塩酸シクロベンザプリン

関: cyclobenzaprine

WordNet

a complex consisting of an organic base in association with hydrogen chloride
muscle relaxant (trade name Flexeril) used for muscle spasms or acute injury (同)Flexeril

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/05/10 03:09:55」(JST)

wiki en

Cyclobenzaprine, brand names Amrix, Flexeril and Fexmid, is a muscle relaxer medication used to relieve skeletal muscle spasms and associated pain in acute musculoskeletal conditions.^[3] It is the best-studied drug for this application.^[4] It has also been used off-label for fibromyalgia treatment.^[5] A new sublingual formulation of cyclobenzaprine is under development for the chronic management of fibromyalgia syndrome.^[6]

Medical use

After sustaining an injury, muscle spasms may occur to stabilize the affected body part and prevent further damage. They also generate pain. Cyclobenzaprine is FDA-approved to treat such muscle spasms associated with acute, painful musculoskeletal conditions.^[3] It decreases pain in the first two weeks,^[4]^[7] peaking in the first few days, but has no proven benefit after two weeks.^[4]^[8] Since no benefit is proven beyond that, therapy should not be continued long-term.^[9] It is not useful for spasticity due to neurologic conditions such as cerebral palsy.^[9]^[10]

Cyclobenzaprine has also shown effectiveness in the treatment of fibromyalgia symptoms, with a report of 4.8 patients needing treatment for each (1) patient reporting pain reduction (but no change in fatigue or tender points).^[11]

In elderly patients, cyclobenzaprine HCl may be started at a lower dose and titrated slowly upward. Cyclobenzaprine is recommended for use up to 3 weeks, but clinical efficacy has not been demonstrated beyond this point and long term use of cyclobenzaprine is not recommended.^[12] Cyclobenzaprine, however, has not been documented to cause intense physical and psychological withdrawal symptoms following discontinuation such as those which occur with its benzodiazepine, barbiturate, and carbamate alternatives, although the potential for rebound plasticity is of clinical relevance.

Side effects

Meta-analysis studies have found significantly increased rates of drowsiness (38% of patients), dry mouth (24%), dizziness (10%), and adverse events of any kind in patients taking cyclobenzaprine versus placebo.^[8] Drowsiness and dry mouth appear to intensify with increasing dose.^[13]

The sedative effects of cyclobenzaprine are likely due to its antagonistic effect on histamine, serotonin, and muscarinic receptors. Agitation is a common side effect observed especially in the elderly. In general, the NCQA recommends avoiding the use of cyclobenzaprine in the elderly because of the potential for more severe side effects.^[14] There is one case report of overdose causing rhabdomyolysis (muscle breakdown).^[15] Treatment protocols and support should follow the same as for any structurally related tricyclic, such as tricyclic antidepressants.^[15]

Overdose

The most common effects of overdose are drowsiness and tachycardia.^[3] Rare but potentially critical complications are cardiac arrest, cardiac dysrhythmias, severe hypotension, seizures, and neuroleptic malignant syndrome.^[3] Life-threatening overdose is rare,^[3] however, as the median lethal dose is approximately 338 mg/kg in mice and 425 mg/kg in rats.^[3] The potential harm is increased when central nervous system depressants and antidepressants are also used; deliberate overdose often includes alcohol among other drugs.^[3]

Interactions

Cyclobenzaprine has major contraindications with monoamine oxidase inhibitors (MAOIs). At least one study also found increased risk of serotonin syndrome when cyclobenzaprine was taken with the serotonergic drugs duloxetine or phenelzine.^[16]

The following substances may interact with cyclobenzaprine:

Alcohol
Central nervous system (CNS) depressants (e.g. opioids, benzodiazepines, nonbenzodiazepines, phenothiazines, carbamates, barbiturates)
Tricyclic antidepressants may increase the chance of side effects.
Monoamine oxidase inhibitors taken within two weeks of cyclobenzaprine may result in serious, life-threatening side effects.^[9]

If co-administered with opioids the dose of one or both medicines should be reduced accordingly. The patient should be monitored for excessive sedation.

Comparison to other medications

Cyclobenzaprine has been found to be non-inferior to tizanidine, orphenadrine, and carisoprodol in the treatment of acute lower back pain, although none have been proven to be effective for long term use (beyond two weeks of treatment). No differences in pain or spasm scores were noted among these agents, nor when compared to benzodiazepines.^[17] However, nonbenzodiazepine (including cyclobenzaprine) treatment was found to have a lower risk of medication abuse and continuation of use against medical advice. Side effects such as sedation and ataxia are also less pronounced with nonbenzodiazepine antispasmodics.

