Rhokiinsa

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ANNEX I 
 

SUMMARY OF PRODUCT CHARACTERISTICS 



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This medicinal product is subject to additional monitoring. This will allow quick identification of 
new safety information. Healthcare professionals are asked to report any suspected adverse reactions. 
See section 4.8 for how to report adverse reactions.  
 
 
1. NAME OF THE MEDICINAL PRODUCT 
 
Rhokiinsa 200 micrograms/ml eye drops, solution. 
 
 
2. QUALITATIVE AND QUANTITATIVE COMPOSITION 
 
Each ml of solution contains 200 micrograms netarsudil (as mesylate). 
 
Excipient(s) with known effect: 
 
Each ml of solution contains 150 micrograms benzalkonium chloride. 
 
For the full list of excipients, see section 6.1. 
 
 
3. PHARMACEUTICAL FORM 
 
Eye drops, solution (eye drops). 
 
Clear solution, pH 5 (approximately). 
 
 
4. CLINICAL PARTICULARS 
 
4.1 Therapeutic indications 
 
Rhokiinsa is indicated for the reduction of elevated intraocular pressure (IOP) in adult patients with 
primary open-angle glaucoma or ocular hypertension. 
 
4.2 Posology and method of administration 
 
Treatment with Rhokiinsa should only be initiated by an ophthalmologist or a healthcare professional 
qualified in ophthalmology. 
 
Posology 
 
Use in adults, including the elderly  
The recommended dosage is one drop in the affected eye(s) once daily in the evening. Patients should 
not instill more than one drop in the affected eye(s) each day. 
 
If one dose is missed, treatment should continue with the next dose in the evening.   
 
Paediatric population 
The safety and efficacy of Rhokiinsa in children below the age of 18 years have not been established. 
No data are available. 
 
Method of administration  
 
For ocular use. 
 



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No data on potential interactions specific to netarsudil is currently available (see section 4.5). If 
netarsudil is to be used concomitantly with other topical ophthalmic medicinal products, each 
medicinal product should be administered at least five (5) minutes apart. Due to netarsudil’s 
vasodilating properties, other eye drops should be administered before. Eye ointments should be 
administered last. 
 
Contact lenses should be removed prior to instillation of netarsudil and may be reinserted 15 minutes 
following its administration (see section 4.4).  
 
The tip of the dispensing container should avoid contacting the eye, surrounding structures, fingers, or 
any other surface in order to avoid contamination of the solution. Serious damage to the eye and 
subsequent loss of vision may result from using contaminated solutions. 
 
4.3 Contraindications 
 
Hypersensitivity to the active substance(s) or to any of the excipients listed in section 6.1. 
 
4.4 Special warnings and precautions for use 
 
Ocular effects 
 
Twice a day dosing is not well tolerated and is not recommended. Netarsudil dosed twice daily 
provided slightly larger IOP reductions, but had a less favorable safety profile as reflected in a higher 
rate and increased severity of ocular adverse reactions. Twice a day dosing was also associated with a 
higher discontinuation rate due to adverse reactions (53.8%) during a 12-month study. It is therefore 
recommended to dose netarsudil once daily.  
 
Benzalkonium chloride content 
 
This medicinal product contains benzalkonium chloride. 
Benzalkonium chloride has been reported to cause eye irritation, symptoms of dry eyes and may affect 
the tear film and corneal surface and is known to discolour soft contact lenses. It should be used with 
caution in dry eye patients and in patients where the cornea may be compromised.  
Patients should be monitored in case of prolonged use. 
 
The efficacy of netarsudil has not been studied beyond 12 months. 
 
4.5 Interaction with other medicinal products and other forms of interaction 
 
No interaction studies have been performed. 
 
4.6 Fertility, pregnancy and lactation 
 
Pregnancy 
 
There are no or limited amount of data from the use of netarsudil in pregnant women. No effects 
during pregnancy are anticipated, since systemic exposure to netarsudil is negligible (see section 5.2). 
Animal studies with intravenous administration do not indicate direct or indirect harmful effects with 
respect to reproductive toxicity at clinically relevant exposures (see section 5.3). Rhokiinsa should not 
be used during pregnancy unless the clinical condition of the woman requires treatment with 
netarsudil. 
 
Breast-feeding 
 
It is unknown whether netarsudil/metabolites are excreted in human milk. However, while no effects 
on the breastfed newborn/infant are anticipated since the systemic exposure of breast-feeding women 
to netarsudil is expected to be negligible, no relevant clinical data are available (see section 5.2). A 



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decision must be made whether to discontinue breast-feeding or to discontinue/abstain from Rhokiinsa 
therapy taking into account the benefit of breast feeding for the child and the benefit of therapy for the 
woman.  
 
