Sedative Hypnotics midazolam

Sedative/Hypnotics Midazolam, triazolam Gl motility agents Cisapride... 

Sedatives/Hypnotics Midazolam, triazolam Because of the required coadministration of tipranavir with ritonavir 200 mg, refer to... 

Nevertheless, the GABAergic properties of benzodiazepines remain their most important clinical application. Over the past 30 years, the most widely used benzodiazepine drug has been diazepam (1.6). It is an anxiolytic, sedative, and muscle relaxant the anxious, depressed person becomes more outgoing and relaxed. There have been many diazepam analogs. Oxazepam (4.177) and lorazepam (4.178) have similar effects. Temazepam (4.179), flunitrazepam (4.180), and flurazepam (4.181) are useful sedative-hypnotics. Clonazepam (4.182) is a clinically useful anticonvulsant. Brotizolam (4.183), a novel benzodiazepine analog, seems to be an effective sedative-hypnotic. Midazolam (4.184) is an imidazolo-benzodiazepine that is water soluble and thus easily injectable. It is a hypnotic sedative with marked amnestic (i.e., memory loss) properties and is used in dentistry, endoscopic procedures, and induction to anesthetics in the elderly and in... 

Sedative -Hypnotics - Midazolam (8) continues to receive substantial support as an effective hypnotic with neither tolerance effects nor rebound insomnia on drug withdrawal. A series of papers has addressed safety and psychomotor performance aspects of this drug. The clinical literature concerning the hypnotic effi-... 

Deep sedation is similar to a light state of general (intravenous) anesthesia involving decreased consciousness from which the patient is not easily aroused. Because deep sedation is often accompanied by a loss of protective reflexes, an inability to maintain a patent airway, and lack of verbal responsiveness to surgical stimuli, this state may be indistinguishable from intravenous anesthesia. Intravenous agents used in deep sedation protocols include the sedative-hypnotics thiopental, methohexital, midazolam, or propofol, the potent opioid analgesics, and ketamine. 

Diazepam, lorazepam, and midazolam are used in anesthetic procedures. The primary indication is for premedication because of their sedative and amnestic properties. (The basic pharmacology of benzodiazepines is discussed in Chapter 22 Sedative-Hypnotic Drugs.) Diazepam and lorazepam are not water-soluble, and their intravenous use necessitates nonaqueous vehicles, which may cause local irritation. Midazolam formulations are water-soluble and thus produce less irritation, but the drug becomes lipid-soluble at physiologic pH and readily crosses the blood-brain barrier. 

Finally the scaffold behind one of the most famous class of drugs the benzodiazepines, such as diazepam (Vilium), and the other sedatives, hypnotics, and anticonvulsants flunitrazepam, midazolam, lorazepam, etc. 

Anesthesia At high doses loss of consciousness may occur, with amnesia and suppression of reflexes. Anterograde amnesia is more likely with benzodiazepines than with other sedative-hypnotics. Anesthesia can be produced by most barbiturates (eg, thiopental) and certain benzodiazepines (eg, midazolam). 

Other uses Thiopental is commonly used for the induction of anesthesia, and certain benzodiazepines (eg, diazepam, midazolam) are used as components of anesthesia protocols. Special uses include the management of seizure disorders (eg, clonazepam, phenobarbital) and muscle spasticity (diazepam). Longer-acting dmgs (eg, chlordiazepoxide, diazepam) are used in the management of withdrawal states in persons physiologically dependent on ethanol and other sedative-hypnotics. 

Intravenous sedatives and nonopioid hypnotics (midazolam, propofol, etomidate, ketamine, dexmedetomidine) undergo mainly hepatic biotransformation to inactive metabolites. Their prolonged excretion owing to renal insufficiency is clinically not relevant. Nevertheless, in patients with renal failure a... 

Administration of oral azoles with midazolam or triazolam has resulted in elevated plasma concentrations and may potentiate and prolong hypnotic and sedative effects of these agents. Administration with HMG-CoA reductase inhibitors has been shown to cause a significant risk of rhabdomyolysis. Therefore, administration of the oral azoles with midazolam, triazolam, or HMG-CoA inhibitors is contraindicated. 

