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Antibacterials , Drugs / November 19, 2016

Class: Antibacterials
Dosage Form: Various
Description: First generation cephalosporin
Stock: Available
Manufacturer: Bristol-Myers Squibb

Composition:

Capsules:
Cephradine……………………………….250 and 500 mg
Tablets:
Cephradine…………………………………………………..1 g
Power for Oral Suspension:
Cephradine………………………125 and 250 mg / 5 ml

Properties:

Pharmacology
Cephradine is acid stable and is rapidly absorbed following oral administration in the fasting state. Following doses of 250 mg, 500 mg, and 1 g in normal adult volunteers, average peak serum levels of approximately 9, 16.5 and 24.2 mcg/ml, respectively, ere obtained at one hour. The presence of food in the gastrointesitnal tract delays the absorption but does not affect the total amount of cephadrine absorbed. Measurable serum levels are present six hours after administration. 48 hours after administration of 100 mg/kg/dayof cephradine for the treatment of otitis media, cephradine was present in the middle ear exudate at an average level of 3.6 mcg/ml. Cephradine does not pass across the blood-brain barrier to any appreciable extent.
Over 90% of th drug is excreted unchanged in the urine within 6 hour. Peak urine concentrations are approximately 1600 mcg/ml following a 250 mg dose, 3200 mcg/ml following a 500 mg dose, and 4000 mcg/ml following a 1 g dose.

Microbiology
Cephradine is a broad-spectrum, bactericidal antibiotic active against both gram-positive and gram-negative bacteria Cephradine is active against the following organisms in vitro:

  • Group A beta-hemolytic streptococci
  • Staphylococci, including coagulase-positive, coagulase-negative and penicillinase-producing strains
  • Streoptoccous pneumoniae (formerly Diplococcus pneumoniae)
  • Escherichia coli
  • Proteus mirabilis
  • Klebsiella species
  • Haemophilus influenzae

Cephradine is not active against most strains of Enterobacter species, Morganella morganii (formerly proteus morganii), and proteus vulgaris. Most strains of enterococci (Enterococcus faecalis) are resistant to cephradine. It has no acitivity against Pseudomonas or Herellea species. When tested by in vtiro methods, Staphylococci exhibit cross-resistance between cephradine and methicillin-type antibiotics.
Cephalosporin-class discs are used in disc susceptibility testing.

Side Effects:

As with other cephalosporins, untoward reactions are limited essentially to gastrointstinal disturbances and, on occasion, to hypersensitivity phenomena. The latter are more likely to occur in individuals who have previously demonstrated hypersensitivity and those with a history of allergy, asthma, hay fever or urticaria.
The following adverse reactions have been reported following the use of cephradine:

1. Gastrointestinal:

  • Glossitis, nausea, vomiting, heartburn, diarrhoea or loose stools, abdominal pain, colitis, and pseudomembranous colitis

2. Hypersensitivity:

  • Mild urticaria or skin rash, pruritus and joint pains. As with other cephaosporins, there have been rare reports of anaphylaxis, erythema multiformes, Stevens-Johnson syndrome and toxic epidermal necroylsis.

3. Hematologic:

  • Mild and transient eosinophilia, leukopenia and neutropenia

4. Liver:

  • Isolated instances of elevated SGOT, SGPT, total bilirubin and alkaline phosphatase have been observed with no evidence of hepatocellular damage

5. Renal:

  • Transitory rises in BUN have been observed in some patients treated with cephalosporins; their frequency increases in patients over 50 years old
  • In adults for whom serum creatinine determinations were preformed, the rise in BUN was not accompanied by a rise in serum creatinine

6. Other:

  • Other adverse reactions have included dizziness, tightness in the chest and candidal vaginitis

Dosage and Administration:

Cephradine may be given without regard to meals.

