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Clinical Nursing Jan exam > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

Define pharmocokinetics

A

What the body does to the drug

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2
Q

Define pharmoacodynamics

A

What the drug does to the body

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3
Q

What are different methods of drug transfer across membranes

A 
Aqueous diffusion
Passive lipid diffusion
Facilitated diffusion
Pinocytosis (budding of membrane to ingest into cell)
Active transport
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4
Q

What factors affect rate of membrane transport according to ficks law?

A 
Diffusion coefficient
Surface area
Membrane thickness
Partition coefficient (how drug distributes in liquid vs oil)
Concentration gradient
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5
Q

What are the methods of drug disposition?

A

Absorption
Distribution
Metabolism
Excretion

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6
Q

Define bioavailability

A

Fraction of dose reaching systemic circulation after administration compared to same dose given intravenously

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7
Q

What factors affect drug absorption?

A

Route of administration

Formulation

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8
Q

How does ionisation affect absorption of drugs?

A

Drugs are weak acids or bases, with ionisation affected by their pKa and surrounding pH
pH changes with infection etc
Non-ionised drugs- cross by passive diffusion
Ionised drugs- cross by transport mechanisms, facilitated diffusion or pinocytosis

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9
Q

List routes of drug administration and how it affects drug absorbtion

A

Intravenous- rapid absorption as directly into systemic circulation
Intramuscular- speed dependent on local blood flow and diffusion of muscle
Subcutaneous- slower and less predictable, depends on site, temperature, hydration etc.
Oral- mainly absorbed in small intestine, effected by GI motility, splanchnic blood flow, drug size etc., will undergo first pass metabolism
Inhalational- causes local effect or absorbed into circulation
Epidural, transmucosal, transepithelial- effects at site of admin, can be taken up systemically

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10
Q

What is meant by first pass metabolism?

A

Concentration of drug given orally is reduced before entering systemic circulation

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11
Q

What determines volume of drug distribution?

A

Amount administered and concentration of the drug in plasma

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12
Q

How does protein and tissue binding of a drug affect its distribution?

A

Albumin binds weak acids
Alpha-1-acid glycoprotein binds weak bases
Only unbound drugs can interact and cause effect on the body
(Tissue binding can be specific or non-specific)

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13
Q

How does organ blood flow, membrane permeability and drug solubility effect drug distribution?

A

Drugs initially go to tissues with high blood flow

Highly lipid soluble drugs will accumulate in fat

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14
Q

Define clearance

A

Volume of plasma from which drug is completely removed per unit of time

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15
Q

Define half-life

A

Time taken for plasma concentration to fall 50% of original level

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16
Q

What factors affect drug metabolism and excretion?

A

Clearance and half life

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17
Q

Define biotransformation

A

Alteration of substance within the body

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18
Q

Name the stages of drug metabolism

A

Biotransformation

Excretion

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19
Q

Why do most drugs need to undergo biotransformation before they can be excreted by the kidneys?

A

Lipophilic and highly bound

Kidneys excrete polar water soluble compounds most easily

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20
Q

What is the main organ of metabolism and how does it work?

A

Liver
Phase one- convert drug to polar metabolites allowing renal excretion
Phase two- conjugation/combining with substrates

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21
Q

What can be the effects when drugs are activated by metabolism?

A

Become active drug
Produces active metabolites causing further effects
Produces toxic metabolites

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22
Q

What is the most common excretion of drugs and how does it work?

A

Renal
Active- tubular secretion
Passive- glomerular filtration

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23
Q

What other methods of drug excretion are there other than renal?

A

Biliary system
Exhalation
GI system

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24
Q

What is meant by enterohepatic circulation?

