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Erlotinib (Tarceva® )

 

Warning:  Erlotinib has been given several warnings from the Federal Drug Administration and it is important to review these warnings carefully as death has occurred to some patients. 

Patients with pancreatic cancer can develop heart attack, Ischemicheart disease (angina pectoris and heart failure), or stroke.  If a patient becomes dehydrated acute renal failure can occur so it is important to stop taking this drug immediately and only resume under physician approval.  Gastrointestinal perforations, skin disorders, corneal perforation, cornea ulceration, hepatic failure, and hepatorenal syndrome has been reported with patients on this drug.  If this happens, the patient should stop taking the drug and a physician should be notified immediately.  Death related to hepatic failure and hepatorenal syndrome has been reported so you should not hesitate to contact your doctor. 

Erlotinib should not be taken by patients who have been diagnosed with Interstitial Lung Disease (ILD).  If ILD is determined in a patient taking this drug, the dosage should be stopped immediately to avoid serious health problems.  Some deaths of ILD patients have been reported that link to the usage of this drug.

Indications: Erlotinib is often referred to as TARCEVA and is used as a maintenance drug in chemotherapy treatments.  It has been shown to slow down the growth of cancer cells and is approved by the FDA for use in patients with lung cancer or pancreatic cancer.  Lung cancer patients are prescribed the drug only after they have undergone four cycles of platinum-based, first-line chemotherapy treatments and shown no cancer progression.  Pancreatic cancer patients are given this drug, along with another drug called gemcitabine for first-line treatment in chemotherapy.  

Erlotinib can be used to treat other medical conditions; talk to your doctor or pharmacist for more information.  

Dosage: Erlotinibcomes as a tablet to take by mouth. Patients on Erlotinib are given up to 150mg a day and the drug is taken orally.  The dose should be ingested one or two hours before the patient eats and it is recommended on an empty stomach for best absorption.  Should the dose need to be cut down, the patient should do so in 50mg increments to avoid any possible reaction.

Storage: Patients are reommended to keet Erlotinib tightly closed in the container it came, out of the reach of children. The drug must be stored at room temperature, away from heat, light and moisture. Erlotinib and all other medications should not be used beyond the expiration date printed on the container.    

Overdose: It is very important to take medication as remmended. overdosing this medication can cost the patient his life. The risk of complication increases considerably when the drug is overdosed for a long period of time. Even in the absence of overdose, Erlotinib tends to damage the bone marrow, and lead to serious decreased blood cells count. It is extremely important that you take Erlotinib as indicated by your physician or pharmacist; don’t ever take it more or more often.  

Missing dose: misusing Erlotinib is a serious matter. Taking less can decrease the therapeutic effects of the drug; taking more can lead to serious health problems and even death. Do your best to take it around the same time every day; do not miss or take less of it. In case you forget to take a dose, take the missed one as soon as you remember it. However, if it is time for your next dose, do not double it to recover the missed one. Contact your doctor or wait to go back to your regular schedule.    

Mechanism of action (MOA): Erlotinib is a kinase inhibitor; it prevents the development and selectively induces death of cancer cells by blocking the action of protein-tyrosine kinase, an abnormal protein that signals cancer cells to multiply.  

Contraindications: Erlotinib is contraindicated or should use with precaution in the following conditions: 

 

  • allergy to the drug or any of the constituents 
  • smoking  
  • pregnancy  
  • breast-feeding 
  • lactase deficiency 
  • prolonged exposure to sunlight  
  • consummation of grape fruit  
  • allergy to lactose or in case of galactosemia
  • Glucose-galactose malabsorption.  

Interactions:  It is important to inform your doctor of all medications you are taking, both prescription and non-prescription.  You should not take this drug if you are on any type of drug thinner, drugs that reduce acid in the stomach, corticosteroids, macrolide antibiotics, CYP3A4 inhibitors, CYP3A4 inducers, CYP1A2 inducers, St. John’s Wart, Liver enzyme drugs, or even some anti-seizure medications. 

A decrease in blood level has been reported with patients that smoke while on Erlotinib so smoking should be avoided.  Paired with pain medications, this drug will increase your risk of stomach bleeding.

Below are common substances and medications that can affect the effects Erlotinib or increase the risk of the development of side effects:

 

  • Omeprazole 
  • Pioglitazone 
  • Rifampin 
  • Warfarin 
  • glucocorticoids (Prednisone, and others)  
  • calcium antagonists (Diltiazem, verapamil, and others) 
  • macrolide antibiotics (Erythromycin, clarithromycin, and others)  
  • anticonvulsants (Phenytoin, carbamazepine, and others)  
  • antifungals (Ketoconazole, fluconazole, and others)  
  • HIV drugs ( Ritonavir, indinavir, efavirenz, and others)  
  • barbiturates (Phenobarbital)  
  • Fluoroquinolones (Ciprofloxacin, norfloxacin, and others).  

Side effects:  Erlotinib may interfere with health cells that reproduce rapidly and cause a number of adverse effects in most patients; common Erlotinib side effects include: 

  • weight loss
  • hair loss
  • tiredness
  • weakness
  • diarrhea
  • dry mouth
  • constipation
  • nausea and vomiting
  • sores on your lips or mouth
  • dry mouth
  • change in taste
  • decreased appetite
  • darkening of skin
  • skin rash
  • muscle or limb pain
  • white horizontal discoloration of the nail plate
  • pain, burning, numbness, or tingling in the hands or feet
  • Swelling of the arms, hands, feet, ankles, or lower legs 

If the side effects above persist for weeks, contact your oncologist. In addition, contact your doctor if you experience any of these symptoms:

  • blurred vision
  • chest pain
  • fainting
  • sunken eyes, scarring or abnormal eyelash growth
  • painful or decreased urination
  • blood in urine or stool
  • difficulty breathing or shortness of breath
  • blistering, peeling, dry, or cracked skin
  • itching and/or burning of the skin
  • skin rash on the face, upper chest, or back
  • infections (cough, fever, chills, etc.)
  • dry, red, painful, or irritated eyes
  • pain in the arms, neck, or upper back
  • rapid, irregular, or pounding heartbeat
  • weakness or numbness of an arm or leg
  • unusual bruising or bleeding
  • black and tarry or bloody stools
  • bloody or coffee-like vomit
  • severe depression symptoms
  • Redness, warmth, pain, tenderness, or swelling in one leg