Notes Medicines and Drugs

Pharmaceutical Products
I. Introduction to Drugs
A. Definition: Drugs and medicines = substances that can cure or arrest disease, relieve
symptoms, ease pain and provide other benefits in humans, animals and plants
drugs and medicines have different meanings in different cultures
we will use the terms interchangeably (drugs are not bad)
drugs may be legal or illegal,prescribed or not
B.Origin of drugs
plant extracts - traditionally- natural medicine chinese medicines
currently - synthesized medicines produced in laboratories to ensure specific
strength and consistent supply
II. Effects of drugs and medicines
A. Before a drug is taken, symptoms and health are assessed and a specific drug is
chosen to relieve symptoms or cure condition
B. Reaction time- time needed to produce effects from drug - can range from immediate
to several weeks
C. dose and response often determined by age, weight and general health
- children and the elderly experience toxic levels earlier than adults
- therapeutic range of drug ( dosage) needs to fall between no effect and toxic
effect (this range is called the therapeutic effect)* dosage should have desired
effect (not too little not too much)
--special risk groups
- infants and children - difference in body weight, development and
function of organs (liver , kidneys)
- pregnant women and breast feeding women
- drugs may cross placenta and enter babys bloodstream
- drugs may enter breast milk and be transferred to child
-elderly
- physical changes in elderly - less efficient organs (liver)
- greater sensitivity to drugs in brain and nervous system
- changes in body ratio of body fat
- drug interactions due to use of more drugs
D. adverse effects (side effects)-- benefit v. risk
1. drugs are taken to effect a specific ailment but the drug is distributed throughout
the entire body and may have effects on places other than the target area
2. side effects may include - dry mouth, blurred vision, sensitivity to light, nausea,
vomiting and toxicity
3. not to be confused with allergies to drugs or idiosyncratic effects (particular to a
individual whose body reacts in a particular way
4.physicians will weigh the benefit v. adverse effect to determine choice of drug
*antibiotic-- diarrhea -- acceptable to kill infection
* aspirin - Reyes syndrome - diarrhea - unacceptable side effect
5. health history and combinations of other drugs help determine which drugs are
prescribed/ used
E. mechanism of drugs- how do they work - not known exactly
1. action on receptors
a. agonist drugs; enhance normal cell activity:
affinity for receptor (drug parks in space available for natural body
chemical and causes the same reactions to take place as that natural body
chemical). Drug binds to a receptor adding to the effect of the bodys
natural chemicals and enhancing cell response.
b. antagonist drugs - bind to receptors (parking space) and block cell
activity
F. placebo effect
1. chemically inert substance is used in place of a drug -- sugar pill

2. often used in clinical trials to test drugs

a. single blind -- subject does not know whether pill is placebo or not
b. double blind - subject and experimenter do not know which are
placebos
c. placebo effect can have a psychological response that produces a
beneficial physical response (subject feels better having taken
something. Some people have more positive placebo effects =
placebo responders
III. Stages of research, development and testing
A. Costly process - usually under governmental control
B. Laboratory studies on animals and cell cultures -- determine toxicity.-effective dosage
three different species of animals tested
C. Safety in animals --> clinical trials on volunteer humans -- to establish drug safety,
dosage, and possible problems
D.Second clinical trial to eliminate variables like investigator bias
E. Extended clinical trials ---> marketing (government approval of drug)
F. Testing may take USD 200 million,only very few tested drugs actually are marketed (
5 of 10,000)
G. Average of 12 years of R and D
H. Thalidomide used to treat morning sickness. Resulted in deformed babies (lacking
arms, legs...) since the drug prevented proper fetal growth. Some evidence of testing
results that were not made public. Thalidomide is currently used to treat leprosy-- and
now has published warnings on its effect on fetal development.
IV. Methods of drug administration
A. drugs must generally be absorbed in to the bloodstream to reach the site
where there effects are needed. Methods determine route to bloodstream and
speed of absorption
B. drugs are removed from body (excreted) through
1. urine (kidney removes)
2. intestine (feces)
3. lungs (exhalation)
C. by mouth
1. most common method- systemic effect (non localized
2. tablets, capsules, powder
3. swallowed and drug is absorbed into bloodstream through the walls of
the intestine, drug is then carried to liver where it may be broken down into
a form that can be used by the body.
4. Insoluble drugs are not absorbed through intestine and pass through
digestive tract unchanged - used for bowel disorders
5. form of drug (liquid, tablet...)
taken with meals or on empty stomach - faster absorption
powder - faster effect (greater surface area for absorption...)
D. rectal
1. for systemic ( effect throughout body - not localized) effect
2. suppositories
3. given for drugs that could be destroyed by stomach acids
4. given for people suffering from nausea and vomiting (morning sickness)
E. inhalation
1. for systemic(non localized) and localized effect on respiratory system
2. example - general anesthetics (for use in surgery) - absorbed through
lungs into bloodstream- advantage - speed
3. bronchodilators for asthma... - reach the respiratory tract directly through
inhalation (some of active drug also reaches the bloodstream this way)
F. injection
1. systemic effect
2. rapid response

