Chemical formula: C₂₀H₂₁FN₂O Molecular mass: 324.392 g/mol PubChem compound: 146570
Escitalopram interacts in the following cases:
Concomitant use of SSRIs and herbal remedies containing St. John’s wort (Hypericum perforatum) may result in an increased incidence of adverse reactions.
The metabolism of escitalopram is mainly mediated by CYP2C19. CYP3A4 and CYP2D6 may also contribute to the metabolism although to a smaller extent. The metabolism of the major metabolite S-DCT (demethylated escitalopram) seems to be partly catalysed by CYP2D6.
Co-administration of escitalopram with omeprazole 30 mg once daily (a CYP2C19 inhibitor) resulted in moderate (approximately 50%) increase in the plasma concentrations of escitalopram.
Co-administration of escitalopram with cimetidine 400 mg twice daily (moderately potent general enzyme-inhibitor) resulted in a moderate (approximately 70%) increase in the plasma concentrations of escitalopram. Caution is advised when administering escitalopram in combination with cimetidine. Dose adjustment may be warranted.
Thus, caution should be exercised when used concomitantly with CYP2C19 inhibitors (e.g. omeprazole, esomeprazole, fluvoxamine, lansoprazole, ticlopidine) or cimetidine. A reduction in the dose of escitalopram may be necessary based on monitoring of side-effects during concomitant treatment.
In vitro studies have demonstrated that escitalopram may also cause weak inhibition of CYP2C19. Caution is recommended with concomitant use of medicinal products that are metabolised by CYP2C19.
Escitalopram is an inhibitor of the enzyme CYP2D6. Caution is recommended when escitalopram is co-administered with medicinal products that are mainly metabolised by this enzyme, and that have a narrow therapeutic index, e.g. flecainide, propafenone and metoprolol (when used in cardiac failure), or some CNS acting medicinal products that are mainly metabolised by CYP2D6, e.g. antidepressants such as desipramine, clomipramine and nortriptyline or antipsychotics like risperidone, thioridazine and haloperidol. Dosage adjustment may be warranted.
Co-administration with desipramine or metoprolol resulted in both cases in a twofold increase in the plasma levels of these two CYP2D6 substrates.
An initial dose of 5 mg daily for the first two weeks of treatment is recommended in patients with mild or moderate hepatic impairment. Depending on individual patient response, the dose may be increased to 10 mg daily. Caution and extra careful dose titration is advised in patients with severely reduced hepatic function.
No pharmacodynamic or pharmacokinetic interactions are expected between escitalopram and alcohol. However, as with other psychotropic medicinal products, the combination with alcohol is not advisable.
Caution is advised in patients with severely reduced renal function (CLCR less than 30 ml/min).
There have been reports of cutaneous bleeding abnormalities, such as ecchymoses and purpura, with SSRIs. Caution is advised in patients taking SSRIs, particularly in concomitant use with oral anticoagulants, with medicinal products known to affect platelet function (e.g. atypical antipsychotics and phenothiazines, most tricyclic antidepressants, acetylsalicylic acid and non-steroidal anti-inflammatory medicinal products (NSAIDs), ticlopidine and dipyridamole) and in patients with known bleeding tendencies.
Concomitant use of non-steriodal anti-inflammatory drugs (NSAIDs) may increase bleeding-tendency.
Animal data have shown that citalopram may affect sperm quality. Human case reports with some SSRIs have shown that an effect on sperm quality is reversible. Impact on human fertility has not been observed so far.
There have been reports of enhanced effects when SSRIs have been given together with lithium or tryptophan, therefore concomitant use of SSRIs with these medicinal products should be undertaken with caution.
Caution is advisable if escitalopram is used concomitantly with medicinal products with serotonergic effects such as sumatriptan or other triptans, tramadol and tryptophan.
In rare cases, serotonin syndrome has been reported in patients using SSRIs concomitantly with serotonergic medicinal products. A combination of symptoms, such as agitation, tremor, myoclonus and hyperthermia may indicate the development of this condition. If this occurs treatment with the SSRI and the serotonergic medicinal product should be discontinued immediately and symptomatic treatment initiated.
Patients with a history of suicide-related events, or those exhibiting a significant degree of suicidal ideation prior to commencement of treatment, are known to be at greater risk of suicidal thoughts or suicide attempts, and should receive careful monitoring during treatment.
SSRIs should be used with caution in patients with a history of mania/hypomania. SSRIs should be discontinued in any patient entering a manic phase.
Escitalopram should therefore be used with caution in patients with angle-closure glaucoma or history of glaucoma.
Due to limited clinical experience, caution is advised in patients with coronary heart disease.
In patients with diabetes, treatment with an SSRI may alter glycaemic control (hypoglycaemia or hyperglycaemia). Insulin and/or oral hypoglycaemic dosage may need to be adjusted.
SSRIs should be avoided in patients with unstable epilepsy, and patients with controlled epilepsy should be closely monitored.
For escitalopram only limited clinical data are available regarding exposed pregnancies.
Animal studies have shown reproductive toxicity. Escitalopram should not be used during pregnancy unless clearly necessary and only after careful consideration of the risk/benefit.
