Dependence on Flupirtine

Gahr, Maximilian; Freudenmann, Roland W.; Kölle, Markus; Schönfeldt‐Lecuona, Carlos

doi:10.1002/jcph.129

Cited by 6 publications

(5 citation statements)

References 13 publications

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“…[ 9 10 ] It is a potent analgesic and muscle-relaxant and also has anticonvulsant and antioxidant properties, without any major adverse effects. [ 11 12 13 ] In most of the studies, analgesic efficacy and adverse effects of oral Flupirtine were observed in patients having chronic musculoskeletal pain or cancer pain. [ 14 15 16 17 18 ] Scant literature is available where oral flupirtine was used for postoperative pain relief.…”

Section: Introductionmentioning

confidence: 99%

Comparative evaluation of oral flupirtine and oral diclofenac sodium for analgesia and adverse effects in elective abdominal surgeries

et al. 2015

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Background:Flupirtine is a centrally-acting, nonopioid analgesic that interacts with N-methyl-D-aspartate receptors.Aim:The present study was designed to compare analgesic efficacy and adverse effects of orally administered flupirtine and diclofenac sodium for postoperative pain relief.Settings and Design:In a prospective, randomized double-blind study, 100 patients of American Society of Anesthesiologist grade I and II in the age group of 18–65 years of either sex undergoing elective abdominal surgeries were included after taking informed consent.Materials and Methods:The present study started after 12 h of surgery and patients were randomly divided into two groups of 50 each. For postoperative analgesia, group A received flupirtine 100 mg orally and group B received diclofenac sodium 50 mg orally and study drugs were repeated every 6 hourly for 5 days postoperatively. Vital parameters and visual analogue scale (VAS) scores for pain were recorded at 0, 1, 2, 4, 6, 8, 12, 16 and 24 h, and adverse effects were noted for 48 h of the study period.Statistical Analysis:Data were compiled and analyzed statistically using Chi-square test and two-tailed Student's t-test.Results:Visual analogue scores decreased more rapidly in diclofenac group during 1st h, hence there was rapid onset of analgesia in this group as compared to flupirtine group but later on VAS was comparable in both groups at all measured intervals (P > 0.05). Patients in diclofenac group experienced significantly more heartburn (P = 0.00), impaired taste sensation (P < 0.001) and dizziness (P = 0.004) as compared to flupirtine group.Conclusion:Oral flupirtine and diclofenac sodium were equally effective for postoperative analgesia. There was faster onset of analgesia with diclofenac sodium, but flupirtine was better tolerated by the patients because of its minimal adverse effects.

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Section: Introductionmentioning

confidence: 99%

Comparative evaluation of oral flupirtine and oral diclofenac sodium for analgesia and adverse effects in elective abdominal surgeries

et al. 2015

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“…In line with the implications of FLP's pharmacodynamic profile and recent clinical observations, our analysis of spontaneous reports of FLP‐related ADR revealed continuous reports of FLP abuse/dependence between the years 1991 and 2013 with a tendency of increasing numbers of annual reports from the year 2006 on. Though it was not possible to check the plausibility of the causative role of FLP with regard to the reported addictive behaviors in terms of true causation versus mere correlation, this finding may at least support the hypothesis that FLP might induce addictive behaviors.…”

Section: Discussionmentioning

confidence: 99%

“…. In line with FLP's pharmacodynamic profile yielding agonistic effects at the GABA A receptor, literature provides anecdotal reports of FLP‐abuse or dependence . Considering that the analgesic FLP is used extensively in clinical practice, for example, in Germany in the year 2010 the defined daily doses (DDD) of FLP were 28.6 × 10 6 versus 17.9 × 10 6 DDD of paracetamol, it is mandatory to consider a possible abuse potential of FLP in order to prevent patients treated with FLP from the development of addictive behaviors.…”

mentioning

confidence: 99%

“…Considering that the analgesic FLP is used extensively in clinical practice, for example, in Germany in the year 2010 the defined daily doses (DDD) of FLP were 28.6 × 10 6 versus 17.9 × 10 6 DDD of paracetamol, it is mandatory to consider a possible abuse potential of FLP in order to prevent patients treated with FLP from the development of addictive behaviors. However, there is a distinct absence of studies and only little evidence from clinical practice addressing this issue although FLP's pharmacodynamics suggests this risk. In this regard, data of national pharmacovigilance databases provide valuable insights into factual drug‐related risks based on spontaneous reports of adverse drug reactions (ADR).…”

