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Salazopyrine 500mg is used to treat ulcerative colitis. On the market today, there is a lot of information about Salazopyrine 500mg drug product, but it is still incomplete. To learn more about Salazopyrin, please read the article below.
1. What is Salazopyrine 500mg?
Salazopyrine is an anti-inflammatory drug that works well in the treatment of arthritis and ulcers in the duodenal or stomach area.
Salazopyrine is manufactured by the multinational pharmaceutical company Pfizer, USA, with the ingredients in the drug that will act on the condition and other related problems quickly, protect the digestive tract the best, Medicine is an indispensable choice for patients.
Main ingredients and content of the drug:
Active ingredient Sulfasalazine for 500mg content; In addition, the drug also contains water and other excipients, just enough for one tablet. The drug has a dosage form that is:
Tablets and packed in the form of a box, each box has 1 vial containing 100 tablets. Pharmacodynamics of Salazopyrine 500mg:
Sulfasalazine is a compound of sulfapyridine and 5-aminosalicylic acid. Sulfasalazine is also considered a prodrug, because after oral administration, the diazo bond is cleaved by intestinal bacteria to form sulfapyridine and 5-aminosalicylic acid (mesalamin) which have local antibacterial and anti-inflammatory effects. . The enteric therapeutic effect of sulfasalazine is due to metabolites produced in the colon. The ADR of sulfasalazine will include ADR caused by sulfapyridine and mesalamin. In addition, the effect of the drug may be due to the action of sulfasalazine to change the pattern of intestinal flora, reduce Clostridium and E. coli bacteria in stool, inhibit prostaglandin synthesis leading to diarrhea and affect motility. Mucus translocation, altered colonic fluid secretion and absorption, electrolytes and/or immunosuppression. Sulfasalazine also contributes to the reduction of inflammatory activities in rheumatoid arthritis, but the role of the drug and its metabolites in this effect is unknown; sulfasalazine is often used alone or in combination with corticosteroids to treat ulcerative colitis, active Crohn's disease, especially of the colon. Sulfasalazine is also used as a disease-modifying drug (DMARD) to treat severe or progressive rheumatoid arthritis. Sulfasalazine is not recommended for the treatment of juvenile rheumatoid arthritis because of the potential for serious ADRs. Pharmacokinetics of Salazopyrine 500mg:
Absorption: After oral administration, about 10-15% of a dose of sufasalazine will be absorbed as unchanged drug from the small intestine. A small percentage of absorbed sulfasalazine is excreted via bile into the intestine (entero-hepatic circulation). The remainder of the oral dose of sulfasalazine passes intact into the colon, where the diazo-linker is cleaved by colonic bacteria into sulfapyridine and mesalamine. Sulfapyridine is also rapidly absorbed from the colon. Only a small amount of mesalamine is absorbed in the colon. Following oral administration of a single 2 g dose of sulfasalazine to healthy subjects, peak plasma sulfasalazine concentrations reached 14 micrograms/ml within 1.5 to 6 hours. Peak plasma sulfapyridine concentrations will reach 21 micrograms/ml within 6-24 hours. Following a single oral dose of 2 g sulfasalazine delayed release and peak plasma sulfasalazine concentrations reached 6 micrograms/ml within 3-12 hours. Peak plasma sulfapyridine concentrations will reach 13 micrograms/ml within 12-24 hours. Distribution: Small amounts of sulfasalazine are also absorbed, strongly bound to plasma proteins and ultimately excreted unchanged in the urine. The drug crosses the placenta and is found in breast milk. Metabolism: After absorption, sulfapyridine undergoes hepatic N4 acetylation and cyclic hydroxylation, followed by conjugation with glucuronic acid. Elimination: The mean plasma half-life of sulfasalazine would be 5.7 hours after a single dose and 7.6 hours after multiple doses. The half-life of sulfapyridine is 8.4 hours after a single dose and 10.4 hours after multiple doses. After the sulfasalazine molecule is broken down in the colon, 60-80% of sulfapyridine is absorbed and extensively metabolized in the liver by acetylation, hydroxylation and conjugation with glucuronic acid. Peak steady-state concentrations of sulfapyridine were also higher in slow acetylators than in fast acetylators with the same oral dose. Like sulfasalazine, sulfapyridine is absorbed across the placenta and into breast milk. Much less mesalamine is absorbed and about one-third of the released mesalamine is absorbed and most of it is acetylated and excreted in the urine.
2. Uses of Salazopyrin 500mg
2.1. Anti-inflammatory effects of Salazopyrin 500mg
Sulfasalazine inhibits superoxide production by granulocytes after they have been stimulated by immune complexes or formyl peptides. In addition, 5-ASA is also a powerful trap for free radicals. Other functions of granulocytes would include degeneration, chemotaxis, and random migration inhibited by sulfasalazine.
Sulfasalazine is a relatively weak inhibitor of cyclooxygenase, but will have a strong inhibitory effect on 15-prostaglandin dehydrogenase (PGDH), the main enzyme in prostate metabolism.
Sulfasalazine has been shown to inhibit several enzymes involved in lipoxygenase arachidonic acid metabolism, including 5-lipoxygenase (5-LO) and leukotriene C4 synthetase (LTC4). In addition, sulfasalazine has been shown to inhibit the release of lipoxygenase products by inflammatory cells and tissues.
