Pharmacokinetics of Rectal Drug Administration, Part II

  title={Pharmacokinetics of Rectal Drug Administration, Part II},
  author={Ewoud J. van Hoogdalem and Albertus G. de Boer and D. D. Breimer},
  journal={Clinical Pharmacokinetics},
SummaryPart I of this article, which appeared in the previous issue of the Journal, covered general considerations, the physiology of the rectum, spreading of drugs into the colon, rectal absorption, partial avoidance of first-pass elimination, rate-controlled rectal delivery of drugs, irritation of the rectal mucosa and clinical applications of rectal administration, and discussed centrally acting drugs. In Part II, this discussion is extended to drugs which act peripherally and to methods of… 
Rectal drug delivery: A promising route for enhancing drug absorption
In the present review various absorption enhancers with their mechanism of action in improving drug absorption through rectal epithelium and the potential of rectal route in delivering protein and peptides, analgesics and antiepileptics are discussed.
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
Practical use of rectal medications in palliative care.
  • D. E. Warren
  • Medicine, Biology
    Journal of pain and symptom management
  • 1996
Symptom control in cancer patients: the clinical pharmacology and therapeutic role of suppositories and rectal suspensions
The pharmacology of rectally administered palliative medications is reviewed and the use of individual drugs is outlined and the pharmacokinetics may differ from those of orally administered medications owing to reduced hepatic first-pass clearance.
Rectal Drug Administration
Rectal Drug Delivery
The rectal route of administration is particularly useful for infants and children who have difficulty in swallowing oral medicine, or where upper intestinal disorders present may affect the absorption of a drug.
Increased bioavailability of tacrolimus after rectal administration in rats.
There is a possibility that rectal administration of tacrolimus is capable of improving its bioavailability and cutting the costs of tacolimus treatment.
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.
Pharmacokinetics and efficacy of rectal versus oral sustained-release morphine in cancer patients
The rectal route is recommended as being suitable for MST administration when the oral route is no longer available, and the findings suggest slower absorption but less first-pass metabolism of MST after rectal administration.


Rectal Drug Administration
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.
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.
Absolute intramuscular, oral, and rectal bioavailability of alizapride.
The intramuscular injection and the tablet administration showed identical results with those of the intravenous injection, but the oral solution and the rectal suppository dosage forms gave lower absorption values.
Bioavailability of rectally administered carbamazepine mixture.
It is concluded that carbamazepine can be administered rectally, e.g. to postoperative patients in doses corresponding with oral doses, provided the mixture was not defaecated within 2 h of administration.
Rectal versus oral absorption of codeine phosphate in man.
It appeared that rectal absorption from an alkaline solution containing codeine phosphate proceeded significantly more rapid than after oral dosing, and almost identical plasma concentration profile with similar interindividual variations was observed.
Plasma concentrations and bioavailability of propranolol by oral, rectal, and intravenous administration in man.
The reduced bioavailability after oral administration indicates a substantial first pass effect but that it is possible to bypass the liver, at least partially, by giving the drug rectally to man.
Use of adjuvants for enhancement of rectal absorption of cefoxitin in humans
The quantity of sodium salicylate was found to have an influence on the quantity of cefoxitin absorbed, and the salicYLate was absorbed over an extended period of time from the rectum.
Characteristics of drug absorption via the rectal route.
  • S. Muranishi
  • Chemistry, Biology
    Methods and findings in experimental and clinical pharmacology
  • 1984
The characteristics of drug absorption from the colorectal area are summarized and the promotive effect on absorption by fatty acids or their monoglycerides in micellar state is stronger in unsaturated long-chain compounds than in saturated ones.
Pharmacokinetics of hydromorphone after intravenous, peroral and rectal administration to human subjects
The pharmacokinetic properties of hydromorphone in healthy young male subjects were studied after i.v., peroral, and rectal administration and the absolute bioavailability after peroral administration was 50.7 ± 29.8 per cent.