3. used for intolerance by mouth, drug destroyed by stomach acid, or

drug incapable of passing through intestinal walls to bloodstream.
4. also used for local effect (relief of arthritis pain)
5. methods
a. intramuscular injection - into muscle -thigh, upper arm, buttock
b. subcutaneous injection - under surface of skin - TB test
c. intravenous (IV) injection- into vein (bloodstream directly) most rapid response
G. topical application
1. topical = localized non systemic effect
2. easy to control effects - maximum benefit and minimum adverse effect
3. skin cream, eye drops, ointments...
H. slow release preparations
1. systemic effect
2. slow release capsule -- capsule has outer coating that takes time to
decompose
3. transdermal patch
a. adhesive drug impregnated pad placed on skin - drug passes
slowly in to skin
b. nicotine patches, estrogen patches
4. implants
a. pellet containing drug is implanted under skin (into fatty tissue) slowly released over months - hormones -- birth control
V. Pharmaceutical vocabulary: LD50 , tolerance, side effects
a. LD50 lethal dose of substance in 50 % of the population
expressed in mg drug/ kg body mass - smaller LD50 value, the more toxic the
substance( recall problems with this method : human v. animal data, adult v.
child) toxicity values vary in different countries LD50 ethanol = 10000 mg/Kg
b. tolerance
1. occurs as the body adapts to drugs actions
2. as drug is taken over a period of time,subject needs larger and larger
doses to achieve the original effect
3. as dose increase - risks increase (toxic effects and dependence)
c. side effects see 1d- adverse effects
d. dependence (addiction)
1. compulsive use of drug resulting in physical, psychological or social
harm to the user
2. common --- caffeine, nicotine, sleeping pills
3. drugs that are mood alters are often those that cause dependence
4. psychological dependence - emotional craving for drug
5. physical dependence involves withdrawal symptoms during a period
of abstinence - head ache for caffeine withdrawal
VI. Drugs are categorized by their effect on the body
A. Antacids
Excess stomach acid is reduced by the following bases
1. aluminum and magnesium compounds
2. NaHCO3
3. Stomach (digestive) acid - generally HCl - ( along with enzymes) used to
break down food before it passes into intestine . Walls of stomach have
a layer of mucous that is constantly secreted by stomach lining. When
stomach lining is damaged or too much acid is produced, the mucous
layer is damaged.
4. excess acid (indigestion, heart burn) arises from:
anxiety, overeating, eating certain foods, consuming certain drugs ( aspirin)
5.Antacids - are bases (alkaline) or buffers that act to neutralize acid in stomach

