Grapezone S

Grapezone S Uses, Dosage, Side Effects, Food Interaction and all others data.

Ceftriaxone is a sterile, semisynthetic, broad-spectrum, 3rd generation cephalosporin antibiotic for intravenous or intramuscular administration. The bactericidal activity of Ceftriaxone results from inhibition of cell wall synthesis. Ceftriaxone has a high degree of stability in the presence of beta-lactamases both penicillinases and cephalosporinases of gram-negative and gram- positive bacteria.

Ceftriaxone is a cephalosporin/cephamycin beta-lactam antibiotic used in the treatment of bacterial infections caused by susceptible, usually gram-positive, organisms. Ceftriaxone has in vitro activity against gram-positive aerobic, gram-negative aerobic, and anaerobic bacteria. The bactericidal activity of ceftriaxone results from the inhibition of cell wall synthesis and is mediated through ceftriaxone binding to penicillin-binding proteins (PBPs). Ceftriaxone is stable against hydrolysis by a variety of beta-lactamases, including penicillinases, and cephalosporinases and extended-spectrum beta-lactamases. However, resistance to ceftriaxone usually occurs through beta-lactamase hydrolysis, altered PBPs, or reduced bacterial cell permeability. Ceftriaxone should not be mixed with or giving in the same IV line as diluents/products containing calcium as they may cause ceftriaxone to precipitate. Ceftriaxone use may also cause biliary sludge or gallbladder pseudolithiasis.

Sulbactam is a β-lactamase inhibitor given in combination with β-lactam antibiotics to inhibit β-lactamase, an enzyme produced by bacteria that destroys antibiotic activity.

Grapezone S
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Grapezone S
Generic	Ceftriaxone + Sulbactam
Type	Injection
Therapeutic Class
Manufacturer	Alna Biotech
Available Country	India
Last Updated:	September 19, 2023 at 7:00 am

Uses

Ceftriaxone is used for the treatment of the following infections when caused by susceptible organisms:

Lower Respiratory Tract Infections caused by Streptococcus pneumoniae, Staphylococcus aureus, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella pneumoniae, E. coli, Enterobacter aerogenes, Proteus mirabilis, Serratia marcescens.

Acute Bacterial Otitis Media caused by Streptococcus pneumoniae, Haemophilus influenzae (including beta-lactamase producing strains), Moraxella catarrhalis (including beta-lactamase producing strains).

Skin and Skin Structure Infections caused by Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pyogenes, Viridans group streptococci, E. coli, Enterobacter cloacae, Klebsiella oxytoca, Klebsiella pneumoniae, Proteus mirabilis, Morganella morganii, Pseudomonas aeruginosa, Serratia marcescens, Acinetobacter calcoaceticus, Bacteroides fragilis, Peptostreptococcus species.

Urinary Tract Infections (complicated and uncomplicated) caused by E. coli, Proteus mirabilis, Proteus vulgaris, Morganella morganii, Klebsiella pneumoniae.

Uncomplicated Gonorrhea (cervical, urethral, pharyngial and rectal) caused by Neisseria gonorrhoeae, including both penicillinase- and nonpenicillinase-producing strains, and pharyngeal gonorrhea caused by nonpenicillinase-producing strains of Neisseria gonorrhoeae.

Pelvic Inflammatory Disease caused by Neisseria gonorrhoeae.

Bacterial Septicemia caused by Staphylococcus aureus, Streptococcus pneumoniae, E. coli, Haemophilus influenzae, Klebsiella pneumoniae.

Bone and Joint Infections caused by Staphylococcus aureus, Streptococcus pneumoniae, E. coli, Proteus mirabilis, Klebsiella pneumoniae, Enterobacter species.

Intra-abdominal Infections caused by E. coli, Klebsiella pneumoniae, Bacteroides fragilis, Clostridium species, Peptostreptococcus species.

Meningitis caused by Haemophilus influenzae, Neisseria meningitidis, Streptococcus pneumoniae. Ceftriaxone has also been used successfully in a limited number of cases of meningitis and shunt infection caused by Staphylococcus epidermidis and E. coli.

Surgical Prophylaxis: The preoperative administration of a single 1 gm dose of Ceftriaxone may reduce the incidence of postoperative infections in patients undergoing surgical procedures classified as contaminated or potentially contaminated.

Sulbactam is an beta-lactamase inhibitor antibiotic combined with other antibiotics to treat a variety of susceptible bacterial infections.

Sulbactam is currently available in combination products with ampicillin. Within this formulation it is indicated for the treatment of infections due to susceptible strains of the designated microorganisms in the conditions listed below. Skin and Skin Structure Infections caused by beta-lactamase producing strains of Staphylococcus aureus, Escherichia coli, Klebsiella spp. (including K. pneumoniae), Proteus mirabilis, Bacteroides fragilis, Enterobacter spp., and Acinetobacter calcoaceticus. Intra-Abdominal Infections caused by beta-lactamase producing strains of Escherichia coli, Klebsiella spp. (including K. pneumoniae), Bacteroides spp. (including B. fragilis), and Enterobacter spp. Gynecological Infections caused by beta-lactamase producing strains of Escherichia coli, and Bacteroides spp. (including B. fragilis).

How Grapezone S works

Ceftriaxone works by inhibiting the mucopeptide synthesis in the bacterial cell wall. The beta-lactam moiety of ceftriaxone binds to carboxypeptidases, endopeptidases, and transpeptidases in the bacterial cytoplasmic membrane. These enzymes are involved in cell-wall synthesis and cell division. Binding of ceftriaxone to these enzymes causes the enzyme to lose activity; therefore, the bacteria produce defective cell walls, causing cell death.

