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7 of 216 medications
Aceclidine 1.44%
Vizz®Aesthetics/Presbyopia
Approved uses
Presbyopia
One drop in each eye, wait 2 minutes, then a second drop in each eye, once daily
Contraindications
None.
Available FormsOphthalmic solution, aceclidine 1.44% preservative-free single-dose vials, carton of 25 vials of 0.4 mL, carton of 25 vials of 0.25 mL
Mechanism of ActionCholinergic muscarinic agonist and predominantly pupil selective miotic that contracts the iris sphincter with minimal ciliary muscle stimulation. The resulting small pupil creates a pinhole effect that extends depth of focus.
Warnings & Precautions
- Dim or dark vision: Temporary after instillation; caution with night driving and other hazardous activity in poor illumination.
- Accommodative spasm: Miotics may cause it; no driving or machinery while vision is not clear.
- Retinal tear and detachment: Rare reports with miotics in susceptible individuals and those with pre-existing retinal disease. Retinal examination advised in all patients before initiation, and immediate care for sudden flashing lights, floaters, or vision loss.
- History of iritis: Miotic use may exacerbate sequelae of ocular inflammation, including synechiae between iris and lens.
- Hypersensitivity: Not recommended with known hypersensitivity to aceclidine or any component of the solution.
- Vial contamination and eye injury: Avoid touching the single-dose vial to the eye or any other surface, and discard it after use.
Common Side Effects
- Ocular: Instillation site irritation 20%, dim vision 16%, conjunctival hyperemia 8%, ocular hyperemia 7%.
- Systemic: Headache 13%.
- Severity: Majority of reactions mild, transient, and self-resolving.
Pregnancy & LactationPregnancy: No adequate and well-controlled studies in pregnant women. Oral dosing of pregnant rats and rabbits throughout organogenesis and lactation produced no maternal, fetal, or neonatal effects at clinically relevant doses.
Lactation: No information on presence in human or animal milk, effects on the breastfed infant, or effects on milk production; systemic levels after topical ocular dosing are low.
Pediatric UsePresbyopia does not occur in the pediatric population.
Bimatoprost 0.03%
Latisse®Aesthetics/Presbyopia
Approved uses
Eyelash hypotrichosis
One drop on a sterile applicator applied along the skin of the upper eyelid margin at the base of the lashes, once nightly, one applicator per eye
Most see no visible change before 2 months, and lashes return to baseline after stopping.
Eyelash hypotrichosis after chemotherapy
One drop on a sterile applicator applied to the upper eyelid margin, once nightly, one applicator per eye
About 4 in 10 respond by month 4 after chemotherapy, with further gain out to 12 months.
OFF-LABELNot in the FDA label for this product
Eyebrow hypotrichosis
Bimatoprost 0.03% solution applied to each eyebrow once daily; the trial dosed daily for 9 months
Pilot RCT · n=20
Randomized, double-blind, vehicle-controlled pilot study, n=20 with mild to moderate eyebrow hypotrichosis. Investigator-assessed eyebrow appearance improved from baseline at 6 months (P=.002) and 7 months (P=.005) in the group treated for 9 months, while the group crossed to 4 months of bimatoprost was not significant at any time point and no adverse effects were observed; pilot-sized, so the estimate is imprecise.
Contraindications
Hypersensitivity to bimatoprost or any component
Available Forms0.03% (0.3 mg/mL) solution, 3 mL bottle with 70 applicators, 5 mL bottle with 140 applicators
Mechanism of ActionStructural prostaglandin analog. The precise mechanism is unknown; lash growth is attributed to increasing the percentage of hairs in the anagen phase and prolonging that phase.
Warnings & Precautions
- IOP-lowering interference: In patients using a prostaglandin analog for elevated IOP, concomitant use may blunt the desired IOP reduction; monitor IOP closely. In trials, in patients with or without elevated IOP, IOP fell, but the magnitude was not judged clinically concerning.
- Iris pigmentation: Increased brown iris pigmentation, likely permanent, from increased melanin content in melanocytes rather than more melanocytes. Spreads concentrically from the pupil and may take months to years to appear; treatment can be continued.
- Lid pigmentation: Darkening of periorbital tissue and lashes, expected to increase as long as dosing continues; reported reversible on discontinuation in most patients.
- Hair growth outside treatment area: Repeated skin contact beyond the upper eyelid margin can grow hair there; blot runoff before it reaches the cheek or other skin.
- Intraocular inflammation: Caution with active intraocular inflammation such as uveitis, which may be exacerbated.
- Macular edema: Cystoid macular edema reported with bimatoprost given for elevated IOP; caution in aphakia, pseudophakia with a torn posterior capsule, or other risk factors for macular edema.
- Applicator contamination: One applicator per eye, then discard; bottle tip must not touch any surface. Bacterial keratitis has been reported with contaminated multiple-dose ophthalmic containers.
- Benzalkonium chloride: May be absorbed by and discolor soft contact lenses; remove lenses before application and reinsert 15 minutes after.
