Lozap

Lozap – the medicine having hypotensive effect.

Form of release and structure

Lozap release in the form of tablets, film coated: oblong, biconvex, almost white or white color; on 50 and 100 mg – with risky from two parties (on 10 pieces in blisters, on 3, 6 or 9 blisters in a cardboard pack; on 15 pieces in blisters, on 2, 4 or 6 blisters in a cardboard pack).

Is a part of 1 tablet:

• Active ingredient: лозартан potassium – 12,5 mg, 50 mg or 100 mg;
• Auxiliary components (12,5/50/100 mg respectively): microcrystallic cellulose – 52,5/80/160 mg, Mannitolum — 25/50/100 mg, кросповидон — 5/10/20 of mg, colloid anhydrous dioxide of silicon – 1/2/4 mg, talc – 2/4/8 mg, magnesium stearate – 2/4/8 mg;
• Film cover (12,5/50/100 mg respectively): white сепифилм 752 (a gipromelloza, microcrystallic cellulose, stearate of a macrogoal 2000, titanium dioxide) – 4,95/7,9/13,8 mg, a macrogoal 6000 – 0,05/0,1/0,2 mg.

Indications to use

• Arterial hypertension;
• Chronic heart failure (along with other drugs at inefficiency or intolerance of use of inhibitors of an angiotensin-converting enzyme);
• Decrease in risk of development of cardiovascular diseases (including a stroke) and mortality at patients with a hypertrophy of a left ventricle and arterial hypertension;
• Diabetic nephropathy at a proteinuria and a giperkreatininemiya (a ratio of albumine of urine and creatinine more than 300 mg/g) at a diabetes mellitus 2 types and the accompanying arterial hypertension (decrease in progressing of a diabetic nephropathy to an end-stage of a chronic renal failure).

Contraindications

Absolute:

• Functional disturbances of a liver in heavy degree (due to the lack of experience of use for patients with values it is more than 9 points on a scale of Chayld-Pyyu);
• The combined use with aliskireny against the background of a diabetes mellitus and at a renal failure (at clearance of creatinine it is less than 60 ml in a minute);
• Pregnancy and period of a lactation;
• Age up to 18 years (safety and efficiency of action of Lozap for this age group of patients are not established);
• Hypersensitivity to drug components.

Relative (Lozap appoint in care in the presence of the following diseases / states):

• Heart failure with the accompanying heavy renal failure;
• Arterial hypotension;
• Heavy chronic heart failure of the IV functional class on NYHA classification;
• Coronary heart disease;
• Heart failure with life-threatening arrhythmias;
• Hyperpotassemia;
• Cerebrovascular diseases;
• Disturbances of water and electrolytic balance, the reduced volume of the circulating blood, a stenosis of an artery of the only kidney or a bilateral stenosis of renal arteries;
• Liver and/or renal failure;
• States after transplantation of a kidney (due to the lack of experience of use);
• Primary hyper aldosteronism;
• Mitral and aortal stenosis;
• Quincke's disease (anamnestic data);
• Hypertrophic subaortic stenosis;
• Belonging to negroid race;
• Age of 75 years.

Route of administration and dosage

Lozap it is necessary to accept inside once a day, does not accord meal on efficiency of drug of influence.

The recommended mode of dosing (daily dose):

• Arterial hypertension: 50 mg once a day. To achieve bigger therapeutic effect increase in a single dose twice (100 mg in 1 reception) or frequency rates of reception in certain cases is possible (2 times a day on 50 mg);
• Chronic heart failure: 12,5 mg once a day. Usually daily dose with a week interval (is defined by portability of drug) is increased twice to average supporting – 50 mg.

The patient receiving high doses of diuretics Lozap appoint in a reduced dose (25 mg once a day).

To patients of advanced age to adjust a dose there is no need.

The initial daily dose at Lozap's appointment for decrease in risk of development of cardiovascular diseases (including a stroke) and mortality at arterial hypertension and a hypertrophy of a left ventricle makes 50 mg. Afterwards the dose can be increased to 100 mg a day in 1-2 receptions, or along with an initial dose of Lozap low doses of a hydrochlorothiazide can be appointed.

Initial dose against the background of the accompanying diabetes mellitus 2 types with a proteinuria – 50 mg once a day, afterwards, considering extent of lowering of arterial pressure, the daily dose is increased twice (frequency rate of reception – 1-2 times a day).

In the presence of instructions in the anamnesis on a liver disease, and also to patients of 75 years, with dehydration and when carrying out a hemodialysis it is recommended to appoint lower initial doses – on 25 mg once a day.

Side effects

The side effects developing in therapy time usually have passing character and Lozap's cancellations do not demand.

The orthostatic dozozavisimy action characteristic of this group of drugs, during Lozap's reception was noted less than at 1% of patients.

