Apremilast: Understanding The Benefits & Side Effects

Psoriasis is a chronic condition that extends beyond the skin, often affecting confidence, daily comfort, and overall well-being. 

For those with psoriatic arthritis, the added burden of joint pain and stiffness can significantly impact mobility and quality of life. Effective, long-term management is essential, but finding the right treatment remains challenging.

While multiple treatment options exist, many come with limitations. Some require injections, others need frequent monitoring, and none provide consistent relief. 

Patients often struggle to find a solution that balances effectiveness, convenience, and tolerability. As a result, some patients seek oral, non-biologic options for symptom management.

Apremilast is an oral medication representing a novel approach to managing psoriasis and psoriatic arthritis. It provides a convenient, non-biologic option that helps simplify treatment while supporting long-term symptom management.

[signup]

What is Apremilast?

Apremilast is an oral medication classified as a small-molecule inhibitor of phosphodiesterase 4 (PDE4). By targeting this enzyme, apremilast is designed to modulate certain inflammatory pathways.

It offers a different approach to treatment compared to injectable biologic therapies and is often used to manage chronic inflammatory conditions.

Mechanism of Action

Apremilast works by inhibiting the enzyme phosphodiesterase 4 (PDE4), which breaks down a molecule called cyclic adenosine monophosphate (cAMP). 

Higher cAMP levels result in a reduction of inflammatory mediators like TNF-α, IL-23, and IL-8. 

This process helps decrease inflammation and may help reduce symptoms in some patients with psoriatic arthritis, plaque psoriasis, and Behcet disease.

Approved Uses

Apremilast is an oral medication FDA-approved to manage certain inflammatory conditions in adults, including:

• Psoriatic arthritis to help manage joint pain, swelling, and stiffness in moderate to severe cases

• Plaque psoriasis in individuals who are candidates for phototherapy or systemic therapy to improve skin symptoms

• Oral ulcers associated with Behcet disease to relieve painful mouth sores

Dosage and Administration of Apremilast

Apremilast is an oral medication used to manage inflammatory conditions, with a recommended maintenance dose of 30 mg twice daily.

To minimize gastrointestinal side effects, the dosage is gradually increased over six days as follows:

• Day 1: 10 mg in the morning

• Day 2: 10 mg in the morning and 10 mg in the evening

• Day 3: 10 mg in the morning and 20 mg in the evening

• Day 4: 20 mg in the morning and 20 mg in the evening

• Day 5: 20 mg in the morning and 30 mg in the evening

• Day 6 and thereafter: 30 mg twice daily

Dosing should follow the prescribing information, and adjustments should be made based on medical supervision.

Administration Instructions

Apremilast can be taken with or without food. The tablets should be swallowed whole without crushing, breaking, or chewing.

Dosage Adjustment for Renal Impairment

For patients with severe kidney impairment (creatinine clearance < 30 mL/min), the maintenance dose should be reduced to 30 mg once daily, following the morning titration schedule only.

Side Effects of Apremilast

Apremilast may cause various side effects. While some are common and manageable, others may require immediate medical attention.

Common Side Effects

• Diarrhea

• Nausea

• Headache

• Upper respiratory tract infection (URTI)

Consult your healthcare provider for guidance for persistent or bothersome common side effects.

Serious Side Effects

Potential serious adverse effects reported with apremilast use include:

• Mood changes or signs of depression

• Suicidal thoughts or behavior

• Severe allergic reactions, such as difficulty breathing or swelling of the face, lips, or throat

• Unexplained significant weight loss

Clinical trials and post-marketing surveillance have reported these side effects, but individual responses may vary. If you experience any serious side effects, seek medical attention immediately.

Contraindications for Apremilast

When considering apremilast, it's important to understand the conditions under which its use is not recommended.

Individuals with known allergies to apremilast or any of its ingredients should not use this medication. Treatment should be discontinued if an allergic reaction occurs—such as rash, itching, or difficulty breathing—and medical attention should be sought promptly.

Apremilast is not recommended for use during pregnancy due to the potential risks of fetal harm observed in animal studies. Although there are no human studies confirming these effects, women of childbearing potential should use effective contraception during treatment.

Breastfeeding is not advised while taking apremilast. The safety of this medication in nursing infants is unknown, and alternative treatments should be considered for breastfeeding mothers.

Live vaccines should be avoided while on apremilast. This medication can impact the immune system, potentially reducing the effectiveness of vaccines and increasing the risk of infections. It is recommended that all immunizations be up to date before starting treatment.

Patients should consult their healthcare provider to determine if apremilast is an appropriate treatment option based on their medical history and individual health needs.

[signup]

Key Takeaways

• Apremilast is an oral treatment option for psoriasis, psoriatic arthritis, and oral ulcers linked to Behcet disease. It offers a non-biologic option for select patients.

• It reduces inflammation by inhibiting phosphodiesterase 4 (PDE4), which leads to decreased production of inflammatory mediators such as TNF-α, IL-23, and IL-8.

• Common side effects include diarrhea, nausea, headache, and decreased appetite. Serious side effects, such as mood changes, suicidal thoughts, or severe allergic reactions, require immediate medical attention.

• Due to potential risks, Apremilast should not be used by individuals with allergies to its ingredients during pregnancy or while breastfeeding. Patients should also avoid live vaccines during treatment.

• Before using apremilast, patients should discuss their medical history and treatment goals with their healthcare provider to ensure it is appropriate for their specific health needs.