Baclosan

Release form, composition and packing Baclosan 

Pill white, round, biconvex, with a separating mark. 1 tab. baclofen 10 mg. Excipients: lactose, potato starch, gelatin, talc, magnesium stearate, ethylcellulose.

Pill white, round, biconvex. 1 tab. baclofen 25 mg. Excipients: lactose, potato starch, gelatin, talc, magnesium stearate, ethylcellulose.

Clinico-pharmacological group: Relaxant central action.

Pharmacological action

Centrally acting muscle relaxant; GABAB-receptor agonist. Reducing the excitability of the terminal divisions of the afferent sensory fibers and suppressing the intermediate neurons, depresses mono-and polysynaptic transmission of nerve impulses, reduces the prestressing muscle spindles. Does not affect the transmission of impulses in the nerve-muscle synapses.

In neurological diseases involving skeletal muscle spasticity, reduces the painful spasms and clonic convulsions. Increases the amount of movement in joints, facilitates active and passive kinesitherapy (exercise, massage, chiropractic).

Pharmacokinetics

Suction

After oral administration, baclofen is rapidly and completely absorbed from the gastrointestinal tract. Cmax in blood plasma is reached 2-3 h after dosing.

Distribution

Plasma protein binding is about 30%. Baclofen crosses the placental barrier, excreted in breast milk.

Metabolism

Metabolized in the liver.

Breeding

Excreted in the urine, mainly unchanged.

Statement

Increased muscle tone:
multiple sclerosis;
in diseases of the spinal cord of an infectious, degenerative and traumatic origin (eg, tumors, syringomyelia, motor neuron disease, injury);
stroke;
with Cerebral Palsy;
of meningitis;
with traumatic brain injuries;
in alcoholism (affective disorders).

Dosing regimen

Set individually. Adult prescribe medication in an initial dose of 5 mg 3 times / day every 3 days gradually increase the dose to the development of optimal therapeutic effect (usually up to 30-75 mg / day). Patients who need to use the drug in higher doses (usually up to 30-75 mg / day), Baklosan prescribed in tablets of 25 mg. The maximum daily dose - 100 mg.

Patients older than 65 years the drug dose should be increased with caution due to an increased risk of side effects. Initial single dose for children is 5 mg, the multiplicity of reception 3 times a day.

If necessary, carefully increase the dose every 3 days. The average recommended doses are for children aged 1 to 2 years - 10-20 mg / day, from 2 to 6 years - 20-30 mg / day, from 6 to 10 years - 30-60 mg / day.

In children older than 10 years, the maximum daily dose is determined by the rate of 1.5-2 mg / kg body weight. The drug is taken with meals. When Missed not take a double dose.

Side effect
CNS and peripheral nervous system: drowsiness, dizziness, gait disturbance, fatigue, confusion, apathy, euphoria, depression, paresthesias, ataxia, tremor, nystagmus, paresis of accommodation, hallucinations, convulsions, decreased seizure threshold.
From the digestive system: nausea, vomiting, dry mouth, constipation, diarrhea.
With the urinary system: urinary retention, dysuria, enuresis, with prolonged use - renal dysfunction.
Cardio-vascular system: blood pressure reduction.

Other: myalgia, muscular weakness.

Contraindications
psychosis;
Parkinson's disease;
epilepsy;
convulsions (history);
chronic renal failure;
pregnancy;
Lactation (breastfeeding), increased sensitivity to baklofenu.

With carefully administered medication in cerebrovascular disease, atherosclerosis of cerebral vessels in patients with gastric ulcer and duodenal ulcer, elderly patients, children under the age of 12 years.

Pregnancy and lactation

The drug is contraindicated during pregnancy and lactation (breastfeeding).

Use in hepatic dysfunction

In patients with liver disease should periodically monitor the activity of hepatic transaminases.

Use in renal impairment

Contraindicated in chronic renal failure.

Cautions

In patients with liver disease and diabetes should regularly monitor the activity of hepatic transaminases and alkaline phosphatase, and blood glucose.

Effects on ability to drive vehicles and management mechanisms

Patients taking Baklosan should refrain from potentially dangerous activities associated with the necessity of increased attention and rapid psychomotor reactions.

Overdose

Symptoms: muscular hypotonia, respiratory center depression, confusion, coma (after the return of consciousness muscular hypotonia may persist for 72 h).

Treatment: excessive drinking, taking diuretics, and respiratory depression - AV. A specific antidote does not exist.

Drug Interactions

While the application Baklosan enhances the action of drugs affecting the central nervous system, hypotensive drugs, ethanol.

