According to the radar, “Sulperazone” is an antibiotic from the class of the third generation of cephalosporins. The tool has the ability to inhibit beta-lactamase. The medication is made in the form of a solution intended for injective administration. The effect of the application is due to two main components: cefoperazone, sulbactam.
Basic information
As the manufacturer explains, Sulperazone is effective against microorganisms, as it inhibits the reproduction process. The drug can be prescribed only if the pathological microflora is sensitive to the active compounds of the drug. Under the influence of active substances, the biological reaction of generating the mucopeptide necessary for building the cell microbial wall is inhibited.
Studies have shown that sulbactam does not have a pronounced antibacterial effect. An exceptional case is infection with the neisseria and acinobacter. This substance is included in the composition of the drug due to its ability to irreversibly inhibit beta-lactamase. Efficiency is observed relative to the overwhelming majority of these compounds produced by microscopic life forms. Due to the ability to produce this compound, certain antibiotics are not harmful to bacteria, while sulbactam can minimize this resistance. Sulbactam may react with proteins capable of binding penicillin. Due to this, the combination of sulbactam with cefoperazone gives a more pronounced effect in comparison with the independent use of only cefoperazone.
When is it shown?
Consisting of sulbactam and cefoperazone “Sulperazone” is a medication effective against all forms of microflora for which cefoperazone is dangerous. The medicinal composition is more effective than the drug program, which involves the use of its components separately, approximately four times. Synergism is observed in the case of infection with a wide range of microbes, and is especially pronounced with the invasion of hemophilic bacillus, bacteroids, enterobacteria, Eicheria, Proteus, Klebsiella, Morganella, and some staphylococci.
In the instructions for use of Sulperazone, the manufacturer indicates that the substance is effective against invasion of gram-positive pathological life forms. You can prescribe a drug if a person has more pathologies associated with staphylococci that can generate penicillinase, and also do not have such quality. You can prescribe a remedy for infection with beta-hemolytic streptococci, enterococci. Studies have shown the effectiveness of drugs against a wide range of gram-negative bacteria. The medication is prescribed for infection with anaerobic gram-negative rods, cocci of various types, gram-positive rods. The effectiveness of Sulperazone injections in case of invasion of clostridia, lactobacilli has been proven.
Kinetic Nuances
When using Sulperazone powder for the preparation of an injectively injected solution, one can expect to achieve the maximum content in blood serum just five minutes after the injection. The drug is injected into a vein. When using two grams of the composition (components in equal amounts), the average concentration five minutes after the procedure was 13.2 μg / ml for sulbactam and 236.8 μg / ml for the second ingredient. Sulbactam has a greater distribution volume. For him, the indicator is estimated at 18-27.6 liters, while for the second substance - no more than 11.3 liters. Both active ingredients are able to penetrate into organs, organic tissues. They are detected in bile, skin, reproductive system, appendix.
According to the instructions, sulbactam present in "Sulperazone" is eliminated by 84% by the kidneys. For the second ingredient, this indicator does not exceed a quarter of the substance received in the body. Residues are predominantly eliminated via bile excretion pathways. The half-life of sulbactam reaches an hour, for cefoperazone it varies about 1.7 hours. There was no significant correction of kinetic parameters during repeated use of the composition. If you pause between injections for 8-12 hours, the cumulative effect does not appear.
Special occasion
In the instructions for Sulperazone, the manufacturer indicates that cefoperazone is predominantly eliminated by bile. If obstruction of the bile excretion ducts is established, if there are liver diseases, the average half-life of this component increases three times, sometimes four. In mild forms of violation, the term doubles relative to the standard. In addition, if there are health problems of these organs, the percentage of the substance excreted by the kidneys increases.
In the instructions, you can see the results of studies conducted with the use of "Sulperazone" in renal failure. A strong dependence on the clearance of sulbactam and creatine was found. With the terminal form of renal failure, the elimination half-life of sulbactam is significantly longer - some studies show a duration of almost ten hours. A significant change in the half-life indicator is possible due to blood dialysis. At the same time, the procedure affects the ability of a substance to be distributed throughout the body. Regarding cefoperazone with kidney problems, no significant kinetic changes were found.
Therapy and age
As studies have shown, the use of Sulperazone by people of advanced age is associated with an increase in half-life and a decrease in clearance of both components. Changes in the kinetics of sulbactam depend on renal impairment, and cefoperazone on hepatic.
Experiments were conducted to determine how much kinetics changes when children use the composition. Relative to adult patients, no fundamental differences were found, on average, the half-life of sulbactam did not exceed one and a half hours, and cefoperazone - two.
When is it shown?
