Apraize
Apraize Uses, Dosage, Side Effects, Food Interaction and all others data.
Apraize is an inhibitor of phosphodiesterase 4 (PDE4) enzyme specific for cyclic adenosine monophosphate (cAMP). PDE4 inhibition results in increased intracellular cAMP levels. The specific mechanism by which Apraize exerts its therapeutic action in psoriatic arthritis patients and psoriasis patients is not well defined.
Apraize reduces but does not completely inhibit various inflammatory cytokines such as IL-1α, IL-6, IL-8, IL-10 MCP-1, MIP-1β, MMP-3, and TNF-α, relieving the symptoms of psoriasis and Behcet's disease, which are caused by an increase in these inflammatory mediators. This drug has also been proven to be effective in relieving the pain associated with oral ulcers in Behcet's disease.
A note on depression and weight loss
Apraize may cause unwanted weight loss and worsen depression, leading to suicidal thoughts or actions. It is advisable to monitor for symptoms of depression and seek medical attention if they occur, especially in patients with pre-existing depression. The need for apremilast should be carefully assessed along with the risk of worsening depression and suicide. If weight loss occurs, the degree of weight loss should be evaluated, and consideration should be made for the possible discontinuation of apremilast.
Trade Name | Apraize |
Availability | Prescription only |
Generic | Apremilast |
Apremilast Other Names | Aprémilast, Apremilast, Apremilastum |
Related Drugs | Otezla, Humira, Cosentyx, prednisone, Enbrel, Remicade, Stelara |
Type | Tablet |
Formula | C22H24N2O7S |
Weight | Average: 460.5 Monoisotopic: 460.130422295 |
Protein binding | The plasma protein binding of apremilast is about 68%. |
Groups | Approved, Investigational |
Therapeutic Class | Disease-modifying antirheumatic drugs (DMARDs) |
Manufacturer | Ipca Laboratories |
Available Country | India |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Apraize is used for the treatment of adult patients with active psoriatic arthritis and moderate to severe plaque psoriasis who are candidates for phototherapy or systemic therapy.
Apraize is also used to associated treatment for these conditions: Psoriatic arthritis aggravated, Severe Plaque psoriasis, Moderate Plaque psoriasis, Ulceration of the mouth
How Apraize works
The full mechanism of action of this drug is not fully established, however, it is known that apremilast is an inhibitor of phosphodiesterase 4 (PDE4), which mediates the activity of cyclic adenosine monophosphate (cAMP), a second messenger. The inhibition of PDE4 by apremilast leads to increased intracellular cAMP levels. An increase in cAMP results in the suppression of inflammation by decreasing the expression of TNF-α, IL-17, IL-23, and other inflammatory mediators. The above inflammatory mediators have been implicated in various psoriatic conditions as well as Behcet's disease, leading to their undesirable inflammatory symptoms such as mouth ulcers, skin lesions, and arthritis. Apraize administration leads to a cascade which eventually decreases the levels of the above mediators, relieving inflammatory symptoms.
Dosage
Apraize dosage
The recommended initial dosage titration of Apraize from Day 1 to Day 5 is shown below. Following the 5-day titration, the recommended maintenance dosage is 30 mg twice daily taken orally starting on Day 6. This titration is intended to reduce the gastrointestinal symptoms associated with initial therapy. Apraize can be administered without regard to meals.
Day 1: 10 mg in morning
Day 2: 10 mg in morning and 10 mg in evening
Day 3: 10 mg in morning and 20 mg in evening
Day 4: 20 mg in morning and 20 mg in evening
Day 5: 20 mg in morning and 30 mg in evening
Day 6 and thereafter: 30 mg twice daily
Dosage adjustment in patients with severe renal impairment
Apraize dosage should be reduced to 30 mg once daily in patients with severe renal impairment. For initial dosage titration, it is recommended that Apraize be titrated using only the morning schedule and the evening doses be skipped.
Side Effects
The most frequently occurring side effects of Apraize are nausea, diarrhea, and headache.
Other less frequent side effects are upper respiratory tract infection, vomiting, nasopharyngitis, abdominal pain, hypersensitivity, gastroesophageal reflux disease, dyspepsia, fatigue, decrease appetite, cough, rash, insomnia.
