Butadion (Ointment) Instructions for Use

ATC Code

M02AA01 (Phenylbutazone)

Active Substance

Phenylbutazone (Rec.INN registered by WHO)

Clinical-Pharmacological Group

NSAIDs for external use

Pharmacotherapeutic Group

Drugs for external use for pain syndrome in diseases of the musculoskeletal system. Non-steroidal anti-inflammatory drugs for external use

Pharmacological Action

NSAID from the group of pyrazolone derivatives. It has anti-inflammatory, analgesic, and antipyretic effects, due to the inhibition of COX activity and a decrease in prostaglandin synthesis. It exhibits a uricosuric effect.

When applied topically, it causes a reduction or disappearance of joint pain at rest and during movement. It reduces morning stiffness and joint swelling, and helps to increase the range of motion.

Pharmacokinetics

When taken orally, it has a high degree of absorption; bioavailability is 85-90% and decreases with long-term use. C_max is reached in 1-2 hours. Plasma protein binding is more than 95%. It is metabolized in the liver to form two main metabolites. T_1/2 is 18-24 hours. It is excreted by the kidneys 70% (5% unchanged), 30% through the intestines in the form of metabolites. It is excreted in significant amounts in breast milk.

With topical application, the systemic absorption of phenylbutazone is no more than 5%.

Indications

For oral administration: for symptomatic therapy of inflammatory and degenerative diseases of the musculoskeletal system; for pain syndrome – bursitis, tenosynovitis, arthralgia, myalgia, neuralgia, dental and headache (including migraine), algodysmenorrhea, pain from injuries, burns.

For topical application: post-traumatic inflammation of soft tissues and joints (for example, resulting from sprains, strains, and contusions); rheumatic diseases of soft tissues (tenosynovitis, bursitis, lesions of periarticular tissues), muscle pain of rheumatic and non-rheumatic origin; pain syndrome and swelling associated with diseases of muscles and joints; rheumatoid arthritis, osteoarthritis, radiculitis, lumbago, sciatica.

ICD codes

Dosage Regimen

Apply the ointment externally only. Use exclusively on intact skin.

Apply a thin layer of ointment to the affected area. Use a strip approximately 2-3 cm long for each application.

Do not rub the ointment in vigorously. Apply gently without massage.

Use the ointment 2-3 times per day. Maintain regular intervals between applications.

The standard treatment course is 7-10 days. Do not exceed a 10-day course of continuous treatment without medical supervision.

Consult a physician if symptoms persist after 10 days of use. Do not extend treatment without professional advice.

For adults and children over 14 years of age, apply as directed. This product is not intended for use in children under 14 years of age.

In elderly patients, use the standard application regimen. No specific dosage adjustment is required for this population.

Avoid contact with eyes, mucous membranes, and open wounds. Do not apply to skin with broken integrity.

Do not use under occlusive dressings. Allow the application site to remain uncovered.

Wash hands thoroughly after each application, unless the hands are the treated area.

Discontinue use immediately and consult a physician if signs of local skin reaction appear, such as itching, redness, swelling, or rash.

Adverse Reactions

From the digestive system: dyspepsia, NSAID-gastropathy, abdominal pain, nausea, vomiting, heartburn, diarrhea or constipation; with long-term use in high doses – ulceration of the gastrointestinal mucosa, aphthous stomatitis, glossitis, erosive esophagitis, bleeding (gastrointestinal, gingival, hemorrhoidal), impaired liver function.

From the cardiovascular system: increased blood pressure, heart failure, tachycardia.

From the nervous system: headache, dizziness, drowsiness, depression, agitation.

From the organ of hearing: hearing loss, tinnitus.

From the hematopoietic system: agranulocytosis, leukopenia, anemia, thrombocytopenia.

Allergic reactions: skin rash, itching, urticaria, bronchospasm, edematous syndrome, angioedema.

Other: increased sweating, uterine bleeding.

With topical application: allergic reactions, eczema, photosensitivity, contact dermatitis (itching, redness, swelling of the treated skin area; papules, vesicles, peeling).

Contraindications

For oral administration: hypersensitivity to pyrazolone derivatives; complete or incomplete combination of bronchial asthma, recurrent nasal and sinus polyposis and intolerance to acetylsalicylic acid or other NSAIDs (including in history); erosive and ulcerative lesions of the gastrointestinal tract in the acute stage (gastric and duodenal ulcer, ulcerative colitis, peptic ulcer), bone marrow depression, decompensated chronic heart failure or cardiopulmonary failure, severe hepatic and/or renal failure (creatinine clearance less than 30 ml/min), period after coronary artery bypass surgery; progressive kidney disease, active liver disease, confirmed hyperkalemia, pregnancy (III trimester), active gastrointestinal bleeding, inflammatory bowel disease; children under 12 years of age.

