Normaten tablets, No. 20

• Arterial hypertension.

Inside, during or immediately after a meal, without chewing, with a small amount of liquid.

The dose is set individually. It is recommended to start treatment with 1 tab. 1 time / day, if necessary (lack of a satisfactory therapeutic effect), you can increase the dose of the drug up to 2 times / day (every 12 hours) 1 tab., And only in exceptional cases - up to 3 times / day (every 8 hours) 1 tab. tab ..

The maximum daily dose is 3 tab.

In connection with the mechanism of action of the drug, the possible lack of effectiveness of the drug can be talked about not earlier than 2 weeks after the start of administration, therefore, during this period, the initial dose should not be increased unnecessarily.

With long-term treatment, in case of a satisfactory therapeutic effect, it is recommended to take 1 tab. 1 time / day, and in some patients the dose of the drug can be reduced to 1 tab. 1 time every other day. With each decrease in the dose of the drug, blood pressure control is necessary.

When carrying out maintenance therapy, the dose should not be exceeded - 2 tablets / day.

Active ingredients:

reserpine - 100 mcg

clopamide - 5 mg

dihydroergocristine mesylate - 580 mcg, which corresponds to the content of dihydroergocristine - 500 mcg

Excipients: lactose monohydrate - 44.9 mg, potato starch - 24.795 mg, povidone - 2.5 mg, talc - 2.5 mg, magnesium stearate - 0.875 mg.

Shell composition: crystalline sucrose - 44.80625 mg, acacia gum - 2.1375 mg, talc - 22.8875 mg, macrogol 6000 - 0.16875 mg.

• hypersensitivity to any component of the drug;

• depression, epilepsy, Parkinson's disease, concomitant electroconvulsive therapy;

• pheochromocytoma, concomitant treatment with monoamine oxidase (MAO) inhibitors;

• peptic ulcer of the stomach and duodenum in the acute phase, erosive gastritis, ulcerative colitis;

• angina pectoris, recent myocardial infarction, chronic heart failure, severe bradycardia, atrioventricular block, intraventricular block;

• severe renal failure (CC below 30 ml / min), nephritis, uremia, nephrosclerosis;

• arterial hypotension, severe cerebral atherosclerosis;

• severe liver dysfunction;

• Addison's disease;

• hypokalemia, hyponatremia, hypochloremia;

• hyperuricemia with clinical manifestations;

• angle-closure glaucoma;

• violation of hematopoiesis;

• pregnancy and lactation;

• bronchial asthma;

• age up to 18 years (efficacy and safety of use have not been established).

With care: diabetes mellitus, gout, old age.

Clinical and pharmacological group: Antihypertensive drug

Pharmaco-therapeutic group: Antihypertensive combined agent (sympatholytic + alpha-blocker + diuretic)

pharmachologic effect

Normatens is a combined antihypertensive drug that contains 3 complementary components.

Reserpine- A sympatholytic, penetrating into the presynaptic endings of postganglionic sympathetic fibers, releases norepinephrine from the vesicles, while simultaneously disrupting its reverse transport and enhancing the process of MAO inactivation. Causes depletion of neurotransmitter reserves and a persistent decrease in blood pressure. It helps to reduce the concentration of dopamine, serotonin and other neurotransmitters in neurons, providing an antipsychotic effect. Weakens the effect of sympathetic innervation on the cardiovascular system, reduces heart rate and OPSS; maintains the activity of the parasympathetic nervous system; deepens and enhances physiological sleep, inhibits interoreceptive reflexes. Increases the peristalsis of the gastrointestinal tract, increases the production of hydrochloric acid in the stomach; slows down metabolic processes in the body; cuts and deepens respiratory movements, causes miosis,hypothermia; reduces the intensity of metabolism. Has a positive effect on lipid and protein metabolism in patients with arterial hypertension and coronary atherosclerosis; increases renal blood flow, enhances glomerular filtration.

Clopamide is a 'loop' sulfanilamide diuretic of medium action that blocks the reabsorption of sodium ions at the level of the cortical segment of Henle's loop, removes sodium, potassium, chlorine and water ions.

Dihydroergocristine is a dihydrogenated ergot alkaloid that blocks alpha-adrenergic receptors, causes vasodilation, reduces total peripheral vascular resistance. The hypotensive effect of the drug is superior to the hypotensive effect of each of the components separately and the action of any combination of the two components; the onset of action is 4-7 days, a persistent hypotensive effect is achieved in 1-4 weeks.

Pharmacokinetics

Suction

The individual components of Normatens are absorbed after oral administration as follows: reserpine by about 30-40%, clopamide - about 90% and dihydroergocristine - less than 25%. Cmax in blood plasma is achieved accordingly: for reserpine - 1-3 hours, for clopamide - about 2 hours, for dihydroergocristine - about 1 hour.

