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|Methoxsalen |
Drugs search, click the first letter of a drug name: | A | B | C | D | E | F | G | H | I | J | K | L | M | N | O | P | Q | R | S | T | U | V | W | X | Y | Z | 1 | 2 | 3 | 4 | 5 | 6 | 8 | 9 Home MethoxsalenPronouncation: (meth-OX-ah-len)Class: Psoralen Trade Names: Trade Names: Trade Names: Trade Names: Mechanism of ActionPharmacologyExact mechanism not known; however, methoxsalen acts as a photosensitizer. PharmacokineticsAbsorption8-MOPMax bioavailability is reached 1.5 to 3 hr after oral administration and lasts up to 8 hr. Oxsoralen-UltraReaches peak blood drug levels in 0.5 to 4 hr, and detectable levels are observed up to 12 hr. DistributionMethoxsalen is reversibly bound to serum albumin and preferentially taken up by epidermal cells. MetabolismMethoxsalen is rapidly metabolized. EliminationApproximately 95% is excreted as a series of metabolites in the urine within 24 hr. Oxsoralen-UltraThe t ½ is approximately 2 hr. DurationOxsoralen-UltraTime of peak photosensitivity is 1.5 to 2.1 hr. Indications and UsageSymptomatic control of severe, recalcitrant, disabling psoriasis not responsive to other forms of therapy and when diagnosis supported by biopsy ( Oxsoralen-Ultra , 8-MOP capsule); use in conjunction with long wave UV radiation for repigmentation of idiopathic vitiligo ( 8-MOP capsule, Oxsoralen lotion); with long wave UV radiation of white blood cells (photopheresis) with the UVAR Photopheresis System in the palliative treatment of skin manifestations of cutaneous T-cell lymphoma in people not responsive to other forms of treatment ( 8-MOP capsule, Oxsoralen lotion); extracorporeal administration with UVAR Photopheresis System in the palliative treatment of skin manifestation of cutaneous T-cell lymphoma that is unresponsive to other forms of treatment ( Uvadex solution). ContraindicationsPatients exhibiting idiosyncratic reactions to psoralen compounds; specific history of light-sensitive disease states should not initiate methoxsalen therapy (eg, lupus erythematosus, porphyria cutanea tarda, erythropoietic protoporphyria, variegate porphyria, xeroderma pigmentosum, albinism); patients exhibiting melanoma or possessing a history of melanoma; patients exhibiting invasive squamous cell carcinomas; patients with aphakia, because of increased risk of retinal damage caused by absence of lenses. Dosage and AdministrationVitiligoAdults 8-MOP PO Take 20 mg daily in 1 dose with milk or food 2 to 4 hr prior to UV exposure. Take on alternate days and never on 2 consecutive days. Sun exposure is based on basic skin color. Initial sun exposure should be 15 min for light skin, 20 min for medium-colored skin, and 25 min for dark skin. The second, third, and fourth exposures may be increased by 5 min/each exposure (if basic skin color is light, the second exposure can be increased to 20 min, the third exposure to 25 min, and the fourth exposure to 30 min). Subsequent exposures may gradually be increased based on erythema and tenderness of amelanotic skin (max, 0.6 mg/kg). Oxsoralen lotionApply lotion to a small, well-defined, vitiliginous lesion, then expose this area to UVA light. Initial exposure time must not exceed one half the minimal erythema dose. Regulate treatment intervals by erythema response (once weekly or less, depending on the results). Pigmentation may begin after a few weeks; significant repigmentation may take up to 6 to 9 mo. Periodic treatment may be needed to retain the new pigmentation. PsoriasisAdults Oxsoralen-Ultra PO Take with food or milk 1.5 to 2 hr prior to UVA exposure. 8-MOPPO Take with food or milk 2 hr prior to UVA exposure. Take according to the following recommendations: Generally, elderly patients should be started at the low end of the dose recommended according to body weight and closely monitored during PUVA therapy. No treatments should be given more often than once every other day because the full extent of phototoxic reactions may not be evident until 48 hr after each exposure. Dosage may be increased by 10 mg after the fifteenth treatment. Patients weighing:
