Side effects with short-term use include nausea, inability to concentrate, insomnia, or feeling tired.[5] More severe side effects include psychiatric problems, which may occur in about 5% of people.[9] Common side effects with long term use include
bone loss, weakness,
yeast infections, and easy bruising.[6] While short-term use in the later part of
pregnancy is safe, long-term use or use in early pregnancy is occasionally associated with harm to the baby.[1] It is a
glucocorticoid made from
hydrocortisone (cortisol).[10]
Prednisolone acetate ophthalmic suspension (eye drops) is an adrenocortical steroid product, prepared as a sterile ophthalmic suspension and used to reduce swelling, redness, itching, and
allergic reactions affecting the eye.[30][8][31] It has been explored as a treatment option for
bacterial keratitis.[32]
Dermatological effects including reddening of face, bruising/skin discoloration, impaired wound healing, thinning of skin, skin rash, fluid build up and abnormal hair growth
Hyperglycemia; patients with diabetes may need increased
insulin or diabetic therapies
Menstrual abnormalities
Lower response to hormones, especially during stressful instances such as surgery or illness
Change in electrolytes: rise in
blood pressure, increased sodium and low potassium, leading to
alkalosis
GI system effects: swelling of stomach lining, reversible increase in liver enzymes, and risk of
stomach ulcers
Muscular and skeletal abnormalities, such as muscle weakness/muscle loss,
osteoporosis (see
steroid-induced osteoporosis), long bone fractures, tendon rupture, and back fractures
Neurological effects, including involuntary movements (
convulsions), headaches, and
vertigo
Psychosocial behavioral and emotional disturbances[38] with
aggression being one of the most common cognitive symptoms or symptoms overall, especially with oral use.[39]
Nasal septum perforation and bowel perforation (in some pathologic conditions).[40][41]
Withdrawal from prednisolone after long-term or high-dose use can lead to
adrenal insufficiency.[38]
Pregnancy and breastfeeding
Although there are no major human studies of prednisolone use in pregnant women, studies in several animals show that it may cause birth defects including increased likelihood of
cleft palate.
Prednisolone is found in breast milk of mothers taking prednisolone.[38]
Local adverse effects in the eye
When used topically on the eye, the following are potential side-effects:
Cataracts: Extended usage of corticosteroids may cause clouding at the back of the lens, also known as posterior subcapsular cataract. This type of cataract reduces the path of light from reaching the eye, which interferes with a person's reading vision. Consumption of prednisolone eye drops post surgery may also retard the healing process.[26]
Corneal thinning: When corticosteroids are used in the long term, corneal and
scleral thinning is also one of its consequences. When not ceased, thinning may ultimately lead to perforation of the cornea.[26]
Glaucoma: Elongated use of corticosteroids has a chance of causing a raised intraocular pressure (IOP), injuring the optic nerve and weakening of visual awareness. Corticosteroids should be used cautiously in patients with concomitant conditions of glaucoma. Doctors track patients' IOP if they are using corticosteroid eye drops for more than 103 days.[26]
Pharmacology
Pharmacodynamics
As a
glucocorticoid, the lipophilic structure of prednisolone allows for easy passage through the cell membrane where it then binds to its respective
glucocorticoid receptor (GCR) located in the cytoplasm. Upon binding, formation of the GC/GCR complex causes dissociation of
chaperone proteins from the glucocorticoid receptor enabling the GC/GCR complex to translocate inside the nucleus.[42] This process occurs within 20 minutes of binding. Once inside the nucleus, the
homodimer GC/GCR complex binds to specific DNA binding-sites known as glucocorticoid response elements (GREs) resulting in gene expression or inhibition. Complex binding to positive GREs leads to synthesis of anti-inflammatory proteins while binding to negative GREs blocks the
transcription of inflammatory genes.[43] They inhibit the release of signals that promote inflammation such as
nuclear factor-Kappa B (NF-κB),
Activator protein 1 (AP-1),
nuclear factor of activated T-cells (NFAT), and stimulate anti-inflammatory signals such as the
interleukin-10 gene.[44][45] All of them will collectively cause a sequence of events, including the inhibition of
prostaglandin synthesis and additional inflammatory mediators.
