Metamizole sodium

Postoperative Pain Management

A single dose of 500 mg of analgin provided effective pain relief (50% or more pain reduction within four to six hours) for 7 out of 10 (70%) participants, compared with 3 out of 10 (30%) with placebo (five studies , 288 comparison participants, moderate evidence of quality), and fewer participants need additional painkillers for four to six hours (7% with dipyrone, 34% with placebo, four studies, 248 participants, low quality data).

Too little data to compare analgin directly with other painkillers.

There was too little information to draw any conclusions about other doses and methods of using dipyrone in these studies, or about the number of people who had side effects. The studies did not report serious side effects or people withdrew from the studies due to side effects, although not all studies provided information about these results. ^{[5] [6]}

Feverish syndrome (infectious and inflammatory diseases, insect bites - mosquitoes , bees , gadflies , etc., post-transfusion complications); Pain syndrome (mild to moderate): including neuralgia , myalgia , arthralgia , biliary colic , intestinal colic , renal colic , trauma, burns , decompression sickness, herpes zoster , orchitis , radiculitis , myositis , postoperative pain, headache , toothache , algodismenorrhea , etc.

Hypersensitivity, suppression of hematopoiesis (agranulocytosis, cytostatic or infectious neutropenia), liver and / or renal failure , hereditary hemolytic anemia associated with deficiency of glucose-6-phosphate dehydrogenase , aspirin asthma , anemia , leukopenia , pregnancy (and especially in the last trimester) weeks), lactation. With caution. The period of the newborn (up to 3 months), kidney disease ( pyelonephritis , glomerulonephritis - including a history ), prolonged abuse of ethanol . Intravenous administration to patients with systolic blood pressure below 100 mmHg or with instability of blood circulation (for example, against the background of myocardial infarction , multiple trauma, beginning shock).

1. From the urinary system:
   • impaired renal function,
   • oliguria
   • anuria
   • proteinuria
   • interstitial nephritis ,
   • staining of urine in red.
2. Allergic reactions :
   • urticaria (including on the conjunctiva and mucous membranes of the nasopharynx ),
   • angioedema ,
   • in rare cases:
     • malignant exudative erythema ( Stevens-Johnson syndrome ),
     • toxic epidermal necrolysis ( Lyell syndrome ),
     • bronchospastic syndrome ,
     • anaphylactic shock .
3. From the hemopoietic organs:
   • agranulocytosis ,
   • leukopenia
   • thrombocytopenia .
4. Other:
   • lowering blood pressure .
5. Local reactions:
   • with intramuscular administration , infiltrates are possible at the injection site, followed by the formation of an abscess in the absence of treatment or a weakened state of the body's defense systems.

Overdose

Symptoms

Nausea , vomiting , gastralgia , oliguria , hypothermia , decreased blood pressure , tachycardia , shortness of breath , tinnitus , drowsiness , delirium , impaired consciousness , acute agranulocytosis , hemorrhagic syndrome , acute renal and / or liver failure, convulsions , respiratory muscle paralysis .

Overdose Treatment

Gastric lavage , saline laxatives , activated charcoal ; forced diuresis , hemodialysis , with the development of convulsive syndrome - intravenous administration of anticonvulsants (in particular, diazepam ) and high-speed barbiturates .

When treating children under 5 years old and patients receiving cytostatic drugs , metamizole sodium should be administered only under the supervision of a doctor. Intolerance is very rare, but the threat of anaphylactic shock after intravenous administration of the drug is relatively higher than after taking the drug inside. Patients with atopic bronchial asthma and pollinosis have an increased risk of allergic reactions. Against the background of taking metamizole sodium, agranulocytosis may develop, in connection with the detection of an unmotivated rise in temperature, chills , sore throat, difficulty swallowing, stomatitis , as well as the development of vaginitis or proctitis , immediate withdrawal of the drug is necessary. With prolonged use, it is necessary to control the picture of peripheral blood. It is unacceptable to use to relieve acute abdominal pain (until the cause is clarified). For intramuscular administration, a long needle must be used. It is possible to stain urine in red due to the release of the metabolite (it does not matter).

