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Alminoprofen/Anakinra 19 Alminoprofen/Anakinra 19 Aluminium Aspirin Acetilsalicilato de aluminio; Aluminum Acetylsalicylate; Alumi- H CCH H C num Aspirin; Aluminum Bis(acetylsalicylate); Aspirin Aluminium. O 3 3 3 Bis(2-acetoxybenzoato-O′)hydroxyaluminium. H3C N Алюминий Аспирина; Аспирин Алюминий N O N H3C C H AlO = 402.3. H 18 15 9 N H N N CAS — 23413-80-1. H3C O CH3 O O O OCH3 O O O O Profile Al Aminopropylone is an NSAID (p.96) that has been used in topi- Profile cal preparations, for the local treatment of pain and inflammatory Amtolmetin guacil is an NSAID (p.96) that is an ester prodrug of H3C O OH O CH3 conditions. The hydrochloride has been used similarly. tolmetin (p.130). It is used in painful and inflammatory disorders Preparations in oral doses of 600 to 1200 mg daily. O O Proprietary Preparations (details are given in Part 3) ◊ References. 1. Biasi G, Marcolongo R. Efficacia e tollerabilità dell’amtolmetina Multi-ingredient: Ital.: Vessiflex†. guacil nel trattamento dell’artrosi in fase di riacutizzazione. Min- Pharmacopoeias. In Jpn. erva Med 2001; 92: 315–24. 2. Jajic Z, et al. Gastrointestinal safety of amtolmetin guacyl in Profile comparison with celecoxib in patients with rheumatoid arthritis. Aluminium aspirin is a salicylic acid derivative (see Aspirin, Ammonium Salicylate Clin Exp Rheumatol 2005; 23: 809–18. p.20) that has been given orally in the management of fever, pain, Salicilato de amonio. Preparations and musculoskeletal and joint disorders. Аммоний Салицилат Proprietary Preparations (details are given in Part 3) Ital.: Artricol; Artromed; Eufans. Preparations C7H9NO3 = 155.2. Proprietary Preparations (details are given in Part 3) CAS — 528-94-9. Multi-ingredient: Indon.: Remasal; S.Afr.: Analgen-SA†. Amyl Salicylate HO Isoamyl Salicylate; Isopentyl Salicylate; Salicilato de isoamilo; Sali- + - cilato de isopentilo. 3-Methylbutyl 2-hydroxybenzoate. NH4 O Aminophenazone (rINN) Амилсалицилат Amidazofen; Amidopyrine; Amidopyrine-Pyramidon; Amino- C12H16O3 = 208.3. fenatsoni; Aminofenazon; Aminofenazona; Aminophénazone; O CAS — 87-20-7. Aminophenazonum; Aminopyrine; Dimethylaminoantipyrine; Dimethylaminophenazone. 4-Dimethylamino-1,5-dimethyl-2- Profile phenyl-4-pyrazolin-3-one. Ammonium salicylate is a salicylic acid derivative used topically Аминофеназон in rubefacient preparations similarly to methyl salicylate (p.85) for the relief of pain in musculoskeletal and joint disorders. O CH3 C13H17N3O = 231.3. CAS — 58-15-1. Preparations ATC — N02BB03. Proprietary Preparations (details are given in Part 3) OH O CH3 ATC Vet — QN02BB03. Multi-ingredient: Austral.: Radian-B†; Irl.: Radian-B†; UK: Radian-B. Pharmacopoeias. In Fr. Profile Ampiroxicam (BAN, rINN) Amyl salicylate is a salicylic acid derivative used topically in ru- befacient preparations similarly to methyl salicylate (p.85) for its Ampiroxicamum; CP-65703. 4-[1-(Ethoxycarbonyloxy)ethoxy]- 2 analgesic and anti-inflammatory actions. It has also been used in 2-methyl-N -pyridyl-2H-1,2-benzothiazine-3-carboxamide 1,1- perfumery. dioxide. N Preparations O CH3 Ампироксикам N Proprietary Preparations (details are given in Part 3) C H N O S = 447.5. 20 21 3 7 Multi-ingredient: Arg.: Atomo Desinflamante; Atomo Desinflamante C; H3C CAS — 99464-64-9. N CH Atomo Desinflamante Familiar; Rati Salil Crema; Fr.: Sedartryl†; Spain: Lin- 3 imento Klari†. CH3 O O Anakinra (BAN, USAN, rINN) Pharmacopoeias. In It. S CH3 N Anakinrum; rhIL-1ra; r-metHuIL-1ra. N2-L-methionylinterleukin 1 Profile H receptor antagonist (human isoform x reduced). Aminophenazone, a pyrazolone derivative, is an NSAID (p.96), N Анакинра but the risk of agranulocytosis is sufficiently great to render it CAS — 143090-92-0. unsuitable for systemic use. Onset of agranulocytosis may be H3C O O OON sudden and unpredictable. Aminophenazone has been used as ATC — L04AC03. salts or complexes, including topically as the salicylate. ATC Vet — QL04AC03. O CH3 Precautions. CARCINOGENICITY. Some1 consider that amino- phenazone should be regarded as a potential carcinogen be- M cause it reacted readily with nitrous acid to form dimethylni- Profile RPSGRKSSKM QAFRIWDVNQ KTFYLRNNQL VAGYLQGPNV NLEEKIDVVP trosamine. The reaction was catalysed by thiocyanate present Ampiroxicam is an NSAID (p.96) that is reported to be metabo- IEPHALFLGI HGGKMCLSCV KSGDETRLQL EAVNITDLSE NRKQDKRFAF in the saliva particularly in smokers. lised to piroxicam (p.117). It has been given orally for the relief of pain and inflammation particularly in musculoskeletal disor- IRSDSGPTTS FESAACPGWF LCTAMEADQP VSLTNMPDEG VMVTKFYFQE 1. Boyland E, Walker SA. Catalysis of the reaction of aminopyrine DE and nitrite by thiocyanate. Arzneimittelforschung 1974; 24: ders such as rheumatoid arthritis and osteoarthritis. 