Chapter 21- Medicines and Drugs:
Chemicals and the Mind
Height and width measure the same
length. The “reality” sometimes
depends on just how we view the
world.
Chemicals, including drugs and
medicines - can affect our views of
reality and our actions.
Hallucinations - remove us from contact
with reality in other ways.
Placebo effect - how a specific chemical
influence our bodies to that chemical.
Double-bind experiment - technique
that allows us to learn whether the action
of any particular medication results from
direct chemical influence.
Aspirin - the leading commercial pain
reliever, results from the dehydration of
acetic acid through the removal of one
water molecule from two molecules of the
acid (initial synthesis in 1853)
-common name of trade name
acetylsalicylic acid
-an analgesic, an antipyretic, an anti-
inflammatory medication
-treatment of rheumatoid arthritis, strokes
and heart attacks
Analgesic - a substance that reduces or
eliminates pain
Antipyretic - a substance that lowers or
eliminates fever.
Anti-inflammatory agent - a substance
that reduces or eliminates inflammation.
Hippocrates - ancient Greek healer
known as Father of Medicine
Salicylates - yielded from its active
agent, salicin, in 1827 willow bark.
-comes from the Latin term of willow
salix, which gives us the name of an
entire family compouns, salicylates
-also the term for botanical genus of the
tree itself, salix
Salicylic acid - relieves pain, fever and
inflammation
Spiraeic acid - derived from the
botanical genus of the meadowsweet
Aspirin - coined by adding an “a” (for
acetylated”)
Methyl salicylate - fragrant methyl ester
of salicylic acid, known as oil of
wintergreen
-flavoring for candy, chewing gums,
medicines.
-active ingredient of liniments used for
relieving the pain of aching muscles and
joints
The irritant action of the methyl
acetate stimulate blood flow into the
deeper regions, adding to its
analgesic effect.
Felix Hofmann - a chemist working for
Baeyer firm in Germany
-started aspirin on its road to success
“Extra strength” aspirin - contains
500mg of acetylsalicylic acid per tablet
The higher the pH, the faster the tablet
breaks up and faster the
acetylsalicylic acid gets in to the
blood.
“Buffered” aspirin - combination of
acetylsalicylic acid and one or more
bases (salt). The combination
accelerates the disintegration of the
tablet.
-e.g. magnesium hydroxide and
aluminum hydroxide
The beneficial effects of aspirin and
other salicylates come from their
ability to prevent the formation of
prostaglandins.
Risks of taking aspirin:
-upset stomach
-allergic reactions
-its effect on the blood’s ability to clot
-prevents the formation of platelets
-causes excessive bleeding
-Reye’s syndrome- a rare and fatal
reaction accompanied by confusion,
irritability, nausea, lethargy
-toxic (has the LD50 of 1.5kg)
Acetaminophen - substitute for aspirin,
active ingredient of Tylenol and Datril
-least toxic member of a class of
analgesic and antipyretic
Acetanilde - alleviate fever as early as
1886
Phenacetin - also called
acetophenetidin, first used as analgesic
then banned by U.S. Food and Drugs
because of its tendency to damage the
kidneys and produce blood disorders
when used excessively
Ibuprofen - prescription drug
-for pain, inflammation and fever
Drugs and medications - chemicals
used medically for treating diseases and
injuries.
Drugs - carries the connotation of
narcotics, addiction and crime.
-bears an uncertain ancestry
Medicine - came into the English
language through French, from the Latin
medicina meaning medication, practice of
the physician or place where the
physician works.
Narcotic - substance that produces
stupefying, dulling effect and that induces
sleep
-comes from the Greek narkotikos,
meaning “numbling” or “stupefying”
Opium - the dried sap of the puppy,
contains several narcotic compounds
-familiar among Sumerians
Thomas Sydenham - the 17th century
English physician known as “English
Hippocrates”, wrote of the substance’s
power to ease pain.
Alkaloids - basic, bitter-tasting, nitrogen
containing compounds that are found in
plants and that produce physiological
reactions of various kinds and intensity
Morphine - major alkaloid of opium
-powerful narcotic, a cough suppressant
Friedrich Serturner - German
pharmacist who obtained morphine in
pure form and named it for Morpheus.
Codeine - another opium alkaloid
-less potent analgesic than morphine
-one of the most powerful cough
suppressant
Pierre-Jean Robiquet Codeine - the
French pharmacist who isolated codeine
in 1832
Papaverine - discovered in 1848, found
in plant extracts
-useful for relaxing the smooth muscles
and for dilating or enlarging blood
vessels
Two important characteristics:
1. They are all addicting.
2. They are all among the most powerful
constipating agents known, with
substantial value in controlling diarrhea.
