ACETPHENETIDIENE (Phenacetinum; synonym: Acetophenetidin, Phenedin, etc.; GFH, joint venture. B) — analgesic and antipyretic. 1-Etok-si-4-atsetaminobenzol; C10H13NO2:
Inodorous white fine-crystalline powder, slightly bitter taste. We will dissolve in water very little, we will difficult dissolve in a boiling water (1:70), we will dissolve in 95% alcohol (1:16), it is a little ether-soluble also chloroform; g°pl 134 — 136 °; pier. weight (weight) 179,22.
Has soothing and febrifugal effect that is caused, apparently, by disturbance of biosynthesis of prostaglandins (see) owing to inhibition it is simple-glandinsintetazy in c. N of page. Unlike salicylates and other non-steroidal anti-inflammatory drugs in therapeutic doses practically does not influence activity it is simple-glandinsintetazy peripheral fabrics and in this regard has no the expressed antiinflammatory effect.
It is well soaked up from went. - kish. a path and in the maximum concentration collects in blood in 30 — 60 min. after intake. Easily gets through gistogemati-chesky barriers. It is metabolized in a liver, partially turning at the same time into an active metabolite paracetamol (see), in comparison with the Crimea F. is less active and more toxic. Metabolites and partially not changed F. are allocated with kidneys. An elimination half-life apprx. 45 — 90 min.
Apply hl. obr. as an anesthetic at joint and muscular pains, neuralgia, headaches, migraine. For this purpose F. often use in a combination with other non-narcotic analgesics. Appoint inside the adult 0,25 — 0,5 g 2 — 3 times a day. The highest doses for adults inside: one-time 0,5 g, daily 1,5 g.
Single doses for children: till 1 year — 0,025 — 0,05 g; 1 — 2 years — 0,1 g; 3 — 4 years — 0,15 g; 5 — 6 years — 0,2 g; 7 — 9 years — 0,25 g; 10 — 14 years — 0,25 — 0,3 g. Drug is appointed by 2 — 3 times a day.
As side effects F. causes allergic reactions, anemia and a methemoglobinemia. At prolonged use (especially at patients with a diabetes mellitus) can cause severe defeats of tubules of nights (so-called acetphenetidiene
vy nephrite) that is perhaps connected with the content in drug as impurity 72 of chloracetanilide. In this regard it is not recommended to appoint F. a sick diabetes mellitus and at diseases of kidneys.
Form of release: powder and tablets on 0,25 g. Storage: in well corked container. T. is also a part of a number of the combined tablets (Asfen, «Novomigrophenum», «Pyraphenum», «Pyrcophenum», «Citramonum», etc.).
See also Analgesic means, Antipyretics. Bibliography: Clinical pharmacology,
under the editorship of V. V. Zakusov, page 152, M., 1978; M and sh to about in with to and y M. D. Pharmaceuticals, p.1, page 185, M., 1984.
V. K. Muratov.