Pharmacokinetics and pharmacodynamics of once-daily controlled-release oxybutynin and immediate-release oxybutynin. 2007

Joseph L Reiz, and Paulette Salem, and Andrew C Darke
Department of Scientific Affairs, Purdue Pharma (Canada), 575 Granite Court, Pickering, Ontario, Canada, L1W 3W8. Joseph.Reiz@purdue.ca

Oxybutynin is used to treat patients with urinary urgency, frequency, and urge incontinence. In this 2-way, multiple-dose, crossover study, the pharmacokinetics and pharmacodynamics of once-daily controlled-release oxybutynin were compared with immediate-release oxybutynin. Eighteen healthy male volunteers received one 15-mg controlled-release oxybutynin tablet once daily for 5 days or one 5-mg immediate-release oxybutynin tablet every 8 hours for 5 days. The washout period between treatments was > or =7 days. The mean steady-state AUC for oxybutynin following controlled-release oxybutynin treatment was higher (73.0 ng.h/mL) than following immediate-release oxybutynin treatment (53.6 ng.h/mL) (P = .0001). The mean C(max) was lower for controlled-release oxybutynin (5.7 ng/mL) than for immediate-release oxybutynin (7.5 ng/mL) (P = .0051), with a smaller fluctuation in oxybutynin plasma concentration for controlled-release oxybutynin (135.6%) than for immediate-release oxybutynin (319.3%) (P = .0001). Mean stimulated saliva output was greater for controlled-release oxybutynin, and mean dry mouth severity was less than immediate-release oxybutynin.

UI MeSH Term Description Entries
D008297 Male Males
D008333 Mandelic Acids Analogs or derivatives of mandelic acid (alpha-hydroxybenzeneacetic acid). Acids, Mandelic
D008875 Middle Aged An adult aged 45 - 64 years. Middle Age
D009325 Nausea An unpleasant sensation in the stomach usually accompanied by the urge to vomit. Common causes are early pregnancy, sea and motion sickness, emotional stress, intense pain, food poisoning, and various enteroviruses.
D010276 Parasympatholytics Agents that inhibit the actions of the parasympathetic nervous system. The major group of drugs used therapeutically for this purpose is the MUSCARINIC ANTAGONISTS. Antispasmodic,Antispasmodic Agent,Antispasmodic Drug,Antispasmodics,Parasympathetic-Blocking Agent,Parasympathetic-Blocking Agents,Parasympatholytic,Parasympatholytic Agent,Parasympatholytic Drug,Spasmolytic,Spasmolytics,Antispasmodic Agents,Antispasmodic Drugs,Antispasmodic Effect,Antispasmodic Effects,Parasympatholytic Agents,Parasympatholytic Drugs,Parasympatholytic Effect,Parasympatholytic Effects,Agent, Antispasmodic,Agent, Parasympathetic-Blocking,Agent, Parasympatholytic,Agents, Antispasmodic,Agents, Parasympathetic-Blocking,Agents, Parasympatholytic,Drug, Antispasmodic,Drug, Parasympatholytic,Drugs, Antispasmodic,Drugs, Parasympatholytic,Effect, Antispasmodic,Effect, Parasympatholytic,Effects, Antispasmodic,Effects, Parasympatholytic,Parasympathetic Blocking Agent,Parasympathetic Blocking Agents
D012044 Regression Analysis Procedures for finding the mathematical function which best describes the relationship between a dependent variable and one or more independent variables. In linear regression (see LINEAR MODELS) the relationship is constrained to be a straight line and LEAST-SQUARES ANALYSIS is used to determine the best fit. In logistic regression (see LOGISTIC MODELS) the dependent variable is qualitative rather than continuously variable and LIKELIHOOD FUNCTIONS are used to find the best relationship. In multiple regression, the dependent variable is considered to depend on more than a single independent variable. Regression Diagnostics,Statistical Regression,Analysis, Regression,Analyses, Regression,Diagnostics, Regression,Regression Analyses,Regression, Statistical,Regressions, Statistical,Statistical Regressions
D003692 Delayed-Action Preparations Dosage forms of a drug that act over a period of time by controlled-release processes or technology. Controlled Release Formulation,Controlled-Release Formulation,Controlled-Release Preparation,Delayed-Action Preparation,Depot Preparation,Depot Preparations,Extended Release Formulation,Extended Release Preparation,Prolonged-Action Preparation,Prolonged-Action Preparations,Sustained Release Formulation,Sustained-Release Preparation,Sustained-Release Preparations,Timed-Release Preparation,Timed-Release Preparations,Controlled-Release Formulations,Controlled-Release Preparations,Extended Release Formulations,Extended Release Preparations,Slow Release Formulation,Sustained Release Formulations,Controlled Release Formulations,Controlled Release Preparation,Controlled Release Preparations,Delayed Action Preparation,Delayed Action Preparations,Formulation, Controlled Release,Formulations, Controlled Release,Prolonged Action Preparation,Release Formulation, Controlled,Release Formulations, Controlled,Sustained Release Preparation,Timed Release Preparation,Timed Release Preparations
D004244 Dizziness An imprecise term which may refer to a sense of spatial disorientation, motion of the environment, or lightheadedness. Lightheadedness,Orthostasis,Dizzyness,Light-Headedness,Light Headedness
D006261 Headache The symptom of PAIN in the cranial region. It may be an isolated benign occurrence or manifestation of a wide variety of HEADACHE DISORDERS. Cephalgia,Hemicrania,Bilateral Headache,Cephalalgia,Cephalodynia,Cranial Pain,Generalized Headache,Head Pain,Ocular Headache,Orthostatic Headache,Periorbital Headache,Retro-Ocular Headache,Sharp Headache,Throbbing Headache,Unilateral Headache,Vertex Headache,Bilateral Headaches,Cephalalgias,Cephalgias,Cephalodynias,Cranial Pains,Generalized Headaches,Head Pains,Headache, Bilateral,Headache, Generalized,Headache, Ocular,Headache, Orthostatic,Headache, Periorbital,Headache, Retro-Ocular,Headache, Sharp,Headache, Throbbing,Headache, Unilateral,Headache, Vertex,Headaches,Headaches, Bilateral,Headaches, Generalized,Headaches, Ocular,Headaches, Orthostatic,Headaches, Periorbital,Headaches, Retro-Ocular,Headaches, Sharp,Headaches, Throbbing,Headaches, Unilateral,Headaches, Vertex,Ocular Headaches,Orthostatic Headaches,Pain, Cranial,Pain, Head,Pains, Cranial,Pains, Head,Periorbital Headaches,Retro Ocular Headache,Retro-Ocular Headaches,Sharp Headaches,Throbbing Headaches,Unilateral Headaches,Vertex Headaches
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man

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