PHARMACEUTICAL UPDATE or Everything You Wanted to Know About Therapeutics, But Were Afraid to Ask

Transcription

1 PHARMACEUTICAL UPDATE or Everything You Wanted to Know About Therapeutics, But Were Afraid to Ask Bruce E. Onofrey, R.Ph., O.D. Professor, University of Houston

2 Better title-favorite therapeutic strategies Proper DX Proper staging Adjunct therapy Proper drug selection Prognosis Patient counseling On-going patient assessment (The Herpes steroid provocative test

3 QUESTIONS? CALL ME E:MAIL EYEDOC3AOL.COM FAX:

4 Name the best anesthetic for LASIK, topical cataract surgery and lachrymal procedures. 1. Proparacaine 2. Tetracaine 3. Lidocaine 4. Cocaine 5. Benoxinate

5 Anesthetics Lidocaine vs Proparacaine Amide VS Esther Cross-Allergy Efficacy Increase duration with phenylephrine 2.5%

6 Clinical Pearl#2: Don t try to Patch Without It Proper technique requires that the patient NOT be wrapped like a mummy with tape. Do not attach tape to nose, ears or glasses One touch technique Requires adhesive- Tincture of benzoin cmpd.

7 Management of Dry Eye How do YOU spell D-R-Y E-Y-E Ocular surface disease is a serious business Chronic condition Multiple dry eye factors Mild to severe presentations

8 Evoxac: New and improved pilocarpine Parasympathomimetic Better tolerated 30mg TID No titration necessary NEVER in asthmatics

9 Step Therapy of Dry Eye Non or soft preserved lubication (gel dosage form) Punctal Occlusion Parasympathomimetic therapy: Salagen 5mg QID/Increases lacrimal production via stimulation of exocrine glands

10 Break-Through Technology in the Management of Tear Film Disorders ONLY A PHARMACIST CAN APPRECIATE THIS CHEMISTRY AIN t technology great

11 The Desperate CL Patient (THE GOOD NEWS) 16 Y/O female (-) 2.50 myope OU MUST wear tinted, EW CLS

12 THE BAD NEWS Tried CL s 2 months ago at the bad Drs. Office. Never felt right. Doctor never got it right Med hx: Acne, pink eye -Probably from those bad CL s Allergic to Pen and Sulfa Meds: Visine daily, Accutane, benzoyl peroxide 10% topical gel

13 The IDEAL Patient? Dry eye Poor hygiene Compliance Atopy

14 Management? Fit with CL s -What kind?? Drug Sideeffects? Treatment?

15 The Ideal Anti-infective Effective and selective Bacteriocidal Not destroyed by enzymes Rapid absorption No allergies Compatible with other drugs High therapeutic index Should not be toxic

16 It s about time we had a replacement for erythromycin ointment

17 Azasite for all Broad spectrum anti-infective Safe in kids (Hemophilus) Anti-inflammatory (Blepharitis) MRSA Chlamydia

18 The New Fluoroquinolones Moxeza (et al) Benefits Pharmacology

19 Let s Start with the Kids: Pediatric conjunctivitis plays by different rules Don t treat pediatric conjunctivitis without first: Check history Check ears Check throat Check temperature

20 What percentage of all bacterial corneal ulcers in a major study were successfully treated with ciprofloxacin mono therapy? 1. 55% 2. 82% 3. 96% 4. 98% %

21 The greatest resistance to the drug is in which organisms? 1. Gram positive 2. Gram negative

22 Cell wall Inhibitors Penicillins Cephalosporins Bacitracin

23 Bacterial Ulcer Guidelines Always culture if you have the means Patients that get better never sue-those that don t-do Consider the rule Fluoroquinolone mono-therapy is not foolproof Grade the ulcer-location, location, etc Step TX based on cultures

24 Sometimes eye drops are just not enough

25 Oral antibiotics used to TX eye disease must be effective against: 1. Resistant acanthamoeba 2. DNA gyrase 3. Beta-lactamase 4. Clavulanate 5. Di-hydrogen oxide

26 The safest oral antibiotic to use at any stage of pregnancy is: 1. Tetracycline 2. Amoxicillin 3. Doxycycline 4. Ciprofloxacin 5. Sulfasoxazole/trimethoprim

27 My Numero Uno Antibiotic of Choice: The Envelope Please

28 Augmentin Indications/Dosage forms Indications: Preseptal cellulitis Dacryocystitis Pediatric Hemophilus Dosage forms: 500 or 875mg tablets BID 125 or 250mg/5cc pediatric suspension

29 Your 7 y/o patient with pre-septal cellulitis is allergic to penicillin-you would give them: 1. Amoxacillin 2. Azithromycin 3. Cephalexin 4. Erythromycin 5. Cephradine

30 But Doctor, I m Allergic to Penicillin

31 15 Y/O female presents with mom-c/o red eye-simple Right?? Has seen one nurse practitioner Has seen Two Optometrists Tx with Ciloxan Tx with Tobradex Mom wonders why nobody can cure her daughter

32 Zithromax Azithromcin Broad spectrum activity 68 hour 1/2 life DOC in penicillin sensitive patients Effective in pediatric Hemophilus Mild-medium GI side effects Excellent compliance (5 day TX) (1 day for chlamydia) Moderate cost Drug Interactions??

