Loxtra is prescribed for corticosteroid responsive inflammatory conditions of the conjunctiva,
cornea and anterior segment of the eye where bacterial infection or a risk of bacterial infection
exists.

Loxtra is to be used only as eye drops. Instill 1-2 drops in to the conjunctival sac of the eye (s)
three to four times daily or as directed by the physician.

Instructions for using eye drops
 Shake the bottle well before use.
 Unscrew the cap from the bottle, check the dropper is clean.
 Pull your lower eyelid gently down, and then carefully instill one drop inside the lower
eyelid, in the corner closest to the nose.
 Release the lower eyelid, and blink a few times to make sure the eye is covered by the
liquid.
 Repeat the procedure for your other eye, if it also needs treatment.

When you have finished, replace the protective cap tightly to prevent spilling or
spoilage.

Prednisolone Acetate Acute untreated purulent ocular infections. Acute superficial herpes simplex (dendritic keratitis); vaccinia, varicella and most other viral diseases of the cornea and conjunctiva. Fungal diseases of the eye. Mycobacterial infection such as tuberculosis of the eye Ofloxacin Contra-indicated in individuals who have shown hypersensitivity to ofloxacin, any of its excipients or any other quinolones. Tetrahydrozoline Hydrochloride Known hypersensitivity to tetrahydrozoline or any ingredient in the formulation

Prednisolone Acetate
Acute purulent infections of the eye may be masked or enhanced by the use of topical steroids.
Prolonged use may also suppress the host immune response and thus increase the hazard of
secondary ocular infections.
Fungal infections of the cornea have been reported coincidentally with long-term steroid
application and fungal invasion may be suspected in any persistent corneal ulceration where a
steroid has been used, or is in use.
Various ocular diseases and long-term use of topical corticosteroids have been known to cause
corneal or scleral thinning. Use of topical corticosteroids in the presence of thin corneal or
scleral tissue may lead to perforation.
The preservative benzalkonium chloride, may be absorbed by and cause discoloration of soft
contact lenses. Patients wearing soft contact lenses should be instructed to remove contact
lenses prior to administration of the solution and wait at least 15 minutes after instilling Loxtra
before reinserting soft contact lenses.
Use of intraocular steroids may prolong the course and may exacerbate the severity of many
viral infections on the eye (including herpes simplex). Patients with a history of herpes simplex
keratitis should be treated with caution. Use of steroid medication in the presence of stromal