Due to the high likelihood of pharmaceutical incompatibility, it cannot be mixed with other drugs in the same syringe . Enhances the effects of ethanol . Radiopaque drugs, colloidal blood substitutes, and penicillin should not be used during treatment with metamizole. With the simultaneous administration of cyclosporine, the concentration of the latter in the blood decreases. Metamizole, displacing oral hypoglycemic drugs, indirect anticoagulants, corticosteroids and indomethacin from the protein bond, increases their activity. Phenylbutazone , barbiturates, and other hepatoinductors with simultaneous administration reduce the effectiveness of metamizole. Simultaneous administration with other non-narcotic analgesics , tricyclic antidepressants , contraceptive hormonal drugs and allopurinol can lead to increased toxicity. Sedative and anxiolytic drugs ( tranquilizers ) enhance the analgesic effect of metamizole. Tiamazole and cytostatics increase the risk of developing leukopenia. The effect is enhanced by codeine , H2-histamine receptor blockers and propranolol (slows inactivation). Myelotoxic drugs increase the hematotoxicity of the drug.

Refers to non-steroidal anti-inflammatory drugs (NSAIDs), a group of pyrazolone derivatives. The mechanism of action is similar to other NSAIDs (non-selectively blocks COX and reduces the formation of prostaglandins from arachidonic acid , however, the effect is not absolute, as is the case with NSAIDs, and can be blocked by stimulation of inflammatory receptors). Prevents pain extra - and proprioreceptive impulses along the Gaulle and Burdach beams , raises the threshold of excitability of thalamic centers of pain sensitivity, increases heat transfer.

A distinctive feature is the slight severity of the anti-inflammatory effect, as a result of which the drug weakly affects the water-salt metabolism (delay of Na ⁺ and water) and the mucous membrane of the gastrointestinal tract . It has a fundamentally analgesic, antipyretic and some antispasmodic (in relation to the smooth muscles of the urinary and biliary tract ) effect. The effect develops 20-30 minutes after ingestion and reaches a maximum after 4 hours. As an antipyretic, it is more effective than ibuprofen and paracetamol ^[7] , but less effective than aspirin. Compared to both drugs, metamizole is the strongest analgesic.

It is well and quickly absorbed in the gastrointestinal tract. It is hydrolyzed in the intestinal wall with the formation of an active metabolite - unchanged metamizole in the blood is absent (only after intravenous administration is an insignificant concentration found in plasma ). The relationship of the active metabolite with proteins is 50-60%. It is metabolized in the liver , excreted by the kidneys . In therapeutic doses, it passes into breast milk.

Synthesized by Ludwig Knorr ( Hoechst ) in 1920 .

In a number of countries, including Sweden (since 1972 ), the USA (since 1977 ), Japan , Australia , and several countries of the European Union , metamizole is prohibited due to side effects, mainly because of the risk of agranulocytosis even with a single use ( according to statistics, when this serious complication occurs, the probability of death is estimated at about 23% ^[8] - in the case of access to medical care). In the 1970s, when bans on the use of this drug began to appear, the risk assessment for agranulocytosis was significantly overestimated ^[9] compared with data at the end of the 1990s (now the risk of this complication is estimated at about 0.2-2 cases per million person-days of use); however, the ban remains in most countries because the drug has so many alternatives available, including aspirin , paracetamol , ibuprofen . In Germany, metamizole is only available on prescription . Since 2009, in Russia , metamizole has been excluded from the list of Essential and Essential Medicines , but has been retained in the free market and in state standards for the provision of emergency medical care for many diseases, such as fever ^[10] in children, injuries ^{[11] [12] [ 13] [14] [15] [16] [17] [18] [19]} , stenosis of the larynx ^[20] , pneumonia ^[21] , renal colic ^[22] , etc.

It reacts with gidroperitom in a crushed state with the release of caustic white smoke (methylammonium hydrosulfide), as a result of which it is used as an effective chemical focus. It also reacts, in crushed form, with a solution of potassium permanganate in an acidic environment, discoloring it, due to sulfite ions.