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APO-ERLOTINIB is a brand name for Erlotinib, supplied as a tablet. The medicine, its uses, side effects and dosage are the same regardless of brand.
Used for: AND CLINICAL USE ..................................................................................... 3 CONTRAINDICATIONS .......................................................................................................... 4 WARNINGS AND PRECAUTIONS…
Verbatim from this product's HC label. Tap a section to expand.
EGFR mutation testing should be performed and EGFR mutation-positive status must be confirmed prior to initiation of APO-ERLOTINIB as first-line, second line or maintenance therapy in patients with locally advanced or metastatic NSCLC.
The recommended daily dose of APO-ERLOTINIB is 150 mg taken orally with a glass of plain water, at least one hour before or two hours after the ingestion of food. Dosage Adjustment When dose reduction is necessary, it is recommended to reduce in 50 mg steps.
Diarrhea can mostly be managed by loperamide. Patients with severe diarrhea that are unresponsive to loperamide or associated with dehydration may require a dose reduction or temporary interruption of therapy. Patients with severe skin reactions may also require a dose reduction or temporary interruption of therapy (see WARNINGS AND PRECAUTIONS).
In patients who develop acute onset of new and/or progressive unexplained pulmonary symptoms, such as dyspnea, cough and fever, APO-ERLOTINIB therapy should be interrupted pending diagnostic evaluation. If ILD is diagnosed, APO-ERLOTINIB should be discontinued and appropriate treatment initiated as necessary (see WARNINGS AND PRECAUTIONS).
In patients being concomitantly treated with a potent CYP3A4 inhibitor such as, but not limited to, ketoconazole, itraconazole, voriconazole, clarithromycin, telithromycin, troleandomycin, or atanazavir, a dose reduction should be considered in the presence of severe adverse events (see DRUG INTERACTIONS).
Dosing Considerations Hepatic impairment:
Erlotinib is eliminated by hepatic metabolism and biliary excretion. Although erlotinib exposure following a single 150 mg was similar in patients with moderately impaired hepatic function (Child-Pugh score 7 to 9) compared with patients with adequate hepatic function, ten of the fifteen patients with hepatic impairment died during treatment or within 30 days of the last dose of erlotinib.
A reduced dose should be considered for patients with moderate hepatic impairment. Hepatic function should be closely monitored in patients with pre-existing liver disease, hepatic impairment and/or taking concomitant hepatotoxic medications.
APO-ERLOTINIB dosing should be interrupted or discontinued if significant changes in liver function tests are observed. The use of APO-ERLOTINIB in patients with severe hepatic dysfunction including total bilirubin of > 3 x ULN and/or transaminases of > 5 x ULN is not recommended (see WARNINGS AND PRECAUTIONS, Special Populations and Conditions - Patients with Hepatic Impairment) Renal impairment: The safety and efficacy of erlotinib has not been studied in patients with Page 19 of 43 renal impairment.
Not medical advice. Always read the patient information leaflet and follow your prescriber or pharmacist.
Other brands of Erlotinib in Canada.
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Brand names are compiled from public regulatory records for active-ingredient mapping only. Drugvu is not affiliated with any manufacturer. This is not medical advice.
Geriatric use:
No meaningful differences in safety or pharmacokinetics were observed between younger and older patients, therefore, no dosing adjustment is necessary.
Smokers:
Cigarette smoking has been shown to reduce erlotinib exposure by 50 to 60%. The maximum tolerated dose of APO-Erlotinib in NSCLC patients who concurrently smoked cigarettes was 300 mg. Efficacy and long term safety of a dose higher than the recommended 150 mg has not been established in patients who continue to smoke cigarettes (see DRUG INTERACTIONS - Drug-Lifestyle Interactions).
Missed Dose A double-dose should not be administered to make up for forgotten individual doses. Special Instructions for Disposal THE RELEASE OF PHARMACEUTICALS IN THE ENVIRONMENT SHOULD BE MINIMIZED. MEDICINES SHOULD NOT BE DISPOSED OF VIA WASTEWATER AND DISPOSAL THROUGH HOUSEHOLD WASTE SHOULD BE AVOIDED.
ANY UNUSED MEDICINAL PRODUCT OR WASTE MATERIAL SHOULD BE DISPOSED OF IN ACCORDANCE WITH LOCAL REQUIREMENTS. OVERDOSAGE For management of a suspected drug overdose, contact your regional Poison Control Centre immediately. Single oral doses of erlotinib up to 1000 mg in healthy subjects, and up to 1600 mg given as a single dose once weekly in cancer patients have been tolerated.
Repeated twice daily doses of 200 mg in healthy subjects were poorly tolerated after only a few days of dosing. Based on the data from these studies, severe adverse events such as diarrhea, rash and possibly liver transaminase elevation may occur above the recommended dose of 150 mg.
In case of suspected overdose, APO-ERLOTINIB should be withheld and symptomatic treatment initiated. ACTION AND CLINICAL PHARMACOLOGY Erlotinib is a Human Epidermal Growth Factor Receptor Type 1/Epidermal Growth Factor Receptor (HER1/EGFR) tyrosine kinase inhibitor.
Mode of Action:
The mechanism of clinical antitumour action of erlotinib is not fully characterized. Erlotinib potently inhibits the intracellular phosphorylation of HER1/EGF receptor. HER1/EGF receptor is expressed on the cell surface of normal cells and cancer cells.
Specificity of erlotinib inhibition on other tyrosine kinase receptors of the ErbB family has not Page 20 of 43 been characterized.
Pharmacokinetics Absorption:
Oral erlotinib is well absorbed and has an extended absorption phase, with mean peak plasma levels occurring at 4 hours after oral dosing. A study in normal healthy volunteers provided an estimate of bioavailability of 59%. The exposure after an oral dose may be increased by food.
e. albumin and alpha-1 acid glycoprotein [AAG]), with a free fraction of approximately 5%.
Distribution:
Erlotinib has a mean apparent volume of distribution of 232 L and distributes into tumour tissue of humans. In a study of 4 patients (3 with non-small cell lung cancer [NSCLC], and 1 with laryngeal cancer) receiving 150 mg daily oral doses of erlotinib, tumour samples from surgical excisions on Day 9 of treatment revealed tumour concentrations of erlotinib that averaged 1,185 ng/g of tissue.
This corresponded to an overall average of 63% of the steady state observed peak plasma concentrations. The primary active metabolites were present in tumours at […]