herpes simplex requires caution and should be followed by frequent, mandatory, slit-lamp
microscopy.
Prolonged use of topical corticosteroids may cause an increase in intraocular pressure in certain
individuals. This may result in glaucoma with damage to the optic nerve with resultant defects
in visual acuity and visual fields. Steroids should be used with caution in the presence of
glaucoma. It is advisable that intraocular pressure be checked frequently during treatment with
Loxtra. Eye drops containing corticosteroids should not be used for more than 10 days except
under strict ophthalmic supervision with regular checks for intraocular pressure.
Posterior subcapsular cataract formation has been reported after heavy or protracted use of
topical ophthalmic corticosteroids.
The use of steroids after cataract surgery may delay healing and increase the incidence of bleb
formation.
Systemic adverse events may occur with extensive use of topical steroids; punctal occlusion
may be recommended.
The possibility of adrenal suppression should be considered with prolonged, frequent, use of
high dose topical steroids, particularly in infants and children.
To prevent eye injury or contamination, care should be taken to avoid touching the bottle tip to
the eye or to any other surface.
Visual disturbance
Visual disturbance may be reported with systemic and topical corticosteroid use. If a patient
presents with symptoms such as blurred vision or other visual disturbances, the patient should
be considered for referral to an ophthalmologist for evaluation of possible causes which may
include cataract, glaucoma or rare diseases such as central serous chorioretinopathy (CSCR)
which have been reported after use of systemic and topical corticosteroids.
Ofloxacin
Safety and effectiveness in infants below the age of one year have not been established.
Serious and occasionally fatal hypersensitivity (anaphylactic/anaphylactoid) reactions, some
following the first dose, have been reported in patients receiving systemic quinolones, including
ofloxacin. Some reactions were accompanied by cardiovascular collapse, loss of consciousness,
angioedema (including laryngeal, pharyngeal or facial oedema), airway obstruction, dyspnoea,
urticaria, and itching.
If an allergic reaction to Ofloxacin occurs, discontinue the drug. Use Ofloxacin with caution in
patients who have exhibited sensitivities to other quinolones antibacterial agents.
When using Ofloxacin the risk of rhinopharyngeal passage which can contribute to the
occurrence and the diffusion of bacterial resistance should be considered. As with other antiinfectives,
prolonged use may result in overgrowth of non-susceptible organisms. If worsening infection occurs, or if clinical improvement is not noted within a reasonable period,
discontinue use and institute alternative therapy.
Cardiac disorders
Caution should be taken when using fluoroquinolones, including Ofloxacin in patients with
known risk factors for prolongation of the QT interval such as, for example:
- Congenital long QT syndrome
- Concomitant use of drugs that are known to prolong the QT interval (e.g. Class IA and III
anti-arrhythmics, tricyclic antidepressants, macrolides, antipsychotics)
- Uncorrected electrolyte imbalance (e.g. hypokalaemia, hypomagnesaemia)
- Cardiac disease (e.g. heart failure, myocardial infarction, bradycardia)
Elderly patients and women may be more sensitive to QTc-prolonging medications. Therefore,
caution should be taken when using fluoroquinolones, including Ofloxacin, in these
populations.
Use Ofloxacin with caution in patients who have exhibited sensitivities to other quinolone
antibacterial agents.
Data are very limited to establish efficacy and safety of Ofloxacin eye drops 0.3% in the
treatment of conjunctivitis in neonates.
The use of Ofloxacin eye drops in neonates with ophthalmia neonatorum caused by Neisseria
gonorrhoeae or Chlamydia trachomatis is not recommended as it has not been evaluated in such
patients.
Use in elderly: No comparative data are available with topical dosing in elderly versus other
age groups.
Clinical and non-clinical publications have reported the occurrence of corneal perforation in
patients with pre-existing corneal epithelial defect or corneal ulcer, when treated with topical
fluoroquinolone antibiotics. However, significant confounding factors were involved in many
of these reports, including advanced age, presence of large ulcers, concomitant ocular
conditions (e.g. severe dry eye), systemic inflammatory diseases (e.g. rheumatoid arthritis), and
concomitant use of ocular steroids or non-steroidal anti-inflammatory drugs. Nevertheless, it is
necessary to advise caution regarding the risk of corneal perforation when using product to treat
patients with corneal epithelial defects or corneal ulcers.
Corneal precipitates have been reported during treatment with topical ophthalmic Ofloxacin.
However, a causal relationship has not been established.
Long-term, high-dose use of other fluoroquinolones in experimental animals has caused
lenticular opacities. However, this effect has not been reported in human patients, nor has it
been noted following topical ophthalmic treatment with Ofloxacin for up to six months in
animal studies including studies in monkeys. Ofloxacin contains the preservative benzalkonium chloride which may cause ocular irritation
and discolour soft contact lenses.
Sun or UV-exposition should be avoided during use of Ofloxacin due to the potential for
photosensitivity.
Use of contact lenses is not recommended in patients receiving treatment for an eye infection.
Tetrahydrozoline Hydrochloride
Glaucoma
Patients with narrow-angle glaucoma or other serious eye disease should consult a clinician
before using ophthalmic solution.102 a c
General Precautions
Overuse: Possible irritation of conjunctiva and adverse systemic effects (particularly in
children) with excessive dosage and/or prolonged or too frequent use. Possible ocular
hyperemia (redness); avoid prolonged use.101 102 a c (See Advice to Patients.)
Overdose may produce CNS depression with drowsiness, decreased body temperature,
bradycardia, shock-like hypotension, apnea, and coma.
Accidental ingestion of imidazoline derivatives (i.e., tetrahydrozoline, naphazoline,
oxymetazoline) in children has resulted in serious adverse events requiring hospitalization (e.g.,
coma, bradycardia, decreased respiration, sedation, somnolence).
High concentrations of ophthalmic solution may liberate pigment granules; more common in
the elderly.
Sympathomimetic Effects
Possible headache, hypertension, weakness, sweating, cardiac irregularities (e.g., palpitations),
tremors, drowsiness, lightheadedness, and insomnia. Use with caution in patients with thyroid
disease (e.g., hyperthyroidism), heart disease (e.g., coronary artery disease), hypertension, or
diabetes mellitus.

