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90 Cards in this Set
- Front
- Back
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3 methods to inactive neurotransmitter (catecholamie)
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1) Reuptake
2) MAO 3) COMT (requires Mg and SAMe) |
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NE will be... by MAO
DA will be .... |
REDUCED
OXIDIZED |
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MAOA acts on..
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NE and 5HT
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MAOB acts on..
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phenylethylamines
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What distinguishes gaba from other neurotransmitters?
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It can be stored in Glia
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Define GABA A Receptor
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inhibitory, more abundant than B
Ionotropic permeable to chloride |
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Define GABA B receptor
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G protein coupled
Metabatropic Linked to K or Ca Slow inhibitory post synaptic potentials Decrease calcium conductance Facilitate opening of K channels Inhibit adenylcyclase |
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2 ways to synthesize glutamate
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Transamination of alpha oxoglutrate
Glutamine --> glutamate via glutaminase |
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3 types of GLU receptors
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NMDA
AMPA Kainate |
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Kainate is found where..
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hippocampus, cerebellum, and spinal cord
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3 types of CNS stimulants
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Psychomimetic
Psychomotor: Cocaine, Amp, Adderol Convulsant (respiratory stim.) |
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2 drugs used to deplete system of DA, and the conclusion
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6-OHDA (neurotoxic). Taken up mostly by DA. can demonstrate that amphetamine behaviors can be abolished..
Alpha OH tyrosine:will form false transmitter which will stop synthesis |
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Amphetamine psychosis
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resembles schizophrenia: hallucinations, paranoia, stereotype behavior
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What can you treat amphetamine psychosis with?
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pysychotomimetics. Block DA receptors so that DA in cleft wont activate it.
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What will increase the rate of excretion for amphetamine?
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decrease the pH of the urine
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Does meth work for depression?
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Not severe. Maybe mild.
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What is amphetamine synthesized from?
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Epinephrine
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Half life of Meth
Half life of Cocaine |
12 hrs
1 hr |
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Is meth neurotoxic?
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Dose dependent neurotoxicity
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Is cocaine neurotoxic?
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No neurotoxicity
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MDMA is an analog of...
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Amphetamine
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Side effects of serotonin syndrome?
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anxiety
irritability decrease in libido decrease in appetite decrease in mental ability impulsive and agressive |
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MDMA and the effect on 5HT
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for the first 24 hours 5HT stores are severely depleted.
Cerebral concentrations decrease |
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Does MDMA demonstrate neurotoxicity?
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YES to 5HT neurons
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MDMA inhibits..
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Tryptophan hydroxylase and MAO
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Characteristics of hallucinogens?
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Most involve Serotonin
Divided self environment-beautiful Increase in sensory awareness attention-great meaning |
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Areas with large concentrations of 5HT receptors?
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GI
Blood vessels Platelets Nerve endings (mediate pain) Cortex, hippocampus, neostriatum, caudate, |
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How does MDMA get into neuron?
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5HT-Uptake receptor
DA-diffusion |
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Decreasing TRPOH will influence..
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Body temperature
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Is MDMA neurotoxic?
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Yes. It involves free radicals.
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Aggregation Toxicity
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Social environment could be crucial to the toxic response of the drug (Raves)
Elevated temperature, external noise, and dehydration worsened the effects |
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Behavioral responses to serotonin syndrome
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Defecation
Ejaculation Head bobbing Paw threading Penile erection Salivation Hyperactivity pileerction |
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Onset of action of MDMA
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20-60minutes
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Duration of MDMA
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5 hours
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peak of MDMA
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60-90 minutes
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half life of MDMA
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24 hours
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9 acute effects of MDMA in humans
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Inc in HR and BP
Nausea and chills Sweating Bruxism Hyper reflexia Muscle aches Nystagnis Insomnia |
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Primary mechanism of cocaine
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blocks the DA transporter
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6 Effects of Cocaine
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Inc in BP, HR, Cardiac Output
Inc in locomotor activity Inc in euphoria Inc in excitement, enhances pleasure Stereotype behavior Increases sympathetic activity |
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Withdrawal symptoms of cocaine
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Paranoia, anxiety, depression, insomnia, anorexia,
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Duration of action of IV dose of cocaine
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only 30 minutes
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4 adverse effects of cocaine
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cardiac arrhythmias
cerebral and coronary thrombosis heart failure |
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How does cocaine alter fetal development?
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inhibits formation of oligodendrocytes which are important for the formation of myelin
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3 things that will influence relapse and drug seeking
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1) Exposure to self administration
2) Exposure to stressors 3) Exposure to drug taking stimuli |
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what is a potent primer of cocaine?
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Sugar
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activating D1 receptors will do what to cocaine seeking?
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attentuate it
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Activating D2 receptors will do what to cocaine seeking?
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Increase it
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Why do stressors induce drug seeking?
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Because they activate the mesolimbic dopamine pathway
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Caffeine is a competitive inhibitor for?
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A2A receptors which are negatively coupled with D2 receptors
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D1 agonist will do what to cocaine?