33 Marginal Blepharitis and the STAR TREK PARADOX IN THE 25TH CENTURY YOU CAN.. TRAVEL FASTER THAN THE SPEED OF LIGHT.. TRANSPORT INSTANTLY 1000 S OF MILES... CURE ANY DISEASE, BUT UNFORTUNATELY..

34 Lid Hygiene-Make it easy for the patient

35 And for infection which OINTMENT would you like Patients hate ointments Patients stop doing what they hate Ointments have poor pharmacokinetics Use a drop Pulse therapy with Ciloxan BID X 2 weeks will reduce S. epi to normal levels

36 Staph epidemidis DOES NOT produce exotoxins, but it does produce a complex organic molecule: OH-POO=POO

37 Staph POO POO Metabolize lipids to fatty acids Fatty acids = Staph Poopy Produce inflammatory response Don t use Steroids-a short term cure for a chronic disease.. Use...

38 The Indirect Antiinflammatory Agent

39 DOXYCYCLINE Long acting/potent tetracycline Resistant to absorption problems Medium GI upset Good compliance (1-2 X/D dosing) No activity in acute bacterial eye disease Inexpensive Contraindicated in kids and pregnant patients

40 Doxycycline Indications/Dosage forms Indications: Back-up drug for Chlamydia Acne rosaceae/chronic Staph blepharitis Dosage forms: 50 and 100mg tablets/capsules 25mg/5ml suspension

41 Does this Look Like a Steroid?

42 RESULTS: Doxycycline significantly decreased IL-1beta bioactivity in the supernatants from LPS-treated corneal epithelial cultures. These effects were comparable to those induced by the corticosteroid, CONCLUSIONS: Doxycycline can suppress the steady state amounts of mrna and protein of IL-beta and decrease the bioactivity of this major inflammatory cytokine. These data may partially explain the clinically observed anti-inflammatory properties of doxycycline. The observation that doxycycline was equally potent as a corticosteroid, combined with the relative absence of adverse effects, makes it a potent drug for a wide spectrum of ocular surface inflammatory diseases.

43 Viral conjunctivitis is the #1 Cause of Acute INFECTIOUS Conjunctivitis

44 Viral Pathogens Adenoviral Herpes simplex Herpes zoster

45 Adenoviral Signs Follicular conjunctivitis- Variable most common in lower fornix Mild to moderate chemosis Lid swelling with mild ptosis Lymphadenopathy in 66%

46 EKC SIGNS Papillary response of upper tarsal conj. Subconj. Heme Pseudomembrane and conjunctival scarring-severe form Subepithelial infiltrates-severe form

47 Is there a Cure for the Common Cold of the eye? Spit and swish Don t spare the steroids

48 Herpes Simplex Primary disease Recurrent disease Conjunctivitis Keratitis Stromal disease Kerato-uveitis

49 Antiviral Agents IDU Vidarabine Trifluridine Acyclovir Famcyclovir Valcyclovir Ganciclovir (ZIRGAN)

50 Trifluorothymidine THE drug of choice for topical management of Herpes simplex ocular disease. Rapid absorption Toxicity occurs when used over 21 days Dosage-5-8X daily Viroptic 1%-7.5cc-Burroughs

51 Herpes Zoster Commonly called shingles Lesions HONOR the mid-line Reoccurrence triggered by decreased immunity- MUST consider cause of reoccurrence

52 Who gets Post-herpetic Neuralgia Immunocompromised folk The elderly Best treatment is prophylactic TX

53 Chronic neural pain-a different kind of animal

54 Neurontin: The New Big Dog for chronic pain Huge dosage range: mg/d Must start slow Must give enough

55 Manage Potential Postherpetic Neuralgia Oral acyclovir 800mg 5X daily Valacyclovir 1000mg TID Famcyclovir 500mg TID Zostrix creme 3-4 times daily Low dose tricyclic antidepressantamitryptyline 25mg/day Neurontin

56 Allergy Update

57 Allergy, So What? What s the big Deal?? Financially it IS a BIG DEAL! Billions of lost productivity Billions on treatments Lost revenue on CL fits Extra chair time Allergy is not a problem, it is an opportunity-a disease that never goes away can be classified as a CHRONIC condition or as...

