Cilastatin
Imipenem
Thienamycins
Cyclopropanes
Drug Combinations
Protease Inhibitors
Sulbactam
Encyclopedias as Topic
Multiple roles for IL-12 in a model of acute septic peritonitis. (1/118)
The present study addressed the role of IL-12 in a murine model of septic peritonitis, induced by cecal ligation and puncture (CLP). Although CLP surgery induced IL-12 production at 6 and 24 h after surgery, IL-12 immunoneutralization was clearly deleterious in this model: 54% of CLP mice receiving preimmune serum survived, whereas mice administered IL-12 antisera prior to CLP experienced a 25% survival rate. IL-12 immunoneutralization not only led to increased mortality, but also appeared to promote a shift away from IL-12 and IFN-gamma, in favor of IL-10. This cytokine shift corresponded to changes in bacterial load, as CLP mice receiving IL-12 antiserum yielded more CFUs from the peritoneal cavity at 24 h after CLP. To address the role of bacterial infection in IL-12 antiserum-induced mortality following CLP, antibiotics were administered for 4 days after surgery. Despite regular antibiotic administration, IL-12 immunoneutralization still reduced survival in CLP mice. Furthermore, histology of the ceca revealed that mice administered IL-12 antisera failed to show typical organization of the damaged cecum wall. Accordingly, Gram staining revealed bacteria within peritoneal fluids from these mice, while peritoneal fluids from CLP mice that received preimmune serum and antibiotics were free of bacteria. Altogether, these data suggested multiple important roles for IL-12 in the evolution of murine septic peritonitis. (+info)Effects of antibiotic therapy on Pseudomonas aeruginosa-induced lung injury in a rat model. (2/118)
The effect of antibiotics on the acute lung injury induced by virulent Pseudomonas aeruginosa PA103 was quantitatively analyzed in a rat model. Lung injury was induced by the instillation of PA103 directly into the right lower lobes of the lungs of anesthetized rats. The alveolar epithelial injury, extravascular lung water, and total plasma equivalents were measured as separate, independent parameters of acute lung injury. Four hours after the instillation of PA103, all the parameters were increased linearly depending on the dose of P. aeruginosa. Next, we examined the effects of intravenously administered antibiotics on the parameters of acute lung injury in D-galactosamine-sensitized rats. One hour after the rats received 10(7) CFU of PA103, an intravenous bolus injection of aztreonam (60 mg/kg) or imipenem-cilastatin (30 mg/kg) was administered. Despite an MIC indicating resistance, imipenem-cilastatin improved all the measurements of lung injury; in contrast, aztreonam, which had an MIC indicating sensitivity, did not improve any of the lung injury parameters. The antibiotics did not generate different quantities of plasma endotoxin; therefore, endotoxin did not appear to explain the differences in lung injury. This in vivo model is useful to quantitatively compare the efficacies of parenteral antibiotic administration on Pseudomonas airspace infections. (+info)Effects of cilastatin on the pharmacokinetics of a new carbapenem, DA-1131, in rats, rabbits, and dogs. (3/118)
DA-1131, a new carbapenem antibiotic, undergoes renal metabolism by renal dehydropeptidase I (DHP-I), located on the brush border of the proximal tubular cell. Species differences with regard to the effects of cilastatin, a renal DHP-I inhibitor, were investigated after a 1-min intravenous infusion of DA-1131, with or without cilastatin, to rats, rabbits, and dogs. After intravenous infusion, the nonrenal clearance (CL(NR)) of DA-1131 was significantly slower in rats (3.00 versus 8.01 ml/min/kg) and rabbits (2.41 versus 6.77 ml/min/kg) when the drug was coadministered with cilastatin; this could be due to the slower metabolism of DA-1131 by rat and rabbit kidney DHP-I. This indicated that renal metabolism of DA-1131 by renal DHP-I was inhibited by cilastatin. However, coadministration with cilastatin to dogs did not affect the CL(NR) of DA-1131. (+info)Modification of acquired immunity in mice by imipenem/cilastatin. (4/118)
The immunomodulating properties of antimicrobial drugs may have important implications for clinical practice, particularly for those patients whose immune system has been compromised. In this study, we assessed the influence of different treatments with a beta-lactam antibiotic (imipenem/cilastatin) on several acquired immune responses of BALB/c mice; splenocyte responses to specific mitogens and to sheep red blood cells, IL-2 production and proportions of the different lympho-monocytic populations. Impenem/cilastatin was shown to modify some lymphocyte-associated immune functions and it would be useful to investigate whether immunomodulatory effects also occur in humans. (+info)Levofloxacin in the empirical treatment of patients with suspected bacteraemia/sepsis: comparison with imipenem/cilastatin in an open, randomized trial. (5/118)
