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136 Kenilworth Avenue North, Hamilton, Ontario, L8H 4R8 Toll Free: 1-888-776-7776 www.sclerodermaontario.ca Medication Guide for Scleroderma Although there isn’t a cure for scleroderma there are effective treatment options that help alleviate symptoms and slow down disease progression. Current prescription and over-thecounter medication are designed to treat scleroderma by targeting: 1) inflammation, 2) autoimmunity, 3) vascular disease, and 4) tissue fibrosis. As a medical doctor or health care professional caring for persons with scleroderma, it is important to ensure patients understand the nature of the medications they may be prescribed and how they work to help control disease symptoms from progressing. Patient knowledge is powerful, as it reduces fear and increases compliance, resulting in a higher percentage of successful treatment. The following list of medication, commonly prescribed by doctors to treat patients with scleroderma, has been compiled, in thanks, by the Scleroderma Foundation. The list is provided for informational purposes only, and is not to be taken as an endorsement of any drug by the Scleroderma Society of Ontario or its Medical Advisory Board. Many of these drugs are prescribed by doctors, but have not been proven useful and should be used only with caution and supervision. It is important to consider, that not every medication is appropriate for every patient. As a medical doctor familiar with your patient's medical history, health status and disease progression, you will be able to determine the most appropriate treatment options. Scleroderma Medications Guide Raynaud's Phenomenon Calcium Channel Blockers nifedipine (Procardia®, Adalat®) amlodopine (Norvasc®) isradipine (Dynacirc®) diltiazem (Cardizem®, Dilacor XR®) nicardipine (Cardene®) nisoldipine (Sular®) felodipine (Plendil®) Angiotensin II Receptor Antagonists losartan (Cozaar®) valsartan (Diovan®) Action Relax blood vessels Most Common Side Effects Low blood pressure, constipation, nausea, may worsen swallowing difficulty, light-headedness, headache, leg edema, palpitations, irregular heartbeats Action Most Common Side Effects Block constriction Diarrhea, dizziness, cough, muscle of blood vessels pain http://www.sclerodermaontario.ca/Medication_Guide_For_Scleroderma.html 136 Kenilworth Avenue North, Hamilton, Ontario, L8H 4R8 Toll Free: 1-888-776-7776 www.sclerodermaontario.ca Others prazosin (Minipress®) doxazosin (Cardura®) Action Relax blood vessels Most Common Side Effects Low blood pressure pentoxifylline (Trental®) Unclear Nausea, dizziness Gastrointestinal Symptoms Gastroesophageal Reflux Disease (GERD) Antacids Action Most Common Side Effects Gaviscon, Maalox, Mylanta, Rolaids, Neutralize Diarrhea, constipation Tums stomach acidity H-2 Blockers Action Most Common Side Effects cimetidine (Tagamet®) Inhibit stomach Mental confusion (cimetidine only), ranitidine (Zantac®) acid secretion diarrhea, headache, dizziness famotidine (Pepcid®) nizatidine (Axid®) Proton Pump Inhibitors Action Most Common Side Effects omeprazole (Prilosec®) Inhibit stomach Diarrhea, headache, dizziness lansoprazole (Prevacid®) acid secretion esomeprazole (Nexium®) rabeprazole (Aciphex®) pantoprazole (Protonix®) Others Action Most Common Side Effects sucralfate (Carafate®) Coat esophagus & Constipation stomach; forms protective barrier Gastrointestinal Symptoms Improve Swallowing GI Stimulants Action Most Common Side Effects bethanecol (Urecholine®) Stimulate intestinal Abdominal cramping, diarrhea, metoclopramide(Reglan®) muscle dizziness, headache, drowsiness contractions, may (Reglan only) improve heartburn erythromycin Gastric irritation, nausea Can be helpful in octreotide acetate (Sandostatin®), an very severe cases Low heart rate, cardiac arrhythmias, injectable medication for improving the nausea, diarrhea, pain at injection motion of the site, expense http://www.sclerodermaontario.ca/Medication_Guide_For_Scleroderma.html 136 Kenilworth Avenue North, Hamilton, Ontario, L8H 4R8 Toll Free: 1-888-776-7776 www.sclerodermaontario.ca bowel Gastrointestinal