Prednisolone Acetate
None known.
Co-treatment with CYP3A inhibitors, including cobicistat-containing products, is expected to
increase the risk of systemic side-effects.
Ofloxacin
No interaction studies have been performed.
It has been shown that the systemic administration of some quinolones inhibits the metabolic
clearance of caffeine and theophylline. Drug interaction studies conducted with systemic
ofloxacin have demonstrated that metabolic clearance of caffeine and theophylline are not
significantly affected by ofloxacin.
Although there have been reports of an increased prevalence of CNS toxicity with systemic
dosing of fluoroquinolones when used concomitantly with systemic nonsteroidal antiinflammatory
drugs (NSAIDs), this has not been reported with the concomitant systemic use of
NSAIDs and ofloxacin.
Ofloxacin, like other fluoroquinolones, should be used with caution in patients receiving drugs
known to prolong the QT interval (e.g. Class IA and III anti-arrhythmics, tricyclic
antidepressants, macrolides, antipsychotics).
Tetrahydrozoline Hydrochloride
None known.

Prednisolone Acetate
Pregnancy
There is inadequate evidence of safety in human pregnancy. Administration of corticosteroids
to pregnant animals can cause abnormalities of fetal development including cleft palate and
intra-uterine growth retardation. There may therefore be a very small risk of such defects in the
human fetus. Therefore this product should be used with caution during pregnancy only if the
potential benefit outweighs the potential risk to the fetus.
Breast-feeding It is not known whether topical administration of Prednisolone acetate could result in sufficient
systemic absorption to produce detectable quantities in breast milk. Therefore, use is not
recommended in women breast- feeding infants.
Ofloxacin
Use in pregnancy: There have been no adequate and well-controlled studies performed in
pregnant women. Since systemic quinolones have been shown to cause arthropathy in immature
animals, it is recommended that Ofloxacin not be used in pregnant women.
Use during lactation: Because ofloxacin and other quinolones taken systemically are excreted
in breast milk, and there is potential for harm to nursing infants, a decision should be made
whether to temporarily discontinue nursing or not to administer the drug, taking into account
the importance of the drug to the mother.
Tetrahydrozoline Hydrochloride
Pregnancy: Category C.
Lactation: Not known whether tetrahydrozoline is distributed into milk. Caution if used in
nursing women.
Pediatric Use: Safety and efficacy of ophthalmic solution not established in children <6 years
of age. Accidental ingestion of OTC ophthalmic solutions or nasal sprays containing
imidazoline derivatives (i.e., tetrahydrozoline, naphazoline, oxymetazoline) in children has
resulted in serious adverse events requiring hospitalization, including nausea, vomiting,
lethargy, tachycardia, decreased respiration, bradycardia, hypotension, hypertension, sedation,
somnolence, mydriasis, stupor, hypothermia, drooling, and coma. Respiratory depression, CNS
depression, and/or lethargy reportedly occurred in infants following accidental ingestion of
small amounts (≤6 mL) of 0.05% tetrahydrozoline ophthalmic solution. Keep out of reach of
children.

Prednisolone acetate may cause short-lasting blurring of vision upon instillation. If affected,
the patient should not use machinery/electric tools or drive until vision has returned to normal.
Ofloxacin
No studies on the effects on the ability to drive and use machines have been performed Transient blurring of vision may occur on instillation of eye drops. Do not drive or operate
hazardous machinery unless vision is clear.
Tetrahydrozoline Hydrochloride
None known.

