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63 Cards in this Set
- Front
- Back
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What is a very small molecule that is structurally similar to the catecholamines?
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Amphetamine
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What is the chemical nature of Amphetamine?
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A Weak base
-Most are a-methyl phenethylamine derivatives |
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How is Amphetamine absorbed?
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Orally
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How is Amphetamine cleared from the body?
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-Metabolized to Benzoic Acid predominantly
-Excreted unchanged |
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What will increase the excretion of Amphetamine?
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Acidic urine
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What is the halflife of Amphetamine (how does it compare to cocaine's)?
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4-6 hrs
MUCH LONGER than cocaine's |
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Why is the halflife of Amphetamine so much longer than Cocaine's?
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Because there are no plasma esterases that metabolize Amphetamine in the plasma.
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What are the 4 pharmacological mechanisms of action of Amphetamine and Methamphetamine?
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-Promotes RELEASE of NE/DA/5HT
-Blocks REUPTAKE of NE/DA/5HT -Partial alpha agonist -MAOI at high doses |
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Why do Amphetamine and Methamphetamine act as partial agonists of alpha receptors?
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Because they are very structurally similar to NE
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What is the predominant NT that is mimicked by
-Amphetamine -Cocaine |
Amphetamine: Norepinephrine
Cocaine: Dopamine |
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What are the 7 main pharmacological effects of Amphetamine and Methamphetamine?
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WEIRDPE
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What is WEIRDPE?
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-Wakefulness/Alert/Less fatigue
-Elevated mood/self-confidence -Increased motor/speech -Respiratory stimulation -Decreased appetite -Peripheral sympathomimetic -Enhanced athletic/intellect performance |
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What is the drawback to the ability of Amphetamines to decrease fatigue and increase wakeful/alertness?
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You can get more done, but with more errors and less quality.
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What is the drawbackk to Amphetamine's ability to increase intellectual performance?
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The learning is situational - you have to be high on meth as you're taking the test to remember what you studied while you were high on it.
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What are the 3 specific sympathomemetic agents to know? Which are used clinically?
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-Amphetamine (used clinically)
-Methylphenidate (used clinically) -Methamphetamine (NOT used clinically) |
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So the 2 drugs that are used clinically are:
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-Amphetamine
-Methylphenidate |
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What is Methylphenidate?
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Not technically an amphetamine, but structurally and mechanistically very similar.
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Why isn't Methamphetamine used clinically?
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It is always a drug of abuse.
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What are the 2 main clinical uses of Amphetamine and Methylphenidate?
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-Narcolepsy
-Attention-deficit Hyperactivity Disorder |
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What is Narcolepsy?
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Daytime sleep attacks
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What limits the use of Amphetamine and Methylphenidate for treating narcolepsy?
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-Risk of abuse
-Tolerance development |
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What is generally needed when Amphetamine and Methylphenidate are used for treating ADHD in kids?
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Several doses per day
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How effective are Amphetamine and Methylphenidate in treating ADHD?
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Good - very effective
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If children with ADHD are already hyperactive, why would you want to increase their sympathetic activity?
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Because it increases their FOCUS
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What are 5 acute, pharmacologic side effects of Amphetamine and Methylphenidate?
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ASIFA
-Abdominal pain -Suppression of growth -Insomnia -Fever -Anorexia/weight loss |
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What are 5 toxic results of longterm illicit use of amphetamines/methylphenidate?
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-Psychosis
-Acute toxicity -Neurotoxicity -Abuse liability -Methmouth |
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How does chronic use of amphetamines produce psychosis?
How does this effect compare to that caused by cocaine? |
By excessive activity of DA due to increased release and decreased reuptake; Psychosis is worse w/ amphetamines than cocaine.
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What are 4 symptoms of acute amphetamine toxicity due to illicit use?
