OXSORALEN-ULTRA

Clinical safety rating: caution

Comprehensive clinical and safety monograph for OXSORALEN-ULTRA (OXSORALEN-ULTRA).

How it works

Oxsoralen-Ultra (methoxsalen) is a psoralen derivative that, upon photoactivation by UVA radiation, forms covalent cross-links with DNA, thereby inhibiting DNA synthesis and cell division. It also suppresses cutaneous immune responses and reduces epidermal cell turnover.

What the body does with it

Metabolism	Oxsoralen-ULTRA undergoes extensive hepatic metabolism via cytochrome P450 enzymes (primarily CYP1A2 and CYP2A6). It is rapidly absorbed and has a half-life of approximately 2 hours. Excretion is primarily renal as metabolites.
Excretion	Primarily renal: 90-95% as metabolites within 24 hours; minimal biliary/fecal (<5%).
Half-life	2 hours (terminal) with clinical context: elimination is rapid; no accumulation with q3-5d dosing.
Protein binding	99% bound to albumin.
Volume of Distribution	Vd ~0.5 L/kg; indicates distribution into total body water with minimal tissue binding.
Bioavailability	Oral: well absorbed, bioavailability >80%.
Onset of Action	Oral: 2-4 hours to reach peak photosensitization.
Duration of Action	Oral: Photosensitivity lasts 8-12 hours; avoid UV/sun exposure for at least 24 hours.

Classification & Brands

Dosing & administration

0.6 mg/kg orally as a single dose 2 hours prior to PUVA therapy, administered 3 times per week on non-consecutive days.

Dosage form	CAPSULE
Renal impairment	No specific guidelines; use with caution in severe renal impairment (CrCl <30 mL/min) due to potential increased toxicity.
Liver impairment	Contraindicated in severe hepatic impairment (Child-Pugh class C). For moderate impairment (Child-Pugh class B), reduce dose by 50% and monitor liver function.
Pediatric use	Not recommended in children under 12 years due to lack of safety data. For children 12-18 years: 0.6 mg/kg orally 2 hours before PUVA, same frequency as adults.
Geriatric use	Start at low end of dosing range (0.4-0.6 mg/kg) and monitor for increased photosensitivity and renal function decline.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for OXSORALEN-ULTRA (OXSORALEN-ULTRA).

Breastfeeding	No data on excretion in human milk; M/P ratio unknown. Due to potential for serious adverse reactions in nursing infants, discontinue nursing or discontinue drug, considering importance to mother.
Teratogenic Risk	Pregnancy category C. First trimester: potential teratogenic effects based on animal studies; avoid use. Second/third trimesters: insufficient human data; use only if benefit outweighs risk. Fetal risks include possible phototoxic reactions and potential for DNA damage.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

WARNING: Squamous cell carcinoma (SCC) and other skin cancers have been reported in patients treated with PUVA therapy. The risk is dose- and time-dependent, and increases with higher cumulative UVA exposure. Patients should be monitored for skin malignancies throughout treatment.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Albinsim or congenital photosensitivity","History of melanoma or invasive squamous cell carcinoma","Pregnancy (category C) and lactation","Concurrent use of photosensitizing drugs (e.g., tetracyclines, thiazides, sulfonamides)","Severe hepatic or renal impairment","Aphakia"]

Clinical Precautions

Precautions

["Risk of severe burns if sun exposure occurs within 24 hours of treatment","Increased risk of cataracts; protective eyewear required during UVA exposure and for 24 hours thereafter","Photosensitivity reactions may be severe; avoid concomitant photosensitizing drugs","Hepatotoxicity has been reported; monitor liver function tests","Avoid in patients with prior history of skin cancer or radiation therapy"]

Clinical Tips & Counseling

Drug interactions

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OXSORALEN-ULTRA

Clinical safety rating: caution

Comprehensive clinical and safety monograph for OXSORALEN-ULTRA (OXSORALEN-ULTRA).

How it works

What the body does with it

Metabolism	Oxsoralen-ULTRA undergoes extensive hepatic metabolism via cytochrome P450 enzymes (primarily CYP1A2 and CYP2A6). It is rapidly absorbed and has a half-life of approximately 2 hours. Excretion is primarily renal as metabolites.
Excretion	Primarily renal: 90-95% as metabolites within 24 hours; minimal biliary/fecal (<5%).
Half-life	2 hours (terminal) with clinical context: elimination is rapid; no accumulation with q3-5d dosing.
Protein binding	99% bound to albumin.
Volume of Distribution	Vd ~0.5 L/kg; indicates distribution into total body water with minimal tissue binding.
Bioavailability	Oral: well absorbed, bioavailability >80%.
Onset of Action	Oral: 2-4 hours to reach peak photosensitization.
Duration of Action	Oral: Photosensitivity lasts 8-12 hours; avoid UV/sun exposure for at least 24 hours.

Classification & Brands

Dosing & administration

0.6 mg/kg orally as a single dose 2 hours prior to PUVA therapy, administered 3 times per week on non-consecutive days.

Dosage form	CAPSULE
Renal impairment	No specific guidelines; use with caution in severe renal impairment (CrCl <30 mL/min) due to potential increased toxicity.
Liver impairment	Contraindicated in severe hepatic impairment (Child-Pugh class C). For moderate impairment (Child-Pugh class B), reduce dose by 50% and monitor liver function.
Pediatric use	Not recommended in children under 12 years due to lack of safety data. For children 12-18 years: 0.6 mg/kg orally 2 hours before PUVA, same frequency as adults.
Geriatric use	Start at low end of dosing range (0.4-0.6 mg/kg) and monitor for increased photosensitivity and renal function decline.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for OXSORALEN-ULTRA (OXSORALEN-ULTRA).

Breastfeeding	No data on excretion in human milk; M/P ratio unknown. Due to potential for serious adverse reactions in nursing infants, discontinue nursing or discontinue drug, considering importance to mother.
Teratogenic Risk	Pregnancy category C. First trimester: potential teratogenic effects based on animal studies; avoid use. Second/third trimesters: insufficient human data; use only if benefit outweighs risk. Fetal risks include possible phototoxic reactions and potential for DNA damage.
Fetal Monitoring