Dosing & Uses
Dosage Forms & Strengths
capsule
- 10mg (Absorica, Amnesteem, Claravis, Myorisan, Zenatane)
- 20mg (Absorica, Amnesteem, Claravis, Myorisan, Zenatane)
- 25mg (Absorica)
- 30mg (Absorica, Claravis, Zenatane)
- 35mg (Absorica)
- 40mg (Absorica, Amnesteem, Claravis, Myorisan, Zenatane)
capsule, micronized (Absorica LD)
- 8mg
- 16mg
- 20mg
- 24mg
- 28mg
- 32mg
Severe, Recalcitrant Nodular Acne
Indicated for severe nodular acne in nonpregnant patients who are unresponsive to conventional therapy, including systemic antibiotics
Micronized capsules: 0.4-0.8 mg/kg day PO divided BID for 15-20 weeks
Conventional capsules
- 0.5-1 mg/kg/day PO divided BID for 15-20 weeks
- Adults whose disease is very severe with scarring or is primarily manifested on the trunk may require dose up to 2 mg/kg/day (as tolerated)
Dosing Considerations
>2 months after discontinuation: if warranted by persistent or recurring, severe nodular acne, may initiate a second course of therapy
If total nodule count reduced by >70% before completing 15-20 weeks, may discontinue drug
Dosage Forms & Strengths
capsule
- 10mg (Absorica, Amnesteem, Claravis, Myorisan, Zenatane)
- 20mg (Absorica, Amnesteem, Claravis, Myorisan, Zenatane)
- 25mg (Absorica)
- 30mg (Absorica, Claravis, Zenatane)
- 35mg (Absorica)
- 40mg (Absorica, Amnesteem, Claravis, Myorisan, Zenatane)
capsule, micronized (Absorica LD)
- 8mg
- 16mg
- 20mg
- 24mg
- 28mg
- 32mg
Severe, Recalcitrant Nodular Acne
Indicated for severe nodular acne in nonpregnant patients who are unresponsive to conventional therapy, including systemic antibiotics
<12 years: Safety and efficacy not established
Aged 12 years or older
- Capsules: 0.5-1 mg/kg/day PO divided BID for 15-20 weeks
- Micronized capsules: 0.4-0.8 mg/kg day PO divided BID for 15-20 weeks
Dosing Considerations
>2 months after discontinuation: if warranted by persistent or recurring, severe nodular acne, may initiate a second course of therapy
If total nodule count reduced by >70% before completing 15-20 weeks, may discontinue drug
Ichthyosis (Orphan)
Orphan designation for treatment of congenital ichthyosis
Orphan sponsor
- Patagonia Pharmaceuticals, LLC; 50 Tice Blvd, Suite A35; Woodcliff Lake, NJ 07677
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious - Use Alternative (18)
- aminolevulinic acid oral
aminolevulinic acid oral, isotretinoin. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.
- aminolevulinic acid topical
isotretinoin, aminolevulinic acid topical. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Each drug may increase the photosensitizing effect of the other.
- brexucabtagene autoleucel
isotretinoin, brexucabtagene autoleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- ciltacabtagene autoleucel
isotretinoin, ciltacabtagene autoleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- demeclocycline
isotretinoin, demeclocycline. Mechanism: unknown. Contraindicated. Risk of pseudotumor cerebri.
- doxycycline
isotretinoin, doxycycline. Mechanism: unknown. Contraindicated. Risk of pseudotumor cerebri.
- idecabtagene vicleucel
isotretinoin, idecabtagene vicleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- lisocabtagene maraleucel
isotretinoin, lisocabtagene maraleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- methyl aminolevulinate
isotretinoin, methyl aminolevulinate. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Each drug may increase the photosensitizing effect of the other.
- minocycline
isotretinoin, minocycline. Mechanism: unknown. Contraindicated. Risk of pseudotumor cerebri.
- omadacycline
isotretinoin increases toxicity of omadacycline by Mechanism: unknown. Avoid or Use Alternate Drug. Concomitant use of oral retinoids with tetracyclines may increase risk of pseudotumor cerebri/intracranial hypertension. .
- oxytetracycline
isotretinoin, oxytetracycline. Mechanism: unknown. Contraindicated. Risk of pseudotumor cerebri.
