CNS stimulants and Marijuana

Question 1

Cocaine

Answer 1

Mech: prevents reuptake of NE, 5HT, and DA

Local vasoconstrictor (avoid epi)

Kinetics:

• T1/2=1 hr
• Weak base
  
  • Treat w/ base–> more readily absorbed
  • Free base or crack cocaine

Clinical use: LA in eye

Toxicity:

• Anxiety
• Paranoia
• General nervousness
• Insomnia
• Psychosis-hallucinations-like schizophrenia
• Seizures
• Vasoconstriction
  
  • Septum can deteriorate
  • Lung damage if smoked
  • These can lead to tissue anoxia and death
• Urticaria-itching→infections
• Decrease in CNS nt→exhaustion
• Cardiac arrythmias
• Fetal damage
  
  • Decrease blood flow to uterus→low birth weight
• Tissue anoxia

Question 2

Caffeine

Answer 2

Mech: Largely unknown-increase cAMP by inh. cAMP phosphodiesterase

Toxicity:

LD50=7.5g

ED50=75

TI=100

• CNS
  
  • Nervousness
  • Insomnia
  • Hand tremors
  • Seizures at very high doses
• Other
  
  • Cardiac arrythmias
• Tolerance and withdrawal
  
  • Chronic poisoning
    
    • Insomnia
    • Tacycardia
    • GI upset
  • Abstention
    
    • Headache
    • Lethargy
    • Irritability

Question 3

(Meth)amphetamine

Answer 3

Indirect acting amine

Mech: Release DA, NE, in CNS

Kinetics: Slow onset (except IV)

T1/2=10hrs

Clinical uses: Narcolepsy, ADHD

Can lead to meth mouth

Question 4

Methylphenidate

Answer 4

aka ritalin

Mech: Inhibit DA reuptake

Kinetics: Slow onset (except IV)

T1/2=10hrs

Clinical uses: ADHD, narcolepsy

Question 5

Modafinil

Answer 5

Other CNS stimulants

Reuptake inhibitor

Question 6

Armodafinil

Answer 6

Other CNS stimulants

Reuptake inhibitor

Question 7

Dexmethylphenidate

Answer 7

Other CNS stimulant

Inhibit DA reuptake

Question 8

Tetrahydrocannabinol

Answer 8

Mech: Binds to cannabinoid receptor

Endogenous THC=Anamdamide

Effects:

• CNS
  
  • Euphoria
  • Antiemetic
  • Decrease intraocular pressure
  • Increased appetite
  • Decrease pain modulating-antinociceptive
• Smooth muscle
  
  • Bronchodilator
  • Dilate conjunctival blood vessels
• Anticholinergic effects-Dry mouth

Toxicity

• TI=1000
• Chronic smokers-lung damage
• Cross placenta
• Don’t operate heavy machinery

Question 9

Dronabinol

Answer 9

Cannabinoid

Antiemetic and appetite stimulant

Question 10

Nabilone

Answer 10

Cannabinoid

Antiemetic and appetite stimulant

Question 11

Nicotine

Answer 11

Effects:

• Short high
• Presynaptic nicotinic receptors
• Increase DA slightly

Pharmacokinetics

• 100micrograms/puff→200 doses a day
• Addiction is easy
• Withdrawal
  
  • Depression
  • Anxiety
  • Irritability
  • Even suicidal