While the application Baklosana with tricyclic antidepressants can significantly decrease muscle tone. Patients with Parkinson's disease while receiving Baklosana with levodopa and carbidopa may have hallucinations, confusion, agitation.

Conditions and terms of

List B. The drug should be stored in a dry place, protected from light and away from children at or above 25 ° C. Shelf life - 5 years.

Basiron AC

Release form, composition and packing Basiron AC 

Gel for external use only 2.5% of 1 g of benzoyl peroxide 25 mg. Other ingredients: acrylate copolymer, poloxamer 182, carbomer 940 (carbopol 980), glycerin, disodium edetate, sodium dioctyl sulfosuccinate, propylene glycol, silica colloidal anhydrous, sodium hydroxide, distilled water.

Gel for external use only 5% of 1 g of benzoyl peroxide 50 mg. Other ingredients: acrylate copolymer, poloxamer 182, carbomer 940 (carbopol 980), glycerin, disodium edetate, sodium dioctyl sulfosuccinate, propylene glycol, silica colloidal anhydrous, sodium hydroxide, distilled water.

Gel for external use only 10% of 1 g benzoyl peroxide, 100 mg. Other ingredients: acrylate copolymer, poloxamer 182, carbomer 940 (carbopol 980), glycerin, disodium edetate, sodium dioctyl sulfosuccinate, propylene glycol, silica colloidal anhydrous, sodium hydroxide, distilled water.

Clinico-pharmacological group: Drug for the treatment of acne.

Pharmacological action

The drug has high antimicrobial activity against Propionibacterium acnes and Staphylococcus epidermidis, has komedonoliticheskoe and anti-inflammatory effect, improves oxygenation of tissues, suppresses production of sebum in the sebaceous glands, absorbs excess sebaceous secretions and moisturizes the skin. Benzoyl peroxide, being a powerful oxidizing agent, has a strong bactericidal effect on microorganisms, with micro-organisms are not able to develop resistance to benzoyl peroxide strains. In in vivo studies on the results of seeding, it was shown that the inhibition of culture growth Propionibacterium acnes by 94% observed at the 7 th day and 15-day - at 97-99%.

Anti-inflammatory effect benzoyl peroxide based on the inactivation of free radicals in the inflammation and inhibition of free fatty acids. Basis of preparation before the complex acrylate copolymer / glycerin, it provides a controlled adsorption of excess sebum and gradual release of glycerin to soften and moisturize the skin.

Pharmacokinetics

Most of benzoyl peroxide biotransformed into benzoic acid (95%) in the human skin; unchanged benzoic acid is rapidly excreted in the urine. Data accumulation in the tissues there. In preparation revealed no systemic action.

Statement
eels.

Dosing regimen

The drug should be applied to clean and dry surface of affected skin areas 1 or 2 times a day (morning or evening). The course of treatment - 3 months. Therapeutic effect develops within 4 weeks after the start of treatment.

Sustained improvement comes after 3 months of therapy. Baziron AU is indicated for the treatment of acne is mild to moderate severity with the prevalence of pustular elements as a single agent, while moderate acne in combination with other local (retinoids) and systemic (antibiotics, antiandrogens for ingestion). If necessary, may conduct re-treatment.

Side effect

Rare: skin irritation at the site of application of the drug, dry skin, allergic reactions. There is no data on the development of systemic side effects when applied externally drug Baziron AU at the recommended doses.

Contraindications
Children up to age 12 years;
hypersensitivity to the drug.

Pregnancy and lactation

It is not recommended to use the drug Baziron AU during pregnancy and lactation.

Cautions

When a skin irritation after applying the gel Baziron AU should be abolished. Do not apply the gel on the skin to damage the integrity of the skin.

In case of accidental contact with the drug on the mucous membrane of eyes, mouth or nose, you should thoroughly rinse it with warm water. During the period of the drug should avoid exposure to the field of its application to direct sunlight, since it can cause skin irritation.

During the period of Bazirona AU is not recommended the simultaneous use of Dries up oily or irritating (or spirits etanolsoderzhaschie means).

Overdose

Symptoms: When a random drawing of a large quantity of the drug on the skin may cause strong irritation at the site of application.

Treatment: The drug should be discontinued and symptomatic treatment.

Drug Interactions

Data on drug interactions drug Baziron AU applied for indications and recommended doses, other drugs for topical and systemic application is currently unavailable.

Conditions and terms of

The drug should be stored at temperatures not above 25 ° C. Shelf life - 3 years.

Byetta

Release form, composition and packing Byetta 

Solution for subcutaneous injection is colorless and transparent. 1 mL of 250 mcg exenatide. Excipients: sodium acetate trihydrate, glacial acetic acid, mannitol, m-cresol, water, d / and.

