Доксорубицин
Доксорубицин Uses, Dosage, Side Effects, Food Interaction and all others data.
Доксорубицин is a cytotoxic anthracycline antibiotic. The cytotoxic action results from its binding to DNA and inhibition of nucleic acid synthesis. Доксорубицин has been shown to produce regression in a variety of disseminated malignancies.
Доксорубицин is an antineoplastic in the anthracycline class. General properties of drugs in this class include: interaction with DNA in a variety of different ways including intercalation (squeezing between the base pairs), DNA strand breakage and inhibition with the enzyme topoisomerase II. Most of these compounds have been isolated from natural sources and antibiotics. However, they lack the specificity of the antimicrobial antibiotics and thus produce significant toxicity. The anthracyclines are among the most important antitumor drugs available. Доксорубицин is widely used for the treatment of several solid tumors while daunorubicin and idarubicin are used exclusively for the treatment of leukemia. Доксорубицин may also inhibit polymerase activity, affect regulation of gene expression, and produce free radical damage to DNA. Доксорубицин possesses an antitumor effect against a wide spectrum of tumors, either grafted or spontaneous. The anthracyclines are cell cycle-nonspecific.
Trade Name | Доксорубицин |
Availability | Prescription only |
Generic | Doxorubicin |
Doxorubicin Other Names | 14-hydroxydaunomycin, 14-hydroxydaunorubicine, Doxorubicin, Doxorubicina, Doxorubicine, Doxorubicinum, Hydroxydaunorubicin |
Related Drugs | prednisone, methotrexate, dexamethasone, Keytruda, Armour Thyroid, Arimidex, rituximab, carboplatin, pembrolizumab, fluorouracil |
Type | |
Formula | C27H29NO11 |
Weight | Average: 543.5193 Monoisotopic: 543.174060775 |
Protein binding | Doxorubicin and its major metabolite, doxorubicinol, is 74-76% bound to plasma protein. The extent to binding is independent of plasma concentration up to 1.1 mcg/mL. Doxorubicin does not cross the blood brain barrier. |
Groups | Approved, Investigational |
Therapeutic Class | Cytotoxic Chemotherapy |
Manufacturer | |
Available Country | Russia, Ukraine |
Last Updated: | September 19, 2023 at 7:00 am |
![Доксорубицин Доксорубицин](https://www.medicinesfaq.com/media/png/ru-doxorubicin.png)
Uses
Доксорубицин is an anthracycline topoisomerase II inhibitor used for:
- Ovarian cancer: After failure of platinum-based chemotherapy.
- AIDS-related Kaposi’s Sarcoma: After failure of prior systemic chemotherapy or intolerance to such therapy.
- Multiple Myeloma: In combination with bortezomib in patients who have not previously received bortezomib and have received at least one prior therapy.
Доксорубицин is also used to associated treatment for these conditions: Acute Lymphoblastic Leukaemias (ALL), Acute Myeloblastic Leukemia, Advanced Endometrial Cancer, Advanced Soft Tissue Sarcoma, Bladder transitional cell carcinoma, Carcinoma, Bronchogenic, Gastric Carcinoma, Kaposi's Sarcoma AIDS Related, Lymphoma, Hodgkins, Malignant Lymphomas, Metastatic Breast Cancer, Multiple Myeloma (MM), Mycosis Fungoides (MF), Neuroblastomas, Ovarian Cancer Metastatic, Ovarian Carcinoma, Sarcoma, Bone, Sezary Syndrome, Soft Tissue Sarcoma (STS), Thyroid Carcinoma, Waldenström's Macroglobulinemia (WM), Wilms' tumor, Advanced Thymoma, Advanced uterine sarcoma
How Доксорубицин works
Доксорубицин has antimitotic and cytotoxic activity through a number of proposed mechanisms of action: Доксорубицин forms complexes with DNA by intercalation between base pairs, and it inhibits topoisomerase II activity by stabilizing the DNA-topoisomerase II complex, preventing the religation portion of the ligation-religation reaction that topoisomerase II catalyzes.
Dosage
Доксорубицин dosage
Administer Доксорубицин at an initial rate of 1 mg/min to minimize the risk of infusion reactions. If no infusion related reactions occur, increase rate of infusion to complete administration over 1 hour. Do not administer as bolus injection or undiluted solution.
