Chem 183 Lecture 2

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Food and Drug Administration (FDA)

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an institution established in 1906 in the USA; many other countries rely on the data and decisions provided by it

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heroin

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was used in cough syrups

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Little Early Risers Cathartic Pills

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created by DeWitt; these pills were used to relieve constipation, but they may have been toxic

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Greatfind

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medicine created by Hoffman that contained peppermint, boneset, white oak bark, and alcohol

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boneset

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a plant extract once thought to make bones stronger

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Linseed and Turpentine

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created by Dr. Chase; contains flaxseed, spruce gum, glycerin, chloroform, 1-11 grains of codeine, and 3% alcohol; probably caused some sort of high

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Mrs. Winslow's soothing Syrup

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a syrup aimed at relieving teething children; it probably contained small amounts of cocaine or heroine and alcohol

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Collier's

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a national weekly magazine at the time; it started a campaign to stir up government involvement after noticing that many people would become sick after consuming some of these products

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laudanum

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another word for opium

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Lydia Pinkham's Vegetable Compound

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claimed to cure a variety of conditions, such as bloating, headaches, nervous prostration, general debility, sleeplessness, depression, and indigestion; persists to this day

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Salversan 606

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one of the first proper drugs; it was given to people with syphilis; however few people were warned about the side effects (it contained minute amounts of arsenic)

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aspirin

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a drug that came alone in the 1800s; it is the best known pain reliever

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Bayer

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the company that discovered aspirin; they had a truck that had "overcome all pain" written in Dutch on it; would advertise aspirin alongside heroin as a cough sedative; their address was 40 Stone Street

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Federal Food, Drug, and Cosmetics Act

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came into effect in 1938; demanded proof of safety, regulated cosmetics, and food standards

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thalidomide

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a drug used in Canada and Europe for nausea in the first trimester of pregnancy; turned out to be a potent teratogen; caused children to be born with short limbs; also used to treat multiple myeloma, multiple sclerosis, ulcerative bowel disease, aphthous ulcer, Kaposi's sarcoma, kidney brain and breast cancers, and leprosy

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Thomas Quasthoff

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a German thalidomide victim who is 1 meter tall and has found success as a bass baratone

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Tony Melendez

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a Thalidomide victim who plays guitar with his feet because he has really short arms

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Dr. Frances Kelsey

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a McGill graduate; discovered thalidomide was a problem; she word for the FDA at the time and didn't think it had gone through enough testing; JFK awarded her for her discoveries in 1963; she will turn 100 next July;

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new drug

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can take 10-15 years to implement and cost 300 million dollars

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1951

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year when drugs were divided into prescription and OTC drugs; previously only narcotics and cocaine required prescription

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Steps involved in bringing a new drug to market

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identify targets; find leads; develop leads; pick and develop a candidate; make drug; formulate; toxicology; clinical trials; regulatory approval

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Kaplan Meier plot

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compares medication to placebo; shows that more people are hospitalized when taking the placebo than when taking Bidil

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Cantharidine

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an extract from Spanish flies; it was thought to be an aphrodisiac; now known to be an irritant

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periwinkle

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a flower that yields vincristine, a widely used chemotherapeutic agent

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Shaman

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witch doctor; a particular member of some cultures that has an understanding of local herbs and remedies that can be used for diseases; pharmaceutical companies sometimes refer to these people to find leads

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Fragment Based Lead Discovery Technique (FBLD)

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a technique used to build molecules for particular targets with smaller fragments based on the knowledge of what those smaller fragments do

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Lipitor and Plavix

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the largest drug sales in the US in 2011

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top-selling drugs in the world (2011)

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Lipitor (Pfizer) - 7.7 billion
Plavis (Bristol-Myers Squibb) 6.8 billion
Nexium (Astra Zeneca) 6.2 billion
Abilify (BMS) 7 billion
Advair (GlaxoSmithKline) 5 billion
Seroquel (Astra Zeneca) 5 billion

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Pfizer

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the worlds biggest pharmaceutical company

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pharmaceutical company sales

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Pfizer: 25 billion
AstraZeneca: 20 billion
Merck: 19 billion
Novartis: 19 billion

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orphan drug

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a drug developed for an extremely rare condition; doesn't have much of a market

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50%

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percentage of world drug consumption by North America

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25%

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percentage of world drug consumption by the European Union

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doubling time/half life

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70/(%)=years it takes to double or half

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Tylenol with Codeine

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drug with the highest amount of prescriptions in Canada in 1996; now it is fifth

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Lipitor

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drug with the highest amount of prescriptions in both Canada and USA currently

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Minoxidil

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a drug originally researched for high blood pressure that is now used for increasing hair growth

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excipients

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materials in a pill that are not the medicine; there are 40 different categories, such as fillers, binders, anti-foaming agents, emulsifiers, antioxidants, pigments, dessicants, granulating agents, flavorings (important for dogs); global market for them is 4billion/year

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Vioxx (Merck)

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a drug withdrawn four years ago due to bad side effects; people on the drug had a higher risk of heart attacks, but it was very effective against arthritis pain; FDA voted to keep the drug, but Merck voluntarily withdrew it

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Qatar

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country with the highest incidence of obesity

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22%

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percentage of the population that smokes

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pain relievers market

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amounts to 30 billion dollars a year, or 50 billion tablets

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16th century remedy for headaches

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put your head in an oven; they thought it got the evil spirits out of your head

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58 billion

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number of aspirin tablets consumed worldwide each year

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salicylates

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extracted from trees of the Salix family, such as the Willow tree

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methyl salicylate

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an active ingredient in Bengay; it is also called oil of wintergreen

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willow bark

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used by the Sumerians to alleviate joint pain, by the Egyptians to lessen wound inflammation, and by Hippocrates to alleviate the pain of childbirth

