QT time prolongation
Adverse drug events
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Explanations of the substances for patients
We have no additional warnings for the combination of abarelix and eperison. Please also consult the relevant specialist information.
The reported changes in exposure correspond to the changes in the plasma concentration-time curve [ AUC ]. We do not expect any change in exposure for abarelix, when combined with eperison (100%). We do not expect any change in exposure for eperison, when combined with abarelix (100%).
The pharmacokinetic parameters of the average population are used as the starting point for calculating the individual changes in exposure due to the interactions.
The bioavailability of abarelix is unknown. The terminal half-life [ t12 ] is rather long at 316.8 hours and constant plasma levels [ Css ] are only reached after more than 1267.2 hours. The protein binding [ Pb ] is 97.5% strong. The metabolism via cytochromes is currently still being worked on.
The bioavailability, half-life, and volume of distribution of eperison are unknown to us.
|Serotonergic Effects a||0||Ø||Ø|
Rating: According to our knowledge, neither abarelix nor eperison increase serotonergic activity.
|Kiesel & Durán b||0||Ø||Ø|
Rating: According to our knowledge, neither abarelix nor eperison increase anticholinergic activity.
QT time prolongation
Rating: In combination, abarelix and eperison can potentially trigger ventricular arrhythmias of the torsades de pointes type.
General adverse effects
|Side effects||∑ frequency||aba||epe|
|Abdominal pain||5.0 %||n.a.||5.0|
Stevens johnson syndrome: eperison
Toxic epidermal necrolysis: eperison
Based on your answers and scientific information, we assess the individual risk of undesirable side effects. These recommendations are intended to advise professionals and are not a substitute for consultation with a doctor. In the restricted test version (alpha), the risk of all substances has not yet been conclusively assessed.
Abstract: Eperisone hydrochloride (4'-ethyl-2-methyl-3-piperidinopropiophenone hydrochloride) is an antispastic agent used for treatment of diseases characterized by muscle stiffness and pain. The aim of this research was to investigate the efficacy of eperisone in patients with acute low back pain and spasticity of spinal muscles. The study design was a randomized, double-blind (double-dummy) study in 160 patients with low back pain and no Rx finding of major spinal diseases, randomly assigned to a treatment with oral eperisone 100 mg three times daily (t.i.d.) or thiocolchicoside 8 mg twice daily (b.i.d.) for 12 consecutive days. Analgesic activity was evaluated by scoring "spontaneous pain" (VAS) and pain on movement and pression (4-digit scale), while muscle relaxant activity of the medication was evaluated by means of the "hand-to-floor" distance and the Lasegue's manoeuvre. All the measures were done at the inclusion day and after 3, 7 and 12 days of treatment. The two medications had comparable analgesic and muscle relaxant efficacy. Sponta-neous pain and pain on movement/pressure were significantly reduced by both treatments. Moreover, both eperisone- and thiocolchicoside-treated patients showed a clinically evident muscle relaxation as proved by a progressive reduction in the "hand-to-floor" distance and increase in the articular excursion (Lasegue's manoeuvre). Only 5% of eperisone-treated patients showed minor gastrointestinal side effects, while the incidence of side effects in the thiocolchicoside group was 21.25%. Moreover, in the thiocolchicoside-treated patients also diarrhoea was present, which reached a moderate intensity in some cases. In conclusions, eperisone represents a valuable and safer alternative to other muscle relaxant agents for treatment of low back pain.
Abstract: INTRODUCTION: Eperisone hydrochloride is a centrally acting muscle relaxant, and triazolam is a short-acting benzodiazepine. Although commonly prescribed, cardiotoxicity induced by a single overdose of either drug is comparatively rare. A patient receiving nifedipine developed torsades de pointes (TdP) because of prolongation of the corrected QT (QTc) interval after an overdose of eperisone hydrochloride and triazolam. CASE REPORT: A 60-year-old man receiving nifedipine was admitted in a comatose condition 3 h after ingesting 5,000 mg of eperisone and 2.5 mg of triazolam. Electrocardiogram showed sinus rhythm with prolongation of the QTc interval (820 ms). The serum electrolyte levels were as follows: potassium, 3.8 mEq/L; magnesium, 2.4 mg/dL. The serum drug concentrations were high: eperisone, 15,360 ng/mL; triazolam, 110.8 ng/mL. A temporary cardiac pacemaker was implanted immediately after the development of TdP, 11 h after the ingestion. The serum triazolam concentration normalized on day 2. The QTc interval and eperisone concentration normalized on day 6. CONCLUSION: Eperisone and triazolam overdose can cause life-threatening cardiotoxicity. Electrocardiographic monitoring and serial determination of QTc interval are likely the best way to observe these patients and evaluate the risk of cardiotoxicity.
Abstract: BACKGROUND: Eperisone hydrochloride is a centrally acting muscle relaxant prescribed for muscle stiffness that acts by depressing the activities of α and γ efferent neurons in the spinal cord and supraspinal structures. Although a case of eperisone-induced severe QT prolongation had been reported, the relationship between serum eperisone concentration and QT interval remains obscure. OBJECTIVE: The aim of this study was to investigate the relationship between serum eperisone concentration and QT interval. METHODS: Four patients who overdosed on eperisone were admitted to our hospital between January 2010 and December 2011. We took simultaneous serial measurements of serum eperisone concentration and QT interval in the intensive care unit. In total, 22 measurement points were plotted for these patients. We analyzed the correlation between the serum eperisone concentration and corrected QT (QTc) interval. RESULTS: Three men and one woman (mean age, 50 years) overdosed on eperisone with an average dose of 3087.5 mg (therapeutic dose, 150 mg/day). The mean QTc interval at arrival was 592 ms (range, 444-825 ms), and the mean serum eperisone concentration at arrival was 1257.5 ng/mL (range, 14.5-4120.0 ng/mL). The correlation coefficient was 0.833 between serum eperisone concentration and QTc interval (P < .001). CONCLUSION: Serum eperisone concentration correlates with QTc interval in patients who overdose on eperisone.
Abstract: No Abstract available