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| Mechanism of Action |
Cyclobenzaprine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Like other tricyclic antidepressants, cyclobenzaprine exhibits anticholinergic activity, potentiation of norepinephrine, and antagonism of reserpine. Cyclobenzaprine does not directly act on the neuromuscular junction or the muscle but relieves muscle spasms through a central action, possibly at the brain stem level. Cyclobenzaprine binds to the serotonin receptor and is considered a 5-HT2 receptor antagonist that reduces muscle tone by decreasing the activity of descending serotonergic neurons.
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| Pharmacology |
Cyclobenzaprine¿¡ ´ëÇÑ Pharmacology Á¤º¸ Cyclobenzaprine, closely related to the antidepressant amitriptyline, is used as a skeletal muscle relaxant to reduce pain and tenderness and improve mobility. Unlike dantrolene, cyclobenzaprine cannot be used to treat muscle spasm secondary to cerebral or spinal cord disease.
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| Metabolism |
Cyclobenzaprine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 1A2 (CYP1A2)
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| Protein Binding |
Cyclobenzaprine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ Very high (93%)
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| Half-life |
Cyclobenzaprine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 18 hours (range 8-37 hours)
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| Absorption |
Cyclobenzaprine¿¡ ´ëÇÑ Absorption Á¤º¸ Slowly but well absorbed after oral administration
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| Pharmacokinetics |
Cyclobenzaprine HClÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
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- Ç÷ÁßÃÖ°í³óµµ µµ´Þ½Ã°£ : 3-8 ½Ã°£ À̳»
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| Biotransformation |
Cyclobenzaprine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Extensively metabolized (gastrointestinal and hepatic).
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| Toxicity |
Cyclobenzaprine¿¡ ´ëÇÑ Toxicity Á¤º¸ Oral mouse and rat LD50 are 338 mg/kg and 425 mg/kg respectively. Signs of overdose include agitation, coma, confusion, congestive heart failure, convulsions, dilated pupils, disturbed concentration, drowsiness, hallucinations, high or low temperature, increased heartbeats, irregular heart rhythms, muscle stiffness, overactive reflexes, severe low blood pressure, stupor, and vomiting.
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| Drug Interactions |
Cyclobenzaprine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Donepezil Possible antagonism of actionGalantamine Possible antagonism of actionRasagiline Increased risk of toxicity with this associationRivastigmine Possible antagonism of action
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸] Cyclobenzaprine¿¡ ´ëÇÑ P450 table
SUBSTRATES
CYP 1A2
clozapine
**cyclobenzaprine**
imipramine
mexiletine
naproxen
riluzole
tacrine
theophylline
INHIBITORS
CYP 1A2
cimetidine
fluoroquinolones
fluvoxamine
ticlopidine
INDUCERS
CYP 1A2
tobacco
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| Food Interaction |
Cyclobenzaprine¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take with food to reduce irritation.Avoid alcohol.
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| Drug Target |
[Drug Target]
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| Description |
Cyclobenzaprine¿¡ ´ëÇÑ Description Á¤º¸ Cyclobenzaprine is a skeletal muscle relaxant and a central nervous system (CNS) depressant. Cyclobenzaprine acts on the locus coeruleus where it results in increased norepinephrine release, potentially through the gamma fibers which innervate and inhibit the alpha motor neurons in the ventral horn of the spinal cord. It is structurally similar to Amitriptyline, differing by only one double bond.
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| Dosage Form |
Cyclobenzaprine¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Tablet Oral
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| Drug Category |
Cyclobenzaprine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Antidepressive Agents, TricyclicMuscle RelaxantsMuscle Relaxants, CentralSkeletal Muscle RelaxantsTranquilizing Agents
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| Smiles String Canonical |
Cyclobenzaprine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CN(C)CCC=C1C2=CC=CC=C2C=CC2=CC=CC=C12
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| Smiles String Isomeric |
Cyclobenzaprine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CN(C)CC\C=C1/C2=CC=CC=C2C=CC2=CC=CC=C12
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| InChI Identifier |
Cyclobenzaprine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/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
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| Chemical IUPAC Name |
Cyclobenzaprine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 3-(5H-dibenzo[a,d]cyclohepten-5-ylidene)-N,N-dimethyl-1-propanamine
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