Gabapentinoids

Table of Contents

• Definition
• How Gabapentinoids Work
• Common Gabapentinoids
• Mental Health Uses
• What to Expect When Starting
• Benefits
• Side Effects and Risks
• Safety Considerations
• Drug Interactions
• Dosing and Administration
• Stopping Gabapentinoids
• Cost and Insurance
• Monitoring and Follow-up
• Alternatives and Combinations
• Remember
• References

Definition

How Gabapentinoids Work

• Calcium channel blocking - reduces release of neurotransmitters
• GABA-related effects - though they don't directly affect GABA receptors
• Nerve stabilisation - calms overactive nerve signals
• Pain pathway interruption - blocks pain signals from reaching the brain
• Anxiety reduction - through calming effects on the nervous system

In the Brain: Gabapentinoids bind to specific calcium channels in nerve cells, reducing the release of excitatory neurotransmitters like glutamate. This creates a calming effect on the nervous system, which can help with both physical symptoms (like pain) and emotional symptoms (like anxiety).

Common Gabapentinoids

• Original gabapentinoid - first developed in the 1990s
• Multiple daily doses - typically taken 3 times per day
• Kidney elimination - processed through the kidneys
• Generic available - less expensive option
• Shorter duration - effects last 6-8 hours

Pregabalin (Lyrica):

• Newer medication - more potent than gabapentin
• Twice daily dosing - more convenient schedule
• Better absorption - more predictable blood levels
• Controlled substance - has potential for abuse
• Longer duration - effects last 8-12 hours

Mental Health Uses

• Generalised anxiety disorder - especially when other medications haven't worked
• Social anxiety - particularly for physical symptoms
• Panic disorder - as add-on treatment
• PTSD - for hyperarousal symptoms
• Off-label use - not FDA-approved for anxiety but commonly prescribed

Sleep Disorders:

• Insomnia - especially when related to anxiety or pain
• Restless leg syndrome - FDA-approved use for pregabalin
• Sleep maintenance - helps people stay asleep
• REM sleep behaviour disorder - in some cases

Other Mental Health Applications:

• Bipolar disorder - as mood stabiliser add-on
• Alcohol withdrawal - to prevent seizures and reduce anxiety
• Chronic pain with depression - addresses both conditions
• Fibromyalgia - FDA-approved use for pregabalin

What to Expect When Starting

• May feel drowsy or dizzy initially
• Some people notice anxiety relief quickly
• Side effects often improve with time
• Start with low dose, gradually increase
• Take with food to reduce stomach upset

First Few Weeks:

• Full effects may take 2-4 weeks to develop
• Side effects typically decrease
• Dose may be adjusted based on response
• Important to take consistently as prescribed
• Regular follow-up with prescriber

Long-term Use:

• Generally well-tolerated for extended periods
• Regular monitoring by healthcare provider
• Periodic review of continued need
• Gradual tapering if discontinuing
• Kidney function monitoring for gabapentin

Benefits

• Rapid onset - some people feel relief within days
• Physical symptoms - helps with racing heart, sweating, trembling
• Sleep improvement - reduces anxiety-related insomnia
• Non-addictive - gabapentin has low abuse potential
• Flexible dosing - can be adjusted based on needs

For Pain:

• Nerve pain relief - particularly effective for neuropathic pain
• Improved function - better ability to perform daily activities
• Sleep quality - pain relief leads to better sleep
• Mood improvement - less pain often means better mood

General Benefits:

• Well-tolerated - fewer side effects than many alternatives
• Multiple conditions - can address pain, anxiety, and sleep together
• No major drug interactions - generally safe with other medications
• Kidney-friendly - gabapentin is safe for most people with kidney issues

Side Effects and Risks

• Drowsiness - most common, especially initially
• Dizziness - particularly when standing up quickly
• Fatigue - feeling tired or low energy
• Weight gain - can increase appetite
• Swelling - in hands, feet, or legs
• Coordination problems - feeling unsteady

Less Common Side Effects:

• Blurred vision
• Dry mouth
• Constipation
• Memory problems
• Mood changes
• Tremor or shaking

Serious Risks:

• Suicidal thoughts - rare but requires monitoring
• Severe allergic reactions - rash, difficulty breathing
• Respiratory depression - when combined with opioids or alcohol
• Withdrawal symptoms - if stopped suddenly
• Abuse potential - particularly with pregabalin

