Rubilem

Rubilem Uses, Dosage, Side Effects, Food Interaction and all others data.

Rubilem forms a stable complex with DNA and interferes with the nucleic acid synthesis. It is a cell-cycle nonspecific agent, but its cytotoxic effects are mostly marked in the S-phase. It also has immunosuppressant and antibacterial effects.

Rubilem 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. Doxorubicin is widely used for the treatment of several solid tumors while daunorubicin and idarubicin are used exclusively for the treatment of leukemia. Rubilem may also inhibit polymerase activity, affect regulation of gene expression, and produce free radical damage to DNA. Rubilem possesses an antitumor effect against a wide spectrum of tumors, either grafted or spontaneous. The anthracyclines are cell cycle-nonspecific.

Trade Name Rubilem
Availability Prescription only
Generic Daunorubicin
Daunorubicin Other Names Acetyladriamycin, Daunomycin, Daunorubicin, Daunorubicina, Daunorubicine, Daunorubicinum, Leukaemomycin C, Rubidomycin
Related Drugs Venclexta, prednisone, methotrexate, cyclophosphamide, Deltasone, vincristine, venetoclax, Cytoxan, azacitidine, cytarabine
Weight 20mg
Type Injection
Formula C27H29NO10
Weight Average: 527.5199
Monoisotopic: 527.179146153
Protein binding

97% binding-albumin

Groups Approved
Therapeutic Class Cytotoxic Chemotherapy
Manufacturer Scharper Pharmaceuticals (pvt) Ltd,
Available Country Pakistan
Last Updated: September 19, 2023 at 7:00 am
Rubilem
Rubilem

Uses

Rubilem in combination with other approved anticancer drugs is used for remission induction in acute nonlymphocytic leukemia (myelogenous, monocytic, erythroid) of adults and for remission induction in acute lymphocytic leukemia of children and adults.

Rubilem is also used to associated treatment for these conditions: Acute Lymphocytic Leukemia (ALL), Acute Myeloid Leukemia (AML), Acute Myeloid Leukemia With Myelodysplasia-Related Changes, Acute erythroid leukemia, Acute monocytic leukaemia, Newly diagnosed Therapy-Related Acute Myeloid Leukemia

How Rubilem works

Rubilem has antimitotic and cytotoxic activity through a number of proposed mechanisms of action: Rubilem 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

Rubilem dosage

Intravenous-

Acute leukaemias:

  • Adult:30-45 mg/m2BSA daily on days 1-3 of the induction course and days 1 and 2 for the subsequent courses. Admin as a solution in 0.9% sodium chloride into a fast-running infusion of sodium chloride or glucose. May repeat course 3-6 wk later. Max (total cumulative dose): 550 mg/m2in patients without risk factors for cardiotoxicity and 400 mg/m2in patients who have received chest radiotherapy.
  • Child:For acute lymphoblastic leukaemia: 25 mg/m2BSA once wkly in combination with other regimens. <2 yr old or BSA <0.5 m2: 1 mg/kg once wkly. Max (total cumulative dose): 300 mg/m2and in children <2 yr: 10 mg/kg.

AIDS-related Kaposi's sarcoma:

  • Adult:As the liposomal formulation: Initially, 40 mg/m2once every 2 wk, diluted in glucose 5% to a concentration of 0.2-1 mg/ml and given over 30-60 minutes. May continue for as long as disease control can be maintained.

Side Effects

GI disturbances; stomatitis; alopoecia and dermatological reactions. Extravasation of daunorubicin may cause severe local tissue necrosis damaging surrounding muscles, tendons and nerves. IV infusion, back pain, flushing and chest tightness.

Toxicity

LD50=20 mg/kg (mice, IV); LD50=13 mg/kg (rat, IV)

Precaution

Regular blood count and ECG monitoring; elderly, children. Hepatic or renal impairment may increase risk of toxicity. Pre-existing cardiac disease and previous treatment with doxorubicin. Myocardial toxicity leading to potentially fatal congestive heart failure may occur during therapy or mth to yr after therapy cessation. Incidence of myocardial toxicity increases after total cumulative dose exceeds 400-550 mg/m2in adults, 300 mg/m2 in children >2 yr, or 10 mg/kg in children <2 yr. Risk of severe myelosuppression leading to infection or haemorrhage.

Interaction

Increased risk of cardiotoxicity when used with cyclophosphamide. Increased risk of hepatic toxicity when used with hepatotoxic drugs e.g. high-dose methotrexate.

Food Interaction

No interactions found.

Half Life

18.5 hours

Elimination Route

Twenty-five percent of an administered dose of daunorubicin hydrochloride is eliminated in an active form by urinary excretion and an estimated 40% by biliary excretion.

Pregnancy & Breastfeeding use

Pregnancy 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

Heart failure. Pregnancy, lactation.

Special Warning

Renal Impairment: Based on serum-creatinine concentrations: 105-265 micromoles/l: 75% of the usual dose; >265 micromoles/l: 50% of the usual dose.

Hepatic Impairment: Based on serum bilirubin concentrations of 12-30 mcg/ml: 75% of the usual dose; >30 mcg/ml: 50% of the usual dose.

Acute Overdose

Severe myelosupression, cardiotoxicity with or without transient reversible ECG changes leading to CHF. Treatment is supportive and symptomatic.

Storage Condition

Powder for inj: Store at 15-25° C. Solution for inj & liposomal inj: Refrigerate at 2-8° C. Do not freeze.

Innovators Monograph

You find simplified version here Rubilem

Rubilem contains Daunorubicin see full prescribing information from innovator Rubilem Monograph, Rubilem MSDS, Rubilem FDA label

*** Taking medicines without doctor's advice can cause long-term problems.
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