Apemilast Tablet
Apremilast
10mg
Healthcare Pharmaceuticals Ltd.
| Pack size | 30's pack |
|---|---|
| Dispensing mode | |
| Source | |
| Agent | |
| Retail Price | 25.00 AED |
Available as:
Indications
Apemilast Tablet is used for:
Plaque Psoriasis, Psoriatic Arthritis, or Behçet’s Disease
Adult Dose
Plaque Psoriasis, Psoriatic Arthritis, or Behçet’s Disease
To reduce risk of gastrointestinal symptoms, titrate to the recommended dose of 30 mg twice daily according to the following schedule:
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 there after: 30 mg twice daily
Child Dose
Child 6 Years of Age and Older and Weighing at Least 20 kg with Moderate to Severe Plaque Psoriasis
50 kg or more
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 there after: 30 mg twice daily
20 kg to less than 50 kg
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 20 mg in evening
Day 6 and there after: 20 mg twice daily
For patients weighing 50 kg or more: The recommended maintenance dosage is 30 mg twice daily
For patients weighing 20 kg to less than 50 kg: The recommended maintenance dosage is 20 mg twice daily
Renal Dose
Mild-to-moderate renal impairment: No dosage adjustment required
Adult Patients: Severe renal impairment (CrCl <30 mL/min): For initial dosage titration, titrate using only the morning schedule and skip afternoon doses.
The recommended maintenance dosage is 30 mg once daily
Day 1: 10 mg in morning
Day 2: 10 mg in morning
Day 3: 10 mg in morning
Day 4: 20 mg in morning
Day 5: 20 mg in morning
Day 6 and there after: 30 mg once daily
Child Patients: Severe renal impairment (CrCl <30 mL/min):
Child 6 Years of Age and Older and Weighing at Least 20 kg with Moderate to Severe Plaque Psoriasis: For initial dosage titration, titrate using only the morning schedule for appropriate body weight category in Table 2 and skip afternoon doses.
50 kg or more
Day 1: 10 mg in morning
Day 2: 10 mg in morning
Day 3: 10 mg in morning
Day 4: 20 mg in morning
Day 5: 20 mg in morning
Day 6 and there after: 30 mg once daily
20 kg to less than 50 kg
Day 1: 10 mg in morning
Day 2: 10 mg in morning
Day 3: 10 mg in morning
Day 4: 20 mg in morning
Day 5: 20 mg in morning
Day 6 and there after: 20 mg once daily
For patients weighing 50 kg or more: The recommended maintenance dosage is 30 mg once daily
For patients weighing 20 kg to less than 50 kg: The recommended maintenance dosage is 20 mg once daily
Administration
To reduce risk of GI symptoms associated with initial therapy, titrate to recommended dose (30 mg PO BID) according to the dosage schedules listed above
Can be administered without regard to meals
Swallow tablet whole; do not crush, split, or chew
Contra Indications
Known hypersensitivity to apremilast.
Precautions
Hypersensitivity: Cases of angioedema and anaphylaxis have been reported during post-marketing surveillance. Avoid the use of Apremilast in patients
with known hypersensitivity to apremilast or to any of the excipients in the formulation. If signs or symptoms of serious hypersensitivity reactions develop during treatment, discontinue Apremilast and institute appropriate therapy.
Diarrhea, Nausea, and Vomiting: Consider Apremilast dose reduction or suspension if patients develop severe diarrhea, nausea, or vomiting
Depression: Advise patients, their caregivers, and families 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.
Carefully weigh risks and benefits of treatment with Apremilastin patients with a history of depression and/or suicidal thoughts or behavior
Weight Decrease: Monitor weight regularly. If unexplained or clinically significant weight loss occurs, evaluate weight loss and consider discontinuation of Apremilast
Drug Interactions: Use with strong cytochrome P450 enzyme inducers (e.g., rifampin, phenobarbital, carbamazepine, phenytoin) is not recommended because loss of efficacy may occur
Monitoring Parameters
Monitor body weight regularly in patients underweight at the start of treatment.
