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Hepatoprotective agent also has choleretic, cholelitolitic, lipid-lowering, cholesterol-lowering and immunomodulatory effects. It stabilizes hepatocyte membrane and cholangiocytes has a direct cytoprotective effect. As a result of the drug in the gastrointestinal circulation of bile acids content decreases hydrophobic (potentially toxic) acids. By reducing cholesterol absorption in the intestine and other biochemical effects having hypocholesterolemic action. Suppresses testosterone suspension reviews cell death caused by toxic bile acids.

With its high polar properties, ursodeoxycholic acid (UDCA) forms a non-toxic mixed micelles with apolar (toxic) bile acids, which reduces the ability of gastric reflyuktata damage cell membranes with biliary reflux gastritis and reflux esophagitis. In addition, UDCA forms double molecules that can be included in the composition of cell membranes, stabilize them and make immune to the effects of cytotoxic micelles. It reduces the saturation of bile cholesterol by inhibiting its absorption in the intestine, suppression of the synthesis in the liver and decrease secretion in the bile; increases the solubility of cholesterol in bile, forming with it the liquid crystals; It reduces the lithogenic index of bile. The result is the dissolution of cholesterol gallstones (a consequence of changes in the ratio of cholesterol / bile acids in bile) and preventing the formation of new stones (the result of reducing the content of cholesterol in bile). Induces cholepoiesis rich in bicarbonate, which leads to an increase in bile passages and stimulates the excretion of toxic bile acids through the intestine.

Immunomodulatory effect due to inhibition of the expression of HLA-antigens. (HLA – human leucocyte antigens – antigens histocompatibility) in the membranes of hepatocytes and cholangiocytes, normalization of natural killer activity of lymphocytes, etc. Significantly delay the progression of fibrosis in patients with primary biliary cirrhosis, cystic fibrosis and alcoholic steatohepatitis, reduces the risk of development of esophageal varices.

Pharmacokinetics :

Absorption and distribution.
UDCA in the jejunum absorbed by passive diffusion, and from the ileum by an active transport. It penetrates through the placental barrier. The concentration in plasma when administered 500 mg achieved after 30, 60, 90 min – 3.8, 5.5, 3.7 mmol / l, respectively. Distribution UDCA is characterized by a high degree of binding to plasma proteins, which may be 96-99%.

Metabolism and excretion.
As a result of the elimination of UDCA presistemna formed taurine and glycine conjugates, which are secreted into bile. Approximately 50-70% of the UDCA dose administered is excreted in the bile. The remainder of UDCA nevsosavsheysya fraction falls into the colon, where it undergoes bacterial cleavage (7-dehydroxylation) to give lithocholic acid. Lithocholic acid is partially absorbed from the gut, biotransformed in the liver and sulfolitoholilglitsinovy sulfolitoholiltaurinovy conjugates and excreted.

Indications for use:

 

  • Primary biliary cirrhosis in the absence of signs of decompensation (symptomatic therapy);
  • Dissolution of small and medium cholesterol stones in the gall bladder functioning;
  • Biliary reflux gastritis and reflux esophagitis;
  • Chronic hepatitis of various genesis;
  • Alcoholic liver disease;
  • Nonalcoholic steatohepatitis;
  • Primary sclerosing cholangitis;
  • Cystic fibrosis (cystic fibrosis);
  • Biliary dyskinesia;

Contraindications:

 

  • Increased individual sensitivity to the drug;
  • rentgenopolozhitelnye (high in calcium) gallstones;
  • non-functioning gall bladder;
  • acute inflammatory diseases of the gallbladder, bile ducts and intestines;
  • cirrhosis of the liver in the stage of decompensation;
  • expressed by the human kidney, liver, pancreas;
  • lactose intolerance;
  • lactase deficiency or glucose-galactose malabsorption;
  • Children up to age 3 years.

With caution used in children aged 3 to 4 years, as possible difficulty in swallowing tablets, although ursodeoxycholic acid has no age restrictions apply.

Pregnancy and lactation:

The use of ursodeoxycholic acid during pregnancy is possible only when the expected benefit to the mother outweighs the potential risk to the fetus (adequate well-controlled studies of ursodeoxycholic acid in pregnant women has not been).

Data on the allocation of ursodeoxycholic acid in breast milk are not currently available. If necessary, the use of ursodeoxycholic acid during lactation should decide the issue of termination of breastfeeding.

Dosage and administration:

The tablets of the drug testosterone suspension reviews is taken orally without chewing, drinking plenty of water. The tablet can be divided in half.

