Imipenem / Cilastatin

Brand Names of Imipenem / Cilastatin  in Kenya

Bacqure®, Sun Pharmaceutical Industries Limited

Cilapen®, Apoorv Nutra- Pharm Pvt. Ltd.

Cispenam®, Incepta Pharmaceutical Ltd

Imbac, Popular Pharmaceuticals Ltd.

Imicil®, Swiss Parenterals (Pvt.) Ltd

Inno-Cila®, Innocia Lifesciences Pvt. Ltd.

Kinem®, Akorn

Lastinem®, Venus Remedies Limited

Mitin® , Laso Healthcare Pvt. Ltd.

Pantin®, M.J. Biopharm Pvt. Limited

Pelastin®, PT Sanbe Farma

Tienam®,MSD (Pty) Ltd


Imipenem / Cilastatin in Kenya
Imipenem / Cilastatin Chemical Structure

Mechanism of Action

Imipenem and Cilastatin for Injection (I.V.) is a combination of imipenem and cilastatin. The bactericidal activity of imipenem results from the inhibition of cell wall synthesis. Its greatest affinity is for penicillin binding proteins (PBPs) 1A, 1B, 2, 4, 5 and 6 of Escherichia coli, and 1A, 1B, 2, 4 and 5 of Pseudomonas aeruginosa. The lethal effect is related to binding to PBP 2 and PBP 1B.

Imipenem has a high degree of stability in the presence of beta-lactamases, both penicillinases and cephalosporinases produced by Gram-negative and Gram-positive bacteria. It is a potent inhibitor of beta-lactamases from certain Gram-negative bacteria which are inherently resistant to most beta-lactam antibacterials, e.g., Pseudomonas aeruginosa, Serratia spp., and Enterobacter spp.

Cilastatin sodium is a renal dehydropeptidase inhibitor that limits the renal metabolism of imipenem.

INDICATIONS

Imipenem and Cilastatin for Injection, USP for intravenous use is a combination of imipenem, a penem antibacterial, and cilastatin, a renal dehydropeptidase inhibitor, indicated for the treatment of the following serious infections caused by designated susceptible bacteria:

  • Lower respiratory tract infections.
  • Urinary tract infections.
  • Intra-abdominal infections.
  • Gynecologic infections.
  • Bacterial septicemia.
  • Bone and joint infections.
  • Skin and skin structure infections.
  • Endocarditis.

DOSAGE AND ADMINISTRATION

The dosage of Imipenem and Cilastatin for Injection (I.V.) in adult patients should be based on suspected or confirmed pathogen susceptibility .

  • For adult patients with normal renal function (creatinine clearance of greater than or equal to 90 mL/min), the recommended dosage regimens are: 500 mg every 6 hours OR 1,000 mg every 8 hours OR 1,000 mg every 6 hours .
  • A reduction in dose must be made for a patient with a creatinine clearance of less than 90 mL/min .
  • Patients with creatinine clearances of less than 15 mL/min should not receive Imipenem and Cilastatin for Injection (I.V.) unless hemodialysis is instituted within 48 hours .
  • Reconstitute Imipenem and Cilastatin for Injection, USP (I.V.) vial with appropriate diluent and dilute the reconstituted suspension with an appropriate infusion solution before administering by intravenous infusion

CONTRAINDICATIONS

  • Known hypersensitivity to any component of Imipenem and Cilastatin for Injection (I.V.)

