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PHRM 828 > Exam 4 > Flashcards

Exam 4 Flashcards

1
Q

Why shouldn’t you store medicines in a humid environment?

A

Water often reacts and degrades drugs.

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2
Q

Why are some drugs stored under nitrogen?

A

To prevent oxidation

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3
Q

How do elevated temperatures impact stability?

A

Elevated temperatures enable accelerated breakdown of a drug

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4
Q

A solution drug will be stable only….

A
  • at a given concentration
  • for a certain time
  • at a certain temperature
  • at a certain degree of light exposure
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5
Q

A solid drug will be stable only…

A
  • for a certain time
  • at a certain temperature
  • at a certain degree of light exposure
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6
Q

Which kind of solutions experience compatibility issues?

A

solutions with longer infusion times (antibiotics, insulins, some vasopressors)

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7
Q

Which decomposes faster – solutions or solids?

A

Solutions decompose 10-100 times faster.

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8
Q

Which kinds of drugs are typically refrigerated for longer stability?

A

IV drugs

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9
Q

Which IV drugs crystalize if kept cold?

A

furosemide and phenytoin

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10
Q

How are medications supplied to protect from light?

A

amber vials

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11
Q

What are the possible negative impacts of light exposure?

A

photodegradation and an increase in toxicity

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12
Q

Which drugs have to be protected from light during administration?

A

Vitamin K, Nitroprusside, Doxycycline

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13
Q

Define stability:

A

Stability is the extent to which a product retains the same properties and characteristics throughout its period of storage and use (shelf life)

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14
Q

Which chemical reactions cause drug degredation?

A

oxidation-reduction, hydrolysis, photolysis

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15
Q

How can oxidation be prevented?

A
  • protection from temperature changes
  • control pH with buffers
  • light protection
  • lower temperatures
  • chelating agents
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16
Q

How do chelating agents prevent oxidation?

A

Chelating agents such as EDTA remove metal ions which can cause oxidation

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17
Q

What is the function of antioxidants?

A

Antioxidants can remove free radicals produced by oxidation.

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18
Q

Which compounds are likely to by hydrolyzed?

A

carbonyls, amides, cyclic amides

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19
Q

How can hydrolysis be prevented?

A
  • remove moisture with absorbents
  • lyophilization
  • non-hygroscopic salts
  • control temp
  • control pH
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20
Q

What is a hygroscopic salt?

A

A solid that absorbs water

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21
Q

Define photolysis

A

Photolysis mean the drug is sensitive to light exposure and react to form new compounds in light

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22
Q

Name 3 drugs that undergo photolysis

A

vitamin c, nitroprusside, phytonadione injection

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23
Q

List functions of dosage forms:

A
  • provide an accurate dose
  • promote drug dissolution
  • promote delivery to the site of action
  • ensure drug stability
  • control drug delivery to the body
  • determine dosing interval
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24
Q

What does a carboxylic acid ester produce once it undergoes hydrolysis?

A

a carboxylic acid and an alcohol

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25
Q

What are the products of the hydrolysis of aspirin under basic conditions?

A

salicylic acid and acetic acid

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26
Q

What mechanism allows aspirin to be used for preventing strokes?

A

acetylation of cyclooxygenase

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27
Q

What is a prodrug?

A

A prodrug is a pharmacologically inactive chemical derivative of a drug.

  • Prodrugs are often created to improve the drug’s solubility or absorption
  • In the body, the prodrug is converted to the active “parent” drug chemically or enzymatically
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28
Q

How can hydrolysis of ester and lactones be prevented?

A
  • protect from moisture
  • protect from heat
  • control pH in solution formulations
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29
Q

How can you protect esters and lactones from moisture?

A

Use solid dosage forms such as tablets and capsules

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30
Q

What is the mechanism of ester and lactone hydrolysis dependent on?

A

pH

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31
Q

What kind of intermediate does the amide hydrolysis mechanism have?

A

tetrahedral intermediate

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32
Q

What does the hydrolysis of amides produce?

