Reboxetine

Chemical name

(R*,R*)-({+})-2-[(2-Этоксифено кси)фенилметил]морфол ин (as nelfinavir)

Gross

C19-H23-N-O3

Of drugs

Drugs, the antidepressant. Vsokoseleguo ingibiruet reverse takeover norarenalina presinapticakimi nerve endings, to the accumulation of neiromediator in synaptic junctions and reinforces noradrainergicescuu transfer. There has to affinnostew receptors нейромедиаторов.Анти��епрессивный effect develops over two weeks after the start of treatment. Improves performance and social adaptation Ballah.horosho extracted from the blood, material-90%, eating does not affect the removals. After admission to dose 4 mg C_max in the blood (130 ng / ml) is achieved in 2 hours Linking plasma proteins (mostly with альфа_1-гликопротеино��) is 97%. The volume of 0.5 l / mm Equilibrium concentration in the blood depends on the dose of 50-160 ng / ml, is for a period of five days after the start of the reception. Metabolised in the liver mainly with the participation of CYP3A4 izofermenta zitohroma P450 with the formation of four inactive derivative (major metabolite - O-dezetilreboksetin). T_1/2 - 1.15 Report mostly kidneys (78% rate, including 10% in unmodified form). T_1/2 increase in older patients, as well as kidney or liver umerennovrajenna недостаточности.Пред��тавляет razemicescuu a mixture of the two enantiomers active, the level of plasma in a stronger S S-enantiomera twice below, and its removal with urine-2 times higher than Rr-enantiomera. Enantiomers are qualitative differences on other farmakokineticski and farmakodinamicakim Swoystwam.pri oral introduction mice doses front mg / kg caused moderate midriaz. At doses of 100 mg / kg in mice does not stimulating effect on the central nervous system. The toxic dose (400 mg / kg) by the advent of Generalized klonicakih convulsing. Toxic effect emerged 20 minutes later after reaching a peak after 60 min and lasted for about 120 minutes. Therapy and chemicals dose in mice differ 10-40 Raz.v clinical studies in healthy volunteers therapeutic dose reboksetina did not cause significant increases heartbeat and pupil diameter, shorten the recovery pupil reaction to light, but significantly reduced slunootdelenie and amplitude zraczkowogo light reflex.

Indications

Depressive state (acute phase and the maintenance therapy).

Restrictions on the use of

Pregnancy, breast feeding, child age (safety and efficacy of the use of children to be determined).

Pregnancy and lactation

Perhaps if the effect of therapy outweighs the potential risk to the fetus. Not recommended breastfeeding (no data on the safety of the nursing women).

Contraindications

Гиперчувствительност ь.

Side-Effects

Insomnia, dizziness, dry mouth, difficulty urinating, constipation, increased sweating, tachycardia, impotence (at doses more than 8 mg / day).

Patient interaction

Not identified meaningful interaction with fluoksetinom, paroxetinom, lorazepam.

Overdosing

Symptoms : ortostatical gipotenzia, hypertension, Trevoga.lechenie : symptomatic therapy, monitoring vital functions.

Precautions

Be wary appoint patients with convulsive seizures in history (in the development of epilepsy during the course of treatment necessary to close the doors), and bipolar disorder affeguom expressed kidney failure, delay urination, glaucome, arterial hypotension. Interaction with other antidepressants (tricyclic, MAO inhibitors, inhibitors of reverse takeover serotonin), lithium salts in the clinical studies was not investigated. It should not be used concurrently with MAO inhibitors. With the caution at the same time as the hypotensive means.

Dosing and Administration

Inside, regardless of meals, and 4 mg twice a day (8 mg / day); In the case of lack of clinical effect in three weeks to increase doses up to 10 mg / sut. Older patients (over 65 years) and in patients with renal or moderately expressed liver failure-2 mg twice a day (4 mg / day) with the dose increase after 3 weeks (if necessary) to 6 mg / sut.

Literature

J. Burns The pharmacology and toxicology of reboxetine / / Int. J. Med. Toxicol 2000 .- .- V. 3-N 4.

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