Sulbacin

Indications

• Bacterial infections
• Listerial meningitis
• Bronchitis
• Urinary tract infections
• Community-acquired pneumonia
• Salmonellosis

Dosage

Children: Refer to the BNF for Children for specific dosing: Neonate up to 7 days: 30 mg/kg every 12 hours; Neonate 7 to 20 days: 30 mg/kg every 8 hours; Neonate 21 to 28 days: 30 mg/kg every 6 hours.

Adults: 500 mg to 1 g every 6 hours, depending on the severity of the infection.

Mechanism of action

Ampicillin works by inhibiting bacterial cell wall synthesis, leading to cell lysis and death in susceptible bacteria.

Pharmacodynamics

Ampicillin exhibits bactericidal activity against a broad spectrum of gram-positive and some gram-negative bacteria, including Streptococcus spp., Enterococcus spp., and certain E. coli strains.

Pharmacokinetics

Ampicillin is well absorbed from the gastrointestinal tract, with a bioavailability of approximately 50-70%. It is distributed widely in body tissues and fluids, including the central nervous system. It is primarily eliminated by the kidneys through glomerular filtration and tubular secretion.

Adverse effects

• Colitis haemorrhagic
• Skin rash

Interactions

• Allopurinol (increases risk of skin rash)

Precautions

• Caution in renal impairment
• Potential for electrolyte accumulation with intravenous use

Pregnancy

Not known to be harmful.

Breast-feeding

Trace amounts in milk, but appropriate to use.

Storage

Store in a cool, dry place, protected from light.

Formulations

• Ampicillin 500 mg capsules
• Ampicillin 125 mg/5 ml oral suspension
• Ampicillin 25 mg per 1 ml oral suspension
• Ampicillin powder for injection

Indications

• Infections caused by beta-lactamase producing organisms
• Complicated skin and soft tissue infections
• Intra-abdominal infections
• Respiratory tract infections
• Urinary tract infections

Dosage

Children: Refer to BNF for Children for specific dosing recommendations based on the child's age, weight, and the type of infection.

Adults: Refer to BNF for specific dosing recommendations based on the type and severity of the infection.

Mechanism of action

Sulbactam is a competitive, irreversible inhibitor of bacterial beta-lactamases, particularly potent against class C beta-lactamases. It binds to the active site of the enzyme, preventing it from hydrolyzing beta-lactam antibiotics, which enhances the effectiveness of these antibiotics against resistant bacterial strains.

Pharmacodynamics

When administered with beta-lactam antibiotics, sulbactam broadens their antibacterial spectrum by inhibiting the enzymes responsible for their hydrolysis. Although sulbactam has weak intrinsic antibacterial activity on its own, it can effectively bind to penicillin-binding proteins in certain bacteria, contributing to its therapeutic effect. It helps restore the activity of beta-lactam antibiotics against a wide range of beta-lactamase-producing gram-positive and gram-negative bacteria.

Pharmacokinetics

Sulbactam is administered parenterally and is typically well absorbed. It has a short half-life, necessitating frequent dosing when used alone. The drug is primarily excreted unchanged in the urine. Its pharmacokinetic profile may vary based on the formulation used and the presence of co-administered antibiotics.

Pregnancy

There is limited data on the use of sulbactam in pregnancy. It should only be used if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

It is not known if sulbactam is excreted in human milk. Caution is advised when administering to breastfeeding women.

Storage

Store in a cool, dry place, away from direct light. Protect from moisture.

Formulations

• Injectable solution

Indications

• Bacterial infections
• Respiratory tract infections
• Urinary tract infections
• Skin and soft tissue infections
• Intra-abdominal infections

Dosage

Children: Refer to the BNF for Children for appropriate dosing recommendations

Adults: Refer to the BNF for specific dosing guidelines based on the infection type and severity.

Mechanism of action

Sultamicillin works by inhibiting the synthesis of bacterial cell walls. Ampicillin, a penicillin derivative, binds to penicillin-binding proteins (PBPs) located inside the bacterial cell wall, disrupting the transpeptidation process necessary for cell wall structural integrity. Sulbactam, a beta-lactamase inhibitor, protects ampicillin from hydrolysis by certain bacteria that produce beta-lactamase enzymes, thus enhancing the efficacy of the ampicillin component.

Pharmacodynamics

The pharmacodynamics of sultamicillin involve its bactericidal action against susceptible bacteria. It achieves this by interfering with bacterial cell wall synthesis, leading to cell lysis and death. The addition of sulbactam broadens the spectrum of activity against organisms that would otherwise be resistant to ampicillin alone. The combination therapy increases the likelihood of therapeutic success in polymicrobial infections.

