tretinoin

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tretinoin

 [tret´ĭ-no″in]
the all-trans stereoisomer of retinoic acid, used topically for treatment of cases of acne vulgaris in which comedones, pustules, and papules predominate; it prevents comedo formation and suppresses keratin synthesis; common adverse effects are erythema and desquamation. It is also administered orally in treatment of acute promyelocytic leukemia.

tretinoin

Atralin, 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 Box 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.

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 will 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.


triamcinolone acetonide

Adcortyl (UK), Kenalog, Kenalog-10, Kenalog-40, Nasacort AQ, Triaderm (CA)


tret·i·no·in

(tret'i-nō'in),
A keratolytic agent. See: retinoic acid.

tretinoin

/tret·i·noin/ (tret´ĭ-noin″) the all-trans stereoisomer of retinoic acid, used as a topical keratolytic in the treatment of acne vulgaris and disorders of keratinization and administered orally in the treatment of acute promyelocytic leukemia.

tretinoin

(trĕt′ĭ-noin′)
n.
An isomer of retinoic acid used topically to treat acne and to mitigate fine facial wrinkling and orally to treat one form of leukemia.

tretinoin

[tret′inō′in]
a retinoic acid derivative.
indications It is prescribed in the topical treatment of acne vulgaris and fine wrinkles and is administered orally for inducing remission in acute promyelocytic leukemia.
contraindications Known hypersensitivity to this drug or pregnancy prohibits its use.
adverse effects Among the more serious adverse effects of topical administration are photosensitivity and red, edematous, blistered, or crusted skin. Almost everybody taking the drug orally experiences some degree of weakness, fatigue, headache, and fever, but adverse effects are seldom reasons for discontinuing use of the drug.

tretinoin

A synthetic form of vitamin A used to treat acne, keratinisation (e.g., keratosis pilaris) and dermatitis. It also stimulates the immune system and is used to treat acute promyelocytic leukaemia. Retinoic acid is the naturally occurring form of the fat-soluble vitamin A, which is critical for the transportation of monosaccharides in glycoprotein synthesis, as occurs in the turnover of mucosal epithelia of the oral cavity and the respiratory and urinary tracts.

Toxicity
Skin blistering, crusting, headache, nausea, vomiting, vertigo.

tretinoin

all-trans-retinoic acid Dermatology A synthetic derivative of vitamin A used topically to reverse some of the effects of photoaging, both clinically–↓ skin wrinkling, improved skin texture and color and microscopically–↑ epidermal thickness, ↑ collagen and dermal vessels and 'erasing' epithelial atypia and dysplasia; tretinoin restores production of collagen I in photodamaged skin and lightens postinflammatory hyperpigmentation, it is also used for acne, keratinization, dermatitis, as a cancer preventive agent, and to induce terminal differentiation of acute promyelocytic leukemia, driving it into a mature nonproliferative state of remission Mechanism Unknown, possibly related to tretinoin's inhibition of collagenase, which degrades anchoring fibril collagen; tretinoin doubles the number of anchoring fibrils at the dermoepidermal junction Adverse effects Skin blistering, dry skin, bone pain, headache, N&V, vertigo, ↑ transferases, hyperhistaminemia. See Retinal, Retinoic acid, Vitamin A.

tretinoin

A RETINOID drug used to treat ACNE, scaly skin conditions such as ICHTHYOSIS, skin ageing and certain forms of LEUKAEMIA. Brand names are Retin-A, Retinova and Vesanoid.

Tretinoin

A drug that works by increasing the turnover (death and replacement) of skin cells.
Mentioned in: Acne

tret·i·no·in

(tret'i-nō'in)
A keratolytic agent.

tretinoin

the all-trans stereoisomer of retinoic acid, used in dermatology for the treatment of disorders of keratinization. It is a potent teratogen and must be used with great caution.

Patient discussion about tretinoin

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