Characterization of antimicrobial drugs for the treatment of uncomplicated acute cystitis

Relevant, effective, timely therapy of any IMP leads to a significantly higher frequency of symptomatic and bacteriological treatment and better prevention of reinfection. Unfortunately, treatment can lead to resistance to antibiotics to comment pathogens and bacteria and have harmful effects on the intestinal flora and vaginas, so it is very important to consult a physician immediately and choose it properly.

Clinical recommendations for the treatment of uncomplicated acute cystitis

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

the nature of the resistance of the uropatogens; Sensitivity of urepatogenic bacteria to antimicrobial drugs; Possibility of side effects of antimicrobial drugs.  

In terms of empathy, two important facts are recorded in this leadership:

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

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

phosphomycin; nitrofurantine.

The following selection criteria were used: pharmacokinetics, interaction, the probability of shock (the probability that microorganism is susceptible to antibiotics), resistance development, specific use for IMP, effectiveness, side effects, dose frequency, duration of treatment, cost.  

The study included the following drugs: Amoxicillin (with or without clavulanic acid), nitrofurantine, sulfametol, trimopry, co-trimoxazole, ciprofloxacin, norfloxacin, offloxacin and trometamol phosphomycin.

Characterization of the first row of treatment of lower urinary tract infections

Table 1. The first line for the treatment of cystitis

 

Substance	Dose	Treatment duration
Trometamol phosphomycin	3 g a single dose	A single dose (once)
Nitrofurantine	50-100 mg four times a day	5-7 days

 

Trometamol phosphomycin

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

Active substance: phosphomycin. Form of release: Granules for the preparation of the solution, in packaging 1 or 2 packages, dosage of phosphomycin 3 g/bag, 2 g/bag.

Refers to the clinical and farmacological group in uroantisipica, antibiotics (phosphonic acid derivatives).  

Spectrum of action

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

Staphylococcus (staphylococcus spp. );   Enterococci (Enterococcus spp. );   Haemophilus spp; Most Gram-negative intestinal bacteria, including 95. 5% E. coli, producing β-lactamases of expanded spectrum (BLRS); E. coli soles producing metals-β-lactamase sensitive to phosphomycin; Citrobacter spp. ;   Enterobacter spp. ; Klebsiella spp. , Klebsiella pneumoniae;   Morganella Morganii;   Proteus mirabilis;   Pseudomonas spp. ;   Serratia spp.  

The feature of the drug

Trometamol phosphomycin is exclusively prescribed for the treatment of uncomplicated acute cystitis in the form of a single dose of 3 g and not prescribed for pyelonephritis.   Absorbed best if you take it before you eat.   Reaches a high concentration in the urine and holds a high level for more than 24 hours.

In some studies, the clinical and microbiological effectiveness of phosphomycin with other antimicrobial first row with uncomplicated cystitis was compared. The clinical efficiency of a dose (3 g) of phosphomycin is 91% (cure occurs in 91% of patients). The indicator is comparable to nitrofurantoine (93%), trimetrome-sulfametoxazole (93%) and fluoroquinolones (90%) in uncomplicated acute cystitis.  

Advantages of treatment with phosphomycin

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

Phosphomycin significantly causes fewer negative reactions, which is most important - including in pregnant women. An additional benefit is to treat highly -resistant microorganisms. Some in Vitro studies demonstrated that phosphomycin is active in relation to Vancico resistance aureus staphylococcus aureus and Gram-negative sticks producing BLR.   Effective in the treatment of IMP caused by K. pneumoniae. Enterobacteriaceae that produces carbapenemase (in doses of 3 g, repeat every 48–72 hours).   It has a minimal side effect on the body. This is indicated by the high frequency of E. coli sensitivity in regions with frequent use of phosphomycin with uncomplicated cystitis in women; The comfort of a single dose way.

Indications

acute cystitis (bacterial origin); repetitive cystitis irritation (bacterial origin); urethritis (non -specific bacterial); Bacteriuria of asymptomatic pregnant women; IMP after operations; Prevention of IMP.

Dosage and method of application

 

Treatment of simple acute cystitis	Repeated/severe forms of IMP	Prevention of IMP
Adults - 3. 0 g (1 pack) once   Child (from 5 years old) - 2. 0 g once	Adults - 3. 0 g twice, the second reception after 24 hours	First technique: 3. 0 g 3 hours prior to operation/diagnostic procedure   Second trick: 3. 0 g 24 hours after starting

Recommendations for use

Follow all the instructions on the label.   Phosphomycin is usually prescribed only at one dose.   Do not take larger/smaller or longer quantities if not prescribed by a doctor. Can be used at the same time/after eating. Phosphomycin is a powder medicine, before using it must be diluted with water. Do not take dry powder without adding water. Spread a bag with 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 provide a full dose. Do not mix with hot water. Good good to get it overnight. There will be a longer rest between urination, which will provide a longer presence of the bladder medicine and a more effective effect. Store at room temperature away from moisture and heat in the original packaging.

Other guidelines:

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 recommended to consult a physician to make sure that phosphomycin is an antibiotic suitable for treatment. Moreover, urine analysis may be required before and after taking this medicine.

Contraindications:

Children under 5; allergic reactions to ingredients; Severe kidney failure.

General side effects:

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

Interaction

Simultaneous intake with meteclopramide is not recommended to avoid weakening phosphomycin action.

Thus, the comfort of a single dose regimen, in vitro activity in conjunction with gram -resistant sticks that cause simple and immature, uncomplicated cystitis,  And the minimum tendency for side damage makes phosphomycin a useful choice in the treatment of low MVP infections (cystitis, urethritis).

