The drug Rastan, the active substance of which is somatotropic hormone (GH), is one of the few medications in its series officially registered in Russia. It can be purchased at a pharmacy, but only with a doctor's prescription.
The basis of the drug is somatropin, the second name of which is growth hormone - reveals the primary purpose of the drug. In medicine, it is prescribed mainly to children with a lack of normal physiological growth. The medication not only stimulates the growth of skeletal bones, but also improves their metabolism, improving the mineral composition and structure. Therefore, its use is possible for patients with osteoporosis.
Peculiarity! Recent studies of the hormone confirm its anti-aging effect. Somatropin has a promising future, doctors say and continue to study it.
The effectiveness of GH is due to its transformation into IGF-1 (insulin-like growth factor), which is associated with protein, which leads to active cell division of muscles, liver, adrenal glands, thyroid and gonads. The main character of the computer game with the same name of the drug Rastan Saga II is the living embodiment of the anabolic effect of the drug:
- increased muscle volume and decreased fat tissue volume;
- tall height and proportional body build;
- enlarged, clearly visible pattern of muscle ligaments and fibers.
Rastan is produced not in tablets, but in the form of a dry substance - lyophilisate, which is dissolved, as well as in a liquid form ready for injection. The hormone solution is placed in a cartridge and removed using a syringe. Typically, BiomaticPen is used, which comes from the same manufacturer as Rastan himself. In appearance, the syringe resembles a writing pen and is easy to use due to the thin needle and sound alert when drawing a solution and moving to the next mark when dosing. Despite the significant advantages: painlessness during administration, precise dosage, information display, ease of use, in bodybuilding the hormone is mainly diluted independently, since the price of a pen syringe is on average from 2000 rubles. and higher, and it can only be used with cartridges from .
Important! After each injection, the needle must be disposed of and a new one used next time. In order to save money, it is prohibited to use the same needle.
pharmachologic effect
Antiaggregant, vasodilator.
The drug PGE1 improves microcirculation and peripheral circulation and has a vasoprotective effect. When administered systemically, it causes relaxation of smooth muscle fibers, has a vasodilating effect, and reduces peripheral vascular resistance without changing blood pressure. In this case, there is a reflex increase in cardiac output and heart rate. Helps increase the elasticity of red blood cells, reduces platelet aggregation and neutrophil activity, increases the fibrinolytic activity of the blood. Has a stimulating effect on the smooth muscles of the intestines, bladder, and uterus; suppresses the secretion of gastric juice.
PGE1 is used in combination with alpha-cyclodextrin IV or IV. During the preparation of the solution, the drug complex breaks down into its component parts - PGE1 and alpha-cyclodextrin. With intravenous administration, a therapeutically significant concentration of the active substance is achieved soon after the start of drug administration, and Cmax in the blood plasma is achieved within 2 hours from the start of administration. PGE 1 is an endogenous substance with an exceptionally short T1/2 - the concentration in the blood plasma returns to its original level within 10 s after cessation of administration. The process of biotransformation of PGE 1 occurs mainly in the lungs; during the “first pass” through the lungs, 60–90% of the active substance is metabolized with the formation of the main metabolites - 15-keto - PGE1, 15-keto - PGE0 and PGE0. The main metabolic products are excreted by the kidneys - 88% and through the gastrointestinal tract - 12% within 72 hours. 93% of PGE1 binds to plasma proteins. Alpha-cyclodextrin has a half-life of about 7 minutes and is excreted unchanged by the kidneys.
Release form, packaging and composition of the drug Rastan®
Lyophilisate for preparing a solution for subcutaneous administration
white or white with a yellowish tint; the attached solvent is a clear, colorless or slightly colored liquid.
1 fl. | |
human somatropin | 4 IU (1.33 mg) |
Excipients
: mannitol, glycine, sodium dihydrogen phosphate dihydrate, sodium hydroxide.
Solvent:
metacresol (3 mg), water d/i (1 ml).
Glass bottles with a capacity of 5 ml (1) complete with solvent (1 ml bottle 1 pc.) - cardboard packs. Glass bottles with a capacity of 5 ml (1) complete with solvent (1 ml bottle, 1 pc.) - contour cell packaging (1) - cardboard packs.
Lyophilisate for preparing a solution for subcutaneous administration
white or white with a yellowish tint; the attached solvent is a clear, colorless or slightly colored liquid.
1 fl. | |
human somatropin | 16 IU (5.33 mg) |
Excipients
: mannitol, glycine, sodium dihydrogen phosphate dihydrate, sodium hydroxide.
Solvent:
metacresol (3 mg), water d/i (1 ml).