Prednisolone Acetate
The following undesirable effects have been reported following use of Prednisolone Acetate
Frequency categories: very common (≥1/10); common (≥1/100 to <1/10); uncommon (≥1/1,000
to <1/100); rare (≥1/10,000 to <1/1,000); very rare (<1/10,000), not known (cannot be estimated
from available data).
Immune system disorders
Not known: Hypersensitivity, Urticaria
Nervous system disorders
Not known: Headache
Eye disorders
Not known: Intraocular pressure increased
Cataract (including subcapsular)
Eye penetration (scleral or corneal perforation)
Foreign body sensation
Ocular infection (including bacterial*, fungal*, and viral* infections)
Ocular stinging
Eye irritation
Ocular hyperemia
Vision blurred/Visual impairment
Mydriasis
Gastrointestinal disorders
Not known: Dysgeusia
Skin and subcutaneous tissue disorders
Not known: Pruritus, Rash
Systemic: extensive topical use of corticosteroids may lead to systemic side effects*. Ofloxacin
General
Serious reactions after use of systemic ofloxacin are rare and most symptoms are reversible.
Since a small amount of ofloxacin is systemically absorbed after topical administration, sideeffects
reported with systemic use could possibly occur.
Frequency categories: Very common (≥1/10); Common (≥1/100 to <1/10); Uncommon
(≥1/1,000 to <1/100); Rare (≥1/10,000 to <1/1,000); Very rare (<1/10,000) and not known
(cannot be estimated from the available data):
Immune System Disorders
Not Known: Hypersensitivity reaction including signs or symptoms of Eye allergy (such as Eye
pruritus and Eyelid pruritus) and anaphylactic reactions (such as angioedema, dyspnea,
anaphylactic shock, oropharyngeal swelling, facial edema and tongue swollen)
Nervous System Disorders
Not known: Dizziness
Eye Disorders
Common: Eye irritation; Ocular discomfort
Not known: Keratitis; Conjunctivitis; Vision blurred; Photophobia; Eye edema; Foreign body
sensation in eyes; Lacrimation increased; Dry eye; Eye pain; Ocular hyperaemia; Periorbital
edema (including eyelid edema)
Cardiac disorders
Not known: ventricular arrhythmia and torsades de pointes (reported predominantly in patients
with risk factors for QT prolongation); ECG QT prolonged. Gastrointestinal Disorders
Not known: Nausea
Skin and Subcutaneous Tissue Disorders
Not Known: Stevens-Johnson syndrome; Toxic epidermal necrolysis
Tetrahydrozoline Hydrochloride
Ophthalmic: Blurred vision, irritation, mydriasis

Prednisolone Acetate
There is no clinical experience of overdosage. Acute overdosage is unlikely to occur via the
ophthalmic route
Ofloxacin
In the event of overdose, symptomatic treatment should be implemented. ECG monitoring
should be undertaken, because of the possibility of QT interval prolongation
Tetrahydrozoline Hydrochloride
None known. To report any side effect(s):
• Saudi Arabia:
The National Pharmacovigilance and Drug Safety Centre (NPC)
Fax: +966-11-205-7662
Call NPC at +966-11-2038222,
Exts: 2317-2356-2353-2354-2334-2340.
Toll free phone: 8002490000
E-mail: npc.drug@sfda.gov.sa
Website: www.sfda.gov.sa/npc
• Other GCC States:
− Please contact the relevant competent authority.

