Erlocip

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BRAND :  ERLOCIP PRICE :  250$ STRENGTH : 150 MG ACTIVE :  ERLOCIP-ERLOTINIB-150MG COMPANY NAME :  CIPLA TABLETS :  30 TABLETS read more

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Drug profile

Erlocip is a cipla product which is containing an active substance known as Erlotinib, a first line drug of choice in metastatic stage of non small cell lung cancer.

Erlocip is usually prescribed for the patients who are not counters to at least one chemotherapy regimen.

Erlocip is chemically characterized as quinazoline derivative, with anti-neoplastic effect against tumor cells.

Erlocip is pharmacologically categorized as tyrosine kinase inhibitor.

Erlocip is significantly raising the serum aminotransferase levels during the therapy and this may causes liver injuries.

Erlocip containing 150mg of Erlotinib as a anti-cancer agent.

 

Brand name: Erlocip

Active constituent: Erlotinib

Strength: 150MG

Mfg: Cipla

Pack: 30 tablets per container

Category: Anti-neoplastic agent

 

Prescribing information of Erlocip;

Before starting therapy with Erlocip, determination of mutation status is necessary for the patients to prevent the conditions like false positive or negative assessment.

 

Non small cell lung cancer:

Erlocip tablets are indicated primarily for the treatment of advanced NSCLC, in patients who are containing exon 19 deletions or 21substitution mutations.

Erlocip tablets are also considered as monotherapy for the advanced NSCLC patients who are progressive after 4 weeks of therapy with platinum based compounds.

Erlocip is mainly indicated for the patients who are not responding for one chemotherapy drugs.

But the potency of Erlocip has not been evaluated, for first line treatment in advanced NSCLC exon 19 deletions or mutations.

Erlotinib is also considered as a first line therapy while combining with gemcitabine which is eligible to treat advanced pancreatic carcinoma.

 

Mechanism of Erlocip

Erlocip has Erlotinib active substance consisting anti-neoplastic activity with tyrosine kinase prohibiting effect.

Erlotinib is describes as epidermal growth factor receptor type I tyrosine kinase inhibitor.

Erlocip exhibits anti-tumor activity by acting on cell surface in which the EGFR presents.

Erlocip intercedes with EGFR phosphorylation which is results in cell lyses.

Erlocip is also involved in blockage of EFGR associated signal transfer which is contributed for cell growth.

Due to blockade of ensuing signaling of EFGR, cell proliferation is stopped and induced cell death.

 

Absorption

Nearly 60% of Erlotinib get absorbed after oral administration of Erlocip tablets.

The oral bioavailability reaches nearly 100%

The maximum plasma concentration time reaches at 4 hours after drug intake.

Erlotinib solubility is depends upon pH value, if pH increases leads to decrease the Erlotinib solubility.

In case of co administration of Erlocip tablets with gastric regulators like proton pump inhibitors causes depletion of Erlotinib exposure and leads to increase its concentration.

 

Distribution

Approximately 93% of Erlotinib get binds to human plasma protein.

The apparent volume of distribution is 232L

 

Metabolism

The metabolism of Erlotinib is induced by CYP3A4 and lesser extent with CYP1A2.

There are three major metabolic pathway involves in Erlotinib metabolism;

Oxidation of carboxylic acids leads to O-demethylation of side chains.

The hydrolysis of aryl carboxylic acid causes oxidation of acetylene moiety.

Phenyl acetylene moiety undergo aromatic hydroxylation

 

Excretion

The mean creatinine clearance value 4.47L/hr

The terminal half life period of Erlotinib is 36.2 hours

The steady state plasma concentration occurs within 7 to 8 days.

 

When to take the Erlocip tablets

Erlocip tablets should be administered on an empty stomach; it should be taken at least 1 hour earlier or 2 hours after food intake.

 

Dosage regimens of Erlocip

In NSCLC:

The prescribed dose of Erlocip in this condition is 150mg of tablet should be taken as once a day.

This therapy should be followed until disease progression and toxicity occurs.

In pancreatic:

The prescribed dose is 100mg of Erlotinib tablet should be combined with gemcitabine.

If patients not getting severe rashes, then therapy with Erlocip should be continue.

In combinational therapy of Erlocip with CYP3A4 substrates or modulators, dosage alteration is necessary for up to 50mg.

 

Dose modification;

In pulmonary symptoms like cough, dyspnea, fever conditions; Erlocip tablets treatment should be postpones.

In interstitial lung disease: Discontinue the therapy.

In Bullous or exfoliative skin conditions or renal disorders; postpone or discontinue the treatment.

Severe diarrhea: Provide with supportive measures like loperamide tablets, or discontinue the treatment.

In case of dose reduction is required for the patients, Erlocip dose may reduced to 50mg

Cigarette smoking should be avoided it may causes reduction in exposure of Erlotinib.

During elevation of bilirubin, an AST or ALT level causes liver injuries; Erlotinib undergoes hepatic metabolism & biliary elimination. Treatment should be interrupt or discontinue and investigate LFT frequently.

