Yohimbine as an Autonomic Test Drug

Nature ◽  
1962 ◽  
Vol 193 (4822) ◽  
pp. 1313-1314 ◽  
Author(s):  
GUNNAR HOLMBERG ◽  
SAMUEL GERSHON ◽  
LLOYD H. BECK
Keyword(s):  
Test Drug ◽  
Autonomic Test

General practitioners and clinical pharmacology

1989 ◽  
Vol 4 (4) ◽  
pp. 241-244
Author(s):  
P. Lemoine
Keyword(s):  
Clinical Pharmacology ◽  
General Practitioners ◽  
Field Studies ◽  
Discussion Group ◽  
Group Method ◽  
Study Group ◽  
Test Drug ◽  
Monthly Basis ◽  
One Year ◽  
The One

SummaryIt is difficult to undertake field studies with non marketed psychotropic drugs because of two apparently contradictory conditions : on the one hand, the methodology has to be rigorously controlled, and on the other hand, such studies have to be carried out in their future environment by general practitioners (GPs). Bearing in mind the lack of training and experience regarding this kind of approach, the author adopted a discussion group method according to the techniques developed by M. Balint. The study group comprised five GPs, a clinical pharmacology expert and a doctor from the pharmaceutical laboratory which had developed the test drug. These persons met on a monthly basis over a one year period. In the present paper, the author indicates the benefits of such a methodology, based on six years’ experience and several trials, with special emphasis placed on the pedagogical aspects.

Pharmacological properties of YM-254890, a specific Gαq/11 inhibitor, on thrombosis and neointima formation in mice

2005 ◽  
Vol 94 (07) ◽  
pp. 184-192 ◽  
Author(s):  
Masatoshi Taniguchi ◽  
Yumiko Moritani ◽  
Toshio Uemura ◽  
Takeshi Shigenaga ◽  
Hajime Takamatsu ◽  
...  
Keyword(s):  
Oral Administration ◽  
Vascular Injury ◽  
Bolus Injection ◽  
Thrombus Formation ◽  
Therapeutic Window ◽  
Pharmacological Properties ◽  
Neointima Formation ◽  
Intravenous Bolus ◽  
Test Drug ◽  
Intravenous Bolus Injection

SummaryThe pharmacological properties of YM-254890,a specific Gαq/11 inhibitor, on acute thrombosis and chronic neointima formation after vascular injury have been investigated. FeCl3 was used to induce vascular injury in the carotid artery of mice. For the thrombosis studies, the test drug was either intravenously or orally administered before vascular injury. For the neointima studies, the test drug was orally administered 1 h before and twice daily for 1 week after vascular injury. Histological analysis was then performed 3 weeks later. YM-254890 significantly inhibited ex vivo platelet aggregation 5 min after intravenous bolus injection at 0.03 mg/kg or more, and 1 h after oral administration at 1 mg/kg. YM-254890 significantly inhibited thrombus formation after intravenous bolus injection at 0.03 mg/kg as well as after oral administration at 1 mg/kg, but tail transection bleeding time was significantly prolonged at 0.1 mg/kg for intravenous injection and 3 mg/kg for oral administration. Furthermore, oral administration of YM-254890 dose-dependently inhibited neointima formation 3 weeks after vascular injury with significant effects at 1 mg/kg twice daily for 1 week. Clopidogrel also significantly inhibited neointima formation at its antithrombotic dose, but its inhibitory potency was less than that of YM-254890. However, YM-254890 significantly reduced systemic blood pressure at doses 3 times higher than those that produced significant inhibitory effects on thrombosis and neointima formation. Though the systemic use of YM-254890 may be limited, owing to its narrow therapeutic window, this unique compound is a useful research tool for investigating the physiological roles of Gαq/11.

Comparative Studies of an Orally-active Factor Xa Inhibitor, YM-60828, with other Antithrombotic Agents in a Rat Model of Arterial Thrombosis

1998 ◽  
Vol 79 (02) ◽  
pp. 410-416 ◽  
Author(s):  
Kazuo Sato ◽  
Yumiko Sakai ◽  
Fukushi Hirayama ◽  
Hiroyuki Koshio ◽  
Yuta Taniuchi ◽  
...  
Keyword(s):  
Electrical Stimulation ◽  
Arterial Thrombosis ◽  
Thrombus Formation ◽  
Factor Xa ◽  
Test Drug ◽  
Antithrombotic Agent ◽  
Antithrombotic Activity ◽  
Thrombosis Model ◽  
Treatment And Prevention ◽  
Orally Active

