Xaloplat
Xaloplat Uses, Dosage, Side Effects, Food Interaction and all others data.
Xaloplat, a platinum-containing complex similar to cisplatin, is an alkylating agent. After intracellular hydrolysis, the platinum compound binds to DNA forming cross-links which inhibit DNA replication and transcription, resulting in cell death.
Xaloplat selectively inhibits the synthesis of deoxyribonucleic acid (DNA). The guanine and cytosine content correlates with the degree of Xaloplat-induced cross-linking. At high concentrations of the drug, cellular RNA and protein synthesis are also suppressed.
| Trade Name | Xaloplat |
| Availability | Prescription only |
| Generic | Oxaliplatin |
| Oxaliplatin Other Names | Diaminocyclohexane Oxalatoplatinum, L-OHP, Oxalatoplatin, Oxalatoplatinum, Oxaliplatin, oxaliplatine, oxaliplatino, oxaliplatinum |
| Related Drugs | Tagrisso, Tarceva, Tabrecta, Gilotrif, Paraplatin, Keytruda, capecitabine, pembrolizumab, Avastin, Xeloda |
| Weight | 5mg/ml |
| Type | IV Infusion |
| Formula | C8H14N2O4Pt |
| Weight | Average: 397.294 Monoisotopic: 397.060149 |
| Protein binding | Plasma protein binding of platinum (active metabolite) is irreversible and is greater than 90%, primarily to albumin and gamma-globulins. It is also irreversibly binds to erythrocytes. |
| Groups | Approved, Investigational |
| Therapeutic Class | Cytotoxic Chemotherapy |
| Manufacturer | Beacon Pharmaceuticals Ltd |
| Available Country | Bangladesh |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Xaloplat, used in combination with infusional 5-fluorouracil/leucovorin, is used for:
- Adjuvant treatment of stage III colon cancer in patients who have undergone complete resection of the primary tumor.
- Treatment of advanced colorectal cancer.
Xaloplat is also used to associated treatment for these conditions: Advanced Colorectal Cancer, Advanced Ovarian Cancer, Advanced Pancreatic Cancer, Chronic Lymphocytic Leukemia (CLL) - Refractory, Colon Cancer Stage III, Esophageal Cancers, Malignant Neoplasm of Stomach, Advanced biliary adenocarcinoma, Refractory Neuroendocrine Tumour, Refractory Non-Hodgkin's lymphoma, Refractory Testicular cancer
How Xaloplat works
Xaloplat undergoes nonenzymatic conversion to active derivatives via displacement of the labile oxalate ligand. Several transient reactive species are formed, including monoaquo and diaquo DACH platinum, which covalently bind with macromolecules. After activation, oxaliplatin binds preferentially to the guanine and cytosine moieties of DNA, leading to cross-linking of DNA, thus inhibiting DNA synthesis and transcription. Cytotoxicity is cell-cycle nonspecific.
Dosage
Xaloplat dosage
Intravenous (Adult)-
Adjuvant therapy in stage III colon cancer: In combination with fluorouracil/ leucovorin: 85 mg/m2 every 2 wk for 12 cycles. Dose to be given by IV infusion over 2-6 hr, dissolved in 250-500 ml of glucose 5%, every 2 wk; given for 12 cycles. After recovery from toxicity, reduce dose to 75 mg/m2. Administer before fluoropyrimidines.
Advanced colorectal cancer: In combination with fluorouracil/ leucovorin: 85 mg/m2 every 2 wk until disease progression or unacceptable toxicity. Dose to be given by IV infusion over 2-6 hr, dissolved in 250-500 ml of glucose 5%, . After recovery from toxicity, reduce dose to 65 mg/m2. Administer before fluoropyrimidines.
Reconstitute with 10 ml (for 50 mg vial) or 20 ml (for 100 mg vial) water for inj or 5% dextrose inj. Reconstituted solution must be further diluted with 250-500 ml of 5% dextrose inj before admin.
Side Effects
Fatigue, fever, pain, headache, insomnia, nausea, diarrheoa, vomiting, abdominal pain, constipation, anorexia, stomatitis, anemia, thrombocytopenia, leukopenia, aspartate and alanine transaminases increased, total bilirubin increased, peripheral neuropathy, back pain, dyspnoea, cough, oedema, chest pain, peripheral oedema, flushing , thromboembolism, dizziness, rash, alopecia , hand-foot syndrome dehydration, hypokalaemia, dyspepsia, taste perversion, flatulence, mucositis, gastroesophageal reflux, dysphagia, dysuria, neutropenia, inj site reaction, rigors, arthralgia, abnormal lacrimation, serum creatinine increased, rhinitis, epistaxis, pharyngitis, pharyngolaryngeal dysesthesia, allergic reactions, hiccup.
