Prednisolone acetate ophthalmic suspension (eye drops) is prepared as a sterile ophthalmic suspension and used to reduce swelling,redness,itching, andallergic reactions affecting the eye.[33][8][34] It has been explored as a treatment option for bacterialkeratitis.[35]
Dermatological effects including reddening of the face, bruising/skin discoloration, impaired wound healing,skin atrophy,skin rash,edema, and abnormal hair growth
Lower response to hormones, especially during stressful instances such as surgery or illness
Change in electrolytes: rise inblood pressure, increased sodium and low potassium, leading toalkalosis
Gastrointestinal system effects: swelling of the stomach lining, reversible increase in liver enzymes, and risk ofstomach ulcers
Muscular and skeletal abnormalities, such as muscle weakness/muscle loss,osteoporosis (seesteroid-induced osteoporosis), long bone fractures, tendon rupture, and back fractures
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 ofcleft palate.
Prednisolone is found in the breast milk of mothers taking prednisolone.[43]
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.[29]
Corneal thinning: When corticosteroids are used in the long term, corneal andscleral thinning is also one of its consequences. When not ceased, thinning may ultimately lead to perforation of the cornea.[29]
Glaucoma: Elongated use of corticosteroids has a chance of causing a raised intraocular pressure (IOP), injuring the optic nerve, and weakening 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.[29]
As aglucocorticoid, the lipophilic structure of prednisolone allows for easy passage through the cell membrane where it then binds to its respectiveglucocorticoid receptor (GCR) located in the cytoplasm. Upon binding, the formation of the GC/GCR complex causes dissociation ofchaperone proteins from the glucocorticoid receptor enabling the GC/GCR complex to translocate inside the nucleus.[47] This process occurs within 20 minutes of binding. Once inside the nucleus, thehomodimer 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 the synthesis of anti-inflammatory proteins while binding to negative GREs blocks thetranscription of inflammatory genes.[48] They inhibit the release of signals that promote inflammation such asnuclear factor-Kappa B (NF-κB),Activator protein 1 (AP-1),nuclear factor of activated T-cells (NFAT), and stimulate anti-inflammatory signals such as theinterleukin-10 gene.[49][14] All of them will collectively cause a sequence of events, including the inhibition ofprostaglandin synthesis and additional inflammatory mediators.Glucocorticoids also inhibitneutrophilcell death anddemargination. As well asphospholipase A2, which in turn lessensarachidonic acid derivative genesis.[50]
Prednisolone has a relatively shorthalf-life, ranging 2–4 hours. It also has a largetherapeutic window, considering the dosage required to produce a therapeutic effect is a few times higher than what the body naturally produces.[14]
Both prednisolonephosphate and prednisoloneacetate go throughesterhydrolysis in the body to form prednisolone. It subsequently undergoes the usualmetabolism of prednisolone. Concomitant use of prednisolone and strongCYP3A4 inhibitors such asketoconazole is shown to cause a rise in plasma prednisolone concentrations by about 50% owing to a diminishedclearance.[49]
Prednisolone predominantly undergoeskidney elimination and is excreted in theurine assulphate and metabolites ofglucuronide conjugate.[14]
Prednisone is aprodrug 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.[51]
Prednisolone is asyntheticpregnanecorticosteroid closely related to its cognateprednisone, having identical structure save for two fewer hydrogens near C11. It is also known asδ1-cortisol,δ1-hydrocortisone,1,2-dehydrocortisol, or1,2-dehydrohydrocortisone, as well as11β,17α,21-trihydroxypregna-1,4-diene-3,20-dione.[52][53]
Co-administration of prednisolone eye drops with ophthalmicnonsteroidal anti-inflammatory drugs (NSAIDs) may perhaps exacerbate its effects, causing unwanted side effects such as toxicity.[clarification needed] The wound healing process may also be hindered.[54]
Prolonged use of prednisolone eye drops in children may lead to 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.[29]
Research on animal reproduction has indicated that there is a trace ofteratogenicity when doses are reduced by 10 times the human recommended dose.[56] There is no sufficient information on human pregnancy at this moment. Use is only recommended when the potential benefits outweigh the potential risks for the pregnant mother and the fetus.[56]
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.[29][56] However, the presence of corticosteroids is recorded when they are administered systemically, and it could affect the fetus' growth.[56] Therefore, the use of prednisolone during breastfeeding is not advocated.[56]
As a glucocorticosteroid, unauthorized or ad hoc use of prednisolone during competition via oral, intravenous, intramuscular, or rectal routes is banned underWorld Anti-Doping Agency (WADA) anti-doping rules.[58]
Prednisolone is used in the treatment of inflammatory and allergic conditions in cats, dogs, horses, small mammals such asferrets, birds, and reptiles.[59][60] Its usage in treating inflammation, immune-mediated disease,Addison's disease, andneoplasia is often consideredoff-label use. Many drugs are commonly prescribed for off-label use inveterinary medicine."[61] Studies in ruminating species, such asalpacas, have shown that oral administration of the drug is associated with a reducedbioavailability compared to intravenous administration; however, levels that are therapeutic in other species can be achieved with oral administration in alpacas.[62]
It is used in a broad spectrum of diseases, for example, inflammation of scleral tissues, cornea, and conjunctiva in dogs.[59] In horses, prednisolone acetate suspensions are priorly used to treat inflammation in the middle layer of the eye, also known asanterior uveitis andequine recurrent uveitis (ERU), which is the leading cause of visual impairment in horses.[60] Prednisolone acetate eye drops are not to be used in other animals such as birds.[59]
Prednisolone acetate eye drops are also prescribed to dogs and cats to lessen swelling,redness, burning, and pain sensations after surgeries of the eye.[59]
Cats with conjunctivitis usually are required to avoid using ophthalmic preparations ofcorticosteroids and its derivatives. The most typical infections are caused byherpes virus.[60]
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^Arslan N, Tepe D, Taştan E, Demirci M, Caydere M, Ustun H, et al. (November 2012). "Evaluation of the effectiveness of topical ciprofloxacin and prednisolone in the prevention of myringosclerosis".European Archives of Oto-rhino-laryngology.269 (11). EUFOS: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.
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