Week 1 Flashcards

1
Q

who is the biggest employers of organic chemists

A

drug manufactures

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2
Q

how is the first round of testing done for antibiotics

A

in vitro

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3
Q

how many samples can big pharma companies test through high throughoutput systems

A

100,000 samples per day

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4
Q

How can antibiotics be tested in rapid form. What is this test called

A

high throughput screening tests

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5
Q

Once a drug shows promise throw in vitro what is the drug tested for_____ and what is the test called (2 names)

A

carcinogenicity

bacterial mutation or Ames test

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6
Q

how many phase’s are there of drug testing before it hits the market?

A

4 phases

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7
Q

what type of people are tested in phase 1 and what are the researchers looking for?
How long does phase one go for?

A

Tested on healthily people
looking for toxicity effects and metabolism.
Only last for days or a few week

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8
Q

Phase II is looking for, how many people, how, and how is it performed.

A

Double blind study and a placebo pill is used.
Smaller amount of patients than phase III
Drug dosages and adverse effects

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9
Q

Phase III looks for what and how many people are in it and how is it performed?

A

Looks for less common adverse side effects

A lot more people and Double blind study and a placebo pill is used.

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10
Q

What is the estimated cost to bringing a new drug on the market

A

802 million

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11
Q

What is considered a blockbuster drug

A

profits with over 1 billion dollars per year

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12
Q

Where are many of the drug trails being outsourced to? (country)

A

ASIA

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13
Q

What does PDUFA and what was the purpose

A

Prescription Drug User Fee Act passed 1992 allowed the FDA to hire additional evaluators due to the 1 million dollar fee

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14
Q

What is Phase IV intended for

A

If the FDA thinks there is safety questions about the drug and they could require additional follow up monitoring.

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15
Q

Drug companies spent around ______ per US physician in 2001

A

$13,000

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16
Q

How can drug companies extend their patent of 20 (2 ways)

A

if they do testing in children

suing companies that are trying to sell a generic

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17
Q

____ in 100,000 potential drugs makes it to the market

A

1

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18
Q

how many % of drugs pay for their development cost

A

30%

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19
Q

How much did omeperazole(prilosec) make in a year and is it a blockbuster drug

A

6 billion a year and yes it is

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20
Q

_____ was originally marketed as _____ but its side effect was growth of hair

A

Rogaine

antihypertensive

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21
Q

___1__ was meant for ___2_ and __3___ but gave a woody

A

1-Viagra
2-angia
3-antihypertensive

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22
Q

an unexpected reaction is known as (x2)

A

idiosyncratic

paradoxical

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23
Q

____ was originally approved for reducing hot flashes but was widely used to keep post-menopausal women feeling feminine and to reduce osteoporosis

A

Premarin

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24
Q

______ was originally tested and marketed for epileptic seizures but off label use for neurological pain, schizophrenia, bipolar disorder. What % of this was prescribed for off label. They were fined how much for this the first time and how much the second time

A

Gabapentin (Neurontin)
80%
430 million
2.3million for lyrica (used for anti-seizure for fibromyalgia)

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25
Q

Molecules which increase risk of birth defects are called______

A

teratogens

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26
Q

What are the 5 classes for pregnant women

A

A,B,C,D and X

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27
Q

Category A

name 1 drug in this category!

A

Well controlled testing. no risk

levothyroxine

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28
Q

Category B

1 drug

A

Insufficient data or little data but safe

amoxicillin

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29
Q

Category C

2 drugs

A

Adverse effects in animal, insufficient data in humans. May be prescribed if benefits out weigh risks
ibuprofen and naproxen(aleve)

30
Q

Ibuprofen & Aleve are listed as ____ in and trimester and _____ in third trimester

A

C

D

31
Q

High doses of ______ in a fetus can cause ____ to close and used after birth to help the ____ to close

A

Ibuprofen
Ductus arteriosus
Ductus arteriosus

32
Q

Category D

name 2 drugs

A

Clinical data on humans suggest that the drug increases the risk of birth defects. May be prescribed if benefits out weigh risks
Diazepam(valium)
Phenytoin(Dilantin)

33
Q

Category X

name 3 drugs

A

Clear evidence of substantial risk of birth defects
thalidomide
DES(diethylstilbestrol)
Accutane

34
Q

Thalidomide was used in the 1950’s in europe to treat _____& _____ but caused ________

A

sleep aid & morning sickness but caused phocomelia

35
Q

DES(____full name____) was used from 1940-1971 to prevent __2___ but caused ___3__ in the daughters and didn’t show up until __4__ years after.

