The mechanism of action of fluoxymesterone halotestin – a specific inhibitor of the reuptake of serotonin (5-HT). He has very little effect on the reuptake of noradrenaline and dopamine. At therapeutic doses, fluoxymesterone halotestin blocks uptake of serotonin in human platelets. He has no stimulating, sedative or anticholinergic action. fluoxymesterone halotestin has no affinity for muscarinic (cholinergic), serotonergic, dopaminergic, adrenergic, histaminergic, GABA – or benzodiazepine receptors.
Antidepressant effect was seen at the end of the second week of the regular intake of fluoxymesterone halotestin, while the maximum effect is achieved only after 6 weeks. Unlike tricyclic antidepressants, fluoxymesterone halotestin when assigning no increase in body weight. fluoxymesterone halotestin does not cause mental or physical drug dependence.
Absorption of fluoxymesterone halotestin from the gastrointestinal tract significantly, but is slow. Maximum plasma concentration is achieved through 4,5-8,4 hours after ingestion of the drug. The equilibrium fluoxymesterone halotestin concentration in plasma is achieved within weeks after a single daily intake. Bioavailability in increased food intake by 25%, while the time to reach maximum concentration is shortened. Distribution. Total binding fluoxymesterone halotestin protein is 98%. The volume of distribution of> 20 l / kg.
Metabolism and excretion. fluoxymesterone halotestin is extensively metabolized during the first passage through the liver, subjected to N-demethylation. Its main metabolite – N-desmetilsertralin less active as compared to the parent compound. The metabolites are excreted with urine and feces in equivalent amounts. About 0.2% of fluoxymesterone halotestin excreted by the kidneys unchanged. Half-life time is 22-36 hours, regardless of age or sex. For N-desmetilsertralina this figure is 62-104 hours.
Half-life of fluoxymesterone halotestin and the area under the plasma concentration curve (AUC) increase with abnormal liver function. Regardless of the severity of renal failure the pharmacokinetics of fluoxymesterone halotestin in his constant use is not changed. fluoxymesterone halotestin passes into breast milk. Data about its ability to pass through the blood-barrier is not. fluoxymesterone halotestin is not dialyzed.
- Depression of various etiologies (prevention and treatment), including anxiety accompanied);
- obsessive – compulsive disorder (OCD); panic disorder; post-traumatic stress disorder (PTSD).
- Hypersensitivity to the active substance or any other ingredients in the composition of the drug;
- concomitant use of fluoxymesterone halotestin and MAOIs (monoamine oxidase). When replacing one drug to another should avoid antidepressants within 14 days;
- concomitant use of fluoxymesterone halotestin with tryptophan or fenfluramine;
- unstable epilepsy;
- Children under 6 years of age;
- pregnancy and lactation.
Precautions: neurological disorders (including mental retardation), manic state, epilepsy, liver and / or kidney failure, a decrease in body weight, children over 6 years.
Pregnancy and lactation
Controlled results of the application of fluoxymesterone halotestin in pregnant women do not have, so the drug should assign them only if the expected benefit to the mother outweighs the potential risk to the fetus. fluoxymesterone halotestin is found in breast milk, and therefore, treatment with this drug is not recommended during breast-feeding. No reliable data on safety of its use in this case. If treatment is necessary, it is better to stop breast-feeding.
Dosing and Administration
Inside, regardless of meals.
Depression and OCD
starting dose is 50 mg fluoxymesterone halotestin once a day, in the morning or evening. The daily dose can be gradually, not earlier than one week, increased from 50 mg to a maximum daily dose of 200 mg.
Panic disorder PTSD
The initial dose is 25 mg fluoxymesterone halotestin once a day, morning or evening. One week dose can be increased to 50 mg 1 time per day and then gradually, not earlier than one week, the daily dose can be gradually increased from 50 mg up to a maximum daily dose of 200 mg.
A satisfactory therapeutic results achieved typically after 7 days from start treatment. However, to achieve full therapeutic effect requires the regular intake of the drug for 2-4 weeks. Patients with obsessive-compulsive disorder to achieve a good result may require 8-12 weeks. The minimum dose that provides the therapeutic effect is retained in the future as a support.
