PHARMACOLOGY
ANALGESIC & ANTIMIGRAINE
Butorphanol Dihydroergotamine Fentanyl Meperidine Methadone Morphine
Naloxone Propoxyphene Sumatriptan Tramadol
BUTORPHANOLDysphoria Nightmares w/drawal in pts dependent on full opioid agonists AVOID MAOIPotentially fatal
Opioid analgesic Mixed opioid agonistantagonist
Partial agonist or antagonist @ opioid receptors Agonist @ receptors @ spinal & supraspinal sites Inhibits spinothalamic pain neurotransmission
Moderate-severe pain Admin intranasally
respiratory depression, constipation, dependence than full receptor agonists
DIHYDROERGOTAMINEN, V Stiff neck, shoulder, extremities Leg weakness Numbness & tingling in fingers & toes
Antimigraine Ergot alkaloid 5-HT 1B/1D receptor agonist
Activates 5-HT 1B/1D receptors
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
FENTANYL
Opioid analgesic Phenylpiperidine
Activates opioid receptors
Inhibits pain transmission @ spinal & supraspinal sites
Sedation Confusion Respiratory depression Anorexia N, V Constipation AVOID MAOI in past 14d
Chronic pain Breakthrough for cancer pain
Transdermal patch
MEPERIDINE
Opioid analgesic Strong opioid agonist
Activates opioid receptors
Confusion Sedation Constipation N, V Dependence Toxic metabolite CNS excitation, convulsions, tremors AVOID MAOIPotentially fatal
Inhibits pain transmission Generalized CNS depression
Moderate-severe pain Analgesia during labor Preoperative sedation
Lacks antitussive activity
METHADONERespiratory depression Constipation Confusion Sedation AVOID MAOI
Opioid analgesic Strong opioid agonist
Activates opioid receptors
Inhibits pain transmission Suppresses opioid w/drawl Sx w/ euphoria or dependence
Moderate-severe pain Prevention of opioid abuse
Orally, once per day
MORPHINESedation Confusion Hypotension Constipation Respiratory depression AVOID MAOI w/ 14 dPotentially fata
Opioid analgesic Strong opioid receptor agonist
Activates receptors
cAMP
Opens K & closes Ca channels release substance P
Inhibits pain @ spinal & supraspinal sites
Severe pain w/ MI Pulmonary edema
Active metabolite
Morphine glucuronate
NALOXONE
Opioid antagonist Opioid receptor antagonist
Blocks opioid , , receptors Rapidly reverses effects of opioid agonists
Opioid OD, dependence
Short half-life needs repeated doses
PROPOXYPHENEDizziness Weakness N dependence
Opioid analgesic Weak opioid agonist
Activates opioid receptors
Inhibits pain transmission
Mid-moderate pain
Combined w/ acetaminophen or aspirin
SUMATRIPTANDizziness Vertigo Tingling Warm sensation Tight feeling head & chest Coronary vasospasm AVOIDMAOI SSRI
Antimigraine 5-HT 1B/1D receptor agonist
Activates 5-HT 1B/1D receptors
Pial & dural vessel constriction
Presynaptic inhibition of trigeminal peptide neurotransmitter release Inhibitions brainstem activation of trigeminal neurons
Vascular HA
Migraine & cluster
Oral, nasal, & subQ
TRAMADOLDizziness HA Constipation Lowers seizure threshold AVOID MAOI risk seizures w/ high dosesPenicillins Phenothiazines
Analgesic Dual action
Activates opioid receptors
Inhibits neuronal reuptake 5-HT & NE inhibition of pain
Moderate pain Chronic pain
Naloxone reverses some but NOT all Sx
ANESTHETICS
Benzocaine Bupivacaine Halothane Ketamine Lidocaine
Midazolam Nitrous oxide Propofol Sevoflurane
BENZOCAINECross-sensitivity w/ other ester-type anesthetics
Local anesthetic Ester-type
Blocks Na channels & nerve conduction
Topical anesthetic
Pain Itching Inflammation
Burns Insect bites Contact dermatitis Wounds
Irritates skin when 1st applied Use caution w/ sunburn & large areas of skin
BUPIVACAINECross-sensitivity w/ amide-type anesthetics
Local anesthetic Amide-type
Blocks Na channels & nerve conduction
Local or regional anesthetic
Surgical Diagnostic Obstetrical therapeutic
HALOTHANESensitizes heart to catecholamine-induced cardiac arrhythmia HepatotoxicFluoride metabolites
General anesthetic Inhalational, halogenated hydrocarbon
Potentiates GABA binding to GABA-A Cl ion channel
Suppresses sensory processing in thalamus
General anesthetic
High blood:gas partition coefficient Slow rate of induction & recovery
KETAMINEDelirium Hallucination Irrational behavior during recovery BP
IV anesthetic Glutamate antagonist
Blocks glutamate NMDA receptors
Dissociate anesthesia Analgesia Immobility Amnesia
Does NOT depression respiration or cause LOC
Anesthesia Minor surgical & diagnostic procedures Children
LIDOCAINECross-reactivity w/ amidetype anesthetics
Local anesthetic Amide-type
Blocks Na channels & nerve conduction
Topical Infiltration Nerve block Epidural Spinal anesthesia Eutectic mixture
Lidocaine & prilocaine Anesthetize intact skin for venipuncture IV cannulation Circumcism
MIDAZOLAMApnea Laryngospasm Respiratory depression Cardiac arrest
Sedative-hypnoticanxiolytic Short-acting BZDP
Potentiates GABA binding to GABA-A Cl ion channel
Sedation Hypnosis Amnesia
Preoperative sedation & anxiolysis Sedation of mechanically vented pts
NITROUS OXIDE
Inhalation general anesthetic Anesthetic gas
Potentiates GABA binding to GABA-A Cl ion channel
Suppresses sensory processing in thalamus Minor surgery & dental procedures
Rapid induction & recovery Euphoria laughing gas
PROPOFOLBradycardia Hypotension
General anesthesia IV anesthetic Diisopropyl phenol
Potentiates GABA binding GABA-A Cl ion channel
Hypnosis Anesthesia Amnesia
NO analgesic effect
Intubation & maintenance of general anesthesia Sedation of intubated pts in ICU
SEVOFLURANE
General anesthetic Inhalation anesthetic
Potentiates GABA binding to GABA-A Cl channel
Suppresses sensory processing in thalamus Causes LOC
General anesthesia
ANTI-INFECTIVE
Acyclovir Albendazole Amantadine Amoxicillin-clavulanate Amphotericin B Azithromycin Aztreonam Caspofungin Cefazolin
Cefepime Cetriaxone Ciprofloxacin Clindamycin Doxycycline Efavirenz Enfuvirtide Erythromycin Ethambutol
Foscarnet Fosfomycin Ganciclovir Gentamicin Griseofulvin Imipenem-cilastatin Isoniazid Itraconazole Ivermectin Levofloxacin
Linezolid Mefloquine Metronidazole Mupirocin Nafcillin Nitrofurantoin Oseltamivir Paromomycin Penicillin G
Pentamidine Piperacillin-tazobactam Praziquantel Primaquine Pyrimethamine Pyrantel Quinine Quinpristein-dalfopristin Ribavirin
Rifampin Ritonavir-lopinavir Streptomycin Terbinafine Trifluridine TMP-SMX Vancomycin Zidovudine
ACYCLOVIRDizziness Diarrhea N Nephrotoxicity Probenecid serum levels
Antiviral Nucleoside analogue
Converted to acyclovir triphosphate by viral & host cell kinases Incorporated into DNA by viral DNA polymerase causing DNA chain termination
HSV2 Herpes zoster
Shingles Chickenpox varicella
viral shedding, pain, & healing time
ALBENDAZOLEGI distress Constipation or diarrhea Hepatitis & hematologic toxicity w/ high doses
Antihelmintic Benzimidazole
Binds & inhibits polymerization of tubulin dimmers to form cytoplasmic microtubules
Impairs glucose uptake & deplete glycogen stores
Intestinal nematode infections
Hookworm Pinworm Whipworm Ascariasis Capillariasis
Trichinosis
Use w/ corticosteroid
Cysticercosis & echinococcus Microsporidiosis
AMANTADINEAtaxia Dizziness Insomnia Skin mottling & livedo reticularis Blurred vision Dry mouth
Anti-influenza, antiparkinson Tricyclic amine
Inhibits influenza-A M2 proton channel & acidification of virus particle
Prevents viral proteinprotein dissociation & uncoating of viral particles
Influenza A
AMOXICILLIN-CLAVULANATEDiarrhea Superinfection Pseudomembranous colitis Allergic rxnRash Serum sickness anaphylaxis
-lactam ABX Extended spectrum aminopenicillin & -lactamase inhibitor
Amoxicillin
Binds PBP Probenecid inhibits renal tubular excretion serum levels
Inhibits 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
AMPHOTERICIN BChills Fever Diarrhea N, V Nephrotoxicity Hypokalemia toxicity w/ cyclosporine, antineoplastics Thiazides, & corticosteroids hypokalemia
Antifungal Polyene ABX
Binds ergosterol & membrane permeability
Leakage of cell contents
Candidiasis Cryptococcal meningitis Aspergillosis Blastomycosis Coccidioidomycosis Histoplasmosis Mucormycosis
AZITHROMYCIN
Macrolide Protein synthesis inhibitor
Binds 50s ribosome Prevents peptide elongation & translocation from acceptor 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
AZTREONAMThrombophlebitis Allergic rxn
-lactam ABX Monobactam
Binds PBP including transpeptidase Inhibits cross-linking of cell wall peptidoglycan
Drug resistant gram (-) infections including Pseudomonas aeruginosa & Enterobacteriaceae
CASPOFUNGINHA Fever Phlebitis Abnormal LFTs
Antifungal Echinocandin
Inhibits synthesis of cell wall component
-1,3-D-glucan
Candida albicans Invasive aspergillosis
IV admin
Not absorbed well by gut
CEFAZOLINRash Diarrhea Pseudomembranous colitis Superinfection Probenecid inhibits excretion & serum levels
-lactam ABX 2nd generation cephalosporin
Binds PBP including transpeptidase Inhibits cross-linking of cell wall peptidoglycan
Surgical wound infections Infections d/t
Staph, strep, E. coli, Klebsiella pneumoniae, Proteus mirabilis
NOT active against MRSA
CEFEPIMERash Diarrhea Pseudomembranous colitis Superinfection Probenecid inhibits excretion & serum levels
-lactam ABX 4th generation cephalosporin
Binds multiple PBP Inhibits cross-linking of cell wall peptidoglycan Resistant to many lactamases
Drug-resistant gram (-) bacteria
Citrobacter Enterobacter
CEFTAZIDIMERash Diarrhea Pseudomembranous colitis Superinfection Probenecid inhibits excretion & serum levels
-lactam ABX 3rd generation cephalosporin
Binds PBP including transpeptidase Inhibits cross-linking of cell wall peptidoglycan
Gram (+), gram (-), & anaerobics Pseudomonas aeruginosa
Pneumonia, meningitis, UTI, skin structures, bones, jts
CETRIAXONERash Diarrhea Pseudomembranous colitis Superinfection Probenecid inhibits excretion & serum levels
-lactam ABX 3rd generation cephalosporin
Binds PBP including transpeptidase Inhibits cross-linking of cell wall peptidoglycan
Infection d/t
Pneumococci, gonococci, meningococci, H. influenzae, Moraxella catarrhalis, Borrelia burgdorferi
