doxorubicin liposomal

Action and Spectrum

Actions and Spectrum 

Action: 

doxorubicin liposomal is a medication that falls under the class of anthracycline antibiotics. It is primarily used in cancer treatment, particularly for solid tumors and hematological malignancies. The drug works by inhibiting the replication of cancer cells and inducing their death through multiple mechanisms. 

The main action of this drug involves intercalating DNA strands, which means it inserts itself between the DNA base pairs, disrupting the DNA structure and preventing proper replication and transcription processes within the cancer cells. This leads to DNA damage and inhibition of DNA and RNA synthesis, ultimately impeding cancer cell proliferation. 

Spectrum:  

The drug exhibits a broad spectrum of activity against various types of cancers. Some of the cancers for which doxorubicin liposomal is commonly used include: 

Breast cancer: The drug is often utilized as part of a combination chemotherapy regimen for both early-stage and advanced breast cancer. 

Ovarian cancer: It may be employed in the treatment of advanced ovarian cancer, either alone or in combination with other chemotherapeutic agents. 

Lung cancer: The drug can be utilized in the management of certain types of lung cancers. 

Sarcomas: It is effective against various types of sarcomas, including soft tissue sarcomas and osteosarcoma. 

Drug Interaction

Adverse Reaction

Frequency defined  

>10% 

(Kaposi’s Sarcoma) 

Thrombocytopenia (>50%) 

Anemia (18.2%) 

Anemia (>50%) 

Nausea (17%)  

Neutropenia (10-50%)  

(Ovarian cancer >25%) 

Nausea (46%) 

Vomiting (32.6%) 

Constipation (>25%) 

Rash (28%) 

Asthenia (40.2%) 

Stomatitis (41%) 

Hand-foot syndrome (50%) 

Abdominal pain (>25%)  

(Ovarian cancer 10-25%) 

Diarrhea (20%) 

Fever (21.3%) 

Anorexia (20%) 

Pharyngitis 

Alopecia 

Dyspepsia 

Dyspnea 

Peripheral edema  

1-10% 

(Kaposi’s Sarcoma 5-10%) 

Increased alkaline phosphatase 

Fever (9.1%) 

Vomiting (7.8%) 

Rash (1-5%) 

Stomatitis (6.8%) 

Alopecia (1-5%) 

Asthenia (9.9%) 

Diarrhea (7.8%)  

(Kaposi’s Sarcoma 1-5%) 

Hypotension 

Dyspnea 

Rash 

Tachycardia 

Hemolysis 

Hand-foot syndrome (3.4%) 

Ovarian cancer (selected) 

Thrombocytopenia (1.3%) 

Anemia (0.4-5.4%) 

Neutropenia (13.3%) 

<1% 

Ketosis 

Acute myeloid leukemia 

Abscess 

Hyperuricemia 

Erythema nodosum 

Cardiomyopathy 

Cardiomegaly 

Hyperkalemia 

Black Box Warning

Black Box Warning:  

Myocardial toxicity 

Infusion-related reactions 

Contraindication / Caution

Contraindication/Caution:  

Hypersensitivity: Individuals with a known hypersensitivity or severe allergic reaction to doxorubicin or any of the ingredients in the liposomal formulation should not receive doxorubicin liposomal. 

Severe myocardial insufficiency: Patients with severe heart failure or other significant heart problems, such as a history of myocardial infarction (heart attack). 

Severe hepatic impairment: Patients with severe liver impairment or dysfunction should be cautious when considering doxorubicin liposomal, as it is primarily metabolized by the liver. 

Severe renal impairment: Individuals with severe kidney impairment or renal dysfunction should use this drug with caution, as the drug may be excreted through the kidneys. 

Recent vaccination: Administration of live vaccines is not recommended in patients receiving this drug due to potential immunosuppressive effects of the drug. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: AU TGA pregnancy category: D
US FDA pregnancy category: Not assigned 

Lactation: Excreted into human milk is unknown 

Pregnancy Categories:         

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

Category B: There were a lack of studies on pregnant women and no evidence of risk to the fetus in animal experiments.   

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.   

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology:  

The drug, also known as liposomal doxorubicin, is a chemotherapeutic agent used in the treatment of various types of cancer. It is a liposome-encapsulated formulation of doxorubicin, a widely used anticancer drug. 

Pharmacodynamics:  

The drug exerts its antitumor effects through multiple mechanisms. The primary mode of action is the inhibition of DNA and RNA synthesis by intercalating into the DNA helix and preventing the synthesis of nucleic acids. doxorubicin also inhibits the activity of topoisomerase II, an enzyme involved in DNA replication and repair. By interfering with these processes, doxorubicin liposomal disrupts the growth and proliferation of cancer cells.   

Pharmacokinetics: 

Absorption 

The drug is typically given intravenously. The liposomes containing doxorubicin circulate in the bloodstream, and the drug is released gradually over time. The encapsulation in liposomes can alter the absorption characteristics compared to the conventional doxorubicin formulation. 

Distribution 

The drug distributes throughout the body via the bloodstream. The liposomes can accumulate in tumor tissues ,which allows for increased drug concentrations at the tumor site. The distribution of liposomal doxorubicin can also occur in normal tissues, although the liposomal formulation may reduce the drug’s distribution in certain organs, such as the heart, compared to conventional doxorubicin.  

Metabolism 

Once the drug is released from the liposomes, it undergoes metabolism in the body. drug is primarily metabolized in the liver by various enzymes, including cytochrome P450 enzymes, into an active metabolite called doxorubicinol. This metabolite can contribute to the drug’s therapeutic and toxic effects.  

Excretion and elimination 

The elimination of doxorubicin and its metabolites primarily occurs through bile and feces. Only a small portion of the drug is excreted unchanged in urine. The liposomal formulation does not significantly affect the excretion pathway compared to conventional doxorubicin. 

Adminstartion

Administration:  

Infusion: The drug is administered as an IV infusion. The liposomes containing the medication are slowly injected into a vein over a specific duration, usually ranging from 30 minutes to 90 minutes. The exact infusion time may vary depending on the specific protocol recommended by the prescribing healthcare provider. 

Pre-medication: Prior to the administration of this drug , patients may receive pre-medication to help manage potential side effects. This may include medications such as corticosteroids or antihistamines to reduce the risk of infusion-related reactions. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: doxorubicin liposomal 

Why do we use doxorubicin liposomal?  

Breast cancer: The drug is often used in the treatment of metastatic breast cancer in patients who have failed previous therapies.  

Ovarian cancer: It can be used as a component of combination chemotherapy for advanced ovarian cancer, typically in combination with other drugs such as paclitaxel. 

Lung cancer: The medication has potential applications in managing specific forms of lung cancer, including small cell lung cancer and advanced non-small cell lung cancer. 

Kaposi’s sarcoma: The drug is used as a treatment option for this condition. 

Soft tissue sarcoma: Soft tissue sarcomas are occasionally treated with the utilization of this medication, which are cancers that develop in the soft tissues of the body, such as muscles, fat, nerves, or blood vessels. 

Multiple myeloma: It can be used in the treatment of multiple myeloma.