Chapter 2 (Drug design, testing, manufacturing and marketing) Flashcards
three names of drugs
chemical (used by manufacturers and chemists), generic (experts define the generic name), and trade (brand) name which only the company that developed it can use
Generic name
can be used by other companies once drug is off patent
trade name
only can be used by other companies if they buy the name rights from the original creator
benzodiazepine tranquilizers naming
all end with -am
ex. diazepam
diazepam
Valium; benzodiazepine
lorazepam
Ativan; benzodiazepine
midazolam
Versed; benzodiazepine
alprazolam
Xanax; benzodiazepine
Azmacort
treats asthma
Rythmol
treats cardiac dysrhythmias
Pepcid
treats peptic ulcer disease
Nasacort
corticosteroid nasal spray
Bronkaid
inhaled bronchodilator
Sudafed
pseudoephedrine
Cipro
ciproflaxacin
Premarin
estrogen compound from pregnant mares’ urine
Kaycel
made of potassium chloride
Elavil
elevates mood
Elimite
treatment for scabies mite
Flexeril
muscle relaxant
Nitro-bid
named for b.i.d which means twice a day
SR in drug name
slow release
Slow-K
slow release form of potassium
DS in drug name
double strength
Tylenol 4
Tylenol with 60 mg codeine/tablet
Tylenol 3
Tylenol with 30 mg codeine/tablet
Wycillin
Wyeth-Ayerst company penicllin
Wygesic
Wyeth-Ayerst company analgesic
Wytensin
Wyeth-Ayerst company med for high BP
fluoroquinolones
quinolones that were modified with a fluoro group which made them better antibiotics
Cipro
a fluoroquinolone
Levaquin
a fluoroquinolone
recombinant DNA technology drugs
first somatostatin, then HGH, but Insulin was the first to be sold
most drugs are first found in nature but…
then modified to be even better
animal trials reveal basic…
toxicology and pharmacokinetic information
ED50 and LD50 are found
drugs in same classes have about the same…
LD50
early clinical trials only use…
micro doses of drug
proof of concept
just for drug company; it is used to convince higher ups to invest money into drug
animal testing
done usually on animals selectively breeded to have the disease
after in vitro and in vivo animal studies, if the drug warrants millions in further testing then…
an IND application is filed with the FDA (investigational New Drug); IND application allows company to transmit drug across state lines for testing
in vivo studies
organ toxicity, addictive potential, side effects, teratogenicity
Ames test
test for carcinogenic properties of drug in bacteria
Drug patent
obtained after IND is granted (so before any clinical testing) and only lasts 17 years so companies hustle to get the most out of their patent before it becomes generic
phase 1 testing
20-100 volunteers that are healthy
takes about 1 year
get information about pharmacokinetic properties and elimination methods of drug (pee, breathe, etc.)
very basic dosage (safe dosage explored but proper dose not set) and safety information
phase 2 testing
100-300 volunteers with disease takes about 2 years start getting efficacy data and some side effect data therapeutic effect determined determine correct dose for phase 3
phase 3 testing
1000-3000 volunteers with disease
takes 2-4 years
test exactly how you plan to use the drug, so actual dose exactly
cost to get drug through testing
about 1 billion
drug patent extension
only last 17 years from IND, but up to 5 years can be given for certain things. 6 months is given for testing the drug on children for example.
IND
investigational new drug
Generic drugs need to have between…
75 and 125% of the brand name’s average mean drug level, but not necessarily bioequivalent
orange book
lists all generic drugs bioequivalence
ED50
effective dose 50%; half would benefit from this dose
LD50
lethal dose 50%; half would die from this dose
Therapeutic index
ratio of ED50/LD50; so high TI indicates effective treatment at low doses and lethal at high. Drugs with low TI must be monitored very closely (like digoxin)
Bioavailability
the fraction of administered dose of medication that reaches systemic circulation; differences in bioavailability can be crucial
bioavailability and bioequivalence
not the same thing; bioavail is just levels in circulation
animal tests reveal
carcinogenic potential, TI (safe dosing ranges), bioavailability (binding of drug, absorption, blood levels,…all kinetic data)
number of classic phases of drug human testing
3
drug half life
T1/2: measures levels in blood, but drugs may not accumulate in blood so there may be build up somewhere and exert effect so pharmacological action of drug over time may not be reflected by half life
side effects primarily determined…
phase 3 and 4 (postmarketing efforts of surveillance that are conducted after drug is approved by more data must still be collected). Rare side effects may not show up until thousands of people are taking the drug, so these cannot be determined until after phase 2.
efficacy primarily determined
phase 2 and 3 (phase 3 really confirms its use because they are typically double blinded and have way more people)
new drugs usually fail in phase 2 because…
lack of efficacy is found, but sometimes phase 3 must be stopped because of poor efficacy not discovered in phase 2 or new toxicity
doubel blinded
used in phase 3, but sometimes cannot be used if it is dangerous to give placebo to patients
generic and Rx drugs
have same active ingredients and are advertised in same way, but inert ingredients may be different (binders and fillers) which supposedly do not affect absorption and distribution of the drug
generic substitution
allows prescriber to insist of specific trade name by writing no substitution or dispense as written, but people often have to fight insurance companies for it
1985
FDA ruled that ads must list side effects
1997
FDA ruled that reminder adds must list side effects
top 10 TV drug commercials
Cialis and Viagra Lyrica for fibromyalgia Eliquis (a blood thinner) Celebrex (a selective cox 2 inhibitor) Monoclonal antibody drugs
phase 0
animal testing
company must have IND and patent before…
NDA and phase 2 and 3
