Drug Detail:Prednisolone (systemic) (monograph) (Orapred)
Drug Class:
1. How it works
- Prednisolone is a corticosteroid that may be used to reduce inflammation and calm down an overactive immune system. It has predominantly glucocorticoid activity and low mineralocorticoid activity, which means it affects the immune response and inflammation rather than affecting the body's balance of electrolytes and water.
- Prednisolone mimics the effect of cortisol, a hormone released by the adrenal glands (located on top of the kidneys) that regulates metabolism and stress.
- Prednisolone belongs to the class of medicines known as corticosteroids. Specifically, it is a glucocorticoid.
2. Upsides
- Prednisolone can help dampen down an over-reactive immune system and reduce inflammation.
- May be used in the treatment of allergies, arthritis, certain blood disorders, cancer, endocrine disorders, inflammatory bowel diseases, swelling, and skin conditions.
- Typically only taken as a short course.
- Prednisolone also helps to control moderate-to-severe asthma attacks by controlling inflammation.
- Prednisolone is the active form of prednisone (prednisone is metabolized in the liver first to become prednisolone).
- Has five times the glucocorticoid activity of hydrocortisone and less than 10% of hydrocortisone's mineralocorticoid activity.
- Available as an oral tablet, orally disintegrating tablet, oral suspension, and ophthalmic solution.
- Generic prednisolone 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:
- Acne, dizziness, facial flushing, general aches and pains, headache, an increased appetite that may result in weight gain, increased sweating, indigestion, and insomnia are the most common side effects reported.
- May also cause facial hair growth (especially in women), high blood pressure, slow skin healing and skin thinning, osteoporosis (brittle bones), the onset of diabetes, sodium and water retention, and stomach ulcers with long-term use.
- Side effects are more likely to be experienced at higher dosages.
- Limit or avoid alcohol use while taking prednisolone to help prevent stomach ulcers.
- With high doses of corticosteroids, ‘live vaccines’ should be delayed until several months after corticosteroid treatment has stopped.
- Children may be especially sensitive to the effects of prednisolone. Prolonged prednisolone use may affect growth and development in children.
- All corticosteroids, including prednisolone, can cause salt and fluid retention, which may lead to blood pressure elevation and increased potassium excretion. Calcium excretion is also increased.
- Cataracts, glaucoma, eye infections, an increase in new episodes of optic neuritis, and corneal perforation associated with herpes simplex of the eye, have all been reported with prednisolone use.
- Prednisolone may cause low potassium levels (hypokalemia), which may be potentiated by other drugs that also cause hypokalemia (such as diuretics, amphotericin B).
- Prednisolone is considerably more expensive than prednisone, but its effectiveness is similar.
- May cause withdrawal symptoms if stopped suddenly after long-term or high-dose therapy. Symptoms include fever, vomiting, loss of appetite, diarrhea, weight loss, general aches, and pains.
- May not be suitable for some people including those with fungal infections, thyroid disorders, herpes infection of the eyes, mental health issues, stomach ulcers, liver disease, high blood pressure, osteoporosis, myasthenia gravis, or multiple sclerosis.
- Prednisolone may interact with several other medications including anticholinesterase agents, antidiabetic agents, anticoagulants, digoxin, estrogens, NSAIDs, and vaccinations (including both live and inactivated vaccines). It may also suppress the reaction to some skin tests.
- Should not be used during pregnancy unless the benefits outweigh the risks. Corticosteroids, such as prednisolone can cause fetal harm when administered to a pregnant woman; an increased risk of orofacial clefts is associated with use during the first trimester. Intrauterine growth restriction and decreased birth weight have also been reported. Animal studies have found prednisolone to be teratogenic. Prednisolone is present in human milk at doses less than 1% of the maternal daily dose. Use the lowest possible dose during breastfeeding because high doses could potentially produce problems in the breastfed infant such as growth and developmental delays and interfere with endogenous corticosteroid production.
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 with food and a full glass of water.
- Single doses are preferred over split doses.
- Take exactly as directed by your doctor. Sometimes dosing for prednisolone may seem complicated. Follow the prescription label and your doctor's instructions exactly. If you have any concerns, ask your doctor. Do not take more or less prednisolone than prescribed.
- Take prednisolone in the morning preferably before 9 AM to more closely mimic your body's natural secretion of cortisol.
- If you are taking prednisolone suspension or giving a dose to a child, shake the suspension well and ensure you use a properly calibrated dosing syringe, rather than a kitchen teaspoon, to accurately measure the dose.
- Keep prednisolone disintegrating tablets unopened in their packet until it is time to take them. Use dry hands to open the packet, and peel back the foil from the tablet, rather than trying to push the tablet through. Place the tablet in your mouth and allow it to disintegrate, do not crush or chew.
- Prednisolone ophthalmic solution is not compatible with contact lenses. Ask your doctor or health care professional when you can wear your lenses again.
- Stopping prednisolone suddenly can be dangerous. Do not stop taking without a doctor's advice. People who have taken prednisolone long-term must slowly wean themselves off it over days or weeks, following their doctor's instructions.
- Avoid alcohol while you are taking prednisolone.
- Prednisolone may affect blood sugar readings in people with diabetes. Talk to your doctor about how you should manage this.
- Talk to your doctor if you become unwell or stressed while taking prednisolone. Your dosage may need to be adjusted temporarily.
- 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.
- Tell other health care professionals, including your dentist, that you are taking prednisolone. Talk to your doctor or pharmacist before taking any other medications with prednisolone, including those bought over-the-counter, because some may not be compatible with prednisolone.
- Tell your doctor if you are breastfeeding, pregnant, or intending to become pregnant because prednisolone may not be suitable for you.
5. Response and effectiveness
- Effects can last from 18-36 hours, meaning that alternate-day dosing is possible.
- Temporary dosage increases may be necessary during disease flare-ups or during times of stress or infection.
- Prednisolone is five times more potent at relieving inflammation than naturally occurring cortisol.
6. Interactions
Medicines that interact with prednisolone may either decrease its effect, affect how long it works for, increase side effects, or have less of an effect when taken with prednisolone. 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 prednisolone 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, diltiazem, or verapamil
- HIV medications (eg, atazanavir, delavirdine, efavirenz, indinavir, etravirine, ritonavir, nevirapine, saquinavir, or tipranavir)
- immunosuppressants, such a cyclosporine
- nonsteroidal anti-inflammatories (NSAIDs), such as celecoxib, diclofenac, etodolac, ibuprofen, ketorolac, meloxicam, nabumetone, or naproxen
- other corticosteroids, such as dexamethasone
- 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.
Prednisolone may increase blood glucose concentrations in people with diabetes and dosage adjustments of antidiabetic agents (eg, insulin, glyburide) may be required. Use with fluoroquinolone antibiotics (such as ciprofloxacin, levofloxacin) may increase the risk of tendon rupture with fluoroquinolones.
In addition, alcohol can increase the likelihood of gastrointestinal side effects with prednisolone, and possibly liver and kidney damage. Prednisolone 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 prednisolone. You should refer to the prescribing information for prednisolone for a complete list of interactions.