Pharmaceutical, Pharmacokinetic and Other Considerations for Intravenous to Oral Stepdown Therapy

Jewesson, Peter J.

doi:10.1155/1995/975209

Cited by 12 publications

(4 citation statements)

References 4 publications

(4 reference statements)

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“…For patients with severe infections who are able to tolerate oral therapy and in whom clinical improvement has been documented, the goal should be to streamline therapy to the oral route as soon as possible. There is evidence to suggest that this approach positively impacts length of stay as well (42).…”

Section: Intravenous Versus Oral Therapy Step-down Options and Additional Carementioning

confidence: 99%

See 1 more Smart Citation

Bacterial Skin and Soft Tissue Infections in Adults: A Review of Their Epidemiology, Pathogenesis, Diagnosis, Treatment and Site Of Care

Rotstein²

2007

Canadian Journal of Infectious Diseases and Medical Microbiolog

413

327

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Skin and soft tissue infections (SSTIs) involve microbial invasion of the skin and underlying soft tissues. They have variable presentations, etiologies and severities. The challenge of SSTIs is to efficiently differentiate those cases that require immediate attention and intervention, whether medical or surgical, from those that are less severe. Approximately 7% to 10% of hospitalized patients are affected by SSTIs, and they are very common in the emergency care setting. The skin has an extremely diverse ecology of organisms that may produce infection. The clinical manifestations of SSTIs are the culmination of a two-step process involving invasion and the interaction of bacteria with host defences. The cardinal signs of SSTIs involve the features of inflammatory response, with other manifestations such as fever, rapid progression of lesions and bullae. The diagnosis of SSTIs is difficult because they may commonly masquerade as other clinical syndromes. To improve the management of SSTIs, the development of a severity stratification approach to determine site of care and appropriate empirical treatment is advantageous. The selection of antimicrobial therapy is predicated on knowledge of the potential pathogens, the instrument of entry, disease severity and clinical complications. For uncomplicated mild to moderate infections, the oral route suffices, whereas for complicated severe infections, intravenous administration of antibiotics is warranted. Recognition of the potential for resistant pathogens causing SSTIs can assist in guiding appropriate selection of antibiotic therapy.

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Section: Intravenous Versus Oral Therapy Step-down Options and Additional Carementioning

confidence: 99%

“…In choosing an appropriate step-down oral antibiotic, there are three options (42). First, one may choose the same active antibiotic in oral form with high bioavailability.…”

Section: Intravenous Versus Oral Therapy Step-down Options and Additional Carementioning

confidence: 99%

Bacterial Skin and Soft Tissue Infections in Adults: A Review of Their Epidemiology, Pathogenesis, Diagnosis, Treatment and Site Of Care

Rotstein²

2007

Canadian Journal of Infectious Diseases and Medical Microbiolog

413

327

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“…For example, they selected cefazoline every 12 h with probenecid (Benemid, Merck Sharpe & Dohme Canada, Kirkland, Quebec) (11), use of once daily aminosides (12), the use of clindamycin (Dalacin C, Pharmacia & Upjohn Inc, Mississauga, Ontario) 1200 mg every 12 h (13) if minimum inhibitory concentrations of isolate bacteria were low. As another example, intravenous use of ciprofloxacin (Cipro, Bayer Inc, Toronto, Ontario) and metronidazol were restricted because of good bioavilability (more than 80%) (14). Infectious disease specialists prepared a routine set of blood tests for toxicity surveillance and recommended drug dosages for each order of intravenous antibiotics (15).…”

Section: Program Descriptionmentioning

confidence: 99%

Ambulatory Intravenous Antibiotic Therapy in Quebec: The Hôpital Charles LeMoyne Experience in 1996

