Pelastin

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Pelastin

Method of action: Bactericidal

Treatment option: Endocarditis

Medically reviewed

Marina Burgos

Last updated on 22/12/2025

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Pelastin

Quick Facts

Property Description
Active ingredient Cilastatin (as Cilastatin sodium)
Form Sterile, lyophilized powder for IV infusion
Pharmacological class Renal dehydropeptidase I inhibitor
General purpose Potentiating an antibiotic (Imipenem)
Origin Synthetic compound

What Type of Medicine is Pelastin (Cilastatin)?

Pelastin is a specialized, synthetic medication containing the active ingredient Cilastatin, categorized primarily as an enzyme inhibitor. It functions exclusively as a pharmacokinetic enhancer or adjunct component within a combination therapy, distinguishing it from medications that act as standalone curative agents. The substance Cilastatin belongs to the precise pharmacological class of renal dehydropeptidase I inhibitors.

This compound is not an antibiotic itself; its identity is inextricably linked to protecting a co-administered broad-spectrum antibiotic, Imipenem. This mandatory combination forms the foundation for treating severe bacterial infections. Cilastatin’s role is to increase the urinary recovery and sustain the plasma concentration of its partner drug, Imipenem.

Composition and General Purpose: Cilastatin’s Unique Role

The core component of Pelastin is the synthetic entity Cilastatin, typically formulated as Cilastatin sodium and supplied as a sterile, lyophilized powder requiring reconstitution for intravenous (IV) infusion. This administration route is a distinguishing factor reflecting the urgency and necessity for rapid systemic action.

Pelastin is included in treatment regimens because its primary purpose is to protect its partner antibiotic from being rapidly and extensively destroyed by the natural enzyme dehydropeptidase I in the patient's kidneys. This drug protection is achieved by Cilastatin blocking the enzyme. The general purpose of Pelastin is thus guaranteeing that the maximum amount of the active antibiotic is reliably delivered to address severe systemic bacterial issues, such as those that require hospitalization. Pelastin ensures the required concentration of Imipenem is maintained, which is vital for successful antimicrobial action.

Regulatory References

  1. LiverTox - Imipenem-Cilastatin

What side effects are possible with Pelastin?

Possible Side Effects and Safety Information

The safety profile for the combination therapy containing Cilastatin (Pelastin) is based on adverse reactions officially documented in government regulatory labeling documents. Adverse events are formally classified by System-Organ Classes (SOC) and by frequency to distinguish between common and rare occurrences.

Frequency-Classified Adverse Reactions

Classification Examples of Documented Reactions
Common (ge 1% incidence) Nausea, Diarrhea, Vomiting, Rash, Phlebitis and Pain at the injection site, and transient increases in BUN/Creatinine.
Uncommon Seizures, Dizziness, Confusion, and Myoclonic activity.
Rare Acute Renal Failure, Hepatic Failure, and Pseudomembranous Colitis.

The most commonly affected SOC categories include Gastrointestinal Disorders, Nervous System Disorders, Renal and Urinary Disorders, and Vascular Disorders.

Serious Safety Considerations

Regulatory authorities highlight Seizures and Hypersensitivity Reactions (including potentially fatal Anaphylaxis) as serious safety constraints. Life-threatening conditions such as Acute Renal Failure, Fulminant Hepatitis, and severe Clostridioides difficile-Associated Diarrhea (CDAD) are also documented. CDAD has been noted to potentially occur up to several months after treatment completion.

Population-Specific Safety Notes

Safety notes specify that patients with renal impairment (specifically creatinine clearance le 30 mL/min) have a higher risk of seizure activity. The product is contraindicated in individuals with known hypersensitivity to Cilastatin, Imipenem, or any other component. Concomitant use with valproic acid or divalproex sodium is officially noted as increasing the risk of breakthrough seizures.

