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Cefepime & Tazobactam for Injection
Each combi pack contains:
(a) 1 Vial of Cefepime & Tazobactam for Injection

Each vial contains:
Cefepime Hydrochloride IP (Sterile) eq. to Cefepime 1.0g, 2.0 gm
(Buffered with L-Arginine)
Tazobactam Sodium (Sterile) eq. to Tazobactam 125 mg, 250 mg
(b) 1 Ampoule of Sterile Water for Injections IP

Each ampule contains:
Sterile Water for Injections IP 10 ml

Dosage Form: Injection

Description: Cefepime Hydrochloride and Tazobactam Sodium is a combination. Cefepime is a semi-synthetic fourth generation Cephalosporin antibiotic with Tazobactam. Tazobactam a beta-lactamase inhibitor, is a synthetic penicillinase sulfone containing a beta-lactam ring derived from 6-aminopenicillanic acid. Although Tazobactam has minimal antibacterial activity when used alone the combined use of Cefepime with Tazobactam results in a synergistic effect that expands the spectrum of activity of Cefepime against many strains of beta-lactamase producing bacteria.

Anti-microbial Spectrum:

Based on the spectrum of activity and decreased susceptibility to certain beta-lactamases. Cefepime is classified as a FOURTH generation Cephalosporin. Its-activity includes coverage against most gram negative bacteria which are susceptible to third generation Cephalosporins. The drug is also active against some gram negative organisms including Pseudomonas aeruginosa and certain Enterobacteriaceae, that generally are resistant to most third generation Cephalosporins. The activity of Cefepime against Pseudomonas aeruginosa is similar to that of Ceftazidime. However, Cefepime is more active in-vitro against some strains of gram-positive bacteria eg. Staphylococci than some third generation Cephalosporins.

Zwitter-ion of Cefepime enhances movement across the cell membrane resulting in high concentration in the periplasmic space and relatively not resistance to drug hydrolysis and Cefepime exhibits only modest inactivation.

Emergence of drug resistance to Cefepime was considered as less of problem till recently. Extended spectrum beta-lactamases (ESBL) are beta-lactamases capable of hydrolyzing penicillin, broad and extended spectrum Cephalosporins.

ESBL can be found in a variety of Enterobacteriaceae species K. pneumoniae, K.oxytoca and Esch. coli. Other organisms to harbor ESBL are Enterobacter spp., Salmonella spp., Morganella morganii, Proteus mirabilis, Serratia marcescens and Pseudomonas aeruginosa.

Cefepime is active against most ESBL producing organisms however susceptibility appears to decrease with increasing inoculums in vitro susceptibility tests and in vivo experimental models.

Use of Cefepime alone has been associated with selection of ESBL producing organisms and outbreaks of infection.

Tazobactam generally acts as an irreversible inhibitor inactivates both plasmid and chromosomally mediated beta-lactamases. ESBL are inhibited by Tazobactam. Therefore combination of Cefepime with Tazobactam is a useful combination for the treatment of infection due to ESBL producing organisms. Tazobactam augments and protects Cefepime, the powerful fourth generation Cephalosporin.

Pharmacodynamic Properties

Mechanism of Action

Cefepime is a bactericidal agent that acts by inhibition of bacterial cell wall synthesis. Cefepime has a broad spectrum in vitro activity that encompasses a wide range of gram-positive and Gram negative bacteria. Cefepime has a low affinity for chromosomally encoded beta lactamases. Cefepime is highly resistant to hydrolysis by most beta lactams and exhibits rapid penetration in to gram-negative bacterial cells. Within bacterial cells, the molecular targets of Cefepime are the penicillin-binding proteins (PBP). Tazobactam sodium has little critically relevant in vitro activity against bacteria due to its reduced affinity to penicillin binding proteins. It is, however, a b inhibitor of the Richmond-Sykes class III (Bush class 2b & 2b) penicillinases and cephalosporinases. Tazobactam does not induce chromosomally-mediated b-lactamases at tazobactam concentrations achieved with the recommended dosage regimen.

Pharmacokinetics:

Cefepime exhibits linear dose dependent pharmacokinetics over the dosage range 250 mg to 2 g and there is no evidence of drug accumulation following multiple doses in healthy adults with normal renal function.

Cefepime is almost completely absorbed following IM administration. The single 500 mg, 1 g or 2 g IM doses of Cefepime attains 13.9, 29.6 or 57.5 mcg/ml respectively. Peak plasma concentration is attained within 1.4 – 1.8 hrs. After 8 hours the average plasma concentration averaged 1.9, 4.5 or 8.7 mcg/ml respectively.

Following IV infusion over 30 min of a single 500 mg, 1 g or 2 g doses, Cefepime peak plasma concentrations of the drug averaged 31.6 –29.1, 65.9 – 81.7 or 126 -139.9 mcg/ml respectively, plasma concentrations 8 hours after the dose averaged 1.4, 2.4 and 3.9 mcg/ml respectively.

