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prazosin extended release

Christopher Rodgman, Christopher D Verrico, Manuela Holst, Daisy Thompson-Lake, Colin N Haile, Richard De La Garza, Murray A Raskind, Thomas F Newton
BACKGROUND: Serotonin and norepinephrine reuptake inhibitors are effective first-line agents for the treatment of posttraumatic stress disorder (PTSD), but treatment is associated with a range of side effects that limit treatment adherence. Prazosin, an α1-noradrenergic antagonist with a half-life of roughly 2-3 hours, has shown promise in the treatment of sleep disturbance and nightmares. Doxazosin extended release (XL) is also an α1-noradrenergic antagonist but with a half-life of approximately 15-19 hours...
May 2016: Journal of Clinical Psychiatry
Paula E Park, Joel E Schlosburg, Leandro F Vendruscolo, Gery Schulteis, Scott Edwards, George F Koob
Opioids represent effective drugs for the relief of pain, yet chronic opioid use often leads to a state of increased sensitivity to pain that is exacerbated during withdrawal. A sensitization of pain-related negative affect has been hypothesized to closely interact with addiction mechanisms. Neuro-adaptive changes occur as a consequence of excessive opioid exposure, including a recruitment of corticotropin-releasing factor (CRF) and norepinephrine (NE) brain stress systems. To better understand the mechanisms underlying the transition to dependence, we determined the effects of functional antagonism within these two systems on hyperalgesia-like behavior during heroin withdrawal utilizing models of both acute and chronic dependence...
March 2015: Addiction Biology
Dai Li-Bo, Zhu Rong-Hua, Li Huan-De, Wang Feng, Fang Ping-Fei, Lou Jiang
A simple, selective, and sensitive high performance liquid chromatography (HPLC) procedure has been developed for determination of trazodone in human plasma. Prazosin was employed as the internal standard (IS). Sample preparation involved liquid-liquid extraction by methyl tert-butyl ether after alkalinization with ammonia. The HPLC separation was performed on a CAPCELL PAK SCX column (250mm×4.6mm, 5.0μm, Shiseido, Japan) with a mobile phase of acetonitrile/80mmol/L ammonium phosphate (pH adjusted to 6.0) (60:40, v/v) at a flow rate of 1...
January 1, 2014: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
Jun Sang Park, Ji Yeon Shim, Jung Soo Park, Young Wook Choi, Seong Hoon Jeong
A novel three-layered tablet consisting of a water-soluble mid-layer and two barrier layers with swellable polymers was investigated to develop a preferable once-a-day formulation containing terazosin HCl as a hydrophilic model drug. When the tablet was exposed to a release medium, the medium quickly permeated to the mid-layer and the two barrier layers swelled surrounding the mid-layer rapidly. It facilitated the tablet to absorb a lot of water compared with monolithic matrix. Moreover, formation of a lot of pores in the tablet during dissolution could be observed, suggesting significant water absorption in the inner matrix and swollen polymers of the tablet...
June 2011: Drug Development and Industrial Pharmacy
Raghavendra V Kulkarni, V Sreedhar, Srinivas Mutalik, C Mallikarjun Setty, Biswanath Sa
Interpenetrating network (IPN) hydrogel membranes of sodium alginate (SA) and poly(vinyl alcohol) (PVA) were prepared by solvent casting method for transdermal delivery of an anti-hypertensive drug, prazosin hydrochloride. The prepared membranes were thin, flexible and smooth. The X-ray diffraction studies indicated the amorphous dispersion of drug in the membranes. Differential scanning calorimetric analysis confirmed the IPN formation and suggests that the membrane stiffness increases with increased concentration of glutaraldehyde (GA) in the membranes...
November 1, 2010: International Journal of Biological Macromolecules
H K Ganesh, Shrikrishna V Acharya, Joe Goerge, Tushar R Bandgar, Padma S Menon, Nalini S Shah
Eleven subjects aged <20 yr with histologically proven pheochromocytoma between 1987 and 2006 were analyzed. Family history was present in 18%. In 2 patients, pheochromocytoma was part of VHL and in one it was associated with MEN 2. Twenty four hour urine VMA level was elevated in 100% and metanephrine level in 73%. CT/ MRI were showing the tumor in all. Prazosin extended release tablets (maximum 30 mg/day) were used in 73% and doxazosin (maximum 12 mg/ day) in 27%. Intraoperative BP fluctuations were seen in 27%...
