Optalgin Injection

/ Teva

Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.
Adults and Adolescents Over 14 Years of Age: Intravenous Administration as an Analgesic: 1 g (2 ml), administered by slow injection, up to 4 times daily. In severe pain, 2.5 g (5 ml) may be administered twice daily (the maximum daily dosage is 5 g).
Intravenous administration of dipyrone should be carried out slowly over a period of at least 5 minutes, followed by a clinical reasonable observation.
Intramuscular administration of dipyrone for relief of pain is not recommended. However, if medical circumstances require such administration, all due
precautions should be exercised to permit reasonable clinical observation.
Intramuscular Administration as an Antipyretic: 2.5 g (5 ml), to be repeated only if deemed necessary.
Infants and Children: Use of dipyrone is contraindicated in infants under 3 months of age or 5 kg/body weight.
In infants 3-12 months, Optalgin Injection must be administered by the intramuscular route only. In older children, the injection may be administered by either the intramuscular or intravenous routes. For full details see prescribing information.
Elderly patients: The dose should be reduced in elderly patients, as excretion of metabolic products of Optalgin® Teva 1g/2ml solution for injection may be delayed.
Cases of poor general health and impaired creatinine clearance: The dose should be reduced in patients in poor general health or with impaired creatinine clearance, as excretion of metabolic products of Optalgin® Teva 1g/2ml solution for injection may be delayed.
Impaired renal or hepatic function: As the elimination rate is reduced in the case of impaired renal or hepatic function, repeated high doses should be avoided. If use is only short-term, no dose reduction is necessary. There are no clinical data from long-term use.
Duration of administration: The duration of administration depends on the nature and severity of the disorder. In the case of prolonged treatment with dipyrone, regular blood counts, including differential blood count, are necessary.

As an Analgesic: Optalgin® Teva 1g/2ml solution for injection, by intravenous administration, is indicated for the relief of severe and acute pain when oral treatment is not feasible or suitable, as in post-traumatic or postsurgical pain, biliary or renal colic, and pain associated with malignant diseases.
As an Antipyretic: Optalgin® Teva 1g/2ml solution for injection, by intramuscular administration, is indicated to lower temperature in life-threatening situations, when this cannot be achieved by other means.
Hyperthermic patients in critical condition may also be treated in a non-hospital environment, under close medical supervision.

* Hypersensitivity to the active substance or to other pyrazolones or pyrazolidines or to any of the excipients
* Agranulocytosis in the medical history induced by dipyrone, other pyrazolones or pyrazolidines.
* Known analgesic asthma syndrome or known urticaria/angio-oedema type intolerance of analgesics.
* Disturbances of bone marrow function.
* Acute intermittent hepatic porphyria.
* Existing hypotension and unstable circulatory situation.
* Newborn babies and infants under 3 months of age or weighing less than 5 kg, as no scientific data are available on the safety of it use.
* Infants (aged 3 months to 1 year) with regard to intravenous injection.

This medical product is associated with the rare but life-threatening risk of shock and agranulocytosis. Patients who display an anaphylactic or other immunologically mediated reaction (e.g.agranulocytosis) to dipyrone are also at particular risk of reacting in the same way to other pyrazolones and pyrazolidines. Patients who display an anaphylactic or other immunologically mediated reaction to other pyrazolones, pyrazolidines or other non-narcotic analgesics are also at high risk of having such a
reaction to dipyrone
Thrombocytopenia
Appearance of thrombocytopenia, with signs such as an increased bleeding tendency and petechiae on the skin and mucosae, the use of dipyrone must be stopped
immediately and the blood count (including differential count) checked.
Pancytopenia
Appearance of pancytopenia, the use of dipyrone must be stopped immediately and the full blood count monitored until it normalizes.
Anaphylactic/Anaphylactoid reactions
parenteral administration of dipyrone is associated with a higher risk of anaphylactic or anaphylactoid reactions.
The risk of potentially serious anaphylactoid reactions to dipyrone is distinctly higher in patients with:
* analgesic asthma syndrome or urticaria/angio-oedema type intolerance of analgesics
* bronchial asthma, especially if accompanied by rhinosinusitis and nasal polyps,
* chronic urticaria.
* intolerance of dyes (e.g. tartrazine) and preservatives (e.g. benzoates).
* alcohol intolerance. Such patients react even to small quantities of alcoholic drinks with symptoms such as sneezing, eye watering and pronounced facial reddening. An alcohol intolerance of this kind can be a sign of a previously undiagnosed analgesic asthma syndrome
Severe skin reactions
Severe cutaneous adverse reactions (SCARs), including Stevens-Johnson syndrome (SJS), toxic epidermal necrolysis (TEN) and drug reaction with eosinophilia and systemic symptoms (DRESS), which can be life-threatening, or fatal, have been reported in connection with dipyrone therapy.
If signs and symptoms suggestive of these reactions occur, dipyrone should be discontinued immediately and dipyrone must not be resumed at any stage.
Hypotensive reactions
Dipyrone can trigger hypotensive reactions These reactions are possibly dosedependent.
They are more likely in the case of parenteral than with enteral administration. The risk of such reactions is also higher in:
* Too rapid intravenous injection
* Pre-existing hypotension, volume depletion or dehydration, unstable circulation or incipient circulatory failure (e.g. patients with myocardial infarction or multiple
injuries)
* High fever
Drug-induced liver damage
Cases of acute hepatitis with a predominantly hepatocellular pattern occurring within a few days to a few months of the start of treatment have been reported in patients treated with dipyrone. The signs and symptoms include raised serum levels of liver enzymes with or without jaundice, often in association with other drug hypersensitivity reactions (e.g., rash, blood count abnormalities, fever and
eosinophilia) or accompanied by features of autoimmune hepatitis. Most patients recovered after the discontinuation of dipyrone treatment. In isolated cases, however, progression to acute liver failure with the need for liver transplantation has been reported.
See prescribing information for full details.

