Somatostatin plasma levels and biological effects following subcutaneous administration of somatostatin in man

1986 ◽  
Vol 113 (4) ◽  
pp. 465-470
Author(s):  
L. Uccioli ◽  
G. Ghirlanda ◽  
P. Cotroneo ◽  
A. Manto ◽  
A. Solini ◽  
...  
Keyword(s):  
Plasma Levels ◽  
Subcutaneous Injection ◽  
Bolus Injection ◽  
Biological Effects ◽  
Subcutaneous Administration ◽  
Normal Subjects ◽  
Transient Effect ◽  
Continuous Administration ◽  
Single Subcutaneous Injection ◽  
Insulin Levels

Abstract. The rate at which somatostatin appears in the circulation after subcutaneous bolus injection and continuous administration by pump was determined in normal subjects by serial radioimmunoassays of immunoreactive somatostatin. Following a single subcutaneous injection of 250 μg, the somatostatin peak in plasma appeared after 5 min and had only a transient effect on insulin levels. During continuous administration, somatostatin reached levels able to reduce significantly insulin and glucagon. Somatostatin plasma levels exerting biological effects were observed during the subcutaneous administration of the peptide.

scholarly journals Features of experimental modeling of tuberculosis in guinea pig with the participation of N'-(2-(5-((thephylline-7' yl)methyl)-4-R-1,2,4-triazole- ylthio)acethyl)isonicotinohydrazide

2020 ◽  
Vol 10 (4) ◽  
pp. 191-194
Author(s):  
A.S. Gotsulya ◽  
V.V. Zazhzharskiy ◽  
P.O. Davidenko
Keyword(s):  
Guinea Pig ◽  
Microscopic Examination ◽  
Subcutaneous Injection ◽  
Subcutaneous Administration ◽  
Toxic Effects ◽  
Internal Organs ◽  
Single Subcutaneous Injection ◽  
Morphological Abnormalities ◽  
Veterinary Practice ◽  
High Degree

In this study, no toxic effects were detected after single subcutaneous injection of 40 mg/kg tadpoles. The results of macro- and microscopic examination of the internal organs 14 days after single subcutaneous administration of N'-(2-(5-((thephylline-7'-yl)methyl)-4-ethyl-1,2,4-triazole-3-ylthio)acethyl)isonicotino-hydrazide (GKP-305) at a dose of 20, 40 mg/kg showed the absence of any anatomical and morphological abnormalities in the tissue structures of the tentacles. The calculated value of the drug indicates a high degree of safety GKP-305 and its prospects for veterinary practice as an effective and safe tuberculocidal drug.

Plasma Heparin Levels and Patient Acceptability with Subcutaneous Heparin Sodium and Heparin Calcium

1979 ◽  
Author(s):  
J. Bonnar ◽  
P.T.S. Ma
Keyword(s):  
Plasma Levels ◽  
Subcutaneous Administration ◽  
Late Pregnancy ◽  
Normal Subjects ◽  
Patient Acceptability ◽  
Double Blind ◽  
Duration Of Action ◽  
Heparin Sodium ◽  
Subcutaneous Heparin ◽  
Plasma Heparin

A double-blind crossover trial in 40 normal subjects was carried out using 5,000 and 10,000 USP units of heparin sodium and heparin calcium given subcutaneously. Plasma heparin was measured by the antifactor Xa method and also using the substrate S-2222. Heparin sodium was found to have a longer duration of action and a greater total absorption than heparin calcium. A second double-blind crossover study in 30 subjects was carried out to determine patient acceptability of self administered subcutaneous heparin (5000 USP units). A preference for heparin sodium was expressed by 77.4% of the subjects and 9.7% preferred heparin calcium, the remainder found no difference. Heparin calcium was found to be significantly more painful during injection than heparin sodium (p< 0. 001). Plasma levels of heparin after subcutaneous administration of 5,000, 7,500 and 10,000 units of heparin sodium and heparin calcium were studied in late pregnancy between 30 and 40 weeks gestation. A wide individual variation was found but none had plasma levels above 0.40 units per ml after 10,000 units 12 hourly. During late pregnancy a regimen of 5000 units of heparin sodium given 8 hourly is safe; a higher dosage of heparin calcium is required to achieve similar levels of plasma heparin.

