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Antibacterial & Antibiotics
 
  • Amikin
  • Cephatin
  • Metaprim
  • Livocin
Amikin DOWNLOAD BROCHURE
Broad spectrum antibacterial
Controls livestock and poultry infections without immunosuppressant effect


Compostion
Each ml contains :
Amikacin sulphate I.P. 250mg

Amikacin
Systematic (IUPAC) name ( international Union Of Pure and Applied Chemistry) (2S)-4-amino-N-[(2S,3S,4R,5S)-5-amino-2-[(2S,3R,4S,5S,6R)-4-amino-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-4-[(2R,3R,4S,5R,6R)-6-(aminomethyl)-3,4,5-trihydroxy- oxan-2-yl]oxy-3-hydroxy-cyclohexyl]-2-hydroxy-butanamide

Salient features
  • Control infections without immunosupresant effect.
  • Broad spectrum antibacterial having decisive bactericidal effect.
  • It is resistant to bacterial enzymes that inactivate other aminoglycosides.
  • Achieves predictable results in the treatment of uterine infections and repeat breeding.
  • Ensures excellent results in respiratory and urogenital tract infections.
  • It is broad spectrum antibacterial, effective against gentamycin resistant infections.
  • It is the most reliable aminoglycoside for serious aerobic gram negative bacillary infections.

Amikin
Amikacin is the newest of the aminoglycosides The spectrum of antimicrobial activity of Amikacin is the broadest of the group, and because of its unique resistance to the aminoglycoside-inactivating enzymes it has a special role in cases where gentamycin resistant micro-organisms are prevalent.

Mechanism of action:
The aminoglycoside are rapidly bactericidal, they act directly on the bacterial ribosome, where they inhibit protein synthesis and decrease the fidelity of translation of the genetic code.

Resistance
Amikacin has high resistance against bacterial inactivation. It resists attacks by most bacterial inactivating enzymes.

Absorption:
Absorption from IM injection sites is rapid and nearly complete (<90% availability). Blood levels usually peak within 30-90 min after IM administration.

Pharmacokinetics
The aminoglycosides are not metabolized in the body. They are eliminated unchanged in the urine by glomerular filtration, with 80-90% of administered drug recoverable from the urine within 24 hr of IM administration. Glomerular filtration rates differ between species and are often less in neonates, which may explain the greater sensitivity to aminoglycosides in newborn foals and puppies.Elimination depends on cardiovascular and renal function, age, volume of distribution, fever, and several other factors.

The aminoglycosides have relatively short plasma half-lives (~1 hr in carnivores and 2-3 hr in herbivores). About 90% of the injected drug is excreted unchanged through the kidneys

Distribution
The aminoglycosides distribute into the extracellular fluid space with minimal penetration into most tissues except the kidneys (where they accumulate in the renal cortex) and the endolymph of the inner ear. The distribution volume of aminoglycosides can increase in animals with congestive heart failure or ascites. Neonates also have a large extracellular fluid compartment relative to body weight. Although aminoglycosides are not appreciably bound to plasma proteins (usually <20%), they do attain therapeutic concentrations in the synovial, pleural, and even peritoneal fluids, especially if inflammation is present. However, effective levels are not reached in CSF, ocular fluids, milk, intestinal fluids, or prostatic secretions. Fetal tissue and amniotic fluid concentrations are very low in most species.

Untoward effects :
Ototoxicity: Both vestibular & auditory disfunction can follow the administration of any of the aminoglycoside.
Nephrotoxicity: Very high concentrations of aminoglycoside accumulate in the renal cortex and this correlates with the potential of these drugs to cause nephrotoxicity.

Although amikacin, like other aminoglycosides, is potentially nephrotoxic, ototoxic and neurotoxic, parenteral (intravenous) administration of amikacin sulfate twice daily at dosages of up to 10 mg/lb for 15 consecutive days in horses resulted in no clinical, laboratory or histopathologic evidence of toxicity.