Single IM injection Tx acute otitis media or gonorrhea
CIPROFLOXACINInsomnia Diarrhea N Absorption by cationsAntacids Iron Zinc bismuth
Antibacterial Fluoroquinolone
Inhibits bacterial DNA topoisomerase type II (DNA gyrase) & type IV Prevents DNA replication & separation of chromosomes
Urinary tract, prostate, intraabdominal w/ metronidazole, bone or jt, skin Inhalational anthrax Gonorrhea Infectious diarrhea
Gram (+), gram (-), Pseudomonas aeruginosa
CLINDAMYCINC. difficile superinfection Diarrhea Pseudomembranous colitis
Aminosugar ABX Protein synthesis inhibitor
Binds 50s ribosome Prevents translocation of nascent peptide from acceptor site to peptidyl site
Strep, staph, gram (+) Acne vulgaris Anaerobes including Bacteroides
DOXYCYCLINEAVOIDPregnancy & children > 8 y/o Outdated preparations are nephrotoxic
Tetracycline ABX Protein synthesis inhibitor
Binds 30s ribosome Reversibly inhibits binding of transfer RNA to acceptor site
Rickettsia, Chlamydia, Mycoplasma, Borrelia Acne Cholera Gonorrhea & syphilis in PCN allergic pts Brucellosis & ehrlichiosis
Permanent teeth discoloration Photosensitivity Diarrhea N, V
EFAVIRENZN Rash Drowsiness Depression
Antiretroviral Non-nucleoside reverse transcriptase inhibitor
Binds reverse transcriptase & disrupts catalytic site
HIV in combo w/ nucleoside reverse transcriptase inhibitor synergistic
High fat meal absorption
ENFUVIRTIDEInjection site rxnRotate sites daily
Antiretroviral HIV fusion inhibitor
Binds HIV virus gp41 & blocks fusion of HIV w/ host cells CD4 Thelper lymphocytes
Drug-resistant HIV
ERYTHROMYCINActivates motilin receptors causing uncoordinated peristalsisAnorexia N, V
Macrolide ABX Protein synthesis inhibitor
Binds 50s ribosome Prevents peptide elongation & translocation from acceptor site to peptidyl site
Pharyngitis, otitis media, sinusitis, pneumonia d/t
Strep, pneumococci, Mycoplasma, Chlamydia, Legionella, MAI
ETHAMBUTOLDose-related retrobulbar optic neuritis Impaired red-green color discriminationMonitor pts color discrimination regularly
Antitubercular Synthetic butanol derivative
Bacteriostatic against mycobacteria Inhibits RNA synthesis
Gouty arthritis
M. tuberculosis MAI
FOSCARNET
Antiviral PyrophosphateHA Diarrhea V Renal failure Hypocalcemia Hypokalemia Hypomagnesemia Anemia Arthralgia Myalgia
Blocks pyrophosphatebinding site on viral DNA polymerase
Prevents attachment of nucleotide precursors to DNA
CMV retinitis in HIV pts Acyclovir-resistant HSV in immunocompromised
Pentamidine causes lifethreatening hypocalcemia
FOSFOMYCIN
ABX Cell wall synthesis inhibitor
Inhibits enopyruvyl transferase & addition of phosphenolpyruvate to N-acetylglucosamine to form Nacetylmuramic acid
Cystitis d/t E. coli or Enterococcus faecalis
Single dose Tx for UTI
GANCICLOVIR visual acuity Neutropenia Thrombocytopenia Anemia
Antiviral Nucleoside analogue
Converted to ganciclovir triphosphate
Inhibits viral DNA polymerase
CMV infection in immunocompromise d & transplants
GENTAMICINNephrotoxicity OtotoxicityVestibular & cochlear w/ loop diuretics
Aminoglycoside ABX Protein synthesis inhibitor
Binds 30s ribosome Prevents initiation of protein synthesis
Misreading of genetic code
Gram (-) bacilli including Enterobacteriaceace & P. aeruginosa Strep, enterococcal, & staph infections
Monitor serum levels
GRISEOFULVINHA Induces CYP450Reduces plasma levels warfarin & OCP
Antifungal Fungistatic ABX
Deposits in keratin precursor cells of skin, hair, & nails Disrupts microtubules & mitotis of dermatophytes
Dermatophyte infections NOT Candida
IMIPENEM-CILASTATINAllergic rxns Diarrhea V Seizures risk w/ ganciclovir or cyclosporine
-lactam ABX Carbapenem ABX & dehydropeptidase inhibitor
Imipenem
Binds PBP & inhibits crosslinking cell wall peptidoglycan
Probenecid inhibits secretion & serum levels
Cilastatin
Inhibits renal dehydropeptidase & degradation of imipenem
Endocarditis, pneumonia, UTI, pelvic, abdominal d/t aerobic & anaerobic
ISONIAZIDHepatitisToxic metabolite acetylhydrazine
Antitubercular Nicotinic acid derivative
Peripheral neuropathyVit. B6 deficiency
Reduces catalaseperoxidase
Inhibits synthesis of mycolic acid component of cell wall
TB
Bimodal distribution d/t fast & slow acetylation Inactivates vit. B6
ITRACONAZOLEGI distress Rash Hepatitis
Antifunal Synthetic triazole
Inhibits 14-demethylase
CYP450 enzyme that converts lanosterol ergosterol
Blastomycosis, candidiasis, coccidioidomycosis, histoplasmosis Onychomycosis nail beds
IVERMECTINVertigo Sedation
Antiparasitic Antihelmintic ABX
Activates glutamategated Cl ion channel
Pharyngeal m. hyperpolarization & paralysis
Strongyloidiasis Cutaneous larva migrans Onchocerciasis filiariasis
W. bancrofti
LEVOFLOXACIN
Antibacterial Fluoroquinolone
Inhibits bacterial DNA topoisomerase type II (DNA gyrase) & type IV Prevents DNA replication & separation of chromosomes
Community-acquired pneumonia UTI Gynecologic & skin infections
Gram (+), gram (-), P. aeruginosa, Mycoplasma, Mycobacterium
LINEZOLIDInhibits MAO
Antibacterial Oxazolidinone protein synthesis inhibitor
Binds 23s ribosomal RNA of 50S subunit
Prevents formation of 70s initiation complex
VRE, MS/MRSA, PCNsensitive pneumococci
MEFLOQUINENeuropsychiatric synHallucination Anxiety Confusion Seizure Coma
Antimalarial 4-quinolone methanol derivative
Inhibits erythrocytic schizogony Inhibit nucleic acid synthesis
Malaria Chloroquinesusceptible/resistant trains of P. falciparum & P. vivax
Perform CBC during chronic prophylactic Tx
METRONIDAZOLEGI pain Anorexia N Dizziness Alcohol causes disulfiram-like effect
Antiprotozoal Nitroimidazole
Reduced by pyruvate:ferredoxin to form nitro-free radicals that attack DNA & proteins
Amebiasis, giardiasis, trichomoniasis Balantidium coli, C. difficile, B. fragilis
MUPIROCIN
ABX Protein synthesis inhibitor
Competes w/ isoleucine 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
NAFCILLINDiarrhea Superinfection Pseudomembranous colitis Allergic rxnRash Serum sickness Anaphylaxis
-lactam ABX Antistaphylococcal, penicillinase-resistant penicillin
Binds PBP
Inhibits cross-linking of cell wall peptidoglycan
Methicillin-sensitive penicillinase producing staph
Probenecid inhibits renal tubular secretion & serum levels
Bone, jt, UTI, respiratory, skin, endocarditis, meningitis
NITROFURANTOINAnorexia N, V Neurotoxicity Pneumonitis Probenecid inhibits urinary excretion
Urinary tract antibacterial Nitrofuran
Inhibits bacterial enzymes
UTI
E. coli, S. saprophyticus
OSELTAMIVIR
Antiviral Neuraminidase inhibitor
Inhibits influenza A & B neuraminidase
Prevents release & spreading of viral particles
Influenza A & B
PAROMOMYCINNephrotoxic & ototoxic if given IV
Antiprotozoal Aminoglycoside ABX
Inhibits protein synthesis
Intestinal amebiasis Cryptosporidiosis in immunocompromised pts
PENICILLIN GDiarrhea Superinfection Pseudomembranous colitis Allergic rxnRash Serum sickness Anaphylaxis
-lactam ABX Narrow-spectrum penicillin
Binds PBP
Inhibits cross-linking of cell wall peptidoglycan
Strep, pneumococcal, meningococcal Syphilis
Probenecid inhibits renal tubular secretion
PENTAMIDINENephrotoxic Hematologic toxicity Hypoglycemia Allergic rxnAnaphylaxis
Antiprotozoal Amidino-pentane derivative
Disrupts nucleic acid synthesis in protozoa
Erythromycin fatal arrhythmias
P. carinii Early stage African trypanosimiasis sleeping sickness
PIPERACILLIN-TAZOBACTAMDiarrhea Superinfection Pseudomembranous colitis Allergic rxnRash Serum sickness Anaphylaxis
-lactam ABX Antipseudomonal penicillin & -lactamase inhibitor
Piperacillin
Binds PBP
Inhibits cross-linking of cell wall peptidoglycan
Tazobactam
Probenecid inhibits renal tubular secretion
Inhibits class A -lactamases
Gram (-) bacilli, P. aeruginosa
PRAZIQUANTELMalaise Anorexia Drowsiness dizziness
Antihelmintic Isoquinoline derivative
Ca permeability of schistosome tegument
Contraction & exposing antigens to host immunity
Schistosomiasis Chinese liver fluke Lung fluke Cestodes tapeworms
PRIMAQUINEHemolytic anemia in G6PD deficiency methemoglobinemia
Antimalarial 8-aminoquinoline
Converted to oxidizing quinolinequinone intermediates
Eradicate exoerythrocytic forms of P. vivax & P. ovale
PYRIMETHAMINEN Anorexia Hypersensitivity rxn
Antiprotozoal Folate reductase inhibitor
Inhibits folate reductase Folate deficiency in protozoa
Malaria in combo w/ sulfadoxine Toxoplasmosis in combo w/ sulfadoxine
NOT effective against P. vivax
PYRANTELAbdominal cramps Anorexia Diarrhea V
Antihelmintic Pyrimidine analogue
Activates cholinergic nicotinic receptors in somatic m. of nematodes Produces depolarizing NM blockade
Ascariasis Hookworm & pinworm
QUININEAbdominal cramps Diarrhea V CinchonismTinnitus Blurred vision
Antimalarial 4-aminoquinoline
Binds plasmodial DNA & prevents replication & transcription during erythrocytic schizogony
MetabolismCimetidine inhibits Rifampin induce
Chloroquine-resistant malaria
Admin w/ doxycycline or pyrimethamine-sulfadoxine
QUINUPRISTIN-DALFOPRISTINInfusion site rxn
Streptogramin ABX Protein synthesis inhibitor
Binds 50s ribosomal subunit Quinupristin
Inhibits aminoacyl tRNA synthesis & addition of AA
Dalfopristin
Inhibits peptidyl transferase
VRE, MS/MRSA
RIBAVIRINAnemia Hypotension Cardiac arrest
Broad-spectrum antiviral Guanosine analogue
Converted to ribavirin triphosphate Depletes guanosine triphosphate Inhibits viral RNA & protein synthesis
RSV in infants or children Chronic hepatitis C Viral hemorrhagic fever Lass fever
RIFAMPIN
Antitubercular Rifampin derivative
Inhibits DNA-dependent RNA polymerase
Red discoloration of tears, urine, saliva, sweat Abdominal pain V Diarrhea Hepatitis Induces CYP450 levelsWarfarin Theophylline Itraconazole Steroids Opioids Phenytoin Verapamil
TB Leprosy Prophylaxis meningococcal meningitis & H. flu B infections
RITONAVIR-LOPINAVIRAnorexia V Altered taste Abnormal thinking Hyperlipidemia Hyperlgycemia
Antiretroviral HIV protease inhibitor
Inhibits HIV protease & conversion of gagpol polyprotein to functional proteins Ritonavir
