Alfentanil in Anesthesia and Analgesia

1986 ◽  
Vol 20 (5) ◽  
pp. 335-341 ◽  
Author(s):  
Jeffrey A. Reitz

Alfentanil is a tetrazole derivative of fentanyl. Many of the pharmacologic effects of alfentanil are similar to those of fentanyl and sufentanil, but of quicker onset than those of fentanyl and of shorter duration than those of fentanyl and sufentanil. Alfentanil may cause less intense respiratory depression than equianalgesic doses of fentanyl. Alfentanil has a lower total body clearance, smaller volume of distribution, and shorter half-life than fentanyl and sufentanil. Clinical trials indicate alfentanil can be used effectively as an analgesic, an analgesic supplement to anesthesia, an anesthetic induction agent, and as the major component of a general anesthetic. Its short duration of effect makes it attractive as an analgesic supplement for short ambulatory surgical procedures. Alfentanil is recommended for addition to drug formularies, but its use should be restricted to anesthesia personnel.

2009 ◽  
Vol 53 (8) ◽  
pp. 3266-3268 ◽  
Author(s):  
Kook-Hwan Oh ◽  
Chiweon Kim ◽  
Hankyu Lee ◽  
Hajeong Lee ◽  
Ji Yong Jung ◽  
...  

ABSTRACT The pharmacokinetic characteristics of piperacillin sodium were studied in five volunteers undergoing on-line hemodiafiltration (HDF). The subjects were given 2 g of piperacillin sodium intravenously over 1 min and placed on on-line HDF for 4 h starting at 60 min after the piperacillin infusion. Noncompartmental models were employed for estimation of the pharmacokinetic parameters, and intradialytic piperacillin clearance was calculated by the recovery method. The mean volume of distribution and the elimination half-life were 0.27 ± 0.13 liter/kg (mean ± standard deviation) and 1.1 ± 0.6 h, respectively. The total body clearance of piperacillin was 0.19 ± 0.08 liter/h/kg. Piperacillin clearance through on-line HDF was 0.11 ± 0.06 liter/h/kg. The mean serum piperacillin concentration was 4.0 ± 1.9 μg/ml at the end of the 4-h on-line HDF session. The concentration of infused piperacillin recovered in the dialysate was 527 ± 236 mg (26.3% ± 11.8%). We suggest the replacement of 500 mg of piperacillin after each on-line HDF session.


1986 ◽  
Vol 20 (9) ◽  
pp. 704-707 ◽  
Author(s):  
Maria J. Otero ◽  
Miguel Barrueco ◽  
Eduardo L. Marino ◽  
Francisco Gomez ◽  
Alfonso Dominguez-Gil

The influence of age on the disposition of theophylline was studied in 95 adult patients (nonsmokers) with bronchial asthma requiring oral theophylline therapy: 17 patients age ≥39 years, 50 patients age 40–59 years, and 28 patients < 60 years. A decrease was observed in total body clearance together with an increase in the elimination half-life of theophylline parallel to the advance in age of the patients. The apparent volume of distribution of theophylline was similar in the three groups of patients. According to the results obtained, recommendations are made regarding the dosage regimens of theophylline in elderly patients.


1992 ◽  
Vol 26 (1) ◽  
pp. 8-10 ◽  
Author(s):  
David E. Nix ◽  
J. Michael Spivey ◽  
Allyn Norman ◽  
Jerome J. Schentag

