Metamizole

Metamizole
Formula C13H16N3NaO4S
Molar Mass (g·mol−1) 333,34
Physical State solid
Melting Point (°C) 224,5–227
CAS Number 68-89-3
PUB Number 3111
Drugbank ID DB04817
Solubility soluble in water

Basics

Metamizole sodium is an analgesic and antipyretic belonging to the group of non-opioid analgesics. Due to a rare but serious side effect (agranulocytosis), metamizole is no longer approved for use in many countries. In German-speaking countries, however, its use is still widespread. It is usually administered in the form of tablets.

Pharmacology

Pharmacodynamics

The exact mechanism of action has not yet been deciphered. What is certain is the inhibition of the enzyme cyclooxygenase, which is essential for the development of pain. However, researchers suspect that opioid and 5-HT receptors are additional targets of the drug, which may also influence pain perception to a certain extent.

Pharmacokinetics

Metamizole is used exclusively as the sodium salt metamizole sodium. This makes it possible to administer the substance as a tablet. The half-life of metamizole is very short. It is metabolized in the liver and the bioavailability is about 90%. The plasma half-life is about 2.5 hours. Excretion occurs through the kidneys.

Drug Interactions

Concomitant administration with chlorpromazine should be avoided as dangerous hypothermia may result.

In combination with methotrexate, liver damage may occur.

Toxicity

Side effects

Due to the rare and life-threatening side effect agranulocytosis, Metamizole is no longer used in many countries. The incidence here is 1 treated per 1 000 000 patients.

Other side effects that may occasionally occur

  • Hypotension
  • Drug exanthema
  • Reddening of the urine
  • Leukopenia
  • Skin reactions

Toxicological data

LD50 (rat, oral): 4351 mg.kg-1

Markus Falkenstätter

Markus Falkenstätter
Author

Markus Falkenstätter ist Autor zu pharmazeutischen Themen in der Medizin-Redaktion von Medikamio. Er befindet sich im letzten Semester seines Pharmaziestudiums an der Universität Wien und liebt das wissenschaftliche Arbeiten im Bereich der Naturwissenschaften.

Mag. pharm Stefanie Lehenauer

Mag. pharm Stefanie Lehenauer
Lector

Stefanie Lehenauer ist seit 2020 freie Autorin bei Medikamio und studierte Pharmazie an der Universität Wien. Sie arbeitet als Apothekerin in Wien und ihre Leidenschaft sind pflanzliche Arzneimittel und deren Wirkung.

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