Actions, Interactions and Indications for Selected Pharmacologic Agents H CH3 O O O O OH O OH O O OH O O O O CH3O O CH3O CH3O CH3O CH3O CH3O Etoposide: Synthetic Analog Podophyllotoxin: Natural product Zora DeGrandpre, MS, ND ©2008 ISBN # 978-0-9818002-2-6 Note: In an effort to replace the Trees needed for the publication of this book, a portion of the proceeds will be donated to maintain the forests. I thank the Trees for their service 1 Table of Contents: PRINCIPLES OF PHARMACOLOGY ................................................................................... 10 ROUTES OF ADMINISTRATION .................................................................................................... 10 Oral:...................................................................................................................................... 10 Sublingual: ............................................................................................................................ 10 Inhalation .............................................................................................................................. 10 Topical .................................................................................................................................. 10 Transdermal .......................................................................................................................... 11 Parenteral ............................................................................................................................. 11 Other ..................................................................................................................................... 11 PHARMACOKINETICS .................................................................................................................. 11 Absorption ............................................................................................................................. 11 Effect of pH ........................................................................................................................... 11 Physical Variables ...................................................................Error! Bookmark not defined. Bio-availability ........................................................................Error! Bookmark not defined. Distribution is dependent on:...................................................Error! Bookmark not defined. Drug Metabolism .................................................................................................................. 12 UNITED STATES FDA PHARMACEUTICAL PREGNANCY CATEGORIES ............... 12 AUTONOMIC NERVOUS SYSTEM DRUGS ........................................................................ 13 CHOLINERGIC AGONISTS ...................................................... ERROR! BOOKMARK NOT DEFINED. Donepezil (Aricept®) ...............................................................Error! Bookmark not defined. ANTI-CHOLINERGICS:MUSCARINIC ANTAGONISTS .............. ERROR! BOOKMARK NOT DEFINED. Oxybutynin (Oxytrol®, Ditropan®) ........................................Error! Bookmark not defined. Tolterodine (Detrol®) ..............................................................Error! Bookmark not defined. NICOTINIC AGONISTS ........................................................... ERROR! BOOKMARK NOT DEFINED. Nicotine (Nicorette®, Nicotrol®, Nicoderm®) .......................Error! Bookmark not defined. SYMPATHOMIMETICS ........................................................... ERROR! BOOKMARK NOT DEFINED. α and β-adrenergic (mixed) agonist ..................................Error! Bookmark not defined. Epinephrine (Adrenalin®, EpiDri™, Epifrin®, SilTrax®, PrimateneMist®, EpiPen®) ..................................................................................................Error! Bookmark not defined. α-adrenergic agonists .........................................................Error! Bookmark not defined. Oxymetazoline (Afrin®, Allerest®, Zicam ®, Mucinex®, Neo-synephrine®, Visine®) Error! Bookmark not defined. Pseudoephedrine (Allermed®, Affrinol®, Ridafed®,Sudofed ®, Dimetapp®, Triaminic® and many other combinations )...............................................Error! Bookmark not defined. α2 Agonists .........................................................................Error! Bookmark not defined. Clonidine (Catapress ®, Duraclon®) .....................................Error! Bookmark not defined. Sympathomimetic amines ..................................................Error! Bookmark not defined. Amphetamine / Dextroamphetamine (Adderall ®, Dexadrine ®, Dextrostat®) ........... Error! Bookmark not defined. 2 Methylphenidate (Concerta®, Daytrana®, Metadate®, Ritalin®) ....... Error! Bookmark not defined. Adrenergic antagonists...................................................................................................... 14 Tamsulosin (Flomax®) ........................................................................................................ 14 β1Antagonists: ....................................................................Error! Bookmark not defined. Atenolol (Tenormin®) .............................................................Error! Bookmark not defined. Metoprolol (Toprol®, Lopressor®) ........................................Error! Bookmark not defined. Mixed α/ β Antagonist: ......................................................Error! Bookmark not defined. Carvedilol (Coreg®) ...............................................................Error! Bookmark not defined. CENTRAL NERVOUS SYSTEM (CNS) DRUGS ... ERROR! BOOKMARK NOT DEFINED. BENZODIAZEPINES ............................................................... ERROR! BOOKMARK NOT DEFINED. Alprazolam (Xanax®Niravam®) .............................................Error! Bookmark not defined. Lorazepam (Ativan®) ..............................................................Error! Bookmark not defined. Temazepam (Restoril®) ...........................................................Error! Bookmark not defined. Clonazepam (Cebercon™, Klonopin®) ..................................Error! Bookmark not defined. IMIDAZOPYRIDINES .............................................................. ERROR! BOOKMARK NOT DEFINED. Zolpidem (Ambien®) ...............................................................Error! Bookmark not defined. TRICYCLIC ANTI-DEPRESSANTS (MONOAMINE REUPTAKE INHIBITORS) ...... ERROR! BOOKMARK NOT DEFINED. Amitriptyline HCl (Elavil®, Tryptano™, Vanatrip®) ............Error! Bookmark not defined. ATYPICAL ANTIDEPRESSANTS: AROMATIC AMINOKETONES ERROR! BOOKMARK NOT DEFINED. Bupropion (Wellbutrin®, Zyban®)..........................................Error! Bookmark not defined. SELECTIVE SEROTONIN REUPTAKE INHIBITORS ......................................................................... 