Dermatology!Clinic!Systemic!Medications!Guide!

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April!2018!
Dermatology!department,!College!of!Medicine,!King!Saud!University,!Riyadh,!Saudi!Arabia!
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Prepared!by:!Sarah!Alsukait!&!Ghadah!Alotaibi!(R2!Dermatology!residents)!
Reviewed!by:!Dr.!Mohammed!Alhaddab!(Dermatology!consultant)!
Reference:!Wolverton,!S.!E.!(2013).!Comprehensive!dermatologic!drug!therapy.!Saunders.!
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Table!of!contents:!
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Methotrexate…………………………………………………………………………………………..2!
Cyclosporine…………………………………………………………………………………………...3!
Azathioprine…………………………………………………………………….................................4!
Mycophenolate!mofetil………………………………………………………………………….…5!
Adalimumab……………………………………………………………………….............................6!
Etanercept………………………………………………………………………………………………7!
Dapsone………………………………………………………………………………………………….8!
Colchicine……………………………………………………………………………………………….9!
Isotretinoin!and!acitretin…………………………………………………………………….…10!
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 METHOTREXATE!(MTX)!
Dose!&!regimen! - Initial!test!dose:!5V10!mg/week.!
- Maintenance!dose:!!
- Escalate!dose!gradually!2.5V5!mg/week.!!
- Psoriasis:!10V15!mg/week!(max!30!mg).!
- DM!and!neutrophilic!dermatoses:!25V35!mg/week.!
- Other!dermatoses:!10V25!mg/week.!
- With!or!after!food!
- Folic!acid!supplements!(1V5!mg!daily!except!MTX!day)!
Formulations! - Oral:!2.5!tablet!
- SC:!7.5V30!mg!
Contraindications! - Absolute:""
Pregnancy,!Lactation,!and!Hypersensitivity!to!MTX"
- Relative:""
Excessive!alcohol!intake,!renal!dysfunction!(Cr!clearance!<60!ml/min!reduce!dose,!avoid!in!
dialysis),!pleural!effusion!or!ascites!(reduce!dose),!metabolic!(DM,!obesity,!hyperlipidemia),!
active!PUD,!concomitant!radiation!therapy,!drug!interactions,!reduced!lung!function,!liver!
disease!(high!LFTs,!active!hepatitis,!NASH,!hx!of!liver!disease!or!cirrhosis,!hepatotoxic!drugs),!
severe!hematologic!abnormalities,!man!or!woman!planning!conception,!active!infection!or!hx!of!
infection!that!could!reactivate,!Immunodeficiency,!recent!live!vaccines!!
Special!situations! - Pregnancy!category!X!(abortifacient!&!teratogen)!
- Contraindicated!in!lactation!(excreted!in!breast!milk)!
- Should!be!stopped!3!months!before!conception!for!males!and!females,!
- Avoid!live!vaccines!
!

Drug!interactions! - Check!for!possible!drug!interactions.!
Monitoring! - Baseline:!
a. Clinical!assessment!
- Careful!history!and!physical!examination!
- Identification!of!patients!at!high!risk!for!liver!toxicity!
- Recording!concomitant!medications!(possible!interactions)!
b. Labs!
- CBC!w!diff,!CMP!(LFTs,!Cr,!BUN,!&!electrolytes)!
- Hep!B!markers,!Hep!C!ab,!TB!quantiferon/PPD!+/V!CXR,!HIV!ag/ab!
- VZV!serology!if!no!history!of!chickenpox.!!
- Pregnancy!test!in!females!of!childbearing!age!
c. Other!!
- Consider!CXR!if!underlying!pulmonary!disease!!
- Liver!biopsy!(can!be!considered;!in!high!risk!patients)!
- Follow!up:! !
a. Labs!
- CBC!w!diff,!LFTs!
! “5V6!days!after!‘test!dose’,!every!1V2!weeks!for!2V4!weeks,!1V2!weeks!after!dose!
escalations,!longVterm!every!8!to!12!weeks”!
! WBC!<3500,!platelet!<100,000!(discontinue!or!decrease!dose,!drug!can!be!
restarted!after!2V3!week!rest)!
! AST!or!ALT!x2!repeat!in!2V4!weeks,!AST!or!ALT!x2V3!(reduce!dose/discontinue,!
repeat!in!2V4!weeks).!
