Disposition of Deracoxib in Cats After Oral Administration

2006 ◽  
Vol 42 (3) ◽  
pp. 212-217 ◽  
Author(s):  
Adam D. Gassel ◽  
Karen M. Tobias ◽  
Sherry K. Cox
Keyword(s):  
Adverse Effects ◽  
Oral Administration ◽  
Drug Administration ◽  
Half Life ◽  
Maximum Concentration ◽  
Efficacy And Safety ◽  
Terminal Half Life ◽  
The Mean ◽  
Chronic Use

The pharmacokinetics of deracoxib in seven healthy cats were determined following a single oral (1 mg/kg) dose. Minimal variability among cats was found for all estimated pharmacokinetic variables. Terminal half-life (t1/2) was 7.9 hours. The mean maximum concentration (Cmax) was 0.28 μg/mL and was measured 3.64 hours after drug administration. Deracoxib was not detectable in the plasma after 60 hours. The compounded liquid formula was accepted readily, and no adverse effects were observed. Further studies are needed to determine the efficacy and safety of deracoxib after acute and chronic use in the cat.

scholarly journals hCGbeta core fragment is a metabolite of hCG: evidence from infusion of recombinant hCG

2000 ◽  
Vol 164 (3) ◽  
pp. 299-305 ◽  
Author(s):  
RJ Norman ◽  
MM Buchholz ◽  
AA Somogyi ◽  
F Amato
Keyword(s):  
Renal Clearance ◽  
Clearance Rate ◽  
Half Life ◽  
Urine Samples ◽  
Molar Ratio ◽  
Gel Chromatography ◽  
Core Fragment ◽  
Terminal Half Life ◽  
Intact Molecule ◽  
The Mean

The availability of recombinant human chorionic gonadotrophin (r-hCG) has allowed us to measure its metabolic and renal clearance rates and to study the origin of the beta core fragment of hCG (hCGbetacf). Serum and urine samples were collected from six subjects, after an intravenous injection of 2 mg (equivalent to 44 000 IU Urinary hCG) r-hCG, and assayed for hCG and the beta subunit (hCGbeta). Urine from four of the subjects was also subjected to gel chromatography and assayed for hCGbetacf and hCG. r-hCG, administered as an intravenous dose, was distributed, initially in a volume of 3.4+/-0.7 l (mean+/-s.d.) and then in 6.5+/-1.15 l at steady-state. The disappearance of r-hCG from serum was bi-exponential, with an initial half-life of 4.5+/-0.7 h and a terminal half-life of 29.0+/-4.6 h. The mean residence time was 28. 6+/- 3.6 h and the total systemic clearance rate of r-hCG was 226+/-18 ml/h. The renal clearance rate was 28.75+/-6.2 ml/h (mean+/-s.d). hCGbetacf was detected in all urine samples collected at 6 h intervals. Over the 138 h period of urine collection, 12.9% (range 10.1-17.3% ) of r-hCG injected was recovered as the intact molecule and 1.7% (range 0.8-2.9%) was recovered as the hCGbetacf, in 4 subjects. The molar ratio of hCGbetacf to hCG in urine increased from 3.1+/-1.7%, on day 1, to 76+/-34.3% (mean+/-s.e.m.) on day 5, after r-hCG infusion, suggesting that hCGbetacf is a metabolic product of the infused r-hCG.

Nimodipine in the Treatment of Subarachnoid Hemorrhage

DICP ◽  
1989 ◽  
Vol 23 (6) ◽  
pp. 451-455 ◽  
Author(s):  
Sally Usdin Yasuda ◽  
Karen J. Tietze
Keyword(s):  
Subarachnoid Hemorrhage ◽  
Adverse Effects ◽  
Oral Administration ◽  
Calcium Channel Antagonist ◽  
Clinical Studies ◽  
Oral Bioavailability ◽  
Half Life ◽  
Cerebral Blood Vessels ◽  
Vasodilatory Effect ◽  
Intravenous And Oral Administration

Nimodipine, a calcium-channel antagonist with a relatively selective vasodilatory effect on cerebral blood vessels, has recently been approved for improvement of neurologic deficits due to spasm following subarachnoid hemorrhage. Nimodipine has low oral bioavailability (2.7–27.9 percent), a short half-life (2 h), is highly protein bound (98–99 percent), and is hepatically metabolized. Clinical studies have evaluated topical, intravenous, and oral administration of nimodipine for the treatment of cerebral artery spasm associated with subarachnoid hemorrhage. These studies document some benefit of the drug in reducing the occurrence of severe neurologic deficit, although this effect is not universal. Few adverse effects have been noted. Further studies are necessary to evaluate the pharmacologic and pharmacokinetic characteristics, the appropriate dose and route of administration, adverse effects, drug interactions, and the therapeutic efficacy of nimodipine before routine use can be recommended.

