DULOXETINE (CYMBALTA). What is used for?

What is Duloxetine?

Duloxetine is a drug used for the treatment of depression, anxiety and diabetic peripheral neuropathy. The product ingredient is Duloxetine hydrochloride (hcl).

The brand names of Duloxetine in the United States are: Cymbalta, Irenka, Drizalma Sprinkle.

Mechanism of action (MOA) Duloxetine

Serotonin and noradrenaline reuptake inhibitor. Weakly inhibits dopamine reuptake without significant affinity for histaminergic, dopaminergic, cholinergic and adrenergic receptors.

Therapeutic indications, benefits and dosage of Duloxetine

Oral.
Adults:

  1. – Major depressive episodes and patients with co-morbid major depressive episodes: initial and maintenance: 60 mg/day.
  2. – Generalized anxiety disorder: initial: 30 mg/day. Maintenance: 60 mg.
    A dose escalation of up to 90 or 120 mg may be considered in those with insufficient response to 60 mg (depending on clinical response and tolerability).
  3. – Diabetic peripheral neuropathic pain: initial and maintenance: 60 mg/day, max: 120 mg/day administered in equally divided doses. Reevaluate regularly (at least every 3 months).

Method of administration of Duloxetine

Oral use.
Take 1 time/day, with or without food.

Contraindications of Duloxetine

  • Hypersensitivity, liver disease leading to liver failure, severe kidney failure, uncontrolled high blood pressure.
  • In combination with: Irreversible, non-selective MAOIs.
  • Potent inhibitors of CYP1A2 such as fluvoxamine, ciprofloxacin or enoxacin.

Warnings and cautions with Duloxetine

  • Mild or moderate kidney failure, history of mania, or diagnosis of bipolar disorder and/or seizures.
  • High IOP or at risk of narrow angle glaucoma.
  • Patients whose underlying pathology may be compromised by an increase in heart rate or blood pressure.
  • Concomitant with other antidepressants (especially with selective reversible MAOIs), substances that impair your metabolism, or that are associated with liver damage, oral anticoagulants, and/or medications that affect platelet function.
  • Known hemorrhagic diathesis.
  • Patients at high risk of hyponatremia (elderly, cirrhosis, dehydration, diuretic treatment).
  • Elderly.
  • Most frequent adverse reactions in combination with Hypericum perforatum.
  • Follow-up, at the beginning of treatment and after dose change, for risk of suicide.
  • There are no data on safety and efficacy in children < 18 years for the treatment of diabetic peripheral neuropathic pain or for generalized anxiety disorder.
  • Do not use in children and adolescents < 18 years for the treatment of major depressive disorder.
  • Do not interrupt treatment abruptly due to the risk of onset of withdrawal symptoms.
  • Acatasia/psychomotor restlessness may develop in the first few weeks of treatment.
  • Risk of serotonergic syndrome, particularly concomitant with other serotonergic agents (including SSRIs , serotonin/noradrenaline reuptake inhibitors, tricyclic antidepressants, or triptans), with agents that affect serotonin metabolism such as MAOIs, or with antispychotics or other dopamine antagonists that may affect serotonergic neurotransmission systems.

Liver failure

Contraindicated in hepatic disease that produces hepatic insufficiency.

Renal insufficiency

Contraindicated in severe renal failure.
Also caution in mild-moderate renal insufficiency.

Interactions with Duloxetine

  • Caution: medications that act in the CNS (alcohol, benzodiazepines, morphinetics, antipsychotics, phenobarbital, sedative antihistamines), medications metabolized by CYP2D6 (risperidone, nortriptyline, amitriptyline, imipramine, flecainide, propafenone, metoprolol).
  • Plasma concentration increased by: inhibitors of CYP1A2 as fluvoxamine.
  • Concentrations decreased by: CYP1A2 inducers.

Pregnancy and Duloxetine

There is no data. Use only if the benefit outweighs the risk to the fetus.

Breastfeeding

Duloxetine is very weakly excreted in human breast milk according to a study of 6 lactating mothers who did not breastfeed.

The estimated daily dose for the infant in mg/kg is approximately 0.14% of the dose consumed by the mother.

Since the safety of duloxetine in children is unknown, its use during breastfeeding is not recommended.

Effects on driving ability

Duloxetine can cause sedation, dizziness.
Therefore, patients should be advised that if they experience sedation or dizziness, they should avoid performing potentially hazardous tasks, such as driving or using machines.

Adverse reactions and side effects of Duloxetine

Headache, drowsiness, dizziness, lethargy, tremors, paresthesia.

Decreased appetite; insomnia, agitation, decreased libido, anxiety, abnormal orgasms, abnormal dreams.

Blurred vision; tinnitus; palpitations; increased blood pressure.

Flushing; yawning; nausea, dry mouth, constipation, diarrhea, abdominal pain, vomiting, dyspepsia, flatulence.

Increased sweating, rash; musculoskeletal pain, muscle spasm.

Dysuria, urinary frequency; erectile dysfunction, ejaculation disorder, delayed ejaculation.

Falls, fatigue; weight loss. Rarely: interstitial lung disease.

⭐⭐⭐⭐⭐ VIDEO OF DULOXETINE/CYMBALTA (DRUG)

Source: The content of this active ingredient has been written taking into account the clinical and molecular information of all medicines authorised and marketed in the United States under the Unique Ingredient Identifier (UNII) by the Substance Registration System (SRS) of the Food and Drug Administration (FDA) and the United States Pharmacopeia (USP).

In order to know in detail the information authorized by the FDA for each drug, you should consult the corresponding medication guide authorized by the FDA.

Resources:

UNII: O5TNM5N07U
ChemIDplus
DrugPortal
PubChem CID: 60835
NCI Thesaurus: C65495

 

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