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Sulfasalazine (Tablets) Instructions for Use

ATC Code

A07EC01 (Sulfasalazine)

Active Substance

Sulfasalazine (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Drug with anti-inflammatory action used for the treatment of Crohn’s disease and UC

Pharmacotherapeutic Group

Antidiarrheals, intestinal anti-inflammatory/antimicrobial agents; intestinal anti-inflammatory agents; aminosalicylic acid and similar agents

Pharmacological Action

A drug for the treatment of ulcerative colitis, it is an azo compound of sulfapyridine and salicylic acid.

Sulfasalazine selectively accumulates in the connective tissue of the intestine with the release of 5-aminosalicylic acid, which has anti-inflammatory activity, and sulfapyridine, which has an antimicrobial effect against Streptococcus spp., including Streptococcus pneumoniae, Neisseria gonorrhoeae, Escherichia coli.

Pharmacokinetics

Sulfasalazine is poorly absorbed in the intestine (no more than 10%).

It is broken down by the intestinal microflora to form 60-80% sulfapyridine and 25% 5-aminosalicylic acid (5-ASA).

Plasma protein binding is 99% for sulfasalazine, 50% for sulfapyridine, and 43% for 5-ASA.

In the liver, sulfapyridine is biotransformed mainly by hydroxylation to form inactive metabolites, and 5-ASA is biotransformed by acetylation.

The T1/2 of sulfasalazine is 5-10 hours, sulfapyridine is 6-14 hours, and 5-ASA is 0.6-1.4 hours.

5% of sulfapyridine and 67% of 5-ASA are excreted in the feces; 75-91% of the absorbed sulfasalazine is excreted by the kidneys within 3 days.

Indications

Ulcerative colitis (treatment of exacerbations and maintenance therapy in the remission phase); Crohn’s disease (mild and moderate forms in the acute phase); rheumatoid arthritis; juvenile rheumatoid arthritis.

ICD codes

ICD-10 code Indication
K50 Crohn’s disease [regional enteritis]
K51 Ulcerative colitis
M05 Seropositive rheumatoid arthritis
M08 Juvenile arthritis
ICD-11 code Indication
DD70.Z Crohn’s disease, unspecified location
DD71.Z Ulcerative colitis, unspecified
FA20.0 Seropositive rheumatoid arthritis
FA24.Z Juvenile idiopathic arthritis, unspecified

Dosage Regimen

The method of application and dosage regimen for a specific drug depend on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly adhere to the compliance of the dosage form of a specific drug with the indications for use and dosage regimen.

Tablets

Ulcerative colitis and Crohn’s disease: when taken orally by adults, it is used after meals: on the 1st day, 500 mg 4 times/day; on the 2nd day, 1 g 4 times/day; on the 3rd and subsequent days, 1.5-2 g 4 times/day.

After the acute clinical symptoms subside, a maintenance dose of 500 mg 3-4 times/day is used for several months.

For children aged 5-7 years – 250-500 mg 3-6 times/day, over 7 years – 500 mg 3-6 times/day.

Rheumatoid arthritis: for adults during the first week – 500 mg once/day; during the 2nd week – 500 mg twice/day; during the 3rd week – 500 mg three times/day.

The therapeutic dose is 1.5-3 g/day.

The course of treatment is 6 months or more.

For children over 6 years of age – 30-50 mg/kg/day in 2-4 divided doses; for children over 16 years of age, the maximum daily dose is 2 g.

Adverse Reactions

Nervous system disorders: headache, dizziness, tinnitus, ataxia, convulsions, sleep disorders, hallucinations, peripheral neuropathy.

Urinary system disorders: impaired renal function, interstitial nephritis.

Digestive system disorders: nausea, vomiting, diarrhea, abdominal pain, anorexia, hepatitis, pancreatitis.

Respiratory system disorders: interstitial pneumonitis and other lung tissue lesions.

Hematopoietic system disorders: anemia, leukopenia, thrombocytopenia, agranulocytosis.

Reproductive system disorders: transient oligospermia, infertility.

Allergic reactions: skin rash, toxic epidermal necrolysis, malignant exudative erythema, fever, anaphylactic shock.

Other: possible yellow staining of the skin, urine, soft contact lenses.

Contraindications

Porphyria, anemia, severe liver dysfunction, severe renal dysfunction, glucose-6-phosphate dehydrogenase deficiency, children under 5 years of age, lactation period; hypersensitivity to sulfonamides and salicylic acid derivatives.

Use in Pregnancy and Lactation

The use of sulfasalazine during pregnancy is possible only for strict indications in the minimum effective dose.

If the course of the disease allows, it is recommended to discontinue Sulfasalazine in the third trimester of pregnancy.

If it is necessary to use the drug during lactation, the issue of discontinuing breastfeeding should be decided.

Use in Hepatic Impairment

Use with caution in patients with impaired liver function.

