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PubMed1985

Effects of diethyldithiocarbamate, a metabolite of disulfiram, on the pharmacokinetics of alcohol and acetaldehyde in the rat.

The effects of diethyldithiocarbamate (DDC), a metabolite of disulfiram which is known as Antabuse, on the blood concentrations of alcohol and acetaldehyde were determined simultaneously by head space gas chromatography in rats. After an intravenous injection of alcohol, the blood concentration of acetaldehyde was much lower than that of the alcohol. A pharmacokinetic model featuring the liver compartment for acetaldehyde was used to estimate pharmacokinetic parameters on the assumption that the distribution volumes of the central compartments were same for alcohol and acetaldehyde, and that the elimination rate of acetaldehyde from liver was large enough to isolate the liver compartment from the central compartment. The results showed that the clearance of alcohol was 0.0226 l/min/kg and the elimination rate constant of acetaldehyde from the liver compartment was very large and 35 min-1. The administration of DDC decreased the above significantly to 0.0132 l/min/kg and 20 min-1, respectively. After intravenous infusion of acetaldehyde, the time course of the blood concentration of acetaldehyde was analyzed by the one compartment model. The estimated elimination rate constants from blood and the distribution volume were in good agreement with those calculated from alcohol injection, indicating the appropriateness of the method used in this study. DDC had no effect on the elimination of infused acetaldehyde from blood indicating that the elimination may be due to the loss from lungs into breath, from skin surfaces and/or from the kidney but not by metabolism in the liver.

Acetaldehyde↗

PubMed1987

[Centrally and peripherally induced anorectic actions of salmon calcitonin (sCT) in rats: separation of its novel derivative [Gly8]-sCT].

It has been reported based on animal studies that salmon calcitonin (sCT), besides hypocalcemic action, exhibits a variety of pharmacological actions. The anorectic action has been observed to ensue not only by central administration but also by peripheral injection, indicating that in clinical use to induce hypocalcemia or for other therapeutic purposes, the anorectic action may develop as a side effect. While studying the anorectic effect of [Gly8]-sCT in rats, a derivative of sCT having rather stronger hypocalcemic potency than the mother molecule, it was found that on peripheral injection, the derivative practically lacks the anorectic effect. Thus, a pharmacological evaluation of the novel peptide was made. When injected subcutaneously in rats at a dose level of 1 U/kg, sCT and the derivative induced similar patterns of hypocalcemia in either of which hypocalcemia reached a peak between 1 and 3 hr after injection. No notable difference existed between the action of the two peptides. In rats which were trained to take the daily food need within 2 hr (17:00 approximately 19:00), an intracerebroventricular injection of 1 U/rat of either peptide 30 min before food presentation significantly reduced both food and water intake, causing a loss of body weight as compared with the control which received the injection of saline alone. By subcutaneous injection of 100 U/kg, sCT was also active to decrease food and water intake. The effect was found to last longer than 24 hr and to cause a marked loss in body weight. In contrast, such effects did not develop in rats treated with the derivative. Both peptides were able to suppress the specific binding of 125I-sCT to the membrane fraction of rat brain and kidney.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗

PubMed1988

[An analysis of the morbid condition in adjuvant arthritic rats and a new method for evaluating anti-rheumatic drugs].

The progress of various symptoms in adjuvant arthritic rats (AA-rats) and the effects of anti-rheumatic drugs were continuously observed on the basis of the Weibull distribution function, and the following results were obtained: 1) The cumulative incidence rates F(t) of various symptoms and abnormalities of measured values gradually increased with the passage of time. The relationship between the F(t) and the days after adjuvant injection indicated a simple Weibull distribution function. On the other hand, the bone damages in the distal limb joints indicated a composite Weibull distribution function with two shape parameters (m1 and m2). It was possible to classify the animals into two groups, fast responders (m1) and slow responders (m2), according to the time of occurrence of bone damages. 2) By using the Weibull probability paper, it was possible to integrate and to evaluate in totality those cases with varying grades of symptoms and cases with different symptoms in the adjuvant-induced syndrome in rats. 3) Azathioprine (AZP) showed an inhibitory effect on the advents of pain and swelling and functional disorders, while indomethacin (IDM), prednisolone (PSL) and gold sodium thiomalate (GST) delayed the advents of these symptoms. As to bone damages in the distal limb joints, IDM, PSL and AZP showed an inhibitory effect in only the fast responder group, while GST showed both an inhibitory and delaying effect in both the fast responder group and the slow one. The above results suggest that the usage of the Weibull distribution function is useful not only for analysis of the morbid condition of AA-rats but also for the evaluation of anti-rheumatic drugs in AA-rats.