A
  1. diethylstilbestrol
  2. miscarriages
  3. cervical cancer & vaginal tumors
  4. 12 years after
36
Q

____1__ is used for acne and requires the use of ____ _____ by all women who are in the child bearing age

A
  1. Accutane

Birth control

37
Q

pc

A

after meals

38
Q

ac

A

before meals

39
Q

hs

A

at bedtime

40
Q

NPO

A

nothing by mouth

41
Q

non-polar molecules have what type of bond

A

covalent

42
Q

Gabapentin is meant to treat _____ buts it’s off label use is x3 was originally tested and marketed for epileptic seizures but off label use for neurological pain, schizophrenia, bipolar disorder. What % of this was prescribed for off lab

A

epileptic seizures

off label use for neurological pain, schizophrenia, bipolar disorder.

43
Q

How can the solubility of a drug be increased? and this converts amine groups into _____ and it then becomes more _____ because of the process

A

adding an acid
ammonium ions
hydrophilic

44
Q

name four lipophilic form of the body

A

fat
blood brain barrier
skin
membranes

45
Q

name 3 hydrophilic forms in the body

A

water
blood
urine

46
Q

the lipophilic form of a drug is sometimes refereed to as the ________

A

free base forum

47
Q

the pH at which the equilibrium is 50:50 is given as the ____

A

pKa

48
Q

at pH higher than the pKa the ____ will predominate

at pH lower than the pKa the ____ will predominate

A

amine form

ammonium ion

49
Q

for each unit change go pH by what factor does the pKa change?

A

by a factor of 10

50
Q

Drug which have a pKa close to physiological pH (7.4) the brig will be both _____ and _____

A

ammonium ion form and amine form

51
Q

___1__ a commonly used anesthetic in the _2__ and __3___ Has a pKa of 9.1 thus exists in the ___4___ form. as a result it dissolves well throughout he blood stream but not cell membranes

A

1 Novocaine
2 1950
3 1960
4 cationic ammonium ion

52
Q

most drugs are marketed in the _____ of the drug shown above by reacting the amine form of the drug with ____ acid, ______ acid and ____ acid

A

ionic form

hydrochloric, sulfuric, and phosphoric

53
Q

the ammonium ion forum of the drug is a ____ compared to the amine which is usually a ____

A

solid

liquid

54
Q

Which form of drug last longer on the shelf and what is it less readily oxidized by

A

ionic ammonium ion form

Oxygen

55
Q

Oral drugs absorption is often variable and hey are usually given in the _____ form because this form is more stable to oxidation by air than the free amine

A

ionic form

56
Q

Pills may be available in the ___ ____ form which dos not dissolve in the stomach but only in the small intestine. This could help from irritation or prevent destruction of the drug in the acidic condition in the stomach

A

enteric coated

57
Q

___ _____ drugs typically have the drug encapsulated in tiny ___ whose coating dissolve at different rates. This drugs are usually indicated by x3

A

sustained release
spheres
SR XL and CD

58
Q

what does CD stand for

A

circe diem

59
Q

Intravenous drugs require ___ conditions and are ____ but produce ____ effect and absorption is complete

A

sterile
expensive
immediate

60
Q

phenytoin(Dilantin) is only water subtle at high pH and when given IV to stop seizures the alkaline pH can cause considerable ____

A

pain

61
Q

____ has a slow effect than IV. Absobtion depends on degree of vascularization and the form of the drug

A

Intramuscular (IM)

62
Q

______(SC or SQ) also has slower absorption

A

subcutaneous

63
Q

_____ _____ are to be applied topically must pass through relatively ___ layers of the epidermal and sub epidermal cells. Thus the the more lipophilic form of the drug is usually dissolved in a lipophilic cream or oil.

A

transdermal administration

lipophilic

64
Q

This ____ form may be useful in patients who can’t swallow or chronic vomiting but there may be problems with variable absorption

A

Rectal suppository

65
Q

_____ is particularly useful for treating asthma and emphysema

A

Respiratory (inhalation)

66
Q

What are there other forms of medication

A

Vaginal suppository (vaginal infection)
Ocular and conjunctival
Otic (ear)

67
Q

Which from of medication provides the most precise dosing and what is one problem with it?

A

IV but its expensive.

68
Q

The ionic ammonium ion form of drugs typically cannot pass through the ___ junctions between cells and thus cannot reach the CNS. This is the basis for the __ ___ ___

A

tight

blood brain barrier

69
Q

tight junctions between cells of the capillary walls in the brain requires that drugs _____ through the membrane or be ____ by specific transport

A

dissolve

transport

70
Q

transport of lipophilic drug molecules such at Coumadin in blood occurs on ____ _____ protein molecules

A

serum albumen

71
Q

Serum albumen binds and transports lipophilic molecules in the blood but is to big to pass through the capillary thus the drug has to separate from this protein which can take a while. Most of the exterior in hydrophilic but does have several non-polar pockets thus the lipophilic drug molecules bind reversibly yo the hydrophobic pockets. This protein transports a natural occurring lipophilic molecule through the blood and it is _____ the metabolic product of heme

A

bilirubin