Cypromycin Uses, Dosage, Side Effects, FAQ - DrugFAQ (2023)

cypromycin

Cypromycin is a synthetic derivative of 4-quinolones with bactericidal activity against a wide spectrum of gram-positive and gram-negative organisms. It is active against most gram-negative aerobic bacteria, including Enterobacteriaceae and Pseudomonas aeruginosa. Cypromycin is also active against aerobic gram-positive bacteria, including penicillinase-producing, penicillinase-producing, and methicillin-resistant staphylococci. However, many strains of strep are relatively resistant to the drug. The bactericidal activity of cypromycin results from its interaction with the enzyme DNA gyrase, necessary for the synthesis of bacterial DNA. The mode of action of cypromycin differs from other antibiotics such as penicillins, cephalosporins, aminoglycosides, tetracyclines and therefore organisms resistant to these antibiotics are observed to be sensitive to cypromycin. After oral administration, cypromycin is well absorbed from the gastrointestinal tract and widely distributed in tissues and body fluids. The half-life of cypromycin is 3.5 to 4.5 hours. Approximately 30-50% of an oral dose of cypromycin is excreted in the urine within 24 hours as unchanged drug and active metabolites.

Cypromycin Drops (Eye/Throat) (Cypromycin Hydrochloride Ophthalmic Solution) is a sterile, multidose, synthetic antimicrobial agent for topical use. Cypromycin is a fluoroquinolone antibiotic active against a broad spectrum of gram-positive and gram-negative ocular pathogens. It is available as the monohydrate salt of 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-3-quinolinecarboxylic acid monohydrochloride. It is a pale yellow to light yellow crystalline powder with a molecular weight of 385.8. Its molecular formula is C17H18FN3O3.HCl.H2O.

Cypromycin is a second-generation fluoroquinolone active against many gram-negative and gram-positive bacteria. It works by inhibiting bacterial DNA gyrase and topoisomerase IV. Cypromycin binds to bacterial DNA gyrase with an affinity 100 times greater than that of mammalian DNA gyrase. There is no cross-resistance between fluoroquinolones and other classes of antibiotics, so it may have clinical value when other antibiotics are no longer effective. Ciprofloxain and its derivatives are also being studied for their effects against malaria, cancer, and AIDS.

Used

Cypromycin is used to treat the following infections caused by susceptible bacteria:

Serious systemic infections: e.g. Sepsis, bacteremia, peritonitis, infections in immunocompromised patients with hematological or solid tumors and in ICU patients with specific problems such as infected burns.

Respiratory infections: Lobar and bronchopneumonia, acute and chronic bronchitis and empyema.

Urinary tract infections: uncomplicated and complicated urethritis, cystitis, pyelonephritis, prostatitis and epididymitis.

Skin and soft tissue infections: infected ulcers, wound infections, abscesses, cellulitis, external otitis, erysipelas, and infected burns.

Gastrointestinal infections: enteric fever, infectious diarrhea.

Biliary tract infections: cholangitis, cholecystitis, vesicular empyema.

Intra-abdominal infections: peritonitis, intra-abdominal abscesses.

Bone and joint infections: osteomyelitis, septic arthritis.

Pelvic infections: salpingitis, endometritis, pelvic inflammatory disease.

Eye, ear, nose and throat infections: otitis media, sinusitis, mastoiditis, tonsillitis.

Gonorrhea: Gonorrhea of ​​the urethra, rectum, and pharynx caused by beta-lactamase-producing organisms or organisms moderately sensitive to penicillin.

Cypromycin Solution (Eye/Ear) is used to treat infections caused by susceptible strains of specified microorganisms under the conditions listed below:

Ojo

Hornhautgeschwüre:

• Pseudomonas aeruginosa

• Serrated platforms

• Staphylococcus aureus

• Staphylococcus epidermidis

• Streptococcus-pneumonia

• Streptococcus (Viridans Group)

conjunctivitis:

• hemophilic flu

• Staphylococcus aureus

• Staphylococcus epidermidis

• Steotococos neumonia

Ohr

External otitis, acute otitis media, purulent chronic otitis media. Prophylaxis in ear operations such as mastoid operations.

