How Effective Is Sulfasalazine for Arthritis?

This product is a sulfa antibiotic. It is a sulfa drug that is not easily absorbed by oral administration. The absorption part is decomposed into 5-aminosalicylic acid and sulfapyridine under the action of intestinal microorganisms. 5-aminosalicylic acid stays in the intestinal wall tissue for a long time after complexing with intestinal wall connective tissue, and plays an antibacterial, anti-inflammatory and immunosuppressive role, such as reducing Escherichia coli and Clostridium, and inhibiting prostaglandin synthesis And the synthesis of other inflammatory mediators leukotriene. Therefore, it is currently believed that the main component of the effect of this product on inflammatory bowel disease is 5-aminosalicylic acid. The sulfadiazine produced by the decomposition of this product shows a weak antibacterial effect on the intestinal flora.

This product is a sulfa antibiotic. It is a sulfa drug that is not easily absorbed by oral administration. The absorption part is decomposed into 5-aminosalicylic acid and sulfapyridine under the action of intestinal microorganisms. 5-aminosalicylic acid stays in the intestinal wall tissue for a long time after complexing with intestinal wall connective tissue, and plays an antibacterial, anti-inflammatory and immunosuppressive role, such as reducing Escherichia coli and Clostridium, and inhibiting prostaglandin synthesis And the synthesis of other inflammatory mediators leukotriene. Therefore, it is currently believed that the main component of the effect of this product on inflammatory bowel disease is 5-aminosalicylic acid. The sulfadiazine produced by the decomposition of this product shows a weak antibacterial effect on the intestinal flora.

Drug Name

Sulfasalazine

Alias

Sulfasalazine

Foreign name

Sulfasalazine

Whether prescription drugs

prescription

Main indications

Inflammatory bowel disease, ankylosing spondylitis

Dosage

2 to 3 g daily, orally 3 to 4 times

Dosage form

Enteric coated tablets

Brief introduction of sulfasalazine compounds

Sulfasalazine Basic Information

Chinese name: Willow sulfonidine

Chinese aliases: sulfasalazine, sulfasalazine salicylate, sulfasalazine salicylate, sulfasalazine

English name: Sulfasalazine

English aliases: Azulfidine, Colo-Pleon, Gastropyrin, Salazopyrin, Salazopyrina, Salazosulfapyridine, Salicylazosulfapyridine, Salicylazosulphapyridine, Salisulf, Sulphasalazine

CAS number: 599-79-1

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

Molecular weight: 398.39300

Exact mass: 398.06800

PSA: 149.69000

LogP: 4.85540

Physiochemical properties of sulfasalazine

Appearance and properties: dark yellow to brown yellow powder, odorless.

Dissolution: Soluble in sodium hydroxide, slightly soluble in ethanol, insoluble in water, chloroform, ether, and benzene.

Density: 1.48g / cm ³

Melting point: 260-265 ° C (dec.) (Lit.)

Boiling point: 630.9ºCat760mmHg

Flash point: 335.4ºC

Refractive index: 1.691

Storage conditions: Store in a cool, dry, and dark container. Keep away from fire.

Sulfasalazine Safety Information

Symbol: GHS08

Signal Word: Danger

Hazard statement: H317; H334

Customs Code: 29350009090

WGK Germany: 2

Danger category code: R42 / 43

Safety instructions: S22-S29 / 56-S45

RTECS number: VO6250000

Dangerous goods mark: Xn ^[1]

Production method of sulfasalazine

2-Aminopyridine is reacted with N-acetylamino-benzenesulfonyl chloride, followed by hydrolysis to obtain sulfonylpyridylamine, that is, sulfapyridine. After diazotization of sulfapyridine, it is coupled with salicylic acid and acidified to produce sulfasalazine ^[1] .

Use of sulfasalazine

For the treatment of ulcerative colitis. This product is rarely absorbed after oral administration and breaks down in the intestinal wall to play a therapeutic role. Has dual effects of anti-inflammatory and antibacterial. Many data in recent years show that it can also suppress immunity

Sulfasalazine

The synthesis of epidemic complexes and rheumatoid factors, thus affecting the immunopathological damage of rheumatoid arthritis. The drug has been used to treat inflammatory bowel disease and rheumatoid arthritis for more than 40 years. Because sulfasalazine was mostly used for short-term and non-control applications, it has been mixed for some time. Tests in the late 1970s have shown that the drug can improve the clinical symptoms of rheumatoid arthritis and can reduce C-reactive protein and erythrocyte sedimentation to varying degrees ^[1] .