Safety Considerations

• Tell your doctor about all medications and supplements
• Discuss history of kidney problems
• Mention any substance use issues
• Review mental health history
• Discuss pregnancy or breastfeeding plans

While Taking:

• Don't stop suddenly - taper gradually under medical supervision
• Avoid alcohol - increases drowsiness and breathing problems
• Be careful driving - especially when starting or changing doses
• Monitor mood changes - report any worsening depression or suicidal thoughts
• Stay hydrated - especially important with gabapentin

Special Populations:

• Elderly - may be more sensitive to side effects
• Kidney disease - gabapentin dose may need adjustment
• Pregnancy - discuss risks and benefits with doctor
• Substance use history - pregabalin has higher abuse potential

Drug Interactions

• Opioid pain medications - increased risk of breathing problems
• Alcohol - dangerous combination, avoid completely
• Sedatives - benzodiazepines, sleep medications
• Antacids - may reduce gabapentin absorption
• Morphine - increases gabapentin levels

Generally Safe Combinations:

• Most antidepressants
• Blood pressure medications
• Diabetes medications
• Most antibiotics
• Over-the-counter pain relievers (when used appropriately)

Dosing and Administration

• Starting dose - usually 300mg once daily
• Typical range - 900-3600mg daily in divided doses
• Maximum dose - up to 3600mg daily
• Timing - three times daily with or without food
• Adjustment - increased gradually over days to weeks

Pregabalin:

• Starting dose - usually 75mg twice daily
• Typical range - 150-600mg daily in divided doses
• Maximum dose - up to 600mg daily
• Timing - twice daily with or without food
• Adjustment - increased gradually based on response

Stopping Gabapentinoids

• Never stop suddenly - can cause withdrawal symptoms
• Reduce dose slowly over weeks to months
• Work with healthcare provider for tapering schedule
• Monitor for withdrawal symptoms
• May need slower taper if on high doses or long-term use

Withdrawal Symptoms:

• Anxiety and agitation
• Insomnia and sleep problems
• Nausea and stomach upset
• Sweating and tremor
• Seizures (rare but serious)
• Return of original symptoms

Cost and Insurance

• Gabapentin is available as generic - much less expensive
• Pregabalin generic (available since 2019) - moderately priced
• Insurance coverage varies
• Patient assistance programs available for brand names
• Pharmacy shopping can reduce costs

Typical Costs:

• Generic gabapentin: $10-30 per month
• Generic pregabalin: $50-150 per month
• Brand name Lyrica: $300-500 per month
• Costs vary by dose, quantity, and pharmacy

Monitoring and Follow-up

• Monitor effectiveness and side effects
• Assess need for dose adjustments
• Review other medications and interactions
• Check kidney function if using gabapentin long-term
• Evaluate continued need for medication

What to Report:

• Worsening depression or suicidal thoughts
• Severe dizziness or coordination problems
• Unusual swelling or weight gain
• Breathing difficulties
• Signs of allergic reaction
• Any concerning side effects

Alternatives and Combinations

• Other anti-anxiety medications
• Different classes of pain medications
• Non-medication treatments (therapy, lifestyle changes)
• Combination approaches
• Alternative medications for specific conditions

Common Combinations:

• With antidepressants for anxiety and depression
• With sleep medications for insomnia
• With other pain medications for chronic pain
• With mood stabilisers for bipolar disorder

Remember

References

U.S. Food and Drug Administration. (2024). Gabapentin Drug Information. Retrieved from https://www.fda.gov/drugs/postmarket-drug-safety-information-patients-and-providers/gabapentin-neurontin-information

Peckham, A. M., et al. (2018). Gabapentin for off-label use: Evidence-based or cause for concern? Substance Abuse: Research and Treatment, 12, 1178221818801311. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6134264/

Yasaei, R., & Saadabadi, A. (2023). Gabapentin. In StatPearls. StatPearls Publishing. https://www.ncbi.nlm.nih.gov/books/NBK493228/

Toth, C. (2014). Pregabalin: Latest safety evidence and clinical implications for the management of neuropathic pain. Therapeutic Advances in Drug Safety, 5(1), 38-56. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3952671/

Evoy, K. E., et al. (2017). Abuse and misuse of pregabalin and gabapentin. Drugs, 77(4), 403-426. https://pubmed.ncbi.nlm.nih.gov/28144823/

National Institute for Health and Care Excellence (NICE). (2020). Neuropathic pain in adults: Pharmacological management in non-specialist settings. Retrieved from https://www.nice.org.uk/guidance/cg173