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At least 19 recordsLinked to original sources
PubMed1975

Plasma concentrations of diazepam and its metabolites after peroral, intramuscular, and rectal administration. Correlation between plasma concentration and sedatory effect of diazepam.

Plasma levels of diazepam, N-demethyldiazepam and free oxazepam were measured gaschromatographically in ten healthy volunteers after 5 mg of diazepam perorally, intramuscularly and rectally (with three different kinds of suppositories). The best absorption of diazepam was found after peroral administration. After an intramuscular injection a delayed absorption with low plasma concentrations of diazepam was found. The basal component of a diazepam suppository seems to have a great effect on the rectal absorption of diazepam. Two of the three different kinds of diazepam suppositories caused higher plasma diazepam concentrations than the intramuscular injection of the drug. There were no great differences in the amount of the metabolites of diazepam after different kinds of administration. The subjective sedatory effect of diazepam lasted approximately as long as the fast distribution of diazepam from plasma took place. A very highly significant correlation between plasma concentration and subjective sedatory effect of diazepam after a single dose was found.

Administration, Oral↗
PubMed1976

Feto-maternal concentrations of diazepam and W-demethyldiazepam after intra-amniotic diazepam injection.

Ten milligrams of diazepam were injected intraamniotically in 8 mothers prior to therapeutic abortion between 12 and 19 weeks. The diazepam concentrations in the maternal plasma were comparable to those found after the same intramuscular diazepam dose to the mother. The concentration of diazepam in the amniotic fluid 12 to 18 hours after the injection was no longer significantly higher than in the maternal plasma. The concentrations of diazepam in the fetal plasma, liver and brain were comparable to the concentrations resulting from a 10 mg intramuscular diazepam dose to the mother about 2 hours before legal abortion. The feto-maternal ratio of diazepam was of same magnitude as after the intramuscular application to the mother. The results indicate that the disappearance of diazepam from the amniotic fluid in this stage of pregnancy occurs extraplacentally, through the mambranes into the uterine circulation. In the treatment of a fetus with drugs having properties similar to diazepam, intra-amniotic administration is no better than intramuscular administration to the mother.

Adolescent↗
PubMed1976

Prolonged recovery after diazepam sedation: the influence of food, charcoal ingestion and injection rate on the effects of intravenous diazepam.

Thirteen subjects received diazepam 0.3 mg/kg i.v. twice with a 2-week interval between the doses. In seven subjects who had eaten at 3 h after the injection, reactive skills in a choice reaction test were impaired significantly (P less than 0.05) and there was a 20% increase in the serum diazepam concentrations at 5 h. When the meal was eaten at 7 h, a 50% increase (P less than 0.01) in the serum diazepam concentration was not associated with a significant impairment in psychomotor skills. In a second group of six subjects charcoal ingestion failed to hasten the clearance of diazepam from serum, and did not affect recovery of co-ordinative skills. In a third group of 12 subjects receiving diazepam 0.15 mg/kg i.v. twice at an interval of 2 weeks, the rapid injection of diazepam resulted in a significantly greater (P less than 0.05) degree of drooping of the upper eyelid and in a greater incidence of amnesia to abdominal pinching. The subjects also experienced more pain in the arm during the faster injection (P less than 0.01). Late effects on psychomotor skills were similar with both rates of injection. The results suggest that the remobilization of diazepam from its storage site after food intake induces a late impairment of psychomotor skills, especially if the food is eaten within less than 5 h after the injection. A rapid i.v. injection of diazepam induces greater sedative and amnesic effects than a slow injection of the same dose, but the slow injection of a greater dose is preferable because of the possibility of thrombophlebitis after rapid injection.

Absorption↗
PubMed1978

Serum diazepam and serum creatine kinase after intra-muscular injection of diazepam in two different vehicles.

Serum diazepam concentration and serum creatine kinase activity (serum CK) were measured in 35 patients (who were divided into three groups (A, B, and C)), over a period of 24 hours after administration of diazepam. An increase in serum CK was regarded as an indication of local muscle injury. In group A, diazepam in a polyethyleneoxydricinolate vehicle was injected intramuscularly; in group B, diazepam in a propyleneglycol-ether alcohol vehicle was injected intramuscularly; and in group C, diazepam was administered orally, combined with intramuscular administration of the vehicle used in group B. The investigation was double-blind and randomized. Serum diazepam absorption expressed as the area under the concentration curve was identical in groups A and C and significantly higher than in group B. Serum CK rose in all groups. The differences among the groups were not significant. There were considerable individual variations in all three groups, and almost half the patients showed no increase in serum CK at all. No negative correlation was found between serum diazepam and serum CK. Thus no effect of muscle injury--if present--on absorption rate could be demonstrated.

Administration, Oral↗
PubMed1978

Plasma concentration of diazepam and N-desmethyldiazepam in children after a single rectal or intramuscular dose of diazepam.

