Emlodin

Emlodin is a selective calcium antagonist that acts on the vascular system.

Indications of the emlodina

It is used for such disorders:

• increase in blood pressure;
• a stable form of angina of a chronic nature;
• variant angina pectoris.

Release form

Release of the drug occurs in tablets, 10 pieces inside the blister plate. The box contains 3 such plates.

Pharmacodynamics

The amlodipine element is a calcium antagonist (dihydropyridine derivative) that blocks the penetration of Ca ions into the myocardium and smooth muscle cells.

The mechanism of the antihypertensive effect of the substance is associated with its immediate relaxing effect on the smooth muscle of the vessels. The mechanism of antianginal influence of drugs has not been fully studied, but it is known that the following factors play an important role in this:

• the expansion of arterioles of a peripheral nature, resulting in a decrease in postload (peripheral resistance). Because the rhythm of the heartbeat remains stable, due to the reduced load on the heart, there is a reduction in energy consumption, as well as the need for myocardium in obtaining oxygen;
• the expansion affecting the main coronary arteries, as well as coronary arterioles (both normal and ischemic), probably also plays an important role in the drug effect of the substance. Due to this expansion, the amount of oxygen produced by the myocardium increases in people with spasms in the arteries of the coronary artery (variant angina).

In people with elevated blood pressure values, a single use of drugs per day leads to a clinically significant decrease in these indicators for a period of 24 hours (the patient may stay in this position for as long as standing or standing). In connection with the slow onset of the manifestation of medicinal effects, a sharp decrease in the level of blood pressure is often not observed.

In persons with angina in the case of the use of a one-time daily portion, the total period of physical activity increases, and in addition, the segment before the onset of an attack of angina and an interval of up to 1 mm of depression of the ST segment. The drug reduces the incidence of angina attacks, as well as the need for nitroglycerin.

Amlodipine does not have any negative effect on metabolism, nor does it cause changes in lipid indices inside the blood plasma. It is allowed to use for people with diabetes, asthma, and in addition to gout.

Pharmacokinetics

Absorption.

When ingested therapeutic portions of drugs, the active element is gradually absorbed into the blood plasma. The bioavailability level of the unchanged molecule is approximately 64-80%. Peak values within the blood plasma are noted after a lapse of 6-12 hours after the use of the drug. The combination of the drug with food does not affect the absorption of amlodipine.

Distribution.

The distribution volume is approximately 21 l / kg, and the pKa value of the active substance is 8.6. In vitro tests demonstrated that the synthesis of the drug with plasma protein is about 97.5%.

Metabolic processes and excretion.

The half-life of the component from the plasma is approximately 35-50 hours. Equilibrium values within the blood plasma drug reaches after 7-8 days of continuous reception. At the same time, amlodipine is mainly metabolized, resulting in the formation of inactive decay products. Approximately 60% of the portion consumed is excreted in the urine, (approximately 10% of them are unmodified amlodipine).

People with eating disorders in the liver.

There is only limited information on the use of drugs in people with problems with hepatic function. In persons with liver failure, the amlodipine clearance rate is lowered, which increases the half-life of the substance and the AUC (approximately 40-60%).

Dosing and administration

Adults.

To reduce the elevated values of blood pressure, as well as the treatment of angina pectoris, a single daily intake of an initial dose of 5 mg is required. Taking into account the patient's response to such treatment, in the future, the daily single dose of the drug can be increased to a maximum of 10 mg.

Persons with angina pectoris may consume the drug in the form of monotherapy or combine it with other antianginal agents in the presence of resistance to nitrates or standard portions of β-blockers.

There are data on the use of drugs, along with diuretics, thiazide type, β- and α-blockers or ACE inhibitors in people with elevated blood pressure. There is no need to select a portion of the medicine in the case of combination with these medications.

Children older than 6 years of age with elevated blood pressure values.

The size of the recommended initial dose of Emlodin for this group of patients is 2.5 mg, with a one-time application per day. In the absence of the desired result (achieving the desired BP values) after the 1st month of therapy, it is allowed to increase the daily dosage to 5 mg. But you need to consider that the use of drugs in a dose of 5 mg in this group of patients not studied.

