Hydrochlorothiazide + Dihydroergotoxin + Reserpine (Hydrochlorothiazidum + Dihydroergotoxinum + Reserpinum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Sympatholytics

Diuretics

Included in the formulation
АТХ:

C.02.L.A.51   Reserpine and diuretics in combination with other drugs

Pharmacodynamics:

Combined antihypertensive.

Hydrochlorothiazide

The benzothiadiazepine derivative selectively blocks the transport system of sodium, potassium and chlorine ions, stopping their transport through the apical membrane into the cells of the epithelium of the thick segment of the ascending section of the Henle loop. The suppression of reabsorption of ions leads to their removal from the body. Simultaneously with ions of sodium, potassium and chlorine ions of calcium and magnesium are deduced. Hypocalcemia does not develop due to active reabsorption in the distal convoluted tubule of the loop of Henle.

Effective with any fluctuations in acid-base balance, retains a diuretic effect in both acidosis and alkalosis.

Dihydroergotoxin

Stimulates α-receptors, increases tone and increases the frequency of contractions of the uterus, narrows the peripheral vessels. Stimulates the centers of the vagus nerve and the trigger zone of the vomiting center, depresses the vasomotor center. Has a sedative effect. Slightly increases blood pressure.By regulating the exchange of ATP, it improves metabolic processes in neurons of the brain, contributing to an increase in oxygen consumption in the central nervous system.

Reserpine

Sympatholytic. By reducing the amount of norepinephrine in varicose thickenings inhibits the transfer of excitation from the end of postganglionic adrenergic fibers to the effector organs. As a result, the influence of sympathetic innervation on the heart and blood vessels decreases, therefore, the force of the heart contractions decreases, the arterioles expand, and the blood pressure decreases.

Due to the compensatory increase in the number of adrenoreceptors on postsynaptic membranes of effector cells, the effects of adrenomimetics are enhanced.

The hypotensive effect is manifested not earlier than 2-3 weeks after the start of the combination.

Pharmacokinetics:

Hydrochlorothiazide

After oral administration, an empty stomach is absorbed up to 80% in the gastrointestinal tract. The maximum concentration in the blood plasma is reached after 2 hours. The connection with plasma proteins is 40%.

The therapeutic effect develops 2 hours after admission and lasts for 8-12 hours.Penetrates through the blood-brain and placental barrier, excreted in breast milk. Metabolism in the liver.

The elimination half-life is 6.4 hours. Elimination by the kidneys, about 75% in unmodified form.

Dihydroergotoxin

After oral administration, fasted to 60% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is reached after 30 minutes.

Penetrates through the blood-brain and placental barrier, excreted in breast milk. Metabolism in the liver.

The half-life is 32 minutes. Elimination by the kidneys in the form of metabolites (95%).

With repeated administration does not cumulate. The duration of action is 4-6 hours.

Reserpine

After oral administration, an empty stomach is absorbed in the gastrointestinal tract up to 50%. The maximum concentration in the blood plasma is achieved in 1-3 hours. The connection with plasma proteins is 96%.

The therapeutic effect develops 4 days after the beginning of the admission. Penetrates through the blood-brain and placental barrier, is found in breast milk. Metabolism in the liver.

The half-life is 11-12 days. Elimination by the kidneys and with feces.

Indications:

It is used for the treatment of arterial hypertension.

ICD-10

IX.I10-I15.I10   Essential [primary] hypertension

IX.I10-I15.I15   Secondary Hypertension

Contraindications:

Severe renal and hepatic insufficiency, depression, epilepsy, Parkinson's disease, peptic ulcer and duodenal ulcer, pheochromocytoma, ulcerative colitis, reception of monoamine oxidase inhibitors, systemic lupus erythematosus, pregnancy and lactation, age under 18, individual intolerance.

Carefully:

Cardiac deficiency, coronary or cerebral atherosclerosis, hypersensitivity.

Pregnancy and lactation:

Recommendations for FDA - Category C. Contraindicated in pregnancy and lactation.

