ACCUTANE
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WARNING
Contraindications and Warning: Isotretinoin must not be used by
females who are pregnant or who may become pregnant while undergoing
treatment. Although not every fetus exposed to isotretinoin has
resulted in a deformed child, there is an extremely high risk that a
deformed infant can result if pregnancy occurs while taking
isotretinoin in any amount even for short periods. Potentially any
fetus exposed during
pregnancy can be affected. Presently, there is no accurate means of
determining after isotretinoin exposure which fetus has been affected
and which fetus has not been affected.
Isotretinoin is Contraindicated in Women of Childbearing Potential Unless the PATIENT MEETS ALL OF THE
FOLLOWING CONDITIONS:
Has severe disfiguring nodular acne that is recalcitrant to standard therapies (see INDICATIONS AND USAGE
for definition).
Is reliable in understanding and carrying out instructions.
Is capable of complying with the mandatory contraceptive measures.
Has received both oral and written warnings of the hazards of taking
isotretinoin during pregnancy and the exposing a fetus to the drug
Has received both oral and written warnings of the risk of possible
contraception failure and of the need to use two reliable forms of
contraception simultaneously, unless abstinence is the chosen method,
or the patient has undergone a hysterectomy and has acknowledged in
writing her understanding of these warnings and of the need for using
dual contraceptive methods
Has had a negative serum pregnancy test with a sensitivity of at least 50 mIU/ml within one week prior to beginning therapy
Will begin therapy only on the second or third day of the next normal menstrual period
It is recommended that a prescription for isotretinoin should not be issued by the physician until a report of a negative
pregnancy test has been obtained and the patient has begun her
menstrual period. It is also recommended that pregnancy testing and
contraception counseling be repeated on a monthly basis. To encourage
compliance with this recommendation, the physician should prescribe no
more than a 1 month supply of the drug.
Major human fetal abnormalities related to isotretinoin
administration have been documented: CNS abnormalities (including
cerebral abnormalities, cerebellar malformation, hydrocephalus,
microcephaly, cranial nerve deficit); skull abnormality; external
ear abnormalities (including anotia, micropinna, small or absent
external auditory canals); eye abnormalities (including
microphthalmia);
cardiovascular abnormalities; facial dysmorphia; thymus gland
abnormality; parathyroid hormone deficiency. In some cases death
has occurred with certain of the abnormalities previously noted. Cases
of IQ scores less than 85 with or without obvious CNS abnormalities
have also been reported. There is an increased risk of
spontaneous abortion. In addition, premature births have been
reported.
Effective contraception must be used for at least 1 month before
beginning isotretinoin therapy, during therapy and for 1 month
following discontinuation of therapy even where there has been a
history of infertility, unless due to hysterectomy. It is
recommended that two reliable forms of contraception be used
simultaneously unless abstinence is the chosen method.
If pregnancy does occur during treatment, the physician and patient should discuss the desirability of continuing the
pregnancy.
Isotretinoin should be prescribed only by physicians who have
special competence in the diagnosis and treatment of severe
recalcitrant nodular acne, are experienced in the use of systemic
retinoids and understand the risk of teratogenicity if
isotretinoin is used during pregnancy.
CONTRAINDICATIONS
Pregnancy Category X
See BOXED WARNING. Isotretinoin should not be given to patients who are
sensitive to parabens, which are used as preservatives in the gelatin
capsule.
WARNINGS
Pseudotumor cerebri: Isotretinoin use has been associated with a number of cases of pseudotumor cerebri (benign
intracranial hypertension). Early signs and symptoms of
pseudotumor cerebri include papilledema, headache, nausea and
vomiting, and visual disturbances. Patients with these symptoms
should be screened for papilledema and, if present, they should
be told to discontinue isotretinoin immediately and be referred to a
neurologist for further diagnosis and care.
Decreased Night Vision: A number of cases of decreased night vision
have occurred during isotretinoin therapy. Because the onset in some
patients was sudden, patients should be advised of this potential
problem and warned to be cautious when driving or operating any vehicle
at night. Visual problems should be carefully monitored.
