Characterization of antimicrobial medications for the treatment of acute complications

Acute cystitis symptoms

The corresponding, effective and timely therapy of any IMP leads to a significantly higher frequency of symptomatic and bacteriological cure and better reinfection prevention. Unfortunately, treatment can lead to antibiotic resistance to pathogens and bacteria comments and have adverse effects on intestinal and vaginal flora, so it is very important to immediately consult a doctor and choose it correctly.

Clinical recommendations for the treatment of acute complications

The American Society of Infectious Disease Specialists (IDSA) in cooperation with the European Society of Infectious Microbiology and Diseases (ESCMID) has published clinical recommendations for treatment with cystitis and uncomplicated pyelonephritis in 2011. This document became an invaluable reference in the IMP office. This manual discusses important factors in choosing the ideal treatment:

  • the nature of the resistance of the uropathogens;
  • Sensitivity of urepatogenic bacteria to antimicrobial drugs;
  • The possibility of side effects of antimicrobial medications.  

As for sensitivity, two important facts are observed in this leadership:

  1. The stability of uropathogens to antibiotics has increased in recent years;  
  2. The nature of resistance demonstrates significant geographical variability between countries and even regions.  

Thus, recommendations review periodically due to the constant development of resistance, the development of new tools and the conduct of research showing the superiority and inefficiency of medicines. According to and recommendations and research, they are best met with the requirements for drugs for the treatment of uncomplicated cystitis, the following substances:

  • phosphomycin;
  • Nitrofurantina.

The following selection criteria were used: pharmacokinetics, interaction, probability of getting it right (the likelihood that the microorganism was sensitive to antibiotics), the development of resistance, specific use for imps, efficacy, side effects, dosage frequency, treatment duration, cost.  

The study included the following drugs: amoxicillin (with or without clavulanic acid), nitrofurantine, sulfametizole, trimtoprimo, co-rimoxazole, ciprofloxacin, norfloxacin, offloxacin and phosphomycin trometamol.

Characterization of the first line of treatment of inferior urinary tract infections

Table 1. First line for the treatment of cystitis

 

Substance Dosage The duration of treatment
Phosphomycin trometamol 3 G A single dose A single dose (once)
Nitrofurantine  50-100 mg four times a day 5-7 days

 

Phosphomycin trometamol

Phosphomycin was opened in 1969 as a representative of the new class of phospho antibiotics.  

Active substance: phosphomycin. Release Form: Granules for the preparation of the solution, in package 1 or 2 packages, fosphomycin dose 3 g/bag, 2 g/bag.

It refers to the clinical and agricultural group to Uroantiseptics, antibiotics (derived from phosphonic acid).  

Action spectrum

Phosphomycin has a bactericidal activity of a broad spectrum of action in relation to:

  • Staphylococci (Staphylococcus spp. );  
  • Enterococcci (Enterococcus spp. );  
  • Haemophilus spp;
  • Most intestinal gram-negative bacteria, including 95, 5% E. coli, producing expanded spectrum β-lactamoses (BLRS);
  • E. coli strains producing phosphomycin-sensitive metal-β-lactamase;
  • Citrobacter spp. ;  
  • Enterobacter spp. ;
  • Klebsiella spp. , Klebsiella Pneumoniae;  
  • Morganella Morganii;  
  • Proteus Mirabilis;  
  • Pseudomonas spp. ;  
  • Serratia spp.  

The peculiarity of the drug

  • Trometamol phosphomycin is prescribed exclusively for the treatment of non -complicated acute cystitis in the form of a single 3 g dose and not prescribed for pyelonephritis.  
  • It is better absorbed if you accept before eating.  
  • It reaches a high concentration in the urine and maintains a high level for over 24 hours.

In several studies, the clinical and microbiological efficacy of phosphomycin with other antimicrobials of the first line with uncomplicated cystitis has been compared. The clinical efficiency of a dose (3 g) of phosphomycin is 91% (cure occurs in 91% of patients). The indicator is comparable to nitrofurantoin (93%), trimetrome-sulfametoxazole (93%) and fluoroquinolones (90%) in non-complicated acute cystitis.  

Benefit Advantages with Phosphomycin

The microbiological level of cure phosphomycin (80%) is lower than that of comparable antibiotics at 88 to 94%. However, a recent meta -analysis of 27 studies did not disclose differences in the efficacy between phosphomycin and other antibiotics for cystitis treatment and discovered the following facts:

  • Phosphomycin significantly causes fewer adverse reactions, which is the most important - even in pregnant women.
  • An additional benefit is to treat multi -resistant microorganisms. Several in vitro studies have shown that phosphomycin is active in relation to the Vancico Staphylococcus aureus and BLRS producing blrs.  
  • Effective in the treatment of IMP caused by K. pneumoniae. Enterobacteriaceae producing carbapenemase (in 3 g doses, repeat every 48-72 hours).  
  • It has a minimal side effect on the body. This is indicated by the high frequency of E. coli susceptibility in regions with frequent use of phosphomycin with non -complicated cystitis in women;
  • Convenience of a single dose mode.