scholarly journals Pharmacokinetics of Novel Erythropoiesis Stimulating Protein Compared with Epoetin Alfa in Dialysis Patients

1999 ◽  
Vol 10 (11) ◽  
pp. 2392-2395 ◽  
Author(s):  
IAIN C. MACDOUGALL ◽  
STEPHEN J. GRAY ◽  
ORLAITH ELSTON ◽  
CORMAC BREEN ◽  
BARBARA JENKINS ◽  
...  
Keyword(s):  
Single Dose ◽  
Half Life ◽  
Epoetin Alfa ◽  
Dialysis Patients ◽  
Open Label ◽  
Double Blind ◽  
Time Curve ◽  
Peptide Mass ◽  
Terminal Half Life ◽  
The Mean

Abstract. Novel erythropoiesis stimulating protein (NESP) is a hyperglycosylated analogue of recombinant human erythropoietin (Epoetin) which has an increased terminal half-life in animal models. The aim of this study was to extend these observations to humans. Using a double-blind, randomized, cross-over design, the single-dose pharmacokinetics of Epoetin alfa (100 U/kg) and an equivalent peptide mass of NESP were compared following intravenous bolus in 11 stable peritoneal dialysis patients. This was followed by an open-label study to determine the single-dose pharmacokinetics of an equivalent peptide mass of NESP by subcutaneous injection in six of these patients. The mean terminal half-life for intravenous NESP was threefold longer than for intravenous Epoetin (25.3 versus 8.5 h), a difference of 16.8 h (95% confidence interval, 9.4 to 24.2 h, P = 0.0008). The area under the serum concentration—time curve was significantly greater for NESP (291.0 ± 7.6 ng · h per ml versus 131.9 ± 8.3 ng · h per ml; mean ± SEM; P < 0.0005), and clearance was significantly lower (1.6 ± 0.3 ml/h per kg versus 4.0 ± 0.3 ml/h per kg; mean ± SEM; P < 0.0005). The volume of distribution was similar for NESP and Epoetin (52.4 ± 2.0 ml/kg versus 48.7 ± 2.1 ml/kg; mean ± SEM). The mean terminal half-life for subcutaneous NESP was 48.8 h. The peak concentration of subcutaneous NESP was approximately 10% of that following intravenous administration, and bioavailability was approximately 37% by the subcutaneous route. The longer half-life of NESP is likely to confer a clinical advantage over Epoetin by allowing less frequent dosing in patients treated for anemia.

The Formation of Deoxycholic Acid and Chenodeoxycholic Acid in Man

1974 ◽  
Vol 46 (2) ◽  
pp. 183-190
Author(s):  
Kurt Einarsson ◽  
Kjell Hellström
Keyword(s):  
Oral Administration ◽  
Cholic Acid ◽  
Chenodeoxycholic Acid ◽  
Half Life ◽  
Deoxycholic Acid ◽  
Pool Size ◽  
Acid Fraction ◽  
Turnover Rates ◽  
Mean Values ◽  
The Mean

1. The turnover of deoxycholic acid and chenodeoxycholic acid was studied in six normolipaemic patients after oral administration of trace amounts of isotopically labelled compounds. 2. The mean values for half-life, pool size and turnover of deoxycholic acid were 3·0 days, 663 mg and 171 mg/day respectively. The corresponding values recorded for chenodeoxycholic acid were 2·8 days, 781 mg and 207 mg/day. 3. A comparison of the turnover rates of deoxycholic acid and cholic acid in three subjects indicated that 25–61% of the cholic acid was converted into deoxycholic acid. 4. Only trace amounts of radioactivity were recovered in the trihydroxycholanic acid fraction of duodenal bile after the administration of [14C]deoxycholic acid or [3H]chenodeoxycholic acid.

