Pharmacological action Vancocin HCl
Vancocin HCL Vancomycin is a tricyclic chromatographically purified glycopeptide antibiotics isolated from Amycolatopsis orientalis. The bactericidal action of vancomycin is shown in the inhibition of cell wall biosynthesis. In addition, vancomycin may alter the permeability of cell membranes of bacteria and alter RNA synthesis. Cross-resistance between vancomycin and other antibiotics classes available.
In vitro vancomycin usually is active against gram-positive organisms including: Staphylococcus aureus and Staphylococcus epidermidis (including heterogeneous methicillin-resistant strains), Streptococcus pyogenes, Streptococcus pneumoniae (including penicillin-resistant strains), Streptococcus agalactiae, viridans group, Streptococcus bovis and enterococci (eg, Enterococcusf aecalis); Clostridium difficile (eg, toxigenic strains are involved in the development of pseudomembranous enterocolitis), and diphtheroids. Other microorganisms that are sensitive to vancomycin in vitro, include Listeria monocytogenes, the bacteria genera Lactobacillus, Actinomyces, Clostridium and Bacillus.
There is evidence that in vitro some isolated strains of enterococci and staphylococci are resistant to vancomycin.
The combination of vancomycin and an aminoglycoside have synergistic in vitro against many strains of Staphylococcus aureus, Streptococcus Group D, not belonging to the enterococcus, enterococcal bacteria of Streptococcus (viridans group).
Vancomycin is not active in vitro against gram-negative bacilli, mycobacteria, and fungi.
Pharmacokinetics Vancocin HCl
In individuals with normal renal function, multiple in / in a 1 g of vancomycin (15 mg / kg) (infused over 60 min) produces average plasma concentration of 63 mg / l immediately after the infusion, 2 h after infusion, the average concentrations in plasma is about 23 mg / l, and at 11 h after infusion – about 8 mg / liter. Repeated infusions of 500 mg, administered over 30 minutes, creating average plasma concentration of about 49 mg / l after the infusion, 2 h after infusion the average plasma concentration is about 19 mg / l, and 6 hours – about 10 mg / l. Plasma concentrations at multiple doses are similar to concentrations in plasma after a single administration. T1 / 2 of vancomycin from plasma is 4-6 hours in patients with normal renal function.
About 75% of the administered dose of vancomycin is excreted in urine by glomerular filtration in the first 24 h. The average plasma clearance is about 0.058 L / kg / h and the average renal clearance is about 0.048 L / kg / h. The renal clearance of vancomycin is relatively constant and provides its excretion by 70-80%.
Vd ranges from 0.3 to 0.43 L / kg. The drug is practically not metabolized. As shown by ultrafiltration at vancomycin concentrations in serum of 10 mg / l to 100 mg / l, 55% of vancomycin found in protein-bound state. After I / administration of vancomycin hydrochloride is found in the pleural, pericardial, ascitic, synovial fluid and tissue in the ear of the atrium, as well as in urine and peritoneal fluid at concentrations that inhibit the growth of microorganisms. Vancomycin is slowly penetrates into the cerebrospinal fluid. When meningitis drug penetrates into the cerebrospinal fluid. Vancomycin crosses the placenta and into breast milk.
Renal dysfunction slows excretion of vancomycin. In patients with absent kidneys average T1 / 2 of 7.5 days. The total systemic and renal clearance of vancomycin may be reduced in elderly patients as a result of a natural slowing of glomerular filtration.
Dosage Vancocin HCl
In / infusion.
With the introduction of vancomycin recommended concentration is less than 5 mg / ml and the infusion rate of 10 mg / min. In patients who showed restriction of fluid can be applied to the concentration of 10 mg / ml and the rate of administration, not to exceed 10 mg / min. However, if such concentration increases the likelihood of side effects associated with the infusion.
Adults
The dose for patients with normal renal function is 2 g / in (500 mg every 6 hours or 1 g every 12 h). Each dose should be administered at a rate not greater than 10 mg / min or for at least 60 minutes. Age and obesity, the patient may require changes to the usual dose on the basis of determination of vancomycin concentrations in serum.
