Dr C P Ravikumar

EVEROLIMUS

Everolimus
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Dr. C P Ravi Kumar

Dr. C. P. Ravi Kumar Lead & Senior Consultant – Paediatric Neurology, The Krishna Institute of Medical Sciences (KIMS), Mahadevapura, Bangalore

What is Everolimus ?

Everolimus belongs to a class of drugs known as mTOR inhibitors, which is used in the treatment of various conditions, including Seizures, cancer and other conditions.

What diseases or conditions does Everolimus help with?

  • Tuberous sclerosis complex–associated partial-onset seizures
  • Tuberous sclerosis complex–associated renal Angiomyolipoma
  • Breast cancer
  • Kidney transplantation
  • Liver transplantation
  • Neuroendocrine tumours
  • Renal cell carcinoma

How is Everolimus available?

This medication is available as Oral tablets in four dose options ranging from 2.5 mg up to 10 mg.

How does Everolimus work in the body?

Everolimus works by inhibiting the mTOR (mechanistic target of rapamycin) pathway, which regulates cell growth, proliferation, and survival. By stopping this protein, it can slow down the growth of cancer cells, prevent the immune system from attacking transplanted organs, and help treat other conditions where cells grow too quickly. In short: it slows down abnormal cell growth and helps the body stay in balance.

How much time do Everolimus take to act?

Everolimus typically starts to take effect within 1 -2 hour when taken orally. BUT the time it takes to see noticeable effects can vary depending on the condition being treated.

For example:

In cases like angiomyolipoma (a type of benign tumour), it may take a few weeks to months for the tumour to shrink.
For other conditions, your doctor will monitor your progress regularly through tests to see how well the medication is working.
It is important to keep taking the medication as prescribed and attend all follow-up appointments to track your progress.
It is important that your child takes Everolimus regularly.
Everolimus only works as long as you take it; it does not treat epilepsy or manage seizures. So do not stop giving Everolimus all of a sudden, as it may result in having more seizures

What is the ideal time to take Everolimus?

Take this medicine one time each day, always at about the same hour. You can take the medicine either with food or on an empty stomach but whichever way you choose, do it the same way every day. Keeping a regular schedule helps your body maintain the right amount of medicine and makes it easier to remember your dose.
Your doctor will give you specific directions about how to take it properly for your treatment. To get the most out of your medication, carefully follow these recommendations.

How should this medication be administered?

What if I miss a dose?

You can take it as soon as you recall, in case your next dose is approaching soon, you can just omit the missed dose and continue with your regular schedule.

NEVER GIVE A DOUBLE DOSE OF EVEROLIMUS

You can give your child another dose if they throw up within 30 minutes of ingesting it. If vomiting happens after 30 minutes, do not take that dose and wait until the next planned time. Regarding missed doses, always heed the instructions given by your physician.

Would there be any side effects on my child from this medication?

Medicines help us get better, but like anything, they can sometimes cause side effects. Most people don’t face major problems, but it’s good to stay alert. Knowing what to watch out for helps you act quickly and get the right care, while still getting the full benefit of your treatment. If you notice any serious symptoms, call your doctor or seek help right away.

Side Effects of Everolimus:

  • Heart: High BP, swollen limbs, irregular heartbeat
  • It May raise sugar/cholesterol levels
  • Stomach: Pain, nausea, diarrhoea, mouth sores
  • Urinary System: Pain or infections
  • Blood: Anaemia.
  • Nervous System: Headaches, fatigue, sleep issues
  • Skin: Rashes, slow healing, hair changes
  • Muscles: Pain or weakness
  • Lungs:Cough or breathing trouble

Rare Adverse Reactions

Angioedema, characterized by swelling of the face, lips, or throat, is a sign of an allergic reaction.
Report Symptoms: Tell your doctor if you notice unusual symptoms like severe infections, breathing problems, or prolonged healing of wounds.

Does Everolimus cause weight gain?

Everolimus does not commonly cause weight gain. In fact, some people may experience weight loss or a reduced appetite as a side effect.
If you notice significant changes in your weight, either gaining or losing—while taking Everolimus, let your doctor know. They can help determine if it’s related to the medication or something else.

Can other common medicines be taken during the course of Everolimus?

Yes, other common medicines can often be taken during the course of Everolimus, but it’s important to do so under the guidance of a healthcare provider. Some medications may interact with Everolimus, affecting its effectiveness or increasing the risk of side effects. For example: Antifungal medications, Immunosuppressive medications, Corticosteroids, Anticonvulsants, Herbal supplements.
Always inform your healthcare provider of any medications or supplements you are taking, including over-the-counter drugs and herbal products. They will be able to make any necessary adjustments to your treatment regimen.

