Stimulants, Anorexigenics, + Hallucinants Flashcards
Which transporter does cocaine act on and what does it go?
DAT - prevents reuptake into the presynaptic cleft of dopamine, serotonin, and NE
What are the two functions of amphetamines?
1) compete with dopamine for uptake
2) compete w/ DA for VMAT -> dopamine released non-vesicularly
Which drug mech is the synthetic cathinones most similar to?
Amphetamines - Stimulate monoamine neurotransmitter release and inhibit reuptake
What happens if cocaine is administered systemically?
Increase in BP, HR, and heart contractility
coronary artery vasoconstriction
How long is the half life for cocaine?
1 hr (less if smoked or IV)
What metabolite of cocaine and for how long does it stay in your system after a binge?
Benzoylecogonine - 1 week
How does the nucleus accumbens react to the repeated exposure to cocaine and amphetamine-like drugs?
Anticipation - sensitization causes an earlier more intense peak (can even happen with saline)
What is the only drug labeled for obesity treatment?
Phentermine
What happens in stimulant withdrawal?
‘Crash’ period - depression, anxiety, agitation and craving
How long can stimulant craving last and what sets it off?
Craving can last for years after abstinence and can be set off by familiar people, places, or stressful situations (PTSD-like)
What happens after the crash period of stimulant withdrawal?
Intermediate period - fatigue, loss of energy and affect
What does amphetamines do to heart rate and why?
Induces a bradycardial reflex because it is increases blood pressure
How is cocaine metabolized?
Ester hydrolysis
How are amphetamines excreted?
Renal - unchanged
What is used to treat ADHD?
Amphetamines and methylphenidate
What is modafinil used for?
1) Narcolepsy
2) Adjunct for OSA
3) Shift work sleep disorder
Which patient population should not take modafinil?
Cardiovascular problems - MI, unstable angina, LVH
Modafinil adverse reactions
Headache
Nausea
Hypersensitivity
Drug interactions
Caffeine use
idiopathic apnea of prematurity
Acute resp depression (not first line)
What mech does caffeine have at high concentrations?
Inhibits phosphodiesterase
Does caffeine have substance dependence?
No
Effects of nicotine
Arousal Relaxation Attention Reaction time Enhances mood
Peripheral effects of nicotine
Increases BP
Increase HR
Vasoconstriction
Increases cardiac output
What type of learned behavior is precipitated in nicotine replacement therapy?
Positive reinforcement to curtail tobacco use
What are the three major groups of hallucinogens?
1) 5HT-2A partial agonists
2) Muscarinic antagonists
3) Glutamate antagonists
In which cells are 5HT-2A receptors found mostly?
Cortical pyramidal cells (prefrontal cortex)
Which drugs bind at the 5HT-2A receptor?
LSD and MDMA
What are some side effects of 5HT-2A partial agonists?
Flashbacks (~4%) and bad trips (anxiety, depression and paranoia)
What receptor does PCP act on? What else acts here?
It is an NMDA antagonist. Ketamine also acts here
Peripheral effects of LSD and other hallucinogens?
Mydriasis
Increased BP
Increased HR
What happens to serotonergic neurons exposed to MDMA?
Degeneration
Adverse effects of PCP
Paranoia Hostility (combative behavior) Increased BP, HR, sweating High risk of addiction Numb and loss of pain sensation
What population is the synthetic cannabinoid used in?
Dronabinol is used to help anorexia in AIDs patients
Nausea in chemotherapy patients
What receptors does THC act on and how?
Agonist at CB1 and CB2 at the presynaptic axon
How does CB1 work?
Gi/o coupled G protein inhibits adenylyl cyclase
What causes the large volume of THC distribution?
HIgh lipid solubility
What toxicities are caused by whippets?
Bone marrow suppressoin Chemical pneumonitis, coughing, and wheezing renal tubular acidosis arrhythmias cerebellar degeneration
