Lyrica (Pregabalin) is a medication approved for the treatment fibromyalgia, neuropathic pain, and partial seizures (as an adjuvant). The drug “pregabalin” was engineered by Pfizer as an improved successor to “gabapentin,” a chemical that had been on the market since 1993. Like gabapentin, pregabalin is considered a lipophilic analogue of the neurotransmitter GABA (gamma-aminobutyric acid), but differs substantially in its bioavailability; Lyrica is more bioavailable.
The drug functions primarily as a modulator of GABA without binding to receptors. Specifically, pregabalin binds to the α2δ subunit of voltage-gated calcium channels to facilitate an increase in levels of the enzyme glutamate decarboxylase (GAD). Elevations in levels of glutamate decarboxylase triggers greater conversion of glutamate to GABA, resulting in increased GABA concentrations.
As a result of Lyrica’s effect on GABA, many users report clinically significant reductions in seizures, neuropathic pain, and fibromyalgia. Though the drug can be therapeutic for some, it often carries unwanted side effects such as: blurred vision, coordination problems, memory impairment, sedation, and weight gain. Should you experience any of these side effects, you may decide to stop taking Lyrica – wondering how long it’ll take to clear from your system.
How long does Lyrica stay in your system? (Pregabalin)
After you’ve ceased usage of the drug, you’ll likely experience an array of prominent (often unexpected) Lyrica withdrawal symptoms. During this time you may wonder how long the pregabalin within Lyrica stays in your system after your last dose. To determine how long the pregabalin is likely to remain in systemic circulation, it is important to consider it’s elimination half-life of 6.3 hours.
An elimination half-life of 6.3 hours indicates that 50% of the drug should be out of your system within 6.3 hours of administration. Based off of this information, we can estimate that the drug is likely to have been fully excreted from your system in 1.44 days. This means that most Lyrica users will have excreted the drug within a day-and-a-half (1.5 days) of their final dose.
Though Lyrica should be excreted from your body within 1-2 days, it is necessary to investigate whether any metabolites are formed that could have longer half-lives. Unlike gabapentin which does not form any metabolites, the pregabalin within Lyrica forms the metabolite “N-methylpregabalin.” Despite the presence of N-methylpregabalin, it is not thought to exhibit a longer half-life than its parent pregabalin.
- Source: https://pubchem.ncbi.nlm.nih.gov/compound/Pregabalin
Variables that influence how long Lyrica stays in your system
Though Lyrica is likely to stay in your system for 1-2 days after administration, there are often differences in excretion times among individuals. Excretion in 1.44 days is considered “average”; some users will excrete the drug in a shorter duration, while others may take longer. The speed of excretion is often influenced by variables such as: renal function, the individual taking the drug, dosage, and term of administration.
It is known that Lyrica undergoes negligible hepatic metabolism and is primarily excreted unchanged by the kidneys. For this reason, optimal renal function is required to efficiently excrete the unchanged drug. Should an individual experience renal impairment, it will slow the clearance rate and increase the elimination half-life of Lyrica.
In general, the greater the extent to which you experience renal impairment, the longer you can expect Lyrica to linger within your system after your last dose. Research has shown that among some individuals with renal impairment, the elimination half-life of pregabalin was extended to 11.5 hours. This was due to greater accumulation of the drug as a result of suboptimal renal function.
This would suggest that among those with renal impairment, it’ll take approximately 2.64 days to excrete Lyrica, more than 24 hours longer than those with normative kidney function. It is possible that those with more severe renal impairment may take between 3 and 4 days to fully excrete the drug. If you exhibit healthy (or normative) kidney function, you should expect to have eliminated pregabalin from your system in under 2 days.
- Source: http://www.ncbi.nlm.nih.gov/pubmed/12638396
- Source: http://www.ncbi.nlm.nih.gov/pubmed/24574633
In theory, two people could administer a single dose of 100 mg Lyrica simultaneously, yet one individual may excrete the drug quicker than the other. Variance in excretion time could be a result of factors such as: age, body mass, hydration, and urinary pH. When attempting to estimate how long it’ll take your body to excrete Lyrica, these factors may warrant consideration.
Age: It is hypothesized that elderly individuals (over the age of 65) often exhibit poorer clearance and an increased elimination half-life of pregabalin. Elderly adults are likely to exhibit heightened plasma concentrations of pregabalin as a result of poorer distribution and diminished renal function. Research estimates that over 33% of individuals over the age of 60 experience Stage III chronic kidney disease.
