Paluxetil

Paluxetil uses

• Pharmacological action
• Pharmacokinetics
• Why is Paluxetil prescribed?
• Dosage and administration
• Paluxetil side effects, adverse reactions
• Paluxetil contraindications
• Restrictions for using
• Using during pregnancy and breastfeeding
• Special instructions
• Paluxetil drug interactions
• Paluxetil in case of emergency / overdose
• Paluxetil reviews

Pharmacological action

Paluxetil is an antidepressant, selective serotonin reuptake inhibitor. This medication has a bicyclic structure distinct from the structures of other known antidepressants. Paluxetil has antidepressant and anxiolytic effects when expressed enough incentive effect.

Antidepressant (thymoleptic) action is related to the ability of Paluxetil selectively block the reuptake of serotonin presynaptic membrane than is caused by increase of free content of this neurotransmitter in the synaptic cleft and enhancement of its activity in the CNS.

Effect on the m-cholinergic receptors, alpha- and beta-adrenergic receptors is only slightly which determines the extremely weak intensity of the side effects.

Pharmacokinetics

After oral administration Paluxetil is well absorbed from the gastrointestinal tract. Ingestion did not affect absorption. C_ss is set to the 7-14 day since the start of therapy. The major metabolites of Paluxetil are polar and conjugated products of oxidation and methylation. Due to the low pharmacological activity of metabolites their impact on therapeutic efficacy is unlikely.

T_1/2 on average is 16-24 hours. Less than 2% excreted in the urine in unchanged form, the rest - in the form of metabolites or urine (64%), or bile.

Excretion of Paluxetil is biphasic.

With long-term continuous using of this drug pharmacokinetic parameters do not change.

Why is Paluxetil prescribed?

Endogenous, neurotic and reactive depression.

Dosage and administration

When Paluxetil administered orally an initial dose is 10-20 mg / day. If necessary, depending on the evidence, the dose was increased to 40-60 mg / day. Increasing the dose spend gradually on 10 mg with intervals of 1 week. Frequency of admission is 1 time / day. The treatment of long-term. Treatment's efficacy is assessed after 6-8 weeks.

For elderly and debilitated patients, as well as renal impairment and hepatic the initial dose is 10 mg / day, the maximum dose is 40 mg / day.

Paluxetil side effects, adverse reactions

CNS: rarely - drowsiness, tremor, fatigue, insomnia.

Digestive system: rarely (when used in doses more than 20 mg) - nausea, dry mouth, and in some cases constipation. Other: rarely (when used in doses more than 20 mg) - increased sweating, ejaculation disorders.

Paluxetil contraindications

Simultaneous treatment with MAO inhibitors, and the period up to 14 days after their withdrawal, hypersensitivity to Paluxetil.

Restrictions for using

Angle-closure glaucoma, prostate adenoma, pregnancy and breastfeeding.

Using during pregnancy and breastfeeding

Category effects on the fetus by FDA - C.

Special instructions

Stop taking of Paluxetil should be gradually reducing the dose to avoid withdrawal syndrome, which manifests itself dizziness, nausea, vomiting, insomnia, confusion, increased sweating.

There is contraindicated drinking alcohol during the treatment with Paluxetil.

Be wary of over 14 days after taking of MAO inhibitors, gradually increasing the dose. MAO inhibitors should not be administered within 2 weeks after complete withdrawal of Paluxetil.

Simultaneous administration with drugs that inhibit the metabolism of liver enzymes, Paluxetil should be used in the smallest recommended doses.

In simultaneous use with drugs that induce the metabolism of enzymes it does not required any changes in the initial doses of Paluxetil.

Be wary of using Paluxetil with lithium therapy and oral anticoagulants.

There was not found carcinogenic and mutagenic properties of Paluxetil in experimental studies.

Use Paluxetil with caution in patients whose activities are connected with the necessity of high concentration of attention and quickness of psychomotor reactions.

Paluxetil drug interactions

Simultaneous administration of Paluxetil with: