Karboplatin

Carboplatin is an anticancer drug, which contains platinum in its composition and exerts an alkylating effect on the DNA cells of malignant tumors.

The drug effect develops through the formation of cross-links inside the DNA-cell helix of the neoplasm, as a result of which the DNA structure itself changes. This leads to the suppression of the replication of nucleic acids, and then the complete destruction of the cells of tumors that have a malignant character.

Indications Carboplatin

Used for the following disorders:

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

[1]

Release form

The release of drugs is implemented in the form of a concentrate for infusion, inside the bottle, having a capacity of 5, 15, as well as 45 or 75 ml.

[2], [3], [4], [5], [6]

Pharmacokinetics

Carboplatin-related metabolic processes are realized through hydrolysis; at the same time active ligaments are formed that interact with the DNA of the neoplasm. Distribution volume figures equal to 16 liters.

Intrasoplasma synthesis with protein is rather weak, but irreversible platinum bundles formed from a combination of carboplatin and plasma proteins are slowly eliminated with the lowest half-life term of 5 days.

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

[7], [8], [9], [10], [11], [12]

Dosing and administration

An antitumor medication is prescribed both for monotherapy and in combination with other medicines with a similar type of influence (for example, complex treatment with the introduction of Carboplatin and paclitaxel).

Taking into account the location and size of the neoplasm, drug bottles are used with a capacity of 0.45 g / 45 ml or with other volumes. It is prescribed intravenous administration via infusion (drip), for a period of 15-60 minutes. Used in such portions:

• 0.1 g / m ^{2 of the} medication, daily for a period of 5 days;
• 0.3-0.4 g / m ² PM, 1 time per 1 month.

The intervals between the use of infusions in the case of a neutrophil ratio of 1500 / mm ² and above, as well as platelets of 100000 / mm ² and above, must be at least 1 month.

Before and after applying the medication, it is not necessary to perform forced diuresis and additionally inject the patient with fluids.

In the case of a hematological form of toxicity (moderate or severe severity) with a neutrophilic leukocyte count below 500 / mm ² and platelets below 50,000 / mm ², a portion may be reduced by 25%.

During kidney disease (the level of QC below 60 ml per minute) increases the likelihood of development of toxic activity of Carboplatin, because of which its portions are reduced, taking into account the values of QC (16-40 / 0.2 g, as well as KK 41-59 / 0.25 l / m ² ).

Older people (age over 65 years), and besides this, when myelosuppressive therapy was performed before, it is required to reduce the dose by 20-25%.

Before the introduction of the medication you need to carefully examine it to identify the possible presence of foreign particles and the violation of the color of the liquid.

Dilution of the drug should be in 5% glucose or 9% NaCl, so that its concentration at the same time was 0.5-1 mg / ml. The drug is administered immediately after production; the finished liquid can be stored no more than 24 hours.

[18], [19],

Use Carboplatin during pregnancy

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

Carboplatin can not be prescribed during breastfeeding either, because it can have a toxic effect on an infant.

[13]

Contraindications

The main contraindications:

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

Caution is required when using for such violations:

• hearing impairment;
• oppressed hematopoiesis within the bone marrow (this includes conditions observed after performing radiation or chemotherapy);
• kidney problems;
• use in conjunction with nephrotoxic drugs (for example, cisplatin);
• recent vaccination;
• infection of fungal, bacterial or viral genesis in the active phase.

[14]

Side effects Carboplatin

Main adverse events:

• digestive disorders: diarrhea, abdominal pain, stomatitis, vomiting, constipation, loss of appetite, nausea and disorders of the liver (increased AST activity with alkaline phosphatase and an increase in intra-serum bilirubin);
• disorders of hematopoietic processes: oppression of blood formation within the bone marrow;
• problems with NA: ear noise, impaired vision or hearing, accumulative neurotoxicity (with prolonged therapy), asthenia, cortical blindness (introduction of large portions to people with renal diseases), polyneuropathy (paresthesia and reduced tendon reflexes), color agnosia and complete loss of vision. Visual impairment often disappears after a few weeks from the time the drug is discontinued;
• lesions of the urogenital system: an increase in the values of intra-serum urea or intraplasma creatinine, amenorrhea or azoospermia;
• changes in EBV values: reduction of plasma indices of Na, K, Mg and Ca;
• allergy symptoms: local allergic manifestations in the injection area, erythematous rashes, urticaria, bronchospasm, fever, anaphylactoid signs, epidermal itching, decrease in blood pressure and exfoliative dermatitis;
• others: taste disorders, alopecia, flu-like symptoms, myalgia or arthralgia, HF, cerebrovascular disorders and HUS.

Severe disorders associated with the activity of the kidneys, were observed only sporadically. Usually, nephrotoxic effects develop in the event of increasing portions of the drug or in individuals who have previously used cisplatin.

[15], [16], [17]

Overdose

In case of Carboplatin poisoning, severe manifestations of negative symptoms of adverse symptoms of drugs are recorded.

Corresponding symptomatic actions are performed. Hemodialysis will be effective within the first 3 hours after the overdose of the medication.

[20], [21],

Interactions with other drugs

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

Introduction in combination with the rest of myelo-suppressors, or through radiation therapy, potentiates the hematotoxic properties of the drug.

The combination with aluminum leads to the formation of a sediment having a black color.

[22], [23], [24], [25], [26]

Storage conditions

Carboplatin must be kept in a place protected from sunlight. The temperature should be no more than 25 ° C.

[27], [28], [29], [30]

Shelf life

Carboplatin is allowed to apply within a 24-month period from the date of manufacture of the therapeutic element.

[31], [32], [33]

Application for children

Because the experience of using drugs in pediatrics is very limited, it can not be used in this subgroup of patients.

[34], [35], [36], [37], [38], [39]

Analogs

Analogues of drugs are the substances Cytoplatin, Occitan, Platinol with Dysplanor, Cisplatin and Oxyplates with Oxaliplatin, and in addition, Ekzorum, Oxatera, Texalok with Platicad and Eloxatin with Plaksat.

[40], [41], [42], [43], [44], [45], [46]

Reviews

Carboplatin receives rather inconsistent feedback from patients regarding its drug effectiveness. There are comments that speak of an excellent result of therapy for a variety of oncological diseases, but there are also reports stating that the drug has a toxic effect and other negative manifestations.

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

[47], [48], [49], [50], [51], [52]