citalopram

Absorption: 80% absorbed after oral administration.

Distribution: Enters breast milk.

Metabolism/Excretion: Mostly metabolized by the liver (10% by the CYP3A4 and CYP2C19 isoenzymes); the CYP2C19 isoenzyme exhibits genetic polymorphism (2% of Whites, 4% of Blacks, and 14% of Asians may be poor metabolizers and may have significantly ↑ citalopram concentrations and an ↑ risk of adverse effects). Excreted unchanged in the urine.

Half-Life: 35 hr.

Time/Action Profile ⬆ ⬇

(antidepressant effect)

ROUTE	ONSET	PEAK	DURATION
PO	1–4 wk	unknown	unknown

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
Concurrent use of MAO inhibitors or MAO-like drugs (linezolid or methylene blue);
Concurrent use of pimozide;
Congenital long QT syndrome, bradycardia, hypokalemia, hypomagnesemia, recent myocardial infarction, decompensated heart failure (↑ risk of QT interval prolongation);
Concurrent use of QT interval prolonging drugs.

Use Cautiously in:

History of mania;
History of suicide attempt/ideation (↑ risk during early therapy and during dose adjustment);
History of seizure disorder;
Illnesses or conditions that are likely to result in altered metabolism or hemodynamic responses;
Severe renal or hepatic impairment (maximum dose of 20 mg/day in patients with hepatic impairment);
Poor CYP2C19 metabolizers (↑ risk of QT interval prolongation) (maximum dose of 20 mg/day);
Concurrent use of CYP2C19 inhibitors (↑ risk of QT interval prolongation) (maximum dose of 20 mg/day);
Angle-closure glaucoma;
OB: Use during pregnancy only if potential maternal benefit justifies potential fetal risk;
Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant;
Pedi: May risk of suicide attempt/ideation especially during early treatment or dose adjustment in children/adolescents; safety and effectiveness not established in children;
Geri: Appears on Beers list. May worsen or cause syndrome of inappropriate antidiuretic hormone (SIADH) secretion and/or hyponatremia in older adults. Use with caution in older adults and closely monitor sodium concentrations when starting therapy or dose. Maximum dose of 20 mg/day in patients >60 yr.

Adv. Reactions/Side Effects ⬆ ⬇

CV: QT interval prolongation, postural hypotension, tachycardia, TORSADES DE POINTES

Derm: sweating, photosensitivity, pruritus, rash

EENT: abnormal accommodation

Endo: SIADH

F and E: hyponatremia

GI: ↑salivation, abdominal pain, anorexia, diarrhea, dry mouth, dyspepsia, flatulence, nausea, altered taste, vomiting

GU: ↓libido, amenorrhea, delayed/absent orgasm, dysmenorrhea, ejaculatory delay/failure, erectile dysfunction, polyuria

Hemat: BLEEDING

Metab: ↑appetite, weight gain, weight loss

MS: arthralgia, myalgia

Neuro: apathy, confusion, drowsiness, insomnia, tremor, weakness, ↓libido, ↑depression, agitation, amnesia, anxiety, dizziness, fatigue, impaired concentration, migraine headache, NEUROLEPTIC MALIGNANT SYNDROME, paresthesia, SUICIDAL THOUGHTS

Resp: cough

Misc: fever, SEROTONIN SYNDROME, yawning

Interactions ⬆ ⬇

Drug-drug:

May cause serious, potentially fatal reactions when used with MAO inhibitors; concurrent use contraindicated; allow at least 14 days between citalopram and MAO inhibitors.
Concurrent use with MAO-inhibitor like drugs, such as linezolid or methylene blue, may ↑ risk of serotonin syndrome; concurrent use contraindicated; do not start therapy in patients receiving linezolid or methylene blue; if linezolid or methylene blue need to be started in a patient receiving citalopram, immediately discontinue citalopram and monitor for signs/symptoms of serotonin syndrome for 2 wk or until 24 hr after last dose of linezolid or methylene blue, whichever comes first (may resume citalopram therapy 24 hr after last dose of linezolid or methylene blue).
Concurrent use with pimozide may result in prolongation of the QT interval and is contraindicated.
QT interval prolonging drugs may ↑ the risk of QT interval prolongation and torsades de pointes (concurrent use should be avoided).
CYP2C19 inhibitors, including cimetidine, may ↑ levels and the risk of toxicity (maximum dose = 20 mg/day).
Drugs that affect serotonergic neurotransmitter systems, including tricyclic antidepressants, SNRIs, fentanyl, lithium, buspirone, tramadol, meperidine, methadone, amphetamines, and triptans, ↑ risk of serotonin syndrome.
Use cautiously with other centrally acting drugs, including alcohol, antihistamines, opioid analgesics, and sedative/hypnotics; concurrent use with alcohol is not recommended.
Serotonergic effects may be ↑ by lithium; concurrent use should be carefully monitored.
Ketoconazole, itraconazole, erythromycin, and omeprazole may ↑ levels.
Carbamazepine may ↓ blood levels.
May ↑ levels of metoprolol.
Use cautiously with tricyclic antidepressants due to unpredictable effects on serotonin and norepinephrine reuptake.
↑risk of bleeding with NSAIDs, aspirin, clopidogrel, prasugrel, ticagrelor, dabigatran, apixaban, edoxaban, rivaroxaban, or warfarin.

