Properties
What is it?
General Characteristics: International and Chemical Name: Streptomycin [0-2-deoxy-2-methylamino-α-L-glucopyranosyl-(1→2)-0-5-deoxy-3-C-formyl-α-L-lyxofuranosyl-(1→4)-N1-diamino-D-streptamine] trisulfate. Main Physicochemical Properties: White or almost white, odorless, hygroscopic powder. Composition: 1 vial contains sterile Streptomycin sulfate, calculated as 0.25 g, 1.0 g, or 0.5 g of streptomycin. Dosage Form: Powder for solution for injection in vials. Pharmacological Group: Antibiotic of the aminoglycoside group. Pharmacological Properties: Streptomycin is a broad-spectrum (bactericidal) antibiotic. It is active against Mycobacterium tuberculosis, most Gram-negative (Escherichia coli, Salmonella spp., Shigella spp., Klebsiella pneumoniae, Klebsiella spp., Haemophilus influenzae, Yersinia pestis, Francisella tularensis, Brucella spp., etc.) and some Gram-positive (Staphylococcus) microorganisms. The drug is less active against streptococci (including pneumococci). Streptomycin is not active against Proteus, Pseudomonas aeruginosa, anaerobic bacteria, spirochetes, rickettsiae, and viruses. The bactericidal action of the drug is due to its binding to the 30S subunit of bacterial ribosomes, which inhibits protein synthesis. Pharmacokinetics: The drug is poorly absorbed from the gastrointestinal tract and is almost entirely excreted through the intestines. It is used only parenterally. Streptomycin is rapidly and completely absorbed into the bloodstream after intramuscular administration. The maximum concentration of the drug in blood serum is observed 1-2 hours after administration. After a single administration of an average therapeutic dose, the antibiotic is detected in the blood for 6-8 hours. The drug accumulates in high concentrations in the lungs, liver, and extracellular fluids. The drug has a weak tropism for fatty and bone tissues. Streptomycin does not cross the intact blood-brain barrier. It penetrates the placenta and breast milk. The binding of the drug to plasma proteins occurs in less than 10% of cases. With normal renal excretory function, the drug does not accumulate in the body with repeated administration. The drug is not metabolized. Its half-life is 2-4 hours. It is mainly excreted from the body by the kidneys (95%) unchanged. The excretion of the drug from the body is slowed down in case of impaired renal function, during which its concentration in the body increases and side effects may develop (neurotoxicity). Indications: The drug is used as an antituberculosis agent, primarily for tuberculosis of the lungs and other organs. In previously treated patients, it is advisable to determine the sensitivity of mycobacteria to it in the laboratory. In addition, Streptomycin-CMP is used for purulent inflammation of various localizations caused by Gram-positive and Gram-negative microorganisms sensitive to the drug: pneumonia caused by Klebsiella (in combination with levomycetin), plague and tularemia (in combination with tetracycline), brucellosis and endocarditis (in combination with other antibiotics). Dosage and Administration: The drug is administered intramuscularly, as well as by aerosol and intratracheally. In adults, the drug is also administered intracisternally. In adults, the drug is administered intramuscularly in a single dose of 0.5-1 g, with a maximum daily dose of 2 g. In patients weighing less than 50 kg and over 60 years of age, the daily dose should generally not exceed 0.75 g. In children and adolescents, the daily dose is determined based on 15-20 mg/kg of body weight, but not more than 0.5 g per day for children and 1 g for adolescents, in a single dose. For the treatment of tuberculosis, the daily dose is usually administered once. In case of intolerance to the drug, the daily dose can be divided into 2 administrations. The duration of treatment depends on the form and phase of the disease (3 months or more). For the treatment of infections of non-tuberculous etiology, the daily dose is administered in 3-4 divided doses at 6-8 hour intervals. The duration of treatment is 7-10 days (should not exceed 14 days). For intramuscular administration, the drug is diluted with sterile water for injection, sodium chloride solution, or 0.25-0.5% novocaine solution at a rate of 4 ml of diluent per 1 g of drug. The solution is prepared extemporaneously. For intratracheal administration in adults, the drug is administered in a dose of 0.5-1 g, dissolved in 5-7 ml of isotonic sodium chloride solution or 0.5% novocaine solution, 2-3 or more times a week. For aerosol administration in adults, the drug is administered in a dose of 0.5-1 g. For this route of administration, the drug is diluted in 4-5 ml (for warm inhalation - 25-100 ml) of isotonic sodium chloride solution. In children, when administered by the