- palifermin
palifermin increases toxicity of isotretinoin by Other (see comment). Avoid or Use Alternate Drug. Comment: Palifermin should not be administered within 24 hr before, during infusion of, or within 24 hr after administration of antineoplastic agents. Coadministration of palifermin within 24 hr of chemotherapy resulted in increased severity and duration of oral mucositis.
- palovarotene
isotretinoin, palovarotene. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Vitamin A in doses higher than the recommended daily allowance and/or other oral retinoids coadministered with palovarotene increases risk of hypervitaminosis A. .
- sarecycline
isotretinoin increases toxicity of sarecycline by Mechanism: unknown. Avoid or Use Alternate Drug. Concomitant use of oral retinoids with tetracyclines may increase risk of pseudotumor cerebri/intracranial hypertension. .
- tetracycline
isotretinoin, tetracycline. Mechanism: unknown. Contraindicated. Risk of pseudotumor cerebri.
- tisagenlecleucel
isotretinoin, tisagenlecleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- valoctocogene roxaparvovec
isotretinoin decreases effects of valoctocogene roxaparvovec by pharmacodynamic antagonism. Avoid or Use Alternate Drug. An in vitro study in human primary hepatocytes indicated that efavirenz suppressed factor VIII transcription independent of hepatotoxicity, and expression was not restored upon discontinuation of efavirenz. One HIV positive patient treated with valoctocogene roxaparvovec while on an antiretroviral therapy (ART) regimen consisting of efavirenz, lamivudine, and tenofovir experienced asymptomatic elevations of ALT, AST, and GGT and serum bilirubin at Week 4. The reaction resolved after the ART regimen was changed to a regimen without efavirenz. The patient later reverted to prophylactic use of factor VIII concentrates.
Monitor Closely (10)
- cannabidiol
cannabidiol will increase the level or effect of isotretinoin by decreasing metabolism. Modify Therapy/Monitor Closely. Cannabidiol may potentially inhibit CYP2C8 activity. Consider reducing the dose when concomitantly using CYP2C8 substrates.
- methotrexate
methotrexate, isotretinoin. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Patients receiving other agents that may cause hepatotoxicity, including systemic retinoids, could be at increased risk of liver-related side effects of methotrexate and such patients should be monitored closely during methotrexate therapy.
- mifepristone
mifepristone will increase the level or effect of isotretinoin by Other (see comment). Use Caution/Monitor. Inhibits CYP2C8/2C9; use smallest recommended doses for substrates and monitor
- mipomersen
mipomersen, isotretinoin. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- omaveloxolone
omaveloxolone will decrease the level or effect of isotretinoin by Other (see comment). Use Caution/Monitor. Omaveloxolone may reduce systemic exposure of sensitive CYP2C8 substrates. Check prescribing information of substrate if dosage modification is needed.
- stiripentol
stiripentol will increase the level or effect of isotretinoin by Other (see comment). Modify Therapy/Monitor Closely. Stiripentol is a CYP2C8 inhibitor. Consider dosage reduction for CYP2C8 substrates if adverse effects are experienced when coadministered.
- tecovirimat
tecovirimat will increase the level or effect of isotretinoin by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. Tecovirimat is a weak inhibitor of CYP2C8 and CYP2C19. Monitor for adverse effects if coadministered with sensitive substrates of these enzymes.
- teriflunomide
teriflunomide increases levels of isotretinoin by Other (see comment). Use Caution/Monitor. Comment: Teriflunomide inhibits CYP2C8; caution when coadministered with CYP2C8 substrates.
- tobramycin inhaled
tobramycin inhaled and isotretinoin both increase nephrotoxicity and/or ototoxicity. Modify Therapy/Monitor Closely. Avoid concurrent or sequential use to decrease risk for ototoxicity
- vitamin A
isotretinoin increases toxicity of vitamin A by pharmacodynamic synergism. Use Caution/Monitor. (Vitamin A) Additive retinoid effects.
Minor (13)
- calcium acetate
isotretinoin increases levels of calcium acetate by enhancing GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown.
- calcium carbonate
isotretinoin increases levels of calcium carbonate by enhancing GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown.
- calcium chloride
isotretinoin increases levels of calcium chloride by enhancing GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown.
- calcium citrate
isotretinoin increases levels of calcium citrate by enhancing GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown.
