Antibiotic Portfolio

Antibiotic Portfolio

 

Antibiotic Portfolio:

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Presentation : Inj Amoxicillin & Potassium Clavulanate 1.2g Vial

Description : Is combination of amoxicillin and the beta-lactamase inhibitor, clavulanate potassium (the potassium salt of clavulanic acid).

Indications : In Upper & lower respiratory tract infections, sinusitis, complicated urinary tract infections, and skin and skin Structure infections, Surgical prophylaxis.

Contra-Indications : Allergy to penicillins and cephalosporins. Safety in pregnancy has not been established. Amonic is contra-indicated in patients with a previous history of Amonic -associated jaundice/hepatic dysfunction. Safety and efficacy in children has not been established with the parenteral forms of Amonic.

Storage : Store in a cool & dry place, below 25°C. Do not freeze. Keep out of reach of children.

Description: Ampitrust is an injectable antibacterial combination consisting of the semisynthetic antibacterial ampicillin sodium and the beta-lactamase inhibitor sulbactam sodium for intravenous and intramuscular administration

Pharmacology:

Mode of Action

Ampicillin/sulbactam is a combination of a β-lactam antibiotic and a β-lactamase inhibitor. Ampicillin works by binding to penicillin-binding proteins (PBPs) to inhibit bacterial cell wall synthesis This causes disruption of the bacterial cell wall and leads to bacterial cell death. However, resistant pathogens may produce β-lactamase enzymes that can inactivate ampicillin through hydrolysis.This is prevented by the addition of sulbactam, which binds and inhibits the β-lactamase enzymes

Pharmacokinetics:

Half-Life: 1.2-1.5 hr
Protein Bound: 38%
Distribution: bile, blister & tissue fluids
Metabolism: liver
Excretion: urine

Pharmacodynamics:

Quality control ranges for ampicillin/sulbactam disk diffusion and MIC determinations

Disk Diffusion (Zone diameter in mm) MIC (mcg/mL ampicillin/ mcg/mL sulbactam)
E. coli (ATCC 25922) 19-24 2/1-8/4
S. aureus (ATCC 25923) 29-37 Not applicable
E. coli (ATCC 35218) 13-19 8/4-32/16
H.influenza (ATCC 49247) 14-22 2/1-8/4

Indications:

Dosage:

The recommended adult dosage of Ampicillin/Sulbactam is 1.5 g (1 g ampicillin as the sodium salt plus 0.5 g sulbactam as the sodium salt) to 3 g (2 g ampicillin as the sodium salt plus 1 g sulbactam as the sodium salt) every six hours. This 1.5 to 3 g range represents the total of ampicillin content plus the sulbactam content of Ampicillin/sulbactam and corresponds to a range of 1 g ampicillin/0.5 g sulbactam to 2 g ampicillin/1 g sulbactam. The total dose of sulbactam should not exceed 4 grams per day

Dosage Guide for Patients with Renal Impairment

Creatinine Clearance (mL/min/1.73m²) Ampicillin/Sulbactam Half-Life (Hours) Recommended UNASYN Dosage
≥ 30 1 1.5-3 g q 6h-q 8h
15-29 5 1.5-3 g q 12h
5-14 9 1.5-3 g q 24h

Stability:

Reconstitution of Ampicillin and Sulbactam for Injection, at the specified concentrations, with these diluents provide stable solutions for the time periods indicated in the following table: (After the indicated time periods, any unused portions of solutions should be discarded.)

Stability
Diluent Maximum Concentration (mg/mL)
ampicillin and sulbactam
Use Periods
Sterile Water for Injection 45 (30/15) 8 hrs @ 25°C
45 (30/15) 48 hrs @ 4°C
30 (20/10) 72 hrs @ 4°C
5% Dextrose Injection 30 (20/10) 2 hrs @ 25°C
30 (20/10) 4 hrs @ 4°C
3 (2/1) 4 hrs @ 25°C
Lactated Ringer’s Injection 45 (30/15) 8 hrs @ 25°C
45 (30/15) 24 hrs @ 4°C
5% Dextrose in 0.45% Saline 3 (2/1) 4 hrs @ 25°C
15 (10/5) 4 hrs @ 4°C

 

Adverse Events

Storage: Store below 30°C.Protect from light and moisture.Do not freeze.

Presentation :
Inj Meroreach /Merofit is available in 500mg & 1g Injection.

Description
Meropenem is an ultra-broad-spectrum injectable antibiotic used to treat a wide variety of infections. It is a β-lactam and belongs to the subgroup of carbapenem, similar to imipenem and ertapenem.  penetrates well into many tissues and body fluids, including cerebrospinal fluidbileheart valvelung, and peritoneal fluid.

Indications:

Contraindications
Lesion of the Brain, Kidney Disease, Clostridium Difficile Bacteria Related Colitis, Seizures, Decreased Blood Platelets

Storage
Store in a cool, dry place. Protect from light.

Presentation :Inj Sulbactam 1g, 2g Vials

Description :Addbactam ( Sulbactam) is an irreversible inhibitor of beta-lactamase; It binds the enzyme and does not allow it to interact with the antibiotic. Sulbactam has intrinsic antimicrobial activity against A. baumannii and is the most active of the β-lactamase inhibitors.

Indications : Beta lactamase resistant pseudomonas, Gynecological infections, Intra-abdominal infections, Methicillin resistant staphylococci, skin infections.

Contra-Indications : Addbactam Injection including IM/IV Injectable Powder should not be used in known hypersensitivity situations against Beta lactam antibiotic combinations.

Storage : Store in a dry & dark place, below 25°C. Do not freeze. Keep out of reach of children.

Description: Imipenem/Cilastatin I.V. (Imipenem and Cilastatin for Injection) is a sterile formulation of imipenem (a thienamycin antibiotic) and cilastatin sodium (the inhibitor of the renal dipeptidase, dehydropeptidase l), with sodium bicarbonate added as a buffer. Imipenem/Cilastatin I.V. is a potent broad spectrum antibacterial agent for intravenous administration

Pharmacology

Mode of Action: Imipenem/Cilastatin is a potent inhibitor of bacterial cell wall synthesis and is bactericidal against a broad spectrum of pathogens—gram-positive and gram-negative, aerobic and anaerobic.

Pharmacokinetics: Absorption Bioavailability (IM): imipenem, 60–75%; cilastatin, 95–100%

Distribution: The drug is distributed rapidly and widely to most tissues and fluids, including sputum, pleural fluid, peritoneal fluid, interstitial fluid, bile, aqueous humor, reproductive organs, and bone; highest concentrations occur in pleural fluid, interstitial fluid, peritoneal fluid, and reproductive organs; low concentrations occur in CSF; it crosses the placenta, and enters breast milk

Protein binding: Imipenem, 13–21%; cilastatin, 40%

Metabolism: Imipenem is metabolized in the kidney by dehydropeptidase 1; activity is blocked by cilastatin.