OBJECTIVE: To assess the pharmacokinetics and tolerance of ciprofloxacin after the administration of single intravenous doses of 200, 300, and 400 mg. DESIGN: Double-blind, three-period, randomized, crossover trial. SETTING: Private, university-affiliated, hospital-based, clinical research center. PATIENTS: Normal healthy male volunteers, 18–40 years of age. INTERVENTIONS: Subjects received 200-, 300-, and 400-mg single intravenous doses of ciprofloxacin via 30-minute infusions in random sequence. MAIN OUTCOME MEASURES: Serum ciprofloxacin concentrations were determined by HPLC after each dose and the results were used to derive pharmacokinetic parameters. Tolerance was assessed by reported and observed adverse events, urine microscopic examinations for crystals, and examination of intravenous infusion sites. RESULTS: The mean area under the time curve (AUC) values displayed linearity with respect to the administered dose. No statistical differences were observed in total body clearance, steady-state volume of distribution, or elimination half-life with respect to dose administered. The mean total body clearance, steady-state volume of distribution, or elimination half-life ranged from 36 to 41 L/h, 146 to 169 L, and 3.5 to 3.7 h for the 200-, 300-, and 400-mg doses, respectively. Adverse effects, including venous irritation (four subjects) and crystalluria (two subjects), were mild and did not require withdrawal of any subject from the study. CONCLUSIONS: Intravenous ciprofloxacin in doses ranging from 200 to 400 mg demonstrated linear pharmacokinetics. These single doses were well tolerated, although cases of transient venous irritation and crystalluria were observed.


2011 ◽  
Vol 2011 ◽  
pp. 1-5
Author(s):  
Harshad B. Patel ◽  
Shailesh K. Mody ◽  
Hitesh B. Patel ◽  
Vipul A. Patel ◽  
Urvesh D. Patel

The present study was carried out to investigate disposition kinetics of moxifloxacin following single-dose intravenous (i.v.), intramuscular (i.m.), and subcutaneous (s.c.) administration at a dose rate of 5 mg/kg of body weight (b.wt.) in goats. Plasma samples collected after treatments were analyzed for drug concentration using high-performance liquid chromatography (HPLC). After i.v. administration, distribution of the drug was rapid and wide as reflected by high steady-state volume of distribution. Drug elimination was relatively faster with a total body clearance of 0.59±0.03 L/h/kg. Following i.m. injection, the drug has shown the rapid and near-to-complete absorption with bioavailability of 98.20±3.96 per cent. The maximum plasma drug concentration (Cmax) of 1.21±0.04 μg/mL was attained at 1 h (Tmax). The drug was widely distributed as reflected by high apparent volume of distribution. The elimination half-life (t1/2β) of the drug was 6.26±0.08  h. Following s.c. administration, the drug was rapidly absorbed (Cmax: 1.16±0.02 μg/mL; tmax: 1 h) and slowly eliminated from the body. The elimination half-life and total body clearance (ClB) were 5.61±0.10 h and 0.60±0.03 L/h/kg, respectively. The bioavailability of moxifloxacin following s.c. administration was 90.44±3.96 per cent.


PEDIATRICS ◽  
1980 ◽  
Vol 66 (4) ◽  
pp. 579-584
Author(s):  
Carolyn M. Sack ◽  
Jeffrey R. Koup ◽  
Arnold L. Smith

We measured serum chloramphenicol concentrations in 17 hospitalized pediatric patients (aged 1 month to 6 years) after intravenous infusion of chloramphenicol succinate. The serum T½ ranged from 2.1 to 8.3 hours with a mean of 3.98 (SD 1.75) hours, while the apparent volume of distribution ranged from 0.78 to 2.09 liters/kg with a mean of 1.39 (SD 0.34) liters/kg. The total body clearance ranged 0.122 to 0.429 liters/kg/hour with a mean of 0.281 (SD 0.117) liters/kg/hour. Two patients were restudied, and had increased clearance during their hospitalization. Because of the wide variability in pharmacokinetics, we conclude that serum chloramphenicol concentrations should be monitored in infants and children.


1981 ◽  
Vol 54 (6) ◽  
pp. 736-739 ◽  
Author(s):  
Susan S. Fish ◽  
Salvador Pancorbo ◽  
Robert Berkseth

✓ Two patients requiring peritoneal dialysis were treated with epsilon-aminocaproic acid (EACA), an antifibrinolytic agent. Samples of serum and dialysate were assayed for EACA concentrations. Total body clearance, dialysis clearance, EACA half-life, and volume of distribution of EACA were calculated. Total body clearance of EACA was 26 ml/min, which is 25% of the drug clearance in patients with normal renal function. Our results suggest that patients undergoing peritoneal dialysis should receive 25% of the usual recommended dose of EACA. Dialysis clearance accounted for only 58% of total body clearance, suggesting an alternative route of elimination of EACA.