You can use "Sulperazone" for sinusitis and other infectious diseases of the respiratory system, localized in different areas. The drug is prescribed for infection of the urinary system, for blood poisoning and meningitis. Indications for injection will be joint, bone, skin infections, soft tissue infections and localized in the abdominal cavity. They resort to medication in case of peritonitis, cholangitis. “Sulperazone” also helps with adnexitis. The substance is used if the inflammatory focus is localized in the pelvis. The drug is prescribed for gonorrhea, other genital infections. It can be used as part of a course to combat endometritis.
How to apply?
Adult patients per day are recommended to use from two to four grams of the drug. This volume should be divided into two equal portions. Between introductions stand strictly 12 hours. With refractory infection, a severe course of the disease, it is allowed to increase the daily dosage to 8 g. The drug is administered in equal parts for two procedures with a twelve-hour break. It is categorically not recommended to use more than eight grams per day.
With a creatinine clearance of 15-30 ml / min, the medication can be used with a dosage of up to two grams every 12 hours, for a day do not prescribe more than 4 g. With a lower creatinine clearance, a single dose is a gram, the interval between administrations is 12 hours, and more cannot be prescribed for a day two grams. In severe cases of an infectious disease, the doctor may recommend additional administration of cefoperazone.
Due to blood dialysis, the half-life of the drug slightly decreases, therefore, it is recommended to administer the drug after such a procedure.
Dosage details
According to reviews, Sulperazone is often prescribed for children. The doctor selects the optimal dose of medication based on the weight of the patient. When calculating the daily dose, it is necessary to take 40-80 mg of medication for each kilogram of the patient's mass. The resulting dosage is divided into two portions, administered at twelve-hour intervals. If the pathology is difficult, refractory infection is established, it is allowed to increase the dose to 150 mg per kilogram of weight. The resulting volume is intended for a day, it is administered in 2-4 procedures, between which maintain equal time intervals.
If the medication is prescribed for a newborn whose age does not exceed a week, the medicine must be administered once every 12 hours. As can be seen from the reviews, “Sulperazone” is not prescribed for children in an amount greater than 160 mg / kg per day.
Undesirable consequences
In the instructions for use of Sulperazone, the manufacturer lists which possible side effects are associated with the use of the medication. Tests have shown that some vomit and feel sick, there is colitis and disturbed stool. There is a risk of an allergic reaction and a decrease in the concentration of neutrophils. With prolonged use of the drug, neutropenia is possible, but the condition is reversible. Hemoglobin concentration, hematocrit level are reduced. Some were diagnosed with leukemia, thrombocytosis, and eosinophilia.
Patients taking Sulperazone complained of pain in the injection. During the course, headache and dizziness, there is a likelihood of vasculitis and changes in the activity of liver enzymes. With the introduction of the drug into a vein at the point of catheter placement, there is a chance of phlebitis formation. A medication can provoke anaphylactic shock.
Is it possible or not?
According to the instructions to “Sulperazone”, in the process of therapy with this drug, you can not use medicines to which increased susceptibility is established. The tool is prohibited in case of an allergic reaction not only to its components, but also to any beta-lactam compounds, cephalosporins, penicillins. If you use "Sulperazone" in the form of a solution, among the components of which there is lidocaine, a blockade inside the heart becomes a contraindication. Injection is allowed only if the patient has a pacemaker. It is forbidden to use the described drug with insufficient functioning of the heart in severe form.
During childbearing and breastfeeding, according to the instructions for use of Sulperazone (analogues, however, are mainly used with the same restriction), the medication is administered only when the obvious benefit significantly exceeds the danger to the fetus. The doctor must familiarize the woman with all the dangers and risks associated with the use of the composition.
Safety comes first
The instructions for Sulperazone and other drugs belonging to the cephalosporin class indicate that the use of beta-lactam medications in some patients provoked a severe response from the body, indicating an increased sensitivity. There is a chance of an anaphylactic response that provokes a fatal outcome. There is a greater risk of a similar situation if the patient has previously had hypersensitivity reactions. If allergy symptoms are observed, it is necessary to immediately cancel the composition and prescribe a suitable therapy to the patient to correct the condition.
If the anaphylactic response is severe, adrenaline is indicated. In some cases, you need to use oxygen, steroid drugs. Doctors should provide the patient with the opportunity to breathe. In some cases, intubation is required.
With severe obstruction of the bile ducts, severe liver diseases, severe impaired renal function, a dosage dosage adjustment is possible. If the patient has impaired liver and kidney function, it is necessary to prescribe Sulperazone only if there are resources to regularly check the concentration of active compounds in the blood serum so that the doctor can determine the need for a dose change in time. If it is not possible to constantly check blood plasma, you can not use cefoperazone more than 2 g per day.