Distribution

The individual components of Normatens are easily distributed in the body (for example, for dihydroergocristine Vd is 52 l / kg). Communication with blood plasma proteins: for reserpine - does not bind, clopamide - about 46%, dihydroergocristine - about 68%. Reserpine and dihydroergocristine penetrate the BBB and through the placental barrier.

Metabolism

Reserpine and dihydroergocristine are extensively metabolized in the liver to inactive metabolites. Clopamide is not significantly metabolized in the liver.

Withdrawal

T1 / 2 Normates is long due to the presence of reserpine, for which T1 / 2 is 4.5 hours in the first phase, and about 271 hours in the second. feces, clopamide, mainly by the kidneys.

Indications

• arterial hypertension.

Dosage regimen

Inside, during or immediately after a meal, without chewing, with a small amount of liquid.

The dose is set individually. It is recommended to start treatment with 1 tab. 1 time / day, if necessary (lack of a satisfactory therapeutic effect), you can increase the dose of the drug up to 2 times / day (every 12 hours) 1 tab., And only in exceptional cases - up to 3 times / day (every 8 hours) 1 tab. tab ..

The maximum daily dose is 3 tab.

In connection with the mechanism of action of the drug, the possible lack of effectiveness of the drug can be talked about not earlier than 2 weeks after the start of administration, therefore, during this period, the initial dose should not be increased unnecessarily.

With long-term treatment, in case of a satisfactory therapeutic effect, it is recommended to take 1 tab. 1 time / day, and in some patients the dose of the drug can be reduced to 1 tab. 1 time every other day. With each decrease in the dose of the drug, blood pressure control is necessary.

When carrying out maintenance therapy, the dose should not be exceeded - 2 tablets / day.

Side effect

From the digestive system: diarrhea, dry mouth, abdominal pain, nausea, vomiting, exacerbation of peptic ulcer disease, decreased appetite. Rarely - ulceration of the mucous membrane of the stomach and duodenum, gastrointestinal bleeding when using reserpine at a dose higher than 1 mg / day (the amount contained in 10 tablets. Normates).

From the side of the cardiovascular system: bradycardia, lowering blood pressure, cerebrovascular disorders, orthostatic hypotension.

From the side of the central nervous system: headache, dizziness, drowsiness, weakness, anxiety, impaired concentration, insomnia, extrapyramidal disorders (tremor, stupor, Parkinson's syndrome);
Since the drug contains reserpine, one should remember about the possibility of depressive reactions (including suicidal tendencies) and depressive syndrome; such symptoms appear rarely and only in cases of using large doses of reserpine (more than 1 mg / day, which corresponds to the content of reserpine in more than 10 tablets. Normates).

From the respiratory system: hyperemia and edema of the nasal mucosa. Reserpine can cause symptoms of bronchospasm, but this effect is rare, and, as a rule, in patients with bronchial asthma or broncho-obstructive syndrome.

Allergic reactions: skin rash, itching.

From the side of hematopoiesis: thrombocytopenia with symptoms of hemorrhagic diathesis.

Laboratory indicators: hypokalemia, hypomagnesemia, hypocalcemia, metabolic alkalosis, hyperuricemia, hyperglycemia, a slight increase in the content of triglycerides, cholesterol.

Others: galactorrhea.

With long-term use in high doses - paresthesias, decreased libido, decreased potency, gynecomastia, urination disorder, accommodation spasm, conjunctival hyperemia, hypothermia.

Contraindications for use

• hypersensitivity to any component of the drug;

• depression, epilepsy, Parkinson's disease, concomitant electroconvulsive therapy;

• pheochromocytoma, concomitant treatment with monoamine oxidase (MAO) inhibitors;

• peptic ulcer of the stomach and duodenum in the acute phase, erosive gastritis, ulcerative colitis;

• angina pectoris, recent myocardial infarction, chronic heart failure, severe bradycardia, atrioventricular block, intraventricular block;

• severe renal failure (CC below 30 ml / min), nephritis, uremia, nephrosclerosis;

• arterial hypotension, severe cerebral atherosclerosis;

• severe liver dysfunction;

• Addison's disease;

• hypokalemia, hyponatremia, hypochloremia;

• hyperuricemia with clinical manifestations;

• angle-closure glaucoma;

• violation of hematopoiesis;

• pregnancy and lactation;

• bronchial asthma;

• age up to 18 years (efficacy and safety of use have not been established).

With care: diabetes mellitus, gout, old age.

Application during pregnancy and lactation

Since reserpine has a teratogenic effect, it is not recommended to use Normatens during pregnancy.

