What Are the Different Sulfasalazine Side Effects?

Sulfasalazine enteric-coated tablets, the indications are: 1. Ulcerative colitis is used to treat mild to moderate ulcerative colitis; it can be used as an adjuvant therapy in severe ulcerative colitis. Can also be used for maintenance treatment of ulcerative colitis in remission. 2. Crohn's disease is used to treat active clonal disease, especially those involving the colon. 3. Rheumatoid arthritis has no significant effect on salicylic acid or other non-steroidal anti-inflammatory drugs. Rheumatoid arthritis and juvenile rheumatoid arthritis (multi-articular type).

Sulfasalazine enteric-coated tablets, the indications are: 1. Ulcerative colitis is used to treat mild to moderate ulcerative colitis; it can be used as an adjuvant therapy in severe ulcerative colitis. Can also be used for maintenance treatment of ulcerative colitis in remission. 2. Crohn's disease is used to treat active clonal disease, especially those involving the colon. 3. Rheumatoid arthritis has no significant effect on salicylic acid or other non-steroidal anti-inflammatory drugs. Rheumatoid arthritis and juvenile rheumatoid arthritis (multi-articular type).

Drug Name

Sulfasalazine enteric-coated tablets

Drug type

Prescription medicines, essential medicines, medicines for medical workers' injuries

Use classification

Synthetic antibacterials

Ingredients for sulfasalazine enteric-coated tablets

The main ingredients of this product are: sulfasalazine; its chemical name is 5- [p- (2-pyridylaminesulfonyl) benzene] azosalicylic acid.
Its chemical structural formula is:

Molecular formula: C ₁₈ H ₁₄ N ₄ O ₅ S
Molecular weight: 398.39

Sulfasalazine enteric-coated tablets

This product is an enteric sugar-coated tablet or an enteric film-coated tablet. After removing the coating, it is yellow to brownish yellow.

Indications of sulfasalazine enteric-coated tablets

1. Ulcerative colitis is used to treat mild to moderate ulcerative colitis; it can be used as adjuvant therapy in severe ulcerative colitis. Can also be used for maintenance treatment of ulcerative colitis in remission.
2. Crohn's disease is used to treat active clonal disease, especially those involving the colon.
3. Rheumatoid arthritis has no significant effect on salicylic acid or other non-steroidal anti-inflammatory drugs. Rheumatoid arthritis and juvenile rheumatoid arthritis (multi-articular type).

Sulfasalazine enteric-coated tablets specifications

0.25g

Dosage of sulfasalazine enteric-coated tablets

The dosage should be determined based on the patient's response to the treatment and the tolerance of the drug. The tablets should be taken at a fixed time daily, preferably with meals. Patients who have not previously been treated with this tablet and enteric-coated tablets are advised to increase the dose gradually over the first few weeks. The use of enteric-coated tablets can reduce the incidence of gastrointestinal side effects. Enteric-coated tablets should not be crushed and taken apart. Inflammatory bowel disease (mostly ulcerative colitis)
adult:
Take 3 to 4 g daily in divided doses. The interval between medications should not exceed 8 hours. To prevent gastrointestinal intolerance, start with a small dose of 1 to 2 g (4-8 tablets) per day. Watch out for increased toxicity.
Severe attacks: 1 to 2 g (4 to 8 tablets) each time, 3 to 4 times a day, can be combined with steroid drugs to form an intensive treatment regimen.
Mild and moderate attacks: 1g (4 tablets) each time, 3 to 4 times a day.
Remission period: It is recommended to give a maintenance dose to prevent the symptoms from recurring, usually 2 to 3 times a day, 1 g (4 tablets) each time.
child:
According to the daily dose of 40 to 60 mg per kg of body weight, divided into 3 to 6 times.
Prevent recurrence: Take 3 to 6 doses at a dose of 20-30 mg per kg of body weight per day.
Rheumatoid arthritis:
According to experience, the clinical effect appears within 1 to 2 months after treatment. It is recommended that this enteric-coated tablet be taken with analgesics and / or non-steroidal anti-inflammatory drugs at least until the efficacy of sulfasalazine enteric-coated tablets appears. Prolonged treatment with sulfasalazine enteric-coated tablets has proven to be effective and well tolerated.
Adults take 1 g (4 tablets) 2 times a day. Enteric-coated tablets should not be crushed and taken apart. When starting treatment, it is recommended to increase the daily dose according to the following table: (sulfasalazine enteric-coated tablets)
In the first week, the second week, the third week, the fourth week, and later, one tablet, two tablets in the morning, one tablet, two tablets in the morning, if no response occurs after two months of treatment, the dose can be increased to 3 g per day. It should be monitored when it exceeds 2g per day.
Children currently do not advocate the use of sulfasalazine enteric-coated tablets for adolescents with chronic arthritis. When it must be used, refer to the following usage and dosage: children over 6 years old, 30-50mg / kg body weight / day, orally divided into two times, the maximum dose is 2g / day.