Children
The usual dose is 10 mg / kg and placed in / every 6 h. Each dose should be administered for at least 60 minutes.
Young children and infants
For infants starting dose is 15 mg / kg, followed by 10 mg / kg every 12 hours during the first week of life. Starting from the second week of life – every 8 hours until the age of 1 month. The drug should be administered for at least 60 minutes. Dosage regimens of vancomycin in neonates is shown in the following table.
This table can not be used to determine the dose in anuria. Such patients should be prescribed an initial dose of 15 mg / kg body weight for quick creation of therapeutic concentrations of drug in serum. The dose required to maintain stable drug concentrations, is 1.9 mg/kg/24 h. In patients with renal impairment is expedient to introduce maintenance doses of 250-1000 mg 1 time a few days. When anuria recommended dose of 1 g every 7-10 days.
Preparation of solutions for on / in a
Solution for injection is prepared immediately before drug administration. To do this in a bottle with dry, sterile vancomycin powder added to the required volume of water for injection to obtain a solution with a concentration of 50 mg / ml, further dilution of the prepared solution. Prepared before the introduction of vancomycin solutions will be further dilution to a concentration of not more than 5 mg / ml. The required dose of vancomycin diluted in the above manner, it should be administered by a fractional / infusion for at least 60 minutes. The solvents can be used 5% dextrose injection or 0.9% sodium chloride for injection. Before the introduction of the prepared solution should be checked visually for the presence of mechanical impurities and discoloration.
Preparation of oral solution
Vancomycin may be administered orally for the treatment of pseudomembranous colitis caused by C. difficile, due to the use of antibiotics, as well as for the treatment of staphylococcal enterocolitis. / V infusion of vancomycin has no advantages for the treatment of these diseases. Vancomycin is not effective when administered in the case of other types of infections. The appropriate dose may be prepared in 30 ml of water and allow the patient to drink it or entering through a tube. To improve the taste of the solution to it can be added to the usual food syrups.
Overdose Vancocin HCl
Treatment: corrective therapy aimed at maintaining the glomerular filtration rate. Vancomycin poorly removed by dialysis. There is evidence that hemofiltration and hemoperfusion through polysulfone ion exchange leads to increased clearance of vancomycin.
Drug Interactions Vancocin HCl
At the same time / in the introduction of vancomycin and anesthetic agents were observed erythema, histamine flushing and anaphylactoid reactions, can reduce blood pressure or risk of neuromuscular blockade. The introduction of vancomycin as a 60-minute infusion before administration of anesthetic can reduce the likelihood of these reactions.
At the same time and / or sequential systemic or topical administration of other potentially ototoxic and / or nephrotoxic drugs (aminoglycosides, amphotericin B, aspirin or other salicylates, bacitracin, capreomycin, carmustine, paromomycin, cyclosporine, loop diuretics, polymyxin B, cisplatin, ethacrynic acid ) requires a thorough control over the possible development of symptoms of ototoxicity (tinnitus, vertigo and hearing loss) and nephrotoxicity (increase in serum creatinine and blood urea, hematuria, proteinuria, rash, eosinophilia, and eozinofiluriya).
Kolestiramin reduces the activity.
Antihistamines meklozin, phenothiazines, thioxanthenes may mask the symptoms of Valium vancomycin (tinnitus, vertigo and hearing loss).
Incompatibility
Vancomycin solution has a low pH, which can cause physical or chemical instability when mixed with other solutions.
It should not be mixed with alkaline solutions.
Solutions Vankotsina and beta-lactam antibiotics are physically incompatible when mixed. The likelihood of precipitation increases with the concentration of vancomycin. Must be well rinsed in / data system between uses of antibiotics. In addition, it is recommended to reduce the concentration of vancomycin to 5 mg / ml or less.
Pregnancy and lactation Vancocin HCl
Safety of vancomycin in the application of a human pregnancy has not been investigated.
