Oxaliplatin

Oxaliplatin is a platinum derivative antitumor drug. The drug has a broad spectrum of action, such as in vitro cytotoxicity and in vivo antitumor activity in various tumor models.

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Indications oxaliplatin

Indications for use Oxaliplatin - metastatic perirectal cancer. This medication is usually prescribed together with 5-fluorouracil and folinic acid.

It is widely used in adjuvant therapy of stage III perirectal cancer (Duke C). This is usually done after radical resection of the primary tumor. It is used together with fluorouracil/calcium foliant. It is not able to provide the necessary effect on its own.

The drug is used for disseminated perirectal cancer as monotherapy. It is often used together with fluorouracil/calcium foliant. The drug is also used for ovarian cancer as a second-line therapy. The drug has a very wide spectrum of action. Usually, it is not used independently, because this is not enough to achieve a positive result. Oxaliplatin has good antitumor properties and can really help, but only in combination with other effective drugs.

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Release form

The drug is released in the form of a liquid in a bottle. Packaging is 25 or 50 ml. The package contains one bottle. It contains the main active substance - oxaliplatin. Depending on the volume of the bottle, the amount of the component can vary from 50 to 100 mg.

The medicine also contains auxiliary substances - lactose monodirate. All these components have a powerful effect on the tumor. This drug is antitumor and is widely used in cancer both independently and in combination with other medications.

Oxaliplatin is not available as a tablet or suspension. It is administered intravenously in the dosage prescribed by the doctor. The dosage directly depends on the problem that bothers the person. Usually, more than one bottle is used to achieve a positive effect. Much depends on the severity of the patient's condition and his disease. Today, Oxaliplatin in combination with other drugs is really capable of a lot.

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Pharmacodynamics

This drug belongs to the class of platinum derivatives, in which the platinum atom forms a complex with oxalate and diaminocyclohexane (DACH).

To date, the exact mechanism of the drug's action is unknown. There are suggestions that it works in the same way as cisplatin. The action of the drug's components is created by reactive platinums, which in turn produce inter-strand and intra-strand cross-links in the DNA molecule. Due to this, DNA synthesis is inhibited.

There is no cross-resistance to oxaliplatin, as there is to cisplatin or carboplatin, possibly due to the DACG group. It is worth noting that the drug has the properties of an agent that can increase sensitivity to radiation. There is no other information regarding this drug. It is only known that all the action "lies" on the active component. Today, Oxaliplatin is widely used both independently and in combination with other medications.

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Pharmacokinetics

After intravenous administration of the drug, it mainly accumulates in erythrocytes and does not pass into plasma. Only 85-88% of platinum binds to proteins in the first 5 hours after administration.

It should be noted that Oxaliplatin is capable of undergoing rapid non-enzymatic biotransformation. In this case, reactive platinum complexes are formed. Active metabolites of oxaliplatin belong to the group of DACG-platinum complexes.

The drug is excreted from the body mainly through the kidneys. Approximately 50% of the administered dose is excreted in the urine during the first 3 days. Excretion with feces in total is 0.5% per day. On the 11th day, it reaches its maximum figure of 5%. The half-life is 19 hours. Complete elimination from red blood cells is observed within 48 hours and is 273. Thus, Oxaliplatin is almost completely excreted from the body, but at the same time leaves a negative effect on the kidneys.

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Dosing and administration

The method of application and dosage are prescribed by the doctor individually. It can only be used by adults. The medicine is administered intravenously in the form of infusions, the duration of which is 2-6 hours. Hyperhydration is not required when using the medicine.

If the drug is used in combination with 5-fluorouracil, oxaliplatin infusion should be the first. For the treatment of perirectal cancer, 85 mg/m2 should be administered once every 2 weeks for 12 cycles. This usually takes six months. For the treatment of disseminated perirectal cancer, 85 mg/m2 once every 2 weeks is sufficient. It is taken as monotherapy or in combination with 5-fluorouracil.

Treatment of ovarian cancer - 85 mg/m2 once every 2 weeks as monotherapy or in combination with other chemotherapeutic drugs. Repeated administrations of the drug are possible, but only if the neutrophil count is less than 1500/mcl and platelets are more than 500,000/mcl. A doctor prescribes such a scheme for administering Oxaliplatin.

Use oxaliplatin during pregnancy

The use of Oxaliplatin during pregnancy is unacceptable. There remains a high risk of severe damage to the fetus, up to the development of various pathologies.

Women of childbearing age should avoid pregnancy by all means during treatment with this drug. High concentration of the drug will not allow the fetus to be carried to term or will lead to the development of irreparable pathologies in the child.

There is no data on the penetration of the drug into breast milk. Therefore, it is prohibited to take the drug during breastfeeding. To prevent serious "injuries" to the baby, treatment is postponed for an indefinite period or, on the contrary, breastfeeding is stopped.

Instructions regarding pregnancy and taking this medicine are given by the attending physician. It is especially dangerous to take the medicine in the first trimester of pregnancy, the risk of developing pathologies is too high. Therefore, Oxaliplatin is taken with special caution or other ways to solve the problem are sought.

Contraindications

There are contraindications to the use of Oxaliplatin and they are quite detailed. So, first of all, people who have increased sensitivity to the main components of the drug should refuse the drug. This can cause a strong allergic reaction. And in general, the body can react in a very peculiar way.