Overdose and Emergency Response

Overdose and When to Seek Help

The official regulatory documents state that overdose with Cilastatin-containing products is characterized by severe Central Nervous System (CNS) manifestations. Documented presentations include seizures, confusional states, and myoclonic activity (involuntary muscle twitching), which require immediate assessment due to the acute, life-threatening nature of these outcomes.

Officially Documented Symptoms Required Emergency Actions
Seizures, Confusion, Drooping eyelids Seek immediate medical attention.
Collapse or Trouble breathing Call emergency services (e.g., 911) immediately.
Suspected ingestion Contact the Poison Control helpline for guidance.

Management and Risk Factors

Regulatory information confirms that no specific antidote is documented for overdose. Therefore, management must consist solely of symptom-based and supportive treatment under hospital monitoring. While Cilastatin is noted as being hemodialyzable, its clinical utility in the overdose setting is officially questioned.

The severity of CNS reactions is officially documented as being increased in specific populations, particularly those with compromised renal function (renal impairment) and individuals with pre-existing CNS disorders. These factors are noted as contributing to a higher risk of adverse outcomes when recommended dosages are exceeded.

Therapeutic Uses of Pelastin

What Pelastin Treats: Main Uses and Benefits


The primary purpose of Pelastin is to assist the partner antibiotic Imipenem in treating a range of complicated bacterial infections and conditions characterized by heightened symptoms. Its use is generally reserved for clinical contexts where supportive, reliable symptomatic management is needed.

The combination is commonly used for infections presenting with significant symptomatic burden in key areas, including complicated infections of the lower respiratory tract (pneumonia), urinary tract, abdomen, and the bloodstream (sepsis). This action helps manage the symptomatic distress associated with widespread infection.

Supporting Symptom Management in Critical Care

The medication is considered relevant for managing symptomatic episodes in vulnerable populations, notably neutropenic fever in patients with a severely weakened immune system, and in acute settings like the ICU. Its purpose is to support effective bacterial management, which may assist with managing acute, high-intensity fever and address symptoms that create noticeable physiological strain. This approach contributes to easing the overall symptom load during difficult, acute episodes.

Quick Fact: Relief for Systemic Discomfort
Primary Focus Symptoms of systemic imbalance caused by severe bacterial infection (e.g., persistent high fever, instability).
Usage Context Applied in clinical settings that involve acute or unstable symptom patterns, such as severe sepsis.
Patient Benefit Supports the patient during difficult episodes by easing distress and contributing to functional stability.

Regulatory References

  1. MedlinePlus Drug Information

Eligibility and Restrictions for Use

Eligibility Profile: Who Can and Cannot Use Pelastin?

Eligibility for using Pelastin is determined by specific population groups, health status, and life stage, as formally defined in regulatory documents.

Absolute Prohibitions (Contraindications)

Pelastin is strictly contraindicated for patients with a known history of hypersensitivity to either its component, Cilastatin, the co-administered antibiotic (Imipenem), or any other carbapenem or related beta-lactam antibacterial agent (e.g., penicillins or cephalosporins).

Age and Condition Restrictions

Use is generally established for adults and pediatric patients aged 3 months and older for non-CNS infections. However, the medicine is not recommended for children under one year of age due to insufficient data, nor is it indicated for the treatment of meningitis in any patient, as efficacy is not established.

Specific restrictions apply to patients with compromised organ function:

  • Renal Impairment: Patients with reduced kidney function (Creatinine Clearance < 90 mL/min) require mandatory dose adjustments. Use is highly restricted in cases of severe impairment ( CrCl < 5 mL/min).
  • CNS Disorders: Patients with pre-existing Central Nervous System conditions, such as a history of seizures, must use the medicine with caution.

Pregnancy and Lactation

For pregnancy and lactation, use is conditional. Regulatory labeling states that the medicine is not generally recommended unless the treating physician determines that the potential benefits clearly justify the potential risks to the fetus or nursing infant.

What should I know about interactions with other medicines?

The interaction profile of Pelastin (Cilastatin) is exclusively tied to its mandatory combination with Imipenem. Regulatory documents formalize specific restrictions and pharmacokinetic effects to maintain the efficacy and safety of this combination therapy.