Fertility 
 
There are no data on the effects of netarsudil on male or female fertility. However, no effects are 
anticipated, since systemic exposure to netarsudil is negligible (see section 5.2). 
 
4.7 Effects on ability to drive and use machines 
 
Rhokiinsa has negligible influence on the ability to drive and use machines.  
If transient blurred vision occurs at instillation, the patient should wait until the vision clears before 
driving or using machines.  
 
4.8 Undesirable effects 
 
Summary of the safety profile 
 
The most common ocular adverse reaction observed is conjunctival hyperemia which was reported in 
51% of patients. Other ocular adverse reactions reported are: cornea verticillata (17%), instillation site 
pain (17%), and conjunctival haemorrhage (8%). Instillation site erythema (8%), corneal staining 
(7%), blurred vision (6%), increased lacrimation (6%) and erythema of eyelid (5%) were also 
reported.  
 
Tabulated list of adverse reactions 
 
The following adverse reactions have been reported with netarsudil, dosed once daily. Reactions are 
classified according to the convention: very common (≥1/10), common (≥1/100 to <1/10), uncommon 
(≥1/1,000 to <1/100), rare (≥1/10,000 to <1/1,000), very rare (<1/10,000) or not known (cannot be 
estimated from the available data). 
 
System Organ Classification Frequency Adverse reactions 
Immune system disorders Uncommon hypersensitivity 
Nervous system disorders Common headache 
 Uncommon dizziness,  

visual field defect 
Eye disorders Very 

common 
conjunctival hyperaemia1,  
cornea verticillata1,  
instillation site pain 

 Common conjunctival haemorrhage,  
vision blurred,  
lacrimation increased,  
erythema of eyelid,  
eye pruritis,  
eye irritation,  
visual acuity reduced,  
eyelid oedema,  
punctate keratitis,  
conjunctival oedema,  
foreign body sensation in eyes, 
conjunctivitis,  
conjunctivitis allergic,  
photophobia,  
eyelid pruritus,  
eye pain,  
corneal opacity,  
dry eye,  
eye discharge,  



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System Organ Classification Frequency Adverse reactions 
instillation site erythema,  
instillation site discomfort,  
instillation site pruritis,  
vital dye staining cornea present, 
intraocular pressure increased 

 Uncommon ocular hyperaemia,  
blepharitis,  
corneal disorder,  
eyelid margin crusting,  
eye allergy,  
conjunctival follicles,  
ocular discomfort,  
eye swelling,  
corneal deposits,  
eyelid disorder,  
meibomian gland dysfuntion,  
corneal pigmentation,  
diplopia,  
ectropion,  
lenticular opacities,  
noninfective conjunctivitis,  
abnormal sensation in the eye,  
asthenopia,  
episcleral hyperaemia,  
halo vision,  
keratitis,  
refraction disorder,  
anterior chamber flare,  
anterior chamber inflammation,  
blindness,  
conjunctival irritation,  
conjunctivochalasis,  
diabetic retinopathy,  
eczema eyelids,  
eyelid skin dryness,  
glaucoma,  
growth of eyelashes,  
iris adhesions,  
iris bombe,  
iritis,  
ocular hypertension,  
visual impairment,  
corneal dystrophy,  
instillation site foreign body sensation, 
instillation site irritation,  
glassy eyes,  
fatigue,  
instillation site dryness,  
instillation site oedema,  
instillation site paraesthesia,  
conjunctival staining,  
optic nerve cup/disc ratio increased, 
madarosis 

Respiratory, thoracic and mediastinal disorders Uncommon nasal discomfort,  
rhinalgia 

Skin and subcutaneous tissue disorders Uncommon dermatitis allergic,  
dermatitis contact,  
lichenification,  
petechiae 

Musculoskeletal and connective tissue disorders Uncommon polychondritis 
Injury, poisoning and procedural complications Uncommon excoriation 
1 See Description of selected adverse reactions for further information 



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Description of selected adverse reactions 
 
Conjunctival Hyperaemia 
Conjunctival hyperaemia was the most frequently reported adverse reaction associated with netarsudil 
treatment in clinical trials and it is attributed to the vasodilation effect of the Rho kinase inhibitor drug 
class. Conjunctival hyperaemia was typically mild in severity and sporadic. However, there was a 
relatively small proportion of subjects with moderate or severe hyperaemia who discontinued 
treatment because of this adverse reaction (6.0% in Phase 3 clinical studies). 
 
