Central nervous system stimulants work by increasing levels of neurotransmitters like dopamine and norepinephrine. They cause initial feelings of euphoria and increased alertness and energy. However, regular use can lead to tolerance and dependence. Common stimulants include caffeine, nicotine, cocaine, and amphetamines. They are used both medically to treat conditions like ADHD, obesity, and narcolepsy, as well as recreationally for their mood enhancing effects. However, stimulants also carry health risks like increased blood pressure, anxiety, and addiction. Their effects are mediated through interactions with neurotransmitter systems in the brain.

1. Central nervous
system stimulants
A GENERAL EXPOSE.

2. Introduction to stimulants
 All stimulants cause an increase in general behavioural activity when taken
short- term(one/two weeks),
 stimulants cause state of euphoria, optimism and general feelings of well-
being.
 Initial feeling of anorexia are frequent. These responses indicate the
involvement of the Hypothalamus.
 The dopamine transmitter system is primarily involved in many of its
effects.

3. Stimulants
what are they?
 DEFINITION: Psychoactive drugs that induce temporary improvement in
either mental or physical functions or both. Effects include; alertness,
wakefulness and locomotion.
 Stimulants are widely used as prescription medicines as well as without
prescription(illicitly).
 Examples of Prescribed Stimulants; Amphetamines, Ephedrine, Caffeine,
Nicotine etc.
 Examples of Illicit Stimulants; Cocaine, Crack Cocaine, Methamphetamine

4. Mechanism of action of stimulants
 1. Block neurotransmitters reuptake (Most reuptake inhibitors affect either
NE or 5-HT(Serotonin) : Cocaine
 2. Promote neurotransmitters release : Amphetamine
 3. Block Metabolism - MAO inhibitors (monoamine oxidase):ex. Phenelzine
 4. Antagonize the effect of inhibitory neurotransmitter: Picrotoxin &
Strychnine

5. sources
They are mostly obtained from Plant Sources;
 Cocaine (Erythroxylum coca)
 Caffeine( Thea sinesis)
 Ephedrine (Ephedra sinica)
 Nicotine (Nicotiana tobaccum)
 Strychnine (Strychnox nux-vomica)
 Tea (Thea sinensis)
 Coffee (Coffea arabica)
 Theophylline / Theobromine (Theobroma cacao)

6. general indications of stimulants
 To counteract lethargy and fatigue throughout the day while at work or while doing
other activities.
 To reduce sleepiness and to treat narcolepsy.
 To decrease appetite and promote weight loss and to treat obesity.
 The CNS stimulants are used to treat conditions characterized by lack of adrenergic
stimulation, including narcolepsy (relatively rare sleep disorder) and neonatal apnea.
They are also used, that is, (Ritalin, Dexedrine) for their paradoxical effect in attention –
deficit hyperactivity disorder (ADHD). The benzphetamine, Sibutramine and the
anorexiants are also used for appetite reduction in severe obesity.
 Because of their ability to improve mood and self-confidence, doctors prescribe
stimulants in combination with anti-depressants to treat depression.
 Stimulants relax the bronchial muscles almost all asthma medications contain stimulants.
 Stimulants are also effective in treating cognitive disturbances in HIV patients and in
cancer patients going through cranial irradiation.

7. GENERAL INDICATIONS
 Caffeine is often added to painkillers in order to make them more
effective.
 Stimulants were also found to aid in smoking cessation (bupropion and
nicotine), reduce sleepiness and to keep the person awake when necessary
as well as to treat narcolepsy. In cases they are used to promote weight
loss, as well as to treat obesity.
 In the late 1880s cocaine was used as remedy for morphine addiction
suffered by many Civil War soldiers. Doctors used to numb the eye during
surgery as it restricted bleeding because it tightened up the blood vessels.
Later, in 1914 was added to the controlled list of drugs after its side and
adverse effects had become well documented.

8. SIDE AND ADVERSE EFFECTS
 Stimulants have a number of common side effects; these include stomach
upset, headache and increased blood pressure.
 Other adverse effects are insomnia, irritability, weakness, dizziness, tremor,
hyperactive reflex.
 Adverse effects of stimulants on the gastrointestinal tract include anorexia,
nausea, vomiting, abdominal cramps and diarrhoea.
 Stimulants also produce increased heart rate , increased blood pressure,
heart failure and arousal .