As a result of suboptimal kidney function among the elderly, dosage reductions are typically required to ensure normative excretion speed of gabapentin. Furthermore, elderly individuals may have other health conditions, reduced blood flow, and/or poorer overall physiologic function compared to younger counterparts. Younger adults tend are often in better health and usually eliminate gabapentin with greater speed and efficiency compared to elderly.
- Source: http://www.ncbi.nlm.nih.gov/pubmed/15903286/
Body mass/fat: Usually the greater a person’s body mass relative to gabapentin dosage, the quicker they’ll excrete the drug. Contrarily, the lesser a person’s body mass relative to administered dosage of gabapentin, the longer they may take to excrete it. A more massive body (bigger system) means that greater amounts of exogenous substances will likely be excreted with greater efficiency than smaller individuals.
Though the exact degree to which body mass affects clearance isn’t fully understood, a 100 mg dose of Lyrica would likely get excreted quicker in a 6’5″ man compared to 4’2″ woman. In addition to body mass, a person’s body fat should also be thought to affect excretion. Since gabapentin is highly hydrophilic, it is soluble in water.
Therefore individuals with greater muscle tissue (and less body fat) may retain the gabapentin for slightly longer durations than those with less muscle. Muscle is known to increase water retention, whereas increased fat is associated with decreased water retention. In other words, individuals with a high body fat percentage may purge gabapentin quicker than those with low body fat.
Hydration: Whether you’re sufficiently hydrated after taking Lyrica (or dehydrated) could affect how quickly the drug is excreted from your system. Hydration is known to impact a person’s urinary flow rate, which in turn is thought to alter clearance rate/excretion speed of drugs. A person who stays properly hydrated after taking Lyrica will likely exhibit increased urinary flow rate compared to someone who’s dehydrated.
Increased urinary flow rate is associated with expedited clearance and excretion of drugs like pregabalin. Therefore, the greater your level of hydration, the quicker you should expect Lyrica to leave your system. Oppositely, someone who’s underhydrated will excrete pregabalin with less efficiency and it will linger in their body for a longer duration.
Urinary pH: A person’s urinary pH is also thought to affect speed of drug clearance. Individuals with acidic (low pH) urine tend to excrete drugs quicker than those with alkaline (high pH) urine. Since a person’s urinary pH is generally influenced by their dietary choices, an individual eating predominantly alkaline foods may excrete pregabalin more slowly than a person eating acidic foods.
Alkalinity of urine is associated with reabsorption of drugs prior to excretion and slower clearance rates. Reabsorption facilitates recirculation throughout the system and may significantly increase elimination half-life of pregabalin. On the contrary, acidification is thought to prevent reabsorption and expedite clearance rate.
Dosage (50 mg to 600 mg)
For most medical conditions, Lyrica is taken within the dosing range of 150 mg to 300 mg per day; typically divided into 2 or 3 doses. The greater the daily dose a person takes of Lyrica, the slower they are likely to excrete it from their system. An individual taking 600 mg of Lyrica per day will likely retain the drug for a longer duration after discontinuation than someone taking just 50 mg per day.
When a high dose such as 600 mg is administered, a greater amount of the drug is distributed throughout the body and heightened plasma concentrations are attained compared to a lower dose. The increase in pregabalin plasma concentrations translates to a greater burden being placed on the kidneys when it comes time to excrete the drug. In other words, when a greater amount of an exogenous substance necessitates renal excretion, the excretion capacity is reduced.
This is because the kidneys are placed under greater stress (as a result of the higher dose) and need to work harder to eliminate the drug. At lower doses such as 50 mg per day, less of a burden is placed on the kidneys because there’s less of the drug that needs to be excreted. Therefore if you discontinue from a high daily dose, you should expect the drug to remain in your system for slightly longer than if you had taken a low daily dose.
Term of Administration
The term over which you’ve been taking Lyrica could influence how long it stays in your body after your last dose. A person who’s taken just a single dose of Lyrica will likely excrete it quicker from their system than a person who’s been taking it for several days. This is because steady state concentrations of pregabalin are thought to be attained after 48 hours (2 days) of consistent administration.
However, long-term users of Lyrica tend to excrete the drug at a slower pace not because of steady state, but because of dosing. Consistent long-term administration of Lyrica often results in users building tolerance to low doses. After awhile, these individuals require upward titrations in dosing to derive the same therapeutic benefit that they once attained from low doses.
