The Experts below are selected from a list of 300 Experts worldwide ranked by ideXlab platform
Mona Darwish - One of the best experts on this subject based on the ideXlab platform.
-
steady state pharmacokinetics of once daily Cyclobenzaprine extended release a randomized double blind 2 period crossover study in healthy volunteers
Clinical Therapeutics, 2011Co-Authors: Mona Darwish, Edward T. HellriegelAbstract:Abstract Background The single-dose pharmacokinetic profile of Cyclobenzaprine extended-release (CER) has been previously characterized and compared with the pharmacokinetics of Cyclobenzaprine immediate-release (CIR) administered 3 times daily for 3 doses. Objective The objective of this study was to characterize the multiple-dose pharmacokinetic properties of once-daily CER 30 mg and CIR 10 mg TID formulations in healthy volunteers. Methods In this double-blind, single-center, 2-period crossover study, healthy subjects were randomized to dosing sequences with once-daily CER 30 mg or CIR 10 mg TID for 7 days. Subjects crossed over to the alternative regimen following a 14-day washout period. Pharmacokinetic assessments at steady state included area under the plasma Cyclobenzaprine concentration–time curve over the dosing interval (AUC 0–τ,ss ), peak plasma Cyclobenzaprine concentration (C max,ss ), time to observed C max (T max,ss ), observed minimum Cyclobenzaprine concentration (C min,ss ), average Cyclobenzaprine concentration (C avg,ss ), accumulation ratio (R ac ), and terminal elimination half-life (t ½ ). Tolerability and safety assessments were conducted. Results A total of 36 subjects were randomized; 34 completed both dosing periods (1 subject was lost to follow-up, 1 withdrew consent). Steady state was reached for CER 30 mg on day 7. Mean C max,ss , C min,ss , and C avg,ss were 41.1, 21.4, and 31.4 ng/mL, respectively. The median T max,ss for CER 30 mg was 7.0 hours, with a mean t ½ of 34.8 hours. At steady state, CER produced a sustained plasma Cyclobenzaprine concentration with a single peak in plasma concentration during the 24-hour dose interval. The R ac for CER was 2.65. Because of a protocol violation (insufficient data), no steady-state pharmacokinetic assessments could be performed for CIR. Most adverse events were mild or moderate in intensity. Somnolence was the most frequently reported adverse event (100% of subjects) in those receiving CER, followed by dry mouth (58%), dizziness (19%), and headache (17%). Conclusions Once-daily CER 30 mg delivered sustained plasma Cyclobenzaprine levels over 24 hours at steady state. Owing to a protocol violation, steady-state pharmacokinetic properties for CIR could not be assessed.
-
Steady-State Pharmacokinetics of Once-Daily Cyclobenzaprine Extended Release: A Randomized, Double-Blind, 2-Period Crossover Study in Healthy Volunteers
Clinical Therapeutics, 2011Co-Authors: Mona Darwish, Edward T. HellriegelAbstract:Background: The single-dose pharmacokinetic profile of Cyclobenzaprine extended-release (CER) has been previously characterized and compared with the pharmacokinetics of Cyclobenzaprine immediate-release (CIR) administered 3 times daily for 3 doses. Objective: The objective of this study was to characterize the multiple-dose pharmacokinetic properties of once-daily CER 30 mg and CIR 10 mg TID formulations in healthy volunteers. Methods: In this double-blind, single-center, 2-period crossover study, healthy subjects were randomized to dosing sequences with once-daily CER 30 mg or CIR 10 mg TID for 7 days. Subjects crossed over to the alternative regimen following a 14-day washout period. Pharmacokinetic assessments at steady state included area under the plasma Cyclobenzaprine concentration-time curve over the dosing interval (AUC0-??,ss), peak plasma Cyclobenzaprine concentration (Cmax,ss), time to observed Cmax (Tmax,ss), observed minimum Cyclobenzaprine concentration (Cmin,ss), average Cyclobenzaprine concentration (Cavg,ss), accumulation ratio (Rac), and terminal elimination half-life (t??). Tolerability and safety assessments were conducted. Results: A total of 36 subjects were randomized; 34 completed both dosing periods (1 subject was lost to follow-up, 1 withdrew consent). Steady state was reached for CER 30 mg on day 7. Mean Cmax,ss, Cmin,ss, and Cavg,ss were 41.1, 21.4, and 31.4 ng/mL, respectively. The median Tmax,ss for CER 30 mg was 7.0 hours, with a mean t?? of 34.8 hours. At steady state, CER produced a sustained plasma Cyclobenzaprine concentration with a single peak in plasma concentration during the 24-hour dose interval. The Rac for CER was 2.65. Because of a protocol violation (insufficient data), no steady-state pharmacokinetic assessments could be performed for CIR. Most adverse events were mild or moderate in intensity. Somnolence was the most frequently reported adverse event (100% of subjects) in those receiving CER, followed by dry mouth (58%), dizziness (19%), and headache (17%). Conclusions: Once-daily CER 30 mg delivered sustained plasma Cyclobenzaprine levels over 24 hours at steady state. Owing to a protocol violation, steady-state pharmacokinetic properties for CIR could not be assessed. ?? 2011 Elsevier HS Journals, Inc.
