IB Chemistry SL Option D: Medicine and Drugs – Flashcards
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Drug
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any substance by its chemical nature, has an influence on the physical/mental functions of the body
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Medicine
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a drug that leads to an improvement of health
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Effect of drugs/medicines
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Alters the physiological state, including consciousness, activity level or coordination Alters incoming sensory sensations Alters mood or emotions
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Placebo
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A pharmacologically inert substance (often a sugar pill) produces a significant reaction because the patient expects, desires, or was told it would happen; used in clinical trials; highlights the body's natural healing powers
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Stages of Drug Development
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Isolation/chem synthesis of the product Laboratory studies Animal testing Clinical testing Approval by the FDA for market
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Drug Development
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Costly, lengthy, controlled by gov't -1970: 3620 drugs were tested. 16 came on the market at an average cost of $20 million -Only 1 in 2000 drugs eventually make it to the market
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Phases of Drug Development
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Phase I: Initial clinical trials on volunteers after the drug has proven safe when given to animals Phase II: Thorough clinical investigation to eliminate investigator bias Phase III: Extended clinical evaluation
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Drug Testing
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All drugs that are approved for market must be clinically tested multiple times: A) Most clinical tests are done on volunteers. B) Neither the researcher know in advance who is receiving the therapeutic medicine and who is receiving a placebo (control group) - This is called a double-blind study since nobody involved in the study is in the know *This limits intentional/unintentional bias C) Half receives the medicine and the other the placebo The initial trial will estb. possible side effects/drug safety
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Thalidomide
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An example of improper drug approval: 1. Developed in Germany in 1953 2. Used as a tranquilizer (1957-1962). Prescribed to combat morning sickness in the early months of pregnancy. 3. Marketed widely in Europe but never approved by the FDA in the USA. 4. Caused major birth defects in ABOUT 10,000 children whose mothers had taken thalidomide. 5. Has two optical isomers, one of which is a powerful teratogen (an agent or factor that causes malformation of an embryo); the other is a tranquilizer (sleep inducing).
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5 common points of drug administration
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1. Oral 2. Inhalation 3. Topical 4. Injection (3 types) 5. Anal
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The method of administration
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What determines the rate at which a drug is absorbed in the blood?
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Subcutaneous
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under the skin injection
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Intramuscular
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in the muscle injection
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intravenous
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directly in the vein injection
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Therapeutic Window
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Relates the therapeutic effects of a drug to its toxic effects
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LD50
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the dose (in mg of substance per kg of body mass) that is lethal to to 50% of laboratory animals
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LD
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Lethal dose
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More toxic
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With decreasing LD50, is the substance more toxic or less toxic?
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Botulism toxin (BoTox)
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Lowest LD50 rating known as of yet: the concentrated form of this substance - most toxic substance known; LD50 of roughly 0.005-0.05 µg/kg
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1.5
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What is the LD50 of Aspirin?
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0.23
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What is the LD50 of Nicotine?
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0.13
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What is the LD50 of Caffeine?
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3x10^-11
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What is the LD50 of Botulism toxin?
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Tolerance
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Over time the body adapts the presence of a drug: 1. The person receiving the drug needs ever larger doses to achieve the original effect 2. Tolerance results in increased risks of dependency/addiction 3. Increased risks of toxic levels 4. Possibility of immunity in anti-bacterials
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Side Effects
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Contraindications are additional and often undesirable effects that result from the use of a particular drug to treat a particular condition; Are somewhat relative depending on the reason the drug is prescribed The prescribing physician must weigh the benefits from the use of a drug against the undesirable side effects when determining a suitable level of risk The level of risk that is acceptable is related to the severity and the degree to which the condition is life threatening Examples: chemotherapy, pain killers, etc.
