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Pronunciation
Algimabo (ES); Algirona (BR); Algopyrin (HU, LI); Alnex (MX); Analgin (BG, CZ, DE, EG, LI, LV, RU);
Analgina (AR, PY); Analgine (BE); Antalgin (ID); Antalgina (PE); Causalon (UY); Conmel (CO, VE); Cornalgin (ID); Defin (MX); Di Shuang (CN);
Dialgin (BG); Diprin (BR); Dolanet (PY); Dolemicin (ES); Dolgan (LI, MX); Dolocalma (PT); Foragin (ID); Hexalgin (BG); Laper (CO); Magnopyrol
(BR); Metamizol (CL); Metazol (ET); Minalgin (CH); Natralgin (GR); Nolotil (ES, PT); Novalcina (VE); Novalgin (AT, CH, CZ, DE, NL, PK);
Novalgina (AR, CO, IT, PE, UY); Novalgine (BE, VN); Optalgin (HU, IL); Proalgin (BG); Promel (VE); Sinalgia (PY); Taxenil (AR); Telalgin (GR); VDalgin (IL)
Pharmacologic Category
Dosing: Adult
Pain (moderate to severe) and fever: Note: Oral solution 500 mg/mL dosing varies based on product dropper and
Dosing: Geriatric
There are no specific dosage adjustments in the manufacturers labeling; use caution and consider reduced
Dosing: Pediatric
Pain (moderate to severe) and fever: Note: Concentrated oral solution (500 mg/mL) dosing varies based on
product dropper and product labeling. Consult product labeling for details.
Children 3 months to Adolescents <15 years:
<5 kg (<3 months): Use is contraindicated
5 to 8 kg (average age 3 to 11 months):
IM: 50 to 100 mg up to 4 times daily. Note: IV injection is not indicated in children <1 year.
Oral solution, 50 mg/mL: Usual dosage: 1.25 to 2.5 mL up to 4 times daily; maximum: 10 mL daily
Rectal (suppository): Use is contraindicated
9 to 15 kg (average age 1 to 3 years):
IM, IV: 100 to 250 mg up to 4 times daily
Oral solution, 50 mg/mL: Usual dosage: 2.5 to 5 mL up to 4 times daily; maximum: 20 mL daily
Rectal (suppository): Use is contraindicated
16 to 23 kg (average age 4 to 6 years):
IM, IV: 150 to 400 mg up to 4 times daily
Oral solution, 50 mg/mL: Usual dosage: 3.75 to 7.5 mL up to 4 times daily; maximum: 30 mL daily
Rectal (suppository): 300 mg up to 4 times daily
There are no specific dosage adjustments in the manufacturers labeling (has not been studied in
multiple doses); use caution and consider reduced doses for chronic therapy since the rate of elimination may be reduced.
There are no specific dosage adjustments in the manufacturers labeling (has not been studied
in multiple doses); use caution and consider reduced doses for chronic therapy since the rate of elimination may be reduced.
Analgesic and antipyretic: For the treatment of moderate to severe pain and fever
Administration: IM
Administration: IV
Administration: Oral
Administer with a sufficient glass of water or other liquid. Use manufacturer supplied dropper for
concentrated oral solution (500 mg/mL). Calibration of dropper may differ between manufacturers (consult specific product labeling for
administration details).
