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Percentage yield for Aspirin
        Synthesis
Describe the different methods of
getting a drug into the human body
 and reasons why each method is
               chosen
   (include 3 types of parenteral
           administration)
Syllabus References
• D1.4 Side effects, therapeutic window,
  tolerance.
Side Effects
• Depends on the medicines intended use, e.g.
  morhpine…..
Tolerance
• With constant use over time need more of the
  drug to produce the same physiological effect.
LD50 / ED50
• Measure of safety
• If ED is small and LD is large then a wide
  therapeutic window exists.
Dependence
• Physical
  – Users body can only function normally with the
    drug


• Psychological
  – Intensifies craving for a drug.


• The above are both forms of drug addiction.
Syllabus Reference
• D2 Antacids – state and explain how acidity in
  the stomach cab be reduced by the use of
  different bases.
Placebo
• Where an inert substance produces a
  significant reaction purely on the belief of the
  individual.
Common Antacid Remedies
•   Magnesium Oxide
•   Magnesium Hydroxide
•   Aluminium Hydroxide
•   Calcium Carbonate
•   Sodium Hydrogen Carbonate
•   Magnesium Trisilicate

• 1. Stomach acid is HCl – write balanced chemical
  equations for the rxn of HCl with the above.
• 2. Which is a better buy ? Sodium Bicarbonate or
  Calcium Carbonate – explain using 1g of each.
Antacid – other ingredients
• Dimethicone – anti-foaming agents

• Alginates – protective neutralising ‘raft’

• http://www.gaviscon.co.uk/how_does_gavisc
  on_work/double_action.php
Analgesics

• Mild




• Strong
Mild Analgesics
• Mild analgesics function by intercepting the
  pain stimulus at the source, often by
  interfering with the production of substances
  (for example,prostaglandins) that cause pain,
  swelling or fever.
Strong Analgesics
• Strong analgesics work by temporarily
  bonding to receptor sites in the brain,
  preventing the transmission of pain impulses
  without depressing the central nervous
  system.
Show me a picture ….
(MILD) Aspirin vsParacetamol
• Create one side of A4 which must include :-
  – Full structural formulae
  – Identification of and designation of all functional
    groups
  – Elucidate all bond angles with a single example of
    each different value.
  – Advantages and disadvantages of both, including but
    not limited to; Reye’s syndrome, ulceration, stomach
    bleeding, allergic reactions, blood disorders,
    overdosage, kidney problems.
  – Mechanism of action
Morphine cfDiamorphine (Heroin)
Social Costs…….
• http://www.youtube.com/watch?v=-
  5GIonSHa8c

• http://www.youtube.com/watch?feature=end
  screen&NR=1&v=TWfRBbRrj2w
Structures / Solubility / Bonding
Advantages and Disadvantages of
           Using Opiates
• Short Term - sedation, stupor, relief from pain,
  euphoria, impaired functioning, reduced tension,
  worry and fear – occasional OD.

• Long term – malnutrition, constipation, risk of
  AIDS due to shared needles, withdrawal, loss of
  job, crime, sterility.

• Tolerance and dependence are both major factors
  in opiate addiction.
Depressants
• At low doses a depressant may exert little or
  no effect. At moderate doses the compound
  may induce sedation (soothing, reduction of
  anxiety).
• At higher doses it may induce sleep. At
  extremely high doses it may cause death.
  Depressants are often described as
  antidepressants because they relieve
  depression.
Types of Depressants
• Tranquilisers – slow down body and brain, include
  ethanol and valium. Produce sleep, relieve
  anxiety and tension.

• Sedatives – may be considered as strong
  tranquilisers – sooth distress.


• Hypnotics – produce sleep, e.g. chloral hydrate.
Oxidation of alcohols
• Set up oxidation of alcohols practical
Ethanol – complete for homework
• Name two routes by which this drug can be
  synthesised.
• List some of the short and long term effects of alcohol
  use / abuse.
• Illustrate how this can be chemically changed from the
  primary alcohol to aldehyde and carboxylic acid,
  include conditions, and reagents.
• How does the breathalyser work ?
• How does blood and urine analysis determine alcohol
  content in a person ?
• Explain synergistic effect with Aspirin.
http://www.youtube.com/watch?v=3-9wyHtN9n4
Starter
• Write the reduction and oxidation half ion
  equations for ethanol / dichromate.