Following parenteral administration Cefepime is widely distributed into tissues and fluids, including blister fluid, bronchial mucosa, sputum, bile, peritoneal fluid, appendix, and gall-bladder. Cefepime is distributed into CSF following parenteral administration. It is also excreted in human milk.

Cefepime is approximately 20% bound to serum proteins. Plasma half-life of Cefepime averages 2 – 2.3 hours. Cefepime is partially metabolized in vivo to N-methyl pynolidine (NMP). The drug is eliminated principally unchanged in urine by glomerular filtration; 80 – 82% of a single dose of Cefepime is excreted unchanged in urine.

Cefepime is removed by haemodialysis and peritoneal dialysis.

Tazobactam 0.5 g when infused over 30 min as a single dose, the peak serum level averages 27.1 mcg/ml, the terminal half life is 0.67 hour and its renal clearance is 268 ml per min.

Indications:

For the treatment of uncomplicated and complicated UTI, uncomplicated skin and skin structure infections, and complicated intra-abdominal infections; LRTI including nosocomial pneumonia & bronchitis; septicemia; empiric treatment in febrile neutropenic patients.

Contraindications:

Cefepime and Tazobactam are contraindicated in patients who are hypersensitive to the drugs or other cephalosporins and should be used with caution in patients with a history of hypersensitivity to penicillins. Use of Cephalosporins should be avoided in patients who have had an immediate type (anaphylactic) hypersensitivity reaction to penicillins. If a hypersensitivity reaction occurs during Cefepime and Tazobactam therapy, the drug should be discontinued and the patient treated with appropriate therapy e.g. epinephrine, corticosteroids and maintenance of an adequate airway and oxygen is indicated.

Warning: Before therapy with Cefepime and Tazobactam for Injection is instituted, careful inquiry should be made to determine whether the patient has previous immediate hypersensitivity reaction to Cefepime, Cephalosporins, Penicillins or other drugs.

Precautions: Pediatric: Safety and efficacy of Cefepime in pediatric age group 2 months to 12 years has been established.

Pregnancy: There are no adequate or controlled studies using Cefepime and Tazobactam in pregnant women or during labor and delivery and the drug should be used during pregnancy only when clearly indicated.

Lactation: Cefepime is distributed into milk in low concentration following parenteral administration and the drug should be used with caution in nursing mothers.

Adverse effects: Adverse effects with Cefepime and Tazobactam are similar to those reported with Cefepime alone and generally are transient and mild to moderate in severity.

Local reactions: Phlebitis, pain and inflammation at the site of injection.

Systemic reactions: Diarrhea, fever, headache, nausea, vomiting, oral moniliasis, skin rash, pruritus, urticaria, and vaginitis.

Dosage:

Cefepime and Tazobactam preferably is administered by IV infusion but also can be given by deep IM injection when indicated. Cefepime with Tazobactam should be administered intravenously over 30 minutes.

The recommended adult and pediatric dosage of Cefepime and Tazobactam are outlined in the following table:

Recommended dosage schedule for Cefepime and Tazobactam (expressed as Cefepime)

SITE AND TYPE OF INFECTION DOSE FREQUENCY DURATION (Days)
Moderate to severe pneumonia 1 – 2 g IV Every 12 h 10
Empiric therapy for febrile neutropenic patients 2 g /IV Every 8 h 7
Mild to moderate urinary tract infections (uncomplicated and complicated) 500 mg – 1 gm IV or IM Every 12 h 7 – 10
Mild to moderate infections including bronchitis, skin and skin-structure infections 1 gm IV or IM Every 12 h 10
Severe infections including pneumonia, urinary tract infections, complicated intra-abdominal infections, including cases with an associated bacteremia 2 gm IV Every 12 h 10
Intra-abdominal infection 2 gm IV Every 12 h 7 – 10

 

Pediatric patients (2 months to 12 years):

The maximum dose for pediatric patients should not exceed recommended adult dose. The usual recommended dose for pediatric patients is 40 to 50 mg/kg dose administered 8 to 12 hours depending on the severity of infection.

Constitution and administration:

IV Infusion: The contents of vials should be constituted with 10 ml of sterile water for injections provided. The appropriate dose of the drug should then be added to a compatible IV solution. The resultant solutions are stable for 24 hours when stored at room temperature of 20-25° C.

Storage condition:- Store below 30° C. Protect from light & moisture. Do not freeze. Keep medicine out of reach of children.

Packaging Information: Specipime 1.125 g, 2.25 g Injection is available in vial packed mono carton with Sterile Water for Injections IP.

Description: Doxycycline is used to treat many different bacterial infections, such as acne, urinary tract infections, intestinal infections, eye infections, gonorrhea, chlamydia, periodontitis (gum disease).