Cornea Verticillata 
Cornea verticillata occurred in approximately 20% of the patients in controlled Phase 3 clinical 
studies. The cornea verticillata seen in netarsudil-treated patients were first noted at 4 weeks of daily 
dosing. This reaction did not result in any apparent visual functional changes in patients. The majority 
of cornea verticillata resolved upon discontinuation of treatment. The incidence of cornea verticillata 
was higher in certain subpopulations: elderly (≥65 years) versus non-elderly (24.8 vs. 15.9%); males 
versus females (24.4 vs. 18.4%) and in white versus other races (25.6 vs. 7.0%). 
 
Special populations 
 
Elderly subjects 
With the exception of cornea verticillata (see above), no difference in the safety profile for Rhokiinsa 
has been observed between subjects aged <65 or ≥65 years. 
  
Reporting of suspected adverse reactions 
 
Reporting suspected adverse reactions after authorisation of the medicinal product is important. It 
allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare 
professionals are asked to report any suspected adverse reactions via the national reporting system 
listed in Appendix V. 
 
4.9 Overdose 
 
Systemic exposure to netarsudil following topical ocular administration has been shown to be 
negligible. If topical overdose of netarsudil should occur, the eye(s) may be flushed with tap water. 
Treatment of an overdose would include supportive and symptomatic therapy. 
 
 
5. PHARMACOLOGICAL PROPERTIES 
 
5.1  Pharmacodynamic properties 
 
Pharmacotherapeutic group: Ophthalmologicals, antiglaucoma preparations and miotics, ATC code: 
S01EX05 
 
Mechanism of action 
 
Netarsudil, a Rho kinase inhibitor, is believed to reduce IOP by increasing outflow of aqueous humor. 
Studies in animal and man suggest that the main mechanism of action is increased trabecular outflow. 
These studies also suggest that netarsudil lowers IOP by reducing episcleral venous pressure.  
 
Clinical efficacy and safety 
 
A randomised, double-blind, multicentre Phase 3 clinical trial compared the efficacy and safety of 
netarsudil once daily with that of timolol maleate 0.5% twice daily in reducing IOP in a total of 708 
patients with open-angle glaucoma or ocular hypertension. The median age of study participants was 
65.5 years (range 18 to 91 years).  
 



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The study was designed to show non-inferiority of netarsudil when dosed once daily in the evening to 
timolol maleate 0.5% dosed twice daily in patients with a baseline IOP of >20 mmHg and <25 mmHg. 
The primary efficacy outcome measure was mean IOP at each of 9 timepoints measured at 08:00, 
10:00 and 16:00 on day 15, day 43 and day 90. The non-inferiority margin applied was a difference in 
mean IOP ≤1.5 mmHg for all time points over all visits through 3 months and ≤1.0 mmHg at a 
majority of these time points. The IOP reduction with netarsudil dosed once daily was non-inferior to 
the effect of timolol 0.5% dosed twice daily in patients with baseline IOP of <25 mmHg (Table 1).  
Efficacy was also investigated in patients with baseline IOP ≥25 mmHg and <30 mmHg. Netarsudil 
demonstrated clinically relevant reductions in IOP at all timepoints, however non-inferiority to timolol 
was not demonstrated in this population with baseline IOP ≥25 mmHg and <30 mmHg (Table 2). 
  
Table 1: Mean IOP by visit: PP population with baseline IOP <25 mmHg 

Study Visit and Time 
Point 

Netarsudil 0.02% Once 
daily 

Timolol 0.5% twice daily Difference (95% CI)  
Netarsudil – Timolol 

N IOP N IOP  
Baseline 08:00 186 22.40 186 22.44  

10:00 186 21.06 186 21.27  
16:00 186 20.69 186 20.69 

Day 15 08:00 184 17.68 183 17.51 0.17 (-0.43, 0.77) 
10:00 181 16.55 183 16.71 -0.16 (-0.73, 0.41) 
16:00 181 16.32 183 16.92 -0.60 (-1.16, -0.04) 

Day 43 08:00 177 17.84 183 17.60 0.25 (-0.34, 0.83) 
10:00 177 16.75 182 16.98 -0.22 (-0.82, 0.37) 
16:00 176 16.57 182 16.67 -0.10 (-0.66, 0.46) 