 

Erlocip caused side effects

The most common adverse effects occurred in this therapy such as;

Severe diarrhea

Rashes

Interstitial lung disease

In NSCLC:

Anorexia

Fatigue

Cough

Dyspnea

Nausea

Diarrhea

Rash

Infection

Vomiting

Stomatitis

Pruritus

Dry skin

Conjunctivitis

Keratoconjuctivitis

Abdominal pain

Hepatic function abnormalities like;

Elevation of;

Bilirubin

AST

ALT

In pancreatic cancer;

Similar to NSCLC but some exceptional like;

Edema

Pyrexia

Constipation

Bone pain

Myalgia

Depression

Loss of weight

Dizziness

Insomnia

Alopecia

Anxiety

Neuropathy

Flatulence

Rigors

Deep venous thrombosis

Hemolytic anemia with thrombocytopenia

Cardiac disorders

Hemorrhage

Renal damage

In both NSCLS & pancreatic;

Peptic ulcer bleeding

Melena

Hematochezia

Hematemesis

Hypokalemia

Post marketing effects;

Skin & subcutaneous effects like hirsutism, eyelash or eyebrows altered, nail disorders,

GI perforations

Hepatic failure

 

Drug -drug interaction

Erlocip tablets are strong inhibitor of CYP1A1, moderate inhibitor of CYP3A4 & CYP2C8 and also potent inhibitor of Glucuronidation by UGT1A1.

Erlocip tablets combined with CYP3A4 inhibitors causes increasing the exposure of Erlocip.

CYP3A4 inhibitors like ketaconazole, ciprofloxacin, ritonavir, clarithromycin, voriconazole.

Erlocip tablet co administered with CYP3A4 inducers like rifampicin causes decresing the exposure of Erlocip. Some CYP3A4 inducers like rifabutin, rifapentine, anti-convulsants.

Cigarette smoking is occurs during the therapy with Erlocip, leads to decreasing the exposure to Erlocip.

Erlocip solubility is occurs by pH values, once pH decreases solubility of Erlotinib get increases and causes loss of effects.

Erlocip should not be co administered with gastric regulators at a time; some time intervals like around 2 hours should be taken before or after ingestion of food.

Erlotinib should not be combined with platinum based compounds; it may increases the effect of concentration of platinum based compounds.

Erlocip should not be concomitant with Capecitabine; it may causes elevation of effect of concentration of Erlotinib.

Proteasome prohibitor like Bortezomib may be conventionally significant the effect of EFGR inhibitors including Erlocip

 

Food drug interaction

Erlocip tablets should be taken on an empty stomach; because pH regulates the solubility of Erlotinib.

Avoid intake of grape fruit or juice during therapy with Erlotinib.

This may results as elevating the Erlotinib levels in the body leads to causes adverse effects.

 

Possible contraindications

Any anaphylactic reactions like rashes, Stevens Johnson syndrome may occur during the therapy due to the patients are contraindicated to the component of Erlocip.

 

Safety measures

Pulmonary toxicities:

Interstitial lung disease may occur to overcome this effect by interrupt or discontinue the treatment with Erlocip.

Patient may frequently examine by undergone ILD analysis; this may occur in combinational therapy with gemcitabine.

Renal damage:

Some renal disorders may occur, to avoid this problem postpone or discontinue the theory with Erlocip tablets and follow the regular renal function test.

Hepatic failure:

Due to increasing levels of bilirubin, AST & ALT causes liver toxicity, to prevent this effect monitor the patients with frequent hepatic function test.

In severe condition, treatment should be stopped.

 Diarrhea:

Providing rehydration due to loss of fluids and also give loperamide as a alternative drug.

 In severity, discontinue the therapy with Erlocip

GI perforations:

This may occur due to concurrent use of Erlocip with NSAIDS, corticosteroids, anti-angiogenic agents, or taxane based compounds causes GI perforation by increasing the acid levels in stomach.

This may overcome by discontinuing the treatment.

Bullous & exfoliative skin disorders:

Interrupt or stop the treatment

Cardiac disorders:

Myocardial infarction may occur due to combination of Erlocip with gemcitabine, to avoid this problem stop the combinational therapy.

Cerebrovascular disorders:

Hemorrhage may occurs, stop the therapy

Hemolytic anemia related to thrombocytopenia:

Frequently counts the blood cells before & after the therapy for avoiding this problem.

Ocular disorders: In serious condition, stop the treatment

Bleeding:

Patient receiving coumarin derivatives or warfarin with Erlocip, must monitor with prothrombin time or INR values periodically to prevent bleeding disorders.

 

Pregnancy and lactation

Pregnancy category D

Erlotinib causes fetal harm; it should not be suggested in pregnancy condition.

Breast feeding should not be allowed.

The potency of Erlotinib has not been evaluated in pediatric patients.

 

Storage and handling

Erlocip tablet container should be stored at 25oC.

The container should be keep away from heat, light & moisture.

 

Missed dose

Missed dose should not be followed, if it may occur patient must be consult with medical oncologist and follow the instructions

Follow the correct dosing schedule to avoid the missed dose condition; this may results as increasing the adverse effects of Erlotinib.

 

Over dosage

Missed dose is the one of the reason for obtaining over dosage condition.

Once over dosage of Erlocip occurs in patients, must provided with supportive measures and follow the preventive measures

The over dosage of Erlotinib causes severe diarrhea & rashes, elevating AST, ALT leads to liver damage.

Discontinue the therapy.

 

 

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