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V300 > Masterclass > Flashcards

Masterclass Flashcards

Overall revision of suggested questions from UOB.

1
Q

What is pharmacokinetics?

A

The way in which the body affects the drug.
Movement of drugs within the body and how the body affects the drug with time.

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2
Q

What are the processes involved in pharmacokinetics?

A

ADME
Absorption
Distribution
Metabolism
Excretion

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3
Q

What is absorption?

A

The process by which a drug gets absorbed into the systemic circulation.

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4
Q

What factors can affect absorption?

A
  • Blood flow to site of absorption.
  • Route of administration.
  • Drug solubility.
  • PO: Food/stomach pH/GI motility.
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5
Q

What is distribution?

A

The process by which drugs move from the bloodstream into different tissues/organs in the body to act at receptor sites.

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6
Q

What can affect distribution?

A
  • Blood flow.
  • Plasma protein binding.
  • Drug solubility.

2) Only unbound drugs can move into tissues/organs.
3) Lipid-soluble drugs can distribute into fat-rich tissue however water-soluble prefers to stay in watery areas like blood.

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7
Q

What is metabolism?

A

The process by which the body breaks down the drug to form metabolites. They can be:
1) Inactive
2) Equally or more active

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8
Q

What are the 2 phases of metabolism?

A

1) Oxidation/Hydrolysis: Usually involves CYP450 enzymes.
2) Conjugation of phase 1 metabolite: To help elimination.

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9
Q

Explain the first pass effect?

A

The metabolism of a drug and its passage from the liver into the circulation.
Orally: Drugs given orally may be extensively metabolised by the liver before reaching the systemic circulation.
IV: Drugs given IV bypass this process therefore more drug reaches circulation.

Explains why doses are changed for PO vs. IV.

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10
Q

What factors can affect metabolism?

A
  • Blood flow to the liver.
  • Hepatic impairment.
  • Genetic variations affecting enzyme systems.
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11
Q

What is excretion?

A

The process by which the body clears the drug usually by the kidneys via urine.
Can also be excreted by sweat, the bilary system and faeces.

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12
Q

What factors can affect excretion?

A

Blood flow to kidneys.
Kidney function.
Urine flow.

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13
Q

What is pharmacodynamics?

A

What the drug does to the body.

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14
Q

Explain bioavailability…

A

The extent the drug reaches systemic circulation and is able to act on its receptor site. E.g., IV route bypasses first pass-metabolism. 100% bioavailiability.

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15
Q

Explain the term ‘onset’?

A

The time taken for a drug to elicit a therapeutic response.

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16
Q

Explain the term ‘peak’?

A

The time taken for a drug to maximal response.

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17
Q

Explain the term ‘duration’?

A

The time a drug concentration is sufficient to elicit a therapeutic response.

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18
Q

What is the lock and key hypothesis?

A

Drug = Key
Lock = Receptor
Door Open = Biochemical or electrical signal to exert an effect
E.g., Oxytocin (key) acts on receptors (locks) within the uterus causing the muscles to contract and progress labour.

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19
Q

What is affinity?

A

Strength of an interaction between a drug and it’s receptor.

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20
Q

Drugs are usually transported by binding to proteins.
Name 4 protein targets….

A

Receptors: trigger or block
Ion Channels: flow in/out
Carrier Proteins: movement of molecules across cell membranes
Enzymes: inhibit/enhance

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21
Q

Outline 3 reasons that proteins make good targets for drugs?

A

Specificity: Drugs can be designed to interact with specific proteins to produce a specific response.
Physiological response: proteins are involved so they can be targetted for therapy.
Drug-protein: interactions can via various mechanisms e.g., RICE.

22
Q

What is an agonist?

A

A drug that binds to a cell receptor and produces a response.

23
Q

What is a partial agonist?

A

A drug that produces a less than maximal response.

24
Q

What is an antagonist?

A

A drug that binds to a receptor but does not produce a response and opposes action of agnonists.

25
Q

What is a partial antagonist?

A

Same as a partial agonist but it also acts as a antagonist by competing for receptor sites in the prescence of full agonists.

26
Q

Explain ‘efficacy’?

A

Ability of a drug to produce a maximal affect after binding to it’s receptor.

27
Q

Explain ‘potency’?

A

Amount of drug required to produce a response.

28
Q

What is ‘down-regulation’?

A

Continuous exposure to an agonist = receptors reduce in number and desensitise.

29
Q

What is ‘up-regulation’?