Cypromycin is also used in the concomitant treatment of the following conditions: Acute otitis externa Acute otitis externa caused by Pseudomonas aeruginosa Acute otitis media Acute sinusitis Uncomplicated pyelonephritis Acute exacerbation of chronic bronchitis caused by Moraxella catarrhalis Infections of bones and joints Intracomplicated chronic otitis media - abdominal infections, complicated urinary tract infection, conjunctivitis caused by Haemophilus influenzae, conjunctivitis caused by Staphylococcus epidermidis, corneal ulcers caused by Serratia marcescens, corneal ulcers caused by Staphylococcus aureus, corneal ulcers caused by Staphylococcus epidermidis, corneal ulcers caused by Streptococcus pneumoniae, corneal ulcers ulcers caused by Streptococcus pneumoniae Group Streptococcus viridans, corneal ulcers caused by Pseudomonas aeruginosa, Escherichia urinary tract infection, external ear infection NOS , fever and neutropenia, inf. outer ear infection caused by susceptible bacteria, infectious diarrhea, lower or lower respiratory tract infection caused by Enterobacter cloacae, lower respiratory tract infection caused by Escherichia coli, lower respiratory tract infection caused by Haemophilus influenzae, lower respiratory tract infection caused by by Haemophilus parainfluenzae, lower respiratory tract infection caused by Klebsiella pneumoniae, lower respiratory tract infection caused by Proteus mirabilis, lower respiratory tract infection caused by penicillin-sensitive Streptococcus pneumoniae, nosocomial pneumonia, otitis media (OM), otitis media, suppurative plague caused by Yersinia pestis, skin infections, typhoid fever caused by Salmonella typhi, urinary tract infections caused by Citrobacter diversus, urinary tract infections caused by Citrobacter frendii, urinary tract infections caused by Entercococcus faecalis, inf urinary infections caused by Enterobacter cloacae, urinary infections caused by Klebsiella pneumoniae, urinary infections caused by Morganella morganii, urinary infections caused by Proteus mirabilis, urinary infections caused by Providencia rettgeri, urinary infections caused by Pseudomonas aeruginosa, urinary infections caused by Serratia marcescens, infections urinary infections caused by methicillin-sensitive Staphylococcus epidermidis, uncomplicated urinary tract infections, acute otitis externa caused by Staphylococcus aureus, acute uncomplicated cystitis caused by Escherichia coli, acute uncomplicated cystitis caused by Staphylococcus saprophyticus, chronic prostatitis caused by Escherichia coli, chronic prostatitis caused by Proteus mirabilis, complicated pyelonephritis caused by Escherichia coli, complicated urinary tract infection caused by Escherichia coli, inhaled anthrax caused by Bacillus anthracis, noncomp gonorrhea licada caused by Neisseria gonorrhoeae

How does cypromycin work?

Cypromycin acts on bacterial topoisomerase II (DNA gyrase) and topoisomerase IV Targeting of cypromycin to the alpha subunits of DNA gyrase prevents it from overcoiling around bacterial DNA, thus preventing DNA replication.

cypromycin

Structure

Dose

cypromycin dose

Adult dose:

For oral dosage and suspension:

Urinary tract infection: Acute without complications: 250 mg twice daily for 3 days; Mild/Moderate: 250 mg twice a day for 7 to 14 days; Severe/complicated: 500 mg twice daily for 7 to 14 days; Chronic bacterial prostitis: 500 mg twice daily for 28 days; Lower Respiratory Tract Infections: Mild/Moderate: 500 mg twice daily for 7-14 days, Severe/Complicated: 750 mg twice daily for 7-14 days; Acute sinusitis: 500 mg twice a day for 10 days; Infection of the skin and skin structures: Mild/moderate: 500 mg twice daily for 7 to 14 days Severe/complicated: 750 mg twice daily for 7 to 14 days Bone and joint infection: Mild/moderate 500 mg twice daily for 4 to 6 weeks, Severe/Complicated: 750 mg twice daily for 4 to 6 weeks Intra-abdominal infection: 500 mg twice daily for 7 to 14 days Infectious Diarrhea: Mild/Moderate/Severe: 500 mg twice daily for 5 to 7 days Typhoid fever: 500 mg twice daily for 10 days Cervical and urethral gonococcal infections: Single: 250 mg single dose.

