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Pharmacy School 2015-16 > PHAR 733 Module 2 > Flashcards

PHAR 733 Module 2 Flashcards

1
Q

What is the Arrhenius equation?

A

k = Ae^(-Ea/RT)

or

ln k = ln A - (Ea/RT)

Ea = activation energy
A = the total number of collision
e^-Ea/RT = the probability that any given collision will result in a reaction 
K = reaction rate constant
T = absolute temperature, in Kelvin
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2
Q

What is the universal gas constant?

A

R = 1.987 cal K^-1 mole^-1

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3
Q

What is the two point Arrhenius Equation?

A

A method to determine the activation energy for a given reaction from experimental data found at two different reaction temperatures.

log K(atT2)/K(atT1) = (Ea/2.303R)(T2-T1/T2T1)

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4
Q

K at what temperature is useful for calculating half and shelf life?

A

25 degrees celcius

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5
Q

When T is increased by ten, reaction increased by ____________?

A

2-fold, shelf life decreased by 2 fold(4-fold if T increased by 20; 8 if by 30)

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6
Q

Shelf-lives for different orders of reaction

A

Zero: t90 = o.1 Ao/Ko
First: t90 = .105/K1
Second: t90 = 0.111/(Ao*k2)

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7
Q

Define Q10

A

The factor by which the rate increases when the temperature is raised by 10 degrees

Q10 = K(T + 10) / K(T)

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8
Q

What Q10 value is most accurate when Ea is unknown?

A

Q10 = 3 is most likely (2 is smallest reasonable, or possible, and 4 is the largest reasonable, or conservative)

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9
Q

Define Q(delta T)

A

Used for an arbitrary temperature change.

Q(delta T) = k(T + delta T) / k (T) = Q10 ^ DeltaT/10

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10
Q

What is the equation for Q10 method of shelf life estimation.

A

t90(forT2) = t90(forT1)/Q10^deltaT/10

A positive deltaT reduces the shelf life, a negative deltaT will increase in the shelf life

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11
Q

High is osmolarity defined

A

By the number of osmoles (osm) of solute per liter of solution

ex. 1 mol/L NaCl = 2 osmol/L of NaCl solution

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12
Q

Hypertonic solution effect on the body

A

Irritation and dehydration since fluid is drawn out (administration of hypertonic is much more consequential than administration of hypotonic solutions)

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13
Q

Define iso-osmotic solution

A

has the same solute concentration as compared to another one and contains both penetrating and non-penetrating solutes.

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14
Q

Define isotonic solution

A

Has the same osmotic pressure and contains only non-penetrating solutes

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15
Q

What are normal blood serum osmolarity values?

A

Between 275 and 300 mOsm/L.

Osmolarity of pharmaceuticals should be close to 285 mOsm/L to minimize discomfort to eyes and nose

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16
Q

What do red blood cells, blood serum, tears and 0.9% NaCl solution all have in common?

A

Have the same number of solute particles per unit volume and are isotonic and iso-osmotic

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17
Q

How to calculate dissociation factor?

A

i = total number of particles after dissociation/number before

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18
Q

Define sodium chloride equivalent (E)

A

The amount of NaCl in grams that is osmotically equivalent to 1 g of the drug

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19
Q

Define Parenteral

A

A route of administration in to the body other than through the GI tract (injection)

Enteral involves absorption through the GI tract

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20
Q

Routes of parenteral administration include

A

IV, IM, Sub-q, and ID

Other routes include:
intraarterial, intraocular, intraperitoneal, intracardiac, intraartiular (into the joints), intrathecal (cerebrospinal fluid), intraspinal and intrasynovial

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21
Q

Describe the gauge of a needle

A

Used to designate the size of the lumen, ranges from 27 (the finest) to 13(largest)

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22
Q

What are the components of an IV administration set?

A

Plastic spike (to pierce seal on iv container), drip chamber (permits adjustment of flow rate and trips air), polyvinyl chloride tubing, flow regulator, injection port, connector

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23
Q

When is the butterfly catheter used?

A

Short term IV

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24
Q

What are the best peripheral veins for IV therapy?

A

The basilic and cephalic veins on back of hand and dorsal forearm

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25
Q

What is the max injection volume for adults?

A

3L/day

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26
Q

What are the 3 categories of IV administration?