•   HL: What is hybridisation in ethanol ?
•   How many lone pairs ?
•   What are the bond angles ?
•   Name a nucleophile that would replace the
    alcohol group, include curly arrow
    mechanism.
Stimulants D5
• What is a stimulant ?

• Amphetamines, nicotine and caffeine are al
  examples.

• They stimulate the CNS increasing wakefulness,
  often accompanied by a decrease in appetite.
• Constrict arteries, increase sweat production,
  increase heart rate, blood pressure, respiration,
  then fatigue, irritability, depression.
Adrenalin
Amphetamine
PEAs
XTC
What do PEAs DO ?
• They are sympathomimetic – their actions
  mimic the bodies natural stimulant –
  adrenalin.

• Medical uses; treats mild depression,
  narcolepsy, and asthma,

• http://www.youtube.com/watch?v=qyXFN4oc
  N_o
D5.3 Nicotine

• Mild stimulant, followed by depression which
  encourages frequent use.

• ST Effects; increases heart rate, and blood pressure, so
  stresses the heart, diuretic.

• LT Effects; heart disease, thrombosis, excess stomach
  acid, ulcers, cancers of the larynx, emphysema, and
  fires !!
• HIGHLY ADDICTIVE !!! Psychological and physiological.
• http://www.youtube.com/watch?v=x4c_wI6kQyE
Caffeine, Nicotine
Effects of Caffeine
• Caffeine; increases cellular metabolism,
  stimulates CNS, increases alertness, energy,
  motivation and concentration. Diuretic. No
  physical addiction, mild psychological.

• Weak diuretic.
D6 Antibacterials
• Research the role of Florey, Chain and Fleming
  in the serendipitous discovery of penicillin.

• Produce a one piece info sheet on the
  discovery, production and impact on the
  world.
Antibac Essentials
Viruses vs Bacteria
• TB, typhoid, syphillis, gonnorhea, fever



• Note: Viruses are different and include;
  influenza, the common cold, hepatitis,
  measles and AIDS.
Action of Antibacterials
• Fleming – found an open petri dish with
  mould in it – no bacterium  YEY

• Subsequently Florey and Chain scaled this up
  to an industrial process.

• Saved thousands of lives in the closing years of
  WW2.
Penicillin Structure
Notes
• Penicillin is deactivated by stomach acid so is
  injected.
• The side chain has been modified to
  counteract this.
• Some bacteria have evolved to deactivate the
  bacterium.
Penicillin Mode of Action
• Penicillin is incorporated into the cell wall of
  the bacterium.
• Ring strain causes the molecule to break and
  create holes in the cell wall.
• Water enters by osmosis, the cell wall
  expands, bursts, and the bacterium dies.

• http://www.youtube.com/watch?v=vK3nxfKM
  4Q4
Broad and Narrow Spectrum Antibacs
• Broad – a wide variety of bacteria – the
  tetracyclines – from soil fungi
   – Prolblematic as kill all bacteria


• Narrow – only a small number ( sometimes
  only one ) – this is the majority of penicillins
Over Prescription
• Safe for MOST people ( 10% allergic ) – shock
  and death
• Can kill good bacteria – allowing bad bacteria
  to proliferate
• Genetic resistance – typhoid, TB, gonnorhea
  have all evolved resistance
• Mutated strains – no treatment
• Animal feedstocks – encourages drug
  resistance
D7 Antivirals
• Submicroscopic, non cellular, parasitic, no
  nucleus, much smaller than bacteria.

• Note : an antibiotic may have antiviral properties

• Most viruses are controlled by inoculations –
  polio, smallpox, yellow fever, influenza.
• UN Smallpox vaccination programme has
  eradicated this virus.
How do Antivirals Work ?
• http://www.youtube.com/watch?v=HhhRQ4t9
  5OI

• Research focusses on blocking the viral
  enzyme activity within the host cell.

