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PubMed1993

Disposition of morphine and its glucuronide metabolites after oral and rectal administration: evidence of route specificity.

Morphine-6-glucuronide is a metabolite of morphine that shows significant analgesic effects in animals and humans. To evaluate route-specific differences in the potential contribution of morphine-6-glucuronide to morphine analgesia, we studied the pharmacokinetics of morphine, morphine-6-glucuronide, and morphine-3-glucuronide after oral and rectal administration of morphine sulfate in a six-subject randomized, single-dose, two-way crossover evaluation. The mean area under the plasma concentration-time curve (AUC) molar ratios of morphine-6-glucuronide (M6G) and morphine-3-glucuronide (M3G) to morphine (M) were greater after oral morphine administration compared with rectal morphine administration (M6G/M ratio, 2.7:1 versus 1.3:1, p = 0.025; M3G/M ratio, 18.3:1 versus 9.3:1, p = 0.002). Systemic bioavailability and peak plasma concentrations of morphine-6-glucuronide and morphine-3-glucuronide were significantly greater after oral morphine administration compared with the rectal route (AUC: M6G, 377.1 +/- 124.2 versus 236.2 +/- 133.7 nmol.hr/L, p = 0.05; M3G, 2610.1 +/- 446.4 versus 1650.2 +/- 309.0 nmol.hr/L, p = 0.004; maximum concentrations: M6G, 110.9 +/- 37.5 versus 64.6 +/- 28.8 nmol/L, p = 0.002; M3G, 576.9 +/- 155.8 versus 266.8 +/- 110.5 nmol/L, p = 0.007). Conversely, the systemic availability of morphine was lower after oral administration, although this difference failed to achieve statistical significance (142.3 +/- 17.1 versus 176.6 +/- 69.4 nmol.hr/L, p = 0.14). These data suggest that rectal administration of morphine is associated with significant avoidance of hepatic biotransformation, and they provide a convincing argument for the evaluation of morphine-6-glucuronide concentrations in pharmacokinetic and pharmacodynamic comparisons involving different routes of morphine administration.

Administration, Oral↗

PubMedDate not supplied

The effectiveness of rectal administration of insulin suppository on normal and diabetic subjects.

The effectiveness of insulin administration by rectal suppository was examined in normal and non-insulin-dependent nonobese diabetic subjects. A 100-U insulin suppository (mean 1.8 U/kg) given to the diabetic subjects caused four times as great a fall in plasma glucose compared with the normal subjects given the same dose (mean 1.6 U/kg). The insulin response after suppository administration demonstrated a significantly positive correlation (r = 0.83, P less than 0.01) with the plasma glucose level before administration. Diabetic subjects given a 100-U insulin suppository (mean 1.7 U/kg) 15 min after meals three times daily showed a significant (P less than 0.05) improvement in postprandial hyperglycemia accompanied by a restoration of the normal circadian profile of plasma IRI and a reduction of urinary glucose from 26 +/- 5.9 to 2.0 +/- 1.0 g/day. No untoward reactions were observed. These data strongly imply a unique characteristic of the insulin suppository in spite of low bioavailability.

Adult↗

PubMed2006

Synthesis and properties of N-nicotinoyl-2-(5-fluorouracil-1-yl)-D,L-glycine ester as a prodrug of 5-fluorouracil for rectal administration.

N-Nicotinoyl-2-(5-fluorouracil-1-yl)-D,L-glycine (NFG) methyl-(NFGM), ethyl-(NFGE) and isopropyl esters (NFGIp) were synthesized and their potential as a prodrug of 5-fluorouracil (5-FU) for rectal administration was investigated. Chemical conversion proceeded either by elimination of (5-FU) or by hydrolysis of ester group. 5-FU was released from NFGIp, NFGE and NFGM 90.5%, 71.3% and 48.5% of the dose, respectively, in 80% human plasma and 79.8%, 56.3% and 31.6%, respectively, in pH 7.4 buffer solution after 48 h of incubation at 37 degrees C. Release of 5-FU occurred mainly from NFG esters but very slightly from NFG, which suggested that release of 5-FU was greatly dependent on the stability of the ester group against hydrolysis. Solubility (M) in pH 7.4 buffer solution was 0.13, 0.09 and 0.04 and apparent partition coefficient in 1-octanol/pH 7.4 buffer solution was 0.76, 1.61 and 4.2, respectively, for NFGM, NFGE and NFGIp, which were in the ranges suitable for rectal absorption. Plasma concentration (microg/mL) of NFGM, NFGE and NFGIp at 50 min after rectal administration to rats was 1.9, 4.6 and 6.7, respectively, and that for 5-FU was below the limit of detection. Their potential as prodrugs of 5-FU for rectal administration is suggested.

Administration, Rectal↗

PubMed1984

Changes in plasma thyrotrophin-releasing hormone, thyrotrophin, prolactin and thyroid hormone levels after intravenous, intranasal or rectal administration of synthetic thyrotrophin-releasing hormone in man.

Changes in plasma thyrotrophin-releasing hormone (TRH), thyrotrophin (TSH), prolactin and thyroid hormone levels after iv, intranasal, or rectal administration of synthetic TRH were studied in man. The plasma TRH concentration increased with all three routes, but remained at higher levels for a longer time after intranasal or rectal administration, in contrast to the rapid decrease after iv administration. Plasma TSH, prolactin and thyroid hormone levels increased significantly after intranasal or rectal administration and also remained elevated for a longer period than iv administration. These findings suggest that TRH administered intranasally or rectally enters the blood stream and stimulates TSH, prolactin and thyroid hormone release in man.

Administration, Intranasal↗

PubMed1954