Clinico-pharmacological group: hypoglycemic agents.

Pharmacological action

Hypoglycemic medication. Exenatide (eksendin-4) is a mimetic inkretina and a 39-amino acid amidopeptidom. Inkretiny, such as glucagon-like peptide-1 (GLP-1), glyukozozavisimuyu increase insulin secretion, improve the function of beta cells, inhibit glucagon secretion increased inadequate and slow gastric emptying after getting into the bloodstream from the intestine. Exenatide is a potent mimetics inkretina, which causes increased insulin secretion glyukozozavisimoy and provides other hypoglycemic effects of inherent inkretinam that allows you to improve glycemic control in patients with type 2 diabetes mellitus.

Amino acid sequence of exenatide partially corresponds to the sequence of human GLP-1, resulting in it binds to and activates the receptor GLP-1 in humans, which leads to increased glyukozozavisimogo synthesis and secretion of insulin from beta cells of the pancreas, with the participation of cyclic AMP and / or other intracellular signaling ways. Exenatide stimulates insulin release from beta cells in the presence of elevated concentrations of glucose.

On the chemical structure and pharmacological action exenatide differs from insulin, sulfonylureas, D-phenylalanine derivatives, and meglitinidov, biguanides, thiazolidinediones and alpha-glucosidase inhibitors.

Exenatide improves glycemic control in patients with type 2 diabetes mellitus through the following mechanisms. At hyperglycemic states exenatide enhances insulin secretion glyukozozavisimuyu of beta cells of the pancreas. This secretion of insulin stops the lowering of blood glucose concentrations and bringing it closer to the norm, thereby decreasing the potential risk of hypoglycemia.

Insulin secretion during the first 10 minutes, known as the "first phase insulin response, specifically absent in patients with type 2 diabetes mellitus. In addition, the loss of first phase insulin response is an early dysfunction of beta cells in diabetes mellitus type 2. Introduction Exenatide restores or greatly enhances both the first and second phase insulin response in patients with type 2 diabetes mellitus. In patients with type 2 diabetes against the background of hyperglycemia introduction of exenatide suppresses excessive secretion of glucagon. However, exenatide does not disturb the normal glucagon response to hypoglycemia.

It was shown that the introduction of exenatide leads to a decrease in appetite and decrease food intake, inhibits the motility of the stomach, which slows down its emptying.

In patients with type 2 diabetes therapy exenatide in combination with metformin and / or a sulfonylurea leads to a decrease in the concentration of fasting blood glucose, postprandial blood glucose, as well as measure HbA1c, thereby improving glycemic control in these patients.

Pharmacokinetics

Suction

After subcutaneous injection exenatide at a dose of 10 mg in patients with type 2 diabetes mellitus exenatide rapidly absorbed and reaches the average C max by 2.1 hours, which amounts to 211 pg / ml, AUCo-inf was 1036 pg x hr / ml. Under the action of exenatide AUC increases proportionally with increasing doses of 5 micrograms to 10 micrograms, with no observed proportional increase Smah. Same effect was observed when s / c infusion exenatide in the abdomen, hip or forearm.

Distribution

Vd exenatide after subcutaneous injection of 3.28 liters. Metabolism and excretion of Exenatide is derived mainly through glomerular filtration with subsequent proteolytic decay. Exenatide clearance is 9.1 l / h. End T1 / 2 is 2.4 h. These pharmacokinetic characteristics Exenatide does not depend on the dose. Measured concentrations of exenatide determined for approximately 10 hours after dosing.

Pharmacokinetics in special clinical situations

Patients with mild or moderate, impaired renal function (creatinine clearance 30-80 ml / min), exenatide clearance was not significantly different from clearance in patients with normal renal function, and therefore correction of the dose is not required. However, in patients with end-stage renal failure on dialysis, the average clearance was reduced to 0.9 l / h (compared with 9.1 l / h in healthy subjects). Because exenatide is mainly excreted by the kidneys, it is believed that liver dysfunction does not alter the concentration of exenatide in the blood. Age does not influence the pharmacokinetic characteristics of exenatide. Therefore, elderly patients do not require correction of the dose.

Exenatide pharmacokinetics in children has not been studied. Between men and women in clinically important differences in the pharmacokinetics of exenatide is not observed.

Exenatide pharmacokinetics in representatives of different races virtually unchanged. Dose adjustment taking into account the ethnic origin do not want to spend. Not observed a significant correlation between body mass index (BMI) and pharmacokinetics of exenatide. Dose adjustment taking into account the BMI of conduct is not required.