Administration: Rectal
Dietary Considerations
Some formulations may contain sucrose, sorbitol, and/or sodium; use with caution in patients with
Storage/Stability
Compatibility
International issues: Metamizole (INN for dipyrone) may be confused with methimazole
Contraindications
any other component of the formulation; history of bronchospasm or other anaphylactoid reactions with salicylate analgesics or other
NSAIDS; acute hepatic porphyria; pregnancy and breast-feeding; genetic deficiency of glucose-6-phophate dehydrogenase (G6PD); bone
marrow suppression or impairment (eg, following chemotherapy); hematopoietic disorders including history of blood dyscrasias; use in
children <3 months of age or weighing <5 kg; IV use in children 3 to 11 months or weighing <9 kg, parenteral use in hemodynamically
unstable patients or patients with hypotension; fructose intolerance (oral products containing sucrose/sorbitol)
Warnings/Precautions
Concerns related to adverse effects:
Agranulocytosis: Rare cases of agranulocytosis have been reported which can be fatal. Reactions can occur at any time during
treatment and may be dose dependent. Discontinue use immediately with neutropenia (neutrophils <1,500 /mm3) or if any of the
following signs or symptoms develop: fever, chills, sore throat, or oral ulcers. Monitor CBC until levels return to normal and do
not reinitiate therapy. Use is contraindicated in patients with previous agranulocytosis reaction to dipyrone or any pyrazolidine
derivatives.
Dermatologic reactions: Serious skin reactions, including Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN)
have been reported. Monitor closely for skin reactions within the first weeks of treatment; if symptoms develop discontinue
dipyrone immediately and do not resume.
Hypersensitivity reactions: Hypersensitivity, anaphylactic, and anaphylactoid reactions have been reported. Risk factors include
patients with asthma, atopic allergies, chronic urticaria, alcohol intolerance, intolerance to dyes (eg, tartrazine) or preservatives
(eg, benzoates), hypersensitivity to pyrazolone and pyrazolidine derivatives, or reactions to other non-narcotic analgesics. Risks
may be greater with parenteral administration.
Hypotension: Hypotensive reactions may occur, particularly with parenteral administration and may be dose dependent; administer
injections slowly. Risk is increased in patients with high fever, preexisting hypotonia, hypovolemia or dehydration, circulatory
instability or initial circulatory failure (eg, cardiac arrest or polytrauma). Closely monitor patients at risk of hypotension and
patients with comorbidities adversely affected by hypotension (eg, coronary artery disease or severe cerebrovascular stenosis).
Pancytopenia: Discontinue immediately with the development of pancytopenia; monitor CBC until levels return to normal. Advise
patients to seek immediate medical attention if they develop signs and symptoms suggestive of blood dyscrasias (eg, malaise,
infection, persistent fever, bruising, bleeding, pallor).
Urine discoloration: Red coloration may appear in urine with acid pH due to a small quantity of the metabolite, rubazonic acid.
Disease-related concerns:
Asthma: Use caution in patients with asthma; risk of severe anaphylactoid reaction may be increased.
Hepatic impairment: Use with caution in patients with hepatic impairment; elimination of dipyrone may be reduced. Dosage
adjustments may be needed.
Renal impairment: Use with caution in patients with renal impairment; elimination of dipyrone may be reduced. Dosage adjustments
may be needed.
Concurrent drug therapy issues:
Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring,
and/or selection of alternative therapy. Consult drug interactions database for more detailed information.
Dosage form specific issues:
Sodium: Some dosage forms may contain sodium; consider the sodium quantities for patients with a controlled sodium diet. See
specific product labeling for sodium content details.
Sucrose or sorbitol: Some dosage forms may contain sucrose or sorbitol. Use with caution in patients with diabetes; avoid use in
patients with fructose intolerance.
Sulfites: Some dosage forms may contain sodium dithionite or sodium metabisulfite. Use with caution in patients with sulfite
allergies.
Other warnings/precautions:
Restricted use: Due to risks for agranulocytosis and anaphylaxis some countries have banned dipyrone use or implemented
restrictions for use relating to specific indications, formulations, and doses. Consult local prescribing information for more
information (United Nations, 2005).
Pregnancy Considerations
Adverse events have not been observed in animal reproduction studies. Dipyrone crosses the
placental barrier. Use of NSAIDs in late pregnancy may increase the risk of premature closure of the ductus arteriosus as well as platelet
disorders. There is insufficient clinical data on the use during pregnancy; the use of dipyrone in pregnancy women is contraindicated by the
manufacturer.
