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ALERT: U.S. Boxed Warning
The FDA-approved labeling includes a boxed warning. See Warnings/Precautions section for a concise summary of this information. For verbatim wording of the boxed warning, consult the product labeling or www.fda.gov.
Pronunciation
(sye TAL oh pram)
Generic Available (U.S.)
Yes
Index Terms
Medication Guide
An FDA-approved patient medication guide, which is available with the product information and at http://www.fda.gov/downloads/Drugs/DrugSafety/ucm088568.pdf, must be dispensed with this medication.
U.S. Brand Names
Canadian Brand Names
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Treatment of depression
Use: Unlabeled/Investigational
Treatment of mild dementia-associated agitation in nonpsychotic patients; smoking cessation; ethanol abuse; obsessive-compulsive disorder (OCD) in children; diabetic neuropathy
Pregnancy Risk Factor
C
Pregnancy Considerations
Due to adverse effects observed in animal studies, citalopram is classified as pregnancy category C. Citalopram and its metabolites cross the human placenta. Nonteratogenic effects in the newborn following SSRI exposure late in the third trimester include respiratory distress, cyanosis, apnea, seizures, temperature instability, feeding difficulty, vomiting, hypoglycemia, hypo- or hypertonia, hyper-reflexia, jitteriness, irritability, constant crying, and tremor. An increased risk of low birth weight and lower Apgar scores have also been reported. Exposure to SSRIs after the twentieth week of gestation has been associated with persistent pulmonary hypertension of the newborn (PPHN). Adverse effects may be due to toxic effects of the SSRI or drug withdrawal without a taper. The long-term effects of in utero SSRI exposure on infant development and behavior are not known.Due to pregnancy-induced physiologic changes, women who are pregnant may require increased doses of citalopram to achieve euthymia. Women treated for major depression and who are euthymic prior to pregnancy are more likely to experience a relapse when medication is discontinued as compared to pregnant women who continue taking antidepressant medications. The ACOG recommends that therapy with SSRIs or SNRIs during pregnancy be individualized; treatment of depression during pregnancy should incorporate the clinical expertise of the mental health clinician, obstetrician, primary healthcare provider, and pediatrician. If treatment during pregnancy is required, consider tapering therapy during the third trimester in order to prevent withdrawal symptoms in the infant. If this is done and the woman is considered to be at risk of relapse from her major depressive disorder, the medication can be restarted following delivery, although the dose should be readjusted to that required before pregnancy. Treatment algorithms have been developed by the ACOG and the APA for the management of depression in women prior to conception and during pregnancy (Yonkers, 2009).
Lactation
Enters breast milk/consider risk:benefit
Breast-Feeding Considerations
Citalopram and its metabolites are excreted in human milk. According to the manufacturer, the decision to continue or discontinue breast-feeding during therapy should take into account the risk of exposure to the infant and the benefits of treatment to the mother. Excessive somnolence, decreased feeding, colic, irritability, restlessness, and weight loss have been reported in breast-fed infants. The long-term effects on development and behavior have not been studied; therefore, citalopram should be prescribed to a mother who is breast-feeding only when the benefits outweigh the potential risks.
Contraindications
Hypersensitivity to citalopram or any component of the formulation; concomitant use with MAO inhibitors or within 2 weeks of discontinuing MAO inhibitors; concomitant use with pimozide
Warnings/Precautions
Boxed warnings:
• Suicidal thinking/behavior: See “Major psychiatric warnings” below.
Major psychiatric warnings:
• [U.S. Boxed Warning]: Antidepressants increase the risk of suicidal thinking and behavior in children, adolescents, and young adults (18-24 years of age) with major depressive disorder (MDD) and other psychiatric disorders; consider risk prior to prescribing. Short-term studies did not show an increased risk in patients >24 years of age and showed a decreased risk in patients ≥65 years. Closely monitor patients for clinical worsening, suicidality, or unusual changes in behavior, particularly during the initial 1-2 months of therapy or during periods of dosage adjustments (increases or decreases); the patient's family or caregiver should be instructed to closely observe the patient and communicate condition with healthcare provider. A medication guide concerning the use of antidepressants should be dispensed with each prescription. Citalopram is not FDA approved for use in children.