Sulfasalazine pharmacopoeia standard

Source (name) and content (valency) of sulfasalazine

This product is 5- [p- (2-pyridylaminesulfonyl) benzene] azosalicylic acid. Calculated on dry basis, containing C18H14N4O5S should be 97.0% to 101.5%.

Sulfasalazine

This product is dark yellow to brown yellow powder; odorless.

This product is very slightly soluble in ethanol, almost insoluble in water; easily soluble in sodium hydroxide test solution.

Sulfasalazine identification

(1) Take the solution under the content determination item and measure it according to the UV-Vis spectrophotometry (Appendix IVA of Pharmacopoeia Part II of the 2010 edition). It has the maximum absorption at the wavelength of 359nm.

(2) The infrared light absorption spectrum of this product should be the same as that of the control ("Infrared Spectra of Medicine" 620).

Sulfasalazine

acidity

Take 1.0g of this product, add 100ml of water, heat in a water bath for 5 minutes, let it cool, filter, take 50ml of the filtrate, add 2 drops of phenolphthalein indicator solution and 0.5ml of sodium hydroxide titration solution (0.1mol / L), it should be red .

chloride

Take 1.0g of this product, add 100ml of water, heat to 70 , let it cool for 5 minutes, filter, and take 25ml of the filtrate, check it according to law (Appendix A of Part Two of the 2010 Pharmacopoeia) and make it with 7.0ml of standard sodium chloride The control solution must not be more concentrated (0.028%).

Sulfate

Take 50ml of the filtrate under chloride inspection and check it according to law (Appendix B of Part II of the Pharmacopoeia 2010), compared with the control solution made of 2.0ml of standard potassium sulfate solution, it must not be more concentrated (0.04%).

relative substance

Take an appropriate amount of this product, accurately weigh it, add ammonia solution (take 8ml of concentrated ammonia solution, and dilute it to 1000ml with water) to dissolve and dilute it to make a solution containing 1mg per 1ml as the test solution; take an appropriate amount of precise amount and use ammonia The solution was quantitatively diluted to make a solution containing 10 g per 1 ml as a control solution. Tested according to high performance liquid chromatography (Appendix VD of Part Two of the Pharmacopoeia, 2010 edition), using octadecylsilane bonded silica as a filler; phosphate buffer (pH 4.8) as mobile phase A, and methanol-phosphate buffer The liquid (pH 4.8) (80:20) is mobile phase B; gradient elution is performed according to the following table, and the detection wavelength is 320 nm. The resolution of the sulfasalazine peak from the adjacent impurity peaks should meet the requirements. Take 20l of the control solution and inject it into the liquid chromatograph, adjust the detection sensitivity so that the peak height of the main component of the control solution is about 50% of the full range, and accurately measure 20l each of the test solution and the control solution, and inject them into the liquid chromatograph respectively. Record the chromatogram. If there is an impurity peak in the chromatogram of the test solution, the area of a single impurity peak should not be greater than the area of the main peak of the control solution (1.0%), except for the sulfadiazine peak and the salicylic acid peak. 4 times the area (4.0%). Any peak less than 0.05 times the area of the main peak of the control solution in the chromatogram of the test solution was ignored ^[2] .

Time (minutes)	Mobile phase A (%)	Mobile phase B (%)
0	60	40
15	45	55
25	45	55
60	0	100
65	0	100
67	60	40
77	60	40

