CNS Stimulant lecture Drug summary.

Done by Hnnen Al-Shikh, Kholoud Fallatah.

Pharmacology committee.

Psychomotor stimulants

Pharmacokinetics
Methylxanthines :
Theophylline
tea
Theobromine
cocoa
Caffeine
coffee

well absorbed
caffeine distributes
throughout the body
and to the fetus and
mothers milk
metabolized by liver
by CYP1A2 pathway
excreted in urine

Nicotine

Highly lipid soluble

cross BBB easily
Cross placenta and
reach mother milk
Metabolized in lung,
liver and urinary
excretion
Tolerance to the toxic
effect develops rapidly

cocaine

increases mental
awareness.
euphoria.
Hallucinations.
Stimulates the
Sympathetic nervous
system: tachycardia,
hypertension,
pupillary dilation.
Cocaine is the only
local anesthetic that
causes
vasoconstriction .

Action

Uses

CNS stimulation
Diuresis

Cardiac muscle
stimulation
Relaxation of smooth

muscle, especially
bronchial muscle
Stimulate HCL secretion
(peptic ulcers patients
should avoid them)
Nicotine receptors in CNS
where actions occur, such
as:
arousal and relaxation
(low doses)
respiratory paralysis
(high doses)

potentiates and
prolongs the CNS and
peripheral actions of
these catecholamines

Adverse effect

Caffeine + ergot alkaloid

(Ergotamine): treat migraine
headache
Theophylline: prophylaxis for
chronic asthma (bronchodilator)

Not used therapeutically

But secondary to caffeine as CNS
stimulant
Secondary to alcohol the most
abused drug (pharmacological
and behavioral therapy for
abusers)
Combined with tars and CO in
cigarette smoke

Not used

Short-Term:
Euphoria
Tachycardia
Respiration rate
Long-Term:
Agitation
Hypertension
Dyspnea
nasal collapse
Then:
seizure
Arrhythmias
Respiratory failure .

Pharmacokinetics

Action

Uses

Adverse effect

Psychomotor stimulants

indirect
elevation of the level of
catecholamine
transmitters in synaptic
spaces.

Amphetamine
o

methamphetamine

o Absorbed from GIT

100%
o Often administered
by IV or smoking.
o Metabolized by the
liver.
o excreted in the urine.
o The euphoria lasts 4
to 6 hours "its 4 to 8
times longer than
cocaine".
o Cause:
1. addictiondependence
2. tolerance
3. drug-seeking
behavior.
o

releasing intracellular
stores of
catecholamines.
also blocks
monoamine oxidase
(MAO).

1. Attention deficit syndrome.

Uses the derivative
methylphenidate
2. Narcolepsy.
a disorder marked by an
uncontrollable desire for sleep.
3. Appetite control
(suppresant)

CNS EFFECTs:
o stimulates the entire
cerebrospinal axis,
Overdoses of amphetamine are
cortex, brain stem, and
treated with chlorpromazine.
medulla.
o stimulates the entire
its -blocking effects on M2 ,H1,
cerebrospinal axis,
D1, D2, 1 receptors .
cortex, brain stem, and
medulla.
o This increased
alertness, decreased
fatigue, depressed
appetite, and
insomnia.

hypertension
insomnia
Anorexia
tremors
risk of exacerbating
schizophrenia
risk of dependence.
Cerebral
haemorrhage

long-term
psychological effects
psychotic symptoms
anxiety depression
cognitive impairment.

Pharmacokinetics

Action

Uses

Adverse effect

Psychomimetic Stimulants

Lysergic acid
diethylamide (LSD)

Tetrahydrocannabino:
From leaves of the
plant- Cannabis sativa

Hashish
Marijuana-

Sometimes high doses

causes:
produce long-lasting
psychotic changes in susceptible individuals.

Serotonin (5-HT) agonist

True dependence is
activity at presynaptic
rare.
receptors in the midbrain,
Haloperidol and other
binding to both 5-HT 1 and 5neuroleptics can block the
HT 2 receptors.
hallucinatory action of LSD
Activation of the sympathetic
nervous system

smoking THC effect:

Euphoria
Uncontrolled laughing
Feeling of relaxation
Altered time sense
Dream like state.
impairs short-term
memory.
mental activity .
decreases muscle
strength.
impairs highly skilled
motor activity "driving a
car".

THC receptors found

endogenously on presynaptic
nerve terminals that interact
synaptically with pyramidal
neurons.

Hyper-reflexia.
Nausea.
muscular weakness.

Haloperidol and other

neuroleptics can block the
hallucinatory action of LSD
and quickly abort the
syndrome.
Dronabinol - CB
(cannabinoid)
receptor agonist:
AIDS patient who
are losing weight.
cancer patients
severe emesis

Rimonabant - CB
(cannabinoid)
receptor antagonists
Obesity treatment
by decrease appetite
and body weight.

An increased heart rate,

Decreased blood
pressure, and a
Reddening of the
conjunctiva.
At high doses, a toxic
psychosis develops.
Tolerance and mild
physical dependence
occur with continued
frequent use of the drug.