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Medicines and Drugs Option D

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Title: Medicines and Drugs Option D


1
Medicines and Drugs Option D
2
D.1 Pharmaceutical products
  • Human body functioning needs defenses
  • 1st line skin, mucous membranes, eye tears, ear
    wax
  • 2nd line white blood cells (wbc), clotting
    mechanisms, inflammatory response
  • 3rd line antibodies, memory cells

3
Inflammatory response
  • Release of histamine
  • Mucous production
  • Fever
  • Blood flow
  • Redness
  • Swelling
  • Pain

4
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5
Therapeutic effects of drugs
  • Alteration of the physiological state
  • Of incoming sensory sensations
  • Of mood or emotions

6
Drugs target
  • Nervous system- analgesics, stimulants,
    depressants and mind-altering drugs
  • Or metabolism like antacids
  • supplement bodies resistance-antibacterials and
    antivirals

7
Placebo
  • Power of suggestion
  • Release opioids
  • 1/3 show improvement

8
Methods of administering drugs
  • Oral
  • Inhalation
  • Dermal
  • Suppositories
  • Eye or ear drops
  • Injection-intramuscular, intravenous(IV),
    subcutaneous

9
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10
effects
  • Therapeutic-intended
  • Side-unintended
  • may be beneficial, benign, or adverse

11
Dosing regimen
  • Amount and frequency
  • Variables-sex, age, weight, diet and environment
  • Interaction with other drugs
  • Only IV drip keeps a constant level in the blood

12
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13
Tolerance
  • Reduced responses
  • Higher doses needed

14
dependence
  • Addiction
  • Will suffer withdrawal symptoms
  • Physical or psychological
  • Can be mild or severe

15
Development of drugs
  • Develop drugs that are more effective and/or have
    less side affects
  • New drugs
  • Much money spent on rich diseases
  • 35 new in 1996 only 22 in 2007
  • 800 million 10-12 years
  • Monitored by FDA

16
Lead compounds
  • Derived from plants or microorganisms
  • Digitalis from foxglove flower
  • Analogues-chemically related
  • Tested on animals

17
Development research on humans
  • 1) 50-100 healthy
  • 2) 200-400 patients
  • 3) 3000 patients ½ with placebos double blind

18
Regulatory review
  • Problem of thalidomide

19
Post-marketing monitoring
  • Establish a database
  • Vioxx withdrawal in 2004
  • 5 billion in lawsuits

20
  • Generic name. Each medicine (drug) has an
    approved name called the generic name. A group of
    medicines that have similar actions often have
    similar sounding generic names. For example,
    penicillin, ampicillin, amoxycillin and
    flucloxacillin are in one group of antibiotics.
  • Brand name. Many medicines also have one or more
    brand names. This is chosen by the company that
    makes it. Several companies may make the same
    medicine, each with their own brand name. The
    name is often chosen to be memorable for
    advertising, or to be easier to say or spell than
    some long generic name! For example, paracetamol
    is a generic name. There are several companies
    that make this with brand names such as Tylenol,
    etc.

21
Functional groups
  • Alkene
  • Alcohol, hydroxyl
  • Ketone
  • Benzene
  • Carboxylic acid
  • Ester
  • Ether
  • Chloro

22
  • Primary, secondary, and tertiary amines
  • Primary, secondary, and tertiary amides
  • Heterocylic ring with N or O in place of C
  • nitro

23
Condensation reactions (byproduct of H2O)
  • Esters
  • amides

24
Development of respiratory drugs Epinephrine
25
  • Epinephrine bronkosol
  • Isuprel terbutaline

26
  • Alupent albuterol
  • levalbuterol

27
  • Do questions 1-3

28
D.2 antacids
  • Solution to excess acidity
  • Stomach pH 1-2 normal
  • Kills bacteria, helps digestion
  • Excess acid causes indegestion, gastric reflux,
    ulcers? (probably bacterial)
  • Basic compounds

