Identification

Name
Loteprednol
Accession Number
DB00873  (APRD01078)
Type
Small Molecule
Groups
Approved
Description

Loteprednol (as Loteprednol Etabonate) is a topical corticoid antiinflammatory. It is used in ophthalmic solution for the treatment of steroid responsive inflammatory conditions of the eye such as allergic conjunctivitis, uveitis, acne rosacea, superficial punctate keratitis, herpes zoster keratitis, iritis, cyclitis, and selected infective conjunctivitides. As a nasal spray, is used for the treatment and management of seasonal allergic rhinitis.

Structure
Thumb
Synonyms
  • Loteprednol
  • Loteprednolum
External IDs
CDDD 5604 / HGP 1 / P 5604
Product Ingredients
IngredientUNIICASInChI Key
Loteprednol etabonateYEH1EZ96K682034-46-6DMKSVUSAATWOCU-HROMYWEYSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
AlrexSuspension / drops2 mg/mLOphthalmicBauch & Lomb Incorporated1998-03-09Not applicableUs
AlrexSuspension / drops2 mg/mLOphthalmicStat Rx USA1998-03-09Not applicableUs
AlrexSuspension / drops2 mg/mLOphthalmicPhysicians Total Care, Inc.2002-10-17Not applicableUs
AlrexSuspension0.2 %OphthalmicBausch & Lomb Inc2009-06-24Not applicableCanada
LotemaxOintment5 mg/gOphthalmicBauch & Lomb Incorporated2011-04-15Not applicableUs
LotemaxSuspension / drops5 mg/mLOphthalmicPhysicians Total Care, Inc.2002-10-17Not applicableUs
LotemaxGel5 mg/gOphthalmicBauch & Lomb Incorporated2012-10-12Not applicableUs
LotemaxSuspension0.5 %OphthalmicBausch & Lomb Inc2009-06-24Not applicableCanada
LotemaxSuspension / drops5 mg/mLOphthalmicBauch & Lomb Incorporated1998-03-09Not applicableUs
Lotemax GelGel0.5 %OphthalmicBausch & Lomb Inc2015-06-25Not applicableCanada
International/Other Brands
Loteflam (Cipla Pharmaceuticals Limited)
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
ZyletLoteprednol etabonate (5 mg/mL) + Tobramycin (3 mg/mL)Suspension / dropsOphthalmicBauch & Lomb Incorporated2004-12-14Not applicableUs
Categories
UNII
Z8CBU6KR16
CAS number
129260-79-3
Weight
Average: 394.889
Monoisotopic: 394.154701681
Chemical Formula
C21H27ClO5
InChI Key
YPZVAYHNBBHPTO-MXRBDKCISA-N
InChI
InChI=1S/C21H27ClO5/c1-19-7-5-13(23)9-12(19)3-4-14-15-6-8-21(26,18(25)27-11-22)20(15,2)10-16(24)17(14)19/h5,7,9,14-17,24,26H,3-4,6,8,10-11H2,1-2H3/t14-,15-,16-,17+,19-,20-,21-/m0/s1
IUPAC Name
chloromethyl (1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0.0²,⁷.0¹¹,¹⁵]heptadeca-3,6-diene-14-carboxylate
SMILES

Pharmacology

Indication

As an ophthalmic it is used for the treatment of steroid responsive inflammatory conditions of the eye such as allergic conjunctivitis, uveitis, acne rosacea, superficial punctate keratitis, herpes zoster keratitis, iritis, cyclitis, and selected infective conjunctivitides. As a nasal spray, used for the treatment and management of seasonal allergic rhinitis.

Structured Indications
Pharmacodynamics

Loteprednol etabonate (LE) is a "soft" steroid belonging to a unique class of glucocorticoids. LE possesses a metabolically labile 17 beta-chloromethyl ester function which was designed in order to be hydrolyzed to an inactive carboxylic acid moiety. This inactive metabolite is more hydrophilic and is thus readily eliminated from the body. Loteprednol etabonate has good ocular permeation properties and good skin permeation properties similar to "hard" steroids. It is used as a topical agent for the treatment of steroid responsive inflammatory conditions of the eye such as allergic conjunctivitis, uveitis and iritis.

Mechanism of action

Loteprednol etabonate (LE) is a "soft" steroid belonging to a unique class of glucocorticoids. Loteprednol etabonate is structurally similar to other glucocorticoids. However, the number 20 position ketone group is absent. It is highly lipid soluble which enhances its penetration into cells. Loteprednol etabonate is synthesized through structural modifications of prednisolone- related compounds so that it will undergo a predictable transformation to an inactive metabolite. It first binds to the type II glucocorticoid receptor. Corticosteroids inhibit the inflammatory response to a variety of inciting agents and probably delay or slow healing. They inhibit the edema, fibrin deposition, capillary dilation, leukocyte migration, capillary proliferation, fibroblast proliferation, deposition of collagen, and scar formation associated with inflammation. 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 postulated that these proteins control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2.

TargetActionsOrganism
AGlucocorticoid receptor
agonist
Human
Absorption

Very limited systemic absorption, but good absorption at the point of delivery.

Volume of distribution
Not Available
Protein binding
Not Available
Metabolism

The drugs 17 beta-chloromethyl ester function is hydrolyzed to an inactive carboxylic acid moiety.

Route of elimination
Not Available
Half life
Not Available
Clearance
Not Available
Toxicity