Nitrofurantine 

Active substance: nitrofurantine. Issuing Form: tablets, dose 100 mg, 50 mg.

It refers to the clinical and farmacological group to urraniteptics, antimicrobies.  

Nitrofurantine, in connection with the group of synthetic nitrofurans, was originally introduced in the form of a form of microcrystalline. In 1967, the form of macrochristaline with improved gastrointestinal tolerance became available.  

Currently, there are two main types of nitrofurantin: a macrochristaline form and a mixture of microcrystalline and macrochristaline forms (25 mg macrocrystals plus 75 mg monohydrate). Mixed species in the patented double distribution system in the Russian Federation are not registered and are not in circulation.  

The mechanism of action

Nitrofurantin bacterial mechanisms include several sites:

ribosomal transmission inhibition;   bacterial DNA damage; Intervention in Cherbs Cycle.  

Nitrofurantin is active in connection with:  

More than 90% of the intestinal strains that cause IMP; Enterococcus, including resistance to vanCromycin; Klebsiella spp. ;   Proteus spp. ; Staphylococci (golden and saprophytic) are usually sensitive.

Resistance to the medicine is rare, perhaps because of numerous areas of the medicine. However, proteus, serratia and pseudomonas have natural resistance to nitrofurantoine.  

Nitrofurantino can also be an additional option for antimicrobial treatment of uncomplicated acute cystitis caused by bacteria producing BLR.

Pharmacokinetics.  Inhalation improves when you eat. The concentrations of nitrofurantine in the serum are low or are not determined 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 to patients with pronounced renal failure (creatinine cleaning<60 m/min), but studies observed high efficiency of medicine in patients with creatinine cleaning of 60-30 ml/min.  

Safe for use in pregnant women and children.

Indications:  Treatment and prevention of cystitis (bacterial origin).

Dose.  It is described by an individually based urologist based on the severity of the state, the duration and the severity of the symptoms.  

Common dose for adults with cystitis:

From 50 to 100 mg oral 4 times daily for 1 week or at least 3 days after urine sterility arrives. Common dose for adults to prevent cystitis: From 50 to 100 mg orally once daily before bedtime. Children's Dosage for Cystitis Treatment: 1 month and older: 5-7 mg/kg/day (up to 400 mg/day) orally in 4 doses. Ordinary Dosage of Children for Cystitis Prevention: 1 month and older: from 1 to 2 mg/kg/day (up to 100 mg/day) orally to 1-2 expectations.

Most experts agree with the recommendation of a 5-day course of medicine for the treatment of uncomplicated acute cystitis. Studies showed the frequency of early clinical cure with nitrofurantoine from 79% to 95% and the frequency of microbiological cure from 79 to 92%. In the aggregate of the clinical effectiveness study, they indicate the overall equivalence between nitrofurantoin, prescribed for 5 or 7 days, and trimetrome-sulfametoxazole (beads), ciprofloxacin and a single dose of trometamol (monural) phosphomycin. However, the speed of the microbiological cure has consistently demonstrated a slightly more favorable effect on comparison medicines.

Recommendations for patients

It is necessary to follow all the recipes and instructions of the doctor in the medicine instructions.   Do not use in large or smaller quantities or longer than recommended. It is better to get nitrofurantine with food (bio -inductance increases). It is recommended to observe the reception throughout the specified period. Symptoms may pass earlier, but treatment may not stop while the infection is completely eliminated. Doses can increase the risk of further developing antibiotic -resistant infection and the risk of relap.   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:

diarrhea with water or bloody; Sudden pain or discomfort in the chest, whistling breathing, dry cough; difficulty breathing; Fever, chills, pain in the body, fatigue, unexplained weight loss; numbness, tingling or pain in the hands or feet; Liver problems - nausea, pain in the upper stomach, itching, feeling fatigue, loss of appetite, dark urine, clay excrement, jaundice (skin or eye);   Lupid -like syndrome - joint pain or fever edema, swollen glands, muscle aches, chest pain, vomiting, thoughts or unusual behavior, polluted redness.

Serious side effects can be more likely in the elderly, long -term or weakened people.

Contraindications:  

serious disorder of kidney excretion function;   kidney failure;   Oliguria; Failure of glucose-6-phosphate dehydrogenase; pregnancy; age up to 1 month; allergic reactions to ingredients; Phases XN II-III;   cirrhosis;   Chronic hepatitis;   Acute porphyria;   Lactation.

Pregnancy

Category of pregnancy medicine: in (according to FDA - US Health Agency). It is believed that this drug will not harm an unborn baby in the early stages of pregnancy. In the last 2-4 weeks of pregnancy, it is contraindicated.

Nitrofurantine is able to penetrate the breast milk, during lactation is not described.

Special instructions

The risk of peripheral neuropathy increases in the presence of anemia, diabetes mellitus, severe Mon, electrolyte balance violations, lack of group B vitamins. Nitrofurantine is not used for the treatment of prostate, cortical kidney substance lesions, purulent paranefritis. With pyelonephritis, they are not described because of inefficiency. Nitrofurantine can give unusual results with certain laboratory glucose (sugar) in the urine.

Interaction

With fluoroquinolons is incompatible. Antacids based on triliic acid magnesium, nastyx while receiving antimicrobial activity of nitrofurantine. The secretion of the canal that blocks the channel secretion is not prescribed, as they increase the toxicity of nitrofurantine (blood content increases), reduce bactericidal properties (urine content decreases).

Nitrofurantine is considered the therapeutic drug of the first row in the uncomplicated acute cystitis due to:  

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