• Acyclovir and Zovirax are common antivirals.
AIDS
• Viruses can cross species, mutating as they go.
• HIV contains RNA not DNA.
• Specific proteins on the surface of HIV bind to
  CD4 receptors on white blood cells. These are
  the bodies immune system.
• HIV mutates, and control is difficult due to the
  high price of anti retro viral drugs.

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G12 medicinesanddrugs

  • 1. Percentage yield for Aspirin Synthesis
  • 2. Describe the different methods of getting a drug into the human body and reasons why each method is chosen (include 3 types of parenteral administration)
  • 3. Syllabus References • D1.4 Side effects, therapeutic window, tolerance.
  • 4. Side Effects • Depends on the medicines intended use, e.g. morhpine…..
  • 5. Tolerance • With constant use over time need more of the drug to produce the same physiological effect.
  • 6. LD50 / ED50 • Measure of safety • If ED is small and LD is large then a wide therapeutic window exists.
  • 7. Dependence • Physical – Users body can only function normally with the drug • Psychological – Intensifies craving for a drug. • The above are both forms of drug addiction.
  • 8. Syllabus Reference • D2 Antacids – state and explain how acidity in the stomach cab be reduced by the use of different bases.
  • 9. Placebo • Where an inert substance produces a significant reaction purely on the belief of the individual.
  • 10. Common Antacid Remedies • Magnesium Oxide • Magnesium Hydroxide • Aluminium Hydroxide • Calcium Carbonate • Sodium Hydrogen Carbonate • Magnesium Trisilicate • 1. Stomach acid is HCl – write balanced chemical equations for the rxn of HCl with the above. • 2. Which is a better buy ? Sodium Bicarbonate or Calcium Carbonate – explain using 1g of each.
  • 11. Antacid – other ingredients • Dimethicone – anti-foaming agents • Alginates – protective neutralising ‘raft’ • http://www.gaviscon.co.uk/how_does_gavisc on_work/double_action.php
  • 13. Mild Analgesics • Mild analgesics function by intercepting the pain stimulus at the source, often by interfering with the production of substances (for example,prostaglandins) that cause pain, swelling or fever.
  • 14. Strong Analgesics • Strong analgesics work by temporarily bonding to receptor sites in the brain, preventing the transmission of pain impulses without depressing the central nervous system.
  • 15. Show me a picture ….
  • 16. (MILD) Aspirin vsParacetamol • Create one side of A4 which must include :- – Full structural formulae – Identification of and designation of all functional groups – Elucidate all bond angles with a single example of each different value. – Advantages and disadvantages of both, including but not limited to; Reye’s syndrome, ulceration, stomach bleeding, allergic reactions, blood disorders, overdosage, kidney problems. – Mechanism of action
  • 18. Social Costs……. • http://www.youtube.com/watch?v=- 5GIonSHa8c • http://www.youtube.com/watch?feature=end screen&NR=1&v=TWfRBbRrj2w
  • 20. Advantages and Disadvantages of Using Opiates • Short Term - sedation, stupor, relief from pain, euphoria, impaired functioning, reduced tension, worry and fear – occasional OD. • Long term – malnutrition, constipation, risk of AIDS due to shared needles, withdrawal, loss of job, crime, sterility. • Tolerance and dependence are both major factors in opiate addiction.
  • 21. Depressants • At low doses a depressant may exert little or no effect. At moderate doses the compound may induce sedation (soothing, reduction of anxiety). • At higher doses it may induce sleep. At extremely high doses it may cause death. Depressants are often described as antidepressants because they relieve depression.
  • 22. Types of Depressants • Tranquilisers – slow down body and brain, include ethanol and valium. Produce sleep, relieve anxiety and tension. • Sedatives – may be considered as strong tranquilisers – sooth distress. • Hypnotics – produce sleep, e.g. chloral hydrate.
  • 23.
  • 24. Oxidation of alcohols • Set up oxidation of alcohols practical
