Drug Study on Erythromycin Eye Ointment

Generic Name: Erythromycin (Ophthalmic, Topical) (er-ith-roe-mye-sin)

Brand Name: Ilotycin
Therapeutic Class: Antibiotics
Pharmacologic Class: Macrolides

AVAILABLE FORMS
Ointment: 2%
Ophthalmic Ointment: 0.5%
Topical Gel: 2%
Topical Pad: 2%
Topical Solution: 2%

Ilotycin is a prescription medicine used to treat the symptoms of Conjunctivitis. Ilotycin

may be used alone or with other medications. Ilotycin belongs to a class of drugs called
Macrolides, Ophthalmic.

Ilotycin may cause serious side effects including:

● new or worsening eye symptoms (pain, swelling, thick discharge or pus),
● rash,
● itching,
● swelling of the face, tongue or throat,
● severe dizziness, and
● trouble breathing
Get medical help right away, if you have any of the symptoms listed above.

The most common side effects of Ilotycin include:

● minor eye irritations, ● redness,
● stinging, ● temporary blurred vision, and
● burning, ● hypersensitivity reactions
Tell the doctor if you have any side effect that bothers you or that does not go away.
DESCRIPTION
ILOTYCIN™ Erythromycin Ophthalmic Ointment belongs to the macrolide group of
antibiotics. It is basic and readily forms a salt when combined with an acid. The base, as crystals
or powder, is slightly soluble in water, moderately soluble in ether, and readily soluble in alcohol
or chloroform. Erythromycin ((3R*, 4S*, 5S*, 6R*, 7R*, 9R*, 11R*, 12R*, 13S*, 14R*) -4-
[(2,6-dideoxy-3-C-methyl-3-0-methyl-α-L-ribo-hexopyranosyl)oxy]-14-ethyl-7, 12,13-
trihydroxy-3, 5, 7, 9, 11, 13-hexamethyl-6-[[3, 4, 6-trideoxy-3-(dimethylamino)-β-D-xylo-
hexopyranosyl]oxy]oxacyclotetradecane-2, 10-dione) is an antibiotic produced from a strain of
Streptomyces erythraeus. It has the following structural formula:

Molecular Formula: C37H67NO13

Molecular Weight: 733.94
Each gram contains Erythromycin USP 5 mg in a sterile ophthalmic base of mineral oil and
white petrolatum.

INDICATIONS & DOSAGES

➢ Acute and chronic conjunctivitis, other eye infections (ophthalmic ointment)
Adults and children: Apply a ribbon of oint- ment about 1 cm long directly to infected eye up to
six times daily, depending on severity of infection.
➢ To prevent ophthalmia neonatorum caused by Neisseria gonorrhoeae or Chlamydia
trachomatis (ophthalmic oint- ment)
Neonates: Apply a ribbon of ointment about 1 cm long in lower conjunctival sac of each eye
shortly after birth.
➢ Inflammatory acne vulgaris (topical gel, topical pads, topical solution)
Adults and children: Apply pads and solution to affected areas b.i.d., morning and evening.
Apply gel once or twice daily. If no improve- ment in 6 to 8 weeks, discontinue drug; pre-
scriber should reevaluate treatment.

ADMINISTRATION
Ophthalmic
● Don't use it for infection unless a causative organism has been identified.
● • To prevent ophthalmia neonatorum, apply ointment no later than 1 hour after birth. Use
drugs in neonates born either vaginally or by cesarean birth. Gently massage eyelids for 1
minute to spread ointment. Use a new tube for each neonate.
Topical
● Wash, rinse, and pat affected areas dry be- fore application.
● Wash hands after each application.
● Avoid contact with eyes, nose, mouth, mucous membranes, and broken skin.

INDICATIONS
For the treatment of superficial ocular infections involving the conjunctiva and/or cornea
caused by organisms susceptible to erythromycin. For prophylaxis of ophthalmia neonatorum
due to N. gonorrhoeae or C. trachomatis.
The effectiveness of erythromycin in the prevention of ophthalmia caused by
penicillinase-producing N. gonorrhoeae is not established.
For infants born to mothers with clinically apparent gonorrhea, intravenous or
intramuscular injections of aqueous crystalline penicillin G should be given; a single dose of
50,000 units for term infants or 20,000 units for infants of low birth weight. Topical prophylaxis
alone is inadequate for these infants.

DOSAGE AND ADMINISTRATION

In the treatment of superficial ocular infections, a ribbon approximately 1 cm in length of
ILOTYCIN™ Ophthalmic Ointment should be applied directly to the infected structure up to 6
times daily, depending on the severity of the infection.
 For prophylaxis of neonatal gonococcal or chlamydial conjunctivitis, a ribbon of
ointment approximately 1 cm in length should be instilled into each lower conjunctival sac. The
ointment should not be flushed from the eye following installation. A new tube should be used
for each infant.

