Midazolam effect

Ghoneim MM, Block RI, Dhanaraj VJ. Interaction of a subanaesthetic concentration of isoflurane with midazolam effects on responsiveness, learning and memory. Br J Anaesth 1998 80(5) 581-7. 

An in vitro study in which midazolam was added to serum found that the free fraction of midazolam in the serum from valproate-treated epileptic patients was almost double that found in serum from untreated healthy subjects. It was suggested that displacement of midazolam by valproate could result in an increase in midazolam effects. . dwima/ studies suggest that pre-treatment with valproate may increase the levels of midazolam in the brain. ... 

Mhttila MJ, Vainio P, Vanakoski I Fluconaa)le moderately increases midazolam effects on performance. BrJ Clin Pharmacol (1995) 39,567P. 

Midazolam and diazepam decrease arterial pressure without a change ia heart rate. Like thiopeatoae, midazolam is a respiratory depressant. Advantages of midazolam are its amnestic effect, coupled with less postoperative depression (102). A reversal agent for the benzodiazepiaes has also become available. Flumazenil [78755-81-4] C25H24FN2O2, (5) displaces the beazodiazepiaes from their receptor but has Httie demoastrable activity of its owa (103,104). 

Ator NA Relation between discriminative and reinforcing effects of midazolam, pentobarbital, chlordiazepoxide, Zolpidem, and imidazenil in baboons. Psychopharmacology (Berl) 163 477 87, 2002... 

Midazolam Midazolam is water-soluble and can be administered intravenously, intramuscularly,13 buccally,14,15 and nasally.16,17 At physiologic pH, it becomes more lipophilic and can diffuse into the CNS. Compared to diazepam and lorazepam, it has fewer effects on the respiratory and cardiovascular systems. Its short half-life requires that it be re-dosed... 

Murai, T., Koshikawa, N., Kanayama, T., Takada, K., Tomiyama, K., and Kobayashi, M., Opposite effects of midazolam and beta-carboline-3-carboxylate ethyl ester on the release of dopamine from rat nucleus accumbens measured by in vivo microdialysis, Eur. J. Pharmacol., 261, 65, 1994. 

Thompson JM, Neave N, Moss MC, Scholey AB, Wesnes K and Girdler NM (1999). Cognitive properties of sedation agents Comparison of the effects of nitrous oxide and midazolam on memory and mood. British Dental Journal, 187, 557-562. 

The midazolam example shows that gut wall cytochrome P450 can contribute significantly to the attenuation of oral bioavailability of substrate drugs. In addition, the variability and site dependence of expression of the major intestinal CYPs can lead to significant effects on the disposition of orally delivered drugs. 

Fig. 18.6. Midazolam administration with and without grapefruit juice (CFJ) treatment [41]. Midazolam (15 mg tablet) was administered to eight male subjects (average body weight 82 kg) before and after consumption of two glasses (200 mL each) of CFJ, 1 h before drug administration. QMPRPIus was used to estimate human effective permeability (12 x 10 4 cm s 1), pure aqueous water...

A benzodiazepine (BZ) should be administered as soon as possible if the patient is actively seizing. Generally one or two IV doses will stop seizures within 2 to 3 minutes. Diazepam, lorazepam, and midazolam are equally effective. If seizures have stopped, a longer-acting anticonvulsant should be given. 

McGregor, I. S., Hargreaves, G. A., Apfelbach, R. and Hunt, G.E. (2004) Neural correlates of cat odor-induced anxiety in rats region-specific effects of the benzodiazepine midazolam. J. Neurosci. 24, 4134-44. 

Figure 2.8 Effective permeability coefficients (Peff) (xlO-6) of verapamil calculated from appearance in venous blood (P 00 ) and disappearance from lumen (Peff) in the presence and absence of PSC833, midazolam, or ketoconazole in the vascularly perfused intestinal.

Lancel M, Cronlein TA, Faulhaber J. (1996). Role of GABAA receptors in sleep regulation. Differential effects of muscimol and midazolam on sleep in rats. Neuropsychopharmacoiogy. 15(1) 63-74. 

Stolerman IP, Rauch RJ, Norris EA (1987) Discriminative stimulus effects of a nicotine-midazolam mixture in rats. Psychopharmacology 93 250-256 Stolerman IP, Naylor C, Elmer GI, Goldberg SR (1999) Discrimination and self-administration of nicotine by inbred strains of mice. Psychopharmacology 141 297-306 Stolerman IP, Childs E, Hahn B, Morley A (2002) Drag trace discrimination with nicotine and morphine in rats. Behav Pharmacol 13 49-58... 

A complication of this can be additional first-pass effects caused by metabolism by the gastrointestinal tract itself In the most extreme cases, such as midazolam, extraction by the gut wall may be as high as 0.38 to 0.54 and comparable to that of the liver itself [9]. 

Midazolam is a rapidly metabolized benzodiazepine (p. 228) that is used for induction of anesthesia. The longer-acting lorazepam is preferred as adjunct anesthetic in prolonged cardiac surgery with cardiopulmonary bypass its am-nesiogenic effect is pronounced. 

The synthesis of these compounds will be described in Section 3.1, Opioid analgesics. Besides opioids, benzodiazepines (diazepam, lorazepam, and midazolam), which have anxiolytic, sedative, and anticonvulsant effects, that cause amnesia and muscle relaxation, are frequently used to relieve patients anxiety during anesthesia. 

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