halotestin

Active substance: halotestin 60 mg, 90 mg, 120 mg Excipients: dibasic calcium phosphate, microcrystalline cellulose, croscarmellose sodium, magnesium stearate.

Coated tablet Opadry II Green 39K11520 (for dosage of 60 mg), Opadry II White 39K18305 (for dosage of 90 mg); Opadry II Green 39K11529 (for dosage 120 mg), carnauba wax.

The composition of the film-coating: Lactose monohydrate, hypromellose, titanium dioxide, triacetin, aluminum lake dye indigo carmine (E132) (for tablets 60 mg and 120 mg), iron colorant oxide yellow (E172) (for tablets 60 mg and 120 mg).

DESCRIPTION: The dosage of 60 mg: Green biconvex tablets apple-shaped, film-coated, embossed ARCOXIA 60 on one side and embossed 200 on the other side. The dosage of 90 mg: White biconvex tablets apple-shaped, film-coated, with ARCOXIA 90 embossed on one side and 202 embossed on the other side.The dosage of 120 mg: Light green apple-shaped, biconvex tablet, film-coated with ARCOXIA 120 embossed on one side and 204 embossed on the other side.

Pharmacological group:

Non-steroidal anti-inflammatory drugs (NSAIDs).

ATX code: M01AN05

Pharmacological properties Pharmacodynamics NSAIDs. Etorikoksib is a selective COX-2 inhibitor, in therapeutic concentrations blocks the formation of prostaglandins and anti-inflammatory, analgesic and antipyretic activity. Selective inhibition of COX-2 halotestin accompanied by a reduction of clinical symptoms associated with inflammation, with no effect on platelet function and mucosa of the gastrointestinal tract. Etorikoksib possesses a dose-dependent effect of inhibiting COX-2 without affecting COX-1 in the application daily doses up to 150 mg. The drug has no effect on production of prostaglandins in the gastric mucosa and bleeding time. In the studies it was observed reduction of arachidonic acid and platelet aggregation caused by collagen.Pharmacokinetics Absorption Rapidly absorbed when taken orally. Oral bioavailability is about 100%. In applying the drug in fasting adult dose of 120 mg of the maximum concentration (C max ) – 3.6 g / ml, the time to reach maximum concentration (TC max ) in the blood plasma after administration -1ch. The geometric mean AUC 0-24ch was 37.8 mcg x h / ml. Pharmacokinetics etorikoksiba within the therapeutic dose is linear. Food intake has no significant effect on the severity and rate of absorption etorikoksiba at a dose of 120 mg. However, a decrease in the values of C max by 36% and increase the TC max for 2 h. Antacids do not affect the pharmacokinetics of the drug. Distribution Communication plasma protein while taking the drug exceeds 92%. The volume of distribution (Vdss) at steady state is about 120 liters. It is shown that halotestin crosses the placental and blood-brain barrier. Metabolism Intensively metabolized in the liver, involving cytochrome P450 isoenzyme (CYP) and the formation of 6-hydroxymethyl-etorikoksiba. Less than 1% of the drug is excreted in the urine in unchanged form. 5 etorikoksiba metabolites detected, major – 6-hydroxymethyl derivative thereof and halotestin – 6-carboxy-acetyl-halotestin. The main metabolites have no effect on COX-1 and completely inactive or inactive against COX-2. Excretion Following single intravenous administration to healthy volunteers labeled radioactive drugs containing halotestin 25 mg, demonstrated that 70% of the drug is excreted through the kidneys, 20% – through the intestine, mainly in the form of metabolites. Less than 2% was found in an unmodified form. Excretion etorikoksiba occurs mainly via the kidneys by metabolism. The equilibrium concentration of the drug achieved with daily intake of 120 mg in 7 days, with a cumulative factor of about 2, which corresponds to the half-life, about 22 hours. Plasma clearance is about 50 ml / min. Pharmacokinetic differences between men and no women. Pharmacokinetics in the elderly ( 65 years and older) is comparable to that of the young. There is no need to adjust the dose of the drug in the elderly. Racial differences do not affect the pharmacokinetic parameters etorikoksiba. liver diseasepatients with minor hepatic impairment (5-6 points on a scale Child-Pugh) single reception etorikoksiba at a dose of 60 mg / day was accompanied by an increase of 16% of the index AUC as compared to healthy individuals. in patients with moderate hepatic impairment (7-9 points on a scale Child-Pugh), taking the drug at a dose of 60 mg every other day , the AUC it was the same as in healthy people taking the drug buy halotestin on a daily basis at the same dose. These clinical and pharmacokinetic studies in patients with severe hepatic impairment (more than 9 points on a scale Child-Pugh) are absent. kidney diseasepharmacokinetic performance single use etorikoksiba a dose 120 mg in patients with moderate to severe renal disease and end-stage renal disease (ESRD) on hemodialysis did not differ significantly from that of healthy individuals. Hemodialysis little effect on the elimination (dialysis clearance – about 50 ml / min). Use in children Pharmacokinetic parameters etorikoksiba in children under the age of 12 years have not been studied. In comparative pharmacokinetic studies to obtain comparable data in the application etorikoksiba in a group of adolescents (12 to 17 years) 40-60 kg body weight a dose of 60 mg / day, in the same age group, and weighing more than 60 kg – 90 mg / day, as well as adults when receiving 90 mg / day.

