Ampicillin + Sulbactam

Oral
Intra-abdominal infections, Pyelonephritis, Respiratory tract infections, Urinary tract infections

Oral
Uncomplicated gonorrhoea

Parenteral
Gynaecological infections, Intra-abdominal infections, Skin and skin structure infections

Oral:

CrCl (mL/min)	Dosage
≤30	Reduce dosing frequency.

Parenteral:
Haemodialysis patient: 1.5-3 g once 24 hrly immediately after dialysis.

CrCl (mL/min)	Dosage
5-14	1.5-3 g 24 hrly.
15-29	1.5-3 g 12 hrly.

May be taken with or without food.

Powd for oral susp: Add water according to manufacturer's instructions, to provide a susp containing 250 mg/5 mL. IM: Add 3.2 mL or 6.4 mL of sterile water for inj or lidocaine HCl 0.5% or 2% inj to vials containing 1.5 g or 3 g, respectively, to provide a soln containing 375 mg per mL (ampicillin 250 mg and sulbactam 125 mg per mL). IV inj or infusion: Add 3.2 mL or 6.4 mL of sterile water for inj to vials containing 1.5 g or 3 g, respectively, to provide a soln containing 375 mg per mL. Further dilute w/ a compatible IV soln to yield soln containing 3-45 mg per mL (ampicillin 2-30 mg and sulbactam 1-15 mg per mL). ADD-Vantage^® vial: Add NaCl 0.9% diluents provided according to manufacturer's directions.

Y-site: Aminoglycosides, amiodarone, amphotericin B cholesteryl sulfate complex, ciprofloxacin, idarubicin, nicardipine, ondansetron.

Hypersensitivity to ampicillin, sulbactam or other β-lactam antibacterials (e.g. penicillins, cephalosporins). History of cholestatic jaundice/hepatic dysfunction associated w/ ampicillin and sulbactam.

Patient w/ infectious mononucleosis. Hepatic and renal impairment. Pregnancy and lactation.

Diarrhoea, nausea, vomiting, flatulence, abdominal discomfort/distension, rectal bleeding, glossitis, gastritis, stomatitis, black/hairy tongue, rash, urticaria, pruritus, dry skin, erythema multiforme, exfoliative dermatitis, cholestatic hepatitis and cholestasis; pain, phlebitis, thrombophlebitis and inflammation at inj site.
Potentially Fatal: Anaphylaxis, Clostridium difficile-associated diarrhoea, hepatotoxicity.

Parenteral/PO: B

Monitor haematologic, renal and hepatic function w/ prolonged therapy. Monitor for signs of anaphylaxis during 1st dose. Regular monitoring of hepatic function in patients w/ pre-existing hepatic impairment at regular intervals.

Symptoms: Neurological effects including convulsions. Management: May be removed by haemodialysis.

Increased and prolonged serum levels w/ probenecid. Increased incidence of rashes w/ allopurinol. May reduce effectiveness of oestrogen-containing OC. May increase risk of methotrexate toxicity. Bacteriostatic drugs (e.g. chloramphenicol) may interfere w/ the bactericidal effect of ampicillin. Additive effect w/ anticoagulants.

False positive urine glucose test using cupric sulfate (e.g. Clinitest^®, Benedict's soln, Fehling's soln).

Description: Ampicillin binds to 1 or more of the penicillin-binding proteins (PBPs), thus inhibiting the final transpeptidation step of peptidoglycan synthesis in bacterial cell walls. Sulbactam inhibits the activity of β-lactamases and extends the spectrum of ampicillin to include β-lactamase producing organisms.
Pharmacokinetics:
Absorption: Ampicillin: Moderately well absorbed from the GI tract. Time to peak plasma concentration: Approx 1-2 hr. Sulbactam: Poorly absorbed from the GI tract.
Distribution: Ampicillin: Widely distributed; therapeutic conc achieved in ascitic, pleural and joint fluids; a little diffusion into CSF except when meninges are inflamed. It crosses the placenta and enters breast milk (small amounts). Plasma protein binding: Approx 20%. Sulbactam: Widely distributed in bile, blister and tissue fluids; distributed in CSF when meninges are inflamed. Plasma protein binding: 38%.
Metabolism: Ampicillin: Converted to some extent to penicilloic acid. Sulbactam: Undergoes enterohepatic recycling.
Excretion: Ampicillin: Via urine (approx 20-40% of oral dose as unchanged drug); faeces. Plasma half-life: Approx 1-1.5 hr. Sulbactam: Via urine (approx 75-85% as unchanged drug). Elimination half-life: 1-1.3 hr.

Tab (375 mg): Store below 30°C. Powd for oral susp/tab (750 mg): Store below 25°C. Reconstituted oral susp: Store between 2-8°C. Powd for inj: Store between 20-25°C. Reconstituted soln: IV: 45 mg/mL soln: Store at 25°C; 30 mg/mL soln: Store at 4°C; ADD-Vantage® vial: Store at 25°C.

Penicillins

Ampicillin Sodium and Sulbactam Sodium Injection, Powder for Solution (Sandoz Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 19/06/2015.

Anon. Ampicillin and Sulbactam. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 18/06/2015.

Buckingham R (ed). Ampicillin. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 19/06/2015.

Buckingham R (ed). Sulbactam. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 19/06/2015.

Buckingham R (ed). Sultamicillin. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 19/06/2015.

McEvoy GK, Snow EK, Miller J et al (eds). Ampicillin Sodium and Sulbactam Sodium. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 18/06/2015.

Unasyn (Ampicillin Sodium/Sulbactam Sodium) Injection. U.S. FDA. https://www.fda.gov/. Accessed 19/06/2015.