| Parameters | Description |
|---|---|
| Category of Drug | Doxorubicin is part of the anthracycline group of chemotherapeutic agents. |
| Mechanism of Action (1) | Doxorubicin causes the breakage of DNA strands and inhibits both DNA and RNA synthesis. Doxorubicin inhibits the enzyme topoisomerase II, causing DNA damage and induction of apoptosis. When combined with iron, doxorubicin also causes free radical-mediated oxidative damage to DNA, further limiting DNA synthesis. Iron chelators, such as dexrazoxane, may prevent free radical formation by limiting doxorubicin binding with iron. |
| Indications | Doxorubicin is used for 1. Soft tissue and bone sarcomas 2. Acute leukemia 3. Malignant lymphoma (3) 4. Hodgkin’s disease 5. Non-Hodgkin’s disease 6. Breast carcinoma (2) 7. Small-cell carcinoma of lungs 8. AIDS-related Kaposi’s sarcoma 9. Multiple myeloma 10. Gastrointestinal tract carcinoma 11. Bladder cancer (4) |
| Structure |  |
| Molecular details | Weight: 543.5193 Chemical Formula- C27H29NO11 |
| Pharmacokinetic properties | 1. Absorption- NA 2. Vd- = 809 to 1214 L/m2 3. Protein binding- 74-76% bound to plasma protein. 4. Metabolism- half of the dose is eliminated from the body unchanged. 5. Route of elimination- 40% of the dose appears in the bile in 5 days. 6. Half-life- 20 – 48 hours. |
| Well Known Pharmaceutical Brands | Doxorubicin is the most widely used anthracycline antibiotic. 1. LIPODOX- SUN 2. ADRIM- FRESENIUS KABI 3. DOXORUBIN- KHANDELWAL 4. ADRIAMYCIN- PFIZER 5. PEGADRIA- INTAS PHARMA |
| Available dosage forms | 1. INJECTION 2. LIPOSOMAL  |
| Dose | Intravenous 50-75 mg/m2 body surface area by slow IV injection every 3 weeks. |
| Contraindications | 1. Known hypersensitivity 2. Cardiac disease 3. Pregnancy 4. Lactation 5. Neonates |
| Precautions | 1. Avoid extravasation 2. Monitor ECG changes 3. Arrhythmias 4. Blood counts 5. Hypotension or congestive heart failure 6. Hepatic impairment 7. Interactions |
| Adverse Effects | 1. Infusion reactions 2. Cardiotoxicity 3. Bone marrow suppression 4. Liver impairment 5. Nausea and voming 6. Reversible alopecia 7. Stomatitis 8. Conjunctivitis 9. Keratitis 10. Mucositis 11. Discolouration of body fluids 12. local skin reactions |
| Pregnancy Category | D |
