Random Shit Flashcards

1
Q

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

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

3 mechanisms by which derugs cross biological membranes

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

Components of pharmacokinetics

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

Components of dosage regimen (5)

A
drug
dose
route
frequency
duration
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5
Q

How to increase rate of absorption for oral route

A
  1. Liquid preparations

2. Rapidly disintegrating tablets

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6
Q

How to decrease rate of absorption for oral route

A
  1. enteric coated products

2. sustained release preparations

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7
Q

Drugs are considered bioequivalent if

A

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

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8
Q

Increased GI motility= ?

A

increase speed of emptying

increase rapidity of absorption

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9
Q

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

A

50%

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10
Q

Acidic drugs bind to

A

albumin

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11
Q

Basic drugs bind to

A

alpha-1 acid glycoprotein

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12
Q

Example of drug-drug displacement

A

salicylate displacing methotrexate

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13
Q

Vd gives an indication of:

A

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

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14
Q

Molecules involved in Cytochrome p450 oxidation (3)

A
  • Cofactor NADPH
  • flavoprotein NADPH-cytochrome P450 reductase
  • Molecular O2
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15
Q

___% of Caucasians are _____ PMs

A

5-10

CYP2D6

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16
Q

___% of Asians are ____ PMs

A

20%

CYP2C19

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17
Q

Detoxifying:

PMs - CYP2D6

A

increased antipsychotic drug toxicity

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18
Q

Detoxifying

UMs - CYP2D6

A

nonresponse to antidepressants reported

19
Q

Activating:

PMs – CYP2C19 

A

decreased efficacy of PPIs for peptic ulcer disease

20
Q

CYP450 independent:

Amine oxidase example

A

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

21
Q

Types of reductions (3)

A

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

22
Q

Enzymes involved in hydrolysis (2)

A
  • 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
23
Q

Where are glucuronyl transferases located?

A

liver, kidney, GI tract

24
Q

Sulfate conjugations result in the formation of

A

Striong acids

25
Q

Alcoholics have higher ___ levels

A

CYP2E1

26
Q

P-glycoproteins are present where? (4)

A

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

27
Q

Ke

A

elimination constant

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

28
Q

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

A
  • aspirin
  • phenytoin
  • ethanol
29
Q

Half life of drugs with zero order kinetics

A

Do not have half lives

30
Q

Dobutamine is similar to the endogenous ligand ______ and binds to

A

Norepinepherine

B1-adrenergic receptors on the heart

31
Q

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

A
  • 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
32
Q

Recommended osmotic cathartic

A

Sorbitol

33
Q

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

A

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

34
Q

Methanol is metabolized to

A

formic acid

35
Q

Ethylene glycol is metabolized to

A

Oxalic acid

36
Q

Inhibition of alcohol dehydrogenase is done by treatment with

A

fomepizole

37
Q

General factors affecting drug absorption (5)

A
  • drug solubility in biologic fluids
  • rate of dissolution
  • concentration of drug at site of administration
  • circulation at site of absorption
  • area of absorbing surface
38
Q

Inhalation:

particle size less than 0.5 microM

A

exhaled

39
Q

Inhalation:

Particle size 1-5microM

A

Deposited in small airways

40
Q

Inhalation:

Particle size greater than 10microM

A

deposited in oropharynx

41
Q

Ionized drugs can cross:

A

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.

42
Q

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

A

omempazole-> a sulfonamide

enalapril-> enalaprilat

valacyclovir-> acyclovir

43
Q

Metabolism to a toxic metabolite:

Acetaminophen->

A

N-acetyl-benzoquinoneimine

44
Q

What type of drugs are typically excreted into bile?

A

high molecular weight