ACTION
Inhibits protein synthesis; usually bacteriostatic, but may be bactericidal in high
concentrations or against highly susceptible organisms.

Route Onset Peak Duration

Ophthalmic, topical Unknown Unknown Unknown

Half-life: Unknown

ADVERSE REACTIONS
EENT: minor ocular irritations, redness.
Skin: burning, dryness, pruritus, erythema, irritation, oily skin, peeling, sensitivity reac- tions.
Other: hypersensitivity reactions.

INTERACTIONS
Drug-drug.
Clindamycin (topical): Topical erythromycin may antagonize clindamycin's effect. Avoid using
it together.
Drug-lifestyle. Abrasive or medicated soaps or cleansers, acne products or other prepa- rations
containing peeling drugs (benzoyl peroxide, resorcinol, salicylic acid, sulfur, tretinoin), alcohol-
containing products (after- shave, cosmetics, perfumed toiletries, shaving creams or lotions),
astringent soaps or cos- metics, medicated cosmetics or cover-ups: May cause cumulative
dryness, resulting in excessive skin irritation. Urge caution.

EFFECTS ON LAB TEST RESULTS

None reported.
CONTRAINDICATIONS & CAUTIONS
● Contraindicated in patients hypersensitive to drugs.
● Safety and effectiveness of topical drugs in children haven't been established. Dialyzable
drug: Unknown.

PREGNANCY-LACTATION-REPRODUCTION
● Use during pregnancy only if clearly needed. Topical drugs may be used to treat acne
during pregnancy.
● It isn't known if the drug appears in human milk after topical application. Use cautiously
in breastfeeding women.

NURSING CONSIDERATIONS
● Ointment and pads are intended only for treatment of inflammatory acne and not for
treatment of superficial skin infections.
● Store ophthalmic drugs at room temperature in tightly closed, light-resistant containers..
O Alert: Prolonged topical use may result in fungal or bacterial superinfection, including
pseudomembranous colitis and CDAD, dur- ing and even 2 months after treatment. Con-
sider these diagnoses in patients who present with diarrhea; stop drug for significant diar-
rhea, abdominal cramps, or passage of blood or mucus
● Topical drugs may be flammable; keep away from heat and flame.

PATIENT TEACHING
● Tell the patient to clean the eye area of excessive discharge before ophthalmic
application.
● Teach patients how to apply drugs and to wash hands before and after applying ointment.
Warn patient not to touch tip of applicator to eye or surrounding tissue.
● Tell the patient that vision may be blurred for a few minutes after applying ophthalmic
ointment. Instruct the patient to keep eyes closed for 1 to 2 minutes after applying the
drug.
● Advise patients to watch for and report signs and symptoms of sensitivity (itching lids,
redness, swelling, or constant burning of eyes or skin).
● Tell patients not to share drugs, washcloths, or towels with family members and to notify
prescriber if anyone develops the same signs or symptoms.
● Tell patient to wash hands after each application
● Stress importance of compliance with recommended therapy
● Advise the patient to wash, rinse, and dry face thoroughly before each topical use.
● Advise the patient to avoid topical use near eyes, nose, mouth, or other mucous
membranes.
● Tell the patient to stop using drugs and notify the prescriber if the condition worsens or if
there is no improvement.
● Caution patients to keep topical drugs away from heat and open flame.
● Advise patients to report diarrhea immediately.
 Drug Study on Chlorhexidine
Generic Name: Chlorhexidine
Brand Names: Betasept, Hibiclens, Instillagel, Nupro
Chlorhexidine, Oris, Oro-Clense, Paroex, Perichlor,
Peridex, Periochip, Periogard, Prevora, X-pur
Chemical Formula: C22H30Cl2N10

Chlorhexidine is an antiseptic used to sterilize for surgeries and in healthcare practice, to

reduce pocket depth in periodontitis, and to treat gingivitis. Chlorhexidine is a broad-spectrum
antimicrobial biguanide used as a topical antiseptic and in dental practice for the treatment of
inflammatory dental conditions caused by microorganisms. It is one of the most common skin
and mucous membrane antiseptic agents in use today. The molecule itself is a cationic bis-
guanide consisting of two 4-chlorophenyl rings and two biguanide groups joined by a central
hexamethylene chain. Topical chlorhexidine for disinfection, as well as oral rinses for dental use,
carries activity against a broad range of pathogens including bacteria, yeasts, and viruses.
Chlorhexidine was developed in the UK by Imperial Chemical Industries in the early
1950s and was introduced to the US in the 1970s. The FDA withdrew its approval for the use of
chlorhexidine gluconate topical tincture 0.5%, due to a significant number of reports concerning
chemical and thermal burns associated with the use of this product. Other formulations of
chlorhexidine continue to be available.