For the dissolution of cholesterol gallstones average daily dose of the drug . The drug is taken in the evening before bedtime. The course of treatment – 6-12 months.To prevent the recurrence of stones is recommended taking the drug for a few months after the dissolution of stones.

Symptomatic treatment of primary biliary cirrhosis: an average daily dose – 10-15 mg / kg (if necessary – up to 20 mg / kg) from 6 months to several years. The drug is taken with food, drinking plenty of fluids.

When biliary reflux gastritis and reflux esophagitis , the dose is 10 mg / kg / day – 1 time a day at bedtime. The course of treatment – from 10-14 days to 6 months, if necessary – up to 2 years.

In chronic hepatitis of various genesis (toxic, drugs, etc..), The primary nealkogolnom steatohepatitis, alcoholic liver disease , the mean daily dose is 10-15 mg / kg body weight in 2-3 hours.The duration of therapy is 6-12 months or more.

Side effect:

The calcination gallstones, increased activity of “liver” enzymes, allergic reactions (including urticaria), diarrhea, nausea, abdominal pain; in the treatment of primary biliary cirrhosis may be a transient decompensation of cirrhosis of the liver, passing after discontinuation of the drug.

Overdose:

Cases of UDCA overdose are not known. Interaction with other drugs:

Interaction with other drugs

Do not use the drug at the same time with antacids containing aluminum and ion-exchange resins, as these drugs may interfere with the absorption of ursodeoxycholic acid.

With simultaneous use of lipid-lowering medications, estrogens, progestogens, or neomycin (oral contraceptives) increase the saturation of bile with cholesterol and may reduce the ability of ursodeoxycholic acid to dissolve cholesterol gallstones.

Ursodeoxycholic acid can enhance cyclosporine absorption from the intestine, which requires monitoring of cyclosporin blood concentration, and if necessary – its correct dosing regimen.

Special instructions:

The successful dissolution requires that the stones were pure cholesterol, no larger than 15-20 mm, gallbladder filled with stones not more than half of the bile duct and retain their function.

When assigning to dissolve gallstones need to control the activity of “liver” transaminases and alkaline phosphatase, gamma-glutamyl, bilirubin concentrations. While maintaining high performance drug should be discontinued.

Holetsistografii should be performed every 4 weeks during the first 3 months of treatment in the future – every 3 months. Monitoring the effectiveness of the treatment carried out every 6 months during the ultrasound examination in the first year of therapy. After completely dissolving concrements encouraged to continue in use for at least three months, in order to facilitate the dissolution of calculi residues that are too small to be detected.

If within 6-12 months testosterone suspension reviews after initiation of therapy partial dissolution of stones did not happen, it is unlikely that treatment will be effective.

Detection during treatment nevizualiziruemaya gallbladder is a testament to the fact that the complete dissolution of the stones did not happen, and the treatment should be discontinued.

When calcified gallstones violation contractility of the gall bladder or frequent attacks of biliary colic treatment should be discontinued.

Effects on ability to drive and perform work that requires high concentration and speed of psychomotor reactions:
No data are available on the effect of UDCA on the ability to drive and use machines.

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testosterone suspension gains

The drug blocks the peripheral units of the cough reflex due to the following effects:

  • a local anesthetic effect, which reduces the excitability of peripheral sensory (cough) testosterone suspension gains respiratory tract receptors;
  • bronchodilator actions, through which there is suppression of the stretch receptors involved in the cough reflex;
  • a slight decrease in activity of the respiratory center (without respiratory depression)

Antitussive effect of the drug is approximately equal to that of codeine. Prenoxdiazine does not cause addiction and drug dependence. In chronic bronchitis marked anti-inflammatory effect prenoxdiazine.
Prenoxdiazine does not affect the central nervous system function, except for the possible indirect anxiolytic action.
Prenoxdiazine rapidly and largely absorbed from the gastrointestinal tract. Maximum plasma concentration achieved prenoxdiazine 30 minutes after taking the drug, its therapeutic concentration is maintained for 6-8 hours. Relationship to plasma proteins is 55-59%. The half-life is 2.6 hours. Most of the dose is metabolized in the liver, only about 1/3 of the dose of the drug is excreted unchanged in, and the rest – in the form of metabolites (emphasis prenoxdiazine metabolite 4). During the first 12 hours prenoxdiazine metabolism the most important role played by biliary excretion and its metabolites. After 24 hours, after ingestion is allocated 93% of the formulation. For 72 hours after ingestion of 50-74% of the dose is excreted in the faeces and 26-50% – with urine.