9. Medical and Non- medical uses of
stimulants
 Elevate Mood, Increase Motor Activity, Increase Alertness, Decrease need for Sleep,
In case of overdose lead to convulsion and death. All stimulant drugs cause an
increase in general behavioral activity.
 When taken short-term (one or two weeks), stimulant drugs cause states of
euphoria, optimism, and general feelings of well-being.
 Initial feelings of anorexia are frequent, a quality that leads to their use/abuse in
weight loss products. Insomnia is also frequent. These responses indicate that the
part of the brain which controls these functions, the hypothalamus, is strongly
affected by these drugs and that the dopamine transmitter system is primarily
involved in many of these effects. Other effects are:
• decreased feelings of depression, increased thoughts and associations, increased
talkativeness, increased blood pressure, anxiety, irritability, decreased fatigue

10. classifications
 Analeptic Stimulants: these are restorative or stimulative medicines, used
to overcome depression. E.g. Strychnine.
 Psychomotor Stimulants; these are psychotropic medications that
stimulate the CNS by boosting the release of certain chemicals. E.g.
Amphetamine, Methamphetamine, Ephedrine, Methylphenidate.
 Methylxanthines; these are E.g. Cocaine, Caffeine, Theophylline,
Theobromine.

11. Analeptic stimulants
 These are central nervous system stimulants used to treat ADHD (Attention Deficit
Hyperactivity Disorder) and Respiratory Depression. They are also used as convulsants.
 They act as Serotonin Receptor Agonists or Potassium Channel blockers. E.g. Doxapram.
 Analeptics have been used throughout history for two main purposes ; helping patients
recover from Anaesthesia more efficiently and the management of respiratory distress and
apnoea.
 FORMS: They generally occur in tablet formulation.

12. STRYCHININE
 MOA:
 Competitive antagonist of the glycin receptors.
 After injecting the mice with Strychinine you well
 notice:
- Tonic convulsion characterized by :
 1. Symmetric
 2. Reflex in origin
 3. Continuous
 4. Uncoordinated.

13. Side effects of analeptics;
 Sweating
 Nausea
 Vomiting
 Urinary retention and muscle spasticity
 Diarrhoea

14. Psychomotor stimulants;
AMPHETAMINES
 Mechanism of action;
 Block the reuptake of norepinephrine and dopamine into the presynaptic neuron
and increase the release of these monoamines into the extra neuronal space.
Clinical use:
 1. Narcolepsy,.
 2. Attention-deficit hyperactivity disorder
 AFTER ADMINISTRATION: Hair Erection, Licking, Sniffing are major side effects

15. amphetamines
common names;Speed Crystal Meth Bennies Dexies
Uppers Pep pills Ice Whiz Diet pills
Jolly beans Copilots Hearts Footballs White crosses
Crank Chalk Glass

16. TYPES OF AMPHETAMINES
 Designer drugs: are a product of amphetamine and methamphetamine
that have prominent psychedelic effects in addition to their CNS
stimulatory action.
Some designer drugs are…
 Meth cathinone (combination of methamphetamine and cocaine)
 Methylenedioxy-n- methylamphetamine (MDMA, Ecstasy)(Stimulant and
Hallucinogen)
 Methylenedioxyamphetamine
 Detroamphetamine: Used for ADHD and narcolepsy
 Levoamphetamine: A psychostimulant used to increase alertness

17. Adverse effects:
 Cardiovascular: Hypertension (7% to 22%, pediatric )
 Endocrine metabolic: Weight loss (4% to 9%, pediatric; 11%, adults )
 Gastrointestinal: Abdominal pain (11% to 14%, pediatrics ), Loss of
appetite (22% to 36%), Xerostomia (35% )
 Neurologic: Headache (26% ), Insomnia (12% to 17%), pediatric;
(27%, adults )
 Psychiatric: Feeling nervous (6% )

18. Forms
Powder
• Can vary in color, most common in white to brown
Tablets And Capsules
• Varies in color
Crystal
• Most potent form of amphetamine
• Large sheet like crystals or crystalline powder