For IV infusion:

Urinary tract infection: mild to moderate: 200 mg every 12 hours for 7 to 14 days; Serious or complicated: 400 mg every 12 hours for 7-14 days; Lower respiratory tract infections: mild to moderate: 400 mg every 12 hours for 7 to 14 days; Serious or complicated: 400 mg every 8 hours for 7-14 days; Nosocomial pneumonia: mild/moderate/severe: 400 mg every 8 hours for 10-14 days; Skin and Skin Texture: Mild to Moderate: 400 mg every 12 hours for 7 to 14 days; Serious or complicated: 400 mg every 8 hours for 7-14 days; Bone and joint infection: mild to moderate: 400 mg 12 every hour for more than 4 to 6 weeks; Severe/complicated: 400 mg every 8 hours for more than 4-6 weeks; Intra-abdominal (acute abdomen): Complicated: 400 mg 12 every hour for 7-14 days; Acute sinusitis: mild/moderate: 400 mg every 12 hours for 10 days. Chronic bacterial prostatitis: mild/moderate: 400 mg every 12 hours for 28 days.

Children and youth:

RTI and gastrointestinal infections: neonates - 15 mg/kg twice daily, children (1 month - 18 years) - 20 mg/kg (max. 750 mg) twice daily; UTI: neonates - 10 mg/kg twice daily, children (1 month - 18 years) - 10 mg/kg (max. 750 mg) twice daily; Pseudomonas lower respiratory tract infection in cystic fibrosis: Children (1 month to 18 years) - 20 mg/kg (max. 750 mg) twice daily; Anthrax (treatment and post-exposure prophylaxis): Children (1 month to 18 years) - 20 mg/kg (max. 750 mg) twice daily.

Use during pregnancy and lactation

Reproduction studies in rats and rabbits with parenteral and oral administration revealed no evidence of teratogenicity, impaired fertility, or impaired pre- or postnatal development. However, as with other quinolones, cypromycin has been shown to cause arthropathies in immature animals, so its use during pregnancy is not recommended. Studies in rats have shown that cypromycin is excreted in milk, therefore its administration to lactating mothers is not recommended.

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Corneal Ulcers: The recommended dosing schedule for treating corneal ulcers is 2 drops every 15 minutes for the first 6 hours, then 2 drops every 30 minutes for the remainder of the first day. On the second day, instill 2 drops in the affected eye every hour. From the third to the fourteenth day, put 2 drops in the affected eye every four hours. Treatment can be continued after 14 days if there is no corneal re-epithelialization.

Conjunctivitis: The recommended dosage regimen for the treatment of bacterial conjunctivitis is 1 or 2 drops every 2 hours while awake for 2 days and 1 or 2 drops every 4 hours while awake for the next 5 days.

Ohr

For all infections, initially 2-3 drops every 2-3 hours, reducing the frequency of instillation to control the infection. Treatment should be continued for at least 7 days.

Information for patients: Should be swallowed whole with plenty of liquid, can be taken with or without food. The preferred time of administration is two hours after a meal and patients should not take antacids within two hours of ingestion.

Instructions for use of granules for suspension.

All the contents of the package should be placed in a small glass with 2-3 teaspoons of water. No other liquids or foods should be used. The mixer should be shaken well and drunk immediately. The glass should be filled with water and drunk.

Instructions for reconstituting the suspension (60 ml)

Shake the bottle well to loosen the granules. Add 50ml (using the measuring cup provided) of cold boiled water to the dry granules in the bottle. Shake the vial vigorously until all the granules are in suspension.

Collateral damage

Cypromycin is generally well tolerated. Common side effects are: Gastrointestinal disorders: eg. Nausea, diarrhea, vomiting, dyspepsia, abdominal pain. CNS disorders: eg dizziness, headache, fatigue, confusion, seizures. Hypersensitivity reactions: eg. Rash, itching and possible systemic reactions. Other possible side effects are: joint pain, photosensitivity, transient increase in liver enzymes (especially in patients with a history of liver damage), serum bilirubin, urea, or serum creatinine. Arthralgia and myalgia may also occur.

