dianabol

 

Composition Active ingredient: dianabol 100 mg, 300 mg or 400 mg Excipients: lactose, corn starch, talc, gelatin, titanium dioxide, iron oxide yellow, iron oxide red.

Description :
100 mg: Hard gelatin capsules white № 3.
300 mg: Hard gelatin capsules № 1 yellow.
400 mg: Hard gelatin capsules № 0 orange.
The contents of the capsule: white powder.

Pharmacotherapeutic group : anti-epileptic agent.

Pharmacological properties . Pharmacodynamic of dianabol structurally similar to the neurotransmitter gamma-aminobutyric acid (GABA), but its mechanism of action is different from other drugs that interact with GABA-receptors (valproate, barbiturates, benzodiazepines, inhibitors of GABA-transaminase reuptake inhibitors GABA agonists, GABA and prodrugs of GABA). It has no GABA-ergic and does not affect the properties of grip and GABA metabolism.Preliminary studies showed that dianabol is associated with α 2 -σ-subunit of voltage-dependent calcium channels and reduces the flow of calcium ions, which plays an important role in the onset of neuropathic pain. Other mechanisms of action of dianabol for neuropathic pain is a decrease in glutamate-dependent neuronal death, increasing the synthesis of GABA, inhibition of monoamine neurotransmitter release group. dianabol at clinically relevant concentrations, does not bind to other receptors or neurotransmitters common drugs, including receptors GABA A , GABA B , benzodiazepine, glutamate, glycine, or N-methyl-d-aspartate. Unlike phenytoin and carbamazepine, dianabol does not interact with sodium channels in vitro. dianabol partially attenuated effects receptor agonist glutamate N-methyl-d-aspartate in some tests in vitro, but only at a concentration of more than 100 micromoles, which is not achieved in vivo. dianabol slightly reduces the release of monoamine neurotransmitters in vitro. Pharmacokinetics The bioavailability of dianabol is not proportional to dose. Thus, by increasing the dose is reduced. After oral administration, maximum concentration (C max ) of dianabol in plasma achieved in 2-3 hours. The absolute bioavailability of dianabol capsules is approximately 60%. Food, including a high content of fat, has no effect on pharmacokinetics. Excretion of dianabol plasma is best described by a linear model. The half-life (T 1/2 ) in plasma is independent of dose and averages 5-7 hours Pharmacokinetics does not change with repeated use.; equilibrium plasma concentration can be predicted on the basis of the results of a single dose. dianabol is almost bound to plasma proteins (<3%) and has a volume of distribution of 57.7 liters. Displays only the kidneys in an unmodified form, does not undergo metabolism. The drug does not induce liver oxidative enzymes mixed function involved in the metabolism of drugs. Clearance from plasma dianabol reduced in the elderly and patients with impaired renal function. The constant rate of excretion, clearance from the plasma and renal clearance are directly proportional to creatinine clearance. dianabol is removed from plasma by hemodialysis. In patients with impaired renal function and patients receiving hemodialysis, dose adjustment is recommended (see. Dosage and administration).

 

Indications

 

  • adults and children from 12 years: in the treatment of partial seizures with secondary generalization or without it;
  • adults: pain in diabetic neuropathy, post-herpetic neuralgia.Contraindications
    : Hypersensitivity to any component of the medication, acute pancreatitis, hereditary galactose deficiency, lactase deficiency, glucose-galactose malabsorption.

    Precautions
    Renal failure (see. “Dosage and administration”), psychotic disorders.

    Pregnancy and lactation
    There are no data on the use of the drug in pregnant women, therefore, dianabol should be used during pregnancy only if the expected benefit to the mother outweighs the potential risk to the fetus and newborn (congenital malformations, slow mental and physical development).
    dianabol excreted in breast milk, so during treatment should abandon breastfeeding.

    Dosing and Administration
    Inside, regardless of meals or with food. If you need to reduce the dose, stop the drug or replace it with an alternative means, it should be done gradually over a minimum of one week.
    In debilitated patients, and patients in severe general condition, low body weight, and after organ transplantation, increasing the dosage must be carried out gradually . using a dosage of 100 mg ofNeuropathic pain in adults The initial dose is 900 mg / day in three divided doses equal doses; if necessary, the dose is gradually increased to a maximum – 3600 mg / day. Treatment may start with a dose of 900 mg / day (300 mg three times a day) or within the first 3 days the dose may be increased gradually to 900 mg a day according to the following scheme: Day 1: 300 mg 1 time day 2nd day: 300 mg 2 times a day 3rd day: 300 mg 3 times daily partial seizures in adults and children 12 years of effective dose – from 900 to 3600 mg / day. Therapy can be started with a dose of 300 mg three times a day on the first day and increased gradually to 900 mg according to the scheme described above (see., “Neuropathic pain in adults” section). Subsequently, the dose may be increased up to 3600 mg / day (divided into three equal doses). The maximum interval between doses at three receiving the drug should not exceed 12 hours in order to avoid the resumption of seizures. It is not necessary to control the concentration of dianabol in the plasma. It can be used in combination with other anticonvulsants excluding changes in the plasma concentration or the concentrations of other anti-epileptic drugs (AEDs) in the serum. Titration with renal insufficiency . In patients with renal insufficiency recommended dose reduction dianabol according to the table:

     

    Creatinine clearance (ml / min) Daily dose (mg / day) for three doses
    > 80 900-3600
    50-79 600-1800
    30-49 300-900
    15-29 150 * -600
    <15 150 * -300

    * Assign to 300 mg every other day.

