Crohn's disease is an intestinal pathology that tends to progress. The inflammatory process spreads transmurally and is characterized by various local and systemic complications. The disease affects the entire thickness of the intestinal wall, narrows its lumen, and forms infiltrates, abscesses and ulcers. To stop the disease process, the patient is prescribed anti-inflammatory drugs.
Such effective medications for eliminating the symptoms of Crohn's disease and ulcerative colitis (UC) include the medications "Sulfasalazine-EN" and "Sulfasalazine". Medicines are also prescribed for rheumatoid arthritis to relieve pain and inflammation. Like many drugs, they have their contraindications and side effects. What does the drug “Sulfasalazine-EN” consist of? What is its difference from “Sulfasalazine”? All information can be found in the article.
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.
Action
The drug is used to eliminate the symptoms of Crohn's disease and UC. Sulfasalazine is released to aminosalicylic acid, which has an anti-inflammatory effect at the site of erosion. Sulfapyridine is also formed, which has antimicrobial activity and inhibits the functions of gonococci, streptococci and Escherichia coli.
When taken orally, the tablets are almost not absorbed in the intestines. Here they are broken down under the influence of intestinal microflora and form sulfapyridine by 75% and aminosalicylic acid by 25%. Over the course of three days, the substances are mainly excreted by the kidneys and only in a tiny percentage by feces. This effect on the patient’s body is exerted by the drug “Sulfasalazine-EN”. The difference from Sulfasalazine, reviews about the drug - all this information should be studied before starting treatment.
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.
Indications and contraindications
The medicine is prescribed for the following pathologies:
- UC;
- Crohn's disease;
- various forms of rheumatoid arthritis.
Contraindications:
- severe pathology of the kidneys and liver;
- blood diseases;
- age up to 5 years;
- increased hypersensitivity to the components.
The drug “Sulfasalazine - EN” has an insignificant difference from “Sulfasalazine”. Instructions for use describe similar indications and contraindications. A specialist will tell you which medication to use in a particular case.
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.
The drug "Salofalk"
The medicine has anti-inflammatory properties and is prescribed for Crohn's disease and UC. Available in the form of yellow tablets. The drug contains mesalazine in doses of 250 and 500 and 1 g. The drug has an anti-inflammatory, antioxidant effect on the intestinal wall
Indications:
- UC;
- Crohn's disease
Contraindications:
- blood diseases;
- preschool children;
- hypersensitivity to components.
At the beginning of the treatment process, you should carefully study all the features of the drug “Salofalk” and “Sulfasalazine-EN”. The difference from Sulfasalazine in application is not significant. The drugs are taken according to a similar scheme.
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.
Instructions for Sulfasalazine and dosage when used in pediatrics:
- children 6-8 years old, weighing 20-29 kg - 1 tablet 2 times a day;
- 8-12 years old, weight 30–39 kg - 1 tablet up to 3 times a day;
- 12 - 16 years old, weight - 40-45 kg - 1 tablet 3 times a day or 2 tablets 2 times a day;
- from 16 years of age with a weight over 50 kg - 2 tablets 2 times a day.
With ankylosing spondylitis
When it turns out that treatment with NSAIDs and hormones is ineffective, Sulfasalazine is used as a basic drug that can inhibit the inflammatory process in the joints. It is taken for a long time – 3-6 months. until the onset of a healing effect and relief of the patient’s condition, then use maximum doses and begin to discontinue other drugs, then reduce the dosage and discontinue the anti-inflammatory drug itself.
Sulfasalazine is not able to stop the pathological process in ankylosing spondylitis, however, the achieved effect can last a couple of months ( NSAIDs in small doses) and then resumption of therapy is required.
Sulfasalazin
A complete clinical blood count, including white blood cell count, red blood cell and platelet counts, and biochemical liver function tests should be performed before starting sulfasalazine and every other week for the first three months of therapy. Over the next three months, the same laboratory tests should be performed monthly, then once every three months and in accordance with clinical indications.
Assessment of renal function (including urinalysis) should be performed in all patients before starting therapy and at least monthly during the first three months of treatment. Thereafter, monitoring should be performed as clinically indicated.
The presence of clinical signs such as sore throat, fever, pale skin, purpura or jaundice during sulfasalazine therapy may indicate myelosuppression, hemolysis or hepatotoxicity.
Treatment with sulfasalazine should be discontinued until the results of blood tests are obtained (see section "Special Instructions", subsection "Influence on laboratory results").
Life-threatening skin reactions: SSD and TEN have been reported with the use of the drug Sulfasalazine. Patients should be alerted to clinical signs and symptoms and should be closely monitored for the development of skin reactions. The highest risk of developing SJS and TEN is during the first weeks of treatment. If clinical manifestations or symptoms of SJS and TEN occur (eg, progressive skin rash, often with blistering or mucosal involvement), treatment with Sulfasalazine should be discontinued.
The best results in the treatment of SJS and TEN are achieved with early diagnosis and immediate discontinuation of any suspicious drug. Early discontinuation of the drug is associated with a better prognosis.
If a patient develops SJS or TEN while taking Sulfasalazine, sulfasalazine therapy should not be restarted in that patient.
Impact on laboratory results
In patients exposed to sulfasalasia or its metabolite (mesalamine/mesalazine), there have been several reports of possible false-positive urinary normeganephrine liquid chromatography results.
