unoprostone ophthalmic

Action and Spectrum

Actions and Spectrum: 

unoprostone ophthalmic is a medication used to treat open-angle glaucoma or ocular hypertension, which causes increased eye pressure. The mechanism of action of unoprostone ophthalmic is believed to involve several different pathways: 

• Increases aqueous outflow: unoprostone is thought to increase the outflow of aqueous humor, the clear fluid that fills the front of the eye through the trabecular meshwork, a sieve-like structure in the eye that drains the fluid. This helps to reduce the pressure in the eye. 
• Modulates ion channels: unoprostone may also modulate ion channels in the eye, which can help to reduce the production of aqueous humor and further lower the pressure in the eye. 
• The spectrum of activity of unoprostone ophthalmic is limited to the eye, and its effects are primarily local. unoprostone ophthalmic is not effective against other types of eye conditions or infections. 

Drug Interaction

Adverse Reaction

Frequency defined 

>10% 

Dry eyes (10-25%) 

Increased length of eyelashes (10-25%) 

Burning/stinging (10-25%) 

Itching (10-25%) 

Conjunctival injection (10-25%)  

1-10% 

Eyelid disorder (5-10%) 

Lacrimation disorder(5-10%) 

Blepharitis (1-5%) 

Conjunctivitis (1-5%) 

Ocular discharge/bleeding/pain (1-5%) 

Irritation (1-5%) 

Vitreous disorder (1-5%) 

Conjunctival hyperemia (1-5%) 

Foreign body sensation (5-10%) 

Decreased length of eyelashes (5-10%) 

Corneal lesion/erosion (1-5%) 

Keratitis (1-5%) 

Photophobia (1-5%) 

Blurred vision (1-5%) 

Abnormal vision (5-10%) 

Cataract (1-5%)  

<1% 

Acute elevated IOP 

Corneal deposits 

Corneal opacity 

Diplopia 

Ptosis 

Visual field defect 

Hyperpigmentation of the eyelid or iris and increased number of eyelashes 

Color blindness 

Corneal edema 

Optic atrophy 

Retinal hemorrhage  

Post marketing reports 

Dry mouth 

Vomiting 

Chemosis 

Nausea 

Palpitations 

Black Box Warning

Contraindication / Caution

Contraindications/caution: 

Contraindications: 

• Hypersensitivity: unoprostone ophthalmic should not be used in patients who are allergic or hypersensitive to the medication or any of its components. 
• Pregnancy and breast-feeding: unoprostone ophthalmic may be unsafe during pregnancy and breast-feeding.  
• Active intraocular inflammation: unoprostone ophthalmic may worsen active intraocular inflammation and should not be used in patients with active inflammation in the eye. 
• Intraocular surgery: unoprostone ophthalmic should not be used immediately before or after intraocular surgery, as it may increase the risk of complications. 
• Contact lens use: unoprostone ophthalmic may contain preservatives that can be absorbed by soft contact lenses, leading to discoloration of the lenses. Patients should be advised to remove their contact lenses before using the medication and wait at least 15 minutes before reinserting them. 

Caution: 

• Corneal problems: Patients with certain types of corneal problems, such as Fuchs’ endothelial dystrophy, may experience worsening of their condition using unoprostone ophthalmic. 
• Cataract surgery: Patients who have had cataract surgery may be at an increased risk of developing inflammation in the eye with the use of unoprostone ophthalmic. 
• Contact lenses: Patients who wear contact lenses should remove them before using unoprostone ophthalmic, as the medication may cause discoloration or damage. 
• Systemic effects: While unoprostone ophthalmic is primarily used locally in the eye, some systemic effects may occur, such as headache, dizziness, and nausea. 
• Eye irritation: Some patients may experience eye irritation, burning, or stinging with unoprostone ophthalmic. 

Pregnancy / Lactation

Pregnancy consideration: C 

Lactation: Excretion of the drug in human breast milk is unknown 

Pregnancy category: 

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.   

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

• unoprostone is a medication used in ophthalmology to treat open-angle glaucoma or ocular hypertension. It is a synthetic prostaglandin analog that increases the outflow of aqueous humor from the eye, thus reducing intraocular pressure. 
• The ophthalmic formulation of unoprostone is available as a sterile ophthalmic solution with a concentration of 0.15% (15 micrograms/mL). The recommended dose is one drop in the affected eye(s) once daily, preferably in the evening. 

Pharmacodynamics: 

• unoprostone ophthalmic solution is a synthetic prostaglandin analog that acts by binding to and activating prostaglandin FP receptors in the eye’s ciliary muscle.  
• This activation leads to an increase in the outflow of aqueous humor from the eye, which results in a reduction in intraocular pressure. 
• The exact mechanism by which unoprostone increases aqueous humor outflow has yet to be fully understood. However, it is thought to be related to changes in the extracellular matrix of the trabecular meshwork, which is the primary site of aqueous humor outflow resistance in the eye.  
• unoprostone may also increase the permeability of the ciliary epithelium to aqueous humor, further enhancing outflow. 

Pharmacokinetics: 

Absorption 

unoprostone is absorbed through the cornea and conjunctival epithelium after topical administration to the eye. The drug is well absorbed, and peak concentrations in the aqueous humor are reached within one hour of administration. 

Distribution 

unoprostone is distributed to the eye tissues after topical administration, with the minimal systemic distribution. 

Metabolism 

unoprostone is metabolized primarily by the liver via hydrolysis by esterases to unoprostone-free acid. The free acid is then metabolized into various metabolites excreted in the urine. 

Elimination and Excretion 

unoprostone and its metabolites are excreted primarily in the urine, with a small amount excreted in the feces. 

Adminstartion

Administration: 

• Use in combination with other topical ophthalmic medications to reduce intraocular pressure; if two medications are used, space administration by at least five minutes. 
• Includes benzalkonium chloride, which is potentially absorbable by soft contact lenses; Before administering, take out your contact lenses, and wait at least 15 minutes before putting them back in. 
• To reduce contamination of the dropper bottle tip and solution, avoid contacting eyes or nearby regions with the dropper bottle tip. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: unoprostone ophthalmic 

Why do we use unoprostone ophthalmic? 

• unoprostone ophthalmic solution is primarily used to treat open-angle glaucoma or ocular hypertension, which can cause an increase in intraocular pressure in the eye. By increasing the outflow of aqueous humor from the eye, unoprostone can help to reduce intraocular pressure and prevent or slow the progression of these conditions. 
• In addition to its use for glaucoma and ocular hypertension, unoprostone ophthalmic solution has also been investigated for its potential use in other ocular conditions. One is cystoid macular edema, which can occur after cataract surgery. 
• unoprostone may also have cosmetic benefits, as it has been shown to stimulate the growth of eyelashes and eyebrows and increase the melanin content of these hairs, leading to darker and thicker lashes and brows.