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D 1. Pharmaceutical products
D 1.1. List the effects of medicines and drugs on the functioning of the body.
D 1.2. Outline the stages involved in the research, development and testing of new pharmaceutical products.
D 1.3. Describe the different methods of administering drugs.
D 1.4. Discuss the terms therapeutic window, tolerance and side-effects.
Target/aim
Nervous systems and brain; affect both sensory sensations and
mood
Target metabolic processes
Assist bodys ability to fight diseases
disadvantage
Can be destroyed by stomach acid
Slow to have an effect
Can cause stomach bleeding or vomiting
Only small amount of drug is absorbed
Patient needs to be conscious
low effective dose (ED50) and larger lethal dose (LD50) as a result there is a big
difference between effective and lethal dose.
for more common and minor diseases
small difference between effective and lethal dose,
usually because lethal dose is small;
only used for serious conditions
overdose is a high risk.
needs to be taken to achieve the same initial physiological effect with the danger of exceeding the lethal
dose.
Side-effects =
Side-effects are physiological effects which are not intended and therefore undesired (intended =
therapeutic effects); these could be:
beneficial e.g. protect against heart disease like aspirin.
benign e.g. causing drowsiness, nausea constipation.
adverse i.e. causing damage to other organs.
The extent of side effects determines who and when a medicine should be administered. Medicines with
severe side-effects should only be administered by qualified staff in medical emergencies.
Placebo effect
The placebo effect occurs when a person experiences a positive therapeutic (in particular with pain
killers) effect because they believe they have been given a medicine although the substance given is not
a medicine, instead a placebo has been administered; the human body is fooled into healing itself
naturally. Placebo is used as a control to measure the real effectiveness of the drug which is the
difference between the effects experienced by the patients who took the drug and those patients who did
not.
Patients and administrators do not know which patients have taken the placebo.
D 2. Antacids
D 2.1 State and explain how excess acidity in the stomach can be reduced by the use of different bases.
Acid indigestion (discomfort in stomach) and heartburn (acid rising into oesaphagus) are conditions that arise
when excess hydrochloric acid is produced by the gastric glands in the walls of the stomach. The acid, which
creates an acidic environment of pH 0.3 to 1.2, is needed to:
Action of antacids
Antacids are substances (usually weak bases) which are used to neutralize excess hydrochloric acid in the
stomach so the pH level returns to the desired level.
Aluminium hydroxide, magnesium hydroxide, magnesium carbonate and sodium hydrogencarbonate are
commonly used as active ingredients in such antacids as they are weak bases. Aluminium hydroxide is the
most effective as it has 3 OH- per formula unit an can therefore neutralize three times as many H+ than sodium
hydrogen carbonate.
Sodium hydroxide or potassium hydroxide are not used as antacids because they are strong alkalis and are
too corrosive to the body tissue.
Equations
Alginates
Some antacids also contain compounds called alginates which prevent heartburn by
producing a neutralizing layer on top of stomach contents and
preventing acid in the stomach from rising into the oesophagus and causing heartburn (inflammation and
pain).
Anti-foaming agents
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Antacids which use carbonates will also contain anti- foaming agents such as dimethicone which reduce the
bloating of the stomach as a result of the carbon dioxide production.
D 3. Analgesics
D 3.1 Describe and explain the different ways that analgesics prevent pain.
D 3.2 Describe the use of derivatives of salicylic acid as mild analgesics, and compare the advantages and
disadvantages of using aspirin and paracetamol (acetaminophen).
D 3.3 Compare the structures of morphine, codeine and diamorphine (heroin, a semi-synthetic opiate).
D 3.4 Discuss the advantages and disadvantages of using morphine and its derivatives as strong analgesics .
aspirin
phenyl/aromatic benzene
ester
carboxylic acid
paracetamol
phenyl/aromatic benzene
hydroxyl
amide
carbonyl
ibuprofen
phenyl/aromatic benzene
carboxylic acid
Some mild analgesics such as aspirin are derivatives of salicylic acid that was used as an analgesic in
the past but which was unpleasant to take and damaged the membranes in the mouth, gullet and
stomach. The structure of salicylic acid is shown below. A derivative = a new compound obtained from
another compound.