Corneal Opacities: Corneal opacities have occurred in patients
receiving isotretinoin for acne and more frequently when higher drug
dosages were used in patients with disorders of keratinization. All
isotretinoin patients experiencing visual difficulties should
discontinue the drug and have an ophthalmological examination. The
corneal opacities that have been observed in patients treated with
isotretinoin have either
completely resolved or were resolving at follow-up 6 to 7 weeks after
discontinuation of the drug. See ADVERSE REACTIONS.
Inflammatory Bowel Disease: Isotretinoin has been temporally associated
with inflammatory bowel disease (including regional ileitis) in
patients without a prior history of intestinal disorders. Patients
experiencing abdominal pain, rectal bleeding or severe diarrhea should
discontinue isotretinoin immediately.
Lipids: Blood lipid determinations should be performed before
isotretinoin is given and then at intervals until the lipid response to
isotretinoin is established, which usually occurs within 4 weeks. See
PRECAUTIONS.
Approximately 25% of patients receiving isotretinoin experienced an
elevation in plasma triglycerides. Approximately 15% developed a
decrease in high density lipoproteins and about 7% showed an increase
in cholesterol levels. These effects on triglycerides, HDL and
cholesterol were reversible upon cessation of isotretinoin therapy.
Patients with increased tendency to develop hypertriglyceridemia
include those with diabetes mellitus, obesity, increased alcohol intake
and familial history.
The cardiovascular consequences of hypertriglyceridemia are not well
understood, but may increase the patient's risk status. In addition,
elevation of serum triglycerides in excess of 800 mg/dl has been
associated with acute pancreatitis. Therefore, every attempt should be
made to control significant triglyceride elevation.
Some patients have been able to reverse triglyceride elevation by
reduction in weight, restriction of dietary fat and alcohol, and
reduction in dose while continuing isotretinoin.5
An obese male patient with Darier's disease developed elevated triglycerides and subsequent eruptive xanthomas.6
Hyperostosis: In clinical trials of disorders of keratinization with a
mean dose of 2.24 mg/kg/day, a high prevalence of skeletal hyperostosis
was noted. Two children showed x-ray findings suggestive of premature
closure of the epiphysis. Additionally, skeletal hyperostosis was noted
in 6 of 8 patients in a prospective study of disorders of
keratinization.7 Minimal skeletal hyperostosis has also been observed
by
x-rays in prospective studies of nodular acne patients treated with a
single course of therapy at recommended doses.
Hepatotoxicity: Several cases of clinical hepatitis have been noted
which are considered to be possibly or probably related to isotretinoin
therapy. Additionally, mild to moderate elevations of liver enzymes
have been observed in approximately 15% of individuals treated during
clinical trials, some of which normalized with dosage reduction or
continued administration of the drug. If normalization does not readily
occur or if hepatitis is suspected during treatment with isotretinoin,
the drug should be discontinued and the etiology further investigated.
Animal Studies: In rats given 32 or 8 mg/kg/day of isotretinoin for 18
months or longer, the incidences of focal calcification, fibrosis and
inflammation of the myocardium, calcification of coronary, pulmonary
and mesenteric arteries and metastatic calcification of the gastric
mucosa were greater than in control rats of similar age. Focal
endocardial and myocardial calcifications associated with calcification
of the
coronary arteries were observed in two dogs after approximately 6 to 7
months of treatment with isotretinoin at a dosage of 60 to 120
mg/kg/day.
In dogs given isotretinoin chronically at a dosage of 60 mg/kg/day,
corneal ulcers and corneal opacities were encountered at a higher
incidence than in control dogs. In general, these ocular changes tended
to revert toward normal when treatment with isotretinoin was stopped,
but did not completely clear during the observation period.
In rats given isotretinoin at a dosage of 32 mg/kg/day for approximately 15 weeks, long bone fracture has been observed.