Elimination: Half-life (both drugs): 60 min; prolonged with renal impairment Excretion (both drugs): Urine (~70% as unchanged drug)

Pharmacodynamics: In vitro tests show imipenem to act synergistically with aminoglycoside antibiotics against some isolates of Pseudomonas aeruginosa. Table 1: Susceptibility Interpretive Criteria for Imipenem

Pathogen Minimum Inhibitory Concentrations MIC (mcg/mL) Disk Diffusion Zone Diameter (mm)
S I R S I R
Enterobacteriaceae ≤ 1 2 ≥ 4 ≥ 23 20 to 22 ≤ 19
Pseudomonas aeruginosa ≤ 2 4 ≥ 8 ≥ 19 16 to 18 ≤ 15
Acinetobacter spp. ≤ 4 8 ≥ 16 ≥ 16 14 to 15 ≤ 13
Staphylococcus spp. ≤ 4 8 ≥ 16 ≥ 16 14 to 15 ≤ 13
Haemophilus influenzae and H. parainfluenzae ≤ 4 - - ≥ 16 - -
Streptococcus pneumoniae ≤ 0.12 0.25 to 0.5 ≥ 1 - - -
Anaerobes ≤ 4 8 ≥ 16 - - -

Indications Imipenem/Cilastatin. is indicated for the treatment of serious infections as listed below:

  1. Lower respiratory tract infections (including severe pneumonia [hospital and ventilator-associated pneumonia as well])
  2. Urinary tract infections (complicated and uncomplicated)
  3. Intra-abdominal infections (including complicated infections)
  4. Gynaecological infections (including intra- and post-partum infections)
  5. Bacterial septicaemia
  6. Bone and joint infections
  7. Skin and skin structure infections (including complicated infections)
  8. Endocarditis
  9. Polymicrobic infections, including those in which S. pneumoniae (pneumonia, septicaemia), S. pyogenes (skin and skin structure), or non-penicillinase-producing S. aureus is one of the causative organisms. However, monobacterial infections due to these organisms are usually treated with narrower spectrum antibiotics, such as penicillin G.

Dosage and Administration: Table 1: I.V. dosage schedule for adults with normal renal function and body weight ≥70 kg

Type or severity of infection  Fully susceptible organisms, including gram-positive and gram-negative aerobes and anaerobes  Moderately susceptible organisms, primarily some strains of Pseudomonas aeruginosa
Mild 250 mg q6h (total daily dose = 1.0 g) 500 mg q6h(total daily dose =2.0 g)
Moderate 500 mg q8h (total daily dose = 1.5 g) or 500 mg q6h (total daily dose = 2.0 g) 500 mg q6h (total daily dose = 2.0 g) or 1 g q8h (total daily dose = 3.0 g)
Severe, life threatening only 500 mg q6h (total daily dose = 2.0 g) 1 g q8h (total daily dose = 3.0 g) or 1 g q6htotal daily dose = 4.0 g)
Uncomplicated urinary tract infection 250 mg q6h (total daily dose = 1.0 g) 250 mg q6h (total daily dose = 1.0 g)
Complicated urinary tract infection 500 mg q6h (total daily dose = 2.0 g) 500 mg q6h (total daily dose = 2.0

Due to the high antimicrobial activity of Imipenem/Cilastatin  I.V., it is recommended that the maximum total daily dosage not exceed 50 mg/kg/day or 4.0 g/day, whichever is lower.

Compatibility and Stability:

Before Reconstitution The dry powder should be stored at a temperature below 25°C (77°F).

Reconstituted Solutions Solutions of IMIPENEM/CILASTATIN  I.V. range from colourless to yellow. Variations of colour within this range do not affect the potency of the product. IMIPENEM/CILASTATIN I.V., reconstituted with 0.9% Sodium Chloride Injection, maintains satisfactory potency for 4 hours at room temperature or for 24 hours under refrigeration (2-8°C). Solutions of IMIPENEM/CILASTATIN  I.V. should not be frozen.

Contraindications: IMIPENEM/CILASTATIN  is contraindicated in patients who have shown a hypersensitivity to any component of this product or to any other carbapenem antibacterial agent and other beta-lactam agents.

Local Adverse Reactions: Adverse local clinical reactions that were reported as possibly, probably, or definitely related to therapy with Cila Safe I.V. were:

Storage: Store below 25°C.

Presentation: IVDAPT  is supplied in single-use vials containing 350 mg daptomycin as a sterile, lyophilised powder. Single-use 10 mL capacity vial: Package of 1. 

Description: Daptomycin is a lipopeptide antibiotic used in the treatment of systemic and life-threatening infections caused by Gram-positive organisms. It is a naturally occurring compound found in the soil saprotroph Streptomyces roseosporus. Its distinct mechanism of action makes it useful in treating infections caused by multiple drug-resistant bacteria.

Indications Skin Infections,Staphylococcus aureus infections(Endocarditis) Complicated skin and skin structure infection

Contraindications: CUBICIN is contraindicated in patients with known hypersensitivity to daptomycin

Storage: Store in original packages at refrigerated temperatures of between 2° to 8°C; avoid excessive heat.

Molecule: Inj. Ceftriaxone

Class : Broad spectrum cephalosporins

Strengths Available: 250mg, 500mg, 1g

Approved indications :  Lower respiratory tract infections, Skin and Skin structure infections, Urinary tract infections,  Uncomplicated Gonorrhea, Pelvic inflammatory disease, Bacterial septicemia, Bone and Joint infections, Intra-Abdominal infections, Meningitis and surgical prophylaxis.

MoA:  Futri  is an antimicrobial agent Inhibits bacterial cell wall synthesis by binding to one or more of the penicillin-binding proteins (PBPs) which in turn inhibits the final trans-peptidation step of peptidoglycan synthesis in bacterial cell walls, thus inhibiting cell wall biosynthesis.

Futri has a high degree of stability in the presence of beta-lactamases, both penicillinases and cephalosporinases, of gram-negative and gram-positive bacteria.

Method Of Administration:

Dosage:

Indication Adult Children
Lower respiratory tract Infections 1-2 g  given once a day or equally divided doses twice a day 50-75 mg /(not to exceed 2g ) given once day or in divided doses   every 12 hours
Urinary tract infections 1-2 g  given once a day or equally divided doses twice a day 50-75 mg /(not to exceed 2g ) given once day or in divided doses   every 12 hours
  Skin & skin structure infections 1-2 g  given once a day or equally divided doses twice a day 50-75 mg /(not to exceed 2g ) given once day or in divided doses   every 12 hours
Uncomplicated Gonorrhoea Single IM dose of 250 mg               –
Bone & Joint Infections 1-2 g  given once a day or equally divided doses twice a day 50-75 mg /(not to exceed 2g ) given once day or in divided doses   every 12 hours
Meningitis 100mg /kg/day up to 4g 50-75 mg /(not to exceed 2g ) given in divided doses   every 12 hours
Surgical prophylaxis Single dose of 1 g  ½- 2 hours before surgery

Contra –indications : 

Presentation :Inj Sulbactam 1g, 2g Vials

Description :Addbactam ( Sulbactam) is an irreversible inhibitor of beta-lactamase;
It binds the enzyme and does not allow it to interact with the antibiotic. Sulbactam has intrinsic antimicrobial activity against A. baumannii and is the most active of the β-lactamase inhibitors.

