Rozin 1000

Rozin 1000
19 Jun

Rozin 1000

Antibiotics & Antibacterial

- Ceftriaxone is a sterile, semisynthetic, long acting, broad spectrum antibiotic   
  belong to third generation cephalosporins.
- Ceftriaxone inhibits bacterial cell wall synthesis following attachment to  
  penicillin binding proteins. This results in the interruption of cell wall  
  (peptidoglycan) biosynthesis, which leads to bacterial cell lysis and death.     
- Ceftriaxone exerts in vitro  activity against a wide range of Gram-negative and
  Gram-positive micro-organisms.
- Ceftriaxone is  usually  active in-vitro  and  in clinical infections against the
   following:   
 Gram-positive  aerobes: Staphylococcus aureus, Staphylococcus epidermi- 
  dis, Streptococcus  pneumoniae, Streptococcus pyogenes, Streptococcus
  agalactiae, Streptococcus viridans, Streptococcus bovis.  
 Gram-negative  aerobes: Aeromonas  spp., Alcaligenes  spp., Branhamella
  catarrhalis, citrobacter  spp., Enterobacter spp. (some strains are  resistant), Escherichia  coli,  Haemophilus ducreyi,  Haemophilus influenzae,
   Haemophilus parainfluenzae, Klebsiella  spp.,  Moraxella spp., Morganella
   morganii, Neisseria  gonorrhoeae, Neisseria  meningitidis, Plesiomonas
   shigelloides, Proteus  mirabilis, Proteus vulgaris, Providencia  spp., Pseud- 
  omonas aeruginosa  (some  strains  are  resistant), Salmonella spp., serratia 
   spp., Shigella   spp., Vibrio  spp., Yersinia   spp.   
 Anaerobic organisms:  Bacteroides spp.,Clostridium  spp. (except Cl. diffi-
  cile ), Fusobacterium  spp. (except  F. mortiferum  and  F. varium ),Peptococ-
  cus  spp., Peptostreptococcus spp. 
 Note: Many strains of ß-lactamase-producing Bacteroides spp. (notably B.
  fragilis) are resistant.
- Ceftriaxone is highly stable to most ß-lactamases, both penicillinases and
  cephalosporinases, of Gram-positive and Gram-negative bacteria.
- The area under the plasma concentration time curves after l.V. and l.M. 
  administration of Ceftriaxone is identical. This means that the bioavailability
  of ceftriaxone administered l.M, is 100%. On intravenous administration, 
  ceftriaxone diffuses rapidly into the interstitial fluid, where bactericidal 
  concentrations against susceptible organisms are maintained for 24 hours.
 -Ceftriaxone is reversibly bound to albumin, and the binding decreases with
  the increase in the concentration. The average extent of diffusion in the 
 cerebrospinal fluid in bacterial meningitis is 17% of the plasma concentration.
- In patients with renal impairment or hepatic dysfunction, the pharmacokinet-
  ics of ceftriaxone are only slightly increased. If kidney function alone is
  impaired, biliary elimination of ceftriaxone is increased; if liver function alone 
  is impaired, renal elimination is increased.
- Ceftriaxone is characterized by an unusually long elimination half-life of 
  approximately eight hours in healthy adults. In infants aged less than eight 
  days and in persons over 75 years of age, the average elimination half-life is
  about twice as long. 

- In adults, 50 - 60% of ceftriaxone is excreted unchanged by the kidneys, while 
  40 - 50% is excreted unchanged in the bile. In neonates, renal elimination 
  accounts for about 70% of the dose.

Indecation

- Infections caused by pathogens sensitive to ROZIN® e.g.: Sepsis; meningitis; 
 abdominal infections (peritonitis, infections of the biliary and gastro-
 intestinaltracts); infections of the bones, joints, soft tissue, skin and of 
 wounds; infections in patients with impaired defence mechanisms; renal and 
 urinary tract infections; respiratory tract infections, particularly pneumonia, and 
 ear, nose and throat infections; genital infections, including gonorrhea.
- Perioperative prophylaxis of infections.

