Tarceva 150mg Roche medicine supports the treatment of lung cancer (3 blisters x 10 tablets)

Dosage form Box of 3 blisters x 10 tablets
Specifications Erlotinib

Ingredient

Composition information	Content
Erlotinib	150mg

Uses

indications

Tarceva drugs indicate treatment in the following cases:

Non -small cell lung cancer: Tarceva is indicated for maintenance treatment in non -small cell lung cancer patients (NSCLC) on -site or metastatic development that has not responded to chemotherapy. Tarceva is indicated to treat non -small cell lung cancer patients on the spot or metastasis after failure with at least one previous chemotherapy regime.

Pancreatic cancer: Tarceva in combination with gemcitabin is assigned to treat step one for patients with pancreatic cancer that progresses on the spot, unable to remove or metastasize.

Pharmacokology

Erlotinib inhibits strongly the internal cell phosphorylation of Her1/EGFR. Her1/EGFR is revealed on the surface of normal cells and cancer cells. In non -clinical models, the inhibition of EGFR phosphormosine causes inhibition and/or cell death.

pharmacokinetic

absorption

Erlotinib is well absorbed and has a towing section, with average plasma peaks achieved after drinking 4 hours.

A study in normal healthy volunteers shows that bioavailability is estimated at 59%. The concentration after drinking can increase by food,

After absorption, Erlotinib is high in the blood, about 95% associated with blood components, mainly with plasma proteins (for example, albumin and alpha-1 glycoprotein [AAG]), with about 5% in free form.

distribution

Erlotinib has an average distribution of 232L and distributed into the human tumor tissue. In a study of 4 patients (3 patients with non -small cell lung cancer (NSCLC), and a patient with laryngeal cancer) Tarceva daily -dose Tarceva 150 mg, a sample of tumor from surgery removed on the 9th day of treatment showed that Erlotinib concentration in the tumor reached an average of 1,185 ng/g.

This value corresponds to the general average value of 63% of plasma peak concentrations recorded in a stable state. The main active metabolites present in the tumor at an average concentration of 160 ng/g, corresponding to the general value of 113% of plasma peak concentrations in a stable state.

Mo tissue distribution studies use all -body radio isotopes after taking Erlotinib marked by 14C in mice without a thymus with a transplant of HN5 species, showing a wide and fast tissue distribution with maximum agriculture of the radioactive drug (about 73% of plasma concentrations) observed after 1 hour.

transformation

Erlotinib is metabolized in the liver by cytochrome P450 enzymes in the liver, mainly by CYP3A4 and less metabolized by CYP1A2.

Metabolic external liver by CYP3A4 in the intestine, CYP1A1 in the lungs, and CYP1B1 in tumor tissue capable of contributing to Ellotinib specialized clearance.

In vitro studies show that about 80 - 95% of erlotinib metabolized by CYP3A4 enzymes. There are three main metabolic paths that are determined:

O-methyl reduction of each chain or both, then oxidized into carboxylic acid. By the reduction of the O-Methyl of each chain, it takes effect equivalent to Erlotinib in preclinical In vitro experiences and Vivo in Vivo models. They are present in plasma with concentrations
Elimination
Erlotinib's very small metabolites and amounts are excreted mainly in feces (> 90%), with the excretion in the kidneys only occupying a small amount of oral doses.

Before taking Tarceva 150mg Roche medicine supports the treatment of lung cancer (3 blisters x 10 tablets)

How to use

Tablets for oral tablets.

Dosage

recommended dose

Non -small cell lung cancer: Tarceva's daily daily dose is 150mg used at least an hour before or two hours after eating.

Pancreatic cancer: The recommended daily dose of Tarceva is 100mg used at least an hour before or two hours after eating, combined with gemcitabin (see Gemcitabin's instructions for pancreatic cancer indication).

Special dose instructions

may need to adjust the dose when used with substrates and regulating substances for CYP3A4 system.

When you need to adjust the dose, it should be reduced by 50 mg at a time.

Hepatic failure

erlotinib is eliminated by metabolism in the liver and bile excretion. Although the Erlotinib concentration is the same in patients with average liver function (Child-Pugh 7-9) compared to patients with normal liver function, so be careful when taking Tarceva for patients with liver failure. Should consider reducing the dose or stop tarceva if the adverse reaction is severe.