Use in Renal Impairment

Use with caution in patients with impaired renal function.

Pediatric Use

Contraindicated in children under 5 years of age.

Special Precautions

Use with caution in patients with impaired liver and/or kidney function, patients with bronchial asthma, allergic reactions.

During treatment, it is recommended to consume an increased amount of fluid.

During treatment, the level of liver enzymes, complete blood count and urinalysis should be monitored.

Drug Interactions

It enhances the effect of anticoagulants, antiepileptic and oral hypoglycemic drugs, as well as the side effects of cytostatics, immunosuppressants, hepatotoxic and nephrotoxic drugs.

When used concomitantly with sulfasalazine, the toxicity of azathioprine and mercaptopurine increases.

When used concomitantly with ampicillin or rifampicin, the release of 5-aminosalicylic acid from the sulfasalazine molecule in the large intestine is reduced (due to the suppression of the activity of anaerobic bacteria, which are involved in this process, under the influence of ampicillin and rifampicin).

In this regard, a decrease in the effectiveness of sulfasalazine is possible.

It is believed that the interaction of sulfasalazine with neomycin manifests itself in the same way.

When used concomitantly with digoxin, a decrease in its absorption is possible; with talinolol – the absorption of talinolol is reduced; with folic acid – a decrease in the absorption of folic acid is possible.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.

Medical Disclaimer

Brand (or Active Substance), Marketing Authorisation Holder, Dosage Form

Marketing Authorization Holder

Krka d.d., Novo mesto (Slovenia)

Dosage Form

Bottle Rx Icon Sulfasalazine Film-coated tablets, 500 mg: 50 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets brownish-yellow in color, round, slightly biconvex; inclusions of a lighter color are allowed; the fracture shows a rough mass of brownish-yellow color.

1 tab.
Sulfasalazine, coated with povidone* 535 mg
   Equivalent to sulfasalazine content 500 mg

* Sulfasalazine, coated with povidone, contains: Sulfasalazine, povidone 3%, water.

Excipients: pregelatinized starch, magnesium stearate, colloidal anhydrous silicon dioxide.

Shell composition: hypromellose, propylene glycol.

10 pcs. – blisters (5) – cardboard packs.

Marketing Authorization Holder

Atoll LLC (Russia)

Manufactured By

Ozon, LLC (Russia)

Dosage Form

Bottle Rx Icon Sulfasalazine Film-coated tablets, 500 mg: 10, 20, 30, 40, 50, 60 or 100 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets from light yellow to brownish-yellow in color, round, biconvex; the cross-section shows two layers: a brownish-yellow core and a film coating.

1 tab.
Sulfasalazine 500 mg

Excipients: pregelatinized starch – 115 mg, sodium carboxymethyl starch – 29 mg, povidone K25 – 24 mg, magnesium stearate – 7 mg, colloidal silicon dioxide – 5 mg.

Shell composition: hypromellose – 8.4 mg, macrogol-4000 – 2.1 mg, titanium dioxide – 4.1 mg, iron oxide yellow dye – 0.4 mg.

10 pcs. – contour cell packs (1) – cardboard packs.
10 pcs. – contour cell packs (2) – cardboard packs.
10 pcs. – contour cell packs (3) – cardboard packs.
10 pcs. – contour cell packs (4) – cardboard packs.
10 pcs. – contour cell packs (5) – cardboard packs.
10 pcs. – contour cell packs (6) – cardboard packs.
10 pcs. – contour cell packs (7) – cardboard packs.
10 pcs. – contour cell packs (8) – cardboard packs.
10 pcs. – contour cell packs (9) – cardboard packs.
10 pcs. – contour cell packs (10) – cardboard packs.
10 pcs. – polyethylene terephthalate jars (1) – cardboard packs.
20 pcs. – polyethylene terephthalate jars (1) – cardboard packs.
30 pcs. – polyethylene terephthalate jars (1) – cardboard packs.
40 pcs. – polyethylene terephthalate jars (1) – cardboard packs.
50 pcs. – polyethylene terephthalate jars (1) – cardboard packs.
60 pcs. – polyethylene terephthalate jars (1) – cardboard packs.
100 pcs. – polyethylene terephthalate jars (1) – cardboard packs.

Marketing Authorization Holder

Usolye-Sibirskiy Chemical and Pharmaceutical Plant, JSC (Russia)

Dosage Form

Bottle Rx Icon Sulfasalazine Film-coated tablets, 500 mg: 10, 20, 30, 40, 50, 60 or 100 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets from light yellow to brownish-yellow in color, round, biconvex; the cross-section shows two layers: a brownish-yellow core and a film coating.

1 tab.
Sulfasalazine 500 mg

Excipients: pregelatinized starch – 115 mg, sodium carboxymethyl starch – 29 mg, povidone K25 – 24 mg, magnesium stearate – 7 mg, colloidal silicon dioxide – 5 mg.