Repetitive and continuous administration of human corticotropin releasing factor to human subjects

1986 ◽  
Vol 112 (2) ◽  
pp. 157-165 ◽  
Author(s):  
J. Schopohl ◽  
A. Hauer ◽  
T. Kaliebe ◽  
G. K. Stalla ◽  
K. von Werder ◽  
...  
Keyword(s):  
Adrenal Insufficiency ◽  
Bolus Injection ◽  
Human Subjects ◽  
Normal Subjects ◽  
Pituitary Hormones ◽  
Corticotropin Releasing Factor ◽  
Secondary Adrenal Insufficiency ◽  
Continuous Administration ◽  
Pulsatile Administration

Abstract. ACTH secretion was studied in response to repetitive and continuous administration of human corticotropin releasing factor (CRF) in 14 healthy volunteers and 2 patients with secondary adrenal insufficiency. ACTH increases during repetitive CRF administration were within the same range in normal subjects independent of the intervals (60– 180 min) between the CRF pulses (100 μg iv). When CRF was infused continuously (100 μg/h for 3 h) after an initial CRF bolus injection (100 μg iv), ACTH and cortisol remained elevated during the infusion at a nearly constant level (ACTH: 60 ± 5 pg/ml; cortisol: 21.2 ± 1 μg/dl; x̄ ± se). A second CRF bolus injection at the end of the infusion did not lead to a significant further increase of ACTH and cortisol levels. This shows that there is no desensitisation or depletion of a ready releasable pool, as it is observed with other pituitary hormones after releasing hormone stimulation. Pulsatile administration of CRF in 2 patients with secondary adrenal insufficiency due to previous cortisol or glucocorticoid excess, respectively, revealed a blunted response to the first pulse which became normal after the following pulses. The latter could not be sustained until the next morning without CRF given overnight. These findings point to a hypothalamic defect being the cause of hypocortisolism after long-term cortisol suppression.

scholarly journals Baseline and stimulated catecholamine secretion in normotensive patients with active acromegaly: acute effects of continuous octreotide infusion

2000 ◽  
pp. 179-186 ◽  
Author(s):  
GD Rio ◽  
A Velardo ◽  
C Mascadri ◽  
G Zalteri ◽  
G Papi ◽  
...  
Keyword(s):  
Plasma Levels ◽  
Cardiovascular Responses ◽  
Normal Subjects ◽  
Cardiovascular Complications ◽  
Left Ventricular ◽  
Upright Posture ◽  
Continuous Administration ◽  
Octreotide Treatment ◽  
Active Acromegaly ◽  
Few Data

OBJECTIVE: Alterations in catecholamine plasma levels may contribute to the cardiovascular complications of acromegaly. Since few data are available on the catecholamine secretory dynamics in active acromegaly and no evidence exists on catecholamine variations during GH decrease, we studied acromegalic patients before and during octreotide administration. METHODS: We evaluated the catecholamine responses to upright posture and a cold pressure test (CPT) in 11 acromegalic (A) patients before and during continuous administration of octreotide (500 microgram/24h by s.c. pump) compared with 11 normal (N) subjects. RESULTS: All the acromegalic patients showed left ventricular cardiac hypertrophy. The cardiovascular responses to upright posture were similar between normal subjects and acromegalics both before and during octreotide treatment. The basal levels of norepinephrine (NE) were significantly higher in A patients compared with N subjects (423+/-45 vs 264+/-32pg/ml, P<0. 05) and decreased during therapy (291+/-32pg/ml; P<0.01). The increase in plasma NE during upright posture was significantly lower in A than in N subjects (P<0.01), but was restored to normal during octreotide treatment. CPT increased systolic and diastolic blood pressure, pulse rate and NE plasma levels in N (P<0.05) but not in A subjects both before and during octreotide treatment. CONCLUSIONS: Our data demonstrate the presence of increased basal NE levels in acromegalic patients with a defective sympathetic response to stimuli. Short-term octreotide infusion is able to induce a reduction in the basal levels of NE and a normalization of the catecholamine response to posture.

Parallel Reduction of Plasma Levels of High and Low Molecular Weight Kininogen in Patients with Cirrhosis

1999 ◽  
Vol 82 (11) ◽  
pp. 1428-1432 ◽  
Author(s):  
Cheryl Scott ◽  
Francesco Salerno ◽  
Elettra Lorenzano ◽  
Werner Müller-Esterl ◽  
Angelo Agostoni ◽  
...  
Keyword(s):  
Molecular Weight ◽  
Liver Disease ◽  
Liver Function ◽  
Plasma Levels ◽  
Plasma Concentrations ◽  
Normal Subjects ◽  
Low Molecular Weight ◽  
Major Band ◽  
Sds Page ◽  
Normal Controls

