Tobramycin - instructions for use, dose, side effects, contraindications

Tobramycin is active against gram-negative bacteria: Escherichia coli, Proteus spp. (indole-positive and indole-negative strains), Klebsiella spp., Serratia spp., Providencia spp., Enterobacter spp., Shigella spp., Salmonella spp., Citrobacter spp., Haemophilus influenzae; Gram-positive bacteria: Staphylococcus spp. (including strains that produce penicillinase).

Pharmacokinetics:

Quickly absorbed after intramuscular injection. Virtually not absorbed from the digestive tract and does not bind to proteins (0-10%). It is well distributed in the organs and tissues of the body. It is not metabolized. The elimination half-life for normal kidney function is 2-3 hours. After intramuscular administration of tobramycin, peak plasma concentrations are achieved within 30-90 minutes (4 μg / ml after a dose of 1 mg / kg). Elimination by the kidneys - 93% in 24 hours mainly unchanged.

Indications:

For systemic use: severe infectious and inflammatory diseases caused by tobramycin-sensitive pathogens (sepsis, meningitis, peritonitis, endocarditis, respiratory tract infections, skin and soft tissue infections, urinary tract infections, bone tissue infections).

For topical application: eye infections (as part of combination therapy).

ICD-10

I.A30-A49.A40 Streptococcal septicemia

I.A30-A49.A41 Other septicemia

VI.G00-G09.G00 Bacterial meningitis, not elsewhere classified

VII.H10-H13.H10 Conjunctivitis

VII.H15-H22.H15.0 Sclerite

VII.H15-H22.H15.1 Episcleritis

VII.H15-H22.H16 Keratite

IX.I30-I52.I33 Acute and subacute endocarditis

X.J00-J06.J01 Acute Sinusitis

X.J00-J06.J02 Acute pharyngitis

X.J00-J06.J03 Acute tonsillitis

X.J00-J06.J04 Acute laryngitis and tracheitis

X.J10-J18.J15 Bacterial pneumonia, not elsewhere classified

X.J20-J22.J20 Acute bronchitis

X.J30-J39.J31 Chronic rhinitis, nasopharyngitis and pharyngitis

X.J30-J39.J32 Chronic Sinusitis

X.J30-J39.J35.0 Chronic tonsillitis

XII.L00-L08.L01 Impetigo

XII.L00-L08.L02 Abscess of skin, boil and carbuncle

XII.L00-L08.L03 Phlegmon

XII.L00-L08.L08.0 Pyoderma

XIII.M86-M90.M86 Osteomyelitis

XIV.N10-N16.N10 Acute tubulointerstitial nephritis

XIV.N10-N16.N11 Chronic tubulointerstitial nephritis

XIV.N30-N39.N30 Cystitis

XIV.N30-N39.N34 Urethritis and urethral syndrome

XIV.N40-N51.N41 Inflammatory diseases of the prostate

Contraindications:

Hypersensitivity, neuritis of the auditory nerve, severe chronic renal failure, pregnancy.

Carefully:

Elderly age, neuritis of the auditory nerve, renal failure, botulism, myasthenia gravis, parkinsonism, dehydration, breast-feeding.

Pregnancy and lactation:

The danger of complete irreversible deafness of the fetus. All aminoglycosides penetrate the placenta, sometimes accumulating in high concentrations in the cord blood and / or amniotic fluid. Aminoglycosides may be nephrotoxic to the fetus. Tobramycin concentrates in embryonic kidneys and can lead to complete irreversible bilateral deafness in the fetus. It is necessary to correlate the benefits and risks in cases when treatment is necessary for life-threatening conditions or serious diseases, if other methods of treatment can not be used or are not effective.

Recommendations FDA - category D.

