Country: Malaysia
Language: English
Source: NPRA (National Pharmaceutical Regulatory Agency, Bahagian Regulatori Farmasi Negara)
APREMILAST
Amgen Biopharmaceuticals Malaysia Sdn Bhd
APREMILAST
Starter pack: 4 tablets of 10 mg apremilast, 4 tablets of 20 mg apremilast, 19 tablets of 30 mg apremilast Tablets
Celgene International Sarl
_CONSUMER MEDICATION INFORMATION LEAFLET (RIMUP) _ 1 OTEZLA ® TABLETS Apremilast (10mg, 20mg, 30mg) WHAT IS IN THIS LEAFLET 1. What Otezla ® is used for 2. How Otezla ® works 3. Before you use Otezla ® 4. How to use Otezla ® 5. While you are using it 6. Side effects 7. Storage and disposal of Otezla ® 8. Product description 9. Manufacturer and product registration holder 10. Date of revision 11. Serial number WHAT OTEZLA ® IS USED FOR Otezla is used to treat adults with the following conditions: • Moderate to severe plaque psoriasis (an inflammatory disease of the skin, which can cause red, scaly, thick, itchy, painful patches on your skin, and can also affect your scalp and nails) • Psoriatic arthritis (an inflammatory disease of the joints, often accompanied by psoriasis) HOW OTEZLA ® WORKS Otezla works by reducing the activity of a natural substance in the body’s cells called ‘phosphodiesterase 4’. This helps regulate the immune response associated with psoriasis and psoriatic arthritis. By regulating the immune response, Otezla can help to control the signs and symptoms of these conditions. In psoriasis, treatment with Otezla results in a reduction in psoriatic skin plaques and other signs and symptoms of the disease. In psoriatic arthritis, treatment with Otezla results in an improvement in swollen and painful joints, and can improve your general physical function. Otezla has also been shown to improve the quality of life in patients with psoriasis or psoriatic arthritis. This means that the impact of your condition on daily activities, relationships and other factors should be less than it was before. _Ask your doctor if you have any _ _questions about how Otezla works, _ _or why this medicine has been _ _prescribed for you. _ Your doctor may have prescribed it for another reason. This medicine is not addictive. BEFORE YOU USE OTEZLA ® _A)_ _ _ _WHEN YOU MUST NOT USE IT _ _Do not take Otezla if you have an _ _allergy to apremilast, the active _ _ingredient of Otezla, or any of the _ _othe Read the complete document
1 OTEZLA ® (APREMILAST) TABLETS I) NAME OF THE MEDICINE Generic name: apremilast Molecular formula: C 22 H 24 N 2 O 7 S Molecular weight: 460.5 CAS number: 608141-41-9 ATC code: L04AA32 Chemical name: N-[2-[(1S)-1-(3-ethoxy-4-methoxyphenyl)-2- (methylsulfonyl)ethyl]-2,3-dihydro-1,3-dioxo-1H-isoindol-4- yl]acetamide Chemical structure: II) DESCRIPTION Apremilast is a white to pale yellow non-hygroscopic powder with a melting point of approximately 156.1°C. It is practically insoluble in water, slightly soluble in ethanol, and soluble in acetone. Apremilast is the S-enantiomer with a specific rotation of +28.1° in acetonitrile at a concentration of 20 mg/mL. LIST OF EXCIPIENTS Otezla tablets contain microcrystalline cellulose, lactose, croscarmellose sodium, magnesium stearate, polyvinyl alcohol, titanium dioxide, macrogol, talc, iron oxide red, iron oxide yellow (20 and 30 mg only) and iron oxide black (30 mg only). III) PHARMACOLOGY Pharmacotherapeutic group: Selective immunosuppressants. PHARMACODYNAMIC PROPERTIES Mechanism of action Apremilast, an oral small-molecule inhibitor of phosphodiesterase 4 (PDE4), works intracellularly to modulate a network of pro-inflammatory and anti-inflammatory mediators. PDE4 is a cyclic adenosine monophosphate (cAMP)-specific PDE and the dominant PDE in inflammatory cells. PDE4 inhibition elevates intracellular cAMP levels, which in turn down-regulates the inflammatory response by modulating the expression of TNF-α, IL-23, IL-17 and other inflammatory cytokines. Cyclic AMP also modulates levels of anti-inflammatory cytokines such as IL-10. These pro- and anti-inflammatory mediators have been implicated in psoriatic arthritis (PsA) and psoriasis (PSOR). Clinical Pharmacodynamics In clinical studies in patients with psoriatic arthritis, apremilast significantly modulated, but did not fully inhibit, plasma protein levels of IL-1α, IL-6, IL-8, MCP-1, MIP-1β, MMP-3, and TNF-α. After 40 weeks of treatment with apremilast, there was a decrease in plasma protein levels of IL-17 a Read the complete document