loteprednol ophthalmic (Rx)

Brand and Other Names:Alrex, Lotemax, more...Inveltys, Lotemax SM
  • Print

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

ophthalmic suspension

  • 0.2% (Alrex)
  • 0.5% (Lotemax)
  • 1% (Inveltys)

ophthalmic ointment

  • 0.5% (Lotemax)

ophthalmic gel

  • 0.38% (Lotemax SM)
  • 0.5% (Lotemax)

Postoperative Inflammation

Indicated for treatment of postoperative inflammation and pain following ocular surgery

Inveltys

  • Instill 1-2 drops into affected eye(s) BID beginning the day after surgery and continuing throughout the first 2 weeks postoperatively

Lotemax

  • Gel or suspension: Apply 1-2 drops into conjunctival sac of affected eye(s) QID beginning the day after surgery and continuing throughout the first 2 weeks postoperatively
  • Ointment: Apply ~0.5 inch ribbon into conjunctival sac(s) QID beginning the day after surgery and continuing throughout the first 2 weeks postoperatively

Lotemax SM

  • Apply 1 drop of gel into conjunctival sac of affected eye(s) TID beginning the day after surgery and continuing throughout the first 2 weeks postoperatively

Seasonal Allergic Conjunctivitis

Indicated for temporary relief of signs and symptoms of seasonal allergic conjunctivitis

Alrex

  • Instill 1 drop into affected eye(s) QID

Steroid Responsive Inflammatory Conditions

Indicated for steroid responsive inflammatory conditions of the palpebral and bulbar conjunctiva, cornea and anterior segment of the globe (eg, allergic conjunctivitis, acne rosacea, superficial punctate keratitis, herpes zoster keratitis, iritis, cyclitis, selected infective conjunctivitides) when steroid use is accepted to obtain an advisable diminution in edema and inflammation

Lotemax

  • Suspension only
  • Apply 1-2 drops into the conjunctival sac of affected eye(s) QID
  • During initial treatment within the first week, may increase dose up to 1 drop q1hr, if necessary
  • Do not to discontinue therapy prematurely; if signs and symptoms fail to improve after 2 days, re-evaluate patient

Dosage Forms & Strengths

ophthalmic suspension

  • 0.5% (Lotemax)

ophthalmic ointment

  • 0.5% (Lotemax)

ophthalmic gel

  • 0.5% (Lotemax)

Postoperative Inflammation

Indicated for treatment of postoperative inflammation and pain following ocular surgery

Lotemax

  • Gel or suspension: Apply 1-2 drops into conjunctival sac of affected eye(s) QID beginning the day after surgery and continuing throughout the first 2 weeks postoperatively
  • Ointment: Apply ~0.5 inch ribbon into conjunctival sac(s) QID beginning the day after surgery and continuing throughout the first 2 weeks postoperatively

Steroid Responsive Inflammatory Conditions

Indicated for steroid responsive inflammatory conditions of the palpebral and bulbar conjunctiva, cornea and anterior segment of the globe (eg, allergic conjunctivitis, acne rosacea, superficial punctate keratitis, herpes zoster keratitis, iritis, cyclitis, selected infective conjunctivitides) when steroid use is accepted to obtain an advisable diminution in edema and inflammation

Lotemax

  • Suspension only
  • Apply 1-2 drops into the conjunctival sac of affected eye(s) QID
  • During initial treatment within the first week, may increase dose up to 1 drop q1hr, if necessary
  • Do not to discontinue therapy prematurely; if signs and symptoms fail to improve after 2 days, re-evaluate patient
Next:

Adverse Effects

>10%

Lotemax ointment only

  • Anterior chamber inflammation (~25%)

5-15%

Lotemax suspension only

  • Abnormal vision/blurring
  • Burning on instillation
  • Chemosis
  • Discharge
  • Dry eyes
  • Epiphora
  • Foreign body sensation
  • Itching
  • Photophobia

<5%

Lotemax gel

  • Anterior chamber inflammation (5%)
  • Eye pain (2%)
  • Foreign body sensation (2%)

Lotemax suspension only

  • Conjunctivitis
  • Corneal abnormalities
  • Eyelid erythema
  • Keratoconjunctivitis
  • Ocular irritation/pain/discomfort
  • Papillae
  • Uveitis

Lotemax ointment

  • Conjunctival hyperemia (4-5%)
  • Corneal edema (4-5%)
  • Eye pain (4-5%)
  • Headache (1.5%)

Frequency Not Defined

Inveltys only

  • Infrequent optic nerve damage
  • Visual acuity and field defects
  • Posterior subcapsular cataract formation
  • Delayed wound healing
  • Secondary ocular infection from pathogens (eg, herpes simplex)
  • Perforation of the globe where there is thinning of the cornea or sclera
Previous
Next:

Warnings

Contraindications

Hypersensitivity to any component of the formulation

Most viral diseases of the cornea and conjunctiva including epithelial herpes simplex keratitis (dendritic keratitis), vaccinia, and varicella, and also in mycobacterial infection of the eye and fungal diseases of ocular structures

Cautions

Prolonged use of corticosteroids may result in glaucoma with damage to the optic nerve, defects in visual acuity and fields of vision; use with caution in the presence of glaucoma; if product is used for ≥10 days, monitor intraocular pressure (IOP)

Use of corticosteroids may result in posterior subcapsular cataract formation

Steroid use after cataract surgery may delay healing and increase the incidence of bleb formation; diseases causing thinning of the cornea or sclera, perforations have been known to occur with the use of topical steroids; examine patient prior to initiating or renewing treatment

Prolonged use of corticosteroids may suppress the host response and thus increase the risk of secondary ocular infections; steroids may mask infection or enhance existing infection