Animals↗

PubMed1991

Key role of complement activation and platelet-activating factor in exudate formation in zymosan-induced rat pleurisy.

Involvement of complement and platelet-activating factor (PAF) in zymosan-induced rat pleurisy was examined. Only a very low level of complement remained in the exudate at 1-5 hr after zymosan injection, indicating that complement activation had occurred during this period in the pleural cavity. When rats were injected with cobra venom factor (CVF) 24 hr prior to the zymosan injection to deplete complement, the exudate volumes at 0.5 and 5 hr after zymosan injection were significantly reduced. Furthermore, combined treatment with CVF and CV-6209, an antagonist of PAF, also significantly suppressed the exudation but to no further extent than the suppression by CVF alone, suggesting that the level of complement depletion achieved was sufficient to halt PAF synthesis/release. To see if complement activation is involved in PAF production, we examined the PAF production by resident leukocytes in response to zymosan in vitro. When pleural leukocytes were stimulated with zymosan in the presence of rat serum, PAF-like activity both in the medium and in the cellular fraction increased. If the serum was heat inactivated, no PAF-like activity was detected. These results suggest that initial activation of the complement system may occur in the pleural cavity by zymosan and that the activated complement may then stimulate the production of PAF, which in turn elicits the exudate.

Animals↗

PubMed1979

High thyroid radiation dose associated with 131-I-19-iodocholesterol adrenal scanning.

We have examined two patients undergoing 131I-19-iodocholesterol adrenal scans in order to assess thyroidal radiation dose. Thyroid uptakes of 3--5% of the administered 2 mCi dose were found despite prior administration of Lugol's iodine. Analysis of serum samples over a ten day period after iodocholesterol injection indicated that less than 10% of the radioactivity was free iodide. Kinetic results showed a high value for the thyroid/plasma 131I ratio indicating thyroid retention of 131I. This was substantiated by thyroid scintigrams. The thyroid radiation dose was estimated to be 200--250 rad for the two patients. The associated carcinogenic risk is of sufficient magnitude, in our opinion, to warrant regular follow-up of all patients who have undergone 131I-19-iodocholesterol adrenal scanning.

19-Iodocholesterol↗

PubMed1990

Bioavailability of iron and cyanide from 59Fe- and 14C-labelled hexacyanoferrates(II) in rats.