With caution

Hyperbilirubinemia, bronchial asthma, chronic heart failure, edema, arterial hypertension, hemophilia, hypocoagulation, hepatic insufficiency, chronic renal failure, hearing loss, vestibular pathology, blood diseases, diabetes mellitus, systemic lupus erythematosus, polymyalgia rheumatica, transient arteritis, ulcerogenic diseases of the gastrointestinal tract, stomatitis, coronary artery disease, cerebrovascular diseases, dyslipidemia/hyperlipidemia, peripheral arterial diseases, smoking, creatinine clearance less than 60 ml/min, history of ulcerative lesions of the gastrointestinal tract, presence of Helicobacter pylori infection, elderly age, long-term use of NSAIDs, alcoholism, severe somatic diseases, simultaneous use of oral glucocorticosteroids (including prednisolone), anticoagulants (including warfarin), antiplatelet agents (including acetylsalicylic acid, clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline); I-II trimesters of pregnancy, lactation period.

For topical application: hypersensitivity to pyrazolone derivatives; history of bronchial asthma attacks, other allergic reactions (such as rhinorrhea, urticaria) after taking acetylsalicylic acid or another NSAID; application to the skin around the eyes, to mucous membranes, open wounds or fractures, impaired skin integrity at the intended application site; use under an occlusive dressing; treatment of deep vein thrombosis; pregnancy (I and III trimesters), breastfeeding period; children under 14 years of age; simultaneous use with other drugs containing Phenylbutazone.

Use in Pregnancy and Lactation

Oral administration is contraindicated in the third trimester of pregnancy and topical application is contraindicated in the first and third trimesters of pregnancy. Use in the second trimester of pregnancy is possible only in cases where the intended benefit to the mother outweighs the potential risk to the fetus. Contraindicated for use during lactation (breastfeeding).

Use in Hepatic Impairment

For oral administration, contraindications are active liver diseases, severe hepatic insufficiency. It should be prescribed with caution to elderly patients with hepatic insufficiency.

Use in Renal Impairment

For oral administration, contraindications are severe renal failure (creatinine clearance less than 30 ml/min), progressive kidney diseases. It should be prescribed with caution to elderly patients with chronic renal failure.

Pediatric Use

Use in children is possible according to indications, in age-appropriate recommended doses and dosage forms. It is necessary to strictly follow the instructions in the phenylbutazone drug leaflets regarding contraindications for the use of specific phenylbutazone dosage forms in children of different ages.

Geriatric Use

It should be used with caution in elderly patients.

Special Precautions

When taking phenylbutazone orally, monitoring of the peripheral blood picture and functional state of the liver and kidneys is necessary during treatment.

When taking phenylbutazone orally, if it is necessary to determine 17-ketosteroids, Phenylbutazone should be discontinued 48 hours before the study.

When taking phenylbutazone orally, to reduce the risk of adverse events from the gastrointestinal tract, the minimum effective dose should be used for the shortest possible course.

Effect on ability to drive vehicles and operate machinery

During treatment, one should refrain from engaging in potentially hazardous activities that require increased attention and speed of mental and motor reactions.

Drug Interactions

With simultaneous use with phenylbutazone, the effect of indirect anticoagulants, antiplatelet agents, fibrinolytics is enhanced, as well as the side effects of glucocorticosteroids and mineralocorticoids, estrogens, morphine, para-aminosalicylic acid, penicillin, and the hypoglycemic effect of sulfonylurea derivatives.

With simultaneous use with phenylbutazone, the effectiveness of uricosuric, antihypertensive drugs and diuretics is reduced.

With simultaneous use with phenylbutazone, the concentration of lithium and methotrexate in the blood increases.

With simultaneous use of phenylbutazone and inducers of microsomal oxidation in the liver (phenytoin, ethanol, barbiturates, rifampicin, tricyclic antidepressants), the production of hydroxylated active metabolites of phenylbutazone increases.

With simultaneous use of antacids and cholestyramine, the absorption of phenylbutazone is reduced.

With simultaneous use with phenylbutazone, myelotoxic drugs enhance the manifestations of the hematotoxicity of phenylbutazone.

Storage Conditions

Store at 2°C (36°F) to 15°C (59°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Over-the-Counter

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.