Adverse effects of sulfasalazine enteric-coated tablets

1. The most common adverse reactions are: nausea, anorexia, elevated body temperature, erythema and pruritus, headache, palpitations.
2. The adverse reactions listed below are rare and may be dose-related:
Hematological reactions: abnormal red blood cells (eg, hemolytic anemia, giant red blood cell disease), cyanosis.
Gastrointestinal reactions: stomach pain and abdominal pain.
Central nervous system reaction: dizziness, tinnitus.
Renal reactions: proteinuria, hematuria.
Skin reaction: yellow skin.
3. The following reactions may not be related to the dose:
Hematological reactions: Bone marrow suppression such as accompanied by leukopenia, granulocytopenia, thrombocytopenia.
Gastrointestinal reactions: hepatitis, pancreatitis.
Central nervous system reaction: peripheral neuropathy, aseptic meningitis.
Skin reactions: rash, urticaria, erythema polymorpha / Stevens-johnson syndrome, exfoliative dermatitis, epidermal necrolysis syndrome, photosensitivity.
Pulmonary reactions: Pulmonary complications (fibrous alveolitis accompanied by: dyspnea, cough, fever, eosinophilia).
Other allergic reactions: periorbital edema, serum disease, LE syndrome, nephrotic syndrome.
Reproductive disorders in men: Semen deficiency infertility has been reported in men treated with sulfasalazine. Stopping medication can reverse this reaction.

Sulfasalazine enteric-coated tablets contraindications

This product is contraindicated in patients who are allergic to sulfa and salicylate, intestinal obstruction or urinary obstruction, and patients with acute intermittent porphyria.

Precautions for sulfasalazine enteric-coated tablets

1. Glucose-6-phosphate dehydrogenase deficiency, liver dysfunction, renal dysfunction, hematoporphyria, platelets, granulocytopenia, hemocyanin, intestinal or urinary tract obstruction should be used with caution.
2. Drink plenty of water while taking this product to maintain a high urine flow to prevent the occurrence of crystallized urine. If necessary, take medications that alkalize urine. Dehydration, shock, and elderly patients are prone to kidney damage when using this product. Use this product with caution or avoidance.
3. Use with caution to those allergic to furosemide, sulfones, thiazide diuretics, sulfonylureas, carbonic anhydrase inhibitors and other sulfa drugs.
4. Pay attention to inspection during treatment:
(1) Whole blood examination is especially important for patients who have received a longer course of treatment.
(2) Proctoscopy and sigmoidoscopy examination, observe the effect of medication and adjust the dose.
(3) Periodic urine examination during the treatment (routine urine inspection every 2 to 3 days) to find crystallized urine that may occur during long courses or high-dose treatments.
(4) Liver and kidney function tests.
5. In case of gastrointestinal tract irritation, in addition to stressing after-meal medication, it can also be divided into small doses and even once every hour to reduce symptoms.
6. According to the patient's response and drug resistance, adjust the dose at any time, and some patients can be treated intermittently (two weeks of medication and one week of withdrawal).
7. When the symptoms of diarrhea do not improve, increase the dose.
8. The interval between drug withdrawal at night should not exceed 8 hours.
9. Those with impaired renal function should reduce the dose.

