Strepsils express tab d rassas 24. Strepsils Express instructions for use

Reserpine is an antihypertensive and antipsychotic drug.

Release form

The drug is available in tablets in dosages of 0.1 and 0.25 mg.


Analogues of Reserpine are drugs that contain the same active substance: Adelfan-Ezidrex, Alserin, Relsidrex-G, Trirezide-K, Rausedil, Rausedan, Cristoserpine, Rau-Sed, Serfin, Serpasil, Tenserpine, Hypnoserpine, etc. Reserpine is also included in some antihypertensive drugs, for example Cristepine.

pharmachologic effect

The active ingredient of the drug is reserpine, one of the alkaloids of the Rauwolfia serpentine plant.(Rauvolfia serpentina). Reserpine is a sympatholytic, i.e. has a predominant effect on the sympathetic nervous system, inhibiting it, and activating the parasympathetic as compensation. Causes a persistent decrease blood pressure, largely due to the inactivation of MAO. The antipsychotic effect of Reserpine is based on a decrease in the concentration of neurotransmitters (serotonin, dopamine, etc.) in neurons. Reduces heart rate, reduces overall peripheral resistance blood vessels, promotes deepening of physiological sleep, potentiates the effect of sleeping pills and painkillers. The use of Reserpine causes a slowdown in metabolism in people suffering from hypertension and coronary atherosclerosis, normalizes protein-fat metabolism. Under the influence of the drug, breathing becomes deeper and at the same time more rare, the pupil constricts (miosis), and body temperature decreases.

Reserpine activates the production of hydrochloric acid in the stomach and enhances intestinal motility, enhances renal blood circulation, increases glomerular filtration in the kidneys.

This drug has a cumulative effect: the primary effect is observed a few days after starting to use Reserpine, reaching its peak only after 3-6 weeks of regular use. The drug is eliminated from the body within 1-6 weeks.

Indications for use of Reserpine

The indication for the use of Reserpine is primarily persistent arterial hypertension; this medicinal substance is included in the list essential means for the treatment of hypertension early stages. The drug is also effective for signs of late gestosis, accompanied by increased blood pressure, thyrotoxicosis, heart failure in mild form accompanied by moderate tachycardia.

Previously, mental illness was considered an indication for the use of Reserpine.: psychosis, schizophrenia, accompanied by psychomotor agitation, manic phase of MDP, depressive agitation in patients with senile psychosis, as well as neurosis and neurosis-like conditions. However, currently the use of Reserpine as antipsychotic limited, it is practically not used due to the availability of more effective and fast-acting drugs.

Instructions for use of Reserpine

The drug is taken orally, after meals, the tablets must be washed down with a sufficient amount of clean water.

In accordance with the instructions, Reserpine is prescribed for treatment initial stages hypertension in the following dosage:

0.1 mg per day, 2 times - morning and evening for 5-7 days. If there is no therapeutic effect during this time, the dosage is increased depending on the indications, adjusting if necessary daily dose up to 0.5 mg, divided into 2 doses. When the patient's condition has stabilized and blood pressure has reached normal indicators, the dosage is gradually reduced, returning to 0.1 mg per day as maintenance therapy. The course of treatment is 2-3 months.

The drug for other indications (late gestosis, tachycardia, thyrotoxicosis, etc.) is prescribed as part of complex therapy, and therefore it is necessary to take into account its interaction with other medicinal substances. In this case, according to the instructions, Reserpine is prescribed according to an individual regimen, in accordance with the instructions of the attending physician.

Reserpine is approved for use in pediatric practice; the dosage is determined by the attending physician individually, depending on the indications.

Side effects

The use of Reserpine may result in the following undesirable effects:

  • From the nervous system - headache, dizziness, sleep disturbance, anxiety, weakness, increased fatigue, hyporeflexia, poor concentration, depression, extrapyramidal disorders, decreased libido;
  • From the outside digestive system– signs of dyspepsia, pain in the epigastric region, loss of appetite, dry mouth, gastrointestinal bleeding(rarely);
  • From the outside of cardio-vascular system– arrhythmia, bradycardia, erectile dysfunction, pain in the chest, redness of the sclera;
  • From the urinary system - disturbances of water-salt metabolism (peripheral edema, swelling or dryness of the mucous membranes), dysuria, anuria;
  • From the outside skin– urticaria, itchy skin, exacerbation of herpetic infection;
  • On the metabolic side, there is an increase in body weight.