These increases in dosing lead to greater plasma concentrations of the drug and place an increased burden on the kidneys for excretion. For this reason, long-term/chronic users of Lyrica may not excrete the drug quite as fast as short-term/infrequent users. That said, the differences in excretion times between a short-term and long-term pregabalin user is unlikely to be as significant as it would be with other drugs.
This is due to the fact that pregabalin is highly hydrophilic, meaning it is soluble in water. Therefore even in long-term users, the drug is unlikely to “accumulate” in bodily tissues. Other substances that are classified as highly lipophilic may accumulate to a greater extent in the tissues (e.g. body fat) of long-term users.
Lyrica (Pregabalin): Absorption, Distribution, Excretion (Details)
Following oral administration of Lyrica, the active ingredient “pregabalin” is efficiently absorbed by the proximal small bowel and exhibits a bioavailability of ~90%. Unlike may psychiatric drugs, pregabalin does not bind to plasma proteins. It is distributed throughout the body at an estimated 0.5 L/kg by way of the L-amino acid transport system (as it is an L-transporter substrate).
Peak plasma concentrations of pregabalin are attained approximately 1.5 hours post-ingestion, with the specific concentration directly relative to the dosage administered. Some sources suggest that co-ingestion of food with pregabalin may decrease its rate of absorption by 30%, thus slightly delaying the time to attain peak plasma concentrations from 1.5 to 3 hours. Steady state concentrations are thought to be attained between 24 and 48 hours after consecutive dosing.
Pregabalin is not subject to hepatic metabolism, and therefore is primarily excreted unchanged by the kidneys. Unlike its predecessor gabapentin, however, approximately 2% of a pregabalin dose is converted to form N-methylpregabalin. In healthy adults, renal clearance of pregabalin occurs at a rate of 67 to 80.9 mL/min.
An estimated 90% of a dose is excreted via the urine as unchanged pregabalin, whereas 0.9% is the N-methylpregabalin metabolite. Accounting for the 6.3 hour half-life of pregabalin, the drug should get fully eliminated from your body within approximately 1.44 days of your last dose. Among those with renal impairment, it could take between 2 and 3 days to completely excrete pregabalin and N-methylpregabalin metabolites.
- Source: https://pubchem.ncbi.nlm.nih.gov/compound/Pregabalin
- Source: http://www.ncbi.nlm.nih.gov/pubmed/20147618
Getting Lyrica out of your system
If you’ve stopped taking Lyrica recently, you probably want to ensure that it is fully cleared from your body as soon as possible after your final dose. Keep in mind that the tips listed below may vary in efficacy among individuals. Furthermore, it is always recommended to consult a medical professional to verify safety of these suggestions prior to actual implementation.
- Discontinue: If you want to ensure that Lyrica leaves your body, you’ll need to fully discontinue treatment. Discontinuation should be done gradually under supervision of a medical professional. Understand that the sooner you stop taking the drug, the quicker you can expect to have completely cleared it from your body.
- Urinary flow rate + pH: Expediting the excretion speed of Lyrica may be accomplished by increasing urinary flow rate and lowering urinary pH. Urinary flow rate can be increased by staying well-hydrated, whereas urinary pH can be lowered via acidification. Though increasing urinary flow rate and lowering pH may not make a huge difference in excretion speed, it could make a minor one.
- Activated charcoal: A useful supplement that can be taken to help detoxify your system after stopping Lyrica is activated charcoal. Obviously you wouldn’t want to take the activated charcoal until the pregabalin has been fully excreted after your final dose. Taking activated charcoal too soon may affect absorption of your final dose and result in premature withdrawal. However, when administered later, activated charcoal can bind to toxins and remnants of the drug if you suspect that it may be lingering within your body after you’ve stopped.
How long has Lyrica stayed in your system after stopping?
If you’ve stopped taking Lyrica, share a comment regarding how long you think it stayed in your body after your last dose. Do you think it stayed in your body for a longer time than usual or was excreted much quicker than average? Share factors that may have affected its elimination half-life in your body such as: renal function, your age, and the dosage of Lyrica you took.
Understand that since Lyrica is highly hydrophilic, there is unlikely to be major interindividual variation in excretion times. Most users will retain the drug for approximately 1.44 days after their final dose. In other words, the drug should be fully excreted from your body (mostly via urine) within 48 hours of your final dose. Only if you have compromised renal function could the excretion exceed 2 days.