A
  1. IV bolus (push) - immediate effects needed, toxicity may occur; usually 1-2mL
  2. Intermittent infusion - drug diluted into volume of parenteral fluid (25-100mL) and infused over course of hour typically at spaced intervals; safer than IV bolus but provides less consistent drug plasma level than continuous infusion
  3. Continuous infusion - drug added to large parenteral volume and slowly administered into vein; allows simultaneous fluid and drug therapy, provides excellent drug plasma level and minimized toxicity and irritation
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27
Q

What are the disadvantages of continuous infusion?

A

Certain drugs can’t be administered like this due to extended run times, can’t be used if patient’s have restricted fluid intake, and can’t be used to admix poorly soluble drugs dissolved in water-miscible drugs

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28
Q

IM needle specs

A

1/2 inch to 1.5 inches long, 19-23 gauge (needle point should be far from nerves)

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29
Q

What is the benefit of IM route

A

Lower but more sustained blood concentrations than IV administration due to an absorption step

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30
Q

Sub-Q needle specs

A

3/8 to 1 inch long; 24-27 gauge

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31
Q

Why is absorption slower in sub-q injection compared with IM?

A

Poor vasculature in sub-q tissue

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32
Q

What are the most important drugs administered sub-q

A

Heparin and insulin

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33
Q

Injection site and limit for intradermal route?

A

anterior surface of forearm and limited to 0.1ml

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34
Q

Intradermal needle specs

A

3/8 inches long; 25-28 gauge

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35
Q

What agents are injected ID and what is the onset fast or slow?

A

Diagnostic agents, desensitization and immunization agents; onset slow

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36
Q

All parenteral products must be…

A

Sterile, pyrogen limited, free from extraneous insoluble materials

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37
Q

Define pyrogen

A

A substance, typically produced by bacterium, that produces fever and hypotension when introduced to the blood; could originate from microbes that get destroyed during sterilization

Max endotoxin level allowed by FDA: 0.2EU/kg for intrathecal, 5 for nonintrathecal, and .25-.5 for sterile water.

1 EU = 100pg of E.Coli lipopolysacharide

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38
Q

What various forms of parenteral products are available for use?

A

Solution, lyophilizied solids, emulsion, suspensions

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39
Q

Official types of injectable materials(USP)

A

Injections, for injection (dry solids that require vehicle for conversion to injection), injectable emulsion, injectable suspension, for injectable solutions (dry solid that requires addition of vehicle for conversion to injectable suspension)

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40
Q

What are the possible components of parenteral formulations?

A

Vehicles, buffering agents, preservatives, antioxidants, chelating agents, tonicity agents

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41
Q

Most common vehicle

A

Water

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42
Q

Describe water for injection, USP

A

Water for injection, USP (pyrogen free, purified and contains no more than 1mg/100mL of trace elements) - intended for use within 24hours, not required to be sterile but terminal products must be sterilized

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43
Q

Describe sterile water for injection, USP

A

Sterile water for injection, USP (water for injection that has been sterilized) - may contain more than 1mg/100ml of solids due to leaching from container during sterilization, stored in single dose not larger than 1L, and commonly used as vehicle for dry-powder injectable products

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44
Q

Describe bacteriostatic water for injection, USP

A

Sterile water for injection that contains one or more antimicrobial agents.

Packed in prefilled syringes not exceeding 30mL of water, container label must state names and proportions of preservatives, not widely used in large volume due to potential toxicity from preservatives, label must state “Note for use in Neonates”

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45
Q

Describe chloride injection, USP

A

Sterile isotonic solution of NaCl (0.9%) in water for injection, which contains no antimicrobial agents.

Often used as vehicle in parenteral solutions and suspensions, and also used as a catheter or IV lines flush to maintain patency

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46
Q

Describe bacteriostatic sodium chloride injection, USP

A

Sterile isotonic solution of sodium chloride (0.9%) in water for injection, which contains antimicrobial agents

Containers no larger than 30mL, often used as vehicle for preparing parenteral solutions and as catheter or IV line flush

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47
Q

Describe 5% dextrose injection, USP (D5W)

A

isotonic with blood and used as a water source and vehicle

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48
Q

Describe Ringer’s Injection, USP

A

Sterile solution of NaCl, potassium chloride and calcium chloride in water.

Used as a vehicle for other drugs or alone as an electrolyte replenisher and plasma volume expander.

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49
Q

What defines a hyper or hypotonic parenteral fluid? How are they used?

A

340
Hypotonic - to dilute excess serum electrolytes as in hyperglycemia
Hypertonic - to correct electrolyte imbalances, as in losses from excess vomiting and diarrhea

50
Q

What are the 2 main uses for non-aqueous vehicles?

