Brand Name : Lapahope
Composition : Lapatinib
Strength availability : 250mg
Manufactured by : Glenmark Pharma
Pack : 150 tablets
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Lapahope 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 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 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.
Primarily Lapahope indicated for advanced breast cancer.
Lapahope 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.
In HER2 positive advanced breast cancer:
The usual dose of Lapahope is 1250mg should be given orally as a single dose on day 1 to 21 repeatedly concomitant with Capecitabine 2000mg/m2/day (administer 2 doses relatively 12 hours apart orally) on day 1 to 14 in continuous 21-day cycle.
Sum of 5 tablets of Lapahope should be given at a time as whole.
Patients with hormone receptor positive HER 2 positive advance breast cancer:
The usual dose is 1500mg should be given orally as a single dose by combination with letrozole.
The usual dose of letrozole is 2.5mg as a once daily
Administer 6 tablets of Lapahope in this condition Dose alteration:
Left ventricular ejection fraction with grade 2 reduction in patients is given treatment with Lapahope should be discontinued.
In this condition, the dose of Lapahope should be started with 1000mg/day in combining with Capecitabine; whereas in combination with letrozole the dose of Lapahope restated with 1250mg/day after 2 weeks, if LVEF turns to normal.
Severe hepatic impairment in patients, the dose reduced from 1250mg/day to 750mg/day or from 1500mg/day to 1000mg/day.
Administer the Lapahope tablet without food as 1 hour before or 2 hours after the uptake of food.
Chemically Lapahope 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.
Incomplete and insufficient absorption, the time to peak plasma concentration is 4 hours after intake of drug.
The drug bounds to human plasma protein like albumin & alpha glycoprotein relatively 99%.
Lapahope is a substrate of P-gp& BCRP and go through intensive metabolism by using CYPP3A4 & CYP3A5 with minimum contribution of CYP2C19 & CYP2C8.
Elimination occurs via feces & urine.
Half-life time in 14.2 hours reaches by single dose of Lapahope and multiple dosing reaches in 24 hours.
Reduction in left ventricular ejection fraction:
While using Lapahope 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, patient must be monitor thoroughly if suspected with LVEF or not.
Raising level of AST, ALT or bilirubin may cause liver injury
To inhibits this condition, periodic LFT should be control
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
Balance ECG periodically
Give the patient substituent for this adverse condition
Hypokalemia and hypomagnesemia correction should be takes place
Some life-threatening reactions may occur, in this condition therapy should be discontinued
Embryo fetal damage:
Lapahope leads to fetal damage and produce some deformities.
During therapy Patient should advice not getting pregnant.
The drug Lapahope are prohibition of CYP3A4, CYP2C8 & P-gp drug transporters; weak inhibitor of CYP3A4.
Interaction of Midazolam with Lapahope, increases the exposure of Midazolam
Interaction of Paclitaxel Will Increase in paclitaxel exposure occurs while concomitant with Lapahope.
Digoxin interaction with Lapahope 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 tablets with CYP3A4 inducers or inhibitors, alteration of dose is necessary.
Interaction of Ketoconazole with Lapahope, the dose reduced to 200mg as two times a day for 7 days.
Interaction of Carbamazepine with Lapahope, 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 reduced to 72%.
Concomitant use of Lapahope with P-gp inhibitors causes increasing the concentration of Lapatinib.
The patients who are contraindicated to the component present in Lapahope tablet then Hypersentivity reaction occurs.
If missed a dose the have it as soon possible or Missed dose should be swapped and continue the regular dosing schedule for avoiding adverse conditions. If missed dose occurs, it should not be resume and continue the next schedule.
The doses of Lapahope ranges from 2500mg to 9000mg daily, the duration of therapy should be varied between 1 & 17 days. Symptoms occurred during over dose of Lapahope are; Sore scalp, Sinus tachycardia & Mucosal inflammation. Patients should be providing with supportive measures.
Store the drug at 25℃ (77℃).
Protect free from moisture, heat or light
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.