Breast-Feeding Considerations
Adverse Reactions
Cardiovascular: Cardiac arrhythmia, circulatory shock, transient hypotension
Dermatologic: Burning sensation of skin, erythema, pruritus, skin rash, Stevens-Johnson syndrome, swelling of the skin, toxic epidermal
necrolysis, urticaria
Gastrointestinal: Gastrointestinal symptoms
Genitourinary: Anuria, oliguria, proteinuria, red urine discoloration
Hematologic & Oncologic: Agranulocytosis, aplastic anemia, leukopenia, pancytopenia, thrombocytopenia
Hypersensitivity: Anaphylactic shock, anaphylactoid reaction, anaphylaxis, angioedema, fixed drug eruption
Renal: Acute interstitial nephritis, acute renal failure
Respiratory: Acute asthma, dyspnea, severe bronchospasm
Metabolism/Transport Effects
Drug Interactions
None known.
Open Interactions
5-ASA Derivatives: Nonsteroidal Anti-Inflammatory Agents may enhance the nephrotoxic effect of 5-ASA Derivatives. Risk C: Monitor
therapy
ACE Inhibitors: May enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents. Specifically, the combination may result
in a significant decrease in renal function. Nonsteroidal Anti-Inflammatory Agents may diminish the antihypertensive effect of ACE
Inhibitors. Risk C: Monitor therapy
Agents with Antiplatelet Properties (e.g., P2Y12 inhibitors, NSAIDs, SSRIs, etc.): May enhance the antiplatelet effect of other Agents with
Antiplatelet Properties. Risk C: Monitor therapy
Alcohol (Ethyl): May enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents. Specifically, the risk of GI bleeding may
be increased with this combination. Risk C: Monitor therapy
Aliskiren: Nonsteroidal Anti-Inflammatory Agents may diminish the antihypertensive effect of Aliskiren. Nonsteroidal Anti-Inflammatory
Agents may enhance the nephrotoxic effect of Aliskiren. Management: Monitor renal function periodically in patients receiving
aliskiren and any nonsteroidal anti-inflammatory agent. Patients at elevated risk of renal dysfunction include those who are elderly,
are volume depleted, or have pre-existing renal dysfunction. Risk C: Monitor therapy
Aminoglycosides: Nonsteroidal Anti-Inflammatory Agents may decrease the excretion of Aminoglycosides. Data only in premature
infants. Risk C: Monitor therapy
Angiotensin II Receptor Blockers: May enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents. Specifically, the
combination may result in a significant decrease in renal function. Nonsteroidal Anti-Inflammatory Agents may diminish the
therapeutic effect of Angiotensin II Receptor Blockers. The combination of these two agents may also significantly decrease
glomerular filtration and renal function. Risk C: Monitor therapy
Anticoagulants: Agents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants. Risk C: Monitor therapy
Anticoagulants: Nonsteroidal Anti-Inflammatory Agents may enhance the anticoagulant effect of Anticoagulants. Risk C: Monitor therapy
Antidepressants (Tricyclic, Tertiary Amine): May enhance the antiplatelet effect of NSAID (Nonselective). Risk C: Monitor therapy
Apixaban: NSAID (Nonselective) may enhance the adverse/toxic effect of Apixaban. Specifically, the risk of bleeding may be increased.
Management: A comprehensive risk to benefit assessment should be done for all patients before any concurrent use of apixaban
and nonsteroidal anti-inflammatory drugs (NSAIDs). If combined, monitor patients extra closely for signs and symptoms of bleeding.
Risk D: Consider therapy modification
Beta-Blockers: Nonsteroidal Anti-Inflammatory Agents may diminish the antihypertensive effect of Beta-Blockers. Exceptions:
Levobunolol; Metipranolol. Risk C: Monitor therapy
Bile Acid Sequestrants: May decrease the absorption of Nonsteroidal Anti-Inflammatory Agents. Risk D: Consider therapy modification
Bisphosphonate Derivatives: Nonsteroidal Anti-Inflammatory Agents may enhance the adverse/toxic effect of Bisphosphonate
Derivatives. Both an increased risk of gastrointestinal ulceration and an increased risk of nephrotoxicity are of concern. Risk C:
Monitor therapy
Collagenase (Systemic): Agents with Antiplatelet Properties may enhance the adverse/toxic effect of Collagenase (Systemic).