A

Limited water solubility of the drug and susceptibility to hydrolysis

51
Q

Examples of water immiscible, non-aqueous vehicles

A

Fixed oils, ethyl oleate, isopropyl myristate, benzyle benzoate

52
Q

Examples of water miscible, non-aqueous vehicles

A

Propylene glycol, glycerol, ethyl alcohol, polyethylene glycol

53
Q

Consideration for barbiturates and digitoxin with water?

A

Barbiturates readily hydrolyzed by water; Digitoxin has poor solubility with water

54
Q

Requirement for non-aqueous vehicles

A

Non toxic in amounts administered, nonirritating, non-sensitizing, it must not exert pharmacological activity

55
Q

Considerations for non-aqueous vehicles

A

stability at various pH levels, viscosity (is it suitable for syringe), fluidity must be maintained over temp range, boiling point should be high to permit heat sterilization, constant purity or ease of purification

56
Q

Fixed-oil considerations

A

Never administer by IV, typically IM; USP restricts oils for parenteral use if oil doesn’t remain clear when cooled to 10 C; can’t contain mineral oil or paraffin since these materials aren’t absorbed by body tissues; when vegetable oils are included, label must say so in case of allergy

57
Q

Non-aqueous co-solvent considerations

A

Co-solvent concentration should be sufficient to render drug soluble with formulation but should not be irritating or toxic; formulation should not be diluted with water or precipitation may occur

58
Q

Role of preservatives and USP requirements

A

Substances added to dosage forms to protect them from microbial contamination

At least 1 suitable preservative must be added to multi dose parenteral containers unless monograph says otherwise or if injection’s active ingredients are bacteriostatic themselves.

59
Q

When are preservatives contraindicated?

A

Neonates and parenteral products with volume greater than 30mL

60
Q

When is it not necessary to add preservatives?

A

Preparation will be used immediately, no water present, ph less than 3 or more than 9

61
Q

Properties of idea preservatives

A

Effective at low concentration against wide variety of organisms, stable, soluble at required concentration, compatible with wide variety of drugs, non-toxic and non-sensitizing, free from odor, taste, color or stinging.

62
Q

What is the acceptable pH range of parenteral products and IV preparations

A

3 to 10.5

4-9

63
Q

pH above 10 can cause _______________

A

necrosis

64
Q

pH below 3 can cause _____________________

A

pain

65
Q

Buffering agent requirements

A

Nontoxic, nonirritating, sterile

66
Q

Define antioxidants and reducing agents

A

substances added to dosage forms to protect against oxidative degradation; true antioxidants have lower oxidation potential than the drugs and are preferentially oxidized

reducing agents - reduce a drug or excipient that has been oxidized

67
Q

Define chelating agents

A

Compounds that can form complexes with metal ions and inactivate their catalytic activity in the oxidation process

68
Q

Define tonicity agents and provide primary examples

A

Used to achieve isotonicity in a parenteral formulation.

Dextrose, sodium chloride, potassium chloride

69
Q

Methods of sterilization

A
  1. Use of sterile starting materials and equipment
  2. Aseptic technique
  3. Sterilization of post manufacture, preferable in final sealed containers

Methods include dry heat, steam, filtration, gas and radiation

70
Q

Describe dry heat sterilization

A

Conducted at 150 - 170 celcius for 2 to 4 hours.

Used for thermostable powders, fixed oils and glass

Disadvantages: non-uniform heat distribution, requires high temperature and long time

71
Q

Describe steam sterilization

A

Autoclave - airtight and designed to maintain high pressure and hot steam saturation (120 degrees C)

Advantages: microogranisms destroyed at lower temp with moisture, heat exchange by steam is more rapid than dry heat

Disadvantages: can’t be used for heat and moisture sensitive materials and those that aren’t penetrated by moisture (oil, fats)

72
Q

Describe filtration

A

Physical removal of microorganism (0.22 micrometer pore size; 5 micrometer for particulate matter)

Advantages: simple and convenient; ability to sterilize thermoliable materials

Disadvantages: macromolecules like proteins may be damaged in filtration, some filters absorb drugs, time consuming for large volume solution

73
Q

Different levels of filtration and what is removed with each

A

Micro (0.1 to 2 microns) - bacteria, fungi, parasites

Ultra (0.01 to 0.1 microns) - viruses

Nano (0.001 to 0.01) - organic compounds with MW 300-1000 DA (almost all pyrogens)

Reverse osmosis (under .001 microns) - also removes 90-99% of all ions

74
Q

Describe gas sterilization

A

Typically uses ethylene oxide to kill microorganism.