In case of an overdose of this drug, in addition to the above, possible following symptoms: parkinsonism, nightmares, liver dysfunction, angina pectoris.

Contraindications to the use of Reserpine

In accordance with the instructions, Reserpine is contraindicated in the following situations:

  • Increased individual sensitivity;
  • Parkinson's disease;
  • History of epilepsy and epilepsy-like seizures;
  • State of depression;
  • Gastric ulcer and duodenum in the acute stage;
  • Ulcerative colitis;
  • Gastritis;
  • Bronchial asthma;
  • Angle-closure glaucoma;
  • Myxedema;
  • Chronic heart failure;
  • Atrioventricular block;
  • Bradycardia;
  • Pheochromocytoma;
  • Atherosclerosis coronary vessels and cerebral vessels;
  • Nephrosclerosis;
  • Pregnancy;
  • Breast-feeding.

Reserpine is not prescribed during electroconvulsive therapy, treatment with MAO inhibitors.

special instructions

Concurrent appointment of others medicines during the use of Reserpine requires medical supervision, since with many of them it enters into unwanted interactions, weakening, strengthening or changing therapeutic effect.

Before the planned surgery treatment with Reserpine is stopped several days before the intervention, if emergency is necessary surgical treatment while taking Reserpine, it is necessary to premedicate with atropine.

The drug Reserpine reduces attention and slows down reaction, and therefore, during therapy with them, performing potentially dangerous work that requires quick reactions is undesirable. You should also be careful when driving a car during this period; doctors recommend stopping driving during treatment.

Storage and release rules

Reserpine is stored in hermetically sealed form, in a dry place inaccessible to direct sunlight, at room temperature within 3 years.

Keep out of reach of children!

Dispensed with a doctor's prescription.

Sincerely,


Included in the preparations

ATX:

C.02.A.A Rauwolfia alkaloids

C.02.A.A.02 Reserpine

Pharmacodynamics:

Depletion of norepinephrine depot (destruction in the MAO axoplasm) in postganglionic sympathetic nerve endings by blocking vesicular transport (sympatholytic effect, persistent reduction in blood pressure), reducing the level of norepinephrine (sedative effect), serotonin (depressive effect) and dopamine (antipsychotic effect) in brain neurons .

Pharmacokinetics:

Absorption is fast. F 50%. Does not bind to plasma proteins. Biotransformation in the liver. The initial half-life is 4.5 hours, the final half-life is 45-168 hours, in case of chronic renal failure - 87-323 hours. Elimination is slow: by the kidneys 8% in the form of metabolites, ‹1% in unchanged form, with feces ›60% in the form of unchanged substances. Not removed by hemodialysis.

Indications:

Arterial hypertension.

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

Contraindications:

Depression, peptic ulcer of the stomach and duodenum in the acute phase, ulcerative colitis in the acute phase, bronchial asthma, bradycardia, serious illnesses cardiovascular system, atherosclerosis cerebral vessels, nephrosclerosis, pregnancy, lactation. Do not use before electropulse therapy.

Pregnancy and lactation:

Contraindicated during pregnancy and breastfeeding.

Directions for use and dosage:

Individual. In adults, it is used at a dose of 200-500 mcg/day, if necessary, the dose is increased. The maximum daily dose is 1 mg.

In children, it is possible to use a dose of 80-400 mcg/day in 2-4 doses, depending on age.

Side effects:

From the cardiovascular system: bradycardia; when used in high doses - increased symptoms of angina pectoris.

From the digestive system: nausea, vomiting, diarrhea, abdominal pain; with long-term use in high doses, liver function may be impaired.

From the central nervous system and peripheral nervous system: drowsiness, fatigue, depressive states, swelling and dryness of the mucous membranes; when used in high doses - nightmares, development of symptoms of parkinsonism.

From the urinary system: urinary retention, increased urination.