Indications : Beta lactamase resistant pseudomonas, Gynecological infections, Intra-abdominal infections, Methicillin resistant staphylococci, skin infections.

Contra-Indications : Addbactam Injection including IM/IV Injectable Powder should not be used in known hypersensitivity situations against Beta lactam antibiotic combinations.

Storage : Store in a dry & dark place, below 25°C. Do not freeze. Keep out of reach of children.

Presentation : Inj. Chromatographically Purified-Vancomycin 500mg and 1g Vials

Description :
Indications : MRSA, Patients not responding to penicillins or cephalosporins, Endocarditis, Septicemia, Bone infections, Lower respiratory tract infections.

Contra-Indications : Vancomycin is contraindicated in patients with known hypersensitivity to this antibiotic.

Storage : Prior to reconstitution, store dry powder at 20 °-25 ° C .

Cefoperazone and Sulbactam for Injection – 1:1 & 2:1
Razone 1g & 2g (Cefoperazone 500 mg – Sulbactam 500 mg & Cefoperazone 1 g – Sulbactam 1 g)
Razone ES 1.5gm (Cefoperazone 1 gm- Sulbactam 500 mg & Cefoperazone 2 gm – Sulbactam 1 gm)

Each Vial Contains:
Sterile Cefoperazone Sodium IP …..Eq. to Cefoperazone 1g & 2 gm
Sterile Sulbactam Sodium USP ……..Eq. to Sulbactam 0.5 g & 1 gm
Powder for reconstitution (IV/IM use only)

DESCRIPTION :
Cefoperazone sodium is a semisynthetic broad-spectrum cephalosporin antibiotic for parenteral use only. Sulbactam sodium is a derivative of the basic penicillin nucleus. It is an irreversible beta-lactamase inhibitor for parenteral use only. The Sulbactum Sodium and Cefoperazone Sodium combination consists of a beta-lactamase inhibitor plus a beta-lactam. This sulbactam /cefoperazone combination is available as a dry powder for reconstitution.

CLINICAL PHARMACOLOGY:

Pharmacodynamics
The anti-bacterial component of sulbactam/cefoperazone is cefoperazone, a third generation cephalosporin, which acts against sensitive organisms during the stage of active multiplication by inhibiting biosynthesis of cell wall mucopeptide.

Sulbactam does not possess any useful antibacterial activity, except against Neisseriaceae and Acinetobacter. Sulbactam is a penicillanic acid sulfone with beta-lactamase inhibitory properties. Sulbactam attaches to certain penicillin binding proteins (PBP) and increases the susceptibility to sulbactam/cefoperazone than to cefoperazone alone.

The combination of sulbactam and cefoperazone is active against all organisms sensitive to cefoperazone. In addition it demonstrates synergistic activity (up to fourfold reduction in minimum inhibitory concentrations for the combination versus those for each component) in a variety of gram positive and gram negative  and anaerobic organisms.

PHARMACOKINETICS
Absorption: The mean serum concentration obtained at 30 min after 1 g I.V. Cefoperazone is 114 mcg/ml. The mean serum concentration obtained at 15 min. after 500 mg and 1000 mg IV Sulbactam are 21- 40 mcg/ml and 48-88 mcg/ml respectively. The average peak plasma concentration at 5 minutes after intravenous dose of 1g is 81mg/litre.

Distribution: The protein binding of Cefoperazone is 82-93% and that of Sulbactam is 38%.

Metabolism and Excretion: No significant quantity of metabolites of Cefoperazone has been found in the urine. Cefoperazone is excreted mainly in the bile. About 75-85% of Sulbactam is excreted in the urine during the first eight hours of administration.

Changes in PK parameters in special population group:

Renal Insufficiency: No significant differences have been observed in the pharmacokinetics of in renally failure patients comparing to the normal patients.

Hepatic Insufficiency: Cefoperazone is extensively excreted in bile. The serum half-life of cefoperazone is usually prolonged and urinary excretion of the drug increased in patients with hepatic diseases and/or biliary obstruction.

INDICATIONS:

Mono-therapy

Sulbactam/cefoperazone is indicated for the treatment of the following infections when caused by susceptible organisms:

Combination Therapy

Combination Therapy Because of the broad spectrum of activity of Sulbactum/ Cefoperazone, most infections can be treated adequately with this antibiotic combination alone. However, Sulbactum/Cefoperazone may also be used concomitantly with other antibiotics if such combinations are indicated. If an aminoglycoside is used, renal function should be monitored during the course of therapy.

DOSAGE AND ADMINISTRATION

Adults: The usual adult dose of the combination is 2 to 4 g/day (i.e, 1-2 g/day each of Cefoperazone and Sulbactam) given IV or IM in equally divided doses every 12 hours. In severe or refractory infections the daily dosage may be increased to 8g (i.e, 4g/day each of Cefoperazone and Sulbactam) given IV in equally divided doses every 12 hours. The recommended maximum daily dosage of Sulbactam is 4g (8g of the combination).

Children: The usual dosage in children is 40-80mg/kg/day (20 to 40 mg/kg/day each of Cefoperazone and Sulbactam) every six to twelve hours. In serious or refractory infections, these dosages may be increased up to 240mg/kg/day (160 mg/kg/day cefoperazone activity). Doses should be administered in two to four equally divided doses.

Use in Neonates: For neonates in the first week of life, the drug should be given every 12 hours. The maximum daily dosage of sulbactam in paediatrics should not exceed 80 mg/kg/day.

Renal Impairment: Dosage regimens of sulbactam/cefoperazone should be adjusted in patients with a marked decrease in renal function (creatinine clearance of less than 30 mL/min) to compensate for the reduced clearance of sulbactam. Patients with creatinine clearances between 15 and 30 mL/min should receive a maximum of 1 g of sulbactam every 12 hours (maximum daily dosage of 2 g sulbactam), while patients with creatinine clearances of less than 15 mL/min should receive a maximum of 500 mg of sulbactam every 12 hours (maximum daily dosage of 1 g sulbactam). The pharmacokinetic profile of sulbactam is significantly altered by haemodialysis. The serum half-life of cefoperazone is reduced slightly during haemodialysis. Thus, dosing should be scheduled to follow a dialysis period.

Hepatic Impairment: Cefoperazone is extensively excreted through the bile. Dose modification may be necessary in cases of severe biliary obstruction, severe hepatic disease or in cases of renal dysfunction coexistent with either of those conditions. In such cases, dosage should not exceed 2 g/day of cefoperazone without close monitoring of serum concentrations.

CONTRAINDICATIONS

It is contraindicated in patients with a known allergy to penicillins, sulbactam, cefoperazone, or any of the cephalosporins.

