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PSYCHOSTIMULANTS
A.T.SAMY SAH M.B.B.S., 2YEAR
Psychostimulant
• Psychostimulants are drugs that substantially influence cognitive and
affective functioning and behaviour pattern.
• Effects are increased motivational desire, agitation, heightened
vigilance, euphoria, hyperactivity, and decreased sleepiness as
well as appetite.
• Commonly used by drug abusers for the sake of kick
Drugs in this category are
Amphetamine
• Amphetamine,methamphetamine,
dexamphetamine are synthetic
symapathomimetic compounds with predominant
central actions
• Mechanism of action of these related drugs are to
increase the neurotransmitter release in the
synaptic cleft Eg, NA,DA,5-HT etc by various
mechanism such as acting on the NET,DAT,VMAT2
by exchange diffusion and reverse transport
• Cental effects- alertness,Inc concentration,
attention, euphoria, talkativeness,work capacity
• Included in dope test in athletes because they use
it to improve the performance
• In case of toxicity, chlorpromazine controls both
central as well as peripheral alpha adrenergic
effects
Methylphenidate
• Chemically and pharmacologically similar to
amphetamine
• Both act primarily by releasing NA and DA in the
brain
• Superior than amphetamine in treating ADHD in
children, because it causes less tachycardia and
growth retardation
• Behavior and learning ability are improved in 3 out 4
treated children
• PK- well absorbed orally,metabolized and excreted
in urine, t1/2 is 4-6hrs
• Side effects- anorexia,insomnia,growth
retardation,abdominal discomfort, bowel upset.
Modafinil
• This newer psychostimulant is popular in night-shift
(call centre)workers and other professionals who want
to improve alertness And to keep awake
• Modafinil inhibit the uptake of NA and DA and also alter
junctional concentration of glutamate and GABA
• Approved indications are Narcolepsy, sleep-apnoea
syndrome, shift-work Disorder
• It also suppress cocaine withdrawal symptoms
Cocaine
• Natural alkaloid from the leaves of erythroxylon coca
• Good Surface anaesthetic, First used for ocular
anaesthesia in 1884, never be injected it is a
protoplasmic poison causes tissue necrosis
• It induces a sense of well-being, delays fatigue and
increases power of endurance
• Cocaine also stimulates vagal center- bradycardia,
VMC- rised BP, VC- vomiting, temp regulating center-
pyrexia
• in periphery, blocks reuptake of NA and Adr into
adrenergic neurons resulting in symapathomimetic
action
Caffeine
• Caffeine is white, bitter, crystalline purine, a methyl xanthine alkaloid
• Caffeine is a CNS stimulant causing alertness And most
psychoactive drug in world
• Sources- coffee, tea leaves, cocoa beans, chocolate, energy drinks
• Effects Low dose(130-300mg) produces alertness,energy,elevation of
mood
• High dose(>400mg) causes
anxiety,dizziness,headache,diuresis,Tolerance
• PK- Poor water solubility,50%bound plasma protein,t1/2-3-6hrs in
adults
• Adverse effects- gi irritation,nervousness,insomnia,muscular
twitching
• Uses- in analgesic mixture in headache, Migraine- in combined
with ergotamine , apnea in premature infants as alternative to
theophylline
Overall therapeutic uses of psychostimulant
• Attention Deficit Hyperactivity Disorder
• Narcolepsy
• Elevation of mood
• Cognitive enhances
• Decongestion
• Increased endurance
• Reduced physical fatigue
• Increased alertness toward surroundings
• Increased libido
• Appetite suppression
Psychostimulants

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Psychostimulants

  • 2. Psychostimulant • Psychostimulants are drugs that substantially influence cognitive and affective functioning and behaviour pattern. • Effects are increased motivational desire, agitation, heightened vigilance, euphoria, hyperactivity, and decreased sleepiness as well as appetite. • Commonly used by drug abusers for the sake of kick
  • 3. Drugs in this category are
  • 4. Amphetamine • Amphetamine,methamphetamine, dexamphetamine are synthetic symapathomimetic compounds with predominant central actions • Mechanism of action of these related drugs are to increase the neurotransmitter release in the synaptic cleft Eg, NA,DA,5-HT etc by various mechanism such as acting on the NET,DAT,VMAT2 by exchange diffusion and reverse transport • Cental effects- alertness,Inc concentration, attention, euphoria, talkativeness,work capacity • Included in dope test in athletes because they use it to improve the performance • In case of toxicity, chlorpromazine controls both central as well as peripheral alpha adrenergic effects
  • 5. Methylphenidate • Chemically and pharmacologically similar to amphetamine • Both act primarily by releasing NA and DA in the brain • Superior than amphetamine in treating ADHD in children, because it causes less tachycardia and growth retardation • Behavior and learning ability are improved in 3 out 4 treated children • PK- well absorbed orally,metabolized and excreted in urine, t1/2 is 4-6hrs • Side effects- anorexia,insomnia,growth retardation,abdominal discomfort, bowel upset.
  • 6. Modafinil • This newer psychostimulant is popular in night-shift (call centre)workers and other professionals who want to improve alertness And to keep awake • Modafinil inhibit the uptake of NA and DA and also alter junctional concentration of glutamate and GABA • Approved indications are Narcolepsy, sleep-apnoea syndrome, shift-work Disorder • It also suppress cocaine withdrawal symptoms
  • 7. Cocaine • Natural alkaloid from the leaves of erythroxylon coca • Good Surface anaesthetic, First used for ocular anaesthesia in 1884, never be injected it is a protoplasmic poison causes tissue necrosis • It induces a sense of well-being, delays fatigue and increases power of endurance • Cocaine also stimulates vagal center- bradycardia, VMC- rised BP, VC- vomiting, temp regulating center- pyrexia • in periphery, blocks reuptake of NA and Adr into adrenergic neurons resulting in symapathomimetic action
  • 8. Caffeine • Caffeine is white, bitter, crystalline purine, a methyl xanthine alkaloid • Caffeine is a CNS stimulant causing alertness And most psychoactive drug in world • Sources- coffee, tea leaves, cocoa beans, chocolate, energy drinks • Effects Low dose(130-300mg) produces alertness,energy,elevation of mood • High dose(>400mg) causes anxiety,dizziness,headache,diuresis,Tolerance • PK- Poor water solubility,50%bound plasma protein,t1/2-3-6hrs in adults • Adverse effects- gi irritation,nervousness,insomnia,muscular twitching • Uses- in analgesic mixture in headache, Migraine- in combined with ergotamine , apnea in premature infants as alternative to theophylline
  • 9. Overall therapeutic uses of psychostimulant • Attention Deficit Hyperactivity Disorder • Narcolepsy • Elevation of mood • Cognitive enhances • Decongestion • Increased endurance • Reduced physical fatigue • Increased alertness toward surroundings • Increased libido • Appetite suppression