Pharmadipine

Farmadipin is used as an emergency treatment in case of hypertensive crisis. In this form, the medicine should not be used for course use.

Indications Pharmadipine

It is recommended to use in case of a sharp increase in blood pressure – to relieve hypertensive crises.

Release form

Available in 5 or 25 ml bottles. One package contains 1 bottle.

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Pharmacodynamics

Farmadipin has pronounced hypotensive and antianginal properties. It prevents Ca ions from entering cardiomyocytes and smooth muscle cells of peripheral and coronary arteries through slow potential-dependent calcium channels of cell membranes. It helps to relax smooth vascular muscles, and also eliminates various spasms, reducing the force of peripheral vascular resistance and blood pressure after exercise, as well as the oxygen demand of the myocardium. In addition, it slightly reduces platelet aggregation and slightly reduces myocardial contractility.

Pharmacokinetics

After oral administration, it is well absorbed from the digestive system. Bioavailability rates are 40-60%. The therapeutic effect is achieved most quickly with sublingual administration - after 5-10 minutes. The peak of effectiveness is reached after 30-40 minutes. The rate of absorption of the drug does not depend on food intake.

The hemodynamic effect lasts for approximately 4-6 hours. About 90% of the nifedipine substance binds to plasma blood proteins. Metabolism occurs in the liver, and the drug is excreted from the body mainly in the form of inactive metabolic products. The overall clearance rate of nifedipine is 0.4-0.6 liters/kg/hour. The half-life of T1/2 is 2-4 hours. This figure may increase approximately 2 times in older people, and in addition, in patients suffering from liver cirrhosis, since they experience a slowdown in the process of nifedipine breakdown. Therefore, in such situations, the dosage should be reduced and the interval between drug administration should be increased.

Nifedipine does not accumulate in the body. A small amount of the drug can pass through the placenta and the blood-brain barrier, and also get into breast milk.

Dosing and administration

In case of a sharp jump in blood pressure, the initial single dosage for an adult will be 3-5 drops (2-3.35 mg), and for an older patient - a maximum of 3 drops (2 mg), while holding the medicine under the tongue or dropping it on a piece of sugar or a cracker, and then holding it in the mouth. If the desired effect is not achieved, the dosage should be increased until there is an improvement in the patient's condition. Then, when the blood pressure level increases, this dosage should be taken as a guideline.

If necessary (if blood pressure rises to 190 over 100/220 over 110 mm Hg), the single dose may sometimes be gradually increased to 10-15 drops (6.7-10 mg), taking into account individual changes in the patient's blood pressure.

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Use Pharmadipine during pregnancy

During pregnancy, the use of the substance nifedipine is prohibited.

Contraindications

Among the contraindications:

• Unstable angina;
• Allergic reaction to the components of the drug;
• State of cardiogenic shock;
• Acute stage of myocardial infarction;
• Severe mitral valve and aortic stenosis;
• Hypotension or tachycardia;
• Lactation period;
• Children under 18 years of age.

Side effects Pharmadipine

If you follow your doctor's recommendations, side effects will be minor and short-lived, and if they occur, there is generally no need to stop using the drug.

Frequent uncontrolled use of the drug may cause the development of side effects that are typical for drugs included in this pharmacological category.

Cardiovascular system: often vasodilation and edema, rarely – hypotension, increased heart rate, tachycardia, and syncope.

CNS and PNS: mainly headache; less common are migraines, anxiety, sleep problems, tremor, vertigo, and dizziness; very rare are agitation, short-term vision problems, and also dysesthesia and paresthesia.

Endocrine system: development of hyperglycemia (this circumstance must be taken into account in patients with diabetes mellitus).

Digestive system: mainly constipation; quite rarely, due to overdosage, dyspepsia, bloating, abdominal pain, vomiting with nausea, a feeling of dry mouth, gingival hyperplasia (in case of prolonged use), as well as a transient increase in the activity of liver enzymes are observed.

Urinary system: occasionally dysuria or polyuria.

Circulatory system: leukopenia, anemia or thrombocytopenia develop quite rarely.