WARNINGS AND PRECAUTIONS

Serious and occasionally fatal hypersensitivity (anaphylactic) reactions have been reported in patients receiving beta-lactam or cephalosporin therapy. These reactions are more apt to occur in individuals with a history of hypersensitivity reactions to multiple allergens. If an allergic reaction occurs, the drug should be discontinued and the appropriate therapy instituted. As with other antibiotics, overgrowth of non-susceptible organisms may occur during the prolonged use of Sulbactum/Cefoperazone. It has not been extensively studied in premature infants or neonates. Therefore, in treating premature infants and neonates, the potential benefits and possible risks involved should be considered before instituting therapy.

Drug Interactions: A reaction characterized by flushing, sweating, headache and tachycardia has been reported when alcohol was ingested during and as late as the fifth day after Cefoperazone administration. A similar reaction has been reported with certain other cephalosporins and patients should be cautioned concerning ingestion of alcoholic beverages in conjunction with administration of Sulbactum/ Cefoperazone. For patients requiring artificial feeding orally or parenterally, solutions containing ethanol should be avoided.

Hepatic Impairment: In severe hepatic dysfunction, therapeutic concentrations of Cefoperazone are obtained in the bile and only a 2-to 4-fold increase in the half-life is seen. Dose modification may be necessary in case of severe biliary obstruction, severe hepatic disease or in case of renal dysfunction coexistent with either of those conditions.

Pregnancy: There are no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.

Lactation: Caution should be exercised when Sulbactum/Cefoperazone is administered to a nursing mother.

SIDE EFFECTS

Sulbactam/cefoperazone is generally well-tolerated. The majority of adverse events are of mild or moderate severity and are tolerated with continued treatment. The most frequent side effects observed with Sulbactum/Cefoperazone have been gastrointestinal. Others include dermatologic reactions, headache, injection pain, chills, and anaphylactoid reactions.

OVERDOSAGE

Limited information is available on the acute toxicity of Cefoperazone Sodium and Sulbactum Sodium in humans. Overdosage of the drug would be expected to produce manifestations that are principally extensions of the adverse reactions reported with the drug.

INTRAVENOUS ADMINISTRATION

Reconstitution: For intravenous infusion, each vial of Sulbactum/Cefoperazone should be reconstituted with the appropriate amount of 5% Dextrose, 0.9% Sodium Chloride Injection or Sterile Water for Injection, then further diluted to 20 mL with the same solution, and followed by administration over 15 to 60 minutes. Lactated Ringer’s Solution is a suitable vehicle for intravenous infusion, but it is not, however, for initial reconstitution. For intravenous injection, each vial should be reconstituted as above and administered over a minimum of 3 minutes.

INTRAMUSCULAR ADMINISTRATION

Lidocaine HCl 2% is a suitable vehicle for intramuscular administration; however, it is not for initial reconstitution.

INCOMPATIBILITY

Aminoglycosides: Solutions of sulbactam/cefoperazone and aminoglycosides should not be directly mixed, since there is a physical incompatibility between them .

Lactated Ringer’s Solution: should be avoided since this mixture has been shown to be incompatible. However, a two-step dilution process involving initial reconstitution in Sterile Water for Injection will result in a compatible mixture when further diluted with Lactated Ringer’s Solution.

STORAGE AND HANDLING INSTRUCTIONS

Store below 25°C. Protect from light. Keep out of reach of children Reconstituted Solution Reconstituted solution is stable for 7 days at 2-8°C and for 24 hours at 8-25°C. How supplied Glass vial with diluent in a carton

Ticarcillin is a carboxypenicillin . Because it is a penicillin, it also falls within the larger class of beta-lactam antibiotics. Its main clinical use is as an injectable antibiotic for the treatment of Gram-negative bacteria, particularly Pseudomonas aeruginosa. It is also one of the few antibiotics capable of treating Stenotrophomonas maltophilia infections.

PHARMACOLOGY

Mode of Action

Ticarcillin’s antibiotic properties arise from its ability to prevent cross-linking of peptidoglycan during cell wall synthesis, when the bacteria try to divide, causing cell death.

Ticarcillin, like penicillin, contains a β-lactam ring that can be cleaved by beta-lactamases, resulting in inactivation of the antibiotic. Those bacteria that can express β-lactamases are, therefore, resistant to β-lactam antibiotics. Due, at least in part, to the common β-lactam ring, ticarcillin can cause reactions in patients allergic to penicillin. Ticarcillin is also often paired with a β-lactamase inhibitor such as clavulanic acid (co-ticarclav).

Pharmacokinetics

Absorption

max is achieved immediately after completion of the infusion. C max is 330 mcg/mL (ticarcillin) and 8 to 16 mcg/mL (clavulanic acid). AUC is about 485 mcg•h/mL and about 8.2 mcg•h/mL for ticarcillin and clavulanic acid, respectively.

Distribution

The drugs are not highly protein bound (approximately 45% and 9% for ticarcillin and clavulanic acid, respectively). Ticarcillin/Clavulanate is detected in tissues and interstitial fluid following IV administration. Penetration into bile and pleural fluid has been demonstrated.

Elimination

Serum t ½ is about 1.1 h. Approximately 60% to 70% of ticarcillin and approximately 35% to 45% of clavulanic acid are excreted unchanged in urine during the first 6 h after a single dose.

Pharmacodynamics

Dilution Techniques: Quantitative methods are used to determine antimicrobial MICs. These MICs provide estimates of the susceptibility of bacteria to antimicrobial compounds. The MICs should be determined using a standardized procedure. Standardized procedures are based on a dilution method (broth or agar) or equivalent with standardized inoculum concentrations and standardized concentrations of ticarcillin/clavulanate potassium powder.

The recommended dilution pattern utilizes a constant level of 2 mcg/mL clavulanic acid in all tubes with varying amounts of ticarcillin. MICs are expressed in terms of the ticarcillin concentration in the presence of clavulanic acid at a constant 2 mcg/mL. The MIC values should be interpreted according to the following criteria:

In vitro synergism between Ticarcillin/Clavulanic acid and gentamicin, tobramycin, or amikacin against multiresistant strains of Pseudomonas aeruginosa has been demonstrated.

RECOMMENDED RANGES FOR TICARCILLIN/CLAVULANIC ACID SUSCEPTIBILITY TESTING*

For Pseudomonas aeruginosa:

MIC (mcg/mL) Interpretation
≤ 64 Susceptible (S)
≥ 128 Resistant (R)

For Enterobacteriaceae:

MIC (mcg/mL) Interpretation
≤ 16 Susceptible(S)
32-64 Intermediate(I)
≥ 128 Resistant(R)

For Staphylococci†:

MIC (mcg/mL) Interpretation
≤ 8 Susceptible(S)
≥ 16 Resistant(R)

*Expressed as concentration of ticarcillin in the presence of clavulanic acid at a constant 2 mcg/mL.
† Staphylococci that are susceptible to ticarcillin/clavulanic acid but resistant to methicillin/oxacillin must be considered as resistant.

