Guest Presentation #1 - Principles of Pharmacology

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Questions and Answers

What is defined as a substance used as a medication or in the preparation of medication, or a substance recognized in an official pharmacopoeia or formulary, intended for use in the diagnosis, cure, mitigation, treatment, or prevention of disease, other than food intended to affect the structure or function of the body, or intended for use as a component of a medicine but not a device or a component, part, or accessory of a device?

A drug.

What is defined as any substance, other than a normal constituent of the body or one that is required for normal bodily function, that, when applied to or introduced into a living organism, has the effect of altering bodily function(s)?

A drug.

What are the 3 different kinds/ types of drug names?

Chemical Generic Trade

What are the 3 ways by which drugs can be classified? (Acronym hint: a knee injury)

<p>Mechanism of action Chemical structure Legal classification</p> Signup and view all the answers

What are the 6 phases of drug approval?

<p>Preclinical testing Phase 1 - clinical trial - healthy Phase 2 - clinical trial - test efficacy, side effects Phase 3 - clnical trial (efficacy, safety) Health Canada process Phase 4 - clinical trial (postmarket surveillance)</p> Signup and view all the answers

What is the name of the overarching legislation for food, drugs, cosmetics and therapeutic devices, and what year was it developed?

<p>Food and drugs act, and in 2020.</p> Signup and view all the answers

What are the 2 parts of the food and drugs act?

<p>Food, Drugs, Cosmetics, Devices, Natural Health Products Administration and Enforcement</p> Signup and view all the answers

What are the 8 legal drug classifications in the controlled drugs and substances act, and what is an example of each?

<p>Schedule I (narcotics, cocaine, etc.) Schedule II (Cannabis related) Schedule III (narcotic-like, LSD, etc.) Schedule IV (Barbiturates) Schedule V (propylhexedrine <stimulant>) Schedule VI (precursors) Schedule VII (cannabis over 3Kg) Schedule VIII (Cannabis small amounts) Schedule IX (Device to make Pills or other medication)</p> Signup and view all the answers

Which 3 legal drug classifications in the controlled drugs and substances act have recently been taken out?

<p>Schedule V (propylhexedrine <stimulant>) Schedule VII (cannabis over 3Kg) 2018 Schedule VIII (Cannabis small amounts) 2018</p> Signup and view all the answers

What is the definition of the study of the effects of drug on the body and its mechanism of action?

<p>Pharmacodynamics</p> Signup and view all the answers

Summarize the dose-response curve for most drugs.

<p>The more drug you give, the more response you'll get until you hit a ceiling</p> Signup and view all the answers

What is the definition of a therapeutic or adverse reaction that is not due to a pharmacological effect of the drug?

<p>Placebo</p> Signup and view all the answers

What are the 3 types of drug effects?

<p>Additive Synergistic Antagonistic</p> Signup and view all the answers

What are the 4 types of adverse drug reactions? (Acronym: system of a down)

<p>Side effects/ sensitivities Overdose toxicity Allergic reactions Drug interactions</p> Signup and view all the answers

What is an issue that is usually centered around the cytotoxicity to a drug?

<p>Organ adverse reactions.</p> Signup and view all the answers

What organ has an adverse rection to Tylenol?

<p>The liver.</p> Signup and view all the answers

What organ has an adverse rection to NSAIDs?

<p>Kidney</p> Signup and view all the answers

What 3 organs has an adverse rection to alcohol?

<p>Liver Gut Heart</p> Signup and view all the answers

What is the definition of study of the time course of a drug and its metabolites in the body after administration by any route?

Signup and view all the answers

Whta are the 4 aspects that pharmacokinetics study? (Acronym: BEAD)

<p>Biotransformation Excretion Absorption Distribution</p> Signup and view all the answers

What is the definition of the process of drug movement from the administration site to the systemic circulation?

<p>Absorption</p> Signup and view all the answers

What are the general 5 routes of administration that affect the drug's absorption?

<p>Oral Topical Vaginal, rectal Injection Inhaled</p> Signup and view all the answers

What are the 3 routes of oral administration?

<p>Swallowing Oral Buccal</p> Signup and view all the answers

What are the 4 routes of topical administration?

<p>Eyes Ears Nose Skin/ transdermal</p> Signup and view all the answers

What are the 6 routes of injection drug administration?

<p>IV IM SQ/ subcutaneous Intra-articular Intra-cardiac Intra-dural</p> Signup and view all the answers

What are the 6 general factors affecting drug absorption?

