SERTOCEF

TRADE NAME

Sertocef

INTERNATIONAL NONPATENTED NAME

Ceftriaxone

 

CHEMICAL NAME

Ceftriaxone (as salt sodium)

Disodium (6R,7R)-7-[[(2Z)-(2- aminothiazol -4-yl)(methoxyimino)acetyl]amino]-3-[[(2-methyl-6-oxido-5-oxo-2,5-dihydro-1,2,4- triazin-3-yl)sulphanyl] methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2- carboxylate 3.5 hydrate

 

DOSAGE FORM

Powder for solution for injections

Description: Almost white or yellowish coloured, partially hygroscopic, crystalline powder.

 

COMPOSITION

Sertocef 0.5 g

1 vial contains

Active ingredient: ceftriaxone (as ceftriaxone sodium) 0.5 g.

 

Solvent (for dosage form with solvent):       

2 mL of 1% lidocaine hydrochloride solution.

 

Sertocef 1.0 g

1 vial contains

Active ingredient: ceftriaxone (as ceftriaxone sodium) 1.0 g.

 

Solvent (for dosage form with solvent):       

3.5 mL of 1% lidocaine hydrochloride solution.

 

ATC CODE        J01DD04

 

PHARMACOTHERAPEUTIC GROUP

Systemic antibacterials, third-generation cephalosporins.

     

PHARMACOLOGICAL PROPERTIES

PHARMACODYNAMICS

Sertocef is a broad-spectrum antibiotic of III generation cephalosporins. It has a bactericidal action by means of synthesis inhibition of bacteria cell membranes. It is active against most gram-negative, many gram-positive causative microorganisms and some anaerobes. It is resistant to beta-lactamases produced by bacteria.

Aerobic gram-negative bacteria that are sensitive to the drug are the following: Aeromonas spp., Alcaligenes spp., Branhamella catarrhalis, Citrobacter spp., Enterobacter spp. (some strains are resistant), E.coli, Haemophilus ducreyi, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella spp. (including Kl. pneumoniae), Moraxella spp., Morganella morganii, Neisseria gonorrhoeae, Neisseria meningitidis, Plesiomonas shigelloides, Proteus mirabilis, Proteus vulgaris, Providencia spp., Pseudomonas aeruginosa (some strains are resistant), Salmonella spp. (including S. typhi), Serratia spp. (including S. marcescens), Shigella spp., Vibrio spp. (including V. cholerae), Yersinia spp. (including Y. enterocolitica).

Many strains of the above mentioned microorganisms that steadily proliferate in presence of other antibiotics, for example, penicillins, first- and second-generation cephalosporins and aminoglycosides, are sensitive to Sertocef. According to clinical data, good drug efficacy is observed during primary and secondary syphilis.

Aerobic gram-positive bacteria, sensitive to Sertocef are the following: Streptococcus agalactiae, Staphylococcus aureus (including penicillinase-producing strains), Streptococcus bovis, Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus viridans.

Methicillin-resistant Staphylococcus spp. is also resistant to cephalosporins, including Sertocef. Most strains of  Enterococcus spp. (e.g., Streptococcus faecalis) are also resistant to the drug.

Anaerobic causative microorganisms are as follows: Bacteroides spp. (including some strains of В. fragilis), Clostridium spp. (including Cl. difficile), Fusobacterium spp. (except for F. mortiferum and F. varium), Peptococcus spp., Peptostreptococcus spp. Some strains of Bacteroides spp. (e.g., В. fragilis) producing beta-lactamase are resistant to Sertocef.

PHARMACOKINETICS

Sertocef for intramuscular/intravenous administration penetrates well into tissues and body fluid. Bioavailability after intramuscular administration is 100%. Peak plasma concentration after intramuscular administration is reached in 2-3 hours. It is reversibly bound to plasma albumin by 85-95%, and this binding is in inverse proportion to its concentration in blood.

Sertocef quickly diffuses in the interstitial fluid, where it maintains its bactericidal action against sensitive microorganisms for 24 hours. The half-life is long, and it is about 8 hours in adults, it approximately twice longer in elderly people older than 75 years, and it is 6.5-8 days in neonates.

In adults, 50-60% of Sertocef is excreted unchanged in urine, 40-50% - in bile. In neonates, approximately 70% of the injected dose is excreted by the kidneys. In adults with renal or hepatic dysfunctions, Sertocef is almost unchanged (insignificant prolongation of the half-life period is possible), due to redistribution of functions: if the renal function is impaired the excretion in bile is increased, and if renal pathology occurs the excretion by the kidneys is increased.