Dermatological reactions: herpes, itchy skin.

Others: weight gain, decreased libido, decreased potency.

Overdose:

Symptoms: dizziness, severe drowsiness, redness of the skin, constricted pupils, slow pulse (indirect cholinomimetic effect).

Treatment: symptomatic. Observation - at least 72 hours.

Interaction:

β-blockers- mutual enhancement of pharmacological effects.

Adrenergic and sympathomimetics- mutual decrease in activity.

Alcohol and CNS depressants- increased depressive effect.

Antihypertensive drugs- potentiation of the antihypertensive effect.

Anticholinergics- reducing the effect on gastric secretion.

Bromocriptine- decreased effect on prolactin levels; bromocriptine dose adjustment is necessary.

MAO inhibitors, including ; also - sudden hypertension and hyperpyrexia. It is not recommended to use it during treatment with MAO inhibitors and for 1 week after their discontinuation.

Levodopa- decreased effect requires increasing the dose of levodopa.

NSAIDs, especially - a decrease in the antihypertensive effect.

Cardiac glycosides, quinidine- proarrhythmic effect.

Drugs that cause extrapyramidal disorders- potentiation of extrapyramidal disorders.

Special instructions:

Sympatholytics are considered second-line drugs for arterial hypertension and psychosis due to numerous side effects and low efficiency.

Monitoring: regular blood pressure monitoring.

Distinctive characteristics:

Alkaloid of Rauwolfia serpentina Benth.

Impotence and erectile dysfunction are more pronounced compared to captopril.

The effect on the central nervous system is dose-dependent, most often manifested when using doses above 0.5 mg/day.

Instructions

Recipe for Reserpine

  • Tablets of 0.0001 g (0.1 mg) and 0.00025 g (0.25 mg), in packs of 50 and 100 tablets.
  • Powder (0.00025 g).

Shelf life and storage conditions

Store locked up (list A) in a dry place, protected from light, in a well-closed container.

The shelf life of Reserpine is 3 years.

Properties

(Reserpinum) - 3,4,5-trimethoxybenzoyl methyl reserpate - C 33 H 40 O 9 N 2 - white crystalline powder, poorly soluble in water, soluble in acetic acid and chloroform.

Reserpine is one of the main compounds obtained from the roots of the Rauwolfia serpentine plant ( Rauwolfia serpentina Benth.), a perennial shrub of the Kutrov family, growing in India, Java, Ceylon and the Malay Peninsula.

Reserpine and other alkaloids contained in Rauwolfia serpentine are also found in such types of Rauwolfia as Rauwolfia quatrefoil ( Rauwolfia tetraphylla), rauwolfia grayish ( Rauwolfia canescens), Rauwolfia parviflora ( Rauwolfia micrantha) and etc.

The calming effect of reserpine on the central nervous system is based on its effect on the cerebral cortex, hypothalamic region and reticular formation of the brain stem.

The sedative and hypotensive effects of reserpine are associated with its effect on the metabolism of serotonin, norepinephrine and adrenaline in the brain tissue. The drug does not have adrenolytic properties, although some rauwolfia alkaloids (ajmalicin, yohimbine) do.

The use of reserpine causes depletion of their reserves in the central nervous system, as well as adrenaline and norepinephrine in the endings of the sympathetic nerves, which reduces the adrenergic effect on the effector systems of peripheral organs, including the adrenergic receptors of blood vessels.

Synonyms

H-520. Alserpil. Banazil. Bioserpin. Hypnoserpilus. Hypnoserpin. Idoserp. Interpin. Carditivo L. Kviescin. Kay-Serpin. Christoserpine. Mephaserpine. Neoserfin. Purserpin. Rauacloxylone. Rauwazedin. Rauwerin. Rauvilid. Rauvoleaf. Raudixoid. Rauzan. Rausedil. Rouserpoid. Raulen. Rauloidin. Raunorin. Raupazil. Raurin. Rau-Sed. Rausedan. . Rouserpoid. Rauthrin. Rau-Tropon. Resedin. Resurlor. Rather "Wander". Reserve. Reservamed. Reserpex. Reserve. Reserved. Reserpoid. Reserve. Resorcen. Residine. Rubber Rivazin. Rivascin. Riserpa. Roxel. Roxinoid. Candrill. Sandrine. Sarpagan. Sedaraupin. Sectarian. Serwolfia. Serolphia. Serpazil. Serpazin. Serpalan. Serpanray. Serpanray. Serpat. Serpzol. Serpt. Serpedin. Serpate. Serpen. Serpentyl. Serpivit. Serpicon. Serpiloid. Serpin. Serpipur. Serpoid. Sertabs. Sertin. Surfin. Temposerpin. Tenserpin. Unilord. Elserpin. Escaerp.