  • 25. Ethanol – complete for homework • Name two routes by which this drug can be synthesised. • List some of the short and long term effects of alcohol use / abuse. • Illustrate how this can be chemically changed from the primary alcohol to aldehyde and carboxylic acid, include conditions, and reagents. • How does the breathalyser work ? • How does blood and urine analysis determine alcohol content in a person ? • Explain synergistic effect with Aspirin.
  • 27. Starter • Write the reduction and oxidation half ion equations for ethanol / dichromate. • HL: What is hybridisation in ethanol ? • How many lone pairs ? • What are the bond angles ? • Name a nucleophile that would replace the alcohol group, include curly arrow mechanism.
  • 28. Stimulants D5 • What is a stimulant ? • Amphetamines, nicotine and caffeine are al examples. • They stimulate the CNS increasing wakefulness, often accompanied by a decrease in appetite. • Constrict arteries, increase sweat production, increase heart rate, blood pressure, respiration, then fatigue, irritability, depression.
  • 31. PEAs
  • 32. XTC
  • 33. What do PEAs DO ? • They are sympathomimetic – their actions mimic the bodies natural stimulant – adrenalin. • Medical uses; treats mild depression, narcolepsy, and asthma, • http://www.youtube.com/watch?v=qyXFN4oc N_o
  • 34. D5.3 Nicotine • Mild stimulant, followed by depression which encourages frequent use. • ST Effects; increases heart rate, and blood pressure, so stresses the heart, diuretic. • LT Effects; heart disease, thrombosis, excess stomach acid, ulcers, cancers of the larynx, emphysema, and fires !! • HIGHLY ADDICTIVE !!! Psychological and physiological. • http://www.youtube.com/watch?v=x4c_wI6kQyE
  • 36. Effects of Caffeine • Caffeine; increases cellular metabolism, stimulates CNS, increases alertness, energy, motivation and concentration. Diuretic. No physical addiction, mild psychological. • Weak diuretic.
  • 37. D6 Antibacterials • Research the role of Florey, Chain and Fleming in the serendipitous discovery of penicillin. • Produce a one piece info sheet on the discovery, production and impact on the world.
  • 39. Viruses vs Bacteria • TB, typhoid, syphillis, gonnorhea, fever • Note: Viruses are different and include; influenza, the common cold, hepatitis, measles and AIDS.
  • 40. Action of Antibacterials • Fleming – found an open petri dish with mould in it – no bacterium  YEY • Subsequently Florey and Chain scaled this up to an industrial process. • Saved thousands of lives in the closing years of WW2.
  • 42. Notes • Penicillin is deactivated by stomach acid so is injected. • The side chain has been modified to counteract this. • Some bacteria have evolved to deactivate the bacterium.
  • 43. Penicillin Mode of Action • Penicillin is incorporated into the cell wall of the bacterium. • Ring strain causes the molecule to break and create holes in the cell wall. • Water enters by osmosis, the cell wall expands, bursts, and the bacterium dies. • http://www.youtube.com/watch?v=vK3nxfKM 4Q4
  • 44. Broad and Narrow Spectrum Antibacs • Broad – a wide variety of bacteria – the tetracyclines – from soil fungi – Prolblematic as kill all bacteria • Narrow – only a small number ( sometimes only one ) – this is the majority of penicillins
  • 45. Over Prescription • Safe for MOST people ( 10% allergic ) – shock and death • Can kill good bacteria – allowing bad bacteria to proliferate • Genetic resistance – typhoid, TB, gonnorhea have all evolved resistance • Mutated strains – no treatment • Animal feedstocks – encourages drug resistance
  • 46. D7 Antivirals • Submicroscopic, non cellular, parasitic, no nucleus, much smaller than bacteria. • Note : an antibiotic may have antiviral properties • Most viruses are controlled by inoculations – polio, smallpox, yellow fever, influenza. • UN Smallpox vaccination programme has eradicated this virus.
  • 47. How do Antivirals Work ? • http://www.youtube.com/watch?v=HhhRQ4t9 5OI • Research focusses on blocking the viral enzyme activity within the host cell. • Acyclovir and Zovirax are common antivirals.
  • 48. AIDS • Viruses can cross species, mutating as they go. • HIV contains RNA not DNA. • Specific proteins on the surface of HIV bind to CD4 receptors on white blood cells. These are the bodies immune system. • HIV mutates, and control is difficult due to the high price of anti retro viral drugs.