PHARMY Flashcards
Antiglaucoma drugs:
- B-blockers: First line for POAG > and all others
inhibit B-adrenergic receptors in ciliary body > decreased aqueous production
Ocular iritation, corneal desens, DED, macular edema
Bronchospasm, cough, arrythmia, headache, nausea
Contra. chronic obstructive PD, asthma, Bradycardia- Non-selective (B-1/2)
- Timolol/Levobunolol
0.25% BID, IOP decreases 25%
- Timolol/Levobunolol
- Selective (B-1)
- Betaxolol
- Less side effect; less efficacy
- Betaxolol
- Non-selective (B-1/2)
- Prost-analogues: All but uveitis glauc: Greater IOP reduction, causes inflammtion
Prodrug metabolized by corneal esterase > binds PGF2a receptor on ciliary muscle > ECM remodeling/MMP regulation > increase uveoscleral outflow
Iris heterochromia, lid pigmentation, lash lengthening, redness, SPEE
Contra. Ocular inflammation (HSK), CMO, allergy
1. Latanoprost (Xalantan)
0.005% daily, IOP decreased 30%- Bimatoprost (Lumigan): 0.03%
- Travoprost (Travatan): 0.004%
- Adrenergic-agonist:
Stimulate A-2 receptors > adenylate cyclase inhibition > decreased cMAP in ciliary cells > aqueous production loss
Stimulation of A-1 receptor > vasoconstriction of CB vessels > reduced aqueous production- Photophobia, blur, stinging
- Dry mouth, hypotension, fatigue
- Apraclonidine: selective A2 (weak A1)
0.5% BID, IOP decrease 20%
Causes tachyphylaxis
- Apraclonidine: selective A2 (weak A1)
- Carbonic anhydrase inhib: CA is critical for aqueous formation
Decreases bicarbonate ion formation > reduced fluid transport in ciliary epith.
Causes blood acidosis, renal stones, metalic taste, confusion
Contra. Heart/kidney disease
1. Acetazolamide (Diamox/Diazamide): IV for Rapid IOP decrease, oral otherwise
250mg BID, 20% decrease by 4h
500mg IV, 20% decrease by 30min- Dorzolamide (trusopt): topical, fewer systemic affects
2% 3/d, 20% IOP decrease
- Dorzolamide (trusopt): topical, fewer systemic affects
- Hyperosmotics: ^Plasma osmolarity > fluid uptake from ocular tissue
Nausea, heart faliure, confusion, kertoacidosis
Contra. DM- Glycerol: oral dose 4ml/kg
20 onset, poor ocular penetration - Mannitol: 20%
Not contra. for renal faliure
- Glycerol: oral dose 4ml/kg
- Cholinergic agonist: Stimulate muscarinic receptors in CB > Miosis > TM opening > increased outflow
Accomodative spasm, pupil block, cataract
Contra. cataract, myopia, young Px- Pilocarpine: 2% QID, 15% IOP decrease
Acyclovir and ganciclovir:
Antiviral prodrug, metabolized by viral enzymes to acyclovir/ganciclovir triphosphate
1. Competes with dGTP for incorporation into viral DNA
2. Chain terminator for DNA formation / Faulty DNA replication
Viral enzymes have higher affinity for acyclovir than host cells
- HSV: 3% ointment 5/d (up to 10d)
- HSV: 400mg 5/d (up to 10d)
- HZO: 800mg 5/d (up to 10d)
Ganciclovir has high affinity for cyclomegalovirus enzymes, but also affects host cells moreso than acyclovir
Prednisolone and Dexamethasone:
Cortico, lipophilic (^penetration)
1. Binds glucocorticoid receptors in cytoplasm
2. Pred.-GR complex moves to nucleus and regulates gene expression
1. Reduces cytokines (IL-1, TNF-a, INF-y)
2. Inhibits cyclooxygenase-2 expression > reduced mediator synthesis (prostaglandins)
3. Inhibits T/B cell proliferation
Dexamethasone (0.1%) has higher potency for faster response, but greater risk (^IOP more)
Same dosage and taper though, Pred 1% QID, or loading dose hourly 6h
Cyclosporin:
Immunosuppressive, used when cortico. non-response or risk
Lipophilic ^Penetration
1. Binds cytoplasmic protein cyclophilin
2. CC complex inhibits calcineurin, which normally
1. Protein phosphate for T-cell activation
