Section 7 - Parenterals 2 Flashcards

(73 cards)

1
Q

What are large volume parenterals packaged in?

A

Glass or plastic

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2
Q

Are large volume parenterals preserved?

A

Never

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3
Q

What are large volume parenterals primarily used for?

A

Volume and electrolyte replacement by IV route

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4
Q

What is the volume of large volume parenterals for IV solutions?

A

100-1000 mL

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5
Q

What is the normal daily intake of water for adults?

A

50 mL/kg

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6
Q

What are the most common components in fluid replacement?

A

Sodium chloride and dextrose

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7
Q

What is an example of a hypotonic, isotonic, and hypertonic fluid replacement?

A
  • Hypotonic = 0.45% sodium chloride
  • Isotonic = 0.9% sodium chloride
  • Hypertonic = D10W
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8
Q

How are electrolyte solutions available?

A

In concentrates, which must be diluted and added to large volume parenterals

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9
Q

What are electrolyte solutions used for?

A
  • Electrolyte deficiency

- Restore pH balance

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10
Q

Why is sodium lactate used for acidosis?

A

Lactic acid is used in the Kreb’s cycle, which produces CO2, which turns into carbonate to help w/ acidosis

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11
Q

What are 2 examples of drugs that require a loading dose?

A

Heparin and lidocaine

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12
Q

Is sodium chloride or dextrose a better option to hydrate a person and why?

A

Dextrose b/c will be metabolized through the Kreb’s cycle

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13
Q

What is mannitol 10% or 20% used for?

A

Osmotic diuretics as an infusion

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14
Q

What is sodium carbonate 5% used for?

A

Treatment of acidosis

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15
Q

What is alcohol 10% in dextrose used for?

A

Methanol or ethylene glycol intoxication

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16
Q

What is the function of dextrans?

A

Plasma expanders

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17
Q

Which blood products are given as LVP?

A

Albumin, fresh-frozen plasma, whole blood

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18
Q

When can large volume parenterals exceed 1000 mL?

A
  • LVP-like products that are not meant for IV administration

- Peritoneal dialysis solutions, parenteral nutrition solutions, irrigation solutions

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19
Q

What must be determined when preparing a small volume parenteral?

A
  • Route of administration
  • Selection of vehicle
  • Required added substances
  • Appropriate container and closure
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20
Q

What is the volume for IM injections?

A

Below 10 mL

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21
Q

Which route shouldn’t be used if drug requires prolonged release?

A

IV

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22
Q

What are the most common vehicles used for SVP?

A

Aqueous, aqueous w/ co-solvents, or non-aqueous

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23
Q

Which vehicle is most desirable for SVP?

A

Aqueous, but drug solubility may be an issue

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24
Q

Which co-solvents are used w/ non-polar substances to increase water solubility?

