Week 1 Flashcards
who is the biggest employers of organic chemists
drug manufactures
how is the first round of testing done for antibiotics
in vitro
how many samples can big pharma companies test through high throughoutput systems
100,000 samples per day
How can antibiotics be tested in rapid form. What is this test called
high throughput screening tests
Once a drug shows promise throw in vitro what is the drug tested for_____ and what is the test called (2 names)
carcinogenicity
bacterial mutation or Ames test
how many phase’s are there of drug testing before it hits the market?
4 phases
what type of people are tested in phase 1 and what are the researchers looking for?
How long does phase one go for?
Tested on healthily people
looking for toxicity effects and metabolism.
Only last for days or a few week
Phase II is looking for, how many people, how, and how is it performed.
Double blind study and a placebo pill is used.
Smaller amount of patients than phase III
Drug dosages and adverse effects
Phase III looks for what and how many people are in it and how is it performed?
Looks for less common adverse side effects
A lot more people and Double blind study and a placebo pill is used.
What is the estimated cost to bringing a new drug on the market
802 million
What is considered a blockbuster drug
profits with over 1 billion dollars per year
Where are many of the drug trails being outsourced to? (country)
ASIA
What does PDUFA and what was the purpose
Prescription Drug User Fee Act passed 1992 allowed the FDA to hire additional evaluators due to the 1 million dollar fee
What is Phase IV intended for
If the FDA thinks there is safety questions about the drug and they could require additional follow up monitoring.
Drug companies spent around ______ per US physician in 2001
$13,000
How can drug companies extend their patent of 20 (2 ways)
if they do testing in children
suing companies that are trying to sell a generic
____ in 100,000 potential drugs makes it to the market
1
how many % of drugs pay for their development cost
30%
How much did omeperazole(prilosec) make in a year and is it a blockbuster drug
6 billion a year and yes it is
_____ was originally marketed as _____ but its side effect was growth of hair
Rogaine
antihypertensive
___1__ was meant for ___2_ and __3___ but gave a woody
1-Viagra
2-angia
3-antihypertensive
an unexpected reaction is known as (x2)
idiosyncratic
paradoxical
____ was originally approved for reducing hot flashes but was widely used to keep post-menopausal women feeling feminine and to reduce osteoporosis
Premarin
______ 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
Gabapentin (Neurontin)
80%
430 million
2.3million for lyrica (used for anti-seizure for fibromyalgia)
Molecules which increase risk of birth defects are called______
teratogens
What are the 5 classes for pregnant women
A,B,C,D and X
Category A
name 1 drug in this category!
Well controlled testing. no risk
levothyroxine
Category B
1 drug
Insufficient data or little data but safe
amoxicillin
Category C
2 drugs
Adverse effects in animal, insufficient data in humans. May be prescribed if benefits out weigh risks
ibuprofen and naproxen(aleve)
Ibuprofen & Aleve are listed as ____ in and trimester and _____ in third trimester
C
D
High doses of ______ in a fetus can cause ____ to close and used after birth to help the ____ to close
Ibuprofen
Ductus arteriosus
Ductus arteriosus
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)
Category X
name 3 drugs
Clear evidence of substantial risk of birth defects
thalidomide
DES(diethylstilbestrol)
Accutane
Thalidomide was used in the 1950’s in europe to treat _____& _____ but caused ________
sleep aid & morning sickness but caused phocomelia
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.
- diethylstilbestrol
- miscarriages
- cervical cancer & vaginal tumors
- 12 years after
____1__ is used for acne and requires the use of ____ _____ by all women who are in the child bearing age
- Accutane
Birth control
pc
after meals
ac
before meals
hs
at bedtime
NPO
nothing by mouth
non-polar molecules have what type of bond
covalent
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.
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
name four lipophilic form of the body
fat
blood brain barrier
skin
membranes
name 3 hydrophilic forms in the body
water
blood
urine
the lipophilic form of a drug is sometimes refereed to as the ________
free base forum
the pH at which the equilibrium is 50:50 is given as the ____
pKa
at pH higher than the pKa the ____ will predominate
at pH lower than the pKa the ____ will predominate
amine form
ammonium ion
for each unit change go pH by what factor does the pKa change?
by a factor of 10
Drug which have a pKa close to physiological pH (7.4) the brig will be both _____ and _____
ammonium ion form and amine form
___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
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
the ammonium ion forum of the drug is a ____ compared to the amine which is usually a ____
solid
liquid
Which form of drug last longer on the shelf and what is it less readily oxidized by
ionic ammonium ion form
Oxygen
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
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
___ _____ 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
what does CD stand for
circe diem
Intravenous drugs require ___ conditions and are ____ but produce ____ effect and absorption is complete
sterile
expensive
immediate
phenytoin(Dilantin) is only water subtle at high pH and when given IV to stop seizures the alkaline pH can cause considerable ____
pain
____ has a slow effect than IV. Absobtion depends on degree of vascularization and the form of the drug
Intramuscular (IM)
______(SC or SQ) also has slower absorption
subcutaneous
_____ _____ 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
This ____ form may be useful in patients who can’t swallow or chronic vomiting but there may be problems with variable absorption
Rectal suppository
_____ is particularly useful for treating asthma and emphysema
Respiratory (inhalation)
What are there other forms of medication
Vaginal suppository (vaginal infection)
Ocular and conjunctival
Otic (ear)
Which from of medication provides the most precise dosing and what is one problem with it?
IV but its expensive.
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
tight junctions between cells of the capillary walls in the brain requires that drugs _____ through the membrane or be ____ by specific transport
dissolve
transport
transport of lipophilic drug molecules such at Coumadin in blood occurs on ____ _____ protein molecules
serum albumen
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