Sulbactam is an irreversible inhibitor of β-lactamase; by binding and inhibiting β-lactamase produced by bacterial cells, sulbactam is thereby able to prevent it from reducing antibiotic activity. Although sulbactam alone possesses little useful antibacterial activity, except against the Neisseriaceae, whole organism studies have shown that sulbactam restores ampicillin activity against beta-lactamase producing strains. In particular, sulbactam has good inhibitory activity against the clinically important plasmid mediated beta-lactamases most frequently responsible for transferred drug resistance. The presence of sulbactam in formulations with ampicillin effectively extends the antibacterial spectrum of ampicillin to include many bacteria normally resistant to it and to other beta-lactam antibacterials. Thus, products with ampicillin + sulbactam possess the properties of a broad-spectrum antibacterial and a beta-lactamase inhibitor.

Dosage

Grapezone S dosage

Generally, Ceftriaxone should be taken once or equally devided twice a day for 4-14 days. Ceftriaxone therapy should be continued for at least 2 days after the sign and symptoms of infection have disappeared.

The usual duration of therapy is 4 to 14 days; in complicated infections longer therapy may be required. No dosage adjustment is required for patients with renal or hepatic impairment.

Use the solution immediately after reconstitution of powder.

Side Effects

Generally Ceftriaxone is well tolerated. However, few side effects including nausea, vomiting, diarrhea, dizziness and fever may occur.

Toxicity

Ceftriaxone overdose may increase the risk of urolithiasis and subsequent post-renal acute renal failure (PARF). Other symptoms of overdose unavailable in the literature. However, they are likely similar to the adverse effects of the medication. If overdose of ceftriaxone occurs, treat with symptomatic and supportive treatment, as ceftriaxone levels will not be reduced by dialysis.

Precaution

Ceftriaxone should be administered with caution to individuals with a history of gastrointestinal disease, particularly colitis.

Interaction

May increase nephrotoxicity of aminoglycosides. May diminish therapeutic effect of BCG, typhoid vaccine, Na picosulfate. May increase anticoagulant effect of vit K antagonists (e.g. warfarin). May increase serum level with probenecid.

Volume of Distribution

The apparent volume of distribution of an intravenous or intramuscular dose in healthy patients is 5.78 to 13.5 L. The volume of distribution of an intravenous or intramuscular dose in septic patients is 6.48 to 35.2 L. Ceftriaxone has good enough CSF penetration to be used as an effective treatment of bacterial meningitis.

Penetration of both ampicillin and sulbactam into cerebrospinal fluid in the presence of inflamed meninges has been demonstrated after IV administration.

Elimination Route

Ceftriaxone is only given as an injection, either intramuscularly or intravenously. Ceftriaxone is less than 1% bioavailable if given orally.

Peak serum concentrations are reached almost immediately following a 15-minute intravenous infusion of sulbactam + ampicillin. Mean peak serum levels for sulbactam range from 48 to 88 mcg/mL following intravenous administration of 2000 mg of ampicillin plus 1000 mg sulbactam. After an intramuscular injection of 1000 mg ampicillin plus 500 mg sulbactam, peak sulbactam serum levels ranging from 6 to 24 mcg/mL are attained.

Half Life

The elimination half-life of ceftriaxone is 5.8-8.7 hours. The half-life of ceftriaxone in the middle ear fluid has been estimated to be 25 hours.

~1 hr

Clearance

The plasma clearance of ceftriaxone in healthy adults receiving a 0.15-3g dose is 0.58 to 1.45 L/hour. The renal clearance of ceftriaxone is 0.32 to 0.73 L/hour. In intensive care unit patients, ceftriaxone's total drug clearance was 0.96L/h (0.55-1.28 L/h), and unbound drug clearance was 1.91 L/h (1.46-6.20 L/h).

Elimination Route

Ceftriaxone is primarily eliminated in the urine (33-67%). The remainder is eliminated through secretion in the bile and removed from the body via the feces.

Approximately 75 to 85% of both ampicillin and sulbactam are excreted unchanged in the urine during the first 8 hours after administration.

Pregnancy & Breastfeeding use

Pregnancy: The safety of Ceftriaxone in the treatment of infections during pregnancy has not been established. Ceftriaxone should only be used during pregnancy if the likely benefit outweighs the potential risk to the fetus and/or the mother.

Lactation: Ceftriaxone is excreted in breast milk at low concentrations. Therefore, caution should be exercised when Ceftriaxone is administered to a nursing mother.

Contraindication

Ceftriaxone should not be given to patients with a history of hypersensitivity to cephalosporin antibiotics. It is contraindicated in premature infants during the first 6 weeks of life. Its safety in human pregnancy has not been established. Ceftriaxone is contraindicated in neonates if they require (or are expected to require) treatment with calcium-containing IV solutions, including continuous calcium containing infusions such as parenteral nutrition because of the risk of precipitation of ceftriaxone-calcium.

Acute Overdose

There is no specific antidote. Treatment of over dosage should be symptomatic.

Storage Condition

Store below 25°C, protected from light & moisture. Use reconstituted solutions immediately.

Reconstituted solutions are stable for 6 hours at room temperature and for 24 hours at 2°-8°C. It should not be mixed in the same syringe with any drug other than 1% Lidocaine Hydrochloride injection BP (for IM injection only).