Bencyclane: A vasodilator agent found to be effective in a variety of peripheral circulation disorders. It has various other potentially useful pharmacological effects. Its mechanism may involve block of calcium channels.Domperidone: A specific blocker of dopamine receptors. It speeds gastrointestinal peristalsis, causes prolactin release, and is used as antiemetic and tool in the study of dopaminergic mechanisms.Galactogogues: Substances that induce LACTATION.Gastrointestinal Motility: The motor activity of the GASTROINTESTINAL TRACT.Encyclopedias as Topic: Works containing information articles on subjects in every field of knowledge, usually arranged in alphabetical order, or a similar work limited to a special field or subject. (From The ALA Glossary of Library and Information Science, 1983)Gastroesophageal Reflux: Retrograde flow of gastric juice (GASTRIC ACID) and/or duodenal contents (BILE ACIDS; PANCREATIC JUICE) into the distal ESOPHAGUS, commonly due to incompetence of the LOWER ESOPHAGEAL SPHINCTER.Suppositories: Medicated dosage forms that are designed to be inserted into the rectal, vaginal, or urethral orifice of the body for absorption. Generally, the active ingredients are packaged in dosage forms containing fatty bases such as cocoa butter, hydrogenated oil, or glycerogelatin that are solid at room temperature but melt or dissolve at body temperature.Gastrointestinal Diseases: Diseases in any segment of the GASTROINTESTINAL TRACT from ESOPHAGUS to RECTUM.Nitroprusside: A powerful vasodilator used in emergencies to lower blood pressure or to improve cardiac function. It is also an indicator for free sulfhydryl groups in proteins.HistoryHypertension, Malignant: A condition of markedly elevated BLOOD PRESSURE with DIASTOLIC PRESSURE usually greater than 120 mm Hg. Malignant hypertension is characterized by widespread vascular damage, PAPILLEDEMA, retinopathy, HYPERTENSIVE ENCEPHALOPATHY, and renal dysfunction.Arterioles: The smallest divisions of the arteries located between the muscular arteries and the capillaries.Venules: The minute vessels that collect blood from the capillary plexuses and join together to form veins.Emergencies: Situations or conditions requiring immediate intervention to avoid serious adverse results.Biotransformation: The chemical alteration of an exogenous substance by or in a biological system. The alteration may inactivate the compound or it may result in the production of an active metabolite of an inactive parent compound. The alterations may be divided into METABOLIC DETOXICATION, PHASE I and METABOLIC DETOXICATION, PHASE II.Dental Prosthesis: An artificial replacement for one or more natural teeth or part of a tooth, or associated structures, ranging from a portion of a tooth to a complete denture. The dental prosthesis is used for cosmetic or functional reasons, or both. DENTURES and specific types of dentures are also available. (From Boucher's Clinical Dental Terminology, 4th ed, p244 & Jablonski, Dictionary of Dentistry, 1992, p643)IndiaEducation, Pharmacy: Formal instruction, learning, or training in the preparation, dispensing, and proper utilization of drugs in the field of medicine.Biological Science Disciplines: All of the divisions of the natural sciences dealing with the various aspects of the phenomena of life and vital processes. The concept includes anatomy and physiology, biochemistry and biophysics, and the biology of animals, plants, and microorganisms. It should be differentiated from BIOLOGY, one of its subdivisions, concerned specifically with the origin and life processes of living organisms.Audiovisual Aids: Auditory and visual instructional materials.Students, Pharmacy: Individuals enrolled in a school of pharmacy or a formal educational program leading to a degree in pharmacy.Prodrugs: A compound that, on administration, must undergo chemical conversion by metabolic processes before becoming the pharmacologically active drug for which it is a prodrug.Patents as Topic: Exclusive legal rights or privileges applied to inventions, plants, etc.Drug Discovery: The process of finding chemicals for potential therapeutic use.Biota: The spectrum of different living organisms inhabiting a particular region, habitat, or biotope.Drug Evaluation, Preclinical: Preclinical testing of drugs in experimental animals or in vitro for their biological and toxic effects and potential clinical applications.Molecular Structure: The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds.Chemistry, Pharmaceutical: Chemistry dealing with the composition and preparation of agents having PHARMACOLOGIC ACTIONS or diagnostic use.Creativity: The ability to generate new ideas or images.Nootropic Agents: Drugs used to specifically facilitate learning or memory, particularly to prevent the cognitive deficits associated with dementias. These drugs act by a variety of mechanisms. While no potent nootropic drugs have yet been accepted for general use, several are being actively investigated.Histamine H3 Antagonists: Drugs that selectively bind to but do not activate HISTAMINE H3 RECEPTORS. They have been used to correct SLEEP WAKE DISORDERS and MEMORY DISORDERS.Neurosciences: The scientific disciplines concerned with the embryology, anatomy, physiology, biochemistry, pharmacology, etc., of the nervous system.Cognition: Intellectual or mental process whereby an organism obtains knowledge.Phimosis: A condition in which the FORESKIN cannot be retracted to reveal the GLANS PENIS. It is due to tightness or narrowing of the foreskin opening.Executive Function: A set of cognitive functions that controls complex, goal-directed thought and behavior. Executive function involves multiple domains, such as CONCEPT FORMATION, goal management, cognitive flexibility, INHIBITION control, and WORKING MEMORY. Impaired executive function is seen in a range of