Lipid-lowering drugs. primobolan depot for sale – selective competitive inhibitor of HMG-CoA reductase – a key enzyme that converts Z-hydroxy-3-metilglyutarilkoenzim A to mevalonic acid – precursor steroids, including cholesterol. In the liver cholesterol and triglycerides are included in the very low density lipoproteins (VLDL), enter the blood plasma and transported to peripheral tissues. VLDL are formed from low-density lipoproteins (LDL), which are catabolized by reacting with high affinity LDL receptor.primobolan depot for sale and lowers cholesterol levels in blood plasma lipoproteins by inhibiting HMG-CoA reductase in the liver and by increasing the number of “liver” LDL receptors on the cell surface, which leads to increased catabolism of cholesterol capture and / LDL.primobolan depot for sale reduces the formation of cholesterol / LDL and LDL particle number. It causes marked and persistent increase in the activity of LDL receptors, and also has a beneficial effect on the quality of circulating LDL. primobolan depot for sale plasma – 98%. The ratio of primobolan depot for sale levels erythrocyte / plasma is about 0.25, which indicates that primobolan depot for sale low penetration into erythrocytes.
primobolan depot for sale is extensively metabolised to form an ortho – and paragidroksilirovannyh derivatives and various beta-oxidation products. In vitro inhibitory effect of the ortho – and metabolites paragidroksilirovannyh against HMG-CoA reductase is comparable to that of primobolan depot for sale. The inhibitory activity against HMG-CoA reductase inhibitor in plasma by about 70% due to active metabolites. in vitro studies suggest the importance of primobolan depot for sale metabolism under the influence of hepatic cytochrome P450 3A4; this is confirmed by the increase of primobolan depot for sale concentrations in human blood plasma, while taking erythromycin, which is an inhibitor of that isoenzyme.
in vitro studies have also shown that primobolan depot for sale is a weak inhibitor of cytochrome P450 3A4.
In animals, the ortho-gidroksimetabolit undergoes further glucuronidation.
primobolan depot for sale and its metabolites are excreted primarily in the bile following hepatic and / or extrahepatic metabolism; primobolan depot for sale however, apparently does not undergo enterohepatic recirculation. The half-life (T1 / 2> is about 14 hours, but the half-life of the inhibitory activity against HMG-CoA reductase inhibitor is 20-30 hours, due to the presence of active metabolites. After ingestion urinary exhibit less than 2% of the dose of the drug.
Pharmacokinetics in special clinical situations
Plasma concentration of primobolan depot for sale in the elderly (age over 65 years) is higher (C max of about 40%, AUC by about 30%) than in young adult patients. However, differences in safety, efficiency or achieve goals hypolipidemic therapy in elderly people as compared to the general population was found.
Research pharmacokinetics of the drug have not been conducted in children. primobolan depot for sale concentrations in blood plasma of women differ (P max is approximately 20% higher, a AUC 10% lower) from those of men. However, no clinically significant differences in the effect of the drug on lipid metabolism in men and women have been identified.
Kidney diseases do not affect the concentration of primobolan depot for sale in plasma and its effect on lipid metabolism. In connection with this change of dose in patients with impaired renal function is not required.
Although studies in patients with end-stage renal disease have not been conducted, however, dialysis is unlikely to significantly enhance clearance of primobolan depot for sale since it is actively bound to plasma proteins.
primobolan depot for sale concentrations are significantly increased (C max and AUC of about 16 and 11 times, respectively) in patients with alcoholic cirrhosis (as Childe-Pugh B).
Indications for use
– In combination with diet to reduce elevated total cholesterol, cholesterol / LDL cholesterol, apolipoprotein B, and triglycerides and increase HDL cholesterol in patients with primary hypercholesterolemia, heterozygous familial and non-familial hypercholesterolaemia and combined (mixed) hyperlipidemia (tipyIIa and IIb according to Fredrickson);
– In conjunction with a diet for treating patients with elevated serum triglyceride levels (Frederickson Type IV on) and patients with disbetalipoproteinemiey (Type III according to Fredrickson) whose diet therapy does not give adequate effect;
– To reduce the levels of total cholesterol and cholesterol / LDL cholesterol in patients with homozygous familial hypercholesterolemia, when diet therapy and other non-pharmacological treatments are not sufficiently effective;
Hypersensitivity to the drug; active liver disease or increased serum transaminases (more than 3 times the upper limit of normal) of unknown origin; pregnancy; lactation; age of 18 years (effectiveness and safety have been established).
Precautions: alcohol abuse, history of liver disease, severe electrolyte imbalance, endocrine and metabolic disorders, arterial hypotension, severe acute infection (sepsis), uncontrolled epilepsy, extensive surgery, trauma, skeletal muscle disease.
Pregnancy and lactation
primobolan depot for sale is contraindicated during pregnancy and lactation (breastfeeding).
