Pharmacology

Analgesic & Antimigraine

Butorphanol Dihydroergotamine Fentanyl Meperidine Methadone Morphine

Naloxone Propoxyphene Sumatriptan Tramadol

Butorphanol
Opioid analgesic Mixed opioid agonist-antagonist 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 Dysphoria Nightmares w/drawal in pts dependent on full opioid agonists AVOID MAOI
Potentially fatal

Dihydroergotamine
Antimigraine Ergot alkaloid 5-HT 1B/1D receptor agonist Activates 5-HT 1B/1D receptors
Pial & dural vessel constriction N, V Stiff neck, shoulder, extremities Leg weakness Numbness & tingling in fingers & toes

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 Chronic pain Breakthrough for cancer pain Transdermal patch Sedation Confusion Respiratory depression Anorexia N, V Constipation AVOID MAOI in past 14d

Meperidine
Opioid analgesic Strong opioid agonist Activates opioid receptors
Inhibits pain transmission Generalized CNS depression Moderate-severe pain Analgesia during labor Preoperative sedation Lacks antitussive activity Confusion Sedation Constipation N, V Dependence Toxic metabolite CNS excitation, convulsions, tremors AVOID MAOI
Potentially fatal

Methadone
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 Respiratory depression Constipation Confusion Sedation AVOID MAOI

Morphine
Opioid analgesic Strong opioid receptor agonist Activates receptors
cAMP
Opens K & closes Ca channels release substance P

Sedation Confusion Hypotension Constipation Respiratory depression AVOID MAOI w/ 14 d

Potentially fata

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

Propoxyphene
Opioid analgesic Weak opioid agonist Activates opioid receptors
Inhibits pain transmission Mid-moderate pain Combined w/ acetaminophen or aspirin Dizziness Weakness N dependence

Sumatriptan
Antimigraine 5-HT 1B/1D receptor agonist Activates 5-HT 1B/1D receptors
Pial & dural vessel constriction Dizziness Vertigo Tingling Warm sensation Tight feeling head & chest Coronary vasospasm AVOID
MAOI SSRI

Presynaptic inhibition of trigeminal peptide neurotransmitter release Inhibitions brainstem activation of trigeminal neurons
Vascular HA
Migraine & cluster

Oral, nasal, & subQ

Tramadol
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 Dizziness HA Constipation Lowers seizure threshold AVOID MAOI risk seizures w/ high doses
Penicillins Phenothiazines

Anesthetics

Benzocaine Bupivacaine Halothane Ketamine Lidocaine

Midazolam Nitrous oxide Propofol Sevoflurane

Benzocaine
Local anesthetic Ester-type Blocks Na channels & nerve conduction
Topical anesthetic
Pain Itching Inflammation

Cross-sensitivity w/ other estertype anesthetics

Burns Insect bites Contact dermatitis Wounds Irritates skin when 1st applied Use caution w/ sunburn & large areas of skin

Bupivacaine
Local anesthetic Amide-type Blocks Na channels & nerve conduction
Local or regional anesthetic
Surgical Diagnostic Obstetrical therapeutic

Cross-sensitivity w/ amide-type anesthetics

Halothane
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 Sensitizes heart to catecholamine-induced cardiac arrhythmia Hepatotoxic
Fluoride metabolites

Ketamine
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

Delirium Hallucination Irrational behavior during recovery BP

Lidocaine
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

Cross-reactivity w/ amide-type anesthetics

Midazolam
Sedative-hypnotic-anxiolytic Short-acting BZDP Potentiates GABA binding to GABA-A Cl ion channel
Sedation Hypnosis Amnesia Preoperative sedation & anxiolysis Sedation of mechanically vented pts

Apnea Laryngospasm Respiratory depression Cardiac arrest

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

Propofol
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 Bradycardia Hypotension

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

Acyclovir
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

Dizziness Diarrhea N Nephrotoxicity Probenecid serum levels

viral shedding, pain, & healing time

Albendazole
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

GI distress Constipation or diarrhea Hepatitis & hematologic toxicity w/ high doses