Persons with disorders of hepatic activity.

The size of portions of medicines for people with disorders in the work of the liver in mild or moderate form are not determined, because of which the dosage should be carefully selected, starting with the lowest portion. Persons with liver problems in severe form should start using drugs with the smallest dosage, then gradually increase it.

To obtain a dosage of 2.5 mg, you should divide the tablet in half by 5 mg.

[1]

Use of the emlodina during pregnancy

There is no data on the safety of amlodipine in pregnant women. During this period, Emlodin can be used exclusively in situations where it is not possible to take an alternative remedy with a safer effect, and the risk associated with pathology is higher than the probability of complications in a woman and fetus.

In animal tests, the use of large doses indicated the development of reproductive toxicity.

There is no information about whether amlodipine is excreted in human milk. Before deciding whether to continue breastfeeding or using the drug, you should evaluate the risk and benefit of taking it for the mother and baby.

Contraindications

The main contraindications:

• the presence of intolerance to dihydropyridines, and in addition to amlodipine and other components of the therapeutic agent;
• extremely low blood pressure;
• shock state (this includes cardiogenic shock);
• obstruction in the area of the outflow tract in the left ventricle (for example, aortic stenosis in severe form);
• heart failure, which is hemodynamically unstable, and developing in connection with acute myocardial infarction.

Side effects of the emlodina

As a result of the use of medication, such negative manifestations as dizziness, tachycardia, sensation of drowsiness, hot flashes, headaches, nausea, severe fatigue, abdominal pains and swelling (including in the region of the shins) often developed.

Taking pills can also cause the following side effects:

• disorders associated with lymph and systemic circulation: leuko- or thrombocytopenia appears sporadically;
• Immune disorders: allergy symptoms are noted;
• problems affecting metabolic processes, as well as alimentary disorders: hyperglycemia develops single-handedly;
• mental disorders: sometimes there may be mood variability (this includes anxiety), depression and insomnia. Occasionally a sensation of confusion is noted;
• disorders affecting the function of the NS: often there are dizziness, drowsiness and headaches (mainly at the beginning of therapy). Sometimes there are syncope, paresthesia, dysgeusia, as well as hypoesthesia. Single polyneuropathy or hypertonus is found;
• visual disorders: they often note problems with visual function (this includes diplopia);
• problems affecting the labyrinth and auditory organs: sometimes there is an ear ring;
• violations of cardiac function: often marked by increased heart rate. Sometimes arrhythmia develops (this includes ventricular tachycardia, bradycardia, and atrial fibrillation). There is a myocardial infarction;
• Disorders of vascular activity: often there are tides. Sometimes there is a decrease in blood pressure. Occurs vasculitis;
• thoracic, respiratory, and mediastinal disorders: dyspnea often appears. Sometimes there is a runny nose or cough;
• problems with the work of the gastrointestinal tract: often there is nausea, abdominal pain, dyspeptic manifestations, and in addition develop disorders of intestinal peristalsis (among them constipation and diarrhea). Sometimes there is dryness of the oral mucosa and vomiting. Gastritis, pancreatitis, and, in addition, gingival hyperplasia develops;
• disorders of hepatobiliary function: jaundice, hepatitis and an increase in the values of liver enzymes (often associated with cholestasis) are noted;
• lesions in the subcutaneous layer and skin surface: sometimes there is purpura, itching, urticaria, rashes, alopecia, hyperhidrosis, and in addition, the shade of the skin changes. Single appears erythema multiforme, edema Quincke, dermatitis exfoliative nature, photosensitivity and Stevens-Johnson syndrome;
• disruption of the function of connective and musculoskeletal tissues: often marked swelling in the region of the shins and muscle cramps. Sometimes there are pain in the back, myalgia or arthralgia;
• lesions affecting the urinary system and the kidneys: sometimes there is nocturia, dysuria, and urination processes become more frequent;
• disorders of the mammary glands and reproductive organs: sometimes there is gynecomastia or impotence;
• systemic disorders: often develop swelling. Also often there is asthenia and a feeling of extreme fatigue. Sometimes there is malaise and pain (in particular, in the sternum);
• test results: sometimes there is an increase or decrease in weight. There was a single reported occurrence of extrapyramidal syndrome.