PRECAUTIONS
Information for the Patient: Women of childbearing potential should be
instructed that they must not be pregnant when isotretinoin therapy is
initiated, and that they should use effective contraception while
taking isotretinoin and for 1 month after isotretinoin has been
stopped. They should also sign a consent form prior to beginning
isotretinoin therapy. See CONTRAINDICATIONS and BOXED WARNING.
Because of the relationship of isotretinoin to vitamin A, patients
should be advised against taking vitamin supplements containing vitamin
A to avoid additive toxic effects.
Patients should be informed that transient exacerbation of acne has been seen, generally during the initial period of therapy.
Patients should be informed that they may experience decreased tolerance to contact lenses during and after therapy.
It is recommended that patients not donate blood during therapy and for at least 1 month following discontinuance of the drug.
Laboratory Tests: The incidence of hypertriglyceridemia is 1 patient in
4 on isotretinoin therapy. Pretreatment and follow-up blood lipids
should be obtained under fasting conditions. After consumption of
alcohol at least 36 hours should elapse before these determinations are
made. It is recommended that these tests be performed at weekly or
biweekly intervals until the lipid response to isotretinoin is
established.
Since elevations of liver enzymes have been observed during clinical
trials, pretreatment and follow-up liver function tests should be
performed at weekly or biweekly intervals until the response to
isotretinoin has been established.
Certain patients receiving isotretinoin have experienced problems in
the control of their blood sugar. In addition, new cases of diabetes
have been diagnosed during isotretinoin therapy, although no causal
relationship has been established. Some patients undergoing vigorous
physical activity while on isotretinoin therapy have experienced
elevated CPK levels; however, the clinical significance is unknown.
Carcinogenesis, Mutagenesis, and Impairment of Fertility: In Fischer
344 rats given isotretinoin at dosages of 8 or 32 mg/kg/day for greater
than 18 months, there was an increased incidence of pheochromocytoma.
The incidence of adrenal medullary hyperplasia was also increased at
the higher dosage. The relatively high level of spontaneous
pheochromocytomas occurring in the Fischer 344 rat makes it a poor
model for
study of this tumor, since the increase in adrenal medullary
proliferative lesions following chronic treatment with relatively high
dosages of isotretinoin may be an accentuation of a genetic
predisposition in the Fischer 344 rat, and its relevance to the human
population is not clear. In addition, a decreased incidence of liver
adenomas, liver angiomas and leukemia was noted at the dose levels of 8
and 32 mg/kg/day.
The Ames test was conducted in two laboratories. The results of the
tests in one laboratory were negative while in the second laboratory a
weakly-positive response (less than 1.6 x background) was noted in S.
typhimurium TA100 when the assay was conducted with metabolic
activation. No dose-response effect was seen and all other strains were
negative. Additionally, other tests designed to assess genotoxicity
(Chinese
hamster cell assay, mouse micronucleus test, S. cerevisiae D7 assay, in
vitro clastogenesis assay in human-derived lymphocytes and unscheduled
DNA synthesis assay) were all negative.
No adverse effects on gonadal function, fertility, conception rate,
gestation or parturition were observed at dose levels of 2, 8 or 32
mg/kg/day in male and female rats.
In dogs, testicular atrophy was noted after treatment with isotretinoin
for approximately 30 weeks at dosages of 20 or 60 mg/kg/day. In
general, there was microscopic evidence for appreciable depression of
spermatogenesis but some sperm were observed in all testes examined and
in no instance were completely atrophic tubules seen. In studies in 66
human males, 30 of whom were patients with nodular acne, no significant
changes were noted in the count or motility of spermatozoa in the
ejaculate. In a study of 50 men (ages 17 to 32 years) receiving
isotretinoin therapy for nodular acne, no significant effects were seen
on ejaculate volume, sperm count, total sperm motility, morphology or
seminal plasma fructose.
Pregnancy Category X: See BOXED WARNING.
Nursing Mothers: It is not known whether this drug is excreted in human
milk. Because of the potential for adverse effects, nursing mothers
should not receive isotretinoin.