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 DisclaimerBrand (or Active Substance), Marketing Authorisation Holder, Dosage Form
Film-coated tablets, 500 mg: 50 pcs.
Marketing Authorization Holder
Krka d.d., Novo mesto (Slovenia)
Dosage Form
 |
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.
Film-coated tablets, 500 mg: 10, 20, 30, 40, 50, 60 or 100 pcs.
Marketing Authorization Holder
Atoll LLC (Russia)
Manufactured By
Ozon, LLC (Russia)
Dosage Form
|
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.
Film-coated tablets, 500 mg: 10, 20, 30, 40, 50, 60 or 100 pcs.
Marketing Authorization Holder
Usolye-Sibirskiy Chemical and Pharmaceutical Plant, JSC (Russia)
Dosage Form
|
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.
Enteric-coated film-coated tablets, 500 mg: 50 pcs.
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
|
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
Enteric-coated tablets, 500 mg: 50 pcs.
Marketing Authorization Holder
Krka, D.D. (Slovenia)
Packaged By
KRKA-RUS, LLC (Russia)
Dosage Form
|
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.
Enteric-coated tablets, 500 mg: 50 pcs.
Marketing Authorization Holder
Krka, D.D. (Slovenia)
Packaged By
KRKA, d.d. (Slovenia)
Dosage Form
|
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.
Film-coated tablets, 500 mg: 50 pcs.
Marketing Authorization Holder
Pharmental Group, LLC (Russia)
Manufactured By
Nativa, LLC (Russia)
Dosage Form
|
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.
![Sulfasalazine [Tablets] 1](https://www.medixlife.com/wp-content/uploads/Medixlife_favi_512.png "Sulfasalazine [Tablets] 2")