Optalgin

/ Teva

The dose should be reduced in elderly patients as well as inpatients with reduced general condition or limited creatinine clearance, since the excretion of the metabolic products of dipyrone may be retarded. Currently there is no sufficient information regarding the long term administration of dipyrone in patients with seriously impaired liver and kidney function
Duration of Treatment: The duration of administration depends on thenature and severity of the medical condition.
Adults and Adolescents from 15 Years Old (over 53 kg body weight) Optalgin Caplets/Tablets:
1-2 caplets or 1-2 tablets up to 4 times daily.
Do not exceed 8 caplets or 8 tablets daily.
Depending on the maximum daily dose, the single dose can be taken in intervals of 6 to 8 hours.
The caplets/tablets should be taken with sufficient liquid. (e.g a glass of water).
Optalgin Drops: The oral drops are taken with a little bit of water. Adults and adolescents From 15 years (over 53 kg) 25-50 drops up to 3 times daily.
Infants and Children: For all age groups except babies, 8-16 mg of dipyrone per kg body weight can be administered as a single dose. The table below shows the recommended single dose and the maximum daily dose as a function of body weight or age.
For full details see prescribing information.

Relief of moderate to severe pain.

Known hypersensitivity to dipyrone or to pyrazolone and pyrazolidine derivatives (e.g.: to medicines containing dipyrone, propyphenazone, phenazone or phenylbutazone) or to any other ingredient of the preparation.
Pregnancy and breastfeeding. Acute hepatic porphyria. Genetic deficiency of the enzyme glucose-6-phosphate dehydrogenase (G6PD). In case of impaired bone marrow function (e.g., following a treatment with cytostatics) or disorders of the hematopoietic system, as well as history of blood dyscrasias or acute bone marrow suppression. In patients with a body weight less than 5 kg.
Warnings: Rare cases of hypersensitivity reactions have been reported; they are manifested by life-threatening risk of circulatory shock or agranulocytosis-due to the pyrazolone derivative dipyrone (metamizole).
Patients that show anaphylactoid reactions to dipyrone are especially prone to react similarly to other non-narcotic analgesics.
Patients that show anaphylactic or other immunologically mediated reactions (e.g. agranulocytosis) to dipyrone are also especially prone to react similarly to other pyrazolones and pyrazolidines.
The appearance of symptoms indicative of agranulocytosis, such as high fever, pain in throat, buccal ulceration, tiredness, and weakness, warrants immediate discontinuation of the drug, and an urgent blood count determination.
Although the risk of shock syndrome is much greater with parenteral dipyrone, this possibility cannot be ruled out with the enteral use of dipyrone. Careful monitoring is warranted in patients with high fever.
As with other pyrazolone derivatives, cutaneous allergic reactions may appear such as urticaria and maculopapular eruption. Exceptionally, they may be severe enough and manifested by epidermal necrolysis (Stevens-Johnson syndrome or Lyell’s syndrome), in which case immediate discontinuation of treatmenf is imperative. In case of symptoms of an agranulocytosis or thrombocytopenia, dipyrone must immediately be discontinued even before the results of the laboratory diagnostic tests become available.
For full details see prescribing information.

Careful inquiry should be made concerning previous hypersensitivity reactions of the patients to drugs and food.
Red coloration may appear in urine with acid pH; it may be due to an exceedingly small quantity of a metabolite (rubazonic acid).
Caution should be exercised when dipyrone is used in patients with hepatic or renal disorders.

The main side effects of dipyrone are hypersensitivity reactions. The most important reactions are circulatory and agranulocytosis. These reactions occur rarely or very rarely but are life-threatening. They can occur even if dipyrone has been formerly used without any complications.
Immune System Disorders: In rare occasions, anaphylactoid or anaphylactic reactions can occur that only very rarely turn out severe and life-threatening. Such reactions to medicines can develop during injection or immediately after administration, but also many hours later. However, they mostly occur within the first hour after administration.
Minor reactions typically appear inform of skin and mucous membrane reactions (such as itching, burning, redness, urticaria, swellings), dyspnea and – less frequently – gastrointestinal complalnts (such as nausea, dyspepsia, vomiting). These minor reactions can develop into severe forms with generalized urticaria, severe angioedemas (also in the larynx region), severe bronchospasm, cardiac arrhythmias, drop in blood pressure (sometimes preceded by a rise in blood pressure) and circulatory shock. In patients with analgesics-asthma-syndrome, intolerance reactions typically appear in form of asthma attacks. At the first signs of a state of shock such as cold sweat, vertigo, dizziness, skin discoloration, feeling of constriction in the heart region, the appropriate immediate actions must be taken.

Dipyrone/ Chlorpromazine: Concurrent use of dipyrone and chlorpromazine may cause severe hypothermia; therefore combined therapy with these two drugs should be avoided.
Dipyrone/Cyclosporin: Dipyrone may cause a reduction in cyclosporin blood levels, by an unknown mechanism. A higher dose of cyclosporin may be required.
Dipyrone/ Alcohol: Concurrent administration is not recommended in patients who react to small quantities of alcoholic beverages (flush, lacrimation and sneezing), since these patients may be more prone to allergic reactions to dipyrone.
Dipyrone/Anticoagulants: Because of possible thrombocytopenia appearing as an adverse reaction of dipyrone, caution is required when dipyrone is administered to patients on anticoagulant therapy.
Oral Anticoagulants/ Pyrazolones/ Captopril/ Lithium/ Methotrexate/ Triamterine/ Anihypertensives/Diuretics: The substance class of pyrazolones is known to cause interactions with oral anticoagulants, captopril, lithium, methotrexate and triamterene as well as to alter the effectiveness of antihypertensives and diuretics. To what extent dipyrone causes these interactions too, is yet unknown.

See Contraindications.

Symptoms: In connection with acute overdose, nausea, vomiting, abdominal pains, impaired kidney function/acute kidney failure (e.g. with signs of an interstitial nephritis) and — more rarely — central nervous symptoms (vertigo, somnolence, coma, spasms) and a drop in blood pressure up to a shock and tachycardia were observed. After administration of very high doses, the excretion of rubazonic acid may cause a red discoloration of the urine.
Therapeutic measures: No specific antidote is known for dipyrone. If dipyrone was only recently administered, it can be tried to limit the absorption in the body by means of absorption reducing measures (e.g. activated carbon). The main metabolite (4-N-methylaminoantipyrine) can be eliminated by means of hemodialysis, hemofiltration, hemoperfuision or plasma filtration. The treatment of the intoxication as well as the prevention of severe complications, may require general and special intensive medical monitoring and treatment.
Treatment of Severe Anaphytactic Reactions (Shock): Emergency measures according to the current guidelines must be initiated.