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Ampicillin


DESCRIPTION
Ampicillin Capsule 250 (Size 2, Black/Red, marked 'UPHA/AMP 250')
Ampicillin Capsule 500 (Size 0, Scarlet/Black, marked 'UPHA/AMP 500')

Ampicillin Tablet 250 (10mm, round, flat, scored, marked 'UP/250' white tablet)

Ampicillin Tablet 500 (Capsule shape, scored, marked 'UP 500' white tablet)
Ampicillin Granules 125 Ampicillin Granules 250 (An almost white powder when reconstituted forms a pink, mixed fruit flavoured homogeneous suspension.)


INDICATIONS
Ampicillin is an aminopenicillin, which has activity against penicillin-sensitive gram-positive bacteria, as well as Escherichia coli, Proteus mirabilis, Salmonella sp., Shigella sp., and Haemophilus influenzae. However, many Enterobacteriaceae, H. Influenzae, Salmonella and Shigella species are resistant to this penicillin because of beta-lactamase production by these organisms. It is inactive against Pseudomonas aeruginosa. Oral ampicillin can be administered for the treatment of the following caused by susceptible bacterial organisms:


Bronchitis

Sinusitis
Biliary Tract Infections

Urinary Tract Infections
Gonorrhoea

Peritonitis
Acute Otitis Media

Gastro-enteritis (including E. Coli enteritis, Salmonella enteritis and shigellosis)
Epiglottitis
Pharyngitis

Typhoid Fever (caused by Salmonella typhi)
Pneumonia


Ampicillin is a possible alternative to erythromycin for chlamydial infections in pregnant women. Ampicillin is also indicated as prophylaxis for perinatal streptococcal infections and bacterial endocarditis.

MECHANISM OF ACTION
Ampicillin is bactericidal and acts by inhibiting bacterial cell wall synthesis. Its action is dependent on its ability to reach and hind penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes responsible for the assembling and reshaping of the bacterial cell wall during growth and division. PBPs inactivation by ampicillin results in the weakening and lysis of the bacterial cell wall.


PHARMACOLOGY
Ampicillin is moderately well absorbed from the GIT after oral administration. Ampicillin is relatively acid-stable. Food can interfere with the absorption of ampicillin so doses should preferable he taken at least 30 minutes before meals. Peak plasma concentrations of about 26 microgram per ml have been observed 1-2 hours after a dose of 500mg. Ampicillin is widen distributed and therapeutic concentrations can be achieved in ascitic, pleural and joint fluids, It crosses the placenta and small amounts are excreted in breast milk. Little ampicillin passes into the CSF unless the meninges are inflamed. About 20% is plasma protein bound. The plasma half-life is about 1-1.5 hours and this increases in renal failure (7-20 hours), neonates and the elderly. Ampicillin is metabolised to some extent to penicilloic acid which is excreted in the urine. About 20-40% of an oral dose is excreted unchanged in the urine in 6 hours by glomerular filtration and tubular secretion; urinary concentrations about 0.251 mg pet ml have been reported after a dose of 500mg. High concentrations have been reported in bile; it undergoes enterohepatic recycling and some may be excreted in the faeces.

 

DOSAGE

Adults :

Uncomplicated gonorrhoea ( gonococci-sensitive ) Single dose of 2 or 3.5g with probenecid 1g
Typhoid fever 25mg per kg of body weight every 6 hours

The usual adult dose is 0.25-1g every 6 hours. The usual adult prescribing limit is up to 4g a day.

 

Children :

Infants and children up to 20kg of body weight 12.5 to 25 mg per kg of body weight every 6 hours, or 16.7 to 33.3mg per kg of body weight every 8 hours
Children 20kg of body-weight and over Usual adult dose

Note : Ampicillin Paediatri Tablet and Ampicillin Granules 125/250 is available to improve medicine compliance in children.

 

OVERDOSAGE
There is no specific antidote In the case of overdosage, discontinue medication, treat symptomatically and institute supportive measures as required. Haemodialysis may aid in the removal of ampicillin from the blood. In patients with renal function impairment, ampicillin can be removed by haemodialysis but not by peritoneal dialysis.

 

Serious hypersensitivity reactions have been reported in patients on penicillin therapy. Serious anaphylactic reactions require immediate emergency treatment with parenteral epinephrine, oxygen, intravenous corticosteroids or air management (including intubation).

For Clostridium difficile colitis, mild cases may respond to discontinuation of the medication alone. Moderate to severe tares may require fluid, electrolyte, and protein replacement. In cases not responding to tine a bow measures, oral doses of the following maybe used:

 

Vancomycin 125mg every 6 hours for 5-10 days
Metronidazole 250-500mg every 8 hours
Cholestyramine 4g four times a day


If diarrhoea occurs, administration of antiperistaltic antidiarrhoeals ( eg. opioids, diphenoxylate and atropine combination, loperamide, paregoric ) is not recommended since they may delay the removal of toxins from the colon, thereby prolonging and/ or worsening the condition.

 

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