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Eye Drops and Medications PDF

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Summary

This document provides a comprehensive overview of various eye drops and medications, categorized by their function (e.g., tear supplementation, anti-inflammatory agents, anti-bacterial agents). It covers details for each category, including specific drugs, mechanisms of action, and potential side effects. The formatting suggests that it may be part of a larger reference or textbook on ophthalmology.

Full Transcript

1. Dry Eye a. Tear supplementation b. Tear stimulation i. Pilocarpine Oral – Salagen c. Anti-inflammatory i. Steroids ii. Cyclosporine 1. Restasis 2. Cequa 3. Verkazia 4. Vevye iii. Lifitegrast 1. Xiidra d. Demodex i. Xdemvy ii. Tea Tree oil e. Neurotrophic keratitis i. Oxervate 2. Anti-Bacterials a...

1. Dry Eye a. Tear supplementation b. Tear stimulation i. Pilocarpine Oral – Salagen c. Anti-inflammatory i. Steroids ii. Cyclosporine 1. Restasis 2. Cequa 3. Verkazia 4. Vevye iii. Lifitegrast 1. Xiidra d. Demodex i. Xdemvy ii. Tea Tree oil e. Neurotrophic keratitis i. Oxervate 2. Anti-Bacterials a. Cell wall synthesis i. Penicillin 1. Dicloxacillin – not inactivated by penicillinase 2. Amoxicillin and clavulanate – not inactivated by penicillinase ii. Cephalosporin – contraindicated in vitamin K deficiency 1. Cephalexin – oral, gen 1, more gram + 2. Cefazolin – injection, gen 1 iii. Vancomycin – toxic, anaphylaxis, ototoxicity, neutropenia, used for MRSA iv. Bacitracin – ointment b. Cell membrane i. Polymyxin B – good with pseudomonas ii. Gramicidin c. Protein synthesis i. 30 S 1. Aminoglycosides a. Neomycin – ineffective pseudomonas b. Gentamicin – effective pseudomonas, ineffective streptococcus c. Tobramycin – effective pseudomonas and more sensitive d. Amikacin – effective pseudomonas 2. Tetracyclines – for chlamydia, acne rosacea, non phlyctenular KC, corneal ulcers, anti-collagenolytic, depress bone growth, blood dyscrasias, tooth issues, photosensitivity a. Tetracycline – take on empty stomach b. Doxycycline – Oracea for rosacea, take w food c. Minocycline ii. 50 S 1. Macrolides a. Erythromycin – for ocular prophylaxis in neonates b. Azithromycin – 1000 mg for chlamydia, improves MGD better than Doxycycline 2. Chloramphenicol – anthrax, oral not in US, aplastic anemia 3. Clindamycin d. Folic acid i. Sulfonamides – chlamydia, toxoplasma, inactivated by PABA, inhibits folic acid synthesis 1. Sulfamethoxazole – oral for toxoplasmosis 2. Sulfadiazine – oral for toxoplasmosis 3. Sulfacetamide – for blepharitis, contraindicated in PABA containing compounds like ester type local anesthetics, and purulent exudates ii. Trimethoprim/Polymyxin B – MRSA, for infants iii. Pyrimethamine – for toxoplasmosis, bone marrow depression, administer with Leucovorin folinic acid e. DNA synthesis i. Fluoroquinolones – inhibits DNA gyrase and topoisomerase IV, may cause tendon rupture, prolonged QT 1. 2nd gen – for corneal ulcers a. Ofloxacin b. Ciprofloxacin – may cause corneal precipitates 2. 3rd gen – more G +, same G - than gen 2 a. Levofloxacin – for bacterial conjunctivitis not keratitis 3. 4th gen – better against single step mutations a. Moxifloxacin – preservative free b. Gatifloxacin – for bacterial conjunctivitis c. Besifloxacin – only ophthalmic, shake, for corneal ulcers 3. Anti-Virals a. Nucleosides i. Acyclovir ii. Valacyclovir iii. Famciclovir b. Antiretroviral i. Zidovudine ii. Ganciclovir iii. Foscarnet c. Topicals i. Idoxuridine ii. Vidabine 4. 5. 6. 