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Pharmacology A to Z
I.
II.
Review of Goals and Objectives of Lecture
a. Be comfortable with the medications discussed.
b. Be able to recognize the uses for each of the medications discussed.
c. Know the indications and contraindications of each of the medications discussed.
d. Be able to recognize the potential ocular effects of these medications.
e. Be able to interact with the presenters and other attendees.
Review of Medications A to Z
a. Azasite
i. Indications, contraindications, dosages
b. Botox
i. Indications, contraindications, dosages
c. Combigan
i. Indications, contraindications, dosages
d. Doxycycline
i. Indications, contraindications, dosages
e. Elestat
i. Indications, contraindications, dosages
f. FreshKote
i. Indications, contraindications, dosages
g. Gabapentin
i. Indications, contraindications, dosages
h. Hytrin
i. Indications, contraindications, dosages
i. Istalol
i. Indications, contraindications, dosages
j. Januvia
i. Indications, contraindications, dosages
k. Keflex
i. Indications, contraindications, dosages
l. Lotemax
i. Indications, contraindications, dosages
m. Macugen
i. Indications, contraindications, dosages
n. Nevanac
i. Indications, contraindications, dosages
o. Optivar
i. Indications, contraindications, dosages
p. Plaquenil
i. Indications, contraindications, dosages
q. Quixin
i. Indications, contraindications, dosages
r. Retisert
i. Indications, contraindications, dosages
III.
s. Salagen
i. Indications, contraindications, dosages
t. Tamoxifen
i. Indications, contraindications, dosages
u. Ultram
i. Indications, contraindications, dosages
v. Vigamox
i. Indications, contraindications, dosages
w. Warfarin
i. Indications, contraindications, dosages
x. Xibrom
i. Indications, contraindications, dosages
y. Yodoxin
i. Indications, contraindications, dosages
z. Zylet
i. Indications, contraindications, dosages
Potential Ocular Sequelae of A to Z Medications
Pharmacology A to Z
Jeffrey R. Varanelli, OD, FAAO
Nicholas Colatrella, OD, FAAO
A
Azasite (azithromycin ophthalmic solution 1%)
Inspire Pharmaceuticals
Broad-spectrum coverage against the most common gram-positive and gram-negative bacteria as
well as
atypical bacteria
Gel-forming drop persists on the ocular surface much longer than conventional aqueous drops with
minimal blurring
Indications
treatment of bacterial conjunctivitis caused by the following organisms: CDC coryneform
group G, Staphylococcus aureus, Streptococcus mitis group, Streptococcus pneumoniae, and
Haemophilus influenzae
Adverse events
most common was eye irritation (1-2%)
Other adverse events (<1%)
burning, stinging, and irritation upon instillation
contact dermatitis
corneal erosion
dry eye
nasal congestion
ocular discharge
punctate keratitis
sinusitis
Dosage
1 drop BID for 2 days, followed by 1 drop QD for the next 5 days
9 drops total
use in patients with lid margin disease
B
Botox®
Botulinum Toxin Type A
produced from fermentation of Hall strain Clostridium botulinum type A
Indications
treatment of strabismus and blepharospasm associated with dystonia, including benign
essential blepharospasm or VII nerve disorders in patients 12 years of age and above.