Trichinosis
Use w/ corticosteroid

Cysticercosis & echinococcus Microsporidiosis

Amantadine
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 Ataxia Dizziness Insomnia Skin mottling & livedo reticularis Blurred vision Dry mouth

Amoxicillin-clavulanate
-lactam ABX Extended spectrum aminopenicillin & -lactamase inhibitor Amoxicillin
Binds PBP
Inhibits cross-linking of cell wall peptidoglycan

Diarrhea Superinfection Pseudomembranous colitis Allergic rxn

Rash Serum sickness anaphylaxis

Clavulanate
Inhibits class-A -lactamase
Protects amoxicillin from destruction

Probenecid inhibits renal tubular excretion

serum levels

NOT antimicrobial by itself Respiratory tract infections

Otitis, sinusitis, pneumonia

Skin or skin structure infections

Bite wounds

Amphotericin B
Antifungal Polyene ABX Binds ergosterol & membrane permeability
Leakage of cell contents Candidiasis Cryptococcal meningitis Aspergillosis Blastomycosis Coccidioidomycosis Histoplasmosis Mucormycosis Chills Fever Diarrhea N, V Nephrotoxicity Hypokalemia toxicity w/ cyclosporine, antineoplastics Thiazides, & corticosteroids hypokalemia

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

Aztreonam
-lactam ABX Monobactam Binds PBP including transpeptidase Inhibits cross-linking of cell wall peptidoglycan
Drug resistant gram (-) infections including Pseudomonas aeruginosa & Enterobacteriaceae Thrombophlebitis Allergic rxn

Caspofungin
Antifungal Echinocandin Inhibits synthesis of cell wall component
-1,3-D-glucan Candida albicans Invasive aspergillosis IV admin
Not absorbed well by gut

HA Fever Phlebitis Abnormal LFTs

Cefazolin
-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

Rash Diarrhea Pseudomembranous colitis Superinfection Probenecid inhibits excretion & serum levels

NOT active against MRSA

Cefepime
-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

Rash Diarrhea Pseudomembranous colitis Superinfection Probenecid inhibits excretion & serum levels

Ceftazidime
-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 Rash Diarrhea Pseudomembranous colitis Superinfection Probenecid inhibits excretion & serum levels

Cetriaxone
-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

Rash Diarrhea Pseudomembranous colitis Superinfection Probenecid inhibits excretion & serum levels

Single IM injection Tx acute otitis media or gonorrhea

Ciprofloxacin
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 Insomnia Diarrhea N Absorption by cations
Antacids Iron Zinc bismuth

Clindamycin
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 C. difficile superinfection Diarrhea Pseudomembranous colitis

Doxycycline
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 AVOID
Pregnancy & children > 8 y/o Outdated preparations are nephrotoxic

Permanent teeth discoloration Photosensitivity Diarrhea N, V

Efavirenz
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 N Rash Drowsiness Depression

Enfuvirtide
Antiretroviral HIV fusion inhibitor Binds HIV virus gp41 & blocks fusion of HIV w/ host cells CD4 Thelper lymphocytes
Drug-resistant HIV Injection site rxn
Rotate sites daily

Erythromycin
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

Activates motilin receptors causing uncoordinated peristalsis

Anorexia N, V

Ethambutol
Antitubercular Synthetic butanol derivative Bacteriostatic against mycobacteria Inhibits RNA synthesis
M. tuberculosis MAI Dose-related retrobulbar optic neuritis Impaired red-green color discrimination
Monitor pts color discrimination regularly

Gouty arthritis

Foscarnet
Antiviral Pyrophosphate Blocks pyrophosphatebinding site on viral DNA polymerase
Prevents attachment of nucleotide precursors to DNA CMV retinitis in HIV pts Acyclovir-resistant HSV in immunocompromised HA Diarrhea V Renal failure Hypocalcemia Hypokalemia Hypomagnesemia Anemia Arthralgia Myalgia Pentamidine causes lifethreatening hypocalcemia

