Dipyrone for acute primary headaches

Ramacciotti, Adriana S; Soares, Bernardo; Atallah, Álvaro Nagib

doi:10.1002/14651858.cd004842.pub2

Cited by 30 publications

(15 citation statements)

References 21 publications

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“…Although it has been withdrawn from the USA, UK, Sweden and Denmark due to severe adverse effects, metamizole is still widely available in Spain, Poland, Bulgaria, Africa, Russia, Latin, India and South America as an effective antipyretic and analgesic drug [1][2][3]. Currently, metamizole is still produced by many companies in China approved by SFDA (State Food and Drug Administration, http:// www.sda.gov.cn/WS01/CL0001/) and widely used despite its potential adverse effects.…”

Section: Introductionmentioning

confidence: 99%

Rapid clinical induction of bupropion hydroxylation by metamizole in healthy Chinese men

Qin

Zhang

Liu

et al. 2012

Brit J Clinical Pharma

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WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT• Bupropion, an antidepressant and smoking cessation drug, is metabolized to its active metabolite, 4-hydroxybupropion, almost exclusively by CYP2B6.• Metamizole, a pyrazolone derivative with analgesic properties, was shown in an in vitro study to increase significantly the expression of CYP2B6 and bupropion hydroxylase activity.• The effect of metamizole on bupropion hydroxylation has not been investigated and drug interactions may occur between metamizole and bupropion. WHAT THIS PAPER ADDS• Oral administration of metamizole for 4 days significantly altered the pharmacokinetics of both bupropion and its active metabolite, 4-hydroxybupropion, and significantly increased the CYP2B6-catalyzed bupropion hydroxylation in all of the subjects.• Dosage adjustment of bupropion may be needed in patients when metamizole is concomitantly administered. AIMSThis study aimed to investigate the effect of metamizole on bupropion hydroxylation related to different CYP2B6 genotype groups in healthy volunteers. METHODSSixteen healthy male volunteers (6 CYP2B6*1/*1, 6 CYP2B6*1/*6 and 4 CYP2B6*6/*6) received orally administered bupropion alone and during daily treatment with metamizole 1500 mg day -1 (500 mg tablet taken three times daily) for 4 days. Serial blood samples were obtained up to 48 h after each bupropion dose. RESULTSAfter metamizole treatment relative to bupropion alone, the geometric mean ratios (GMRs) and 90% confidence interval (CI) of the AUC(0,•) ratio of 4-hydroxybupropion over bupropion were 1.99 (1.57, 2.55) for the CYP2B6*1/*1 group, 2.15 (1.53, 3.05) for the CYP2B6*1/*6 group and 1.86 (1.36, 2.57) for the CYP2B6*6/*6 group. The GMRs and 90% CI of bupropion were 0.695 (0.622, 0.774) for AUC(0,•) and 0.400 (0.353, 0.449) for Cmax, respectively. The corresponding values for 4-hydroxybupropion were 1.43 (1.28, 1.53) and 2.63 (2.07, 2.92). The t1/2 value was significantly increased for bupropion and decreased for 4-hydroxybupropion. The tmax values of bupropion and 4-hydroxybupropion were both significantly decreased. The mean percentage changes in pharmacokinetic parameters among the CYP2B6 genotype groups were not significantly different. CONCLUSIONSOral administration of metamizole for 4 days significantly altered the pharmacokinetics of both bupropion and its active metabolite, 4-hydroxybupropion, and significantly increased the CYP2B6-catalyzed bupropion hydroxylation in all of the subjects. Cautions should be taken when metamizole is co-administered with CYP2B6 substrate drugs.

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Section: Introductionmentioning

confidence: 99%

Rapid clinical induction of bupropion hydroxylation by metamizole in healthy Chinese men

Qin

Zhang

Liu

et al. 2012

Brit J Clinical Pharma

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“…1 The observed reactions are idiosyncratic and are not dose-dependent. 1,2 Metamizole is an effective antipyretic and analgesic drug 3,4 but there is controversy regarding the exact level of risk of haematological toxicity associated with its use. 5 -7 This is reflected in the notable differences in regulatory policies of different countries.…”

Section: Introductionmentioning

confidence: 99%

“…While metamizole is prohibited in the USA, UK, Denmark and Sweden, it is widely available in Spain, Africa, Poland, Bulgaria, Russia, India and Latin and South America. 3,5 Differences in the methods used in the various pharmacovigilance studies …”

Section: Introductionmentioning

confidence: 99%

Update on the Incidence of Metamizole Sodium-Induced Blood Dyscrasias in Poland

2010

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Metamizole sodium (metamizole) is a popular non-opioid analgesic and a common non-prescription product in Poland. Controversy exists regarding the level of risk of agranulocytosis or aplastic anaemia associated with its use. Two previous pharmacovigilance studies conducted in Poland found the risk was low. Twenty-four of the 25 haematology centres that provide specialist care for the 30 million adults in Poland participated in this prospective 12-month study. Twentyone cases of agranulocytosis, 48 of aplastic anaemia, 15 of neutropenia and 11 of pancytopenia were reported. Of these cases, three (two agranulocytosis; one aplastic anaemia) were judged as being possibly related to metamizole. Crude estimates of the rate of agranulocytosis and aplastic anaemia associated with metamizole were 0.16 and 0.08 cases/million person-days of use, respectively. Ongoing national safety surveillance in Poland shows that, despite the possibility of drug-induced blood dyscrasias with metamizole, the risk is very low.

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“…Dipyrone was also effective for the treatment of migraine and episodic TTHs (Ramacciotti et al, 2007 Level I). …”

Section: Simple Analgesicsmentioning

confidence: 99%

Safety of opioid patch initiation in Australian residential aged care

Gadzhanova

Roughead

Pont

2015

Medical Journal of Australia

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Objective: To explore opioid use by aged care facility residents before and after initiation of transdermal opioid patches. Design: A cross‐sectional cohort study, analysing pharmacy data on individual patient supply between 1 July 2008 and 30 September 2013. Setting: Sixty residential aged care facilities in New South Wales. Participants: Residents receiving an initial opioid patch during the study period. Main outcome measure: The proportion of residents who were opioid‐naive in the 4 weeks prior to patch initiation was determined. In addition, the patch strength at initiation and the daily dose of transdermal patches and of additional opioids 1 month after initiation were determined. Results: An opioid patch was initiated in 596 of 5297 residents (11.3%: 2.6% fentanyl, 8.7% buprenorphine) in the 60 residential aged care facilities. The mean age at initiation was 87 years, and 74% of the recipients were women. The proportion of recipients who were opioid‐naive before patch initiation was 34% for fentanyl and 49% for buprenorphine. Most were initiated at the lowest available patch strength, and the dose was up‐titrated after initiation. Around 15% of fentanyl users and 10% of buprenorphine users needed additional regular opioids after patch initiation. Conclusions: The results suggest some inappropriate initiation of opioid patches in Australian residential aged care facilities. Contrary to best practice, a third of residents initiated on fentanyl patches were opioid‐naive in the 4 weeks before initiation.

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Dipyrone for acute primary headaches

Cited by 30 publications

References 21 publications

Rapid clinical induction of bupropion hydroxylation by metamizole in healthy Chinese men

Rapid clinical induction of bupropion hydroxylation by metamizole in healthy Chinese men

Update on the Incidence of Metamizole Sodium-Induced Blood Dyscrasias in Poland

Safety of opioid patch initiation in Australian residential aged care

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