Dormicum

We have examined the effects of commercially available preparations and drug-free solvents of Midazolam (Dormicum) and Propofol (Disoprivan) by N-formyl-methionyl-leucyl-phenylalanine (FMLP) -induced polymorphonuclear cell (PMN) chemiluminescence system. In the case of propofol and drug-free solvent, PMN chemiluminescence was suppressed. With Midazolam, only the active drug depressed PMN chemiluminescence.

Authors report on the sedative anxiolytic and anterograde amnesia causing effect of "Dormicum", in connection with 170 dental and/or oral surgery interventions. Initial dose of Dormicum was 0.1 mg/body weight kgs,--necessary repetitions occurred with 0.02-0,03 mg/body weight kgs. In 75% of the patients an acceptable level of sedation developed by using 0.1 mg/body weight kgs. In more than 90% of the cases anterograde amnesia could be observed, which seemed to be the most important element of this kind of treatment...

The authors analyze the efficacy of midazolam (dormicum, Egys, Hungary) used for induction anesthesia in 35 patients subjected to planned surgery for varicose disease of the lower limbs and on the abdominal organs and in 17 critical patients in intensive care units. To assess the hemodynamics, catheterization of the peripheral and pulmonary arteries was carried out, cardiac output, pressure in cardiac cavities, pulmonary capillary wedging pressure assessed, total peripheral and total pulmonary resistance, cardiac and stroke indexes estimated, gaseous composition of arterial and mixed venous blood analyzed...

In a randomized double-blind study, Midazolam (Dormicum) (7.5 mg) was compared with Promethazine (Phenergan) (25 mg), Droperidol (2.5 mg) and placebo as premedication for 98 pre-selected patients undergoing surgery. The anxiolytic effect of the above drugs was monitored by Beck's Anxiety Inventory. 83.3% of patients who received Midazolam had a decrease in their anxiety state compared to 55.6% for Promethazine, 12% for Droperidol and 25% for placebo. The study clearly proved that Midazolam is a better anxiolytic drug compared to Droperidol and Promethazine...

The effect on intraocular pressure of induction of anesthesia with 8-chloro-6-(2-fluorophenyl)-1-methyl-4H-imidazol[1,5-a][1,4]benzodiazepine (midazolam, Ro 21-3981, Dormicum) as maleate or 7-chloro-1,3-dihydro-1-methyl-5-phenyl-(2H)-1,4-benzodiazepin-2-one (diazepam) has not previously been reported. We induced anesthesia in 30 patients, free of ophthalmologic disease and in good general health, with either midazolam maleate, diazepam or 5-ethyl-5-(1-methylbutyl)-2-thiobarbituric acid (thiopental). Ten patients were treated with each agent for induction...

This study summarizes our results with various ataralgesic combinations and their effects on circulation and respiration. Together with the new water-soluble 8-chloro-6-(2-fluorophenyl)-1-methyl-4H-imidazo[1,5-a][1,4]benzodiazepine midazolam, Ro 21-3981, Dormicum), 7-chloro-1,3-dihydro-1-methyl-5-phenyl-(2H)1,4-benzodiazepin-2-one (diazepam) and 5-(o-fluorophenyl)-1,3-dihydro-1-methyl-7-nitro-2H-1,4-benzodiazepin-2-one (flunitrazepam) are also considered, for the purpose of comparison. Pharmacokinetic studies confirm the clearly shorter duration of action of midazolam...

In 43 patients electively scheduled for myocardial revascularization surgery, a hemodynamic comparison of 8-chloro-6-(2-fluorophenyl)-1-methyl-4H-imidazo[1,5-a][1,4] benzodiazepine (midazolam, Ro 21-3981, Dormicum) and 7-chloro-1,3-dihydro-1-methyl-5-phenyl-(2H)1,4-benzodiazepin-2-one (diazepam) was made during cardiopulmonary bypass. Midazolam and diazepam were compared in patients with ischemic heart disease to determine the effects of the drugs on systemic vascular resistance at constant flow (cardiac output) and temperature...

8-Chloro-6-(2-fluorophenyl)-1-methyl-4H-imidazol[1,5-a][1,4]benzodiazepine (midazolam maleate, Ro 21-3981, Dormicum) or thiopental were administered to 99 women undergoing short gynecological surgical procedures for induction and maintenance of anesthesia along with 67% nitrous oxide. Either fentanyl 1.5 microgram kg-1 or a saline placebo were given i.v. as acute premedication 5 min before induction. We measured the quality of induction and maintenance. Induction was more rapid after thiopental but thiopental produced more apnea especially when combined with fentanyl...

Diazepam is widely used as a sedative for loco-regional anesthesia. The venous irritation and long duration of action and hangover may be a drawback. We compared 8-chloro-6-(2-fluorophenyl)-1-methyl-4H-imidazo[1,5-a] [1,4]benzodiazepine (midazolam, Ro 21-3981, Dormicum), a new water-soluble benzodiazepine, with diazepam for cardio-respiratory changes, onset time, duration of action, amnesia and venous irritation after a single i.v. shot in loco-regional anesthesia.

8-Chloro-6-(2-fluorophenyl)-1-methyl-4H-imidazo[1,5-a] [1,4]benzodiazepine (midazolam Ro 21-3981, Dormicum) has a number of useful properties--including good tolerance on i.v. injection, and short duration of action--which make it a valuable substance in anesthesiology. The present study deals in particular with the general, coronary and cerebral hemodynamics. Observed hemodynamic effects lasted no more than 10 min, which renders midazolam a drug of good controllability.

