Streptomycin (When ATH A07AA04)
When ATH:
A07AA04
Characteristic.
Aminoglycosides I generation, TB medication I series. Producing luminous mushrooms Streptomyces globisporus streptomycini or other related microorganisms.
Streptomycin sulfate - powder or porous mass of white or nearly white, bitter taste. Hygroscopic. Practically insoluble in ethyl alcohol, xloroforme, ether; easily soluble in water. So, solubility (mg / ml) at 28 °C: water >20; methanol 0,85; ethanol 0,30; isopropanol 0,01; petroleum ether 0,015; carbonic tetrachloride 0,035; ether 0,035. Stable in mildly acidic conditions, easily destroyed in solutions of strong acids and alkalis under heating. Molecular weight 1457,39.
Streptomycin sulfate used / m, inside (to influence the intestinal flora), is introduced into the body cavity. For injection under the lining of the brain with meningitis only use streptomycin-calcium chloride complex (double streptomycin hydrochloride salt and calcium chloride), which has minimal irritant, than other drugs streptomycin. The toxicity of streptomycin calcium chloride complex of significant, so use it in case of emergency.
Pharmacological action.
Broad-spectrum antibacterial, bactericide, TB.
Application.
Tuberculosis various localization (incl. tuberculous meningitis) in combination with other anti-tuberculosis agents, venereal granuloma, tulyaremiya, Brucellosis, plague, bacterial endocarditis (in combination with penicillin, ampicillin or vancomycin), intestinal infections and urinary tract infections (after the establishment of the sensitivity of the pathogen).
Contraindications.
Hypersensitivity (incl. other aminoglycosides history), organic lesions VIII cranial nerves, severe chronic renal failure with azotemia and uremia.
Restrictions apply.
Myasthenia, parkinsonizm, botulism (aminoglycosides can cause a violation of neuromuscular transmission, which leads to a further weakening of the skeletal muscles), diseases of the blood, tendency to bleeding, cerebrovascular accident, occlusive disease, cardiac insufficiency II-III art., severe forms of hypertension and coronary artery disease, recent myocardial infarction, chronic renal failure, degidratatsiya, liver, the elderly and children's age, the neonatal period, incl. in preterm infants.
Pregnancy and breast-feeding.
During pregnancy, used only for health (adequate and well-controlled studies in humans have not held). The concentration of streptomycin in the blood of the fetus is generally less 50% that of the mother's blood. Streptomycin cause deafness in children, whose mothers received it during pregnancy. It penetrates through the placenta, It determined the serum concentrations of fetal, of about 50% the concentration in maternal serum. It has nephro- and ototoksicheskoe effect of fruit.
Category actions result in FDA - D. (There is evidence of the risk of adverse effects of drugs on the human fetus, obtained in research or practice, However, the potential benefits, associated with drugs in pregnant, may justify its use, in spite of the possible risk, if the drug is needed in life-threatening situations or severe disease, when safer agents should not be used or are ineffective.)
In small amounts excreted in breast milk, may have an impact on the intestinal microflora, However, due to low absorption from the gastrointestinal tract, other complications in infants is not registered. At the time of treatment should stop breastfeeding.
Side effects.
From the nervous system and sensory organs: headache, muscle twitching, inhibition of neuromuscular transmission (muscular weakness, difficulty breathing), drowsiness, clonus, paraesthesia, seizures, vestibular and labyrinth disorders (unsteady gait, uncoordinated movements, dizziness, nausea, vomiting), ototoxicity (noise or ringing in the ears, the feeling of "stuffiness" ear, diminished hearing, up to complete deafness), neuritis of the facial nerve (burning sensation in the facial area, paraesthesia), amblyopia, peripheral neuritis, araxnoidit, encephalopathy; rarely - neuromuscular blockade with simultaneous introduction to muscle relaxants (difficulty breathing, sleep apnea, respiratory arrest).
Cardio-vascular system and blood (hematopoiesis, hemostasis): heartbeat, tachycardia, increased bleeding, trombo- and leukopenia, pancytopenia, gemoliticheskaya anemia, eozinofilija.
From the digestive tract: nausea, vomiting, dysbiosis, diarrhea, abnormal liver function (increase in liver transaminases, giperʙiliruʙinemija).
