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netarsudil

Rho kinase inhibitor (ophthalmic, IOP-lowering) · Antiglaucoma agent

START
1 drop 0.02% in affected eye(s) once daily in evening
TYPICAL MAX
1 drop once daily per eye (do not dose more often)
STOP IF
Vision-affecting corneal deposits or hypersensitivity
WATCH
IOP response, corneal status, conjunctival hyperaemia
CDSCO approvedATC S01EX05
Renal dose adjustmenteGFR mL/min/1.73m²
FULLNo dose adjustment (negligible systemic)90

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours
1hONSET3hPEAK30min1dDURATION
ONSET
1h · IOP fall
PEAK
3h · peak effect
30min · local
DURATION
1d · once-daily
EXCRETION
Negligible systemic; local ocular
route + CYP
INTERACTIONS
none in our sources
PREGNANCY
Limited data; use only if benefit outweighs risk.
FDA category + note

Mechanism

Inhibits Rho-associated kinase (and norepinephrine transporter), increasing trabecular-meshwork outflow and reducing episcleral venous pressure and aqueous production — lowering intraocular pressure.

Indications

Elevated intraocular pressure in open-angle glaucomaOcular hypertension

Dosing

Adult
1 drop of 0.02% in the affected eye(s) once daily in the evening.
Pediatric
Not established.
Renal adjustment
No adjustment (negligible systemic absorption).
Hepatic adjustment
No adjustment.
Geriatric
No specific adjustment.
Max dose
1 drop once daily per eye (more frequent dosing less effective/more hyperaemia)

Pharmacokinetics

Onset
IOP reduction within hours
Peak effect
~2–4 h post-instillation; max effect over weeks
Duration
~24 h (once-daily)
Half-life
Local (negligible systemic exposure)
Bioavailability
Negligible systemic
Protein binding
Not relevant systemically
Metabolism
Ocular esterases (active metabolite)
Excretion
Negligible systemic; local

Contraindications

  • Hypersensitivity to netarsudil

Side effects

Common
Conjunctival hyperaemiaCorneal verticillata (whorl deposits)Conjunctival haemorrhageInstillation-site painBlurred vision
Serious
  • Corneal deposits affecting vision (rare, usually reversible)
  • Severe hypersensitivity

Pregnancy & lactation

Pregnancy

Limited data; use only if benefit outweighs risk.

Lactation

Unknown excretion in milk; caution.

Drug interactions

Contact Lenses
Mild
Database

Benzalkonium absorption by lenses

Remove lenses; reinsert after 15 min

Source: Kimi deep-research + Cla

Other Topical Iop Lowering Agents
Mild
Database

Additive IOP reduction (intended)

Separate instillation by ≥5 min

Source: Kimi deep-research + Cla

Prostaglandin Analogues
Mild
Database

Complementary outflow mechanisms

Common combination; space instillation

Source: Kimi deep-research + Cla

Systemic Drugs
Mild
Database

Negligible systemic absorption

No action required

Source: Kimi deep-research + Cla

Topical Nsaids
Mild
Database

No significant systemic interaction

Routine ophthalmic co-use acceptable

Source: Kimi deep-research + Cla

Related guidelines

Ask House about netarsudil

Continue into a citation-backed clinical answer with the drug context already attached.

Sources: Goodman & Gilman 14e·Verified: 2026-05-20 · House clinical team·Cockpit curated: 2026-05-20