Agen 10

The drug Agen 10 is a cardiovascular drug – calcium ion antagonist. It is capable of blocking calcium channels, primarily affecting the vascular wall.

Indications Agena 10.

The drug is used in the treatment of the following diseases and conditions:

• arterial pressure increase of the second and third stages;
• various courses of ischemic heart disease (for example, stable angina, vasospastic angina);
• chronic course of heart failure in the decompensation stage.

Release form

The drug Agen 10 is produced in a tablet dosage form of a light, almost white shade. The tablet is elongated, has a dividing notch on one side, the letter A (according to the first letter of the drug name) and the number 10 (indicates the dosage of the active component). The active substance of the drug is amlodipine, which is presented as amlodipine besylate. Additional substances include MCC, dicalcium phosphate, sodium starch glycolate, magnesium stearate.

Pharmacodynamics

A medicinal antianginal and hypotensive agent, a synthetic derivative of dihydropyrine, representing a group of calcium channel blockers of the second generation. Reduces signs of myocardial ischemia, increasing the lumen in the coronary arteries and distal arterioles, thereby reducing myocardial oxygen consumption, smoothing out cardiac preload. Under the influence of the drug, the intensity of pain attacks in heart failure decreases, the need for nitroglycerin is reduced.

The drug gently expands the lumen of blood vessels, which also helps to reduce blood pressure. The drug, taken once, ensures stabilization of blood pressure during the day. In case of coronary heart disease, the drug exhibits anti-sclerotic and cardioprotective effects, and also reduces hypertrophic signs in the tissue of the left ventricular myocardium, which occur with constantly elevated blood pressure. During severe chronic heart failure, it reduces the likelihood of cardiac arrest.

Agen 10 does not affect cardiac conductivity or contractility of the cardiac muscle, but it can normalize heart rate, reduce platelet aggregation, and reduce the risk of thrombus formation. The drug increases glomerular renal filtration and removes excess sodium from the bloodstream.

Agen 10 does not affect metabolic processes in the body.

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Pharmacokinetics

When taken orally, the drug is well absorbed, with the maximum amount of the active component in the serum being detected within 6-12 hours after administration of the drug.

The drug becomes 64-80% bioavailable.

The distribution percentage may be approximately 21 l/kg. The amount of food consumed and its presence in the stomach do not affect the degree of absorption of the drug.

Scientific research has shown that on average 97% of the distributed active substance binds to plasma proteins.

The half-life of the drug can be from 35 to 50 hours. Stability in the amount of the substance in the blood serum is achieved on the 7-8th day of continuous use of the drug.

Biotransformation of the active component occurs in the liver, where conversion into an inactive form of metabolites is observed.

The active component of the drug is removed from the body through urine: up to 10% of the total amount is in unchanged form, up to 60% are inactive metabolites.

The active component of the drug is not susceptible to hemodialysis.

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Dosing and administration

Agen 10 should be taken orally, half a tablet (5 mg) per day at a time. Over the course of 1-2 weeks, the dosage of the medication is gradually increased to one tablet (10 mg) once a day.

For long-term treatment of hypertension, a maintenance dosage of no more than ¼-½ tablet daily is prescribed.

Angina pectoris requires the administration of ½ or a whole tablet daily at one time.

For patients with short stature and underweight, elderly people, patients with liver pathology and chronic coronary heart disease, the drug is prescribed in a dosage of ¼ tablet daily, if necessary, gradually increasing the dose to ½ and a whole tablet per day.

The tablet is taken without chewing, regardless of food intake, with water, tea or juice.

Completion of the course of therapy is carried out by gradually reducing the dosage in order to prevent the formation of withdrawal syndrome. It is not recommended to abruptly stop using the drug.

You should not take the drug on your own without consulting a specialist.

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Use Agena 10. during pregnancy

Since there is no scientifically proven data on the use of this drug during pregnancy and lactation, the use of Agen 10 during these periods is not recommended. The decision to prescribe the drug to pregnant and lactating women can be made by a specialist on an individual basis, based on an assessment of possible risks and the benefits received from treatment.

Contraindications

The use of the drug is not recommended in case of hypersensitivity to the components of the drug or to other drugs of the dihydropyridine group.