Fosfomycin
ABX Cell wall synthesis inhibitor Inhibits enopyruvyl transferase & addition of phosphenolpyruvate to Nacetylglucosamine to form N-acetylmuramic acid
Cystitis d/t E. coli or Enterococcus faecalis Single dose Tx for UTI

Ganciclovir
Antiviral Nucleoside analogue Converted to ganciclovir triphosphate
Inhibits viral DNA polymerase CMV infection in immunocompromise d & transplants visual acuity Neutropenia Thrombocytopenia Anemia

Gentamicin
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 Nephrotoxicity Ototoxicity
Vestibular & cochlear w/ loop diuretics

Griseofulvin
Antifungal Fungistatic ABX Deposits in keratin precursor cells of skin, hair, & nails Disrupts microtubules & mitotis of dermatophytes
Dermatophyte infections NOT Candida HA Induces CYP450
Reduces plasma levels warfarin & OCP

Imipenem-cilastatin
-lactam ABX Carbapenem ABX & dehydropeptidase inhibitor Imipenem
Binds PBP & inhibits crosslinking cell wall peptidoglycan Allergic rxns Diarrhea V Seizures
risk w/ ganciclovir or cyclosporine

Cilastatin
Inhibits renal dehydropeptidase & degradation of imipenem Endocarditis, pneumonia, UTI, pelvic, abdominal d/t aerobic & anaerobic

Probenecid inhibits secretion & serum levels

Isoniazid
Antitubercular Nicotinic acid derivative Reduces catalaseperoxidase
Inhibits synthesis of mycolic acid component of cell wall TB Bimodal distribution d/t fast & slow acetylation Inactivates vit. B6 Hepatitis
Toxic metabolite acetylhydrazine

Peripheral neuropathy
Vit. B6 deficiency

Itraconazole
Antifunal Synthetic triazole Inhibits 14--demethylase
CYP450 enzyme that converts lanosterol ergosterol Blastomycosis, candidiasis, coccidioidomycosis, histoplasmosis Onychomycosis nail beds GI distress Rash Hepatitis

Ivermectin
Antiparasitic Antihelmintic ABX Activates glutamate-gated Cl ion channel
Pharyngeal m. hyperpolarization & paralysis Strongyloidiasis Cutaneous larva migrans Onchocerciasis filiariasis
W. bancrofti

Vertigo Sedation

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

Linezolid
Antibacterial Oxazolidinone protein synthesis inhibitor Binds 23s ribosomal RNA of 50S subunit
Prevents formation of 70s initiation complex VRE, MS/MRSA, PCNsensitive pneumococci Inhibits MAO

Mefloquine
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 Neuropsychiatric syn
Hallucination Anxiety Confusion Seizure Coma

Metronidazole
Antiprotozoal Nitroimidazole Reduced by pyruvate:ferredoxin to form nitro-free radicals that attack DNA & proteins
Amebiasis, giardiasis, trichomoniasis Balantidium coli, C. difficile, B. fragilis GI pain Anorexia N Dizziness Alcohol causes disulfiram-like effect

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

Nafcillin
-lactam ABX Antistaphylococcal, penicillinase-resistant penicillin Binds PBP
Inhibits cross-linking of cell wall peptidoglycan Methicillin-sensitive penicillinase producing staph
Bone, jt, UTI, respiratory, skin, endocarditis, meningitis

Diarrhea Superinfection Pseudomembranous colitis Allergic rxn

Rash Serum sickness Anaphylaxis

Probenecid inhibits renal tubular secretion & serum levels

Nitrofurantoin
Urinary tract antibacterial Nitrofuran Inhibits bacterial enzymes
UTI
E. coli, S. saprophyticus