- calcium gluconate
isotretinoin increases levels of calcium gluconate by enhancing GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown.
- carbamazepine
isotretinoin decreases levels of carbamazepine by increasing renal clearance. Minor/Significance Unknown.
- ciprofloxacin
ciprofloxacin, isotretinoin. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Both drugs have increased risk of phototoxicity, use caution with concomitant use.
- fleroxacin
fleroxacin, isotretinoin. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Increased phototoxicity.
- food
food increases levels of isotretinoin by enhancing GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown.
- gemifloxacin
gemifloxacin, isotretinoin. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Increased phototoxicity.
- levofloxacin
levofloxacin, isotretinoin. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Increased phototoxicity.
- moxifloxacin
moxifloxacin, isotretinoin. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Increased phototoxicity.
- ofloxacin
ofloxacin, isotretinoin. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Increased phototoxicity.
Adverse Effects
>10%
Cheilitis (90%)
Xerosis
Xerostomia
Dry nose
Epistaxis
Pruritus
Conjunctivitis (including blepharoconjunctivitis) (40%)
Irritation (40%)
Increased erythrocyte sedimentation rates (40%)
Thinning of hair (which has persisted in rare instances)
Palmoplantar desquamation
Skin fragility
Skin infections (eg, paronychial infections)
Rash (including erythema, seborrhea, eczema), photosensitivity
Hypertriglyceridemia (25%)
Bone or joint pain
Generalized muscle aches
Arthralgia
Decreased HDLs (15%)
Increased LFTs (15%)
Increased CPK (12-24%)
Decreased hemoglobin concentration and hematocrit
Decreased erythrocyte and leukocyte counts
Increased platelet count
1-10%
Decreased bone mineral density (8.8%)
Premature epiphyseal closure (3%)
Frequency Not Defined
Lethargy
Fatigue
Headache
Anorexia
Nausea
Vomiting
Increased appetite
Thirst
Postmarketing Reports
Reproductive system: Abnormal menses and sexual dysfunction, including erectile dysfunction, decreased libido, decreased vaginal lubrication, and vaginal dryness
Warnings
Black Box Warnings
Embryofetal toxicity
- Do not use in female patients who are or may become pregnant, because therapy poses an extremely high risk for severe birth effects (with any dose or duration)
- Documented embryofetal effects include internal and external abnormalities, IQ scores of <85, spontaneous abortion, premature birth, and fetal death
- Documented external abnormalities include skull abnormality, ear abnormalities (including anotia, micropinna, small or absent external auditory canals), eye abnormalities (including microphthalmia), facial dysmorphia, and cleft palate
- Documented internal abnormalities include CNS abnormalities (including cerebral abnormalities, cerebellar malformation, hydrocephalus, microcephaly, cranial nerve deficit), cardiovascular abnormalities, thymus gland abnormality, and parathyroid hormone deficiency
- Discontinue immediately if pregnancy occurs and refer patient to an obstetrician-gynecologist experienced in reproductive toxicity for evaluation
- Potentially any fetus exposed during pregnancy can be affected, but there are no accurate methods to determine whether an exposed fetus has been affected
Restricted distribution program
- Prescribers must register with iPLEDGE, an FDA-approved risk management program designed to minimize pregnancy exposures to isotretinoin (enhancement of earlier riskMAP [risk minimization action plan]); patients must be registered and meet all requirements of iPLEDGE
- Pharmacies that dispense drug must be registered and activated with iPLEDGE, must only dispense to patients who are authorized to receive drug, and agree to comply with the REMS requirements described in the booklet entitled Pharmacist Guide, specifically the “Key Information for Pharmacists” section including the following dispensing information:
- Prescriptions must be obtained no later than the “Do Not Dispense To After” date, and if not obtained, then the RMA must be reversed in the iPLEDGE Program system and the product returned to inventory
- Patients of childbearing potential must not be pregnant or breastfeeding, must be capable of complying with approved contraceptive methods, and must be reliable in following instructions
Contraindications
Pregnancy (see Black Box Warnings)
Hypersensitivity to isotretinoin or vitamin A
Cautions
Significant adverse effects are associated with isotretinoin use
Neutropenia and agranulocytosis (rare) reported; discontinue if white cell counts decrease significantly
Embryofetal toxicity; major congenital malformations, spontaneous abortions, and premature births documented (see Black Box Warnings)
