1. Disclaimer
The information provided in this report is intended for educational and professional reference purposes only and does not replace medical judgment, diagnosis, or treatment. Healthcare professionals should consult official prescribing information and local regulatory approvals before clinical use.
We do not guarantee the accuracy, currency or completeness of information regarding medications or medical products, and official sources should be verified before making any decisions. By using this blog, you agree to assume personal responsibility for relying on the information provided.
2. Summary
Octomotol® is a non-steroidal anti-inflammatory drug (NSAID) containing bumadizone calcium, a pyrazolone derivative historically used for inflammatory, traumatic, and rheumatic conditions. While it demonstrated peripheral analgesic, anti-inflammatory, and anti-exudative effects, bumadizone has been withdrawn or restricted in many countries due to safety concerns, particularly serious hematological adverse reactions. Its current use is limited to a small number of regional markets, and it is considered obsolete compared with modern NSAIDs.
3. Brand Name
Octomotol®
4. Category
- Therapeutic Class: Non-Steroidal Anti-Inflammatory Drug (NSAID)
- Pharmacological Class: Pyrazolone derivative
- Therapeutic Effects: Analgesic, anti-inflammatory, anti-exudative
5. Active Ingredient
Bumadizone Calcium (as calcium semihydrate)
6. Pharmaceutical Form & Strength
- Pharmaceutical Form: Coated tablets
- Strength: Each tablet contains bumadizone calcium semihydrate equivalent to 110 mg
7. Manufacturer & Marketing Authorization Holder
October Pharma S.A.E.
6th of October City, Egypt
Note: The product is not approved by major international regulatory authorities such as the FDA or EMA.
8. Mechanism of Action
Bumadizone exerts its pharmacological effects primarily through non-selective inhibition of cyclooxygenase (COX) enzymes, leading to decreased synthesis of prostaglandins involved in pain, inflammation, and vascular permeability.
Its activity is predominantly peripheral, reducing inflammatory exudation, edema, and nociceptor sensitization.
Important scientific note: Bumadizone is metabolized into phenylbutazone and oxyphenbutazone, compounds associated with serious toxicity. This metabolic pathway is a key factor in its unfavorable safety profile.
9. Spectrum of Activity
- Anti-inflammatory
- Analgesic (peripheral)
- Anti-exudative
There is no clinically relevant antimicrobial activity, and antipyretic activity is not consistently documented in reliable sources.
10. Pharmacokinetics
Available pharmacokinetic data are limited and largely historical.
- Absorption: Rapid absorption following oral administration
- Distribution: Systemic distribution with accumulation at inflammatory sites
- Metabolism: Predominantly hepatic, producing phenylbutazone-related metabolites
- Elimination: Mainly renal excretion of metabolites
Precise parameters such as bioavailability, half-life, and clearance are not well defined in modern literature.
11. Indications
Historical indications (now largely obsolete):
- Acute and chronic inflammatory rheumatic disorders (arthrosis, spondylosis, extra-articular rheumatism)
- Post-traumatic inflammation (contusions, sprains, fractures, dislocations, hematomas)
- Post-surgical and post-radiotherapy inflammatory swelling
- Certain ENT inflammatory conditions
- Gynecological inflammatory disorders
- Ophthalmic inflammatory conditions (e.g., iridocyclitis, keratitis)
Current clinical guidelines favor safer alternatives.
12. Administration
- Route: Oral
- Tablets should be taken during or immediately after meals to minimize gastrointestinal irritation
- Use should occur only under medical supervision
13. Method of Preparation
Not applicable. Octomotol® is supplied as a ready-to-use oral tablet.
14. Contraindications
- Hypersensitivity to bumadizone, phenylbutazone, or other pyrazolone derivatives
- History of blood dyscrasias (e.g., leukopenia, agranulocytosis)
- Active or previous gastrointestinal ulceration or bleeding
- Hemorrhagic diathesis
- Severe hepatic, renal, or cardiac impairment
- Pregnancy
- Children under 6 years of age
15. Warnings & Precautions
- Serious hematological reactions, including agranulocytosis and aplastic anemia, have been reported
- Long-term use requires regular complete blood count (CBC) monitoring
- Use the lowest effective dose for the shortest possible duration
- Increased risk of gastrointestinal bleeding and fluid retention
- Use with extreme caution in elderly patients and those with cardiovascular risk factors
16. Drug Interactions
- Oral anticoagulants: Increased bleeding risk
- Oral antidiabetic agents: Potentiation of hypoglycemic effect
- Other NSAIDs or corticosteroids: Increased risk of gastrointestinal toxicity
- Lithium and methotrexate: Potential for increased toxicity
Concurrent use generally requires avoidance or close monitoring.
17. Side Effects
Common:
- Gastrointestinal discomfort, nausea, dyspepsia
- Skin rash or hypersensitivity reactions
- Fluid retention and edema
Serious:
- Hematological toxicity (leukopenia, agranulocytosis, aplastic anemia)
- Gastrointestinal bleeding or ulceration
- Renal or hepatic impairment
Any serious adverse reaction warrants immediate discontinuation and medical evaluation.
18. Use in Special Populations
- Pregnancy: Contraindicated
- Lactation: Safety not established; use not recommended
- Pediatrics: Contraindicated under 6 years
- Elderly: High-risk group; avoid if possible
19. Storage Conditions
- Store below 30°C
- Keep in a dry place
- Protect from moisture
- Keep out of reach of children
20. Additional Sections
Regulatory and Clinical Status
Bumadizone has been withdrawn or severely restricted in many countries due to safety concerns, particularly hematological toxicity. Its continued availability is limited to certain regional markets and is not supported by contemporary evidence-based guidelines.
21. Frequently Asked Questions (FAQ)
Is Octomotol® a modern NSAID?
No. It is an older NSAID with a safety profile inferior to currently available alternatives.
Why is its use discouraged today?
Because of the risk of severe hematological adverse effects and the availability of safer NSAIDs.
Can it be used long term?
Long-term use is strongly discouraged and requires strict medical supervision and blood monitoring.
22. References
- Manufacturer’s product documentation (October Pharma)
- WHO: Consolidated List of Products Withdrawn or Restricted
- PubChem & NCBI chemical and pharmacological data on bumadizone
- Peer-reviewed historical NSAID literature