What foods to avoid while taking Everolimus?

  • Grapefruit and Grapefruit Juice: Avoid, since Grapefruit might increase the possibility of adverse effects.
  • Alcohol: Drinking alcohol while on Everolimus may increase the risk of certain side effects, such as liver toxicity and impaired immune function. Alcohol use should be avoided or limited while using this medicine.
  • Seville Oranges (Bitter Oranges): Found in marmalades and some drinks, they can also interfere with the medication.
  • Unhealthy Foods: Avoid foods high in sugar, fat, or salt, as they can contribute to conditions like high cholesterol or blood sugar, which Everolimus may worsen.

Additional Tips:

Stay hydrated and maintain a balanced diet.
Since Everolimus may interact with herbal teas, dietary supplements, and over-the-counter drugs, talk to your doctor about them.

Is it safe to take Everolimus when nursing or pregnant?

Everolimus should be avoided during pregnancy and breastfeeding due to potential risks.
Always discuss family planning and any concerns with your doctor before starting or continuing Everolimus.

Is there any risk if I conceive while taking Everolimus?

Getting Conceived while taking Everolimus may carry some risk, therefore you should talk to your doctor before beginning Everolimus if you intend to become pregnant. Women of childbearing age should use effective birth control while taking this medication and for at least 8 weeks after stopping it.
If you think you might be pregnant while taking the medication, speak to your doctor right away for advice. They will ensure the best options for you and your baby.

Contraindications of Everolimus:

  • Hypersensitivity to Everolimus
  • Severe liver impairment (Child-Pugh Class C)
  • Pregnancy and breastfeeding
  • Use with strong CYP3A4 inhibitors simultaneously.
  • Concomitant use with live vaccines
  • Severe renal impairment
  • People with galactose or lactase deficiency should avoid Everolimus

Can I stop taking Everolimus (withdrawal)?

Withdrawal from Everolimus is not commonly associated with severe effects, but stopping it abruptly can lead to potential issues, particularly if it was being used for conditions like glaucoma, epilepsy, or altitude sickness.

Where should you store Everolimus?

The tablet should be kept out of direct sunlight and dampness.
Keep it securely closed, out of children’s reach, and in its original container.
Verify the expiry date of the medication on the bottle before giving it to the child

Regular health parameter to undergo:

  • Complete blood count with differential test
  • Cardiopulmonary status
  • Blood sugar and cholesterol
  • Kidney function test
  • Liver function test
  • Infections
  • Weight and fluid balance
Always attend your follow-up appointments and inform your doctor if you feel unwell or notice any new symptoms. Regular monitoring helps keep you safe while using the medication.

How to cope with side effects of Everolimus?

  • Fatigue: Rest often, stay hydrated, and eat well.
  • Nausea: Have small and light meals; ginger tea may help. Consult a doctor if it persists.
  • Rash / Itching: Moisturize; wear soft clothes; consult if severe.
  • Mouth Sores: Saltwater rinses; avoid spicy/acidic foods.
  • Swelling: Elevate legs; reduce salt; inform doctor if worsening.
  • Stomach Issues:
  • diarrhoea: Drink fluids.
  • Constipation: Eat fibre + water.
  • Infections: Maintain proper hand hygiene, wash hands frequently, monitor for fever or sore throat, and wear a cotton mask in crowded places.
  • Sleep Trouble: Relaxing routine; cool/quiet room.

Monitor Your Health:

Follow up with your doctor for regular check-ups and blood tests to keep track of any side effects.
If any side effect gets too uncomfortable or you have concerns, talk to your doctor. To assist control the negative effects, they can modify your treatment or prescribe medication.

SUMMARY:

Everolimus is an oral medicine that lowers the immune system. It is used to prevent organ rejection after kidney or liver transplants and to treat certain cancers. Regular doctor monitoring is needed, as it can increase infection risk and cause side effects like mouth sores, liver or lung problems.
Let us know if this information was useful!

REFERENCE:

Author:
  1. Dr. Likitha B S, Pharm. D, Clinical Pharmacologist, Aster Hospitals, Bengaluru
  2. Dr Praveen Kumar, B. Pharm, Pharm D(PB), Lead Clinical Pharmacologist, REGIONAL HEAD KIMS Hospitals, Bengaluru
  3. Dr. C. P. Ravi Kumar Lead & Senior Consultant – Paediatric Neurology KIMS HOSPITALS BENGALURU
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