Pharmacology: Doxycycline inhibits bacterial protein synthesis by binding to the 30S ribosomal subunit. Doxycycline has bacteriostatic activity against a broad range of Gram -positive and Gram-negative bacteria. Cross-resistance of these organisms to tetracycline is common.

Pharmacodynamics:

Bacteria3 Minimal Inhibitory Concentration (mcg/mL) Zone Diameter (mm) Agar Dilution (mcg/mL)
S I R S I R S I R
Acinetobacter spp.
  Doxycycline ≤ 4 8 ≥ 16 ≥ 13 10-12 ≤ 9
  Tetracycline ≤ 4 8 ≥ 16 ≥ 15 12-14 ≤ 11
Anaerobes
  Tetracycline ≤ 4 8 ≥ 16
Bacillus anthracisb
  Doxycycline ≤ 1
  Tetracycline ≤ 1
Brucella speciesb
  Doxycycline ≤ 1
  Tetracycline ≤ 1
Enterobacteriaceae
  Doxycycline ≤ 4 8 ≥ 16 ≥ 14 11-13 ≤ 10
  Tetracycline ≤ 4 8 ≥ 16 ≥ 15 12 -14 ≤ 11
Francisella tularensisb
  Doxycycline ≤ 4
  Tetracycline ≤ 4
Haemophilus influenzae
  Tetracycline ≤ 2 4 ≥ 8 ≥ 29 26-28 ≤ 25
Mycoplasma pneumoniaeb
  Tetracycline ≤ 2
Nocardiae and other aerobic Actinomyces speciesab
  Doxycycline ≤ 1 2-4 ≥ 8
Neisseria gonorrhoeaec
  Tetracycline ≥ 38 31-37 ≤ 30 ≤ 0.25 0.5-1 ≥ 2
Streptococcus pneumoniae
  Doxycycline ≤ 0.25 0.5 ≥ 1 ≥ 28 25-27 ≤ 24
  Tetracycline ≤ 1 2 ≥ 4 ≥ 28 25-27 ≤    24
Vibrio cholerae
  Doxycycline ≤ 4 8 ≥ 16
  Tetracycline ≤ 4 8 ≥ 16
Yersinia pestis
  Doxycycline ≤ 4 8 ≥ 16
  Tetracycline ≤ 4 8 ≥ 16
Ureaplasma urealyticum
  Tetracycline ≤ 1 ≥ 2
a Organisms susceptible to tetracycline are also considered susceptible to doxycycline. However, some organisms that are intermediate or resistant to tetracycline may be susceptible to doxycycline

 Pharmacokinetics: Doxycycline–metal ion complexes are unstable at acid pH, therefore more doxycycline enters the duodenum for absorption than the earlier tetracycline compounds. In addition, food has less effect on absorption than on absorption of earlier drugs with doxycycline serum concentrations being reduced by about 20% by test meals compared with 50% for tetracycline

 Dosage

Adults: The usual dose of doxycycline is 200 mg loading dose(administered 100 mg every 12 hours), followed by a maintenance dose of 100 mg OD(For severe infections 100mg Bid).

For children above eight years of age: In  Children <45kg loading dose is 4mg/kg/day and main tenance dose is 2mg/kg/day.

Indications:

Stability:

Doxycycline is stable for 4hrs in solution when diluted with sodium chloride Injection,or 5%dextrose Injection to concentrations between 1mg/ml and 0.1mg/ml  and stored at 25°c.Doxycycline in these solutions is stable under flourescent light for 4hrs.but must be protected from direct sunlight during storage and infusion if refrigerated and protected from sunlight and artificial light.Infusion must then be completed within 4hrs.Solutions must be used within these time periods or discarded.

When diluted with Lactated Ringer’s Injection,or Dextrose 5%in   Lactated Ringer’s Infusion of the solution(ca 1mg/ml)or lower concentrations.(not less than 0.1mg/mL)must be completed within 4hrs after reconstitution into adequate stability.During infusion ,solution must be protected from direct sunlight.Solutions must be used within time period or discarded.

Parenteral drug products should be inspected visually for particulate matter and discoloration when ever solution and container permit.

Contraindications:

The drug is contraindicated in persons who have shown hypersensitivity to any of the tetracyclines.

Adverse Effects:

An erythematous rash in sun-exposed parts of the body has been reported to occur in 7.3–21.2% of persons taking doxycycline for malaria prophylaxis. One study examined the tolerability of various malaria prophylactic regimens and found doxycycline did not cause a significantly higher percentage of all skin events (photosensitivity not specified) when compared with other antimalarials. The rash resolves upon discontinuation of the drug.

Unlike some other members of the tetracycline group, it may be used in those with renal impairment. Doxycycline is contraindicated in the pediatric treatment of acute bacterial rhinosinusitis.

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