Lecture 36 - Drugs are Poisons Flashcards

1
Q

Give an example of a nicotinic agonist and antagonist

A

Agonist: nicotine

Antagonist: d-turbocurarine

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2
Q

Give an example of a muscarinic agonist and antagonist

A

Agonist: muscarine

Antagonist: atropine

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3
Q

Give an example of a AChE inhibitor, and the source

A

Physostigmine

Calabar bean from the ordeal plant

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4
Q

What plant does nictine come from?

A

Nicotiana tobacum

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5
Q

What plant does muscarine come from?

A

Amanita muscara

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6
Q

What plant does atropine come from?

A

Atropa beladonna

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7
Q

Where does Digitalis come from?

A

Foxgloves

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8
Q

Who was the start of modern therapeutics?

What did he discover?

A

William Withering

The effects of foxglove extracts

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9
Q

Describe the mode of action of digitalis

A
  1. Inhibits Na+/K+ ATPase
  2. Na+ build up in cells
  3. Decreased Ca2+ extrusion
  4. Increased cardiac contractile force
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10
Q

What is the overall effect of Digitalis?

A

Increased cardiac force

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11
Q

What can digitalis be used for to bring about a favourable response?

A

Heart failure

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12
Q

What adverse effects can Digitalis bring about?

A

Cardiac arrythmias

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13
Q

What is ‘the right dose’

A

AKA The Therapeutic dose

More than lowest effective dose
Less than highest safe dose

Not definite: rather a continuum

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14
Q

What are the good and bad outcomes of Paracetamol?

A

Good:

  • analgesic
  • (inhibition of PG synthesis in the brain)

Bad:
- liver necrosis

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15
Q

What do we have to think about when taking paracetamol?

A

How much will relieve my headache?

At what point will i start to damage my liver?

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16
Q

What do we have to think about when taking digitalis?

A

How much will stimulate the cardiac muscle?

When will I start to get cardiac arrythmias?

17
Q

Which process brings about the positive and negative effects of digitalis?

A

Blockage of Na/K ATPase

18
Q

What is the right dose not ‘all-or-none’?

A

People are different

It is a continuum

19
Q

What are on-target and off-target effects?

A

On-target: too much of a good thing

Off-target: lack of specificity

20
Q

What is the relationship between Terfenadine and Fexofenadine?

A

Fexo. is a product of CYP metabolism of Terf.

21
Q

What is the bioavailability of Terfenadine?

A

Nearly zero

22
Q

How does grapefruit interact with terfenadine?

A
  1. Dihydrobergamottin inhibits CYP
  2. Terf not converted to Fex.
  3. Terf. now bioavailable
  4. Torsades de Pointes (tachycardia)
23
Q

Which drugs have their bioavailability increased by grapefruit juice?

A

Simvastatin

Terfenadine

24
Q

Which drugs will be affected by grapefruit juice?

A

Any drug that is metabolised by that particular CYP

25
Q

Two drugs are metabolised by the same CYP. What happens if these drugs are taken at the same time?

A

Competition for metabolism

Increased half life

26
Q

Why are selective drugs better?

A

They bring about the desired action at a much lesser concentration

27
Q

What is the ABCD of drug interactions?

A

A: augmented
B: bizarre
C: chronic
D: delayed

28
Q

Describe an example of type A ADR

A

Digitalis

Taking too much leads to cardiac arrythmias

29
Q

Describe an example of type B ADR

A

Penicillin

  • Some people have allergies to penicillin
  • idiosyncratic
30
Q

What is Type B ADR normally due to?

A

Phenotypic variation in metabolism

31
Q

Give an example of Type C ADR

A

Cocaine:

  • tolerance
  • dependence

Bex, Vincent’s
- nephropathy

Adrenal insufficiency
- when taking glucocorticoids

32
Q

What are some examples of Type D ADR?

A

Cancer

Infertility

Thalidomide use

  • Phocomelia
  • antagonist of angiogenesis in limbs
33
Q

Explain the ADR of morphine

A

A: constipation, respiratory depression
B: allergy
C: addiction
D: withdrawal

34
Q

Explain the ADR of cortisone

A

A: immunosuppresion
C: thin skin
D: adrenal insufficiency

35
Q

Which type of ADR is predictable?

A

Type A

36
Q

Who said that all drugs are poisons?

A

Paracelsus