angina attacks, secondary prevention of myocardial infarction; heart failure in the stage of decompensation; arterial hypotension (systolic blood pressure 90 mm Hg); ventricular tachycardia with extended qrs complex; sick sinus syndrome; wolff-parkinson-white syndrome (wpw), laun-genong-levine syndrome (lgl); av-blockade ii and iii degrees; porphyria; ileostomy, installed after proctocolectomy; period of pregnancy; period of breastfeeding; childhood; hypersensitivity to nifedipine and other components of the preparation; hypersensitivity to other dihydropyridines; do not take at the same time with rifampicin.

Side effects

Subject to the recommendations for the use of the preparation, side effects are insignificant and transient, as a rule, do not require discontinuation of therapy.

With frequent and uncontrolled use, side reactions typical for preparations of this pharmacological group are possible.

From the side of the cardiovascular system: often - edema, vasodilation, infrequently - tachycardia, increased heart rate, arterial hypotension, syncope.

From the side of the central and peripheral nervous system: often - headache; infrequently - vertigo, migraine, dizziness, tremor, sleep disorder, anxiety; rarely - short-term visual impairment, agitation, paresthesia, dysesthesia.

From the endocrine system: hyperglycemia (should be considered in patients with diabetes mellitus).

From the digestive system: often - constipation; infrequently - when using high doses, abdominal pain, dyspeptic symptoms, flatulence, nausea, vomiting (very rare), gingival hyperplasia (with prolonged use), dry mouth, transient increase in liver enzymes.

From the urinary system: infrequently - polyuria, dysuria.

From the hematopoietic system: rarely - anemia, leukopenia, thrombocytopenia.

Allergic reactions: infrequently - allergic reaction, allergic edema / angioedema (including laryngeal edema); rarely - itching, urticaria, rash; very rarely - anaphylactic / anaphylactoid reactions.

Others: often - feeling unwell; infrequently - epistaxis, nasal congestion, erythema; rarely - leg edema, muscle cramps, joint edema, erectile dysfunction, nonspecific pain, fever, dyspnea.

Special instructions

The preparation should be used only under conditions of close clinical observation of the patient: with unstable angina pectoris, severe heart failure and severe aortic stenosis, severe pulmonary hypertension, hypertrophic cardiomyopathy, severe cerebrovascular accidents, diabetes mellitus, impaired liver and kidney function, as well as elderly patients. in elderly patients, a decrease in cerebral blood flow is more likely due to a sharp peripheral vasodilation. in patients with malignant arthritis and hypovolemia, who are on hemodialysis, while taking nifedipine, a significant decrease in blood pressure can be observed. especially at the beginning of treatment and with the simultaneous use of β-receptor blockers, hypotension may develop, which some patients do not tolerate well. the condition of such patients must be closely monitored. in patients taking β-receptor blockers, signs of congestive heart failure may appear at the beginning of treatment. in patients with severe coronary insufficiency due to reflex tachycardia, the course of coronary heart disease may worsen, and at the same time, angina attacks may become more frequent. nifedipine should be used with caution in patients with angina pectoris or after a heart attack. if nifedipine appears on the background of treatment of pain behind the sternum, it should be canceled. you should not drink alcohol or smoke during treatment with nifedipine.

Doses of other preparations used with nifedipine should be set on an individual basis. Cardiac glycosides can also be used during treatment with nifedipine. With the use of nifedipine, a false increase in the results of the spectrophotometric determination of the concentration of vanilyl mandelic acid in urine is possible.

When using nifedipine with simultaneous intravenous administration of magnesium sulfate, pregnant women need careful monitoring of blood pressure because of the possibility of its decrease, which can harm the mother and the fetus.

Patients with impaired liver function require careful monitoring, and in severe cases, dose reduction.

Nifedipine is metabolized through the cytochrome P450 3A4 system. Therefore, preparations that inhibit or induce this enzyme system can alter the first-pass effect or clearance of nifedipine (see INTERACTIONS).

With the concomitant use of nifedipine with these preparations, it is necessary to control blood pressure and, if necessary, consider reducing the dose of nifedipine.

Separate in vitro experiments have revealed a relationship between the use of calcium antagonists, in particular nifedipine, and reverse biochemical changes in spermatozoa, which impair the ability of the latter to fertilize. In the event that an in vitro fertilization attempt has failed in the absence of other explanations, calcium antagonists, in particular nifedipine, can be considered as a possible cause of this phenomenon.

The ability to influence the reaction rate when driving or working with other mechanisms. When using the preparation, one should refrain from potentially hazardous activities that require increased attention (driving, working with other mechanisms, etc.).

Use during pregnancy and lactation. Nifedipine is contraindicated during pregnancy. Nifedipine passes into breast milk, therefore, breastfeeding should be discontinued while using the preparation.

Children. The preparation is not used to treat children.