Toxicity
The oral LD50 in mice was greater than 2000 mg/kg in mice. In rats, oral LD50 was 2000 mg/kg males and 300 mg/kg in females.
Overdose information
In healthy subjects receiving a maximum dose of 100 mg (given as 50 mg twice daily) for about 5 days, no significant toxicity was observed. In cases of an overdose, supportive and symptomatic treatment should be administered. Contact the local poison control center for the most recent overdose management for apremilast.
Precaution
Treatment with Apraize is associated with an increase in adverse reactions of depression. Patients, their caregivers and families should be advised of the need to be alert for the emergence or worsening of depression, suicidal thoughts or other mood changes and if such changes occur to contact their healthcare provider. Prescribers should carefully evaluate the risks and benefits of continuing treatment with Apraize if such events occur.
During the controlled period of the studies in psoriatic arthritis, weight decrease between 5%-10% of body weight was reported in 10% of subjects treated with Apraize 30 mg twice daily compared to 3.3% treated with placebo.
Interaction
Co-administration of strong cytochrome P450 enzyme inducer Rifampin resulted in a reduction of systemic exposure of Apraize.Therefore.the use of cytochrome P450 enzyme inducers (e.g. Rifampin, Phenobarbital,Carbamazepine, Phenytoin) with Apraize is not recommended.
Food Interaction
- Avoid St. John's Wort. Apraize is a CYP3A substrate; therefore, co-administration with St. John's wort, a CYP3A inducer, may reduce the serum level of apremilast.
- Take with or without food.
Apraize Drug Interaction
Unknown: charcoal, fluticasone / salmeterol, contained in alcoholic beverages , aspirin, sulfamethoxazole / trimethoprim, calcium / vitamin d, ubiquinone, duloxetine, cholecalciferol, omega-3 polyunsaturated fatty acids, sodium iodide, pregabalin, metoprolol, naproxen, acetaminophen, sars-cov-2 mrna , alirocumab, multivitamin with minerals, ocular lubricant ophthalmic, cholecalciferol
Apraize Disease Interaction
Volume of Distribution
The average apparent volume of distribution (Vd) is about 87 L, suggesting that apremilast is distributed in the extravascular compartment.
Elimination Route
An oral dose of apremilast is well-absorbed and the absolute bioavailability is approximately 73%. Tmax is approximately 2.5 hours and Cmax has been reported to be approximately 584 ng/mL in one pharmacokinetic study. Food intake does not appear to affect apremilast absorption.
Half Life
The average elimination half-life of this drug ranges from 6-9 hours.
Clearance
In healthy patients, the plasma clearance of apremilast is about 10 L/hour.
Elimination Route
Only 3% and 7% of an apremilast dose are detected in the urine and feces as unchanged drug, respectively, indicating extensive metabolism and high absorption.
Pregnancy & Breastfeeding use
Pregnancy: Pregnancy Category C.
Nursing mothers: It is not known whether Apraize or its metabolites are present in human milk; however Apraize was detected in milk of lactating mice. Caution should be exercised when Apraize is administered to a nursing woman.
Usage in Pediatric Patients
The safety and effectiveness of Apraize in pediatric patients less than18 years of age have not been established.
Contraindication
Apraize is contraindicated in patients with a known hypersensitivity to Apraize or to any of the excipients in the formulation.
Special Warning
Use in Paediatric patient: The safety and effectiveness of Apraize in paediatric patients less than 18 years of age have not been established.
Interaction with other Medicine
Co-administration of strong cytochrome P450 enzyme inducer, rifampin, resulted in a reduction of systemic exposure of Apraize. Therefore, the use of cytochrome P450 enzyme inducers (e.g., rifampin, phenobarbital, carbamazepine, phenytoin) with Apraize is not recommended.
Storage Condition
Store at cool & dry place, protected from light & moisture. Keep the medicine out of the reach of children.
Innovators Monograph
You find simplified version here Apraize
Apraize contains Apremilast see full prescribing information from innovator Apraize Monograph, Apraize MSDS, Apraize FDA label