Lozartan

Lozartan – drug with anti-hypertensive action.

Form of release and structure

Lozartan release in the form of tablets, film coated: round, biconvex, the small roughness of a surface is admissible; on a break – white with a yellowish shade or white; 12,5 and 25 mg – white with a grayish shade or white color, 50 mg – pink color, 100 mg – yellow color (in blisters on 10 pieces, on 3 blisters in a cardboard pack; in blisters on 15 pieces, on 2, 4, 6 blisters in a cardboard pack; in blister strip packagings on 10, 30 pieces, on 1-6, 10 packagings in a cardboard pack; in blister strip packagings on 20 pieces, on 1, 3 packagings in a cardboard pack; in blister strip packagings on 7 pieces, on 1-4 packagings in a cardboard pack; in banks (jars) on 10, 20, 30,40, 50, 60, 100 pieces, after 1 bank in a cardboard pack).

Is a part of 1 tablet:

• Active agent: лозартан potassium – 12,5 mg, 25 mg, 50 mg or 100 mg;
• Excipients (tablets on 12,5/25/50/100 mg respectively): monohydrate of lactose (milk sugar) – 114,63/149,5/270,6/115 mg, microcrystallic cellulose – 5,72/12,24/26,6/40 mg, croscarmellose sodium (primelloza) – 4,29/9,18/15,2/11,2 mg, colloid silicon dioxide (aerosil) – 1,43/2,04/3,8/2 mg, povidone (low-molecular polyvinylpirrolidone) – 0/0/0/9 mg, magnesium stearate – 1,43/2,04/3,8/2,8 mg.

Structure of a cover:

• 12,5 and 25 mg (respectively): Opadry II white (polyvinyl alcohol (E1203) – 40%, titanium dioxide (E171) – 25%, polyethyleneglycol (macrogoal) (E1521) – 20,2%, talc (E553b) – 14,8%) – 2,983/3,975 mg, an emulsion of a simetikon of 30% (water – 50-69,5%, dimethyl silicone – 25,5-33%, polyethyleneglycol sorbitan tristearate – 3-7%, methyl cellulose – 1-5%, silica gel – 1-5%) – 0,017/0,025 mg;
• 50 mg: Opadry II pink (polyvinyl alcohol (E1203) – 40%, titanium dioxide (E171) – 24,18%, talc (E553b) – 14,8%, polyethyleneglycol (macrogoal) (E1521) – 20,2%, dye a carmine red (E120) – 0,54%, an aluminum varnish on the basis of dye of red charming (E129) – 0,08%, an aluminum varnish on the basis of dye a sunset yellow (E110) – 0,15%, an aluminum varnish on the basis of dye of quinolinic yellow (E104) – 0,05%) – 9,923 mg, an emulsion of a simetikon of 30% (water – 50-69,5%, polyethyleneglycol sorbitan tristearate – 3-7%, dimethyl silicone – 25,5-33%, methyl cellulose – 1-5%, silica gel – 1-5%) – 0,077 mg;
• 100 mg: (a gipromelloza – 4,8 mg, talc – 1,6 mg, titanium dioxide – 0,826 mg, polyethyleneglycol 4000 (a macrogoal 4000) – 0,72 mg, ferrous oxide yellow (ferrous oxide) – 0,054 mg) or (dry mix for a film covering with contents: a gipromelloza – 60%, talc – 20%, titanium dioxide – 10,33%, a macrogoal 4000 (polyethyleneglycol 4000) – 9%, yellow iron oxide (ferrous oxide) – 0,67%) – 8 mg.

Indications to use

• Arterial hypertension;
• Protection of kidneys at a diabetes mellitus 2 types with a proteinuria (action is shown by delay of progressing of a renal failure, namely decrease in frequency of development of a giperkreatininemiya, proteinuria, end-stage of the chronic renal failure (demanding performing transplantation of a kidney or a hemodialysis), rates of mortality);
• Decrease in risk of the associated cardiovascular incidence and mortality at arterial hypertension and a hypertrophy of a left ventricle (action is shown by decrease in cumulative frequency of a stroke, cardiovascular mortality and a myocardial infarction);
• Chronic heart failure in case of inefficiency of performing treatment by inhibitors of an angiotensin-converting enzyme.

Contraindications

Absolute:

• Heavy liver failure (due to the lack of experience of use);
• Refractory hyperpotassemia;
• Dehydration;
• Deficit of lactase, lactose intolerance and syndrome of glyukozo-galaktozny malabsorption;
• Simultaneous use with aliskireny for patients with a diabetes mellitus and/or with functional disturbances of kidneys (at a glomerular filtration rate it is less than 60 ml in a minute);
• Pregnancy and period of a lactation;
• Age up to 18 years;
• Hypersensitivity to drug components.