15 Citalopram (Celexa®) .......................................................................................................... 15 Fluoxetine (Prozac®, Sarafem®) ............................................Error! Bookmark not defined. Paroxetine (Paxil®, Pexeva®) ................................................Error! Bookmark not defined. Sertraline (Zoloft®) .................................................................Error! Bookmark not defined. SEROTONIN AGONISTS ......................................................... ERROR! BOOKMARK NOT DEFINED. Sumatriptan (Imitrex®) ...........................................................Error! Bookmark not defined. DOPAMINE AGONISTS .......................................................... ERROR! BOOKMARK NOT DEFINED. Carbidopa-Levodopa (Sinemet®) ............................................Error! Bookmark not defined. SELECTIVE SEROTONIN/NOREPINEPHRINE REUPTAKE INHIBITORS (SNERI) ERROR! BOOKMARK NOT DEFINED. Trazodone (Desyrel®) .............................................................Error! Bookmark not defined. MISCELLANEOUS CNS-ACTIVE AGENTS ............................... ERROR! BOOKMARK NOT DEFINED. Lithium carbonate (Eskalith ®, Lithobid®, Lithonate®) ........Error! Bookmark not defined. ANTI-CONVULSANTS- MIXED PHARMACOLOGIC CLASSES..... ERROR! BOOKMARK NOT DEFINED. Phenytoin (Dilantin®) .............................................................Error! Bookmark not defined. Carbamazapine (Atretol®, Tegretol®, Epitol®, Carbatrol®, Epitol®) ..... Error! Bookmark not defined. Divalproex (Depakote®) .........................................................Error! Bookmark not defined. Valproic acid (Depakene®) .....................................................Error! Bookmark not defined. Valproate Na (Depacon®) .......................................................Error! Bookmark not defined. Gabapentin (Neurontin®, Gabarone™)..................................Error! Bookmark not defined. ANTI-PSYCHOTICS- TYPICAL AND ATYPICAL ....................... ERROR! BOOKMARK NOT DEFINED. Olanzapine (Zyprexa®, Zydis®)..............................................Error! Bookmark not defined. 3 Quetiapine (Seroquel®) ...........................................................Error! Bookmark not defined. Risperidone (Risperdal®) ........................................................Error! Bookmark not defined. MUSCLE-RELAXANTS .......................................................... ERROR! BOOKMARK NOT DEFINED. Cyclobenzaprine (Flexeril®, Fexmid™, Amrix®) ..................Error! Bookmark not defined. Carbamic ester derivatives .................................................Error! Bookmark not defined. Carisoprodol (Soma®, Vanadom®, Soprodal 350™) ............Error! Bookmark not defined. OPIATES AND OPIATE ANALOGS ........................................... ERROR! BOOKMARK NOT DEFINED. Hydrocodone bitartrate (Hydromet®, Hydropane®, Mycodone®, Tussigon®) ......... Error! Bookmark not defined. Hydrocodone bitartrate +Acetaminophen (Vicodin®, Anexia®, CETA-Plus®, Dolacet®, Duocet®, Lorcet®, Lortab®, Hydrocet®) ..............................Error! Bookmark not defined. Hydrocodone bitartrate +Aspirin (Azdone®) ........................Error! Bookmark not defined. Hydrocodone bitartrate +Ibuprofen (Vicoprofen®) ..............Error! Bookmark not defined. Fentanyl citrate (Fentora®, Sublimaze®) ...............................Error! Bookmark not defined. Fentanyl Transdermal (Duragesic®) ......................................Error! Bookmark not defined. Fentenyl Transmucosal (Actiq®, Fentenyl Oralet®) ..............Error! Bookmark not defined. Oxycodone HCl (Oxycontin®, OxyFast®, Percolone®, OxyDose™, Endocodone ®, Roxicodone®) ..........................................................................Error! Bookmark not defined. Codeine (Phosphate or Sulfate salts).......................................Error! Bookmark not defined. Methadone (Diskets®, Dolophine®, Methadose®)................Error! Bookmark not defined. RESPIRATORY SYSTEM AGENTS........................ ERROR! BOOKMARK NOT DEFINED. ANTI-ASTHMATICS ............................................................... ERROR! BOOKMARK NOT DEFINED. Sympathomimetics .............................................................Error! Bookmark not defined. Albuterol (Proventil®, Ventolin®, AccuNeb®, Volmax®, ProAir®, VoSpire®) ......... Error! Bookmark not defined. Beclomethasone (Beconase®, QVAR ®, Beclovent®, Vancenase®) .... Error! Bookmark not defined. Salmeterol (Serevent Diskus®) ................................................Error! Bookmark not defined. Anti-Cholinergics ...............................................................Error! Bookmark not defined. Ipratropium (Atrovent®) .........................................................Error! Bookmark not defined. Corticosteroids .................................................................................................................. 17 Budesonide (Entocort®, Pulmicort®, Rhinocort®) ................Error! Bookmark not defined. Fluticasone (Flonase®, Flovent ®, Cutivate ®,Veramyst™) .Error! Bookmark not defined. Triamcinolone (Aristocort®, Kenacort®, Azmacort®, Flutex™, Oralone ®, Nasacort ®) ..................................................................................................Error! Bookmark not defined. RESPIRATORY DRUGS: MISCELLANEOUS ............................. ERROR! BOOKMARK NOT DEFINED. Cromolyn sodium (Crolom®, Gastrocrom ®, Intal ®, Nasalcrom®) .. Error! Bookmark not defined. Montelukast (Singulair ®) .......................................................Error! Bookmark not defined. ANTI-HISTAMINES ................................................................ ERROR! BOOKMARK NOT DEFINED. Cetirizine (Zyrtec ®) ................................................................Error! Bookmark not defined. Diphenhydramine (Allermax®, Benedryl®, Compoz®, Diphen®, Hyrexin®, Genahist®, Nytol®, Sleepinal®, Midol®, Sominex®, Unisom®) ..............Error! Bookmark not defined. Loratadine (Alavert®, Claritin®, Equate®) ...........................Error! Bookmark not defined. HEMATOPOIETIC SYSTEM DRUGS .................... ERROR! BOOKMARK NOT DEFINED. 