28 - 185 - RETINOIDS

Question 1

US FDA approved as oral therapy for CTCL

A. Tretinoin

B. Alitretinoin

C. Tazarotene

D. Bexarotene

Answer 1

D

Question 2

Example of second generation retinoid

A. Alitretinoin

B. Adapalene

C. Acitretin

D. Tazarotene

Answer 2

C

Question 3

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

Answer 3

C

Question 4

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

A. Ketoconazole

B. Alcohol

C. Liazole

D. A and C

Answer 4

D

Question 5

High incidence of neutropenia has been identified with this retinoid

A. Alitretinoin

B. Bexarotene

C. Acitretin

D. Etretinate

Answer 5

B

Question 6

Most frequent laboratory abnormality seen with retinoid therapy

A. Serum lipid changes

B. Elevated transaminases

C. Elevated kidney function test

D. Increased FBS

Answer 6

A

Question 7

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

Answer 7

Retinoid

Question 8

predominant retinoid receptors in human skin

Answer 8

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

Question 9

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

Answer 9

RAR-γ/RXR-α heterodimers

Question 10

Approved indications of topical retinoids

Answer 10

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

Question 11

Approved indications of oral retinoids

Answer 11

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

Question 12

Most concerning side effect of retinoids

Answer 12

Teratogenicity

Question 13

First-generation retinoids

Answer 13

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

Question 14

Second-generation retinoids

Answer 14

Etretinate
Acitretin

Question 15

Third Generation Retinoids

Answer 15

Adapalene
Tazarotene
Bexarotene

Question 16

Also known as synthetic retinoids

Answer 16

2nd and 3rd gen retinoids

Question 17

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

Answer 17

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.”
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Question 18

Prodrug of acitretin

Answer 18

Etretinate

Question 19

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

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

Answer 19

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. “

Question 20

Retinoid approved for management of cutaneous T-cell lymphoma

Answer 20

Bexarotene

Question 21

Retinoid approved for patients with Kaposi sarcoma (KS)

Answer 21

Alitretinoin

Question 22

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

Answer 22

Retinoid

Question 23

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

Answer 23

Alitretinoin

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

Question 24

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.

Answer 24

Acitretin

Question 25

For photoaging, which topical retinoid are approved

Answer 25

Tretinoin and Tazarotene

Question 26

most important element in topical retinoid therapy

Answer 26

patient education

Question 27

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

Answer 27

0.5 to 1 mg/kg of body weight per day

Question 28

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

Answer 28

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.

Question 29

The recommended alitretinoin dose in treatment of chronic hand eczema

Answer 29

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.

Question 30

Question 31

The recommended initial dosage of bexarotene

Answer 31

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

Question 32

The most common adverse effect associated with topical retinoid use

Answer 32

Local skin irritation

Question 33

most common cutaneous side effect with bexarotene

Answer 33

localized or extensive exfoliative dermatitis

Question 34

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

Answer 34

pseudotumor cerebri

Question 35

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

Answer 35

800 mg/dL

Question 36

Transaminase elevations of more than ______ warrant discontinuation of retinoid therapy

Answer 36

3x the upper normal range

Question 37

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

Answer 37

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.

Question 38

Hypothyroidism may occur in patients taking these retinoids

Answer 38

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

Question 39

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

Answer 39

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

Question 40

Molecular storage form of retinol

Answer 40

Retinyl esters

Question 41

Tazarotene is approved for what indications?

Answer 41

Acne, psoriasis, photoaging