• The possibility of a suicide attempt is inherent in major depression and may persist until remission occurs. Patients treated with antidepressants should be observed for clinical worsening and suicidality, especially during the initial few months of a course of drug therapy, or at times of dose changes, either increases or decreases. Worsening depression and severe abrupt suicidality that are not part of the presenting symptoms may require discontinuation or modification of drug therapy. Use caution in high-risk patients during initiation of therapy.
• Prescriptions should be written for the smallest quantity consistent with good patient care. The patient's family or caregiver should be alerted to monitor patients for the emergence of suicidality and associated behaviors such as anxiety, agitation, panic attacks, insomnia, irritability, hostility, impulsivity, akathisia, hypomania, and mania; patients should be instructed to notify their healthcare provider if any of these symptoms or worsening depression or psychosis occur.
• May worsen psychosis in some patients or precipitate a shift to mania or hypomania in patients with bipolar disorder. Monotherapy in patients with bipolar disorder should be avoided. Patients presenting with depressive symptoms should be screened for bipolar disorder. Citalopram is not FDA approved for the treatment of bipolar depression.
Concerns related to adverse effects:
• Anticholinergic effects: Relatively devoid of these side effects.
• Bleeding risk: May impair platelet aggregation resulting in increased risk of bleeding events, particularly if used concomitantly with aspirin, NSAIDs, warfarin, or other anticoagulants. Bleeding (including GI bleeding) related to SSRI or SNRI use has been reported to range from relatively minor bruising and epistaxis to life-threatening hemorrhage.
• CNS depression: Has a low potential to impair cognitive or motor performance; caution operating hazardous machinery or driving.
• Serotonin syndrome (SS)/neuroleptic malignant syndrome (NMS)-like reactions: SS and NMS-like reactions have occurred with serotonin/norepinephrine reuptake inhibitors (SNRIs) and selective serotonin reuptake inhibitors (SSRIs) when used alone, and particularly when used in combination with serotonergic agents (eg, triptans) or antidopaminergic agents (eg, antipsychotics). The diagnosis of SS can be made using the Hunter Serotonin Toxicity Criteria (Dunkley, 2003). Identification and differentiation of SS (eg, tremor, myoclonus, agitation) and more severe NMS-like reactions (eg, hyperthermia, muscle rigidity, autonomic instability, mental status changes) can be complex; monitor patients closely for either syndrome. Discontinue treatment (and any concomitant serotonergic and/or antidopaminergic agents) immediately if signs/symptoms arise.
• Sexual dysfunction: May cause or exacerbate sexual dysfunction.
• SIADH and hyponatremia: SSRIs and SNRIs have been associated with the development of SIADH; hyponatremia has been reported rarely (including severe cases with serum sodium <110 mmol/L), predominately in the elderly; reversible with discontinuation of treatment. Volume depletion and/or concurrent use of diuretics likely increases risk.
Disease-related concerns:
• Hepatic impairment: Use with caution in patients with hepatic impairment; clearance is decreased and plasma concentrations are increased; a lower dosage may be needed.
• Renal impairment: Use with caution in patients with severe renal impairment.
Concurrent drug therapy issues:
• Anticoagulants/Antiplatelets: Use caution with concomitant use of aspirin, NSAIDs, warfarin, or other drugs that affect coagulation; the risk of bleeding may be potentiated.
• CNS depressants: Use caution with concomitant therapy.
• MAO inhibitors: Potential for severe reaction when used with MAO inhibitors; autonomic instability, coma, death, delirium, diaphoresis, hyperthermia, mental status changes/agitation, muscular rigidity, myoclonus, neuroleptic malignant syndrome features, and seizures may occur. Concurrent use is contraindicated.