An open, randomized, multinational, multicentre study was conducted to compare the efficacy, safety and tolerability of levofloxacin 500 mg twice daily with imipenem/cilastatin 1 g iv three-times daily in the treatment of hospitalized adult patients with clinically suspected bacteraemia/ sepsis. Levofloxacin patients could change from iv to oral administration after a minimum of 48 h iv treatment if clinical signs and symptoms of sepsis had improved. The primary efficacy analysis was based on the clinical and bacteriological response at clinical endpoint. A total of 503 patients were randomized and 499 included in the intent-to-treat population. The per-protocol population comprised 287 patients with bacteriologically proven infection. Clinical cure rates at clinical endpoint in the intent-to-treat population and per-protocol population were 77% (184/239) and 89% (125/140), respectively, for levofloxacin and 68% (178/260) and 85% (125/147), respectively, for imipenem/cilastatin. At follow-up, the cure rates in the per-protocol population were 84% for levofloxacin and 69% for imipenem/cilastatin. The 95% confidence interval for both populations showed that levofloxacin was as effective as imipenem/cilastatin. A satisfactory bacteriological response was obtained in 87% (96/110) of levofloxacin patients and 84% (97/116) of imipenem/cilastatin patients at clinical endpoint. Adverse events possibly related to the study drug were reported in 74 (31%) levofloxacin patients and 79 (30%) imipenem/cilastatin patients. There were no clinically appreciable differences between the treatment groups. Levofloxacin 500 mg twice daily, either iv or as sequential iv/oral therapy, was as effective and well tolerated as imipenem/cilastatin 1 g iv three-times daily in the treatment of hospitalized patients with suspected bacteraemia/sepsis. (+info)Molecular homology and the luminal transport of Hg2+ in the renal proximal tubule. (6/118)
The aim of this study was to define mechanisms involved in the luminal uptake of inorganic mercury in the kidney using isolated perfused straight (S2) segments of the proximal tubule. When mercuric conjugates of glutathione (GSH), cysteinylglycine. or cysteine (containing 203Hg2+) were perfused through the lumen, the rates of luminal disappearance flux (JD) of inorganic mercury were approximately 39, 53, and 102 fmol/min per' min, respectively. Thus, the rates of luminal uptake of mercury are greater when the mercury is in the form of a mercuric conjugate of cysteine than in the form of a mercuric conjugate of cysteinylglycine or GSH. Addition of acivicin to the perfusate, to inhibit activity of the y-glutamyltransferase, caused significant reductions in the J,, for mercury in tubules perfused with mercuric conjugates of GSH. Addition of cilastatin, an inhibitor of dehydropeptidase- l (cysteinylglycinase) activity, caused significant reductions in the uptake of mercury in tubules perfused with mercuric conjugates of cysteinylglycine. These findings indicate that a significant amount of the luminal uptake of mercury, when mercuric conjugates of GSH are present in the lumen, is dependent on the activity of both y-glutamyltransferase and cysteinylglycinase. Finally, the JD for mercury in tubules perfused with mercuric conjugates of cysteine was reduced by approximately 50% when 3.0 mM L-lysine or 5.0 mM cycloleucine was added to the perfusate. It is concluded that these findings indicate that at least some of the luminal uptake of mercuric conjugates of cysteine occurs at the site of one or more amino acid transporters via a mechanism involving molecular homology. (+info)Acute necrotizing pancreatitis: treatment strategy according to the status of infection. (7/118)
