Calcitriol (Topical)

Pronunciation

(kal si TRYE ole)

Index Terms

• 1,25 Dihydroxycholecalciferol

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Ointment, External:

Vectical: 3 mcg/g (100 g)

Generic: 3 mcg/g (100 g)

Brand Names: U.S.

• Vectical

Pharmacologic Category

• Vitamin D Analog

Pharmacology

The mechanism by which calcitriol is beneficial in the treatment of psoriasis has not been established.

Absorption

Oral: Rapid

Metabolism

Primarily to calcitroic acid and a lactone metabolite

Excretion

Excretion: Feces (27%); urine (7%, unchanged in 24 hours)

Clearance: Children 1.8 to 16 years undergoing peritoneal dialysis: 15.3 mL/hour/kg

Time to Peak

Oral: 3 to 6 hours; Hemodialysis: 8 to 12 hours

Duration of Action

Oral, IV: 3 to 5 days

Half-Life Elimination

Children 1.8-16 years undergoing peritoneal dialysis: 27.4 hours; Healthy adults: 5 to 8 hours; Hemodialysis: 16 to 22 hours

Protein Binding

99.9%

Use: Labeled Indications

Plaque psoriasis: Management of mild-to-moderate plaque psoriasis

Contraindications

U.S. labeling: There are no contraindications listed in the manufacturer's labeling.

Canadian labeling: Ophthalmic or internal use; hypercalcemia or a history of abnormal calcium metabolism; concurrent systemic treatment of calcium homeostasis; severe renal impairment or end-stage renal disease (ESRD)

Dosing: Adult

Psoriasis: Topical: Apply twice daily to affected areas (maximum: 200 g weekly); Canadian labeling recommends maximum of 30 g daily

Dosing: Renal Impairment

There are no dosage adjustments provided in the manufacturer’s labeling. However, the Canadian labeling does not recommend use in patients with renal impairment.

Dosing: Hepatic Impairment

There are no dosage adjustments provided in the manufacturer’s labeling. However, the Canadian labeling does not recommend use in patients with reduced hepatic function.

Administration

Topical: Apply externally; not for ophthalmic, oral, or intravaginal use. Do not apply to eyes, lips, or facial skins. Rub in gently so that no medication remains visible. Limit application to only the areas of skin affected by psoriasis.

Storage

Store at room temperature of 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F); do not refrigerate; do not freeze.

Drug Interactions

Aluminum Hydroxide: Vitamin D Analogs may increase the serum concentration of Aluminum Hydroxide. Specifically, the absorption of aluminum may be increased, leading to increased serum aluminum concentrations. Avoid combination

Aminolevulinic Acid: Photosensitizing Agents may enhance the photosensitizing effect of Aminolevulinic Acid. Monitor therapy

Bile Acid Sequestrants: May decrease the serum concentration of Vitamin D Analogs. More specifically, bile acid sequestrants may impair absorption of Vitamin D Analogs. Management: Avoid concomitant administration of vitamin D analogs and bile acid sequestrants (e.g., cholestyramine). Separate administration of these agents by several hours to minimize the potential risk of interaction. Monitor plasma calcium concentrations. Consider therapy modification

Calcium Salts: May enhance the adverse/toxic effect of Vitamin D Analogs. Monitor therapy

Cardiac Glycosides: Vitamin D Analogs may enhance the arrhythmogenic effect of Cardiac Glycosides. Monitor therapy

Danazol: May enhance the hypercalcemic effect of Vitamin D Analogs. Monitor therapy

Mineral Oil: May decrease the serum concentration of Vitamin D Analogs. More specifically, mineral oil may interfere with the absorption of Vitamin D Analogs. Management: Avoid concomitant, oral administration of mineral oil and vitamin D analogs. Consider separating the administration of these agents by several hours to minimize the risk of interaction. Monitor plasma calcium concentrations. Consider therapy modification

Multivitamins/Fluoride (with ADE): May enhance the adverse/toxic effect of Vitamin D Analogs. Avoid combination

Multivitamins/Minerals (with ADEK, Folate, Iron): May enhance the adverse/toxic effect of Vitamin D Analogs. Avoid combination

Orlistat: May decrease the serum concentration of Vitamin D Analogs. More specifically, orlistat may impair absorption of Vitamin D Analogs. Management: Monitor clinical response (including serum calcium) to oral vitamin D analogs closely if used with orlistat. If this combination must be used, consider giving the vitamin D analog at least 2 hrs before or after orlistat. Consider therapy modification

Porfimer: Photosensitizing Agents may enhance the photosensitizing effect of Porfimer. Monitor therapy

Sucralfate: Vitamin D Analogs may increase the serum concentration of Sucralfate. Specifically, the absorption of aluminum from sucralfate may be increased, leading to an increase in the serum aluminum concentration. Avoid combination

Thiazide and Thiazide-Like Diuretics: May enhance the hypercalcemic effect of Vitamin D Analogs. Monitor therapy

Verteporfin: Photosensitizing Agents may enhance the photosensitizing effect of Verteporfin. Monitor therapy

Vitamin D Analogs: May enhance the adverse/toxic effect of other Vitamin D Analogs. Avoid combination

Adverse Reactions

>10%: Endocrine: Hypercalcemia (24%)

1% to 10%:

Dermatologic: Psoriasis (4%), pruritus (1% to 3%), skin discomfort

Genitourinary: Urine abnormality (4%), hypercalciuria (3%)

<1%, postmarketing, and/or case reports: Burning sensation of skin, dermatitis (acute; blistering), eczema (including extensive flare up), erythema, nephrolithiasis, skin atrophy

Warnings/Precautions

Concerns related to adverse effects:

• Hypercalcemia: May cause hypercalcemia; if alterations in calcium occur, discontinue treatment until levels return to normal.

Disease-related concerns:

• Hepatic impairment: Canadian labeling does not recommend use in patients with hepatic impairment.

• Renal impairment: Canadian labeling does not recommend use in patients with mild to moderate renal impairment.

Other warnings/precautions:

• Appropriate use: For external use only; not for ophthalmic, oral, or intravaginal use. Do not apply to facial skin, eyes, or lips. Absorption may be increased with occlusive dressings. Avoid or limit excessive exposure to natural or artificial sunlight, or phototherapy. The safety and effectiveness has not been evaluated in patients with erythrodermic, exfoliative, or pustular psoriasis.

Pregnancy Risk Factor

C

Pregnancy Considerations

Adverse effects have been observed in some animal reproduction studies. When treatment for psoriasis in pregnancy is needed, the use of other agents is generally preferred (Babalola 2013; Bae 2012).

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience itching. Have patient report immediately to prescriber signs of high calcium (weakness, confusion, fatigue, headache, nausea and vomiting, constipation, or bone pain) or severe skin irritation (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.