Comparison of Pharmacodynamic Effects and Plasma Levels of Oral and Rectal Ergotamine

Cephalalgia ◽  
1986 ◽  
Vol 6 (2) ◽  
pp. 107-111 ◽  
Author(s):  
PM Bülow ◽  
JJ Ibraheem ◽  
G Paalzow ◽  
P Tfelt-Hansen

Plasma levels and the vasoconstrictive effect of 1 mg ergotamine tartrate given as tablets or suppositories were compared. In a crossover study, eight male volunteers received tablets or suppositories containing ergotamine in a drug combination (Anervan®) and, as a control, suppositories without ergotamine. Blood sampling and measurement of toe-arm systolic gradients with a strain-gauge technique were done for up to 6 h and again after 24 h and 48 h. Only 29 of 160 blood samples contained detectable (>0.1 mg/ml) amounts of ergotamine, and kinetic comparison could not be performed. Only ergotamine-containing suppositories caused a significant ( p < 0.008) decrease in toe-arm systolic gradient which was significantly different ( p < 0.003) from the effects of ergotamine tablets and control suppositories. Rectal ergotamine is thus more biologically active, for the factor used, than oral ergotamine. We suggest that a rectal dose of 1 mg ergotamine tartrate should be tried as the initial dose in the treatment of migraine attacks.

Cephalalgia ◽  
1985 ◽  
Vol 5 (3_suppl) ◽  
pp. 52-53
Author(s):  
P. Bülow ◽  
J.J. Ibraheem ◽  
L. Paalzow ◽  
P. Tfelt-Hansen

2021 ◽  
Vol 8 ◽  
Author(s):  
Zahra Solati ◽  
Arun Surendran ◽  
Andrea Edel ◽  
Marynia Roznik ◽  
David Allen ◽  
...  

Objective: ST-segment Elevation Myocardial Infarction (STEMI) occurs as a result of acute occlusion of the coronary artery. Despite successful reperfusion using percutaneous coronary intervention (PCI), a large percentage of myocardial cells die after reperfusion which is recognized as ischemia/reperfusion injury (I/R). Oxidized phosphatidylcholines (OxPCs) are a group of oxidized lipids generated through non-enzymatic oxidation and have pro-inflammatory properties. This study aimed to examine the roles of OxPCs in a clinical setting of myocardial I/R.Methods: Blood samples were collected from STEMI patients at presentation prior to primary PCI (PPCI) (Isch) and at 4 time-points post-PPCI, including 2 h (R-2 h), 24 h (R-24 h), 48 h (R-48 h), and 30 days (R-30 d) post-PPCI. As controls, blood samples were collected from patients with non-obstructive coronary artery disease after diagnostic coronary angiography. Aspiration thrombectomy was also performed in selected STEMI patients. High-performance lipid chromatography-electrospray mass spectrometry (LC-MS/MS) was used for OxPCs analysis.Results: Twenty-two distinct OxPC species were identified and quantified in plasma samples in patients presenting with STEMI. These compounds were categorized as fragmented and non-fragmented species. Total levels of OxPCs did not significantly differ between Isch and control groups. However, total levels of fragmented OxPCs increased significantly in the ischemic period compared with controls (Isch: 4.79 ± 0.94, Control: 1.69 ± 0.19 ng/μl of plasma, P &lt; 0.05). Concentrations of non-fragmented OxPCs had significant reductions during ischemia compared to the control group (Isch: 4.84 ± 0.30, Control: 6.6 ± 0.51 ng/μl, P &lt; 0.05). Levels of total OxPCs in patients with STEMI were not significantly different during reperfusion periods. However, fragmented OxPCs levels were elevated at 48 h post-reperfusion and decreased at 30 days following MI, when compared to R-2 h and R-24 h time points (Isch: 4.79 ± 0.94, R-2 h: 5.33 ± 1.17, R-24 h: 5.20 ± 1.1, R-48 h: 4.18 ± 1.07, R-30 d: 1.87 ± 0.31 ng/μl, P &lt; 0.05). Plasma levels of two fragmented OxPCs, namely, POVPC and PONPC were significantly correlated with peak creatine kinase (CK) levels (P &lt; 0.05). As with plasma levels, the dominant OxPC species in coronary aspirated thrombus were fragmented OxPCs, which constituted 77% of total OxPC concentrations.Conclusion: Biologically active fragmented OxPC were elevated in patients presenting with STEMI when compared to controls. PONPC concentrations were subsequently increased after PPCI resulting in reperfusion. Moreover, levels of POVPC and PONPC were also associated with peak CK levels. Since these molecules are potent stimulators for cardiomyocyte cell death, therapeutics attenuating their activities can result in a novel therapeutic pathway for myocardial salvage for patients undergoing reperfusion therapy.


