Polymyxin B
When ATH:
A07AA05
Pharmacological action
Antibiotics polypeptide structure. The mechanism of action is mainly due to the blockade of the permeability of the cytoplasmic membrane of bacterial cells, which leads to their destruction.
It is active against most Gram-negative bacteria: Escherichia coli, Enterobacter spp., Klebsiella spp., Haemophilus influenzae, Bordetella pertussis, Salmonella spp., Shigella spp.; especially active against Pseudomonas aeruginosa.
К полимиксину B также чувствителен Vibrio cholerae (за исключением Vibrio cholerae eltor), Merciless coccidioides, but basically mushrooms exhibit resistance to the antibiotic.
Usually resistant Serratia marcescens, Providencia spp., Bacteroides fragilis. Not active against Proteus spp., Neisseria spp., Obligate anaerobic and gram-positive bacteria.
It has a cross-resistance to colistin.
Pharmacokinetics
After the / m of Cmax plasma levels achieved after 2 no. It is widely distributed in the organs and tissues of the body. Repeated administration of possible cumulation. Do not cross the BBB. T1/2 is 6 no. Excreted in the urine.
Testimony
Infectious-inflammatory diseases, caused by susceptible pathogens to polymyxin B, incl. skin infections, ears, eye, GI infections.
Dosage regimen
It is used topically, I /, / m, intrathecal.
When the / m and in / in a daily dose of 1.5-2.5 mg / kg, when other routes of administration dosage is determined individually.
Side effect
From the central and peripheral nervous system: paresthesia, visual impairment, dizziness, ataxia, disturbance of consciousness, drowsiness; in predisposed patients – the development of neuromuscular blockade, respiratory paralysis and apnea.
From the urinary system: violation of renal excretory function, hematuria, proteinuria, tubular necrosis (at / in the introduction).
Allergic reactions: skin rash, itch.
Local reactions: irritation and pain at the injection site (when i / m administration), signs of meningeal irritation (intrathecal).
Contraindications
The perforation of the eardrum (topical), extensive skin lesions (for outdoor use), Hypersensitivity to polymyxin B.
Pregnancy and lactation
The use of polymyxin B when pregnancy is possible only in the case, when the intended benefits to the mother outweighs the potential risk to the fetus.
If necessary, use during lactation should decide the issue of termination of breastfeeding.
Cautions
With careful use of polymyxin B in renal impairment, and diseases, involving violation of neuromuscular transmission (incl. myasthenia). In such cases, the necessary correction mode and monitoring of renal function.
When parenteral application is needed to control the concentration of polymyxin B in plasma.
It can be used in combination with neomycin, bacitracin, Nystatin, trimethoprim.
Drug Interactions
In an application with the means for anesthesia, novokainamidom, muscle relaxants peripherally acting observed enhancement of neuromuscular blockade.
Synergistic effect with chloramphenicol, karbenicillinom, tetracycline, sulfonamides and trimethoprim against Pseudomonas aeruginosa, Proteus, Serratia; ampicillin – in their effect on gram-negative rods.
Compatible with bacitracin and nystatin.
Enhances GRT- and nephrotoxicity of aminoglycosides (kanamycin, streptomycin, neomycin, gentamicin), and caused the blockade of neuromuscular transmission.
It reduces the concentration of heparin in the blood (complexed).
Pharmaceutical incompatibility with the sodium salt of ampicillin, chloramphenicol, cephalosporin antibiotics, tetracycline, 0.9% sodium chloride solution, solutions of amino acids, geparina.