Pharmacodynamics and pharmacokinetics

Sulfasalazine is an anti-inflammatory drug. It has an immunosuppressive effect in connective tissue, in the thickness of the intestinal wall and serous fluid (its highest concentration is located). Thanks to the intestinal flora, the drug breaks down:

• to sulfapyridine , which suppresses the proliferation of T-killer and the transformation of lymphocytes;
• to 5-aminosalicylic acid ( Mesalazine ), the most significant compound for the treatment of inflammatory diseases of the large intestine. Mechanism of action: binding of free oxygen radicals, local inhibition of cyclooxygenase and lipoxygenase , which is necessary to prevent the formation of prostaglandins , leukotrienes and other inflammatory mediators .

Pharmacokinetics

Approximately 30% of the dose is absorbed in the wall of the small intestine, the remaining 70% is broken down by the intestinal flora of the large intestine. Subsequently, the active substance enters the intestines along with bile , and is also excreted in unchanged form in the urine in small quantities. The half-life is 5-10 hours.

The released sulfapyridine in the liver (via acetylation , hydroxylation , conjugation with glucuronic acid ), excretion occurs through the kidneys. Approximately 30% of mesalazine is absorbed and acetylated by the liver, excreted by the kidneys in urine or in unchanged form in feces.

pharmachologic effect

The active substance Sulfasalazine has an anti-inflammatory and antimicrobial effect aimed at pathogens of intestinal diseases. The use of the drug in the treatment of nonspecific colitis is quite effective.

The active component of this drug selectively accumulates in the tissues of the intestinal walls and promotes the release of acids, which are characterized by anti-inflammatory activity. The drug also has an antimicrobial effect against Streptococcus spp., including Streptococcus pneumoniae, Neisseria gonorrhoeae and Escherichia coli.

Contraindications

• blood diseases;
• severe liver or kidney dysfunction;
• porphyria;
• deficiency of glucose-6-phosphate dehydrogenase;
• children under 5 years old;
• III trimester of pregnancy, lactation;
• overreaction to the components of the drug, sulfonamides , as well as salicylic acid .
• Prescribe with caution for bronchial asthma and the risk of allergic reactions.

Side effects of Sulfasalazine

Undesirable side effects may occur from the following systems and organs of the human body during therapy with Sulfasalazine

• Peripheral and central nervous system: attacks of headache, dizziness, hallucinations , tinnitus, ataxia , convulsions, various sleep disorders, development of peripheral neuropathy .
• Urinary system: renal dysfunction, possible interstitial nephritis .
• Digestive system: nausea, vomiting, diarrhea, abdominal pain, anorexia , development of hepatitis , pancreatitis .
• Respiratory system: can cause damage to lung tissue, interstitial pneumonitis .
• Hematopoietic system: agranulocytosis , anemia , thrombocytopenia , leukopenia .
• Reproductive system: infertility , a transient phenomenon of oligospermia .
• Allergic reactions: fever , skin rash , possible anaphylactic shock .
• Among others: yellowness of the skin, contact lenses , urine.

Side effects

When metabolized, sulfasalazine becomes sulfapyridine. Its blood concentration should be checked every three months, and even more often before travel. Concentrations of about 50 mg/l lead to side effects. In rare cases, sulfasalazine can cause severe depression, malaise, paresthesia, convulsions, tremors, tinnitus, and infertility. There have been cases of immune thrombocytopenia.

Sulfasalazine inhibits dihydropteroate synthase and may cause folate deficiency and megaloblastic anemia.

Sulfasalazine may cause hemolytic anemia in people with favism (glucose-6-phosphate dehydrogenase deficiency).

Sulfasalazine may cause stomach upset, nausea, vomiting, loss of appetite, headache, dizziness or strange tiredness, or allergic reactions.

Instructions for use of Sulfasalazine (Method and dosage)

The tablets should be taken orally, after meals.