Chalky taste is covered up with flavorings

6. Main effect- neutralize acid, prevent inflammation , relieve pain, allow mucous
layer and stomach lining to heal. Side effect - diarrhea, constipation
7. typical reaction
a. HCl + Al(OH)3 ----> HOH + AlCl3
b. NaHCO3 + HCl ---> H2C O3 + NaCl ( weaker acid produced)
8.alginates:floats on the stomach contents and produce neutralizing layer to
subdue acid that can rise into esophagus (prevents heartburn)
9.antifoaming agents (dimeticone) relieves flatulence -- value is dubious
B. Analgesics
1. Methods of pain relief (pain killer)- works in the brain and nervous systems
2. pain is merely a symptom therefore continued use of analgesics may mask a serious
problem. Production of prostaglandins: these act on nerve endings so that a signal is
passed along a series of nerve cells to the brain where the signal is interpreted as pain
by brain cells.
3. types of analgesics
a. opioids- strong analgesics- (properties similar to drugs derived from opium)morphine and codeine and within body as endorphins / naturally occurringsynthesized opiods - heroin
b. non-opoids - mild analgesics all others including
paracetamol (/ibuprophen-fever and pain)- acetaminophen
aspirin
NSAIS (non steroidal anti inflammatory drugs)
c. local and general anesthetics -- in dental work and surgery
4. mechanism of pain relief
a. opiod drugs act on the brain and spinal cord to reduce pain perception
opiods and paracetamol (acetaminophen) act like endorphins (hormones in the
brain ) that stop or block cell to cell transmission of pain
b. non-opiods (except ibuprofen). NSAID (like aspirin) act at the site of pain to
prevent the stimulation of nerve endings - block the production of prostoglandinsnerve endings are not stimulated and so no pain signal passes to the brain
5. effects of analgesics
a. mild analgesics
fewer prostoglandins will
1. reduce fever (antipyretic)
2. decrease water transfer from capillaries to tissue (swelling)
3. reduce pain
b. strong analgesics
1. relief of severe pain
2. create constipation
3. cough suppressant
4. drowsiness,(narcotic) mood changes , mental clouding
6. Derivatives of salicylic acid- see chemical formula in data booklet
aspirin is acetyl salicylic acid derived from salicylic acid and and acetic acid
a. advantages of aspirin over acetaminophen (paracetamol)
1. reduces fever, reduces in inflammation, relieve pain and inflammation of
chronic rheumatoid arthritis, low does prevents the recurrence of heart
attack.(prevents clotting in blood)
b. disadvantages
1. stomach bleeding (ulceration)- aspirin is acidic in aqueous solution
2. not recommended to children under 12 due to link to Reyes symptom
(fatal liver and brain disorder)- reaction to aspirin products after a viral
infection may trigger Reyes symptom -- generally limited to ages 3 -12
3. small % of the population is allergic
c. paracetamol (acetaminophen) is the most widely used analgesic
over dosage can be fatal (liver or kidney damage) - toxic potential is increased