Overdose

There is only limited information on the intentional drug overdose.

Manifestations of intoxication: based on the available data, it can be assumed that significant intoxication with Emlodin will cause a strong peripheral vasodilation, and possibly the development of reflex type tachycardia. There is information about a significant and probably long-lasting systemic decrease in blood pressure values (this includes a fatal state of shock).

In the treatment of a clinically significant reduction in blood pressure caused by amlodipine poisoning, it is necessary to maintain the CCC function qualitatively-to constantly monitor the work of the respiratory system and the heart, to lift the patient's legs, and to control the volume of the circulating fluid along with the urination processes.

To restore vascular tone and blood pressure, vasoconstrictive agents should be used, making sure beforehand that there are no contraindications to their use. It can also help the introduction of / in the calcium gluconate method - to eliminate the symptoms that have arisen because of the blockade of the channels Ca.

Sometimes a gastric lavage procedure may be required. After receiving a volunteer activated charcoal, during 2 hours after using 10 mg of LS, its absorption was significantly reduced.

Because a significant part of amlodipine is synthesized with protein, the dialysis procedure will be ineffective.

Interactions with other drugs

Drugs that slow down the activity of the element CYP3A4.

Combination of the drug with substances that slow down the CYP3A4 component with moderate or potent effect (protease inhibiting drugs, azole antimycotics and macrolides (eg, erythromycin with clarithromycin, and diltiazem with verapamil)) can cause a significant increase in drug exposure, may increase the likelihood of lowering blood pressure. The medicinal value of such changes can be expressed more clearly in the elderly. Clinical monitoring of the patient's condition and selection of a portion size may be necessary.

It is forbidden to combine the medicine with grapefruits or juice from this fruit, because in some people this increases the indicator of the bioavailability of amlodipine, and therefore its antihypertensive effect is enhanced.

Medications inducing the activity of the element CYP3A4.

The combination of the drug with drugs inducing the CYP3A4 component (such as St. John's wort or rifampicin) can cause a decrease in plasma values of amlodipine, which is why it is necessary to combine such drugs with caution.

Dantrolene infusion.

Ventricular fibrillation followed by death, as well as collapse of the SSS function, were observed in animals (this is associated with hyperkalemia) as a result of the use of dantrolene with verapamil. Due to the high likelihood of hyperkalemia, people with a tendency to develop malignant hyperthermia, as well as in the period of its treatment, should abandon the use of drugs that block the channels of Ca.

The effect of drugs on other medicines.

The antihypertensive effect of amlodipine increases the similar effect of other antihypertensive drugs.

Tacrolimus.

There is a possibility of an increase in tacrolimus values within the blood with its combination with Emlodin, but the pharmacokinetic scheme of this interaction could not be fully established. In order to avoid the development of toxic effects of tacrolimus when combined with amlodipine, one should constantly monitor the indices of the first within the blood and, if necessary, adjust the dose sizes.

Cyclosporine.

Tests on the combination of the drug with cyclosporine have not been previously performed, except for use in people with kidney transplantation, who have a variable increase in the residual values of cyclosporine (mean - 0-40%). People with a kidney transplant using Emlodin should consider the option of tracking the level of cyclosporine and reducing its dose when such a need arises.

Simvastatin.

The combined use of reusable dosages of amlodipine (10 mg) with simvastatin in a dose of 80 mg causes an increase in the exposure of the latter by 77% (compared with the use of one simvastatin). Taking simvastatin with Emlodin should be limited to a dosage of 20 mg per day.

[2], [3]

Storage conditions

Emlodin should be kept in a dark place and closed from children. Temperature - not more than 25 ° C.

[4]

Shelf life

Emlodin can be used for 5 years since the release of the drug.

Application for children

It is forbidden to appoint Emlodin to children younger than 6 years of age, because there is no data on the effect of amlodipine on blood pressure in this age group.

Analogues

The analogues of the drug are Azolex preparations with Amlong, Amlo and Amlodipine-Farmak, Amlodipine-Norton, Amlopril-Darnitsa and Equator, and also Amlodipine-Health, Normodipine and Stamlo.