Pharmacology exam Flashcards

1
Q

What is pharmacokinetics

A

What the body does to a drug

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2
Q

What are the stages of drug action

A

ADME

Absorption
Distribution
Metabolism (not all drugs are metabolised)
Excretion

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3
Q

List factors that affect Absorption

A

Contact time
Surface area
Blood flow

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4
Q

Particles move from high concentration to low concentration

A

Diffusion

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5
Q

What are the two types of absorption

A

Physiological

Physio-chemical

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6
Q

Physico-chemical factors affecting absorption

A

SLIC

Solubility- how soluble the drug is in the body fluids

Lipid to Water Partition Coefficient - is it more fat soluble than water soluble

Ionisation - degree of chemical charge

Chemical Stability - will it break down readily

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7
Q

Distribution into body fluids are mainly

A

Extra cellular
Intracellular
Plasma

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8
Q

Uptake of drugs into different body tissues depends on

A

Blood flow
Tissue mass
Lipid to Water Partition Coefficient

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9
Q

Time to onset

A

The time it takes for a drug to reach its site of action at a concentration necessary for it to work

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10
Q

Duration of effect

A

The time interval where the concentration of a drug at the site of action is above its therapeutic concentration - may be prolonged in the elderly or people with poor liver or kidney function

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11
Q

Half life

A

The time it takes for the peak concentration of a drug in the plasma to reduce by half

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12
Q

First pass metabolism

A

When a drug is completely destroyed in the stomach before being absorbed or when it is metabolised by the liver before reaching the systemic circulation

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13
Q

Clearance

A

A measurement of a persons ability to metabolise and excrete a drug or how quickly a drug is cleared from the blood - affected by renal function, blood pressure, and urine PH

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14
Q

Key principles of pharmacodynamics =

The four drug body actions are

A

RITE
Receptor = agonist and antagonist

Ion Channel = blockers and modulators

Transport system interactions

Enzyme= inhibitor, false substrate and pro-drug

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15
Q

What are receptors

A

Sensing element in a system of chemical communication that coordinates the function of all the different cells in the body

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16
Q

Name the four main types of receptors

A

Ligand gated ion Chanel
G -proline receptor
Kinase-linked receptor
Nuclear Receptors

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17
Q

What is a Ligand

A

A chemical or drug that binds to a receptor

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18
Q

What is a G- protien

A

G- proteins are found within the cell, are linked to the receptor and activate after drug molecule binding

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19
Q

How does a kinase linked receptor work

A

Kinase linked receptors produce a cascade of events after drug binding that lead to an action

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20
Q

What is a nuclear receptor

A

Nuclear receptors are located WITHIN the cell nucleus and require the drug molecule to cross the nuclear membrane

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21
Q

Explain G - protein receptors

A

Use proteins to link to receptors in the cell membrane
EG. Salbutamol acts on
Adrenoseptors and histamine receptors in the bronchioles

22
Q

Give an example of a drug that exerts its effect using kinase linked receptor

23
Q

Give an example of a drug that exerts its effect via nuclear receptor

A

Levothyroxine and prednisolone

24
Q

What is an agonist

A

A drug that binds to a receptor and causes a response

Eg; many hormones neurotransmitters and drugs act as agonists - such as ventolin a beta 2 agonist activates beta cells that relax the smooth muscle of airways in the treatment of asthma

