Principles Of Pharmacology Textbook Notes PDF
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University of Guelph
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These notes provide a basic overview of pharmacology, focusing on the scientific study of drug actions and effects. They cover specialized areas such as neuropharmacology and psychopharmacology.
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..... PRINCIPLES PHARMACOLOGY PHARMACOLOGY - Scientific study of actions of drugs and...
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PRINCIPLES PHARMACOLOGY PHARMACOLOGY - Scientific study of actions of drugs and their effects Specialized a re a s : ↳ Neuropharmacology - > drug induced changes In cell and nervous system function ↳ psychopharmacology - > drug Induced changes on mood , thinking , behaviour Neuropsychopharmacology-> drugs/chemical substances that act on NS and alter behaviour ↳ combination of 2 specializations Placebo-pharmacologically inert compound that has both therapeutic and side effects drug action ↳ when binds to molecular changes drug effect of site placebo = common example non-specific target classical conditioning + placebo ↳ drug effects improvement associated With characteristics of symptom ↳ the (taste physiological/psychological functions of drugs medication , colour , shape , size) O alternate days medication and placebo = minimize side effects specific drug effect ② conscious effect-anticipating outcome , bring more relief ↳ physical/biomedical interactions at target site ↳ individuals have high natural pain relief neuropeptides therapeutic effects Nocebo - > opposite of placebo (negative impact/changes) ↳ desired (ex : pain relief) changes ↳ having When substance can i n c re a s e negative expectations given anxiety side effects typically induces pain/stress ↳ ALL other undesired effec ts vary in severity non-specific effects ↳ based on characteristics of Individuals experience present mood attitude. expectations · drug , , Pharmacokinetics factors of determining drug action happens at same time other where whereargeraise materials ↳ no (1) route -how drugsbind ase target steps cycle fast where administered how or is determines the and a drug and completely When here of administration absorbed blood. sites drug is in i stribute binding is reversible mostly (2) absorption of distribution - > and drugs enters RARELY blood act plasma where it (transfers contacts drug the to body ALL it cells) enters through many cell membranes molecules move to tissues and bind to active target Sites (receptors) (3) binding - > drug bone/fat become na a proteins /be stored temporarily In and drugcanalso bindtoplasma Inac tivation a ka biotransformation - influences duration + intensity of drug effects (4) Inactivation - of metabolic In liver + other tissues result processes blood drugs from body urine/feces is to with -> into blood need get · liver metabolites eliminated circulatory (drugs go through the body) (5) excretion > - amount of drug in blood FREE to bind some eliminated by Kidney bio-availability - > to target-sites to brain of drug drug methods of administration influence onset ac tion access drug DENTERNAL blood level Gl variable O (B-B-B) the trac t drug 2 : use slow onset and Fluid major categories blood-brain-barrier of Cerebrospinal , - -> made ↳ rectal ② oral and routes extracellular fluid ↳ selectively ②PARENTAL : all other routes that do NOT use tract ↳ Injection permeable. Inhalation , subcutaneous network of blood vessels that permeate brain blood plasma supplied by dense ↳ brain with CO2 Waste supplies cells oxygen , glucose , amino acids and removes + depot binding : such as plasma proteins drug binding at Inactive sites are called drug depots ↳ drug molecules at depots can NOT reach active sites or be metabolized by liver is bound blood drug binding only until drops drug level · = reve rs i b l drug unbinds and circulates in plasma first-pass effect - > drugs enters administered the general orally circulation pass through liver before it I drug cose/concentration occurs in first-order Kinetics drug Clearance > usually - ↳ individual differences based on sex and body size first-order kinetics expressed as my of drug/kg of body weight ↳ constant Fraction (50 % ) of free blood is exponential elimination > drug in removed in each drug · - rate of this process is called drug half-life (tv) route of administration alters absorption through Zero-order Kinetics ↳. area of absorption surface ↳ drug molecules cleared at constant rate regardless of concentration of cell layers layers destr a ·amountofdrug biotransformation by microsomalenzumze liver solubility of ionization of drug · variety of chemical · common enzyme = cytochrome P450 (CYP450) transport across membranes ↳ bi-layerhe negatchargeChudrophila oxidizes Most psychoactive drugs (antidepressants , morphine , amphetamines cell membranes = phospholipid obic some liver (enzyme drugs · can induce enzymes induction) > ex : repeated Usage of carbamazepine - passive antiseizure (YP4S0 diffusion drug Tegretol increases enzymes leading to faster metabolism , lowe blood level ↳ highly lipid soluble drugs pass through membrane by