Acitretin

Oral
Darier's disease

Oral
Congenital ichthyosis, Severe lichen planus, Severe psoriasis

Severe: Contraindicated.

Severe: Contraindicated.

Should be taken with food. Take w/ main meals or w/ a glass of milk.

Hyperlipidaemia. Severe hepatic and renal impairment. Pregnancy and lactation. Concomitant use w/ methotrexate, tetracyclines, vit A or other retinoids, low dose progesterone-only products (minipills).

Females of reproductive potential.

Cheilitis, alopecia, skin peeling, rhinitis, dry skin, nail disorder, pruritus, rigors, xerophthalmia, dry mouth, epistaxis, arthralgia, spinal hyperostosis, rash, hyperaesthesia, paraesthesia, paronychia, skin atrophy, decreased night vision, abdominal pain; abnormal hair texture; dermatitis; diarrhoea; epidermal fragility; erythema; headache; myalgia; nausea, vomiting; peripheral oedema; psudomotor cerebri, depression and other psychiatric symptoms (e.g. aggressive feelings, suicidal thoughts); increased liver enzymes, uric acid, BUN, triglycerides and cholesterol levels; increased or decreased electrolytes, haematocrit, Hb, glucose.
Potentially Fatal: Hepatotoxicity, fulminant pancreatitis.

PO: X

Avoid exposure to natural or artificial sunlight. This drug may decrease night vision, if affected, do not drive or operate any vehicle.

Monitor plasma lipid, glucose levels (esp in diabetic patients) regularly; bone abnormalities (long-term use). Perform LFTs; pregnancy tests (2 negative tests prior to therapy, mthly during treatment and 3 mthly for 3 yr after stopping therapy).

May reduce the protein binding of phenytoin.
Potentially Fatal: Increased risk of hepatitis w/ methotrexate. Increased intracranial pressure w/ tetracyclines. Risk of hypervitaminosis A w/ concomitant vit A and/or other oral retinoids. Interferes w/ the contraceptive effect of low dose progesterone-only products (minipills).

Increased absorption w/ food. Increased duration of teratogenic effects w/ concurrent ingestion of alcohol.

Description:
Mechanism of Action: Acitretin is a synthetic aromatic analogue of retinoic acid and an active metabolite of etretinate. The exact mechanism of action has not been established but may be mediated by activation of α, β and γ subtypes of retinoic acid and retinoid X receptors to inhibit the expression of the pro-inflammatory cytokines interleukin-6 (IL-6), migration inhibitory factor-related protein-8 (MRP-8), and interferon-γ, resulting to normalisation of epidermal cell proliferation, differentiation and keratinisation.
Onset: Full effect: 2-3 mth. Improvement: W/in 8 wk.
Pharmacokinetics:
Absorption: Absorbed in the GI tract. Increased absorption w/ food. Bioavailability: Approx 60-70%. Time to peak plasma concentration: 1-5 hr.
Distribution: Distributed into skin w/ highest concentration in stratum corneum; semen (small amounts). Penetrates adipose tissue, crosses the placenta and enters breast milk. Plasma protein binding: >99.9%, mainly to albumin.
Metabolism: Undergoes extensive hepatic metabolism and interconversion via simple isomerization to 13-cis-acitretin.
Excretion: Via Urine (16-53%) and faeces (34-54%). Elimination half-life: Approx 2 days.

Source: National Center for Biotechnology Information. PubChem Database. Acitretin, CID=5284513, https://pubchem.ncbi.nlm.nih.gov/compound/Acitretin (accessed on Jan. 20, 2020)

Store between 20-25°C.

Psoriasis, Seborrhea & Ichthyosis Preparations

D05BB02 - acitretin ; Belongs to the class of systemic retinoids used in the treatment of psoriasis.

Acitretin capsule (Actavis Pharma Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 25/05/2016.

Anon. Acitretin. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 25/05/2016.

Buckingham R (ed). Acitretin. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 25/05/2016.

Joint Formulary Committee. Acitretin. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 25/05/2016.

McEvoy GK, Snow EK, Miller J et al (eds). Acitretin (Topical). AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 25/05/2016.