Cefalotin (Powder) Instructions for Use

ATC Code

J01DB03 (Cefalotin)

Active Substance

Cefalotin (Rec.INN registered by WHO)

Clinical-Pharmacological Group

First generation cephalosporin

Pharmacotherapeutic Group

Antibiotic-cephalosporin

Pharmacological Action

A first-generation broad-spectrum cephalosporin antibiotic for parenteral use. It exerts a bactericidal effect by disrupting the synthesis of the microorganism’s cell wall.

It is active against gram-positive bacteria: Staphylococcus spp. (penicillinase-producing and non-producing strains), Streptococcus spp. (including Streptococcus pneumoniae), Corynebacterium diphtheriae, Bacillus anthracis; gram-negative bacteria: Neisseria meningitidis, Neisseria gonorrhoeae, Shigella spp., Salmonella spp., Escherichia coli, Haemophilus influenzae, Klebsiella spp. It is also active against Spirochaetaceae, Leptospira spp.

It is not active against Pseudomonas aeruginosa, Proteus spp. (indole-positive strains), Mycobacterium tuberculosis, anaerobic bacteria.

Pharmacokinetics

C_max after intramuscular administration of cefalotin in doses of 0.5 and 1 g is reached after 30 minutes and is 10 and 20 µg/ml, respectively; 60-70% of the dose is excreted by the kidneys within the first 6 hours.

15 minutes after a single intravenous administration of 1 g of cefalotin, C_max was about 30 µg/ml, after 1 hour – 3-12 µg/ml, after 4 hours it decreased to approximately 1 µg/ml. After continuous infusion at a dose of 500 mg/h, C_max was 14-20 µg/ml. 30 minutes after infusion of 2 g of cefalotin, C_max is approximately 80-100 µg/ml; after 1 hour – 10-40 µg/ml, after 2 hours – approximately 3-6 µg/ml; after 5 hours, Cefalotin was not detected in the blood.

Binding to plasma proteins is 65%, V_d – 18±4 l/1.73 m². With parenteral administration, Cefalotin penetrates well and is found in therapeutic concentrations in the kidneys, myocardium, skin, muscles, liver, lungs, and pleural fluid.

Cefalotin is metabolized in the liver (20-30%). T_1/2 after intramuscular administration is 0.5-1 hour. It is excreted by the kidneys through tubular secretion within 6 hours – 70-80% unchanged, 30% as a metabolite (deacetyl). It is moderately excreted during hemodialysis, well – during peritoneal dialysis.

Indications

Infectious and inflammatory diseases caused by microorganisms sensitive to cefalotin, including diseases of the upper and lower respiratory tract, urinary tract, pelvic organs, skin and soft tissues, bones and joints; endocarditis, sepsis, peritonitis, otitis media, osteomyelitis, mastitis; wound, burn, and postoperative infections.

ICD codes

Dosage Regimen

Powder

It is administered intramuscularly, intravenously, and intraperitoneally. The dosage regimen is set individually, taking into account the severity and localization of the infection, the sensitivity of the pathogen, and the patient’s age.

For adults, a single dose is 0.5-1 g every 4-6 hours. In severe infections, the dose may be increased to 2 g every 4 hours. For the prevention of intra- and postoperative infection – 1-2 g 30 minutes before the start of surgery, in the same dose – during surgery and then every 6 hours for 24 hours after surgery. When treating an infection caused by group A beta-hemolytic streptococcus, the minimum duration of the course is 10 days. During peritoneal dialysis procedures, Cefalotin may be added to the dialysis fluid.

The dosage regimen for children is established taking into account age, body weight, and the severity of the disease. The recommended dose is 60 mg/kg/day (from 40 to 80 mg/kg/day) divided into equal doses throughout the day. In newborns weighing less than 2 kg, the recommended dose is 20 mg/kg every 12 hours. For perioperative prophylaxis – 20-30 mg/kg intravenously according to the scheme specified for adult patients.

Adverse Reactions

Infections and infestations frequency unknown – secondary infections caused by non-susceptible microorganisms.

Blood and lymphatic system disorders uncommon – eosinophilia, thrombocytopenia, neutropenia; very rare – hemolytic anemia, granulocytopenia, pancytopenia.

Immune system disorders rare – serum sickness; very rare – anaphylactic shock.