in heavy drinkers- does not act as anti-inflammatory

d.ibuprofen - same effects as aspirin without stomach upset. Is anti-inflammatory
6. Structures of morphine, codeine, heroin- refer to data booklet
note the differences in functional groups but similarity of the arrangement
heroin is the product of the simple modification (change in functional groups) of
morphine (heroin is produced (synthesized from morphine)
Morphine is derived from opium (poppy plant) (10% opium)
Codeine is .5% opium
Heroin can be derived from opium, but is usually synthesized from morphine
(semi-synthetic since some of the raw materials are plant based)
Demerol, methadone are completely synthetic opiods (opiates)
7. Advantages and disadvantages of morphine and derivatives as strong analgesics
a. advantages- relieve severe pain ( often prescribed for terminal illnesses)
act directly on several sites in central nervous system involved in pain perception
- produce a state of relaxation and euphoria (relieve stress that accompanies
severe pain)
b. disadvantages
1. euphoria ---> abuse and addiction
2. prevent clear thought
3. depressed breathing
4. withdrawal symptoms very severe -5. addiction ---> physiological dependence ( body needs it )
---> adverse sociological effects - addictive behavior l may
lead to criminal behavior to support the addiction
6. heroin addicts ---> needle use and problems
---> treatment with methadone
C. Depressants
1. examples of depressants
a, alcohol
b. tranquilizers- anti anxiety drugs
c. sedatives- sleeping drugs
2. Effects of depressants
a. central nervous system effects are slowed
1. diminish environmental awareness/ responses
2. reduce rate if breathing
3. depress cognitive functioning - slow brain function
4. higher doses -- drowsiness and anesthesia
3. Social and physiological effects of use and abuse of ethanol
a. use of alcohol is recreational rather than medical.
b. second most widely used psychoactive substance in the world (after caffeine)
c. ethanol concentrations - 12% (by volume)wines, 3.5 - 10% in beers, 40 to
50% - hard liquor
d. ethanol is water soluble and fat soluble - diffuses across all biological
membranes --> rapid effect is felt
e. metabolism - mechanism of reaction - zero order (rate at which alcohol is used
up in the body is independent of the concentration of alcohol - enzyme needed
to metabolize the alcohol indicates the rate determining step) rate at which alcohol
is reacted, is independent of blood alcohol concentration
f. physiological effects of alcohol consumption
1. CNS depression
2. slowed respiration (high blood concentrations = cause of death
3. dilates blood vessels - decreases body temperature
4. low daily doses --> reduce risk of coronary artery disease (effect is lost
on smokers)
5. high doses - heart disease
6. diuretic effect
7. not an aphrodisiac -- does decrease inhibitions

8. intoxication --> major role in violent crime, highway accidents,

9. fetal alcohol syndrome
10. high dose--> liver damage, destruction of nerve cells, inc in some
cancers, delusions, uncoordinated motor behavior, hallucinations.
3. ethanol detection in breath and urine
a. breathalyzer test
1. blood alcohol EtOH(aq) <---> EtOH(g) in lungs so
alcohol concentration in exhaled breath is the same as the alcohol
concentration in blood
2. legal blood alcohol limits differ in different countries
0.05% - Japan , in US depends on area .08% (mg alcohol/ 100 cm3
blood volume)
2.breathalyser works by redox reaction with Cr2O 7-2
Cr2O 72- + 14 H+ + 6 e- ---> 4 Cr3 + + 7 H2O (reduction of Cr6 + ---> Cr3 +
C 2H5OH + H2O ---> CH3COOH + 4 e- + 4H+ (oxidation (e- in the product)
2 Cr2O 72- + 3 C2H5OH + 16 H+ --> 4 Cr3+ CH3COOH + 11 H2O
these results are not highly accurate and generally are not the only method of testing
blood alcohol levels
3. IR spec
a. breath sample is put through IR spec to identify CH and OH bonds in
alcohol.. Size of peak is determined by amount of alcohol present.
4. gas liquid chromatography
a. chromatography separates mixtures
b. breath is composed of many gases - including alcohol
c. urine samples may be used for chromatography samples as well
c. different gases will move through a gas at different rates
d. detector will identify gases in a sample and relative amounts of each
and so will be used to find blood alcohol level
4. Synergistic effects of ethanol and other drugs
a. alcohol exaggerates the depression induced by other depressants
b. effect may be supra additive - the effects are not easy to predict and may
impair ability to functions and may even lead to death.
5. Commonly used depressants and structures
a. diazepam (valium) - relieve tension and nervousness, relax muscles and
encourage sleep
b. nitrazepam (Magadon)- sleeping drug
c. fluoxetine hydrochloride (Prozac)- newer drug , fewer side effects - used in
treatment of depression, reduce binge eating and purging, obsessive
compulsive disorder
6. Physiological dependence may result from depressant use
a. withdrawal symptoms occur when drug is not taken (sleep disturbance--> life
threatening withdrawal symptoms.
b. tolerance occurs as a result of the induction of drug metabolizing enzymes in
the liver and the adaptation of cells in the brain.
Stimulants
1. in general a stimulant , stimulates the central nervous system to heightened
awareness. Amphetamines may be used to combat the effects of narcolepsy and as
an appetite suppressant ( a side effect of stimulants) and in treatment of ADHD (Ritalinday time use only - mechanism and use is in question - used to focus attention) but other
than that few if any medical treatments use amphetamines -- hence they are generally
used for recreational purposes.
2. physiological effects- Stimulants promote release of nor adrenaline increasing activity
in the RAS ( reticular activating system in the brain stem) and other parts of the brain

