Cypromycin: uses, side effects, interactions, dosage / pill trip (2023)

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Cypromycin 2 mg/ml solution for infusion is indicated for the treatment of the following infections. Particular attention should be paid to the available information on cypromycin resistance before initiating therapy.

Official guidelines on the appropriate use of antibacterial agents should be considered.

Adult

- Lower respiratory tract infections caused by gram-negative bacteria

- Exacerbations of chronic obstructive pulmonary disease

- bronchopulmonary infections in cystic fibrosis or bronchiectasis

- Lung infection

- Chronic purulent otitis media

- Acute exacerbation of chronic sinusitis, especially when caused by gram-negative bacteria

- urinary tract infection

- Infections of the genital tract

- Epididymo-orchitis, including cases due toNeisseria gonorrhoeae

- pelvic inflammatory disease, including cases due toNeisseria gonorrhoeae

- Infections of the gastrointestinal tract (e.g. traveler's diarrhoea)

- Intra-abdominal infections

- Skin and soft tissue infections caused by gram-negative bacteria

- Malignant otitis externa

- Bone and joint infections.

- Inhalational anthrax (post-exposure prophylaxis and curative treatment)

Cypromycin can be used to treat neutropenic patients with fever thought to be caused by a bacterial infection.

children and young people

- Bronchopulmonary infections in cystic fibrosis caused byPseudomonas aeruginosa

- Complicated urinary tract infections and pyelonephritis

- Inhalational anthrax (post-exposure prophylaxis and curative treatment)

Cypromycin can also be used to treat severe infections in children and adolescents if needed.

Treatment should only be initiated by physicians experienced in the management of cystic fibrosis and/or severe infections in children and adolescents.

dosage

The dosage depends on the indication, severity and location of the infection, sensitivity of the pathogen to cypromycin, the kidney function of the patient and, in children and adolescents, the body weight.

The duration of treatment depends on the severity of the disease and the clinical and bacteriological course.

After initiation of intravenous therapy, treatment may be switched to oral tablet or suspension therapy if clinically indicated, at the discretion of the physician. Intravenous treatment should be continued orally as soon as possible.

In severe cases or when the patient is unable to take tablets (e.g. in patients on enteral nutrition), it is recommended to start treatment with intravenous cypromycin until a switch to oral administration is possible.

Treatment of infections caused by certain bacteria (eg.Pseudomonas aeruginosa,AcinetobacterÖstaphylococci) may require higher doses of cypromycin and concomitant administration with other appropriate antibacterial agents.

Treatment of some infections (eg, pelvic inflammatory disease, intra-abdominal infections, infections in neutropenic patients, and bone and joint infections) may require concomitant administration with other appropriate antibacterial agents, depending on the pathogen involved.

Adult

pediatric population

elderly patients

Elderly patients should receive a dose selected according to the severity of the infection and the patient's creatinine clearance.

Patients with impaired kidney and liver function.

Recommended starting and maintenance dose for patients with renal impairment:

No dose adjustment is required in patients with hepatic impairment.

Dosing in children with renal and/or hepatic impairment has not been studied.

method of administration

Cypromycin should be inspected visually prior to use. It should not be used if cloudy.

Cypromycin should be administered as an intravenous infusion. In children, the infusion time is 60 minutes.

In adult patients, the infusion time is 60 minutes for cypromycin 400 mg and 30 minutes for cypromycin 200 mg. A slow infusion into a large vein minimizes patient discomfort and reduces the risk of venous irritation.

The infusion solution can be infused directly or mixed with other compatible infusion solutions.

-

- Simultaneous administration of cypromycin and tizanidine.

Severe infections and mixed infections with gram-positive and anaerobic pathogens

Cypromycin monotherapy is not suitable for the treatment of severe infections and infections that can be caused by gram-positive or anaerobic pathogens. In such infections, cypromycin should be administered together with other appropriate antibacterial agents.

