Bumadizone

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Bumadizone
Nome IUPAC
Acido 2-[fenil-(fenillammino)carbamoil]esanoico
Caratteristiche generali
Formula bruta o molecolareC19H22N2O3
Massa molecolare (u)326.38958 g/mol
Numero CAS3583-64-0
Numero EINECS222-710-1
PubChem19161
DrugBankDBDB13286
SMILES
CCCCC(C(=O)N(C1=CC=CC=C1)NC2=CC=CC=C2)C(=O)O
Indicazioni di sicurezza

Il bumadizone è un farmaco ad attività antinfiammatoria.[1]

Farmacocinetica

Dopo somministrazione orale il bumadizone viene rapidamente assorbito a livello intestinale e distribuito nell'organismo. La concentrazione riscontrabile nei tessuti infiammati è maggiore che nel resto dell'organismo. Da 30 a 60 minuti dopo la somministrazione orale la concentrazione massima viene raggiunta nel fegato, nei reni, nel cuore, milza, muscolo e cervello, il che ne indica una buona diffusione nei tessuti. I livelli plasmatici raggiungono un picco tra 1 e 6 ore dopo la somministrazione.

L'emivita plasmatica è di circa 7 ore.[2][3].

Il farmaco viene eliminato con le urine e con le feci.

Usi clinici

Il farmaco viene utilizzato nel trattamento di forme reumatiche acute e croniche,[4][5][6] ed in particolare nella spondilite anchilosante[7] e nella artrite reumatoide[8].

Dosi terapeutiche

Bumadizone viene somministrato per via orale, in compresse, alla dose iniziale di 220 mg ogni otto ore.

Come per altri antinfiammatori è bene che le compresse siano assunte durante o dopo i pasti.

La dose di mantenimento è di 110 mg 2-3 volte al giorno.

Controindicazioni

È controindicato in caso di scompenso cardiaco, epatopatie, nefrite cronica, emopatie, ulcere gastrointestinali antecedenti. In caso di elevato dosaggio o in presenza di edema si consiglia una dieta iposodica.

Effetti collaterali

Il farmaco può causare disturbi gastrointestinali tra cui (gastralgia, nausea, diarrea), nonché ritenzione idrica, fenomeni allergici, leucopenia, trombocitopenia, anemia aplastica (rara) e, in casi eccezionali, ulcera gastrointestinale perforante.[9]

Gravidanza ed allattamento

Bumadizone non deve essere utilizzato durante la gravidanza, tranne che il medico non lo ritenga assolutamente essenziale.

In questo caso il suo utilizzo richiede una attenta e prudente valutazione dei potenziali benefici contro gli eventuali rischi per la madre ed il feto, in particolare nel primo e nel terzo trimestre di gravidanza. Il farmaco è stato rilevato nel latte materno, quindi è bene evitarne l'uso durante l'allattamento.

Note

  1. ^ (DE) Riedel R, Schoetensack W, [Pharmacology of butylmalonic acidmono-(1,2-diphenylhydrazide)-calcium (bumadizone-calcium)], in Arzneimittelforschung, vol. 23, n. 9, settembre 1973, pp. 1215–25, PMID 4801213.
  2. ^ (DE) Spahn H, Mutschler E, Geissler HE, Faust-Tinnefeldt G, [Comparison of bumadizone-, phenylbutazone- and oxyphenbutazone-plasma levels after a single oral dose of phenylbutazone and of bumadizone, respectively (author's transl)], in Arzneimittelforschung, vol. 31, n. 3, 1981, pp. 499–503, PMID 6894380.
  3. ^ (DE) Spahn H, Mutschler E, [Determination of bumadizone, phenylbutazone and oxyphenbutazone in human plasma by high-performance liquid chromatography (author's transl)], in Arzneimittelforschung, vol. 31, n. 3, 1981, pp. 495–9, PMID 6894379.
  4. ^ (DE) Bröll H, Tausch G, Sochor H, Eberl R, [Bumadizone-calcium in rheumatic diseases. Clinical study], in MMW Munch Med Wochenschr, vol. 116, n. 15, febbraio 1974, pp. 339–40, PMID.
  5. ^ (CS) Pavelka K, Vojtísek O, Hándlová D, [Bumadizone in long term therapy of progressive polyarthritis. (Open controlled experiment)], in Fysiatr Revmatol Vestn, vol. 55, n. 4, agosto 1977, pp. 217–22, PMID 332608.
  6. ^ (DE) Medenica R, Abele I, Dobryk R, Kuzmanovic I, Junet R, [Double-blind clinical study with placebo versus bumadizone-Ca in 113 patients with rheumatism], in Arzneimittelforschung, vol. 23, n. 12, dicembre 1973, pp. 1817–22, PMID 4544615.
  7. ^ (DE) Franke M, Manz G, [Bumadizone-calcium-semihydrate (Eumotol) and oxyphenbutazone in the treatment of ankylosing spondylitis. A clinical double-blind study], in Med Welt, vol. 26, n. 27-28, luglio 1975, pp. 1335–40, PMID 1100983.
  8. ^ Solomon L, Abrams G, Bumadizone calcium in the treatment of rheumatoid arthritis, in S. Afr. Med. J., vol. 52, n. 10, agosto 1977, pp. 391–3, PMID 331502.
  9. ^ (DE) Widhammer M, Frenger W, [Efficacy and compatibility of bumadizone-Ca in rheumatoid diseases. A comparison with oxyphenbutazone], in Arzneimittelforschung, vol. 23, n. 12, dicembre 1973, pp. 1813–6, PMID 4544614.

Bibliografia

  • Schmid, Helv. Chim. Acta 53, 2239, 1970; Pawelczyk, Wachowiak, Acta Pol. Pharm. 26, 433, 1969.

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