Oral Pharmaceutical Agents for the Treatment of Ocular Pathologies.
Greg Caldwell, OD, FAAO
225 Terrace Drive
Lilly, PA 15938
814-931-2030 mobile
Grubc@aol.com
Outline
I.
II.
III.
Medical History
A. Chief complaint
B. History of the present illness
C. Review of systems
D. Dialysis
E. Past, Family and Social history
F. Current medications
G. Allergies/Adverse reactions
H. Pregnancy
Adverse Reaction/Allergic Reaction
A. Hypersensitivity
1. Fever
2. Rash
3. Photosensitivity
4. ANAPHYLAXIS
B. Hematologic
1. Neutropenia
2. Eosinophilia
3. Increase in PT/PTT
C. Gastrointestinal
1. Nausea
2. Vomiting
3. Diarrhea
D. Liver failure
E. Central nervous system
F. Ototoxicity
G. Cardiac
1. Dysrrhymia
FDA Pregnancy Categories
A. Category A
1. Studies in pregnant women
2. No risk
B. Category B
1. Animal studies no risk but human not adequate…or
2. Animal toxicity but human studies no risk
3. Safe
C. Category C
1. Animal studies show toxicity human studies inadequate but benefit of
use may exceed risk
2. Avoid
D. Category D
1. Evidence of human risk but benefits may out weigh risks
2. Avoid
E. Category X
1. Fetal abnormalities
2. Risks > benefits
3. Avoid
2
IV.
V.
VI.
VII.
VIII.
IX.
Renal Impairment
A. Identify patients on hemodialysis
B. Adjustment made by patient’s creatinine clearance (CrCl) ml/min
C. Work with patient’s primary care physician or internist
Case 1- Dacryocystitis, Preseptal Cellulitis and Bacterial Conjunctivitis
A. 58 year old male with red and painful OS
B. Visual acuity 20/20 OD, 20/60 OS
C. Picture of above conditions
D. Patient is allergic to Penicillin and Keflex
E. Treatment
1. Polytrim gtts QID OS
2. Zithromax
a. 1 Z-pack, use as directed PO
3. Dilation and irrigation
a. Contraindication versus indication
4. Confirmed nasolacrimal duct blockage, dacryocystorhinostomy DCR
5. Discussion on treatment
Augmentin
A. Amoxicillin and potassium clavulanate
B. Kills everything, good for everyone
1. 12 weeks old and older
C. Safe in pregnancy, category B
D. Watch for Penicillin allergies
E. Adults: 500mg BID (875mg BID)
F. Children < 100 pounds, oral suspension 25-45 mg/kg divided into two doses
G. Covers Staph, Strep, and Haemophilus influenzae
Zithromax (azithromycin)
A. Macrolide antibiotic
1. Like erythromycin
B. Drug of choice in Penicillin sensitive patients
C. All age groups
D. Safe in pregnancy, category B
E. No renal adjustment
F. Adults: 250mg BID, day 1 and 250mg QD, day 2-5
1. Dispense: 1 Z-pack as directed
G. Children <16: 10mg/kg, day 1 and 5mg/kg, day 2-5
H. Covers Staph, Strep, and Haemophilus influenza
I. Better tolerated than erythromycin, little GI upset
J. Chlamydia, 1 gram QD
Keflex
A.
B.
C.
D.
E.
F.
(cephalexin)
Cross reaction with Penicillin sensitive patients
First generation, moderately affective against Penicillin-ase
Good for gram +, not good for Haemophilus which is gram –
Category B
Adult: 500mg BID for one week
Drug of choice for blow out fractures
Ceftin (cefuroxime)
A. Cross reaction with Penicillin sensitive patients
B. Second generation
C. Better for Haemophilus (-)
D. Children: 3 months to 12 years old, oral suspension 20-30mg/kg/day divided
into two doses
E. Adults: 250mg BID for 10 days
3
F.
X.
XI.
XII.
Category B
Cipro (ciprofloxacin), Levoquin (levofloxacin)
A. End of the line antibiotic
B. Really effective
C. Category C
1. Avoid during pregnancy
D. Only use if 18 years old or older
E. 500mg BID for one week, Cipro
F. 500mg QD for one week, Levoquin
Sulfa Drugs
A. Bactrim (sulfamethoxazole/trimethoprim)
B. Limited use…last line of defense
C. High incidence of Steven-Johnsons
D. Avoid in pregnancy
1. Category C
E. Avoid in sickle cell disease
F. Cross reaction with:
1. Oral hypoglycemics
2. Carbonic anhydrase inhibitors
3. Celebrex
4. Thiazide diuretics
5. All the above are sulfa based
G. Bactrim BID for ten days
H. Bactrim DS BID for ten days
Summary
A. Adults
1. Augmentin
2. Zithromax
3. Keflex
4. Cipro
5. Bactrim
B. Children
1. Augmentin
2. Zithromax
3. Ceftin
4. Avoid Cipro
5. Bactrim
XIII.
