阿普斯特不良反应有哪些

Apremilast is a PDE4 inhibitor. PDE4 plays an important role in the hydrolysis process of cAMP. The inhibition of PDE4 leads to an increase in intracellular cAMP levels, thereby inhibiting immune and inflammatory responses. Apremilast is effective in treating psoriasis, but there are also adverse reactions during use, including diarrhea, nausea, upper respiratory tract infections and headaches, including tension headaches, as detailed below.

Adult subjects with active psoriatic arthritis were evaluated in 3 similarly designed multicenter, randomized, double-blind, placebo-controlled trials (PsA-1, PsA-2, and PsA-3). Across the three trials, 1493 subjects were equally divided into placebo groups, apremilast 20 mg twice daily or apremilast 30 mg twice daily. Titrate during the first 5 days. At Week 16, placebo subjects who did not experience at least a 20% improvement in joint tenderness and swelling counts were rerandomized in a blinded 1:1 manner to apremilast 20 mg twice daily or 30 mg while the apremilast subject remained on initial treatment. Participants ranged in age from 18 to 83 years old, with an overall median age of 51 years.

Most of the most common adverse reactions shown in Table 1 occurred within the first 2 weeks of treatment and tended to resolve over time with continued dosing. Diarrhea, headache, and nausea were the most common adverse reactions.

The most common adverse reactions leading to discontinuation were nausea (1.8%), diarrhea (1.8%), and headache (1.2%). The proportion of psoriatic arthritis subjects who discontinued treatment due to any adverse effects was 4.6% (apremilast 30 mg twice daily) and 1.2% (placebo treatment).

Table 1: As of Day 112 (Week 16), adverse reactions were reported in ≥ 2% of subjects taking apremilast 30 mg twice daily and ≥ 1% were observed in subjects taking placebo

	Placebo		Apremilast30 mg*
Adverse reactions	Day 1 to Day 5 days (N = 495) n (%) †	Day 6 to Day 112 days (N = 490) n (%)	Day 1 to Day 5 days (N = 497) n (%)	Day 6 to Day 112 days (N = 493) n (%)
Diarrhea	6 (1.2)	8 (1.6)	46 (9.3)	38 (7.7)
Disgusting	7 (1.4)	15 (3.1)	37 (7.4)	44 (8.9)
headache	9 (1.8)	11 (2.2)	24 (4.8)	29 (5.9)
upper respiratory tract infection	3 (0.6)	9 (1.8)	3 (0.6)	19 (3.9)
Vomiting	2 (0.4)	2 (0.4)	4 (0.8)	16 (3.2)
Nasopharyngitis	1 (0.2)	8 (1.6)	1 (0.2)	13 (2.6)
upper abdominal pain	0 (0.0)	1 (0.2)	3 (0.6)	10 (2.0)

*BID = twice daily.

†n (%) indicates the number and percentage of subjects.

‡Among the gastrointestinal adverse reactions reported, 1 subject experienced serious adverse reactions of nausea and vomiting after taking OZLA 30 mg twice daily; 1 subject receiving OZLA 20 mg twice daily experienced severe diarrhea; and 1 subject receiving OZLA 30 mg twice daily experienced serious adverse reactions of headache.

§None of the reported adverse drug reactions were serious.

Patients have different conditions and constitutions, and the adverse reactions after taking the medicine are also different. It is recommended that patients take the medicine under the guidance of a doctor. If there is intolerance, contact the doctor in time for symptomatic treatment.

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