The absorption of diazepam and N-desmethyldiazepam after administration of diazepam solution for parenteral injection per rectum and intramuscularly was studied in 9 children (ages 3--12 years). Rectal administration of diazepam 1 mg/kg led to rapid absorption with plasma levels of 270--320 ng/ml within 5 min, and peak levels of 600--1300 ng/ml 10--60 min after administration. The absorption was comparable to that after intramuscular administration. A second peak in plasma diazepam concentration 6--12 h after dosing was observed in 6 children, which may have been due to mobilization of diazepam from the gastrointestinal mucosa produced by feeding 4 h after administration of the drug. A slowly increasing plasma level of N-desmethyldiazepam was observed during the first 24 h after administration of diazepam.

Child↗
PubMed1976

The cardiovascular effects of diazepam and of diazepam and pancuronium during fentanyl and oxygen anaesthesia.

The cardiovascular effects of diazepam 0.5 and 1.0 mg/kg and diazepam with pancuronium 0.1 mg/kg after fentanyl 0.5 mg/kg were determined in thirteen dogs premedicated with atropine. Fentanyl produced significant reductions in heart rate, cardiac ouptut and arterial blood pressure. Administration of 0.5 mg/kg of diazepam after fentanyl did not significantly alter stroke volume, arterial blood pressure or peripheral vascular resistance but did increase heart rate and cardiac output. Additional diazepam did not further change the heart rate, but did reduce stroke volume, cardiac output, arterial blood pressure and peripheral vascular resistance. Administration of pancuronium after fentanyl and diazepam produced marked elevations in heart rate, cardiac output and arterial blood pressure. There was no difference in mean heart rate and cardiac output when values prior to fentanyl and those obtained three minutes following pancuronium were compared. These data demonstrate that large doses of fentanyl decrease heart rate, cardiac these changes can be partially reversed with diazepam 0.5 mg/kg and completely antagonized with pancuronium 0.1 mg/kg.

Anesthesia, Inhalation↗
PubMed1978

Plasma concentrations of diazepam and desmethyldiazepam during chronic diazepam therapy.

1 Plasma concentrations of diazepam and its metabolite, desmethyldiazepam, have been measured in both in- and out-patient groups treated with diazepam for periods varying between 1 month and 10 years. 2 The diazepam concentration was directly related to the dose of diazepam ingested and inversely related to the age of the patient. 3 A highly significant relationship was obtained between the concentration of desmethyldiazepam and diazepam. 4 The plasma concentrations of both diazepam and its metabolite were independent of sex, duration fo therapy and patient group.

Adult↗
PubMed1977

Urine catecholamine excretion after large doses of fentanyl, fentanyl and diazepam and fentanyl, diazepam and pancuronium.

The effects of fentanyl (0.5 mg/kg iv), fentanyl with diazepam (1 mg/kg iv) and fentanyl, diazepam and pancuronium (0.1 mg/kg iv) on heart rate (HR), mean arterial blood pressure (BP), cardiac output (QT), urine flow rate and urine epinephrine and norepinephrine excretion were determined in nine dogs. Fentanyl did not significantly change QT or BP but did reduce HR and urine flow rate (P less than 0.05). Urine epinephrine and norepinephrine excretion rates were signicantly increased by fentanyl (P less than 0.05). Diazepam caused no significant further changes in QT, BP or HR 30 minutes after administration, but urine epinephrine and norepinephrine excretion rates were reduced to control (pre-fentanyl) levels. Addition of pancuronium after fentanyl and diazepam increased urine flow rate to pre-fentanyl levels and elevated QT, BP and HR above controls but produced no significant change in urine epinephrine or norepinephrine excretion. These data suggest that fentanyl increases catecholamine blood levels and imply that the latter may be one mechanism by which cardiovascular dynamics are maintained stable during fentanyl anaesthesia. Our findings also demonstrate that cardiovascular stimulation after pancuronium is not associated with increased urinary catecholamine excretion.

Animals↗
PubMed1979

Increased specific binding of [3H]diazepam in rat brain following chronic diazepam administration.

Male rats (175 g) were given 30 mg of diazepam in their food daily for 35 days. The animals became drowsy and ataxic from this high dose of drug. After the 35-day dosing, the rats were killed daily, and specific binding of [3H]diazepam and [3H]flunitrazepam was determined in synaptosomal preparations from these and corresponding control rats. On days 3, 4, 6, and 7 after the treatment period the specific binding and specific binding of [3H]diazepam was double that of the control binding and specific binding of [3H]flunitrazepam was 1.67 times that of control. The data indicate that very high doses of diazepam, given for long periods, cause increased specific binding of radiolabeled ligand to brain subfractions. The possible mechanisms and implications are discussed. When lower doses or shorter dosage regimens are used, increased binding is not observed.

Animals↗
PubMed1979

Use of the overturn end point in goldfish to measure the interaction of diazepam and ethanol and the effects of the binding of diazepam to bovine serum albumin.