Adverse effects include abnormal vision / blurring, burning on instillation, chemosis, discharge, dry eyes, epiphora, foreign body sensation, itching, injection, and photophobia.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
1,10-PhenanthrolineThe risk or severity of adverse effects can be increased when Loteprednol is combined with 1,10-Phenanthroline.Experimental
AceclofenacThe risk or severity of adverse effects can be increased when Aceclofenac is combined with Loteprednol.Approved, Investigational
AcemetacinThe risk or severity of adverse effects can be increased when Acemetacin is combined with Loteprednol.Approved, Experimental, Investigational
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Loteprednol.Approved, Vet Approved
AdapaleneThe risk or severity of adverse effects can be increased when Adapalene is combined with Loteprednol.Approved
AlclofenacThe risk or severity of adverse effects can be increased when Alclofenac is combined with Loteprednol.Approved, Withdrawn
AldesleukinLoteprednol may decrease the antineoplastic activities of Aldesleukin.Approved
AlmasilateThe bioavailability of Loteprednol can be decreased when combined with Almasilate.Approved, Experimental
AlminoprofenThe risk or severity of adverse effects can be increased when Alminoprofen is combined with Loteprednol.Experimental
AloglutamolThe bioavailability of Loteprednol can be decreased when combined with Aloglutamol.Experimental
AloxiprinThe risk or severity of adverse effects can be increased when Aloxiprin is combined with Loteprednol.Experimental
AluminiumThe bioavailability of Loteprednol can be decreased when combined with Aluminium.Approved
Aluminium acetoacetateThe bioavailability of Loteprednol can be decreased when combined with Aluminium acetoacetate.Experimental
Aluminium glycinateThe bioavailability of Loteprednol can be decreased when combined with Aluminium glycinate.Experimental
Aluminum hydroxideThe bioavailability of Loteprednol can be decreased when combined with Aluminum hydroxide.Approved
AmbenoniumThe risk or severity of adverse effects can be increased when Loteprednol is combined with Ambenonium.Approved
Aminosalicylic AcidThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Loteprednol.Approved
AmiodaroneThe serum concentration of Loteprednol can be increased when it is combined with Amiodarone.Approved, Investigational
Amphotericin BLoteprednol may increase the hypokalemic activities of Amphotericin B.Approved, Investigational
AndrographolideThe risk or severity of adverse effects can be increased when Andrographolide is combined with Loteprednol.Investigational
AnisodamineThe risk or severity of adverse effects can be increased when Anisodamine is combined with Loteprednol.Investigational
AntipyrineThe risk or severity of adverse effects can be increased when Antipyrine is combined with Loteprednol.Approved
ApocyninThe risk or severity of adverse effects can be increased when Apocynin is combined with Loteprednol.Investigational
ApremilastThe risk or severity of adverse effects can be increased when Apremilast is combined with Loteprednol.Approved, Investigational
AprepitantThe serum concentration of Loteprednol can be increased when it is combined with Aprepitant.Approved, Investigational
AtazanavirThe serum concentration of Loteprednol can be increased when it is combined with Atazanavir.Approved, Investigational
Atracurium besylateAtracurium besylate may increase the adverse neuromuscular activities of Loteprednol.Approved
AzapropazoneThe risk or severity of adverse effects can be increased when Azapropazone is combined with Loteprednol.Withdrawn
AzelastineThe risk or severity of adverse effects can be increased when Azelastine is combined with Loteprednol.Approved
BalsalazideThe risk or severity of adverse effects can be increased when Balsalazide is combined with Loteprednol.Approved, Investigational
BCG vaccineThe risk or severity of adverse effects can be increased when Loteprednol is combined with BCG vaccine.Investigational
BendazacThe risk or severity of adverse effects can be increased when Bendazac is combined with Loteprednol.Experimental
BendroflumethiazideLoteprednol may increase the hypokalemic activities of Bendroflumethiazide.Approved
BenorilateThe risk or severity of adverse effects can be increased when Benorilate is combined with Loteprednol.Experimental
BenoxaprofenThe risk or severity of adverse effects can be increased when Benoxaprofen is combined with Loteprednol.Withdrawn
Benzoic AcidThe therapeutic efficacy of Benzoic Acid can be decreased when used in combination with Loteprednol.Approved
BenzydamineThe risk or severity of adverse effects can be increased when Benzydamine is combined with Loteprednol.Approved
BevoniumThe risk or severity of adverse effects can be increased when Bevonium is combined with Loteprednol.Experimental
Bismuth SubcitrateThe bioavailability of Loteprednol can be decreased when combined with Bismuth Subcitrate.Approved
Bismuth subnitrateThe bioavailability of Loteprednol can be decreased when combined with Bismuth subnitrate.Experimental
BoceprevirThe serum concentration of Loteprednol can be increased when it is combined with Boceprevir.Approved, Withdrawn
BromfenacThe risk or severity of adverse effects can be increased when Bromfenac is combined with Loteprednol.Approved
BucillamineThe risk or severity of adverse effects can be increased when Bucillamine is combined with Loteprednol.Investigational
BufexamacThe risk or severity of adverse effects can be increased when Bufexamac is combined with Loteprednol.Experimental
BumadizoneThe risk or severity of adverse effects can be increased when Bumadizone is combined with Loteprednol.Experimental
BumetanideLoteprednol may increase the hypokalemic activities of Bumetanide.Approved
CalcitriolThe therapeutic efficacy of Calcitriol can be decreased when used in combination with Loteprednol.Approved, Nutraceutical
Calcium CarbonateThe bioavailability of Loteprednol can be decreased when combined with Calcium Carbonate.Approved
Calcium silicateThe bioavailability of Loteprednol can be decreased when combined with Calcium silicate.Experimental
Capromab pendetideLoteprednol may decrease effectiveness of Capromab pendetide as a diagnostic agent.Approved
CarbamazepineThe serum concentration of Loteprednol can be decreased when it is combined with Carbamazepine.Approved, Investigational
CarprofenThe risk or severity of adverse effects can be increased when Carprofen is combined with Loteprednol.Approved, Vet Approved, Withdrawn
CastanospermineThe risk or severity of adverse effects can be increased when Castanospermine is combined with Loteprednol.Experimental
CelecoxibThe risk or severity of adverse effects can be increased when Celecoxib is combined with Loteprednol.Approved, Investigational
CeritinibLoteprednol may increase the hyperglycemic activities of Ceritinib.Approved
ChloroquineThe risk or severity of adverse effects can be increased when Chloroquine is combined with Loteprednol.Approved, Vet Approved
ChlorothiazideLoteprednol may increase the hypokalemic activities of Chlorothiazide.Approved, Vet Approved
ChlorotrianiseneThe serum concentration of Loteprednol can be increased when it is combined with Chlorotrianisene.Investigational, Withdrawn
ChlorthalidoneLoteprednol may increase the hypokalemic activities of Chlorthalidone.Approved
CholestyramineCholestyramine can cause a decrease in the absorption of Loteprednol resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Choline magnesium trisalicylateThe risk or severity of adverse effects can be increased when Choline magnesium trisalicylate is combined with Loteprednol.Approved
CinoxacinThe risk or severity of adverse effects can be increased when Loteprednol is combined with Cinoxacin.Approved, Investigational, Withdrawn
ClarithromycinThe serum concentration of Loteprednol can be increased when it is combined with Clarithromycin.Approved
ClonixinThe risk or severity of adverse effects can be increased when Clonixin is combined with Loteprednol.Approved
Clostridium tetani toxoid antigen (formaldehyde inactivated)The risk or severity of adverse effects can be increased when Loteprednol is combined with Clostridium tetani toxoid antigen (formaldehyde inactivated).Approved
CobicistatThe serum concentration of Loteprednol can be increased when it is combined with Cobicistat.Approved
ColesevelamColesevelam can cause a decrease in the absorption of Loteprednol resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
ColestipolColestipol can cause a decrease in the absorption of Loteprednol resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Conjugated estrogensThe serum concentration of Loteprednol can be increased when it is combined with Conjugated estrogens.Approved