For ulcerative colitis and granulomatous enteritis (Crohn's disease)

Treatment regimen for adults and children over 16: first daily dose - 2 g, divided into 4 doses, second - 4 g, divided into 4 doses; the third and all subsequent ones - 6-8 g, divided into 4 doses. When acute clinical manifestations subside, a maintenance daily dose of 1.5-2 g, divided into 3-4 doses, is sufficient. Maintenance therapy can last several months, but it is not recommended for children under 16 years of age weighing up to 65 kg.

Maximum daily doses depending on the age of patients: adults - 8 g, children - 2 g.

For left-sided distal localization of the lesion, microenemas and suppositories can be used - 1 g of Sulfasalazine with 1.6 g of cocoa butter is injected into the rectum 2 times a day.

For rheumatoid arthritis, incl. juvenile

Standard treatment regimen for adults and children over 16: in the first week of treatment, the recommended daily dose is 500 mg, in the second - 1000 mg (divided into 2 doses), in the third - 1500 mg (divided into 3 doses).

The therapeutic dose ranges from 1.5 to 3 g per day. To achieve a clinical effect, 6–10 weeks are needed, treatment can last more than 6 months.

Sulfasalazine

Stock

dyucha speech:

1 tablet of sulfasalazine 500 mg;

additional speeches:

povidone, pregelatinized starch, magnesium stearate, anhydrous silica, hypromelose, propylene glycol.

Medicine form Tablets, covered with spit coating.

Pharmacotherapeutic group

Anti-inflammatory properties that can stagnate when the intestines are sick. Aminosalicylic acid and similar products.

ATX code A07E C01.

Clinical characteristics

Showing

– Induction and maintenance of remission in viral colitis; treatment of Crohn's disease in the active stage.

– Treatment of rheumatoid arthritis in adults due to the insufficient effectiveness of non-steroidal anti-inflammatory drugs (NSAIDs).

– Treatment of juvenile polysubglobal or oligosubglobal rheumatoid arthritis.

Contraindicated

– Hypersensitivity to sulfasalazine, its metabolites, sulfonamides or salicylates;

– intestinal obstruction or obstruction of the sechovidous passages;

– porphyria, fragments were reported about the effects of sulfonamides during acute attack;

– level of severe level of liver (glomerular filtration rate < 30 ml/xv/1.73 m2) and/or level of severe level of liver;

– patients with a history of severe asthma attacks, urticaria, rhinitis or other allergic reactions caused by acetylsalicylic acid or other NSAIDs. In such patients, fatal anaphylactic reactions have been reported;

– children up to 6 years of age.

Method of congestion and dosage

The dose should be adjusted according to the severity of illness and possible side effects. The tablets must be taken within an hour of driving, washed down with a bottle of ripeness. If you miss a dose, take it earlier before you have too little time to take the next dose. In such a situation, the patient should only take the prescribed dose.

The tablets must be rolled whole, do not break or crack.

Summer age patients: special precautions during the day.

Virascovian colitis

mature

A hard fight

: 2-4 tablets of the drug Sulfasalazine 4 times per dose, which can be taken in patients taking steroids as part of an intensive therapy regimen. If the tablets are used too quickly, the effectiveness of the drug may be reduced.

The initial interval between doses may not exceed 8 years.

Overcoming mortal gravity

: 2-4 tablets 4 times per dose, possibly stagnant if taking steroids.

Overcoming light severity

: 2 tablets 4 times per dose with or without steroids.

Supportive therapy

: after induction of remission, the dose of the drug is gradually reduced to 4 tablets per dose. At this dose, the drug must be taken gradually, the fragments from the administered bath are passed through a splinter of rocks after an acute attack, the risk of relapse increases 4 times.

Children

Change the dose proportionally to body weight.

In case of acute attack or relapse: 40-60 mg/kg per dose.

Supportive treatment: 20-30 mg/kg per dose.

Crohn's disease

In case of Crohn's disease, the drug should be taken according to the same scheme as for viral colitis (virulent colitis).