4 ANEMIA ............................................................................... ERROR! BOOKMARK NOT DEFINED. Vitamin B12, Cyanocobalamin (BigShot B12®, Cyanoject®, Rubramin®, Hydro-Crysti12®, LA-12®, CaloMist™) .....................................................Error! Bookmark not defined. Folic acid (Folvite ®, FA-8®, Folacin®, Folicet™) ..............Error! Bookmark not defined. Iron Dextran (DexFerrum ®, InFed®)....................................Error! Bookmark not defined. Iron sucrose (Venofer®) ..........................................................Error! Bookmark not defined. COAGULATION DISORDERS................................................... ERROR! BOOKMARK NOT DEFINED. Acetylsalicylic acid (Aspirin®, Acuprin®, Bayer®, Ecotrin®, EMPIRIN®, Norwich®, Sureprin®, Zorprin®) ..............................................................Error! Bookmark not defined. Clopidogrel (Plavix®) .............................................................Error! Bookmark not defined. Heparin (Hep-Lock®, Hep-Pak®, Uniparin®, Homochron™, Monoject®)................ Error! Bookmark not defined. Warfarin (Coumadin®, Jantoven™) .......................................Error! Bookmark not defined. Vitamin K (AquaMEPHYTON®, Mephyton®) ........................Error! Bookmark not defined. ANTI-HYPERLIPIDEMIC AGENTS ........................................... ERROR! BOOKMARK NOT DEFINED. Niacin/ Vitamin B3/ Nicotinic acid/ Niacinamide (Slo-Niacin®, Niacor®, Nicolar®) Error! Bookmark not defined. STATIN DRUGS ..................................................................... ERROR! BOOKMARK NOT DEFINED. Atorvastatin (Lipitor®) ............................................................Error! Bookmark not defined. Lovastatin (Altocor®, Mevacor®, Altoprev®) ........................Error! Bookmark not defined. ANTI-INFLAMMATORY AGENTS ........................................... ERROR! BOOKMARK NOT DEFINED. Anti-Arthritic Agents .........................................................Error! Bookmark not defined. Hydroxychloroquine (Plaquenil®, Quineprox®) ....................Error! Bookmark not defined. Methotrexate (Amethopterin®, MTX®, Rheumatrex®, Trexall®) ........ Error! Bookmark not defined. ANALGESICS ........................................................................ ERROR! BOOKMARK NOT DEFINED. Prostaglandin synthesis inhibitors .....................................Error! Bookmark not defined. Acetylsalicylic acid (Aspirin®, Acuprin®, Bayer®, Ecotrin®, EMPIRIN®, Norwich®, Sureprin®, Zorprin®) ..............................................................Error! Bookmark not defined. Acetaminophen (Acephen®, Aceta®, Aminofen® Anacin®, Tylenol ®, Datril®, Feverall®, Liquiprin®Genapap®, Maranox®, Tempra®) .......................Error! Bookmark not defined. NSAIDs ..............................................................................Error! Bookmark not defined. Ibuprofen (Advil®, Motrin®, Genpril®, Medipren®, Menadol®, Midol®, Nuprin ®) Error! Bookmark not defined. Naproxen (Aflaxen™, Anaprox®, Aleve®, Mediproxen®, Naprosyn ®, Naprelan®) . Error! Bookmark not defined. Celecoxib (Celebrex ®) ...........................................................Error! Bookmark not defined. Miscellaneous: ...................................................................Error! Bookmark not defined. Sulfasalazine (Azulfidine ®, Salazopyrn ®, Sulfazine®).........Error! Bookmark not defined. CARDIOVASCULAR SYSTEM DRUGS ................. ERROR! BOOKMARK NOT DEFINED. Β1 ANTAGONISTS: ................................................................. ERROR! BOOKMARK NOT DEFINED. Atenolol (Tenormin®) .............................................................Error! Bookmark not defined. Metoprolol (Toprol®, Lopressor®) ........................................Error! Bookmark not defined. MIXED Α/ Β ANTAGONIST: ................................................... ERROR! BOOKMARK NOT DEFINED. Carvedilol (Coreg®) ...............................................................Error! Bookmark not defined. α2 Agonists .........................................................................Error! Bookmark not defined. 5 Clonidine (Catapress ®, Duraclon®) .....................................Error! Bookmark not defined. ACE INHIBITORS.................................................................. ERROR! BOOKMARK NOT DEFINED. Benazapril (Lotensin®) ..........................................................Error! Bookmark not defined. Lisinopril (Prinvil®, Zestril®) ...............................................Error! Bookmark not defined. CA2+ CHANNEL BLOCKERS .................................................. ERROR! BOOKMARK NOT DEFINED. Verapamil (Calan®, Covera®, Isoptin ®, Verelan®) ...........Error! Bookmark not defined. Diltiazem (Cardizem®, Cartia ®, Diltia®, Dilacor® Tiazac®, Taztia™) Error! Bookmark not defined. NITRATES ............................................................................. ERROR! BOOKMARK NOT DEFINED. Isosorbide dinitrate (Dilatrate®, Isordil ®) ............................Error! Bookmark not defined. Isosorbide mononitrate (Imdur®, Imso®, Monoket ®) ...........Error! Bookmark not defined. Nitroglycerin (Diponit®, Minitran®, Nitro-Dur ®, Nitolingual®, Nitrostat®, Nitrotab™, Nitrol®)....................................................................................Error! Bookmark not defined. CARDIAC GLYCOSIDES ......................................................... ERROR! BOOKMARK NOT DEFINED. Digoxin (Digitek®, Lanoxicaps®, Lanoxin ®)........................Error! Bookmark not defined. ANTI-ARRHYTHMICS ............................................................ ERROR! BOOKMARK NOT DEFINED. Amiodorone (Cordorone®, Pacerone ®) ................................Error! Bookmark not defined. Propafenone (Rythmol ®) ........................................................Error! Bookmark not defined. DIURETICS ........................................................................... ERROR! BOOKMARK NOT DEFINED. Furosemide (Lasix®) ...............................................................Error! Bookmark not defined. Hydrochlorothiazide (HCTZ) (Esidrix®, Ezide ™, HydroDiuril®, Hydro-Par®, Microzide®, Oretic®) ..............................................................Error! Bookmark not defined. Spironolactone (Aldactone®, Spirono™)................................Error! Bookmark not defined. GASTROINTESTINAL SYSTEM AGENTS ........... ERROR! BOOKMARK NOT DEFINED. ANTACIDS ............................................................................ ERROR! BOOKMARK NOT DEFINED. Calcium carbonate (Alka-Mints®, Alkets®, Calci-Chew®, Caltrate®, Os-Cal®, OystCal®, Rolaids®, Tums® ..........................................................Error! Bookmark not defined. + H PUMP INHIBITORS ............................................................ ERROR! BOOKMARK NOT DEFINED. Esomeprazole (Nexium®) ........................................................Error! Bookmark not defined. HISTAMINE2 RECEPTOR ANTAGONISTS ................................. ERROR! BOOKMARK NOT DEFINED. Ranitidine (Zantac®) ...............................................................Error! Bookmark not defined. CATHARTICS AND LAXATIVES ............................................. ERROR! BOOKMARK NOT DEFINED. Irritants ...............................................................................Error! Bookmark not defined. Stimulants ..........................................................................Error! Bookmark not defined. Stool softeners....................................................................Error! Bookmark not defined. Bisacodyl (Bisac-Evac ®, Carter’s Little Pills®, Correctol®, Dacodyl®, Deficol®, Dulcolax®, Feen-a-Mint®, Fleet®, Theralax® ......................Error! Bookmark not defined. Docusate Calcium (DC Softgels®, Pro-Cal Sof®, Sulfolax®)Error! Bookmark not defined. Docusate sodium (Colace®, Correctol®, DOS Softgels®, Modane Soft®, Regulax SS®, Silace®, Regulax®) .................................................................Error! Bookmark not defined. Osmotic Agents ..................................................................Error! Bookmark not defined. Polyethylene glycol (GlycoLax™, MiraLax®) ........................Error! Bookmark not defined. Magnesium Hydroxide (Milk of Magnesia®, Freelax™) ........Error! Bookmark not defined. Magnesium Sulfate (Epsom Salts) ...........................................Error! Bookmark not defined. Bulking Agents ..................................................................Error! Bookmark not defined. 6 Psyllium (Alramucil®, Fiberall®, Genfiber®, Hydrocil®, Konsyl®, Maalox®, Metamucil®, Modane Bulk®, Reguloid®, Restore®, Serutan®, Sylact®, V-Lax®) .... Error! Bookmark not defined. ANTI-DIARRHEAL ................................................................. ERROR! BOOKMARK NOT DEFINED. Loperamide (Imodium®, Kaopectate®, Diarrhea Control®) .Error! Bookmark not defined. ANTI-EMETIC ....................................................................... ERROR! BOOKMARK NOT DEFINED. Prochlorperazine maleate (Compazine®, Compro™) ............Error! Bookmark not defined. GENITOURINARY SYSTEM DRUGS .................... ERROR! BOOKMARK NOT DEFINED. MALE GU SYSTEM .............................................................. ERROR! BOOKMARK NOT DEFINED. Tamsulosin (Flomax®) ............................................................Error! Bookmark not defined. Sildenafil (Viagra®, Revatio™) ..............................................Error! Bookmark not defined. ENDOCRINE SYSTEM DRUGS ............................... ERROR! BOOKMARK NOT DEFINED. THYROID AGENTS ................................................................ ERROR! BOOKMARK NOT DEFINED. Dessicated Thyroid (Armour Thyroid®, Bio-Throid®, Etwon™, Thyrotab®, Westhroid®) ..................................................................................................Error! Bookmark not defined. Levothyroxine (Estre™, Synthroid®, Levolet®, Levo-T®, Levothroid®, Levoxyl®, ThyroTabs®, Unithroid®).................................................................Error! Bookmark not defined. Tri-iodothyronine, ....................................................................Error! Bookmark not defined. (Cytomel®, Triostat®) .............................................................Error! Bookmark not defined. CORTICOSTEROIDS ............................................................... ERROR! BOOKMARK NOT DEFINED. Beclomethasone (Beconase®, Beclovent ®,Vancenase®, Vanceril®,QVAR ®) .......... Error! Bookmark not defined. Hydrocortisone (Cortef®, Cortenema®, Hydrocortone ®, Anusol®, Cortizone®, Dermarest®) ............................................................................Error! Bookmark not defined. Prednisone (Deltosone®, Predone™, Sterapred®) ................Error! Bookmark not defined. Triamcinolone (Aristocort®, Kenacort, Azmacort®, Cinalog™, Cinolar™, Flutex™, Nasacort ®, Kenalog®, Oralone®) ........................................Error! Bookmark not defined. FEMALE REPRODUCTIVE HORMONES ......................................................................................... 19 SERMs .............................................................................................................................. 19 Clomiphene citrate (Clomid®, Milophene®, Serophene®) ....Error! Bookmark not defined. Raloxifene (Evista®) ................................................................Error! Bookmark not defined. Estrogens and estrogen derivatives ....................................Error! Bookmark not defined. Conjugated Estrogens (Premarin®, Cenestin™, Enjuvia™)..Error! Bookmark not defined. Estrone (Estra AQ®, Estragyn 5®, Estro-A®, Primestrin®) .Error! Bookmark not defined. Estriol: .....................................................................................Error! Bookmark not defined. Estradiol: Estrace®, Estring®, EstroGel®, Gynodiol®, Innofem® ..... Error! Bookmark not defined. Estradiol acetate: Femring™ ..................................................Error! Bookmark not defined. Estradiol cyprionate: Depo-Estradiol® ..................................Error! Bookmark not defined. Transdermal: Alora®, Climara®, Delestrogen®, Esclim®, Estraderm®, Menostar™, Vivelle®, Vivelle-Dot® ............................................................Error! Bookmark not defined. Estradiol hemihydrate: Estrasorb™........................................Error! Bookmark not defined. Estradiol valerate: Clinagen LA40®, Delestrogen® ..............Error! Bookmark not defined. Progesterone and progesterone derivatives ........................Error! Bookmark not defined. 