Corticorelin ovine triflutateThe therapeutic efficacy of Corticorelin ovine triflutate can be decreased when used in combination with Loteprednol.Approved
Corynebacterium diphtheriae toxoid antigen (formaldehyde inactivated)The risk or severity of adverse effects can be increased when Loteprednol is combined with Corynebacterium diphtheriae toxoid antigen (formaldehyde inactivated).Approved
CoumaphosThe risk or severity of adverse effects can be increased when Loteprednol is combined with Coumaphos.Vet Approved
CurcuminThe risk or severity of adverse effects can be increased when Curcumin is combined with Loteprednol.Investigational
CyclopenthiazideLoteprednol may increase the hypokalemic activities of Cyclopenthiazide.Experimental
D-LimoneneThe risk or severity of adverse effects can be increased when D-Limonene is combined with Loteprednol.Investigational
DaidzeinThe serum concentration of Loteprednol can be increased when it is combined with Daidzein.Experimental
DanazolLoteprednol may increase the fluid retaining activities of Danazol.Approved
DarunavirThe serum concentration of Loteprednol can be increased when it is combined with Darunavir.Approved
DecamethoniumThe risk or severity of adverse effects can be increased when Loteprednol is combined with Decamethonium.Approved
DeferasiroxThe risk or severity of adverse effects can be increased when Loteprednol is combined with Deferasirox.Approved, Investigational
DemecariumThe risk or severity of adverse effects can be increased when Loteprednol is combined with Demecarium.Approved
dersalazineThe risk or severity of adverse effects can be increased when dersalazine is combined with Loteprednol.Investigational
DichlorvosThe risk or severity of adverse effects can be increased when Loteprednol is combined with Dichlorvos.Vet Approved
DiclofenacThe risk or severity of adverse effects can be increased when Diclofenac is combined with Loteprednol.Approved, Vet Approved
DienestrolThe serum concentration of Loteprednol can be increased when it is combined with Dienestrol.Approved, Investigational
DiethylstilbestrolThe serum concentration of Loteprednol can be increased when it is combined with Diethylstilbestrol.Approved, Investigational
DifenpiramideThe risk or severity of adverse effects can be increased when Difenpiramide is combined with Loteprednol.Experimental
DiflunisalThe risk or severity of adverse effects can be increased when Diflunisal is combined with Loteprednol.Approved
DihydrotestosteroneLoteprednol may increase the fluid retaining activities of Dihydrotestosterone.Illicit
DistigmineThe risk or severity of adverse effects can be increased when Loteprednol is combined with Distigmine.Experimental
DonepezilThe risk or severity of adverse effects can be increased when Loteprednol is combined with Donepezil.Approved
DroxicamThe risk or severity of adverse effects can be increased when Droxicam is combined with Loteprednol.Approved
DuvelisibThe risk or severity of adverse effects can be increased when Duvelisib is combined with Loteprednol.Investigational
E-6201The risk or severity of adverse effects can be increased when E-6201 is combined with Loteprednol.Investigational
EchothiophateThe risk or severity of adverse effects can be increased when Loteprednol is combined with Echothiophate.Approved
EdrophoniumThe risk or severity of adverse effects can be increased when Loteprednol is combined with Edrophonium.Approved
EnoxacinThe risk or severity of adverse effects can be increased when Loteprednol is combined with Enoxacin.Approved, Investigational
EnzalutamideThe serum concentration of Loteprednol can be decreased when it is combined with Enzalutamide.Approved
EpimestrolThe serum concentration of Loteprednol can be increased when it is combined with Epimestrol.Experimental
EpirizoleThe risk or severity of adverse effects can be increased when Epirizole is combined with Loteprednol.Approved
EquolThe serum concentration of Loteprednol can be increased when it is combined with Equol.Investigational
EstradiolThe serum concentration of Loteprednol can be increased when it is combined with Estradiol.Approved, Investigational, Vet Approved
EstriolThe serum concentration of Loteprednol can be increased when it is combined with Estriol.Approved, Investigational, Vet Approved
Estrogens, esterifiedThe serum concentration of Loteprednol can be increased when it is combined with Estrogens, esterified.Approved
EstroneThe serum concentration of Loteprednol can be increased when it is combined with Estrone.Approved
Etacrynic acidLoteprednol may increase the hypokalemic activities of Etacrynic acid.Approved
EtanerceptThe risk or severity of adverse effects can be increased when Etanercept is combined with Loteprednol.Approved, Investigational
EthenzamideThe risk or severity of adverse effects can be increased when Ethenzamide is combined with Loteprednol.Experimental
Ethinyl EstradiolThe serum concentration of Loteprednol can be increased when it is combined with Ethinyl Estradiol.Approved
EtodolacThe risk or severity of adverse effects can be increased when Etodolac is combined with Loteprednol.Approved, Investigational, Vet Approved
EtofenamateThe risk or severity of adverse effects can be increased when Etofenamate is combined with Loteprednol.Approved, Investigational
EtoricoxibThe risk or severity of adverse effects can be increased when Etoricoxib is combined with Loteprednol.Approved, Investigational
Evening primrose oilThe risk or severity of adverse effects can be increased when Evening primrose oil is combined with Loteprednol.Approved, Investigational
exisulindThe risk or severity of adverse effects can be increased when exisulind is combined with Loteprednol.Investigational
FelbinacThe risk or severity of adverse effects can be increased when Felbinac is combined with Loteprednol.Experimental
FenbufenThe risk or severity of adverse effects can be increased when Fenbufen is combined with Loteprednol.Approved
FenoprofenThe risk or severity of adverse effects can be increased when Fenoprofen is combined with Loteprednol.Approved
FenthionThe risk or severity of adverse effects can be increased when Loteprednol is combined with Fenthion.Vet Approved
FentiazacThe risk or severity of adverse effects can be increased when Fentiazac is combined with Loteprednol.Experimental
FeprazoneThe risk or severity of adverse effects can be increased when Feprazone is combined with Loteprednol.Experimental
Ferulic acidThe risk or severity of adverse effects can be increased when Ferulic acid is combined with Loteprednol.Experimental
FleroxacinThe risk or severity of adverse effects can be increased when Loteprednol is combined with Fleroxacin.Approved
FloctafenineThe risk or severity of adverse effects can be increased when Floctafenine is combined with Loteprednol.Approved, Withdrawn
FlumequineThe risk or severity of adverse effects can be increased when Loteprednol is combined with Flumequine.Withdrawn
FlunixinThe risk or severity of adverse effects can be increased when Flunixin is combined with Loteprednol.Vet Approved
FlunoxaprofenThe risk or severity of adverse effects can be increased when Flunoxaprofen is combined with Loteprednol.Experimental
FluoxymesteroneLoteprednol may increase the fluid retaining activities of Fluoxymesterone.Approved, Illicit
FlurbiprofenThe risk or severity of adverse effects can be increased when Flurbiprofen is combined with Loteprednol.Approved, Investigational
FosaprepitantThe serum concentration of Loteprednol can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe serum concentration of Loteprednol can be decreased when it is combined with Fosphenytoin.Approved
FurosemideLoteprednol may increase the hypokalemic activities of Furosemide.Approved, Vet Approved
G17DTThe risk or severity of adverse effects can be increased when Loteprednol is combined with G17DT.Investigational
GalantamineThe risk or severity of adverse effects can be increased when Loteprednol is combined with Galantamine.Approved
Gallamine TriethiodideThe risk or severity of adverse effects can be increased when Loteprednol is combined with Gallamine Triethiodide.Approved
GarenoxacinThe risk or severity of adverse effects can be increased when Loteprednol is combined with Garenoxacin.Investigational
GatifloxacinThe risk or severity of adverse effects can be increased when Loteprednol is combined with Gatifloxacin.Approved, Investigational
GemifloxacinThe risk or severity of adverse effects can be increased when Loteprednol is combined with Gemifloxacin.Approved, Investigational
GenisteinThe serum concentration of Loteprednol can be increased when it is combined with Genistein.Investigational
GI-5005The risk or severity of adverse effects can be increased when Loteprednol is combined with GI-5005.Investigational
GLPG-0492Loteprednol may increase the fluid retaining activities of GLPG-0492.Investigational