Monitor for psychiatric symptoms (including depression, suicidal ideation, and behavior)—discontinue treatment if ne
Pregnancy-Lactation
Pregnancy
Available pharmacovigilance data use in pregnant women have not established a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes, but data are extremely limited
Based on findings from animal reproduction studies, may increase the risk for fetal loss
Animal data
In a pre- and postnatal study in mice, apremilast was administered to pregnant female mice at doses of 10, 80, or 300 mg/kg/day from Day 6 of gestation through Day 20 of lactation, with weaning on Day 21
Dystocia, reduced viability, and reduced birth weights occurred at doses corresponding to > 4 times the MRHD (on an AUC basis at doses ?80 mg/kg/day)
No adverse effects occurred at a dose 1.3- times the MRHD (10 mg/kg/day) No evidence for functional impairment of physical development, behavior, learning ability, immune competence, or fertility in the offspring at doses up to 7.5-times the MRHD (on an AUC basis at a dose of 300 mg/kg/day)
Apremilast distributed across the placenta into the fetal compartment in mice and monkeys
Advise pregnant women of the potential risk of fetal loss
Consider pregnancy planning and prevention for females of reproductive potential
Lactation
There are no data on the presence of apremilast in human milk, the effects on the breastfed infant, or the effects on milk production
Detected in the milk of lactating mice
Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need and any potential adverse effects on the breastfed infant or from the underlying maternal condition
Interactions
Coadministration with strong CYP inducers (eg, rifampin, carbamazepine, phenobarbital, phenytoin) may occur and result in a loss of efficacy of apremilast; therefore, coadministration is not recommended.
Contraindicated (0)
Serious - Use Alternative (28)
apalutamide
bosentan
carbamazepine
dabrafenib
dexamethasone
efavirenz
enzalutamide
eslicarbazepine acetate
etravirine
fexinidazole
fosphenytoin
idelalisib
ivosidenib
lonafarnib
lopinavir
mitotane
nafcillin
nevirapine
oxcarbazepine
pentobarbital
phenobarbital
phenytoin
primidone
rifabutin
rifampin
rifapentine
secobarbital
voxelotor
Adverse Effects
Side effects of Apremilast :
>10% (Psoriasis and Psoriatic Arthritis)
Diarrhea (7.7-17%)
Nausea (7.4-17%)
>10% (Behςet Disease)
Diarrhea (41.3%)
Nausea (19.2%)
Headache (14.4%)
Upper respiratory tract infection (11.5%)
1-10% (Behςet Disease)
Upper abdominal pain (8.7%)
Vomiting (8.7%)
Back pain (7.7%)
Viral upper respiratory tract infection (6.7%)
Arthralgia (5.8%)
1-10% (Psoriasis and Psoriatic Arthritis)
Upper respiratory tract infection (0.6-9%)
Tension headache (8%)
Headache (4.8-6%)
Vomiting (0.8-4%)
Fatigue (3%)
Dyspepsia (3%)
Decreased appetite (3%)
Insomnia (2%)
Back pain (2%)
Migraine (2%)
Frequent bowel movements (2%)
Depression (1%)
Bronchitis (1%)
Tooth abscess (1%)
Folliculitis (1%)
Frequency Not Defined (Psoriasis and Psoriatic Arthritis)
Immune system disorders: Hypersensitivity
Investigations: Weight decrease
Gastrointestinal disorders: Frequent bowel movement, gastroesophageal reflux disease, dyspepsia
Metabolism and nutrition disorders: Decreased appetite
Nervous system disorders: Migraine
Respiratory, thoracic, and mediastinal disorders: Cough
Skin and SC tissue disorders: Rash
Mechanism of Action
Apremilast is an oral small-molecule inhibitor of phosphodiesterase 4 (PDE4) specific for cyclic adenosine monophosphate (cAMP). PDE4 inhibition results in increased intracellular cAMP levels. The specific mechanism(s) by which apremilast exerts its therapeutic action in psoriatic arthritis patients and psoriasis patients is not well defined.
Note
Apemilast 10mg Tablet manufactured by Healthcare Pharmaceuticals Ltd.. Its generic name is Apremilast. Apemilast is availble in Bangladesh.
Farmaco BD drug index information on Apemilast Tablet is not intended for diagnosis, medical advice or treatment; neither intended to be a substitute for the exercise of professional judgment.