Overview
Mepolizumab is a monoclonal antibody against interleukin-5. It is believed to be obtained from hamster ovary cells. The Food and Drug Administration (FDA) approved Mepolizumab in 2015 as an additional therapy to treat severe asthma. Identifying the drug to treat severe asthma has reduced the need for hospitalization. Later, it was also used to treat eosinophilic granulomatosis with polyangiitis. In addition, Mepolizumab was proven effective for treating adults and children above twelve years with non-blood-related hypereosinophilic syndrome.
How Does Mepolizumab Work?
Mepolizumab reduces the white blood cell activity that stimulates asthmatic attacks. It happens by binding with the interleukin-5, thereby preventing its attachment to the receptor on the eosinophil surface.
Uses
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Severe asthma patients above 12 years of age with an eosinophilic phenotype.
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Eosinophilic granulomatosis with polyangiitis.
Dosage and Administration
Mepolizumab can be administered subcutaneously.
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Asthma: Mepolizumab 100 mg once every four weeks is injected into the abdomen, upper arm, and thigh.
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Eosinophilic Granulomatosis With Polyangiitis: Mepolizumab 300 mg is separated into three 100 mg and injected once every four weeks.
For Patients
Learn About Asthma
Asthma is a respiratory condition associated with swelling of the lungs' airways. But a variant called eosinophilic asthma involves swelling the complete respiratory system from the nose to the small bronchioles. This is the reason for the shortness of breath experienced during the condition. In addition, as the name indicates, this type of asthma shows eosinophilia (increased eosinophil count) in the saliva and usually responds to corticosteroids. However, the identification of Mepolizumab has reduced the use of corticosteroids.
Learn More About Mepolizumab
When and How Often to Take Mepolizumab?
Mepolizumab 100 mg injection is given subcutaneously every four weeks by a healthcare professional. Individuals can self-take the injection themselves or by a caregiver.
How Effective Is Mepolizumab?
The effectiveness of Mepolizumab on asthma control and lung function has reduced the daily use of oral corticosteroids.
Things to Inform the Doctor Before They Prescribe Mepolizumab
The following information must be informed to the doctor before they prescribe Mepolizumab.
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Have parasitic infection.
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Taking oral or inhaled corticosteroids.
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Pregnant or planning for pregnancy.
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Breastfeeding or planning to breastfeed.
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Taking over-the-counter medications and herbal or nutritional supplements.
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Have allergies to Mepolizumab.
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History of shingles.
Starting Mepolizumab
How to Take Mepolizumab?
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The healthcare provider injects Mepolizumab subcutaneously every four weeks.
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If the injection is self-taken, get clarification from the doctor before administering it. Also, read the instructions given with the drug.
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Inject Mepolizumab subcutaneously into the thigh or stomach while self-taking.
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An injection can be administered in the upper arm if a care provider gives it.
Things to Do After Start Taking Mepolizumab
Inform the doctor about the symptom's progress and if it worsens after Mepolizumab administration. Also, do not stop taking other asthma medications without consent from the doctor. In addition, schedule regular appointments and get monitored regularly.
Look Out for Side Effects
The following side effects must be reported to the doctor immediately.
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Allergic reactions.
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Painful blisters.
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Breathing problems.
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Dizziness.
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Fever or chills.
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Cough.
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Difficult urination.
The side effects that are not bothersome until they persist for a long time are
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Backache.
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Headache.
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Weakness.
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Pain, irritation, and redness at the injection site.
Dietary Alterations
No specific dietary alterations are required while taking Mepolizumab. However, tell the doctor all the herbs and dietary supplements taken to ensure no interaction with the medications.
What Should Be Done When a Dose Is Missed?
If the injection is taken in the hospital, try to take the dose. If the dose is self-taken, take the injection as soon as possible if missed. Ensure to avoid taking an extra dose to compensate for the missed dose. However, get an opinion from the physician for better clarification.
What Should Be Done to Treat Mepolizumab Overdose?
No specific treatment has been identified to treat Mepolizumab overdose. If an overdose occurs, immediately report it to the doctor and get monitored and treated.
How to Store Mepolizumab?