<p>Solubility, particle size Surface area at the site of administration (determined by the route of administration) Exercise – decrease gut BF, increase BF to muscle and skin Concentration Circulation to the site of administration Ice vs massage of area where drug applied</p> Signup and view all the answers

What are the 6 factors that affect ORAL drug absorption? Acronym: FLSMD)

<p>Motility of gut Lipid solubility Stability to acid and enzymes Formulation (tablet, liquid, delayed release) Food in stomach Degree of first-pass metabolism</p> Signup and view all the answers

What is the definition of the extent to which (and sometimes rate at which) the active moiety (drug or metabolite) enters systemic circulation, thereby gaining access to the site of action?

<p>Bioavailability.</p> Signup and view all the answers

What are the 4 steps of the first-pass effect?

<p>Drug is taken orally Drug enters GI tract Active drug is absorbed from stomach and small intestines High blood concentration of drug is in hepatic portal vein Low blood levels after passing through liver</p> Signup and view all the answers

What effect does heavy exercise have on gastric emptying?

<p>It decreases it.</p> Signup and view all the answers

What effect does light exercise have on gastric emptying?

<p>Decreases it</p> Signup and view all the answers

What effect does exercise have on the blood flow to the gut?

<p>Decreases it.</p> Signup and view all the answers

To what 2 places is a drug distributed immediately after administration?

<p>Interstitial fluids Cellular fluids</p> Signup and view all the answers

To what 3 places is a drug distributed the first minute after administration?

<p>Heart Kidney Brain</p> Signup and view all the answers

To what 2 places is a drug distributed first several minutes and hours after administration?

<p>Muscle Skin Fat Other internal organs</p> Signup and view all the answers

Signup and view all the answers

What is the main limiting factor for drug tissue distribution?

<p>Pattern of blood flow</p> Signup and view all the answers

What are the 2 physiological factors affecting drug distribution?

<p>Cardiac output Local blood flow</p> Signup and view all the answers

What are the 3 categories of local blood flow that affect the distribution of a drug?

<p>Blood-brain barrier (some drugs don't cross it) Local capillary structure Placenta (lipid soluble drugs cross more readily)</p> Signup and view all the answers

What are the 4 physiochemical factors affecting drug distribution? (Acronym: BALP)

<p>Binding to plasma proteins Accumulation in tissues Lipid solubility Permeability</p> Signup and view all the answers

What is the difference between a bound and free drug?

<p>Bound drug - a drug that is attached to plasma proteins (such as albumin). While bound, the drug is inactive because it cannot cross cell membranes or exert its effects.</p> <p>Free drug - drug that is not bound to plasma proteins and is available to interact with receptors, cross membranes, and exert its therapeutic effect.</p> Signup and view all the answers

What are the 2 definitions of the change of the chemical structure of a drug to get rid of it via conversion by enzymes to more polar/ less lipid soluble forms?

<p>Biotransformation/ metabolism</p> Signup and view all the answers

Where does biotransformation of drugs occur primarily, and what 2 other places does it occur in?

<p>In the smooth endoplasmic reticulum of cells in the liver, and can occur in the kidney and intestine</p> Signup and view all the answers

How many reactions does biotransformation consist of?

<p>Two (phase 1 and 2)</p> Signup and view all the answers

What two phases does phase 1 of biotransformation consist of?

<p>Conversion to polar metabolite Effects</p> Signup and view all the answers

What are the 3 stages of the first "conversion to polar metabolite" stage of phase 1 of biotransformation?

<p>Oxidation Reduction Hydrosis</p> Signup and view all the answers

What are the 3 effects of phase 1 of drug biotransformation?

<p>Inactivation Increase activity (more rarely) Reduction of activity</p> Signup and view all the answers

What needs to occur for a drug in order for it to be in its more effective form?

<p>It needs to be converted to its more active form</p> Signup and view all the answers

What is the more active version of cadeine?

<p>Morphine</p> Signup and view all the answers

What is the less active version of morphine?

<p>Codeine</p> Signup and view all the answers

What are the 2 ways to convert codeine to morphine?

<p>Allele can be deleted Extra allele can be formed</p> Signup and view all the answers

What are the 2 parts of phase 2 of biotransformation of a drug?

<p>Conjugation Effects</p> Signup and view all the answers

What is the definition of the coupling of drug (or its polar metabolite) with an endogenous substance?

