Included as part of the PRECAUTIONS section.
Contamination of Tip and Solution
To minimize contaminating the dropper tip and solution, care
should be taken not to touch the eyelids or surrounding areas with the dropper
tip of the bottle. Keep bottle tightly closed when not in use.
Benign Intracranial Hypertension
There have been reports of benign intracranial hypertension
(or pseudotumor cerebri) associated with oral cysteamine treatment that has
resolved with the addition of diuretic therapy.
There have also been reports associated with ophthalmic use
of cysteamine; however, all of these patients were on concurrent oral
Use with Contact Lenses
CYSTARAN contains benzalkonium chloride, which may be
absorbed by soft contact lenses. Contact lenses should be removed prior to
application of solution and may be reinserted 15 minutes following its
administration [see PATIENT INFORMATION].
Topical Ophthalmic Use Only
CYSTARAN is for topical ophthalmic use only.
Carcinogenesis, Mutagenesis, Impairment of Fertility
Cysteamine has not been tested for
its carcinogenic potential in long-term animal studies. Cysteamine was not
mutagenic in the Ames test. It produced a negative response in an in vitro sister
chromatid exchange assay in human lymphocytes but a positive response in a
similar assay in hamster ovarian cells.
Repeat breeding reproduction
studies were conducted in male and female rats. Cysteamine was found to have no
effect on fertility and reproductive performance at an oral dose of 75
mg/kg/day (450 mg/m²/day, 0.4 times the recommended human dose based
on body surface area). At an oral dose of 375 mg/kg/day (2,250 mg/m²/day,
1.7 times the recommended human dose based on body surface area), it reduced
the fertility of the adult rats and the survival of their offspring.
Use In Specific Populations
There are no adequate and well-controlled studies of
ophthalmic cysteamine in pregnant women. CYSTARAN should be used during pregnancy
only if the potential benefit justifies the potential risk to the fetus.
Teratogenic Effects - Pregnancy Category C
Teratology studies have been
performed in rats at oral doses in a range of 37.5 mg/kg/day to 150 mg/kg/day
(about 0.2 to 0.7 times the recommended human maintenance dose on a body
surface basis) and have revealed cysteamine bitartrate to be teratogenic.
Observed teratogenic findings were cleft palate, kyphosis, heart ventricular
septal defects, microcephaly, and exencephaly.
Cysteamine was fetotoxic, resulting in intrauterine death
and growth retardation in rats at oral doses of 0.2 to 0.7 times the
recommended human maintenance dose on a body surface basis.
It is not known whether oral cysteamine is excreted in human
milk. Because many drugs are excreted in human milk and because of the
manifested potential of cysteamine for developmental toxicity in suckling rat
pups when it was administered to their lactating mothers at an oral dose of 375
mg/kg/day (2,250 mg/m²/day, 1.7 times the recommended human dose
based on body surface area), a decision should be made whether to discontinue
nursing or to discontinue the drug, taking into account the importance of the drug
to the mother. The incremental increase in systemic cysteamine levels derived
from drug applied topically to the eye in patients treated with oral cysteamine
The safety and effectiveness of CYSTARAN (cysteamine ophthalmic
solution) 0.44% have been established.
When the clinical studies with CYSTARAN were conducted, the
reduced life expectancy from cystinosis did not make it possible to include
patients in the geriatric age range.
The effect of renal impairment on the pharmacokinetics of
cysteamine following ophthalmic administration of cysteamine ophthalmic
solution has not been evaluated because ophthalmic exposure compared to
systemic exposure is negligible. The majority of the patients in the ophthalmic
clinical studies are assumed to have had some degree of renal impairment due to
their underlying systemic disease. The total daily ophthalmic dose is less than
2% of the recommended oral daily dose of cysteamine; thus, the systemic
exposure following ophthalmic administration is expected to be negligible
compared to oral administration.