Rheumatoid arthritis

mature

In patients with rheumatoid arthritis and patients who have been taking NSAIDs for at least three hours, they may be sensitive to the disease, and in those who become ill, the drug Sulfasalazine should be taken according to recommendations. ій. Treatment should be started with 1 tablet per dose, gradually increasing the dose by 1 tablet per day until the dose reaches 1 tablet 4 times per dose or 2 tablets 3 times per dose depending on the tolerability and effectiveness of the drug. The effect manifests itself in full and a pronounced effect may not be prevented for 6 days. A decrease in the friability of the pulp may be accompanied by changes in erythrocyte sedimentation fluidity (ESF) and C-reactive protein levels. Possible alternative to NSAIDs and the drug Sulfasalazine.

Juvenile polyglobular or oligoglobular rheumatoid arthritis.

Children have been around for 6 years.

30-50 mg/kg/dose, divided into 4 doses. Set the maximum dose to 2000 mg/dose. To relieve possible intolerance in the side of the scolio-intestinal tract, start by taking ¼ of the planned booster dose with further advancements of ¼ skin stretch until the booster dose is reached.

Adverse reactions

The most common adverse reactions associated with sulfasalazine administration in viral colitis were decreased appetite, headache, boredom, vomiting, scholax disorder and renal oligospermia. These reactions occurred in approximately one third of patients. Taki Victorich reaction, Yak Sverbiz, Kropiv'yanka, Visipannia, Pirdvishennya Tizhni Tila, anemia size of the Heinz, hemolic anemia і tsanosis, vinikeli ridhe (1 to 30 Patsіtvs Abo Mensher). Evidence shows that with a stable dose of 4 g or more and with a total level of sulfapyridine in blood serum of 50 mcg/ml, the frequency of adverse reactions tends to increase.

Administration of sulfasalazine for rheumatoid arthritis in adults was associated with a high incidence of similar adverse reactions, although the frequency of such reactions was significant. In studies of rheumatoid arthritis, the following adverse reactions were often identified: tiredness (19%), dyspepsia (13%), nausea (13%), headache (9%), abdominal pain (8%), vomiting (8%), and nausea body temperature (5%), congestion (4%), stomatitis (4%), itching (4%), abnormal liver function test results (4%), leukopenia (3%) and thrombocytopenia (1%). There was one message about 10% suppression of immunoglobulin. This reaction has little reversal and is rarely accompanied by clinical symptoms.

Overall, adverse reactions in patients with juvenile rheumatoid arthritis are similar to those expected in adult patients with rheumatoid arthritis, except for the high incidence of rheumatoid arthritis-like syndrome. ї illness, in case of systemic treatment of juvenile rheumatoid arthritis. In one clinical study, there was a 10% decrease in immunoglobulin suppression.

Although the number of side reactions that have been reported in the treatment of this particular drug is limited, the pharmacological similarity of the sulfonamides is similar, so that in the case of the treatment with the drug Sulfasalazine there is no harm The skin was affected by these reactions.

Adverse reactions that occur infrequently or rarely

Infections and invasions:

aseptic meningitis, pseudomembranous colitis.

On the side of the blood and lymphatic systems:

pancytopenia, aplastic anemia, agranulocytosis, megaloblastic (macrocytic) anemia, purpura, hypoprothrombinemia, methemoglobinemia, macrocytosis, congenital neutropenia and myelodysplastic syndrome.

On the side of the immune system:

erythema multiforme (Stevens-Johnson syndrome), exfoliative dermatitis, epidermal necrolysis (Lyell's syndrome) with corneal scars, drug therapy with eosinophilia and systemic symptoms (DRESS), anaphylaxis, Syrovatkov's syndrome illness, interstitial disease, pneumonitis with or without eosinophilia, vasculitis , fibrous alveolitis, pleurisy, pericarditis for or without tamponade, allergic myocarditis, polyarteritis nodules, wolf-like syndrome, hepatitis and liver necrosis for or without immune complexes, fulminant hepatitis, which should be brought to trans liver plantations, acute parapsoriasis (Much-Haberman syndrome) , rhabdomyolysis, photosensitization, arthralgia, periorbital plaque, injection of the conjunctiva and tunica albuginea and alopecia, hypersensitivity reactions.

On the side of the scolio-intestinal tract:

hepatitis, liver failure, pancreatitis, bloody diarrhea, impaired absorption of folic acid, impaired absorption of digoxin, stomatitis, diarrhea, abdominal pain and neutropenic enterocolitis, acute viral colitis.