58 AN ANNUITY

59 THE TRICK TO SUCCESSFUL MANAGEMENT OF A CHRONIC ILLNESS? THE PATIENT MUST KNOW THEY CAN T BE CURED THE DOCTOR MUST KNOW THAT THEY CANNOT CURE THE PATIENT STAGE THE DISEASE PICK A TREATMENT THAT FITS THE LEVEL OF DISEASE BE AGGRESSIVE WHEN NECCESSARY

60 So, What s New? Better understanding of immune mechanisms User friendly, multi-tasking drugs Safer, more effective therapy Better understanding of disease means better patient counseling

61 THE MAJOR PLAYERS 1 Histamine: Immediate hypersensitivity reaction; Itching, swelling and hyperemia Primarily seen in seasonal allergy No permanent tissue damage-minimal inflammation except in extreme cases

62 THE MAJOR PLAYERS 2 Eosinophils-Nasty little WBC s full of ACID (Major basic protein) Attracted by release of PAF (platelet activating factor) and ECF (Eosinophilic chemotactic factor) Produce permanent tissue changes seen in VKC and GPC

63 THE MAJOR PLAYERS 3 PRODUCTS OF ARACHNODONIC ACID DERIVED FROM THE MAST CELL MEMBRANE PROSTAGLANDINS LEUKOTRIENES STIMULATE LATE PHASE T-CELL RESPONSE SEEN IN AKC AND GPC

64 ASK YOURSELF THE FOLLOWING QUESTIONS What am I treating-a histamine response or an inflammatory response? What is the severity (stage ) of the disease? What do I start treatment with and what is the best maintenance therapy?

65 NSAIDS AND ALLERGY 1/2 WAY IS NO WAY NSAIDS block production of prostaglandins, not leukotrienes May shift inflammation to leukotriene pathway Good analgesic, poor ant-inflammatory effect Corneal infiltrates Corneal melting??

66 IT DOES IT ALL -SAFELY?- Extremely effective Anti-inflammatory Cures everybody Fewer side-effects- soft steroid How long do I use it for?? Maintenance drug??

67 Oral antihistamines should be avoided in contact lens patient due to their side-effects 1. Parasympathetic 2. Cholinergic 3. Parasympatholytic 4. Anticholinergic 5. Sympathetic

68 WAIT, YOU FORGOT THE ORALS Just hold your pants Dog Breath Never TX systemically when topical therapy is safer and more effective Anticholinergic is a bad word

69 ARE THERE TOPICALS BESIDES THE EYE DROPS YES OH HAIRY NOSED ONE Do what allergists do Nasal sprays before orals Mast cell inhibitors or long acting steroids Safe Effective Synergistic with eye drops Safer than orals

70 THE PHARMACOLOGY OF GLAUCOMA-The New Paradigm User Friendly is in

71 PILOCARPINE IS NEW?? NOT QUITE, BUT IS DOC FOR A SPECIAL GLAUCOMA DOC FOR PIGMENTARY GLAUCOMA SURGICAL TX IS LASER IRIDOTOMY

72 To be considered effective, pilocarpine must lower the IOP in pigmentary glaucoma patients by at least: 1. 15% 2. 20% 3. 25% 4. 30%

73 Pilocarpine-A QID Drug? I DON T THINK SO Go low and go slow- Pilostarter packs from Ciba BID dose-in combination with other meds Lid closure increases absorption

74 AND STILL CHAMPION-THE BETA-BLOCKERS Peak flow testing is IN -standard of care-only objective test of lung function Check pulse and BP Betoptic S-less affect on pulmonary function-also less efficacy-use it and the lawyers will hate you

75 Alphagan P-Alpha-2 specificity makes for a better drug Alpha-2 Specific No tachyphylaxis Reduced allergy BID dosage??? Beta blocker equivalent Good choice for pulmonary compromised patients Neuroprotective? Not in humans yet

76 Prostaglandins-Wonder Drug!! Yes, But.. Lowers IOP up to 33% Produces red eye and darkens the iris HA, Herpes, CME, IRITIS Use Travatan Z

77 CAI Contraindications Sulfonamide sensitivity Sickle cell disease Pregnancy Liver/kidney disease Aplastic anemia risk Quality of life issues

78 Topical CAI s -Wonder Drug or Wonder DUD -Trusopt- WHEN it works it works real good When it fails it fails real bad A HOT and COLD drug Should you order CBC before use??

79 Azopt VS Trusopt Remember your pharmacokinetics!!!! Stinging solution VS no sting suspension Equal efficacy and dosage Azopt is BID Trusopt is TID CAI s best with prostaglandins

80 A MARRIAGE MADE IN HEAVEN (Or in the Sales Department) Timoptic + Trusopt = Cosopt LESS effective than separate dosing CAI underdosed B-blocker overdosed

81 REASONS FOR TREATMENT FAILURE Adverse drug effects/ contraindications Too many drugs Efficacy

82 THE NEW GLAUCOMA PARADIGM FRONT LINE DRUGS Beta blockers-still cost effective Betoptic/ a better B-Blocker?? Xalatan-Look up in the sky, it s a bird, it s a plane, no it s... Alphagan-Beta blocker efficacy, minimal systemic SE s, reduced allergy and tachyphylaxis

83 The Bridesmaids Non selectivebeta blockers Topical CAI s Pilocarpine-YES PILOCARPINE Epinephrine-LEFT AT THE ALTER-No real place in today s Tx strategies

84 KILLER COMBINATIONS Prostaglandin alone: So effective it rarely needs help Prostaglandin + BB: q AM BB and Prostaglandin HS-What could be easier? Prostaglandin + Alphagan: Alphagan BID and prostaglandin HS-A heavy lifting combo with few systemic SE s