To convert salicylic acid into aspirin the hydrogen atom of
the OH group is replaced by a COCH3 group to form an
ester functional group which makes the compound less
irritating to the stomach and therefore easier to take.
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morphine
benzene ring
hydroxyl (2)
ether;
tertiary amine;
double bond/alkene;
diamorphine/heroin
benzene ring
tertiary amine
alkene
ester (2)
ether
codeine
benzene ring
hydroxyl/alcohol
ether (2)
alkene
tertiary amine
All three compounds are derived from opium which is an extract from poppy seeds. Both codeine and
diamorphine are derived from morphine and are called semi-synthetic opiate. An opiate is any chemical
that has the same physiological effect as morphine.
As the structures above show, heroins structure is only slightly different from morphine. Both the
hydroxyl or alcohol groups in morphine have been replaced with ester groups. This is achieved by
reacting the morphine with ethanoic acid; as a result an esterification occurs during which also water is
produced.
The amine in morphine, diamorphine and codeine is a tertiary amine as the nitrogen atom has three alkyl
groups bonded onto it.
Comparison of aspirin and paracetamol as mild analgesics
analgesic
aspirin
paracetamol
advantage
reduces fever more effectively
antipyretic (=drug which reduces fever)
beneficial side-effects:
o preventing the recurrence of heart
attacks and strokes
o thins the blood
o reduces blood clotting
o also anti-inflammatory reduces
inflammation or swelling
does not irritate stomach wall
suitable for children
allergic reactions rare
can be made in liquid form
disadvantage
ulceration
stomach bleeding due to its acidic
properties
allergic reactions
Reyes syndrome in children (a
potentially fatal liver and brain
disorder) so not suitable for children
can, in rare cases, cause blood
disorders and kidney damage.
easier to overdose and overdosage
can lead to serious liver damage,
brain damage and even death.
not a good anti-inflammatory
advantage
strong analgesics and
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disadvantage
euphoria, lack of self-control even dangerous behaviour
kidney failure.
addiction or physical dependence which leads to withdrawal
symptoms when drug is not taken e.g. restlessness, sweating, fever,
cramping,
tolerance can become an issue with this type of drug as more of the
drug needs to be taken to achieve the same effect; in order to achieve
the desired effect heroin users may take doses which exceed the
lethal dose
Social:
o heroin users are more likely to commit crimes to pay for
gradually increasing doses of the drug
o diversion of energy and money; loss of job
o when administered intravenously can lead to transmission of
dangerous infections e.g. AIDS.
o prostitution
D 4. Depressants
D 4.1 Describe the effects of depressants.
D 4.2 Discuss the social and physiological effects of the use and abuse of ethanol.
D 4.3 Describe and explain the techniques used for the detection of ethanol in the breath, the blood and urine.
D 4.4. Describe the synergistic effects of ethanol with other drugs.
D 4.5. Identify other commonly used depressants and describe their structures.
Depressants are often described as antidepressants (act against depression) because they relieve the
symptoms of (mental) depression by depressing (decreasing the activity of) the central nervous system.
They calm and relax the nervous system as they slow down the action of the brain, heart and other
organs.
Effects of depressants
dose
low
moderate
high
extremely high
effect
may exert little or no effect.
may induce sedation, soothing, reduction of anxiety, relaxes muscles, impaired
judgement, lowers heart rate,
may induce sleep, unconsciousness, slurred speech, altered perception
may cause organ failure, coma or death
Social
increased risk when driving or
operating machinery
involvement in violence or crime
relationship problems
taking time off work as a result of
sickness or death associated with
alcohol abuse
loss of income
hospital costs
lower economical production
cost of medical treatment to society
Physiological
Short term:
reduces tension, anxiety and inhibitions
impairs function of central nervous system
dehydration
high dose can cause vomiting, unconsciousness
Long term:
liver damage/cirrhosis liver disease
increased blood pressure
heart disease or stroke
miscarriage and fetal abnormalities
tolerance and physical dependence
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Ethanol produces a synergic effect with other drugs i.e. their effect is enhanced in the presence of alcohol
which can be dangerous e.g. with aspirin it can increase risk of stomach bleeding. In the case of sleeping
tablets and other sedatives it can cause coma or death.