Reserpine is an antihypertensive and antipsychotic drug.

Release form

The drug is available in tablets in dosages of 0.1 and 0.25 mg.

Analogues of Reserpine are drugs that contain the same active substance: Adelfan-Ezidrex, Alserin, Relsidrex-G, Trirezid-K, Rausedil, Rausedan, Cristoserpine, Rau-Sed, Serfin, Serpasil, Tenserpine, Hypnoserpine, etc. Reserpine is included also in the composition of some antihypertensive drugs, for example Kristepine.

pharmachologic effect

The active ingredient of the drug is reserpine, one of the alkaloids of the Rauwolfia serpentine plant.(Rauvolfia serpentina). Reserpine is a sympatholytic, i.e. has a predominant effect on the sympathetic nervous system, inhibiting it and, as compensation, activating the parasympathetic. Causes a persistent decrease in blood pressure, largely due to the inactivation of MAO. The antipsychotic effect of Reserpine is based on a decrease in the concentration of neurotransmitters (serotonin, dopamine, etc.) in neurons. Reduces heart rate, reduces total peripheral vascular resistance, promotes deepening physiological sleep, potentiates the effect of sleeping pills and painkillers. The use of Reserpine causes a slowdown in metabolism and normalizes protein-fat metabolism in people suffering from hypertension and coronary atherosclerosis. Under the influence of the drug, breathing becomes deeper and at the same time more rare, the pupil constricts (miosis), and body temperature decreases.

Reserpine activates the production of hydrochloric acid in the stomach and enhances intestinal motility, enhances renal blood circulation, increases glomerular filtration in the kidneys.

This drug has a cumulative effect: the primary effect is observed a few days after starting to use Reserpine, reaching its peak only after 3-6 weeks of regular use. The drug is eliminated from the body within 1-6 weeks.

Indications for use of Reserpine

The indication for the use of Reserpine is primarily persistent arterial hypertension; this medicinal substance is included in the list of the most important drugs for the treatment of hypertension in the early stages. The drug is also effective for signs of late gestosis, accompanied by increased blood pressure, thyrotoxicosis, mild heart failure, accompanied by moderate tachycardia.

Previously, mental illness was considered an indication for the use of Reserpine.: psychosis, schizophrenia, accompanied by psychomotor agitation, manic phase of MDP, depressive agitation in patients with senile psychosis, as well as neurosis and neurosis-like conditions. However, at present, the use of Reserpine as an antipsychotic drug is limited; it is practically not used, due to the availability of more effective and fast-acting drugs.

Instructions for use of Reserpine

The drug is taken orally, after meals, the tablets must be washed down with a sufficient amount of clean water.

In accordance with the instructions, Reserpine is prescribed for the treatment of the initial stages of hypertension in the following dosage:

0.1 mg per day, 2 times - morning and evening for 5-7 days. If there is no therapeutic effect during this time, the dosage is increased depending on the indications, if necessary, bringing the daily dose to 0.5 mg, divided into 2 doses. When the patient's condition has stabilized and blood pressure has reached normal levels, the dosage is gradually reduced, returning to 0.1 mg per day as maintenance therapy. The course of treatment is 2-3 months.

The drug for other indications (late gestosis, tachycardia, thyrotoxicosis, etc.) is prescribed as part of complex therapy, and therefore it is necessary to take into account its interaction with other medicinal substances. In this case, according to the instructions, Reserpine is prescribed according to an individual regimen, in accordance with the instructions of the attending physician.