<p>Conjugation</p> Signup and view all the answers

What are the 3 potential 3 effects of drug biotransformation?

<p>Inactivation Partial inactivation Increase</p> Signup and view all the answers

What are the 3 general categories of factors affecting biotransformation of a drug?

<p>Generic Environmental Physiological</p> Signup and view all the answers

What is the genetic factor affecting biotransformation of a drug?

<p>Mutation leading to gene deletion</p> Signup and view all the answers

What is the genetic factor affecting biotransformation of a drug?

<p>Mutation leading to gene deletion</p> Signup and view all the answers

What is the environmental factor affecting biotransformation of a drug?

<p>Drug interactions</p> Signup and view all the answers

What is primary physiological factor affecting biotransformation of a drug?

<p>Liver disease, a.k.a. cirrhosis</p> Signup and view all the answers

What effect does exercise have on blood flow, urine output, and renal clearance?

<p>A decreased one.</p> Signup and view all the answers

What does exercise do for renal blood flow and urinary pH?

<p>Decreases blood flow, and increases urinary pH.</p> Signup and view all the answers

What 2 anatomical structures does the excretion process occur through?

<p>Urine Kidneys</p> Signup and view all the answers

What are the 5 substances that are excreted by the body, and drugs are in?

<p>Urine Feces Bile Sweat Exhalation</p> Signup and view all the answers

What are the 2 net effects of renal excretion?

<p>Decrease in renal clearance Change in reabsorption of drugs Transient proteinuria, hemoglobinuria (high intensity)</p> Signup and view all the answers

What is it called when a constant AMOUNT of drug is eliminated per unit of time?

<p>Zero order</p> Signup and view all the answers

What is it called when a constant FRACTION of drug is eliminated per unit of time?

<p>First order.</p> Signup and view all the answers

What is it called when the drug elimination kinetics may vary with time and dose (not specific zero or 1st order, but rather a combination of them?)

<p>2nd order or multi-exponential Kinetics</p> Signup and view all the answers

What is the definition of the drug interaction between genes and the body?

<p>Pharmacogenetics</p> Signup and view all the answers

Clinical pharmacokinetics

<p>What is the definition of the specific quantitative pharmacokinetic properties of a drug determine its dosing schedule, dose and means of administration?</p> Signup and view all the answers

In regards to a therapeutic range, what is the concentration that produces half the greatest possible effect called?

<p>Lower limit</p> Signup and view all the answers

In regards to a therapeutic range, what is that which is no more than 5-10% of when patients experience a harmful side effect called?

<p>Upper limit</p> Signup and view all the answers

What are 2 examples of narrow therapeutic window drugs?

<p>Coumadin Lithium</p> Signup and view all the answers

What are 2 examples of narrow therapeutic window drugs?

<p>Some antibiotics (penicillin) Some anti-inflammatories (ibuprofen)</p> Signup and view all the answers

What is the definition of when a drug's rate of input equals teh drug's rate of loss?

<p>Steady state.</p> Signup and view all the answers

What 3 things is drug dosing and frequency related to?

<p>Bioavailability Clearance Volume of distribution</p> Signup and view all the answers

What is the definition of the time required for the plasma concentration of the drug to be reduced by half?

<p>Half-life</p> Signup and view all the answers

Generally, when are drugs that are given intermittently given?

<p>At the half-life interval.</p> Signup and view all the answers

Within how many doses of a drug does steady state typically occur?

<p>Approximately 3 doses</p> Signup and view all the answers

What is the definition of diminished tolerance to a drug over time?

<p>Tolerance.</p> Signup and view all the answers

How quickly does tolerance to a drug develop?

<p>Slowly.</p> Signup and view all the answers

When tolerance occurs, what happens to the other agents in the same class?

<p>Cross tolerance.</p> Signup and view all the answers

What 3 changes occur to the receptors of the drug?

<p>Change in number of receptors Changes in affinity of the receptor for the drug Decreased responsiveness at the receptor</p> Signup and view all the answers

How are tolerance and addiction different?

<p>Tolerance is the diminished action of the drug, while addiction is a biopsychological process that results in repeated use of drug/ behavior despite harm to oneself and/ or others</p> Signup and view all the answers

What is the definition of the extent to which a patient tales the prescribed medication?

<p>Patient adherence.</p> Signup and view all the answers

What are the main 4 reasons for nonadherence to a drug?