The disturbances developing in therapy time (> 10% – are very frequent;> 1% and <10% – is frequent;> 0,1% and <1% – infrequently;> 0,01% and <0,1% – are rare; <0,01% taking into account separate messages – are very rare; at impossibility to estimate emergence frequency – with an unknown frequency), depend on indications.

Arterial hypertension:

• Nervous system: often – dizziness; infrequently – drowsiness, a headache, sleep disorders;
• Cardiovascular system: infrequently – stenocardia, a heart consciousness, orthostatic hypotension;
• Hearing and labyrinth disturbances: infrequently – вертиго;
• Alimentary system: infrequently – abdominal pains, intestinal impassability;
• Hypodermic fabrics and skin: infrequently – rash;
• Tool and laboratory researches: often – a hyperpotassemia; seldom – increase in activity of alaninaminotranspherase;
• General frustration: infrequently – an adynamy, weakness, hypostases.

Arterial hypertension and hypertrophy of a left ventricle:

• Nervous system: often – dizziness;
• Hearing and labyrinth disturbances: often – вертиго;
• General frustration: often – an adynamy, weakness.

Chronic heart failure:

• Lymphatic system and blood: often – anemia;
• Nervous system: often – dizziness; infrequently – a headache; seldom – migraine;
• Cardiovascular system: often – orthostatic hypotension; seldom – faints, a ciliary arrhythmia, an acute disorder of cerebral circulation;
• Respiratory system, thorax and mediastinum: infrequently – cough, short wind;
• Alimentary system: infrequently – diarrhea, vomiting, nausea;
• Hypodermic fabrics and skin: infrequently – a skin itch, a small tortoiseshell, rash;
• Connecting and skeletal muscular tissue: infrequently – muscular spasms;
• Urinary tract and kidneys: often – functional disturbances of kidneys, a renal failure;
• Tool and laboratory researches: often – increase in concentration of urea, creatinine and potassium in a blood plasma; infrequently – a hyperpotassemia;
• General frustration: infrequently – an adynamy, weakness.

Arterial hypertension and diabetes mellitus 2 types with functional disturbances of kidneys:

• Nervous system: often – dizziness;
• Cardiovascular system: often – orthostatic hypotension;
• Tool and laboratory researches: often – a hyperpotassemia, a hypoglycemia;
• General frustration: often – an adynamy, weakness.

Post-registration observations:

• Lymphatic system and blood: with an unknown frequency – anemia, thrombocytopenia;
• Immune system: seldom – a vasculitis, anaphylactic reactions, allergic reactions, a Quincke's edema;
• Mentality: with an unknown frequency – a depression;
• Nervous system: with an unknown frequency – migraine, taste disturbances;
• Hearing and labyrinth disturbances: with an unknown frequency – вертиго;
• Respiratory system, thorax and mediastinum: with an unknown frequency – cough;
• Alimentary system: with an unknown frequency – diarrhea;
• Biliary tract and liver: seldom – hepatitis; with an unknown frequency – pancreatitis, abnormal liver functions;
• Hypodermic fabrics and skin: with an unknown frequency – a skin itch, a photosensitization, a small tortoiseshell, rash;
• Connecting and skeletal muscular tissue: with an unknown frequency – an arthralgia, a mialgiya, рабдомиолиз;
• Mammary glands and generative organs: with an unknown frequency – impotence and/or erectile dysfunction;
• Tool and laboratory researches: with an unknown frequency – a hyponatremia;
• General frustration: with an unknown frequency – hypostases, an indisposition.

Dorsodynias, grippopodobny symptoms and infections of uric ways arose at the patients receiving Lozap than at the receiving placebos of patients more often.

At patients from risk group functional disturbances of kidneys were noted, including an acute renal failure (at timely cancellation of therapy of disturbance have reversible character).

Special instructions

Patients with anamnestic instructions on a Quincke's edema (hypostasis of lips, faces, drinks and/or language) need strict medical observation.

At the hypovolemia and/or a hyponatremia connected with reception of high doses of diuretics, diarrhea, vomiting, observance of a diet with the low content of table salt after Lozap's reception development of arterial hypotension and disturbances of water and electrolytic balance is possible. Prior to therapy it is necessary to carry out correction of these states. If it was not made, it is necessary to appoint lower doses of drug.

Water and electrolytic disturbances are characteristic of patients with functional disturbances of kidneys against the background of a diabetes mellitus or without it and demand correction. Such patients need constant control of contents in a blood plasma of potassium and indicators of clearance of creatinine (in particular strict observation is necessary for patients with heart failure and clearance of creatinine within 30-50 ml a minute).

Simultaneous use of Lozap with kaliysberegayushchy diuretics, drugs of potassium and kaliysoderzhashchy solezamenitel is not recommended.

