Rectal Drug Administration

  title={Rectal Drug Administration},
  author={Albertus G. de Boer and Frits Moolenaar and L. G. J. Leede and D. D. Breimer},
  journal={Clinical Pharmacokinetics},
SummaryThe human rectum represents a body cavity in which drugs can be easily introduced and retained and from which absorption is well possible. There are important therapeutic reasons why it is sometimes preferable to give a drug rectally rather than orally, e.g. in cases of nausea and vomiting. Drawbacks of rectal drug administration include the interruption of absorption by defaecation and lack of patient acceptability. The mechanism of drug absorption from the rectum is probably no… 

Drug absorption by sublingual and rectal routes.

The disadvantages associated with administration of drugs rectally include: interruption of absorption by defaccation, which may occur particularly with irritant drugs; the surface area of the rectum is far smaller for absorption than that of the duodenum, and this may produce problems with dissolution of some drugs.

Physiological and Pharmaceutical Considerations for Rectal Drug Formulations

  • S. Hua
  • Biology, 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 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

Pharmacokinetics of Rectal Drug Administration, Part II

In Part II of this article, this discussion is extended to drugs which act peripherally and to methods of enhancing rectal drug absorption.

Relative Bioavailability of Rectally Administered Phenobarbital Sodium Parenteral Solution

The parenteral phenobarbital sodium solution given rectally is well absorbed and provides a useful alternative route of administration in comparison with the same preparation given intramuscularly.

Evaluation of the Colonic Drug Absorption in Patients with an Artificial Intestinal Stoma and by Colonoscopy in Normal Volunteers

Plasma concentration/ time profiles of both drugs after oral and colonic dosing followed similar time courses, and mean peak concentrations were lower after colonic compared with oral dosing.

Review of the rectal use of opioids.





The pharmacological effect and metabolism in man of two drugs, propranolol and isoproterenol, with which there are important differences in metabolism when administered by different routes are studied.

Avoidance of first pass elimination of propranolol after rectal administration to rats

These findings indicate that the rectal route of administration does offer the possibility of absorption of drugs from the rectum bypassing the liver, and similar availability after oral and rectal administration was similar availability (F), results are described after Rectal administration to rats.

Absorption and excretion of drugs. XXV. On the mechanism of rectal absorption of sulfonamides.

The results suggest that sulfonamides are absorbed from the Rectum by a passive transport, and that the patterns of absorption in the rectum are similar as a gastro-intestinal absorption of drugs.

ACUTE TOXICITY: following Rectal Thiopental, Phenobarbital and Leptazol

Because therapeutic rectal administration of drugs is not common in North America, toxicologists rarely include routine assessment of the toxicity of drugs given rectally. The common assumption is

Rectal bioavailability of lidocaine in rats: absence of significant first-pass elimination.

It is shown that it is possible to bypass the liver, at least partially, when giving a high clearance drug rectally to rats, and for lidocaine, this bypass is almost complete.

Absorption of diazepam in man following rectal and parenteral administration.

It is concluded that administration by rectal tube provides a useful alternative to the tablets (and intramuscular injections) when a rapid onset of effect of the drug is wanted, and when intravenous administration is not applicable or practical.

Rectal bioavailability of lidocaine in man: Partial avoidance of “first‐pass” metabolism

This investigation indicates that in principle it is possible to avoid, at least partly, drug loss caused by “first‐pass” metabolism by giving the drug rectally, and that oral and rectal bioavailability of lidocaine is reproducible in individuals.

Destruction of chlorpromazine during absorption by rat intestine in vitro.

Observations indicated that chlorpromazine was decomposed during absorption in vitro, and the possibility that the drug could be converted to absorbable metabolites during the process of absorption was investigated.

Absorption and exretion of drugs. XXXIV. An aspect of the mechanism of drug absorption from the intestinal tract in rats.

The confirmation of the suggestion that the binding process to the mucosal surface is an important factor of the absorption from the small intestine was made and the absorption of the ionized form of drugs was interpreted by this binding factor.

The kinetics of rectal absorption. III. The absorption of undissociated molecules.

  • S. RiegelmanW. Crowell
  • Chemistry
    Journal of the American Pharmaceutical Association. American Pharmaceutical Association
  • 1958
First order analysis of the results indicated that the drugs are best absorbed from true solutions in water, or from water suspensions of the drug.