Pharmacology & Drugs Flashcards

1
Q

What is it thought paracetamol inhibits the release of?

A

COX-3

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2
Q

What are the 2 route by which paracetamol is broken down?

A

98% - Glucuronic & sulphuric acids

2% P450 enzymes

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3
Q

What is the toxic substance produced by the P450 enzymatic breakdown of paracetamol?

A

NAPQ1

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4
Q

What is NAPQ1 deactivated by?

A

Glutathione

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5
Q

What is the maxium dose of paracetamol for an average adult in 24hours?

A

4g.

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6
Q

What is the half life of paracetamol?

A

2-4 hours in a health individual

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7
Q

What is the half life of a drug?

A

the time taken for drug plasma concentrations to half

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8
Q

In linear Pharmacokinetics how many half lives does it take to clear a drug?

A

4-5

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9
Q

What does Pharmacokinetics involve?

A

Administration
Distribution
Metabolism
Excretion

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10
Q

Whats the biggest difference between enteral and parental administration?

A

Parental by-passes liver metabolism

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11
Q

What is the bio-availability of a drug?

A

The percentage of the drug that enters systemic circulation

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12
Q

What is volume of distribution?

A

The apparent volume of drug in a given amount of plasma. The drug dose must first be known. - “If i give this much, how much will be in blood plasma of a given volume”

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13
Q

What is drug clearance?

A

The theoretical amount of drug eliminated from plasma/ unit time

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14
Q

What are the THREE mechanism by which bacteria use to be resistant to antibiotics?

A

Mutation of target site
Inactivating enzymes - Beta Lactase
Limiting access - increased reflux of the antibiotic

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15
Q

What are the THREE main ways antibiotics are used?

A

Guided therapy
Empircal Therapy
Prophylactic therapy

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16
Q

What kind of antibiotics are used in guided therapy?

A

narrow spectrum

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17
Q

What kind of antibiotics are used in empirical therapy?

A

Broad spectrum

18
Q

What are ideal characteristics are wanted in antibiotics?

A

Highly toxic to bacteria
Able to easily access the required area in the body
Able to neutralise the toxins of the bacteria
Easily Administered
Limited co-lateral damage to the patient
Limited damage to comensal bacteria

19
Q

What are the Four main target areas of antibiotics?

A

Peptoglycan wall - Penicillin, glycopepitides
DNA - quinolones
Ribosomes - Macrolides, Aminoglycosides
Metabolism - Trimethoprim

20
Q

How do Beta lactams works?

A

The structure of the Beta lactam is almost identical to the final structure of the peptoglycan wall synthesis - called the transpepidase protein - thus inhibiting cross linking of the peptides

21
Q

What resistance is present to beta lactams?

A

Mutations in penicilin binding protein
Change in porins allowing access to the bacteria
Productions of beta lactamases

22
Q

What can be given in combination with penicillin to inhibit beta lactamases?

A

Beta lactamases inhibitors - co-amoxiclav

23
Q

Example of a glycopeitides?

A

Vancomyocin

24
Q

What is vancomyocin used to treat and what can’t it treat and why?

A

MRSA.

it can’t treat gram-negative because it can’t cross cell membranes

25
Q

What are common/ dangerous sides of Beta Lactams?

A
Type I hypersensitivity reactions 
Type IV - this is dangerous and delayed 
Diarrhea
Liver dysfunction 
Secondary infection - C.Diff, Thrush
26
Q

What are macrolides useful for?

A

They are good at entering cell, therefore if there is a bacterial infection intraceullular infection they are useful. Used alot in upper respiratory infections

27
Q

What is used to break down Macrolides?

A

CYP 3A4

28
Q

What do Aminoglycosides inhibit?

A

30S ribosomes, inhibiting protein synthesis

29
Q

Abatacept function?

A

Blocks T cell activation

30
Q

Tocilizumab function?

A

Blockage of IL-6

31
Q

What is the loading dose?

A

The initial dose giving to bring the concentration up the therapeutic dose

32
Q

What is the loading dose calculation?

A

Volume of distribution x target concentration

33
Q

What is the maintenance dose?

A

The dosing to keep the wanted concentration constant

34
Q

what is the maintenance dose calculation?

A

Clearance rate x target dose

35
Q

If a drug has a low volume of distribution, will more or less drug be needed and why?

A

less - because more remains in the plasma as opposed to other compartments

36
Q

What is Emax?

A

It is the maximum efficacy of the drug - its maximum stimulus.
we presume the receptors are fully saturated here.

37
Q

What is E50? and how does it relate to potency?

A

The concentration that the drug is at when it reaches half its maximum efficacy (Emax).
the lower the E50 the more potent the drug as it reaches a the stimulus at lower concentrations

38
Q

Give an example of a bacterial-static antibiotic.

A

Clarithromyocin

39
Q

What antibiotic would cause the adverse effect of red man syndrome?

A

Vancomyocin

40
Q

What are the two beta lactamase inhibitors that be co-given with antibiotics?

A

Clavulanic acid

Tazobactam

41
Q

Name a reversible Nicotine receptor antagonist

A

Atracurium