SummaryWe examined the antithrombotic activity of a novel synthetic inhibitor of factor Xa, YM-60828, in an electrically-induced carotid artery thrombosis model in rats. In the first experiment, the antithrombotic activity of YM-60828 after i.v. infusion was compared with those of heparin, darteparin and argatroban. Test drug was administered by i.v. infusion from 30 min before electrical stimulation to the end of the experiment. YM-60828 at 1 mg/kg/h significantly improved patency status, prolonged the time to occlusive thrombus formation and duration of patency. Heparin at 300 U/kg/h also improved these parameters, but were accompanied by a marked increase in systemic coagulation time. In the second experiment, the antithrombotic activity of YM-60828 after oral administration was compared with those of ticlopidine, cilostazol, aspirin, beraprost, ethyl icosapentate and warfarin. Test drug was orally administered to fasted rats 60 min before electrical stimulation. YM-60828 at 30 mg/kg p.o., but not ticlopidine, cilostazol, aspirin, beraprost, ethyl icosapentate or warfarin, significantly reduced the incidence of occlusion and improved carotid arterial patency. These results suggest that YM-60828 may be a promising antithrombotic agent for the treatment and prevention of arterial thrombosis which can be given by oral as well as intravenous administration.

Dissociation of Appetitive Overexpectation and Extinction in the Infralimbic Cortex

2018 ◽  
Vol 29 (9) ◽  
pp. 3687-3701 ◽  
Author(s):  
Belinda P P Lay ◽  
Melissa Nicolosi ◽  
Alexandra A Usypchuk ◽  
Guillem R Esber ◽  
Mihaela D Iordanova
Keyword(s):  
Behavioral Change ◽  
Reward Learning ◽  
Behavioral Modification ◽  
Test Drug ◽  
Infralimbic Cortex ◽  
Stimulus Response ◽  
Conditioned Responses ◽  
Conditioned Responding ◽  
Drug Free

Abstract Behavioral change is paramount to adaptive behavior. Two ways to achieve alterations in previously established behavior are extinction and overexpectation. The infralimbic (IL) portion of the medial prefrontal cortex controls the inhibition of previously established aversive behavioral responses in extinction. The role of the IL cortex in behavioral modification in appetitive Pavlovian associations remains poorly understood. Here, we seek to determine if the IL cortex modulates overexpectation and extinction of reward learning. Using overexpectation or extinction to achieve a reduction in behavior, the present findings uncover a dissociable role for the IL cortex in these paradigms. Pharmacologically inactivating the IL cortex left overexpectation intact. In contrast, pre-training manipulations in the IL cortex prior to extinction facilitated the reduction in conditioned responding but led to a disrupted extinction retrieval on test drug-free. Additional studies confirmed that this effect is restricted to the IL and not dependent on the dorsally-located prelimbic cortex. Together, these results show that the IL cortex underlies extinction but not overexpectation-driven reduction in behavior, which may be due to regulating the expression of conditioned responses influenced by stimulus–response associations rather than stimulus–stimulus associations.

scholarly journals Antipyretic, Analgesic and Anti-inflammatory Activity of Qurs Afsanteen Saghir (A Polyherbal Unani Tablet) in Experimental Animals

2022 ◽  
Author(s):  
MD Maseehullah ◽  
Gulam Mohammed Husain ◽  
Mohammed Zakir ◽  
Mohd Kashif Husain ◽  
Ghazala Javed ◽  
...  
Keyword(s):  
Diclofenac Sodium ◽  
Study Drug ◽  
Prunus Dulcis ◽  
Inflammatory Activity ◽  
Apium Graveolens ◽  
Dependent Manner ◽  
Test Drug ◽  
Artemisia Absinthium ◽  
Hot Plate Test ◽  
Anti Inflammatory