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Antacids
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compounds that are used to neutralize excess stomach acid(HCl); typically weak inorganic bases; often combined with alginates and antifoaming agents Examples: CaCO3, NaHCO3, Mg(OH)2, Al(OH)3, MgO and Mg(OH)2 (Milk of Magnesia)
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Neutralization reactions
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Write out the neutralization reactions between HCl and Aluminum Hydroxide, Magnesium Hydroxide, and Sodium Hydrogen Carbonate Answer: Neutralization reactions
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Alginates
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float on the stomach contents to form a neutralizing layer preventing heart burn
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Antifoaming agents
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agents such as dimethicone prevent the formation of gases and reduce flatulence
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Antigesics
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substances that reduce pain without the aid of sleep; many also act as a antipyretic
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antipyretic
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reducing fever to normal body temperature (anti = opposite of; pyro = fire / heat)
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Mild analgesics
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Intercept the pain stimulus at the source of injury or interfere with production of substances (like prostaglandins) that cause pain, swelling or fever. Ex. Aspirin and Paracetamol
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Strong Analgesics
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Temporarily bond with receptor sites in the brain, preventing the transmission of pain impulses without depressing the CNS. Ex. Morphine
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Analgesic mild pain reliever
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<3 out of 10 on NRS; non opioids Ex. paracetamol (acetaminophen), NSAIDs
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Analgesic moderate pain reliever
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3-6 out of 10 on NRS; Weak opioids Ex. codeine, dihydrocodeine, tramadol
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Analgesic strong pain reliever
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>6 out of 10 on NRS; strong opioids Ex. morphine, diamorphine, fentanyl, hydromorphone, oxycodone
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Aspirin
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In 1899, Bayer introduced the ethanoate ester of salicylic acid: 2-acetoxybenzoic acid or acetyl salicylic acid; derived from earlier salicylic acid Used as an analgesic for minor aches and pains, as an antipyretic to reduce fever, and as an anti-inflammatory medication.
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Paracetamol (Acetaminophen)
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Less side effects than aspirin. May cause kidney, liver damage Functional group: amide Preferred in the USA Overdose can cause brain damage to liver and kidneys
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Opiates
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Strong analgesics are given to relieve severe pain caused by injury, surgery, heart attack or chronic diseases. Go straight to the brain, find chemical receptors that receive pain messages and bind with (and blocking) the receptors, which stops the transmission of pain Problems: Tolerance can develop -> OD -> death
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Aspirin (Pros/Cons)
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Pros: Preventing recurrence of heart attacks & strokes (prevents blood clotting) Cons: Ulceration & stomach bleeding Allergic reactions Reye's syndrome in children - a potentially fatal liver and brain disorder Overdose can lead to acidosis (low blood pH)
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Paracetamol (Acetaminophen) (Pros/Cons)
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Pros: Very safe in the correct dose Safe for children - no side effects Cons: In rare cases, can cause blood disorders and kidney damage OD can lead to serious liver damage, brain damage and even death
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Morphine
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Basic structure of morph, codeine, and heroin but with an alcohol (hydroxyl group)
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Codeine
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Basic structure of morph, codeine, and heroin but with a methyl group that replaces the hydroxyl group
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Diacodeine (Heroin)
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Basic structure of morph, codeine, and heroin but with 2 acetyl groups (ethanoate)
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Advantages
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Advantages of using morphine and its derivatives as strong analgesics: Extremely strong, relieve severe pain caused by injury, surgery, heart attack or chronic diseases Treatment of diarrhea (produces constipation) Cough suppressant
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Short-Term Disadvantages
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Short term disadvantages of using morphine and its derivatives as strong analgesics: Euphoria Depress nervous system (slow breathing) Nausea & vomiting May lead to coma / death
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Long-Term Disadvantages
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Long term disadvantages of using morphine and its derivatives as strong analgesics: Constipation, poor eating habits Increased tolerance -> addiction 1. Social problems, such as theft & prostitution 2. Risk of AIDS, hepatitis, etc. from sharing needles 3. Cross-tolerance: increases tolerance for other opiates
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Depressants/sedatives
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a group of drugs that, according to dosage, reduce anxiety, produce calm and induce sleep 1. Often described as antidepressants b/c they relieve depression 2. Examples: alcohol, barbituates (phenobarbital) and benodiazepines
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Low doses
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depressants that exert little or no effect due to dosage
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Moderate doses
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depressants that may include sedation (soothing, reduction of anxiety) due to dosage
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High doses
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depressants that may induce sleep due to dosage
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Extremely high doses
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depressants that may cause death due to dosage
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Physiological Effects (of the use/abuse of ethanol)
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Due to using ethanol: Reduction in inhibitions, short-term reduction in reaction speed, short-term hangover, and long-term liver (and much other) damage
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Social/Economic Consequences (of the use/abuse of ethanol)
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Due to using ethanol: Violent behavior to family/strangers (from reduction in inhibition), Increase in car accidents (from short-term reduction in reaction speed), Absenteeism from work (from short-term hangover), cost of intensive medical care (from long-term liver (and much other) damage).
