Cyclobenzaprine
- Atc Codes:M03BX08
- CAS Codes:6202-23-9#303-53-7
- PHARMGKB ID:6202-23-9#303-53-7
Table of contents
- Brand Names
- Drug Combinations
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Italy: Flexiban; Portugal: Flexiban; Spain: Yurelax.
North America
Canada: Cyclobenzaprine, Novo-Cycloprine, Riva-Cycloprine; USA: Amrix, Cyclobenzaprine, Flexeril.
Latin America
Brazil: Ciclobenzaprina, Miosan, Mirtax.
Drug combinations
Cyclobenzaprine and L-Lysine
Chemistry
Cyclobenzaprine Hydrochloride: C~20~H~21~N HCl. Mw: 311.85. (1) 1-Propanamine, 3-(5H-dibenzo[a,d]cyclohepten-5-ylidene)-N,N-dimethyl-, hydrochloride; (2) N,N-Dimethyl-5H-dibenzo[a,d]cycloheptene-Δ^5^,γ-propylamine hydrochloride. CAS-6202-23-9; CAS-303-53-7 (cyclobenzaprine)(1977).
Pharmacologic Category
Centrally Acting Skeletal Muscle Relaxants. (ATC-Code: M03BX08).
Mechanism of action
CNS depressant with sedative and skeletal muscle relaxant effects. Mechanism of action unknown. Does not directly relax skeletal muscle and does not depress neuronal conduction, neuromuscular transmission, or muscle excitability. Like tricyclic antidepressants, potentiates the effects of norepinephrine and has anticholinergic effects.
Therapeutic use
Muscle spasm associated with acute painful musculoskeletal conditions.
Pregnancy and lactiation implications
Teratogenic effects not observed in animal studies. There are no adequate studies in pregnant women. Use during pregnancy only if clearly needed. Excretion in breast milk unknown (use caution).
Unlabeled use
Contraindications
Hypersensitivity to cyclobenzaprine or any component of the formulation. Concomitant use or within 14 days of MAO inhibitors. Hyperthyroidism. Congestive heart failure, arrhythmias, heart block. Acute recovery phase of myocardic infarct.
Warnings and precautions
May cause CNS depression. Cyclobenzaprine shares the toxic potentials of tricyclic antidepressants (prolongation of conduction time, arrhythmias, tachycardia). Use with caution in angle-closure glaucoma or increased intraocular pressure. Use with caution in mild hepatic impairment (plasma concentrations increase; not recommended in moderate-to-severe hepatic impairment; extended release capsules not recommended in hepatic impairment of any severity). Use with caution in urinary hesitancy or retention. Do not use concomitantly with or within 14 days after MAO inhibitors (risk of hypertensive crisis and/or severe convulsions). Effects may be potentiated when used with other sedative drugs or ethanol. Use with caution in the elderly (higher risk of adverse reactions; extended release capsules not recommended for use in the elderly).