A

Alcohol, glycerol, propylene glycol, or polyethylene glycol

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25
What are the uses of co-solvents?
- Increase solubility | - Prevent chemical degradation
26
What are some disadvantages to co-solvents?
- Tissue irritation (if given IM) - Dilution may cause drug to come out of solution - Potential toxicities if given in large dose
27
What is another way to increase solubility besides co-solvents?
Non-ionic surfactants (ex: span, tween, cremophor, labrasol)
28
What are the common concentrations of surfactants?
0.05-0.5%
29
Why are ionic surfactants not generally used?
Irritation or damage to membranes
30
What must be evaluated when using surfactants?
Safety, tissue tolerance, and hemolytic activity
31
What do surfactants do at low concentrations?
Can adsorb to the surface of the drug molecule and give the drug some polar properties
32
What do surfactants do at high concentrations?
May orient into concentrated polar and non-polar centres and form micelles
33
What are cyclodextrins?
Oligomers of glucose
34
What do cyclodextrins do?
- Can exert solubilizing effect by forming stable inclusion complexes - Amphipathic w/ exterior being hydrophilic while interior is hydrophobic
35
Which cyclodextrins can be used for parenterals?
Modified or substituted
36
What effect does an oil vehicle have on drug solubility?
Metabolizable vegetable oils may increase drug solubility
37
Oily injections are intended for ____ use
IM
38
Can oils provide prolonged/sustained release?
Yes
39
Which substances are often added to parenterals to improve efficacy, elegance, and stability?
- Buffers - Antioxidants - Antimicrobial agents - Tonicity adjusters
40
What are buffers used for in parenterals?
- Enhance stability and/or solubility | - Resist pH changes on storage
41
What can pH above 9 cause?
Tissue necrosis
42
What can pH below 3 cause?
Pain and/or phlebitis
43
What are common buffers used in parenterals?
Citrate, acetate, phosphate, and tromethamine
44
What effect does citrate on thiamine (vitamin B1)?
Increases degradation rate of thiamine
45
What effect do phosphates have on phenethicillin?
Increases degradation of phenethicillin
46
What effect do phosphates have on citrate?
Calcium will precipitate
47
What is buffer capacity?
Number of moles of strong acid/base which has to be added to 1000 mL of buffer to cause a change of 1 pH unit
48
How can you make a drug less vulnerable to oxidation?
- Lowering pH by addition of H ions - Chelating agents - Protection from light - Replacement of air w/ inert gas - Slightly acidic pH - Addition of antioxidants
49
What do antioxidants do?
Have higher oxidation potential than the drug, so are preferentially oxidized
50
What are common antioxidants used in parenterals?
Bisulfites and ascorbic acid
51
When can antioxidants not be used?
- LVPs, intrathecal, or intraocular injectables | - Avoided or used w/ caution in young children
52
What do bisulfites react w/?
- Formation of insoluble salts when bisulfites oxidize to sulfate - Bisulfate reacts w/ aldehyde functional groups
53
Antimicrobial agents must be added to parenterals in _____
Multi-dose containers
54
When are antimicrobial agents not to be used?
- LVPs, intrathecal, or intraocular injectables | - Avoided or used w/ caution in young children
55
What must be done to ensure an effective concentration of antimicrobial agents is maintained?
- Must ensure packaging doesn't adsorb to the point where the [ ] is ineffective - Ensure no other component may inactivate the antimicrobial
56
What are some common antimicrobial preservatives used in parenterals?
Benzalkonium chloride, benzyl alcohol, parabens, phenol, and chlorocresol
57
What is the easiest way to determine quantity of tonicity adjuster needed?
Sodium chloride equivalent method
58
What is the easiest way to determine quantity of tonicity adjuster needed if the product is buffered?
White-Vincent method
59
What are examples of tonicity adjusters?
Sodium chloride, dextrose, mannitol, glycerol
60
What can be added if a product is hypertonic and is to be administered by IM route?
Local anesthetic (ex: benzyl alcohol)
61
What are the 4 categories for the antimicrobial effectiveness test?
1) Parenterals, ophthalmics, otics, sterile nasal products made w/ aqueous bases or vehicles 2) Topically used products w/ aqueous bases or vehicles; non-sterile nasal products; emulsions and products applied to mucous membranes 3) Oral products other than antacids made w/ aqueous bases or vehicles 4) Antacids made w/ aqueous base
62
What is done to the product during the antimicrobial effectiveness test?
Product in original container inoculated to provide 10^5 - 10^6 colony forming units per mL of product
63
When should the effectiveness of a preservative system be retested?
Any time the formulation is changed
64
What are the functions of containers for parenterals?
- Facilitate manufacture - Maintain product integrity - Allow inspection of product - Permit shipping and storage - Provide for convenient clinical use
65
What are the 3 types of glass recognized by the USP?
1) Borosilicate, least reactive (best but most expensive) 2) Soda lime glass treated w/ sulfate, sulfite, or sulfide to make it less reactive (used for products that remain below pH 7 during shelf life) 3) Soda lime glass untreated (used for dry powders which require reconstitution)
66
What container is usually used for products which are light-sensitive?
Amber glass
67
What is a disadvantage to amber glass containers?
Ions of iron or manganese can be extracted from the glass and function as catalysts for oxidation of the drug
68
What are rubber closures used for?
Parenteral products
69
What are some problems w/ closures?
- Leaching of materials into products - Adsorption of product - Particulate contamination from container/closure combination
70
Which physical properties are important in selection of closure?
- Compression set (good plastic/elastic properties to ensure leaf-proof fit) - Flexibility - Hardness (soft enough to allow easy passage of needle - Resistance to passage of water vapor - Resealability - Tackiness (don't want closures to stick together or clump)
71
Which plastics are used for packaging parenterals?
PVC and polyethylene
72
What are advantages to plastics?
Light weight, break resistant
73
What are disadvantages to plastics?
- Moisture and gas permeability - Leaching - Adsorption of drug material