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Question 1

Factors that determine a drug’s ability to cross membranes (4)

Answer 1

1. Molecular size
2. Lipid solubility
3. Degree of ionization
4. Concentration gradient

Question 2

3 mechanisms by which derugs cross biological membranes

Answer 2

1. Passive diffusion
2. Carrier mediated diffusion
3. Endocytosis

Question 3

Components of pharmacokinetics

Answer 3

1. Absorption
2. Distribution
3. Biotransformation
4. Excretion

Question 4

Components of dosage regimen (5)

Answer 4

drug
dose
route
frequency
duration

Question 5

How to increase rate of absorption for oral route

Answer 5

1. Liquid preparations

2. Rapidly disintegrating tablets

Question 6

How to decrease rate of absorption for oral route

Answer 6

1. enteric coated products

2. sustained release preparations

Question 7

Drugs are considered bioequivalent if

Answer 7

90% confidence interval of the mean AUC and

the mean Cmax of the generic product (T-test) is within 80-125% of the brand product

Question 8

Increased GI motility= ?

Answer 8

increase speed of emptying

increase rapidity of absorption

Question 9

Percent of dose that will bypass first pass metabolism for rectal route

Answer 9

50%

Question 10

Acidic drugs bind to

Answer 10

albumin

Question 11

Basic drugs bind to

Answer 11

alpha-1 acid glycoprotein

Question 12

Example of drug-drug displacement

Answer 12

salicylate displacing methotrexate

Question 13

Vd gives an indication of:

Answer 13

the extent to which a drug DISTRIBUTES from plasma to extravascular tissue

Question 14

Molecules involved in Cytochrome p450 oxidation (3)

Answer 14

• Cofactor NADPH
• flavoprotein NADPH-cytochrome P450 reductase
• Molecular O2

Question 15

___% of Caucasians are _____ PMs

Answer 15

5-10

CYP2D6

Question 16

___% of Asians are ____ PMs

Answer 16

20%

CYP2C19

Question 17

Detoxifying:

PMs - CYP2D6

Answer 17

increased antipsychotic drug toxicity

Question 18

Detoxifying

UMs - CYP2D6

Answer 18

nonresponse to antidepressants reported

Question 19

Activating:

PMs – CYP2C19 

Answer 19

decreased efficacy of PPIs for peptic ulcer disease

Question 20

CYP450 independent:

Amine oxidase example

Answer 20

Monoamine oxidase, located in outer membrane of mitochondria. Important
enzyme in neurotransmitter metabolism.

Question 21

Types of reductions (3)

Answer 21

Azo reduction: Involved in activation of certain sulfonamides.
• Nitro reduction: Several different enzymes (microsomal, soluble, bacteria). Can produce toxic
intermediates.
• Carbonyl reduction

Question 22

Enzymes involved in hydrolysis (2)

Answer 22

• Esterases - reach adult values within first few months. Utilized in design of pro-drugs.
   Hydrolyze esters to corresponding alcohol and acid; extremely reactive enzymes
   Enzymes present in plasma, liver and other tissues
  • Amidases
   Primarily in liver and in gut flora
   Hydrolyze amides to acids and amines

Question 23

Where are glucuronyl transferases located?

Answer 23

liver, kidney, GI tract

Question 24

Sulfate conjugations result in the formation of

Answer 24

Striong acids

Question 25

Alcoholics have higher ___ levels

Answer 25

CYP2E1

Question 26

P-glycoproteins are present where? (4)

Answer 26

renal brush border membranes, bile canaliculi, astrocyte foot processes in brain microvessels, and in the GI tract.

Question 27

Ke

Answer 27

elimination constant Fraction of drug leaving body per unit of time via all elimination processes

Question 28

Drugs that most often experience enzyme saturation with therapeutic doses and, thus, zero order kinetics (3)

Answer 28

- aspirin - phenytoin - ethanol

Question 29

Half life of drugs with zero order kinetics

Answer 29

Do not have half lives

Question 30

Dobutamine is similar to the endogenous ligand ______ and binds to

Answer 30

Norepinepherine B1-adrenergic receptors on the heart

Question 31

Patient categories at high risk for drug-drug interactions (4)

Answer 31

- The elderly • Patients in high risk clinical situations: dependent on the drug treatment, acute illness, unstable disease • Patients with renal / hepatic disease (alteration of major elimination mechanisms) • Patients with multiple prescribing physicians

Question 32

Recommended osmotic cathartic

Answer 32

Sorbitol

Question 33

Ethylene glycol poisoning results in damage to the ___ due to ______.

Answer 33

Ethylene glycol poisoning results in damage to the kidneys due to deposition of calcium oxalate crystals leading to acute renal failure in most patients

Question 34

Methanol is metabolized to

Answer 34

formic acid

Question 35

Ethylene glycol is metabolized to

Answer 35

Oxalic acid

Question 36

Inhibition of alcohol dehydrogenase is done by treatment with

Answer 36

fomepizole

Question 37

General factors affecting drug absorption (5)

Answer 37

- drug solubility in biologic fluids - rate of dissolution - concentration of drug at site of administration - circulation at site of absorption - area of absorbing surface

Question 38

Inhalation: | particle size less than 0.5 microM

Answer 38

exhaled

Question 39

Inhalation: | Particle size 1-5microM

Answer 39

Deposited in small airways

Question 40

Inhalation: | Particle size greater than 10microM

Answer 40

deposited in oropharynx

Question 41

Ionized drugs can cross:

Answer 41

can cross capillary walls through pores. Thus ionized drugs can enter the plasma circulation following parenteral administration and can enter the urine tubular fluid following filtration at the glomerulus.

Question 42

Examples of metabolism of inactive compound to active ingredient (3)

Answer 42

omempazole-> a sulfonamide enalapril-> enalaprilat valacyclovir-> acyclovir

Question 43

Metabolism to a toxic metabolite: Acetaminophen->

Answer 43

N-acetyl-benzoquinoneimine

Question 44

What type of drugs are typically excreted into bile?

Answer 44

high molecular weight