Streptococcal infections (including Streptococcus pneumoniae)

Cypromycin is not recommended for the treatment of streptococcal infections due to insufficient efficacy.

Genital tract infections

Orchiepididymitis and pelvic inflammatory disease can be caused by resistance to fluoroquinolones.Neisseria gonorrhoeae. In epididymitis-orchiditis and pelvic inflammatory disease, empiric cypromycin should only be considered in combination with another appropriate antibacterial agent (eg, a cephalosporin) unless cypromycin-resistant Neisseria gonorrhoeae can be excluded. If clinical improvement is not achieved after 3 days of treatment, the therapy should be reconsidered.

urinary tract infection

Fluoroquinolone ResistanceEscherichia coli- the most common causative agent of urinary tract infections - varies in the European Union. Prescribers are advised to consider the local prevalence of resistanceEscherichia coliand the fluoroquinolones.

intra-abdominal infections

There is limited data on the efficacy of cypromycin in the treatment of postoperative intra-abdominal infections.

Travel diarrhea

When choosing cypromycin, information on cypromycin resistance in relevant pathogens in the countries visited should be considered.

Bone and joint infections

Depending on the results of microbiological documentation, cypromycin should be used in combination with other antimicrobial agents.

Anthrax when inhaled

Human use is based onin-vitroAnimal sensitivity and experimental data, together with limited human data. Treating physicians should consult national and/or international consensus documents on anthrax management.

pediatric population

The use of cypromycin in children and adolescents should follow available official guidelines. Cypromycin treatment should only be initiated by physicians experienced in the treatment of cystic fibrosis and/or severe infections in children and adolescents.

Cypromycin has been shown to cause arthropathy in the weight-bearing joints of immature animals. Safety data from a randomised, double-blind study of cypromycin use in children (cypromycin: n=335, mean age=6.3 years; comparators: n=349, mean age=6.2 years; age range=1 to 17 years) showed an incidence suspected drug-related arthropathy (as distinct from joint-related clinical signs and symptoms) on day +42 of 7.2% and 4.6%, respectively. The incidence of drug-related arthropathy at 1-year follow-up was 9.0% and 5.7%, respectively. The increase in suspected cases of drug-related arthropathy over time was not statistically significant between groups. Due to possible adverse events related to the joints and/or surrounding tissues, treatment should only be initiated after careful benefit/risk assessment.

Bronchopulmonary infections in cystic fibrosis

Clinical trials included children and adolescents aged 5 to 17 years. There is more limited experience in treating children aged 1 to 5 years.

Complicated urinary tract infections and pyelonephritis

Treatment with cypromycin for urinary tract infections should be considered when other treatments cannot be used and should be based on the results of microbiological documentation.

Clinical studies included children and adolescents aged 1 to 17 years.

Other specific serious infections

Other serious infections according to official guidelines or after careful benefit-risk assessment, when other treatments cannot be used, or after failure of conventional therapy and when microbiological documentation can justify the use of cypromycin.

The use of cypromycin in specific serious infections other than those mentioned above has not been evaluated in clinical trials and clinical experience is limited. Therefore, caution should be exercised when treating patients with these infections.

hypersensitivity

Hypersensitivity and allergic reactions, including anaphylaxis and anaphylactoid reactions, can occur after a single dose and can be fatal. If such a reaction occurs, cypromycin should be discontinued and appropriate medical treatment sought.

musculoskeletal system

Cypromycin should generally not be used in patients with tendon disorders or a history of disorders associated with quinolone therapy. However, in very rare cases, after microbiological documentation of the pathogen and evaluation of the risk/benefit ratio, these patients may be prescribed cypromycin for the treatment of certain serious infections, particularly when standard treatment has failed or a bacterial infection has occurred. . Resistance when microbiological data can justify the use of cypromycin.

