Irinotecan HCl trihydrate (Irinotecan HCl trihydrate) is a cancer medicine that interferes with the growth and spread of cancer cells in the body.
Irinotecan HCl trihydrate is used to treat cancers of the colon and rectum. It is usually given with other cancer medicines in a combination chemotherapy.
Irinotecan HCl trihydrate may also be used for purposes not listed in this medication guide.
Irinotecan HCl trihydrate indications
An indication is a term used for the list of condition or symptom or illness for which the medicine is prescribed or used by the patient. For example, acetaminophen or paracetamol is used for fever by the patient, or the doctor prescribes it for a headache or body pains. Now fever, headache and body pains are the indications of paracetamol. A patient should be aware of the indications of medications used for common conditions because they can be taken over the counter in the pharmacy meaning without prescription by the Physician.
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Irinotecan HCl trihydrate is indicated as a component of first-line therapy for patients with metastatic carcinoma of the colon or rectum. Irinotecan HCl trihydrate is also indicated for patients with metastatic carcinoma of the colon or rectum whose disease has recurred or progressed following initial therapy.
How should I use Irinotecan HCl trihydrate?
Use Irinotecan HCl trihydrate as directed by your doctor. Check the label on the medicine for exact dosing instructions.
Irinotecan HCl trihydrate is usually given as an injection at your doctor's office, hospital, or clinic. If you will be using Irinotecan HCl trihydrate at home, a health care provider will teach you how to use it. Be sure you understand how to use Irinotecan HCl trihydrate. Follow the procedures you are taught when you use a dose. Contact your health care provider if you have any questions.
Do not use Irinotecan HCl trihydrate if it contains particles, is cloudy or discolored, or if the vial is cracked or damaged.
Drink plenty of water and other clear liquids while using Irinotecan HCl trihydrate.
If you spill Irinotecan HCl trihydrate on your skin, wash it off right away with soap and water.
Keep this product, as well as syringes and needles, out of the reach of children and pets. Do not reuse needles, syringes, or other materials. Ask your health care provider how to dispose of these materials after use. Follow all local rules for disposal.
If you miss a dose of Irinotecan HCl trihydrate, contact your doctor right away.
Ask your health care provider any questions you may have about how to use Irinotecan HCl trihydrate.
Uses of Irinotecan HCl trihydrate in details
There are specific as well as general uses of a drug or medicine. A medicine can be used to prevent a disease, treat a disease over a period or cure a disease. It can also be used to treat the particular symptom of the disease. The drug use depends on the form the patient takes it. It may be more useful in injection form or sometimes in tablet form. The drug can be used for a single troubling symptom or a life-threatening condition. While some medications can be stopped after few days, some drugs need to be continued for prolonged period to get the benefit from it.
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This medication is used to treat cancer of the colon and rectum.
OTHER USES: This section contains uses of this drug that are not listed in the approved professional labeling for the drug but that may be prescribed by your health care professional. Use this drug for a condition that is listed in this section only if it has been so prescribed by your health care professional.
This drug may also be used to treat other types of cancer (such as lung, bone cancer).
How to use Irinotecan HCl trihydrate intravenous
This medication is given by injection into a vein by a health care professional. The dosage is based on your medical condition, body size, and response to treatment.
If this medication comes into contact with your skin, wash the skin right away and completely with soap and water. If this medication gets into your eyes, mouth, or nose, flush completely with plenty of water. Consult your doctor for more details.
Irinotecan HCl trihydrate description
Chemical name: (4S)-4,11-diethyl-4-hydroxy-9-[(4-piperidinopiperidino)carbonyloxy]-1H- pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H) dione hydrochloride trihydrate.
Irinotecan HCl trihydrate is an antineoplastic agent of the topoisomerase I inhibitor class.
Irinotecan HCl trihydrate hydrochloride is a semisynthetic derivative of camptothecin, an alkaloid extract from plants such as Camptotheca acuminata. It is a pale yellow to yellow crystalline powder, with the empirical formula C33H38N4O6·HCl·3H2O and a molecular weight of 677.19. Irinotecan HCl trihydrate hydrochloride is slightly soluble in water and organic solvents.
Irinotecan HCl trihydrate has a pH of 3.5. It is intended for dilution with 5% Glucose Injection or 0.9% Sodium Chloride Injection prior to infusion. The 2 mL and 5 mL injections contain 40 mg and 100 mg of Irinotecan HCl trihydrate hydrochloride trihydrate respectively.
Excipients/Inactive Ingredients: Sorbitol and lactic acid. Sodium chloride and hydrochloric acid are used for pH adjustment.