Reserpine is approved for use in pediatric practice; the dosage is determined by the attending physician individually, depending on the indications.

Side effects

The use of Reserpine may result in the following undesirable effects:

  • From the nervous system - headache, dizziness, sleep disturbance, anxiety, weakness, increased fatigue, hyporeflexia, poor concentration, depression, extrapyramidal disorders, decreased libido;
  • From the digestive system - signs of dyspepsia, pain in the epigastric region, loss of appetite, dry mouth, gastrointestinal bleeding (rarely);
  • From the cardiovascular system - arrhythmia, bradycardia, erectile dysfunction, pain in the chest space, redness of the sclera;
  • From the urinary system - disturbances of water-salt metabolism (peripheral edema, swelling or dryness of the mucous membranes), dysuria, anuria;
  • On the part of the skin – urticaria, skin itching, exacerbation of herpetic infection;
  • On the metabolic side, there is an increase in body weight.

In case of an overdose of this drug, in addition to the above, the following symptoms are possible: parkinsonism, nightmares, liver dysfunction, angina pectoris.

Contraindications to the use of Reserpine

In accordance with the instructions, Reserpine is contraindicated in the following situations:

  • Increased individual sensitivity;
  • Parkinson's disease;
  • History of epilepsy and epilepsy-like seizures;
  • State of depression;
  • Peptic ulcer of the stomach and duodenum in the acute stage;
  • Ulcerative colitis;
  • Gastritis;
  • Bronchial asthma;
  • Angle-closure glaucoma;
  • Myxedema;
  • Chronic heart failure;
  • Atrioventricular block;
  • Bradycardia;
  • Pheochromocytoma;
  • Atherosclerosis of coronary and cerebral vessels;
  • Nephrosclerosis;
  • Pregnancy;
  • Breast-feeding.

Reserpine is not prescribed during electroconvulsive therapy or treatment with MAO inhibitors.

special instructions

The parallel administration of other medications while using Reserpine requires medical supervision, since it interacts with many of them in undesirable ways, weakening, enhancing or changing the therapeutic effect.

Interaction

Enhances the effects of alcohol, central nervous system depressants, beta-blockers, antidepressants (MAO inhibitors), antihypertensive drugs, and increases adverse reactions when prescribing cardiac glycosides and quinidine. Reduces the effectiveness of antiparkinsonian drugs and sympathomimetics.

Overdose

Symptoms: drop in blood pressure, bradycardia, central nervous system depression, nightmares, coma, hypothermia, miosis, tremor, parkinsonism, diarrhea, vomiting; with long-term use in high doses - liver dysfunction

Treatment: symptomatic: intravenous fluid infusion, positioning with legs elevated, and, if necessary, intravenous infusion of pressor amines.

In the article we will look at the instructions for use for the drug "Reserpine", price, reviews and analogues.

It is a complex sympatholytic drug that has antihypertensive, antipsychotic and sedative effect. Active substance this drug is one of the alkaloids of such rare plant, How

Pharmacokinetics

The drug "Reserpine" is an antispasmodic that mainly affects the nervous system. sympathetic system, reducing the effect of which allows you to activate the parasympathetic. It has a compensatory effect.

This drug can cause a persistent decrease in blood pressure. This is indicated by the instructions for use. At what pressure it is permissible to prescribe Reserpine is of interest to many. It is effective in case of elevated

The antipsychotic effect is based on a decrease in the concentrations of certain neurotransmitters in neurons, these include serotonin and dopamine. The medicine contains the active substance - reserpine, hydrochlorothiazide, dihydralazine sulfate.

Reserpine produces the following therapeutic effect on the human body:

  • inhibits heart contractions;
  • reduces total peripheral vascular resistance;
  • deepens and strengthens physiological sleep;
  • slows down metabolism in patients suffering from hypertension and coronary atherosclerosis;
  • strengthens the influence of such a group of drugs as sleeping pills and painkillers;
  • stabilizes the metabolism of fats and proteins;
  • normalizes breathing, it becomes rarer and deeper;
  • the pupil narrows, the temperature decreases;
  • the production of hydrochloric acid by the stomach is activated;
  • intensifies intestinal peristalsis;
  • blood supply to the kidneys improves;
  • renal glomerular filtration increases.