Agen 10 is not prescribed for low blood pressure, during pregnancy and breastfeeding.

The drug should be used with caution in cases of acquired heart defects (mitral and aortic stenosis), progressive chronic heart failure, in the acute phase of myocardial infarction, and in elderly patients.

The drug is not recommended for use in combination with any other medications without the approval of the attending physician.

During treatment with the drug Agen 10, the patient's weight should be monitored, as this drug can provoke the development of obesity. It is also necessary to monitor the condition of the gums by regularly visiting the dentist.

The drug is used only by adult patients, as its use in children has not been studied.

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Side effects Agena 10.

When using Agen 10, some side effects may occur:

• insomnia or drowsiness, irritability, tearfulness, depression or anxiety;
• increased fatigue, headaches, tendency to sudden mood swings;
• convulsions, disturbances of consciousness, disturbances of sensitivity in the extremities, tremors in the hands, asthenia;
• pain in the stomach, nausea, thirst, changes in body weight, bowel disorders, inflammatory diseases of the digestive system;
• rapid or slow heartbeat, swelling of the lower body, extrasystoles, chest pain, persistent low blood pressure, migraine;
• frequent and painful urination, impaired sexual function and libido;
• pain in muscles, joints, bones;
• dermatitis, baldness, allergic reactions, itchy dermatosis;
• deterioration of visual functions, conjunctivitis, double vision and pain in the eyes, lacrimation disorders;
• tinnitus, nosebleeds, hyperhidrosis;
• male-type gynecomastia, back pain, obesity;
• feeling of heat, redness of the face.

Rarely, coordination disorders, memory impairment, and signs of agitation (motor restlessness) may be observed.

A blood test may show bilirubinemia, high activity of blood enzymes.

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Overdose

Signs of an overdose of Agen 10 include the development of increased heart rate, decreased blood pressure due to excessive relaxation and dilation of blood vessels.

If signs of overdose are detected, gastric lavage should be performed, a suspension of sorbent agents (sorbex, activated carbon) should be taken. If necessary, injections of drugs to support the heart and blood vessels can be administered, and symptomatic therapy measures can be taken. Measures in case of overdose should include mandatory monitoring of diuresis and circulating blood volume, assessment of the state of the pulmonary system and heart.

To slow down the effects of a large amount of the drug on the body, calcium gluconate can be administered by intravenous injection.

Interactions with other drugs

The following medications may interfere with the drug's action to lower blood pressure:

• nonsteroidal anti-inflammatory drugs (aspirin, ibuprofen, diclofenac);
• hormonal drugs-estrogens (due to sodium ion retention);
• sympathomimetic agents (adrenaline, ephedrine, salbutamol);
• α-adrenergic agonists (norepinephrine, phenylephrine, metaraminol, mephentermine, methoxamine).

Drugs that inhibit microsomal oxidation (ketoconazole, erythromycin, cyclosporine) increase the concentration of Agen 10 in the blood serum, which may result in increased side effects of the drug. At the same time, drugs that induce liver microsomal enzymes (rifampicin, phenobarbital, phenytoin) are able to reduce the amount of Agen 10 in the blood.

Diuretics (hydrochlorothiazide, indapamide, furosemide, spironolactone), β-blockers (timolol, metoprolol, labetalol), ACE inhibitors (captopril, enalapril, fosinopril) enhance the hypotensive and antianginal effects of Agen 10. The hypotensive effect is also enhanced by α-blockers (tropafen, prazosin), amiodarone, quinidine, neuroleptics (chlorpromazine, haloperidol, zeldox).

The drug does not affect the action of digitoxin and warfarin.

The use of the drug together with medications containing lithium (lithium carbonate, oxybutyrate, lithium nicotinate) can lead to the appearance of signs of neurotoxicosis, which is characterized by the development of dyspeptic phenomena and coordination disorders.

Concomitant use of quinidine and procainamide with Agen 10 may result in prolongation of the QT interval on ECG.

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Storage conditions

The medicine Agen 10 is usually stored in the original packaging at a temperature of up to 24°C, in dry and dark conditions. Keep the medicine out of the reach of children.

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Shelf life

The shelf life of Agen 10 is up to 3 years. Any unused expired drug must be discarded.