For children from 6 to 12 years, the starting dose is 25 mg fluoxymesterone halotestin once a day, morning or evening. After one week the dose can be increased to 50 mg once a day. For children aged 12 to 17 years of the initial dose is 50 mg once a day, in the morning or evening. The daily dose can be gradually, not earlier than one week, increased from 50 mg to a maximum daily dose of 200 mg. To avoid overdose should take into account the smaller body weight in children compared to adults, and by increasing the dose of 50 mg / day should be carefully monitored for this category of patients and stop the drug at the first sign of overdose.
In elderly patients there is no need for a special dose selection. Patients with impaired hepatic function require special attention in the treatment of fluoxymesterone halotestin. In severe liver function disorder the dose should be reduced or increased intervals between doses. In patients with impaired renal function specially select a dose is not required.
On the part of the digestive system: dry mouth, decreased appetite (rarely – increased) up to anorexia, dyspepsia (bloating, nausea, vomiting, diarrhea or unstable stool, constipation), stomach cramps, abdominal pain, pancreatitis, hepatitis, jaundice or liver failure.
From the nervous system: drowsiness, headache, dizziness, tremors, insomnia, anxiety, agitation, hypomania, mania, akathisia, paresthesias, depression symptoms, hallucinations, aggression, agitation, anxiety, psychosis, gait abnormalities, extrapyramidal disorder, dyskinesia, tremor , convulsions. Movement disorders were more common in patients with indications of their presence in the history or concomitant use of antipsychotics.
With the genitourinary system: delayed ejaculation, decreased libido and / or libido, erectile dysfunction, anorgasmia, menstrual disorders, gynaecomastia, priapism, hyperprolactinemia, galactorrhea.
From the respiratory system: asthma, or a feeling of “compression of the chest.”
Cardio-vascular system: palpitation, chest pain, hypertension, hypotension, edema, syncope and tachycardia (very rare). From the senses: visual disturbances (including blurred vision). Allergic reactions: skin redness, hives, swelling of the eyelids, face or lips, skin rash, generalized pruritus, erythema multiforme exudative. Laboratory data: reversible increases in transaminases, thrombocytopenia, leukopenia, transient hyponatremia (syndrome of inappropriate secretion antidiuriticheskogo hormone, more often in elderly patients, as well as when taking diuretics or some other drugs).
Other: sporadic bleeding (including epistaxis), hypothyroidism, increased sweating, weight loss, weakness, yawning, “tides” of blood to the face. “Cancellation” syndrome may occur when stopping treatment with fluoxymesterone halotestin.
Symptoms: serotonin syndrome – nausea, vomiting, drowsiness, ECG changes, mydriasis, tachycardia, agitation, dizziness, anxiety, agitation, diarrhea, increased sweating, myoclonus and hyperreflexia.Treatment is symptomatic: to ensure a normal airway (oxygenation and ventilation) and monitoring of cardiac rhythm and vital organs and systems. Induce vomiting is not recommended. Introduction of the activated charcoal and sorbitol may be more efficient than a gastric lavage. No specific antidote. At the large volume of distribution of fluoxymesterone halotestin, in this regard, increased diuresis, dialysis, hemoperfusion or blood transfusion may be inconclusive.
Interaction with other medicinal products . Monoamine oxidase inhibitors (MAOIs) There have been severe complications, while the use of fluoxymesterone halotestin and MAOIs (including MAOIs selectively acting reversible type of action – selegelin and moclobemide). Perhaps the development of serotonin syndrome. Similar complications, sometimes fatal, occur in the appointment of MAOI antidepressants during treatment, depressing neuronal uptake of monoamines or immediately after their withdrawal.
With simultaneous use of selective inhibitors of reverse neuronal uptake of serotonin and MAOIs arise: hyperthermia, rigidity, seizures, myoclonus, lability of the autonomic nervous system (rapid fluctuations in the parameters of the respiratory and cardiovascular system), mental status changes, including increased irritability, marked agitation, confusion which in some cases may go into state delirious or coma.
