Rastocin
Rastocin Uses, Dosage, Side Effects, Food Interaction and all others data.
Rastocin is a cytotoxic anthracycline antibiotic. The cytotoxic action results from its binding to DNA and inhibition of nucleic acid synthesis. Rastocin has been shown to produce regression in a variety of disseminated malignancies.
Rastocin 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. Rastocin is widely used for the treatment of several solid tumors while daunorubicin and idarubicin are used exclusively for the treatment of leukemia. Rastocin may also inhibit polymerase activity, affect regulation of gene expression, and produce free radical damage to DNA. Rastocin possesses an antitumor effect against a wide spectrum of tumors, either grafted or spontaneous. The anthracyclines are cell cycle-nonspecific.
| Trade Name | Rastocin |
| 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 | Lithuania, Russia |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Rastocin 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.
Rastocin 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 Rastocin works
Rastocin has antimitotic and cytotoxic activity through a number of proposed mechanisms of action: Rastocin 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
Rastocin dosage
Administer Rastocin 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
Rastocin 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.
Rastocin 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
Rastocin 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 Rastocin
Rastocin contains Doxorubicin see full prescribing information from innovator Rastocin Monograph, Rastocin MSDS, Rastocin FDA label
FAQ
What is Rastocin used for?
Rastocin 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 Rastocin?
Rastocin effects help patients achieve lengthy and good quality of life remission and survival times for many types of malignancies. Although Rastocin 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 Rastocin?
Rastocin has antimitotic and cytotoxic activity through a number of proposed mechanisms of action: Rastocin 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 Rastocin?
Common side effects of Rastocin 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 Rastocin safe during pregnancy?
Cyclophosphamide and Rastocin are pregnancy category D agents; however, potential benefits may warrant treatment with these agents during pregnancy under special circumstances.
Is Rastocin safe during breastfeeding?
Most sources consider breastfeeding to be contraindicated during maternal antineoplastic Rastocin therapy, especially anthracyclines such as Rastocin.
Can I drink alcohol with Rastocin?
The drinking of alcohol does not appear to affect the safety or usefulness of pegylated liposomal Rastocin.
How often do I take Rastocin?
Rastocin is usually given once every 21 to 28 days.
How long does Rastocin take to work?
Rastocin 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 Rastocin treatment?
You usually have liposomal Rastocin every 2 to 4 weeks. Your treatment plan will depend on the type of cancer you have.
What is the half life of Rastocin?
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 Rastocin 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 Rastocin?
You should not use Rastocin 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 Rastocin 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 Rastocin affect my fertility?
We know that certain chemotherapy medicines are more likely than others to cause infertility, including Rastocin.
Can Rastocin affects my heart?
Rastocin is well recognized that Rastocin may cause damage to the heart in some individuals.
Can Rastocin affect my kidneys?
Researches have shown that Rastocin chemotherapy could generate severe tissue injury in heart and kidney and the symptoms of renal damage like hematuresis and proteinuria are especially evident.
Can Rastocin affects my liver?
While hepatotoxicity from Rastocin, epirubicin or idarubicin may be rare, it is likely due to direct toxic injury to the liver. Rastocin 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 Rastocin?
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