Specifically, the risk of injection site bruising and/or bleeding may be increased. Risk C: Monitor therapy
Corticosteroids (Systemic): May enhance the adverse/toxic effect of NSAID (Nonselective). Risk C: Monitor therapy
CycloSPORINE (Systemic): Nonsteroidal Anti-Inflammatory Agents may enhance the nephrotoxic effect of CycloSPORINE (Systemic).
Nonsteroidal Anti-Inflammatory Agents may increase the serum concentration of CycloSPORINE (Systemic). CycloSPORINE
(Systemic) may increase the serum concentration of Nonsteroidal Anti-Inflammatory Agents. Specifically, elevated diclofenac
concentrations have been reported. Management: Consider alternatives to nonsteroidal anti-inflammatory agents (NSAIDs). Monitor
for evidence of nephrotoxicity, as well as increased serum cyclosporine concentrations and systemic effects (e.g., hypertension)
during concomitant therapy with NSAIDs. Risk D: Consider therapy modification
Dabigatran Etexilate: NSAID (Nonselective) may enhance the adverse/toxic effect of Dabigatran Etexilate. Specifically, the risk of bleeding
may be increased. Management: A comprehensive risk to benefit assessment should be done for all patients before any concurrent
use of dabigatran and nonsteroidal anti-inflammatory drugs (NSAIDs). If combined, monitor patients extra closely for signs and
symptoms of bleeding. Risk D: Consider therapy modification
Deferasirox: Nonsteroidal Anti-Inflammatory Agents may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI
ulceration/irritation or GI bleeding may be increased. Risk C: Monitor therapy
Deoxycholic Acid: Agents with Antiplatelet Properties may enhance the adverse/toxic effect of Deoxycholic Acid. Specifically, the risk for
bleeding or bruising in the treatment area may be increased. Risk C: Monitor therapy
Desmopressin: Nonsteroidal Anti-Inflammatory Agents may enhance the adverse/toxic effect of Desmopressin. Risk C: Monitor therapy
Dexketoprofen: May enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents. Risk X: Avoid combination
Diclofenac (Systemic): May enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents. Management: Seek alternatives
to the combined use of diclofenac with other nonsteroidal anti-inflammatory agents (NSAIDs). Avoid the use of
diclofenac/misoprostol with other NSAIDs. Risk D: Consider therapy modification
Digoxin: Nonsteroidal Anti-Inflammatory Agents may increase the serum concentration of Digoxin. Risk C: Monitor therapy
Drospirenone: Nonsteroidal Anti-Inflammatory Agents may enhance the hyperkalemic effect of Drospirenone. Risk C: Monitor therapy
Edoxaban: NSAID (Nonselective) may enhance the adverse/toxic effect of Edoxaban. Specifically, the risk of bleeding may be increased.
Management: A comprehensive risk to benefit assessment should be done for all patients before any concurrent use of edoxaban
and nonsteroidal anti-inflammatory drugs (NSAIDs). If combined, monitor patients extra closely for signs and symptoms of bleeding.
