Acinobactam-AG (Powder) Instructions for Use

Marketing Authorization Holder

Altegra, JSC (Russia)

ATC Code

J01CG01 (Sulbactam)

Active Substance

Sulbactam (Rec.INN registered by WHO)

Dosage Forms

	Acinobactam-AG	Powder for solution for intravenous and intramuscular administration 500 mg
		Powder for solution for intravenous and intramuscular administration 1000 mg

Dosage Form, Packaging, and Composition

Powder for solution for intravenous and intramuscular administration crystalline, white or almost white in color.

500 mg – vials – cardboard packs – By prescription

Powder for solution for intravenous and intramuscular administration crystalline, white or almost white in color.

1000 mg – vials – cardboard packs – By prescription

Clinical-Pharmacological Group

Beta-lactamase inhibitor

Pharmacotherapeutic Group

Systemic antibacterial agents; beta-lactam antibacterial agents, penicillins; beta-lactamase inhibitors

Pharmacological Action

Sulbactam does not possess clinically significant antibacterial activity (with the exception of bacteria of the Neisseriaceae and Acinetobacter spp. families).

Sulbactam is an irreversible inhibitor of most major beta-lactamases produced by microorganisms resistant to beta-lactam antibiotics.

The ability of sulbactam to prevent the destruction of penicillin and cephalosporins by resistant microorganisms has been confirmed in studies using resistant strains, against which Sulbactam demonstrated pronounced synergy with penicillins and cephalosporins.

Furthermore, Sulbactam interacts with some penicillin-binding proteins, therefore Sulbactam often has a more pronounced effect on susceptible strains than a single beta-lactam antibiotic.

Sulbactam should be used in combination with other beta-lactam antibiotics.

Pharmacokinetics

After parenteral administration, Sulbactam is well distributed in most body tissues and fluids, such as peritoneal fluid, prostate, appendix, and partially penetrates the placenta.

The degree of penetration into the brain and cerebrospinal fluid is low. The V_d is approximately 15 L.

Bioavailability after intramuscular administration is almost 100%. Plasma protein binding is 38%.

Approximately 80% of sulbactam is excreted by the kidneys with a T_1/2 of about 1 hour. The total clearance is 270 ml/min.

In case of renal impairment, T_1/2 increases depending on CrCl. Hemodialysis alters the pharmacokinetics of sulbactam.

Indications

Infectious and inflammatory diseases caused by strains of microorganisms sensitive to the combination of sulbactam with beta-lactam antibiotics, strictly in combination with beta-lactam antibiotics (ampicillin, cefepime, cefoperazone, cefotaxime, ceftriaxone).

The combination should be used if it provides greater safety than the administration of the corresponding beta-lactam antibiotic as monotherapy.

The use of sulbactam without the simultaneous administration of a beta-lactam antibiotic is not advisable, because Sulbactam does not possess clinically significant antibacterial activity.

ICD codes

Dosage Regimen

Administered intramuscularly or intravenously.

For adults, with each administration of a beta-lactam antibiotic (at the usual dosage), depending on the sensitivity of the pathogen, the addition of 0.5-1 g of sulbactam is recommended.

The maximum daily dose of sulbactam is 4 g regardless of the dose of the simultaneously administered antibiotic.

The daily dose is recommended to be divided into equal parts and administered every 6, 8, or 12 hours, taking into account the frequency of administration of the beta-lactam antibiotic.

In case of renal failure, adjustment of the dosage regimen is required depending on CrCl.

In elderly patients without renal failure, no dose adjustment of sulbactam is required.

For children, the recommended daily dose of sulbactam is 50 mg/kg of body weight, divided into equal parts and administered every 6, 8, or 12 hours.

The maximum daily dose of sulbactam in children should not exceed 80 mg/kg of body weight.

Treatment with sulbactam should be continued for as long as the beta-lactam antibiotic is used.

Adverse Reactions

Infections and parasitic diseases uncommon – fungal infection/stomatitis; frequency unknown – pseudomembranous colitis.

