LOPATINIB 250 Tablets

Product Description

Lapahope 250mg (Lapatinib 250mg) tablets are classified as anti-cancer agent, which is orally active drug used for treating breast cancer.
Chemically classified as quinazoline with strong anti-cancer effect and the tablet Lapahope 250mg (Lapatinib 250mg) is a synthetic oral tablet.
Normally targeted therapy or tyrosine kinase inhibitor drugs can increase the plasma amino transferase levels which may leads to liver injury.
Lapahope 250mg (Lapatinib 250mg) tablets are classified as;
1. Tyrosine kinase prohibitor
2. Stop the HER2/neu& epidermal growth factor receptor activity
3. Targeted therapy
4. Signal transduction prohibitor.

INDICATIONS of  Lapahope 250mg (Lapatinib 250mg)

Primarily Lapahope 250mg (Lapatinib 250mg) indicated for advanced breast cancer. Lapahope 250mg (Lapatinib 250mg) is indicated for the combination with Capecitabine tablets are normally indicated for the treatment of metastatic breast cancer patients in whose cancer cells expressed with EGFR 2 (HER2) and already patients may get an anthracycline, taxane & Trastuzumab.

MECHANISM OF ACTION  of Lapahope 250mg (Lapatinib 250mg)

Chemically Lapahope 250mg (Lapatinib 250mg) is classify as 4-anilinoquinazoline derivative, that evacuate anti-cancer activity by inhibiting intracellular tyrosine kinase domains of EFGR & HER type 2.
The ErbB forced cancer cell production has been prevented by Lapatinib.
This growth factor receptor present on cell surface of cancer mass which may leads to cause cell death.

Absorption of  Lapahope 250mg (Lapatinib 250mg)

Incomplete and insufficient absorption, the time to peak plasma concentration is 4 hours after intake of drug.

Distribution of  Lapahope 250mg (Lapatinib 250mg)

The drug bounds to human plasma protein like albumin & alpha glycoprotein relatively 99%.

Metabolism of  Lapahope 250mg (Lapatinib 250mg)

Lapahope 250mg (Lapatinib 250mg) is a substrate of P-gp& BCRP and go through intensive metabolism by using CYPP3A4 & CYP3A5 with minimum contribution of CYP2C19 & CYP2C8.         

Excretion of  Lapahope 250mg (Lapatinib 250mg)

Elimination occurs via feces & urine.
Half-life time in 14.2 hours reaches by single dose of Lapahope 250mg (Lapatinib 250mg) and multiple dosing reaches in 24 hours.

 SIDE EFFECTS  of  Lapahope 250mg (Lapatinib 250mg)

Stomatitis, Dyspepsia, Diarrhea, Nausea, Vomiting, Liver toxicity, Interstitial lung disease, Anaphylactic reactions, Stevens Johnson syndrome, Ventricular arrhythmias, QT prolongation, Palmar plantar erythrodysesthesia, Rash, Dry skin, Mucosal inflammation, Musculoskeletal pain in extremity, Back pain, Dyspnea, Insomnia, Alopecia, Pruritus, Nail disorders, Asthenia, Headache, Epistaxis, Elevation of hemoglobulin, platelets, neutrophils, Increase in AST & ALT, bilirubin, Reduction of left ventricular ejection fraction.

PRECAUTIONS  of  Lapahope 250mg (Lapatinib 250mg)

Reduction in left ventricular ejection fraction:
While using Lapahope 250mg (Lapatinib 250mg) in patient with LVEF Caution should be taken
The resentment of LVEF should be decreased within first 12 weeks of treatment
Before starting the therapy with Lapahope 250mg (Lapatinib 250mg), patient must be monitor thoroughly if suspected with LVEF or not.
Liver damage: Raising level of AST, ALT or bilirubin may cause liver injury
To inhibits this condition, periodic LFT should be control
Diarrhea:
Serious diarrhea may cause to dehydration leads death also; if patient do not recover from this severity must stop with this therapy.
Interstitial lung disease:
Patient should be check with pulmonary symptoms and give supportive measures.
On Serious condition, treatment should be discontinuing
QT prolongation:
Balance ECG periodically
Give the patient substituent for this adverse condition
Hypokalemia and hypomagnesemia correction should be takes place
Cutaneous reactions:
Some life-threatening reactions may occur, in this condition therapy should be discontinued
Embryo fetal damage:
Lapahope 250mg (Lapatinib 250mg) leads to fetal damage and produce some deformities.
During therapy Patient should advice not getting pregnant.

DRUG INTERACTION  of  Lapahope 250mg (Lapatinib 250mg)

The drug Lapahope 250mg (Lapatinib 250mg) are prohibition of CYP3A4, CYP2C8 & P-gp drug transporters; weak inhibitor of CYP3A4.
Interaction of Midazolam with Lapahope 250mg (Lapatinib 250mg), increases the exposure of Midazolam
Interaction of Paclitaxel Will Increase in paclitaxel exposure occurs while concomitant with Lapahope 250mg (Lapatinib 250mg).
Digoxin interaction with Lapahope 250mg (Lapatinib 250mg) then the Serum digoxin concentration should be examined periodically prior starting the concomitant use.
Drug that induce or inhibit CYP3A4 enzymes:
If the interaction of Lapahope 250mg (Lapatinib 250mg) tablets with CYP3A4 inducers or inhibitors, alteration of dose is necessary.
Interaction of Ketoconazole with Lapahope 250mg (Lapatinib 250mg), the dose reduced to 200mg as two times a day for 7 days.
Interaction of Carbamazepine with Lapahope 250mg (Lapatinib 250mg), the dose of carbamazepine at 100mg as two times a day for 3 days & 200mg for two times a day for 17 days, the exposure of Lapahope 250mg (Lapatinib 250mg) reduced to 72%.
Concomitant use of Lapahope 250mg (Lapatinib 250mg) with P-gp inhibitors causes increasing the concentration of Lapatinib.