Pharmacological properties testosterone enanthate powder belongs to the bisphosphonate and is an analogue of the natural pyrophosphate.Bisphosphonates have high affinity for bone mineral components. The main mechanism of action of testosterone enanthate powder is to inhibit osteoclast activity and reduction mediated their bone resorption. The ability of testosterone enanthate powder to inhibit bone resorption in humans has been confirmed in the histological, kinetic and biochemical studies. However, the exact mechanisms of this process are not fully understood. testosterone enanthate powder inhibits osteoclast activity, reducing the concentration of calcium in blood serum, as well as the excretion of calcium and hydroxyproline in urine. In vitro bisphosphonates inhibit the precipitation of calcium phosphate, block its transformation into hydroxyapatite, delay aggregation of apatite crystals into larger crystals and slow down the dissolution of the crystals. when applying testosterone enanthate powder alone at doses sufficient to inhibit bone testosterone enanthate vs cypionate resorption, effects on normal human bone mineralization was not observed. In patients with breast cancer and multiple myeloma, a decrease likelihood of bone fractures. testosterone enanthate powder reduces the incidence of metastases in bone development during the primary breast cancer. In patients with operable breast cancer for the prevention of bone metastases was also observed reduction in mortality.
Absorption testosterone enanthate powder in the gastrointestinal tract is rapid and is approximately 2%. Maximum serum concentration after a single oral dose is reached after 30 minutes. Due testosterone enanthate powder pronounced affinity for calcium and other divalent cations testosterone enanthate powder absorption is greatly reduced while taking the drug with food or drugs containing divalent cations. When receiving testosterone enanthate powder inwardly beyond 1 hour before a meal relative bioavailability of 91%, for 30 minutes – 69%, respectively (thus lowering the bioavailability was not statistically significant). Significant variations in terms of absorbability testosterone enanthate powder in the gastrointestinal tract are also observed among the different patients and in one and the same patient. Although significant fluctuations in terms of absorption in the same patient, the amount obtained during the prolonged treatment of testosterone enanthate powder remains constant.
testosterone enanthate powder binding to plasma proteins is low.
Excretion testosterone enanthate powder from serum is characterized by two phases: the distribution phase with a half life of about 2 hours and elimination phase flowing very slowly as testosterone enanthate powder binds tightly with the bone tissue. testosterone enanthate powder is excreted mainly by the kidneys.
About 80% is determined in urine within a few days after ingestion. testosterone enanthate powder associated with bone tissue (about 20% of the absorbed dose), excreted more slowly. Renal clearance is approximately 75% of plasma clearance.
The explicit link between testosterone enanthate powder concentration in the blood plasma and the therapeutic effect or adverse reactions absent. The pharmacokinetic profile of the drug is not dependent on age, drug metabolism or functional abnormalities, renal failure, except causing a decrease renal clearance of testosterone enanthate powder.
- Osteolytic metastases of malignant tumors in the bone and multiple myeloma (multiple myeloma).
- Prevention of bone metastasis of primary breast cancer.
- Giperkatsiemiya caused by malignant tumors.
- Hypersensitivity to testosterone enanthate powder, other bisphosphonates, or any other components of the drug.
- Pregnancy and lactation.
- Concomitant therapy other bisphosphonates.
- Children’s age (due to the lack of clinical experience)
The use caution
Caution should be exercised when using the drug Bonefos in patients with impaired renal function.
Dosing and Administration
Inside, intravenous infusion
Capsules 400 mg should be swallowed without chewing. 800 mg tablets can be divided into two parts, but the two parts to be taken simultaneously. Do not crush or dissolve the tablets before taking.
The daily dose of 1600 mg is recommended to be taken once in the morning on an empty stomach, a glass of water. After dosing the patient must hour refrain from eating, drinking (except plain water) and the administration of other drugs.
When exceeding 1600 mg daily dose take it in two steps. The first dose should be taken as recommended above. The second dose should be taken between meals, two hours after and one hour before eating, drinking (except plain water) or ingestion of any whatsoever other drugs. Bonefos not be taken with milk, food, as well as preparations containing calcium or other divalent cations because they violate absorption testosterone enanthate powder.
To prepare the solution needed for the infusion dose dissolved in 500 ml of 0.9% sodium chloride solution or 5% solution dextrose.
Before and during treatment should ensure adequate intake of fluid to the patient, as well as to control the function of the kidneys and the calcium concentration in the serum. hypercalcemia due to malignancy.
- 300 mg intravenously for 2 hours (at least) every day (no more than 7 consecutive days) to reach a normal concentration of calcium in blood serum (usually occurs within 5 days) or 1500 mg intravenously over 4 hours once. If necessary, the infusion can be repeated or assign Bonefos inside. With the development of hypocalcemia recommended short break in treatment
- At impossibility of intravenous drug Bonefos appointed inside in an initial dose of 2400-3200 mg daily. By reducing the blood calcium to normal levels gradually reduce the dose of 1600 mg.
