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Anxiolytics: Predicting Response/Maximizing Efficacy
Published in Mark S. Gold, R. Bruce Lydiard, John S. Carman, Advances in Psychopharmacology: Predicting and Improving Treatment Response, 2018
Acute potentiation of adrenergic transmission results in enhanced alpha-1 and beta effects; however, chronic potentiation shifts the transmission towards alpha-1 because of a down regulation of beta receptor number and thus activity over about 3 weeks.100,166 Some recently discovered pharmacological manipulations of the beta receptor may come to be important for the treatment of anxiety. Hyperthyroidism increases B receptor density.167 Combination of antidepressant and alpha-2 blocker accelerates and increases the beta adrenergic and the alpha-2 receptor subsensitivity induced by either alone.168–171 Acute and chronic administration of amphetamine or cocaine caused an increase beta adrenergic density in rat brain.172 Chronic fluphenazine causes increased beta adrenergic receptor density without binding directly to the beta adrenergic receptor.173 Chronic desmethylimipraminl doesn’t change norepiniphrine transporter, alpha, adrenergic, serotonergic, enkephlinergic, cholinergic or histaminergic receptor density.174 Chronic trazodone doesn’t change beta adrenergic receptors, but results in increased numbers of 5HT receptors.149 The K, of trazodone on 5HT is 570 nm.175
Complex Regional Pain Syndrome, Types I and II
Published in Mark V. Boswell, B. Eliot Cole, Weiner's Pain Management, 2005
Various authors have reported that sympathetic blocks are or are not effective, with efficacy for sympathectomy reported to be between 12 and 97% (Payne, 1986). However, Raja et al. (1986, 1991) reported no relief with sympathetic blocks. Payne has suggested that a dorsal root entry zone (DREZ) procedure may prove effective. Ghostine et al. (1984) have suggested the use of phenoxybenzamine. They reported 40 consecutive cases of CRPS II, all of which involved nerve injuries from bullet or shrapnel wounds. The hydraulic effect of high-speed bullet injuries is well demonstrated by photographs taken of a bullet striking an object. The Ghostine group noted partial motor paralysis in the distribution of the damaged nerve in 70% of the cases. Over time, these deficits resolved in many of the cases, however. They also noted vasomotor changes, usually severe vasodilatation and sweating and less often vasoconstriction (Ghostine et al., 1984). Rarely were trophic changes noted. The majority of the cases involved the sciatic nerve, median nerve, brachial plexus, cauda equina, and occipital nerve, in descending order. The treatment that Ghostine et al. (1984) used was phenoxybenzamine, which is a postsynaptic alpha-1-blocker and a presynaptic alpha-2-blocker. As mentioned earlier under the etiology of CRPS II, nerve sprouts, which are one of the theoretical origins of this disorder, seem to be highly excitable on the administration of norepinephrine; the excitability can be reversed with alpha-blocking agents such as phentolamine, but are unaffected by beta-blocking agents. The dosage of the drug used by Ghostine et al. initially was 10 mg three times a day, although this varied from patient to patient. Eventually maximum dosages of 40 to 120 mg/day were reached, with treatment lasting 6 to 8 weeks. Common side effects were orthostatic hypotension in about 45% of the patients and reduced ejaculatory ability in about 8% of the patients. In some instances, treatment lasted as long as 16 weeks. It is important to note that the patients were all treated within 2 to 70 days after the onset of their injury.
Pharmacotherapy for erectile dysfunction in diabetic males
Published in Expert Opinion on Pharmacotherapy, 2018
Yohimbine is an alpha 2-blocker that is reported to have a marginal effect on erectile function. Limited studies had shown that yohimbine to be a promising therapy for ED in type 2 DM [50]. Studies on nonorganic ED patients have shown some response over placebo. Side effects include anxiety, tremors, palpitation, and hypertension.