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Trade Names:
Tarceva
- Tablets 25 mg
- Tablets 100 mg
- Tablets 150 mg

Mechanism of Action

Pharmacology

Inhibits intracellular phosphorylation of tyrosine kinase associated with epidermal growth factor receptor.

Pharmacokinetics

Absorption

Approximately 60% after oral administration; increased to almost 100% by food.

Distribution

Approximately 93% protein bound to albumin and alpha-1 acid glycoprotein. Apparent Vd is 232 L.

Metabolism

Metabolized primarily by CYP3A4 and, to a lesser degree, by CYP1A2 and the extrahepatic isoform CYP1A1.

Elimination

About 83% excreted in feces and 8% in urine. The t _½ is about 36 h. Smokers had a 24% higher rate of Cl.

Indications and Usage

Treatment of locally advanced or metastatic nonsmall cell lung cancer (NSCLC) after failure of at least 1 prior chemotherapy regimen; first-line treatment of locally advanced, unresectable, or metastatic pancreatic cancer.

Unlabeled Uses

Treatment of squamous cell head and neck cancer.

Contraindications

Standard considerations.

Dosage and Administration

PO 150 mg at least 1 h before or 2 h after food. Continue treatment until disease progression or unacceptable toxicity occurs.

PO 100 mg 1 h before or 2 h after food. Continue treatment until disease progression or unacceptable toxicity occurs.

PO When dose reduction is necessary, decrease the dose in 50 mg decrements.

General Advice

May be used alone or in combination with other chemotherapy agents (except platinum-based chemotherapy).

Storage/Stability

Store tablets in at controlled room temperature (59° to 86°F).

Drug Interactions

May reduce erlotinib plasma concentrations, decreasing the therapeutic effect and necessitating dosage adjustments or changes in therapy.

May elevate erlotinib plasma concentrations, increasing the risk of adverse reactions and necessitating dosage reduction.

INR elevations and bleeding have been reported with erlotinib coadministration.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Arrhythmias, cerebrovascular accidents including cerebral hemorrhage, MI/ischemia, syncope (less than 5%).

CNS

Fatigue (52%).

Fatigue (73%); pyrexia (36%); depression (19%); dizziness, headache, insomnia (15%); anxiety, neuropathy (13%).

Dermatologic

Rash (75%); pruritus (13%); dry skin (12%).

Rash (69%); alopecia (14%).

EENT

Conjunctivitis, keratoconjunctivitis (12%); corneal ulcerations.

GI

Diarrhea (54%); anorexia (52%); nausea (33%); vomiting (23%); stomatitis (17%); abdominal pain (11%).

Nausea (60%); anorexia (52%); diarrhea (48%); abdominal pain (46%); vomiting (42%); constipation (31%); stomatitis (22%); dyspepsia (17%); flatulence (13%); ileus, pancreatitis (less than 5%).

Genitourinary

Renal insufficiency (less than 5%).

Hematologic-Lymphatic

Hemolytic anemia (less than 5%).

Lab Tests

Abnormal LFTs.

Metabolic-Nutritional

Weight decrease (39%).

Musculoskeletal

Bone pain (25%); myalgia (21%); rigors (12%).

Respiratory

Dyspnea (41%); cough (33%).

Cough (28%); dyspnea (25%).

Miscellaneous

Infection (24%).

Infection (39%); edema (37%).

Precautions

Pregnancy

Category D .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Hepatic function impairment

Use with caution. Consider periodically evaluating liver function (eg, alkaline phosphatase, bilirubin, transaminases) during treatment with erlotinib. Consider erlotinib dose reduction (in 50 mg increments) or interruption of therapy if severe changes in liver function develop.

Pulmonary toxicity

Serious, sometimes fatal, interstitial lung disease has been reported. Monitor patient for acute onset or progression of pulmonary symptoms (eg, cough, dyspnea, fever). Interrupt therapy and notify health care provider. If diagnostic evaluation indicates interstitial lung disease, discontinue erlotinib and be prepared to institute appropriate treatment.

Overdosage

Symptoms

Diarrhea, liver transaminase elevations, rash.

Patient Information

• Explain name, action, and potential side effects of the treatment regimen. Review the treatment regimen, including dosing schedule, duration of treatment, and monitoring that will be required.
• Advise patient to take prescribed dose once daily, at least 1 h before or 2 h after meals or snacks.
• Advise patient or caregiver to immediately report noted or significant side effects, including any of the following, to health care provider: severe or persistent diarrhea, nausea, appetite loss, or vomiting; eye irritation; new onset or worsening of unexplained shortness of breath or cough.
• Caution woman of childbearing potential to avoid becoming pregnant during therapy. Advise patient to use effective contraceptive methods during and for 2 wk following completion of therapy.