Opthalmic, Nasal And Otic Drug Products

Front 1

3 ways to deliver opthalmic drugs

Back 1

1) topically applied to eye
2) surface or intraocular conditions
3) Infections, allergies ,inflammation, elevated IOP, dry eye

Front 2

Can you use systemic effects opthalmically?

Back 2

No, local effects only

Front 3

3 ways to apply opthalmic drugs

Back 3

1) dropwise
2) thin ribbon on lower lid margin
3) insertion of device for continuous release of drug

Front 4

General info on the capacity of the eye 4 things

Back 4

1) blinking and flushing effect of lachrymal fluid
2) tear fluid in cul-de-sac = 7-8 mcL
3) non-blinking 30 mcL X blinking 10 mcL
4) Blinking: 80% of 50 mcL dose lose after 5 min of admin.

Front 5

Extended periods of therapy need increased contact time, occurs by what 5 processes?

Back 5

1) multiple-drop therapy with timer intervals
2) increased viscosity
3) suspensions, ointments, gels
4) inserts
5) oral or parenteral therapy if serious condition

Front 6

Main pharmaceutical requirement for all opthalmics

Back 6

Sterility and Preservation

Front 7

4 main ways to gain sterility for opthalmics

Back 7

1) Autoclave 121 celsius for 15 min
2) Bacterial filtration: 0.2 mcm pore size
3) Sterilizing oven with petrolatum (similar) ointment bases with non heat sensitive drug --> melts but re-solidifies
4) Antibacterial agents --> especially in preparations for intact corneal membranes (multiple dose containers)

Front 8

When are preservatives not used for opthalmics?

Back 8

For preparations used during surgery, for inserts, eye washes used in large quantities on burned or abnormal corneas, or any single dose preparations

Front 9

4 most common preservatives for opthalmics?

Back 9

1) Benzalkonium chloride
2) chlorobutanol
3) phenylmercuric acetate/nitrate
4) thimerosal

Some agents are incompatible with drugs or other ingredients

Front 10

Concentrations of preservatives tolerated by the are are ineffective against what?

Back 10

some strains of Pseudomonas Aeruginosa --> causes ulceration and blindness

Front 11

Mixtures of preservatives and other agents in opthalmics to make more preserved or more stable ore more effective for extended shelf life….

Back 11

Preservatives combined with:
1) Antibiotics (polymixin B)
2) Chelating agents (EDTA)

Ex: Benzalkonium + polymixin B (or EDTA or ALL 3!)

Front 12

Isotonicity of opthalmics have osmotic pressure similar to what?

What % can eye tolerate with tonicity?

Back 12

Lachrymal fluid = 0.9% NaCl (eye can tolerate NaCl concentrations from 0.6% to 2% --> causes discomfort b/c not isotonic)

Front 13

Why is isotonicity of opthalmics necessary?

Back 13

Needed for efficacy, safety and comfort

Front 14

A given volume of a solution of electrolyte will exert a ???? osmotic pressure than the same volume of a non-electrolyte solution?

Back 14

Greater

Front 15

If 2 liquids have same osmotic pressure they are called ????
But a liquid is ISOTONIC only when it has the same ????

Back 15

1) Isosmotic
2) same osmotic pressure as body fluid

Front 16

T or F
All solutes and agents contribute to the osmotic pressure?

Back 16

True!
Even non-electolytes
Each agent of a combination of drugs contribute to tonicity

Front 17

2 ways to calculate tonicity of opthalmic solutions?

Back 17

NaCl equivalent and freezing point depression

Front 18

USP provides pre-calibrated volumes of sterile water to be added to ????

Back 18

1g of some common opthalmic drugs to prepare isotonic solutions

Front 19

Hypertonic solutions cause what?

Back 19

If added to eye --> draws water out of cells causing shrinking

Front 20

Hypotonic solutions cause what?

Back 20

If added to eye --> water enters cells of eye and can cause bursting

Front 21

Buffering of Opthalmics help or reduce 3 things...

Back 21

1) helps maintain stability of drug b/c most drugs are weak acids or bases and need some buffer to remain stable
2) helps control therapeutic activity
3) reduces discomfort of the patient

Front 22

pH of lachrymal fluid

Back 22

7.4 with some small buffering capacity but since it is almost neutral, if a drug needs to be buffered it needs to be provided in the preparation

Front 23

2 main USP buffer vehicles

Back 23

1) Boric Acid: 1.9% boric acid solution with pH of 5.0
2) Isotonic phosphate: mixture of mono basic and dibasic salts of phosphate with pH of 5.9 - 8.0

Front 24

Fast lachrymal drainage affects what?

Back 24

Liquids with low viscosity have little contact times with corneal membranes and may not reach therapeutic effect needed

Front 25

Thickening agents added to opthalmic solutions and suspensions do what 2 things?

