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Development Status

US Approved Rx

2

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Primary Target

Aldehyde oxidase

2

Cytochrome P450 1A2

2

Cytochrome P450 2D6

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Cytochrome P450 3A4

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Serotonin 2 (5-HT2) receptor

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Highest Phase

Approved

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Approval Year

1977

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Condition

Acute, painful musculoskeletal conditions

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Treatment Modality

Palliative

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CNS Activity

CNS Active

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Originator

Hoffman-La Roche

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Chemical

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CAS

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CHEBI

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ChEMBL

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DAILYMED

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DRUG BANK

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ATC Level 1

MUSCULO-SKELETAL SYSTEM

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ATC Level 2

MUSCLE RELAXANTS

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ATC Level 3

MUSCLE RELAXANTS, CENTRALLY ACTING AGENTS

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ATC Level 4

Other centrally acting agents

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Substance Form

Principal Form

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CYCLOBENZAPRINE

69O5WQQ5TI

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Status:

US Approved Rx (1995)

First approved in 1977

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Cytochrome P450 2D6

Aldehyde oxidase

Cytochrome P450 1A2

Serotonin 2 (5-HT2) receptor

Cytochrome P450 3A4

Conditions:

Acute, painful musculoskeletal conditions

Cyclobenzaprine is a centrally-acting muscle relaxant which boosts levels of norepinephrine and binds to serotonin receptors in the brain to reduce spasm. Cytochromes P-450 3A4, 1A2, and, to a lesser extent, 2D6, mediate N-demethylation, one of the o...

xidative pathways for cyclobenzaprine. Cyclobenzaprine relieves skeletal muscle spasm of local origin without interfering with muscle function. Drowsiness, fatigue and sedation (up to 40%) is the most common side effect of Cyclobenzaprine. It may have life-threatening interactions with monoamine oxidase (MAO) inhibitors. Postmarketing cases of serotonin syndrome have been reported during combined use of cyclobenzaprine and other drugs such as selective serotonin reuptake inhibitors (SSRIs), serotonin norepinephrine reuptake inhibitors (SNRIs), tricyclic antidepressants (TCAs), tramadol, bupropion, meperidine, verapamil, or MAO inhibitors.

CYCLOBENZAPRINE HYDROCHLORIDE

0VE05JYS2P

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Search for Structure

Status:

US Approved Rx (1995)

First approved in 1977

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Cytochrome P450 2D6

Aldehyde oxidase

Cytochrome P450 1A2

Serotonin 2 (5-HT2) receptor

Cytochrome P450 3A4

Conditions:

Acute, painful musculoskeletal conditions

Cyclobenzaprine is a centrally-acting muscle relaxant which boosts levels of norepinephrine and binds to serotonin receptors in the brain to reduce spasm. Cytochromes P-450 3A4, 1A2, and, to a lesser extent, 2D6, mediate N-demethylation, one of the o...

xidative pathways for cyclobenzaprine. Cyclobenzaprine relieves skeletal muscle spasm of local origin without interfering with muscle function. Drowsiness, fatigue and sedation (up to 40%) is the most common side effect of Cyclobenzaprine. It may have life-threatening interactions with monoamine oxidase (MAO) inhibitors. Postmarketing cases of serotonin syndrome have been reported during combined use of cyclobenzaprine and other drugs such as selective serotonin reuptake inhibitors (SSRIs), serotonin norepinephrine reuptake inhibitors (SNRIs), tricyclic antidepressants (TCAs), tramadol, bupropion, meperidine, verapamil, or MAO inhibitors.

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