-
pharmacokinetic profile of once daily Cyclobenzaprine extended release
Expert Opinion on Drug Metabolism & Toxicology, 2010Co-Authors: Mona Darwish, Edward T. HellriegelAbstract:Importance of the field: Cyclobenzaprine immediate-release (CIR) is a widely prescribed skeletal muscle relaxant with an established efficacy and safety profile in patients with muscle spasm associated with acute, painful conditions, although it is commonly associated with sedation. CIR is typically prescribed at a dosage of 10 mg three-times-daily. This review focuses on the pharmacokinetic profile of a new formulation, Cyclobenzaprine extended-release (CER), which delivers a sustained plasma Cyclobenzaprine concentration over 24 h, allowing once-daily dosing. Areas covered in this review: Results from CER pharmacokinetic studies conducted through August 2010 are summarized. What the reader will gain: This review provides information on the first four studies assessing the single-dose and steady-state pharmacokinetic profile of CER. Take home message: Once-daily CER 30 mg and three-times-daily CIR 10 mg produced comparable systemic exposures to Cyclobenzaprine, but pharmacokinetic profiles were qualitati...
-
Pharmacokinetic profile of once-daily Cyclobenzaprine extended-release
Expert Opinion on Drug Metabolism & Toxicology, 2010Co-Authors: Mona Darwish, Edward T. HellriegelAbstract:IMPORTANCE OF THE FIELD: Cyclobenzaprine immediate-release (CIR) is a widely prescribed skeletal muscle relaxant with an established efficacy and safety profile in patients with muscle spasm associated with acute, painful conditions, although it is commonly associated with sedation. CIR is typically prescribed at a dosage of 10 mg three-times-daily. This review focuses on the pharmacokinetic profile of a new formulation, Cyclobenzaprine extended-release (CER), which delivers a sustained plasma Cyclobenzaprine concentration over 24 h, allowing once-daily dosing. AREAS COVERED IN THIS REVIEW: Results from CER pharmacokinetic studies conducted through August 2010 are summarized. WHAT THE READER WILL GAIN: This review provides information on the first four studies assessing the single-dose and steady-state pharmacokinetic profile of CER. TAKE HOME MESSAGE: Once-daily CER 30 mg and three-times-daily CIR 10 mg produced comparable systemic exposures to Cyclobenzaprine, but pharmacokinetic profiles were qualitatively different. CER was characterized by a single daily peak in Cyclobenzaprine concentration versus three peaks/day for CIR. With once-daily dosing of CER, Cyclobenzaprine concentration is sustained over 24 h. CER 30 mg provides approximately twice the exposure as CER 15 mg. Systemic exposure to CER is increased in the presence of food and in elderly subjects. Steady-state is achieved by day 7 of dosing.
