Pharmacology Overview by Drug Class Dr Andrew P Mallon Learning Objectives Recognize frequently prescribed drugs Identify brand/generic names, drug families, common indications, and common side effects Describe some legal issues with OTCs and prescription drugs (federal and state) How a drug goes to market FDA estimates average time for drug approval is 8.5 years Patents last 20 years Exclusivity, lasts 3-7 years, designed by FDA to promote balance between new drug innovation and generic competition. http://www.fda.gov/cder/handbook/develop.htm Certain drugs can be fast-tracked if there is a great need Gastrointestinal: Acid Reducers “Acid Reducers all OTC?” Switched to OTC when “safe without MD advice” Long term or short term use Know when to seek medical attention Gastrointestinal: Acid Reducers Proton Pump Inhibitors H2 Receptor antagonists Omeprazole = Prilosec OTC Lansoprazole = Prevacid Pantoprazole = Protonix Esomeprazole = Nexium Rabeprazole = AcipHex Ranitidine = Zantac OTC Famotidine = Pepcid OTC Side Effects rare Cardiovascular: Statins “What statin are you taking?” Highest use drugs Diet control should accompany drug therapy Debatable difference between drugs BUT switch if not effective Expect long term use Cardiovascular: “statins” Cholesterol Lowering Atorvastatin = Lipitor Fluvastatin = Lescol Lovastatin = Mevacor Simvastatin = Zocor Pravastatin = Pravachol Rosuvastatin = Crestor Side Effects: few overall, muscle aches, weakness Cardiovascular: Beta blockers “Look, one more use for betablockers” Don’t stop taking abruptly Watch for low blood pressure symptoms (dizziness) Can decrease sexual ability Other uses: performance anxiety, essential tremor, Raynaud’s syndrome, migraine prophylaxis, esophagus bleeding in ESLD Cardiovascular: Beta Blockers, “olols” Hypertension (high blood pressure), Arrhythmias, Heart Failure, MI (Myocardial Infarction), etc. Metoprolol = Toprol XL, Lopressor Atenolol = Tenormin Propranolol = Inderal Carvedilol = Coreg Cardiovascular: “Heart-ache” drugs Digitalis: Heart Failure, A-fib Digoxin = Lanoxin Side effects: Dose dependent, nausea Nitrates: Angina Isosorbide Mononitrate = Imdur Nitroglycerin sublingual tablets Side effects: headache but can adapt Refill every 6 months - 1 year Cardiovascular: Anticoagulants “When to clot and when to not…” Hold prior to surgery then bridge therapy with low-molecular weight heparin Too much warfarin = Vitamin K Monitoring is vital to safety Avoid the term “blood thinner” Cardiovascular: Anticoagulants Use: blood clot prevention or decrease further development Warfarin = Coumadin Clopidogrel = Plavix Side effects: signs of bleeding/bruising Diet should be consistent regarding vitamin K content Cardiovascular: Diuretics “Latest study says add diuretics…” Dramatic increase in use of inexpensive drugs Effective to decrease blood volume and hence the pressure Cardiovascular: Diuretics Decrease excess inside water Hydrochlorothiazide = HCTZ, Hydrodiurel Furosemide = Lasix Triamterene/HCTZ= Maxzide, Dyazide Side effects: Nausea, photosensitivity, dizziness Low blood pressure Cardiovascular: ACE-I and ARBs Angiotensin constricts blood vessels ACE-Inhibitors = “-prils” Captopril = Capoten Lisinopril = Zestril/Prinivil Quinapril = Accupril Fosinopril = Monopril Perindopril = Aceon Side effects Enalapril = Vasotec Ramipril = Altace Benazepril = Lotensin Trandolapil = Mavik Moexipril = Univasc Cough, swollen tongue/lips, increased K+ Cardiovascular: ACE-I and ARBs Angiotensin Receptor Blockers (ARBs) Losartan = Cozaar Valsartan = Diovan Candesartan = Atacand Irbesartan = Avapro Olmesartan = Benicar Telmisartan = Micardis Eprosartan = Teveten Side effects Increased K+, little/no cough or angioedema Cardiovascular: ACE-I and ARBs Uses Diabetes - prevent progression to chronic kidney disease Heart failure - decreased stiffening of heart muscle Hypertension Cardiovascular: Hypertension “I feel fine, why treat high blood pressure?” Check blood pressure frequently