Immunosuppressants - DMARD, Aminosalicylic acid

Question 1

Sulfasalazine and Mezaline are DMARDs.

• Sulfasalazine = RA and colitis
• Mezaline = colitis (1st choice)

Recognised as aminosalicylic acid due to their 5-aminosalicylic acid (5-ASA) linked to sulfapyridine through an azo bond. Is Sulfasalazine a pro or active drug?

Answer 1

• pro-drug

Reduced by bacterial enzyme azoreductase to its two components, sulfapyridine and 5-ASA

Mesalazine is a 5-aminosalicylic acid, so produced following the reduction of Sulfasalazine

Question 2

Although the exact mechanism of action is not understood in Sulfasalazine and Mezaline, which 2 of the following properties are they supposed to have?

1 - anti-inflammatory
2 - immunosuppressive
3 - COX-1 and 2 inhibitors
4 - immunoglobulin inhibitors

Answer 2

1 - anti-inflammatory
2 - immunosuppressive

Question 3

Sulfasalazine and Mezaline are DMARDs.

• Sulfasalazine = RA and colitis
• Mezaline = colitis (1st choice).

Do these drugs act systemically or topically in the GIT?

Answer 3

• topically in the GIT

Mesalazine is 1st line in colitis as the sulfapyridine released during the reduction of Sulfasalazine can cause side effects

Question 4

Sulfasalazine, a DMARDs is a prodrug that when reduced forms two components, sulfapyridine and 5-ASA. Which of these is the active component that has effects in RA?

Answer 4

• sulfapyridine

Caused side effects in colitis, but is affective in RA

Question 5

What is a typical dose of Sulfasalazine?

1 – 500mg to 3g/day
2 - 1g/day
3 - 3-6g/day
4 - 10-100mg/day

Answer 5

1 – 500mg to 3g/day

Question 6

Which of the following is NOT anindication for the use of Sulfasalazine according to the BNF?

1 - RA
2 - severe ulcerative colitis and
3 - active Crohn’s disease
4 - non-Hodgkin’s lymphoma

Answer 6

4 - non-Hodgkin’s lymphoma

Question 7

Which of the following is NOT a common adverse effect of Sulfasalazine and Mezaline?

1 - GI upset
2 - leukopenia
3 - nephrotoxicity
4 - thrombocytopenia
5 - hepatotoxicity
6 - headaches

Answer 7

5 - hepatotoxicity

Question 8

Sulfasalazine and Mezaline, both have side effects, but more so in Sulfasalazine. In men which 2 of the following can Sulfasalazine cause?

1 - seizures
2 - oligospermia
3 - serious hypersensitivity reaction
4 - seizures

Answer 8

2 - oligospermia
3 - serious hypersensitivity reaction

Question 9

Sulfasalazine has been described as having idiosyncratic reactions. Which of the following is NOT one of these idiosyncratic reactions linked with Sulfasalazine?

1 - hypersensitivity
2 - skin reactions (SJS, TEN)
3 - seizures
4 - agranulocytosis
5 - hepatitis
6 - aplastic and haemolytic anaemia

Answer 9

3 - seizures

• aplastic anaemia = RBC production stops
• haemolytic anaemia = RBCs destroyed quicker than made
• Stevens-Johnson syndrome (SJS) = <10% skin affected
• Toxic epidermal necrolysis (TEN) = >30% skin affected

Question 10

If a patient has taken Sulfasalazine and has had idiosyncratic reactions previously, can they take this in the future?

Answer 10

• no

Permanent cessation of reaction of this drug

Question 11

Prior to starting Sulfasalazine, which of the following should be screened for?

1 - glucose-6-phosphate dehydrogenase (G6PD) deficiency
2 - anti-phospholipid syndrome
3 - gilbert syndrome
4 - SLE

Answer 11

1 - glucose-6-phosphate dehydrogenase (G6PD) deficiency

G6PD is important for maintaining glucose levels in RBCs, without it RBCs are haemolysed