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medicalmeds.eu Medicines Angionezina II of receptors antagonist. Lozap

Lozap

Препарат Лозап. Zentiva (Зентива) Чешская Республика


Producer: Zentiva (Zentiva) Czech Republic

Code of automatic telephone exchange: C09CA01

Release form: Firm dosage forms. Tablets.

Indications to use: Stroke. Arterial hypertension. Diabetic nephropathy. Proteinuria. Chronic renal failure. Chronic heart failure.


General characteristics. Structure:

Active agent
Lozartan of potassium of 12,5 mg and 50 mg
Excipients
Kernel
Cellulose microcrystallic, Mannitolum, кросповидон, silicon dioxide colloid anhydrous, talc, magnesium stearate.
Film cover
Sepifilm 752 (white) (gipromelloza, cellulose microcrystallic, macrogoal of 2000 stearate, titanium dioxide), macrogoal 6000.

DESCRIPTION
Tablets of 12,5 mg: white or almost white, oblong, biconvex tablets, film coated.
Tablets of 50 mg: white or almost white, oblong, biconvex tablets, film coated, with risky on both sides.




Pharmacological properties:

Pharmacodynamics. Lozartan is a specific antagonist of receptors of angiotensin II (AT1 subtype). Does not suppress a kininaza of II - enzyme which catalyzes reaction of transformation of angiotensin I into angiotensin II. Reduces the general peripheric vascular resistance (GPVR), concentration in blood of adrenaline and Aldosteronum, the arterial pressure (AP), pressure in a small circle of blood circulation; reduces an afterload, renders diuretic effect. Interferes with development of a hypertrophy of a myocardium, increases tolerance to an exercise stress at patients with chronic heart failure. Lozartan does not inhibit an angiotensin-converting enzyme (APF) - a kininaza of II and, respectively, does not interfere with destruction of bradikinin therefore the side effects indirectly connected with bradikinin (for example, a Quincke's disease) arise rather seldom.
After a single dose inside hypotensive action (the ABP decreases systolic and diastolic) reaches a maximum in 6 hours, then within 24 hours gradually decreases.
The maximum hypotensive effect develops in 3-6 weeks after the beginning of administration of drug.
At patients with arterial hypertension without the accompanying diabetes mellitus with a proteinuria (more than 2 g/days), drug use authentically reduces a proteinuria, excretion of albumine and immunoglobulins G.
Stabilizes urea level in a blood plasma. Does not influence vegetative reflexes, and does not make long impact on concentration of noradrenaline in a blood plasma. Lozartan in a dose to 150 mg a day does not influence the level of triglycerides, the general cholesterol and cholesterol of lipoproteids of the high density (LPVP) in blood serum at patients with arterial hypertension. In the same dose, лозартан does not influence glucose level in blood on an empty stomach.

Pharmacokinetics. Absorption
At intake лозартан it is well soaked up, and at the same time is exposed to metabolism at "the first passing" through a liver by a carboxylation with the participation of a CYP2C9 cytochrome isoenzyme with formation of an active metabolite. System bioavailability of a lozartan - about 33%. The maximum concentration of a lozartan and its active metabolite are reached in blood serum approximately in 1 hour and in 3-4 hours after intake, respectively. Meal does not influence bioavailability of a lozartan.
Distribution
More than 99% of a lozartan and its active metabolite contact proteins of a blood plasma, generally albumine. The volume of distribution of a lozartan - 34 l. Lozartan practically does not get through a blood-brain barrier.
Metabolism
About 14% of the lozartan entered to the patient intravenously or inside turn into an active metabolite.
Removal
The plasma clearance of a lozartan makes 600 ml/min., and an active metabolite - 50 ml/min. The renal clearance of a lozartan and its active metabolite makes 74 ml/min. and 26 ml/min., respectively. At intake about 4% of the accepted dose it is removed by kidneys in not changed look and about 6% are removed by kidneys in the form of an active metabolite. The linear pharmacokinetics at intake in doses to 200 mg is inherent to Lozartan and his active metabolite.
After intake plasma concentration of a lozartan and its active metabolite decrease polieksponentsialno with a final elimination half-life of a lozartan about 2 hours, and an active metabolite - about 6-9 hours. At administration of drug in a dose of 100 mg a day лозартан, the active metabolite is kumulirut considerably in a blood plasma. Lozartan and his metabolites are brought out of an organism through intestines and kidneys. Healthy volunteers, after intake have C14 isotope of a marked lozartan, about 35% of a radioactive label are found in urine and 58% in Calais.

Pharmacokinetics at special groups of patients
Patients with alcoholic cirrhosis of easy and moderate severity had a concentration of a lozartan by 5 times, and than an active metabolite - is 1,7 times higher, than at healthy volunteers - men.
At the clearance of creatinine (CC) higher than 10 ml/min. concentration of a lozartan in a blood plasma does not differ from that at normal function of kidneys. At patients who need a hemodialysis value of the area under a curve "concentration - time" is approximately twice higher (AUC), than at patients with normal function of kidneys. лозартан, its active metabolite is removed from an organism by means of a hemodialysis.
Concentration of a lozartan and its active metabolite in a blood plasma at elderly men with arterial hypertension do not differ significantly from values of these parameters at young men with arterial hypertension.
Values of plasma concentration of a lozartan at women with arterial hypertension exceed the corresponding values at men with arterial hypertension twice. Concentration of an active metabolite at men and women do not differ. This pharmacokinetic distinction has no clinical importance.