Device accuracy: Arm cuff vs. finger device When to contact the physician Cardiovascular: Hypertension High Blood Pressure: Clonidine = Catapres Doxazosin = Cardura Amlodipine/Benazepril = Lotrel Side effects: dizziness, headache Respiratory: Allergies Antihistamines Cetirizine = Zyrtec OTC Fexofenadine = Allegra Loratadine = Claritin OTC Side Effects Drowsiness or stimulant Respiratory: “Allergies/Cold Sxs: What works?” Combinations with pseudoephedrine? Combinations with phenylephrine? Combinations with dextromethorphan effective? Chicken soup, water and rest? Hot Toddy? Pseudoephedrine scoop Effective decongestant Schedule III in Oregon All “EPP” products restricted by federal law Why? Precursor to methamphetamine Ephedrine No longer marketed Phenylpropanolamine (PPA) No longer marketed FDA proposed final rule to place PPA in Category III (not approved for use) regarding OTC products Pseudoephedrine Limited access by federal law Respiratory: Allergies Nasal Corticosteroids Fluticasone = Flonase Mometasone = Nasonex Side Effects Headache, bloody nose Concern regarding long term use? Respiratory: Asthma Inhalers “Rescue” Albuterol = Proair, Proventil Side effects: “Controllers” Fluticasone/Salmeterol = Advair Diskus Side effects: Increased heart rate, “jittery” Headache Thrush, voice changes Aero Chamber device for accurate administration Respiratory: Asthma Oral Medications Corticosteroids Prednisone Methylprednisolone Side effects: Insomnia, nervousness Nausea: Take With Food Long term use concern Montelukast = Singulair Side effects: rare Antibiotics: “The latest is the best! I want that one!” Side effects: Diarrhea Nausea Yeast infections Tips: New drug isn’t always best Resistance is inevitable--but we can delay it Take until gone With or w/o food variable Antibiotics: Penicillins & their relatives Penicillin VK Amoxicillin = Trimox Amoxicillin/Clavulanate = Augmentin Cephalexin = Keflex Cautions: Cross-sensitivities and allergies Can still be very effective even though “old drugs” Antibiotics: Azithromycin = Zithromax Doxycycline Cautions: Do not take with milk, antacids Sun sensitivity Trimethoprim/sulfamethoxazole = Cotrim, Septra, Bactrim Cautions: Sun sensitivity, Increase fluid intake, allergies Antibiotics: Quinolones Ciprofloxacin = Cipro Levofloxacin = Levaquin Cautions: Do not take with milk, antacids Sun sensitivity Moxifloxacin = Avelox Cautions: Do not take with milk, antacids Sun sensitivity CNS: Antidepressants “Let’s add them to the water” Frequently prescribed Long term or short term use Time to effect Switch to another if not effective Often taper off drug Okay for adolescents? Suicidal ideology? “Antidepressants a Suicide Risk for Young Adults Study Says Cases Double for Those 18 to 25 Using Medicine to Control Depression” Black box warning 2004 Washington Post 2006 FDA investigations 2007 Pediatric studies lacking CNS: Antidepressants SSRIs Fluoxetine = Prozac Sertraline = Zoloft Paroxetine = Paxil, Paxil CR Citalopram = Celexa Escitalopram = Lexapro Side effects: headache, nausea, insomnia or somnolence CNS: Antidepressants TCAs Amitriptyline = Elavil Side effects: sedation, dry mouth “Other” types Bupropion = Wellbutrin, Wellbutrin XL Venlafaxine = Effexor, Effexor XR Trazodone = Deseryl Side effects: dizziness, drowsiness CNS: Antianxiety and/or Insomnia “Popular” drugs Half-life varies Long - Diazepam Short - Triazolam Infrequent use extends effectiveness Caution in elderly CNS: Antianxiety and/or Insomnia Benzodiazepines Lorazepam = Ativan Clonazepam = Klonipin Diazepam = Valium Temazepam = Restoril Alprazolam = Xanax Side effects: drowsiness Insomnia Zolpidem = Ambien Side effects: headache CNS: Insomnia Ambien and it’s interesting side effects Sleepwalking Binge eating at night Nightmares How to interpret and advise patients: Take pill as you get into bed. Questions? Endocrine: Osteoporosis Alendronate = Fosamax Risedronate = Actonel Side Effects: Esophagitis, Nausea Once weekly dosing possible