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154 Cards in this Set
- Front
- Back
What is the definition of drug abuse?
|
Drug abuse is the excessive self-
administration of any substance for nonmedical purposes. |
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What is the definition of reinforcing properties?
|
properties of the drug that are
responsible for drug-seeking behavior |
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What drugs of abuse do not cause addiction?
|
Hallucinogens
Dissociative anesthetics |
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What 4 behaviors characterize addiction?
|
1. impaired control over drug use
2. compulsive use 3. continued use despite harm 4. craving |
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What is a patient that abuses prescribed drugs?
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Medical addict
|
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What is a state of adaptation manifested by a drug class-specific withdrawal syndrome?
|
physical dependence
|
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What 4 things can produce withdrawal?
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1, abrupt cessation
2. rapid dose reduction 3. decreasing blood level of the drug 4. administration of an antagonist |
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Which is a state of adaptation in which exposure to a drug decreases the drug's effect over time?
|
tolerance
|
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What characteristics of the drug are subject to tolerance?
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Tolerance to both:
Desired (euphoria) Undesired (constipation) Tolerance can: Develop slowly (analgesia) Develop more rapid (respiratory depression) |
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What classes of drugs can patients become physically dependent upon?
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Physical dependence is a normal
response that often occurs with the persistent use of certain medications including β-blockers, α2 adrenergic agents, corticosteroids, antidepressants, and other medications that are not associated with addictive disorders. |
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How often do prescribed drugs cause addiction?
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rarely
|
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What is the different between addiction and pseudoaddiction?
|
ADDICTION: Patient with addiction is not in control, uses drugs without regards to proper or legal use, and
continues with no regards to their own or others' safety. PSEUDOADDICTION: Patient with undertreated pain exhibits behaviors that are focused on obtaining meds for pain. When pain is being effectively treated, the behaviors cease. Patient remains in control and uses meds as prescribed. |
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What area in the brain is the prime target of addictive drugs?
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The mesolimbic dopamine system is
the prime target of addictive drugs. As a general rule, ALL addictive drugs activate the mesolimbic dopamine system. |
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Where does the mesolimbic system originate?
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This system originates in the ventral
tegmental area and projects to the nucleus accumbens, the amygdala, and the prefrontal cortex. |
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What are the 3 classes of CNS depressants?
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Ethanol
Benzodiazepines Barbituates |
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What are the 3 classes of psychostimulants?
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Methylxanthines
Cocaine Amphetamines |
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What are the 4 psychedelic agents?
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LSD
Mescaline Psilocibin MDMA |
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What are the 5 classes/drugs that do not fit into a class?
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Nicotine
Opioids Marijuana Inhalants Anabolic Steroids |
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What is the most common liquid drug?
|
ethanol
|
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What does ethanol produce?
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sedation
sleep |
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Is ethanol a depressant or a stimulant?
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depressant
|
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Why do some think its a stimulant?
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because it depresses inhibition in low doses
|
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What 6 cellular functions does alcohol influence?
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GABA-R
Kir3/GIRK channels Adenosine reuptake Glycine receptors NMDA receptors 5HT3 receptors |
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What are the 2 consequences of heavy consumption of alcohol?
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acquired tolerance
physical dependence |
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When does alcohol dependence become apparent (in hours)?
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6-12 hours after cessation of heavy drinking
|
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What are the early sx of alcohol withdrawal (6-12 hours after cessation)?
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more common:
tremor nausea vomiting sweating anxiety agitation less common: hallucinations *visual *tactile *auditory |
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What are the late sx of alcohol withdrawal (24-72 hours after cessation)?
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generalized seizures (24-48 hrs)
delirium tremens (48-72 hrs) **associated with 5-15% mortality |
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What are the DOC for alcohol withdrawal?
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DOC Benzodiazepines:
Diazepam and chlordiazepoxide *long-acting For liver failure or elderly patients: Lorazepam and oxazepam *intermediate acting |
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What are the three drugs approved for tx of alcoholism?