Day 90 08:00 167 17.86 179 17.29 0.56 (-0.02, 1.15) 
10:00 166 16.90 179 16.69 0.21 (-0.37, 0.79) 
16:00 165 16.73 179 16.80 -0.07 (-0.68, 0.55) 

 
Table 2: Mean IOP by visit: PP population with baseline IOP ≥25 and <30 mmHg 

Study Visit and Time 
Point 

Netarsudil 0.02% Once 
daily 

Timolol 0.5% twice daily Difference (95% CI)  
Netarsudil – Timolol 

N IOP N IOP  
Baseline 08:00 120 26.30 130 25.96  

10:00 120 25.18 130 24.91  
16:00 120 24.48 130 23.99 

Day 15 08:00 118 21.57 129 20.15 1.42 (0.51, 2.34) 
10:00 116 20.09 129 19.34 0.75 (-0.15, 1.64) 
16:00 116 20.01 129 19.17 0.83 (0.00, 1.67) 

Day 43 08:00 112 21.99 127 19.84 2.14 (1.16, 3.13) 
10:00 109 20.33 127 19.19 1.15 (0.30, 1.99) 
16:00 109 20.03 127 19.63 0.41 (-0.47, 1.29) 

Day 90 08:00 94 21.71 121 19.91 1.79 (0.74, 2.85) 
10:00 93 20.80 120 18.95 1.85 (0.89, 2.81) 
16:00 93 20.31 120 18.94 1.37 (0.46, 2.28) 

 
The safety of netarsudil has been evaluated in clinical studies, including four well-controlled Phase 3 
studies.   
 
Approximately 75% of subjects included in the netarsudil treatment groups of Phase 3 studies were 
Caucasian and 24% Black or African American.  Over half were aged ≥ 65 years.  With the exception 
of the incidence of cornea verticillata, no other difference in safety profile was observed between races 
or age groups (see section 4.8). 
 
Completion rates in Phase 3 studies were lower in the netarsudil treatment group when compared with 
the timolol maleate group. Subjects with known contraindications or hypersensitivity to timolol were 



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excluded from the studies. Discontinuation rates due to adverse reactions were 19.3% for the 
netarsudil treatment group versus 1.7% for the timolol maleate group. The majority of 
discontinuations in the netarsudil group were associated with ocular adverse reactions, whereas the 
majority of discontinuations in the timolol group were associated with non-ocular adverse reactions. 
The most frequently reported adverse reactions associated with discontinuation in the Rhokiinsa 
groups were conjunctival hyperemia (5.8%), cornea verticillata (3.7%) and vision blurred (1.4%). The 
incidences of hyperemia and vision blurred were sporadic in nature.  
 
The efficacy and safety of netarsudil in subjects with compromised corneal epithelium or co-existing 
ocular pathologies e.g. pseudoexfoliation and dispersion pigment syndrome has not been established. 
 
Paediatric population 
 
The European Medicines Agency has waived the obligation to submit the results of studies with 
Rhokiinsa in all subsets of the paediatric population for the reduction of elevated intraocular pressure 
in patients with open-angle glaucoma or ocular hypertension. (see section 4.2 for information on 
paediatric use). 
 
5.2 Pharmacokinetic properties 
 
Absorption 
 
The systemic exposures of netarsudil and its active metabolite, AR-13503, were evaluated in 18 
healthy subjects after topical ocular administration of netarsudil once daily (one drop bilaterally in the 
morning) for 8 days. There were no quantifiable plasma concentrations of netarsudil (lower limit of 
quantitation (LLOQ) 0.100 ng/ml) post dose on day 1 and day 8. Only one plasma concentration at 
0.11 ng/ml for the active metabolite was observed for one subject on day 8 at 8 hours post-dose. 
 
Biotransformation 
 
After topical ocular dosing, netarsudil is metabolised by esterases in the eye to an active metabolite, 
AR-13503. 
 
5.3 Preclinical safety data 
 
Non-clinical data reveal no special hazard for humans based on conventional studies of safety 
pharmacology, repeated dose toxicity, genotoxicity and toxicity to development.  
Effects in non-clinical studies were observed only at exposures considered sufficiently in excess of the 
maximum human exposure indicating little relevance to clinical use. 
 
Intravenous administration of netarsudil mesylate to pregnant rats and rabbits during organogenesis 
did not produce adverse embryofetal effects at clinically relevant systemic exposures. In pregnant rats, 
0.3 mg/kg/day (1000 times the recommended ophthalmic dose) and higher showed increased post-
implantation loss and reduced foetal viability.  In pregnant rabbits, 3 mg/kg/day (10000 times the 
recommended ophthalmic dose) and higher showed an increase in post-implantation loss and a 
decrease in foetal weight. 
 