Adults Uvadex Extracorporeal with the UVAR Photopheresis System only. (Not for parenteral administration.) Normal treatment schedule: Treatment is given on 2 consecutive days q 4 wk for a minimum of 7 treatment cycles (6 mo). Accelerated treatment schedule: If assessment of the patient during the fourth treatment cycle (approximately 3 mo) reveals an increased skin score from the baseline score, the frequency of treatment may be increased to 2 consecutive treatments q 2 wk. If a 25% improvement in the skin score is attained after 4 consecutive wk, the regular treatment schedule may be resumed (max, 20 cycles). Consult UVAR Photopheresis System Operator"s Manual before using this product. Treatment involves collection of leukocytes, photoactivation, and reinfusion of photoactivated cells. During each photopheresis treatment, 200 mcg (10 mL) of Uvadex is injected directly into photoactivation bag during the first buffy coat collection cycle. At the end of 6 cycles, a total of 740 mL (240 mL of buffy coat, 300 mL of plasma, and 200 mL of normal saline priming fluid) is collected and mixed with the 200 mcg of Uvadex present in the photoactivation bag. After photoactivation, the cells are reinfused. Storage/StabilityStore at controlled room temperature (59° to 86°F). Drug InteractionsKnown photosensitizers (eg, anthralin, coal tar, coal tar derivatives, fluoroquinolone antibiotics, griseofulvin, halogenated salicylanilides, nalidixic acid, organic staining dyes [eg, methylene blue, methyl orange, rose bengal, toluidine blue], phenothiazines, sulfonamides, tetracyclines, thiazide diuretics)Exercise care when using these agents and methoxsalen concurrently. Laboratory Test InteractionsNone well documented. Adverse ReactionsCardiovascular8-MOP , Oxsoralen-UltraHypotension. UvadexHypotension (secondary to extracorporeal volume [greater than 1%]). CNS8-MOP , Oxsoralen-UltraDizziness; headache, malaise, depression. Dermatologic8-MOP , Oxsoralen-UltraPruritus (10%); erythema; hypopigmentation; vesiculation and bullae formation; nonspecific rash; urticaria; folliculitis; cutaneous tenderness; extension of psoriasis. GI8-MOP , Oxsoralen-UltraNausea (10%); GI disturbances. Miscellaneous8-MOP , Oxsoralen-UltraEdema; herpes simplex; miliaria; leg cramps. UvadexInfection. Precautions
PregnancyCategory C ( 8-MOP , Oxsoralen-Ultra ); Category D ( Uvadex ). LactationUndetermined. ChildrenSafety and efficacy not established. ElderlyUse with caution, start at low end of dosing range. Hepatic FunctionBecause hepatic biotransformation is necessary for drug urinary excretion, use with caution. CarcinogenesisRisk of squamous cell carcinoma among PUVA-treated patients is increased (especially in patients who are fair-skinned or have had pre-PUVA exposure to prolonged tar and UVB treatment) ionizing radiation, or arsenic. Risk of basal cell carcinoma may also be increased. Special Risk PatientsDiligently observe and treat patients with basal cell carcinoma or a history of basal cell carcinoma; diligently observe patients with a history of previous x-ray therapy, grenz ray therapy, or arsenic therapy for signs of carcinoma; patients with cardiac disease or others who may be unable to tolerate prolonged standing or exposure to heat stress should not be treated in a vertical UVA chamber. Actinic degenerationExposure to sunlight and/or UV radiation may result in premature aging of the skin. CataractBecause the concentration of methoxsalen in the lens is proportional to the serum level, if the lens is exposed to UVA while methoxsalen is present, photochemical action may lead to irreversible binding of the methoxsalen to proteins and DNA components of the lens. SunbathingThe presence of sunburn may prevent the accurate evaluation of the patient"s response to photochemotherapy. Total dosageTotal cumulative dose of UVA that can be given safely over long periods of time has not been established. Patient Information
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