Mental disorders:

depression.

On the side of the central nervous system:

disorders due to relish, transverse myelitis, somitis, meningitis, transverse damage to the dorsal cord of the spinal cord, Quinn's tail syndrome, Guyan-Baré syndrome, encephalopathy, peripheral neuropathy, suppression of mental functions, seizure confusion, loss of hearing, disturbances in smell, insomnia, ataxia, hallucinations , vomiting noise and drowsiness.

On the side nirok:

toxic nephropathy with oliguria and anuria, nephritis, nephrotic syndrome, infections of the thyroid gland, hematuria, crystalluria, proteinuria and hemolytic-uremic syndrome, interstitial nephritis t.

Other reactions:

change in color of the skin, change in color of the skin, erythema, alopecia, skin stain.

Sulfonamides may have significant chemical similarities to certain goitrogenic drugs, diuretics (acetazolamide and thiazides) and oral hypoglycemic drugs. Patients who withdraw from sulfonamides rarely experience severe goiter, hypoglycemia, and diuresis.

These individuals may be wary of over-sensitivity. Obviously, the squirrels are especially sensitive to the goitrogenic effects of sulfonamides, and their long-term stagnation in the animal species resulted in malignant swellings of the thyroid gland.

Post-launch updates

Below are the indications that were revealed during the postoperative period of stagnation in clinical practice of drugs that replace mesalamine (or are metabolized before its administration). Remnants of awareness were voluntarily fed into a population of unknown size, and it is impossible to estimate their frequency. These findings were determined through a combination of factors such as severity, frequency of reporting, or potential causal association with mesalamine.

On the side of the blood system and lymphatic blood system:

pseudomononucleosis.

On the side of the heart:

myocarditis.

On the side of the hepatobiliary system:

information about hepatotoxicity, time-dependent liver function analysis (CGOT/AST, SGPT/ALT, GGT, LDH, urinary phosphatase, bilirubin), cholestatic hepatitis, cirrhosis, cholestatic hepatitis, cholestasis and possible hepatocellular damage, including necrosis of the liver and liver insufficiency. Several of these episodes resulted in death. One episode of a syndrome similar to Kawasaki syndrome, involving changes in liver function, has been reported.

On the side of the immune system:

anaphylaxis.

On the side, the exchange of speech, metabolism:

loss of appetite, folate deficiency.

On the side of the thyroid system:

nephrolithiasis.

On the side of the respiratory system, chest and mediastinum:

cough, dyspnea, oropharyngeal pain.

On the side of the skin and under the skin fabric:

angioedema, purpura, exanthema, toxic pustuloderma, lichen planus, photosensitivity, Gougerot-Sjögren syndrome.

From the side of the vessel:

brightness.

The danger of medicinal use and its longevity:

was not reported.

Laboratory research:

Enhancement of liver enzymes, induction of autoantibodies.

Overdose

There is evidence that the frequency and severity of toxic reactions during overdose are directly related to the total concentration of sulfapyridine in blood serum. Symptoms of overdose may include nausea, vomiting, bowel dysfunction and abdominal pain. In more severe episodes, symptoms from the side of the central nervous system, drowsiness, and other symptoms may occur. To monitor the process of swelling after overdose, sulfapyridine concentrations in blood serum can be measured.

Patients with impaired function are at risk of severe toxicity.

There are no documented reports of fatalities resulting from the use of large single doses of sulfasalazine. It is impossible to calculate LD50 in laboratory animals, zokrem mice, animal fragments, the oral dose of sulfasalazine that could be administered (12 g/kg) did not lead to lethal results. Regular administration of sulfasalazine at a dose of 16 g per dose in the form of tablets did not lead to death in patients.

Instructions for overdose.

The indications include rinsing the mucus or stimulating vomiting and stagnation of carry-over preparations. Subdued section. For normal function, it is never necessary to intensively saturate the body with water. If oliguria is detected, separate the amount of injected liquid and salt and carry out further treatment. In case of complete blockade of nitric crystals, catheterization of the sechoducts can be performed. The low molecular weight of sulfasalazine and its metabolites may be used as an aid to dialysis.

