Overview on

Stimulants, Depressant
and Hallucinogens
First

Introduction to CNS
Pharmacology
The nervous system can be classified into:

The Central Nervous
System (CNS)
Brain and spinal cord

The Peripheral
Nervous System (PNS (
The nervous system outside
of the brain and spinal cord



Ion channels & neurotransmitter
receptors
Voltage gated channels
Ligand gated channels

Ionotropic receptors
Metabotropic receptors
Membrane delimited
Diffusible second messenger

Ion channels
Metabotropic receptors
Neurons
They are the basic functional unit of the nervous system
by conducting nerve impulses.

They contain three major parts:
1. cell body.
2. dendrites.
3. axon.


Chemical transmission in the CNS

The CNS controls the main functions of the body
through the action of endogenous chemical
substances known as neurotransmitters.

Neurotransmitters

are stored in and secreted by neurons to
transmit information to the postsynaptic sites
producing either excitatory or inhibitory
responses.

Neurotransmitters can be classified into:
Excitatory:
Acetylcholine
Glutamate
Aspartate
Serotonin
Norepinephrine

Inhibitory:
GABA
Glycine
Stimulants
speed up the operation of the brain and
spinal cord

they cause the brain and the rest of the nervous
system to work harder

Effects:
1- Elevate Mood
2- Increase Motor Activity
3- Increase Alertness
4- Decrease need for Sleep

Stimulants

Mechanism of action:

1. Block neurotransmitters reuptake
2. Promote neurotransmitters release
3. Block Metabolism
4. Antagonize the effect of inhibitory neurotransmitter


CNS Stimulants
I. Cocaine, Crack (free base or hydrochloride).
II. Amphetamines:
D-Amphetamine, Methamphetamine, methylphenidate
(use to treat attention deficit disorders in children),
phenmetrazine (Preludin) - used to treat obesity,
(hallucinogens = MDA, MDMA, DOM;
methylenedioxymethamphetamine, "ecstasy,"
dimethoxyamphetamine).
III. Khat: Cathinone, methcathinone.
IV. Methylxanthines: caffeine (coffee), theophyline (tea),
theobromide (chocolate).

Effects on Mind, Brain, Behavior
alertness/vigilance, concentration
mental acuity, sensory awareness
euphoria/elevated mood
brain electrical activity
self-confidence, grandiosity
need for sleep (insomnia)
appetite
brain blood flow, glucose metabolism
London et al., 1999
Effects on Mind, Brain, Behavior (cont.)
sexual desire
anxiety, suspiciousness, paranoia
convulsions, tremor, seizure
psychosis, delirium
locomotion at low/moderate doses
repetitiveness, stereotypy at high doses
reinforcement/addiction
judgement, complex multi-tasking
Peripheral Effects
(sympathomimetic)
Blood pressure
Blood sugar
Heart rate
Irregular heart beat
Vasoconstriction
Body temperature
Bronchodialation
& Impaired breathing
Fight/Flight/Fright Syndrome
(sympathetic nervous system arousal)
slow down the operations of the brain
They first affect those areas of the brain that control a
person's conscious, voluntary actions.
As dosage increases, depressants begin to affect the parts of
the brain controlling the body's automatic, unconscious
processes, such as heartbeat and respiration.
CNS Depressants
Sedatives
Drugs that have an inhibitory effect on the
CNS to the degree that they reduce:
Nervousness
Excitability
Irritability
without causing sleep
CNS Depressants
CNS Depressants
Hypnotics
Calm or soothe the CNS to the point that they
cause sleep

Sedative-Hypnoticsdose dependent:
At low doses, calm or soothe the CNS
without inducing sleep
At high doses, calm or soothe the CNS
to the point of causing sleep

Opioid pain relievers
Codeine, heroin, hydrocodone, hydromorphone, methadone,
morphine, oxycodone, pentazocine
Alcohol
Inhalants
Gases, volatile solvents, nitrites
Anxiolytics
Benzodiazepines, Barbiturates, buspirone
Hypnotics
Chloral hydrate, zopiclone
CNS Depressants
Hallucinogens
Indolealkylamines
DMT, LSD, LSA, psilocybin
Phenylethylamines
Mescaline, MDA, MDMA, PMA, TMA
Cannabinoids
Anticholinergics
Deadly nightshade, jimsonweed, scopolamine
drugs that have the capacity to alter perceptual, cognitive,
and emotional states. They can alter consciousness in
profound and bizarre ways
Hallucinogens are divided into four classes:
serotonergic hallucinogens
methylated amphetamines
anticholinergic hallucinogens,
dissociative anesthetics

Hallucinogens
Serotonergic hallucinogens
include the synthetic compound LSD and
related drugs
mescaline (from the peyote cactus) and psilocybin
(from certain mushrooms)
All produce vivid visual hallucinations and a variety
of other effects on consciousness. They also have in
common the action of influencing serotonin
transmission in the brain
Methylated amphetamines
include MDA and MDMA (ecstacy).
structurally related to amphetamines
produce alterations in mood and consciousness
with little or no sensory change.
They act like amphetamine and cocaine on
dopamine, norepinephrine, and serotonin
synapses

Anticholinergic hallucinogens

include drugs like atropine and scopolamine
found in plants such as mandrake, henbane, belladonna, and
jimson weed.
These drugs produce a dreamlike trance
where the user awakens with little or no memory of the
experience




Dissociative anesthetics
The fourth class of hallucinogens include
phencyclidine (PCP or angel dust)
and the related compound ketamine.

They have the ability to produce surgical
anesthesia while the individual remains at least
semiconscious

Mechanisms of Action of LSD-like Drugs
LSD and other drugs in this class mimic serotonin.
Mescaline
is similar to LSD in that it produces vivid visual hallucinations,
and tolerance to its effects develop rapidly.


There is cross-tolerance between LSD, mescaline, and
other drugs of this class suggesting a common
mechanism of action
Effects of Serotonergic Hallucinogens
Physiological effects are similar to amphetamine and
cocaine
they include pupil dilation, increased heart rate and blood
pressure, increased body temperature, and increased
sweating.
Most common are profound changes in visual perception
form constants such as spiral explosions and a lattice pattern,
flashing lights, increased brightness
intensity of colors
trails or plumes around objects
sense of movement in stable objects, e.g., walls breathing
Synesthesia is also common
An effect sometimes produced by
hallucinogens characterized by the perception
of a stimulus in a modality other than the one
in which it was presented (for example, a
subject may report seeing music)

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