Ciprofloxacin

Posted onApril 17, 2018

A synthetic antibacterial preparation of a broad spectrum of action from the group of fluoroquinolones.

Pharmacological properties

Ciprofloxacin is a broad-spectrum antimicrobial agent of the fluoroquinolones group. Has a bactericidal effect, the mechanism of which is due to the inhibition of DNA-gyrase of bacteria with a violation of DNA synthesis, growth and division of microorganisms.

Has antimicrobial effect with the highest activity against aerobic gram-negative and gram-positive bacteria: Pseudomonas aeruginosa, Haemophilus influenzae, Escherichia coli, Shigella spp., Salmonella spp., Neisseria meningitidis, N. gonorrhoeae. It is active against many strains of Staphylococcus spp. (producing and non-producing penicillinase), some strains of Enterococcus spp., as well as Campylobacter spp., Legionella spp., Mycoplasma spp., Chlamidia spp., Mycobacterium spp. Ciprofloxacin is active against bacteria that produce beta-lactamase. Resistant to ciprofloxacin Streptococcus faecium, Ureaplasma urealyticum, Nocardia asteroides, Treponema pallidum. Resistance of bacteria to ciprofloxacin develops slowly.

When ingested quickly and completely absorbed in the digestive tract. Cmax in blood plasma is achieved 1-2 hours after admission, bioavailability is 70%, T1 is 4 hours. Approximately 20-40% of ciprofloxacin binds to plasma proteins. Ciprofloxacin is well distributed in tissues and body fluids, and its concentration can significantly exceed the concentration in the blood plasma. Penetrates into the CSF through the placenta, excreted in breast milk, high concentrations are determined in the bile. It is excreted from the body up to 40% with urine (unchanged) for 24 hours, in part – with bile.

Application:

Infections caused by drug-susceptible microorganisms:

infections of the lower respiratory tract caused by gram-negative bacteria (pneumonia, except pneumococcal, bronchopulmonary infection in chronic obstructive pulmonary disease, cystic fibrosis, bronchiectasis);
infections of the middle ear and paranasal sinuses caused by gram-negative bacteria;
infections of the kidneys and urinary tract;
skin and soft tissue infections caused by gram-negative bacteria;
infection of bones and joints;
infections of the pelvic organs (including adnexitis and prostatitis), gonorrhea;
infections of the gastrointestinal tract (including diarrhea, caused by enterotoxigenic strains of Escherichia coli, Campylobacter jejuni);
intra-abdominal infections;
infection in patients with reduced immunity (with neutropenia).

Do not take Ciprofloxacin in the following cases:

hypersensitivity to ciprofloxacin, other quinolones or excipients of the drug;
pregnancy, the period of breastfeeding;
children and adolescents under 18;
simultaneous use with tizanidine.

Possible side effects: Like all medicines, ciprofloxacin can cause side effects with varying frequency, regardless of whether it was previously taken.

Often (1 to 10 – 100 cases): nausea, diarrhea.

Infrequently (1 per 100 to 1,000 cases): fungal superinfections, eosinophilia, lack of appetite, hyperactivity, agitation, headaches, dizziness, sleep disorders, taste disorders, vomiting, stomach and bowel pain, dyspepsia, flatulence, increased hepatic activity enzymes, increased bilirubin, rash, itching, urticaria, musculoskeletal pain (in the extremities, back, chest), joint pain, impaired renal function, fatigue, fever.

Rarely (1 per 1,000 – 10,000 cases): inflammation of the colon, changes in the number of leukocytes, anemia, a decrease in the number of platelets, allergic reactions, increased blood sugar, confusion, pathological dreams, depression with the appearance of suicidal thoughts, changes in sensitivity, trembling , convulsions, dizziness, visual impairment, hearing disorders, tachycardia, decreased blood pressure, fainting, choking, liver function disorders, jaundice, hepatitis, photosensitivity, muscle pain, joint inflammation, increased muscle -screw tone, muscle spasms, renal failure, blood / crystals in the urine, nephritis, increased amylase activity.

Very rarely (less than 1 in 10 000 cases): hemolytic anemia, decreased number of blood cells, suppression of bone marrow function, anaphylactic reaction, anaphylactic shock, mental reactions with possible suicidal attempts, migraine, impaired coordination, unstable gait, odor perception disorder, increased intracranial pressure, changes in color perception, vasculitis, pancreatitis, liver necrosis, petechiae, erythema, Stevens-Johnson syndrome, toxic epidermal necrolysis, muscle weakness, inflammation and tearing of tendons (mainly Achilles), swelling, increased sweating.

The frequency is unknown (can not be estimated from the available data): peripheral neuropathy, ventricular tachycardia, arrhythmia, acute generalized pustular exanthema, increased prothrombin time.

If you took a dose of ciprofloxacin more than the doctor recommended: If the number of tablets a day you took exceeds the amount that your doctor recommended, or your child swallowed the tablets, consult a doctor or call an ambulance! Stop taking medication! Overdosing can be manifested by dizziness, headache, fatigue, convulsions, hallucinations, confusion, a feeling of discomfort in the abdomen, a violation of kidney and liver function, the presence of crystals and blood in the urine. As a first aid it is recommended to wash the stomach and take antacids.

Precautions and special instructions for taking Ciprofloxacin:

Severe infectious diseases and mixed infectious processes. In these conditions, ciprofloxacin is administered in combination with other antimicrobial agents.