Interactions

Nifedipine can increase the severity of the antihypertensive effect of antihypertensive preparations that are used simultaneously, such as diuretics, β-receptor blockers, APF inhibitors, AT1-receptor antagonists, other calcium antagonists, α-adrenergic receptor blockers, FDE-5, α-methyldopa inhibitors.

When combined with β-receptor blockers, along with an increase in the hypotensive effect, in some cases the development of heart failure is possible.

Diltiazem slows down the elimination of nifedipine from the body (if necessary, reduce the dose of nifedipine).

Amiodarone and quinidine can enhance the negative inotropic effect of nifedipine. In some cases, with a combination of nifedipine and quinidine when taken orally, there is a decrease in the concentration of quinidine in the blood plasma.

Combinations of nifedipine with cardiac glycosides, theophylline are usually well tolerated by patients; in very rare cases, an increase in the level of digoxin and theophylline in the blood plasma is possible (the content of the latter in the blood plasma should be monitored).

Nifedipine increases the concentration of carbamazepine, phenytoin in blood plasma. The combined use of nifedipine and cimetidine can lead to an increase in the level of nifedipine in the blood plasma.

Rifampicin induces the activity of liver enzymes, accelerating the metabolism of nifedipine, which may lead to a decrease in the clinical effect of nifedipine (this combination is contraindicated).

Treatment with nifedipine should be discontinued 36 hours before planned anesthesia with fentanyl. Nifedipine is compatible with X-ray contrast agents.

Nifedipine in combination with IV administration of magnesium sulfate in pregnant women can cause neuromuscular blockade.

Nifedipine is metabolized through the cytochrome P450 3A4 system located in the intestinal and liver mucosa. Based on this, preparations that inhibit or induce this enzyme system can alter the first pass effect (after oral administration) or the clearance of nifedipine. Concomitant use of macrolide antibiotics (eg erythromycin), anti-HIV protease inhibitors (eg ritonavir), azole antimycotics (eg ketaconazole), nefazodone, fluoxetine, quinupristine / dalfopristine, cimetidine, cisapride and nifedipine may lead to an increase in the concentration of nifedipine in blood plasma.

It is known that valproic acid increases the plasma concentration of a structurally similar calcium channel blocker nimodipine due to enzyme inhibition. Therefore, an increase in the concentration and effectiveness of nifedipine in blood plasma cannot be ruled out.

Tacrolimus is known to be metabolized through the cytochrome P450 3A4 system.

Published data indicate that in some cases, the dose of tacrolimus can be reduced when used concomitantly with nifedipine. With the simultaneous use of two preparations, monitor the concentration of tacrolimus in blood plasma and, if necessary, consider reducing the dose of tacrolimus.

Grapefruit juice inhibits the cytochrome P450 3A4 system. The use of grapefruit juice with the use of nifedipine leads to an increase in the concentration of the preparation in the blood plasma and an increase in the duration of action of nifedipine due to a decrease in metabolism during the first passage or a decrease in clearance. Because of this, the antihypertensive effect of the preparation may increase. After drinking grapefruit juice regularly, this effect can last for up to 3 days after the last juice intake.

Therefore, during therapy with nifedipine, the use of grapefruit / grapefruit juice should be avoided.

The use of nifedipine can lead to false results in the spectrophotometric determination of the concentration of vanilyl mandelic acid in urine (this effect was not observed when using the method of high performance liquid chromatography).

Overdose

Symptoms of acute intoxication with nifedipine: impaired consciousness up to coma, decreased blood pressure, tachycardia / bradycardia, hyperglycemia, metabolic acidosis, hypoxia, cardiogenic shock, which is accompanied by pulmonary edema.

Treatment. Emergency measures should be primarily aimed at removing the preparation from the body and restoring stable hemodynamics.

After oral administration, it is recommended to completely empty the stomach, if necessary, in combination with washing the small intestine.

Since nifedipine is characterized by a high degree of binding to blood plasma proteins and a relatively low volume of distribution, hemodialysis is ineffective, but plasmapheresis is recommended.

Bradycardia can be treated with β-sympathomimetics. If a life-threatening heart rate slows down, an artificial pacemaker is recommended.

Hypotension, which has arisen as a result of cardiogenic shock and vasodilation, can be eliminated with calcium preparations (10–20 ml of 10% solution of calcium chloride or gluconate is injected intravenously slowly, then repeated if necessary). As a result, the level of calcium in the blood plasma may reach the upper limit of normal or be slightly increased. If the administration of calcium is not effective enough, it is advisable to use such sympathomimetics as dopamine or norepinephrine. Doses of these preparations are selected taking into account the achieved therapeutic effect.

The additional administration of fluid should be approached very carefully, as it increases the risk of overloading the heart.

Storage conditions

In a dry, dark place at a temperature not exceeding 25 ° C. after opening the bottle, the preparation is stored for 28 days.