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PHARMACOLOGY

Pharmacology flash cards

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  • 1. PHARMACOLOGY
  • 2. ANALGESIC & ANTIMIGRAINE
  • 3. Butorphanol Dihydroergotamine Fentanyl Meperidine Methadone Naloxone Propoxyphene Sumatriptan Tramadol Methadone Morphine
  • 4. BUTORPHANOL Opioid analgesic Mixed opioid agonist- antagonist Partial agonist or antagonist @ opioid receptors Dysphoria Nightmares w/drawal in pts dependent on full opioid agonists AVOID MAOI Potentially fatal Agonist @ receptors @ spinal & supraspinal sites Inhibits spinothalamic pain neurotransmission Moderate-severe pain Admin intranasally respiratory depression, constipation, dependence than full receptor agonists
  • 5. DIHYDROERGOTAMINE Antimigraine Ergot alkaloid 5-HT 1B/1D receptor agonist Activates 5-HT 1B/1D receptors Pial & dural vessel N, V Stiff neck, shoulder, extremities Leg weakness Numbness & tingling in fingers & toes Pial & dural vessel constriction Presynaptic inhibition of trigeminal peptide neurotransmitter release Inhibitions brainstem activation of trigeminal neurons Vascular HA Migraine & cluster Injection or nasal spray
  • 6. FENTANYL Opioid analgesic Phenylpiperidine Activates opioid receptors Inhibits pain Sedation Confusion Respiratory depression Anorexia N, V ConstipationInhibits pain transmission @ spinal & supraspinal sites Chronic pain Breakthrough for cancer pain Transdermal patch Constipation AVOID MAOI in past 14d
  • 7. MEPERIDINE Opioid analgesic Strong opioid agonist Activates opioid receptors Inhibits pain Confusion Sedation Constipation N, V Dependence Toxic metabolite CNS excitation, convulsions, tremorsInhibits pain transmission Generalized CNS depression Moderate-severe pain Analgesia during labor Preoperative sedation Lacks antitussive activity tremors AVOID MAOI Potentially fatal
  • 8. METHADONE Opioid analgesic Strong opioid agonist Activates opioid receptors Inhibits pain Respiratory depression Constipation Confusion Sedation AVOID MAOI Inhibits pain transmission Suppresses opioid w/drawl Sx w/ euphoria or dependence Moderate-severe pain Prevention of opioid abuse Orally, once per day
  • 9. MORPHINE Opioid analgesic Strong opioid receptor agonist Activates receptors cAMP Opens K & closes Ca channels Sedation Confusion Hypotension Constipation Respiratory depression AVOID MAOI w/ 14 d Potentially fataOpens K & closes Ca channels release substance P Inhibits pain @ spinal & supraspinal sites Severe pain w/ MI Pulmonary edema Active metabolite Morphine glucuronate Potentially fata
  • 10. NALOXONE Opioid antagonist Opioid receptor antagonist Blocks opioid , , receptors Rapidly reverses effects ofRapidly reverses effects of opioid agonists Opioid OD, dependence Short half-life needs repeated doses
  • 11. PROPOXYPHENE Opioid analgesic Weak opioid agonist Activates opioid receptors Inhibits pain Dizziness Weakness N dependence Inhibits pain transmission Mid-moderate pain Combined w/ acetaminophen or aspirin
  • 12. SUMATRIPTAN Antimigraine 5-HT 1B/1D receptor agonist Activates 5-HT 1B/1D receptors Pial & dural vessel constriction Presynaptic inhibition of Dizziness Vertigo Tingling Warm sensation Tight feeling head & chest Coronary vasospasm AVOID MAOI Presynaptic inhibition of trigeminal peptide neurotransmitter release Inhibitions brainstem activation of trigeminal neurons Vascular HA Migraine & cluster Oral, nasal, & subQ MAOI SSRI
  • 13. TRAMADOL Analgesic Dual action Activates opioid receptors Inhibits neuronal Dizziness HA Constipation Lowers seizure threshold AVOID MAOIInhibits neuronal reuptake 5-HT & NE inhibition of pain Moderate pain Chronic pain Naloxone reverses some but NOT all Sx AVOID MAOI risk seizures w/ high doses Penicillins Phenothiazines
  • 14. ANESTHETICS
  • 15. Benzocaine Bupivacaine Halothane Ketamine Lidocaine Midazolam Nitrous oxide Propofol Sevoflurane Lidocaine
  • 16. BENZOCAINE Local anesthetic Ester-type Blocks Na channels & nerve conduction Topical anesthetic Pain Cross-sensitivity w/ other ester-type anesthetics Pain Itching Inflammation Burns Insect bites Contact dermatitis Wounds Irritates skin when 1st applied Use caution w/ sunburn & large areas of skin
  • 17. BUPIVACAINE Local anesthetic Amide-type Blocks Na channels & nerve conduction Cross-sensitivity w/ amide-type anesthetics & nerve conduction Local or regional anesthetic Surgical Diagnostic Obstetrical therapeutic
  • 18. HALOTHANE General anesthetic Inhalational, halogenated hydrocarbon Potentiates GABA binding to GABA-A Cl ion Sensitizes heart to catecholamine-induced cardiac arrhythmia Hepatotoxic Fluoride metabolites binding to GABA-A Cl ion channel Suppresses sensory processing in thalamus General anesthetic High blood:gas partition coefficient Slow rate of induction & recovery
  • 19. KETAMINE IV anesthetic Glutamate antagonist Blocks glutamate NMDA receptors Dissociate anesthesia Analgesia Immobility Delirium Hallucination Irrational behavior during recovery BP Immobility Amnesia Does NOT depression respiration or cause LOC Anesthesia Minor surgical & diagnostic procedures Children
  • 20. LIDOCAINE Local anesthetic Amide-type Blocks Na channels & nerve conduction Topical Cross-reactivity w/ amide- type anesthetics Topical Infiltration Nerve block Epidural Spinal anesthesia Eutectic mixture Lidocaine & prilocaine Anesthetize intact skin for venipuncture IV cannulation Circumcism
  • 21. MIDAZOLAM Sedative-hypnotic- anxiolytic Short-acting BZDP Potentiates GABA binding to GABA-A Cl Apnea Laryngospasm Respiratory depression Cardiac arrest binding to GABA-A Cl ion channel Sedation Hypnosis Amnesia Preoperative sedation & anxiolysis Sedation of mechanically vented pts
  • 22. NITROUS OXIDE Inhalation general anesthetic Anesthetic gas Potentiates GABA binding to GABA-A Cl ion channelion channel Suppresses sensory processing in thalamus Minor surgery & dental procedures Rapid induction & recovery Euphoria laughing gas
  • 23. PROPOFOL General anesthesia IV anesthetic Diisopropyl phenol Potentiates GABA binding GABA-A Cl ion channel Hypnosis Bradycardia Hypotension channel Hypnosis Anesthesia Amnesia NO analgesic effect Intubation & maintenance of general anesthesia Sedation of intubated pts in ICU
  • 24. SEVOFLURANE General anesthetic Inhalation anesthetic Potentiates GABA binding to GABA-A Clbinding to GABA-A Cl channel Suppresses sensory processing in thalamus Causes LOC General anesthesia
  • 25. ANTI-INFECTIVE
  • 26. Acyclovir Albendazole Amantadine Amoxicillin-clavulanate Amphotericin B Cefepime Cetriaxone Ciprofloxacin Clindamycin DoxycyclineAmphotericin B Azithromycin Aztreonam Caspofungin Cefazolin Doxycycline Efavirenz Enfuvirtide Erythromycin Ethambutol
  • 27. Foscarnet Fosfomycin Ganciclovir Gentamicin Griseofulvin Linezolid Mefloquine Metronidazole Mupirocin NafcillinGriseofulvin Imipenem-cilastatin Isoniazid Itraconazole Ivermectin Levofloxacin Nafcillin Nitrofurantoin Oseltamivir Paromomycin Penicillin G
  • 28. Pentamidine Piperacillin-tazobactam Praziquantel Primaquine Pyrimethamine Rifampin Ritonavir-lopinavir Streptomycin Terbinafine TrifluridinePyrimethamine Pyrantel Quinine Quinpristein-dalfopristin Ribavirin Trifluridine TMP-SMX Vancomycin Zidovudine
  • 29. ACYCLOVIR Antiviral Nucleoside analogue Converted to acyclovir triphosphate by viral & host cell kinases Incorporated into DNA by Dizziness Diarrhea N Nephrotoxicity Probenecid serum levels Incorporated into DNA by viral DNA polymerase causing DNA chain termination HSV2 Herpes zoster Shingles Chickenpox varicella viral shedding, pain, & healing time