Indications

Nonproductive cough of any origin (for catarrh of the upper respiratory tract, flu, acute and chronic bronchitis, testosterone suspension gains pneumonia, emphysema, night cough in patients with heart failure, preparing patients for bronchoscopic or bronhograficheskomu study).

Contraindications

Hypersensitivity to the drug.
Diseases associated with abundant bronchial secretion.
Condition after inhalation anesthesia.
Galactose intolerance, lactase deficiency or glucose-galactose malabsorption. Precautions: children’s age.

Pregnancy and lactation

During pregnancy and lactation use libeksin possible only if the potential benefit to the mother outweighs the potential risk to the fetus or child.

Dosing and Administration

The average dose for adults is 100 mg three or four times a day (1 tablet 3-4 times a day). In more complex cases, the dose can be increased up to 200 mg three – four times or 300 mg three times a day (2 tablets 3-4 times daily or 3 tablets 3 times a day).
The average dose for children, according to the age and body weight, or 25-50 mg three to four times a day (1/4 – 1/2 4/3 tablet twice a day). The maximum single dose for children – 50 mg (1/2 tablet), for adults – 300 mg (3 tablets). The maximum daily dose for children – 200 mg (2 tablets), for adults – 900 mg (9 tablets). In preparation for bronchoscopy dose of 0.9 – 3.8 mg / kg body weight is combined with 0.5 – 1 mg atropine for 1 hour prior to the procedure.
The tablets swallowed without chewing (to avoid mucosal anesthesia mouth).

Side effect

Allergic reactions
Rare: skin rash, angioedema. On the part of the gastrointestinal tract Rare: dry mouth or throat, anesthesia (temporary numbness and loss of sensitivity) of the oral mucosa. Less than 10% of cases: stomach pain, addiction constipation, nausea. From the nervous system (when using the drug in high doses): light sedation, fatigue. it should be emphasized that, as the sedation and fatigue, occur at doses above the therapeutic, and all the symptoms spontaneously stopped within testosterone suspension gains a few hours after discontinuation of the drug

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suspension testosterone

Suspension testosterone is rapidly and almost completely absorbed after oral administration. Food intake has little effect on the speed and completeness of removals. Bioavailability of 500 mg oral levofloxacin after is nearly 100%. After administration of a single 500 mg dose of levofloxacin is the maximum concentration of 5.2-6.9 g / ml, time to maximum concentration -. 1,3ch half-life – 8.6 hours.
Relationship to plasma proteins – 30-40%. It penetrates the tissues and organs: lungs, bronchial mucosa, sputum, organs of the urogenital system, bone tissue, cerebrospinal fluid, the prostate gland, polymorphonuclear leukocytes, alveolar macrophages.
In the liver, a small part of the oxidized and / or deacetylated. Report from the body mainly by the kidneys by glomerular filtration and tubular secretion. Following oral administration, approximately 87% of the dose is excreted in the urine unchanged within 48 hours, less than 4% in the faeces within 72 hours.

INDICATIONS
Infectious-inflammatory diseases, caused by susceptible microorganisms: acute sinusitis, acute exacerbations of chronic bronchitis, community-acquired pneumonia, complicated urinary tract infections (including pyelonephritis), uncomplicated urinary tract infections, prostatitis, infections of skin and soft tissues, septicemia / bacteremia related with the above indications, an intra-abdominal infection.

CONTRAINDICATIONS

 

  • hypersensitivity to levofloxacin or other quinolones;
  • epilepsy;
  • tendon injury during the earlier treatment of quinolones;
  • childhood and adolescence (18 years);
  • pregnancy and lactation.Precautions
    The drug should be used with caution in the elderly, due to the high probability of the presence of a concomitant decrease in renal function, with a deficit of glucose-6-phosphate dehydrogenase.DOSAGE AND ADMINISTRATION
    The drug is taken orally once or twice a day. Tablets do not chew and drink plenty of fluids (0.5 to 1 cup), can be taken before meals or between meals. Doses are determined by the nature and severity of the infection and the sensitivity of the alleged pathogen.
    In patients with normal or mildly reduced kidney function (creatinine clearance> 50 mL / min.), The recommended drug dosage regimen: Sinusitis (inflammation of the sinuses): 500 mg 1 times per day – 10 -14 days. Exacerbation of chronic bronchitis: . 250 mg or 500 mg 1 time per day – 7-10 days Community-acquired pneumonia: 500 mg 1-2 times a day – 7-14 days. Uncomplicated urinary infections ways: . 250 mg 1 time per day – 3 days Prostatitis: 500 mg – 1 per day – 28 days. Complicated urinary tract infections, including pyelonephritis: 250 mg 1 time per day – 7-10 days. skin infections and soft tissues: 250 mg 1 time per day or 500 mg 1-2 times a day – 7-14 days. Septicemia / bacteremia: 250 mg or 500 mg 1-2 times a day – 10-14 days ( after intravenous administration to continue therapy). Intra-abdominal infections: 250 mg or 500 mg 1 time per day – 7-14 days (in combination with antibacterial drugs acting on the anaerobic flora, after intravenous administration to continue therapy).