19. Amphetamine effects
Increases
Energy
Insomnia Euphoria
Decreases
appetite
• Weight loss
Increases
concentration
Increases
Motivation
Irritability Dry mouth Alertness
Anxiety and
panic
Headache
Increased
heart rate and
blood pressure
Increased
body
temperature
and sweating
Increased
breathing rate
Mood swings
Depression
Behavioral
stereotypy
•Meaningless repetition
of single activity

20. Cocaine
MECHANISM OF ACTION;
 Binding with adenosine (“purine”) receptors in brain (endogen ligand of
these receptors – adenosine - decreases processes of excitation in CNS)
 Inhibiting of phosphodiesterase, which leads to accumulation of cAMP and
stimulation of many physiological processes and metabolism

21. Pharmacological effects;
 CNS-behavioral effects result from powerful stimulation of cortex and
brain stem.
 Cocaine acutely increases mental awareness and produces a feeling of
wellbeing and euphoria similar to that produced by amphetamine.
 Like amphetamine, cocaine can produce hallucinations and delusions of
paranoia or grandiosity.
 Cocaine increases motor activity, and at high doses, it causes tremors and
convulsions, followed by respiratory and vasomotor depression.

22. Pharmacological effects of cocaine
 Enhanced activity of dopamine, noradrenaline, adrenaline and serotonin
transmitters
 Blocks the reuptake and inactivation of these elements following their release
from neurons
 CNS Effects
 Creates increased strength, energy, and performance
 Increases euphoria, self-confidence, well-being, and sociability
 Cardiovascular System Effects
 Increases the levels of adrenaline, increases heart rate, raises blood pressure
 Local Anesthetic Effects
 Reduces bleeding
 Topical numbing effects

23. cocaine
Blow Snow Flake C
Coke Toot White lady Nuggets
Tornado Rock(s) Fat Bags Nose Candy

24. forms
Little Pellets also known as rocks
• Must be crushed before use
Flakes or Powder
Speedball: cocaine typically mixed with heroin and
smoked

25. Mode of administration
Orally
Inhaled
(snorted)
Injected Smoked

26. Crack cocaine
Cocaine
Hydrochlori
de
Baking
soda
Water
Paste which
dries into hard
rock pieces
Already processed cocaine and making it pure again is crack cocaine
Could contain as much as 90% pure cocaine
Inexpensive
Typically smoked in a glass water pipe
A rush or high happens within 8 to 10 seconds
The high can last about 3 to 5 minutes
“Crash” occurs for 10 to 40 minutes
Extreme state of depression

27. methylxanthines
 1.Theophylline (found in tea): long-acting, prescribed for night-time
asthma
 2.Theobromine: found in cocoa.
 3.Caffeine: (short-acting) the most widely consumed
 found in coffee (200 mg/cup),
 carbonated soft drinks (60 mg/can),
 cocoa and chocolate

28. Pharmacologic actions of caffeine
 Vessels: Stimulation of vasomotor center ;contraction of vessels,
increasing of BP, Peripheral myotropic spasmolytic action – dilation of
vessels, decreasing of BP
 Heart : Central action (increasing of n. vagus tone) – bradycardia,
Peripheral action (direct influence on heart) – tachycardia, possible
extrasystolia
 Diuretic effect : It has a mild diuretic action that increases urinary output
of sodium, chloride and potassium
 Gastric mucosa :Since all methylxantines stimulate secretion of
hydrochloric acid (HCl) from the gastric mucosa, individuals with peptic
ulcers should avoid beverages containing methylxantines

29. Adverse effects
 If administered regularly – psychological addiction – theism, which is
accompanied by development of abstinent syndrome (headache,
retardness, fatigue, somnolence, depression)
 Insomnia, anxiety, agitation
 Acute poisoning in case of overdosing (lethal dose – 10g for caffeine –
about 100 cups)

30. Adverse effects;
 Increased happiness and excitement
 Talk, move, and think quickly, alertness, wakefulness, restlessness, Heart beats faster,
Nervousness and anxiety
 Mood swings
 Aggressiveness
 Paranoia, Twitching and shaking of the body
 Increased Blood Pressure, Could lead to heart attack or stroke
 Suppressed appetite, Possible weight loss

31. ADVERSE EFFECTS
 Anxiety reaction that includes: hypertension, tachycardia, sweating, and
paranoia.
 Because of the irritability, many users take cocaine with alcohol.
 A product of cocaine metabolites and ethanol is cocaethylene, which is
also psychoactive and cause cardiotoxicity.