Back 25

1) help drug remain in cul-de-sac of eye
2) enhance therapeutic effect

Front 26

Most common opthalmic thickening agent used to increase viscosity

Back 26

Methylcellulose and cellulose derivatives

Front 27

Bioavailability of opthalmics affected by 4 things

Back 27

1) protein binding
2) Drug metabolism
3) lachrymal drainage
4) product formulation

Front 28

Protein binding affects bioavailability how?

Back 28

Proteins in tears: 0.6 - 2% make drug unavailable for absorption and therefore when binds it makes drug ineffective
Certain diseases can increase ocular protein levels

Front 29

What is uveitis?

Back 29

Inflammation of uveal tract of the eye may lead to visual impairment and blindness

Front 30

Drug metabolism affects bioavailability how?

Back 30

Lysozymes in lachrymal fluid may destroy drug before absorption occurs

Front 31

Lachrymal drainage affects bioavailability how?

Back 31

Fast removal of drug causes too brief contact with tissues

Front 32

Product formulation affects bioavailability how?

Back 32

Un-ionizied drugs (doesn't look like water or act like water) permeate cornea easier (greater lipid solubility)

Ionized drugs look and act like water and become hydrated and get absorbed less

Front 33

4 main characteristics of opthalmic solutions (eye drops/ CL products)

Back 33

1) sterile
2) isotonic
3) aqueous
4) free of particulate matter

Front 34

Opthalmic suspensions 3 main things

Back 34

1) used less than solutions but sometimes only way drug can be used opthalmically
2) extended corneal contact for improved drug action
3) particle size of suspension: very small and non-irritating to eye (no agglomeration/not gritty upon storage)

Front 35

Opthalmic ointments 4 main things (includes 2 disadvantages and 1 main advantage)

Back 35

1) manufacture from sterile ingredients or sterilized after preparation by dry heat/sterilized oven
--> ointment melts and is sterile then re-solidifiys and can use dry powders to be sterilized then added to ointment
2) Provide increased ocular contact time comported to liquid forms --> advantage
3) blurred vision disadvantage --> disadvantage
4) cannot be used with CL --> disadvantage

Front 36

Opthalmic gels designed for what?

Back 36

Extended drug action but is washed away faster than ointments because they are water soluble

Front 37

Disadvantages of opthalmic gels?

Back 37

Similar to opthalmic ointments
1) cannot be used with CL
2) blurred vision occurs

Front 38

2 examples of opthalmic gels

Back 38

1) Pilocarpine HS gel --> carbopol 949 (high MW cross-linked polymer of acrylic acid)
2) Timoptic XE: contains gellan gum which forms gel uptown contact with pre-corneal tear film

Front 39

Opthalmic inserts: structure (4 things)

Back 39

1) flexible, multilayered structure similar principle as TDDS (trans dermal delivery systems)
2) drug-controlling core: reservoir
3) rate-controlling copolymer membranes on each side
4) drug diffusion at constant rate

Front 40

Pilocarpine Insert "Ocusert"

Back 40

Type of opthalmic insert in treatment of glaucoma with either 1 week or 1 month dose

Pilocarpine placed on cul-de-sac and is sandwiched between 2 ethylene vinyl acetate membrane and alginic acid (seaweed carb) is carrier for drug

Front 41

Lacrisert

Back 41

Rod-shaped water-soluble hydroxypropyl cellulose insert for dry eyes
Q.d or b.i.d

Front 42

Nasal preparations applied how?

Back 42

1) through nasal pathway for systemic effects (inhalation)
2) into nasal passage for local effects

Front 43

3 main types of nasal preparations

Back 43

1) solution: drops, sprays, inhalants
2) suspension
3) jellies

Front 44

5 usual active ingredients

Back 44

1) Adrenergic agents as decongestants for rhinitis and sinusitis but can become desensitized to tissues
2) Anti-inflammatory agents for internal effects
3) anti-allergic agents
4) synthetic oxytocin (hormone) for breast feeding
5) insulin (inconsistent absorption so hardly used), growth hormones, other

Front 45

What occurs when adrenergic agents/decongestants are used too often?

Back 45

Should be only used 4-5 days max as rhinitis medicaments (rebound congestion) can occur and relief to congestion becomes addictive

Front 46

Types of dosage preparations for Otic/Aural/Ear preparations

Back 46

1) solutions
2) suspensions
3) ointments

All placed in ear canal for local effect ONLY

Front 47

Treatment of what types of issues?

Back 47

Inflammation, infections, pain: antibiotics, analgesics, anesthetics can be used

Front 48

Removal of excessive cerumen (ear wax) uses what ( "3" main things)

Back 48

Cerumenolytic surfactants --> triethanolamine polypeptide oleate-condensate or carbamide perioxide

Or can use light mineral oil, vegetable oil, hydrogen peroxide all dissolve cerumen

Hygroscopic co-solvents: anhydrous glycerin and PEG reduce moisture and bacterial growth and inflammation secretions