Blood and lymphatic system disorders common – eosinophilia; uncommon – thrombocytopenia, leukopenia; frequency unknown – thrombocytosis, leukocytosis, neutropenia, anemia.

Immune system disorders uncommon – hypersensitivity; frequency unknown – anaphylactic shock.

Nervous system disorders common – dizziness; frequency unknown – headache, seizures.

Gastrointestinal disorders common – diarrhea; uncommon – vomiting; frequency unknown – nausea, decreased appetite, flatulence.

Hepatobiliary disorders common – increased activity of hepatic transaminases; frequency unknown – increased bilirubin concentration.

Skin and subcutaneous tissue disorders uncommon – allergy, skin reactions; frequency unknown – Stevens-Johnson syndrome, toxic epidermal necrolysis.

Musculoskeletal and connective tissue disorders frequency unknown – muscle spasms.

Renal and urinary disorders frequency unknown – increased blood creatinine concentration, interstitial nephritis.

General disorders and administration site conditions common – thrombophlebitis; uncommon – pain at the injection site.

Contraindications

Hypersensitivity to sulbactam, as well as to cephalosporins, penicillins, and other beta-lactam antibiotics.

Contraindications indicated in the prescribing information of the antibiotic used in combination with sulbactam should be taken into account.

With caution

In patients with severe renal and hepatic impairment, in patients with bronchial asthma, urticaria, and hay fever, in newborns, including premature infants.

Use in Pregnancy and Lactation

Sulbactam crosses the placental barrier.

The use of sulbactam during pregnancy is possible only in cases where the intended benefit to the mother outweighs the potential risk to the child.

Sulbactam passes into breast milk.

If use during lactation is necessary, breastfeeding should be discontinued.

Use in Hepatic Impairment

Use with caution in patients with severe hepatic impairment.

Use in Renal Impairment

Use with caution in patients with severe renal impairment.

Pediatric Use

Use with caution in newborns, including premature infants.

Geriatric Use

In elderly patients without renal failure, no dose adjustment of sulbactam is required.

Special Precautions

The efficacy of sulbactam in children under 1 year of age has not been fully studied; use in this patient group only after careful assessment of risk and benefit.

Use with caution in patients with bronchial asthma, urticaria, and hay fever.

Cases of serious hypersensitivity reactions have been reported in patients using beta-lactam antibiotics.

The risk is particularly high in patients with known hypersensitivity to penicillin and in patients with a history of hypersensitivity reactions to many allergens.

In cases of severe biliary obstruction, severe liver disease, as well as impaired renal function, dose adjustment is necessary.

With simultaneous use of aminoglycosides, renal function should be monitored.

With prolonged antibiotic treatment, overgrowth of non-susceptible microorganisms, including fungi, may be observed.

Antibiotic treatment alters the normal intestinal flora and may lead to overgrowth of Clostridium difficile.

In case of severe diarrhea, the use of sulbactam should be discontinued immediately and appropriate therapy initiated.

Drugs that inhibit peristalsis are contraindicated.

During long-term therapy, it is recommended to periodically monitor indicators of the function of internal organs, including kidneys, liver, and the hematopoietic system.

This is especially important for newborns, primarily premature, and young children.

Drug Interactions

With simultaneous use with probenecid or shortly before it, the renal excretion of sulbactam is competitively slowed down, so increased plasma concentrations of sulbactam may persist for a longer period of time.

Sulbactam in combination with beta-lactam antibiotics does not cause interactions that were not observed with the use of the beta-lactam antibiotic alone.

All interactions reported in combination with sulbactam are possible interactions of the antibiotic.

Sulbactam is pharmaceutically incompatible with the following drugs and therefore must be administered separately: aminoglycosides, metronidazole, injectable tetracycline derivatives (doxycycline), sodium thiopental, prednisolone, procaine 2%, suxamethonium chloride, and norepinephrine.

Signs of pharmaceutical incompatibility are precipitation, cloudiness, discoloration of the solution.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°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.