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Block reinstatement
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D2 antagonists will do what to cocaine seeking?
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Will reduce it
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Name 4 cross over reinstatements
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Amphetamine <--> Cocaine
Heroin <--> morphine/methadone Barbs <---> sedative hypnotics Looking for cocaine, cant find, any of the morphine, methadone, heroin will work and will reinstitute cocaine seeking behavior. However it will not work in other direction. (amphetamine --> morphine) |
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What were some drugs that they tried to solve cocaine addiction?
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Methadone (but had to use near lethal dose)
GBR: uptake inhibitor (didnt work longterm) Modafinil Ibogaine |
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What is the dose response curve of benzodiazepines used for insomnia?
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Steep dose curve
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what is the dose response curve of benzodiazepines used for anxiety?
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shallow dose curve (affective over wide ranges)
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5 classes of drugs for anxiety
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1) Benzodiazepines
2) 5HT 1AR Agonists 3) Barbiturates 4) Beta Adrenoreceptor antagonists 5) miscellanous 3) |
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Paradoxial effect is often seen in...
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Benzos like valium and short acting benzos
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Benzodiazepines are metabolized how..
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Microsomal enzyme system in the liver will turn it into water soluble metabolites
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Half life of barbiturates
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18-48 hours
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Half life of phenobarb
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4-5 days
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Half like of fluorazapam
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(benzo for insomnia)
100 hours |
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How to increase the rate of elimination of benzos?
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Increase the pH of the urine
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Primary site of action of barbiturates
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Hippocampus
Amygdala Posterior Hypothalamus midbrain reticular formation |
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Primary site of action of benzodiazepines?
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Limbic system
Thalamus Midbrain reticular formation |
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Sedative hypnotics, and their role in sleep
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They induce sleep but
1) Less REM sleep 2) More non-REM sleep 3) Latency to sleep is decreased |
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What are some examples of anti-convulsants?
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1) Phenobarbiturate
2) Diazapam 3) Nitrazepam: infantile spasms |
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Negative effects of benzos?
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Decreases respiration and cardiovascular system. But not trivial.
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Benzo effect on those with digestive heart failure
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1) Decrease in myocardial contraction
2) Decrease in tone |
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Withdrawal of benzos
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Physiological and psychological
Similar to neurotic person |
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Barbiturates produce tolerance by...
Benzos produce tolerance by.. |
1) inducing hepatic enzymes
2) Producing changes at the receptor level |
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Benzo effects when withdrawn
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Increase in anxiety
Severe tremors Dizziness Early morning insomnia Short acting: produce worse withdrawal |
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What effected the withdrawal from benzodiazepines?
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1) Abrupt or Gradual
2) Duration 3) Long acting vs short acting |
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What did not effect the withdrawal from benzodiazepines?
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Personality type, age and dose
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4 things done for barbiturate poisoning
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1) Pump Stomach
2) Support respiration 3) Support cardiovascular system 4) Increase pH with alkaline to increase rate of elimination |
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What happens if treatment is not present for someone with barb. poisoning.
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Hypotensive --> shock --> cardiovascular collapse -->renal failure and then death
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CNS effects of amphetamine?
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Increase locomotor activity
Increase in excitement/euphoria Anorexia Stereotype behavior Increase alertness |
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Peripheral effects of amphetamine?
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In in BP, Increase in HR, increase in cardiac output, decrease in GI motility
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Reasons they used amphetamine?
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Narcolepsy
ADHD/ADD |
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Withdrawal of ampthetamine
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Psychological withdrawal, not physical. Often suicidal due to depletion of DA.
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How is amphetamine taken?
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IV, snorted, orally
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CNS effects of methamphetamine?
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Increase locomotor activity
Anorexia Euphoria Stereotype behavior Increase libido increases energy and mood |
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Negative symptoms of methamphetamine?
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Dry mouth
Increase in libido Increase in temperature of internal organs Generalized hyperthermia Decrease in 02 to the extremities Decrease in appetite increased activity Nausea/vomiting hallucinations Cardiac arrhythmias Itching Paranoia Anorexia Increase in irritability |
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1/2 life of methamphetamine
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12 hrs
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CNS effects of MDMA
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increases locomotor activity
increases temperature serotonin syndrome |
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Negative symptoms of MDMA
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Hyperthermia can lead to kidney failure and protein/muscle degredation
Acute effects: increase in HR/BP, nausea, chills, sweating, bruxism, nystagnis, insomnia |
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CNS effects of Cocaine
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Increase in locomotor activity
increase in euphoria increase in excitement magnifies pleasure, stereotype behavior |
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Negative symptoms of cocaine
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Hallucinations, paranoia, dellusion, anxiety. With increased dose you can get tremors, convulsions, respiratory depression, vascular collapse, death.
Cardiac arrhythmias, coronary and cerebral thrombosis, heart failure, alters fetal development |
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1/2 life of MDMA
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24 hours
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Duration of MDMA
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5 hours
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Onset of action of MDMA
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20-60 minutes
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