Glucocorticoids also inhibit
neutrophilcell death and
demargination. As well as
phospholipase A2, which in turn lessens
arachidonic acid derivative genesis.[46]
Pharmacokinetics
Prednisolone has a relatively short
half-life, ranging 2–4 hours. It also has a large
therapeutic window, considering the dosage required to produce a therapeutic effect is a few times higher than what the body naturally produces.[45]
Both prednisolone
phosphate and prednisolone
acetate go through
esterhydrolysis in the body to form prednisolone. It subsequently undergoes the usual
metabolism of prednisolone. Concomitant use of prednisolone and strong
CYP3A4 inhibitors such as
ketoconazole is shown to cause a rise in plasma prednisolone concentrations by about 50% owing to a diminished
clearance.[44]
Prednisolone predominantly undergoes
kidney elimination and is excreted in the
urine as
sulphate and metabolites of
glucuronide conjugate.[45]
Prednisone
Prednisone is a
prodrug that is activated in the liver. When it enters the body, prednisone is triggered by the liver and body chemicals to turn into its active form, prednisolone.[47]
Chemistry
Prednisolone is a
syntheticpregnanecorticosteroid closely related to its cognate
prednisone, having identical structure save for two fewer hydrogens near C11. It is also known as δ1-cortisol, δ1-hydrocortisone, 1,2-dehydrocortisol, or 1,2-dehydrohydrocortisone, as well as 11β,17α,21-trihydroxypregna-1,4-diene-3,20-dione.[48][49]
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Minor contraindications and drug reactions
Co-administration of prednisolone eye drops with ophthalmic
nonsteroidal anti-inflammatory agents (NSAIDs) may perhaps exacerbate its effects, causing unwanted side effects such as toxicity. The wound healing process may also be hindered.[51]
When used in low doses, corticosteroids serve as an
anti-inflammatory agent. At higher doses, they are considered as
immunosuppressives.[45] Corticosteroids inhibit the inflammatory response to a variety of inciting agents and, it is presumed, delay or slow healing.[52] They inhibit the edema, fibrin deposition, capillary dilation,
leukocyte migration, capillary proliferation, fibroblast proliferation, deposition of
collagen, and scar formation with inflammation.[53]
Special populations
Child use
Prolonged use of prednisolone eye drops in children may lead to a raised intraocular pressure. While this phenomenon is dose dependent, it is shown to have a greater effect especially in children under 6 years of age.[26]
Pregnancy and breastfeeding
Researches on animal reproduction have indicated that there is a trace of
teratogenicity when doses are reduced by 10 times of the human recommended dose.[54] There is no sufficient information on human pregnancy at this moment. Use is only recommended when the potential benefits outweigh the potential risks of the pregnant mother and the fetus.[54]
Prednisolone when delivered systemically can be found in the mother's breast milk, however, there is no data provided for the extent of prednisolone found in the system after administering eye drops.[26][54] However, the presence of corticosteroids is recorded when they are administered systemically, and it could possibly affect the fetus' growth.[54] Therefore, use of prednisolone during breastfeeding is not advocated.[54]
Society and culture
Dosage forms
Prednisolone is supplied as oral liquid, oral suspension, oral syrup, oral tablet, and oral disintegrating tablet. It may be a generic medication or supplied as brands Flo-Pred (prednisolone acetate oral suspension),[37] Millipred (oral tablets),[22] Orapred (prednisolone sodium phosphate oral dissolving tablets),[7] Pediapred (
prednisolone sodium phosphate oral solution),[38] Veripred 20, Prelone, Hydeltra-T.B.A., Hydeltrasol, Key-Pred, Cotolone, Predicort, Medicort, Predcor, Bubbli-Pred, Omnipred (prednisolone acetate ophthalmic suspension),[8] Pred Mild,[31] Pred Forte,[30] and others.[55]
Athletics
