Pregabalin

Pregabalin, commonly branded as Lyrica, is a medication initially developed for managing epilepsy but has since been used to treat other conditions such as neuropathic pain, fibromyalgia, and generalised anxiety disorder.¹

Historically, pregabalin is a member of the gabapentinoids drug class, which includes gabapentin.² These drugs were formulated to mimic the neurotransmitter GABA, although they do not directly bind to GABA receptors. Instead, pregabalin binds tightly to the alpha2-delta site, a specific auxiliary subunit of voltage-gated calcium channels in the central nervous system.³ By doing so, it modulates calcium influx at nerve terminals and reduces the release of neurotransmitters, such as glutamate, noradrenaline, and substance P.

In terms of effects, pregabalin acts predominantly on the central nervous system. The medication often produces sensations of calmness and relaxation and is used for varying types of neuropathic pain, as well as anxiety disorders. Some users also report significant decreases in symptoms related to their conditions, such as nerve pain or seizures, although efficacy can differ among individuals. ⁴

However, pregabalin comes with a range of side effects. Short-term side effects may include dizziness, drowsiness, and occasionally, weight gain.⁵ More severe side effects, like respiratory depression, can occur, particularly when the drug is consumed in high doses or combined with other central nervous system depressants like alcohol or opioids.

In summary, pregabalin is a multi-purpose drug with varied applications, from treating epilepsy to managing pain and alleviating anxiety. Despite its effectiveness, it also has a range of side effects and risks, including the potential for misuse and dependency.⁶ As such, it should be used cautiously and always under medical supervision.

Appearance

Pregabalin is most commonly available as oral capsules or tablets. These capsules are often white or off-white and may vary in size depending on the dosage. They can also bear identifying imprints, such as the brand name or dosage information.¹ Some versions may include coloured bands or markings to facilitate easier identification.⁷

Tastе

As pregabalin is generally encapsulated or tableted for oral use, it is designed to be swallowed whole, which makes its taste largely irrelevant from a medical standpoint. However, pregabalin is also available as an oral solution, which may contain additives or artificial flavours to make it more palatable. However, the specific taste can vary depending on the manufacturer.⁸

Smell

There is limited information regarding the smell of pregabalin. This is likely because pregabalin, as a medication, is not designed to engage with olfactory senses. Its intended function is internal, typically either ingested orally or used intravenously in hospital settings. Therefore, medical guidelines generally do not provide details about the smell of the medication.³

The dosage of pregabalin varies depending on the medical condition being treated and individual factors such as age, kidney function, and other medications being used. The following are general guidelines:

• Minimum to Feel Something (mg)
  The starting dose for treating conditions like neuropathic pain, fibromyalgia, or epilepsy usually ranges from 25 mg to 50 mg, taken two to three times a day.⁴
• Low Dose
  A low dose typically refers to daily dosages ranging from 50 to 150 mg, usually split into two or three doses. ⁹
• Common Dose
  The most commonly prescribed dosage usually falls between 150 mg to 300 mg daily, depending on the treated condition. This is often split into two or three doses.
• High Dose
  High doses can reach 600 mg daily, usually divided into two or three doses. Such high doses are typically reserved for severe conditions and should only be taken under close medical supervision to monitor potential side effects.³

Notes on What May Happen When Exceeding the High Dose

When high doses of pregabalin are exceeded, the risk of severe adverse effects increases substantially. Overdose symptoms may include severe drowsiness, confusion, agitation, and restlessness. In extreme cases, it could lead to respiratory failure, unconsciousness, or even death. Overdose is a medical emergency, and immediate treatment is necessary. Often, overdosing can lead to complications when combined with other substances like alcohol or opioids. If the kidneys are compromised, the drug may accumulate in the body, leading to toxicity. Patients with a history of drug or alcohol misuse are at a higher risk of overdose. Prolonged high doses can also lead to an increased risk of developing tolerance, dependence, and potential misuse. Medical professionals usually recommend starting with lower doses and carefully monitoring the patient to avoid overdose scenarios. ^3,6

Pregabalin is primarily used for its anxiolytic, analgesic, and anticonvulsant effects. Patients generally report feeling relief from pain and a decrease in anxiety levels. Some people also report a sense of relaxation or calm. However, not everyone experiences positive effects; some have reported feeling dizzy or drowsy. Other common side effects include dry mouth and oedema. The drug can also have mood-altering effects, including euphoria, which is why it has the potential for misuse. ^3,9

The onset of effects for pregabalin typically ranges from 30 minutes to two hours post-consumption. This can vary based on a range of factors, including the individual’s metabolism, age, and food in the stomach. Oral forms of pregabalin are absorbed rapidly and have bioavailability close to 90%. The drug reaches peak plasma concentrations within 1.5 hours when fasting. Food can delay the rate of absorption but does not affect the extent of absorption. Patients often feel relief from their symptoms within the first week of treatment. ^1,4

The half-life of pregabalin is approximately 6.3 hours, but this can be influenced by individual factors such as age and kidney function. Patients usually need to take the medication two to three times a day for sustained effects. The effects of the drug can last several hours, but this varies from person to person and depends on the dosage taken. In prolonged use, pregabalin is usually reviewed periodically by healthcare providers to assess its continued effectiveness and safety. ^2,4

