Citalopram

Aka: Citalopram, Celexa, Escitalopram, Lexapro, Citalopram Overdose

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II. Indications

  1. Major Depression
  2. Generalized Anxiety Disorder
  3. Social Anxiety Disorder

III. Mechanism

  1. Selective Serotonin Reuptake Inhibitor (SSRI)
  2. Minimal effects on other Neurotransmitters

IV. Pharmacokinetics

  1. Citalopram
    1. Half-Life: 20 to 35 hours
    2. Bioavailability: 80%
    3. Peak drug levels: 4 hours
  2. Escitalopram
    1. Half-Life: 27-33 hours
    2. Bioavailability: 80%
    3. Peak drug levels: 5 hours

V. Safety

  1. Pregnancy Category C
  2. Considered safe in Lactation with caution
    1. Both Citalopram and Escitalopram have acceptably low levels in Breast Milk
    2. Citalopram and Escitalopram are ACOG L3 (moderately safe in Lactation)

VI. Preparations

  1. Citalopram (Celexa)
    1. Tablets: 10, 20 (scored), 40 (scored)
    2. Oral Solution: 10 mg/5 ml
  2. Escitalopram (Lexapro)
    1. Active isomer of racemic Citalopram
    2. Tablets: 5, 10 (scored), 20 mg (scored)

VII. Dosing

  1. Citalopram (Celexa)
    1. Starting dose: 20 mg orally daily
    2. Most effective dose: 40 mg orally daily
    3. Maximum Dose: 40 mg
      1. Maximum dose 20 mg in hepatic Impairment or concurrent use of Cytochrome P450 2C19 Inhibitors (see below)
  2. Escitalopram (Lexapro)
    1. Starting Dose: 10 mg daily (equivalent to 40 mg Celexa)
    2. Higher dose at 20 mg is not more effective than 10 mg
      1. Maximum dose 10 mg in hepatic Impairment or use of Cytochrome P450 2C19 Inhibitors (see below)

VIII. Adverse Effects: General

  1. No increased weight gain
  2. Midway on spectrum between Anxiolytic and anxiogenic
    1. Similar to Zoloft on this spectrum
    2. Well tolerated
  3. Nausea
    1. May occur initially but is transient
    2. Consider decreasing dose to 10 mg initially
  4. Less Sexual Dysfunction than Prozac, Zoloft, Paxil
    1. Sexual Dysfunction in 10-15% of cases
    2. Similar to Luvox and Effexor in terms of this effect
    3. See Antidepressant Induced Sexual Dysfunction
  5. Arrhythmia risk
    1. Prolonged QTc Interval and Torsades de Pointes risk
    2. Avoid in Prolonged QTc (e.g. congenital Prolonged QTc) or combined with other causes of Drug-Induced QTc Prolongation
    3. Monitor and correct for Electrolyte abnormalities (e.g. Hypokalemia, Hypomagnesemia) if risks

IX. Adverse Effects: Overdose

  1. See SSRI Overdose
  2. P450 Metabolism to di-desmethylcitalopram
    1. Di-desmethylcitalopram is cardiotoxic (inhibits cardiac Potassium and Calcium channels)
  3. Overdose presentation (esp. ingestions >600 mg)
    1. Sedation
    2. Seizures
    3. Tachycardia
    4. QTc Prolongation
    5. Torsades de Pointes
    6. Metabolic Acidosis
    7. Hypokalemia
  4. Evaluation and Management
    1. See SSRI Overdose
    2. See Serotonin Syndrome
    3. See Unknown Ingestion
    4. Correct Electrolyte abnormalities (e.g. Hypokalemia, Hypomagnesemia)
  5. Monitoring
    1. Asymptomatic
      1. Monitor up to 12 hours if suspected ingestion >400 mg
    2. Symptomatic or QTc Prolongation
      1. Monitor until resolution of symptoms and QTc normalization
  6. References
    1. Tomszewski (2021) Crit Dec Emerg Med 35(12): 32

X. Drug Interactions

  1. Avoid with MAO Inhibitors or Tryptophan
  2. Cytochrome P450 2C19 Inhibitors (or poor 2C19 metabolizers)
    1. Arrhythmia risk
      1. Prolonged QTc Interval and Torsades de Pointes risk
      2. Avoid combining with other medication causes of Drug-Induced QTc Prolongation
    2. Most significant agents
      1. Proton Pump Inhibitors: Omeprazole, Esomeprazole, Cimetidine
      2. Ethinyl Estradiol (Oral Contraceptives)
    3. Agents that do not appear to have significant interactions
      1. Proton Pump Inhibitors: Pantoprazole, Lansoprazole, Dexlansoprazole
    4. Precautions
      1. Limit Citalopram to 20 mg daily in those on Omeprazole, Esomeprazole, Oral Contraceptives
      2. Consider Escitalopram (Lexapro) instead which appears safe to at least 20 mg daily with these agents
    5. Resources
      1. FDA Drug Safety Notice
        1. http://www.fda.gov/Drugs/DrugSafety/ucm269086.htm

XI. Resources

  1. Citalopram (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=9f5a14c2-b460-402e-acb4-04402278e64b
  2. Escitalopram (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=3019a647-9bcf-48cf-928c-0467f9b921a8

XII. References

  1. (2023) Med Lett Drugs Ther 62(1592): 25-32
  2. Olson (2020) Clinical Pharmacology, Medmaster Miami, p. 38-9
  3. Hamilton (2020) Tarascon Pocket Pharmacopoeia

