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sulfasalazine

Sulfasalazine (or sulfasalazopyridine) is a drug belonging to the class of sulfonamides (antibacterial chemotherapy).

However, sulfasalazine is not used as an antibacterial, but as an anti-inflammatory drug.

Sulfasalazine - Chemical Structure

In fact, once taken orally, sulfasalazine undergoes reductive metabolism by intestinal bacteria and is converted into sulfapyridine (an antibacterial sulfonamide) and into 5-aminosalicylic acid (or 5-ASA, also known as mesalazine), a non-steroidal anti-inflammatory drug (or NSAID).

Therefore, sulfasalazine is considered a prodrug.

Indications

For what it uses

The use of sulfasalazine is indicated for:

  • Treatment of mild to moderate ulcerative colitis;
  • Adjunctive therapy in the treatment of severe ulcerative colitis;
  • Prevention of relapses of ulcerative colitis;
  • Crohn's disease;
  • Rheumatoid arthritis.

Warnings

During sulfasalazine therapy, cases of serious infections (including pneumonia and sepsis) related to myelosuppression (bone marrow suppression) have been reported. Therefore, if any kind of infection develops, treatment with sulfasalazine should be immediately suspended.

Before starting treatment with sulfasalazine and for the entire duration of the treatment, regular checks of liver and kidney function and blood crasis must be performed.

Sulfasalazine should not be given to patients with hepatic and / or renal dysfunction and / or with blood dyscrasias.

Caution should be exercised when administering sulfasalazine in patients with bronchial asthma or severe allergies.

If any type of allergic reaction occurs, treatment with sulfasalazine should be stopped immediately and the doctor should be contacted immediately.

The use of sulfasalazine in children with juvenile systemic onset arthritis can promote the onset of serum disease, therefore, the drug should not be used in this category of patients.

Patients who lack the enzyme glucose-6-phosphate dehydrogenase - and who are on sulfasalazine therapy - should be carefully monitored because of the risk of developing haemolytic anemia.

Since sulfasalazine can cause crystalluria and kidney stones, it is good to take plenty of fluids during treatment with the drug.

Sulfasalazine can give the urine and skin a yellow-orange color.

Due to the presence of the salicylic derivative (5-ASA), when sulfasalazine is administered to patients already on therapy with anticoagulant drugs, constant medical checks must be performed.

Interactions

Sulfasalazine can reduce the absorption of folic acid and digoxin (a drug used to increase the strength of contraction of the heart).

Sulfasalazine may interfere with drugs used in the treatment of goiter, with certain types of diuretics and with oral hypoglycemic agents .

Concomitant administration of sulfasalazine and thiopurine or aziatropine increases the risk of onset of myelosuppression.

Concomitant administration of sulfasalazine and methotrexate for the treatment of rheumatoid arthritis may increase the risk of developing gastrointestinal side effects.

In any case, it is still advisable to inform your doctor if you are taking - or have recently been taken - drugs of any kind, including over-the-counter drugs and herbal and / or homeopathic products.

Side effects

Sulfasalazine can induce various types of side effects, although not all patients experience them. This is due to the different sensitivity that each person has towards the drug. Therefore, it is said that the adverse effects do not occur all with the same intensity in each individual.

Below are the main side effects that can occur during treatment with sulfasalazine.

Myelosuppression

Treatment with sulfasalazine may induce myelosuppression which can lead to:

  • Leukopenia, ie the decrease in the number of white blood cells in the bloodstream, with consequent increased susceptibility to the contraction of infections;
  • Plateletopenia, or the decrease in the number of platelets in the bloodstream, with consequent increased risk of the onset of abnormal bleeding and / or bleeding;
  • Agranulocytosis, ie the decrease in the number of granulocytes in the blood;
  • Aplastic anemia;
  • Hemolytic anemia;
  • Megaloblastic anemia;
  • Hypoprothrombinemia, a blood disorder characterized by a prothrombin deficiency with consequent bleeding defects;
  • Methaemoglobinaemia.

Allergic reactions

Sulfasalazine can cause serum sickness, angioedema and anaphylaxis in sensitive individuals.

Infections

Sulfasalazine therapy may favor the development of infections that can lead to aseptic meningitis or pseudomembranous colitis.

Nervous system disorders

Treatment with sulfasalazine may cause:

  • Headache;
  • Migraine;
  • Dizziness;
  • Alterations in the sense of taste;
  • Peripheral neuropathy;
  • Odor alterations;
  • Encephalopathy;
  • Ataxia;
  • Convulsions;
  • Transient lesions of the spine;
  • Transverse myelitis.

Psychiatric disorders

Sulfasalazine therapy can cause insomnia, hallucinations and depression.