29
Types
  • Al(OH)3
  • Mg(OH)2 milk of magnesia faster acting
  • NaHCO3
  • CaCO3 add antifoaming agents like dimethicone to
    carbonates
  • Alginates form rafts on top of stomach to stop
    reflux

30
  • Do question 4

31
D.3 Analgesics
  • Is pain good or bad?
  • A symptom of a
  • Bigger problem
  • Treat the problem

32
Reception of pain
  • Pain receptors
  • Stimulated by prostaglandins (PG) released by
    injured cells
  • PG Mediate the inflammatory response
  • PG effect temperature

33
Blocking pain
34
Mild analgesics
  • NSAIDS
  • Prevent stimulation at the site of pain
  • Stop PG release
  • Non-narcotics (dont involve the brain)

35
Strong analgesics
  • Opiods (related to morphine)
  • Blocks pain signals in the brain
  • Can cause drowsiness (narcotics)
  • Must be monitored

36
Pain triangle
  • 1 mild analgesic
  • 2 weak opiod (codeine or tramadol)
  • 3 strong opiods (morphine fentanyl, or methadone)

37
aspirin
  • Willow bark
  • Bayer made the ester derivative of salicylic acid
    in 1890
  • Most widely used drug in the world

38
benefits
  • Painkiller
  • Fever reducer
  • Anti-inflammatory
  • Reduces ability of blood to clot
  • Prevents heart attacks and strokes

39
Adverse effects
  • Irritation of the stomach
  • GI bleeding (especially with alcohol)
  • Allergies
  • Reyes syndrome in children (liver and brain
    disorder)
  • Can be buffered

40
Tylenol ( acetaminophen or paracetamol)
  • Painkiller
  • Fever reducer
  • Not anti-inflammatory
  • Does not irritate the stomach
  • Rare allergies
  • Can use for children

41
Adverse effects
  • Serious kidney, liver and brain damage

42
Strong analgesics
  • Opium-an extract of poppy seeds
  • codeine, morphine, heroin
  • Side effects constipation, cough suppresant,
    constriction of the pupil of the eye

43
codeine
  • One alcohol and one ether
  • Use on second stage of pain management
  • Cough suppresent

44
morphine
  • 2 OH groups
  • Severe pain management
  • Can be addictive

45
Heroin (diamorphine)
  • Legal in Britain and Belgium
  • More oily (lipid, hydrophobic) so it can cross
    the blood-brain barrier quickly
  • Most abused narcotic
  • Produces euphoric effects
  • Withdrawal problems

46
  • Heroin addict video
  • poppy field

47
Long term use
  • Dulling of pain
  • Less fear and tension
  • Constipation
  • Poor nutrition
  • Quick dependence
  • Increased tolerance
  • Infections from injecting the drug
  • Methadone can reduce the craving

48
  • Video on the brain

49
Natural highsvideo
  • What is your philosophy of life?
  • Original American philosophy
    WESTMINSTER SHORTER CATECHISM
  • Q. 1. What is the chief end of man?A. Mans
    chief end is to glorify God, and to enjoy him
    forever.
  • Are emotions good or bad? Anger, fear, hurt
  • Life is a balance.

50
Natural highs
  • Falling in love.
  • Laughing so hard your face hurts.
  • A hot shower.
  • Getting mail.
  • Taking a drive on a pretty road.
  • Hearing your favorite song on the radio.
  • Lying in bed listening to the rain outside.
  • Hot towels out of the dryer.
  • Finding the sweater you want is on sale for half
    price.
  • Chocolate milkshake. (or vanilla!)
  • A long distance phone call.
  • A bubble bath.
  • Giggling.
  • A good conversation

51
  • The beach.
  • Finding a 20 bill in your coat from last winter.
  • Laughing at yourself.
  • Midnight phone calls that last for hours.
  • Running through sprinklers.
  • Laughing for absolutely no reason at all.
  • Having someone tell you that you're beautiful.
  • Laughing at an inside joke.
  • Friends.
  • Falling in love for the first time.
  • Accidentally overhearing someone say something
    nice about you.
  • Waking up and realizing you still have a few
    hours left to sleep.

