Pharmacology 1


Pharmacology 1 Flashcards on Pharmacology 1, created by Shannon Austen on 26/07/2016.
Shannon Austen
Flashcards by Shannon Austen, updated more than 1 year ago
Shannon Austen
Created by Shannon Austen over 7 years ago

Resource summary

Question Answer
What are the 3 main types of names used to recognize drugs? Brand name Chemical composition Generic names
What are the 4 main types of drug classification? Pharmacotherapeutic Pharmacological actions Chemical Structure Company Classification
Which type of name does the WHO recommend using within the clinical setting and why? Generic as they are the most simplified name and provide clues to the origin, use, action or structure of the drug
What is another name for generic drugs? International non-propriety names (INN)
Which type of drug classification is according to the condition being treated? Pharmacotherapeutic applications
Which type of drug classification is based on how the drug achieves its effect? Pharmacological actions
Which type of drug classification is based on molecular structure? Chemical structure
Which type of drug classification is based on code names used for drugs still within the early stages of development? Company classification
What are the 4 major types of Molecular targets? Carriers, Enzymes, Receptors and Ion Channels
What are the 3 mechanisms for how drugs work? Agonists/ Antagonists Affinity (potency) Efficacy
How do drugs work? Interfering or inhibiting natural processes required for normal physiological function which may have been disrupted by disease
What is the physiological function of carriers? Moving nutrients and waste products into and out of cells and organs
Where are Carriers located? In the cell membrane
List a clinical example of Carriers as the drug target Depression: inhibitor of neurotransmitter uptake (serotonin)
What is the physiological function of Enzymes? Regulating protein concentrations and
What is the difference between competitive and non-competitive enzyme inhibitors Competitive Enzyme inhibitors can be displaced (effects slowed or stopped) by adding more substrate, non-competitive Enzyme inhibitors cannot be displaced with more substrate
What is substrate? The substance on which enzymes act
What is a clinical example of competitive Enzyme inhibitors? Monoamine Oxidase Enzyme Inhibitor, depression eg, phenelzine
What is a clinical example of non competitive enzyme inhibitors? Cyclo oxygenase enzyme inhibitor, anti-inflammatory eg, aspirin
What is the physiological function of Receptors? Proteins which recognise drugs and endogenous compounds and which have a role in regulating cell functions
How many receptors are there in the body? Thousands
What is the main drug target? Receptors
What are the 4 receptor types? Ligand gated ion channels G-protein (guanosine binding protein) coupled Enzyme (tyrosine Kinase) Linked Nuclear
Where are Ligand gated ion channels located? In the cell membrane
What is the structure of ligand gated ion channels? 4 or 5 sub units which, together, form an ion channel
What is the mechanism of Agonist binds to open or close ion channel
What is the speed of response from drugs target Fast - milliseconds
Where are G protein coupled receptors located Found throughout the body in cell membranes
What is one of the physiological functions of G protein coupled Controlling blood pressure
What is the structure of G protein coupled receptors? 7 trans membrane segments; extra cellular and intracellular sections
What is the mechanism of G protein coupled receptors? Activation of intracellular messengers via the G-protein
Why is the G-protein coupled receptor an important drug site? More than 50 percent of drugs target that site
What are some examples of G-protein receptors? Adrenoreceptors Histamine receptors Serotonin receptors Dopamine receptors Opioid receptors
Where are Enzyme linked, Tyrosine Kinase receptors located? cell membranes
What is the response time of drugs using G protein coupled receptors Fast - seconds
What is the structure of Enzyme linked, tyrosine kinase receptors? Large extracellular ligand binding domain linked to a tyrosine kinase extra cellular domain
What is Tyrosine Kinase? Tyrosine kinase is an enzyme that can transfer a phosphate group from ATP to a protein in a cell. It functions as an "on" or "off" switch in many cellular functions.