Pharmacokinetics

Sultamicillin is administered intravenously or intramuscularly, leading to rapid absorption. Once in circulation, it is distributed throughout body tissues and fluids. The bioavailability is high, with peak plasma concentrations reached shortly after administration. Sultamicillin is metabolized in the liver, and its metabolites, along with some unchanged drug, are excreted primarily through the kidneys. The half-life of sultamicillin is approximately 1 to 2 hours, necessitating multiple doses for sustained therapeutic effects.

Contra-indications

• Hypersensitivity to sultamicillin, penicillins or any of the excipients
• History of severe allergic reactions to beta-lactam antibiotics

Adverse effects

• Gastrointestinal disturbances such as nausea, vomiting, and diarrhea
• Allergic reactions including rash and urticaria
• Hematological reactions such as eosinophilia and thrombocytopenia
• Liver enzyme elevations
• Superinfection due to prolonged use

Interactions

• Anticoagulants - sultamicillin may enhance the effects of anticoagulants
• Probenecid - may increase sultamicillin levels by decreasing renal excretion
• Other antibiotics - may have additive or antagonistic effects

Precautions

• Renal impairment - dosage adjustments may be necessary
• History of gastrointestinal disease, particularly colitis
• Use with caution in patients with liver impairment
• Monitor for signs of superinfection during prolonged therapy

Pregnancy

Sultamicillin should be used in pregnancy only if the potential benefit justifies the potential risk to the fetus. Consult relevant guidelines and clinical judgment.

Breast-feeding

Sultamicillin is excreted in breast milk, and caution should be exercised when administering to nursing mothers. Monitor infant for possible side effects.

Storage

Store below 25°C. Protect from moisture and light. Keep out of reach of children.

Formulations

• Oral tablets
• Injectable solution

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. SINCE PENICILLIN HAS NO EFFECT ON EXISTING CELL WALLS, BACTERIA MUST BE MULTIPLYING FOR BACTERICIDAL ACTION OF PENICILLIN TO BE MANIFEST. /PENICILLINS/ The penicillins and their metabolites are potent immunogens because of their ability to combine with proteins and act as haptens for acute antibody-mediated reactions. The most frequent (about 95 percent) or "major" determinant of penicillin allergy is the penicilloyl determinant produced by opening the beta-lactam ring of the penicillin. This allows linkage of the penicillin to protein at the amide group. "Minor" determinants (less frequent) are the other metabolites formed, including native penicillin and penicilloic acids. /Penicillins/ Bactericidal; inhibit bacterial cell wall synthesis. Action is dependent on the ability of penicillins to reach and bind penicillin binding proteins located on the inner membrane of the bacterial cell wall. Penicillin binding proteins (which include transpeptidases, carboxypeptidases, and endopeptidases) are enzymes that are involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Penicillins bind to, and inactivate, penicillin binding proteins, resulting in the weakening of the bacterial cell wall and lysis. /Penicillins/

Pharmacodynamics

Ampicillin is a penicillin beta-lactam antibiotic used in the treatment of bacterial infections caused by susceptible, usually gram-positive, organisms. The name "penicillin" can either refer to several variants of penicillin available, or to the group of antibiotics derived from the penicillins. Ampicillin has <i>in vitro</i> activity against gram-positive and gram-negative aerobic and anaerobic bacteria. The bactericidal activity of Ampicillin results from the inhibition of cell wall synthesis and is mediated through Ampicillin binding to penicillin binding proteins (PBPs). Ampicillin is stable against hydrolysis by a variety of beta-lactamases, including penicillinases, and cephalosporinases and extended spectrum beta-lactamases.

Mechanism of action

Sulbactam is a competitive, irreversible bacterial beta (β)-lactamase inhibitor. It is reported to be more potent against class C beta-lactamases.

Pharmacodynamics

When given together with beta-lactam antibiotics, sulbactam broadens their antibacterial spectrum by blocking the enzyme involved in their hydrolysis. Sulbactam alone possesses weak intrinsic antibacterial activity except against the _Neisseriaceae_, _Acinetobacter spp._, and _Bacteroides fragilis_ as it can bind to the penicillin-binding proteins. Sulbactam restores the activity of beta-lactam antibiotics against a range of beta-lactamase-producing gram-positive and gram-negative bacteria.