Trade name : Erlocip
Active ingredient : Erlotinib
Strength : 150mg
Manufactured by : Cipla
Pack : 30 tablets in a container
Erlocip tablets consist of active ingredients known as Erlotinib (Generic Tarceva), that is considered as quinazoline derivative and anti-cancer agents that responses as a protein kinase prohibitors for EGFR related to tyrosine kinase. Erlocip is majorly used in the treatment of non-small cell lung cancer and pancreatic carcinoma and also involved to treat various cancers. Erlocip is especially aimed the epidermal growth factor receptor tyrosine kinase.
USES OF Erlocip
Non small cell lung cancer:
Erlocip is indicated 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. Erlocip is used in this condition only after the failure of one prior chemotherapy regimen. No clinical advantages occur while using Erlocip with platinum based compounds like Carboplatin, gemcitabine or cisplatin.
Erlocip (Erlotinib Hydrochloride) is indicated for the treatment concurrently with gemcitabine, gemcitabine is a chemotherapy drug used to treat the cancer of ovary, breast, pancreas, bladder and non small cell lung cancer. Cisplatin is also a chemotherapic drug used for the treatment of various types of cancer.
Erlotinib mechanism of action
The mechanism of clinical action of erlotinib is not fully revealed/characterised, Erlocip has pharmacological effects like anti-neoplastic activity, which exhibits its action by inhibiting the intracellular phosphorylation of tyrosine kinase related with epidermal growth factor receptor. This EGFR is present on the surface of the tumor cells, the main ingredient which is used as erlotinib. Thus results as inhibition causes interfere with signal transduction and lead to cell lyses.
In case of patients suffered with pulmonary symptoms like dyspnea, fever, cough, or any other conditions, Erlocip treatment should be discontinued. In interstitial lung disease: To avoid the Erlocip therapy. In case of gastrointestinal perforation or hepatic failure: Post pone or discontinue the Erlocip treatment. If diarrhea occurs during the therapy, substitute with loperamide for managing this condition. If dosage reduction is necessary then the dose of Erlocip reduced into 50mg. Dose reduction is essential in the condition, while concomitant of Erlocip with strong CYP3A4 inhibitors like atazanavir, clarithromycin, indinavir, itraconazole, ketaconazole, voriconazole, grape fruit juice etc. Dosage elevation occurs in case of concurrent use of Erlocip with strong CYP3A4 inducers like rifampin, rifampicin, anti-convulsants etc. The dosage should be increased by 50mg. In chain smoking conditions, increase the Erlotinib dose into 50mg at two intervals to higher dose of 300mg. Then the dose is suddenly reduced to 100mg or 150mg in discontinuation of smoking. Erlocip should not be administered with gastric regulators drug, like proton pump inhibitors or H2 receptor antagonist. In H2 receptors antagonist: Administer Erlocip at least 10 hours after or 2 hours before H2 receptors antagonist. In proton pump inhibitors: Do not use concurrently if possible.
The peak plasma concentration time reaches at 4 hours after drug intake After an oral administration of Erlocip, 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 Erlocip, 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.
DOSAGE AND ADMINISTRATION
The usual recommended dosage of Erlocip 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 Erlocip 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 Erlocip in pancreatic carcinoma is 100mg should be taken on an empty stomach as a single dose. In this condition Erlocip is combined with gemcitabine.
WARNING AND PRECAUTIONS
Pulmonary toxicity: Interstitial lung disease and other pulmonary toxicity conditions, Avoid the treatment with Erlocip Renal failure: Frequent monitoring of renal function or serum electrolytes occurs or avoids the treatment. 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 Erlocip should be avoided. Hepatic failure: Hepatic function should be periodically monitored, or otherwise discontinue the therapy with Erlocip. Gastro intestinal perforation: In this condition, discontinue the Erlocip therapy permanently. This condition is occurs due to concurrent use of Erlocip with NSAIDS, anti-angiogenic drugs, corticosteroids, taxane based chemotherapy or other drugs etc.
SOME INTERACTION WITH SOME OTHER DRUGS
Co administration of Erlocip 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 Erlocip. Avoid concomitant use of warfarin with Erlocip, causes increasing the bleeding condition. Co administration of Erlocip with CYP3A4 strong inhibitors like ketaconazole causes increasing Erlotinib exposure. Erlocip concomitant with statins drugs (lipid lowering drug), causes increasing the concentration of these drugs (rosuvastatin, simvastatin or atorvastatin). Erlocip concurrently used with ciprofloxacin, CYP3A4 & CYP1A2 inhibitor causes elevation of exposure of Erlotinib tablets. CYP3A4 strong inhibitors like itraconazole, grape fruit juice, rotonavir, indinavir etc CYP3A4 inducers concurrently used with Erlocip tablets causes decreasing the exposure of Erlotinib. CYP3A4inducers like, rifampin, rifampicin, carbamazepine, phenytoin etc Cigarette smoking is decreasing the AUC of Erlotinib.
ERLOTINIB SIDE EFFECTS
During the therapy, some undesirable effects like; Paronychia, Bullous, blistering and expoliative skin conditions like Stevens Johnson’s syndrome. Gastrointestinal perforation Hepatic failure occurs during monotherapy or combination with other chemotherapy agents Some common side effects of Erlotinib are Diarrhea, Fatigue, Anorexia, Pruritus, Acne, Dermatitis, Dry skin, Loss of weight, Paronychia, Cough, Vomiting, Conjunctivitis, Keratoconjuctivities sicca, Abdominal pain, Stomatits, Infection, nausea, Bone pain, Alopecia, Anxiety, Neuropathy, Renal disorders, hepatic disorders, ocular disorders, skin, hair and nail disorders
In case of over dosage, Erlocip therapy should be postponed and symptomatic treatment should be recommended.
In Erlocip therapy, no contraindication occurs. In some patients hypersensitivity reactions present due to patients are contraindicated to the ingredients in Erlocip.