1. The Central Nervous System
Pharmacology I
BMS 242
The Central Nervous System
CNS Stimulants
L. Aya M. Serry
2017

2. Lecture Objectives Introduction and Classification of CNS Stimulants
Psychomotor Stimulants;
Body Effects
Therapeutic Uses
Side Effects
Psychotomimetic Stimulants;

3. What are CNS Stimulants?
CNS Stimulants are drugs that induce temporary improvements in either mental or physical functions or both
Examples of these kinds of effects may include enhanced alertness and wakefulness

4. CNS Stimulants General Body Effects
Elevate Mood
Increase Motor Activity
Increase Alertness
Decrease need for Sleep
In case of overdose lead to convulsion and death

5. CNS Stimulants 

6. A) Psychomotor Stimulants

7. 1- Methylxanthines Caffeine Theophylline Theobromine
They are all from plant origin, Caffeine is the most widely consumed stimulant in the world which is present in high concentrations in coffee beans , also in tea and cocoa

8. Effects on different organs
1- Methylxanthines (Caffeine)
Effects on different organs
Caffeine Normal Dose is 400 mg/day which is equivalent to 4 cups of coffee, 10 cans of coke and 2 energy boosting drinks

9. Methylxanthines (Caffeine)
Withdrawal symptoms start with people consuming <600 mg/day
It has a synergistic effect with NSAIDs and increases their absorption

10. 2- Nicotine CNS stimulant found in Tobacco plant
No Therapeutic value (Except Nicorette®)
Cigarette smoke has a serious risk factors for respiratory, CVS diseases and Cancers (Cigarette: Not only nicotine, Tar and Carbon Monoxide)
It causes dependence and withdrawal symptoms are not easily overcome

11. 2- Nicotine Effects on the body:
Low doses: Arousal, relaxation, Increased attention and decreased appetite
High doses: Central respiratory depression and severe hypotension ( only with nicotine-containing pesticides)
Nicotine stimulates Nicotinic receptors (Nn), as a result increased both Sympathetic and Parasympathetic body effects

12. 2- Nicotine
Smoking cessation program (Drug and Behavioral treatments):
Varenicline (Champix®)
Very effective drug that is a partial agonist on Nn receptors
A treatment program of 12 weeks
Side effects : Nausea, Vomiting and sleep disturbances
Day 1-3; 0.5 mg once daily
Day mg twice / day
Day weeks , 1 mg twice/day

13. 3- Cocaine Strong CNS stimulant from Coca plant
Used topically as local anaesthetic
Mechanism Of Action: Serotonin, NE, Dopamine reuptake inhibitor [ SNDRI]
Administration: smoking-snorting or I.V.

14. 3- Cocaine Effects on the body: Feeling of well-being and euphoria
Increases mental alertness and attention
Side effects:
Increased heart rate, Mydriasis, increased body temperature
Overdose: tachycardia, convulsions and respiratory failure
Highly addictive, withdrawal symptoms appear soon after discontinuation

15. 4- Amphetamines

16. Amphetamines

17. 4- Amphetamines These drugs are highly addictive
Body Effects: Wakefulness- euphoria – increase alertness and suppress appetite
They are administered illegally (I.V. and smoking) and abused as performance and cognitive enhancers (e.g: athletes)

18. 4- Amphetamines

19. 4- Amphetamines
Methamphetamine (Street name: Speed) and Fenethylline (Captagon®)
Most addictive and highly abused amphetamines
Methylphenidate [ Ritalin®]
The least addictive so it is used in ADHD treatment
Modafinil
Wakefulness-promoting agent
Used in Narcolepsy treatment
Used by aviators in military services to increase wakefulness

20. B) Psychotomimetic Stimulants

21. Dronabinol
The pharmacological actions of Dronabinol (THC) result from its partial agonist activity at the cannabinoid receptor CB1, Located mainly in the central nervous system, and the CB2 receptor, mainly expressed in cells of the immune system
The psychoactive effects of THC are primarily mediated by its activation of CB1 G-protein coupled receptors

22. Dronabinol

23. Dronabinol

24. CNS Stimulants Uses Indications
Analeptics (CNS stimulants) Reversal of anaesthesia-induced respiratory depression
Anorexiants Thought to suppress the appetite control centre in the brain (Withdrawn lately from Markets)
ADHD Stimulate the areas in the brain responsible for mental alertness and attentiveness
Narcolepsy Increase mental alertness
Migraine headaches
*Caffeine, co-administered with other drugs, used to treat headaches