In addition, reserpine can cause arterial hypotension and bradycardia, which are dangerous for the fetus. In newborns, reserpine can contribute to rhinorrhea and swelling of the nasal mucosa, leading to difficulty breathing and cyanosis.

Clopamide can cause thrombocytopenia in the fetus.

The drug should not be used during lactation. This is mainly due to the penetration of reserpine and dihydroergocristine into milk.

Dihydroergocristine may cause ergot-like symptoms in newborns and may inhibit / weaken lactation in the mother.

Application for violations of liver function

The drug is contraindicated in severe liver dysfunction.

Application for impaired renal function

The drug is contraindicated in severe renal failure.

Application in children

The efficacy and safety of use in children under the age of 18 have not been established.

Use in elderly patients

Use with caution in elderly patients.

special instructions

Since the Normates effect develops relatively slowly, the dosage should not be increased more often than once a week, due to the possibility of a pronounced decrease in blood pressure; special care must be taken in the case of joint use with other antihypertensive drugs; during treatment, periodically monitor the level of blood pressure to determine the optimal dosage regimen.

During the period of treatment, the level of glucose and uric acid in the blood serum may increase, it is recommended to periodically monitor these parameters, especially in patients with impaired glucose tolerance and hyperuricemia.

Monitoring of renal function is necessary, especially in patients with chronic renal failure.

In the event of bradycardia during the treatment period, the dose of the drug must be reduced or the drug withdrawn.

During treatment, it is necessary to control serum potassium. In most patients, additional prescription of potassium supplements is not required, provided that the diet contains a sufficient amount of foods rich in potassium (fruits, vegetables, fish, low-fat cheese, etc.).

Caution should be exercised in patients with bronchial asthma and bronchospasm; in case of exacerbation, it is necessary to stop taking Normatens.

At least 2 weeks before the planned surgical intervention, you should stop taking the drug and replace it with another antihypertensive agent.

Alcohol should not be consumed during treatment.

The dose of Normatens should be modified accordingly in the case of the simultaneous use of other drugs interacting with it.

7 days before the start of electroconvulsive therapy, Normatens should be canceled.

Influence on the ability to drive vehicles and work with mechanisms

Normatens can interfere with the patient's ability to respond quickly, especially at the beginning of treatment. During the period of treatment, one should not drive vehicles and engage in any activities that require increased concentration of attention and speed of psychomotor reactions.

Overdose

Symptoms: nausea, vomiting, diarrhea, muscle weakness, dizziness, headache, marked decrease in blood pressure, bradycardia, arrhythmias, depression, hyporeflexia, confusion and coma.

Treatment: as first aid, if the patient is conscious, induce vomiting, gastric lavage or give activated charcoal. Conducting symptomatic therapy aimed at maintaining the function of the cardiovascular system, correcting electrolyte balance.

Reserpine, which is part of Normates, is not excreted from the body using dialysis.

Drug interactions

Reduces the effectiveness of oral hypoglycemic drugs, tricyclic antidepressants, anticoagulants.

Increases the concentration of lithium in the blood plasma (slowing down its excretion).

Weakens the action of antiepileptic drugs and levodopa, anticholinergics, reduces the analgesic effect of morphine.

Enhances the action of barbiturates, ethanol, drugs for inhalation anesthesia, antihistamines.

Enhances the action of adrenergic agonists.

Barbiturates, ethanol, beta-blockers, peripheral vasodilators enhance the hypotensive effect.

Glucocorticosteroids, non-steroidal anti-inflammatory drugs, laxative drugs reduce diuretic, hypotensive effects, increase the risk of hypokalemia.

Against the background of treatment with MAO inhibitors - an increase in the inhibitory effect on the central nervous system.

During treatment with the drug, MAO inhibitors cause moderate or severe arterial hypertension, hyperreflexia.

јнтиаритмические средства Ц в случае гипокалиемии, котора¤ может сопутствовать лечению, повышаетс¤ риск токсического действи¤ амиодарона, дизопирамида, хинидина; гипокалиеми¤ ослабл¤ет эффект лидокаина, мексилетина.

Ќе рекомендуетс¤ сочетание с допамином (усиление вазоконстрикторной реакции).

ѕри совместном применении с дигоксином Ц повышаетс¤ риск брадикардии; в случае гипокалиемии, котора¤ может сопутствовать лечению, повышен риск усилени¤ побочных реакций дигоксина.

”слови¤ хранени¤

’ранить в сухом, защищенном от света месте, при температуре от 15? до 25?—. ’ранить в недоступном дл¤ детей месте.

—рок годности

—рок годности 5 лет. Ќе использовать после истечени¤ срока годности, указанного на упаковке.

”слови¤ реализации

ѕрепарат отпускаетс¤ по рецепту.