Application features
Like some analogues of Sulperazone, also belonging to the category of antibiotics, the drug in question can cause a lack of vitamin K. This is quite rare. Doctors suggest that vitamin deficiency is associated with the inability of microflora to function normally - normally the microorganisms living in the intestinal tract produce the compound. The risk of vitamin deficiency is increased if a person eats poorly, if malabsorption syndrome is detected, if the patient receives food directly into a vein for a long time.
Prolonged use of Sulperazone and analogs in tablets can cause bacteria that are not sensitive to antibiotics. In order to minimize the risk of such a phenomenon, to fix it in time, it is necessary to closely monitor the patient's condition during the treatment period. With prolonged use of antibiotics, they regularly check how effectively the internal organs work. Particular attention is paid to the liver, kidneys, blood-forming organs. Higher danger for newborns, infants, children born prematurely.
Many or few?
There is a risk of overdose when used by patients and some analogues in tablets, and "Sulperazone". Information about an overdose regarding the medication in question is rather scarce. Excessive intake is known to increase the likelihood of side effects. An increase in the concentration in the fluid of the spinal cord can cause neurological failures, and the risk of convulsions increases.
If an overdose is observed, symptomatic treatment is indicated. The medication can be withdrawn by blood dialysis. Presumably, in case of impaired renal, hepatic functionality, it is by this method that it is best to remove the drug from the body.
Alternatives
The analogues of Sulperazone in the modern pharmaceutical market are:
- "Sulcef."
- Sulperaceph.
- Sulcephazone.
There is a drug “Cefoperazone and Sulbactam Spencer” on sale, it contains the same active components as the substance discussed above. Sometimes the doctor advises taking a closer look at the analogues of Sulperazone, which are, as follows from the composition described in the instructions for use, the Sulzoncef and Bakperazon medicines. A good reputation is the drug "Cefpar SV".
In some cases, the doctor may recommend Augmentin as an alternative. This antibiotic is based on other active compounds and is available in tablet form. As a rule, they resort to it as an alternative if the disease is localized in the respiratory system. The drug was manufactured using amoxicillin, an increase in the effectiveness of which is ensured by the inclusion of clavulanic acid in the composition, which minimizes microflora resistance to the main component.
Whatever drug the doctor prescribes from the above, replacing it with an analogue of Sulperazone alone is unacceptable and unreasonable. If it is not possible to purchase a medicine, you need to come for a second consultation, where the doctor will select an effective medication for a particular case. The choice is based on the diagnosis, indications and contraindications, the characteristics of the patient's body.
Synonyms for "Sulperazon": "Sulcef"
This medicine belongs to the third generation of semi-synthetic cephalosporins. A distinctive feature is the combined composition. The medication is on sale by a powder intended for the preparation of a solution. One ampoule contains: sulbactam, cefoperazone. The good effectiveness of "Sulcef" in the fight against negative, positive grams by the study of microorganisms is proved. You can treat infection with anaerobes, aerobes. Sulbactam, which is present in the composition of the drug, does not give a pronounced antibacterial effect, but provides inhibition of beta-lactamase, due to which many microorganisms are resistant to antibiotics. "Sulcef" shows a positive effect in the treatment of all invasions of microbes, which cefoperazone is dangerous.
The analogue of "Sulperazone" "Sulcef" is prescribed for diseases of the respiratory system. The drug is used in the fight against pneumonia, they treat bronchitis and pleural empyema, pulmonary abscess. The drug is effective for cystitis, pyelonephritis, gonorrhea and some other infectious diseases of the urinary and reproductive systems. You can use the composition for peritonitis, cholangitis, cholecystitis. , -. , . , , . «» , .
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Features of use
If the drug is supposed to be injected into a vein, the powder must be diluted with five percent dextrose solution, sodium chloride (concentration 0.9%) or specialized purified water. The drug is advised to be administered in drops. The duration of the procedure is up to half an hour. The drug is injected into muscle tissue within three minutes. For this use, the powder is dissolved in water for injection.
Hazards and Risks
The use of medicines is always associated with the risk of adverse reactions. As noted by persons who were prescribed "Sulperazone" or "Sulcef," to one degree or another, side effects bothered almost any patient. Some complained of pain at the injection site, while others noted headaches that became more frequent during the course. Someone was dizzy, while others had an upset stool. According to the instructions for the analogue of “Sulperazone”, to minimize side effects, the doctor may recommend additional funds (for example, pre-, probiotics), as well as the easiest version of the therapeutic course in terms of dosage and duration. Patients who developed severe enough adverse reactions noted that the doctor recommended switching to an alternative medication. The replacement is selected based on the diagnosis.