Techniques used for the detection of alcohol
Using potassium
dichromate
intoximeter
chromatography
Other commonly used depressants prescribed for stress relief: (see table 20 in data booklet)
depressant
Fluoxetine hydrochloride (Prozac)
diazepam/Valium;
nitrazepam/Mogadon;
D 5. Stimulants
D 5.1 List the physiological effects of stimulants.
D 5.2 Compare amphetamines and epinephrine (adrenaline).
D 5.3 Discuss the short- and long-term effects of nicotine consumption.
D 5.4 Describe the effects of caffeine and compare its structure with that of nicotine.
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Stimulants are drugs that act on the central nervous system as they increase the activity of the brain by
increasing the levels of neurotransmitters. They are the opposite to depressants.
Examples of stimulants
Caffeine, nicotine, amphetamines (synthetic drugs e.g. in diet pills). The intention of these drugs is to have
similar effects to adrenaline which is a natural stimulant that is released in times of stress e.g. pain, cold,
fear. The effects of adrenaline are increased heart beat, increased blood pressure, increased blood flow
to brain and muscles, increased air flow to lungs all resulting in an increased alertness to allow the
organism to deal with the stress or fight or flight.
Amphetamines are synthetic drugs that have similar structures to epinephrine/adrenaline and therefore
mimic its effects of which is to stimulate the sympathetic nervous system. They are therefore known as
sympathomimetic drugs.
Physiological effects of stimulants
Short term
Increased brain activity
increased heart rate,
increase breathing rate,
increased alertness and concentration
decreased appetite
shakes
sleeplessness
Long term
increased risk of heart disease
increased blood pressure
coronary thrombosis (blood clots in blood vessels)
stomach ulcers.
tolerance: which leads to increased use as increased
amounts needed to produce same effect; increasing
amounts cause damage/death/overdose/lethal dose
epinephrine
Functional groups:
benzene ring
primary amine
Functional groups:
benzene ring
secondary amine
hydroxyl (3) can form more hydrogen bonds
and is therefore more soluble in water
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stomach ulcers
emphysema
bronchitis
shortage of breath
coughing
bad breath
yellowing of teeth or fingers
adverse effect on pregnancy
addiction to tobacco
reduction in capacity of blood to carry oxygen;
withdrawal symptoms / weight gain (on quitting);
Caffeine
Caffeine is a stimulant. When consumed in large amounts it can cause
anxiety, irritability and sleeplessness. It is a weak diuretic (=causes
increase in urine output).
Its structure is similar to nicotine as shown on the right; in this structure
highlight in blue the functional groups which both nicotine and caffeine
have: benzene ring and tertiary amine (caffeine has three of those) and in
red the group which caffeine has but not nicotine i.e. the amide group. It
could also be considered that caffeine has 2 amide groups circle them in
green.
D 6. Antibacterials
D 6.1 Outline the historical development of penicillins.
D 6.2 Explain how penicillins work and discuss the effects of modifying the side-chain.
D 6.3 Discuss and explain the importance of patient compliance and the effect of penicillin overprescription .
Antibacterials are drugs that kill or inhibit the growth of bacteria that cause infectious diseases. Penicillins
are a group of compounds that are produced by micro-organisms and kill harmful micro-organisms; they
are therefore called antibiotics.
Examples of infectious diseases caused by bacteria: tuberculosis, syphilis, cholera, salmonella,
bronchitis, anthrax, meningitis, gonorrhea, chlamydia.
Historical development of penicillins
Alexander Fleming, Howard Florey and Ernst Chain shared the Nobel Prize for the discovery of penicillin
and its curative effect in various infectious diseases.
Scientist
Alexander Fleming
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Label functional groups A and B and any other functional groups you recognize.