Ceftriaxone crosses well the blood-brain barrier.    

 

THERAPEUTIC INDICATIONS

Sertocef is effective against all infections caused by bacterial strains sensitive to the drug:

- sepsis;

- inflammation of cerebral meninges (bacterial meningitis, including in neonates);

- infections of abdominal cavity organs (peritonitis, infections of bile passages, including cholangitis, gallbladder empyema and other gastrointestinal tract infections);

- infections of bones and joints, maxillofacial infections;

- infections of skin and soft tissues, infected wounds and burns;

- prophylaxis and treatment of infections in patients with compromised immunity (including those with neutropenia and oncological diseases);

- renal and urinary tract infections (uncomplicated and complicated, including pyelitis, acute and chronic pyelonephritis, cystitis, prostatitis, epididymitis);

- respiratory tract infections (acute and chronic bronchitis, pneumonia, lung abscess, pleural empyema, bronchiectases, etc.);

- infections of ENT organs (mastoiditis, otitis media, etc.);

- sexually-transmitted infections (including gonorrhea);

- prior surgical interference in order to prevent infections.

 

 

 

 

POSOLOGY AND METHOD OF ADMINISTRATION

Sertocef is injected intramuscularly and intravenously by stream or drop infusions.

Rules for the drug preparation and injection

For intramuscular injection:

Dissolve 500 mg Sertocef in 2 mL of 1% lidocaine hydrochloride solution,

Dissolve 1 g Sertocef in 3.5 mL of 1% lidocaine hydrochloride solution.

Inject deeply in the glute. It is recommended to inject not more than 1 g in one clunis.

For intravenous injection:

Dissolve 500 mg Sertocef in 5 mL of water for injections,

dissolve 1 g Sertocef in 10 mL of water for injections.

Inject slowly in vein for 2-4 munites.

 

The prepared solution for injection of Sertocef 0.5 g or 1.0 g should be used within 24 hours when stored at 2°С - 8°С or within 6 hours when stored at 15°С - 25°С.

 

Neonates (up to 2-week age): Sertocef is prescribed in a dose of 20-50 mg/kg bw once a day. The dose exceeding is unacceptable due to immaturity of enzyme system in neonates. 

For infants and children under 12 years old: daily dose of Sertocef is 20-80 mg/kg bw once a day. Usual doses for adults are used in children with body weight 50 kg and more.

Adults and children older than 12 years: 1 g once a day (every 24 hours). In serious cases or during infections caused by bacteria with only moderate sensitivity to ceftriaxone, daily dose is 2 - 4 g.

The treatment duration depends on the nature and seriousness of disease. As with other antibiotics, Sertocef administration is recommended to continue at least for 3 days after body temperature normalization.

Intravenous injection of the drug in a dose of more than 50 mg/kg bw must be performed by drop infusion for not less than 30 minutes.

In bacterial meningitis, the drug is given in initial dose of 100 mg/kg bw once a day to neonates and children. Maximum daily dose is 4 g. After causative agent identification, the dose can be reduced.

During gonorrhoea treatment, the recommended dose is 250 mg Sertocef for single intramuscular injection.

It is not necessary to reduce the drug dose in patients with renal dysfunction provided that hepatic function is normal and in patients with hepatic dysfunction provided that renal function is normal. In case of pronounced renal insufficiency (creatinine clearance <10 ml/min), Sertocef dose must not exceed 2 g a day.

In case of concurrent hepatic and renal dysfunction, and also in patients undergoing hemodialysis, serum ceftriaxone concentration should be regularly controlled.

For prophylaxis of postoperative infections it is recommended a single injection of 1-2 g Sertocef for 30-90 minutes before operation. In colorectal surgery, 2 g should be given intramuscularly, in conjunction with a suitable agent active against anaerobic bacteria.

 

CONTRAINDICATIONS

- known hypersensitivity to cephalosporins and penicillins;

- concurrent administration with calcium-containing infusions, due to the risk of ceftriaxone calcium precipitation;

- neonates with hyperbilirubinemia;

- premature neonate aged up to 41 weeks old (a weeks of pregnancy + weeks of life);

- neonates aged up to 28 days old, born with jaundice, hyperbilirubinemia or acidosis.

Contraindications for lidocaine should also be considered if lidocaine is used as a solvent (intramuscular injection).

 

SIDE EFFECTS

In most cases Sertocef is well tolerated. Side effects are usually reversible and disappear after the drug withdrawal.