2020 ◽  
Vol 90 (5-6) ◽  
pp. 411-416 ◽  
Author(s):  
Carina Kolot ◽  
Ana Rodriguez-Mateos ◽  
Rodrigo Feliciano ◽  
Katharina Bottermann ◽  
Wilhelm Stahl

Abstract. Chalcones are a type of flavonoids characterized by an α-β unsaturated structural element which may react with thiol groups to activate pathways such as the Nrf2-Keap-1 system. Naringenin chalcone is abundant in the diet but little is known about its bioavailability. In this work, the bioavailability of naringenin chalcone from tomatoes was investigated in a group of healthy men (n=10). After ingestion of 600 grams of tomatoes providing a single dose of 17.3 mg naringenin chalcone, 0.2 mg of naringenin, and 195 mg naringin plasma levels of free and conjugated naringenin and naringenin chalcone (glucuronide and sulfate) were analyzed by UHPLC-QTOF-MS at 0.5, 1, 3, and 6 h post-consumption. Plasma levels of conjugated naringenin increased to about 12 nmol/L with a maximum at about 3 h. Concentrations of free naringenin hardly elevated above baseline. Plasma levels of free and conjugated naringenin chalcone significantly increased. A maximum of the conjugated chalcone was reached at about 3 h after ingestion with an average concentration of about 0.5 nmol/L. No free chalcone was detectable at baseline but low amounts of the unconjugated compound could be detected with an average maximum of 0.8 nmol/L at about 1 h after ingestion. The data demonstrate that naringenin chalcone is bioavailable in humans from cherry tomatoes as a dietary source. However, availability is poor and intramolecular cyclisation as well as extended metabolism likely contribute to the inactivation of the reactive alpha-beta unsaturated reactive center as well as the excretion of the biologically active molecule, respectively.


2014 ◽  
Vol 1 (3) ◽  
pp. 3-7
Author(s):  
O. Zhukorskyy ◽  
O. Hulay

Aim. To estimate the impact of in vivo secretions of water plantain (Alisma plantago-aquatica) on the popula- tions of pathogenic bacteria Erysipelothrix rhusiopathiae. Methods. The plants were isolated from their natural conditions, the roots were washed from the substrate residues and cultivated in laboratory conditions for 10 days to heal the damage. Then the water was changed; seven days later the selected samples were sterilized using fi lters with 0.2 μm pore diameter. The dilution of water plantain root diffusates in the experimental samples was 1:10–1:10,000. The initial density of E. rhusiopathiae bacteria populations was the same for both experimental and control samples. The estimation of the results was conducted 48 hours later. Results. When the dilution of root diffusates was 1:10, the density of erysipelothrixes in the experimental samples was 11.26 times higher than that of the control, on average, the dilution of 1:100 − 6.16 times higher, 1:1000 – 3.22 times higher, 1:10,000 – 1.81 times higher, respectively. Conclusions. The plants of A. plantago-aquatica species are capable of affecting the populations of E. rhusiopathiae pathogenic bacteria via the secretion of biologically active substances into the environment. The consequences of this interaction are positive for the abovementioned bacteria, which is demon- strated by the increase in the density of their populations in the experiment compared to the control. The intensity of the stimulating effect on the populations of E. rhusiopathiae in the root diffusates of A. plantago-aquatica is re- ciprocally dependent on the degree of their dilution. The investigated impact of water plantain on erysipelothrixes should be related to the topical type of biocenotic connections, the formation of which between the test species in the ecosystems might promote maintaining the potential of natural focus of rabies. Keywords: Alisma plantago-aquatica, in vivo secretions, Erysipelothrix rhusiopathiae, population density, topical type of connections.