Anorexia N, V Neurotoxicity Pneumonitis Probenecid inhibits urinary excretion

Oseltamivir
Antiviral Neuraminidase inhibitor Inhibits influenza A & B neuraminidase
Prevents release & spreading of viral particles Influenza A & B

Paromomycin
Antiprotozoal Aminoglycoside ABX Inhibits protein synthesis
Intestinal amebiasis Cryptosporidiosis in immunocompromised pts Nephrotoxic & ototoxic if given IV

Penicillin G
-lactam ABX Narrow-spectrum penicillin Binds PBP
Inhibits cross-linking of cell wall peptidoglycan Strep, pneumococcal, meningococcal Syphilis Diarrhea Superinfection Pseudomembranous colitis Allergic rxn
Rash Serum sickness Anaphylaxis

Probenecid inhibits renal tubular secretion

Pentamidine
Antiprotozoal Amidino-pentane derivative Disrupts nucleic acid synthesis in protozoa
P. carinii Early stage African trypanosimiasis sleeping sickness Nephrotoxic Hematologic toxicity Hypoglycemia Allergic rxn
Anaphylaxis

Erythromycin fatal arrhythmias

Piperacillin-tazobactam
-lactam ABX Antipseudomonal penicillin & lactamase inhibitor Piperacillin
Binds PBP
Inhibits cross-linking of cell wall peptidoglycan

Diarrhea Superinfection Pseudomembranous colitis Allergic rxn

Rash Serum sickness Anaphylaxis

Tazobactam
Inhibits class A -lactamases Gram (-) bacilli, P. aeruginosa

Probenecid inhibits renal tubular secretion

Praziquantel
Antihelmintic Isoquinoline derivative Ca permeability of schistosome tegument
Contraction & exposing antigens to host immunity Schistosomiasis Chinese liver fluke Lung fluke Cestodes tapeworms Malaise Anorexia Drowsiness dizziness

Primaquine
Antimalarial 8-aminoquinoline Converted to oxidizing quinoline-quinone intermediates
Eradicate exo-erythrocytic forms of P. vivax & P. ovale Hemolytic anemia in G6PD deficiency methemoglobinemia

Pyrimethamine
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 N Anorexia Hypersensitivity rxn

Pyrantel
Antihelmintic Pyrimidine analogue Activates cholinergic nicotinic receptors in somatic m. of nematodes Produces depolarizing NM blockade
Ascariasis Hookworm & pinworm Abdominal cramps Anorexia Diarrhea V

Quinine
Antimalarial 4-aminoquinoline Binds plasmodial DNA & prevents replication & transcription during erythrocytic schizogony
Chloroquine-resistant malaria Admin w/ doxycycline or pyrimethamine-sulfadoxine Abdominal cramps Diarrhea V Cinchonism
Tinnitus Blurred vision

Metabolism
Cimetidine inhibits Rifampin induce

Quinupristin-dalfopristin
Streptogramin ABX Protein synthesis inhibitor Binds 50s ribosomal subunit Quinupristin
Inhibits aminoacyl tRNA synthesis & addition of AA Infusion site rxn

Dalfopristin
Inhibits peptidyl transferase VRE, MS/MRSA

Ribavirin
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 Anemia Hypotension Cardiac arrest

Rifampin
Antitubercular Rifampin derivative Inhibits DNA-dependent RNA polymerase
TB Leprosy Prophylaxis meningococcal meningitis & H. flu B infections Red discoloration of tears, urine, saliva, sweat Abdominal pain V Diarrhea Hepatitis Induces CYP450 levels
Warfarin Theophylline Itraconazole Steroids Opioids Phenytoin Verapamil

Ritonavir-lopinavir
Antiretroviral HIV protease inhibitor Inhibits HIV protease & conversion of gag-pol polyprotein to functional proteins Ritonavir
lopinavir levels HIV in combo w/ nucleoside reverse transcriptase inhibitor Anorexia V Altered taste Abnormal thinking Hyperlipidemia Hyperlgycemia