Salicylic acid and sulfadiazine

Take the test solution under the relevant substance as the test solution; take appropriate amounts of the salicylic acid reference substance and the sulfapyridine reference substance, accurately weigh, add ammonia solution to dissolve and quantitatively dilute to make a solution containing 5 g per 1 ml. As a reference solution. Tested according to high performance liquid chromatography (Appendix V D of Part Two of the Pharmacopoeia, 2010 edition), using octadecylsilane bonded silica as a filler; phosphate buffer solution (pH 4.8) (take 1.0g sodium dihydrogen phosphate and acetic acid) 2.5g of sodium, add 900ml of water to dissolve, adjust the pH to 4.8 with glacial acetic acid, and dilute to 1000ml with water)-methanol (76:24) as mobile phase A, and methanol-phosphate buffer (pH 4.8) (80:20 ) Is mobile phase B. Gradient elution is performed according to the following table; the detection wavelength is 300 nm. The resolution of the salicylic acid peak and the sulfadiazine peak should be greater than 2.0. Take 20l of the reference solution and inject it into the liquid chromatograph to adjust the detection sensitivity so that the peak height of salicylic acid in the reference solution is about 20% of the full range. Precisely take 20l each of the test solution and the reference solution and inject them separately. Liquid chromatograph, record chromatogram. If the chromatogram of the test solution has chromatographic peaks with the same retention times as the salicylic acid and sulfadiazine, the peak area must not be larger than the corresponding peak area in the reference solution (both must not exceed 0.5%) ^[2] .

Time (minutes)	Mobile phase A (%)	Mobile phase B (%)
0	100	0
10	100	0
11	0	100
twenty three	0	100
twenty four	100	0
33	100	0

Loss on drying

Take this product and dry it at 105 ° C to constant weight, and the weight loss shall not exceed 1.0% (Appendix L of Pharmacopoeia Part II of 2010 Edition).

Residue on ignition

Must not exceed 0.2% (Appendix N of Part Two of the 2010 Pharmacopoeia).

Heavy metal

Take 1.0g of this product and check it according to law (Appendix H, the second method of the 2010 Pharmacopoeia, the second method). The content of heavy metals must not exceed 20 parts per million.

Analysis of sulfasalazine

Method name:

Determination of sulfasalazinespectrophotometry

Application:

This method uses spectrophotometry to determine the content of sulfasalazine.

This method is applicable to sulfasalazine.

Method principle:

Take an appropriate amount of this product, add 0.1mol / L sodium hydroxide to dissolve, and then add acetic acid-sodium acetate buffer solution, take water as blank, and measure the absorbance at 359nm according to UV-visible spectrophotometry. Press C ₁₈ H The absorption coefficient (E1 m) of ₁₄ N ₄ O ₅ S is calculated as 658.

Reagent:

0.1mol / L sodium hydroxide solution

Acetic acid-sodium acetate buffer (pH 4.5)

equipment:

Visible spectrophotometer

Sample preparation:

0.1mol / L sodium hydroxide solution

Take 5.6mL of a clear saturated sodium hydroxide solution, add freshly boiled cold water to 1000mL, and shake to obtain.

Acetic acid-sodium acetate buffer (pH 4.5)

Take 18g of sodium acetate, add 9.8mL of glacial acetic acid, and then dilute to 1000mL with water.

Preparation of test solution

Take 0.15g of this product, weigh it accurately, place it in a 100mL volumetric flask, add 10mL of 0.1mol / L sodium hydroxide solution to dissolve, and dilute to the mark with water, as the test solution.

Note: "Precision weighing" means that the weighed weight should be accurate to one thousandth of the weighed weight. "Precision measurement" means that the accuracy of measuring the volume should meet the accuracy requirements of the volume pipette in national standards.

Steps:

Precisely measure 5mL of the above test solution, put it into a 1000mL volumetric flask, add 900mL of water, dilute to the mark with acetic acid-sodium acetate buffer (pH4.5), take water as blank, and apply UV-visible spectrophotometry at 359nm At the wavelength, the absorbance is measured according to the law, and the absorption coefficient (E1 m) of C ₁₈ H ₁₄ N ₄ O ₅ S is calculated as 658, which is ^[3] .

