Extreme Sinusbradykardie (30/min) mit akuter Rechtsherzbelastung unter Tizanidin (Sirdalud�)

Kick, Anastas; Bertoli, Raffaela; Moschovitis, Giorgio; Janosa, Pia Caduff; Cerny, Andreas

doi:10.1007/s00063-005-1024-2

Cited by 9 publications

(11 citation statements)

References 3 publications

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“…Similar exaggerated pharmacodynamic effects of tizanidine were seen in our healthy subjects after ingestion of tizanidine during the rofecoxib phase. In one case report, QT-prolongation was also observed during the combination [2]. However, we found no evidence of QTc-prolongation after tizanidine intake during either the rofecoxib or placebo phases.…”

Section: Discussioncontrasting

confidence: 71%

“…Thus, it is most probable that the cardiovascular and central nervous system adverse reactions (e.g. hypotension, bradycardia, somnolence), observed in several patients after the concomitant intake of rofecoxib and tizanidine [1,2], were caused by this pharmacokinetic interaction. Until now, the mechanism of this suspected interaction was unknown.…”

Section: Discussionmentioning

confidence: 99%

“…Cases of symptomatic hypotension, bradycardia and somnolence have been observed (one with a fatal outcome) during coadministration of rofecoxib and tizanidine [1,2], demonstrating the potential hazards of this interaction. Similar exaggerated pharmacodynamic effects of tizanidine were seen in our healthy subjects after ingestion of tizanidine during the rofecoxib phase.…”

Section: Discussionmentioning

confidence: 99%

“…Recent case reports have suggested an interaction between rofecoxib and tizanidine [1,2]. The adverse reactions observed involved both the central nervous and cardiovascular systems.…”

Section: Introductionmentioning

confidence: 99%

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Rofecoxib is a potent inhibitor of cytochrome P450 1A2: studies with tizanidine and caffeine in healthy subjects

Backman

Karjalainen

Neuvonen

et al. 2006

Brit J Clinical Pharma

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AimsCase reports suggest an interaction between rofecoxib and the CYP1A2 substrate tizanidine. Our objectives were to explore the extent and mechanism of this possible interaction and to determine the CYP1A2 inhibitory potency of rofecoxib. MethodsIn a randomized, double-blind, two-phase cross-over study, nine healthy subjects took 25 mg rofecoxib or placebo daily for 4 days and, on day 4, each ingested 4 mg tizanidine. Plasma concentrations and the urinary excretion of tizanidine, its metabolites (M) and rofecoxib, and pharmacodynamic variables were measured up to 24 h. On day 3, a caffeine test was performed to estimate CYP1A2 activity. ResultsRofecoxib increased the area under the plasma concentration-time curve (AUC 0-∞ ) of tizanidine by 13.6-fold [95% confidence interval (CI) 8.0, 15.6; P < 0.001), peak plasma concentration ( C max ) by 6.1-fold (4.8, 7.3; P < 0.001) and elimination halflife ( t 1/2 ) from 1.6 to 3.0 h ( P < 0.001). Consequently, rofecoxib markedly increased the blood pressure-lowering and sedative effects of tizanidine ( P < 0.05). Rofecoxib increased several fold the tizanidine/M-3 and tizanidine/M-4 ratios in plasma and urine and the tizanidine/M-5, tizanidine/M-9 and tizanidine/M-10 ratios in urine ( P < 0.05). In addition, it increased the plasma caffeine/paraxanthine ratio by 2.4-fold (95% CI 1.4, 3.4; P = 0.008) and this ratio correlated with the tizanidine/ metabolite ratios. Finally, the AUC 0 − 25 of rofecoxib correlated with the placebo phase caffeine/paraxanthine ratio ( r = 0.80, P = 0.01). ConclusionsRofecoxib is a potent inhibitor of CYP1A2 and it greatly increases the plasma concentrations and adverse effects of tizanidine. The findings suggest that rofecoxib itself is also metabolized by CYP1A2, raising concerns about interactions between rofecoxib and other CYP1A2 substrate and inhibitor drugs.

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Section: Discussioncontrasting

confidence: 71%

Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

“…Recent case reports have suggested an interaction between rofecoxib and tizanidine [1,2]. The adverse reactions observed involved both the central nervous and cardiovascular systems.…”

Section: Introductionmentioning

confidence: 99%

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Rofecoxib is a potent inhibitor of cytochrome P450 1A2: studies with tizanidine and caffeine in healthy subjects

Backman

Karjalainen

Neuvonen

et al. 2006

Brit J Clinical Pharma

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“…Es wird vermutet, dass NSAR dadurch in die sy− naptische Zellübertragung eingreifen, insbesondere auch in den Dopaminstoffwechsel, und so psychiatrische Nebenwirkungen entfalten können [6]. Rofecoxib ist ein Hemmer der Cytochrom− oxidase P450 1A2, sodass ein Teil der Nebenwirkungen des Prä− parates durch pharmakokinetische Interaktionen verursacht sein kann [10]; für die bei unseren Fällen eingenommenen Medi− kamente ist jedoch keine Interaktion mit der Cytochromoxidase P450 1A2 beschrieben. Die COX−2 interagiert mit Neurotrans− mittern wie Azetylcholin, Dopamin [11], Serotonin (Aktivierung serotonerger Signalwege) und Glutamat [12,13].…”

Section: Fallunclassified

Psychotische Störung unter Rofecoxib

Sabolek

Unrath²,

Sperfeld³

et al. 2007

Psychiat Prax

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Acute psychosis is a possible side effect of many centrally acting drugs. Its appearance is facilitated by certain conditions like advanced age, comedication, or comorbidity. We report two cases of acute psychotic syndromes with visual (Case 1 + 2) and auditory (Case 1) hallucinations under rofecoxib, a cyclooxygenase-2-inhibitor. This is one of the first reports of psychotic disorders under rofecoxib intake. We present a review of the literature on mental side effects of NSAID and on the pharmacological basis of the association of cyclooxygenase-inhibitors and mental disorders.

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Risk of tizanidine-induced adverse events after concomitant exposure to ciprofloxacin: A cohort study in the U.S.

Giannouchos¹,

Gómez-Lumbreras

Malone

2022

The American Journal of Emergency Medicine

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Extreme Sinusbradykardie (30/min) mit akuter Rechtsherzbelastung unter Tizanidin (Sirdalud�)

Abstract: When prescribing Sirdalud, the possible pharmacological side effects and interactions should be taken into careful account.

Cited by 9 publications

References 3 publications

Rofecoxib is a potent inhibitor of cytochrome P450 1A2: studies with tizanidine and caffeine in healthy subjects

Rofecoxib is a potent inhibitor of cytochrome P450 1A2: studies with tizanidine and caffeine in healthy subjects

Psychotische Störung unter Rofecoxib

Risk of tizanidine-induced adverse events after concomitant exposure to ciprofloxacin: A cohort study in the U.S.

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