Conventional preparations of diazepam for i.v. use contain solvents which cause pain on injection and thrombophlebitis in a high percentage of cases. However, diazepam can be dissolved with advantage in the oleaginous phase of an oil-in-water emulsion (Diazemuls). Diazemuls has been given to 9492 patients without serious side-effects. Following i.v. injection, 2435 patients were studied with respect to pain and clinical effect. Only 0.4% experienced pain. The intended clinical effect was recorded in 99% of the patients. I.m. injection of Diazemuls resulted in a significantly smaller frequency of pain in connection with the injection than did the injection of Valium (7% and 43% respectively). Pharmacokinetic studies have been made after i.v. and i.m. injection of Diazemuls and Valium. The distribution and elimination phases after i.v. injection were the same with both forms. Thus the drug probably quickly separates from the oil particles of the emulsion after injection. After i.m. administration, the plasma concentration shows a wide spread with both preparations. A brief survey of other substances tested in emulsion form is presented.

Adolescent↗

PubMed1982

[Guidelines for total parenteral nutrition].

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Humans↗

PubMed1977

Allergy to diazepam--or vehicle.

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Diazepam↗

PubMed1976

Diazepam in emulsion form for intravenous usage.

Since aqueous solutions of diazepam were introduced into clinical practice, the problem has arisen of local vascular side effects after intravenous injection. A new preparation of diazepam as a lipid emulsion is presented. It was prepared by Vitrum and shows many similarities to Intralipid. A clinical trial was designed to study the incidence of pain in connection with the intravenous injection of diazepam and the incidence of subsequent thrombophlebitis. The preparation was used as a sedative to patients before gastroscopic investigation and as an inductor to general anaesthesia. In the material of 88 patients, thrombophlebitis was observed in 1.1%. Only 1 patient in the group of 314 patients studied complained of pain in connection with injection. The results observed were compared with previous investigations from the literature and with parallel control investigations. The new lipid emulsion form of the preparation was found to reduce significantly the incidence of local side effects involving the venous system. No significant difference in the therapeutic effect of the different preparative forms of the active substance was observed. The possible mechanisms involving the production of thrombophelbitis in connection with the injection of aqueous solutions of diazepam are discussed.

Adjuvants, Anesthesia↗