NOVOBIOCIN (synonym: Albamycin, Cathomycin, Cathocin, Inamycin, Novomycin, Spheromycin, Vulcamycine) — the antibacterial antibiotic which is formed at biosynthesis of Streptomyces spheroides. It is received in 1955.
Crystal powder of yellow color, is sensitive to effect of light, in medical practice is applied in the form of sodium and calcic salts.
Total formula of sodium salt of novobiocin (Novobiocinum-nat-rium) C 31 H 36 N 2 O 11 , pier. weight 634,6, constitutional formula:
Sodium salt of novobiocin at pH 7,5 well of a rastvorim in water (100 mg/ml), calcic is dissolved badly. Water solutions of novobiocin of sodium salt at pH 7,0 — 10,0 and t ° 24 ° within 2 months are inactivated for 50%.
The N on an action spectrum is close to to macroleads (see), it is active concerning gram-positive and gram-negative cocci (stafilokokk, pneumococci, meningokokk and gonokokk, to a lesser extent — streptococci and enterococci), anthracic sticks, korinebakteriya, nek-ry gram-negative bacteria (Haemophilus influenzae, bacteria of the sort Proteus). Among gram-negative bacteria practical value has sensitivity to N. a protea, growth of many strains to-rogo is suppressed with an antibiotic at the concentration arising in an organism after introduction of the recommended doses of an antibiotic.
The mechanism of action of N. on a bacterium is connected with suppression of a DNA polymerase of a bacterial cell that causes blocking of synthesis of DNA. Resistance to N. of in vitro and in the course of treatment by an antibiotic develops quickly. Cross stability with other antibiotics is not observed. N.'s combination to other drugs (amine of of l iko z ides, those a Torah a cycle other, levomycetinum) detains formation of stability and strengthens antibacterial effect of an antibiotic.
The N is well soaked up at intake, serum proteins communicates for 95 — 98%. Therapeutic concentration in blood would be maintained during — 8 hours after introduction; at repeated introductions cumulation of drug is observed. The N has bad diffusion properties, its concentration in fabrics and liquids of an organism is much lower found in blood.
From N.'s organism it is allocated preferential to cookies, in bile its concentration is 2 — 8 times higher, than in blood. To 30% of the entered dose also only 4% with urine are allocated with a stake.
N apply inside at treatment of the infections caused by microorganisms, steady against other antibiotics and sensitive to its action (hl. obr. stafilokokkam): at sepsis, pneumonia, a coloenteritis, infections of urinary tract, a wound fever, etc. The single dose of novobiocin for adult 250 — 500 mg, is appointed with an interval of 6 — 12 hour. An average daily dose of 1 g, maximum 2 g (on 500 mg 4 times a day at a severe disease). Detyakhm drug appoint at the rate of 20 — 40 mg/kg a day, newborn — 15 mg/kg.
At N.'s treatment side reactions are observed in 7 — 20% of cases in the form of various skin rashes, an itch, temperature increase. The N possesses the sensibilizing action, at repeated courses of use the frequency of emergence of allergic reactions can increase. Dispeptic frustration are observed in 1 — 8% of cases. Seldom at N.'s treatment icteric coloring of visible mucous membranes and scleras appears. The passing leukopenia, anemia are described.
Due to the bystry development of stability of microflora to drug N.'s treatment is carried out under control of definition of sensitivity of the activator in dynamics.
Novobiocin sodium salt is produced in tablets on 0,125 and 0,25 g.
Store drug in the dry, protected from light place at the room temperature; the list B.
See also Antibiotics .
Bibliography: Navashin G. M and F ohms and N and I. P. Reference book on antibiotics, page 130, M., 1974; T an u with h-n i t z Ch. Rationelle antimikrobielle Chemotherapie, S. 145, Lpz., 1976.
I. P. Fomina.