Hepacef

Hepacef is an antibiotic from the β-lactam group with a broad spectrum of action. [ 1 ]

The active ingredient of the drug is the component cefoperazone – an antimicrobial therapeutic agent from the subgroup of cephalosporins of the 3rd generation. The drug demonstrates an intense bactericidal effect on pathogenic microorganisms. The principle of action of the drug is based on the ability of the active component to suppress protein binding processes inside bacterial cells. [ 2 ]

Indications Hepacef

It is used in the treatment (monotherapy or combination with other substances) of people with infections associated with bacteria that demonstrate sensitivity to cefoperazone. Among such disorders are:

• lesions affecting the pelvic organs, biliary tract and urethra;
• infections in the lower and upper respiratory tract;
• lesions of joints with bones, subcutaneous layers and epidermis;
• meningitis of postoperative or traumatic origin, septicemia, peritonitis and urethritis of gonococcal origin, occurring without the development of complications.

The medication may be prescribed to prevent infections in the event of surgery.

Release form

The drug is released in the form of a parenteral liquid - inside vials with a capacity of 1 g. There are 10 such vials in a pack.

Pharmacodynamics

The drug affects strains of gram-negative and -positive anaerobes with aerobes. Among them are individual strains that produce β-lactamases (this includes strains of Haemophilus influenzae and gonococci that produce β-lactamases). [ 3 ]

Pharmacokinetics

With intravenous injections, the values of intraplasmic Cmax of the active component are recorded after 15 minutes, and with intramuscular injections - after 1 hour. In bile, the Cmax level is observed after 1-3 hours. Approximately 93% of the administered cefoperazone is synthesized with protein.

Cefoperazone is well distributed inside the body, forming high drug levels inside the lungs, liver tissue, tonsils, and also the walls of the gallbladder, kidneys, bone tissue and pelvic organs. The active element of the drug forms high levels inside bile and sputum.

Cefoperazone is able to overcome the hematoplacental barrier and is also excreted with mother's milk. If the patient's BBB is not damaged, the drug is almost not excreted into the cerebrospinal fluid, but in people with traumatic or postoperative meningitis, it forms high levels in the cerebrospinal fluid.

A small part of the drug is involved in metabolic processes.

The half-life of the drug is approximately 2 hours. Excretion occurs mainly with bile, and approximately 30% with urine.

Dosing and administration

Hepacef in the form of a parenteral liquid is administered intramuscularly or intravenously.

To prepare the intravenous liquid, injection water, 5% or 10% injection glucose, 5% glucose solution, physiological fluid and injection 0.9% NaCl can be used. A compatible solvent (2.8 ml) is added to the vial, after which the container is shaken. The liquid is administered when the lyophilisate is completely dissolved. To make dissolution more effective, the volume of the added solvent can be increased to 5 ml.

For intravenous injections through a dropper, the prepared liquid is dissolved in a compatible solvent (20-100 ml). In this case, the volume of injection liquid during administration through a dropper may not exceed 20 ml (if more solvent is needed, other compatible solutions must be used). The duration of use through a dropper is often 15-60 minutes.

If jet intravenous administration of the drug is performed, the maximum 1-fold dose of cefoperazone is 2 mg (for an adult) and 50 mg/kg (for a child). During jet injections, the cefoperazone indicator inside the solution should be 0.1 g/ml. The duration of jet administration of the drug is within 3-5 minutes.

When preparing the liquid for intramuscular injections, injection water and 2% lidocaine can be used. The required volume of injection liquid is added into the vial with the lyophilisate, shaken, and then, after waiting for the powder to dissolve, 2% lidocaine is added to it.

Lidocaine should only be used in situations where the final level of cefoperazone inside the solution is more than 0.25 g / ml. The lidocaine indicators inside the finished liquid should be 0.5%. The medicinal liquid must be transparent - after obtaining this state, it is deeply injected into the gluteal muscle (upper outer quadrant).

An epidermal test must be performed before the drug is administered. In addition, people who are given intramuscular injections of lidocaine must be tested for tolerance to this substance.

For adults, the dosage is often 1-2 g of medication at 12-hour intervals.

If a severe infection is observed, the dose for an adult is increased to 2-4 g of the drug, also with 12-hour breaks.

In case of severe infection, an adult can be administered no more than 12-16 g of Hepacef (the dose is divided into 3 injections at equal time intervals).

The standard duration of treatment is 7-14 days.

For an adult with gonococcal urethritis (without complications), 0.5 g of the drug should be administered intramuscularly once.

For a child, the dosage is prescribed at 12-hour intervals of 0.025-0.1 g/kg of the substance. In case of severe infections, the child's dose can be increased to 0.2-0.3 g/kg per day (this dosage is divided into 2-3 injections, administered at equal time intervals).