SummaryLittle is known about the regulation of high-molecular-weight-kininogen (HK) and low-molecular-weight-kininogen (LK) or the relationship of each to the degree of liver function impairment in patients with cirrhosis. In this study, we evaluated HK and LK quantitatively by a recently described particle concentration fluorescence immunoassay (PCFIA) and qualitatively by SDS PAGE and immunoblotting analyses in plasma from 33 patients with cirrhosis presenting various degrees of impairment of liver function. Thirty-three healthy subjects served as normal controls. Patients with cirrhosis had significantly lower plasma levels of HK (median 49 μg/ml [range 22-99 μg/ml]) and LK (58 μg/ml [15-100 μg/ml]) than normal subjects (HK 83 μg/ml [65-115 μg/ml]; LK 80 μg/ml [45-120 μg/ml]) (p < 0.0001). The plasma concentrations of HK and LK were directly related to plasma levels of cholinesterase (P < 0.0001) and albumin (P < 0.0001 and P < 0.001) and inversely to the Child-Pugh score (P < 0.0001) and to prothrombin time ratio (P < 0.0001) (reflecting the clinical and laboratory abnormalities in liver disease). Similar to normal individuals, in patients with cirrhosis, plasma HK and LK levels paralleled one another, suggesting that a coordinate regulation of those proteins persists in liver disease. SDS PAGE and immunoblotting analyses of kininogens in cirrhotic plasma showed a pattern similar to that observed in normal controls for LK (a single band at 66 kDa) with some lower molecular weight forms noted in cirrhotic plasma. A slight increase of cleavage of HK (a major band at 130 kDa and a faint but increased band at 107 kDa) was evident. The increased cleavage of HK was confirmed by the lower cleaved kininogen index (CKI), as compared to normal controls. These data suggest a defect in hepatic synthesis as well as increased destructive cleavage of both kininogens in plasma from patients with cirrhosis. The decrease of important regulatory proteins like kininogens may contribute to the imbalance in coagulation and fibrinolytic systems, which frequently occurs in cirrhotic patients.

A Novel Chimaeric Derivative of Saruplase, rscu-PA-40kDA/Hir, Binds to Thrombin and Exerts Thrombus-specific Fibrinolysis in Arterial and Venous Thrombosis in Dogs

1997 ◽  
Vol 77 (03) ◽  
pp. 535-539 ◽  
Author(s):  
J Schneider ◽  
R Hauser ◽  
H-H Hennies ◽  
J Korioth ◽  
G Steffens ◽  
...  
Keyword(s):  
Venous Thrombosis ◽  
Plasma Levels ◽  
Time Course ◽  
Bolus Injection ◽  
Specific Activity ◽  
Intravenous Bolus ◽  
Protease Domain ◽  
Parent Molecule ◽  
Significant Prolongation ◽  
Inhibitory Domain

SummaryThe chimaeric molecule rscu-PA-40kDA/Hir (M23) comprises the kringle and protease domain of saruplase (rscu-PA) and a thrombin inhibitory domain fused to the C-terminus of the protease domain. The 27 amino acid long thrombin inhibitory domain contains a sequence directed to the active site of thrombin and a fragment from the C-terminal region of hirudin. 125I-radiolabelled M23 (0.03 µM) bound to thrombin that was immobilised onto CNBr-activated sepharose beads. Unlabelled M23 (0.01-10 |xM) and hirudin (0.001-10 µµM) concentra-tion-dependently displaced 125I-M23 from its binding to thrombin. Saruplase (up to 10 (iM) did not influence the thrombin binding of M23. The fibrinolytic properties of M23 and saruplase were compared in anaesthetized dogs with femoral artery and saphenous vein thrombosis. Under concomitant heparinization, the intravenous bolus injections of 1 mg/kg M23 or saruplase induced reperfusion of thrombotically occluded femoral arteries in 4 out of 5 treated animals in each case. There was one reocclusion in the M23-treated group. Time to reperfusion (23 ± 4 vs 25 ± 11 min) and maximal height of reperfusion blood flow (98 ± 21 vs 108 ± 15 % of baseline flow) did not differ significantly between the treatment groups. The time course of the lysis of incorporated 125I-fibrin radioactivity in thrombosed saphenous veins was similar after bolus injections of M23 and saruplase. The maximal dissolution of 125I-fibrin in the venous thrombosis model was 91 ± 1 % in M23-and 88 ± 5 % in saruplase-treated animals. Plasma levels of fibrinogen were not influenced and a2-antiplasmin levels were slightly reduced (-27 ± 3 %) after bolus injection of M23. In contrast, bolus injection of saruplase was accompanied by a significant decrease of fibrinogen (-55 ± 19 %) and a2-antiplasmin (-75 ±11%) plasma levels. Template bleeding times virtually did not differ before (2.8 ± 0.3 min) and 60 min after bolus injection of M23 (3.1 ± 0.3 min), whereas treatment with saruplase resulted in a significant prolongation of template bleeding time from 2.6 ± 0.2 min to 28 ± 13 min. It is concluded that the saruplase derivative M23, while inducing equieffective thrombolysis after intravenous bolus injection in dogs, causes much fewer haemostatic side effects than its parent molecule. The high thrombus-specific activity of M23 is tentatively attributed to its affinity to clot-bound thrombin.

