Confusing Drug Names

• Brand names are the problem

• ~3500 on market vs. 500 in 1970
• Valium (tranquillizer) vs. Kalium
(potassium supplement)
• Moditen (anti-psychotic) vs. Monitan
(treats hypertension/angina)
 Name change mandated
• Merck Frosst (Montreal) named new anti-
ulcer drug “Losec” in 1994
• Health Canada decision: Dangerously
similar to Lasix (a diuretic)
• Name changed to “Prilosec”
• Pharmaceutical Manufacturers Ass’n of
Canada: represents ~70 drug companies
 Wrong Drugs dispensed
• Chlorpromazine (anti-depressant) confused
with Chlorpropamide (diabetes).
 Reducing the Risk
• Get proper description of the prescribed
drug from physician and what condition is
being treated
• Check with Pharmacist that dispensed drug
is for prescribed condition
• Get clear dosage instructions and follow
them!
• Finish the prescribed amount ( antibiotics!)
 Cumbersome new names!
• Anthera Pharmaceuticals has a new
“cholesterol lowering drug” on trial

• Varespladib!!

• Hoping to get to market in 2011, when

Pfizer’s Lipitor is off patent
 What’s in the news?
• Pill parties
• ~20% of teens in grades 7-12 use
prescription pain killers for non-medical
purposes
 Abuse of Prescription Drugs
• Ottawa Sun; March 13, 2008
• “ Pill parties bad buzz”
 Oxy’s and Perc’s
• Pain killers: Oxycontin and Percocet
(morphine derivatives)
• Active ingredient in both is oxycodone.HCl
• Blocks signals to pain receptors in the brain
• “controlled release” 9 up to 12 hours relief
• Oxycontin: up to 160mg /tablet
• Percocet: 5 mg + acetaminophen
• Taken with alcohol “ recipe for trouble”
 Oxycodone (Morphine deriv)
• Opioid agonist: blocks signals to pain
receptors in brain
• BPEA unit
 Speeding up the time release
• Grind the pills into a powder
• Increased surface area increases the rate of
the reaction!
 Pharmaceutical Pollution
• Traces (ppb) of drugs now found in
drinking water
• Treatment facilities not designed to remove
these
• Sources: metabolites in urine, unused
prescriptions flushed away, farms
• 2008 Drug “recycling” centers being set up
• Ottawa River: Oct 20,2008: acetaminophen,
progesterone (BC) , carbamazepine Valium
 Fighting Fakes
• Counterfeit drugs~35-40B$ WW /year
• Sold under a product name without
authorization; source of drug is intentionally
mislabeled to suggest it is the approved
product; may lack any of the active
ingredients; contain > or< proper amounts
of ai’s; may have dangerous contaminants
 Sources and occurence
• WHO estimates <1% of total in USA, but
>30% in Latin America, Africa and Asia
• Epicentres of production: China and LA
18. Fitness
supplementary
ie. not in text
 Blood - the Wonder Fluid!
Blood carries -
to tissues/cells: oxygen from lungs
nutrients from intestines
hormones from endocrine glands
from tissues: carbon dioxide to lungs
metabolic wastes to excretory organs
Also -
helps maintain: 'constant' body temperature
pH/electrolyte/water balances
contains: three major kinds of blood cells
-globulins(antibodies)
 More 'Bloody' Facts!
Represents: 10-15% of body fluids(5-5.5Liters),
5-8% of body mass
Composition: 55% red cells(erythrocytes),
45% plasma,
~1% white cells(leukocytes)/'platelets'
Contained in ~100,000 km of arteries, veins and
capillaries(walls only 1 cell thick, so narrow
cells must line up to get through!
A heart beat 'pumps' ~80mL of blood, at 70beats/min
=>entire supply(6 -7L)/ min
Kidneys/liver get ~1.2L/min
Blood Composition proteins 7%
other 1%
water 92%

platelets 0.1
leukocytes
erythrocytes 99.9
Albumins(60%) Electrolytes
Globulins(35%) Organic nutrients
Fibrinogen(4%) Organic wastes
Regulatory proteins 7%
proteins (1%) other 1%
water 92%

platelets 0.1
leukocytes
erythrocytes 99.9
 Lots of Red Cells!
No nuclei  can't reproduce; formed in red 'bone
marrow' at ~3 million/sec to maintain supply,
thus average lifetime = 120 days.
Each drop of blood contains ~250 million or
30 trillion in total in the human body
Each red blood cell contains ~300 million hemo-
globin molecules
~900 trillion molecules of hemoglobin must be
synthesized every second!
Heme… Iron complex
in the globin
hemoglobin
N
2+
N Fe N
N
HOOC
- bilirubin
COO COO-
COOH