Risk D: Consider therapy modification
Eplerenone: Nonsteroidal Anti-Inflammatory Agents may diminish the antihypertensive effect of Eplerenone. Nonsteroidal AntiInflammatory Agents may enhance the hyperkalemic effect of Eplerenone. Risk C: Monitor therapy
Floctafenine: May enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents. Risk X: Avoid combination
Glucosamine: May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Risk C: Monitor therapy
Haloperidol: Nonsteroidal Anti-Inflammatory Agents may enhance the adverse/toxic effect of Haloperidol. Specifically including
drowsiness and confusion. Risk C: Monitor therapy
Herbs (Anticoagulant/Antiplatelet Properties) (eg, Alfalfa, Anise, Bilberry): May enhance the adverse/toxic effect of Agents with
Antiplatelet Properties. Bleeding may occur. Risk D: Consider therapy modification
Herbs (Anticoagulant/Antiplatelet Properties) (eg, Alfalfa, Anise, Bilberry): May enhance the adverse/toxic effect of Nonsteroidal AntiInflammatory Agents. Bleeding may occur. Management: Concomitant treatment with these agents should generally be avoided. If
used concomitantly, increased diligence in monitoring for adverse effects (eg, bleeding, bruising, altered mental status due to CNS
bleeds) must be employed. Risk D: Consider therapy modification
HydrALAZINE: Nonsteroidal Anti-Inflammatory Agents may diminish the antihypertensive effect of HydrALAZINE. Risk C: Monitor therapy
Ketorolac (Nasal): May enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents. Risk X: Avoid combination
Ketorolac (Systemic): May enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents. Risk X: Avoid combination
Limaprost: May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Risk C: Monitor therapy
Lithium: Nonsteroidal Anti-Inflammatory Agents may increase the serum concentration of Lithium. Risk D: Consider therapy modification
Loop Diuretics: Nonsteroidal Anti-Inflammatory Agents may diminish the diuretic effect of Loop Diuretics. Loop Diuretics may enhance
the nephrotoxic effect of Nonsteroidal Anti-Inflammatory Agents. Management: Monitor for evidence of kidney injury or decreased
therapeutic effects of loop diuretics with concurrent use of an NSAID. Consider avoiding concurrent use in CHF or cirrhosis.
Concomitant use of bumetanide with indomethacin is not recommended. Risk D: Consider therapy modification
Methotrexate: May enhance the adverse/toxic effect of Dipyrone. Specifically, the risk for agranulocytosis and pancytopenia may be
increased. Dipyrone may enhance the adverse/toxic effect of Methotrexate. Risk X: Avoid combination
Morniflumate: May enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents. Risk X: Avoid combination
Multivitamins/Fluoride (with ADE): May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Risk C: Monitor therapy
Multivitamins/Minerals (with ADEK, Folate, Iron): May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Risk C:
Monitor therapy
Multivitamins/Minerals (with AE, No Iron): May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Risk C: Monitor
therapy
Myelosuppressive Agents: Dipyrone may enhance the adverse/toxic effect of Myelosuppressive Agents. Specifically, the risk for
agranulocytosis and pancytopenia may be increased Risk X: Avoid combination
Nonsteroidal Anti-Inflammatory Agents: May enhance the adverse/toxic effect of other Nonsteroidal Anti-Inflammatory Agents. Risk C:
Monitor therapy
NSAID (COX-2 Inhibitor): Nonsteroidal Anti-Inflammatory Agents may enhance the adverse/toxic effect of NSAID (COX-2 Inhibitor). Risk X:
Avoid combination
Omacetaxine: Nonsteroidal Anti-Inflammatory Agents may enhance the adverse/toxic effect of Omacetaxine. Specifically, the risk for
bleeding-related events may be increased. Management: Avoid concurrent use of nonsteroidal antiinflammatory drugs (NSAIDs) with
omacetaxine in patients with a platelet count of less than 50,000/uL. Risk X: Avoid combination
Omega-3 Fatty Acids: May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Risk C: Monitor therapy
Pentosan Polysulfate Sodium: May enhance the adverse/toxic effect of Agents with Antiplatelet Properties. Specifically, the risk of
bleeding may be increased by concurrent use of these agents. Risk C: Monitor therapy
Pentoxifylline: May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Risk C: Monitor therapy
Porfimer: Photosensitizing Agents may enhance the photosensitizing effect of Porfimer. Risk C: Monitor therapy
Potassium-Sparing Diuretics: Nonsteroidal Anti-Inflammatory Agents may diminish the antihypertensive effect of Potassium-Sparing
Diuretics. Nonsteroidal Anti-Inflammatory Agents may enhance the hyperkalemic effect of Potassium-Sparing Diuretics. Risk C:
Monitor therapy
PRALAtrexate: Nonsteroidal Anti-Inflammatory Agents may increase the serum concentration of PRALAtrexate. More specifically, NSAIDS
may decrease the renal excretion of pralatrexate. Management: Closely monitor for increased pralatrexate serum levels and/or
toxicity if used concomitantly with an NSAID. Monitor for decreased pralatrexate serum levels with NSAID discontinuation. Risk C:
Monitor therapy
Probenecid: May increase the serum concentration of Nonsteroidal Anti-Inflammatory Agents. Risk C: Monitor therapy
Prostacyclin Analogues: May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Risk C: Monitor therapy
Prostaglandins (Ophthalmic): Nonsteroidal Anti-Inflammatory Agents may diminish the therapeutic effect of Prostaglandins (Ophthalmic).
