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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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