Indirect acting sympathomimetics act on adrenergic neurone to release noradrenaline NA, which then act on adrenoceptors.
  Drugs present in this class: Amphetamine, Tyramine

Amphetamine

Trade Name Adzenys XR-ODT | Dyanavel XR | Evekeo | Evekeo ODT

Drug Class CNS Stimulant

Pharmacological Action

 Amphetamines having a pharmacological profile similar to ephedrine.

CNS

 They exert potent CNS stimulant. The central effects include
  • Alertness
  • Increased concentration and attention span
  • Postponement of sleep
  • Euphoria (a state of intense happiness and self-confidence)
  • Talkativeness
  • Increased work capacity

Reticular Activating System (RAS)

 RAS is stimulated resulting in wakefulness and postponement of sleep deprivation.

Respiratory Center

 Amphetamines stimulate respiratory centre, specifically if it has been depressed.

Other actions

 Hunger is suppressed due to inhibition of hypothalamus feeding center.
 Hear rate and BP are not significant at usual doses.
 Tone of vesical sphincter (sphincter present in urinary bladder) is increased.

Adverse drug reactions

Central effects

 High doses produce,
  • Euphoria
  • Restlessness
  • Insomania
  • Aggression
  • Mental confusion
  • Delirium (confused thinking and reduced awareness of the environment)
  • Hallucination

Peripheral effects

  • Rise in BP
  • Palpitation
  • Arrhythmias
  • Vomiting
  • Abdominal cramps
  • Vascular collapse

Toxicity treatment

 Administration of chlorpromazine which controls both central as well as peripheral alpha adrenergic effects.

Mechanism of Action

Amphetamine (Amph) enters the adrenergic neurone through neuronsl Norepinephrine Transporter (NET) or Dopamine Transporter (DAT)
↓
Enters storage vesicles through Vesicular Monamine Transporter (VMAT2)
↓
It displaces the stored Noradrenaline (NA) into the neuronal cytoplasm
↓
NA is released into synaptic cleft by exchange diffusion with extracellular amphetamine or by reverse transport, both uses NET

amphetamine mechanism
Uses

  • Attention Deficit Hyperactivity Disorder (ADHD)
  • Narcolepsy
  • Obesity
  • Depression