equipoise side effects – a synthetic nucleoside analogue with a pronounced antiviral effect. It has a broad spectrum of activity against various DNA and RNA viruses.
equipoise side effects is readily penetrates into the affected cells and virus rapidly phosphorylated equipoise side effects in intracellular adenosine mono-, di- and triphosphate. These metabolites, especially equipoise side effects triphosphate, have pronounced antiviral activity.
The mechanism of action of equipoise side effects is not well understood. However, it is known that equipoise side effects inhibits inosine monophosphate dehydrogenase (IMP), this effect leads to a marked decrease in the level of intracellular guanosine triphosphate (GTP), which is in turn accompanied by suppression of the synthesis of viral RNA and virus-specific proteins. equipoise side effects inhibits the replication of new virions that reduces viral load. equipoise side effects selectively inhibits the synthesis of viral RNA without inhibiting RNA synthesis in the normally functioning cells.
equipoise side effects is effective against many RNA and DNA viruses. The most sensitive to equipoise side effects DNA viruses include: Simplex herpes virus, porks-virus, virus of Marek`s illness. Insensitive to equipoise side effects DNA viruses include: Varicella Zoster, pseudorabies, cow smallpox. The most sensitive to equipoise side effects RNA viruses are: influenza A, B, paramyxovirus (parainfluenza, epidemic paratotite, Nucasl`s illness), reoviruses, RNA tumoral viruses. Insensitive to equipoise side effects RNA viruses are: enteroviruses, rhinovirus, Semlicy Forest.
equipoise side effects has activity against hepatitis C virus (HCV). The mechanism of action of equipoise side effects against HCV have not been fully elucidated. It is assumed that accumulates as phosphorylation equipoise side effects triphosphate competitively inhibits the formation of guanosine triphosphate, thereby reducing the synthesis of viral RNA. It is also believed that the mechanism of the synergistic action of equipoise side effects and alpha interferon against HCV due to increased phosphorylation of equipoise side effects with interferon.
Absorption: with oral equipoise side effects is rapidly absorbed in the gastrointestinal tract. Moreover, its bioavailability is greater than 45%.
Distribution: equipoise side effects is distributed in plasma, mucous secretions and airway erythrocytes. A large number of equipoise side effects triphosphate accumulates in red blood cells, reaching a plateau at Day 4 and continue for several weeks after administration. Poluraspredeleniya period of 3.7 hours, volume of distribution (Vd) -. 647 – 802 liters. In exchange reception equipoise side effects accumulates in plasma in large quantities. The ratio of the bioavailability (AUC – area under “concentration / time” curve) and by repeated single dose equal to 6. The high equipoise side effects concentrations (over 67%) can be detected in cerebrospinal fluid after prolonged use.
Protein binding: slightly bound to plasma proteins.
The time to reach maximum plasma concentration – from 1 to 1.5 hours.
The time to reach a therapeutic concentration in the plasma depends on the minute blood volume.
The average value of the maximum concentration (C max ) in the plasma of about 5 micromoles per liter at the end of 1 week of receiving 200 mg every 8 hours and about 11 micromoles per liter at the end of 1 week of receiving 400 mg every 8 hours.
Biotransformation: equipoise side effects phosphorylated in liver cells in active metabolites as mono-, di- and triphosphate, which is then metabolized into 1,2,4 – triazolkarboksamid (amide hydrolysis trikarboksilovuyu deribozilirovanie and acid to form a triazole carboxylic metabolite).
Excretion: equipoise side effects is excreted from the body slowly. Half-life (T 1/2 ) after receiving a single 200 mg dose of from 1 to 2 hours due to the plasma and erythrocytes of 40 days. Upon termination of a course of reception the T 1/2 is about 300 hours. equipoise side effects and its metabolites are primarily excreted in the urine. Only about 10% is excreted in the feces. In unmodified form about 7% of equipoise side effects is displayed for 24 hours and about 10% – for 48 hours.
Pharmacokinetics in special clinical conditions: When taking the drug in patients with renal insufficiency AUC and the C max of equipoise side effects increased, due to a decrease in the true clearance. Patients with liver failure (A, B and C degrees) pharmacokinetics equipoise side effects does not change. After receiving a single dose with food containing fat varies significantly equipoise side effects pharmacokinetics (AUC and C max is increased by 70%).
Indications for use:
Chronic hepatitis C (treatment in combination with alpha-interferon).