Indications & Dosage

ticarcillin/clavulanate
injection, powder for reconstitution
(3g/100mg)/vial
(30g/1g)/bulk vial
ready-to-use IV solution
(3g/100mg)/100mL

Septicemia

Indicated for septicemia caused by beta-lactamase–producing isolates of Klebsiella spp, Escherichia coli, Staphylococcus aureus, or Pseudomonas aeruginosa
3.1 g IV q4-6hr

Lower Respiratory Infections

Indicated for lower respiratory infections caused by beta-lactamase–producing isolates of S. aureus, Haemophilus influenzae, or Klebsiella spp
3.1 g IV q4-6hr

Bone & Joint Infections

Indicated for bone and joint infections caused by beta-lactamase–producing isolates of S. aureus
3.1 g IV q4-6hr

Skin & Skin Structure Infections

Indicated for skin and skin structure infections caused by beta-lactamase–producing isolates of S. aureus, Klebsiella spp, or E. coli
3.1 g IV q4-6hr

Urinary Tract Infections

Indicated for UTIs (complicated or uncomplicated) caused by beta-lactamase–producing isolates of E. coli, Klebsiella spp, P. aeruginosa (or other Pseudomonas spp), Citrobacter spp, Enterobacter cloacae, Serratia marcescens, or S. aureus

3.1 g IV q4-6hr

Intra-abdominal Infections

Indicated for peritonitis caused by beta-lactamase–producing isolates of E. coli, K. pneumoniae, or Bacteroides fragilis group

3.1 g IV q4-6hr

Gynecologic Infections:

Indicated for endometritis caused by beta-lactamase–producing isolates of Prevotella melaninogenicus, Enterobacter spp (including E. cloacae), E. coli, Klebsiella pneumoniae, S. aureus, or Staphylococcus epidermidis

Dose based on ticarcillin component
Moderate: 200 mg/kg/day IV divided q4-6hr
Severe: 300 mg/kg/day IV divided q4hr

Renal Impairment:

Load: 3.1 g IV, THEN reduce maintenance dose based on creatinine clearance
CrCl 30-60 mL/min: 2 g q4hr
CrCl 10-30 mL/min: 2 g q8hr
CrCl <10 mL/min: 2 g q12hr
CrCl<10 mL/min & hepatic impairment: 2 g qDay
Peritoneal dialysis: 3 g q12hr
Hemodialysis: 2 g q12hr; supplement with 3 g after each dialysis session

Stability:

Store powder for injection at or below 75°F. Reconstituted solution is stable for up to 6 h if stored at room temperature (70° to 75°F) or up to 72 h if refrigerated (40°F). IV solution diluted (10 to 100 mg/mL) with lactated Ringer’s injection or sodium chloride injection may be stored for up to 24 h at room temperature, up to 4 days if refrigerated, or 30 days if frozen (0°F). IV solution diluted (10 to 100 mg/mL) with dextrose 5% injection may be stored for up to 24 h at room temperature, up to 3 days if refrigerated, or 7 days if frozen. Frozen diluted IV solutions must be used within 8 h of thawing. Do not refreeze thawed solutions. Store premixed, frozen solutions at or below 4°F. Thaw at room temperature (72°F) or in refrigerator (39°F). Do not force thaw by immersion in water baths or by microwave irradiation. Thawed solution is stable for 24 h at room temperature or 7 days if refrigerated. Do not refreeze thawed solutions.

Contraindications:

Ticarcillin/Clavulanic acid  is contraindicated in patients with a history of hypersensitivity reactions to any of the penicillins.

Adverse Reactions:

As with other penicillins, the following adverse reactions may occur:

Hypersensitivity Reactions:

Skin rash, pruritus, urticaria, arthralgia, myalgia, drug fever, chills, chest discomfort, erythema multiforme, toxic epidermal necrolysis, Stevens-Johnson syndrome, and anaphylactic reactions.

Central Nervous System:

Headache, giddiness, neuromuscular hyperirritability, or convulsive seizures.

Gastrointestinal Disturbances:

Disturbances of taste and smell, stomatitis, flatulence, nausea, vomiting and diarrhea, epigastric pain, and pseudomembranous colitis have been reported. Onset of pseudomembranous colitis symptoms may occur during or after antibiotic treatment.

Hemic and Lymphatic Systems:

Thrombocytopenia, leukopenia, neutropenia, eosinophilia, reduction of hemoglobin or hematocrit, and prolongation of prothrombin time and bleeding time.

Abnormalities of Hepatic Function Tests:

Elevation of serum aspartate aminotransferase (SGOT), serum alanine aminotransferase (SGPT), serum alkaline phosphatase, serum LDH, serum bilirubin. There have been reports of transient hepatitis and cholestatic jaundice—as with some other penicillins and some cephalosporins.

Renal and Urinary Effects:

Hemorrhagic cystitis, elevation of serum creatinine and/or BUN, hypernatremia, reduction in serum potassium, and uric acid.

Local Reactions:

Pain, burning, swelling, and induration at the injection site and thrombophlebitis with intravenous administration.

Available safety data for pediatric patients treated with Ticarcillin/Clavulanic acid demonstrate a similar adverse event profile to that observed in adult patients.

Drug Abuse And Dependence:

Neither abuse of nor dependence on Ticarcillin/Clavulanic acids  has been reported.

Storage: Store dry powder below 25°c.

Presentation :. Piract ( Piperacillin & Tazobactam ) available in 1.125 g, 2.25 g, 4.5 g Vials

Description : Piract (piperacillin and tazobactam for injection) is an injectable antibacterial combination product consisting of the semisynthetic antibiotic piperacillin sodium and the ß-lactamase inhibitor tazobactam sodium for intravenous administration.

Indications :Appendicitis, Peritonitis, Uncomplicated and complicated skin and skin structure infections , Postpartum endometritis or pelvic inflammatory disease , Community-acquired pneumonia (moderate severity only) , Nosocomial pneumonia (moderate to severe).

Contra-Indications : Patients with a history of allergic reactions to penicillins, cephalosporins or ß lactamase inhibitors.

Presentation: IVDAPT  is supplied in single-use vials containing 350 mg daptomycin as a sterile, lyophilised powder. Single-use 10 mL capacity vial: Package of 1. 

Description: Daptomycin is a lipopeptide antibiotic used in the treatment of systemic and life-threatening infections caused by Gram-positive organisms. It is a naturally occurring compound found in the soil saprotroph Streptomyces roseosporus. Its distinct mechanism of action makes it useful in treating infections caused by multiple drug-resistant bacteria.

Indications
Skin Infections,Staphylococcus aureus infections(Endocarditis)
Complicated skin and skin structure infection

Contraindications:
CUBICIN is contraindicated in patients with known hypersensitivity to daptomycin

Storage: Store in original packages at refrigerated temperatures of between 2° to 8°C; avoid excessive heat.