See prescribing information for full details.

Dipyrone can cause a decrease in the plasma ciclosporin level. The latter must therefore be monitored if Optalgin® Teva 1g/2ml solution for injection is co-administered.
If dipyrone and chlorpromazine are co-administered, severe hypothermia can occur.
The concomitant administration of dipyrone with methotrexate can potentiate the haematotoxicity of methotrexate, especially in elderly patients. This combination should therefore be avoided.
Dipyrone, if co-administered, can reduce the effect of aspirin on platelet aggregation. Dipyrone should therefore be used with caution in patients who are
taking low-dose aspirin for cardioprotection.
Plasma bupropion levels can be reduced by dipyrone. Therefore caution is indicated for the coadministration of dipyrone and bupropion.
It is known of the pyrazolone substance class that interactions can occur with oral anticoagulants, captopril, lithium and triamterene, as well as changes in the efficacy of antihypertensives and diuretics.
It is not known to what extent dipyrone has these interactions.
Posible interaction between dipyrone and diagnostics marketed by Teva Medical (Beckman):
1. Enzymatic Creatinine
2. Cholesterol
3. Triglyceride
4. Uric acid
5. Lactase
6. Lipase.
The possible interaction is significantly lower results than the real values in patients treated by dipyrone prior to undergoing the above testing. In case any of those tests have to be performed, dypirone has to be administered after the testing.

Pregnancy: There are insufficient data for the use of dipyrone in pregnant women. Dipyrone crosses the placenta. Dipyrone did not show any teratogenic effects in animal studies.
As sufficient data for humans are not available, dipyrone should be used during pregnancy only after a rigorous risk-benefit assessment by a doctor.
Although dipyrone is only a weak inhibitor of prostaglandin synthesis, the possibility of premature closure of the ductus arteriosus (Botallo’s duct) and of
perinatal complications resulting from a reduction in foetal and maternal platelet aggregability cannot be ruled out. The use of dipyrone in the third trimester (after week 28) should be limited to cases which do not respond to the use of paracetamol and used at the lowest effective dose.
Lactation: Dipyrone metabolites are excreted in breast milk. The use of dipyrone should be limited to cases which do not respond to the use of paracetamol or ibuprofen.

Symptoms: Nausea, vomiting, abdominal pain, impairment of kidney function/acute kidney injury (e.g., in the form of interstitial nephritis) and – more rarely – central-nervous symptoms (dizziness, drowsiness, coma, convulsions) and hypotension, even shock and tachycardia, have been observed in the context of acute overdose.
After very high doses, the excretion of rubazonic acid can cause red discoloration of the urine.
Treatment: There is no known specific antidote to dipyrone. The main metabolite (4-N-methylaminoantipyrine) can be eliminated by haemodialysis, haemofiltration, haemoperfusion or plasma filtration.
Treatment of intoxication, like the prevention of serious complications, can require general and specialist intensive care monitoring and treatment.
Emergency treatment of serious hypersensitivity reactions (shock): At the first signs (e.g., skin reactions such as urticaria and flushing, agitation, headache, sweating, nausea), stop the injection. Leave the cannula in the vein, or create a venous access. In addition to standard emergency measures such as the head-down position, keeping the airways clear, and administering oxygen, the administration of sympathomimetics, volume replacement or glucocorticoids may be necessary.