"Soluble" (KFe(III)[Fe(II)(CN)6]) and "insoluble Prussian blue" (Fe(III)4[Fe(II)(CN)6]3 labelled with 59Fe either in the ferric (Fe(III)) or ferro (Fe(II)) position and 14C in the cyanide group were synthesized and administered intraperitoneally or orally to adult female rats with normal body iron stores. Following i.p. injection of KFe[Fe(CN)6], the colloidal complex is disintegrated into ferric iron and hexacyanoferrate(II) anion almost completely. About 96% of the ferric iron was retained in the body. Nearly 90% of both ferrous iron and cyanide were excreted with the urine within 7 days after i.p. injection, indicating that most of the undissociated hexacyanoferrate(II) anion ([Fe(CN)6]4-) was excreted through the kidney. Only 9% of the ferrous iron from [Fe(CN)6]4- was found mainly in carcass, liver and gut. As the 59Fe/14C-ratios in organs were found close to 1.0, the dissociation of the hexacyanoferrate(II) anion can only be small in vivo. No detectable 14CO2-activity (less than 0.01%) was monitored in the breath of rats after i.p. injection of the 14C-labelled KFe[Fe(CN)6], also indicating that no significant amounts of cyanide were released after parenteral administration. After oral administration of the soluble and insoluble Prussian blue, 0.3-0.7% of the ferric iron was absorbed and retained mainly in carcass, liver and blood. Only 0.06-0.18% of the ferrous iron was absorbed and mostly excreted with the urine (0.05-0.15%), so that only 0.01-0.03% of the oral ferrous 59Fe was retained in the body after 7-10 days. Very small fractions of 14C-label from the 14CN-group of the soluble and insoluble hexacyanoferrate(II) were observed in the exhaled air (0.04-0.08% of the oral dose). From the 14CO2-exhalation, the 14C-urine excretion and the distribution of iron in blood and organs it can be concluded that the hexacyanoferrate(II) moiety disintegrated only to a small extent in the intestinal tract after oral administration. From a dose of 36 mg hexacyanoferrate(II)/kg, an amount of free (non-complex bound) cyanide can be calculated which is in maximum two orders of magnitude below the LD100-level. Thus, the very low bioavailability of iron and cyanide from hexacyanoferrate(II) compounds after oral application is demonstrated in rats. In the case of a severe nuclear accident, appropriate doses of "soluble" and "insoluble" Prussian blue can be used as safe and effective antidote against radiocaesium contamination.

Animals↗

PubMed1985

Orbital decompression in endocrine exophthalmos of Graves' disease.

Transantral decompression was performed bilaterally in 27 and unilaterally in 3 patients with endocrine exophthalmos of Graves' disease. In 28 patients there was an immediate reduction of proptosis and in about half of the patients in addition a marked decrease in chemosis and conjunctival injection indicating that these signs were mostly due to orbital vascular congestion. In one patient with exophthalmos of more than 2 years duration and progressive swelling of the eye muscles no response was observed. In another patient decompression did not reduce proptosis which, however, 4 months later responded to retrobulbar irradiation. In one further patient much more marked reduction of proptosis and disappearance of persistent periorbital swellings were obtained after glucocorticoid treatment given half a year after decompression. Postoperatively diplopia occurred in about half of the patients but corrective operations were required only in a quarter of the patients. Transantral decompression is an effective method for rapid treatment of progressive exophthalmos of Graves' disease. In patients with unilateral exophthalmos the asymmetry may be reversed after unilateral operation. The authors use decompression not only in the most severe cases (categories 5 and 6a-c according to the classification of the American Thyroid Association) but also in less severe cases (categories 2b-c and 3b-c) when there is a steady progression as a primary treatment possibly combined with other forms of therapy.

Adult↗

PubMed1993

GnRH-dependent and -independent components of FSH secretion after acute treatment of anoestrous ewes with ovine follicular fluid and a GnRH antagonist.

Gonadotrophin and inhibin concentrations were measured in anoestrous ewes after acute treatment with either saline, ovine follicular fluid (oFF), GnRH antagonist, or oFF and GnRH antagonist in combination. The increase in mean LH concentrations observed in ewes treated with oFF alone, was not seen in either of the groups treated with GnRH antagonist, in which LH pulsatility was completely inhibited. This result suggests that the LH rebound that follows follicular fluid treatment is GnRH dependent. Blockade of GnRH had no effect on the suppression of FSH seen after follicular fluid injection, indicating that this component of FSH secretion is independent of short-term GnRH input. After this initial suppression, a rebound release of FSH was seen in the group treated with oFF alone. The addition of GnRH antagonist appeared to decrease the rebound, suggesting that this rebound release of FSH may have a GnRH-dependent component. Inhibin concentrations in both oFF-treated groups increased after oFF injection and then declined to pretreatment values. However, a second rise in inhibin concentration, concomitant with the FSH rebound in ewes receiving oFF alone, was seen in the group treated with oFF and GnRH antagonist. As this rise in endogenous inhibin concentration could also act to suppress the rebound release of FSH, it cannot be conclusively proved from this study that GnRH input is required for the generation of the rebound release of FSH after treatment with oFF.

