Primary hypertension and all forms of secondary hypertension in which monotherapy is ineffective. It can be used at the same time as other medicines used to treat high blood pressure, such as beta-blockers, vasodilators.
Composition:
1 tabl it contains 5 mg of clopamide, 0.5 mg of dihydroergocristine (as mesilate) and 0.1 mg of reserpine. The product contains sucrose and lactose.
Action:
The preparation combines the action of 3 substances that lower blood pressure: reserpine, clopamide and dihydroergocristine. Reserpine has neuroleptic and hypotensive effects. It causes leaching of neurotransmitters from granule bubbles of adrenergic presynaptic structures. It also prevents the uptake and storage of catecholamines and serotonin in the central and peripheral nervous system. As a result, it reduces the content of catecholamines in the nervous system and peripheral tissues. Reserpine causes reflexive tonsillness. As a result of its action, blood vessels dilate, slow heart rate and long-term blood pressure drops. Klopamid exhibits moderate diuretic effect on average. It inhibits the reabsorption of sodium ions in the cortex of the ascending arm of the Henle's loop and in the ileal coils, which results in increased diuresis and natriuresis and a decrease in blood pressure. Inhibition of reabsorption of sodium ions results in increased calorie and may lead to hypokalemia. Dihydroergocristin belongs to the group of hydrogenated ergot alkaloids. It acts agonistically against dopaminergic and serotoninergic receptors as well as antagonists to α-adrenergic receptors. It reduces the tension of the smooth muscle of blood vessels, reducing the blood pressure. In addition, it inhibits reflexes from the baroreceptors and reduces reactive tachycardia. After oral administration, the individual components of the preparation are absorbed from the gastrointestinal tract in the following amounts: reserpine in approximately 40%, clopamide in more than 90%, dihydroergocristine in approximately 25%. They reach their maximum concentration in blood: 1-3 h, 1-2 h and 0.6 h after oral administration. Reserpine does not bind to plasma proteins, whereas clopamide and dihydroergocristine bind to 46% and 68% respectively. Rezerpine and dihydroergocristine pass through the blood-brain barrier and through the placental barrier. All components of the preparation are metabolised in the liver to inactive metabolites. Reserpine is mainly excreted as metabolites, faeces and urine; T0,5 is about 4.5 h in the alpha phase and about 271 h in the beta phase. Dihydroergocristine is mainly excreted in the faeces; T0,5 is about 2 hours in the alpha phase and about 14 hours in the beta phase. Clopamide is mainly excreted in the urine; T0,5 is about 6 hours.
Contraindications:
Hypersensitivity to sulphonamides, reserpine, ergot alkaloids or other ingredients of the preparation. Hypokalemia. Pregnancy and breastfeeding.
Precautions:
Do not use in children or in patients with severe hepatic and renal impairment (creatinine clearance <30 ml / min). Particularly cautiously used in patients with renal insufficiency, with gout, in the elderly. In patients with diabetes or Glucose metabolism disorders, glycaemia should be periodically monitored and the dose of the antidiabetic medication adjusted as necessary. Due to the content of sucrose and lactose, the preparation should not be used in patients with fructose intolerance, galactose intolerance, sucrase-isomaltase deficiency, Lapp lactase deficiency, malabsorption of glucose-galactose.
Pregnancy and lactation:
The preparation is contraindicated in pregnancy and breast-feeding.
Side effects:
The following may occur: nausea, vomiting, hypokalaemia, orthostatic hypotension, myasthenia gravis, rhinitis, increased glucose and uric acid in the blood, weakness, thrombocytopenia, depression.
Dosage:
Orally. Adults: initially 1 tabl. coated daily. Depending on the effectiveness of treatment and the possible presence and severity of side effects, this dose can be increased to a maximum of 3 tablets.daily administered in 3 divided doses. However, it should be remembered that due to the mechanism of action and pharmacological properties of individual active substances, the possible lack of efficacy of treatment can be said no sooner than after about 14 days from the beginning of treatment and therefore it is not necessary to increase the dose during this period. The expected effect of the drug occurs after 1-4 weeks of use. The dose should be increased gradually. The supporting effective dose is usually 1 tabl. once a day. Some patients can use 1 tablet. every other day. Sometimes, however, it is necessary to use 2 tables. daily in divided doses, and in exceptional cases 3 tables. daily in divided doses. The tablets should be taken with or immediately after a meal.