Barbiturates hypnotic

Hypnotics. Common hypnotics are thiopental, propofol, midazolam, etomidate, ketamine and inhaled anesthetics. The incidence of hypersensitivity reactions with thiopental is rare. Recently, thiopental was involved in less than 1% of allergic reactions in France [9]. Ever since Cremophor EL, used as a solvent for some non-barbiturate hypnotics, has been avoided, many previously reported hypersensitivity reactions have disappeared. In the last French surveys, reactions to propofol accounted for less than 2.5% of allergic reactions, and reactions to midazolam, etomidate or ketamine appear to be really rare [9]. Finally, no immune-mediated immediate hypersensitivity reaction involving isoflurane, desflurane or sevoflurane has been reported despite their wide use. 

Adults. 3 g PO q6h x 4 PRN Supl 1-2 g IM or IV repeat PRN Preeclampsia/pre-mature labor 4 g load then g/h IV inf Cardiac arrest 1-2 g IV push (2-4 mL 50% soln) in 10 mL DjW AMI Load 1-2 g in 50-100 mL D5W, over 5-60 min IV then 0.5-1.0 g/h IV up to 24 h (ECC 2005) Feds. 25-50 mg/kg/dose IM or IV q4-6h for 3-4 doses repeat PRN dose w/ low urine output or renal insuff Caution [B, +] Contra Heart block, renal failure Disp Inj 10, 20, 40, 80, 125, 500 mg/mL bulk powder SE CNS depression, D, flushing, heart block Interactions T CNS depression W/ antidepressants, antipsychotics, anxiolytics, barbiturates, hypnotics, narcotics EtOH T neuromuscular blockade Wf aminoglycosides, atracurium, gallamine, pancuronium, tubocurarine, vecuronium EMS Check for absent patellar reflexes this may indicate tox may cause hypokalemia (flattened T waves) and hypocalcemia OD May cause hypotension, resp arrest, T PR, QRS, and QT interval, AV block, and cardiac arrest calcium salts can be given to reverse resp depression... 

Schedule IV - Drugs have an accepted medical use and are generally the long-acting barbiturates,hypnotics and minor tranquilizers, e.g., meprobamate, phenobarbital. 

Glenn JB (1980) Animal studies of the anesthetic activity of ICI 35868. Br J Anaesth 52 731-742 Goldenthal El (1971) A compilation of LD50 values in newborn and adult animals. Toxicol Appl Pharmacol 18 185-207 Janssen PAJ, Niemegeers CJE, Marsboom RPH (1975) Etomidate, a potent non-barbiturate hypnotic. Intravenous etomidate in mice, rats, guinea pigs, rabbits and dogs. Arch Int Pharmacodyn 214 92-132... 

Clinically important, potentially hazardous interactions with alcohol, barbiturates, hypnotics, narcotic analgesics, sedatives, tranquilizers, tricyclic antidepressants... 

Barbiturates. Based on the finding that some compounds containing a quaternary carbon (sulfonal and amylene) displayed hypnotic properties, in 1903, Emil Fischer and J. von Mehring synthesized 5,5-diethylbarbi-turic acid. This was marketed by Bayer as Veronal in the early 1900s. Since 1903, hundreds of barbiturates have been synthesized, but only a few turned out to be useful. In addition, because of their side effects, the synthesis of non-barbiturate hypnotics has been undertaken. 

Atropine - emergency treatment of hypotension with bradycardia Azathioprine - immunosuppressant cancer chemotherapy, rheumatoid arthritis Baclofen - skeletal muscle relaxant spasticity Barbiturate - hypnotic (little therapeutic use)... 

Butabarbital, a barbiturate hypnotic sedative (15 to 30 mg p.o. t.i.d.), is indicated for causing sedation, and preoperative sedation and treating insomnia. 

A barbiturate with a hydroxy group in the side chain (XXXV) (ipronal) was reported to have tranquiilising activity in a clinical study when given orally for a 2 to 3 week period [182]. Its short-term hypnotic effect was found to be very weak, and it was reported not to be an anticonvulsant. However, it markedly potentiates the hypnotic effect of phenobarbitone and barbitone. This effect is not produced with non-barbiturate hypnotics, such as chloral hydrate or ether. 

The concurrent use of small or moderate amounts of alcohol and therapeutic doses of drugs that are CNS depressants can increase drowsiness and reduce alertness. These drugs include antidepressants, antiemetics, antiepileptics, antihistamines, antipsychotics, anxiolytics, barbiturates, hypnotics, opioid analgesics, skeletal muscle relaxants, and others. This increases the risk of accident when driving or handling other potentially dangerous machinery, and may make the performance of everyday tasks more difficult and hazardous. 

One reviewer briefly mentions that on three or four occasions patients taking an MAOI continued, without the prescriber s knowledge, to take their usual barbiturate hypnotic and thereby ... unknowingly raised their dose of barbiturate by five to ten times, and as a consequence barely managed to stagger through the day. No details are given, so it is not known whether the serum barbiturate levels of these patients were measured, or whether the raised levels are only a surmise. 

Storage Store in cool, dry place away from ignition sources keep tightly closed Uses Chem. intermediate in mfg. of pharmaceuticals, diuretics, barbiturates, hypnotics, varnishes, polymers, epichlorohydrin, epoxy resins, adhesives, plastics, glyceryol, insecticides synthesis of allyl compds. alkylating agent formerly as chem. intermediate for allyl starch Regulatory HAP SARA 313 reportable Calif. 

The Identification of Non-Barbiturate Hypnotics from Biological Specimens J. Chromatogr. Sci. 12(5) 237-245 (1974) CA 81 115339g... 

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