Chapter 1-3 Exam

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Flashcards on Chapter 1-3 Exam, created by Madeline Luedke on 25/09/2016.
Madeline Luedke
Flashcards by Madeline Luedke, updated more than 1 year ago
Madeline Luedke
Created by Madeline Luedke over 7 years ago
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Question Answer
Pharmacology The scientific study of the actions of drugs, and their effects on living organisms
Neuropharmacology drug-induced changes in the functioning of cells in the nervous system
Psychopharmacology Drug-induced changes in mood, thinking or behavior
Neuropsychopharmacology Identify substances that act on nervous system, to help alter behavior for hurt or disease
Drug Actions Refer to the biological changes or the specific molecular changes produces when a drug binds to particular target site or receptor
Drug Effects the widespread physiological or psychological changes that occur as a result of drug action
Specific Drug Effects based on physical and biochemical actions of drug at target site on the body
Non-specific drug effects not based on chemical action, but unique characteristics of person (previous drug experience, present mood, environment, expectation, attitudes)
Bioavailability the amount of drug in the blood that is free to bind at target sites and causes actions
Pharmacokinetics the dynamic other factors that contribute to drug action (absorption, distribution, elimination)
Absorption movement of drug from site of administration to blood circulation
Drug Map 1. Route of administration 2. Absorption/Distribution 3. Binding 4. Inactivation 5. Excretion
Different routes of administration 1. oral 2. intravenous 3. intramuscular 4. intraperitoneal 5. subcutaneous 6. inhalation 7. topical 8. transdermal
Oral (PO) • easy, painless • must dissolve in stomach fluid • be able to pass through stomach walls to blood • resist destruction by stomach fluids • most drugs are not fully absorbed until in small intestine
First-pass metabolism (first-pass effect) PO drugs goes to the liver before the blood which reduce the amount of bioavailability • PO drugs produce blood levels that are irregular, unpredictable, and rise slowly
Intravenous (IV) • placed directly into blood stream • Pros: rapid & accurate • Cons: easy to overdose
Intramuscular (IM) • into muscle •Pro: slower and even absorption (slower if in vegetable oil suspension) • Con: irritation at injection site
Intraperitoneal (IP) • into abdominal cavity • Pro: Rapid (less than IV) • Con: Rarely used in humans
Subcutaneous (SC) • inject below the skin • Pro: slow and steady absorbtion
Inhalation • inhaled directly into lungs • Pro: rapid • lungs have large surface area with capillaries, blood goes directly to brain (no liver first) • surpasses first-pass metabolism
T • applied to mucus membrane • provides local drug effect, but can go system wide
Transdermal • through skin • skin blocks water soluble drugs, but fat soluble can pass • Pro: controlled, sustained passage, at given rate
phospholipids complex lipid molecules • look like Y • single head is negatively charged & hydrophilic (likes water) • two tails are uncharged, fatty & hydrophobic (hates water)
hydrophollic • single head of phospholipid that likes water • touches intra and extra cellular fluids
hydrophobic • two-tail fatty ends stick together
Lipid-soluble drugs • can pass through membranes • move from high concentration to low
passive diffusion move from higher concentration to lower concentration
concentration gradient differences in concentration • the steeper the gradient, the faster the diffusion
Ionization Dissolve into charged ion particles when in water • ionized stuff doesn't pass through membranes easily
pH scale and ionization Strong acids: low numbers, ionize completely in water | battery acid weak acids: kinda ionize | tomatoes Neutral: 7 Weak Bases: kinda ionize | SLC Strong bases: high numbers, ionize completely completely in water | drain cleaner
Weak • tends to dissolve into charged ions • weak doesn't mean not concentrated • most drugs are weak acids/bases
Environmental factors and Ionization • depends on ionizeability of drug (pH) • pH of place drug is being dissolved in • same pH = less ionization • acid <3 base = baby ions • lack of charge means more lipid soluble so it can pass through into blood
Ion trapping drugs can't go back into blood
Absorption Factors 1. Rate: at which stomach empties into small intestine 2. Size: of person, dosages based on 18-65 at 150 lb 3. Sex: of person, women have more fat, less water volume = higher drug concentrations
Blood Brain Barrier • Protects blood-borne substances by dense network of blood vessels • "net"
Blood flow and concentration • most blood flow have higher concentration • heart, brain, kidneys, liver • brain gets 20% of blood that leaves the heart
Cerebral Spinal Fluid (CSF) • made by choroid plexus • fills "spaces" • cushions brain against injury • blood vessels pass through subarachnoid space
Typical Capillaries • Nutrients in/waste out • small openings (intercellular clefts) • big openings (fenestrations) • pinocytotic vesicles (transport stuff through/elevator)
Intercellular Clefts small openings in capillaries
Fenestrations big openings in capillaries
Pinocytotic Vesicles • like an elevator • transports stuff through
Brain Capillaries • Cleft closed with tight junctions • no fenestrations • rare pinocytotic vesicles • surrounded by glial feet of astrocytes
Area Postrema | Chemical Trigger Zone (CTZ) • in medulla of brain stem • detects toxic substances in blood • vomiting center
Median Eminence • of hypothalamus • has fenestrations that let hormones made in hypothalamus move to pituitary gland
Placental Barrier seperates blood circulation of pregnant mother and fetus • lipid-soluble drugs pass easily
Drug Depots reservoirs of drug at inactive sites which trigger no biological effects • plasma protein, muscle, fat
Depot Binding • drug binding at depot sites • displaced drug gets dumped back into circulation
Biotransformation metabolically transformed
First-Order Kinetics • elimination is exponential: constant faction of drug is removed from blood at each time interval
Half-life amount of time needed to remove 50% of drug in blood • after 6 half-lives the drug is gone
Zero-Order Kinetics • drug molecules cleared at constant rate, regardless of concentration • alcohol
Microsomal Enzymes • in the liver • most drugs metabolize through this
Two kinds of biotransformation 1. Phase 1, Nonsynthetic 2. Phase 2, Synthetic
Phase 1, Nonsynthetic • by oxidation • resulting metabolite is less lipid soluble and often less active
Phase 2, Synthetic • required combination of drug with another small molecule (gulcoronide, sulfate, or methyl group) • Resulting metabolite is less lipid soluble, always inactive
Cytochrome P450 • 30 enzymes in this family oxidize a majority of psychoactive drugs
Notes on biotransformation both create metabolites which are more water soluble and easier to excrete • metabolites are returned to the bloodstream • metabolites eliminated by kidneys or bile/feces
Factors Influencing Drug Metabolism • Can affect the magnitude and duration of drug effects • responsible for drug interactions, and individual responses 1. Enzyme Induction 2. Enzyme Inhibition 3. Drug Competition 4. Genetic Polymorphisms
Enzyme Induction repeated use increases liver enzymes = faster metabolism for that drug and all others that need that enzyme • tolerance & cross-tolerance
Enzyme Inhibition some drugs block enzymes = slower metabolism for that and all other drugs needing that enzyme
Drug Competition for same enzymes • can't metabolize both, so levels of one get out of control
Genetic Polymorphisms people vary in metabolism
Acetaldehyde metabolite of alcohol • effects 50% of Asians when this builds up
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