O N N N N O
H H H H
Hemoglobin - a colourful career (trivia!)
When Fe2+  Fe3+, hemoglobin turns brown =
methemoglobin (cooked meat, bloodstains)
Diet supplies 15mg iron/day but only 10% absorbed;
body must recover 20-25mg/day(stored by storage
proteins) from breakdown of hemoglobin.
Heme(porphyrin)  bilirubin(yellow)a bile pigment),
bruises, jaundice and further changes(darkening)
until it gets to the end(dark brown feces).
Blood Substitutes (artificial blood?)
• Neither term is accurate: blood performs many
imp functions; but 2 types of functions can be
produced by substitutes
• 1.Volume Expanders: widely available, used in
hospitals and in 1st response situations by
paramedics and emergency medical tech’s.
• 2. Oxygen therapeutics: perfluorocarbon based
and hemoglobin based
 Blood (Plasma) Volume Expanders

• Why Important?
• In case of blood loss, 1st need is to stop it.
• 2nd greatest need is to replace the lost
volume
• Normal blood has excess of O2 transport
capability: only use in cases of great
exertion
 We can handle low hemoglobin
(HG) levels!
• Provided blood volume is maintained by
volume expanders, a quiescent patient can
survive on ~ 1/4 of HG of a healthy person
• Body detects low HG; compensates by
pumping more volume with each beat
• If levels go to <.15 of normal, need
transfusion or packed red cells, or O2
therapeutics
 Hyperbaric Oxygen therapy
• Can be used in cases where rbc levels are
below normal life-sustaining levels
 Volume Expanders
• Are inert and merely increase blood plasma volume
• Contain lactate, saline and 5% dextrose in water
 Oxygen Therapeutics
• (i) Perfluorocarbon (PFC) emulsions
“Oxygent”
• Perfluorodecalin, surrounded by lecithin,
suspended in water to give O2 carrying
capacity
• PFC’s are exhaled; lecithin is digested
• Approved in Russia (1996) “Perftoran, not
yet in NA
 Perfluorodecalin
• Used in Oxygen therapeutics
• Can dissolve large amounts of O2.
Hemoglobin based O2 Therapeutics

• “Hemopure”
• Bovine hemoglobin (polymerized) in a salt
solution
• Need to keep Hemoglobin from dissociating
–free HG takes up NO, causing
vasoconstriction
• Approved in South Africa
The Oxygen/Carbon Dioxide Equilibrium
1) CO2 + H2O(H2CO3) <-> H+ + HCO3
2) Hmglb(H+) + O2 <-> Hmglb(O2) + H+
In lungs(exhale) when CO2 leaves blood #1 shifts to
left and (H+) (acidity) decreases. When acidity
decreases then #2 shifts to right, ie. more
hemoglobin becomes oxygenated (inhale).
Chemistry is everywhere!
 The “Freshman 15”
• Average U. or College student gains~15
pounds in 1st year
• More fast food
• More beer
• Less exercise
• Away from home “healthy” meals
 Is this you?
• It’s normal!
Fitness - help your
body do its thing
Weight: reduce strain on
bodily functions, eg.
heart, joints
(1kg 'fat' = 1000km
new capillaries!)
Rest: keep Immuno system 'tuned up'
Muscles: assists skeletal support(spine, joints),
increases bone density, helps agility/balance
Cardiorespiratory: oxygen efficiency - to burn up
carbs/ lipids for energy, to metabolize
'toxins' for excretion
 Fit or Fat!
Body Mass Index(BMI) =weight(kg)/height(meters)2
Should be between 20 -25
<20 = dangerously underweight(anorexia, bulemia)
25-27 = (overweight), take a hint!
27-30 = obese(dangerous)
>30 = life threatening
For 175lb and 5’11”: BMI = 175x.453/(1.775)2,
=25.16