Statement
Type 2 diabetes as adjunctive therapy to metformin, sulfonylureas, thiazolidinediones, a combination of metformin and sulfonylureas, or metformin and tiazoldindiona in case of failure to reach adequate glycemic control.

Dosing regimen

The drug is administered sc in the thigh, abdomen or upper arm. The initial dose is 5 mg, is administered 2 times a day, at any time during the 60-minute period before the morning and evening meals. Should not be given the drug after meals.

In the case of pass the injection treatment is continued without changing the dose. 1 month after starting treatment dose can be increased to 10 mg 2 times a day. At a joint appointment with metformin, thiazolidinediones, or with a combination of these drugs, starting dose of metformin and / or thiazolidinediones can not be changed. In the case of a combination drug Byetta with derivatives of sulfonylurea may need to decrease the dose of sulfonylurea derivatives to reduce the risk of hypoglycemia.

Side effect

Adverse reactions are more common than in isolated cases are listed in accordance with the following scale: very common (≥ 10%), frequent (≥ 1% but <10%),> 0.1% but <1%)> 0.01% but <0.1%), rarely (<0.01%).
From the digestive system: Very common - nausea, vomiting, diarrhea, and often - loss of appetite, indigestion, gastroesophageal reflux, and sometimes - abdominal pain, bloating, belching, constipation, impaired sense of taste, flatulence.
CNS: Frequently - dizziness, headache, rarely - drowsiness.
From the endocrine system: very often - hypoglycemia (in combination with sulfonylureas), and often - the feeling tremors, weakness, hyperhidrosis.

Allergic reactions: seldom - a rash, itching, angioedema, is extremely rare - anaphylactic reaction.

Other: often - a skin reaction at the injection site, rarely - dehydration (associated with nausea, vomiting and / or diarrhea). Several reported cases increasing clotting time (INR), while the application of warfarin and exenatide, which is sometimes accompanied by bleeding. Because frequency of hypoglycemia increases when the joint appointment of the drug Byetta with sulfonylureas, there should be reduction of the dose sulfonylureas increases the risk of hypoglycemia.

Most episodes of hypoglycemia, the intensity was weak or moderate, were stopped and oral intake of carbohydrates. In general, side effects from the intensity was weak or moderate and did not lead to the abolition of the treatment. Most frequently recorded nausea of mild or moderate intensity was dose dependent and decreased with time, not interfering with daily activities.

Contraindications
type 1 diabetes mellitus or the presence of diabetic ketoacidosis;
severe renal insufficiency (creatinine clearance <30 ml / min);
the presence of severe gastrointestinal illness associated with gastroparesis;
pregnancy;
Lactation (breastfeeding);
Children up to age 18 (safety and efficacy in children has not been established);
hypersensitivity to the drug.

Pregnancy and lactation

The drug is contraindicated during pregnancy and lactation.

Use in renal impairment

The drug is contraindicated in severe renal insufficiency (creatinine clearance <30 ml / min).

Cautions

Not recommended w / or / m administration. The drug Byetta should not be used if the solution is detected particles or if the solution is cloudy or has a stain. During therapy with the drug Byetta may appear antibodies to exenatide.

However, this does not affect the frequency and types of recorded side effects. Patients should be informed that treatment with Byetta may lead to a decrease in appetite and / or body weight, and that because of these effects is not necessary to modify the dosing regimen.

Patients before starting treatment with Byetta should familiarize themselves with the drug attached to the "Guidelines on the use of syringe-pen." Results of experimental studies in preclinical studies in mice and rats revealed no carcinogenic effects exenatide. When rats dose, in doses 128 times higher than the dose in humans, noted a numerical increase in C-cell adenomas of the thyroid gland without any signs of malignancy, which was associated with increased longevity in experimental animals receiving exenatide.

Overdose

In case of overdose (dose 10 times higher than the maximum recommended dose) were observed following symptoms: severe nausea and vomiting and rapid development of hypoglycemia.

Treatment: symptomatic therapy, including parenteral administration of glucose in the case of severe hypoglycemia.

Bagothyrox

Release form, composition and packing Bagothyrox 
Pill yellow, rectangular, with three notches on each side, on each of four equal parts tablets impression "T4" on both sides. 1 tab. levothyroxine sodium 50 mg. Inactive ingredients: microcrystalline cellulose, powdered cellulose, lactose monohydrate, magnesium stearate, sodium croscarmellose, Quinoline yellow dye.