What else does the instructions for use for Reserpine tell us?

The drug also has a cumulative effect, since the primary effect is observed after a few days of its use, the maximum effect is achieved after 2-6 weeks if taken regularly.

The time for complete removal of the drug from the body is approximately 4-6 weeks.

According to the instructions for use, what are the indications for Reserpine?

Indications

"Reserpine" is used for the following pathologies:

Possible contraindications

According to the instructions for use, Reserpine cannot be used by all patients who need it, so its use should be avoided if:

  • peptic ulcers of the duodenum and stomach;
  • depression;
  • bronchial asthma;
  • serious illnesses heart and blood vessels;
  • bradycardia;
  • nephrosclerosis;
  • Parkinson's disease;
  • atherosclerosis of cerebral type vessels;
  • prescribing therapy using electrical impulses;
  • hypersensitivity to the components of this drug;
  • respiratory failure;
  • cholelithiasis;
  • pheochromocytoma;
  • angle-closure glaucoma;
  • chronic failure hearts;
  • breastfeeding and pregnancy.

Side symptoms

Below you will find the price and reviews of Reserpine.

The instructions for use indicate that when using the drug, undesirable symptoms may also occur:

  • digestive system: patients note painful sensations in the epigastric region, symptoms of dyspepsia, a feeling of dryness in the mouth, severe loss of appetite, bleeding from the intestines and stomach is rarely observed;
  • nervous system: headaches, sleep disturbances, the patient’s anxiety, excessive fatigue, decreased libido, hyporeflexia are recorded;
  • blood vessels and heart: arrhythmia, bradycardia and pain in the space behind the sternum are noted;
  • urinary system: responds to the drug "Reserpine" with disturbances in the exchange of salts and water, manifested in dryness and peripheral edema of the mucous membranes, in addition, dysuria and anuria may appear;
  • epidermal integuments: urticaria, skin itching, exacerbation of herpetic infection;
  • Cases of liver dysfunction and human weight gain have been observed.

Instructions for use "Reserpine"

The drug is taken orally after meals and washed down with water or any liquid in sufficient volume. In accordance with the instructions, the drug is prescribed for the treatment of the initial stage of hypertension at a dosage of 0.1 mg twice a day. The duration of its use is approximately seven days. If there is no therapeutic effect during this period, it is recommended to increase the dose of the drug to 0.5 mg, also dividing into two doses.

If a person’s stable condition has been achieved and blood pressure has reached the required levels, then the dosage is gradually reduced to 0.1 mg. The medicine is taken after this for maintenance therapy.

Full treatment course lasts from two to four months.

Also, the medicine can be prescribed for complex therapy for other indications (tachycardia, thyrotoxicosis, late gestosis) and used along with other drugs. In such cases, it is prescribed strictly individually.

Overdose

According to the instructions for use for Reserpine tablets, when using them in excessive dosage, the following symptoms may appear:

  • sudden decrease in blood pressure;
  • diarrhea;
  • bradycardia;
  • nightmares;
  • parkinsonism;
  • coma;
  • vomit;
  • hypothermia;
  • tremor;
  • liver dysfunction.

Therapy for such symptoms is symptomatic and consists of intravenous administration of medication. In special situations, intravenous infusion of pressor amines is required.

Drug interactions

The instructions for use for Reserpine also indicate that with parallel use of the product and other medical supplies Supervision by a specialist is always required, because this substance can interact with many medications, weakening or enhancing their therapeutic effect. Let us describe such interactions in more detail.

  1. Foxglove remedies enhance possible risk the appearance of bradycardia.
  2. Combined use with ethanol, barbiturates, tricyclic antidepressants, drugs inhalation anesthesia enhances their influence.
  3. "Reserpine" can reduce the effectiveness of antiepileptic drugs and anticholinergic drugs, as well as reduce the analgesic effect of morphine.
  4. "Reserpine" promotes a longer-lasting effect of direct adrenomimetic drugs.
  5. When eye drops are prescribed, an increase in blood pressure is recorded.
  6. When using tricyclic antidepressants, the hypotensive effect of Reserpine decreases.
  7. The drug "Fenfluramine" enhances the hypotensive effect of the drug, and "Methyldopa" develops a state of depression.

