Etretinate

Etretinate Uses, Dosage, Side Effects, Food Interaction and all others data.

Etretinate is a medication used to treat severe psoriasis. It is a synthetic aromatic retinoid. The mechanism of action of etretinate is still incompletely understood although, like retinoic acid, it is thought to interfere with the terminal differentiation of keratinocytes. It is thought to bind to the retinoic acid receptors. Etretinate is also believed to enhance the binding of cAMP to the regulatory RI subunit of cAMP dependent protein kinases. Etretinate was taken off the market in Canada in 1996 and America in 1998 due to the risk of birth defects. Etretinate is now used to treat T-cell lymphomas. It also appears to inhibit NADH oxidase activity.

The active metabolite responsible for etretinate's effects, acitretin, is a retinoid. Retinoids have a structure similar to vitamin A and are involved in the normal growth of skin cells. Acitretin works by inhibiting the excessive cell growth and keratinisation (process by which skin cells become thickened due to the deposition of a protein within them) seen in psoriasis. It therefore reduces the thickening of the skin, plaque formation and scaling.

Etretinate
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Etretinate
Availability	Discontinued
Generic	Etretinate
Etretinate Other Names	Etretinate, etretinato
Related Drugs	Humira, Cosentyx, methotrexate, Remicade, Stelara, cyclosporine, infliximab
Type
Formula	C₂₃H₃₀O₃
Weight	Average: 354.4825 Monoisotopic: 354.219494826
Protein binding	More than 99% bound to plasma proteins, predominantly lipoproteins, whereas its active metabolite, acetretin (etretin), is predominantly bound to albumin.
Groups	Withdrawn
Therapeutic Class
Manufacturer
Available Country
Last Updated:	September 19, 2023 at 7:00 am

Uses

For the treatment of severe psoriasis in adults.

How Etretinate works

The mechanism of action of the active metabolite, acitretin, is unknown, however it is believed to work by targeting specific receptors (retinoid receptors) in the skin which help normalize the growth cycle of skin cells.

Toxicity

Symptoms of overdose include headache and vertigo.

Food Interaction

Avoid alcohol. Alcohol should be completely avoided for up to 2 months after discontinuation.
Take with food. Food increases absorption.

Etretinate Cholesterol interaction

[Moderate] The use of retinoids is associated with elevations in serum triglycerides and cholesterol, and decreases in HDL.

In addition to cardiovascular risks, elevation of serum triglycerides to greater than 800 mg

Patients at increased risk for developing hypertriglyceridemia during retinoid therapy include those with diabetes mellitus, obesity, high alcohol consumption, or a family history of these conditions.

Blood lipid determinations should be performed prior to initiation of therapy and at 1- to 2- week intervals until the lipid response to the drug is established (usually 4 to 8 weeks).

Patients with preexisting hyperlipidemia may require closer monitoring during retinoid therapy, and adjustments made accordingly in their lipid-lowering regimen.

Etretinate Disease Interaction

Major: intracranial hypertension, psychiatric disordersModerate: elevated serum triglycerides, liver disease

Elimination Route

Absorbed in the small intestine. Studies in normal volunteers indicate that the absorption of etretinate is greater in patients consuming whole milk or a high-fat diet than in patients in a fasting state.

Half Life

In one study, the apparent terminal half-life of etretinate after 6 months of therapy was approximately 120 days. In another study of 47 patients who had undergone chronic therapy with etretinate, 5 patients had detectable serum drug concentrations (0.5 to 12 ng/mL) 2.1 to 2.9 years after therapy was completed.