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4th yr- CMS- drugs and medication > Commonly prescribed analgesic > Flashcards

Commonly prescribed analgesic Flashcards

1
Q

What are commonly prescribed analgesics Called

A

Non steroidal anti inflammatory drugs (NSAIDS)

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2
Q

What do we need to consider before prescribing NSAIDS

A
  1. Drug interactions

2. Patient factors

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3
Q

What is the major ode of action of NSAIDS

A

Inhibition of the cyclo-oxygenase enzymes 1 and 2 to reduced prostaglandin synthesis

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4
Q

Talk through the synthesis of prostaglandins

A 
1. Phospholipid 
(Phosphlipase)
2. Arachidonic acid
(Cyclic oxygenase COX1, COX2)
3. Cyclic endopeloxides PGG2
(Cyclo oxygenase)
4. prostaglandin
5. PGE2, PGD2, PGF2,
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5
Q

What do prostaglandins produce

A
  1. Analgesic actions
  2. Antipyretic action
    3Inflammatory actions
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6
Q

Name the 2 Cyclic oxygenase enzymes

A

COX1

COX2

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7
Q

Describe COX 1

A
  1. It is constitutionally active
  2. Expressed in many tissues eg kidneys, blood vessels, stomachs
  3. Unwanted/ adverse affects of NSAID are predominately down to COX 1
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8
Q

Describe COX 2

A

Is an inducible enzyme inducted by inflammatory cells

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9
Q

The unwanted effects of NSAIDS are due to which COX enzyme

A

COX1

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10
Q

What do several prostaglandin make

A

Nociceptors that response to mediators such as 5-HT, bradykinin

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11
Q

How are NSAIDS effective painkillers

A

They stop prostaglandin synthesis

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12
Q

Talk through the antipyretic effect of NSAIDS

A
  1. Bacteria leads to infection in a healthy body
  2. Bacterial toxin released
  3. Macrophages activated
  4. NSAIDS block COX2 metabolised PG synthesis
  5. This returns the body back to normal rather than pyrexia occurring
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13
Q

What is pyrexia

A

Body temperature greater than 38

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14
Q

What are the anti inflammatory effects of NSAIDS

A

COX-2 inhibition of prostaglandins synthesis leads to:

  1. Less vasodilaiton
  2. Less tissue oedema
  3. Less sensitisation of nociceptors
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15
Q

What does less vasodilation lead to

A

Reduced flushing and reduced redness of skin

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16
Q

What do we mean by less tissue oedema

A

Reduced swelling

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17
Q

What do we mean by less sensitisation of nociceptors

A

Analgesia

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18
Q

Name the most common NSAID agents

A
  1. Salicylates e.g. aspirin
  2. Paracetamol
  3. Proprionic acid derivatives EG ibuprofen, naproxen
  4. Selective COX-2 inhibitors
  5. Enoic acids
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19
Q

What is aspirin made of

A

acetylsalicylic acid

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20
Q

Give examples of Proprionic acid derivatives

A

Ibuprofen

Naproxen

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21
Q

What is the half life of ibuprofen

22
Q

What is the half life of naproxen

23
Q

why might we prefer Proprionic acid derivatives over aspirin

A

As Proprionic acid derivatives are better tolerated in regards to gastrointestinal effects

24
Q

Give examples of selective COX-2 inhibitors

A

etoricoxib,
celecoxib,
parecoxib

25
When are selective COX-2 inhibitors used
most commonly prescribed in Rheumatology
26
Give example of Enoic acids NSAIDS
piroxicam, meloxicam, ketorolac, diclofenac
27
Aspirin and ibuprofen selectively inhibit which form of COX
Weakly COX-1 Selective
28
How does aspirin work
It binds irreversibly to COX-1 hence the effects outlasts presence of the drug
29
Diclofenac selectively inhibit which form of COX
Weakly COX-2 selective
30
Celecoxib selectively inhibit which form of COX
Moderately COX-2 selective
31
Etoricoxib selectively inhibit which form of COX
Very COX-2 Selective
32
How does paracetamol work
It is a reversible non competitive COX inhibitor
33
What is paracetamol effective against
Pain relief and anti pyretic actions
34
What are gastrointestinal effects of NSAIDS
1. Dyspepsia 2. Nausea 3. Gastritis 4. Intestinal damage 5. Bleeding 6. Oral ulcerations
35
what are the bleeding risks of NSAIDS
1. Anti platelets activity exacerbates gastrointestinal bleeding 2. Increased risk of thrombotic effects eg MI or stroke
36
What other side effects may NSAIDS have
1. May have irritant effect on skin or mucosa 2. Skin rashes 3. Bronchospasm 4. Nephritis and papillary necrosis
37
What does aspirin overdose have an impact on
Acid base balance
38
What can changes in acid base balance lead to
respiratory alkalosis or respiratory and metabolic acidosis
39
What can overdose of aspirin cause
1. Hyperpyrexia 2. Nausea and vomiting 3. Vertigo, tinnitus and haring impatient
40
What is Hyperpyrexia
Body temperature of 40 plus
41
What is reyes syndrome
A syndrome present in children given aspirin for viral infections to lower their high temper
42
What is the mortality rate for reyes syndrome
20-40%
43
How do we avoid reyes syndrome
Never prescribe aspirin for those under the age of 16
44
Above what dose can paracetamol start causing problems
A dose of 10-15g
45
What is the maximum dose of paracetamol for a Healthy adult
1g per day in 4 divided doses
46
What are the major side effects of paracetamol overdose
Severe liver damage
47
How does liver damage manifest as a consequence of paracetamol over dose
Hepatitis which can be severe enough to end in acute liver failure and death
48
What is the toxic metabolite produced as a consequence of paracetamol overdose
N-acetyl-p-benzoquinone
49
Why is N-acetyl-p-benzoquinone toxic
There is limited capacity for the body to remove this
50
How is N-acetyl-p-benzoquinone toxic usually metabolised
In conjugation with GLUTATHIONE
51
What are paracetamol overdose patients given
given IV N-acetylcysteine or PO methionine to increase glutathione production to mop up the excess toxic metabolite

4th yr- CMS- drugs and medication (4 decks)

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