  • 30. ALBENDAZOLE Antihelmintic Benzimidazole Binds & inhibits polymerization of tubulin dimmers to form cytoplasmic microtubules Impairs glucose uptake & deplete glycogen stores GI distress Constipation or diarrhea Hepatitis & hematologic toxicity w/ high doses Intestinal nematode infections Hookworm Pinworm Whipworm Ascariasis Capillariasis Trichinosis Use w/ corticosteroid Cysticercosis & echinococcus Microsporidiosis
  • 31. AMANTADINE Anti-influenza, antiparkinson Tricyclic amine Inhibits influenza-A M2 proton channel & Ataxia Dizziness Insomnia Skin mottling & livedo reticularis Blurred vision M2 proton channel & acidification of virus particle Prevents viral protein- protein dissociation & uncoating of viral particles Influenza A Blurred vision Dry mouth
  • 32. AMOXICILLIN-CLAVULANATE -lactam ABX Extended spectrum aminopenicillin & -lactamase inhibitor Amoxicillin Binds PBP Inhibits cross-linking of cell wall peptidoglycan Diarrhea Superinfection Pseudomembranous colitis Allergic rxn Rash Serum sickness anaphylaxis Probenecid inhibits renal tubularInhibits cross-linking of cell wall peptidoglycan Clavulanate Inhibits class-A -lactamase Protects amoxicillin from destruction NOT antimicrobial by itself Respiratory tract infections Otitis, sinusitis, pneumonia Skin or skin structure infections Bite wounds Probenecid inhibits renal tubular excretion serum levels
  • 33. AMPHOTERICIN B Antifungal Polyene ABX Binds ergosterol & membrane permeability Leakage of cell contents Chills Fever Diarrhea N, V Nephrotoxicity Hypokalemia toxicity w/ cyclosporine,Leakage of cell contents Candidiasis Cryptococcal meningitis Aspergillosis Blastomycosis Coccidioidomycosis Histoplasmosis Mucormycosis toxicity w/ cyclosporine, antineoplastics Thiazides, & corticosteroids hypokalemia
  • 34. AZITHROMYCIN Macrolide Protein synthesis inhibitor Binds 50s ribosome Prevents peptide elongation & translocation from acceptor site to peptidyl siteacceptor site to peptidyl site Respiratory infections d/t strep, pneumo, H. influenzae, Legionella Otitis media, sinusitis Single-dose Tx for chlamydial urethritis, chancroid, MAI infections
  • 35. AZTREONAM -lactam ABX Monobactam Binds PBP including transpeptidase Inhibits cross-linking Thrombophlebitis Allergic rxn Inhibits cross-linking of cell wall peptidoglycan Drug resistant gram (-) infections including Pseudomonas aeruginosa & Enterobacteriaceae
  • 36. CASPOFUNGIN Antifungal Echinocandin Inhibits synthesis of cell wall component -1,3-D-glucan HA Fever Phlebitis Abnormal LFTs -1,3-D-glucan Candida albicans Invasive aspergillosis IV admin Not absorbed well by gut
  • 37. CEFAZOLIN -lactam ABX 2nd generation cephalosporin Binds PBP including transpeptidase Inhibits cross-linking of cell wall peptidoglycan Rash Diarrhea Pseudomembranous colitis Superinfection Probenecid inhibits excretion & serum levels wall peptidoglycan Surgical wound infections Infections d/t Staph, strep, E. coli, Klebsiella pneumoniae, Proteus mirabilis NOT active against MRSA
  • 38. CEFEPIME -lactam ABX 4th generation cephalosporin Binds multiple PBP Inhibits cross-linking of Rash Diarrhea Pseudomembranous colitis Superinfection Probenecid inhibits excretion & serum levels Inhibits cross-linking of cell wall peptidoglycan Resistant to many - lactamases Drug-resistant gram (-) bacteria Citrobacter Enterobacter Probenecid inhibits excretion & serum levels
  • 39. CEFTAZIDIME -lactam ABX 3rd generation cephalosporin Binds PBP including transpeptidase Inhibits cross-linking of cell wall peptidoglycan Rash Diarrhea Pseudomembranous colitis Superinfection Probenecid inhibits excretion & serum levels wall peptidoglycan Gram (+), gram (-), & anaerobics Pseudomonas aeruginosa Pneumonia, meningitis, UTI, skin structures, bones, jts
  • 40. CETRIAXONE -lactam ABX 3rd generation cephalosporin Binds PBP including transpeptidase Inhibits cross-linking of cell wall peptidoglycan Rash Diarrhea Pseudomembranous colitis Superinfection Probenecid inhibits excretion & serum levels wall peptidoglycan Infection d/t Pneumococci, gonococci, meningococci, H. influenzae, Moraxella catarrhalis, Borrelia burgdorferi Single IM injection Tx acute otitis media or gonorrhea
  • 41. CIPROFLOXACIN Antibacterial Fluoroquinolone Inhibits bacterial DNA topoisomerase type II (DNA gyrase) & type IV Prevents DNA replication & separation of chromosomes Insomnia Diarrhea N Absorption by cations Antacids Iron Zinc bismuthseparation of chromosomes Urinary tract, prostate, intraabdominal w/ metronidazole, bone or jt, skin Inhalational anthrax Gonorrhea Infectious diarrhea Gram (+), gram (-), Pseudomonas aeruginosa bismuth
  • 42. CLINDAMYCIN Aminosugar ABX Protein synthesis inhibitor Binds 50s ribosome C. difficile superinfection Diarrhea Pseudomembranous colitis Prevents translocation of nascent peptide from acceptor site to peptidyl site Strep, staph, gram (+) Acne vulgaris Anaerobes including Bacteroides
  • 43. DOXYCYCLINE Tetracycline ABX Protein synthesis inhibitor Binds 30s ribosome Reversibly inhibits binding of transfer RNA to acceptor site AVOID Pregnancy & children > 8 y/o Outdated preparations are nephrotoxic Permanent teeth discoloration Photosensitivity Diarrhea Rickettsia, Chlamydia, Mycoplasma, Borrelia Acne Cholera Gonorrhea & syphilis in PCN allergic pts Brucellosis & ehrlichiosis Diarrhea N, V
  • 44. EFAVIRENZ Antiretroviral Non-nucleoside reverse transcriptase inhibitor Binds reverse transcriptase & disrupts catalytic site N Rash Drowsiness Depression transcriptase & disrupts catalytic site HIV in combo w/ nucleoside reverse transcriptase inhibitor synergistic High fat meal absorption
  • 45. ENFUVIRTIDE Antiretroviral HIV fusion inhibitor Binds HIV virus gp41 & blocks fusion of HIV Injection site rxn Rotate sites daily & blocks fusion of HIV w/ host cells CD4 Thelper lymphocytes Drug-resistant HIV
  • 46. ERYTHROMYCIN Macrolide ABX Protein synthesis inhibitor Binds 50s ribosome Prevents peptide elongation & translocation Activates motilin receptors causing uncoordinated peristalsis Anorexia N, V Prevents peptide elongation & translocation from acceptor site to peptidyl site Pharyngitis, otitis media, sinusitis, pneumonia d/t Strep, pneumococci, Mycoplasma, Chlamydia, Legionella, MAI
  • 47. ETHAMBUTOL Antitubercular Synthetic butanol derivative Bacteriostatic against Dose-related retrobulbar optic neuritis Impaired red-green color discrimination Monitor pts colorBacteriostatic against mycobacteria Inhibits RNA synthesis M. tuberculosis MAI Monitor pts color discrimination regularly Gouty arthritis
  • 48. FOSCARNET Antiviral Pyrophosphate Blocks pyrophosphate- binding site on viral HA Diarrhea V Renal failure Hypocalcemia Hypokalemia Hypomagnesemiabinding site on viral DNA polymerase Prevents attachment of nucleotide precursors to DNA CMV retinitis in HIV pts Acyclovir-resistant HSV in immunocompromised Hypomagnesemia Anemia Arthralgia Myalgia Pentamidine causes life- threatening hypocalcemia
  • 49. FOSFOMYCIN ABX Cell wall synthesis inhibitor Inhibits enopyruvyl transferase & addition of phosphenolpyruvate transferase & addition of phosphenolpyruvate to N-acetylglucosamine to form N- acetylmuramic acid Cystitis d/t E. coli or Enterococcus faecalis Single dose Tx for UTI