INDICATIONS

Symptomatic treatment of osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, pain and inflammatory symptoms associated with acute gouty arthritis.

CONTRAINDICATIONS

  • Hypersensitivity to any component of the drug;
  • complete or incomplete combination of bronchial asthma, recurrent nasal polyposis, or paranasal sinuses and intolerance of aspirin and other NSAIDs (including history);
  • erosive and ulcerative changes in gastric mucosa and 12 duodenal ulcer, active gastrointestinal bleeding; cerebrovascular bleeding or other;
  • inflammatory bowel disease (Crohn’s disease, ulcerative colitis) in the acute phase;
  • hemophilia and other bleeding disorders;
  • severe heart failure (NYHA II-IV);
  • severe hepatic insufficiency (more than 9 points on a scale Child-Pugh) or active liver disease;
  • severe renal insufficiency (creatinine clearance less than 30 ml / min), advanced kidney disease, confirmed hyperkalemia;
  • period after coronary artery bypass surgery; peripheral artery disease, cerebrovascular disease, symptomatic ischemic heart disease;
  • firmness remaining blood pressure values exceeding 140/90 mmHg. Art. with uncontrolled hypertension;
  • pregnancy, breast-feeding;
  • Children up to age 16 years.

WITH CARE A history of the development of ulcerative lesions gastrointestinal tract, the presence of infection Helicobacter pylori, old age, long-term use of NSAIDs, frequent alcohol consumption, severe somatic diseases, dyslipidemia / hyperlipidemia, diabetes mellitus, hypertension, edema, fluid retention, smoking, creatinine clearance less than 60 ml / min, concomitant therapy following medications:

– Anticoagulants (eg, warfarin) – antiplatelet agents (e.g., aspirin, clopidogrel), – oral steroids (e.g., prednisone), – selective serotonin reuptake inhibitor (such as citalopram, fluoxetine, paroxetine, sertraline).

In patients with hepatic insufficiency (5-9 points on a scale Child-Pugh) do not exceed a daily dose of 60 mg.

