Ocular drugs Flashcards
How can a drug be delivered to ocular tissue?
Locally (eye drops, ointments, periocular injections, intraocular injections) and systemically (orally, IV).
What is the most commonly used route for ocular drug administration?
The topical route.
What factors influence the absorption of topically instilled drugs?
Elimination by nasolacrimal drainage, time in the conjunctival cul-de-sac & precorneal tear film, drug binding to tear proteins, drug metabolism by tear & tissue proteins, and rate of diffusion across the cornea & conjunctiva.
Describe the distribution process of ocular drugs.
Transcorneal absorption, accumulation in aqueous humor, distribution to intraocular structures, trabecular meshwork pathway, and distribution to systemic circulation.
What is significant in the metabolism of ocular drugs?
Enzymatic biotransformation, particularly by esterases, with examples including prodrugs like dipivefrin hydrochloride and latanoprost.
What are some methods of topical ocular drug delivery?
Drops, ointments, and gels.
What are periocular injections and their examples?
Injections that reach behind the iris-lens diaphragm better than topical application, such as subconjunctival, subtenon, peribulbar, and retrobulbar
What is the purpose of intraocular injections and examples?
For anterior segment surgery or infections, such as intracameral acetylcholine during cataract surgery and intravitreal antibiotics for endophthalmitis.
What are sustained-release devices in ocular drug delivery?
Devices that deliver medication at a steady-state level, such as Ocusert delivering pilocarpine and Timoptic XE delivering timolol.
What factors influence systemic drug penetration into ocular tissue?
Lipid solubility, protein binding, and ocular inflammation.
What are the advantages and limitations of topical ocular drug administration?
Convenient, economical, relatively safe. Limitations: Compliance, corneal & conjunctival toxicity, nasal mucosal toxicity, systemic side effects from nasolacrimal absorption.
What is the special utility of sub-conjunctival, sub-Tenon’s, and retrobulbar injections?
Useful for anterior segment infections, posterior uveitis, and cystoid macular edema (CME).
What are the potential complications of sub-conjunctival, sub-Tenon’s, and retrobulbar injections?
Local toxicity, globe perforation, optic nerve trauma, central retinal artery or vein occlusion.
What are intraocular injections and when are they used?
Injections directly into the eye, used for anterior segment surgery or infections. Examples include intracameral acetylcholine during cataract surgery and intravitreal antibiotics for endophthalmitis.
What is the use of intravitreal injections?
To provide an immediate local effect for conditions like macular edema or diabetic retinopathy (DR).
What are the advantages of periocular injections?
They bypass the conjunctival and corneal epithelium, useful for drugs with low lipid solubility, such as penicillins and steroids.
How does drug concentration and solubility affect local drug penetration into ocular tissue?
Higher concentration results in better penetration. Example: Pilocarpine 1-4%, but limited by reflex tearing.
What is the role of viscosity in drug penetration into ocular tissue?
Addition of methylcellulose and polyvinyl alcohol increases drug penetration by increasing contact time with the cornea and altering the corneal epithelium.