disorders, e.g., SCHIZOPHRENIA; and ADHD.Carbonic Anhydrases: A family of zinc-containing enzymes that catalyze the reversible hydration of carbon dioxide. They play an important role in the transport of CARBON DIOXIDE from the tissues to the LUNG. EC 4.2.1.1.Fructose: A monosaccharide in sweet fruits and honey that is soluble in water, alcohol, or ether. It is used as a preservative and an intravenous infusion in parenteral feeding.Anticonvulsants: Drugs used to prevent SEIZURES or reduce their severity.Calcium Channels: Voltage-dependent cell membrane glycoproteins selectively permeable to calcium ions. They are categorized as L-, T-, N-, P-, Q-, and R-types based on the activation and inactivation kinetics, ion specificity, and sensitivity to drugs and toxins. The L- and T-types are present throughout the cardiovascular and central nervous systems and the N-, P-, Q-, & R-types are located in neuronal tissue.Sodium Channels: Ion channels that specifically allow the passage of SODIUM ions. A variety of specific sodium channel subtypes are involved in serving specialized functions such as neuronal signaling, CARDIAC MUSCLE contraction, and KIDNEY function.Receptors, Kainic Acid: A class of ionotropic glutamate receptors characterized by their affinity for KAINIC ACID.Isoenzymes: Structurally related forms of an enzyme. Each isoenzyme has the same mechanism and classification, but differs in its chemical, physical, or immunological characteristics.Anthramycin: A broad-spectrum spectrum antineoplastic antibiotic isolated from Streptomyces refuineus var. thermotolerans. It has low toxicity, some activity against Trichomonas and Endamoeba, and inhibits RNA and DNA synthesis. It binds irreversibly to DNA.Altretamine: A hexamethyl-2,4,6-triamine derivative of 1,3,5-triazine.Aclarubicin: An anthracycline produced by Streptomyces galilaeus. It has potent antineoplastic activity.Dosage Forms: Completed forms of the pharmaceutical preparation in which prescribed doses of medication are included. They are designed to resist action by gastric fluids, prevent vomiting and nausea, reduce or alleviate the undesirable taste and smells associated with oral administration, achieve a high concentration of drug at target site, or produce a delayed or long-acting drug effect.Methyltestosterone: A synthetic hormone used for androgen replacement therapy and as an hormonal antineoplastic agent (ANTINEOPLASTIC AGENTS, HORMONAL).Inventions: A novel composition, device, or process, independently conceived de novo or derived from a pre-existing model.Alphaprodine: An opioid analgesic chemically related to and with an action resembling that of MEPERIDINE, but more rapid in onset and of shorter duration. It has been used in obstetrics, as pre-operative medication, for minor surgical procedures, and for dental procedures. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1067)Dextropropoxyphene: A narcotic analgesic structurally related to METHADONE. Only the dextro-isomer has an analgesic effect; the levo-isomer appears to exert an antitussive effect.Bromazepam: One of the BENZODIAZEPINES that is used in the treatment of ANXIETY DISORDERS.Clorazepate Dipotassium: A water-soluble benzodiazepine derivative effective in the treatment of anxiety. It has also muscle relaxant and anticonvulsant actions.Barbital: A long-acting barbiturate that depresses most metabolic processes at high doses. It is used as a hypnotic and sedative and may induce dependence. Barbital is also used in veterinary practice for central nervous system depression.Dextromoramide: An opioid analgesic structurally related to METHADONE and used in the treatment of severe pain. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1070)

Slow channel inhibitor effects on brain function: tolerance to severe hypoxia in the rat. (1/2)

1. The protective effects of ten slow channel inhibitor drugs against severe progressive hypoxia were investigated in rats breathing spontaneously during light anaesthesia. Respiration, heart rate, electrocorticogram (ECoG) and/or electroencephalogram (EEG) were recorded. 2. Tolerance times were monitored from hypoxia onset until cessation of respiration, ECoG, EEG synchronization, and 'background-EEG'. Drugs were administered i.v. 5 min before the onset of hypoxia. 3. Verapamil, gallopamil, and nimodipine resulted in a significant increase of tolerance times; fendiline and bepridil showed a small increase (not significant); bencyclan and prenylamine were ineffective; cinnarizine and diltiazem slightly reduced tolerance times as did flunarizine at low doses. 4. At protective doses, verapamil, gallopamil, and nimodipine significantly raised the respiration rate but had little or no cardiac depressor effects. Bencyclan showed ventilatory drive but cardiocirculatory depression. A clear-cut ventilatory drive did not occur with the other ineffective slow channel inhibitors. 5. It is suggested that the protective actions observed were not due to slow channel inhibition per se, nor to spasmolytic potency or increased cerebral blood flow. Ventilatory drive associated with other cardiopulmonary actions which secondarily raise the brain oxygen supply are likely to be responsible for this effect.  (+info)

Comparative studies of cerebral vasodilators on relaxation activities in isolated basilar, mesenteric and pulmonary arteries of rabbits. (2/2)