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confidence: 99%

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Abuse liability of flupirtine revisited: Implications of spontaneous reports of adverse drug reactions

Gahr¹,

Freudenmann²,

Connemann³

et al. 2013

The Journal of Clinical Pharmacology

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Early studies suggested that the centrally acting non-opioid and non-steroidal analgesic flupirtine (FLP) has no potential for abuse. However, FLP's agonistic effects at the GABAA receptor might prime addictive behaviors, and literature provides some anecdotal reports on FLP abuse/dependence. To shed more light on this topic we acquired and evaluated data obtained from a national German pharmacovigilance database. We analyzed all reports of FLP abuse/dependence that were recorded in the database of the German Federal Institute for Drugs and Medical Devices (BfArM). A total of n = 48 reports of FLP abuse/dependence could be identified (mean age 45 years, 62.5% female). First reports were submitted to BfArM in 1991 with increasing numbers of annual reports from the year 2006 on. Mean daily FLP dosage was 805 mg (range 200-3,000 mg). Current or previous substance abuse/dependence was reported in 21% and 17%, respectively. Mean duration of FLP abuse/dependence until report to BfArM was 23 months (range 1-84 months). Withdrawal syndromes after discontinuation of FLP were reported in n = 9 (19%). Our findings strengthen the hypothesis that FLP features a potential to cause addictive behaviors. Female sex, age >40 years, and long-term FLP-treatment may be possible risk factors for the development of FLP abuse/dependence.

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“…55 Analysis of the database of the German Federal Institute for Drugs and Medical Devices (BfArM) for the period 1991 to 2013 only revealed 48 reports of flupirtine abuse or dependence. 56 Further, treatment with flupirtine and development of addictive behaviour being de facto causative or mere correlation could not be clarified.…”

Section: Fibromyalgiamentioning

confidence: 99%

Flupirtine as a Potential Treatment for Fibromyalgia

Lawson¹,

Singh²,

Kantsedikas³

et al. 2021

Journal of Exploratory Research in Pharmacology

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Fibromyalgia is a complex disorder characterised by chronic pain, fatigue, sleep disturbance and cognitive dysfunction with limited benefit gained with current therapies. The mean global prevalence of 2.7% is estimated for this chronic condition. Pharmacological and non-pharmacological therapeutic approaches are often required as treatments of the challenges associated with fibromyalgia. Flupirtine, a non-opioid drug, exhibits effective analgesia in a range of acute and persistent pain conditions, and evidence as treatment of fibromyalgia is considered. Activation of Kv7 potassium channels and agonism at gamma-aminobutyric acid receptor A leading to indirect N-methyl-D-aspartate receptor antagonism is responsible for the analgesic effects of flupirtine and appears to be involved in other symptoms associated with fibromyalgia. Patients with fibromyalgia reported improved control of their symptoms without significant adverse effects in an observational audit in clinical practice. This article presents evidence that flupirtine, or related drugs, is a therapeutic option for the treatment of fibromyalgia. The pharmacology of flupirtine and mechanisms of action involved provide a spectrum of effects that would not only control the chronic pain characteristic of fibromyalgia but many of the other symptoms. Thus, further investigation of the efficacy of flupirtine or related drugs exhibiting a similar pharmacology as a treatment of fibromyalgia would be of interest.

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Dependence on Flupirtine

Abstract: The triaminopyridine derivative flupirtine (FLP) is a centrally acting non-opioid and non-steroidal analgesic with muscle relaxant and neuroprotective properties.

Cited by 6 publications

References 13 publications

Comparative evaluation of oral flupirtine and oral diclofenac sodium for analgesia and adverse effects in elective abdominal surgeries

Comparative evaluation of oral flupirtine and oral diclofenac sodium for analgesia and adverse effects in elective abdominal surgeries

Abuse liability of flupirtine revisited: Implications of spontaneous reports of adverse drug reactions

Flupirtine as a Potential Treatment for Fibromyalgia

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