  • 50. GANCICLOVIR Antiviral Nucleoside analogue Converted to ganciclovir visual acuity Neutropenia Thrombocytopenia Anemia Converted to ganciclovir triphosphate Inhibits viral DNA polymerase CMV infection in immunocompromise d & transplants
  • 51. GENTAMICIN Aminoglycoside ABX Protein synthesis inhibitor Binds 30s ribosome Prevents initiation of protein synthesis Misreading of genetic code Nephrotoxicity Ototoxicity Vestibular & cochlear w/ loop diuretics Misreading of genetic code Gram (-) bacilli including Enterobacteriaceace & P. aeruginosa Strep, enterococcal, & staph infections Monitor serum levels
  • 52. GRISEOFULVIN Antifungal Fungistatic ABX Deposits in keratin precursor cells of skin, hair, & nails HA Induces CYP450 Reduces plasma levels warfarin & OCP skin, hair, & nails Disrupts microtubules & mitotis of dermatophytes Dermatophyte infections NOT Candida
  • 53. IMIPENEM-CILASTATIN -lactam ABX Carbapenem ABX & dehydropeptidase inhibitor Imipenem Binds PBP & inhibits cross- linking cell wall peptidoglycan Allergic rxns Diarrhea V Seizures risk w/ ganciclovir or cyclosporine Probenecid inhibits secretion & serum levelspeptidoglycan Cilastatin Inhibits renal dehydropeptidase & degradation of imipenem Endocarditis, pneumonia, UTI, pelvic, abdominal d/t aerobic & anaerobic Probenecid inhibits secretion & serum levels
  • 54. ISONIAZID Antitubercular Nicotinic acid derivative Reduces catalase- peroxidase Hepatitis Toxic metabolite acetyl- hydrazine Peripheral neuropathy Vit. B6 deficiency peroxidase Inhibits synthesis of mycolic acid component of cell wall TB Bimodal distribution d/t fast & slow acetylation Inactivates vit. B6
  • 55. ITRACONAZOLE Antifunal Synthetic triazole Inhibits 14-- demethylase CYP450 enzyme that GI distress Rash Hepatitis CYP450 enzyme that converts lanosterol ergosterol Blastomycosis, candidiasis, coccidioidomycosis, histoplasmosis Onychomycosis nail beds
  • 56. IVERMECTIN Antiparasitic Antihelmintic ABX Activates glutamate- gated Cl ion channel Pharyngeal m. Vertigo Sedation Pharyngeal m. hyperpolarization & paralysis Strongyloidiasis Cutaneous larva migrans Onchocerciasis filiariasis W. bancrofti
  • 57. LEVOFLOXACIN Antibacterial Fluoroquinolone Inhibits bacterial DNA topoisomerase type II (DNA gyrase) & type IV Prevents DNA replication &Prevents DNA replication & separation of chromosomes Community-acquired pneumonia UTI Gynecologic & skin infections Gram (+), gram (-), P. aeruginosa, Mycoplasma, Mycobacterium
  • 58. LINEZOLID Antibacterial Oxazolidinone protein synthesis inhibitor Binds 23s ribosomal Inhibits MAO Binds 23s ribosomal RNA of 50S subunit Prevents formation of 70s initiation complex VRE, MS/MRSA, PCN- sensitive pneumococci
  • 59. MEFLOQUINE Antimalarial 4-quinolone methanol derivative Inhibits erythrocytic schizogony Inhibit nucleic acid synthesis Neuropsychiatric syn Hallucination Anxiety Confusion Seizure Coma Inhibit nucleic acid synthesis Malaria Chloroquine- susceptible/resistant trains of P. falciparum & P. vivax Perform CBC during chronic prophylactic Tx
  • 60. METRONIDAZOLE Antiprotozoal Nitroimidazole Reduced by pyruvate:ferredoxin to form nitro-free GI pain Anorexia N Dizziness Alcohol causesto form nitro-free radicals that attack DNA & proteins Amebiasis, giardiasis, trichomoniasis Balantidium coli, C. difficile, B. fragilis Alcohol causes disulfiram-like effect
  • 61. MUPIROCIN ABX Protein synthesis inhibitor Competes w/ isoleucine for binding bacterial isoleucyl tRNA for binding bacterial isoleucyl tRNA synthetase Prevents addition of isoleucine during protein synthesis Impetigo by staph or strep Eradicate nasal colonization of MRSA Infected traumatic skin lesions
  • 62. NAFCILLIN -lactam ABX Antistaphylococcal, penicillinase-resistant penicillin Binds PBP Diarrhea Superinfection Pseudomembranous colitis Allergic rxn Rash Serum sickness AnaphylaxisBinds PBP Inhibits cross-linking of cell wall peptidoglycan Methicillin-sensitive penicillinase producing staph Bone, jt, UTI, respiratory, skin, endocarditis, meningitis Anaphylaxis Probenecid inhibits renal tubular secretion & serum levels
  • 63. NITROFURANTOIN Urinary tract antibacterial Nitrofuran Inhibits bacterial Anorexia N, V Neurotoxicity Pneumonitis Inhibits bacterial enzymes UTI E. coli, S. saprophyticus Probenecid inhibits urinary excretion
  • 64. OSELTAMIVIR Antiviral Neuraminidase inhibitor Inhibits influenza A &Inhibits influenza A & B neuraminidase Prevents release & spreading of viral particles Influenza A & B
  • 65. PAROMOMYCIN Antiprotozoal Aminoglycoside ABX Inhibits protein synthesis Nephrotoxic & ototoxic if given IV synthesis Intestinal amebiasis Cryptosporidiosis in immunocompromised pts
  • 66. PENICILLIN G -lactam ABX Narrow-spectrum penicillin Binds PBP Diarrhea Superinfection Pseudomembranous colitis Allergic rxn RashBinds PBP Inhibits cross-linking of cell wall peptidoglycan Strep, pneumococcal, meningococcal Syphilis Rash Serum sickness Anaphylaxis Probenecid inhibits renal tubular secretion
  • 67. PENTAMIDINE Antiprotozoal Amidino-pentane derivative Disrupts nucleic acid Nephrotoxic Hematologic toxicity Hypoglycemia Allergic rxn Anaphylaxis Disrupts nucleic acid synthesis in protozoa P. carinii Early stage African trypanosimiasis sleeping sickness Anaphylaxis Erythromycin fatal arrhythmias
  • 68. PIPERACILLIN-TAZOBACTAM -lactam ABX Antipseudomonal penicillin & -lactamase inhibitor Piperacillin Binds PBP Inhibits cross-linking of cell wall peptidoglycan Diarrhea Superinfection Pseudomembranous colitis Allergic rxn Rash Serum sickness Anaphylaxis Inhibits cross-linking of cell wall peptidoglycan Tazobactam Inhibits class A -lactamases Gram (-) bacilli, P. aeruginosa Probenecid inhibits renal tubular secretion
  • 69. PRAZIQUANTEL Antihelmintic Isoquinoline derivative Ca permeability of schistosome tegument Malaise Anorexia Drowsiness dizziness schistosome tegument Contraction & exposing antigens to host immunity Schistosomiasis Chinese liver fluke Lung fluke Cestodes tapeworms
  • 70. PRIMAQUINE Antimalarial 8-aminoquinoline Converted to oxidizing quinoline- Hemolytic anemia in G6PD deficiency methemoglobinemia oxidizing quinoline- quinone intermediates Eradicate exo- erythrocytic forms of P. vivax & P. ovale
  • 71. PYRIMETHAMINE Antiprotozoal Folate reductase inhibitor Inhibits folate reductase Folate deficiency in protozoa Malaria in combo w/ sulfadoxine N Anorexia Hypersensitivity rxn Malaria in combo w/ sulfadoxine Toxoplasmosis in combo w/ sulfadoxine NOT effective against P. vivax
  • 72. PYRANTEL Antihelmintic Pyrimidine analogue Activates cholinergic nicotinic receptors in Abdominal cramps Anorexia Diarrhea V nicotinic receptors in somatic m. of nematodes Produces depolarizing NM blockade Ascariasis Hookworm & pinworm
  • 73. QUININE Antimalarial 4-aminoquinoline Binds plasmodial DNA & prevents replication & transcription during erythrocytic schizogony Abdominal cramps Diarrhea V Cinchonism Tinnitus Blurred vision& transcription during erythrocytic schizogony Chloroquine-resistant malaria Admin w/ doxycycline or pyrimethamine-sulfadoxine Blurred vision Metabolism Cimetidine inhibits Rifampin induce
  • 74. QUINUPRISTIN-DALFOPRISTIN Streptogramin ABX Protein synthesis inhibitor Binds 50s ribosomal subunit Infusion site rxn subunit Quinupristin Inhibits aminoacyl tRNA synthesis & addition of AA Dalfopristin Inhibits peptidyl transferase VRE, MS/MRSA