Case 2- Rosacea Blepharitis
A. 48 year old male both eyes are red, gritty, sandy and dry
B. Visual acuity 20/20 OU
C. Show multiple pictures of rosacea, lid margins and conjunctiva
D. Treatment
1. Warm compresses
2. Lid hygiene
3. Artificial tears
4. Doxycycline 100mg QD for at least one month
5. Dermatological consult
6. Discussion on treatment
XIV.
Vibramycin (doxycycline)
A. Drug of choice for marginal inflammatory blepharitis
B. Antibiotic, anti-inflammatory and anti-collagenase
C. Inhibits the lipase enzyme
D. Avoid in children
E. Category D
4
1. Avoid in pregnancy
F. No renal adjustment
G. Can enhance coumadin
H. 50-100mg QD for 2-12 weeks
I.
XV.
XVI.
XVII.
XVIII.
XIX.
XX.
XXI.
XXII.
XXIII.
XXIV.
Lower maintenance dose
1. 20 mg Periostat (Doxycycline)
2. Helpful in those with stomach or GI sensitivity
3. Excellent for those requiring long maintenance dose
J. My Paradigm for Minocycline / Doxycycline
1. Status of MG
a. Inspissated
b. Turbid
c. Clear
K. Maximum dosage for 2-12 weeks (pulse)
1. 100 mg BID, QD
2. 50-100mg qd while turbid
3. 20 mg longer treatments
L. Customize Treatment
M. 50 mg Minocycline with pill cutter (25 mg)
Oracea- 40 mg of Doxycycline total
A. 30 mg immediate release
B. 10 mg sustained release
Alodox Kit
A. 20 mg Doxycycline
B. Ocusoft lid scrub
AzaSite (azithromycin opthalmic solution) 1.0%
A. Initiate early in treatment
B. Adjunctive when patient is already on Doxycycline
C. Alternative in states that do not have oral therapeutic licensure
Precautions With Oral Tetracycline Analogs
A. Enhanced photosensitivity
B. Avoid in children and pregnancy (Category D)
C. Can enhance Coumadin
D. Can enhance the action of digoxin
E. ?Long term use with increase risk of breast cancer?
F. 1 paper/study, not regarded as highly reliable study
G. Further investigation discredited the association
H. Benign intracranial hypertension, reported cases
1. 17 cases from 1978-2002
Benign intracranial hypertension
“It’s not rare if it’s in your chair”
Minocycline
A. Less photosensitivity
B. Less GI upset
C. Less bacterial resistance
Minocycline for Ulcers?
Are the anti-inflammatory benefits useful to help reduce the corneal degradation that
occurs in sterile and infectious keratitis?
Final Thoughts
A. Penicillin, Ampicillin and Amoxicillin are of no benefit for treating ocular
infections
B. Popular Penicillin derivative, Dicloxacillin 250mg QID for a week
Case 3- Varicella Zoster Virus, Herpes Zoster Ophthalmicus
A. 52 year old male with red and painful OD
B. Visual acuity 20/30 OD, 20/20 OS
C. Show multiple pictures of lids and conjunctiva
D. Discussion on treatment
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XXV.
XXVI.
Oral Anti-Virals
A. Third generation, go into every cell but only activate in viral infected cells
B. First generation were mutogenic
C. Can be used prophalactically prior to PKP, LASIK or PTK
Zovirax (acyclovir)
A. Good for simplex
B. Poor absorption
C. Dosage: 800mg 5 times per day
D. Maintenance dose: 200-400mg BID
E. Category B
XXVII.
Famvir
A.
B.
C.
XXVIII.
Valtrex
A.
B.
C.
D.
E.
XXIX.
XXX.
(famcyclovir)
Proven to reduce post-herpetic trigeminal neuralgia
Drug of choice for zoster patients 50 years old and older
Dosage:
1. Zoster 500mg TID
2. Recurrent simplex 125-250mg BID
D. Category B
(valacyclovir)
Pro-drug of acyclovir
GI upset
HSV-1, HSV-2 and VZV
Dosage: 1 g TID for one week
Category B
Case 4- Recurrent Herpes Simplex Keratitis
A. 47 year old female with a red and painful OD
B. Visual acuity 20/30 OD, 20/20 OS
C. First episode
1. Discussion on treatment
D. Second episode
1. Discussion on treatment
E. Third episode
1. Discussion on treatment
Herpetic Eye Disease Study
A. HEDS I
1. Benefit from steroids in stromal keratitis
2. No benefit from oral acyclovir in stromal keratitis
3. Benefit from steroids if iritis present
B. HEDS II
1. No benefit from acyclovir to stop progression to stromal or iridocyclitis
2. Maintenance dose 400mg BID, decreases recurrence by 41% within
first year
XXXI.
