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Amantadine
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Four drugs have been approved to fight the Flu: Amantadine (Symmetrel);
Oseltamivir (Tamiflu); Rimantadine (Flumadine) ; and Zanamivir (Relenza)

Amantadine has the chemical formula C10H17N. It is an anti-viral drug that was
approved in 1976 for treatment of influenza A. Other approved drugs for
influenza are rimantadine, and oseltamivir. All of these medications are
prescription drugs, and a doctor should be consulted before the drugs are
used. When used for prevention, they are about 70% to 90% effective for
preventing illness in healthy adults. If taken within 2 days of getting sick, these
drugs can reduce the symptoms of the flu and shorten the time you are sick by
1 or 2 days. They also can make you less contagious to others. All of these
drugs must be prescribed by a doctor and taken for 5 days. Antiviral drugs are
effective only against influenza viruses. They will not help the symptoms
associated with the common cold or many other flu-like illnesses caused by
viruses that circulate in the winter. All of the antiviral drugs are different in terms
of who can take them, how they are given, any dosing changes based on age
or medical conditions, and side effects. Your doctors will help decide whether
you should get antivirals and which one you should get. For complete text and
more information from CDC see: http://www.cdc.gov/flu/protect/antiviral/

Amantadine (1-aminoadamantane, sold as Symmetrel) is both an antiviral

drug used both as an antiviral and an antiparkinsonic.

Uses

Approved

It was approved by the Food and Drug Administration in 1976 for the treatment
of Influenzavirus A in adults. In 1969 the drug was also discovered by accident
to help reduce symptoms of Parkinson's disease and drug-induced
extrapyramidal syndromes. It is a derivative of adamantane, like rimantadine, a
similar drug.
As an antiparkinsonic it can be used as monotherapy; or together with L-DOPA
to treat L-DOPA-related motor fluctuations (i.e., shortening of L-DOPA duration
of clinical effect, probably related to progressive neuronal loss) and L-DOPA-
related dyskinesias (choreiform movements associated with long-term L-DOPA
use, probably related to chronic pulsatile stimulation of dopamine receptors).

Off-label uses

There have been anecdotal reports, based on research by Dr. William Singer of
Harvard University, that low-dose amantadine has been successfully used to
treat ADHD.[1] Amantadine has been shown to relieve SSRI-induced
anorgasmia in some people, though not in all people.

Side Effects

Amantadine has been associated with several central nervous system side
effects, including nervousness, anxiety, agitation, insomnia, difficulty in
concentrating, and exacerbations of pre-existing seizure disorders and
psychiatric symptoms in patients with schizophrenia or Parkinson's disease.
These side effects are likely due to amantadine's dopaminergic and adrenergic
activity, and to a lesser extent, its activity as an anticholinergic.

Cases of suicidal ideation in patients treated with amantadine have been

described,[2] although this psychiatric adverse event is relatively rare.
Nonetheless, clinical surveillance of suicidal ideation in patients on amantadine
is warranted at the clinician's discretion, as amantadine has been implicated as
the major fatal (biologically toxic) factor in completed patient suicides.[3]

Another potential side effect is livedo reticularis, a dermatological reaction that

results in skin mottling and purpurish mesh network of blood vessels.

Mechanism of its effects

The mechanism of its antiparkinsonic effect is not fully understood, but it

appears to be releasing dopamine from the nerve endings of the brain cells,
together with stimulation of norepiephrine response. Furthermore, it appears to
be a weak NMDA receptor antagonist and an anticholinergic.

The antiviral mechanism seems to be unrelated. The drug interferes with a viral
protein, M2 (an ion channel), which is needed for the viral particle to become
"uncoated" once it is taken inside the cell by endocytosis.

Misuse

Recently, amantadine is reported to have been used in China poultry farming in

an effort to protect the birds against avian influenza.[4] In western countries and
according to international livestock regulations, amantadine is approved only
for use in humans. Chickens in China have received an estimated 2.6 billion
doses of amantadine.[4] Avian flu (H5N1) strains in China and southeast Asia
are resistant to amantadine, but strains circulating elsewhere seem to be
sensitive. If amantadine resistant strains of the virus spread, the drug of choice
in an avian flu outbreak will likely be restricted to one of the scarcer and costlier
oseltamivir or zanamivir, which work by a different mechanism and are less
likely to trigger resistance.

Declining effectiveness

Early in the 2005/2006 flu season, the United States' Center for Disease
Control [CDC] found rates of amantadine resistance to be much higher than in
previous seasons. Looking at samples from 26 states yielded the following
findings:
 A total of 193 (92.3%) of 209 influenza A(H3N2) and 2 (25%) of
8 influenza A(H1N1) viruses analyzed contained point
mutations resulting in a serine-to-asparagine change at amino
acid 31 (S31N) of the M2 protein that conferred adamantane
resistance. [1]

A resistance rate of 92% for the major flu strain was called "alarmingly high".
The CDC issued an alert to doctors not to prescribe amantadine any more for
the season.[2] Among some Asian countries, A/H3N2 and

References

1. Hallowell, Edward M. and John J. Ratey, Delivered from Distraction:

Getting the Most out of Life with Attention Deficit Disorder (2005), pp. 253-
5.
2. Endo Pharmaceuticals (May 2003). "Symmetrel (Amantadine) Prescribing
Information" (PDF). Retrieved on 2007-08-02.
3. Cook et al, "Fatal overdose with amantadine". Can. J. Psychiatry (Nov
1986); 31(8), pp. 757-758.
4. Sipress, Alan. "Bird Flu Drug Rendered Useless", Washington Post, 2005-
06-18, pp. A01. Retrieved on 2007-08-02.
5. Deyde, Varough M.; Xu, Xiyan; Bright, Rick A.; Shaw, Michael; Smith,
Catherine B.; Zhang, Ye; Shu, Yuelong; Gubareva, Larisa V.; Cox, Nancy
J.; Klimov, Alexander I. (2007-07-15). "Surveillance of Resistance to
Adamantanes among Influenza A(H3N2) and A(H1N1) Viruses Isolated
Worldwide". Journal of Infectious Diseases 196 (2): 249-257. Retrieved on
2007-08-02.

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