Presentation : Inj. Promistin ( Colistimethate sodium) available in 1 M IU/ml, 2 M IU/ml, 3 M IU/ml Vials

Description : Colistimethate sodium is a cyclic polypeptide antibiotic derived from Bacillus polymyxa var. colistinus and belongs to the polymyxin group.

Indications :

Contra-Indications : Hypersensitivity to colistimethate sodium (colistin) or to polymyxin B. Patients with myasthenia gravis.

Storage : Store below 25C. Protected from light.

JECTOPHEN INJECTION
1 g/Vial (lyophilized powder)

COMPOSITION:
Each vial contains Chloramphenicol Sodium Succinate equivalent to 1 g Chloramphenicol.

MECHANISM OF ACTION & PHARMACOKINETICS:
Chloramphenicol is a broad spectrum antibiotic which was first isolated from cultures of Streptomyces venezuelae but is now produced synthetically. It acts by interfering with bacterial protein synthesis by binding reversibly to the 50S ribosomal subunit. It’s action is mainly bacteriostatic. Chloramphenicol sodium succinate is partially hydrolysed to free chloramphenicol in the liver, lungs and kidneys. It is inactivated in the liver and approximately 30% is excreted unchanged in the urine. Chloramphenicol has a half life range of 4 hours and about 50% in the circulation is bound to plasma protein. Chloramphenicol enters the cerebrospinal fluid, even in the absence of meningitis, giving concentrations of about 60% of those existing in the blood. It crosses the placenta into the foetal circulation, into breast milk and into the aqueous and vitreous humours of the eye.

INDICATIONS:
Typhoid fever and other types of systemic salmonella infections. (not the carrier state).

Bacterial meningitis caused by Haemophilus influenzae; Anaerobic infections caused by bacteroides species especially B.fragilis, such as foci in the pelvis or bowel, or brain abscesses.

Rickettsial diseases –drug of choice in severely ill patients e.g. in diseases like Rocky Mountain spotted fever, epidemic murine scrub and recrudescent typhus, Q-fever.

Brucellosis chronic and acute form.

Other infections caused by K. pneumoniae, Mycoplasma pneumoniae and Y. pestis and diseases such as lymphogranuloma venereum and psittacosis.

CONTRA-INDICATIONS:
Hypersensitivity to Chloramphenicol.

WARNINGS:
Jectophen (chloramphenicol) should never be used for minor infections or for prophylaxis.

Repeated courses and prolonged treatment should be avoided. Routine periodic blood examinations are advisable in all patients, but will not warn of aplastic anaemia.

Reduced doses should be given to patients with impaired liver function or with severe renal failure and in premature and full-term neonates who have immature metabolic processes. Newborn infants should never be given Jectophen (chloramphenicol) unless it may be life-saving and there is no alternative treatment.

Avoid during pregnancy and while nursing as Jectophen (chloramphenicol) is excreted in mother’s milk. It should also be avoided during active immunization.

Drug interactions: Jectophen (chloramphenicol) enhances the effects of coumarin anticoagulants, some hypoglycaemic agents such as chlorpropamide and tolbutamide, and anti-epileptics such as phenytoin. The half-life may be affected by paracetamol, phenobarbitone, phenytoin or rifampicin.

Resistance occurs in salmonellae and cross-resistance with thiamphenicol. Jectophen (chloramphenicol) may interfere with the haematological response of Vitamin B12, folic acid or iron in patients with anaemia. It may also reduce the reliability of the oral contraceptive pill and increase the incidence of breakthrough bleeding. It is also dangerous in porphyria sufferers.

DOSAGE AND DIRECTIONS FOR USE:
Jectophen Injection (chloramphenicol) should be administered when oral treatment is not feasible and should be substituted as soon as possible.

The 10% dilution of Jectophen Injection (chloramphenicol) should be administered by intravenous injection over at least one minute or in larger volumes of fluid, by slow intravenous infusion. Intramuscular injection is not recommended as the absorption may be slow and unpredictable.

Jectophen (chloramphenicol) should be reconstituted with Water for Injections, Sodium Chloride injection, or Dextrose injection 5%. The following dilution table may be useful for the administration of the proportion of the contents of a vial:

 

Concentration Solution strength Volume of Diluent to be added Total volume after dilution
40% 400 mg/mL 1,7 mL 2,5 mL
25% 250 mg/mL 3,2 mL 4,0 mL
20% 200 mg/mL 4,2 mL 5,0 mL
10% 100 mg/mL 9,2 mL 10,0 mL

 

Adults and children:

50 mg/kg body mass daily in divided doses every 6 hours.

Maximum dosage: 100 mg/kg body mass daily in severe cases. This should be reduced as soon as possible.

Treatment should be continued for 4 days after the patient’s temperature has returned to normal to avoid the risk of relapse in the case of rickettsial diseases, and for 8 to 10 days in typhoid fever.

Neonates –premature and full-term: It is not recommended in these cases. In cases of severe infection, 25 mg/kg body mass daily in 4 divided doses.

Infants over 2 weeks in age: Full term infants over 2 weeks of age may be given up to 50 mg/kg body mass daily in 4 divided doses.

Patients with impaired renal or hepatic function may require reduced doses. Discard any unused portion after dilution.

Jectophen (chloramphenicol) should only be used when there is no other suitable treatment for the severe infection and when blood concentrations can be monitored.

SIDE-EFFECTS AND SPECIAL PRECAUTIONS:
Adverse reactions to Jectophen (chloramphenicol) may be serious and sometimes fatal.

The most serious is bone marrow depression. This may take one of two forms: the first is more common and is dose-related and reversible. It occurs when the plasma concentrations of chloramphenicol exceed 25 µg/mL. It is characterised by morphological changes in the bone marrow, decreased iron utilization, reticulocytopenia, anaemia, leucopenia and thrombocytopenia. The second, irreversible aplastic anaemia is apparently not dose related. Aplastic anaemia is relatively rare and usually develops after a latent period of weeks or months. There is no way of identifying susceptible patients. It may cause death.

Haemolytic anaemia has occurred when a genetic deficiency of glucose-6-phosphate dehydrogenase is present.

The “grey-syndrome” characterised by abdominal distension, vomiting, ashen colour, hypothermia, progressive pallid cyanosis, irregular respiration and circulatory collapse followed by death has occurred in premature and newborn infants receiving doses mainly in excess of 25 mg/kg body mass daily. A similar syndrome has been reported in adults and older children given very high doses.

Peripheral and optic neuritis has been reported in patients receiving the drug over prolonged periods.

Ocular symptoms are often reversible on withdrawal of treatment. Optic atrophy with blindness has occurred. Hypersensitivity and Jarisch-Herxheimer-like reactions may also occur. Patients may experience an intensely bitter taste following rapid intravenous administration.

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT:
See “side effects and special precautions”.
Treatment is symptomatic and supportive.

IDENTIFICATION:
A white or yellowish-white hygroscopic solid or powder in 10 mL clear vials.