Hemodynamic and renal effects following bolus injection of atrial natriuretic peptide (α-hANP) in normal subjects

1988 ◽  
Vol 117 (4_Suppl) ◽  
pp. S235-S236
Author(s):  
G. MÜLLER-ESCH ◽  
J. POTRATZ ◽  
W. KLINGLER ◽  
R. GERZER ◽  
R. LAWRENZ ◽  
...  
Keyword(s):  
Atrial Natriuretic Peptide ◽  
Natriuretic Peptide ◽  
Bolus Injection ◽  
Normal Subjects ◽  
Renal Effects ◽  
Atrial Natriuretic

Effect of [Asu,]eel calcitonin on prolactin release in normal subjects and patients with prolactinoma

1985 ◽  
Vol 108 (3) ◽  
pp. 297-304 ◽  
Author(s):  
Hidesuke Kaji ◽  
Kazuo Chihara ◽  
Naoto Minamitani ◽  
Hitoshi Kodama ◽  
Tetsuya Kita ◽  
...  
Keyword(s):  
Body Weight ◽  
Bolus Injection ◽  
Normal Subjects ◽  
Regular Insulin ◽  
Prolactin Release ◽  
Saline Administration ◽  
The Central Nervous System ◽  
Plasma Prl ◽  
Male Subjects

Abstract. The effect of [Asu]eel calcitonin (ECT), an equipotent analogue of eel CT, on prolactin (Prl) secretion was examined in 12 healthy male subjects and in 6 patients with prolactinoma. In healthy subjects, ECT (0.5 μg/kg body weight · h) or saline was infused for 2 h and TRH was injected iv as a bolus of 500 μg at 1 h of ECT or saline administration. ECT did not affect basal Prl levels during 1 h of infusion. TRH caused a significant increase of plasma Prl with peak values of 75.2 ± 11.6 ng/ml in ECT-infused subjects, which did not differ from those infused with saline (68.5 ± 8.3 ng/ml). Next, an iv bolus injection of regular insulin (0.1 U/kg body weight) was followed by an infusion of ECT or saline alone. Plasma Prl peaks after hypoglycaemic stress were significantly lower in ECT-infused subjects than those in saline-injected controls (ECT, 16.5 ± 3.1 vs 33.5 ± 9.6 ng/ml, P < 0.05). In patients with prolactinoma, basal levels of plasma Prl ranging from 42.0–4130 ng/ml failed to change during iv infusion of ECT. Moreover, ECT (10−9–10−6m) did not affect Prl release from prolactinoma tissues perifused in vitro. These findings suggest that ECT may not act directly on the pituitary to modify Prl release. Rather, peripherally administered ECT appears to suppress Prl release via the central nervous system.

Superovulatory response to single subcutaneous injection of Folltropin in Holstein and Sahiwal cows

1992 ◽  
Vol 37 (1) ◽  
pp. 260 ◽  
Author(s):  
A.K. Misra ◽  
S.A. Chaubal ◽  
G. Krishna Kishore ◽  
S. Rajeshwaran ◽  
B.V. Joshi ◽  
...  
Keyword(s):  
Subcutaneous Injection ◽  
Single Subcutaneous Injection ◽  
Sahiwal Cows

HORMONAL REQUIREMENTS FOR THE MAINTENANCE OF OESTRADIOL-INDUCED INHIBITION OF UTERINE SENSITIVITY IN THE OVARIECTOMIZED RAT

1970 ◽  
Vol 46 (3) ◽  
pp. 341-346 ◽  
Author(s):  
K. P. MEYERS
Keyword(s):  
Subcutaneous Injection ◽  
Ovariectomized Rats ◽  
Ovariectomized Rat ◽  
Single Subcutaneous Injection ◽  
The Third ◽  
Oestradiol Treatment ◽  
Progesterone Treatment ◽  
Endometrial Scratching

SUMMARY Ovariectomized rats treated with 2·5 or 5·0 mg. progesterone daily received a single subcutaneous injection of 0·2 μg. oestradiol on the third day of the progesterone treatment. The deciduomal response to trauma by endometrial scratching was used to determine the degree of uterine sensitivity at various times after oestradiol. Uterine sensitivity was partially and then completely lost 36 and 48 hr. after oestradiol administration. The inhibition of uterine sensitivity persisted until 9 and 11 days after oestradiol when the animals received 2·5 and 5·0 mg. progesterone daily. Uterine sensitivity was completely inhibited on day 11 with doses of oestradiol from 0·2 to 0·05 μg. Withdrawal of progesterone treatment for 48 or 72 hr., but not for 24 hr., after oestradiol treatment restored uterine sensitivity. These results show that the oestradiol-induced inhibition of uterine sensitivity in the progestational endometrium is maintained by continuous progesterone treatment and that the duration of this effect is dependent on the dose of progesterone given.

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