Otezla (Apremilast) for Psoriasis and Psoriatic Arthritis

Otezla (apremilast) is an oral drug approved by the U.S. Food and Drug Administration (FDA) for the treatment of psoriasis and psoriatic arthritis. Used in adults, Otezla is taken twice daily with or without food. Otezla works by selectively inhibiting inflammatory compounds that contribute to the recurrence of psoriatic disease symptoms.

Although effectively, Otezla can sometimes cause depression and significant weight loss, both of which may warrant the discontinuation of treatment. Research is ongoing as to whether Otezla can treat other inflammatory diseases.

How It Works

Otezla is a selective inhibitor of an enzyme known as phosphodiesterase-4 (PDE4). PDE4 is used by the body to make tumor necrosis factor (TNF), the substance of which incites inflammation in tissues. By blocking the PDE4 enzyme, TNF levels are decreased and, with them, the inflammation that triggers symptoms.

Otezla is quickly absorbed in the gut and reaches peak concentration in the blood within 2 to 3 hours. Otezla has a relatively short drug half-life (6 to 8 hours), meaning that it needs to be taken twice daily without fail to ensure that drug concentrations remain steady.

The drug is metabolized in the liver and excreted from the body in urine and, to a lesser degree, in feces.

Who Can Take It

Otezla is approved for use in adults with moderate to severe psoriasis in whom topical medications have not provided relief. It is also used in adults with active psoriatic arthritis (a form of arthritis caused by inflammatory effects of psoriasis). Otezla is not approved for children and remains untested in children under 8.

Dosage

Otezla comes in a diamond-shaped, film-coated tablet in three strengths: 10 milligrams (mg), 20 mg, and 30 mg.

Otezla requires a five-day "loading dose" in which you slowly increase the dose each day to achieve the optimal drug concentration. Doing so reduces the risk of gastrointestinal side effects. Thereafter, you would take a "maintenance dose" to sustain the concentration.

The dose and dosing schedule is the same for both psoriasis and psoriatic arthritis:

  • 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 beyond: 30 mg in the morning and 30 mg in the evening

You can take Otezla with or without food. Do not crush, split, or chew the pill.

If you miss a dose, take it as soon as you remember. However, if it is close to the time of your next dose, just skip the dose and continue as normal. Never double up the dose.

Special Consideration

If you have severe kidney impairment (in which your kidneys are less able to clear the drug from your body), the dosage may need to be reduced to prevent drug toxicity. In this instance, you would only take the morning loading dose and, thereafter, only take 30 mg daily as your maintenance dose.

People with mild to moderate kidney impairment do not require a dose adjustment. You only need to do so if your creatinine clearance (CrCl) is less than 30 milliliters per minute (mL/min)

Side Effects

In clinical trials, diarrhea, headache, and nausea were the most commonly reported side effects associated with Otezla. Other include stomach ache, sore throat, cough, fever, and nasal congestion. Most of the adverse events occurred within the first two weeks of treatment and resolved over time with continued use of the drug.

Other uncommon side effects like depression and weight loss are far more concerning. In some cases, the symptoms may be serious enough to require a treatment change. According to premarket research issued by the FDA:

  • Depression and suicidal thoughts were reported in 0.8 percent of users. Of these, 0.3 percent stopped treatment as a result of the side effect.
  • Weight loss of 10 to 15 percent was reported in 10 percent of users. This is three times the incidence seen in people provided a placebo.

Due to the risk of weight loss, your body weight should be monitored throughout treatment and treatment stopped should the weight loss become extreme.

Contraindications

The only absolute contraindication to Otezla is a known hypersensitivity to apremilast or any of the drug's inactive ingredients. With that being said, drug hypersensitivity was not reported in any of the premarket studies but was identified, albeit rarely, in postmarket research.

Interactions

Otezla relies on a liver enzyme, known as cytochrome P450 (CYP450), for metabolism. Many other drugs need the same enzyme to be metabolized and dispersed. If Otezla is taken with some of these drugs, they may "compete" for the same enzyme. If this were to happen, the concentration of one or both drugs may be affected.

In some cases, the interaction can slow metabolization, leading to the accumulation of the drug and toxic side effects. In others, it can speed metabolization, reducing the drug concentration as well as the effectiveness of treatment.

Among some of the drugs that can interact with Otezla are:

Tell your doctor about any and all drugs you are taking, whether pharmaceutical or over-the-counter, to avoid interactions and unexpected side effects.

Other Considerations

While Otezla is not contraindicated for use in pregnancy, it is classified as a Pregnancy Category C drug. This means that animal studies have shown that Otezla may cause fetal harm. but there are no well-controlled studies in humans.

Most of the harm occurred at relative doses two to four times greater than that used in humans. Miscarriage was the most common pregnancy complication. It is unknown whether Otezla can be transmitted through breastmilk and what harm, if any, that may cause.

Because of the potential harm, Otezla should only be used during pregnancy if the benefits outweigh the risks. Speak with your rheumatologist to obtain all the facts you need to make an informed choice.

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