Interactions:
Enhanced nephrotoxicity may become evident with concurrent administration of aminoglycosides and other potentially nephrotoxic agents. Neuromuscular blockade is more likely when aminoglycosides are administered at the same time as skeletal muscle relaxants and gas anesthetics. Aminoglycoside ototoxicity is enhanced by the loop-acting diuretics, especially furosemide. Cardiovascular depression may be aggravated by aminoglycosides when administered to animals under halothane anesthesia. High concentrations of carbenicillin, ticarcillin, and piperacillin inactivate aminoglycosides both in vitro and in vivo in the presence of renal failure.

Safety
Amikacin Solution (Amikacin Sulfate Solution) is non-irritating to equine endometrial tissue when infused into the uterus as directed (see “Dosage and Administration”). In laboratory animals as well as equine studies, the drug was generally found not to be irritating when injected intravenously, subcutaneously or intramuscularly.

Intrauterine infusion of 2 grams of Amikacin Solution (Amikacin Sulfate Solution) 8 hours prior to breeding by natural service did not impair fertility in mares. Therefore, mares should not be bred for at least 8 hours following uterine infusion.

Therapeutic uses:
Amikacin has become the preffered drug where resistance to gentamycin has become a significant problem. Because of its unique resistance to Aminoglycoside inactivating enzymes, Amikacin is active against the vast majority of aerobic gram negative bacilli. This includes most strains of Serratia, Proteus and Pseudmonas aeruginosa. It is active against nearly all strains of Klebsiella, Enterobacter and E. Coli that are resistant to Gentamycin & Tobramycin.

Indications
Cattle, Horse & Camel
  Repeat breeding
Rispiratory tract & Umblical infections caused by E. Coli & Salmonella
Mastitis. Metritis & systemic infections
Enteritis.
Pig, Sheep, Goat, Calf & Dog
  Respiratory & Urogenital Tract infections
Secondary bacterial infections associated with viral disease like Canine distemper, Haemorrhagic gastroentritis, Proteus infections.
Post surgical care
Calf Scours
Poultry
  Chronic respiratory disease (CRD) Bronchitis, E. Coli, Salmonella infections & prevention of early chick mortality.


Administration & dosages:
For susceptible infections
Cattle, Sheep, Goat , Pig and Dog 5-12 mg/kg of body weight I M for 3-5 days.
Horses 4.4 - 6.6 mg / kg of body weight I M or I V bid – tid, if severe infection.
Poultry 20 mg / kg b.wt. by SC injection.

For uterine infusion in mares
Amikacin Solution (Amikacin Sulfate Solution) is indicated for the treatment of uterine infections (endometritis, metritis and pyometra), caused by susceptible organisms including Escherichia coli, Pseudomonas sp, and Klebsiella sp. For treatment of uterine infections 2 grams (8 ml) of Amikin (Amikacin Sulfate Solution), mixed with 200 ml 0.9% Sodium Chloride sterile solution or distilled water infused aseptically into the uterus daily for three consecutive days, has been found to be the most efficacious.

Presentation
30 ml & 100 ml vials
Cephatin DOWNLOAD BROCHURE
Cefoperazone & Sulbactam

Composition:
Each vial contains:
Cefoperazone Sodium I.P. 3.0 g
eqv. to Cefoperazone
Sulbactam sodium U.S.P. 1.5g
eqv. to anhydrous sulbactam

Cefoperazone: Cefoperazone sodium is a semi- synthetic third generation cephalosporin contains a piperazine side chain giving it antipseudomonal activity. It is one of few cephalosporin antibiotic effective in treating pseudomonal bacterial infections which are otherwise resistant to these antibiotics.

Sublactam: Sulbactam sodium is a penicillanic acid sulfone with ß–Lactamase (an enzyme produced by bacteria that destroys the antibiotics) inhibitory properties. Sulbactam is a molecule which is given in combination with ß–Lactam antibiotics. It has weak antibacterial activity but is chemically stable ß–Lactamase inhibitor that synergistically increases the activity of ß–Lactam antibiotics against ß–Lactamase producing bacteria. Sulbactam can therefore enhance the activity of penicillin & cephalosporin against many resistant strains of bacteria.

