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Chem 1004- Midterm Review.docx

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Carleton University
CHEM 1004
Gerald Buchanan

Chem 1001- Midterm Review Drugs on the Human Body Terms • Acute: brief, intense, severe vs. chronic: not severe, long lasting • Carcinogenic: causes cancer vs. teratogenic: causing birth defects • Euphoria: state of exaggerated well being • Peripheral: at the extremities • Peristalsis: rhythmic motion of GI system in digestion • Syndrome; signs and symptoms associated with a disease • Synergistic: working together to give super additive effects • Tachycardia: abnormally fast heart rate vs.bradycardia: slow • Renal: pertaining to kidneys • Visceral: pertaining to internal organs • Febrile: feverish • Emetic: drug that induces vomiting • Antipyretic: drug that reduces fever • Analgesic: drug that reduces pain Prefixes and Suffixes • Hyper: more than normal vs. hypo: less • Cardio: related to heart • Gastro: related to GI system (often stomach) • Myo:muscle • Intra: within • Inter:between • Poly:many • Dys: painful,bad,difficult • Osteo:pertaining to bone ---------------------------------------------------------------------------------------- • -emia :in or of the blood • -itis : inflammation of • -ectomy:incision or removal of a part • -algia:pain in a part –i.e. neuralgia (nerve pain) • -uria: in or of the urine Pharmacodynamics: studies drug actions and effects Pharmacokinetics: studies rates of change of drug concentrations in the body and includes rates of absorption, distribution, metabolism and excretion of a drug What is a Drug? - Any absorbed substances that alters or enhances any physical or psychological function in the body Drug Dependence and Addiction • Occasional use > frequent use > physiological dependence > compulsive use > overwhelming involvement = addiction • Upon termination of drug use the addict suffer withdrawal syndrome • Addicts often develop a tolerance and so increased doses are required to achieves desired effect • 3 types of drugs producing withdrawal syndrome 1. Depressants: alcohol, benzodiazepines, barbiturates 2. Opiates: heroin, morphine, methadone 3. Stimulants: cocaine, amphetamines, caffeine Use of Prescription Drugs - relieve symptom, fight disease, maintain health, restore normal function, aid in diagnosis - Double Blind Studies: 50% or patients receive placebo and 50% receive real drug o Placebo effect can be seen in 30-40% of patients - Tamiflu: effective or not? o Non reporting of side effects o Stockpiled by CAN gov’t in case of flu epidemic Chemotherapy - planned attack on a disease using specific chemical designed for that purpose - Paul Erlich- 1st agent Salvarsan, treatment of Syphilis - Other forms of treatment not involving chemicals: o Holistic- considers emotional, spiritual & psychological factors o Herbal- some unconventional bee venom, shark cartilege, Echinacea o Homeopathy- uses tiny doses of active constituent Other Medicine Naturopathy- techniques used to restore heath rather than to treat disease - Mind body systems: hypnosis, meditation Bioelectromagnetic- magnets, electric currents, copper bracelets Body Based- chiropractor, acupuncture, massage How do drugs work? Receptor Site Theory- drugs act at specific locations in organs and tissue - Lock and key mechanism: drug my spacially fit into receptor site and have correct electrical charge - Sites exists to receive hormones and other natural substances the body produces - Agonist- drug that fits in a receptor site and cause a response - Antagonist- drug that binds to receptor site and successfully excludes other substances from binding (may not cause response) Where do drugs come from? Historically from plants: Morphine and Codeine- extracted from opium poppies Aspirin- Willow bark Cocaine- coca bush Marijuana- Cannabis sativa Taxol (new anti-cancer drug)- Yew tree Drugs from animal sources: Insulin- promotes and regulates glucose metabolism - Dog pancreas Steroids- biosynthesized in humans from cholesterol Majority of drugs on the market are made by Chemical Synthesis Viagra Patent Ruled Invalid - Discovered by accident when a drug to act as a vasodilator was being tested - Pfizer made billions - Patent later ruled invalid because it didn’t specify active ingredient - Opens door for generic version - November 2012 - Other drug companies (Teva) can now distribute generic drug but cant name it Viagra, the name remains protected by patent Drug Naming - Every drug has at least 3 names - Brand, Generic, Chemical Fatality from too much water - Woman drank 4L in 2 hours - Died from electrolyte imbalance Therapeutic Index - Defined in terms of effective dose in 50% of patients and toxic dose in 50% of patients - Larger the value safer the drug o Marijuana- 1000 o Cocaine- 15 o Alcohol- 10 - TI= TD / ED . 