8-Chloro-6-(2-fluorophenyl)-1-methyl-4H-imidazo[1,5-a] [1,4]benzodiazepine (midazolam, Ro 21-3981, Dormicum) is a new benzodiazepine which, when compared with its predecessors diazepam (Valium) and flunitrazepam (Rohypnol), has several outstanding advantages: We conducted hemodynamic investigations with 0.15 mg/kg b.w. midazolam in a total of 28 coronary patients divided into 3 groups. The new water-soluble benzodiazepine is at the dose given useful in the induction of and as an adjuvant to anesthesia because of its hemodynamic effect...

Our investigations have shown the following: 1. 8-Chloro-6-(2-fluorophenyl)-1-methyl-4H-imidazo[1,5-a] [1,4]benzodiazepine (midazolam, Ro 21-3981, Dormicum) produces no adverse haemodynamic changes in healthy subjects. 2. The reduction in peripheral resistance becomes apparent mainly in the case of raised baseline values, as, for example, in hypertensive subjects, but it can also be of significance prior to anaesthesia, when there may be raised systemic vascular resistance due to stress. 3. Venous pooling, which leads to a decrease in pre-load and subsequent lowering of the cardiac index, can have a compensatory effect in cardiac insufficiency...

After oral dosing of 10 mg 8-chloro-6-(2-fluorophenyl)-1-methyl-4H-imidazo[1,5-a][1,4] benzodiazepine (midazolam, Ro 21-3981, Dormicum) labelled with 14C (25 microCi) to 4 human volunteers, the total radioactivity is mainly excreted via the kidneys. Nearly 90% are excreted within 24 h. Main urinary metabolite is the conjugated 1-hydroxymethyl derivative, which amounts to 60-70% of the administered dose within 24 h. Compared to total radioactivity, levels of unchanged drug in plasma are rather low and differ from one subject to the next...

A HPLC (high performance liquid chromatography) method for the determination of 8-chloro-6-(2-fluorophenyl)-1-methyl-4H-imidazo[1,5-a] [1,4]benzodiazepine (midazolam, Ro 21-3981, Dormicum) and its hydroxy metabolites has been developed. The half-life of elimination of midazolam and the glucuronides of the metabolites 1-hydroxymethyl-midazolam, 4-hydroxy-midazolam and 1-hydroxymethyl-4-hydroxy-midazolam are identical, 53 min in dogs and 90 min in man.

8-Chloro-6-(2-fluorophenyl)-1-methyl-4H-imidazo[1,5-a] [1,4] benzodiazepine (midazolam, Ro 21-3981, Dormicum) is a special type of benzodiazepine. Its salts are water-soluble and also stable in an aqueous solution. Following i.v. injection of the substance, the human body eliminates midazolam almost entirely by means of biotransformation. Following rapid i.v. injection of midazolam into 8 normal volunteers, the plasma concentration of the substance decreases to approximately 10% within 1 h owing to a rapid rate of distribution...

Midazolam (Ro 21-3981; Dormicum ) is a new water-soluble benzodiazepine. Compared with diazepam and flunitrazepam, it has the advantage of a short half-life and good tolerability after intravenous administration. It induces light sleep 1/2 to 2 min after injection, and anterograde amnesia. It has minimal hemodynamic and respiratory effects. We administered midazolam by intravenous injection in a dose of 3-7 mg to 100 patients about to undergo esophago-, gastro-, or duodenoscopy. The patient became quiet and relaxed, falling into a light sleep but remaining capable of following simple instructions...

The hypnotic action and residual effects of a single bedtime dose of 8-chloro-6(2-fluorophenyl)-1-methyl-4H-imidazo[1,5-a][1,4]benzodiazepine (midazolam, Ro 21-3981, Dormicum) (7.5 or 15 mg) or 8-chloro-6(o-chlorophenyl)-1-methyl-4H-S-triazolo[4,3-a] [1,4]benzodiazepine (triazolam) (0.25 or 0.5 mg) were investigated in young, healthy adults. Motor activity was continuously recorded by a wrist-worn activity monitor. In comparison to placebo, all compounds reduced night-time motor activity in the first half, but not in the second half of the night...

The effects of a single dose of 8-chloro-6-(2-fluorophenyl)-1-methyl-4H-imidazo[1,5-a] [1,4]benzodiazepine (midazolam, Ro 21-3981, Dormicum), 15 mg, on both self-evaluated and all-night EEG-recorded sleep parameters were studied in 10 normal young volunteers. All self-evaluated parameters were modified under midazolam compared with placebo: the sleep onset latency was estimated to be shorter, the sleep duration longer, the sleep quality better. Furthermore, the feeling on awakening in the morning was rated better after midazolam...

In a double-blind parallel study performed in 40 hospitalized patients, suffering from mild to moderate insomnia, the efficacy and tolerance of 15 mg of 8-chloro-6-(2-fluorophenyl)-1-methyl-4H-imidazo[1,5-a][1,4]benzodiazepine (midazolam, Ro 21-3981, Dormicum) administered p.o. were compared with those of 7-chloro-1,3-dihydro-3-hydroxy-5-phenyl-2H-1,4-benzodiazepin-2-one (oxazepam) in the same dosage. The results show comparable values for the two drugs but with significantly better results for midazolam in the parameters: time taken to fall asleep and number of nocturnal awakenings...

Efficacy (sleep--sedation) and tolerance of 8-chloro-6-(2-fluorophenyl)-1-methyl-4H-imidazo[1,5-a][1,4]benzodiazepine (midazolam, Ro 21-3981, Dormicum) in a dosage of 10 mg to 30 mg p.o. were evaluated in a multi-center pilot study in 75 hospitalized patients, with an age range of 20 to 80 years. The patients suffered from mild to moderate insomnia, secondary to musculoskeletal disorders, peripheral nerve diseases and allergies. The optimal dose range was established on the basis of the relation between the degree of insomnia, age of the patients and the dose needed to obtain the optimal results for the sleep parameters...