Prednizol

Therapeutic action

Prednizol contains Prednisolone, an anti-inflammatory Corticosteroid


Pharmacokinetics and pharmacodynamics in humans

Prednisolone is a glucocorticoid with an anti-inflammatory potency 3 to 5 times greater than that of hydrocortisone. Its concentration at 1% gives it a high anti-inflammatory power that quickly controls inflammatory eye conditions, whether due to complicated surgeries, trauma or uveitis or allergic eye reactions.

Prednisolone is acceptably absorbed in the aqueous humor, cornea, iris, choroid, ciliary body, and retina. It is transported by a simple diffusion mechanism from a concentration gradient to subsequently pass into the systemic circulation. The drug can accumulate in the aqueous humor and later distribute to other ocular structures, as well as potentially to the systemic circulation via the trabecular meshwork.

Systemic absorption is significant at high doses or in prolonged pediatric treatment. Prednisolone is bound to plasma proteins in 70 to 90% and its half-life is 2 to 4 hours.

Ophthalmic drugs when excreted via tears and drain into the nasal mucosa may undergo systemic distribution by virtue of the nasal absorption present. The biotransformation of the drug is significant, since the local tissues of the eye contain a variety of enzymes including esterases, oxidoreductoras, glutathione-conjugating enzymes and metabolite-producing corticosteroids beta hydroxylase, which once transported to the systemic circulation are mainly metabolized in the liver and are excreted in the urine in the form of conjugated sulfates and glucuronides.

Like other steroids, prednisolone inhibits the inflammatory response of edema, fibrin deposition, capillary dilation, collagen deposition, and scarring due to agents of a mechanical, immunological, or chemical nature.


Composition

Each ml contains:

Prednisolone Acetate 10 mg

Excipients and purified water C.S.P. 1 ml

Posology and administration 

 

Administration route: Ophthalmic.

Dosage:

1 to 2 drops instilled into the conjunctival sac twice daily. During the initial 24 hours to 48 hours, the dose can be safely increased to two drops every hour. Care should be taken not to discontinue therapy prematurely.

Storage recommendations

Store at a temperature between 15 °C and 25 °C. Protect  from freezing.

 

Presentation

Box containing a dropper bottle with 5 ml of suspension.

Note: Sale by prescription.

Shake well before use.

Indications

Prednizol is indicated to treat noninfectious inflammations of the palpebral and bulbar conjunctiva, the cornea, and the anterior segment of the globe that responds to the steroid.

Drug interactions

Steroids decrease the action of antibiotics but this can be avoided by increasing the dose of antibiotics. Topical anesthetics can increase the absorption of topical drugs and favor the appearance of adverse effects. Combinations containing any of the following medications, depending on the amount present, may interact with the product: antiglaucomatous agents, (chronic or intense use of ophthalmic corticosteroids can increase intraocular pressure and decrease the efficacy of antiglaucomatous agents). Anticholinergics, especially atropine or related compounds (the risk of ocular hypertension may increase with the use of prolonged corticosteroid therapy; it may be more likely to occur during therapy of cycloplegic / mydriatic agents in acute angle glaucoma). Contact lenses (increased risk of infections).

Contraindications

Hypersensitivity to the components of the formula, epithelial herpes simplex keratitis (dendritic keratitis), vaccinia, chickenpox and other virulent corneal diseases, ocular tuberculosis, fungal conditions of the eyeball, acute purulent eye infections, viral keratoconjunctivitis, corneal erosion by strange body.

Warnings

Long-term use of steroids can cause glaucoma, with damage to the optic nerve, defect in visual acuity and visual field, and formation of posterior subcapsular cataract. Intraocular pressure should be routinely recorded, even if this is difficult in children and in uncooperative patients. Prolonged use can suppress the patient’s defense response and thus increase the risk of secondary eye infections. In those diseases that cause a thinning of the cornea or sclera, perforations have been reported with the use of topical steroids. In acute purulent infections of the eyeball, steroids can mask the infection and thus promote it.

The application of corticosteroids can activate, exacerbate or mask eye infections by viruses, bacteria or fungi.

Precautions or restrictions on use during pregnancy and lactation

There are no controlled studies in pregnant women. However, Prednizol should not be used during pregnancy, unless its use is strictly necessary. It is not known whether prednisolone topical can be excreted in human milk. It is recommended to use with caution during lactation.

Pediatric use

Corticosteroids should be used with caution in children 2 years of age or younger, because the different dose / weight ratio for children increases the risk of adrenal suppression. This risk increases with the duration of treatment, which should therefore be limited to a period as short as possible (preferably less than 5 days).

Side Effects

 

Prolonged use of topical corticosteroids may promote increased intraocular pressure, which can be associated with damage to the optic nerve and defects in the visual fields, formation of posterior subcapsular cataract, secondary eye infections by viruses or fungi released from the eye tissues. and delayed wound healing. In addition, myopathy characterized by palpebral ptosis or mild mydriasis may occur, as well as probable corneal perforation in patients who are thinning the cornea.