Oral Gabapentin Disposition in Patients with Epilepsy After a High‐Protein Meal

Benetello, P.; Furlanut, M; Fortunato, M; Baraldo, Massimo; Pea, Federico; Tognon, Alexandre Pereira; Testa, G

doi:10.1111/j.1528-1157.1997.tb01204.x

Cited by 21 publications

(14 citation statements)

References 3 publications

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“…59,60 Nevertheless, there is significant correlation (r 2 . 59,60 Thus, saliva may be a useful alternative matrix for gabapentin TDM. 59,60 Thus, saliva may be a useful alternative matrix for gabapentin TDM.…”

Section: Saliva Tdm For Gabapentinmentioning

confidence: 95%

Therapeutic Drug Monitoring of Antiepileptic Drugs by Use of Saliva

Patsalos¹,

Berry²

2013

Therapeutic Drug Monitoring

170

126

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Blood (serum/plasma) antiepileptic drug (AED) therapeutic drug monitoring (TDM) has proven to be an invaluable surrogate marker for individualizing and optimizing the drug management of patients with epilepsy. Since 1989, there has been an exponential increase in AEDs with 23 currently licensed for clinical use, and recently, there has been renewed and extensive interest in the use of saliva as an alternative matrix for AED TDM. The advantages of saliva include the fact that for many AEDs it reflects the free (pharmacologically active) concentration in serum; it is readily sampled, can be sampled repetitively, and sampling is noninvasive; does not require the expertise of a phlebotomist; and is preferred by many patients, particularly children and the elderly. For each AED, this review summarizes the key pharmacokinetic characteristics relevant to the practice of TDM, discusses the use of other biological matrices with particular emphasis on saliva and the evidence that saliva concentration reflects those in serum. Also discussed are the indications for salivary AED TDM, the key factors to consider when saliva sampling is to be undertaken, and finally, a practical protocol is described so as to enable AED TDM to be applied optimally and effectively in the clinical setting. Overall, there is compelling evidence that salivary TDM can be usefully applied so as to optimize the treatment of epilepsy with carbamazepine, clobazam, ethosuximide, gabapentin, lacosamide, lamotrigine, levetiracetam, oxcarbazepine, phenobarbital, phenytoin, primidone, topiramate, and zonisamide. Salivary TDM of valproic acid is probably not helpful, whereas for clonazepam, eslicarbazepine acetate, felbamate, pregabalin, retigabine, rufinamide, stiripentol, tiagabine, and vigabatrin, the data are sparse or nonexistent.

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Section: Saliva Tdm For Gabapentinmentioning

confidence: 95%

Therapeutic Drug Monitoring of Antiepileptic Drugs by Use of Saliva

Patsalos¹,

Berry²

2013

Therapeutic Drug Monitoring

170

126

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“…As a result of this, gabapentin bioavailability decreases with increasing dosage and increments in serum gabapentin concentration may be less than proportional to increments in dosage, even though this does not necessarily occur in all patients on high-dose therapy [32]. Food has no major influence on the bioavailability of the new AEDs, with the possible exception of gabapentin for which there are conflicting data concerning possible enhancement of its absorption after intake with a protein-rich meal [33][34][35]. In the case of tiagabine, administration together with a meal decreases substantially the rate of absorption without affecting the total amount absorbed [36]: this is advantageous because it reduces the fluctuations in serum tiagabine concentrations during a dosing interval [29].…”

Section: Clinical Pharmacokineticsmentioning

confidence: 94%

The New Antiepileptic Drugs Pharmacological and Clinical Aspects

Gatti¹,

Bonomi²,

Jannuzzi³

et al. 2000

CPD

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In recent years several new drugs (oxcarbazepine, lamotrigine, topiramate, gabapentin, zonisamide, tiagabine, fosphenytoin, vigabatrin and felbamate) have been added to the therapeutic armamentarium against epilepsy. Some of these represent structural modifications of pre-existing compounds, others were developed with the specific objective of modifying neurotransmitter function, and many more were found to be clinically useful even though their mode of action is unclear or differs from that originally planned. The pharmacokinetics of these drugs differ widely from one agent to another. Some (gabapentin and vigabatrin) are eliminated unchanged in urine and have little or no interaction potential; others (tiagabine, lamotrigine, topiramate, oxcarbazepine, zonisamide, felbamate) are subject to induction of metabolism by concomitant anticonvulsants; lamotrigine is vulnerable to metabolic inhibition by valproate, and felbamate is a powerful enzyme inhibitor in addition to being an inducer of the metabolism of carbamazepine and steroid oral contraceptives. All new antiepileptic drugs have been found to be effective in improving seizure control in patients with partial and secondarily generalized seizures. However, lamotrigine, topiramate, zonisamide and felbamate appear to have broader efficacy against both partial and many generalized seizure types, while vigabatrin is also valuable in the management of infantile spasms. In monotherapy studies, new drugs have not been found to be more efficacious than older agents, but some may offer limited advantages in terms of improved tolerability. On the other hand, serious toxicity restricts considerably the use of vigabatrin and felbamate. Overall, new drugs represent valuable tools in the fight against epilepsy, but because of limited experience and cost considerations their first-line use cannot be recommended in most situations.