In a study on the treatment of musculoskeletal pain treatment with cyclobenzaprine alone or in combination with ibuprofen, no significant differences in pain scores were noted among the three treatment groups. Peak benefit was found to occur on day 7 of the treatment for all groups.^[18]

Formulations

Cyclobenzaprine 10mg

Orally, cyclobenzaprine is marketed as Apo-Cyclobenzaprin, Flexeril, Fexmid and Novo-Cycloprine. It is available in generic form. A once-a-day, extended-release formulation, Amrix, is available.^[19] Cyclobenzaprine is also used by compounding pharmacies in topical creams.

Cyclobenzaprine is regulated in the U.S. for prescription use only. Though it does not fall within most governmental guidelines as a controlled substance, possession of it without a valid or current prescription may be illegal, depending upon various state and local laws.

References

^ Micromedex® 2010 - DRUGDEX® Evaluations (Cyclobenzaprine Hydrochloride)
^ Cyclobenzaprine HCl Oral tablets USP Revised, April 2005
^ ^a ^b ^c ^d ^e ^f ^g "Flexeril (Cyclobenzaprine HCl) Tablets" (PDF). U. S. Food and Drug Administration. 2003. Retrieved 26 July 2009
^ ^a ^b ^c Chou R, Peterson K, Helfand M (2004). "Comparative efficacy and safety of skeletal muscle relaxants for spasticity and musculoskeletal conditions: a systematic review". Journal of Pain Symptom Management 28 (2): 140–175. doi:10.1016/j.jpainsymman.2004.05.002. PMID 15276195.
^ "Cyclobenzaprine Hydrochloride" (SUBSCRIPTION REQUIRED). MicroMedex. 5 Feb 2010. Retrieved 16 Feb 2010.
^ http://www.tonixpharma.com
^ van Tulder MW, Touray T, Furlan AD, Solway S, Bouter LM (2003). Van Tulder, Maurits W, ed. "Muscle relaxants for non-specific low back pain". Cochrane Database Systematic Reviews 2 (1–2): 91–9. doi:10.1002/14651858.CD004252. PMID 12804507.
^ ^a ^b Browning R, Jackson JL, O’Malley PG (2001). "Cyclobenzaprine and back pain: a meta-analysis". Archives of Internal Medicine 161 (13): 1613–1620. doi:10.1001/archinte.161.13.1613. PMID 11434793.
^ ^a ^b ^c "Cyclobenzaprine official FDA information, side effects, and uses". Drugs.com. October 2009. Retrieved 19 Feb 2010.
^ Ashby P, Burke D, Rao S et al. (1972). "Assessment of cyclobenzaprine in the treatment of spasticity". J Neurol Neurosurg Psychiatry 35 (5): 599–605. doi:10.1136/jnnp.35.5.599. PMC 494138. PMID 4563483.
^ Tofferi JK, Jackson JL, O'Malley PG (15 Feb 2004). "Treatment of fibromyalgia with cyclobenzaprine: A meta-analysis". Arthritis Rheum. 51 (1): 9–13. doi:10.1002/art.20076. PMID 14872449.
^ Cyclobenzaprine Information and Uses - RxWiki.com
^ "Flexeril: Side effects". RxList.com. Retrieved 22 Feb 2010.
^ "High risk medications" (PDF). National Committee for Quality Assurance. Retrieved 22 Feb 2010.
^ ^a ^b Chabria, Shiven B (17 July 2006). "Rhabdomyolysis: a manifestation of cyclobenzaprine toxicity". Journal of Occupational Medicine and Toxicology 1 (1): 16. doi:10.1186/1745-6673-1-16. PMC 1540431. PMID 16846511.
^ Keegan MT, Brown DR & Rabinstein AA (2006). "Serotonin syndrome from the interaction of cyclobenzaprine with other serotoninergic drugs". Anesthesia & Analgesia 103 (6): 1466–8. doi:10.1213/01.ane.0000247699.81580.eb. PMID 17122225.
^ http://www.medscape.com/viewarticle/572676_4. Missing or empty |title= (help)
^ http://www.annemergmed.com/article/S0196-0644(04)01009-1/abstract. Missing or empty |title= (help)
^ Amrix website

UpToDate Contents

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1. 成人における線維筋痛症の初期治療 initial treatment of fibromyalgia in adults
2. 急性腰痛の治療 treatment of acute low back pain
3. 頚部痛の治療 treatment of neck pain
4. 筋骨格系の胸痛の治療 treatment of musculoskeletal chest pain
5. 成人における初期治療の効果がない線維筋痛症の治療 treatment of fibromyalgia in adults not responsive to initial therapies

English Journal

Intranasal delivery of cyclobenzaprine hydrochloride-loaded thiolated chitosan nanoparticles for pain relief.