Safety and effectiveness of Tarceva has not been studied in patients with severe liver failure.

kidney failure

Safety and effectiveness of Tarceva has not been studied in patients with renal failure.

used for children

Safety and effectiveness of Tarceva has not been studied in patients under the age of 18.

Smokers

Smoking can cause 50-60% to reduce the distribution of Erlotinib. The maximum tarceva dose is tolerated in cancer patients not small cells and smoking is 300 mg. Effective and long -term safety with higher bureaucracy is advised that the report has not been determined for patients who continue smoking.

Note: The above dose is for reference only. Specific dosage depends on the condition and level of progression of the disease. For a suitable dose, you need to consult a doctor or medical specialist.

What to do when overdose?

The dose repeats twice a day 200mg in healthy subjects with poor tolerance after only a few days of use. Based on data from these studies, heavy adverse effects such as diarrhea, rash, and increased liver transaminase enzyme can occur at the recommended dose.

In case of suspicion of Tarveva overdose, it is advisable to stop using and treating symptoms.

In an emergency, call the 115 emergency center immediately or go to the nearest local health station.

What to do when forgetting 1 dose? However, if the time to relax with the next dose is too short, skip the dose and continue the calendar of the drug. Do not use double dose to compensate for missed dose.

Side Effects

The following adultery reactions are recorded in patients using the Tarceva 150mg and Tarceva 100mg or 150mg in combination with Gemcitabin.

Gastrointestinal disorders:

Cases of gastrointestinal bleeding are regularly recorded in the trials, some cases use with warfarin.

Liver disorders:

Liver functional tests (including Alt, AST, Bilirubin) are observed regularly in Tarceva's clinical trials. In PA3 study, these abnormalities occur very often. These adverse effects are largely mild to medium, airy or accompanied by metastasis in the liver. Some rare cases with liver failure (with death) have been reported while using Tarceva. Interference factors include liver disease before or using poison for the liver simultaneously.

Eye disorders:

Ulcerative or corneal perforation has been reported, though very rare in Tarceva treatment patients. Cerodenitis and conjunctivitis are also often told to Tarceva. Abnormal eyelash growth includes: eyelashes growing in, plenty of eyelashes and dense have been reported.

Respiratory, chest and medical disorders:

There are irregular reports on severe interstitial pneumonia, (with death), in patients using Tarveva to treat NSCLC or other tumors.

Cases of nosebleeds are also often reported in NSCLC clinical trials and pancreatic cancer.

The skin and tissue dysplasies

The rash is very commonly reported in patients using Tarceva and in general, manifested in the form of rash and mild or medium -sized pus, which can occur or worsen in areas of sunlight exposure. Patients can be recommended to have sunlight exposure to use protective clothes and/or use sunscreen (for example, a mineral -containing type). Acne, acne -like dermatitis and folliculitis appear quite often, most of these events are light or moderate and not serious. Mild reactions such as hyperpigmentation skin have also been reported, though rare (out of less than 1% of patients).

Water balls, blisters and skin peeling have been reported, including very few cases of suggesting the diagnosis of Stevens-Johnson syndrome/poisoned epidermal necrosis, including some deaths.

Change hair and nails, mostly not serious, have been reported in clinical trials, such as inflammation around the nails and bushes, eyelashes / eyebrows and brittle nails that are broken or peeling have been reported but rarely encountered.

Warnings

Before using the drug you need to read the instructions carefully and refer to the information below.

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Tarceva is contraindicated in patients with severe hypersensitivity to erlotinib or with any component of Tarceva.

Precautions when using

Interpretation disease

Cases of interstitial lung disease (ILD), including deaths, are sometimes reported in patients using Tarceva to treat non -small cell lung cancer (NSCLC), pancreatic cancer or other specialized tumors.

In a key Branch 21 study in NSCLC, the rate of ILD -like events is 0.8% in the placebo group and the Tarceva group. In pancreatic cancer studies in combination with gemcitabin, the ratio of the variable like ILD is 2.5% in the Tarceva group in combination with gemcitabine compared to 0.4% in the fake group in combination with Gemcitabin.