-
Comparison of the Single-Dose Pharmacokinetics of Once-Daily Cyclobenzaprine Extended-Release 30 mg and Cyclobenzaprine Immediate-Release 10 mg Three Times Daily in the Elderly
Drugs & Aging, 2009Co-Authors: Mona DarwishAbstract:Background and objective: The clinical utility of Cyclobenzaprine for the treatment of muscle spasm associated with acute, painful musculoskeletal conditions is limited by cholinergic adverse effects associated with its use. As expected, these effects may be pronounced in the elderly in whom altered renal and hepatic function may change drug pharmacokinetics. The goal of this study was to characterize the pharmacokinetics of the extended-release formulation of Cyclobenzaprine (CER) in elderly volunteers. Methods: This randomized, open-label, two-period crossover study compared the pharmacokinetics, safety and tolerability of a single oral 30-mg dose of CER with those of 10 mg of Cyclobenzaprine immediate-release (CIR) administered every 8 hours for a total of three doses in 18 healthy volunteers aged 65–75 years. Volunteers were assigned to either CER or CIR on days 1 and 15 (separated by a 14-day washout). Outcome measures included area under the plasma Cyclobenzaprine concentration versus time curve (AUC) to 168 hours (AUC_168) and infinity (AUC_∞), peak plasma Cyclobenzaprine concentration (C_max), time to observed C_max (t_max) and terminal elimination half-life of Cyclobenzaprine. Adverse events (AEs) were monitored during the study through 3 weeks after the last dose of study drug. Results: Eighteen subjects were randomized and completed the first treatment period; 17 completed both periods of the study. The pharmacokinetics of CER 30 mg were characterized by an absorption phase with a median tmax of 8 hours compared with an initial peak for CIR (following the first dose) at about 5 hours. Plasma Cyclobenzaprine concentrations at 5 hours were 13.6 ng/mL for CER and 11.0 ng/mL for CIR. Systemic Cyclobenzaprine exposure (AUC_168, AUC_∞ and C_max) was similar for a single dose of CER and three doses of CIR and met bioequivalence criteria. Most AEs were mild in intensity; the most common AE was somnolence. No serious AEs or discontinuations as a result of AEs were reported during the study. Conclusion: Once-daily CER 30 mg exhibited controlled release of Cyclobenzaprine and resulted in systemic exposure similar to that of CIR in subjects aged 65–75 years.
Edward T. Hellriegel - One of the best experts on this subject based on the ideXlab platform.
-
steady state pharmacokinetics of once daily Cyclobenzaprine extended release a randomized double blind 2 period crossover study in healthy volunteers
Clinical Therapeutics, 2011Co-Authors: Mona Darwish, Edward T. HellriegelAbstract:Abstract Background The single-dose pharmacokinetic profile of Cyclobenzaprine extended-release (CER) has been previously characterized and compared with the pharmacokinetics of Cyclobenzaprine immediate-release (CIR) administered 3 times daily for 3 doses. Objective The objective of this study was to characterize the multiple-dose pharmacokinetic properties of once-daily CER 30 mg and CIR 10 mg TID formulations in healthy volunteers. Methods In this double-blind, single-center, 2-period crossover study, healthy subjects were randomized to dosing sequences with once-daily CER 30 mg or CIR 10 mg TID for 7 days. Subjects crossed over to the alternative regimen following a 14-day washout period. Pharmacokinetic assessments at steady state included area under the plasma Cyclobenzaprine concentration–time curve over the dosing interval (AUC 0–τ,ss ), peak plasma Cyclobenzaprine concentration (C max,ss ), time to observed C max (T max,ss ), observed minimum Cyclobenzaprine concentration (C min,ss ), average Cyclobenzaprine concentration (C avg,ss ), accumulation ratio (R ac ), and terminal elimination half-life (t ½ ). Tolerability and safety assessments were conducted. Results A total of 36 subjects were randomized; 34 completed both dosing periods (1 subject was lost to follow-up, 1 withdrew consent). Steady state was reached for CER 30 mg on day 7. Mean C max,ss , C min,ss , and C avg,ss were 41.1, 21.4, and 31.4 ng/mL, respectively. The median T max,ss for CER 30 mg was 7.0 hours, with a mean t ½ of 34.8 hours. At steady state, CER produced a sustained plasma Cyclobenzaprine concentration with a single peak in plasma concentration during the 24-hour dose interval. The R ac for CER was 2.65. Because of a protocol violation (insufficient data), no steady-state pharmacokinetic assessments could be performed for CIR. Most adverse events were mild or moderate in intensity. Somnolence was the most frequently reported adverse event (100% of subjects) in those receiving CER, followed by dry mouth (58%), dizziness (19%), and headache (17%). Conclusions Once-daily CER 30 mg delivered sustained plasma Cyclobenzaprine levels over 24 hours at steady state. Owing to a protocol violation, steady-state pharmacokinetic properties for CIR could not be assessed.