lopinavir levels
HIV in combo w/ nucleoside reverse transcriptase inhibitor
STREPTOMYCINNephrotoxic Ototoxic w/ loop diuretics
Aminoglycoside Protein synthesis inhibitor
Binds 30s ribosome Prevents initiation of protein synthesis
Misreading of genetic code
Drug-resistant TB Plague Tularemia
IV admin
TERBINAFINEItching Rash Diarrhea Anorexia MetabolismCimetidine inhibits Rifampin induce
Antifungal Allylamine
Inhibits squalene oxygenase & formation of squalene epoxide during fungal membrane ergosterol synthesis
Topical
Tinea corporis, cruris, pedis, versicolor
Oral
Onychomycosis fungal nail infection
TRIFLURIDINEOcular irritationRedness Itching
Antiviral Thymidine analogue
Inhibits HSV DNA polymerase
Herpetic keratitis Keratoconjunctivitis
Topical ocular admin
TRIMETHOPRIM-SULFAMETHOXAZOLEN, V Rash Stevens-Johnson syn Allergic rxn AnemiaHemolytic anemia Megalobalstic anemia
Antibacterial Folate antagonist
Sulfamethoxazole
Inhibits folate synthesis
Trimethoprim
Inhibits folate reduction
Leukopenia Thrombocytopenia Crystalluria Added folate deficiency w/ phenytoin or MTX
UTI, travelers diarrhea Shigella enteritis P. carinii & Nocardia pneumonia
VANCOMYCINRed man synExtensive rate of infusion Erythematous rash on face & upper body
Glycopeptide ABX Cell wall synthesis inhibitorOtotoxicity
Binds D-alanyl-Dalanine portion of peptidoglycan Prevents cross-linking of D-alanine & pentaglycine chain
Vestibular & cochlear
MRSA, penicillin-resistant enterococci, C. difficile
ZIDOVUDINEAnemia
Antiretroviral Nucleoside reverse transcriptase inhibitor
Activated nucleotide triphosphate incorporated into DNA causing chain termination
HIV Prevent maternal-fetal HIV transmission
1st line Tx for HIV infections
Zidovudine w/ lamivudine or emtricitabine & efavirenz or lapinavir-ritonavir
ANTINEOPLASTIC
Anastrozole Bleomycin Busulfan Carmustine Cisplatin Cyclophosphamide Doxorubicin Etoposide Fluorouracil Gemtuzumab ozogamicin
Imatinib Leuprolide Meraptopurine Methotrexate Paclitaxel Tamoxifen Trastuzumab Vincristine
ANASTROZOLEN HA Hot flashes Back pain
Estrogen antagonist Nonsteroidal aromatase inhibitor
Inhibits aromatase & conversion to estrone precursor to estradiol Lowers estrogen levels Halts progression of estrogen-sensitive breast cancers
Breast cancer in postmenopausal women
BLEOMYCINPneumonitis & pulmonary fibrosis Hyperpigmentation Mucocutaneous toxicity Hematology toxicity
Antitumor DNA intercalating
Complexes ironforming oxygen free radicals that cause single strand breaks G2 phase specific
Lymphomas SCC Testicular carcinoma Choriocarcinoma
BUSULFANN, V Myelosuppression Pulmonary fibrosis
Antineoplastic Alkyl sulfonate bifunctional alkylating agent
Cross-links DNA strands by covalently bonding guanine residues Prevents DNA replication & transcription
CML
Use w/ cyclophosphamide prior allogenic hematopoietic progenitor cell transplant for CML
CARMUSTINEN, V Hepatotoxicity Anemia Leucopenia Thrombocytopenia Pulmonary fibrosis
Antineoplastic Nitrosurea bifunctional akylating agent
Cross-links DNA strands by covalently bonding guanine residues Prevents DNA replication & transcription
Brain tumors Myeloma Lymphoma
Causes prolonged myelosuppression
CISPLATINSevere N, V Ototoxicity & tinnitus Hypocalcemia Hypokalemia Hypomagnesemia Anemia
Antineoplastic Platinum compound
Forms reactive metabolites that covalently bond DNA bases & cross-link DNA strands
Testicular, ovarian, cervical, bladder, lung, head/neck cancers
Less bone marrow suppression
CYCLOPHOSPHAMIDEAnorexia N, V Hemorrhagic cystitis & hematuria Alopecia Thrombocytopenia Leukopenia Anemia Rifampin induces CYP & toxicity
Antineoplastic Nitrogen mustard bifunctional akylating agent
Cross-links DNA strands by covalently bonding guanine residues Prevents DNA replication & transcription
Hodgkins ds Lymphomas, myeloma Leukemia Ovarian & breast tumors RA
Converted to active metabolites by CYP enzymes
DOXORUBICINColors urine red
Antitumor DNA intercalating agent
Inserts b/w DNA bases
Causes deformation & uncoupling
Complexes iron forming hydroxyl free radicals that cause strand breaks Inhibits topoisomerase II
Causes strand breaks
S phase specific
Cardiomyopathy doselimiting Anemia Leukopenia Thrombocytopenia Diarrhea V Stomatitis Alopecia
Breast, ovarian, bladder tumors Bronchogenic carcinoma Lymphoma & leukemia
ETOPOSIDEN, V Leukopenia Thrombocytopenia Alopecia
Antineoplastic Podophyllotoxin, topoisomerase inhibitor
Inhibits mammalian topoisomerase II & prevents resealing of nicked DNA strands G2 phase specific
Testicular, small cell lung carcinoma Lymphoma Leukemia
FLUOROURACIL
Antineoplastic Pyrimidine antimetabolite
Converted to active nucleotide form
Inhibits thymidylate synthetase
S phase specific
Diarrhea V Stomatitis Alopecia Maculopapular rash Anemia Leukopenia Thrombocytopenia
Colon, breast, rectal, gastric, pancreatic cancer Topical for basal cell carcinoma & actinic keratosis
GEMTUZUMAB OZOGAMICINSevere myelosuppression & hypersensitivity rxnanaphylaxis
Antineoplastic Monoclonal Ab & cytotoxic ABX calicheamicin
Gemtuzumab
Binds CD33 Ag on hematopoietic cells & sequesters lysosomes where calicheamicin is released
Severe pulmonary rxns Chills Fever N Dyspnea
Calicheamicin
Causes DNA dbl strand breaks
CD33 (+) AML
IMATINIB
Antineoplastic Tyrosine kinase inhibitor
Inhibits oncoprotein bcrabl tyrosine kinase expressed by Philadelphia chromosome Inhibits leukemic cell proliferation & induced apoptosis
CML
Cause hematologic & cytogenetic remission
Cough Dyspnea Pharyngitis Pneumonia Abdominal pain V Petechiae Pruritis Rash Night sweats Myalgia Arthralgia Thrombocytopenia Neutropenia
LEUPROLIDETransient in testosterone w/ 1st doseUse flutamide or other androgen antagonist
Antineoplastic, agent for precocious puberty GnRH analogueHot flashes
Pulsatile admin FSH & LH release Continuous admin downregulates GnRH receptors & FSH & LH
Central precocious puberty Advanced prostate cancer Endometriosis Uterine fibroids
IM depot & implants for prostate cancer
MERCAPTOPURINECross-react w/ thioguanine Myelosuppression Hyperuricemia Hepatotoxicity Allopurinol inhibits degradation
Antineoplastic Purine antimetabolite
Converted to nucleotide triphosphate by phosphoribosyl transferase Inhibits purine biosynthesis & salvage pathways S phase specific
Acute leukemia CML Lymphomas
Tumors that delete phosphoribosyl-transferase acquire resistance
METHOTREXATEN, V Stomatitis Hepatotoxicity Anemia Leukopenia Thrombocytopenia Nephropathy
Antineoplastic Folate reductase inhibitor
Inhibits dihydrofolate reductase Prevents formation of active folate & addition of single carbon units to DNA base precursors 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
PACLITAXEL
Antineoplastic Mitotic inhibitor
Binds tubulin & prevents depolymerization of microtubules of mitotic spindle M phase specific
D N, V Alopecia Anemia Leukopenia Thrombocytopenia Peripheral neuropathy Arthralgia Myalgia
Advanced ovarian cancer w/ cisplatin Non-small-cell lung cancer Metastatic ovarian or breast cancer
TAMOXIFENCI during pregnancy & lactation N Hot flashes Menstrual irregularities
Antineoplastic Estrogen receptor antagonist & partial agonist
Competes w/ estrogen for receptors in breast & other tissues Suppresses breast tumor growth
Breast cancer & ductal carcinoma following surgery & radiation Advanced breast cancer
TRASTUZUMABAbdominal pain Anorexia Diarrhea V Back pain Chills Fever Allergic rxns Doxorubicin risk of cardiotoxicity
Antineoplastic Monoclonal Ab
Binds human epidermal growth factor-2 (HER2) receptor on breast cancer cells Prevents receptor stim. & cell proliferation Regression of breast cancer metastases
Metastatic breast cancer w/ overexpression HER2
Combined w/ paclitaxel
blood levels
VINCRISTINEN, V Alopecia Peripheral neuropathy
Antineoplastic Vinca alkaloid, mitotic inhibitor
Binds tubulin & prevents polymerization of tubulin dimers forming microtubules of mitotic spindle M phase specific
Hodgkins ds Lymphoma Leukemia Neuroblastoma Rhabdomyosarcoma Wilms tumor
AUTONOMIC & NEUROMUSCULAR
Atenolol Atropine Dobutamine Edrophonium Epinephrine Phenoxybenzamine Phentolamine Phenylephrine Pilocarpine
Pralidoxime Propranolol Pseudoephrine Pyridostigmine Rocuronium Sildenafil Succinylcholine Tamsulosin Terazosin
ATENOLOLBronchoconstriction w/ high doses b/c 1 blockade Additive hypotension w/ nitrates
Sympatholytic, antihypertensive 1 receptor antagonist
1 receptor antagonist
Angina Post MI Hypertension
ATROPINE
Anticholinergic Muscarinic receptor antagonistMydriasis & cycloplegia Warm, dry, flushed skin Tachycardia Delirium Hallucinations
Muscarinic receptor blocker
Bradycardia IBS Anticholinesterase poisoning Antisecretory agent
DOBUTAMINETachycardia Arrhythmia
Sympathomimetic, cardiac stimulant 1 receptor agonist
Selective 1 receptor agonist
1 > 2 > 1
Cardiac contractility & output Acute heart failure Cardiogenic shock
Synergistic on cardiac output w/ nitroprusside
EDROPHONIUMMuscarinic effectsMiosis Salivation
Diagnostic agent Cholinesterase inhibitor
Reversible cholinesterase inhibitor
Dx myasthenia gravis
EPINEPHRINEHTN Tachycardia Ischemia Hyperglycemia
Sympathomimetic, bronchodilator, vasopressor Nonselective adrenergic agonist
Activates & receptors
IP3 & cAMP 1 vasoconstrict & BP 1 HR, conduction, & contractility 2 vasodilate, BP, bronchodilate
Cardiac arrest, V fib Shock, asthma COPD
PHENOXYBENZAMINEPostural hypotension Hypotension w/ blockers & Ca channel blockers
Vasodilator Irreversible receptor antagonist
receptor antagonist 1 > 2
Presurgical Tx of HTN d/t pheochromocytoma
PHENTOLAMINEHypotension Severe hypotension w/ Epi
Vasodilator receptor antagonist
Blocks 1 & 2 receptors
Control BP during surgical removal of pheochromocytoma
IV admin only
PHENYLEPHRINERebound nasal congestion HTN MAOI cause severe HTN
Vasocontrictor, decongestant
Selective 1 receptor
agonist
Activates 1 receptor
Increase IP3 causing contraction of vascular smooth m.