7 Medroxyprogesterone (Amen®, Depo-Provera®, Provera®, Prodroxy™, Provera®) Error! Bookmark not defined. Progesterone (Crinone®, Progesterone MC 10 ®, First™- ®, First™-Progesterone VGS 100 ® Progesterone VGS 25, 50, 200, 400 ®, Gesterone™, Gestrin™, Prochieve®, Prometrium®) ..........................................................................Error! Bookmark not defined. Contraceptives....................................................................Error! Bookmark not defined. Norgestimate/Ethinyl Estradiol (MonoNessa®, Ortho Tri-Cyclen® Lo Ortho-Cyclen®, Ortho-Tri-Cyclen®, Previfem®, Sprintec-28®, Tri-Previfem®, Tri-Sprintec®, TriNessa®) ..................................................................................................Error! Bookmark not defined. Norgestimate/Estradiol (Ortho-Prefest™, Prefest®) ..............Error! Bookmark not defined. Norelgestromin/ethinyl estradiol (OrthoEvra®) .....................Error! Bookmark not defined. Male Hormones ..................................................................Error! Bookmark not defined. Testosterone (Androderm®, AndroGel®, Striant®, Testim®, Testoderm®, Testopel®DepoTestosterone®, TestaSpan™, Testopel®, Tostrelle™, Virilon®Injection) . Error! Bookmark not defined. Testosterone cypionate (Depo-Testoserone®) ........................Error! Bookmark not defined. Testosterone enanthate (Delatestryl®) ....................................Error! Bookmark not defined. Miscellaneous Hormones ...................................................Error! Bookmark not defined. Androstenedione ......................................................................Error! Bookmark not defined. Calcitonin (Fortical®, Miacalcin®, Salmonine®) ..................Error! Bookmark not defined. Dehydroepiandrosterone: (Prestara™, Vitamist®, DHEA-M for Men, DHEA-W for Women) ....................................................................................Error! Bookmark not defined. Pregnenolone ...........................................................................Error! Bookmark not defined. Insulin, Glucagon and Anti-Hypoglycemic agents ............Error! Bookmark not defined. Glucagon (GlucaGen®, Glucagon®) ......................................Error! Bookmark not defined. Insulin ................................................................................................................................... 20 Oral Hypoglycemics ..........................................................Error! Bookmark not defined. Glyburide (DiaBeta®, Glynase PresTab®, Micronase ®, Glycron™) Error! Bookmark not defined. Metformin (Fortamet ™, Glucophage®, Riomet®) ................Error! Bookmark not defined. Rosiglitazone (Avandia®) ........................................................Error! Bookmark not defined. ANTI-NEOPLASTICS .............................................................. ERROR! BOOKMARK NOT DEFINED. Tamoxifen citrate (Sotamox®, Nolvadex®).............................Error! Bookmark not defined. Anastrozole (Arimidex®) .........................................................Error! Bookmark not defined. Cyclophosphamide (Cytoxan®, Neosar®) ..............................Error! Bookmark not defined. Doxorubicin (Adriamycin ®, Rubex®) ....................................Error! Bookmark not defined. Etoposide (VP16-213) (Toposar®, VePesid®, Etopophos®) .Error! Bookmark not defined. 5-Flurouracil (Adrucil®, Carac™, Efudex ®, Fluroplex®) ...Error! Bookmark not defined. Cyclosporine (Gengraf®, Neoral®, Sandimmune®, Restasis™, Pulminiq™, SangCya™) ..................................................................................................Error! Bookmark not defined. Methotrexate, MTX (Amethopterin®,Rheumatrex®, Trexall®) ............ Error! Bookmark not defined. Vinblastne (Velban ®) .............................................................Error! Bookmark not defined. Paclitaxel (Onxol ™, Taxol®) .................................................Error! Bookmark not defined. DERMATOLOGICAL AGENTS ................................................. ERROR! BOOKMARK NOT DEFINED. 8 Isotretinoin (Accutane®, Amnesteem ™, Claravis®, Sotret®) ............. Error! Bookmark not defined. Benzoyl peroxide (Benzac ®, Benzagel®, Clearplex™, Clearskin™, Desquam®, Fostex®, Lavoclen ™, Loroxide®, Panoxyl®, Zodem®) .......................Error! Bookmark not defined. TOPICAL ANALGESICS.......................................................... ERROR! BOOKMARK NOT DEFINED. Benzocaine (Americaine®, Anacaine®, Anbesol®, Boil-Ease®, Cepacol®, Comfort Caine™, DentiCare™, Dermoplast®, Detane®, Dry Socket™, Freez Eez™, Gingicaine™, Hurricaine®, Isodettes®, Lanacane®, Numzident®, Orabase ®, Orajel®, Otocain®, Outgro®, Pro-caine™, Retre Gel™, Rid-A-Pain®, Solarcaine®, Sting-Kill®, Topex™, Topicale™, Zilactin®) .............................................................Error! Bookmark not defined. Capsaicin (Analgesic Balm with Capsaicin, ArthriCare®, Arthritis Formula®, Arthritis Pain Relief Rub®®, Axsain™, Capzasin® HP Arthritis Formula, Dr. S®, Eucalyptamint® 2000, Icy Hot®, Menthac®, Pain-X™, Rid-a-Pain®, RT Capsin®, Salonpas®, Trixaicin®, Zostrix®) ..................................................................................Error! Bookmark not defined. Methyl salicylate (Oil of Wintergreen, Sweet Birch Oil, Exocaine®, Gordogesic®, Bengay® (with menthol)) .........................................................................Error! Bookmark not defined. MUSCULOSKELETAL AGENTS .............................................. ERROR! BOOKMARK NOT DEFINED. Bisphosphonates ................................................................Error! Bookmark not defined. Alendronate (Fosamax®) ........................................................Error! Bookmark not defined. Calcitonin (Fortical®, Miacalcin®, Salmonine®) ..................Error! Bookmark not defined. ANTI-MICROBIALS ............................................................... ERROR! BOOKMARK NOT DEFINED. β-lactams: Cell wall synthesis inhibitors ...........................Error! Bookmark not defined. Amoxicillin (Amoxil ®, DisperMox™, MOXATAG™, Moxilin™, Sumox ™, Trimox®) ..................................................................................................Error! Bookmark not defined. Amoxicillin/ Clavulanate (Augmentin®Amoclan) ...................Error! Bookmark not defined. Cephalosporins ...................................................................Error! Bookmark not defined. Cephalexin (Keftab®, Bio-Cef™, Keflex®, Keftab®, Panixine DisperDose™)........... Error! Bookmark not defined. Protein synthesis inhibitors: Macrolides, Tetracyclines ....Error! Bookmark not defined. Macrolides:: Azithromycin, Erythromycin ........................Error! Bookmark not defined. Azithromycin (Azasite™, Zithromax®, Zmax™).....................Error! Bookmark not defined. Erythromycin (A/T/S®, Akne Mycin®, Akne-Mycin®, E-Mycin®, E.E.S.