Effects of cerebral vasodilators such as bencyclane, cinnarizine, and papaverine were comparatively studied using helically cut basilar and superior mesenteric arteries and radial muscle preparations of pulmonary arteries with the sympathetic nerve isolated from rabbits. The order of relaxation activities on high K+-induced contractures was cinnarizine>bencyclane>papaverine in basilar strips and cinnarizine>papaverine>bencyclane in mesenteric strips. Relaxation responses of basilar strips to cinnarizine and bencyclane were faster and more marked than those seen in mesenteric strips. Responses to papaverine were equipotent in both preparations. The action of cinnarizine alone was irreversible. In mesenteric strips, the order of the sensitivity of contractile responses to cumulatively applied biogenic amines was serotonin>noradrenaline>histamine. Cinnarizine produced an antihistaminergic action, while bencyclane produced an antiserotonergic action. In pulmonary arteries, 6 x 10(-6) g/ml papaverine inhibited contractile responses to 2, 5, and 25 Hz nerve stimulation in a frequency-independent manner together with inhibition of responses to noradrenaline. Bencyclane at 6 x 10(-6) and 10(-5) g/ml selectively inhibited in a dose-dependent manner contractile responses only to 25 Hz without inhibition of responses to noradrenaline. These results were discussed in comparison with findings of the cerebral vasodilators obtained using other experimental techniques. Spiral strips of basilar arteries from rabbits in combination with peripheral arteries may be used as a simple quantitative, and reproducible screening method in a preclinical stage for drug evaluation of cerebral vasodilators.  (+info)

Patients with a specific kind of lung cancer may benefit from a Phase III clinical trial offered by the Moores UCSD Cancer Center. The new drug, crizotinib, under development by Pfizer, showed dramatic results in reducing lung cancer tumors in some patients during Phase I and II clinical trials.
In the convergence of information and entertainment there is a conflict between the consumers expectation of fast access to high quality multimedia content through narrow bandwidth channels versus the size of this content. During the retrieval and information presentation of a multimedia application there are two problems that have to be solved: the limited bandwidth during transmission of the retrieved multimedia content and the limited memory for temporary caching. In this paper we propose an approach for latency optimization in information browsing applications. We proposed a method for flattening hierarchically linked documents in a manner convenient for network transport over slow channels to minimize browsing latency. Flattening of the hierarchy involves linearization, compression and bundling of the document nodes. After the transfer, the compressed hierarchy is stored on a local device where it can be partly unbundled to fit the caching limits at the local site while giving the user ...
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An ergot derivative that has been used as a cerebral vasodilator and in peripheral vascular disease. It has been suggested to ameliorate cognitive deficits in cerebrovascular disease.
Face recognition takes place within a distinct heritable module of the brain and includes the ability to distinguish between male and female human faces. To identify gender, this module targets a number of sexually dimorphic features, particularly the hue and luminosity of facial skin. Men look browner and ruddier in hue because melanin and blood are more present in their skins outer tissues. Women have a higher luminous contrast between their facial skin and their lips and eyes. Hue seems to provide a "fast channel" for gender recognition. If the observer is too far away or the lighting too dim, the brain switches to the "slow channel" and targets luminosity. In addition to assisting gender recognition, the skins hue and luminosity may also alter the observers mental state in a number of areas, ranging from sexual attraction to emotional distancing ...
Face recognition takes place within a distinct heritable module of the brain and includes the ability to distinguish between male and female human faces. To identify gender, this module targets a number of sexually dimorphic features, particularly the hue and luminosity of facial skin. Men look browner and ruddier in hue because melanin and blood are more present in their skins outer tissues. Women have a higher luminous contrast between their facial skin and their lips and eyes. Hue seems to provide a "fast channel" for gender recognition. If the observer is too far away or the lighting too dim, the brain switches to the "slow channel" and targets luminosity. In addition to assisting gender recognition, the skins hue and luminosity may also alter the observers mental state in a number of areas, ranging from sexual attraction to emotional distancing ...
We also fished a little upstream from the Bath Tub Pool. This high water level has created all kinds of currents both in the Pool and a little upstream: rapids, deep and small plunge pools, fast and slow channels. Each of them holds fish ...
BioAssay record AID 400370 submitted by ChEMBL: Relaxation activity in guinea pig ileum assessed as relaxation of KCl-induced muscle contractions.
0008]In some existing approaches, the codeword index is fed back in a differential manner. In other words the difference between a current index and a previous index is fed back rather than the codeword index per se. Another problem with common pilot based closed-loop MIMO schemes relates to errors that occur in the transmission of the differential codeword index. Closed-loop MIMO is typically intended for nomadic UEs for whom channel conditions will not change very quickly. For each given currently used pre-coding matrix, a small subset of possible next codewords is defined, for example those that would most likely be selected from the full set due to slow channel variation. This subset of codewords can be determined in several ways, such as spatial correlation and matrix correlation. If an index associated with this subset is fed back rather than an index from the entire set of codewords, fewer bits are needed. However, if a feedback error occurs the transmitter will keep using the wrong ...