Relative (diseases/states at which Lozartan it is necessary to apply with care):

• Renal failure;
• Disturbances of water and electrolytic balance;
• Liver failure (it is less than 9 points on Chayld-Pyyu);
• Coronary heart disease;
• Arterial hypotension;
• The reduced volume of the circulating blood;
• Hyperpotassemia;
• Stenosis of an artery of the only kidney or bilateral stenosis of renal arteries;
• States after transplantation of a kidney;
• Mitral and aortal stenosis;
• Subaortic hypertrophic stenosis;
• Heavy heart failure (the IV functional class on NYHA classification), a Quincke's disease in the anamnesis;
• The heart failure which is followed by life-threatening arrhythmias;
• The heart failure which is followed by a heavy renal failure;
• Primary aldosteronism;
• Cerebrovascular diseases.

Route of administration and dosage

Lozartan accept inside, irrespective of meal time.

Drug can be used in the form of monotherapy or along with other hypotensive medicines.

If there are no other appointments, the daily dose is accepted in 1 reception.

In most cases at arterial hypertension the standard initial and supporting daily dose make 50 mg. As a rule, the maximum anti-hypertensive effect is reached in 3-6 weeks from the moment of the beginning of therapy. At some patients for achievement of bigger effect increase in a dose to maximum – 100 mg a day is possible.

At the reduced volume of the circulating blood (for example, at reception of high doses of diuretics) Lozartan begin to accept with a dose in 25 mg a day.

Elderly patients have no need for individual selection of an initial dose and at a renal failure, including the patients who are on dialysis.

At a liver failure (it is less than 9 points on a scale of Chayld-Pyyu) when holding a procedure of a hemodialysis, and also patients of 75 years are recommended to appoint drug in lower initial daily dose – 25 mg.

The standard daily initial dose of Lozartan for decrease in risk of the associated cardiovascular incidence and mortality at patients with a hypertrophy of a left ventricle and arterial hypertension makes 50 mg. Further increase in a dose of drug twice (in 1 or 2 receptions depending on extent of lowering of arterial pressure) or addition of a hydrochlorothiazide is recommended.

The standard initial daily dose of Lozartan for protection of kidneys at patients with a diabetes mellitus 2 types with a proteinuria makes 50 mg. Further depending on extent of lowering of arterial pressure increase in a dose of drug is recommended twice. Lozartan it is possible to apply along with other hypotensive medicines (alpha and beta adrenoblockers, diuretics, hypotensive drugs of the central action, blockers of "slow" calcium channels), insulin and other hypoglycemic drugs (inhibitors of glucosidase, a glitazonama and derivatives of sulphonylurea).

At chronic heart failure the initial daily dose of Lozartan makes 12,5 mg. Usually the dose is titrated with a week interval to a usual maintenance dose – 50 mg once a day (depending on individual portability).

Side effects

Lozartan is, as a rule, had well, side effects have passing and slight character and cancellations of therapy do not demand.

At use of drug the disturbances from some systems of an organism which are shown with various frequency can develop (> 1% – is frequent; <1% – редко):

• Alimentary system: often – an abdominal pain, dyspepsia, diarrhea, nausea; seldom – dryness of a mucous membrane of an oral cavity, anorexia, a meteorism, a dentagra, gastritis, a lock, abnormal liver functions, hepatitis, vomiting;
• Cardiovascular system: often – a heart consciousness, tachycardia; seldom – stenocardia, symptomatic arterial hypotension (especially at patients with intravascular dehydration, for example, at heavy heart failure or at reception of high doses of diuretics), dozozavisimy orthostatic hypotension, bradycardia, a myocardial infarction, arrhythmias, a vasculitis;
• Central nervous system and sense bodys: often – a headache, dizziness, sleeplessness; seldom – concern, a sleep disorder, memory disturbance, drowsiness, peripheral neuropathy, giposteziya, paresthesias, a tremor, a depression, an ataxy, a faint, conjunctivitis, disturbances of taste and sight, a ring in ears, migraine;
• Urinary system: seldom – infections of urinary tract, imperative desires on an urination, functional disturbances of kidneys;
• Respiratory system: often – cough, a rhinedema, bronchitis, sinusitis, pharyngitis, infections of upper parts of respiratory tracts;
• System of a hemopoiesis: seldom – anemia, an eosinophilia, thrombocytopenia, Shenleyna-Genokh's purpura;
• Reproductive system: seldom – impotence, decrease in a libido;
• Musculoskeletal system: often – muscular spasms, an onychalgia and to back; seldom – arthritis, an arthralgia, knee and shoulder pain, fibromyalgia;
• Integuments: seldom – the increased sweating, a xeroderma, an erythema, ecchymomas, a photosensitization, an alopecia;
• Allergic reactions: seldom – skin rash, a small tortoiseshell, an itch, a Quincke's disease (including the hypostasis of a voice fold and a throat causing obstruction of respiratory tracts, and/or hypostasis of lips, faces, language and/or a throat);
• General disturbances: often – peripheral hypostases, an adynamy, increased fatigue, weakness, pain in a thorax;
• Others: seldom – nasal bleeding, an aggravation of a course of gout.