  • 75. RIBAVIRIN Broad-spectrum antiviral Guanosine analogue Converted to ribavirin triphosphate Depletes guanosine Anemia Hypotension Cardiac arrest Depletes guanosine triphosphate Inhibits viral RNA & protein synthesis RSV in infants or children Chronic hepatitis C Viral hemorrhagic fever Lass fever
  • 76. RIFAMPIN Antitubercular Rifampin derivative Inhibits DNA-dependent RNA polymerase TB Red discoloration of tears, urine, saliva, sweat Abdominal pain V Diarrhea Hepatitis Induces CYP450TB Leprosy Prophylaxis meningococcal meningitis & H. flu B infections Induces CYP450 levels Warfarin Theophylline Itraconazole Steroids Opioids Phenytoin Verapamil
  • 77. RITONAVIR-LOPINAVIR Antiretroviral HIV protease inhibitor Inhibits HIV protease & conversion of gag- Anorexia V Altered taste Abnormal thinking Hyperlipidemia Hyperlgycemia& conversion of gag- pol polyprotein to functional proteins Ritonavir lopinavir levels HIV in combo w/ nucleoside reverse transcriptase inhibitor Hyperlgycemia
  • 78. STREPTOMYCIN Aminoglycoside Protein synthesis inhibitor Binds 30s ribosome Prevents initiation of Nephrotoxic Ototoxic w/ loop diuretics Prevents initiation of protein synthesis Misreading of genetic code Drug-resistant TB Plague Tularemia IV admin
  • 79. TERBINAFINE Antifungal Allylamine Inhibits squalene oxygenase & formation of squalene epoxide during fungal Itching Rash Diarrhea Anorexia Metabolism Cimetidine inhibitsof squalene epoxide during fungal membrane ergosterol synthesis Topical Tinea corporis, cruris, pedis, versicolor Oral Onychomycosis fungal nail infection Cimetidine inhibits Rifampin induce
  • 80. TRIFLURIDINE Antiviral Thymidine analogue Inhibits HSV DNA polymerase Ocular irritation Redness Itching polymerase Herpetic keratitis Keratoconjunctivitis Topical ocular admin
  • 81. TRIMETHOPRIM-SULFAMETHOXAZOLE Antibacterial Folate antagonist Sulfamethoxazole Inhibits folate synthesis N, V Rash Stevens-Johnson syn Allergic rxn Anemia Hemolytic anemia Megalobalstic anemia Inhibits folate synthesis Trimethoprim Inhibits folate reduction UTI, travelers diarrhea Shigella enteritis P. carinii & Nocardia pneumonia Megalobalstic anemia Leukopenia Thrombocytopenia Crystalluria Added folate deficiency w/ phenytoin or MTX
  • 82. VANCOMYCIN Glycopeptide ABX Cell wall synthesis inhibitor Binds D-alanyl-D- alanine portion of Red man syn Extensive rate of infusion Erythematous rash on face & upper body Ototoxicity Vestibular & cochlear alanine portion of peptidoglycan Prevents cross-linking of D-alanine & pentaglycine chain MRSA, penicillin-resistant enterococci, C. difficile
  • 83. ZIDOVUDINE Antiretroviral Nucleoside reverse transcriptase inhibitor Activated nucleotide triphosphate incorporated into DNA causing chain termination Anemia termination HIV Prevent maternal-fetal HIV transmission 1st line Tx for HIV infections Zidovudine w/ lamivudine or emtricitabine & efavirenz or lapinavir-ritonavir
  • 84. ANTINEOPLASTIC
  • 85. Anastrozole Bleomycin Busulfan Carmustine Cisplatin Imatinib Leuprolide Meraptopurine Methotrexate PaclitaxelCisplatin Cyclophosphamide Doxorubicin Etoposide Fluorouracil Gemtuzumab ozogamicin Paclitaxel Tamoxifen Trastuzumab Vincristine
  • 86. ANASTROZOLE Estrogen antagonist Nonsteroidal aromatase inhibitor Inhibits aromatase & conversion to estrone N HA Hot flashes Back pain conversion to estrone precursor to estradiol Lowers estrogen levels Halts progression of estrogen-sensitive breast cancers Breast cancer in postmenopausal women
  • 87. BLEOMYCIN Antitumor DNA intercalating Complexes iron- forming oxygen free radicals that cause Pneumonitis & pulmonary fibrosis Hyperpigmentation Mucocutaneous toxicity Hematology toxicity radicals that cause single strand breaks G2 phase specific Lymphomas SCC Testicular carcinoma Choriocarcinoma
  • 88. BUSULFAN Antineoplastic Alkyl sulfonate bifunctional alkylating agent Cross-links DNA strands by covalently bonding N, V Myelosuppression Pulmonary fibrosis by covalently bonding guanine residues Prevents DNA replication & transcription CML Use w/ cyclophosphamide prior allogenic hematopoietic progenitor cell transplant for CML
  • 89. CARMUSTINE Antineoplastic Nitrosurea bifunctional akylating agent Cross-links DNA strands by covalently bonding guanine residues N, V Hepatotoxicity Anemia Leucopenia Thrombocytopenia Pulmonary fibrosis guanine residues Prevents DNA replication & transcription Brain tumors Myeloma Lymphoma Causes prolonged myelosuppression
  • 90. CISPLATIN Antineoplastic Platinum compound Forms reactive metabolites that covalently bond DNA Severe N, V Ototoxicity & tinnitus Hypocalcemia Hypokalemia Hypomagnesemia Anemia covalently bond DNA bases & cross-link DNA strands Testicular, ovarian, cervical, bladder, lung, head/neck cancers Less bone marrow suppression Anemia
  • 91. CYCLOPHOSPHAMIDE Antineoplastic Nitrogen mustard bifunctional akylating agent Cross-links DNA strands by covalently bonding guanine residues Anorexia N, V Hemorrhagic cystitis & hematuria Alopecia Thrombocytopenia Leukopenia Anemia Prevents DNA replication & transcription Hodgkins ds Lymphomas, myeloma Leukemia Ovarian & breast tumors RA Converted to active metabolites by CYP enzymes Rifampin induces CYP & toxicity
  • 92. DOXORUBICIN Antitumor DNA intercalating agent Inserts b/w DNA bases Causes deformation & uncoupling Complexes iron forming hydroxyl free radicals that Colors urine red Cardiomyopathy dose- limiting Anemia Leukopenia Thrombocytopeniahydroxyl free radicals that cause strand breaks Inhibits topoisomerase II Causes strand breaks S phase specific Breast, ovarian, bladder tumors Bronchogenic carcinoma Lymphoma & leukemia Thrombocytopenia Diarrhea V Stomatitis Alopecia
  • 93. ETOPOSIDE Antineoplastic Podophyllotoxin, topoisomerase inhibitor Inhibits mammalian topoisomerase II & N, V Leukopenia Thrombocytopenia Alopecia topoisomerase II & prevents resealing of nicked DNA strands G2 phase specific Testicular, small cell lung carcinoma Lymphoma Leukemia
  • 94. FLUOROURACIL Antineoplastic Pyrimidine antimetabolite Converted to active nucleotide form Inhibits thymidylate Diarrhea V Stomatitis Alopecia Maculopapular rash AnemiaInhibits thymidylate synthetase S phase specific Colon, breast, rectal, gastric, pancreatic cancer Topical for basal cell carcinoma & actinic keratosis Anemia Leukopenia Thrombocytopenia
  • 95. GEMTUZUMAB OZOGAMICIN Antineoplastic Monoclonal Ab & cytotoxic ABX calicheamicin Gemtuzumab Binds CD33 Ag on Severe myelosuppression & hypersensitivity rxn anaphylaxis Severe pulmonary rxns Chills FeverBinds CD33 Ag on hematopoietic cells & sequesters lysosomes where calicheamicin is released Calicheamicin Causes DNA dbl strand breaks CD33 (+) AML Fever N Dyspnea
  • 96. IMATINIB Antineoplastic Tyrosine kinase inhibitor Inhibits oncoprotein bcr- abl tyrosine kinase expressed by Philadelphia Cough Dyspnea Pharyngitis Pneumonia Abdominal pain Vexpressed by Philadelphia chromosome Inhibits leukemic cell proliferation & induced apoptosis CML Cause hematologic & cytogenetic remission V Petechiae Pruritis Rash Night sweats Myalgia Arthralgia Thrombocytopenia Neutropenia
  • 97. LEUPROLIDE Antineoplastic, agent for precocious puberty GnRH analogue Pulsatile admin FSH & LH release Continuous admin down- Transient in testosterone w/ 1st dose Use flutamide or other androgen antagonist Hot flashes Continuous admin down- regulates GnRH receptors & FSH & LH Central precocious puberty Advanced prostate cancer Endometriosis Uterine fibroids IM depot & implants for prostate cancer