Salient features
  • Cefoperazone-sulbactam fixed ratio 2:1 maximized the Cefoperazone spectrum activity.
  • Cefoperazone-sulbactam combination exhibited broad spectrum activity (antibiotic sensitivity 94.4%)
  • Cefoperazone-sulbactam therapy demonstrates enhanced efficacy against the Staphylococci, Pseudomonads and Enterobactriaceae.

Cephatin
  • Cefoperazone has a braod spectrum bactericidal action with increased activity against Pseudomonas spp.
  • Cefoperazone is relatively stable to hydrolysis to ß–Lactamases produced by gram–negative bacteria.
  • Sulbactam protects Cefoperazone from ß–Lactamases produced by staphylococci & Entero bacteriaceae.
  • Drug can be used safely during pregnancy.
  • The combination of sulbactam & Cefoperazone demonstrates synergistic activity (up to fourfold reduction and MIC for the combination versus those for each component).

Antibacterial spectrum :
Cefoperazone has a bactericidal action & broad spectrum activity. With increased activity against pseudomonas spp. It is highly stable to hydrolysis by most beta lactamases. Cefoperazone has antibacterial activity similar to that of ceftazidime. Activity particularly against enterobacteriaceae & bacteroides spp. has been enhanced in the presence of the ß–lactamase inhibitor sulbactam.

Cefoperazone possesses broad spectrum activity against most of the gram-positive, gram-negative and anaerobic bacteria.
  • Gram-positive bacteria-Staphylococcus aureus, Steptococcus agalactiae, S.pneumoniae, S. pyogenes, Enterococcus faecalis.
  • Gram-negative bacteria – Escherichia coli, Klebsiella pneumoniae, Proteus spp., Psudomonas aeruginosa, Citrobacter freundii, Enterobacter cloacae, and Serratia marcescens, Haemophilus influenza, Neisseria meningitides.
  • Anaerobic organisms: Gram negative bacilli, Gram positive and Gram negative cocci and Gram positive bacilli.

Mechanism of action:
Cefoperazone acts against sensitive organism during the stage of active multiplication by inhibiting biosynthesis of cell wall mucopeptide. The cell walls of bacteria are essential for their normal growth & development. Peptidoglycan is a heteropolymeric component of the cell wall that provides rigid mechanical stability. Sulbactam is an irreversible inhibitor of beta-lactamase; it binds the enzyme & does not allow it to interact with the antibiotic.

ß–Lactam antibiotics produce certain characteristic morphological effects on bacteria :-
  • Bacteria may form long filamentous forms & fail to devide.
  • Growth may take place at the midportion with formation of bulge.
  • Microorganism may swell & then rupture.
  • Stable cell wall deficient bactria may be formed.
  • In general at the lowest effective concentration of ß–lactam antibiotic, cell division is inhibited but elongation continues. As the concentration of antibiotics is increased growth is inhibited, bulges may form, & lysis is then observed.

Pharmacokinetics
Cephalosporins are rapidly absorbed following IM or SC administration. After intramuscular administration peak plasma concentrations have been reported after 1-2 hrs. The plasma half life of Cefoperazone is 2 hrs. (65-97 mcg per ml). Cefoperazone is 82 to 93% bound to plasma proteins. Cefoperazone is weidely distributed in body tissue and fluids. Penetration into the CSF is generally poor; in case of first & second generation ciphalosporins, where as Cefoperazone enters the CSF in sufficient concentration due to greater lipid solubility. It crosses the placenta and low concentration have been detected in milk. Following intravenous administration in cross bred calves, the drug could not be detected in urine upto 24 hrs of administration, indicating its non-renal route of excretion and the major route of elimination of cefoperazone has been reported via bile. Cefoperazone is excreted mainly in the bile resulting in longer half life. The urinary recovery of Cefoperazone under normal conditions is in the range of 3.89% in buffalo calves.