Exercise caution with steroid use in patients with a history of herpes; use of ocular steroids may prolong the course and may exacerbate the severity of many viral infections of the eye (eg, herpes simplex)

Fungal infections of the cornea are particularly prone to develop coincidentally with long-term local steroid application; consider fungus invasion in any persistent corneal ulceration where a steroid has been used or is in use; take fungal cultures when appropriate

Do not wear contact lenses during therapy

Previous
Next:

Pregnancy & Lactation

Pregnancy

Inveltys

  • Drug is not absorbed systemically following topical ophthalmic administration and maternal use is not expected to result in fetal exposure to drug

Lotemax and Alrex

  • There are no adequate and well controlled studies in pregnant women; use during pregnancy only if the potential benefit justifies the potential risk to the fetus
  • Animal data
    • Drug shown to be embryotoxic (delayed ossification) and teratogenic (increased incidence of meningocele, abnormal left common carotid artery, and limb flexures) when administered orally to rabbits during organogenesis at a dose of 3 mg/kg/day (35 times the maximum daily clinical dose), a dose which caused no maternal toxicity; no-observed-effect-level (NOEL) for these effects was 0.5 mg/kg/day (6 times the maximum daily clinical dose)
    • Oral treatment of rats during organogenesis resulted in teratogenicity (absent innominate artery at ≥5 mg/kg/day doses, and cleft palate and umbilical hernia at ≥50 mg/kg/day) and embryotoxicity (increased post-implantation losses at 100 mg/kg/day and decreased fetal body weight and skeletal ossification with ≥50 mg/kg/day)
    • Treatment of rats with 0.5 mg/kg/day (6 times the maximum clinical dose) during organogenesis did not result in any reproductive toxicity; loteprednol etabonate was maternally toxic (significantly reduced body weight gain during treatment) when administered to pregnant rats during organogenesis at doses of ≥5 mg/kg/day
    • Oral exposure of female rats to 50 mg/kg/day of loteprednol etabonate from the start of the fetal period through the end of lactation, a maternally toxic treatment regimen (significantly decreased body weight gain), gave rise to decreased growth and survival, and retarded development in the offspring during lactation; NOEL for these effects was 5 mg/kg/day; no effect on the duration of gestation or parturition when administered orally to pregnant rats at doses up to 50 mg/kg/day during the fetal period

Lactation

Inveltys

  • Drug is not absorbed systemically by the mother following topical ophthalmic administration, and breastfeeding is not expected to result in exposure of the child

Lotemax and Alrex

  • There are no data on presence of loteprednol etabonate in human milk, effects on breastfed infant, or on milk production; developmental and health benefits of breastfeeding should be considered, along with mother’s clinical need for therapy and any potential adverse effects on breastfed infant
  • It is not known whether topical ophthalmic administration of corticosteroids could result in sufficient systemic absorption to produce detectable quantities in human milk
  • Systemic steroids appear in human milk and could suppress growth, interfere with endogenous corticosteroid production, or cause other untoward effects

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Previous
Next:

Pharmacology

Mechanism of Action

There is no generally accepted explanation for the mechanism of action of ocular corticosteroids

However, corticosteroids are thought to act by the induction of phospholipase A2 inhibitory proteins, collectively called lipocortins

It is believed that these proteins control the biosynthesis of potent mediators of inflammation (eg, prostaglandins, leukotrienes) by inhibiting the release of arachidonic acid

Arachidonic acid is released from membrane phospholipids by phospholipase A2

Corticosteroids are capable of producing a rise in IOP

Absorption

Following topical instillation into the conjunctival sac, absorbed into the aqueous humor and minimal systemic absorption occurs

Submicron particles (Lotemax SM) have faster dissolution in tears and twice the penetration into aqueous humor compared with original Lotemax formulation

Metabolism

Based upon in vivo and in vitro preclinical metabolism studies, loteprednol etabonate undergoes extensive metabolism to inactive carboxylic acid metabolites, PJ-91 and PJ-90

Previous
Next:

Administration

Ophthalmic Administration

Inveltys: Shake bottle 1-2 seconds before using

Alrex and Lotemax suspension: Shake vigorously before using

Lotemax or Lotemax SM gel: Invert closed bottle and shake once to fill tip before instilling drops

Lotemax ointment

  • Do not to touch the eyelid or surrounding areas with the tip of the tube
  • Keep cap on the tube when not in use
  • Wash hands prior to using ointment; do not use if tamper evident skirt is visible on bottom of cap

Storage

All formulations

  • Do not use if tamper-evident overcap seal is not intact
  • Store upright at 15-25°C (59-77°F); do not freeze
Previous
Next:

Images

Previous
Next:

Formulary

FormularyPatient Discounts

Adding plans allows you to compare formulary status to other drugs in the same class.

To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

Adding plans allows you to:

  • View the formulary and any restrictions for each plan.
  • Manage and view all your plans together – even plans in different states.
  • Compare formulary status to other drugs in the same class.
  • Access your plan list on any device – mobile or desktop.

The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

Tier Description
1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
NC NOT COVERED – Drugs that are not covered by the plan.
Code Definition
PA Prior Authorization
Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
QL Quantity Limits
Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
ST Step Therapy
Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
OR Other Restrictions
Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
Additional Offers
Email to Patient

From:

To:

The recipient will receive more details and instructions to access this offer.

By clicking send, you acknowledge that you have permission to email the recipient with this information.

Email Forms to Patient

From:

To:

The recipient will receive more details and instructions to access this offer.

By clicking send, you acknowledge that you have permission to email the recipient with this information.

Previous
Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.