Acitrok 2 mg - Acitretin

What It Is

Acitrok 2 mg is a brand formulation of Acitretin 2 mg, a second-generation aromatic retinoid (vitamin A derivative) used in dermatology. It is the active metabolite of the older drug etretinate. The 2 mg strength is a low-dose option used for maintenance therapy or in patients who are dose-sensitive.

Drug Class & Mechanism

Class: Second-generation systemic retinoid
Mechanism: Activates all three retinoic acid receptor (RAR) subtypes, leading to:
- Normalization of epidermal differentiation and proliferation
- Modification of inflammatory responses
- Reduction in neutrophil function
Half-life: ~2 days (much shorter than etretinate's 120 days), so it does not accumulate in adipose tissue - Dermatology 2-Volume Set 5e

Indications

Indication	Notes
Psoriasis (pustular - von Zumbusch)	First-line; clears rapidly
Erythrodermic psoriasis	Highly effective as monotherapy
Chronic plaque psoriasis	Best combined with PUVA/NB-UVB or vitamin D analogues
Palmoplantar keratodermas	Listed indication
Pityriasis rubra pilaris	Listed indication
Darier disease	Listed indication
Lamellar ichthyosis	Listed indication
Congenital ichthyosiform erythroderma	Listed indication
Cutaneous T-cell lymphoma (mycosis fungoides)	Used in combination with PUVA or interferon
Lichen planus	Off-label use
Other keratinization disorders	Subcorneal pustular dermatosis, verruca vulgaris, condyloma (off-label)

Dermatology 2-Volume Set 5e, Katzung's Basic and Clinical Pharmacology 16e

Dosing

Form	Standard Adult Dose
Oral (tablets)	25-50 mg/day (standard)
Low-dose / maintenance	2 mg/day (Acitrok 2 mg) or titrated up

Maximal therapeutic efficacy is reached after 2-3 months
The 2 mg formulation allows flexible dose titration and maintenance dosing

Adverse Effects

These resemble hypervitaminosis A:

Mucocutaneous (very common):

Cheilitis (lip dryness) - most common
Xerosis (dry skin), xerophthalmia (dry eyes)
Skin fragility, peeling, hair loss
Paronychia

Metabolic:

Elevated triglycerides and cholesterol (common)
Elevated liver enzymes (up to one-third of patients) - can require drug discontinuation
Hepatotoxicity (rare, but fatal hepatitis reported)

Musculoskeletal (with long-term use):

Hyperostosis, enthesopathy
Premature epiphyseal closure in children

Other:

Pseudotumor cerebri (rare, risk increased if combined with tetracyclines)
Photosensitivity

Contraindications

Absolute:

Pregnancy or lactation
Women of childbearing potential who cannot guarantee contraception for 3 years after stopping (FDA recommendation)
Severe liver or kidney dysfunction
Uncontrolled hypertriglyceridemia
Excessive alcohol intake

Relative / Caution:

Poorly controlled diabetes mellitus
History of pancreatitis
Atherosclerosis
Concomitant methotrexate (hepatotoxicity risk - reserved for treatment-resistant cases only)
Phenytoin co-administration (competes for plasma protein binding)
Dermatology 2-Volume Set 5e, Table 8.13

Critical Drug Interactions

Interaction	Risk
Alcohol	Converts acitretin back to etretinate - extends teratogenic risk for years. Alcohol must be strictly avoided during therapy and for 2 months after stopping
Methotrexate	Additive hepatotoxicity
Tetracyclines	Risk of benign intracranial hypertension (pseudotumor cerebri)
Phenytoin	Protein-binding competition; dose adjustment needed
Vitamin A supplements	Additive hypervitaminosis A toxicity

Monitoring

Before starting:

Pregnancy test
LFTs (AST, ALT, GGT, ALP, bilirubin)
Fasting lipid profile (triglycerides, cholesterol, HDL)
Blood glucose
Serum creatinine
CBC
Consider baseline spinal X-ray if long-term therapy is planned

During therapy:

Repeat LFTs and lipid panel every 4-8 weeks initially, then every 3 months
Monitor for mucocutaneous side effects

Key Safety Points

Teratogenicity - Acitretin is a potent teratogen. Contraception must be used for at least 3 years after stopping (FDA), or 2 years (manufacturer) if alcohol has been strictly avoided.
Blood donation - Prohibited during treatment and for 3 years after stopping.
Alcohol avoidance - Alcohol causes re-esterification of acitretin back to etretinate (much longer half-life), extending the period of teratogenic risk.
Contact lens wearers - May need lubricants or switch to glasses due to dry eyes.

Combination Use

Acitretin + PUVA (Re-PUVA): Highly effective for plaque psoriasis - reduces the UVA dose required
Acitretin + NB-UVB: Effective and commonly used
Acitretin + Vitamin D3 analogues (calcipotriol): Additive benefit in plaque psoriasis

Combination therapy is indicated for chronic plaque psoriasis where monotherapy efficacy is limited (~70% achieve moderate or better response as monotherapy; only 23% achieve PASI 75 at 50 mg/day for 8 weeks).

Sources: Dermatology 2-Volume Set 5e; Fitzpatrick's Dermatology Vol. 1 & 2; Katzung's Basic and Clinical Pharmacology, 16th Ed.

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