-
Steady-State Pharmacokinetics of Once-Daily Cyclobenzaprine Extended Release: A Randomized, Double-Blind, 2-Period Crossover Study in Healthy Volunteers
Clinical Therapeutics, 2011Co-Authors: Mona Darwish, Edward T. HellriegelAbstract:Background: The single-dose pharmacokinetic profile of Cyclobenzaprine extended-release (CER) has been previously characterized and compared with the pharmacokinetics of Cyclobenzaprine immediate-release (CIR) administered 3 times daily for 3 doses. Objective: The objective of this study was to characterize the multiple-dose pharmacokinetic properties of once-daily CER 30 mg and CIR 10 mg TID formulations in healthy volunteers. Methods: In this double-blind, single-center, 2-period crossover study, healthy subjects were randomized to dosing sequences with once-daily CER 30 mg or CIR 10 mg TID for 7 days. Subjects crossed over to the alternative regimen following a 14-day washout period. Pharmacokinetic assessments at steady state included area under the plasma Cyclobenzaprine concentration-time curve over the dosing interval (AUC0-??,ss), peak plasma Cyclobenzaprine concentration (Cmax,ss), time to observed Cmax (Tmax,ss), observed minimum Cyclobenzaprine concentration (Cmin,ss), average Cyclobenzaprine concentration (Cavg,ss), accumulation ratio (Rac), and terminal elimination half-life (t??). Tolerability and safety assessments were conducted. Results: A total of 36 subjects were randomized; 34 completed both dosing periods (1 subject was lost to follow-up, 1 withdrew consent). Steady state was reached for CER 30 mg on day 7. Mean Cmax,ss, Cmin,ss, and Cavg,ss were 41.1, 21.4, and 31.4 ng/mL, respectively. The median Tmax,ss for CER 30 mg was 7.0 hours, with a mean t?? of 34.8 hours. At steady state, CER produced a sustained plasma Cyclobenzaprine concentration with a single peak in plasma concentration during the 24-hour dose interval. The Rac for CER was 2.65. Because of a protocol violation (insufficient data), no steady-state pharmacokinetic assessments could be performed for CIR. Most adverse events were mild or moderate in intensity. Somnolence was the most frequently reported adverse event (100% of subjects) in those receiving CER, followed by dry mouth (58%), dizziness (19%), and headache (17%). Conclusions: Once-daily CER 30 mg delivered sustained plasma Cyclobenzaprine levels over 24 hours at steady state. Owing to a protocol violation, steady-state pharmacokinetic properties for CIR could not be assessed. ?? 2011 Elsevier HS Journals, Inc.
-
pharmacokinetic profile of once daily Cyclobenzaprine extended release
Expert Opinion on Drug Metabolism & Toxicology, 2010Co-Authors: Mona Darwish, Edward T. HellriegelAbstract:Importance of the field: Cyclobenzaprine immediate-release (CIR) is a widely prescribed skeletal muscle relaxant with an established efficacy and safety profile in patients with muscle spasm associated with acute, painful conditions, although it is commonly associated with sedation. CIR is typically prescribed at a dosage of 10 mg three-times-daily. This review focuses on the pharmacokinetic profile of a new formulation, Cyclobenzaprine extended-release (CER), which delivers a sustained plasma Cyclobenzaprine concentration over 24 h, allowing once-daily dosing. Areas covered in this review: Results from CER pharmacokinetic studies conducted through August 2010 are summarized. What the reader will gain: This review provides information on the first four studies assessing the single-dose and steady-state pharmacokinetic profile of CER. Take home message: Once-daily CER 30 mg and three-times-daily CIR 10 mg produced comparable systemic exposures to Cyclobenzaprine, but pharmacokinetic profiles were qualitati...
