Description: Anticonvulsive Agent/other, GABA analogue
Gabapentinoid Safety Alert December 2019
The FDA is warning that serious, life-threatening, and fatal respiratory depression may occur in patients using gabapentinoids (Lyrica, Lyrica CR [pregabalin]; Neurontin, Gralise, Horizant [gabapentin]). The risk may be increased with the concomitant use of opioids and other central nervous systems (CNS) depressants, and with conditions such as chronic obstructive pulmonary disease. The elderly are also at higher risk. Health care providers should start gabapentinoids at the lowest dose and monitor patients for symptoms of respiratory depression and sedation when co-prescribing gabapentinoids with an opioid or other CNS depressants (eg, benzodiazepines). Patients with underlying respiratory disease and elderly patients are also at increased risk and should be managed similarly.
Further information may be found at https://www.fda.gov/drugs/drug-safety-and-availability/fda-warns-about-serious-breathing-problems-seizure-and-nerve-pain-medicines-gabapentin-neurontin.”
CSA NA – FDA Approved – REMS (N) – Can Ship
How Does it Work
Gabapentin/Neurontin/Gralise is structurally related to GABA, however, does not bind GABA A/B receptors. Binding sites have been found in the brain presynaptically and the effect on these sites is thought to modulate excitatory neurotransmitters which are involved in both neuropathic pain and seizures.
Indications For Use
Gabapentin/Neurontin/Gralise is officially indicated for focal seizures or post-herpetic neuralgia. It is also commonly prescribed off label for use in alcohol withdrawal/dependence, chronic cough, fibromyalgia, various forms of neuropathic pain, restless leg syndrome, vasomotor symptoms of menopause (may be used for other conditions not listed)
Before starting Gabapentin/Neurontin/Gralise make sure your physician is aware of any allergies or medications you currently take, if you have kidney disease, myasthenia gravis, a history of substance abuse, or are pregnant or breastfeeding
100-1200mg one to three times per day depending on the condition it is used for, efficacy, and patient tolerance to side effects
Pharmacist Tips On Using
How to Take: Follow instructions provided by physician/pharmacy label, swallow whole, take consistently at same times each day unless otherwise directed, store at room temperature
You Need to Avoid: Mixing with sedatives, opioid pain killers, or other CNS depressants may cause decreased breathing rate which can result in overdose related mortality.
Dizziness, drowsiness, ataxia (uncoordinated movement), fatigue
Note this is not a complete list of side effects, only common ones
Frequently Asked Questions
Why do I feel so down/depressed since starting Gabapentin/Neurontin/Gralise? /Why am I having mood swings since starting this medication?
Rarely antiepileptic medications such as gabapentin can cause mood or behavior changes and in severe cases result in suicidal ideation. If you are feeling any of these things or family members are reporting mood or behavioral changes, see your physician immediately to discuss your options as it could be a result of this medication. Many scenarios where gabapentin is used such as chronic pain can also result in these mood or behavioral changes so it is important to be open and honest with your physician about your feelings to make sure they have all of the information to treat you.
My physician has started me on Gabapentin/Neurontin/Gralise, however, I have had no pain relief, why does he want me to continue?
Generally, people are started on low doses that are not high enough to treat pain. Due to the fatigue caused by this medication, it is important to slowly work your way up to slowly build a tolerance to said fatigue. This is true of most medications used for neuropathic pain, so it is a slower process than standard painkillers such as acetaminophen or ibuprofen. The medication will need to be used regularly and may take time to find the correct dose that works for you so work with your physician until you reach your goal. It is important to note that being completely pain free in most cases of chronic pain is not realistic and so it is finding a tolerable level balanced with tolerable side effects.