Analgin ExtraCap, 500 mg capsules 10 pcs

Analgesic non-narcotic.
It has analgesic, antipyretic and mild anti-inflammatory effects, it is a derivative of pyrazolone.

Pharmacokinetics:

Indications

Severe acute or chronic pain syndrome in trauma and post-operative pain syndrome, colic, cancer and other conditions where other therapeutic measures are contraindicated.

Fever resistant to other therapies.

Active ingredient

Composition

How to take, the dosage

The dose depends on the severity of the pain or fever and on individual sensitivity to analgesics.

The capsules should be swallowed whole with plenty of fluid (e.g., a glass of water).

The lowest effective dose should be used initially.

The potency of the drug usually reaches its maximum effect 30-60 minutes after oral administration.

The single dose for adults and adolescents over 15 years of age (body weight >53 kg) is 500-1000 mg (1-2 capsules). In case of insufficient effect a single dose may be taken up to 4 times a day. Maximum daily dose is 4000 mg (8 capsules). The duration of use is not more than 5 days as an analgesic and not more than 3 days as antipyretic.

Elderly patients

Elderly patients need to reduce the dose because they may have reduced excretion of sodium metabolites of sodium metamizole.

Severe general condition and impaired creatinine clearance

Patients with severe general condition and impaired creatinine clearance need to reduce the dose because their excretion of sodium metabolites of metamizole may be reduced.

Renal or hepatic impairment

Because patients with impaired renal or hepatic function have slower excretion rates, multiple high doses should be avoided. No dose reduction is required with short-term use. There is no experience with long-term use.

Interaction

With cyclosporine

Sodium metamizole may cause decreased plasma concentrations of cyclosporine; therefore, cyclosporine concentrations should be monitored when using them concomitantly.

With chlorpromazine

Severe hypothermia may occur with concomitant use of sodium metamizole and chlorpromazine.

With methotrexate

The concomitant use of sodium methamisole and methotrexate or other myelotoxic agents may increase the hematotoxicity of the latter, especially in elderly patients. Therefore, this combination should be avoided.

With other non-narcotic analgesic agents

Simultaneous use of sodium metamizole with other non-narcotic analgesic agents may lead to mutually reinforcing toxic effects.

With tricyclic antidepressants, oral contraceptives, allopurinol

Tricyclic antidepressants, oral contraceptives, allopurinol impair metabolism of sodium metamizole in the liver and increase its toxicity.

With barbiturates, phenylbutazone and other inducers of microsomal liver enzymes

With sedatives and tranquilizers

Sedatives and tranquilizers increase the analgesic effect of metamizole sodium.

With drugs with high plasma protein binding (oral hypoglycemic agents, indirect anticoagulants, glucocorticosteroids and indomethacin)

With drugs that have high plasma protein binding (oral hypoglycemic agents, indirect anticoagulants, glucocorticosteroids and indomethacin)br> Sodium metamizole, displacing oral hypoglycemic agents, indirect anticoagulants, glucocorticosteroids and indomethacin, increases their activity.

With thymazole

Thymazole increases the risk of leukopenia.

With codeine, H2-histamine receptor blockers and propranololol

Codeine, H2-histamine receptor blockers and propranololol increase the effects of sodium metamizole.

With acetylsalicylic acid (ASA)

With bupropion

Sodium metamizole may decrease the concentration of bupropion in blood, which should be taken into account when using them simultaneously.

With other medicinal products

It is well known that pyrazolone derivatives may interact with indirect anticoagulants, captopril, lithium and triamterene, and may also affect the effectiveness of hypotensive agents and diuretics. Drug interaction of sodium metamizole with these drugs has not yet been studied. Because of the increased risk of anaphylactic/anaphylactoid reactions during treatment with sodium metamizole should not use X-ray contrast agents, colloidal blood substitutes and penicillin.

Special Instructions

Patients who experience anaphylactic or other immune-mediated reactions (e.g., agranulocytosis) in response to the use of sodium metamizole are also at risk of developing them in response to the use of other pyrazolones and pyrazolidines.

Agranulocytosis

If signs of agranulocytosis or thrombocytopenia appear (see section “Side effects”), the drug should be discontinued immediately and a general blood count (with determination of the leukocyte formula) performed. Discontinuation of therapy should not be postponed until the results of laboratory tests are obtained.