Pharmacokinetic Comparison of Intravenous and Oral Chloramphenicol in Patients with Haemophilus in fluenzae Meningitis

PEDIATRICS ◽  
1981 ◽  
Vol 67 (5) ◽  
pp. 656-660
Author(s):  
Ram Yogev ◽  
William M. Kolling ◽  
Tommy Williams
Keyword(s):  
Serum Level ◽  
Oral Administration ◽  
Intravenous Administration ◽  
Half Life ◽  
Peak Serum ◽  
Peak Serum Level ◽  
Wide Range ◽  
Csf Levels ◽  
The Mean ◽  
Intravenous And Oral Administration

The pharmacokinetics of chloramphenicol following intravenous and oral administration were studied in 14 infants with Haemophilus influenzae meningitis. Following five days of treatment with intravenous chloramphenicol (100 mg/kg/day every six hours), oral chloramphenicol was substituted at the same dose. Multiple serum levels of chloramphenicol were determined after an intravenous dose on day 4 and after an oral dose on day 10. CSF levels were measured six hours after intravenous or oral chloramphenicol dose on those days (CSF trough). Following intravenous administration, the mean peak serum level of 15.0 µ/g ml was reached at 45 minutes. In comparison, after oral chloramphenicol in the same dosage, the mean peak serum level of 18.5 µg ml was achieved at two to three hours. The mean serum half-life of the drug (6.5 hours) was significantly longer after oral administration than after intravenous chloramphenicol (4.0 hours) (P .001). The increased serum half-life following orally administered chloramphenicol was occasionally associated with drug accumulation. In addition, mean trough CSF levels were somewhat higher when the patient received oral medication (6.6 µg/ml) compared to intravenous administration (4.2 µ/ml) (P .001). For any treatment regimen for H influenzae meningitis that includes a period of oral chloramphenicol therapy the patient should be hospitalized to ensure compliance. Because of the wide range of individual variation in serum half-life that may result in accumulation, periodic monitoring of serum chloramphenicol levels is also recommended.

Pharmacokinetics and Inflammatory Fluid Penetration of Clinafloxacin

1998 ◽  
Vol 42 (2) ◽  
pp. 428-430 ◽  
Author(s):  
R. Wise ◽  
S. Jones ◽  
I. Das ◽  
J. M. Andrews
Keyword(s):  
Half Life ◽  
Maximum Concentration ◽  
Healthy Male ◽  
Elimination Half Life ◽  
Concentration Time ◽  
Healthy Male Volunteers ◽  
Elimination Half ◽  
The Mean ◽  
Fluid Penetration ◽  
Mean Time

ABSTRACT A single 200-mg dose of clinafloxacin was given orally to each of nine healthy male volunteers, and the concentrations of the drug were measured in plasma, cantharidin-induced inflammatory fluid, and urine over the following 24 h (48 h in the case of urine). The mean maximum concentration in plasma was 1.34 μg/ml at a mean time of 1.8 h postdose. The mean maximum concentration in the inflammatory fluid was 1.3 μg/ml at 3.8 h postdose. The mean elimination half-life of clinafloxacin in plasma was 5.65 h. The overall penetration into the inflammatory fluid was 93.1%, as assessed by determining the ratio of area under the concentration-time curves. Recovery of clinafloxacin in urine was 58.8% by 24 h and 71.8% by 48 h postdose.

Opioids in Spine Pain: Indications, Challenges, and Controversies

2018 ◽  
Author(s):  
Puneet Sayal ◽  
Jianren Mao
Keyword(s):  
Adverse Effects ◽  
Risk Stratification ◽  
Close Monitoring ◽  
Efficacy And Safety ◽  
Term Efficacy ◽  
Spine Pain ◽  
Term Basis ◽  
Opioid Medications ◽  
Chronic Use

Opioid medications are commonly used in the treatment of spine-mediated pain. They are used on a chronic, long-term basis, and their use is on the rise. The available evidence supports their use for short periods if much effort is put into patient and opioid selection, and with close monitoring. Challenges include numerous adverse effects, aberrant behaviors, and the comfort and skill set of providers. Controversies surrounding the chronic use of opioids center on the inconclusive evidence regarding long-term efficacy and safety. More research is necessary to determine whether these medications are appropriate, efficacious, and safe over the long term, and also to aid providers in managing patients on chronic opioids in terms of patient and opioid selection, risk stratification, monitoring, and discontinuation/weaning.

scholarly journals Single-dose pharmacokinetics of thalidomide in human immunodeficiency virus-infected patients.

