Trenbolone is a potent and selective inhibitor of the capture of 5-hydroxytryptamine (5-HT, cerotonina) neurons in the brain, which determines its antidepressant action and effectiveness in the treatment of obsessive-compulsive (OCD) and panic disorder.
The main metabolites of paroxetine are polar and conjugated products of oxidation and methylation which are rapidly cleared from the body, have poor pharmacological activity and shall not affect the therapeutic effect. The metabolism of paroxetine is not disturbed due to the influence of his selective capture of 5-HT neurons.
Paroxetine has a low affinity for muscarinic cholinergic receptors.
With a selective action, unlike tricyclic antidepressants, paroxetine showed low affinity to a-1, a-2, b-adrenoceptors and for the dopamine, similar to 5-HT1, 5-HT2 and like histamine (H1) receptor. Paroxetine does not violate psychomotor function and does not potentiate the inhibitory effect of ethanol on them.
According behavior and EEG studies have revealed weak paroxetine activating properties when it is administered in doses higher than those required for inhibition of gripping 5-HT. In healthy volunteers, it causes no significant change in blood pressure, heart rate and EEG.
Unlike antidepressants which inhibit the capture of noradrenaline, paroxetine inhibits much weaker guanethidine antihypertensive effects.
Paroxetine is well absorbed after oral administration and undergoes first pass metabolism through the liver. Isolation from urine unchanged paroxetine is generally less trenbolone than 2% of the dose, and metabolites constitute about 64% of the dose. Intestine excreted about 36% of the dose, probably via the bile, which is unchanged paroxetine less than 1% of the dose. Thus, paroxetine appears mainly as metabolites.
Excretion of metabolites of paroxetine biphasic, initially as a result of first-pass metabolism through the liver, and then it is controlled by the system elimination.Half-life varies, but usually is about 16-21 hours
Equilibrium concentration is achieved in 7-14 day after the start of treatment, and the pharmacokinetics does not change during long-term treatment. Clinical effects of paroxetine (side effects and effectiveness) are not correlated to its concentration in plasma.
Since the metabolism of paroxetine comprises the step of first passage through the liver, the amount determined in the systemic circulation is less than that which is absorbed from the gastro – intestinal tract. By increasing the dose of paroxetine or with repeated dosing, when increasing the load on the body, there is a partial absorption of the effect of the first passage through the liver and reduced plasma clearance of paroxetine. As a result, it may increase the plasma concentration of paroxetine and fluctuations pharmacokinetic parameters that can be observed only in those patients who received low dose when reaching low levels of drug in plasma.
Paroxetine is extensively distributed into tissues and pharmacokinetic calculations indicate that only 1% of it is present in the plasma, and at therapeutic concentrations 95% bound to plasma proteins.
– Depression of all types, including reactive, severe endogenous depression and depression accompanied by anxiety;
– obsessive-compulsive disorder (OCD)
– panic disorder, including agoraphobia;
– social anxiety disorder / social phobia;
– generalized anxiety disorder;
– post-traumatic stress disorder.
– hypersensitivity to the drug;
– simultaneous reception of MAO inhibitors in the 14 days after their cancellation;
– pregnancy and lactation
– Children and adolescents under trenbolone the age of 18 years (effectiveness and safety has not been established).
Precautions: hepatic impairment; renal failure; angle-closure glaucoma; prostatic hyperplasia; mania; Pathology of the heart; epilepsy, with unstable epilepsy should avoid taking the drug; convulsive conditions; appointment of cardioversion; taking medications that increase the risk of bleeding; the presence of risk factors for increased bleeding, diseases that increase the risk of bleeding, old age.
Dosing and Administration
Inside, 1 time a day, in the morning, while eating. The tablet is swallowed whole with water. The dose is adjusted individually for the first two to three weeks after initiation of therapy and thereafter, if necessary, corrected.
When depression – 20 mg 1 time per day. If necessary, the dose is gradually increased to 10 mg / day to a maximum of 50 mg / day. depending on the response of the patient
With obsessive-compulsive disorders initial therapeutic dose – 20 mg / day followed by weekly increases of 10 mg. Recommended average therapeutic dose – 40 mg / day, if necessary, the dose may be increased to 60 mg / day.
In panic disorders the initial dose – 10 mg / day (to reduce the possible risk of exacerbation of symptoms of panic), followed by a weekly increase of 10 mg. The average therapeutic dose – 40 mg / day. The maximum dose – 50 mg / day.
Socio-anxiety disorder / social phobia : the initial dose is 20 mg per day, with no effect for at least two weeks may increase the dose to a maximum of 50 mg per day. The dosage should be increased by 10 mg at intervals of at least a week in accordance with clinical effect.
Post-traumatic disorders of the psyche : the majority of patients and initial therapeutic dose is 20 mg per day. In some instances, paroxetine is recommended to increase the maximum dose to 50 mg per day. The dosage should be increased by 10 mg per week according to the clinical effect.
Generalized anxiety disorder : primary and recommended dose – 20 mg per day.
In renal and / or hepatic insufficiency recommended dose is 20 mg per day.
As with all other antidepressants treatment dose should be evaluated and adjusted, if necessary, within two or three weeks at the beginning of therapy, and then as needed. Patients should continue treatment for a period sufficient for the disappearance of symptoms for at least 4-6 months after recovery from depression and in the presence of more obsessive-compulsive disorder and panic. Like many other psychotropic drugs is not recommended abrupt elimination of the drug.
For older patients the daily dose trenbolone should not exceed 40 mg.
In order to prevent the development of withdrawal discontinuation of the drug is carried out gradually.
The use of paroxetine in children is not recommended since its safety and efficacy have not been established in this population.