Nervous system disorders : very rare – encephalopathy.

Respiratory, thoracic and mediastinal disorders: very rare – bronchospasm, dyspnea, laryngospasm.

Cardiac disorders very rare – decreased blood pressure, arrhythmia.

Hepatobiliary disorders uncommon – transient increase in the activity of hepatic transaminases and alkaline phosphatase; very rare – cholestatic jaundice.

Gastrointestinal disorders common – vomiting, nausea, diarrhea, pseudomembranous colitis; rare – abnormal breath odor.

Skin and subcutaneous tissue disorders uncommon – maculopapular rash, urticaria, erythema; rare – skin rash; very rare – cyanosis.

Renal and urinary disorders common – transient increase in urea concentration and decrease in creatinine clearance (usually in patients with renal failure); uncommon – unspecified nephropathy and other manifestations of nephrotoxicity.

Investigations frequency unknown – false-positive Coombs test.

Local reactions: with intramuscular administration common – pain at the injection site, sometimes with the development of induration; with intravenous administration uncommon – phlebitis, thrombophlebitis.

Contraindications

Hypersensitivity to cefalotin and other cephalosporins; severe immediate-type hypersensitivity reactions (e.g., anaphylactic reaction) to penicillins and other beta-lactam antibiotics (monobactams, carbapenems); breastfeeding period; children with impaired renal function; newborns – depending on the route of administration.

With caution

Impaired renal function, simultaneous use with nephrotoxic drugs, history of non-severe hypersensitivity reactions to penicillins and other beta-lactam antibiotics (monobactams, carbapenems), intestinal diseases (including history of colitis); pregnancy.

Use in Pregnancy and Lactation

Use during pregnancy is possible only in cases where the intended benefit to the mother outweighs the potential risk to the fetus.

If it is necessary to use during lactation, the issue of discontinuing breastfeeding should be decided.

Use in Renal Impairment

Use with caution in patients with impaired renal function; in this case, dose adjustment is necessary. Not recommended for use in patients with renal failure.

Pediatric Use

Contraindicated in children with impaired renal function. It can be used in children according to indications, in recommended doses and regimens. It is necessary to strictly follow the instructions for medical use of cefalotin preparations in children.

Special Precautions

Before starting the use of cefalotin, the patient’s allergy history should be collected due to the possibility of developing cross-hypersensitivity reactions between cephalosporins and penicillins or other beta-lactam antibiotics. In case of a hypersensitivity reaction, it is necessary to discontinue cefalotin and prescribe appropriate symptomatic therapy.

Particularly careful monitoring is necessary for patients with a tendency to allergic reactions (allergic rhinitis, bronchial asthma), since against the background of such conditions the risk of hypersensitivity reactions increases.

During the use of cefalotin, false-positive reactions for the determination of glucose in urine are possible when using Benedict’s or Fehling’s reagent, as well as false-positive results of the direct and indirect Coombs test.

With prolonged use of cefalotin, monitoring of the peripheral blood picture is necessary.

Long-term use of cefalotin may provoke the emergence of resistant strains of bacteria. The condition of patients should be carefully monitored for the possibility of developing superinfection and appropriate measures should be taken in case of its development.

Due to the possibility of developing disulfiram-like reactions during the use of cefalotin, patients should refrain from consuming alcohol during the treatment period.

Drug Interactions

With simultaneous use with probenecid, the renal clearance of cefalotin decreases, which leads to an increase in its elimination time and an increase in its plasma concentration.

With simultaneous use, Cefalotin can reduce the effectiveness of oral contraceptives, which may require the use of additional non-hormonal methods of contraception.

The risk of kidney damage increases with the simultaneous use of cefalotin with aminoglycosides, polymyxins, ethacrynic acid, furosemide.

With simultaneous use of cefalotin with “loop” diuretics (e.g., furosemide), blockade of tubular secretion of cefalotin occurs, which leads to an increase in its plasma concentration.

With simultaneous use of cefalotin with anticoagulants, an additive effect is possible; with methotrexate – a decrease in the effectiveness of methotrexate is possible.

The risk of bleeding may be increased with the simultaneous use of cefalotin with salicylates, cephalosporins, NSAIDs, sulfinpyrazone.

Storage Conditions

Store at 2°C (36°F) to 30°C (86°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.