An Erlonat tablets comprising of active component known as Erlotinib, which is considered as quinazoline derivative and anti-cancer agents that responses as a protein kinase prohibitors for EGFR related to tyrosine kinase Erlotinib is majorly used in the treatment of non-small cell lung cancer and pancreatic carcinoma and also involved to treat various cancers. Erlotinib is especially aimed the epidermal growth factor receptor tyrosine kinase. Cyclin dependent kinase are protein kinases, it should be characterised by the support of subunit as cyclin.
Erlonat tablets are used in the conditions like;
Non small cell lung cancer
Erlonat is used as continuance therapy, in patients with long lasting or metastasis non small cell lung carcinoma, whose disease has not get advance after four cycles with platinum based first line therapy. Erlonat is used in this condition only after the failure of one prior chemotherapy regimen. No clinical advantages occur while using Erlonat with platinum based compounds like carboplatin, gemcitabine or cisplatin.
Erlonat is used concurrently with gemcitabine, in this condition of metastatic pancreatic carcinoma.
The usual recommended dosage of Erlonat is 150mg should be administered as a single dose by taking in an empty stomach for at least one hour earlier or two hours after intake of food. Therapy with Erlonat should be continued until the disease advanced or undesirable toxicity occurs. It is not confirmed that the advancement after the therapy is beneficial or not.
In pancreatic cancer:
The daily usual recommended dosage of Erlonat in pancreatic carcinoma is 100mg should be taken on an empty stomach as a single dose. In this condition Erlonat is combined with gemcitabine.
In case of patients suffered with pulmonary symptoms like dyspnea, fever, cough, or any other conditions, Erlonat treatment should be discontinued. In interstitial lung disease: To avoid the Erlonat therapy. In case of gastrointestinal perforation or hepatic failure: Post pone or discontinue the Erlonat treatment. If diarrhea occurs during the therapy, substitute with loperamide for managing this condition. If dosage reduction is necessary then the dose of Erlonat reduced into 50mg. Dose reduction is essential in the condition, while concomitant of Erlonat with strong CYP3A4 inhibitors like atazanavir, clarithromycin, indinavir, itraconazole, ketaconazole, voriconazole, grape fruit juice etc. Dosage elevation occurs in case of concurrent use of Erlonat with strong CYP3A4 inducers like rifampin, rifampicin, anti-convulsants etc. The dosage should be increased by 50mg. In chain smoking conditions, increase the dose of Erlotinib into 50mg at two intervals to higher dose of 300mg. Then the dose is suddenly reduced to 100mg or 150mg in discontinuation of smoking. Erlonat should not be administered with gastric regulators drug, like proton pump inhibitors or H2 receptor antagonist. In H2 receptors antagonist: Administer Erlonat at least 10 hours after or 2 hours before H2 receptors antagonist. In proton pump inhibitors: Do not use concurrently if possible.
Severe renal impairment
Concurrent severe diarrhea
Worsening of ocular disorders
Elevation of billirubin levels
Evaluation of ILD
Erlonat has pharmacological effects like anti-neoplastic activity, which exhibits its action by inhibiting the intracellular phosphorylation of tyrosine kinase related with (EGFR) epidermal growth factor receptor. This EGFR signaling pathway is present on the surface of the tumor cells, this EGFR signaling is a critical pathway that involves in the treatment of effective cancer therapies. Thus results as inhibition causes interfere with signal transduction and lead to cell lyses.
The peak plasma concentration time reaches at 4 hours after drug intake After an oral administration of Erlonat, causes 60% of oral bioavailability. Increased by meals to 100%. The solubility of Erlotinib is depends upon pH level. If solubility decreases then leads to increasing pH levels. Smoking should be avoided during the treatment with Erlonat, causes decreasing the exposure of Erlotinib. The apparent volume of distribution of Erlotinib is 232L Human protein binding to Erlotinib is occurs as 93%. The metabolism of Erlotinib is occurs by CYP3A4 The route of elimination of Erlotinib metabolites occurs via; Feces: 83%; urine: 8% half life period of Erlotinib is 36.2 hours.
Pulmonary toxicity: Interstitial lung disease and other pulmonary toxicity conditions, Avoid the treatment with Erlonat Renal failure: Frequent monitoring of renal function or serum electrolytes occurs or avoids the treatment. Hepatic failure: Hepatic function should be periodically monitored, or otherwise discontinue the therapy with Erlonat. Gastro intestinal perforation: In this condition, discontinue the Erlonat therapy permanently. This condition is occurs due to concurrent use of Erlonat with NSAIDS, anti-angiogenic drugs, corticosteroids, taxane based chemotherapy or other drugs etc. Bullous & exfoliative skin disorders Myocardial infarction or Ischemia Cerebrovascular accident Ocular disorder Elevation of bleeding while concurrent use with warfarin Hemolytic anemia or thrombocytopenia In pregnancy condition In all these condition, treatment using with Erlonat should be avoided.
Co administration of Erlonat with CYP3A4 strong inhibitors like ketaconazole causes increasing Erlotinib exposure. Erlonat concurrently used with ciprofloxacin, CYP3A4 & CYP1A2 inhibitor causes elevation of exposure of Erlotinib. CYP3A4 strong inhibitors like itraconazole, grape fruit juice, rotonavir, indinavir etc CYP3A4 inducers concurrently used with Erlonat tablets causes decreasing the exposure of Erlotinib. CYP3A4inducers like, rifampin, rifampicin, carbamazepine, phenytoin etc Cigarette smoking is decreasing the AUC of Erlotinib. Co administration of Erlonat with midazolam causes decreasing the AUC of CYP3A4 substrate. Drugs involved in alteration of pH levels causes variation in solubility of Erlotinib. Avoid concomitant use of gastric regulators with Erlonat. Avoid concomitant use of warfarin with Erlonat, causes increasing the bleeding condition. Erlonat concomitant with statins drugs (lipid lowering drug), causes increasing the concentration of these drugs (rosuvastatin, simvastatin or atorvastatin).
In case of missed dose, patients must consult with medical oncologist and follow the regular dosing schedule.
In case of over dosage, Erlonat therapy should be postponed and symptomatic treatment should be recommended.
No breast feeding is recommended
Erlonat has effective and potency in elder patients who are failure to treat with platinum based compounds.
Erlonat tablets should be stored at 25 0C (77 0 F). Protect from light, heat & moisture
Erlonat has effective and potency in elder patients who are failure to treat List of various erlotinib side ffects as sycg as,
Some common various erlotinib side effects are
Loss of weight,
Renal disorders, hepatic disorders, ocular disorders, skin, hair and nail disorders.
During the therapy, some undesirable effects like; Paronychia, Bulbous, blistering and exploitative skin conditions like Stevens Johnson’s syndrome. Gastrointestinal perforation, Hepatic failure occurs during monotherapy or combination with other chemotherapy agents.
Pregnancy category: D Erlonat should not be used in pregnancy condition
The potency of Erlotinib and its effectiveness has not been established in pediatric patients
In Erlonat therapy, no contraindication occurs. In some patients hypersensitivity reactions present due to patients are contraindicated to the ingredients in Erlonat.
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