Sulfasalazine

When ATH:
A07EC01

Pharmacological action

Sulfasalazine is selectively accumulated in the connective tissue of intestines to release 5-aminosalicylic acid, Has anti-inflammatory activity, and sulfapyridine, has antimicrobial action.

The connective tissue of the bowel wall dissociates 5-aminosalicylic acid, Determining anti-inflammatory properties of sulfasalazine, and sulfapyridine - competitive antagonist of parabens, stopping the synthesis of folates in microbial cells and cause antibacterial activity. Effective against diplokokkov, streptococci, gonokokkov, E. coli.

Pharmacokinetics

Absorption

Sulfasalazine is poorly absorbed in the gut (no more 10 %). Undergoes cleavage to form the intestinal microflora 60-80 % and sulfapyridine 25 % 5-aminosalicylic acid (5-ASK).

Distribution

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

Metabolism

In the liver, sulfapyridine biotransformed principally through acetylation, 5-ASK - by acetylation.

Deduction

T1 / 2 of sulfasalazine 5-10 no, sulfapyrydyna - 6-14 no, 5-ASK - 0.6-1.4 no. Since feces derived 5 % and sulfapyridine 67 % 5-ASK; 75-91 % sulfasalazine excreted by the kidneys within 3 days.

Testimony

Nespetsificheskiy yazvennыy colitis (treatment exacerbations and maintenance therapy in remission).

Crohn's Disease (mild and moderate exacerbations).

Rheumatoid arthritis.

Juvenile rheumatoid arthritis.

Dosing and Administration

Inside, after meal.

Nespetsificheskiy yazvennыy colitis, Crohn's disease:

Adult. On the first day 500 mg 4 once a day; the 2nd day 1 g 4 once a day; in the third and following days 1,5-2 g 4 once a day. After calming down of acute clinical symptoms of ulcerative colitis prescribe a maintenance dose of 500 mg 3-4 times a day for several months.

Children. At the age of 5-7 years 250-500 mg 3-6 once a day; senior 7 years 500 mg 3-6 once a day.

Rheumatoid arthritis:

Adult. During the first week appoint 500 mg once daily, for a second – by 500 mg 2 once a day, during the third – by 500 mg 3 times a day, etc.. The therapeutic dose may be from 1,5 g to 3 g per day. A course of treatment – 6 months or more.

Children. At the age of 6 years at a dose 30-50 mg / kg body weight per day, razdelennoy of 2-4 admission. For children over 16 years, the maximum daily dose is 2 g.

Side effect

From the central and peripheral nervous system: headache, dizziness, noise in ears, ataxia, convulsions, sleep disorders, hallucinations, perifericheskaya neuropathy. From the urinary system: renal dysfunction, interstitial nephritis. From the digestive system: nausea, vomiting, diarrhea, abdominal pain, anorexia, hepatitis, pancreatitis. The respiratory system: interstitial pneumonitis and other lesions of the lung tissue. From the hematopoietic system: anemia, leukopenia, thrombocytopenia, agranulocytosis. Reproductive system: transient oligospermia, infertility. Allergic reactions: skin rash, fever, anaphylactic shock. Other: possible staining in yellow color, Urine, soft contact lenses.

Contraindications

• blood disease;
• porphyria;
• expressed human liver;
• expressed by the human kidney;
• deficit ferment glucose-6-fosfatdegidrogenazы;
• Children up to age 5 years;
• hypersensitivity to sulfonamides and salicylic acid derivatives.

Pregnancy and lactation

The use of sulfasalazine during pregnancy is possible only under strict indications in the minimum effective dose. If you allow the disease, It recommended to remove the drug in the III trimester of pregnancy. If necessary, use during lactation should decide the issue of termination of breastfeeding.

Cautions

Precautions should be prescribed to patients with impaired liver function and / or kidneys, patients with bronchial asthma, allergic reactions. During the period of the drug is recommended to use an increased amount of fluid.

Overdose

Symptoms: nausea, vomiting, stomach ache, dizziness. Treatment: gastric lavage, diurez; simptomaticheskaya therapy.

Drug Interactions

With simultaneous use of sulfasalazine reduces the absorption of folic acid, and digoxin. With simultaneous use of sulfasalazine increases the effects of anticoagulants and sulfonylurea derivatives. With simultaneous use of sulfasalazine and antibiotics may reduce the effectiveness of sulfasalazine, because antibiotics have a depressing effect on the intestinal flora.