CENTRAL NERVOUS SYSTEM STIMULANTS
Definition
Stimulants are a substance which tends to increase behavioral activity when administered. Primary action of a diverse group of pharmacologic agents – adverse effect associated with many drugs.
Signs and symptoms * Elevate Mood * Increase Motor Activity * Increase Alertness * Decrease need for Sleep
*In case of overdose lead to convulsion and death.
Mode of Action * Block neurotransmitters reuptake: Cocaine * Promote neurotransmitters release : Amphetamine * Block Metabolism - MAO inhibitors (monoamine oxidase):ex. Phenelzine * Antagonize the effect of inhibitory neurotransmitter:
Picrotoxin & Strychnine
Classification of CNS Stimulants * Analeptic Stimulants * Respiratory Stimulants * Convulsants * Methylxanthines * Psychomotor Stimulants * Sympathomimetics or Andrenergic CNS Stimulants
Analeptic Stimulants * To diverse chemical class of agents * Majority can be absorbed orally * Have a short duration of action * Pharmacological effect is terminated through hepatic metabolism * Ability to alter movement of chloride ions across neuronal membranes. (Possible common mechanism of action)
Pentylenetetrazole
Used clinically as a tool for screening latent epileptics and experimentally to screen compounds for anti-epileptic activity.
Picrotoxin
Used to study CNS mechanisms; it interferes with pathways that are strychnine resistant.
Strychnine
Is a source of accidental poisoning. Also used to study CNS mechanism, because of its relatively specific action as a glycine antagonist
Treatment for Strychnine Poisoning * Remove or reduce external sensory stimuli * Diazepam or Clonazepam IV or Nitrous Oxide by inhalation to depress CNS and stop convulsions which can be fatal.
Methylxanthines
Increase