Toxicity
There have been five cases of oxaliplatin overdose reported. One patient received two 130 mg/m2 doses of oxaliplatin (cumulative dose of 260 mg/m2) within a 24-hour period. The patient experienced Grade 4 thrombocytopenia (3) without any bleeding, which resolved. Two other patients were mistakenly administered oxaliplatin instead of carboplatin. One patient received a total oxaliplatin dose of 500 mg and the other received 650 mg. The first patient experienced dyspnea, wheezing, paresthesia, profuse vomiting and chest pain on the day of administration. She developed respiratory failure and severe bradycardia, and subsequently did not respond to resuscitation efforts. The other patient also experienced dyspnea, wheezing, paresthesia, and vomiting. Most common adverse reactions (incidence ≥ 40%) were peripheral sensory neuropathy, neutropenia, thrombocytopenia, anemia, nausea, increase in transaminases and alkaline phosphatase, diarrhea, emesis, fatigue and stomatitis.
Precaution
Should be administered under the supervision of an experienced cancer chemotherapy physician. Use appropriate precautions for handling and disposal. Monitor neurological status and dose should be reduced if symptoms are prolonged or severe. Monitor blood counts during treatment and courses should not be repeated until blood counts have recovered. Caution in elderly, moderate degrees of renal impairment. Avoid using aluminum-containing needles or IV admin sets that may come into contact with oxaliplatin as aluminum has been reported to cause degradation of platinum compounds.
Interaction
May decrease plasma levels of digoxin. May increase risk of toxicity with nephrotoxic drugs. When administered as sequential infusions, taxane derivatives (docetaxel, paclitaxel) should be administered before oxaliplatin to limit myelosuppression and enhance efficacy.
Food Interaction
No interactions found.Xaloplat Drug Interaction
Moderate: palonosetron, prochlorperazine, loperamide, polyethylene glycol 3350, pegfilgrastim, capecitabine, ondansetronUnknown: lorazepam, bevacizumab, diphenhydramine, docusate, dexamethasone, apixaban, fentanyl, omega-3 polyunsaturated fatty acids, acetaminophen, acetaminophen, cyanocobalamin, ascorbic acid, cholecalciferol
Xaloplat Disease Interaction
Major: arrhythmias, pulmonary toxicityModerate: neurologic toxicity, neutropenia, renal impairment, rhabdomyolysis, thrombocytopenia
Volume of Distribution
- 440 L [single 2-hour IV infusion at dose of 85 mg/m^2] At the end of a 2-hour infusion of oxaliplatin, approximately 15% of the administered platinum is present in the systemic circulation. The remaining 85% is rapidly distributed into tissues or eliminated in the urine.
Elimination Route
Bioavailability is complete following intravenous administration. When a single 2-hour intravenous infusion of oxaliplatin at a dose of 85 mg/m^2 is given, the peak serum concentration was 0.814 mcg/mL.
Half Life
The decline of ultrafilterable platinum levels following oxaliplatin administartion is triphasic, with two distribution phases: t1/2α; 0.43 hours and t1/2β; 16.8 hours. This is followed by a long terminal elimination phase that lasts 391 hours (t1/2γ).
Clearance
- 10 - 17 L/h [renal clearance]
Elimination Route
The major route of platinum elimination is renal excretion. At five days after a single 2-hour infusion of oxaliplatin, urinary elimination accounted for about 54% of the platinum eliminated, with fecal excretion accounting for only about 2%.
Pregnancy & Breastfeeding use
Category D: There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).
Contraindication
Pregnancy. Peripheral neuropathy with functional impairment. Severe renal impairment.
Special Warning
Renal Impairment: Dose adjustment may be needed
Acute Overdose
Extensions of known adverse reaction (e.g. thrombocytopenia, myelosuppression, nausea, vomiting, neurotoxicity, respiratory symptoms). Treatment is supportive.
