Tretinoin

DEA Class; Rx

Common Brand Names; Vesanoid

• Antineoplastics, Retinoids

tretinoin topical (Rx)

• Classes: Acne Agents, Topical

Naturally occurring retinoid analog; also known as all-trans-retinoic acid (aTRA)
Oral form used in acute promyelocytic leukemia; topical form used for cutaneous disorders like acne and photoaging
Treatment with oral form may cause acute promyelocytic leukemia differentiation syndrome

Indicated for the treatment of acne vulgaris.

For adjunctive treatment of photoaging including palliation of fine facial wrinkles, facial mottled hyperpigmentation (i.e., ‘liver spots’), and facial skin roughness.

For the treatment of acute promyelocytic leukemia (APL).

Hypersensitivity to retinoids, parabens, or formulation components

• Headache (86%)
• Fever (83%)
• Bone pain (77%)
• Dry mucous membranes (77%)
• Malaise (67%)
• URI (63%)
• Shivering (60%)
• Dyspnea (60%)
• Hemorrhage (60%)
• Elevated liver function tests (50-60%)
• Hyperlipidemia (60%)
• Infections (58%)
• Nausea and vomiting (57%)
• Rash (54%)
• Peripheral edema (52%)
• Leukocytosis (40%)
• Pain (37%)
• Abdominal pain (31%)
• DIC (26%)
• Respiratory insufficiency (26%)
• Mucositis (26%)
• GI disorder (26%)
• Retinoic acid-APL syndrome (25%)
• Ear ache (23%)
• Diarrhea (23%)
• Pleural effusion (20%)
• Dizziness (20%)
• Pruritus (20%)
• Sweating (20%)
• Anxiety (17%)
• Paresthesia (17%)
• Constipation (17%)
• Vision changes (17%)
• Dyspepsia (14%)
• Rales (14%)
• Depression (14%)
• Insomnia (14%)
• Alopecia (14%)
• Skin changes (14%)
• Confusion (11%)
• Abdominal distention (11%)
• Renal insufficiency (11%)

Ability to drive or operate machinery might be impaired in patients receiving therapy, particularly if they are experiencing dizziness or severe headache

Microdosed progesterone oral contraception (“minipill”) may not be adequate for contraception during tretinoin therapy

Initiation of therapy with may be based on morphological diagnosis of acute promyelocytic leukemia; confirmation of diagnosis of APL should be sought by detection of the t(15;17) genetic marker by cytogenetic studies; if these are negative, 200 PML/RARα fusion should be sought using molecular diagnostic techniques; patients without the t(15;17) translocation genetic marker should be considered for alternative treatment

Therapy has potentially significant toxic side effects in APL patients; patients undergoing therapy should be closely observed for signs of respiratory compromise and/or leukocytosis; supportive care appropriate for APL patients, eg, prophylaxis for bleeding, prompt therapy for infection, should be maintained during therapy (see Black Box Warnings)

Leukocytosis may occur (see Black Box Warnings)

Up to 60% incidence of hypercholesterolemia and/or hypertriglyceridemia, which were reversible upon completion of treatment reported; the clinical consequences of temporary elevation of triglycerides and cholesterol are unknown, but venous thrombosis and myocardial infarction reported in patients who ordinarily are at low risk for such complications

Elevated liver function test results occur in 50% to 60% of patients during treatment; liver function test results should be carefully monitored during treatment and consideration given to a temporary withdrawal of the drug if test results reach >5 times upper limit of normal values; however, majority of these abnormalities resolve without interruption of therapy or after completion of treatment

There is risk of thrombosis (both venous and arterial) which may involve any organ system, during first month of treatment; therefore, caution should be exercised when treating patients with combination of tretinoin with anti-fibrinolytic agents, such as tranexamic acid, aminocaproic acid or aprotinin

Do not coadminister with other retinoids or in combination with vitamin A because symptoms of hypervitaminosis A

Pregnancy category: D (systemic)

Lactation: Unknown if excreted in breast milk; do not breast-feed, because of potential for serious adverse reactions in infant

45 mg/m2 per day PO.

45 mg/m2 per day PO.

45 mg/m2 per day PO.

45 mg/m2 per day PO.

Safety and efficacy not established.

Safety and efficacy not established.

Tretinoin

capsule

• 10mg

topical cream

• 0.02% (Renova)
• 0.025% (Retin-A, Avita)
• 0.05% (Retin-A, Renova, Refissa)
• 0.06% (Retin-A Micro Pump)
• 0.1% (Retin-A)

topical gel

• 0.01% (Retin-A)
• 0.025% (Retin-A, Avita)
• 0.04% (Retin-A Micro)
• 0.05% (Atralin)
• 0.08% (Retin-A Micro)
• 0.1% (Retin-A Micro)

topical solution

• 0.05% (Retin-A)

topical lotion

• 0.05% (Altreno)