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Adelphane
Adelfan is a combined remedy that helps lower blood pressure (arterial pressure). The active components of the drug are reserpine, as well as dihydralazine.
Pharmacodynamics
Reserpine exerts a neurotropic vasodilating effect on the body. Adelphan lowers blood pressure and improves sleep. As a result of using the drug in neurons, the saturation with neurotransmitters decreases, which causes its antipsychotic effect.
Tablets improve the peristalsis of the gastrointestinal tract, increase the glomerular reaction, and increase the volume of blood flow in the liver. In addition, the drug reduces the metabolic rate, causes miosis and hypothermia. It also promotes deepening of respiratory movements. The constant effect from the use of Adelphan begins to appear after 2-3 weeks. Since the start of therapy.
Under the influence of dihydralazine, the tone of the smooth myocytes of the arterioles decreases, the blood flow increases, and the resistance force in the vessels of organs such as the kidneys, the brain, and also the skin and heart is reduced.
Pharmacokinetics
After oral administration of reserpine is soon absorbed, the systemic bioavailability is 50%. The relative average Vd of the reserpine is 9.1 l / kg (with fluctuations in the range of 6.4-11.8 l / kg). With blood plasma proteins bind more than 96% (with albumins and lipoproteins). The active substance in the liver is metabolized, and also in the intestine. The main products of metabolism are trimethoxybenzoic acid together with methyl reserpate. It is excreted from the blood plasma together with metabolites in 2 stages: the half-life in the α-phase is 4.5 hours, and in the β-phase - 271 hours. The average half-life of the unchanged component is 33 hours. The overall cleansing ratio of reserpine has an average value of 245 ml / minute. In the first 96 hours after oral administration, 8% of the dose taken by the patient is excreted through the kidneys (mainly as metabolites), and 62% by the intestine (often under the guise of unchanged substance).
After internal reception, dihydralazine is soon absorbed, mainly remaining in the blood plasma unchanged. In the process of metabolism of this component, hydrazone substances are also formed. About 10% of dihydralazine resides in the blood plasma under the guise of hydralazine. Metabolization of the substance is mainly carried out by oxidation (hydrazones are formed at the same time), as well as acetylation. In this case, the half-life of the unchanged basic component takes on average 4 hours. The average total purification rate is 1450 ml / minute. In the first 24 hours after ingestion, approximately 46% of the dose used is excreted from the body (predominantly the intestine), mainly in the form of metabolites. Approximately 0.5% of the dose of the drug in unchanged form leaves with urine.
Contraindications
Among the contraindications to Adelphan's admission:
- The state of depression;
- Parkinson's disease;
- Postponed in the recent past myocardial infarction;
- Epilepsy;
- An aggravated ulcer;
- Arrhythmia or angina in severe form;
- Bright tachycardia;
- Problems with liver function;
- Severe form of renal insufficiency;
- Hypersensitivity to the components of the drug - reserpine or dihydralazine;
- Breastfeeding period;
- The age is under 18 years.
Side effects of the adelfana
Among the side effects of taking medication are the following disorders:
Redness of the eyes, rash on the skin, impaired motor function of the digestive process, development of bradycardia, dizziness, a feeling of general weakness, as well as shortness of breath. In some cases, there may be a depressive state, a sense of anxiety, insomnia, as well as manifestations of parkinsonism (a disorder of motor coordination with the appearance of trembling, and a decrease in the volume of movements).
Dosing and administration
Adelfan at the first stage of treatment is prescribed in a dosage of 1 table. Three times a day after eating. If there is such a need, the dosage can be increased to 2 tables. Three times a day. After the therapeutic effect is achieved, the daily dosage of the medicine is gradually reduced.
Interactions with other drugs
Other drugs that lower blood pressure, increase the hypotensive effect of Adelphane. The combination of reserpine with cardiac glycosides lowers the heart rate, thereby increasing the risk of arrhythmia. Reduces the effectiveness of antiparkinsonian drugs, as well as morphine and holinoblokatorov. When combined with methyldopa, the likelihood of developing a depressive state increases. Increases the central effect of hypnotics, drugs used as inhalation anesthetics, barbiturates, antihistamines, medications containing ethanol, as well as tricyclics. In the case of combined administration with MAO inhibitors, there is an increase in blood pressure and development of hyperreactivity.
Tricyclics, antipsychotics, drugs containing ethanol, and diazoxide in combination with Adelphan increase the hypotensive effect of hydralazine sulphate.