escitalopram (Rx)

>10%

Headache (24%)

Nausea (18%)

Ejaculation disorder (9-14%)

Somnolence (4-13%)

Insomnia (7-12%)

1-10%

Xerostomia (4-9%)

Constipation (3-6%)

Fatigue (2-8%)

Libido decrease (3-7%)

Anorgasmia (2-6%)

Flatulence (2%)

Toothache (2%)

Weight gain (1%)

Menstrual disorder (2%)

Neck/shoulder pain (3%)

Rhinitis (5%)

Flu-like syndrome (5%)

Ejaculation disorder (9-14%)

<1%

Arthralgia

Abdominal pain

Abnormal bleeding

Abnormal dreams

Allergy

Blurred vision

Bronchitis

Chest pain

Constipation

Decreased appetite

Decreased concentration

Disrupts platelets/hemostasis

Dizziness

Dyspepsia

Fever

Heartburn

Hot flashes

Impotence

Irritability

Jaw stiffness

Lethargy

Lightheadedness

Menstrual disorder

Hypertension

Palpitations

Migraine

Myalgia

Paresthesia

Rash

Sweating

Tinnitus

Tremor

Urinary frequency

Urinary tract infection

Vertigo

Vomiting

Yawning

Contraindications

Hypersensitivity

Coadministration with serotonergic drugs

• Concomitant use or within 14 days of MAOIs increases risk of serotonin syndrome
• Symptoms include tremor, myoclonus, diaphoresis, nausea, vomiting, flushing, dizziness, hyperthermia with features resembling neuroleptic malignant syndrome, seizures, rigidity, autonomic instability with possible rapid fluctuations of vital signs, and mental status changes that include extreme agitation progressing to delirium and coma
• Starting escitalopram in a patient who is being treated with linezolid or IV methylene blue is contraindicated because of an increased risk of serotonin syndrome
• If linezolid or IV methylene blue must be administered, discontinue SSRI immediately and monitor for CNS toxicity; may resume 24 hr after last linezolid or methylene blue dose, or after 2 weeks of monitoring (5 weeks for fluoxetine), whichever comes first

Cautions

Conflicting evidence regarding use of SSRIs during pregnancy and increased risk of persistent pulmonary hypertension of the newborn, or PPHN (see Pregnancy)

In neonates exposed to SNRIs/SSRIs late in third trimester: risk of complications such as feeding difficulties, irritability, and respiratory problems

Caution with seizure disorder, bipolar mania, severe renal impairment; not FDA approved for the treatment of bipolar depression

NRIs/SSRIs have been associated with the development of SIADH; hyponatremia has been reported rarely

May worsen psychosis in some patients and precipitate a shift to mania or mypomania in patients with bipolar disorder

Risk of hyponatremia

Risk of mydriasis; may trigger angle closure attack in patients with angle closure glaucoma with anatomically narrow angles without a patent iridectomy

Bone fractures are associated with antidepressant therapy; consider the possibility of a fracture in patients with unexplained bone pain, swelling, or bruising

Prescriptions should be written for smallest quantity consistent with good patient care and the family or care giver alerted to monitor patient for emergence of suicidality and associated behaviors (anxiety, agitation, panic attacks, insomnia, hostility, akathisia, impulsivity, irritabilty)

SSRIs/SNRIs increase risk of abnormal bleeding (further increased if concomitant aspirin, NSAIDs or anticoagulants, or hemorrhagic diathesis)

Prolongation of QT interval and ventricular arrhythmias reported, especially in female patients with preexisting QT prolongation or other risk factors

Risk of cognitive and motor function impairment; use caution when operating heavy machinery

Use with caution in patients with history of seizure disorders or or conditions predisposing to seizures including brain damage and alcoholism

May impair platelet aggregation that can result in increased risk of bleeding events including GI bleeding especially if taken concomitantly with aspiring, warfarin, or NSAIDs

Risk of serotonin syndrome or neuroleptic malignant syndrome (NMS)-like reactions have been reported with SSRIs and SNRIs, including desvenlafaxine, both when taken alone, but especially when co-administered with other serotonergic agents (including triptans, tricyclic antidepressants, fentanyl, lithium, tramadol, tryptophan, buspirone, amphetamines, and St. John’s Wort); if symptoms occur, discontinue therapy and initiate supportive treatment; if concomitant use of desvenlafaxine with other serotonergic drugs is clinically warranted, patients should be made aware of increased risk for serotonin syndrome, particularly during treatment initiation and dose increases

No additional benefits at 20 mg/day

May cause or exacerbate sexual dysfunction

Gradually taper dose before discontinuation; abrupt discontinuation may cause dysphoric mood, dizziness, sensory disturbances, agitation, confusion, anxiety, headache, insomnia, tinnitus, seizures, irritability

Pregnancy

Pregnancy category: C

Use late in the third trimester associated with complications in newborns and may require prolonged hospitalization, respiratory support, and tube feeding

Persistent pulmonary hypertension of the newborn

• Potential risk of persistent pulmonary hypertension of the newborn when used during pregnancy
• Initial Public Health Advisory in 2006 was based on a single published study; since then, there have been conflicting findings from new studies, making it unclear whether use of SSRIs during pregnancy can cause PPHN
• FDA has reviewed the additional new study results and has concluded that, given the conflicting results from different studies, it is premature to reach any conclusion about a possible link between SSRI use in pregnancy and PPHN
• FDA recommendation: FDA advises health-care professionals not to alter their current clinical practice of treating depression during pregnancy and to report any adverse events to the FDA MedWatch program
• A meta-analysis of 7 observational studies, found exposure to SSRIs in late pregnancy (ie, >20 weeks' gestation) more than doubled the risk of PPHN that could not be explained by other etiologies (eg, congenital malformations, meconium aspiration) (BMJ 2014;348:f6932)

Lactation

Excreted in breast milk; consider risk/benefit ratio

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

S-enantiomer of racemic citalopram; inhibits the reuptake of serotonin, with little or no effect on norepinephrine or dopamine reuptake

Absorption

Bioavailability: 80%

Peak plasma time: 3.5-6.5 hr

Distribution

Protein bound: 56%

Vd: 20 L/kg

Metabolism

CYP3A4, CYP2C19

Metabolites: Insignificant potency

Enzymes inhibited: CYP2D6

Elimination

Half-life: 27-32 hr

Dialyzable: No

Renal clearance: 42 mL/min

Total body clearance: 600 mL/min

Excretion: Urine (8%)