<p>Cost Forgetfulness Inconvenience Poor patient education</p> Signup and view all the answers

How is the drug response different from the elderly than for the young and middle aged? (in 2 ways)

<p>Sensitivity - enzymes aren't like they used to be Dosing changes for organ changes (liver, kidney function)</p> Signup and view all the answers

What are the 3 main reasons for medication errors?

<p>Wrong dose Miscommunication Drugs that look or sound alike</p> Signup and view all the answers

Which 2 classes/ kinds of drugs especially look or sound alike?

<p>Cough medications Cold medications</p> Signup and view all the answers

For alcohol, where does the absorption occur, and which portions does 70-80% of it occur?

<p>In the gastrointestinal tract, and in the duodenum and jejunum.</p> Signup and view all the answers

For alcohol, what reduces its absorption?

<p>Food in the stomach.</p> Signup and view all the answers

Which kinds of areas in the body rapidly reach equillibrium for alcohol absorption, what are 4 of these areas, and which one of them is toxic?

<p>Areas with high blood flow, brain + heart + lungs + liver, the heart is the most toxic</p> Signup and view all the answers

What percentage of alcohol is absorbed into fatty tissues?

<p>4%.</p> Signup and view all the answers

Who is the volume of distribution less for - women or men? And for that gender, are the blood concentrations higher or lower?

<p>Women, and higher.</p> Signup and view all the answers

How does principle elimination of alcohol occur?

<p>By oxidation to CO2 and H2O</p> Signup and view all the answers

What percentage of alcohol can be eliminated by urine?

<p>1%</p> Signup and view all the answers

What percentage of alcohol can be eliminated by the lungs?

<p>1-3%</p> Signup and view all the answers

What percentage of alcohol can be eliminated by liver oxidation?

<p>90-95%</p> Signup and view all the answers

In order, what are the 5 substances that are required for alcohol metabolism?

<p>Ethanol ...then NAD+ to ADH to NAH ...lastly, acetaldehyde</p> Signup and view all the answers

In order, what are the 5 substances that are required for alcohol oxidation?

<p>Acetaldehyde ...then NAD+ to ALDH to NADH ...to acetate</p> Signup and view all the answers

Where is alcohol metabolized, and by what substance?

<p>In the liver, and by cytosol</p> Signup and view all the answers

Where does alcohol oxidation occur?

<p>In mitochondria.</p> Signup and view all the answers

When acetate is released to the blood, what is it oxidized into?

<p>Carbon dioxide/ CO2</p> Signup and view all the answers

What are the 3 clinical effects of alcohol?

<p>CNS depressant Diuretic Toxic effects on muscle, heart, brain (cerebellum), liver</p> Signup and view all the answers

In what percentage of 3 populations does alcohol dehydrogenase operate 5x than normal?

<p>In 85% of Asian populations In 5-10% of English populations In 20% of Swiss individuals</p> Signup and view all the answers

What 4 effects does alcohol dehydrogenase operating 5x than normal cause?

<p>Vasodilation Facial flushing Bronshospasm Tachycardia</p> Signup and view all the answers

What percentage of asian populations have Aldehyde dehydrogenase-2 deficiency?

<p>50%</p> Signup and view all the answers

What effects does aldehyde dehydrigenase-2 deficiency result in?

<p>Facial flushing Tachycardia Diaphoresis Muscle weakness</p> Signup and view all the answers

What receptor do codeine and morphine act on, and in what 3 organs?

<p>u-opioid in the brain, gut, and kidney</p> Signup and view all the answers

What is the best opioid receptor antagonist?

<p>Naloxone</p> Signup and view all the answers

What is the appropriate dosing for codeine and morphine pills, respectively?

<p>15-45mg q 6 hours, and 5-15 mg q 4 hours</p> Signup and view all the answers

What is the appropriate time to effect for codeine and morphine pills, respectively?

<p>30+ minutes, and 15+ minutes</p> Signup and view all the answers

What is the appropriate duration for codeine and morphine pills, respectively?

<p>4-8 hours, 3-6 hours</p> Signup and view all the answers

What % of caucasians are either a rapid or poor metabolizer?

<p>10%</p> Signup and view all the answers

What are 8 signs of opioid intoxication and overdose? (Acronym: BCCPSSUV)

<p>Breathing problems, apnea Cyanosis Cold, clammy skin Pinpoint pupils Slurred speech, drowsy, confusion Slowing heart beat Unconsciousness Vomit, seizures</p> Signup and view all the answers

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Capital of France (example flashcard)

Paris

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