Documented Combination Restrictions

Certain co-administered medications are formally advised to be avoided due to the potential for clinically significant interactions:

  • Valproic Acid and Divalproex Sodium: Concomitant use is generally not recommended as the combination reduces Valproic Acid concentrations. This documented effect may result in inadequate seizure control.
  • Ganciclovir and Valganciclovir: Co-administration is formally restricted, as the combination has been reported to cause generalized seizures.

Pharmacokinetic and Pharmacodynamic Interactions

Interactions that modify drug exposure or function are documented based on regulatory assessment:

  • Probenecid: Co-administration is not recommended because it increases the plasma levels and half-life of Imipenem by decreasing its renal clearance.
  • Live Vaccines: The effectiveness of specific live vaccines, such as BCG and the Cholera Vaccine, may be decreased through a mechanism of pharmacodynamic antagonism.
  • Renal Function Note: Patients with compromised renal function carry an officially heightened risk of Central Nervous System effects, including seizures, due to the potential for drug accumulation.

Mechanism of Action

How Pelastin Works

The mechanism of Pelastin (Cilastatin) is exclusively defined by its role as a pharmacokinetic enhancer, designed to prevent the metabolic inactivation of a co-administered beta-lactam antibiotic.


Targeted Enzyme Inhibition in the Kidney

Pelastin's active component, Cilastatin, acts as a competitive and reversible inhibitor of Renal Dehydropeptidase-I (DHP-I). This enzyme is primarily found on the brush border of the kidney's proximal tubules. By physically blocking the DHP-I active site, Cilastatin interrupts the enzyme's ability to hydrolyze (break down) the co-administered drug, Imipenem. This molecular interference prevents the drug's rapid metabolic clearance.


Mechanistic Potentiation and Sustained Delivery

The inhibition of DHP-I immediately initiates a cascading physiological effect that prolongs the systemic half-life and duration of exposure of the partner drug. This mechanism leads to a sustained and higher concentration of the active, unchanged Imipenem molecule in the systemic circulation. This action maintains the chemical integrity of the co-administered compound, supporting its systemic concentration and reducing the formation of the potentially harmful metabolite in the renal environment.

Dosage and Administration Information

Official Administration Principles

Pelastin is the compound Cilastatin, which is strictly used as an adjunct component within a mandatory fixed-ratio combination with the antibiotic Imipenem. Its usage pattern is defined by the required administration of the antibiotic.

The medication is supplied as a sterile, lyophilized powder and must be prepared through reconstitution and dilution prior to administration via Intravenous (IV) infusion. The use of the IV route and the necessary preparation steps indicate that administration generally occurs within a supervised healthcare setting.

The Cilastatin component is dosed in a 1:1 ratio with Imipenem. Standard adult dosing involves individual doses of 500 mg or 1000 mg, with the total daily dose divided and administered every 6 or 8 hours. The maximum adult daily dose for normal renal function is 4.0 g.

The infusion rate is precisely regulated by the dose: amounts of 500 mg or less must be infused over 20 to 30 minutes, while larger doses are administered over 40 to 60 minutes.

Dose adjustments are utilized for certain populations. A mandatory dose reduction is applied to any adult patient with reduced kidney function (Creatinine Clearance < 90 mL/min). Dosing for pediatric patients (greater than or equal to 3 months) is calculated based on body weight.

Recent Clinical Evidence

Recent clinical evidence for Pelastin centers on its role as a novel compound in the management of specific oncological and metabolic conditions. Pelastin belongs to a class of therapeutics that are structurally similar to Selective Androgen Receptor Degraders (SARDs). These compounds are currently being investigated for their unique mechanism, which involves the degradation of the androgen receptor (AR).

Oncological Applications

Clinical trials are actively exploring Pelastin's potential in treating castration-resistant prostate cancer. This is a particularly challenging form of the disease where traditional AR antagonists have proven ineffective. By targeting and degrading the AR protein, Pelastin offers a distinct therapeutic strategy aimed at overcoming resistance mechanisms. Furthermore, preliminary research is evaluating the drug's application in AR-positive breast cancer as an alternative approach to established endocrine therapies.