November 2009: Indian Journal of Pediatrics
David R P Guay
BACKGROUND: Extended-release (ER) alfuzosin hydrochloride is the most recently approved alpha-adrenergic receptor antagonist (AARA) for the management of symptomatic benign prostatic hyperplasia (BPH). Although new to the United States, alfuzosin has been available in immediate-release (IR) and sustained-release (SR) formulations in other countries for many years. OBJECTIVE: This article reviews data on the pharmacodynamics, pharmacokinetics, efficacy, tolerability, drug-interaction potential, and dosing of alfuzosin ER...
March 2004: American Journal of Geriatric Pharmacotherapy
A Dekeyne, M J Millan
Though drug discrimination techniques have proven invaluable in characterizing the interoceptive properties of drugs of abuse, antipsychotics and anxiolytics, with the exception of some fragmentary data with tricyclic agents, surprisingly few studies have been undertaken with antidepressants. Nevertheless, the preferential dopamine (DA) reuptake inhibitor, bupropion, elicits a robust discriminative stimulus in rodents. Moreover, in rats trained on a two-lever FR-10 schedule for food reward, the selective serotonin (5-HT) reuptake inhibitor (SSRI), citalopram, and the noradrenaline (NA) reuptake inhibitor (NARI), reboxetine, elicit discriminative stimuli at doses that selectively elevate extracellular levels of 5-HT and NA, respectively...
September 2003: Behavioural Pharmacology
Analía Bortolozzi, Mercè Amargós-Bosch, Albert Adell, Llorenç Díaz-Mataix, Jordi Serrats, Sebastià Pons, Francesc Artigas
In the rat, postsynaptic 5-hydroxytryptamine2A receptors medial prefrontal cortex control the activity of the serotonergic system through changes in the activity of pyramidal neurons projecting to the dorsal raphe nucleus. Here we extend these observations to mouse brain. The prefrontal cortex expresses abundant 5- hydroxytryptamine2A receptors, as assessed by immunohistochemistry, Western blots and in situ hybridization procedures. The application of the 5-hydroxytryptamine2A/2C agonist DOI (100 microm) by reverse dialysis in the medial prefrontal cortex doubled the local release of 5-hydroxytryptamine...
September 2003: European Journal of Neuroscience
K M Smith, J B Macmillan, K M McCulloch, J C McGrath
OBJECTIVE: The in vitro interaction between sympathetic nerves and basal nitric oxide release was studied in a resistance artery, since these interact powerfully in large vessels. METHODS: The pharmacological interaction between L-NAME and vasoconstriction to field stimulation of sympathetic nerves or exogenous norepinephrine was studied in rabbit cutaneous resistance arteries in wire myographs. RESULTS: Relaxation of norepinephrine-induced tone by acetylcholine, but not sodium nitroprusside, was blocked by N omega-nitro-L-arginine methyl ester (L-NAME: 100 microM), indicating that the agonist-induced release of nitric oxide could oppose the vasoconstrictor effect of norepinephrine and confirming that L-NAME had no effect on endothelium-independent vasodilatation...
August 15, 1999: Cardiovascular Research
E Carboni, M T Rolando, A Silvagni, G Di Chiara
Neuroleptics are known to stimulate dopamine release in neostriatal terminal areas. In the present study, we have investigated by brain microdialysis in freely moving rats the effect of typical and atypical neuroleptics on dopamine transmission in the bed nucleus of stria terminalis, a dopamine terminal area belonging to the limbic system and recently assigned the so-called extended amygdala. Mean basal dialysate dopamine values were 14.3 f moles/20 microliters sample. Dopamine output in dialysates was increased dose-dependently by clozapine (max + 158%, 298%, and 461% of basal at 5, 10, and 20 mg/kg i...
February 2000: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
E F LaBelle, E Polyak
The mechanism of agonist-activated arachidonate release was studied in segments of rat tail artery. Tail artery segments were prelabeled with [3H]arachidonate and then stimulated with norepinephrine (NE), and the radioactivity of the extracellular medium was determined. NE stimulated arachidonate release from the tissue without increasing arachidonic acid levels within cellular cytosol or crude membranes. About 90% of the extracellular radioactivity was shown to be unmetabolized arachidonate by TLC. Arachidonic acid release was not inhibited by the removal of the endothelium from the artery...
April 1998: American Journal of Physiology
G Weidinger
Bunazosin (CAS 52712-76-2), a quinazoline derivative, selectively blocks alpha1-receptors. In addition to its potent antihypertensive property, beneficial effects on lipid metabolism, glucose metabolism, vascular smooth muscle cell proliferation, it can be used in the presence of concomitant diseases, such as obstructive bronchitis, chronic renal insufficiency, peripheral arterial occlusive disease, and diabetes mellitus. In its extended-release formulation (bunazosin retard), it is generally a well-tolerated alpha1-blocker when compared to other agents in its class...