®, Emcin Clear, Emgel®, Ery Pads™, Ery-Tab®, ERYC®, Erycette®, EryDerm®, Erygel®, Erymax®, EryPed®, Erythra-Derm®, Erythrocin®, Ilosone®, Ilotycin®, My-E®, Staticin®, T-Stat®) ..................................................................................................Error! Bookmark not defined. Tetracyclines: Tetracycline, Doxycycline .........................Error! Bookmark not defined. Tetracycline (Emtet™, Panmycin™, Sumycin®, Tetra 250™ Error! Bookmark not defined. Doxycycline (Adoxa®, Alodox™, Atridox™, Bio-Tab™, Doryx®, Doxal™, Doxy™, Monodox®, Oracea™, Oraxyl™, Periostat®, Vibra-Tabs®, Vibramycin®) .............. Error! Bookmark not defined. Aminoglycosides:Tobramycin ...........................................Error! Bookmark not defined. Tobramycin (AK-Tob®, Nebcin®, TOBI®, Tobrex®) ............Error! Bookmark not defined. Sulfonamides: Sulfamethoxazole-trimethoprim(SMX-TMP) ......... Error! Bookmark not defined. Sulfamethoxazole-trimethoprim (SMX-TMP) (Bacter Aid™, Bactrim™, Septra®, Sulfatrim®, Sultrex™) .............................................................Error! Bookmark not defined. 9 Fluoroquinolines: Ciprofloxacin ........................................Error! Bookmark not defined. Ciprofloxacin (Ciloxan®, Cipro®, Ciprofloxacin, ProQuin®) ............ Error! Bookmark not defined. ANTI-FUNGALS .................................................................... ERROR! BOOKMARK NOT DEFINED. Azoles: Clotrimazole, fluconazole .....................................Error! Bookmark not defined. Clotrimazole (Anti-Fungal™, Clotrimazole, Cruex®, Desenex®, Femcare®, GyneLotrimin®, Gynix™, Jock Itch Relief, Lotrimin®, Mycelex®, Trivagizole 3™) .......... Error! Bookmark not defined. Fluconazole (Diflucan®) .........................................................Error! Bookmark not defined. Polyenes: Nystatin .............................................................Error! Bookmark not defined. Nystatin (BioStatin™, Mycostatin®, Nyamyc™, Nystex®, Nystop®) .. Error! Bookmark not defined. Allylamine: Terbinafine .....................................................Error! Bookmark not defined. Terbinafine (Desenex Max®, Lamisil®) .................................Error! Bookmark not defined. ANTI-VIRALS: DNA POLYMERASE INHIBITORS: ACYCLOVIR, PENCICLOVIR, FAMCICLOVIR ............................................................................................. ERROR! BOOKMARK NOT DEFINED. Acyclovir (Zovirax®) ...............................................................Error! Bookmark not defined. Famciclovir (Famvir®) ..........................................................Error! Bookmark not defined. Valcyclovir (Valtrex®) ............................................................Error! Bookmark not defined. ANTI-VIRALS- MISCELLANEOUS : AMANTADINE ................. ERROR! BOOKMARK NOT DEFINED. Amantadine (Symmetrel®) ......................................................Error! Bookmark not defined. ANTI-RETROVIRALS: NRTIS, PROTEASE INHIBITORS ........... ERROR! BOOKMARK NOT DEFINED. Nucleoside reverse transcriptase inhibitors (NRTIs): Didanosine, Lamivudine, Zidovudine .........................................................................Error! Bookmark not defined. Didanosine (ddI, Videx®) ........................................................Error! Bookmark not defined. Lamivudine, 3TC (Epivir®) ....................................................Error! Bookmark not defined. Zidovudine, ZDV (Retrovir®) .................................................Error! Bookmark not defined. Protease inhibitors: Indinavir .............................................Error! Bookmark not defined. Indinavir, ZDV (Crixivan®) ...................................................Error! Bookmark not defined. VACCINATION ...................................................................... ERROR! BOOKMARK NOT DEFINED. HEAVY METAL TOXICITY DRUGS......................................... ERROR! BOOKMARK NOT DEFINED. : ..........................................................................................Error! Bookmark not defined. Penicillamine (Cuprimine®, Depen ®) ..................................Error! Bookmark not defined. DMPS: 2,3-Dimercapto-1-propanesulfonic acid (Unithiol®, Dimaval®) . Error! Bookmark not defined. DMSA ™, Succimer (Chemet®) .............................................Error! Bookmark not defined. Edetate Calcium Disodium, Calcium EDTA ............................Error! Bookmark not defined. Deferoxamine ...........................................................................Error! Bookmark not defined. EMERGENCY SITUATIONS: ................................................... ERROR! BOOKMARK NOT DEFINED. Ringers lactate (VisIV™) .........................................................Error! Bookmark not defined. Saline (Sodium Chloride) .........................................................Error! Bookmark not defined. D5W, D10W (5% and 10% Dextrose in water) .......................Error! Bookmark not defined. D50 (50 g Dextrose/Glucose) ..................................................Error! Bookmark not defined. Glucose (B-D® Glucose, Dex4® Glutol™, Glutose 15™, Glutose™, Insta-Glucose®) ..................................................................................................Error! Bookmark not defined. 