Pharmacokinetics of Rectal Drug Administration, Part II

@article{Hoogdalem1991PharmacokineticsOR,
  title={Pharmacokinetics of Rectal Drug Administration, Part II},
  author={E. J. Hoogdalem and A. Boer and D. Breimer},
  journal={Clinical Pharmacokinetics},
  year={1991},
  volume={21},
  pages={110-128}
}
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… Expand
Hepatic first-pass effect and controlled drug delivery following rectal administration
TLDR
The potentials of the rectal route, as an example of a non-invasive route for drug administration partially avoiding hepatic first-pass effect, are discussed and rate controlled absorption enhancement can be achieved if adequate knowledge about the pharmacokinetics and pharmacodynamics of the enhancer is available. Expand
Rectal drug delivery: A promising route for enhancing drug absorption
TLDR
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. Expand
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 canExpand
Practical use of rectal medications in palliative care.
  • D. E. Warren
  • Medicine
  • Journal of pain and symptom management
  • 1996
TLDR
The physiology and general considerations surrounding rectal drug administration are described, and the literature pertaining to analgesic and adjuvant medications and dosage forms that are and are not approved for rectal administration by the U.S. Food and Drug Administration are evaluated. Expand
Symptom control in cancer patients: the clinical pharmacology and therapeutic role of suppositories and rectal suspensions
TLDR
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. Expand
Rectal Drug Administration
TLDR
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. Expand
Rectal Drug Delivery
TLDR
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. Expand
Increased bioavailability of tacrolimus after rectal administration in rats.
TLDR
There is a possibility that rectal administration of tacrolimus is capable of improving its bioavailability and cutting the costs of tacolimus treatment. Expand
The relative bioavailability of metoprolol following oral and rectal administration to volunteers and patients
TLDR
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. Expand
Pharmacokinetics and efficacy of rectal versus oral sustained-release morphine in cancer patients
TLDR
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. Expand
...
1
2
3
4
5
...

References

SHOWING 1-10 OF 160 REFERENCES
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. Expand
Absolute intramuscular, oral, and rectal bioavailability of alizapride.
TLDR
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. Expand
Drug absorption by sublingual and rectal routes.
TLDR
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. Expand
Bioavailability of rectally administered carbamazepine mixture.
TLDR
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. Expand
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. Expand
Biopharmaceutics of rectal administration of drugs in man IX. 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. Expand
Rectal versus oral absorption of codeine phosphate in man.
TLDR
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. Expand
Plasma concentrations and bioavailability of propranolol by oral, rectal, and intravenous administration in man.
TLDR
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. Expand
Use of adjuvants for enhancement of rectal absorption of cefoxitin in humans.
TLDR
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. Expand
Characteristics of drug absorption via the rectal route.
  • S. Muranishi
  • Medicine
  • Methods and findings in experimental and clinical pharmacology
  • 1984
TLDR
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. Expand
...
1
2
3
4
5
...