Irinotecan HCl trihydrate dosage
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It is recommended that patients receive premedication with anti-emetic agents. Prophylactic or therapeutic administration of atropine should be considered in patients experiencing cholinergic symptoms.
Combination Therapy in First Line Treatment of Metastatic Colorectal Cancer: Irinotecan HCl trihydrate should be ad ministered as an intravenous infusion (IV) over 90 minutes. For all regimens, the dose of LV should be administered immediately after Irinotecan HCl trihydrate, with the administration of fluorouracil to follow immediately after the administration of LV. The recommended regimens are shown in Table 7.
Dosing for patients with bilirubin >34 mmol/L cannot be recommended since such patients were not included in clinical trials.
Irinotecan HCl trihydrate in Combination with Cetuximab: For dosage and administration of concomitant cetuximab, refer to the full prescribing information for cetuximab. Normally, the same dose of Irinotecan HCl trihydrate is used as administered in the last cycles of the prior Irinotecan HCl trihydrate-containing regimen. Irinotecan HCl trihydrate must not be administered earlier than 1 hour after the end of the cetuximab infusion.
Dose Modifications: Patients should be carefully monitored for toxicity and assessed prior to each treatment, especially during the first cycle of therapy. Doses of Irinotecan HCl trihydrate and fluorouracil should be modified as necessary to accommodate individual patient tolerance to treatment. Based on the recommended dose levels described in Table 7, subsequent doses should be adjusted as suggested in Table 8, which shows the recommended dose modifications for combination schedules. All dose modifications should be based on the worst preceding toxicity. Patients should be diarrhoea free (return to pre treatment bowel function) without requiring antidiarrhoeal medications for at least 24 hours before receiving the next chemotherapy administration.
A new cycle of therapy should not begin until the toxicity has recovered to NCI grade 1 or less, the granulocyte count has recovered to ≥1.5 x 109/L, the platelet count has recovered to ≥100 x 109/L and treatment-related diarrhoea is fully resolved. Treatment should be delayed for 1 to 2 weeks to allow recovery from treatment-related toxicity. If the patient has not recovered after a 2 week delay, consideration should be given to discontinuing therapy. Provided intolerable toxicity does not develop, treatment with additional cycles of Irinotecan HCl trihydrate/fluorouracil/LV may be continued indefinitely as long as patients continue to experience clinical benefit.
Single Agent Therapy in Recurrent or Progressive Metastatic Colorectal Cancer: Irinotecan HCl trihydrate should be administered as an intravenous infusion over 90 minutes in a recommended weekly or once every 3 week dosage schedule as shown as follows..
A reduction in the starting dose by one level of Irinotecan HCl trihydrate may be considered for patients with any of the following circumstances: over 65 years, prior pelvic/abdominal radiotherapy, performance status of 2 or moderately increased bilirubin levels (17-34 mmol/L). Dosing for patients with bilirubin >34 mmol/L cannot be recommended since such patients were not included in clinical trials.
Dose Modifications: Patients should be carefully monitored for toxicity and doses of Irinotecan HCl trihydrate should be modified as necessary to accommodate individual patient tolerance to treatment. Based on recommended dose-levels described in Table 9, subsequent doses of Irinotecan HCl trihydrate should be adjusted as suggested in Table 10. All dose modifications should be based on the worst preceding toxicity.
A new cycle of therapy should not begin until the toxicity has recovered to NCI grade 1 or less, the granulocyte count has recovered to ≥1.5 x 109/L, the platelet count has recovered to ≥100 x 109/L and treatment-related diarrhoea is fully resolved. Treatment may be delayed for 1 to 2 weeks to allow recovery from treatment-related toxicity. If the patient has not recovered, consideration should be given to discontinuing Irinotecan HCl trihydrate therapy. Provided intolerable toxicity does not develop, treatment with additional cycles of Irinotecan HCl trihydrate may be continued indefinitely as long as patients continue to experience clinical benefit.
Neuromuscular Blocking Agents: Interaction between Irinotecan HCl trihydrate and neuromuscular blocking agents cannot be ruled out, since Irinotecan HCl trihydrate has anticholinesterase activity. Drugs with anticholinesterase activity may prolong the neuromuscular blocking effects of suxamethonium and the neuromuscular blockade of non-depolarizing drugs may be antagonized.
Antineoplastic Agents: The adverse effects of Irinotecan HCl trihydrate eg, myelosuppression and diarrhoea, would be expected to be exacerbated by other antineoplastic agents having a similar adverse effect profile.