Sulfasalazine enteric-coated tablets for pregnant and lactating women

1. Sulfa drugs can cross the blood placental barrier to the fetus. Animal experiments have found teratogenic effects. Research in humans lacks sufficient data, so pregnant women should be contraindicated.
2. Sulfonamide can be secreted from breast milk. The concentration in breast milk can reach 50% to 100% of the blood concentration of the mother. The drug may affect the infants. Sulfonamide is used in newborns with glucose-6-phosphate dehydrogenase deficiency. The application may lead to the occurrence of hemolytic anemia. Therefore lactating women should be disabled.

Sulfasalazine enteric-coated tablets for children

Because sulfa drugs compete with bilirubin for binding sites on plasma proteins, and the neonatal acetyltransferase system is not well-developed, the free blood concentration of sulfa drugs is increased, which increases the risk of nuclear jaundice. Newborns and children under 2 should be disabled.

Sulfasalazine enteric-coated tablets for elderly

Elderly patients have an increased chance of serious adverse reactions with sulfa drugs. Such as severe rash, bone marrow suppression and thrombocytopenia are common in severe adverse reactions in the elderly. Therefore, it should be avoided in elderly patients, and the pros and cons should be weighed when there are indications.

Sulfasalazine enteric-coated tablets drug interactions

1. Combined with urinary alkalization drugs can enhance the solubility of sulfa drugs in alkaline urine and increase excretion.
2. P-aminobenzoic acid can be taken up by bacteria instead of sulfonamide, which antagonizes the bacteriostatic effect of sulfa drugs, so the two are not suitable for use.
3. When the following drugs are combined with sulfa drugs, the latter can replace the protein binding sites of these drugs, or inhibit their metabolism, so that the drug action time is prolonged or toxicity occurs. Therefore, when these drugs are combined with sulfa drugs, or after application of sulfa drugs The dosage needs to be adjusted during use. Such drugs include oral anticoagulants, oral hypoglycemic agents, methotrexate, phenytoin, and thiopental.
4. The combination of bone marrow inhibitory drugs and sulfa drugs may enhance the adverse reactions of these drugs to the hematopoietic system. If there are indications that the two types of drugs are used in combination, close observation should be made on possible toxic reactions.
5. Contraceptives (estrogen), combined with sulfa drugs for a long time can reduce the reliability of contraception and increase the chance of extramenstrual bleeding.
6. When combined with thrombolytic drugs and sulfa drugs, their potential toxic effects may be increased.
7. The combination of hepatotoxic drugs and sulfa drugs may increase the incidence of hepatotoxicity. Liver function should be monitored in such patients, especially those who have been taking the drug for a long time and have a previous history of liver disease.
8. The combination of photosensitive drugs and sulfa drugs may cause the additive effect of photosensitive.
9. The need for vitamin K is increased in those receiving sulfa drugs.
10. Urotropine can be decomposed to produce formaldehyde in acid urine, which can form insoluble precipitate with sulfa. The risk of crystallized urine is increased, so the combination of two drugs is not suitable.
11. The sulfa drugs can replace the plasma protein binding site of Baotaisong. When the two are combined, the effect of Baotaisong can be enhanced.
12, sulfinpyrazone (sulfinpyrazone) with sulfa drugs can reduce the secretion of the latter from the renal tubules, its blood concentration is increased and lasting, resulting in toxicity, so during the application of sulfinpyrazone or after its treatment The dose of sulfa drugs may need to be adjusted. When the duration of the sulfazone treatment is long, the blood concentration of the sulfa drug should be monitored to help adjust the dose and ensure safe medication.
13. When combined with digitalis or folic acid, the latter absorbs less and the blood concentration decreases. Therefore, the effects and effects of digitalis must be observed at any time.
14. Combined with probenecid, it will reduce the excretion of sulfa in renal tubules, which will cause the blood concentration of sulfa to rise, prolong the effect and be prone to poisoning.
15. In combination with neomycin, neomycin inhibits the intestinal flora, affects the decomposition of this product in the intestine, and reduces the effect.