Long-term studies in animals have not been performed to evaluate the carcinogenic potential of 
netarsudil. 
 
Netarsudil was not mutagenic in a bacterial mutation assay, in a mouse lymphoma assay, or in a rat 
micronucleus test. 
 
Netarsudil and its active metabolite AR-13503 was found to have a possible phototoxic potential in a 
modified 3T3 NRU-PT in vitro assay, where the wavelength was extended to include UVB light. 
 
 



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6. PHARMACEUTICAL PARTICULARS 
 
6.1 List of excipients 
 
Benzalkonium chloride 
Mannitol 
Boric acid 
Sodium hydroxide (for pH-adjustment) 
Water for injections 
 
6.2 Incompatibilities 
 
Not applicable. 
 
6.3 Shelf life 
 
3 years.  
 
Opened bottle: 4 weeks after first opening the bottle. Do not store above 25oC. 
 
6.4 Special precautions for storage 
 
Store in a refrigerator (2°C – 8°C) until opened. 
 
For storage conditions after first opening of the medicinal product, see section 6.3. 
 
6.5 Nature and contents of container  
 
Rhokiinsa is supplied sterile in opaque white low density polyethylene bottles (2.5 ml fill in a 4 ml 
container) and tips with white polypropylene caps and anti-tamper seals.  
 
Carton containing 1 bottle. 
 
6.6 Special precautions for disposal  
 
Any unused medicinal product or waste material should be disposed of in accordance with local 
requirements.  
 
 
7. MARKETING AUTHORISATION HOLDER 
 
Aerie Pharmaceuticals Ireland, Limited 
Athlone Business and Technology Park,  
Dublin Road,  
Garrycastle,  
Athlone, Co Westmeath,  
N37 DW40,  
Ireland 
 
 
8. MARKETING AUTHORISATION NUMBER(S)  
 
EU/1/19/1400/001 
 
 
  



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9. DATE OF FIRST AUTHORISATION/RENEWAL OF THE AUTHORISATION 
 
Date of first authorisation:  
 
 
10. DATE OF REVISION OF THE TEXT 
 
Detailed information on this medicinal product is available on the website of the European Medicines 
Agency http://www.ema.europa.eu 
 
  



11 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 

ANNEX II 
 

A. MANUFACTURER(S) RESPONSIBLE FOR BATCH 
RELEASE 

 
B. CONDITIONS OR RESTRICTIONS REGARDING SUPPLY 

AND USE 
 

C. OTHER CONDITIONS AND REQUIREMENTS OF THE 
MARKETING AUTHORISATION 

 
D. CONDITIONS OR RESTRICTIONS WITH REGARD TO 

THE SAFE AND EFFECTIVE USE OF THE MEDICINAL 
PRODUCT 

 



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A. MANUFACTURER(S) RESPONSIBLE FOR BATCH RELEASE 
 
Name and address of the manufacturer(s) responsible for batch release 
 
Aerie Pharmaceuticals Ireland, Limited 
Athlone Business and Technology Park,  
Dublin Road,  
Garrycastle,  
Athlone, Co Westmeath,  
N37 DW40,  
Ireland 
 
 
B. CONDITIONS OR RESTRICTIONS REGARDING SUPPLY AND USE  
 
Medicinal product subject to restricted medical prescription. 
 
 
C.  OTHER CONDITIONS AND REQUIREMENTS OF THE MARKETING 

AUTHORISATION 
 
• Periodic safety update reports (PSURs) 
 
The requirements for submission of PSURs for this medicinal product are set out in the list of 
Union reference dates (EURD list) provided for under Article 107c(7) of Directive 2001/83/EC 
and any subsequent updates published on the European medicines web-portal. 
 
The marketing authorisation holder (MAH) shall submit the first PSUR for this product within 
6 months following authorisation.  
 
 
D. CONDITIONS OR RESTRICTIONS WITH REGARD TO THE SAFE AND 

EFFECTIVE USE OF THE MEDICINAL PRODUCT   
 
• Risk management plan (RMP) 

 
The marketing authorisation holder (MAH) shall perform the required pharmacovigilance 
activities and interventions detailed in the agreed RMP presented in Module 1.8.2 of the 
marketing authorisation and any agreed subsequent updates of the RMP. 
 
