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Objectives

Objectives.

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Objectives

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    1. Transdermal Pain Management Courtney Yee, Pharm.D. Apothecary Shops of Arizona Introduce topicIntroduce topic

    2. Objectives • Introduction to compounding pharmacies • Describe the benefits of transdermal pain management • Discuss specific medications for use in transdermal gels • Discuss specific formulas for different conditions

    3. Com•pound•ing, v. 1. The custom-making of medications by a pharmacist on the prescription order of a physician. Compounding is the traditional method of preparing customized medications to help meet unique physician and patient needs. It’s our goal as Compounding pharmacists to provide innovative patient care. This may involve compounding a preservative free eye drop in a sterile compounding lab, making an injection for impotency, preparing medications for veterinarians, or providing natural hormone replacement therapy. compounding pharmacist’s ultimate goal in preparing customized medications is to help the physician and patient achieve a more positive therapeutic outcome. Compounding is the traditional method of preparing customized medications to help meet unique physician and patient needs. It’s our goal as Compounding pharmacists to provide innovative patient care. This may involve compounding a preservative free eye drop in a sterile compounding lab, making an injection for impotency, preparing medications for veterinarians, or providing natural hormone replacement therapy. compounding pharmacist’s ultimate goal in preparing customized medications is to help the physician and patient achieve a more positive therapeutic outcome.

    4. The Paradox By going back to the ancient art, modern compounding offers the freedom & flexibility of more therapeutic options to choose from. Compounding allows you to do what your colleagues were able to do 100 years ago – customize the medicine to each individual patients exact needs. Today, you amazing high-tech, bio-tech diagnostic equipment to allow you to hone in on the exact diagnosis and then when it comes to treating that exact diagnosis, your restricted to the medication typically being available only in 1 or 2 strengths and only in tablets. So now you have to fit the patient to the closest medication, instead of the exact medication at the exact dose, in the best dosage form available.Compounding allows you to do what your colleagues were able to do 100 years ago – customize the medicine to each individual patients exact needs. Today, you amazing high-tech, bio-tech diagnostic equipment to allow you to hone in on the exact diagnosis and then when it comes to treating that exact diagnosis, your restricted to the medication typically being available only in 1 or 2 strengths and only in tablets. So now you have to fit the patient to the closest medication, instead of the exact medication at the exact dose, in the best dosage form available.

    5. Compounding allows you to: Prescribe what is BEST for each individual patient Not just what is COMMERCIALLY AVAILABLE for your patient.

    6. Goals of Transdermal Therapy To deliver local concentrations of medication higher than possible through the oral or parenteral routes Reduce side effects and drug interactions through avoidance of systemic absorption and renal/hepatic exposure Higher concentrations Fewer side effects Higher concentrations Fewer side effects

    7. Transdermal Advantages Little to no GI upset with NSAIDS Local action, site specific Easy to titrate to individual patient Fast onset of action High drug concentrations in the tissue that requires analgesia GI upset history of PUD, GERD, elderly Gastric bypass – Dr. Blackstone storyGI upset history of PUD, GERD, elderly Gastric bypass – Dr. Blackstone story

    8. Pain medications used in transdermal preparations Ketoprofen Ibuprofen Lidocaine Cyclobenzaprine Guaifenesin Ketamine Diclofenac Amitriptyline Carbamazepine Gabapentin Clonidine Nifedepine Baclofen Morphine Also, medications are not new to anyone…they are medications that are widely used in other forms such as IV or PO.Also, medications are not new to anyone…they are medications that are widely used in other forms such as IV or PO.

    9. Anti-inflammatory Agents Inhibit Prostaglandin synthesis Decrease sensitivity of vessels to bradykinin and histamine Ketoprofen (10-20%) Diclofenac (2-5%) Ibuprofen (10-20%) Piroxicam (0.5-3%) The NSAIDS inhibit prostaglandin synthetase which prevents the conversion of PGG2 and PGH2 to PGE2 and PGF2alpha which are responsible for pain and vasodilation. The NSAIDS inhibit prostaglandin synthetase which prevents the conversion of PGG2 and PGH2 to PGE2 and PGF2alpha which are responsible for pain and vasodilation.