Nasal & ocular decongestant Dilate pupil for opthalmoscopy Mydriasis w/o cycloplegia
Paralysis of
PILOCARPINEMiosis Blurred visionAccommodative spasm
Antiglaucoma, sialogogue Muscarinic receptor agonist
Activates muscarinic receptors in ciliary m. & salivary gland
Sjogrens syn
Glaucoma
Ciliary m. aqueous humor
Xerostomia
Salivary gland salivation
PRALIDOXIME
Organophosphate antidote Cholinesterase reactivator
Binds phosphorous & breaks organophosphate bond w/ cholinesterase
Organophosphate toxicity Reverses muscle weakness
PROPRANOLOLBronchoconstriction Inhibits glycogenolysis Nightmares & depression
Sympatholytic, antihypertensive Nonselective receptor antagonist
Blocks 1 & 2 receptors
Angina HTN Benign tremor Migraine prophylaxis thyrotoxicosis Post-MI
Highly lipophilic CNS effects
PSEUDOEPHEDRINETachycardia CNS stim. BP MAOI cause severe HTN
Decongestant Indirect/directacting adrenergic receptor agonist
release NE directly activates adrenergic receptors causing vasoconstriction & cardiac stim.
Allergic & viral rhinitis
PYRIDOSTIGMINEMuscarinic effectsMiosis Salivation
Antimyasthenic Cholinesterase inhibitor, cholinergic agonistProlongs effects of succinylcholine
Reversibly inhibits cholinesterase
Tx myasthenia gravis Reverse nondepolarizing NM blockers
ROCURONIUMRespiratory m. paralysis Apnea
Paralytic agent Nondepolarizing NM blockade
Blocks nicotinic receptors in skeletal m.
Skeletal m. relaxation for intubation, surgery, ECT
Effects reversed by neostigmine & edrophonium
SILDENAFILHA Nasal congestion Back pain Visual disturbances
Vasodilator Phosphodiesterase inhibitor
Inhibits type 5 phosphodiesterase & degradation of cGMP
vasodilation in corpus cavernosum d/t Ach release from sacral PNS neurons
Erectile dysfunction
SUCCINYLCHOLINERespiratory m. paralysis Apnea
Paralytic agent Depolarizing NM blockade
Binds nicotinic receptors causing prolonged depolarization of skeletal m. & paralysis
Skeletal m. relaxation for intubation & surgery
Transient m. fasciculations
TAMSULOSINDizziness HA Postural hypotension Cimetidine increases blood levels & effects
Urologic agent Uroselective 1 receptor antagonist
Blocks 1A receptors in prostate
Tx urinary outflow obstruction d/t prostatic hyperplasia
TERAZOSIN1st dose syncope
Antihypertensive, urologic agent Selective 1 receptor antagonist
Blocks 1 receptors
HTN Outflow obstruction d/t prostate hyperplasia
CARDIOVASCULAR
Acetazolamide Adenosine Amiloride Amiodarone Amlodipine Carvedilol Clonidine Digoxin Diltiazem Dofetilide Enalapril Esmolol Fenoldopam Furosemide Hydralazine
Hydrochlorothiazide Labetalol Mannitol Methyldopa Minoxidil Nesiritide Nitroglycerin Nitroprusside Propafenone Quinidine Sotalol Spironolactone Valsartan verapamil
ACETAZOLAMIDEParasthesia Urinary stone formation
Diuretic Carbonic anhydrase inhibitor
Inhibits interconversion of carbonic acid & bicarbonate NaHCO3 excretion Inhibit aqueous humor formation Hyperchloremic metabolic acidosis
Tx open-angle glaucoma Mtn sickness Metabolic alkalosis
ADENOSINETransient asystole
Antiarrhythmic Purine nucleoside, cardiac node membrane stabilizer
Opens K channels & blocks Ca influx in SA & AV nodes Slows AV conduction AV refractory period
Terminate SVT
AMILORIDEHyperkalemia
K-sparring diuretic Epithelial Na channel blocker
Blocks Na Channel distal tubule & collecting duct
Inhibits Na reabsorption & K excretion
Prevent & Tx hypokalemia
AMIDARONEHypo/hyperthyroidism Photosensitivity Blue-gray skin Corneal microdeposits Pulmonary fibrosis
Antiarrhythmic Cardiac ion channel blocker
Blocks K, Na, Ca channels & receptors
Prolongs repolarization refractory period Slows HR PR & QT intervals
SVT, VT, VF
AMLODIPINEHA Edema Hypotension Effects w/ grapefruit juice
Antihypertensive, antianginal Dihydropyridine Ca channel blocker
Ca channel blocker in vascular smooth m. Arteriolar vasodilation & coronary blood flow
HTN Angina pectoris
CARVEDILOLOrthostatic hypotension Dizziness Bradycardia
Antihypertensive & heart failure Tx Nonselective adrenergic receptor agonist
Blocks 1, 2, 1 receptors Cause vasodilation
HTN Heart failure
remodeling
CLONIDINEAbrupt w/drawal severe rebound HTN Sedation Dry mouth
Antihypertensive 2 receptor agonist
Central 2 receptor agonist
sympathetic outflow from vasomotor center Inhibits pain neurotransmission in spinal cord
HTN Opioid w/drawal
DIGOXINArrhythmias N, V Blurred vision Yellow vision
Cardiac stimulant Digitalis glycoside
Inhibits Na/K ATPase
IC Ca & cardiac contractility AV conduction AV refractory period
Heart failure Serum levels assess dosage & toxicity
DILTIAZEMDizziness Hypotension Peripheral edema Constipation Gingival hyperplasia Grapefruit juice serum levels
Vasodilator, antiarrhythmic Non-dihydropyridine Ca channel blocker
Block Ca channels in cardiac tissue & vascular smooth m.
Vasodilation HR & conduction contractility
HTN Angina pectoris SVT
DOFETILIDEQT prolongation Torsade de pointes
Antiarrhythmic K channel blocker
Blocks delayed K channels in cardiac tissue
Slows repolarization & prolongs refractory period QT interval
AF, A flutter
Monitor QT interval during initial dose titration
ENALAPRILCough & angioedemaInhibits bradykinin degradation
Antihypertensive ACE inhibitor
Inhibits ACE & formation of AT II
Vasodilation aldosterone secretion CO V remodeling survival in heart failure
Hypotension Taste disturbances
HTN Heart failure Post-MI progression of diabetic nephropathy
ESMOLOLHypotension Bradycardia
Antiarrhythmic Class II Selective 1 blocker
Blocks SNS stim. SA & AV nodes
HR AV conduction AV refractory period
Sinus tachycardia & SVT during/after surgery
Rapidly metabolized by plasma esterase
FENOLDOPAM serum K levelsMonitor for hypokalemia
Antihypertensive D1-like receptor agonist
D1 receptor agonist
Arteriolar vasodilation
Afferent & efferent renal arterioles
renal blood flow
Hypertensive emergencies
FUROSEMIDEHypokalemia Metabolic alkalosis Hyperuricemia Hypomagnesemia ototoxicity of aminoglycoside ABX
Loop-acting diuretic Membrane ion transport inhibitor
Inhibits Na/K/2Cl cotransporter in ascending loop of Henle
Blocks NaCl reabsorption
Edema Heart failure HTN Hypercalcemia
Ca excretion Na/K exchange in collecting duct
HYDRALAZINEEdema Reflex tachycardia & MI Lupus syndrome
Antihypertensive. heart failure Vasodilator
Alters IC Ca metabolism
Relaxes arteriolar smooth m.
vasodilation
afterload
Heart failure in combo w/ isosorbide dinitrate
More effective than ACEI in black people
Moderate-severe HTN
HYDROCHLOROTHIAZIDEHypokalemia Metabolic alkalosis Hyperuricemia & gout excretion of lithium
Antihypertensive Thiazide diuretic
Inhibits NaCl transporter in distal tubule
excretion Na, K, Cl Ca excretion
HTN Nephrogenic DI Nephrolithiasis
LABETOLOLPostural hypotension Abrupt w/drawal cause lifethreatening HTN, arrhythmias, or MI
Antihypertensive Adrenergic & receptor antagonist
Selective 1 & nonselective 1, 2 blockers
HTN
MANNITOLElectrolyte imbalances Transient volume expansionPulmonary edema or heart failure
Diuretic Osmotic Diuretic
Osmotic attraction of edematous & ocular fluid
Filtered by glomerulus
electrolyte excretion
Oliguric renal failure Cerebral edema ICP Acute glaucoma
METHYLDOPAPositive direct Coombs test
Antihypertensive Adrenergic 2 receptor agonist
Converted to active form methylnorepinephrine which activates central 2 receptor agonist
SNS outflow from vasomotor center
HTN HTN in pregnancy
MINOXIDILSystemic admin.Reflex tachycardia Angina pericarditis Pulmonary HTN hypertrichosis
Antihypertensive, hair growth stimulant Vasodilator, K channel opener
Opens K channels in vascular smooth m.
Hyperpolarization m. relaxation vasodilation
Stim. resting hair follicle growth follicles
Severe HTN Topical for alopecia
NESIRITIDEHypotension
Heart failure Tx Recombinant human Btype natriuretic peptide
Activate guanylate cyclase cGaMP
Dilates venous & arterial smooth m. venous pressure, cardiac preload, vascular congestion, & dyspnea
Decompensated heart failure
NITROGLYCERINHA Hypotension Syncope Reflex tachycardia vasodilative effect of sildenafil, tadalafil, vardenafil
Antianginal Organic nitrate
Releases NO in vascular smooth m.
