Mesporin TM. Ceftriaxone sodium. Rapid onset, sustained action, for a broad spectrum of infections

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1 Ceftriaxone sodium Rapid onset, sustained action, for a broad spectrum of infections

2 1, 2, 3 Antibiotic with a broad spectrum of activity Broad spectrum of activity against gram-positive* and gram-negative bacteria Plasma concentrations > MIC**, *** Good tissue penetration (measurable in over 60 tissues and tissue fluids) 1 Therapeutic action sustained for over 24 hours 1 Micro-organisms Median values MIC 50 a (mg/l) MIC 90 b (mg/l) Staphylococcus aureus (met-s) 4 4 Staphylococcus, coagulase-negative 4 16 Streptococcus pyogenes (ß-haemolytic, group A) Streptococcus pneumoniae Escherichia coli Haemophilus influenzae Klebsiella pneumoniae Moraxella catarrhalis Pseudomonas spp a: MIC 50 = Minimal Inhibitory Concentration for 50% of tested strains b: MIC 90 = Minimal Inhibitory Concentration for 90% of tested strains After administration of 1 2 g ceftriaxone, concentrations above the MIC for most pathogens are measured for more than 24 hours in over 60 tissues and fluids, including lung, heart, biliary tract, liver, middle ear, nasal mucous membranes and bones, as well as cerebrospinal, pleural, synovial and prostate fluids. * Most of Gram + bacteria ** Minimal Inhibitory Concentration *** After 1 2 g ceftriaxone administration (intravenous or intramuscular)

1, 2, 3 Established efficacy in many infections Respiratory tract infections Renal and urinary tract infections Genital tract infections (including gonorrhea)

3 1, 2, 3 Established efficacy in many infections Respiratory tract infections Renal and urinary tract infections Genital tract infections (including gonorrhea) Abdominal infections (including gastrointestinal tract) Sepsis Meningitis Infections of the bones, joints, soft tissues, skin and wounds in outpatient or hospital setting 2, 4

4 1, 2, 3 Established efficacy in many infections Urinary tract infections* Cephalosporin comparative efficacy (IM or IV) 3 Ceftriaxone (1 to 2 g 1 x/day) Ceftrizoxime (2 g 2x/day) Cefotaxime (1 to 2 g 2x/day) Cefazolin (1 g 3x/day) 78% 72% 66% 62% % Ceftriaxone once daily is as efficacious as other standard cephalosporins administered in several divided doses daily 3 Bacterial meningitis Cure rates following once daily IV or IM administration of ceftriaxone 80 to 100 mg/kg in neonates, infants or children with bacterial meningitis 3 Bacteriological cure Clinical cure 92% 100% % CSF** culture sterile patients (%) Bacteriological cure: sterile CSF** found in 95% of the patients within 24 hours after treatment, and in 100% of the patients within 48 hours after treatment 3 Clinical cure: resolution of fever and meningeal signs 3 Impressive clinical and bacteriological cure rates (92 100%) following once daily ceftriaxone treatment (IV or IM) 3 * In patients with (i) acute and complicated, or (ii) severe or complicated urinary tract infection (UTI) ** Cerebrospinal fluid

coli 75% 75% 100% 100% 100% 100% 0 10 20 30 40 50 60 70 80 90 100 % Ceftriaxone alone,

5 Community-acquired respiratory tract infections Bacterial eradication (%) 3 S. aureus P. mirabilis H. influenzae S. pneumoniae K. pneumoniae E. coli 75% 75% 100% 100% 100% 100% % Ceftriaxone alone, administered once daily, is effective in eradicating pathogens in patients with pneumonia or exacerbated chronic bronchitis, including elderly patients 3

6 Once-a-day therapy 3, 5 Effective ceftriaxone plasma concentration over 24 hours*, 5 after IV administration Plasma concentration (μg/ml) adapted from 5 Average plasma concentrations of ceftriaxone 2.0 g ceftriaxone I.V. 1.0 g ceftriaxone I.V. 0.5 g ceftriaxone I.V. n = 12 healthy volunteers 0 30 min hours Maximum plasma concentrations of ceftriaxone are achieved within 30 minutes after administration High binding to plasma proteins ensures long-lasting plasma concentrations Concentrations remain above MIC 50 for 24 hours **, ***, 1, 2, 3, 6 Longer half-life than with any other cephalosporin**** Half-life (hours) Cefotiam Cefmenoxime Cefotaxime Cefoperazone Cefsulodine Ceftazidime Ceftizoxime Latamoxef Ceforanide Cefotetan Cefonicide Ceftriaxone Half-life of various cephalosporins 6 An unusually long elimination half-life for ceftriaxone allows for its administration once a day only 6 * Mean values ** MIC 50 : Minimal concentration to achieve 50% inhibition *** For most of the micro-organisms **** In healthy adults

7 A wide distribution 3 Broad and good tissue and body fluid penetration 1, 2, 6 A dual mode of elimination Renal filtration Biliary excretion 50 60% 40 50%, 1, 3, 6 No dosage adjustment necessary in* Patients with renal insufficiency** Patients with hepatic insufficiency*** Elderly patients * In adult. For a paediatric use, please refer to the SmPC. ** Provided that the hepatic function is normal. *** Provided that the renal function is normal. In renal insufficiency with a reduced creatinine clearance <10 ml/min the daily dose of ceftriaxone should not exceed 2 g in adult patients.