7. iii. Trifluridine iv. Ganciclovir gel v. Acyclvir d. Povidone Iodine Antifungals a. Topicals i. Polyenes 1. Natamycin b. Systemic i. Polyenes 1. Amphotericin B 2. Nystatin ii. Pyrimidines iii. Imidazoles iv. Trizoles 1. Voriconazole Steroids a. Prednisolone – cortisol, increase IOP, not for DED b. Dexamethasone – cortisol, increase IOP c. Fluorometholone – progesterone, good for DED, lower increase in IOP d. Medrysone – progesterone e. Loteprednol – prednisolone, amplify delivery, ester, gel form f. Rimexolone g. Difluprednate – prednisolone, half dose equal to Predforte, sorbic acid preservative h. Triamcinolone – Xipere, injection NSAIDs a. Aryl acetic i. Ketorlorac – allergic conjunctivitis ii. Dicofenac – decreased corneal sensation iii. Bromfenac – prolensa – low pH increased penetration, bromsite – durasite, COX2 enhanced inhibition, similar to amfenac iv. Nepafenac – prodrug, non charged increases penetration b. Arylproprionic acid i. Flurbiprogen ii. Suprofen Analgesics a. Aspirin – irreversible, ceiling effect b. Ibuprofen – superior to aspirin, less side effects, 400 mg equal to tylenol 3 c. Naproxen d. Acetaminophen – no anti inflammation, blood thinner, GI irritation, max 4g/day e. Opioids – all bind to mu i. Morphine – binds to kappa, pinpoint pupils ii. Heroin – pinpoint pupils iii. iv. v. Hydrocodone Codeine – no ceiling effect, prodrug, CYP Tramadol – CYP, M1 high affinity to mu, do not take with erythromycin, SSRIs, or MAOIs f. Naloxone – effective in 30-90 minutes, reverses opioid effects g. Opvee – nasal spray, reverses opioid effects 8. Local Anesthetics a. Topicals (all esters except lidocaine) i. Cocaine – not synthetic, no aromatic/hydrophobic domain ii. Proparacaine – MABA, less penetration iii. Tetracaine – more epithelial damage, more painful iv. Benoxinate – less side effects v. Lidocaine – Amide, ophthalmic gel b. Injectables i. Procaine – ester, PABA ii. Lidocaine – Amide iii. Mepivacaine – amide iv. Bupivacaine – amide, increased potency and duration, made from Mepivacaine v. Etidocaine – amide vi. Tetracaine – ester, PABA, increased lipid solubility/protein binding, and potency and duration, made from procaine 9. Immunosuppressants a. Cytotoxic – antineoplastic, prevent cell growth, suppress hyperactive immune response i. Methotrexate – Folate antagonist, Tx of JIA, Leucovorin (Folinic acid) used to counter toxic effects, Black box warning, cotton wool spots, pregnancy category X b. Immunomodulators i. Cyclosporine A ii. Tacrolimus – Calcineurin inhibitor, 100x more potent than cyclosporine, topically for atopic dermatitis and off label for VKC, black box warning, skin malignancies and lymphoma, effective in AKC iii. Adalimumab (Humira) – TNF blocker, in synovial fluid, for non-infectious uveitis 10. Dyes a. Fluorescein – Xanthene, intracellular spaces, healthy/dead/damaged cells, quenching, discolors skin and urine, inactivates BAK b. Rose Bengal – Xanthene, not vital, white light, mucous strands, healthy/dead/damaged cells, toxic to cells c. Lissamine Green – Triarylmethane, white light, mucous strands, dead/damaged cells d. Methylene Blue – Thiazine, lacrimal sac e. Tryptan Blue – Azo, endothelial cell viability f. Indocyanine Green – Cyanine, choroid abnormalities 11. Anti-Allergy a. Allergic reaction – exaggerated response to antigen AND tissue damage i. Exception is seasonal allergic conjunctivitis – no tissue damage due to no clinically relevant late phase b. H1 – itching and pain, H2 – gastric acid secretion (non-mast cell) c. a1 both arteries and veins, tachyphylaxis d. a2 mainly veins, no tachyphylaxis or rebound hyperemia e. Ocular decongestants i. Phenylephrine – rebound hyperemia and dilation ii. Imidazole derivatives – less rebound hyperemia and dilation 1. Naphazoline – pupil dilate, increase IOP 2. Oxymetazoline – no pupil/IOP increase, caution with MAOIs, angle closure 3. Tetrahydrozoline – no pupil/IOP increase iii. Brimonidine – a2 selective, high dose → hyperemia, low dose → blanching, decrease tachyphylaxis and rebound 1. Lumify f. Antihistamines i. Used in allergic conjunctivitis Type I, Lid myokymia, and motion sickness PO ii. Contraindicated in NAG iii. May cause mydriasis, rebound hyperemia, and follicular conjunctivitis iv. 1st gen – lipophilic, ADRs, cross BBB v. 2nd gen – hydrophilic, less ADRs, does not cross BBB, longer elimination time with lower doses vi. Orals 1. Chlorpheniramine maleate – 1st gen 2. Diphenhydramine – Benadryl – 1st gen, strong anticholinergic 3. Loratadine – Claritin – 2nd gen, c amiodarone → torsades de pointes 4. Cetirizine – Zyrtec – drowsiness, most potent 2nd gen 5. Fexofenadine – Allegra – absorption decreases with grapefruit juice and increases with erythromycin or ketoconazole 6. Desloratadine – Clarinex – metabolite of loratadine, longer half life 7. Levocetirizine – Xyzal – enantiomer of cetirizine, greater half life 8. Food delays absorption of cetirizine and loratadine g. Mast cell stabilizers i. MOA – prevents calcium influx, inhibits degranulation and mediator release (prevents arachidonic acid pathway) ii. HA common ADRs iii. Cromolyn sodium 4% – Crolom – frequent dosing (4-6hrs), long onset (2 weeks) iv. v. Pemirolast – Alamast Nedocromil – Alocril – more potent than Crolom, less frequent dosing (BID), faster onset (2-15 mins), unpleasant taste vi. Lodoxamide – Alomide – 2,500x more potent than Crolom, used for VKC due to effect on CD4+ cells h. Multi Action drugs – antihistamines (H1) + mast cell stabilizers i. Burning, stinging, HA ii. Azelastine – bitter taste iii. Epinastine – H2 and inhibits eosinophil chemotaxis iv. Olopatadine – better than Ketotifen at preventing itch > tearing v. Ketotifen – inhibit eosinophil chemotaxis and activation 1. Ketotifen 19 mcg – daily disposable CL vi. Bepotastine – Bepreve vii. Alcaftadine – Lastacaft 12. Retinal and Neovascular Drug Treatment a. anti-VEGF i. May increase IOP briefly, for glaucoma may include IOP lowering prophylactic meds b. Photodynamic therapy i. Verteporfin (Visudyne) – dye that selectively damages fibrovascular tissue ii. Pt should avoid sunlight for 2 days c. Antiangiogenesis i. Pegaptanib (Macugen) – D/C, slows vision loss but does not improve VA ii. Monoclonal Antibodies 1. Ranibizumab (Lucentis) – Fab fragment, blocks all VEGF isoforms, improves VA by 3 lines, expensive a. Susvimo – ocular implant can be refilled, as good as injections 2. Ranibizumab-nuna (Byooviz) 3. Bevacizumab (Avastin) – full sized antibody, cheaper, same efficacy iii. VEGF trap 1. Eylea – Aflibercept – 2 or 8 mg (less doses), PIGF and VEGF, better than Beva and Rani iv. Single chain variable fragment 1. Brolucizumab (Beovu) – DME needs reinjection longer than nARMD, better than aflibercept at nARMD anatomic tx v. Bispecific antibody 1. Faricimab-svoa (Vabysmo) – targets VEFG-A and angiopoietin-2, PTI, every 4 mo non inferior to aflibercept every 2 mo, better at reducing central thickness than aflibercept d. Corticosteroids i. Triamcinolone (Xipere) – combine with PDT, off label ii. Dexamethasone (Ozurdex) – biodegradable intravitreal implant, 1-3 mo iii. Iluvien – Non-erodible intravitreal implant, Fluocinolone e. Geographic atrophy drugs i. Pegcetacoplan (Syfovre) – complement inhibitor (complement contributes to AMD), binds to C3 and C3b, ii. Avacincaptad pegol (Izervay) – Darpin, complement inhibitor, C5, f. Vitreomacular Adhesion drugs i. Ocriplasmin (Jetrea) – D/C 13. Nutraceuticals