2.3: Ocular Pharmacology Flashcards
Name four routes of specifically for ocular drugs?
Topical
Subconjunctival
Subtenons
Intravitreal
Topical application lets the drug work in two places - where?
Act on the surface of the eye
Penetrate through the cornea to act on the deeper layers
Describe the composition of the cornea?
Lipid sandwich:
- Lipid epithelium
- Fluid layer (Stroma)
- Lipid tear film
Stroma makes up most of the cornea
Describe how drugs can pass through the cornea?
Low molecule weight drugs can pass through (small).
Large drugs must be either lipid or water soluble to pass through
Lipid soluble drugs are able to penetrate epithelium
Water soluble drugs are able to penetrate stroma
Some drugs are lipophilic and hydrophilic
Give an example of a drug that is lipophilic and hydrophilic that is used in eyes?
Chloramephenicol
Describe the affect of inflammation on the absorption of topical applications?
Occular surface inflammation can limit the hydrophobic nature of the endothelium
Describe the affect of the lipid layer (of the tear film) on drug penetration?
The lipid layer of the tear film may impede drug penetration
What limits hydrophobic drugs?
Stroma
What limits hydrophilic drugs?
Lipid Layer (Epithelium)
Are topical steroids hydrophobic or hydrophillic? Why?
They require both hydrophobic and hydrophilic ability
They are altered depending on what they are required for
Eg: Can penetrate the cornea or remain on surface
Describe a hydrophobic steroid?
Prednisolone Acetate
Describe a hydrophilic steroid?
Prednisolone Phosphate
How do you make a steroid hydrophilic?
Add phosphate
How do you make a steroid hydrophobic?
Add acetate or alcohol
Describe Prednisolone Acetate?
Hydrophobic Steroid
Used in un-inflamed eye
Is absorbed into the eye
If cornea is normal, a large amount of prednisolone acetate will get into the eye
Used post-operatively
Describe Prednisolone Phosphate?
Hydrophillic steroid
Used in inflamed eye
Poor penetration
Sits on the surface of the eye - very little drug penetrates into the actual eye
Used for corneal disease
Describe how to enhance corneal penetration?
Breaking up the lipid layer increases penetration
Benzalkonium is a preservative used in eye drops that helps to break the lipid layer and increase corneal penetration
Describe the job of Benzalkonium?
- Preservative in eye drops (prevents bacterial soup)
- Increases corneal penetration by punching holes
Describe Bimatoprost? What happened?
Drug used to lower Intra-ocular pressure in glaucoma
High dose of drug, low dose of preservative
Led to red eye
Swapped now to lower dose of drug but higher dose of preservative - allows for corneal penetration but no red eye
Describe systemic absorption of topical drugs?
Excess eye drops can result in systemic absorption at nasopharynx
- Tears pumped out of lacrimal sac rapidly
- Drops can be washed into nasopharynx
- Explains bad taste
How can the systemic absorption of topical drugs be limited?
Punctal occlusion
Pressing down on the puncta when administering topical drugs causes excess to wash down face as tears
Describe subconjunctival route of administration?
Injection directly into the space between conjunctiva and sclera
Steroids can be given topically - what is another (preferred) method of administration?
Subconjunctival Injection
Describe Subtenons route of administration?
Injection directly behind the eye into Tenon’s capsule/Sub tenon’s space