- Renal!function!tests!!
! Twice!every!year!except!for!patients!at!risk!of!renal!impairment.!
a. Other!investigations!
- Liver!biopsy:!after!3.5V4!g!total!cumulative!dosage!
!

Adverse!effects!
- Hepatotoxicity!(acute/chronic),!lung!toxicity!(CXR!if!hx!of!dry!cough!&!SOB),!hematologic!
(pancytopenia),!GI!effects!(can!be!reduced!with!folic!acid!use,!with!food,!reduce!or!divide!dose,!
SC!injection),!renal!effects!(with!high!dose!IV),!reproductive!effects!(teratogen!&!abortifacient!
in!females,!reversible!oligospermia!in!males),!lymphoma!induction!(?!no!clear!evidence!in!
psoriasis),!other!effects!(alopecia,!headaches,!fatigue,!infections,!radiation!recall)!
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 CYCLOSPORINE!(CsA)!
Dose!&!regimen! - Initial!dose:!2.5V3!mg/kg/d!in!two!divided!doses!
- Maintenance!dose:!!
- Titrated!up!to!4V5!mg/kg/d!two!divided!doses!over!6V8!weeks!
- Once!improved!reduce!the!dose!by!0.5V1!mg/kg/d!to!the!lowest!effective!dose.!
- Intermittent!short!courses!lasting!3V6months!ideally!(not!to!exceed!1!year).!!!
Formulations! - Oral:!25,!50,!100!mg!
Contraindications! - Absolute:!!
Uncontrolled!hypertension!significantly!reduced!renal!function,!hypersensitivity!to!CsA!or!any!
ingredients,!clinically!cured!or!persistent!malignancy!(except!NMSCs),!Cutaneous!TVcell!
lymphoma.!
- Relative:!!
Age!<18!or!>64!years,!controlled!hypertension,!recent!live!vaccination,!drug!interactions,!active!
infection!or!evidence!of!immunodeficiency,!concomitantly!receiving!phototherapy,!hx!of!>200!
PUVA,!or!radiation!therapy,!methotrexate,!or!other!immunosuppressive!agents,!pregnancy!or!
lactation,!and!unreliable!patients.!!

Special!situations! - Pregnancy!category!C!(not!shown!to!be!teratogenic)!
- Excreted!in!breast!milk!(shouldn’t!breastfeed)!
- Elderly:!monitor!closely!for!nephrotoxicity!
- Avoid!live!vaccinations!
Drug!interactions! - Check!for!possible!drug!interactions.!
Monitoring!! - ! Baseline:!
a. Clinical!assessment:!
- Careful!history!and!examination!(rule!out!active!infections,!skin!malignancy,!high!risk!
for!renal!toxicity,!2!baseline!blood!pressures!at!least!a!day!apart)!
- Recording!concomitant!medications!(possible!interactions)!
b. Labs!
- CBC,!LFTs,!BUN,!Cr!(two!baseline!creatinine!values!at!least!a!day!apart)!
- Urine!analysis!!
- Fasting!lipid!panel!
- Mg!(may!decrease),!K!(may!increase),!uric!acid!(for!patients!at!risk!for!gout)!
- TB!Quantiferon/PPD,!HIV!if!at!risk!
- Follow!up:! !
a. Clinical!assessment!
- ReVevaluate!q2!weeks!for!1V2!months,!then!q4V6!weeks!!
- Blood!pressure!checked!at!each!visit!
! If!BP!>140/90!check!again!in!2!weeks,!if!it!remains!high!reduce!the!dose!by!25V
50%!or!treatment!with!an!antihypertensive!should!be!considered.!!
b. Labs!
- Labs!every!2!weeks!for!the!first!1V2!months,!then!monthly!
- Creatinine,!BUN,!Mg,!K,!and!uric!acid!
! Cr!>25%!above!baseline!"!repeat!within!2!weeks!"!still!>25%!"!reduce!
CsA!dose!by!1!mg/kg!/day!for!at!least!1!month!"!if!Cr!remains!>25%!then!
stop!CsA,!if!Cr!<25%!continue!CsA!at!a!new!dose.!
! Cr!rises!>50%!"!discontinue!CsA!
- CBC,!LFTs,!and!Lipid!panel!
