Products
Prostaglandin analogues are commercially available in the form of eye drops in vials or as monodoses without preservatives. Latanoprost (Xalatan) was the first agent from this group to be approved in 1996. Prostaglandin analogues are also combined with the beta-blocker timolol fix.
Structure and properties
Prostaglandin analogs are derivatives of prostaglandin F2α. Except for bimatoprost, an amide, they are ester prodrugs that are biotransformed in the cornea by esterases by cleavage of the isopropyl ester to the active acid. Esterification serves to increase permeability and bioavailability. Latanoprost example:
Effects
Prostaglandin analogs (ATC S01EE) lower intraocular pressure primarily by increasing uveoscleral outflow of aqueous humor. The effects are due to agonism at the prostaglandin F receptor (FP receptor). Prostaglandin F2α is the natural ligand at this receptor. Binding leads to increased expression of metalloproteases in the ciliary muscle, promoting degradative processes in the extracellular matrix (remodeling). As a result, aqueous humor passes more easily through the tissue.
Indications
For the reduction of intraocular pressure in open-angle glaucoma and elevated intraocular pressure (ocular hypertension). Because of its positive effect on eyelashes, a drug containing bimatoprost has been approved to promote eyelash growth in hypotrichosis (USA: Latisse).
Dosage
According to the SmPC. The drops are usually placed in the eyes once daily in the evening (1 drop). The application must not be more frequent. The intraocular pressure-lowering effect lasts at least 24 hours. See also under Administering eye drops.
Active Ingredients
- Bimatoprost (Lumigan, Ganfort).
- Latanoprost (Xalatan, generic).
- Latanoprostenbunod (Vyzulta)
- Tafluprost (Saflutan)
- Travoprost (Travatan, generic)
Contraindications
Prostaglandin analogues are contraindicated in the presence of hypersensitivity. Refer to the drug label for complete precautions.
Interactions
Concomitant use of two prostaglandin analogues may result in a paradoxical increase in intraocular pressure. Other eye drops should be instilled at a time interval.
Adverse effects
The most common possible adverse effects include:
- Local reactions to the eye, such as a burning, pain, scratching, itching, and stinging sensation
- Increased blood flow to the eye (red eye, ocular hyperemia).
- Hyperpigmentation of the iris: increase in brown pigment in the iris, permanent change in eye color, especially in mixed-color iris.
- Changes in eyelashes and vellus hairs on the eyelid: increase in length, thickness, pigmentation and number of eyelashes.
- Headache