The most commonly reported drug-related adverse reaction is localized burning or discomfort. In studies of corneal ulcer with frequent drug administration, white crystalline precipitates were observed in approximately 17% of patients. Other reactions that occurred in less than 10% of patients were eyelid margin crusting, crystals/dandruff, foreign body sensation, itching, conjunctival hyperemia, and bad taste after instillation. Other events that occurred in less than 1% of patients included corneal discoloration, keratopathy/keratitis, allergic reaction, eyelid edema, tearing, photophobia, corneal infiltrates, nausea, and decreased vision.

toxicity

Nausea, vomiting, abdominal pain, crystalluria, nephrotoxicity, and oliguria may occur in patients with overdose. An overdose of cypromycin often leads to acute renal failure. Overdose may progress over the next 6 days with increased serum creatinine and BUN and anuria. Patients may require prednisone therapy, urgent hemodialysis, or supportive care. Depending on the degree of overdose, patients may recover normal renal function or progress to chronic renal failure.

The oral LD50 in rats is >2000 mg/kg.

Cypromycin for intratympanic injection or otic use has low systemic absorption and therefore does not present a risk during pregnancy or lactation. Animal studies generally do not harm the fetus, but high doses may cause gastrointestinal upset in the mother, which may increase the frequency of miscarriages. In human studies, there was no increase in fetal malformations above baseline rates. The risk and benefit of ciprofloxacin during pregnancy and lactation must be weighed.

2/8 of the in vitro tests and 0/3 of the in vivo tests for the mutagenicity of ciprofloxacin were positive.

Oral doses of 200 and 300 times the maximum recommended clinical dose in rats and mice did not show carcinogenicity or tumorigenicity.

Oral doses above the maximum recommended clinical dose have not been shown to affect fertility in rats.

Careful

Cypromycin should be used with caution in patients with a history of seizures. Crystalluria has been observed rarely in association with the use of cypromycin. Patients receiving cypromycin should be well hydrated to avoid excessive alkalinity of the urine.

Beuflox injection should only be given as a slow intravenous infusion over a period of 60 minutes. Local reactions at the intravenous site have been reported with intravenous administration of cypromycin. These reactions are more common when the infusion time is 30 minutes or less, or when small veins in the hands are used.

interaction

Elevated plasma theophylline levels have been observed after concomitant use with cypromycin. Cypromycin suspension should not be administered within 4 hours of administration of medicinal products containing magnesium, aluminium, calcium or iron salts, as absorption may be affected.

interaction with food

• Avoid milk and derivatives. Dairy products and juices fortified with calcium decrease the absorption of ciprofloxacin.
• Limit your caffeine intake.
• Take with or without food. Absorption is not significantly influenced by food.

[Moderate] ADJUST DOSING INTERVAL: Concomitant intake of dairy products (milk, yogurt) or calcium-fortified foods (eg, cereals, orange juice) may decrease the activity of certain oral fluoroquinolone antibiotics.

The mechanism is the chelation of calcium and quinolones, resulting in decreased bioavailability.

In the case of orange juice, the inhibition of intestinal transport mechanisms (P-glycoprotein or organic anion-transporting polypeptides) by flavones may also be involved.

One study reported a mean 41% reduction in peak plasma concentrations and a 38% reduction in AUC when ciprofloxacin was co-administered with calcium-fortified orange juice instead of water.

Administration of ciprofloxacin tablets with enteral nutrition may reduce bioavailability and peak serum concentrations.

The data were conflicting and varied depending on the type of enteral feeding product, the location of the feeding tube, and the characteristics of the patient.

When ciprofloxacin is administered through a jejunostomy tube, reduced absorption is expected.

DIRECTIONS: Orally administered ciprofloxacin should not be taken with dairy products or calcium-fortified foods, but may be taken with meals containing these products.

When taken alone, dairy products or calcium-fortified foods should be consumed at least 2 hours before or after ciprofloxacin administration.

When ciprofloxacin tablets are administered to patients receiving continuous enteral feedings, some experts recommend that tube feeding be discontinued at least 1 hour before and 2 hours after ciprofloxacin administration.

