Tretinoin
All-trans retinoic acid (ATRA), is medication used for the treatment of acne and acute promyelocytic leukemia.
It is in the retinoid family of medications.
It is synthesized from Beta-carotene.
It is applied to the skin as a cream, gel or ointment for acne.
For leukemia, it is taken by mouth for up to three months.
Pregnancy category
US: D (Oral), C (Topical)
Routes of administration topical, by mouth
Protein binding > 95%
Elimination half-life 0.5-2 hours
Common side effects when used as a cream: skin redness, peeling, and sun sensitivity.
With oral use side effects include: shortness of breath, headache, numbness, depression, skin dryness, itchiness, hair loss, vomiting, muscle pains, vision changes, high white blood cell counts and blood clots.
Use during pregnancy is contraindicated due to the risk of birth defects.
Topical tretinoin is used for the treatment of acne.
Ot is most commonly used to treat acne vulgaris.
Retinoids accelerate the resolution of acne-induced postinflammatory hyperpigmentation, and is used as maintenance therapy for people who have responded to initial treatment of acne and as maintenance therapy can reduce the use of antibiotics.
In its topical form it has a pregnancy category C and should not be used by pregnant women.
Tretinoin is used to induce remission in people with acute promyelocytic leukemia who have a the t(15;17) translocation and/or the presence of the PML/RARα gene, and who don’t respond to anthracyclines or can’t take that class of drug.
Tretinoin is not used for maintenance therapy.
Topical retinoids increase collagen production, induce epidermal hyperplasia, and decrease keratinocyte and melanocyte atypia.
It is is the most extensively investigated retinoid therapy for photoaging, used for mild to severe photoaging in people of all skin types.
Common side effects of topical retinoin include: skin irritation, redness, swelling, and blistering.
Topical retinoids may be associated with increased sun sensitivity, by thinning of the stratum corneum leading to a decreased barrier against ultraviolet light exposure, as well as an enhanced sensitivity due to the presence of cutaneous irritation.
Systemic retinoids can cause: risk of thrombosis, benign intracranial hypertensio, high lipids and liver damage.
Additionally, significant side effects include: malaise, shivering, hemorrhage, infections, peripheral edema. pain, chest discomfort, edema, disseminated intravascular coagulation, weight increase, injection site reactions, anorexia, weight decrease, and myalgia
Respiratory side effects are associated with the retinoic acid syndrome, and include: upper respiratory tract disorders, dyspnea, respiratory insufficiency, pleural effusion, pneumonia, rales, and expiratory wheezing.
Many patients taking the drug have report earache or a feeling of fullness in their ears.
Gastrointestinal disorders include bleeding, abdominal pain, diarrhea, constipation,dyspepsia, and abdominal distention.
Cardiovascular side effects include, arrhythmias, flushing. hypotension, hypertension, phlebitis, and cardiac failure, cardiac arrest, myocardial infarction, enlarged heart, heart murmur, ischemia, stroke, myocarditis, pericarditis, pulmonary hypertension, and secondary cardiomyopathy.
Nervous system side effects include: dizziness, paresthesias, anxiety, insomnia, depression, and confusion.and
Urinary system, side effects include chronic kidney disease.
Tretinoin forces APL cells to differentiate and stops them from proliferating, forcing the primary cancerous promyelocytes to differentiate into their final form, allowing normal cells to take over the bone marrow.
In acne, tretinoin are vitamin A derivatives that act by binding to two nuclear receptor families within keratinocytes.
Tretinoin decreases the ability of epithelial cells in hair follicles to stick together, leading to fewer blackheads and whiteheads.
Tretinoin makes the epithelial cells divide faster, causing the blackheads to be pushed out.
The retinoid-receptor complex competes for transcription factors involved in inflammation, and down-regulate expression of toll-like receptor (TLR)-2, which has been implicated in the inflammatory response in acne.
Tretinoin and retinoids may enhance the penetration of other topical acne medications.