Symptoms Relieve Constipation Bulking Agents calcium polycarbophil (FiberCon®, Fiberall®) psyllium (Metamucil®) Softening Agents docusate calcium (Surfak®, Sulfolax®) docusate sodium (Colace®) Others lactulose (Cephulac®, Cholac®) polyethylene glycol (MiraLax®) Action Soften stool Most Common Side Effects Abdominal bloating, flatulence Action Soften stool Most Common Side Effects Mild abdominal cramping Action Make bowels move Most Common Side Effects Abdominal cramping, flatulence Nausea, abdominal bloating, cramping, flatulence Gastrointestinal Symptoms Small Intestine Dysfunction: Bacterial Overgrowth/Diarrhea Broad Spectrum Antibiotic use is the mainstay of treatment for this complication. There are many potential approaches to this therapy. Example: Antibiotics are given in 2–3 week courses followed by a 1–2 week drug holiday. Generally a few cycles of this treatment can allow for quiet periods of a few months to a few years. However, some persons may require almost continuous antibiotics. Alternating antibiotics and increasing the antibiotic-free period will decrease the development of resistant strains of bacteria. Note: Prolonged use of Broad Spectrum Antibiotics may be complicated by superinfection. Broad Spectrum Antibiotics Action Most Common Side Effects Examples include: Decrease bacterial GI upset, diarrhea, nausea, and tetracycline overgrowth vomiting, prolonged use may be ampicillin complicated by superinfection metronidazole (Flagyl®) vancomycin, ciprofloxacin (Cipro®) amoxicillin/clavulanate (Augmentin®) clarithromycin (Biaxin®) azithromycin (Zithromax®) Joint & Tendon Pain Non-Steroidal Anti-Inflammatory Action Most Common Side Effects http://www.sclerodermaontario.ca/Medication_Guide_For_Scleroderma.html 136 Kenilworth Avenue North, Hamilton, Ontario, L8H 4R8 Toll Free: 1-888-776-7776 www.sclerodermaontario.ca Drugs (NSAIDs) flurbiprofen (Ansaid®) fenoprofen (Nalfon®) nabumeton (Relafen®) diclofenac (Voltaren®, Cataflam®) diclofenac & misoprostol (Arthrotec®) diclofenac sodium (Voltaren®) etodolac (Lodine®) ibuprofen (Motrin®, Advil®, Nuprin®) indomethacin (Indocin®) ketoprofen (Orudis®) ketorolac (Toradol®) meloxicam (Mobic®) naproxen (Naprosyn®, Anaprox®, Aleve®) oxaprozin (Daypro®) piroxicam (Feldene®) suldinac (Clinoril®) COX-2 Inhibitors celecoxib (Celebrex®) Suppress inflammation GI upset, stomach ulcers, impaired kidney function, liver inflammation, confusion Action Suppress inflammation Action Relieve pain Most Common Side Effects Headache, edema, rash Analgesics acetaminophen (Tylenol®) tramadol (Ultram®) Narcotics Action acetaminophen/propoxyphene Relieve severe (Darvocet-N®) pain acetaminophen/hydrocone (Vicodin®) acetaminophen/oxycodone (Percocet®) oxycodone hydrochloride (OxyContin®, OxyIR®) Most Common Side Effects Risk of liver & kidney damage Esophagus irritation & sedation Most Common Side Effects Addiction possible, constipation, dizziness, drowsiness, nausea, vomiting Sedation, low blood pressure, nausea, vomiting Pulmonary Fibrosis/Alveolitis Immunosuppressants Action Most Common Side Effects http://www.sclerodermaontario.ca/Medication_Guide_For_Scleroderma.html 136 Kenilworth Avenue North, Hamilton, Ontario, L8H 4R8 Toll Free: 1-888-776-7776 www.sclerodermaontario.ca (none proven in controlled trials; the following have been used) cyclophosphamide (Cytoxan®) azathioprine (Imuran®) cyclosporine (Neoral®, Sandimmune®) mycophenolate mofetil (Cellcept®) Suppress immune Bone marrow damage, hair loss, response nausea, diarrhea, bladder inflammation, increased cancer risk, increased infection Suppress immune response Nausea, pancreatitis, increased infection, increased cancer risk, Impair anemia lymphocytes Tremor, headache, hypertension, nausea, vomiting, kidney & liver injury, Impair infections lymphocytes Tremor, headache, hypertension, chest pain, GI hemorrhage, nausea, vomiting, anemia, fever, infection, sepsis, leg edema Pulmonary Arterial Hypertension Patients diagnosed with pulmonary arterial hypertension should be referred to a pulmonary hypertension center for experienced evaluation and management of this serious scleroderma complication. Endothelin