Advantage: sterilization of thermoliable and moisture-sensitive materials

Disadvantages: some drugs lose potency

75
Q

Describe radiation sterilization

A

Accomplished by UV light or high-energy ionizing radiation such as gamma rays.

Used for thermoliable drugs like penicillin, streptomycine, thiamine, riboflavin

Disadvantages: highly specialized equipment required, some materials are sensitive to irradiation

76
Q

Difference between large and small volume parenteral dosage forms

A

Large greater than 100

77
Q

Uses for large volume parenterals

A
  1. Maintenance therapy - used for fluid and electrolyte balance
  2. Replacement therapy - replacement of fluid and electrolytes
  3. Drug vehicle for administering other drugs
78
Q

Define physical incompatibility and list causes.

A

Interaction between 2 or more substances which lead to change insolubility, precipitation, color, odor, viscosity and morphology.

  1. pH
  2. dilution of mixed solvent systems
  3. cation-anion interactions
79
Q

Describe the pH effect

A

The sodium salts of weak acids precipitate as free acids when added to intravenous fluids with an acidic pH

80
Q

Describe dilution of mixed solvent systems

A

Precipitation on dilution in aqueous IV fluids is common with nonionized drugs that are formulated as injections with greater than 40% alcohol by volume (intermolecular h water-alcohol bonds deprive drugs of van der waals forces, solubilizing them)

81
Q

Describe cation-anion interactions

A

Precipitation is likely when oppositely charged, organic drug ions that contain aromatic rings are combined in relatively strong concentrations.

82
Q

Define chemical incompatibility

A

Decomposition of drug substance resulting from combination of parenteral dosage forms. Most result from oxidation, hydrolysis or other reactions.

83
Q

Give examples of protein drugs

A

Insulin, erythropoietin

84
Q

Stages of DNA recombination in E.coli

A

Plasmid removed and opened by restriction enzymes; DNA coding inserted into opened plasmid and plasmid then closed by ligase; introduction of recombined plasmid into E.coli host cells

85
Q

Define biotechnology

A

Any technique that uses living organisms in the production or modification of products

86
Q

How are biopharmaceuticals administered?

A

Parenteral due to their sensitive nature (would be degraded in GI if administered orally)

87
Q

Describe insulin structure

A

Two polypeptide chains (subunit A and B) connected by two disulfide bridges.

Have a tendency to form dimers in solution due to H-bonding, which will form hexamers in presence of zinc ions in blood.

Insulin produced and stored as hexamer (diffuses poorly into blood), but the active form is the monomer (readily diffuses)

88
Q

What are the general types of insulin?

A

Basal insulin (intermediate or long-acting) - the background insulin that is normally supplied by the pancreas and is present 24 hours a day, whether or not the person eats

Bolus insulin (rapid or short-acting) - the extra amounts secreted by the pancreas in response to food intake (depends on meal size)

89
Q

What are the types of pre-mixed insulin?

A

70%NPH/30% regular: 30-60 min onset, peak 2-10 hours, duration 10-18 hours

50%NPH/50%regular: 30 minutes onset, 2-5 hour peak, duration 18-24 houros

75%NPL/25% Lispro: Onset 5 minutes, peak 7-12 hours, duration 16-20 hours

90
Q

Define IU

A

International Unit - a unit of measurement for the amount of a substance, based on biological activity or effect

1 IU = 0.0347 mg of human insulin

91
Q

What level of glucose in blood plasma indicates hyperglycemia?

A

Over 200 mg/dl

92
Q

Describe Regular insulin

A

Clearly identical to human insulin synthesized through rDNA technology in a non-disease-producing lab strain of E.coli

Covers insulin needs for meals eaten within 30-60 minutes.

Can be given SC, IM or IV

93
Q

Describe formulation of regular insulin

A 
Human insulin - 100units/mL
Glycerin (isotonic agent)
Metacresol (preservative) 
Endogenouos zinc (stabilizer)
Water for injection
94
Q

Describe storage of short-acting insulin (regular insulin)

A

Stable if stored in cold place but freezing should be avoided since it reduces potency. Vial can can be stored at room temp for 28 days. Should appear clear.

95
Q

Describe rapid-acting insulin

A

Analogue of human insulin of recombinant DNA origin. Changes in structure block the formation of insulin dimers and hexamers, allowing larger amount of active monomeric insulin immediately following injection.