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disulfiram
naltrexone acomprosate |
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How is disulfiram effective?
|
It is an inhibitor of aldehyde
dehydrogenase and creates an aversion to drinking. If ethanol is consumed by a patient who has taken disulfiram, acetaldehyde accumulation leads to nausea, headache, flushing, and hypotension. |
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How is naltrexone effective?
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It is an orally available opioid receptor antagonist with a mild effect on reducing cravings.
|
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How is acamprosate effective?
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It is an NMDA receptor antagonist and
prevents relapse by interfering with the hyperactive glutamate system that persists even after alcohol consumption ceases. |
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What does topiramate do to help with alcohol addiction?
|
Facilitates GABA function and
antagonizes glutamate and may decrease mesocorticolimbic dopamine release and reduce cravings. Antiepileptic. Not FDA approved. |
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What are the most commonly prescribed drugs worldwide?
|
benzodiazepines
|
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What are benzo's main indications?
|
anxiety disorders
insomnia |
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Does benzo cause addiction?
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yes, but rarely
|
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What about benzo dependence?
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2 types:
normal dose high dose |
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How long is the average time for 50% of patients to achieve benzo dependence from therapeutic doses?
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3 years
|
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What is the minimal time to develop tolerance to benzo?
|
1. several weeks - little tolerance - no difficulty in stopping meds
2. several months - proportion of patients developing tolerance increases - withdrawal occurs |
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What are the sx of low dose benzo withdrawal from normal dose dependence?
|
Mild or moderate:
"BRIAN SaVonT" Blurred vision Restlessness Incoordination Anorexia Nausea Sweating Vomiting Tremor |
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What are the sx of high dose benzo withdrawal fro high dose dependence?
|
BRIAN SaVonT
AND seizures psychosis depression |
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What is the treatment for a benzo low dose withdrawal?
|
If patient is on short acting drug:
SWITCH to LONG ACTING DIAZEPAM to reduce the severity of withdrawal and reduce dose over 4-8 weeks. |
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What is the tx for high dose benzo withdrawal?
|
If no other drugs are taken, take
DIAZEPAM or other long-acting benzo. If the situation is complicated by alcohol or other illicit drug, wean off of alcohol or other drug first and then tackle the benzo. |
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How are barbitutates used?
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They aren't!
|
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Where are methylxanthine (MX) compunds found?
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Coffee, tea, cola, chocolate, OTC meds
|
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What are the 3 MX compounds?
|
CAFFEINE (mose widely consumed)
theophylline theobromine |
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What do MX drugs block?
|
adenosine receptors
|
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Where are adenosine receptors located?
|
on presynaptic boutons on many
neurons, including adrenergic neurons |
|
What do adenosine receptors do?
|
all over: inhibit NE release
in the CNS:promote sleep and drowsiness |
|
How does caffeine affect adenosine receptors?
|
Caffeine et al competitively
antagonizes adenosine receptors, removing inhibition, and allowing NE release--> stimulant effects of caffeine in addition to producing alertness and insomnia (from CNS effects) |
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How many cups of coffee is 100-200mg of caffeine?
What are the effects? |
1-2 cups
decrease fatigue increase mental alertness |
|
How many cups of coffee is 1.5g of caffeine?
What are the effects? |
12-15 cups
anxiety tremors |
|
What do very high doses (2-5g) of caffeine stimulate?
