Sofdra (sofpironium bromide)
Topical Anticholinergic Hyperhidrosis Treatment Agents Topical Gel With Pump (Ml)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Sofpironium, a quaternary ammonium analogue of glycopyrrolate, is an anticholinergic drug.
Sofpironium is a quaternary ammonium analogue of the anticholinergic agent glycopyrrolate.
Sofpironium competitively binds to M3 muscarinic receptors, the main receptor type on axillary sweat glands, preventing activation from acetylcholine. Without receptor stimulation, the glands will not receive the signal to secrete sweat, decreasing overall sweating.
Following topical application of sofpironium in adults with primary axillary hyperhidrosis, mean time to peak plasma concentration was 5.34 hours. Sofpironium exhibits plasma protein binding of 34.8-37.8%, while its major metabolite, BBI-4010, binds at 2.3-3.7%. Sofpironium is primarily metabolized through nonenzymatic hydrolysis, cytochrome P-450 (CYP) 2D6 and CYP3A4 oxidative pathways, and glycine conjugation, with minimal urinary excretion (<0.5%).
After metabolism, sofpironium remained the predominant plasma component at 38%, followed by BBI-4010 at 20%. In pediatric patients 9-16 years of age, mean time to peak plasma concentrations of sofpironium was 4 hours and there was no evidence of drug accumulation after 24 weeks of daily dosing. Pharmacokinetics have not been studied in pregnant patients or those with renal or hepatic impairment.
USES: Sofpironium is used to treat excessive sweating from your underarms. It works on the sweat glands to reduce sweating. Sofpironium belongs to a class of drugs known as anticholinergics.
Generic name: sofpironium bromide
Pronunciation: (SOF-pir-OH-nee-um)
Drug class: Topical Anticholinergic Hyperhidrosis Treatment Agents
Therapeutic class: Dermatological
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Sofdra
Indications
The following indications are listed for Sofdra:
- Primary Focal Hyperhidrosis Of Axilla
Also known as: Primary Axillary Hyperhidrosis.
Dosing
Dosage of sofpironium bromide is expressed in terms of sofpironium.
Administer sofpironium topically. Sofpironium bromide is available as a topical gel that contains 12.45% of sofpironium in a 50 mL bottle with a metered pump; each full pump delivers 72 mg in 0.67 mL of gel.
Apply sofpironium gel to clean, dry, unshaven underarms (do not shave within 8 hours or shower within 30 minutes prior). Dispense one pump onto the supplied applicator and apply to one underarm, spreading to cover entire underarm area; repeat with a separate pump for the other underarm. Allow to dry for 5 minutes before dressing. Wash hands with soap immediately after use. Do not touch underarms after applying. Do not wash or shower for at least 8 hours after application. Do not apply to broken skin or use with occlusive dressings. Avoid contact with the eyes and avoid fires, flames, or smoking during and shortly after application.
Store sofpironium gel upright at 20-25degreesC (excursions permitted between 15-30degreesC). Keep away from heat or flame, as the product is flammable.
| Drug label | Dosing type | Instructions |
|---|---|---|
| Sofdra 12.45% Gel | Maintenance | Apply 1 pump (72 mg) to each underarm by topical route once daily at bedtime. |
No dosing information is available for this tab.
Drug interactions
Sofpironium is metabolized by cytochrome P-450 (CYP) 2D6 and CYP3A4. The drug inhibits CYP2D6, CYP3A4, organic cation transporter (OCT)1 and OCT2, and multidrug and toxin extrusion protein (MATE)1, but does not induce CYP1A2, CYP2B6, or CYP3A4.
Contraindicated Drug Combination: This drug combination is contraindicated and generally should not be dispensed or administered to the same patient.
Sofpironium/Strong Cyp2d6 Inhibitors
SEVERITY LEVEL: 1-Contraindicated Drug Combination: This drug combination is contraindicated and generally should not be dispensed or administered to the same patient.
MECHANISM OF ACTION: Strong inhibitors of CYP2D6 may inhibit the metabolism of sofpironium.(1)
CLINICAL EFFECTS: Concurrent use of strong CYP2D6 inhibitors may result in elevated levels and adverse effects of sofpironium, including increased risk of anticholinergic side effects.
PREDISPOSING FACTORS: None determined.
PATIENT MANAGEMENT: The concurrent use of sofpironium and strong CYP2D6 inhibitors should be avoided.(1) If concurrent therapy is warranted with a strong CYP2D6 inhibitor, monitor patients closely for anticholinergic side effects.
DISCUSSION: In a drug interaction study in healthy subjects, coadministration of paroxetine (a strong CYP2D6 inhibitor) with sofpironium increased the maximum concentration (Cmax) and area-under-the-curve (AUC) by approximately 2-fold compared to sofpironium administration alone.(1) Strong CYP2D6 inhibitors linked to this monograph include bupropion, dacomitinib, fluoxetine, paroxetine, quinidine, and terbinafine.(2,3)
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Patients with conditions worsened by anticholinergic effects, such as glaucoma, paralytic ileus, unstable cardiovascular status in acute hemorrhage, severe or complicating ulcerative colitis, toxic megacolon, myasthenia gravis, and Sjogren's syndrome.
- Glaucoma
- Myasthenia gravis
- Paralytic ileus
- Shock
- Sjogren's syndrome
- Toxic megacolon
- Benign prostatic hyperplasia
- Ulcerative colitis
- Urinary retention
There are no moderate contraindications for this drug.
Adverse reactions
The most common adverse reactions (incidence >=2%) reported with sofpironium gel in clinical studies were dry mouth, blurred vision, mydriasis, urinary retention, and application site pain, erythema, dermatitis pruritus, and irritation.
There are no severe adverse reactions for this drug.
More Frequent
- Acute pain at drug application site
- Blurred vision
- Dermatitis due to topical drug
- Erythema
- Mydriasis
- Skin irritation
- Urinary retention
- Xerostomia
Less Frequent
- Dry eye
- Dry skin
- Exfoliative dermatitis
- Folliculitis
- Headache disorder
- Hypertension
- Influenza
- Pain
- Pruritus of skin
- Skin rash
- Upper respiratory infection
Precautions
No enhanced messaging available.
The safety, effectiveness, and pharmacokinetics of sofpironium have been established in pediatric patients >=9 years of age, based on data from 2 randomized controlled trials and 2 long-term, open-label studies involving 72 children.
There are no human data on sofpironium use in pregnancy; animal studies showed no adverse effects at doses 10-31 times the maximum recommended human dose, but the risk of birth defects or miscarriage in humans remains unknown.
There are no data on sofpironium in human milk or its effects on infants or milk production. Administration of a subcutaneous dose of sofpironium to lactating rats resulted in detectable drug levels in their milk. The benefits of breastfeeding should be weighed against the mother's clinical need and potential risks.
Clinical trials of sofpironium included too few patients >=65 years of age to assess age-related differences, though no differences have been reported; dosing in elderly patients should be cautious due to potential declines in organ function, presence of comorbidities, and use of concurrent therapies.
ICD codes
| Code | Type | Description |
|---|---|---|
| Primary focal hyperhidrosis of axilla | ||
| L74.510 | ICD10CM | Primary focal hyperhidrosis, axilla |
ICD code information from First Databank (FDB).
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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