Analeptics 1
Analeptics
Alfred Hofmeister, Chemische Werke Minden GmbH, Minden/Westphalia, Federal Republic of Germany
Analeptics are pharmaceuticals for treatment
of depressed excitability of the central nervous
system. They comprise a varied group of sub-
stances, whose use in medicine is decreasing
in importance continually. This fact can be ex-
plained by the increasing awareness that analep-
tics, as far as they are used as psychostimulants
(e.g., amphetamines), frequently lead to abuse
and drug dependence. Therefore, these drugs are
controlled by narcotics laws, or they have been
withdrawn completely from the market. How-
ever, this has not prevented their extensive use
on the drug scene.
Analeptics have only one indication, namely,
acute intoxication, such as hypnotic poisoning
or postnarcotic complications with lesion of the
respiratory and circulatory centers. For these
cases, the following preparations are still avail-
able:
Bemegride [64-65-3], 4-ethyl-4-methyl-2,6-
piperidinedione, C8 H13 NO2 , M r 155.19, mp
127 ◦ C. Trade names: Mikedimide (Panray), Eu-
kraton (Nordmark), Malysol (Arco, Switzer-
land), Megimide (Nicholas). Bemegride is used
in place of picrotoxin in acute poisoning with
hypnotics.
Crotetamide [6168-76-9], N-(1-di-
methylcarbamoylpropyl)-N-ethylcrotonamide,
C12 H22 N2 O2 , M r 226.31, bp 132 – 134 ◦ C
(30 Pa). Trade name (in combination with cro-
propamide [633-47-6]): Micoren (Ciba-Geigy).
Fominoben hydrochloride [18053-31-1],
3 -chloro-α-[methyl[(morpholinocarbonyl)-
methyl]-amino]-o-benzotoluidide · HCl,
C21 H25 Cl2 N3 O3 , M r 438.36, mp 206 – 208 ◦ C
(decomp.). Trade name: Noleptan (Thomae),
Oleptan (Bender, Austria), Terion (Lusofar-
maco, Italy).
Amiphenazol hydrochloride [490-55-1], 5-
phenyl-2,4-thiazole diamine · HCl,C9 H10 ClN3 S,
M r 259.78. Trade name: Daptazile (Nicholas).

c 2005 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim
10.1002/14356007.a02 267
Crotetamide, fominoben, and amiphenazol
are used especially for treating acute respiratory
disorders. Today the alkaloid lobelin [90-69-7]
is seldom used.
Derivatives of amphetamine, which in fact
are also analeptics, now are used only as appetite
depressants, whereas derivatives of ephedrine
are used mainly in combination drugs as bron-
chospasmolytics. The strongly psychostimulat-
ing drugs, such as methamphetamine hydrochlo-
ride [537-46-2], trade name Pervitin (Temmler),
and methylphenidate hydrochloride [113-45-1],
trade name Ritalin (Ciba), are considered cor-
rectly to be narcotics. Pemolin [2152-34-3],
trade name Tradon (Beiersdorf), is still available
as a mild stimulant.
The stimulating drugs used in psychiatry, for
example, for depressions with retarded activ-
ity, are classified as psycho-active drugs, in par-
ticular, as the so-called thymoleptics. The anti-
hypotonics used for treating low blood pressure
are not classified as analeptics.
The methods available to modern intensive
medicine have made the analeptics, which were
much used previously, largely unnecessary. At-
tempts to deal with widespread misuse – by nar-
cotics laws, obligatory prescriptions, and with-
drawal of some preparations from the market –
have been partially successful.
References
1. D. R. Curtis: “The Pharmacology of Central
and Peripheral Inhibition,” Pharmacol. Rev.
15 (1963) 333 – 364.
2. D. W. Esplin, B. Zablocka-Esplin:
“Mechanism of Action of Convulsants,” in:
H. H. Jasper, A. A. Ward, Jr., A. Pope (ed.):
Basic Mechanism of the Epilepsies, Little,
Brown & Co., Boston 1969, pp. 167 – 183.
3. F. Hahn: “Analeptics”, Pharmacol. Rev. 12
(1960) 446 – 530.