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PENICILLINS

BY:
ESPAÑA, LOREBETH L.
FLORES, CHIENA MAE S.

3-dimethyl-7-oxo-4-thia1-azabicyclo[3.AMPICILLIN • ( (2S.2.5R.carboxylic acid) Innovator: Penbritin (SmithKline Beecham) .0]heptane-2.6R)-6-([(2R)-2-amino-2phenylacetyl]amino) -3.

Chemistry and Stability Mechanism of Action By binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall Spectrum • Ampicillin has in vitro activity against gram-positive and gram-negative aerobic and anaerobic bacteria .

C max is approximately 3 mcg/mL (500 mg capsules) and 3.4 mcg/mL (500 mg oral suspension). Food affects absorption.Pharmacokinetics Absorption Well absorbed from GI tract. take on empty stomach. .

excreted in breast milk. Elimination/Excretion Excreted largely unchanged in the urine .Distribution Diffuses readily into most body tissues and fluids. Approximately 20% protein bound. penetrates into the CSF and brain only when meninges are inflamed.

Uses • Treatment of respiratory. . and GU tract and soft tissue infections • bacterial meningitis • enterococcal endocarditis • Septicemia • gonococcal infections caused by susceptible microorganisms. GI.

CAUTION • Fever • sore throat and headache with a severe blistering • 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 .

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

.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.

TOXICITY • ToxIcity of ampicillin trihydrate was studied in acute and chronic experiments.1 mg/m3 induced tension of the immunological reactivity of the organism. decreased their immunity. • The general toxic effect of the drug was slightly pronounced. • On its inhalation in concentrations of 5 mg/m3 for 4 months. Ampicillin in a concentration of 0. did not cumulate and had no skin-irritating effect. • It was shown that the antibiotic had low acute toxicity. ampicillin induced allergization of albino rats. .

oral May reduce efficacy of oral contraceptives. .Drug Interactions • Allopurinol Increases potential for ampicillin-induced skin rash. • Atenolol Antihypertensive and antianginal effects may be impaired. • Contraceptives. • Tetracyclines May impair bactericidal effects of ampicillin.

Injection powder for solution • Administration . Intravenous .• Pharmaceutical Dosage Form .Intramuscular.

PREPARATION • 250 mg in 10mL vial • 500mg in 10ml vial • 1g in 15mL vial • 2g in 24mL vial .

PHASE: 3 METHODOLOGY: Randomized Controlled Trial RATIONALE: To evaluate the clinical usefulness of sulbactam/ampicillin therapy for communityacquired pneumonia in the elderly .Clinical comparative study of sulbactam/ampicillin and imipenem/cilastatin in elderly patients with community-acquired pneumonia.

5%). bacteriological efficacy. improvement of chest X-ray findings and adverse reactions.RESULTS: Overall clinical efficacy of sulbactam/ampicillin therapy (6 g/day) in these patients (efficacy rate: 91. the two therapies were comparable. . With regard to clinical efficacy based on disease severity.4%) was comparable to that of imipenem/cilastatin therapy (1 g/day. efficacy rate: 87. when each therapy was administered intravenously twice daily for 7-14 days.