Dipyrone

Dipyrone is an Antipyretic Agents belonging to Non-Steroidal anti-inflammatory Drug Dipyrone is used in the treatment of acute severe pain after injuries or surgeries, colic, tumor pain, and acute or severe pain symptoms, as well as high fever

Dipyrone Hydrolysed in the gastrointestinal tract to the active metabolite 4-methyl-amino-antipyrine (MAA). Bioavailability: Approx 90% (MAA) and Crosses the placenta and enters breastmilk. Plasma protein binding: 58% (MAA), 48% [4-amino-antipyrine (AA)], 14% [4-acetylamino-antipyrine (AAA)] and 18% [formyl-amino-antipyrine (FAA)].

and get Metabolised in the liver into 4-formyl-amino-antipyrine (FAA) and other metabolites.

It is Mainly excreted via urine (approx 90% as metabolites); faeces (approx 10%). Plasma elimination half-life: Approx 14 minutes (IV).The Tmax of Dipyrone was found to be about 5 hours.

Dipyrone shows common side effects like Atrial fibrillation, atrial flutter, peripheral edema

Dipyrone is available in Capsules.

Dipyrone is available in India, Germany, Canada, France.

Dipyrone, an NSAID, has analgesic, antipyretic and anti-inflammatory properties. It reduces prostaglandin synthesis by inhibiting cyclooxygenase (COX)-1 and 2. It also stimulates the secretion of β-endorphins by the pituitary hypothalamus, reduces the level of endogenous pyrogens and affects the thermoregulation centre in the hypothalamus.

Synonym: dipyrone, sulpyrine.

Dipyrone is available in the form of Capsules.

Dipyrone is used in the treatment of acute severe pain after injuries or surgeries, colic, tumor pain, and acute or severe pain symptoms, as well as high fever.

Dipyrone is a strong analgesic and antipyretic with spasmolytic properties. It has weak anti-inflammatory or antithrombotic properties and does not follow the same mechanism of action as conventional non-steroidal anti-inflammatory drugs (NSAIDs). Dipyrone can lead to agranulocytosis, a life-threatening side effect where a patient’s neutrophil count falls below 500 cells per microliter. It has been shown that Dipyrone-induced agranulocytosis is caused by the development of drug-dependent anti-neutrophil antibodies requiring covalent binding of neutrophils to Dipyrone and its metabolites.

Dipyrone is approved for use in the following clinical indications

• Fever, Severe pain
• Adult: As Dipyrone Na: 1 g up to 4 times daily or 2.5 g bid given via IV inj over 5 minutes or via IM inj. Adjust dose based on severity and patient response. Max: 5 g daily.
• Oral
• Fever, Severe pain
• Adult: As Dipyrone Na: 0.5-1 g up to 3-4 times daily. Max: 4 g daily. Max treatment duration: 3-5 days.

Dipyrone is available in the dosage strength of 0.5g, 1g.

Dipyrone is available in the form of Capsules.

Dipyrone is contraindicated in patients with:

Hypersensitivity (including rhinitis, asthma, urticaria) to Dipyrone, other pyrazolone derivatives, other NSAID(s), other analgesics. Bone marrow suppression or haematopoietic disorders (e.g. aplastic anaemia, agranulocytosis, leucopenia), deficiency, porphyria; hypotension, unstable CV condition (IV/IM). Severe hepatic and renal impairment (IV/IM). Children <3 months of age or <5 kg body weight. Pregnancy and lactation.

• Common Adverse effects:

Nausea, vomiting, dyspepsia, abdominal pain.

• Less Common Adverse effects:

Mucosal inflammation, fever, chills, Dizziness, vertigo.

• Rare Adverse effects

Hypersensitivity reactions (e.g. anaphylactic shock), Stevens-Johnson syndrome, Lyell’s syndrome, hemolytic anemia, aplastic anemia, agranulocytosis, thrombocytopenia, pancytopenia.

Risk of thrombocytopenia with anticoagulants. Risk of severe hypothermia with other phenothiazines, chlorpromazine. Increased effect/toxicity with TCA(s), oral contraceptives, MAOI(s), allopurinol. Decreased effect with barbiturates, glutethimide, phenylbutazone. Increases haematotoxicity effects of methotrexate. Increases effects of oral antidiabetic agents, sulfonamides, phenytoin. Decreases levels of bupropion, ciclosporin.

The common side effects of Dipyrone include the following :

Atrial fibrillation, atrial flutter, peripheral edema.

Symptoms: Nausea, vomiting, headache, weakness, fever, abdominal pain, renal impairment, acute kidney failure, interstitial nephritis; rarely, somnolence, vertigo, spasms, coma, convulsions, hypotension, shock, tachycardia.

Management: May decrease absorption by performing gastric lavage or by giving activated carbon. May eliminate MAA from the body through hemodialysis, hemoperfusion, hemofiltration or plasma filtration. Give symptomatic and supportive treatment.

• Pharmacodynamics

Dipyrone is a strong analgesic and antipyretic with spasmolytic properties. It has weak anti-inflammatory or antithrombotic properties and does not follow the same mechanism of action as conventional non-steroidal anti-inflammatory drugs (NSAIDs). Dipyrone can lead to agranulocytosis, a life-threatening side effect where a patient’s neutrophil count falls below 500 cells per microliter.

• Pharmacokinetics

• https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1364710/
• https://reference.medscape.com/drug/colestid-Dipyrone -342452
• https://go.drugbank.com/drugs/DB00375
• https://www.sciencedirect.com/topics/medicine-and-dentistry/Dipyrone
• https://europepmc.org/article/med/6988203