1997 ◽  
Vol 41 (12) ◽  
pp. 2797-2799 ◽  
Author(s):  
S C Piscitelli ◽  
W D Figg ◽  
B Hahn ◽  
G Kelly ◽  
S Thomas ◽  
...  
Keyword(s):  
Human Immunodeficiency Virus ◽  
Single Dose ◽  
Adverse Effects ◽  
Half Life ◽  
Elimination Half Life ◽  
Elimination Half ◽  
Immunodeficiency Virus ◽  
The Mean ◽  
Standard Deviations

The pharmacokinetics of thalidomide in nine human immunodeficiency virus-infected patients were studied. Single doses of thalidomide were well absorbed, with mean peak concentrations (+/- standard deviations) of 1.17 +/- 0.21 and 3.47 +/- 1.14 microg/ml in the 100- and 300-mg dosing groups, respectively, and the mean elimination half-life was approximately 6 h. Adverse effects were mild, with drowsiness being reported for seven of nine patients.

Pharmacokinetics of pimobendan following oral administration to New Zealand White rabbits (Oryctolagus cuniculus)

2022 ◽  
pp. 1-8
Author(s):  
Sarah M. Ozawa ◽  
David Sanchez-Migallon Guzman ◽  
Michelle G. Hawkins ◽  
Stephanie M. Diao ◽  
Acacia E. Masri ◽  
...  
Keyword(s):  
Critical Care ◽  
New Zealand ◽  
Oral Administration ◽  
Half Life ◽  
Maximum Concentration ◽  
Plasma Concentrations ◽  
Pharmacokinetic Parameters ◽  
Pilot Studies ◽  
New Zealand White Rabbits ◽  
Target Plasma Concentration

Abstract OBJECTIVE To determine the pharmacokinetics and potential adverse effects of pimobendan after oral administration in New Zealand White rabbits (Ocytolagus cuniculi). ANIMALS 10 adult sexually intact (5 males and 5 females) rabbits. PROCEDURES 2 pilot studies were performed with a pimobendan suspension or oral tablets. Eight rabbits received 7.5 mg of pimobendan (mean 2.08 mg/kg) suspended in a critical care feeding formula. Plasma concentrations of pimobendan and O-demethylpimobendan (ODMP) were measured, and pharmacokinetic parameters were calculated for pimobendan by noncompartmental analysis. Body weight, food and water consumption, mentation, urine, and fecal output were monitored. RESULTS Mean ± SD maximum concentration following pimobendan administration was 15.7 ± 7.54 ng/mL and was detected at 2.79 ± 1.25 hours. The half-life was 3.54 ± 1.32 hours. Plasma concentrations of pimobendan were detectable for up to 24 hours. The active metabolite, ODMP, was detected in rabbits for 24 to 36 hours. An adverse event occurred following administration of pimobendan in tablet form in 1 pilot study, resulting in death secondary to aspiration. No other adverse events occurred. CLINICAL RELEVANCE Plasma concentrations of pimobendan were lower than previously reported for dogs and cats, despite administration of higher doses, and had longer time to maximum concentration and half-life. Based on this study, 2 mg/kg of pimobendan in a critical care feeding formulation should maintain above a target plasma concentration for 12 to 24 hours. However, further studies evaluating multiple-dose administration as well as pharmacodynamic studies and clinical trials in rabbits with congestive heart failure are needed to determine accurate dose and frequency recommendations.

Pharmacokinetics and penetration into inflammatory fluid of trovafloxacin (CP-99,219).

1996 ◽  
Vol 40 (1) ◽  
pp. 47-49 ◽  
Author(s):  
R Wise ◽  
D Mortiboy ◽  
J Child ◽  
J M Andrews
Keyword(s):  
Oral Dose ◽  
Half Life ◽  
Maximum Concentration ◽  
Healthy Male ◽  
Elimination Half Life ◽  
Concentration Time ◽  
Elimination Half ◽  
The Mean ◽  
Systemic Infections ◽  
Mean Time

A single 200-mg oral dose of trovafloxacin (CP-99,219) was given to each of eight healthy male volunteers, and the concentrations of the drug were measured in plasma, cantharides-induced inflammatory fluid, and urine over the subsequent 36 h. The mean maximum concentration observed in plasma was 2.9 micrograms/ml at a mean time of 0.75 h postdose. The mean maximum concentration observed in inflammatory fluid was 1.2 micrograms/ml at 4.0 h postdose. The mean elimination half-life in plasma was 7.8 h. The overall penetration into inflammatory fluid was 64%, as assessed by determining the ratio of the area under the concentration-time curves. Recovery of the dose in urine within the first 36 h postdose was 5.0% of the administered dose. Our results indicate that trovafloxacin, at a dosage of 200 mg once or twice daily, should be adequate for the treatment of systemic infections caused by most common bacterial pathogens.

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