A

Pathway drugs take until plasma concentration drops

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25
Describe the pathway taken by drugs in enterohepatic circulation
``` Drug metabolised by liver Biliary excretion Deglucorinidation/reverse metabolism by gut microflora Reabsorption in gut Drug metabolised by liver ```
26
List the stages a drug takes when causing an effect on the body
Drug site of action Pharmacological effect Clinical response- therapeutic effect and toxicity
27
Define clinical response
What is seen due to drug
28
Define therapeutic effect
Desired effect of a drug
29
Define toxicity
Side effects of a drug
30
List non-cellular mechanisms of effect of drugs
Physical Chemical Physiochemical Modification of body fluid composition
31
List cellular mechanisms of effects of drugs
Alter physicochemical mechanisms of the body Cell membrane structure and function modification Enzyme inhibition Receptor mediation
32
Define therapeutic index
Maximum non-toxic/minimum effective dose of a drug based off 50% of animals
33
Why is using therapeutic index for drugs flawed?
Effective dose will vary depending on what is being treated | Wont account for idiosyncratic drug reactions (reactions unrelated to dose)
34
Define affinity
How well a drug binds to its receptor
35
Define intrinsic activity/efficiacy
Magnitude of effect once bound, measured 0-1
36
Define agonist and state an example
Generate maximal response when bound to a receptor, have high affinity and intrinsic activity/efficacy Morphine
37
Define partial agonist and state an example
Intrinsic activity less than 1 so cant generate maximal response even with full receptor occupancy Buprenorphine
38
Define inverse agonist and state an example
Drug binding exerts opposite effect compared to endogenous agonist Antihistamines
39
Define antagonist and state and example
Exhibits affinity without intrinsic activity | Atipamezole
40
Define potency
How much of the drug is needed to cause wanted response
41
List the molecular targets for drugs
``` Receptors Enzymes Transporters Ion channels Nucleic acid ```
42
Define ligand
Substance that forms complex with boimolecule
43
Define receptors
Protein interacting with extracellular physiological signals, converting them to intracellular effects
44
Name an example of a receptor for drugs
Mu opioid receptor
45
What is the difference in effect of agonists and antagonists on receptors?
Agonists- cause direct effects (ion channel opening/closing) or transduction mechanisms (enzyme activation or inhibition, ion channel modulation, DNA transcription) to cause effect Antagonists- no effect caused or prevent agonist binding preventing or reversing effect of agonist
46
List the 4 main types of receptor
Ligand gated ion channels (ionotropic- membrane bound) G-protein coupled receptors (metabotropic- initiates metabolic processes to modulate cell activity) Kinase linked receptors Nuclear receptors
47
What are the characteristics of ligand gated ion channel receptors? (Speed of action, how they cause effect, example)
Act in milliseconds Hyperpolarise or depolarise Nicotinic ACh receptor in neuromuscular junction post synaptic membrane
48
What are the characteristics of G-protein coupled receptors? (Speed of action, how they cause effect, example)
Act in seconds Change membrane excitability or second messengers cause effect leading to cellular effects Muscarinic ACh receptor in smooth muscle of blood vessels
49
What are the characteristics of kinase linked receptors? (Speed of action, how they cause effect, example)
Act in hours Protein phosphorylation leading to protein synthesis and cellular effects Cytokine recpetors
50
What are the characteristics of nuclear receptors? (Speed of action, how they cause effect, example)
Act in hours Gene transcription and protein synthesis causing cellular effects Oestrogen receptor
51
How do enzymes act as drug target and what is an example?
Become activated by agonists and inhibited by antagonists | Cyclooxygenase enzyme
52
What effect do enzymes have on prodrugs?
Converts to active drug undergoing reaction to produce more effect on the body
53
Define prodrug
Molecules converted into active drug
54
How do transporters work as drug target and what is an example?
Agonists bind and move into cell Antagonists bind and block transporter Insulin
55
How do ion channels work as drug targets and what is an example?
Agonists increase or decrease probability of opening Antagonists block channel Local anaesthetics on nerves channels
56
How do nucleic acids work as drug targets and what is an example?
Alter gene transcription | Chemotherapy drugs
57
How are antimicrobial agents classified?
Type of organisms effective against | Either bacteriostatic or bactericidal
58
Define bacteriostatic
Prevent bacterial multiplication to remove infection by immune system
59
Define bactericidal
Kill bacteria
60
What are antibiotic dependent on to be effective?
Concentration- outcome related to peak antibiotic concentration at site of infection compared to minimum inhibitory concentration Time- concentration needs to be above minimum for enough time between doses
61
What are the mechanisms of action of antibiotics?
Cell wall- ruptures Cytoplasmic membrane- altered structure Nucleic acid metabolism- interfere with DNA replication or repair
62
Explain the process of antibiotic therapy
Make diagnosis Remove barriers which prevent antibiotics working Decide if therapy is needed Select best drug Administer drug at best frequency and route Test if drug has worked

Clinical Nursing Jan exam (7 decks)

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