DOSAGE AND ADMINISTRATION . Inside, regardless of meals, washed down with a little water Osteoarthritis: The recommended dose is 60 mg once daily. Rheumatoid arthritis and ankylosing spondylitis: The recommended dose is 90 mg once daily. Acute gouty arthritis: Recommended to acute period halotestin, the dose is 120 mg once daily. The duration of use of the drug at a dose of 120 mg is not more than 8 days. It is necessary to use the minimum effective dose as low as possible short course. The average therapeutic dose for pain syndrome is single 60 mg per day. SIDE EFFECTS Very often> 10%, often -1-10%; infrequently – 0.1-1%;rarely – 0.01-0.1%; very rarely – less than 0.01%, including individual cases. From the digestive system: often – epigastric pain, nausea, diarrhea, dyspepsia, flatulence; infrequently – bloating, belching, increased peristalsis, constipation, dryness of the oral mucosa, gastritis, ulcers of the gastric mucosa and 12 duodenal ulcer, irritable bowel syndrome, esophagitis, ulcers of the oral mucosa, vomiting; very rarely – gastrointestinal ulcers (bleeding or perforation). On the part of the hepatobiliary system: very rarely – hepatitis. From the nervous system: often – headache, dizziness, weakness; seldom – taste disturbance, drowsiness, sleep disturbances, sensitivity infringement, including paresthesia / hypersensitivity, anxiety, depression, impaired concentration, rarely – hallucinations, confusion. From the sensory organs: rarely – blurred vision, conjunctivitis, tinnitus, vertigo. From the urinary system: rarely – proteinuria; very rarely – renal failure halotestin cycle, usually reversible remove the drug. Allergic reactions: very rare – anaphylactic / anaphylactoid reactions, including a pronounced reduction in blood pressure and shock; the part of the cardiovascular system: often – heartbeat, increased blood pressure; seldom – flushing, cerebrovascular disease, atrial fibrillation, congestive heart failure, nonspecific ECG changes; myocardial infarction, very rarely – hypertensive crisis. With the respiratory system: rarely – cough, shortness of breath, nosebleeds; very rarely – bronchospasm. For the skin: often – ecchymosis; rare – swelling of the face, itching, rash; very rarely – urticaria, Stevens-Johnson syndrome, Lyell’s syndrome.Infections: infrequent – gastroenteritis, upper respiratory tract infection, urinary tract. From the musculoskeletal system: rarely – muscle cramps, arthralgia, myalgia. Violations of metabolism: often – swelling, fluid retention; rarely – changes in appetite, weight gain. Other: often – flu-like symptoms; rarely – pain in the chest. The results of laboratory tests: often – increase in “liver” transaminase; rarely – increase of nitrogen in the blood and urine, increased creatine kinase activity, decreased hematocrit, decreased hemoglobin, hyperkalemia, leukopenia, thrombocytopenia, increased serum creatinine, increased uric acid; rarely – increased sodium in the blood serum.

Overdose

In clinical trials on overdose Arcoxia has not been reported. In clinical trials, reception Arcoxia at a dose of 500 mg or multiple reception of up to 150 mg / day did not cause significant toxic effects for 21 days. If overdose may cause harmful effects on the gastrointestinal tract, the cardiovascular system and kidneys. In case of overdose symptomatic therapy. Etorikoksib not appear in hemodialysis, elimination of the drug in peritoneal dialysis has not been studied.