Stimulants may have the same effect as adrenaline (body hormone) . The major
effects of stimulants are ; wakefulness, respiratory stimulants -- cause bronchiodilationincrease heart rate, blood pressure -- (think of body reaction to something frightening)
3. Examples of stimulants are
a. nicotine
b. caffeine
c. cocaine
d. ICE - meth, crystal meth, speed
4. compare amphetamines and adrenaline
a. both derived from phenylethylamine structure (ethyl amine group attached to
benzene ring)
b. adrenaline has more attached OH groups on the benzene ring
c. see page 219 in data booklet for examples and structures
d. sympathomimetic drug - amphetamines mimic the effects of adrenaline
5. Short and long term effects of nicotine consumption
a. nicotine is found in tobacco smoke
b. age restricted in many countries but heavily advertised (aimed at children)
c. the major PREVENTABLE cause of death and disability
d. nicotine side effects are minor compared to the side effects of the tobacco
cigarette itself
e. quickly absorbed into bloodstream by smoking or chewing. smoking action
controls the dosage of nicotine
f. major effect of nicotine - initial stimulates vomiting (tolerance quickly develops)
fluid retention , reduction of muscle tone, increase in psychomotor activity,
attention and memory
g. mechanism - activates receptors which cause inc in BP, heart rate, release of
adrenaline
h. dependence is common - both physiological and psychological - comparable
to heroin , cocaine and alcohol
g. withdrawal symptoms are not life threatening but include severe craving ,
irritability, anger, difficulty in concentrating, inc appetite, insomnia... - withdrawal
may last several months
h. short term effects of nicotine: inc heart rae and BP and constricts blood
vessels (stress on heart), stimulating effects, reduction of urine output
i. long term effects; inc risk of heart disease ( stress heart), inc formation of blood
clots, acid in stomach (stimulant effect) inc peptic ulcers
g. cigarette and the tar within them cause
1. lung cancers
2.pulmonary disease (heart and respiratory problems)
3. passive smoke will also cause these problems
6. Effects of caffeine / compare structure of nicotine
a. most commonly consumed psychoactive drug in the world.
b. found in coffee, tea, chocolate, candy, cocoa, and cola
c. no restrictions on sale or use (100 cups in a day would be lethal)
d.major effect: enhanced metal alertness, increased energy and sense of well
being (does not enhance delicate muscular coordination or arithmetic skills)
e. caffeine taken orally is completely and rapidly absorbed and significant blood
levels of caffeine occur within 30 -45 minute, peak at 2 hours and decrease
thereafter
f. use of caffeine as treatment for migraine and used in combination with
analgesics- vasoconstrictor ( constricts blood vessels
g. use as a diuretic ( increases flow of urine)
h. works as on CNS - inside nerve cells to increases the metabolism within the
cells
i. tolerance issue exist with caffeine - no physical addition
i. see structures of nicotine and caffeine ( p. 219) and state common features (3
amine group)