Allergies: sometimes allergic edema/Quincke's edema (including laryngeal edema); quite rarely skin rashes, itching and urticaria; extremely rare – anaphylactic/anaphylactoid shock.

Others: mainly malaise; sometimes nasal congestion or bleeding, as well as erythema; quite rarely – muscle cramps, swelling of the leg or joints, non-specific pain, dyspnea, fever, impotence.

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Overdose

Signs of acute nifedipine poisoning: development of impaired consciousness, which may result in coma, drop in blood pressure, tachycardia or bradycardia, increased blood sugar levels, metabolic acidosis, oxygen starvation, cardiogenic shock, often accompanied by pulmonary edema.

Interactions with other drugs

Nifedipine, when used simultaneously with AT-1 receptor antagonists of nerve endings and other calcium antagonists, diuretics, ACE and PDE5 inhibitors, alpha-adrenergic receptor blockers, alpha-methyldopa, and β-blockers, can increase their antihypertensive properties.

In case of simultaneous use with β-blockers, in addition to increasing the strength of the hypotensive effect, there is sometimes a risk of developing heart failure.

Diltiazem reduces the rate of elimination of nifedipine, so if necessary, the dosage of nifedipine is reduced.

Amiodarone together with quinidine can increase the negative inotropic effect of the active component of the drug. Sometimes, with combined oral administration of nifedipine and quinidine, the saturation of the latter in the blood plasma decreases.

The simultaneous use of nifedipine with theophyllines, and in addition to it, cardiac glycosides, in patients occasionally increases the level of theophylline, as well as digoxin in the blood plasma (which is why their levels must be carefully monitored).

Nifedipine increases the saturation level of blood serum with carbamazepine, as well as phenytoin. The combination of nifedipine with cimetidine can increase the level of the former in blood plasma.

Rifampicin enhances enzyme activity, increasing the rate of breakdown of nifedipine, thereby reducing the strength of the clinical effect of nifedipine (therefore, such a combination is contraindicated).

Treatment with nifedipine should be stopped 36 hours before the planned use of fentanyl. Nifedipine has good compatibility with radiocontrast agents.

As a result of the simultaneous use of the active ingredient Farmadipin with magnesium sulfate administered intravenously, women during pregnancy may experience a disruption of neuromuscular transmission.

Nifedipine is broken down by cytochrome P450 3A4, which is located in the intestinal and liver mucosa. Therefore, drugs that help suppress or enhance this enzyme system can affect the effect of the so-called "first pass" (when taken orally) or the coefficient of purification of nifedipine.

When combined with nifedipine, macrolide antibiotics (for example, erythromycin), substances that inhibit HIV proteases (such as ritonavir), azole antifungals (for example, ketaconazole), fluoxetine, as well as nefazodone and, in addition, cimetidine with quinupristin or dalfopristin, as well as cisapride, an increase in the saturation of the active substance of the drug in the plasma is possible.

Since valproic acid, due to the slowing down of enzyme activity, increases the saturation in plasma of nimodipine, which is similar in structure to nifedipine (it is a calcium channel blocker), an increase in the saturation of the former can also be observed, along with an increase in the effectiveness of the effect.

Also, tacrolimus is broken down by cytochrome P450 3A4. Therefore, in some cases, when taking it together with nifedipine, the dosage should be reduced. Also, during the use, the saturation of tacrolimus in the plasma should be monitored and, if necessary, its dosage should be reduced.

Grapefruit juice slows down the activity of cytochrome P450 3A4, so its use in combination with nifedipine causes an increase in the saturation level of this substance in the plasma, and also prolongs the duration of its effect (because the metabolism process slows down at the time of the first pass or a decrease in the purification coefficient). As a result, the antihypertensive properties of the drug may increase. If you drink grapefruit juice regularly, such an effect can last for 3 days from the moment of the last use. This is why you should avoid drinking juice based on this citrus or grapefruits while treatment with the active component of the drug lasts.

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Storage conditions

It is recommended to store the medicine in a dry place, out of reach of children, away from sunlight. The room temperature should not exceed 25 °C.

Shelf life

Farmadipin is permitted to be used for 3 years from the date of manufacture of the drug.