Humalog adjusted to pH 7 - 8 and typically injected within 15 minutes of a meal. Typically used in combination with medium or long-acting insulin

Novolog adjusted to pH 7.2-7.6. Administered 5 to 10 minutes before meal. Used with long or intermediate acting insulin

Apidra (Generic Glulisine) adjusted to pH of 7.3 and usually given with long-acting insulin. Should be given with 15 minutes of starting or 20 minutes following a meal. Used with long or intermediate acting insulin

96
Q

Describe Isophane insulin

A

Intermediate acting insulin.

Also called NPH, has neutral pH around 7.1-7.4 and is an equivalent balance between insulin and protamine.

Onset 1-2 hours, peak 6-10 and duration 16-20 (basal insulin needs for about half the day)

Suspension for SC injection, may be mixed with both rapid and short acting human regular insulin.

97
Q

Describe long-acting insulins

A

Analogues of human insulin of recombinant DNA origin.

Glargine: onset 2 hours, no peak and 20-24 duration

Detemir: onset 3-4 hours, peak 6-8 and duration up to 24

98
Q

Describe Lantus

A

pH 4 due to isoelectric shift caused by structural modifications. Precipitation shortly after injection allows for hexamer stabilization, allowing slow absorption into systemic circulation.

Injected once daily. Should not be mixed with other insulins. If used with rapid-acting, injection must be separate.

99
Q

Describe detemir

A

Neutral solution. Attached to fatty acid which causes binding to albumin, preventing fast transport into cells.

Dosed once or twice daily (duration dose dependent).

Should not be diluted or mixed with any other insulin preparations. Short or rapid-acting insulin should be given in a separate syringe.

100
Q

Describe pre-mixed insulin

A

Combination of rapid or short-acting and intermediate-acting insulin in a fixed proportion.

Twice daily injections and helps avoid administration errors if the two were injected separately.

Humulin 70/30, Novolin 70/30, Humulin 50/50

Humalog Mix 75/25, Humalog Mix (NPL/Lispro) 50/50 75/50 mix provides lower response than 50/50 SC only

101
Q

Define lipohypertrophy

A

Lump under the skin caused by accumulation of extra fat at the site of many SC injections of insulin

102
Q

Describe any disadvantages to use of insulin pens

A

More expensive, 1-2 units lost when pen is primed, not all insulin types are available in pen, pens do not let you mix insulin types.

103
Q

Describe Inhaled insulin

A

Exubera; removed from pharmacy shelves in 2007

Afrezza (Technosphere insulin) - FKDP reassembly in acidic environment to form microspheres for inhalation; proteins can be incorporated into microspheres

  • uses rapid acting with peak levels within 12-15 minutes
  • available in 4 and 8 unit and can be used for 15 days
  • not recommended for smokers
104
Q

Describe growth hormone deficiency

A

A medical condition caused by problems arising in the pituitary gland, in which the body does not produce enough growth hormone (or somatotropin)

In adults results in alteration of physiology of different systems, manifesting as altered lipid metabolism, increased SC visceral fat, decreased muscle mass, decreased bone density and low exercise performance.

105
Q

Brand name products for Somatotropin

A

Humatrope, Genotropin, Norditropin, Nutropin, Saizen

106
Q

Describe somatotropin

A

Lyophilized powder for SC after reconstitution for Bacteriostatic Water for injection, USP; Stable in refrigerator for 14 days following dilution with preservative containing dilutent; if sterile water for injection used for reconstitution, each vial should be refrigerated and used within 24 hours; administered SC at 0.16 to 0.24 mg/kg/week

107
Q

Describe Lepirudin

A

Anticoagulant drug; Brand Refludan.

Recombinant hirudin (peptide with blood anticoagulant properties) derived from yeast cells and is a highly specific direct inhibitor of thrombin

Supplied as sterile, white, freeze-dried powder for injection or infusion and is freely soluble in sterile water for injection USP or 0.9% sodium chloride for injection USP

108
Q

Describe tPA

A

Tissue plasminogen activator - protein that breaks down blood clots (only acts at clot)

Plasminogen converted to plasmin which breaks down fibrin

Generic Alteplse; Brand Activase (used in acute MI, stgroke or embolism)

Comes in sterile, white to off-white powder for IV admin after reconstitution with Sterile Water for Injection USP

109
Q

Describe clotting factor replacement medication

A

Generic: Anitihemophilic Factor (Recombinant) (rAHF)
Brand: Kogenate; Recombinate

Synthesized by genetically engineered Chinese Hamster Ovary cell line; sterile water for injection used as dilutent

110
Q

Describe Colony-stimulating factors

A

Glycoproteins that stimulate stem cells in bone marrow to form a specific kind of white blood cells that defend body against infection.

