Ampimax Tablet

Pharmacologic Classification: Antibacterial.
Pharmacology: Ampicillin is an aminopenicillin which exerts its bactericidal activity by interfering with the synthesis of the bacterial cell wall. It inhibits transpeptidase, an enzyme responsible for the synthesis of the peptidoglycan layer of the bacterial cell wall. This results in the interruption of peptidoglycan synthesis causing spheroplast formation and bacterial lysis.
Sulbactam is a penicillanic acid sulfone with beta-lactamase inhibitory properties. It is an irreversible inhibitor of many plasmid-mediated and some chromosomal beta-lactamases and has a similar spectrum of beta-lactamase inhibition as clavulanic acid. Sulbactam can therefore enhance the activity of penicillins and cephalosporins against many strains of bacteria.
Pharmacokinetics: Bioavailability: After oral administration, sultamicillin is hydrolyzed during absorption to equivalent molar quantities (1:1) of ampicillin and sulbactam. The bioavailability of an oral dose of sultamicillin is 80% of an equal intravenous (IV) dose of ampicillin and sulbactam.
Food does not affect the systemic bioavailability of sultamicillin. After sultamicillin administration, peak serum levels of ampicillin are approximately twice those of an equal dose of oral ampicillin.
Elimination half-lives are about 1 hour and 0.75 hour for ampicillin and sulbactam, respectively, in healthy volunteers, with 50-75% of each drug being excreted unchanged in the urine. The elimination half-lives are increased in the elderly and in patients with renal impairment.
Probenecid decreases the renal tubular secretion of both ampicillin and sulbactam.

For the treatment of the following infections caused by susceptible microorganisms: Upper respiratory tract infections including sinusitis, otitis media, epiglottitis, and tonsillitis; Lower respiratory tract infections including bacterial pneumonia and bronchitis; Urinary tract infections including pyelonephritis; Intraabdominal infections including peritonitis, cholecystitis, endometritis, and pelvic cellulitis; Bacterial septicemia; Skin and skin structure infections; Bone and joint infections; Gonococcal infections.
As step down treatment for infections due to susceptible organisms, initially given antimicrobial therapy, particularly parenteral ampicillin-sulbactam.

Usual Dose in Adults and Children weighing ≥ 30 kg who can swallow tablet whole: 750 mg twice daily.
Usual Duration of Treatment: 5 to 14 days which may be extended depending on the type and severity of infection.
Non-complicated gonococcal infection: 2.25 g (three 750 mg tablets) as a single dose.
For most infections, therapy should be continued for a minimum of 48 hours after the patient becomes asymptomatic or evidence of bacterial eradication has been obtained.
In the treatment of group A β-hemolytic streptococcal infections, penicillin therapy should be continued for at least 10 days to help prevent the occurrence of acute rheumatic fever or glomerulonephritis.
Cases of gonorrhea with a suspected lesion of syphilis should have dark field examinations before receiving sultamicillin and monthly serological tests for a minimum of four months.
Or, as prescribed by a physician.

Serious and occasionally fatal hypersensitivity (anaphylactic) reactions have been reported in patients on penicillin therapy including sultamicillin. These reactions are more likely to occur in individuals with a history of penicillin hypersensitivity and/or hypersensitivity to multiple allergens. Careful inquiry should be made concerning previous hypersensitivity to penicillins, cephalosporins or other drugs before initiating therapy with sultamicillin. If an allergic reaction occurs, the drug should be discontinued and appropriate therapy instituted.
Serious anaphylactoid reactions require immediate emergency treatment with epinephrine. Oxygen, IV steroids, and airway management, including intubation, should be administered as indicated.
Clostridium difficile-associated diarrhea (CDAD) and colitis have been reported with the use of nearly all antibacterial agents, including sultamicillin, and may range in severity from mild to life threatening. It is important to consider this diagnosis in patients who present with diarrhea following administration of antibacterial agents.
The renal, hepatic, and hematologic status of patients undergoing prolonged treatment with aminopenicillins should be evaluated periodically, particularly when administered to patients with liver or renal impairment.
Prescribing sultamicillin in the absence of a proven or strongly suspected bacterial infection or a prophylactic indication is unlikely to provide benefit to the patient and increases the risk of antibiotic resistance.
As with other antibacterial agents, long term or repeated use may result in overgrowth of non-susceptible organisms, including fungi.

 

Sultamicillin is generally well-tolerated. Most adverse effects (AEs) are mild to moderate in severity and are normally tolerated with continued treatment.
Body as a Whole: Fatigue/malaise and headache have been rarely observed.
Dermatologic/Hypersensitivity reactions: Rash, itching, pemphigus vulgaris, angioedema, dermatitis, urticaria; allergic reaction, anaphylaxis/anaphylactic shock, anaphylactoid reaction, superinfections, adult respiratory distress syndrome.
Gastrointestinal (GI): Vomiting, nausea, diarrhea, loose stools, epigastric distress, melena, abdominal pain/cramps.
Nervous system: Taste disturbances, ototoxicity, dizziness, drowsiness/sedation.
Renal: Kidney function disorder.
Respiratory: Dyspnea.
The following AEs have also been reported for aminopenicillin-class antibiotics including ampicillin and/or parenteral ampicillin/sulbactam: Dermatologic/Hypersensitivity reactions: Pruritus, dry skin, erythema; rare reports of exfoliative dermatitis, toxic epidermal necrolysis, erythema multiforme, and Stevens-Johnson syndrome; serum sickness-like reactions (urticaria or skin rash accompanied by arthritis, arthralgia, myalgia, and frequently fever); systemic allergic reactions (characterized by neck tightness, difficulty and pain when breathing, generalized weakness, and hypertension); facial swelling; positive direct antiglobulin (Coombs' test).
GI: Anorexia, gastritis, black hairy tongue, glossitis, stomatitis, CDAD and colitis; acute, transient enterocolitis with severe abdominal pain and bloody diarrhea, but without evidence of CDAD and colitis; acute pancreatitis; flatulence, abdominal discomfort or distension, rectal bleeding.
Nervous system: Headache, confusion; rare reports of convulsions/myoclonic seizures; generalized seizures.
Hematologic: Anemia, hemolytic anemia, hypothrombinemia, eosinophilia, leukopenia, neutropenia, agranulocytosis, thrombocytopenia, thrombocytopenic purpura, abnormal platelet aggregation, prolongation of bleeding time, and prolongation of activated partial thromboplastin time (APTT); decreased hemoglobin concentration, hematocrit, erythrocyte, lymphocyte, and platelet counts; increased lymphocyte, monocyte, basophil, eosinophil, and platelet counts.
Hepatobiliary: Transient elevations of aspartate aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase, lactate dehydrogenase (LDH), creatine kinase (CK), bilirubin, and γ-glutamyltransferase (γ-glutamyltranspeptidase, GT, GGTP); bilirubinemia, abnormal hepatic function, and jaundice.
Renal: Rare reports of acute interstitial nephritis; glomerulonephritis; increased blood urea nitrogen (BUN) and serum creatinine concentrations; presence of red blood cells and hyaline casts in urine, urine retention, dysuria, hematuria, crystalluria.
Other Adverse Effects: Decreased concentrations of serum albumin and total protein; chest pain or tightness, edema, chills, throat tightness, substernal pain, epistaxis, mucosal bleeding; changes in smell perception.

Penicillins

J01CR04 - sultamicillin ; Belongs to the class of penicillin combinations, including beta-lactamase inhibitors. Used in the systemic treatment of infections.

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