Drug Detail:Methylprednisolone (Methylprednisolone (oral) [ meth-il-pred-nis-oh-lone ])
Drug Class: Glucocorticoids
1. How it works
- Methylprednisolone may be used to reduce inflammation and calm down an overactive immune system.
- Methylprednisolone works by mimicking the effects of glucocorticoid hormones that are secreted naturally by our adrenal glands in response to stress and which are essential for life. Methylprednisolone is a man-made (synthetic) version of these hormones.
- Methylprednisolone belongs to the class of medicines known as glucocorticoids. It may also be called a corticosteroid.
2. Upsides
- May be used as an anti-inflammatory or immunosuppressive agent in a variety of conditions, such as hematological disorders, allergic reactions, gastrointestinal conditions (eg, Crohn's disease or ulcerative colitis), neurological conditions (such as multiple sclerosis), skin conditions, autoimmune disorders, ophthalmic diseases, and many others.
- Used for the palliative care of certain cancers.
- May be given into the joint space or soft tissue by injection to treat acute gout flares, bursitis, tenosynovitis, epicondylitis, and to relieve joint pain caused by rheumatoid arthritis and osteoarthritis.
- May be administered by injection directly into lesions caused by alopecia areata, keloids, lichen planus, psoriasis, and other conditions.
- May be used off-label to treat acute respiratory distress syndrome, to prevent cellular and antibody-mediated rejection after cardiac transplant, for acute exacerbations of COPD, as well as other conditions.
- The glucocorticoid activity of methylprednisolone is greater than its mineralocorticoid activity, which means that it has more effects on the immune response and inflammation than it does on electrolytes and fluid.
- Helps to dampen down an over-reactive immune system and reduces inflammation.
- Causes less fluid retention compared to prednisone.
- Available as oral tablets and an IV and IM formulation.
- Generic methylprednisolone is available.
3. Downsides
If you are between the ages of 18 and 60, take no other medication or have no other medical conditions, side effects you are more likely to experience include:
- Nausea, vomiting, headache, menstrual changes, mild muscle pain or weakness, difficulty sleeping, fluid retention (swelling in the hands or ankles), and agitation are commonly reported side effects of methylprednisolone. Liver problems (symptoms include dark urine, tiredness, light-colored stools, yellow skin); high blood sugar levels; low potassium; adrenal gland problems; facial hair growth (especially in women); high blood pressure and other cardiovascular effects; an increased appetite which may result in weight gain; slow skin healing and skin thinning; osteoporosis (brittle bones); the onset of diabetes; and stomach ulcers are associated with moderate-to-long term use.
- May increase a person's susceptibility to infection and may mask some signs of an infection. The risk is greater with higher dosages.
- Methylprednisolone exacerbates systemic fungal infections and should not be used by people with a systemic fungal disease (such as candidiasis or aspergillosis). Latent diseases (caused by pathogens such as amoeba, tuberculosis, or Toxoplasma) may also be activated.
- Long-term methylprednisolone administration has been associated with the suppression of the hypothalamic-pituitary-adrenal (HPA) axis (a complex interactive signaling and feedback system involving the hypothalamus, the pituitary gland, and the adrenal glands). Suppression of this axis can result in corticosteroid insufficiency - where natural corticosteroid levels are no longer adequate to maintain vital bodily processes - after the withdrawal of treatment. For this reason, moderate-to-long-term methylprednisolone therapy should be withdrawn gradually.
- The dosage of methylprednisolone requires adjusting during times of stress.
- All corticosteroids, including methylprednisolone, can cause salt and fluid retention, which may lead to blood pressure elevation and increased potassium excretion. Calcium excretion is also increased.
- Alcohol should be limited or avoided to help reduce the risk of gastrointestinal side effects.
- With high doses of corticosteroids, live or live-attenuated vaccines should be delayed until several months after corticosteroid treatment has stopped.
- May not be suitable for some people including those with cardiovascular disease, low thyroid levels, gastrointestinal disease, pre-existing bone disease, or psychiatric disorders.
- The dosage of methylprednisolone may need to be adjusted in the elderly and in people who are obese.
- May interact with several other drugs including some anti-infectives, antidiabetic agents, bupropion, NSAIDs, and drugs metabolized by CYP 3A4 liver enzymes.
- Only use during pregnancy if the benefits outweigh the risks. Observe infants born to mothers who have been taking methylprednisolone during pregnancy for signs of hypoadrenalism.