With cypromycin, tendinitis and tendon ruptures (particularly Achilles tendon) can also occur during the first 48 hours of treatment, sometimes bilaterally. Inflammation and tendon rupture can occur up to several months after stopping treatment with cypromycin. The risk of tendinopathy may increase in elderly patients or in patients treated concomitantly with corticosteroids.

Cypromycin should be discontinued at any sign of tendinitis (eg, painful swelling, inflammation). Care must be taken to keep the affected limb at rest.

Cypromycin should be used with caution in patients with myasthenia gravis.

sensitivity to light

Cypromycin has been shown to cause photosensitivity reactions. Patients taking cypromycin should be instructed to avoid exposure to direct sunlight or ultraviolet radiation during treatment.

Central nervesystem

Cypromycin, like other quinolones, is known to trigger seizures or lower the seizure threshold. Cases of status epilepticus have been reported. Cypromycin should be used with caution in patients with CNS disorders that may predispose them to seizures. If seizures occur, cypromycin should be discontinued. Psychiatric reactions can occur even after the first dose of cipromycin. In rare cases, depression or psychosis can lead to suicidal thoughts/thoughts, culminating in a suicide attempt or completed suicide. If such cases occur, administration of cypromycin should be discontinued.

Cases of polyneuropathy (based on neurological symptoms such as pain, burning sensation, sensory disturbances or muscle weakness, alone or in combination) have been reported in patients receiving cypromycin. Cypromycin should be discontinued in patients with symptoms of neuropathy including pain, burning, tingling, numbness and/or weakness to prevent the development of an irreversible condition.

heart diseases

Use of fluoroquinolones, including cypromycin, in patients with known risk factors for QT prolongation, such as e.g.:

- Congenital long QT syndrome

- Concomitant use of drugs that prolong the QT interval (e.g. class IA and III antiarrhythmics, tricyclic antidepressants, macrolides, antipsychotics)

- Uncorrected electrolyte imbalance (eg, hypokalemia, hypomagnesemia)

- Cardiac disorders (e.g. heart failure, myocardial infarction, bradycardia)

Elderly patients and women may be more sensitive to drugs that prolong the QTc interval.

Therefore, caution should be exercised when using fluoroquinolones, including cypromycin, in these populations.

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hypoglycemia

As with other quinolones, hypoglycaemia has been reported more frequently in diabetics, particularly in the elderly. Careful monitoring of blood sugar is recommended for all diabetics.

gastrointestinal system

The occurrence of severe and persistent diarrhea during or after treatment (including several weeks after treatment) may indicate antibiotic-associated colitis (life-threatening with a possible fatal outcome) that requires immediate treatment. In such cases, cypromycin should be discontinued immediately and appropriate therapy instituted. Antiperistaltic drugs are contraindicated in this situation.

renal and urinary systems

Cypromycin-related crystalluria has been reported. Patients receiving cypromycin should be well hydrated and excessive urinary alkalinity should be avoided.

renal insufficiency

sistema hepatobiliar

Cases of life-threatening hepatic necrosis and liver failure have been reported with cypromycin. If signs and symptoms of liver disease (such as anorexia, jaundice, dark urine, itching or abdominal pain) appear, treatment should be discontinued.

Glucose-6-Phosphat-Dehydrogenase-Mangel

Haemolytic reactions have been reported in patients with glucose-6-phosphate dehydrogenase deficiency receiving cypromycin. Cypromycin should be avoided in these patients unless the potential benefit outweighs the potential risk. In this case, the possible occurrence of haemolysis must be controlled.

Resistance

Bacteria resistant to cypromycin can be isolated during or after treatment with cypromycin, with or without clinically evident superinfection. With longer treatment times and when treating nosocomial infections and/or infections caused by cypromycin, there may be a particular risk of selecting for cypromycin-resistant bacteriastaphylococcijPseudomonasSpecies.

