BIGUMALUM (Bigumalum; Chlorguanid, Paludrine, Proguanili Hydrochloridum; GFH, joint venture. B) — antimalarial means. N1-para-Hlorfenil-N5-izopropilbiguanida hydrochloride, C 11 H 16 N 5 Cl • HCl.
Crystal powder of white color, bitter taste, inodorous. We will dissolve in water a little (at t ° 20 ° in concentration 1: 100).
B. it is quickly soaked up from went. - kish. path. Appears in urine in 20 — 30 min. after intake, after intravenous administration — in 5 — 10 min. B.'s removal continues within a week, and sometimes 11 — 17 days after the termination of treatment. B. affects preferential sexless forms of malarial plasmodiums, but has also gametotropny property.
Apply B. at all forms of malaria; the highest effect is reached at tropical malaria.
Appoint inside after food (wash down with water 1/4 — 1/2 glasses) according to the scheme: in the 1st day 0,6 g on 2 receptions with an interval of 6 hours; on 2 — the 4th day on 0,3 g once a day. Appoint to a course of treatment (4 — 5 days) 1,5 g of B.
the Highest doses for adults: one-time 0,3 g, daily 0,6 g. At a heavy current the course of treatment is increased up to 7 days (a daily dose from the 2nd to the 7th day — 0,3 g). At the first signs indicating development of a malarial coma, the daily dose is increased to 0,8 g (2 times on 0,3 g and 1 time of 0,2 g with a 6-hour interval). Then in the next 4 days appoint 0,3 g a day.
At unconsciousness and vomiting enter 10 — 15 ml of 1% of solution into a vein; in need of an injection repeat; the single dose shall not exceed 0,15 g (15 ml of 1% of solution), daily — 0,45 g. For receiving 1% of solution of 1 g of B. dissolve in 100 ml the solution of sodium chloride which is slightly warmed up 0,5 — 0,6%; after full dissolution of powder liquid is filtered and sterilized fluid steam or on the water bath within 30 — 40 min.
Feverish paroxysms at most of patients (apprx. 90%) are stopped in the first 2 days; schizonts of malarial parasites in peripheral blood can remain up to 7 — 11 days, but, as a rule, disappear within 3 — 5 days of treatment.
To children appoint according to age: till 1 year — 0,025 g a day, 1 — 2 years — 0,05 g, 2 — 4 years — 0,075 g, 4 — 6 years — 0,1 g, 6 — 8 years — 0,15 g, 8 — 12 years — 0,15-0,2 g, 12 — 16 years - 0,25 g in one step; course of treatment of 5 days. To children up to 5 years B. is appointed inside in the form of 0,5% of the solution prepared from powder or tablets (5 tablets on 0,1 g on 100 ml of water; one teaspoon of solution contains 0,025 g of drug).
For the purpose of prevention appoint the adult 0,2 g (2 tablets) 2 times a week (to the 1st and 4th day).
B. it is well transferred by patients, including pregnant women and children; nausea, vomiting is sometimes observed, children have a vomiting, skoroprokhodyashchy increase in number of leukocytes and emergence in peripheral blood of young neutrophils; the temporary decrease in anti-toxic function of a liver revealed by Pytel's test — Kvika is described; the albuminuria and existence in urine of erythrocytes is occasionally noted. B. is defined in urine and fabrics by a colorimetric method of Spinks — Totti (A. Spinks, M. of Tottey) in A. I. Ilkhamov's modification (1949).
In those areas where B. is widely applied, especially in low doses, bystry development of resistance to it of all types of malarial plasmodiums is noted.
Forms of release: tablets on 0,1 and 0,05 g (for children), powder for preparation of solutions. Keep in well corked container.
See also Antimalarial means .
Bibliography: Gontayeva A. A., Novoselov E. I. and Kostylyuk K. F. Treatment of malaria to Bigumalums (r-chlorophenyls-N-izopropilbiguanid), Medical parazitol., t. 17, century 4, page 289, 1948; Ilkhamov A. I. Absorbability, distribution and allocation bigumalya from an organism, in the same place, t. 18, century 6, page 546, 1949, bibliogr.; Kai-sirski y I. A. and P l about t of N and to about in H. H. Diseases of tropical countries, page 9, M., 1964; Lysenko A. Ya. and Levitan-s to and I am P. B. To a question of homotropic properties bigumalya at a tetrian fever, Medical parazitol., t. 19, century 5, page 420, 1950; The Multivolume guide to microbiology, clinic and epidemiology of infectious diseases, under the editorship of H. N. Shue-kova-Verezhnikova, t. 9, page 37, M., 1968; Instructions on treatment and chemoprophylaxis of malaria, under the editorship of Sh. D. Moszkowski, page 29, M., 1972.
H. N. Plotnikov.