52
  • Making new friends or spending time with old
    ones.
  • Playing with a new puppy.
  • Having someone play with your hair.
  • Sweet dreams.
  • Hot chocolate.
  • Road trips with friends.
  • Swinging on swings.
  • Watching a good movie cuddled up on a coach with
    someone you love.
  • Wrapping presents under the Christmas tree while
    eating cookies and drinking eggnog.
  • Song lyrics printed inside your new CD so you can
    sing along without feeling stupid.
  • Going to a really good concert.
  • Riding a bike downhill.

53
  • Do questions 5 and 6

54
D.4 Depressants
  • Act on the central nervous system
  • Alters the concentration or activity of
    neurotransmitters
  • Antidepressants are used to treat people who are
    depressed
  • Increasing dosage tranquilizer (calmness)to
    sedative (sleep induced) to hypnotic (respiratory
    depression or coma)

55
ethanol
  • Usually fermented grapes and grains
  • Relaxes people
  • Disinfectant
  • How important is alcohol consumption to you?

56
Short term effects
  • Loss of self-restraint, memory, concentration,
    balance, judgment
  • Violent behavior (domestic abuse)
  • Risk taking causing accidents
  • Dehydration leading to hangovers
  • Vomiting
  • Loss of consciousness

57
Long term effects
  • Dependence
  • Liver disease
  • Heart disease
  • High blood pressure
  • Fetal alcohol syndrome
  • Brain damage (10,000 cells lost per shot of
    whiskey)
  • child abuse
  • DWI (accidents)

58
Effects of alcohol
59
Metabolism of ETOH
  • Readily soluble in water
  • Also in lipids
  • Crosses cell membranes quickly
  • Detoxified by the liver
  • easily passed on through the placenta and breast
    milk

60
Synergism-enhance other drugs
  • Aspirin-increased stomach bleeding
  • Depressants-heavier sedation
  • Tobacco-increase of cancer, heart disease
  • Interfere with other drugs to decrease the
    detoxifying power of the liver- greater and
    longer effects

61
Ethanol detection
  • 80 mg/100cm3 or .08 upper limit for driving

62
breath
  • Breathalyser-potassium dichromate
  • Cr6 orange to Cr3 green
  • Not accurate
  • Intoximeter-gives an absorption band of OH at
    2950 nm in spectrosopy
  • Fuel cell

63
Blood or urine
  • Gas-liquid chromatography
  • Most specific

64
Other depressants
  • Benzodiazepines-affect part of the brain that
    control emotions
  • Treats anxiety, lack of sleep, muscle relaxants
  • Valium (diazepam) and mogadon (nitrozepam)
  • Benzene rings and 7 member ring with C and N

65
Valium vs. mogadan
  • Name 3 structural features these molecules have
    in common and 1 difference

66
Prozac-an antidepressant
  • Fluoxetine hydrochloride
  • Increases the level of serotonin in the brain so
    is an anti-depressant
  • Racemic mixture

67
Depressant therapy
  • Refuse to think negative thoughts
  • Name ten things about your family that you
    appreciate
  • List ten things you are thankful for
  • Tell a friend how much you appreciate them
  • What natural high do you need?