Tablets white, rectangular, with three notches on each side, on each of four equal parts tablets impression "T4" on both sides. 1 tab. levothyroxine sodium 100 mcg. Inactive ingredients: microcrystalline cellulose, powdered cellulose, lactose monohydrate, magnesium stearate, sodium croscarmellose.

Pill blue, rectangular, with three notches on each side, on each of four equal parts tablets impression "T4" on both sides. 1 tab. levothyroxine sodium 150 mcg. Inactive ingredients: microcrystalline cellulose, powdered cellulose, lactose monohydrate, magnesium stearate, sodium croscarmellose, brilliant blue dye.

Clinico-pharmacological group: preparation of thyroid hormones.

Pharmacological action

The preparation of thyroid hormones, synthetic levogyrate isomer of thyroxine. After partial conversion to triiodothyronine (in the liver and kidneys) and the transition to the body's cells, influences the growth and development of tissue metabolism.

When used in low doses has anabolic effects on protein and fat metabolism.

When used in moderate doses stimulate the growth and development of the organism, increases in oxygen demand of tissues, stimulates the metabolism of proteins, fats and carbohydrates, increases the functional activity of the cardiovascular system and central nervous system. When used in high doses inhibits the production of thyrotropin-releasing hormone, hypothalamus and pituitary thyroid stimulating hormone. Therapeutic effect observed after 7-12 days, during the same time preserves the action after the drug. Clinical effect of hypothyroidism is manifested in 3-5 days. Basedow's disease is reduced or disappears within 3-6 months.

Statement
hypothyroidism;
euthyroid goiter;
as replacement therapy for prevention of recurrence of goiter after thyroid gland resection;
thyroid cancer (after surgery);
toxic goiter after reaching the euthyroid state thyreostatics (as a combination therapy or monotherapy);
as a diagnostic tool during the test thyroid suppression.

Dosing regimen

The daily dose is determined individually depending on the evidence. Bagotiroks take 1 time per day in the morning on an empty stomach, at least 30 minutes before meals. Wash down the pill a little liquid (half a cup of water) and do not chew.

During replacement therapy of hypothyroidism in patients under the age of 55 years in the absence of cardiovascular disease drug is prescribed a daily dose of 1.6-1.8 mg / kg body weight in patients older than 55 years or concomitant cardiovascular diseases - 0.9 mg / kg body. With significant obesity dose calculation should be done on an "ideal weight".

Babies Bagotiroksa daily dose given in 1 reception for 30 minutes before the first feeding. Tablet dissolved in water to a fine mist just before taking this medication. In severe, long-existing hypothyroidism, treatment should be started with caution at low doses - 12.5 mg / day. Increase the dose to maintenance at longer intervals - 12.5 mg / day every 2 weeks - and often determine the level of TSH.

Hypothyroid Bagotiroks usually take in a lifetime. When thyrotoxicosis take medication in the treatment of thyreostatics after reaching the euthyroid state. In all cases, the duration of drug treatment is determined individually.

Side effect

Using the drug in recommended doses and under the supervision of a doctor side effects are not observed. Hypersensitivity to the drug may experience allergic reactions.

Contraindications
untreated hyperthyroidism;
Acute myocardial infarction;
acute myocarditis;
untreated adrenal insufficiency;
increased individual sensitivity to the drug.

Precautions should be prescribed the drug for coronary heart disease (including atherosclerosis, angina pectoris, history of myocardial infarction), hypertension, arrhythmia, diabetes, severe long-existing hypothyroidism, malabsorption syndrome (may require dose adjustment).

Pregnancy and lactation

During pregnancy and lactation (breastfeeding) should continue therapy with drugs prescribed at the hypothyroidism.

During pregnancy require increased doses of the drug because of elevated levels of thyroxine-binding globulin. Number of thyroid hormone secreted in breast milk during lactation (even during treatment with high-dose) is insufficient to cause any disturbances in the child.

Use of the drug during pregnancy in combination with thyreostatics contraindicated because receiving levothyroxine may require increased doses thyreostatics. Since thyreostatics, unlike levothyroxine, can cross the placenta, the fetus may develop hypothyroidism.

During breastfeeding the drug should be taken with caution, under medical supervision, is strictly at the recommended doses.

Cautions

In hypothyroidism, caused the defeat of the pituitary gland, it is necessary to determine whether there is a simultaneous failure of the adrenal cortex. In this case, substitution therapy, corticosteroids should begin before the treatment of hypothyroidism with thyroid hormone in order to avoid the development of acute adrenal insufficiency.

Overdose

Symptoms associated with hyperthyroidism: palpitations, cardiac arrhythmias, heart pain, anxiety, tremor, sleep disturbance, increased sweating, decreased appetite, weight loss, diarrhea.