Glass bottles (1) complete with solvent (1 ml bottle, 1 pc.) - cardboard packs. Glass bottles (1) complete with solvent (2 ml bottle, 1 pc.) - cardboard packs. Glass bottles (1) complete with solvent (1 ml bottle, 1 pc.) - contour cell packaging (1) - cardboard packs. Glass bottles (1) complete with solvent (2 ml bottle, 1 pc.) - contour cell packaging (1) - cardboard packs.
Lyophilisate for preparing a solution for subcutaneous administration
white or white with a yellowish tint; the attached solvent is a clear, colorless or slightly colored liquid.
1 fl. | |
human somatropin | 20 IU (6.67 mg) |
Excipients
: mannitol, glycine, sodium dihydrogen phosphate dihydrate, sodium hydroxide.
Solvent:
metacresol (3 mg), water d/i (1 ml).
Glass bottles (1) complete with solvent (1 ml bottle, 1 pc.) - cardboard packs. Glass bottles (1) complete with solvent (2 ml bottle, 1 pc.) - cardboard packs. Glass bottles (1) complete with solvent (1 ml bottle, 1 pc.) - contour cell packaging (1) - cardboard packs. Glass bottles (1) complete with solvent (2 ml bottle, 1 pc.) - contour cell packaging (1) - cardboard packs.
Directions for use and doses
V/a introduction. Dissolve the contents of 1 ampoule of Vazaprostan® lyophilisate (corresponding to 20 mcg of alprostadil) in 50 ml of physiological solution.
In the absence of other prescriptions, half the contents of the Vazaprostan® ampoule (corresponding to 10 mcg of alprostadil) are administered intravenously over 60–120 minutes using an infusion device. If necessary, especially in the presence of necrosis, under strict tolerance control, it is possible to increase the dose to 20 mcg of alprostadil (contents of 1 ampoule). This dosage is usually used as a single daily infusion.
If intravenous infusion is administered through an inserted catheter, depending on tolerability and severity of the disease, a dose of 0.1–0.6 ng/kg/min is recommended over 12 hours using an infusion device (corresponding to 0.25–0.6 ng/kg/min). 1.5 ampoules of Vazaprostan).
IV infusion. Dissolve the contents of 2 ampoules of Vazaprostan® lyophilisate (corresponding to 40 μg of alprostadil) in 50–250 ml of physiological solution and administer the resulting solution intravenously for 2 hours 2 times a day or 3 ampoules (60 μg of alprostadil) for 3 hours 1 time per day day.
In patients with impaired renal function (renal failure with a creatinine level of more than 1.5 mg/dL), intravenous administration begins with 20 mcg over 2 hours. If necessary, after 2-3 days the single dose is increased to 40-60 mcg.
For patients with renal and heart failure, the maximum volume of fluid administered is 50–100 ml/day. The course of treatment is 4 weeks.
The duration of treatment is on average 14 days; if the effect is positive, treatment with the drug can be continued for another 7–14 days. If there is no positive effect within 2 weeks from the start of treatment, further use of the drug should be discontinued.
Preparation of the solution. The solution must be prepared immediately before the infusion. The lyophilisate dissolves immediately after adding saline. At first, the solution may turn out milky-cloudy. This effect is created by air bubbles and has no significance. After a short time the solution becomes transparent. Do not use a solution prepared more than 12 hours ago.
Rastan: important points of instruction
The instructions for use indicate groups of people who are contraindicated in taking the drug:
- with special sensitivity to the main active ingredient and additional ones;
- with intracranial tumors (if they are inactive, use is possible only under the supervision of a doctor);
- with urgent (critical) conditions after surgical interventions in the abdominal cavity, heart function, etc.;
- pregnant and breastfeeding women.
Only in case of constant medical diagnostic control can Rastan be used:
- for diabetes mellitus (dosage adjustment of hypoglycemic drugs taken simultaneously with Rastan may be required);
- for hypertension (high blood pressure requires regular monitoring of the fundus; in case of papilledema, the appointment is canceled);
- when interacting with glucocorticosteroids (GCS). The hormone increases the rate of purification of steroids from the blood, and they, in turn, reduce the effect of triggered growth processes;
- with hypothyroidism (long-term lack of hormones produced by the thyroid gland);
- with Prader-Willi syndrome.
The dose taken is calculated individually, taking into account the manifestations of growth hormone deficiency, the desired result and the age of the recipient. For children, on average - 2-3 IU per day, for adults - 0.45-0.9 IU per day, with subsequent dose changes depending on the effect. Traditional maintenance dosage usually does not exceed 3 IU per day.
Please note! When selecting the optimal dose concentration, experts advise paying attention to the level of IGF-1 in the blood serum.
