Clinical drug investigation
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Randomized Controlled Trial Comparative Study
Single-dose pharmacokinetics of once-daily cyclobenzaprine extended release 30 mg versus cyclobenzaprine immediate release 10 mg three times daily in healthy young adults : a randomized, open-label, two-period crossover, single-centre study.
Cyclobenzaprine immediate release (CIR) has shown efficacy in the treatment of muscle spasm associated with acute, painful musculoskeletal conditions. An extended-release formulation of cyclobenzaprine (CER) has been developed to provide effective muscle spasm relief with once-daily dosing. The objective of this study was to compare the pharmacokinetics of CER and CIR. ⋯ The pharmacokinetic profile of once-daily CER reflected the mode of administration, providing a controlled release of cyclobenzaprine with sustained plasma concentrations, in contrast to the fluctuating profile of CIR. CER 30 mg once daily and CIR 10 mg three times daily resulted in comparable systemic exposures.
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Clinical Trial
Formula for use of mannitol in patients with intracerebral haemorrhage and high intracranial pressure.
Although mannitol has been widely used in hospitals to treat patients with high intracranial pressure (ICP) secondary to intracerebral haemorrhage (ICH), no universal agreement has been reached regarding the optimal dosage of this agent for achieving appropriate intracranial decompression. The aim of this study was to investigate the effects of different mannitol dosages on ICP and the effects of other factors, such as sex, age, haemorrhage location and haematoma volume, on the ICP-lowering effect of mannitol. The data obtained were then used to construct a formula for estimating the total dosage of mannitol required to reduce ICP in individual patients with ICH. ⋯ The total mannitol dosage required for individual patients with ICH and elevated ICP can be calculated by considering the location of the haemorrhage, the volume of the haematoma and the pretreated ICP reading. To this end, the following formula was derived in the study: Total dosage of mannitol (mL of 20% mannitol) = (x + 31.17900 x y - 3.39853 x z - 244.47590)/0.00752, where x = the pretreated ICP (mmH(2)O), y = the haemorrhage location (supratentorial ICH: y = 0, infratentorial ICH: y = 1) and z = the volume of haematoma (mL). Use of this formula in the clinical setting should help reduce the possibility of adverse effects resulting from administration of excessive dosages of mannitol.
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Randomized Controlled Trial
Bioequivalence following buccal and sublingual placement of fentanyl buccal tablet 400 microg in healthy subjects.
The fentanyl buccal tablet (FBT) is formulated to enhance the rate and extent of fentanyl absorption across the buccal mucosa. FBT is indicated for the management of breakthrough pain (a transient flare of pain on a background of chronic pain otherwise controlled by treatment with opioids) in patients with cancer who are already receiving and who are tolerant to opioid therapy for their underlying persistent cancer pain. This study assessed the bioequivalence of a single 400-microg dose of FBT following buccal (i.e. above a molar tooth between the upper gum and cheek) and sublingual (i.e. placed under the tongue) placement in order to provide an alternative option to patients. ⋯ The results of this study support sublingual FBT placement as a viable alternative to buccal placement in patients who may require an alternate administration site.
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A novel transdermal matrix patch delivery system for fentanyl has been developed to deliver improved management of cancer pain compared with that obtained using current fentanyl reservoir patches. This study was carried out to assess the efficacy, safety and pharmacokinetic profiles of a 12.5 microg/h transdermal matrix fentanyl patch administered with the objective of replacing morphine, oral oxycodone or fentanyl injection formulations. The study also evaluated how the pharmacokinetic profiles of higher dose fentanyl patches (25, 37.5 and 50 microg/h) changed following dose adjustments to optimize management of cancer pain. ⋯ The fentanyl matrix transdermal patch formulation employed in this study demonstrated sufficient cancer pain control for patients switching from morphine or oral oxycodone preparations. The patch tested was well tolerated and its use did not result in any increased incidence of adverse drug reactions over those commonly found with opioid analgesics.
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A 48-year-old woman suddenly lost consciousness as a result of a right rostral pontine tegmentum haemorrhage. The patient presented with decerebrate rigidity (DR) and regained full consciousness 5 days after the initial onset. ⋯ The patients' preserved consciousness and motor-evoked potentials to transcranial magnetic stimulation indicated a derangement of the extrapyramidal tracts with preservation of the pyramidal tracts. This case report discusses the possible mechanisms of action of gabapentin in DR.