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Questions and Answers
What is the class of prescribed agents that have a high risk for misuse, abuse, and dependency?
What is the class of prescribed agents that have a high risk for misuse, abuse, and dependency?
- Gabapentinoids (correct)
- Anticonvulsants
- Opioids
- Benzodiazepines
What is the primary mechanism of action of pregabalin?
What is the primary mechanism of action of pregabalin?
- Binding to benzodiazepine receptors
- Binding to and blocking α2-δ subunit of voltage-gated calcium channels (correct)
- Binding to GABA receptors
- Inhibiting the release of glutamate
What is the main difference between pregabalin and gabapentin?
What is the main difference between pregabalin and gabapentin?
- Pregabalin is more effective in treating epilepsy
- Gabapentin is more effective in treating anxiety disorders
- Pregabalin has a faster onset of action
- Pregabalin is 6 times more potent than gabapentin (correct)
What is a common off-label use of gabapentinoids?
What is a common off-label use of gabapentinoids?
What is the total sales of pregabalin worldwide in 2013?
What is the total sales of pregabalin worldwide in 2013?
What is the effect of pregabalin on excitatory neurotransmitters?
What is the effect of pregabalin on excitatory neurotransmitters?
What is the effect of gabapentin administration on GABA concentration?
What is the effect of gabapentin administration on GABA concentration?
Why does pregabalin produce an euphoric effect?
Why does pregabalin produce an euphoric effect?
What is a psychotropic effect of pregabalin?
What is a psychotropic effect of pregabalin?
What is a side effect of pregabalin overdose?
What is a side effect of pregabalin overdose?
What is a withdrawal symptom of pregabalin?
What is a withdrawal symptom of pregabalin?
How should pregabalin dependence be treated?
How should pregabalin dependence be treated?
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Study Notes
Gabapentinoids
- Gabapentinoids (pregabalin and gabapentin) are a class of prescribed agents with a high risk for misuse, abuse, and dependency.
- They are used to treat epilepsy, neuropathic pains, generalized anxiety disorder, and fibromyalgia.
- Off-label uses include treatment of bipolar disorder, alcoholic/narcotic withdrawal state, ADHD, and migraine.
Pregabalin
- Pregabalin is an analog of γ-aminobutyric acid (GABA) but does not bind directly to GABA or benzodiazepine receptors.
- Total sales of pregabalin worldwide reached $5 billion in 2013.
- Pregabalin is 6 times more potent than gabapentin and has higher binding affinity at their receptors.
- Oral pregabalin has rapid absorption and higher bioavailability.
Pharmacology of Pregabalin
- Pregabalin binds to and blocks α2-δ subunit of voltage-gated calcium channels on neurons, decreasing excitatory neurotransmitters (e.g., glutamate, noradrenaline, and substance P).
- Pregabalin has GABA-mimetic activity, inhibiting GABA metabolism and altering neuronal GABA transporters.
- Gabapentin administration increases GABA concentration by about 50%.
Psychotropic Effects of Pregabalin
- Pregabalin is considered an ideal psychotropic drug for recreational purposes, producing sedation, euphoria, improved sociability, marijuana-like high/relaxant effect, opioid-like sedative effects, and dissociative/psychedelic effects.
Pregabalin Overdose and Withdrawal
- High doses of pregabalin cause sedation, suicidal ideation, dizziness and somnolence, impaired driving, respiratory depression, and death.
- Withdrawal symptoms include anxiety, depression, agitation, nausea, palpitations, insomnia, hyperhidrosis, and diarrhea.
Pregabalin in Addiction Treatment
- Pregabalin has beneficial effects in managing addiction to various drugs, including alcohol, benzodiazepines, opioids, and cannabis.
- Treatment of pregabalin dependence involves discontinuation by tapering the dose and administration of CNS depressants to control withdrawal symptoms.
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