Receptor Antagonists Action Most Common Side Effects ambrisentan (Letairis®) Act on blood Edema, and birth defects vessels bosentan (Tracleer®) Potential liver injury, headache, Act on blood flushing, edema, anemia, male vessels infertility, birth defects Prostaglandin Derivatives Action Most Common Side Effects epoprostenol (Flolan®) Act on blood Headache, flushing, jaw pain, vessels diarrhea, foot/bone pain, potential serious infection associated with central line catheter in the chest wall Flushing, increased cough, low blood Act on blood pressure, headaches, nausea, spasm iloprost (Ventavis®) inhalation vessels of jaw muscles, fainting http://www.sclerodermaontario.ca/Medication_Guide_For_Scleroderma.html 136 Kenilworth Avenue North, Hamilton, Ontario, L8H 4R8 Toll Free: 1-888-776-7776 www.sclerodermaontario.ca solution Act on blood vessels trepostinil (Remodulin®) Calcium Channel Blockers Action Can be helpful to a small proportion of See Raynaud's patients; see Raynaud’s section section Phosphodiesterase Type 5 (PDE5) Action Inhibitor sildenafil citrate (Revatio®) Act on blood vessels tadalafil (Adcirca®) Act on blood vessels Renal Crisis/New Onset Hypertension ACE Inhibitors Action captopril (Capoten®) Block constriction enalapril (Vasotec®) of blood vessels lisinipril (Prinivil®, Zestril®) quinapril (Accupril®) ramipril (Altace®) fosinopril (Monopril®) benazopril (Lotensin®) moexipril (Univasc®) trandolapril (Mavik®) Headache, flushing, pain at infusion site Most Common Side Effects See Raynaud's section Most Common Side Effects headache, dyspepsia, flushing, nosebleeds, insomnia headache, stomach upset, back pain, muscle pain, nasal stuffiness, flushing, pain in arms or legs, dizziness, or vision change Most Common Side Effects Skin rash, dry mouth, taste disturbances, fluid retention, drowsiness, light-headedness, diarrhea, cough If taking corticosteroids, monitor your blood pressure frequently, and report changes to your healthcare provider immediately. http://www.sclerodermaontario.ca/Medication_Guide_For_Scleroderma.html 136 Kenilworth Avenue North, Hamilton, Ontario, L8H 4R8 Toll Free: 1-888-776-7776 www.sclerodermaontario.ca Warning About Corticosteroids and Renal Crisis Corticosteroids, such as prednisone and medrol, have been used to treat several complications of systemic scleroderma, such as pulmonary fibrosis, pruritis (itchy skin), and joint pain. Recent findings indicate that corticosteroids can be implicated in precipitating renal crisis. Therefore, the medical community has concluded corticosteroids should be used cautiously, in a carefully screened patient population. For example: to manage patients who also have myositis (muscle inflammation). Anyone taking corticosteroids should monitor blood pressure frequently, and report changes to the healthcare provider immediately. Skin Fibrosis Immunosuppressants (none proven in controlled trials; the following have been used) cyclophosphamide (Cytoxan®) cyclosporine (Neoral®), Sandimmune®) D-penicillamine (Cuprimine®, Depen®) methotrexate (Rheumatrex®, Trexall®) mycophenolate mofetil (Cellcept®) Action Most Common Side Effects Suppress immune Bone marrow damage, hair loss, response nausea, diarrhea, bladder inflammation, increased cancer risk, Impair increased infections lymphocytes Tremor, headache, hypertension, nausea, vomiting, kidney & liver injury, May inhibit infections collagen crossBone marrow damage (rare), kidney linking damage, mouth sores, skin rash, Suppress immune nausea, diarrhea response Liver inflammation, nausea, mouth Impair sores, skin rash lymphocytes Tremor, headache, hypertension, chest pain, GI hemorrhage, nausea, vomiting, anemia, fever, infection, sepsis, leg edema Sjögren's Syndrome Prescription Drugs Action pilocarpine hydrochloride (Salagen®) Improves dry mouth symptoms in patients with Sjögren’s Most Common Side Effects Dizziness, headache, flushing, urinary frequency, nausea, sweating, hypertension, tachycardia http://www.sclerodermaontario.ca/Medication_Guide_For_Scleroderma.html 136 Kenilworth Avenue North, Hamilton, Ontario, L8H 4R8 Toll Free: 1-888-776-7776 