- Urine!analysis!
- q!1!month!if!abnormal;!otherwise!yearly.!
c. Others!
- Consider!trough!CsA!drug!levels!if!inadequate!clinical!response!or!suspected!drug!
interactions!or!noncompliance!
- Creatinine!clearance!(consider!if!1!year!therapy)!
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Adverse!effects! - Nephrotoxicity,!hypertension,!neurologic!(tremor,!headache,!parethesia,!hyperesthesia),!
! mucocutaneous!(hypertrichosis,!gingival!hyperplasia),!MSK!(myalgia,!lethargy,!arthralgia),!
! malignancy!risk!(NMSC!esp.!SCCs!with!hx!of!PUVA,!some!lymphoma),!hyperkalemia,!
! hyperuricemia,!hypomagnesmia,!hyperlipidemia.!
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AZATHIOPRINE!(IMURAN)!
Dose!&!regimen - Initial!dose:!1!mg/kg/day!
- Maintenance!dose:!!!
- Titrated!up!to!2V2.5!mg/kg!daily!
- Drug!dosing!ideally!should!be!guided!by!TPMT!level!!!
- With!food!to!reduce!gastric!upset!!
Formulations! - Oral:!25,!50,!75,!100!mg!
Contraindications - Absolute:!
Pregnancy,!hypersensitivity!to!azathioprine,!and!active!infections!
- Relative:!
Allopurinol!use!(need!to!reduce!dose!of!azathioprine),!prior!use!of!alkylating!agents!
(increased!malignancy!risk),!very!low!level!of!TPMT.!
Special!situations - Pregnancy!category!D!(teratogenic)!
- Excreted!in!breast!milk!and!mothers!should!not!breastfeed!
- Avoid!live!vaccinations!!
Drug!interactions - Check!for!possible!drug!interactions.!
Monitoring - Baseline:!
a. Clinical!assessment:!
- Discuss!the!risk/benefit!profile!and!adverse!effects!
- Discuss!alternative!treatments!and!frequency!of!monitoring!
- Sun!avoidance!and!birth!control/abstinence!if!child!bearing!female!
- History!of!alkylating!agents!or!current!use!of!allopurinol/febuxostat!
- Physical!examination!with!focus!on!skin!and!lymphoreticular!system!
b. Labs!
- Pregnancy!test!!
- CBC,!BUN,!Cr,!GFR,!electrolytes,!LFTs!
! If!GFR!<10!ml/min!reduce!dose!by!50%!of!AZA!
! If!GFR!10V50!ml/min!reduce!dose!by!25%!of!AZA!
- Urine!analysis!
- Quantiferron!TB/PPD+/V!CXR,!Hepatitis!B!&!C!serology,!HIV!if!at!risk!!
- TPMT!assay:!If!unavailable;!monitor!hematologic!parameters!closely!
- Follow!up! !
a. Clinical!assessment:!!
- Annual!complete!physical!examination!with!particular!attention!to!possible!
lymphoma!and!squamous!cell!carcinoma!!
- Age!appropriate!cancer!screening!
b. Labs!
- q!2!weeks!for!the!first!2!months,!then!every!2V3!months!if!stabke!
- CBC!with!differential!
! WBC!<3500V4000,!Hgb!<10,!Plts!<100,000!"!stop!treatment!
- LFTs!(AST!and!ALT)!
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Adverse!effects! - Malignancies:!cutaneous!SCC,!lymphomas!
- Myelosuppression!(correlates!with!low!TPMT!activity):!neutropenia,!agranulocytosis,!
pancytopenia!(rarely)!
- Infections:!HPV,!HSV,!scabies,!true!opportunistic!infections!uncommon!
- Teratogenicity!!
- Hypersensitivity!syndrome:!morbilliform,!purpura,!erythema!multiforme,!urticaria,!
angioedema,!erythema!nodosum!!
- Gastrointestinal:!gastritis,!pancreatitis!
- Hepatic:!transaminase!elevations,!severe!hepatocellular!toxicity!(rare)!
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MYCOPHENOLATE!MOFETIL!(CELLCEPT)!!
Dose!&!regimen! - Initial!dose:!500!mg!BID!
- Maintenance!dose:!!
- If!no!improvement!after!1!month,!increase!dose!to!1!gm!BID!can!be!
increased!to!maximum!1.5!gm!BID.!