Note: In general, seniors or children, people with certain medical conditions (such as liver or kidney problems, heart disease, diabetes, seizures) or people who take other medications are more at risk of developing a wider range of side effects. View complete list of side effects
4. Tips
- Take oral methylprednisolone with food and a full glass of water to reduce the risk of it adversely affecting your stomach.
- Take exactly as directed by your doctor. Sometimes it may only need to be taken every other day. Follow the dosage instructions exactly and never increase the dosage unless under your doctor's advice. The dosage of methylprednisolone varies widely among individuals and can change depending on underlying conditions and concomitant medications. Some doctors will prescribe methylprednisolone to be taken every other day (this is called Alternate Day Therapy).
- Stopping methylprednisolone suddenly can be dangerous. Your doctor will advise you on how to taper down your methylprednisolone dose if you have been taking it for more than a few weeks.
- If you are taking methylprednisolone, you should not receive any live or live-attenuated vaccines. Your response to killed or inactivated vaccines may also be diminished.
- Avoid contact with anybody known to have, or recently exposed to, viral illnesses such as chickenpox or measles. If you inadvertently come into contact with somebody, contact your doctor immediately as immune globulin or antiviral treatment may be required.
- Limit or avoid alcohol use while taking methylprednisolone to help reduce the risk of indigestion and the development of stomach ulcers.
- Talk with your doctor as soon as possible if you are taking methylprednisolone and you develop any worrying side effects, such as fluid retention, muscle weakness, abdominal distention, convulsions, or difficulties with your vision.
- Tell your doctor if you intend to become pregnant or if you inadvertently become pregnant while taking methylprednisolone. No adverse effects on the infant have been reported when methylprednisolone has been used during breastfeeding.
5. Response and effectiveness
- The onset of effect is one hour for the IV injection and up to one week when given into a joint. The effects of methylprednisolone, when given directly into a joint, last for one to five weeks.
- For the oral formulation, the time to peak effect is two hours.
6. Interactions
Medicines that interact with methylprednisolone may either decrease its effect, affect how long it works, increase side effects, or have less of an effect when taken with methylprednisolone. An interaction between two medications does not always mean that you must stop taking one of the medications; however, sometimes it does. Speak to your doctor about how drug interactions should be managed.
Common medications that may interact with methylprednisolone include:
- antibiotics, such as clarithromycin, erythromycin, rifabutin, rifampin, or troleandomycin
- anticholinesterases, such as neostigmine, or pyridostigmine
- anticoagulants (blood thinners) such as apixaban, dabigatran, fondaparinux, heparin, or warfarin
- antidepressants, such as desipramine, fluoxetine, sertraline, or St. John's Wort
- antifungal medications, such as itraconazole, ketoconazole, or voriconazole
- antinausea medications, such as aprepitant
- aspirin
- epilepsy medications, such as carbamazepine, oxcarbazepine, phenobarbital, phenytoin, or primidone
- estrogen-containing hormonal contraceptives (includes birth control pills, patches, rings, implants, and injections)
- heart medications, such as amiodarone, atenolol, diltiazem, or verapamil
- HIV medications (eg, atazanavir, delavirdine, efavirenz, indinavir, etravirine, ritonavir, nevirapine, saquinavir, or tipranavir)
- immunosuppressants, such as cyclosporine
- nonsteroidal anti-inflammatories (NSAIDs), such as celecoxib, diclofenac, etodolac, ibuprofen, ketorolac, meloxicam, nabumetone, or naproxen
- other corticosteroids, such as dexamethasone or prednisone
- potassium-depleting agents, such as amphotericin B Injection and diuretics (eg, furosemide, hydrochlorothiazide)
- some asthma medications, such as zafirlukast
- vaccines (may inhibit the immune response)
- others, such as aminoglutethimide, bupropion, cholestyramine, cyclosporine, digoxin, isoniazid, quetiapine, or thalidomide.
Methylprednisolone may increase blood glucose concentrations in people with diabetes and dosage adjustments of antidiabetic agents (eg, insulin, glyburide) may be required. Using methylprednisolone with fluoroquinolone antibiotics (such as ciprofloxacin or levofloxacin) may increase the risk of tendon rupture with fluoroquinolones.
In addition, alcohol can increase the likelihood of gastrointestinal side effects with methylprednisolone, and possibly liver and kidney damage. Methylprednisolone may suppress the inflammatory response to skin tests.
Note that this list is not all-inclusive and includes only common medications that may interact with methylprednisolone. You should refer to the prescribing information for methylprednisolone for a complete list of interactions.