Streptomycin
Aminoglycoside Protein synthesis inhibitor Binds 30s ribosome Prevents initiation of protein synthesis
Misreading of genetic code Drug-resistant TB Plague Tularemia IV admin Nephrotoxic Ototoxic
w/ loop diuretics

Terbinafine
Antifungal Allylamine Inhibits squalene oxygenase & formation of squalene epoxide during fungal membrane ergosterol synthesis
Topical
Tinea corporis, cruris, pedis, versicolor

Itching Rash Diarrhea Anorexia Metabolism

Cimetidine inhibits Rifampin induce

Oral
Onychomycosis fungal nail infection

Trifluridine
Antiviral Thymidine analogue Inhibits HSV DNA polymerase
Herpetic keratitis Keratoconjunctivitis Topical ocular admin Ocular irritation
Redness Itching

Trimethoprim-sulfamethoxazole
Antibacterial Folate antagonist Sulfamethoxazole
Inhibits folate synthesis N, V Rash Stevens-Johnson syn Allergic rxn Anemia
Hemolytic anemia Megalobalstic anemia

Trimethoprim
Inhibits folate reduction UTI, travelers diarrhea Shigella enteritis P. carinii & Nocardia pneumonia

Leukopenia Thrombocytopenia Crystalluria Added folate deficiency w/ phenytoin or MTX

Vancomycin
Glycopeptide ABX Cell wall synthesis inhibitor Binds D-alanyl-D-alanine portion of peptidoglycan Prevents cross-linking of D-alanine & pentaglycine chain
MRSA, penicillin-resistant enterococci, C. difficile Red man syn
Extensive rate of infusion Erythematous rash on face & upper body

Ototoxicity
Vestibular & cochlear

Zidovudine
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

Anemia

Antineoplastic

Anastrozole Bleomycin Busulfan Carmustine Cisplatin Cyclophosphamide Doxorubicin Etoposide Fluorouracil Gemtuzumab ozogamicin

Imatinib Leuprolide Meraptopurine Methotrexate Paclitaxel Tamoxifen Trastuzumab Vincristine

Anastrozole
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

N HA Hot flashes Back pain

Bleomycin
Antitumor DNA intercalating Complexes ironforming oxygen free radicals that cause single strand breaks G2 phase specific
Lymphomas SCC Testicular carcinoma Choriocarcinoma
Pneumonitis & pulmonary fibrosis Hyperpigmentation Mucocutaneous toxicity Hematology toxicity

Busulfan
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

N, V Myelosuppression Pulmonary fibrosis

Carmustine
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

N, V Hepatotoxicity Anemia Leucopenia Thrombocytopenia Pulmonary fibrosis

Cisplatin
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

Severe N, V Ototoxicity & tinnitus Hypocalcemia Hypokalemia Hypomagnesemia Anemia

Cyclophosphamide
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 Anorexia N, V Hemorrhagic cystitis & hematuria Alopecia Thrombocytopenia Leukopenia Anemia Rifampin induces CYP & toxicity

Doxorubicin
Antitumor DNA intercalating agent Inserts b/w DNA bases
Causes deformation & uncoupling

Colors urine red Cardiomyopathy doselimiting Anemia Leukopenia Thrombocytopenia Diarrhea V Stomatitis Alopecia

Complexes iron forming hydroxyl free radicals that cause strand breaks Inhibits topoisomerase II
Causes strand breaks

S phase specific
Breast, ovarian, bladder tumors Bronchogenic carcinoma Lymphoma & leukemia

Etoposide
Antineoplastic Podophyllotoxin, topoisomerase inhibitor Inhibits mammalian topoisomerase II & prevents resealing of nicked DNA strands G2 phase specific
Testicular, small cell lung carcinoma Lymphoma Leukemia

N, V Leukopenia Thrombocytopenia Alopecia

Fluorouracil
Antineoplastic Pyrimidine antimetabolite Converted to active nucleotide form
Inhibits thymidylate synthetase