Sulfasalazine or its metabolites may interfere with ultraviolet absorption, especially at 340 nm, as well as with some laboratory tests using dihydronicotinamide adenine dinucleotide (NADH) or dihydronicotinamide adenine dinucleotide phosphate (NADPH) to measure ultraviolet absorption at this wavelength. Examples of such tests may include: determination of concentrations of urea, ammonia, lactate dehydrogenase (LDH), α-hydroxybutyrate dehydrogenase and glucose.
When using sulfasalazine in high doses, changes in serum alanine aminotransferase (ALT), aspartate aminotransferase (AST), creatine kinase-muscle/brain (CK-MB), glutamate dehydrogenase, or serum thyroxine concentrations may occur.
Consult with your diagnostic laboratory regarding the laboratory testing technique to be used. Caution should be used when interpreting these results in patients taking sulfasalazine. Results should be interpreted in conjunction with clinical data.
Sulfasalazine analogs
Level 4 ATC code matches:
Mesacol
Salofalk
Mesalazine
Pentasa
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.
When is the medication used?
The medicine is prescribed for the following pathologies:
- UC;
- Crohn's disease;
- rheumatoid arthritis.
It is prohibited to take the medicine in the following cases:
- kidney and liver disease;
- anemia;
- porphyria;
- pregnancy;
- lactation;
- hypersensitivity to substances included in the drug.
Before starting the treatment process, it is necessary to carefully study all contraindications to taking the drug “Sulfasalazine-EN”. Difference from “Sulfasalazine, special instructions - all information is important. The drug can be used after consultation with a specialist.
Reviews of Sulfasalazine
Feedback from patients is only positive, but in 2015 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.
Dosage
On the first day of treatment for adults, the medicine is prescribed in a dose of 500 mg 4 times, then on the second day - 1 g 4 times, then the drug is taken from 1.5 to 2 g per day. The course of treatment depends on the severity of the process and the individual characteristics of the body.
An overdose can lead to the development of the following symptoms:
- migraine;
- convulsions;
- insomnia;
- epigastric pain;
- vomit;
- diarrhea;
- allergy.
The drug Sulfasalazine-EN has less pronounced side effects. The difference from Sulfasalazine is that the medication is coated.
If it was not possible to purchase any of the drugs described at the pharmacy, a specialist will select a high-quality substitute.
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 tablets p.p.o.
500 mg 50 pcs. Ozon LLC 325 rub. order - Sulfasalazine tab. p/o captivity. 0.5g 50pcs JSC KRKA, d.d., Novo Mesto
RUB 373 order
- Sulfasalazine-EN tablets p.p.o. intestinal 500 mg 50 pcs. KRKA JSC/KRKA RUS LLC
RUR 386 order
Pharmacy Dialogue
- Sulfasalazine-EN (tablet p/o 500 mg No. 50) KRKA-RUS./KRKA
476 rub. order
- Sulfasalazine-EN (tablet p/o 500 mg No. 50)KRKA/Vector-Medica
476 rub. order
- Sulfasalazine-EN (tablet p/o 500 mg No. 50)KPKA
RUB 432 order
- Sulfasalazine (tablet p/o 500 mg No. 50)KPKA
RUB 447 order
- Sulfasalazine (tab.p.pl.vol. 500 mg No. 50) Ozone LLC
RUB 231 order
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Pharmacy24
- Sulfasalazine-EH 500 mg No. 50 tablets KRKA, Slovenia
366 UAH. order - Sulfasalazine 500 mg No. 50 tablets KRKA, Slovenia
362 UAH order
PaniPharmacy
- SULFASALAZINE tablets Sulfasalazine film-coated tablets 500 mg No. 50 Slovenia, KRKA dd Novo Mesto
353 UAH. order
- Sulfasalazine EN tablets Sulfasalazine EN tablets 500 mg No. 50 Slovenia, KRKA dd Novo Mesto
414 UAH order
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The drug "Sulfasalazine"
The drug belongs to the group of anti-inflammatory drugs, prescribed for the treatment of Crohn's disease and ulcerative colitis. Produced in yellow-brown tablet form. The medicine contains sulfasalazine (500 mg).
The drug has anti-inflammatory and antimicrobial effects. It also has immunosuppressive and antirheumatic effects. The main substance of the tablets, sulfasalazine, has a positive effect on the intestines thanks to two active components. These are sulfapyridinone and aminosalicylic acid. The drug “Sulfasalazine-EN” has a bacteriostatic effect against diplococci, staphylococci and Escherichia coli. Difference from "Sulfasalazine", description of the active ingredient - all information is presented in the instructions.
Medicine "Sulfasalazine-EN". Difference from Sulfasalazine: patient reviews
Two drugs identical in composition. The only difference is that Sulfalazine-EN is coated, soluble only in the intestines, unlike Sulfasalazine tablets, which are film-coated. Also, the first medicine causes more allergic reactions, which manifest themselves in the form of rashes and itching on the skin. If you believe the reviews of patients, the drug "Sulfasalazine" is in great demand.
Experts note that both drugs can lead to the development of side effects. There is nausea, vomiting and stomach pain. At the same time, Sulfasalazine-EN has a slight difference from Sulfasalazine. Photos of medicines are also similar.
Experts note that this group of medications does not help everyone to the same extent. These drugs are not reliable enough for damage to peripheral joints. To avoid the development of urolithiasis, it is advisable to take the tablets with plenty of mineral water and drink plenty of fluids throughout the day. What other difference does “Sulfasalazine-EN” have from “Sulfasalazine”? Although the analogue (the drug “Salofalk”) is prescribed for similar pathologies, it has many more discrepancies. This is due to the difference in composition.