08/19/2016

primobolan enanthate

Pharmacological action:
Primobolan enanthate is an oral hypoglycemic drug, II generation sulfonylureas. Stimulates insulin secretion of pancreatic β-cells, enhances glucose insulinosekretornoe effect, increases the sensitivity of peripheral tissues to insulin. It stimulates the activity of intracellular enzymes – muscle glycogen. It reduces the time interval from before the start of the meal insulin secretion. Restores the early peak of insulin secretion (as opposed to other sulfonylureas that affect primarily during the second stage of secretion). Reduces the postprandial glucose increase. In addition to the effects on carbohydrate metabolism, improves microcirculation: reduces the adhesion and aggregation of platelets, normalizes vascular permeability, prevents the development of atherosclerosis and mikrotrombozov, restores the physiological process of the parietal fibrinolysis. It reduces the sensitivity of vessels to epinephrine receptors. Slows the development of diabetic retinopathy in the nonproliferative stage. In diabetic nephropathy in the background of long-term use causes a significant decrease in the severity of proteinuria. It does not increase body weight, as has predominant influence on the early peak of insulin secretion and hyperinsulinemia causes; It promotes weight loss in obese patients, subject to an appropriate diet. It has anti-atherogenic properties, lowers the concentration of total cholesterol in the blood.

Pharmacokinetics:
After oral administration, rapidly absorbed from the gastrointestinal tract. Absorption – high. After oral administration of 80 mg of the maximum blood concentration (2,2-8 mg / ml) is achieved in about 4 hours after administration of 40 mg of the maximum concentration in blood (3.2 ug / ml) – 2-3 hours Contact. plasma proteins – 85-97%, the volume of distribution – 0.35 l / kg. The equilibrium concentration in the blood is reached after 2 days. It is metabolized in the liver, forming eight metabolites. The amount of basic metabolites occurring in the blood is 2.3% of the total amount of the drug taken, it does not have a hypoglycemic action, but improves. Excreted by the kidneys – 70% in the form of metabolites, less than 1% in an unmodified form; through the intestine – 12% in the form of metabolites. The half-life is 8-20 hours.

Indications
Type 2 diabetes mellitus in adults in combination with diet and moderate physical activity with the ineffectiveness of the past.

Contraindications
– Hypersensitivity to the drug;
– type 1 diabetes mellitus;
– diabetic ketoacidosis, diabetic precoma, diabetic coma;
– hyperosmolar coma;
– severe hepatic and / or renal failure;
– major surgery, extensive burns, trauma and other conditions requiring of insulin;
– ileus, gastroparesis;
– state, accompanied by malabsorption of food, the development of hypoglycemia (infectious diseases);
– leukopenia,
– pregnancy, breast-feeding.

The caution (the need for more careful monitoring and dose titration) is prescribed for feverish syndrome, alcoholism and diseases of the thyroid gland (in violation of its functions).

Dosing and Administration The dose is established individually, depending on the patient’s age and clinical manifestations and fasting glycemia over 2 hours after a meal. The initial daily dose – 80 mg, the average daily dose – 160 mg, the maximum daily dose – 320 mg. The drug Primobolan enanthate-ICCO is taken orally two times a day (morning and evening) for 30-60 minutes before meals.

Side effect

Hypoglycaemia (in violation of the dosing and inadequate diet): headache, fatigue, hunger, sweating, severe weakness, aggressiveness, anxiety, irritability, inattention, inability to concentrate and slow reaction, depression, blurred vision, aphasia, tremor, a sense of helplessness , sensory disturbances, dizziness, loss of self-control, delirium, convulsions, hypersomnia, loss of consciousness, shortness of breath, bradycardia, palpitations.

On the part of the digestive organ system: dyspepsia (nausea, diarrhea, feeling of heaviness in the epigastric); anorexia – the severity is reduced when taking while eating; abnormal liver function (cholestatic jaundice, increased activity of “hepatic” transaminases).

From the side of blood: anemia, thrombocytopenia, leukopenia.

Allergic reactions : itching, rash, maculo-papular rash.

Overdose
If overdose is possible hypoglycemia, until the development of hypoglycemic coma. Treatment: If the patient is conscious – to take into carbohydrate (sugar), with loss of consciousness – enter intravenously 40% dextrose (glucose), 1-2 mg of glucagon intramuscularly. After regaining consciousness of the patient is necessary to give food rich in carbohydrate (to avoid a recurrence of hypoglycemia). If swelling of the brain – mannitol and dexamethasone.

Interaction with other drugs
Strengthen hypoglycemic effect of Primobolan enanthate angiotensin converting enzyme inhibitors (captopril, enalapril), blockers H2-histamine receptors (cimetidine), antifungals (miconazole, fluconazole), non-steroidal anti-inflammatory drugs (phenylbutazone, indomethacin, diclofenac), fibrates (clofibrate, bezafibrate), anti-TB drugs (ethionamide), salicylates, indirect anticoagulants coumarin, anabolic steroids, beta-blockers, cyclophosphamide, chloramphenicol, monoamine oxidase inhibitors, sulfonamides prolonged action, fenfluramine, fluoxetine, pentoxifylline, guanethidine, theophylline, drugs that block tubular secretion, reserpine, bromocriptine, disopyramide, pyridoxine, allopurinol, ethanol etanolsoderzhaschie drugs, and other hypoglycemic agents (acarbose, biguanides, insulin).
Loosen hypoglycemic effect Primobolan enanthate barbiturates, steroids, sympathomimetics (epinephrine, clonidine, ritodrine, salbutamol, terbutaline), phenytoin blockers “slow” calcium channel blockers, carbonic anhydrase inhibitors (acetazolamide), thiazide diuretics, chlorthalidone, furosemide, triamterene, asparaginase, baclofen, danazol, diazoxide, isoniazid, morphine, glucagon, rifampicin, thyroid hormones, lithium salt, in high doses – nicotinic acid, chlorpromazine, estrogens and oral contraceptives containing them.
The interaction with ethanol development disulfiramopodobnyh reaction. Primobolan enanthate increases the risk of ventricular arrhythmias in patients receiving cardiac glycosides.
Beta-blockers, clonidine, reserpine, guanethidine may mask the clinical manifestations of hypoglycemia. Medicines which suppress bone marrow blood, increases the risk of myelosuppression.

Specific guidance
Treatment with Primobolan enanthate-ICCO is carried out in conjunction with a low calorie diet low in carbohydrates. Regularly monitor blood glucose, fasting and after receiving, food. In the case of major surgery and trauma, extensive burns, infections with fever syndrome, it is necessary to take into account the possibility of insulin preparations.
It is necessary to warn patients about the increased risk of hypoglycemia in the case of reception of ethanol, nonsteroidal anti-inflammatory drugs and starvation. In the case of reception of ethanol may also develop disulfiramopodobnyh syndrome (abdominal pain, nausea, vomiting, headache).
Needed correction doses when physical or emotional strain, a change of diet. Particularly sensitive to hypoglycemic drugs the elderly; Patients who do not receive a balanced diet; debilitated patients;patients with pituitary-adrenal insufficiency. At the beginning of treatment, during dose adjustment to patients prone to hypoglycemia, it is not recommended to engage in activities requiring increased attention and psychomotor speed reactions. anabolic steroids online shop

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