CENTRAL NERVOUS SYSTEM

STIMULANTS STIMULANTS
PRESENTED BY
SHWETA . D. SURWASE
M.Sc psychiatric Nursing First year
OBJECTIVES
 To define CNS stimulants
 To enlist general signs and symptoms of CNS stimualtion
 To classify CNS stimulants
 To know the mechanism of action of CNS stimulants
 To decribe cerebral stimulants
 To describe medullary stimulants
 Todescibe spinal stimulants
THE NERVOUS SYSTEM
The nervous system can be classified into:
 Brain and spinal cord
The Peripheral Nervous System (PNS )
 The nervous system outside of the brain
and spinal cord.
CNS STIMULATION.
CNS STIMULANTS-
INTRODUTION
CNS stimulants mostly produce a generalized
action which may, at high doses, result in
convulsions.
Their effects vary from the increase in the
alertness and wakefulness (as with caffeine) to the
production of convulsion ( as with strychnine) and
sometimes lead to death in over dose.
DEFINITION
CNS stimulants are the psychoactive
drugs that induce temporary
improvement in either mental or
physical function or both.
CLASSIFICATION
They can be divided based on their site of action:
1.Cerebral stimulants or cortical stimulant
(amphetamines)
2.Medullary stimulants (picrotoxin)
3.Spinal stimulants (strychnine)
CLASSIFICATION
On the basis of clinical use they can be classified as;
1. Convulsants: Strychnine,Picrotoxin,Bicuculline,
Pentylenetetrazol (PTZ).
2. Analeptics: Doxapram
3. Psycho stimulants: Amphetamines, Methylphenidate,
Atomoxetine, Modafinil, Armodafinil, Pemoline, Cocaine, Caffeine.
Many other drugs are capable of causing CNS stimulation as side
effect or at high doses
MECHANISM OF ACTION
 Block neurotransmitters reuptake (Most reuptake inhibitors
affect either NE or 5- HT(Serotonin) : Cocaine
 Promote neurotransmitters release : Amphetamine
 Block Metabolism - MAO inhibitors: Phenelzine
 Antagonize the effect of inhibitory neurotransmitter:
Picrotoxin & Strychnine
CEREBRAL/ CORTICAL
STIMULANTS
Cerebral, or psychic stimulants act on
the central nervous system and provide
a temporary sense of alertness and well
being as well as relief from fatigue.
PSYCHOMIMETICS
*Psychomimetics includes following agents
 i. Amphetamine
 ii. Methylphenidate
 iii. Methamphetamine
 iv. Cocaine HCl
MECHANISM OF ACTION
DRUG ENTER N ENDINGS BY ACTIVE TRANSPORT

DISPLACE DA(ALSO NE) FROM VESICLES BY ALTERING PH

↑DA CONC. IN SYNAPTIC CLEFT

ALSO INHIBITS MOA-B, ↓DA METABOLISM & DA

RELEASE TO SYNAPTIC CLEFT

 AMPHETAMINES
Amphetamines are chemically related to adrenaline.
They are sympathomimetic drugs which mimic the effect of stimulation on the nervous
system by increasing the levels of dopamine.
 USES
 Narcolepsy
 weight loss
 ADHD

ADVERSE EFFECT
 With prolonged use, they are neurotoxic, causing degeneration of amine-containing
nerve terminals and eventually cell death.
 • Regular use can lead to both tolerance & dependence.
 METHYLPHENIDATE (MPH)
 Methylphenidate (MPH) is a prescription stimulant commonly used to treat Attention-deficit hyperactivity
disorder, or ADHD.
 It is also one of the primary drugs used to treat the daytime drowsiness symptoms of narcolepsy and
chronic fatigue syndrome.
The drug is seeing early use to treat cancer-related fatigue Indications
1- ADHD
2- Narcolepsy
3- Treatment-resistant depression
4- Appetite suppressant
5- Antidepressant augmentation
 Contraindication

Use of tricyclic antidepressants: (e.g. desipramine), as methylphenidate may dangerously increase their
plasma concentrations, leading to potential toxic reactions (mainly, cardiovascular effects).
 METHAMPHETAMINE
 It is considered a second line of treatment, used when amphetamine and
methylphenidate cause the patient too many side effects. It is also used illegally
for weight loss and to maintain alertness, focus, motivation, and mental clarity for
extended periods of time, and for recreational purposes.
 Side effects
1.Methamphetamine has the potential to cause addiction.
2.Methamphetamine is a potent neurotoxin, shown to cause dopaminergic
degeneration.
3.Methamphetamine addicts may lose their teeth abnormally quickly, a condition
known as "meth mouth".
COCAINE
 Strong stimulant mostly used as recreational drug.
 Commonly snorted, inhaled or injected into veins.
 It is addictive & after short period of use, there is a
high risk that dependence will occur.