9 Ceftriaxone sodium A full range for all ages*, 1 Adults (including elderly patients) and adolescents aged over 12 years or with a body weight > 50 kg: 1 to 2 g once daily. Up to 4 g/day in case of severe infections or infections caused by moderately sensitive micro-organisms Children (aged between 15 days and 12 years): 20 to 80 mg/kg/day Newborn infants (aged between 0 and 14 days): 20 to 50 mg/kg/day** * Normal dosage ** Not to exceed 50 mg/kg

10 Ceftriaxone sodium Rapid onset, sustained action, for a broad spectrum of infections 1, 2, 3 Antibiotic with a broad spectrum of activity 1, 2, 3 Established efficacy in many infections Once-a-day therapy (IV or IM) 3, 5 1, 3, 6 No dosage adjustment necessary A full range for all ages 1 Reduced injection-associated pain due to lidocaine (for IM injection) 1 References 1 Summary of Product Characteristics (SmPC) 2 Bijie H. et al: In vitro activity, pharmacokinetics, clinical efficacy, safety and pharmacoeconomics of ceftriaxone compared with third and fourth generation cephalosporins: review. J Chemother. 2005; 17(1): Brogden R. et al: A reappraisal of its antibacterial activity and pharmacokinetic properties, and an update on its therapeutic use with particular reference to once-daily administration. Drugs. 1988; 35: Duncan C. et al: Outpatient parenteral antimicrobial therapy with ceftriaxone, a review. Int J Clin Pharm. 2012; 34(3): Patel M. et al: Pharmacokinetics of ceftriaxone in humans. Antimicrob Agents Chemother. 1981; 20(5): Singlas E.: Pharmacocinetique clinique de la ceftriaxone. Medecine et Maladies Infectieuses. 1989; 19: 8 15 Composition: active ingredient is ceftriaxone. 500/1000 IM consists of a vial containing 500 or 1000 mg ceftriaxone as powder and a vial (2 ml solvent or 5 ml water for injection, respectively) containing 1% lidocaine; 500/1000 IV consists of a vial containing 500 or 1000 mg ceftriaxone and a vial of 5 ml or 10 ml, respectively, of water for injection; 2000 IM consists of a vial containing 2000 mg ceftriaxone as powder. Indications and dosage: is a bactericidal agent, it inhibits bacterial wall synthesis of several Gram-negative and Gram-positive bacteria. is indicated for (1) treatment of respiratory tract infections, abdominal infections, renal/urinary tract infections, genital infections, sepsis, meningitis, disseminated Lyme borreliosis, and infections of bone, joints, soft tissues, skin, wounds and in immunocompromised patients, and (2) prophylactic treatment of perioperative infection, in cases of potential or established contamination, of GI, biliary and urogenital tracts. is given to adults and children aged >12 years or weighing >50 kg: 1 2 g/day and up to 4 g/d in severe infection or in infection by moderately-susceptible pathogens; in neonates aged 14 days: mg/kg/day; infants and children aged 15 days 12 years: mg/kg/day. Contraindications: Hypersensitivity to cephalosporins or penicillin; neonates with hyperbilirubinemia, neonates under parenteral calcium treatment; premature infants. Precautions: (i) is not to be mix with calcium-containing solutions before administering (ii) in neonates, calcium-containing solutions should not be administered within 48 hours of last dose (iii) risk of fatal anaphylactic reactions with outcomes, of thromboplastin time prolongation (such as in cases of vitamin K deficiency), of pancreatitis, of immune-mediated haemolytic anaemia ( should be stopped until cause is clarified), of CDAD, of proliferation of non-sensitive pathogens (iv) in long-term use, regular blood count monitoring is required (v) ultrasound investigations may show mistaken evidence of gall bladder stones, possibly due to precipitated ceftriaxone-calcium salts (vi) caution in patients with renal impairment, with concomitant aminoglycosides and diuretics, and when driving or using machinery (vii) treatment to be stopped if anaemia develops. Pregnancy/lactation: It is recommended not to use during the first trimester of pregnancy, unless absolutely needed, or during breast-feeding. Undesirable effects: Eosinophilia, leukopenia, granulocytopenia, haemolytic anaemia, thrombocytopenia, thromboplastin time prolongation; loose stools/diarrhoea, nausea, vomiting, stomatitis, glossitis; exanthema, allergic dermatitis, pruritus, urticaria, oedema; elevated serum liver enzymes; in children: symptomatic precipitation of calcium salt of ceftriaxone in the gall bladder, reversible cholelithiasis. Interactions: should not be administered with other chloramphenicol, aminoglycosides or bacteriostatic agents. Prior to administration, should not be mixed with amsacrine, vancomycin, fluconazole or any calcium-containing solutions. Presentation: -500/1000 IM are packs of 1x 15 ml vial of ceftriaxone disodium powder with 1 ampoule of 1% lidocaine HCl solution; -500/1000 IV are packs of 1x 15 ml vial of ceftriaxone disodium powder with 1 ampoule of water for injection IV are packs of 1 vial of ceftriaxone disodium powder. Since indications, dosage forms and strengths may vary from country to country, please consult your local prescribing information. Full prescribing information, details and literature references are available on request. Latest update of information: February AC.R/05.13/EN/V1/MES/01 Acino Pharma AG Aesch Switzerland Phone Fax info@acino-pharma.com

Aciphin Ceftriaxone Sodium

Aciphin Ceftriaxone Sodium Only for the use of Medical Professionals Description Aciphin is a bactericidal, long-acting, broad spectrum, parenteral cephalosporin preparation, active against a wide range