Shell composition: Opadry II yellow (hypromellose – 8.4 mg, titanium dioxide – 4.1 mg, macrogol-4000 – 2.1 mg, iron oxide yellow dye – 0.4 mg) – 15 mg.

10 pcs. – contour cell packs – cardboard packs.
10 pcs. – contour cell packs (2) – cardboard packs.
10 pcs. – contour cell packs (3) – cardboard packs.
10 pcs. – contour cell packs (4) – cardboard packs.
10 pcs. – contour cell packs (5) – cardboard packs.
10 pcs. – contour cell packs (6) – cardboard packs.
10 pcs. – jars – cardboard packs.
20 pcs. – jars – cardboard packs.
30 pcs. – jars – cardboard packs.
40 pcs. – jars – cardboard packs.
50 pcs. – jars – cardboard packs.
60 pcs. – jars – cardboard packs.
100 pcs. – jars – cardboard packs.

Marketing Authorization Holder

Krka d.d., Novo mesto (Slovenia)

Manufactured By

Krka d.d., Novo mesto (Slovenia)

Packaging and Quality Control Release

KRKA d.d., Novo mesto (Slovenia)

Or

KRKA-RUS, LLC (Russia)

Dosage Form

Bottle Rx Icon Sulfasalazine-EN Enteric-coated film-coated tablets, 500 mg: 50 pcs.

Dosage Form, Packaging, and Composition

Enteric-coated film-coated tablets from yellow to brownish-yellow in color, round, biconvex, with a beveled edge, with a characteristic odor; the fracture view is a rough mass from orange to brownish-orange in color with a film coating from yellow to brownish-yellow.

1 tab.
Sulfasalazine, coated with povidone 535 mg,
   Equivalent to sulfasalazine content 500 mg

Excipients: pregelatinized starch, magnesium stearate, colloidal anhydrous silicon dioxide.

Shell composition: titanium dioxide (E171), iron oxide yellow dye (E172), talc, triethyl citrate, macrogol-6000, carmellose sodium, methacrylic acid and ethyl acrylate copolymer (1:1)*.

10 pcs. – blisters (5) – cardboard packs.

* dry substance

Marketing Authorization Holder

Krka, D.D. (Slovenia)

Packaged By

KRKA-RUS, LLC (Russia)

Dosage Form

Bottle Rx Icon Sulfasalazine-EN Enteric-coated tablets, 500 mg: 50 pcs.

Dosage Form, Packaging, and Composition

Enteric-coated tablets from yellow to brownish-yellow in color, round, biconvex, with a beveled edge, with a characteristic odor; on the fracture – from orange to brownish-orange in color.

1 tab.
Sulfasalazine 500 mg

Excipients: povidone, pregelatinized starch, magnesium stearate, colloidal anhydrous silicon dioxide.

Shell composition: titanium dioxide, iron oxide yellow 10 dye (E172), talc, triethyl citrate, macrogol-6000, carmellose sodium, methacrylic acid and ethyl acrylate copolymer (1:1).

10 pcs. – blisters (5) – cardboard packs.

Marketing Authorization Holder

Krka, D.D. (Slovenia)

Packaged By

KRKA, d.d. (Slovenia)

Dosage Form

Bottle Rx Icon Sulfasalazine-EN Enteric-coated tablets, 500 mg: 50 pcs.

Dosage Form, Packaging, and Composition

Enteric-coated tablets from yellow to brownish-yellow in color, round, biconvex, with a beveled edge, with a characteristic odor; on the fracture – from orange to brownish-orange in color.

1 tab.
Sulfasalazine 500 mg

Excipients: povidone, pregelatinized starch, magnesium stearate, colloidal anhydrous silicon dioxide.

Shell composition: titanium dioxide, iron oxide yellow 10 dye (E172), talc, triethyl citrate, macrogol-6000, carmellose sodium, methacrylic acid and ethyl acrylate copolymer (1:1).

10 pcs. – blisters (5) – cardboard packs.

Marketing Authorization Holder

Pharmental Group, LLC (Russia)

Manufactured By

Nativa, LLC (Russia)

Dosage Form

Bottle Rx Icon Sulfasalazine-nativ Film-coated tablets, 500 mg: 50 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets yellow in color, round, biconvex with beveled edges; on the fracture – a brownish-yellow core, inclusions are allowed.

1 tab.
Sulfasalazine 500 mg

Excipients: crospovidone – 35 mg, pregelatinized starch – 89.7 mg, colloidal silicon dioxide – 3.3 mg, magnesium stearate – 12 mg.

Film coating composition: 6 mg, including polyvinyl alcohol – 40%, talc – 14.8%, macrogol 3350 – 20.2%, titanium dioxide – 21.65%, iron oxide yellow dye – 3.35%.

50 pcs. – polyethylene terephthalate bottles (1) – cardboard packs.

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