Imipenem + Cilastatin: An Effective Duo in Fighting Infections

1. Origin

• Imipenem and cilastatin are completely synthesized.

2. Antibiotic Class

• Imipenem belongs to the carbapenem group, a class of beta-lactam antibiotics.

3. Mechanism of Action

• Imipenem: Inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs) in bacteria, similar to other penicillin antibiotics.

4. Physical Form

• Imipenem is a white crystalline powder.

5. Solubility

• Imipenem is poorly soluble in water.

6. Physical Properties

• Imipenem has a UV absorption spectrum, an IR absorption spectrum, and optical rotation.

7. Quantification Methods

• Imipenem can be quantified using high-performance liquid chromatography (HPLC), UV spectrophotometry, or microbiological methods.

8. Spectrum of Activity

• Imipenem has a broad spectrum of activity, including gram-positive, gram-negative, aerobic, anaerobic bacteria, group B beta-hemolytic streptococci, Listeria, and it is potent against multidrug-resistant bacteria.

9. Stability in Beta-Lactamase

• Imipenem is highly stable in beta-lactamase, an enzyme that can degrade beta-lactam antibiotics.

10. Absorption

• Imipenem is not absorbed orally, so it is administered only intravenously or intramuscularly.

11. Cilastatin

• Cilastatin is a dehydropeptidase inhibitor, an enzyme that can break down imipenem in the renal tubules. Cilastatin prevents this breakdown, helping to maintain sufficiently high imipenem blood levels for therapeutic efficacy.

12. Distribution

• Imipenem is widely distributed throughout the body, including the placenta and breast milk.

13. Metabolism

• Imipenem is mainly metabolized in the kidneys.

14. Indications

• Imipenem + cilastatin is indicated for the treatment of severe infections when other antibiotics are ineffective. However, imipenem is not the first-line antibiotic due to its broad spectrum of activity.

15. Antibiotic Combinations

• Imipenem + cilastatin should not be combined with other antibiotics.

16. Major Side Effects

• Nephrotoxicity: Imipenem can cause nephrotoxicity, especially in patients with renal insufficiency.
• Neurotoxicity: Imipenem can cause seizures.
• Allergic reactions: Allergic reactions such as rash, itching, facial swelling, and difficulty breathing may occur.

17. Drug Interactions

• Probenecid: Probenecid decreases the blood levels of imipenem and cilastatin.

18. Configuration

• Imipenem has a 5R-6S configuration, which is different from most other penicillin antibiotics (which have a 6R configuration).

19. Beta-Lactamase Inhibitors

• Beta-lactamase inhibitors have a general structure of X-SO2, where X is O (as in clavulanate) or SO2 (as in sulbactam and tazobactam), instead of S as in penicillin.

20. Antibacterial Activity of Beta-Lactamase Inhibitors

• Beta-lactamase inhibitors have weak antibacterial activity, mainly supporting the protection of some antibiotics that are not stable in beta-lactamase, such as penicillin A and penicillin that acts on multidrug-resistant bacteria.

Note:

• The use of imipenem + cilastatin should be monitored by a qualified physician.
• Dosage and administration should be adjusted for each individual case.
• Inform your doctor about underlying medical conditions, medications currently being used, and allergic reactions before using imipenem + cilastatin.

Conclusion:

Imipenem + cilastatin is an effective duo in the treatment of severe infections, especially when other antibiotics are ineffective. However, it is necessary to be aware of the side effects and drug interactions to ensure safety for the user.