PRESENTATION:
1 g Vial

 

STORAGE INSTRUCTIONS:
Store below 25°C.
Protect from light.
Keep out of reach of children.

Tigecycline is a tetracycline derivative (a glycylcycline) for intravenous infusion. Tigecycline has a broad spectrum of activity, including the multidrug-resistant organisms such as Acinetobacter spp. and extended spectrum beta-lactamase (ESBL) producers, as well as methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococci.

B.Clinical Pharmacology

Mode of Action:

Tigecycline  is broad spectrum glycylcycline that acts as a protein synthesis inhibitor. It exhibits bacteriostatic activity by binding to the 30S ribosomal subunit of bacteria and thereby blocking the interaction of aminoacyl-tRNA with the A site of the ribosome. In addition, tigecycline has demonstrated bactericidal activity against isolates of S. pneumoniae and L. pneumophila.

Tigicycline is metabolized through glucuronidation into glucuronid conjugates and N-acetyl-9-aminominocycline metabolite.Therefore, dose adjustments are needed for patients with severe hepatic impairment. More so, it is primarily eliminated unchanged in the feces and secondarily eliminated by the kidney No renal adjustments are necessary.

Pharmacodynamics

Cardiac Electrophysiology: No significant effect of a single intravenous dose of Tigecycline 50 mg or 200 mg on QTc interval was detected in a randomized, placebo-and active-controlled four-arm crossover thorough QTc study of 46 healthy subjects.

Pharmacokinetics

Tigecycline is metabolized through glucuronidation into glucuronid conjugates and N-acetyl-9-aminominocycline metabolite. Therefore, dose adjustments are needed for patients with severe hepatic impairment. More so, it is primarily eliminated unchanged in the feces and secondarily eliminated by the kidneys. No renal adjustments are necessary.

Tigecycline is indicated for the treatment of infections caused by susceptible isolates of the designated microorganisms in the conditions listed below for patients who are 18 years of age and older:

Dosage & Administration

Method of Administration:

Each vial of tigecycline should be reconstituted with 5 mL of 0.9% Sodium Chloride solution for Injection to achieve a concentration of 10 mg/mL of tigecycline. The vial should be gently swirled until the drug dissolves. Withdraw 5 mL of the reconstituted solution from the vial and add to a 100 mL I.V. bag for infusion (for a 100 mg dose, reconstitute two vials; for a 50 mg dose, reconstitute one vial). The maximum concentration in the I.V. bag should be 1 mg/mL. The reconstituted solution should be yellow to orange in colour; if not, solution should be discarded. Parenteral drug products should be inspected visually for particulate matter and discolouration (e.g., green or black) prior to administration

Caution:Tigecycline  should not be reconstituted with Sterile Water for Injection.

Contraindications:

Tigecycline is contraindicated for use in patients who have a known hypersensitivity to tigecycline. Patients hypersensitive to the tetracycline-class antibiotics may be hypersensitive to tigecycline. 

Storage: Store vials at 20-25°C (68-77°F).May be stored in IV bag at room temp for up to 6 hr or refrigerated at 2-8°C for up to 24 hr

POLYMYXIN B FOR INJECTION
500,000 IU/vial
Composition: Each Vial Contains Polymyxin B Sulphate BP 500,000 IU

To reduce the development of drug-resistant bacteria and maintain the effectiveness of polymyxin B and other antibacterial drugs, polymyxin B should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria.

  1. DESCRIPTION

Polymyxin B for Injection is one of a group of basic polypeptide antibiotics derived from B polymyxa (B aerosporous). Polymyxin B sulfate is the sulfate salt of Polymyxins B1 and B2, which are produced by the growth of Bacillus polymyxa (Prazmowski) Migula (Fam. Bacillacea). It has a potency of not less than 6000 polymyxin B units per mg, calculated on the anhydrous basis. The structural formulae are:

Each vial contains 500,000 polymyxin B IU for Parenteral administration. Each milligram (mg) of pure polymyxin B base is equivalent to 10,000 IU of polymyxin B and each microgram of pure polymyxin B base is equivalent to 10 IU of polymyxin B.

  1. CLINICAL PHARMACOLOGY

MODE OF ACTION & PHARMACODYNAMICS:
Polymyxin B sulfate has bactericidal action against almost all gram-negative bacilli except the Proteus group. Polymyxins increase the permeability of bacterial cell wall membranes. Polymyxins are resistant to all gram positive bacteria, fungi, and the gram-negative cocci, N gonorrhoeae and N meningitis. Polymyxins increase the permeability of the bacterial cell membrane leading to death of the cell.

CLSI 2014 EUCAST 2014
Micro-organism Susceptible Intermediate Resistant Susceptible Resistant
Enterobacteriaceae* ≤2 μg/ml 4 μg/ml ≥8 μg/ml ≤2 μg/ml >2 μg/ml
P. aeruginosa ≤2 μg/ml 4 μg/ml ≥8 μg/ml ≤4 μg/ml >4 μg/ml
A. baummanni ≤2 μg/ml ≥4 μg/ml ≤2 μg/ml >2 μg/ml

(* Does not refer to isolates inherently resistant to polymyxins)

Susceptibility plate testing : If the Kirby-Bauer method of disc susceptibility testing is used, a 300- uv polymyxin B disc should give a zone of over 11 mm when tested against a polymyxin B susceptible bacterial strain. 

In vitro susceptibility test quality control ranges for polymyxin B sulfate against
Pseudomonas aeruginosa
Quality Control Organism
(ATCC* Number)
Minimum Inhibitory Concentration (MIC) Range (mcg/mL) Disk DiffusionQuality Control Range (300 unit disk) (mm)
Pseudomonas aeruginosa
(27853)
1  –  4 14  –  18

(*American Type Culture Collection)

Polymyxin B sulfate is not absorbed from the normal alimentary tract. Since the drug loses 50 percent of its activity in the presence of serum, active blood levels are low. Repeated injection may give a cumulative effect. Levels tend to be higher in infants and children. Tissue diffusion is poor and the drug does not pass the blood brain barrier into the cerebrospinal fluid.

PHARMACOKINETICS:

Polymyxin B is administered as its sulfate salt which is the active antibiotic. Thus conversion is not required

 

  1. INDICATIONS AND USAGE

 Acute infections Caused by Susceptible Strains of Pseudomonas aeruginosa (less resistance of 1.3% only). Polymyxin B sulfate is a drug of choice in the treatment of infections of the –

  1. Urinary Tract Infections
  2. Meningitis
  3. Blood stream infections caused by susceptible strains of Pseudomonas aeruginosa

 

It may be indicated in serious infections caused by susceptible strains of the following organisms, when less potentially toxic drugs are ineffective or contraindicated:

– H influenzae, specifically meningeal infections
– Escherichia coli, specifically urinary tract infections
– Aerobacter aerogenes, specifically bacteremia
– Klebsiella pneumoniae, specifically bacteremia (less than 2% resistance)
– MDR Acinetobacter baumannii infections (minimal resistance of 2.1%)

DOSAGE AND ADMINISTRATION

 PARENTERAL:

INTRAVENOUS – Dissolve 500,000 polymyxin B IU in 300 to 500 ml solutions of parenteral dextrose injection 5% for continuous drip. This solution should be given over 60 – 90 minutes. An infusion <30 minutes should not be used.