-
Pharmacokinetic profile of once-daily Cyclobenzaprine extended-release
Expert Opinion on Drug Metabolism & Toxicology, 2010Co-Authors: Mona Darwish, Edward T. HellriegelAbstract:IMPORTANCE OF THE FIELD: Cyclobenzaprine immediate-release (CIR) is a widely prescribed skeletal muscle relaxant with an established efficacy and safety profile in patients with muscle spasm associated with acute, painful conditions, although it is commonly associated with sedation. CIR is typically prescribed at a dosage of 10 mg three-times-daily. This review focuses on the pharmacokinetic profile of a new formulation, Cyclobenzaprine extended-release (CER), which delivers a sustained plasma Cyclobenzaprine concentration over 24 h, allowing once-daily dosing. AREAS COVERED IN THIS REVIEW: Results from CER pharmacokinetic studies conducted through August 2010 are summarized. WHAT THE READER WILL GAIN: This review provides information on the first four studies assessing the single-dose and steady-state pharmacokinetic profile of CER. TAKE HOME MESSAGE: Once-daily CER 30 mg and three-times-daily CIR 10 mg produced comparable systemic exposures to Cyclobenzaprine, but pharmacokinetic profiles were qualitatively different. CER was characterized by a single daily peak in Cyclobenzaprine concentration versus three peaks/day for CIR. With once-daily dosing of CER, Cyclobenzaprine concentration is sustained over 24 h. CER 30 mg provides approximately twice the exposure as CER 15 mg. Systemic exposure to CER is increased in the presence of food and in elderly subjects. Steady-state is achieved by day 7 of dosing.
-
A pharmacokinetic comparison of single doses of once-daily Cyclobenzaprine extended-release 15 mg and 30 mg: A randomized, double-blind, two-period crossover study in healthy volunteers
Clinical Therapeutics, 2009Co-Authors: Mona Darwish, Steven Chang, Edward T. HellriegelAbstract:Objective: The purpose of this study was to compare the pharmacokinetics and tolerability of single oral doses of Cyclobenzaprine extended-release (CER) 15- and 30-mg capsules. Methods: This was a randomized, double-blind, 2-period crossover study in healthy adults aged 18 to 40 years. Subjects were assigned to receive a single dose of either CER 15 mg or 30 mg on days 1 and 15, separated by a 14-day washout. Study comparisons included the plasma Cyclobenzaprine AUC to 168 hours after dosing (AUC0-168), AUC0-???, and Cmax. Plasma Cyclobenzaprine Tmax, terminal elimination t1/2, and adverse events (AEs) were also assessed. Results: Sixteen subjects (9 women, 7 men) were randomized to receive Cyclobenzaprine 15 mg or 30 mg; 13 (81.3%) were white and 3 (18.8%) were black. Mean age and weight were 30.2 years and 70.7 kg, respectively. The shapes of the pharmacokinetic profiles for CER 15 and 30 mg were parallel. Mean observed values for dose-dependent pharmacokinetic parameters of CER 15 and 30 mg were as follows: AUC0-168, 318.3 and 736.6 ng ?? h/mL, respectively; AUC0-???), 354.1 and 779.9 ng ?? h/mL; and Cmax, 8.3 and 19.9 ng/mL. Dose-independent parameters were comparable across doses. Median observed Tmax was 6.0 hours for both CER doses; mean t1/2 was 33.4 hours for CER 15 mg and 32.0 hours for CER 30 mg. The bioavailability of the 2 doses, as indicated by the least squares mean AUC0-???, was 330.3 ng ?? h/mL for CER 15 mg and 755.1 ng ?? h/mL for CER 30 mg. During the CER 15-mg treatment sequence, 5 subjects experienced 5 AEs (headache, dizziness, musculoskeletal pain, dermatitis, and glossodynia); during the CER 30-mg treatment sequence, 2 subjects experienced 2 AEs (somnolence and dysmenorrhea). All AEs were mild in intensity. No serious AEs occurred during the study. Conclusions: Once-daily CER 15 and 30 mg exhibited similarly shaped pharmacokinetic profiles. AUC0-168, AUC0-???), and Cmax values for the 30-mg dose were approximately double those for the 15-mg dose, a result consistent with previously reported data on the dose proportionality of Cyclobenzaprine immediate release. ?? 2009 Excerpta Medica Inc. All rights reserved.