Anestrus↗

PubMed1995

Recombinant FSH (Org32489) induces follicle growth and ovulation in the adult cyclic rat.

The effects of a single injection of recombinant human FSH (rhFSH; Org32489) on ovulation rate and timing and on antral follicle growth were studied in adult 5-day cyclic rats. Rats injected at 1700 h on dioestrus-2 with a dose of 10 IU rhFSH showed, on average, no increase in ovulation rate on the day of expected oestrus. However, an additional, precocious ovulation resulting in a normal number of corpora lutea (13.3 +/- 0.4, n = 6) was found to take place on the night after injection, i.e. dioestrus-3. No mating behaviour, as shown by the absence of vaginal plugs the next morning, was observed at this ovulation. Follicle counts showed a loss of large antral follicles due to ovulation and increased numbers of healthy small antral follicles at 17 and 41 h after injection, indicating a decrease of atresia of growing follicles as well as additional recruitment of new antral follicles. The endogenous serum FSH concentration on the subsequent day of oestrus (65 h after the rhFSH injection) as well as recruitment of small antral follicles were lower in the rhFSH-treated rats than in saline-treated controls. The ovulation at oestrus, 48 h after the precocious, rhFSH-induced ovulation showed large differences in the number of oocytes between the rats in one treatment group. Similar results in terms of immediate ovulation induction were obtained by using a highly purified human urinary FSH preparation (i.e. metrodin). Furthermore, the direct induction of ovulation by rhFSH or metrodin could not be prevented by the injection of an LHRH antagonist.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗

PubMed1988

A review of the animal pharmacology of roxatidine acetate.

Roxatidine acetate (TZU 0460/HOE 760) [N-(3-[3-(1-piperidinylmethyl)-phenoxy]-propyl)acetoxyacetamide hydrochloride] is a specific and competitive H2-receptor antagonist with a chemical structure different from those of cimetidine, ranitidine and famotidine. Roxatidine acetate and its main metabolite roxatidine inhibit histamine-induced gastric acid secretion in vitro with a potency greater than that of cimetidine, and in the range of that produced by ranitidine. Gastric acid secretion following stimulation with dibutyryl cyclic adenosine monophosphate remains unaffected by roxatidine acetate. In vivo experiments in rats and dogs confirm these in vitro findings. Thus, in rats roxatidine acetate inhibits gastric acid secretion with similar values following intraduodenal or intraperitoneal injection, indicating excellent absorption of the drug from the gastrointestinal tract. In all studies it was shown that roxatidine acetate was more potent than cimetidine. In rats single or repeated dosing with roxatidine acetate did not influence drug metabolising enzymes in the liver nor did the drug show antiandrogenic activity in long term animal studies. Extensive general pharmacological studies with roxatidine acetate demonstrate the lack of effects on the central nervous system, on gastrointestinal motility, the autonomic nervous system and the cardiovascular and urogenital systems. Studies on the pharmacokinetics and metabolism of roxatidine acetate demonstrate that there is a presystemic deacetylation producing the main metabolite roxatidine, which is responsible for the in vivo effects of the drug.

Animals↗

PubMed1996

Effects of B vitamin injection on bovine herpesvirus-1 infection and immunity in feed-restricted beef calves.

Because feed and water deprivation during marketing and transport of feedlot calves may reduce ruminal B vitamin synthesis at a time when calves are most susceptible to infectious agents, we studied the effect of B vitamin injections on infection and immunity in 12 6-mo-old beef steer calves (153 +/- 8 kg) that were weaned, limit-fed, and deprived of feed. Six calves were injected with B vitamins and ascorbic acid every 48 h for 28 d starting 2 wk before virus inoculation. All calves were infected with an attenuated strain of bovine herpesvirus type 1 (BHV-1) on d 0. From time of arrival (d -20) until the end of a 3-d period without food (d -6), calves lost 13.1% of their initial weight. However, they regained weight after re-feeding so that net weight loss was 7.7% for the 20-d period prior to infection. The stress/BHV-1 model resulted in a mild respiratory infection in all calves with no difference observed between treatment groups. Vitamin injections did not significantly affect virus and interferon titers in nasal secretions, or lymphocyte blastogenesis. However, the B vitamin treatment tended to increase serum IgG titers to BHV-1 on both d 14 (1,120 vs 550, P = .115) and d 28 (2,400 vs 1,830, P = .37) after infection. Averaged across d 14 and d 28, IgG titers tended to be higher (P < .09) for the calves receiving B vitamin injections, indicating that the humoral immune response was enhanced by B vitamin treatment. B vitamin status in stressed calves at the time of vaccination or disease challenge may affect the success of the immune response.