Nonsteroidal Anti-Inflammatory Agents may also enhance the therapeutic effects of Prostaglandins (Ophthalmic). Risk C: Monitor
therapy
Quinolone Antibiotics: Nonsteroidal Anti-Inflammatory Agents may enhance the neuroexcitatory and/or seizure-potentiating effect of
Quinolone Antibiotics. Nonsteroidal Anti-Inflammatory Agents may increase the serum concentration of Quinolone Antibiotics. Risk
C: Monitor therapy
Rivaroxaban: NSAID (Nonselective) may enhance the adverse/toxic effect of Rivaroxaban. Specifically, the risk of bleeding may be
increased. Management: A comprehensive risk to benefit assessment should be done for all patients before any concurrent use of
rivaroxaban and nonsteroidal anti-inflammatory drugs (NSAIDs). If combined, monitor patients extra closely for signs and symptoms
of bleeding. Risk D: Consider therapy modification
Salicylates: NSAID (Nonselective) may enhance the adverse/toxic effect of Salicylates. An increased risk of bleeding may be associated
with use of this combination. NSAID (Nonselective) may diminish the cardioprotective effect of Salicylates. Salicylates may decrease
the serum concentration of NSAID (Nonselective). Exceptions: Choline Magnesium Trisalicylate. Risk D: Consider therapy
modification
Salicylates: Agents with Antiplatelet Properties may enhance the adverse/toxic effect of Salicylates. Increased risk of bleeding may result.
Risk C: Monitor therapy
Selective Serotonin Reuptake Inhibitors: May enhance the antiplatelet effect of NSAID (Nonselective). NSAID (Nonselective) may diminish
the therapeutic effect of Selective Serotonin Reuptake Inhibitors. Management: Consider using alternative analgesics, when
appropriate, and/or addition of a gastroprotective agent. Monitor patients closely for signs/symptoms of bleeding, and for evidence
of diminished SSRI effectiveness with concurrent use. Risk D: Consider therapy modification
Serotonin/Norepinephrine Reuptake Inhibitors: May enhance the antiplatelet effect of NSAID (Nonselective). Risk C: Monitor therapy
Sodium Phosphates: May enhance the nephrotoxic effect of Nonsteroidal Anti-Inflammatory Agents. Specifically, the risk of acute
phosphate nephropathy may be enhanced. Management: Consider avoiding this combination by temporarily suspending treatment
with NSAIDs, or seeking alternatives to oral sodium phosphate bowel preparation. If the combination cannot be avoided, maintain
adequate hydration and monitor renal function closely. Risk D: Consider therapy modification
Talniflumate: May enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents. Risk X: Avoid combination
Tenofovir Products: Nonsteroidal Anti-Inflammatory Agents may enhance the nephrotoxic effect of Tenofovir Products. Management:
Seek alternatives to these combinations whenever possible. Avoid use of tenofovir with multiple NSAIDs or any NSAID given at a high
dose. Risk D: Consider therapy modification
Thiazide and Thiazide-Like Diuretics: May enhance the nephrotoxic effect of Nonsteroidal Anti-Inflammatory Agents. Nonsteroidal AntiInflammatory Agents may diminish the therapeutic effect of Thiazide and Thiazide-Like Diuretics. Risk C: Monitor therapy
Thrombolytic Agents: Agents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents. Risk C: Monitor
therapy
Tipranavir: May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Risk C: Monitor therapy