Dosing and Administration:

Inside, 1 dragee 1-2 times a day.

The highest daily dose: 3 tablets.

The highest single dose: 1 dragee.

Side effects:

Hydrochlorothiazide

Central and peripheral nervous system: headache, dizziness, depression, sleep disorders, paresthesia.

Respiratory system: pneumonitis, pulmonary edema.

Hemopoietic system: thrombocytopenia, agranulocytosis, leukopenia, hemolytic anemia.

The cardiovascular system: orthostatic hypotension, rarely - arrhythmia.

Musculoskeletal system: spasms of the calf muscles.

Dermatological reactions: photosensitization, rash, rarely - toxic epidermal necrolysis.

Sense organs: visual impairment.

Urinary system: glycosuria, hyperuricemia.

Reproductive system: impotence.

Dihydroergotoxin

Central and peripheral nervous system: headache, dizziness, rarely - hallucinations.

The cardiovascular system: increased blood pressure, arrhythmia, spasm of peripheral vessels.

Respiratory system: shortness of breath is possible.

Dermatological manifestations: hyperhidrosis, rash.

Reproductive system: hypogalactia.

Reserpine

Central and peripheral nervous system: dizziness, weakness, nightmares, anxiety, cognitive disorders, stupor, hallucinations, disorientation, rarely - cerebral edema.

Respiratory system: swelling of the nasal mucosa, shortness of breath, rarely - nosebleeds.

Hemopoietic system: anemia, purpura, thrombocytopenia.

The cardiovascular system: sinus bradycardia, arrhythmias, angina pectoris, orthostatic hypotension, syncope, rarely - cerebral circulation disorders.

Digestive system: dry mouth, hypersalivation, nausea, vomiting, peptic ulcer, bulimia, rarely - gastrointestinal bleeding.

Dermatological reactions: itching, eczema.

Sense organs: conjunctival hyperemia, blurred vision, rarely - hearing impairment.

Urinary system: dysuria, rarely glomerulonephritis.

Reproductive system: gynecomastia, galactorrhea, mastodynia, decreased libido.

Allergic reactions.

Overdose:

Confusion, drowsiness, coma, convulsions, miosis, extrapyramidal disorders, respiratory depression, oliguria.

Treatment is symptomatic.

Interaction:

Hydrochlorothiazide

Strengthens the effects of nondepolarizing muscle relaxants.

Patients with diabetes mellitus when using hydrochlorothiazide requires a correction of doses of oral hypoglycemic agents and insulin preparations.

Enhance the hypokalemic effect of glucocorticosteroids, adrenocorticotropic hormone, carbenoxolone, amphotericin, cardiac glycosides.

Anticholinergic drugs increase the bioavailability of hydrochlorothiazide.

With simultaneous use with lithium preparations, a paradoxical antidiuretic effect is possible.

With simultaneous application with vitamin D and calcium preparations may develop hypercalcemia.

With simultaneous use with cyclosporine, the risk of developing gout and hyperuricemia increases.

Dihydroergotoxin

Strengthens the vasoconstrictive effects of sympathomimetics.

With simultaneous application with oxytocin, the development of hypertensive crisis is possible.

Reserpine

When used simultaneously with monoamine oxidase inhibitors, it is possible to develop hypertensive crisis, hyperactivity.

Strengthens the depressing effects on the central nervous system of drugs for general anesthesia, ethanol, tricyclic antidepressants and barbiturates.

With simultaneous use with digitalis preparations, the risk of sinus bradycardia increases.

Strengthens the effects of epinephrine and other sympathomimetic drugs: antitussive drugs, drops in the nose and eye drops.

Special instructions:

Control of the content of electrolytes in blood plasma.

Before surgery, it is necessary to warn the anesthesiologist about the use of reserpine, since the instability of hemodynamics during the anesthesia can be possible.

In the treatment it is not recommended to drive vehicles and work with moving mechanisms.

Instructions
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