Sulfasalazine substance toxicity

Toxicity data from literature and journals

Numbering	Toxicity type	testing method	Test object	Dosage used	Toxic effect
1	Acute toxicity	oral	Adult male	122 mg / kg / 8Y-I	1. Peripheral neurotoxicity-paresthesia 2. Vascular toxicity-other changes
2	Acute toxicity	oral	Adult male	1286 mg / kg / 30D-I	1. Lung, chest or respiratory toxicity-other changes 2. Hematological toxicity-increased eosinophils 3. Hematological toxicity-changes in blood cell count
3	Acute toxicity	oral	Adult woman	570 mg / kg / 11D-I	1. Hematological toxicity-Leukopenia 2. Hematological toxicity-Thrombocytopenia 3. Hematological toxicity-Other changes
4	Acute toxicity	oral	child	3800 mg / kg / 19D-I	1. Liver toxicity-hepatitis (necrosis of liver cells), spread
5	Acute toxicity	oral	Adult male	7143 ug / kg	1. Gastrointestinal toxicity-excessive exercise, diarrhea 2. Gastrointestinal toxicity-nausea, vomiting
6	Acute toxicity	oral	Adult male	143 mg / kg / 10D-I	1. Hematological toxicity-thrombocytopenia
7	Acute toxicity	oral	Adult male	3200 mg / kg / 31D-I	1. Hematological toxicity-agranulocytosis 2. Hematological toxicity-other changes 3. Skin and accessory toxicity-allergic dermatitis (after systemic exposure)
8	Acute toxicity	oral	Humanity	429 mg / kg / 10D-I	1. Hematological toxicity-hemolysis but not necessarily anemia
9	Acute toxicity	oral	Adult male	357 mg / kg	1. Behavioral toxicity-Appearing hallucinations and perceived distortions 2. Behavioral toxicity-headache
10	Acute toxicity	oral	Adult woman	140 mg / kg / 2W-I	1. Behavioral toxicity-headache 2. Gastrointestinal toxicity-excessive exercise, diarrhea 3. Nutrition and metabolic system toxicity-elevated body temperature
11	Acute toxicity	oral	Adult woman	700 mg / kg / 4W-I	1. Behavioral toxicity-Excitement 2. Hepatotoxicity-Decreased liver function 3. Hematological toxicity-Changes in white blood cell count
12	Acute toxicity	Not reported	Adult woman	840 mg / kg / 3W-I	1. Hepatotoxicity-hepatitis (necrosis of liver cells), spread 2. Skin and attachment toxicity-dermatitis (after systemic exposure) 3. Immune system toxicity-increase immune response
13	Acute toxicity	Not reported	Adult male	1300 mg / kg / 4W-I	1. Behavioral toxicity-hallucinations, perception distortion 2. Behavioral toxicity-ataxia 3. Gastrointestinal toxicity-nausea, vomiting
14	Acute toxicity	Not reported	Adult woman	2700 mg / kg / 13W-I	1. Skin and accessory toxicity-dermatitis (after systemic exposure) 2. Immune system toxicity-unknown
15	Acute toxicity	Rectal injection	Adult male	7143 ug / kg	1. Gastrointestinal toxicity-excessive exercise, diarrhea 2. Gastrointestinal toxicity-nausea, vomiting
16	Acute toxicity	oral	Rat	15600 mg / kg	Detailed effects are not reported other than lethal dose
17	Acute toxicity	Subcutaneous injection	Rat	3870 mg / kg	Detailed effects are not reported other than lethal dose
18	Acute toxicity	Intravenous injection	Rat	1520 mg / kg	Detailed effects are not reported other than lethal dose
19	Acute toxicity	oral	Mouse	12500 mg / kg	Detailed effects are not reported other than lethal dose
20	Acute toxicity	Subcutaneous injection	Mouse	3 mg / kg	Detailed effects are not reported other than lethal dose
twenty one	Acute toxicity	Intravenous injection	Mouse	1096 mg / kg	Detailed effects are not reported other than lethal dose
twenty two	Acute toxicity	oral	rabbit	> 7500 mg / kg	Detailed effects are not reported other than lethal dose
twenty three	Chronic toxicity	oral	Rat	32400 mg / kg / 16D-I	1. Hematological toxicity-changes in serum composition (such as TP, bilirubin, cholesterol) 2. Endocrine toxicity-changes in thymus weight 3. Nutrition and metabolic system toxicity-weight loss or rate of weight loss
twenty four	Chronic toxicity	oral	Mouse	32400 mg / kg / 16D-I	1. Gastrointestinal toxicity-other changes
25	Mutation toxicity		Human lymphocyte	40 mg / L
26	Mutation toxicity		Human lymphocyte	20 mg / L
27	Mutation toxicity	oral	Mouse	5634 mg / kg
28	Carcinogenicity	oral	Rat	177 mg / kg / 2Y-I	1. Carcinogenicity-Carcinogenic (according to RTECS standards) 2. Kidney, ureter and bladder toxicity-tumor
29	Carcinogenicity	oral	Mouse	141 mg / kg / 2Y-I	1. Carcinogenicity-Carcinogenic (according to RTECS standards) 2. Liver toxicity-tumor
30	Reproductive toxicity	oral	Adult woman	8100 mg / kg, 1-40 weeks after female conception	1. Reproductive toxicity-abnormal skull and facial development (including nose / tongue) 2. Reproductive toxicity-abnormal development of the cardiovascular circulatory system
31	Reproductive toxicity	oral	Rat	8400 mg / kg, male mated 14 days ago	1. Reproductive toxicity-abnormal male spermatogenesis (including genetic material, sperm morphology, sperm motility and count)
32	Reproductive toxicity	oral	Rat	5460 mg / kg, male mated 13 weeks ago	1. Reproductive toxicity-abnormal male spermatogenesis (including genetic material, sperm morphology, sperm motility and count)
33	Reproductive toxicity	oral	Rat	8400 mg / kg, male mated 28 days ago	1. Reproductive toxicity-Decreased male fertility
34	Reproductive toxicity	oral	Rat	16800 mg / kg, male mated 28 days ago	1. Reproductive toxicity-increased pre-implantation mortality
35	Reproductive toxicity	oral	Rat	7 mg / kg, male mated 35 days ago	1. Reproductive toxicity-abnormal male spermatogenesis (including genetic material, sperm morphology, sperm motility and count)
36	Reproductive toxicity	oral	Rat	8400 mg / kg, male mated 14 days ago	1. Reproductive toxicity-changes in testis, epididymis, and vas deferens 2. Reproductive toxicity-Decreased male fertility
37	Reproductive toxicity	oral	Mouse	43875 mg / kg, male mating 13 weeks ago	1. Reproductive toxicity-changes in testis, epididymis, and vas deferens

