AMPHETAMINES

Itzel Martnez Ocampo

WHAT IS IT?
It is a synthetic adrenergic agent

Powerful central nervous system stimulant
Amphetamine
Dextroamphetamine
Methamphetamine
ATS
HISTORY
Amphetamine is a chemical derivative of
ephedrine, first synthesized in 1887 by the
Romanian chemist L. Edeleano, who called the
compound as fenilisopropilamina.

Preliminary investigations focused on the
peripheral effects and found that it was a
sympathomimetic amine with bronchodilator
properties.

The experimental medical use of
amphetamines began in the twenties. The
drug would be used by the military since
several nations, especially the Air Force, to
combat fatigue and increase awareness
among the militias
Amphetamines would be used for purposes
as varied as narcolepsy, obesity, depression,
ADHD in children and adults, the treatment
of sedative overdose, and even the
rehabilitation of alcoholism and other drug
habit.

Amphetamine has been used as an agent to
improve performance, both physically
(opening the sports doping), and
intellectual (cognitive doping). The
indiscriminate dispensing of the product,
coupled with the lack of public awareness
about their potential dangers and the lack
of a suitable system of pharmacovigilance,
triggered phenomena of abuse and
addiction. In 1971, amphetamine was
subject to international control under the
International Convention on Psychotropic
Substances.
PHARMACOKINETICS

Amphetamine is administered orally and
has a good absorption, so that the onset of
therapeutic action occurs after about 30 to
60 minutes. The elimination half-life is
about 10 hours. Clinical effects are
prolonged for 6 to 8 hours
MECHANISM OF ACTION
Amphetamine is an indirect agonist of the
presynaptic receptors for norepinephrine (NE)
and dopamine (DA) to the central nervous
system level. Amphetamine binds to and
activates these receptors, inducing the release
of neurotransmitters booking housed in vesicles
in nerve endings by converting the respective
molecular transporters into open channels. It
also has a serotonergic agonist action, albeit
relatively weaker.
As methylphenidate (Ritalin),
amphetamine also prevents monoamine
transporters DA and NA recapture the
synaptic space (reuptake inhibition), which
leads to an increase in extracellular DA
levels and NA. The power level of
amphetamine to block these carrier
molecules is less than the
methylphenidate.

2

Promoting nerve impulse
transmission in the dopaminergic
and noradrenergic neuronal
networks.
THERAPEUTIC ACTION
Amphetamine stimulates the central
nervous system improving wakefulness
and increasing levels of alertness and
ability to concentrate.
Favors higher cognitive functions such
as attention and memory (in particular,
working memory) and shows its effects
on executive functions.
Reduces levels of impulsivity
It is an activating agent of the sympathetic
nervous system; peripheral adrenergic
effects, resulting in:

1. An increase in the level of motor activity (resistance to
fatigue)
2. In the cardio-respiratory activity
3. Thermogenic metabolic processes of the organism,
leading to increased fat burning.

1. Attention deficit disorder with
hyperactivity

2. Narcolepsy

3. obesity