Dihydromorphine
(Paramorfan, DHM, Paramorphan) is a
semi-synthetic opioid invented in
Germany in the first years of the
twentieth century. Structurally, it is
very similar to morphine—the only
difference being the reduction of the
double bond between positions 7 and 8 in
morphine to a single bond.
Dihydromorphine can be made by several
processes, including hydrogenating
morphine or opium or by demethylating
either dihydrocodeine or
tetrahydrothebaine. Dihydromorphine is
available as tablets for oral use,
ampoules of solution for injection by
various routes, suppositories, and
liquids for oral and sublingual use.
Dihydromorphine is slightly stronger
than morphine as an analgesic with a
nearly identical side-effect profile,
and is a somewhat more active euphoriant
-- therefore making it theoretically a
bit superior in alleviating suffering --
and perhaps in a way subjectively closer
to that of morphine than hydromorphone,
other morphine derivatives, the
codeine-based series, or the synthetics.
Like metopon, dihydromorphine may be
less addictive overall and have better
bioavailability after oral
administration than morphine. The onset
of action is more rapid than morphine
and it also tends to have a longer
duration of action, generally 4-7 hours.
Other drugs with faster onset of action
such as nicomorphine and hydromorphone
also tend to burn off more quickly, with
a mean duration of action around 3 hours
in most patients.
Dihydromorphine is most commonly, though
still rarely, used in Europe but has in
fact been used more and in greater
overall quantities in recent decades in
some countries such as the Czech
Republic, Slovakia and others in the
region. In the United States and other
countries, it is most often seen these
days as an intermediate in the
manufacture of dihydrocodeine as well as
in some methods of manufacture of
hydrocodone, hydromorphone, and related
drugs. It is available as the
hydrochloride, hydroiodide, or
monohydrate salt, with the former being
the form almost exclusively used in
pharmaceuticals but the hydroiodide also
used especially in making dihydrocodeine
hydroiodide (Paracodin). Individuals and
organisations are lobbying for the
United States to legalise and approve
dihydromorphine for use alongside other
analgesics. The Usenet newsgroup
alt.politics.usa.legalise-dihydromorphine
is one example, albeit atypical in its
post volume and pattern.
Dihydromorphine was never introduced in
the United States as was the case of
many similar drugs invented in Europe in
the intense search for stronger cough
suppressants, especially to slow the
spread of tuberculosis and other
airborne diseases in the two decades
prior to the First World War such as
thebacon, nicomorphine (Vilan),
benzylmorphine (Peronine),
dihydroisocodeine, dihydrocodeine enol
acetate (Acedicon), acetylmorphone,
diacetylmorphine (Heroin), nicocodeine,
acetyldihydrocodeine, nicodicodeine, and
others. For this reason, in the United
States, dihydromorphine shares a
Schedule I designation with these other
opioids, under the Controlled Substances
Act of 1970. In most other countries,
dihydromorphine is classified at the
same level as morphine, pethidine and
the like where it is available and used;
international law and treaties list it
as a narcotic subject to control, and
other countries' laws may vary. Its role
in the production of dihydrocodeine
makes it the Schedule I substance with
one of the higher annual manufacturing
quotas granted by the US Drug
Enforcement Administration.
One scientific controversy deals with
the relative strength of dihydromorphine;
according to various official sources,
is either 50 per cent or 115-120 per
cent of the analgesic strength of
morphine. Clinical experience points to
the latter. In comparison,
dihydrocodeine is 1˝ times the strength
of codeine but also differs from codeine
in not having a ceiling effect on
analgesia imposed by metabolism -- i.e.,
above a certain point (400 mg in most
people), the codeine is wasted.
Dihydromorphine has a longer duration of
action (6 hours vs 4 hours for
morphine).
Dihydromorphine, often labelled with the
isotopes iodine-129 and tritium, was
amongst tools utilised in the 20th
century research which eventually led to
the theory and discovery of opioid
receptors in the human nervous system.
Other opioids like buprenorphine,
morphine and others are similarly used
for research on the actions of drugs of
this type in various systems of the
body. |