ABSTRACT Objective: Efficacy and tolerability of the fixed combination cinnarizine 20mg/dimenhydrinate 40mg was compared to cinnarizine 50mg and dimenhydrinate 100mg in peripheral, central or mixed peripheral/central vertigo. Methods: 189 patients were randomized to receive 1 tablet of medication, 3 times daily, for 4 weeks. Vertigo (mean vertigo score, MVS) and concomitant symptoms, balance (craniocorpography) and […]. ...
Cinnarizine(Antigeron) generic is an antihistamine, prescribed for the control of nausea and vomiting due to motion sickness. It is also used for vertigo and brain disorder. It blocks the histamine action, which reduces allergy symptoms.
The dihydrochloride of this compound (IVp KB-2796) was selected augmentin cpr prospect a candidate for the development of a cerebral vasodilator, M. Cambridge University Press, with intermittent acute relapses, and have the cardinal features of painful proptosis, possible scleritis, optic neuritis or dacryo- adenitis, and occasional bilateral involvement. 5, 2. 11.
Hydrocarbon reservoirs of fluviatile origin are the product of a number of geological processes acting on a variety of scales. Reservoir characterization must be approached holistically in order to understand these processes fully. Tectonic style produces the macro-architectural framework and influences the behaviour of rivers at a mesoarchitectural scale. Tectonics controls the magnitude, position and development of drainage basins and thus, with climate and local geology, controls the flux of sediment fed into any fluviatile system. Migration of normal faulting may lead to the initiation of drainage basins in previously depositional areas, erosion and reworking thus enhancing reservoir quality. Sediment may be introduced as axial or transverse fluxes. Deducing these contributions in ancient basins establishes basin geometry and the basis for reservoir characterization. Individual river channels are highly susceptible to gradient changes caused by tectonic tilting. This causes slow channel belt ...
Mental toughness, relaxation activities, and sleep in sports Study of the relationship between mental toughness, relaxation, and sleep in athletes at different skill levels. Psychologie LAP LAMBERT Academic Publishing (13.10.2011) - ISBN-13: 978-3-8465-2853-2 ...
Cinnarizine is an antihistamine and a calcium channel blocker. Histamines mediate a number of activities such as contraction of smooth muscle of the airways and gastrointestinal tract, vasodilatation, cardiac stimulation, secretion of gastric acid, promotion of interleukin release and chemotaxis of eosinophils and mast cells. Competitive antagonists at histamine H1 receptors may be divided into first (sedating) and second (non-sedating) generation agents. Some, such as Cinnarizine also block muscarinic acetylcholine receptors and are used as anti-emetic agents. Cinnarizine through its calcium channel blocking ability also inhibits stimulation of the vestibular system ...
Cinnarizine is an antihistamine and a calcium channel blocker. Histamines mediate a number of activities such as contraction of smooth muscle of the airways and gastrointestinal tract, vasodilatation, cardiac stimulation, secretion of gastric acid, promotion of interleukin release and chemotaxis of eosinophils and mast cells. Competitive antagonists at histamine H1 receptors may be divided into first (sedating) and second (non-sedating) generation agents. Some, such as Cinnarizine also block muscarinic acetylcholine receptors and are used as anti-emetic agents. Cinnarizine through its calcium channel blocking ability also inhibits stimulation of the vestibular system ...
19. , and Brooker, G. (1977). Fluoride stimulation of slow Ca2+current in cardiac muscle. J . Mol. Cell. Cardiol. 9, 461-475. 20. , and Hofmann, F. (1982). Injection of subunits of cyclic AMP-dependent protein kinase into cardiac myocytes modulates Ca2+current. Nature (London) 298, 576-578. 21. , and Sperelakis, N. (1984). Injection of protein kinase inhibitor into cultured heart cells blocks calcium slow channels. A m . J. Physiol. 246, H630-H634. 22. , and Trautwein, W. (1986). On the mechanism of padrenergic regulation of the Ca2+channel in the guinea pig heart. 8Br-CAMP ( I mM) added to the bath produced a small stimulation of I,, (in the continued presence of G-kinase). This action of the cyclic nucleotide was also reversed by washout. The current tracings illustrated correspond to the two time points labeled a and b in the graph. 0 m M Ba2+as the charge camer. (H. Masuda and N. Sperelakis, 1994). lished, 1994). Note that inhibition of basal I,, began within about 90 sec after breaking into ...
... is a member of the sodium channel blocking class of antiepileptic drugs.[60] This may suppress the release of glutamate and aspartate, two of the dominant excitatory neurotransmitters in the CNS.[61] It is generally accepted to be a member of the sodium channel blocking class of antiepileptic drugs,[62] but it could have additional actions since it has a broader spectrum of action than other sodium channel antiepileptic drugs such as phenytoin and is effective in the treatment of the depressed phase of bipolar disorder, whereas other sodium channel blocking antiepileptic drugs are not, possibly on account of its sigma receptor activity. In addition, lamotrigine shares few side-effects with other, unrelated anticonvulsants known to inhibit sodium channels, which further emphasises its unique properties.[63] It is a triazine derivate that inhibits voltage-sensitive sodium channels, leading to stabilization of neuronal membranes. It also blocks L-, N-, and P-type calcium channels and ...