Drugs that suppress the central nervous system, and ethanol. The combined use of fluoxymesterone halotestin and substances depressing the central nervous system requires close attention, and prohibited the use of alcohol during treatment with fluoxymesterone halotestin.
Coumarin derivatives – in their joint appointment with fluoxymesterone halotestin showed a significant increase in prothrombin time – in these cases it is recommended to monitor the prothrombin time at the beginning of treatment with fluoxymesterone halotestin and after its cancellation.
Pharmacokinetic interaction of
fluoxymesterone halotestin is bound to plasma proteins. It is therefore necessary to consider the possibility of interaction with other drugs that bind to the protein (eg, diazepam, tolbutamide and warfarin).
Cimetidine: simultaneous application substantially reduces the clearance of fluoxymesterone halotestin.
Medicaments metabolyziruemye cytochrome P450 2D6 isoenzyme: long-term treatment with fluoxymesterone halotestin at a dose of 50 mg per day accompanied by increased concentrations of desipramine.
Medicaments metabolyziruemye other tsytohroma P450 enzyme systems. Experiments on the interaction in vitro have shown that CYP isoenzymes carried ZAZ / 4 betagidroksilirovanie endogenous cortisol and metabolism of carbamazepine and long-term administration of terfenadine with fluoxymesterone halotestin at a dose of 200 mg per day are not changed. The concentration in the blood plasma tolbutamide, warfarin and phenytoin prolonged assignment of fluoxymesterone halotestin in the same dose also varies. Thus, we can conclude that fluoxymesterone halotestin does not inhibit the isoenzymes CYP2C9.
fluoxymesterone halotestin has no effect on the concentration of diazepam in blood serum, which indicates the absence of inhibition of isoenzymes CYP 2C19. According to in vitro studies, fluoxymesterone halotestin has virtually no effect or minimally inhibits CYP 1A2 isoenzyme.
Lithium: the pharmacokinetics of lithium is not changed by concomitant administration of fluoxymesterone halotestin. However, the tremor occurs more often when they are used together. As well as the appointment of other selective inhibitors of reverse neuronal serotonin reuptake, fluoxymesterone halotestin joint application with drugs that affect the serotonergic transmission (eg, lithium), requires increased caution.
Drugs affecting serotonergic transmission. When replacing one inhibitor of neuronal uptake of serotonin on the other there is no need to “washout period”. However, you want to be careful with changes in the course of treatment. Avoid concomitant administration of tryptophan or fenfluramine with fluoxymesterone halotestin.
Induction of hepatic microsomal enzymes. fluoxymesterone halotestin causes minimal induction of liver enzymes. Co-administration of fluoxymesterone halotestin and antipyrine at a dose of 200 mg leads to a significant reduction in the half-life of antipyrine, although there is only 5% of cases.
Atenolol: when co-administered fluoxymesterone halotestin does not change its b-adrenoceptor blocking action.
Glibenclamide and digoxin: the introduction of fluoxymesterone halotestin in a daily dose of 200 mg of drug interactions with these drugs have been identified.
fluoxymesterone halotestin should not be used in conjunction with the IM AD, and within 14 days after discontinuation of treatment MI SA. Similarly, after the abolition of fluoxymesterone halotestin for 14 days did not prescribe MAOIs.
It should be noted that in patients undergoing electroconvulsive therapy, sufficient experience with fluoxymesterone halotestin is not. The possible success or the risk of such combined treatment has not been studied.Patients with depression are at risk for suicide attempts. This risk persists until the development of remission. Therefore, from the beginning of the treatment and to achieve optimal clinical response for patients should establish a permanent medical supervision.
Women of childbearing age during treatment should use adequate contraception methods.
Effects on ability to drive vehicles and management mechanisms
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Purpose fluoxymesterone halotestin is usually not accompanied by violation of psychomotor functions. However, its use in conjunction with other drugs may impair attention and motor coordination. Therefore, during treatment with fluoxymesterone halotestin drive vehicles, special equipment or practice associated with an increased risk of the activity is not recommended. steroiden kaufen
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