Treprostinil: May enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents. Bleeding may occur. Risk C: Monitor therapy
Urokinase: Agents with Antiplatelet Properties may enhance the anticoagulant effect of Urokinase. Risk X: Avoid combination
Vancomycin: Nonsteroidal Anti-Inflammatory Agents may increase the serum concentration of Vancomycin. Risk C: Monitor therapy
Verteporfin: Photosensitizing Agents may enhance the photosensitizing effect of Verteporfin. Risk C: Monitor therapy
Vitamin E: May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Risk C: Monitor therapy
Vitamin E (Oral): May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Risk C: Monitor therapy
Vitamin K Antagonists (eg, warfarin): NSAID (Nonselective) may enhance the anticoagulant effect of Vitamin K Antagonists. Risk D:
Consider therapy modification
Monitoring Parameters
CBC; liver function and renal function; observe for bleeding, bruising, signs/symptoms of
Excipient information presented when available (limited, particularly for generics); consult
specific product labeling. Note: Availability of specific dosage forms may vary by country/region.
Solution, Injection, as monohydrate: 500 mg/mL
Solution, Oral, as monohydrate: 50 mg/mL, 500 mg/mL
Suppository, Rectal, as monohydrate: 300 mg
Tablet, Oral, as monohydrate: 500 mg, 1 g
Mechanism of Action
Dipyrone is a pyrazolone derivative with analgesic, antipyretic, and spasmolytic properties. The mechanism
of action is not known in detail; however, effects are thought to be related to inhibition of cyclooxygenase, inhibition of prostaglandin
synthesis, and central nervous system desensitization of peripheral nociceptors.
Pharmacodynamics/Kinetics
Absorption: Oral: Rapid and complete
Onset of Action: ~30 to 60 minutes
Duration of Action: ~4 hours
Distribution: 4-methyl-amino-antipyrine (MAA): IV: 33.5 L; Oral: 1.19 L/kg (Levy, 1995)
Protein binding: 4-methyl-amino-antipyrine (MAA): 58%; 4-amino-antipyrine (AA): 48%; 4-formyl-amino-antipyrine (FAA): 18%; 4-acetylamino-antipyrine (AAA): 14%
Metabolism: Dipyrone is metabolized via nonenzymatic hydrolysis to its main active moiety, 4-methyl-amino-antipyrine (MAA). MAA is
subsequently demethylated to the active 4-amino-antipyrine (AA) metabolite and either directly or via AA to 4-formyl-amino-antipyrine
(FAA). AA is metabolized via acetylation to 4-acetyl-amino-antipyrine (AAA) (Levy, 1995)
Bioavailability: MAA (active metabolite): IM: 87% (Levy, 1995); Oral: 85% to 89%
Half-life elimination: IV: Dipyrone: 14 minutes; Oral: MAA (active metabolite): 3 hours; AA: 4 hours; FAA: 11 hours; AAA: 9 hours
Time to peak: Single dose:
IV: AA: ~3 to 5 hours; FAA: ~7 to 8 hours; AAA: ~13 to 17 hours
IM: MAA: ~2 hours; AA: ~5 hours; FAA: ~11 hours; AAA: ~18 hours
Oral: ~1 to 2 hours; AA: ~3 to 7 hours; FAA: ~6 to 9 hours; AAA: ~10 to 18 hours (Levy, 1995)
Excretion: Urine (~96%); feces (~6%)
Related Information
Beers Criteria Potentially Inappropriate Medications for Geriatrics
Index Terms
References
Dipirona; Dipirona sodica; Metamizol sodico; Metamizole; Metamizole sodium; Methampyrone ; Sulpyrine
References
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Levy M, Sylber-Katz e, Rosenkranz B. Clinical pharmacokinetics of dipyrone and its metabolites. Clinical Pharmacokinetics.
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