Patients are monitored for signs of the development of methemoglobinemia or sulfhemoglobinemia. If these conditions are evident, appropriate therapy is prescribed.

Suspension during pregnancy or breastfeeding

Vaginism

According to the published data on the use of sulfasalazine in pregnant women, there is no evidence of the risks of teratogenic influx. The likelihood of a negative effect on the pregnancy when taking sulfasalazine during pregnancy is low. When administered orally, sulfasalazine inhibits the absorption and metabolism of folic acid and can lead to folic acid deficiency. The loose influx does not turn off completely, sulfasalazine should be frozen during the period of pregnancy unless absolutely necessary.

Breast bath period

Sulfasalazine and sulfapyridine are excreted in breast milk. It is necessary to administer the drug with care to women who are breastfeeding, especially when nursing premature babies or those who suffer from a deficiency of glucose-6-phosphate dehydrogenase. The decision to wash the breast is taken by the doctor at the doctor’s office and the breast tissue/risis for the mother and child.

Children

It was reported to investigate the safety and effectiveness of sulfasalazine in treating the signs and symptoms of juvenile rheumatoid arthritis with polyarthritis syndrome in patients with rheumatoid arthritis of the age. 6 to 16 roki. Extrapolation of data from adult patients with rheumatoid arthritis to children with juvenile rheumatoid arthritis and polyarthritic syndrome is based on the similarity of illness and the effectiveness of therapy in these two groups of patients. ntiv. The published results confirm the possibility of extrapolating data on the safety and effectiveness of sulfasalazine in juvenile rheumatoid arthritis with polyarthritic syndrome (section “Adverse reactions”).

A high incidence of unexpected symptoms was reported in patients with systemic juvenile arthritis. Administration of the drug to children with systemic history of juvenile rheumatoid arthritis often resulted in a reaction similar to that of serum sickness. Often this reaction was severe and manifested itself as increased body temperature, nausea, vomiting, headache, vomiting and nausea, which were not normal in liver function tests. Treatment with sulfasalazine in systemic cases of juvenile rheumatoid arthritis is not recommended.

Features of stastosuvannya

Sulfasalazine zocrema indications for patients with viral colitis who cannot take uncoated sulfasalazine tablets due to intolerance in the side of the scolio-intestinal tract and in whom there are signs that intolerance is not mainly associated with high blood levels sulfapiridine and its metabolites in the blood, for example, in patients with fatigue and vomiting when taking the first few doses of the drug, or in patients in whom a reduced dose did not change the side effects on the side of the intestinal tract. Patients with rheumatoid arthritis or juvenile rheumatoid arthritis should continue to maintain a regimen of repairs and physical procedures as indicated. When used with anti-inflammatory drugs, the effect of the drug Sulfasalazine is not immediately avoided. It is recommended to carry out concomitant treatment with analgesics and/or non-steroidal anti-inflammatory drugs until the effect of the drug appears.

It was reported about liver disease and a decrease in the level of enzymes in blood syringation during treatment with 5-aminosalicylic acid/mesalazine products in patients with a history of liver diseases. Therefore, Sulfasalazine is contraindicated for patients with severe liver disease (section “Contraindications”). It is necessary to exercise caution when stagnating the drug in patients with liver problems ranging from mild to moderate severity and to use the drug only in the wash, since the crustiness from stagnation significantly outweighs the risk for the patient nta. It is necessary to monitor liver functions before starting therapy and periodically during treatment. Reports of illnesses, which included minimal change nephropathy and chronic interstitial nephritis, were associated with mesalamine and other derivatives. Sulfasalazine is contraindicated for patients with severe nitric disorders (section “Contraindications”). It is necessary to exercise caution when stagnating the drug in patients with mild to moderate levels of severity and sterilize the drug only in the wash, since the crustiness of stagnation significantly outweighs the risk for the patient . It is necessary to control the functions of the skin before starting therapy and periodically during treatment. Fatal episodes due to hypersensitivity reactions, agranulocytosis, aplastic anemia, other blood dyscrasias, liver damage, and irreversible nerve changes have been reported to be associated with sulfasalazine administration. ovo-muscular and central nervous system and fibrous alveolitis. The presence of clinical symptoms such as sore throat, increased body temperature, pallor, purpura or erythema may be signs of serious blood disorders or hepatotoxicity. Patients who are discontinuing the drug Sulfasalazine should undergo a complete blood test, as well as a blood test with detailed microscopic examination. During the period of checking the results of blood tests, it is necessary to treat with sulfasalazine.