The medication should not be taken in case of myelosuppression, especially when the neutrophil count is less than 2000/μl and/or platelets are less than 100,000/μl. There is also a restriction in case of peripheral sensory neuropathy with functional impairment before the start of the first course of treatment.

The drug can negatively affect kidney function. Therefore, people with problems with this organ are strictly prohibited from using the drug. Naturally, pregnancy and breastfeeding are a special risk group. In any case, the drug is taken exclusively on the doctor's recommendations. You won't even be able to buy it on your own. Oxaliplatin is a powerful drug in the fight against tumors.

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Side effects oxaliplatin

Side effects of Oxaliplatin affect many organs and systems. Thus, limb cramps may be observed. This symptom occurs in almost 85-95% of all patients. The duration of these effects depends on the number of treatment courses. In some cases, neurological symptoms are also observed, such as dysarthria, loss of deep tendon reflexes and Lhermitte's symptom. Pain and/or functional disorders are not excluded. In this case, it is necessary to adjust the dose. All neurological symptoms completely disappear after completion of treatment.

Hematopoietic system. Anemia, neutropenia and thrombocytopenia may occur. Grade 3 or 4 hematological toxicity has been reported in some cases but is rare.

Digestive system. Often there is anorexia, vomiting, nausea, diarrhea, abdominal pain, in most cases - not severe. To prevent such symptoms, antiemetic agents are used.

Allergic reactions. Bronchospasm, angioedema, hypotension and anaphylactic shock are possible. In extremely rare cases, renal dysfunction may occur. Increased body temperature has been reported quite often. Oxaliplatin may cause serious side effects.

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Overdose

An overdose of the drug is not excluded. There are no antidotes as such. Certain negative effects on the body are possible. Thus, neuropathy is not excluded, characterized by dysesthesia and/or paresthesia of the extremities with or without convulsions.

In some cases, functional disorders are possible. This means complications in performing precise movements. Suppression of bone marrow function is possible. This manifests itself in the form of anemia, neutropenia, and thrombocytopenia.

If any strange symptoms or complications occur, it is recommended to inform the attending physician. In such a case, symptomatic therapy is performed, taking into account possible toxic manifestations and full hematological control.

If the dose is calculated correctly and no deviations are observed, then there can be no talk of an overdose. Oxaliplatin is a powerful drug with a wide range of action. Therefore, self-adjustment of the dose can lead to serious consequences.

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Interactions with other drugs

Oxaliplatin interactions with other drugs are possible and there is evidence of this. Thus, the drug is widely used in combination with other drugs. This allows you to enhance the effect and quickly reach a positive result.

But it is worth noting such options when it is inappropriate to use this drug. Thus, it is capable of stimulating the development of cholinergic syndrome associated with the use of irinotecan, due to increased inhibition of acetylcholinesterase.

It should be noted that the drug does not affect the pharmacokinetics of fluorouracil and topotecan in any way. Preclinical studies have shown a synergistic effect with fluorouracil and SN-38, the active metabolite of irinotecan. That is why the drug should be used with extreme caution. It is important not to exceed the prescribed dosage in any case, as this can lead to the development of serious consequences. Oxaliplatin can be used both independently and in combination with other drugs.

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Storage conditions

The storage conditions of Oxaliplatin must be strictly observed. Thus, it must be stored in a place protected from light. It is desirable that the temperature does not exceed 25 degrees Celsius. In no case should the product be frozen.

Children should not have access to the medicine. It is taken exclusively by adults. Therefore, a small dose of it can negatively affect a child's body. It is worth understanding this and keeping the drug away from children.

The product does not like high humidity, so it should not be there either. In general, this medication is administered mainly in the hospital, so there is no need to store it at home. But if, nevertheless, this should be done, you must follow all the above rules. You cannot use the product after the expiration date, which is 2 years. There are no other recommendations regarding the storage of the drug. Oxaliplatin can only be taken under the supervision of a doctor.

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Special instructions

There are special instructions regarding the use of the drug. Thus, it should never be used by pregnant girls and nursing mothers. The mechanism of action of the drug on the child's body is unknown, so it is better to avoid such an effect.

The product can be used only under the guidance of a physician who has experience in using antitumor chemotherapeutic drugs. During the preparation and administration of the solution, special rules must be followed and everything must be done consistently and carefully. The product cannot be used undiluted. Mixing it with drugs that have a similar effect is strictly prohibited.

Nothing is known about the excretion of the drug into breast milk. Therefore, in order to prevent damage to the child's body, it is necessary to stop taking the drug or breastfeeding.

Before use, the product must be visually assessed, it must be transparent, without particles and sediment. All these "indicators" must be monitored. In this case, Oxaliplatin will not cause harm.

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Shelf life

The shelf life of the product is 2 years. But this is just a figure. If a person does not comply with special storage conditions, this figure can decrease significantly.

So, it is important to maintain a certain temperature regime, it should not exceed 25 degrees Celsius. In addition, do not put the product in the refrigerator, it should not be exposed to the negative effects of cold. Direct sunlight, excessive heat and especially moisture are completely excluded.

Children should not have access to this drug. It can only be taken by adults and any impact on a child's body can lead to serious problems. You should also pay attention to the appearance of the bottle. The liquid should not change color, smell or acquire sediment. If you follow all the above rules, you can store the product for the specified 2 years. But you should also pay attention to the appearance of the bottle itself, there should be no damage on it. In this case, Oxaliplatin will last for the specified period.

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