described method, it is used in the same proportions as for intramuscular administration of the drug. Depending on the indications, other drugs compatible with streptomycin can be added to the inhalation solution. For intracisternal administration, the drug is administered by insufflation in the form of a finely dispersed powder or by instillation of a 10% solution under surgical hospital conditions once a day with a total dose not exceeding 1 g, regardless of the number of cavities and the method of administration. In patients with hypertension and ischemic heart disease, the drug is used in small doses (up to 0.25 g) regardless of the route of administration. If the drug is well tolerated, the dose can be increased. In patients with impaired renal and liver function, the daily dose of the drug should be reduced. With an endogenous creatinine clearance of 50-60 ml/min, the dose of the drug should not exceed 0.5 g, and with 40-50 ml/min - not more than 0.4 g. Side Effects: Relatively severe side effects during the use of the drug include blockade of the VIII cranial nerve pair and resulting vestibular disorders (dizziness, nausea, vomiting, impaired coordination), hearing loss (tinnitus, noise, deafness), peripheral neuritis, optic neuritis, suppression of neuromuscular transmission (difficulty breathing, apnea, weakness, drowsiness). Very rarely - blockade of neuromuscular transmission leading to respiratory arrest, especially in patients with myasthenia gravis, or in the postoperative period against the background of residual effects of non-depolarizing muscle relaxants. At the first sign of neuromuscular disorder, intravenous administration of calcium chloride and subcutaneous administration of prozerin are necessary. In case of apnea, the patient is transferred to artificial respiration. Impaired renal function (albuminuria, hematuria), diarrhea, muscle cramps, increased bleeding, polyneuropathy, allergic reactions (skin rash, urticaria, eosinophilia, Quincke's edema, etc., rarely anaphylactic shock), redness and pain at the injection site may occur. Rarely, pain in the cardiac region, tachycardia are observed. In case of neurotoxic complications (headache, paresis, hearing loss), the drug intake is discontinued and symptomatic or pathogenetic therapy is carried out, in particular, calcium pantothenate, thiamine, pyridoxine, pyridoxal phosphate are prescribed. At the first sign of an allergic reaction during drug administration, it is necessary to discontinue the drug and carry out desensitizing therapy. At the first sign of anaphylactic shock, it is necessary to manage the patient out of this condition. Contraindications: Diseases of the auditory and vestibular apparatus associated with neuritis of the VIII cranial nerve pair, or residual effects of otoneuritis, severe renal and cardiovascular failure, cerebrovascular accident, obliterating endarteritis, hypersensitivity to streptomycin, myasthenia gravis, botulism, pregnancy and lactation. Intracisternal administration of the drug is contraindicated in case of unhealed pleural cavity (catheter insertion site) and in case of close localization of the cavity to the lung hilum. Interactions with Other Drugs: It is not recommended to mix Streptomycin-CMP in the same syringe with antibiotics of the penicillin group (carbenicillin and others) and cephalosporins. Simultaneous use of the drug with aminoglycosides, polymyxins, capreomycin increases the risk of oto- and nephrotoxic effects. Parenteral administration of indomethacin hinders the excretion of Streptomycin-CMP from the body. Streptomycin-CMP enhances the side effects of oto- and nephrotoxic agents, muscle relaxants, methoxyflurane, and reduces the effectiveness of antiasthmatic agents. It is not used against the background of dehydrating therapy and in combination with diuretics. Overdose: Manifested as blockade of neuromuscular transmission leading to respiratory arrest. Treatment: Calcium chloride is administered intravenously, and prozerin subcutaneously; in case of apnea, the patient is transferred to artificial lung ventilation. Special Instructions: With prolonged use of the drug, nephrotoxic effects (proteinuria, hematuria, cylindruria) are observed, therefore, during the treatment period, it is necessary to examine the urine at least once a month. Kidney damage is reversible and disappears with timely discontinuation of the drug. During the treatment period, it is necessary to check hearing function and the vestibular apparatus. The drug is prescribed to infants and pregnant women only in cases of vital necessity. Untimely discontinuation of the drug can lead to deafness. Storage Conditions and Shelf Life: Store in a dry place, protected from children, at a temperature not exceeding +25 °C. Shelf life - 3 years. Dispensing: By prescription
