ETRETINATE
(e-tret'i-nate)
Tegison
Classifications: skin and mucous membrane agent; antipsoriatic; retinoid
Prototype: Isotretinoin
Pregnancy Category: X
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10 mg, 25 mg capsules
Second-generation retinoid related to retinoic acid and retinol (vitamin A). Mechanism of action unknown.
Reduces redness, scaling, and thickness of psoriasis lesions by normalizing epidermal differentiation; also decreases stratum
corneum thickness and inflammation in epidermis and dermis.
Treatment of severe recalcitrant psoriasis in patients unresponsive to or intolerant of standard therapies.
Intolerance to isotretinoin, tretinoin, vitamin A derivatives, or to parabens (preservative in etretinate formulation); severe
obesity; pregnancy (category X), lactation.
Cardiovascular disease or family history of; children (used only if all alternative therapies have been ineffective); hepatic
impairment; diabetes mellitus, patients predisposed to hypertriglyceridemia.
Psoriasis
Adult: PO 0.75–1 mg/kg/d in divided doses (max: 1.5 mg/kg/d), may be able to decrease to 0.5–0.75 mg/kg/d after 8–10
wk of therapy
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Oral
- Give consistently with whole milk or other high-fat food increases drug absorption and allows smaller doses. This may allow
easier titration to lowest effective dosage range. Discuss with physician.
- Store at 15°–30° C (59°–86° F); protect capsules from light and moisture.
Body as a Whole: Nearly all resemble those of hypervitaminosis A syndrome. CNS: Fatigue, headache, fever, dizziness, lethargy, amnesia, anxiety, depression, pseudotumor cerebri. CV: Edema; cardiac thrombotic or obstructive events; postural hypotension, coagulation disorders, MI (rare). Special Senses: Dry nose, nose bleeds, change in hearing, earache, otitis externa; Eye irritation, decreased night vision, eyelid abnormalities; double vision; corneal erosion and abrasions; dry eyes, eye pain, blurred vision, excessive tearing, conjunctivitis, scotomas, photophobia. GI: Abdominal pain, appetite change, stomatitis, sore tongue, thirst, nausea, constipation, diarrhea, flatulence, weight loss, gingival bleeding, dry mouth. Urogenital: Abnormal menses, atrophic vaginitis, dysuria, polyuria. Hematologic: Anemia; increased or decreased serum potassium, calcium, sodium, phosphorus, chloride, fasting blood sugars, platelets, Hgb, Hct, PTT, MCHC, prothrombin time; increased BUN, creatinine. Metabolic: Hypertriglyceridemia, hepatitis (hepatotoxicity), hypercholesterolemia, lowered HDL, increased AST, ALT, bilirubin. Musculoskeletal: Bone and joint pain, muscle cramps, myalgia, gout, hyperkinesia, hyperostosis. Respiratory: Dyspnea, coughing. Skin: Nail disorders, photosensitivity; skin fragility and peeling; changes in perspiration, hair loss, dry skin, rash, itching, skin atrophy, fissures, ulcerations; hirsutism, herpes simplex. Other: Chapped lips, cheilitis; malignant neoplasms.
Drug: Alcohol may increase plasma triglyceride levels; isotretinoin, vitamin a preparations compound toxic effects; methotrexate may increase risk of hepatotoxicity; tetracyclines may increase risk of pseudotumor cerebri. Food: Milk will increase absorption of etretinate.
Absorption: Readily absorbed from GI tract with significant first pass metabolism. Peak: 2.5–5 h. Duration: Detectable serum levels for years after discontinuation. Distribution: Accumulates in adipose tissue, liver, and subcutaneous fat; crosses placenta; distributed into breast milk. Metabolism: Metabolized in liver. Elimination: Excreted primarily in feces; some excretion in urine. Half-Life: 120 h.
Assessment & Drug Effects
- Monitor therapeutic effectiveness. Transient exacerbation of psoriasis may occur during the initial treatment.
- Lab tests: Perform baseline hepatic function tests prior to treatment, then at 1- to 2-wk intervals for 1–2 mo. Continue
with periodic tests at intervals of 1–3 mo during treatment. Discontinue drug in presence of hepatitis. Determine blood
lipid before treatment and repeat at 1- to 2-wk intervals until lipid response is established (usually 4–8 wk).
Patient & Family Education
- Use effective contraception at least 1 mo before starting treatment, throughout treatment, and for as long as 4 y after treatment
ends.
- Note: Complete clearing of the disease has been observed after 4–9 mo of therapy in most patients.
- Notify physician immediately of pain and limitation of motion; drug will be discontinued. Common sites for drug-induced hyperostosis
(abnormal growth of bone tissue) in adults are in the ankles, pelvis, and knees. Promptly report similar pain and limitation
of motion when drug is prescribed for child.
- Notify physician immediately of S&S of hepatitis: jaundice (see Appendix F), flu-like symptoms.
- Discontinue drug if any visual difficulties develop and schedule an ophthalmic examination.
- Avoid high-fat foods in diet because this drug can cause hypertriglyceridemia and increased LDLs.
- Avoid vitamin A supplements because of the possibility of additive toxic effects.
- Report early symptoms of pseudotumor cerebri: Headache, vomiting, nausea, blurred vision.
- Avoid excessive sun exposure and sunlamp treatments because of potential drug-induced photosensitivity and photophobia.
- Notify physician of dry mouth; drug-induced effects on oral mucosa and gingiva need to be treated.
- Be completely aware of the teratogenic danger. Discuss the risk of becoming pregnant or continuing a pregnancy with your physician.
- Do not donate blood while taking etretinate or for several years after therapy.
- Do not breast feed while taking this drug.
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Canadian drug name; 
Prototype drug