Pharmacological properties
The preparation acting on the central mechanisms of regulation of blood pressure. penetrates the blood-brain barrier; metabolized with the formation of alpha-methylnorepinephrine, which stimulates postsynaptic α-adrenergic receptors of brain stem neurons in the central nervous system, which leads to inhibition of the vasomotor center. the hypotensive effect with prolonged use of the preparation is mainly associated with a decrease in the ovarian pressure, the minute volume of blood does not change. increases the rate of glomerular filtration and renal blood circulation, reduces the level of renin in the blood plasma. also causes a moderate decrease in cardiac output and heart rate. the effect of the preparation is manifested 2 hours after application and lasts 24–48 hours.
After oral administration, about 50% of the preparation is absorbed into the gastrointestinal tract. Protein binding - up to 20%. Up to 10% of the dose taken is metabolized to form alpha-methyldopa and alpha-methylnorepinephrine. It is excreted mainly by the kidneys. About 70% of the absorbed preparation is excreted in the urine in the form of methyldopa and its sulfoconjugates.
With prolonged use, the preparation can accumulate in the body. The half-life is no more than 8 hours; with renal failure, it increases. After oral administration, complete elimination of the preparation occurs after 36 hours. It is removed during hemodialysis, peritoneal dialysis.
Indications
Mild to moderate ar, ar in pregnant women.
Application
The dose is set individually. as a rule, the initial dose of methyldopa for adults is 250 mg (1 tablet) 2-3 times a day for the first 2 days.
Then the daily dose is increased by 250 mg (1 tablet) sequentially every 2 days until an adequate level of blood pressure reduction is achieved. If necessary, increase the dose to 1–1.5 g / day. The maximum daily dose for adults is 3 g (12 tablets).
Children, if necessary, are prescribed Dopegit, starting with a dose of 10 mg / kg of body weight (in 2-4 doses), then the dose is selected individually, depending on the effect obtained. The maximum daily dose for children is 65 mg / kg of body weight.
Contraindications
Dopegit tablets should not be used in the case of:
• allergies to any component of the preparation;
• active form of hepatitis and / or liver failure, liver cirrhosis;
• autoimmune hemolytic anemia;
• pheochromocytomas;
• hyperprolactinemia;
• porphyrias;
• depression.
Side effects
From the side of the cardiovascular system: peripheral edema, orthostatic hypotension, bradycardia.
From the side of the central nervous system: headache, dizziness, weakness, drowsiness, rarely - Parkinson's syndrome, hallucinations.
From the gastrointestinal tract: nausea, vomiting, dry mouth, diarrhea, constipation, pancreatitis, liver dysfunction, jaundice, colitis.
From the hematopoietic system: rarely - leukopenia and thrombocytopenia, autoimmune hemolytic anemia.
From the endocrine system: gynecomastia, galactorrhea, decreased libido, impotence.
Allergic reactions: exanthema.
Rarely - fever, myalgia, arthralgia, lupus syndrome.
Special instructions
The preparation should be used with extreme caution in patients with impaired cerebral circulation; a history of depression; Parkinson's disease (possibly exacerbation).
In case of kidney disease, before using Dopegit, an examination should be carried out in order to determine the presence of renal failure.
During the first 1-3 months of treatment, it is recommended to periodically monitor the hemogram, the level of hepatic transaminases in the blood serum.
After the first 6–10 weeks of treatment, it is necessary to exclude the possibility of autoimmune hemolytic anemia (Coombs' test), which, with long-term treatment, must be repeated every 6 months – 1 year.
With methyldopa treatment, a positive catecholamine test may appear, indicating the possibility of pheochromocytoma development.
Dopegit administration at a dose of ≥750 mg / day can also lead to a positive porphobilinogen test. Due to the effect of the preparation on the water balance, peripheral edema may appear, which sometimes requires the appointment of diuretics. Since edema is the most common side effect when using the preparation Dopegit, during the period of treatment it is necessary to ensure control of the patient's body weight, drinking and dietary regimen.
With general anesthesia, the narcotic effect may increase.
During pregnancy, women taking Dopegit do not have to stop taking it. The use of Dopegit in this case should be carefully weighed taking into account the ratio of benefits to the mother with the potential risk to the child.
Methyldopa passes into breast milk, therefore, when Dopegit is prescribed, the patient must stop breastfeeding.
During the period of treatment, you should avoid drinking alcoholic beverages.
It is necessary to refrain from potentially hazardous activities that require concentration of attention, including driving.
Interactions
Caution should be exercised when taking dopegit in combination with any of the following preparations:
• levodopa, levadopa / cardidopa - it is possible to increase the antihypertensive effect;
• preparations belonging to the group of MAO inhibitors (for example, phenelzine, transcypromine) - it is possible to increase hypotension or hypertension with psychomotor agitation;
• preparations for the treatment of patients with depression (for example, tricyclic antidepressants) - a decrease in the antihypertensive effect, the appearance of tachycardia, agitation, headache;
• diuretics, apressin, calcium antagonists, ACE inhibitors, β-adrenergic receptor blockers, α-adrenergic receptor blockers or other antihypertensive preparations, as well as anesthetics enhance the effect of Dopegit;
• digoxin - bradycardia, asystole may appear;
• iron preparations weaken the effect of Dopegit;
• indomethacin and other NSAIDs reduce the antihypertensive effect of Dopegit;
• lithium - an increase in the toxicity of lithium is possible;
• alcohol and preparations that cause depression of the central nervous system, increase the depressive effect;
• anticoagulants derivatives of coumarin, indadione increase the anticoagulant effect;
• anorexigenic preparations weaken the effect of Dopegit;
• sympathomimetics dopamine, mezaton enhance the effect of Dopegita.
The combination of Dopegit with tranquilizers causes an increase in the antihypertensive effect. With urine alkylization, the concentration of Dopegit in the blood increases, with acidolization, the effect decreases.
The use of Dopegita in combination with any of these preparations can change their effect on the body or be dangerous to the body.
Overdose
Symptoms: severe arterial hypotension, tremor, bradycardia, stomach atony, vomiting, mental retardation.
Treatment: gastric lavage (if the preparation was recently taken); if detoxification is carried out with a significant delay, the use of hemodialysis is more effective than the method of forced diuresis. According to indications, plasma-substituting solutions, adrenergic agonists (for example, epinephrine) are prescribed. In case of an overdose of Dopegita tablets, you should immediately consult a doctor at the nearest emergency room or hospital.
Storage conditions
At a temperature of 15-25 ° C.