LENALID 25MG

Drug profile

Lenalid25mg containing active substance known as Lenalidomide which is considered as thalidomide derivative and it is originated from Generic Revlimid.

Lenalidomide is a naturally established compound which plays important role in myeloma at first, later it is used for hematological disorders like myelodysplastic syndromes.

Lenalidomide is an Immuno modulatory agent which has both anti-angiogenic & anti-cancer activity.

Lenalid is available in the strength of 25mg

LENALID 25MG

Trade name: Lenalid25mg

Active ingredient: Lenalidomide

Strength: 25mg

Mfg: Natco pharma

Pack: 30 tablets in a container

Classified as: Anti-neoplastic drug

Prescribing information of Lenalid 25mg;

The most important therapeutic indication of Lenalidomide is given below as follows;

    In multiple myeloma

    In myelodysplastic syndrome

    In mantle cell lymphoma

Multiple myeloma:

Lenalid25mg (Generic Revlimid) is used in myeloma condition by combining with dexamethasone

In myeloma patients with autologous hematopoietic stem cell transplantation, Lenalid25mg is used as a continuation therapy.

Myelodysplastic syndrome:

Lenalid25mg (Generic Revlimid), is also used in the therapy of patients with transfusion vulnerable anemia expected low or moderate exposure of myelodysplastic syndrome related to deletion 5q cytogenetic aberrant.

Mantle cell lymphoma:

Lenalid25mg (Generic Revlimid) is used in mantle cell lymphoma as a second line therapy. The patient’s disease conditions are reoccurred or advanced after prior two therapies like Bortezomib.

Drawback of use;

Lenalid25mg is not suggested in chronic lymphocytic leukemia.

Mechanism of Lenalid 25mg;

Lenalid25mg (Generic Revlimid), is a thalidomide analogue.

The pharmacological activity of Lenalid25mg is;

Immuno modulatory

Anti-angiogenic activity

Anti-neoplastic activity

Immuno modulatory effect by;

Elevates the counts and activates the effect of T-cells and natural killer cells

Elevates the count of natural killer T cells

Prohibits the pro-inflammatory cytokines like TNF-alpha & IL-6 monocytes

Anti-neoplastic activity by;

Prohibiting cell multiplication & activates apoptosis of cancer cells in vitro and causes prohibition of cell growth in vivo, prominently to reduce in tumor strain.

Postponing the growth of cancer cells

Combined effort of dexamethasone leads to inhibits cell replication and promotes apoptosis in myeloma cells.

Anti-angiogenesis;

Angiogenesis (cell development) is blocked by reducing the levels of VEGF, TNF-alpha & IL-6.

VEGF: Vascular Endothelial Growth Factor

Lenalidomide is expel its activity by inhibits the interpretation of cyclo oxygenase 2 (COX 2) in vitro, it may trigger the apoptosis directly by involving in prohibition of bone marrow stromal cell backing by anti-angiogenic and anti-osteoclastogenic activity & by Immuno modulatory effect 

Absorption

After an oral administration of Lenalid 25mg, the absorption occurs very quickly.

The peak plasma concentration time occurs between 0.5 to 6 hours after drug intake.

Distribution

Lenalid25mg is bounds to human plasma protein at relatively 30%

Lenalidomide is occurs in semen after administration, at 2 hours & 24 hours after the dose of 25mg Lenalid 25mg.

Metabolism

The metabolism of Lenalidomide is occurs in limited range, mostly unchanged form of Lenalidomide is a major circulating substance present in the human body.

There are two major metabolites like;

5-hydroxy Lenalidomide

N-acetyl Lenalidomide

Not more than 5% of parent form is present in the circulation.

Excretion

The primary elimination of Lenalidomide is occurs via renally.

Nearly 82% of radioactive dose is eliminated in urine within 24 hours; the two metabolites are excreted in 4.6% & 1.8%.

Total excretion occurs within 10 days.

The terminal half life period of Lenalidomide in healthy person is 3 hours; whereas in myeloma & MDS or MCL is 3 to 5 hours

When to take the tablet Lenalid 25mg

Lenalid25mg (Generic Revlimid) should be taken with or without food.

Lenalid25mg capsules should not be opened, broken or chewed.

It should be administered with whole water.3

Dosage regimens of Lenalid 25mg

The potency of Lenalidomide is not evaluated in pediatric patients with the age of <18 years.

In adults;

In myelodysplastic syndrome:

The recommended dosage is 10mg of Lenalidomide should be taken as a single dose.

In renal damaged patients:

In CrCl 30 to 60ml/min: 5mg of Lenalidomide should be suggested for once a day.

In CrCl <30ml/min: 2.5mg PO as a single dose

In CrCl >60ml/min: No dosage adjustment is required

Multiple myeloma:

The therapy should be followed by combining of Lenalid25mg with dexamethasone as a single dose.

The recommended dose of Lenalid25mg is 25mg should be given as a single dose on day 1 to 21 of repeated 28 day cycles.

The dosage of dexamethasone;

For first 4 cycles;

40mg of dexamethasone should be recommended on days 1 to 4; 9 to 12; & 17 to 20 of each 28 day cycles.