An updated RMP should be submitted: 

• At the request of the European Medicines Agency; 
• Whenever the risk management system is modified, especially as the result of new information 

being received that may lead to a significant change to the benefit/risk profile or as the result of 
an important (pharmacovigilance or risk minimisation) milestone being reached. 

  



13 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 

ANNEX III 
 

LABELLING AND PACKAGE LEAFLET 
  



14 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 

A. LABELLING 



15 

PARTICULARS TO APPEAR ON OUTER PACKAGING 
 
OUTER CARTON 
 
 
1. NAME OF THE MEDICINAL PRODUCT 
 
Rhokiinsa 200 micrograms/ml eye drops, solution  
netarsudil  
 
 
2. STATEMENT OF ACTIVE SUBSTANCE(S) 
 
1 ml of solution contains 200 micrograms netarsudil (as mesylate). 
 
 
3. LIST OF EXCIPIENTS 
 
Benzalkonium chloride, boric acid, mannitol, sodium hydroxide, water for injections. 
Read the package leaflet before use. 
 
 
4. PHARMACEUTICAL FORM AND CONTENTS 
 
Eye drops, solution 
1 x 2.5 ml 
 
 
5. METHOD AND ROUTE(S) OF ADMINISTRATION 
 
Read the package leaflet before use. 
Ocular use. 
 
 
6. SPECIAL WARNING THAT THE MEDICINAL PRODUCT MUST BE STORED OUT 

OF THE SIGHT AND REACH OF CHILDREN 
 
Keep out of the sight and reach of children. 
 
 
7. OTHER SPECIAL WARNING(S), IF NECESSARY 
 
 
8. EXPIRY DATE 
 
EXP 
Discard 4 weeks after first opening. 
Open date: __________ 
 
 
9. SPECIAL STORAGE CONDITIONS 
 
Store in a refrigerator until opened.  
Once opened, do not store above 25°C. 
 



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10. SPECIAL PRECAUTIONS FOR DISPOSAL OF UNUSED MEDICINAL PRODUCTS 

OR WASTE MATERIALS DERIVED FROM SUCH MEDICINAL PRODUCTS, IF 
APPROPRIATE 

 
 
11. NAME AND ADDRESS OF THE MARKETING AUTHORISATION HOLDER 
 
Aerie Pharmaceuticals Ireland, Limited 
Athlone Business and Technology Park,  
Dublin Road,  
Garrycastle,  
Athlone, Co Westmeath,  
N37 DW40,  
Ireland 
 
 
12. MARKETING AUTHORISATION NUMBER(S)  
 
EU/1/19/1400/001 
 
 
13. BATCH NUMBER 
 
Lot 
 
 
14. GENERAL CLASSIFICATION FOR SUPPLY 
 
 
15. INSTRUCTIONS ON USE 
 
 
16. INFORMATION IN BRAILLE 
 
Rhokiinsa 
 
 
17. UNIQUE IDENTIFIER – 2D BARCODE 
 
2D barcode carrying the unique identifier included. 
 
 
18. UNIQUE IDENTIFIER - HUMAN READABLE DATA 
 
PC  
SN 
NN 
 
 
  



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MINIMUM PARTICULARS TO APPEAR ON SMALL IMMEDIATE PACKAGING UNITS 
 
BOTTLE LABEL 
 
 
1. NAME OF THE MEDICINAL PRODUCT AND ROUTE(S) OF ADMINISTRATION 
 
Rhokiinsa 200 micrograms/ml eye drops 
netarsudil 
Ocular use 
 
 
2. METHOD OF ADMINISTRATION 
 
 
3. EXPIRY DATE 
 
EXP 
 
 
4. BATCH NUMBER 
 
Lot 
 
 
5. CONTENTS BY WEIGHT, BY VOLUME OR BY UNIT 
 
2.5 ml 
 
 
6. OTHER 
 
 
 
 
 
 
 
 
 
 
 
 
  



18 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 

 
B. PACKAGE LEAFLET 



19 

Package leaflet: Information for the patient 
 

Rhokiinsa 200 micrograms/ml eye drops, solution 
netarsudil  

 
This medicine is subject to additional monitoring. This will allow quick identification of new 

safety information. You can help by reporting any side effects you may get. See the end of section 4 
for how to report side effects.  
 
Read all of this leaflet carefully before you start using this medicine because it contains 

important information for you. 
- Keep this leaflet. You may need to read it again.  
- If you have any further questions, ask your doctor or pharmacist. 
- This medicine has been prescribed for you only. Do not pass it on to others. It may harm them, 

even if their signs of illness are the same as yours. 
- If you get any side effects, talk to your doctor or pharmacist. This includes any possible side 

effects not listed in this leaflet. See section 4. 
 