As a glucocorticosteroid, unauthorized or ad hoc use of prednisolone during competition via oral, intravenous, intramuscular or rectal routes is banned under
World Anti-Doping Agency (WADA) anti-doping rules.[56]
Veterinary uses
Prednisolone is used in the treatment of inflammatory and allergic conditions in cats, dogs, horses, small mammals such as
ferrets, birds, and reptiles.[57][58] Its usage in treating inflammation, immune-mediated disease,
Addison's disease, and
neoplasia is often '
off label' or 'extra label'. Many drugs are commonly prescribed for off label use in
veterinary medicine."[59] Studies in ruminating species, such as alpacas, have shown that oral administration of the drug is associated with a reduced
bioavailability compared to intravenous administration; however, levels that are therapeutic in other species can be achieved with oral administration in alpacas.[60]
It is used in a broad spectrum of diseases, for example, inflammation of scleral tissues, cornea, conjunctiva in dogs.[57] In horses, prednisolone acetate suspensions are priorly used to treat inflammation in the middle layer of the eye, also known as
anterior uveitis and
equine recurrent uveitis (ERU), which is the leading cause of visual impairment in horses.[58] Prednisolone acetate eye drops are not to be used in other animals such as birds.[57]
Prednisolone acetate eye drops are also prescribed to the dogs and cats to lessen swelling,
redness, burning and pain sensations after surgeries of the eye.[57]
Cats with conjunctivitis usually are required to avoid using ophthalmic preparations of
corticosteroids and its derivatives. The most typical infections are caused by
herpes virus.[58]
^Bergrem H, Grøttum P, Rugstad HE (1983). "Pharmacokinetics and protein binding of prednisolone after oral and intravenous administration". European Journal of Clinical Pharmacology. 24 (3): 415–9.
doi:
10.1007/BF00610064.
PMID6861855.
S2CID33189235.
^
abStuart MC, Kouimtzi M, Hill SR, eds. (2009). WHO Model Formulary 2008. World Health Organization. pp. 53–54.
hdl:
10665/44053.
ISBN978-924154765-9.
^
abcde"Prednisolone". The American Society of Health-System Pharmacists.
Archived from the original on 23 December 2016. Retrieved 8 December 2016.
^Organization, World Health (2019). World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization.
hdl:10665/325771. WHO/MVP/EMP/IAU/2019.06.
^Lambrou GI, Vlahopoulos S, Papathanasiou C, Papanikolaou M, Karpusas M, Zoumakis E, Tzortzatou-Stathopoulou F (December 2009). "Prednisolone exerts late mitogenic and biphasic effects on resistant acute lymphoblastic leukemia cells: Relation to early gene expression". Leukemia Research. 33 (12): 1684–95.
doi:
10.1016/j.leukres.2009.04.018.
PMID19450877.
^Arslan N, Tepe D, Taştan E, Demirci M, Caydere M, Ustun H, Oguz H (November 2012). "Evaluation of the effectiveness of topical ciprofloxacin and prednisolone in the prevention of myringosclerosis". European Archives of Oto-Rhino-Laryngology. 269 (11): 2335–2341.
doi:
10.1007/s00405-011-1889-z.
PMID22197890.
S2CID23472925.
^Wilhelmus KR, Gee L, Hauck WW, Kurinij N, Dawson CR, Jones DB, et al. (April 2020). "Herpetic Eye Disease Study: A Controlled Trial of Topical Corticosteroids for Herpes Simplex Stromal Keratitis". Ophthalmology. 127 (4S): S5–S18.
doi:
10.1016/j.ophtha.2020.01.037.
PMID32200827.
S2CID214616647.
^Gayam K, Ramulu PY, Rengaraj V, Srinivasan K (29 February 2020). "Safety and Efficacy of 0.1% Nepafenac versus 1% Prednisolone Acetate Eye Drops after Laser Peripheral Iridotomy: A Prospective, Randomized Trial". Ophthalmology. Glaucoma. 3 (3): 174–180.
doi:
10.1016/j.ogla.2020.02.006.
PMID32672612.
S2CID90234022.
^Cervin A, Andersson M (September 1998). "Intranasal steroids and septum perforation--an overlooked complication? A description of the course of events and a discussion of the causes". Rhinology. 36 (3): 128–32.
PMID9830677.
US patent 2837464, Arthur Nobile, "Process for production of dienes by corynebacteria", published 1958-06-03, issued 1958-06-03, assigned to Schering Corp