Adults and children: 15,000 to 25,000 IU /kg body weight/day in individuals with normal kidney function. This amount should be reduced from 15,000 IU/kg downward for individuals with kidney impairment. Infusions may be given every 12 hours; however, the total daily dose must not exceed 25,000 IU/kg/day. Infants: Infants with normal kidney function may receive up to 40,000 IU/kg/day without adverse effects.

INTRAMUSCULAR – Not recommended routinely because of severe pain at injection sites, particularly in infants and children. Dissolve 500,000 polymyxin B units in 2 ml sterile water for injection or sodium chloride injection or procaine hydrochloride injection 1%.

Adults and children: 25,000 to 30,000 IU/kg/day. Dose should be reduced in the presence of renal impairment. The dosage may be divided and given at either 4 or 6 hour intervals. Infants: Infants with normal kidney function may receive up to 40,000 IU/kg/day without adverse effects.

Note: Doses as high as 45,000 IU/kg/day have been used in limited clinical studies in treating pre-matures and newborn infants for sepsis caused by Ps aeruginosa.

 

Recommendation by Antibiotic Degree of renal impairment
Normal (≥80 ml/min) Mild (CrCl 50-79 ml/min) Moderate (CrCl 30-49 ml/min) Severe (CrCl 10-29 ml/min) Renal replacement
Manufacturer Polymyxin B 1.5-2.5 mg/kg (divided in 2 doses) The dose should be reduced from 1.5 mg/kg downwards according to renal impairment
PK studies Polymyxin B 1.5-2.5 mg/kg (divided in 2 doses) Dose adjustment is not required

 INTRATHECAL – A treatment of choice for Pseudomonas aeruginosa meningitis – Dissolve 500,000 polymyxin B IU in 10 ml sodium chloride injection USP for 50,000 IU per ml dosage unit. Adults and children over 2 years of age: Dosage is 50,000 IU once daily intrathecally for 3 to 4 days, then 50,000 IU once every other day for at least 2 weeks after cultures of the cerebrospinal fluid are negative and sugar content has returned to normal.. Children under 2 years of age: 20,000 IU once daily, intrathecally for 3 to 4 days or 25,000 IU once every other day. Continue with a dose of 25,000 IU once every other day for at least 2 weeks after cultures of the cerebrospinal fluid are negative and sugar content has returned to normal.

NOTE: IN MENINGEAL INFECTIONS, POLYMYXIN B SULFATE SHOULD BE ADMINISTERED ONLY BY THE INTRATHECAL ROUTE.

To reduce the development of drug resistant bacteria and maintain the effectiveness of polymyxin B and other antibacterial drugs, polymyxin B should be used only to treat or prevent infections that are proven or strongly suspected to be caused by susceptible bacteria. When culture and susceptibility information are available, they should be considered in selecting or modifying antibacterial therapy. In the absence of such data, local epidemiology and susceptibility patterns may contribute to the empiric selection of therapy

ORAL INHALATION* – For oral inhalation via nebulization, 0.5% solutions have been prepared using 0.9% sodium chloride. Polymyxin B concentrations >10 mg/mL should not be used for administration by oral inhalation since bronchial irritation may occur.

(*not an US-FDA approved indication).

HEPATIC FAILURE – No dose modification is required in patients with hepatic failure.

STABILITY

IN THE INTEREST OF SAFETY, SOLUTIONS OF PARENTERAL USE SHOULD BE STORED UNDER REFRIGERATION, AND ANY UNUSED PORTIONS SHOULD BE DISCARDED AFTER 72 HOURS

CONTRAINDICATIONS

This drug is contraindicated in persons with a prior history of hypersensitivity reactions to polymyxins.

PRECAUTIONS

General: Prescribing polymyxin B in the absence of a proven or strongly suspected bacterial infection or a prophylactic indication is unlikely to provide benefit to the patient and increases the risk of the development of drug-resistant bacteria. Baseline renal function should be done prior to therapy, with frequent monitoring of renal function and blood levels of the drug during parenteral therapy. Avoid concurrent use of a curariform muscle relaxant and other neurotoxic drugs (ether, tubocurarine, succinylcholine, gallamine, decamethonium and sodium citrate) which may precipitate respiratory depression. If signs of respiratory paralysis appear, respiration should be assisted as required, and the drug should be discontinued. As with other antibiotics, use of this drug may result in overgrowth of non susceptible organisms, including fungi. If super infection occurs, appropriate therapy should be instituted.

Information for Patients: Patients should be counseled that antibacterial drugs including polymyxin B should only be used to treat bacterial infections. They do not treat viral infections (e.g., the common cold). When polymyxin B is prescribed to treat a bacterial infection, patients should be told that although it is common to feel better early in the course of therapy, the medication should be taken exactly as directed, Skipping doses or not completing the full course of therapy may (1) decrease the effectiveness of the immediate treatment and (2) increase the likelihood that bacteria will develop resistance and will not be treatable by polymyxin B or other antibacterial drugs in the future.

ADVERSE REACTIONS

Nephrotoxic reactions – Albuminuria, cylin-duria, azotemia, and rising blood levels without any increase in dosage.

Neurotoxic reactions – Facial flushing, dizziness progressing to ataxia, drowsiness, peripheral paresthesias (circumoral and stocking glove), apnea due to concurrent use of curariform muscle relaxants, other neurotoxic drugs or inadevertent over dosage, and sings of meningeal irritation with intrathecal administration, e.g., fever, headache, stiff neck and increased cell count and protein cerebrospinal fluid.

Other reactions occasionally reported – Drug fever, urticarial rash, pain (severe) at intramuscular injection sites, and thrombophlebitis at intravenous injection sites.

STORAGE RECOMMENDATION

 Before reconstitution: Store at a temperature not exceeding 25°C.

Protect from light. Retain in carton until time of use. After reconstitution: Product must be stored under refrigeration, between 2⁰ to 8⁰ C (36 to 46 F) and any unused portion should be discarded after 72 hours.

Presentation : Inj Xontaz ( Ceftriaxone & Tazobactam) is available in 1g Vial

Description : Xontaz is a combination of Ceftriaxone (3rd generation cephalosporin) and Tazobactam is a penicillanic acid sulfone derivative with beta lactamase inhibitory properties.

Indications : Intra-abdominal infections, Meningitis, Surgical prophylaxis, Lower respiratory tract infections, UTI, Septicemia, Bone & joint infections

Contra-Indications : Combination is contraindicated in patients with known allergy to the cephalosporin or betalactam class of antibiotics.

Storage : Xontaz sterile powder is stored at room temperature (25 °C ) OR below and protected from light.

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