Study of Pharmacokinetics and Comparative Bioavailability of Nefopam 30 mg Tablets in Twelve Fasting Healthy Pakistani Male Young Subjects: Single-Dose, Randomized, Two-Period, Two-Treatment and Two-Way Cross-Over Design

Ahmad, Mahmood; Yaqoob, Muhammad; Murtaza, Ghulam

doi:10.1159/000333560

Cited by 3 publications

(2 citation statements)

References 8 publications

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“…Nefopam undergoes significant first pass metabolism as the bioavailability (F) is 0.36 + 0.13 (24,26). The peak plasma concentration (T max ) has been reported as 0.073 -0.155 mg/L (90 mg dose (19)), 0.067 + 0.002 mg/L (30 mg dose (23) (25), and between 3 -8 h in both oral and intravenous studies (19). The drug distributes throughout the body with estimated volumes of distribution (V d ) of 410 + 115 L; 447 + 98 L (25) and 535 + 139 L (24).…”

Section: Discussionmentioning

confidence: 99%

Nefopam Hydrochloride: A Fatal Overdose

et al. 2015

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Nefopam is a non-opiate analgesic commonly used for the treatment of moderate to severe pain. A case of a 37-year-old male who was found dead in the morning is presented. An autopsy was performed and femoral venous blood, heart blood, urine, and vitreous humor were submitted for toxicological analysis. A general drug screen detected the presence of nefopam, caffeine, nicotine, citalopram, gabapentin, amitriptyline, diazepam and paracetamol in cardiac blood. Nefopam was quantitated by high-performance liquid chromatography with diode-array detection. Nefopam was found at the following concentrations: 13.6 mg/L in unpreserved femoral blood; 14.7 mg/L in preserved (fluoride-oxalate) femoral blood; 21.2 mg/L in unpreserved cardiac blood and 4.5 mg/L in preserved vitreous. Citalopram was present at a concentration of 0.7 mg/L (femoral blood) and 0.9 mg/L (cardiac blood). Ethanol analyzed by headspace gas chromatography (GC-FID) was detected in preserved (fluoride-oxalate) vitreous (14 mg/100 mL) and preserved (fluoride-oxalate) urine 50 mg/100 mL. Death was attributed to atherosclerotic coronary artery disease and therapeutic drug toxicity.

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Section: Discussionmentioning

confidence: 99%

Nefopam Hydrochloride: A Fatal Overdose

et al. 2015

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“…The first sequence received nefopam alone, whereas second sequence received nefopam with modulated electro-hyperthermia. Based on the results of a previous study [ 11 ] on the wash-out period (the time until the drug is excreted from the body) the time between the first sequence and sequence of nefopam from the human body was set at 7 days.…”

Section: Methodsmentioning

confidence: 99%

The effect of modulated electro-hyperthermia on the pharmacokinetic properties of nefopam in healthy volunteers: A randomised, single-dose, crossover open-label study

Lee

Kim

2015

International Journal of Hyperthermia

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Purpose: Nefopam is a widely available analgesic for the management of pain. The aim of this study was to reveal the effect of regional hyperthermia of the abdominal area on the pharmacokinetics of nefopam. Materials and methods: A randomised, single-dose, crossover, open-label study was conducted to reveal the effect of hyperthermia using modulated electro-hyperthermia on the pharmacokinetics of nefopam. The pharmacokinetics of orally administered nefopam without hyperthermia was studied in 12 healthy volunteers and then 7 days later they were treated with nefopam plus modulated electro-hyperthermia to the abdominal area for 1 h. Blood samples were collected up to 24 h after the drug administration. From the blood concentration-time curve, the maxinum plasma concentration (Cmax), time to Cmax (Tmax) and the area under the curve (AUC) were obtained. The safety and tolerability of these treatments were also assessed. Results: The geometric mean ratios (GMRs) ((nefopam + modulated electro-hyperthermia)/nefopam) and the associated 90% confidence intervals (CIs) for Cmax, AUClast and AUCinf were 1.2804 (1.1155∼1.4696), 1.0512 (0.9555∼1.1566) and 1.0612 (0.9528∼1.1819), respectively. The increase in Cmax was statistically significant, and Tmax was significantly shortened. Conclusions: The significant increase in Cmax and decrease in Tmax indicated that modulated electro-hyperthermia increased the absorption of the orally administered nefopam, thereby transitionally increasing the blood concentration of the drug. The AUC is an important parameter that contributes to the therapeutic effect of drugs. The lack of significant change in AUC suggests that modulated electro-hyperthermia may increases the absorption of orally administered drugs without increasing the systemic adverse effect of the drugs.

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Morphine-Sparing Effect of Intermittent Versus Continuous Intravenous Infusion of Nefopam in Patients After Total Knee Arthroplasty: A Randomized Trial

Kachacheewa,

Wattanavijitkul,

Wongsak

et al. 2024

Rama Med J

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Background: Nefopam, a nonopioid analgesic, is recommended to improve pain control and minimize opioid-related side effects following total knee arthroplasty (TKA). Objective: To compare cumulative morphine consumption between intermittent infusion (II) and continuous infusion (CI) of nefopam, combined with other multimodal analgesics, in TKA patients. Methods: Fifty-eight patients were randomly assigned to receive either intermittent nefopam infusion (II group) (20 mg IV every 6 hours) or continuous infusion (CI group) (80 mg/day). The primary outcome was cumulative morphine consumption via patient-controlled analgesia, with secondary outcomes including pain scores every 4 hours and adverse drug reactions (ADRs). Results: No significant difference was found in cumulative morphine consumption (median [range], 4 [0 -12] mg in II and 6 [0 - 18] mg in CI; P = .579) and the ADRs over 48 hours between groups. At 4 hours, the II group had significantly lower pain scores compared to the CI group (median [range], 0 [0 - 4] and 0 [0 - 8]; P = .008). However, by 24 and 36 hours, the CI group reported significantly lower pain scores compared to the II group; median (range), 0 (0 - 5) vs 2 (0 - 9) at 24 hours (P = .020) and 0 (0 - 4) vs 2 (0 - 8) at 36 hours (P = .014). Conclusions: Both intermittent and continuous nefopam infusion in primary TKA showed no significant difference in morphine-sparing or occurrence of ADRs within the 48-hour follow-up period. These findings suggest that both infusion methods are comparable in managing post-operative pain in TKA patients.

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Study of Pharmacokinetics and Comparative Bioavailability of Nefopam 30 mg Tablets in Twelve Fasting Healthy Pakistani Male Young Subjects: Single-Dose, Randomized, Two-Period, Two-Treatment and Two-Way Cross-Over Design

Cited by 3 publications

References 8 publications

Nefopam Hydrochloride: A Fatal Overdose

Nefopam Hydrochloride: A Fatal Overdose

The effect of modulated electro-hyperthermia on the pharmacokinetic properties of nefopam in healthy volunteers: A randomised, single-dose, crossover open-label study

Morphine-Sparing Effect of Intermittent Versus Continuous Intravenous Infusion of Nefopam in Patients After Total Knee Arthroplasty: A Randomized Trial

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