Isticilline

Uses

Isticilline 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.

Isticilline 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 Infections

How Isticilline works

By binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, Isticilline 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 Isticilline interferes with an autolysin inhibitor.

Dosage

Isticilline 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.

Food Interaction

• Take on an empty stomach.

[Moderate] ADJUST DOSING INTERVAL: Certain penicillins may exhibit reduced gastrointestinal absorption in the presence of food.

The therapeutic effect of the antimicrobial may be reduced.

MANAGEMENT: The interacting penicillin should be administered one hour before or two hours after meals.

Penicillin V and amoxicillin are not affected by food and may be given without regard to meals.

Isticilline Hypertension interaction

[Moderate] Parenteral ampicillin sodium contains approximately 67 to 71 mg (2.9 to 3.1 mEq) of sodium per each gram of ampicillin activity.

The combination, ampicillin-sulbactam, contains approximately 115 mg (5 mEq) of sodium per 1.5 gram of total drug.

The sodium content should be considered when these products are used in patients with conditions that may require sodium restriction, such as congestive heart failure, hypertension, and fluid retention.

Isticilline Drug Interaction

Unknown: amoxicillin / clavulanate, amoxicillin / clavulanate, diphenhydramine, diphenhydramine, ciprofloxacin, ciprofloxacin, furosemide, furosemide, acetaminophen, acetaminophen, acetaminophen, acetaminophen, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol, ondansetron, ondansetron

Isticilline Disease Interaction

Major: colitisModerate: mononucleosis, sodium, renal dysfunction, hemodialysis

Elimination Route

Isticilline is excreted largely unchanged in the urine.

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).

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