  • 98. MERCAPTOPURINE Antineoplastic Purine antimetabolite Converted to nucleotide triphosphate by phosphoribosyl transferase Inhibits purine biosynthesis Cross-react w/ thioguanine Myelosuppression Hyperuricemia Hepatotoxicity Allopurinol inhibits degradationInhibits purine biosynthesis & salvage pathways S phase specific Acute leukemia CML Lymphomas Tumors that delete phosphoribosyl-transferase acquire resistance
  • 99. METHOTREXATE Antineoplastic Folate reductase inhibitor Inhibits dihydrofolate reductase Prevents formation of active folate & addition of single carbon units to DNA base precursors S phase specific N, V Stomatitis Hepatotoxicity Anemia Leukopenia Thrombocytopenia Nephropathy S phase specific Choriocarcinoma, trophoblastic tumors Leukemia Breast, head, neck, lung cancers Severe psoriasis RA Mycosis fungoides Leucovorin used to minimized hematologic toxicity & Tx OD
  • 100. PACLITAXEL Antineoplastic Mitotic inhibitor Binds tubulin & prevents depolymerization of microtubules of mitotic D N, V Alopecia Anemia Leukopenia Thrombocytopeniamicrotubules of mitotic spindle M phase specific Advanced ovarian cancer w/ cisplatin Non-small-cell lung cancer Metastatic ovarian or breast cancer Thrombocytopenia Peripheral neuropathy Arthralgia Myalgia
  • 101. TAMOXIFEN Antineoplastic Estrogen receptor antagonist & partial agonist Competes w/ estrogen for CI during pregnancy & lactation N Hot flashes Menstrual irregularitiesCompetes w/ estrogen for receptors in breast & other tissues Suppresses breast tumor growth Breast cancer & ductal carcinoma following surgery & radiation Advanced breast cancer Menstrual irregularities
  • 102. TRASTUZUMAB Antineoplastic Monoclonal Ab Binds human epidermal growth factor-2 (HER2) receptor on breast cancer cells Prevents receptor stim. & cell proliferation Abdominal pain Anorexia Diarrhea V Back pain Chills Feverproliferation Regression of breast cancer metastases Metastatic breast cancer w/ overexpression HER2 Combined w/ paclitaxel blood levels Fever Allergic rxns Doxorubicin risk of cardiotoxicity
  • 103. VINCRISTINE Antineoplastic Vinca alkaloid, mitotic inhibitor Binds tubulin & prevents polymerization of tubulin dimers forming microtubules of mitotic spindle N, V Alopecia Peripheral neuropathy mitotic spindle M phase specific Hodgkins ds Lymphoma Leukemia Neuroblastoma Rhabdomyosarcoma Wilms tumor
  • 104. AUTONOMIC & NEUROMUSCULAR
  • 105. Atenolol Atropine Dobutamine Edrophonium Epinephrine Pralidoxime Propranolol Pseudoephrine Pyridostigmine RocuroniumEpinephrine Phenoxybenzamine Phentolamine Phenylephrine Pilocarpine Rocuronium Sildenafil Succinylcholine Tamsulosin Terazosin
  • 106. ATENOLOL Sympatholytic, antihypertensive 1 receptor antagonist Bronchoconstriction w/ high doses b/c 1 blockade Additive 1 receptor antagonist Angina Post MI Hypertension Additive hypotension w/ nitrates
  • 107. ATROPINE Anticholinergic Muscarinic receptor antagonist Muscarinic receptor blocker Mydriasis & cycloplegia Warm, dry, flushed skin Tachycardia receptor blocker Bradycardia IBS Anticholinesterase poisoning Antisecretory agent Delirium Hallucinations
  • 108. DOBUTAMINE Sympathomimetic, cardiac stimulant 1 receptor agonist Selective 1 receptor agonist 1 > 2 > 1 Tachycardia Arrhythmia 1 > 2 > 1 Cardiac contractility & output Acute heart failure Cardiogenic shock Synergistic on cardiac output w/ nitroprusside
  • 109. EDROPHONIUM Diagnostic agent Cholinesterase inhibitor Reversible Muscarinic effects Miosis Salivation Reversible cholinesterase inhibitor Dx myasthenia gravis
  • 110. EPINEPHRINE Sympathomimetic, bronchodilator, vasopressor Nonselective adrenergic agonist Activates & HTN Tachycardia Ischemia Hyperglycemia Activates & receptors IP3 & cAMP 1 vasoconstrict & BP 1 HR, conduction, & contractility 2 vasodilate, BP, bronchodilate Cardiac arrest, V fib Shock, asthma COPD
  • 111. PHENOXYBENZAMINE Vasodilator Irreversible receptor antagonist receptor Postural hypotension Hypotension w/ blockers & Ca channel blockers receptor antagonist 1 > 2 Presurgical Tx of HTN d/t pheochromocytoma blockers
  • 112. PHENTOLAMINE Vasodilator receptor antagonist Blocks 1 & 2 Hypotension Severe hypotension w/ Epi Blocks 1 & 2 receptors Control BP during surgical removal of pheochromocytoma IV admin only
  • 113. PHENYLEPHRINE Vasocontrictor, decongestant Selective 1 receptor agonist Rebound nasal congestion HTN MAOI cause severe HTN Activates 1 receptor Increase IP3 causing contraction of vascular smooth m. Nasal & ocular decongestant Dilate pupil for opthalmoscopy Mydriasis w/o cycloplegia Paralysis of
  • 114. PILOCARPINE Antiglaucoma, sialogogue Muscarinic receptor agonist Activates Miosis Blurred vision Accommodative spasm Activates muscarinic receptors in ciliary m. & salivary gland Sjogrens syn Glaucoma Ciliary m. aqueous humor Xerostomia Salivary gland salivation
  • 115. PRALIDOXIME Organophosphate antidote Cholinesterase reactivator Binds phosphorous & breaksbreaks organophosphate bond w/ cholinesterase Organophosphate toxicity Reverses muscle weakness
  • 116. PROPRANOLOL Sympatholytic, antihypertensive Nonselective receptor antagonist Blocks 1 & 2 receptors Bronchoconstriction Inhibits glycogenolysis Nightmares & depression receptors Angina HTN Benign tremor Migraine prophylaxis thyrotoxicosis Post-MI Highly lipophilic CNS effects
  • 117. PSEUDOEPHEDRINE Decongestant Indirect/direct- acting adrenergic receptor agonist Tachycardia CNS stim. BP MAOI cause severe HTN release NE directly activates adrenergic receptors causing vasoconstriction & cardiac stim. Allergic & viral rhinitis HTN
  • 118. PYRIDOSTIGMINE Antimyasthenic Cholinesterase inhibitor, cholinergic agonist Muscarinic effects Miosis Salivation Prolongs effects of succinylcholine Reversibly inhibits cholinesterase Tx myasthenia gravis Reverse nondepolarizing NM blockers succinylcholine
  • 119. ROCURONIUM Paralytic agent Nondepolarizing NM blockade Blocks nicotinic receptors in skeletal m. Respiratory m. paralysis Apnea in skeletal m. Skeletal m. relaxation for intubation, surgery, ECT Effects reversed by neostigmine & edrophonium
  • 120. SILDENAFIL Vasodilator Phosphodiesterase inhibitor Inhibits type 5 phosphodiesterase HA Nasal congestion Back pain Visual disturbances phosphodiesterase & degradation of cGMP vasodilation in corpus cavernosum d/t Ach release from sacral PNS neurons Erectile dysfunction
  • 121. SUCCINYLCHOLINE Paralytic agent Depolarizing NM blockade Binds nicotinic receptors causing prolonged depolarization of skeletal Respiratory m. paralysis Apnea depolarization of skeletal m. & paralysis Skeletal m. relaxation for intubation & surgery Transient m. fasciculations
  • 122. TAMSULOSIN Urologic agent Uroselective 1 receptor antagonist Blocks 1A Dizziness HA Postural hypotension Blocks 1A receptors in prostate Tx urinary outflow obstruction d/t prostatic hyperplasia Cimetidine increases blood levels & effects
  • 123. TERAZOSIN Antihypertensive, urologic agent Selective 1 receptor antagonist 1st dose syncope Blocks 1 receptors HTN Outflow obstruction d/t prostate hyperplasia
  • 124. CARDIOVASCULAR
  • 125. Acetazolamide Adenosine Amiloride Amiodarone Amlodipine Carvedilol Clonidine Hydrochlorothiazide Labetalol Mannitol Methyldopa Minoxidil Nesiritide NitroglycerinClonidine Digoxin Diltiazem Dofetilide Enalapril Esmolol Fenoldopam Furosemide Hydralazine Nitroglycerin Nitroprusside Propafenone Quinidine Sotalol Spironolactone Valsartan verapamil