Dexamethasone: Lymphocytopenia has been reported in patients receiving Irinotecan HCl trihydrate, and it is possible that the administration of dexamethasone as antiemetic prophylaxis may have enhanced the likelihood of lymphocytopenia. However, serious opportunistic infections have not been observed and no complications have specifically been attributed to lymphocytopenia.
Hyperglycemia has been observed in patients with a history of diabetes mellitus or evidence of glucose intolerance prior to administration of Irinotecan HCl trihydrate. It is probable that dexamethasone, given as antiemetic prophylaxis, contributed to hyperglycemia in some patients.
Laxatives: Laxative use during therapy with Irinotecan HCl trihydrate is expected to worsen the incidence or severity of diarrhea.
Diuretics: Dehydration secondary to vomiting and/or diarrhea may be induced by Irinotecan HCl trihydrate. The physician may wish to withhold diuretics during dosing with Irinotecan HCl trihydrate and during periods of active vomiting or diarrhea.
Anticonvulsants: Concomitant administration of CYP3A-inducing anticonvulsant drugs (eg, carbamazepine, phenobarbital or phenytoin) leads to reduced exposure to the active metabolite SN-38. Consideration should be given to starting or substituting non-enzyme-inducing anticonvulsants at least 1 week prior to initiation of Irinotecan HCl trihydrate therapy in patients requiring anticonvulsant treatment.
Ketoconazole: Irinotecan HCl trihydrate clearance is greatly reduced in patients receiving concomitant ketoconazole, leading to increased exposure to SN-38. Ketoconazole should be discontinued at least 1 week prior to starting Irinotecan HCl trihydrate therapy and should not be administered during Irinotecan HCl trihydrate therapy.
St. John's Wort (Hypericum perforatum): Exposure to the active metabolite, SN-38, is reduced in patients taking concomitant St. John's wort.
St. John's wort should be discontinued at least 1 week prior to the 1st cycle of Irinotecan HCl trihydrate and should not be administered during Irinotecan HCl trihydrate therapy.
Atazanavir Sulfate: Co-administration of atazanavir sulfate, a CYP3A4 and UGT1A1 inhibitor has the potential to increase systemic exposure to SN-38, the active metabolite of Irinotecan HCl trihydrate.
Physicians should take this into consideration when co-administering these drugs.
Bevacizumab: Results from a dedicated drug-drug interaction trial demonstrated no significant effect of bevacizumab on the pharmacokinetics of Irinotecan HCl trihydrate and theits active metabolite SN-38.
Incompatibilities: Other drugs should not be added to the infusion solution.
Clinical Studies: Adverse reaction data has been extensively collected and analyzed for the clinical studies program in metastatic colorectal cancer that recurred or progressed following 5-FU-based therapy (2nd-line) and are presented as follows (patient population described as follows). The adverse reactions for other indications are expected to be similar to those for 2nd-line colorectal cancer.
Adverse reactions detailed in this section refer to Irinotecan HCl trihydrate. There is no evidence that the safety profile of Irinotecan HCl trihydrate is influenced by cetuximab or vice versa. In combination with cetuximab, additional reported adverse reactions were those expected with cetuximab (eg, acneform rash). Therefore, also refer to the full prescribing information for cetuximab.
Grade 3 hypertension was the principal significant risk involved with the addition of bevacizumab to bolus Irinotecan HCl trihydrate/5-FU/FA. In addition, there was a small increase in the grade 3/4 chemotherapy adverse events of diarrhea and leucopenia with this regimen compared to patients receiving bolus Irinotecan HCl trihydrate/5-FU/FA alone. For other information on adverse reactions in combination with bevacizumab, refer to the bevacizumab full prescribing information.
Adverse drug reactions reported in patients treated with the combination Irinotecan HCl trihydrate plus capecitabine in addition to those seen with capecitabine monotherapy or seen at a higher frequency grouping with the combination compared to capecitabine monotherapy include: Very Common (All Grade): Thrombosis/embolism. Common (All Grade): Hypersensitivity reaction, cardiac ischemia/infarction. Common (Grade 3 and 4): Febrile neutropenia.
For complete information on adverse reactions of capecitabine, refer to the capecitabine full prescribing information.
Grade 3 and grade 4 adverse drug reactions reported in patients treated with Irinotecan HCl trihydrate in combination with capecitabine and bevacizumab in addition to those seen with capecitabine monotherapy or seen at a higher frequency grouping with the combination compared to capecitabine monotherapy include: Common, Grade 3 and Grade 4: Neutropaenia, thrombosis/embolism, hypertension and cardiac ischemia/infarction.
