Apremilast

Ajanta Pharma Ltd ,

Ipca Laboratories Ltd

Apxenta 30mgTablet 10s ,

Apraize 30mg Tablet

Arthritis ,

Psoriatic

DRUG STATUS

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Approvals

US. FDA / uk mhra / ema / pdma

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Essential Medicine

WHO / India

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Use in Pregnancy

Not Advised / Caution

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Pharmaceutical Class

ama / pdma

Summary

  • Apremilast is primarily used for treating moderate to severe plaque psoriasis, active psoriatic arthritis, and oral ulcers associated with Behçet's disease. It helps reduce inflammation and symptoms related to these conditions, thereby improving quality of life and physical function.

  • Apremilast works by blocking an enzyme called phosphodiesterase 4 (PDE4) that is involved in the inflammatory process. By inhibiting PDE4, it increases the levels of a substance called cyclic AMP in cells, which helps reduce the production of pro-inflammatory substances, controlling inflammation and immune responses.

  • The usual daily dosage of Apremilast for adults is 30 mg taken orally twice a day with food. The starting dose is typically 10 mg taken once a day for the first week, then increased to 20 mg taken once a day for the second week. It's important to take Apremilast exactly as prescribed by your doctor.

  • Common side effects of Apremilast include diarrhea, nausea, headache, upper respiratory tract infections, and fatigue. Some people may also experience mood changes, depression, suicidal thoughts, weight loss, and gastrointestinal issues like vomiting or abdominal pain. Rarely, severe allergic reactions or heart issues can occur.

  • Apremilast should be used with caution in patients with a history of depression or suicidal thoughts as it can worsen these conditions. It's contraindicated in patients with hypersensitivity to the drug, severe renal impairment, or active infections. Regular monitoring of weight, mood, and gastrointestinal health is recommended during treatment.

Indications and Purpose

How does Apremilast work?

Apremilast works by inhibiting phosphodiesterase 4 (PDE4), an enzyme involved in the inflammatory process. By blocking PDE4, it increases cyclic AMP levels in cells, which helps reduce the production of pro-inflammatory cytokines. This action helps control inflammation and immune responses in conditions like psoriasis and psoriatic arthritis.

 

 

How does one know if Apremilast is working?

The benefit of Apremilast is typically evaluated through clinical assessments, including improvement in symptoms and disease activity. For conditions like psoriatic arthritis or psoriasis, the evaluation includes monitoring the reduction in joint pain, inflammation, and skin lesions, as well as patient-reported outcomes and physical assessments. Regular follow-up visits help determine whether the treatment is providing sufficient benefit.

 

 

Is Apremilast effective?

Clinical trials have shown that Apremilast effectively reduces symptoms in conditions like moderate-to-severe psoriasis and psoriatic arthritis. Studies indicate significant improvements in skin lesions, joint symptoms, and overall quality of life. Its efficacy was demonstrated through reduced Psoriasis Area Severity Index (PASI) scores and improvements in physical function in patients with psoriatic arthritis.

 

 

What is Apremilast used for?

Apremilast is primarily indicated for the treatment of moderate to severe plaque psoriasis, active psoriatic arthritis, and the management of Behçet’s disease, specifically for oral ulcers. It is used to reduce inflammation and symptoms associated with these conditions, improving quality of life and physical function.

 

 

Directions for Use

How do I take Apremilast?

Apremilast should always be taken with food, preferably with a meal or a snack. Eating smaller, more frequent meals can help to reduce the risk of side effects. There are no specific food restrictions for people taking Apremilast, but it's important to talk to your doctor if you have any dietary concerns.


How long does it take for Apremilast to start working?

It can take up to 12 weeks for Apremilast to reach its full effect, and some people may not see any improvements in their symptoms until they've been taking the medication for several weeks or months. However, other people may start to see some improvement in their symptoms within a few weeks of starting Apremilast.


How should I dispose of Apremilast?