Storage Condition
Store intact vials at 15-30°C; do not freeze. Reconstituted solution: May store at 2-8°C for up to 24 hr. Diluted solutions: Stable up to 6 hr at 20-25°C or up to 24 hr under refrigeration at 2-8°C.
Innovators Monograph
You find simplified version here Xaloplat
Xaloplat contains Oxaliplatin see full prescribing information from innovator Xaloplat Monograph, Xaloplat MSDS, Xaloplat FDA label
FAQ
What is Xaloplat used for?
Xaloplat is a cancer medication used to treat colorectal cancer. Often it is used together with fluorouracil and folinic acid (leucovorin) in advanced cancer.
How safe is Xaloplat?
While Xaloplat has only mild hematologic and gastrointestinal side effects, its dose-limiting toxicity is a cumulative sensory neurotoxicity that resembles that of cisplatin with the important difference of a more rapid and complete reversibility.
How does Xaloplat work?
Xaloplat interferes with the development of DNA in a cell. This stops it from dividing into 2 new cells and kills it.
What are the common side effects of Xaloplat?
Common side effects of Xaloplat are include: Diarrhea, changes in taste, mouth sores, nosebleeds, tiredness, headache, dizziness, or trouble sleeping. Nausea and vomiting may be severe in some patients. Your doctor may prescribe medication to prevent or relieve nausea and vomiting.
Is Xaloplat safe during pregnancy?
During pregnancy is contraindicated. Use of this drug is not recommended during pregnancy, especially during the first trimester, based on the results of animal studies and the pharmacological action of this drug.
Is Xaloplat safe during breastfeeding?
The manufacturer recommends that women should not breastfeed during treatment with Xaloplat injection and for 3 months after the final dose.
Can I drink alcohol Xaloplat?
The drinking of alcohol (in small amounts) does not appear to affect the safety or usefulness of Xaloplat. It is best to use birth control while being treated with Xaloplat.
Can I drive after taking Xaloplat?
This Xaloplat can cause dizziness, vision problems or vision loss. You should not drive or operate machinery until you know how the medication affects you.
When should be taken of Xaloplat?
You should take them within 30 minutes of finishing a meal.
How often can I take Xaloplat?
You usually take the tablets twice a day, about 12 hours apart.
How effective is Xaloplat?
The introduction of Xaloplat was associated with no significant improvement in the slopes (per half-year) of the three-year disease-free survival rate (0.2%, 95% CI: −1.7∼2.2%) and five-year overall survival rate (0.6%, 95% CI: −1.8∼3%).
How long does Xaloplat stay in my system?
The first elimination half-life (t1/2) for cisplatin was 5.02 months and the second 37.0 months. For Xaloplat, these half-lifes were 1.37 and 535 months.
How long can I take Xaloplat?
Each cycle lasts 3 weeks (21 days). Depending on your needs, you may have between 4 and 8 cycles.
Will I lose my hair with Xaloplat?
You could lose all your hair.
Can Xaloplat cause liver damage?
There are an increasing number of reports indicating that Xaloplat-based chemotherapy can cause liver damage (1–5). Xaloplat-induced liver damage is characterized histologically by sinusoidal dilatation, hepatocyte atrophy and/or fibrosis and venular obstruction.
Can Xaloplat cause cancer?
In cancer survivors, neuropathy induced by Xaloplat has a deleterious impact on their quality of life.
Who should not take Xaloplat?
A patient who is producing milk and breastfeeding. muscle pain or tenderness with increase creatine kinase. a type of brain disorder called posterior reversible encephalopathy syndrome. chronic kidney disease stage 4.
What happens if I miss a dose?
Contact your doctor if you miss an appointment for your oxaliplatin injection.
Can Xaloplat cause heart damage?
Xaloplat is able to induce coronary vasoconstriction leading to acute but reversible heart failure.
What happens if I overdose?
Seek emergency medical attention.
Can Xaloplat affect my kidneys?
Xaloplat is an experimental anti-cancer drug that can shrink tumors such as colon cancer. However, because this drug can damage the kidneys, it is necessary to determine what doses of the drug can safely be given to patients with poor kidney function.
Can Xaloplat affects my heart ?
Xaloplat is able to induce coronary vasoconstriction leading to acute but reversible heart failure.
Will Xaloplat affect my fertility?
The risk for infertility and hypogonadism in males and females after adjuvant oxaliplatin-based chemotherapy seems to be low to moderate, but the general recommendation of appropriate fertility conserving measures shall should not be changed.