Do not donate blood during therapy and for 1 month after discontinuing treatment, because of embryofetal toxicity risk
Restricted distribution program (iPLEDGE), a risk management program to minimize pregnancy exposure, has been implemented (see Black Box Warnings)
Microdosed, progesterone-only preparations (‘minipills’) are an inadequate method of contraception during treatment
Pseudotumor cerebri reported; some reports involved concomitant tetracycline use; concomitant treatment with tetracyclines should be avoided; early signs and symptoms of intracranial hypertension include papilledema, headache, nausea and vomiting, and visual disturbances; screen patients with these symptoms for papilledema and, if present, discontinue therapy immediately and refer patient to a neurologist for further diagnosis and care
Serious skin reactions reported (eg, Stevens-Johnson syndrome, toxic epidermal necrolysis); discontinue therapy if skin reaction occurs
Acute pancreatitis reported with either elevated or normal serum triglyceride levels, including rare instances of fatal hemorrhagic pancreatitis; discontinue if unable to control hypertriglyceridemia; discontinue therapy if pancreatitis occurs
Increased triglycerides and total cholesterol levels reported; whereas, decreased HDL-cholesterol reported
Hearing impairment reported and may persist after discontinuing therapy; patients who experience tinnitus or hearing impairment should discontinue treatment and be referred for specialized care for further evaluation
Hepatitis may occur; mild to moderate liver enzymes elevations also reported; some normalized with dosage reduction or continued administration of drug’ if normalization does not readily occur or if hepatitis is suspected during treatment, therapy should be discontinued
Associated with inflammatory bowel disease (including regional ileitis); discontinue immediately if abdominal pain, rectal bleeding, or severe diarrhea occurs
Negative effect on bone mineral density reported; caution with childhood osteoporosis, osteomalacia, chronic corticosteroid use, or anorexia nervosa
Musculoskeletal symptoms, including arthralgia and rhabdomyolysis may occur; consider discontinuing therapy if any significant abnormality found
Skeletal hyperostosis observed in clinical trial for keratinization disorders
Avoid prolonged exposure to uv rays or sunlight
Premature epiphyseal closure reported spontaneously with normal doses
Ocular abnormalities observed, including corneal opacities, decreased night vision, and dry eye; discontinue therapy in patients experiencing visual difficulties
Hypersensitivity reactions (eg, anaphylactic, cutaneous, allergic vasculitis) reported; severe allergic reaction requires discontinuation and medical management
Healthcare providers should be alert to warning signs of psychiatric disorders to help ensure patients receive help they need (Prescribers should read the brochure, Recognizing Psychiatric Disorders in Adolescents and Young Adults: A Guide for Prescribers of Isotretinoin)
Use caution in diabetes mellitus; impaired glucose control reported
Patients in early and late adolescence who participate in sports with repetitive impact may be at an increased risk of spondylolisthesis with and without pars fractures, and hip growth plate injuries reported
Psychiatric effects
- Depression and psychosis reported; rare reports of suicidal ideation, suicide attempts, suicide, and aggressive and/or violent behaviors
- Prior to initiation of therapy, patients and family members should be asked about any history of psychiatric disorder, and at each visit during therapy patients should be assessed for symptoms of depression, mood disturbance, psychosis, or aggression to determine if further evaluation is necessary
- Patients should immediately stop therapy and the patient (or caregiver) should promptly contact their prescriber if patient develops depression, mood disturbance, psychosis, or aggression
- Discontinuation of treatment may be insufficient; further evaluation may be necessary such as a referral to a mental healthcare professional
Laboratory monitoring
- Pretreatment monitoring: LFTs (1 day before starting initiating therapy), 2 pregnancy tests (negative result 2 weeks before), and fasting lipid profile (including triglycerides)
- During treatment: Monitor LFTs and lipids at weekly or biweekly intervals until response to isotretinoin established
- Blood glucose, CPK (particularly in those undergoing vigorous physical activity)
- Ongoing negative pregnancy tests required according to iPLEDGE rules
Pregnancy & Lactation
Preganacy