68
  • Do questions 7-10

69
D.5 Stimulants
  • Based upon adrenaline
  • Opposite of depressants
  • Relax the muscles of air passages
  • Reduce appetites
  • May cause heart to beat harder and faster
  • Can cause restlessness

70
Amphetamines
  • Adrenalin (epinephrine) fight or flight increases
    heart rate, blood pressure, blood flow to brain
    and muscles away from the skin, air flow to the
    lungs, mental awareness
  • Similar to noradrenalin-neural transmitter
  • Adrenaline amphetamine

71
comparison
  • Difference primary vs. secondary amine
  • Derivatives of phenyl-ethyl-amines
  • Increases mental alertness and energy
  • Side effect- pupil dilation, decreased appetite,
    dizziness
  • Long term- dependence, depression, infections
  • Adderall, Vyvanse and Dexedrine
  • Illegal-methampthetamine ie speed, crystal meth,
    ectasy

72
  • Video
  • Another one

73
nicotine
  • Found in tobacco plants
  • Used as an insecticide and herbivore
  • Heterocylic ring and tertiary amine
  • Lipid soluble so crosses the blood brain barrier
    easily
  • Highly addictive

74
Short term effects
  • Increases concentration
  • Relieves tension
  • Counters fatigue
  • Increases heart rate and blood pressure
  • Decreases urine output
  • Poisonous chemicals in cigarettes
  • Second hand smoke

75
Long term
  • High blood pressure
  • Risk of heart disease
  • Blood clots in the heart arteries
  • Thickening or hardening of the arteries
  • Ulcers in the stomach
  • 5 million deaths a year in the world
    2nd most cause(1 out of 10)

76
Withdrawal symptoms
  • Nausea
  • Weight gain
  • Drowsiness
  • Depression
  • Lack of concentration

77
smoking
  • Tar
  • CO
  • Lung diseases
  • 19 known chemical carcinogens

78
caffeine
  • In coffee, tea, chocolate, colas
  • 90 of adults consume caffeine daily
  • Respiratory stimulant
  • Compare structure to nicotine
  • Heterocylic ring and tertiary amine

79
effects
  • Increase alertness concentration
  • Increase urine output
  • More than 4 cups of coffee sleeplessness,
    anxiety, irritability
  • Addictive
  • Helps alleviate headaches

80
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81
  • Do question 11 and 12

82
D.6 antibacterials
  • Antibiotics
  • First one was penicillin discovered by Alexander
    Fleming (1928) when mould killed bacteria
  • Serendipity
  • Isolated in 1940
  • First used in 1941 in World War II

83
  • Penicillin G from bread mold
  • 4 membered ring beta-lactam
  • Cell walls cannot form causing bacteria to burst
  • Must be injected
  • Modify the R so it can be injested

84
Antibiotic resistance
  • Resistant bacteria produce penicillinase
  • Superbugs
  • MRSA in hospitals
  • over prescribed especially if infection is viral
  • Animals get 55 of all antibiotics which then
    shows up in food

85
Overcome antibiotic resistance by
  • Develop different forms
  • Restrict use
  • Encourage doctors to not overprescribe
  • Complete the full course of the prescription
  • Do question 13

86
D.7 Antivirals
  • Nature of viruses-cant exist outside of a host
  • No cellular structure
  • Use the host to reproduce

87
T4 Bacteriophage
88
HIV virus
89
H1N1 virus
90
Treatments for viral infections
  • No cell wall so antibiotics dont work
  • Multiply quickly
  • Mutate rapidly
  • Vaccines
  • Amantadine (pentamadine)-prevents entry into the
    cell (prophylactic)
  • Prevent the virus from using the cell to multiply
  • Stop enzyme activity within the host cell

91
  • acyclovir similar to DNA,Tricks the virus to try
    to replicate with it
  • Amantadine (pentamadine)-keeps virus from
    entering the cell

92
AIDS-HIV
  • Failure of the immune system
  • 40 million current infections
  • Africa 1/3 of a country
  • Attacks T white blood cells
  • Retro (RNA) virus

93
HIV therapy
  • Transmitted by sexual encounters, blood, sharing
    of needles
  • Antiretroviral drugs delay the progress ( very
    expensive)
  • Treat concurrent infections

94
  • Do question 14

95
D.8 Drug action
  • Stereoisomerism
  • Geometric
  • Cis-platin
  • Binds to quinine bases tying them up and
    preventing transcription

96
Optical isomerism
  • Chiral drugs react the same until there is a
    chiral environment like enzymes
  • One enantiomer in biological synthesis
  • -like morphine in poppy seeds
  • Synthetic produces racemic mixtures
  • R-Thalidomide alleviates morning sickness in
    pregnant women, L-Thalidomide causes deformities
    in the limbs of the fetus.