What are the effects? |
spinal cord
convulsions |
|
What are caffeine effects on the heart?
|
Positive inotrope and chronotrope
|
|
What are caffeine effects on circulation?
|
Mild diaretic
Increases urinary output of: *Na *Cl *K |
|
What are MX effects on the GI?
|
Stimulate HCl secretion from gastric mucosa (avoid w/peptic ulcers)
|
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When does tolerance to caffeine stimulation happen?
|
rapidly
|
|
So what does the normal person do?
|
Drinks MORE caffeine
|
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What are the withdrawal sx from caffeine?
|
Fatigue
Sedation |
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How addictive is caffeine?
|
VERY (from my experience)
acutally, not listed as an addictive substance WHA?????? |
|
What are 3 AE from caffeine?
|
Insomnia
Anxiety Agitation |
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What are 2 AE from high doses of caffeine?
|
Emesis
Convulsions |
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What is the lethal dose of caffeine?
|
10 g (about 100 cups of coffee)
Cardiac arrhythmias Death (highly unlikely) |
|
On to the big hitters....
COCAINE What is its MOA? |
Inhibits DOPAMINE reuptake
Inhibits NE reuptake Inhibits 5HT reuptake |
|
What is the major outcome of cocaine actions?
|
Potentiates and prolongs CNS and
peripheral actions of those monoamines. In particular, the dopaminergic affect produces the intense euphoria that is characteristic of cocaine. |
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What are the cocaine actions on the sympathetic nervous system?
|
Cocaine also potentiates NE action
and produces a flight or fight syndrome of noradrenergic stimulation: tachycardia HTN pupillary dilation peripheral vasoconstriction |
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What are the other CNS actions of cocaine?
|
1. Stimulation of cortex and brainstem
2. Increases mental awareness and produces a feeling of well-being and euphoria. 3. Involuntary motor activity, stereotyped behaviour and paranoia 4. Irritability and increased risk of violence are found among heavy chronic users. 5. Increases heat production by direct action on thermoregulatory centers in the hypothalamus and increased psychomotor activity. 6. Impairs sweating, cutaneous vasodilation, and heat perception. |
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What are the effects of high doses of cocaine?
|
1. tremors
2. convulsions 3. respiratory 4. vasomotor depression |
|
When are cocaine related deaths more common?
|
In summer, due to direct
thermoregulatory effects and the subsequent strain on cardiac reserve. |
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What 2 methods of administration are the most common for cocaine OD?
|
1. IV administration
2. freebase (crack) smoking |
|
What is found in the urine that would ID a cocaine user?
|
benzoylecgonine
|
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What are the 6 sx of cocaine withdrawal?
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Generally mild:
Dysphoria Depression Sleepiness Fatigue Cocaine withdrawal Bradycardia |
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What is the treatment for cocaine withdrawal?
|
Nothing has shown to be effective.
|
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What are the 2 Class II Drugs by the DEA?
|
Cocaine
Amphetamines |
|
What 4 drugs are in the class of amphetamines?
|
amphetamine
methamphetamine phenmetrazine methylphenidate |
|
What 3 MOA for amphetamines?
|
1. increase release of catecholamines, including dopamine
2. weak inhibition of MAO 3. direct catecholaminergic agonists in the CNS |
|
What are the CNS effects of amphetamines in the CNS?
|
BEHAVIORAL effects similar to
COCAINE (d/t release of DOPAMINE and to a lesser degree NE): 1. increased alertness 2. decreased fatigue 3. depressed appetite 4. insomnia |
|
What are the CNS effects of high dose amphetamines in the CNS?
|
PHYCHOSIS
CONVULSIONS |
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What are 2 clinical indications for amphetamines?
|
Attention deficit disorder AND Narcolepsy can both be tx with:
1. amphetamine 2. methylphenidate |
|
What are the withdrawal sx of amphetamine use?
|
increased appetite
sleepiness exhaustion mental depression |
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What is the tx for withdrawal sx of amphetamine use?
|
Antidepressants
|
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What is the second most common CNS stimulant after caffeine?
|
Nicotine
|
|
What is the second most abused drug after alcohol?
|
Nicotine
|
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What is nicotine's MOA?
|
Full selective agonist of nicotinic receptor
|
|
What does the rewarding effect of nicotine depend on?