Glycerol PhenylbutyrateThe therapeutic efficacy of Glycerol Phenylbutyrate can be decreased when used in combination with Loteprednol.Approved
GrepafloxacinThe risk or severity of adverse effects can be increased when Loteprednol is combined with Grepafloxacin.Investigational, Withdrawn
GuacetisalThe risk or severity of adverse effects can be increased when Guacetisal is combined with Loteprednol.Experimental
Hemoglobin crosfumarilThe risk or severity of adverse effects can be increased when Hemoglobin crosfumaril is combined with Loteprednol.Experimental
Hepatitis A VaccineThe risk or severity of adverse effects can be increased when Loteprednol is combined with Hepatitis A Vaccine.Approved
Hepatitis B Vaccine (Recombinant)The risk or severity of adverse effects can be increased when Loteprednol is combined with Hepatitis B Vaccine (Recombinant).Approved, Withdrawn
HexestrolThe serum concentration of Loteprednol can be increased when it is combined with Hexestrol.Withdrawn
HigenamineThe risk or severity of adverse effects can be increased when Higenamine is combined with Loteprednol.Investigational
Huperzine AThe risk or severity of adverse effects can be increased when Loteprednol is combined with Huperzine A.Investigational
HyaluronidaseThe therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Loteprednol.Approved, Investigational
HydrochlorothiazideLoteprednol may increase the hypokalemic activities of Hydrochlorothiazide.Approved, Vet Approved
HydroflumethiazideLoteprednol may increase the hypokalemic activities of Hydroflumethiazide.Approved, Investigational
HydrotalciteThe bioavailability of Loteprednol can be decreased when combined with Hydrotalcite.Experimental, Investigational
IbuprofenThe risk or severity of adverse effects can be increased when Ibuprofen is combined with Loteprednol.Approved
IbuproxamThe risk or severity of adverse effects can be increased when Ibuproxam is combined with Loteprednol.Withdrawn
IcatibantThe risk or severity of adverse effects can be increased when Icatibant is combined with Loteprednol.Approved
IdelalisibThe serum concentration of Loteprednol can be increased when it is combined with Idelalisib.Approved
Imidazole salicylateThe risk or severity of adverse effects can be increased when Imidazole salicylate is combined with Loteprednol.Experimental
IndacaterolIndacaterol may increase the hypokalemic activities of Loteprednol.Approved
IndapamideLoteprednol may increase the hypokalemic activities of Indapamide.Approved
IndinavirThe serum concentration of Loteprednol can be increased when it is combined with Indinavir.Approved
IndobufenThe risk or severity of adverse effects can be increased when Indobufen is combined with Loteprednol.Investigational
IndomethacinThe risk or severity of adverse effects can be increased when Indomethacin is combined with Loteprednol.Approved, Investigational
IndoprofenThe risk or severity of adverse effects can be increased when Indoprofen is combined with Loteprednol.Withdrawn
INGN 201The risk or severity of adverse effects can be increased when Loteprednol is combined with INGN 201.Investigational
INGN 225The risk or severity of adverse effects can be increased when Loteprednol is combined with INGN 225.Investigational
IpidacrineThe risk or severity of adverse effects can be increased when Loteprednol is combined with Ipidacrine.Experimental
IsoflurophateThe risk or severity of adverse effects can be increased when Loteprednol is combined with Isoflurophate.Approved, Investigational, Withdrawn
IsoniazidThe serum concentration of Isoniazid can be decreased when it is combined with Loteprednol.Approved
IsoxicamThe risk or severity of adverse effects can be increased when Isoxicam is combined with Loteprednol.Withdrawn
ItraconazoleThe serum concentration of Loteprednol can be increased when it is combined with Itraconazole.Approved, Investigational
KebuzoneThe risk or severity of adverse effects can be increased when Kebuzone is combined with Loteprednol.Experimental
KetoconazoleThe serum concentration of Loteprednol can be increased when it is combined with Ketoconazole.Approved, Investigational
KetoprofenThe risk or severity of adverse effects can be increased when Ketoprofen is combined with Loteprednol.Approved, Vet Approved
KetorolacThe risk or severity of adverse effects can be increased when Ketorolac is combined with Loteprednol.Approved
LeflunomideThe risk or severity of adverse effects can be increased when Leflunomide is combined with Loteprednol.Approved, Investigational
LevofloxacinThe risk or severity of adverse effects can be increased when Loteprednol is combined with Levofloxacin.Approved, Investigational
LisofyllineThe risk or severity of adverse effects can be increased when Lisofylline is combined with Loteprednol.Investigational
LonazolacThe risk or severity of adverse effects can be increased when Lonazolac is combined with Loteprednol.Experimental
LopinavirThe serum concentration of Loteprednol can be increased when it is combined with Lopinavir.Approved
LornoxicamThe risk or severity of adverse effects can be increased when Lornoxicam is combined with Loteprednol.Approved, Investigational
LoxoprofenThe risk or severity of adverse effects can be increased when Loxoprofen is combined with Loteprednol.Approved, Investigational
LumacaftorThe serum concentration of Loteprednol can be decreased when it is combined with Lumacaftor.Approved
LumiracoxibThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Loteprednol.Approved, Investigational
MagaldrateThe bioavailability of Loteprednol can be decreased when combined with Magaldrate.Approved, Withdrawn
Magnesium HydroxideThe bioavailability of Loteprednol can be decreased when combined with Magnesium Hydroxide.Approved
Magnesium oxideThe bioavailability of Loteprednol can be decreased when combined with Magnesium oxide.Approved
Magnesium peroxideThe bioavailability of Loteprednol can be decreased when combined with Magnesium peroxide.Experimental
Magnesium salicylateThe risk or severity of adverse effects can be increased when Magnesium salicylate is combined with Loteprednol.Approved
Magnesium silicateThe bioavailability of Loteprednol can be decreased when combined with Magnesium silicate.Approved, Experimental
Magnesium TrisilicateThe bioavailability of Loteprednol can be decreased when combined with Magnesium Trisilicate.Approved
MalathionThe risk or severity of adverse effects can be increased when Loteprednol is combined with Malathion.Approved, Investigational
MasoprocolThe risk or severity of adverse effects can be increased when Masoprocol is combined with Loteprednol.Approved, Investigational
Meclofenamic acidThe risk or severity of adverse effects can be increased when Meclofenamic acid is combined with Loteprednol.Approved, Vet Approved
Mefenamic acidThe risk or severity of adverse effects can be increased when Mefenamic acid is combined with Loteprednol.Approved
MefloquineThe risk or severity of adverse effects can be increased when Loteprednol is combined with Mefloquine.Approved
MeloxicamThe risk or severity of adverse effects can be increased when Meloxicam is combined with Loteprednol.Approved, Vet Approved
MemantineThe risk or severity of adverse effects can be increased when Loteprednol is combined with Memantine.Approved, Investigational
MesalazineThe risk or severity of adverse effects can be increased when Mesalazine is combined with Loteprednol.Approved
MesteroloneLoteprednol may increase the fluid retaining activities of Mesterolone.Experimental
MestranolThe serum concentration of Loteprednol can be increased when it is combined with Mestranol.Approved
MetamizoleThe risk or severity of adverse effects can be increased when Metamizole is combined with Loteprednol.Investigational, Withdrawn
MethallenestrilThe serum concentration of Loteprednol can be increased when it is combined with Methallenestril.Experimental
Methanesulfonyl FluorideThe risk or severity of adverse effects can be increased when Loteprednol is combined with Methanesulfonyl Fluoride.Investigational
MethyclothiazideLoteprednol may increase the hypokalemic activities of Methyclothiazide.Approved
Methyl salicylateThe risk or severity of adverse effects can be increased when Methyl salicylate is combined with Loteprednol.Approved, Vet Approved
MethyltestosteroneLoteprednol may increase the fluid retaining activities of Methyltestosterone.Approved
MetoclopramideThe risk or severity of adverse effects can be increased when Loteprednol is combined with Metoclopramide.Approved, Investigational
MetolazoneLoteprednol may increase the hypokalemic activities of Metolazone.Approved
MifepristoneThe therapeutic efficacy of Loteprednol can be decreased when used in combination with Mifepristone.Approved, Investigational
MinaprineThe risk or severity of adverse effects can be increased when Loteprednol is combined with Minaprine.Approved