The hormone prolactin stimulates lactation (production of breast milk). Dopamine, released by the hypothalamus stops the release of prolactin from the pituitary gland. Domperidone, by acting as an anti-dopaminergic agent, results in increased prolactin secretion, and thus promotes lactation (that is, it is a galactogogue). In some nations, including Australia, domperidone is used off-label, based on uncertain and anecdotal evidence of its usefulness, as a therapy for mothers who are having difficulty breastfeeding.[24][25] In the United States, domperidone is not approved for this or any other use.[26][27] A study called the EMPOWER trial was designed to assess the effectiveness and safety of domperidone in assisting mothers of preterm babies to supply breast milk for their infants.[28] The study randomized 90 mothers of preterm babies to receive either domperidone 10 mg orally three times daily for 28 days (Group A) or placebo 10 mg orally three times daily for 14 days followed by domperidone ...
InChI=1S/C20H27N5O5S/c1-15-14-18(23-30-15)19(26)21-11-10-16-6-8-17(9-7-16)31(28,29)24-20(27)22-25-12-4-2-3-5-13-25/h6-9,14H,2-5,10-13H2,1H3,(H,21,26)(H2,22,24,27) ...
... (CBZ), sold under the trade name Tegretol among others, is an anticonvulsant medication used primarily in the treatment of epilepsy and neuropathic pain.[1] It is not effective for absence or myoclonic seizures.[1] It is used in schizophrenia along with other medications and as a second-line agent in bipolar disorder.[3][1] Carbamazepine appears to work as well as phenytoin and valproate for focal and generalised seizures.[4] Common side effects include nausea and drowsiness.[1] Serious side effects may include skin rashes, decreased bone marrow function, suicidal thoughts, or confusion.[1] It should not be used in those with a history of bone marrow problems.[1] Use during pregnancy may cause harm to the baby; however, stopping the medication in pregnant women with seizures is not recommended.[1] Its use during breastfeeding is not recommended.[1] Care should be taken in those with either kidney or liver problems.[1] Carbamazepine was discovered in 1953 by Swiss chemist Walter ...
A channel that is "inwardly-rectifying" is one that passes current (positive charge) more easily in the inward direction (into the cell) than in the outward direction (out of the cell). It is thought that this current may play an important role in regulating neuronal activity, by helping to stabilize the resting membrane potential of the cell. By convention, inward current (positive charge moving into the cell) is displayed in voltage clamp as a downward deflection, while an outward current (positive charge moving out of the cell) is shown as an upward deflection. At membrane potentials negative to potassium's reversal potential, inwardly rectifying K+ channels support the flow of positively charged K+ ions into the cell, pushing the membrane potential back to the resting potential. This can be seen in figure 1: when the membrane potential is clamped negative to the channel's resting potential (e.g. -60 mV), inward current flows (i.e. positive charge flows into the cell). However, when the ...
... also binds to and blocks α2δ subunit-containing VDCCs, similarly to gabapentin and pregabalin, and hence is a gabapentinoid.[9][16] Both (R)-phenibut and (S)-phenibut display this action with similar affinity (Ki = 23 and 39 μM, respectively).[9] Moreover, (R)-phenibut possesses 4-fold greater affinity for this site than for the GABAB receptor (Ki = 92 μM), while (S)-phenibut does not bind significantly to the GABAB receptor (Ki , 1 mM).[9] As such, based on the results of this study, phenibut would appear to have much greater potency in its interactions with α2δ subunit-containing VDCCs than with the GABAB receptor (between 5- to 10-fold).[9] For this reason, the actions of phenibut as a α2δ subunit-containing voltage-gated calcium channel blocker or gabapentinoid may be its true primary mechanism of action, and this may explain the differences between phenibut and its close relative baclofen (which, in contrast, has essentially insignificant activity as a gabapentinoid; Ki = 6 ...
InChI=1S/C24H34N2O/c1-21(2)19-27-20-24(25-15-9-10-16-25)18-26(23-13-7-4-8-14-23)17-22-11-5-3-6-12-22/h3-8,11-14,21,24H,9-10,15-20H2,1-2H3 ...
... (marketed as Depamide by Sanofi-Aventis) is a carboxamide derivative of valproic acid used in the treatment of epilepsy and some affective disorders. It is rapidly metabolised (80%) to valproic acid (another anticonvulsant) but has anticonvulsant properties itself. It may produce more stable plasma levels than valproic acid or sodium valproate and may be more effective at preventing febrile seizures. However, it is over one hundred times more potent as an inhibitor of liver microsomal epoxide hydrolase. This makes it incompatible with carbamazepine and can affect the ability of the body to remove other toxins. Valpromide is no safer during pregnancy than valproic acid. Valpromide is formed through the reaction of valproic acid and ammonia via an intermediate acid chloride. In pure form, valpromide is a white crystalline powder and has melting point 125-126 °C. It is practically insoluble in water but soluble in hot water. It is available on the market in some European countries. ...
Class Ib antiarrhythmic agents are sodium channel blockers. They have fast onset and offset kinetics, meaning that they have little or no effect at slower heart rates, and more effects at faster heart rates. Class Ib agents shorten the action potential duration and reduce refractoriness. These agents will decrease Vmax in partially depolarized cells with fast response action potentials. They either do not change the action potential duration, or they may decrease the action potential duration. Class Ib drugs tend to be more specific for voltage gated Na channels than Ia. Lidocaine in particular is highly frequency dependent, in that it has more activity with increasing heart rates. This is because lidocaine selectively blocks Na channels in their open and inactive states and has little binding capability in the resting state. Class Ib agents are indicated for the treatment of ventricular tachycardia and symptomatic premature ventricular beats, and prevention of ventricular fibrillation. Class Ib ...