Formulations! - Oral:!250!mg!capsules!and!500!mg!tablets!
Contraindications! - Absolute:!
Pregnancy!(teratogenic),!hypersensitivity!to!MMF!
- Relative:!
Lactation!(may!be!excreted!in!breast!milk),!peptic!ulcer!disease,!hepatic/renal!
disease!(may!need!to!reduce!dose),!cardiopulmonary!disease,!drugs!that!interfere!
with!enterohepatic!circulation!(cholestyramine),!azathioprine!(increased!risk!of!
bone!marrow!suppression),!recent!live!vaccinations.!
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Special!situations! - Pregnancy!category!D!(teratogenic)!
- Females!of!childbearing!age!should!have!effective!contraception!4!weeks!
prior!to!therapy!and!for!6!weeks!following!discontinuation!of!therapy!
- Excreted!in!breast!milk!and!mothers!should!not!breastfeed.!!
Drug!interactions! - Check!for!possible!drug!interactions.!
Monitoring!! ! - Baseline:!
a. Clinical!assessment:!
Careful!history!and!physical!examination!!
b. Labs!
- CBC!with!differential!and!platelet!
- Creatinine,!BUN!and!electrolytes!
- LFTs!
- Hepatitis!B!and!C,!PPD/Quantiferon!TB!+/V!CXR,!HIV!ag/ab.!!!
- Pregnancy!test!!
- Follow!up:! !
a. Clinical!assessment:!!
- Complete!physical!examination!every!3V6!months!(to!exclude!
malignancy,!lymphadenopathy,!breast!lumps,!organomegaly)!!
d. Labs!
- Lab!surveillance!every!2V4!weeks!following!dose!escalation!and!every!
2V3!months!once!dose!is!stable!!
- CBC!with!differential!and!platelet!count!
- Serum!creatinine!and!electrolytes!
- LFTs!
Adverse!effects!! - Carcinogenic:!lymphoproliferative!disorders,!nonVmelanoma!skin!cancer!
- Gastrointestinal:!doseVdependent!(most!common),!nausea,!diarrhea,!soft!
stools,!anorexia,!abdominal!cramps,!vomiting,!anal!tenderness!
- Genitourinary:!urgency,!frequency,!dysuria,!burning,!sterile!pyuria!
- Infectious;!viral,!bacterial,!atypical!mycobacterial,!fungal!(>transplant!
patients),!progressive!multifocal!leukoencephalopathy.!
- Neurologic!effects:!weakness,!fatigue,!headache,!tinnitus,!insomnia!
- Hematologic:!doseVdependent!(reversible),!neutropenia,!anemia,!
thrombocytopenia,!agranulocytosis,!neutrophil!dysplasia!
- Teratogenicity:!first!trimester!loss,!external!ear/facial!abnormalities,!
anomalies!of!distal!limbs,!heart,!esophagus,!and!kidneys.!
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ADALIMUMAB!(HUMIRA)!
Dose!&!regimen - Initial!dose:!80!mg!week!0,!40!mg!week!1,!no!dose!week!2!
- Maintenance!dose:!!40!mg!every!2!weeks!!
Formulations! - Subcutaneous:!40!mg!stored!in!a!refrigerator!!
Contraindications - Absolute:!
Avoid!with!active!infections,!chronic!or!localized!infections!(including!TB),!
hypersensitivity!to!adalimumab!,!and!concurrent!administration!with!
anakinra!(ILV1!receptor!antagonist)!
- Relative:!
a. Family!history!of!demyelinating!disease!(including!MS)!!
b. Congestive!heart!failure!(especially!class!III!or!IV).!
Special!situations - Pregnancy!category!B!
- Excreted!very!low!level!in!breast!milk!
- Avoid!live!vaccinations,!
Drug!interactions - Drugs!that!increase!risk!of!infection;!ILV1!receptor!antagonist!
!Monitoring - Baseline:!
a. Clinical!assessment!!
- Complete!history!and!physical!examination!
- Focus!on!history/risk/symptoms!of!TB!and!other!infections,!malignancy,!
neurologic!disorders,!congestive!heart!failure!
b. Labs!
- CBC!with!platelet!count!
- CMP!(UE!&!LFTs)!