5.1 Pharmacodynamic properties
Prednisolone Acetate
Pharmacotherapeutic group: corticosteroids, ATC code: S01BA04.
Prednisolone acetate is a synthetic adrenocorticoid with the general properties of prednisolone.
Adrenocorticoids diffuse across cell membranes to complex with cytoplasmic receptors and
subsequently stimulate synthesis of enzymes with anti-inflammatory effects. Glucocorticoids
inhibit the edema, fibrin deposition, capillary dilation and phagocytic migration of the acute
inflammatory response as well as capillary proliferation, deposition of collagen and scar
formation. Prednisolone acetate has, on a weight to weight basis, a potency three to five times
that of hydrocortisone Ofloxacin
Pharmacotherapeutic group: Ophthalmologicals, anti-infectives, fluoroquinolones
ATC code: S01AE01.
Ofloxacin is a synthetic fluorinated 4-quinolone antibacterial agent with activity against a broad
spectrum of Gram negative and to a lesser degree Gram positive organisms.
Ofloxacin has been shown to be active against most strains of the following organisms both in
vitro and clinically in ophthalmic infections. Clinical trial evidence of the efficacy of Ofloxacin
against S. pneumoniae was based on a limited number of isolates.
Gram-negative bacteria: Acinetobacter calcoaceticus var. anitratum, and A. calcoaceticus var.
iwoffi; Enterobacter Sp. including E. cloacae; Haemophilis Sp, including H. influenza and H.
aegyptius; Klebsiella Sp., including K. Pneumoniae; Moraxella Sp., Morganella morganii;
Proteus Sp., including P. Mirabilis; Pseudomonas Sp.; including P. Aeruginosa, P. cepacia, and
P. fluoroscens; and Serratia Sp., including S. marcescens.
Gram-positive bacteria: Bacillus Sp.; Corynebacterium Sp.; Micrococcus Sp.; Staphylococcus
Sp., including S. aureus and S. epidermidis; Streptococcus Sp., including S. Pneumoniae (see
above), S. viridans and Beta-haemolytic.
The primary mechanisms of action is through inhibition of bacterial DNA gyrase, the enzyme
responsible for maintaining the structure of DNA.
Ofloxacin is not subject to degradation by beta-lactamase enzymes nor is it modified by
enzymes such as aminoglycoside adenylases or phosphorylases, or chloramphenicol
acetyltransferase.
Tetrahydrozoline Hydrochloride
Structurally and pharmacologically related to naphazoline, oxymetazoline, and xylometazoline.
Directly stimulates α-adrenergic receptors; exerts little or no effect on β-adrenergic receptors.
Conjunctival application constricts small arterioles and temporarily relieves conjunctival
congestion.
 

5.2 Pharmacokinetic properties
Prednisolone Acetate
Prednisolone acetate has been shown to penetrate rapidly the cornea after topical application of
a suspension preparation. Aqueous humour Tmax occurs between 30 and 45 minutes after
installation. The half-life of prednisolone acetate in human aqueous humour is approximately
30 minutes.
Ofloxacin
After ophthalmic instillation, ofloxacin is well maintained in the tear-film. In a healthy volunteer study, mean tear film concentrations of ofloxacin measured four hours
after topical dosing (9.2 μg/g) were higher than the 2μg/ml minimum concentration of ofloxacin
necessary to inhibit 90% of most ocular bacterial strains (MIC90) in-vitro.
Maximum serum ofloxacin concentrations after ten days of topical dosing were about 1000
times lower than those reported after standard oral doses of ofloxacin, and no systemic sideeffects
attributable to topical ofloxacin were observed.
Tetrahydrozoline Hydrochloride
Bioavailability
Absorption may occasionally be sufficient to produce systemic effects.
Onset
Following ocular administration, local vasoconstriction usually occurs within minutes.
Duration
Local vasoconstriction may persist for 4–8 hours

Prednisolone Acetate
Non-clinical data reveal no special hazard for humans based on conventional studies on the
acute toxic potential of Prednisolone acetate.
Ofloxacin
There are no toxicological safety issues with this product in man as the level of systemic
absorption from topical ocular administration of ofloxacin is minimal.
Animal studies in the dog have found cases of arthropathy in weight bearing joints of juvenile
animals after high oral doses of certain quinolones. However, these findings have not been seen
in clinical studies and their relevance to man is unknown.
Tetrahydrozoli

1. Benzalkonium Chloride
2. Sodium Chloride
3. Hydroxypropylmethyl cellulose
4. Water for Injection
5. Hydrochloric acid 1N and/or Sodium Hydroxide 1N (to adjust pH)

Not applicable.

2 years. Shelf-life after first opening Discard after 30 days of opening

Do not store above 30⁰C.

LDPE (Low Density Polyethylene) bottle with screw caps contains 5ml of Loxtra Ophthalmic
Suspension.

 Keep out of reach of children.
 LoxtraTM eye drops are sterile when first opened, it is important to keep the drops as
clean as possible during use.
 Discard after 30 days of opening.