Therapy is contraindicated during pregnancy; it can cause fetal harm when administered to a pregnant patient; there is increased risk of major congenital malformations, spontaneous abortions, and premature births following isotretinoin exposure during pregnancy in humans; there is extremely high risk of life-threatening birth defects that will result if pregnancy occurs while taking any amount of this drug even for short periods of time
If drug is used during pregnancy, or if patient becomes pregnant while receiving therapy, patient should be apprised of potential hazard to a fetus
If pregnancy occurs during treatment of patient receiving therapy, it must be discontinued immediately and patient should be referred to Obstetrician-Gynecologist experienced in reproductive toxicity for further evaluation and counseling
If a pregnancy occurs during treatment, discontinue therapy immediately and refer patient to obstetrician/gynecologist experienced in reproductive toxicity for further evaluation and counseling; any suspected fetal exposure during or 1 month after initiating therapy must be reported immediately to the FDA via MedWatch telephone number 1-800-FDA-1088, and also to the iPLEDGE pregnancy registry at 1-866-495-0654 or via the internet (www.ipledgeprogram.com)
Contraception
- Patients who can become pregnant must use 2 forms of contraception simultaneously, at least 1 of which must be a primary form, for at least 1 month prior to initiation of therapy, during therapy, and for 1 month after discontinuing therapy; however, 2 forms of contraception is not required if the patient commits to continuous abstinence from not having any sexual contact with a partner which may result in pregnancy, has undergone a hysterectomy or bilateral oophorectomy, or has been medically confirmed to be post-menopausal
- Micro-dosed progesterone preparations (“minipills” that do not contain estrogen) are an inadequate method of contraception during therapy.
- Any birth control method can fail; there have been reports of pregnancy from patients who have used combination oral contraceptives, as well as contraceptive vaginal systems, vaginal inserts, transdermal systems, and injections; these pregnancies occurred while taking isotretinoin
- It is critically important that patients who can become pregnant use 2 methods of contraception simultaneously
- A clinical drug interaction study did not show any clinically significant interaction between isotretinoin and norethindrone and ethinyl estradiol; however, it is not known if there is an interaction between isotretinoin with other progestins
- Prescribers are advised to consult the prescribing information of any medication administered concomitantly with hormonal contraceptives, since some medications may decrease effectiveness of these birth control products
- Patients who can become pregnant should be prospectively cautioned not to self-medicate with herbal supplement St. John’s Wort because of a possible interaction with hormonal contraceptives based on reports of breakthrough bleeding on oral contraceptives shortly after starting St. John’s Wort; pregnancies have been reported by users of combined hormonal contraceptives who also used some form of St. John’s Wort
- If patient has unprotected sexual contact with a partner that could result in pregnancy at any time 1 month before, during, or 1 month after therapy, the patient must: Stop taking therapy immediately
-
If had unprotected sexual contact and on therapy
- Have a pregnancy test at least 19 days after the last act of unprotected sexual contact with a partner that could result in pregnancy
- Start using 2 forms of contraception simultaneously again for 1 month before resuming therapy
- Have a second pregnancy test after using 2 forms of contraception for 1 month
Reproductive Potential
- Must only be prescribed to patients who are known not to be pregnant as confirmed by a negative CLIA-certified laboratory conducted pregnancy test; patients who can become pregnant must have had two negative urine or serum pregnancy tests with a sensitivity of at least 25 mIU/mL before receiving the initial therapy (the interval between the two tests must be at least 19 days)
- The first test (a screening test) is obtained by the prescriber when the decision is made to prescribe therapy
Therapy is available only through a restricted program under a REMS called the iPLEDGE REMS because of the risk of embryo-fetal toxicity
Under REMS, prescribers must be certified with the program and comply with the following requirements
- Determine reproductive status of all patients prior to initiating treatment;
- Provide contraception counseling to patients who can get pregnant prior to and during treatment, or refer patients who can get pregnant to an expert for such counseling
- Provide scheduled pregnancy testing, and verify and document negative pregnancy test result prior to writing each prescription, for no more than a 30-day supply
-