OBJECTIVE: To determine benefits of conservative versus surgical treatment in patients with necrotizing pancreatitis. SUMMARY BACKGROUND DATA: Infection of pancreatic necrosis is the most important risk factor contributing to death in severe acute pancreatitis, and it is generally accepted that infected pancreatic necrosis should be managed surgically. In contrast, the management of sterile pancreatic necrosis accompanied by organ failure is controversial. Recent clinical experience has provided evidence that conservative management of sterile pancreatic necrosis including early antibiotic administration seems promising. METHODS: A prospective single-center trial evaluated the role of nonsurgical management including early antibiotic treatment in patients with necrotizing pancreatitis. Pancreatic infection, if confirmed by fine-needle aspiration, was considered an indication for surgery, whereas patients without signs of pancreatic infection were treated without surgery. RESULTS: Between January 1994 and June 1999, 204 consecutive patients with acute pancreatitis were recruited. Eighty-six (42%) had necrotizing disease, of whom 57 (66%) had sterile and 29 (34%) infected necrosis. Patients with infected necrosis had more organ failures and a greater extent of necrosis compared with those with sterile necrosis. When early antibiotic treatment was used in all patients with necrotizing pancreatitis (imipenem/cilastatin), the characteristics of pancreatic infection changed to predominantly gram-positive and fungal infections. Fine-needle aspiration showed a sensitivity of 96% for detecting pancreatic infection. The death rate was 1.8% (1/56) in patients with sterile necrosis managed without surgery versus 24% (7/29) in patients with infected necrosis (P <.01). Two patients whose infected necrosis could not be diagnosed in a timely fashion died while receiving nonsurgical treatment. Thus, an intent-to-treat analysis (nonsurgical vs. surgical treatment) revealed a death rate of 5% (3/58) with conservative management versus 21% (6/28) with surgery. CONCLUSIONS: These results support nonsurgical management, including early antibiotic treatment, in patients with sterile pancreatic necrosis. Patients with infected necrosis still represent a high-risk group in severe acute pancreatitis, and for them surgical treatment seems preferable. (+info)Treatment of severe nosocomial pneumonia: a prospective randomised comparison of intravenous ciprofloxacin with imipenem/cilastatin. (8/118)
BACKGROUND: A prospective multicentre study was undertaken to compare the efficacy of intravenous ciprofloxacin or imipenem in the treatment of severe nosocomial pneumonia requiring mechanical ventilation. METHODS: Patients with a clinical suspicion of pneumonia were randomised to receive either ciprofloxacin (800-1200 mg/day) or imipenem (2-4 g/day) in doses adjusted for renal function and specimens of the lower respiratory tract were taken. Patients were included in the study when specimens showed significant growth for potentially pathogenic microorganisms in quantitative bacterial cultures (n = 75, ciprofloxacin 41/75 (55%); imipenem 34/75 (45%)). The clinical and bacteriological success rates were the primary and secondary efficacy variables. An intent-to-treat analysis was performed for all randomised patients who received at least one dose of the study medication (n = 149, ciprofloxacin 72/149 (48%), imipenem 77/149 (52%)). RESULTS: The success rates were generally good, but neither the clinical success rates (ciprofloxacin, 29/41 (71%), imipenem, 27/34 (79%); 95% CI -10.8 to 28.1; p = 0.435) nor the bacteriological response rate (ciprofloxacin, 20/41 (49%), imipenem, 17/34 (50%); 95% CI -21.5 to 23.9; p = 1.0) were significantly different between the study arms. Pseudomonas aeruginosa was recovered in 26/75 patients (35%) and clinical (ciprofloxacin, 10/14 (71%), imipenem, 8/12 (67%); 95% CI -40.4 to 30.9; p = 1.0) and bacteriological response rates (ciprofloxacin, 7/14 (50%), imipenem, 3/12 (25%), 95% CI -60.9 to 10.9, p = 0.247) were not significantly different in this subgroup of patients. Resistance of Pseudomonas aeruginosa developed in 5/26 cases (19%), 1/14 (7%) to ciprofloxacin and 4/12 (33%) to imipenem (p = 0.147), and the mortality was 12/75 (16%) with no difference between treatment groups (ciprofloxacin, 8/41(24%), imipenem 4/34 (17%); p = 0.362). The clinical response was evaluable in 109/149 patients (73%) in the intent-to-treat analysis and was successful in 74/109 patients (68%). The clinical response rates were also not significantly different in the intent-to-treat analysis (ciprofloxacin, 34/52 (65%), imipenem, 40/57 (70%); 95% CI -12.8 to 22.3; p = 0.746). CONCLUSIONS: Treatment with either ciprofloxacin or imipenem was effective in a selected group of patients with microbiologically confirmed, severe nosocomial pneumonia requiring mechanical ventilation. Although no differences between the study medication could be documented in this trial, smaller differences between treatment arms may have been missed because of sample size limitations. (+info)Cilastatin is a medication that is primarily used as a stabilizer and renal protective agent for the antibiotic imipenem. Cilastatin works by inhibiting the deactivation of imipenem by renal dehydropeptidase-I, which helps maintain its therapeutic effectiveness in the body.
