Oxaliplatin: Formula, Indications, Mechanism of Action, Dosage, Side Effects, Warnings, Contraindications and Interactions

It is a drug that belongs to the largest group of alkylating agents and is known as a platinum-containing compound.

It works by stopping or slowing the growth of cancer cells .

Although it belongs to the same class of drugs as cisplatin and carboplatin, oxaliplatin shows marked differences in its pharmacokinetic and pharmacodynamic profiles, as well as in its spectrum of antitumor activity and its toxicity.

Oxaliplatin pharmacology has uncovered one of the drug’s most attractive characteristics: its lack of cross-resistance with cisplatin and carboplatin, which complements a manageable toxicity profile.

The pharmacodynamic characterization of oxaliplatin has also helped to gain an understanding of the pathogenesis of peripheral neuropathy, which should result in a more effective management of this complication.

Chemical formula of oxaliplatin

  • C8H12N2O4Pt.

Presentation

Oxaliplatin is available on the market as a solution to be administered parentally, in single-use bottles of 50 mg and 100 mg.

Indications of oxaliplatin

Oxaliplatin is used to treat colon and rectal cancer .

It is an adjunctive treatment for stage III colon cancer in patients who have undergone complete resection of a primary tumor and treatment of advanced colon rectal cancer in combination with 5-fluorouracil-leucovorin infusion.

Mechanism of action

Several mechanisms of action are attributed to oxaliplatin.

Like other platinum-based compounds, oxaliplatin exerts its cytotoxic effect primarily through damage to deoxyribonucleic acid.

Cancer cell apoptosis can be caused by formation of deoxyribonucleic acid lesions, arrest of deoxyribonucleic acid synthesis, inhibition of ribonucleic acid synthesis, and triggering of immune reactions.

Oxaliplatin also exhibits synergy with other cytotoxic drugs.

Despite the initial sensitivity to oxaliplatin, most cancer cells will eventually develop resistance.

Many resistance mechanisms have been described or hypothesized due to the similarity between oxaliplatin and cisplatin.

Combining oxaliplatin with other antineoplastic drugs can prevent resistance, or even reverse it.

Oxaliplatin dosage

This medicine is given by injection into a vein, once every 2 weeks.

The exact dose and treatment schedule depend on several factors, including how well the cancer patient is responding to the drug.

The physician will determine the best approach for the patient based on the results obtained.

Side effects

Oxaliplatin can cause diarrhea, taste changes, mouth sores, nosebleeds, tiredness, headache, dizziness, or trouble sleeping.

Nausea and vomiting can be severe in some patients.

Your doctor may prescribe medications to prevent or relieve nausea and vomiting.

Eating several small meals a day, not eating before treatment, or limiting activity can help lessen some of these effects.

Temporary hair loss can occur rarely. However, normal hair growth returns after oxaliplatin treatment is finished.

You should tell your doctor immediately if you have any of these serious side effects with the administration of oxaliplatin treatment, including:

  • The presence of pain, redness, swelling at the injection site.
  • Bruising, easy-onset and unusual bleeding.
  • Mood swings such as depression .
  • Signs of loss of body water, such as decreased urination, increased thirst, dry mouth.
  • Muscle pain, tenderness, weakness, and cramps.
  • Signs of kidney problems, such as changes in the amount of urine.
  • Pain, redness, swelling of the arms and legs.
  • Pain in the groin and calf.

Oxaliplatin can sometimes affect how your nerves work (peripheral neuropathy) and develop the following symptoms:

  • Sensitivity to cold
  • Difficulty breathing, swallowing, or speaking.
  • Tension in the jaw.
  • Strange sensation on the tongue.
  • Pain in the eye
  • Pressure in the chest.
  • Numbness, “tingling” sensation in the hands, feet,
    mouth, and throat.

These nervous problems can be lessened by avoiding cold drinks and ice and by dressing in warm clothing.

The physician should be informed if nervous problems begin to interfere with the patient’s normal daily activities such as walking, writing, and eating.

As well as in the case of very serious side effects, which include:

  • Severe dizziness.
  • Fainting.
  • Fast and irregular heartbeat.
  • Dry cough.
  • A shortness of breath.
  • Chest pain
  • The black vomit.
  • Vision changes, such as blurred vision or temporary
    vision loss .
  • Seizures.
  • The confusion.

This medicine can lower the body’s ability to fight infections.

The doctor should be informed immediately if the patient develops any signs of infection, such as fever, chills, or a persistent sore throat.

In very rare cases this medicine can cause a very serious allergic reaction.

However, you should seek immediate medical help if you notice any symptoms of a severe allergic reaction, including:

  • The eruptions.
  • Itching and swelling, especially of the face, tongue, and throat.
  • Severe dizziness.
  • Difficulty breathing.

Warnings and Contraindications

Before using oxaliplatin, you should tell your doctor if you are allergic to the drug or other platinum-containing products such as cisplatin, carboplatin, or if you have any other allergies.

This product may contain inactive ingredients, which can also cause allergic reactions or some other problem.

Before using this medicine, the medical history of the patient should be informed to the doctor, especially of diseases such as:

  • Kidney-type problems.
  • Blood disorders.
  • Diseases of the bone marrow.
  • Nervous system disorders.
  • Heart disease: certain heart problems such as heart failure , slow heartbeat, prolongation of the QT interval on the electrocardiogram.

Low levels of potassium or magnesium in the blood can also increase the risk of QT prolongation.

This risk can be increased if certain medications such as diuretics are used or if you have conditions such as heavy sweating, diarrhea, or vomiting.

Once the treatment is administered, you should avoid driving cars, using machinery, or doing any activity that requires alertness or clear vision.

This precaution should be followed until you can safely perform these activities. The use of alcoholic beverages or drugs should be limited, including the use of marijuana.

Immunizations or vaccinations should not be received without informing the treating physician and contact with people who recently received the oral polio vaccine or the flu vaccine inhaled through the nose should be avoided .

General aseptic conditions must be maintained to avoid the spread of bacteria as well as infections.

The use of sharp objects such as razor blades and nail clippers should be reduced, as well as the performance of activities such as contact sports, where the patient is at risk of being cut, hurt or injured.

Older adults may be even more sensitive to the side effects of this drug, especially diarrhea, loss of too much body water and potassium, low white blood cell count, tiredness, fainting, and QT interval prolongation.

This medicine can affect sperm production in men.

Male patients must use several reliable contraceptive methods during treatment and for some time after it has been completed.

The use of Oxaliplatin during pregnancy is not recommended. This medicine could have adverse effects on the fetus.

The use of reliable contraceptive methods (such as condoms or birth control pills) should be discussed with the doctor.

There is no information on whether oxaliplatin is excreted in human milk.

Due to the possible risk to the baby, breastfeeding is not recommended when using this medicine.

Oxaliplatin interactions

Oxaliplatin can change the action of medicines taken concomitantly or increase the risk of serious side effects.

Do not start, stop or change the dosage of the medicine without consulting your doctor.

Some of the medications that can negatively interact with oxaliplatin include:

  • Aminoglycosides like gentamicin and , amikacin .
  • Amphotericin B.
  • Nalidixic acid.
  • Nonsteroidal anti-inflammatory drugs such as ibuprofen.
  • The tacrolimus, pimecrolimus and sirolimus.
  • Vitamin K antagonists such as warfarin .
  • Inactivated vaccines.
  • Live vaccines.