Vasodilation coronary blood flow myocardial O2 demand
Angina pectoris
Sublingual or lingual admin. Short half-life
NITROPRUSSIDECN toxicity Hypotension HA
Antihypertensive Vasodilator
Relaxes venous & arteriolar smooth m.
Metabolized to CN & thiocyanate
Tx toxicity w/ sodium nitrite & sodium thiosulfate
HTN crisis Acute heart failure or cardiogenic shock Controlled hypotension during pregnancy
PROPAFENONEProarrhythmic 1st 2 wksMonitor ECG when starting Tx
Antiarrhythmic Class IC Na channel blockerGI disturbances digoxin levels
Blocks Na channel in cardiac tissue conduction & prevent re-entry PR, QRS, & QT duration
SVT & life-threatening V arrhythmias
QUINIDINECinchonismBlurred vision Tinnitus Photophobia
Antiarrhythmic Class IA Na channel blocker
Blocks Na & K channels in cardiac tissue conduction QRS & QT duration
levels w/Amiodarone Cimetidine Diltiazem Verapamil Grapefruit juice
SVT & VT D-isomer = quinine, used to treat malaria pts
SOTALOLTorsades de pointes
Antiarrhythmic Class III K channel blocker
Blocks K channels in cardiac tissue
Prolongs repol. refractory period & QT interval
Blocks adrenergic receptors
SVT & life-threatening arrhythmias
SPIRONOLACTONEGynecomastia Impotence Hyperkalemia
K-sparring diuretic Aldosterone antagonist
Blocks aldosterone receptors Na excretion K excretion
Primary hyperaldosteronism HTN hypokalemia
VALSARTAN
Antihypertensive Angiotensin receptor antagonist
Blocks AT II receptor in vascular smooth m. & adrenal cortex
Vasodilation & aldosterone secretion
HTN Nephropathy
Less cough & angioedema than ACEI
VERAPAMILPeripheral edema Constipation Gingival hyperplasia
Antihypertensive, antianginal Non-dihydropyridine Ca channel blocker
Blocks Ca channels in cardiac m. & vascular smooth m.
Vasodilation HR & conduction contractility
Suppress contractility more than other Ca channel blockers
HTN Angina pectoris SVT Prevent migraine HA
CNS DEPRESSANTS
Buspirone Carbamazepine Diazepam Disulfiram Ethosuximide Flumazeil Gabapentin Lamotrigine
Lorazepam Phenobarbital Phenytoin Topiramate Valproate Zolpidem
BUSPRIONE
Antianxiety 5-HT1A partial agonist
Activates presynaptic 5HT1A receptors in dorsal raphe nucleus
firing serotonergic neurons
Generalized anxiety disorder
NO
Dizziness Drowsiness Fatigue HA Excitement Nervousness Blurred vision Tachycardia N Rash Myalgia Sweating levels byErythromycin Itraconazole Grapefruit juice
Drug dependence Significant sedation Muscle relaxation Anticonvulsant effects
CARBAMAZEPINEAtaxia Drowsiness Blurred vision Agranulocytosis Aplastic anemia Thrombocytopenia Induces its own metabolism
Anticonvulsant Neuronal Na channel blocker
Blocks Na channels in CNS
firing of ectopic foci & spread of epileptic seizures
Partial seizures & generalized tonic-clonic seizures Bipolar disorders Trigeminal neuralgia Neuropathic pain
DIAZEPAMDrowsiness Lethargy Physical/psychological dependence Tolerance
Antianxiety Benzodiazepine
Binds receptors on GABA operated Cl ion channel
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
DISULFIRAMDrowsiness
Alcohol abuse Tx Acetaldehyde dehydrogenase inhibitor
Inhibits acetaldehyde degradation following alcohol ingestion
Blurred vision Chest pain Dizziness Palpitations N, V HA Weakness
Reinforcement of alcohol abstinence
ETHOSUXIMIDEDizziness Drowsiness Gastric distress N
Anticonvulsant Succimide
Binds T-type Ca channels in thalamic neurons Suppresses nerve transmissions to motor cortex
Generalized absence seizures
Petit mal epilepsy
FLUMAZENILSeizures Dizziness Emotional lability
Antidote Benzodiazepine receptor antagonist
Blocks benzodiazepine receptors
Counteract adverse effects of benzodiazepines
Respiratory depression d/t IV OD
CI in status epilepticus
GABAPENTINAtaxia Dizziness Drowsiness Nystagmus Tremor
Anticonvulsant GABA analogue
GABA release from central neurons
Inhibits neuronal discharges from seizure foci Inhibits pain neurotransmission
Partial seizures Chronic pain Migraine prophylaxis
LAMOTRIGINESkin rash in 1st 8 wk of TxCan progress to Stevens-Johnson syn
Anticonvulsant Phenyltriazine
Blocks voltagesensitive Na channels
Release of glutamate Prevents spread of seizure foci discharges
Ataxia Dizziness Drowsiness Photosensitivity metabolism & ADR w/ valproate
Adjunct/monotherapy for partial seizures in adults
LORAZEPAMDizziness Drowsiness Apnea & cardiac arrest w/ rapid IV admin Additive depression w/ alcohol & other depressants
Sedative-hypnotic, anxiolytic Benzodiazepine
Binds benzodiazepine receptors on GABA operate Cl ion channel
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
PHENOBARBITALDrowsiness Lethargy Delirium Hangover Physical & psychological dependence Induces CYP P450 metabolism of drugs
Sedative-hypnotic, anticonvulsant Barbiturate
Binds GABA operated Cl ion channel 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
PHENYTOINAtaxia Diplopia Nystagmus Gingival hyperplasia
Anticonvulsant Hydantoin
Blocks voltage-sensitive Na channels
Release glutamate 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
TOPIRAMATE
Anticonvulsant Monosaccharide derivative
Block voltage-sensitive Na channels
Augments GABA activation of GABA receptors
Blocks glutamate receptors
Ataxia Dizziness Drowsiness Fatigue Impaired concentration & memory Psychomotor slowing Speech problems Diplopia Nystagmus
Partial & tonic-clonic seizures
Decrease dose in pts w/ renal impairment
VALPROATEIndigestion N, V Dizziness Sedation Hepatotoxicity
Anticonvulsant Branched-chain FA
GABA levels by release or metabolism or reuptake
Reduced Na dependent action potentials
Simple & complex absence seizures Complex partial seizures Tonic-clonic seizures Myoclonic seizures Migraine prevention Manic phase of bipolar
ZOLPIDEM
Non-benzodiazepine hypnotic Imidazopyridine
Activates BZBP receptors on GABA operated Cl ion channel
channel affinity for GABA & frequency of channel opening
Neuronal hyperpolarization
Insomnia
ENDOCRINE
Acarbose Alendronate Calcitonin Danazol Desmopressin Ergocalciferol Ethinyl estradiol & drospirenone Ethinyl estradiol & norethindrone Finasteride Fludrocortisone Glyburide Hydrocortisone
Insulin Levothyroxine Medroxyprogesterone Metformin Methimazole Mifepristone Octreotide Oxytocin Pioglitazone Prednisone Raloxifene Repaglinide Somatropin Testosterone
ACARBOSEIntestinal bloating Flatulence oral bioavailability of metformin iron absorption
Antidiabetic -glucosidase inhibitor
Inhibits intestinal enzyme that converts oligosaccharides & disaccharides to glucose digestion of starch & sucrose postprandial blood glucose & HbA1c
Type II DM
ALENDRONATEAbsorption by Ca supplements, antacids, foods, beverages (except water)
Bone resorption inhibitor Bisphosphonate
Prevents attachment of osteoclast precursor cells to bone metabolic activity of osteoclasts & ability to resorb bone
Prevent/Tx
Osteoporosis Corticosteroid-induced osteoporosis Pagets ds of bone hypercalcemia
CALCITONIN
Ca hormone Thyroid gland hormone
Binds calcitonin receptor on osteoclasts
cAMP & inhibits osteoclast activity
bone resorption, bone pain, & serum [Ca]
Postmenopausal osteoporosis Pagets ds of bone hypercalcemia
DANAZOLCI in pregnancy androgenic effects on female fetus Emotional lability Deepening voice Acne Hirsutism Amenorrhea breast size
Ovarian inhibitor Synthetic androgen, antiestrogen
Feedback inhibits pituitary FSH & LH secretion ovarian estrogen secretion & stim. endometrial & breast tissue.