Store the prefilled syringes or autoinjectors in the original container in the refrigerator at 36 to 46 degree Celsius. However, do not allow them to freeze. In addition, avoid using the medication if kept outside the refrigerator for more than seven days, even if left unopened. Keep them out of reach from children and pets.
How to Dispose of Mepolizumab?
The used syringe and needle cap must be disposed of in a sharp disposal container immediately after administration. If a sharp disposal container is unavailable, a household container can be used with the following properties.
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Heavy-duty plastic container.
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Leak-resistant.
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Tight-fitting and puncture-resistant cap.
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Stable during use.
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Labeled as hazardous waste on the container.
Once the container is full, the local pharmacy disposal company has to be contacted to dispose of it properly. In addition, avoid throwing the quick disposal with household trash.
Avoid Self-Medication
Avoid taking the injection without the doctor's consent. Also, do not recommend the injection to individuals with similar symptoms.
Staying On Mepolizumab:-
Tips to Stay On Track
If the injection is administered regularly in the hospital or at home, setting the alarm is the best way to stay on track and avoid missing the dose. If the patient is severely ill, the caregiver must be alert to give the injection to the patient.
However, if any adverse effects are noticed immediately, a few hours, or days after injection, the doctor must be informed for further monitoring and management.
For Doctors
Indication:
Mepolizumab treats severe asthma patients above 12 years of age with an eosinophilic phenotype. It also treats adults with eosinophilic granulomatosis with polyangiitis. However, it cannot be used to ease symptoms of acute bronchospasm.
Pharmacology:
Mechanism of Action
Mepolizumab is a humanized monoclonal antibody that binds with interleukin-5 and prevents it from binding to interleukin-5R cells. This process can reduce eosinophil levels and can treat eosinophilic disease. However, the exact mechanism of action of Mepolizumab has yet to be identified. Also, patients with mild asthma and a sub-type of hypereosinophilic syndrome do not benefit from Mepolizumab.
Pharmacodynamics
On administration of Mepolizumab 100 mg every four weeks for severe asthma, eosinophil count was reduced to a mean of 40 cells/microliters. This reduction can be noticed in four weeks and maintained throughout the treatment. On administration of Mepolizumab 300 mg every four weeks for eosinophilic granulomatosis with polyangiitis, the eosinophil count was reduced to a mean of 38 cells/microliters.
Chemical Taxonomy
Kingdom- Organic compounds.
Superclass- Organic acids.
Class- Carboxylic acids and derivatives.
Subclass- Amino acids, peptides, and analogs.
Direct Parent- Peptides.
Ingredients
Active Ingredient: Mepolizumab.
Inactive Ingredients: The vials contain sucrose, polysorbate 80, and sodium phosphate dibasic heptahydrate.
The prefilled autoinjectors and syringes contain ethylenediaminetetraacetic acid (EDTA), citric acid monohydrate, disodium dihydrate, sodium phosphate dibasic heptahydrate, polysorbate 80, and sucrose.
Absorption
When 100 mg of Mepolizumab is administered subcutaneously to an adult, the approximate bioavailability is 80 percent. When the dose is administered for four weeks, approximately two-fold drug accumulation occurs at a steady state.
Distribution
The volume of distribution of Mepolizumab is 3.6 liters in an adult asthma patient.
Metabolism
Mepolizumab undergoes proteolytic degradation (hydrolysis of peptide bonds of proteins) when distributed throughout the body.
Elimination
The mean half-life of Mepolizumab is around 16 to 22 days, and the systemic clearance is 0.28 liters a day.
Toxicity
The carcinogenic potential of Mepolizumab has been studied but has yet to be proven because the results of various studies indicate different properties of tumor rejection and growth.
In a clinical study, Mepolizumab was administered to monkeys, which showed no significant effects on their reproductive potential. No significant pathological findings in the monkeys’ reproductive organs are proof.
Warning and Precaution
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Hypersensitivity Reactions: The hypersensitivity reactions that occurred after Mepolizumab administration are hypotension, anaphylaxis, bronchospasm, rash, and urticaria. They can occur within hours or days after administration. In such a case, the drug has to be discontinued.