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Short Term health effects (of use/abuse of ethanol)
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Reduces anxiety and inhibitions Increases confidence & sociability Dilates small blood vessels -> warmth Impairs attention, judgment, and control Violent or aggressive behavior Loss of motor function
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Long term health effects (of the use/abuse of ethanol)
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Alcoholism is caused by an inability to reduce alcohol intake 1. Withdrawal symptoms: nausea, sweating, anxiety, hypertension or delirium tremens (shaking) 2. Tolerance Cirrhosis (scarring) and cancer of the liver (the major detoxification organ) Heart disease Hypertension Strokes Gastritis Ulcers Depression Miscarriage / birth defects
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Methods of alcohol level detection
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1. Breathalyser by potassium dichromate (VI) 2. Blood or urine analysis by chromatography 3. Absorption of infrared radiation or fuel cell in an intoximeter
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Stages of Alcohol influence
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Subclinical Euphoria Excitement Confusion Stupor Coma Death
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Clinical Signs/Symptoms of Alcohol
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Nearly normal Impairment Disorientation Inertia Unconsciousness Death
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Breathalyser analysis
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Subject breathes into an analyzer containing an oxidizing agent and a detector Potassium dichromate (K2CrO4) is the oxidizing agent Oxidizes ethanol to ethanoic acid This is an oxidation-reduction reaction that involves an electron transfer Cr+6 (orange) is reduced into Cr+3 (green) --- KNOW THIS This electron transfer generates an electric current which can be detected by the machine
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Blood/urine analysis
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More precise than breathalyzer Uses a stationary phase (non-volatile liquid or solid support) and a mobile phase (inert gas, like N2) Breath components (CO2, H2O, and alcohol vapor) are injected into the machine and partitioned (divided) between the stationary and mobile phases Components exit at different intervals (each substance has a different affinity and bond strength for the two phases, and thus move through at different rates) Components are detected 1. Retention time for each component is measured (time taken for each component to pass through the column) 2. Blood alcohol's retention time is compared to the retention time for a standard ethanol sample
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Absorpion of IR/fuel cell in intoximeter
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IR light does not promote electrons to higher levels, but does provide enough energy to make molecules "vibrate" 1. Vibrational motion depends on the mass of the molecule and the types of bonds present IR spectrum therefore depends on types of molecules present ("molecular fingerprint") Scale is based on wavenumber (1/wavelength) Police use intoximeter (IR spectrometer) to confirm breathalyzer test 1. IR radiation is passed through breath sample 2. C-H group in alcohol absorbs a certain frequency of IR light 3. % transmittance of the C-H frequency is determined, indicating amount of alcohol present
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synergistic effect
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the combination of the two drugs may be more harmful than either drug alone
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coma/death
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When alcohol interacts with sleeping pills/barbiturates
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stomach bleeding
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when aspirin interacts with alcohol
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extend high (also severe vasoconstriction - leads to rise in blood pressure + cardiac arrhythmia)
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when alcohol is mixed with cocaine
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inhibit breakdown
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when alcohol interacts with other drugs
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Diazepam (Valium)
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drug that relieves anxiety and tension, muscle relaxer
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Nitrazepam (Mogadon)
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hypnotic drug used to induce sleep
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Fluoxetine hydrochloride (Prozac)
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drug used to treat mental depression by increasing serotonin activity (a neurotransmitter)
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Benzodiazepine structure
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Structure comprised of a benzene, and a 7 member ring along with different side gps (see p 54 of powerpoint)
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stimulants
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Molecules that increase alertness and give greater sensitivity to external stimuli: 1.Mental processes may speed up 2. May create feelings of elation or possibly anxiety
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Adrenaline (aka epinephrine)
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naturally occurring hormone and stimulant - fight or flight; Amphetamines mimic the effects of this See pages 60-61 of ppt for more info
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sympathomimetic drugs
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Drugs, such as amphetamines, mimic the effects of epinephrine (adrenaline) and are known as _______