    Skin reactions and general hypersensitivity reaction times: the itching and redness of the skin. Rare: general reactions of hypersensitivity (anaphylactic and anaphylactoid reaction) with symptoms such as urticaria, bronchoconstriction and possibly – heavy gasps. In very rare cases, – swelling of the skin and mucous membranes ( for example in the areas of the face and throat), sudden drop in blood pressure and shock; increased sensitivity to sunlight and ultraviolet radiation (see “Cautions.”); hypersensitivity pneumonitis; vasculitis. In some cases: severe rash with blistering, such as Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell’s syndrome) and exudative erythema multiforme. General hypersensitivity reactions may sometimes be preceded by lighter skin reactions. The above-mentioned reaction may develop after the first dose in a few minutes or hours after administration.

    Action on the gastrointestinal tract and metabolism Common: nausea, diarrhea. Sometimes: loss of appetite, vomiting, abdominal pain, dyspepsia. Rare: bloody diarrhea which in very rare cases, it may be a sign of bowel inflammation and even pseudomembranous colitis (see .. “Cautions”) Very rare: drop in blood sugar levels (hypoglycemia), which has particular importance for patients with diabetes; Possible symptoms of hypoglycemia: “wolf” appetite, nervousness, sweating, trembling. Experience with other quinolones suggests that they are capable of causing an exacerbation of porphyria (a very rare metabolic disease) in patients who are already suffering from the disease. Such an effect is not excluded the application Lefoktsin drug.

    Nervous system Occasionally: headache, dizziness, and / or numbness, drowsiness, and sleep disorders. Rare: depression, anxiety, psychotic reactions (eg, hallucinations), discomfort (eg, paresthesias in the hands), tremor, agitation , confusion, convulsions, anxiety. Very rare: visual and hearing impairment, disturbances of taste and smell sensitivity, reduction of tactile sensitivity.

     

    The action on the cardiovascular system Rare: increased heart rate, decreased blood pressure. Very rare: (shock-like) vascular collapse. In some cases: lengthening of the QT interval.

     

    The action on the muscles, tendons and bones Rare: defeat tendons (including tendonitis), joint and muscle pain. Very rare: tendon rupture (eg Achilles tendon); this side effect may occur within 48 hours after the start of treatment and may be bilateral in nature (see “Cautions.”); muscle weakness, which is of particular importance for patients with bulbar syndrome. In some cases: muscle damage (rhabdomyolysis).

     

    Action on the liver and kidney Common: increase in liver enzymes (eg, alanine aminotransferase and aspartate aminotransferase). Rare: increased levels of bilirubin and serum creatinine (sign of limitation of the liver or kidney). Very rare: hepatic reactions (eg, inflammation of the liver); deterioration of renal function until suspension testosterone the acute renal failure, for example, due to allergic reactions (interstitial nephritis).

     

    Effects on blood Occasionally: increased number of eosinophils, a decrease in the number of white blood cells. Rare: neutropenia; thrombocytopenia, which may be accompanied by increased bleeding. Very rare: agranulocytosis and the development of severe infections (persistent or recurrent fever, deterioration of health). In some cases: haemolytic anemia; pancytopenia.

    Other side effects sometimes: . General weakness (asthenia) Very rarely . Fever Any antibiotic therapy can cause changes in the microflora (bacteria and fungi), which is normally present in humans. For this reason, it may happen enhanced reproduction of bacteria and fungi that are resistant to antibiotics are used (secondary infection and superinfection), which in rare cases may require additional treatment.

     

    Overdose
    Symptoms of overdose Lefoktsin occur at the level of the central nervous system (confusion, dizziness, impairment of consciousness and seizures seizures by type epipripadkov). In addition, it can be marked gastrointestinal symptoms (eg, nausea) and erosive lesions of the mucous membranes.
    In the studies conducted by the supra-therapeutic doses of levofloxacin was shown lengthening the QT interval.
    Treatment should be focused on presenting symptoms. Levofloxacin is not displayed by dialysis (hemodialysis, peritoneal dialysis and continuous peritoneal dialysis). Specific antidote (counteracting agent) does not exist.