General ratio in patients treated with Tarceva from all studies (including non -control studies and studies using simultaneous chemotherapy) is about 0.6%.

Diagnosis is recorded in patients with suspected ILD diseases including coordination, radiotherapy pneumonia, hypersensitivity pneumonia, interstitial pneumonia, pulmonary disease, obstructive bronchitis, pulmonary fibrosis, acute respiratory insufficiency syndrome, pulmonary infection, and alveoli.

These ILD -like events start a few days to a few months after starting the Tarceva treatment. Most cases accompanied by disturbing factors or contributing factors such as simultaneous chemotherapy or before that, previous radiation therapy, previous lung parenchyma disease, metastatic diagonal disease, or pulmonary infection.

In patients with new acute and//or unexplained symptoms that are progressive, such as shortness of breath, cough and fever, should stop treating with Tarceva while waiting for diagnostic evaluation. If diagnosed with ILD, it should be stopped using Tarceva and appropriate treatment depending on the situation.

diarrhea, dehydration, then electrolyte and kidney failure

Diarrhea has occurred in patients using Tarceva and average and severe diarrhea should be treated with Loperamide. In some cases, the dose should be reduced.

In case of severe or persistent diarrhea, nausea, anorexia or vomiting causing dehydration, it is advisable to stop using Tarceva and take appropriate measures to treat dehydration. There have been a number of rare cases of hematuria and kidney failure (including death). A few cases of kidney failure are caused by severe dehydration due to diarrhea, vomiting and/or anorexia while other cases are interfered with chemotherapy simultaneously.

In cases of severe or prolonged diarrhea, patients are dehydrated, especially in groups of patients with risk factors for severe illness (using other drugs at the same time, symptoms or diseases or promotions including high age), Tarceva should be temporarily suspended and apply appropriate measures to activate water to actively compensate patients by intravenous. In addition, the kidney and electrolyte function should be monitored in serum including potassium in patients at risk of dehydration.

hepatitis, liver failure

Some rare cases of liver failure (can die) have been reported while using Tarceva. Interference factors include liver disease before or using poison for the liver simultaneously. Therefore, periodic liver function test should be tested for such patients. Tarceva should be stopped if there is a lot of liver function changes.

Gastrointestinal tract puncture

Patients using Tarceva have an increased risk of gastrointestinal perforation, although they are rarely observed. Patients treated simultaneously with anti -vascular drugs, corticosteroids, nsaids, and/or chemotherapy of Taxane, or those with a history of stomach ulcers or patients with excess bags, who are high -risk patients.

Tarceva should be completely stopped in patients with gastrointestinal perforation.

Water ball, peeling skin and skin disorders

Water balls, blisters and skin peeling have been reported, in which there are very few cases of stevens-johnson syndrome/epidermal necrosis of the epidermis, which is dead in some cases. Should suspend or stop treating with Tarceva if the patient has a serious water ball, blistering or skin peeling.

Eye disorders

Very rare cases of ulcer or corneal perforation are reported during Tarceva's use. Other disorders include abnormal eyelid growth, horny conjunctivitis or keratitis that has been observed with patients treated with Tarceva that is also a risk factor for puncture/corneal ulcer. Tarceva should be suspended or stopped completely if the patient shows more severe/severe eye disorders such as eye pain.

Use drugs for women during pregnancy and lactation

Pregnant women

There is no appropriate or good control in pregnant women using Tarceva. Animal studies have shown some reproductive toxicity. Potential risk for unknown people.

Women who are likely to be pregnant must be advised to avoid pregnancy when using Tarceva. The appropriate contraceptive should be used during treatment, and at least 2 weeks after the end of treatment. Treatment should only continue in pregnant women if the benefits bring mothers higher than the risk of pregnancy.

breastfeeding women

It is not known whether Erlotinib is secreted through breast milk. Due to the ability to harm the child, the mother should not breastfeed while using Tarceva.

The effect of the drug on driving and operating machinery

There is no research on the impact on the ability to drive and operate machinery, however, Erlotinib does not reduce intelligence.