November 1995: Arzneimittel-Forschung
D J Pettibone, G P Mueller
Parallel measurements of plasma alpha-melanotropin-like immunoreactivity (alpha-MSH-LI) and beta-endorphin-like immunoreactivity (beta-END-LI) were used to examine the differential adrenergic control of beta-END secretion from the anterior lobe (AL) versus the intermediate lobe (IL) of the rat pituitary gland in vivo. Changes in plasma alpha-MSH-LI levels after treatment with various adrenergic agents served as an index of the secretion of the peptides by the IL. Secretion of beta-END-LI from the AL in vivo was evaluated using the selective inhibitory effects of dexamethasone on AL release...
June 1984: Proceedings of the Society for Experimental Biology and Medicine
E Saltiel, A G Ellrodt, J P Monk, M S Langley
Felodipine is a dihydropyridine calcium antagonist which selectively relaxes vascular smooth muscle. By acting at peripheral arterioles, it lowers systemic vascular resistance and thereby produces substantial decreases in blood pressure and increases in cardiac output. Felodipine is indicated for the management of hypertension, and in patients with mild to moderate disease felodipine monotherapy markedly lowers blood pressure. It proved as effective as atenolol, and equivalent to hydrochlorothiazide, either with or without amiloride, in terms of antihypertensive activity...
October 1988: Drugs
T A Day, J C Randle, L P Renaud
The effects of pressure-applied noradrenaline (NA) on the activity of neurosecretory cells of the supraoptic nucleus (SON) were examined in anaesthetized male rats. Spontaneously active, antidromically identified neurosecretory cells were classified as vasopressin (VP)-secreting on the basis of activity patterns and responsiveness to baroreceptor activation. The probability of encountering VP units was enhanced by confining electrode penetrations to the caudal aspect of the SON. Application of low concentrations of NA (50-150 microM) excited 75% of putative VP neurones tested (n = 45), while very high concentrations (1-100 mM) were inhibitory (79%, n tested = 14)...
December 9, 1985: Brain Research
A Lucchelli, M G Santagostino Barbone, E Grana
Previous researches demonstrated that in the rat vas deferens the effects of noradrenaline released by tyramine were more easily affected than those induced by exogenous noradrenaline by the non selective alpha-blockers, phentolamine and dihydroergocristine. The investigation has now been extended to the effects of selective alpha-blockers, prazosin and yohimbine with the aim to see whether the major sensitivity of tyramine to alpha-blockade correlates with the type of receptor activated. The results obtained with the two antagonists which selectively block alpha 1 and alpha 2 receptors strongly resemble each other and those previously obtained with the non selective alpha-adrenoceptor blockers...
August 1985: Pharmacological Research Communications
M L Maayan, R V Sellitto, E M Volpert
Previous studies had suggested that norepinephrine (NE) and its precursors dopamine (DA) and L-DOPA acted similarly on iodine metabolism of isolated thyroid cells. Present studies indicate that this similarity extends to the inhibition by catecholamines of TSH-stimulated T4 release by mouse thyroids incubated in vitro. DA (5 X 10(-4) M), like NE, shown previously, inhibits TSH-stimulated T4 release. This inhibition was reversed by the alpha-blockers phentolamine, prazosin, and yohimbine, but not by the beta-blocker L-propranolol...
February 1986: Endocrinology
D Parkinson, E Coscia, N W Daw
The concentration and location of adrenergic receptors in cat visual cortex have been determined by radioligand binding techniques using [3H]prazosin (alpha 1-adrenergic receptors), [3H]yohimbine (alpha 2-adrenergic receptors) and [3H]dihydroalprenolol (beta-adrenergic receptors). Saturable high affinity binding sites for all of these ligands were found. The beta-adrenergic receptor population was resolved into beta 1- and beta 2-sites that were present in the ratio 35:65. The laminar distributions of the alpha 1-, alpha 2- and beta-adrenergic receptors were different...
August 2, 1988: Brain Research
W Singleton, R K Dix, L Monsen, D Moisey, M Levenstein, D F Bottiglieri, L Silver
The efficacy and safety of prazosin GITS (gastro-intestinal therapeutic system), a new extended-release once-a-day formulation, were assessed both as monotherapy in mild essential hypertension and in combination with a diuretic in moderate essential hypertension in two multicenter, double-blind, placebo-controlled trials. Prazosin GITS (Minipress XL) given once daily in doses of either 10 or 20 mg significantly reduced sitting and standing systolic and diastolic blood pressure compared with placebo in both mild and moderate essential hypertension...
August 16, 1989: American Journal of Medicine
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