Raloxifene = Evista Side Effects: Hot flashes, Nausea CNS Antipsychotics Risperidone = Risperdal Side effects: agitation, insomnia Don’t stop abruptly Aripiprazole = Abilify Side effects: akathisia, HA, weakness Don’t confuse with PPI’s which also end in “prazole” CNS Anticonvulsant Gabapentin = Neurontin Pregabalin = Lyrica Side effects: dizziness, fatigue, nausea Used for nerve pain, etc Approved for fibromyalgia! Phenytoin = Dilantin Side effects: gingival hyperplasia Important to monitor drug levels Analgesic: Anti-inflammatory Ibuprofen = Motrin, Advil OTC Naproxen = Naprosyn, Anaprox OTC Side Effects: GI = take with food Dizziness? Caution with warfarin, history of ulcer/GERD Analgesic: Anti-inflammatory “The next generation or off the market?” Celecoxib = Celebrex Side Effects: GI (less)= take with food Vioxx = Rofecoxib (09/04 off market) Bextra = Valdecoxib (04/05 off market) Analgesic: Muscle Relaxants Cyclobenzaprine = Flexeril Effectiveness vs. gorkiness Carisoprodol = Soma Schedule IV in Oregon Side Effects: Dizziness, Drowsiness Dependence? Should it be a Scheduled drug? Do not take with alcohol Controlled Substances Schedules I - High potential for abuse and/or no medical use Heroin, LSD, mescaline II - Highest potential for abuse with medical use Opiate (eg, meperidine, codeine, morphine, oxycodone, methadone, cocaine) Non-opiate stimulants (eg, methylphenidate, amphetamine, phenmetrazine, methamphetamine) Non-opiate depressants (eg, barbiturates, methaqualone) CS Schedules - continued III - Narcotic combinations and others Up to 90 mg codeine per dose plus other active ingredients Hydrocodone plus APAP Doriden (glutethimide) Anabolic steroids (eg, methyltestosterone) Benzphetamine and phendimetrazine (Didex) Barbiturate suppositories Barbiturate combos (eg, Fiorinal, Fioricet with Codeine) Marinol Ephedrine, Pseudoephedrine, Phenylpropanolamine in Oregon CSA Schedules - continued IV - Primarily non-narcotics Benzodiazepines (eg, Valium, Halcion) Meprobamate Phenobarbital Chloral hydrate Phentermine, mazindol, diethylpropion Propoxyphene dosage forms (powder = CII) Dichloralphenazone (component of Midrin®) 9/01 Carisoprodol in OR CSA Schedules - continued V - “Exempt narcotics” Low dose combinations of codeine with other ingredients for diarrhea, pain, or cough -some may be sold OTC in other states Diphenoxylate with atropine Generally no more than 10 mg codeine per 5 mL (Tylenol w/ Codeine 12 mg/5mL) No OTC Schedule V in Oregon currently Analgesic: Narcotic Combinations Hydrocodone/APAP = Vicodin, Lortab Codeine/APAP = Tylenol #3 Propoxyphene/APAP = Darvocet Oxycodone/APAP = Percocet Side Effects: Dizziness, Drowsiness Constipation Dependence? Abuse? Do not take with alcohol Analgesic: Opioids “Abuse potential high yet effective” Oxycodone = Oxycontin Side effects: see previous slide High abuse potential due to extended release formulation Tramadol = Ultram Side Effects: Dizziness, Drowsiness Dependence? Abuse? Do not take with alcohol Analgesics: “Abuse vs. Legitimate Use?” Sickle cell anemia Fibromyalgia Terminal cancer Chronic back pain Muscular dystrophy Neuropathic pain ADD, ADHD How do you evaluate and help? Medical Marijuana Act Oregon Medical Marijuana Act ORS 475.300 475.346This Act allows use of marijuana by Oregonians with debilitating medical conditions for medical purposes determined by their physician. “Debilitating medical condition” includes glaucoma, cancer, HIV or AIDS, or a condition which produces cachexia, severe pain, severe nausea, seizures, persistent muscle spasms or condition approved by the department A medical registry identification card is required for the patient and caregiver A registrant may possess 6 mature plants and 24 ounces of usable marijuana at a time Death With Dignity Act Death With Dignity Act http://www.oregon.gov/DHS/ph/pas/index.shtmlOAR 333-009-0000 – 333-009-0030 ORS 127.800 – 127.897An adult, who is a resident of Oregon, has been determined by the attending physician