Pharmacology 3 Flashcards

1
Q

What is meant by the term pharmacokinetics?

A
  • The process by which a drug is absorbed, distributed, metabolised and eliminated by the body
  • What the body does to drugs
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2
Q

What is meant by the term pharmacodynamics?

A
  • The branch of pharmacology concerned with the action of drugs in the physiology or pathology of the body
  • What drugs do to the body
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3
Q

What are the different phases of what happens to drugs in the body? (4 points)

A
  • Absorption
  • Clinical effect
  • Metabolism
  • Excretion
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4
Q

What is meant by the excretion of a drug from the body?

A
  • how the body gets rid of a drug
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5
Q

What are the different routes or administration for drugs into the body? (6 points)

A
  • Oral
  • Intravenous
  • Intramuscular
  • Subcutaneous (under the skin)
  • Inhalation
  • Sublingually
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6
Q

What does subcutaneous mean?

A
  • Under the skin
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7
Q

What is the advantage of giving drugs orally?

A
  • Socially acceptable
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8
Q

What are the disadvantages of giving drugs orally? (4 points)

A
  • Slow onset
  • Variable absorption
  • Gastric acid may destroy drug
  • ‘first pass’ metabolism
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9
Q

What is first pass metabolism?

A
  • The intestinal and hepatic degradation or alterations of a drug or substance taken by the mouth, after absorption, removing some of the active substance from the blood before it enters the general circulation
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10
Q

Where can first pass metabolism occur?

A
  • In the gut and in the liver
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11
Q

What are 5 factors that can affect oral absorption of drugs?

A
  • Lipid solubility and ionisation
  • Drug formulation
  • Gastrointestinal motility
  • Interactions with other substances in the gut
  • GI tract disease
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12
Q

What considerations need to be given about lipid solubility and ionisation I relation to affecting oral drug absorption?

A
  • Can only absorb a drug if it is lipid soluble

- Can’t hold it in the gut unless it is in ionic suspension (polar form)

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13
Q

What considerations need to be given about drug formulation in relation to affecting oral drug absorption?

A
  • Can give a drug that is delayed absorption
  • If the drug has a coating on it then different bits of the drug can be absorbed at different times
  • Coated bits will take longer to be absorbed as coating will take time to dissolve
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14
Q

What considerations need to be given about gastrointestinal motility in relation to affecting oral drug absorption?

A
  • If stomach is not stimulated the drug will not move through the body
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15
Q

What considerations need to be given about GI tract disease in relation to affecting oral drug absorption?

A
  • If some of the bowel is removed due to disease then you might not have enough bowel for the drug to be absorbed
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16
Q

In first pass metabolism, where does all of the blood from the GIT drain to?

A
  • The hepatic portal vein (except sublingual and rectal veins)
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17
Q

In first pass metabolism, where does the hepatic portal vein drain to?

A
  • The liver
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18
Q

In first pass metabolism, where does the drug need to pass through once before it reaches the systemic circulation?

A
  • Liver
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19
Q

In first pass metabolism, what can the liver do to drugs?

A
  • Inactivate drug = more needed by oral route to get desired clinical effect
  • Activates drug = makes an active form of an inactive drug so less in needed by oral route
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20
Q

In terms of considering drug dosage for drugs involved in first pass metabolism what is very important?

A
  • Need to consider if patient has normal or abnormal liver function
  • Especially need to consider this when treating someone with abnormal liver function as do not want to give them a dose that is too high
  • This can lead to extremes of life, liver disease or drug interactions changing drug metabolism
21
Q

What are the advantages of giving a drug through non-oral administration? (2 points)

A
  • Predictable plasma levels

- No first pass metabolism

22
Q

What are the disadvantages of giving a drug through non-oral administration? (3 points)

A
  • Allergic reactions are more severe
  • Access difficulties/self-medication
  • Drug cost is higher
23
Q

What is meant by the term ‘bioavailability’?

A
  • The proportion of a drug which enters the circulation when introduced into the body and so is able to have an active/clinical effect
24
Q

What can bioavailability to modified by? (4 points)

A
  • Dosage form
  • Destruction in the gut
  • Poor absorption
  • First pass metabolism
25
Q

What is meant by dosage form?