• Serotonin syndrome/NMS-like reactions: Symptoms of agitation, confusion, hallucinations, hyper-reflexia, myoclonus, shivering, and tachycardia may occur with concomitant proserotonergic drugs (ie, SSRIs/SNRIs or triptans), agents which reduce citalopram's metabolism, or antidopaminergic agents (including antipsychotics). Concurrent use of serotonin precursors (eg, tryptophan) is not recommended.
Special populations:
• Elderly: Use caution in elderly patients; risk of hyponatremia and other adverse events may be increased.
• Pediatrics: Safety and efficacy in children have not been established.
• Pregnancy: Use caution in pregnant patients; high doses of citalopram have been associated with teratogenicity in animals.
Other warnings/precautions:
• Electroconvulsive therapy (ECT): Use with caution; no clinical studies have assessed the combined use of citalopram and electroconvulsive therapy; may increase the risks (eg, cognitive adverse effects) associated with electroconvulsive therapy; consider discontinuing, when possible, prior to ECT treatment.
• Withdrawal syndrome: May cause dysphoric mood, irritability, agitation, dizziness, sensory disturbances, anxiety, confusion, headache, lethargy, emotional lability, insomnia, hypomania, tinnitus, and seizures. Upon discontinuation of citalopram therapy, gradually taper dose. If intolerable symptoms occur following a decrease in dosage or upon discontinuation of therapy, then resuming the previous dose with a more gradual taper should be considered.
Adverse Reactions
>10%:
Central nervous system: Somnolence (18%; dose related), insomnia (15%; dose related)
Gastrointestinal: Nausea (21%), xerostomia (20%)
Miscellaneous: Diaphoresis (11%; dose related)
1% to 10%:
Cardiovascular: Heart rate decreased, postural hypotension, tachycardia
Central nervous system: Fatigue (5%; dose related), anorexia (4%), anxiety (4%), agitation (3%), fever (2%), yawning (2%; dose related), amnesia, apathy, concentration impaired, confusion, depression, migraine, suicide attempt
Dermatologic: Rash, pruritus
Endocrine & metabolic: Libido decreased (1% to 4%), dysmenorrhea (3%), amenorrhea, sexual dysfunction
Gastrointestinal: Diarrhea (8%), dyspepsia (5%), vomiting (4%), abdominal pain (3%), flatulence, salivation increased, taste perversion, weight gain/loss
Genitourinary: Ejaculation disorder (6%), impotence (3%; dose related), polyuria
Neuromuscular & skeletal: Tremor (8%), arthralgia (2%), myalgia (2%), paresthesia
Ocular: Abnormal accommodation
Respiratory: Rhinitis (5%), upper respiratory tract infection (5%), sinusitis (3%), cough
<1% (Limited to important or life threatening): Aggressiveness, alkaline phosphatase increased, alopecia, anemia, angina pectoris, ataxia, cardiac failure, cerebral vascular accident, dyspnea, dystonia, eczema, edema (extremities), epistaxis, extrapyramidal symptoms, extrasystoles, hallucinations, hypertension, leukocytosis, leukopenia, liver enzymes increased, lymphadenopathy, muscle weakness, myocardial infarction, neuralgia, photosensitivity, purpura, rigors, tinnitus, urinary incontinence, urinary retention, urticaria
Postmarketing and/or case reports: Acute renal failure, akathisia, allergic reaction, anaphylaxis, angioedema, choreoathetosis, chest pain, delirium, dyskinesia, ecchymosis, epidermal necrolysis, erythema multiforme, gastrointestinal hemorrhage, glaucoma, grand mal seizure, hemolytic anemia, hepatic necrosis, hyponatremia, myoclonus, neuroleptic malignant syndrome, nystagmus, pancreatitis, priapism, prolactinemia, prothrombin decreased, QT prolonged, rhabdomyolysis, serotonin syndrome, SIADH, spontaneous abortion, thrombocytopenia, thrombosis, ventricular arrhythmia, torsade de pointes, withdrawal syndrome
Metabolism/Transport Effects