Endometriosis Fibrocystic breast ds Hereditary angioedema
C1 esterase inhibitor & C4 complement component
DESMOPRESSIN
Posterior pituitary hormone Vasopressin, ADH analogue
Mimics natural vasopression
Increases water reabsorption in kidneys Vasoconstriction
DI Nocturnal enuresis Control bleeding in hemophilia & wWFs ds
Intranasal, oral, or IV
ERGOCALCIFEROLHypercalcemia Hypercalciuria
Vit. D Fat-soluble
Activated in liver & kidneys to form calcitriol
Ca & phosphorus absorption from gut
Cholestyramine inhibits vit. D absorption Induce vit. D metabolismPhenytoin Barbiturates
Vit. D deficiency
Rickets, osteomalacia
Chronic renal failure Familial hypophosphatemia Hypocalcemia d/t hypoparathyroidism Postoperative & idiopathic tetany
ETHINYL ESTRADIOL & DROSPIRENONEDrospirenone Antiandrogenic Blocks aldosterone salt & water retention BP
OCP Estrogen & progesterone
Feedback inhibit GnRH
Estrogen
FSH secretion & maturation of dominant follicle
Progesterone
Thromboembolis m risk w/ smoking
Inhibits midcycle LH surge & ovulation
Edema Efficacy w/ABX Carbamazepine phenytoin
Contraception Regulate menstrual cycle Acne in women
ETHINYL ESTRADIOL & NORETHINDRONENorethidroneSlightly androgenic
OCP Estrogen & progesterone
Feedback inhibit GnRH
Estrogen
FSH secretion & maturation of dominant follicle
Thromboembolism Edema Depression Gallbladder ds
Progesterone
Inhibits midcycle LH surge & ovulation
Contraception
Regulate menstrual cycle Acne in women
FINASTERIDECI pregnancyRisk to male fetus Do NOT handle tablets
Androgen synthesis inhibitor 5--reductase inhibitor
Inhibits conversion testosterone dihydrotestosterone & androgenic stimulation of prostate & skin prostate size & promotes hair growth
Impotence
BPH Male pattern baldness
FLUDROCORTISONEHypokalemia by thiazide & loop diuretics
Corticosteroid Mineralocorticoid
Activates aldosterone receptors in renal distal tubule
Na reabsorption K & H excretion
Adrenal insufficiency
Addisons ds
Congenital adrenogenital syn
Tx idiopathic orthostatic hypotension w/ Na intake
GLYBURIDEPhotosensitivity Hypoglycemia
Antidiabetic Sulfonylurea hypoglycemia
Closes ATP-sensitive K channels preventing K efflux & depolarizing pancreas B cells
Influx Ca & relaxing insulin
amount of insulin secreted during each pulse
Type II DM
HYDROCORTISONE
Short-acting corticosteroid, low-potency topical corticosteroid Glucocorticoid
Replaces endogenous cortisol in deficiency states Suppresses inflammation & immune response topical
Adrenocortical insufficiency Topical
Insect bites Contact dermatitis
INSULINHypoglycemia
Antidiabetic Pancreatic hormone-blockers mask signs of hypoglycemia & prolong recovery
Replaces endogenous insulin
DM
Rapid acting lispro Intermediate acting lente Long acting ultralente
LEVOTHYROXINEInsomnia Irritability Tachycardia Wt loss Bile acid sequestrants absorption
Thyroid hormone Tetraiodothyronine
Binds nuclear receptors & gene transcription
metabolic rate, protein synthesis, gluconeogenesis, cell growth & differentiation, & CNS development
Converted to T3 in tissues
Hypothyroidism
MEDROXYPROGESTERONEAmenorrhea Breakthrough bleeding Dysmenorrhea
Progestin, contraceptive Progesterone analogue
endometrial hyperplasia in women receiving estrogen Prevents conception by thickening cervical mucus
Estrogen-progestin HRT Injectable contraceptive Progestin-only injectable contraceptive
IM depot injection lasts 3mo
METFORMINN, V, D Abdominal bloating
Antidiabetic Biguanide, antihyperglycemic
# & affinity of insulin receptors in peripheral tissues hepatic glucose output glucose absorption from gut glucose uptake & utilization in skeletal m. & adipose tissue
Type II DM
Used in combo w/ sulfonylureas
METHIMAZOLERash Agranulocytosis
Antithyroid Thiourea, thyroid hormone synthesis inhibitor
Inhibits peroxidase & iodination & coupling of tyrosine residue of thyroglobulin thyroxine secretion
Hyperthyroidism Graves ds
MIFEPRISTONEAbdominal pain Diarrhea N, V Uterine bleeding Cramping
Abortificient Progesterone antagonist
Partial agonist or antagonist progesterone receptors
Medical termination of pregnancy through 49d gestation
Single dose + prostaglandin for 48hr stim. uterine contractions
OCTREOTIDEArrhythmias Hyperglycemia Hypoglycemia Constipation Diarrhea Flatulence N
GH inhibitor, antidiarrheal Somatostatin analogue w/ greater effects on GH than insulin secretion
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
OXYTOCINExcessive & painful uterine contractions
Oxytocic Posterior pituitary hormone
Stim. Uterine smooth m. & induce labor 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
PIOGLITAZONE
Antidiabetic Thiazolidinedione antihyperglycemic
Activates peroxisome proliferator-activated receptor- in adipose tissue, skeletal m., & liver gene transcription, insulin sensitivity, & glucose transports in muscle & adipose tissue Suppresses hepatic glucose output
Type II DM
Used w/ metformin
PREDNISONE
Anti-inflammatory Corticosteroid
Suppresses inflammation & immune response
Inflammatory, allergic, autoimmune, & neoplastic ds Prevent organ transplant rejection Asthma
Depression or euphoria HTN Acne Impaired wound healing Adrenal suppression Muscle wasting Osteoporosis Cushingoid appearanceMoon facies Buffalo hump
susceptibility to infection
RALOXIFENEHot flashes Cholestyramine inhibits absorption
Bone resorption inhibitor Selective estrogen receptor modulator SERM
Estrogen-like effect on 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
REPAGLINIDEHypoglycemia
Antidiabetic Meglitinide hypoglycemic
Closes ATP-sensitive K channels & insulin secretion postprandial blood glucose & [HbA1c]
Taken before meals to control postprandial hyerglycemia
Used w/ metformin NOT sulfonylureas
SOMATROPIN
GH Recombinant somatotropin
release of insulin-like growth factors in liver & 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
TESTOSTERONEEdema Acne Gynecomastia Impotence Oligospermia Priapism
Androgen Gonadal steroid
Activated gene transcription & development of male sex organs & secondary sex characteristics lean body mass Stim. skeletal growth Accelerates epiphyseal closure sebaceous gland sebum production EPO secretion HDL levels
Hypogonadism in androgendeficient men Delayed puberty in males
GASTROINTESTINAL
Bisacodyl Calcium carbonate Dicyclomine Docusate Lactulose Loperamide Mesalamine Metoclopramide
Misoprostol Omeprazole Ondansetron Promethazine Ranitidine Sucralfate Tegaserod
BISACODYLCramping N Fluid & electrolyte depletionHypokalemia
Stimulant laxative
Inhibits GI fluid reabsorption & stimulates peristalsis
Bowel evacuation prior colonoscopy or surgery Acute constipation
CALCIUM CARBONATEConstipation absorption of drugsTetracyclines Fluoroquinolones Phenytoin Iron salts
Antacid, Ca supplement Ca salt
Neutralizes gastric acid Provides Ca supplementation
Dyspepsia Hypocalcemia Prevention of osteoporosis
Admin 1-1.5hr after meals & @ bedtime
DICYCLOMINEConstipation Dyspepsia Dry mouth Urinary retention Blurred vision Decreased sweating
Antispasmodic Muscarinic receptor antagonist
Blocks PNS stim. intrinsic nervous system & GI tone & motility
Directly relaxes GI smooth m.
IBS cramping & pain
DOCUSATE
Stool softener, laxative Surface-active agent
Facilitates hydration of fecal material & softens feces
Constipation Fecal impaction rectal enema
LACTULOSECramping Abdominal distention Flatulence
Laxative Osmotic agent
water content & softens feces Lowers pH of colon
Converts ammonia ammonium ion & ammonia absorption & blood levels
Chronic constipation Hepatic encephalopathy
Improves mental status
LOPERAMIDEConstipation Drowsiness Additive effectsKava Chamomile Valerian
Antidiarrheal Opioid analogue
Activates opioid receptors in GI smooth m.
Segmental contraction & inhibits peristalsis
Mild-moderate acute diarrhea Chronic diarrhea d/t IBD volume of ileostomy drainage
AVOID
Pregnancy Lactation Children < 2 y/o
MESALAMINE
GI anti-inflammatory Salicylate 5-ASA
Inhibits prostaglandin synthesis & migration of inflammatory cells into bowel wall Scavenges superoxide-free radicals
IBD UC Proctitis
Sulfasalazine mesalamine & sulfapyridine
METOCLOPRAMIDECI in Parkinsons ds & seizure disorders Drowsiness EPS rxns restlessness
Promotility & antiemetic D2 receptor antagonist
Blocks relaxant effect of D on GI smooth m. Blocks presynaptic D receptors & Ach release & stim. smooth m. Blocks D2 receptors in chemoreceptor trigger zone & vomiting center
Chemotherapy-induced emesis Gastric stasis postsurgical & diabetic GE reflux
MISOPROSTOLCI in pregnancy Abdominal pain D Miscarriage
Cytoprotective Synthetic PGE1 analogue
gastric mucosal secretion & secretion of bicarbonate & mucus
Prevent gastric mucosal injury from NSAIDs Abortificient in combo w/ mifepristone
OMEPRAZOLEAbdominal pain Inhibits metabolismDiazepam Cyclosporine Phenytoin
Antiulcer Proton pump inhibitor
Irreversibly inhibits H/K ATP pump in gastric parietal cells
Prevents gastric acid secretion
Peptic ulcer ds GE reflux Zollinger-Ellison syn dyspepsia
ONDANSETRONHA Constipation D
Antiemetic 5-HT3 receptor antagonist
Blocks 5-HT3 receptors in GI vagal afferent nerves, solitary tract nucleus, & chemoreceptor trigger zone
Prevent N, V from chemotherapy & radiation therapy Postoperative N, V
PROMETHAZINENeuroleptic malignant syn Sedation Confusion Disorientation
Antiemetic, antihistamine, sedative H1 receptor antagonist, phenothiazine
Blocks H1 & M1 receptors Inhibits stim. chemoreceptor trigger zone & vomiting center
N, V Preoperative sedation Allergic rxns
RANITIDINE
Antiulcer H2 receptor antagonist
Blocks H2 receptors in gastric parietal cells
gastric acid secretion
Peptic ulcer ds GE reflux Dyspepsia
SUCRALFATEConstipation absorptionFat soluble vitamins fluoroquinolones
Antiulcer Cytoprotective, sulfated polysaccharide
Adheres ulcer crater & forms protective barrier Prevents acid secretion & pepsin hydrolysis of mucosal proteins Stim. prostaglandin synthesis
Peptic ulcer ds GE reflux Prevent NSAID-induced gastric injury
TEGASERODDiarrhea Ischemic colitis
GI motility agent Partial agonist @ 5HT4 receptors
Activates 5-HT4 receptors on sensory neurons in enteric nervous system
Release neurotransmitters & peristalsis
IBS in women w/ constipation
HEMATOLOGIC
Abciximab Alteplase Aspirin Atorvastatin Bivalirudin Cholestyramine Cilostazol Clopidogrel Cyclosporine Enoxaparin
Epoetin Eptifibatide Ezetimibe Filgrastim Folic acid Gemfibrozil Heparin Niacin Sirolimus Warfarin
ABCIXIMABBleeding Thrombocytopenia
Antithrombotic Monoclonal Ab
Inactivates platelet gp llb/llla receptors
Prevents platelet aggregation
Prevent thrombosis during coronary angioplasty & stent placement
ALTEPLASEReperfusion arrhythmia ContraindicationsInternal bleeding Recent CNS surgery or trauma
Thrombolytic Plasminogen activator
Converts plasminogen plasmin
Degrades fibrin & fibrinogen
AMI Acute ischemic stroke Occluded central venous access devices
Streptokinase & urokinase for pulmonary embolism
ATORVASTATINMyalgia Myositis Rhabdomyolysis Hepatitis GI distress Effects w/Grapefruit juice Azole antifungals cyclosporine
Cholesterol lowering agent HMG-CoA reductase inhibitor
HMG-CoA reductase, ratelimiting enzyme for cholesterol
hepatic cholesterol uptake LDL levels
Hypercholesterolemia
Cholesterol-lowering effects w/ ezetimibe & bile acidbinding agents
BIVALIRUDINBleeding
Anticoagulant Hirudin analogue
Inhibits thrombin
Prevents blood coagulation
Thrombosis in unstable angina AMI Stent insertion
Used in pts w/ heparininduced thrombocytopenia
CHOLESTYRAMINEConstipation Abdominal discomfort
Cholesterol-lowering agent Bile-acid binding resin
Binds intestinal bile acids
Prevents reabsorption cholesterol utilization
LDL levels
Hypercholesterolemia Diarrhea d/t excess bile acids
CILOSTAZOLHA Effects w/ CYP3A4 inhibitorsAzole antifungals Erythromycin Grapefruit juice
Antiplatelet Platelet aggregation inhibitor
Inhibits phosphodiesterase III & cAMP in platelet & blood vessels
Inhibit platelet aggregation Causes vasodilation
Intermittent claudication
Improves blood flow & walking distance
Additive effects w/ aspirin
CLOPIDOGRELHypersensitivity reaction
Antiplatelet Platelet aggregation inhibitor
Irreversibly inhibits binding of ADP to platelet receptors
gp IIb/IIIa mediated aggregation
Stroke MI Peripheral vascular ds
Additive effects w/ aspirin
CYCLOSPRINEHTN Nephrotoxic Gingival hyperplasia Hirsutism Tremor Induce metabolismRifampin Barbiturates Carbamazepine
Immunosuppressant IL2 expression inhibitor
Bind immunophilins
Complex binds calcineurin inhibits transcription of IL2 gene
Inhibits metabolismGrapefruit juice
Prevent rejection of renal, cardiac or hepatic allografts Severe RA & psoriasis
ENOXAPARINThrombocytopenia
Parenteral anticoagulant LMWH
Binds/potentiates antithrombin III on factor Xa
Prevent
DVT Pulmonary embolism after knee, hip, or abdominal surgery Thrombosis in unstable angina & non Q-wave MI
Effects reversed w/ protamine sulfate NO monitoring w/ PTT
EPOETINHTN
Hematopoietic growth factor Recombinant human EPO
Binds receptors on erythroid progenitor cells & stim. cell maturation & prolif.