Price

The price of the drug ranges from 380-420 rubles. It depends on the pharmacy chain and region.

Analogs

“Reserpine” has such analogues as “Christoserpin”, “Eskazerp”, “Rausedil”, “Raupazil”, “Alserin”, “Raused Serfin”, “Tenserpin”, “Kvescin”, “Rausedan”, “Serpin”, “ Roksinoid", "Serpiloid", "Sedaraupin", "Tenserpin", "Serpat".

POLFA ICN ICN Polfa Rzeszow SA

Country of origin

Poland

Product group

Cardiovascular drugs

Antihypertensive drug

Release forms

  • Film-coated tablets - 20 pcs per pack.

Description of the dosage form

  • Film-coated tablets white, round, biconvex, with a smooth surface.

pharmachologic effect

Normatens is a combined antihypertensive drug containing 3 complementary components. Reserpine, a sympatholytic, penetrating into the presynaptic endings of postganglionic sympathetic fibers, releases norepinephrine from vesicles while simultaneously disrupting its reverse transport and enhancing the process of inactivation by monoamine oxidase (MAO). Causes depletion of neurotransmitter reserves and a persistent decrease in blood pressure (BP). Helps 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 (HR) and total peripheral vascular resistance; maintains the activity of the parasympathetic nervous system; deepens and enhances physiological sleep, inhibits interoceptive reflexes. Increases peristalsis of the gastrointestinal tract, increases the production of hydrochloric acid in the stomach; slows down metabolic processes in organism; cuts and deepens breathing movements, causes miosis, hypothermia; reduces metabolic rate. Renders positive influence to lipid and protein metabolism in patients arterial hypertension and coronary atherosclerosis; increases renal blood flow, enhances glomerular filtration. Clopamide is a “loop” sulfonamide diuretic of medium strength, blocks the reabsorption of sodium ions at the level of the cortical segment of the loop of Henle, removes sodium, potassium, chlorine and water ions. Dihydroergocristine is a dihydrogenated ergot alkaloid, blocks alpha-adrenergic receptors, causes vasodilation, and reduces overall peripheral vascular resistance. The hypotensive effect of the drug exceeds the hypotensive effect of each of the components separately and the effect of any combination of two components; onset of action is on days 4-7, a persistent hypotensive effect is achieved after 1-4 weeks.

Pharmacokinetics

Absorption The individual components of Normatens are absorbed after oral administration as follows: reserpine by approximately 30-40%, clopamide by about 90% and dihydroergocristine by less than 25%. Maximum concentration 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, the volume of distribution is 52 l/kg). Bonding with blood plasma proteins: for reserpine - no binding, clopamide - about 46%, dihydroergocristine - about 68%. Reserpine and dihydroergocristine penetrate the blood-brain barrier and the placental barrier. Metabolism Reserpine and dihydroergocristine are extensively metabolized in the liver to inactive metabolites. Clopamide does not undergo significant metabolism in the liver. Elimination The half-life (T 1/2) of Normatens is long due to the presence of reserpine, for which T 1/2 is 4.5 hours in the first phase, and about 271 hours in the second. The route of elimination is different for individual components: reserpine and dihydroergocristine - inactive metabolites are excreted in urine and feces, clopamide, mainly by the kidneys.

Special conditions

Since the effect of Normatens develops relatively slowly, the dosage should not be increased more than once a week, due to the possibility of a pronounced decrease in blood pressure; special care must be taken in case of joint use with other antihypertensive drugs; During treatment, periodically monitor blood pressure levels to determine optimal mode dosing. During treatment, glucose levels may increase and uric acid in blood serum, 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. If bradycardia occurs during treatment, the dose of the drug must be reduced or the drug discontinued. During treatment, monitoring of serum potassium is necessary. In most patients, additional potassium supplementation is not required, provided that the diet contains sufficient quantity foods rich in potassium (fruits, vegetables, fish, low-fat cheese, etc.). Caution should be exercised in patients with bronchial asthma and bronchospasms, 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 drug. During treatment you should not drink alcohol. The dose of Normatens should be modified accordingly in case of simultaneous use of other drugs that interact with it. 7 days before the start of electroconvulsive therapy, Normatens should be discontinued. Effect on the ability to drive vehicles and operate machinery Normatens may impair the patient’s ability to react quickly, especially at the beginning of treatment. During the treatment period, you should not drive vehicles or engage in any activities that require increased concentration attention and speed of psychomotor reactions.