Imipenem/cilastatin is a combination medication used to treat various bacterial infections, including pneumonia, sepsis, and skin and urinary tract infections. Cilastatin does not have any antibacterial activity on its own.
It's important to note that the use of cilastatin should be under medical supervision, as with any medication. Always consult a healthcare professional for accurate information regarding medications and their uses.
Imipenem is an antibiotic medication that belongs to the class of carbapenems. It is used to treat various types of bacterial infections, including pneumonia, sepsis, and skin infections. Imipenem works by inhibiting the synthesis of bacterial cell walls, leading to bacterial death.
Imipenem is often combined with another medication called cilastatin, which helps to prevent the breakdown of imipenem in the body and increase its effectiveness. The combination of imipenem and cilastatin is available under the brand name Primaxin.
Like other antibiotics, imipenem should be used with caution and only when necessary, as overuse can lead to antibiotic resistance. It is important to follow the prescribing physician's instructions carefully and complete the full course of treatment, even if symptoms improve before the medication is finished.
Dipeptidases are a group of enzymes that break down dipeptides, which are composed of two amino acids joined by a peptide bond. These enzymes catalyze the hydrolysis of dipeptides into individual amino acids, helping to facilitate their absorption and utilization in the body. Dipeptidases can be found on the brush border membrane of the small intestine, as well as in various tissues and organs, such as the kidneys, liver, and pancreas. They play a crucial role in protein metabolism and maintaining amino acid homeostasis within the body.
Thienamycins are a group of antibiotics that are characterized by their beta-lactam structure. They belong to the class of carbapenems and are known for their broad-spectrum antibacterial activity against both gram-positive and gram-negative bacteria, including many that are resistant to other antibiotics. Thienamycins inhibit bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs), which leads to bacterial cell death.
Thienamycin itself is not used clinically due to its instability, but several semi-synthetic derivatives of thienamycin have been developed and are used in the treatment of serious infections caused by multidrug-resistant bacteria. Examples of thienamycin derivatives include imipenem, meropenem, and ertapenem. These antibiotics are often reserved for the treatment of severe infections that are unresponsive to other antibiotics due to their potential to select for resistant bacteria and their high cost.
Cyclopropanes are a class of organic compounds that contain a cyclic structure consisting of three carbon atoms joined by single bonds, forming a three-membered ring. The strain in the cyclopropane ring is due to the fact that the ideal tetrahedral angle at each carbon atom (109.5 degrees) cannot be achieved in a three-membered ring, leading to significant angular strain.
Cyclopropanes are important in organic chemistry because of their unique reactivity and synthetic utility. They can undergo various reactions, such as ring-opening reactions, that allow for the formation of new carbon-carbon bonds and the synthesis of complex molecules. Cyclopropanes have also been used as anesthetics, although their use in this application has declined due to safety concerns.
A drug combination refers to the use of two or more drugs in combination for the treatment of a single medical condition or disease. The rationale behind using drug combinations is to achieve a therapeutic effect that is superior to that obtained with any single agent alone, through various mechanisms such as:
* Complementary modes of action: When different drugs target different aspects of the disease process, their combined effects may be greater than either drug used alone.
* Synergistic interactions: In some cases, the combination of two or more drugs can result in a greater-than-additive effect, where the total response is greater than the sum of the individual responses to each drug.
* Antagonism of adverse effects: Sometimes, the use of one drug can mitigate the side effects of another, allowing for higher doses or longer durations of therapy.
Examples of drug combinations include:
* Highly active antiretroviral therapy (HAART) for HIV infection, which typically involves a combination of three or more antiretroviral drugs to suppress viral replication and prevent the development of drug resistance.
* Chemotherapy regimens for cancer treatment, where combinations of cytotoxic agents are used to target different stages of the cell cycle and increase the likelihood of tumor cell death.
* Fixed-dose combination products, such as those used in the treatment of hypertension or type 2 diabetes, which combine two or more active ingredients into a single formulation for ease of administration and improved adherence to therapy.
However, it's important to note that drug combinations can also increase the risk of adverse effects, drug-drug interactions, and medication errors. Therefore, careful consideration should be given to the selection of appropriate drugs, dosing regimens, and monitoring parameters when using drug combinations in clinical practice.
Protease inhibitors are a class of antiviral drugs that are used to treat infections caused by retroviruses, such as the human immunodeficiency virus (HIV), which is responsible for causing AIDS. These drugs work by blocking the activity of protease enzymes, which are necessary for the replication and multiplication of the virus within infected cells.
