Pharmacokinetics of Rectal Drug Administration, Part I

  title={Pharmacokinetics of Rectal Drug Administration, Part I},
  author={Ewoud J. van Hoogdalem and Albertus G. de Boer and D. D. Breimer},
  journal={Clinical Pharmacokinetics},
SummaryGenerally, oral administration is the route of choice in the daily practice of pharmacotherapy. However, in some circumstances this is impractical or even impossible (during nausea and vomiting or convulsions, in uncooperative patients and before surgery). In these cases, the rectal route may represent a practical alternative and rectal administration is now well accepted for delivering, for example, anticonvulsants, non-narcotic and narcotic analgesics, theophylline, antiemetics and… 
Rectal Drug Administration
Rectal administration may be a very useful route for a variety of drugs in horses that are unwilling or unable to be medicated orally or parenteral, and the convenience and safety may well make up for the lower and variable bioavailability of drugs administered rectally.
Physiological and Pharmaceutical Considerations for Rectal Drug Formulations
  • S. Hua
  • Medicine
    Front. Pharmacol.
  • 2019
This review will address the physiological and pharmaceutical considerations influencing rectal drug delivery as well as the conventional and novel drug delivery approaches.
The relative bioavailability of metoprolol following oral and rectal administration to volunteers and patients
Metoprolol suppositories appear to be an effective, safe and suitable alternative for patients who are in need for beta blocking medication and who are unable to take oral medication for a certain amount of time.
Rectal Bioavailability of Sertraline Tablets in a Critically Ill Patient With Bowel Compromise.
The case of a 55-year-old woman in whom sertraline tablets were administered rectally for depression and anxiety and where PK monitoring was performed is described.
Pharmacokinetics and pharmacodynamics of clomethiazole after oral and rectal administration in healthy subjects.
The results suggest that rectal administration of a single 600-mg clomethiazole edisylate dose bears no safety risk and could be considered when neither oral nor parenteral administration is possible and a later onset of effect is not critical.
Pharmacokinetics and bioavailability of denaverine hydrochloride in healthy subjects following intravenous, oral and rectal single doses.
  • A. Staab, B. Schug, +4 authors H. Blume
  • Medicine
    European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences
  • 2003
First-pass metabolism leading to the formation of N-monodemethyl denaverine was found to be one reason for the incomplete bioavailability after oral administration.
Relative Bioavailability, Metabolism and Tolerability of Rectally Administered Oxcarbazepine Suspension
It is unlikely that adequate monohydroxy derivative concentrations can be achieved with rectal administration of diluted oxcarbazepine suspension, and the bioavailability, metabolism and tolerability of rectal and oral routes are characterised.
The suppository form of antibiotic administration: pharmacokinetics and clinical application.
The rectal route of antibiotic administration might be used effectively when other routes of administration are inadequate or unsuitable. With the use of various adjuvants, the rectal route can
Mucosal delivery systems of antihypertensive drugs: A practical approach in general practice.
A practical approach leading to successful control of severe hypertension with four antihypertensive drugs delivered via the mucosal route is described, with a case report of the prolonged-term use of mucosal delivery of sublingual Captopril and Nitrendipine combined with rectal Metoprolol tartrate and Furosemide in a patient with severe hypertension unable to receive medication p.o.
Rectal and sublingual administration of tacrolimus: a single-dose pharmacokinetic study in healthy volunteers.
Sublingual administration of a single dose of tacrolimus does not result in systemic exposure if care is taken not to swallow saliva and to rinse the oral cavity afterwards, and rectal administration results in clinically relevant systemic exposure and might represent an alternative formulation in case oral administration is not feasible.