Trade Names:Celexa- Tablets 10 mg- Tablets 20 mg- Tablets 40 mg- Oral solution 10 mg per 5 mLApo-Citalopram (Canada)CO Citalopram (Canada)Gen-Citalopram (Canada)PMS-Citalopram (Canada)RAN-Citalopram (Canada)ratio-Citalopram (Canada)Sandoz Citalopram (Canada)
Inhibits the CNS neuronal uptake of serotonin, potentiating serotonergic activity.
T max is about 4 h. About 80% bioavailable. Steady state reached in about 1 wk.
Vd is about 12 L/kg. About 80% bound to plasma proteins.
Metabolized in the liver; CYP3A4 and CYP2C19 are the primary isozymes involved in N-demethylation of citalopram. Metabolites are demethylcitalopram (DCT), didemethylcitalopram (DDCT), citalopram-N-oxide, and deaminated propionic acid derivative; metabolites do not appear to contribute to antidepressant actions.
About 10% is excreted in urine as citalopram. Systemic Cl is 330 mL/min (about 20% is due to renal Cl). The t ½ is about 35 h.
Oral Cl decreased by 17%.Hepatic Function Impairment
Oral Cl decreased by 37% and t ½ doubled.ElderlySingle dose
AUC increased 30% and t ½ increased 50%.Multiple dose
AUC increased 23% and t ½ increased 30%.
Treatment of major depression as defined in DSM-III and DSM-III-R .
Treatment of panic disorder, obsessive-compulsive disorder, premenstrual dysphoria, posttraumatic stress disorder, generalized anxiety disorder.
Standard considerations; concomitant use of MAOIs or pimozide.
PO Initiate with 20 mg once daily and titrate up to 40 mg/day; max, 60 mg/day.Elderly
PO Initiate with 20 mg once daily; titrate up to 40 mg/day if needed.Hepatic Function Impairment
PO Initiate with 20 mg once daily; titrate up to 40 mg/day if needed.Maintenance
Periodically reevaluate long-term usefulness if used for extended periods.
Store tablets and oral solution at controlled room temperature (59° to 86°F).
Inhibition of beta-blocker's metabolism may occur, resulting in excessive beta blockade (eg, bradycardia). Coadministration of metoprolol with citalopram has increased plasma levels of metoprolol 2-fold.Cimetidine
Serum levels of citalopram may be increased 40%.CNS drugs
Use citalopram with caution in patient receiving CNS drugs.Cyproheptadine
May decrease the pharmacologic effect of citalopram.Ketoconazole
Ketoconazole plasma levels may be reduced slightly.Lithium
Lithium may enhance the serotonergic effects of citalopram; use caution if coadministered.MAOIs, pimozide
Concomitant use with citalopram is contraindicated.Sumatriptan
Rare postmarketing reports of weakness, hyperreflexia, and incoordination following coadministration.
None well documented.
Hypotension, postural hypotension, tachycardia (at least 1%); QT prolongation, ventricular arrhythmia, torsades de pointes (postmarketing).
Somnolence (18%); insomnia (15%); tremor (8%); fatigue (5%); anorexia, anxiety (4%); agitation (3%); decreased libido, dizziness, yawning (2%); asthenia (1%); aggravated depression, amnesia, apathy, confusion, depression, increased appetite, impaired concentration, migraine, paresthesia, suicide attempts (at least 1%); akathisia, delirium, dyskinesia, grand mal convulsions, neuroleptic malignant syndrome, nystagmus (postmarketing).
Increased sweating (11%); pruritus, rash (at least 1%), epidermal necrolysis, erythema multiforme (postmarketing).
Abnormal accommodation, taste perversion (at least 1%).
Nausea (21%); dry mouth (20%); diarrhea (8%); dyspepsia (5%); vomiting (4%); abdominal pain (3%); flatulence, increased saliva (at least 1%); GI hemorrhage, pancreatitis (postmarketing).
Ejaculation disorder (6%); dysmenorrhea, impotence (3%); amenorrhea, polyuria (at least 1%); acute renal failure. Priapism, prolactinemia, spontaneous abortion (postmarketing).