efficacy in deviations over 50 prism diopters, in restrictive strabismus, in Duane's syndrome
with lateral rectus weakness, and in secondary strabismus caused by prior surgical overrecession of the antagonist has not been established
Blepharospasm
EMG guidance
Injected into medial and lateral pre-tarsal orbicularis oculi
Avoid levator to avoid ptosis
Initial effect seen within 3 days
May see swelling/ecchymosis
Strabismus
EMG guidance or surgical exposure recommended
Creates paralysis of injected muscle
Lasts 2-6 weeks
Recommendations
Vertical muscles and horiz
1.25-2.5 units in any one muscle
Horizontal strabismus (202.5-5.0 units in any one muscle
Persistent CN VI palsy (> 1 month)
1.25-2.5 units in medial rectus
C
Combigan™0.2/0.5%
Allergan
2 mg/mL of brimonidine tartrate and 5 mg/mL of timolol
Dosage
1 drop in affected eye(s), twice daily, approximately 12 hours apart
Indications
indicated for the reduction of elevated intraocular pressure (IOP) in patients with glaucoma or
ocular hypertension who require adjunctive or replacement therapy due to inadequately
controlled IOP
Contraindications
Bronchial asthma, a history of bronchial asthma, severe COPD
Sinus bradycardia, second or third degree atrioventricular block, overt cardiac failure,
cardiogenic shock
Hypersensitivity to any component of this product
D
Doxycycline
Tetracycline family
Bacteriostatic
Inhibit protein synthesis
Careful of resistance
Good gram positive and gram negative coverage
Indications
Blepharitis
Meibomian Gland Disease
Recurrent Corneal Erosion
Rosacea
Contraindications
Pregnancy Category D
Children under 8
Precautions
Photosensitivity
Dosage
100 mg BID x _____ days
Taper as needed
Monitor closely
E
Elestat (epinastine HCl 0.05%)
Inspire Pharmaceuticals
Anti-histamine with mast cell-stabilizing activity
Indications
For the prevention of ocular itching associated with allergic conjunctivitis
Contraindications
In patients who have shown hypersensitivity to epinastine or to any of the other ingredients
Administration
BID dosing
Adverse effects
burning sensation, hyperemia, pruritus
Non-ocular adverse events were infection (cold symptoms and upper respiratory infections),
headache, rhinitis, sinusitis, increased cough, and pharyngitis
Recent studies about the ocular surface after ELESTAT® treatment
No change in corneal staining
No change in tear volume
No change in tear-film break-up time
F
FreshKote
Focus Laboratories
2.0% Polyvinyl pyrrodilone
0.9% Polyvinyl alcohol (87% hydrolyzed)
1.8% Polyvinyl alcohol (99% hydrolyzed)
Treats all 3 tear film layers
Lipid layer
Aqueous layer
Mucin layer
Has a high oncotic pressure
Re-establishes integrity of epithelium
Reduces microcystic edema
Prevents recurrent damage
Indications:
a lubricant indicated for the treatment of moderate to severe dry eye
Contraindications:
in patients with known severe hypersensitivity to any of the ingredients in the formulation
Prescription only
Supplied in 3.5 ml or 15 ml bottles
Dosage
1 or 2 drops in affected eye(s) as needed
G
Gabapentin (Neurontin, Gabarone)
GABA analog
initially synthesized to mimic the structure of gamma-aminobutyric acid (GABA)
Mechanism of Action: unknown
Indications
Epiliepsy
Post-herpetic neuralgia
Contraindications/Cautions
Impaired renal function
Elderly patients
Hypersensitivity to drug/class/compound
Off label uses
Migraines
Neuropathic pain
Neuropathic pain
Post-PRK use
100-300 mg tid x days
Benefit to prescribing before surgery?
Maximum daily dose 3600 mg
H
Hytrin (terazosin)
alpha-adrenergic blocker
causes the blood vessels to dilate
also relaxes muscles in the prostate and bladder neck
used to treat hypertension and benign prostatic hyperplasia (BPH)
Sympathetic stimulation of ANS causes pupillary _____
Alpha 1 blocker
Leads to miosis
Challenges in cataract surgery
IFIS
Intraoperative Floppy Iris Syndrome
poor pre-operative pupil dilation
iris billowing and prolapse
progressive intra-operative miosis
Optometrist’s role
Be cautious of patient medications
Review case with co-managing surgeon
Ophthalmologist’s role
Iris hooks, iris retractors, OVD (Healon 5)
I
Istalol 0.5% (timolol maleate 0.5%)
Ista Pharmaceuticals
non-selective beta-blocker
has the action of reducing elevated as well as normal IOP
Indications
treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle
glaucoma
Contraindications
bronchial asthma
history of bronchial asthma
severe COPD
sinus bradycardia
second or third degree atrio-ventricular block
overt cardiac failure
cardiogenic shock
hypersensitivity to any component of this product
Cautions
Same as other beta blockers
Dosage/Administration
1 drop in affected eye(s) qAM
Concomitant treatment with other beta blocker not recommended
Onset of Action
usually detected within 30 minutes after a single dose
maximum effect usually occurs in 1-2 hours
significant lowering of IOP can be maintained for periods as long as 24 hours with a single
