A Comparison of the Pharmacokinetics and Pharmacodynamics of Pregabalin and Gabapentin

@article{Bockbrader2010ACO,
  title={A Comparison of the Pharmacokinetics and Pharmacodynamics of Pregabalin and Gabapentin},
  author={Howard N. Bockbrader and David L. Wesche and Raymond Miller and Sunny Chapel and Nancy Janiczek and Paula Burger},
  journal={Clinical Pharmacokinetics},
  year={2010},
  volume={49},
  pages={661-669}
}
Pregabalin and gabapentin share a similar mechanism of action, inhibiting calcium influx and subsequent release of excitatory neurotransmitters; however, the compounds differ in their pharmacokinetic and pharmacodynamic characteristics. Gabapentin is absorbed slowly after oral administration, with maximum plasma concentrations attained within 3–4 hours. Orally administered gabapentin exhibits saturable absorption — a nonlinear (zero-order) process — making its pharmacokinetics less predictable… Expand
Pharmacokinetic and pharmacodynamic profile of pregabalin and its role in the treatment of epilepsy
TLDR
The rapid onset of action with significant antiepileptic effects at dosages of 150 – 600 mg/day makes pregabalin an option in patients with high seizure frequency and favorable effects on mood offer advantages in many patients with chronic epilepsy and psychiatric comorbidities. Expand
A comparison of pregabalin and gabapentin in palliative care #289.
TLDR
Overall, literature suggests that pregabalin has a small pharmacokinetic advantage over gabapentin, although there is little evidence-based literature to support its clinical superiority in patient care. Expand
Lack of a Clinically Significant Pharmacokinetic Interaction Between Pregabalin and Thioctic Acid in Healthy Volunteers.
TLDR
The combination of pregabalin and thioctic acid can safely be administered concomitantly without dose adjustment and the mean concentration-time curves were similar between each drug alone and in combination with the other drug. Expand
Gabapentin to Pregabalin Therapy Transition: A Pharmacokinetic Simulation
TLDR
Trans transitioning patients from gabapentin to pregabalin could theoretically be achieved by either of the 2 approaches assessed, and pharmacokinetic simulations show that during the transition period in both designs, predicted preGabalin-equivalent concentrations did not depart from those calculated during periods of steady-state gabAPentin or pregABalin monotherapy. Expand
Mirogabalin: could it be the next generation gabapentin or pregabalin?
TLDR
Mirogabalin besylate is anticipated to be a novel, safe gabapentinoid anticonvulsant with a greater therapeutic effect for neuropathic pain in the DRG and lower ADRs in the cerebellum. Expand
Population pharmacokinetics of gabapentin in healthy Korean subjects with influence of genetic polymorphisms of ABCB1
TLDR
The results of the present study indicate that the oral bioavailability of gabapentin is decreased when its dosage is increased, and ABCB1 2677G > T/A polymorphism can explain the substantial inter-individual variability in the absorption of gABapentin. Expand
Misuse and Abuse of Pregabalin and Gabapentin: Cause for Concern?
TLDR
Physicians considering prescribing gabapentinoids for neurological/psychiatric disorders should carefully evaluate a possible previous history of drug abuse, whilst being able to promptly identify signs of pregabalin/gabAPentin misuse and provide possible assistance in tapering off the medication. Expand
A pharmacokinetic drug-drug interaction study between pregabalin and tramadol in healthy volunteers
TLDR
There were no significant drug interactions between pregabalin and tramadol, considering that all of the 90% CI of PK measures were within the conventional bioequivalence range. Expand
Pharmacokinetic Profiles of Gabapentin after Oral and Subcutaneous Administration in Black-tailed Prairie Dogs (Cynomys ludovicianus).
TLDR
It is demonstrated that oral administration of gabapentin at low (30 mg/kg) doses likely would achieve and maintain plasma concentrations at half maximum effective concentration for 12 h, making it a viable option for an every 12-h treatment. Expand
Gabapentinoid Pharmacology in the Context of Emerging Misuse Liability
TLDR
The epidemiology and pharmacology of gapapentinoids (gabapentin and pregabalin) relevant to their emerging misuse potential are reviewed to provide guidance for clinical and regulatory management and harm reduction efforts are necessary. Expand
...
1
2
3
4
5
...

References

SHOWING 1-10 OF 64 REFERENCES
Clinical pharmacokinetics of gabapentin
TLDR
Gabapentin is a new, water-soluble, antiepileptic agent with properties of an amino acid that is rapidly absorbed and exhibits dose-dependent bioavailability as a result of a saturable transport mechanism. Expand
The absorption of gabapentin following high dose escalation
TLDR
It is concluded that larger than recommended doses of GBP can be efficiently absorbed by some patients and also that GBP plasma levels do not fluctuate greatly between dosage intervals, therefore, twice daily dosage is a possibility. Expand
Clinical Pharmacokinetics of Pregabalin in Healthy Volunteers
TLDR
Pregabalin demonstrates desirable, predictable pharmacokinetic properties that suggest ease of use, and is essentially equivalent to renal clearance, indicating that pregabalin undergoes negligible nonrenal elimination. Expand
A Saturable Transport Mechanism in the Intestinal Absorption of Gabapentin Is the Underlying Cause of the Lack of Proportionality Between Increasing Dose and Drug Levels in Plasma
TLDR
These findings support absorption of gabapentin by a saturable pathway, system L, shared by the large hydrophobic amino acids, L-Phe and L-Leu, made a major contribution to the lack of proportionality in plasma levels of drug with increasing dose ob-served in the clinic. Expand
Inter- and intra-subject variability in gabapentin absorption and absolute bioavailability
TLDR
The within subject variability of gabapentin is small enough that plasma drug monitoring may be used to assess gABapentin absorption for a given subject and the benefit of dose individualization. Expand
Pharmacokinetics of gabapentin in subjects with various degrees of renal function
TLDR
Impaired renal function results in higher plasma gabapentin concentrations, longer elimination half‐lives, and reduced CL/F and CLR values, based on pharmacokinetic considerations. Expand
Effect of a high-protein meal on gabapentin pharmacokinetics
TLDR
Despite significantly higher plasma concentrations at 2 h, subjects reported significantly fewer adverse effects after the high-protein meal, and potential mechanisms to explain these unexpected findings may be that the large amino acid load delivered with theHighprotein meal enhanced gabapentin absorption via trans-stimulation, the process by which acutely increased intestinal luminal amino acid concentrations result in an acute up regulation in System-L activity. Expand
Clinical pharmacokinetics of gabapentin.
TLDR
Gabapentin is a new, water-soluble, antiepileptic agent with properties of an amino acid that is rapidly absorbed and exhibits dose-dependent bioavailability as a result of a saturable transport mechanism. Expand
Pharmacokinetics and metabolism of gabapentin in rat, dog and man.
TLDR
Experiments in rats and dogs demonstrate that pharmacokinetics are not sex-dependent and are not changed after multiple dosage, and gabapentin is shown to be linear in the range tested of 4 to 500 mg/kg i.v. in rats. Expand
Selected CSF biochemistry and gabapentin concentrations in the CSF and plasma in patients with partial seizures after a single oral dose of gabapentin
Gabapentin (GBP) is a neutral amino acid and a GABA analog which in animal experimental models has shown a broad anticonvulsant spectrum. To evaluate the penetration of GBP into the CSF in humans asExpand
...
1
2
3
4
5
...