阿普斯特使用注意事项、用法用量、不良反应？

Apprex is an orally available, small molecule phosphodiesterase inhibitor. Because it can increase intracellular cAMP levels and inhibit the production of pro-inflammatory factors and chemokines, it is helpful in the treatment of autoimmune diseases such as psoriasis. Apremilast is rapidly absorbed and has an appropriate half-life. Clinical studies have shown that Apremilast has certain efficacy in the treatment of psoriasis and psoriatic arthritis, with mild adverse reactions and good tolerance.

Precautions for use

1. Pay attention to your diet: While using Apremilast, avoid eating it with grapefruit, grapefruit juice and other citrus fruits, as well as foods with high caffeine and tea content, as these foods may interfere with the metabolism and absorption of the drug.

2. Observe drug side effects: Severe diarrhea, nausea and vomiting may occur when using Apremilast. Most events occur within the first few weeks of treatment. Therefore, patients are advised to closely observe their own reactions in the first few weeks of medication.

3. Observe the patient’s reaction: Treatment with Apremilast will increase the incidence of depression. Therefore, the benefits and risks of apremilast therapy should be carefully weighed before being administered to patients with a history of depression, suicidal thoughts, or behavioral problems.

Patients, their caregivers, and their family members should be informed of the development or worsening of depression, suicidal thoughts, or other emotional changes and should contact their health care provider if these changes occur. If such an event occurs, the prescriber should carefully evaluate the risks and benefits of continued treatment with apremilast.

4. Drug interactions: Pay attention to drug interactions during use of Apremilast. Concomitant use of apremilast with the CYP450 inhibitor rifampicin may reduce the systemic exposure of apremilast, thereby affecting the therapeutic efficacy of apremilast. Therefore, it is not recommended to use rifampicin, phenobarbital, carbamazepine, phenytoin and other drugs in combination with Apremilast.

5. Special medication groups: Since the safety and effectiveness of Apremilast in children under 18 years of age have not yet been determined, it is not recommended for children under 18 years of age to use Apremilast.

If you are pregnant, planning to become pregnant, or breastfeeding, you should consult your doctor before using Apremilast. The safety and effectiveness of Apremilast in pregnant or lactating women is currently unclear, so the decision to use Apremilast needs to be made under the guidance of a doctor.

6. Regular follow-up: During the period of using Apremilast, regular follow-up visits and examinations are required to ensure efficacy and safety. At the same time, communicate with your doctor regularly and report any new symptoms or changes promptly.

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The recommended initial dose titration of Apremilast from Days 1 to 5 is shown in Table 1. After 5 days of dose escalation, the recommended maintenance dose is 30 mg twice daily orally starting on Day 6. This titration is intended to reduce gastrointestinal symptoms associated with initial treatment.

In patients with severe renal impairment (muscle clearance (CLcr) less than 30 m/min as estimated by the Cockcroft-Gault formula), the dose of apremilast should be reduced to 30 mg once daily. For initial dose titration in this group, it is recommended to titrate apremilast using only the AM regimen listed in Table 1, skipping the PM dose.

Apremire and treatment measures

Apremilast is an oral medication used to treat psoriasis and may cause some adverse effects. The following are some common adverse reactions and their treatments:

1. Nausea and diarrhea: Apremilast may cause nausea and diarrhea. It is recommended to take the medication after meals to reduce gastrointestinal discomfort. If severe nausea and diarrhea persist, it is recommended to inform your doctor promptly, as the dose may need to be adjusted or the medication may need to be discontinued.

2. Headache: Some patients may experience headache when using Apremilast. You can try rest and relaxation to relieve symptoms. If the headache lasts for a long time or seriously affects the quality of life, you should consult a doctor. Ibuprofen, celecoxib and other drugs can be used under the guidance of the doctor.

3. Depression and anxiety: A small number of patients may experience psychological symptoms such as depression and anxiety. If severe depression, anxiety or other mental status changes occur, you should consult a doctor, adjust the dose or discontinue the drug under the doctor's evaluation, and use fluoxetine and other drugs for treatment.

4. Infection: Using Apremilast may increase the risk of infection. If infection symptoms such as fever, cough, sore throat, frequent urination, and urgency of urination occur, anti-infective drugs can be used for treatment.

5. Skin reactions: A few patients may develop skin reactions such as rash and urticaria. If skin discomfort occurs, it may be caused by allergies. Patients can use loratadine, cetirizine and other drugs as directed by the doctor.

Apremilast treatment effect

One study evaluated the efficacy/safety of 30 mg of apremilast taken twice daily in the treatment of moderate to severe plaque psoriasis. A total of 844 patients were randomized. At Week 16, patients taking apremilast experienced a 75% or greater reduction in Psoriasis Area and Severity Index score (PASI-75) from baseline compared with placebo (33.1%; primary endpoint).

The majority (61.0%) of patients were randomized again to apremilast at Week 32 and reached a PASI-75 score at Week 52, while 11.7% were randomized again to placebo. Among patients who were rerandomized to receive apremilast at Week 32, the mean percentage change from baseline PASI score was -88% to -81% (Weeks 32-52).

Summary

The above describes the precautions, usage and dosage of Apremilast. However, due to individual differences in each patient, the most accurate usage guidance should be provided by a doctor based on the patient's specific situation.