Pain and Clinical Thrombophlebitis following Intravenous Diazepam and Lorazepam

Graham, Charles W.; Pagano, R. R.; Conner, J. T.

doi:10.1097/00132586-197904000-00013

Cited by 6 publications

(8 citation statements)

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“…However, some volunteers who received AM149 1% experienced postinjection thrombophlebitis although no pain was felt during drug injection. Similar findings were also reported during the introduction of intravenous diazepam in the late 1970s [29].…”

Section: Discussionsupporting

confidence: 88%

Pharmacological characteristics and side effects of a new galenic formulation of propofol without soyabean oil*

et al. 2003

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SummaryWe compared the pharmacokinetics, pharmacodynamics and safety profile of a new galenic formulation of propofol (AM149 1%), which does not contain soyabean oil, with a standard formulation of propofol (Disoprivan Ò 1%). In a randomised, double-blind, cross-over study, 30 healthy volunteers received a single intravenous bolus injection of 2.5 mg.kg )1 propofol. Plasma propofol levels were measured for 48 h following drug administration and evaluated according to a three-compartment model. The pharmacodynamic parameters assessed included induction and emergence times, respiratory and cardiovascular effects, and pain on injection. Patients were monitored for side effects over 48 h. Owing to a high incidence of thrombophlebitis, the study was terminated prematurely and only the data of the two parallel treatment groups (15 patients in each group) were analysed. Plasma concentrations did not differ significantly between the two formulations. Anaesthesia induction and emergence times, respiratory and cardiovascular variables showed no significant differences between the two treatment groups. Pain on injection (80 vs. 20%, p < 0.01) and thrombophlebitis (93.3 vs. 6.6%, p < 0.001) occurred more frequently with AM149 than with Disoprivan Ò . Although both formulations had similar pharmacokinetic and pharmacodynamic profiles the new formulation is not suitable for clinical use due to the high incidence of thrombophlebitis produced.

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Section: Discussionsupporting

confidence: 88%

Pharmacological characteristics and side effects of a new galenic formulation of propofol without soyabean oil*

et al. 2003

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“…While intravenous (IV), per rectum (PR), and intranasal (IN) administration of diazepam have been reported (Averill, ; Mealey & Boothe, ; Papich & Alcorn, ; Podell, ; Platt et al ., ; Musulin et al ., ), the intramuscular (IM) route is not feasible owing to slow systemic absorption and severe tissue irritation that can potentially lead to necrosis (Steiness et al ., ; Magnussen et al ., ). In addition, IV administration has been associated with a high incidence of thrombophlebitis and pain during injection in people (Graham et al ., ). In contrast, midazolam (MDZ) causes minimal irritation when injected IV and can also be administered IM.…”

Section: Introductionmentioning

confidence: 97%

The pharmacokinetics of midazolam after intravenous, intramuscular, and rectal administration in healthy dogs

Schwartz

Muñana

Nettifee-Osborne

et al. 2012

Vet Pharm & Therapeutics

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Intravenous benzodiazepines are utilized as first-line drugs to treat prolonged epileptic seizures in dogs and alternative routes of administration are required when venous access is limited. This study compared the pharmacokinetics of midazolam after intravenous (IV), intramuscular (IM), and rectal (PR) administration. Six healthy dogs were administered 0.2 mg/kg midazolam IV, IM, or PR in a randomized, 3-way crossover design with a 3-day washout between study periods. Blood samples were collected at baseline and at predetermined intervals until 480 min after administration. Plasma midazolam concentrations were measured by high-pressure liquid chromatography with UV detection. Rectal administration resulted in erratic systemic availability with undetectable to low plasma concentrations. Arithmetic mean values ± SD for midazolam peak plasma concentrations were 0.86 ± 0.36 μg/mL (C0) and 0.20 ± 0.06 μg/mL (Cmax), following IV and IM administration, respectively. Time to peak concentration (Tmax ) after IM administration was 7.8 ± 2.4 min with a bioavailability of 50 ± 16%. Findings suggest that IM midazolam might be useful in treating seizures in dogs when venous access is unavailable, but higher doses may be needed to account for intermediate bioavailability. Rectal administration is likely of limited efficacy for treating seizures in dogs.

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“…[10] Diazepam, a benzodiazepine, is included in the "WHO Essential Drug list" for the treatment of convulsion and epileptic seizure [11][12][13][14]. Although intravenous therapy is the most rapid way to suppress epileptic convulsion, it may produce toxic manifestation due to excessive drug concentration [15,16], requires great care and caution to avoid thrombophlebitis and irritation [17] and may not be feasible where adequate medical facilities are not available in the immediate vicinity. While absorption of diazepam from intramuscular route is poor and erratic [18], the time to reach peak plasma concentration following oral administration is 1-2 hours [19] and is accompanied with acid hydrolysis and extensive liver metabolism [10].…”

Section: Introductionmentioning

confidence: 99%

Preparation and Evaluation of Rapidly Disintegrating Fast Release Tablet of Diazepam-Hydroxypropyl-β-Cyclodextrin Inclusion Complex

Giri¹,

Sa²

2010

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This study was undertaken to develop tablets of diazepam-hydroxypropyl-β-cyclodextrin inclusion complex that disintegrate within 3 minutes and release 85% of drug within 30 minutes to provide rapid action of the drug through oro-mucosal route. Formation of inclusion complex was verified using X-ray diffraction and differential scanning calorimetric studies. Enhanced of aqueous solubility, as evident from phase solubility study, and dissolution of the drug were related with the formation of inclusion complex. Among the various formulations, tablet containing inclusion complex of drug/hydroxypropyl-β-cyclodextrin in a molar ratio of 1:2, and a combination of microcrystalline cellulose/lactose in a ratio of 4:1 disintegrated in 13 seconds and released 85% drug within 9 minutes. Addition of 10% w/w polyvinyl pyrrolidone in the tablet formulation further enhanced the drug release. Accelerated stability study indicated that mean dissolution time of the drug from the tablet did not change significantly within 6 months.

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Pain and Clinical Thrombophlebitis following Intravenous Diazepam and Lorazepam

Cited by 6 publications

References 0 publications

Pharmacological characteristics and side effects of a new galenic formulation of propofol without soyabean oil*

Pharmacological characteristics and side effects of a new galenic formulation of propofol without soyabean oil*

The pharmacokinetics of midazolam after intravenous, intramuscular, and rectal administration in healthy dogs

Preparation and Evaluation of Rapidly Disintegrating Fast Release Tablet of Diazepam-Hydroxypropyl-β-Cyclodextrin Inclusion Complex

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