Nominations

  • Acute cystitis (bacterial origin);
  • Exacerbation of recurrent cystitis (bacterial origin);
  • urethritis (not bacterial specific);
  • Bacteriuria of asymptomatic pregnant women;
  • Imp after operations;
  • Prevention of imp.

Dosage and application method

 

Simple acute cystitis treatment Recurring/heavy forms of IMP Prevention
Adults - 3, 0 g (1 package)

 

Children (5 years) - 2, 0 g once

Adults - 3, 0 g twice, the second reception after 24 hours First technique: 3, 0 g 3 hours before the operation/diagnosis procedure

 

Second trick: 3, 0 g 24 hours after the primary

Recommendations for use

  • Follow all instructions on the label.  
  • Phosphomycin is usually prescribed only at a dose.  
  • Do not enjoy large/smaller quantities or more if not prescribed by a doctor.
  • It can be used simultaneously/after eating.
  • Phosphomycin is a medicine powder before using it should be diluted with water. Do not take dry powder without adding water.
  • Dissolve a bag of 1/2 cup of cold water, mix and drink immediately. You can add a little more water to the same glass, shake carefully and drink immediately to ensure a full dose.
  • Do not mix with hot water.
  • It's good to take it overnight. There will be a longer rupture between urination, which will ensure a longer presence of the medicine in the bladder and a more effective effect.
  • Store at room temperature away from moisture and heat in the original packaging.

Other instructions:

  • Symptoms cannot pass completely immediately, after 2-3 days;
  • It is necessary to contact a urologist if the symptoms do not disappear within 3 days after treatment, a fever or other new complaints will appear;
  • Before applying the patient, it is advisable to consult a doctor to ensure that phosphomycin is a suitable antibiotic for treatment. In addition, urine analysis may be required before and after taking this medicine.

Against -indications:

  • Children under 5;
  • allergic reactions to components;
  • Severe renal failure.

General Side Effects:

  • nausea, stomach disorder, light diarrhea;
  • headache, dizziness;
  • Itching or vaginal discharge (rarely).

Drug interaction

Simultaneous ingestion with meleclopramide is not recommended to avoid weakening phosphomycin.

Thus, the convenience of a single dose regime, in vitro activity in relation to gram -gram toughness that causes simple and immature cystitis and without complications, Like this,  And the minimum tendency of collateral damage makes phosphomycin a useful choice in the treatment of lower MVP infections (cystitis, urethritis).

Nitrofurantine 

Active substance: nitrofurantine. Release Form: Tablets, 100 mg dosage, 50 mg.

It refers to the clinical and agricultural group to Uroantiseptics, antimicrobials.  

Nitrofurantine, related to the group of synthetic nitrofuans, was originally presented in the form of a microcrystalline form. In 1967, the form of Macrocrystalline with improved gastrointestinal tolerance became available.  

Currently, there are two main types of nitrofurantine: a macrocrystalline form and a mixture of microcrystalline and macrocrystalline forms (25 mg of 75 mg macrocrystals of monohydrate). The mixed species in the patented double delivery system in the Russian Federation are not registered and are not in circulation.  

The mechanism of action

Nitrofurantine bacterial activity mechanisms include multiple sites:

  • inhibition of ribosomal transmission;  
  • damage to bacterial DNA;
  • CREBS intervention.  

Nitrofurantine is active in relation to:  

  • More than 90% of intestinal strains causing the impass;
  • Enterococcus, including vancomycin resistant;
  • Klebsiella spp. ;  
  • SPP Proteus. ;
  • Staphylococci (gold and saprophites) are usually susceptible.

Drug resistance is rare, probably due to various areas of the drug. However, Proteus, Serratia and Pseudomonas have natural resistance to nitrofurantoin.  

Nitropurantine can also be an additional option for oral antimicrobial treatment of acute complications caused by bacteria that produce BLRS.

Pharmacokinetics.  Absorption improves when eating. Nitrofurantine concentrations in serum are low or not defined in standard doses, the content of the prostate gland is not detected. It is mainly excreted with urine, where the concentration of the drug (from 50 to 250 mg/ml) easily exceeds 32 mg/ml MPC.  