Interaction with other drugs Pharmacodynamic interactions Oral anticoagulants (warfarin): In patients receiving warfarin, reception Arcoxia at a dose of 120 mg per day, accompanied by an increase of about 13% of international normalized ratio (MHO) of prothrombin time. In patients receiving warfarin or similar medicaments should monitor MHO performance during start or change treatment Arcoxia, especially in the first few days. Diuretic drugs, angiotensin-converting enzyme (ACE): It has been reported that non-selective NSAIDs and selective inhibitors COX-2 may reduce the hypotensive effect of ACE inhibitors. This interaction should be taken into account when treating patients receiving Arcoxia simultaneously with ACE inhibitors. In patients with impaired renal function (for example, dehydration or in old age) this combination may worsen kidney function failure. Aspirin: Arcoxia can be used in conjunction with acetylsalicylic acid in low doses, intended for the prevention of cardiovascular diseases.However, co-administration of low-dose acetylsalicylic acid and Arcoxia may lead to an increase in the frequency of GI ulceration or other complications compared to taking one Arcoxia. At equilibrium, halotestin 120 mg once daily has no effect on anti-platelet activity of acetylsalicylic acid in low dose (81 mg daily). The drug is not a substitute for preventive action of acetylsalicylic acid in cardiovascular disease. Cyclosporine and tacrolimus increase the risk of nephrotoxicity while taking the drug. Pharmacokinetic interaction Lithium: there is evidence that non-selective NSAIDs and selective COX-2 inhibitors may increase the concentration of lithium in plasma. This interaction should be taken into account when treating patients receiving Arcoxia simultaneously with lithium. Methotrexate: Two studies investigated the effects of Arcoxia at a dose of 60, 90 and 120 mg 1 time per day for seven days in patients receiving 1 weekly methotrexate dose of from 7.5 to about 20 mg for rheumatoid arthritis. Arcoxia at a dose of 60 mg and 90 had no effect on plasma concentration (by AUC) and renal clearance of methotrexate. In one study, Arcoxia 120 mg did not affect the plasma concentration (by AUC) and renal clearance of methotrexate. In another study, Arcoxia 120 mg increased the concentration of MTX in the plasma by 28% (by AUC) and reduced renal clearance of methotrexate to 13%. While appointing Arcoxia at doses higher than 90 mg daily and methotrexate be monitored for possible appearance of toxic effects of methotrexate. Oral Contraceptives: reception Arcoxia 120 mg with oral contraceptives motivation bodybuilding containing 35 mcg of ethinyl estradiol (EE) and 0.5 to 1 mg norethindrone for 21 days, at the same time or with the difference of 12 hours AUC increased stationary 0-24ch for energy efficiency by 50-60%.However, norethisterone concentration usually does not increase to a clinically significant degree. This increase in EE concentration should be considered when selecting an appropriate oral contraceptive for the simultaneous application of Arcoxia. This fact may lead to an increase in the frequency of thromboembolism by increasing the energy efficiency of exposure. Significant pharmacokinetic interaction withcorticosteroids is not detected. Digoxin: halotestin does not affect the equilibrium AUC 0-24ch or elimination of digoxin. However, halotestin increases C max (mean 33%), which may be important in the development of digoxin overdose. Rifampicin: Simultaneous reception Arcoxia and rifampicin – a potent inducer of hepatic metabolism – leads to a decrease of 65% AUC for etorikoksiba plasma. This interaction should be taken into account while appointing Arcoxia with rifampicin. Antacids and ketoconazole (a potent inhibitor of CYP3A4) did not have a clinically meaningful effect on the pharmacokinetics of Arcoxia.

Cautions

Taking medication Arcoxia requires careful blood pressure control. All patients in the appointment of the drug should be monitoring of blood pressure during the first two weeks of treatment and periodically thereafter. Also, should regularly monitor liver function and kidney. In the case of raising the level of “liver” transaminases 3 times or more, with the upper limit of normal, the drug should be discontinued. Given the increased risk of adverse effects with increasing duration of the reception, you need to periodically evaluate the need to continue taking the drug and the possibility of reducing the dose. Do not use drug concurrently with other NSAIDs. Use of the drug can impair female fertility and is not recommended for women planning pregnancy. The shell of the drug Arcoxia contains lactose in small quantities, which should be considered when administering the drug to patients with lactase deficiency. During the period of treatment must be careful when driving and occupation of other potentially hazardous activities that require high concentration and psychomotor speed reactions. Patients were observed episodes of dizziness, drowsiness, or weakness, should refrain from activities that require concentration. Ou acheter des steroides, steroide anabolisant steroide anabolisant effet secondaire. bulking steroids bodybuilding for beginners female dmz15 bodybuilding dietitian

jim stoppani bodybuilding boldenone steroids bodybuilding coach

Post tags: halotestin