www.sclerodermaontario.ca cevimeline hydrochloride (Evoxac®) Over-the-Counter Products Dry Mouth: Salivart® Biotene Oral Balance Moisturizing Gel® Biotene Dry Mouth Gum® Biotene Dry Mouth Toothpaste® Biotene Dry Mouth Mouthwash® Optimoist® Salix Lozenges® Dry Eyes: Artificial tears® Action Headache, rhinitis, diarrhea, nausea, sweating, urinary frequency Most Common Side Effects Saliva substitute, No significant side effects observed alleviate dry mouth Provide tear-like lubrication Mild stinging, temporary blurred vision Action Most Common Side Effects Reactive Depression Selective Serotonin Reuptake Inhibitors (SSRI's) sertraline (Zoloft®) paroxetine (Paxil®) fluoxetine (Prozac®) fluvoxamine (Luvox®) Tricyclic Antidepressants amitriptyline (Elavil®) nortriptyline (Pamelor®) imipramine (Tofranil®) clomipramine (Anafranil®) Other Treatments bupropion (Wellbutrin®) venlafaxine (Effexor®) nefazodone (Serzone®) Improve symptoms Headache,insomnia, sleepiness, of depression and nervousness, diarrhea, nausea, peripheral pain; constipation (Paxil® only) Prozac may also improve Raynaud's Action Most Common Side Effects Improve symptoms Drowsiness, dry mouth, blurred vision, of depression, may orthostatic hypotension, weight gain, improve restorativeconstipation sleep Action Most Common Side Effects Improve symptoms Headache, insomnia, dry mouth, high of depression blood pressure, nausea Improve depression http://www.sclerodermaontario.ca/Medication_Guide_For_Scleroderma.html 136 Kenilworth Avenue North, Hamilton, Ontario, L8H 4R8 Toll Free: 1-888-776-7776 www.sclerodermaontario.ca trazadone (Desyrel®) May improve depression-related insomnia Sedation, nausea, orthostatic hypotension Localized Scleroderma Medications (none proven in controlled trials; the following have been used) hydroxychloroquine sulfate (Plaquenil®) methotrexate (Rheumatrex®, Trexall®) Action Most Common Side Effects Unclear prednisone (Deltasone®, Cortan®) Seizures, leukopenia, thrombocytopenia Suppress immune Liver inflammation, nausea, mouth response sores, skin rash Suppress Fluid retention, GI irritation inflammation phenytoin (Dilantin®) Unclear potassium p-aminobenzoate (POTABA®) Unclear D-penicillamine (Cuprimine®, Depen®) May inhibit collagen crosslinking Decrease skin thickening PUVA (phototherapy) Dizziness, confusion, nausea, vomiting Skin rash, nausea, diarrhea Bone marrow damage (rare), kidney damage, mouth sores, skin rash, nausea, diarrhea Burning, itching, nausea, skin aging Skin Itching (Pruritis)/Dryness To relieve dry itchy skin, it is necessary to moisturize often. Also, you must protect your skin from harsh detergents, hot water, and the cold winter air, all of which will rob moisture from your skin. You may want to consider using a humidifier in the home during the cold winter heating months to replace much-needed moisture into the air. Remember that not everyone will have the same response to every product. You may have to try a few products until you find one that will work for you. Over-the-Counter Skin Lotions Action Most Common Side Effects KeriCream® Moisturize skin No significant side effects observed Lanalor® Lubriderm® http://www.sclerodermaontario.ca/Medication_Guide_For_Scleroderma.html 136 Kenilworth Avenue North, Hamilton, Ontario, L8H 4R8 Toll Free: 1-888-776-7776 www.sclerodermaontario.ca Eucerin Moisturizing® creams and lotions Nivea Moisturizing® UltraDerm® Alpha Keri Bath Oil® Penederm alpha hydroxy cream® Aveeno bath oil & moisturizer® Antihistamines (Prescription) diphenhydramine (Benadryl®) hydroxyzine (Atarax®) Colchicine Action Most Common Side Effects Block histamine Drowsiness, dry mouth response, thereby decreasing itching Reduce inflammation associated with Diarrhea calcinosis To learn more about prescription and over-the-counter medication as well as new medications, supplements and herbal remedies not listed in the table above, the U.S. National Library of Medicine National Institutes of Health has developed the "MedlinePlus" web-site, which can be found at: ww.nlm.nih.gov/medlineplus/druginformation.html http://www.sclerodermaontario.ca/Medication_Guide_For_Scleroderma.html