Imipenem

imipenem + cilastatin

Class : ( Other Beta-lactams )

imipenem + cilastatin

P - Caution when used during pregnancy

L - Caution when used during lactation

related imipenem + cilastatin information

Indication & Dosage

Intravenous

Susceptible infections

Adult: In terms of imipenem, 1-2 g daily in divided doses every 6-8 hr, 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 mth and <40 kg: 15-25 mg/kg every 6 hr by IV infusion. Up to 90 mg/kg may be given to older children with cystic fibrosis. Neonates and infants <3 mth: 4 wk-3 mth, 25 mg/kg every 6 hr; 1-4 wk, 25 mg/kg every 8 hr; up to 1 wk, 25 mg/kg every 12 hr.

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 hr

21-30

500 mg every 8-12 hr

6-20

250 mg or 3.5 mg/kg (whichever is lower) every 12 hr

=5

Only give if haemodialysis started within 48 hr

Intravenous

Prophylaxis of surgical infections

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

Intramuscular

Mild to moderate susceptible infections

Adult: In terms of imipenem, 500 mg or 750 mg every 12 hr.

Intramuscular

Uncomplicated gonorrhoea

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

Contraindications

Hypersensitivity.

Special Precautions

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

Adverse Drug Reactions

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 inj site.

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

Drug Interactions

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

Pregnancy Category (US FDA)

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.

Mechanism of Action

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 ß-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 hr (imipenem after IM admin).

Other Beta-lactams

*imipenem + cilastatin information:

Note that there are some more drugs interacting with imipenem + cilastatin

imipenem + cilastatin

imipenem + cilastatin brands available in India

Always prescribe with Generic Name : imipenem + cilastatin, formulation, and dose (along with brand name if required)

Brands : CILANEM vial CILASPENE vial CIMISPECT vial IME-CILA 1V-vial IME-CILA IV-vial IMELASTIN vial IMINEM vial IMITOP vial I-NEM vial LASTINEM vial ZIENAM vial