What is in this leaflet 
 
1. What Rhokiinsa is and what it is used for  
2. What you need to know before you use Rhokiinsa  
3. How to use Rhokiinsa  
4. Possible side effects  
5. How to store Rhokiinsa 
6. Contents of the pack and other information 
 
 
1. What Rhokiinsa is and what it is used for 
 
Rhokiinsa contains an active substance called netarsudil. Netarsudil belongs to a group of medicines 
called “Rho kinase inhibitors”, which work to reduce the amount of fluid inside the eye and so lower 
its pressure.  
 
Rhokiinsa is used to lower pressure in the eyes in adults who have an eye condition known as 
glaucoma or who have raised pressure in their eyes. If the pressure in the eye is too high, it can 
damage your sight. 
 
 
2. What you need to know before you use Rhokiinsa  
 
Do not use Rhokiinsa: 
- if you are allergic to netarsudil or any of the other ingredients of this medicine (listed in section 

6).  
 
Warnings and precautions  

• Do not use Rhokiinsa more than once a day, as you may experience more side effects. 
 
Children and adolescents 
Rhokiinsa should not be used in children and teenagers under 18 years of age as it has only been 
studied in adults.  
 
Other medicines and Rhokiinsa 
Tell your doctor or pharmacist if you are using, have recently used or might use any other medicines. 
 
  



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Pregnancy and breast-feeding  
If you are pregnant or breastfeeding, think you may be pregnant or are planning to have a baby, ask 
your doctor or pharmacist for advice before taking this medicine. Do not use Rhokiinsa if you are 
pregnant unless your doctor still recommends it. 
 
Driving and using machines 
You may find that your vision is blurred or abnormal just after using Rhokiinsa. Do not drive or use 
machines until the symptoms are cleared. 
 
Rhokiinsa contains benzalkonium chloride 
This medicine contains approximately 150 micrograms benzalkonium chloride in each ml of solution.   
 
Benzalkonium chloride may be absorbed by soft contact lenses and may change the colour of the 
contact lenses. You should remove contact lenses before using this medicine and put them back 15 
minutes afterwards.   
 
Benzalkonium chloride may also cause eye irritation, especially if you have dry eyes or disorders of 
the cornea (the clear layer at the front of the eye).  If you feel abnormal eye sensation, stinging or pain 
in the eye after using this medicine, talk to your doctor. 
 
 
3. How to use Rhokiinsa 
 
Always use this medicine exactly as your doctor or pharmacist has told you. Check with your doctor 
or pharmacist if you are not sure.  
 
Only use Rhokiinsa for your eyes (ocular use). Do not swallow or inject.  
 
The recommended dose is one drop in the affected eye or eyes once a day in the evening. Use the 
medicine at around the same time each day. 
 
How to use 
 

 
 
• Wash your hands before you start. 
• Do not touch the dropper with your fingers when opening or closing the bottle. It could infect 

the drops. 
• Twist off the bottle cap, and lie the cap on a clean surface on its side. Continue to hold the 

bottle, ensuring that the tip doesn’t come into contact with anything.  
• Hold the bottle, pointing down, between your thumb and fingers. 
• Tilt your head back. 
• Pull down your lower eyelid with a clean finger to form a ‘pocket’ between the eyelid and your 

eye. The drop will go in here (Picture 1). 
• Bring the bottle tip close to the eye. Do this in front of a mirror if it helps. 
• Do not touch your eye, eyelid, surrounding areas or other surfaces with the dropper. It could 

infect the drops. 
• Gently squeeze the bottle to release one drop of Rhokiinsa into your eye. 
• Only put one drop into your eye each time. If a drop misses your eye, try again. 



21 

• If you need to use the drops in both eyes, repeat the steps for your other eye while you have 
the bottle open. 

• Put back the bottle cap to close the bottle. 
 
If you are using other eye drops, wait at least five minutes after using them and then use Rhokiinsa. 
If you are using eye ointments, these should be used last. 
  
If you use more Rhokiinsa than you should  
Rinse your eye with warm water. Do not put in any more drops until it is time for your next regular 
dose.  
 
If you forget to use Rhokiinsa 
Continue with the next dose as planned. Do not use a double dose to make up for a forgotten dose.  
Do not use more than one drop in the affected eye(s) once a day.  
 