What is the mechanism of drugs which target enzyme linked, tyrosine kinase receptors? The occupation of the receptor = phosphorylation of proteins in the cytoplasm which results in altered enzyme actvity
What is the speed of response of drugs which target Enzyme linked tyrosine kinase receptors? slower - minutes to hours
Where are nuclear receptors located? intracellular, cell nucleus
What is the structure of nuclear receptor? A large monomeric (molecule which can combine with others to make polymers) protein
What is the mechanism of nuclear receptors? binds to hormone responsive elements of DNA to regulate transcription
What is the speed of response for drugs which target nuclear proteins? Slow - hours
What are agonists? Drugs which mimic effects of endogenous ligand (produce more of a physiological function associated with the endogenous ligand)
What are antagonists? Competitive (reversible) or non competitive (non reversible) interferer or inhibitors of physiological function associated with endogenous ligand
What is selectivity? How selective (picky) a drug is about the receptor it attaches to
What does affinity mean? How strong a drug binds to the receptor
What does efficacy mean? The maximum effect a drug can have
What is the therapeutic index? LD50 - lethal to 50 % of population ED50 - effective in 50 % of the population Crude measure of safety which doesn't predict many adverse effects of drugs
What are some genetic sources of PD variability? mutation identified at drug receptors disease susceptibility response to drugs
How does the process of G-protein coupled receptors drugs work? Drug is administered extracellularly Reacts with G-protein in the membrane which acts on the 2nd messenger system intracellularly to produce cellular effects
What is a drug concentration - response curve (cr curve)? Determines drug's potency it is maximal efficacy
What is the process that agonist drugs use to produce maximal efficacy? Binds to and activates the receptor to produce a response (mimicking endogenous ligand) Response increases in proportion to the dose administered until receptors are saturated
In regards to agonists what happens when receptors become saturated? Any increase in dose will produce no additional response
What is the endogenous ligand? A chemical messenger
What is a drug's potency? How strong a drug is
What is a partial agonist? A drug with sub-optimal response when all receptors are occupied, resulting in decreased efficacy in comparison with full agonists
Which direction does the CR curve move with competitive antagonists? Shifts to the right but remains parallel with agonist curve Has the same shape as agonist curve and same maximal efficacy
How does the CR curve move with no- competitive antagonists Does not obey normal concentration - response relationship. Non-parallel shift with agonist curve max response decreased
What is the scheduling of medicines and poisons? A way of classifying which drugs are accessible to the general public based on factors like margin of safety and potential to cause dependency
List the prescription only drugs and their associated scheduling S4: Prescription drugs like antibiotics, vaccines, antidepressants S8: Controlled drugs like morphine and and opioids
List the non-prescription drugs an and their associated scheduling S2: Pharmacy medicine like cold medicine and cough medicine S3: Pharmacist only medicine on professional advice like metered dose asthma aerosols
What are unscheduled drugs? Drugs which can be sold in super markets such as paracetamol
Why are schedule 8 drugs controlled? They are drugs of dependence and whilst they need to be available for use manufacture, supply, possession and use need to be restricted
What is drug abuse? Continued administration of a drug in excessive quantities despite clear harmful effects
What is tolerance? A decrease in response to a drug occurring with continued use and which requires a higher dose to achieve same results
What is dependence? Pre-occupation with obtaining and using the drug of choice for its psychoactive effects and continued administration to prevent withdrawal syndrome
What are 3 generic names for opioids? Morphine, Methadone and Buprenorphine
What are 3 names for Benzodiazepines? Diazepam, Alprazolam and Temazepam
What are 2 generic names or stimulants/ Dexamphetamine and Methylphenidate
What are 3 kinds of controlled drugs? Opioids, Benzodiazepines and stimulants
What are 3 things you can do to be safe when administering controlled drugs? Always check the dose, refer to institution protocols when administering controlled drugs an monitor patient before and after administration
What are some examples of types of drug discovery? chemical modification random screening of biological products Traditional remedies Rational drug design
What is some typical criteria for a successful new drug? Effective against target protein, no serious adverse drug reactions, oral formulation if possible, good solubility and permeability which means it is readily absorbed and stable and long lasting in the body
What is target selection in drug development? Finding a target protein which is the best site in the disease pathway. typically a receptor or enzyme
What is optimisation in drug development? Figuring out if your drug can be improved for potency, selectivity and reduced toxicity
What is high throughput screening? A process within optimisation in drug development where lots of cells are used in conjunction with a chemical library to see if chemicals in library will give you a better drug
What is a chemical library? When a chemist makes lots of compounds like the drug being developed but slightly different to be tested during high throughput screening
What are pharmacodynamics? What the drug does to the body
What are pharmacokinetics? What the body does to the drug
What is toxicology? Does the drug cause organ failure, cancer or sterility?
