DOSAGE I: Exam 4

Question 1

drugs with longer infusion times

Answer 1

1. piperacillin
2. tazobactam
3. azithromycin
4. ciprofloxacin
5. tobramycin
6. vancomycin
7. insulin

Question 2

IV drugs stored at room temperature

Answer 2

1. phenytoin (crystallizes)
2. furosemide (crystallizes)
3. metronidazole
4. moxifloxacin
5. acetaminophen
6. acyclovir
7. pentamidine
8. valproate

Question 3

light sensitive drugs

Answer 3

1. vitamin K
2. nitroprusside
3. doxycycline

supplied in amber vials to protect from light

Question 4

chemical reactions that cause drug degradation

Answer 4

1. redox
2. hydrolysis
3. photolysis

Question 5

oxidation prevention methods

Answer 5

1. pH buffers
2. protect from light - amber vials
3. lower temps
4. chelating agents (i.e. EDTA) remove metal ions
5. antioxidants (remove free radicals)

Question 6

compounds likely to be hydrolyzed

Answer 6

1. carbonyls
2. amides + cyclic amides

Question 7

hydrolysis prevention methods

Answer 7

1. protect from moisture
2. protect from heat (hydrolysis occurs faster at higher temps)
3. control pH (ester + lactone hydrolysis is pH-dependent)

Question 8

zero-order kinetics can be observed:

Answer 8

1. when drug concentration in solution is constant (i.e. suspension)
2. in solid-state

rate of drug degradation of constant - linear!

Question 9

stability issues of biologics

Answer 9

1. protein drugs tend to be more fragile than small molecule drugs
2. bigger molecules - more bonds that can break
3. lose activity if they unfold (made up of amino acids)
4. can aggregate (increases potential for adverse immune response)

Question 10

protein degradation: chemical

Answer 10

1. break/form covalent bonds
2. hydrolysis reactions
3. oxidation reactions
4. condensation

Question 11

protein degradation: physical

Answer 11

1. changes in protein structure (without breaking covalent bonds)
2. unfolding
3. aggregation -> precipitation
4. phase separation

Question 12

examples of chemical protein degradation

Answer 12

hydrolytic reactions:
-asparagine deamidation
-peptide bond hydrolysis (clipping)

oxidation reactions:
-methionine oxidation
-disulfide bond scrambling

Question 13

What is true about PEOs?

Answer 13

1. forms a net structure with water to produce a gel
2. key component of abuse deterrent drugs

Question 14

How are antiviral drugs made more soluble?

Answer 14

1. prodrug
2. formulation:
   -melt extrusion
   -spray drying

Question 15

What is sofosbuvir (prodrug) converted into?

Answer 15

the triphosphate form that inhibits the NS5B polymerase

Question 16

Amidon et al. defined a drug as having a high solubility if…

Answer 16

“the largest human dose is soluble in 250 mL (or less) of water throughout the physiological pH range of 1-8 at 37°C”

Question 17

jejunal permeability of at least _______ is considered high

Answer 17

2-4 x 10^-4 cm/s

Question 18

What do enteric polymers do?

Answer 18

resist release of API in the stomach acid, and allows for release of API in small intestine

Question 19

What is OROS?

Answer 19

osmotic-controlled release oral delivery system