Aprezo (Apremilast) 30 mg Tablets

Aprezo is available in the form of film-coated tablets, each containing an exact therapeutic dosage of the active component:

• Active Compound: Apremilast — 30 mg in each tablet.
• Excipients: Lactose monohydrate, microcrystalline cellulose, croscarmellose sodium (ensuring proper and stable disintegration of the tablet), magnesium stearate, film coating (polyvinyl alcohol, titanium dioxide, macrogol, talc, iron oxide red).
• Appearance: Biconvex tablets of a specific shape, film-coated, packed in blister strips and a cardboard box.

Pharmacodynamics: Apremilast is a PDE4 inhibitor, specific for adenosine monophosphate (cAMP). Inhibition of PDE4 results in increased intracellular cAMP levels, which, in turn, modulates the expression of inflammatory factors. This leads to a significant reduction in inflammatory responses in skin and joint tissues.

Pharmacokinetics: After oral administration, the drug is well and rapidly absorbed, reaching peak plasma concentration in approximately 2.5 hours. Bioavailability is around 73%. Food intake does not have a clinically significant effect on the absorption of apremilast, allowing the medication to be taken regardless of meal schedules.

Aprezo 30 mg is prescribed by a qualified dermatologist or rheumatologist for systemic therapy in:

• 🔹 Moderate to Severe Psoriasis: In adult patients with plaque psoriasis when other methods of systemic therapy (including cyclosporine, methotrexate, or PUVA therapy) are contraindicated or ineffective.
• 🔹 Psoriatic Arthritis (PsA): As monotherapy or in combination with other disease-modifying antirheumatic drugs in adult patients with active disease who have had an inadequate response to prior therapy.

Strict compliance with the prescribed dosage regimen and gradual dose titration reduces the risk of adverse effects:

• Standard Dose: The maintenance therapeutic dosage is 60 mg per day, divided into two intakes — 1 tablet of 30 mg in the morning and evening.
• Treatment Initiation Scheme: During the first 5-6 days of therapy, a gradual increase in dose (titration) is recommended, starting with 10 mg in the morning, smoothly reaching the full dosage by the sixth day.
• Special Groups: In patients with severe renal impairment (creatinine clearance less than 30 mL/min), the daily dose should be reduced to 30 mg (once daily).
• Method of Use: Tablets must be swallowed whole, accompanied by a sufficient volume of water, regardless of meals. It is prohibited to chew or crush the tablets before intake.

Prescribing the drug is excluded or strictly limited in the presence of the following clinical factors:

• ⛔ Pregnancy and Lactation: The drug is strictly contraindicated in pregnant women and during breastfeeding due to risks to the fetus and child.
• ⛔ Age Restrictions: The safety and efficacy of apremilast in children and adolescents under 18 years of age have not yet been established.
• ⛔ Severe Infections: The presence of active acute or chronic infectious processes in the decompensation stage requires postponement of therapy.
• ⛔ Rare Pathologies: Hereditary galactose intolerance, lactase deficiency, or glucose-galactose malabsorption (due to the presence of lactose in the formulation).
• ⛔ Hypersensitivity: Presence of allergic reactions to apremilast or any other excipient of the medication.

Apremilast is metabolized in the liver with the participation of cytochrome isoenzymes, which requires consideration of drug interactions:

• ❌ CYP3A4 Enzyme Inducers: Concurrent use with strong inducers (rifampicin, phenobarbital, carbamazepine, phenytoin, or St. John's wort extract) significantly reduces plasma concentrations of apremilast, decreasing its therapeutic effect.
• ❌ Other Drugs: No clinically significant interactions have been observed with ketoconazole, methotrexate, or oral contraceptives, extending the possibilities of combination therapy.
• ⚠️ Special Attention: When prescribing to patients receiving concurrent sedative therapy, general somatic indicators should be taken into account.

Compliance with reproductive safety rules is a mandatory condition for therapy with Aprezo:

• Measures for Women: Women of childbearing potential must use a reliable method of contraception throughout the entire course of treatment to prevent accidental pregnancy.
• Planning: In case of planning a pregnancy, the use of apremilast must be stopped in advance, after prior consultation with the treating physician.
• Lactation Period: Data on the penetration of apremilast into human milk are limited, therefore, if treatment is necessary, breastfeeding should be discontinued immediately.

Due to its mechanism of action, the drug can cause adverse reactions, the severity of which usually decreases over time:

• 🟢 Very Common: Short-term diarrhea, nausea, minor headaches, and upper respiratory tract infections (during the first weeks of therapy).
• 🟡 Gastrointestinal: Decreased appetite, vomiting, dyspepsia, upper abdominal pain, frequent bowel movements.
• 🟡 Psychiatric Status: Insomnia, increased fatigue; rarely — depressive states or mood lability.
• 🟠 Body Weight: Some patients may experience a gradual decrease in body weight (averaging 5-10% from baseline), which requires periodic weighing.
• ⚠️ Urgent Doctor Consultation: It is required to contact a doctor immediately in case of a sharp worsening of mood, appearance of signs of depression, or suicidal thoughts.

Cases of acute specific overdose with apremilast in clinical practice are poorly described, but exceeding the dose increases toxicity:

• Possible Symptoms: Pronounced increase in gastrointestinal side effects, profuse diarrhea, severe nausea, dizziness, headache.
• First Aid: Immediate discontinuation of the drug, gastric lavage (if taken recently), and use of enterosorbents.
• Treatment: No specific antidote exists. Symptomatic therapy aimed at maintaining water-electrolyte balance during diarrhea is carried out. Hemodialysis is ineffective.

Proper storage of the medication guarantees the preservation of its full therapeutic activity:

• 🌡️ Temperature Regimen: Store in a dry place at a stable temperature not exceeding 30°C. Avoid excessive overheating and exposure to moisture.
• 📦 Packaging: Keep the tablets in their original blister strips and cardboard box to protect them from direct sunlight and mechanical damage.
• 👶 Safety: Store in a secure, hidden place that is absolutely inaccessible to children and pets.
• ⏳ Package Contents: The original box contains blisters with **60 tablets** (6 blisters of 10 tablets), which is fully designed for a standard 30-day course of maintenance therapy.