Patients who can become pregnant must be enrolled by signing an informed consent form and must comply with the following requirements
- Comply with the pregnancy testing and contraceptive requirements;
- demonstrate comprehension of the safe-use conditions of the program every month
- Obtain the prescription within 7 days of pregnancy test collection; patients who cannot become pregnant must be enrolled by signing an informed consent form and must obtain the prescription within 30 days of the office visit
-
Pharmacies that dispense the product
- Must be certified by being registered and activated in the program, must only dispense to patients who are authorized to receive the treatment, and comply with the following requirements:
- Only dispense a maximum of a 30-day supply with a Medication Guide;
- Do not dispense refills; dispense only with a new prescription and a new authorization from the program
- Return product to inventory if patients do not obtain the prescription by the “Do Not Dispense to After” date
- Wholesalers and distributors must be registered with the program and must only distribute to certified pharmacies
- Further information, including a list of qualified pharmacies and distributors, is available at www.ipledgeprogram.com or 1-866-495-0654
Lactation
There are no data on either animal or human milk, effects on breastfed infant, or on milk production; because of potential for serious adverse reactions in nursing infants from isotretinoin, advise patients that breastfeeding is not recommended during treatment and for at least 8 days after the last dose
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Retinoid; inhibits sebaceous gland function and keratinization; clinical improvement of nodular acne associated with sebum secretion reduction
Absorption
Bioavailability: Low
Peak plasma time
- 5.3 hr (fed); 3.2 hr (fasted)
- Absorica: 6.4 hr (fed); 2.9 hr (fasted)
- Absorica LD: 5 hr (fed); 3.5 hr (fasted)
Peak plasma concentration
- 862 ng/mL (fed); 301 ng/mL (fasted)
- Absorica: 395 ng/mL (fed); 314 ng/mL (fasted)
- Absorica LD: 646 ng/mL (fed); ~6% lower under fasting conditions
AUC
- 10,004 ng•hr/mL (fed): 3703 ng•hr/mL (fasted)
- Absorica: 6095 ng•hr/mL (fed); 4055 ng•hr/mL (fasted); AUC (fasted state) greater than Accutane, and therefore not interchangeable with generic products
- Absorica LD: 10,209 ng•hr/mL; ∼20% lower under fasting conditions
Distribution
Protein bound: 99.9% (primarily albumin)
Metabolism
Metabolized by liver oxidation via hepatic isoenzymes CYP2B6, CYP2C8/9, and CYP3A4
Metabolites: 4-oxo-isotretinoin, retinoic acid (tretinoin), 4-oxo-retinoic acid
Elimination
Half-life: 18 hr (Absorica); 24 hr (Absorica LD); 38 hr (4-oxo-isotretinoin metabolite)
Excretion: 65-83% of drug excreted in feces and urine in relatively equal amounts
Administration
Oral Administration
Swallow capsule whole with full glass of water to reduce esophageal irritation
Amnesteem, Claravis, Myorisan, Zenatane: Take with food (significantly improves absorption)
Absorica, Absorica LD: May be taken with or without food
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| Accutane oral - | 40 mg capsule |  | |
| Accutane oral - | 30 mg capsule |  | |
| Accutane oral - | 20 mg capsule |  | |
| Claravis oral - | 30 mg capsule |  | |
| Claravis oral - | 10 mg capsule |  | |
| Claravis oral - | 10 mg capsule |  | |
| Claravis oral - | 40 mg capsule |  | |
| Claravis oral - | 20 mg capsule |  | |
| Claravis oral - | 40 mg capsule |  | |
| Claravis oral - | 10 mg capsule |  | |
| Claravis oral - | 40 mg capsule |  | |
| Amnesteem oral - | 40 mg capsule |  | |
| Amnesteem oral - | 20 mg capsule |  | |
| Amnesteem oral - | 10 mg capsule |  | |
| Absorica oral - | 30 mg capsule |  | |
| Absorica oral - | 40 mg capsule |  | |
| Absorica oral - | 35 mg capsule |  | |
| Absorica oral - | 20 mg capsule |  | |
| Absorica oral - | 10 mg capsule |  | |
| Absorica oral - | 25 mg capsule |  | |
| Zenatane oral - | 40 mg capsule | | |
| Zenatane oral - | 20 mg capsule | | |
| Zenatane oral - | 10 mg capsule |  | |
| Zenatane oral - | 30 mg capsule | | |
| isotretinoin oral - | 20 mg capsule |  | |
| isotretinoin oral - | 30 mg capsule |  | |
| isotretinoin oral - | 35 mg capsule | | |
| isotretinoin oral - | 10 mg capsule |  | |
| isotretinoin oral - | 40 mg capsule | | |
| isotretinoin oral - | 30 mg capsule | | |
| isotretinoin oral - | 25 mg capsule | | |
| isotretinoin oral - | 20 mg capsule | | |
| isotretinoin oral - | 10 mg capsule | | |
| isotretinoin oral - | 10 mg capsule |  | |
| isotretinoin oral - | 10 mg capsule |  | |
| isotretinoin oral - | 40 mg capsule |  | |
| isotretinoin oral - | 30 mg capsule |  | |
| isotretinoin oral - | 40 mg capsule |  | |
| isotretinoin oral - | 20 mg capsule |  |
Copyright © 2010 First DataBank, Inc.
