Test 4: Drugs of Abuse pt 2 Flashcards
What kind of drug is Methamphetamine?
-Class 3: Dopamine Transporter
-Synthetic INDIRECT Sympathomimetic
-Works on release of the NTs
-Impacts amount of circulating catechols
-Highly lipophillic
-Onset route dependent (Instant – 30 min)
-DOA: 4-8 hours
-Metabolized in liver & excreted by the kidney
-Neurotoxic (antagonist) to the NMDA receptor
-Tolerance develops quickly, resulting in dose escalation with chronic use.
-5/5 on addiction scale
What is the MOA of Methamphetamine?
-Dopamine transporter is reversed, so more dopamine is exiting the presynaptic membrane.
-Blocks VMAT so that Dopamine cannot be placed into the vesicles
-Dopamine stays floating in the presynaptic membrane, so by concentration gradient, it is released into the synapse
-Results in increased circulating dopamine.
How does Methamphetamine cause different characteristics?
By working on different catecholamines.
-Impact on dopamine seems to be larger, but does hit NE and 5HT3 as well
What are the Dopamine effects of Methamphetamine?
Effects are more aggressive on dopamine than other catecholamines.
-Euphoria
-Abnormal movements
-Psychotic episodes
What are the Norepi effects of Methamphetamine?
Increase arousal
Reduce sleep
Tachycardia
HTN
What are the Serotonin effects of Methamphetamine?
Hallucinations
Anorexia
Hyperthermia
What are withdrawal symptoms of methamphetamine?
Dysphoria
Drowsiness
Insomnia (some cases)
General irritability
Why does teeth decay occur with methamphetamine use?
Due to SNS stimulation = dry mouth.
-Airway hazard.
What is Amphetamine psychosis?
Psychosis can happen with acute or chronic use of crystal meth. Hyperstimulation of SNS.
-Visual & Auditory Hallucinations
-Paranoia
-Self-absorption
-Irritability
-Aggressive & erratic behavior
-Picking at skin
-Insomnia
What kind of drug is Cocaine?
-Class 3 (Dopamine Transporter). Has greater effects on NE than meth.
-Water soluble salt stimulant of the SNS
-Highly addictive (5/5)
-Injected or absorbed by any mucous membrane
-Smoked for instant onset “rush”
Onset/Duration
-Smoking: 6-8 sec. for 20 min.
-IV: 15 sec. for 30-60 min.
-Nasal: 5 min. for 90 min.
How was cocaine used in medicine?
-Local anesthetic
-Dilate pupils in opthamology
-Freud tried to use it to treat depression and alcohol dependence but its high rate of addiction was counterproductive
What is the “cycle” of cocaine use?
Use is cyclical:
-Use
-Euphoria
-Depression
-Craving
Dependence and addiction may develop after only a few uses.
What effects occur with chronic use of cocaine?
Loss of appetite
Hyperactivity
Insomnia
Increased risk for intracranial hemorrhage, ischemic stroke, MI and seizures
OD = hyperthermia, coma, and death
What are withdrawal symptoms of Cocaine?
Similar to but not as strong as that of opioids
-Dysphoria, sweating
-Nausea, vomiting, diarrhea
-Muscle aches, fever
-Lacrimation, rhinorrhea, mydriasis
-Piloerection
-Yawning
How is cocaine metabolized?
-90% by plasma cholinesterases to 2 inactive metabolites
-10% by liver cholinesterases to norcocaine (active)
-Half-life 30-90 min depending on route of administration
Metabolism is so rapid that patient in OR being acutely intoxicated is unlikely.