Drug interaction

erlotinib is metabolized in the liver by the liver cytochrome system in humans, mainly by CYP3A4 and less by CYP1A2, and CYP1A1 in the lungs. Interactive ability can occur with drugs passed by, or inhibitors or stimulating these enzymes.

Strong active inhibitors CYP3A4 reduces Erlotinib's metabolism and increases the plasma concentration of Erlotinib. Ketoconazole inhibits CYP3A4 metabolism (200mg oral twice daily in 5 days) increasing the concentration of erlotinib (Ellotinib median distribution concentration [AUC] increased by 86%) and CMAX increased by 69% when compared to the use of Erlotinib.

When using Tarceva at the same time as Ciprofloxacin, the drug inhibits both CYP3A4 and CYP1A1, the level of Erlotinib distribution [AUC] and the maximum concentration (CMAX) increased by 39% and 17% respectively. So be careful when using Tarceva with strong CYP3A4 inhibitors or CYP3A4/CYP1A1 inhibitors. In these cases, Tarceva should be reduced when recorded toxic.

Strong stimulants of CYP3A4 activity increase Erlotinib pass chemistry and reduce Erlotinib plasma levels significantly. Rifampicin stimulates the metabolism of CYP3A4 (600mg taken daily for 7 days) as the median AUC of Erlotinib decreased by 69%, after using Tarceva at a dose of 150mg, compared to the tarceva simple.

Previous treatment or simultaneous use of Rifampicin with a single dose of 450mg Tarceva as AUC with Erlotinib decreased to 57.5% compared to the value when using a single dose of 150mg tarva without using rifampicin. If possible, consider the replacement regime not to use strong CYP3A4 stimulants. For patients who need to treat Tarceva simultaneously with a strong CYP3A4 stimulant such as Rifampicin, it is advisable to consider increasing the dose to 300mg while closely monitoring safety, and if tolerance is good for more than 2 weeks, it can increase to 450mg and closely monitor safety. There is no higher dosage research in this case.

previous treatment or simultaneous use with Tarceva does not change the clearance of the typical substrates of CYP3A4, Midazolam and Erythromycin. Therefore, it is less likely to interact with important drugs with other substrates of CYP3A4. The user after taking Midazolam seems to be reduced by up to 24%, but not due to the effect on CYP3A4 activity.

Erlotinib's solubility depends on pH. Erlotinib's solubility decreases when the pH increases. The drugs that change the pH of the above gastrointestinal tract may change the solubility of erlotinib and thus affect its bioavailability.

Simultaneous use of Tarceva with Omeprazole, a proton pump inhibitor, reduces Erlotinib concentration (AUC) and the maximum concentration is 46% and 61% respectively. There is no change in Tmax or the sale time. Simultaneous use of Tarceva with 300 mg of Ranitidine, a H2 receptor antagonist, reducing Erlotinib levels [AUC] and the maximum concentration is 33% and 54% respectively. Therefore, it is necessary to avoid with stomach acid reduction drugs with Tarceva if possible.

Increase Tarceva dose when used simultaneously with such drugs is hard to compensate for a decrease in concentration. However, when Tarceva was staggered 2 hours before or 10 hours after using 150mg Ranitidine, Erlotinib levels [AUC] and CMAX were only reduced by 15% and 17% respectively.

If the patient needs to be treated with such drugs, a H2 receptor antagonist like Ranitidine needs to be considered and used in a staggered manner. Patients must take Tarceva at least 2 hours before or 10 hours after taking H2 receptor antagonistic drugs.

Increased international standardization ratio (INR) and cases of bleeding including stomach bleeding were recorded in clinical studies, some cases used with warfarin. Patients taking warfarin or anticoagulants of Coumarin should be followed on a regular basis to detect any change in prothrombin or INR.

Smokers should be advised to stop smoking because of cigarette smoke, which stimulates CYP1A1 and CYP1A2, which is researched showing that reducing the Erlotinib distribution concentration is about 50 - 60%.

In a IB phase study, there is no significant effect of gemcitabin for Erlotinib's pharmacokinetics as well as no significant effects of Erlotinib on Gemcitabin's dynamic pharmacokinetics.

Storage

Do not use tarceva after expiry date (exp) on the box.

Do not store drugs at temperatures above 30 ° C.

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