Sulfasalazine enteric-coated tablets overdose

When the daily dosage reaches or exceeds 4 g or the serum drug concentration exceeds 50 g / ml, adverse reactions or toxic reactions increase. Nausea and vomiting often occur when overdose. For excessive treatment, gastric lavage should be performed first, followed by intravenous rehydration and diuresis. Intravenous sodium bicarbonate should be given to treat alkalinity. Be alert to oliguria and anuria. If anuria occurs, dialysis should be performed in time. If methemoglobinemia (cyanosis) occurs, methylene blue (Melan) should be given intravenously slowly at 1 to 2 mg per kg of body weight or other appropriate treatment. If there is severe thiohemoglobinemia, blood transfusion replacement therapy can be performed.

Pharmacology and toxicology of sulfasalazine enteric-coated tablets

Pharmacological action The mechanism of action of sulfasalazine and its metabolites 5-aminosalicylic acid and sulfadiazine is not clear, and it may be related to its anti-inflammatory and immunomodulatory effects in animal and in vitro experiments. Autoradiographic studies of animals It shows that sulfasalazine (SSZ) can be compatible with connective tissues and is at a relatively high level in the serum, liver and intestinal wall. Clinical studies of rectal administration of sulfasalazine and its main metabolites 5-aminosalicylic acid and sulfadiazine to patients with ulcerative colitis have shown that 5-aminosalicylic acid may produce the main therapeutic effect. It is not clear whether this product produces rheumatism mainly through sulfasalazine or its main metabolite.
Toxicological studies of genotoxicity: SSZ showed no mutagenic effect in Ames test and HGPRT gene test of L51784 mouse lymphoma cells. However, in rat and mouse bone marrow micronucleus test, mouse peripheral RBC test, sister chromosome interchange test, chromosome aberration test and human lymphocyte micronucleus test, its mutagenic effect is not clear.
Reproductive toxicity: Male fertility is impaired at a dose of 800 mg / kg / day (4800 mg / m ² ) in male rats. There have been clinical reports of spermatozoa and infertility caused by sulfasalazine administration. Can recover by itself afterwards. When rats and rabbits were administered 6 times as much as humans, there was no significant damage to female animals' fertility and fetuses. There are currently no adequate and strictly controlled clinical studies on the administration of this product in pregnant women.
Carcinogenicity: Carcinogenicity studies of F344 / N rats and B6C3F1 mice administered orally for two years were performed. Rats were dosed at 84 mg / kg / day (496 mg / m ² ), 168 mg / kg / day, and 337.5 mg / kg / day, respectively. As a result, the incidence of urethral bladder transitional cell papilloma in male rats increased ( Statistically significant), renal transitional cell papilloma occurred in 2 cases (4%) of female rats in the 337.5 mg / kg / day dose group; increased incidence of urinary bladder and kidney tumors in rats and formation and migration of kidney stones Cell epithelium is involved. When the doses of the mice were 675 mg / kg / day (2025mg / m ² ), 1350 mg / kg / day and 2700mg / kg / day, the hepatocyte adenoma and cancer of the female and male mice in each administration group were The incidence was significantly higher than the control group.

Pharmacokinetics of sulfasalazine enteric-coated tablets

After oral administration of sulfasalazine, a small portion is absorbed in the gastrointestinal tract, and can be re-entered into the intestine through the bile (gut-liver circulation). Most of the products that are not absorbed are broken down by bacteria in the terminal ileum and colon into 5-aminosalicylic acid and sulfapyridine, and the remaining part is excreted from feces. 5-aminosalicylic acid is hardly absorbed, and most of it is excreted from the feces in its original form, but the N-acetyl derivative of the former is found in the urine. Sulfadiazine can be absorbed and excreted, and its acetylated metabolites can be detected in urine. The concentration of serum sulfadiazine and its metabolites (20-40 g / ml) is related to toxicity. It is toxic when the concentration exceeds 50 g / ml, so the dose should be reduced to avoid toxic reactions. Sulfadiazine and its metabolites can also be found in breast milk.

Storage of sulfasalazine enteric-coated tablets

Shaded and sealed.

Sulfasalazine enteric-coated tablets packaging

PVC aluminum plastic blister board, 12 pcs / board, 60 pcs / box.

Sulfasalazine enteric-coated tablets

Tentative 24 months.

Sulfasalazine enteric-coated tablets

"Chinese Pharmacopoeia" 2010 edition two. ^[1]