ampicillin report clinpharm-2

8/10/2019 Ampicillin Report Clinpharm-2

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PENICILLINS

BY:ESPAA, LOREBETH L.

FLORES, CHIENA MAE S.


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AMPICILLIN

( (2S,5R,6R)-6-([(2R)-2-amino-2-

phenylacetyl]amino) -3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2- carboxylic acid)

Innovator: Penbritin (SmithKline Beecham)


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Mechanism of Action

By binding to specific penicillin-bindingproteins (PBPs) located inside the bacterial

cell wall

Spectrum

Ampicillin has in vitro activity againstgram-positive and gram-negative aerobicand anaerobic bacteria

Chemistry and Stability


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Pharmacokinetics

Absorption

Well absorbed from GI tract. C max is

approximately 3 mcg/mL (500 mgcapsules) and 3.4 mcg/mL (500 mg oral

suspension). Food affects absorption;

take on empty stomach.


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Distribution

Diffuses readily into most body tissues andfluids; penetrates into the CSF and brain

only when meninges are inflamed.

Approximately 20% protein bound;excreted in breast milk.

Elimination/Excretion

Excreted largely unchanged in the urine


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Uses

Treatment of respiratory, GI, and GU

tract and soft tissue infections

bacterial meningitis enterococcal endocarditis

Septicemia gonococcal infections caused by

susceptible microorganisms.


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CAUTION Fever

sore throat and headache with a severeblistering

peeling and red skin rash

diarrhea that is watery or bloody fever

Chills

body aches

flu symptoms

easy bruising or bleeding

unusual weakness urinating less than

usual or not at all


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Agitation

Confusion

unusual thoughts or behavior

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

thrush (white patches or inside your mouth or throat)


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Pregnancy

Category Risk B

Pediatric An uncontrolled observation of the

breastfed infants of mothers taking

ampicillin noted a seeming increase in

cases of diarrhea and candidiasis that

was attributed to ampicillin in

breastmilk.


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TOXICITY ToxIcity of ampicillin trihydrate was studied in acute

and chronic experiments. It was shown that the antibiotic had low acute

toxicity, did not cumulate and had no skin-irritating

effect. On its inhalation in concentrations of 5 mg/m3 for 4

months, ampicillin induced allergization of albino

rats, decreased their immunity.

The general toxic effect of the drug was slightly

pronounced. Ampicillin in a concentration of 0.1

mg/m3 induced tension of the immunological

reactivity of the organism.


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Drug Interactions

AllopurinolIncreases potential for ampicillin-induced skin rash.

Atenolol

Antihypertensive and antianginal effects may beimpaired.

Contraceptives, oral

May reduce efficacy of oral contraceptives. Tetracyclines

May impair bactericidal effects of ampicillin.


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Pharmaceutical Dosage Form

- Injection powder for solution

Administration- Intramuscular, Intravenous


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PREPARATION

250 mg in

10mL vial

500mg in

10ml vial

1g in

15mL vial 2g in

24mL vial


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Clinical comparative study of

sulbactam/ampicillin and

imipenem/cilastatin in elderly patients withcommunity-acquired pneumonia.

PHASE: 3

METHODOLOGY: Randomized Controlled Trial

RATIONALE:To evaluate the clinical usefulnessof sulbactam/ampicillin therapy for community-

acquired pneumonia in the elderly


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RESULTS: Overall clinical efficacy of

sulbactam/ampicillin therapy (6 g/day) in

these patients (efficacy rate: 91.4%) wascomparable to that of imipenem/cilastatin

therapy (1 g/day; efficacy rate: 87.5%),

when each therapy was administeredintravenously twice daily for 7-14 days. With

regard to clinical efficacy based on disease

severity, bacteriological efficacy,improvement of chest X-ray findings and

adverse reactions, the two therapies were

comparable.

ampicillin report clinpharm-2

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