Cytochrom P450

Cypromycin inhibits CYP1A2 and may therefore cause an increase in serum concentrations of concomitant substances metabolised by this enzyme (e.g. theophylline, clozapine, olanzapine, ropinirole, tizanidine, duloxetine, agomelatine). Simultaneous use of cypromycin and tizanidine is contraindicated. Therefore, patients taking these substances concomitantly with cypromycin should be carefully monitored for clinical signs of overdose and serum concentrations (e.g. theophylline) may need to be determined.

methotrexate

Concomitant use of cypromycin with methotrexate is not recommended.

Interacting with tests

Isin-vitroActivity of cypromycin againstmycobacterial tuberculosismay cause false negative results in bacteriological testing of samples from patients currently taking cypromycin.

Injection site reaction

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. These can appear as local skin reactions that quickly disappear at the end of the infusion. Subsequent intravenous administration is not contraindicated unless reactions recur or worsen.

charge NaCl

In patients for whom sodium intake is a medical problem (patients with congestive heart failure, renal insufficiency, nephrotic syndrome, etc.), the additional sodium load should be taken into account (for sodium chloride content, see section 2).

visual disturbances

If vision deteriorates or effects on the eyes occur, an ophthalmologist should be consulted immediately.

The most commonly reported adverse drug reactions (ADRs) are nausea and diarrhea, vomiting, transient increases in transaminases, rash, and injection and infusion site reactions.

Adverse reactions from clinical studies and post-marketing surveillance with cypromycin (oral, intravenous and sequential therapy) are listed below by frequency category. The frequency analysis considers data from oral and intravenous administration of cypromycin.

The following side effects have a higher frequency category in subgroups of patients receiving intravenous or sequential (intravenous to oral) treatment:

pediatric population

The incidence of arthropathy mentioned above relates to data collected from studies in adults. Arthropathies have been reported to be common in children.

Notification of Suspected Side Effects

It is important to report suspected adverse drug reactions after approval. Allows continuous monitoring of the benefit-risk balance of the drug. Healthcare professionals are asked to report any suspected side effects via: Yellow Card Scheme - website: www.mhra.gov.uk/yellowcard.

An overdose of 12g has been reported to produce mild symptoms of toxicity. Acute overdose of 16 g has been reported to cause acute renal failure.

Overdose symptoms include dizziness, tremors, headache, fatigue, seizures, hallucinations, confusion, abdominal discomfort, kidney and liver failure, and crystalluria and hematuria. Reversible renal toxicity has been reported.

In addition to the usual emergency measures, e.g. ventricular emptying followed by medicinal charcoal, it is recommended that renal function, including urinary pH, be monitored and acidified as necessary to prevent crystalluria. Patients must remain well hydrated. Theoretically, antacids containing calcium or magnesium could reduce the absorption of cypromycin in overdose.

Only a small amount of cypromycin (<10%) is removed by hemodialysis or peritoneal dialysis.

In case of overdose, symptomatic treatment should be carried out. Because of the possibility of QT prolongation, ECG monitoring should be performed.

Pharmacotherapeutic group: fluoroquinolones, ATC code: J01MA02

mechanism of action

As a fluoroquinolone antibacterial agent, cypromycin's bactericidal activity results from inhibition of topoisomerase type II (DNA gyrase) and topoisomerase IV, which are required for replication, transcription, repair and recombination of bacterial DNA.

Pharmacokinetic/pharmacodynamic relationship

Efficacy depends mainly on the ratio of peak serum concentration (C_maximal) and the minimum inhibitory concentration (MIC) of cypromycin for a bacterial pathogen and the relationship between the area under the curve (AUC) and the MIC.

resistance mechanism

in-vitroResistance to cypromycin can be acquired through a gradual process through mutations at the target site in both DNA gyrase and topoisomerase IV. The degree of resulting cross-resistance between cypromycin and other fluoroquinolones is variable. Single mutations may not confer clinical resistance, but multiple mutations usually confer clinical resistance to many or all drugs in the class.