Treatment: Depending on the severity of symptoms showed reduction of daily dose, treatment interruption for several days, the appointment of beta-blockers. After the disappearance of side effects of treatment should be started cautiously with lower doses.

Drug Interactions

Together, levothyroxine sodium enhances the effect of indirect anticoagulants, which may require reduction of their dose. The use of tricyclic antidepressants with levothyroxine sodium may lead to increased action of antidepressants. Thyroid hormones may increase the need for insulin and oral hypoglycemic agents (when using this combination is recommended more frequent monitoring of blood glucose, especially in the early appointment of levothyroxine sodium, as well as its dose).

Together, levothyroxine sodium reduces the effect of cardiac glycosides. While the application kolestiramin, colestipol, and aluminum hydroxide, reducing the concentration of levothyroxine sodium in the blood plasma due to inhibition of its absorption from the gastrointestinal tract.

With the simultaneous application of levothyroxine sodium with anabolic steroids, asparaginase, tamoxifen might pharmacokinetic interaction at the level of binding protein.

In an application with phenytoin, salicylates, clofibrate, furosemide in high doses increases the content of unbound to plasma proteins of levothyroxine sodium and T4.

Receiving estrogenosoderzhaschih drugs increases the content of thyroxine-binding globulin (may increase the need for levothyroxine sodium in some patients).

Growth hormone, while the application of levothyroxine sodium may speed up the closure of the epiphyseal growth zones. Acceptance of phenobarbital, carbamazepine and rifampin may increase the clearance of levothyroxine sodium (which will require increased doses).

Conditions and terms of

List B. The drug should be kept in the dark and inaccessible to children at or above 25 ° C. Shelf life - 2 years.

Bagopril

Release form, composition and packing Bagopril. 

Pill white, round, biconvex, with the inscription "GLI 2.5" on one side and company logo - on the other.

1 tab.

Enalapril Maleate 2.5 mg.

Pill white, round, biconvex, with the inscription "GLI" and the numeral "5" under it on one side and company logo - on the other.

1 tab.

Enalapril Maleate 5 mg.

Pill white, round, biconvex, scored with a cross on one side, a segment of a circle notation "G", "L", "I" and "10", on the other side - the corporate logo.

1 tab.

enalapril 10 mg.

Pill white, round, biconvex, scored with a cross on one side, a segment of a circle notation "G", "L", "I" and "20", on the other side - the corporate logo.

1 tab.

enalapril 20 mg.

Excipients: sodium starch glycolate, povidone, microcrystalline cellulose, magnesium stearate, lactose monohydrate.

Pharmacological action

Bagopril - an antihypertensive drug, its mechanism of action is associated with a decrease in formation of angiotensin I angiotensin II, decrease of which leads to a direct reduction of aldosterone release. At the same time decreases the total peripheral vascular resistance, systolic and diastolic blood pressure, fasting and preload on the myocardium.

Expands the artery to a greater extent than the vein, with a reflex increase in heart rate is not marked.

Reduces the degradation of bradykinin, increases prostaglandin synthesis.

Hypotensive effect was more pronounced at high levels of plasma renin blood than normal or reduced its level.

Blood pressure reduction in the therapeutic range has no effect on cerebral blood flow, blood flow in the vessels of the brain is maintained at a sufficient level on the background of reduced pressure.

Strengthens the coronary and renal blood flow.

With prolonged use decreases left ventricular hypertrophy and myocardial muscle cells of the arteries resistant type, prevents the progression of heart failure and slowing the development of dilatation of the left ventricle.

Improves blood flow to ischemic myocardium.

Reduces platelet aggregation.

Has some diuretic effect. Enalapril is a "prodrug": as a result of its hydrolysis formed enalaprilat, which inhibits ACE.

Time of onset of hypotensive effect when taken orally - 1 hour, reaches a maximum after 4-6 h and persists up to 24 hours. In some patients, achieving optimal blood pressure level is required therapy for several weeks.

Heart failure significant clinical effect observed with prolonged use - 6 months or more.

Pharmacokinetics

After oral administration, absorbed 60% of the drug. Food intake did not affect the absorption of enalapril. Enalapril and 50% bound to plasma proteins. Enalapril is rapidly metabolized in the liver with the formation of the active metabolite enalaprilat, which is more active ACE inhibitor than enalapril. Bioavailability 40%. The maximum concentration of enalapril in plasma is reached after 1 hour, enalaprilat - 3-4 hours. Enalaprilat easily passes through gistogematicheskie barriers, except the blood-brain, small amounts cross the placenta and breast milk. Half-life of enalaprilat about 11 hours. Enalapril is derived primarily (60%) through the kidneys (20% as enalapril and 40% as enalaprilat), through the intestines - 33% (6% as enalapril and 27% as enalaprilat). Removed during dialysis (rate 62 ml / min) and peritoneal dialysis.

