Carboplatin

Brand Pharmakhemi B.V.

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Available since: 2019-09-19

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Clinical Pharmacology

Carboplatin is an inorganic complex compound containing a heavy metal - platinum.

It is believed that the main mechanism of action of this drug is due to binding to DNA, resulting in the formation of predominantly intra-helix stitching, which alter the structure of DNA and inhibit its synthesis. This effect appears regardless of the phase of the cell cycle. Hydration of carboplatin, which results in the formation of the active form (s) of the drug, is slower than the hydration of cisplatin.

Pharmacokinetics

After a single injection of carboplatin as an intravenous infusion for 1 hour, the concentration in plasma of total platinum and free (ultrafiltrable) platinum decreases in accordance with a two-phase model of first-order kinetics. Initial t_1/2 free platinum is about 1-2 hours, and terminal T_1/2 equal to 3-6 hours; total platinum has a similar initial T_1/2but terminal t_1/2 she has a longer (about 24 hours). With repeated dose injections for four consecutive days, accumulation of platinum in plasma was not observed. 24 hours after dosing, more than 85% of platinum in plasma is in a state bound to proteins.

Carboplatin is excreted primarily by the kidneys, and about 30% of the administered dose is excreted unchanged. In patients with a CC of 60 ml / min or more, approximately 65% and 70% of the administered dose are eliminated, respectively, 12 and 24 hours after the administration. Since carboplatin is eliminated almost entirely by glomerular filtration, only a very small concentration of carboplatin is present in the renal tubules, which may explain the small nephrotoxic potential of the drug compared with cisplatin.

Indications

Treatment of the following solid tumors:

ovarian cancer;
germ cell tumors of men and women;
lung cancer;
cervical cancer;
head and neck tumors;
osteogenic sarcomas;
medulloblastoma.

Composition

1 bottle contains:

Active substances: carboplatin 150 mg.

Excipients: mannitol.

Carboplatin is marketed under different brands and generic names, and comes in different dosage forms:

Brand name	Manufacturer	Country	Dosage form
Carboplatin-Teva	Pharmakhemi B.V	Netherlands	lyophilisate
Carboplatin-Lance	Lance farm	Russia	bottle

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Dosage and Administration

Carboplatin can be used both as monotherapy, and in combination with other anticancer drugs. The drug is introduced into / in the following dose regimens:

300 - 400 mg / m² IV drip for 15-60 minutes or as a 24-hour infusion;
100 mg / m2 / drip for 15-60 minutes daily for 5 days.

The introduction of carboplatin is repeated at intervals of at least 4 weeks with platelet counts of at least 100,000 cells / mm.³ blood and neutrophils at least 1500 blood cells / mm3.

Fluid injection before or after the use of carboplatin, as well as forced diuresis is not required.

Depending on the state of the bone marrow or kidney function, the therapeutic dose of carboplatin can be corrected as follows:

For patients who have symptoms of moderate or severe hematologic toxicity (i.e., the number of platelets and neutrophilic leukocytes are less than 50,000 and 500 / mm3, respectively), the possibility of reducing the dose — both in monotherapy and combined treatment regimens — should be considered 25%;
in patients with symptoms of impaired renal function (CK <60 ml="" min="" the="" risk="" of="" developing="" toxic="" effects="" carboplatin="" increases="" so="" dose="" should="" be="" reduced="" as="" follows:="" li="">

Creatinine clearance (ml / min)	Recommended Dose of Carboplatin (mg / m²)
41-59	250
16-40	200

If there are risk factors, such as, for example, previous courses of myelosuppressive therapy and / or age over 65 years, a dose reduction of 20-25% is recommended; Careful use of carboplatin is also recommended if the patient has previously been treated with nephrotoxic drugs such as cisplatin.

Before use, the carboplatin solution must be visually inspected for the presence of mechanical impurities and discoloration. Carboplatin should be diluted in physiological solution or 5% glucose solution to achieve a concentration of 1-0.5 mg / ml immediately before use - an infusion should be made no more than 24 hours after preparation of the solution.

Adverse reactions

From the hemopoietic system: The main toxic factor limiting the dose of carboplatin is the suppression of the function of bone marrow hematopoiesis. Myelosuppression is dose-dependent. The lowest level of platelets and leukocytes / granulocytes, as a rule, is achieved in 2-3 weeks after the start of the drug, with thrombocytopenia occurs more often. Adequate recovery to a level that allows the next dose of carboplatin to be taken usually takes at least 4 weeks. A sufficiently large number of patients may also show symptoms of anemia (hemoglobin level less than 11 g / dl), the intensity of which depends on the total dose of the drug. It may be necessary to conduct transfusion therapy, especially in patients undergoing long-term treatment (for example, more than 6 cycles of taking the drug). There is also a chance of clinical complications, such as fever, infectious diseases, sepsis / septic shock and bleeding.

