tret·i·noin (tr t n-oin )n. An isomer of retinoic acid, used in the treatment of acne. |
Tretinoin
tretinoin
tretinoin [tret´ĭ-no″in]
tretinoin (vitamin A acid, retinoic acid),
drug class: vitamin A acid;
action: decreases cohesiveness of follicular epithelium, decreases microcomedone formation;
use: treatment of acne vulgaris.
tretinoin Warning - Hazardous drug!
Avita, Renova, Retin-A, Retin-A Micro, Vesanoid
Pharmacologic class: Retinoid
Therapeutic class: Antineoplastic, dermatologic agent (topical)
Pregnancy risk category C (topical), D (oral)
FDA Boxed Warning
• Patients with acute promyelocytic leukemia (APL) are at high risk in general and may have severe adverse reactions. Give drug under supervision of physician experienced in managing patients with acute leukemia, in facility with laboratory and supportive resources sufficient to monitor drug tolerance and protect and maintain patient compromised by drug toxicity.
• Before using drug, physician must conclude that possible benefit to patient outweighs the following known adverse effects:
• Retinoic acid-APL (RA-APL syndrome), which may be accompanied by impaired myocardial contractility, hypotension, and progressive hypoxemia. Several patients have died with multiorgan failure. Syndrome generally occurs during first month of therapy (in some cases, after first dose).
• Leukocytosis at presentation or evolving rapidly during drug therapy. Patients with high white blood cell (WBC) at diagnosis (above 5 × 109/L) have increased risk of further rapid rise in WBC counts. Rapidly evolving leukocytosis raises risk of life-threatening complications.
• Teratogenic effects. Drug therapy during pregnancy carries high risk of severe birth defects. Nonetheless, if drug is best available treatment for pregnant woman or woman of childbearing potential, ensure that she has received full information and warnings of risk to fetus and of risk of possible contraception failure, and has been taught to use two reliable contraceptive methods simultaneously during therapy and for 1 month afterward.
Action
Unknown. Thought to cause differentiation of promyelocytic leukemic blast cells, leading to apoptosis (cell shrinkage and death) and cancer remission.
Availability
Capsules: 10 mg
Topical cream: 0.02%, 0.025%, 0.05%, 0.1%
Topical gel: 0.01%, 0.025%, 0.04%, 0.1%
⊘Indications and dosages
➣ APL when anthracycline chemotherapy fails or is contraindicated
Adults and children ages 1 and older: 45 mg/m2/day P.O. in two evenly divided doses. Discontinue after 90 days of therapy or 30 days after complete remission occurs, whichever comes first.
➣ Acne vulgaris
Adults: Apply Avita cream, Retin-A cream gel, or Retin-A Micro gel daily before bedtime or in evening. Cover entire affected area lightly.
➣ Adjunct for mitigating fine wrinkles in patients who use comprehensive skin care and sun avoidance programs
Adults: Apply Renova 0.02% cream to face daily in evening for up to 52 weeks, using only enough to lightly cover entire affected area.
➣ Adjunct for mitigating fine wrinkles, mottled hyperpigmentation, and tactile roughness of facial skin when comprehensive skin care and sun avoidance programs alone fail
Adults ages 50 and younger: Apply Renova 0.05% cream to face daily in evening for up to 48 weeks, using only enough to lightly cover entire affected area.
Contraindications
• Hypersensitivity to drug or parabens
• Pregnancy or breastfeeding (oral use)
Precautions
Use cautiously in:
• eczema, sunburn, photosensitivity
• concurrent use of over-the-counter (OTC) acne products or abrasive soaps or cleansers with strong drying effects or high alcohol or lime content (with all topical forms)
• concurrent use of astringents, spices, permanent wave solutions, electrolysis, hair depilatories or waxes, or photosensitizing drugs (such as fluoroquinolones, phenothiazines, tetracyclines, thiazides)
• heavily pigmented, elderly, pregnant, or breastfeeding patients (safety and efficacy not established for topical use)
• children younger than age 1 for oral use or younger than age 18 for topical use (safety and efficacy not established).
Administration
• Verify that female patient has had required pregnancy test before P.O. therapy starts.