|
Stimulation of the ventral tegmental area where nicotinic receptors are expressed on dopaminergic neurons.
|
|
What happens when nicotine excites these neurons?
|
Dopamine is released in the nucleus accumbens and prefrontal cortex.
|
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What are nicotine's actions in low doses?
|
ganglionic stimulation by depolarization
|
|
What are nicotine's actions in high doses?
|
ganglionic blockade
|
|
What are nicotine's specific actions in the CNS?
|
Euphoria
Arousal Relaxation Improved attention, learning, problem solving, reaction time Appetite supressant |
|
What does the nicotine high-dose ganglionic blockade cause?
|
Central respiratory paralysis
Severe hypotension caused by medullary paralysis |
|
What is the amount of nicotine per cigarette?
|
Most cigarettes contain 6-8 mgs of nicotine
|
|
What is the amount of nicotine per cigarette that a person takes in?
|
1-2 mgs
|
|
What is the lethal dose of nicotine?
|
60 mgs
|
|
What percent of inhaled nicotine in smoke is absorbed?
|
90%
|
|
Is nicotine withdrawal mild, moderate, or severe?
|
mild
|
|
What are the sx of nicotine withdrawal?
|
irritability
sleeplessness |
|
Is nicotine addictive?
|
Nicotine is among the most addictive
drugs and relapse is very common. |
|
Can a pregnant/nursing woman smoke?
|
Not advised. Nicotine crosses the placenta and is secreted in breast milk.
|
|
What is nicotine replacement tx?
|
Nicotine is administered by:
transdermal patch gum nasal spray vapor inhaler buccal lozenge |
|
What other drugs are used for nicotine addiction?
|
Buproprion
*mechanism unclear Varenicline *partial agonist at nicotinic CNS receptors |
|
What are the most commonly abused opioids by non health professionals?
|
Heroin
Morphine Codeine Oxycodone |
|
What are the most commonly abused opioids by health professionals?
|
meperidine
fentanyl |
|
Do opioids cause dependence and addiction?
|
yes, strongly
|
|
What does addiction to heroin cause?
|
behavior problems that are
incompatible w/productive life (same as for other short-acting opioids) |
|
Is opioid withdrawal life-threatening?
|
no, but its very unpleasant
|
|
What are the sx of opioid withdrawal?
|
dysphoria
lacrimation rhinorrhea yawning sweating weakness gooseflesh nausea vomiting tremor muscle jerks hyperpnea |
|
What is the detox regimen for opioid withdrawal?
|
Long acting opioid
Dose slowly reduced |
|
What is the DOC for opioid withdrawal?
|
Methadone is preferred
Buprenorphine is next |
|
What is an alternative to using an opioid for opioid withdrawal?
|
Use adrenergic agonists
|
|
What are the 2 presynaptic α2 agonists used for this?
|
Clonidine
Lofexidine |
|
Why do they work?
|
1. Tolerance to opioids in the CNS is
mediated by noradrenergic pathways. 2. Withdrawal leads to a rebound firing of the neurons. 3. A noradrenergic storm results and is responsible for many of the withdrawal symptoms. 4. Clonidine and Lofexidine act as presynaptic α2 agonists, which inhibit this and are able to attenuate symptoms |
|
What is the active ingredient in pot?
|
Δ9-tetrahydrocannabinol
(Δ9-THC, THC, dronabinol) |
|
What are the 2 cannabinoid receptor subtypes?
|
CB1 found in brain
CB2 on immune cells |
|
What type of receptors are CB1 and CB2?
|
G-protein receptors (Gi)
|
|
Activation of CB1 and CB2 receptors leads to what?
|
INHIBITION of adenylyl cyclase
Opening of K+ channels Closing of Ca++ channels |
|
What are the 2 endogenous cannabinoid ligands?
|
anandamide
2-arachidonylglycerol |
|
THC causes euphoria followed by what?