... has a potential for drug interactions; caution should be used in combining other medicines with it, including other antiepileptics and mood stabilizers.[12] Lower levels of carbamazepine are seen when administrated with phenobarbital, phenytoin, or primidone, which can result in breakthrough seizure activity. Carbamazepine, as a CYP450 inducer, may increase clearance of many drugs, decreasing their concentration in the blood to subtherapeutic levels and reducing their desired effects.[19] Drugs that are more rapidly metabolized with carbamazepine include warfarin, lamotrigine, phenytoin, theophylline, and valproic acid.[12] Drugs that decrease the metabolism of carbamazepine or otherwise increase its levels include erythromycin,[20] cimetidine, propoxyphene, and calcium channel blockers.[12] Carbamazepine also increases the metabolism of the hormones in birth control pills and can reduce their effectiveness, potentially leading to unexpected pregnancies.[12] As a drug that induces ...
... occludes the pore of calcium-activated voltage-gated shaker K+ channels by binding to one of four independent, overlapping binding sites.[6][7] It binds both to the open and the closed states. In addition, the block is enhanced as the ionic strength is lowered.[8] This block occurs as the Asn 30 on the CTX interacts with the Asp 381 on the K+ channel.[9] The blockade of K+ channels by the charybdotoxin peptide causes neuronal hyperexcitability. Mutations of the Lys31Gln and the Asn30Gln had the effect of lessening the CTX block of the pore on the shaker channel.[9] ...
... has several uses including the treatment of abnormal heart rhythms or arrhythmias, chronic pain, and myotonia. In general when treating arrhythmias, mexiletine is reserved for use in dangerous heart rhythm disturbances such as ventricular tachycardia.[2] It is of particular use when treating arrhythmias caused by long QT syndrome.[3] The LQT3 form of long QT syndrome is amenable to treatment with mexiletine as this form is caused by defective sodium channels that continue to release a sustained current rather than fully inactivating, however other forms of long QT syndrome can also be treated with this medication.[3] Mexiletine has been used to treat chronic pain and may also be used to treat muscle stiffness resulting from myotonic dystrophy (Steinert's disease) or nondystrophic myotonias such as myotonia congenita (Thomsen syndrome or Becker syndrome).[4][5] ...
... is available as a generic medication and usually not too expensive.[7] Wholesale it costs between US$0.003 and US$0.15 per dose.[8] A month of treatment is about US$30 in the United States.[2] Since September 2012, the marketing licence in the UK has been held by Flynn Pharma Ltd, of Dublin, Ireland, and the product, although identical, has been called Phenytoin Sodium xxmg Flynn Hard Capsules. (The xxmg in the name refers to the strength-for example "Phenytoin sodium 25 mg Flynn Hard Capsules").[49] The capsules are still made by Pfizer's Goedecke subsidiary's plant in Freiburg, Germany and they still have Epanutin printed on them.[50] After Pfizer's sale of the UK marketing licence to Flynn Pharma, the price of a 28-pack of 25 mg phenytoin sodium capsules marked Epanutin rose from 66p (about $0.88) to £15.74 (about $25.06). Capsules of other strengths also went up in price by the same factor-2384%,[51] costing the UK's National Health Service an extra £43 million (about $68.44 ...
... is effective for prevention of shivering during surgery or recovery from surgery.[5][6] Nefopam was significantly more effective than aspirin as an analgesic in one clinical trial,[7] although with a greater incidence of side effects such as sweating, dizziness and nausea, especially at higher doses.[8][9] The estimated relative potency of nefopam to morphine indicates that 20 mg of nefopam HCl is the approximate analgesic equal of 12 mg of morphine with comparable analgesic efficacy to morphine,[10][11][12] or oxycodone,[13] while Nefopam tends to produce fewer side effects, does not produce respiratory depression,[14] and has much less abuse potential, and so is useful either as an alternative to opioids, or as an adjunctive treatment for use alongside opioid(s) or other analgesics.[12][15] Nefopam is also used to treat severe hiccups.[16] ...
Bencyclane, a spasmolytic agent and vasodilator is produced from it, for example. Pimelic acid is produced by the oxidative ...
C04AF01 Kallidinogenase C04AX01 Cyclandelate C04AX02 Phenoxybenzamine C04AX07 Vincamine C04AX10 Moxisylyte C04AX11 Bencyclane ...
... bencyclane MeSH D02.455.426.392.368.284.900 --- tropolone MeSH D02.455.426.392.368.367 --- cyclohexanes MeSH D02.455.426.392. ...
... bencyclane (INN) bendacalol (INN) bendamustine (INN) bendazac (INN) bendazol (INN) Bendectin benderizine (INN) Bendopa ...
... is an antispasmodic, vasodilator & platelet aggregation inhibitor. https://books.google.co.uk/books?isbn=1475720858 ...
