Exam 4: Psychomotor Stimulants, Inhalants, and Hallucinogens Flashcards
What are psychomotor stimulants classified as?
Schedule 2 drugs- meaning they have high potential for abuse but can be used for medical purposes. includes cocaine, methamphetamine, dexedrine, adderall, and ritalin.
What do psychomotor stimulants do?
These are all sympathomimetic drugs meaning they cause sensorimotor activation which increase alertness, heightens arousal, and causes behavioral excitement. All stimulants stimulate catecholamine (NE, Dopamine, Epi) function and some serotonin function.
What act prohibited the over the counter sale of cocaine?
The 1914 Harrison Narcotic Act
What is the pharmacology of cocaine?
- It is fat soluble so easily passes BBB
- Half life is 0.5-1.5 hours
- High lasts around 30 min
What are the 3 NTs that cocaine acts on?
- Dopamine- the euphoric.rewarding effects are related to the blocking of the dopamine reuptake transporter in the nucleus accumbens
- Serotonin
- Norepinephrine
Cocaine inhibits the reuptake of these NTs.
How does cocaine effect the D1 Gs stimulatory receptor?
When cocaine blocks reuptake at D1 dopamine receptors, this is where we see the locomotor and rewarding effects of cocaine.
How does cocaine affect the D3 Gi inhibitory receptor?
When cocaine blocks reuptake at the D3 dopamine receptor, this is where we also see the rewarding effect of cocaine.
What are the acute effects of cocaine administration?
It is a sympathomimetic drug so it acutely produces symptoms related to sympathetic nervous system activation. Includes increased heart rate, vasoconstriction, hypertension, and hyperthermia.
Acute exposure can lead to sensitization that can last for a few weeks to a year in humans.
What are the chronic effects of cocaine usage?
10-15% of recreational users become dependent. These individuals show abnormal prefrontal cortical functioning which manifests as deficits in inhibitory control.
Chronic exposure leads to tolerance which is typically seen in the euphoric effects in humans.
Is there any FDA approved treatment for psychomotor stimulant dependence?
No. There is a contingency management program that can help. It is based on the premise that drug taking is an operant response that persists as a result of reinforcement. Even more effective when combined with the SSRI Citalopram.
What are the majority of ampethamines classified as?
Schedule 2 drug. High potential for abuse with well known medicinal value.
What are the two plants compounds that are similar to amphetamines?
- Cathinone- active ingredient is khat. Mephedrone is a derivative of this and was sold as bath salts. Legal until 2011.
- Ephedrine- from the herb Ephedra vulgaris. FDA banned sale of supplements with this compound in 2004 because it elevates BP and increases risk of heart attack and stroke.
How were amphetamines initially used?
Used as anti-asthmatic first and then narcolepsy. Pilots took it in WWII to stay awake. After WWII, usage soared and peaked around 1970s.
What is the pharmacology of amphetamines and methamphetamine?
- They are metabolized by the liver at a slow rate.
- Oral admin- 10-16 hour half life. High lasts 8 hours.
What is the mechanism of action in which amphetamines exert their effects?
It acts like an indirect agonist of the catecholaminergic system.
1. It enters dopamine, NE, and serotonin nerve terminals via uptake by dopamine transporter, NET, or serotonin transporter and causes the vesicles to release more of that NT.
2. It reverses the reuptake transporters making dopamine, NE, and serotonin be pumped out instead of taken back up.
3. Some amphetamines inhibit the monoamine oxidase enzyme preventing breakdown of the NT.
Amphetamines also have _____________ symptoms like what we see with cocaine.
Sympathomimetic. Lead to release of NE in brain and sympathetic nervous system.
What are amphetamines used to treat?
It is used to treat attention deficits.
Why do amphetamines help with ADHD?
In those with ADHD, there is abnormal functioning of the prefrontal cortex and possible hypofrontality. The neurons in the prefrontal cortex are innervated by noradrenergic and dopaminergic systems. By using these drugs and increasing the concentration of NTs, we can improve symptoms of ADHD.