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Lecture Two


The drugs job (i.e. get to the right binding site, fit snugly, turn receptor on/off or just occupy the site) is pharmacodynamics or pharmacokinetics? * Pharmacodynamics
The body's job (i.e. to try prevent drug entry to tissues, manage drug if it does get in (break it down, eliminate it) is pharmacodynamics or pharmacokinetics? * Pharmacokinetics
What are the pros and cons of taking a drug orally? PRO: Easy, preferred ROA. CON: Slow time of onset, especially in fed state, decreased bioavailability, peptide degraded
What are the pros and cons of taking drugs sublingually? PRO: Easy, faster onset than oral, better bioavailability than oral. CON: Not many drugs can be absorbed this way.
What are the pros and cons of IV, IP, IM, SC route of administration? PRO: Rapid onset (can be positive or negative), IV has optimal bioavailability. CON: once injected its non reversible, is aversive, skilled techniques are required, infection risk
What are the pros and cons of Inhalational route of administration? PRO: Rapid onset, better bioavailability than oral. CON: Not many drugs can be easily volatized, health risk if combusted
What are the pros and cons of taking drugs via insulfation? PRO: Faster onset than oral, better bioavailability than oral. CON: tissue damage to nose & vasculature, generally aversive.
What are the pros and cons of Rectal route of drug administation? PRO: useful of oral ROA not practical (person vomitting), better bioavailability than oral. CON: generally aversive.
What are the pros and cons of taking drugs Transdermally? PRO: Easy, non invasive ROA. CON: Not many drugs can be absorbed this way.
Describe what pharmacokinetics stands for. Pharmaco = drugs. Kinetics = movement/time. How the drug moves through your body and the processes that occur during that journey.
What are the 4 subdivision of pharmacokinetics? * Absorption, Distribution, Metabolism, Elimination
Describe the subdivision Absorption of pharmacokinetics * Absorption = movement of drug into the bloodstream.
Describe Bioavailability * The portion (%) of administered drug that reaches the systemic circulation. Different drugs have different bioavailability
What are the three factors that affect absorption? * - The drug molecule itself (particle size(tiny), ionization, lipothilic) - The route of administation e.g. IV injection means 100% bioavailabiltiy so all the drug is absorbed directly into bloodstream. - First-pass metabolism (needs to get past liver)
Describe the first-pass metabolism. Find out what exactly need to say for this first. ...
Describe distribution * Movement of the drug from the bloodstream into TISSUES
What are the factors that effects DISTRIBUTION of drug from the blood to the tissue? * 1. The drug molecule itself(tiny and lipothilic then will get out of blood and into tissue easier). 2. Perfusion of tissue/amount of tissue (easier to distribute into tissue of child than adult. 3. Kind of tissue. 4. Protein binding. See lecture notes
The portion (%) of a drug that gets bound to protein gets distributed. T or F? False it cant get distributed into tissue as it is no longer tiny and lipothilic.
What is the first attempt of metabolism called? First-Pass metabolism
What is the second parts of metabolism called? Phase I and Phase II metabolism
What does 'Half-life (t - 1/2)' refer to? = time required to metabolism 50% of the drug. So not dependent on concentration
What is an example of a Pro-Drug? and describe what this means * Codeine. Its a drug that actually needs to go through metabolism to actually become active. Codeine turns into morphine by going through FPM.
Describe Metabolism * Enzymatic breakdown of drug
What are the 2 factors (including 3 subpoints of second factor) that effect metabolism? * 1.Liver function (how well lover is working, if unwell from alcohol or hepititis then metabolism wont work as well). 2.Enzyme function (Genetics - asians don't have enyzyme to turn codeine into morphine, Enzyme workload, enzyme induction.see lecture notes
Why is half-life important? (2 reasons) 1. It is key to effective drug presribing e.g. Lorazepam v.s. Triazalam (drugs for imsomnia). 2. Is key to effective dosing regimens - how regularly you take the drug.
Define 'Elimination' as the fourth phase. * The removal of the drug from the body (clearance)
What are the 5 routes of elimination? * Renal (via the kidney, most common), Billiary (fecally), Exhalation (alcohol), lactation (breastfeeding), Perspiration (minor route through sweat - not alcohol)
Pharmacodynamics is all about the ....? design of the drugs
Who first described "receptive substance" in tissue? * John Langley
Who first defined 'receptor' and the Magic Bullet idea? * Paul Ehrlich
What did Otto Loewi do? * He showed that neurons release some substance capable of exerting physiological effects in another tissue preparation - showed that neurons communicate via chemicals.
What experiment did Otto Loewi do? Draw the diagram. The frog heart experiment.
Why is Otto Loewi's finding important? * Because it showed that neurons must release chemicals and that tissues must have receptors for these chemicals.
What did Henry Dale find? * That Acetylcholine (ACH) can slow and fasten responses so shows that there are Receptor subtypes. Showed that you can use exogenous chemicals to mimic endogenous chemical.
What experiment did Henry Dale do? Draw the diagram. * The skeletal muscle and heart experiment
Why is Henry Dale's findings important? (two reasons) * Because we now know that one endogenous neurochemical can have both +/- effects which suggests that there are receptor subtypes. Also that we can mimic the +/- effects by using exogenous chemicals.
Ligands can be e______________ (NT) or e_____________ (drug) Endogenous, Exogenous
Good ligands should have what two attributes? High affinity (hot tightly they fit into receptor), Selectivity
Some ligands also need? Efficacy (be an agonist rather than an antagonist).
