Carboplatin

Carboplatin is an antitumor drug that contains platinum and has an alkylating effect on the DNA of malignant neoplasms.

The medicinal effect develops by forming cross-links inside the DNA spirals of the neoplasm cells, as a result of which the DNA structure itself changes. This leads to the suppression of nucleic acid replication, and then the complete destruction of tumor cells that are malignant.

Indications Carboplatin

It is used in case of the following disorders:

• germ cell neoplasms affecting the testicles or ovaries;
• ovarian carcinoma;
• seminoma;
• malignant tumors in the head or neck area;
• pulmonary carcinoma;
• malignant melanoma;
• carcinoma of the uterine body and cervix;
• osteogenic sarcoma;
• bladder carcinoma.

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Release form

The drug is released in the form of a concentrate for infusions, in vials with a capacity of 5, 15, and also 45 or 75 ml.

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Pharmacokinetics

Metabolic processes associated with carboplatin are realized by hydrolysis; in this case, active bonds are formed that interact with the DNA of neoplasms. The distribution volume indicators are equal to 16 liters.

Intraplasmic synthesis with protein is quite weak, but irreversible platinum bonds formed from a combination of carboplatin and plasma proteins have a slow elimination with the shortest half-life equal to 5 days.

The half-life of carboplatin at the initial stage is 65-120 minutes, and at the final stage - 280-350 minutes. Through the kidneys (with CC values of at least 60 ml per minute) 71% of the drug is excreted in 24 hours.

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Dosing and administration

The antitumor drug is prescribed both for monotherapy and in combination with other medications with a similar type of effect (for example, complex treatment with the introduction of Carboplatin and paclitaxel).

Taking into account the location and size of the neoplasm, vials of the drug with a capacity of 0.45 g/45 ml or other volumes are used. Intravenous use is prescribed via infusion (drip), over a period of 15-60 minutes. It is used in the following portions:

• 0.1 g/m2 ^of medication, daily for 5 days;
• 0.3-0.4 g/m2 ^LS, once a month.

The intervals between infusions in the case of a neutrophil ratio of 1500/mm2 ^or higher, and a platelet ratio of 100,000/mm2 ^or higher, should be at least 1 month.

Before and after using the medication, there is no need to perform forced diuresis or administer additional fluids to the patient.

In case of hematological toxicity (moderate or severe) with neutrophil count below 500/mm2 ^and platelet count below 50,000/mm2 ^, a 25% dose reduction may be required.

During kidney disease (CC level below 60 ml per minute), the likelihood of developing toxic activity of Carboplatin increases, which is why its doses are reduced, taking into account the CC values (16-40/0.2 g, as well as CC 41-59/0.25 l/m2 ⁾.

Elderly people (over 65 years of age), and also those who have previously undergone myelosuppressive therapy, require a 20-25% reduction in dosage.

Before administering the medication, it is necessary to carefully examine it to detect the possible presence of foreign particles and discoloration of the liquid.

The medicine should be diluted in 5% glucose or 9% NaCl so that its concentration is 0.5-1 mg/ml. The drug is administered immediately after preparation; the prepared liquid can be stored for no more than 24 hours.

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Use Carboplatin during pregnancy

The tests performed revealed the development of teratogenic, mutagenic and embryotoxic effects of the drug, which is why it is not used during pregnancy.

Carboplatin should also not be prescribed during breastfeeding, as it may have a toxic effect on the infant.

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Contraindications

Main contraindications:

• severe renal disease (CC values below 15 ml per minute);
• severe intolerance associated with carboplatin and other platinum-containing medications;
• significant blood loss that has occurred recently;
• intense myelosuppression.

Caution is required when using in the following disorders:

• hearing disorders;
• depressed hematopoiesis within the bone marrow (this includes conditions observed after radiation or chemotherapy);
• problems with kidney function;
• use in combination with nephrotoxic drugs (for example, cisplatin);
• recent vaccination;
• fungal, bacterial or viral infections in the active phase.

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Side effects Carboplatin

Main side effects:

• digestive disorders: diarrhea, abdominal pain, stomatitis, vomiting, constipation, loss of appetite, nausea and liver dysfunction (increased AST activity with alkaline phosphatase and increased serum bilirubin levels);
• disorders of hematopoiesis: suppression of hematopoiesis within the bone marrow;
• problems with the functioning of the nervous system: tinnitus, visual or hearing impairment, cumulative neurotoxicity (with prolonged therapy), asthenia, cortical blindness (administration of large doses to people with kidney disease), polyneuropathy (paresthesia and decreased tendon reflexes), color agnosia and complete loss of vision. Visual impairment often disappears within a few weeks after stopping the use of the drug;
• urogenital system lesions: increased serum urea or plasma creatinine levels, amenorrhea or azoospermia;
• changes in EBV values: decrease in plasma levels of Na, K, Mg and Ca;
• allergy symptoms: local allergic reactions in the injection area, erythematous rashes, urticaria, bronchospasm, fever, anaphylactoid symptoms, epidermal itching, decreased blood pressure and exfoliative dermatitis;
• Others: taste disturbances, alopecia, flu-like symptoms, myalgia or arthralgia, heart failure, cerebrovascular disorders and HUS.

Severe renal dysfunction has been observed only in isolated cases. Nephrotoxicity usually occurs when the dose of the drug is increased or in people who have previously used cisplatin.

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Overdose

In case of poisoning with Carboplatin, severe manifestations of negative symptoms of side effects of the drug are recorded.

Appropriate symptomatic measures are taken. Hemodialysis will be effective within the first 3 hours from the moment of drug overdose.

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Interactions with other drugs

Use together with nephro- or ototoxic drugs or aminoglycosides increases the toxicity of the drug associated with the corresponding organs.

Administration in combination with other myelosuppressants or radiation therapy potentiates the hematotoxic properties of the drug.

Combination with aluminum leads to the formation of a black sediment.

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Storage conditions

Carboplatin should be stored in a place protected from sunlight. The temperature should not exceed 25°C.

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Shelf life

Carboplatin is approved for use within 24 months from the date of manufacture of the therapeutic element.

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Application for children

Because experience with the use of drugs in pediatrics is very limited, it cannot be used in this subgroup of patients.

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Analogues

The analogs of the drug are Cytoplatin, Oxitan, Platinol with Displanor, Cisplatin and Oxiplat with Oxaliplatin, and in addition Exorum, Oxatera, Texalok with Platicad and Eloxatin with Plaxat.

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Reviews

Carboplatin receives quite contradictory reviews from patients regarding its medicinal effectiveness. There are comments that speak of excellent results of therapy in various oncological diseases, but there are also reports that claim that the drug has a toxic effect and other negative effects.

It is likely that such polarity of reviews is associated with personal sensitivity to the active element of the drug, as well as with the general well-being of the patient.

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