With the genitourinary system: nephrotoxicity (substantial increase or decrease in urinary frequency, oligurija, polyuria, albuminuria, hematuria).
Allergic reactions: itching, rash, dermahemia, hives, angioedema, anaphylactic shock.
Other: fever, dermatitis, joint pain; Local reactions - redness and pain at the injection site.
Cooperation.
When used together with penicillins or cephalosporins observed synergy against some aerobic. However unacceptable streptomycin mix in the same syringe or a fluid system with beta-lactam antibiotics (penicillins, cephalosporins), and heparin due physicochemical incompatibility. Indomethacin, phenylbutazone and other NSAIDs, violate renal blood flow, can inhibit the excretion of streptomycin from the body. With the simultaneous and / or sequential use of two or more aminoglycosides (neomycin, gentamicin, monomitsin and tobramycin, netilmycin, amikacin) their antibacterial activity is weakened (competition for a mechanism of "capture" of microbial cells), and toxic effects are amplified. It should not be used in conjunction with viomycin, полимиксином B, metoksifluranom, амфотерицином B, ethacrynic acid, vancomycin, capreomycin and other GTR- and nephrotoxic agents, and furosemide. In an application with means for inhalation anesthesia, incl. metoksifluranom, kurarepodobnymi drugs, opioid analgesics, magnesium sulfate and polymyxin for parenteral administration, as well as large quantities of blood transfusions with citrate preservative enhanced neuromuscular blockade. Reduces the effectiveness of drugs antimiastenicheskih (during and after treatment with streptomycin dose adjustment is required antimiastenicheskih funds).
Overdose.
Symptoms: neuromuscular blockade until the cessation of breathing, infants - CNS depression (slackness, stupor, coma, profound respiratory depression).
Treatment: calcium chloride / in, antiholinesteraznye funds (neostigmine n / a), simptomaticheskaya therapy, if necessary - IVL.
Dosing and Administration.
/ M, intratracheal, intrabronhialno (in the form of aerosols), vnutrykavernozno, inside (for topical treatment of infections of the gastrointestinal tract). In tuberculosis: / m, single dose for adults - 0.5-1 g, daily - 1 g (The maximum daily dose - 2 g), administered 2-3 times per week for 3 months or more; children and adolescents - at the rate of 15-20 mg / kg / day / m, the maximum daily dose for children - 0,5 g, for teens - 1 g. And intratracheally as aerosols - 0.5-1 g adult 2-3 times per week. Vnutrikavernozno - fine powder insufflation and instillation 10% solution for 0, 250.5 g / day (no more 1,0 g / day), in a surgical hospital.
Infections nontuberculous etiology: / m, children and adults on the basis of 15 mg / kg / day (no more 2,0 g / day), Exchange 7-10 (no more 14) days.
Patients with hypertension and coronary heart disease, treatment is initiated with a reduced dose (0,25 g / day), if tolerated dose was increased to normal. If the kidney function is calculated daily dose based on creatinine clearance: Cl creatinine at 50-60 ml / min - max 0,5 g, 40-50 Ml / min - max 0,4 g.
Precautions.
Due to the high toxicity and development of resistance of microorganisms with the use of other infections (except tuberculosis) It should be strictly limited. Previously treated TB patients should be given streptomycin after laboratory susceptibility allocated patients mycobacteria. In elderly patients, the daily dose should be reduced. Newborns and infants streptomycin appoint only for health. Treatment should be under close medical supervision. If you have risk factors for toxic effects should regularly identify the peak and residual concentration of streptomycin in the blood serum (conduct therapeutic drug monitoring). Before and during treatment should regularly monitor function VIII cranial nerves (audiogram, caloric test) and kidney. At the first sign of GR- or nephrotoxicity drug overturned. People, long in contact with streptomycin (medical staff, pharmacists, employees of pharmaceutical companies), may develop contact dermatitis. To avoid this, precautions need to observe (work gloves etc.)
Doses calculate the mass (weight) terms, or in terms of action (ED); 1 ED is 1 g chemically pure streptomycin base. Given the poor distribution of aminoglycosides in adipose tissue, patients, body weight exceeds the ideal more than 25%, daily dose, calculated on actual body weight, must be reduced by 25%. In malnourished patients increase the dose 25%.