Stimulants & Psychotomimetics (General) Flashcards
Amphetamine Effects
Locomotor Stimulation
Insomnia
Anorexia
Euphoria
Amphetamine Long Term Effects
If taken repeatedly over a few days
–> Psychotic Symptoms, Anxiety, Depression, Cognitive Impairment
Amphetamine Mechanism
End Goal = Increase DA and NE
4 Methods
1) Block Reuptake (Inhibit DAT and NET)
2) Displace endogenous monoamines in vesicles and move them into cytoplasm
3) DAT and NET work in reverse
4) At high concentrations inhibit MAO
Amphetamine Locomotor and Rewarding Effects
- Cause?
Dopamine Release (Not NA release)
Amphetamine Peripheral Effects
Increase BP/Heart Rate
Reduces Gastrointestinal Motility
Amphetamine Effects of Stopping
Period of deep sleep
When waking up, feel lethargic
Amphetamine Drug of Abuse Effects
- Tolerance to drug’s weight loss effects
- Dependence develops as dose increases
- Uncontrolled binges can cause high risk of acute toxicity
What is more potent synthetic cathinones or natural cathinone
Synthetic derivatives are more potent```````````
Methedrone Mechanism of Action
Increase extracellular 5-HT and DA levels:
- Inhibit reuptake
- Enhance release
Methylphenidate (Ritalin) Mechanism of Action
Inhibits NET and DAT transporters on plasma membrane
Do not enter nerve terminals
–> Does not cause release of NE or DA
Inhibits SERT but at a lower potency
Methylphenidate (Ritalin) Treats What?
Treats ADHD (Kids with ADHD have low dopamine)
Treats Narcolepsy (Increase Hyperactivity to wake up)
Modafinil Treats What?
Treats Narcolepsy
- Improves wakefulness, memory and executive action in sleep-deprived people
Modafinil Mechanism of Action
Blocks Dopamine Reuptake
- Inhibit DAT
Has other CNS effects
Cocaine Effect
Psychomotor Stimulant
Enhances sympathetic nerve activity
Produces euphoria
Local Anaesthetic and a Drug of Abuse
Cocaine Mechanism of Action
Inhibits NET, DAT, and SERT transporters on nerve terminals
Cocaine Adverse Effects
Strong Psychological Dependence (Similar to amphetamine)
Excessive Dosage can cause:
- Tremors, convulsions, cardiovascular events
Can impair brain development and cause fetal malformation
Methylxanthines Effects
CNS Stimulant: Reduces fatigue, improved concentration
Also Causes:
- Diuresis (Urinate a lot)
- Stimulates cardiac muscle
- Relaxes bronchi smooth muscle
Adenosine Mechanism of Action
Adenosine inhibits transmitter release from neurons in the CNS (Greater effect on inhibiting excitatory neurons)
Methylxanthines Mechanism of Action (CNS)
Antagonist of A2 Receptors, prevents adenosine from inhibiting excitatory neurons in CNS
Methylxanthines Mechanism of Action (Cardiac and Bronchi Muscles)
Inhibits PDEs (Break down cAMP) and Increases cAMP
- More cAMP –> Greater stimulation of cardiac muscle and dilation of bronchi muscle
Methylxanthines Mechanism of Action (Diuretic)
Vasodilation of afferent arterioles resulting in increased GFR
Lysergic Acid Diethylamide Effects
Sensory Distortion, awareness that disturbances are caused by drug
Hallucinations can become paranoid delusions
Can cause long lasting psychopathological changes
Lysergic Acid Diethylamide Mechanism of Action
Agonist at 5-HT2A Receptors in Brain
Psilocybin Effects
Similar to LSD
Psilocybin Mechanism of Action
Chemically related to 5-HT
Agonist at 5-HT2A Receptors in Brain
MDMA Mechanism of Action
Ecstasy
Inhibits DA, NA, SERT reuptake/transporters
Euphoria and Rebound Dysphoria
- Inhibition of NA and DA reuptake
Psychomimetic Effects
- Inhibition of 5-HT reuptake
Mescaline Mechanism of Action
Probably by 5-HT Signaling
Ketamine Mechanism of Action
Blocks NMDA Receptor Channel
At Higher Doses:
- Feeling of detachment (Anaesthetic)
- Euphoria
- Hallucinations
- Disorientation
- Numbness
Phencyclidine Mechanism of Action
AKA PCP
Blocks NMDA Receptor Channel
At Higher Doses:
- Feeling of detachment (Anaesthetic)
- Euphoria
- Hallucinations
- Disorientation
- Numbness
Can cause psychotic episodes/schizophrenic attacks
