Metamizole: A Review Profile of a Well-Known “Forgotten” Drug. Part I: Pharmaceutical and Nonclinical Profile

Nikolova, Irina; Tencheva, Jasmina; Voinikov, Julian; Petkova, Valentina; Benbasat, Niko; Danchev, Nikolai

doi:10.5504/bbeq.2012.0089

Cited by 63 publications

(73 citation statements)

References 104 publications

(55 reference statements)

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“…One of the hypotheses states that the underlying mechanism may involve cytotoxic lymphocytes which generate killer cells against drug-coupled bone marrow granulocytic cells (Nikolova et al 2012). There are also reports suggesting that the side effect discussed could be a result of a direct toxic effect of the drug towards granulocytes (Uetrecht et al 1995).…”

Section: Side Effectsmentioning

confidence: 99%

Pharmacological characteristics of metamizole

Jasiecka¹,

Maślanka²,

Jaroszewski³

2014

Polish Journal of Veterinary Sciences

113

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Metamizole (dipyrone) is a popular analgetic, non-opioid drug, commonly used in human and veterinary medicine. In some cases, this agent is still incorrectly classified as a non-steroidal anti-inflammatory drug (NSAID). Metamizole is a pro-drug, which spontaneously breaks down after oral administration to structurally related pyrazolone compounds. Apart from its analgesic effect, the medication is an antipyretic and spasmolytic agent. The mechanism responsible for the analgesic effect is a complex one, and most probably rests on the inhibition of a central cyclooxygenase-3 and activation of the opioidergic system and cannabinoid system. Metamizole can block both PG-dependent and PG-independent pathways of fever induced by LPS, which suggests that this drug has a profile of antipyretic action distinctly different from that of NSAIDs. The mechanism responsible for the spasmolytic effect of metamizole is associated with the inhibited release of intracellular Ca 2+ as a result of the reduced synthesis of inositol phosphate. Metamizole is predominantly applied in the therapy of pain of different etiology, of spastic conditions, especially affecting the digestive tract, and of fever refractory to other treatments. Co-administration of morphine and metamizole produces superadditive, antinociceptive effects. Metamizole is a relatively safe pharmaceutical preparation although it is not completely free from undesirable effects. Among these side-effects, the most serious one that raises most controversy is the myelotoxic effect. It seems that in the past the risk of metamizole-induced agranulocytosis was exaggerated. Despite the evidence showing no risk of teratogenic and embryotoxic effects, the drug must not be administered to pregnant women, although it is allowed to be given to pregnant and lactating animals. This paper seeks to describe the characteristics of metamizole in the light of current knowledge.

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Section: Side Effectsmentioning

confidence: 99%

Pharmacological characteristics of metamizole

Jasiecka¹,

Maślanka²,

Jaroszewski³

2014

Polish Journal of Veterinary Sciences

113

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“…Their anticancer [11][12][13][14] and antimicrobial [15][16][17] properties have also been studied. Pyrazolones have traditionally been used due to their analgesic, antipyretic, and anti-inflammatory activities [18][19][20][21][22]. For example, dipyrone, phenazone, propyphenazone, and ampyrone, drugs in current use, show some or all of these properties (Fig.…”

Section: Introductionmentioning

confidence: 98%

Morita–Baylis–Hillman adducts as building blocks of heterocycles: a simple approach to 4-substituted pyrazolones, and mechanism investigation via ESI–MS(/MS)

et al. 2015

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We describe herein an efficient approach for the preparation of 4-substituted 2,3-dihydro-1H-pyrazol-3-ones starting from Morita-Baylis-Hillman adducts. These heterocycles were obtained in two or three steps as single isomers with moderate to good overall yields. One efficient and alternative methodology for the synthesis of a-methylb-ketoesters is also reported (up to 91 % yield). Additionally, the mechanism of formation of pyrazolones was investigated employing ESI-MS/MS reaction monitoring. Graphical abstract

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“…Se cree que inhibe especialmente la isoenzima ciclooxigenasa-3 en el sistema nervioso central. Tiene propiedades antiespasmódicas relajando el músculo liso y efectos antipiréticos a nivel del centro hipotalámico termorregulador 1,2 .…”

Section: Introductionunclassified