865
Severe acute cardiomyopathy associated with venlafaxine
overdose and possible role of CYP2D6 and CYP2C19
polymorphisms
MARCO VINETTI
1
, VINCENT HAUFROID
2
, ARNAUD CAPRON
2
, JEAN-FRANÇOIS CLASSEN
2
,
SEBASTIEN MARCHANDISE
3
, and PHILIPPE HANTSON
1
1
Cliniques St-Luc, Université catholique de Louvain, Intensive Care, Avenue Hippocrate 10, Brussels, 1200 Belgium
2
Université catholique de Louvain, Louvain Centre for Toxicology and Applied Pharmacology, Avenue Hippocrate 10, Brussels, 1200 Belgium
3
Cliniques St-Luc, Cardiology, Avenue Hippocrate 10, Brussels, 1200 Belgium
Introduction. Venlafaxine (VEN) is a serotonin-norepinephrine-dopamine reuptake inhibitor that causes usually a mild cardiotoxicity
when ingested in overdose. We report a patient who developed acute heart failure following overdose. As the toxicokinetic data suggested
a prolonged metabolism, genetic polymorphisms for cytochrome P450 isoenzymes CYP2D6 and CYP2C19 were also investigated.
Case report. A 34-year-old woman was admitted to the hospital 10 hours after the ingestion of an 11.25 g overdose of VEN. She was
comatose and suffered two self-limited seizures. The electrocardiogram showed diffuse ST segment depression, but normal QRS and
QTc duration. The plasma levels on admission were 18 015 and 3 846 ng/ml for VEN and the metabolite O-desmethylvenlafaxine (ODV),
respectively. The patient developed severe cardiodepression. The left ventricular shortening fraction was only 9% on echocardiography.
The patient was oliguric and required continuous venovenous hemofiltration. The administration of milrinone was required for 12 days,
and norepinephrine for 10 days. Left ventricular function recovered. The calculated elimination half-life was 30.8 and 72.2 hours for VEN
and ODV, respectively. The patient genotype was CYP2D6*1/*5, the *5 allele corresponding to a complete deletion of CYP2D6 gene.
Conclusions. Severe and sustained cardiotoxicity following VEN overdose may be related to the amount ingested, as well as to the genetic
polymorphism for CYP2D6 leading to a delayed elimination of active metabolite.
Keywords Heart; Cardiac support; CNS/ Psychological
Introduction
Venlafaxine(VEN) is a serotonin-norepinephrine-dopamine
reuptake inhibitor (SNRI) that rarely causes life-threatening
cardiac manifestations following overdose. We report here a
case of severe and sustained cardiotoxicity after an overdose
of 11.25 g in a 34-year-old patient without previous cardiac
disease. VEN is extensively metabolized by the liver mainly
through the cytochrome P450-2D6 and -2C19 isoenzymes
(CYP2D6 and CYP2C19) to form its major pharmacologi-
cally active metabolite, O-desmethylvenlafaxine (ODV); a
minor metabolite, N-desmethylvenlafaxine, is also formed
by CYP3A4 and possibly CYP2C19. We investigated
in this case the possible role of CYP2D6 and CYP2C19
genetic polymorphism in VEN/ODV toxicokinetics and
toxicodynamics.
Case report
A 34-year-old depressive woman (65 kg weight) was admit-
ted to the Emergency Department (ED) 10 hours after a drug
overdose. According to the relatives, she could have ingested
a maximal dose of 20 g of acetaminophen, 7.5 g of extended-
release VEN and 3.75 g of immediate-release VEN. She had
been found unresponsive by the first medical rescuers, with
a Glasgow Coma Score (GCS) of 8/15. As cough and gag
reflexes were preserved, intubation was not performed at the
scene. Vital signs on admission in the ED were as follows:
arterial blood pressure 116/53 mmHg, heart rate 130/minute,
temperature 37.3°C. Her GCS was still 8/15, and the pupils
were dilated bilaterally. She suffered two self-limited gener-
alized seizures soon after admission and orotracheal intuba-
tion was subsequently performed. The brain computerized
tomography was normal. The admission 12-lead ECG
performed after seizures episode (Fig. 1) showed a sinus
rhythm 107/min, QRS duration 80 msec, QTc 403 msec,
and ST segment depression in the anterior-and inferior-
leads consistent with subendocardial ischemia. The com-
prehensive blood toxicological screen (ultra-performance
liquid chromatography method with diode array detection)
Clinical Toxicology (2011), 49, 865–869
Copyright © 2011 Informa Healthcare USA, Inc.
ISSN: 1556-3650 print / 1556-9519 online
DOI: 10.3109/15563650.2011.626421
BRIEF COMMUNICATION
Received 27 April 2011; accepted 16 September 2011.
Address correspondence to Prof. Marco Vinetti, Cliniques St Luc,
Intensive Care, Avenue Hippocrate 10, Brussels, 1200 Belgium.
E-mail: philippe.hantson@uclouvain.be