Oxaliplatin

Oxaliplatin is one of the antitumor agents, platinum derivatives. The drug has a wide spectrum of action, such as in vitro cytotoxicity, and in vivo antitumor activity in various tumor models.

[1], [2], [3], [4],

Indications of the oxaliplatin

Indications Oxaliplatin is a metastatic rectal cancer. Usually, this medication is prescribed together with 5-fluorouracil and folinic acid.

It is widely used in the adjuvant therapy of rectal cancer of the III stage (C according to Duke). This is usually done after a radical resection of the primary tumor. Apply it together with fluorouracil / calcium folio. Independently, he is not able to provide the necessary action.

The drug is used for disseminated rectal cancer as a monotherapy. Often it is used together with fluorouracil / calcium folio. The medication is also used in ovarian cancer as a second line of therapy. The spectrum of action of the drug is very wide. Usually, it is not used on its own, because this is not enough to achieve a positive result. Oxaliplatin has good antitumour properties and is able to really help, but only in combination with other effective drugs. 

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Release form

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

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

Oxaliplatin is not released as tablets or suspensions. It is administered intravenously in the dosage prescribed by the doctor. The dose directly depends on the problem that bothers the person. Usually, to achieve a positive effect, not one bottle is used. Much depends on the severity of the patient's condition and disease. To date, oxaliplatin in combination with other drugs is really capable of much. 

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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 (DACG).

To date, the exact mechanism of the drug is not known. There are suggestions that it works just like cisplatin. The action of the drug components creates reactive platinum, which in turn produces interstitial and interstitial crosslinks in the DNA molecule. Due to this, DNA synthesis is suppressed.

There is no cross-resistance to oxaliplatin, as to cisplatin or carboplatin, possibly due to the DACG group. It should be noted that the drug has the properties of an agent that is capable of increasing sensitivity to radiation exposure. No other information is available regarding this drug. It is only known that the whole action "lies" on the active component. To date, Oxaliplatin has been widely used both in its own form and in combination with other medicines.  

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Pharmacokinetics

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

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

Medication is excreted from the body mainly through the kidneys. Approximately 50% of the administered dose is excreted in the urine for the first 3 days. Excretion with feces in total is 0.5% per day. At day 11, it reaches its maximum figure of 5%. The half-life is 19 hours. Total elimination from erythrocytes is observed within 48 hours and is 273. Thus, Oxaliplatin is almost completely eliminated from the body, but it leaves a negative effect in the kidneys. 

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Dosing and administration

The way of application and dose is appointed by the doctor in an individual order. It can only be used by adults. The drug is administered intravenously in the form of infusions, the duration of which is 2-6 hours. Hyperhydration with the use of medication is not required.

If the agent is used in combination with 5-fluorouracil, oxaliplatin infusion should be the first. In the treatment of rectal cancer, 85 mg / m2 should be administered once every 2 weeks for 12 cycles. Usually it takes six months. To treat disseminated rectal cancer, 85 mg / m 2 is sufficient once every 2 weeks. Proceed as a monotherapy or in combination with 5-fluorouracil.

Treatment of ovarian cancer - 85 mg / m2 once in 2 weeks as a monotherapy or in combination with other chemotherapeutic drugs. Repeated administration of the drug is possible, but only if the number of neutrophils is less than 1500 / μl and platelets more than 500,000 / μl. A similar scheme of administration Oxaliplatin is prescribed by a doctor.

Use of the oxaliplatin during pregnancy

Use of Oxaliplatinum during pregnancy is unacceptable. There is a high risk of severe fetal damage, up to the development of various pathologies.

Women of childbearing age during the treatment of these drugs should avoid pregnancy in any way. High concentration of the drug will not allow bearing fruit or lead to the development of the child's irreparable pathologies.

There is no data on the penetration of the drug into breast milk. Therefore, take the product during the period of breastfeeding is prohibited. To prevent serious injuries to the baby, the treatment is postponed indefinitely or the feeding stops on the contrary.

Instructions regarding pregnancy and taking this medication are given by the attending physician. It is especially dangerous to take the drug in the first trimester of pregnancy, the risk of developing pathologies is too high. Therefore, oxaliplatin is taken with extreme caution or is looking for other ways to solve the problem. 

Contraindications

Contraindications to the use of oxaliplatinum are available and they are quite developed. So, in the first place, it is necessary to give up medicine to people who have an increased sensitivity to the main components of the drug. This can cause a strong allergic reaction. And in general, the body can react very peculiarly.

You can not take medication with myelosuppression, especially when the number of neutrophils is less than 2000 / μL and / or platelets is less than 100,000 / μL. There is also a limitation in peripheral sensory neuropathy with functional impairment before the start of the first course of treatment.

The drug can negatively affect the function of the kidneys. Therefore, people who have problems with this body, the use of the drug is strictly prohibited. Naturally, a special risk group is pregnancy and the period of breastfeeding. In any case, the medicine is taken solely on the advice of a doctor. Independently it can not even be purchased. Oxaliplatin is a powerful remedy in the fight against tumors.

