Antibiotic Ampicillin Pharmacology and Mechanism of action

 Indication:
For treatment of infection (Respiratory, GI, UTI and meningitis) due to E. coli, P. mirabilis, enterococci, Shigella, S. typhosa and other Salmonella, nonpenicillinase-producing N. gononhoeae, H. influenzae, staphylococci, streptococci including streptoc

Side Effects 

•     fever, sore throat, and headache with a severe blistering, peeling, and red skin rash;


•     fever, chills, body aches, flu symptoms;


•     easy bruising or bleeding, unusual weakness;


•     urinating less than usual or not at all;


•     agitation, confusion, unusual thoug


•     diarrhea that is watery or bloody;


•     hts or behavior; or


•     seizure (black-out or convulsions).

Less serious side effects may include

•     nausea, vomiting, stomach pain;


•     vaginal itching or discharge;


•     headache;


•     swollen, black, or "hairy" tongue; or


•     thrush (white patches or inside your mouth or throat).

Pharmacology - Ampicillin and the other aminopenicillins have increased activity against many strains of gram negative aerobes not covered by either the natural penicillins or penicillinase-resistant penicillins, including some strains of E. coli, Klebsiella and Haemophilus. Like the natural penicillins they are susceptible to inactivation by beta-lactamase-producing bacteria (e.g., Staph aureus). Although not as active as the natural penicillins, they do have activity against many anaerobic bacteria, including Clostridial organisms. Organisms that are generally not susceptible include Pseudomonas aeruginosa, Serratia, Indole-positive Proteus (Proteus mirabilis is susceptible), Enterobacter, Citrobacter, and Acinetobacter. The aminopenicillins also are inactive against Rickettsia, mycobacteria, fungi, Mycoplasma, and viruses.
Mechanism of action
By binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, Ampicillin inhibits the third and last stage of bacterial cell wall synthesis. Cell lysis is then mediated by bacterial cell wall autolytic enzymes such as autolysins; it is possible that Ampicillin interferes with an autolysin inhibitor.

Dosing
Adults and Children Weight Over 20 kg.
For genitourinary or gastrointestinal tract infections other than gonorrhea in men and women, the usual dose is 500 mg qid in equally spaced doses; severe or chronic infections may require larger doses.

For the treatment of gonerrhea in both men and women, a single oral dose of 3.5 grams of ampicillin administered simultaneously with 1 gram of probenecid is recommended. Physicians are cautioned to use no less than the above recommended dosage for the treatment of gonorrhea. Follow-up cultures should be obtained from the original site(s) of infection 7 to 14 days after therapy. In women, it is also desirable to obtain culture test-of-cure from both the endo-cervical and anal canals. Prolonged intensive therapy is needed for complications such as proshtitis and epididymitis. For respiratory tract infections, the usual dose is 250 mg qid in equally spaced doses.

Children Weighing 20 kg or Less
For genitourinary or gastrointestinal tract infections, the usual dose is 100 mg/kg/day total, qid in equally divided and spaced doses. For respiratory infections, the usual dose is 50 mg/kg/day total, in equally divided and spaced doses three to four times daily. Doses for children should not exceed doses recommended for adults,

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Ditulis oleh: Unknown - Thursday, 11 August 2011