Animals↗

PubMedDate not supplied

Water soluble marihuana-derived material: pharmacological actions in rabbit and primate.

Further studies have been made with water soluble marihuana-derived material (MDM). Neither adrenergic, cholinergic, aldosterone, dopamine or serotonin antagonism affected the fall in intraocular pressure induced by MDM. Partial blockade was obtained with galactose, glucose, or mannose, but not arabinose, when the latter were given at intravenous concentrations of 1 gm/animal and MDM was given at 25 micrograms animal, suggesting that these sugars may be involved at the active site of the MDM glycoproteins. Dexamethasone was without effect on either intravenous or intravitreal MDM indicating that the MDM effect is not a non-specific response to a protein. A similar plant glycoprotein, larch arabinogalactan, at 200 micrograms/animal was without effect on intraocular pressure. Aqueous humor flow rate was increased 3 hours after MDM administration, a period corresponding to the intraocular pressure increase caused by MDM, and fell to 20% of control values when the fall in intraocular pressure occurred. Blood flow through the iris was increased at both one and six hours after intravenous MDM injection indicating a vasodilation which could contribute to the initial increase in intraocular pressure. Intravitreal injection of MDM in rabbit and rhesus monkey caused a fall in intraocular pressure only after a 24 hour delay: the unilateral response indicated that systemic metabolism was not required for activity and the delay was likely caused by the diffusion time to the ciliary processes from the mid-vitreal injection site. The changes in beta-receptors, adenylate cyclase and carbonic anhydrase in the ciliary processes are minimal indicating a possible vascular mechanism of action of MDM.

Animals↗

PubMed1979

The efficacy of intra-articularly administered MYC 2095, triamcinolone hexacetonide and placebo in gonarthritis. A combined double-blind clinical trial.

We report the results of a double-blind three-centre study, employing a cross-over design, set up to compare the efficacy of intra-articular injections of Myc 2095 (20 mg), triamcinolone hexacetonide (Lederspan) (20 mg) and placebo in 40 patients with synovitis of the knee joint. Each patient included in the study contributed data on 2 of the 3 treatment variables being compared. Seven clinical parameters were assessed every 6 weeks, while the doctor's and the patient's assessments were scored. Intra articular treatment both with Myc 2095 and triamcinolone hexacetonide proved to be effective. Placebo response was also very high. After the first Myc 2095 injection, improvement in "tenderness", "pain under load" and "swelling and hydrops" was significantly superior to that following placebo treatment. The evaluation of the second injections indicated a marked carry-over effect from the first course. This was also evident from the doctor's and patient's assessments. The importance of including a placebo in the evaluation of anti-phlogistic drugs in clinical trials, emerged from this study.

Adult↗

PubMed1988

Chemonucleolysis for sciatica. A critical review.

Intradiscal injection of chymopapain for the treatment of sciatica due to disc herniation has been used for more than 25 years, but is still under debate. We review the indications, complications, and clinical results, and discuss the tissue effects of chymopapain. The results following surgical disc removal versus chymopapain injection indicate that surgery with removal of the disc hernia through a small laminotomy remains the documented treatment of choice for patients with proven disc herniation and sciatica in whom conservative treatment has failed.

Chymopapain↗

PubMed1985

Failure of injection of rat placental lactogen to inhibit prolactin in vivo.

