citalopram, CeleXA

 Indications

Depression. Unlabeled Use: Premenstrual dysphoric

disorder (PMDD). Obsessive-compulsive disorder

(OCD). Panic disorder. Generalized anxiety disorder

(GAD). Post-traumatic stress disorder (PTSD).

Social anxiety disorder (social phobia).

Action

Selectively inhibits the reuptake of serotonin in the CNS.

Therapeutic Effects: Antidepressant action.

Pharmacokinetics

Absorption: 80% absorbed after oral administration.

Distribution: Enters breast milk.

Metabolism and Excretion: Mostly metabolized

by the liver (10% by CYP3A4 and 2C19 enzymes);

excreted unchanged in urine.

Half-life: 35 hr.

TIME/ACTION PROFILE (antidepressant effect)

ROUTE ONSET PEAK DURATION

PO 1–4 wk unknown unknown

Contraindications/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 (qrisk of QT interval prolongation);

Concurrent use of QT interval prolonging drugs.

Use Cautiously in: History of mania; History of suicide

attempt/ideation (qrisk 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 metabolizers

of CYP2C19 (qrisk of QT interval prolongation) (maximum

dose of 20 mg/day); Concurrent use of CYP2C19

inhibitors (qrisk of QT interval prolongation) (maximum

dose of 20 mg/day); Angle-closure glaucoma; OB:

Use during third trimester may result in neonatal serotonin

syndrome requiring prolonged hospitalization,

respiratory and nutritional support; Lactation: Present

in breast milk and may result in lethargy withpfeeding

in infants; weigh risk/benefits; Pedi: Mayqrisk of suicide

attempt/ideation especially during early treatment

or dose adjustment in children/adolescents (unlabeled

for pediatric use); Geri:pdoses recommended (maximum

dose of 20 mg/day in patients 60 yr).

Adverse Reactions/Side Effects

CNS: NEUROLEPTIC MALIGNANT SYNDROME, SUICIDAL

THOUGHTS, apathy, confusion, drowsiness, insomnia,

weakness, agitation, amnesia, anxiety,plibido, dizziness,

fatigue, impaired concentration,qdepression,

migraine headache. EENT: abnormal accommodation.

Resp: cough. CV: TORSADE DE POINTES, postural

hypotension, QT interval prolongation, tachycardia. GI:

abdominal pain, anorexia, diarrhea, dry mouth, dyspepsia,

flatulence,qsaliva, nausea, altered taste,qappetite,

vomiting. GU: amenorrhea, dysmenorrhea,

ejaculatory delay, erectile dysfunction, polyuria.

Derm: sweating, photosensitivity, pruritus, rash. Metab:

weight loss, weight gain. F and E: hyponatremia.

MS: arthralgia, myalgia. Neuro: tremor, paresthesia.

Misc: SEROTONIN SYNDROME, fever, 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, mayqrisk 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 QTc interval

and is contraindicated. QT interval prolonging

drugs mayqthe risk of QT interval prolongation and

torsade de pointes (concurrent use should be

avoided). CYP2C19 inhibitors, including cimetidine

mayqlevels and the risk of toxicity (maximum dose

20 mg/day). Drugs that affect serotonergic neurotransmitter

systems, including tricyclic antidepressants,

SNRIs, fentanyl, buspirone, tramadol, amphetamines,

and triptansqrisk 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

beqby lithium (concurrent use should be carefully

monitored). Ketoconazole, itraconazole, erythromycin,

and omeprazole mayqlevels. Carbamazepine

maypblood levels. Mayqlevels of metoprolol.

Use cautiously with tricyclic antidepressants due to

unpredictable effects on serotonin and norepinephrine

reuptake.qrisk of bleeding with aspirin, NSAIDs,

clopidogrel, or warfarin.

Drug-Natural Products:qrisk of serotonergic

side effects including serotonin syndrome with St.

John’s wort and SAMe.

Route/Dosage

PO (Adults): 20 mg once daily initially, may beqin 1

wk to 40 mg/day (maximum dose); Poor metabolizer

of CYP2C19 or concurrent use of CYP2C19 inhibitor—

Do not exceed dose of 20 mg/day.

PO (Geriatric Patients): 20 mg once daily initially

(do not exceed dose of 20 mg/day in patients 60 yr).

Hepatic Impairment

PO (Adults): 20 mg once daily (do not exceed dose of

20 mg/day).

Availability (generic available)

Tablets: 10 mg, 20 mg, 40 mg. Cost: Generic—10

mg $7.11/100, 20 mg $9.73/100, 40 mg $10.83/100.

Oral solution (peppermint flavor): 10 mg/5 mL.

Cost: Generic—10 mg/5 mL $117.50/240 mL.