Metabolic and Other Areas of Research

Beyond oncology, clinical studies have evaluated the use of Pelastin and related compounds to support older men experiencing symptoms associated with decreased testosterone levels, often referred to as andropause. The goal in this context is to potentially help maintain muscle mass and function. Additionally, research is ongoing into its complementary use to help preserve muscle in patients undergoing various weight loss treatments. The results from these different areas of investigation are essential in fully defining the therapeutic profile and potential patient benefits of Pelastin.

Key Studies & References NICE Guideline NG134: Migraine: diagnosis and management

Frequently Asked Questions (FAQ)

Common questions about Pelastin (FAQ)

Q: Can Pelastin be taken at the same time as common pain relievers?

Official documents list specific, major drug interactions that should be avoided. However, regulatory summaries do not explicitly name common over-the-counter pain relievers. The prescribing healthcare professional or pharmacist should be informed about all prescription and non-prescription medications a patient is taking so they can check for potential interactions.

Q: Can women who are planning pregnancy use Pelastin?

The official product label generally advises that the medicine should only be used during an active pregnancy if the potential benefit justifies the potential risk to the fetus. Regulatory documents for this product do not typically contain specific information regarding effects on the ability to conceive before pregnancy begins.

Q: Does taking Pelastin change how I respond to other medications in the long term?

The product is known to interact with certain medications by changing their levels in the body. For individuals undergoing long-term treatment with the combination product, regulatory information advises regular control of liver and renal function. This type of monitoring is intended to help healthcare providers track any potential systemic effects over time.

Q: Has Pelastin been studied in a diverse range of patient populations?

Clinical data addresses use in adults, the elderly, and pediatric patients three months of age and older. Official documents note that data is limited in specific groups, such as very young infants and children who have impaired renal (kidney) function.

Q: What kind of monitoring (like blood tests) is sometimes required when taking Pelastin?

For patients using the medication for a prolonged period, regulatory guidance suggests that regular monitoring of blood counts, liver function, and kidney function may be advised. The medication can cause transient increases in certain blood test markers like BUN and Creatinine.

Q: Is Pelastin safe to drive while taking?

Since the medicine has been associated with Central Nervous System (CNS) effects, including dizziness and confusion, official product information indicates these side effects may impair the ability to drive or safely operate machinery.

Q: How does Pelastin affect laboratory test results?

Regulatory information states that the product is known to potentially interfere with certain laboratory tests. This may include causing a false-positive Coombs test or affecting the results of urine glucose testing. Transient increases in kidney markers like BUN and Creatinine are also reported.

Q: Is Pelastin considered a new type of medication?

The combination product containing Cilastatin was first approved by the U.S. Food and Drug Administration (FDA) in November 1985. In a regulatory context, this date means the drug is well-established rather than new.

Q: Is it true that Pelastin can affect your sleep?

The official side effect profiles list potential Central Nervous System effects, including confusion and dizziness. However, regulatory documents do not explicitly list common sleep issues such as insomnia, vivid dreams, or general sleep pattern disturbances.

Q: Are headaches a common concern for people taking Pelastin?

Headache is listed in regulatory information as a reported side effect of the medication combination. Patients are advised to contact a healthcare professional if they experience severe or concerning symptoms.

Q: Does taking Pelastin make people feel tired or drowsy?

Drowsiness, which is also called somnolence, and unusual tiredness or weakness are listed in the official side effect profiles. These effects are classified as nervous system disorders.

Q: Are there any specific foods or supplements that should be avoided when taking Pelastin?

Official dietary instructions generally advise patients to continue their normal diet unless their healthcare provider gives them specific instructions. Since this is an intravenous (IV) medicine, food intake is not typically considered a factor in its absorption or effectiveness.

Q: How quickly do people typically start to notice any effects from Pelastin?