Patient Handout
isotretinoin oral
ISOTRETINOIN - ORAL
(EYE-soeTRET-i-noyn)
COMMON BRAND NAME(S): Absorica, Absorica LD, Accutane, Amnesteem, Claravis, Sotret
WARNING: Women who are pregnant must not use isotretinoin. Women must avoid becoming pregnant while taking this medication. Serious (sometimes fatal) birth defects, miscarriages, and premature births have occurred when this drug has been used during pregnancy.For female patients, two effective forms of birth control (or complete avoidance of sexual intercourse) must be used for 1 month before starting isotretinoin, during use, and for 1 month after stopping this drug. You must also have monthly pregnancy-avoidance counseling from your doctor. Do not use "minipills" for birth control (non-estrogen-containing pills) since they may not work as well with isotretinoin. If you are late in having your period, or if you have sexual intercourse at any time without using two effective forms of birth control, stop taking this medication and contact your doctor right away. (See also the Precautions section.)To receive this medication in the United States, you must understand, agree to, and carefully follow the requirements of the iPLEDGE REMS Program. If you live in Canada or any other country, consult your doctor and pharmacist for your country's regulations.Talk with your doctor about the risks and benefits of using this medication.
USES: This medication is used to treat severe cystic acne (also known as nodular acne) that has not responded to other treatment (such as benzoyl peroxide or clindamycin applied to the skin or tetracycline or minocycline taken by mouth). It belongs to a class of drugs known as retinoids. It works by decreasing facial oil (sebum) production. High amounts of sebum can lead to severe acne. If left untreated, severe acne may cause permanent scarring.
HOW TO USE: Read the Medication Guide provided by your pharmacist before you start using isotretinoin and each time you get a refill. Read and sign a Patient Information/Informed Consent form before you start taking this medication. If you have any questions about isotretinoin, consult your doctor or pharmacist before taking the medication.Take this medication by mouth as directed by your doctor, usually twice daily for 15 to 20 weeks. Swallow the capsules whole. Do not crush or chew them. Some brands of this drug say to take this medication with meals while other brands say that it may be taken with or without food. Food helps increase absorption of this drug into your bloodstream. Ask your doctor or pharmacist for more information.Take this medication with a full glass of water (8 ounces/240 milliliters) unless your doctor directs you otherwise. Do not lie down for at least 10 minutes after taking this medication.The dosage is based on your medical condition, weight, and response to treatment.Your acne may worsen during the first few days of taking this drug, and it may take up to 1-2 months before you notice the full benefit of this medication. If severe acne returns, a second course of treatment may be started after you have stopped taking the drug for 2 months. The manufacturer does not recommend long-term use of isotretinoin. Do not take more than the recommended dose.Since this drug can be absorbed through the skin and lungs and may harm an unborn baby, women who are pregnant or who may become pregnant should not handle this medication or breathe the dust from the capsules.