10 Principles of Pharmacology Routes of Administration Oral: Drug must be stable to enzyme degradation (e.g. salivary) and acid hydrolysis/denaturation in the stomach. Drug must be absorbed by the GI and must also be stable for First-Pass metabolism. Easy self-administration. First Pass Metabolism: Any drug that is absorbed through the GI tract must first pass through the portal system. Drugs are metabolized by the liver to inactive or less active derivatives to varying degrees. Many drugs therefore cannot be given by mouth. Sublingual: Avoids the problems of oral administration and First Pass metabolism. Absorption is through the mucosa directly to capillaries and is dependent on the properties of the drug. Easy selfadministration. Inhalation Generally is a rapid absorption and easy self-administration. Not suitable for some patients or conditions. Topical Useful for local action and or with agents that can cause systemic problems such as hypersensitivity or toxicity. Used primarily for dermatologic, otic, ophthalmologic, vaginal, rectal, and nasal applications. Easy self-administration Transdermal Useful for “patch” applications and when sustained drug release is desirable. Drug must be lipophilic. Easy self-administration. Parenteral Intravenous (IV) Intramuscular (IM) Subcutaneous (SC, SubQ) 11 Other Intranasal Intrathecal /Intraventricular: The drug is delivered directly into the CSF Pharmacokinetics Half-life: (t1/2) amount of time required for the concentration of the drug to decrease by ½ Therapeutic Index = Toxic Dose/ Effective Dose Absorption Passive diffusion: driven by concentration gradients (from higher to lower drug concentration). No energy is required. No carrier is necessary (therefore no saturation effects). Lipid-soluble drugs: cross the cell membrane Water-soluble drugs: pass through aqueous channels/pores in the membrane Active transport: Requires energy and a specific transport system. Saturation kinetics are present. May be transported against a concentration gradient. Effect of pH Most drugs are weak acids or weak bases Weak acids: HA⇋H+ + A A charged (anionic) drug, A- will not pass through the cell membrane. The drug must be in the protonated form to pass into the cell. Weak acids (higher pKa) will be absorbed more easily in weakly acidic environments pH = pKa+ log [A-]/[HA] Weak bases Drug Metabolism Kinetics: Most drugs follow first-order Michaelis-Menten kinetics. The rate of metabolism is directly related to the concentration of the drug and a constant fraction of the total drug is metabolized per unit of time. Some drugs follow zero-order (non-linear) kinetics and the rate of metabolism remains constant over time. Zero order kinetics: High Dose Rate of Metabolism 12 1st order kinetics: Low Dose Hydrophobic drugs cannot generally be eliminated by the kidneys and are handled by the liver using two sets of reactions to make the drugs more water-soluble. The drug activity may be increased, decreased or unchanged by Phase I reactions. In general, Phase II reactions decrease pharmacologic activity. Phase I: Phase II Some drugs undergo Phase II and then Phase I reactions United States FDA Pharmaceutical Pregnancy Categories Pregnancy Category A o No risk to fetus in the all trimesters of pregnancy. (Animal and human studies) Pregnancy Category B o Animal studies have failed to demonstrate a risk to the fetus. Either there are no adequate and well-controlled studies in pregnant women or there are no negative animal studies, but adequate and well-controlled studies in pregnant women have failed to demonstrate a risk to the fetus in any trimester. Pregnancy Category C o Animal studies have shown an adverse effect on the fetus. There are no adequate and well-controlled studies in humans. Potential benefits may necessitate use of the drug in pregnant women despite potential risks. 13 Autonomic Nervous System Drugs Motor Neuron: Nicotinic receptor Neurotransmitter: ACh Autonomic, Sympathetic Neuron: Pre-synaptic Neurotransmitter: ACh (Nicotinic) Post-synaptic (Adrenergic) Neurotransmitter: NE (α or β) Autonomic, Parasympathetic Neuron: Pre-synaptic Neurotransmitter: ACh (Nicotinic) Post-synaptic Neurotransmitter: ACh (muscarinic) Cholinergic Responses: ↓ HR, CO, bp⇒ ↑ intestinal, salivary secretions and intestinal motility⇒ Diarrhea, nausea, vomiting ↑ Bronchiolar smooth muscle tone ↑ ciliary m. ⇒ ↑ miosis ↑ tone of detrusor m⇒ ↑ urination ↑ sweat gland activity⇒ diaphoresis Bradycardia, Dizziness 14 Adrenergic antagonists MOA: α1 antagonists: Act primarily on the CV system. Vasoconstriction is inhibited, bringing about a net decrease in bp. Decreases smooth muscle contraction and increases ease of urine flow. Overall clinical effect depends on status and specificity of blockage. If α2receptors are also blocked, there will be an increased sympathetic response and potentially a smaller drop in bp due to increased NE release and baroreceptor reflex. α2 antagonists: Centrally, these antagonists block either post-synaptic α2adrenergic receptors (↑ sympathetic response) or pre-synaptic α2- adrenergic receptors, ↑NE release. The net result is an increase in bp, decreased resistance to urine outflow, increased insulin release and increase smooth muscle tone. β1 antagonists: Act primarily on the CV system, decreased heart rate (↓ SA node rate), decreased contractility and decreased peripheral arteriolar resistance. Renin secretion is decreased, but it is not known if this is important in the hypotensive effects. β2 antagonists: Act to increase bronchiolar constriction. Generally little effect in normal individuals, but may induce bronchospasm in patients with asthma or COPD. Increased CA release may increase serum glucose in diabetics. Mixed adrenergic antagonists: The overall effect will be dependent on degree of selectivity and clinical status. Often difficult to predict. α1 Antagonists Tamsulosin (Flomax®) Canadian Brand Names Flomax Uses: BPH Pharmacologic class: α1-adrenergic blocker Therapeutic class: Anti-adrenergic Pregnancy Risk Category B CI: Hypersensitivity Adverse Reactions Dizziness, restlessness, vertigo, headache, insomnia, Orthostatic hypotension Decreased libido and ejaculation Cough Precautions: Hypertension, orthostatic hypotension 15 Concurrent use of other adrenergic antagonists Females Elderly Pregnancy, lactation Renal, hepatic disease Drug-Lab interactions None known Lab monitoring: None necessary Selected interactions Protease inhibitors, anti-hypertensives, concurrent use of adrenergic blockers, alcohol Food Grapefruit juice Herbal α, β agonists: Ephedra, Yohimbe, Hypericum Herbs with hypertensive effects: Zingiber, Glycyrrhiza Anti-hypertensive herbs: Allium cepa, Allium sativa, Borago, Capsicum, Centella, Rauwolfia. Selective Serotonin Reuptake Inhibitors MOA: Block the re-uptake of 5HT thereby increasing local concentrations of the neurotransmitter. Reflex decrease of receptors may be the basis of long-term action. Citalopram (Celexa®) Uses: Depression Pharmacologic class: Selective Serotonin Re-uptake Inhibitor (SSRI) Therapeutic class: Anti-depressant Pregnancy Risk Category C CI: Hypersensitivity MAOI use Abrupt withdrawal Adverse Reactions Major: Suicide, akathisia, choreoathetosis, coagulopathy, hemolytic anemia, hepatic necrosis, GI bleed, neuroleptic malignant syndrome, renal failure, serotonin syndrome, SIADH, toxic epidermal necrolysis, torsade