Oligospermia and infertility may occur in men treated with sulfasalazine. When the drug is removed, the development of these effects occurs over a period of 2-3 months.

Serious infections, including fatal sepsis and pneumonia, have been reported. Some infections were associated with agranulocytosis, neutropenia or myelosuppression. If a patient has a serious infection, it is necessary to stop the drug. Before and after treatment with the drug, it is necessary to carefully monitor the patient's condition for signs and symptoms of infection. A patient who develops a new infection during treatment with the drug should undergo immediate and extensive diagnostic follow-up to identify infection and myelosuppression. It is necessary to be careful when considering the possibility of sulfasalazine ingestion in patients with a history of recurrent or chronic infections or concomitant illnesses or sudden drug ingestion, which may cause complications development of infection in the patient.

Severe hypersensitivity reactions can affect the internal organs, causing hepatitis, nephritis, myocarditis, mononucleosis-like syndrome (pseudomononucleosis), pathological changes in the side of the blood (zocrema, hematophagic g istiocytosis) and/or pneumonitis, including eosinophilic infiltration.

Serious skin reactions have been reported in association with sulfasalazine ingestion, such as lethal hepatitis, exfoliative dermatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis. Patients are at greatest risk for developing these symptoms early in therapy, and most of these symptoms occur during the first month of treatment.

Sulfasalazine should be discontinued at the first appearance of rash on the skin, pathological changes in the mucous membrane, or other signs of hypersensitivity.

Severe life-threatening systemic hypersensitivity reactions have been reported, such as drug treatment for eosinophilia and systemic symptoms in patients taking sulfasalazine. If symptoms are not avoided, early signs of hypersensitivity may appear, such as elevated body temperature or lymphadenopathy. If such signs or symptoms are evident, it is necessary to carefully bandage the patient’s waist. If it is impossible to identify another cause for the development of these signs or symptoms, treatment with sulfasalazine must be initiated.

Monitor patients with hypersensitivity to furosemide, thiazide diuretics, carbonic anhydrase inhibitors for signs of sagging on the skin, deterioration of the mucous membranes, or other manifestations and allergic reactions, through possible hypersensitivity to the drug Sulfasalazine in such patients.

Zapobizhni come in.

Zagalni position.

The drug should be prescribed with caution to patients with severe allergies or bronchial asthma. To preserve crystalluria and dissolve stones, it is necessary to ensure that a sufficient amount of the source reaches the body. Patients with glucose-6-phosphate dehydrogenase deficiency should be closely monitored for signs of hemolytic anemia. This reaction needs to be stored in the dose. In case of toxic reactions or hypersensitivity reactions, administer the drug carefully.

Information for patients.

Patients should be informed of the possibility of side effects and the need for close medical care. The appearance of a sore throat, increased body temperature, pallor, purpura or erythematosus may indicate a serious blood disorder. If any reaction occurs, the patient must seek medical help.

Patients should be instructed that the drug should be taken in two equal doses, within an hour, and to crush the tablets as needed. It is necessary to know that sulfasalazine can be used to change the color of the cut or skin to orange-yellow.

Virus colitis.

Patients with virulent colitis should be aware that virulent colitis is rarely present, and the risk of acute inflammation may be significantly reduced after prolonged use of the drug Sulfasalazine at an adjustable dose. .

Rheumatoid arthritis.

Rheumatoid arthritis is rarely known completely. This is why the drug is recommended to be used in a trival manner. Further monitoring of patients who need to take sulfasalazine is carried out by physicians to ensure that the drug does not require constant administration.