Mechanisms of impermeability and/or resistance of the drug efflux pump may differentially affect susceptibility to fluoroquinolones, depending on the physicochemical properties of the different drugs within the class and the affinity of the drugs in the respective transport systems principle active. Allin-vitroMechanisms of resistance are frequently observed in clinical isolates.

Resistance mechanisms that inactivate other antibiotics, such as permeation barriers (common inPseudomonas aeruginosa) and exit mechanisms may affect susceptibility to cypromycin.

Plasmid-mediated resistance encoded by qnr genes has been reported.

Antibacterial spectrum of action

Breakpoints separate susceptible strains from moderately susceptible strains and the latter from resistant strains:

EUCAST recommendations

¹ staphylococcisp. - Cypromycin limits are associated with high-dose therapy.

*Non-species breakpoints were determined primarily based on PK/PD data and are independent of species-specific MIC distributions. They are only intended for species that have not been assigned a species-specific cut-off point and not for species for which susceptibility testing is not recommended.

The prevalence of acquired resistance may vary geographically and over time for selected species, and local information on resistance is desirable, particularly when treating severe infections. As appropriate, specialist advice should be sought when the local prevalence of resistance is such that the utility of the agent in at least some types of infections is questionable.

Relevant species groupings by susceptibility to cypromycin

Absorption

After an intravenous infusion of cypromycin, mean maximum serum concentrations were reached at the end of the infusion. The pharmacokinetics of cypromycin were linear over the dose range up to 400 mg intravenous administration.

A comparison of pharmacokinetic parameters for a twice daily and three times daily intravenous dosing regimen revealed no evidence of drug accumulation of cypromycin and its metabolites.

A 60-minute intravenous infusion of 200 mg cypromycin or an oral administration of 250 mg cypromycin, both given every 12 hours, produced an equivalent area under the serum concentration curve (AUC).

A 60-minute intravenous infusion of 400 mg cypromycin every 12 hours was bioequivalent in AUC to an oral dose of 500 mg every 12 hours.

The 400 mg intravenous dose given over 60 minutes every 12 hours resulted in C_maximalsimilar to an oral dose of 750 mg.

A 60-minute infusion of 400 mg cypromycin every 8 hours corresponds in AUC to an oral dose of 750 mg every 12 hours.

distribution

Protein binding of cypromycin is low (20-30%). Cypromycin is present in plasma mainly in the unionized form and has a large steady-state volume of distribution of 2-3 L/kg body weight. Cypromycin reaches high concentrations in a variety of tissues, including the lungs (epithelial fluid, alveolar macrophages, biopsy tissue), sinuses, inflamed lesions (cantharidic bladder fluid), and the urogenital tract (urine, prostate, endometrium). when total concentrations above plasma concentrations are reached.

Biotransformation

Low levels of four metabolites identified as: diethylenecypromycin (M1), sulfocypromycin (M2), oxocypromycin (M3) and formylcypromycin (M4) have been reported. The metabolites are displayedin-vitroantimicrobial activity, but to a lesser extent than the parent compound.

Cypromycin is known to be a moderate inhibitor of CYP 450 1A2 isoenzymes.

elimination

Cypromycin is eliminated practically unchanged both in the kidneys and, to a lesser extent, in the faeces.

The renal clearance ranges from 180-300 ml/kg/h and the total body clearance ranges from 480-600 ml/kg/h. Cypromycin undergoes glomerular filtration and tubular secretion. Severely impaired renal function leads to a prolonged half-life of cypromycin of up to 12 hours.

The non-renal clearance of cypromycin is mainly due to active transintestinal secretion and metabolism. 1% of the dose is excreted in the bile. Cypromycin is present in high concentrations in the bile.

pediatric population

Pharmacokinetic data in pediatric patients are limited.

In a study on children C_maximaland AUC did not depend on age (more than one year). No noticeable increase in C_maximaland AUC was observed after multiple doses (10 mg/kg three times daily).