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Acute Asthma Symptoms: Mepolizumab is not to treat acute asthma symptoms. If the patient experiences uncontrolled symptoms or it worsens after Mepolizumab administration, immediate medical attention is essential, and the drug must be discontinued for such acute symptoms.
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Opportunistic Infections: In a clinical trial, Mepolizumab caused herpes zoster infection in a few subjects. Vaccination can be considered in such cases.
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Corticosteroid Dosage Reduction: Beginning Mepolizumab administration, the corticosteroid intake should not be halted. However, the dosage can be reduced accordingly to avoid exacerbating the condition for which corticosteroids were taken.
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Helminth Infection: Mepolizumab therapy should not be started before treating helminth infections. However, if an individual acquires helminth infection after Mepolizumab administration, discontinue the drug, treat the helminth infection, and then continue Mepolizumab.
Dosage and Forms
100 mg white lyophilized powder is reconstituted in a single-dose vial. The resultant injection solution is colorless to pale brown, injected using a single-dose auto-injector or prefilled syringe.
Mepolizumab 100 mg is used for asthma patients and 300 mg (three 100 mg doses) for eosinophilic granulomatosis with polyangiitis once every four weeks.
Administration of the Drug
A 1 ml polypropylene syringe with a disposable needle is used for subcutaneous administration. Before administration, the reconstituted solution of Mepolizumab is made ready. The solution must not be shaken to avoid foaming or precipitation. Then, the 1 ml injection containing 100 mg of Mepolizumab can be administered subcutaneously into the upper arm, thigh, or abdomen.
Contraindications
Individuals hypersensitive or allergic to the drug's ingredients, such as sodium phosphate, dibasic heptahydrate, polysorbate 80, and sucrose, are contraindicated to taking Mepolizumab.
Clinical Studies for Mepolizumab
A clinical trial was conducted to assess the effectiveness of Mepolizumab for severe asthma. A randomized placebo-controlled trial for 24 to 52 weeks was conducted. The subjects selected were positive for eosinophils in the airways. Mepolizumab was administered subcutaneously or intravenously every four weeks. The common adverse effects noticed in the subjects were headache, injection site reaction, back pain, fatigue, influenza, urinary tract infection, abdominal pain, pruritus, eczema, and muscle spasms. Post-marketing of Mepolizumab also resulted in a few adverse effects, which were not considered reliable as the population size of the study is negligible, and various external factors might also induce those adverse events.
Drug Interactions
1. The severity of adverse reactions can increase when the following drugs are administered with Mepolizumab.
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Abciximab.
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Adalimumab.
- BCG (Bacille Calmette-Guerin) vaccine.
2. The efficacy of anthrax immune globulin can decrease when administered with Mepolizumab.
Other Specifications:-
Mepolizumab in Pregnant Women
Mepolizumab can get transmitted through the placenta to the fetus during pregnancy. Hence they can cause adverse effects on the fetus during the second and third trimesters of pregnancy. The drug can cause low birth weight, infant prematurity, and preeclampsia (pregnancy complication with high blood pressure) in the mother. Hence the treatment for an asthmatic pregnant woman is maintained and adjusted accordingly.
Mepolizumab in Lactating Women
No data indicates the presence of Mepolizumab in breast milk and its effects on the fetus. However, the following factors must be considered before administration.
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The clinical need of the mother for the drug.
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The beneficial effects of breastfeeding.
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Risks of potential adverse effects on the infant.
Mepolizumab in Pediatric Patients
The efficacy and safety of Mepolizumab use in pediatric patients have not been established yet.
In addition, no significant differences in dose alterations were identified between younger and older patients.
Mepolizumab in Geriatric Patients
No significant differences were identified between younger and older adults regarding the dosage of administration of Mepolizumab. However, on a cautious note, older individuals are started with a lower drug dose, which is then altered depending on the need.
Mepolizumab in Renal Impairment Patients
No significant data has been collected regarding the effects of Mepolizumab on renal impairment patients. However, certain evidence shows that Mepolizumab is not really excreted renally.
Mepolizumab in Hepatic Impairment Patients
No clinical studies have been conducted to establish the use of Mepolizumab in hepatic impairment patients. Also, Mepolizumab is metabolized primarily by proteolytic enzymes, so hepatic functioning and the elimination of the drug do not correlate.