  • 126. ACETAZOLAMIDE Diuretic Carbonic anhydrase inhibitor Inhibits interconversion of carbonic acid & bicarbonate Parasthesia Urinary stone formation bicarbonate NaHCO3 excretion Inhibit aqueous humor formation Hyperchloremic metabolic acidosis Tx open-angle glaucoma Mtn sickness Metabolic alkalosis
  • 127. ADENOSINE Antiarrhythmic Purine nucleoside, cardiac node membrane stabilizer Transient asystole Opens K channels & blocks Ca influx in SA & AV nodes Slows AV conduction AV refractory period Terminate SVT
  • 128. AMILORIDE K-sparring diuretic Epithelial Na channel blocker Blocks Na Channel Hyperkalemia Blocks Na Channel distal tubule & collecting duct Inhibits Na reabsorption & K excretion Prevent & Tx hypokalemia
  • 129. AMIDARONE Antiarrhythmic Cardiac ion channel blocker Blocks K, Na, Ca Hypo/hyperthyroidism Photosensitivity Blue-gray skin Corneal microdeposits Pulmonary fibrosis Blocks K, Na, Ca channels & receptors Prolongs repolarization refractory period Slows HR PR & QT intervals SVT, VT, VF
  • 130. AMLODIPINE Antihypertensive, antianginal Dihydropyridine Ca channel blocker Ca channel blocker in HA Edema Hypotension Effects w/ grapefruitCa channel blocker in vascular smooth m. Arteriolar vasodilation & coronary blood flow HTN Angina pectoris Effects w/ grapefruit juice
  • 131. CARVEDILOL Antihypertensive & heart failure Tx Nonselective adrenergic receptor agonist Orthostatic hypotension Dizziness Bradycardia Blocks 1, 2, 1 receptors Cause vasodilation HTN Heart failure remodeling
  • 132. CLONIDINE Antihypertensive 2 receptor agonist Central 2 receptor agonist sympathetic outflow Abrupt w/drawal severe rebound HTN Sedation Dry mouth sympathetic outflow from vasomotor center Inhibits pain neurotransmission in spinal cord HTN Opioid w/drawal
  • 133. DIGOXIN Cardiac stimulant Digitalis glycoside Inhibits Na/K ATPase IC Ca & cardiac Arrhythmias N, V Blurred vision Yellow vision IC Ca & cardiac contractility AV conduction AV refractory period Heart failure Serum levels assess dosage & toxicity
  • 134. DILTIAZEM Vasodilator, antiarrhythmic Non-dihydropyridine Ca channel blocker Block Ca channels in cardiac tissue & vascular Dizziness Hypotension Peripheral edema Constipation Gingival hyperplasia cardiac tissue & vascular smooth m. Vasodilation HR & conduction contractility HTN Angina pectoris SVT Grapefruit juice serum levels
  • 135. DOFETILIDE Antiarrhythmic K channel blocker Blocks delayed K channels in cardiac tissue Slows repolarization & QT prolongation Torsade de pointes Slows repolarization & prolongs refractory period QT interval AF, A flutter Monitor QT interval during initial dose titration
  • 136. ENALAPRIL Antihypertensive ACE inhibitor Inhibits ACE & formation of AT II Vasodilation aldosterone secretion Cough & angioedema Inhibits bradykinin degradation Hypotension Taste disturbances aldosterone secretion CO V remodeling survival in heart failure HTN Heart failure Post-MI progression of diabetic nephropathy
  • 137. ESMOLOL Antiarrhythmic Class II Selective 1 blocker Blocks SNS stim. SA & AV nodes HR Hypotension Bradycardia HR AV conduction AV refractory period Sinus tachycardia & SVT during/after surgery Rapidly metabolized by plasma esterase
  • 138. FENOLDOPAM Antihypertensive D1-like receptor agonist D1 receptor agonist serum K levels Monitor for hypokalemia D1 receptor agonist Arteriolar vasodilation Afferent & efferent renal arterioles renal blood flow Hypertensive emergencies
  • 139. FUROSEMIDE Loop-acting diuretic Membrane ion transport inhibitor Inhibits Na/K/2Cl cotransporter in ascending loop of Henle Blocks NaCl reabsorption Hypokalemia Metabolic alkalosis Hyperuricemia Hypomagnesemia ototoxicity of aminoglycoside ABX Blocks NaCl reabsorption Edema Heart failure HTN Hypercalcemia Ca excretion Na/K exchange in collecting duct aminoglycoside ABX
  • 140. HYDRALAZINE Antihypertensive. heart failure Vasodilator Alters IC Ca metabolism Relaxes arteriolar smooth m. Edema Reflex tachycardia & MI Lupus syndrome Relaxes arteriolar smooth m. vasodilation afterload Heart failure in combo w/ isosorbide dinitrate More effective than ACEI in black people Moderate-severe HTN
  • 141. HYDROCHLOROTHIAZIDE Antihypertensive Thiazide diuretic Inhibits NaCl transporter in distal Hypokalemia Metabolic alkalosis Hyperuricemia & gout excretion of lithium transporter in distal tubule excretion Na, K, Cl Ca excretion HTN Nephrogenic DI Nephrolithiasis
  • 142. LABETOLOL Antihypertensive Adrenergic & receptor antagonist Selective 1 & Postural hypotension Abrupt w/drawal cause life- threatening HTN, Selective 1 & nonselective 1, 2 blockers HTN threatening HTN, arrhythmias, or MI
  • 143. MANNITOL Diuretic Osmotic Diuretic Osmotic attraction of edematous & ocular Electrolyte imbalances Transient volume expansion Pulmonary edema or heart failure edematous & ocular fluid Filtered by glomerulus electrolyte excretion Oliguric renal failure Cerebral edema ICP Acute glaucoma
  • 144. METHYLDOPA Antihypertensive Adrenergic 2 receptor agonist Converted to active form methyl- Positive direct Coombs test form methyl- norepinephrine which activates central 2 receptor agonist SNS outflow from vasomotor center HTN HTN in pregnancy
  • 145. MINOXIDIL Antihypertensive, hair growth stimulant Vasodilator, K channel opener Opens K channels in vascular smooth m. Systemic admin. Reflex tachycardia Angina pericarditis Pulmonary HTN hypertrichosis vascular smooth m. Hyperpolarization m. relaxation vasodilation Stim. resting hair follicle growth follicles Severe HTN Topical for alopecia
  • 146. NESIRITIDE Heart failure Tx Recombinant human B- type natriuretic peptide Activate guanylate cyclase cGaMP Hypotension cGaMP Dilates venous & arterial smooth m. venous pressure, cardiac preload, vascular congestion, & dyspnea Decompensated heart failure
  • 147. NITROGLYCERIN Antianginal Organic nitrate Releases NO in vascular smooth m. HA Hypotension Syncope Reflex tachycardia smooth m. Vasodilation coronary blood flow myocardial O2 demand Angina pectoris Sublingual or lingual admin. Short half-life vasodilative effect of sildenafil, tadalafil, vardenafil
  • 148. NITROPRUSSIDE Antihypertensive Vasodilator Relaxes venous & arteriolar smooth m. Metabolized to CN & CN toxicity Hypotension HA Metabolized to CN & thiocyanate Tx toxicity w/ sodium nitrite & sodium thiosulfate HTN crisis Acute heart failure or cardiogenic shock Controlled hypotension during pregnancy
  • 149. PROPAFENONE Antiarrhythmic Class IC Na channel blocker Blocks Na channel in cardiac tissue Proarrhythmic 1st 2 wks Monitor ECG when starting Tx GI disturbances cardiac tissue conduction & prevent re-entry PR, QRS, & QT duration SVT & life-threatening V arrhythmias digoxin levels
  • 150. QUINIDINE Antiarrhythmic Class IA Na channel blocker Blocks Na & K channels in cardiac Cinchonism Blurred vision Tinnitus Photophobia levels w/channels in cardiac tissue conduction QRS & QT duration SVT & VT D-isomer = quinine, used to treat malaria pts levels w/ Amiodarone Cimetidine Diltiazem Verapamil Grapefruit juice
  • 151. SOTALOL Antiarrhythmic Class III K channel blocker Blocks K channels in cardiac tissue Torsades de pointes cardiac tissue Prolongs repol. refractory period & QT interval Blocks adrenergic receptors SVT & life-threatening arrhythmias
  • 152. SPIRONOLACTONE K-sparring diuretic Aldosterone antagonist Blocks aldosterone receptors Gynecomastia Impotence Hyperkalemia receptors Na excretion K excretion Primary hyperaldosteronism HTN hypokalemia