MitotaneThe serum concentration of Loteprednol can be decreased when it is combined with Mitotane.Approved
MivacuriumMivacurium may increase the adverse neuromuscular activities of Loteprednol.Approved
MizoribineThe risk or severity of adverse effects can be increased when Mizoribine is combined with Loteprednol.Investigational
MofebutazoneThe risk or severity of adverse effects can be increased when Mofebutazone is combined with Loteprednol.Experimental
MoxestrolThe serum concentration of Loteprednol can be increased when it is combined with Moxestrol.Experimental
Mycophenolate mofetilThe risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Loteprednol.Approved, Investigational
Mycophenolic acidThe risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Loteprednol.Approved
NabumetoneThe risk or severity of adverse effects can be increased when Nabumetone is combined with Loteprednol.Approved
NafamostatThe risk or severity of adverse effects can be increased when Nafamostat is combined with Loteprednol.Approved, Investigational
NaftifineThe risk or severity of adverse effects can be increased when Naftifine is combined with Loteprednol.Approved
Nalidixic AcidThe risk or severity of adverse effects can be increased when Loteprednol is combined with Nalidixic Acid.Approved, Investigational
NandroloneLoteprednol may increase the fluid retaining activities of Nandrolone.Experimental, Investigational
Nandrolone decanoateLoteprednol may increase the fluid retaining activities of Nandrolone decanoate.Approved, Illicit
NaproxenThe risk or severity of adverse effects can be increased when Naproxen is combined with Loteprednol.Approved, Vet Approved
NefazodoneThe serum concentration of Loteprednol can be increased when it is combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Loteprednol can be increased when it is combined with Nelfinavir.Approved
NemonoxacinThe risk or severity of adverse effects can be increased when Loteprednol is combined with Nemonoxacin.Investigational
NeostigmineThe risk or severity of adverse effects can be increased when Loteprednol is combined with Neostigmine.Approved, Vet Approved
NepafenacThe risk or severity of adverse effects can be increased when Nepafenac is combined with Loteprednol.Approved
NevirapineThe serum concentration of Loteprednol can be decreased when it is combined with Nevirapine.Approved
NicorandilThe risk or severity of adverse effects can be increased when Loteprednol is combined with Nicorandil.Approved, Investigational
NifenazoneThe risk or severity of adverse effects can be increased when Nifenazone is combined with Loteprednol.Experimental
Niflumic AcidThe risk or severity of adverse effects can be increased when Niflumic Acid is combined with Loteprednol.Approved
NimesulideThe risk or severity of adverse effects can be increased when Nimesulide is combined with Loteprednol.Approved, Investigational, Withdrawn
NitroaspirinThe risk or severity of adverse effects can be increased when Nitroaspirin is combined with Loteprednol.Investigational
NorfloxacinThe risk or severity of adverse effects can be increased when Loteprednol is combined with Norfloxacin.Approved
OlopatadineThe risk or severity of adverse effects can be increased when Olopatadine is combined with Loteprednol.Approved
OlsalazineThe risk or severity of adverse effects can be increased when Olsalazine is combined with Loteprednol.Approved
OrgoteinThe risk or severity of adverse effects can be increased when Orgotein is combined with Loteprednol.Vet Approved
OxandroloneLoteprednol may increase the fluid retaining activities of Oxandrolone.Approved, Investigational
OxaprozinThe risk or severity of adverse effects can be increased when Oxaprozin is combined with Loteprednol.Approved
Oxolinic acidThe risk or severity of adverse effects can be increased when Loteprednol is combined with Oxolinic acid.Experimental
OxymetholoneLoteprednol may increase the fluid retaining activities of Oxymetholone.Approved, Illicit
OxyphenbutazoneThe risk or severity of adverse effects can be increased when Oxyphenbutazone is combined with Loteprednol.Approved, Withdrawn
ParaoxonThe risk or severity of adverse effects can be increased when Loteprednol is combined with Paraoxon.Experimental
ParecoxibThe risk or severity of adverse effects can be increased when Parecoxib is combined with Loteprednol.Approved
ParthenolideThe risk or severity of adverse effects can be increased when Parthenolide is combined with Loteprednol.Investigational
PazufloxacinThe risk or severity of adverse effects can be increased when Loteprednol is combined with Pazufloxacin.Investigational
PefloxacinThe risk or severity of adverse effects can be increased when Loteprednol is combined with Pefloxacin.Approved
PentobarbitalThe serum concentration of Loteprednol can be decreased when it is combined with Pentobarbital.Approved, Vet Approved
PhenobarbitalThe serum concentration of Loteprednol can be decreased when it is combined with Phenobarbital.Approved
Phenylacetic acidThe therapeutic efficacy of Phenylacetic acid can be decreased when used in combination with Loteprednol.Approved
PhenylbutazoneThe risk or severity of adverse effects can be increased when Phenylbutazone is combined with Loteprednol.Approved, Vet Approved
Phenylbutyric acidThe therapeutic efficacy of Phenylbutyric acid can be decreased when used in combination with Loteprednol.Approved, Investigational
PhenytoinThe serum concentration of Loteprednol can be decreased when it is combined with Phenytoin.Approved, Vet Approved
PhysostigmineThe risk or severity of adverse effects can be increased when Loteprednol is combined with Physostigmine.Approved
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Loteprednol.Approved, Investigational
Pipemidic acidThe risk or severity of adverse effects can be increased when Loteprednol is combined with Pipemidic acid.Experimental
PiretanideLoteprednol may increase the hypokalemic activities of Piretanide.Experimental
PirfenidoneThe risk or severity of adverse effects can be increased when Pirfenidone is combined with Loteprednol.Approved, Investigational
Piromidic acidThe risk or severity of adverse effects can be increased when Loteprednol is combined with Piromidic acid.Experimental
PiroxicamThe risk or severity of adverse effects can be increased when Piroxicam is combined with Loteprednol.Approved, Investigational
PirprofenThe risk or severity of adverse effects can be increased when Pirprofen is combined with Loteprednol.Experimental
Polyestradiol phosphateThe serum concentration of Loteprednol can be increased when it is combined with Polyestradiol phosphate.Approved
PolythiazideLoteprednol may increase the hypokalemic activities of Polythiazide.Approved
PosaconazoleThe serum concentration of Loteprednol can be increased when it is combined with Posaconazole.Approved, Investigational, Vet Approved
PranoprofenThe risk or severity of adverse effects can be increased when Pranoprofen is combined with Loteprednol.Experimental, Investigational
PrimidoneThe serum concentration of Loteprednol can be decreased when it is combined with Primidone.Approved, Vet Approved
ProglumetacinThe risk or severity of adverse effects can be increased when Proglumetacin is combined with Loteprednol.Experimental
PromestrieneThe serum concentration of Loteprednol can be increased when it is combined with Promestriene.Investigational
PropacetamolThe risk or severity of adverse effects can be increased when Propacetamol is combined with Loteprednol.Approved, Investigational
PropyphenazoneThe risk or severity of adverse effects can be increased when Propyphenazone is combined with Loteprednol.Experimental
ProquazoneThe risk or severity of adverse effects can be increased when Proquazone is combined with Loteprednol.Experimental
PrulifloxacinThe risk or severity of adverse effects can be increased when Loteprednol is combined with Prulifloxacin.Investigational
PTC299The risk or severity of adverse effects can be increased when PTC299 is combined with Loteprednol.Investigational
PyridostigmineThe risk or severity of adverse effects can be increased when Loteprednol is combined with Pyridostigmine.Approved
QuinestrolThe serum concentration of Loteprednol can be increased when it is combined with Quinestrol.Approved
QuinethazoneLoteprednol may increase the hypokalemic activities of Quinethazone.Approved
Rabies virus inactivated antigen, AThe risk or severity of adverse effects can be increased when Loteprednol is combined with Rabies virus inactivated antigen, A.Approved
RapacuroniumRapacuronium may increase the adverse neuromuscular activities of Loteprednol.Withdrawn
ResveratrolThe risk or severity of adverse effects can be increased when Resveratrol is combined with Loteprednol.Approved, Experimental, Investigational
