Codeine
Other Names
Codein, codeina, codeine, codeinum, 4,5u-epoxy3-
methoxy-17-methyl-7-morphinen-6u-ol, kodein
Substance type: opium alkaloid
In 1832, codeine was isolated from opium, which
has a codeine content of 2 to 30/0 (see Papaver
somniferum). Codeine is also biosynthesized in the
roots of Papaver somniferum 1. cv. Marianne (Tam
et al. 1980). It is possible that trace amounts of
codeine can also be found in other Papaver species
(Papaver bracteatum, Papaver decaisnei; cf. Papaver
spp.) (Theuns et al. 1986). Codeine is also an endogenous
neurotransmitter in humans (cf. morphine).
A dosage of 20 to 50 mg produces "general
mental stimulation, warmth in the head, and an
increase in the pulse rate, as also appear after the
consumption of alcohol" (Rompp 1950*). Codeine
does not appear to be metabolized in the body and
is excreted unchanged.
Because codeine suppresses the urge to cough,
its most important pharmaceutical use is in cough
syrups. The dosage when codeine is used as a
cough suppressant is 50 mg three times a day. A
dosage of 100 to 200 mg results in sleep and
sedation. Higher dosages elicit effects comparable
to those of morphine. The medical literature
contains repeated mentions of "codeine addiction."
Codeine "addicts" are said to ingest up to 2 g
of codeine daily (Rompp 1950, 115*). Today,
codeine is gaining increasing medicinal importance
as a substitution therapy for heroin addicts
(Gerlach and Schneider 1994). The pharmaceutical
industry synthesizes codeine primarily
from thebaine, the main active constituent in Papaver bracteatum Lindl. (cf. Papaver spp.)
(Morton 1977, 125*; Theuns et al. 1986).
Codeine has acquired a certain significance in
the music scene (jazz, rock, psychedelia), primarily
as a substitute for heroin or morphine. Buffy
Saint-Marie sang about the anguish of her codeine
dependence in the song "Cod'ine" (LP It's My Way!
Vanguard Records 1964). Quicksilver Messenger
Service later covered the song and made it famous.
In the 1990s, the wave band Codeine had several
albums out through Sub Pop. Cough syrups496
with a high codeine content were often consumed
as inebriants at concerts, festivals, et cetera
(usually in combination with alcohol and
cannabis) (Bangs 1978, 158).
Commercial Forms and Regulations
Codeine is available as a pure substance and as
codeine hydrochloride, codeine phosphate, and
codeine phosphate hemihydrate. Codeine is on
Schedule III in the United States. Preparations
containing codeine (tinctures, cough syrups, et
cetera) require a special prescription (i.e., with no
refills allowed and/or on special prescription
forms). But in other countries, including France,
Spain, Nepal, and India, a prescription is still
unnecessary and the medicine can be obtained
over the counter from any pharmacy.
Literature
See also the entries for Papaver somniferum,
morphine, and opium alkaloids.
Bangs, Lester. 1978. Ich sah Gott und/oder Tangerine
Dream. Rocksession 2:155-58. Reinbek: Rowohlt.
Esser, Barbara. 1998. Vom Regen in die Traufe: Das
Verbot des Ersatzstoffs Codein ... Focus 26 (6):
58-60.
Gerlach, Ralf, and Wolfgang Schneider. 1994.
Methadon- und Codeinensubstitution:
Erfahrungen, Forschungsergebnisse,
Praxiskonsequenzen. Berlin: VWB.
Tam, W. H. John, Friedrich Constabel, and Wolfgang
G. W. Kurz. 1980. Codeine from cell suspension cultures of Papaver somniferum. Phytochemistry
19:486-87.
Theuns, Hubert G., H. Leo Theuns, and Robert J. J.
Ch. Lousberg. 1986. Search for new natural
sources of morphinians. Economic Botany 40 (4):
485-97.