Drugs online research references
Eur J Pharm Biopharm. 2002 Jul;54(1):9-15.
Once daily sustained release tablets of venlafaxine, a novel antidepressant.
Makhija SN, Vavia PR.
Pharmaceutical Division, Department of Chemical Technology (Autonomous), University of Mumbai, Nathalal Parikh Marg, Matunga, Mumbai-400019, India.
Venlafaxine is a unique antidepressant that differs structurally from other currently available antidepressants. Sustained release tablets of venlafaxine to be taken once daily were formulated with venlafaxine hydrochloride equivalent to 75 mg of venlafaxine base. Matrix system based on swellable as well as non-swellable polymers was selected for sustaining the drug release. Different polymers viz. hydroxypropylmethylcellulose (HPMC), cellulose acetate, Eudragit RSPO, ethylcellulose etc. were studied. Combinations of non-swellable polymers with HPMC were also tried in order to get the desired sustained release profile over a period of 16 h. The effect of drug to polymer ratio on in vitro release was studied. The marketed formulation was evaluated for different parameters such as appearance, weight variation, drug content and in vitro drug release. The optimized formulation was subjected to stability studies at different temperature and humidity conditions as per ICH guidelines. These were evaluated for appearance, weight variation, thickness, hardness, friability, drug content and in vitro drug release at selected time intervals. In vivo studies were carried out for the optimized formulation in 12 healthy human volunteers and the pharmacokinetic parameters were compared with the marketed one.
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In this article, health care expenditures are assessed for patients diagnosed with depression who are being treated with either venlafaxine (immediate or extended release) or a selective serotonin-reuptake inhibitor (SSRI). Patients beginning treatment for a new depressive episode were identified retrospectively from 1994 to 1998. Before beginning therapy, patients prescribed venlafaxine (N = 353) had more nonmental illnesses (0.84 vs. 0.75 clinical events/patient, respectively; P < .01) and hospitalizations for mental illness (0.56 vs. 0.30 hospitalizations/patient; P = .06) than patients prescribed SSRIs (N = 7,330). In the six months after initiating treatment, venlafaxine was associated with lower hospitalization expenditures for nonmental illness than were SSRIs ($206 vs. $472, respectively; P = .02), but total health care expenditures were not significantly different.
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unica.it
Venlafaxine is an antidepressant drug that inhibits the reuptake of serotonin and norepinephrine with different efficacies. The effects of repeated administration of this drug on the increase in the extracellular concentration of norepinephrine in the prefrontal cortex, induced by stress or by the anxiogenic drug FG 7142, were studied in freely moving rats. Exposure to foot-shock stress induced a marked increase (+120%) in the extracellular norepinephrine concentration in the prefrontal cortex of control rats. Long-term administration of venlafaxine (10 mg/kg i.p., once a day for 21 days) reduced the effect of stress on norepinephrine output by 75%. This effect of venlafaxine persisted for at least 5 days after discontinuation of drug treatment. Acute administration of FG 7142 (20 mg/kg i.p.), a benzodiazepine receptor inverse agonist, increased norepinephrine output (+90%) in control rats. Chronic treatment with venlafaxine prevented the effect of FG 7142. In contrast, the acute administration of this antidepressant had no effect on the stress- or FG 7142-induced increase in norepinephrine output. These plastic changes in the sensitivity of norepinephrine neurones to foot-shock stress and to an anxiogenic drug may reveal an important neuronal mechanism for the physiological regulation of emotional state. Furthermore, this mechanism might be relevant to the anxiolytic and antidepressant effects of venlafaxine.
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