RESUMO
Treatment with Tenutex® should be considered in patients diagnosed with scabies if the first-line treatment with 5% permethrin fails. Treatment failure with 5% permethrin may be due to tolerance or resistance in scabies mites.
RESUMO
Patients who are undergoing treatment with bleomycin and develop prurigo or rash should be suspected of bleomycin-induced flagellate erythema and treated early with antihistamines, topical, and oral corticosteroids.
RESUMO
We describe the synthesis of tetrahydroisoquinolines and tetrahydroisoquinolinium salts together with their pharmacological properties at various nicotinic acetylcholine receptors. In general, the compounds were α4ß2 nAChR antagonists, with the tetrahydroisoquinolinium salts being more potent than the parent tetrahydroisoquinoline derivatives. The most potent α4ß2 antagonist, 6c, exhibited submicromolar binding Ki and functional IC50 values and high selectivity for this receptor over the α4ß4 and α3ß4 nAChRs. Whereas the (S)-6c enantiomer was essentially inactive at α4ß2, (R)-6c was a slightly more potent α4ß2 antagonist than the reference ß2-nAChR antagonist DHßΕ. The observation that the α4ß2 activity resided exclusively in the (R)-enantiomer was in full agreement with docking studies. Several of tetrahydroisoquinolinium salts also displayed agonist activity at the α7 nAChR. Preliminary in vivo evaluation revealed antidepressant-like effects of both (R)-5c and (R)-6c in the mouse forced swim test, supporting the therapeutic potential of α4ß2 nAChR antagonists for this indication.
Assuntos
Simulação de Acoplamento Molecular , Receptores Nicotínicos/efeitos dos fármacos , Tetra-Hidroisoquinolinas/farmacologia , Animais , Antidepressivos/química , Humanos , Camundongos , Antagonistas Nicotínicos , Sais/farmacologia , Estereoisomerismo , Natação , Tetra-Hidroisoquinolinas/síntese química , Receptor Nicotínico de Acetilcolina alfa7/agonistasRESUMO
Primary hyperparathyroidism (pHPT) is almost exclusively the result of a solitary parathyroid adenoma. In most cases, the affected gland can be surgically removed, but precise preoperative imaging is essential for adenoma localization prior to surgical intervention. In this study, we evaluated the diagnostic value of four-dimensional computed tomography (4D-CT) as a preoperative imaging tool in relation to the localization of pathologic parathyroid glands in patients with pHPT and negative sestamibi scans. This study included 43 consecutive patients with pHPT referred for parathyroidectomy at the Department of Head and Neck Surgery of Copenhagen University Hospital Rigshospitalet in 2011 and 2012. All patients had a 4D-CT performed prior to parathyroidectomy. CT localization of the suspected adenoma was correlated to the actual surgical findings and subsequent histological diagnosis was also available as references for the accuracy of this imaging tool. Hyperfunctioning parathyroid glands were found in 40 patients. 4D-CT identified 32 solitary hyperfunctioning parathyroid glands located on the correct side of the neck (PPV 76 %) and 21 located within the correct quadrant (PPV 49 %). Unilateral resection was performed in 72 % of patients due to the localization findings of preoperative imaging. 4D-CT can, therefore, be considered an effective method for the preoperative localization of parathyroid adenomas and is an important tool in surgical intervention for patients referred to parathyroidectomy.