Combinib 250mg (Lapatinib)
Description of Combinib 250mg (Lapatinib 250mg)
Combinib 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 Combinib 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.
Combinib 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 Combinib 250mg (Lapatinib 250mg)
Primarily Combinib 250mg (Lapatinib 250mg) indicated for advanced breast cancer. Combinib 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 Combinib 250mg (Lapatinib 250mg)
Chemically Combinib 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 Combinib 250mg (Lapatinib 250mg)
Incomplete and insufficient absorption, the time to peak plasma concentration is 4 hours after intake of drug.
Distribution of Combinib 250mg (Lapatinib 250mg)
The drug bounds to human plasma protein like albumin & alpha glycoprotein relatively 99%.
Metabolism of Combinib 250mg (Lapatinib 250mg)
Combinib 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 Combinib 250mg (Lapatinib 250mg)
Elimination occurs via feces & urine.
Half-life time in 14.2 hours reaches by single dose of Combinib 250mg (Lapatinib 250mg) and multiple dosing reaches in 24 hours.
SIDE EFFECTS of Combinib 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 Combinib 250mg (Lapatinib 250mg)
Reduction in left ventricular ejection fraction:
While using Combinib 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 Lanib 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:
Combinib 250mg (Lapatinib 250mg) leads to fetal damage and produce some deformities.
During therapy Patient should advice not getting pregnant.
DRUG INTERACTION of Combinib 250mg (Lapatinib 250mg)
The drug Combinib 250mg (Lapatinib 250mg) are prohibition of CYP3A4, CYP2C8 & P-gp drug transporters; weak inhibitor of CYP3A4.
Interaction of Midazolam with Lanib 250mg (Lapatinib 250mg), increases the exposure of Midazolam
Interaction of Paclitaxel Will Increase in paclitaxel exposure occurs while concomitant with Lanib 250mg (Lapatinib 250mg).
Digoxin interaction with Combinib 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 Combinib 250mg (Lapatinib 250mg) tablets with CYP3A4 inducers or inhibitors, alteration of dose is necessary.
Interaction of Ketoconazole with Lanib 250mg (Lapatinib 250mg), the dose reduced to 200mg as two times a day for 7 days.
Interaction of Carbamazepine with Lanib 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 Combinib 250mg (Lapatinib 250mg) reduced to 72%.
Concomitant use of Combinib 250mg (Lapatinib 250mg) with P-gp inhibitors causes increasing the concentration of Lapatinib.
OVERDOSAGE of Combinib 250mg (Lapatinib 250mg)
The doses of Combinib 250mg (Lapatinib 250mg) ranges from 2500mg to 9000mg daily, the duration of therapy should be varied between 1 & 17 days. Symptoms occurred during over dose of Combinib 250mg (Lapatinib 250mg) are; Sore scalp, Sinus tachycardia & Mucosal inflammation. Patients should be providing with supportive measures.
CONTRAINDICATION of Combinib 250mg (Lapatinib 250mg)
The patients who are contraindicated to the component present in Combinib 250mg (Lapatinib 250mg) tablet then Hypersentivity reaction occurs.
PREGNANCY of Combinib 250mg (Lapatinib 250mg)
Pregnancy category: D Combinib 250mg (Lapatinib 250mg) should not be recommended during pregnancy condition
LACTATION of Combinib 250mg (Lapatinib 250mg)
Breast feeding should not be allowed In pediatric patients the potency of Combinib 250mg (Lapatinib 250mg) has not been evaluated. While using this medication the patients In both renal & hepatic impairment, then caution should be taken
DOSAGE of Combinib 250mg (Lapatinib 250mg)
In HER2 positive advanced breast cancer:
The usual dose of Combinib 250mg (Lapatinib 250mg) 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 Combinib 250mg (Lapatinib 250mg) 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 Combinib 250mg (Lapatinib 250mg) in this condition
Dose alteration:
Cardiac events:
Left ventricular ejection fraction with grade 2 reduction in patients is given treatment with Combinib 250mg (Lapatinib 250mg) should be discontinued. In this condition, the dose of Combinib 250mg (Lapatinib 250mg) should be started with 1000mg/day in combining with Capecitabine; whereas in combination with letrozole the dose of Combinib 250mg (Lapatinib 250mg) restated with 1250mg/day after 2 weeks, if LVEF turns to normal.
Hepatic impairment:
Severe hepatic impairment in patients, the dose reduced from 1250mg/day to 750mg/day or from 1500mg/day to 1000mg/day. Administer the Combinib 250mg (Lapatinib 250mg) tablet without food as 1 hour before or 2 hours after the uptake of food.
STORAGE of Combinib 250mg (Lapatinib 250mg)
Store the drug at 25℃ (77℃). Protect free from moisture, heat or light
MISSED DOSE of Combinib 250mg (Lapatinib 250mg)
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.
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