Duloxetine Hcl (duloxetine HCl)

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Last reviewed · Source: First Databank (FDB) drug data

Overview

Duloxetine hydrochloride, a selective serotonin- and norepinephrine-reuptake inhibitor (SNRI), is an antidepressant and anxiolytic agent.

Duloxetine hydrochloride, a selective serotonin- and norepinephrine-reuptake inhibitor (SNRI), is an antidepressant and anxiolytic agent. The drug also has demonstrated analgesic activity in animal models of chronic and persistent pain and in clinical trials evaluating the drug's activity in conditions associated with chronic pain (e.g., neuropathic pain, fibromyalgia).

The exact mechanisms of the antidepressant, anxiolytic, and central pain inhibitory actions of duloxetine have not been fully elucidated, but appear to be associated with the drug's potentiation of serotonergic and noradrenergic activity in the CNS. Duloxetine is a potent inhibitor of neuronal serotonin and norepinephrine reuptake and a less potent inhibitor of dopamine reuptake. Duloxetine does not inhibit monoamine oxidase (MAO) and has not demonstrated significant affinity for dopaminergic, adrenergic, cholinergic, gamma-aminobutyric acid (GABA), glutamate, histaminergic, and opiate receptors in vitro.

Duloxetine is well absorbed following oral administration, with peak plasma concentrations usually attained in 6 hours. With evening administration, there is a 3 hour delay in absorption and a 33% increase in clearance of the drug compared to morning administration. Food increases the time to peak plasma concentrations from 6 to 10 hours, and marginally decreases the extent (about 10%) of absorption.

Duloxetine pharmacokinetics are dose-proportional over the therapeutic dosing range (30-120 mg daily). Steady state plasma concentrations are attained after 3 days of once daily dosing. Mean duloxetine concentrations at steady state are about 30% lower in pediatric patients 7-17 years of age relative to adult patients, and are considered comparable between these age groups.

Duloxetine is extensively metabolized in the liver, principally via oxidation by the cytochrome P-450 (CYP) 2D6 and 1A2 isoenzymes. Major circulating metabolites do not significantly contribute to the pharmacologic activity of duloxetine. Duloxetine is a moderate inhibitor of CYP2D6 and a somewhat weak inhibitor of CYP1A2.

The drug is not an inhibitor of CYP2C9, CYP2C19, or CYP3A, nor is it an inducer of CYP1A2 or CYP3A. Duloxetine is highly bound (>90%) to human plasma proteins, which is not affected by renal or hepatic impairment. The interaction potential of duloxetine with other highly protein bound drugs has not been fully elucidated.

Duloxetine is excreted principally in the urine as metabolites (about 70%) and unchanged drug (<1%), and in feces (20%). The elimination half-life of duloxetine is approximately 12 hours (range: 8-17 hours). The bioavailability of duloxetine is decreased by approximately 33% in smokers.

Pharmacokinetics of duloxetine are not affected by sex; half-life is similar in men and women. The impact of race on duloxetine pharmacokinetics has not been evaluated.

USES: This medication is used to treat certain mental/mood disorders (such as depression, anxiety). It is also used to help relieve nerve pain (peripheral neuropathy) in people with diabetes or ongoing pain due to medical conditions such as arthritis, chronic back pain, or fibromyalgia (a condition that causes widespread pain). Duloxetine belongs to a class of drugs known as serotonin-norepinephrine reuptake inhibitors (SNRIs).

It works by helping to restore the balance of certain natural substances (serotonin and norepinephrine) in the brain.

Generic name: duloxetine HCl
Pronunciation: (doo-LOX-e-teen)

Reference product & biosimilars

No reference, biosimilar or interchangeable associated with this drug.

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Indications

The following indications are listed for Duloxetine Hcl:

  • Anxiety With Depression
  • Chronic Musculoskeletal Pain
  • Diabetic Peripheral Neuropathy
  • Fibromyalgia
  • Generalized Anxiety Disorder
  • Major Depressive Disorder

Also known as: Anxiety Associated With Depression, Diabetic Neuropathy, Fibromyalgia Syndrome, Major Unipolar Illness, Mixed Anxiety And Depressive Disorder, Unipolar Mood Disorder.

Dosing

Dosage of duloxetine hydrochloride is expressed in terms of duloxetine.

Because withdrawal effects may occur, abrupt discontinuance of duloxetine should be avoided. When duloxetine therapy is discontinued, dosage should be tapered gradually and the patient carefully monitored to reduce the risk of withdrawal symptoms. If intolerable symptoms occur following dosage reduction or upon discontinuance of treatment, duloxetine therapy may be reinstituted at the previously prescribed dosage until such symptoms abate. Clinicians may resume dosage reductions at that time but at a more gradual rate.

Drug interactions

Duloxetine is metabolized by cytochrome P-450 (CYP) isoenzymes, principally CYP2D6 and CYP1A2. Duloxetine is a moderate inhibitor of CYP2D6 and also inhibits CYP1A2. In vitro studies indicate that duloxetine does not inhibit CYP2C9, CYP3A, or CYP2C19. In vitro studies indicate that duloxetine does not induce CYP1A2 or CYP3A.

Contraindications

*Concurrent or recent (i.e., within 14 days) therapy with a monoamine oxidase (MAO) inhibitor intended to treat psychiatric disorders. Use of an MAO inhibitor intended to treat psychiatric disorders within 5 days of duloxetine discontinuance.

*Initiation of duloxetine in a patient receiving MAO inhibitors such as linezolid or IV methylene blue.

Adverse reactions

Adverse effects reported in 5% or more of adults receiving duloxetine include nausea, dry mouth, somnolence, constipation, decreased appetite, and increased sweating.

Adverse effects reported in 5% or more of pediatric patients receiving duloxetine include decreased weight, decreased appetite, nausea, vomiting, fatigue, and diarrhea.

Precautions

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ICD codes

No ICD codes are available for this drug.

Formulary status

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Last reviewed · Source: First Databank (FDB) drug data