Hideki Ono - One of the best experts on this subject based on the ideXlab platform.
-
Tricyclic analogs Cyclobenzaprine, amitriptyline and cyproheptadine inhibit the spinal reflex transmission through 5-HT2 receptors
European Journal of Pharmacology, 2003Co-Authors: Motoko Honda, Takashi Nishida, Hideki OnoAbstract:The centrally acting muscle relaxant Cyclobenzaprine decreases the amplitude of monosynaptic reflex potentials by inhibiting the facilitatory descending serotonergic influences in the spinal cord. Interestingly, the structure of Cyclobenzaprine is much similar to those of amitriptyline and cyproheptadine. In the present study, we attempted to elucidate the relationship between 5-HT2 receptor antagonistic and inhibitory effects of Cyclobenzaprine, amitriptyline, cyproheptadine and ketanserin on the spinal reflexes. Cyclobenzaprine, amitriptyline, cyproheptadine, and ketanserin significantly inhibited facilitatory effects of 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) on flexor reflexes and mono- and polysynaptic spinal reflex potentials in spinalized rats. In intact rats, these drugs significantly reduced the mono- and polysynaptic reflex potentials. 5-HT depletion significantly prevented the depression of the spinal reflex potentials induced by these drugs. These results suggest that the inhibitory effects of Cyclobenzaprine, amitriptyline, and cyproheptadine on mono- and polysynaptic reflex potentials are due to the inhibition of descending serotonergic systems through 5-HT2 receptors in the spinal cord. ?? 2002 Elsevier Science B.V. All rights reserved.
-
Cyclobenzaprine, a centrally acting muscle relaxant, acts on descending serotonergic systems
European Journal of Pharmacology, 1996Co-Authors: Hiroyuki Kobayashi, Yutaka Hasegawa, Hideki OnoAbstract:The centrally acting muscle relaxant Cyclobenzaprine was thought to be an ??2-adrenoceptor agonist that reduced muscle tone by decreasing the activity of descending noradrenergic neurons. In the present study, we examined the effects of Cyclobenzaprine on descending neurons by measuring the monosynaptic reflex in rats. Cyclobenzaprine reduced the monosynaptic reflex amplitude dose dependently and this effect was not inhibited by the ??-adrenoceptor antagonists idazoxan and yohimbine. Cyclobenzaprine-induced monosynaptic reflex depression was not attenuated by noradrenergic neuronal lesions produced by B-hydroxydopamine. However, Cyclobenzaprine inhibited monosynaptic reflex facilitation induced by (??)-1-(4-iodo-2,5-dimethoxyphenyl)-2-aminopropane, a 5-HT2 receptor agonist, in spinalized rats markedly, and 5-HT depletion by DL-p-chlorophenylalanine inhibited the depressive effect of Cyclobenzaprine on the monosynaptic reflex. These results suggest that Cyclobenzaprine is a 5-HT2 receptor antagonist and that its muscle relaxant effect is due to inhibition of serotonergic, not noradrenergic, descending systems in the spinal cord.
Crystal A. Kunka - One of the best experts on this subject based on the ideXlab platform.