    INTERACTION WITH OTHER DRUGS
    There are reports of pronounced lowering the threshold of convulsive readiness, while the use of quinolones and substances that can, in turn, lower the cerebral seizure threshold. Equally, it also relates to the simultaneous use of quinolones and theophylline, fenbufena or similar to it nonsteroidal antiinflammatory drugs (for the treatment of rheumatic diseases).
    The action of the drug Lefoktsin significantly attenuated while the use of sucralfate (means to protect the gastric mucosa). The same thing happens with the simultaneous use of magnesium-aluminum containing antacids or (drugs for the treatment of heartburn and gastralgia), as well as salts of iron (for the treatment of anemia). Lefoktsin should take no less than 2 hours before or 2 hours after the administration of these agents. With calcium carbonate interaction have been identified.
    With the simultaneous use of vitamin K antagonists should be monitored for blood coagulation system.
    Excretion (renal clearance) Lefoktsina slightly slowed down by the action of cimetidine and probenicid. It should be noted that this interaction is almost does not have any clinical significance. However, while the use of drugs such as probenicid and cimetidine, blocking certain way of deducing (tubular secretion) treatment Lefoktsinom should be made with caution.
    This applies primarily to patients with reduced renal function.
    Lefoktsin slightly increases the half-life of cyclosporin.
    Receiving glucocorticoids increases the risk of tendon rupture.

    Cautions
    Lefoktsin can not be used to treat children and adolescents because of the probability of destruction of the articular cartilage.
    In the treatment of elderly patients should be aware that patients in this group often have impaired renal function (see. Section “Dosage and administration”).
    In severe inflammation lung caused by pneumococcus Lefoktsin may not give the optimal therapeutic effect. Nosocomial infections caused by certain pathogens (P. aeruginosa), may require a combined treatment. During treatment with Lefoktsin may develop seizures attack in patients with previous brain damage caused by, for example, stroke or severe injury. Seizure may be increased, and while the application fenbufena similar to them of non-steroidal anti-inflammatory drugs, or theophylline (see. “Interactions”).
    Despite the fact that the photosensitivity observed when applying Lefoktsina very rarely, to prevent it from patients is not recommended to be exposed unnecessarily to strong sunlight or artificial ultraviolet light.
    If you suspect pseudomembranous colitis should immediately cancel Lefoktsin and start appropriate treatment. In such cases, you can not use drugs that suppress intestinal motility.
    Rarely observed when using the drug Lefoktsin tendinitis (especially inflammation of the Achilles tendon) may lead to tendon rupture. Elderly patients are more prone to tendonitis. Corticosteroid treatment ( “cortisone preparations”) are likely to increase the risk of tendon rupture. If you suspect tendonitis, stop treatment with Lefoktsin and start appropriate treatment of the affected tendon, for example, providing him rest state (see. “Contraindications” and “Side effects”).
    Patients with deficiency of glucose-6-phosphate dehydrogenase (an inherited metabolic disorder) fluoroquinolones can respond to the destruction of erythrocytes (hemolysis). In this regard, the treatment of such patients Lefoktsinom should be carried out with great care.
    These side effects Lefoktsin drug like dizziness or numbness, drowsiness and visual disturbances (see. Also section “Side effects), can impair reactivity and ability to concentrate. this can be a risk in situations where these abilities are of special suspension testosterone importance (eg while driving, during maintenance of machines and mechanisms, when working in an unstable position). in particular as it concerns cases of drug interactions with alcohol.

     

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The antibacterial drug group of fluoroquinolones. Levofloxacin – laevorotatory isomer of ofloxacin. Levofloxacin testosterone suspension half life blocking DNA gyrase enzyme (topoisomerase II) and topoisomerase IV, and crosslinking gives supercoiling of DNA breaks, causing profound morphological change in the cytoplasm, membrane and cell wall of bacteria.