1181–4. Adverse effects. Photosensitivity reactions have occurred dur- ing ampiroxicam treatment.1-3 Adverse Effects and Precautions PORPHYRIA. Aminophenazone has been associated with acute Mild to moderate injection site reactions with symptoms of ery- attacks of porphyria and is considered unsafe in porphyric pa- 1. Kurumaji Y. Ampiroxicam-induced photosensitivity. Contact thema, bruising, swelling, and pain are common with anakinra tients. Dermatitis 1996; 34: 298–9. 2. Toyohara A, et al. Ampiroxicam-induced photosensitivity. Con- particularly in the first month of treatment. Other common reac- Preparations tact Dermatitis 1996; 35: 101–2. tions include headache, nausea, diarrhoea, and abdominal pain. Antibodies to anakinra may develop. Allergic reactions such as Proprietary Preparations (details are given in Part 3) 3. Chishiki M, et al. Photosensitivity due to ampiroxicam. Derma- tology 1997; 195: 409–10. rashes have been reported rarely; if a severe allergic reaction oc- Multi-ingredient: Braz.: Gineburno†; Cz.: Dinyl†; Eunalgit†; Hung.: An- Preparations curs, anakinra should be stopped and appropriate treatment giv- tineuralgica; Demalgon; Demalgonil; Dolor; Germicid-C; Germicid†; Kefal- en. gin; Meristin; Ital.: Virdex; Mex.: Flumil; Switz.: Thermocutan†; Venez.: Proprietary Preparations (details are given in Part 3) Flexidone†. Serious infections have been reported with anakinra, particularly Jpn: Flucam†. in patients with asthma. These infections are mainly bacterial, such as cellulitis, pneumonia, and bone and joint infections. More rarely, opportunistic infections involving fungal, mycobac- Aminopropylone Amtolmetin Guacil (rINN) terial, and viral pathogens have also been seen. Anakinra should Aminopropilona; Aminopropylon. N-(2,3-Dihydro-1,5-dimethyl- Amtolmetina guacilo; Amtolmétine Guacil; Amtolmetinum be stopped in those who develop a serious infection. In addition, therapy should not be started in patients with active infections, 3-oxo-2-phenyl-1H-pyrazol-4-yl)-2-(dimethylamino)propana- Guacilum; MED-15; ST-679. N-[(1-Methyl-5-p-toluoylpyrrol-2- mide. including chronic or localised infections; caution is recommend- yl)acetyl]glycine o-methoxyphenyl ester. ed in those with a history of recurrent infections or with underly- Аминопропилон Амтолметин Гуацил ing conditions that may predispose to infections. C16H22N4O2 = 302.4. C24H24N2O5 = 420.5. A small decrease in absolute neutrophil count (ANC) is com- CAS — 3690-04-8. CAS — 87344-06-7. monly seen with anakinra treatment; however, true neutropenia The symbol † denotes a preparation no longer actively marketed The symbol ⊗ denotes a substance whose use may be restricted in certain sports (see p.vii) 20 Analgesics Anti-inflammatory Drugs and Antipyretics 3 (ANC <1500 cells/mm ) is rare. Licensed product information 2. Cohen S, et al. Treatment of rheumatoid arthritis with anakinra, Aspirin (BAN) recommends that neutrophil counts should be taken before start- a recombinant human interleukin-1 receptor antagonist, in com- bination with methotrexate: results of a twenty-four-week, mul- _ ing anakinra and periodically throughout treatment. UK licensed ticenter, randomized, double-blind, placebo-controlled trial. Ar- Acetilsalicílico, ácido; Acetilsalicilo rugštis; Acetilszalicilsav; Ace- information recommends monthly monitoring during the first 6 thritis Rheum 2002; 46: 614–24. tylsal. Acid; Acetylsalicylic Acid; Acetylsalicylsyra; Acide acétylsal- months and then quarterly thereafter; US licensed information 3. Nuki G, et al. Long-term safety and maintenance of clinical im- icylique; Acidum acetylsalicylicum; Asetilsalisilik Asit; Asetyylisal- requires monthly monitoring for the first 3 months and then quar- provement following treatment with anakinra (recombinant hu- isyylihappo; Kwas acetylosalicylowy; Kyselina acetylsalicylová; Pol- terly monitoring for a period of up to 1 year. Anakinra should not man interleukin-1 receptor antagonist) in patients with rheuma- toid arthritis: extension phase of a randomized, double-blind, opiryna; Salicylic Acid Acetate. O-Acetylsalicylic acid; 2-Acetoxy- be started in patients with neutropenia. Small reductions in the placebo-controlled trial. Arthritis Rheum 2002; 46: 2838–46. benzoic acid. total white blood cell and platelets counts and a small increase in 4. Fleischmann RM, et al. Anakinra, a recombinant human inter- eosinophils have also been noted. Anakinra is also associated leukin-1 receptor antagonist (r-metHuIL-1ra), in patients with Аспирин with an increased incidence of lymphoma in patients with rheu- rheumatoid arthritis: a large, international, multicenter, placebo- C9H8O4 = 180.2. matoid arthritis. controlled trial. Arthritis Rheum 2003; 48: 927–34. 5. NICE. Anakinra for rheumatoid arthritis: Technology Appraisal CAS — 50-78-2. For caution
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