- Hepatitis!B!&!C!serology,!HIV!if!at!risk!!
- Quantiferon!TB/PPD,!+/V!CXR!!
- +/V!baseline!ANA!
- Follow!up! !
a. Labs!
- Follow!up!CBC!and!CMP!q!3!months,!and!then!every!6V12!months!
- Annual!TB!testing!!
Adverse!effects! - Injection!site!reactions!(erythema,!swelling,!localized!itching)!
- Antidrug!antibodies!
- Malignancy!risk;!lymphoma?!skin!cancer?!
- Infections:!reactivation!of!latent!TB,!invasive!fungal!infections,!hepatitis!B!
reactivation!!
- Neurological!disease:!demyelinating!diseases!!
- Congestive!heart!failure!!!
- Autoimmunity!(induction!of!ANA!and!antiVdsDNA,!drug!induced!lupus)!
- Hematologic!toxicity!(rare!reports)!
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Dose!&!regimen!
Formulations!!
Contraindications!
Special!situations!
Drug!interactions!
Monitoring!! ! -
Adverse!effects!!
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ETANERCEPT!(ENBREL)!!
- Initial!dose:!50!mg!twice!weekly!for!12!weeks!
- Maintenance!dose:!!!
50!mg!once!weekly!or!25!mg!once!weekly!or!50!mg!every!2!weeks!!
- Subcutaneous!25!mg!or!50!mg!stored!in!refrigerator!(allow!to!return!to!
room!temperature!for!15!minutes)!!
- Absolute:!
Avoid!with!active!infections,!chronic/localized!infections!(including!TB),!
hypersensitivity!to!etanercept,!concurrent!administration!with!anakinra!(ILV1!
receptor!antagonist)!
- Relative:!
Family!history!of!demyelinating!disease!(including!MS),!congestive!heart!
failure!(especially!class!III!or!IV)!
- Pregnancy!category!B!
- Excreted!very!low!level!in!breast!milk!
- Avoid!live!vaccinations!(2!weeks!prior,!during,!and!for!6!months!after)!
- Children:!used!in!2V17!years!for!juvenile!idiopathic!arthritis.!
- Drugs!that!increase!risk!of!infection;!ILV1!receptor!antagonist!
Baseline:!
a. Clinical!assessment!!
- Complete!history!and!physical!examination!
- Focus!on!history/risk/symptoms!of!TB!and!other!infections,!
malignancy,!neurologic!disorders,!congestive!heart!failure!
b. Labs!
- CBC!with!platelet!count!
- CMP!(LFTs,!Urea,!Cr,!and!Electrolytes)!
- Hepatitis!B!&!C!serology,!HIV!if!at!risk!!
- Quantiferon!for!TB/PPD!+/V!CXR!!
- +/V!baseline!ANA!
- Follow!up! !
c. Labs!
- CBC,!BUN,!Cr,!and!LFT!in!2V3!months,!and!then!every!6V12!months!
- Annual!TB!testing!
- Injection!site!reactions!(erythema,!swelling,!localized!itching)!
- Antidrug!antibodies!
- Malignancy!risk:!Lymphoma?!skin!cancer?!
- Infections:!reactivation!of!latent!TB,!invasive!fungal!infections,!hepatitis!B!
reactivation!!
- Neurological!disease:!demyelinating!diseases!
- Congestive!heart!failure!!
- Autoimmunity!(induction!of!ANA!and!antiVdsDNA,!drug!induced!lupus)!
- Hematologic!toxicity!(rare!reports)!
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Dose!&!regimen!
Formulations!!
Contraindications!
Special!situations!!
Drug!interactions!
Monitoring!! ! -
Adverse!effects!
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DAPSONE!
- Dose:!50V200!mg/day!
- Oral!25,!100!mg!tablets!!
- Absolute:!
Prior!hypersensitivity!to!dapsone,!including!agranulocytosis!and!
hypersensitivity!syndrome.!
- Relative:!
G6PD!deficiency,!allergy!to!sulfonamide!antibiotics,!significant!
cardiopulmonary!disease,!significant!liver!or!renal!function!
impairment,!preVexisting!peripheral!neuropathy!
- Pregnancy!category!C!
- Can!be!secreted!in!breast!milk!and!rarely!cause!hemolytic!anemia!in!
infants!breastfeeding!from!mothers!on!dapsone!