Levofloxacin is active against most strains of microorganisms in conditions in vitro and in vivo:

Grampolozhitelnye aerobic microorganisms: Staphylococcus spp. (Koagulazonega-tive, methicillin / moderate methicillin-susceptible strains), Staphylococcus aureus, Staphylococcus epidermidis (methicillin-susceptible strains); Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus pneumoniae (penicillin-susceptible / moderately penicillin / penicillin-resistant strains), Streptococcus (group C, G), Viridans group streptococci (penitsilinnochuvstvitelnye and penicillin-resistant); Enterococcus faecalis; Corynebacterium diphtheriae; Listeria monocytogenes;

Aerobic gram-negative microorganisms: Acinetobacter spp, Acinetobacter anitratus, Acinetobacter baumannii, Acinetobacter calcoaceticus;. Actinobacillus actinomycetemcomitans; Citrobacter freundii, Citrobacter diversus; Eikenella corrodens; Enterobacter spp, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter cloacae, Enterobacter sakazakii.; Escherichia coli; Gardnerella vaginalis;Haemophilus ducreyi, Haemophilus influenzae (ampitsillinochuvstvitelnye / ampicillin-resistant strains), Haemophilus parainfluenzae; Helicobacter pylori; Klebsiella spp, Klebsiella oxytoca, Klebsiella pneumoniae.; Moraxella catarrhalis; Morganella morganii; Neisseria gonorrhoeae (including penitsillinazoprodutsiruyuschie strains), Neisseria meningitidis; Pasteurella spp, Pasteurella canis, Pasteurella dagmatis, Pasteurella multocida.; Proteus mirabilis, Proteus vulgaris; Providencia spp, Providencia rettgeri, Providencia stuartii.; Pseudomonas spp, Pseudomonas aeruginosa, Pseudomonas fluorescens.;Salmonella spp .; Serratia spp, Serratia marcescens.;

Anaerobic microorganisms: Bacteroides fragilis; Bifidobacterium spp .; Clostridium perfringens; Fusobacterium spp .; Peptostreptococcus spp .; Propionibacterium spp .; Veillonella spp .;

Other micro-organisms: Bartonella spp .; Chlamydia pneumoniae, Chlamydia psittaci, Chlamydia trachomatis; Legionella spp, Legionella pneumophila.; Mycobacterium spp, Mycobacterium leprae, Mycobacterium tuberculosis.; Mycoplasma hominis; Mycoplasma pneumoniae; Rickettsia spp .; Ureaplasma urealyticum.

Pharmacokinetics. If ingestion is rapidly and almost completely absorbed (eating little effect on the speed and completeness of removals). Bioavailability – 99%. The time required to reach maximum concentration – 2.1 hours; when receiving 250 mg and 500 mg of the maximum concentration of 2.8 and 5.2 ug / ml, respectively. Relationship to plasma proteins – 30-40%. It penetrates the tissues and organs: lungs, bronchial mucosa, sputum, organs of the urogenital system (including the prostate gland..), Bone tissue, cerebrospinal fluid, polymorphonuclear leukocytes, alveolar macrophages.

In the liver, a small part of the oxidized and / or deacetylated.

Report from the body mainly by the kidneys in the urine by glomerular filtration and tubular secretion in an unmodified form. Renal clearance is 70% of the total clearance. The half -. 6-8 hours Less than 5% of levofloxacin is excreted as metabolites. Following oral admission in an unmodified form with the kidneys within 24 hours to return to 70% and in 48 hours – 87% of the dose; in the rectum for 72 hours, found 4%.

Indications for use:

Infectious-inflammatory diseases caused by susceptible organisms:

  • lower testosterone suspension half life respiratory tract (chronic bronchitis, pneumonia);
  • Upper respiratory tract (sinusitis, otitis media);
  • urinary organs (including acute pyelonephritis, prostatitis, urogenital chlamydia-Lake);
  • skin and soft tissue (atheroma festering, abscesses, boils);
  • in the complex therapy of drug-resistant forms of TB.

Contraindications:

Hypersensitivity, epilepsy, tendons defeat at the earlier treatment of quinolones, pregnancy, lactation, childhood and adolescence (18 years), impairment of renal function: with creatinine clearance less than 20 ml / min, while on hemodialysis.

With care
Advanced age (a high probability of the presence of a concomitant decrease in renal function), deficiency of glucose-6-phosphate dehydrogenase.

Dosage and administration:

Inside, before a meal or in between meals, without chewing, drinking plenty of fluids (0.5 to 1 cup). During exacerbation of chronic bronchitis – 250-500 mg 1 time / day for 7-10 days. When CAP – 500 mg 1-2 times / day, for 7-14 days. When sinusitis – 500 mg 1 time / day, for 10-14 days.

In uncomplicated urinary tract infections: 250 mg 1 times / day for 3 days.

In the complicated urinary tract infections (including pyelonephritis) – 250 mg 1 times / day for 7-10 days.

When prostatitis – 500 mg 1 time / day, for 28 days.

With infections of the skin and soft tissues – 250-500 mg 1-2 times / day, for 7-14 days. When tuberculosis – in the complex therapy of drug-resistant forms of TB, 500 mg 1-2 times / day (500 – 1000 mg / day) up to 3 months.