Author(s):  
M. M. Chaudhary ◽  
C. T. Khasatiya ◽  
S. B. Patel ◽  
S. S. Chaudhary ◽  
V. B. Atara ◽  
...  

The serum progesterone and estradiol profiles during synchronization of estrus by buck effect and PGF2α treatments were monitored in Surti does. Total eighteen non-pregnant does selected were evenly divided into 3 groups, 6 does in each group. The does of Group I were teased with a sexuallyactive- apronized buck; and those of Group II were treated with PGF2α, i.e., Inj. Lutalyse® @ 7.5 mg/doe IM twice 11 days apart, while the Group III served as untreated control. Blood samples were collected from all the animals on day 0 (before 1st PGF2α injection), 3rd day (during treatment), 11th day (before 2nd PGF2α injection), 14th day (after treatment) and 40th day (post-service) by jugular vein puncture. The serum separated was stored at -20°C till further analysis. In all the three groups, 83.33% does, conceived at first service in the sampling cycle. The overall mean serum progesterone concentration of Group I does (5.82±0.72 ng/ml) was significantly higher (p less than 0.01) as compared to Group II (2.93±0.38 ng/ml) and III (2.88±0.30 ng/ml). Similarly, the overall mean serum progesterone concentration of Surti does on day 0 (2.65±0.46 ng/ml), 3rd (2.56±0.80 ng/ml), 11th (4.45±0.84 ng/ml) and 14th (3.40±0.63 ng/ml) did not differ significantly, but the overall mean level at day 40 (6.31±0.45 ng/ml) was significantly (p less than 0.01) higher, because most of animals became pregnant at that time. The overall mean serum oestradiol-17β levels of Group I (24.40±2.98 pg/ ml) was significantly higher (p less than 0.01) than in Group II (15.77±1.77 pg/ml) and III (12.21±1.45 pg/ ml). On the other hand, the overall mean serum oestradiol-17β levels of Surti does on day 0 (12.89±1.21 pg/ml), 3rd (15.84±1.74 pg/ml), 11th (14.81±1.96 pg/ml), 14th (22.15±2.97 pg/ml) and 40th (21.64±5.16 pg/ml) did not differ significantly (p>0.05) and the slightly higher overall mean level found at 40th day might be the influence of the non-pregnant does at first service in the cumulative animals. The hormonal profile reflected the initiation of cyclicity and establishment of pregnancy in treated and control animals.


2021 ◽  
Vol 9 (6) ◽  
pp. 1163
Author(s):  
Eduarda Alexandra Gonçalves de Oliveira Moura ◽  
Daniela Gomes da Silva ◽  
Caio Henrique Turco ◽  
Thainara Vitoria Carnevalli Sanches ◽  
Gabriel Yuri Storino ◽  
...  

Since the occurrence of swine salmonellosis has increased over time and control strategies other than biosecurity are highly recommended, the present study aimed to evaluate the efficacy of vaccination with Salmonella Choleraesuis and Salmonella Typhimurium bacterins in pigs. Two experimental groups were formed: G1, animals immunized with two doses of a commercial vaccine (n = 20); G2, control group (n = 20). After vaccination, all pigs were orally challenged (D0) with 108 CFU of Salmonella Typhimurium and evaluated for 40 days. Every 10 days after D0, five piglets from each experimental group were euthanized and submitted to the necroscopic examination, when organ samples were collected. Blood samples and rectal swabs were collected before the first dose of the vaccine (D−42), before the second dose (D−21), before the challenge (D0), and thereafter, every three days until D39. Blood count, serum IgG measurement by ELISA, and the excretion of Salmonella Typhimurium in feces were evaluated. While the results from blood count and serum IgG concentration did not differ, the detection and excretion of Salmonella between G1 and G2 differed (p < 0.05). Therefore, it was observed that this vaccine partially protected the animals against experimental infection with Salmonella Typhimurium, reducing the excretion of bacteria in feces.


