Drug Detail:Pregabalin (Pregabalin [ pre-gab-a-lin ])
Drug Class: Gamma-aminobutyric acid analogs
1. How it works
- Pregabalin may be used to relieve nerve pain and control some types of seizure.
- Pregabalin is thought to work by binding to certain pathways in the nervous system, specifically voltage-gated calcium channels which modulate the influx of calcium into nerves of the central nervous system. This inhibits the release of neurotransmitters such as dopamine, glutamate, norepinephrine, serotonin, substance P, and others.
- As well as having anticonvulsant activity, pregabalin is also thought to affect pain transmission pathways.
- Pregabalin does not bind to GABA or benzodiazepine receptors, even though it is structurally related to GABA.
2. Upsides
- Pregabalin relieves nerve pain and also some types of seizures.
- Used as an anticonvulsant in addition to other anticonvulsants for the treatment of partial-onset seizures.
- May be used in the treatment of neuropathic pain associated with diabetes or spinal cord injury.
- Indicated for the treatment of fibromyalgia and postherpetic neuralgia (nerve pain that occurs following shingles).
- May be used off-label for generalized anxiety disorder, hot flashes, restless legs syndrome, and social anxiety disorder.
- The dosage of pregabalin does not need adjusting in people with liver disease.
- Brand names of pregabalin include Lyrica and Lyrica CR.
- Generic pregabalin is available.
3. Downsides
If you are between the ages of 18 and 60, take no other medication or have no other medical conditions, side effects you are more likely to experience include:
- Edema, dizziness, drowsiness, ataxia (the loss of control of body movements), headache, fatigue, dry mouth, tremor, double vision, and weight gain.
- Sudden discontinuation has been associated with symptoms such as anxiety, diarrhea, headache, increased sweating, sleeplessness, nausea, and increased seizure frequency (in those taking pregabalin for partial-onset seizures). Taper off slowly over at least one week.
- The dosage of pregabalin should be reduced in renal disease.
- May interact with several drugs, particularly those that also have a CNS depressant effect (such as azelastine, antidepressants, antipsychotics, benzodiazepines, and opioid analgesics).
- May not be suitable for some people including those with cardiovascular disease or kidney disease.
- In some countries, restrictions have been placed on the prescribing of pregabalin because of its potential for misuse. Experts rate the addiction potential of pregabalin as higher than that of gabapentin because it is more rapidly absorbed and has a faster onset of action.
- Information about the use of pregabalin during pregnancy is limited. Animal studies using up to 16 times the maximum recommended human dose have reported adverse effects on the offspring such as fetal structural abnormalities and decreased body weight. There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to pregabalin during pregnancy (phone 1-888-233-2334 or http://www.aedpregnancyregistry.org/). Weigh up benefits to the mother versus risks to the fetus. Breastfeeding is not recommended during treatment with pregabalin due to the potential risk of tumorigenicity with pregabalin exposure via breast milk to the breastfed infant.
Note: In general, seniors or children, people with certain medical conditions (such as liver or kidney problems, heart disease, diabetes, seizures) or people who take other medications are more at risk of developing a wider range of side effects. View complete list of side effects
4. Tips
- Pregabalin may be taken with or without food.
- May interfere with your ability to drive or operate machinery or perform other hazardous tasks. Alcohol may enhance this effect.
- See a doctor urgently if you develop any allergy-type symptoms, unexplained bruising or shortness of breath, thoughts about suicide, visual disturbances, or unexplained muscle pain.
- May cause you to gain weight. Talk to your doctor about exercising and make sure you don't consume more calories than you need.
- Do not stop pregabalin suddenly. Talk to your doctor about tapering it off slowly when it comes time to discontinue it.
- Tell your doctor if you are pregnant or breastfeeding before you start taking pregabalin because it may not be suitable for you. If you are planning to father a child, be aware that an association between pregabalin and birth defects has been reported in some animal studies.
5. Response and effectiveness
- Peak concentrations of pregabalin are reached within one and a half hours on an empty stomach or three hours with food. A reduction in seizure frequency or relief from nerve pain may occur within a week of starting therapy.
6. Interactions
Medicines that interact with pregabalin may either decrease its effect, affect how long it works, increase side effects, or have less of an effect when taken with pregabalin. An interaction between two medications does not always mean that you must stop taking one of the medications; however, sometimes it does. Speak to your doctor about how drug interactions should be managed.
Common medications that may interact with pregabalin include:
- anti-anxiety medications, such as diazepam, lorazepam
- antidepressants, such as amitriptyline, citalopram, fluoxetine, paroxetine
- antihistamines, such as chlorpheniramine, promethazine
- antipsychotics, such as aripiprazole, chlorpromazine, haloperidol
- buprenorphine
- heart medications, such as ACE inhibitors (eg, benazepril, captopril, enalapril)
- narcotic pain relievers, such as oxycodone
- propoxyphene
- sedatives or sleeping pills
- some diabetes medications, such as pioglitazone, rosiglitazone
- tramadol.
Note that this list is not all-inclusive and includes only common medications that may interact with pregabalin. You should refer to the prescribing information for pregabalin for a complete list of interactions.