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“…Concomitant intake of food has not been reported to cause any major alteration in the bioavailability of new AEDs, with the possible exception of gabapentin, for which there are conflicting data concerning possible enhancement of its absorption after intake with protein-rich meals (14,15). In the case of tiagabine, food may reduce peak drug concentrations and delay the time to peak without affecting the total amount absorbed ( 16).…”

Section: Absorption and Oral Bioavailabilitymentioning

confidence: 99%

The Clinical Pharmacokinetics of the New Antiepileptic Drugs

Perucca

1999

Epilepsia

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Summary: Because pharmacokinetics is a major determinant of the magnitude and duration of pharmacologic response, understanding the kinetic properties of the new antiepileptic drugs (AEDs) is essential for the correct use of these compounds in clinical practice. After oral administration, absorption is rapid and relatively efficient for the new AEDs, the most notable exception being gabapentin, whose bioavailability decreases with increasing dosage. None of the new AEDs is extensively bound to plasma proteins except for tiagabine, which is over 95% protein-bound. The route of elimination differs to an important extent from one compound to another, and elimination half-lives range from over 30 h for zonisamide to 5-7 h for gabapentin. For all drugs that are metabolized, half-life is shortened and clearance is increased when patients receive concomitant enzyme-inducing agents such as barbiturates, phenytoin, and carbamazepine. Lamotrigine metabolism is markedly inhibited by valproic acid, and felbamate may increase the serum levels of most other AEDs. Felbamate, topiramate, and oxcarbazepine may also reduce the efficacy of the contraceptive pill by stimulating its metabolism. Key Words: AntiepilepticsPharmacokinetics-Drug interactions.To exert their therapeutic effects, antiepileptic drugs CLINICAL PHARMACOKINETICS (AEDs) must be absorbed and reach their sites of action in the brain at concentrations sufficient to produce the desired pharmacologic response. The pharmacokinetic profile is a major determinant of the magnitude and duration of drug action and is one of the factors to be considered in determining the optimal number of daily doses and the minimal interval that should elapse between dosage adjustments. For any given drug, pharmacokinetics may vary markedly from one patient to another (in relation to genetic background, age, physiologic states such as pregnancy, associated disease, and concomitant treatments), resulting in altered dosage requirements. Therefore, full understanding of the pharmacokinetic properties of individual compounds, and the factors affecting them, is essential for correct use of AEDs in clinical practice. Over the past decade, several new AEDs (felbamate, gabapentin, lamotrigine, oxcarbazepine, tiagabine, topiramate, vigabatrin, and zonisamide) have been introduced into routine clinical practice in a number of counThe pharmacokinetics of the new AEDs have been evaluated in healthy volunteers and in patients with epilepsy receiving a variety of concomitant treatments. For vigabatrin and for monohydroxycarbazepine (the active metabolite of oxcarbazepine), evaluation of pharmacokinetic properties is complicated by the presence of an asymmetric carbon in the molecule, which determines the existence of two different stereoisomers. Although vigabatrin is administered as a racemic mixture of the (R)-and (S)-isomers, only the (S)-form is pharmacologically active, and pharmacokinetic data for vigabatrin quoted in' this review refer to the (S)-enantiomer. In the case of monohydroxycarbazepine...

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Oral Gabapentin Disposition in Patients with Epilepsy After a High‐Protein Meal

Cited by 21 publications

References 3 publications

Therapeutic Drug Monitoring of Antiepileptic Drugs by Use of Saliva

Therapeutic Drug Monitoring of Antiepileptic Drugs by Use of Saliva

The New Antiepileptic Drugs Pharmacological and Clinical Aspects

The Clinical Pharmacokinetics of the New Antiepileptic Drugs

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