Indications
Livestock
  • Severe respiratory & genitourinary infections.
  • Enteric, urinary tract infections & urinary peritonitis cholecysitic, cholangitis.
  • Bovine mastitis
  • Skin, soft tissue, bone & joint infections.
  • Endometritis
  • Pneumonia in calves,
  • Meningitis

Poultry
  • Septicemia in chicken
  • Infectious bronchitis
  • Ulcerative entritis.
  • Complicated C.R.D. problems & pneumonia
  • Colibacillosis, coryza & fowl cholera

Contra indications
  • Cephatin Inj. is contraindicated in patients with known allergy to penicillin, sulbactam, Cefoperazone or any of the cephalosporin.
  • The drug in horses may be used with caution, as it is contraindicated in herbivores with an expended large bowel.

Dosage & Administration:
Deep IM or IV by intermittent or continuous infusion.
Live stock 10 – 15mg / kg b. wt. for 3 -5 days
Poultry 20 mg / kg b.wt. for 2 -3 days.
or
as directed by the registered veterinary practitioner.
Note: Prepare solution by dissolving the contents of the vial with 10-20 ml sterile water. 20ml sterile water for injection I.P. provided with the pack.

Presentation
4.5 gm vial with 20ml sterile water for injection
3.0 gm vial with 20ml sterile water for injection
 
EXCELLENCE THROUGH INNOVATION
3rd GENERATION CEPHALOSPORIN
CEPHATIN ® Inj.
 
CEPHALOSPORINS: are broad spectrum antibiotics that, are divided into 3 generations.
  1. The first generation cephalosporins:
    (Cefadroxil, Cephalexin, Cephapirin, Cefazolin)
    They are more effective against Gram-positive than Gram-negative bacteria & are susceptible to ß – Lactamases.
  2. The second generation cephalosporin:
    (Cefoxitin & Cefotetan, the Cephamycins)
    They are more active against certain gram-negative bacteria (Hemophilus, Proteus, E. coli, & Klebsiella) than the first generation but less than the third generation & are relatively resistant to ß-lactamases.
  3. The third generation cephalosporins:
    (Cefoperazone, Cefotaxime, Ceftiofur, Ceftazidime & Ceftriaxone)
    They are most effective against Gram-negative bacteria, resistant to ß-lactamases & enter the CSF in sufficient concentration due to greater lipid solubility.
    • This class of drugs was developed for use in specialized situation where antibiotic resistant Gram – negative infections are common & safety is of prime concern.
    • Third generation cephalosporins typically have greater activity against Gram-negative than others.
    • Third generation cephalosporins are active even against some strains of Enterobacter, E. coli, Klebsiella, Proteus & Serratia that are resistant to the first & second generation cephalosporins.
    • Most third generation cephalosporins also have some activity against Pseudomonas spp.
    • The product containing cefoperazone in oil base for intra-mammary infusion is effectively used. The non-irritant properties of cefoperazone plus persistence of therapeutic concentration of the drug in treated quarters for 3-4 milking make this drug very useful for the treatment of bovine mastitis.
 
References:
  • Jones, RN ; Barry, AL; Pacter, RR; Gregory, ww; Thornsberoy C. In Vitro antimicrobial spectrum, occurrence of synergy & recommendations for dilution susceptibility testing concentrations of the Cefoperazone – sulbactam combination. J. Clin Microbiol 1987 September 25 (9) ; 1725-1729, PMCID: PMC 269316.
  • Wilson, CD; Agger, A; Gilbert, GA; Thomsson, CA; Tolling, ST. field trials with cefoperazone in the treatment of bovine clinical mastitis. The veterinary record Vol. 118, issue 1, 17-19 copy right © 1986 by British Veterinary Association.
METAPRIM Dispersible Powder DOWNLOAD BROCHURE
A synergistic combination of bactericidal chemotherapeutics

Composition
Each 5 gram contains:
Sulphamethoxazole I.P. 400mg
Trimethoprim I.P. 80mg

Metaprim is a combination of sulphamethoxazole (a sulphonamide) and trimethoprim. Trimethoprim when used alone is only bacteriostatic and resistance develops rapidly. However, when combined with sulphamethoxazole, a sequential blockade of microbial enzyme system occurs with bactericidal consequences.