Laboratory analyses.

Before starting treatment with the drug Sulfasalazine for the skin during the first 3 months of therapy, it is necessary to carry out a complete blood test with a leukocyte count and an analysis of liver function. Before the next 3 months, such analyzes must be carried out once a month, and then every 3 months and for clinical indications. Also, periodically, during treatment with the drug Sulfasalazine, it is necessary to conduct an internal analysis of the tissue and evaluate the function of the drug.

It may be possible that the concentration of sulfapyridine in serum is higher than that of 50 mcg/ml, which is likely to be associated with an increased frequency of adverse reactions.

Oral sulfasalazine inhibits the absorption and metabolism of folic acid, which can cause its deficiency in the body (section “Congestion during pregnancy or breastfeeding”) and, in turn, increases potency but be aware of the development of serious disorders on the side of the blood system (such as macrocytosis and pancytopenia).

This is due to the fluidity of the reaction when using vehicles or robots with other mechanisms.

The effect of sulfasalazine on the fluidity of the reaction during treatment with vehicles or robots with other mechanisms has not been systematically assessed.

Interactions with other medicinal drugs and other types of interactions

There was a decrease in the absorption of folic acid and digoxin when they were ingested for one hour with sulfasalazine.

It was reported about bone marrow suppression and leukemia with one-hour infusion of thiopurine 6-mercaptopurite or its derivatives, azathioprine, and sulfasalazine (oral infusion).

Single-dose administration of high doses of sulfasalazine 2 g and upper doses of methotrexate 7.5 mg in 15 patients with rheumatoid arthritis (with drug interactions observed) did not change the pharmacokinetics data these medicinal services.

Additional doses of sulfasalazine 2 g (maximum 3 g) and upper doses of methotrexate 7.5 mg (maximum 15 mg) were administered as monotherapy or as a combination in 310 patients with rheumatoid arthritis in two controls 52- Current clinical studies. The overall toxicity profile for this combination revealed an increase in the frequency of unwanted side effects of the scolio-intestinal tract, especially nausea, equal to the frequency that should be avoided when these drugs are frozen. in Okremo.

Laboratory displays.

There was a notice about the possible influx of normetanephrine on the results of laboratory tests (uniform chromatography), which led to a negative-positive result in patients who took sulfasalazine or its metabolite, mesalamine/mesalazine .

Pharmacological authorities

Pharmacodynamics.

Sulfasalazine is used as an anti-inflammatory agent. Carry out immunosuppressive action, especially in healthy tissue, intestinal tract and serous tissue, where the concentration is found. Due to the intestinal flora, sulfasalazine is broken down to sulfapyridine and 5-aminosalicylic acid. Sulfapiridine suppresses the proliferation of cellin cells and the transformation of lymphocytes. The anti-inflammatory action of 5-aminosalicylic acid (mesalazine) is most important for the treatment of inflammatory diseases of the large intestine. The main effect is that it locally inhibits cyclooxygenase and lipoxygenase at the intestinal station, thereby preventing the creation of prostaglandins, leukotrienes and other mediators of inflammation. Also, it probably binds acid radicals.

Pharmacokinetics.

Approximately 30% of the administered dose of sulfasalazine is absorbed from the small intestine; The other 70% is metabolized by the intestinal flora in the large intestine to sulfapyridine and 5-aminosalicylic acid. Maximum concentrations of sulfasalazine and its metabolites in plasma may vary greatly in different patients - at low levels of acetylation, stench is more pronounced and is associated with frequent episodes of unpleasant symptoms. It binds well to plasma proteins and healthy tissue. The majority of the absorbed amount of sulfasalazine is lost from the intestines; an insignificant amount of thickness is visible in the unchanged appearance from the cross-section. The period of administration of sulfasalazine should be 5 to 10 years.

Most of the compounded sulfapyridine is absorbed and reaches maximum concentration in blood serum 12-24 years after taking the drug. Metabolized in the liver (by acetylation, hydroxylation and conjugation with glucuronic acid) and excreted by nitric acid. The recovery period is 6 to 14 years, depending on the speed of acetylation. Only about 30% of 5-aminosalicylic acid is absorbed and acetylated in the liver and excreted through the skin. Rashta appears unchanged with feces.