  • 153. VALSARTAN Antihypertensive Angiotensin receptor antagonist Blocks AT II receptor in vascular smooth m. & adrenal cortexadrenal cortex Vasodilation & aldosterone secretion HTN Nephropathy Less cough & angioedema than ACEI
  • 154. VERAPAMIL Antihypertensive, antianginal Non-dihydropyridine Ca channel blocker Blocks Ca channels in cardiac m. & vascular smooth m. Vasodilation Peripheral edema Constipation Gingival hyperplasia Vasodilation HR & conduction contractility Suppress contractility more than other Ca channel blockers HTN Angina pectoris SVT Prevent migraine HA
  • 155. CNS DEPRESSANTS
  • 156. Buspirone Carbamazepine Diazepam Disulfiram Ethosuximide Lorazepam Phenobarbital Phenytoin Topiramate ValproateEthosuximide Flumazeil Gabapentin Lamotrigine Valproate Zolpidem
  • 157. BUSPRIONE Antianxiety 5-HT1A partial agonist Activates presynaptic 5- HT1A receptors in dorsal raphe nucleus firing serotonergic neurons Dizziness Drowsiness Fatigue HA Excitement Nervousness Blurred vision Tachycardia firing serotonergic neurons Generalized anxiety disorder NO Drug dependence Significant sedation Muscle relaxation Anticonvulsant effects Tachycardia N Rash Myalgia Sweating levels by Erythromycin Itraconazole Grapefruit juice
  • 158. CARBAMAZEPINE Anticonvulsant Neuronal Na channel blocker Blocks Na channels in CNS firing of ectopic foci Ataxia Drowsiness Blurred vision Agranulocytosis Aplastic anemia Thrombocytopenia firing of ectopic foci & spread of epileptic seizures Partial seizures & generalized tonic-clonic seizures Bipolar disorders Trigeminal neuralgia Neuropathic pain Induces its own metabolism
  • 159. DIAZEPAM Antianxiety Benzodiazepine Binds receptors on GABA operated Cl ion channel channel affinity for GABA & frequency of Drowsiness Lethargy Physical/psychological dependence Tolerance channel affinity for GABA & frequency of channel opening Potentiates inhibitory effects of GABA Anxiety Status epilepticus Muscle spasm Alcohol w/drawal Anterograde amnesia Long-lasting active metabolites
  • 160. DISULFIRAM Alcohol abuse Tx Acetaldehyde dehydrogenase inhibitor Inhibits acetaldehyde degradation following alcohol ingestion Blurred vision Drowsiness Blurred vision Chest pain Dizziness Palpitations N, V HA Weakness Reinforcement of alcohol abstinence
  • 161. ETHOSUXIMIDE Anticonvulsant Succimide Binds T-type Ca channels in thalamic neurons Dizziness Drowsiness Gastric distress N thalamic neurons Suppresses nerve transmissions to motor cortex Generalized absence seizures Petit mal epilepsy
  • 162. FLUMAZENIL Antidote Benzodiazepine receptor antagonist Blocks benzodiazepine Seizures Dizziness Emotional lability benzodiazepine receptors Counteract adverse effects of benzodiazepines Respiratory depression d/t IV OD CI in status epilepticus
  • 163. GABAPENTIN Anticonvulsant GABA analogue GABA release from central neurons Ataxia Dizziness Drowsiness Nystagmus Tremor neurons Inhibits neuronal discharges from seizure foci Inhibits pain neurotransmission Partial seizures Chronic pain Migraine prophylaxis
  • 164. LAMOTRIGINE Anticonvulsant Phenyltriazine Blocks voltage- sensitive Na Skin rash in 1st 8 wk of Tx Can progress to Stevens-Johnson syn Ataxia sensitive Na channels Release of glutamate Prevents spread of seizure foci discharges Adjunct/monotherapy for partial seizures in adults Ataxia Dizziness Drowsiness Photosensitivity metabolism & ADR w/ valproate
  • 165. LORAZEPAM Sedative-hypnotic, anxiolytic Benzodiazepine Binds benzodiazepine receptors on GABA operate Cl ion channel channel affinity for GABA & frequency of Dizziness Drowsiness Apnea & cardiac arrest w/ rapid IV admin Additive depression w/ alcohol & other depressants channel affinity for GABA & frequency of channel opening Potentiates inhibitory effects of GABA Anxiety Insomnia Preoperative sedation Light anesthesia Anterograde amnesia Flumazenil used to counteract severe OD
  • 166. PHENOBARBITAL Sedative-hypnotic, anticonvulsant Barbiturate Binds GABA operated Cl ion channel increasing duration of Drowsiness Lethargy Delirium Hangover Physical & psychological dependence Induces CYP P450 increasing duration of channel opening Cl influx in absence of GABA Tonic-clonic & partial seizures Febrile seizures in children Preoperative sedation Short-term hypnotic folate requirement during long-term Tx Induces CYP P450 metabolism of drugs
  • 167. PHENYTOIN Anticonvulsant Hydantoin Blocks voltage-sensitive Na channels Release glutamate Prevents spread of seizure foci discharges Ataxia Diplopia Nystagmus Gingival hyperplasia Prevents spread of seizure foci discharges Partial seizures Generalized tonic-clone seizures Status epilepticus following IV diazepam Zero-order @ high doses Fosphenytoin for IV use
  • 168. TOPIRAMATE Anticonvulsant Monosaccharide derivative Block voltage-sensitive Na channels Augments GABA Ataxia Dizziness Drowsiness Fatigue Impaired concentration & memory Psychomotor slowingAugments GABA activation of GABA receptors Blocks glutamate receptors Partial & tonic-clonic seizures Decrease dose in pts w/ renal impairment Psychomotor slowing Speech problems Diplopia Nystagmus
  • 169. VALPROATE Anticonvulsant Branched-chain FA GABA levels by release or metabolism or reuptake Reduced Na dependent Indigestion N, V Dizziness Sedation Hepatotoxicity Reduced Na dependent action potentials Simple & complex absence seizures Complex partial seizures Tonic-clonic seizures Myoclonic seizures Migraine prevention Manic phase of bipolar
  • 170. ZOLPIDEM Non-benzodiazepine hypnotic Imidazopyridine Activates BZBP receptors on GABAreceptors on GABA operated Cl ion channel channel affinity for GABA & frequency of channel opening Neuronal hyperpolarization Insomnia
  • 171. ENDOCRINE
  • 172. Acarbose Alendronate Calcitonin Danazol Desmopressin Ergocalciferol Insulin Levothyroxine Medroxyprogesterone Metformin Methimazole MifepristoneErgocalciferol Ethinyl estradiol & drospirenone Ethinyl estradiol & norethindrone Finasteride Fludrocortisone Glyburide Hydrocortisone Mifepristone Octreotide Oxytocin Pioglitazone Prednisone Raloxifene Repaglinide Somatropin Testosterone
  • 173. ACARBOSE Antidiabetic -glucosidase inhibitor Inhibits intestinal enzyme that converts oligosaccharides & Intestinal bloating Flatulence oral bioavailability of metforminoligosaccharides & disaccharides to glucose digestion of starch & sucrose postprandial blood glucose & HbA1c Type II DM metformin iron absorption
  • 174. ALENDRONATE Bone resorption inhibitor Bisphosphonate Prevents attachment of osteoclast precursor cells to bone metabolic activity of Absorption by Ca supplements, antacids, foods, beverages (except water) metabolic activity of osteoclasts & ability to resorb bone Prevent/Tx Osteoporosis Corticosteroid-induced osteoporosis Pagets ds of bone hypercalcemia
  • 175. CALCITONIN Ca hormone Thyroid gland hormone Binds calcitonin receptor on osteoclasts cAMP & inhibits cAMP & inhibits osteoclast activity bone resorption, bone pain, & serum [Ca] Postmenopausal osteoporosis Pagets ds of bone hypercalcemia
  • 176. DANAZOL Ovarian inhibitor Synthetic androgen, antiestrogen Feedback inhibits pituitary FSH & LH secretion ovarian CI in pregnancy androgenic effects on female fetus Emotional lability Deepening voicesecretion ovarian estrogen secretion & stim. endometrial & breast tissue. Endometriosis Fibrocystic breast ds Hereditary angioedema C1 esterase inhibitor & C4 complement component Deepening voice Acne Hirsutism Amenorrhea breast size