A

carboxylic acid and an amine

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33
Q

Which degrades slower: amides or esters?

A

amides

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34
Q

How can hydrolysis of amides and lactams be prevented?

A
  • protect from moisture
  • protect from heat
  • control pH in solution formulations
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35
Q

What drugs are amides and lactams commonly found in?

A

proteins and B-lactam antibiotics

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36
Q

What can promote oxidation?

A

exposure to oxygen, metal ions, light or heat

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37
Q

What are the two major types of oxidation?

A

auto-oxidation and chain oxidation (free radical reactions)

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38
Q

Which is slower: chain oxidation or auto-oxidation?

A

auto-oxidation

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39
Q

Define auto-oxidation

A

Auto-oxidation is the uncatalyzed oxidation of a drug by molecular oxygen

40
Q

What are the three reactions that make up chain oxidation?

A

initiation, propagation, termination

41
Q

Define initiation for chain oxidation

A

Generation of free radicals by:
- auto-oxidation
- exposure to heat
- exposure to light
- exposure to metal ions

42
Q

Define propagation

A

reaction of free radicals with oxygen or other species, with generation of new free radicals

43
Q

Define termination

A

re-combination of free radicals to form stable products

44
Q

What are the toxicity concerns with hydroquinone?

A

superoxide and hydroxyl radical (HO.) generated from it

45
Q

How can oxidation be minimized?

A
  • protecting from air, light, and metals
  • excipients added to the formulation
46
Q

How can oxidation and photolysis be prevented?

A
  • protect from oxygen (nitrogen fill)
  • protect from heat
  • protect from light
  • include anti-oxidants
  • include metal chelators
47
Q

What kind of kinetics describe drug degradation kinetics?

A

first-order

48
Q

Define half-life

A

the time required for the drug concentration to decrease to one-half of its initial value

49
Q

define shelf-life

A

the period of time that a drug product maintains its properties within specified limits

50
Q

Define expiration date

A
  • the end of the shelf-life
  • FDA requires expiration dating of all drug products
51
Q

What is shelf-life based on?

A

t90

52
Q

What is t90?

A

The time for the drug concentration to decrease to 90% of its initial value

53
Q

What is the common target shelf-life?

A

two years

54
Q

What kind of intermediate does the amide hydrolysis mechanism have?

A

tetrahedral intermediate

55
Q

What is an example of zero-order kinetics?

A
  • degradation of a drug in suspension
  • rate of drug degradation is constant – independent of concentration
56
Q

What are the stability issues for biologics?

A
  • they tend to be more fragile than small molecule drugs
  • biologics are larger than small molecules, so there are more bonds that can break
  • biologics can also lose activity if they unfold
  • biologics can aggregate
57
Q

Why is aggregation a stability issue for biologics?

A
  • it can increase or decrease potency
  • it leads to increased potential for adverse immune response
58
Q

List examples of biologics:

A
  • recombinant proteins
  • vaccines
  • stem cells
  • gene therapy
59
Q

Which are more fragile: protein drugs or small molecule drugs?

A

Protein drugs tend to be more fragile than small molecule drugs

60
Q

How do protein drugs degrade?

A
  • chemical degradation
  • physical degradation
61
Q

List characteristics of chemical degradation of protein drugs:

A
  • breaks the correct covalent bonds and forms incorrect ones
  • hydrolytic reactions
  • oxidation reactions
62
Q

List characteristics of physical degradation of protein drugs:

A
  • changes protein structure, usually without breaking covalent bonds
  • unfolding
  • aggregation
63
Q

What are examples of hydrolytic reactions for chemical protein degradation?

A
  • asparagine deamidation
  • peptide bond hydrolysis (clipping)
64
Q

What are examples of oxidation reactions for chemical protein degradation?

A
  • methionine oxidation
  • disulfide bond scrambling
65
Q

What may be more relevant than solubility alone?

A

dose solubility volume

66
Q

The solubility of a drug should be considered together with its dose.

A

True

67
Q

How did Amidon define high solubility?