All of these effects of sulfasalazine on enzymes that metabolize arachidonic acid lead to a decrease in lipoxygenase-induced inflammatory responses, parallel to an increase in immunosuppressive and anti-inflammatory prostaglandins paralysis may affect the clinical activity of the drug.
2.2. Impact on immune function
Salazopyrine 500mg clinically active is also considered to be of autoimmune origin, so the effect of Sulfasalazine on immune cells is of interest. In vitro, Sulfasalazine inhibits both natural killer (NK) activity and T-cell proliferation.
2.3. Antibacterial activity Sulfasalazine and its major metabolites inhibit bacterial overgrowth. It also had a decrease in the proliferation of certain bacterial species of the gut microbiota after treatment with Salazopyrine. Salazopyrine 500mg is also indicated as adjunctive therapy for severe ulcerative colitis, appendicitis or distal ulcerative colitis, and Crohn's disease. This drug is especially useful in long-term treatment. Salazopyrine 500mg is indicated for the treatment of active rheumatoid arthritis when treatment with any of the usual first-line drugs has been ineffective.
3. Side effects of Salazopyrine 500mg
During treatment, patients may also encounter undesirable effects such as: Common:
For the whole body: Fever, anorexia and headache; Blood: Decreased white blood cell count, hemolytic anemia and megaloblastic anemia; On the digestive system: Nausea, vomiting, epigastric pain and abdominal pain; On the skin: Rash, urticaria, rash and erythema; On the liver: Transaminase elevation transient; Other reactions: Reversible decrease in sperm count. Uncommon:
For the whole body: body fatigue; Blood: Loss of granulocyte count; On nerves: Depression ; On hearing: Tinnitus. Rare:
On the immune system: Angioedema and serum sickness; Blood: Pancytopenia, loss of granulocyte count, platelet count and macrocytic anemia; On the digestive system: Pancreatitis; On the skin: systemic lupus erythematosus, Lyell syndrome- epidermal necrolysis, Stevens-Johnson syndrome, exfoliative dermatitis and increased photosensitivity; On the liver: Hepatitis; On the respiratory system: Alveolitis will be accompanied by fibrosis, cough and respiratory failure; On musculoskeletal: Pain in joints.; On the nervous system: Aseptic meningitis and diseases related to peripheral nerves; On the urinary system: Proteinuria, hematuria, the appearance of crystals in the urine and nephrotic syndrome; Other reactions: Disorders of perception of smell and changes in taste. 4. Salazopyrine 500mg Drug Interactions There may be an interaction between Salazopyrine 500mg and any of the following substances: Azathioprine, Benzocaine, Benzydamine, Celecoxib, Cyclosporine, Dapsone, folic acid, Heparin, Hexylresorcinol, Lidocaine, Heparin fecal weight low mortality, drugs that increase sun sensitivity, mercaptopurine, methotrexate, nitric oxide, nonsteroidal anti-inflammatory drugs, olsalazine, prilocaine, regorafenib, other salicylates, sulfinpyrazone, tedizolid, teriflunomide, tetracaine, tolvaptan, micro-vaccines - withdraw varicella.
5. How to use Salazopyrine 500mg effectively
5.1. How to take Salazopyrine 500mg Take the tablet whole with plenty of water, do not crush, break, crush, do not mix the medicine with water to drink. You can drink it before or after you eat.
5.2. Recommended dosage For peptic ulcer disease, the colon will have:
Elderly people: No indication to restrict use; Adults: Initially use 1-2g per day corresponding to 2-4 tablets / day, take 3-4 times / day, each time is about 6-8 hours apart. An enteric delayed-release tablet is possible for doses of 0.5-1g per day. When feeling much better, reduce the dose to 2 tablets per day. In addition, the drug is recommended to be maintained for a certain period of time to avoid recurrence of the disease; Children: The amount of medicine prescribed will depend on the age and weight of the child. For acute illness, use 40mg/kg to 60mg/kg daily. The recommended maintenance dose to avoid relapse is 20mg/kg to 30mg/kg. Salazopyrine is also prescribed flexibly depending on the development of the disease as well as the body's tolerance to the drug.
5.3. Overdose and overdosage treatment It is necessary to strictly follow the dose and use method prescribed by the doctor; If abnormal symptoms appear, the patient should be taken to the nearest medical facility for timely treatment.
6. Be careful when using and storing
Notes and cautions:Please read the instructions for use carefully before you take this medicine. Use caution when using the drug in patients with impaired liver and kidney function. Do not use expired drugs or show signs of spoilage, mold... Pregnant and lactating women:
Consider before using the drug for pregnant or breastfeeding women. mother milk. Drivers and machine operators:
Be careful when using the drug on drivers, operators of dangerous machinery and equipment, patients with impaired liver and kidney function. Storage:
Store the medicine in a cool, dry place, with appropriate humidity, the temperature is below 30 degrees Celsius. Avoid placing the medicine in humid places, where children or pets can reach or places where there is direct sunlight for a long time. In summary, Salazopyrine is an anti-inflammatory drug that works well in the treatment of arthritis and ulcers in the duodenal or stomach area. To ensure safety and promote treatment effectiveness, users need to use the drug exactly as prescribed by the doctor.
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