Evaluation of the results of experimental studies in animals revealed no direct or indirect adverse effect of vancomycin on the embryo or fetus, pregnancy, and peri-and postnatal development. Vancomycin should be administered to pregnant women only if the expected benefit to the mother outweighs the potential risk to the fetus.
If necessary, the drug while breastfeeding, you should stop feeding at the time of treatment.
Side effects Vancocin HCl
Allergic reactions: anaphylactoid reaction, hypersensitivity reactions.
With the cardiovascular system: cardiac arrest, flushing, lowering blood pressure, shock (these symptoms are mainly related to rapid infusion of the drug).
Part of the digestive system: nausea, pseudomembranous colitis.
With the hematopoietic system: agranulocytosis, eosinophilia, neutropenia, and thrombocytopenia.
Urinary tract: interstitial nephritis, renal function tests, modified, impaired renal function.
For the skin: exfoliative dermatitis, benign (IgA) dermatosis vesicular, itchy dermatitis, rashes, symptoms of “red man” Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria, vasculitis.
From the senses: ototoxic effects. A number of patients treated with vancomycin were observed symptoms such as ototoxicity, tinnitus, vertigo and hearing loss. They may be transient or permanent wear. The majority of cases observed in patients receiving excessive doses of vancomycin, with a history of hearing loss or in patients receiving concurrent treatment with other drugs with potential ototoxicity, such as aminoglycosides.
Other: chills, drug fever, tissue necrosis at injection site, pain at injection site, thrombophlebitis.
During or soon after rapid infusion of vancomycin too patients may develop anaphylactoid reactions. Rapid infusion may also cause the syndrome of “red man” (reddening of the upper body or pain and muscle spasm of the chest and back). After cessation of infusion reactions usually pass these within 20 minutes, but sometimes can last up to several hours.
Statement Vancocin HCl
- Endocarditis. Vankotsin effective as monotherapy and in combination with an aminoglycoside for the treatment of endocarditis caused by Streptococcus viridans or Streptococcus bovis.Pri endocarditis caused by enterococci (eg, E. faecalis), vankotsin effective only in combination with aminoglycosides.
There is evidence that effective treatment Vankotsin diphtheroid endocarditis. Vankotsin successfully used in combination with rifampin, an aminoglycoside, or with both antibiotics at an early endocarditis, caused Streptococcus epidermidis, or Streptococcus diphtheroids, after prosthetic valve. In some cases Vankotsin indicated for the prevention of endocarditis.
- Sepsis;
- Bone and joint infections;
- Infections of the lower respiratory tract;
- Infections of skin and soft tissues;
- Pseudomembranous colitis (as oral solution).
Vancomycin may also be used for infections caused by gram-positive microorganisms in cases of allergy to penicillin, intolerance or lack of response to treatment with other antibiotics, including penicillins and cephalosporins, as well as infections caused by pathogens susceptible to vancomycin, but resistant to other antimicrobial agents.
Contraindications Vancocin HCl
- Neuritis of the auditory nerve;
- Set sensitivity to vancomycin.
Sostorozhnostyu: with hearing loss (including history), renal insufficiency and in patients with allergies to teicoplanin because have reported cases of cross-allergy.
Cautions Vancocin HCl
The rapid introduction (for example, within a few minutes), vancomycin may be accompanied by a marked reduction of blood pressure and, in rare cases, cardiac arrest. Vancomycin should be administered in a diluted solution for at least 60 minutes to avoid adverse reactions associated with infusion.
Patients receiving vancomycin / O, should be periodically conducted blood tests and monitoring of renal function.
Vancomycin should be used with caution in patients with renal insufficiency because high and persisting for a long time drug concentration in blood may increase the risk of toxic manifestations of the drug. For patients with renal insufficiency the dose of vancomycin should be selected individually.
Vancomycin is an irritant, and so getting the drug in the tissue adjacent to the vessel may cause their death. Thrombophlebitis may be observed, although the likelihood of their development can be reduced by slow injection of a low concentration (2.5-5 g / l) and alternating injection sites.