... , also known as thymoxamine, is a drug used in urology for the treatment of erectile dysfunction.[1] It is an α1-adrenergic antagonist.[2] In the United Kingdom, Moxisylte is marketed as Opilon (Archimedes Pharma UK Ltd) and is used for the short-term treatment of primary Reynaud's syndrome. This is a condition where the fingers and toes become discoloured and is triggered by responses to cold, or emotional distress. Opilon tablets help by improving blood circulation to the extremities.[3][4] ...
Bencyclane is an antispasmodic, vasodilator & platelet aggregation inhibitor. https://books.google.co.uk/books?isbn=1475720858 ...
Lamotrigine is a member of the sodium channel blocking class of antiepileptic drugs.[60] This may suppress the release of glutamate and aspartate, two of the dominant excitatory neurotransmitters in the CNS.[61] It is generally accepted to be a member of the sodium channel blocking class of antiepileptic drugs,[62] but it could have additional actions since it has a broader spectrum of action than other sodium channel antiepileptic drugs such as phenytoin and is effective in the treatment of the depressed phase of bipolar disorder, whereas other sodium channel blocking antiepileptic drugs are not, possibly on account of its sigma receptor activity. In addition, lamotrigine shares few side-effects with other, unrelated anticonvulsants known to inhibit sodium channels, which further emphasises its unique properties.[63] It is a triazine derivate that inhibits voltage-sensitive sodium channels, leading to stabilization of neuronal membranes. It also blocks L-, N-, and P-type calcium channels and ...
The hormone prolactin stimulates lactation (production of breast milk). Dopamine, released by the hypothalamus stops the release of prolactin from the pituitary gland. Domperidone, by acting as an anti-dopaminergic agent, results in increased prolactin secretion, and thus promotes lactation (that is, it is a galactogogue). In some nations, including Australia, domperidone is used off-label, based on uncertain and anecdotal evidence of its usefulness, as a therapy for mothers who are having difficulty breastfeeding.[24][25] In the United States, domperidone is not approved for this or any other use.[26][27] A study called the EMPOWER trial was designed to assess the effectiveness and safety of domperidone in assisting mothers of preterm babies to supply breast milk for their infants.[28] The study randomized 90 mothers of preterm babies to receive either domperidone 10 mg orally three times daily for 28 days (Group A) or placebo 10 mg orally three times daily for 14 days followed by domperidone ...
Omega, delta and kappa families of conotoxins have a knottin or inhibitor cystine knot scaffold. The knottin scaffold is a very special disulfide-through-disulfide knot, in which the III-VI disulfide bond crosses the macrocycle formed by two other disulfide bonds (I-IV and II-V) and the interconnecting backbone segments, where I-VI indicates the six cysteine residues starting from the N-terminus. The cysteine arrangements are the same for omega, delta and kappa families, even though omega conotoxins are calcium channel blockers, whereas delta conotoxins delay the inactivation of sodium channels, and kappa conotoxins are potassium channel blockers.[7] ...
Bencyclane. Bencyclane may increase the hypotensive activities of Nitroprusside.. Experimental. Bendroflumethiazide. The risk ...
Bencyclane. The therapeutic efficacy of Mineral oil can be decreased when used in combination with Bencyclane.. Experimental. ...
BIOTRANSFORMATION. Prof. Dr. Basavaraj K. Nanjwade M. Pharm., Ph. D Department of Pharmaceutics KLE Universitys College of Pharmacy BELGAUM - 590010, Karnataka, India Cell No: 0091 9742431000 E-mail: [email protected] Contents:-. Introduction Phase I reaction Phase II reaction Slideshow 1137530 by zayit
Effects of Bencyclane on Human Platelet Aggregation and on Prostaglandin Synthesis by the Platelet (1977) ...
Bencyclane, a spasmolytic agent and vasodilator is produced from it, for example. Pimelic acid is produced by the oxidative ...
The Effect of Bencyclane on the K+- and Ca++-Induced Pial Arterial Constriction ...
... bencyclane, quinidine, bretylium, lifarizine, lamotrigine, flunarizine, and fluspirilene. 10. 10.-12. (canceled) 13. The method ... bencyclane, lifarizine, and strychnine. Still other ion channel blockers can be modified to incorporate a nitrogen atom ... bencyclane, quinidine, bretylium, lifarizine, lamotrigine, flunarizine, and fluspirilene. 31. The quarternary amine derivative ... bencyclane, quinidine, bretylium, lifarizine, lamotrigine, flunarizine, and fluspirilene. Exemplary derivatives are described ...
... bencyclane, ifenprodil tartarate, molsidomine, clonidine, prazosin and the like; 16. Anti-convulsants such as, nitrazepam, ...
Halidor (Bencyclane). Expiration date: tablets 08/2021, vials 01/2020 Structure and Composition:Tablets. 1 tablet con.. ...
... bencyclane, bendamustine, bendazac, bendazol, benderizine, bendroflumethiazide, benethamide penicillin, benexate, benflorex, ...