Ecchymosis, hemolytic anemia, thrombocytopenia, thrombosis (postmarketing).
Hepatic necrosis (postmarketing).
Decreased prothrombin (postmarketing).
Decreased weight (at least 1%).
Arthralgia, myalgia (2%); myoclonus, rhabdomyolysis (postmarketing).
Upper respiratory tract infection, rhinitis (5%); sinusitis (3%); coughing (at least 1%).
Fever (2%); allergic reaction, anaphylaxis, angioedema, choreoathetosis, chest pain, serotonin syndrome, withdrawal syndrome (postmarketing).
Antidepressants increased the risk of suicidal thinking and behavior (suicidality) in short-term studies in children and adolescents with major depressive disorder and other psychiatric disorders. When considering the use of any antidepressant in a child or adolescent, balance this risk with clinical need. Closely observe children or adolescents for clinical worsening, suicidality, or unusual changes in behavior during the initial few months of therapy or at times of increases or decreases in dose. Advise families and caregivers of the need for close observation and communication with the prescriber.
Monitor pediatric and adult patients for clinical worsening, suicidality, and unusual changes in behavior, especially during the first few months of therapy or at times of increases or decreases in dose. Evaluate children at least weekly with face-to-face contact with the patient or their family members or caregiver during the first 4 wk of therapy, then every other week for the next 4 wk, then at 12 wk, and as clinically indicated thereafter. The following symptoms may represent precursors to suicidality and should be reported to health care provider immediately if noted or suspected: aggressiveness, agitation, anxiety, hostility, hypomania, impulsivity, insomnia, irritability, mania, panic attacks, and psychomotor restlessness. Frequently assess patient for response to treatment. Periodically review therapy to determine if therapy needs to be continued without change or if a dose change (eg, increase, decrease, discontinuation) is indicated.
Category C . Neonates exposed to citalopram late in the third trimester have developed complications requiring prolonged hospitalization, respiratory support, and tube feeding. Consider potential risks and benefits of treatment when treating women during the third trimester.
Excreted in breast milk; may adversely affect infant.
Safety and efficacy not established.
May require lower dose; 20 mg/day is max recommended dose.
Use with caution in patients with severe renal impairment (CrCl less than 20 mL/min).
Use with caution; lower max dose is recommended.
May impair judgment, thinking, or motor skills.
Has been rarely reported.
Bleeding episodes have occurred in patients treated with psychotropic drugs that interfere with serotonin reuptake.
Has been reported. Use cautiously in patients with history of mania/hypomania.
Use with caution in patients with diseases or conditions that could affect hemodynamic responses or metabolism. Consider using lower or less frequent dosing.
Withdrawal symptoms have been reported following rapid discontinuation of therapy. If treatment is to be discontinued or the dose reduced, gradually taper the dose and monitor patient for withdrawal symptoms (eg, abnormal skin sensations, agitation, anxiety, confusion, dizziness, dysphoric mood, emotional lability, headaches, hypomania, insomnia, irritability, lethargy). If significant withdrawal symptoms develop, reinstitute previous dosing schedule and attempt a less rapid tapering regimen after patient has stabilized.
Hyponatremia and/or SIADH may occur. Use with caution in patients who are elderly, volume-depleted, or taking diuretics.
A major depressive episode may be the initial presentation of bipolar disorder and treating such an episode with an antidepressant alone may increase the likelihood of precipitating a mixed/manic episode in patients at risk for bipolar disorder. Screen patients with depression for risk of bipolar disorder prior to initiating therapy with an antidepressant.
May occur; use with caution in patients with a history of seizures or with conditions that potentially lower the seizure threshold. Discontinue use if seizures occur.
Suicidal ideation is inherent in depression and may persist until significant remission occurs. Closely supervise high-risk patients during initial drug therapy. Prescribe smallest quantity of medication consistent with good patient management in order to reduce risk of overdose.
Amnesia, coma, confusion, convulsions, cyanosis, dizziness, ECG changes (including QT prolongation, nodal rhythm, ventricular arrhythmia, torsades de pointes), hyperventilation, nausea, rhabdomyolysis, sinus tachycardia, somnolence, sweating, tremor, vomiting.
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