Circle the side chain which is the benzene ring and CH2 to the left of the carbonyl group of the amide.
Penicillins prevent the growth of bacteria. They do this by deactivating (the beta-lactam group does that)
the enzymes in the bacteria that are involved in developing cross-links in the cell wall of bacteria. As a
result the bacterial cell absorbs too much water which causes the cell to burst. Bacteria constantly
replace cell walls.
Administering of penicillins
There are two types of antibiotics:
broad-spectrum antibiotics that are effective against a wide range of bacteria. They are administered
against bacteria that might be or have shown resistance to one or even two (less likely) antibacterials.
Broad-spectrum but can therefore also kill useful bacteria.
narrow-spectrum only attack a limited range of bacteria, usually administered when doctor has
identified type of infectious bacteria after taking samples of blood, urine,
With some diseases, e.g. tuberculosis (TB), it is important to administer a cocktail of different
antibacterials because bacteria that cause TB are usually extremely resistant to penicillins so a mixture of
different antibiotics is used.
Increased resistance in bacteria to antibacterials
As a result of mutations, bacteria have become resistant to penicillins because of their misuse by
patients. Resistant bacteria produce an enzyme, penicillinase, which causes the break up of the penicillin
molecule (the beta lactam ring to break open); these bacteria then reproduce and pass on their
resistance to succeeding generations.
Examples of misuse of antibiotics include:
1. Patient compliance
Refers to patients not completing the full course of antibiotics and this resuts in prolonging the disease as
not all bacteria are killed. By allowing the bacteria to live longer there can be more mutations eventually
producing bacteria with resistance. Patient compliance also allows disease to spread as bacteria are not
all killed.
2. Overprescription of antibacterials
Many doctors are too quick to prescribe antibiotics. Patients should be encouraged to fight an infection
using their own immune system. Problems associated with overprescriptions: allergic reactions by the
patients, the wiping out harmless bacteria in the alimentary canal and destroyed bacteria might be
replaced by more harmful bacteria..
3. Use of antibacterials in animal feedstock
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Some antibiotics are also effective in animals but these antibiotics are sometimes administered without
the animals having any disease. These antibiotics end up in the food chain.
Modifying the side-chain of penicillin G to develop new semi-synthetic penicillins
Modern or semi-synthetic penicillins, such as ampicillin, are penicillin molecules that have been modified
by replacing the side-chain with other atoms or groups of atoms.
For instance, in the case of ampicillin, the side chain now still contains a benzene or C6H5 ring but has a
hydrogen atom and an amine (-NH2) group instead of the CH2 group that was there.
Such modifications to the side-chain bring advantages such as:
Reducing the occurence of penicillin resistant bacteria as the modified penicillins are able to
withstand the action of the enzyme, penicillinase, which is an enzyme produced by penicillin-resistant
bacteria and which causes the break down of penicillin.
Resistance to breakdown or deactivation by stomach acid (so can be taken orally, e.g. ampicillin);
penicillin G had to be administered by injection because it was decomposed by stomach acid.
Produce penicillin that do not cause allergic reactions to some patients.
D 7. Antivirals
D 7.1. State how viruses differ from bacteria.
D 7.2 Describe the different ways in which antiviral drugs work.
D 7.3 Discuss the difficulties associated with solving the AIDS problem.
Examples of diseases caused by viruses: AIDS, influenza, rabies, common cold, small pox, measles,
Difference between bacteria and viruses
Bacteria
bacteria are self-reproducing i.e. by cell division
do not need a host
preventing viruses from entering host cell as it changes the cell membrane of the host cell
preventing the viruses from multiplying in the host cell:
o by blocking enzyme activity within the host cell.
o by altering genetic material in the host cell
preventing the release of viruses after reproduction from the cell
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bacteria can be killed or their actions reduced by simple chemical agents but viruses cannot be killed
and must be targeted on genetic level
different types of bacteria employ similar metabolic processes and thus can be targeted by common
antibacterials whilst each kind of virus usually requires special drugs.
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