1. Adults:

  • Respiratory tract infections (other than lobar pneumonia) and skin and soft tissue infections:
    • The usual dose is 250 mg every 6 hours or 500 mg every 12 hours
    • Severe infections may require larger doses
  • Lobar pneumonia:
    • The usual dose is 500 mg every 6 hours  or 1 g every 12 hours
  • Uncomplicated urinary tract infections:
    • The usual dose for uncomplicated infections is 500 mg every 12 hours
    • For more serious infections including prostatitis, 500 mg every 6 hours or 1 g every 12 hours is recommended
    • Prolonged intensive therapy is recommended for prostatitis and epididymitis

2. Children:
In mild to moderately severe infections the usual daily dose is from 25 to 50 mg/kg administered in equally divided doses every 6 to 12 hours.
For otitis media due to H. influenzae, daily doses from 75 to 100 mg/kg administered in equally divided doses every 6 or 12 hours is recommended.
The maximum dose should not exceed 4 g per day.
In all patients, regardless of age and weight, doses up to 1 g every 6 hours may be given for severe or chronic infections.
As with antibiotic treatment in general, therapy should be continued for a maximum of 48 to 72 hours after the patient becomes asymptomatic or evidence of bacterial eradication has been obtained. In infections caused by group A beta-hemolytic streptococci, a minimum of 10 days of treatment is recommended to guard against the risk of rheumatic fever or glomerulonephritis. In the treatment of chronic urinary tract infections, frequent bacteriologic and clinical appraisal is necessary during therapy and may be necessary for several months afterwards. Persistent infections may require treatment for several weeks. Doses smaller than those indicated above should not be used. Doses for children should not exceed doses recommended for adults.
Oral cephradine may be utilized following clinical improvement achieved with parenteral therapy for the continunation of therapy for persistent or severe infections where prolonged therapy is indicated.

3. Dosage in Patients with Renal Impairment:
Not on diaylsis: The following dosage schedule based on a dosage of 500 mg Q6H and on creatinine clearance is suggested as a guideline. Further modification in the dosage schedule may be required because of the dosage selected and individual variation.
On chronic intermittent, hemodialysis:

  • 250 mg start
  • 250 mg at 12 hours
  • 250 mg, 36-48 hours (after start)

Children may require dosage modification proportional to their weight and severity of infection.

Warnings:

There is evidence of partial corss-allergenicity between the penicillins and the cephalosporins. Therefore, cephradine should be used with caution in patients with known hypersensitivity to penicillins. There ahve been instances of patients who have had reactions to both drug classes, including anaphylaxis (see Adverse Reactions).
Pseudomembranous colitis has been reported with the use of cephalosporins (and other broad spectrum antibiotics), including cephradine; therefore, it is important to consider this diagnosis in patients who develop diarrhoea in association with antibiotic use. Mild cases of colitis may respond to drug discontinuance alone, moderate to severe cases should be managed as indicated.
In patients with known or suspected renal impairment, careful clinical observation and appropriate laboratory studies should be performed since cephradine accumulates in the serum and tissues unless dosage is suitably reduced (see Dosage and Administration).
After treatment with cephradine, a false-positive reactions for glucose in the urine may occur Benedict’s solution, Fehling’s solution, or with Clinitest tablets, and Tes-Tape, as with other cephalosporins, positive direct Coomb’s tests have been infrequently reported.
As with all antibiotics, prolonged use may result, in overgrowth of non-susceptible organisms.

Packaging:

Boxes of 12 capsules: Store at a temperature not exceeding 30°C and avoid excessive heat and protect from light and humidity.
Boxes of 8 tablets: Store at a temperature not exceeding 30°C and avoid excessive heat and protect from light and humidity.
Bottles of 60 ml (125 mg/5 ml) and 100 ml (250 mg/5 ml): Prior to constitution, store at temperature below 25°C, in tightly closed containers. Avoid excessive heat and protect from light. After constitution as directed on the container label, keep tightly closed, store under refrigeration (2-8°C), and discard any unused portion after 14 days. If stored at temperature below 25°C, after constitution, discard any unused portion after 7 days.

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