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Pharmacology I > Test 1 Part V > Flashcards

Test 1 Part V Flashcards

1
Q

what is the fx of the transferase enzyme during a phase II biotransformation reaction

A

catalyze the coupling of an activated endogenous substance and a drug

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2
Q

which biotransformation reaction occurs faster, the P450 reaction of phase I or the conjugation reaction of phase II

A

conjugation (phase II)

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3
Q

which reaction/enzyme of phase II biotransformation is microsomal

A

glucuronide conjugation

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4
Q

which enzymes/reactions of a phase II biotransformation is non-microsomal

A

acetic acid
sulfate
glutathione
methyl

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5
Q

why does a toxic dose of tylenol cause liver failure?

A

CYP (phase I) works great, but the glutathione required for conjugation of phase II is depleted faster than it can be regenerated –> toxic metabolite build up in liver –> liver failure

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6
Q

__________________ is based on genetic inheritance of P450s

A

allergic reactions

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7
Q

what is a genetic polymorphism

A

the occurrence of a variant allelle of a gene at a population frequency of >/= 1% resulting in altered expression or functional activity of the gene product or both

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8
Q

___________________ results in altered efficacy of drug therapy or adverse drug reactions

A

genetic polymorphism

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9
Q

what is the phase II biotransformation genetic difference that is found in 50% of blacks and whites in the US causing longer time to metabolize certain drugs

A

slow acetylator

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10
Q

genetic differences causing changes in biotransformation and drug metabolism is predominately a ___________________ trait

A

autosomal recessive

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11
Q

slow acetylators are seen in _____________ of blacks and whites in the US, and there is an increased incidence in ____________________ living in high northern latitudes

A

50%; europeans

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12
Q

slow acetylation is less common in which people

A

asians and eskimos

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13
Q

in what age groups of people are there an increased pharmacologic and toxic activity

A

very young; very old

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14
Q

who metabolize certain drugs (ethanolol, propranolol, benzos, estrogens, and salicylates) faster men or women

A

men

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15
Q

your patient states in a genetic test they had done they are a slow acetylator, this means you would do what to their benzodiazepine dose prior to entering the OR

A

lower it

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16
Q

what diseases can affect drug metabolism

A
  1. acute or chronic disease of the liver
  2. cardiac disease
  3. thyroid dysfunction
  4. pulmonary disease
  5. infections (bacterial or viral)
  6. cancer
  7. inflammation
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17
Q

how does cardiac disease cause impairment of drug metabolism?

A

limits the blood flow to the liver, thus impairing the metabolism of the drugs that are flow limited or flow dependent

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18
Q

how does bacterial infections, viral infections, cancers, and inflammatory processes impair the metabolism of drugs?

A

causes release of inflammatory mediators impairing the function of P450

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19
Q

what is the first step in drug development

A

discovery/synthesis of a new drug compound or a new target (receptor)

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20
Q

in the U.S. ______________ and ____________ of drug must be defined before marketing can legally begin

A

safety; efficacy

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21
Q

in the US _______ - _______ % of healthcare money is spent on prescription drugs

A

10; 12

22
Q

less than ____________ of drugs tested in clinical trials make it to market

A

1/3

23
Q

what is teh approximate cost of developing a new drug

A

150 million to several billion

24
Q

where do most drugs orginate?

A

private sector (universities, research institutes)

25
Q

of the new drugs that achieve marketing approval, ____________% are drugs with significant advances in safety and efficacy; the rest are molecular varient compounds that are already in circulation

A

10-15

26
Q

only _______ out of 10 drugs produce a return on investment

A

2

27
Q

what is the purpose of “drug screening”

A

to define the pharmacologic profile of the drug at the molecular, cellular, organ, organ system, and organism level

28
Q

they type and number of initial drug screening tests depends on what factors?

A

the pharmacologic and therapeutic goal of a new potential drug

29
Q

drug screening results must be ______________ and ____________ to develop a pharmacologic profile

A

reliable; reproduceable

30
Q

drug screen at the molecular level

A

screen for activity on the target receptor
effects evaluated on P450 enzymes

31
Q

which level of the drug screen determines whether the drug is an antagonist, agonist, partial agonist, or inverse agonist at the target receptor

A

cellular level drug screen

32
Q

what part of the drug screen is the new drug characterized by its pharmacologic activity and selectivity

A

organ drug screen

33
Q

what part of the drug screen is the drug tested in animal studies?

A

organ system

34
Q

what information is derived from the organ system drug screen?

A

duration of action and efficacy after oral and IV administration

35
Q

drug screen at the level of the organism examines what?

A

signs and sx of adverse effects on all major organ systems

36
Q

what drug screen level is there an estimation of tolerance and/or abuse potential, physical or psychological dependence, and drug-drug interaction information obtained

A

organism level

37
Q

successful drug screening leads to the development of a ________________

A

lead compound

38
Q

what is a lead compound

A

A compound demonstrating a property that is likely to be therapeutically useful (through drug screening)

39
Q

when can someone apply for a patent on a new drug they are developing

A

after drug screening

40
Q

__________________________ is an essential step in the drug development process where limiting toxicities, therapeutic index, and risk and benefits are identified

A

preclinical safety and toxicity testing

41
Q

what is the goal of preclinical safety and toxicity testing

A
  1. ID potential human toxicities
  2. design tests to further define the toxic mechanisms
  3. predict the most relevant toxicities to be monitored during clinical trials
  4. quantitative dose estimates (used to calculate initial dose for human trials)
42
Q

in preclinical safety and toxicity testing what is the no-effect dose?

A

the max dose at which a specific toxic effect is not seen in animals

43
Q

what quantitative estimate dose from preclinical safety and toxicity testing is used as the start dose for human trials

A

1/10th - 1/100th of no-effect dose

44
Q

what is the minimal lethal dose that is obtained from preclinical safety and toxicity testing

A

smallest dose that is observed to kill any experimental animal

45
Q

what is the medial lethal dose obtained from preclinical safety and toxicity testing?

A

the dose that kills approx 50% of animals, estimated from the smallest number of animals possible

46
Q

what are the limits to preclinical safety and toxicity testing?

A
  1. time consuming and expensive
  2. large numbers of animals needed
  3. data from animal studies may not translate all potential toxicities in humans
  4. rare adverse effects are unlikely to be detected
47
Q

how long does preclinical safety and toxicity testing potentially take before a drug is ready for human testing?

A

2-6 years

48
Q

what are the 3 major confounding factors in human evaluation of a new drug

A
  1. variable natural hx of diseases
  2. presence of other diseases and risk factors
  3. subject and observer bias
49
Q

if the FDA approves a drug or food as “safe and effective” is does NOT mean ___________________________

A

free of side effects

50
Q

the pure food and drug act of 1906 is a response to what?

A

unsanitary and unethical practices in the meat packing industry

Pharmacology I (16 decks)

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