Stability Flashcards

1
Q

Accelerated Stability

A

-speed up process of degradation
-use higher temps of aq solutions

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2
Q

a SOLUTION drug will be stable only

A

-at given concentration
-certain time
-certain temp
-certain light exposure

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3
Q

a SOLID drug will be stable only

A

-certain time
-certain temp
-certain light exposure

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4
Q

do solutions or solids decompose faster?

A

solutions

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5
Q

Hydrolysis

A

-water cleaves molecule
-reacts and degrades drugs
-slide 3

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6
Q

Rate of hydrolysis

A

-DEcreaases as pH INCREASES

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7
Q

Oxidation

A

-catalyzed by copper
-use oxygen from atmosphere
-OH to =O
-browning onions
-store some drugs under nitrogen!

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8
Q

Oxidation of vitamin C

A

ascorbic acid + copper =dehydroacorbic acid
-makes -O to =O
-slide 12

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9
Q

Compatibility issues

A

-problem for long infusion times with piperacillin/tazobactam extended fusions
-NOT in shorter infusion times tho

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10
Q

Compatibility issues with longer infusions can occur with:

A

-other antibiotics (azithromycin, ciprofloxacin, tobramycin)
-insulin
-some vasopressors

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11
Q

Long infusion time

A

amount of time for IV to deliver drug

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12
Q

High temperature effect on stability

A

-speed up degradation

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13
Q

IV drug storage

A

-most refrigerated
-some room temperature

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14
Q

Furosemide and phenytoin

A

-crystalize if kept cold
=less bioavailability

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15
Q

Light exposure

A

-photodegradation
-may increase toxicity
-amber vials for protection
-change in color/appearance

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16
Q

Light sensitive drugs

A

-Vitamin K
-Nitroprusside
-Doxycycline

-must be protected from light during administration

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17
Q

Stability

A

the extent to which a product retains same properties and characteristics during shelf-life

18
Q

Chemical Reactions that Cause drug Degradation

A

-oxidation
-hydrolysis
-photolysis

19
Q

Oxidation of epinephrine

A

-OH oxidized to =O

20
Q

Oxidation examples

A

-vitamin C
-epinephrine
-browning onions

21
Q

Prevention of oxidation

A

-NO temp change
-buffers for pH
-light protection
-or lower temp to slow
-chelating agents
-antioxidants

22
Q

chelating agents

A

-EDTA
-remove metal ions that can cause oxidation

23
Q

antioxidants

A

remove free radicals produced by oxidation

24
Q

Compounds likely to be hydrolyzed

A

-carbonyl
-amide

25
Q

Hydrolysis prevention

A

-remove moisture with absorbants
-lyophilization (freeze-drying)
-non-hygroscopic salt (dont absorb water like other solids)
-control TEMP and PH

26
Q

Photolysis

A

-drug sensitive to light
-vitamin C
-nitroprusside
-phytonadione injection

27
Q

Other processes that degrade drugs

A

-isomerization
-epimerization
-decarboxylation

28
Q

Isomerization

A

compound changes into form with same atoms but inactive structure = cant fit

29
Q

epimerization

A

-change to isomer with diff chirality
-active or inactive

30
Q

Decarboxylation

A

-carboxylic acid lose CO2
-can be avoided by refrigeration

31
Q

function of dosage form

A

-right dose
-promote dissolution
-delivery to site of action
-ensure drug stability
-dosing interval

32
Q

Hydrolysis of esters and lactones

A

-nucleophillic attack
-MIGHT just need to know intermediate

33
Q

hydrolysis of carboxylic acid ester

A

-RCOOR
-produces carboxylic acid and alcohol

34
Q

Hydrolysis mechanism in BASIC conditions

A
  1. free OH- attacks carbon
  2. move double bond electrons to O
    (tetrahedral intermediate)
    3.move electrons back down to kick out OR ESTER group
  3. carboxylic acid with negative oxygen + OR-
  4. OR- takes H of carboxylic acid
  5. carboxylate
35
Q

Hydrolysis mechanism in BASIC conditions

A
  1. carboxylic acid protonated
  2. water attacks carbon
    (tetrahedral intermediate)
    3.
36
Q

Aspirin Hydrolysis

A

-produces salicylic acid and acetic acid
-old bottles smell like vinegar
-acetylation of COX prevents stroke

37
Q

Open an aspirin bottle what do you smell

A

VINegar

38
Q

Lactone hydrolysis

A

-cyclic esters
-opens ring = hydroxy acid

39
Q

GBL hydrolysis (lactone)

A

-opens five-membered ring
-converted to GHB in the body

40
Q

GBL

A

-lactone
-inactive
-prodrug for GBH
-absorbed more rapidly

41
Q
A