Description

Simple

A medication used to treat depression.

Clinical

A selective serotonin reuptake inhibitor (SSRI) used in the treatment of depression.

Overview

Citalopram belongs to a class of antidepressant agents known as selective _serotonin-reuptake inhibitors_ (SSRIs) and is widely used to treat the symptoms of depression. Its chemical structure is unrelated to that of other SSRIs or of tricyclic, tetracyclic, or other prescribed antidepressants [FDA label]. Citalopram is also known as _Celexa_, and available in tablet and solution forms [FDA label]. This drug was initially approved by the FDA in 1998 [18].

Pharmacology

Indication

For the treatment of depression, as indicated by the FDA label [FDA label]. Off-label indications include but are not limited to: treatment of sexual dysfunction, post-stroke behavioural changes, ethanol abuse, obsessive-compulsive disorder (OCD) in children, and diabetic neuropathy [FDA label], [ Read more

Pharmacodynamic

Citalopram belongs to a class of antidepressants known as selective serotonin reuptake inhibitors (SSRIs). It has been found to relieve or manage symptoms of depression, anxiety, eating disorders and obsessive-compulsive disorder among other mood disorders. The antidepressant, anti-anxiety, and othe... Read more

Mechanism of action


The mechanism of action of citalopram results from its inhibition of CNS neuronal reuptake of serotonin (5-HT) [FDA label]. The molecular target for citalopram is the serotonin transporter (solute carrier family 6 member 4, _SLC6A4_), inhibiting its serotonin reuptake in the synaptic cleft [ Read more

Absorption

Rapidly and well absorbed from the GI tract. Peak plasma concentrations occur within 4 hours of a single orally administered dose. Bioavailability is 80% following oral administration. Food does not affect absorption [FDA label].

Protein binding

Citalopram, dimethylcitalopram, and didemethylcitalopram are 80% bound to plasma proteins [FDA label].

Volume of distribution

12 L/kg [FDA label]Citalopram is highly lipophilic and likely widely distributed throughout the body, including the blood-brain-barrier. However, its metabolite, _demethylcitalopram_ does not penetrate the blood-brain-barrier well [FDA label].

Clearance

The systemic clearance of citalopram is 330 mL/min, with approximately 20% renal clearance [FDA label].

Half life

About 35 hours [FDA label].

Route of elimination

12-23% of an oral dose of citalopram is found unchanged in the urine, while 10% of the dose is found in the faeces [FDA label].

Toxicity

**Oral (Human) LD**: 56 mg/kg
**Intraperitoneal (Mouse) LD50**: 179 mg/kg

**Acute toxicity**

Symptoms of toxicity include dizziness, sweating, nausea, vomiting, tremor, somnolence, and sinus tachycardia. Rarely, symptoms included amnesia, confusion, coma, convulsions, hyperventilation, cyanos... Read more

Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Nausea US
  • Kind: experimental
    • Percent: 21%
  • Kind: placebo
    • Percent: 14%
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 20%
  • Kind: placebo
    • Percent: 14%
  • Clinical Trial
    Somnolence US
  • Kind: experimental
    • Percent: 18%
  • Kind: placebo
    • Percent: 10%
  • Clinical Trial
    Insomnia US
  • Kind: experimental
    • Percent: 15%
  • Kind: placebo
    • Percent: 14%
  • Clinical Trial
    Sweating increased US
  • Kind: experimental
    • Percent: 11%
  • Kind: placebo
    • Percent: 9%
  • Clinical Trial
    Tremor US
  • Kind: experimental
    • Percent: 8%
  • Kind: placebo
    • Percent: 6%
  • Clinical Trial
    Diarrhea US
  • Kind: experimental
    • Percent: 8%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Abnormal ejaculation US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Ejaculation disorder US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Dyspepsia US
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Rhinitis US
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Upper Respiratory Tract Infection US
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Fatigue US
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Vomiting US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Libido decreased US
  • Kind: experimental
    • Percent: 2-4%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Anorexia US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Anxiety US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Anxiety US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Dysmenorrhea US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Agitation US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Abdominal Pain US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Impotence US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Sinusitis US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Yawning US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Myalgia US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Arthralgia US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Fever US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    QTc interval prolongation US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Back Pain US
  • Kind: experimental
    • Percent: ≥2%
  • Clinical Trial
    Micturition Disorder US
  • Kind: experimental
    • Percent: ≥2%
  • Clinical Trial
    Nervousness US
  • Kind: experimental
    • Percent: ≥2%
  • Clinical Trial
    Pharyngitis US
  • Kind: experimental
    • Percent: ≥2%
  • Clinical Trial
    Palpitation US
  • Kind: experimental
    • Percent: ≥2%
  • Clinical Trial
    Vision abnormal US
  • Kind: experimental
    • Percent: ≥2%
  • Clinical Trial
    Sleep Disorder US
  • Kind: experimental
    • Percent: ≥2%
  • Clinical Trial
    Asthenia US
  • Kind: experimental
    • Percent: ≥2%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: ≥2%
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: ≥2%
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: ≥2%
  • Clinical Trial
    Accommodation abnormal US
  • Kind: experimental
    • Percent: ≥1%
  • Clinical Trial
    Pruritus US
  • Kind: experimental
    • Percent: ≥1%
  • Clinical Trial
    Hypertension US
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Polyuria US
  • Kind: experimental
    • Percent: ≥1%
  • Clinical Trial
    Taste perversion US
  • Kind: experimental
    • Percent: ≥1%
  • Clinical Trial
    Confusion US
  • Kind: experimental
    • Percent: ≥1%
  • Clinical Trial
    Suicide Attempt US
  • Kind: experimental
    • Percent: ≥1%
  • Clinical Trial
    Aggravated depression US
  • Kind: experimental
    • Percent: ≥1%
  • Clinical Trial
    Rash US
  • Kind: experimental
    • Percent: ≥1%
  • Clinical Trial
    Coughing US
  • Kind: experimental
    • Percent: ≥1%
  • Clinical Trial
    Amenorrhea US
  • Kind: experimental
    • Percent: ≥1%
  • Clinical Trial

    Contraindications

    • Route:
      • Oral
    • Regions: US
    • With Categories:
        • Name: Monoamine Oxidase Inhibitors
        • Drugbank Id: DBCAT001004
        • Mesh Id: D008996
    • Route:
      • Oral
    • Regions: US
    • With Drugs:
        • Name: Pimozide
        • Drugbank Id: DB01100
    • Route:
      • Oral
    • Hypersensitivity:
      • true
    • Regions: US

    Food Interactions

    Avoid alcohol.

    Avoid St. John's Wort.

    Take with or without food. The absorption is unaffected by food.