If you stop using Rhokiinsa 
Do not stop using Rhokiinsa without first speaking to your doctor. If you stop using Rhokiinsa the 
pressure in your eye will not be controlled which could lead to loss of sight.  
 
If you have any further questions on the use of this medicine, ask your doctor or pharmacist. 
 
 
4. Possible side effects 
 
Like all medicines, this medicine can cause side effects, although not everybody gets them.  
 
The following side effects have been observed with Rhokiinsa: 
 
Very common side effects (may affect more than 1 in 10 people) 
• Effects in the eye: Eye redness; fine deposits on the front of the eye and pain where the drops 

have been put in  
 
Common side effects (may affect up to 1 in 10 people) 
• Effects in the eye: Infection or inflammation of the eye; dryness of the eye or small breaks in the 

film of liquid on the surface of the eye; eye discharge; itchy eyelids; clouding of the eye and 
vision may decrease somewhat; eye pain; feeling of grittiness or having something in the eye; 
general eye redness shortly after drops are put in; spots or patches of eye redness; eye 
inflammation caused by an allergic reaction or prominent blood vessels; eyes can become 
watery, sensitive to light; swelling around the eye; blurred vision  

• General side effects: Headache 
 
Uncommon side effects (may affect up to 1 in 100 people) 
• Effects in the eye: Increased fluid pressure inside the eye; inflammation of the coloured part of 

the eye (the iris); bulging of iris; growth of eyelashes; eyelid dryness; eye disease related to 
diabetes; excess folds of the conjunctiva; blindness; blurred, double and halo vision; cataracts; 
abnormal turning outward of the lower eyelid; small colored spots on the eye surface; eye 
dryness caused by inflammation of the glands of the eyelids; eye allergy; eyelid crusting; glassy 
eyes; loss of eyelashes; tiredness 

• General side effects: Increased allergic symptoms; dizziness; blurred vision; nasal discomfort 
and pain; redness or itching of the skin; rash on skin; inflammation of the cartilage; picking of 
the skin  

 
Reporting of side effects 
If you get any side effects, talk to your doctor,  or pharmacist. This includes any possible side effects 
not listed in this leaflet. You can also report side effects directly via the national reporting system 



22 

listed in Appendix V. By reporting side effects you can help provide more information on the safety of 
this medicine. 
 
 
5. How to store Rhokiinsa 
 
Keep this medicine out of the sight and reach of children. 
 
Do not use this medicine after the expiry date which is stated on the bottle and the carton after “EXP”. 
The expiry date refers to the last day of that month. 
 
Unopened bottles: Store in a refrigerator (2°C - 8°C). 
After opening the bottle: Do not store above 25°C. 
Throw away the bottle 4 weeks after first opening to prevent infections and use a new bottle.  
 
Do not throw away any medicines via wastewater or household waste. Ask your pharmacist how to 
throw away medicines you no longer use. These measures will help protect the environment. 
 
 
6. Contents of the pack and other information 
 
What Rhokiinsa contains  
- The active substance is netarsudil. Each ml of solution contains 200 micrograms netarsudil (as 

mesylate).  
- The other excipients are benzalkonium chloride (see section 2 under ‘Rhokiinsa contains 

benzalkonium chloride’), mannitol, boric acid, sodium hydroxide and water for injections.  
 
What Rhokiinsa looks like and contents of the pack 
Rhokiinsa is a clear, liquid eye drop solution in a plastic bottle. Each bottle contains 2.5 ml of the 
medicine and each pack contains one bottle with a screw-cap.  
 
Marketing Authorisation Holder and Manufacturer 
Aerie Pharmaceuticals Ireland, Limited 
Athlone Business and Technology Park,  
Dublin Road,  
Garrycastle,  
Athlone, Co Westmeath,  
N37 DW40,  
Ireland 
 
This leaflet was last revised in  
 
Other sources of information 
 
Detailed information on this medicine is available on the European Medicines Agency web site: 
http://www.ema.europa.eu. 
 

 
 


	SUMMARY OF PRODUCT CHARACTERISTICS
	A. MANUFACTURER(S) RESPONSIBLE FOR BATCH RELEASE
	B. CONDITIONS OR RESTRICTIONS REGARDING SUPPLY AND USE
	C. OTHER CONDITIONS AND REQUIREMENTS OF THE MARKETING AUTHORISATION
	D. CONDITIONS OR RESTRICTIONS WITH REGARD TO THE SAFE AND EFFECTIVE USE OF THE MEDICINAL PRODUCT
	A. LABELLING
	B. PACKAGE LEAFLET