Apremilast: Uses, Dosage, Side Effects, and More

Introduction to Apremilast

Apremilast is an oral medication used to treat inflammatory conditions, including moderate to severe plaque psoriasis and psoriatic arthritis. It belongs to a class of drugs known as phosphodiesterase-4 (PDE4) inhibitors, which work by reducing inflammation within the body. Unlike traditional treatments for psoriasis and psoriatic arthritis that target the immune system more broadly, apremilast specifically targets enzymes that play a role in inflammation, making it a more selective treatment option. This guide provides a comprehensive overview of apremilast, covering its uses, recommended dosage, potential side effects, interactions with other medications, and answers to frequently asked questions.

What is Apremilast?

Apremilast is a phosphodiesterase-4 (PDE4) inhibitor that works by decreasing the production of certain inflammatory chemicals within the body. By reducing levels of these chemicals, such as TNF-alpha, interleukin-23, and interleukin-17, apremilast helps alleviate inflammation and control symptoms associated with autoimmune conditions like psoriasis and psoriatic arthritis. This targeted mechanism makes apremilast effective in reducing the severity of skin plaques, joint pain, and other inflammatory symptoms associated with these conditions.

Uses of Apremilast

1. Plaque Psoriasis: Apremilast is used to treat moderate to severe plaque psoriasis, a chronic skin condition characterized by red, scaly patches on the skin. It is prescribed for patients who are candidates for systemic or phototherapy treatments.

2. Psoriatic Arthritis: Apremilast is also indicated for the treatment of psoriatic arthritis, a type of arthritis that affects some individuals with psoriasis. It helps reduce joint pain, swelling, and stiffness associated with the condition.

3. Oral Ulcers in Behçet’s Disease: In certain cases, apremilast may be prescribed to manage oral ulcers in patients with Behçet’s disease, an inflammatory disorder that can cause painful sores in the mouth and other areas.

Dosage and Administration

Apremilast is available as an oral tablet, and the dosage typically involves a gradual increase over several days to help the body adjust and reduce the risk of side effects, especially gastrointestinal ones.

1. Starting Dosage (Titration Schedule): Apremilast is initially prescribed at a low dose, gradually increasing over five days to reach the maintenance dose. The titration schedule usually involves:

• 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

2. Maintenance Dose: After the initial titration, the recommended maintenance dose is 30 mg twice daily, taken orally.

3. Administration Instructions: Apremilast tablets should be taken with water and can be taken with or without food. Consistent timing of doses each day can help maintain stable blood levels of the medication.

Side Effects of Apremilast

While apremilast is generally well-tolerated, some patients may experience side effects. These range from mild to moderate, but in rare cases, serious side effects may occur.

Common Side Effects

1. Diarrhea and Nause Gastrointestinal side effects, such as diarrhea and nausea, are common, particularly during the initial dose titration phase.

2. Headache: Some patients experience mild headaches, which may improve as the body adjusts to the medication.

3. Upper Respiratory Tract Infections: Respiratory infections, such as colds or sinus infections, are a possible side effect.

4. Weight Loss: Apremilast may lead to weight loss in some individuals, particularly those who experience gastrointestinal side effects.

5. Fatigue: Fatigue and tiredness are relatively common, particularly at the beginning of treatment.

Rare but Serious Side Effects

1. Mood Changes and Depression: Apremilast has been associated with mood changes, including depression and, in rare cases, suicidal thoughts. Patients with a history of depression should be closely monitored.

2. Severe Diarrhe Although mild gastrointestinal symptoms are common, some patients may experience severe diarrhea, which may require medical intervention.

3. Hypersensitivity Reactions: Rarely, hypersensitivity reactions such as rash, itching, or swelling may occur. If severe, immediate medical attention is necessary.

4. Severe Weight Loss: Significant weight loss may occur, especially in individuals prone to gastrointestinal side effects, and may necessitate discontinuation of the medication.

Interaction with Other Medications

Apremilast can interact with certain medications, which may alter its effectiveness or increase the risk of side effects. Patients should inform their healthcare provider about all medications they are taking, including over-the-counter drugs, supplements, and herbal products.

1. Strong CYP450 Inducers (e.g., Rifampin, Carbamazepine): These drugs can decrease blood levels of apremilast, reducing its effectiveness. Concurrent use is generally not recommended.

