Streptomycin

General characteristics. Structure:

Active ingredient: 1 g of streptomycin of sulfate sterile in terms of streptomycin.

Antibiotic of a broad spectrum of activity.

Pharmacological properties:

Pharmacodynamics. Aminoglycoside. It is formed in the course of life activity of radiant mushrooms of Streptomyces globisporus or other types. In low concentration has bacteriostatic action: getting in a microbic cell, contacts specific proteins receptors on 30S subunit of ribosomes, breaking formation of the initiating complex — matrix PHK-30S ribosome subunit that leads to disintegration of polyribosomes, and, as a result of it, - there are defects when reading information from DNA. Defective proteins are synthesized that leads to a stunt and development of a microbic cell. In higher concentration renders bactericidal effect (damages cytoplasmic membranes, causing death of a microbic cell). Possesses a broad spectrum of activity.

 It is active concerning Mycobacterium tuberculosis. majority of gram-negative bacteria (Escherichia coli, Salmonella spp., Shigella spp. Yersinia spp. Klebsiella spp. Haemophilias iniluenzae. Klebsiella pneumoniae. Neisseria gonorrhoeae. Neisseria meningitidis. Brucella spp. Francisella tularensis, Yersinia pcstis), some gram-positive microorganisms (Staphylococcus spp.). It is moderately active concerning Streptococcus spp. including an izheesta at a temperature not vysheugimbeta-laktamny the place, to eparata from group penitsillinovstreptococcus pneumop.iae. F.nterococcus spp. It is steady in the subacidic environment, but easily collapses in solutions of strong acids and alkalis when heating. Secondary stability of bacteria develops quickly. In a combination with penicillin or Vancomycinum it is effective in treatment of the endocarditis caused by Enterococcus fecal is or Streptococcus viridans

Pharmacokinetics. At intramuscular introduction (in oil) it is quickly and completely soaked up. Time of achievement of the maximum concentration in blood - 0.5-1.5 h, the maximum concentration in blood after introduction of 1 g in oil - 25-50 mkg/ml. Communication with proteins of plasma - less than 10%. It is distributed in extracellular liquid, liquid of abscesses, a pleural exudate, in ascitic, pericardiac, synovial, lymphatic and peritoneal liquids. High concentration are created in kidneys, a liver, lungs; low - in bone and fatty tissue. Distribution volume adults — 0.26 l/kg, at children have 0.2-0.4 l/kg, at newborns at the age of less than 1 week and with a body weight less than 1500 - to 0.68 l/kg, at the age of less than 1 week and with a body weight more than 1500 - to 0:58 l/kg, at patients with a mucoviscidosis - 0.3-0.39 l/kg.

Does not get through the unimpaired blood-brain barrier. Gets through a placenta and into breast milk. Is not exposed to metabolism. Adults - 2-4 h have an elimination half-life at newborns - 5-8 h. Children of more advanced age have 2.5-4 h. A final elimination half-life — more than 100 h (release from intracellular depots). At patients with a renal failure of a periodpoluvyvedeniye varies depending on insufficiency degree - to 100 h, patients with a mucoviscidosis have 1-2 h, at patients with burns and a hyperthermia can be shorter in comparison with average values owing to the increased clearance. It is removed by kidneys (95%) in not changed look.

Indications to use:

Tuberculosis of various localization (including tubercular meningitis), a venereal granuloma, a tularemia, a brucellosis, plague, an endocarditis (in combination with ampicillin), intestinal infections, infections of urinary tract (after establishment of sensitivity of the activator).

Route of administration and doses:

Intramusculary, intratrakhealno, intrabronkhialno (in the form of aerosols) Intramuscular introduction the Single dose for adults at introduction in oil - 0.5-1 g, daily - 1-2 g. At bad portability the patient with body weight less than 50 kg and to persons are more senior than 60 years - in a daily dose of 750 mg. For children aged up to 3 months - in a dose at the rate of 10 mg/kg/days, aged from 3 up to 6 months - 15 mg/kg, from 6 months to 2 years - 20 mg/kg. For children up to 13 years and teenagers a daily dose - 15-20 mg/kg, but no more than 500 mg/days - for children up to 13 years and 1 g/days - for teenagers.

Maximum doses: to children under 2 years of-20 mg/kg/days; 3-4 years - one-time - 150 mg, daily - 300 mg; 5-6 years - one-time - 175 mg, daily – 350 mg; 7-9 years - one-time - 200 mg, daily - 400 mg; 9-14 years - one-time - 250 mg, daily - 500 mg.