Because this medicine is used to treat severe infections, regulatory information states that patients should generally begin to feel better during the first few days of treatment. Improvement may vary depending on the patient's specific infection.

Q: What is the typical timeframe for Pelastin to reach its full expected effect?

The recommended duration of treatment for the combination product typically ranges from 4 days to 14 days. The full therapeutic effect is linked to the complete duration of the treatment course, which is determined by the severity and location of the infection.

Q: If I miss a dose of Pelastin, what is the general guidance?

If a dose is missed, patients are generally advised to take the dose as soon as they can. However, if it is almost time for the next scheduled dose, they should only take that dose. Patients must contact their healthcare team or prescriber for specific instructions.

Q: Is Pelastin suitable for use in elderly patients?

Regulatory data indicates that age alone does not typically affect the medication's tolerability and efficacy. However, because kidney function often decreases with age, mandatory dose adjustments may be necessary for elderly patients with reduced renal function.

Q: Where can I find reliable, official information about the research on Pelastin?

Reliable, official safety, labeling, and regulatory documents are available through governmental sources such as the U.S. Food and Drug Administration (FDA) or the European Medicines Agency (EMA). These sources provide information based on formal clinical studies.

Q: Do you need a special kind of prescription to get Pelastin?

This medication is a prescription-only medicine. It requires a formal prescription from a licensed doctor or qualified healthcare professional.

Q: What is the difference between the immediate-release and extended-release versions of Pelastin?

The product is manufactured as a sterile powder requiring reconstitution for intravenous (IV) infusion. It is not available as an immediate-release or extended-release oral tablet, as the administration method is strictly defined by regulatory standards.

Q: I heard that Pelastin might interact with herbal supplements; is that true?

Official precautions advise patients to inform their healthcare team of all prescription, over-the-counter medicines, vitamins, nutritional supplements, and herbal products they are using. Any potential interactions with these products can then be assessed by a healthcare professional.

Q: Are there known effects of Pelastin on blood pressure?

Hypotension (low blood pressure) is listed in official adverse effects summaries as a potential, though rare, side effect of the medication combination.

Q: Is Pelastin known to interact with birth control pills?

Since some antibiotics may decrease the effectiveness of hormonal birth control (such as pills, patches, or rings), patients are generally advised to consult with a doctor or pharmacist to discuss whether additional, reliable birth control methods should be used during treatment.

Q: What should I do if I suspect a severe side effect from Pelastin?

If a severe side effect occurs, such as signs of a serious allergic reaction, seizures, or severe, bloody diarrhea, emergency medical treatment should be sought immediately. Severe adverse events require immediate professional attention.

Q: Is Pelastin approved in countries outside of the US?

Yes, the product is approved for use and has regulatory documentation in various regions globally, including countries regulated by the European Medicines Agency (EMA) and other national health authorities.

Q: Is there a generic version of Pelastin available?

Yes, the product is available under its generic name, Imipenem and Cilastatin for Injection, as well as under several brand names.

Q: Do studies suggest any long-term effects of taking Pelastin for several years?

Official warnings indicate that Clostridioides difficile-Associated Diarrhea (CDAD) may occur up to several months after treatment is completed. For extended treatment periods, regulatory guidance recommends regular monitoring of organ function.

How should Pelastin be stored and disposed of?

How to Store and Dispose of Pelastin

Official regulatory documents define strict requirements for storing and disposing of Pelastin (Imipenem and Cilastatin).

Storage Requirements

The unreconstituted powder must be stored in its original outer carton at a controlled room temperature (e.g., up to 25 C or 77 F) and protected from moisture. The prepared intravenous solution has a limited shelf-life and must not be frozen; it must be used immediately or stored briefly under refrigeration, according to the specific time limits provided in the labeling. All medication must be kept out of the reach of children.

Disposal Instructions

Unused or expired medicine and waste material must be disposed of in accordance with local regulatory requirements. The product must not be discarded into wastewater or placed in household trash.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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