28 - 185 - RETINOIDS Flashcards

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1
Q

US FDA approved as oral therapy for CTCL

A. Tretinoin

B. Alitretinoin

C. Tazarotene

D. Bexarotene

A

D

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2
Q

Example of second generation retinoid

A. Alitretinoin

B. Adapalene

C. Acitretin

D. Tazarotene

A

C

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3
Q

Discontinuation of isotretinoin is warranted in which situation/s

A. Elevation of transaminases three times from the normal range

B. Triglyceride levels reaches 800mg/dl

C. A and B

D. None of the above

A

C

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4
Q

These medications can prolong the half-life of tretinoin locallt on the skin

A. Ketoconazole

B. Alcohol

C. Liazole

D. A and C

A

D

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5
Q

High incidence of neutropenia has been identified with this retinoid

A. Alitretinoin

B. Bexarotene

C. Acitretin

D. Etretinate

A

B

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6
Q

Most frequent laboratory abnormality seen with retinoid therapy

A. Serum lipid changes

B. Elevated transaminases

C. Elevated kidney function test

D. Increased FBS

A

A

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7
Q

any molecule that by itself or through metabolic conversion binds to and activates retinoic acid receptors

A

Retinoid

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8
Q

predominant retinoid receptors in human skin

A

retinoic acid receptor α (RAR-α),
RAR-γ,
retinoid X receptor α (RXR-α),
RXR-β

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9
Q

bind to retinoic acid–responsive elements and are responsible for retinoid signaling

A

RAR-γ/RXR-α heterodimers

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10
Q

Approved indications of topical retinoids

A

acne, psoriasis, cutaneous T-cell lymphoma, Kaposi sarcoma, melasma, photoaged skin

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11
Q

Approved indications of oral retinoids

A

acne, chronic hand eczema, psoriasis, and cutaneous T-cell lymphoma

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12
Q

Most concerning side effect of retinoids

A

Teratogenicity

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13
Q

First-generation retinoids

A
  • all-trans-retinoic acid (tretinoin),
  • 13-cis-retinoic acid (isotretinoin),
  • 9-cis-retinoic acid (alitretinoin)
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14
Q

Second-generation retinoids

A

Etretinate
Acitretin

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15
Q

Third Generation Retinoids

A

Adapalene
Tazarotene
Bexarotene

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16
Q

Also known as synthetic retinoids

A

2nd and 3rd gen retinoids

17
Q

Until how long should you give contraception after discontinuation of isotretinoin?

A

1 month

“After the end of treatment, endogenous concentrations of isotretinoin and its major metabolite are reached within 2 weeks. Therefore, a 1-month posttherapy period of contraception provides an adequate safety margin.”
Page 3399

18
Q

Prodrug of acitretin

A

Etretinate

19
Q

Until how long should a patient take contraception after discontinuation of acitretin?

Patients should avoid alcohol for how how many months after discontinuation?

A

2 years (contraception)

2 months (alcohol)

“Whereas etretinate is approximately 50 times more lipophilic than acitretin and binds strongly to plasma lipoproteins, acitretin binds to albumin. Thus, after etretinate is taken, it is stored in adipose tissue from which it is released slowly; it has a half-life of up to 120 days. In contrast, acitretin has a half-life of only 2 days. 15 However, small amounts of etretinate can be formed in patients receiving acitretin if it is taken simultaneously with alcohol. 16 This has prompted the manufacturer to extend the time of compulsory contraception in patients taking acitretin to 2 years (3 years in the United States). Acitretin still has a pharmacokinetic advantage over etretinate; however, all women must strictly avoid alcohol consumption during treatment and for 2 months thereafter. “

20
Q

Retinoid approved for management of cutaneous T-cell lymphoma

A

Bexarotene

21
Q

Retinoid approved for patients with Kaposi sarcoma (KS)

A

Alitretinoin

22
Q

Out of all the acne medications, this is thought to be the best, if not the only, agents to normalize the abnormal follicular epithelial differentiation and desquamation that occur in acne

A

Retinoid

23
Q

approved in Europe and Canada for treatment-resistant chronic hand eczema

A

Alitretinoin

Between 3 and 6 months of therapy is usually required to fully appreciate the effect

24
Q

effective in the treatment of premalignancies, including human papillomavirus–induced tumors and actinic keratoses. In basal cell nevus syndrome and xeroderma pigmentosum, these drugs dramatically reduce the incidence of malignant degeneration of the precancers.

A

Acitretin

25
Q

For photoaging, which topical retinoid are approved

A

Tretinoin and Tazarotene

26
Q

most important element in topical retinoid therapy

A

patient education

27
Q

optimal benefit in acne would be achieved with a daily dose of isotretinoin, approximately _____

A

0.5 to 1 mg/kg of body weight per day

28
Q

For patients taking isotretinoin, Posttherapy relapse is minimized by administering a cumulative dose of at least ________

A

120 mg/kg

This implies 6 to 8 months of therapy.

A lag period of 1 to 3 months may occur before the onset of the therapeutic effect, and a flare-up of disease during the first few weeks may be observed.

29
Q

The recommended alitretinoin dose in treatment of chronic hand eczema

A

10 to 30 mg/day

Treatment periods of up to 6 months are often needed before a full evaluation of the therapeutic effects can be made.

30
Q
A
31
Q

The recommended initial dosage of bexarotene

A

300 mg/m2 /day, administered as a single oral dose with meals

32
Q

The most common adverse effect associated with topical retinoid use

A

Local skin irritation

33
Q

most common cutaneous side effect with bexarotene

A

localized or extensive exfoliative dermatitis

34
Q

Concomitant use of isotretinoin and tetracyclines, which rarely produce increased intracranial hypertension, is the major risk factor for development of _____________

A

pseudotumor cerebri

35
Q

Discontinuation of therapy is required if the triglyceride level reaches what level

A

800 mg/dL

36
Q

Transaminase elevations of more than ______ warrant discontinuation of retinoid therapy

A

3x the upper normal range

37
Q

With isotretinoin, women with childbearing potential must have how many negative pregnancy tests

A

two negative results on a pregnancy test spaced 30 days apart and must practice effective contraception during treatment and for 1 month (2 months in some countries) after the completion of therapy.

38
Q

Hypothyroidism may occur in patients taking these retinoids

A

Bexarotene and alitretinoin

both drugs bind to RXR that dimerizes with the nuclear thyroid receptor

39
Q

concurrent use of these azoles and topical tretinoin can prolong the half-life of tretinoin locally in the skin, thereby aggravating local side effect

A

Ketoconazole and liarozole

The major avenue of tretinoin inactivation is through CYP26. Ketoconazole and liarozole are effective inhibitors of CYP26