Short-acting derivatives

The benzodiazepine hypnotics midazolam, triazolam, and brotizolam, together with zopiclone, eszopiclone, zolpidem, and zaleplon are short-acting derivatives. The benzodiazepines flunitrazepam and temazepam are intermediate-acting hypnotics,... 

Barbiturates are absorbed orally and distributed widely throughout the body. All barbiturates redistribute in the body from the brain to the splanchnic areas, to skeletal muscle, and finally to adipose tissue. This movement is important in causing the short duration of action of thiopental and similar short-acting derivatives (see p. 115). Barbiturates are metabolized in the liver, and inactive metabolites are excreted in the urine. 

The number of cases of sulfonamide hepatitis published annually fell markedly after 1947, with the introduction of the newer short-acting derivatives (106). 

The synthesis of benzo[Z>]furan derivatives has become a very active field because these molecules have been recently identified as having a variety of biological activities. For example, they can function as inhibitors of protein tyrosine phosphatase IB with antihyperglycemic properties <00JMC1293>, as well as potent and short-acting p-blockers in the treatment of various cardiovascular diseases . An inexpensive, reusable clay has been utilized to catalyze a facile cyclodehydration under microwave without solvent to form 3-substituted benzo[2>]furans from substituted a-phenoxy acetophenones 104. One of the important features of this procedure is that all the selected cyclodehydration reactions are complete in less than 10 minutes <00SL1273>. 

Hydrocortisone is a relatively short-acting agent. For replacement therapy in adrenal insufficiency it is administered orally and in combination with fludrocortisone. Hydrocortisone sodium succinate is a water-soluble derivative which can be used parenter-ally in emergencies such as acute bronchospasm and hypersensitivity reactions like anaphylactic shock. 

It is an oily liquid eugenol derivative and less potent than thiopentone. It is a very short acting intravenous anaesthetic and specially used for very short outpatient operations and dental procedures. 

Janssens, F., Torremans, J., Janssen, P.A.J. Synthetic 1,4-disubstituted 1,4-dihydro-5H-tetrazol-5-one derivatives offentanyl alfentanil (R 39209), a potent, extremely short-acting narcotic analgesic, J. Med. Chem. 1986, 29, 2290-2297. 

Presently available hypnotic drugs for the treatment of transient, short-term, or chronic insomnia differ significantly in pharmacokinetic properties, including elimination half-life and presence of active metabolites. On the other hand, they have in common short absorption and distribution times. As a result, in most circumstances they induce sleep rapidly. According to their elimination half-life, hypnotics can be divided into short-, intermediate-, or long-acting derivatives. 

For the past 40 and more years, a modified form of ECT has been standard, involving sedation with a short-acting barbiturate, muscle paralysis with a curare derivative or similar drugs that prevent activation of the muscles of the body, and artificial respiration with oxygen. The purpose... 

In large doses, injected intravenously, it would bum and hurt horribly, because it s a salt and because it instantly throws off the chemical balance of the blood with which it comes into contact. It makes all muscles lock up in extreme contraction that would hurt unbearably. It wouldn t get to all muscles when a prisoner is being killed with it, however. Since the heart is a muscle and it pumps the blood -- the minute that massive dose of potassium salt hits the heart, one would be history and that would be as far as it would travel. "In lethal injection, three chemicals are used to kill. First, sodium pentothal (its trade name) or thiopental sodium (its chemical name). Then one minute later they inject pavulon. One minute later the potassium chloride. Pentothal is a short acting barbituric acid (barbiturate used in anaesthesia) and is commonly called "truth serum" as it s used in narcoanalysis. It knocks one out. It s a hypnotic. Pavulon is a curare derivative which locks up the lungs so one can t breathe. 

In utilizing this pharmacologically-aided method, many previously therapy-resistant patients could be treated. Psilocybin, as well as its quick-acting derivative, CZ 74 (4-hydroxy-N-diethyltryptamine), distinguishes itself by its unique properties of short duration of effects, mild neurovegetative side effects, few instances of depersonalization or anxiety provocation, as well as a stable and positive influence on the emotional experience (Hofmann 1959 Leuner et al. 1965 Baer 1967). Since it offers a more gentle and direct control of the altered state than LSD, it appears to be a substance of choice for future applications in psychotherapy (Leuner 1968, 1981). 

Tropicamide is an anticholinergic drug that tends to have a greater mydriatic than cycloplegic effect. It is a short-acting atropine-like derivative and has been regarded as an effective and safe mydriatic, used for pupillary dilatation by professionals, who are not always medical doctors. 

Nitric oxide (NO) is a short-acting, potent vasodilator derived from the enzymatic oxidation of arginine. Its production is under control of nitric oxide synthase (NOS). This enzyme is present (expressed) in two forms a constitutive form (ecNOS) and an inducible form (iNOS). Small amounts of NO normally are produced by the vascular endothehum under the control of ecNOS for the physiologic control of vascular tone and blood flow distribution. Under pathophysiologic... 

Ipratropium bromide is a nonselective muscarinic receptor blocker, and blockade of inhibitory muscarinic receptors theoretically could result in an increased release of acetylcholine and overcome the block on the smooth muscle receptors (M3). Oifly the quaternary ammonium derivatives such as ipratropium bromide should be used because they have the advantage of poor absorption across mucosae and the blood-brain barrier. This results in negligible systemic effects with a prolonged local effect (i.e., bronchodilation). In addition, the quaternary compounds do not appear to produce a decrease in mucocfliary clearance. Ipratropium bromide has a duration of action of 4 to 8 hours. Both intensity and duration of action are dose-dependent. Time to reach maximum bronchodilation is considerably slower than from aerosolized short-acting 82-agonists (2 hours versus 30 minutes). However, this is of little clinical consequence because some bronchodilation is seen within 30 seconds, 50% of maximum response occurs within 3 minutes, and 80% of maximum is reached within 30 minutes. Ipratropium bromide is oifly indicated as adjunctive therapy in severe acute asthma not completely responsive to 82-agonists alone because it does not improve outcomes in chronic asthma. ... 

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