Side effect:

From the digestive system: nausea, vomiting, diarrhea (including blood), indigestion, loss of appetite, abdominal pain, pseudomembranous enterocolitis; increased activity of “liver” transaminases, hyperbilirubinemia, hepatitis, dysbiosis.

Cardio-vascular system: decrease in blood pressure, circulatory collapse, tachycardia, prolongation of the QT interval.

From a metabolism: hypoglycaemia (increased appetite, increased sweating, trembling).

From the nervous system: headache, dizziness, weakness, sleepiness, insomnia, tremor, anxiety, paresthesia, anxiety, hallucinations, confusion, depression, movement disorders, seizures (in predisposed patients).

From the senses: blurred vision, hearing, smell, taste and tactile sensitivity.

From the musculoskeletal system: arthralgia, muscle weakness, myalgia, tendon rupture, tendonitis, rhabdomyolysis.

From the urinary system: hypercreatininemia, interstitial nephritis, acute renal failure.

From the side of hematopoiesis: eosinophilia, testosterone suspension half life hemolytic anemia, leukopenia, neutropenia, agranulocytosis, thrombocytopenia, pancytopenia, hemorrhage.

Allergic reactions: itching, and flushing of the skin, swelling of the skin and mucous membranes, urticaria, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome), bronchospasm, asthma, anaphylactic shock, hypersensitivity pneumonitis, vasculitis.

Other: fatigue, aggravation of porphyria, photosensitivity, persistent fever, the development of superinfection.

 

Overdose:

Symptoms: nausea, erosive lesions of the mucous membranes of the gastrointestinal tract (GIT), lengthening the interval QT, confusion, dizziness, seizures.
Treatment: gastric lavage, symptomatic, dialysis is ineffective. No specific antidote.

Interaction with other drugs:
increases the half-life of cyclosporin. Effect reduce drugs that suppress intestinal motility sucralfate, aluminum and magnesium antacid drugs and salts of iron (needed a break between the intake of at least 2 hours). Nonsteroidal anti-inflammatory drugs (NSAID) of the ibuprofen group, theophylline increase seizure, glucocorticosteroids (GCS) increase the risk of tendon rupture. Cimetidine and drugs that block tubular secretion, slows down. With the combination of levofloxacin with vitamin K antagonists requires monitoring of blood coagulation system.

Special instructions:

After normalization of body temperature, it is recommended to continue treatment for at least 48-78 hours.

During treatment should avoid sunlight and artificial UV radiation in order to avoid damage to the skin (photosensitivity).

If signs of tendinitis, pseudomembranous colitis levofloxacin immediately overturned.

It should be borne in mind that in patients with brain damage history (stroke, major trauma) may develop seizures, with insufficient glucose-6-phosphate dehydrogenase – the risk of hemolysis.

During the period of treatment must be careful when driving and other lesson. Potentially hazardous activities that require high concentration and psychomotor speed reactions. tretizen

testosterone suspension

Blocks the synthesis of estrogens in peripheral and in tumor tissues. In postmenopausal women, estrogens are mainly formed by the enzyme aromatase, which converts adrenal androgens (primarily androstenedione and testosterone) to estrone and estradiol. Daily treatment with letrozole leads to lower concentrations of estradiol, estrone and estrone sulfate in plasma at 75-95% of the initial content. Violation of the synthesis of steroid hormones in the adrenal gland is not observed. The suppression of the synthesis of estrogen is maintained throughout the treatment. The blockade of estrogen biosynthesis does not lead to the accumulation of androgens are precursors of estrogens. Patients treated with letrozole, there were no changes in the concentrations of LH and follicle-stimulating hormone in the blood plasma, and there were no changes in thyroid function.

The pharmacokinetics of
Letrozole is rapidly and completely absorbed from testosterone suspension the gastrointestinal tract (GIT), the mean bioavailability of 99.9%. Food slightly decreases the rate of absorption, but the clinical significance of this has, therefore letrozole may be taken regardless of meals.
Contact letrozole to plasma proteins is approximately 60% (mainly albumin – 55%). The equilibrium concentration is reached within 2-6 weeks of daily administration of a daily dose of 2.5 mg. Pharmacokinetics is not linear.
Cumulation of long-term use are not observed.
Letrozole is largely metabolized by the action of CYP2A6 and CYP3A4 isoenzymes of cytochrome P450 to form a pharmacologically inactive carbinol compounds.
Write mainly kidneys as metabolites, to a lesser extent – through the intestines. The final half-life (T ½ ) is 48 hours.
Report from the plasma by hemodialysis.
The pharmacokinetic parameters of letrozole does not depend on the age of the patient.
The pharmacokinetic parameters are not changed in renal insufficiency.
In patients with moderate hepatic dysfunction (Child-Pugh B), the mean AUC values at and up to 37%, but remain within the range of values that have been reported in individuals without liver dysfunction. In patients with liver cirrhosis and severe impairment of its function (Child-Pugh C) AUC increased by 95% and the T ½ to 187%. However, given the good tolerability of high doses (5-10 mg / day) in these cases need not to change the dose of letrozole.

