Flavoxate

JFDA label: Urispas Tab

Mechanism of Action

Synthetic antispasmotic with similar actions to that of propantheline; it exerts a direct relaxant effect on smooth muscles via phosphodiesterase inhibition, providing relief to a variety of smooth muscle spasms; it is especially useful for the treatment of bladder spasticity, whereby it produces an increase in urinary capacity

Indications

Off-label

• Polyuria
• Urinary Incontinence

Contraindications

Source: Lexicomp

• Pyloric or duodenal obstruction Absolute
• gastrointestinal hemorrhage Absolute
• obstructive intestinal lesions Absolute
• obstructive uropathies of lower urinary tract (eg, BPH) Absolute

Adverse Reactions

Cardiac disorders (2)

Not Known Palpitations · tachycardia

Nervous system disorders (6)

Not Known Confusion (especially in the elderly) · drowsiness · headache · hyperpyrexia · nervousness · vertigo

Renal and urinary disorders (1)

Not Known Dysuria

Blood and lymphatic system disorders (2)

Not Known Eosinophilia · leukopenia

Gastrointestinal disorders (3)

Not Known Nausea · vomiting · xerostomia

Skin and subcutaneous tissue disorders (2)

Not Known Rash · urticaria

Other (3)

Not Known Blurred vision · intraocular pressure increased · ocular accommodation disorder

Dosing

Source: Lexicomp

Warnings & Precautions

Source: Lexicomp

CNS effects

May cause CNS drowsiness and blurred vision, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving). Disease-related concerns:

Glaucoma

Use with caution in patients with suspected glaucoma. Concurrent drug therapy issues:

Sedatives

CNS effects may be potentiated when used with other sedative drugs or ethanol. Special populations:

Pregnancy & Lactation

Monitoring

Clinical pearl	Monitor I & O closely, anticholinergic signs and symptoms

Chemistry & Properties

Formula	C24H25NO4
Molecular weight	391.47 g/mol
IUPAC name	2-piperidin-1-ylethyl 3-methyl-4-oxo-2-phenylchromene-8-carboxylate
CAS	15301-69-6
PubChem CID	3354
InChIKey	SPIUTQOUKAMGCX-UHFFFAOYSA-N
logP	4.41 (XLogP 4.3)
Polar surface area	59.75 Ų
H-bond acceptors / donors	5 / 0
Drug-likeness (QED)	0.60
Lipinski violations	0

SMILES

Cc1c(-c2ccccc2)oc2c(C(=O)OCCN3CCCCC3)cccc2c1=O

Biology & Pharmacokinetics

Pharmacokinetics

BBB penetrant	No

Enzyme interactions

Enzyme	Role	Detail
CYP1A2	Inhibitor	—
CYP2B6	Inhibitor	—
CYP2C8	Inhibitor	—
CYP3A4	Substrate	—

Transporters

BCRP (Inhibitor)BCRP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)

Drug–drug interactions (74, DDInter)

Interacting drug	Severity	Management
Potassium chloride	major
Potassium citrate	major
Aclidinium	moderate
Acrivastine	moderate
Alimemazine	moderate
Atropine	moderate
Azatadine	moderate
Azelastine (nasal)	moderate
Brimonidine (ophthalmic)	moderate
Brimonidine (topical)	moderate
Brompheniramine	moderate
Carbinoxamine	moderate
Cetirizine	moderate
Chlorcyclizine	moderate
Chlorphenesin	moderate
Chlorpheniramine	moderate
Clemastine	moderate
Clidinium	moderate
Clofedanol	moderate
Codeine	moderate
Cyclizine	moderate
Cyproheptadine	moderate
Dexbrompheniramine	moderate
Dextromethorphan	moderate
Dicyclomine	moderate
Diphenhydramine	moderate
Doxepin	moderate
Doxepin (topical)	moderate
Doxylamine	moderate
Dronabinol	moderate
Edrophonium	moderate
Eluxadoline	moderate
Ethanol	moderate
Glycopyrronium	moderate
Glycopyrronium (topical)	moderate
Hydrocodone	moderate
Hyoscyamine	moderate
Ipratropium	moderate
Ketoconazole	moderate
Levocetirizine	moderate

Showing 40 of 74.

Registered Products (1)

Brand	Form / strength	Pack	Agent	Citizen (JOD)
Urispas Tab	Tablet 200 mg	30 tab	Adatco Drug Store	4.830