Then followed by 40mg should be given as single dose, days 1 to 4 every 28 days

Age >75 years: 20mg of dexamethasone is recommend, on day 1, 8, 15 & 22 of each 28 cycle.

Mantle cell lymphoma:

The recommended dosage of Lenalid25mg is 25mg should be administered orally as a single dose.

CrCl 30 to 60ml/min: 10mg PO single dose

CrCl <30ml/min: 15mg should be recommend as a single dose.

In ESRD: 5mg should be given

Lenalid25mg caused side effects

The major adverse effects;

Embryo fetal damage

Hematological toxicity

Venous & arterial thromboembolism

Elevation in mortality with CLL

Malignancies

Liver damage

Serious cutaneous reactions

Tumor lysis syndrome

Tumor flare syndrome

Damaged stem cell mobilization

Thyroid disorders

Increased extinct rate in MCL

The most common side effects;

Fatigue

Asthenia

Pyrexia

Chest pain

Diarrhea

Abdominal pain

Dyspepsia

Back pain

Muscle spasms

Arthralgia

Bone pain

Pain in extremity

Musculoskeletal pain

Neck pain

Respiratory infection

Pneumonia

Influenza

Rhinitis

Cellulitis

Lab abnormalities

Anemia

Thrombocytopenia

Neutropenia

Pancytopenia

Hypokalemia

Hyperglycemia

Hypocalcaemia

Hypophosphatemia

Hyponatremia

Other effects;

Rash

Pruritus

Deep vein thrombosis

Loss of appetite, weight

Insomnia

Squamous cell cancer

Basal cell cancer

Drug - drug interaction of Lenalid 25mg

With digoxin:

Lenalid25mg is combined used with digoxin causes increasing the plasma concentration of Lenalidomide lead to increase the adverse effects.

 To avoid this problem, monitor the digoxin plasma concentration periodically during this concomitant.

Warfarin:

There is no pharmacokinetic changes occurs during this concomitant of Lenalidomide with warfarin, but patients may get alteration in prothrombin time & INR. To avoid this condition, monitor the values frequently during this combinational therapy.

Some combination treatment may increase the exposure of thrombosis:

Erythropoietic drugs or some other medicines that may elevate the exposure of thrombosis like estrogen containing treatment.

This type of concomitant treatment should be used cautiously to reduce the risk factors.

Food drug interaction of Lenalid 25mg

Food should be avoided during chemotherapy of multiple myeloma;

Lenalid25mg cause renal impairment;

Food rich in potassium

Avocados, bananas, spinach, citrus, tomatoes should be avoided

Rich in phosphorus

Whole grains, oats, bran cereals, sunflower seeds

Food avoid during therapy;

Raw meats, sea foods, poultry

Unpasteurized dairy

Raw sprouts

Raw egg

Possible contraindications of Lenalid 25mg;

Lenalidomide is contraindicated to pregnancy condition, may cause fetal damage

Some hyper sensitivity reactions like Stevens Johnsons syndrome, angioedema may occur, due to patients may contraindicate to the components present in Lenalid25mg tablets.

Safety measures of Lenalid 25mg;

Warning;

During Lenalid25mg therapy, some life threatening conditions may occur like;

    Embryo fetal damage

    Hematological toxicity

    Venous & arterial thromboembolism

In tumor flare reaction:

This condition may occurs in patients who undergone Lenalidomide therapy, in CLL & lymphoma have chance of getting inflammation on lymph nodes, fever, pain, & rash

In liver toxicity:

Constant hepatic function test should be done, before and during the therapies.

In this condition, treatment should be postponed and continue if required.

In tumor lysis syndrome:

In this condition, patients must be monitored carefully and precaution should be provide.

In allergic conditions:

Lenalid25mg treatment should be withheld or discontinue in case of angioedema, rash, bullous rashes.

In venous thromboembolism:

In MDS, Lenalid25mg is used as a monotherapy, in this condition there is a chance of getting increased exposure of DVT & PE.

In hematological risk:

Lenalid25mg causes thrombocytopenia and neutropenia, patients receiving Lenalid25mg for MDS should be completely examine by investigating blood counts weekly for first 8 weeks.

In MM patients should be monitored with counting blood cells for every 2 weeks for first 12 weeks and then monthly afterwards.

In this condition, dose reduction is applicable.

In embryo fetal harm:

Lenalidomide is contraindicated to pregnancy conditions.

Pregnancy and lactation

Pregnancy category: X

Lenalid25mg should not be recommended in pregnancy condition

Breast feeding should not be recommended.

The initial dose of Lenalidomide is depending upon the creatinine clearance value and for the patients in dialysis.

Storage and handling

Lenalid25mg tablets should be stores at 20oC to 25oC; excursion between 15oC to 30oC.

Keep the container away from heat, moisture & light

Missed dose

The missed dose of Lenalid25mg should be avoided, and follow the regular dosing schedule.

Over dosage

There is no special treatment for over dosage of Lenalidomide; In case of this condition patient must be provided with adjuvant therapy and monitor the signs & symptoms frequently.