• Know that Renova topical cream isn't indicated for acne vulgaris, and that other topical forms are indicated only for acne vulgaris. Also know that some absorption of topical products occurs.
| Route | Onset | Peak | Duration |
| P.O. | Unknown | 1-2 hr | Unknown |
| Topical | Unknown | Unknown | Unknown |
Adverse reactions
CNS: dizziness, headache, asthenia, paresthesia, confusion, agitation, hallucinations, anxiety, aphasia, depression, agnosia, insomnia, asterixis, cerebellar edema, hypotaxia, drowsiness, slow speech, facial paralysis, hemiplegia, hyporeflexia, hypotaxia, dementia, spinal cord disorder, tremors, dysarthria, cerebrovascular accident (CVA), coma, seizures, intracranial hypertension, cerebral hemorrhage
CV: heart murmur, chest discomfort, peripheral edema, hypertension, hypotension, phlebitis, edema, enlarged heart, ischemia, arrhythmias, secondary cardiomyopathy, myocarditis, myocardial infarction (MI), heart failure, pericardial effusion, impaired myocardial contractility, progressive hypoxemia
EENT: vision disturbances, visual acuity changes, visual field defect, absence of light reflex, hearing loss, earache, full sensation in ears
GI: nausea, vomiting, constipation, diarrhea, abdominal pain and distention, GI disorders, mucositis, dyspepsia, ulcer, anorexia, GI hemorrhage
GU: dysuria, urinary frequency, enlarged prostate, renal insufficiency , renal tubular necrosis, acute renal failure
Hematologic: leukocytosis, disseminated intravascular coagulation (DIC), hemorrhage
Hepatic: ascites, hepatosplenomegaly, hepatitis
Metabolic: fluid imbalance, acidosis
Musculoskeletal: bone pain or inflammation, myalgia, flank pain
Respiratory: respiratory tract disorders, dyspnea, expiratory wheezing, crackles, pneumonia, laryngeal edema, pulmonary infiltrates, pleural effusion, bronchial asthma, pulmonary hypertension
Skin: rash; pallor; flushing; diaphoresis; alopecia; dry skin and mucous membranes; skin changes; pruritus; cellulitis; burning, erythema, peeling, and stinging (with topical use)
Other: weight changes, fever, lymphatic disorder, hypothermia, infections, facial edema, pain, RA-APL syndrome, multisystem failure, septicemia
Interactions
Drug-drug. Photosensitizing drugs (such as fluoroquinolones, phenothiazines, tetracyclines, thiazides): increased risk of photosensitivity reaction (with topical forms)
Drug-diagnostic tests. Cholesterol, triglycerides: increased levels
Drug-food. Any food: enhanced tretinoin absorption
Drug-behaviors. Sun exposure: increased risk of photosensitivity
Patient monitoring
☞ Watch closely for septicemia, multisystem failure, and retinoic acid-APL syndrome (which causes pulmonary and pericardial effusion, fever, weight gain, and dyspnea).
☞ Monitor for significant adverse CNS reactions, including seizures, CVA, and cerebral hemorrhage.
☞ Monitor cardiovascular status. Stay alert for signs and symptoms of arrhythmias, MI, and heart failure.
☞ Closely monitor liver and kidney function tests. Watch for evidence of hepatitis and renal failure.
☞ Monitor coagulation studies. Watch closely for DIC and hemorrhage.
• Evaluate respiratory status. Stay alert for indications of pulmonary hypertension and respiratory insufficiency.
• Frequently assess lipid panel and CBC with white cell differential.
Patient teaching
• Instruct patient to take oral doses with food.
☞ Teach patient to recognize and immediately report serious adverse reactions.
• Tell patient he'll undergo regular blood testing during oral therapy.
• Instruct patient using topical form to gently wash face with mild soap, pat skin dry, and then wait 20 to 30 minutes before applying. Advise him to apply to face in evening, using only enough to cover entire affected area lightly and only for prescribed duration.
• Caution patient to avoid OTC acne drugs and extreme weather conditions (such as wind and cold). Urge him to adhere to prescribed skin care and sunlight avoidance programs when using topical form.
• Tell patient using topical form that transient burning, erythema, peeling, pruritus, and stinging may occur. Advise him to notify prescriber if these symptoms become severe.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, foods, and behaviors mentioned above.
tretinoin
Patient discussion about tretinoin.
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