Salient Features
  • Metaprim is bactericidal combination of Sulphamethoxazole and trimethoprim.
  • Metaprim is effective even in the multi-resistant infections.
  • Metaprim produces a sequential double blockade of bacterial metabolism, giving a level of activity many times greater than that obtained by either drug alone.
  • Metaprim provides effective antibacterial activity against a wide range of infections caused by Gram-positive and Gram-negative bacteria.

Metaprim
Mechanism of action:
Para- amino benzoic acid (PABA) is required by bacteria for their growth and multiplication. The sulphonamides are structural analog of PABA. In the first step the synthesis of dihydrofolic acid from PABA is blocked by competitive inhibition of PABA with sulphamethoxazole. In second step trimethoprim block the synthesis of tetrahydrofolic acid from dihydrofolic acid by competitive inhibition of dihydrofolate reductase (bacterial enzyme). Tetrahydrofolic acid is required for the synthesis of the precursor of DNA in bacteria. Blocking both steps of folic acid metabolism leads to an arrest in DNA synthesis and subsequent parasite death. Trimethoprim and sulphamethoxazole, when used separately, are bacteriostatic but when used in combination, it becomes bactericidal and increases the spectrum of antimicrobial activity.

Pharmacokinetics
Orally administered sulfamethoxazole and trimethoprim are rapidly absorbed. The maximum serum concentrations reached 0.5-1 h after administration. The bioavailability was 81% for sulfamethoxazole and 41% for trimethoprim.(in japanese quails.)

Precautions and Side Effects
Trimethoprim and sulfamethoxazole should not be used in animals with known hypersensitivity or allergy to these or other sulfa drugs.

Indications
Poultry : E.Coli infections, chronic respiratory disease (CRD), fowl coryza, coccidiosis, fowl cholera, typhoid and secondary bacterial infections.
Live stock: Gastro-intestinal tract infections, respiratory tract infections, urinary tract infections, genital tract infections.
Sheep and Goat 2 tablets daily for 2-3 weeks.

Administration and dosage
Poultry : 12.5 g. per 10 lt. of drinking water for 5-7 days.
Live stock: 12.5 g. per 80 kg. b.wt. twice daily for 5-7 days.

Presentation
100 g. and 500 g.
Livocin Premix DOWNLOAD BROCHURE
A Third Generation Fluoroquinolone Antibiotic
Water Soluble and Feed Premix.


Formulation :
Each gram contains : Levofloxacin Hemi hydrate
Equivalent to Levofloxacin 100 mg

Levofloxacin is a third generation fluoroquinolone antibiotic. It is twice as active as it’s isomer ofloxacin, effective against number of Gram- positive, Gram- negative and specifically effective against the organisms that cause atypical pneumonia. levofloxacin is one of the so called respiratory quinolones. Levofloxacin is to be considered a drug of last resort when all other antibiotics have failed.

Chemical structure
Levofloxacin

Systematic name
7-fluoro-6-(4-methylpiperazin-1-yl)-10-oxo-4-thia-1-azatricyclo [7.3.1.05,13] trideca-5(13),6,8,11-tetraene-11-carboxylic acid.

Livocin Premix
Pharmacology :
Levofloxacin is the L-isomer of the racemate, ofloxacin, a quinolone antimicrobial agent. Chemically, levofloxacin, a chiral fluorinated carboxyquinolone, is the pure (-)-(S)-enantiomer of the racemic drug substance ofloxacin. The chemical name is (-)-(S)-9fluoro-2,3-dihydro-3-methyl – 10 - ( 4 – methyl – 1 – piperazinyl ) – 7 – oxo - 7H –pyrido [1,2,3 – de] - 1, 4 benzoxazine – 6 - carboxylic acid hemihydrate. The empirical formula is C18H20FN3O4 • ½ H2O and the molecular weight is 370.38. Levofloxacin is a light yellowish-white to yellow-white crystal or crystalline powder.

