Drug Types

Question 1

ANTI-HISTAMINES

Answer 1

(Bepotastine, Emedastine, Levocabastine)

(Topical, Levocabastine- Nasal) - Inhibit mediator action - Block H1 receptors on smooth muscles (BVs, bronchi, GI) (preventing H1&raquo_space; (inc) IP3, DAG&raquo_space; (inc) Ca&raquo_space; VC), Also preventing VD (precapillary/capillary)

Tx - Symptoms of seasonal allergies, allergic rxn (itch/edema), local anaesthetic

SE - Stinging, Mydriasis (NOT for narrow angles), Allergies (w/ chronic use), Category C (NOT for pregnant women), NOT for patients w/ GI, urinary tract disease, NOT for antifungal/macrolide users (Cytochrome P450 drug interactions - Effect on cardiac K+ rectifying current&raquo_space; Drug toxicit

Question 2

ANTI-HISTAMINES + ADJUNCT MAST CELL STABILIZERS

Answer 2

(Alcaftadine, Ketotifen)

Question 3

ANTI-HISTAMINES + ADJUNCT MAST CELL STABILIZERS + INHIBIT OTHER MEDIATORS RELEASED

Answer 3

(Olopatadine - Maybe does NOT cause mydriasis, Azelastine, Epinastine)

Question 4

1ST GEN ANTI-HISTAMINES

Answer 4

(Diphenhydramine, Promethazine, Chlorpheniramine - Weakly sedating)

(Oral)
Anti-M, Lipophilic&raquo_space; CNS effects

Tx Anti-nausea, Alt to Botox (lid myokymia)

SE - CNS depression, Strongly sedating (but excitation in young children) - (NOT for alcohol, CNS depressant users), Dry mouth, Dysrhythmia, May cause convulsions

Question 5

2ND GEN ANTI-HISTAMINES

Answer 5

(Loratadine, Desloratadine, Fexofenadine, Cetirizine)

(Oral)

More H1-selective, Longer acting

SE - HA

Question 6

MAST CELL STABILIZERS

Answer 6

(Cromolyn, Lodoxamide)

Inhibit mediator release (from mast cells) - (Lag time in action)

(Topical) - Poor absorption

Tx - (Alt to corticosteroid for chronic care) for vernal/atopic keratoconjunctivitis, For gen seasonal allergies/asthma, GPS, Prophylaxis

Few syst SE

Question 7

MAST CELL STABILIZERS + INHIBIT OTHER MEDIATORS

Answer 7

(Neodocromil, Pemirolast)

Question 8

ANTI-IGE ANTIBODY

Answer 8

(Omalizumab)

Prevents IgEs from binding and activating mast cells

Question 9

DECONGESTANTS

Answer 9

(Phenylephrine)

Alpha1-agonists (inc) IP3, DAG&raquo_space; (inc) CA&raquo_space; VC

Tx - FASTEST relief for (symptoms) of allergic conjunctivitis, conj hyperemia, mild allergies

SE - Rebound congestion

Question 10

IMIDAZOLES

Answer 10

(-AZOLINE)
(Visine)
(Naphazoline, Oxymetazoline, Tetrahydrozoline)

DECONGESTANTS

(Potent) More alpha1-selective

SE - Less rebound congestion

Question 11

Tx options for wet AMD

Answer 11

Anti-VEGF vitreal injections (every 4-6 weeks)

(Pegaptanib, Bevacizumab, Ranibizumab, Aflibercept), Photodynamic therapy (Verteporfin), Laser surgery

Question 12

ANTI-VEGF

Answer 12

(Pegaptanib, Bevacizumab, Ranibizumab, Aflibercept)

Binds to VEGF-A (NOT receptor)

Vitreal injection (every 4-6 weeks)

Against neovascularization in PDR, wet AMD

SE - Endophthalmitis, Ret detachment, Traumatic cataract / (inc) IOP

Question 13

PHOTODYNAMIC THERAPY

Answer 13

(Verteporfin)

Dye - Binds to plasma lipoproteins - Activated by bright lights - Generate oxygen radicals - Collapse small, immature BVs

SE - HA, Visual impairment

Question 14

NSAID

Answer 14

COX inhibitior, Fibroblast (scarring) inhibitor

Tx - Against inflammation (esp during/after cataract/corneal ref surgery), Mild/Mod pain (Analgesic, for specific inflammatory-induced pain NOT anaesthetic, which has non-specific blocking of action potentials&raquo_space; numbing effect), Antipyretic