28 year old woman, curling her hair. She turned her head and thinks she touched her
eye. Currently her eye is very painful.
A. Debride?
B. Antibiotic gtts
C. Artificial tears
D. Pain Management
1. BCL
2. Oral pain management
3. NSAID gtts
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XXXII.
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XXXIV.
XXXV.
XXXVI.
Oral Pain Relievers
A. Acetaminophen typically with opioid derivative
B. Synergism (peripheral and central acting)
C. Avoid acetaminophen in alcoholics or people who have 3 or more
drinks/day…causes liver failure…bleeding
D. Avoid acetaminophen with coumadin…inc pro-time
E. FYI-avoid ibuprofen/nsaids in Type 1 & 2 DM, causes reduced renal function,
Type 2 reacts with oral hypoglycemic agents
F. What is APAP?
1. Acetaminophen
2. Usually found on Rx bottles
3. APAP/Codeine
Federal Law Categorizes Controlled Substances into Five Schedules
A. SCHEDULE I
1. Drugs cannot be prescribed except in special research situations
2. There is no approved medical use
3. LSD, marijuana, heroin
B. SCHEDULE II
1. Drugs with significant addictive potential
2. Maximum 30-day supply for any one prescription
3. No refills
4. No phoned prescriptions except in emergency
5. Opium, Demerol, oxycodone
C. SCHEDULE III
1. Drugs which have some potential for abuse
2. Maximum 90-day supply
3. Maximum five refills within a six-month period
4. Phone prescriptions allowed
D. SCHEDULE IV
1. Drugs which have low potential for abuse
2. Maximum 90-day supply
3. Maximum five refills within a six-month period
4. Phone prescriptions allowed
E. SCHEDULE V
1. Low abuse potential and have been designated for regulation by
individual states
2. Maximum 90-day supply
3. Phone prescriptions allowed
Oral Pain Reliever Pearls
A. OD’s in all states are now allowed to prescribe or recommend OTC pain
relievers
B. Drug Enforcement Agency (DEA) numbers are required to prescribe controlled
substances
C. The real value of schedule III and schedule IV narcotic analgesics
1. They provide good pain relief
2. A degree of sedation
3. Tend to minimally impact the digestive system and kidneys
4. It's not that they're dramatically more potent than OTC analgesics like
aspirin, acetaminophen, ibuprofen or naproxen
Pain Reliever Help
A. Know your maximum daily allowances
1. APAP 4000 mg
2. ASA 6000 mg
3. Ibuprofen 3200 mg
4. Naproxen 1000 mg (Aleve/Naprosyn)
5. Propoxyphene HCl 600 mg
6. Codeine 240 mg
7. Hydrocodone 60 mg
Acetaminophen and Propoxyphene Napsylate-Sch IV
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XXXVIII.
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XL.
XLI.
A. Darvocet-N 50-325mg/50 mg
1. maximum dose of propoxyphene 600 mg/day
2. 1-2 tablets q 4-6 hours, mild to moderate pain
B. Darvocet-N 100-650 mg/100 mg
1. max 600 mg/day
2. 1 tablet q 4-6 hours, mild to moderate pain
ASA and Propoxyphene HCl
A. Darvon-N
B. Schedule IV
C. Mild analgesic
D. Good sedative
E. ASA 389mg and 65mg propoxyphene
F. Dosage q 4 hours prn for pain
G. Maximum ASA 6 grams daily
Acetaminophen with Codeine (Sch III)
A. T1-300mg/7.5 mg
B. T2-300mg/15 mg
C. T3-300mg/30 mg
D. T4-300mg/60 mg
E. Maximums
1. Acetaminophen- 1 g QID
1. 4000 mg per day
2. Codeine- 60 mg QID
1. 240 mg per day
Acetaminophen with Hydrocodone (Sch III)
A. Lortab
1. 500 mg/2.5 mg
2. 500 mg/5.0 mg
3. 500 mg/7.5 mg*
4. 500 mg/10 mg
B. 1-2 tablets q4-6 hours for moderate to severe pain
C. Category C
D. Vicodin HP
1. 660 mg/10 mg*
E. Vicodin
1. 500 mg/5 mg
F. Vicodin ES
1. 750 mg/7.5 mg
G. Vicodin 1-2 tablets q4-6 hours for moderate to severe pain
H. Category C
Questions
XXIV.
Thank-you