2. processes transcription factors for IL-2
Commercially used for organ transplant
Side effects:
- HT, kidney damage
Antiglaucoma drugs:
- B-blockers: First line for POAG > and all others
inhibit B-adrenergic receptors in ciliary body > decreased aqueous production
Ocular iritation, corneal desens, DED, macular edema
Bronchospasm, cough, arrythmia, headache, nausea
Contra. chronic obstructive PD, asthma, Bradycardia- Non-selective (B-1/2)
- Timolol/Levobunolol
0.25% BID, IOP decreases 25%
- Timolol/Levobunolol
- Selective (B-1)
- Betaxolol
- Less side effect; less efficacy
- Betaxolol
- Non-selective (B-1/2)
- Prost-analogues: All but uveitis glauc: Greater IOP reduction, causes inflammtion
Prodrug metabolized by corneal esterase > binds PGF2a receptor on ciliary muscle > ECM remodeling/MMP regulation > increase uveoscleral outflow
Iris heterochromia, lid pigmentation, lash lengthening, redness, SPEE
Contra. Ocular inflammation (HSK), CMO, allergy
1. Latanoprost (Xalantan)
0.005% daily, IOP decreased 30%- Bimatoprost (Lumigan): 0.03%
- Travoprost (Travatan): 0.004%
- Adrenergic-agonist:
Stimulate A-2 receptors > adenylate cyclase inhibition > decreased cMAP in ciliary cells > aqueous production loss
Stimulation of A-1 receptor > vasoconstriction of CB vessels > reduced aqueous production- Photophobia, blur, stinging
- Dry mouth, hypotension, fatigue
- Apraclonidine: selective A2 (weak A1)
0.5% BID, IOP decrease 20%
Causes tachyphylaxis
- Apraclonidine: selective A2 (weak A1)
- Carbonic anhydrase inhib: CA is critical for aqueous formation
Decreases bicarbonate ion formation > reduced fluid transport in ciliary epith.
Causes blood acidosis, renal stones, metalic taste, confusion
Contra. Heart/kidney disease
1. Acetazolamide (Diamox/Diazamide): IV for Rapid IOP decrease, oral otherwise
250mg BID, 20% decrease by 4h
500mg IV, 20% decrease by 30min- Dorzolamide (trusopt): topical, fewer systemic affects
2% 3/d, 20% IOP decrease
- Dorzolamide (trusopt): topical, fewer systemic affects
- Hyperosmotics: ^Plasma osmolarity > fluid uptake from ocular tissue
Nausea, heart faliure, confusion, kertoacidosis
Contra. DM- Glycerol: oral dose 4ml/kg
20 onset, poor ocular penetration - Mannitol: 20%
Not contra. for renal faliure (no renal metabolism)
- Glycerol: oral dose 4ml/kg
- Cholinergic agonist: Stimulate muscarinic receptors in CB > Miosis > TM opening > increased outflow
Accomodative spasm, pupil block, cataract
Contra. cataract, myopia, young Px- Pilocarpine: 2% QID, 15% IOP decrease
Chemotherapeutic agents topical:
Indicated for OSSN as corneal extension or contacting more than half the limbus
Mitomycin C (0.02%): inhibits DNA/protein synthesis, cell migration, ECM production
- causes hyperemia, punctate erosions, DED
5-fluorouracil (1%): inhibits thymidylate synthetase, DNA/RNA syntesis
- causes conj. hyperemia, lid erythema
Interferon a2b 1million IU/ml: anti-microbial
- causes SPEE, follicular conjunctivitis
50S subunit drugs:
Antibacterial, binds 50s ribosomal subunit, inhibiting peptide formation
- Chloramphenicol
- Azithromycin
- Erythromycin .5%
Quinolones:
BS antibacterial
Inhibition of topoiosomerase-2 (DNA gyrase) and topoisomerase 4 > transcription/replication loss
- Ciprofloxacin .3%
- Ofloxacin .3%
- moxifloxacin
30S subunit drugs:
Aminoglycosides: bactericidal via faulty protein synthesis
- Gentamicin: Gram-ve species
- Tobramycin .3%
- Framycetin
Tetracyclines: Bacteriostatic via inhibited protein synthesis
- Tetracycline: alternate trachoma management
- Doxycycline
NSAIDs
COX enzyme inhibition > loss of prostaglandin synthesis
- Ketorolac .5 QID
- Diclofenac .1%