Author(s):  
Meemansha Sharma ◽  
Vinod Kumar Dumka

Disposition of antimicrobials is known to be altered during disease conditions and fever is one of the common manifestations of bacterial infections in animals. The disposition of lincomycin (10 mg/kg, IV) during Echerichia coli endotoxin-induced fever in goats followed two compartment open model and drug was detected in plasma up to 8 h. The high AUC (39.5±6.21 mg.h/mL) indicated good antibacterial activity of lincomycin in goats. The volume of distribution and total body clearance were 3.35±0.45 L/kg and 0.28±0.03 L/h/kg, respectively. The long elimination half life 9.93± 2.83 h indicated persistence of drug for longer period in body. Lincomycin, is suggested to be repeated at 24 h interval for organisms sensitive to lincomycin having MIC up to 0.6 µg/mL for the treatment of bacterial infections manifested with fever in goats.


1983 ◽  
Vol 3 (3) ◽  
pp. 135-137 ◽  
Author(s):  
Salvador Pancorbo ◽  
Christina Comty

The pharmacokinetics of cefamandole have been evaluated in five patients undergoing continuous ambulatory peritoneal dialysis (CAPD). The drug was absorbed rapidly from the peritoneum reaching peak serum concentrations averaging 31.3 mcg/ml. Approximately 72% of the dose instilled into the peritoneum was absorbed over a six hour period. Subsequently cefamandole disappeared from the serum slowly with a mean half-life of 10.4 hours. The volume of distribution was 0.25 I/kg. The calculated total body clearance averaged 20.0 ml/min and the mean dialysis clearance was 3.2 ml/min. The authors postulate that in renal failure patients cefamandole may be eliminated by an alternate route.


2007 ◽  
Vol 85 (5) ◽  
pp. 502-506 ◽  
Author(s):  
Mara Medeiros ◽  
José Pérez-Urizar ◽  
José Pedraza-Chaverri ◽  
Ricardo Muñoz-Arizpe ◽  
Gilberto Castañeda-Hernández

Components of whole blood and plasma are highly altered during the presentation of nephrotic syndrome. The present study was aimed to explore the influence of nephrotic syndrome on the pharmacokinetics of cyclosporine (CsA) (10 mg/kg) administered i.v. to control or puromycin-induced nephrotic rats (P-NS). We found an increase in CsA bioavailability in the nephrotic group compared with controls. The area under the curve of blood CsA versus time (AUCiv) increased from 27.7 ± 5.3 to 60.6 ± 13.8 μg·h·mL–1 in control and P-NS rats, respectively. The AUCiv augmentation was positively correlated with cholesterol levels. On the other hand, the total body clearance was significantly lower (0.38 ± 0.06 vs. 0.17 ± 0.03 L·(kg body mass)–1·h–1) and the volume of distribution at steady state (3.70 ± 0.52 vs. 2.85 ± 0.32 L/kg) was significantly smaller in nephrotic rats as compared with control. These pharmacokinetic changes lead to a longer terminal half-life of CsA in P-NS rats (11.8 ± 1.6 vs. 6.9 ± 0.91 h). We conclude that the physiopathologic changes induced by the nephrotic syndrome in P-NS animals result in a significant increase in CsA blood exposure by both the decrease in drug distribution and the reduction in elimination rate of CsA.


1987 ◽  
Vol 1 (3) ◽  
pp. 147-149 ◽  
Author(s):  
Sheldon L. Spector ◽  
Robert Altman

Cetirizine, an oxidative metabolite of hydroxyzine, is a cyclizine class H1-receptor antagonist with diminished CNS activity currently under investigation. It has a novel pharmacokinetic profile with a 9-hour half-life, lower volume of distribution and total body clearance, minimal metabolism and essentially renal excretion. Minimal binding to CNS receptors has been demonstrated in animal models. In contrast to its parent compound and diphenhydramine, cetirizine has an effect comparable to placebo on psychomotor function and multiple sleep latency tests. Inhibition of histamine-induced bronchospasm and mild bronchodilation has also been demonstrated. U.S. and European clinical trials have affirmed its safety and efficacy in histamine-associated disorders.


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