LINCOMYCIN (synonym: lincocinum, Mycivinum etc.) — antibacterial antibiotic , representative of 4-alkyl substituted compounds of gigranovy acid. It is received for the first time in 1962 from cultural Actinomyces lincolnensis var liquid. lincolnensis. It is formed also by other species of actinomycetes; in the USSR L. receive at biosynthesis of Actinomyces roseolus. Total formula L. — With 18 H 34 N 2 O 6 S; constitutional formula:
Hydrochloride of L. represents white crystal powder, well water soluble, a little soluble in methanol and almost insoluble in acetone. It is highly stable both in a crystal look, and in water solutions.
L. suppresses development of gram-positive bacteria: stafilokokk, streptococci (except for enterococci), pneumococci, causative agents of diphtheria, a malignant anthrax, gas gangrene and tetanus. On gram-negative bacteria, fungi and viruses L. does not work. Depending on sensitivity of bacteria and concentration of L. has bacteriostatic or bactericidal action. At the heart of the mechanism of antibacterial action of L. suppression of synthesis of protein in a microbic cell as a result of interaction of an antibiotic with 50 S-sub-units of ribosomes and disturbances of binding phenylalanine-S-PHK with a complex a ribosome — a matrix lies.
L. it is a little toxic. DL50 at intravenous administration to white mice averages 231 (213 - 251) mg/kg. At peroral and intramuscular introduction of L. it is quickly soaked up in blood and gets into all bodies and fabrics; its highest concentration are found in a bone tissue. So, after intramuscular introduction by the patient in a dose of 600 mg of L. appears in long tubular bones in concentration from 2,2 to 6,6 mkg on 1 g of a bone tissue that exceeds the minimum overwhelming concentration for the majority of strains of staphylococcus.
L. it is brought out of an organism with urine and bile. Time of semi-removal makes 5,4 ± 1 hour
Use in medicine
L. has high performance at the infection caused by antibiotic-resistant stafilokokka that allows to consider it an antibiotic of a reserve. Due to the high osteotropnost of L. is drug of the choice at treatment of acute and chronic osteomyelites. Indications to use of L. the staphylococcal infections (a septicaemia, pneumonia, an empyema of a pleura, an infection of skin and soft tissues, etc.) caused by strains, steady against other antibiotics, the staphylococcal osteomyelites, infections caused by streptococci, pneumococci and other gram-positive bacteria in patients with an allergy to penicillin are.
L. it is appointed inside, intramusculary and intravenously. At oral administration the daily dose for adults makes 2 g, for children of 30 — 60 mg/kg. The daily dose is given by fractionally equal parts in each 6 hours, for 1 — 2 hour to capsular food. At parenteral use the daily dose for adults makes 1,0 — 1,5 g, for children of 10 — 20 mg/kg and is entered for 2 — 3 times. Intravenously L. enter only kapelno. Single dose of drug dissolve in 250 ml 5% of solution of glucose or isotonic solution of sodium chloride and enter within 1,5 — 2 hour.
At disturbance of secretory function of kidneys of a dose of L. it is necessary to reduce to 1/3 — 1/2 doses or to increase intervals between introductions.
Drug is generally well transferred by patients. In 10 — 20% of cases nausea, abdominal pains, ponosa is observed (is more often at use of an antibiotic inside). At parenteral use the leukopenia, thrombocytopenia, increase of bilirubin in blood, increase in transaminazny activity of blood are noted. Emergence of allergic reactions is described (a small tortoiseshell, etc.).
Bibliography:Melnikova B. M . Chemotherapy of a wound fever in traumatology and orthopedics, page 45, M., 1975; Navashin S. M. and Fomina I. P. Reference book on antibiotics, page 126, M., 1974; Chernomordik A. B. Antibiotic lincomycin, Antibiotics, t. 13, No. 12, page. IZO, D968, bibliogr.
L. E. Goldberg.