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
Molecules which increase risk of birth defects are called______
teratogens
26
What are the 5 classes for pregnant women
A,B,C,D and X
27
Category A | name 1 drug in this category!
Well controlled testing. no risk | levothyroxine
28
Category B | 1 drug
Insufficient data or little data but safe | amoxicillin
29
Category C | 2 drugs
Adverse effects in animal, insufficient data in humans. May be prescribed if benefits out weigh risks ibuprofen and naproxen(aleve)
30
Ibuprofen & Aleve are listed as ____ in and trimester and _____ in third trimester
C | D
31
High doses of ______ in a fetus can cause ____ to close and used after birth to help the ____ to close
Ibuprofen Ductus arteriosus Ductus arteriosus
32
Category D | name 2 drugs
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
Category X | name 3 drugs
Clear evidence of substantial risk of birth defects thalidomide DES(diethylstilbestrol) Accutane
34
Thalidomide was used in the 1950's in europe to treat _____& _____ but caused ________
sleep aid & morning sickness but caused phocomelia
35
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.
1. diethylstilbestrol 2. miscarriages 3. cervical cancer & vaginal tumors 4. 12 years after
36
____1__ is used for acne and requires the use of ____ _____ by all women who are in the child bearing age
1. Accutane | Birth control
37
pc
after meals
38
ac
before meals
39
hs
at bedtime
40
NPO
nothing by mouth
41
non-polar molecules have what type of bond
covalent
42
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
epileptic seizures off label use for neurological pain, schizophrenia, bipolar disorder.
43
How can the solubility of a drug be increased? and this converts amine groups into _____ and it then becomes more _____ because of the process
adding an acid ammonium ions hydrophilic
44
name four lipophilic form of the body
fat blood brain barrier skin membranes
45
name 3 hydrophilic forms in the body
water blood urine
46
the lipophilic form of a drug is sometimes refereed to as the ________
free base forum
47
the pH at which the equilibrium is 50:50 is given as the ____
pKa
48
at pH higher than the pKa the ____ will predominate | at pH lower than the pKa the ____ will predominate
amine form | ammonium ion
49
for each unit change go pH by what factor does the pKa change?
by a factor of 10
50
Drug which have a pKa close to physiological pH (7.4) the brig will be both _____ and _____
ammonium ion form and amine form
51
___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
1 Novocaine 2 1950 3 1960 4 cationic ammonium ion
52
most drugs are marketed in the _____ of the drug shown above by reacting the amine form of the drug with ____ acid, ______ acid and ____ acid
ionic form | hydrochloric, sulfuric, and phosphoric
53
the ammonium ion forum of the drug is a ____ compared to the amine which is usually a ____
solid | liquid
54
Which form of drug last longer on the shelf and what is it less readily oxidized by
ionic ammonium ion form | Oxygen
55
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
ionic form
56
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
enteric coated
57
___ _____ drugs typically have the drug encapsulated in tiny ___ whose coating dissolve at different rates. This drugs are usually indicated by x3
sustained release spheres SR XL and CD
58
what does CD stand for
circe diem
59
Intravenous drugs require ___ conditions and are ____ but produce ____ effect and absorption is complete
sterile expensive immediate
60
phenytoin(Dilantin) is only water subtle at high pH and when given IV to stop seizures the alkaline pH can cause considerable ____
pain
61
____ has a slow effect than IV. Absobtion depends on degree of vascularization and the form of the drug
Intramuscular (IM)
62
______(SC or SQ) also has slower absorption
subcutaneous
63
_____ _____ 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.
transdermal administration | lipophilic
64
This ____ form may be useful in patients who can't swallow or chronic vomiting but there may be problems with variable absorption
Rectal suppository
65
_____ is particularly useful for treating asthma and emphysema
Respiratory (inhalation)
66
What are there other forms of medication
Vaginal suppository (vaginal infection) Ocular and conjunctival Otic (ear)
67
Which from of medication provides the most precise dosing and what is one problem with it?
IV but its expensive.
68
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 __ ___ ___
tight | blood brain barrier
69
tight junctions between cells of the capillary walls in the brain requires that drugs _____ through the membrane or be ____ by specific transport
dissolve | transport
70
transport of lipophilic drug molecules such at Coumadin in blood occurs on ____ _____ protein molecules
serum albumen
71
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
bilirubin