Delorme

Frenette

Corre

et al. 2000

Canadian Journal of Infectious Diseases and Medical Microbiolog

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From January 1, 1996 to December 31, 1996, 343 patients received outpatient intravenous antibiotic therapy at Charles LeMoyne Hospital, a 436-bed, acute care hospital in Greenfield Park, south of Montréal, Québec. The infectious diseases department saved 2660 bed-days using outpatient therapy. The mean duration of outpatient therapy was 7.76 days; 81.6% of patients were admitted to the program directly from the emergency room, or outpatient hospital clinics or private offices in the community. Hospitalized patients constituted only 18.4% of admissions to the outpatient intravenous antibiotic therapy program. Forty per cent of the surgical/medical staff participated in the program and they were able to generate a significant impact by diverting patients to outpatient therapy. Two types of patients can benefit from an outpatient intravenous antibiotic therapy program. One group of patients needs empirical short term therapy and can be switched to oral sequential therapy after two to five days of outpatient intravenous antibiotic therapy. A second group of patients needs specific long term therapy for the full duration of the antibiotic therapy. Empirical short term therapy can be managed by emergency department or hospital-based primary physicians, or medical/surgical specialists. Specific long term therapy can be managed by microbiology/infectious disease specialists or medical/surgical specialists. Hospitals that want to relieve pressure on emergency rooms and hospital bed demands should create facilities for both types of patients. Cefazolin and gentamicine/tobramycine were the most commonly used antibiotics in empirical short term therapy and in terms of number of patients treated. Ceftriaxone and vancomycin were most commonly used for long term therapy. The Drug acquisition antibiotic cost was $73,117 but constituted only 20% of the total outpatient intravenous antibiotic therapy cost. The per diem ambulatory cost was $140/patient/day.

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“…Inserting a 1-acetoxyethyl ester group into the cefuroxime molecule yields the prodrug cefuroxime axetil (CA), which increases its lipophilicity and facilitates absorption through the intestinal mucosa [6]. After oral administration, the prodrug is rapidly hydrolyzed and de-esterified in the intestinal mucosa and portal circulation, releasing an active moiety of cefuroxime into the systemic circulation [7][8][9]. CA exhibits weak antibacterial activity in its prodrug form, and it only becomes active after de-esterification to cefuroxime [2].…”

Section: Introductionmentioning

confidence: 99%

Optimization of a Cefuroxime Axetil-Loaded Liquid Self-Nanoemulsifying Drug Delivery System: Enhanced Solubility, Dissolution and Caco-2 Cell Uptake

et al. 2022

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Cefuroxime axetil (CA) is an oral cephalosporin which hydrolyzes rapidly to the active parent compound cefuroxime. CA is known to have incomplete oral bioavailability (30–50%) due to its poor solubility and enzymatic conversion to cefuroxime in the gut lumen. In order to overcome these drawbacks, a lipid-based self-nanoemulsifying drug delivery system (SNEDDS) has been developed and optimized. The SNEDDS formulations were prepared using the aqueous phase titration method. The greatest self-emulsifying area was found in the 2:1 Smix ratio. As a result, different SNEDDS formulations were carefully selected from this phase diagram based on their smaller droplet size < 100 nm, polydispersity index ≤ 0.5, dispersibility (Grade A), and transmittance (%) > 85%. Thermodynamic stability tests were carried out in order to rule out any metastable/unstable SNEDDS formulations. The droplet size, polydispersity index, zeta potential, and entrapment efficiency (% EE) of optimized CA-loaded SNEDDS (C-3) were 18.50 ± 1.83 nm, 0.064 ± 0.008, −22.12 ± 1.20 mV, and 97.62 ± 1.06%, respectively. In vitro release studies revealed that the SNEDDS formulation had increased CA solubility. CA-SNEDDS-C3 increased CA cellular uptake, possibly due to increased CA solubility and the inhibition of enzymatic conversion to cefuroxime. Finally, in terms of the improvement of oral bioavailability, CA-loaded-SNEDDS could be a viable alternative to commercially available CA formulations.

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Pharmaceutical, Pharmacokinetic and Other Considerations for Intravenous to Oral Stepdown Therapy

Cited by 12 publications

References 4 publications

Bacterial Skin and Soft Tissue Infections in Adults: A Review of Their Epidemiology, Pathogenesis, Diagnosis, Treatment and Site Of Care

Bacterial Skin and Soft Tissue Infections in Adults: A Review of Their Epidemiology, Pathogenesis, Diagnosis, Treatment and Site Of Care

Ambulatory Intravenous Antibiotic Therapy in Quebec: The Hôpital Charles LeMoyne Experience in 1996

Optimization of a Cefuroxime Axetil-Loaded Liquid Self-Nanoemulsifying Drug Delivery System: Enhanced Solubility, Dissolution and Caco-2 Cell Uptake

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