Acitretin

Registered South African indications:

• Psoriasis
• Disorders of keratinization

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Pregnancy
• Breastfeeding
• Severe renal impairment
• Severe hepatic impairment
• Severe hyperlipaemia
• Coadministration with vitamin A or other retinoids
• Coadministration with methotrexate
• Coadministration with tetracyclines 
• Coadministration with low dose progesterone-only products 

Cautions

• Mild to moderare renal impairment 
• Mild to moderate hepatic impairment
• Blood donation to women of childbearing potential
• History of disturbances of lipid metabolism
• Diabetes mellitus
• Obesity
• Alcoholism
• Children
• Exposure to sunlight and the unsupervised use of sun lamps
• Concomitant use of contact lenses
• May impair ability to drive at night

Forms avail. in SA and covered in this monograph: cap

Psoriasis
- Pustulous psoriasis
- Severe extensive psoriasis

• Oral (cap): Initial: 25-30mg, dly for 2-4 weeks; Maintenance: 25-50mg/day for 6-8 weeks; Max: 75mg/24hrs

Disorders of keratinisation
- Congenital ichthyosis
- Pityriasis rubra pilaris
- Darier's disease

• Oral (cap): 20-50mg, dly

Not established for use in children below 18 years

Pregnancy

• Contraindicated
• Acitretin is highly teratogenic. Its use is contraindicated in women who might become pregnant during or within 3 years of the cessation of treatment. The risk of giving birth to a deformed child (craniofacial, central nervous system, cardiovascular, skeleton, thymus) is exceptionally high if acitretin is taken before or during pregnancy, no matter for how long or at what dosage. Also after use of acitretin during pregnancy, a single case with similar deformations has been reported
• Acitretin in common with vitamin A and other retinoids may cause malformations in offspring of various animal species, even at the dose levels recommended for humans. As acitretin is teratogenic in animals at human dose levels, Acitretin is absolutely contraindicated during pregnancy and women of childbearing age must not be treated with Acitretin, if pregnancy cannot be excluded
• At treatment of female patients of childbearing age with a very severe or disabling clinical picture, the treating physician may consider prescribing Acitretin, in case no alternative therapy, is available. Acitretin should only be prescribed by doctors, who have experience in treatment with systemic retinoids, preferably dermatologists, and who are aware of the teratogenic risk associated with acitretin if used during pregnancy
• Transformation of acitretin into etretinate is enhanced by alcohol. The formation, in vivo, of etretinate from acitretin with concomitant intake of alcohol, cannot be excluded. Etretinate is also teratogenic. As etretinate may be stored in fatty tissue and has a longer elimination half-time (approximately 120 days) than acitretin, women of childbearing age must not consume alcohol (in drinks, food or medicines) during treatment with acitretin and for 2 months after cessation of acitretin therapy. Also women of childbearing age should keep on practicing contraception for 3 years after stopping treatment

Breastfeeding

• Contraindicated
• Acitretin is lipophilic and passes into the breast milk. Patients must not breastfeed during treatment with Acitretin

Renal Impairment

• Mild to moderate: No dose adjustment recommended
• Severe: Contraindicated

Hepatic Impairment

• Mild to moderate: Caution; no dose adjustment recommended
  Hepatic function should be checked before starting treatment with Acitretin, every 1-2 weeks for the first 2 months after commencement and then every 3 months during treatment. If abnormal results are obtained, weekly checks should be instituted. If hepatic function fails to return to normal or deteriorates further, Acitretin must be withdrawn. In such cases it is advisable to continue monitoring hepatic function for at least 3 months
• Severe: Contraindicated

Elderly

• No dose adjustment recommended

Porphyria Information

• Possibly porphyrinogenic (PSP)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Increased intracranial pressure 
• Severe headache
• Lightheadedness
• Dizziness 

Cardiovascular Disorders

• Capillary leak syndrome
• Retinoic acid syndrome

Respiratory Disorders

• Dysphonia
• Epistaxis

Gastrointestinal Disorders

• Gastrointestinal symptoms 
• Dysgeusia
• Rhagades
• Inflammation of oral mucosa 
• Gingiva 
• Taste disturbances

Hepatobiliary Disorders

• Hepatitis 
• Jaundice
• Increased hepatic enzymes

Genitourinary Disorders

• Vulvovaginitis
• Increased createnine

Endocrine and Metabolic Disorders

• Thirst
• Feeling cold
• Sensation of heat
• Hypervitaminosis A
• Increased lactate dehydrogenase 
• Increased uric acid

Musculoskeletal Disorders

• Myalgia
• Arthralgia 
• Bone pain
• Bone changes 
• Soft-tissue calcification 
• Increased creatine phosphokinase

Skin and Subcutaneous Tissue Disorders

• Peripheral oedema
• Dry lips
• Inflamed lips
• Dry mucous membranes
• Peeling skin
• Skin thinning
• Erythema
• Pruritus
• Sensation of burning skin
• Sensation of sticky skin
• Dermatitis
• Hair loss
• Inflammation of the nail wall
• Nail fragility
• Blistering of the skin
• Change in pigmentation of the skin and hair
• Change in growth rate of hair
• Change in hair structure
• Dry skin
• Increased sensitivity
• Hair loss
• Sensitivity to light
• Madarosis 
• Exfoliative dermatitis

Immune, Blood and Lymphatic System Disorders

• Type 1 hypersensitivity
• Increased triglycerides
• Increased total cholesterol
• Lowering high density lipoprotein cholesterol

Sensory Disorders

• Conjunctivitis 
• Visual disturbances
• Impaired night vision
• Inflammation or ulcers of the cornea

• Tetracyclines 
• Phenytoin
• Methotrexate
• Vitamin A 
• Other retinoids 
• Alcohol
• Progesterone-only products 

• Hepatic function
• Lipid profile
• Renal function
• Full blood count

Specific cases may require

• Blood glucose
• X-rays
• Pregnancy test

• The capsules should be taken once daily with meals or with milk
• Patients should be instructed never to give this medicinal product to another person and to return any unused capsules to their pharmacist at the end of treatment
• Patients should not donate blood during therapy and for 3 years following discontinuation of acitretin because of the potential risk to the foetus of a pregnant transfusion recipient

Acitretin is a synthetic aromatic analogue of retinoic acid and the free acid derivative and main metabolite of etretinate. In psoriasis and orders of keratinisation acitretin brought about a more normal epidermal cell proliferation, differentiation and cornification. The action is purely symptomatic and the mechanism of action is unknown.  

Capsule 10mg

• Neotigason 10 mg (Teva Pharmaceuticals) originator

Capsule 25mg

• Neotigason 25 mg (Teva Pharmaceuticals) originator