^[4-28]

Salsalazine Drug Description

Sulfasalazine pharmacological effects

Sulfasalazine is an azo compound of salicylic acid and sulfadiazine, which has antibacterial, anti-rheumatic, and immunosuppressive effects. In the intestine, the bacteria break down into sulfadiazine (SP) and 5-aminosalicylic acid (5-ASA). SP has a weak antibacterial effect. It mainly acts as a carrier in the drug molecule, preventing 5-ASA from being absorbed in the stomach and duodenum. Only in the intestinal alkaline conditions, intestinal microorganisms break the diazo bond and release it. Active ingredients. Its mechanism is currently believed that 5-ASA stays in the intestinal wall tissue for a long time after complexing with connective tissue of the large intestine wall to play an antibacterial, anti-inflammatory and immunosuppressive effect, reduce E. coli and clostridium, and inhibit the intestinal prostaglandin. Synthesis (increased prostaglandins in patients with ulcerative colitis) and other inflammatory mediators (leukotriene). Its anti-rheumatic effect may be caused by the inhibition of certain antigenic substances in the intestine by sulfadipyridine, thereby inhibiting the immune processes of ankylosing spondylitis and rheumatoid arthritis. Sulfasalazine has almost no absorption in the gastrointestinal tract, has a special affinity for connective tissue, and releases sulfapyridine from the connective tissue of the intestinal wall ^[2] .

Pharmacokinetics of sulfasalazine

Sulfasalazine absorption varies from individual to individual and is generally poor. After oral administration, it is less absorbed in the gastrointestinal tract and can be re-entered into the intestine through bile. The drug appears in the plasma 1 to 2 hours after taking it. It can be decomposed and release sulfapyridine in 3 to 5 hours. The unabsorbed part is taken into the terminal ileum and colon The bacteria are broken down into 5-aminosalicylic acid and sulfadiazine, and the remainder is excreted from the feces. 5-Aminosalicylic acid is hardly absorbed, and is mostly excreted from the feces in its original form. The concentration in the feces is high, and only part of it is absorbed. About 1/3 is excreted in urine in acetylated form, but the former is derived from N-acetyl. Things can be 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 the therapeutic effect. When the concentration exceeds 50 g / ml, it is toxic. Therefore, the dose should be reduced to avoid toxic reactions. Sulfadiazine and its metabolites can also be found in breast milk. Can pass through the placenta ^[2] .

