Capreomycin
When ATH:
J04AB30
Characteristic.
Anti-TB drugs, polypeptide antibiotics, produced Streptomyces capreolus. It is a complex of 4 microbiologically active components, whose structure is not fully established. A mixture of capreomycin IA, IB, IIA and IIB has the approximate percentage 25, 67, 3 and 6%. Capreomycin is a white substance. Soluble in water to form a colorless solution. Practically insoluble in most organic solvents. It is used in the form of capreomycin sulfate.
Pharmacological action.
Antiphthisic.
Application.
Pulmonary tuberculosis (incl. with inefficiency and intolerance of drugs I series).
Contraindications.
Hypersensitivity, childhood (Safety and efficacy have not been determined).
Restrictions apply.
The defeat of the VIII cranial nerves (may cause auditory and vestibular disorders), myasthenia, parkinsonizm, degidratatsiya (may increase risk of toxicity due to elevated concentrations of serum), impairment of renal function (due to nephrotoxicity), advanced age.
Pregnancy and breast-feeding.
When pregnancy is possible, if the potential benefit to the mother outweighs the potential risk to the fetus (capreomycin passes through the placenta, adequate and well-controlled studies in pregnant women were not conducted).
In experiments on rats, receiving daily doses of ≥50 mg / kg (3,5 human dose), shown teratogenic effects, manifested in the appearance of some animals curved ribs.
Category actions result in FDA - C. (The study of reproduction in animals has revealed adverse effects on the fetus, and adequate and well-controlled studies in pregnant women have not held, However, the potential benefits, associated with drugs in pregnant, may justify its use, in spite of the possible risk.)
In the period of treatment should stop breastfeeding (unknown, Do penetrates capreomycin in breast milk).
Side effects.
With the genitourinary system: Nephrotoxicity is chronic nephritis, kidney damage with necrosis of the tubules, dizurija (increase / decrease the frequency of urination or amount of urine), renal failure, increasing the level of urea nitrogen in the blood more than 20-30 mg/100 ml (46%) and serum creatinine, цilindrurija, mikrogematuriâ, leucocyturia.
From the nervous system and sensory organs: unusual tiredness or weakness, drowsiness, neuromuscular block, difficulty breathing (as a result of lowering the tone of respiratory muscles) up to cessation of breathing; ototoxicity is a decrease in hearing (subclinical — 11%, clinically expressed — 3%), incl. irreversible, noise, ringing, buzz or sense of "laying" in the ears; vestibulotoksičnost′-coordination of movements, unsteady gait, dizziness.
From the digestive tract: nausea, vomiting, anorexia, thirst, hepatotoxicity in violation of the functional parameters of the liver (especially against liver disease history).
Allergic reactions: macular-papular rash, itch, erythema, fever.
Cardio-vascular system and blood (hematopoiesis, hemostasis): arrhythmia (due to electrolyte imbalance), leukocytosis, leukopenia, eozinofilija (5%), thrombocytopenia.
Other: electrolyte imbalance, incl. kaliopenia, hypocalcemia, gipomagniemiya; myalgia; soreness, the infiltration, the development of sterile abscesses or increased bleeding at the injection site.
Cooperation.
Vancomycin and cisplatin increases the probability of general relativity- and nephrotoxic action. Incompatible with drugs, have ototoksicheskoe (aminoglikozidy, Polymyxin, furosemid, ethacrynic acid) and nephrotoxic (aminoglikozidy, Polymyxin, metoksifluran) effect and cause neuromuscular blockade (aminoglikozidy, Polymyxin, diethyl ether, and halogenated hydrocarbons inhalation anesthesia, citrate blood preservatives). Muscle-relaxant effect is weakened neostigmine.
Overdose.
Symptoms: impairment of renal function, up to acute tubular necrosis (the risk increases in the elderly, against the background of the original renal dysfunction, Dehydration), damage hearing and vestibular divisions VIII cranial nerves, neuromuscular blockade until the cessation of breathing (especially with the rapid on / in), electrolyte imbalance (kaliopenia, hypocalcemia, gipomagniemiya).
Treatment: takes into account the possibility of an overdose of multiple drugs and their interaction, the appointment of activated carbon, gastric lavage, simptomaticheskaya therapy: maintenance of respiration and blood circulation, gidratatsiya, providing urine outflow at the level of 3-5 mL/kg/h (normal renal function); for the relief of neuromuscular blockade, incl. respiratory depression and apnea — introduction antiholinesteraznah funds, calcium supplements, hemodialysis (especially in patients with severely impaired renal function); requires monitoring of fluid and electrolyte balance and creatinine clearance.
Dosing and Administration.
Only parenterally: / m (deep in the muscle) or / drip (during 60 m). For the / m 1 g previously dissolved in 2 ml 0,9% sodium chloride solution or sterile water for injection; the on/in infusion throw in 100 ml 0,9% sodium chloride solution. The usual dose is 1 g 1 once a day, daily for 60-120 days, then 2-3 times a week for 12-24 months, in combination with other anti-TB drugs. The maximum daily dose is not more than 20 mg / kg. Against the background of renal dysfunction: if Cl creatinine less than 110, 100, 80 and 60 mL/min-on 13,9; 12,7; 10,4 and 8,16 mg/kg, respectively, every 24 no, less 50 and 40 mL/min-on 7,01 and 5,87 mg / kg every 24 or h 14,0 and 11,7 mg / kg every 48 h, respectively, less 30, 20 and 10 mL/min-on 4,72; 3,58 and 2,43 mg / kg every 24 or h 9,45; 7,16 and 4,87 mg / kg every 48 no, either on 14,2; 10,7 and 7,3 mg / kg every 72 h, respectively; if Cl creatinine, equal 0, - By 1,29 mg / kg every 24 or h 2,58 mg / kg every 48 no, or 3,87 mg / kg every 72 no.
Precautions.
The appointment may after determining the sensitivity of strain. Before and during treatment, it is necessary to periodically audiometriu (1-2 times a week) to diagnose hearing loss at high frequencies, the determination of indicators of vestibular function, kidney (weekly) and the liver, the level of potassium in the blood serum (monthly). During and after a surgical procedure to use caution against a backdrop of funds, causing neuromuscular blockade (especially at high likelihood of incomplete termination of neuromuscular blockade in the postoperative period). During treatment should continuously monitor mode and dosing schema, the correctness and regularity of appointments. In case of injection missed dose administered as soon as possible, only if the time has not come the introduction next dose; double dose. In the absence of improvement status within 2-3 weeks or when new symptoms requires a specialist's consultation.
