CNS STIMULANTS

Presented by : K. SHIVAKUMAR B- Pharmacy 4th Year 2nd sem. Roll No. : 180920 _______________________________ Arya college of pharmacy

I NTRODUCTION
C N S S T I M U L A N T S

Def:

a group of drugs which produce an increase in mental and motor activity when administered

S IGNS
C N S S T I M U L A N T S

AND SYMPTOMS :

1- Elevate

Mood.

2- Increase in motor activity.

3- Increase Alertness.
4- Decrease sleeping. 5- In case of overdose,convulsion and death. 6-Increased b.p& talkativeness

C LASSIFICATION
C N S S T I M U L A N T S

1.Cerebral stimulants:

Amphetamine, Methamphetamine, Methylphenedate, Caffine,Theophyllin,

Cocaine.

2.Medullary stimulants:

Doxapran, Picrotoxin, Nikethamide,

3.Spinal stimulants:

Strychnine,

Cerebral stimulants Amphetamine:

C N S S T I M U L A N T S

C: N 2-phenylethan-1-amine

M.O.A Increase the amount of NE such as norepinephrine and dopamine Inhibition of reuptake mechanism for several biogenic amines

Mechanism action:
C N S S T I M U L A N T S

Enhancement of neuronal release of catecholamine

C LINICAL
C N S S T I M U L A N T S

USES :

Appetite suppressant ADHD

Narcolepsy and chronic fatigue syndrome Treatment-resistant depression

A DVERSE EFFECTS :
C N S S T I M U L A N T S

1- Cardiovascular: Vasoconstriction ,Tachycardia

2- Ear, nose, and throat: Decongestant, Xerostomia 3- Eye: Mydriasis, Relaxation of ciliary muscle 4- Gastrointestinal: Decreased secretions,
peristalsis

5- Genitourinary: Urinary retention, Erectile

dysfunction

6- Others: Decrease in appetite/weight loss

S IDE
C N S S T I M U L A N T S

EFFECTS :

Constipation
Dizziness loss of appetite Nervousness restlessness stomach pain or upset trouble sleeping

C N S S T I M U L A N T S

Pharmacokinetics:
Amphetamine is completely absorbed from the GI tract, metabolized in the liver and excreted in the urine.

Contraindications:

CNS depressants Agitated states Patients with a history of drug abuse Glaucoma

METHYLPHENIDATE:
C N S S T I M U L A N T S

C:N-Methyl phenyl(piperidin-2-yl)acetate

Methylphenidate is a norepinephrine and dopamine reuptake inhibitor,

USES & SIDE EFFECTS

C N S S T I M U L A N T S

USES:
1. 2. 3. 4. 5. ADHD Narcolepsy Treatment-resistant depression Appetite suppressant Antidepressant augmentation

Side effects:

Cardiovascular: Arrhythmia or increase in blood pressure Endocrinal: Appetite loss Eye: Blurred vision Gastrointestinal: Nausea/vomiting, abdominal pain

METHAMPHETAMINE
C N S S T I M U L A N T S C:N-N-methyl-1-phenylpropan-2-amine

M.O.A
Methamphetamine acts as a dopaminergic and adrenergic reuptake inhibitor
Uses:

ADHD Extreme obesity Narcolepsy

Side effects:

High blood pressure Increased heart rate, Dizziness

C OCAINE HC L :
C N S S T I M U L A N T S

Methyl (1R,2R,3S,5S)-3- (benzoyloxy)-8-methyl-8azabicyclo[3.2.1] octane-2-carboxylate

uses :
Local anasesthesia (eye, nose & throat surgery) Eye drops cause mydriasis (used in eye examination). Appetite suppressant

Side effects : Abortion and premature labour in women . Cocaine base (Crack) is more toxic than the salt Dizziness; dry mouth; Loss of appitite

M ECHANISM
C N S S T I M U L A N T S

ACTION :

Prevents reuptake of NA in the CNS and Periphery (prolongs the action)

X ANTHINE DERIVATIVES
C N S S T I M U L A N T S 1.Caffine 2.Theophylline 3.Theobromine 4.Methyl xanthine

T HE X ANTHINE D ERIVATIVES :
C N S S T I M U L A N T S

M.O.A:

Methylxantines inhibit phosphodiesterase enzymewhich convert 3,5 cyclic AMP to the inactive 5-AMP, thus increasing concentration of cyclic AMP and cyclic GMP inthe tissues. Xanthines inhibit adenosine receptors . This action is responsible for their Bronchodilator effect

C N S S T I M U L A N T S

Pharmacological actions :

Smooth muscle: relaxation (esp. bronchi) Theophylline most effective .

CNS stimulatins (theophylline > caffeine) . Cardiovascular Tachycardia & dysrhythmias at high doses .

Clinical uses :

Theophylline-- Bronchial asthma Aminophylline (theophylline + ethylene diamine) used in asthma Caffeine: headache caffeine + ergot alkaloids migraine Pentoxiphylline (derivative of theobromine) for vascular Disorders.

1).P ICROTOXIN :
1).Picrotoxin:

it is central nervous system and respiratory stimulant formerly used in barbiturate and other anesthetic poisonings;
Mechanism of action:
Picrotoxin antagonizes the GABAA receptor channel directly, which is a ligand-gated ion channel concerned chiefly with the passing of chloride ions across the cell membrane. Therefore picrotoxin prevents Cl- channel permeability and thus promtes an inhibitory influence on the target neuron

M EDULLARY STIMULANTS N IKETHAMIDE

C N S S T I M U L A N T S

C:N N-N-DIETHYL-3-PYIDINE CARBOXAMIDE

M.O.A:

Reflex-mediated stimulation of respiratoin by stimulating chemoreceptor in carotid body increasing sensitivity of respiratory center to CO2

USES: Useful for mountain climbers to increase endurance at high altitudes.

S PINALSTIMULANTS S TRYCHNINE
C N S S T I M U L A N T S

MOA:

Competitive antagonist of the glycine receptors.

In large doses strychnine causes tonic convulsion

Tonic convulsion characterized by : 1. Symmetric.

2. Reflex in origin.
3. Continuous. 4. Uncoordinated

C N S S T I M U L A N T S

Adverse effect: Tremors, Severe spasm. Respiratory arrest, Painful convulsions

Contraindications:

Uses: Bronchial asthma, Constipation, Diabetesmellitus, Urinary tract dis order Opthalamic disease

Excessive reflex irritability, Acute inflammatory conditions of the spinal cord.

C ONCLUSION :
C N S S T I M U L A N T S

Central nervous system (CNS) stimulants may be used to reduce tiredness and increase alertness, competitiveness, and aggression. They are more likely to be used in competition but may be used during training to increase the intensity of the training session. There are several potential dangers involving their misuse in contact sports.