WARNINGS AND PRECAUTIONS

Hypersensitivity Reactions: Serious and occasionally fatal hypersensitivity (anaphylactic) reactions have been reported in patients receiving therapy with beta-lactams. If an allergic reaction to Imipenem and Cilastatin for Injection (I.V.) occurs, discontinue the drug immediately.
Seizure Potential: Seizures and other CNS adverse reactions, such as confusional states and myoclonic activity, have been reported during treatment with Imipenem and Cilastatin for Injection (I.V.). If focal tremors, myoclonus, or seizures occur, patients should be evaluated neurologically, placed on anticonvulsant therapy if not already instituted, and the dosage of Imipenem and Cilastatin for Injection (I.V.) re-examined to determine whether it should be decreased or the antibacterial drug discontinued .
Increased Seizure Potential Due to Interaction with Valproic Acid:
Co-administration of Imipenem and Cilastatin for Injection (I.V.), to patients receiving valproic acid or divalproex sodium results in a reduction in valproic acid concentrations. The valproic acid concentrations may drop below the therapeutic range as a result of this interaction, therefore increasing the risk of breakthrough seizures. The concomitant use of Imipenem and Cilastatin for Injection (I.V.) and valproic acid/divalproex sodium is generally not recommended
Clostridium difficile-Associated Diarrhea (CDAD): has been reported with use of Imipenem and Cilastatin for Injection (I.V.) and may range in severity from mild diarrhea to fatal colitis. Evaluate if diarrhea occurs

DRUG INTERACTIONS

Ganciclovir: Generalized seizures have been reported in patients who received ganciclovir. Do not co-administer unless benefit outweighs risk
Probenecid: Concomitant administration of Imipenem and Cilastatin for Injection (I.V.) and probenecid results in increases in the plasma level and half-life of imipenem. Concomitant administration is not recommended .
Valproic acid/divalproex sodium: Concomitant use with Imipenem and Cilastatin for Injection (I.V.) is generally not recommended. Consider other antibacterial drugs to treat infections in patients whose seizures are well-controlled on valproic acid or divalproex sodium

USE IN SPECIFIC POPULATIONS

Renal Impairment: Dosage adjustment is necessary in patients with renal impairment .
Adult patients with creatinine clearances of less than or equal to 30 mL/min, whether or not undergoing hemodialysis, had a higher risk of seizure activity than those without impairment of renal function .
Therefore, close adherence to the dosing guidelines and regular monitoring of creatinine clearance for these patients is recommended

ADVERSE REACTIONS

The most frequently occurring adverse reactions (≥ 0.2%) in adults were phlebitis, nausea, diarrhea, vomiting, rash, pain injection site, fever, hypotension, seizures, erythema at injection site, dizziness, pruritus, vein induration, urticaria, somnolence .
The most frequently occurring adverse reactions (> 1%) in pediatric patients greater than or equal to 3 months of age were diarrhea, rash, phlebitis, gastroenteritis, vomiting, IV site irritation, urine discoloration .
The most frequently occurring adverse reactions (> 1%) in neonates to 3 months of age were convulsions, diarrhea, oliguria/anuria, oral candidiasis, rash, tachycardia

Reporting of suspected adverse reactions:

The PPB Department of Pharmacovigilance was set up with a vision to develop, implement and continuously upgrade an appropriate system for detecting, reporting, and monitoring adverse drug reactions (ADRs) and other relevant problems with medicines in Kenya. The department strives to ensure the safety and efficacy of pharmaceutical products in Kenya.
Reporting suspected adverse reactions after authorization of the medicinal product are important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals/ Patients are encouraged to report any suspected adverse reactions via Pharmacovigilance Yellow Form, pv@pharmacyboardkenya.org or clicking below button:


Imipenem / Cilastatin in Kenya
Imipenem / Cilastatin in Kenya
Imipenem / Cilastatin in Kenya
Imipenem / Cilastatin in Kenya
Imipenem / Cilastatin in Kenya
Imipenem / Cilastatin in Kenya

Clinical | Pharmacokinetic data


Pregnancy Category: US: C (Risk not ruled out)
Routes of Administration: I.V, I. M
Bioavailability: ℞-only
Protein Binding: Not Available
Metabolosim: Not Available
Onset of Action: Not Available
Elimination Half life: Not Available
Excretion: Not Available

Legal Status | Dosage forms & Strengths


Prescription Category:
℞-only
Narcotic Drugs and Psychotropic Substances (Control ) Act Schedule:
This drug is not a controlled substance under Narcotic Drugs and Psychotropic Substances (Control ) Act
Dosage Forms | Strengths:


Drug Indentifiers:

CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)


Drug Images

References/ Citation:




What was the patient being treated for
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