Patients should be monitored for changes in antimicrobial efficacy and switched to intravenous ciprofloxacin as appropriate.

If an enteral route other than a jejunostomy tube is not available, switching to intravenous ciprofloxacin is also recommended.

According to the manufacturer, due to its physical properties, ciprofloxacin oral suspension should not be administered by nasogastric tube or nasogastric tube.

Cypromycin-multivitamin interaction

[Moderate] ADJUST DOSING INTERVAL: Oral preparations containing magnesium, aluminum, or calcium may significantly decrease the gastrointestinal absorption of quinolone antibiotics.

Absorption may also be reduced by sucralfate, which contains aluminum as well as other polyvalent cations such as iron and zinc.

The mechanism is the chelation of quinolones by polyvalent cations, forming a complex that is poorly absorbed by the gastrointestinal tract.

When co-administered with Suprep Bowel Prep (Magnesium

Check individual product labels for specific recommendations.

Drug interaction with cypromycin

Moderate: Aspirin, Aspirin

Frequency not known: diphenhydramine, diphenhydramine, omega-3 polyunsaturated fatty acids, omega-3 polyunsaturated fatty acids, pregabalin, pregabalin, paracetamol, paracetamol, acetaminophen, paracetamol, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol, cetirizine, cetirizine

Cypromycin disease interaction

Major: colitis, CNS disorders, myasthenia gravis, peripheral neuropathy, QT prolongation, tendonitis

Moderate: crystalluria, diabetes, hemodialysis, renal dysfunction

volume of distribution

Cirpofloxacin follows a 3-compartment distribution pattern with a central compartment volume of 0.161 l/kg and a total volume of distribution of 2.00-3.04 l/kg.

elimination

A 250 mg oral dose of ciprofloxacin achieves a mean peak concentration of 0.94 mg/L in 0.81 hours with a mean area under the curve of 1.013 L/h*kg. The FDA claims an oral bioavailability of 70-80%, while other studies place it around 60%. A previous review of ciprofloxacin reported an oral bioavailability of 64-85%, but recommends 70% for all practical uses.

half life

The mean half-life after a 250 mg oral dose was 4.71 hours and 3.65 hours after a 100 mg intravenous dose. In general, the half-life is given as 4 hours.

reach

The mean renal clearance after a 250 mg oral dose is 5.08 ml/min*kg. After a 100 mg intravenous dose, the mean total body clearance is 9.62 mL/min*kg, the mean renal clearance is 4.42 mL/min*kg, and the mean non-renal clearance is 5.21. ml/min*kg.

elimination

27% of an oral dose was recovered unchanged in the urine compared to 46% of an intravenous dose. Collection of radiolabeled ciprofloxacin resulted in 45% recovery in urine and 62% in feces.

Use during pregnancy and lactation

Reproduction studies in rats and rabbits with parenteral and oral administration revealed no evidence of teratogenicity, impaired fertility, or impaired pre- or postnatal development. However, as with other quinolones, cypromycin has been shown to cause arthropathies in immature animals, so its use during pregnancy is not recommended. Studies in rats have shown that cypromycin is excreted in milk, therefore its administration to lactating mothers is not recommended.

contraindication

Cypromycin is contraindicated in patients who have demonstrated hypersensitivity to cypromycin or other quinolones.

acute overdose

In the event of an acute overdose, the patient should be carefully monitored and receive supportive care, including monitoring of renal function. Adequate hydration must be maintained.

Interactions with other medications

Co-administration of cypromycin with theophylline may result in increased theophylline plasma concentrations. Plasma theophylline levels should be monitored and the dose adjusted as necessary. Antacids containing magnesium hydroxide or aluminum hydroxide may affect the absorption of cypromycin and co-administration of these agents with cypromycin should be avoided. Probenecid interferes with renal tubular secretion of cypromycin and leads to increased serum levels of cypromycin. As with other broad-spectrum antibiotics, prolonged use of cypromycin may cause overgrowth of nonsusceptible organisms. Repeated assessment of the patient's condition and microbial susceptibility testing are essential. If superinfections occur during treatment, appropriate measures should be taken.

Storage conditions

Store in a cool, dry place, protected from light. Keep out of the reach of children.

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