Nicergoline

Nicergoline (INN, marketed

under the trade name Sermion)
is an ergot derivative used to
treat senile dementia and other
disorders with vascular origins.
It decreases vascular
resistance and increases
arterial blood flow in the brain,
improving the utilization of
oxygen and glucose by brain
cells. It has similar vasoactive
properties in other areas of the
body, particularly the lungs.
Unlike many other ergolines,
such as ergotamine, nicergoline
is not associated with fibrosis
[1]
Nicergoline

Clinical data
AHFS/Drugs.com International
Drug Names
Pregnancy Not
category
recommended
Routes of Oral, IM, IV
administration
ATC code C04AE02 (WHO )

Legal status
Legal status In general: Over-
the-counter (OTC)

Pharmacokinetic data
It is used for vascular disorders
such as cerebral thrombosis
and atherosclerosis, arterial
blockages in the limbs,
Raynaud's disease, vascular
migraines, and retinopathy.

Nicergoline has been registered

in over fifty countries and has
been used for more than three
decades for the treatment of
cognitive, affective, and
behavioral disorders of older
people.[2]

Clinical uses
Nicerogline is used in the
following cases:

Acute and chronic cerebral

metabolic-vascular disorders
(cerebral arteriosclerosis,
thrombosis and cerebral
embolism, transitory cerebral
ischaemia). Acute and
chronic peripheral metabolic-
vascular disorders (organic
and functional arteriopathies
of the limbs), Raynaud’s
disease and other syndromes
caused by altered peripheral
irrigation.
 Migraines of vascular origin
Coadjutant therapy in clinical
situations accompanied by
platelet hyper-aggregability,
arterial tension.
Corio-retinal vascular
disorders: diabetic
retinopathy, macular
degeneration and retinal
angiosclerosis
Oto-vestibular problems of a
vascular nature: dizziness,
auditory hallucinations,
hypoacusis.

Dosages for known conditions

are usually administered at
5–10 mg three times a day,
however anti-aging preventative
purposes may want to consider
5 mg once or twice a day more
adequate.[3]

Contraindications
Persons suffering from acute
bleeding, myocardial infarction
(heart conditions),
hypertension, bradycardia or
using alpha or beta receptor
agonists should consult with
their physician before use.
Although toxicology studies
have not shown nicergoline to
have any teratogenic effect, the
use of this medicine during
pregnancy should be limited to
those cases where it is
absolutely necessary.

On 28 June 2013 the European

Medicines Agency
recommended restricting the
use of medicines containing
ergot derivatives, including
nicergoline. They stated that
"these medicines should no
longer be used to treat several
conditions involving blood
circulation problems or
problems with memory and
sensation, or to prevent
migraine headaches, since the
risks are greater than the
benefits in these indications.
This is based on a review of
data showing an increased risk
of fibrosis (formation of excess
connective tissue that can
damage organs and body
structures) and ergotism
(symptoms of ergot poisoning,
such as spasms and
obstructed blood circulation)
with these medicines."[4]
However, only a subset of
ergolines are associated with
fibrosis and evidence suggests
that nicergoline does not carry
fibrotic risk like other ergoline
derivatives such as
ergotamine.[1]

Nicergoline is considered
unsafe in porphyria.[5]

Adverse e�ects
The side effects of nicergoline
are usually limited to nausea,
hot flushes, mild gastric upset,
hypotension and dizziness.[5] At
high dosages bradycardia,
increased appetite, agitation,
diarrhea and perspiration have
been known to occur. A single
case of acute interstitial
nephritis has been reported.[6]

Interactions
Nicergoline is known to
enhance the cardiac depressive
effects of propranolol.[5] At high
dosages, it is advisable to seek
one’s physician's guidance if
combining with potent
vasodilators such as
bromocriptine, Ginkgo biloba,
picamilon, vinpocetine or
xantinol nicotinate.

Mechanism of action
Nicergoline is an ergot alkaloid
derivative that acts as a potent
and selective alpha-1A
adrenergic receptor
antagonist.[7] The IC50 of
nicergoline in vitro has been
reported to be 0.2 nM.[8] The
primary action of nicergoline is
to increase arterial blood flow
by vasodilation. Furthermore, it
is known that nicergoline
inhibits platelet aggregation.
Studies have shown that
nicergoline also increases
nerve growth factor in the aged
brain.[9][10]

References
1. Zajdel, P; Bednarski, M; Sapa,
J; Nowak, G (2015). "Ergotamine
and nicergoline - facts and
myths". Pharmacological
Reports. 67 (2): 360–3.
doi:10.1016/j.pharep.2014.10.0
10 . PMID 25712664 .
2. Fioravanti M, Flicker L (2001).
"Efficacy of nicergoline in
dementia and other age
associated forms of cognitive
impairment". Cochrane
Database Syst Rev (4):
CD003159.
doi:10.1002/14651858.CD0031
59 . PMID 11687175 .
3. Nicergoline drug insert,
Pharmacia & Upjohn, October
2000
4. European Medicines Agency
(28 June 2013), "New
restrictions on use of medicines
containing ergot derivatives",
Press Release
5. Sweetman SC, ed. (2009).
"Supplementary drugs and other
substances". Martindale: The
complete drug reference (36th
ed.). London: Pharmaceutical
Press. p. 2352.
ISBN 978-0-85369-840-1.
6. Kim MJ, Chang JH, Lee SK, et
al. (2002). "Acute interstitial
nephritis due to nicergoline
(Sermion)". Nephron. 92 (3):
676–9.
doi:10.1159/000064096 .
PMID 12372954 .
7. Alvarez-Guerra M, Bertholom
N, Garay RP (1999). "Selective
blockade by nicergoline of
vascular responses elicited by
stimulation of alpha 1A-
adrenoceptor subtype in the rat".
Fundam Clin Pharmacol. 13 (1):
50–8.
doi:10.1111/j.1472-8206.1999.t
b00320.x . PMID 10027088 .
8. Moretti A, Carfagna N, Caccia
C, Carpentieri M (1988). "Effect
of ergolines on neurotransmitter
systems in the rat brain". Arch
Int Pharmacodyn Ther. 294:
33–45. PMID 2906797 .
9. Nishio T, Sunohara N,
Furukawa S, Akiguchi I, Kudo Y
(1998). "Repeated injections of
nicergoline increase the nerve
growth factor level in the aged
rat brain and production of brain-
derived neurotrophic factor by
activeted astrocytes". The
Japanese Journal of
Pharmacology. 76 (3): 321–323.
PMID 9593228 .
10. Mizuno T, Kuno R, Nitta A,
Nabeshima T, Zhang G,
Kawanokuchi J, Wang J, Jin S,
Takeuchi H, Suzumura A (2005).
"Protective effects of nicergoline
against neuronal cell death
induced by activated microglia
and astrocytes". Brain Research.
1066 (1–2): 78–85.
doi:10.1016/j.brainres.2005.10.
050 . PMID 16325157 .

External links
National Electronic Library
for Medicines Nicergoline
for dementia and other age
associated forms of
 cognitive impairment.

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