a. AREDS – vitamin C, E, beta carotene, and zinc i. Do not affect cataracts ii. Reduce AMD development in high risk categories iii. Combination better than alone – 25% reduction b. AREDS 2 – Lutein, zeaxanthin, DHA, and EPA i. Did not further reduce AMD progression ii. Low zinc same as high zinc iii. Lutein and zeaxanthin may be good substitute for beta carotene in smokers – less chance of lung cancer c. Genetic testing not recommended d. Mediterranean diet reduces AMD 41% e. Vitamin E hastens progression of Retinitis Pigmentosa while omega 3 (DHA) slows it 14. Autonomics a. Edrophonium i. Tensilon Test for Myasthenia Gravis b. Botox i. Tx of blepharospasm and strabismus ii. Increase risk of ptosis iii. MOA 1. Blocks transmission, inhibiting ACh release 2. Targets SNARE proteins presynaptic and on vesicles c. Testing anisocoria i. Anticholinergic mydriasis 1. Pilocarpine 0.5% or 1% will not constrict if caused by atropine but will constrict if caused by pupil paralysis (third nerve palsy) ii. Third nerve palsy with pupil involvement 1. Aneurysm until proven otherwise 2. Pilocarpine 0.5% or 1% will constrict pupil iii. Adie’s 1. Signs – sluggish/tonic pupil during accommodation, and diminished deep tendon reflexes 2. Pilocarpine 0.1% and 0.125% will constrict Adie’s a. Normal pupil will only constrict with 0.125% b. Third nerve palsy will also not constrict iv. v. Horner’s 1. Cocaine 10% will not dilate Horner’s pupil 2. Apraclonidine 1% will dilate Horner’s pupil Pre ganglionic 1. Hydroxyamphetamine (Paredrine) will dilate pre ganglionic lesion 2. Phenylephrine 1% will not dilate preganglionic lesion 15. Glaucoma a. Beta blockers – do not work at night, decrease aq production i. Timolol maleate – 30% decrease, XE gel forming ii. Timolol Hemihydrate – less effect on HR iii. Levobunolol – QD iv. Betaxolol – BID, low effect on IOP, great effect on VF, B1 selective v. Carteolol – lipid levels negligible, ISA activity b. Cholinergic agonists – increase aq outflow via TM i. Pilocarpine – QID, HA, pupil block, lid myokymia, direct acting, will not work if IOP > 60 mmHg, RD, permanent miosis, 4% only on dark irises, not for narrow angles 1. Vuity – 1.25%, BID, Tx presbyopia 2. QLOSI – 0.4%, Preservative free, Tx presbypia ii. Echothiophate – iris cysts, indirect irreversible, for AccET c. Adrenergic agonists – decrease aq production and increase uveoscleral outflow i. Apraclonidine 1. Iopidine – some alpha 1, tachyphylaxis, dry mouth ii. Brimonidine – alpha 2 1. Alphagan P – Purite not BAK 2. Lumify – relieves redness at low dose, no tachyphylaxis d. Carbonic Anhydrase Inhibitors i. Alter intracellular pH and ATPase activity to decrease aq production ii. Sulfonamide derivatives iii. Oral 1. Acetazolamide – tx pseudotumor cerebri, increase ventilation for altitudinal sickness, 95% protein bound, many ADRs 2. Methazolamide – better tolerated than acetazolamide, 55% protein bound iv. Topical 1. Dorzolamide a. Trusopt – inhibits CA II and XII, works during sleep, BID additive to timolol, TID monotherapy, do not use with oral CAIs → could lead to corneal edema 2. Brinzolamide a. Azopt – suspension, less sting than dorzolamide v. Combinations 1. Cosopt a. Dorzolamide and Timolol 2. Simbrinza a. Brinzolamide and Brimonidine e. Prostaglandins i. Latanoprost 1. Xalatan 2. Iyuzeh 3. Xelpros ii. Latanoprostene bunod 1. Vyzulta iii. Travoprost 1. Travatan Z 2. iDose TR iv. Tafluprost v. Bimatoprost 1. Lumigan 2. Latisse 3. Durysta vi. Unoprostone vii. Omidenepag 1. Omlonti f. Rock Inhibitor i. Netarsudil 1. Rhopressa a. ROCK and NET inhibitor b. Lowers episcleral venous pressure

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