- Ovarian cancer: 50 mg/m2 IV every 4 weeks
- AIDS-related Kaposi’s Sarcoma: 20 mg/m2 IV every 3 weeks
- Multiple Myeloma: 30 mg/m2 IV on day 4 following bortezomib
Side Effects
Leucopenia, thrombocytopenia, nausea, vomiting, diarrhoea. Rarely facial flushing, rash, alopecia. Blurred vision, headache, seizures, paraesthesia, confusion, malaise, lethargy, skin pigmentation.
Toxicity
LD50=21800 ug/kg (rat, subcutaneous)
Precaution
Elderly, children, hepatic impairment. Monitor blood counts and ECG.
Interaction
Доксорубицин interacts with a number of other drugs e.g. antibiotics (aminoglycosides), steroids, aminophylline and propranolol.
Food Interaction
- Avoid St. John's Wort. This herb induces CYP3A4 metabolism, which may reduce the serum concentration of doxorubicin.
- Exercise caution with grapefruit products. Grapefruit inhibits CYP3A4 metabolism, which may increase the serum concentration of doxorubicin.
Доксорубицин Drug Interaction
Moderate: aprepitant, aprepitant, pegfilgrastim, pegfilgrastim, ondansetron, ondansetronMinor: sulfamethoxazole / trimethoprim, sulfamethoxazole / trimethoprim, cyclophosphamide, cyclophosphamideUnknown: lorazepam, lorazepam, diphenhydramine, diphenhydramine, loratadine, loratadine, cyanocobalamin, cyanocobalamin, cholecalciferol, cholecalciferol
Доксорубицин Disease Interaction
Major: infections, cardiomyopathy, hepatic dysfunction, myelosuppression
Volume of Distribution
The distributive half-life is 5 minutes, which suggests that doxorubicin is rapidly taken up by tissue. Steady state volume of distribution = 809 to 1214 L/m2
Half Life
Terminal half life = 20 - 48 hours.
Clearance
- 324-809 mL/min/m2 [by metabolism and biliary excretion]
- 1088 mL/min/m2 [Men]
- 433 mL/min/m2 [Women]
- 1540 mL/min/m2 [children greater than 2 years of age receiving administration of 10 to 75 mg/m2 doses]
- 813 mL/min/m2 [infants younger than 2 years of age receiving administration of 10 to 75 mg/m2 doses]
Elimination Route
40% of the dose appears in bile in 5 days. 5-12% of the drug and its metabolites appears in urine during the same time period. <3% of the dose recovered in urine was doxorubicinol.
Pregnancy & Breastfeeding use
Category D: There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).
Contraindication
Cardiac disease, neonates, pregnancy and lactation, prior irradiation to mediastinum. IM/SC admin. Severe myelosuppression due to previous treatment with antitumour agents or radiotherapy.
Special Warning
Hepatic Impairment-
serum-bilirubin: 12-30 mcg/ml: Half the normal dose;
serum-bilirubin: >30 mcg/ml: Quarter of the usual dose.
Acute Overdose
Acute overdosage may increase the toxic effects of mucositis, leukopenia and thrombocytopenia. Treatment includes hospitalisation of the severely myelosuppressed patient, antimicrobials, platelet transfusions and symptomatic treatment of mucositis. Use of haemopoietic growth factor (G-CSF, GM-CSF) may be considered. Cumulative dosage increases risk of cardiomyopathy and resultant congestive heart failure which may be managed with digitalis preparations, diuretics, and after load reducers such as ACE inhibitors.
Storage Condition
Powder for injection: Store at 15-30°C.
Solution for injection & liposomal formulations: Refrigerate at 2-8°C. Do not freeze.
Innovators Monograph
You find simplified version here Доксорубицин
Доксорубицин contains Doxorubicin see full prescribing information from innovator Доксорубицин Monograph, Доксорубицин MSDS, Доксорубицин FDA label
FAQ
What is Доксорубицин used for?
