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 Compositionproteins 7% other 1% water 92%

platelets 0.1 leukocytes erythrocytes 99.9

proteins 7% other 1% water 92%

platelets 0.1 leukocytes erythrocytes 99.9

Albumins(60%) Globulins(35%) Fibrinogen(4%) Regulatory proteins (1%)

Electrolytes Organic nutrients Organic wastes

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

N

N

N

N

HOOC

COOH

Fe2+

COO

NH

NH

NH

NH

O

COO

O

- -

hemoglobin

bilirubin

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

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

Weight: reduce strain on bodily functions, eg. heart, joints (1kg 'fat' = 1000km new capillaries!)

Rest: keep Immuno system 'tuned up'

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

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).

O

NOP

O

OH

OP

O

OH OH

N

N

NH2

N

OH

OP

O

OH

OH

Pi + ADP (creatine) ATP

7.5 kcal/mol released

Adenosine Triphosphate(ATP: Synthesis Details not totally known )

Carbohydrates Fats

Proteins

ADP + Pi ATP

Muscle contraction

Anabolism Transport of ions & nutrients

-Metabolic Energy $$$ -Catabolism (Breakdown of glucose, fatty acids & (sometimes)deaminated amino acids) catalyzed by enzyme ATP synthase: a multicomponent complex, MW~500,000. Crystal structure known

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 !

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.

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

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!