Drug-Natural Products:

↑risk of serotonergic side effects, including serotonin syndrome, with St. John’s wort and SAMe.

Route/Dosage ⬆ ⬇

PO (Adults ): 20 mg once daily initially, may be ↑ in 1 wk to 40 mg/day (maximum dose); CYP2C19 poor metabolizers or concurrent use of CYP2C19 inhibitor: Not to exceed 20 mg/day.
PO Geriatric Patients ): 20 mg once daily initially (not to exceed 20 mg/day in patients >60 yr).

Hepatic Impairment

PO (Adults ): 20 mg once daily (not to exceed 20 mg/day).

Availability ⬆ ⬇

(Generic available)

Capsules: 30 mg
Tablets: 10 mg; 20 mg; 30 mg; 40 mg
Oral solution peppermint flavor: 10 mg/5 mL

Assessment ⬆ ⬇

Screen patient for a personal or family history of bipolar disorder, mania, or hypomania before starting therapy; may precipitate a mixed/manic episode.
Monitor mood changes during therapy.
- Assess for suicidal tendencies, especially during early therapy and dose changes. Restrict amount of drug available to patient. Risk may be increased in children, adolescents, and adults ≤24 yr. After starting therapy, children, adolescents, and young adults should be seen by health care professional at least weekly for 4 wk, every 3 wk for the next 4 wk, and on advice of health care professional thereafter.
Assess sexual function before starting citalopram. Assess for changes in sexual function during treatment, including timing of onset; patient may not report.
Assess for serotonin syndrome (mental changes [agitation, hallucinations, coma], autonomic instability [tachycardia, labile BP, hyperthermia], neuromuscular aberrations [hyperreflexia, incoordination], and/or GI symptoms [nausea, vomiting, diarrhea]), especially in patients taking other serotonergic drugs (SSRIs, SNRIs, triptans).

Lab Test Considerations:

Monitor electrolytes (potassium and magnesium) in patients at risk for electrolyte imbalances prior to and periodically during therapy.

Implementation ⬆ ⬇

Do not confuse with Celexa with Celebrex, Cerebyx, or Zyprexa. Do not confuse citalopram with escitalopram.
PO: Administer as a single dose in the morning or evening without regard to food.

Patient/Family Teaching ⬆ ⬇

Instruct patient to take citalopram as directed. Take missed doses as soon as remembered unless almost time for next dose; do not double doses. Do not stop abruptly; may cause anxiety, irritability, high or low mood, feeling restless or changes in sleep habits, headache, sweating, nausea, dizziness, electric shock-like sensations, shaking, and confusion. Advise patient to read the Medication Guide prior to starting therapy and with each refill in case of changes.
May cause drowsiness, dizziness, impaired concentration, and blurred vision. Caution patient to avoid driving and other activities requiring alertness until response to the drug is known.
Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking any other Rx, OTC, or herbal products, especially alcohol or other CNS depressants, including opioids, and St. John's wort.
Caution patient to change positions slowly to minimize dizziness.
Advise patient, family, and caregivers to look for suicidality, especially during early therapy or dose changes. Notify health care professional immediately if thoughts about suicide or dying, attempts to commit suicide, new or worse depression or anxiety, agitation or restlessness, panic attacks, insomnia, new or worse irritability, aggressiveness, acting on dangerous impulses, mania, or other changes in mood or behavior or if symptoms of serotonin syndrome occur.
Advise patient to use sunscreen and wear protective clothing to prevent photosensitivity reactions.
Inform patient that frequent mouth rinses, good oral hygiene, and sugarless gum or candy may minimize dry mouth. If dry mouth persists for more than 2 wk, consult health care professional regarding use of saliva substitute.
Inform patient that citalopram may cause symptoms of sexual dysfunction. In males, ejaculatory delay or failure, decreased libido, and erectile dysfunction may occur. In female patients, may result in decreased libido and delayed or absent orgasm. Advise patient to notify health care professional if symptoms occur.
Rep: Instruct females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding. If used during pregnancy, should be tapered during 3rd trimester to avoid neonatal serotonin syndrome and increased risk of maternal postpartum hemorrhage. Monitor infants exposed to citalopram for excess sedation, restlessness, agitation, poor feeding, poor weight gain, respiratory distress; may risk of persistent pulmonary hypertension of the newborn. Inform patient of pregnancy exposure registry that monitors pregnancy outcomes in women exposed to antidepressants during pregnancy. Encourage pregnant patients to enroll in pregnancy exposure registry that monitors outcomes of women exposed to antidepressants during pregnancy by contacting National Pregnancy Registry for Antidepressants at 1-866-961-2388 or visiting online at https://womensmentalhealth.org/research/pregnancyregistry/antidepressants/.
Emphasize the importance of follow-up exams to monitor progress.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