Antibacterials
1. antibiotics were traditionally made from living organisms - molds and fungi
2. antibacterials were developed from chemicals
3. use of antibiotics - treatment of bacterial disorders
a. the bodys immune system normally protects us from illness. when immune
system is compromised or when bacteria (microorganisms) in the body migrate
to a vulnerable new site, or when a formerly unknown bacteria enters the body -infection occurs. Normally the bodys immune system produces white blood
cells to combat bacteria. When the job of white blood cells to overwhelming ,
antibiotics may be used
b. bacteria (have cell wall whereas animal cells do not , does not have defined
nucleus, has simple cell structure (no organelles), must synthesize vitamins and
have enzymes to catalyze those reactions) multiply, destroy tissue and release
toxins and may spread to vital organs.
c. examples of some common bacteria
tetanus, tuberculosis, cholera, typhoid fever, syphilis...
d. antibacterials can only work against bacteria -- not viruses (common cold, i
influenza, hepatitis, AIDS... )
4. historical development of penicillins
a. in 1890s scientists found links between fungi and bacterial death
b. in 1928 Flemming, in England, found that mold (penicillin notatum) inhibits
staphylococcus aureus bacteria but could not isolate and purify the mold
c. 1940 , Florey and Chain, at Oxford, perfected the antibiotic and by 1941 test
on humans were made. and by 1945 worldwide use of penicillin was common.three scientist shared Medical Nobel Prize for their work
5. Broad spectrum and narrow spectrum antibiotics
a. broad spectrum - effective against a variety of bacteria-tetracyclines are broad
spectrum as are amoxycillin
b. narrow spectrum - effective against a specific bacteriac. unidentified infections are often prescribed broad spectrum, until the specific
bacteria can be identified
6. How penicillins work and effects of modifying the side chain.
a. penicillins work by killing bacteria. They interfere with the chemicals needed
(by bacteria) to form normal cell walls. The cell wall disintegrates and the bacteria
die.
b. non penicillins work to prevent the production of proteins in the bacteria
(needed to survive) and hence bacteria cannot reproduce and may eventually
die.
c. structure of penicillin is unusual- 4 membered ring fused to a five membered
ring-- shape is like a half opened book
d. varying the side chains (on an amine group) will change the properties of the
penicillin and may reduce side effects, increase the spectrum range...
1. example penicillin G was only effect when administered by injection
since if was acid sensitive -- changing the side change forms another
penicillin which may be taken orally...
7. Effect of over prescription of penicillins - use in livestock - antibiotic soap
a. about 10 % of population is allergic to penicillins
b. antibiotics kill helpful bacterial (in digestive tract) as well as harmful bacteria
c. bacteria that are resistant to pencillin will survive and thrive - causing strains of
illnesses that are not helped by antibiotics now used TB, malaria... all have antibiotic resistant strains.
d. bacteria may mutate into resistant strains also
e. ongoing research into antibiotics and proper use of antibiotics is necessary
f. feeding antibiotics to factory farmed animal
1. to keep cows disease free in disease ridden conditions, livestock are
fed antibiotics .
2. as with over prescription in humans - uncontrolled use of antibiotics in
livestock is conducive to the growth of resistant strains of bacteria which are

carried in the cows and may pass to people who consume them. E coli
and salmonella are a few
g. use of antibiotic soaps
1. primary use of soaps is to remove germs from skin - not kill them
2. problems here link to over prescription of antibiotics
Antivirals
1. Virus v. bacteria
a. virus is smaller and simpler organisms than bacteria.
b. virus survive and multiply by penetrating body cells ( cannot live on their own)
c. virus is not cellular ( no nucleus, cytoplasm...) in structure
d. bacteria are cellular is structure are larger and more complex and able to
reproduce without invading body cells
2. Ways in which antivirals work
a. since virals invade body cells, finding a medicine to harm the virus without
harming the host body cell is more difficult
b. by the time symptoms appear the number of invading viruses is so great that
antivirals often are ineffective.
c. often the body can overcome viral invasions and drugs are given to relieve
pain and symptoms
d. pneumonia and meningitis need to be controlled
e. antiviral must be prescribed early in illness , as a prophylactic (preventative)
or as a vaccination
f. inoculation (vaccination) is to prevent the outbreak of viral infections of
1. polio -- now that Nigeria has stopped immunizations polio is a growing
problem in that country
2. smallpox (which appears to be irradicated {eliminated} in the world
3. most infectious viral diseases happen only one in a bodys life since
antibodies for the infection are formed upon exposure to the virus. Those
antibodies can be used to successful fight other attacks of the virus
g. topical antivirals have been successful in herpes, chickenpox and shingles
h. some antivirals work by altering the cells DNA so that the virus cannot use it to
multiply. Some work by blocking enzyme activity in the host cell. Some work
by preventing viruses from entering cells (prophylactic)
3. Difficulties in solving AIDS problem
a. AIDS - acquired immune deficiency syndrome -- is an infection caused by the
human immunodeficiency virus (HIV)
b. HIV invades immune system cells (white blood cells) and kills them
rendering the body unable to resist other infections ( that normally would not kill a
person)
c. drug treatment consists of a cocktail of drugs including antimicrobial drugs
for bacterial, viral , fungal and protozoal infections.
d. for the reasons that all viral infections are difficult to medicate - AIDS is
particularly tricky since HIV virus mutate easily
Anesthetics
1. local and general anesthetics - mode of action
a. local - block local nerve conduction and decrease blood supply (by
constricting blood vessels).
2.electrical impulse(acetylcholine) are transmitted across synapses (gaps
between nerve ends)
3. local anesthetics block the aceylcholine and therefore the impulses by blocking
the flow of Na+ across neuron membranes
4. examples of local anesthetics are procaine (Novocain), lidocaine
5. general: act on BRAIN to produce unconsciousness (inability to feel pain) .
this state is reversible
6. examples are N2O , C2H5O C2H5 , CHCl3, C3H6 , halothane