dose
repeated observations over a period of one year indicate that the IOP lowering effect of
ISTALOL is well maintained
J
Januvia (sitagliptin)
Merck
Increases insulin made in pancreas
Decreases sugar made in liver
Combine with proper diet and exercise
Indications
as an adjunct to diet and exercise to improve glycemic control in adults with Type 2 DM
JANUVIA should not be used in patients with type 1 diabetes
JANUVIA should not be used for the treatment of diabetic ketoacidosis
JANUVIA has not been studied in combination with insulin
Contraindications
History of a serious hypersensitivity reaction to sitagliptin
Dosage/Administration
100 mg tablet once a day
With or without food
No ocular side effects noted
Newer studies
K
Keflex (cephalexin)
Cephalosporin
Gram positive and Gram negative
Indications
treatment of the following infections when caused by susceptible strains of the designated
microorganisms:
Respiratory tract infections caused by Streptococcus pneumoniae and Streptococcus
pyogenes
Otitis media due to Streptococcus pneumoniae, Haemophilus influenzae,
Staphylococcus aureus, Streptococcus pyogenes, and Moraxella catarrhalis
Skin and skin structure infections caused by Staphylococcus aureus and/or
Streptococcus pyogenes
Bone infections caused by Staphylococcus aureus and/or Proteus mirabilis
Genitourinary tract infections, including acute prostatitis, caused by Escherichia coli,
Proteus mirabilis, and Klebsiella pneumoniae
Contraindications
Those with known allergy to cephalosporin group of antibiotics
Supplied as:
250 mg capsules
333 mg capsules
500 mg capsules
750 mg capsules
Relevance to Optometry
Pre-septal cellulitis
250-500 mg qid
Hordeolum
250 mg tid
Any external lid disease
Red, swollen eyes/lids
L
Lotemax (loteprednol etabonate 0.5%)
Bausch and Lomb
0.5% ophthalmic suspension
Unique site active mechanism of action
Less effect on IOP
Highly lipid soluble
Indications
treatment of steroid responsive inflammatory conditions associated with the palpebral and
bulbar conjunctiva, cornea, and anterior segment of the globe
Contraindications
most viral diseases of the cornea and conjunctiva and in mycobacterial and fungal diseases of
the eye
Precautions
Prolonged use may result in secondary glaucoma, cataract formation, and secondary ocular
infections
Dry eye treatment
QID x 2(or 4) weeks, then BID x 2 (or 4) weeks
Works well in conjunction with Restasis
Better than with artificial tears
M
Macugen (pegaptanib sodium injection)
Eyetech/Pfizer
(VEGF) Inhibitor
inhibits VEGF, which is responsible for inducing angiogenesis, increasing vascular
permeability and inflammation. VEGF has also been implicated in blood retinal
barrier breakdown and pathological ocular neovascularization
First anti-VEGF approved by FDA (2004)
Indications
For the treatment of neovascular age-related macular degeneration
Contraindications
Ocular or peri-ocular infections
Administration
0.3mg by intra-vitreous injection once every 6 weeks
Adverse reactions
Anterior chamber inflammation
blurred vision
Cataract
conjunctival hemorrhage
corneal edema
eye discharge, eye irritation, eye pain
increased IOP
ocular discomfort
punctate keratitis
reduced visual acuity
visual disturbance
vitreous floaters and vitreous opacities
N
Nevanac (nepafenac 0.1% suspension)
Alcon
Topical NSAID
Indications
Treatment of pain and inflammation associated with cataract surgery
Contraindications
Hypersensitivity to any ingredients in the formula or to other NSAIDs
Warnings/Precautions
Increased bleeding due to increased thrombocyte aggregation
Delayed healing
Corneal effects (including keratitis)
Adverse Reactions
Capsular opacity
Decreased VA
Increased IOP
Sticky sensation
Dosage/Administration
1 drop applied to the affected eye(s) beginning three-times-daily 1 day prior to cataract
surgery, continued on the day of surgery, and through the first two weeks of the postoperative period
Off-label uses
Allergies
Foreign Bodies
Corneal Abrasions
RGP Adaptation
Topical NSAIDs
Study by Weaver et al:
Compared topical NSAID to placebo in corneal abrasion patients
Patients had similar corneal healing time
Quicker pain relief with topical NSAID
O
Optivar (azelastine hydrochloride ophthalmic solution 0.05%)
Meda Pharmaceuticals
Relatively selective histamine H1 antagonist and an inhibitor of the release of histamine and
other mediators involved in the allergic response
Indications
treatment of itching of the eye associated with allergic conjunctivitis
Contraindications
in persons with known or suspected hypersensitivity to any of its components
Warnings
for ocular use only and not for injection or oral use
Dosage/Administration
one drop instilled into each affected eye twice a day
Adverse reactions
most frequently reported adverse reactions were transient eye burning/stinging (30%),
headaches (15%) and bitter taste (10%). The occurrence of these events was generally mild.