Neonates should be observed if maternal use of escitalopram continues into the later stages of pregnancy, particularly in the third trimester. Abrupt discontinuation should be avoided during pregnancy.
The following symptoms may occur in the neonate after maternal SSRI/SNRI use in later stages of pregnancy: respiratory distress, cyanosis, apnoea, seizures, temperature instability, feeding difficulty, vomiting, hypoglycaemia, hypertonia, hypotonia, hyperreflexia, tremor, jitteriness, irritability, lethargy, constant crying, somnolence and difficulty sleeping. These symptoms could be due to either serotonergic effects or discontinuation symptoms. In a majority of instances the complications begin immediately or soon (<24 hours) after delivery.
Epidemiological data have suggested that the use of SSRIs in pregnancy, particularly in late pregnancy, may increase the risk of persistent pulmonary hypertension in the newborn (PPHN). The observed risk was approximately 5 cases per 1000 pregnancies. In the general population 1 to 2 cases of PPHN per 1000 pregnancies occur.
It is expected that escitalopram will be excreted into human milk.
Consequently, breast-feeding is not recommended during treatment.
Animal data have shown that citalopram may affect sperm quality. Human case reports with some SSRIs have shown that an effect on sperm quality is reversible. Impact on human fertility has not been observed so far.
Although escitalopram has been shown not to affect intellectual function or psychomotor performance, any psychoactive medicinal product may impair judgement or skills. Patients should be cautioned about the potential risk of an influence on their ability to drive a car and operate machinery.
Adverse reactions are most frequent during the first or second week of treatment and usually decrease in intensity and frequency with continued treatment.
Adverse reactions known for SSRIs and also reported for escitalopram in either placebo-controlled clinical studies or as spontaneous post-marketing events are listed below by system organ class and frequency.
Frequencies are taken from clinical studies; they are not placebo-corrected. Frequencies are defined as: very common (≥1/10), common (≥1/100 to <1/10), uncommon (≥1/1,000 to <1/100), rare (≥1/10,000 to <1/1,000), very rare (<1/10,000), or not known (cannot be estimated from the available data).
Not known: Thrombocytopenia
Rare: Anaphylactic reaction
Not known: Inappropriate ADH secretion
Common: Decreased appetite, increased appetite, weight increased
Uncommon: Weight decreased
Not known: Hyponatraemia, anorexia1
Common: Anxiety, restlessness, abnormal dreams, libido decreased
Female: anorgasmia
Uncommon: Bruxism, agitation, nervousness, panic attack, confusional state
Rare: Aggression, depersonalisation, hallucination
Not known: Mania, suicidal ideation, suicidal behaviour2
Very common: Headache
Common: Insomnia, somnolence, dizziness, paraesthesia, tremor
Uncommon: Taste disturbance, sleep disorder, syncope
Rare: Serotonin syndrome
Not known: Dyskinesia, movement disorder, convulsion, psychomotor restlessness/akathisia1
Uncommon: Mydriasis, visual disturbance
Uncommon: Tinnitus
Uncommon: Tachycardia
Rare: Bradycardia
Not known: Electrocardiogram QT prolonged Ventricular arrhythmia including torsade de pointes
Not known: Orthostatic hypotension
Common: Sinusitis, yawning
Uncommon: Epistaxis
Very common: Nausea
Common: Diarrhoea, constipation, vomiting, dry mouth
Uncommon: Gastrointestinal haemorrhages (including rectal haemorrhage)
Not known: Hepatitis, liver function test abnormal
Common: Sweating increased
Uncommon: Urticaria, alopecia, rash, pruritus
Not known: Ecchymosis, angioedemas
Common: Arthralgia, myalgia
Not known: Urinary retention
Common: Male: ejaculation disorder, impotence
Uncommon: Female: metrorrhagia, menorrhagia
Not known: Galactorrhoea
Male: priapism
Common: Fatigue, pyrexia
Uncommon: Oedema
1 These events have been reported for the therapeutic class of SSRIs.
2 Cases of suicidal ideation and suicidal behaviours have been reported during escitalopram therapy or early after treatment discontinuation.
Cases of QT interval prolongation and ventricular arrhythmia including torsade de pointes have been reported during the post-marketing period, predominantly in patients of female gender, with hypokalaemia, or with pre-existing QT interval prolongation or other cardiac diseases.
Epidemiological studies, mainly conducted in patients 50 years of age and older, show an increased risk of bone fractures in patients receiving SSRIs and TCAs. The mechanism leading to this risk is unknown.
Discontinuation of SSRIs/SNRIs (particularly when abrupt) commonly leads to discontinuation symptoms. Dizziness, sensory disturbances (including paraesthesia and electric shock sensations), sleep disturbances (including insomnia and intense dreams), agitation or anxiety, nausea and/or vomiting, tremor, confusion, sweating, headache, diarrhoea, palpitations, emotional instability, irritability, and visual disturbances are the most commonly reported reactions. Generally these events are mild to moderate and are self-limiting, however, in some patients they may be severe and/or prolonged. It is therefore advised that when escitalopram treatment is no longer required, gradual discontinuation by dose tapering should be carried out.
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