Apilast Tablet 10 mg

Apilast Tablet 10 mg Uses, Dosage, Side Effects, Food Interaction and all others data.

Apilast Tablet 10 mg 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 Apilast Tablet 10 mg exerts its therapeutic action in psoriatic arthritis patients and psoriasis patients is not well defined.

Apilast Tablet 10 mg 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

Apilast Tablet 10 mg 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 Apilast Tablet 10 mg
Availability Prescription only
Generic Apremilast
Apremilast Other Names Aprémilast, Apremilast, Apremilastum
Related Drugs Otezla, Humira, Cosentyx, prednisone, Enbrel, Remicade, Stelara
Weight 10 mg
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 Labaid Pharma Ltd.
Available Country Bangladesh
Last Updated: October 19, 2023 at 6:27 am
Apilast Tablet 10 mg
Apilast Tablet 10 mg

Uses

Apilast Tablet 10 mg 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.

Apilast Tablet 10 mg is also used to associated treatment for these conditions: Psoriatic arthritis aggravated, Severe Plaque psoriasis, Moderate Plaque psoriasis, Ulceration of the mouth

How Apilast Tablet 10 mg 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. Apilast Tablet 10 mg administration leads to a cascade which eventually decreases the levels of the above mediators, relieving inflammatory symptoms.

Dosage

Apilast Tablet 10 mg dosage

The recommended initial dosage titration of Apilast Tablet 10 mg 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. Apilast Tablet 10 mg 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

Apilast Tablet 10 mg dosage should be reduced to 30 mg once daily in patients with severe renal impairment. For initial dosage titration, it is recommended that Apilast Tablet 10 mg be titrated using only the morning schedule and the evening doses be skipped.

Side Effects

The most frequently occurring side effects of Apilast Tablet 10 mg 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 Apilast Tablet 10 mg 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 Apilast Tablet 10 mg 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 Apilast Tablet 10 mg 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 Apilast Tablet 10 mg.Therefore.the use of cytochrome P450 enzyme inducers (e.g. Rifampin, Phenobarbital,Carbamazepine, Phenytoin) with Apilast Tablet 10 mg is not recommended.

Food Interaction

  • Avoid St. John's Wort. Apilast Tablet 10 mg 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.

Apilast Tablet 10 mg Disease Interaction

Moderate: depression, renal dysfunction, weight loss

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 Apilast Tablet 10 mg or its metabolites are present in human milk; however Apilast Tablet 10 mg was detected in milk of lactating mice. Caution should be exercised when Apilast Tablet 10 mg is administered to a nursing woman.

Usage in Pediatric Patients

The safety and effectiveness of Apilast Tablet 10 mg in pediatric patients less than18 years of age have not been established.

Contraindication

Apilast Tablet 10 mg is contraindicated in patients with a known hypersensitivity to Apilast Tablet 10 mg or to any of the excipients in the formulation.

Special Warning

Use in Paediatric patient: The safety and effectiveness of Apilast Tablet 10 mg 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 Apilast Tablet 10 mg. Therefore, the use of cytochrome P450 enzyme inducers (e.g., rifampin, phenobarbital, carbamazepine, phenytoin) with Apilast Tablet 10 mg 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 Apilast Tablet 10 mg

Apilast Tablet 10 mg contains Apremilast see full prescribing information from innovator Apilast Tablet 10 mg Monograph, Apilast Tablet 10 mg MSDS, Apilast Tablet 10 mg FDA label

*** Taking medicines without doctor's advice can cause long-term problems.
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