Over the ranges 2.8 X 10(-5) to 8.78 X 10(-5) M diazepam and 4.85 X 10(-2) to 1.22 X 10(-1) M ethanol, addition of the effects of these agents on the overturn end point in goldfish was observed. The addition of bovine serum albumin (1.56 X 10(-5) M) to aqueous solutions of diazepam modifies the diazepam effect by reducing the "free" drug concentrations.

Animals↗
PubMedDate not supplied

Reversal of central benzodiazepine effects by flumazenil after conscious sedation produced by intravenous diazepam. The Flumazenil in Intravenous Conscious Sedation with Diazepam Multicenter Study Group I.

Flumazenil is a competitive benzodiazepine antagonist that rapidly reverses the residual effects of benzodiazepines following intravenous conscious sedation. In a double-blind, multicenter study, postoperative patients who had been sedated with intravenous diazepam were randomly allocated to receive intravenous doses of flumazenil (0.4 mg to 1 mg) or placebo. Levels of sedation and psychomotor impairment were evaluated prestudy, at baseline, and at 6 intervals from 5 to 180 minutes posttreatment. A global evaluation of effectiveness was made at the 5-minute assessment, and memory was assessed at the 180-minute assessment. Flumazenil (mean dose: 0.73 mg [7.3 ml]) was significantly more effective than placebo (mean dose: 8.9 ml) in reversing sedation, psychomotor impairment, and amnesia within 5 minutes after the start of administration. At the 5-minute posttreatment assessment, 84% of 102 flumazenil-treated patients (compared with 42% of 52 placebo-treated patients) experienced complete reversal of sedation. Ninety-two percent of 93 flumazenil-treated patients (compared with 41% of 46 placebo-treated patients) had normal psychomotor function. Reversal of amnesia at the 5-minute assessment was achieved in 75% of 101 flumazenil-treated patients and in 20% of 51 placebo-treated patients. Statistically significant differences between flumazenil and placebo were also observed at the 15-minute assessment. Thereafter there were no significant differences between the two treatment groups. Most (70%) flumazenil-treated patients exhibited no recurrence of sedation during the 180-minute assessment period. The most frequent adverse reaction in the flumazenil group was dizziness (6%). There were no serious adverse experiences related to the test drug. Flumazenil provided prompt, controlled reversal of residual effects, especially sedation, in the majority (84%) of patients recovering from intravenous conscious sedation induced by diazepam. For most (70%) of these flumazenil-treated patients, the reversal was maintained throughout the 180-minute assessment.

Adolescent↗
PubMedDate not supplied

Reversal of central benzodiazepine effects by flumazenil after intravenous conscious sedation with diazepam and opioids: report of a double-blind multicenter study. The Flumazenil in Intravenous Conscious Sedation with Diazepam Multicenter Study Group II.

The efficacy and safety of a new benzodiazepine antagonist, flumazenil, were assessed in a double-blind multicenter study. Flumazenil (mean dose, 0.76 mg) or placebo (mean dose, 8.9 ml) was administered intravenously to 130 and 67 patients, respectively, who had been given diazepam in conjunction with an opioid (fentanyl, meperidine, or morphine) for the induction and maintenance of intravenous conscious sedation for diagnostic or therapeutic surgical procedures. The group assessable for efficacy comprised 122 patients treated with flumazenil and 64 patients given placebo. After 5 minutes, 80/115 (70%) flumazenil-treated patients, compared with 21/63 (33%) placebo-treated patients, were completely awake and alert, as indicated by a score of 5 on the Observer's Assessment of Alertness/Sedation Scale. Ninety-five percent of patients in each group who attained a score of 5 at the 5-minute assessment showed no loss of alertness throughout the 180-minute assessment period. Flumazenil-treated patients also performed significantly better on the Finger-to-Nose Test and the recall of pictures shown at the 5-minute assessment. Flumazenil was well tolerated, with no serious adverse effects reported. Thirty-nine (30%) of flumazenil-treated patients, compared with 17 (25%) of placebo-treated patients had one or more drug-related adverse experiences. The most common adverse effects were nausea and vomiting in the flumazenil group and nausea and injection-site pain in the placebo group. Flumazenil was found to promptly reverse sedation induced by diazepam in the presence of opioids.

Adolescent↗
PubMed1979

Comparison of recovery tests after intravenous sedation with diazepam-methohexital and diazepam-methohexital and fentanyl.

A model for the assessment of recovery to street fitness from two commonly used techniques for intravenous sedation is described. Well-known psychometric research methods and simple paper-and-pencil tests that could be given by interested clinicians were used. The speed of recovery from diazepam-methohexital, and diazepam-methohexital and fentanyl (with naloxine reversal), did not differ significantly. Psychomotor skills were recovered before both perceptual and cognitive functions. Two simple paper-and-pencil tests easily identified perceptual and cognitive deficits at least three hours postoperatively.

Adult↗