Qurs Afsanteen Saghir is a polyherbal Unani formulation in the form of tablet. This formulation consists of multiple medicinal plants like Afsanteen (Artemisia absinthium L.), Badam Talkh (Prunus dulcis (Mill.) D.A.Webb), Asaroon (Asarum europaeum L.), Anisoon (Pimpinella anisum L.) and Tukhm-e-Karafs (Apium graveolens L.). The clinical adult dose of study drug is 3.5 –7 g per day as mentioned in Unani literature. The present study evaluated the antipyretic, analgesic and anti-inflammatory potential of Qurs Afsanteen Saghir using different animal models. Antipyretic activity was measured using yeast-induced pyrexia model in rats at 360 and 720 mg/kg bw dose of test drug and paracetamol (70 mg/kg bw p.o.) as standard control. Analgesic effect was evaluated using acetic acid-induced writhing test in mice using test drug at dose 720 and 1440 mg/kg bw and diclofenac sodium (15 mg/kg bw p.o.) as standard control. Eddy’s hot plate test was conducted in rats using test drug at the dose of 360 and 720 mg/kg bw and buprenorphine (0.10 mg/kg s.q.) as standard control. Anti-inflammatory activity was assessed by carrageenan-induced paw edema model in rats with the dose of 360 and 720 mg/kg of test drug and Indomethacin (10 mg/kg p.o.) as standard control. The study drug significantly reduced the temperature and pain at both dose levels in a time-dependent manner as compared to normal control. However, the reduction of inflammation was observed at low dose (360 mg/kg bw) only after 3 hours of carrageenan administration. These findings indicated that tested drug showed potential activity as antipyretic and analgesic; whereas the drug may not be considered quite effective as an anti-inflammatory agents.

scholarly journals Quality evaluation of minoxidil topical solutions obtained from magistral pharmacies

2019 ◽  
Vol 3 (2) ◽  
pp. 30-35
Author(s):  
Karen N. Dartora ◽  
Paula C. Bona ◽  
Francielli L. Dos Santos ◽  
Paula Bianchetti ◽  
Renata Vidor Contri
Keyword(s):  
Statistical Difference ◽  
Quality Evaluation ◽  
Quality Parameters ◽  
Centrifuge Test ◽  
Test Drug ◽  
Organoleptic Properties ◽  
Industrial Sample ◽  
Drug Content ◽  
Ph Values

The objective of this study was to evaluate quality parameters of magistral topical solutions containing minoxidil (A, B and C), comparing the results with the ones obtained for the industrial formulation. Organoleptic tests, evaluation of the pH and density, centrifuge test, drug content determination, comparison of indicated dosages and in vitro follicular penetration of minoxidil were performed. Regarding the organoleptic properties, differences in color and viscosity were observed between the magistral (composed of minoxidil sulfate) and the industrial formulations (composed of minoxidil base). For pH values, the magistral solutions presented considerably more acidic pH, compared to the industrial sample. For the density test, the samples with the highest ethanol percentages (B and C) presented lower density. In the centrifuge test, none of the samples showed changes. Considering the drug content test, only the industrial sample and the magistral sample C showed drug percentage within the expected (90-110%), indicating lack of correction factor determination by the magistral pharmacies. Furthermore, it was observed that the dosage indicated by the magistral pharmacies do not correspond to the dose indicated by the industry, being significantly lower. All topical solutions tested presented hair follicle penetration of minoxildil, without statistical difference. The results indicate that there is a failure in the magistral pharmacies regarding the production and the indication of dosage of minoxidil topical solutions.

scholarly journals DETERMINATION OF RASA PANCHAKA (5 AYURVEDIC PRINCIPLES OF DRUG ACTION) OF A FOLK DRUG - Alstonia venenata R. Br.

2020 ◽  
Vol 8 (8) ◽  
pp. 4125-4132
Author(s):  
Anusha P R ◽  
Chandrakanth Bhat ◽  
Hariprasad Shetty ◽  
Sudhakar Bhat
Keyword(s):  
Stem Bark ◽  
Drug Action ◽  
Albino Rats ◽  
Test Drug ◽  
Herbal Drug ◽  
Small Tree ◽  
Detailed Review ◽  
Snake Bites ◽  
Trial Drug

Background and Objective: Systematic study of the folklore knowledge on herbal drug contributes to its conservation and preservation. Documentation of drugs in Ayurveda is based on the five principles called Rasa Panchaka (5 Ayurvedic principles of drug action). Alstonia venenata R. Br is a small tree belonging to Apocynaceae family. Its stem bark is used by tribes in fever, epilepsy and as anti-venom in snake bites. The aim of this study is to determine the Rasa Panchaka (5 Ayurvedic principles of drug action) of Al-stonia venenata R. Br. Methods: Detailed review of the trial drug was carried out. Rasa (taste) was determined by using direct per-ception method on 30 healthy volunteers. Veerya (potency) was determined by assessing the exothermic and endothermic reaction of the drug in water. Vipaka (taste after digestion), Guna (properties) and Prab-hava (specific action) were assessed by experimental study of the drug on 12 Wister Albino rats. Result and Conclusion: After the study Rasa panchaka (5 Ayurvedic principles of drug action) of the test drug was accessed as Tikta (bitter) Rasa (taste), Laghu (light) Rooksha (dry) Guna (property), Sheetha (cold) Veerya (potency)and Katu (pungent) Vipaka (taste after digestion).