S phase specific
Colon, breast, rectal, gastric, pancreatic cancer Topical for basal cell carcinoma & actinic keratosis

Diarrhea V Stomatitis Alopecia Maculopapular rash Anemia Leukopenia Thrombocytopenia

Gemtuzumab ozogamicin
Antineoplastic Monoclonal Ab & cytotoxic ABX calicheamicin Gemtuzumab
Binds CD33 Ag on hematopoietic cells & sequesters lysosomes where calicheamicin is released

Severe myelosuppression & hypersensitivity rxn

anaphylaxis

Calicheamicin
Causes DNA dbl strand breaks CD33 (+) AML

Severe pulmonary rxns Chills Fever N Dyspnea

Imatinib
Antineoplastic Tyrosine kinase inhibitor Inhibits oncoprotein bcr-abl 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

Leuprolide
Antineoplastic, agent for precocious puberty GnRH analogue 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 Transient in testosterone w/ 1st dose
Use flutamide or other androgen antagonist

Hot flashes

Mercaptopurine
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 Cross-react w/ thioguanine Myelosuppression Hyperuricemia Hepatotoxicity Allopurinol inhibits degradation

Methotrexate
Antineoplastic Folate reductase inhibitor Inhibits dihydrofolate reductase Prevents formation of active folate & addition of single carbon units to DNA base precursors S phase specific
Choriocarcinoma, trophoblastic tumors Leukemia Breast, head, neck, lung cancers Severe psoriasis RA Mycosis fungoides Leucovorin used to minimized hematologic toxicity & Tx OD

N, V Stomatitis Hepatotoxicity Anemia Leukopenia Thrombocytopenia Nephropathy

Paclitaxel
Antineoplastic Mitotic inhibitor Binds tubulin & prevents depolymerization of microtubules of mitotic spindle M phase specific
Advanced ovarian cancer w/ cisplatin Non-small-cell lung cancer Metastatic ovarian or breast cancer

D N, V Alopecia Anemia Leukopenia Thrombocytopenia Peripheral neuropathy Arthralgia Myalgia

Tamoxifen
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

CI during pregnancy & lactation N Hot flashes Menstrual irregularities

Trastuzumab
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

Abdominal pain Anorexia Diarrhea V Back pain Chills Fever Allergic rxns Doxorubicin risk of cardiotoxicity

Vincristine
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

N, V Alopecia Peripheral neuropathy

Autonomic & Neuromuscular

Atenolol Atropine Dobutamine Edrophonium Epinephrine Phenoxybenzamine Phentolamine Phenylephrine Pilocarpine

Pralidoxime Propranolol Pseudoephrine Pyridostigmine Rocuronium Sildenafil Succinylcholine Tamsulosin Terazosin

Atenolol
Sympatholytic, antihypertensive 1 receptor antagonist 1 receptor antagonist
Angina Post MI Hypertension

Bronchoconstriction w/ high doses b/c 1 blockade Additive hypotension w/ nitrates

Atropine
Anticholinergic Muscarinic receptor antagonist Muscarinic receptor blocker
Bradycardia IBS Anticholinesterase poisoning Antisecretory agent
Mydriasis & cycloplegia Warm, dry, flushed skin Tachycardia Delirium Hallucinations

Dobutamine
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 Tachycardia Arrhythmia

Edrophonium
Diagnostic agent Cholinesterase inhibitor Reversible cholinesterase inhibitor
Dx myasthenia gravis Muscarinic effects
Miosis Salivation

Epinephrine
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

HTN Tachycardia Ischemia Hyperglycemia

Phenoxybenzamine
Vasodilator Irreversible receptor antagonist receptor antagonist
1 > 2
Presurgical Tx of HTN d/t pheochromocytoma

Postural hypotension Hypotension w/ blockers & Ca channel blockers

Phentolamine
Vasodilator receptor antagonist Blocks 1 & 2 receptors
Control BP during surgical removal of pheochromocytoma IV admin only Hypotension Severe hypotension w/ Epi