  • 177. DESMOPRESSIN Posterior pituitary hormone Vasopressin, ADH analogue Mimics naturalMimics natural vasopression Increases water reabsorption in kidneys Vasoconstriction DI Nocturnal enuresis Control bleeding in hemophilia & wWFs ds Intranasal, oral, or IV
  • 178. ERGOCALCIFEROL Vit. D Fat-soluble Activated in liver & kidneys to form calcitriol Ca & phosphorus Hypercalcemia Hypercalciuria Cholestyramine inhibits vit. D absorption Induce vit. D Ca & phosphorus absorption from gut Vit. D deficiency Rickets, osteomalacia Chronic renal failure Familial hypophosphatemia Hypocalcemia d/t hypoparathyroidism Postoperative & idiopathic tetany Induce vit. D metabolism Phenytoin Barbiturates
  • 179. ETHINYL ESTRADIOL & DROSPIRENONE OCP Estrogen & progesterone Feedback inhibit GnRH Estrogen Drospirenone Antiandrogenic Blocks aldosterone salt & water retentionEstrogen FSH secretion & maturation of dominant follicle Progesterone Inhibits midcycle LH surge & ovulation Contraception Regulate menstrual cycle Acne in women retention BP Thromboembolis m risk w/ smoking Edema Efficacy w/ ABX Carbamazepine phenytoin
  • 180. ETHINYL ESTRADIOL & NORETHINDRONE OCP Estrogen & progesterone Feedback inhibit GnRH Estrogen Norethidrone Slightly androgenic Thromboembolism EdemaEstrogen FSH secretion & maturation of dominant follicle Progesterone Inhibits midcycle LH surge & ovulation Contraception Regulate menstrual cycle Acne in women Edema Depression Gallbladder ds
  • 181. FINASTERIDE Androgen synthesis inhibitor 5--reductase inhibitor Inhibits conversion testosterone CI pregnancy Risk to male fetus Do NOT handle tablets Impotence testosterone dihydrotestosterone & androgenic stimulation of prostate & skin prostate size & promotes hair growth BPH Male pattern baldness Impotence
  • 182. FLUDROCORTISONE Corticosteroid Mineralocorticoid Activates aldosterone receptors in renal distal tubule Na reabsorption Hypokalemia by thiazide & loop diuretics Na reabsorption K & H excretion Adrenal insufficiency Addisons ds Congenital adrenogenital syn Tx idiopathic orthostatic hypotension w/ Na intake
  • 183. GLYBURIDE Antidiabetic Sulfonylurea hypoglycemia Closes ATP-sensitive K channels preventing K Photosensitivity Hypoglycemia channels preventing K efflux & depolarizing pancreas B cells Influx Ca & relaxing insulin amount of insulin secreted during each pulse Type II DM
  • 184. HYDROCORTISONE Short-acting corticosteroid, low-potency topical corticosteroid Glucocorticoid Replaces endogenousReplaces endogenous cortisol in deficiency states Suppresses inflammation & immune response topical Adrenocortical insufficiency Topical Insect bites Contact dermatitis
  • 185. INSULIN Antidiabetic Pancreatic hormone Replaces Hypoglycemia -blockers mask signs of hypoglycemia &Replaces endogenous insulin DM Rapid acting lispro Intermediate acting lente Long acting ultralente hypoglycemia & prolong recovery
  • 186. LEVOTHYROXINE Thyroid hormone Tetraiodothyronine Binds nuclear receptors & gene transcription Insomnia Irritability Tachycardia Wt loss transcription metabolic rate, protein synthesis, gluconeogenesis, cell growth & differentiation, & CNS development Converted to T3 in tissues Hypothyroidism Bile acid sequestrants absorption
  • 187. MEDROXYPROGESTERONE Progestin, contraceptive Progesterone analogue endometrial hyperplasia in women receiving estrogen Amenorrhea Breakthrough bleeding Dysmenorrhea receiving estrogen Prevents conception by thickening cervical mucus Estrogen-progestin HRT Injectable contraceptive Progestin-only injectable contraceptive IM depot injection lasts 3mo
  • 188. METFORMIN Antidiabetic Biguanide, antihyperglycemic # & affinity of insulin receptors in peripheral tissues N, V, D Abdominal bloating hepatic glucose output glucose absorption from gut glucose uptake & utilization in skeletal m. & adipose tissue Type II DM Used in combo w/ sulfonylureas
  • 189. METHIMAZOLE Antithyroid Thiourea, thyroid hormone synthesis inhibitor Inhibits peroxidase Rash Agranulocytosis Inhibits peroxidase & iodination & coupling of tyrosine residue of thyroglobulin thyroxine secretion Hyperthyroidism Graves ds
  • 190. MIFEPRISTONE Abortificient Progesterone antagonist Partial agonist or antagonist Abdominal pain Diarrhea N, V Uterine bleeding Crampingantagonist progesterone receptors Medical termination of pregnancy through 49d gestation Single dose + prostaglandin for 48hr stim. uterine contractions Cramping
  • 191. OCTREOTIDE GH inhibitor, antidiarrheal Somatostatin analogue w/ greater effects on GH than insulin secretion Suppresses secretion of Arrhythmias Hyperglycemia Hypoglycemia Constipation Diarrhea Flatulence Suppresses secretion of GH, insulin-like growth factors, 5-HT & GI peptides gastrin, motilin, secretin, & VIP Acromegaly Severe diarrhea & flushing d/t carcinoid tumors & VIP tumors Bleeding GE varices Complications of pancreatic surgery N
  • 192. OXYTOCIN Oxytocic Posterior pituitary hormone Stim. Uterine smooth m. & induce labor Stim. mammary gland Excessive & painful uterine contractions Stim. mammary gland smooth m. & lactation Induce labor @ term Facilitate uterine contractions Postpartum control of uterine bleeding Promote milk let-down IV for uterine stim. Nasal for milk let-down
  • 193. PIOGLITAZONE Antidiabetic Thiazolidinedione antihyperglycemic Activates peroxisome proliferator-activated receptor- in adipose tissue, skeletal m., & livertissue, skeletal m., & liver gene transcription, insulin sensitivity, & glucose transports in muscle & adipose tissue Suppresses hepatic glucose output Type II DM Used w/ metformin
  • 194. PREDNISONE Anti-inflammatory Corticosteroid Suppresses inflammation & immune response Depression or euphoria HTN Acne Impaired wound immune response Inflammatory, allergic, autoimmune, & neoplastic ds Prevent organ transplant rejection Asthma Impaired wound healing Adrenal suppression Muscle wasting Osteoporosis Cushingoid appearance Moon facies Buffalo hump susceptibility to infection
  • 195. RALOXIFENE Bone resorption inhibitor Selective estrogen receptor modulator SERM Estrogen-like effect on bone & lipid Hot flashes Cholestyramine inhibits absorption bone & lipid metabolism Estrogen antagonist in breast & uterine tissue bone mineral density & vertebral fractures Osteoporosis in postmenopausal women Used in woman @ risk for breast cancer
  • 196. REPAGLINIDE Antidiabetic Meglitinide hypoglycemic Closes ATP-sensitive K channels & insulin Hypoglycemia channels & insulin secretion postprandial blood glucose & [HbA1c] Taken before meals to control postprandial hyerglycemia Used w/ metformin NOT sulfonylureas
  • 197. SOMATROPIN GH Recombinant somatotropin release of insulin-like growth factors in liver & cartilage& cartilage Stim. skeletal growth, AA transport, protein synthesis, nucleic acid synthesis & cell prolif. Short stature in children d/t GH deficiency Turner syn Chronic renal failure Prader-Will syn
  • 198. TESTOSTERONE Androgen Gonadal steroid Activated gene transcription & development of male sex organs & secondary sex characteristics lean body mass Edema Acne Gynecomastia Impotence Oligospermia Priapism lean body mass Stim. skeletal growth Accelerates epiphyseal closure sebaceous gland sebum production EPO secretion HDL levels Hypogonadism in androgen- deficient men Delayed puberty in males