scholarly journals The Effect of Glycopyrrolate on Induction Dose of Propofol during General Anesthesia

2015 ◽  
Vol 49 (2) ◽  
pp. 62-65
Author(s):  
Suman Arora ◽  
Harihar Vishwanath Hegde ◽  
Jyotsna Wig
Keyword(s):  
Heart Rate ◽  
Cardiac Output ◽  
General Anesthesia ◽  
Significant Positive Correlation ◽  
Saline Group ◽  
Small Extent ◽  
Loss Of Consciousness ◽  
Test Drug ◽  
Normal Saline Group ◽  
Induction Dose

ABSTRACT Background Preinduction cardiac output (CO) is a small but significant predictor of induction dose of propofol. We hypothesized that glycopyrrolate, by inducing tachycardia (although to a small extent) would increase CO, and hence the induction dose of propofol. Aim of the study was to find out the dose of propofol required to induce anesthesia in patients receiving glycopyrrolate as compared to those not receiving it. Meterials and methods Eighty female patients (25-60 years, ASA-1, 2) undergoing elective procedures under general anesthesia were randomized into group G (glycopyrrolate) and group C (control). Patients received 1 ml (0.2 mg) glycopyrrolate (group G) or 1 ml normal saline (group C) intravenously 5 minutes before induction. Anesthesia was induced with propofol at a rate of 0.8 mg/kg/min titrated to achieve a target BIS = 40. Dose of propofol required for induction of anesthesia (loss of consciousness) and to reach the target BIS, heart rate (HR) and mean arterial pressure (MAP) at various intervals were compared. Correlation between the dose of propofol required to reach target BIS = 40 and heart rate after giving the test drug was performed by regression analysis. Results The dose of propofol required for achieving target BIS was significantly higher (p < 0.001) in group G (2.08 ± 0.42 mg/kg) (mean ± SD) as compared to group C (1.66 ± 0.23 mg/ kg). There was a significant positive correlation between the preinduction HR (3 minutes after giving the test drug) and the propofol dose required to reach target BIS = 40 (r = 0.356, p < 0.01). Conclusion Administration of 0.2 mg of glycopyrrolate intravenously before induction of general anesthesia significantly increased the dose of propofol required for induction of anesthesia. How to cite this article Arora S, Hegde HV, wig J, Puri GD. The Effect of Glycopyrrolate on Induction Dose of Propofol during General Anesthesia. J Postgrad Med Edu Res 2015;49(2): 62-65.

Combined effects of a factor Xa inhibitor YM466 and a GPIIb/IIIa antagonist YM128 on thrombosis and neointima formation in mice

2004 ◽  
Vol 92 (12) ◽  
pp. 1221-1228 ◽  
Author(s):  
Yoshiyuki Iwatsuki ◽  
Kazumi Hayashi ◽  
Yumiko Moritani ◽  
Tomoko Nii ◽  
Keiji Miyata ◽  
...  
Keyword(s):  
Platelet Aggregation ◽  
Vascular Injury ◽  
Coronary Angioplasty ◽  
Bleeding Time ◽  
Factor Xa ◽  
Neointima Formation ◽  
Combined Effects ◽  
Test Drug ◽  
Thrombotic Occlusion ◽  
Acute Thrombosis

SummaryThrombosis and neointima formation limit the efficacy of coronary angioplasty. Factor Xa inhibitors and GPIIb/IIIa antagonists have shown to be effective on acute thrombosis and late neointima formation, however, their combined effects remain to be elucidated. Vascular injury was induced by FeCl3 in the carotid artery in mice. For thrombosis studies, the test drug was orally administered 1 hour before vascular injury. For neointima studies, the test drug was orally administered 1 hour before and twice daily for 1 week after vascular injury, and then histological analysis was performed 3 weeks after vascular injury. YM466 inhibited thrombotic occlusion at 30 mg/kg with prolongation of prothrombin time (PT), and tail transection bleeding time (BT) was affected at 100 mg/kg. YM466 also inhibited neointima formation at 10 mg/kg. YM128 inhibited thrombotic occlusion and neointima formation at 10 and 30 mg/kg, respectively, with inhibition of platelet aggregation and prolongation of BT. In contrast, the combination of 10 mg/kg YM466 and 3 mg/kg YM128 inhibited thrombotic occlusion and neointima formation without affecting PT, platelet aggregation and BT. Concomitant inhibition of factor Xa and GPIIb/IIIa may provide a safer and more effective therapeutic regimen for treatment of coronary angioplasty.

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