logo image

Cilastatin + Imipenem information from DrugsUpdate  

See Available Brands of Cilastatin + Imipenem in India

P - Caution when used during pregnancy
L - Caution when used during lactation

Imipenem/cilastatin is a broad spectrum beta-lactam antibiotic containing equal quantities of imipenem and cilastatin. It is related to the penicillin/cephalosporin family of antibiotics but is classified as belonging to the carbapenem class.

Pharmacodynamics

Pharmacokinetics

Imipenem is a potent inhibitor of bacterial cell wall synthesis and is bactericidal against a broad spectrum of pathogens. It is resistant to degradation by bacterial β-lactamases. Cilastatin is an inhibitor of dehydropeptidase I, an enzyme found in the brush border of the renal tubules. It is given as the sodium salt with imipenem to prevent its renal metabolism and protect against nephrotoxic effects.


Absorption
IM admin: 60-75% (imipenem); 95-100% (cilastatin).


Distribution
Rapidly and widely distributed to most tissues and fluids. Protein binding: 20% (imipenem) and 40% (cilastatin).


Metabolism
Imipenem: Metabolised renally by dehydropeptidase I; cilastatin: Partly metabolised renally.


Excretion
Via urine (about 70% as unchanged drug). Half-life: 2-3 hours (imipenem after IM admin).

Cilastatin + Imipenem Indications / Cilastatin + Imipenem Uses

Information Not Available

Cilastatin + Imipenem Adverse Reactions / Cilastatin + Imipenem Side Effects

Skin rashes, urticaria, eosinophilia, fever, nausea, vomiting, diarrhoea, tooth or tongue discoloration and altered taste. Erythema multiforme, exfoliative dermatitis. Pain and thrombophlebitis may occur at the injection site.


Potentially Fatal: Stevens-Johnson syndrome, toxic epidermal necrolysis.

Precautions

Hypersensitivity
Administer drug with caution to penicillin-sensitive patients due to possible cross-activity.

Renal Function
Dosage reduction or alteration of dosage interval is required.

Superinfection
May result in bacterial or fungal overgrowth of nonsusceptible organisms.

Benzyl alcohol
Benzyl alcohol as a preservative has been associated with toxicity in newborns, especially those younger than 3 months. Do not use diluents containing benzyl alcohol when IV is constituted for administration to pediatric patients.

CNS
IV administration may result in myoclonic activity confusional states or seizures.

Pseudomembranous colitis
Consider possibility in patients with diarrhea.


Overdosage
Symptoms
Seizures.

Special Precautions

Caution when used in patients with known hypersensitivity to other β-lactams due to possibility of cross-sensitivity. CNS disorders such as epilepsy; renal, hepatic impairment; pregnancy, lactation.

Other Drug Interactions

Concurrent admin with probenecid may increase the half-life of cilastatin. Increased risk of generalised seizures when used concurrently with ganciclovir.

Other Interactions

Information Not Available

Dosage

Intravenous
Susceptible infections
Adult: In terms of imipenem, 1-2 g daily in divided doses every 6-8 hours, given via IV infusion. Doses 250 or 500 mg are infused over 20-30 minutes, and doses of 750 mg or 1 g over 40-60 minutes.
Child: >40 kg: same as adult dose. >3 months and <40 kg: 15-25 mg/kg every 6 hours by IV infusion. Up to 90 mg/kg may be given to older children with cystic fibrosis.
Neonates and infants <3 months: 4 weeks-3 months, 25 mg/kg every 6 hours; 1-4 weeks, 25 mg/kg every 8 hours; up to 1 week, 25 mg/kg every 12 hours.
Max Dosage: Adults and children >40 kg: 4 g/day or 50 mg/kg. Children <40 kg: 2 g/day.

CrCl (ml/min)    Dosage Recommendation
31-70               500 mg every 6-8 hours
21-30               500 mg every 8-12 hours
6-20                 250 mg or 3.5 mg/kg (whichever is lower) every 12 hours
≤5                    Only give if haemodialysis started within 48 hours

Intravenous
Surgical prophylaxis
Adult: In terms of imipenem, 1 g given on induction of anaesthesia, followed by 1 g 3 hours later, with additional doses of 500 mg at 8 and 16 hours after induction if necessary.

Intramuscular
Mild to moderate susceptible infections
Adult: In terms of imipenem, 500 mg or 750 mg every 12 hours.

Intramuscular
Uncomplicated gonorrhoea
Adult: In terms of imipenem: A single 500 mg dose may be used.

Food(before/after)

Information Not Available

List of Contraindications

Cilastatin + Imipenem and Pregnancy

Caution when used during pregnancy.


Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Cilastatin + Imipenem and Lactation

Caution when used during lactation

Cilastatin + Imipenem and Children

Safety and efficacy in children younger than 12 years of age are not established with IM use. IV use in newborns to 16 years of age (with non-CNS infections) is supported by evidence from adequate and well-controlled studies. IV use is not recommended in pediatric patients with CNS infections because of the risk of seizures, or in pediatric patients less than 30 kg with impaired renal function as no data are available.

Cilastatin + Imipenem and Geriatic

Information Not Available

Cilastatin + Imipenem and Other Contraindications

Hypersensitivity

Storage

Store unreconstituted powder at or below 77°F.

Lab interference

Store unreconstituted powder at or below 77°F.

© 2011-2020 DrugsUpdate.com. Disclaimer | Site Map

Feedback
  • Companies that own platforms will own the market
  • Trusted and recognized by all Doctors
  • Access to Millions of Visitors instantly.
  • Companies that own platforms will own the market
  • Trusted and recognized by all Doctors
  • Access to Millions of Visitors instantly.