Common Side Effects
- Ocular, most common: Eye pruritus and conjunctival hyperemia, each approximately 3% to 4%; ocular irritation and dry eye symptoms under 4%; foreign body sensation reported without a frequency.
- Periocular skin: Skin hyperpigmentation approximately 3% to 4%; periorbital erythema under 4%; dry skin and skin exfoliation of the eyelid or periocular area postmarketing.
- Pigmentation: Iris hyperpigmentation and periorbital skin discoloration.
- Lash changes: Abnormal hair growth, madarosis, trichorrhexis, and trichiasis; disparity between eyes in length, thickness, pigmentation, number, or direction of lashes.
- Periorbital fat atrophy: Skin tightness with deepening of the eyelid sulcus and eyelid ptosis; postmarketing.
- Other ocular, postmarketing: Eye swelling, eyelid edema, hordeolum, increased lacrimation, blurred vision, local allergic reactions.
- Systemic, reported with the IOP-lowering formulation: Headache, asthenia, colds and upper respiratory infections.
Pregnancy & LactationPregnancy: No adequate and well-controlled studies in pregnant women; postmarketing experience shows no increase in major birth defects or miscarriage. Oral dosing during organogenesis caused abortion and early delivery in mice and rats at oral doses at least 33 times (mice) and 94 times (rats) human exposure by AUC, and these effects were not seen at 2.6 times (mice) or 47 times (rats). Use only if the benefit justifies fetal risk.
Lactation: Unknown whether topical ocular use yields detectable quantities in human milk; present in rat milk at an IV dose 324 times the recommended human ophthalmic dose on a mg/m2 basis.
Pediatric UseStudied in patients 5 to 17 with no new safety issues; benefit seen only in adolescents 15 to 17 with hypotrichosis.
Brimonidine 0.025%
Lumify®Aesthetics/Presbyopia
Approved uses
Ocular redness from minor eye irritation
1 drop in the affected eye(s) every 6 to 8 hours, maximum 4 times daily
Redness is reduced for 8 hours, with no tachyphylaxis or rebound through 29 days of use.
Contraindications
- Do not use if the solution changes color or becomes cloudy
- The label gives no other condition under which the drops must not be used
Available FormsOphthalmic solution, 0.025% (0.25 mg/mL), 2.5 mL, 3.5 mL, 5 mL, 7.5 mL dropper bottles
Mechanism of ActionHighly selective alpha-2 adrenergic receptor agonist producing conjunctival vasoconstriction and blanching. Alpha-2 selectivity is the point of difference from the alpha-1 and mixed alpha-1/alpha-2 decongestants (phenylephrine, tetrahydrozoline, naphazoline, oxymetazoline), which are associated with tachyphylaxis and rebound redness.
Warnings & Precautions
- Persistent redness: Eye pain, vision change, or redness or irritation that worsens or lasts more than 3 days warrants examination rather than continued use.
- Scotopic miosis: Uncontrolled before-after study in 28 healthy adults found mean scotopic pupil diameter fell from 7.28 mm to 6.36 mm 60 minutes after instillation, with a larger effect in light irides than dark (1.55 mm vs 0.67 mm).
Common Side Effects
- Ocular: In pooled trial safety data (426 treated, 209 vehicle), reduced visual acuity 4.0% and conjunctival hyperemia 2.6%, both at vehicle rates (4.3% and 2.9%).
- Systemic: Not characterized; this OTC label has no adverse reactions section and the pooled analysis reported ocular events.
Pregnancy & LactationPregnancy: No data in this OTC label.
Lactation: No data in this OTC label.
Pediatric UseLabeled for age 5 years and over; under 5, the label directs consultation.
Carbachol 2.75% / Brimonidine Tartrate 0.1%
Yuvezzi®Aesthetics/Presbyopia
GoodRxApproved uses
Presbyopia in adults
One drop in each eye once daily
Pairs a cholinergic agonist with an alpha agonist, so miosis comes with a whitening effect
Contraindications
Known hypersensitivity to the active ingredients or to any of the excipients.
Available FormsCarbachol and brimonidine tartrate ophthalmic solution 2.75% / 0.1%.
Mechanism of ActionThe proposed mechanism of action of this fixed-dose combination of carbachol and brimonidine in presbyopia is pupillary constriction and the creation of a pinhole effect that improves near visual acuity and depth of focus.
Warnings & Precautions
- Blurred vision: advise patients not to drive or operate machinery when vision is not clear, and to take care with night driving.
- Retinal detachment has been reported with miotics; advise patients to report a sudden loss of vision at once.
- Iritis: not recommended in active iritis.
- Remove contact lenses before instillation.
Common Side Effects
Most common adverse reactions (incidence >5%) are eye pain upon instillation, visual impairment, eye irritation upon instillation, and headache.
Pregnancy & LactationPregnancy: No adequate and well-controlled studies in pregnant women.
Lactation: No data on presence in human milk.
Pediatric UsePresbyopia does not occur in the pediatric population.
