Gastrointestinal motor effects of erythromycin

1990 ◽  
Vol 259 (3) ◽  
pp. G355-G363 ◽  
Author(s):  
M. F. Otterson ◽  
S. K. Sarna
Keyword(s):  
Small Intestine ◽  
Cycle Length ◽  
Amplitude Ratio ◽  
Contractile Activity ◽  
Low Doses ◽  
Control Activity ◽  
Distal Small Intestine ◽  
Gastrointestinal Motor ◽  
High Doses ◽  
Motor Effects

We studied the small intestinal motor effects of oral and intravenous (iv) erythromycin in 10 conscious dogs. After control recordings with placebo, oral or iv erythromycin was given at 40% of the migrating motor complex (MMC) cycle. Recordings were made after administration until normal contractile activity had returned or 12 h postdrug administration. Low doses initiated a premature MMC. High doses, however, prolonged the MMC cycle length. Erythromycin reduced the MMC propagation velocity at all doses. Both oral and iv erythromycin induced amyogenesia. During this pattern, electrical control activity was obliterated in the proximal and destabilized in the distal small intestine. Erythromycin also increased the incidence of retrograde giant contractions (RGCs) and vomiting. These effects occurred within the first 2 h after oral and within the first 30 min after iv administration. The incidence of giant migrating contractions (GMCs) increased significantly from 5 to 12 h but not from 0 to 5 h after administration. The distance of origination of GMCs from the ileocolonic junction was significantly increased from 5 to 12 h. The amplitude ratio, duration, and velocity of migration of GMCs induced after erythromycin were similar to control values. Clusters of coordinated antral and duodenal contractions also occurred early after administration. Our findings suggest that erythromycin has multiple motor effects on the stomach and small intestine. Diarrhea, abdominal cramping, and vomiting associated with erythromycin may be related to increased incidence of GMCs and RGCs. Erythromycin has a biphasic effect on MMC cycle length, initiating premature MMCs at low doses and prolonging their cycle length at higher doses.(ABSTRACT TRUNCATED AT 250 WORDS)

FURTHER STUDIES OF THE PHARMACOLOGY OF THE PYLORIC REGION: ANALYSIS OF THE EFFECTS OF INTRA-ARTERIAL HISTAMINE, SEROTONIN, PHENYLDIGUANIDE, MORPHINE, AND OTHER DRUGS ON THE ANTRUM AND DUODENAL BULB

1966 ◽  
Vol 44 (6) ◽  
pp. 981-1019 ◽  
Author(s):  
E. E. Daniel
Keyword(s):  
Intravenous Injection ◽  
Contractile Activity ◽  
Duodenal Bulb ◽  
Gastroepiploic Artery ◽  
Low Doses ◽  
Common Site ◽  
Site Of Action ◽  
Small Doses ◽  
Release Of Acetylcholine ◽  
High Doses

The actions of drugs on the antrum and duodenum of the dog were analyzed by the use primarily of intra-arterial injections into the gastroepiploic artery while the electrical and contractile activity of these regions was recorded. Histamine (0.1 to 5 μg) usually caused excitation of second potentials (antrum) or fast spikes (duodenum), and contractions (both) and other effects similar to those produced by acetylcholine, though usually delayed in onset and more prolonged. Its effects were diminished or prevented by atropine, nicotine, and hexamethonium as well as by antihistaminics such as antazoline, cyproheptadine, and phenoxybenzamine. In the duodenum, histamine excitation was usually preceded by inhibition, and most antihistaminics also depressed responses to serotonin (5-HT), acetylcholine, or both. Low doses of serotonin (0.1 to 1 μg) most frequently caused excitation of the antrum and duodenum similar to that evoked by acetylcholine. This response was sometimes prolonged. These effects in the antrum were diminished or prevented by atropine, nicotine, methysergide, and bromolysergic acid (BOL), and less effectively antagonized by hexamethonium, morphine, and pronethalol. Phenoxybenzamine did not prevent excitation of the antrum by low doses of 5-HT, but tachyphylaxis following high doses of 5-HT (5 to 100 μg) or of phenyldiguanide (25 to 500 μg) did prevent such responses. Several of these agents also inhibited excitation of the duodenum induced by 5-HT and cross tachyphylaxis between 5-HT and phenyldiguanide was also observed. It was suggested that low doses of 5-HT, like phenyldiguanide, acted at a preganglionic site in the antrum and duodenum different from that at which histamine acts, presumably the non-medullated mucosal mechanoreceptors, and ultimately caused release of acetylcholine from postganglionic fibers. Phenyldiguanide in small doses (2 to 25 μg) acted like 5-HT to excite the antrum and duodenum. Analysis of its action with antagonists yielded results similar to those with 5-HT, and the occurrence of cross tachyphylaxis with 5-HT suggested a common site of action. Morphine (10 to 1000 μg) usually inhibited electrical and contractile activity in the antrum and stimulated these activities in the duodenum. The same results were obtained with intravenous injection (0.1 to 0.35 mg/kg). It. diminished responses to histamine, 5-HT, phenyldiguanide, and to a lesser extent, acetylcholine.