(1lb=.453kg) 1”=2.5 cm

40% of NA (including many 6 -12 yrs) have BMI >27

 Exceptions to BMI
• Pregnant or lactacting women
• Under age 18 (growth incomplete)
 Konishiki
6’1’’(185cm)
606lb(275kg)
BMI = 80
 Muscles - Twitch are You?
Two types of muscle -
Fast twitch: white, anaerobic, uses little glycogen
(weight lifters, sprinters-up to 70%)
Slow twitch: red, aerobic, high glycogen use
(marathon runners-up to 85%)

'relaxed' muscle + ATP'contracted' muscle + ADP

ADP (creatine) ATP

Muscle from exercise begins to 'shrink' after 2 days

and is 'gone' after 2 months.
Probably Both
 Adenosine TriPhosphate - ATP
NH2
Pi + ADP (creatine) ATP N
N
O O O N
N
HO P O P O P O
O
OH OH OH
7.5
kcal/mol
HO OH
released
At rest body uses ATP at 40kg(~80moles)/day but at
any instant only 50g(0.1mol) available in body. May
use ~0.5kg(~1024 molecules!)/min during intense
exercise(~200X normal).
Adenosine Triphosphate(ATP:
Synthesis Details not totally known )
-Metabolic Energy $$$ -
Catabolism (Breakdown of glucose,
Carbohydrates fatty acids & (sometimes)deaminated
Fats amino acids) catalyzed by enzyme
Proteins ATP synthase: a multicomponent
complex, MW~500,000. Crystal
structure known

ADP + Pi ATP

Muscle Anabolism Transport of

contraction ions & nutrients
 Give your Heart (muscle) a Chance
At ~70 beats/min needs to stay in shape -
70b/m x 60m/h x 24h/d x 365d/y x 80y/life = !!!
Body requires ~20 moles O2/day(20% by brain)
Increase O2 supply by:
faster circulation; larger volume; efficient delivery
For VO2 max improvement(with good lungs!):
Find Maximal Rate = 220 – age
Do 65 - 80% of max rate for at least 20 mins
3x/wk just to maintain proper cardio fitness
>4x/wk to improve
Psychology of Sport and Exercise

• Individuals who have lower levels of

physical activity suffer more from stress
and anxiety
• Work off the stress (physically) and
increase your tolerance to it
 Treating Depression with Exercise
• ~25% of women and ~16% of men will suffer
from depression sometime
• Factors include: heredity, env., lifestyle, brain
chemicals, psychology, personality
• Regular exercise increases serotonin levels in the
brain: improved mood and well being
• Endorphins produced: mood elevating
• An alternative to medication for mild or moderate
depression
Exercise: Other therapeutic benefits

• Increase in self-esteem: active role in own

recovery
• Team sports also social events
• Stress chemicals such as adrenaline are used
up
• Exercise can break the cycle of pessimistic
thinking
Depression, Health and Heart attacks

• Depressed people exercise~50% less

• Lack of cardiovascular fitness increases
heart attack risk
• Sedentary lifestyle increases risk of
depression and depression increases the
likelihood of a sedentary lifestyle
 Winning Gold !

Blood doping - remove

blood(1L) 10 weeks
early, store(frozen),
then reinject day
before the event.

Erythropoietin(EPO) - natural kidney protein

available by recombinant DNA technology for
anemia treatment. Increases red blood cells by
10%. Now used(illegally) by endurance athletes
(marathoners & 'Tour de France'); excess makes
blood too viscous, won't flow and person dies.
 from London (UK) Telegraph(Sept. ’00)
‘Olympic star runs on hornet juice’
Naoko Takahashi, women’s marathon world record
holder(2hr 47 min), drank the stomach juices of
giant, killer hornets(vespa mandarina japonica)
before and during her gold-medal win at the Sydney
Olympic games.
The hornets fly 100kms/day at up to 32kms/hr and
the juice - made up of amino acids –exhibits
astonishing powers to boost human stamina. A
Japanese firm will be formulating the juices into a
palatable –and ‘legal’ drink.
Here it is!