de pointes, ventricular fibrillation, anaphylaxis 16 Apathy, psychosis, mania, migraine, dizziness, drowsiness, agitation, headache, insomnia, nervousness, poor concentration, worsening depression Tachycardia, orthostatic hypotension Blurry vision, nausea, vomiting, diarrhea Rash, polyuria, amenorrhea, dysmenorrhea, ED, priapism Arthralgia, myalgia, dyspnea Erythema multiforme, rash, pruritis, yawning. Precautions: Hepatic, renal, cardiac dysfunction History of mania, seizure disorder, suicidal tendencies History of addictive behaviors Driving, operating machinery Electroconvulsive therapy Elderly Pregnancy, lactation Hyponatremia Children < 18 yo Drug Lab interactions ↓ Na+ Lab Monitoring Liver function tests Thyroid function tests Serum Na+ Selected interactions Adrenergics, protease inhibitors, anti-depressants, anti-histamines, barbiturates, CNS depressants, H+ pump inhibitors, statins, MOAI’s, other SSRIs, NSAIDs, sympathomimetics, opiates/opioids, TCAs Herbal Nervines Avena, Humulus, Hypericum, Leonurus, Matricaria, Passiflora, Piper methysticum, Piscidia, Pulsatilla, Roseminarius, Scutelleria, Verbena, Viburnum, Viscum. Mentha X piperita: activates endogenous opioids MAO inhibition in vitro Ginkgo, Hypericum, Panax, Eschoscholazia, Piper methysticum Cardiac glycosides: Hypericum, Crataegus, Digitalis, Convallaria, Selenicereus GABA containing herbs: Astragalus Herbs that may interfere with serotonin: Aspidosperma, Hypericum, Iris versicolor, Mentha X piperita, Pausinystalia, Tanacetum, Urtica. α and β agonist: Ephedra, Hypericum, Pausinystalia Herbs containing PA 17 Borago, Petasites, Eupatorium purpurea and Eupatorium spp, Senecio spp, Pulmonaria. Thyroid active herbs: Capsella, Lycopus, Lithospermum, Melissa, Leonurus, Thymus serpyllum, Viscum album, Withania Herbs with histaminic interactions Aloe vera, Hyoscyamus, Phytolacca, Scutelleria, Urtica Herbs with anti-protease activity Curcuma, Ligusticum Herbs with opiate interactions: Hypericum, Piscidia, Silybum Herbs which induce endorphins Viscum album Corticosteroids MOA: Corticosteroids are primarily used clinically as anti-inflammatory agents and immunosuppressants. Corticosteroids may have glucocorticoid and mineralocorticoid effects, depending on the particular agent. The effect of corticosteroids is generally delayed, as the mechanism involves interaction with target receptors followed by import into the nucleus and eventual alteration of gene expression and protein synthesis. Metabolic effects Carbohydrate metabolism ↑ gluconeogenesis ↑ glycogen synthesis Protein metabolism ↑ proteolysis Lipid metabolism Electrolyte /water metabolism ↑ lipolysis ↑ Na+, H2O reabsorption 18 ↓ glucose utilization in periphery⇒ ↑ [glucose]plasma ↑ use of aa for gluconeogenesis ↑ fat redistribution ↑ K+, H+, Ca2+ excretion ↓ Ca2+ intestinal uptake Adverse effects Steroid withdrawal Prolonged high dose Systemic effects Cardiovascular Skeletal muscle CNS Hematopoietic Exacerbation of underlying disease process Acute adrenal insufficiency HPA suppression recovery varies from weeks to > 1 year HPA suppressive effects Fluid/Electrolyte/metabolic: Hypokalemic alkalosis, edema, hypertension, hyperglycemia, glucosuria Immune: ↑ susceptibility to infection Skeletal system: ↑ osteoporosis, osteonecrosis GI: ↑ PUD, GI bleeds Muscles: Steroid myopathy Ophthalmic: cataracts Psychological: Mood changes, neuroses, psychoses, suicidal behavior, “steroid rage” ↑ vascular reactivity to vasoactive substances ↑ vascular permeability ↑ muscle wasting (steroid Low corticosteroid levels: myopathy) after high concentrations fatigue, weakness for prolonged periods Direct effects: Mixed. Appear to Indirect effects: depend on bp, depend on dose, duration and glucose and electrolyte endogenous production of concentrations neurotransmitters. Effects include mood elevation, depression, neuroses, psychoses ↑ hematopoiesis ↑ neutrophils ↓ lymphoid tissue ↓ lymphocytes, eosinophils, monocytes, basophils ↑ Na+/ H2O⇒ ↑ bp Inflammation and ↓ Arachidonic acid AA metabolites Immunosuppression and acute phase reactants ↓ cytokines, lymphokines ↓ Adhesion molecules ↓ Histamine, Leukotrienes 19 Suppression of both humoral and cellular immune response. Multiple mechanisms of both inflammatory and immunological effects. Female Reproductive Hormones SERMs MOA: Selective estrogen receptor modulators (SERMs) compete with estradiol for hypothalamic estrogen receptors, blocking the negative feedback control pathways. Treatment with SERMs therefore increases the release of gonadotropin releasing hormone (GnRH), in turn increasing the release of both FSH and LH. FSH and LH then stimulate the ovaries to develop follicles, produce estrogens that then induce the FSH/LH rise from the pituitary. SERMs are usually given in the follicular phase of the menstrual cycle. The SERMs also have estrogen agonist effects as well as antagonistic effects in the ovary, endometrium, cervix, bone and mammary tissues. With Clomiphene, the estrogen agonist effects on the HP axis are secondary to the antagonist effects, while with raloxifene, the effects on bone and lipid metabolism are estrogen agonistic and the effects on the uterus and mammary tissue are antagonistic. Aldosterone Cholesterol Pregnenolone Corticosterone Progesterone 17-α-OH- Pregnenolone 17-α-OH- Progesterone Dehydroepiandrosterone Androstenedione Androstenediol Testosterone Cortisol Estrone Estradiol Dihydrotestosterone 20 Insulin Route SubQ Onset 15 min Peak 1 hr Duration 3-4 hr Type Rapid/Aspart SubQ 15 min. 30-90 min 3-4 hr Rapid/Lispro 15 min. 10-20 min 30-90 min 2 hr 3-4 hr Rapid/ Glulisine Rapid Insulin glulisine, recombinant: Apidra® SubQ 30-60 min 2-4 hr Unknown Short/ Regular Insulin IV 10-30 min 1-3 hr 15-30 Unknown min 6-8 hr 12-16 hr Short/ Regular Insulin Intermediate/ Lente/NPH/ Isophane Humulin R, Iletin II Regular, Novolin R, Penfill, Velosulin BR Canadian names: Insulin-Toronto, Novolin ge Toronto. Mixed insulins as needed Inhalation SubQ SubQ 60-60 min 6-10 hr 6 hr 24 hr Names Insulin Aspart (rDNA): NovoLog® Insulin Aspart (rDNA)+ Insulin Aspart protamine: NovoLogMix 70/30® Insulin (lispro): Humalog® Insulin glulisine recombinant: Apidra® Insulin lispro protamine: Humulog Mix 50/50® Insulin inhalation (rDNA): Exubera® Lente: Humulin L, Lente Iletin II NPH/Isophane: Humulin N, Novolin N, NPHN, NPH Iletin II Canadian names: Novolin ge Lente Long/ Humulin U, Novolin ge Ultralente, Novolin U, Ultralente Ultralente U Very Lantus Long//Glargine 21