At functional disturbances of a liver (it is more than 9 points on a scale of Chayld-Pyyu) in the anamnesis it is necessary to appoint Lozap in lower doses. Patients do not have data on purpose of therapy with a heavy liver failure (Lozap's reception is contraindicated to this group of patients).

Because of inhibition the system renin-angiotensin-aldosteronovoy (SRAA) during therapy cases of development of functional disturbances of kidneys were noted, up to a renal failure (in particular it is characteristic of patients at whom function of kidneys depends on RAAS, for example, against the background of already available renal failure and heavy heart failure). At a bilateral stenosis of renal arteries or a stenosis of an artery of the only kidney increase in concentration of creatinine and urea in a blood plasma was noted. At treatment cancellation these changes can take place. Patients at Lozap's appointment need to be careful with a stenosis of an artery of the only kidney or a bilateral stenosis of renal arteries.

Too expressed lowering of arterial pressure at patients with cerebrovascular diseases and coronary heart disease can lead to an ischemic stroke or a myocardial infarction.

At the heart failure which is followed by a renal failure or without it there is a probability of development of an acute renal failure and heavy arterial hypotonia (due to the lack of experience of use of drug for this category of patients at Lozap's appointment it is necessary to be careful).

At a combination therapy with inhibitors of an angiotensin-converting enzyme increase in risk of development of side effects, in particular a hyperpotassemia and functional disturbances of kidneys is possible (careful observation and control of laboratory indicators is necessary).

The patients who are on a hemodialysis should control carefully arterial pressure and to adjust a drug dose.

There are no data on Lozap's use for the patients who recently transferred renal transplantation.

When carrying out surgical interventions and the general anesthesia because of blockade of RAAS development of arterial hypotension is possible. Development of heavy arterial hypotension is seldom or never possible that demands intravenous administration of angiotonic medicines and/or liquid.

At purpose of therapy at a hypertrophic subaortic stenosis or hemodynamically significant stenosis of the mitral or aortal valve it is necessary to be careful.

With primary hyper aldosteronism it is not recommended to patients to accept Lozap as they usually show resistance to therapy by the hypotensive drugs influencing RAAS.

Aged from 75 years therapy it is recommended to patient to begin 25 mg with a daily dose.

At the patients belonging to negroid race, Lozap reduces arterial pressure less effectively, than at representatives of other races (possibly, because of low activity of a renin).

During Lozap's use drowsiness, dizziness and unconscious states can be observed that patients need to consider at control of motor transport and performance of potentially dangerous types of the works demanding bystry psychomotor reactions and the increased concentration of attention.

Medicinal interaction

Simultaneous use of Lozap with aliskireny at patients with a renal failure (at clearance of creatinine <60 ml a minute), and also at a diabetes mellitus is contraindicated.

Carrying out a combination therapy with other hypotensive drugs is possible.

The combined therapy with inhibitor of an angiotensin-converting enzyme has to be limited to exceptional cases according to individual indications. It needs to be seen off at strict monitoring of function of kidneys. As a result of conduct of clinical trials it was established that at the confirmed atherosclerosis, heart failure or a diabetes mellitus with damage of target organs joint purpose of drugs increases risk of development of unconscious states, arterial hypotension, a renal failure and a hyperpotassemia in comparison with use of RAAS inhibitors separately.

Pharmacokinetic interactions with warfarin, a hydrochlorothiazide, digoxin, Cimetidinum, ketokonazoly, phenobarbital, erythromycin are noted.

At joint appointment of Lozap with some drugs there can be following effects:

• Sympatholytics, β-adrenoblockers:::::::::: mutual strengthening of effect;
• Diuretics: development of the additive effect;
• Other drugs capable to cause development of arterial hypotension as undesirable reaction (амифостин, Baclofenum, antipsychotic drugs, tricyclic antidepressants): increase in risk of development of arterial hypotension;
• Kaliysberegayushchy diuretics (amiloride, Triamterenum, Spironolactonum and its derivative эплеренон), potassium drugs, salt substitutes with the content of potassium, other means which can increase the content of potassium in a blood plasma: development of a hyperpotassemia;
• Non-steroidal anti-inflammatory drugs, including the selection TsOG-2 inhibitors: easing of hypotensive effect;
• Non-steroidal anti-inflammatory drugs: increase in risk of emergence of renal failures, including a hyperpotassemia and an acute renal failure, in particular at patients with already available renal failure (the combination is appointed with care, in particular to elderly patients; patients have to receive liquid in adequate quantity and be under medical observation along with monitoring procedure of indicators of function of kidneys).

Terms and storage conditions

To store in the place, dry, unavailable to children, at a temperature up to 30 °C.

Period of validity – 2 years.