伊曲莫德(Etrasimod)的副作用如何缓解

Common side effects and incidence rates of Etrasimod

1. Headache: the incidence rate is about 9% (UC-1) and 6% (UC-2/UC-3).

2. Elevated liver enzymes: the incidence is about 6% (UC-1) and 5% (UC-2/UC-3).

3. Dizziness: the incidence rate is about 5% (UC-1).

4. Nausea, joint pain, high blood pressure, urinary tract infection, etc. have also been reported, with the incidence rate ranging from 2% to 5%.

Serious side effects and management strategies of Etrasimod

1. Increased risk of infection

It can cause a decrease in peripheral blood lymphocyte count, making patients susceptible to various infections.

Routine blood tests (including lymphocyte count) need to be tested before treatment; signs of infection need to be closely monitored during treatment and within 5 weeks after stopping treatment; treatment should be interrupted when serious infection occurs; live vaccines should be avoided, and vaccination should be completed 4 weeks before the start of treatment.

2. Bradycardia and conduction delay

A series of special electrophysiological reactions such as a transient decrease in heart rate and atrioventricular conduction delay can often be seen when taking the drug for the first time.

An electrocardiogram is required before treatment; those with a history of heart disease need to consult a cardiologist; avoid combined use with antiarrhythmic drugs, beta-blockers, etc.

3. Liver damage

A few patients have ALT elevations exceeding 3 times the upper limit of normal.

Check liver function and bilirubin before treatment and regularly during treatment; the drug should be discontinued when symptoms of liver damage (such as nausea, jaundice, dark urine) occur.

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.

4. Macular edema

Although vision changes occur relatively rarely, we should not take it lightly and be alert to vision changes at any time.

Carry out fundus examinations before and regularly during treatment; if vision loss occurs, seek medical attention immediately.

5. Skin malignant tumors

Long-term use of itrimod may increase the risk of skin cancer.

Regular skin examination before and during treatment; avoid UV exposure and use high protection factor sunscreen.

Itramod (Etrasimod) pharmacokinetics

1. Absorption and distribution

The median Tmax after oral administration of Etrasimod is about 4 hours; high-fat diet does not affect its absorption; the apparent volume of distribution is about 66L, and the plasma protein binding rate is as high as 97.9%.

2. Metabolism and excretion

Mainly metabolized through CYP2C8, CYP2C9 and CYP3A4; secondary metabolic pathways include UGT-mediated conjugation reactions. The average elimination half-life is about 30 hours; about 82% is excreted in feces, 11% is unchanged drug; 5% is excreted in urine.

3. Pharmacokinetics in special groups

(1) People with liver dysfunction: The exposure of patients with severe liver damage (Child-PughC) increases by 57%, and its use is not recommended.

(2) CYP2C9 slow metabolizers: Exposure increases when combined with CYP2C8 or CYP3A4 inhibitors, so combined use should be avoided.

(3) Age, gender, and renal insufficiency: No dosage adjustment is required.