Apremilast: 7 things you should know

Medically reviewed by Carmen Pope, BPharm. Last updated on Sep 28, 2023.

1. How it works

• Apremilast is a small molecule phosphodiesterase 4 (PDE4) inhibitor that may be used for the treatment of plaque psoriasis, psoriatic arthritis, and oral ulcers associated with Behçet’s Disease.
• Apremilast works by blocking the phosphodiesterase type 4 (PDE4) enzyme which helps to reduce levels of inflammation in the body, and decreases symptoms such as pain, redness, and swelling. Its exact mechanism is not known.
• Apremilast belongs to the class of medicines known as phosphodiesterase 4 (PDE4) inhibitors.

2. Upsides

• May be used to treat plaque psoriasis, psoriatic arthritis, and oral ulcers associated with Behçet’s Disease.
• Apremilast is taken orally (by mouth) twice a day.
• Can be administered with or without food.
• Apremilast is available in three dosage strengths: 10mg (pink), 20mg (brown), and 30mg (beige).
• No dosage adjustment is needed in people with liver disease.
• Apremilast is a generic, it is also available under the brand name Otezla.

3. Downsides

If you are between the ages of 18 and 60, take no other medication or have no other medical conditions, side effects you are more likely to experience include:

• Diarrhea, nausea, vomiting, stomach pain, weight loss, upper respiratory tract infections, headache, and tension headaches are the most commonly reported side effects of apremilast. Over time, many of these side effects will subside. Some people experienced severe diarrhea, nausea, and vomiting that required hospitalization. Older patients may be at greater risk, especially if they are at risk of low blood pressure or dehydration, or taking medications that can worsen these effects.
• Apremilast may lower a person's mood and increase suicidal thoughts. Tell your doctor if you have ever had problems with mood or depression. You and your family members should be on the alert for signs of worsening depression, suicidal thoughts, or other mood changes. If such changes should occur with your treatment, contact your doctor immediately.
• The dosage of apremilast needs to be reduced to 30mg once daily in people with moderate to severe kidney disease (creatinine clearance (CLcr) of less than 30 mL per minute). During the titration period, apremilast should be given as 10mg daily for 3 days then increased to 20mg daily for two days, then 30mg daily thereafter.
• Experience with using apremilast in pregnant women is extremely limited and there is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to apremilast during pregnancy (call 1-877-311-8972). Animal studies have shown that apremilast may increase the risk of miscarriage and that it is present in the milk of lactating animals, so it is likely to be present in human milk.

Note: In general, seniors or children, people with certain medical conditions (such as liver or kidney problems, heart disease, diabetes, seizures) or people who take other medications are more at risk of developing a wider range of side effects. View complete list of side effects

4. Bottom Line

Apremilast is a PDE4 inhibitor that may be used to treat plaque psoriasis, psoriatic arthritis, and oral ulcers associated with Behçet’s Disease. It has been associated with severe diarrhea, nausea, and vomiting and the initial dosage should be increased slowly up to the recommended maintenance dose.

5. Tips

• Most stomach-related side effects, like diarrhea, nausea, vomiting, and stomach pain due to apremilast occur within the first weeks of starting treatment. In some cases, patients were hospitalized for these effects. To help reduce your risk of gastrointestinal side effects, your doctor will gradually increase your dose over 5 days. The recommended maintenance dosage is 30 mg twice daily starting on Day 6.
• Do not crush, split, or chew apremilast, swallow the tablets whole. Apremilast may be taken with or without food.
• If you develop severe diarrhea, nausea, or vomiting, tell your doctor immediately. Side effects of severe diarrhea or vomiting typically improve quickly with dose reduction or discontinuation of apremilast. Do not stop taking apremilast unless recommended by your doctor.
• If you notice that you are having signs or symptoms of depression or worsened depression, suicidal thoughts, or other mood changes while taking apremilast, contact your doctor immediately. Your family members should also help to monitor you for these changes. Before starting treatment with apremilast, tell your doctor if you have ever had problems with mood or depression.
• Weight loss can be a significant side effect of apremilast. Your doctor will monitor your body weight regularly, and decide if it is safe for you to remain on apremilast.
• Tell your doctor or pharmacist that you are taking apremilast before you take any other medications, such as those for cancer, epilepsy, or depression. Apremilast may interact with some herbal supplements and other medications.
• Tell your doctor if you are breastfeeding, pregnant, or intending to become pregnant before taking apremilast because it may not be suitable for you. If you inadvertently become pregnant while taking apremilast, enroll on the registry that monitors pregnancy outcomes in women exposed to apremilast during pregnancy (call 1-877-311-8972).

6. Response and effectiveness

• A decrease in symptoms may be noted within the first few weeks of apremilast treatment; however, it may take up to 12 to 16 weeks for the full effects to be seen.
• Research has shown that 32% to 41% of adults with psoriatic arthritis had at least a 20% improvement after 16 weeks (compared to 18% to 19% of the inactive placebo group). Improvements in physical functioning and the ability to perform daily activities (like dressing, walking, eating, grip, and personal hygiene) were also improved in patients with psoriatic arthritis.
• 28.8% to 33.1% of adults with plaque psoriasis saw at least a 75% improvement after 16 weeks (compared to 5.3% to 5.8% of the inactive placebo group). For adults with Behcet's disease, 52.9% were free of oral ulcers at 12 weeks (compared to 22.3% in the inactive placebo group). Of this group, 30% of patients taking apremilast were ulcer-free at 6 weeks. Pain relief began as early as 2 weeks.

7. Interactions

Medicines that interact with apremilast may either decrease its effect, affect how long it works, increase side effects, or have less of an effect when taken with apremilast. An interaction between two medications does not always mean that you must stop taking one of the medications; however, sometimes it does. Speak to your doctor about how drug interactions should be managed.

Common medications that may interact with apremilast include:

• antiandrogens, such as apalutamide and enzalutamide, which can reduce blood levels of apremilast
• chemotherapy agents such as mitotane
• corticosteroids, such as dexamethasone
• CYP450 3A4 inducers, such as carbamazepine, fosphenytoin, phenobarbital, phenytoin, and rifampin (may reduce the effectiveness of apremilast)
• echinacea
• griseofulvin
• St. John's Wort
• targeted treatments such as brigatinib and dabrafenib.

Apremilast may also increase the metabolism of modafinil and armodafinil.

Note that this list is not all-inclusive and includes only common medications that may interact with apremilast. You should refer to the prescribing information for apremilast for a complete list of interactions.

References

• Apremilast. Updated 07/2023. Amneal Pharmaceuticals NY LLC https://www.drugs.com/pro/apremilast.html

Further information

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use apremilast only for the indication prescribed.

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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