Phenylephrine
Vasocontrictor, decongestant Selective 1 receptor
Rebound nasal congestion HTN MAOI cause severe HTN

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 accommodation

Pilocarpine
Antiglaucoma, sialogogue Muscarinic receptor agonist Activates muscarinic receptors in ciliary m. & salivary gland
Sjogrens syn
Glaucoma
Ciliary m. aqueous humor

Miosis Blurred vision

Accommodative spasm

Xerostomia
Salivary gland salivation

Pralidoxime
Organophosphate antidote Cholinesterase reactivator Binds phosphorous & breaks organophosphate bond w/ cholinesterase
Organophosphate toxicity Reverses muscle weakness

Propranolol
Sympatholytic, antihypertensive Nonselective receptor antagonist Blocks 1 & 2 receptors
Angina HTN Benign tremor Migraine prophylaxis thyrotoxicosis Post-MI Highly lipophilic effects CNS Bronchoconstriction Inhibits glycogenolysis Nightmares & depression

Pseudoephedrine
Decongestant Indirect/direct-acting adrenergic receptor agonist release NE directly activates adrenergic receptors causing vasoconstriction & cardiac stim.
Allergic & viral rhinitis Tachycardia CNS stim. BP MAOI cause severe HTN

Pyridostigmine
Antimyasthenic Cholinesterase inhibitor, cholinergic agonist Reversibly inhibits cholinesterase
Tx myasthenia gravis Reverse nondepolarizing NM blockers Muscarinic effects
Miosis Salivation

Prolongs effects of succinylcholine

Rocuronium
Paralytic agent Nondepolarizing NM blockade Blocks nicotinic receptors in skeletal m.
Skeletal m. relaxation for intubation, surgery, ECT Effects reversed by neostigmine & edrophonium

Respiratory m. paralysis Apnea

Sildenafil
Vasodilator Phosphodiesterase inhibitor Inhibits type 5 phosphodiesterase & degradation of cGMP
vasodilation in corpus cavernosum d/t Ach release from sacral PNS neurons Erectile dysfunction HA Nasal congestion Back pain Visual disturbances

Succinylcholine
Paralytic agent Depolarizing NM blockade Binds nicotinic receptors causing prolonged depolarization of skeletal m. & paralysis
Skeletal m. relaxation for intubation & surgery Transient m. fasciculations

Respiratory m. paralysis Apnea

Tamsulosin
Urologic agent Uroselective 1 receptor antagonist Blocks 1A receptors in prostate
Tx urinary outflow obstruction d/t prostatic hyperplasia Dizziness HA Postural hypotension Cimetidine increases blood levels & effects

Terazosin
Antihypertensive, urologic agent Selective 1 receptor antagonist Blocks 1 receptors
HTN Outflow obstruction d/t prostate hyperplasia 1st dose syncope

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

Acetazolamide
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

Parasthesia Urinary stone formation

Adenosine
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
Transient asystole

Amiloride
K-sparring diuretic Epithelial Na channel blocker Blocks Na Channel distal tubule & collecting duct
Inhibits Na reabsorption & K excretion Prevent & Tx hypokalemia Hyperkalemia

Amidarone
Antiarrhythmic Cardiac ion channel blocker Blocks K, Na, Ca channels & receptors
Prolongs repolarization refractory period Slows HR PR & QT intervals SVT, VT, VF Hypo/hyperthyroidism Photosensitivity Blue-gray skin Corneal microdeposits Pulmonary fibrosis

Amlodipine
Antihypertensive, antianginal Dihydropyridine Ca channel blocker Ca channel blocker in vascular smooth m. Arteriolar vasodilation & coronary blood flow
HTN Angina pectoris HA Edema Hypotension Effects w/ grapefruit juice

Carvedilol
Antihypertensive & heart failure Tx Nonselective adrenergic receptor agonist Blocks 1, 2, 1 receptors Cause vasodilation
HTN Heart failure
remodeling

