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