No

Antidepressant, Selective Serotonin Reuptake Inhibitor

Depression

C

Animal reproductive studies have revealed adverse effects on fetal and postnatal development (at doses higher than human therapeutic doses). Should be used in pregnancy only if potential benefit justifies potential risk. Citalopram is excreted in human milk; a decision should be made whether to continue or discontinue nursing or discontinue the drug.

Hypersensitivity to citalopram; use of MAO inhibitors within 14 days

Potential for severe reaction when used with MAO inhibitors - serotonin syndrome (hyperthermia, muscular rigidity, mental status changes/agitation, autonomic instability) may occur. May precipitate a shift to mania or hypomania in patients with bipolar disease. Has a low potential to impair cognitive or motor performance - caution operating hazardous machinery or driving. Use caution in patients with depression, particularly if suicidal risk may be present. Use caution in patients with a previous seizure disorder or condition predisposing to seizures such as brain damage, alcoholism, or concurrent therapy with other drugs which lower the seizure threshold. Use with caution in patients with hepatic or renal dysfunction and in elderly patients. May cause hyponatremia/SIADH. Use with caution in patients with other concurrent illness (due to limited experience). May cause or exacerbate sexual dysfunction.

>10%:

Central nervous system: Somnolence, insomnia

Gastrointestinal: Nausea, xerostomia

Miscellaneous: Diaphoresis

<10%:

Central nervous system: Anxiety, anorexia, agitation, yawning

Dermatologic: Rash, pruritus

Gastrointestinal: Diarrhea, dyspepsia, vomiting, abdominal pain

Endocrine & metabolic: Sexual dysfunction

Neuromuscular & skeletal: Tremor, arthralgia, myalgia

Respiratory: Cough, rhinitis, sinusitis

Signs of overdose include: Dizziness, nausea, vomiting, sweating, tremor, somnolence, sinus tachycardia. Rare symptoms have included amnesia, confusion, coma, seizures, hyperventilation, EKG changes (including QT_c prolongation, ventricular arrhythmia, and torsade de pointes); management is supportive.

CYP3A3/4 and CYP2C19 enzyme substrate; CYP2D6, 1A2, and 2C19 enzyme inhibitor (weak)

Cimetidine may inhibit the metabolism of citalopram

The combined use of citalopram with buspirone, MAO inhibitors, moclobemide, nefazodone, or tramadol may result in serotonin syndrome

Citalopram may increase plasma level of metoprolol

Store below 25°C

A bicyclic phthalane derivative, citalopram selectively inhibits serotonin reuptake in the presynaptic neurons

Onset of effect: Usually >2 weeks

Distribution: V_d: 12 L/kg

Protein binding, plasma: ~80%

Metabolism: Extensive hepatic metabolism, including cytochrome P-450 oxidase system, to N-demethylated, N-oxide, and deaminated metabolites

Bioavailability: 80%

Half-life: 24-48 hours; average 35 hours (doubled in patients with hepatic impairment)

Time to peak serum concentration: 1-6 hours, average within 4 hours

Elimination: 10% recovered unchanged in urine; systemic clearance: 330 mL/minute (20% renal)

Clearance was decreased, while AUC and half-life were significantly increased in elderly patients and in patients with hepatic impairment. Mild to moderate renal impairment may reduce clearance of citalopram (17% reduction noted in trials). No pharmacokinetic information is available concerning patients with severe renal impairment.

Oral: Initial: 20 mg/day, generally with an increase to 40 mg/day; doses of more than 40 mg are not usually necessary. Should a dose increase be necessary, it should occur in 20 mg increments at intervals of no less than 1 week. Maximum dose: 60 mg/day; reduce dosage in elderly or those with hepatic impairment.

Monitor patient periodically for symptom resolution, heart rate, blood pressure, liver function tests, and CBC with continued therapy

Although caution should be used in patients taking tricyclic antidepressants, no interactions have been reported with vasoconstrictors and fluoxetine, a nontricyclic antidepressant which acts to increase serotonin

Dry mouth in >10% of patients; premarketing trials reported abnormal taste

The effects of this medication may take up to 3 weeks. Take as directed; do not alter dose or frequency without consulting prescriber. Avoid alcohol, caffeine, and CNS stimulants. You may experience sexual dysfunction (reversible). May cause dizziness, anxiety, or blurred vision (rise slowly from sitting or lying position and use caution when driving or engaging in tasks requiring alertness until response to drug is known); nausea or dry mouth (frequent small meals, frequent mouth care, chewing gum, or sucking lozenges may help). Report confusion or impaired concentration, severe headache, palpitations, rash, insomnia or nightmares, changes in personality, muscle weakness or tremors, altered gait pattern, signs and symptoms of respiratory infection, or excessive perspiration. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to be pregnant. Do not breast-feed.

Solution, oral: 10 mg/5 mL

Tablet, as hydrobromide: 20 mg, 40 mg, 60 mg