In 10 children with severe sepsis C_maximalwas 6.1 mg/L (range 4.6-8.3 mg/L) after a 1-hour intravenous infusion of 10 mg/kg in children less than 1 year old compared to 7.2 mg/L (range 4.7- 11.8 mg/l) for children between 1 and 5 years. The AUC values ​​were 17.4 mgh/L (range 11.8-32.0 mgh/l) and 16.5 mgh/L (range 11.0-23.8 mgh/l) in the respective age groups.

These values ​​are within the range given for adults at therapeutic doses. Based on population pharmacokinetic analyzes of pediatric patients with various infections, the expected mean half-life in children is approximately 4-5 hours and the bioavailability of the oral suspension ranges from 50 to 80%.

Non-clinical data reveal no special hazard for humans based on conventional studies of single dose toxicity, repeated dose toxicity, carcinogenic potential or toxicity to reproduction.

Like other quinolones, cypromycin is phototoxic in animals at clinically relevant exposure levels. Photomutagenicity/photocarcinogenicity data indicate that cypromycin has a weak photomutagenic or phototumor effectin-vitroand in animal experiments. This effect was comparable to that of other gyrase inhibitors.

common compatibility

As reported for other gyrase inhibitors, cypromycin causes damage to large weight-bearing joints in immature animals. The extent of cartilage damage varies with age, type, and dose; Damage can be reduced by relieving the joints. Studies with adult animals (rats, dogs) gave no evidence of cartilage damage. In a study in young beagle dogs, therapeutic doses of cypromycin caused severe joint changes after two weeks of treatment that were still evident after 5 months.

Unless compatibility with other solutions/drugs has been confirmed, the solution for infusion must always be administered separately. Visual signs of incompatibility are, for example, precipitation, turbidity and discoloration.

Incompatibility occurs with all infusion solutions/drugs that are physically or chemically unstable at the pH of the solutions (e.g. penicillins, heparin solutions), especially in combination with solutions adjusted to alkaline pH (pH of Cypromycin solutions: 3.9 - 4.5).

The solution should be inspected visually prior to use and only clear, particle-free solutions should be used.

The infusion contains no preservatives. For single use. Any remaining solution and vials and/or sachets must be properly disposed of in accordance with local regulations.

Cypromycin is compatible with sodium chloride saline, Ringer's solution, lactated Ringer's solution, glucose 50 mg/mL (5%) or 100 mg/mL (10%) and glucose 50 mg/mL. (5%) with 2.25 mg/mL (0.225%) or 4.5 mg/mL (0.45%) sodium chloride solution and 10% fructose solution. Compatibility with these solutions has been tested at concentrations of 1 mg/mL cypromycin. Chemical and physical in-use stability has been demonstrated immediately after dilution, 24 hours at 2-8°C and 24 hours at room temperature. Unless compatibility has been proven, the infusion solution must always be administered separately.

Diluted solutions should be visually inspected for particulate matter and discolouration prior to administration. Only clear and colorless solutions may be used.

Handling glass vials:

Cypromycin 2 mg/ml can be infused directly through a suitable needle or diluted with one of the liquids listed above.

Handling plastic bags:

Do not remove the device from the packaging until it is ready for use. The shell is a moisture barrier. The inner bag maintains the sterility of the product.

Open,Tear open the packaging along the slit side and remove the solution container. Some opacity of the plastic can be observed due to moisture absorption during the sterilization process. This is normal and does not affect the quality or safety of the solution. The opacity gradually decreases. After removing the packaging, check for minimal leaks by firmly squeezing the inner bag. If leaks are found, discard the solution as sterility may be compromised.

CAUTION: Do not use plastic containers in series connections. Such use can result in an air embolism due to the removal of residual air from the primary container before delivery of fluid from the secondary container is complete.

References:

• https://www.drugs.com/search.php?searchterm=cipromicina
• https://pubmed.ncbi.nlm.nih.gov/?term=cipromicina

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