Mexiletine has several uses including the treatment of abnormal heart rhythms or arrhythmias, chronic pain, and myotonia. In general when treating arrhythmias, mexiletine is reserved for use in dangerous heart rhythm disturbances such as ventricular tachycardia.[2] It is of particular use when treating arrhythmias caused by long QT syndrome.[3] The LQT3 form of long QT syndrome is amenable to treatment with mexiletine as this form is caused by defective sodium channels that continue to release a sustained current rather than fully inactivating, however other forms of long QT syndrome can also be treated with this medication.[3] Mexiletine has been used to treat chronic pain and may also be used to treat muscle stiffness resulting from myotonic dystrophy (Steinerts disease) or nondystrophic myotonias such as myotonia congenita (Thomsen syndrome or Becker syndrome).[4][5] ...
This article is issued from Wikipedia - version of the 3/7/2016. The text is available under the Creative Commons Attribution/Share Alike but additional terms may apply for the media files ...
... is a drug which acts as a potent blocker of the Cav2 type calcium channels. It was developed as a potential analgesic after the discovery that the selective Cav2.2 blocker ziconotide is an active analgesic with similar efficacy to strong opioid drugs but comparatively milder side effects. Unlike ziconotide, TROX-1 is not so selective, and also blocks the Cav2.1 and Cav2.3 calcium channel subtypes, but it has the great advantage of being orally active, whereas ziconotide must be administered intrathecally, by injection into the spinal fluid. In animal studies of TROX-1, analgesic effects were observed with similar efficacy to NSAIDs such as naproxen or diclofenac, and anti-allodynia effects equivalent to pregabalin or duloxetine.[1]. ...
Bencyclane). 520. 240.00...1070.00. ????? 183. 240.00...1070.00. ????? 337. 303.00...1044.00. ????? ...
Chemically, topiramate is a sulfamate modified fructose diacetonide - a rather unusual chemical structure for a pharmaceutical. Topiramate is quickly absorbed after oral use. Most of the drug (70%) is excreted in the urine unchanged. The remainder is extensively metabolized by hydroxylation, hydrolysis, and glucuronidation. Six metabolites have been identified in humans, none of which constitutes more than 5% of an administered dose. Several cellular targets have been proposed to be relevant to the therapeutic activity of topiramate.[38] These include (1) voltage-gated sodium channels; (2) high-voltage-activated calcium channels; (3) GABA-A receptors; (4) AMPA/kainate receptors; and (5) carbonic anhydrase isoenzymes. There is evidence that topiramate may alter the activity of its targets by modifying their phosphorylation state instead of by a direct action.[39] The effect on sodium channels could be of particular relevance for seizure protection. Although topiramate does inhibit ...
Bencyclane *Carbocromen *Cinnarizine *Crataegus *Dyphylline *Etamivan *Etofylline *Hexobendine *Magnesium Aspartate *Magnesium ...
Lamotrigine is a member of the sodium channel blocking class of antiepileptic drugs.[56] It is a triazine derivate that inhibits voltage-sensitive sodium channels, leading to stabilization of neuronal membranes. It also blocks L-, N-, and P-type calcium channels and has weak 5-hydroxytryptamine-3 (5-HT3) receptor inhibition. These actions are thought to inhibit release of glutamate at cortical projections in the ventral striatum limbic areas,[57] and its neuroprotective and antiglutamatergic effects have been pointed out as promising contributors to its mood stabilizing activity.[58] Observations that lamotrigine reduced γ-aminobutyric acid (GABA) A receptor-mediated neurotransmission in rat amygdala,[59] suggest that a GABAergic mechanism may also be involved, although this concept is controversial.[60]. Lamotrigine does not have pronounced effects on any of the usual neurotransmitter receptors (adrenergic, dopamine D1 and D2, muscarinic, GABA, histaminergic H1, serotonin 5-HT2, and ...
... blocks hERG-type potassium channels [5][6] by binding to the open channels.[7] Its structural target within the hERG-channel is unclear, but some other methanesulfonanilide class III antiarrhythmic drugs are known to bind to the S6 domain or C-terminal of the hERG-channel.[8][9][10][11][12][13] Reducing IKr in myocardial cells prolongs the cardiac action potential and thus prolongs the QT-interval.[7][14] In non-cardiac cells, blocking Ikr has a different effect: it increases the frequency of action potentials.[5] ...
Benzocaine, sold under the brand name Orajel among others, is an ester local anesthetic commonly used as a topical pain reliever or in cough drops. It is the active ingredient in many over-the-counter anesthetic ointments such as products for oral ulcers. It is also combined with antipyrine to form
Calcium channel blockers work by blocking voltage-gated calcium channels (VGCCs) in cardiac muscle and blood vessels. This decreases intracellular calcium leading to a reduction in muscle contraction. In the heart, a decrease in calcium available for each beat results in a decrease in cardiac contractility. In blood vessels, a decrease in calcium results in less contraction of the vascular smooth muscle and therefore an increase in arterial diameter (CCBs do not work on venous smooth muscle), a phenomenon called vasodilation. Vasodilation decreases total peripheral resistance, while a decrease in cardiac contractility decreases cardiac output. Since blood pressure is determined by cardiac output and peripheral resistance, blood pressure drops. Calcium channel blockers are especially effective against large vessel stiffness, one of the common causes of elevated systolic blood pressure in elderly patients.[2]. With a relatively low blood pressure, the afterload on the heart decreases; this ...
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