Substrate of CYP2C19 (major), 2D6 (minor), 3A4 (major); Inhibits CYP1A2 (weak), 2B6 (weak), 2C19 (weak), 2D6 (weak)
Drug Interactions
Alcohol (Ethyl): May enhance the adverse/toxic effect of Selective Serotonin Reuptake Inhibitors. Specifically, the risk of psychomotor impairment may be enhanced. Management: Patients receiving selective serotonin reuptake inhibitors should be advised to avoid alcohol. Monitor for increased psychomotor impairment in patients who consume alcohol during treatment with selective serotonin reuptake inhibitors. Risk D: Consider therapy modification
Alfuzosin: May enhance the QTc-prolonging effect of QTc-Prolonging Agents. Risk C: Monitor therapy
Alpha-/Beta-Blockers: Selective Serotonin Reuptake Inhibitors may decrease the metabolism of Alpha-/Beta-Blockers. Risk C: Monitor therapy
Analgesics (Opioid): May enhance the serotonergic effect of Selective Serotonin Reuptake Inhibitors. This may cause serotonin syndrome. Risk C: Monitor therapy
Anticoagulants: Antiplatelet Agents may enhance the anticoagulant effect of Anticoagulants. Risk C: Monitor therapy
Antidepressants (Serotonin Reuptake Inhibitor/Antagonist): Selective Serotonin Reuptake Inhibitors may enhance the serotonergic effect of Antidepressants (Serotonin Reuptake Inhibitor/Antagonist). This may cause serotonin syndrome. Risk C: Monitor therapy
Antiplatelet Agents: May enhance the anticoagulant effect of other Antiplatelet Agents. Risk C: Monitor therapy
Artemether: May enhance the QTc-prolonging effect of QTc-Prolonging Agents. Risk X: Avoid combination
Aspirin: Selective Serotonin Reuptake Inhibitors may enhance the antiplatelet effect of Aspirin. Risk C: Monitor therapy
BusPIRone: May enhance the serotonergic effect of Selective Serotonin Reuptake Inhibitors. This may cause serotonin syndrome. Selective Serotonin Reuptake Inhibitors may decrease the metabolism of BusPIRone. Risk C: Monitor therapy
CarBAMazepine: May increase the metabolism of Selective Serotonin Reuptake Inhibitors. Specifically those agents metabolized via CYP1A2, 2C, and/or 3A4 isoenzymes. Selective Serotonin Reuptake Inhibitors may decrease the metabolism of CarBAMazepine. Specifically those SSRIs that inhibit CYP3A4 isoenzymes. Risk D: Consider therapy modification
Chloroquine: May enhance the QTc-prolonging effect of QTc-Prolonging Agents. Risk C: Monitor therapy
Cimetidine: May decrease the metabolism of Selective Serotonin Reuptake Inhibitors. Risk D: Consider therapy modification
Ciprofloxacin: May enhance the QTc-prolonging effect of QTc-Prolonging Agents. Risk C: Monitor therapy
Ciprofloxacin (Systemic): May enhance the QTc-prolonging effect of QTc-Prolonging Agents. Risk C: Monitor therapy
CloZAPine: Selective Serotonin Reuptake Inhibitors may decrease the metabolism of CloZAPine. Risk D: Consider therapy modification
CNS Depressants: May enhance the adverse/toxic effect of Selective Serotonin Reuptake Inhibitors. Specifically, the risk of psychomotor impairment may be enhanced. Risk C: Monitor therapy
Collagenase (Systemic): Antiplatelet Agents may enhance the adverse/toxic effect of Collagenase (Systemic). Specifically, the risk of injection site bruising and/or bleeding may be increased. Risk C: Monitor therapy
Conivaptan: May increase the serum concentration of CYP3A4 Substrates. Management: Upon completion/discontinuation of conivaptan, allow at least 7 days before initiating therapy with drugs that are CYP3A4 substrates. Risk D: Consider therapy modification
CYP2C19 Inducers (Strong): May increase the metabolism of CYP2C19 Substrates. Risk C: Monitor therapy
CYP2C19 Inhibitors (Moderate): May decrease the metabolism of CYP2C19 Substrates. Risk C: Monitor therapy
CYP2C19 Inhibitors (Strong): May decrease the metabolism of CYP2C19 Substrates. Risk D: Consider therapy modification