At not tubercular etiology introduction frequency - 3-4 times a day, treatment duration - 7-10 days. At treatment of tuberculosis the daily dose is entered into 1 reception, at bad portability - into 2 receptions, treatment duration - 3 months and more.

Intratracheal introduction of Intratrakhealno, the adult - on 0.5-1 g 2-3 times a week.

For patients with the accompanying arterial hypertension and coronary heart disease an initial dose - 250 mg/days. At good tolerance the dose is increased. At a renal failure the modes of therapy korrigirut according to its degree.

Features of use:

Use at pregnancy and during breastfeeding. Use at pregnancy and in the period of a lactation is contraindicated. Streptomycin gets through a placental barrier and can have nephrotoxic effect on a fruit of the person. At babies whose mothers received streptomycin at pregnancy development of deafness is possible. It is allocated with breast milk.

During treatment it is necessary at least 1 time a week to control function of kidneys, an acoustical nerve and vestibular mechanism.

The probability of development of nephrotoxicity is higher at patients with a renal failure, and also at purpose of high doses or for a long time (at this category of patients daily control of function of kidneys can be required).

At unsatisfactory audiometric tests the dose of drug is reduced or stop treatment.

Aminoglycosides get into breast milk in small amounts (as they are badly soaked up from a GIT, the related complications at babies it was not registered).

In the absence of positive clinical dynamics it is necessary to remember a possibility of development of resistant microorganisms. In similar cases it is necessary to cancel treatment and to begin performing the corresponding therapy.

Side effects:

From the alimentary system: nausea, vomiting, diarrhea, abnormal liver function (increase in activity of "hepatic" transaminases, hyperbilirubinemia).

From a nervous system: a headache, drowsiness, weakness, peripheral neuritis, neuritis of a facial nerve (a burning sensation in a face or an oral cavity, paresthesia), it is rare - neuromuscular blockade at simultaneous introduction with muscle relaxants (breath difficulty, a night apnoea, an apnoea), neurotoxic action (twitching of muscles, paresthesias, epileptic seizures).

From sense bodys: ototoxicity (a hearing loss, a ring, buzz or feeling of a congestion in ears, decrease in hearing, up to irreversible deafness), vestibular and labyrinth disturbances (a diskoordination, dizziness, nausea, vomiting, instability).

From an urinary system: nephrotoxicity (significant increase or reduction of frequency of an urination, oliguria, polyuria, thirst, loss of appetite, nausea, vomiting).

Allergic reactions: itch, dermahemia, rash, Quincke's disease, fever.

Local reactions: a hyperemia and pain in an injection site.

Interaction with other medicines:

It is incompatible with other nefro-and ototoksichny HP (including with other aminoglycosides, polymyxins).

Reduces efficiency of anti-myasthenic HP.

Shows a synergism at interaction with a beta laktamnymi antibiotics.

Metoksifluran increases risk of development of side effects.

HP for inhalation general anesthesia (galogensoderzhashchy hydrocarbons), narcotic analgetics, transfusion of large amounts of blood with citrate preservatives as anticoagulants, other. The hp blocking neuromuscular transmission strengthen neuromuscular blockade.

Contraindications:

The obliterating endarteritis, myasthenia, diseases connected with an inflammation of the VIII couple of cranial nerve (a predverno-cochlear or acoustical nerve), severe forms of a cardiovascular and renal failure, disturbance of cerebral circulation, hypersensitivity to streptomycin, pregnancy, a lactation (breastfeeding).

With care. A myasthenia, parkinsonism, botulism (aminoglycosides can cause neuromuscular transmission disturbance that leads to further weakening of skeletal muscles), an obliterating endarteritis, chronic heart failure of the II-III Art., a chronic renal failure, dehydration, disturbance of cerebral circulation, tendency to bleeding, advanced and children's age.

Overdose:

Symptoms: toxic reactions (a hearing loss, an ataxy, dizziness, frustration of an urination, thirst, a loss of appetite, nausea, vomiting, a ring or feeling of a congestion in ears, breath disturbance).

Treatment: for lifting the siege of neuromuscular transmission and its effects - a hemodialysis or peritoneal dialysis, the antikholinesterazny medicines (M), salts of calcium ions, artificial ventilation of the lungs, other symptomatic and maintenance therapy.

Storage conditions:

Period of validity 3 years. After the period of validity specified on packaging not to use drug. List B. In the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Powder on 1,0 g of active agent in bottles from a tube glass for medicines with a capacity of 10 ml. For hospitals: on 50 bottles with drug together with the application instruction place in a box with lattices from a cardboard for a retail container.