- Check!for!possible!drug!interactions.!!!
Baseline:!
a. Clinical!assessment:!
- Complete!history!and!physical!with!emphasis!on!
cardiopulmonary,!gastrointestinal,!neurologic,!and!renal!signs.!
b. Labs!!
- CBC!with!diff!
- LFTs,!!BUN,!Creatinine,!and!electrolytes!
- Urinalysis!
- GlucoseV6Vphosphate!dehydrogenase!level!(G6PD)!
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- FollowRup:!
a. Clinical!assessment:!
- Each!visit!reassess!peripheral!motor!neurologic!examination!
- Each!visit!assess!for!signs/symptoms!of!methemoglobinemia!
(i.e.!headache,!SOB,!lethargy,!and!bluish!discoloration!of!lips!
and!finger!tips).!
- Question!for!any!other!significant!adverse!effects!!
b. Laboratory!!
- CBC!with!diff!q1!week!for!4!weeks,!q!2!weeks!until!week!12,!
then!q!3–4!months!
- Reticulocyte!count!if!anemia!develops!(hemolysis)!
- LFTs,!renal!function,!and!urine!analysis!q!3–4!months!!!
- Methemoglobin!levels!as!clinically!indicated!
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Pharmacologic:!!
- Hemolytic!anemia;!SOB,!angina,!fatigue!and!jaundice!!
- Methemoglobinemia!(headache,!lethargy)!
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Idiosyncratic:!
- Hematologic!(leukopenia,!agranulocytosis);!purpura,!bleeding,!sore!
throat,!mouth!ulcers.!!
- Hepatic!(hepatitis,!infectious!mononucleosisVlike!syndrome,!cholestatic!
jaundice,!hypoalbuminemia)!
- Cutaneous!hypersensitivity!reactions!(morbilliform!eruption,!
exfoliative!erytherodema,!toxic!epidermal!necrolysis)!
- Gastrointestinal!(gastric!irritation!with!nausea,!anorexia)!
- Neurologic!and!psychiatric!(psychosis,!peripheral!neuropathy)!
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Dose!&!regimen!
Formulations!!
Contraindications!
Special!situations!
Drug!interactions!
Monitoring!! ! -
Adverse!effects!
! !
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COLCHICINE!
- Dose:!0.5!or!0.6!mg!qd/bid/tid!
- Tablet!0.5V0.6!mg!
- Must!be!shielded!from!light!(degraded!by!UVR)!
- Absolute:!
Hypersensitivity!to!colchicine!
Blood!dyscrasias!
- Relative:!
‘Serious’!GI,!renal,!hepatic,!or!cardiac!disorders!
- Pregnancy!category!C!!(parenteral!forms!category!D)!
- Extruded!in!breast!milk.!
- Check!for!possible!drug!interactions.!!!
Baseline:!!
- CBC!w!diff!
- CMP!(LFTs,!Cr,!BUN,!and!electrolytes)!!
- Urine!analysis!
- Follow!up:!
- CBC!w!diff,!CMP,!and!urine!analysis!q!3!months.!!
- Monthly!lab!monitoring!for!the!first!few!months.!
- GI!effects!(doseVrelated):!!
Abdominal!cramping,!hyper!peristalsis,!and!watery!diarrhea!(diarrhea!
can!be!controlled!with!aluminumVcontaining!antiVacids!or!antidiarrheal!
medication!such!as!loperamide).!
- Colchicine!overdose:!
CholeraVlike!syndrome!with!dehydration,!hypokalemia,!hyponatremia,!
metabolic!acidosis,!renal!failure,!and!shock.!!!
Respiratory!distress!syndrome,!DIC,!and!BM!failure.!
Hepatic!failure,!and!late!CNS!disorders.!
Myopathy,!hypocalcemia,!alopecia,!stomatitis,!and!PCT!in!acutely!
intoxicated!patients!who!survived.!!
- Chronic!intoxication!after!prolonged!therapy!with!at!least!1!mg!daily.!
Complications!include!leukopenia,!aplastic!anemia,!myopathy,!alopecia.!
- Azospermia!&!megaloblastic!anemia!secondary!to!vitamin!B12!
malabsorption!have!been!reported.!!
 SYSTEMIC!RETINOIDS!