The medical value of morphine in
vanquishing pain is counterbalanced
by its great capacity to produce
addiction.
Heroin - diacetylmorphine, morphine in
which two -OH functional groups have
been converted to ester functional
groups.
-because of the size of effective doses
were so low, it first gave the promise of
being nonaddictive
-proved to be one of the most addictive
drugs known
-one if its by-product is acetic acid, major
organic component of vinegar
Cocaine - produced by South American
coca bush, alkaloid caine
-resembles morphine in the case it’s used
as local anesthetic and in its ability to
produce a fast and powerful addiction
-produces euphoria - a great sense of
well-being, delusions of immense power
all followed by a depression
-reacts with hydrochloric acid to form
salts (cocaine hydrochloride)
Sigmund Freud - founder of
psychoanalysis, one of the first to
recognize the effects of cocaine.
Karl Koller - broke his morphine habit at
the cost of being addicted to cocaine
instead.
-discovered cocaine’s use as local
anesthetic during experimentation
Belladonna - favorite posion in the
intrigues of the Middle Ages
-comes from the combination of Italian
words bella and donna “beautiful lady”
Atropine - the major alkaloid of the plant,
active ingredient of belladonna
Scopolamine - dilutes pupils, a powerful
sedative
-used to induce “twilight sleep” to ease
child-birth.
Caffeine - an alkaloid that occurs in
coffee beans
-stimulates the central nervous system
and heightens a sense of awareness
-lethal dose for adults: 10g
-LD50 : 0.13g/kg
Nicotine - lethal substance used as a
powerful agricultural insecticide
-poisonous alkaloid that occurs in
tobacco leaves
-LD50 : 0.23g/kg
The products of nature must
necessarily be good, or at least far
less harmful than what we humans
manufacture with our intellects and
our skills in laboratories and factories.
Whether the drug is legal and sanctioned
by society or illegal depends on the
outlook of that particular society, at that
particular time in history.
Marijuana - whose major, active
component is tetrahydrocannabinol or
THC, has also been the subject of mixed
signals.
-controls glaucoma, a disease of the
eyes
Synthetic narcotics
-levorphanol: strongest resemblance to
morphine
-meripidine: most widely used synthetic
narcotic
-oxymorphone most powerful:
-propoxyphene and oxycodone:
combined with aspirin
Methadone - as its hydrochloride salt,
both an analgesic and and useful
treatment for heroin addiction
Three molecular regions of synthetic
anesthetics:
1. An aromatic ring, usually substituted at
one end of the molecule;
2. A substituted nitrogen at the other; and
3. A section, normally containing an
amide or an ester group, connecting the
two.
Procaine - the oldest local anesthetic
Vasoconstrictor - drug that consists
blood vessels.
Lidocaine - patented in United States
and used as Xylocaine
-stronger anesthetic than procaine
Mescaline - forms mescal bottoms at the
top of the peryote cactus
LSD - “intense kaleidoscopic play of
colors”
Amphetamines - powerful stimulants
that raise the pulse rate and blood
pressure
Lithium carbonate - provides stability to
the mood swings of manic depression, a
condition that produces the extremes of
raging exhilaration and intense paralyzing
condition
Reserpine - major rauwolfia alkaloid
produced by rawolfia scrubs
-treats mental illness
-registered as carcinogen by
Environmental Protection Agency
Tranquilizers:
-diazepam (Valium)
-flurazepam (Dalmane)
-oxazepam (Serax)
-clorazepate (Tranxene)
-chlordiazepoxide (Librium)
Opitate antagonists - compounds that
counteract or nullify the effects of opiates,
including heroin
Opiate receptors - extremely large
molecules within the nervous system.
When narcotic molecules interact with
opiate receptors, they block or alter
signals following the nervous system.
Endorphins - opiates produced within
the bodies of animals
-combination of two words: endongenous
(meaning “formed within the body”) and
morphins (the kinds of narcotics they
mimic)
Pituatary gland - a small, round gland
that hangs down from the base of the
brain, roughly at the center of the head
Pentapeptides - molecular keys of the
animal kingdom
-which their discoverers named
enkephalins from Greek words meaning
“within the head”
Structures of two enkephalins:
-methionine enkephalin
-leucine enkephalin
Placebo - a harmless and normally
ineffective substance given to someone
who complains of a particular ailment,
simply to please and pacify the patient.
-from Latin meaning “I shall please” or “I
shall pacify”
The five amino acids of methionine
enkephalin
-Tyr: Tyrosine
-Gly: Glycine
-Gly: Glycine
-Phe: Phenylalanine
-Met: Methionine
Double-blind study - powerful scientific
technique that operates a simple test of
reality.