Acitretin
- I. Introduction
- II. Uses of Acitretin
- III. Off-label Use of Acitretin
- IV. How Acitretin Works
- V. Dosage and Administration
- VI. Common and Severe Side Effects of Acitretin
- VII. Contraindications and Warnings
- VIII. Careful Administration Considerations
- IX. Interactions with Acitretin
- X. Composition and Storage
- XI. Overdosage and Management
- XII. Important Precautions While Using Acitretin
- XIII. Handling Precautions for Acitretin
- XIV. Summary and Key Takeaways
I. Introduction
Brief History of Acitretin
Acitretin, a type of retinoid that belongs to the second generation, was first introduced in the early 1980s. It was initially created as a replacement for etretinate, aiming to provide therapeutic advantages while minimizing potential side effects. Due to concerns regarding etretinate elimination half-life acitretin emerged as a safer but equally effective option for treating severe skin conditions.
General Classification (Retinoid)
Acitretin, a form of vitamin A, is classified as a retinoid and is used in dermatology and oncology to regulate the growth of epithelial cells.
FDA Approval Status and Indications
Acitretin was granted approval by the FDA in 1996. Its primary purpose is to treat psoriasis in adults, including instances where other treatments have proven ineffective. This medication is specifically created to address symptoms in patients whose condition necessitates the acceptance of risks due to its severity.
II. Uses of Acitretin
Treatment of Severe Psoriasis
Acitretin has shown efficacy in the treatment of severe psoriasis, a long-lasting autoimmune skin condition marked by red and scaly patches12. It aids in:
1: Acitretin: Drug Information – DermNet 2: Acitretin capsules & psoriasis. Acitretin side-effects - Patient 3: Acitretin - Psoriasis Association 4: Soriatane (Acitretin) - The National Psoriasis Foundation 5: Acitretin (Oral Route) Description and Brand Names - Mayo Clinic
Other FDA Approved Uses
Acitretin is primarily used for treating psoriasis, but it has also received FDA approval for other conditions, like pustular psoriasis12 and congenital ichthyosis3. Acitretin works by suppressing the proliferation of keratinocytes and downregulating the expression of inflammatory cytokines4.
1: Acitretin for Psoriasis | Therapeutic Cheat Sheet - Next Steps in Dermatology 2: (acitretin) Capsules - Food and Drug Administration 3: Acitretin for the management of generalized cutaneous lichen planus - NCBI 4: Acitretin-Conjugated Dextran Nanoparticles Ameliorate Psoriasis-like Skin Lesions in Mice - Frontiers
Comparison with Other Retinoids
Acitretin is famous for its ability to specifically target the retinoic acid receptors in the skin1. Unlike its predecessor, etretinate, acitretin has a shorter half-life, which makes it a safer choice for numerous patients23. Etretinate has a long elimination half-life of up to 175 days4, while acitretin has a half-life of only 39-96 hours5.
1: Acitretin for the management of generalized cutaneous lichen planus - NCBI 2: Acitretin - Wikipedia 3: Acitretin: Dosage, Mechanism/Onset of Action, Half-Life - Medicine.com 4: Concentration of etretinate in plasma and subcutaneous fat after long-term acitretin therapy - The Lancet 5: (acitretin) Capsules - Food and Drug Administration
III. Off-label Use of Acitretin
Acitretin in Dermatologic Conditions
Apart from the FDA-approved uses, acitretin has also been utilized for dermatologic conditions not officially listed. These conditions include Darier’s disease12, lichen planus23, and cutaneous lupus erythematosus4. Acitretin is a highly versatile instrument in the dermatologist’s toolbox, with a variety of off-label applications for difficult-to-treat dermatologic diseases2.