Доксорубицин is used in combination with other medications to treat certain types of bladder, breast, lung, stomach, and ovarian cancer; Hodgkin's lymphoma (Hodgkin's disease) and non-Hodgkin's lymphoma (cancer that begins in the cells of the immune system); and certain types of leukemia (cancer of the white blood cells). It is often used together with other chemotherapy agents.
How safe is Доксорубицин?
Доксорубицин effects help patients achieve lengthy and good quality of life remission and survival times for many types of malignancies. Although Доксорубицин poses significant risks in administration and toxicity, it is one of the most effective chemotherapeutic agents in veterinary medicine.
What is the mechanism of action of Доксорубицин?
Доксорубицин has antimitotic and cytotoxic activity through a number of proposed mechanisms of action: Доксорубицин forms complexes with DNA by intercalation between base pairs, and it inhibits topoisomerase II activity by stabilizing the DNA-topoisomerase II complex, preventing the religation portion of the ligation-religation reaction that topoisomerase II catalyzes.
What are the common side effects of Доксорубицин?
Common side effects of Доксорубицин are include:
- Atazanavir
- Boceprevir
- Cobicistat
- Lopinavir
- Measles Virus Vaccine, Live
- Mumps Virus Vaccine, Live
- Nelfinavir
- Rotavirus Vaccine, Live
- Rubella Virus Vaccine, Live
- Saquinavir
- Tasonermin
- Telaprevir
- Varicella Virus Vaccine, Live
- Zoster Vaccine, Live
Is Доксорубицин safe during pregnancy?
Cyclophosphamide and Доксорубицин are pregnancy category D agents; however, potential benefits may warrant treatment with these agents during pregnancy under special circumstances.
Is Доксорубицин safe during breastfeeding?
Most sources consider breastfeeding to be contraindicated during maternal antineoplastic Доксорубицин therapy, especially anthracyclines such as Доксорубицин.
Can I drink alcohol with Доксорубицин?
The drinking of alcohol does not appear to affect the safety or usefulness of pegylated liposomal Доксорубицин.
How often do I take Доксорубицин?
Доксорубицин is usually given once every 21 to 28 days.
How long does Доксорубицин take to work?
Доксорубицин is a light red liquid that you have through a drip (infusion) into your bloodstream. It usually takes between 30 to 90 minutes each time you have it.
How long is Доксорубицин treatment?
You usually have liposomal Доксорубицин every 2 to 4 weeks. Your treatment plan will depend on the type of cancer you have.
What is the half life of Доксорубицин?
The initial distribution half-life of approximately 5 minutes suggests rapid tissue uptake of doxorubicin, while its slow elimination from tissues is reflected by a terminal half-life of 20 to 48 hours.
What happens if I miss a dose?
Call your doctor for instructions if you miss an appointment for your Доксорубицин injection.
What happens if I overdose?
Since this medication is given by a healthcare professional in a medical setting, an overdose is unlikely to occur.
Who should not take Доксорубицин?
You should not use Доксорубицин if you have severe liver disease, severe heart problems, very low blood cell counts caused by prior chemotherapy, or if you recently had a heart attack. You should not use this medicine if you are allergic to Доксорубицин or similar medications or if you have:
very low blood cell counts caused by chemotherapy you received in the past; severe liver disease; severe heart problems; or if you have recently had a heart attack.
Will Доксорубицин affect my fertility?
We know that certain chemotherapy medicines are more likely than others to cause infertility, including Доксорубицин.
Can Доксорубицин affects my heart?
Доксорубицин is well recognized that Доксорубицин may cause damage to the heart in some individuals.
Can Доксорубицин affect my kidneys?
Researches have shown that Доксорубицин chemotherapy could generate severe tissue injury in heart and kidney and the symptoms of renal damage like hematuresis and proteinuria are especially evident.
Can Доксорубицин affects my liver?
While hepatotoxicity from Доксорубицин, epirubicin or idarubicin may be rare, it is likely due to direct toxic injury to the liver. Доксорубицин and its analogues are metabolized in the liver via microsomal enzymes, and production of a toxic or immunogenic intermediate may trigger liver injury.
What happen If I stop taking Доксорубицин?
If you decide to stop chemotherapy, be sure you're still getting relief from symptoms such as pain, constipation, and nausea. This is called palliative care, and it's meant to improve your quality of life