In an attempt to demonstrate a negative feedback of rat placental lactogen (rPL) on prolactin secretion, pregnant rats were hysterectomized and injected intraperitoneally with placental extracts. Hysterectomy alone prolonged the incidence of nocturnal prolactin surges and injection of placental extracts did not alter this response. However, the absence of rPL in the serum following the injections indicated a primary reason why no inhibition was seen. Only when rPL was given intravenously was there detectable amounts found in the blood. The slow disappearance of rPL from the circulation following hysterectomy in Day 11 pregnant rats suggests that the lack of rPL in the blood following ip injection of placental extracts is not due to rapid clearance of rPL from blood. The failure to show a negative feedback of rPL on prolactin in vivo may be due primarily to the lack of appearance of rPL in the circulation following an ip injection of placental extracts.

Animals↗

PubMed1975

Thyroid metabolism in the recessive sex-linked dwarf female chicken. 3. The influence of exogenous thyroid hormones in glycogen metabolism.

The influence of exogenous thyroid hormones on glycogen-body and liver glycogen was studied in fasted and full-fed 3 wk. old dwarf and non-dwarf White Leghorn chickens. The results indicated that in contrast to normals, the glycogen-body of the dwarf was still physiologically active at age 3 wks. and they also exhibited a relatively higher liver glycogen concentration. The liver glycogen concentration was significantly higher in T3-treated, full-fed dwarf chickens when compared with other groups. The data were interpreted to suggest that the differential response observed in both dwarf and non-dwarf chickens of increasing liver glycogen levels with T3 and T4 injections indicated that the proper ratios of serum T3:T4 were probably more vital to the normal metabolic functions than changes in the individual concentrations of either T3 or T4.

Animals↗

PubMed1981

Role of the dopaminergic system in luteinizing hormone release and ovulation in the hen.

Two experiments were conducted to examine further the role of the dopaminergic system in the ovulatory cycle of the hen. In experiment 1, dopamine (DA; 8 microgram) was injected intraventricularly 14 hr prior to the C1 ovulation (to determine the efficacy of DA in causing premature ovulation) and the DA-receptor blocker, pimozide, implanted intraventricularly for the previous 24 hr was used to assess the specificity of the response. The luteinizing hormone (LH) radioimmunoassays from serial blood samples subsequent to the injection, indicated no effect of the DA treatment on either the time or the magnitude of the preovulatory LH surge. In Experiment 2, an intraventricular injection of DA (10 microgram) was made 8 hr prior to the C1 ovulation (to examine the effect of DA on the normal preovulatory LH surgery) and assay results from blood samples at short intervals immediately after the injection showed no effect of the treatment on plasma LH levels. These results, in addition to the finding that the pimozide implant caused no disruption of the ovulatory cycle, suggest that the dopaminergic system is not essential to the ovulatory process in the hen.

Animals↗

PubMed1993

[Crossed inhibition of lateral pterygoid motoneurons in guinea pig].

The effects of stimulation of the lateral pterygoid (LP) nerve on the contralateral LP motoneurons (Mns) were investigated in the decerebrate guinea pig. 1. Stimulation of the LP nerve induced a hyperpolarizing potential (HP) in the contralateral LP Mn. The onset and peak latency of this HP were 2.14 ms and 4.10 ms in 11 LP Mns on the average, respectively. The HP was reversed to a depolarizing potential after intracellular Cl- injection, indicating that it mainly consisted of IPSPs. 2. The antidromically evoked field potential (AFP) in the LP Mn pool was depressed by the stimulation of the contralateral LP nerve. The threshold intensity was about 1.2 times the LP nerve threshold. 3. The crossed depression of AFP was significantly diminished after the destruction of the caudal part of the contralateral trigeminal mesencephalic nucleus, but not by the lesion of the trigeminal spinal tract. 4. The most rostral level in the trigeminal spinal tract nucleus, where the HRP-labelled axon terminals were found after its injection into the LP muscle, was located caudally to the lesion of the spinal tract. It is concluded that the muscle spindle afferents from the LP muscle are involved in the crossed inhibition of the LP Mns evoked by the stimulation of the LP nerve.

Animals↗