1: Acitretin: Dosage, Mechanism/Onset of Action, Half-Life - Medicine.com 2: Acitretin for Psoriasis | Therapeutic Cheat Sheet - Next Steps in Dermatology 3: Acitretin dosing, indications, interactions, adverse effects, and more. 4: Acitretin Monograph for Professionals - Drugs.com
Acitretin in Oncology
The study of how retinoids can inhibit cell growth has sparked curiosity about the potential of acitretin as a therapy for specific types of cancer, particularly cutaneous T-cell lymphoma12. Acitretin is a synthetic retinoid that has effects on cell cycle control, induction of apoptosis, promotion of cellular differentiation, and immunomodulation1. Acitretin has also been used off-label to manage refractory multikinase inhibitor–associated hand-foot skin reaction, a common adverse effect of some anticancer drugs3.
1: 11.3 Strategies to manage keratinocyte cancer in organ transplant recipients - Cancer Guidelines Wiki 2: For the Patient Acitretin - BC Cancer 3: Outcomes of Acitretin Treatment for Refractory Multikinase Inhibitor–Associated Hand-Foot Skin Reaction | Dermatology | JAMA Dermatology | JAMA Network
Legal and Ethical Considerations
Acitretin is an oral, systemic retinoid approved for the treatment of psoriasis1. It has been used off-label for skin conditions such as Darier’s disease, palmoplantar pustulosis, lichen planus, Sjogren-Larsson syndrome2, and multikinase inhibitor-associated hand-foot skin reaction3. Prescribing acitretin for off-label purposes requires consideration. Doctors should communicate to patients that the prescription is off-label and thoroughly discuss the risks and benefits.
1: Oral retinoids | DermNet 2: Acitretin dosing, indications, interactions, adverse effects, and more. 3: Outcomes of Acitretin Treatment for Refractory Multikinase Inhibitor …
IV. How Acitretin Works
Mechanism of Action
Acitretin mainly focuses on receptors for acid (RARs) and retinoid X (RXRs) in the skin. It affects gene expression leading to changes in differentiation and growth.
Pharmacokinetics: Absorption, Distribution, Metabolism, and Excretion
Acitretin is readily absorbed when consumed with a meal. It firmly attaches to proteins in the blood. Breaks down into shorter substances. The time it takes for the body to eliminate half of the acitretin ranges from 49 to 96 hours through bowel movements and, to a lesser degree, urine.
V. Dosage and Administration
Standard Dosage Guidelines
The recommended starting dose of acitretin for adults with psoriasis is between 25 and 50 mg daily. Adjustments to the dosage will depend on how the individual patient responds to the medication and their tolerance levels.
Adjusting Dosage: Special Circumstances
It is essential to adjust the dosage for patients with liver or kidney problems. Close monitoring is crucial to prevent any harm to these patients.
Administration Techniques and Tips
It is recommended to take Acitretin capsules along with your meal. Taking it consistently with food helps improve absorption and maintains levels in your body.
VI. Common and Severe Side Effects of Acitretin
Common Side Effects: List and Descriptions
Some observed effects of using acitretin are dry skin, lips becoming chapped, skin scaling, and increased liver enzyme levels. Additionally, it may cause an increase in cholesterol levels.
Severe Side Effects and Warning Signs
Severe adverse reactions may include indications of liver damage, increased triglyceride levels that can result in pancreatitis, and the possibility of displaying aggressive behavior or having thoughts of self-harm.
Managing Side Effects: Tips and Recommendations
It may be necessary to decrease the dosage or stop taking the medication altogether to handle any reactions. It's essential to take action, like using moisturizers for dry skin and regularly monitoring your lab results.
VII. Contraindications and Warnings
Absolute Contraindications
Women should never use acitretin as it poses a significant risk of causing severe fetal deformities. It is also not recommended for individuals with liver or kidney disease.
Relative Contraindications
Some factors to consider are avoiding alcohol while taking acitretin because it can interact with the medication and if you have a history of pancreatitis, it's essential to be aware that acitretin could potentially cause an increase, in levels.
Black Box Warning and Rationale
A box warning accompanies Acitretin because it can cause birth defects. Women in their years need to follow strict contraceptive measures while undergoing treatment and for a few years to avoid any risk of exposing the developing fetus.