50 50 Unit Conversions • Gram (basic mass unit) : 454 g=1 lb • .001 g= 1mg (milligram) or 10 g -3 -6 • .001mg= 1ug (microgram) or 10 g -9 • .001ug=1ng (nanogram) or 10 g • 1L= 1000mL • 1mL = 1 cm or 1 cc. Organic Chemistry Organic chemicals: are those compounds containing carbon Inorganic compounds: don’t contain carbon Families of compounds have a similar structure and therefore similar properties Functional group is a small set of atoms, held together by covalent bonds in a specific and characteristic arrangement, that is responsible for the principal chemical and physical properties of that compound What defines a steroid? - The fused 6,6,6,5 membered ring sturctures Why is cholesterol important? - Can be converted to vitamin D during the day - Biosynthetic precursor for many hormones in our body ie. Testosterone and estrogen - Additional structure to cell membranes What happens to drugs after we take them? Routes of Administration - oral, inhalation, injection, skin application, implantable, microsponges Orally Ingested Drugs - Expected to disintegrate in stomach and enter bloodstream by absorption from stomach or small intestine - Enterically coated- designed not to dissolves until in the stomach Inhaled Drugs - Rapidly absorbed due to large number of blood vessels in lungs and nasal region Parenteral (Injected) - Hypodermic injection into muscle, veins, beneath skin, - Rapid access to bloodstream - Disadvantages: possible pain, need for sterilization, costly, possible contamination Powder injection - A jet of He gas accelerates fine particles of tiny amounts of vaccine into outer layer of skin - Small quantities present a limitation Body Orifices - Eye, ear, nose drops - Buccal cavity- behind teeth and cheek o Tobacco Skin Application - Petroleum based creams - Some aerosol sprays - Transdermal Skin Patches o Slow absorption into bloodstream o Drug must have significant solubility to pass through semipermeable membrane o Nicotine patches o Thigh, buttocks, upper arm or back Implantable Drug Delivery - Pellets, reservoirs or pumps - Slow release - Insulin, morphine, antibiotics, contraceptive Microsponges - High prosperity of sponge allows large surface area to be filled with drug Tablet Treatments - Some foil wrapped to keep out moisture - Contain binders to hold active ingredient together Bayer Advanced Aspirin - Smaller particle sizes means it dissolves 6x faster than previous formulation - Only in USA Pharmacokinetics - Study of rates of change of concentrations in the body - Factors involved: absorption, distribution, metabolism and excretion Body Mass Index (BMI) - Weight in kg/height in m .2 The Blood Brain Barrier - As a general rule, fat soluble drugs penetrate more easily than water soluble materials - Drugs that easily penetrate barrier include o Alcohol, marijuana, tranquilizers, LSD • Glucose is the most abundant organic compound on earth Penetration of Membranes - Passive Diffusion: most drugs cross membranes by diffusion from an area of high to low concentration - Active Transport: rare for drugs, involves a series of chemical interactions between transported substance and cell membrane o Glucose across blood brain barrier Placental Barrier - Almost all drugs taken by mother cross the barrier - But the barrier protects against bacteria - Cocaine, caffeine, and heroin easily pass through barrier Xenobiotic- foreign substance in the body - Drugs, pesticides - Body must be able to break these down in order to eliminate them from body - CYP enzymes found in liver assume responsibility of breaking down them down Drug Half Life - Time needed for initial level of drug in blood to fall to half its value Age on Metabolism - Lose water, increase fat levels and lose muscle mass o Therefore fat soluble drugs stay in body longer - Kidney function diminishes - Enhanced brain sensitivity to drugs 3 Types of Drug Tolerance 1. Metabolic- liver makes more enzyme to cope with increased dose 2. Cellular-Adaptive- receptor site loses sensitivity to drug, tissue become accustomed to drug 3. Behavioral Tolerance- user learns how to handle the drug in way a nonuser cannot Drug-Drug Interactions - Synergism: 2 drugs may act on each other to enhance each others effects Birth Control Pills: can be rendered inactive after eating lime, grapefruit, pomelos Taking one tablet with a glass of grapefruit juice is equivalent to taking 20 with a glass of water - 85 known drugs effected by grapefruit - 43 have serious side effects: sudden death, acute kidney failure, - Contains “furanocoumarins” - Aspirin, acetaminophen, ibuprofen not a effected NSAIDS - Non-steroidal anti-inflammatory drugs - Alleviation of pain (analgesia) - Aspirin is the only with anti-inflammatory effects Evolution of a Drug - Investigate ‘folk’ medicine - Isolate active ingredient and prove structure - Synthesize natural compound to confirm structure and provide material - Test of physiological effects; often many - Synthesize compounds to emphasize desired effects and ‘delete’ unwanted ones - Test of efficiency and safety Aspirin: Case Study - The beneficial effects of willow bark has been known since ancient Greek times - In
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