25
What is an antagonist
A drug that binds to a target receptor and effects no response or blocks a response they bind to the same site that an agonist usually occupies thereby preventing an action
26
State the two classifications of adverse drug reaction
Type A - augmented and Type B- Bizarre
27
List four strategies used by a NMP to reduce the likelihood of ADRs
Prescribe as few drugs as possible Prescribe known or familiar drugs Reduce polypharmacy if possible by regular medication review Check for allergies an previous ADRs Prescribe only if there is good indication Simplify drug regimens or arrange to fit in with patients current medication times Regular reviews to monitor drug response/side effects
28
Discuss your understanding of concordance
Factors affecting pt concordance BNF p1 Purpose of medication not clear Perceived lack of efficacy Real or perceived adverse effects Instructions for administration not clear Physical difficulty in taking the medicines eg swallowing tablets, handling small tablets, opening containers Unattractive formulations eg unpleasant taste or route Complicated regime
29
Give example of a drug that undergoes extensive fist pass metabolism and the implication for route of administration
Insulin if given orally would be metabolised in the GI or liver and therefore greater bioavailability is achieved by subcutaneous route
30
Define drug interactions
A pharmacokinetic drug interaction when one drug alters the absorption, protein binding,metabolism or excretion of another leading to altered bioavailability altering its pharmacological effect Eg magnesium reduces absorption of iron
31
Steady state
When a drug going in to the body= drug going out of the body - achieved after 5 half lives
32
Bioavailability
The fraction or percentage of an administered drug that reaches the systemic circulation after absorption unless given IV where it is 100% of the given dose
33
Polypharmany
Four or more medications
34
Adverse drug reaction
Unwanted or unintended effect Side effect = tolerable But if you need to stop drug it’s classed as an ADR
35
Prescribing in the elderly
``` Decreased drug metabolism and excretion Altered sensitivity of some target organs Multiple pathologies Drugs with narrow therapeutic index Poor compliance Polypharmacy ```
36
List goals of a medication review
``` NOTEARS Need + indication Open questions explore pt perceived problems, compliance, and pt opinion of effectiveness Test and monitoring Evidence + guidelines Adverse events Risk reduction + prevention Simplifications and switches ``` Reach agreement with pt and review changes
37
Explain why knowledge of a pts renal function is essential before prescribing a drug which is heavily excreted by the kidney
``` BNF p19 Toxicity Sensitivity Increased side effects Reduced efficacy ```
38
What factors can affect the ONSET of drug action, Relate this to pharmacokinetics
Absorption Distribution Metabolism (prodrug)
39
What factors can affect the DURATION of a drug action, relate this to pharmacokinetics
Metabolism | Elimination
40
Briefly outline the mechanisms by which the liver metabolise and eliminate drugs and the need for knowledge of liver function prior to prescribing and implications for elderly patients
Liver - phase 1 (oxidation, reduction, hydrolysis) phase 2 (conjugation) metabolism to make drugs more water soluble Must know the LFT results as the liver may not be working as well as expected leading to the concentration in the blood being higher and drug doses need to adjusted accordingly. Especially important in the elderly who have reduced liver function
41
Briefly outline the mechanism by which the kidneys eliminate drugs, the need to know kidney function prior to prescribing and implications for elderly patients.
Kidney - glomerular filtration, active tubular secretion, distal reabsorption. Drug goes in the renal tubule and is excreted in urine. Must know the GRF results as the liver may not be working as well as expected leading to the concentration in the blood being higher and drug doses need to adjusted accordingly. Especially important in the elderly who have reduced liver function
42
Plasma proteins can affect drug distribution. Name a plasma protein and a drug that is extensively plasma protein bound. Discuss their role in binding drugs and affecting their availability for pharmacodynamic action
Albumin is a plasma protein. Drugs bound to plasma protein are pharmacologically inert and do nor reach their site of action. This may mean the oral dose if far greater than needed due to the bioavailability being reduced due to the plasma protein binding. They may also be displaced by other drugs from their binding sites. Implications for pts with altered plasma protein = elderly, pregnant and malnourished pts.
43
Interactions can be described as pharmacokinetic and pharmacodynamic. explain what is meant by this and give examples of each.
Pharmacodynamic- drugs with similar antagonistic actions and influence each other’s effects. Digoxin acts on cardiac fibres and its effects in crease if there are low levels of potassium in the blood. Frusemide is a diuretic and favours the loss of potassium when lowering the tension in the arteries. The concomitant effect can lead hypokalaemia which could result in digoxin toxicity Pharmacokinetics- interaction affecting ADME Example metoclopramide may accelerate gastric emptying and decrease the absorption of digoxin.
44
Advantages and disadvantages or giving medication via the oral route
Easy Preferred by patients Slow release preparations may be available to extend duration of action Drugs can be formulated in such a way as to protect them from digestive enzymes - acid etc Unsuitable for pts who are uncooperative, swallowing issues or strictly nil by mouth Most oral medications are absorbed slowly Unpredictable absorption due to degradation by stomach acid and enzymes
45
Advantages and disadvantages of iv route
Dependable and reproducible effects 100% of dose reaches systemic circulation immediately and dose accurately titrated against response Requires functioning cannula More expensive and labour intensive than other routes Cannulation distressing especially in children Iv injection of drug may cause local reaction
46
Explain enzyme inhibitors
Attaches to an enzyme , stops it from working and decrease enzyme related process, enzyme production or enzyme activity.
47
Explain enzyme inducers
Increase the activity of an enzyme other by binding to it or activating it carbamazepine is a liver enzyme inducer and increases the rate of elimination of the contraceptive pill
48
Ion channel
Channel in a cell membrane where ions such as sodium can pass, target for drug action
49
Prescribing a drug with the words schedule 4 next to it in the BNF what does this mean for you as a prescriber
It’s a controlled drug It’s a schedule 4 preparation It’s subject to controlled drug prescription writing requirements Prescription valid for 28 days only 30 days max supply best practice due to abuse potential
50
You are prescribing a drug in your personal formulary when you notice a black triangle appearing next to it in the BNF, what does this mean for you as prescriber
It’s a newly licensed medicine It’s a drug with limited experience of use You must report ALL suspected ADRs
51
What is a pro drug
Inactive drug that is metabolised into an active compound Codeine is a pro drug metabolised by the liver and it’s metabolite is morphine Might not be activated in pts with liver impairment as the enzymes are not there to activate it therefore drug action delayed
52
Half life
Time it takes for the concentration of a drug in the plasma to be reduced by half Elimination takes 4-5 half lives Steady state - requires a consistent level of drug in the body (In = Out) Therefore kidney impairment will reduce excretion allowing concentration to increase in the blood (?toxicity)