The following events were reported in 1-10% of patients:
Asthma
Conjunctivitis
Dyspnea
eye pain
fatigue
influenza-like symptoms
pharyngitis, pruritus, rhinitis
temporary blurring
P
Plaquenil (hydroxychloroquine sulfate)
Sanofi-Aventis
Quinine derivative
Indications
Suppression and treatment of acute attacks of malaria in adults and children. Treatment of
discoid and systemic lupus erythematosus and rheumatoid arthritis (RA) in adults
Contraindications
Long term therapy in children or if retinal/visual field changes due to 4-aminoquinoline
compounds
Optometrist’s role
Visual acuity
Color vision
HVF 10-2 (Macular field)
Dilated fundus exam
Baseline fundus photos
Letter to patient’s doctor(s)
Plaquenil toxicity
Drug accumulates in RPE
Gives Bull’s eye appearance to retina
Frequency <5% when dose is under 400 mg/day
Plaquenil Toxicity
Risk factors
daily dose greater than 6.5 mg/kg
>400 mg/day
greater than 10 years of use
liver problems
kidney problems
age over 60
Q
Quixin (levofloxacin ophthalmic 0.5%)
Vistakon/Santen
Good Gram positive and Gram negative coverage
Inhibits both topoisomerase IV and DNA gyrase enzymes
Interferes with DNA replication, transcription, repair, and recombination
Appropriate for children >1 year
Indications
treatment of bacterial conjunctivitis caused by susceptible strains of the following organisms
Corynebacterium species
Staphylococcus aureus
Staphylococcus epidermidis
Streptococcus pneumoniae
Streptococcus (Groups C/F)
Streptococcus (Group G)
Viridans group streptococci
Acinetobacter Iwoffii*
Haemophilus influenzae
Serratia marcescens
Contraindications
contraindicated in patients with a history of hypersensitivity to levofloxacin, to other
quinolones, or to any of the components in this medication
Dosage
Days 1 and 2:
Instill one to two drops in the affected eye(s) every 2 hours while awake, up to 8 times
per day.
Days 3 through 7:
Instill one to two drops in the affected eye(s) every 4 hours while awake, up to 4 times
per day.
R
Retisert (fluocinolone acetonide intravitreal implant 0.59 mg)
Bausch and Lomb
Indications
indicated for the treatment of chronic non-infectious uveitis affecting the posterior segment of
the eye
Contraindications
most viral diseases of the cornea and conjunctiva including epithelial herpes simplex keratitis
(dendritic keratitis), vaccinia, and varicella, and also in mycobacterial infections of the eye
and fungal diseases of ocular structures
in individuals with known or suspected hypersensitivity to any of the ingredients of this
preparation and to other corticosteroids
Contains specially formulated ocular steroids
Slowly releases the steroid medication in precise, measured amounts into the eye, on a daily basis for
about 2.5 years
Most frequently reported ocular adverse events in the overall study population were:
cataract
increased IOP
procedural complications
eye pain
occurred in approximately 50% to 90% of patients
Surgical procedure
Generally implanted under local anesthesia
Implanted using a limbal conjunctival peritomy and creating a 3.5-mm pars plana
sclerectomy
Secured in vitreous cavity with 8-0 Prolene™ anchoring suture
Sclerectomy closed in with 8-0 or 9-0 Prolene suture
S
Salagen (pilocarpine hydrochloride)
cholinergic parasympathomimetic agent
can increase secretion by the exocrine glands
sweat, salivary, lacrimal, gastric, pancreatic, and intestinal glands and the mucous
cells of the respiratory tract
Indications
treatment of symptoms of dry mouth from salivary gland hypofunction caused by
radiotherapy for cancer of the head and neck
treatment of symptoms of dry mouth in patients with Sjögren's syndrome
Contraindications
patients with uncontrolled asthma
known hypersensitivity to pilocarpine
when miosis is undesirable
acute iritis and narrow-angle/angle closure glaucoma
Potential ocular side effects
Visual disturbances, especially at night, that could impair their ability to drive safely
Cataract
Conjunctivitis
Dry eyes
Eye disorder
Eye hemorrhage
Glaucoma
Lacrimation disorder
Retinal disorder
Abnormal vision
T
Tamoxifen (Novaldex, Soltamox)
Anti-estrogen
Indications
Treatment of metastatic breast cancer in women and men
Treatment of node-positive and axillary node-negative breast cancer in women
following mastectomy, axillary dissection and breast irradiation
To reduce risk of invasive breast cancer in women with DCIS
Reduction of breast cancer incidence in high risk women
Use for up to 5 yrs
Contraindications
Reduction in breast cancer incidence in high risk women and women with DCIS who
require Coumadin-type anticoagulant therapy or have a history of DVT, PE.