Prevention of bone metastasis of breast cancer primary
to 1600 mg daily inside. Osteolytic bone changes caused by malignant tumors without hypercalcemia. The dosage in each case is determined individually. The recommended starting dose is 1,600 mg per day. According to clinical indications, it may be increased as much as possible -. To 3200 mg per day, patients with renal failure Inside should not take the drug in doses exceeding 1600 mg per day, for an extended period of time. Should be reduced during the intravenous administration of a dose in accordance with the following recommendations:
|The degree of renal
ml / min
The most common, approximately 10% of patients, there are such side effects as nausea, vomiting, diarrhea; These reactions are usually mild and occur most often when using the drug in high doses.
These reactions may occur as the ingestion of the drug, and when it is administered intravenously, although the incidence of these reactions may vary. Disorders of metabolism : often – asymptomatic hypocalcemia rarely – hypocalcemia accompanied by clinical symptoms. Changes in the concentration of alkaline phosphatase in serum. Patients with metastatic level of alkaline phosphatase may be increased due to the presence of metastases in the liver and bone. Endocrine system : increasing the concentration of parathyroid hormone in the serum (usually in combination with a reduction in the level of calcium). The respiratory system : very rarely – y patients with asthma, with increased sensitivity to acetylsalicylic acid in the history of observed violations of respiratory function, bronchospasm. On the part of the digestive system :. frequently – nausea, vomiting and diarrhea are usually mild liver and biliary tract : often – increase in transaminases usually within the normal range, rarely – increased levels of aminotransferases, twice the normal rate, not accompanied by impaired liver function. on the part of the skin and its appendages : rarely – skin reactions, according to the clinical picture of the corresponding allergic reactions. From the urogenital system : rarely – a violation renal function (elevation of serum creatinine and proteinuria), severe renal insufficiency, especially after rapid intravenous infusion of high doses of clodronate.
In intravenous administration of high doses of acid clodronic reported an increase in creatinine serum concentration and impaired renal function. Should be symptomatic treatment in case of overdose. It is necessary to ensure the patient a sufficient amount of fluid, as well as monitoring of renal function and calcium content in serum.
Interaction with other drugs
There is evidence on the relationship between the intake of clodronate and the violation of the kidneys, while the appointment of non-steroidal anti-inflammatory drugs, most often diclofenac.
Due to the high likelihood of developing hypocalcemia, caution should be exercised in the appointment of clodronate together with aminoglycosides. It was reported that co-administration of estramustine phosphate with clodronate, increases the concentration of estramustine phosphate in the serum to 80%. Clodronate forms with divalent cations poorly soluble complexes, so simultaneous intake of foods or drugs containing divalent cations, such as antacids or iron preparations, leads to a significant reduction in the bioavailability of testosterone enanthate powder.
- During therapy the patient bonefos necessary to provide a sufficient amount of liquid. This is particularly important when assigning bonefos as an intravenous infusion, as well as for patients with hypercalcemia and renal insufficiency.
- Intravenous bonefos in doses considerably above the recommended may cause severe kidney damage, especially at too high infusion rates.
- The safety and efficacy of the drug for pediatric patients have not been proved.
Compatibility concentrate for infusion solution with other drugs or solutions for injection has not been studied. The drug should be diluted and administered only in accordance with these recommendations.
- Concentrate for solution for intravenous administration of 60 mg / ml: 5 ml glass ampoules of hydrolytic. 5 ampoules in the liner of the cardboard together with instructions for use placed in a cardboard box
- Tablets of 800 mg. 10 tablets in blisters (blister) PVC / aluminum foil. 6 blisters with instruction on use in carton box.
- Capsules 400 mg. 10 capsules in blister PVC / aluminum foil. At 100 capsules in a plastic bottle of high pressure polyethylene. At 3 or 6 blisters or each bottle with instructions for use in a pile of cardboard.
Another problem of using Enanthate is that it has a strong degree of aromatization, i. E. turns into estrogens. As a result, the body accumulates a lot of fat, and often there is gynecomastia. But here everything is strictly individual, tk. most of these phenomena are in a certain dependence on predisposition to them. There are athletes who, even at a dose of 1000 mg or more per day, do not suffer from feminization, fat testosterone enanthate powder accumulation and delay only a small amount of water if they are detained altogether, while others already complain of nipple pain when they see one ampoule of Testosterone Depot. Therefore, you should pay attention to the additional reception of Nolvadex and Proviron.
It’s good that in testosterone, as already mentioned above, they act on anyone, whether it’s a beginner or “Mr. Olympia”. TE also very strongly stimulates the body’s recovery processes. Therefore, it works well in terms of increasing vitality, obtaining additional energy and accelerating the phases of compensation. This is the reason that some athletes can train 6 times a week twice a day and at the same time manage to become more massive and stronger.
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