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amphetamine/epinephrine structure
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both derive from the phenylethylamine structure (i.e. a benzene ring with a 2-C chain and an amine group at the end) - therefore very chemically similar
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amphetamine
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drug that is a primary amine, having a -NH2 group also very chemically similar to adrenaline
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Short term effects (of) nicotine consumption
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Increased heart rate (↑ oxygen consumption) Increased blood pressure Reduction in urine output (anti-diuretic) Decrease in reflex times Stimulating effects
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Long term effects (of) nicotine consumption
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Emphysema: damage to alveoli shortness of breath Chronic bronchitis prolonged bouts of coughing Lung and throat cancer Increased risk of heart disease Pregnant women who smoke increase their risk for miscarriage, premature birth or stillbirth: 1. Babies born to smoking mothers have an increased risk of cot or crib death
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nicotine
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addictive properties of this drug are comparable to crack cocaine
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Caffeine
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respiratory stimulant 1. When consumed in large amounts it can cause anxiety, irritability and sleeplessness 2. It is a weak diuretic (promotes the formation of urine)
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a tertiary amine group
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What do both caffeine and nicotine share in common? Hint: (a nitrogen atom bonded to three carbons)
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antibacterial
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a destructive to or inhibiting the growth of bacteria
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Penicillin
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any of several antibiotics of low toxicity, produced naturally by molds of Penicillium
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Alexander Fleming
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the bacteriologist who found that Penicillium produces "penicillin" when its food resources are limited & that it inhibits the growth of a wide range of bacteria
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penicillin history
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A bacteriologist, Alexander Fleming, studied an antibacterial agent present in tears and nasal mucus, as well as in egg whites (called lysozyme) - in the 1920s Left a pile of used culture plates containing a growth of a Staphylococcus bacterium A rare stain of fungus called Penicillium notate entered through a window and landed on one of the plates A month later the fungus multiplied and inhibited the growth of the surrounding Staphylococcus bacteria Ultimately, Fleming found that Penicillium produces "penicillin" when its food resources are limited & that it inhibits the growth of a wide range of bacteria Chain (Florey's student) showed that lysozyme attcks the cell walls of bacteria disintegration - 1937 Chain (& 2 other scientists) improved the method of isolating penicillin, improving its purity - 1938
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Ernst Chain
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Researcher who was known for producing large quantities of penicillin and conducting medical trials; Also the student of Howard Florey
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Howard Florey
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researcher who continued research on lysozyme (the antibacterial agent in egg whites) - in the 1920s & 1930s
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1945
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In what year were Fleming, Florey & Chain were jointly awarded the Nobel Prze in Physiology or Medicine?
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penicillin function
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Bacterium that works by interfering with the chemicals that bacteria need to form normal cell walls 1. Therefore, Cell wall is weakened and the bacterial cell bursts, killing the bacteria 2. Humans do not have cell walls and are thus unaffected by ______
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(Type of) side chain
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How do penicillins differ?
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Resistance (to the penicillinase enzyme)
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What does modifying the side chain in penicillins result in?
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Mode of action (of penicillin) (aka function as well)
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They work by interfering with the enzymes that bacteria need to make normal cell walls. These enzymes can become resistant. As the cell swells, the osmotic pressure causes the wall to disintegrate.
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Penicillin G
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The origin penicillin notation mold was found to produce a mixture of different penicillin's that are called G (connected to CH2), X (connected to OCH2), F (connected to two side OCH2 groups) and K (connected to a CHCOOH group). Which one is most useful, based on a high effectiveness and yield from the fermentation process?
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antibiotic
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What was penicillin quickly used as against a variety of bacteria?