CYP3A4 Inducers (Strong): May increase the metabolism of CYP3A4 Substrates. Risk C: Monitor therapy
CYP3A4 Inhibitors (Moderate): May decrease the metabolism of CYP3A4 Substrates. Risk C: Monitor therapy
CYP3A4 Inhibitors (Strong): May decrease the metabolism of CYP3A4 Substrates. Risk D: Consider therapy modification
Cyproheptadine: May diminish the therapeutic effect of Selective Serotonin Reuptake Inhibitors. Risk C: Monitor therapy
Deferasirox: May decrease the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy
Desmopressin: Selective Serotonin Reuptake Inhibitors may enhance the adverse/toxic effect of Desmopressin. Risk C: Monitor therapy
Dextromethorphan: Selective Serotonin Reuptake Inhibitors may enhance the adverse/toxic effect of Dextromethorphan. Risk D: Consider therapy modification
Dronedarone: QTc-Prolonging Agents may enhance the QTc-prolonging effect of Dronedarone. Risk X: Avoid combination
Drotrecogin Alfa: Antiplatelet Agents may enhance the adverse/toxic effect of Drotrecogin Alfa. Bleeding may occur. Management: When possible, avoid use of drotrecogin within 7 days of use of any IIb/IIIa antagonists, higher dose aspirin (more than 650 mg/day), or use of other antiplatelet agents. Risk D: Consider therapy modification
Fluconazole: May increase the serum concentration of Citalopram. Risk C: Monitor therapy
Gadobutrol: May enhance the QTc-prolonging effect of QTc-Prolonging Agents. Risk D: Consider therapy modification
Glucosamine: May enhance the antiplatelet effect of Antiplatelet Agents. Risk C: Monitor therapy
Haloperidol: Selective Serotonin Reuptake Inhibitors may decrease the metabolism of Haloperidol. Risk C: Monitor therapy
Herbs (Anticoagulant/Antiplatelet Properties) (eg, Alfalfa, Anise, Bilberry): May enhance the adverse/toxic effect of Antiplatelet Agents. Bleeding may occur. Risk D: Consider therapy modification
Ibritumomab: Antiplatelet Agents may enhance the adverse/toxic effect of Ibritumomab. Both agents may contribute to impaired platelet function and an increased risk of bleeding. Risk C: Monitor therapy
Iobenguane I 123: Selective Serotonin Reuptake Inhibitors may diminish the therapeutic effect of Iobenguane I 123. Risk X: Avoid combination
Lithium: Selective Serotonin Reuptake Inhibitors may enhance the adverse/toxic effect of Lithium. Risk C: Monitor therapy
Lumefantrine: May enhance the QTc-prolonging effect of QTc-Prolonging Agents. Risk X: Avoid combination
Macrolide Antibiotics: May decrease the metabolism of Selective Serotonin Reuptake Inhibitors. Exceptions: Azithromycin; Azithromycin (Systemic); Spiramycin. Risk C: Monitor therapy
MAO Inhibitors: May enhance the serotonergic effect of Selective Serotonin Reuptake Inhibitors. This may cause serotonin syndrome. Risk X: Avoid combination
Methadone: Selective Serotonin Reuptake Inhibitors may decrease the metabolism of Methadone. Fluvoxamine appears to be the only interacting SSRI. Risk D: Consider therapy modification
Methylene Blue: Selective Serotonin Reuptake Inhibitors may enhance the serotonergic effect of Methylene Blue. This could result in serotonin syndrome. Risk X: Avoid combination
Metoclopramide: May enhance the adverse/toxic effect of Selective Serotonin Reuptake Inhibitors. Management: Seek alternatives to this combination when possible. Monitor patients receiving metoclopramide with selective serotonin reuptake inhibitors for signs of extrapyramidal symptoms, neuroleptic malignant syndrome, and serotonin syndrome. Risk D: Consider therapy modification
Mexiletine: Selective Serotonin Reuptake Inhibitors may decrease the metabolism of Mexiletine. Risk D: Consider therapy modification
Nilotinib: May enhance the QTc-prolonging effect of QTc-Prolonging Agents. Risk X: Avoid combination