Indications and Dosage

Mouth/Throat
Aphthous ulcer, Oral candidiasis, Oral hygiene
● Adult: As chlorhexidine digluconate 0.2% spray: Apply bid. Max: 12 actuations bid. As
chlorhexidine digluconate 1% gel: Brush teeth with 1 inch of gel once or bid for about 1
minute. As chlorhexidine digluconate 0.2% solution: Rinse mouth bid with 10 mL for
about 1 minute or soak dentures for 15 minutes bid.
● Child: ≥12 years Same as adult dose.
Mouth/Throat
Gingivitis
● Adult: For treatment and prevention: As chlorhexidine digluconate 0.2% spray: Apply
bid for 1 month. Max: 12 actuations bid. As chlorhexidine gluconate 0.12% solution:
Rinse mouth bid with 15 mL for about 30 seconds. As chlorhexidine digluconate 0.2%
solution: Rinse mouth bid with 10 mL for about 1 minute. As chlorhexidine digluconate
1% gel: Brush teeth with 1 inch of gel once or bid for about 1 minute for 1 month.
● Child: ≥12 years Same as adult dose.

Mouth/Throat
Prophylaxis of dental caries
● Adult: As chlorhexidine digluconate 1% gel: Apply for 5 minutes every night for 14 days
in a close-fitting tray. Repeat treatment every 3-4 months.
● Child: ≥12 years Same as adult dose.

Topical/Cutaneous
Antiseptic and disinfectant
● Adult: As chlorhexidine acetate 0.05% solution: Irrigation of wound and burn. As
chlorhexidine gluconate 4% solution: General cleansing of skin and wounds. As
chlorhexidine gluconate 0.25% cream: Minor burns and abrasions.

Mechanism of action
Chlorhexidine’s broad-spectrum antimicrobial effects are due to its ability to disrupt
microbial cell membranes. The positively charged chlorhexidine molecule reacts with negatively
charged phosphate groups on microbial cell surfaces - this reaction both destroys the integrity of
the cell, allowing leakage of intracellular material, and allows chlorhexidine to enter the cell,
causing precipitation of cytoplasmic components and ultimately cell death. The specific means
of cell death is dependent on the concentration of chlorhexidine - lower concentrations are
bacteriostatic and result in leakage of intracellular substances such as potassium and
phosphorous, whereas higher concentrations are bactericidal and cause cytoplasmic precipitation.
Protein binding
● Chlorhexidine is known to bind albumin in both serum and saliva, though the extent of
this binding is unclear.
Metabolism
● As chlorhexidine is very poorly absorbed in the gastrointestinal tract, it is unlikely to
undergo metabolic conversion to any significant extent.
Route of elimination
● Excretion of chlorhexidine gluconate occurs almost exclusively via the feces, with less
than 1% of an ingested dose excreted in the urine.
Toxicity
● The LD50 of subcutaneously administered chlorhexidine in mice is >5 g/kg.
● Small children are likely to be more susceptible to chlorhexidine overdose - ingestion of
1-2 ounces by a small child may result in gastric distress, nausea, and intoxication.
Treatment should consist of symptomatic and supportive measures. Seek medical
attention if a child ingests >4 ounces of chlorhexidine solution or if symptoms of
intoxication develop post-exposure.
Drug Interactions
Drug
● Allogeneic cultured keratinocytes and dermal fibroblasts in murine collagen
Interaction
● The therapeutic efficacy of Allogeneic cultured keratinocytes and dermal fibroblasts in
murine collagen can be decreased when used in combination with Chlorhexidine.
Food Interactions
● Take it separately from meals. May affect the taste of food and beverages. Avoid eating
or drinking for 30 minutes following use.
Adverse Reactions
● Significant: Chemical burns in neonates.
● Gastrointestinal disorders: Dry mouth, taste alteration.
● Skin and subcutaneous tissue disorders: Dermatitis, pruritus, erythema, eczema, rash,
urticaria, skin irritation, blisters.
● Potentially Fatal: Serious allergic reactions (e.g. anaphylactic shock).
Pregnancy Category (US FDA)
● Mouth/Throat/Topical/Vag: B; Periodontal: C
Patient Counseling Information
● Not intended for use in the eye, auditory canal, meninges, brain, spinal cord and genital
area. This drug may stain teeth and tongue.
Action
● Description: Chlorhexidine exerts its bactericidal activity against gram-positive and
gram-negative organisms by binding cationic molecule to negatively charged bacterial
cell walls and extra microbial complexes leading to precipitation of cytoplasmic contents
of bacterial cell wall which results in cell death. At low concentration, it acts as a
bacteriostatic by alteration of bacterial cell osmotic equilibrium and leakage of potassium
and phosphorus.
● Absorption: Poorly absorbed from gastrointestinal tract.
● Excretion: Via feces (approx 90%); urine (<1%).

Chemical Structure

Chlorhexidine