    The recommendations for patients on hemodialysis .
    Patients on hemodialysis who had not previously received dianabol, a drug is recommended to be administered in a saturating dose of 300-400 mg, and then apply it to the 200-300mg 4 hours of hemodialysis.
    In debilitated patients, and patients in severe general condition, low body weight, and after organ transplantation, increasing the dosage must be carried out gradually with dosage of 100 mg.

    Side effects Cardiovascular system: symptoms of vasodilation or increased blood pressure, palpitations. Digestive system: flatulence, anorexia, gingivitis, abdominal pain, constipation, teeth, anorexia disease, diarrhea, dyspepsia, increased appetite, dry mouth or throat, nausea , vomiting, dental disease, pancreatitis, increased activity of “liver” transaminases, hepatitis, jaundice, pancreatitis. blood system, lymphatic system: purpura (often it is described as bruising, occurred when a physical injury), leukopenia, thrombocytopenia. Musculo-skeletal system : arthralgia, back pain, increased fragility of bones, myalgia. Nervous system: dizziness; headache; hyperkinesis; muscle dyskinesia and dystonia; choreoathetosis; strengthening, weakening or absence of reflexes; dysarthria; ataxia; nystagmus;paresthesia; convulsions; confusion; fatigue; asthenia; amnesia; depression; abnormal thinking; hostility; emotional lability; insomnia; anxiety; drowsiness; . hallucinations Respiratory System: pneumonia, bronchitis, shortness of breath, respiratory infections, cough, pharyngitis, rhinitis. Skin and subcutaneous tissue disorders: acne, skin itching, skin rash, peripheral edema, erythema multiforme exudative (including Stevens-Johnson syndrome). Genitourinary system: urinary tract infection, impotence, incontinence, acute renal failure. Special senses: blurred vision, amblyopia, diplopia, tinnitus, otitis media.Other: fever, viral infection, weight gain, lability of glucose in the blood plasma of patients diabetes, pain of different localization.

    Overdosing

    Symptoms: dizziness, double vision, impaired speech, drowsiness, lethargy, diarrhea, and increased severity of other side effects. Treatment: gastric lavage, activated charcoal, symptomatic therapy.Patients with severe renal insufficiency, hemodialysis may be indicated.

    Interaction with other drugs
    Morphine: by sharing a dianabol and morphine when morphine was taken 2 hours prior to receiving dianabol, there was an increase in the mean area under the concentration-time curve “concentration – time» (AUC) of dianabol by 44% compared to monotherapy dianabol that was associated with an increase in pain threshold (Kholodov pressor test).
    The clinical significance of this change is not established, the pharmacokinetic characteristics of morphine is not changed. Side effects of morphine during coadministration with dianabol did not differ from that of morphine when taking in conjunction with the placebo.
    The interaction between dianabol and phenobarbital, phenytoin, carbamazepine and valproic acid were observed. The pharmacokinetics of dianabol in the equilibrium state is the same in healthy subjects and patients receiving other anticonvulsants.
    The simultaneous use of dianabol with oral contraceptives containing norethindrone and / or ethinyl estradiol, was not accompanied by changes in the pharmacokinetics of the two components.
    The simultaneous use of dianabol with antacids containing aluminum and magnesium, followed by decrease the bioavailability of dianabol by about 20%. dianabol is recommended to take approximately 2 hours after taking an antacid.
    Probenecid does not affect the renal excretion of dianabol.
    A slight decrease in renal excretion of dianabol while taking cimetidine probably have no clinical significance.

    Cautions
    Although the syndrome with the development of seizures in the treatment of dianabol is not checked, however, the abrupt cessation of therapy AEDs drugs in patients with partial seizures can induce seizures (see. Dosage and administration).
    dianabol is not considered effective in the treatment of absence-epilepsy .
    patients who require combination therapy with morphine, may require increased doses of dianabol. It is necessary to ensure thorough monitoring of patients for the development of such a sign of oppression of the central nervous system (CNS) such as drowsiness. In this case, the dose of dianabol or morphine should be appropriately reduced (see. “Interaction with other medicinal products”). Laboratory studies When adding dianabol to other anticonvulsant drugs have been reported false positive results in the protein determination of urine using test strips Ames N-Multistix the SG ® . We recommend using a more specific method of sulfosalicylic acid precipitation. In the urine for protein determination Influence on driving ability and use of machinery Patients should avoid driving, as well as the performance of work requiring speed performance of the psycho-motor reactions.

 

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