Development of disturbances from laboratory indicators is also possible:> 1% and 0,1% and <1% – увеличение концентрации остаточного азота, мочевины, креатинина в сыворотке крови; <0,01% – умеренное увеличение активности трансаминаз (аланинаминотрансферазы, аспартатаминотрансферазы), гипербилирубинемия.

At development or aggravation of the specified side effects, and also at development of uncharacteristic symptoms it is necessary to see a doctor.

Special instructions

In rare instances at Lozartan's use disturbances in the form of anaphylactic reactions, the Quincke's disease with involvement of a throat and throat causing obstruction of respiratory tracts, and/or a face edema, lips, language and/or a throat develop. Therefore in the presence of instructions on a Quincke's disease in the anamnesis drug needs to be accepted with extra care.

At patients with a reduced volume of the circulating blood (for example, the diuretics receiving high doses) symptomatic arterial hypotension can develop. It is necessary to carry out correction of these states before Lozartan's appointment or to begin therapy with reception of lower doses.

Disturbances of water and electrolytic balance are characteristic of patients with a renal failure against the background of a diabetes mellitus 2 types, or without it. At Lozartan's appointment this category of patients needs to observe extra care because of risk of development of a hyperpotassemia.

During therapy it is regularly necessary to control the content of potassium in blood, in particular at elderly patients and at functional disturbances of kidneys. Without preliminary approval of the doctor it is not necessary to accept drugs of potassium or substitutes of salt with the content of potassium.

In the presence of instructions on liver diseases in the anamnesis Lozartan it is necessary to accept in lower doses that is connected with increase in concentration of drug in a blood plasma.

During therapy it is regularly necessary to control concentration of creatinine in blood serum at regular intervals.

It is necessary to be careful at control of motor transport and performance of other potentially dangerous works demanding the increased concentration of attention and bystry psychomotor reactions because of possible development of dizziness, in particular at the patients who were accepting diuretic drugs and passed to therapy by Lozartan.

Medicinal interaction

At simultaneous use of Lozartan with some medicines there can be following effects:

• Rifampicin, флуконазол: reduction of level of an active metabolite;
• Kaliysberegayushchy diuretics (for example, Spironolactonum, amiloride, Triamterenum, эплеренон) or the drugs promoting increase in content of potassium (for example, heparin), potassium additives and salts with the content of potassium: increase in content of potassium in blood serum;
• Lithium drugs: decrease in excretion of sodium and increase in serumal concentration of lithium (it is necessary to carry out control of its serumal concentration);
• Non-steroidal anti-inflammatory drugs, including the selection inhibitors of cyclooxygenase-2: decrease in anti-hypertensive effect; at patients with functional disturbances of the kidneys receiving treatment of NPVP, perhaps further deterioration in function of kidneys;
• Other antihypertensives: increase in expressiveness of anti-hypertensive action;
• The drugs reducing arterial pressure (for example, tricyclic antidepressants, neuroleptics, Baclofenum, амифостин): increase in risk of development of arterial hypotension;
• The medicines influencing renin-angiotensin-aldosteronovuyu system: increase in risk of development of arterial hypotension, a hyperpotassemia, a syncope and renal failures (including an acute renal failure); it is necessary to carry out careful control of arterial pressure, water and electrolytic balance and function of kidneys.

Lozartan it is possible to apply along with other hypotensive drugs.

Combined use with aliskireny is not recommended to patients with a diabetes mellitus and a renal failure (at a glomerular filtration rate it is less than 60 ml in a minute).

Terms and storage conditions

To store in protected from light, the place, unavailable to children, at a temperature up to 25 °C.

Period of validity – 3 years.