For complete information on adverse reactions of capecitabine and bevacizumab, refer to the respective capecitabine and bevacizumab full prescribing information.
Clinical Studies of the 100- to 125-mg/m2 Single-Agent Weekly Dosage Schedule: The weekly dosage schedule of Irinotecan HCl trihydrate was evaluated in 3 clinical studies of 304 patients with metastatic carcinoma of the colon or rectum that had recurred or progressed following 5-FU-based therapy. Five (1.6%) deaths were potentially drug-related. These 5 patients experienced a constellation of medical events (myelosuppression, neutropenic sepsis without fever, small bowel obstruction, fluid accumulation, stomatitis, nausea, vomiting, diarrhea and dehydration) that are known effects of Irinotecan HCl trihydrate. Neutropenic fever, defined as NCI grade 4 neutropenia and grade 2 or greater fever, occurred in 9 other patients; these patients recovered with supportive care.
Eighty-one (26.6%) patients were hospitalized for events judged to be related to administration of Irinotecan HCl trihydrate. The primary reasons for drug-related hospitalization were diarrhea, with or without nausea and/or vomiting; neutropenia/leucopenia, with or without diarrhea and/or fever; and nausea and/or vomiting.
Adjustments in the dose of Irinotecan HCl trihydrate were made during the cycle of treatment and for subsequent cycles based on individual patient tolerance. The most common reasons for dose reduction were late diarrhea, neutropenia and leucopenia. Thirteen (4.3%) patients discontinued treatment with Irinotecan HCl trihydrate because of adverse events.
Clinical Studies of the 300- to 350-mg/m2 Once-Every-3-Week Single-Agent Dosage Schedule: A total of 316 patients with metastatic colorectal cancer whose disease had progressed following prior 5-FU therapy received Irinotecan HCl trihydrate in 2 studies involving once-every-3-week administration. Three (1%) deaths were potentially related to Irinotecan HCl trihydrate treatment and were attributed to neutropenic infection, grade 4 diarrhoea and aesthenia, respectively. Hospitalizations due to serious adverse events, whether or not related to Irinotecan HCl trihydrate administration, occurred at least once in 60% of patients who received Irinotecan HCl trihydrate and 8% of patients treated with Irinotecan HCl trihydrate discontinued treatment due to adverse events.
Listing of Adverse Events: The drug-related adverse events (NCI grades 1-4) as judged by the investigator that were reported in >10% of the 304 patients enrolled in the 3 studies of the weekly dosage schedule are listed by body system in descending order of frequency as follows.
NCI Grade 1-4 Drug-Related Adverse Events Observed in >10% of Patients in Clinical Studies: Gastrointestinal Disorders: Late diarrhea, nausea, vomiting, early diarrhea, abdominal cramping/pain, anorexia, stomatitis.
Blood and Lymphatic System Disorders: Leucopenia, anemia, neutropenia.
General Disorders and Administration Site Conditions: Aesthenia, fever.
Metabolism and Nutrition Disorders: Decreased weight, dehydration.
NCI grade 3 or 4 adverse events reported in the clinical studies of the weekly and once-every-3-week-dosage schedules (N=620) are listed as follows.
NCI Grade 3 or 4 Drug-Related Adverse Events Observed in >10% of Patients in Clinical Studies: Gastrointestinal Disorders: Late diarrhoea, nausea, abdominal cramping/pain.
Blood and Lymphatic System Disorders: Leucopenia, neutropenia.
Skin and Subcutaneous Tissue Disorders: Alopecia.
NCI Grade 3 or 4 Drug-Related Adverse Events Observed in 1-10% of Patients in Clinical Studies: Infections and Infestations: Infection.
Gastrointestinal Disorders: Vomiting, early diarrhea, constipation, anorexia, mucositis.
Blood and lymphatic System Disorders: Anemia, thrombocytopenia.
General Disorders and Administration Site Conditions: Aesthenia, fever, pain.
Metabolism and Nutrition Disorders: Dehydration, hypovolemia.
Hepatobiliary Disorders: Bilirubinemia.
Respiratory, Thoracic and Mediastinal Disorders: Dyspnea.
Investigations: Increased creatinine.
NCI Grade 3 or 4 Drug-Related Adverse Events Observed in <1% of Patients in Clinical Studies: Infections and Infestations: Sepsis.
Renal and Urinary Disorders: Urinary tract infection.
Reproductive System and Breast Disorders: Breast pain.
Investigations: Increased alkaline phosphatase and γ-glutamyl transferase.