Streptococcal infection (including Streptococcus pneumoniae). Ciprofloxacin is not recommended for treatment due to inadequate efficacy.

Urogenital infections. These infections can be caused by fluoroquinolone resistant Neisseria gonorrhoeae. In these cases, ciprofloxacin should be administered along with other antimicrobials. If no improvement is observed within 3 days of treatment, then treatment is recommended to be reviewed.

Intra-abdominal infectious diseases. Data on the effectiveness of ciprofloxacin for the treatment of postoperative intra-abdominal infectious diseases are limited.

Diarrhea of ​​the “traveler”. When choosing ciprofloxacin, the available information on drug resistance of the relevant microorganisms in the visited country is taken into account.

Infectious diseases of bones and joints. Ciprofloxacin is administered in combination with other antimicrobials after a microbiological examination.

Anthrax: Information on the use of the drug in humans is limited. It is recommended to be guided by national and / or international documents on the treatment of this disease.

Other specific severe infectious diseases: Ciprofloxacin is used according to treatment protocols or after careful assessment of the “risk-benefit” ratio and microbiological analysis in cases where other treatment is not possible or after an adverse outcome of previous therapy.

Hypersensitivity. After taking a single dose of the drug, hypersensitivity reactions are possible, including anaphylactic and anaphylactoid reactions, which are life-threatening conditions. Take the medicine immediately and immediately inform the doctor or call an ambulance!

The musculoskeletal system. Ciprofloxacin should not be given to patients with tendon disorders or disorders in the administration of quinolones in the past. If necessary, treatment of severe infectious diseases in such patients for the treatment of severe infectious diseases, a microbiological study and an assessment of the ratio of “risk-benefit.” Perhaps the occurrence of inflammation or rupture of tendons, mainly in elderly patients or concomitantly taking corticosteroids. With any signs of this disease (swelling, inflammation), the drug is taken to stop and immobilize the affected limb. It is used with caution in patients with myasthenia gravis.

Photosensitivity. Patients taking ciprofloxacin should avoid direct exposure to sunlight and UV radiation.

Central nervous system. It is known that quinolones can lower the convulsive threshold and initiate convulsions. It is used with caution by patients with CNS diseases, provoking convulsive seizures. There were reports of cases of polyneuropathy (pain, burning, feeling of excitement, tinnitus, muscle weakness, sensitivity disorders, including tactile, pain, temperature, vibration, and musculo-articular). When these phenomena occur, stop taking the drug! Immediately inform the doctor.

The cardiovascular system. Since the use of ciprofloxacin is associated with cases of prolongation of the QT interval on the ECG, care must be taken when treating patients at risk of arrhythmia: congenital lengthening of the QT interval; simultaneous reception of antiarrhythmic drugs of class IA and III, antidepressants, macrolides, antipsychotics; electrolyte disturbances; women and elderly patients are more sensitive; heart disease.

Pseudomembranous colitis: If you suspect a pseudomembranous colitis (loose stool for a long time, possibly with an admixture of blood or mucus in it), stop taking it immediately and call a doctor immediately for the appropriate treatment! Do not use drugs that depress intestinal motility. Immediately inform the doctor.

Renal and urinary systems: Sufficient fluid should be taken.

Hepatobiliary system: There were reports of cases of liver necrosis and life-threatening liver failure (jaundice, dark urine, itching, lack of appetite). When these phenomena occur, stop taking the drug! Immediately inform the doctor.

Deficiency of glucose-6-phosphate dehydrogenase. Possible development of hemolytic reactions. The drug is not assigned to such patients, except when the potential benefit exceeds the possible risk.

Resistance. During long-term therapy and in cases of treatment of some infections, ciprofloxacin-resistant bacteria can be released.

Eating and dairy products. You should avoid simultaneous reception with dairy products or beverages enriched with minerals (milk, yogurt, calcium fortified, orange juice), since the absorption of ciprofloxacin may decrease.

Contraindications

Hypersensitivity to ciprofloxacin or other quinolones, pregnancy and lactation, age 12 years, severe liver and kidney dysfunction, history of tendonitis caused by the use of quinolones.

Side effects

As a rule, it is well tolerated, but the following side effects are possible: dizziness, headache, fatigue, agitation, tremor; in isolated cases – peripheral disorders of sensitivity, sweating, hot flashes, gait disturbance, increased intracranial pressure, a sense of fear, depression, visual disturbances; nausea, vomiting, diarrhea, digestive disorders, abdominal pain, flatulence, hepatitis, necrosis of liver cells; tachycardia, rarely – AH; skin itching, rash; extremely rare – edema Quincke, bronchospasm, arthralgia; anaphylactic shock, petechiae, vasculitis, Stevens-Johnson syndrome, Lyell’s syndrome; eosinophilia, leukopenia, anemia, thrombocytopenia; leukocytosis, thrombocytosis, hemolytic anemia; increase in plasma creatinine, hepatic transaminases, alkaline phosphatase, LDH, bilirubin.

Special instructions

With caution appoint patients with epilepsy and patients with other organic diseases of the central nervous system, as well as with cerebral atherosclerosis.

With simultaneous treatment with ciprofloxacin and barbiturates, it is necessary to monitor heart rate, blood pressure, and ECG. During the treatment should monitor the concentration in the blood of urea, creatinine, liver transaminases.

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