Pregabalin comes with a variety of risks, including dizziness, drowsiness, and the potential for allergic reactions. There is also a risk of developing suicidal thoughts, particularly in the first weeks of treatment or when changing the dose. Overdose can lead to severe complications such as respiratory depression. Long-term use of pregabalin can lead to dependency, and sudden withdrawal can result in symptoms like insomnia, nausea, and headache. Other serious side effects include blurred vision, muscle pain, and easy bruising.^2,3

Pregabalin has garnered attention for its potential for misuse and dependency. Though it is primarily prescribed for legitimate medical conditions like neuropathic pain, seizures, and generalized anxiety disorder, it has also been misused recreationally. The drug’s psychoactive effects, which can include euphoria and a sense of relaxation, make it susceptible to misuse, especially in higher doses or when taken without a prescription.⁶

Long-term use of pregabalin can lead to both physical and psychological dependency. Once a person is dependent, they may require higher doses to achieve the same therapeutic effects, known as developing a tolerance. Tolerance can accelerate the cycle of dependency and potentially lead to addiction.⁹

Withdrawal from pregabalin can be challenging and may entail a range of symptoms such as insomnia, headache, nausea, and, in severe cases, seizures. For this reason, individuals need to consult healthcare providers for a tapering schedule if discontinuation of the drug is planned.¹⁰

Combining pregabalin with other substances like opioids or alcohol can further increase the risk of addiction and the severity of withdrawal symptoms. It’s essential to understand that misuse of pregabalin can lead to serious complications, including overdose and death.²

The phenomenon of pregabalin addiction has led to policy changes in the UK, where the drug has been reclassified as a Class C controlled substance. The reclassification aims to curb the rates of misuse, addiction, and associated fatalities.¹¹

In the UK, pregabalin is classified as a Class C controlled substance, making it illegal to possess without a prescription and illegal to supply or produce without a proper licence. The penalties for unlawful possession can include up to 2 years in prison, an unlimited fine, or both. The classification was revised in 2019 due to concerns about misuse and associated deaths.¹¹

Mixing pregabalin with other drugs or substances can be a hazardous practice, as it can lead to severe side effects, interactions, and even overdose. One of the most difficult combinations is that of pregabalin and opioids. When taken together, both substances can act synergistically to depress the central nervous system, resulting in slowed breathing or even respiratory failure, which can be fatal.⁴

Combining pregabalin with alcohol is another high-risk scenario. Both substances are depressants, which means that they slow down brain activity. This can lead to increased sedative effects, affecting cognitive and motor skills and significantly raising the risk of accidents or injuries. The combination can also have detrimental effects on respiratory function.⁸

Benzodiazepines, commonly used for treating anxiety, can also interact adversely with pregabalin. Both drugs affect the neurotransmitter gamma-aminobutyric acid (GABA) and can amplify each other’s sedative effects. This can lead to an increased risk of sedation, respiratory depression, and even coma.²

Other interactions can include antihistamines, which are commonly used to treat allergies. When used concurrently with pregabalin, antihistamines can enhance the sedative effects of both substances, thereby impairing the user’s ability to operate machinery or drive.⁵

Because of these risks, healthcare providers generally advise against mixing pregabalin with other substances, especially without medical supervision. It’s crucial to consult a healthcare provider to review medications and substances to prevent harmful interactions comprehensively.³

1. Drugs.com. (n.d.). Pregabalin: Uses, Dosage & Side Effects. Retrieved from https://www.drugs.com/pregabalin.html)
2. DrugBank. (n.d.). Pregabalin. Retrieved from https://go.drugbank.com/drugs/DB00230)
3. NHS. (n.d.). Pregabalin. Retrieved from https://www.nhs.uk/medicines/pregabalin/)
4. WebMD. (n.d.). Pregabalin Oral: Uses, Side Effects, Interactions. Retrieved from https://www.webmd.com/drugs/2/drug-93954-1903/pregabalin-oral/pregabalin-extended-release-oral/details)
5. Healthline. (n.d.). Pregabalin Oral Capsule. Retrieved from https://www.healthline.com/health/pregabalin-oral-capsule)
6. Addiction Center. (n.d.). Lyrica Addiction and Abuse. Retrieved from https://www.addictioncenter.com/drugs/lyrica-addiction-abuse/)
7. RxList. (n.d.). Pregabalin. Available at: https://www.rxlist.com/pregabalin/generic-drug.htm)
8. Cleveland Clinic. (n.d.). Pregabalin Capsules. Available at: https://my.clevelandclinic.org/health/drugs/19097-pregabalin-capsules)
9. Medical News Today. (n.d.). What is pregabalin? Available at: https://www.medicalnewstoday.com/articles/322429)
10. step by Step Recovery. (n.d.). The Danger of Pregabalin (Lyrica). Available at: https://stepbysteprecovery.co.uk/danger-of-pregabalin-lyrica/)
11. BBC. (1 April 2019). Pregabalin and gabapentin are to be controlled as class C drugs. Available at: https://www.bbc.com/news/uk-northern-ireland-66579996)