Cymbalta (Duloxetine)

$ 119.48$ 403.74

Category: Anti-Depressants
Commercial name: Cymbalta
Active ingredient: Duloxetine
Production form: Pills
Available dosage: 20mg, 30mg, 40mg, 60mg

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Description

Cymbalta (Duloxetine). Dosage, Side Effects, Interactions

Cymbalta (Duloxetine) is a drug used to treat depression, pain associated with diabetic neuropathy, and generalized anxiety disorder. The antidepressant is a selective serotonin and norepinephrine reuptake inhibitor (SSNRI).

Cymbalta (Duloxetine) is used to treat:

  • depressive illnesses (major depression )
  • Pain in diabetic polyneuropathy
  • generalized anxiety disorder

How Cymbalta (Duloxetine) works

Duloxetine is a selective serotonin noradrenaline reuptake inhibitor (SSNRI ). The active ingredient also inhibits dopamine reuptake to a small extent , but has no significant affinity for histaminergic, dopaminergic, cholinergic and adrenergic receptors.

 

Pharmacokinetics

Duloxetine is metabolised by oxidation via CYP1A2 and polymorphic CYP2D6 , followed by conjugation. The pharmacokinetics of duloxetine are subject to large inter-subject variability (generally 50 to 60 percent). Gender, age, smoking status and CYP2D6 metabolization status, among other things, can have an influence on this.

absorption

After oral administration, duloxetine is well absorbed and reaches its maximum concentration after 6 hours. The absolute oral bioavailability is between 32 and 80 percent (mean 50 percent).

distribution

Duloxetine is approximately 96 percent plasma protein bound. Duloxetine binds to both albumin and alpha-1 acid glycoprotein. Renal or hepatic impairment does not affect protein binding.

biotransformation

Duloxetine undergoes extensive metabolism. The metabolites are mainly eliminated via the kidneys. CYP2D6 and CYP1A2 catalyze the formation of two major metabolites which, based on in vitro studies, are considered to be pharmacologically inactive: the glucuronic acid conjugate of 4-hydroxyduloxetine and the sulfate conjugate of 5-hydroxy-6-methoxyduloxetine.

elimination

The mean elimination half-life of duloxetine is 12 hours. After intravenous administration, the plasma clearance is on average 36 l/h and after oral intake on average 101 l/h).

 

Dosage of Cymbalta (Duloxetine)

Depending on the indication, there are different dosage recommendations:

  • Depressive disorders: The starting dose and the recommended maintenance dose are 60 mg once a day. Two to four weeks may elapse before a therapeutic response is achieved.
     
  • Diabetic polyneuropathy pain: The starting dose and the recommended maintenance dose are 60 mg once daily. Efficacy should be assessed after 2 months, as after this time further improvement in efficacy is unlikely in patients with an inadequate initial response.
     
  • Generalized Anxiety Disorder: The recommended starting dose is 30 mg once daily. If the response is insufficient, the dose can be increased to 60 mg once daily.

Side effects of Cymbalta (Duloxetine)

The most frequently reported side effects, most of which were only reported at the start of treatment, were:  

  • Nausea
  • headache
  • dry mouth
  • Sleepiness
  • dizziness

Duloxetine should not be discontinued abruptly, otherwise discontinuation symptoms may occur, such as: dizziness, sensory impairment (paraesthesia), sleep disturbances, tiredness, somnolence, agitation or anxiety, nausea and/or vomiting, tremor, headache, myalgia, irritability, diarrhea, increased sweating and dizziness.

 

Interactions

Monoamine oxidase inhibitors (MAOIs) -> risk of serotonin syndrome

CYP1A2 inhibitors (e.g. fluvoxamine ) -> higher concentrations of duloxetine possible.

CNS active drugs (e.g. alcohol and sedatives such as benzodiazepines , opioids , antipsychotics , phenobarbital , sedative antihistamines ) -> Caution required

Serotonergic drugs ( e.g. SSRIs , SNRIs , tricyclic antidepressants such as clomipramine or amitriptyline , MAO inhibitors such as moclobemide orLinezolid , St. John’s wort, triptans , tramadol , pethidine , tryptophan ) -> risk of serotonin syndrome

Duloxetine is a moderate inhibitor of CYP2D6. Interactions can therefore occur when used simultaneously with active substances metabolized via CYP2D6 (e.g. risperidone , tricyclic antidepressants such as nortriptyline , amitriptyline and imipramine , flecainide , propafenone and metoprolol ) ,

anticoagulants and platelet aggregation inhibitors -> increased risk of bleeding

CYP1A2 inducers (eg, smoking): Smokers have approximately a 50 percent reduced plasma concentration of duloxetine compared to non-smokers.

 

Contraindication

The following contraindications exist for treatment with duloxetine:

  • Hypersensitivity to the active substance
  • Concomitant treatment with non-selective, irreversible monoamine oxidase inhibitors (MAOIs)
  • Liver disease with hepatic impairment
  • Combination with fluvoxamine, ciprofloxacin or enoxacin (ie strong CYP1A2 inhibitors) -> plasma level of duloxetine is increased
  • Severe renal impairment (creatinine clearance < 30 ml/min)
  • Uncontrolled hypertension

Pregnancy

There is evidence that selective serotonin reuptake inhibitor use, particularly late in pregnancy, may increase the risk of primary pulmonary hypertension in newborns.

In addition, ingestion near term may result in withdrawal symptoms (such as hypotension, tremor, restlessness, difficulty in feeding, shortness of breath, and seizures) in the newborn.

It should therefore only be used during pregnancy if the potential benefit to the mother justifies the potential risk to the foetus.

 

Lactation

A small study showed that duloxetine is excreted in human milk in very small amounts. Since it is not known whether and to what extent duloxetine is tolerated by infants, use during breastfeeding is not recommended.

 

Driving ability

Taking duloxetine can cause tiredness and dizziness. If these symptoms occur, patients should avoid driving or using machines.

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Additional information

Dosage

20 mg, 30 mg, 40 mg, 60 mg

Quantity

30, 60, 90, 120, 180

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