T effects OF amiodarone, astemizole, atorvastadn, barbiturates, bepridil, bupropion, cerivastatin, cisapride, clorazepate, clozapine, clarithromycin, desipramine, diazepam, encainide, ergot alkaloids, estazolam, flecainide, flurazepam, indinavir, ketoconazole, lovastatin, meperidine, midazolam, nelfinavir, phenytoin, pimozide, piroxicam, propafenone, propoxyphene, quinidine, rifabutin, saquinavir, sildenafil, simvastatin, SSRIs, TCAs, terfenadine, triazolam, troleandomycin, zolpidem X effects W/ barbiturates, carbamazepine, phenytoin, rifabutin, rifampin, St. John s wort, tobacco X effects OF didanosine, hypnotics, methadone, OCPs, sedatives, theophylline, warfarin EMS T Effects of amiodarone, diazepam, midazolam and BBs, may need X- doses concurrent use of Viagra-type drugs can lead to hypotension X- effects of warfarin concurrent EtOH use can T adverse effects T glucose ODs May cause an extension of adverse SEs symptomatic and supportive Rivasrigmine (Exelon) [Cholinesterase Inhibitor/Anri ... 

Many benzodiazepines have potent hypnotic activity and are useful in the treatment of insomnia. Examples include flurazepam (Dalmane, A.93), midazolam (Versed, A.94), temazepam (Restoril, A.95), and triazolam (Halcion, A.96) (Figure A.28). Flunitrazepam (Rohypnol, A.97) is a particularly notorious sedative. Often called roofie or the date rape drug, flunitrazepam causes sedation and amnesia. Because of flunitrazepam s tendency to be abused, almost all nations tightly regulate the drug s availability. 

Clinically important, potentially hazardous interactions with alcohol, anticholinergics, barbiturates, benzodiazepines, butabarbital, chloral hydrate, chlordiazepoxide, chlorpromazine, clonazepam, clorazepate, diazepam, ethchlorvynol, fluphenazine, flurazepam, hypnotics, lorazepam, MAO inhibitors, mephobarbital, mesoridazine, midazolam, narcotics, oxazepam, pentobarbital, phenobarbital, phenothiazines, phenylbutazone, primidone, prochlorperazine, promethazine, quazepam, secobarbital, sedatives, temazepam, thioridazine, tranquilizers, trifluoperazine, zolpidem... 

Loprazolam mesylate is a potent hypnotic/sedative belonging to the second generation of annulated-1,4-benzodiazepines. The of loprazolam ( 6 hr.) is longer than those of triazolam and midazolam, but shorter than the "effective" TJs of flurazepam. 

Twenty patients undergoing surgery were given repeated 1-mg intravenous doses of midazolam as induction anaesthesia every 30 seconds until they failed to respond to three repeated commands to squeeze the anaesthetist s hand. This was considered as the induction end-point titrated dose. It was found that the 10 who had been given prior spinal anaesthesia with tetracaine 12 mg needed only half the dose of midazolam (7.6 mg) than the 10 other patients who had not received tetracaine (14.7 mg). The reasons are not known. The authors of this report simply advise care in this situation. In another study in which patients were given intravenous midazolam following an intramuscular injection of either bupivacaine, lidocaine or saline, it was found that both anaesthetics enhanced the effect of midazolam. This effect was dose-dependent and it was concluded that the use of lidocaine or bupivacaine for regional blocks or local infiltration could alter the effect of midazolam from sedative to hypnotic. ... 

Fluconazole, itraconazole and ketoconazole very markedly increase the serum levels of midazolam and triazolam, thereby increasing and prolonging their sedative and amnesic effects. Similar but smaller effects are seen with itraconazole or ketoconazole and alprazolam and with itraconazole and brotizolam. Even less effect is seen with etizolam and itraconazole and no important interaction occurs between estazolam and itraconazole. Small effects are found with the non-benzodiazepine hypnotic, zolpidem, with ketoconazole and even less effects with zopiclone and itraconazole. 

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