What attribute of ligands are a bonus? Potency, with very potent drugs you don't need as much dose.
Go over the different Receptor Ligands - GABA, alcohol, Valium, bicuculline. ...
What are they three different manipulations that are drug can be? Agonist, Antagonist, Inverse Agonist.
A drug that binds to a receptor and 'turns it on' is a what? Agonist
A drug that binds to a constitutively active receptor and turns it off is a what? (would use this is receptors are doing something bad all the time to shut it down) Inverse Agonist
A drug that binds to a receptor but does not activate it is a what? Antagonist
Membrane Receptors can be ? Ligand-gated ion channels, G-protein coupled receptors, tyrosine kinases, nuclear receptors
What are the two types of classes/types of Receptors that we will focus on? Ionotropic Receptors (receptor itself is an ion channel) and Metabotropic Receptor (G-protein receptors)
What are the 3 attributes of Ionotropic Receptors? fast acting (changes (incr or decr. excitability fast), Opens/closes channel, short duration effect
What are the 3 attributes of Metabotropic Receptors? Slow acting, diverse range of effects, long lasting effect
There are 3 different types of G-proteins. What are they? Gs (Stimulatory), Gi (inhibitory), Gq
What does the Gs protein do? It activates AC (adenylate cyclase) so makes cAMP (?) to send message downstream.
What does Gi protein do? Inhibits AC (adenylate cyclase).
What does Gq protein do? It activates PLC to make 2nd messenger DAG & IP3
What are the four major steps of Synaptic Transmission? 1. Synthesis and packaging of neurotransmitter. 2. Release of neurotransmitter, 3. Binding of neurotransmitter to post-synaptic receptors. 4. Clearance of neurotransmitter via enzymatic breakdown and /or reuptake transporter.
What are the 4 major targets/aims of psychoactive drugs? * see revision notes
Define drug tolerance. * Decreased responsiveness to drug
Define drug dependence * Physiological withdrawal symptoms upon cessation of the drug.
What type of tolerance is this? "Receptor desensitisation and/or downregulation of receptor number" Pharmacodynamic tolerance
What type of tolerance is this? "Metabolism increased because CP450 enzymes upregulated (so less gets distributed to the brain)" Pharmacokinetics tolerance
What type of tolerance is this? "Behavioural conditioning to counterbalance effects (e.g. if you drink every day at 5pm)" Contextual tolerance
Withdrawal symptoms (in relation to drug dependence) indicates that new h___________ has been achieved during drug use. homeostasis
What is a drug-drug interaction? One drug alters the effect of another.
The drug-drug interaction can be pharmaco___________ (e.g. CYP induction, renal clearance - kidneys dont filter at the same rate). The drug-drug interaction can be pharmaco___________ (e.g. valium + alcohol = addictive GABA(A) effect) kinetic, dynamic
Valium is a ? Depressant
Are drug-drug interactions seen as good or bad? Bad. We want to avoid and minimise them. Unless to reverse the overdose of a drug like alcohol for example.
What does does a therapeutic window mean? * The rang of drug dosage which can be effective whilst staying within the safety range.
If a drug has a narrow therapeutic window, what does this mean? * It means that there is only a small dosage where the drug is therapeutic and will therefore go from therapeutic to toxic with only a small amount in the blood
What kind of dosing schedule is needed to reach a steady state within the optimal therapeutic dose? * The amount you administer each dose at each half-life (time required to metabolise 50% of the drug) e.g. take another dose every 4 hours if the half life is 4 hours. So would reach steady state in 5-6half lives (20-24 hours).
Is there any way you could shorten the time it takes to reach a steady state? * Yes, have a large dose for the first dose only = loading dose e.g. take 100mg to get concentration up immediately and then 50mg from then on.
Why is receptor theory important for a course in Drugs and Behaviour? Appreciate the contributions of Langley, Ehrlich, Loewi and Dale. * In revision book. Memorise
What did John Langley do? * He described 'receptor substance' in tissues
What did Paul Ehrlich do? * He defined 'receptor' and the Magic Bullet idea
What did Otto Loewi do? * Showed that neurons release substance capable of exerting physiological effects in another tissue preparations. This is important as it tells use that neurons release chemicals to communicate & that tissue have receptors for those chemicalsegfrog/HR/water
What did Henry Dale do? * Showed that ACh can slow and fasten responses of cells/organs. This is important as it shows us that there are receptor subtypes and that we can mimic +/- effects using exogenous chemicals.
Define agonist * A drug that binds to a receptor and 'turns it on'
Define anatagonist* A drug that binds to a receptor but does not activate it, just occupies it
Define Inverse Agonist * A drug that binds to a constitutively active receptor and turns it off. (if receptor is active all the time you want to shut it down).
What is a Ligand? * A molecule that binds to a receptor such as a drug, ion or hormone. It has the following characteristics: exogenous or endogenous, agonist/antagonist/inverse agonist, high/low affinity, high/low efficacy and high/low potency.
Define affinity * Affinity refers to how well the ligand (drug) fits into the receptor. A ligand with high affinity fits perfectly and with low affinity it might fall out, sort of fits.
Define efficacy * Efficacy refers to the degree of effect that a ligand (drug) has. High efficacy means high effect e.g. an agonist and antagonist both have good efficacy as turn on/off. But inverse agonist has no efficacy as it has neutral effect.
Define potency * Potency of ligand/drug refers to how strong in concentration the ligand is e.g drugs with high potency you only need 1mg but low potency you need 10mg
Compare and contrast metabotropic and ionotropic receptors * See revision notes!
Created by: alice476