Patel D, Naik S, Chuttani K, Mathur R, Mishra AK, Misra A.SourceTIFAC CORE IN NDDS, Pharmacy Department, Faculty of Technology and Engineering, Kalabhavan, The Maharaja Sayajirao University of Baroda , Vadodara, Gujarat , India and.
Journal of drug targeting.J Drug Target.2013 Jul 24. [Epub ahead of print]
Abstract The purpose of present investigation was to formulate and characterize the cyclobenzaprine HCl (CBZ)-loaded thiolated chitosan nanoparticles and assessment of in-vitro cell viability, trans-mucosal permeability on RPMI2650 cell monolayer, in-vivo pharmacokinetic and pharmacodynamic study of
PMID 23879335

Risk of injury associated with skeletal muscle relaxant use in older adults.

Spence MM, Shin PJ, Lee EA, Gibbs NE.SourcePharmacy Outcomes Research Group, Kaiser Permanente, Downey, CA.
The Annals of pharmacotherapy.Ann Pharmacother.2013 Jul;47(7-8):993-8. doi: 10.1345/aph.1R735. Epub 2013 Jul 2.
BACKGROUND: The use of skeletal muscle relaxants (SMRs) among older adults is associated with sedation and confusion, which may lead to an increased risk of falls and injuries. SMRs continue to be used among older adults, although they are on the Beers list as drugs to avoid in the elderly.OBJECTIVE
PMID 23821610

Medications as a potential source of exposure to phthalates among women of childbearing age.

Hernández-Díaz S, Su YC, Mitchell AA, Kelley KE, Calafat AM, Hauser R.SourceDepartment of Epidemiology, Harvard School of Public Health, Boston, MA, USA.
Reproductive toxicology (Elmsford, N.Y.).Reprod Toxicol.2013 Jun;37:1-5. doi: 10.1016/j.reprotox.2013.01.001. Epub 2013 Jan 18.
OBJECTIVE: To evaluate the association between the use of medications potentially containing phthalates and urinary concentrations of specific phthalate metabolites around conception.METHODS: Women enrolled in the Environment and Reproductive Health project from 2006 to 2009 completed questionnaires
PMID 23333816

Japanese Journal

CAFC(連邦巡回控訴裁判所)最新判決ウォッチング(第153回)[EMC Corporation事件-Misc. Dkt. No. 100 (May 4, 2012), Bayer Schering Pharma AG対Lupin Ltd.事件-Nos. 2011-1143, -1228 (April 16, 2012), Cyclobenzaprine Hydrochloride Extended Release Capsule特許訴訟事件-Nos. 2011-1399, -1409 (April 16, 2012)]

チャルセンクリストファー・E,キャノムハンナ
The Lawyers 9(7), 48-52, 2012-07-00
NAID 40019381344

「シクロベンザプリン」

Cyclobenzaprine
Systematic (IUPAC) name
	3-(5H-dibenzo[a,d]cyclohepten-5-ylidene)- N,N-dimethyl-1-propanamine
Clinical data
Trade names	Amrix (former Flexeril)
AHFS/Drugs.com	monograph
MedlinePlus	a682514
Pregnancy; category	Category B;
Legal status	℞ (Prescription only);
Routes of; administration	Oral
Pharmacokinetic data
Bioavailability	33% to 55%
Metabolism	hepatic
Half-life	18 hours (range 8–37 hours; n=18)
Excretion	renal
Identifiers
CAS Registry Number	303-53-7
ATC code	M03BX08
PubChem	CID 2895
DrugBank	DB00924
ChemSpider	2792
UNII	69O5WQQ5TI
KEGG	D07758
ChEBI	CHEBI:3996
ChEMBL	CHEMBL669
Chemical data
Formula	C20H21N
Molecular mass	275.387 g/mol
	SMILES c3cc\2c(\C=C/c1c(cccc1)C/2=C/CCN(C)C)cc3;
	InChI InChI=1S/C20H21N/c1-21(2)15-7-12-20-18-10-5-3-8-16(18)13-14-17-9-4-6-11-19(17)20/h3-6,8-14H,7,15H2,1-2H3 ; Key:JURKNVYFZMSNLP-UHFFFAOYSA-N ;
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　　[★]