Indications to use:

• Arterial hypertension;
• Chronic heart failure (as a part of a combination therapy, at intolerance or inefficiency of therapy by APF inhibitors);
• Decrease in risk of development of cardiovascular diseases (including a stroke) and mortality at patients with arterial hypertension and a hypertrophy of a left ventricle;
• A diabetic nephropathy at a giperkreatiniyemiya and a proteinuria (a ratio of albumine of urine and creatinine more than 300 mg/g) at patients a diabetes mellitus 2 types and the accompanying arterial hypertension (decrease in progressing of a diabetic nephropathy to a terminal chronic renal failure).


Route of administration and doses:

The drug LOZAP®prinimayut inside, regardless of meal, frequency rate of reception - 1 time a day.
At arterial hypertension the average daily dose makes 50 mg. In some cases, for achievement of bigger therapeutic effect, the dose is increased to 100 mg in two steps or once a day.
The initial dose for patients with chronic heart failure makes 12,5 mg of 1 times a day. As a rule, the dose increases with a week interval (i.e. 12,5 mg/days, 25 mg/days and 50 mg/days) to an average maintenance dose of 50 mg of 1 times a day, depending on portability of drug the patient.
At purpose of drug to the patients receiving diuretics in high doses, it is necessary to lower an initial dose of the drug LOZAP® to 25 mg (1/2 tablets on 50 mg) 1 time a day.
It is not required to adjust a dose to patients of advanced age.
Decrease in risk of development of cardiovascular diseases (including a stroke) and mortality at patients with arterial hypertension and a hypertrophy of a left ventricle: the initial dose of drug makes 50 mg a day once. Further the hydrochlorothiazide in low doses can be added and/or the drug LOZAP® dose to 100 mg a day in one or two receptions is increased.
To patients with the accompanying diabetes mellitus 2 types with a proteinuria: ЛОЗАП® appoint in an initial dose - 50 mg once a day with further increase in a dose to 100 mg/days (taking into account extent of decrease in the ABP) in one or in two steps.
The patient with liver diseases in the anamnesis, dehydration, when holding a procedure of a hemodialysis, and also to patients 75 years are more senior lower initial dose of drug - 25 mg (1/2 tablets on 50 mg) 1 time a day is recommended.

Use in pediatrics
Safety and efficiency of drug at children up to 18 years are not established.


Features of use:

It is necessary to carry out correction of dehydration to purpose of the drug LOZAP® or to begin treatment with use of drug in lower dose.
The drugs making impact on a renin-angiotenzinovuyu system can increase concentration of urea in blood and serumal creatinine at patients with a bilateral renal stenosis or a stenosis of an artery of the only kidney.
At patients with cirrhosis concentration of a lozartan in a blood plasma considerably increases in this connection in the presence of liver diseases in the anamnesis it is necessary to appoint it in lower doses.
During treatment it is regularly necessary to control potassium concentration in blood, especially at patients of advanced age, at renal failures.
Influence on ability to concentration of attention: лозартан does not influence ability to drive the car or to work with mechanisms.


Side effects:

Side effects of a lozartan usually passing also do not demand drug withdrawal. At use of a lozartan for treatment of essential hypertensia in controlled researches, among all side effects only the frequency of development of dizziness differed from placebo more, than for 1% (4,1% against 2,4%).
The Dozozavisimy orthostatic action characteristic of anti-hypertensive means, at use of a lozartan was noted less, than at 1% of patients.
The side effects observed at drug use are classified on category depending on the frequency of their emergence: very often ≥ 1/10; often> 1/100, ≤ 1/10; sometimes ≥ 1/1000, ≤ 1/100; seldom ≥ 1/10000, ≤ 1/1000; very seldom ≤ 1/10000, including separate messages.

The side effects meeting with frequency more than 1%:

General symptoms                       Lozartan (n=2085)         of Placebo (n=535) 
Adynamy, fatigue                                                       3,8 3,9
Pain in the area
thorax                                                                  1,1 2,6
Peripheral hypostases                                                      1,7 1,9
Cardiovascular system
Heartbeat                                                                   1,0 0,4
Tachycardia                                                                       1,0 1,7
Alimentary system
Abdominal pain                                                                  1,7 1,7
Diarrhea                                                                              1,9 1,9
Dispepsichesky phenomena                                                  1,1 1,5
Nausea                                                                            1,8 2,8
Musculoskeletal system
Dorsodynia, legs                                                          1,6 1,1
Spasms of gastrocnemius muscles                                              1,0 1,1
Neurology/psychiatry
Dizziness                                                                 4,1 2,4
Headache                                                                14,1 17,2
Sleeplessness                                                                        1,1 0,7
Respiratory system 
Cough, bronchitis                                                                3,1 2,6
Congestion of a nose                                                             1,3 1,1
Pharyngitis                                                                           1,5 2,6> 
Sinusitis                                                                             1,0 1,3
Infections of upper
respiratory tracts                                                           6,5 5,6