Indications

  • Common forms of hormone-dependent breast cancer in postmenopausal women (with natural or artificially induced).

Contraindications

  • Hypersensitivity to letrozole or to any other component of the drug.
  • Endocrine status characteristic premenopauznom period.
  • Pregnancy, lactation.
  • Age up to 18 years.

Precautions : when expressed violations of liver and kidney function (creatinine clearance less than 10 ml / min). Before prescribing letrozole should be carefully weigh the relationship between the potential risk and the expected effect of treatment.

Dosing and Administration
Inside, regardless of meals.
The recommended dose of letrozole is 2.5 mg once a day, every day, for a long time.
If signs of disease progression receiving letrozole should be discontinued.
In elderly patients letrozole dose adjustment is required. Patients with impaired liver and / or kidney disease. In testosterone suspension patients with impaired hepatic or renal function (creatinine clearance > 10 ml / min) dose adjustment is required. However, patients with severe hepatic impairment should be under constant supervision.

Side effects:
The frequency of side effects: very common – > 10%, often – > 1-10%, sometimes – > 0.1% – <1%, rarely – > 0.01-0.1%, rarely – <0.01%, including isolated reports . On the part of the digestive system : often -toshnota, vomiting, anorexia, dyspepsia, constipation, diarrhea; sometimes – pain in the abdominal area, stomatitis, dry mouth, increased activity of “liver” enzymes. On the part of the central and peripheral nervous system : often – headache, dizziness, weakness; sometimes – depression, anxiety, drowsiness, insomnia, memory impairment, dysesthesia; rarely – irritability, nervousness, hyperesthesia, hypoesthesia. From the hematopoietic system and lymphatic system : sometimes -leykopeniya. On the part of the cardiovascular system : sometimes – palpitations, tachycardia, thrombophlebitis, increased blood pressure (BP); rarely – pulmonary embolism, arterial thrombosis, cerebrovascular accident. Respiratory system : sometimes – shortness of breath. Skin and skin appendages: common – alopecia, increased sweating, skin rash; sometimes – itching, dry skin, urticaria. From the musculoskeletal system : often – myalgia, arthralgia, ossalgia arthritis. From the senses : sometimes – cataract, eye irritation, “blurred” vision, taste disturbance. On the side urinary system : rarely – urinary frequency. reproductive system : sometimes – vaginal bleeding, vaginal discharge, vaginal dryness. Other : very often – hot flashes ( “hot flushes”), often -Increased fatigue, asthenia, malaise, peripheral edema, weight gain; sometimes – hypercholesterolemia, generalized edema, pain at tumor sites, urinary tract infection; rarely – fever, thirst, weight loss.

Overdose
Specific treatment of overdose is unknown. Symptomatic and supportive therapy.

Interaction with other drugs
of clinical experience on the use of letrozole in combination with other anticancer drugs are not available at the moment.
According to the results of studies in vitro, , letrozole inhibits the activity of cytochrome P450 isoenzymes – CYP2A6 and CYP2C19 (last – in moderation). In deciding on the significance of these data for the clinic, please note that isoenzyme CYP2A6 does not play a significant role in the metabolism of drugs. Experiments in vitro showed that letrozole in concentrations 100 times the equilibrium value of plasma has no ability to significantly inhibit the metabolism of diazepam (substrate for CYP2C19). Thus, clinically relevant interactions with CYP2C19 isoenzyme are unlikely. However, caution should be exercised when used together letrozole and drugs metabolized mainly with the participation of the aforementioned isoenzymes and having a narrow therapeutic index.

Cautions
Patients with severely impaired liver function should be under constant supervision.
Some side effects of the drug, such as testosterone suspension general weakness and dizziness, may affect the ability to perform potentially hazardous activities that require concentration and fast reactions. In this regard, care must be taken in the management of vehicles and mechanisms. buy anabolic steroids online bruce lee’s workout anabolic steroids online uk