gamma hydroxybutyrate Flashcards
what is GHB and where is it found?
it is a synthetic drug and a natural occurring chemical in the body
found: wine, beef, small citrus fruit, almost all living creatures
where are the prodrugs that are turned into GHB found?
in household products (not inhaled but INGESTED)
where are the highest concentrations of GHB found and lowest concentrations in the brain?
highest: striatum
lowest: cerebellum
where do we see GHB occurring naturally in the body and what does it act as?
- in CNS
- Byproduct of GABA metabolism
- Precursor to GABA, glutamate, glycine
- Similar structure to GABA
- GABAb receptor agonist
what type of schedule drug is GHB?
schedule 1
how are GHB used recreationally?
Club drug: euphoria
Date rape drug: soapy or salty taste OR undetectable
Body builders: growth hormone release during sleep
what is GHB when used instrumentally? what is its schedule? what is its instrumental use?
name: Xyrem (sodium oxybate)
schedule: 3
instrumental use: narcolepsy, opiate/alcohol detox
what is narcolepsy? how does xyrem help with narcolepsy?
Narcolepsy is generally considered a disorder of daytime sleepiness, it also consists of fragmented and nonrestorative sleep.
When given at night time, sodium oxybate, increases the length of night-time sleeping in narcolepsy patients.
As a result of improved night-time sleeping, patients have reduced episodes of sleeping during the day.
what is the most common route of admin?
oral
as a liquid - recreationally
as a pill - instrumentally
rectal, injection, and nasal also are possible
what are the light, common, and strong doses of GHB?
“Light” 5-15 mg/kg
“common” 10-30 mg/kg
“strong” 20-50 mg/kg
what is the absorption?
Rapidly absorbed from the GI tract
- Significant first-pass metabolism so not a lot makes it out
- Bioavailability ~25%
- Peak concentrations with 45 min
what is the distribution?
Readily crosses blood–brain barrier
No depot binding concerns
where is it metabolized? what is it metabolized into?
location: liver
enzyme: GHB dehydrogenase enzyme
metabolite: SSA (succinic semialdehyde)
what is the half life?
30 minutes
what is the timeframe of detecting GHB in an individual’s urine?
4-12 hours post consumption
VERY SMALL TIME FRAME
once synthesized, what does GHB do?
- GHB is stored in the same synaptic vesicles as GABA
- GABA neurons likely release both GHB and GABA
- GHB is transported back into the releasing neuron where it is converted into GABA.
- Therefore, many of the effects of GHB may be attributed to GABA activity.
what is the GHB receptor? where are these receptors found?
receptor: excitatory G-protein coupled receptor
found: hippocampus, cortex, striatum, often on glutamate neurons
in low doses of GHB, what occurs?
it causes stimulant effects… acts as GHB receptor agonist
in high doses of GHB, what occurs?
it causes depressant effects…acts as a GABAb receptor agonist
what type of effects are seen with light and common doses of GHB?
euphoria, happiness, increased sexuality, optimism
Effects are very similar to alcohol and amphetamines!
what effects occur if GHB and alcohol are combined?
SYNERGISTIC EFFECT
Intoxication and memory loss “blackout” - (anterograde amnesia)
Sexual predator victims appear inebriated
what type of effects are seen with high doses of GHB?
coma, bradycardia, respiratory depression, and death
what are the depressant like effects we see at higher doses?
Common (moderate) - Strong doses of GHB cause confusion, drowsiness, significantly impairs balance/ coordination.
Memory loss often occurs after finishing GHB use, rather than during GHB use for ~50% of users.
what is seen in an individual who is overdosing on GHB?
however symptoms vary based on how much GHB was taken and if it was taken with alcohol
Nausea
Decreased blood pressure
Decreased heart rate
Unconsciousness or coma
Respiratory depression
ER visits often due to combined use of GHB with alcohol (non-reactive coma)
what does repeated use of GHB lead to?
development of tolerance and dependence with withdrawal symptoms
does GHB meet the criteria of substance use disorder?
rarely
Acute withdrawal period follows episodes of GHB use. Regular users report: exhaustion, memory loss confusion, clumsiness.
Round the clock use (every 1-3 hours) may create physical dependence resulting in severe withdrawal symptoms 2-6 hours post use.
what are withdrawal symptoms?
Weakness
Tremor
Increased anxiety
Confusion
Seizures
what can GHB reduce?
alcohol withdrawal