Dose!&!regimen! - Isotretnoin:0.5–2!mg/kg/day!
Acne:!0.5V1mg/kg/day!until!a!total!cumulative!dose!of!120V150!mg/kg.!
Rosacea:!low!dose!10V20!mg!per!day!
- Acitretin:!25–50!mg/day!!
Formulations!! - Oral!!(tablets)!
Contraindications! - Absolute:!pregnancy/plan!to!become!pregnant,!contraception!nonV
compliance,!nursing,!parabens!hypersensitivity!(isotretinoin!capsules).!
- Relative:!Leukopenia,!hypothyroidism!(bexarotene),!moderateVsevere!
cholesterol/TG!elevation,!significant!hepatic/renal!dysfunction!
Cautions!! - Pregnancy!category!X!,!contraindicated!in!lactation!
- Isotretnoin!requires!contraception!for!1!month!prior!to!starting!and!1!
month!after!stopping.!!
- Acitretin!requires!contraception!for!1Vmonth!prior!and!3!years!after!
stopping.!
- Patients!shouldn’t!donate!blood!for!1!month!after!isotrenoin!and!3!
years!after!acitretin.!
Drug!interactions! - Please!check!possible!drug!interactions.!
- Concomitant!vitamin!A!should!be!limited!<5000!IU!daily.!!
Monitoring!! ! - Baseline:!
- Clinical!assessment:!!
- Careful!history!and!physical!examination!
- Identify!those!patients!at!high!risk!for!toxicity/adverse!effects!
- Document!concomitant!drugs!that!may!interact!with!retinoids.!
- Labs:!
- Pregnancy!test!(2!tests!should!be!negative!prior)!!
- CBC,!LFTs,!fasting!lipid!panel,!renal!function!tests!
- +/V!Urinalysis!(if!renal!disease/proteinuria/DM/HTN).!!
- Special!tests:!
- Consider!baseline!XVrays!of!wrists,!ankles!or!thoracic!spine!if!
plan!longVterm!retinoid!therapy!
- Consider!optha!exam!if!hx!of!cataracts!or!retinopathy!
- Follow!up! !
a. Clinical!assessment:!
- Clinical!evaluation!q1month!for!3–6!months,!then!q!3!months!
- Assessment!of!response,!improvement,!and!adverse!effects!!
- Routine!physical!examination!of!lesional!skin!!
b. Labs:!
- Monthly!for!the!first!3V6!months,!then!every!3!months!
- LFTs!
! LFTs!>2V3x!withdraw!until!normalization!
! LFTs>3x!discontinue!!
- Fasting!lipid!panel!
! TG!>300!mg/dl!“3.39!mmol/l!weight,!diet,!and!exercise!
! TG!>500!mg/dl!“5.65!mmol/l”!reduce!dose,!LLA,!monitor!closely!
! TG!>!800!“9.04!mmol/l”!pancreatitis!risk,!discontinue.!!!
- CBC!&!UE!tests!with!every!other!time!the!lab!is!done!
- Pregnancy!test!q!1!month!for!women!of!childbearing!potential!
c. Other!investigations:!
- Periodically!as!indicated!by!symptoms!!
! Annual!XVrays!of!wrists,!ankles!or!thoracic!spine!with!
longVterm!retinoid!therapy!if!symptomatic.!!
! Radiography!of!symptomatic!joints!with!longVterm!tx!!
! Ophthalmologic!exam!if!patients!report!visual!changes!
Adverse!effects!! - Teratogenicity:!Retinoic!acid!embryopathy,!spontaneous!abortions.!
- Ocular:!reduced!night!vision,!dry!eyes,!and!staph!aureus!infections.!!
- MSK:!Diffuse!skeletal!hyperostosis,!osteophyte!formation,!and!
premature!epiphyseal!closure,!arthralgia!and!myalgia!
- Lipids:!hypercholesterolemia,!hypertriglyceridemia!
- GI:!IBD!flare,!Pancreatitis!(↑!TG),!high!LFTs.!
- Neurologic!/psychiatric:!pseudotumor!cerebri,!headache,!depression,!
psychosis,!and!suicidal!ideation.!
- Mucocutaneous:!dryness,!nail!fragility,!and!alopecia.!
- Others:!hematologic,!diabetes!mellitus!(controversial)!!