|
drowsiness
relaxation |
|
How does THC affect:
memory? mental activity? muscle strength? motor activity? |
decreases or impairs all of those functions
|
|
What are other effects of THC?
|
appetite stimulation
xerostomia visual hallucinations delusions enhancement of sensory activity |
|
What are THC AE?
|
increased HR
decreased BP reddening of the conjunctiva toxic psychosis (at high doses) |
|
What about tolerance and dependence?
|
mild
|
|
What is therapeutoc THC called?
|
Dronabinol
|
|
What is dronabinol approved for?
|
Anorexia in AIDS
Nausea, vomiting associated w/cancer chemo |
|
What do psychedelic agents affect?
|
thought
perception mood |
|
Do they cause psychomotor stimulation?
|
No
|
|
Do they cause depression?
|
No
|
|
Why not?
|
Psychedelic agents are not stimulants or depressants
|
|
What are the the 3 drugs in the LSD class?
|
LSD
mescaline psilocybin |
|
What are the LSDs similar to?
|
NE, 5HT, Dopamine
|
|
What are the LSDs MOA?
|
Agonists at 5HT2 receptors in the CNS
(remember 5HT2 receptors inhibit dopamine release). |
|
So, why is inhibition of dopamine important?
|
LSDs are not associated with physical
dependence, addiction, or withdrawal (which are mainly effects of increased dopamine). |
|
What do LSDs have?
|
tolerance develops after 3-4 doses
|
|
What are normal dose LSDs AE?
|
Hyperreflexia
Nausea Muscular weakness |
|
What are high dose AE?
|
Long lasting psychoses
|
|
What are the drugs needed to block LDSs hallucinatory effects?
|
Haloperidol and other neuroleptics
|
|
What was PCP introduced as?
|
anesthetic
|
|
Due to AE, what was PCP replaced with as an anesthetic?
|
Ketamine
|
|
What is PCPs mechanism?
|
Non-competitive antagonist at NMDA
subtype Glutamate receptor |
|
What does PCP do at higher doses?
|
inhibits reuptake of dopamine
|
|
What does PCP stand for?
|
phenylcyclidine
|
|
What sx does normal dose PCP cause?
|
Dissociative anesthesia
(insensitivity to pain w/o loss of consciousness) Analgesia Staggered gait Slurred speech Muscular rigidity Behavior can be hostile |
|
What sx does PCP cause at high doses?
|
Anesthesia
Stupor Coma (though eyes remain open) |
|
What is another name for MDMA?
|
ecstasy
|
|
What sx does MDMA cause?
|
Empathy
Intimacy Tachycardia Muscle aches Agitation Hyperthermia Seizures |
|
What is the MOA for MDMA?
|
*similar to amphetamines
*displaces 5HT from presynaptic intrabouton vesicles *preferential affinity for 5HT SERT transporter *reverses action of transporter and pumps out 5HT |
|
What is the affect of a single dose of MDMA?
|
almost complete depletion of 5HT
reserves inside the cell for 24 hours after the single dose |
|
What are the sx of MDMA withdrawal?
|
Mood offset
Depression Lasts several weeks Produces degeneration of serotonergic neurons in rats |
|
What does nitrous oxide inhalant cause?
|
35% N2O mixed with O2
euphoria analgesia loss of consciousness |
|
What does 100% N2O cause?
|
asphyxia
death |
|
Who sniffs volatile organic solvents (VOS) like paint thinner?
|
teen boys from lower SES
|
|
What are the sx of VOS use?
|
exhilaration
light-headedness |
|
What are some toxic effects of VOS?
|
Cancer
Cardiotoxicity Neuropathy Hepatotoxicity |
|
What organic nitrites are abused and what are their sx?
|
Amyl nitrite: dilates smooth mm,
enhances erection, used in angina Butyl nitrite: enhances erection |
|
What are anabolic steroids used for?
|
Used to increase mm size in
body-building competitors. |