32. effects
 a. CNS:
 decrease in fatigue, increased alertness: 100-200 mg caffeine in 1 or 2 cups of coffees
 Spinal cord stimulation: 2-5 g (very high dose)
 Tolerance can rapidly develop
 Withdrawal symptoms: feeling of fatigue & sedation.
 b. CVS: at high dose of caffeine +ve inotropic and chronotropic effects on the heart,
↑COP
 c. Diuretic action: mild ↑ urinary output of Na+, Cl-and K+
 d. Gastric mucosa: all methylxanthines stimulate secretion of HCl
 e. Respiratory smooth muscle: bronchodilator, Rx asthma replaced by β-agonists,
corticosteroids.

33. Caffeine and caffeine like products
(xanthines)
CNS Effects
 100-200 mg/day - Alertness, arousal, and reduces tiredness
 300+ mg/day – Insomnia, increased tension, anxiety, and muscle
twitches
 500+ mg/day – panic sensations, chills, nausea, and clumsiness
 Extreme doses/day – May result in seizures, respiratory failure, and
even death
Cardiovascular and Respiratory Effects
 500+ mg leads to increased heart activity
 Can help with asthma-related respiratory problems

34. Adverse effects
 Moderate doses: insomnia, anxiety, agitation
 High doses: emesis, convulsion
 Lethal dose (10 gm of caffeine): cardiac arrhythmia
 Suddenly stop: lethargy, irritability, headache

35. Mode of administration
Oral
Insufflation (Snorting)
Injection
Rectal

36. nicotine
 Nicotine is the active ingredient in tobacco.
 Used in smoking cessation therapy,
 Actions of Nicotine:
 Low dose: ganglionic depolarization
 High dose: ganglionic blockade

37. effects
 CNS:
 1.Low dose: euphoria, arousal, relaxation, improves attention, learning,
problem solving and reaction time. 2.High dose: CNS paralysis, severe
hypotension (medullary paralysis)
 II. Peripheraleffects:
 Stimulation of sympathetic ganglia and adrenal medulla→↑ BP and HR
(harmful in HTN patients), Stimulation of parasympathetic ganglia→↑ motor
activity of the bowel
 At higher doses, BP falls & activating ceases in both GIT and bladder.
 The acute lethal dose is 60 mg.
 Adverse effects:
 CNS: irritability and tremors, Intestinal cramps, diarrhea, ↑HR & BP

38. Withdrawal symptoms of cns
stimulants
Hunger Anxiety Irritability Aggression
Radical mood
swings
Depression Paranoia
Extreme
fatigue
Long but
restless sleep
Nightmares
Severe distress
and panic

39. remedy
 The first step of treating an addiction is detoxification (the process of
letting the body remove drugs in it). During detox, doctors manage the
physical part of the addiction by getting the stimulants out of the person’s
system. Detox typically lasts up to a week but could last longer depending
on the severity of the addiction. Also, the type of stimulant used affects
how long it takes to detox; for example, people addicted to cocaine tend
to have a short time to detox than people addicted to prescription
stimulants like Adderall.
 Some studies have been able to come up with certain drugs that may
reduce cravings and lead to a successful recovery. Examples of such drugs
are Prozac which is prescribed for mood disorders like depression and
obsessive compulsive disorder and also Naltrexone, which has also shown
potential in treating prescription stimulant-depression.

40. remedy
 Psychotherapy and counselling may also be used in alleviating problems in
cases. Psychotherapy is a general term for treating mental health problems
by talking with a psychiatrist, psychologist or other mental health provider.
During psychotherapy, you learn about your condition and your moods,
feelings, thoughts and behaviours.
 Reduction of dose of stimulants using devices such as the electronic
cigarette and chewing gums, is also another alternate remedy. In the cases
of remedy for smoking habits, cigarette, containing nicotine, is substituted
with electronic cigarettes which can be regulated to stop the habit in
entirety. Medicated chewing gums may also be recommended instead of
the electronic cigarette depending on the intensity of the addiction.

41. THANK YOU!