Pharmaceutical characteristics

The main physical and chemical agents are round, brownish-yellow, slightly biconvex tablets with beveled edges, covered with a clear, barless spitting film.

The term of attachment is 5 rocks.

Umovi sberіgannya

Store at a temperature not exceeding 25 °C. Keep out of the reach of children.

Package

10 tablets per blister; 5 blisters per cardboard box.

Release category

For the recipe.

Virobnik

KRKA, d.d., Novo mesto/KRKA, dd, Novo mesto.

Misceznahodzhennya

Smarjeska cesta 6, 8501 Novo mesto, Slovenia/Smarjeska cesta 6, 8501 Novo mesto, Slovenia.

Sulfasalazine analogs

Level 4 ATX code matches:

Analogs where the active substance is the same are Salazopyrin En and Sulfasalazine En . There are generics that are similar in pharmacological action, but the active ingredient is mesalazine , among them the most famous are:

• Asakol;
• Mesacol;
• Pentasa;
• Samesil.

Which is better: Sulfasalazine or EH?

The main difference between Sulfasalazine EH and Sulfasalazine is the chemical structure of the film shell of the tablets. Sulfasalazine EH has a special enteric film coating, which gives better bioavailability and absorption of the active substance, for example, when taking Sulfasalazine EH, 90% of the dose reaches the large intestine, and only 70% of the “simple” intestine. However, Sulfasalazine EH is produced by the American company Pfizer and therefore costs about a third more.

Reviews of Sulfasalazine

Reviews from patients are only positive, but in 2020 the issue of the lack of the drug in pharmacies in the Russian Federation became acute. At the forums, they agree on the possibility of sending the drug by mail from the nearest countries of the former CIS.

Reviews of Sulfasalazine for rheumatoid arthritis indicate its effectiveness, and, importantly, the possibility of treating the juvenile form of the disease. However, the course is quite long and some people note side reactions in the form of a rash and are worried about the negative impact on the functioning of the liver and kidneys.

Sulfasalazine price, where to buy

Average price of Sulfasalazine per pack of 50 tablets. dosage 500 mg – 310 rub.

• Online pharmacies in RussiaRussia
• Online pharmacies in UkraineUkraine
• Online pharmacies in KazakhstanKazakhstan

ZdravCity

• Sulfasalazine-EN tablets p.p.o. intestinal 500 mg 50 pcs. KRKA JSC/KRKA RUS LLC
• Sulfasalazine tablets p.p.o. 500 mg 50 pcs. Ozone LLC

Pharmacy Dialogue

• Sulfasalazine-EN (tablet p/o 500 mg No. 50)KPKA
• Sulfasalazine-EN (tablet p/o 500 mg No. 50) KRKA-RUS./KRKA

Europharm* 4% discount using promo code medside11

• Sulfasalazin-ene 500 mg 50 tablets KRKA-rus./KRKA
• Sulfasalazine 500 mg 50 tablets Ozon LLC

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Pharmacy24

• Sulfasalazine-EH 500 mg No. 50 tablets KRKA, Slovenia
• Sulfasalazine 500 mg No. 50 tablets KRKA, Slovenia

PaniPharmacy

• SULFASALAZINE tablets Sulfasalazine film-coated tablets 500 mg No. 50 Slovenia, KRKA dd Novo Mesto
• Sulfasalazine EN tablets Sulfasalazine EN tablets 500 mg No. 50 Slovenia, KRKA dd Novo Mesto

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Release form and composition

The drug Sulfasalazine-EN is manufactured in the dosage form of enteric-coated tablets intended for oral administration. They have a round shape, a biconvex surface, and a yellow or light brown color. The main active ingredient of the drug is sulfasalazine, its content in one tablet is 500 mg. It also contains additional components

Sulfasalazine-EN tablets are contained in a blister of 10 pieces. The cardboard pack contains 5 blisters with tablets (50 pieces), as well as instructions for use.