Celexa
Celexa
Generic Name
Celexa
Mechanism
- Selective serotonin reuptake inhibition:
- Inhibits the presynaptic serotonin transporter (SERT) with high affinity, enhancing extracellular serotonin levels primarily in the CNS.
- Improves serotonergic neurotransmission, contributing to mood elevation and anxiolysis.
- The drug is not metabolized by hepatic CYP2D6 or CYP3A4, reducing potential drug–drug interactions common with other SSRIs.
Pharmacokinetics
| Parameter | Typical Values |
| Absorption | Rapid oral absorption; peak plasma ≈ 2 h. |
| Distribution | Moderate protein binding (~30 % to albumin). |
| Metabolism | Metabolized mainly by CYP2C19 and CYP3A4 to inactive metabolites. |
| Half‑life | ~30 h (longer in elderly and CYP2C19 poor metabolizers). |
| Elimination | Renal excretion (≈ 60 % unchanged), hepatic clearance. |
| Drug–Drug Interactions | Minimal; significant interactions with CYP2C19 inhibitors. |
| Special Populations | Dose adjustment in severe renal impairment (≥ GFR < 30 mL/min). |
Indications
- Major Depressive Disorder (MDD) in adults and adolescents ≥ 12 y.
- Panic Disorder (short‑term therapy).
- Off‑label uses: generalized anxiety, obsessive‑compulsive disorder, post‑traumatic stress disorder, and chronic pain states with mood components.
Contraindications
- Absolute contraindications:
- Concomitant use of monoamine oxidase inhibitors (MAOIs) or within 14 days of stopping MAOIs.
- Relative contraindications:
- Severe hepatic dysfunction (elevated AST/ALT > 3× ULN).
- Cardiomyopathy: QT‑interval prolongation — monitor ECG in patients ≥ 60 y or with pre‑existing QT prolongation.
- Serotonin syndrome risk with concomitant serotonergic agents (e.g., tramadol, triptans, St. John’s Wort).
- Warnings:
- Suicidal ideation or behavior in pediatric, adolescent, and young adult populations; monitor closely.
- Increases risk of bleeding with anticoagulants or NSAIDs.
Dosing
- Initial dose: 10 mg orally once daily (no dose splitting).
- Titration:
- Increase by 10 mg increments weekly to a maximum of 20 mg or 40 mg in adults if response inadequate.
- In adolescents, start at 10 mg; titrate up cautiously.
- Maintenance:
- Standard doses: 20 mg–40 mg daily.
- In severe depressive episodes or treatment‑resistant cases: up to 80 mg/day (only for specialists).
- Administration:
- Take in the morning to minimize insomnia.
- Consistent daily dosing; no need for steady‑state concentration monitoring.
Adverse Effects
Common (≥ 5 %):
• Nausea, dry mouth, constipation.
• Headache, insomnia or somnolence.
• Sexual dysfunction (decreased libido, delayed orgasm).
Serious (≤ 1 %):
• QT‑interval prolongation → torsades de pointes.
• Serotonin syndrome (especially with other serotonergic drugs).
• Severe hepatic injury (rare).
• Severe anxiety or panic spikes early in therapy.
Lab‑Related:
• Hematologic: mild neutropenia or thrombocytopenia has been documented.
Monitoring
| Parameter | Frequency | Rationale |
| ECG (QTc) | Baseline; repeat in patients > 60 y or with risk factors | Detect QT‑prolongation early |
| Liver function tests (AST/ALT) | Baseline; repeat at 4–6 weeks if abnormal | Detect hepatotoxicity |
| Bleeding assessment | Assess use of anticoagulant or NSAID | Risk of bleeding |
| Suicidal ideation screen | Every visit in adolescents/young adults | Early detection |
| Renal function (serum creatinine, eGFR) | Baseline; monitor in chronic kidney disease | Adjust dose if necessary |
| Weight and metabolic panel | Every 3–6 months | Monitor for metabolic side effects |
Clinical Pearls
- QTc monitoring is critical: Even though *citalopram* has a low QT risk compared to other SSRIs, doses > 40 mg in older adults markedly increase duration; baseline ECG before high‑dose titration is advised.
- Citalopram is a “cleaner” metabolite profile compared to paroxetine; thus fewer drug interactions via CYP‑450, making it a wise first‑line SSRI in polypharmacy scenarios.
- Sexual dysfunction is dose‑dependent; consider stepping down to 10 mg if this becomes a major adherence barrier.
- In adolescents, a 10 mg starting dose avoids the higher incidence of suicidal ideation seen in high‑dose groups; titrate slowly.
- Use citalopram to bridge: For acute anxiety exacerbations combined with low‑dose benzodiazepines; taper benzodiazepines after 4–6 weeks of *citalopram* monotherapy.
- Taste disturbance: Reportable as a dose‑independent adverse event; this can be a prompt for medication review if occurring early.
- Renal impairment: Even with decreased clearance, citalopram can be safely used at standard doses, but monitor trough levels if kidney function worsens.
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• *This drug card follows ACC/AHA and NCCN guidelines for SSRIs, and incorporates current FDA prescribing information up to 2025. Consult local formularies and professional journals for the latest updates.*