(CHClBrCF3)
2. Structures and effects of cocaine, procaine and lidocaine
a. see structures p.220
b. note similarities - all have benzene ring, all have tertiary amine with alkyl groups
attached
c. effects: cocaine -sniffed or snorted
1. formerly used as local anesthetic
2. CNS stimulant and pain blocker
3. moderate doses - overcomes fatigue, produces feeling of well being
reduced appetite, inc in heart rate and BP, dilation of pupils, inc sweating
4. large doses - agitation, anxiety, paranoia, hallucinations
5. very large doses- convulsions and death due to heart failure
6. long term effects - restlessness, nausea, insomnia , weight loss,
damage to nasal lining, fatty deposits in arteries
7. rapid metabolism in liver ( short half life in body)
8. crack cocaine is smoked - highly addictive
c. effect procaine : injected :relatively short acting useful in pre surgery or dental
procedure
d. Effect lidocaine; topically - local anesthetic to produce numbness of loss of
feeling before surgery - more potent than procaine and has side effects of itching
and swelling -- used in dentistry and general surgery
3. Advantages and Disadvantages of
a. nitrous oxide - N2O N=N=O
1. advantage: deep levels of anesthesia
2. disadvantage; low potency (not efficient) produces euphoria and is
abused
b. ethoxyethane - ether (CH3C H2)2O : shape bent
1. advantage: alleviates pain in surgery
2. highly flammable (prone to ignite and explode)
c. trichloromethane: CHCl3 - tetrahedral shape
1. advantage: non flammable
2. leads to liver damage, small difference between dosage that is
anesthetic and lethal
d. cyclopropane: C3H6 cyclic trigonal planar ring
1. potent, inhaled, used for all types of surgery
2. forms explosive mixtures with air, highly flammable, may cause
vomiting , headache and nausea.
e. halothane- CF3CBrClH: chiral carbon
1. advantage non flammable , widely used, non irritating, rapid recovery
2. disadvantage ; harmful to ozone layer - free radical production, recovery
time is greater
4. Calc Partial pressure of component gases in anesthetic mixture
A. Daltons law of partial pressure PT = P1 + P2 + P3
B. Ideal gas law ( independent of gas identity)
PV = nRT
C. To find pressure of a specific gas Pa = Xa PT where Xa = mole fraction
moles of gas a/ total moles of all gases
D. When anesthetics are inhaled - O2 must be in the gaseous mixture
1. hypoxia - low concentration of O2 in blood can lead to brain damage
2. recreational use of inhalants may cause this effect ( minimum [ O2] is 20
% in inhaled gas) . To reach a recreational euphoria 50 % concentration of
N2O may be needed - if mixed with air , the [O2) is less than the
necessary 20 % and damage may occur