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-Dizzy
-Increased HR, SNS activity -Restless -Tremor |
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How does the longterm neuronal degeneration and permanent intellectual damage caused by Amphetamines compare to cocaine?
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Much worse!
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How does the abuse liability of meth compare to cocaine?
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Much much harder to stop meth than cocaine
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What increases the abuse liability of meth?
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Smoking or IV administration
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What is the naturally occurring alkaloid in tobacco products?
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Nicotine
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How is Nicotine administerd?
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Self-administered by chewing tobacco, smoking, or snuff
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What is the mechanism of action of Nicotine?
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Nicotinic cholinergic agonist
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At what 3 sites are Nicotinic cholinergic receptors located?
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-NMJ
-Autonomic ganglia -CNS receptors |
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What is the effect of Nicotine at the neuromuscular junction?
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No effect
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What effect does Nicotine have at the autonomic ganglia and which predominates?
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SNS - increases EPI release
PNS - increases ACh release - predominates |
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What sx does activation of PNS ganglia by nicotine result in?
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GI effects - nausea and increased intestinal motility
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Where are nicotinic receptors found within the CNS?
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Many locations ie Nu: accumbens
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What ARE nicotinic cholinergic receptors?
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Monovalent Cation channels (Na/K)
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What does the activation of nicotinic receptors produce?
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EPSP - membrane depolarization
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What are the 2 main pharmacologic actions of Nicotine?
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-CNS stimulant
-Muscle relaxant |
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What is the main result seen by Nicotine stimulation of the CNS?
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Increased alertness
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Why is Nicotine so reinforcing?
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It increases DA release in the limbic reward centers (nucleus accumbens)
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What is a common result of first exposure to nicotine?
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Activation of the CTZ causing nausea
(chemoreceptor trigger zone) |
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What is more rewarding; a single dose of cocaine or nicotine?
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Cocaine
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Why is the abuse liability of nicotine so much higher than nicotine?
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-Reaches the brain in 7 sec
-Increases DA signaling/reward pathway -Each puff (10/cig) is an individual reward |
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What are 3 environmental factors that become associated with the reward of nicotine?
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-Setting (bars)
-Time of day (after dinner) -Preparation (sight of ashtray) |
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What is the very fast tolerance to nicotine that develops over a very short time period called?
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Tachyphylaxis
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So what are 2 issues that make it very difficult to quit using nicotine?
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-Psychological dependence - brain craves its reward
-Physical dependance - withdrawal symptoms occur |
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What are 5 withdrawal Nicotine symptoms that occur?
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-Depression
-Increased appetite/lb gain -Difficulty concentrating -Irritability -Anxiety |
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What is the most dangerous thing about nicotine?
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The consequences of smoking it on health.
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How can the psychological dependence/physical dependence on nicotine be treated?
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By REPLACING the nicotine
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What are 3 types of active nicotine replacement formulations?
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-Gum
-Nasal spray/inhaler -Lozenges |
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What is a passive nicotine replacement formulations?
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Patches
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What is the bad thing about nicotine replacement?
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Only 20% are abstinent for one year
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What are 2 non-nicotine pharmacotherapies for nicotine dependence?
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-Bupropion
-Varenicline |
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What is Bupropion? How does it treat nicotine dependence?
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An antidepressent
-Reduces cravings -Lessins withdrawal symptoms (esp depression) |
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How is Bupropion given for txmt of nicotine dependence? What are 2 side effects?
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As a sustained release prep
Side effects = drymouth/insomnia |
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What is the mechanism of Varenicline?
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Partial agonist of nicotinic receptors
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How does partial activation of nicotine receptors by Varenicline reduce craving?
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-By activating the nicotinic receptors w/o desensitizing
-By blocking the effects of nicotine if patient smokes |
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So what is more efficacious in treating nicotine addiction; Varenicline or bupropion?
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Varenicline
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What are 4 side effects of Varenicline?
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-Nausea
-Insomnia -Constipation -Headaches |