Sulfasalazine indications

1. Mainly used for inflammatory bowel disease, namely acute and chronic ulcerative colitis and Crohn's disease, and can prevent the recurrence of ulcerative colitis.

2. Prevention of infection after bowel surgery.

3. For the treatment of rheumatoid arthritis and ankylosing spondylitis ^[2] .

Sulfasalazine Contraindications

1. Allergic to sulfasalazine and its metabolites, sulfa drugs or salicylic acid;

2. Thrombocytopenia;

3. Intestinal or urinary tract obstruction;

4.6- deficiency of phosphoglucose dehydrogenase;

5. Hemocyaninosis;

6. Severe liver damage;

7. Severe renal insufficiency;

Children under 8.2 years old (as sulfasalazine may cause bilirubin encephalopathy);

9. Pregnant women ^[2] .

Sulfasalazine Precautions

1. (1) Use with caution in patients with liver and kidney dysfunction and patients with bronchial asthma; (2) Use with caution in the last month of pregnancy and in the first month of pregnancy. (3) People with slow acetylation; (4) Impaired liver and kidney function; (5) Systemic medication for juvenile rheumatoid arthritis; (6) Fibrotic alveolitis.

2. Others: Patients allergic to sulfa drugs will also have cross-allergies to sulfasalazine. People who are allergic to furosemide, sulfonyls, thiazines, diuretics, carbonic anhydrase inhibitors or salicylic acids will also be allergic to sulfasalazine.

3. During the treatment, pay attention to check the blood picture and the presence or absence of sulfa crystals in the urine. Urinary tract stones may appear during long-term use. Proctoscopy should be performed regularly.

4. Stop administration when skin symptoms and blood disorders occur.

5. Adequate water supply should be ensured during medication ^[2] .

Sulfasalazine adverse reactions

1. Fever and rash may occur, and severe cases may cause skin necrosis (Lyell syndrome).

2. Respiratory system: Adverse reactions of the respiratory system are rare. Fibrous alveolitis has been reported, but it should be distinguished from the symptoms of ulcerative colitis such as fever, dyspnea, increased eosinophils, and pulmonary infiltration. Such adverse reactions usually appear within 1 to 6 months after taking the drug, and can be recovered after stopping the drug, but there have been reports of death. In such patients, azosalicylic salicylate can be used instead.

3. Hematological system: The most important side effect of sulfasalazine is the inhibition of the hematopoietic system. (1) Thrombocytopenia (severe can cause bleeding tendency) and leukocytopenia (severe can cause infection); (2) sulfasalazine can also reduce folic acid absorption and cause megaloblastic anemia; ( 3) For patients lacking 6-phosphate glucose dehydrogenase, the tendency of blood cells to lyse is more serious; (4) There are also reports of death due to damage to the hematopoietic system.

4. Digestive system: Nausea, vomiting, and abdominal discomfort are common, sore throat, dysphagia can also occur, and rare pancreatitis, toxic hepatitis, and colitis worsen. For patients with slow acetylation metabolism, the incidence of adverse reactions in the digestive system is higher.

5. Reproductive system: sulfasalazine can cause a decrease in male sperm counts, decreased mobility, and an increased proportion of malformations, leading to decreased fertility or infertility.

6. Psycho-nervous system: For some patients with abnormal allergies, taking sulfasalazine may cause neuro-psychological symptoms. There have been reports of severe depression.

7. Urinary system: Sulfasalazine contained in sulfasalazine can cause dysuria, crystallized urine and hematuria after absorption.

8. Drug resistance: Some studies have found that sulfasalazine can induce drug resistance in bacteria.

9. Other: rare goiter ^[2] .

Sulfasalazine usage dosage

1. The initial dose is 2 to 3 g per day, divided into 3 to 4 times, swallow without chewing. When there is no response, it gradually increases to 4-6g per day. After the symptoms are relieved, it gradually decreases to 1.5-2g per day until the symptoms disappear. The total course of treatment can reach 1 year. For children over 2 years old, the initial amount is 10-15 mg / kg, and the maintenance amount is 7.5-10 mg / kg, 4 times a day.