Protease enzymes play a crucial role in the life cycle of retroviruses by cleaving viral polyproteins into functional units that are required for the assembly of new viral particles. By inhibiting the activity of these enzymes, protease inhibitors prevent the virus from replicating and spreading to other cells, thereby slowing down the progression of the infection.
Protease inhibitors are often used in combination with other antiretroviral drugs as part of highly active antiretroviral therapy (HAART) for the treatment of HIV/AIDS. Common examples of protease inhibitors include saquinavir, ritonavir, indinavir, and atazanavir. While these drugs have been successful in improving the outcomes of people living with HIV/AIDS, they can also cause side effects such as nausea, diarrhea, headaches, and lipodystrophy (changes in body fat distribution).
Sulbactam is not a medication itself, but it's a type of β-lactamase inhibitor. It's often combined with other antibiotics such as ampicillin or cefoperazone to increase their effectiveness against bacteria that produce β-lactamases, enzymes that can inactivate certain types of antibiotics (like penicillins and cephalosporins). By inhibiting these enzymes, sulbactam helps to protect the antibiotic from being deactivated, allowing it to maintain its activity against bacteria.
The combination of sulbactam with other antibiotics is used to treat various infections caused by susceptible bacteria, including skin and soft tissue infections, respiratory tract infections, urinary tract infections, and intra-abdominal infections. It's important to note that the specific medical definition of sulbactam would be a β-lactamase inhibitor used in combination with other antibiotics for treating bacterial infections.
An encyclopedia is a comprehensive reference work containing articles on various topics, usually arranged in alphabetical order. In the context of medicine, a medical encyclopedia is a collection of articles that provide information about a wide range of medical topics, including diseases and conditions, treatments, tests, procedures, and anatomy and physiology. Medical encyclopedias may be published in print or electronic formats and are often used as a starting point for researching medical topics. They can provide reliable and accurate information on medical subjects, making them useful resources for healthcare professionals, students, and patients alike. Some well-known examples of medical encyclopedias include the Merck Manual and the Stedman's Medical Dictionary.
Anti-bacterial agents, also known as antibiotics, are a type of medication used to treat infections caused by bacteria. These agents work by either killing the bacteria or inhibiting their growth and reproduction. There are several different classes of anti-bacterial agents, including penicillins, cephalosporins, fluoroquinolones, macrolides, and tetracyclines, among others. Each class of antibiotic has a specific mechanism of action and is used to treat certain types of bacterial infections. It's important to note that anti-bacterial agents are not effective against viral infections, such as the common cold or flu. Misuse and overuse of antibiotics can lead to antibiotic resistance, which is a significant global health concern.
Cilastatin - Wikipedia
Cilastatin - Janusinfo.se
DailyMed - RECARBRIO- imipenem anhydrous, cilastatin, and relebactam anhydrous injection, powder, for solution
Cilastatin/Imipenem/Relebactam Injection 500 mg/500 mg/250 mg | Cigna
Primaxin (imipenem/cilastatin) dosing, indications, interactions, adverse effects, and more
Cilastatin 500 mg
Imipenem/cilastatin/relebactam (Recarbrio) | Davis's Drug Guide
Zienam : Imipenem and Cilastatin 500mg injection - Anticancercure.com
Online sale of Tienam ampoules for IV 0.5 g (Primaxin, Imipenem/Cilastatin)
imipenem-cilastatin intravenous Reviews and User Ratings: Effectiveness, Ease of Use, and Satisfaction
Injectable Products - Amoxicillin Potassium Clavulanate Wholesale Trader from Mumbai
The implication of Mycobacterium tuberculosis-mediated metabolism of targeted xenobiotics | Nature Reviews Chemistry
Cost-effectiveness of imipenem/cilastatin/relebactam for hospital-acquired and ventilator-associated bacterial pneumonia:...
Sepsis (Blood Poisoning): Septicemia, Causes, Treatment, 3 Stages & Risks
Treatment of childhood tb | PPT
Acyclovir Monograph for Professionals - Drugs.com
Imipenem/cilastatin sodium (IPM/CS) as an embolic agent for transcatheter arterial embolisation: a preliminary clinical study...
Treatment of Nursing Home-Acquired Pneumonia | AAFP
Auro-Valganciclovir - Uses, Side Effects, Interactions - MedBroadcast.com
Mara Dinsmoor, MD, MPH | NorthShore