What is the pharmaceutical aspect of drug development? Can the drug be made large scale, cheaply and is it stable (what is the shelf life)
What stage of drug development do target selection, optimisation and animal testing occur? Pre-clinical
What is acute toxicity in animal testing? Single dose lethal in 50% of animals This dose compared with therapeutic dose
What is sub chronic toxicity in animal testing? Multiple doses in a longer term (28 days) used with multiple species to find the target organs of toxicity
What is chronic toxicity in animal testing? One to two years used especially for drugs which require us to take them for extended periods
What is reproductive toxicity in animal testing? Does the drug affect mating behaviour, fertility, birthing, birth defects, litter numbers etc
What is the process for cancer testing within the animal testing phase? two years on two species looking at organ tumour expression
What is meant by the term genotoxic in drug safety testing? Does it damage DNA?
What are some drawbacks of pre clinical testing? Time consuming (2-5 yrs) and expensive with lots of animals used. The effects on animals don't necessarily translate to humans and rare effects might not be detected
What is the motto for administering drugs? Start slow and small and build up
What are the main international controls on drugs signed and ratified by Australia? UN single convention on Narcotic Drugs
What does the UN Single Convention on Narcotic Drugs control? Production, manufacture, trade and use of narcotics (outlawed except for medical use) as well as limiting possession to authorized personnel and taking control of all opium transactions and import/export
What does the Government assess therapeutic drugs for when considering drug controls? Safety, Effectiveness, Manufacture quality: purity, stability, strength as well as availability and marketing and manufacturer's license
Do the State and Territories or the Commonwealth control therapeutic goods? Commonwealth
Does the State and territories or Commonwealth control medicines and poisons? The State and Territories
What is the Therapeutic Goods Act? Regulates therapeutic goods including medicines, blood products, medical devices and public access level and evaluates drug quality, safety and efficacy vs how cost effective it is before marketing
True or false: each state/territory has it's own laws/ regulations on drug control? True
What do the state and territory laws on drug control deal with? Imposing restrictions on who can purchase, possess, store and supply medicines, poisons and controlled drugs
What does ARTG stand for? Australian Register of Therapeutic Goods
What are the two types of Australian Register of Therapeutic Goods? AUST L (listed) AUST R (registered)
What is the difference between AUST L and AUST R? AUST L - vitamins, herbals, fish oils etc lower risk of harm from self medication, purpose on label AUST R - prescription and over the counter (all meds)
Who is responsible for scheduling of medicines? State - based
List 5 prescription requirements? Patient name, address, drug name (generic), drug form (tablets, capsules), drug quantity
What is PBS? Pharmaceutical benefits scheme - subsidises a select list of medicines for medical and dental treatment designed to meet community need of essential medicines
What is pharmacokinetics? What the body does to the drug
What are the mechanisms of pharmacokinetics? Absorption (getting into the body) Distribution (traveling around the body) Elimination (body getting rid of it, metabolism, excretion)
How can therapy fail in pharmacokinetics? Concentration too high or too low
What is the therapeutic index? The ratio of the toxic dose (TD) to the effective dose (ED)
Why is pharmacokinetics important? It determines: Dose needed by patient to be in therapeutic range, adverse effects, if a patient does not get better or worse on a medicine (genetic factors, other medicine)
What is meant by patient response variable? Same dose does not suit all patients
What are some patient response variables which could affect the effectiveness of the drug? Disease, age extremes, other medicines, diet, environment, pregnancy, genes
How do you fix problems arising from altered pharmacokinetics? Alter dosage regimen by changing route of administration, dose, frequency or duration
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