A
  • If the largest human dose is soluble in 250 mL (or less) of water throughout the physiological pH range of 1-8 at 37 C.
68
Q

What does bioavailability depend on?

A
  • having the drug in solution
  • drug’s permeability
69
Q

What is a high jejunal permeability?

A
  • at lease 2-4 x 10^-4
  • corresponds to a fraction absorbed of 90% or better
70
Q

What drug are enteric polymers used for?

A

omeprazole

71
Q

What are characteristics of enteric polymers?

A
  • don’t dissolve in the stomach
  • release drug in small intestine
72
Q

What is a matrix tablet?

A

a drug embedded in polymer matrix

73
Q

Describe erosion

A

the polymer and AED go away at the same time

74
Q

Describe diffusion

A
  • outer layer of polymers swell to form gel layer
  • AED diffuse through gel
75
Q

Explain how elementary osmotic pumps (EOPs) work?

A
  • drug has osmotic core, semipermeable membrane, and a delivery orifice
  • water seeps through membrane to dissolve the drug
  • the dissolved drug is slowly released through the delivery orifice throughout the whole day
76
Q

What makes a double chamber different?

A
  • one chamber holds the drug
  • the other chamber swells with water, pushed the drug compartment out
77
Q

Describe the serum concentration of an immediate release drug:

A
  • the serum concentration levels wavers in and out of the therapeutic range.
  • this increases the risk of experiencing adverse effects and toxicity
78
Q

How does the serum concentration curve of delayed release compare to that of immediate release?

A
  • they have the same shape, but the delayed release curve is shifte to the right since it took time prior to release
79
Q

How does the serum concentration curve of extended release compare to that of immediate release?

A
  • the extended release curve has a much broader, shorter peak
  • stays within the therapeutic range
80
Q

What was the issue with generic concerta?

A

It was being substituted for Concerta even though it didn’t have the OROS system.

81
Q

What is the significance of the dry mouth graph that compares IR to XL?

A

It shows that extended release products reduce the frequency of patients experiencing adverse effects.

82
Q

Which group are most pharmaceutical advances in?

A

Group A - involves incremental tweaking of existing products

83
Q

What are the categories for the inventive ideation model?

A

change, copy, combine, separate, convert (with the problem in the center)

84
Q

What are the primary principles of the Lean Start Up?

A
  • practice makes perfect
  • quick and dirty prototype testing
  • aim for the minimum viable product
  • use customer feedback
85
Q

Describe disruptive innovation:

A
  • radical changes
  • produced by outsiders – not well established leaders
  • valued by niche customers
  • no one sees it coming – fitbit
86
Q

What is the increased life expectancy likely due to?

A

drug development

87
Q

What is the dip in life expectancy due to?

A

COVID

88
Q

Describe the solubility of antiviral drugs?

A
  • anti-viral drugs are typically very insoluble
89
Q

What is sofosbuvir?

A
  • Sofosbuvir is a prodrug.
  • it is converted to the triphosphate and inhibits the NS5B polymerase
90
Q

One way to improve solubility and bioavailability is to make an amorphous dosage form; how is this done?

A

melt extrusion

91
Q

melt extrusion

A
  • melt API and matrix powder
  • mix together
  • cool and disperse the homogenous mixture
92
Q

What are two methods to improve solubility and bioavailability?

A

melt extrusion and spray drying

93
Q

What is the purpose of abuse-deterrent technologies?

A
  • make product manipulation more difficult
  • make abuse of manipulated product less attractive
94
Q

What are examples of abuse-deterrent technologies?

A
  • improve taper resistance – OxyContin
  • incorporate deterrent – Suboxone
95
Q

How is OxyContin abuse-deterrent?

A

the new formulation can’t be crushed into powder and it turns into a gel upon trying to dissolve it

96
Q

What is the function of polyethylene oxide?

A
  • it turns into a gel when water is added
97
Q

How does PEO work?

A

PEO forms a net structure with water to produce a gel.

PHRM 828 (2 decks)

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