The following additional drug-related events have been reported in clinical studies with Irinotecan HCl trihydrate, but do not meet the criteria as defined previously as either >10% drug-related NCI grades 1-4 or as a NCI grade 3 or 4 drug-related event: Rhinitis, increased salivation, miosis, lacrimation, diaphoresis, flushing, bradycardia, dizziness, extravasation, tumor lysis syndrome and colonic ulceration.
Post-Marketing Surveillance: Cardiac Disorders:Myocardial ischemic events have been observed following Irinotecan HCl trihydrate therapy predominantly in patients with underlying cardiac disease, other known risk factors for cardiac disease or previous cytotoxic chemotherapy.
Gastrointestinal Disorders: Infrequent cases of intestinal obstruction, ileus, megacolon or gastrointestinal hemorrhage and rare cases of colitis, including typhlitis, ischemic and ulcerative colitis were reported. In some cases, colitis was complicated by ulceration, bleeding, ileus or infection. Cases of ileus without preceding colitis have also been reported. Rare cases of intestinal perforation were reported.
Rare cases of symptomatic pancreatitis or asymptomatic elevated pancreatic enzymes have been observed.
Hypovolemia: There have been rare cases of renal impairment and acute renal failure, generally in patients who became infected and/or volume depleted from severe gastrointestinal toxicities.
Infrequent cases of renal insufficiency, hypotension or circulatory failure have been observed in patients who experienced episodes of dehydration associated with diarrhea and/or vomiting or sepsis.
Immune System Disorders: Hypersensitivity reactions including severe anaphylactic or anaphylactoid reactions have been reported.
Musculoskeletal and Connective Tissue Disorders: Early effects eg, muscular contraction or cramps and paresthesia have been reported.
Nervous System Disorder: Speech disorders, generally transient in nature, have been reported in patients treated with Irinotecan HCl trihydrate; in some cases, the event was attributed to the cholinergic syndrome observed during or shortly after infusion of Irinotecan HCl trihydrate.
Respiratory, Thoracic and Mediastinal Disorders: Interstitial pulmonary disease presenting as pulmonary infiltrates is uncommon during Irinotecan HCl trihydrate therapy. Early effects eg, dyspnea have been reported. Hiccups have also been reported.
Investigations: Rare cases of hyponatremia mostly related with diarrhea and vomiting have been reported. Increases in serum levels of transaminases (ie, AST and ALT) in the absence of progressive liver metastasis have been very rarely reported.
Laboratory Tests: Monotherapy: Increases in serum levels of either transaminases (ie, AST and ALT), alkaline phosphatase or bilirubin were observed in 9.2%, 8.1% and 1.8% of the patients, respectively, in the absence of progressive liver metastasis have been very rarely reported.
Transient and mild to moderate increases of serum levels of creatinine have been observed in 7.3% of the patients.
Combination Therapy: Transient serum levels (grades 1 and 2) of either SGPT, SGOT, alkaline phosphatase or bilirubin were observed in 15%, 11%, 11% and 10% of the patients, respectively, in the absence of progressive liver metastasis. Transient grade 3 was observed in 0%, 0%, 0% and 1% of the patients, respectively. No grade 4 was observed.
Increases of amylase and/or lipase have been rarely reported.
Rare cases of hypokalemia and hyponatremia mostly related with diarrhea and vomiting have been reported.
Irinotecan HCl trihydrate is contraindicated in patients with a known hypersensitivity to the drug or its excipients. Irinotecan HCl trihydrate antigenicity has not been observed in clinical trials, but Irinotecan HCl trihydrate hydrochloride antigenicity occurred in tests for passive cutaneous anaphylaxis in guinea pigs and rabbits, and in tests for active systemic anaphylaxis in guinea pigs. In these tests, both animal species produced antibodies against Irinotecan HCl trihydrate hydrochloride, and some deaths occurred in guinea pigs sensitised to Irinotecan HCl trihydrate hydrochloride.
Irinotecan HCl trihydrate is contraindicated in women who intend to become pregnant.
Irinotecan HCl trihydrate is contraindicated in pregnancy and lactation.
Active ingredient matches for Irinotecan HCl trihydrate:
Irinotecan HCl trihydrate
List of Irinotecan HCl trihydrate substitutes (brand and generic names)
DTP/NCI. "irinotecan: The NCI Development Therapeutics Program (DTP) provides services and resources to the academic and private-sector research communities worldwide to facilitate the discovery and development of new cancer therapeutic agents.". https://dtp.cancer.gov/dtpstandard/s... (accessed September 17, 2018).
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