英: cyclobenzaprine、cyclobenzaprine hydrochloride
関: 塩酸シクロベンザプリン

「塩酸シクロベンザプリン」

　　[★]

英: cyclobenzaprine hydrochloride
関: シクロベンザプリン

「hydrochloride」

　　[★] 塩酸塩、ハイドロクロライド　

[1] Micromedex® 2010 - DRUGDEX® Evaluations (Cyclobenzaprine Hydrochloride)

[2] Cyclobenzaprine HCl Oral tablets USP Revised, April 2005

[FDA-3] ^ ^a ^b ^c ^d ^e ^f ^g "Flexeril (Cyclobenzaprine HCl) Tablets" (PDF). U. S. Food and Drug Administration. 2003. Retrieved 26 July 2009

[chou-4] Chou R, Peterson K, Helfand M (2004). "Comparative efficacy and safety of skeletal muscle relaxants for spasticity and musculoskeletal conditions: a systematic review". Journal of Pain Symptom Management 28 (2): 140–175. doi:10.1016/j.jpainsymman.2004.05.002. PMID 15276195.

[MicroMedex-5] "Cyclobenzaprine Hydrochloride" (SUBSCRIPTION REQUIRED). MicroMedex. 5 Feb 2010. Retrieved 16 Feb 2010.

[6] ttp://www.tonixpharma.com

[7] van Tulder MW, Touray T, Furlan AD, Solway S, Bouter LM (2003). Van Tulder, Maurits W, ed. "Muscle relaxants for non-specific low back pain". Cochrane Database Systematic Reviews 2 (1–2): 91–9. doi:10.1002/14651858.CD004252. PMID 12804507.

[browning-8] Browning R, Jackson JL, O’Malley PG (2001). "Cyclobenzaprine and back pain: a meta-analysis". Archives of Internal Medicine 161 (13): 1613–1620. doi:10.1001/archinte.161.13.1613. PMID 11434793.

[drugs.com-9] "Cyclobenzaprine official FDA information, side effects, and uses". Drugs.com. October 2009. Retrieved 19 Feb 2010.

[10] Ashby P, Burke D, Rao S et al. (1972). "Assessment of cyclobenzaprine in the treatment of spasticity". J Neurol Neurosurg Psychiatry 35 (5): 599–605. doi:10.1136/jnnp.35.5.599. PMC 494138. PMID 4563483.

[tofferi-11] Tofferi JK, Jackson JL, O'Malley PG (15 Feb 2004). "Treatment of fibromyalgia with cyclobenzaprine: A meta-analysis". Arthritis Rheum. 51 (1): 9–13. doi:10.1002/art.20076. PMID 14872449.

[12] Cyclobenzaprine Information and Uses - RxWiki.com

[rxlist-13] "Flexeril: Side effects". RxList.com. Retrieved 22 Feb 2010.

[14] "High risk medications" (PDF). National Committee for Quality Assurance. Retrieved 22 Feb 2010.

[chabria-15] Chabria, Shiven B (17 July 2006). "Rhabdomyolysis: a manifestation of cyclobenzaprine toxicity". Journal of Occupational Medicine and Toxicology 1 (1): 16. doi:10.1186/1745-6673-1-16. PMC 1540431. PMID 16846511.

[16] Keegan MT, Brown DR & Rabinstein AA (2006). "Serotonin syndrome from the interaction of cyclobenzaprine with other serotoninergic drugs". Anesthesia & Analgesia 103 (6): 1466–8. doi:10.1213/01.ane.0000247699.81580.eb. PMID 17122225.

[17] ttp://www.medscape.com/viewarticle/572676_4. Missing or empty |title= (help)

[18] ttp://www.annemergmed.com/article/S0196-0644(04)01009-1/abstract. Missing or empty |title= (help)

[19] Amrix website

リンク元	「シクロベンザプリン」「塩酸シクロベンザプリン」
関連記事	「hydrochloride」

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cyclobenzaprine hydrochloride