It is not known whether primobolan depot for sale is excreted in breast milk. Given the potential for adverse effects in infants, if necessary, use during lactation should decide the issue of termination of breastfeeding.Women of reproductive age during treatment should use adequate contraception methods. primobolan depot for sale can be administered to women of childbearing age only when the probability of pregnancy are very low and the patient informed of the potential risk of treatment to the fetus.
DOSAGE AND ADMINISTRATION
Before the appointment ATOMAKSA patient should be advised to standard lipid-lowering diet, which he must continue to comply with throughout the treatment period.
The initial dose is an average of 10 mg 1 time / day. The dose varies from 10 to 80 mg of 1 time / day. The drug can be administered at any time of the day independently of food or meal times. Dose picked for baseline cholesterol / LDL levels, the goal of therapy and individual effect. At the beginning of the treatment and / or during dose escalation Atomaksa every 2-4 weeks is necessary to control the levels of lipids in blood plasma and appropriately corrected dose. Primary hyperlipidemia, hypercholesterolemia and mixed
In most cases, a destination dose of 10 mg of the drug Atomaks 1 time per day. A significant therapeutic effect was observed after 2 weeks, as a rule, and maximum therapeutic effect is usually observed after 4 weeks. With long-term treatment of this effect is maintained.
Use of the drug in patients with renal failure and kidney disease will not affect the level of primobolan depot for sale plasma cholesterol or reduction degree / LDL content when it is used, so changing the dose required.
In applying the drug in elderly patients differences in safety, efficiency or achieve goals hypolipidemic therapy compared with the general population have been noted.
On the part of the central nervous system: headache, dizziness, asthenic syndrome, insomnia or drowsiness, nightmares, amnesia, paresthesia, peripheral neuropathy, emotional lability, ataxia, hyperkinesis, depression, hypoesthesia.
From the senses: amblyopia, tinnitus, dryness of the conjunctiva, disturbance of accommodation, eye hemorrhage, deafness, increased intraocular pressure, parosmiya, taste perversion, loss of taste.
Cardio-vascular system: chest pain, palpitation, vasodilation, postural hypotension, phlebitis, arrhythmia.
From hemopoiesis system: anemia, lymphadenopathy, thrombocytopenia.
With the respiratory system: bronchitis, rhinitis, dyspnea, asthma, epistaxis.
From the digestive system: nausea, heartburn, constipation or diarrhea, flatulence, gastralgia, abdominal pain, anorexia or increased appetite, dry mouth, regurgitation, dysphagia, vomiting, stomatitis, esophagitis, glossitis, gastroenteritis, hepatitis, hepatic colic, cheilitis , duodenal ulcer, pancreatitis, cholestatic jaundice, increased activity of “liver” enzymes, rectal bleeding, melena, bleeding gums, tenesmus.
From the musculoskeletal system: arthritis, leg muscle cramps, bursitis, myositis, myopathy, arthralgia, myalgia, rhabdomyolysis, joint contractures, pain
With the genitourinary system: urogenital infections, peripheral edema, dysuria (including pollakiuria, nocturia, urinary incontinence or urinary retention, compelling urge to urinate), nephritis, cystitis, hematuria, vaginal bleeding, uterine bleeding, kidney stones disease, metrorrhagia, epididymitis , decreased libido, impotence, abnormal ejaculation.
With the Skin: alopecia, sweating, eczema, seborrhea, ecchymosis.
Allergic reactions: itching, skin rash, contact dermatitis, rare – urticaria, angioneurotic edema, facial edema, photosensitivity, anaphylaxis, erythema multiforme exudative (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome).
Laboratory findings: hyperglycemia, hypoglycemia, increased serum creatine phosphokinase (CPK), albuminuria, increased activity of ACT, ALT.
Other: weight gain, gynecomastia, exacerbation of gout,
increased body temperature.
Treatment: No specific antidote, being symptomatic therapy. Hemodialysis is ineffective.
INTERACTION WITH OTHER DRUGS
The risk of myopathy during treatment with other drugs of this class is increased by the simultaneous use of cyclosporine, fibrates, erythromycin, antifungal agents belonging to the azole and niacin.
In simultaneous ingestion of primobolan depot for sale and a suspension containing magnesium and aluminum hydroxides, decreased primobolan depot for sale plasma concentrations approximately 35%, but the degree of decrease in cholesterol / LDL level is not changed.
With simultaneous use of primobolan depot for sale does not affect the pharmacokinetics of antipyrine, therefore, interactions with other drugs metabolized by the same cytochrome isozymes are not expected.
With simultaneous application of colestipol primobolan depot for sale plasma concentration decreased by about 25%. However, lipid-lowering effect of the combination of primobolan depot for sale and colestipol than that for each drug individually.
If readmission of digoxin and primobolan depot for sale 10 mg equilibrium concentration of digoxin in the blood plasma did not change. However, the application of digoxin in combination with primobolan depot for sale 80 mg / day.digoxin concentration increased by about 20%). Patients receiving digoxin in combination with primobolan depot for sale, should be observed.