Cardiac disorders

Treatment with sulfasalazine may cause pericarditis and allergic myocarditis.

Gastrointestinal disorders

During sulfasalazine therapy, the following may occur:

  • Nausea;
  • He retched;
  • Abdominal pain;
  • Diarrhea;
  • Aggravated ulcerative colitis;
  • Pancreatitis;
  • Stomatitis;
  • Mumps;
  • Heartburn.

Lung and respiratory tract disorders

Treatment with sulfasalazine may cause:

  • Cough;
  • Dyspnoea;
  • Oropharyngeal pain;
  • Eosinophilic infiltration;
  • Interstitial lung disease;
  • Pulmonary fibrosis.

Infertility

Sulfasalazine therapy can cause oligospermia and infertility in men. Generally, this effect is temporary and regresses after a few months from the end of the treatment.

Skin and subcutaneous tissue disorders

Treatment with sulfasalazine may cause:

  • Itch;
  • Urticaria;
  • Alopecia;
  • Purple;
  • Drug rash with eosinophilia and systemic symptoms (DRESS syndrome);
  • Stevens-Johnson syndrome;
  • Toxic epidermal necrolysis;
  • Rash;
  • Exfoliative dermatitis;
  • rashes;
  • Photosensitization reactions.

Hepatobiliary disorders

Sulfasalazine therapy can promote the onset of jaundice, liver failure, fulminant hepatitis, cholestatic hepatitis and cholestasis.

Kidney and urinary tract disorders

Treatment with sulfasalazine may cause:

  • Proteinuria;
  • Nephrotic syndrome;
  • Interstitial nephritis;
  • nephrolithiasis;
  • crystalluria;
  • Presence of blood in the urine.

Other side effects

Other side effects that may occur during sulfasalazine therapy are:

  • Temperature;
  • Facial edema;
  • Alteration of skin and urine color;
  • Decreased folic acid absorption;
  • Pseudo-mononucleosis;
  • Tinnitus;
  • Pallor;
  • arthralgia;
  • Systemic lupus erythematosus;
  • Sjögren syndrome;
  • Knotty periarthritis.

Overdose

If overdose of sulfasalazine is taken, nausea and vomiting may occur. Patients suffering from renal impairment are more likely to experience serious toxic effects.

In any case, if a overdosage with sulfasalazine is suspected, it is necessary to inform the doctor immediately or go to the nearest hospital.

Action mechanism

As mentioned above, sulfasalazine is a prodrug that is converted by the bacteria of the intestinal bacterial flora into sulfapyridine and into 5-aminosalicylic acid (5-ASA).

Sulfasalazine is used in the treatment of inflammatory pathologies thanks to the release of the salicylic derivative.

5-ASA exerts its anti-inflammatory action by inhibiting the enzyme cyclooxygenase (or COX), in particular, COX-1 and COX-2. In fact, these enzymes are involved in the synthesis of prostaglandins, the chemical mediators of the inflammatory response. Therefore, by inhibiting its synthesis, inflammation ceases.

Mode of Use - Posology

Sulfasalazine is available for oral administration in the form of gastro-resistant tablets.

The dose of sulfasalazine administered and the duration of treatment must be established by the doctor, depending on the type and severity of the pathology to be treated.

Below are some indications on the doses of medication usually used in therapy.

Ulcerative colitis and Crohn's disease

In adults, the dose of sulfasalazine usually used is 1-2 g four times a day.

In children, the dose of sulfasalazine usually administered is 40-60 mg / kg of body weight per day, to be divided into 3-6 divided doses.

Rheumatoid arthritis

For the treatment of rheumatoid arthritis, the dosage schedule prescribed by the doctor must be followed.

Pregnancy and breastfeeding

Since sulfasalazine inhibits the absorption and metabolism of folic acid, folic acid deficiency may occur in pregnant women. Furthermore, some newborns whose mothers took sulfasalazine during gestation developed neural tube defects, although the role of sulfasalazine in the onset of such defects is still not entirely clear.

In any case, the drug should not be used during pregnancy unless the doctor considers it absolutely essential.

Sulfasalazine is excreted in breast milk and may cause side effects in newborns, therefore the drug should not be used by breastfeeding mothers.

Contraindications

The use of sulfasalazine is contraindicated in the following cases:

  • In patients with known hypersensitivity to sulfasalazine;
  • In patients with known hypersensitivity to other sulfonamides or salicylates;
  • In patients suffering from severe renal insufficiency accompanied by hyperazotemia;
  • In patients suffering from severe liver disease;
  • In patients with porphyria;
  • In babies and children under 12 years of age;
  • In the last period of pregnancy;
  • During breastfeeding.

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