Hypersensitivity, pregnancy, lactation, chronic heart failure stages IIb-III, myocardial infarction, renal insufficiency (creatinine clearance – less than 50 ml / min), severe anemia, liver failure, decompensated cirrhosis, autoimmune diseases (including autoimmune hepatitis), not treatable thyroid disease, severe depression with suicidal intentions, children and Youth age (up to 18 years).
Women of childbearing age (pregnancy is not desirable), decompensated diabetes (with bouts of ketoacidosis); chronic obstructive pulmonary disease, pulmonary embolism, chronic heart failure, thyroid disease (including hyperthyroidism), bleeding disorders, thrombophlebitis, mielodeprescia, hemoglobinopathies (including thalassemia, sickle-cell anemia), depression, suicidal (including history).
Dosage and administration:
The drug is taken by mouth without chewing and drinking water, along with the food intake.
Patients with hepatitis C is recommended to take arviron the rate of 15 mg per 1 kg of body weight, which corresponds to 800-1200 mg per day, ie, 2-3 capsules in the morning and 2-3 capsules in the evening. Typically, the recommended dosage for patients weighing less than 75 kg is 1000 mg per day (2 capsules 3 capsules in the morning and evening) patients with body weight more than 75 kg are advised to take 1200 mg per day (3 capsules in the morning and 3 capsules in the evening).
Duration arvironom combination therapy with interferon-alpha typically is 24 – 48 weeks. In addition, for treatment-naïve patients with duration of the course is at least 24 weeks and patients with genotype 1, the course duration is 48 weeks. In patients refractory to monotherapy with interferon alpha, as well as the duration of a relapse rate of the disease is not less than 6 months.
- From the nervous system: headache, insomnia, asthenic syndrome, depression.
- Cardio-vascular system: decrease in blood pressure, bradycardia, cardiac arrest.
- From the side of hematopoiesis: hemolytic anemia, leukopenia, neutropenia, granulocytopenia, thrombocytopenia.
- From the digestive system: loss of appetite, nausea, hyperbilirubinemia.
- Allergic reactions: skin rash, urticaria, angioedema, bronchoconstriction, anaphylaxis.
- Other: hair loss.
Perhaps the increased severity of side effects.
Treatment: removal of the drug, symptomatic therapy.
Interaction with other drugs:
When combined equipoise side effects and interferon alfa-marked synergism of their actions.
In clinical use of different drugs at therapeutic doses in combination with equipoise side effects showed no significant interactions.
Purpose equipoise side effects zidovudine treatment during and / or simultaneously with stavudine existing HIV infection accompanied by a decrease in phosphorylation of these drugs, resulting in HIV viremia and treatment regimen requires a change. Not detected interaction equipoise side effects and nucleoside reverse transcriptase inhibitors or protease inhibitors. It is therefore possible joint use of these drugs and equipoise side effects for the treatment of patients co-infected with HIV and hepatitis C.
Medicaments containing compounds of magnesium and aluminum, simethicone reduces the bioavailability.
Medical staff working with the preparation, one should consider its teratogenicity. Men and women of reproductive age during treatment and for 7 months after the end of treatment should use effective contraception.
Laboratory tests (complete blood count with leukocyte and platelet count, determination of electrolytes, creatinine, liver function tests) should be carried out before the start of therapy, at 2 and 4 weeks and then regularly.
During treatment with equipoise side effects maximum decrease in hemoglobin in the majority of cases it occurs after 4-8 weeks of starting treatment. By reducing the hemoglobin is less than 110 mg / mL should be temporarily reduce the dose of equipoise side effects at 400 mg per day, with a decrease in hemoglobin of less than 100 mg / ml dose should be reduced to 50% of the original. In most cases, the recommended dose modifications provide restoration of hemoglobin levels. By reducing the hemoglobin is less than 85 mg / ml should stop taking the drug.
In acute manifestations of hypersensitivity (urticaria, angioedema, bronchoconstriction, anaphylaxis) use of the drug should be discontinued immediately. Transient rashes do not serve as grounds for interruption of treatment.
During treatment, those experiencing fatigue, drowsiness or disorientation, should refrain from driving motor vehicles and activities potentially hazardous activities that require high concentration and psychomotor speed reactions.
In connection with a possible worsening of renal function in elderly patients prior to use of the drug is necessary to determine kidney function, in particular creatinine clearance.