Nitrofurantine should not be prescribed for patients with pronounced kidney failure (creatinine clearance<60 m/min), but studies observed high drug efficiency in patients with 60-30 ml/min creatinine clearance.  

Safe for use in women and pregnant children.

Indications:  Cystitis (bacterial origin) treatment and prevention.

Dosage.  It is prescribed by an individual urologist based on the severity of the state, duration and severity of symptoms.  

The usual dose for adults with cystitis:

  • 50 to 100 mg oral 4 times a day for 1 week or at least 3 days after the sterility of the urine. The usual dose for adults for cystitis prevention:
  • 50 to 100 mg orally once a day before bed. Child dosage for the treatment of cystitis:
  • 1 month or more: 5–7 mg/kg/day (up to 400 mg/day) orally at 4 doses. The usual dose of children for cystitis prevention:
  • 1 month or more: 1 to 2 mg/kg/day (up to 100 mg/day) orally in 1-2 receptions.

Most experts agree with the recommendation of a 5 -day drug course for the treatment of acute complications. Studies have shown the frequency of early clinical cure with nitrofurantoin from 79% to 95% and the frequency of microbiological cure from 79 to 92%. In the aggregate of the study of clinical efficacy, they indicate the overall equivalence between nitrofurantoin, prescribed for 5 or 7 days and trimetrome-sulfametoxazole (accounts), ciploxacin and a single dose of trometamol phosphomycin (monura). However, the speed of microbiological cure has constantly demonstrated a slightly more favorable effect for comparison drugs.

Recommendations for patients

  • It is necessary to follow all the prescriptions and instructions of the doctor in the instructions for the medicine.  
  • Do not use in large or smaller quantities or more than recommended.
  • It is best to take Nitrofurantina with food (increases bioavailability).
  • It is recommended to observe the reception throughout the prescribed period. Symptoms may pass earlier, but treatment cannot be interrupted while the infection is completely eliminated. Doses may increase the risk of additional development of antibiotic resistant infections and relapse risk.  
  • Nitrofurantine does not treat viral infections, for example, a cold or flu.

Side effect

General Side Effects:

  • headache, dizziness;
  • Gas formation, stomach disorder;
  • Light diarrhea;  
  • Itching or vaginal discharge.

Much less often found:

  • aqueous or bloody diarrhea;
  • Sudden pain or chest discomfort, whistling breathing, dry cough;
  • difficulty breathing;
  • fever, chills, body aches, fatigue, inexplicable weight loss;
  • Numbness, tingling or pain in the hands or legs;
  • Hepatic problems - nausea, pain in the upper stomach, itching, fatigue sensation, loss of appetite, dark urine, clay feces, jaundice (yellowing of the skin or eye);  
  • Lupid type syndrome - pain in the joints or edema with fever, swollen glands, muscle pain, chest pain, vomiting, unusual thoughts or behavior, spotted rashes.

Severe side effects may be more likely in elderly, long -term patients or weakened people.

Against -indications:  

  • severe disorders of the excretory function of the kidneys;  
  • renal failure;  
  • Oliguria;
  • Failure in glucose-6-phosphate dehydrogenase;
  • pregnancy;
  • age up to 1 month;
  • allergic reactions to components;
  • XN II-III Stages;  
  • cirrhosis;  
  • chronic hepatitis;  
  • acute porphyria;  
  • lactation.

Pregnancy Application

The category of the drug in relation to pregnancy: in (according to the US health agenda). It is believed that this medicine does not harm a unborn in the early stages of pregnancy. In the last 2-4 weeks of pregnancy, it is contraindicated.

Nitrofurantine is able to penetrate breast milk during lactation is not prescribed.

Special Instructions

  • The risk of peripheral neuropathy increases in the presence of anemia, diabetes mellitus, severe, violation of electrolytic balance, lack of group B vitamins.
  • Nitrofurantine is not used for the treatment of prostatitis, injuries of the cortical substance of the kidneys, purulent paranephritis. With pyelonephritis, they are not prescribed due to inefficiency.
  • Nitrofurantine can provide unusual results with certain laboratory glucose (sugar) in the urine.

Drug interaction

  • With fluoroquinolon is incompatible.
  • Trill -based antacids, nastyx acid, while taking antimicrobial activity of nitrofurantine.
  • Channel secretion that blocks channel secretion is not prescribed as it increases nitrofurantine toxicity (blood content increases), reduces bactericidal properties (urine content is reduced).

Nitrofurantine is considered the therapeutic remedy of the first line in acute complications without complications due to:  

  • the effectiveness of a 5 -day course;  
  • A small risk of side effects and damage to a person's normal flora;  
  • minimum bacteria resistance;
  • Effectiveness comparable to other antimicrobial drugs.