Mix the lyophilisate with water for injection with caution, pointing the syringe with the solution at the wall of the bottle and not into the powder. Do not shake, but shake, until it dissolves. If you use a syringe pen, you should remember that “1” on the indicator equals 0.05 mg of the hormone, and the maximum value “60” corresponds to 3 mg. Thus, the formula is applicable: X * 0.05 = number of mg of the drug, where X is equal to the numerical value on the electronic display.
The medication should be injected subcutaneously into the abdomen, shoulders or thigh area, using your fingers to form a small fold in the skin. After the injection, it is necessary to leave the needle under the skin for 6-10 seconds with the syringe button pressed to prevent incomplete use of the medicine and limit the entry of blood into the needle.
Please note! Before puncturing with a needle, it is necessary to pre-disinfect all rubber surfaces of the drug bottles and cartridges each time.
Storage conditions for somatropin require strict adherence to temperature conditions. Both powder and liquid forms should be stored in a cool, dry place between 2-8°C.
If you forgot to put the hormone in the dry substance in the refrigerator, then it must be used within 1 month, but the prepared solution, when left in a warm place, loses all its effectiveness and becomes useless. The prepared open solution, stored in the refrigerator, should be used within 28 days.
Please note! Sub-zero temperatures lead to loss of quality of growth hormone. The product cannot be placed in the freezer.
Side effects from taking Rastan are as follows:
- delayed fluid outflow, which contributes to the appearance of edema, joint stiffness (impaired mobility), arthralgia (joint pain), myalgia (inflammation of muscle fibers);
- allergic reactions;
- hyperglycemia (excess blood sugar);
- headache, lack of sleep, carpal tunnel syndrome (inflammation of the median nerve);
- gynecomastia (female breast swelling).
Contraindications
Hypersensitivity to alprostadil and other components of the drug, chronic heart failure, severe cardiac arrhythmias, exacerbation of coronary artery disease, previous myocardial infarction (within the next 6 months), pulmonary edema, infiltrative pulmonary disease, chronic obstructive pulmonary disease, liver dysfunction (increased AST levels , ALT or GGT) and a history of liver disease, as well as diseases accompanied by an increased risk of bleeding and hemorrhage (peptic ulcer of the stomach or duodenum, severe cerebral vascular damage, proliferative retinopathy with a tendency to bleed, extensive trauma, etc. ), concomitant therapy with vasodilators and anticoagulants, pregnancy, breastfeeding.
Contraindicated during pregnancy. Breastfeeding should be stopped during treatment.
Overdose
Symptoms: decreased blood pressure, increased heart rate. Vasovagal reactions may develop with pallor of the skin, increased sweating, nausea and vomiting, which may be accompanied by myocardial ischemia and symptoms of heart failure, as well as possible pain, swelling and redness of the tissue at the infusion site.
Treatment: it is necessary to reduce the dose of the drug or stop the infusion. If there is a pronounced decrease in blood pressure, the patient in a lying position needs to raise his legs. If symptoms persist, sympathomimetics should be used.
Precautionary measures
Use Vazaprostan® with caution in case of arterial hypotension, cardiovascular failure (special attention should be paid to monitoring the load with the volume of the carrier solution), in patients on hemodialysis (treatment with the drug should be carried out in the post-dialysis period), in patients with type 1 diabetes mellitus, especially with extensive vascular lesions.
Vazaprostan® may affect the ability to actively participate in street traffic or operate machinery, especially at the beginning of treatment, with increasing doses and withdrawal of the drug, as well as with simultaneous intake of alcohol.
Pharmacological properties of the drug Rastan
Somatropin (human growth hormone) is a single-chain polypeptide consisting of 191 amino acid residues, produced by the genetically modified culture of Escherichia coli BL21(DE3)/pESl-6. Stimulates the growth of skeletal bones, affecting the epiphyseal plates of tubular bones and bone tissue metabolism. In patients with growth hormone deficiency and osteoporosis, replacement therapy leads to normalization of mineral composition and bone density. Increases the number and size of cells in muscles, liver, thymus, gonads, adrenal glands, and thyroid gland. Stimulates the transport of amino acids into the cell and protein synthesis, reduces the level of cholesterol in the blood serum, affects the spectrum of lipids and lipoproteins. Suppresses insulin release. Promotes the retention of sodium, potassium and phosphorus. Increases body weight, muscle strength and physical endurance. 80% of the drug administered subcutaneously is absorbed, the maximum concentration in the blood serum is reached after 4–6 hours. The half-life is 3 hours.
Side effects
From the nervous system: headache, convulsive syndrome, dizziness, increased fatigue, feeling of malaise, impaired sensitivity of the skin and mucous membranes.