A

Cell receptors increase due to lack of stimulation by agonist or exposure to antagonist.

The cell compensates for reduced signaling to maintain normal function.

30
Q

Why can salbutamol cause tachycardia?

A

Salbutamol is a β2 agonist and targets receptors in the bronchioles in the
lungs to cause bronchodilation.
BUT not specific: can also bind to
β1 receptors in heart and produce the same effect as adrenaline. This causes
tachycardia.

31
Q

What is the key difference between an ion channel and a carrier protein?

A

A carrier protein requires energy in the form of ATP to transport ions across
membranes. An ion channel does not- passive.

32
Q

Explain what occurs during phase 1 and phase 2 of metabolism undertaken
by Cytochrome P450 enzymes?

A

Phase 1: Oxidation/hydrolysis by Cytochrome P450 enzymes.
Phase 2: Conjugation of metabolites/drug to make the drug more water-soluble to enable elimination via the kidneys.

Conjugation = attaching of chemical group to drug/metabolite.

33
Q

What is the role of plasma proteins in drug distribution?

A

Plasma proteins control how much of the drug stays in the bloodstream and how much is free to distribute into tissues and take action. Only unbound/free drug can act on receptor sites. Drugs extensively bound to proteins will have a low Vd.

34
Q

What is meant by the “therapeutic range” of a drug? Give an example of a
common drug with a narrow therapeutic range.

A

The difference between a drug having the right affect and a toxic affect.
Gentamicin
Warfarin
Digoxin
Lithium

35
Q

Describe the 4 different types of enzyme inhibition?

A

Reversible
Irreversible
Competitive
Non-Competitive
RICN

36
Q

Explain how Serotonin Selective Reuptake Inhibitors (SSRIs) work?

A

They block the reuptake of serotonin in the brain, which increases the amount of serotonin available to pass messages between nerve cells.

37
Q

List 5 points of a good drug history.

A

POPAA
Prescribed
Other (OTC/herbal)
Past
Allergies
Adherence

38
Q

Renal impairment.

A

Clear, Dose, Monitor, Avoid, Alternate
Clearence of drug.
Start low, go slow.
Monitor patient.
Avoid drugs = toxicity.
Use an alternative.

39
Q

Hepatic impairment.

A

Clear, Dose, Monitor, Avoid, Alternate
Clearence of drug.
Start low, go slow.
Monitor patient.
Avoid drugs = toxicity.
Use an alternative.

40
Q

When the amount of drug excreted equals the amount being absorbed, the condition is called:

A

Steady-State

41
Q

The time taken for the concentration of a drug to fall to half its original level
is called:

A

Half-life

42
Q

Drugs administered orally can be subject to first-pass effect which is:

A

The metabolism of a drug by the liver before the drug has become availiable for use.

43
Q

What factors can affect bioavailability?

A
  • Route.
  • Plasma-protein binding.
  • Drug solubility.
  • Prescence of other drugs that induce or inhibit metabolism.
44
Q

What does half-life depend upon?

A

Volume of distribution.
Elimination.

45
Q

What is volume of distribution?

A

How widely a drug spreads throughout the body after entering the bloodstream. How much will stay in the blood vs. how much will move into tissues.

46
Q

What are the legal implications you need to be aware of in your prescribing practice? List 5 implications.

A

DOC
Consent
Confidentiality/GDPR
Mental Capacity
Pharmaceutical Industry

Welcome to the DCC….

47
Q

Name 10 things that a prescriber must complete on a prescription, in order for it to be valid and legal.

A

Patient: Name, address, DOB, age.
Prescriber: Name, address, contact details, type of prescriber, NMC no.
Drug: Name, strength, frequency, preparation, route, course length.
DATE

PPDD

48
Q

State at least five factors that may be assessed when obtaining a drug history. For each of these factors explain its importance.

A

Past
Other (illegal, herbal, OTC)
Prescribed
Allergies
Adherence

POPAA

49
Q

Explain how H2 receptor antagonists work in the prevention of GORD?

A
  • Block H2 receptors in gastric muscosa.
  • Histamine triggers secretion of HCL thus by blocking = less HCL.
  • Less HCL = less irritation, inflammation and increased healing.
50
Q

Explain how PPI’s work in the prevention of GORD.

A
  • Block H+/K+/ATPase enzyme (PP) in gastric parietal cells.
  • H+ plus CL = HCL thus by blocking = less HCL.
  • Irreversibly inhibited = long acting.

V300 (2 decks)

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