Statement
Bagopril prescribed for various forms of hypertension, including renovascular hypertension.
The drug is also effective in chronic heart failure (as part of combination therapy).

Dosing regimen

Bagopril appointed interior, regardless of meal times.

In monotherapy of hypertension the initial dose - 5 mg once a day.

In the absence of clinical effect in 1-2 weeks increase the dose of 5 mg.

After receiving the initial dose, patients should be under medical supervision for 2 hours and an additional 1 hour, until it stabilizes blood pressure.

If necessary, and reasonably good tolerability, the dose may be increased to 40 mg / day for 1-2 reception. After 2-3 weeks go to the maintenance dose equal to 10 - 40 mg per day, divided into 1 -2 reception.

With moderate hypertension average daily dose is about 10 mg.

The maximum daily dose - 40 mg.

In fact, if you want to assign Bagopril patients who take diuretics, treatment with diuretics should be discontinued 2-3 days prior to the start of Bagoprila. If it is not possible, the initial dose Bagoprila should be 2.5 mg / day.

Patients with hyponatremia (sodium ion concentration in the serum of less than 130mmol / L) or with increasing concentrations of serum creatinine over 0.14 mmol / L designate Bagopril in an initial dose of 2.5 mg 1 time per day.

When renovascular hypertension the initial dose - 2,5 - 5 mg / day.

The maximum daily dose is 20 mg.

In chronic heart failure the initial dose Bagoprila - 2.5 mg dose, then increase the dose of 2,5 - 5 mg every 3-4 days according to clinical response up to maximum tolerable doses, depending on the values of blood pressure, but not exceeding 40 mg single dose or in 2 divided doses.

In patients with low systolic blood pressure (less than 110 mm Hg), therapy should begin with a dose of 1.25 mg / day.

Titration should be carried out for 2-4 weeks or when necessary and possible in the shortest possible time.

The average maintenance dose - 5 - 20 mg / day for 1 -2 reception.

Older people more often, a more pronounced hypotensive effect and prolonged time of action of enalapril, which is associated with a decrease in clearance rate of the drug, so the recommended initial dose for elderly patients - 1,25 mg / day.

In chronic renal failure, accumulation of enalapril comes with a decrease in filtering of less than 10 ml / min.

When creatinine clearance (CC) 80-30 ml / min dose of enalapril should be 5-10 mg / day, while reducing spacecraft to 10.30 ml / min - 2,5 - 5 mg / day, with CC <10>

Bagomet

Release form, composition and packing Bagomet 

Tablets, coated white, round, biconvex, with two cross-positioned risks on one side and a logo - on the other, on a break - the rough surface of white. 1 tab. metformin hydrochloride 500 mg.

Inactive ingredients: croscarmellose sodium, povidone, stearic acid, corn starch, lactose monohydrate, purified water. The composition of the shell: Opadry White YS-30-18056 (ready mix for the shell, consisting of lactose, hypromellose, titanium dioxide and triacetin in a ratio of 40:40:10:10), Opadry clear YS 1-7006 (ready mix for the shell, consisting of hypromellose and polyethylene glycol in a ratio of 90:10), purified water, sodium saccharin.

Extended release tablets, coated in blue, Valium, with Valium on one side and a logo - on the other, on a break - the rough surface of white. 1 tab. metformin hydrochloride 850 mg. Inactive ingredients: hypromellose, povidone, magnesium stearate, alcohol, lactose monohydrate, methylene chloride. The composition of the shell: Opadry White YS-30-18056 (ready mix for the shell, consisting of lactose, hypromellose, titanium dioxide and triacetin in a ratio of 40:40:10:10), Opadry clear YS 1-7006 (ready mix for the shell, consisting of hypromellose and polyethylene glycol in a ratio of 90:10), purified water, sodium saccharin, vanilla, food coloring Brilliant Blue.

Clinico-pharmacological group: oral hypoglycemic agents.

Pharmacological action

Hypoglycemic drug from biguanide group. Inhibits hepatic gluconeogenesis, decreases absorption of glucose from the intestine, enhances peripheral glucose utilization and increases tissue insulin sensitivity. In this case, has no effect on the secretion of insulin β-cells in the pancreas. Bagomet lowers triglyceride and LDL cholesterol in the blood.