2000 ◽  
Vol 69 (Supplement) ◽  
pp. S402 ◽  
Author(s):  
Pablo J. Inigo ◽  
Josep M. Campistol ◽  
Sergio Lario ◽  
Monica Bescos ◽  
Carlos Piera ◽  
...  

1974 ◽  
Vol 77 (2) ◽  
pp. 401-407 ◽  
Author(s):  
J. A. Mahoudeau ◽  
A. Delassalle ◽  
H. Bricaire

ABSTRACT Plasma levels of testosterone (T) and 5α-dihydrotestosterone (DHT) were determined by radioimmunoassay in 29 patients with benign prostatic hypertrophy (BPH) and in 56 control men of various ages. No significant difference was found in T, DHT nor DHT/T ratio between BPH and control subjects of similar age. Plasma DHT was higher in the prostatic than in the peripheral veins in 8/9 patients with BPH during laparotomy, indicating a prostatic secretion of DHT. No difference in the mean T nor the mean DHT was found in peripheral plasma before and after adenomectomy.


1989 ◽  
Vol 123 (2) ◽  
pp. 173-179 ◽  
Author(s):  
B. K. Campbell ◽  
A. S. McNeilly ◽  
D. T. Baird

ABSTRACT In sheep, secretion of oestradiol by the ovary is stimulated by pulses of LH but the factors controlling ovarian inhibin secretion are not well understood. We have investigated the effect of a single injection of LH on the ovarian secretion of inhibin. Six anoestrous Finn–Merino ewes which had one ovary autotransplanted to a site in the neck had jugular and timed ovarian venous blood samples collected at 10-min intervals for a total of 5 h. The secretion rates of both inhibin (1–3 ng/min) and oestradiol (0·5–8 ng/min) were similar to those observed during the breeding season indicating significant follicular development in these animals. After injection of 2·5 μg NIH-LH-S25 intravenously the concentration of LH in plasma rose from a baseline of 1·8 ±0·1 (s.e.m.) μg/l to a peak of 3·9 ±0·3 μg/l (P<0·01). This LH pulse stimulated a corresponding increase (P<0·01) in oestradiol secretion from a basal level of 0·9±0·2 ng/min to a peak of 4·6±0·6 ng/min that occurred within 30 min of injection. Although inhibin secretion was episodic in nature, increases were not related to either exogenous or endogenous LH pulses. We conclude that, in contrast to oestradiol, the secretion of inhibin by the ovary is not controlled acutely by changes in plasma levels of LH during anoestrus. Journal of Endocrinology (1989) 123, 173–179


1992 ◽  
Vol 263 (2) ◽  
pp. R258-R266 ◽  
Author(s):  
A. M. Schreihofer ◽  
A. F. Sved

To determine the role of the nucleus tractus solitarius (NTS) in the tonic maintenance of arterial pressure (AP) following chronic baroreceptor denervation, the present study examined the effect of inhibition of the NTS on AP in chronic sinoaortic denervated (SAD) and control rats. One to two weeks after complete SAD (no residual arterial baroreceptor reflexes) mean AP was not significantly different from that of control rats. Bilateral microinjections of muscimol and lidocaine into the NTS markedly increased AP in alpha-chloralose-anesthetized control rats. However, microinjections of these neuroinhibitory drugs had no effect on AP in SAD rats. Similarly, 1 h after bilateral destruction of the NTS conscious control rats were hypertensive, while AP in SAD rats was not changed. Plasma levels of vasopressin (VP), which were also elevated in control rats 1 h after NTS lesions, were not significantly altered in SAD rats. These results demonstrate that inhibition of the NTS has no effect on AP or plasma levels of VP in chronic SAD rats. This suggests neither the NTS nor afferents to the NTS supply a tonic inhibitory influence on AP after chronic baroreceptor denervation.


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