Erythromycin mimics exogenous motilin in gastrointestinal contractile activity in the dog

1984 ◽  
Vol 247 (6) ◽  
pp. G688-G694 ◽  
Author(s):  
Z. Itoh ◽  
M. Nakaya ◽  
T. Suzuki ◽  
H. Arai ◽  
K. Wakabayashi
Keyword(s):  
Small Intestine ◽  
Gastrointestinal Tract ◽  
Intravenous Infusion ◽  
Contractile Activity ◽  
Contractile Force ◽  
Naturally Occurring ◽  
Gastrointestinal Motor ◽  
Plasma Motilin ◽  
Interdigestive Migrating Contractions ◽  
Gastrointestinal Contractile Activity

The gastrointestinal motor stimulating activity of erythromycin (EM) was studied in conscious dogs. It was found that a 20-min intravenous infusion of EM lactobionate at a dose of 50–100 micrograms (potency) X kg-1 X h-1 induced a group of strong contractions in the stomach and the duodenum, and the contractions migrated along the small intestine to the terminal ileum. The EM-induced contractions were quite similar to the naturally occurring interdigestive migrating contractions (IMC) in the gastrointestinal tract in frequency, contractile force, and duration of the contractions, migrating velocity, and accompanying peaks of plasma motilin concentration. The EM-induced contractions in the stomach were inhibited by feeding and intravenous infusion of pentagastrin (1.5 micrograms X kg-1 X h-1) but were not affected by secretin; these findings are identical to those found with the naturally occurring and motilin-induced contractions. Like motilin, EM stimulated motor activity only during the interdigestive state. We conclude that EM induces IMC associated with the release of endogenous motilin in the dog.

ANTAGONISTIC ACTION OF NORETHYNODREL ON THE TESTOSTERONE-DEPENDENT PROCESS OF FRUCTOSE FORMATION IN MOUSE SEX ACCESSORY ORGANS

1966 ◽  
Vol 51 (2) ◽  
pp. 224-230 ◽  
Author(s):  
John A. Thomas ◽  
Edward T. Knych
Keyword(s):  
Antagonistic Activity ◽  
Low Doses ◽  
Antagonistic Action ◽  
Dependent Process ◽  
High Doses

ABSTRACT Norethynodrel antagonized the fructose stimulating effects of exogenous testosterone in sex accessory organs of castrate mice. It was antiandrogenic at both low doses (50 μg) and high doses (400 μg) of testosterone. Norethindrone and ethisterone suppressed fructose formation in the testosterone-treated castrate mouse, but not as effectively as norethynodrel. Norethandrolone exerted no antagonistic activity.

scholarly journals Antifertility Actions of a-Chlorohydrin in the Male

1983 ◽  
Vol 36 (4) ◽  
pp. 333 ◽  
Author(s):  
A RJones
Keyword(s):  
Male Fertility ◽  
Human Sperm ◽  
Male Rat ◽  
Low Doses ◽  
Dose Regime ◽  
Male Contraceptive ◽  
The Past ◽  
High Doses ◽  
Species Specific ◽  
Daily Oral Administration