NSAID (COX-2 Inhibitor): Selective Serotonin Reuptake Inhibitors may enhance the antiplatelet effect of NSAID (COX-2 Inhibitor). Risk D: Consider therapy modification
NSAID (Nonselective): Selective Serotonin Reuptake Inhibitors may enhance the antiplatelet effect of NSAID (Nonselective). NSAID (Nonselective) may diminish the therapeutic effect of Selective Serotonin Reuptake Inhibitors. Management: Consider using alternative analgesics, when appropriate, and/or addition of an gastroprotective agent. Monitor patients closely for signs/symptoms of bleeding, and for evidence of diminished SSRI effectiveness with concurrent use. Risk D: Consider therapy modification
Omega-3-Acid Ethyl Esters: May enhance the antiplatelet effect of Antiplatelet Agents. Risk C: Monitor therapy
Peginterferon Alfa-2b: May decrease the serum concentration of CYP2D6 Substrates. Risk C: Monitor therapy
Pentosan Polysulfate Sodium: May enhance the adverse/toxic effect of Antiplatelet Agents. Specifically, the risk of bleeding may be increased by concurrent use of these agents. Risk C: Monitor therapy
Pentoxifylline: May enhance the antiplatelet effect of Antiplatelet Agents. Risk C: Monitor therapy
Pimozide: Selective Serotonin Reuptake Inhibitors may enhance the adverse/toxic effect of Pimozide. Risk X: Avoid combination
Pimozide: QTc-Prolonging Agents may enhance the QTc-prolonging effect of Pimozide. Risk X: Avoid combination
Prostacyclin Analogues: May enhance the antiplatelet effect of Antiplatelet Agents. Risk C: Monitor therapy
QTc-Prolonging Agents: May enhance the adverse/toxic effect of other QTc-Prolonging Agents. Their effects can be additive, causing life-threatening ventricular arrhythmias. Risk D: Consider therapy modification
QuiNINE: QTc-Prolonging Agents may enhance the QTc-prolonging effect of QuiNINE. QuiNINE may enhance the QTc-prolonging effect of QTc-Prolonging Agents. Risk X: Avoid combination
RisperiDONE: Selective Serotonin Reuptake Inhibitors may decrease the metabolism of RisperiDONE. Risk C: Monitor therapy
Salicylates: Antiplatelet Agents may enhance the adverse/toxic effect of Salicylates. Increased risk of bleeding may result. Risk C: Monitor therapy
Serotonin Modulators: May enhance the adverse/toxic effect of other Serotonin Modulators. The development of serotonin syndrome may occur. Risk D: Consider therapy modification
Sibutramine: May enhance the serotonergic effect of Serotonin Modulators. This may cause serotonin syndrome. Risk X: Avoid combination
Tetrabenazine: QTc-Prolonging Agents may enhance the QTc-prolonging effect of Tetrabenazine. Risk X: Avoid combination
Thioridazine: QTc-Prolonging Agents may enhance the QTc-prolonging effect of Thioridazine. Risk X: Avoid combination
Thrombolytic Agents: Antiplatelet Agents may enhance the anticoagulant effect of Thrombolytic Agents. Risk C: Monitor therapy
Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy
Toremifene: QTc-Prolonging Agents may enhance the QTc-prolonging effect of Toremifene. The risk for potentially dangerous arrhythmias may be increased. Risk X: Avoid combination
Tositumomab and Iodine I 131 Tositumomab: Antiplatelet Agents may enhance the adverse/toxic effect of Tositumomab and Iodine I 131 Tositumomab. Specifically, the risk of bleeding-related adverse events may be increased. Risk C: Monitor therapy
TraMADol: Selective Serotonin Reuptake Inhibitors may enhance the neuroexcitatory and/or seizure-potentiating effect of TraMADol. TraMADol may enhance the serotonergic effect of Selective Serotonin Reuptake Inhibitors. This may cause serotonin syndrome. Risk D: Consider therapy modification
Tricyclic Antidepressants: Selective Serotonin Reuptake Inhibitors may decrease the metabolism of Tricyclic Antidepressants. Risk D: Consider therapy modification