With simultaneous use of primobolan depot for sale and erythromycin (500 mg four times / day) and clarithromycin (500 mg, 2 times / day), which inhibit cytochrome P450 3A4, was an increase in the concentration of primobolan depot for sale in plasma.
With simultaneous use of primobolan depot for sale (10 mg 1 time / day) and azithromycin (500 mg 1 times / day) of primobolan depot for sale plasma concentrations did not change.
primobolan depot for sale had no clinically significant effect on the concentration of terfenadine in the blood plasma, which is metabolized primarily by cytochrome P450 3A4; therefore it seems unlikely that primobolan depot for sale can significantly affect the pharmacokinetic parameters of other substrates cytochrome P450 3A4.
With simultaneous use of primobolan depot for sale and oral contraceptive containing norethindrone and ethinyl estradiol, showed a significant increase in AUC of norethindrone and ethinyl estradiol is about 30%> and 20% respectively. This effect should be considered when selecting an oral contraceptive for a woman receiving primobolan depot for sale.
not revealed the study of the interaction of primobolan depot for sale with warfarin and cimetidine evidence of clinically significant interaction.
With simultaneous use of primobolan depot for sale 80 mg and amlodipine 10 mg the pharmacokinetics of primobolan depot for sale at steady state did not change.
Simultaneous use of primobolan depot for sale with protease inhibitors, known as inhibitors of cytochrome P450 3A4, was accompanied by an increase in the concentration of primobolan depot for sale in plasma.
There were no clinically significant adverse interaction of primobolan depot for sale and antihypertensive agents, as well as estrogen. interaction studies with all specific drugs have not been conducted. Pharmaceutical incompatibility is not known.
Before therapy Atomaksom patient must assign a standard hypolipidemic diet, which he must comply during the entire treatment period.
The use of inhibitors of HMG-CoA reductase inhibitors to reduce the level of lipids in the blood can lead to changes in biochemical parameters that reflect the function of the liver. liver function should be monitored before treatment and after 6 weeks, 12 weeks after the start of Atomaksa and after each dose escalation, and periodically, for example every 6 months. The increased activity of “liver” enzymes in the serum can be observed during therapy Atomaksom. Patients in whom there is an increase in transaminase levels should be controlled to the level of enzymes return to normal. In that case, if the values of alanine aminotransferase (ALT) or asparaginaminotransferazy (ACT) is more than 3 times higher than the level of the upper allowable limit, it is advisable to reduce the dose Atomaksa or discontinue treatment.
Atomaks should be used with caution in patients who abuse alcohol and / or have liver disease. Active liver disease or persistent elevation of transaminases of unknown origin are contraindications to Atomaks purpose.
Treatment with primobolan depot for sale can cause myopathy. The diagnosis of myopathy (pain and weakness in the muscles, combined with increased activity of creatine phosphokinase (CPK) more than 10 times compared to the upper limit of normal) should be discussed in patients with widespread myalgia, muscle tenderness or weakness and / or marked increase in activity of CK. Patients should be warned that they should immediately inform your doctor about the appearance of unexplained pain or weakness in muscles, if accompanied by malaise or fever. Atomaksom Therapy should be discontinued in the event expressed increasing CPK or in the presence of confirmed or suspected myopathy. The risk of myopathy during treatment with other drugs in this class increased, while the use of cyclosporine, fibrates, erythromycin, niacin or azole antifungal agents. Many of these drugs inhibit metabolism mediated by cytochrome P450 3A4, and / or transport of drugs. primobolan depot for sale is biotransformed by the action of CYP 3A4. Appointing primobolan depot for sale in combination with fibrates, erythromycin, immunosuppressive agents, azole antifungals or niacin in lipid-lowering doses should carefully weigh the potential benefits and risks of treatment and regularly monitor patients to detect pain or weakness in muscles, especially during the first months of treatment and periods of increased doses of any drug. In such situations, we can recommend periodic determination of CPK activity, although such control does not prevent the development of severe myopathy.
When using primobolan depot for sale, as well as other tools in this class, cases of rhabdomyolysis described with acute renal failure due to myoglobinuria. Therapy Atomaksom should suspend or abolish the appearance of signs of a possible myopathy or presence of risk factors for renal failure with rhabdomyolysis (eg, severe acute infection, hypotension, major surgery, trauma, severe metabolic, endocrine and electrolyte disorders, and uncontrolled seizures).
Before therapy Atomaksom need to try to achieve adequate hypercholesterolemia control through diet therapy, physical activity, weight loss in obese patients, and the treatment of other conditions.
Patients should be warned that they should immediately consult a doctor if unexplained pain or weakness in muscles, especially if accompanied by malaise or fever.
Effects on driving ability and work with the mechanisms
About Atomaksa adverse impact on the ability to drive and work with the mechanisms have not been reported.
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