Potential Ocular Side Effects
crystalline retinal deposits
macular edema
corneal changes
extensive retinal lesions and macular edema with visual impairment have been reported in a
few patients receiving high-dose tamoxifen
Less extensive retinal changes may occur in patients receiving low doses for long
periods, and isolated retinal crystals may be observed in patients without visual
symptoms
Papilledema
optic neuritis
color vision defects
decreased vision
visual field abnormalities
vortex keratopathy
toxic crystalline maculopathy
cataract
Tamoxifen Retinopathy
-Superficial yellowish-white crystalline deposits
-Reversible upon discontinuation of drug
-Any macular deposition may be permanent
Tamoxifen Keratopathy
-Bilateral white, whorl-like, central, subepithelial opacities in the cornea
U
Ultram (tramadol HCl)
Central acting analgesic
Synthetic analog of codeine
Binds to opioid receptors
Not a controlled substance
Low abuse potential
Opioid-type dependence has been reported
Ultram tablets
50 mg Tramadol HCl
1-2 tablets every 4-6 hours
Do not exceed 400 mg/day
Safe for geriatric patients
Indications
Management of moderate to moderately severe pain
Contraindications
Acute intoxication with any of the following: alcohol, hypnotics, narcotics, centrally-acting
analgesics, opioids or psychotropic drugs
V
Vigamox (moxifloxacin HCl 0.5%)
Alcon
4th generation fluoroquinolone
Indications
Treatment of bacterial conjunctivitis caused by susceptible organisms
Contraindications
Patients with a history of hypersenstivity to moxifloxacin, to other quinolones, or to any of the
components of this medication
Non-approved uses
Corneal ulcers, corneal abrasions
Approved for children >1 year
Recommended dosage: 1 drop TID x 7 days
W
Warfarin (Coumadin)
an anticoagulant which acts by inhibiting vitamin K-dependent coagulation factors
Indications
prophylaxis and/or treatment of venous thrombosis and its extension, and pulmonary
embolism.
prophylaxis and/or treatment of the thrombo-embolic complications associated with
atrial fibrillation and/or cardiac valve replacement
reduce the risk of death, recurrent myocardial infarction, and thrombo-embolic
events such as stroke or systemic embolization after myocardial infarction
Potential ocular side effects
Subconjunctival hemorrhage
Retinal/macular hemorrhage
Consult with patient’s physician and ophthalmologist when referring for any ocular surgery
X
Xibrom (bromfenac sodium 0.09%)
ISTA Pharmaceuticals
Topical NSAID
No safety information on patients <18 years old
Indications
treatment of post-operative inflammation and reduction of ocular pain in patients who have
undergone cataract extraction
Contraindications
in patients with known hypersensitivity to any ingredient in the formulation
Dosage/Adminstration
one drop should be applied to the affected eye(s) two times daily beginning 24 hours after
cataract surgery and continuing through the first 2 weeks of the postoperative period
Adverse Reactions (2-7%)
abnormal sensation in eye
conjunctival hyperemia
eye irritation (including burning/stinging)
eye pain, eye pruritus, eye redness
headache
iritis
Y
Yodoxin (iodoquinol)
Glenwood
amebicidal against Entamoeba histolytica and is considered effective against the trophozoite
and cyst forms
Anti-protozoal
Indications
treatment of intestinal amebiasis
Contraindications
known hypersensitivity to iodine and 8-hydroxyquinolines
patients with hepatic damage
Potential ocular side effects
optic neuritis
optic atrophy
decreased vision
eye pain
Z
Zylet (loteprednol etabonate 0.5% and tobramycin 0.3% ophthalmic suspension)
Bausch and Lomb
Anti-inflammatory and anti-infective
First and only ophthalmic corticosteroid/antibiotic combination to contain an "ester"
corticosteroid
First FDA approved anti-inflammatory/anti-infective ophthalmic combination since the 1980’s
Indications
steroid-responsive inflammatory ocular conditions for which a corticosteroid is indicated and
where superficial bacterial ocular infection or a risk of bacterial ocular infection exists and
where the inherent risk of steroid use in certain infective conjunctivitides is accepted to
obtain a diminution in edema and inflammation
Contraindications
in most viral diseases of the cornea and conjunctiva and also in mycobacterial infection of the
eye and fungal diseases of ocular structures
Dosage/Administration
Apply one or two drops of Zylet into the conjunctival sac of the affected eye(s) every four to
six hours
During the initial 24 to 48 hours, the dosing may be increased to every one to two hours
Frequency should be decreased gradually as warranted by improvement in clinical signs
Care should be taken not to discontinue therapy prematurely