Tryptophan: May enhance the serotonergic effect of Selective Serotonin Reuptake Inhibitors. This may cause serotonin syndrome. Risk X: Avoid combination
Vandetanib: QTc-Prolonging Agents may enhance the arrhythmogenic effect of Vandetanib. Risk X: Avoid combination
Vitamin K Antagonists (eg, warfarin): Selective Serotonin Reuptake Inhibitors may enhance the anticoagulant effect of Vitamin K Antagonists. Risk C: Monitor therapy
Ziprasidone: QTc-Prolonging Agents may enhance the QTc-prolonging effect of Ziprasidone. The risk of a severe arrhythmia may be increased. Risk X: Avoid combination
Ethanol/Nutrition/Herb Interactions
Ethanol: May increase CNS depression; monitor for increased effects with coadministration. Caution patients about effects.
Herb/Nutraceutical: Avoid valerian, St John's wort, SAMe, kava kava, and gotu kola (may increase CNS depression).
Storage
Store at 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F).
Mechanism of Action
A racemic bicyclic phthalane derivative, citalopram selectively inhibits serotonin reuptake in the presynaptic neurons and has minimal effects on norepinephrine or dopamine. Uptake inhibition of serotonin is primarily due to the S-enantiomer of citalopram. Displays little to no affinity for serotonin, dopamine, adrenergic, histamine, GABA, or muscarinic receptor subtypes.
Pharmacodynamics/Kinetics
Onset of action: Depression: The onset of action is within a week; however, individual response varies greatly and full response may not be seen until 8-12 weeks after initiation of treatment.
Distribution: Vd: 12 L/kg
Protein binding, plasma: ~80%
Metabolism: Extensively hepatic, via CYP3A4 and 2C19 (major pathways), and 2D6 (minor pathway); forms metabolites, N-demethylcitalopram (DCT) and didemethylcitalopram (DDCT) which are at least eight times less potent than citalopram
Bioavailability: 80%
Half-life elimination: 24-48 hours (average: 35 hours); doubled with hepatic impairment
Time to peak, serum: 1-6 hours, average within 4 hours
Excretion: Urine (Citalopram 10% and DCT 5%)
Note: 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 (17%) and prolong half-life of citalopram. No pharmacokinetic information is available concerning patients with severe renal impairment.
Dosage
Oral:
Children and Adolescents: Obsessive-compulsive disorder (unlabeled use): 10-40 mg/day
Adults: Depression: 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.
Elderly:
Depression: Initial: 20 mg once daily; increase dose to 40 mg/day in nonresponsive patients
Alzheimer's dementia-related depression (unlabeled use): Initial: 5-10 mg/day; may increase at multi-week intervals to maximum of 40 mg/day
Dosage adjustment in renal impairment:
Mild-to-moderate impairment: No dosage adjustment needed
Severe impairment: Clcr <20 mL/minute: Use with caution
Dosage adjustment in hepatic impairment: 20 mg once daily; increase dose to 40 mg/day in nonresponsive patients
Administration: Oral
May be administered without regard to food.
Monitoring Parameters
Monitor patient periodically for symptom resolution; mental status for depression, suicidal ideation (especially at the beginning of therapy or when doses are increased or decreased), anxiety, social functioning, mania, panic attacks; akathisia
Dietary Considerations
May be taken without regard to food.
Patient Education
It may take up to 3 weeks to see therapeutic effects from this medication. May be taken with or without food. Avoid alcohol. You may experience sexual dysfunction (reversible). May cause dizziness, anxiety, blurred vision, nausea, or dry mouth. Report confusion or impaired concentration, suicide ideation, 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.
