Methyldopa

When ATH:
C02AB02

Characteristic.

Antihypertensive. White or yellowish-white powder;. Soluble in water.

Pharmacological action.
Gipotenzivnoe.

Application.

Arterial hypertension, mild to moderate.

Contraindications.

Hypersensitivity, hepatitis, cirrhosis of the liver, renal failure, pheochromocytoma, depression, acute myocardial infarction, cerebrovascular diseases, severe coronary artery disease, autoimmunnaya gemoliticheskaya anemia, collagenase, parkinsonizm, porphyria, Simultaneous use of MAO inhibitors, levodopa.

Restrictions apply.

Hepatitis (history), acute left ventricular failure, diencephalic syndrome.

Pregnancy and breast-feeding.

In experiments on rabbits, Mice and rats, dosed up 1000 mg / kg / day (in 16,6 times higher than MRDC), adverse effects were detected. Methyldopa passes through the placenta. There are no adequate and well-controlled studies in women dopegyt actions I and II trimester of pregnancy has not been carried out. In the study of the use of methyldopa in the III trimester of adverse effects were found. Application during pregnancy is possible (on strict conditions).

Category actions on the fetus by the FDA — B. (The study of reproduction in animals revealed no risk of adverse effects on the fetus, and adequate and well-controlled studies in pregnant women have not done.)

Be wary of lactation (Methyldopa passes into breast milk).

Side effects.

From the nervous system and sensory organs: weakness, asthenia, drowsiness, dizziness, headache (occur in the early stages of treatment and usually disappear soon), lethargy, anxiety, parkinsonizm, Bell's paralysis, horeoatetoidnye spontaneous movement, paraesthesia, staggering when walking, deterioration of intelligence, symptoms of cerebrovascular insufficiency, changes in mental status (including nightmares or unusually vivid dreams, depression or anxiety).

Cardio-vascular system and blood (hematopoiesis, hemostasis): bradycardia, orthostatic hypotension, peripheral edema, flushing of the skin of the upper half of the body, increased angina pectoris, worsening symptoms of heart failure; rarely — myocarditis, perikardit, obratimaya leykopeniya and thrombocytopenia, autoimmunnaya gemoliticheskaya anemia, eozinofilija.

From the digestive tract: dry mouth, nausea, vomiting, constipation / diarrhea, glossalgiya, inflammation of the salivary glands, stomatitis, pancreatitis, colitis (severe or prolonged diarrhea or stomach cramps), abnormal liver function with the development of cholestasis, jaundice, hepatitis.

With the genitourinary system: hyperprolactinemia, gynecomastia, galactorrhea, amenorrhea, increase in blood urea nitrogen, decreased libido, impotence.

Allergic reactions: rash, toxic epidermal necrolysis.

Other: arthralgia, myalgia, feverish syndrome, nasal congestion, lupus-like syndrome.

Cooperation.

The antihypertensive effect of reducing agonists and NSAIDs. In a joint application with haloperidol possible adverse effect on activity psihicheckuyu, in particular the occurrence of disorientation and deceleration / difficulty thinking processes. It increases the risk of toxic effects of lithium salts (even while maintaining the concentration of lithium in blood serum at the recommended therapeutic levels).

It should not be used in combination with MAO inhibitors (including furazolidone, procarbazine and selegiline), because, At first, methyldopa may cause hyperexcitability in patients, receiving MAO inhibitors and, Secondly, there are reports of headaches, severe hypertension and hallucinations. The joint appointment with tricyclic antidepressants may reduce antihypertensive effect of methyldopa (Careful monitoring of patients). If concomitant use of levodopa may vary antiparkinson effect of levodopa, and possibly an additive toxic action on the central nervous system, In particular development psychosis. To enhance the hypotensive effect is advisable to use at the same time with hydralazine, diuretics and nifedipine. It is also possible to use verapamil, captopril.

The combination with anxiolytics enhances the hypotensive effect. By increasing the pH of the urine while taking the patient urine alkalizing PM, enhanced action methyldopa, tk. concentration in the blood is maintained at a high level for a longer time, due to increased reabsorption in the renal tubules. When the acidification of urine decreases the action of methyldopa.

Be wary appoint patients, receiving methyldopa, Drugs for general anesthesia (halothane and thiopental sodium); ethyl ester is contraindicated. Patients, receiving methyldopa, during general anesthesia may develop collaptoid state (it is advisable to cease its reception 7-10 days before general anesthesia).

Overdose.

Symptoms: severe hypotension, bradycardia, lethargy, dizziness, tremor, drowsiness, nausea, vomiting, constipation / diarrhea, flatulence, bowel atony.

Treatment: recommended gastric lavage or induction of vomiting, diurez, appointment agonists (norepinephrine, epinephrine). Necessary to monitor the heart rhythm, OCK, electrolyte balance, renal function, and central nervous system.

Dosing and Administration.

Inside. Dose picked individually. The initial dose for adults is 250 mg / day (the first admission-evening, before bedtime), then every 2 day dose 250 mg depending on the severity of the therapeutic effect, The maximum daily dose - 3 g. When reaching the required stable gipotenzivnogo effect dose reduced to a supporting minimum effective on 250 mg every 2 day. For the elderly initial dose is 125 mg 1-2 times a day, The maximum daily dose - 2 g 2 admission.

Precautions.

To prevent the development of withdrawal symptoms it is recommended a gradual reduction of the dose. Patients with impaired renal function is necessary to reduce the single dose.

It is necessary to take into account, that after the discontinuation of antihypertensive effect relatively quickly terminated, the ad occurs usually within 48 no. The therapy required monitoring of liver function and pattern of peripheral blood. When long-term therapy in the first 6-10 weeks of treatment, and then every 6-12 months is recommended Coombs; A positive direct Coombs test and hemolytic anemia requires removal and treatment of glucocorticoids. In the case of fluid retention and edema appearance prescribe diuretics, wherein the dose is reduced. In combination with other antihypertensive agents to reduce the daily dosage recommended.

May mask the rise in temperature in infectious diseases. The drug and its metabolites react with standard chemical agents, used for the determination of catecholamines. Changes of physiological indicators / laboratory tests for uric acid, serum creatinine and some other substances. The urine of patients during treatment while standing gets dark.

At the beginning of the treatment is not allowed to drive a vehicle, and the other classes, potentially dangerous and require attention activities. In the future, the degree of limitation is determined depending on individual tolerance of drugs. During treatment excludes alcohol intake.

Cooperation