A

A term for the physical characteristics of a drug product - e.g. tablet, capsule or solution - which contains the drug substance and almost invariably other ingredients

26
Q

What is meant by the term ‘volume of distribution of a drug?

A

How much of the body is the drug diluted in?

  • Compartments (vascular, tissues, CNS)
  • Some drugs will go to an area of the body more easily than other areas of the body
27
Q

How are drugs distributed by lipid binding?

A
  • Slow release from accumulation
28
Q

How are drugs distributed by drugs that are binding to plasma proteins?

A
  • Bound drug is inactive (acting as a reservoir)

- Drug actions are possible by competitive binding

29
Q

What is meant by drug metabolism?

A
  • Preparing the drug for elimination from the body
30
Q

What are the 2 different phases of drug metabolism (preparing the drug for elimination from the body)?

A

Phase 1 reactions:

  • Oxidation, reduction, hydrolysis
  • Can be enough to change the conformation of the molecule and therefore the drug is inactive as it can no longer bind to the receptor
  • It might take more than one reaction for this to occur

Phase 2 reactions

  • Conjugation (the combination, especially in the liver, of certain toxic substances formed in the intestine, drugs; a mens by which the biologic activity of certain chemical substances is terminated and the substances made ready for excretion
  • Glucuronidation, sulphation, methylation, acetylation, glutathione
31
Q

What are the different ways drugs can be excreted from the body? (5 points)

A
  • Renal - urin
  • Liver - bile
  • Lungs - exhale gas
  • Sweat
  • Saliva
32
Q

What is the most common way in which drugs are excreted from the body?

A
  • Renal excretion - majority of the drug will be excreted through urine
  • Renal disease will impact on the ability for the body to get rid of the drug - so the drug will build up in the body circulation
33
Q

What are the 2 main disorders that can affect drug excretion from the body and what must we do in relation to the drug dose given to the patient?

A
  • Renal disease (chronic renal failure)
  • Liver disease (liver failure)
  • Drug doses must be reduced
34
Q

Do drugs distribute themselves evenly throughout the body?

A
  • No
35
Q

Planning drug use is based in the idea of ‘body compartments’ . What is the single compartment model?

A
  • Drug behaves as if it is evenly distributed throughout the body
36
Q

Planning drug use is based on the idea of ‘body compartments’. What is meant by two compartment model?

A
  • Drug behaves as if it is in equilibrium with the different tissues in the body
37
Q

Generally, what is the connection between blood in the tissues and the amount of drug in tissues?

A
  • More blood you’ve got in the tissue the more drug you’ve got in the tissue
38
Q

What is the plasma half-life of a drug?

A
  • How long it takes for half of the drug to be removed from the body
39
Q

What 2 things do you need to know to create a dosgae schedule for a drug?

A
  • The clearance of a drug

- The half life of a drug

40
Q

What are the 2 processes in which drug clearance can work?

A
  • First order kinetics

- Zero order kinetics

41
Q

Which order of kinetics are most drugs cleared from the body by?

A
  • First order kinetics
42
Q

What are the properties of drug clearance by first order kinetics? (3 points)

A
  • Drug elimination or absorption is by PASSIVE DIFFUSION only
  • Drug removal is proportional to the drug concentration
  • Logarithmic graph of elimination is a straight line
43
Q

What is the drug half life like in first order kinetics?

A
  • Half life is constant, from this you can predict how long it will take for the drug to be removed from the body
44
Q

What are the properties of drug clearance by zero order kinetics? (3 points)

A
  • Drug elimination is an ACTIVE process and can be saturated by high drug concentrations
  • The drug is removed from the body at a stead rate irrespective of how much drug has been consumed
  • Linear graph of drug elimination
45
Q

What is meant by drug accumulation?

A
  • How the plasma concentration builds up if repeated doses of a drug are given
46
Q

What happens if drugs are given more frequently than the drug schedule suggests?

A
  • TOO FREQUENT will result in plasma levels that may be toxic
  • Depends on the drug’s therapeutic index
47
Q

What happens if drugs are given less frequently than the dosing schedule suggests?

A
  • TOO INFREQUENT will result in sub-therapeutic plasma levels and no clinical effect
48
Q

What is meant by the therapeutic index of a drug?

A

The comparison of the amount of a therapeutic agent that causes the therapeutic effect to the amount that causes death or toxicity