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Pronunciation |
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(e
TRET i
nate) |
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U.S. Brand
Names |
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Tegison® |
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Generic
Available |
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No |
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Pharmacological Index |
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Antipsoriatic Agent |
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Use |
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Treatment of severe recalcitrant psoriasis in patients intolerant of or
unresponsive to standard therapies |
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Pregnancy Risk
Factor |
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X |
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Contraindications |
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Pregnancy, known hypersensitivity to etretinate; because of the high
likelihood of long lasting teratogenic effects, do not prescribe etretinate for
women who are or who are likely to become pregnant while or after using the
drug |
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Warnings/Precautions |
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Not to be used in severe obesity or women of childbearing potential unless
woman is capable of complying with effective contraceptive measures; therapy is
normally begun on the second or third day of next normal menstrual period;
effective contraception must be used for at least 1 month before beginning
therapy, during therapy, and for 1 month after discontinuation of therapy;
pregnancy test must be performed prior to starting therapy |
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Adverse
Reactions |
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>10%:
Central nervous system: Fatigue, headache, fever
Dermatologic: Chapped lips, alopecia
Endocrine & metabolic: Hypercholesterolemia, hypertriglyceridemia
Gastrointestinal: Nausea, appetite change, xerostomia, sore tongue
Neuromuscular & skeletal: Hyperostosis, bone pain, arthralgia
Ocular: Eye irritation
Respiratory: Epistaxis
1% to 10%:
Cardiovascular: Edema
Central nervous system: Dizziness, lethargy
Hepatic: Hepatitis
Neuromuscular & skeletal: Myalgia
Ocular: Blurred vision
Otic: Otitis externa
Respiratory: Dyspnea
<1%: Syncope, amnesia, confusion, pseudotumor cerebri, depression,
urticaria, mouth ulcers, diarrhea, constipation, flatulence, weight loss,
gingival bleeding, gout, dysuria, polyuria, phlebitis, hyperkinesia, hypertonia,
photophobia, ear infection, kidney stones, rhinorrhea |
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Drug
Interactions |
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Increased effect: Milk increases absorption of etretinate
Increased toxicity: Additive toxicity with vitamin A |
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Mechanism of
Action |
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Unknown; related to retinoic acid and retinol (vitamin
A) |
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Pharmacodynamics/Kinetics |
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Absorption: Oral: Absorbed from small intestine; absorption enhanced when
coadministered with whole milk or a high lipid meal (highly lipophilic)
Protein binding: 99%
Metabolism: Undergoes significant first-pass metabolism to form acitretin
(active)
Half-life: 4-8 days (with multiple doses)
Elimination: By metabolism and by excretion in feces of unchanged drug and
metabolites |
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Usual Dosage |
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Adults: Oral: Individualized; Initial: 0.75-1 mg/kg/day in divided doses,
increase by 0.25 mg/kg/day at weekly intervals up to 1.5 mg/kg/day; maintenance
dose established after 8-10 weeks of therapy 0.5-0.75
mg/kg/day |
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Dietary
Considerations |
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May be administered with food |
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Mental Health: Effects
on Mental Status |
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Sedation is common; may cause dizziness; may rarely cause confusion or
depression |
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Mental Health:
Effects on Psychiatric
Treatment |
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Concurrent use with psychotropics may produce additive sedation or dry
mouth |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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>10% of patients experience dry mouth |
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Patient
Information |
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Take with food. Do not take additional vitamin A supplements. You may
experience dizziness, blurred vision, or fatigue; use caution when driving or
engaging in tasks that require alertness until response to drug is known. Report
persistent severe nausea, abdominal pain, visual disturbances, yellowing of skin
or eyes, unusual bruising or bleeding, muscle pain or cramping, or unusual
nosebleeds. Pregnancy/breast-feeding precautions: Inform prescriber if
you are pregnant. Do not get pregnant for 1 month following therapy. Consult
prescriber for instruction on appropriate contraceptive measures. This drug
cause severe fetal defects. Do not donate blood during therapy or for an
indefinite period following therapy. Do not breast-feed. |
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Dosage Forms |
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Capsule: 10 mg, 25 mg |
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