Reticulocytosis & Hct
Anemia d/t
CRF Chemotherapy Zidovudine therapy Hematologic malignancy
lymphoma
Used as performance-enhancing drug by athletes
EPTIFIBATIDEBleeding
Antiplatelet GP IIb/IIIa receptor antagonist
Reversibly inhibits fibrinogen binding to gp IIb/IIIa receptors
Prevents platelet aggregation
Prevent coronary thrombosis in
Unstable angina or non-ST segment elevation MI Coronary angioplasty or stent placement
EZETIMIBE
Cholesterol-lowering agent Cholesterol absorption inhibitor
Disrupts annexin-caveolin complex mediating cholesterol transport intestinal brush border Inhibits absorption of biliary dietary cholesterol
Pro-drug converted to active glucuronide metabolite
Hypercholesterolemia
Additive effect w/ statins
FILGRASTIMBone pain
Hematopoietic growth factor Recombinant human GCSF
Binds receptors on myeloid progenitor cells & stim. maturation & prolif. Accelerates neutrophil recovery after myelosuppressive chemotherapy
infection incidence
Neutropenia assoc/ w/ chemotherapy & bone marrow transplants
Avoid 24 hrs prior & after chemotherapy
FOLIC ACIDAbsorption byPhenytoin Cholestyramine
Vitamin, hematologic agent Metabolic cofactor for DNA synthesis
Activated folate transfer one-carbon units to purine & pyrimidine precursors
Folate reductase inhibited by MTX
Megaloblastic anemia Fetal neural tube defects Coronary artery ds
Pregnant woman have requirements
GEMFIBROZILGI distress Myositis Statins risk rhabdomyolisys
Lipid-lowering agent Fibric acid derivative
Activates peroxisome proliferator activated receptor-
Oxidizes FA & apo-AI & AII plasma triglycerides HDL
Hypertriglyceridemia HDL levels
Monitor LFTs throughout Tx
HEPARINThrombocytopenia
Parenteral anticoagulant Antithrombotic
Binds/potentiates antithrombin III
inactivation factor Xa & thrombin
Venous thromboembolism Pulmonary embolism AF w/ embolism Consumptive coagulopathies In vitro & catheter coagulation
Monitor PTT Protamine sulfate for OD
NIACINFlushing Pruritis GI distress, peptic ulcer Hyperglycemia Hepatotoxicity Statins risk rhabdomyolysis
Vitamin, lipid-lowering agent G-protein coupled receptor ligand
Activates G-protein coupled receptor
Inhibits lipolysis & release of FA hepatic triglyceride synthesis & VLDL secretion
Hypertriglyceridemia HDL Hypercholesterolemia Pellagra
SIROLIMUSLeukopenia Thrombocytopenia Hyperlipidemia Rash blood levelsCyclosporine Azole antifungals Erythromycin Grapefruit juice Cimetidine
Immunosuppressant T-lymphocyte inhibitor
Inhibits regulatory kinase in cytokinedriven T-cell prolif.
Combo w/ corticosteroid & cyclosporine
Prevent
Rejection renal allograph Coronary stent restenosis
WARFARINFetal malformations Abnormal bone development
Oral anticoagulant Coumarin vit. K antagonist
Inhibits reduction of oxidized vit. K
Prevents vit. K dependent carboxylation of glutamate residues of factors II, VII, IX, X, proteins C & S
Delayed onset d/t circulating coagulation factors
Monitor INR Give vit. K if bleeding
MUSCULOSKELETAL
Acetaminophen Allopurinol Celecoxib Cyclobenaprine Etanercept Ibuprofen
Indomethacin Infliximab Ketorolac Probenecid & colchicine
ACETAMINOPHENOD cause fatal hepatic failure hepatotoxicity w/ alcohol renal toxicity w/ salicylates & NSAIDs
Analgesic, antipyretic COX-3 inhibitor
Inhibits COX-3 selectively Inhibits synthesis of PG causing pain & fever
Mild-moderate pain Fever
Lacks anti-inflammatory & antiplatelet activity
ALLOPURINOLRash Inhibits metabolismMercaptopurine
Antigout Xanthine oxidase inhibitor
Inhibits xanthine oxidase & catabolism of purines xanthine & uric acid
uric acid levels
Prevent hyperuricemia & gout
CELECOXIBGI bleeding risk stroke & MI
NSAID COX-2 inhibitor
Inhibits COX-2 & synthesis of PG causing pain, fever, & inflammation
OA RA Inflammatory jt ds
CYCLOBENZAPRINEDizziness Drowsiness Dry mouth AVOID MAOI
Skeletal m. relaxant Tricyclic centralacting m. relaxant
Acts on brainstem & spinal cord to reduce tonic somatic m. activity via & motor neurons
Acute muscle spasm
ETANERCEPTURI HA Ab response to live virus vaccines
Antirheumatic agent, antitumor necrosis factor Antitumor necrosis factor p57 combined w/ Fc of IgG
Binds TNF- & jt inflammation & pain Slows progression of RA
RA
IBUPROFENGI bleeding N, V Dyspepsia Allergic rxns Hepatitis & renal failure
NSAID Nonselective COX inhibitor
Inhibits COX-1 & COX-2 & synthesis of PG causing pain, fever, & inflammation
Mild-moderate pain or dysmenorrhea Inflammatory disorders
OA RA
risk colon, breast, lung, & prostate cancers
INDOMETHACIN
NSAID Nonselective COX inhibitor
Inhibits COX-1 & COX-2
Inflammatory disorders
GI bleeding N, V Dyspepsia Allergic rxns Dizziness Drowsiness HA
Gouty arthritis OA RA Ankylosing spondylitis
PDA in premature neonates
INFLIXIMABFatigue N, V URI
Ds modifying antirheumatic Monoclonal Ab to TNF-
Inactivates TNF- & jt inflammation, pain, & destruction Sx of Crohns ds
RA Crohns ds
KETOROLACAspirin-allergy Allergic rxn in pt w/ asthma Nasal polyps
NSAID Nonselective COX inhibitor
Inhibits COX-1 & COX-2 & synthesis of PG causing pain, fever, & inflammation
Short-term pain management
Prolongs bleeding time
Limit use to < 5d
PROBENECID & COLCHICINEProbenecidInhibits renal tubular secretion of PenicillinsUsed to penicillin serum levels
Antigout Uricosuric probenicid Anti-inflammatory colchicine Colchicine
Probenecid
Inhibits renal reabsorption of uric acid & uric acid secretion
D N, V Agranulocytosis & aplastic anemia
Colchicine
Inhibits leukocyte response to monosodium urate crystals in jt
Acute gouty arthritis Prevent gouty arthritis
NEURODEGENERATIVE
Baclofen Benztropine Donepezil Entacapone Interferon-beta-1b
Levodopa-carbidopa Memantine Pergolide Selegiline
BACLOFENDrowsiness Dizziness Fatigue Weakness Additive effectsAlcohol Kava Valerian Chamomile
Antispasticity GABA-B receptor agonist
neuronal cAMP & Ca influx
K influx motor neuron excitability & inhibits spinal reflexes
Spasticity
MS Spinal cord injury ALS
BENZTROPINEBlurred vision Dry eyes Constipation Dry mouth Urinary retention
Anti-Parkinson Central anticholinergic
Blocks cholinergic receptors & restores neurotransmitter balance in basal ganglia
Parkinsons ds Drug-induced EPS
tremor > bradykinesia & rigidity
DONEPEZILN, D HA
Anti-Alzheimer Cholinesterase inhibitor
Inhibits cholinesterase in CNS
Ach neurotransmission Slows decline in cognitive function
Alzheimers ds
Does NOT prevent ds progression
ENTACAPONERhabdomyolysis Neuroleptic malignant syndrome
Anti-Parkinson Catechol-Omethyltransferase inhibitor
Inhibits catechol-omethyltransferase inactivation of levodopa
levodopa in CNS Prolongs response to levodopa & S/Sx Parkinsons ds
Adjunct to levodopa/carbidopa for Parkinsons ds
AVOID nonselective MAOI
INTERFERON-BETA-1B
Anti-multiple sclerosis Interferon
Binds cell surface receptors producing immuno-suppressive effects
relapse & slows physical disability in MS
HA Weakness GI distress Sweating Neutropenia Myalgia Chills Fever
Relapsing-remitting MS
SubQ daily
LEVODOPA-CARBIDOPADyskinesia involuntary movements N, V Hallucinations arrhythmia w/ halothane
Anti-Parkinson Dopamine precursor, decarboxylase inhibitor
Levodopa
Converted to D in CNS
Augments neurotransmission in basal ganglia
Carbidopa
Inhibits peripheral dopadecarboxylase
levodopa availability in CNS
Parkinsons ds
HTN crisis w/ MAOI
MEMANTINE
Anti-Alzheimer Glutamate antagonist
Glutamate NMDA receptor antagonist
Prevent excitotoxic effects of glutamate causing neuronal loss Slows decline in cognitive function
Alzheimers ds
PERGOLIDEDyskinesia Hallucination Orthostatic hypotension Constipation
Anti-Parkinson Dopamine receptor agonist
Activates D receptors in basal ganglia
Parkinsons ds in conjunction w/ levodopa/carbidopa
SELEGILINEAVOID Meperidine & opioidsFatal rxn Excitation Rigidity HTN coma
Anti-Parkinson Type B MAOI
SSRISerotonin syn
Converted to active form by MAO Irreversibly inhibits D degradation by MAO
TricyclicsAsystole HTN Syncope Rigidity seizures
response to levodopa/carbidopa Tx
Parkinsons ds w/ levodopa/carbidopa
Slows progression of Parkinsons ds
OTHER DRUGS
Alprostadil Bosentan Epoprostenol
Latanoprost Mesna Succimer
ALPROSTADILIV infusionApnea Hypotension Arrhythmia
Vasodilator Prostaglandin E1Local products
Activates PG EP receptors
Vascular smooth m. relaxation & vasodilation
Prolonged/painful erection lightheadedness
Maintain PDA in neonates awaiting surgery
IV infusion
Male erectile dysfunction
Local injection or pellets
BOSENTANCI in pregnancyCauses birth defects
Vasodilator Endothelin-1 receptor antagonist
Blocks endothelin A & B receptors pulmonary vascular resistance & dyspnea Improves walking distance
serum aminotransferase levels
Pulmonary arterial HTN
EPOPROSTENOLFlushing Hypotension Tachycardia Diarrhea N, V
Vasodilator Naturally occurring prostacyclin (PGI2)
Activated prostaglandin IP receptors