RifabutinThe serum concentration of Loteprednol can be decreased when it is combined with Rifabutin.Approved
RifampicinThe serum concentration of Loteprednol can be decreased when it is combined with Rifampicin.Approved
RifapentineThe serum concentration of Loteprednol can be decreased when it is combined with Rifapentine.Approved
RindopepimutThe risk or severity of adverse effects can be increased when Loteprednol is combined with Rindopepimut.Investigational
RivastigmineThe risk or severity of adverse effects can be increased when Loteprednol is combined with Rivastigmine.Approved, Investigational
RofecoxibThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Loteprednol.Investigational, Withdrawn
RosoxacinThe risk or severity of adverse effects can be increased when Loteprednol is combined with Rosoxacin.Approved, Investigational
Rotavirus VaccineThe risk or severity of adverse effects can be increased when Loteprednol is combined with Rotavirus Vaccine.Approved
Rubella virus vaccineThe risk or severity of adverse effects can be increased when Loteprednol is combined with Rubella virus vaccine.Approved
RufloxacinThe risk or severity of adverse effects can be increased when Loteprednol is combined with Rufloxacin.Experimental
SalicylamideThe risk or severity of adverse effects can be increased when Salicylamide is combined with Loteprednol.Approved
Salicylic acidThe risk or severity of adverse effects can be increased when Salicylic acid is combined with Loteprednol.Approved, Vet Approved
Salmonella typhi ty21a live antigenThe risk or severity of adverse effects can be increased when Loteprednol is combined with Salmonella typhi ty21a live antigen.Approved
SalsalateThe risk or severity of adverse effects can be increased when Salsalate is combined with Loteprednol.Approved
SaquinavirThe serum concentration of Loteprednol can be increased when it is combined with Saquinavir.Approved, Investigational
SecoisolariciresinolThe serum concentration of Loteprednol can be increased when it is combined with Secoisolariciresinol.Investigational
SemapimodThe risk or severity of adverse effects can be increased when Semapimod is combined with Loteprednol.Investigational
SeratrodastThe risk or severity of adverse effects can be increased when Seratrodast is combined with Loteprednol.Approved
SerrapeptaseThe risk or severity of adverse effects can be increased when Serrapeptase is combined with Loteprednol.Investigational
SitafloxacinThe risk or severity of adverse effects can be increased when Loteprednol is combined with Sitafloxacin.Experimental, Investigational
Sodium bicarbonateThe bioavailability of Loteprednol can be decreased when combined with Sodium bicarbonate.Approved
SparfloxacinThe risk or severity of adverse effects can be increased when Loteprednol is combined with Sparfloxacin.Approved, Investigational
SRP 299The risk or severity of adverse effects can be increased when Loteprednol is combined with SRP 299.Investigational
SRT501The risk or severity of adverse effects can be increased when SRT501 is combined with Loteprednol.Investigational
St. John's WortThe serum concentration of Loteprednol can be decreased when it is combined with St. John's Wort.Investigational, Nutraceutical
StanozololLoteprednol may increase the fluid retaining activities of Stanozolol.Approved, Vet Approved
StiripentolThe serum concentration of Loteprednol can be increased when it is combined with Stiripentol.Approved
SulfasalazineThe risk or severity of adverse effects can be increased when Sulfasalazine is combined with Loteprednol.Approved
SulindacThe risk or severity of adverse effects can be increased when Sulindac is combined with Loteprednol.Approved
SuprofenThe risk or severity of adverse effects can be increased when Suprofen is combined with Loteprednol.Approved, Withdrawn
SuxibuzoneThe risk or severity of adverse effects can be increased when Suxibuzone is combined with Loteprednol.Experimental
Synthetic Conjugated Estrogens, AThe serum concentration of Loteprednol can be increased when it is combined with Synthetic Conjugated Estrogens, A.Approved
Synthetic Conjugated Estrogens, BThe serum concentration of Loteprednol can be increased when it is combined with Synthetic Conjugated Estrogens, B.Approved
TacrineThe risk or severity of adverse effects can be increased when Loteprednol is combined with Tacrine.Investigational, Withdrawn
TarenflurbilThe risk or severity of adverse effects can be increased when Tarenflurbil is combined with Loteprednol.Investigational
TecemotideThe risk or severity of adverse effects can be increased when Loteprednol is combined with Tecemotide.Investigational
TelaprevirThe serum concentration of Telaprevir can be decreased when it is combined with Loteprednol.Approved, Withdrawn
TelithromycinThe serum concentration of Loteprednol can be increased when it is combined with Telithromycin.Approved
TemafloxacinThe risk or severity of adverse effects can be increased when Loteprednol is combined with Temafloxacin.Withdrawn
TenidapThe risk or severity of adverse effects can be increased when Tenidap is combined with Loteprednol.Experimental
TenoxicamThe risk or severity of adverse effects can be increased when Tenoxicam is combined with Loteprednol.Approved
TepoxalinThe risk or severity of adverse effects can be increased when Tepoxalin is combined with Loteprednol.Vet Approved
TeriflunomideThe risk or severity of adverse effects can be increased when Teriflunomide is combined with Loteprednol.Approved
TestosteroneLoteprednol may increase the fluid retaining activities of Testosterone.Approved, Investigational
Testosterone PropionateLoteprednol may increase the fluid retaining activities of Testosterone Propionate.Approved, Vet Approved
TG4010The risk or severity of adverse effects can be increased when Loteprednol is combined with TG4010.Investigational
Tiaprofenic acidThe risk or severity of adverse effects can be increased when Tiaprofenic acid is combined with Loteprednol.Approved
TiboloneThe serum concentration of Loteprednol can be increased when it is combined with Tibolone.Approved, Investigational
TinoridineThe risk or severity of adverse effects can be increased when Tinoridine is combined with Loteprednol.Investigational
Tolfenamic AcidThe risk or severity of adverse effects can be increased when Tolfenamic Acid is combined with Loteprednol.Approved
TolmetinThe risk or severity of adverse effects can be increased when Tolmetin is combined with Loteprednol.Approved
TorasemideLoteprednol may increase the hypokalemic activities of Torasemide.Approved
TranilastThe risk or severity of adverse effects can be increased when Tranilast is combined with Loteprednol.Approved, Investigational
TribenosideThe risk or severity of adverse effects can be increased when Tribenoside is combined with Loteprednol.Experimental
TrichlorfonThe risk or severity of adverse effects can be increased when Loteprednol is combined with Trichlorfon.Vet Approved
TrichlormethiazideLoteprednol may increase the hypokalemic activities of Trichlormethiazide.Approved, Vet Approved
TriptolideThe risk or severity of adverse effects can be increased when Triptolide is combined with Loteprednol.Investigational
Trolamine salicylateThe risk or severity of adverse effects can be increased when Trolamine salicylate is combined with Loteprednol.Approved
TromethamineThe bioavailability of Loteprednol can be decreased when combined with Tromethamine.Approved
TrovafloxacinThe risk or severity of adverse effects can be increased when Loteprednol is combined with Trovafloxacin.Approved, Investigational, Withdrawn
TubocurarineThe risk or severity of adverse effects can be increased when Loteprednol is combined with Tubocurarine.Approved
ValdecoxibThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Loteprednol.Investigational, Withdrawn
Varicella Zoster Vaccine (Live/Attenuated)The risk or severity of adverse effects can be increased when Loteprednol is combined with Zoster vaccine.Approved
VoriconazoleThe serum concentration of Loteprednol can be increased when it is combined with Voriconazole.Approved, Investigational
WarfarinLoteprednol may increase the anticoagulant activities of Warfarin.Approved
Yellow fever vaccineThe risk or severity of adverse effects can be increased when Loteprednol is combined with Yellow fever vaccine.Approved
ZaltoprofenThe risk or severity of adverse effects can be increased when Zaltoprofen is combined with Loteprednol.Approved, Investigational
ZeranolThe serum concentration of Loteprednol can be increased when it is combined with Zeranol.Vet Approved
ZileutonThe risk or severity of adverse effects can be increased when Zileuton is combined with Loteprednol.Approved, Investigational, Withdrawn
ZomepiracThe risk or severity of adverse effects can be increased when Zomepirac is combined with Loteprednol.Withdrawn
Food Interactions
Not Available