Non-steroidal chemicals that affect male fertility have been known for over 25 years but only one compound, oc-chlorohydrin, possesses most of the attributes of an ideal male contraceptive. In the male rat, for example, continuous daily oral administration of low doses produces an almost immediate and continuous antifertility response that ceases when treatment is withdrawn. Such a dose regime does not interfere with libido, is apparently not toxic and the action is specific towards mature sperm. Furthermore, the action of the compound is species-specific: it is effective in the rat, ram, boar, guinea pig, hamster,rhesus monkey and upon ejaculated human sperm but it is ineffective in the mouse and the rabbit. High doses of oc-chlorohydrin can be neurotoxic, nephrotoxic and, in rats, lead to prolonged or permanent infertility. However, the antifertility response and the toxicity of racemic oc-chlorohydrin may be due, respectively, to the separate enantiomers. No other antifertility chemical has been investigated to such an extent as oc-chlorohydrin; this article reviews the progress that has been achieved with oc-chlorohydrin during the past six years.

scholarly journals The Effect of an Encapsulated Nutrient Mixture on Food Intake and Satiety: A Double-Blind Randomized Cross-Over Proof of Concept Study

Nutrients ◽  
2018 ◽  
Vol 10 (11) ◽  
pp. 1787 ◽  
Author(s):  
Annick Alleleyn ◽  
Mark van Avesaat ◽  
Dina Ripken ◽  
Sinéad Bleiel ◽  
Daniel Keszthelyi ◽  
...  
Keyword(s):  
Small Intestine ◽  
Food Intake ◽  
Area Under The Curve ◽  
Double Blind ◽  
Distal Small Intestine ◽  
Active Product ◽  
Non Invasive ◽  
Control Product ◽  
Scale Scores ◽  
And Control

Activation of the intestinal brake by infusing nutrients into the distal small intestine with catheters inhibits food intake and enhances satiety. Encapsulation of macronutrients, which protects against digestion in the proximal gastrointestinal tract, can be a non-invasive alternative to activate this brake. In this study, we investigate the effect of oral ingestion of an encapsulated casein and sucrose mixture (active) targeting the distal small intestine versus a control product designed to be released in the stomach on food intake, satiety, and plasma glucose concentrations. Fifty-nine volunteers received the active and control product on two separate test days. Food intake was determined during an ad libitum meal 90 min after ingestion of the test product. Visual analogue scale scores for satiety and blood samples for glucose analysis were collected at regular intervals. Ingestion of the active product decreased food intake compared to the control product (655 kcal compared with 699 kcal, respectively, p < 0.05). The area under the curve (AUC) for hunger was decreased (p < 0.05) and AUC for satiety was increased (p < 0.01) after ingestion of the active product compared to the control product. Ingestion of an encapsulated protein-carbohydrate mixture resulted in inhibition of food intake compared to a non-encapsulated control product.

Sequence, tissue distribution, and functional characterization of the rat fructose transporter GLUT5

1993 ◽  
Vol 264 (6) ◽  
pp. G1169-G1176 ◽  
Author(s):  
E. B. Rand ◽  
A. M. Depaoli ◽  
N. O. Davidson ◽  
G. I. Bell ◽  
C. F. Burant
Keyword(s):  
Small Intestine ◽  
Functional Characterization ◽  
Cdna Probe ◽  
Amino Acid Identity ◽  
Human Testis ◽  
Cdna Clones ◽  
Rat Tissues ◽  
Rat Small Intestine ◽  
Cross Hybridization ◽  
Distal Small Intestine

cDNA clones encoding rat GLUT5-small intestinal facilitative hexose transporter were isolated from a jejunum library by cross-hybridization with a human GLUT5 cDNA probe. The cDNA sequence indicates that rat GLUT5 is composed of 502 amino acids and has 81.5% amino acid identity and 87.3% similarity with the sequence of human GLUT5. Expression of synthetic rat GLUT5 mRNA in Xenopus oocytes showed that rat GLUT5 was able to mediate the uptake of fructose and, to a lesser extent, of glucose. RNA blotting studies showed that GLUT5 mRNA was present in rat small intestine, kidney, and brain. Although GLUT5 mRNA is expressed in human testis, adipose tissue, and skeletal muscle, it could not be detected by RNA blotting in these rat tissues. Developmental studies showed low levels of GLUT5 mRNA in rat small intestine and kidney during the prenatal period with a rapid induction of GLUT5 expression occurring postnatally. In situ hybridization studies of GLUT5 mRNA expression in the small intestine revealed differential expression along the crypt-villus axis with the highest levels of mRNA being in the midvillus region. In addition, there was quantitatively more GLUT5 mRNA detected in the proximal as opposed to the distal small intestine.