-
treatment of levator ani syndrome with Cyclobenzaprine
Annals of Pharmacotherapy, 2012Co-Authors: Maheen Sheikh, Crystal A. KunkaAbstract:Objective To report a case of levator ani syndrome (LAS) that was successfully treated with Cyclobenzaprine. Case summary A 26-year-old male presented with a 3-week history of severe, intermittent, aching anorectal pain that would last for 30-60 minutes per episode and occurred between 1 and 3 times per day. The pain was aggravated by squatting, with no alleviating factors. Physical examination revealed no prostate tenderness, lesions, hemorrhoids, or fissures and rectal tone was intact. The patient had moderate posterior rectal tenderness. After a standard workup, he was diagnosed with LAS and treated with oral Cyclobenzaprine 5 mg 3 times daily for 7 days. The patient experienced resolution of his symptoms after 3 days of treatment and remained symptom-free 6 months after completion of therapy. The only reported adverse effect was mild drowsiness, which resolved after discontinuation of the Cyclobenzaprine. Discussion A review of the literature via StatRef (April 1965-December 2011), Ovid (April 1965-December 2011), and MEDLINE (April 1965-December 2011) reveals that existing treatment options for LAS have been limited to levator massage, sitz baths, nonsteroidal antiinflammatory drugs, diazepam, biofeed-back, botulinum toxin, steroid injections, and electrogalvanic stimulation, all of which offer minimal support. Cyclobenzaprine is a muscle relaxant; however, its mechanism of action is unclear. It is thought to influence the α and γ motor neurons in the central nervous system, which leads to the attenuation of muscle spasm. To our knowledge, Cyclobenzaprine has not been reported as a treatment for LAS. In our patient, however, the clinical efficacy of Cyclobenzaprine was clearly apparent. Conclusions Cyclobenzaprine effectively treated our patient's LAS. Given that Cyclobenzaprine is safe, inexpensive, and shown to be effective in our case study, we believe it warrants further investigation as a first-line treatment option for LAS.
-
Treatment of levator ani syndrome with Cyclobenzaprine
Annals of Pharmacotherapy, 2012Co-Authors: Maheen Sheikh, Crystal A. Kunka, Ken S. OtaAbstract:OBJECTIVE: To report a case of levator ani syndrome (LAS) that was successfully treated with Cyclobenzaprine. CASE SUMMARY: A 26-year-old male presented with a 3-week history of severe, intermittent, aching anorectal pain that would last for 30-60 minutes per episode and occurred between 1 and 3 times per day. The pain was aggravated by squatting, with no alleviating factors. Physical examination revealed no prostate tenderness, lesions, hemorrhoids, or fissures and rectal tone was intact. The patient had moderate posterior rectal tenderness. After a standard workup, he was diagnosed with LAS and treated with oral Cyclobenzaprine 5 mg 3 times daily for 7 days. The patient experienced resolution of his symptoms after 3 days of treatment and remained symptom-free 6 months after completion of therapy. The only reported adverse effect was mild drowsiness, which resolved after discontinuation of the Cyclobenzaprine. DISCUSSION: A review of the literature via StatRef (April 1965-December 2011), Ovid (April 1965-December 2011), and MEDLINE (April 1965-December 2011) reveals that existing treatment options for LAS have been limited to levator massage, sitz baths, nonsteroidal antiinflammatory drugs, diazepam, biofeed-back, botulinum toxin, steroid injections, and electrogalvanic stimulation, all of which offer minimal support. Cyclobenzaprine is a muscle relaxant; however, its mechanism of action is unclear. It is thought to influence the alpha and gamma motor neurons in the central nervous system, which leads to the attenuation of muscle spasm. To our knowledge, Cyclobenzaprine has not been reported as a treatment for LAS. In our patient, however, the clinical efficacy of Cyclobenzaprine was clearly apparent. CONCLUSIONS: Cyclobenzaprine effectively treated our patient's LAS. Given that Cyclobenzaprine is safe, inexpensive, and shown to be effective in our case study, we believe it warrants further investigation as a first-line treatment option for LAS.
Maheen Sheikh - One of the best experts on this subject based on the ideXlab platform.