If you can, bring unused medicines to a drug take-back program or collection site at a pharmacy or hospital. They will dispose of the medicines properly so they don't harm people or the environment. If you can't find a take-back program, you can throw most medicines in the trash at home. But first, take them out of their original containers, mix them with something undesirable like used coffee grounds, seal the mixture in a plastic bag and throw it away.

How should I store Apremilast?

Apremilast should be stored at room temperature, between 20°C to 25°C (68°F to 77°F), away from moisture and heat. It should be kept in its original packaging to protect it from light. Do not store it in the bathroom or near the kitchen sink, and keep it out of reach of children.

 

 

What are the consequences to stopping Apremilast?

Stopping Apremilast abruptly is generally safe, as it does not cause withdrawal symptoms. However, discontinuation may lead to a return of the condition it was treating, such as psoriasis or psoriatic arthritis. It's advisable to consult with a healthcare provider before stopping Apremilast to ensure the best management of your condition.

 

 

What is Apremilast’s dose and duration?

The usual daily dosage of Apremilast for adults is 30 mg, taken orally twice a day with food. The starting dose is usually 10 mg, taken once a day for the first week, then increased to 20 mg, taken once a day for the second week.

It's important to take Apremilast exactly as prescribed by your doctor and not to stop taking it without talking to your doctor first. If you miss a dose, take it as soon as you remember, unless it's almost time for your next dose.

What should I do if I miss a dose of Apremilast?

If you forget to take one or more doses: take your next dose at the normal time and in the normal amount. Do not take any more than your doctor prescribed.

Warnings and Precautions

Can Apremilast be taken safely while breastfeeding?

Apremilast is not recommended during breastfeeding, as it is not known if the drug passes into breast milk. Due to potential risks to the infant, it's advised that mothers either discontinue breastfeeding or avoid using apremilast. Women should discuss with their healthcare provider to determine the best course of action while breastfeeding.

 

 

Can Apremilast be taken safely while pregnant?

Apremilast is classified as a Category C drug during pregnancy, meaning animal studies have shown adverse effects, but there are no well-controlled human studies. The potential risks to the fetus are not fully known, so it should only be used if the benefits outweigh the risks. Pregnant women should consult their healthcare provider before using this medication.

 

 

Can Apremilast be taken safely while trying to conceive?

There is limited information on the effects of apremilast on fertility in men and women of reproductive age. Animal studies did not show any adverse effects on fertility, but human data is insufficient to draw definitive conclusions. It’s recommended to consult a healthcare provider for personalized guidance if planning for pregnancy or facing fertility concerns.

 

 

Can I take Apremilast with other prescription drugs?

Apremilast may interact with certain medications, especially those that affect the CYP450 enzyme system. Significant interactions include:

  1. Strong CYP450 inducers (e.g., rifampin) may decrease Apremilast effectiveness.
  2. CYP450 inhibitors (e.g., ketoconazole) may increase Apremilast levels and increase the risk of side effects.

 

Can I take Apremilast with vitamins or supplements?

There are no significant interactions between Apremilast and most vitamins or supplements. However, caution should be used when combining Apremilast with supplements that affect the immune system or mood, such as St. John's Wort, as they may alter the effectiveness of Apremilast. Always consult with a healthcare provider before combining supplements with Apremilast.

 

 

What are Apremilast possible harms and risks?

Common side effects of Apremilast include diarrhea, nausea, headache, upper respiratory tract infections, and fatigue. Significant adverse effects may include mood changes, depression, suicidal thoughts, weight loss, and gastrointestinal issues like vomiting or abdominal pain. Rarely, severe allergic reactions or heart issues can occur, and monitoring is recommended during treatment.

 

 

Who should avoid taking Apremilast?

Apremilast should be used with caution in patients with a history of depression or suicidal thoughts, as it can worsen these conditions. It is contraindicated in patients with hypersensitivity to the drug. Caution is advised in those with severe renal impairment or active infections. Regular monitoring of weight, mood, and gastrointestinal health is recommended during treatment.

 

 

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