    10. Muscle Relaxants/Spasmolytics Baclofen (2-5%) Cyclobenzaprine (1-4%) Structurally related to TCA May also act as NMDA partial agonist, NE and 5-HT reuptake inhibitor Guaifenesin (10%) Depresses or blocks nerve impulse transmission

    11. Local Anesthetics Prevent generation and conduction of nerve impulses Lidocaine 2-10% Tetracaine 2-10 % Bupivicaine 0.5-0.75 % Act by preventing both the generation and conduction of nerve impulses by reducing or preventing large transient increases in the permeability of the membrane to sodium ions. The blockade of sodium channels by these agents blocks nociceptive transmission, interupts sympathetic reflexes and prevents increased skeletal muscle activity – which helps relieve painAct by preventing both the generation and conduction of nerve impulses by reducing or preventing large transient increases in the permeability of the membrane to sodium ions. The blockade of sodium channels by these agents blocks nociceptive transmission, interupts sympathetic reflexes and prevents increased skeletal muscle activity – which helps relieve pain

    12. Local Pain Problems That Can be Solved: Inflammation Muscle spasms Chronic Back Pain Neuropathy Plantar Fasciitis Tendonitis Carpal Tunnel RSD

    13. Evidence Based Medicine Quantitative systematic review of topically applied NSAID’s BMJ, Jan 31, 1998 86 randomized, controlled trials 10,160 patients

    14. BMJ Review Conclusions: “Topical NSAIDs are effective in relieving pain in acute and chronic conditions” “Adverse events & withdrawal from the studies related to the drug had a low incidence and were no different from placebo.” The study shows the results were exactly what was expected…local efficacy with little side effectThe study shows the results were exactly what was expected…local efficacy with little side effect

    15. More Evidence of Safety of Transdermal NSAIDs BMJ Post-Marketing Survey 23,590 pts using topical NSAIDs 6 cases of definite or probable adverse GI events (BMJ 1995;311:22-6) BlackstoneBlackstone

    16. Kinetics Explains Safety Oral Ketoprofen ?? 60% bioavailabilty vs Transdermal ?? <5% bioavailability Pharmacokinetics of Ketoprofen in man after repeated percutaneous administration Arzneimeittelforshung, 1989;39 7:812-815

    17. Kinetics Explains Local Efficacy “Application of ketoprofen to knee of pts about to undergo knee surgery showed ketoprofen concentrations 100 times greater in: synovial fluid, intra-articular adipose tissue, and capsular tissue than in the blood. Antirheumatic Drug Concentrations in Human Synovial Fluid and Synovial Tissue Clin Pharmacokinetics 8:496-522(1983)

    18. Formulas for Inflammation: Ketoprofen Gel 10-20% in PLO 4% with DMSO/n-decylmethylsulfoxide Ketoprofen/Lidocaine Gel 20/10 in PLO 4%/2% with DMSO/n-decylmethylsulfoxide KICK Gel Diclofenac, piroxicam – longer actingDiclofenac, piroxicam – longer acting

    19. Formulas for Muscle Spasms Ketoprofen/baclofen Gel Baclofen 2-5% 4%/2% with DMSO/N-decylmethylsulfoxide Ketoprofen/guaifenesin Gel Guaifenesin 10%

    20. Formulas for Neuropathy NeuroGel Ketoprofen 20% Amitriptyline 5% Carbamazepine 2% Diabetic Neuropathy Add nifedipine 2% KetoGabaClon Gel Ketoprofen 20% Gabapentin 6% Clonidine 0.2% KetaGabaClon Gel Ketamine 10% Nifedipine - non-NMDA calcium channel blocker Provides direct vasodilatory effect on vessels, nerve conduction, hypoxic resistance and capillary density additive protective effect of topical ketamine and nifedipine in combinationNifedipine - non-NMDA calcium channel blocker Provides direct vasodilatory effect on vessels, nerve conduction, hypoxic resistance and capillary density additive protective effect of topical ketamine and nifedipine in combination

    21. Transdermal Drug Delivery: A More Conservative Approach Lower doses being used Drugs being delivered to site of action Fewer side-effects Fewer drug interactions Better/Faster efficacy

    22. Keys to Positive Outcomes Multiple ingredients with complementary modes of action NMDA antagonist, glutamate/AMPA antagonist, alpha-2 or GABA-b agonist Base that is penetration enhancing PLO, Lipoderm Evaluation Apply at 6-8 hour intervals and up to every 2 hours as needed in between Additional medication with different modes of action can be added within 1-2 weeks and dose escalation and evaluation should be repeatedApply at 6-8 hour intervals and up to every 2 hours as needed in between Additional medication with different modes of action can be added within 1-2 weeks and dose escalation and evaluation should be repeated

    23. The Bottom Line: Compounding can be a cost-effective key to solving many common problems as well as individualizing a patient’s therapy.

    24. Contact Information Apothecary Shop of Scottsdale 9777 N 91st Street #102 Scottsdale, AZ 85258 Pharmacy 480-451-3771 Fax 480-451-3503

    25. Thank You Thanks to doctor ____ for inviting me to speak.Thanks to doctor ____ for inviting me to speak.

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