Mechanism of action :
Fluoroquinolones are bactericidal drugs, actively killing bacteria by inhibiting bacterial DNA gyrase or the topoisomerase IV enzyme, thereby inhibiting DNA replication and transcription.. Quinolones can enter cells easily via porins and therefore are often used to treat intracellular pathogens such as Legionella pneumophila and Micoplasma pneumonae. For many Gram- negative bacteria DNA gyrase is the target, whereas topoisomerase is the target for many Gram- positive bacteria.

Activity :
Levofloxicin exhibit good activity against most of the gram-positive, gram- negative and anaerobic bacteria.

Susceptible organisms are :
Gram- positive bacteria- Enterococcus faecalis, Staphylococcus- aureus, Staphylococcus epidermidis, Staphylococcus saprophytics, Streptococcus pneumoniae, S. pyogenes

Gram-negative bacteria- Enterobacter cloacae, Klebsiella pneumoniae, Pseudomonas aeurginosa, Escherichia coli, Serratia marcescens , Haemophilus influenzae, Haemophilus parainfluenzae, Proteus mirabilis, Legionella pneumophilia, Moraxilla catarrhalis, Campylobacter spp.,

Other- Mycoplasma pneumoniae, Peptostreptococcus sp.

Pharmacokinetics :
Levofloxacin is rapidly and almost completely absorbed following oral administration with peak plasma concentration achieved within an hour of the dose.

It is distributed into the body tissues including the bronchial mucosa and lungs, but penetration into CSF is relatively poor. Levofoxacin is approximately 30-40% bound to plasma proteins. It is only metabolised to a small degree to inactive metabolites. The elimination half life of levofloxacin is 6-8 hrs. It is excreted largely unchanged, primarily in urine.

Safety :
Fluoroquinolones have had a remarkably good safety record.

Because these drugs do not alter the anaerobic flora of the gastrointestinal tract, there is minimal disruption of the intestinal bacterial population even when these drugs are administered orally.

There have been no reports of cutaneous drug reaction resulting from fluoroquinolones usage in the veterinary.

Drug interactions :
Nonsteroidal anti-inflammatory drugs and corticosteroids enhance the toxicity of fluoroquinolones. Medication or supplements containing aluminium, magnesium, calcium, ferrous sulfate, iron and zinc are believed to form chelation complexes with fluoroquinolone antibiotics and thereby prevent the drug from being properly absorbed during therapy.

Indications :
Livocin is indicated in the following bacterial infections :
  • Pneumonia
  • Acute bacterial sinusitis
  • Acute and chronic bronchitis
  • Skin infections
  • Urinary tract infections
  • Acute pylonephritis

Poultry (chicken, duck, goose):- Escherichia coli, yellow and white dysentery, enteritis, pericarditis, ovarian inflammation, green suppuration bacillus, staphylococcus infection, cholera etc.

Pig: many kind of bacterium diseases such as enteritis, yellow and white dysentery, etc.

Administration :
It is to be given orally.

Mixing rate:
Poultry: 1 gram in 1-2 liter of drinking water for 5-7 days. or 500 grams in 1000 Kilogram of feed material for 5-7 days.
Pig : 1 gram in 1-2 liters of drinking water for 5-7days. or 1 kilogram in 1000 kilogram of feed material for 5-7 days.
Horse and Cattle Oral administration 20-40 mg per kilogram of body weight for 3-5 days.

Packing / Presentation :
1 kg and 25 kg.

Ref.:Levofloxacin 10 mg./ kg. body weight after repeated oral administration at 12 hrs. interval for 14 days in layer birds (30-35) weeks old weighing 1.5-2.0kg.) was found safe. Levofloxacin could not be deducted in the tissues (liver & skeletal muscles) at 12 hrs. after the last administration. Study indicates that, levofloxacin is well tolerated following multiple oral administration at 10 mg./ kg. body weight in layers.
Vinod K. Dumka,Anil K. Srivastava J. Vet. Sci. (2006),7(4),333-337