美沙拉秦(Salofalk)的注意事项和药物相互作用

Mesalazine (Salofalk) exerts local anti-inflammatory effects by releasing the drug in specific parts of the intestine.

Mesalazine (Salofalk) Precautions

1. Monitoring of vital organ function

(1) Kidney function: Serum creatinine, urea nitrogen and urinary sediment need to be monitored regularly before and during treatment. If renal damage occurs, the drug should be discontinued immediately.

(2) Liver function: Use with caution in patients with mild to moderate hepatic insufficiency, and contraindicated in patients with severe impairment. It is recommended to monitor liver enzyme indicators such as ALT and AST.

(3) Pulmonary function: People with existing asthma or sulfonamide allergy need to be cautious, and should be evaluated promptly if they experience pulmonary symptoms such as difficulty breathing and coughing.

2. Blood and skin reactions

(1) Blood system: occasionally thrombocytopenia, aplastic anemia, etc. If abnormal bleeding, fever, or sore throat occurs, routine blood tests must be performed immediately.

(2) Skin reactions: Although serious skin adverse reactions (such as DRESS, SJS) are rare, once they occur, the drug must be permanently discontinued.

3. Other special warnings

(1) Acute intolerance syndrome: manifests as abdominal pain, fever, rash, etc., which is easily confused with disease recurrence and needs to be promptly identified and discontinued.

(2) Intracranial hypertension: Rare pseudotumor cerebri, manifesting as persistent headache and visual impairment, drug discontinuation and investigation need to be considered.

(3) Sodium intake: Each 500mg tablet contains 49mg of sodium. Patients with sodium restriction should pay attention to the total daily intake.

The pictures are from public channels (such as the official website of the FDA, the official website of the original drug manufacturer, etc.) and are for reference only.

Mesalazine (Salofalk) drug interactions

1. Enhance the effects of other drugs

(1) Anticoagulants: combination with warfarin may increase the risk of bleeding, and coagulation indicators need to be closely monitored.

(2) Antidiabetic drugs: They may enhance the hypoglycemic effect of sulfonylurea drugs, so be wary of hypoglycemia.

(3) Immunosuppressants: Combination with azathioprine, etc. may aggravate bone marrow suppression, and routine blood monitoring should be strengthened.

2. Weaken the efficacy or increase the toxicity

(1) Diuretics: The diuretic effect of spironolactone and furosemide may be weakened.

(2) Methotrexate: Its hematological and hepatotoxicity may increase when used together.

(3) Uric acid excretion drugs: The effects of uric acid excretion-stimulating drugs such as probenecid may be weakened.

3. Other interactions

(1) Influence of intestinal pH: Lactulose and other drugs that lower intestinal pH may interfere with the enteric release of mesalazine.

(2) Rifampicin: It may weaken the anti-inflammatory effect of mesalazine, so please pay attention to the changes in efficacy.

Mesalazine (Salofalk) Pharmacokinetics

1. Absorption and distribution

(1) Absorption characteristics: Enteric coating ensures the release of the drug in the ileocecal region and colon. The fasting gastric emptying time is about 0.79 hours, and the absorption rate is low.

(2) Protein binding: The plasma protein binding rate of mesalazine is 43%, and its main metabolite N-acetyl-5-ASA is 78%.

2. Metabolism and excretion

(1) Metabolic pathway: Mainly converted into the inactive metabolite N-acetyl-5-ASA through acetylation in the intestinal mucosa and liver.

(2) Excretion mode: <1% of the original drug is excreted through the kidneys, about 24% of the metabolites are excreted through urine, and most of them are excreted through feces.

3. Advantages of dosage form

Targeted release: Relying on pH-dependent coating technology to ensure precise release of the drug in the diseased intestinal area and maximize the local anti-inflammatory effect.