Oxidation of glucose carbon entering the TCA cycle is reduced by glutamine in small intestine epithelial cells

1995 ◽  
Vol 268 (6) ◽  
pp. G879-G888 ◽  
Author(s):  
C. E. Kight ◽  
S. E. Fleming
Keyword(s):  
Small Intestine ◽  
Epithelial Cells ◽  
Glucose Oxidation ◽  
Tca Cycle ◽  
Proximal Segment ◽  
Distal Small Intestine ◽  
Glucose Carbon ◽  
The Tca Cycle ◽  
Oxidation Of Glucose ◽  
In Cells

The influence of glutamine on glucose oxidation was assessed in epithelial cells isolated from the mucosa of the proximal, mid-, and distal small intestine of young, fed, male rats. Glucose oxidation declined along the length of the small intestine, with values from the mid- and distal segments representing approximately 55% and 40%, respectively, of the value from the proximal segment. A gradient along the small intestine was noted also in the influence of glutamine on glucose oxidation: glutamine suppressed glucose oxidation approximately 60% in the proximal small intestine, 39% in the mid-intestine, and 31% in the distal small intestine. Glutamine suppressed the oxidation of glucose carbon that entered the tricarboxylic acid (TCA) cycle; this was determined using CO2 ratios derived from acetate and glucose isotopes. In cells from the proximal segment, the probability that carbon entering the cycle would complete one full turn was reduced by glutamine from 0.77 to 0.28. The entry of glucose-derived pyruvate into the TCA cycle did not appear to be influenced by the presence of glutamine, however. Glutamine had no influence on the proportion of glucose metabolism that occurred via the pentose phosphate pathway (which averaged 5% or less), but reduced flux of carbon through pyruvate carboxylase relative to flux through pyruvate dehydrogenase from 40% to 9% in cells from the proximal segment. These data suggest that, in the presence of glutamine, the fate of pyruvate carbon (derived from glucose or elsewhere) entering the TCA cycle is altered from that of oxidation to anaplerosis and subsequent efflux of TCA cycle intermediates into newly synthesized compounds.

Sodium, potassium, and intestinal transport of glucose, l-tyrosine, phosphate, and calcium

1963 ◽  
Vol 205 (1) ◽  
pp. 107-111 ◽  
Author(s):  
Harold E. Harrison ◽  
Helen C. Harrison
Keyword(s):  
Small Intestine ◽  
Calcium Transport ◽  
Inorganic Phosphate ◽  
Choline Chloride ◽  
Sodium Concentration ◽  
Phosphate Transport ◽  
Metabolic Energy ◽  
Transport Systems ◽  
Bicarbonate Buffer ◽  
Distal Small Intestine

Everted loops of rat small intestine were incubated in media varying in their concentrations of sodium and potassium. Reduction of sodium concentration was effected by substitution of choline chloride in equimolar amounts for sodium chloride in the saline-bicarbonate buffer. Concentrative transport of glucose, l-tyrosine, inorganic phosphate, and calcium was measured by determination of the final ratio of the concentrations of the solute in serosal and mucosal fluids, and the increment of the solute in serosal fluid during incubation. Ca45 was used as an indicator of calcium distribution. The glucose, l-tyrosine, and inorganic phosphate transport systems require sodium, and at a submaximal concentration of sodium an increased concentration of potassium is inhibitory. The calcium transport system does not require sodium and in loops from the distal small intestine calcium transport is enhanced by reduction of sodium concentration in the medium. It is postulated that there is a common sodium-requiring system which is necessary for the linkage of metabolic energy to glucose, amino acid, and inorganic phosphate transport.

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