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History of penicillin
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During World War II, penicillins helped to rid of infected wounds (the biggest wartime killer) Also used to treat infected transmitted infections (STI's) that were common in soldiers
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(Penicillin) issues (of) overprescription
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Drug companies began mass producing penicillin in 1943 Penicillin-resistant bacteria Bacteria can become resistant to penicillin (and other antibiotics) because of overprescription Problem: If people take penicillin for a minor bacterial infection than their immune system would be able to deal with it, they are increasing the chances of resistant strain emerging When the non-resistant bacteria are destroyed, the small numbers of resistant forms will be able to multiply due to an absence of competition A process of natural selection that occurred in the bacterial population Similar reasoning can also be applied to people who do need to take antibiotics, but do not complete their course of treatment
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Tuberculosis Treatment
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This takes 6-12 months of antibiotics to rid of the bacteria TB resistance to penicillin and antibiotics is growing since the process takes so long This could be considered an overprescription It gives time for bacteria to build up resistance.
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Livestock
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Antibiotics have been widely used in the livestock industry to treat sick animals and to promote growth Other drugs prescribed to livestock include hormones to fatten and build up bulk weight and to reduce stress
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Bacteria
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Individual cell (has the machinery to do all it needs to survive itself) Reproduces on its own Circular DNA Use and obtain energy/metabolize on their own Bigger Grows and develops on its own *SEE page 88 on powerpoint for comparison to Viruses
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Virus
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Acellular (don't have organelles & can't survive without a host) Req. a living host to reproduce DNA/RNA in a capsid Uses and obtains energy from its host Smaller Cannot grow or develop
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size
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SEE page 89-92 on powerpoints for size comparisons between viruses, bacteria, and blood cells, along with how viruses invade Answer: size
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How antivirals work
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Antiviral drugs may work by: 1. altering the cell's genetic material so the virus cannot use it to multiply 2. OR preventing the viruses from multiplying by blocking enzyme activity within the host cell
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The trojan horse
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Viruses uses host's DNA-polymerase to replicate viral DNA Some antiviral drugs are structurally similar to viral DNA and codes for the replication process to stop This is a challenge because the drug has to be "activated" by a viral enzyme
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(3 possible approaches) to kill a virus
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1. The Trojan Horse 2. Retrovirus Inhibitors 3. Blunting the scissors
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Retrovirus inhibitors
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A retrovirus (such as AIDS) contains RNA rather than DNA Normally, when retroviruses inject their RNA into host cells, they use an enzyme, reverse-transcriptase, to convert their RNA into viral DNA in the cell Retrovirus inhibitors work by inhibiting the reverse-transcriptase enzyme and preventing the formation of viral DNA Example: AZT (Azidothymadine) is the best known anti-AIDS drug SEE: Page 97 on ppt
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Blunting the scissors
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When new baby viruses are created in their host cells, they need to escape so they can infect other cells They are able to do this by using an enzyme (neuraminidase) which cuts open the host cell wall, sort of like a pair of scissors If we introduce an inhibitor molecule (making it so they can't make those cuts), then the viruses permanently stay inside of the cell, rendering itself harmless (since it can't replicate)
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AZT (Azidothymadine)
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the best known anti- HIV/AIDS drug
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Selective toxicity
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A drug that kills harmful microbes without damaging the host
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T cells (a receptor protein on white blood cells)
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Where do specific proteins on the HIV virus bind to on white blood cells?
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Difficulties with antiviral drugs (and viral resistance)
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Difficulties with antiviral drugs since: 1. Viruses are simple & replicate quickly 2. Viruses can mutate quickly & "learn" to cope with the drugs 3. Viral metabolism is linked closely with the host cell 4. Killing the virus could actually be easy if you didn't care about making sure the host lives :/
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Factors in solving aids
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Cost: it's expensive Societal & cultural: 1. 95% of HIV positive people live in developing countries 2. Less than 8% who need retroviral therapy actually receive it AIDS stigma... leads to a fear of discrimination and/or violence, which can prevent many people from getting tested
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Prevention
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The key aim in trying to prevent the spread of/controlling of AIDS