Dosage & Administration

  After  reconstitution,  ROZIN® is  administered  by intermittent  intravenous   
  injection and  by deep intramuscular injection.
•   Adults  and  children  over 12  years: The usual dosage  is 1-2  g of ROZIN®
  administered once daily (every 24 hours). In severe cases or in infections
  caused by moderately sensitive organisms, the  dosage may be raised  to  4  g,
   administered  once  daily.
•   Infants and Children (3 weeks to 12 years):  A daily  dose of  20-80 mg/kg. 
   Intravenous  doses of  50 mg/kg  or  more  should be given by infusion over at 
    least 30 minutes.
•   Elderly  patients: The  dosage  recommended  for adults  require  no  modifica- 
   tion  in  the  case  of  geriatric  patients.
•  Special dosage  instructions:
-  Meningitis:  In  bacterial  meningitis  in  infants  and  children,  treatment 
   begins  with  doses  of  100 mg/kg (not to  exceed  4 g) once  daily. The best results
  have been found with the following duration of therapy:
-  Gonorrhea:  A single  IM  dose  equivalent to 500 mg  ROZIN® .
-   Perioperative  prophylaxis:  A  single  dose   of   1-2 g   ROZIN® administered    
   30-90 minutes  prior  to  surgery.
-   Impaired  renal   function:  Only  in  cases  of  preterminal  renal  failure
    (creatinine clearance   <10 ml/min)  should  the  ROZIN® dosage  not  exceed  
    2 g daily.
-  Impaired  hepatic function:  No  need  for  the  dosage  to be  reduced.
-   Reconstitution:  Reconstituted  solutions  retain  their  physical  and  chemical  
   stability  for  6  hours  at room  temperature  or  for  24  hours  at  5ºC. As a 
   general  rule;  however, the  solutions  should  be used  immediately  after
    preparation. They  range  in  color  from pale  yellow  to amber (depending on
    the  concentration  and  the  length  of  storage),  this is of  no significance for  the
    efficacy or  tolerance  of   the  drug.   
  Intramuscular  injection:  ROZIN® 500 mg is dissolved  in  1.8 ml of 1%  
  lidocaine solution, and  ROZIN® 1 g  in  3.6  ml  of  1%  lidocaine solution,  
  and administered by deep intra-muscular injection. Intramuscular injection 
  without lidocaine solution is painful.
  Intravenous   injection:   ROZIN® 500  is  dissolved  in  4.8  ml of  sterile  water 
 for  injection and  ROZIN® 1000  in  9.6ml  of  sterile  water  for  injection and
  
   then administered by I.V. injection lasting 3 to 5 minutes.

- Each vial of  ROZIN® 500 mg contains:
      Ceftriaxone                   500 mg   (as Ceftriaxone Sodium)
- Each vial of  ROZIN® 1 g contains:
      Ceftriaxone                          1 g   (as Ceftriaxone Sodium)

- ROZIN®  is contraindicated in patients with known hypersensitivity to the 
  cephalosporin class of antibiotics. In patients hypersensitive to penicillin, the 
  possibility of allergic cross reactions should be borne in mind. 

 No  impairment  of renal  function  has so  far been  observed  after  simultanous 
   administration  of  larger  doses  of  Ceftriaxone  and  potent diuretics  like
  furosemide.There  is  no  evidence  that Ceftriaxone  increases   renal  toxicity  of 
   aminoglycosides. No  effect  similar  to  that  of  disulfiram  has  been 
  demonstrated  after  administration  of  alcohol  with Ceftriaxone.  The
  elimination  of Ceftriaxone  is  not  altered  by  probenecid.

 Ceftriaxone  should  not  be used in  pregnancy (particularly  in  the  first trimester) 
   unless  absolutely  indicated. Low concentrations of ceftriaxone are excreted in 
   human milk, caution should be exercised when ROZIN® is administered to a 
   nursing woman.

- ROZIN®  is  generally  well  tolerated. The  following side   effects  may  arise:
   diarrhea,  nausea,  vomiting,  stomatitis,  glossitis, eosinophilia,  leukopenia, 
  granulocytopenia,  hemolytic anemia, thrombocytopenia,  pruritus,   urticaria, 
  erythema multiforme, headache  and dizziness,  increase in  liver enzymes. In rare 
  cases, phlebitic reactions occurred after I.V. administration. These may be 
  prevented by slow (2 - 4 minutes) injection of the substance. 

- Prolonged  use  of  antibiotics  may  result  in  over-growth  of  non-susceptible 
   organisms.
- Because  Ceftriaxone  can  displace  bilirubin from  serum  albumin,  it  should 
   not  be  administered  to  hyperbilirubinemic  neonates,  particularly  those  who  
  are  premature. Alterations  in  prothrombin  times  have  been   reported  only   rarely  in  patients   receiving  Ceftriaxone. Patients   with  impaired  vitamin K  
  synthesis  or  low  vitamin K  stores  (e.g.  chronic  hepatic disease, malnutrition)  
  may  require  monitoring  of  prothrombin  time  during  Ceftriaxone  treatment.   
 10 mg of   vitamin  K  weekly  may  be  necessary  if   the  prothrombin time  is 
  prolonged  before or  during therapy.

- Store below 25ºC, and protect from light.