From digestive system: nausea, vomiting, diarrhea or constipation, flatulence, abdominal pains, taste disorder, stomatitis, glossitis, pseudomembranous enterocolitis, incresed activity of hepatic transaminases (more seldom – alkaline phosphatase, bilirubin, cholestatic jaundice), dysbacteriosis. Ceftriaxone administration in high doses can lead to pseudocholelytiasis development.

Hematologic changes: leukopenia, neutropenia, granulocytopenia, lymphocytopenia, thrombocytosis, thrombocytopenia, hemolytic anemia, coagulation failure, elongation of prothrombin time, rare – eosinophilia, individual cases of agranulocytosis.

From urinary system: glucosuria, increase in urea and creatinine in blood plasma, cylindruria, haematuria, oliguria, anuria.

Allergic and immunopathological reactions: urticaria, chills and fever, rash, pruritus, rare - bronchospasm, erythema multiform, Stevens Johnson's syndrome, toxic epidermal necrolysis, serum disease, angioneurotic edema, anaphylactic shock.

Local reactions: possible development of phlebitis after intravenous injection of the drug. It can be avoided when the drug is injected slowly (for 2-4 minutes); intramuscular injection without lidocaine is painful, it is possible the formation of infiltrate at injection site.

Other: headache, dizziness, nasal hemorrhage, candidiasis.

 

SPECIAL INDICATIONS

As with other cephalosporins, it is necessary to take into account the possibility of anaphylactic reactions during Sertocef treatment.

Regular control of peripheral blood picture is required during a long-term treatment with the drug.

In rare cases during ultrasonic diagnosis it is possible the occurrence of gall bladder obscuration, which disappears after the drug cancellation. If this sign is accompanied by pains in right hypochondrium, it is recommended to continue drug administration on background of symptomatic treatment.

Each gram of Sertocef contains approximately 3.6 mmol sodium. It should be taken into consideration by patients on a controlled sodium diet.

 

INFLUENCE ON ABILITY FOR DRIVING AND OPERATING WITH MECHANISMS

No data on Sertocef influence on ability for driving and operating with mechanisms are available. But one should keep in mind the possibility of dizziness during the drug therapy.

 

ADMINISTRATION DURING PREGNANCY AND LACTATION

Sertocef administration during pregnancy is possible only if potential benefit to the mother outweighs any potential risk to the fetus (ceftriaxone crosses the placental barrier).

If it is necessary to administer the drug during lactation period it should be decided on breastfeeding cancellation, as ceftriaxone is excreted in breast milk.

 

INTERACTION WITH OTHER DRUGS

In case of concurrent administration with loop diuretics (e.g., furosemide), renal dysfunction is not observed.

In concurrent administration with nonsteroidal antiinflammatory drugs and other inhibitors of platelet aggregation the probability of hemorrhage is increased.

Sertocef and aminoglycosides exert synergistic effects against many gram-negative bacteria. Such combination is justified during treatment of serious and life threatening infections (e.g., caused by such causative microorganism as Pseudomonas aeruginosa).

Sertocef should not be mixed in one vial or in a syringe with other antibiotics.

 

OVERDOSE

No data on the drug overdose are available.

 

PACKAGING

Sertocef 0.5 g or 1.0 g No. 1 with a solvent

0.5 g or 1.0 g powder for solution for injections in a vial together with a solvent.

1 vial with powder for solution for injections and 1 ampoule with solvent in a carton box with enclosed leaflet.

 

Sertocef 0.5 g or 1.0 g No. 10

0.5 g or 1.0 g powder for solution for injections in a vial.

10 vials in a contour tray.

1 contour tray in a carton box with enclosed leaflet.

 

STORAGE CONDITIONS

Sertocef 0.5 g or 1.0 g No. 1 with a solvent (1% lidocaine hydrochloride solution)

Store in a protected from light place at temperature 15ºС - 25ºС.

Keep out of reach of children!

Constituted solution is stable within 24 hours at temperature 2°С - 8°С or 6 hours at temperature 15°С - 25°С.

 

Sertocef 0.5 g or 1.0 g No. 10

Store in a protected from light place at temperature 15ºС - 25ºС.

Keep out of reach of children!

 

SHELF LIFE

3 years from the date of manufacture.

Do not apply after the expiry date.

 

SALES TERMS

Sold under prescription.

 

MANUFACTURER

The holder of Marketing Authorization is

“DR SERTUS İLAÇ SAN. VE TİC. LTD. ŞTİ.”, TURKEY.

Manufactured by

“PharmaVision Sanayi ve Ticaret A.Ş.”, Turkey

(Davutpaşa Caddesi No.145, Topkapı, İstanbul).