Ambacitam

Ambacitam Uses, Dosage, Side Effects, Food Interaction and all others data.

Ampicillin inhibits bacterial cell wall synthesis by binding to 1 or more of the penicillin-binding proteins (PBPs) which in turn inhibit the final transpeptidation step of peptidoglycan synthesis in bacterial cell walls. Bacteria eventually lyse due to ongoing activity of cell wall autolytic enzymes (autolysins and murein hydrolases) while cell wall assembly is arrested.

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 in vitro 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.

Sulbactam is a β-lactamase inhibitor given in combination with β-lactam antibiotics to inhibit β-lactamase, an enzyme produced by bacteria that destroys antibiotic activity.

Trade Name Ambacitam
Generic Ampicillin + Sulbactam
Type
Therapeutic Class
Manufacturer
Available Country Philippines, Thailand, Vietnam
Last Updated: September 19, 2023 at 7:00 am
Ambacitam
Ambacitam

Uses

Ampicillin is used for the treatment of infections caused by susceptible strains of the designated organism listed below:

  • Infections of the Genitourinary Tract Including Gonorrhea: E. coli, P. mirabilis, enterococci, Shigella, S. typhosa and other Salmonella, and nonpenicillinase-producing N. gononhoeae.
  • Infections of the Respiratory Tract: Nonpenicillinase-producing H. influenzae and staphylococci, and streptococci including streptococcus pneumoniae.
  • Infections of the Gastrointestinal Tract: Shigella, S. typhosa and other Salmonella, E. coli, P. mirabilis, and enterococci.
  • Meningitis: O. Meningitides.

Bacteriology studies to determine the causative organisms and their sensetivity to ampicillin should be performed. Therapy may be instituted prior to the results of susceptibility testing.

Sulbactam is an beta-lactamase inhibitor antibiotic combined with other antibiotics to treat a variety of susceptible bacterial infections.

Sulbactam is currently available in combination products with ampicillin. Within this formulation it is indicated for the treatment of infections due to susceptible strains of the designated microorganisms in the conditions listed below. Skin and Skin Structure Infections caused by beta-lactamase producing strains of Staphylococcus aureus, Escherichia coli, Klebsiella spp. (including K. pneumoniae), Proteus mirabilis, Bacteroides fragilis, Enterobacter spp., and Acinetobacter calcoaceticus. Intra-Abdominal Infections caused by beta-lactamase producing strains of Escherichia coli, Klebsiella spp. (including K. pneumoniae), Bacteroides spp. (including B. fragilis), and Enterobacter spp. Gynecological Infections caused by beta-lactamase producing strains of Escherichia coli, and Bacteroides spp. (including B. fragilis).

Ambacitam is also used to associated treatment for these conditions: Bacterial Infections, Bloodstream Infections, Endocarditis, Gastrointestinal Infections, Genitourinary tract infection, Infection, Infection caused by eikenella corrodens, Listeria infection, Meningitis, Bacterial, Pertussis, Respiratory Tract Infections (RTI), Salmonella, Salmonella Typhi Infection, Shigella, Skin Infections, Bacterial, Subcutaneous bacterial infection, Urinary Tract Infection, Perinatal group B streptococcus, Susceptible Bacterial InfectionsAnimal bite, Bacterial Infections, Bacterial Infections caused by Beta lactamase producing bacteria, Bacterial Sinusitis, Bites, Human, Catheter Related Infections, Community Acquired Pneumonia (CAP), Gynaecological infection, Infective Endocarditis, Intra-Abdominal Infections, Nosocomial Pneumonia, Postoperative Infections, Postoperative Wound Infection, Skin and Subcutaneous Tissue Bacterial Infections, Complicated Bacterial Infections caused by Beta lactamase producing bacteria, Moderate Bacterial Infections, Severe Bacterial Infections

How Ambacitam works

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.

Sulbactam is an irreversible inhibitor of β-lactamase; by binding and inhibiting β-lactamase produced by bacterial cells, sulbactam is thereby able to prevent it from reducing antibiotic activity. Although sulbactam alone possesses little useful antibacterial activity, except against the Neisseriaceae, whole organism studies have shown that sulbactam restores ampicillin activity against beta-lactamase producing strains. In particular, sulbactam has good inhibitory activity against the clinically important plasmid mediated beta-lactamases most frequently responsible for transferred drug resistance. The presence of sulbactam in formulations with ampicillin effectively extends the antibacterial spectrum of ampicillin to include many bacteria normally resistant to it and to other beta-lactam antibacterials. Thus, products with ampicillin + sulbactam possess the properties of a broad-spectrum antibacterial and a beta-lactamase inhibitor.

Dosage

Ambacitam dosage

Intra-articular:Supplement in systemic therapy for treatment of susceptible infections-

  • Adult:500 mg daily.
  • Child:<10 yrHalf of adult routine dosage.

Intraperitoneal:

Supplement in systemic therapy for treatment of susceptible infections-

  • Adult:500 mg daily.
  • Child:<10 yrHalf of adult routine dosage.

