Central stimulants

Therapeutic Function Central stimulant Chemical Name (S)-a-methylbenzeneethanamine sulfate Common Name d-j3-phenylisopropylamine sulfate Structural Formula... 

Therapeutic Function Central stimulant antihypotensive Chemical Name 2-Diphenylmethylenebutylamine Common Name —... 

In contrast to the nicotinic antagonists and indeed both nicotinic and muscarinic agonists, there are a number of muscarinic antagonists, like atropine, hyoscine (scopolamine) and benztropine, that readily cross the blood-brain barrier to produce central effects. Somewhat surprisingly, atropine is a central stimulant while hyoscine is sedative, as least in reasonable doses. This would be the expected effect of a drug that is blocking the excitatory effects of ACh on neurons but since the stimulant action of atropine can be reversed by an anticholinesterase it is still presumed to involve ACh in some way. Generally these compounds are effective in the control of motion but not other forms of sickness (especially hyoscine), tend to impair memory (Chapter 18) and reduce some of the symptoms of Parkinsonism (Chapter 15). 

Hemmi, T. How we handled the problem of drug abuse in Japan. In Sjogvist, F., and Lottie, M., eds. Abuse of Central Stimulants. 

Post, R.M. Central stimulants. Clinical and experimental evidence on tolerance and sensitization. In Israel, Y. Glaser, F.B. Kalant, H. Popham, R.E. Schmidt, W. and Smart, R.G., eds. Research Advances in Alcohol and Drug Problems. Vol. 6. New York Plenum, 1981. pp. 1-65. 

Two current foci in pain management are to identify the mechanisms that are responsible for pain hypersensitivity and to prevent this initial hypersensitivity. Therefore, the goal of pain therapy is to reduce peripheral sensitization and subsequent central stimulation and amplification associated with wind-up, spread, and central sensitization.17... 

Amphetamine (53) is the prototype drug in this group. One significant objective of molecular manipulation in this group is to retain the appetite depressant activity without significant central stimulation. This is as yet unrealized. Some of the drugs prepared with this purpose in mind are discussed in this section. Reductive alkylation of the nitrogen... 

While the closely related central stimulant pyrova-lerone (193) can also be made simply by reacting the requisite a-haloaralkylketone with pyrrolidine, a... 

Svensson, K. (1986) Thesis Dopamine autoreceptor antagonists A new class of central stimulants. University ofGoteborg, Gdteborg, Sweden, ISBN 91-7900-078-9. Nedelec, L., Guillaume, J. and Dumont, C. (1976) Fr. Patent 76-3933 (1977) Chem. Abstr. 87, 152038. 

Excessive central stimulation, usually exhibited as tremors, insomnia and hyperhidrosis, can occur following therapeutic doses of the MAOIs, as can agitation and hypomanic episodes. Peripheral neuropathy, which is largely restricted to the hydrazine type of MAOI, is rare and has been attributed to a drug-induced p)n idoxine deficiency. Such side effects as dizziness and vertigo (presumably associated with hypotension), headache, inhibition of ejaculation (which is often also a problem with the TCAs), fatigue, dry mouth and constipation have also been reported. These side effects appear to be more frequently associated with phenelzine use. They are not associated with any antimuscarinic properties of the drug but presumably arise from the enhanced peripheral sympathetic activity which the MAOIs... 

Catiline is a known inhibitor of monoamine oxidase and a central stimulant as an indirect sympathomimetic. It is found in anorectic products. 

Many antidepressant drugs have pronounced effects on sleep. Several tricyclic compounds (amitriptyline and others) have sedative actions while others (imipramine and others) are less sedative or even stimulant. Monoamine oxidase inhibitors (MAOIs) have central stimulant effects and may cause insomnia. Specific serotonin reuptake inhibitors (SSRls) and combined serotonin, noradrenaline reuptake inhibitors (SNRIs) can also cause insomnia. 

Gillberg, C., Melander, H., von Knotting, A., Janols, L., Thernlund, G., Heggel, B., Edievall-Walin, L., Gustafsson, P., and Kopp, S. (1997) Long-term central stimulant treatment of children with attention-deficit hyperactivity disorder. A randomized double-blind placebo-controlled trial. Arch Gen Psychiatry 54 857—864. 

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