-
treatment of levator ani syndrome with Cyclobenzaprine
Annals of Pharmacotherapy, 2012Co-Authors: Maheen Sheikh, Crystal A. KunkaAbstract:Objective To report a case of levator ani syndrome (LAS) that was successfully treated with Cyclobenzaprine. Case summary A 26-year-old male presented with a 3-week history of severe, intermittent, aching anorectal pain that would last for 30-60 minutes per episode and occurred between 1 and 3 times per day. The pain was aggravated by squatting, with no alleviating factors. Physical examination revealed no prostate tenderness, lesions, hemorrhoids, or fissures and rectal tone was intact. The patient had moderate posterior rectal tenderness. After a standard workup, he was diagnosed with LAS and treated with oral Cyclobenzaprine 5 mg 3 times daily for 7 days. The patient experienced resolution of his symptoms after 3 days of treatment and remained symptom-free 6 months after completion of therapy. The only reported adverse effect was mild drowsiness, which resolved after discontinuation of the Cyclobenzaprine. Discussion A review of the literature via StatRef (April 1965-December 2011), Ovid (April 1965-December 2011), and MEDLINE (April 1965-December 2011) reveals that existing treatment options for LAS have been limited to levator massage, sitz baths, nonsteroidal antiinflammatory drugs, diazepam, biofeed-back, botulinum toxin, steroid injections, and electrogalvanic stimulation, all of which offer minimal support. Cyclobenzaprine is a muscle relaxant; however, its mechanism of action is unclear. It is thought to influence the α and γ motor neurons in the central nervous system, which leads to the attenuation of muscle spasm. To our knowledge, Cyclobenzaprine has not been reported as a treatment for LAS. In our patient, however, the clinical efficacy of Cyclobenzaprine was clearly apparent. Conclusions Cyclobenzaprine effectively treated our patient's LAS. Given that Cyclobenzaprine is safe, inexpensive, and shown to be effective in our case study, we believe it warrants further investigation as a first-line treatment option for LAS.
-
Treatment of levator ani syndrome with Cyclobenzaprine
Annals of Pharmacotherapy, 2012Co-Authors: Maheen Sheikh, Crystal A. Kunka, Ken S. OtaAbstract:OBJECTIVE: To report a case of levator ani syndrome (LAS) that was successfully treated with Cyclobenzaprine. CASE SUMMARY: A 26-year-old male presented with a 3-week history of severe, intermittent, aching anorectal pain that would last for 30-60 minutes per episode and occurred between 1 and 3 times per day. The pain was aggravated by squatting, with no alleviating factors. Physical examination revealed no prostate tenderness, lesions, hemorrhoids, or fissures and rectal tone was intact. The patient had moderate posterior rectal tenderness. After a standard workup, he was diagnosed with LAS and treated with oral Cyclobenzaprine 5 mg 3 times daily for 7 days. The patient experienced resolution of his symptoms after 3 days of treatment and remained symptom-free 6 months after completion of therapy. The only reported adverse effect was mild drowsiness, which resolved after discontinuation of the Cyclobenzaprine. DISCUSSION: A review of the literature via StatRef (April 1965-December 2011), Ovid (April 1965-December 2011), and MEDLINE (April 1965-December 2011) reveals that existing treatment options for LAS have been limited to levator massage, sitz baths, nonsteroidal antiinflammatory drugs, diazepam, biofeed-back, botulinum toxin, steroid injections, and electrogalvanic stimulation, all of which offer minimal support. Cyclobenzaprine is a muscle relaxant; however, its mechanism of action is unclear. It is thought to influence the alpha and gamma motor neurons in the central nervous system, which leads to the attenuation of muscle spasm. To our knowledge, Cyclobenzaprine has not been reported as a treatment for LAS. In our patient, however, the clinical efficacy of Cyclobenzaprine was clearly apparent. CONCLUSIONS: Cyclobenzaprine effectively treated our patient's LAS. Given that Cyclobenzaprine is safe, inexpensive, and shown to be effective in our case study, we believe it warrants further investigation as a first-line treatment option for LAS.