References

General References
  1. Pavesio CE, Decory HH: Treatment of ocular inflammatory conditions with loteprednol etabonate. Br J Ophthalmol. 2008 Apr;92(4):455-9. doi: 10.1136/bjo.2007.132621. Epub 2008 Feb 1. [PubMed:18245274]
External Links
Human Metabolome Database
HMDB15011
KEGG Drug
D01689
PubChem Compound
9865442
PubChem Substance
46504713
ChemSpider
8041134
ChEBI
50848
Therapeutic Targets Database
DAP001045
PharmGKB
PA164764569
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Loteprednol
ATC Codes
S01BA14 — Loteprednol
AHFS Codes
  • 52:08.08 — Corticosteroids
FDA label
Download (1.1 MB)
MSDS
Download (57.6 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailablePharmacokinetics1
1CompletedSupportive CareOcular Pain1
1CompletedTreatmentHealthy Volunteers1
2CompletedPreventionConjunctivitis, Seasonal Allergic1
2CompletedTreatmentDry Eye Syndromes / Keratoconjunctivitis Sicca1
2CompletedTreatmentEye Dryness1
2CompletedTreatmentKeratoconjunctivitis Sicca1
2CompletedTreatmentBacterial blepharitis1
3Active Not RecruitingTreatmentCataracts1
3CompletedTreatmentCataracts / Inflammatory Reaction / Pain2
3CompletedTreatmentConjunctivitis, Seasonal Allergic1
3CompletedTreatmentBacterial blepharitis / Conjunctivitis / Corneal Inflammation1
3CompletedTreatmentDry Eye Syndromes / Keratoconjunctivitis Sicca1
3CompletedTreatmentInflammatory Reaction / Pain2
3CompletedTreatmentOcular Infections, Irritations and Inflammations1
3CompletedTreatmentPost Surgical Ocular Inflammation and Pain1
3CompletedTreatmentOcular inflammatory conditions2
3RecruitingTreatmentDry Eye Syndromes / Keratoconjunctivitis Sicca1
4Active Not RecruitingTreatmentConjunctivitis, Giant Papillary / Conjunctivitis, Seasonal Allergic / Inflammatory Reaction1
4Active Not RecruitingTreatmentMeibomian Gland Dysfunction (MGD) / Posterior Blepharitis1
4CompletedPreventionCorneal Edema / Fuchs' Dystrophy1
4CompletedTreatmentBlepharokeratoconjunctivitis1
4CompletedTreatmentCataract Extraction1
4CompletedTreatmentChalazion / Hordeolum1
4CompletedTreatmentConjunctivitis1
4CompletedTreatmentConjunctivitis, Seasonal Allergic2
4CompletedTreatmentDry Eye Syndrome (DES)1
4CompletedTreatmentDry Eye Syndrome (DES) / Keratoconjunctivitis Sicca1
4CompletedTreatmentEpithelial Defect After Phototherapeutic Keratectomy1
4CompletedTreatmentInflammatory Reaction1
4CompletedTreatmentOcular Hypertension / Open-angle Glaucoma (OAG)1
4Not Yet RecruitingTreatmentMust be PRK Candidate1
4Unknown StatusPreventionCataract operation / Pseudophakia1
4Unknown StatusTreatmentContact Lenses Dryness1
4WithdrawnTreatmentDry Eye Syndrome (DES)1
Not AvailableCompletedNot AvailableOcular Hypertension1
Not AvailableCompletedPreventionEye Dryness1
Not AvailableCompletedTreatmentDiabetic Macular Edema (DME) / Retinal Vein Occlusions(RVO)1
Not AvailableUnknown StatusNot AvailableInflammatory Reaction / Pseudophakia1
Not AvailableUnknown StatusTreatmentDry Eye Syndrome (DES)1
Not AvailableUnknown StatusTreatmentEye Dryness1
Not AvailableUnknown StatusTreatmentPost-operative Healing Following Blepharoplasty and Ptosis Repair1

