Relative Bioavailability of Rectally Administered Phenobarbital Sodium Parenteral Solution

@article{Graves1989RelativeBO,
  title={Relative Bioavailability of Rectally Administered Phenobarbital Sodium Parenteral Solution},
  author={Nina M. Graves and Gregory B. Holmes and Robert L. Kriel and C M Jones-Saete and B Y Ong and David J. Ehresman},
  journal={Annals of Pharmacotherapy},
  year={1989},
  volume={23},
  pages={565 - 568}
}
Rectal administration of antiepileptic drugs may be a useful alternative route when oral administration is not possible due to illness, surgery, or status epilepticus. Although parenteral administration often replaces oral administration in these circumstances, there is not always a desirable intravenous line available or repeated intramuscular injections may not be practical. The purpose of this study was to determine the relative bioavailability and time course of absorption of the… 
Intramuscular and rectal therapies of acute seizures
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The intramuscular (IM) and rectal routes are alternative routes of delivery for antiepileptic drugs (AED) when the intravenous route is not practical or possible and some drugs cannot be administered rectally owing to factors such as poor absorption or poor solubility in aqueous solutions.
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In healthy adults, rectally administered TPM is absorbed to a similar extent as the oral dosage form and rectal administration is an acceptable route of administration for TPM, when the oral route is temporarily unavailable.
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These results suggest phenobarbital oral tablets crushed and suspended in water and administered via the MC is superior to suppository in delivering the medication reliably and rapidly.
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TLDR
There is a significant need for new non-oral formulations of the antiepileptic drugs when oral administration is not possible and the use of the rectal route of delivery to treat acute seizures or to maintain therapeutic concentrations is suitable for many, but not all antiePileptic medications.
Rectal Absorption of Lamotrigine Compressed Tablets
TLDR
The single‐dose pharmacokinetics of la‐motrigine (LTG) compressed tablets after rectal and oral administration in healthy volunteers were compared to show whether rectal administration can be a useful alternative when the oral route of administration is not possible.
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TLDR
Phenobarbital clearance may be predicted from previously developed population pharmacokinetic models and their significant covariate-parameter relationships along with Bayesian forecasting, but when applying these models in a target population, an external evaluation of these models using the target population is warranted.
Perioperative substitution of anti-epileptic drugs
TLDR
For a substantial number of AEDs, unofficial perioperative treatment strategies need to be followed for lack of alternatives to oral administration, and there is little clinical research addressing the equivalence of oral and parenteral formulas.
Pharmacokinetics of Rectal Drug Administration, Part II
TLDR
In Part II of this article, this discussion is extended to drugs which act peripherally and to methods of enhancing rectal drug absorption.
Perioperative substitution of anti-epileptic drugs Wilma S. W. WichardsAlfred F. A. M. Schobben •
TLDR
For a substantial number of AEDs, unofficial perioperative treatment strategies need to be followed for lack of alter- natives to oral administration, and there is little clinical research addressing the equivalence of oral and parenteral formulas.
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References

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Relative Bioavailability of Rectally Administered Carbamazepine Suspension in Humans
TLDR
The slow absorption after rectal administration precludes the use of this route in status epilepticus; however, it may be a satisfactory alternative for maintenance therapy when administration by the oral route is not possible.
PLASMA CONCENTRATIONS OF DIAZEPAM AND N‐DESMETHYLDIAZEPAM IN NEWBORN INFANTS AFTER INTRAVENOUS, INTRAMUSCULAR, RECTAL AND ORAL ADMINISTRATION
TLDR
Rectal administration could be a suitable treatment for seizures in the newborn infant as next to intravenous administration rectal administration caused the most rapid increase in plasma‐diazepam concentration.
Biopharmaceutics of rectal administration of drugs in man. Part 9. : Comparative biopharmaceutics of diazepam after single rectal, oral, intramuscular and intravenous administration in man
TLDR
The mechanism of the rapid rectal absorption of diazeparn from the solute state was discussed and no essential difference in bioavailability was observed between the intramuscular injection, rectal solution and tablets as compared with the intravenous injection.
Serum concentration of clonazepam after rectal administration
TLDR
Clonazepam is well‐absorbed after rectal administration and can be used in the treatment of status epilepticus, possibly in larger doses than those used in this study.
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TLDR
Diazepam was administered rectally as a new experimental suppository formulation immediately after a seizure and was highly effective in preventing recurrent fits within a 24 h observation period.
Rectal administration of sodium valproate in status epilepticus
TLDR
The rectal route of administration was effective in achieving systemic absorption of sodium valproate in the treatment of status epilepticus, suggesting that bioavailability is similar for the two forms of the drug.
Rectal absorption and disposition of secobarbital in epileptic children.
TLDR
If rectal secobarbital is considered for treatment of prolonged seizure, a rectal solution may offer a more rapid and consistent onset of action than with the suppository preparation.
Bioavailability of phenobarbital by rectal administration.
TLDR
The results obtained suggest that rectal administration of phenobarbital is more reliable than intramuscular or oral administration of the drug for rapid treatment in children.
Plasma Levels of Diazepam After Parenteral and Rectal Administration in Children
Plasma levels of diazepam and N‐des‐methyldiazepam were investigated in 19 children by a gas chromatographic method permitting the use of capillary samples. Intravenous administration was studied in
Rectal Drug Administration
TLDR
Only in a limited number of cases has it been adequately shown that the rectal route of administration gives plasma concentrations which are comparable to the oral route, but the influence of the formulation seems to be very critical.
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