Compound

  • dihydroergocristine mesylate 580 mcg, which corresponds to the content of dihydroergocristine 500 mcg clopamide 5 mg reserpine 100 mcg Excipients: lactose monohydrate, potato starch, povidone (polyvinylpyrrolidone), talc (magnesium hydrosilicate), magnesium stearate. Shell composition: crystalline sucrose, acacia gum (gum arabic), talc (magnesium hydrosilicate), macrogol 6000

Normatens indications for use

  • Arterial hypertension.

Normatens contraindications

  • * increased sensitivity to any of the components of the drug. * depression, Parkinson's disease, epilepsy, concomitant electroconvulsive therapy; * pheochromocytoma, concomitant treatment monoamine oxidase inhibitors (MAO); * peptic ulcer of the stomach and duodenum in the acute phase, erosive gastritis, nonspecific ulcerative colitis; * angina pectoris, recent myocardial infarction, chronic heart failure, severe bradycardia, atrioventricular block, intraventricular block; * heavy renal failure(creatinine clearance below 30 ml/min), nephritis, uremia, nephrosclerosis; * arterial hypotension, severe cerebral atherosclerosis; * severe violations liver functions; * Addison's disease; * hypokalemia, hyponatremia, hypochloremia; * hyperuricemia with clinical manifestations; * angle-closure glaucoma; * hematopoietic disorder;

Normatens side effects

  • From the digestive system: diarrhea, dry mouth, abdominal pain, nausea, vomiting, exacerbation of the disease peptic ulcer, loss of appetite. Rarely - ulceration of the mucous membrane of the stomach and duodenum, gastrointestinal bleeding when using reserpine at a dose above 1 mg per day (the amount contained in 10 Normatens tablets); From the cardiovascular system: bradycardia, decreased blood pressure, cerebrovascular disorders, orthostatic hypotension; From the central nervous system: headache, dizziness, drowsiness, weakness, anxiety, impaired concentration, insomnia, extrapyramidal disorders (tremor, stupor, Parkinson's syndrome). Since the drug contains reserpine, you should be aware of the possibility of depressive reactions(including suicidal tendencies) and depressive syndrome; such symptoms appear rarely and only in cases of large doses of reserpine (more than 1 mg/day, which corresponds to the reserpine content of more than 10 Normatens tablets). From the outside respiratory system: hyperemia and swelling of the nasal mucosa. Reserpine can cause symptoms of bronchospasm, but this effect occurs rarely, and, as a rule, in patients with bronchial asthma or broncho-obstructive syndrome. Allergic reactions: skin rash, itching. From the hematopoietic organs: thrombocytopenia with symptoms of hemorrhagic diathesis.

Drug interactions

Reduces the effectiveness of oral hypoglycemic drugs, tricyclic antidepressants, anticoagulants. Increases the concentration of lithium in the blood plasma (slowing its excretion). Weakens the effect of antiepileptic drugs and levodopa, anticholinergics, reduces the analgesic effect of morphine. Enhances the effect of barbiturates, ethanol, drugs for inhalation anesthesia, antihistamines. Enhances the effect of adrenergic agonists. Barbiturates, ethanol, beta-blockers, peripheral vasodilators enhance the hypotensive effect. Glucocorticosteroids, non-steroidal anti-inflammatory drugs, laxatives medicines reduce diuretic, hypotensive effects, increase the risk of hypokalemia. During treatment with MAO inhibitors, the inhibitory effect on the central nervous system increases. During treatment with the drug, MAO inhibitors cause moderate or severe arterial hypertension.

Storage conditions

  • keep away from children
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