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Reverend Edward Stone

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rediscovered the potential of the Willow tree in 1763; his use of it was brought about by him applying the Doctrine of Signature

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Henri Leroux

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extracted Salicin from Willow bark (1829), which is the active ingredient; it was used to treat pain and fever; it is an impure substance

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Rafaelle Piria

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purified Salicin into Salicylic acid in 1838

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salicylic acid

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a compound that is an analgesic, antipyretic, and anti-inflammatory; it also is bitter tasting and causes severe stomach irritation

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Compound W

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a drug for fighting warts that has salicylic acid as an active ingredient; it is powerful enough to kill layers of skin

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Felix Hoffman

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a chemist at the Bayer company; his father had arthritis, but salicylic acid was too bad for his stomach; he created a compound that was easier on the stomach, ASA

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A-Spirin

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A: acetyl
Spirin: another name for Salix tree family

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Carl Duisberg

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the person that promoted the use of ASA; he was the director of Hoffman's lab, and was a marketing genius; ASA became the first mass-marketed drug

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heroin

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produced when morphine is treated with acetic acid; it is more addictive than morphine

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American Bayer

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lost the patent for ASA, and the name Aspirin; they then lost the right to the name Bayer; it was recuperated when the German Bayer company bought the American one; it sells Aspirin for 3x the price of generic ASA

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study performed on pain

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found that blondes feel more pain; introverts also feel more pain than extroverts, but complain less

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Ulf Von Euler (1934)

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discovered prostaglandins and won the Nobel Prize in Medicine (1970)

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John Vane

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elucidated the mode of action of prostaglandins in 1971; damaged cells produce arachidonic acid, which is a precursor to prostaglandins, which signal to the nerves that you feel pain; won the NObel Prize in Medicine in 1981

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mechanism of action of ASA

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blocks the conversion of arachidonic acid to prostaglandins; the enzyme in question is COX (cyclooxygenase); thus ASA is a Cox inhibitor

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Physician's Health Study (1989)

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studied over 22 thousand male physicians aged 40 to 84 over 5 years; men in this study were either taking a 325mg aspirin tablet every other day, or a placebo every other day; ASA decreased the rates of fatal and nonfatal heart attacks

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Thromboxane A2

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a prostaglandin that aids in blood clotting; it is blocked by ASA, which helps reduce heart attacks; however, this also thins blood

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Uses of ASA

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heart disease: 38% (30mg is sufficient for this)

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risks of ASA

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stomach bleeding and hemorrhagic stroke

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colon cancer deaths

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reduced in chronic ASA users because they are more likely to have colon bleeding and catch the cancer early; also colon cancer is associated with high COX enzyme levels

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Salicylism

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can be caused by ingesting 12-25 tablets of ASA

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Tinnitus

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can be caused by salicylism; it is a disease caused by a debilitating ringing in the ears; can push people to suicide

Front 69

children's aspirin

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comes in a lower dose (80mg) and in small bottle sizes to prevent overdose if a child gets its hands on it

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main side effects of ASA

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gastric irritation, gastrointestinal bleeding, ulcers

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allergic reactions to ASA

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rare, but can be very severe; a man in Toronto who was taking penicillin and ASA together had a severe reaction that blinded him

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Reye Syndrome

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a rare side effect of ASA named after Dr. Reye; it is the reason ASA is not recommended for teenagers and children; it causes inflammation of the brain when used to treat flu or chicken pox; this is often fatal, and causes about 300 deaths a year

Front 73

aspirin can delay delivery

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occurs because prostaglandins promote uterine contractions

Front 74

Anacin

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a drug that contains 325mg ASA and 32mg caffeine (~1/4 cup of coffee); the caffeine may help by vasoconstriction (headache is caused by blood vessel dilation) or it may cause faster absorption of the ASA

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Midol

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a drug that contains 500mg ASA, and 32mg caffeine

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Chaser

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a hangover cure that contains ASA and an antacid

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acetaminophen

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the most widely used pain reliever in North America; called paracetamol in some countries

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acetaminophen benefits

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pain relief, lowers fever, no association with Reye Syndrome

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acetaminophen downsides

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it is useless against inflammation; ineffective for heart disease prevention; affects the liver, so it should not be taken with alcohol; very toxic to cats; #1 OTC product for poisoning

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Tempra

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acetaminophen for children

Front 81

ASA free Anacin

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same as regular Anacin except with acetaminophen instead of ASA; it is easier on the stomach

Front 82

Excedrin

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a drug that used to contain ASA, but now contains acetaminophen; it contains 65mg of coffee (1/2 a cup); if you take the daily recommended amount it is like having six cups of coffee

Front 83

1982 Tylenol recall

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caused when a man replaced the Tylenol in a store bottle with cyanide; 7 people died; Tylenol recalled all the bottles and implemented safety seals

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ibuprofen

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another form of pain reliever; it is the active ingredient of Advil and Motrin

Front 85

ibuprofen benefits

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pain relief (better at relieving menstrual pain); lowers fever, lowers inflammation, no association with Reye Syndrome

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ibuprofen drawbacks

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does not help with heart disease

Front 87

Naproxen sodium

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a pain reliever that gives much longer pain relief than others; the brand name for the medication is Aleve

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market share of pain relievers in Canada

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Acetaminophen 43%
ASA 28%
ibuprofen 26%
naproxen sodium 3%

Front 89

NSAID

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non-steroidal anti-inflammatory drugs; this includes all the pain relievers except acetaminophen

Front 90

Celebrex

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a prescription drug that inhibits COX-2 specifically; Vioxx does this as well

Front 91

Merck Frosst

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was ordered to pay a woman 250 million due to the supposed Vioxx induced death of her husband (this was rejected on appeal)