SE - NO rebound inflammation, Allergies, GI distress, Affect renal clearance of other drugs, (Inc) duration of bleeding, (NOT) for pregnant women (COX expressed in fetal development)

Question 15

More COX-1 selective NSAID

Answer 15

(Flurbiprofen, Suprofen, Ketorolac, Aspirin)

Question 16

More COX-2 selective NSAID

Answer 16

(Bromfenac, Nepafenac, Diclofenac, Rofecoxib, Meloxicam)

Question 17

CORTICOSTEROIDS

Answer 17

Inhibit Phospholipase A2 (work at top of overall signalling cascade&raquo_space; Eicosanoids) but NOT analgesics (NOT specific enough)

(Cont made endogenously) Inhibit gene expression related to immune responses

Tx - Anti-inflammatory, NOT analgesic

SE - Rebound inflammation, NOT for pregnant women, ENHANCE fungal growth

Question 18

OPIOIDS

Answer 18

Opioid receptor (u, k, delta) agonists/ antagonists

Oral / Injection, (Inc) tol for analgesics/euphoria effects&raquo_space; Have to (inc) dose, but NO tol for resp/GI/pupil/ effects

Tx - Mild/mod/severe pain (Analgesia), but NOT for non-nociceptive nerve pain (damaged&raquo_space; chronic firing) / CNS effects (Euphoria,calming / Anesthesia), Cough suppressant (Antitussive), Diarrhea (Flush system)

SE - Euphoria (Addiction), (Dec) respiration, Sedation, (Dec) GI, Miosis, Nausea (Vomiting), Constipation

Question 19

Types of ANTIBACTERIALS

Answer 19

Folate synthesis inhibitors, Cell wall synthesis inhibitors (inc Beta-lactams), Protein synthesis inhibitors (inc Aminoglycosides, Macrolides), DNA gyrase/Topoisomerase IV inhibitors, Cell membrane inhibitors

Question 20

BETA-LACTAMS

Answer 20

CELL WALL SYNTHESIS INHIBITORS

(BacteriCIDAL) Prevent building blocks from attaching to existing cell wall lattice

(T > MIC) - Time-dep - Difficult to maintain therapeutic levels (for vitreal infection) - b/c Removed quickly by transporters on ret BVs

Tx - (Gram +) First-line antibiotic for most systemic infections

Question 21

AMINOGLYCOSIDES

Answer 21

PROTEIN SYNTHESIS INHIBITORS

BacteriCIDAL (on 30 S) Abnormal codon:anticodon&raquo_space; Misreading of message

(Cmax/MIC) - Conc-dep - Topical, Synergystic effect w/ Beta-lactams, Vancomycin

Tx - Gram (-)

SE - Corneal toxicity, Neurotoxicity, Oxotoxicity, Nephrotoxicity, Photosensitivity (of skin)&raquo_space; Hives

Question 22

MACROLIDES

Answer 22

PROTEIN SYNTHESIS INHIBITORS

(BacteriCIDAL) - (on 50 S) Inhibits translocation (tRNA from A-site&raquo_space; P-site)

Tx - Mostly narrow - Gram (+) / Blepharitis, Chlamydia

SE - GI toxicity

Question 23

ENTRY/FUSION INHIBITORS

Answer 23

Inhibit host cell receptors OR virus surface receptors&raquo_space; Prevent viral entry/fusion

Question 24

NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS

Answer 24

Denatures reverse transcriptase enzyme (RNA&raquo_space; DNA)

Tx - Against RNA viruses

SE - Better tolerated

Question 25

NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS

Answer 25

Compete w/ host cell triphosphates (RNA&raquo_space; DNA)

Tx - Against RNA viruses

SE - Sig syst SE (Myelotoxicity, lactic acidosis, polyneuropathy, pancreatitis, mitochondrial DNA damage&raquo_space; cell death)

Question 26

DNA POLYMERASE INHIBITORS

Answer 26

Nucleoside analogues (structurally similar to guanosine)

Most commonly used

Question 27

PROTEASE INHIBITORS

Answer 27

Inhibit viral protease function (cleaving newly synthesized viral proteins to assemble new virions)&raquo_space; Blocks viral replication

SE - Promote lipid redistrib&raquo_space; (dec) in face, (inc) in abdomen&raquo_space; Syst SE - Hyperlipidaemia, Type 2 diabetes, Lipodystrophy