Mildly anorectics effect that helps patients to diet, stabilize or reduce body weight. Improves fibrinolytic properties of blood due to suppression of plasminogen activator inhibitor type of tissue.

Pharmacokinetics

Absorption and distribution

After oral administration, metformin is absorbed from the gastrointestinal tract. Bioavailability after administration of standard dose is 50-60%. Cmax in plasma achieved 2 h after ingestion. Practically does not bind to plasma proteins. Accumulates in the salivary glands, liver and kidneys.

Breeding

Stands unchanged by the kidneys. T1 / 2 is approximately 6.5 hours

Pharmacokinetics in special clinical situations

If the kidney function is possible cumulative effect of the drug.

Statement
Type 2 diabetes patients without the propensity to ketoacidosis with the ineffectiveness of diet (especially in obese).

Dosing regimen

Set individually depending on the level of glucose in the blood. The initial dose is 0.5-1 g / day. 10-15 days may further gradual increase in the dose depending on the level of glucose in the blood. Maintenance dose is usually 1.5-2 g / day. The maximum dose - 3 g / day. To reduce the side effects on the digestive system of the daily dose should be divided into 2-3 doses.

Elderly patients recommended daily dose should not exceed 1 g.

In severe metabolic disturbances dose

Bagometa be reduced (due to an increased risk of lactic acidosis). The tablets should be taken entirely Bagometa during or immediately after the meal with a small amount of liquid (water glass).

Side effect
From the digestive system: nausea, vomiting, metallic taste, anorexia, diarrhea, flatulence, abdominal pain.
From the hemopoietic system: in some cases - megaloblastic anemia.
From the Endocrine: hypoglycemia (when used in inadequate doses) and in rare cases, lactic acidosis (requires treatment).

Allergic reactions: skin rash.

Other: long-term use - Hypovitaminosis B12 (due to malabsorption).

Contraindications
diabetic ketoacidosis;
diabetic precoma;
coma;
marked impairment of renal function;
liver function;
cardiac and respiratory failure;
acute phase of myocardial infarction;
acute cerebrovascular accident;
dehydration;
lactic acidosis (including history);
chronic alcoholism, and other conditions that might promote lactic acidosis;
major surgery and trauma (when shown an insulin);
acute alcohol poisoning;
application for at least 2 days before and within 2 days after the application of radioisotope iodine-containing drugs or X-ray;
adherence to a strict diet (less than 1000 kcal / day).
pregnancy;
Lactation (breastfeeding);
hypersensitivity to the drug.

Not recommended to prescribe the drug to people over 60 years of performing heavy physical load (due to an increased risk of lactic acidosis).

Pregnancy and lactation

The drug is contraindicated during pregnancy and lactation (breastfeeding).

Use in hepatic dysfunction

Contraindicated in marked hepatic dysfunction.

Use in renal impairment

Contraindicated in marked renal impairment.

Cautions

During the period of treatment needed to control renal function. Need to monitor lactate levels were at least 2 times a year, as well as the appearance of myalgia.

Bagometa possible to use in combination with sulfonylureas. In this case, requires particularly careful monitoring of blood glucose.

At the use of ethanol during treatment

Bagometa may develop lactic acidosis.

Overdose

Symptoms: may develop lactic acidosis with fatal consequences (for reasons of development may also include the cumulation of the drug due to renal dysfunction). The early symptoms include nausea, vomiting, diarrhea, drop in body temperature, abdominal pain in muscles and in the future possibly shortness of breath, dizziness, impaired consciousness and the development of coma.

Treatment: medication to terminate immediately, the patient should be hospitalized immediately and determine the concentration of lactate. The most effective hemodialysis. If necessary, symptomatic treatment.

Combination therapy with sulfonylureas Bagometa possible hypoglycemia.

Drug Interactions

In an application with sulfonylureas, acarbose, insulin, NSAIDs, MAO inhibitors, oxytetracycline, ACE inhibitors, derivatives of clofibrate, cyclophosphamide, beta-blockers may increase hypoglycemic action of metformin.

In an application with corticosteroids, oral contraceptives, epinephrine, sympathomimetics, glucagon, thyroid hormone drugs, thiazide and loop "diuretics, phenothiazine derivatives, derivatives of nicotinic acid may decrease hypoglycemic effect of metformin.

With the simultaneous application of cimetidine slows the excretion of metformin, which increases the risk of developing lactic acidosis. With the simultaneous application of metformin may reduce the action of anticoagulants (coumarin derivatives).

Conditions and terms of

List B. The drug should be stored in a dry place, protected from light and away from children, at up to 25 ° C. Shelf life - 2 years.