From the digestive tract: within 6-12 hours after taking the drug, there is a chance of nausea and / or vomiting (mild to moderate), lasting up to 24 hours or more. The risk of emetic effects can be reduced by pre-treatment with antiemetic agents, continuous IV infusion of carboplatin for 24 hours, or fractional dosing for 5 consecutive days. Other types of adverse effects on the gastrointestinal tract, such as inflammation of the oral mucosa, diarrhea, constipation and abdominal pain, have also been observed in some cases.

From the side of the central nervous system and peripheral nervous system: there is a likelihood of peripheral neuropathies, mainly in the form of paresthesia and a decrease in deep tendon reflexes, which is more likely in patients over 65 years of age with prolonged or previous treatment with cisplatin. It is also possible the appearance of symptoms of dysfunction of the central nervous system. Long-term drug therapy can lead to cumulative neurotoxicity.

On the part of the hearing: ototoxicity manifests itself in the form of tinnitus and hearing impairment.

From the organs of vision: there is a possibility of temporary deterioration or complete loss of vision (possible loss of the ability to distinguish colors and see the light), as well as other violations of visual function. Improvement and / or full recovery of vision, as a rule, occurs within a few weeks after stopping the drug. Cortical blindness was observed in patients with impaired renal function treated with high doses of carboplatin.

On the part of the kidneys: there may be a slight and temporary increase in serum creatinine and urea concentrations. Acute kidney damage was rarely observed. The risk of nephrotoxicity with carboplatin intake (reduced creatinine clearance) increases with increasing doses of carboplatin, as well as in patients who have previously been treated with cisplatin.

Liver: there may be a slight and, as a rule, a temporary increase in serum concentrations of ACT, bilirubin and alkaline phosphatase. Patients treated with high doses of carboplatin with autologous bone marrow transplantation showed significant impairment of liver function.

From the electrolyte balance: possible hypokalemia, hypocalcemia, hyponatremia and / or hypomagnesemia.

Allergic reactions: erythematous rash, fever, pruritus, urticaria, bronchospasm, arterial hypotension and anaphylactic reactions. These reactions can occur within a few minutes after the introduction of carboplatin. In rare cases, exfoliative dermatitis may also occur.

Other side effects: alopecia, asthenia, flu-like symptoms, hemolytic-uremic syndrome, myalgia / arthralgia, heart failure, cerebrovascular disorders and allergic reactions directly at the injection site.

Contraindications

Severe renal dysfunction;
severe myelosuppression;
heavy bleeding;
pregnancy and lactation period;
hypersensitivity to carboplatin or other platinum-containing compounds.

Drug interactions

The use of carboplatin in combination with other myelosuppressive drugs or radiation therapy may increase the risk of hematological toxicity.

The use of carboplatin in combination with aminoglycosides, as well as with other nephrotoxic drugs increases the risk of nephrotoxic and / or ototoxic effects.

Pregnancy and Lactation

Contraindicated in pregnancy and lactation period.

Special instructions

The introduction of carboplatin should be carried out under the supervision of a physician with experience in the use of cytotoxic drugs. Continuous monitoring of possible toxic effects in the treatment of carboplatin is required, especially when using high doses of the drug.

Aluminum needles, syringes, catheters and infusion systems containing aluminum should not be used for the preparation and administration of the drug. Aluminum may react with carboplatin, leading to the formation of a precipitate or loss of activity of the drug.

Patients should regularly (for example, once a week) calculate the peripheral blood cells and monitor renal function (the most sensitive indicator is CC).

Periodically it is recommended to conduct neurological examinations, especially in patients who have previously undergone cisplatin therapy and in patients over 65 years of age. Carboplatin may cause cumulative ototoxic effects. Audiographic studies should be carried out before and during treatment or in the event of symptoms of hearing impairment. In the case of a clinically significant impaired hearing function, a corresponding change in the dose of the drug or discontinuation of treatment may be required.

Women and men during treatment with carboplatin and for 3 months after should use reliable methods of contraception.In case of contact with the eyes, immediately wash them with plenty of water or sodium chloride solution.

In case of contact with the skin, immediately rinse the place of contact with the drug with a large amount of water. In the case of inhalation of the drug or getting it into the mouth, you should immediately consult a doctor.

Overdosage

Special antidotes used in case of overdose of carboplatin does not exist. In case of overdose, more pronounced above-mentioned adverse reactions should be expected.

Symptomatic treatment. In the first 3 hours after administration of the drug, hemodialysis may be used.

Brand name: Carboplatin-Teva
Active ingredient: Carboplatin
Dosage form: Lyophilized powder for solution for intravenous administration.
Manufacturer: Pharmakhemi B.V.
Country of Origin: Netherlands