Question 28

MACROLIDE POLYENE

Answer 28

Binds to ergosterol (in fungal membrane)&raquo_space; Change membrane permeability&raquo_space; Ion leakage

Tx - Fungal keratitis

SE - Bind sterols in host membrane

Question 29

BETA-BLOCKERS for glaucoma

Answer 29

(-OLOL)
(Betaxolol, Metipranolol, Timolol, Levobunolol, Carteolol)

ONLY during the day (NO 24h control) when symp activity is present to block - Blood&raquo_space; Ultrafiltrate&raquo_space; Ciliary body (stroma)&raquo_space; Block beta2 receptors on NPE&raquo_space; (dec) cAMP&raquo_space; (dec) Cl&raquo_space; (dec) H2O

(2nd most commonly Rx), (3x day) - In generic / non-preserved (cheaper), (> Throat&raquo_space; Lungs&raquo_space; Respiratory distress (constriction) (beta2) / CHF / Depression, NOT for patients taking anti-HTN med

Question 30

ALPHA-2 AGONISTS for glaucoma

Answer 30

(-ONIDINE)
(Aproclonidine, Brimonidine)

(24h control) - Act on alpha-2 receptors (on presynaptic symp nerve fiber) - (dec) cAMP&raquo_space; (dec) Cl&raquo_space; (dec) H2O / Prevent normal NE from acting - (dec) NE release

(3rd most commonly Rx), (3x day)

Tx - (dec) aq produ, (late inc) uveoscleral outflow

SE - NOT for patients taking anti-HTN med

Question 31

Carbonic anhydrase inhibitors (CAIs) for glaucoma

Answer 31

(-AMIDE)
All sulfa drugs
(Dorzolamide, Brinzolamide, Acetazolamide, Methazolamide)

(24h control) - (dec) HCO3- bicarbonate&raquo_space; (dec) H2O

(3-4x day)

Tx - (dec) aq produ

SE - (Topical) - Sting, Bitter, RARE systemic SE / (Oral) - Serious systemic SE (so high intolerance)

Question 32

MIOTICS for glaucoma

Answer 32

(Pilocarpine, Carbachol, Echothiophate, Dipivefrin)

Anticholinesterase / Muscarinic (M3) agonists - (On iris sphincter) - (dec) pupil size - Pull iris - Open angle - Schlemm’s Canal / (On ciliary body) - (contract) cil muscles - Open TM / (dec) spaces within cil body

(3-4x) / (1-2x) day dosing

Tx - (inc) conventional aq outflow / (dec) uveoscleral outflow

SE - (Oc) - Ciliary spasm, post synechiae, hyperemia (b/c Ach - (inc) NO&raquo_space; VD) but does NOT change BP / (Syst) - Brachycardia, GI, (inc) gland produ, bronchospasm, HA / NOT for asthma/Parkinson’s disease patients (b/c Ach - (dec) dopamine)

Question 33

Prostaglandin/Prostamide/Prostone analogues (PGAs) for glaucoma

Answer 33

(-PROST)(ONE)
(Latanoprost, Travoprost, Tafluprost, Bimatoprost, Unoprostone)

(24h control) PGF2-alpha receptors - (inc) MMPs/ECM remodeling / Prostamide receptors on TM

(Most common Rx), (>) duration (1 or 2 x day dosing)

Tx - (inc) Uveoscleral outflow, (dec) Outflow resistance

SE - (> Oc SE) - (Irrev) iris color change (green/hazel&raquo_space; brown), darker periorbital dermis, thicken/inc lash length (hypertrichosis), conj hyperemia, irritation/SPK, (Rare) - Choroidal detach, (Re)Activation ofCME/Uveitis, (NO Syst SE (b/c short syst half life), otherwise rare/mild,e g. nasal congestion, flu-like symptoms, nausea/vomitiing, little effect on BP)

Question 34

Hyperosmotic agents for glaucoma

Answer 34

(Glycerol, Isosorbide, Mannitol)

(dec) Inflow, (inc) Outflow

Tx - ACG (can also use alcohol), Pre-surgery (dec IOP)

SE - (Syst SE) - Nausea (vomiting), Dehydration, HA, Confusion, Lethargy / (For IV) - Arm, chest pain, Chills, Rapid diuresis (urea)

Question 35

Glaucoma drugs - Least&raquo_space; Most potent

Answer 35

(Least) Epi, Topical CAI/Betaxolol, Alpha2 agonists / Beta-blockers / Miotics, PGAs / Oral CAIs (Most potent)