Geriatric Considerations
In open-label and placebo-controlled studies, elderly patients with or without dementia have shown significant improvement in depressive symptoms, irritability, anxiety, behavior, and restlessness. Effects on intellectual function have not been consistent. Thus, it appears that citalopram has additional effects in stabilizing emotion. A seven- to eightfold variation in citalopram S(+) (active) and R(-) enantiomer concentrations have been reported in the elderly. The racemic citalopram concentration-to-dose ratio was 1.8 times greater in elderly patients compared to younger patients.
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. The elderly are more prone to SSRI/SNRI-induced hyponatremia.
Dental Health: Effects on Dental Treatment
Key adverse event(s) related to dental treatment: Xerostomia (normal salivary flow resumes upon discontinuation). Premarketing trials reported abnormal taste. See Effects on Bleeding and Dental Health Professional Considerations.
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
Although caution should be used in patients taking tricyclic antidepressants, no interactions have been reported with vasoconstrictors and citalopram, a nontricyclic antidepressant which acts to increase serotonin; no precautions appear to be needed
Dental Comment
Problems with SSRI-induced bruxism have been reported and may preclude their use; clinicians attempting to evaluate any patient with bruxism or involuntary muscle movement, who is simultaneously being treated with an SSRI drug, should be aware of the potential association.
Mental Health: Child/Adolescent Considerations
Twenty-three patients with OCD (9-18 years of age) received 10-40 mg/day (40 mg modal) (Thomsen, 1997).
Thomsen PH, “Child and Adolescent Obsessive-Compulsive Disorder Treated With Citalopram: Findings From an Open Trial of 23 Cases,” J Child Adolesc Psychopharmacol, 1997, 7(3):157-66.
Wagner KD, Robb AS, Findling RL, et al, "A Randomized, Placebo-Controlled Trial of Citalopram for the Treatment of Major Depression in Children and Adolescents," Am J Psychiatry, 2004, 161(6):1079-83.
Mental Health: Comment
The SSRIs as a class are generally considered to be safe and equally effective. Allow sufficient dose-response time (6-12 weeks). Differences lie in approved indications, receptor profiles, pharmacokinetics, and cytochrome P450 activity profile. Subtle differences exist in adverse effect profiles. All SSRIs have the potential to cause sexual dysfunction. Among the SSRIs, citalopram possesses a mild effect on CYP isoenzymes.
Nursing: Physical Assessment/Monitoring
Assess mental status for depression, signs of clinical worsening, suicide ideation, anxiety, social functioning, mania, or panic attack. Teach patient hypotensive precautions. Taper dosage slowly when discontinuing.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, oral: 10 mg/5 mL (240 mL)
Tablet, oral: 10 mg, 20 mg, 40 mg
CeleXA®: 10 mg
CeleXA®: 20 mg, 40 mg [scored]
Pricing: U.S. (www.drugstore.com)
Solution (Citalopram Hydrobromide)
10 mg/5 mL (240): $99.99
Tablets (CeleXA)
10 mg (30): $110.99
20 mg (30): $120.49
40 mg (30): $128.29
Tablets (Citalopram Hydrobromide)
40 mg (30): $26.99
References
American College of Obstetricians and Gynecologists, ACOG Practice Bulletin: Clinical Management Guidelines for Obstetricians-Gynecologists No. 92 April 2008 (Replaces Practice Bulletin Number 87, November 2007), “Use of Psychiatric Medications During Pregnancy and Lactation,” Obstet Gynecol, 2008, 111(4):1001-20.
Bernard L, Stern R, Lew D, et al, “Serotonin Syndrome After Concomitant Treatment With Linezolid and Citalopram,” Clin Infect Dis, 2003, 36(9):1197.
Boyer EW and Shannon M, “The Serotonin Syndrome,” N Engl J Med, 2005, 352:1112-20.
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Content last modified May 2011
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