Netarsudil, sold under the brand name Rhopressa among others, is a medication for the treatment of glaucoma. In the United States, in December 2017, the Food and Drug Administration (FDA) approved a 0.02% ophthalmic solution for the lowering of elevated intraocular pressure in people with open-angle glaucoma or ocular hypertension. The European Medicines Agency approved it in 2019 for the same uses under the brand name Rhokiinsa.The FDA considers it to be a first-in-class medication. Contraindications
Netarsudil has no contraindications apart from known hypersensitivity to the drug. Adverse effects
The most common side effects are hyperaemia (increased blood flow associated with redness, in 51% of patients) in the conjunctiva, cornea verticillata (drug deposits in the cornea, in 17%), and eye pain (in 17%). All other side effects occur in fewer than 10% of people. Hypersensitivity reactions occur in fewer than 1%. Overdose
Overdosing netarsudil is unlikely because concentrations in the body are so low that they are generally not detectable. Interactions
No interaction studies have been done. The European label recommends to apply other eye drops at least five minutes before, and eye ointments at least five minutes after netarsudil drops. Pharmacology
Mechanism of action
This drugs mechanism of action is not entirely clear. It inhibits the enzyme rho kinase. This appears to increase outflow of aqueous humor through the trabecular meshwork, and also to reduce pressure in the veins of the episcleral layer. The drug also inhibits the norepinephrine transporter. Pharmacokinetics
After instillation into the eye, netarsudil is cleaved by esterases in the cornea to AR-13503, which is the active metabolite.
Lisinopril is a medication of the angiotensin-converting enzyme (ACE) inhibitor and is used to treat high blood pressure, heart failure, and after heart attacks. For high blood pressure it is usually a first-line treatment. It is also used to prevent kidney problems in people with diabetes mellitus. Lisinopril is taken by mouth. Full effect may take up to four weeks to occur.Common side effects include headache, dizziness, feeling tired, cough, nausea, and rash. Serious side effects may include low blood pressure, liver problems, high blood potassium, and angioedema. Use is not recommended during the entire duration of pregnancy as it may harm the baby. Lisinopril works by inhibiting the renin–angiotensin–aldosterone system.Lisinopril was patented in 1978 and approved for medical use in the United States in 1987. It is available as a generic medication. In 2020, it was the fourth most commonly prescribed medication in the United States, with more than 88 million prescriptions. In July 2016, an oral solution formulation of lisinopril was approved for use in the United States. Structure–activity relationships
Lisinopril has a proline group that is responsible for the availability of the drug in oral formulation. The carboxylate group interacts with zinc ions to inhibit the ACE enzyme found in the kidneys and lungs. The other substituents participate in binding the same enzyme. Unlike Captopril, another ACE Inhibitor, Lisinopril lacks a thiol group. Medical uses
Lisinopril is typically used for the treatment of high blood pressure, congestive heart failure, and diabetic nephropathy and after acute myocardial infarction (heart attack).