Generic: Filgrastim; Brand: Neupogen, Imumax or Grafeel

Used in cancer patients who have low white blood cell counts, putting them at risk of infection.

111
Q

Describe erythropoietine

A

Glycoprotein hormone that stimulates the production of red blood cells by stem cells in bone marrow (EPO) and is mainly produced by the kidneys. Released in response to decreased oxygen in tissue.

Generic: Epoetin Alfa
Brand: Epogen; Procrit

Approved for anemia as related to cancer chemo and chronic kidney disease

112
Q

Describe Monoclonal antibodies

A

Monospecific antibodies that are the same because they are made by identical immune cells that are clones of a unique parent cell, in contrast with polyclonal antibodies which are made from several different immune cells.

Produced by Hybridoma technology in almost unlimited quantities.

Generation 1: Murine MAbs - limited therapeutic value; recognized by human body as foreign and illicit immune response
Generation 2: Chimeric MAbs - contains human constant and murine variable region; HAMA reactions much lower
Generation 3: Humanized MAbs - 90% human, 10% mouse protein
Generation 4: Human MAbs

113
Q

Types of MAbs based on function

A

Trigger the immune system to attack cancer cells.
Generic: Rituximab
Brand: Rituxan

Block the growth of cancer tumor
Generic: Trastuzumab
Brand: Herceptin

MAbs stop new blood vessels from forming.
Generic: Bevacizumab
Brand: Avastin

Delivery of radiation drugs to cancer cells.
Generic: Ibritumomab Tiuxetan
Brand: Zevalin

Delivery of chemo drugs to cancer cells
Generic: Ado-trastuzumab Emtansine
Brand: Kadcyla

Cancer diagnosis.
Generic: Satumomab Pendetide
Brand: OncoScint

Used to reduce the body’s natural immunity in patients with organ transplants
Generic: Muromonab-CD 3
Brand: Orthoclone OKT3

Rheumatoidf Arthritis caused by overproduction of tumor necrosis factor (TNF)
Generic: Adalimumab
Brand: Humira

Pregnancy testing (by binding to hCG)

114
Q

Describe Antisense Drugs

A

Used for genetic disorders or infections. Nucleic acid strand used to bind to mRNA of gene known to cause disorder, inactivating it.

Formivirsen Sodium (Brand: Vitravene) blocks translation of viral mRNA - Indicated for cytomegalovirus (CMV) retinitis in patients with AIDS

115
Q

Diseases of the eye

A 
Myopia (nearsightedness)
Hyperopia (farsightedness)
Astigmatism (irregular cornea)
Presbyopia (lens can't bring close objects to sharp focus)
Cataracts
Glaucoma (fluid pressure)
Conjunctivitis (inflammation of conjunctiva)
Keratitis (inflammation of cornea)
116
Q

Describe Astringents

A

Used in treatment of conjunctivitis. Shrinks or constricts body tissues.

117
Q

Describe Miotics

A

Treats glaucoma. Lowers intraocular pressure by increasing drainage of aqueous humor.

118
Q

Describe mydriatics

A

Allows examination of the fundus by dilating the pupil. Cycloplegics paralyze the ciliary muscles.

119
Q

Topical administration advantages and disadvantages

A

Advantages: convenient, easy, noninvasive, fewer systemic drug effects.

Disadvantages: Low bioavailability, ineffective in treatment of posterior segment diseases

120
Q

What factors effect bioavailability (ocular)

A
  1. Precorneal factors/fluid drainage (eye maintains volume of 7 to 10 microliters; can take 30; optimal volume 7 to 10)

Solution usually flushed from eye in 1-2 minutes with less than 1% ocular absorption. Drainage influenced by viscosity and pH (excessive tear secretion). Drugs can also bind to tear proteins (0.7% of total body proteins)

  1. Corneal factors: lipophilic corneal epithelium acts as major barrier for hydrophilic drugs, hydrophilic stroma for lipophilic
  2. Postcorneal factors: Melanin binding and drug metabolism by eye enzymes
121
Q

Characteristics of Topical Formulations

A

Sterile, free from foreign particles, clarity, nonirritating, proper preservatives, pH, tonicity, viscosity, stability

Pharmacy School 2015-16 (34 decks)

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