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Side effects of the oxaliplatin

Side effects Oxaliplatin affects many organs and systems. So, cramps of extremities can be observed. This symptom occurs in almost 85-95% of all patients. The duration of these actions depends on the number of treatment courses. In some cases, neurological symptoms are observed, such as dysarthria, loss of deep tendon reflexes, and a symptom of Lermitt. It does not exclude pain and / or functional disorders. In this case, you need to adjust the dose. All neurological symptoms disappear completely after the treatment is completed.

System of blood formation. Anemia, neutropenia and thrombocytopenia can occur. In some cases, cases of hematological toxicity of the 3rd or 4th degree of severity were recorded rarely.

The digestive system. Often there is anorexia, vomiting, nausea, diarrhea, abdominal pain, in most cases - not very severe. Antimetics are used to prevent such symptoms.

Allergic reactions. It is not excluded: bronchospasm, angioedema, hypotension and anaphylactic shock. In extremely rare cases, renal dysfunction may occur. A rise in body temperature was often recorded. Oxaliplatin can cause serious side effects. 

[21], [22]

Overdose

An overdose of the drug is not ruled out. As such, there are no antidotes. There are certain negative manifestations on the part of the body. Thus, neuropathy characterized by dysesthesia and / or paresthesia of the extremities with or without convulsions is not excluded.

In some cases, functional abnormalities are possible. Underneath this are the complications of performing precise movements. It is possible that the bone marrow function is suppressed. This manifests itself in the form of anemia, neutropenia and thrombocytopenia.

If you have any strange symptoms or complications, it is recommended that you tell your doctor about it. In this case, symptomatic therapy should be performed, taking into account possible toxic manifestations and complete hematological control.

If the dose is calculated correctly and there are no abnormalities, there can be no question of overdose. Oxaliplatin is a potent drug with a wide spectrum of action. Therefore, self-adjusting the dose can lead to serious consequences. 

[23], [24],

Interactions with other drugs

Interactions Oxaliplatin with other drugs are possible and there is confirmation. So, the medication is widely used in combination with other drugs. This allows you to strengthen the effect and quickly reach a positive result.

But it is worth noting and such options when it is not practical to use this drug. So, he is able to stimulate the development of the cholinergic syndrome associated with the use of irinotecan, because of the increased oppression of acetylcholinesterase.

It should be noted that the drug in no way affects the pharmacokinetics of fluorouracil and topotecan. Pre-clinical studies showed a synergistic effect with fluorouracil and SN-38, an active metabolite of irinotecan. That's why you need to use the drug with extreme caution. It is important not to exceed the prescribed dosage in any case, this can lead to the development of serious consequences. Oxaliplatin may be used alone or in combination with other agents. 

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Storage conditions

Storage conditions Oxaliplatin should be observed without fail. So, you need to store it in a place protected from light. It is desirable that the temperature does not exceed 25 degrees Celsius. In no case can you give in to a freezer.

The children should not have access to the medicine. It is taken only by adults. Therefore, a small dose of it can adversely affect the child's body. You should understand this and take the drug away from the children.

He does not like the means and increased moisture, so it should not be too. In general, this medication is administered mainly in the hospital, so it is not necessary to store it at home. But if, after all, this should be done, all the above rules must be observed. Do not use the product at the expiration date, but it is 2 years. No other recommendations regarding the storage of the drug are available. Take Oxaliplatinum can be exclusively under the guidance of a doctor. 

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Special instructions

Special instructions regarding the use of the drug are observed. So, in no case it can not 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 influence.

The agent can be used exclusively under the guidance of a physician who has experience in the use of antitumor chemotherapeutic drugs. During the preparation and introduction of the solution, you need to use special rules and do everything consistently and accurately. In undiluted form, the product can not be used. Mix it with drugs that have a similar effect is strictly prohibited.

Nothing is known about the drug in breast milk. Therefore, in order to prevent damage to the child's organism, it is necessary to stop taking the medication or breast-feeding.

Before use, the product must be visually assessed, it must be clear, free from particles and sediment. All these "indicators" need to be monitored. In this case Oxaliplatin will not cause harm. 

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Shelf life

Shelf life of the product is 2 years. But this is just a figure. If a person does not observe special storage conditions, then this indicator may decrease at times.

So, it is important to maintain a certain temperature regime, it should not exceed 25 degrees of heat. In addition, do not put the product in the refrigerator, it should not be affected by 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 be taken only by adults and any impact on the child's body can lead to serious problems. You need to pay attention to the appearance of the bottle. The liquid should not change color, smell and get sediment. If all the above rules are followed, it will be possible to keep the remedy for the specified 2 years. But at the same time, attention should be paid to the appearance of the vial itself, there should not be any damage on it. In this case Oxaliplatin will serve for a set period of time.

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