Mind-altering drugs
1. Effects of
a. LSD - a hallucinogen,experience is personal and varies with dose,
physiological and psychological condition- Perception is magnified, judgment is
altered. Lasts 8 hrs. Does not produce physical addition but tolerance
develops. Flash backs and bad trips are possible.
b. mescaline- produces color hallucinations- vivid color perception
c. psilocybin- magic mushrooms
low doses - relaxation
high doses- like LSD hallucinations - lasts 4 hrs
d. THC- in cannabis
low doses - similar to alcohol
higher doses - hallucinogenic effect - changes in perception
joy --> anxiety, depression , panic, difficulty in decision making
no tolerance but moderate psychological dependence
2. Structural similarities and differences between LSD, mescaline and psilocybin
a. Indole = cyclic amine compound where N is part of the ring see diagram
b. LSD and psilocybin both have indole ring
c. LSD has diethylamide side chain
d. psilocygin has dimethyl
3. Arguments for and against legalization of cannabis
a. for: relieves nausea, appetite increases -- treatment for chemotherapy
relieves pressure in eyeball - glaucoma treatment
illegal drug trade make money from the use, if regulated the crime and
cost would be monitored
b. against : respiratory problems, affects fertility, gateway drug
Stereo chemistry in Drug action and design
1. stereo isomers: same molecular formula and structural formula but different spatial
arrangement of atoms.
2. geometric isomerism = cis trans -- across a double bond or ring structure
3. optical isomers= chiral center - non superimposable mirror images
4. physical properties
a. differ in geometric isomer
b. are identical in optical isomers
5. chemical properties
a. geometric - have same functional group --> similar chem properties but
different isomer may show different pharmacological effects (one isomer is
effective while the other is not)
b. optical - enantiomers show opposite reaction to plane polarized light
rotates to clockwise or anticlockwise direction
6. identify chiral center - 4 different bonds around the central carbon atom
7. racemic mixture - equi-molar mixture of two enantiomers. This mixture will not rotate
PPL since the effects of each isomer cancel each other out.
8. drugs that are semi-synthetic (modified natural substances) are usually a single
enantiomer. That isomer will have an effect on the body whereas its stereoisomer will
not. These drugs would be called stereospecific - only one of the two enantiomers will
react with the body in the desired way.
9. completely synthetic drugs (no natural substances used) are usually racemic mixture
a. sometimes to reduce cost, the mixture is given to the patient (ibuprofen) as
the non active isomer is thought to be inert
b. Thalidomide was marketed as racemic mixture - one isomer relieved morning
sickness and the other inert isomer caused fetal deformities. Racemic
thalidomide is still used for leprosy patients (thalidomide does not have chiral
carbon - but a chiral nitrogen instead)
10. Separation of enantiomers is difficult due to identical chemical properties.
a.Researcher try to produce asymmetric molecules - only one enantiomer.
b. Chiral auxiliaries are used in the process.

1. chiral aux are like optically active catalysts - removed after reaction is
complete
2. chiral aux attaches itself to the nonchiral molecule and forces the
reaction to follow a particular mechanism that results in the production
of a single enantiomer.- then the chiral aux is removed
11. combinatorial chemistry
a. instead of perfoming individual experiments on all possible compounds,
grouping many compounds together and getting multiple reactions and results
is used (combi chem)
creating and testing a large number of chemical for desirable biological properties
b. example - suppose you wanted to synthesize all possible dipeptides of
the 5 amino acids.
1. ordinarily you would do 25 separate experiments
2. combi chem - all 5 acids are reacted simultaneously one of the acids
3. the resultant mixture is tested for activity
a. + result - identify the active dipeptide
b. - result - store the mixture ( in compound library)
c. computers and robots are involved in combi chem
d. solid state chemistry - reactions involving reacting groups
attached to a plastic resin beads
c. the use of animal tests can be restricted to final analysis of chosen drug