2. Rectal administration: 1 anal suppository for severe patients every morning, middle and night after defecation; 1 anal suppository for morning and evening defecation for moderate or mild patients. After the symptoms have improved significantly, take 1 anal suppository every night or every other night. The suppository was placed laterally for 0.5h after being inserted into the anus.

3. Enema: 2 g of sulfasalazine powder, white powder and 3 g powder, 1 tin powder, and appropriate amount of hydrocortisone and procaine, mixed with warm boiled water 100-200 ml, for retention enemas, 1 or 2 times a day .

Sulfasalazine drug interactions

1. The effect of sulfasalazine may be enhanced when used in combination with Butepine.

2. When sulfasalazine is combined with probenecid, it can reduce the excretion of sulfa by renal tubules, increase the sulfa concentration in blood, and easily cause poisoning.

3. When combined with anticoagulants, phenytoin, oral hypoglycemic agents, thiopental, methotrexate, etc., the effect of sulfasalazine is prolonged and toxicity is increased. Pay attention to adjusting the dosage.

4. Riluzole has potential hepatotoxicity, and combined with sulfasalazine can increase the risk of liver damage. To date, there is no safety data available for both.

5. When sulfasalazine is used in combination with urinary alkali chemicals, it can increase the solubility of sulfamin in urine and promote its excretion.

6. When sulfasalazine is combined with digitalis, the absorption of the latter is reduced and the blood concentration is reduced. Therefore, the effects and efficacy of digitalis must be observed at any time.

7. When sulfasalazine is combined with cyanocobalamin tablets (vit12 tablets), it will affect the absorption of the latter.

8. Drugs that inhibit intestinal flora, especially various broad-spectrum antibacterial drugs, can inhibit intestinal flora, affect the decomposition of sulfasalazine in the intestine, and reduce the effect of sulfasalazine.

9. Ampicillin can affect the absorption of sulfasalazine and reduce its utilization, but it has no significant effect on the absorption start time, peak concentration time, absorption half-life and distribution half-life (its mechanism of action is unclear). When the two are combined, attention should be paid to observe whether the efficacy of sulfasalazine is reduced.

10. When combined with tetracycline antibiotics, the anti-inflammatory effect of sulfasalazine is weakened (the mechanism is that the tetracycline antibiotics inhibit the intestinal flora and prevent the decomposition of sulfasalazine to 5-aminosalicylic acid, which makes it have anti-inflammatory effects. Weakened). Therefore, it is best to avoid the use of tetracycline antibiotics during the treatment with sulfasalazine.

11. Due to complexation, ferrous sulfate may interfere with the absorption of sulfasalazine in the body.

12. In vivo studies on rats have shown that cholestyramine can be combined with sulfasalazine in the intestine, so that sulfasalazine cannot be broken down by bacteria in the intestine, so it increases with fecal excretion in its original form. Whether this interaction occurs in the human body has yet to be confirmed. However, to avoid this interaction, it is recommended that the interval between the two drugs be taken as long as possible.

13. When sulfasalazine is combined with folic acid, the absorption of the latter is reduced, and the blood concentration is reduced (the mechanism is not clear). For patients with inflammatory bowel disease who need simultaneous medication, parenteral administration of folic acid can avoid this interaction.

14. Combined with calcium gluconate, it can cause delayed absorption of sulfasalazine.

15. Sulfasalazine can induce cytochrome P450-mediated cyclosporine metabolism, thereby reducing the efficacy of cyclosporine.

16. The combination of sulfasalazine and live typhoid vaccine can reduce the latter's antibacterial activity against Salmonella typhi. Therefore, a typhoid vaccine should be given 24 hours or more after the last application of sulfasalazine ^[2] .

Sulfasalazine Expert Review

Sulfasalazine should be a clinical immunosuppressant, and it is often the drug of choice for non-specific inflammation. Such as ulcerative colitis, arthritis of unknown origin and other significant effects. Can also be used for Crohn's disease. Sulfasalazine is an azo compound of salicylic acid and sulfasalazine. It has special affinity for connective tissue of the intestinal wall, and has antibacterial, anti-inflammatory and immunosuppressive effects. After oral administration, most of the bacteria in the intestine break down into salicylic acid and sulfadiazine and work ^[2] .