and consulting physician to be suffering from a terminal disease. The adult must make an oral and written request to end their life. 15 days between oral request and written request Authorized prescribers include MD or DO Health care providers may choose not to participate See link for necessary reporting Endocrine: Estrogens “Estrogen replacement unnecessary?” How safe? How necessary? Risk vs. benefit 1970’s data and marketing campaign Women’s Health Initiative study Endocrine: Female Hormones Menopausal women Oral contraceptives Conjugated Estrogens = Premarin Conjugated Estrogens/ Medroxyprogesterone = Prempro Estradiol Medroxyprogesterone Ortho-Tricyclen Ortho-Novum Ortho-Evra (transdermal) Side effects: Breast tenderness, spotting Bloating, Nausea Plan B OTC August 2006 Without a prescription if >18yo Behind the counter at licensed pharmacies or healthcare facilities Pharmacist must be on duty but not necessary to make the transaction No gender distinction, no log required Patient must receive information, pharmacist must be available for questions http://www.fda.gov/cder/foi/label/2006/021045s011lbl.pdf Endocrine: Injectable Diabetic agents Insulin Rapid acting Short-acting Regular Intermediate acting Novolog, Humalog NPH Combination products Mixed insulin (70/30) Synthetic vs. animal source Endocrine: Diabetes Side Effects: Dose dependent Okay at room temperature once opened x 30days Roll before withdrawing dose, rotate sites, change syringes Scheduled pump option Endocrine: Oral Diabetic agents Rosiglitazone = Avandia Pioglitazone = Actos Side Effects: dose dependent Metformin = Glucophage Side Effects: dose dependent Glipizide ER Glyburide Endocrine: Diabetes “Avandia May Cause Risk of Heart Attack and Death” How relevant? Open display of results? Remove from market? Class effect? Do all glitazones cause this Would this happen anyway? Endocrine: Diabetes Start with oral therapy, progress to insulin if cannot control Diet control in tandem with drug therapy Diligent foot care, eye care, wound care Consistency http://www.diabetes.org/home.jsp Endocrine: Erectile Dysfunction Erectile Dysfunction Sildenafil = Viagra Side Effects: Nausea, Headache, Visual Tadalafil = Cialis Another indication: pulmonary hypertension Compounded preparations Endocrine: Erectile Dysfunction “Fastest growing drug class” Little blue pill DTC advertising Paradigm shift Dietary supplement availability Drug content found Supplements/Vitamins Potassium supplements for low potassium Potassium chloride = K-Dur, Klor Con, Micro-K” Side effects: nausea, diarrhea Folic Acid deficiency for neonatal development Folic Acid = Folate Side effects: nausea Prescription vs. Dietary Supplement “Long Weekend Dietary Supplement” FDA Recall 2007 Contained undeclared tadalafil (Cialis) “Zencore” recalled 9/2007 Keeping prescription drugs behind the counter What is really in a dietary supplement? Dietary Supplement Health and Education Act (DSHEA) Federal Trade Commission regulates advertising FDA through the DSHEA DSHEA 1994: power by FDA to ensure safe, properly labeled and claims made are substantiated Pharmacists must use care in making claims not otherwise allowed under this law http://www.fda.gov/opacom/laws/dshea.html Great Natural Products and Complementary Care website: http://nccam.nih.gov/ What is really in that pill? Manufacturer Standards? USP Consumer Lab http://www.usp.org/USPVerified/dietarySupplemen ts/ http://www.consumerlab.com/aboutcl.asp#testpro g NSF International http://www.nsf.org/ Cool Resources For You Pharmacists Manual DEA APhA Links http://www.cfsan.fda.gov/~dms/supplmnt.html Pharmacy Compounding http://www.clinicaltrials.gov/ Dietary Supplements http://www.ashp.org/ahfs/index.cfm Clinical Trials Repository http://www.pharmacist.com/AM/Template.cfm?section=Links2 ASHP Drug Information http://www.deadiversion.usdoj.gov/pubs/manuals/pharm2/index .htm http://www.fda.gov/cder/pharmcomp/default.htm Medication Information http://medlineplus.gov/