Test 1 Flashcards
(103 cards)
benzalkonium chloride (BAK)
preservative. surfactant. very stable. excellent antimicrobial. toxic effects on tear film and corneal epith. inc drug penetration. red TBUT in half. also a wetting agent.
thimerosal
preservative. organic mercury. inactivates respiratory enzymes. most effective in weakly acidic solutions. requires high continuous concentrations for biological effect. high rate of allergic and toxic rxns.
chlorohexidine
preservative. cationic diguanide. destroys semi-permeable layer of cytoplasmic membrane (bacteria). antimicrobial. not as effective as BAK or other preservatives.
chlorobutanol
preservative. detergent. cell lysis via disruption of microbial cell membrane lipid configuration. less effective antimicrobial than BAK. volatile-has odor. only effective in acidic pH. not effective alone, often combined w/ EDTA.
ethylenediaminetetraacetic acid (EDTA)
preservative. chelating agent that binds metal ions. effective by removing trace metal ions that organisms require (Ca2+, Mg). very slow acting-used in combo w/ other preservatives. contact dermatitis can occur
stabilized oxychloro-complex
oxidative preservative system. dissipates H2O, O2, Na and Cl free radicals. Cl free radicals inhibit microorganism protein synthesis-cell death (bacteriocidal?). neutralized by cells so no accummulation. effective antimicrobial but low toxicity. Purite (Refresh Tears and Alphgan-P (Allergan)).
sodium perborate
oxidative preservative system. catalyzed into H2O2, H2O, and O2. alters protein synthesis by oxidizing cell membranes and altering membrane-bound enzymes. neutralized by cells so no accumulation. effective antimicrobial but low toxicity. GenAqua (Genteal AT).
methyl/propyl/paraben
preservative. causes disorganization of microbial cells. used in AT, and non-medicated ointments. cause allergic rxns. unstable at high pH.
SofZia
preservative. most recent advancement. proprietary mixture of boric acid, propylene glycol, sorbitol, and zinc chloride. disrupts bacteria metabolic processes. rendered inactive when exposed to cations in tear film. less cytotoxicity to ocular surface than conventional preservatives. used in travaprost (Travatan Z).
polyvinyl alcohol (PVA)
viscocity agent. water-soluble viscosity enhancer. hydrophilic and hydrophobic sites. common conc: 1.4%. tx: corneal epithelial erosion, dry eye syndrome. inc drug residence time and ocular absorption. enhances oc contact time of drugs. wetting agent for CL. less viscous than MC. doesn’t disrupt cornea
hydroxypropyl methylcellulose (HPMC)
enhances viscosity. different MW and group substitutions. prolong tear film wetting time. inc fluorescein and dexamethasone penetration. 0.5% HPMC 2x ocular retention time of 1.4% PVA. less viscous than MC
carboxymethylcellulose/hydroxymethylcellulose (CMC)
enhances viscosity. carboxylic and hyroxylic groups provide anionic charge. promotes mucoadhesion. inc tear retention time. carboxym has greatest mucin adhesion than any other viscous agent. more bioadhesive than HPMC. more likely to create insoluble adhesives
polysorbate
viscosity and wetting agent. wetting agent: dec surface tension and inc spreading and penetration
methylcellulose (MC)
viscosity inc agent in AT. most freq used. forms viscous sol when added to water. stable compound at pH range tolerated by eye. unaffected by light or aging in sol. doesn’t support growth of microorganisms. conc 0.25-1%. conc >2% is viscous enough to be classified as an ung.
polyvinylpyrrolidone (povidone) (PVP(
viscosity agent. non-ionic surfactant. 3% and 5% sol. can form hydrophilic coatings in the form of absorbed layers; would mimic conj mucin
proplyene glycol
viscosity agent, tonicity agent
acetic, boric, and hydrochloric acids
buffers. adjusts pH of solution, varied solubility, weak acid or weak base
K and Na bicarbonate
buffer. adjusts pH of a solution, varied solubility, weak acid or base
K and Na borate
buffer. adjusts pH of a solution, varied solubility, weak acid or base
K and Na phosphate
buffer. adjusts pH of a solution, varied solubility, weak acid or base
K and Na citrate
buffer. adjusts pH of a solution, varied solubility, weak acid or base.
buffers, dextrans, dextrose, glycerin, propylene glycol, K and Na chloride
tonicity agents. effective osmolality. tonicity: sum of concentration of solutes that have the capacity to exert osmotic force across a membrane.
pilocarpine gel, vexol, betoptic S, azopt
polyacrylic acids. carbopol gels. inc viscosity with inc shear rate, blinking and ocular movement. good mucoadhesive and wetting properties.
betaxolol (Betoptic-S)
cation exchange resin (amberlite). dissolve and deliver hydrophilic and lipophilic compounds. red amount of free drug in solution. enhances ocular comfort.