COCAINE CONTD…
Cocaine increase, mental alertness & produce a feeling of wellbeing & euphoria that is
similar to that caused by amphetamine like amphetamine.
 cocaine can produce hallucinations, delusion & paranoia cocaine increases motor
activity & at high doses causes tremors, convulsion & followed by respiratory &
vasomotor depression.
Uses
Cocaine has a local anesthetic action for the therapeutic use of cocaine, cocaine is
applied topically as a local anesthetic for eye, ear & nose & throat surgery
Adverse effect
cocaine stimulation of CNS is followed by a period of mental depression. Physical
dependence after only single use
 METHYLXANTHINES
Xanthine is a purine base found in most human
body Tissues and fluids and in Other organism
and it is also Bronchodilators.
Methylxanthines also antagonize many of the
effects of adenosine, acting on both A1 and A2
receptors.
  CAFFEINE – SHORT-ACTING
METHYLXANTHINE FOUND IN COFFEE (200
MG/CUP), CARBONATED SOFT DRINKS (60
MG/CAN), COCOA AND CHOCOLATE.

 THEOPHYLLINE – LONG-ACTING
METHYLXANTHINE FOUND IN TEA AND
PRESCRIBED FOR NIGHTTIME ASTHMA
 
PICROTOXIN
 Obtained from ‘fish berries’ of East Indies Anamirta cocculus. It is a potent
convulsant— convulsions are clonic, spontaneous and asymmetrical. The
convulsions are accompanied by vomiting, respiratory and vasomotor
stimulation.
 MOA
Picrotoxin antagonizes the GABA receptor channel directly. Therefore picrotoxin
prevents channel permeability and thus promotes an inhibitory influence on the
target neuron.
 Uses
It is most often used as a research tool, it has been used as a CNS stimulant and an
antidote in poisoning by CNS depressants, especially barbiturates ,for relieving
respiratory distress
DOXAPRAM
HYDROCHLORIDE
Doxapram hydrochloride (marketed as Dopram, Stimulex or Respiram) is a

respiratory stimulant.
 Administered intravenously, doxapram stimulates an increase in tidal volume,
and respiratory rate.
MOA
Doxapram stimulates chemoreceptors in the carotid bodies of the carotid
arteries, which in turn, stimulates the respiratory centre in the brain stem.
USES
Stimulate the respiratory rate in patients with respiratory failure. It may be
useful for treating respiratory depression in patients who have taken excessive
doses of drugs such as buprenorphin, also used for recovery after anesthesia
PENTYLENETETRAZOLE
 Pentylenetetrazole or cardiazole Pentylenetetrazol, also known as
pentylenetetrazole, metrazol, pentetrazol (INN),
pentamethylenetetrazol, Corazol, Cardiazol or PTZ, is a drug
formerly used as a circulatory and respiratory stimulant.
MOA
It is specifically a GABA-a receptor antagonist it acts at the
picrotoxin (PTX) site of the gamma-aminobutyric acid type A
(GABA(A)) receptor
CNS STIMULANT ADDICTION
 Increased intolerance
 Withdrawal symptoms
 Severe depression & suicidal thoughts
 Damage to body organ including heart & respiratory
system
 Illness due to poor nutrition
 Work & family problems
RESEARCH
QUESTION?????

 The nurse would expect the physician to order which drug for
the treatment of ADHD in children?
 A. Zolmitriptan (zomig)
 B. Doxapram HCL (dopran)
 C. Benzphetamine HCL (didrex)
 D. Methylphenidate HCL (ritalin)
ANSWERS
 METHYLPHENIDATE is most commonly used to treat ADHD
 • ZOLMITRIPTAN is used to treat migraines
 • DOXAPRAM is used as a respiratory stimulant •
 BENZPHETAMINE is an anorexiant
THANKYOU