VIII. Careful Administration Considerations
Administration to Elderly Patients
Elderly individuals might experience a decline in their kidney and liver function, which can decrease the way drugs are processed within their bodies. To address this, it is essential, to begin with doses initially, closely monitor for any potential side effects, and make adjustments based on the patient's ability to handle acitretin.
Administration to Pregnant Women and Nursing Mothers
Acitretin can potentially cause birth defects making it unsafe for pregnant women and those who may become pregnant. It is also recommended that nursing mothers avoid using acitretin as it is uncertain whether the medication can be passed through breast milk and potentially harm their infants.
Administration to Children
The use of acitretin in children has not been definitively proven to be safe and effective. Therefore it is advisable to exercise caution when considering pediatric use and to consult with a specialist beforehand.
Special Populations: Renal and Hepatic Impairment
Patients who have liver or kidney problems should be cautious when taking acitretin. It is essential to check their liver and kidney function and make any necessary changes to the dosage to avoid potential harm.
IX. Interactions with Acitretin
Drug-Drug Interactions
Acitretin has the potential to interact with types of medications such as antiepileptic drugs, certain antibiotics, and oral antifungals.
Drug-Food Interactions
It is advisable to refrain from consuming alcohol while undergoing acitretin therapy as it can result in the production of etretinate, which has a longer duration of action.
Effect on Laboratory Tests
When taking Acitretin, it is important to monitor liver function tests, lipid profiles, and blood glucose levels. This helps in identifying any abnormal changes that may occur.
X. Composition and Storage
Active and Inactive Ingredients
Acitretin serves as the component in the capsule alongside other inactive ingredients, like gelatin, sorbitol, and microcrystalline cellulose.
Proper Storage Conditions
Store the Acitretin capsules at room temperature in a controlled environment from extreme heat and moisture. It's essential to keep this medication out of the reach of children and pets.
Stability and Shelf Life
The packaging of acitretin mentions its expiration date. It is essential not to use it beyond that date to ensure its effectiveness and safety.
XI. Overdosage and Management
Symptoms of Overdosage
When an excessive amount of the substance is taken, individuals may experience headaches, dizziness, feelings of nausea, and episodes of vomiting. Additionally, the skin might become excessively dry. Start to peel.
Emergency Management and Antidote Information
There is no remedy for an overdose of acitretin. The approach involves providing support and symptomatic treatment with prompt medical attention being necessary.
Reporting Procedures and Resources
Healthcare providers are advised to notify the poison control center or use the FDAs MedWatch program if they encounter acitretin overdose cases.
XII. Important Precautions While Using Acitretin
Monitoring Parameters and Frequency
It is crucial to monitor the laboratory, which includes conducting liver function tests and lipid profiles while undergoing acitretin therapy. This helps in identifying any adverse effects as soon as possible.
Lifestyle Modifications
Patients might have to make some changes to their routine when taking acitretin. These changes could include avoiding alcohol, using moisturizers for skin, and minimizing exposure to sunlight and UV rays.
Compliance and Follow-Up Care
Patients must prioritize following their treatment plan and consistently participating in ongoing medical checkups to achieve the best possible results while minimizing potential risks.
XIII. Handling Precautions for Acitretin
Safe Handling for Healthcare Professionals
Healthcare providers need to be cautious while dealing with acitretin. They need to wear gloves to avoid any skin contact.
Disposal of Unused or Expired Medication
You should follow the guidelines for disposing of unused or expired acitretin to ensure it doesn't harm others or the environment.
XIV. Summary and Key Takeaways
Summary of Acitretin’s Efficacy and Risks
Acitretin is a medicine mainly prescribed to treat severe cases of psoriasis. Although it provides advantages for individuals with resistant conditions, it does come with notable risks, such as the potential for severe birth defects and liver toxicity.
Patient Counseling Points
Patients should receive counseling regarding the potential risks associated with acitretin. It is crucial to emphasize the significance of adhering to the treatment plan, undergoing monitoring, and implementing effective contraception measures for women in their childbearing years.
Resources for Further Information
To find out more, healthcare professionals and patients should refer to the prescribing information. Reach out to reputable dermatological societies or government health departments.