97
Thalidomide R then L
98
Ring strain in penicillin
  • The high reactivity of the amide group within the
    four-membered ring structure is a result of
    strain. The ring opens so that the penicillin
    becomes covalently bonded to the enzyme that
    synthesizes bacterial cell walls, thus blocking
    its action.
  • Why doesnt penicillin work on viruses?

99
Solubility and uptake
  • The polar hydroxyl groups in morphine are
    replaced by non-polar ester groups, facilitating
    transport into the non-polar environment of the
    central nervous system.
  • Brain is hydrophobic
  • Only L-morphine is effective

100
  • Internet Friedman_Talkon drug action.pdf
  • Do questions 15 and 16

101
D.9 Drug design
  • Bind to a biological molecule i.e. enzyme,
    receptor, or DNA
  • Interrupts activity
  • Traditional- trial and error starting with a
    natural remedy

102
Rational drug design
  • Attacking the target molecule
  • Finding a lead compound
  • Compound libraries details of molecules
    activities

103
Combinational synthesis
  • Make large numbers of similar drugs in a short
    time
  • Screen for desired activity
  • Occur on insoluble resin beads (solid-phase
    chemistry)
  • Produces a mixture with a large library
  • Need to separate the mixture in the end

104
  • Combinatorial Chemistry A Strategy for the Future

105
Parallel synthesis
  • Single product in each reaction vessel

106
High-throughput screening (HTS)
  • Robotics and micro scale chemistry
  • Reactions of compounds with target molecules
    using colored changes
  • Common biochemicals in the wells

107
Computer-aided design (CAD)
  • Molecular modeling software

108
Modification for absorption
  • Bioavailability 20-49
  • What of the drug gets into the blood stream
  • More polar or ionic have higher
  • COOH group with NaOH to COO- Na
  • NH with HCl to NH2Cl-

109
Aspirin
110
Prozac
111
Asymmetric synthesis
  • Synthesis a single enantiomer
  • Chiral auxiliary

112
taxol
113
Taxol again
114
  • Do question 17

115
D.10 Mind altering drugs
  • Serotonin-neurotransmitter

116
Hallucinogens
  • Alters perception of reality
  • LSD non polar molecule
  • Indole ring
  • Synthesized from ergot a fungus of rye
  • 12 hour effect hallucinogenic blocks the action
    of serotonin

117
Mescalinenot as solublefrom flowers of the
peyote cactus1000 times less potent than LSD6
hours
118
Magic mushrooms Psilocybinleast soluble more
ionicnotice the indole ring-benzene attached to
a 5 member ring with at least one N and a
119
marijuana
  • From the hemp plant cannabis
  • Marijuana or hashish(resin from the plant)
  • Major component is tetrahydrocannabinol (THC)

120
effects
  • Smoked or chewed
  • Depresses the central nervous system
  • Causes mental relaxation and euphoria
  • 15 minutes to 4 hours
  • Relaxation, increased auditory and visual
    perception, loss of sense of time, confusion

121
Long term
  • apathy, lethargy, smoking effects
  • Withdrawal-insomnia, anxiety, and restlessness

122
Legalization of THC
  • Most used illegal drug
  • 147 million users 2.5 of world
  • Against-dependence, lack of responsibility Costs
    of dependence, lends to harder drugs
  • For-not more harmful than tobacco and alcohol,
    take away illegal operators
  • Therapeutic effects-relief from nausea and
    vomiting in cancer therapy, glaucoma, asthma,
    convulsive disorders

123
review
  • Do questions 18 and 19
  • Do the review questions on page 130 of your study
    guide
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