passive diffusion and biological effect of drug leaves blood / stomach and enters lipid layers Juice other inhibit liver lenzym inhibition) drugs > reduces metabolism other · can at enzymes of drugs taken - moves by concentration gradient - > from high to low concentration same time , experiences more intense/prolonged effect ↳the the rapid the diffusion and risk of Toxicity larger the concentration difference more 2 majortypes ofphasenonsyntheticmoderate is lipid soluble unionized drugs = insoluble lonized drugs = lipid I- phase nonsynthetic modifications occur through oxidation (loss of electrons) reduction , (gain electron O (PH) or hydrolosis ionization depends on - > relative acidity/alkalinity of solution ② Intrinsic property of the molecule (pKa)-s youhe phase II-L-synthetic reactions that combine drug with molecule such to be ionized small as glucuronide , sulfate they ionize at of the or methyl groups BASES -> range drugs either weak ACID or weak fluid they are dissolved interactions drug-receptor located on the surface or Within cells (cell sur face or intracellular receptors - > large protein molecules cell ligands-any moule thabtoreceptor speacres fit ligand efrcacy-c ability of ligand to changes a se ↳ response Lagonists typically have better affinity) agonist- high biological > excellent fit and response , fit low biological response Antagonist - worse , STRUCTURE FUNCTION NERVOUS SYSTEM · -. or electric transmission within a neuron cells of the nervous system ① neurons 2 mantupes of glial cells - supporting alls (metabolic support , protection , insulato a restingmembrane potential-TOm n outside neuron = polarized at rest neurons · ↳ the positive ions outside the cell main principle = transmit info in electrical signals more negative charged i o n s I n cell , more sensory neuron-sensitive to environmental stimuli · K + (potassium) moves more freely -> some channels NOT gated at rest convert stimuli into electric signals ↳ the cell higher concentration inside Interneuron- brain spinal cord Nat (sodium) concentrated outside the cell >. nerve cells with and are higher recieve Signals from Neuron responsible for conscious sensations recognition mem decisions C1-(chlorides sensory , - , , Since inside of cell is more negative , the ions Inside do not move through membrane appropriate for situation ↳ KI by electrostatic motor neuron - > direc t behavioural responses positive charged = pulled into cell pressure It concentration rises , + leaves the cell in exchange (inward electrostatic pressure + outward concentration gradient 3 main anatomical ↳ equilibrium potential for potassium features smallleaks ofWatintothe of neurons : · cell - their is an exchange ora a set O every 3 Na pumped out - 2 K pumped in (keeps cell negative dendrites ↳ dendrites/soma recieve info from other cells across gaps called synapses summary : · dendrites contain thousands of receptors covered With dendritic - > Increase SA - spines recieving gapsof ↳ · at myelin cells are polarized rest ② Tom AXOnS resting potential - - single long , extension from axon potential is due to uneven distribution of ions across membrane - > lons more through specific channels ↳ tubular · , filled with axoplasm , vary In length and diameter that are NOT usually open a xo n hillock · transmit electrical signal generated in + moves more freely branches axon collaterals change potential = · rapid In membrane potential = action terminal buttons = contain NT that allow for chemical transmission to-Somu (threshold for firing to AP-1 membrane potential from-70mu generate goes · of info across the synapse -50mV Na channel opens 3 o u t- 2 k at every in made of · axons Wrapped In Myelin-fatty Insulating coating AP and electric transmission glial cells speed up - ③ SOMG : responsible for metabolic care of n e u ro n conduction ↳ synthesizes proteins needed for cell growth/maintenance saltutory ↳ enzymes , receptors , cell membrane ↳ in myelinated axons. AP regenerate ONLY at nodes contains of DNA nucleus > has chromosomes -- strands saltatory conduction (produces rapid - thato a of ranvier of chromosomes genes -Smallportons jumps between from node-node ions at nodes Na-K pump only exchanges ·transcripton MessengerRNA(mRNAmakCoPhOFTe efficient because ge · more to ribosomes , decodes recipe and links amino acids of nervous system protein to form organization D NA-transcription - mRNA-translation protein brainanda - CNS -> c o rd PNS - > all nerves axoplasmic transport-how proteins are mored to required destination ↳ Somatic NS-voluntary ↳ · depends on structure of cytoskeleton - > matrix composed of tubular struc tures , provide · autonomic WS-Involuntary track for newly synthesized proteins carried by motor proteins ↳ sympathetic NS · movement occurs in both directions NS · parasympathetic ↳anterograde:van fromsumpruten growthmochondriaproteinsneedfor NT Synthesis look at the PNS cells for closer glial - provide support neurons Oligodendroglia -L in multiple axons CNS ① in 4 types - somatic nervous system ② Schwann cells -- in single neuron in PNS ↳ astrocytes largea eachspinalhervehasmanyneuros · mixed nerves offerents to the spinal cord = Sensory signals going signals to