2. Immunosuppressive Agents (e.g., Methotrexate): While no specific interactions have been identified, combining apremilast with other immunosuppressive agents should be done with caution due to potential additive effects.

3. Antidepressants: Apremilast may cause mood changes, so patients taking antidepressants should be closely monitored to avoid compounded effects.

4. Nonsteroidal Anti-Inflammatory Drugs (NSAIDs): There are no known interactions between NSAIDs and apremilast, making them generally safe to use together for additional pain relief.

Benefits of Apremilast

Apremilast offers several therapeutic benefits, particularly for individuals with inflammatory conditions who may not respond well to other treatments.

1. Targeted Treatment for Inflammation: Apremilast specifically targets PDE4, helping reduce inflammation without broadly suppressing the immune system, which can be beneficial for long-term treatment.

2. Improvement in Skin and Joint Symptoms: By reducing inflammatory markers, apremilast helps relieve symptoms of plaque psoriasis and psoriatic arthritis, improving quality of life.

3. Convenient Oral Administration: Unlike some other treatments for psoriasis and psoriatic arthritis that require injections or infusions, apremilast is taken orally, making it more convenient.

4. Lower Risk of Serious Infections: Compared to biologic treatments, apremilast has a lower risk of serious infections, making it suitable for individuals who need a less immunosuppressive option.

5. Positive Impact on Quality of Life: By effectively managing symptoms, apremilast can significantly improve daily functioning and quality of life for individuals with chronic inflammatory conditions.

Frequently Asked Questions (FAQs)

1. What is apremilast used to treat?

Apremilast is used to treat moderate to severe plaque psoriasis and psoriatic arthritis. It is also prescribed for managing oral ulcers associated with Behçet’s disease.

2. How does apremilast work?

Apremilast works by inhibiting the enzyme phosphodiesterase-4 (PDE4), reducing the production of inflammatory chemicals in the body. This action helps decrease inflammation and alleviates symptoms of psoriasis and psoriatic arthritis.

3. How long does it take for apremilast to work?

Some patients may begin to notice symptom improvement within 2–4 weeks, but it may take up to 16 weeks to experience the full benefits of apremilast.

4. Can apremilast cause weight loss?

Yes, weight loss is a potential side effect of apremilast. In some cases, the weight loss may be significant, especially if gastrointestinal symptoms are present.

5. What should I do if I miss a dose of apremilast?

If you miss a dose, take it as soon as you remember. If it is close to the next scheduled dose, skip the missed dose and continue with your regular dosing schedule. Do not double the dose to make up for a missed one.

6. Can I take apremilast with other medications?

While apremilast can be taken with certain medications, it should not be combined with strong CYP450 inducers, as they can reduce its effectiveness. Always inform your healthcare provider about all other medications you are taking.

7. Is apremilast safe during pregnancy?

The safety of apremilast during pregnancy has not been established, and it is generally not recommended. Women of childbearing age should discuss contraceptive options with their healthcare provider before starting apremilast.

8. How should I take apremilast?

Apremilast is taken orally, usually at a starting dose that gradually increases over five days to reach the maintenance dose. It can be taken with or without food.

9. Can I stop taking apremilast if my symptoms improve?

It’s important to continue taking apremilast as prescribed, even if symptoms improve. Stopping the medication without consulting your healthcare provider can lead to a recurrence of symptoms.

10. Does apremilast require any special monitoring?

Patients may require monitoring for weight changes, mood changes, and gastrointestinal side effects, especially at the beginning of treatment. Regular check-ins with a healthcare provider are recommended to ensure optimal treatment.

Brand Names of Apremilast

Apremilast is available under the

following brand name:

• Otezla

Otezla is commonly prescribed in tablet form for treating moderate to severe plaque psoriasis and psoriatic arthritis. It is also approved for oral ulcers in Behçet’s disease.

Conclusion

Apremilast is an effective and convenient oral medication for managing chronic inflammatory conditions such as plaque psoriasis and psoriatic arthritis. With its targeted action on inflammatory enzymes, apremilast helps alleviate skin and joint symptoms while posing a lower risk of serious infections compared to other immunosuppressive therapies. However, like all medications, apremilast may cause side effects and interact with other drugs, so regular monitoring and communication with a healthcare provider are essential for safe and effective treatment.