The side effects meeting with frequency less than 1%:
From cardiovascular system: orthostatic hypotension (dozozavisimy), nasal bleeding, bradycardia, arrhythmias, stenocardia, vasculitis, myocardial infarction.
From a digestive tract: anorexia, dryness of a mucous membrane of an oral cavity, dentagra, vomiting, meteorism, gastritis, lock, hepatitis, abnormal liver function.
From integuments: a xeroderma, an erythema, ecchymomas, a photosensitization, the increased sweating, an alopecia.
Allergic reactions: urticaria, skin rash, an itch, a Quincke's disease (including the hypostasis of a throat and language causing obstruction of respiratory tracts and/or a face edema, lips, a throat).
From system of a hemopoiesis: sometimes - anemia (insignificant decrease in concentration of hemoglobin and a hematocrit, on average on 0,11 g of % and 0,09 volume of %, respectively, is rare - the having clinical value), thrombocytopenia, an eosinophilia, Shenleyn-Genokh's purpura.
From a musculoskeletal system: arthralgia, arthritis, shoulder, knee pain, fibromyalgia.
From the central nervous system and sense bodys: concern, a sleep disorder, drowsiness, dysmnesias, peripheral neuropathy, paresthesias, giposteziya, a tremor, an ataxy, a depression, a faint, a ring in ears, disturbance of taste, a vision disorder, conjunctivitis, migraine.
From urinogenital system: imperative desires on an urination, infections of urinary tract, a renal failure, decrease in a libido, impotence.
Others: gout.
Laboratory indicators: often: a hyperpotassemia (potassium level in a blood plasma more than 5,5 mmol/l); sometimes - increase in level of urea and residual nitrogen or creatinine in blood serum; very seldom - moderate increase in activity of "hepatic" transaminases: aspartate aminotransferases (nuclear heating plant) and alaninaminotranspherase (ALT), hyperbilirubinemia.


Interaction with other medicines:

It can be appointed with other antihypertensives. Mutually strengthens effect of beta adrenoblockers and sympatholytics. Combined use of a lozartan with diuretics renders the additive effect.
Pharmacokinetic interactions of a lozartan with a hydrochlorothiazide, digoxin, warfarin, Cimetidinum, phenobarbital, ketokonazoly and erythromycin are noted. According to messages rifampicin and флуконазол reduce the level of an active metabolite in a blood plasma. Clinical value of these interactions is still unknown. As well as at use of other means inhibiting angiotensin II or its action, combined use of a lozartan with kaliysberegayushchy diuretics (for example, Spironolactonum, Triamterenum, amiloride), drugs of potassium and the salts containing potassium increases risk of a hyperpotassemia.
Nonsteroid protivospalitelny drugs (NPVP), including the selection inhibitors of cyclooxygenase-2 (TsOG-2), can reduce effect of diuretics and other antihypertensives.
At combined use of antagonists of receptors of angiotensin II and lithium increase in concentration of lithium in a blood plasma is possible. Considering it, it is necessary to weigh advantage and risk of combined use of a lozartan with lithium salts. If it is necessary to use drugs jointly, it is regularly necessary to control concentration of lithium in a blood plasma.


Contraindications:

• Hypersensitivity to drug components;
• Pregnancy and period of a lactation;
• Age up to 18 years (efficiency and safety are not established).
With care: arterial hypotension, reduced volume of the circulating blood, disturbances of water and electrolytic balance, a bilateral stenosis of renal arteries or a stenosis of an artery of the only kidney, a renal/liver failure.

Pregnancy and period of a lactation
There are no data on use of a lozartan at pregnancy. However, it is known that, the drugs influencing directly renin-angiotensin-aldosteronovuyu system at use in II and III trimesters of pregnancy, can cause defects of development or even death of the developing fruit. Therefore at pregnancy emergence administration of drug ЛОЗАП® should be stopped immediately. At appointment in the period of a lactation it is necessary to make the decision on the termination of breastfeeding or on the treatment termination by the drug LOZAP®.


Overdose:

Symptoms: the expressed decrease in the ABP, tachycardia, because of parasympathetic (vagal) stimulation can develop bradycardia.
Treatment: artificial diuresis, symptomatic therapy; the hemodialysis is not effective.


Storage conditions:

List B. To store at a temperature not above 30 °C. To store in the place, unavailable to children! Period of validity 2 years. Drug cannot be used after the expiry date specified on packaging.


Issue conditions:

According to the recipe


Packaging:

Tablets film coated on 12,5 mg and 50 mg.
On 10 tablets in the blister from PVH/PVDH/Al or Al/Al. On 3,6 or 9 blisters together with the application instruction are placed in a cardboard pack.



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