From the cardiovascular system: decreased blood pressure, chest pain, heart rhythm disturbances, AV block.
From the digestive system: a feeling of discomfort in the epigastric region, dyspeptic symptoms - diarrhea, nausea, vomiting.
From the musculoskeletal system: hyperostosis of long tubular bones (with treatment for more than 4 weeks).
Local reactions: pain, swelling, erythema, sensory disturbance, phlebitis (proximal to the IV injection site).
Laboratory indicators: leukocytosis, leukopenia, increased titer of C-reactive protein, increased transaminase levels.
Other: increased sweating, hyperthermia, swelling of the limb into which the infusion is administered.
Rarely: joint pain, confusion, central convulsions, fever, chills, bradypnea, arthralgia, psychosis, renal failure, anuria. Several cases of pulmonary edema and acute left ventricular failure have been reported.
Extremely rare (up to 1% of cases): shock, acute heart failure, hyperbilirubinemia, bleeding, drowsiness, bradypnea, decreased respiratory function, tachypnea, anuria, renal dysfunction, hypoglycemia, ventricular fibrillation, 2nd degree AV block, supraventricular arrhythmia, tension neck muscles, increased irritability, hypothermia, hypercapnia, skin hyperemia, hematuria, peritoneal symptoms, tachyphylaxis, hyperkalemia, thrombocytopenia, anemia.
Allergic reactions: skin rash, itching.
Side effects associated with the use of the drug or with the catheterization procedure itself disappear after reducing the dose or stopping the infusion.
special instructions
Alprostadil can only be used by doctors who have experience in angiology, are familiar with modern methods of continuous monitoring of the cardiovascular system and have the appropriate equipment for this.
During the treatment period, it is necessary to monitor blood pressure, heart rate, biochemical blood parameters, and the blood coagulation system (in case of disorders of the blood coagulation system or during simultaneous therapy with drugs that affect the coagulation system).
Patients with coronary artery disease, as well as patients with peripheral edema and renal dysfunction (serum creatinine >1.5 mg/dL) should be monitored in the hospital during treatment with Vazaprostan® for 1 day after stopping its use.
To avoid the appearance of symptoms of overhydration in patients with renal failure, the volume of fluid administered should, if possible, not exceed 50–100 ml/day. Dynamic monitoring of the patient's condition is mandatory: monitoring blood pressure and heart rate, and, if necessary, monitoring body weight, fluid balance, measuring central venous pressure or conducting an echocardiographic study.
Phlebitis (proximal to the injection site), as a rule, is not a reason to discontinue therapy; signs of inflammation disappear a few hours after stopping the infusion or changing the injection site; specific treatment is not required in such cases. Central vein catheterization can reduce the incidence of this side effect of the drug.
If the ampoule is damaged, the lyophilisate becomes wet and sticky, and greatly decreases in volume. In this case, the drug cannot be used.
Special instructions for the use of the drug Rastan
During treatment with Rastan, it may be necessary to adjust the doses of hypoglycemic drugs in patients with diabetes, manifestation of latent hypothyroidism may occur, and in patients receiving thyroxine, signs of hyperthyroidism may appear. During treatment, it is necessary to monitor the condition of the fundus, especially with symptoms of intracranial hypertension. Swelling of the optic nerve requires discontinuation of the drug. Detection of lameness during Rastan therapy requires careful monitoring. It is necessary to change the sites of subcutaneous injections due to the possibility of developing lipoatrophy.
Drug interactions
Vazaprostan® may enhance the effect of antihypertensive drugs, vasodilators and antianginal drugs. The simultaneous use of Vazaprostan® in patients taking drugs that prevent blood clotting (anticoagulants, platelet aggregation inhibitors) may increase the likelihood of bleeding. In combination with cefamandole, cefoperazone, cefotetan and thrombolytics, it increases the risk of bleeding. Sympathomimetics - adrenaline, norepinephrine - reduce the vasodilating effect.
It must be taken into account that drug interactions are possible even if the above drugs were used shortly before Vazaprostan® therapy was started.
Application of Rastan: reviews of those who took it
Use in bodybuilding is explained by its ability to reduce fat. Users also report stronger joints and muscles, resulting in fewer workout injuries. To increase muscle volume, athletes recommend the parallel use of steroids, and in this case it is necessary to remember their inhibitory interaction with each other. At the same time, there are reviews from athletes who do not observe a significant increase in endurance and strength. Among the advantages are the ease of use of the ready-made solution and the trustworthy factory packaging of the drug.
The downside for many was the high price of pharmacy products. Compared to other growth hormone preparations, purchasing Rastan for a course is more expensive.