Saliva carbamazepine and phenytoin level monitoring.

Rylance, G; Moreland, T. A.

doi:10.1136/adc.56.8.637

Cited by 22 publications

(14 citation statements)

References 7 publications

(6 reference statements)

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“…[48][49][50][51][52][53][54]56,73,[84][85][86][87][88][89][90][91][92][93][94][95] The salivary concentration of carbamazepine is similar to the free, non-protein bound concentration in serum with mean saliva/serum total carbamazepine concentration ratios ranging 0.26-0.44, whereas the mean saliva/serum-free carbamazepine concentration ratios ranged 1.39-1.44. [48][49][50][51][52][53][54]56,73,[84][85][86][87][88][89][90][91][92][93][94][95] The salivary concentration of carbamazepine is similar to the free, non-protein bound concentration in serum with mean saliva/serum total carbamazepine concentration ratios ranging 0.26-0.44, whereas the mean saliva/serum-free carbamazepine concentration ratios ranged 1.39-1.44.…”

Section: Saliva Tdm For Carbamazepinementioning

confidence: 99%

“…26,49,53,54,56,57,73,76,90,95,134,135,137,[142][143][144][145][146] Phenytoin distributes into saliva such that the salivary concentration is similar to the free non-protein bound concentration in serum. 26,49,53,54,56,57,73,76,90,95,134,135,137,[142][143][144][145][146] Phenytoin distributes into saliva such that the salivary concentration is similar to the free non-protein bound concentration in serum.…”

Section: Saliva Tdm For Phenytoinmentioning

confidence: 99%

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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 Carbamazepinementioning

confidence: 99%

Section: Saliva Tdm For Phenytoinmentioning

confidence: 99%

Therapeutic Drug Monitoring of Antiepileptic Drugs by Use of Saliva

Patsalos¹,

Berry²

2013

Therapeutic Drug Monitoring

170

126

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“…39,40 Early work emphasized a relationship between unbound drug in plasma and anticonvulsant efficacy or toxicity. 41,42 Some researchers 43 found that CBZ and PTN saliva concentrations were related to toxicity, but not to efficacy. When monotherapy was used, saliva and plasma concentrations of both PTN and CBZ showed marked interindividual variability and a respective mean S/P ratio of 0.26 and 0.13, and both drugs showed good saliva-to-plasma correlations.…”

Section: Ethanol and Drugs Of Abusementioning

confidence: 99%

The Use of Oral Fluid for Therapeutic Drug Management

Langman

2007

Annals of the New York Academy of Sciences

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One of the underlying tenets of clinical pharmacology is that only free drugs are pharmacologically active. It is thought that only free drugs can cross biological membranes to interact with a given receptor to alter its function, and that drug responses, both efficacious and toxic, are a function of unbound concentrations. The rationale for measuring drugs in oral fluid is that the free fraction of a drug in plasma reaches equilibrium with the drug in saliva. Although reports concerning the appearance of organic solutes in saliva have been in the literature for over 70 years, it has only been in the past 30 years that there has been emphasis on the appearance of drugs. Although many assumptions for drug level monitoring in saliva are made, the primary requisite for salivary monitoring to be useful is a constant or predictable relationship between the drug concentration in saliva and the drug concentration in plasma. Measurement of oral fluid drug levels for the purpose of managing patients and making dosage adjustments may be useful for select drugs or drug classes. However, it does not appear to be useful for the majority of drugs therapeutically monitored. Some work with antipsychotic medications has indicated that although the measurement of drug concentrations themselves may not be useful for dosage adjustment, the ratio of parent drug to metabolite may reflect altered metabolic status due to either pharmacogenetic variation or other clinical conditions. Furthermore, analysis of saliva may provide a cost-effective approach for the screening of large populations.

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“…Measurement of the anticonvulsant concentration in saliva could be substituted for by measurement of the serum concentration [8] because it represents the free, (unbound to the serum protein), pharmacologically active fraction of the drug. For several anticonvulsants, good correlations between saliva and serum concentrations were reported [1,2,6,9]. However, for phenobarbital (PB), this correlation has been controversial, especially because of the salivary pH (2.6).…”

Section: Introductionmentioning

confidence: 94%

Correlation between the saliva and free serum concentration of phenobarbital in epileptic children

et al. 1986

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Twenty epileptic children taking phenobarbital (PB) were evaluated for the concentration of PB in their saliva (Sa), total serum concentration (TS), free serum concentration (FS), and also the pH of the saliva samples. The Sa/TS ratio was 43.0 +/- 5.2% (mean +/- SD), and showed a close relationship between the two (r = 0.98). The free serum concentrations for PB were also observed to be closely correlated to the saliva concentration (r = 0.99), as well as to the total serum concentration, with the FS/TS ratio being 45.0 +/- 5.6%. However, no obvious relationship between the salivary pH and the Sa/TS ratio for PB was observed. This suggested the usefulness of monitoring the PB saliva concentrations in clinical management of epilepsy.

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Saliva carbamazepine and phenytoin level monitoring.

Cited by 22 publications

References 7 publications

Therapeutic Drug Monitoring of Antiepileptic Drugs by Use of Saliva

Therapeutic Drug Monitoring of Antiepileptic Drugs by Use of Saliva

The Use of Oral Fluid for Therapeutic Drug Management

Correlation between the saliva and free serum concentration of phenobarbital in epileptic children

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