Pancytopenia

In case of pancytopenia the drug should be discontinued immediately and the CBC should be monitored until the blood count returns to normal (see section “Adverse effects”). All patients should be advised to seek immediate medical attention if signs and symptoms resembling blood disorders occur during treatment (e.g., general weakness, infections, persistent fever, bruising, bleeding, pallor).

Anaphylactic/anaphylactoid reactions

In susceptible patients, anaphylactic shock may occur, so special caution should be exercised in patients with bronchial asthma or atopy.

Serious skin reactions

Life-threatening skin reactions have been described with sodium metamizole: Stevens-Johnson syndrome (SSD) and toxic epidermal necrolysis (TEN). If signs of SDS or TEN appear (such as a progressive skin rash often accompanied by blisters or mucosal ulceration), treatment with methamisole should be stopped immediately and never resumed. Patients should be informed about the signs and symptoms of these diseases. Skin reactions should be carefully monitored in them, especially during the first weeks of treatment.

Isolated hypotensive reactions

Abdominal pain

The drug should not be used for acute abdominal pain (until the cause is known).

Perhaps renal or hepatic impairment

In the recommended dose range, no effect on concentration and rapid psychomotor reactions has been established. When taking high doses, caution is recommended for driving vehicles, operating machinery and engaging in other potentially hazardous activities requiring increased concentration and rapid psychomotor reactions.

Contraindications

– Hypersensitivity to sodium metamisole and other pyrazolone derivatives and to pyrazolidines such as phenylbutazone (including patients with agranulocytosis due to these drugs) or other drug components;

– Disorder of medullary hematopoiesis (for example, after cytostatic therapy) or diseases of the hematopoietic organs;

– Hereditary deficiency of glucose-6-phosphate dehydrogenase (hemolysis);

– Acute intermittent hepatic porphyria (risk of porphyria attacks);

– Pregnancy and breastfeeding period;

– Childhood under 15 years.

– Arterial hypotension (systolic blood pressure below 100 mmHg.), decreased circulating blood volume, hemodynamic instability (myocardial infarction, multiple trauma, incipient shock), incipient heart failure, high fever (increased risk of rapid decrease in blood pressure).

– Diseases in which a significant decrease in blood pressure may have an increased risk (patients with severe coronary heart disease and cerebral artery stenosis).

– Chronic alcohol abuse.

– Bronchial asthma, especially in combination with concomitant polyposis rhinosinusitis; chronic urticaria and other types of atopy (allergic diseases in the development of which a significant role belongs to genetic predisposition to sensitization: pollinosis, allergic rhinitis, etc.) (increased risk of anaphylactic/anaphylactoid reactions).

– Alcohol intolerance (reaction to even small amounts of certain alcoholic beverages with symptoms such as itching, lacrimation, and pronounced redness of the face) (increased risk of anaphylactic/anaphylactoid reactions).

– Intolerance to dyes (e.g., tartrazine) or preservatives (e.g., benzoates) (increased risk of anaphylactic/anaphylactoid reactions).

– Severe hepatic and renal dysfunction (low doses are recommended due to possible delayed excretion of sodium metamizole).

If you have any of the above diseases/conditions, always consult your doctor before taking the drug.

Side effects

Unwanted reactions are classified as follows according to the WHO (World Health Organization) classification: very common (≥1/10), common (≥1/100 to <1/10), infrequent (≥1/1000 to <1/100), rare (≥1/10000 to <1/1000), very rare (to <1/ 10000) and frequency unknown (cannot be estimated based on available data).

Cardiac disorders

Frequency unknown: Coneys syndrome (allergic coronary syndrome, manifested by clinical and laboratory signs of angina pectoris caused by inflammatory mediators).

Immune system disorders

Rare: anaphylactic/anaphylactoid reactions.

Very rare: analgesic bronchial asthma.

Prevalence unknown: anaphylactic shock.

Sodium metamizole can cause anaphylactic or anaphylactoid reactions, which in very rare cases can be severe and life-threatening. They can occur even if the drug has previously been taken many times without any complications.

Such drug reactions may develop immediately or several hours after taking sodium metamizole, usually within one hour.