Vascular smooth m. relaxation
pulmonary blood flow & reduces dyspnea
Pulmonary arterial HTN
LATANOPROSTAlters color of iris causing permanent eye color change by amount of melanin in melanocytes
Ocular hypotensive agent Prostaglandin F2 analogue
Activates prostaglandin FP receptors aqueous humor outflow via uveoscleral pathways Lowers intraocular pressure
Chronic open-angle glaucoma
Topical ocular admin
MESNA
Antidote Sulfhydryl compound
Detoxifies urotoxic metabolites acrolein of ifosfamide & cyclophosphamide
Hemorrhagic cystitis d/t ifosfamide & cyclophosphamide
SUCCIMER
Antidote Metal chelating agent dimercaptosuccinic acid
Chelates lead
Water-soluble chelates to excreted in urine
blood lead levels
PSYCHOTHERAPEUTICS
Amitriptyline Amphetamine & dextroamphetamine Atomoxetine Buproprion Desipramine Fluoxetine Haloperidol Lithium
Methylphenidate Mirtazapine Olanzapine Phenelzine Risperidone Thioridazine Venlafaxine
AMITRIPTYLINELethargy Sedation Blurred vision Constipation Urinary retention appetite & wt gain OD wide QRS complex VT Altered effects by drugs that inhibit/induce CYP450Carbamazepine Quinidine Rifampin
Antidepressant Tricyclic
Blocks neuronal reuptake of serotonin > norepinephrine Blocks muscarinic & adrenergic receptors
Chronic pain Depression
Delayed onset of antidepressant effect >4 wks
AVOID
MAOI SSRI
AMPHETAMINE
CNS stimulant Sympathomimetic amineTachycardia HTN Anorexia Irritability Insomnia Tremor Growth inhibition Drug dependence
neuronal release of norepinephrine
ADHD
attention span motor restlessness
HTN crisis w/ MAOI
Narcolepsy
mental alertness drowsiness & fatigue
ATOMOXETINE appetite Insomnia Levels & effects altered by drugs that inhibit/induce CYP2D6
ADHD agent Selective NE reuptake inhibitor
Inhibits neuronal reuptake of NE in CNS
ADHD in children/adults
levels & effect in slow metabolizers CYP2D6
BUPROPION
Antidepressant Neuronal reuptake inhibitor
Inhibits neuronal reuptake of DA > 5-HT & NE
Agitation HA Dry mouth N Tremor Impaired motor & cognitive skills MAOI adverse effects Seizure risks w/ phenothiazines
Depression Smoking cessation
Delayed onset for antidepressant effects
DESIPRAMINELethargy Sedation Blurred vision Constipation Urinary retention appetite & wt gain OD wide QRS complex VT
Antidepressant Tricyclic
Blocks neuronal reuptake NE > 5-HT Blocks muscarinic & adrenergic receptors
Depression Chronic pain
Delayed onset for antidepressant effects
AVOID
MAOI SSRI
FLUOXETINE
Antidepressant SSRI
Inhibits neuronal reuptake of serotonin
Anxiety Drowsiness Insomnia Nervousness Sexual dysfunction Sweating Tremor levels metabolized by CYP2D6
Depression OCD Bulimia nervosa Anorexia nervosa Fibromyalgia Panic attacks Phobias Prementsrual dysmorphic disorder
Active metabolite 5-7d half-life AVOID MAOI
HALOPERIDOLNeuroleptic malignant synFever Respiratory distress Tachycardia Seizures Severe m. stiffness Altered BP
Typical antipsychotic Butyrophenone
Blocks D2 receptors in mesolimbic area, chemoreceptor trigger zone, solitary tract, & basal ganglia Blocks muscarinic & adrenergic receptors
Psychotic disorders
Schizophrenia
Extrapyramidal rxns Tardive dyskinesia Blurred vision Constipation Dry mouth Urinary retention Hypotension
Tourettes syn
LITHIUMPolyuria Impaired memory Acne Tremor ECG changes GI distress Hypothyroidism Leukocytosis
Mood stabilizer, antimanic Inorganic cation
noradrenergic neurotransmission or effects b/c of cAMP Inhibition of inositol-1phosphataseDiuretics NSAIDS Fluoxetine
Depletion of inositol & IP3
NM toxicity w/ haloperidol toxicity
Improved Na transport via Na pump
Bipolar affective disorder
Monitor serum levels
Toxicity > 2.5
METHYPHENIDATE
CNS stimulant Sympathomimetic amine
neuronal release NE
ADHD
attention span motor restlessness
Tachycardia HTN Anorexia Irritability Insomnia Tremor Growth inhibition Dependence HTN crisis w/ MAOI
Narcolepsy
mental alertness drowsiness & fatigue
MIRTAZAPINE appetite & wt gain Constipation Dry mouth Drowsiness
Antidepressant Tetracyclic
Inhibits presynaptic 2 autoreceptors & heteroreceptors
NE & 5-HT release
Depression Appetite stimulation
AVOID MAOI
HTN, seizure, death
OLANZAPINE
Atypical antipsychotic Thienobenzodiazepine
Blocks D2 & 5-HT2 receptors in CNS Blocks H1, muscarinic, & adrenergic receptors
Schizophrenia Manic episodes of biploar Anorexia nervosa
Agitation Dizziness Restlessness Sedation Amblyopia Orthostatic hypotension Tachycardia Constipation Dry mouth Wt gain Tremor
Oral tablets contain aspartame
Avoid in phenylketonuria
PHENELZINE
Antidepressant MAOI
Inhibits MAO & CNS levels of NE & 5-HT
Dizziness Insomnia Restlessness Blurred vision Orthostatic hypotension Diarrhea Potentially fatalSSRI Tricyclics
Neurotic & atypical depression
Avoid
Fluoxetine Tyramine
HTN crisisTyramine Amphetamines Methyldopa Levodopa
RISPERIDONEAggressive behavior Extrapyramidal rxns Sleep disturbances Insomnia Sedation Constipation or diarrhea Wt gain
Atypical antipsychotic Benzisoxazole
Blocks 5-HT2 > D2 receptors in CNS Blocks H1 & adrenergic receptors
Schizophrenia Psychotic disorders
Monitor pt for neuroleptic malignant syn
THIORIDAZINEExtrapyramidal rxns Tardive dyskinesia Photosensitivity Potential for V arrhythmias & sudden death Retinal pigmentation w/ high dosesmelanosis
Typical antipsychotic Phenothiazine
Blocks D2 receptors in mesolimbic area, chemoreceptor trigger zone, solitary tract, & basal ganglia Blocks muscarinic receptors
Psychotic disorders Schizophrenia
VENLAFAXINESexual dysfunction GI distress Dizziness Insomnia Nervousness
Antidepressant Phenethylamine
Inhibits neuronal reuptake 5-HT & NE
Depression Generalized anxiety disorder
AVOID MAOI
RESPIRATORY
Albuterol Cromolyn Diphenhydramine Fluticasone Ipratropium Loratadine
Montelukast Omalizumab Salmeterol Theophylline Zileuton
ALBUTEROLMuscle tremor Nervousness Restlessness Tachycardia HTN crisis w/ MAOI
Bonchodilator 2 receptor agonist
Activates 2 receptors in bronchial smooth m.
cAMP activating kinases Inhibiting myosin phosphorylase m. relaxation
Asthma
Acute bronchospasm Prevent exercise-induced asthma
Chronic bronchitis & emphysema
Reversible airway obstruction
CROMOLYNNasal & throat irritation
Antiasthmatic & antiallergy Mast cell stabilizer
Prevents Ca influx & stabilizes mast cell & eosinophil membranes
Prevents degranulation & release of histamine, leukotrienes
Asthma prophylaxis Exercise-induced bronchospasm Allergic disorders
Oral or nasal inhalation
DIPHENHYDRAMINEDrowsiness Blurred vision Dry mouth Urinary retention Anorexia
Antihistamine, sedative, antiemetic H1 receptor antagonist
Blocks H1 & muscarinic receptors
Prevents histamineinduced allergic rxns Prevents vestibular stim. of vomiting center Sedation
Allergic rxns Prevent motion sickness Insomnia
FLUTICASONENasal & throat irritation Oral candidiasis
Anti-inflammatory Corticosteroid
Inhibits cytokine production by Thelper cells Prevents mediator release from mast cells, basophils, eosinophils Stabilizes lysosomal membranes Vasoconstriction & capillary permeability
Allergic rhinitis Chronic nasal inflammation Chronic asthma
IPRATROPIUMCough Nasal dryness & irritation
Bronchodilator Muscarinic receptor antagonist
Blocks muscarinic receptors in bronchial smooth m. & nasal mucosa Prevents vagalstimulated bronchoconstriction
COPD Rhinitis Asthma
Inhalation admin
LORATADINE
Antihistamine H1 receptor antagonist
Blocks H1 receptors in nasal mucosa Prevents allergic rxns
Seasonal rhinitis Chronic idiopathic urticaria
Less sedating than diphenhydramine
MONTELUKAST
Antiasthmatic Leukotriene antagonist
Blocks cysteinyl leukotriene-1 receptor for leukotrienes C4, D4, E4 Prevent airway inflammation, edema, bronchoconstriction, & secretion viscous mucus Inhibits early/late phase bronchoconstriction
Long-term asthma control
Oral admin
OMALIZUMABAllergic rxnsanaphylaxis
Antiasthmatic IgE antagonist
Blocks IgE
Severe asthma in combo w/ corticosteroid therapy
SubQ every 2-4 wks
SALMETEROLTachycardia Nervousness HA
Bronchodilator 2 agonist
cAMP Relaxes bronchial smooth m. Inhibits late phase allergen-induced bronchoconstriction
Asthma
Prevent nocturnal attacks Exercise-induced asthma
NOT acute bronchospasm
Inhalation admin
THEOPHYLLINEN, V Anxiety Insomnia Tachycardia
Bronchodilator Methylxanthine
Inhibits phosphodiesterase isoenzymes & cAMP Relaxes bronchial smooth m. Inhibits T-lymphocyte proliferation & cytokine production
Chronic asthma Obstructive pulmonary ds Neonatal apnea respiratory stim.
Half-life
Shorter in smokers & children Longer in elderly Monitor blood levels
ZILEUTONFlu-like syn HA Drowsiness Dyspepsia serum aminotransferase levels & hepatitis Inhibits CYP450 & 3A4 theophylline & warfarin levels
Antiasthmatic Leukotriene synthesis inhibitor
Inhibits 5lipoxygenase & leukotriene synthesis
Prevents airway inflammation & bronchoconstriction
Long-term asthma control