Scopolamine

Hyoscine-Butylbromide (EP)

BUTYLSCOPOLAMINE
Hyoscine-Butylbromide (EP)
One of the earliest alkaloids to be isolated from
plant sources is Scopolamine, which has been in
use since it was isolated by the German scientist
Albert Ladenburg in 1880. The use of various
preparations from its plant-based form is learnt
from the healing arts of some of the world’s oldest
cultures and perhapseven pre-historic times.
In India Ancient Hindu physicians knew of the
antispasmodic effects of a relative of the Duboisia
shrub. In the search for a safe and effective treatment
for abdominal pain and cramp, scientists based
at Ingelheim prepared a semisynthetic derivative
from the extract of elite Duboisia plants grown in
greenhouses. This molecule, Butylscopolamine,

was free of theundesirable side-effects on the
central nervous system, typical of Scopolamine,
and the medication, on sale since 1952, was
immediately recognized as a safe and effective
antispasmodic.
Today, Butylscopolamine, also known as
Scopolamine butylbromide, butylhyoscine or
hyoscine butylbromide, is the world’s leading and
most trusted treatment for pain and discomfort
caused by muscle spasms andcramps. It cannot
be considered an analgesic in the normal sense,
in that it does not ‘mask’ or ‘cover’ the pain, but
rather works to prevent the pain from occurring in
the first place.

Source
Linnea Butylscopolamine is derived from the
leaves of an Australian native tree, known as the
corkwood tree or Duboisia myoporoides belonging
to the Solanaceae family.
Scopolamine butylbromide isobtained from
Scopolamine isolated and purified from dried
Duboisia leaves and stalks harvested on specialized
plantations.

These plantations had initially been established by
the government of Queensland for the extraction
of Scopolamine for use as a surgical anaesthetic
during the Second World War [1]. In the mid-1950s,
the plantations were purchased and managed by
Australian farmers(A), who now use sophisticated
and environmentally-friendly farming methods
that respect the rules of GAP (Good Agricultural
Practice) and ensure full process traceability.

Activity
Butylscopolamine, like its precursor Scopolamine,
has a high affinity for acetylcholine receptors
located on smooth-muscle cells. It blocks the

action of acetylcholine at parasympathetic sites
in smoothmuscle and secretory glands binding
muscarinic and nicotinic receptors [2].

Butylscopolamine decreases the motility of
the gastrointestinal tract and the genitourinary
tract and is useful in the treatment of spasms in
these regions, as may be seen in gastroenteritis,
colitis, inflammatory bowel disease, diverticulitis,
biliary colic, cystitis, ureteric colic and primary
dysmenorrhea. Theinhibitory action on glands
in the oral cavity, gastrointestinal tract, and
respiratory tract causes a reduction in secretion.

intravenous Butylscopolamine was shown to
decrease both the mechanical and electrical
motility index [3,4].

The scientific base of its activity was objectively
demonstrated by a recent study conducted

Since it is only partially absorbed following oraladministration, it remains available at the site of

to investigate its electrical and biomechanical
activity in the stomach. A quantity of 20 mg of

action in the intestine and has a local relaxing/
spasmolytic effect with a low systemic availability.

The addition of the butyl-bromide moiety to
Scopolamine has resulted in a significant
increase in the water solubility of this drug, whicheffectively prevents movement across the bloodbrain barrier with a marked peripheral activity.

Common Applications
Scopolamine butylbromide is a generally safe and
affordable drug with a wide range of applications.
It was originally used as a treatment for nonspecific colicky abdominal pain (in adults and
children) for which it is currently the recommended
symptomatic treatment.
Abdominal...