In milder cases they manifest as skin and mucous membrane symptoms (itching, burning, hyperemia, urticaria, edema) or as shortness of breath, or gastrointestinal complaints. In severe cases, these reactions develop into generalized urticaria, severe angioedema (especially involving the larynx), severe bronchospasm, cardiac arrhythmias, a sharp decrease in blood pressure (sometimes preceded by an increase in blood pressure) and the development of circulatory shock. In individuals with analgesic bronchial asthma syndrome with intolerance to analgesic drugs, these reactions manifest as bronchial asthma attacks.

Skin and subcutaneous tissue disorders

Infrequent: fixed drug dermatitis.

Rarely: skin rash.

Prevalence unknown: Stevens-Johnson syndrome, Lyell syndrome (toxic epidermal necrolysis).

Disorders of the croca and lymphatic system

Rarely: leukopenia.

Very rare: agranulocytosis, including cases with fatal outcome and thrombocytopenia.

Prevalence unknown: aplastic anemia, pancytopenia, including fatal cases.

These reactions are immunological in nature. They can occur even if the drug has previously been taken many times without any complications.

The typical symptoms of agranulocytosis are lesions of the mucous membranes (horn and pharynx, anorectal area and genitalia), sore throat, and fever. However, when antibiotics are used, these phenomena may be mild. Sometimes, but not always, there is a slight increase in lymph nodes or spleen.

The sedimentation rate of erythrocytes is significantly increased, the granulocyte content is sharply reduced or they are not detected. As a rule, hemoglobin, erythrocyte and platelet counts remain normal, but abnormalities may occur. Typical symptoms of thrombocytopenia are an increased tendency to bleed and the occurrence of petechiae on the skin and mucous membranes.

If there is a sudden worsening of the general condition, if fever persists, or if new or painful ulcers appear on mucous membranes, particularly in the mouth, nose, or throat, the treatment strategy is to discontinue the drug immediately, without waiting for laboratory results.

If pancytopenia develops, the drug should be discontinued and the blood count should be monitored until the blood count returns to normal (see Special Precautions).

Vascular disorders

Infrequent: isolated arterial hypotension.

After taking the drug, an isolated transient decrease in blood pressure may occur (possibly pharmacologically conditioned and not accompanied by other manifestations of anaphylactic/anaphylactoid reactions); in rare cases, the decrease in blood pressure may be very pronounced. In fever, a dose-dependent sharp decrease in blood pressure without other signs of a hypersensitivity reaction is also possible.

Remorbidities of the urinary tract

Very rarely: impairment of renal function.

Prevalence unknown: interstitial nephritis.

In very rare cases, patients with impaired renal function may have acute deterioration of renal function (acute renal failure), in some cases with oliguria, anuria or proteinuria.

General disorders

Infrequent: possible staining of urine red due to the presence of the metabolite rubazonic acid in the urine.

Overdose

Do not exceed the recommended dose and duration of use!

Symptoms

. Acute overdose is manifested by nausea, vomiting, abdominal pain, impaired renal function/acute renal failure (e.g., as a manifestation of interstitial nephritis) and, rarely, symptoms of the central nervous system (dizziness, drowsiness, coma, seizures) and decreased blood pressure leading to tachycardia and shock, abnormal heart rhythm (tachycardia), hypothermia, shortness of breath, acute agranulocytosis, hemorrhagic syndrome, respiratory muscle paralysis.

In high overdose, excretion of rubazonic acid may stain the urine red.

Treatment

The treatment of overdose, as well as the prevention of serious complications, may require general and special intensive medical supervision and treatment.

Pregnancy use

The use in pregnancy and during breastfeeding is contraindicated.

Pregnancy

Sodium metamizole penetrates the placental barrier. There are limited data on the use of sodium metamizole during pregnancy. According to the results of preclinical studies, teratogenic effects of sodium metamizole in rats and rabbits were not found, in high doses fetotoxicity was observed.

Since there are no adequate data on use in humans, sodium metamizole should not be taken in the first trimester of pregnancy, in the second trimester of pregnancy sodium metamizole can be used only if the expected benefits to the mother exceed the potential risk to the fetus.

Despite the fact that sodium metamizole weakly inhibits prostaglandin synthesis, the possibility of premature (intrauterine) closure of the arterial (Botalus) duct as well as perinatal complications due to impaired platelet aggregation in the mother or the newborn cannot be excluded. Therefore, sodium metamizole is contraindicated in the third trimester of pregnancy.

Lactation period

The metabolites of sodium metamizole penetrate into breast milk, so breastfeeding should be stopped when using the drug and for 48 hours after the last dose.

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