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Related Studies

Cost: Medications

citalopram (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
CITALOPRAM HBR 10 MG TABLET Generic $0.03 each
CITALOPRAM HBR 10 MG/5 ML SOLN Generic $0.24 per ml
CITALOPRAM HBR 20 MG TABLET Generic $0.03 each
CITALOPRAM HBR 30 MG CAPSULE Generic $4.68 each
CITALOPRAM HBR 40 MG TABLET Generic $0.04 each
escitalopram (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
ESCITALOPRAM 10 MG TABLET Generic $0.05 each
ESCITALOPRAM 20 MG TABLET Generic $0.08 each
ESCITALOPRAM 5 MG TABLET Generic $0.04 each
ESCITALOPRAM OXALATE 5 MG/5 ML Generic $0.20 per ml
lexapro (on 1/14/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
LEXAPRO 10 MG TABLET Generic $0.05 each
LEXAPRO 20 MG TABLET Generic $0.08 each
LEXAPRO 5 MG TABLET Generic $0.04 each
FPNotebook does not benefit financially from showing this medication data or their pharmacy links. This information is provided only to help medical providers and their patients see relative costs. Insurance plans negotiate lower medication prices with suppliers. Prices shown here are out of pocket, non-negotiated rates. See Needy Meds for financial assistance information. GoodRx is another tool for finding lower drug prices.

Ontology: Citalopram (C0008845)

Definition (CHV) a kind of antidepressant drug
Definition (CHV) a kind of antidepressant drug
Definition (NCI) A bicyclic phthalene derivative and selective serotonin reuptake inhibitor (SSRI), with antidepressant and anxiolytic activities. Citalopram selectively inhibits the neuronal reuptake of the neurotransmitter serotonin (5-HT) in presynaptic cells in the central nervous system, thereby increasing levels of 5-HT within the synaptic cleft and enhancing the actions of serotonin on its receptors. Increased serotonergic neurotransmission results in antidepressive and anxiolytic effects.
Definition (MSH) A furancarbonitrile that is one of the SEROTONIN UPTAKE INHIBITORS used as an antidepressant. The drug is also effective in reducing ethanol uptake in alcoholics and is used in depressed patients who also suffer from tardive dyskinesia in preference to tricyclic antidepressants, which aggravate this condition.
Definition (CSP) selective neuronal serotonin reuptake inhibitor and a clinically effective antidepressant with tolerable side effects; effective in reducing ethanol uptake in alcoholics.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D015283
SnomedCT 321986007, 372596005
LNC LP20806-3, MTHU012380
English Citalopram, Cytalopram, 5-Isobenzofurancarbonitrile, 1-(3-(dimethylamino)propyl)-1-(4-fluorophenyl)-1,3-dihydro-, CITALOPRAM, Citalopram [Chemical/Ingredient], cytalopram, Nitalapram, 1,3-Dihydro-1-(3-(dimethylamino)propyl)-1-(4-fluorophenyl)-5-isobenzofurancarbonitrile, citalopram, Citalopram (product), Citalopram (substance)
Swedish Citalopram
Czech citalopram
Finnish Sitalopraami
Russian TSITALOPRAM, ЦИТАЛОПРАМ
Japanese シタロプラム
Polish Citalopram
Spanish citalopram (producto), citalopram (sustancia), citalopram, Citalopram
French Citalopram
German Citalopram
Italian Citalopram
Portuguese Citalopram
Derived from the NIH UMLS (Unified Medical Language System)

Ontology: Celexa (C0719199)

Definition (CHV) depression treatment drug
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
English Celexa, citalopram hydrobromide (Celexa), CeleXA
Derived from the NIH UMLS (Unified Medical Language System)

Ontology: Escitalopram (C1099456)

Definition (NCI_NCI-GLOSS) A drug used to treat depression and certain anxiety disorders. It belongs to the family of drugs called selective serotonin reuptake inhibitors (SSRIs).
Definition (NCI) The active S-stereoisomer of the selective serotonin reuptake inhibitor (SSRI) citalopram with antidepressant, anti-obsessive-compulsive and antibulimic properties. Escitalopram inhibits the reuptake of the neurotransmitter serotonin (5-HT) at the serotonin reuptake pump of the neuronal membrane of the presynaptic cell, thereby increasing levels of 5-HT within the synaptic cleft and enhancing the actions of serotonin on 5HT1A autoreceptors. Unlike other SSRIs, escitalopram appears to not only bind to a primary high-affinity site on the serotonin transporter protein but also to a secondary lower-affinity allosteric site that is considered to stabilize and prolong drug binding.
Definition (MSH) S-enantiomer of citalopram.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D015283
SnomedCT 395246009, 400447003
LNC LP31801-1, MTHU016070
French Escitalopram
English S(+)-Citalopram, (S)-Citalopram, ESCITALOPRAM, escitalopram, Escitalopram (product), Escitalopram (substance), Escitalopram
Japanese エスシタロプラム
Czech escitalopram
Spanish escitalopram (producto), escitalopram (sustancia), escitalopram
Derived from the NIH UMLS (Unified Medical Language System)

Ontology: Lexapro (C1170371)

Definition (CHV) a drug used to treat depression and anxiety
Definition (MSH) Trade name of escitalopram, the active S-enantiomer of the racemic citalopram.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D015283
English Lexapro
Czech Lexapro
Derived from the NIH UMLS (Unified Medical Language System)

Related Topics in Pharmacology

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