SIDE EFFECTS: Dry lips and mouth, minor swelling of the eyelids or lips, crusty skin, nosebleeds, upset stomach, or thinning of hair may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.To relieve dry mouth, suck on (sugarless) hard candy or ice chips, chew (sugarless) gum, drink water, or use a saliva substitute.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if you have any serious side effects, including: mental/mood changes (such as depression, anxiety, thoughts of suicide), tingling feeling in the skin, back/joint/muscle pain, signs of infection (such as sore throat that doesn't go away, fever), painful swallowing, peeling skin on palms/soles.Isotretinoin may rarely cause disease of the pancreas (pancreatitis) that may rarely be fatal. Stop taking this medication and tell your doctor right away if you develop: severe stomach pain, nausea/vomiting that is severe or doesn't stop.Stop taking this medication and tell your doctor right away if you have any very serious side effects, including: severe headache, vision changes, ringing in the ears, hearing loss, chest pain, yellowing eyes/skin, dark urine, severe diarrhea, rectal bleeding.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
PRECAUTIONS: Before taking isotretinoin, tell your doctor or pharmacist if you are allergic to it; or to vitamin A-related drugs (other retinoids such as tretinoin); or if you have any other allergies. This product may contain inactive ingredients (such as soybean, parabens), which can cause allergic reactions or other problems. Some people who are allergic to peanuts may also be allergic to soy. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: diabetes, family or personal history of high blood fats (triglycerides), mental/mood problems (such as depression), liver disease, obesity, eating disorders (such as anorexia nervosa), alcohol abuse, pancreatitis, bone loss conditions (such as osteoporosis/osteomalacia, decreased bone density).Do not donate blood while you are taking isotretinoin and for at least 1 month after you stop taking it.This medication may make you more sensitive to the sun. Limit your time in the sun. Avoid tanning booths and sunlamps. Use sunscreen and wear protective clothing when outdoors. Tell your doctor right away if you get sunburned or have skin blisters/redness.Isotretinoin can affect your night vision. Do not drive, use machinery, or do any activity that requires clear vision after dark until you are sure you can perform such activities safely.If you wear contact lenses, you may not tolerate them as well as usual while using this medication. Contact your doctor for more information.Do not have cosmetic procedures to smooth your skin (such as waxing, laser, dermabrasion) during and for 6 months after isotretinoin therapy. Skin scarring may occur.Avoid the use of alcohol while taking this medication because it may increase the risk of certain side effects (such as pancreatitis).Limited information suggests isotretinoin may cause some bone loss effects. Playing contact or repetitive impact sports (such as football, basketball, soccer, tennis) may result in bone problems, including an increased risk of broken bones. Limited information also suggests isotretinoin may stop normal growth in some children (epiphyseal plate closure). Consult your doctor for more details.Older adults may be more sensitive to the side effects of this drug, especially the effects on bones.Children may be more sensitive to the side effects of this drug, especially back/joint/muscle pain.This drug must not be used during pregnancy or by those who may become pregnant during treatment. If you become pregnant or think you may be pregnant, inform your doctor right away. See also Warning section.Since this drug can be absorbed through the skin and lungs and may harm an unborn baby, women who are pregnant or who may become pregnant should not handle this medication or breathe the dust from the capsules.You must have two negative pregnancy tests before starting this medication. You must have a monthly pregnancy test during treatment with isotretinoin. If the test is positive, you must stop taking this medication and consult your doctor right away.It is unknown if this medication passes into breast milk. However, similar drugs pass into breast milk. Breast-feeding while using this drug is not recommended. Ask your doctor when you can breast-feed after stopping treatment. Consult your doctor before breast-feeding.
DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Some products that may interact with this drug are: tetracyclines (such as minocycline, tetracycline), vitamin A-type drugs (such as acitretin, bexarotene), vitamin A, drugs that cause bone loss (for example, anti-seizure drugs such as phenytoin, corticosteroids such as prednisone).Tell your doctor when you start any new drug, and discuss if you should use additional reliable birth control. Also tell your doctor if you have any new spotting or breakthrough bleeding, because these may be signs that your birth control is not working well. (See also Warning section.)
OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: vomiting, stomach pain, facial flushing, headache, loss of balance.
NOTES: Do not allow anyone else to take this medication. It can cause birth defects and other serious health problems.Lab and/or medical tests (such as pregnancy test, blood cholesterol/triglyceride levels, liver function, white blood count, eye exams) should be done while you are taking this medication. Keep all medical and lab appointments. Consult your doctor for more details.
MISSED DOSE: If you miss a dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.
STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications out of reach of children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.
Information last revised December 2022. Copyright(c) 2023 First Databank, Inc.
IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.
Formulary
Adding plans allows you to compare formulary status to other drugs in the same class.
To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.
Adding plans allows you to:
- View the formulary and any restrictions for each plan.
- Manage and view all your plans together – even plans in different states.
- Compare formulary status to other drugs in the same class.
- Access your plan list on any device – mobile or desktop.