Oxymetazoline 0.1%
Upneeq®Aesthetics/Presbyopia
Approved uses
Acquired blepharoptosis
1 drop into one or both ptotic eyes once daily
Lid elevation is measurable at 5 minutes, peaks near 2 hours, and persists through 8 hours.
OFF-LABELNot in the FDA label for this product
Ptosis of ocular myasthenia gravis
1 drop in the ptotic eye once daily, the labeled frequency
Case report
Single case report, one 68-year-old patient: one drop raised MRD1 by 2.0 mm and gained 15 points on a superior 36-point field screening within 2 hours, with the effect lasting at least 7 hours. The untreated contralateral lid fell, which the authors suggest may be specific to myasthenia. N of 1, no controlled data.
Cosmetic eyelid elevation and conjunctival redness in patients without severe ptosis
1 drop in each eye once daily, the labeled frequency
RCT · n=114 · single dose
Randomized double-masked single-center trial, N=114 (57 treated, 57 control), mean ages 36 and 31: two hours after one drop, MRD1 changed 0.9 mm versus -0.3 mm with placebo (p<0.001) and redness scores fell 2.6 versus 0.5 (p=0.002), with better patient-perceived appearance (p=0.002). Adverse events were all mild and did not differ between groups; the trial measured a single instillation, not chronic use.
Contraindications
None.
Available FormsOphthalmic solution, carton of 30 single patient-use containers, 0.3 mL each, oxymetazoline HCl 0.1% (1 mg/mL, equivalent to 0.09% oxymetazoline base)
Mechanism of ActionAlpha adrenoceptor agonist acting on a subset of adrenoreceptors in Müller's muscle of the eyelid. Marginal reflex distance 1 reaches its maximum increase about 2 hours after dosing and the increase continues through 8 hours.
Warnings & Precautions
- Ptosis from neurologic disease: Rule out stroke, cerebral aneurysm, Horner syndrome, myasthenia gravis, external ophthalmoplegia, orbital infection, and orbital masses, particularly with decreased levator function or other neurologic signs.
- Cardiovascular effects: Alpha-adrenergic agonists may impact blood pressure; caution in severe or unstable cardiovascular disease, orthostatic hypotension, and uncontrolled hypertension or hypotension.
- Vascular insufficiency: Caution in cerebral or coronary insufficiency and in Sjögren's syndrome; watch for signs of potentiation.
- Angle closure glaucoma: Risk may increase in untreated narrow-angle glaucoma; pain, redness, blurred vision, and photophobia warrant immediate evaluation.
- Container contamination: Tip contact with the eye or any surface risks injury and contamination of this unpreserved solution.
- Antihypertensives and cardiac glycosides: Caution with beta-blockers, antihypertensives, cardiac glycosides, and alpha-adrenergic antagonists used for cardiovascular disease or benign prostatic hypertrophy.
- MAO inhibitors: Caution, since they affect the metabolism and uptake of circulating amines.
- Pediatric ingestion: Accidental oral ingestion of imidazolines by children has caused hospitalization, including bradycardia, hypotension, sedation, and coma.
Common Side Effects
- Ocular (1-5%): Punctate keratitis, conjunctival hyperemia, dry eye, blurred vision, instillation site pain, eye irritation.
- Systemic (1-5%): Headache.
Pregnancy & LactationPregnancy: No human data. No adverse developmental effects in rats or rabbits at up to 7 and 278 times the maximum recommended human ophthalmic dose respectively; maternal toxicity with delayed skeletal ossification occurred at the highest rabbit dose.
Lactation: No human data on milk levels or milk production; oxymetazoline was detected in the milk of lactating rats.
Pediatric UseSafety and effectiveness not established under 13 years of age.
Pilocarpine
Qlosi® · Vuity®Aesthetics/Presbyopia
GoodRxApproved uses
Presbyopia in adults
One drop in each eye, repeatable once after 2 to 3 hours for an effect lasting up to 8 hours; daily or as needed
A low-concentration, preservative-free pilocarpine: the 0.4% strength is chosen to limit brow ache and dim vision
Contraindications
Hypersensitvity
Available FormsPilocarpine hydrochloride ophthalmic solution 0.4% in single-dose vials.
Mechanism of ActionPilocarpine hydrochloride is a cholinergic muscarinic agonist which activates muscarinic receptors located at smooth muscles such as the iris sphincter muscle and ciliary muscle. QLOSI contracts the iris sphincter muscle, constricting the pupil to enhance the depth of focus and improve near visual acuity while maintaining some pupillary response to light.
Warnings & Precautions
- Blurred vision: advise patients not to drive or operate machinery when vision is not clear, and to take care with night driving.
- Retinal detachment has been reported with miotics; advise patients to report a sudden loss of vision at once.
- Iritis: not recommended in active iritis.
- Remove contact lenses before instillation.
Common Side Effects
Most common adverse reactions (5% to 8%) are instillation site pain and headaches.
Pregnancy & LactationPregnancy: No adequate and well-controlled studies in pregnant women.
Lactation: No data on presence in human milk.
Pediatric Use≥45 years