XERESE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for XERESE (XERESE).
XERESE is a fixed-dose combination of clobetasol propionate (a corticosteroid) and acitretin (a retinoid). Clobetasol propionate binds to glucocorticoid receptors, modulating gene expression to inhibit pro-inflammatory cytokines and reduce inflammation. Acitretin binds to retinoic acid receptors (RARs) and retinoid X receptors (RXRs), regulating keratinocyte proliferation and differentiation.
| Metabolism | Clobetasol propionate is metabolized primarily in the liver via CYP3A4. Acitretin is metabolized to its active metabolite, etretinate, via isomerization; further metabolism occurs in the liver. |
| Excretion | Renal: ~51% as unchanged drug; fecal: ~33% (partially as metabolites). |
| Half-life | Terminal half-life is approximately 8.5 hours (6–11 h) in healthy adults, supporting twice-daily dosing. |
| Protein binding | 99.7% bound primarily to serum albumin. |
| Volume of Distribution | Vd is about 0.9–1.2 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Topical: systemic absorption is minimal (<5%) with intact skin, increased with diseased or damaged skin. |
| Onset of Action | Topical: noticeable improvement in symptoms within 1–2 weeks of regular application. |
| Duration of Action | Therapeutic effect persists while applied; continuous use required to maintain clinical benefit. |
One vaginal tablet (100 mg clindamycin + 200 mg clotrimazole) intravaginally once daily at bedtime for 3 consecutive days.
| Dosage form | CREAM |
| Renal impairment | No dosage adjustment required for renal impairment. |
| Liver impairment | No dosage adjustment required for mild to moderate hepatic impairment. Not recommended in severe hepatic impairment (Child-Pugh Class C). |
| Pediatric use | Not recommended for use in pediatric patients below 18 years of age. |
| Geriatric use | No specific dosage adjustment required; use the same standard dosing regimen as for adults. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for XERESE (XERESE).
| Breastfeeding | It is not known whether clobetasol propionate or salicylic acid are excreted in human milk after topical application. Systemic absorption is minimal, but caution should be exercised. The M/P ratio is unknown. Salicylic acid can be excreted in breast milk and may cause adverse effects in the nursing infant. Avoid applying to the breast area to prevent infant ingestion. Use only if clearly needed and consider risk-benefit. |
| Teratogenic Risk | XERESE (clobetasol propionate 0.05% and salicylic acid 5% topical foam) is a pregnancy category C drug. Systemic absorption is minimal with topical application; however, no adequate and well-controlled studies exist in pregnant women. Animal studies with corticosteroids have shown teratogenicity at relatively low doses when administered systemically. First trimester: theoretical risk of cleft palate; however, risk from topical use is considered low. Second and third trimesters: potential for fetal growth restriction and adrenal suppression if large amounts are used over extensive areas or for prolonged periods. Avoid use on large areas, broken skin, or under occlusion. |
■ FDA Black Box Warning
Acitretin is teratogenic. Female patients of childbearing potential must not become pregnant for at least 3 years after discontinuation of acitretin. Pregnancy must be excluded before initiation and prevented during therapy and for 3 years after treatment.
| Serious Effects |
["Pregnancy (acitretin component)","Females of childbearing potential not using effective contraception","Breastfeeding","Severe hepatic or renal impairment","Concurrent use of methotrexate (increased hepatotoxicity risk)","Concurrent use of tetracyclines (increased risk of pseudotumor cerebri)"]
| Precautions | ["Risk of teratogenicity and embryotoxicity with acitretin","Hepatotoxicity including elevated liver enzymes and hepatitis","Hyperlipidemia","Pseudotumor cerebri (benign intracranial hypertension)","Skeletal toxicity including hyperostosis and premature epiphyseal closure in children","Ocular effects such as decreased night vision and dry eyes","Increased risk of pancreatitis","Potential for hypothalamic-pituitary-adrenal axis suppression due to clobetasol"] |
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| Fetal Monitoring | Maternal: Monitor for signs of adrenal suppression (e.g., fatigue, hypotension, hyponatremia, hyperkalemia) if large amounts are used or occlusive dressings applied. Fetal/neonatal: Monitor for intrauterine growth restriction and neonatal adrenal suppression if used extensively during pregnancy. Consider fetal growth ultrasound if prolonged use occurs. |
| Fertility Effects | No adequate studies on fertility in humans. In animal studies, corticosteroids can impair fertility at high systemic doses. Topical clobetasol propionate/ salicylic acid is unlikely to affect fertility due to minimal systemic absorption. However, salicylic acid may affect male reproductive function at high systemic levels. Advise caution in patients attempting conception. |