Intrapleural:

Supplement in systemic therapy for treatment of susceptible infections-

  • Adult:500 mg daily.
  • Child:<10 yrHalf of adult routine dosage

Intravenous:

Meningitis-

  • Adult:2 gm 6 hrly.
  • Child:150 mg/kg daily in divided doses.

Intrapartum prophylaxis against group B Streptoccocal infection in neonates-

  • Adult:Initially, 2 gm via IV inj followed by 1 gm 4 hrly until delivery.

Oral:

Biliary tract infections, Bronchitis, Endocarditis, Gastroenteritis, Listeriosis, Otitis media, Perinatal streptococcal infections, Peritonitis-

  • Adult:0.25-1 gm 6 hrly.
  • Child:<10 yrHalf of adult routine dosage.

Typhoid and paratyphoid fever-

  • Adult:1-2 gm 6 hrly for 2 wk in acute infections, and 4-12 wk in carriers.

Uncomplicated gonorrhoea-

  • Adult:2 gm with 1 gm of probenecid as single dose, recommended to be repeated in female patients.

Urinary tract infections-

  • Adult:500 mg 8 hrly.

Parenteral:

Susceptible infections-

  • Adult:500 mg 6 hrly, via IM or slow IV inj over 3-5 min or by infusion.
  • Child:<10 yrHalf of adult routine dosage.

Septicaemia-

  • Adult:150-200 mg/kg daily. Initiate with IV admin for at least 3 days, then continue with IM inj 3-4 hrly. Continue treatment for at least 48-72 hr after the patient has become asymptomatic or when there is evidence of bacterial eradication. Recommended treatment duration for infections caused by group-A β-haemolytic streptococci: At least 10-days, to prevent occurrence of acute rheumatic fever or acute glomerulonephritis.
  • Child:Same as adult dose.

Should be taken on an empty stomach. Take 1 hr before or 2 hr after meals.

Intramuscular: Add 1.5 mL water for inj to 500 mg vial contents.

Intravenous: Dissolve 500 mg in 10 mL water for inj. May be added to infusion fluids or injected, suitably diluted into the drip tube.

Intra-articular: Dissolve 500 mg in up to 5 mL of water for inj or sterile procaine HCl 0.5% soln.

Intraperitoneal: Dissolve 500 mg in up to 10 mL water for inj.

Intrapleural: Dissolve 500 mg in 5-10 mL water for inj.

Side Effects

Nausea, vomiting, diarrhoea, erythematous maculo-papular rashes, sore mouth, black/hairy tongue, rash, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, angioedema, fever, joint pains, serum sickness-like symptoms, haemolytic anaemia, thrombocytopenia, leucopenia, neutropenia, coagulation disorders, prolonged bleeding time and prothrombin time, CNS toxicity (e.g. convulsions); paraesthesia, nephropathy, interstitial nephritis, hepatitis, cholestatic jaundice, moderate and transient increase in transaminases, Anaphylaxis, Clostridium difficile-associated diarrhoea (CDAD).

Precaution

Patient with history of β-lactam allergy. During renal impairment, Pregnancy and lactation.

Interaction

May reduce the efficacy of oral contraceptives. May alter INR while on warfarin and phenindione. May reduce the efficacy of oral typhoid vaccines. May reduce the excretion of methotrexate. Reduced excretion with probenecid and sulfinpyrazone, resulting to increased risk of toxicity. Allopurinol increases ampicillin-induced skin reactions. Reduced absorption with chloroquine. Bacteriostatic antibacterials (e.g. erythromycin, chloramphenicol, tetracycline) may interfere with the bactericidal action of ampicillin.

Volume of Distribution

Penetration of both ampicillin and sulbactam into cerebrospinal fluid in the presence of inflamed meninges has been demonstrated after IV administration.

Elimination Route

Peak serum concentrations are reached almost immediately following a 15-minute intravenous infusion of sulbactam + ampicillin. Mean peak serum levels for sulbactam range from 48 to 88 mcg/mL following intravenous administration of 2000 mg of ampicillin plus 1000 mg sulbactam. After an intramuscular injection of 1000 mg ampicillin plus 500 mg sulbactam, peak sulbactam serum levels ranging from 6 to 24 mcg/mL are attained.

Half Life

~1 hr

Elimination Route

Ampicillin is excreted largely unchanged in the urine.

Approximately 75 to 85% of both ampicillin and sulbactam are excreted unchanged in the urine during the first 8 hours after administration.

Pregnancy & Breastfeeding use

Pregnancy Category B. Either animal-reproduction studies have not demonstrated a fetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1st trimester (and there is no evidence of a risk in later trimesters).

Contraindication

Hypersensitivity to ampicillin and other penicillins.

Special Warning

Renal Impairment: CrCl<10: Dose reduction or increase in dose interval.

Acute Overdose

Symptoms: Nausea, vomiting and diarrhoea. Management: Symptomatic and supportive treatment. May be removed from the circulation by haemodialysis.

Storage Condition

Store between 20-25° C. Reconstituted oral susp: Store between 2-8° C (discard after 14 days).

Innovators Monograph

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