For premature and newborn babies, the dose of medication is selected individually.

Therapy usually lasts 7-14 days.

For prophylaxis in case of operations, the drug is used in a dose of 1-2 g, 30-90 minutes before the procedure. Then cefoperazone is administered in a dosage of 1-2 g with 12-hour breaks during the period of 24 hours after the completion of the operation (when performing procedures related to cardiovascular diseases, joint prosthetics, and in the case of colonoproctology, the drug should be used for a period of 3 days from the moment of surgery).

People with renal dysfunction (CC level below 18 ml per minute) can take no more than 4 g of Hepacef per day.

For people undergoing hemodialysis, the medication is administered after the completion of the treatment session.

During treatment with drugs, it is necessary to constantly monitor the PT values.

Use Hepacef during pregnancy

Cefoperazone is used in pregnant women only if there are strict indications.

If it is not possible to prescribe an alternative medicine during breastfeeding, breastfeeding should be discontinued for the duration of treatment. Breastfeeding can be resumed only with the permission of the attending physician.

Contraindications

Contraindicated for use in people with intolerance to cephalosporins and other β-lactam antimicrobial agents. In addition, do not use in chronic alcoholism and in people using medications that contain ethanol.

It is used with caution in people with an increased tendency to bleeding, liver dysfunctions and diseases of the biliary tract that have an obstructive nature, as well as in the elderly. In case of renal/liver dysfunctions, the drug can be used only after a thorough assessment of the possible risks and benefits.

Due to the possibility of disruption of vitamin K binding processes during treatment with Hepacef, it is used with extreme caution in people with cystic fibrosis, as well as in people on partial or complete parenteral nutrition.

Side effects Hepacef

The drug is usually tolerated without complications. Possible side effects include:

• disorders affecting the hepatobiliary system and gastrointestinal tract: vomiting, bowel disorders, nausea and increased intrahepatic enzyme levels. Pseudomembranous colitis may occasionally occur (also after several days from the end of treatment);
• disorders of hematopoietic processes: eosinophilia, decreased hematocrit values with hemoglobin and hypothrombinemia. Curable neutropenia is observed sporadically;
• allergy symptoms: urticaria, fever and epidermal itching. Sometimes anaphylaxis has developed, requiring immediate therapy (for example, it is necessary to administer corticosteroids and epinephrine; in addition, if necessary, tracheal intubation, oxygen therapy and artificial ventilation are performed);
• Others: in case of intravenous injection, phlebitis may be observed; in case of intramuscular injection, pain in the area of the procedure may occur. At the same time, when using cefoperazone, patients developed vitamin K deficiency, and in addition, a false-positive response to the Coombs test and determination of sugar levels in the urine, carried out by non-enzymatic methods. Long-term treatment can provoke candidiasis (vaginal or oral).

Overdose

The use of large doses of cefoperazone may provoke an epileptic seizure, convulsions, and also hemolytic anemia, thrombocyto-, neutro- or leukopenia. The introduction of Hepacef in high doses increases the likelihood of anaphylaxis (also fatal).

The drug has no antidote. When symptoms of poisoning appear, symptomatic substances are used. At the same time, in case of overdose, the use of the drug is also canceled. When convulsions appear, diazepam is administered.

When using high doses of cefoperazone, the possibility of anaphylaxis must be taken into account. Therefore, treatment with the drug is performed only in a hospital, under constant medical supervision.

Interactions with other drugs

The drug is not used together with substances that contain ethanol, because this can cause disulfiram-like symptoms associated with the accumulation of acetaldehyde in the blood. Characteristic signs appear within 15-30 minutes from the moment of ethanol use and disappear on their own after 2-3 hours.

The risk of bleeding increases when the medication is combined with heparin, anticoagulants, and thrombolytics.

Loop diuretics and aminoglycosides increase the nephrotoxic activity of cefoperazone (the intensity of this disorder is most pronounced in individuals with renal dysfunction).

The introduction of Hepacef in combination with salicylic acid derivatives, NSAIDs and sulfinpyrazone increases the likelihood of ulcers in the gastrointestinal tract, as well as bleeding inside the stomach.

The drug should not be used parenterally in combination with aminoglycoside fluids. If a combined use of these agents has been prescribed, Gepacef is administered first; then the infusion system is flushed (a compatible solution is used), and then the aminoglycoside solution is administered.

Storage conditions

Hepacef should be stored at temperatures between 2-8°C. The prepared liquid is administered immediately and cannot be stored.

Shelf life

Gepacef can be used within 24 months from the date of sale of the drug.

Analogues

The analogs of the drug are the substances Cefoperazone and Medocef with Cefobid.