Hepacef

Hepacef is an antibiotic from the β-lactam group with a wide range of effects. [1]

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

Indications Hepacef

It is used in the treatment (monotherapy or in combination with other substances) in people with infections associated with bacteria that show sensitivity to cefoperazone. These violations include:

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

The medication can be prescribed to prevent infections in the event of operations.

Release form

The release of drugs is carried out in the form of parenteral liquid - inside bottles with a capacity of 1 g. In a pack - 10 such bottles.

Pharmacodynamics

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

Pharmacokinetics

With i / v injections, the values of the intraplasmic Cmax of the active ingredient are recorded after 15 minutes, and with i / m injections - after 1 hour. Inside the bile, the Cmax level is observed after 1-3 hours. Approximately 93% of cefoperazone administered is synthesized with protein.

Cefoperazone undergoes good distribution within the body, forming high medicinal parameters inside the lungs, hepatic tissues, palatine tonsils, and in addition to the walls of the gallbladder, kidneys, bone tissues and pelvic organs. The active ingredient of the drug forms high values and inside bile with sputum.

Cefoperazone is able to cross the hematoplacental barrier, as well as excreted in mother's milk. If the patient's BBB is not damaged, the drug is almost not excreted inside the cerebrospinal fluid, but in people with traumatic or postoperative meningitis, it forms high values inside the cerebrospinal fluid.

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

The half-life of a drug is approximately 2 hours. Excretion is carried out mainly with bile, and about 30% more - with urine.

Dosing and administration

Hepacef in the form of a parenteral fluid is injected intramuscularly or intravenously.

To make an i / v 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 inside of the bottle, after which the container is shaken. The introduction of the liquid is made when the lyophilisate is completely dissolved. To make the dissolution more effective, you can increase the volume of the added solvent to 5 ml.

For intravenous injections through a dropper, the prepared liquid is dissolved in a compatible solvent (20-100 ml). At the same time, the volumes of injectable liquid during administration through a dropper can be no more than 20 ml (if more solvent is needed, other compatible solutions must be used). The duration of application through a dropper is often 15-60 minutes.

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

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

It is necessary to use lidocaine only in situations where the final level of cefoperazone inside the solution is more than 0.25 g / ml. The lidocaine values inside the finished liquid should be 0.5%. The medicinal liquid must be transparent - after obtaining such a state, it is deeply injected into the muscles of the buttock (upper outer quadrant).

An epidermal test must be performed prior to drug administration. In addition, people who are injected with IM injections using lidocaine need to be tested for tolerance to this substance.

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

If there is a severe infection, the portion for an adult is increased to 2-4 g of the medicine, also with a 12-hour break.

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

The standard duration of treatment is 7-14 days.

An adult with a gonococcal type of urethritis (without the appearance of complications) needs to inject 0.5 g of drugs intramuscularly.

For a child, the application is prescribed with 12-hour intervals of dosages of 0.025-0.1 g / kg of the substance. In the case of severe infections, the children's portion can increase to 0.2-0.3 g / kg per day (this dosage is divided into 2-3 injections, with the introduction at the same time intervals).

For premature and newborn babies, a portion of the medication is selected personally.

Therapy usually lasts 7-14 days.

For prophylaxis in case of operations, the medication is used in portions of 1-2 g, 30-90 minutes before the procedure. Further, cefoperazone is administered at a dosage of 1-2 g with 12-hour breaks during the period of the day after the completion of the operation (when performing procedures related to CVS, performing joint prosthetics, as well as in the case of colonoproctology, the drug should be used within 3 days from the date of surgery).

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

For persons who are on hemodialysis, the medication is used at the end of the treatment session.

During treatment with the use of drugs, it is necessary to constantly monitor the PTV values.

Use Hepacef during pregnancy

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

If there is no possibility of prescribing an alternative medication for breastfeeding, it is necessary to discontinue hepatitis B during treatment. It is allowed to restore feeding only with the permission of the attending doctor.

Contraindications

It is contraindicated to appoint people with intolerance to cephalosporins, as well as other β-lactam antimicrobial substances. In addition, they are not used for alcoholism of a chronic nature and in persons using medications that contain ethanol.

It is used with caution in people with an increased tendency to bleeding, hepatic dysfunctions and obstructive gastrointestinal tract diseases, as well as in the elderly. In the case of renal / hepatic dysfunction, the medication can be used only after a careful assessment of the possible risks and benefits.

Due to the likelihood of a disorder in the binding processes of K-vitamin in the treatment of Hepacef, it is used with extreme caution in people with cystic fibrosis, and in addition to those who are on partial or complete parenteral nutrition.

Side effects Hepacef

The medication is usually tolerated without complications. Possible side signs include:

• disorders affecting the hepatobiliary system and gastrointestinal tract: vomiting, stool disorders, nausea and an increase in the values of intrahepatic enzymes. Occasionally (also after several days from the end of treatment), colitis of a pseudomembranous nature may appear;
• disorders of hematopoietic processes: eosinophilia, a decrease in hematocrit values with hemoglobin and hypothrombinemia. Curable neutropenia is noted only once;
• allergy symptoms: urticaria, fever and epidermal itching. Sometimes the development of anaphylaxis was observed, requiring immediate therapy (for example, it is necessary to administer corticosteroids and epinephrine; in addition, if necessary, tracheal intubation, oxygen therapy and mechanical ventilation are performed);
• others: in the case of intravenous injection, phlebitis may occur; with an intramuscular injection, pain may occur in the area of the procedure. At the same time, when using cefoperazone, patients developed a K-vitamin deficiency, and in addition, a false positive response to the Coombs' test and the determination of sugar values inside the urine, carried out by non-enzymatic methods. Long-term treatment can provoke candidiasis (vaginal or oral).

Overdose

The use of large portions of cefoperazone can provoke an attack of epilepsy, convulsions, and in addition, hemolytic anemia, thrombocyto-, neutro- or leukopenia. The introduction of Hepacef in high doses increases the likelihood of anaphylaxis (also fatal).

The medicine has no antidote. When symptoms of poisoning appear, symptomatic substances are used. At the same time, in case of an overdose, the use of the medication is also canceled. If seizures occur, diazepam is given.

When using large doses of cefoperazone, the likelihood of anaphylaxis must be taken into account. Therefore, treatment with the use of drugs is performed only in a hospital, under the constant supervision of doctors.

Interactions with other drugs

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

The likelihood of bleeding increases in the case of a combination of medication with heparin, anticoagulants, and thrombolytics.

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

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

You can not use the medicine parenterally in combination with aminoglycoside fluids. If the combined use of these funds was prescribed, Hepacef is first introduced; after that, the infusion system is flushed (a compatible solution is used), and then the aminoglycoside solution is injected.

Storage conditions

Hepacef must be kept at temperatures within the 2-8oC range. The finished liquid is injected immediately, it cannot be stored.

Shelf life

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

Analogs

Analogues of drugs are the substances Cefoperazone and Medocef with Cephobid.