Dosing and Administration:For the dosage form "eye drops:
infections with mild - 1 or 2 drops in the conjunctival sac every 4 hours;
infections with severe course - 2 drops into the conjunctival sac at an interval of one hour until the improvement is achieved, after which, before the drug is canceled, the dose should be gradually reduced.
Duration of treatment is 6-8 days.
For the ophthalmic ointment dosage form:
infection with mild course - a strip of ointment about 1.5 cm into the conjunctival sac 2-3 times a day;
acute infections with severe course - a strip of ointment of about 1.5 cm in the conjunctival sac every 3-4 hours, with a decrease in the frequency of application of the drug as the phenomena of inflammation decrease.
For the dosage form "capsules with powder for inhalation":
appoint adults and children of 112 mg (contents of 4 capsules) 2 times a day (morning and evening) for 28 days regardless of the patient's body weight.The interval between inhalations should be about 12 hours, but not less than 6 hours. After a 28-day course of therapy, a break in the use of the drug should be 28 days. It is necessary to strictly adhere to the above treatment regimen, alternating 28-day courses of therapy with 28-day intervals.
For the dosage form "inhalation solution":
inhalation for about 15 minutes, using a nebulizer, sitting or standing upright. Adults and children over 6 years of 300 mg twice a day for 28 days. The interval between administrations should be about 12 hours, but not less than 6 hours. After the completion of the course, take a break for 28 days and follow the next course as described above.
For the dosage form "solution for intravenous and intramuscular administration":
when administered intramuscularly - the contents of the bottle are dissolved in 3-5 ml of 0.5% solution of procaine or water for injection.
with intravenous administration - injected drip, before the introduction of diluted in 100-200 ml of 0.9% solution of sodium chloride or 5% solution of dextrose, injected for 20-60 minutes.
Single dose for adults and children over 1 year - 1 mg / kg body weight, daily - 3 mg / kg body weight; the maximum daily dose is 5 mg / kg body weight.
Children from 1 week to 1 year: 6-7.5 mg / kg per day, divided into 3-4 identical doses (2-2.5 mg / kg every 8 hours or 1.5-1.89 mg / kg every 6 hours).
Preterm or newborns before 1 week of age: up to 4 mg / kg per day, divided into 2 equal doses every 12 hours.
The usual duration of treatment is 7-10 days.

Side effects:

From the side CNS and peripheral nervous system: ototoxic effect, headache, lethargy, disorientation, violation of neuromuscular transmission.

From the side digestive system: nausea, vomiting, increased levels of hepatic transaminases and bilirubin in the blood.

From the side hematopoiesis system: anemia, granulocytopenia, thrombocytopenia.

Local reactions: pain at the injection site.

From the side metabolism: hypocalcemia, hyponatremia, hypokalemia, hypomagnesemia.

Other: possibly nephrotoxic action, allergic reactions.

Overdose:

Symptoms: toxic reactions (hearing loss, ataxia, dizziness, urination disorders, thirst, decreased appetite, nausea, vomiting, ringing or feeling of "stuffing" in the ears, nephronecrosis - increased urea concentration, hypercreatinemia, proteinuria, oliguria), respiratory muscle paralysis.

Treatment: patients with normal renal function are given a fluid infusion and forced diuresis; patients with impaired renal function - hemodialysis or peritoneal dialysis. With neuromuscular blockade - anticholinesterase funds, salts Ca2 +; when breathing is stopped - ventilation, other symptomatic and supportive therapy.

Interaction:

Tobramycin is incompatible with other drugs: since injection solutions have acidic pH values, they can be incompatible with alkaline drugs or drugs with variable pH.

Special instructions:

Aminoglycoside II generation, is active mainly against gram-negative microorganisms, including - Pseudomonas spp. (excluding resistant strains), Staphylococcus aureus.

Tobramycin in vitro is somewhat more active in relation to Pseudomonas aeruginosathan gentamicin, and less active in relation to Serratia, staphylococci and enterococci, but these differences may not be clinically significant.

Bacterial resistance to gentamicin and tobramycin is usually similar, but some strains of bacteria (≈10%) resistant to gentamicin retain sensitivity to tobramycin.

With systemic application it is effective in the treatment of severe or hospital infections caused by gram-negative microorganisms,in most cases - in combination with other antibacterial drugs.

Ophthalmic ointment and drops are effective in treating external eye infections.

When combined with tobramycin for inhalation with other inhaled medications, these drugs should be used before the first dose of tobramycin is given. Before tobramycin is used for inhalations, renal function should be examined by repeating the evaluation every 6 months.

A systematic review of the antibacterial strategy of eradication P. aeruginosa with cystic fibrosis. Treatment of peritonitis, including cirrhosis of the liver; hospital respiratory infections, including cystic fibrosis (including inhalation therapy); complicated urinary tract infections, osteomyelitis, severe infections of the skin and soft tissue, sepsis. Early eradication P. aeruginosa It is still possible to determine whether it is interconnected with positive clinical outcomes in patients with cystic fibrosis (insufficient statistical power of included CI, only microbiological outcomes were evaluated).

Instructions

Tobramycin (Tobramycinum)