Pharmacoeconomics

Manufacturers
  • Bausch and lomb inc
  • Pharmos corp
Packagers
Dosage forms
FormRouteStrength
SuspensionOphthalmic0.2 %
Suspension / dropsOphthalmic2 mg/mL
GelOphthalmic5 mg/g
OintmentOphthalmic5 mg/g
SuspensionOphthalmic0.5 %
Suspension / dropsOphthalmic5 mg/mL
GelOphthalmic0.5 %
OintmentOphthalmic0.5 %
Suspension / dropsOphthalmic
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5540930No1993-10-252013-10-25Us
US4996335No1995-03-092012-03-09Us
CA2174550No2002-10-012014-10-21Canada
US5800807No1997-01-292017-01-29Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)220-224 °CNot Available
water solubility5 mg/mLNot Available
logP3.4Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0336 mg/mLALOGPS
logP2.2ALOGPS
logP2.52ChemAxon
logS-4.1ALOGPS
pKa (Strongest Acidic)12.01ChemAxon
pKa (Strongest Basic)-2.9ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area83.83 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity102.65 m3·mol-1ChemAxon
Polarizability41.29 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9884
Blood Brain Barrier+0.9294
Caco-2 permeable+0.5426
P-glycoprotein substrateSubstrate0.7489
P-glycoprotein inhibitor INon-inhibitor0.6379
P-glycoprotein inhibitor IINon-inhibitor0.6419
Renal organic cation transporterNon-inhibitor0.7633
CYP450 2C9 substrateNon-substrate0.862
CYP450 2D6 substrateNon-substrate0.914
CYP450 3A4 substrateSubstrate0.794
CYP450 1A2 substrateNon-inhibitor0.8987
CYP450 2C9 inhibitorNon-inhibitor0.8866
CYP450 2D6 inhibitorNon-inhibitor0.872
CYP450 2C19 inhibitorNon-inhibitor0.9233
CYP450 3A4 inhibitorNon-inhibitor0.5687
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8468
Ames testNon AMES toxic0.8574
CarcinogenicityNon-carcinogens0.9436
BiodegradationNot ready biodegradable0.9614
Rat acute toxicity2.2305 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9647
hERG inhibition (predictor II)Non-inhibitor0.5773
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as androgens and derivatives. These are 3-hydroxylated C19 steroid hormones. They are known to favor the development of masculine characteristics. They also show profound effects on scalp and body hair in humans.
Kingdom
Organic compounds
Super Class
Lipids and lipid-like molecules
Class
Steroids and steroid derivatives
Sub Class
Androstane steroids
Direct Parent
Androgens and derivatives
Alternative Parents
3-oxo delta-1,4-steroids / 17-hydroxysteroids / 11-beta-hydroxysteroids / Delta-1,4-steroids / Tertiary alcohols / Secondary alcohols / Cyclic ketones / Cyclic alcohols and derivatives / Carboxylic acid esters / Monocarboxylic acids and derivatives
show 4 more
Substituents
Androgen-skeleton / 3-oxo-delta-1,4-steroid / 3-oxosteroid / 17-hydroxysteroid / 11-hydroxysteroid / 11-beta-hydroxysteroid / Oxosteroid / Hydroxysteroid / Delta-1,4-steroid / Tertiary alcohol
show 18 more
Molecular Framework
Aliphatic homopolycyclic compounds
External Descriptors
organochlorine compound, 11beta-hydroxy steroid, 17alpha-hydroxy steroid, androstanoid, 3-oxo-Delta(1),Delta(4)-steroid, steroid acid ester (CHEBI:50848)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Agonist
General Function
Zinc ion binding
Specific Function
Receptor for glucocorticoids (GC). Has a dual mode of action: as a transcription factor that binds to glucocorticoid response elements (GRE), both for nuclear and mitochondrial DNA, and as a modula...
Gene Name
NR3C1
Uniprot ID
P04150
Uniprot Name
Glucocorticoid receptor
Molecular Weight
85658.57 Da
References
  1. Druzgala P, Hochhaus G, Bodor N: Soft drugs--10. Blanching activity and receptor binding affinity of a new type of glucocorticoid: loteprednol etabonate. J Steroid Biochem Mol Biol. 1991 Feb;38(2):149-54. [PubMed:2004037]
  2. Bodor N, Buchwald P: Corticosteroid design for the treatment of asthma: structural insights and the therapeutic potential of soft corticosteroids. Curr Pharm Des. 2006;12(25):3241-60. [PubMed:17020532]
  3. Szelenyi I, Hochhaus G, Heer S, Kusters S, Marx D, Poppe H, Engel J: Loteprednol etabonate: a soft steroid for the treatment of allergic diseases of the airways. Drugs Today (Barc). 2000 May;36(5):313-20. [PubMed:12861354]
  4. Samudre SS, Lattanzio FA Jr, Williams PB, Sheppard JD Jr: Comparison of topical steroids for acute anterior uveitis. J Ocul Pharmacol Ther. 2004 Dec;20(6):533-47. [PubMed:15684812]
  5. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]

Drug created on June 13, 2005 07:24 / Updated on December 10, 2017 17:18