Orthostatic hypotension Dizziness Bradycardia

Clonidine
Antihypertensive 2 receptor agonist Central 2 receptor agonist
sympathetic outflow from vasomotor center Inhibits pain neurotransmission in spinal cord HTN Opioid w/drawal

Abrupt w/drawal severe rebound HTN Sedation Dry mouth

Digoxin
Cardiac stimulant Digitalis glycoside Inhibits Na/K ATPase
IC Ca & cardiac contractility AV conduction AV refractory period Heart failure Serum levels assess dosage & toxicity Arrhythmias N, V Blurred vision Yellow vision

Diltiazem
Vasodilator, antiarrhythmic Non-dihydropyridine Ca channel blocker Block Ca channels in cardiac tissue & vascular smooth m.
Vasodilation HR & conduction contractility HTN Angina pectoris SVT

Dizziness Hypotension Peripheral edema Constipation Gingival hyperplasia Grapefruit juice serum levels

Dofetilide
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

QT prolongation Torsade de pointes

Enalapril
Antihypertensive ACE inhibitor Inhibits ACE & formation of AT II
Vasodilation aldosterone secretion CO V remodeling survival in heart failure HTN Heart failure Post-MI progression of diabetic nephropathy

Cough & angioedema

Inhibits bradykinin degradation

Hypotension Taste disturbances

Esmolol
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

Hypotension Bradycardia

Fenoldopam
Antihypertensive D1-like receptor agonist D1 receptor agonist
Arteriolar vasodilation
Afferent & efferent renal arterioles

serum K levels
Monitor for hypokalemia

renal blood flow Hypertensive emergencies

Furosemide
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

Hypokalemia Metabolic alkalosis Hyperuricemia Hypomagnesemia ototoxicity of aminoglycoside ABX

Hydralazine
Antihypertensive. heart failure Vasodilator Alters IC Ca metabolism
Relaxes arteriolar smooth m.
vasodilation

Edema Reflex tachycardia & MI Lupus syndrome

afterload Heart failure in combo w/ isosorbide dinitrate

More effective than ACEI in black people

Moderate-severe HTN

Hydrochlorothiazide
Antihypertensive Thiazide diuretic Inhibits NaCl transporter in distal tubule
excretion Na, K, Cl Ca excretion HTN Nephrogenic DI Nephrolithiasis Hypokalemia Metabolic alkalosis Hyperuricemia & gout excretion of lithium

Labetolol
Antihypertensive Adrenergic & receptor antagonist Selective 1 & nonselective 1, 2 blockers
HTN Postural hypotension Abrupt w/drawal cause life-threatening HTN, arrhythmias, or MI

Mannitol
Diuretic Osmotic Diuretic Osmotic attraction of edematous & ocular fluid
Filtered by glomerulus

Electrolyte imbalances Transient volume expansion

Pulmonary edema or heart failure

electrolyte excretion Oliguric renal failure Cerebral edema ICP Acute glaucoma

Methyldopa
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 Positive direct Coombs test

Minoxidil
Antihypertensive, hair growth stimulant Vasodilator, K channel opener Opens K channels in vascular smooth m.
Hyperpolarization m. relaxation vasodilation

Systemic admin.
Reflex tachycardia Angina pericarditis Pulmonary HTN hypertrichosis

Stim. resting hair follicle growth follicles

Severe HTN Topical for alopecia

Nesiritide
Heart failure Tx Recombinant human B-type natriuretic peptide Activate guanylate cyclase cGaMP
Dilates venous & arterial smooth m. venous pressure, cardiac preload, vascular congestion, & dyspnea Decompensated heart failure

Hypotension

Nitroglycerin
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

HA Hypotension Syncope Reflex tachycardia vasodilative effect of sildenafil, tadalafil, vardenafil

Nitroprusside
Antihypertensive Vasodilator Relaxes venous & arteriolar smooth m.
Metabolized to CN & thiocyanate
Tx toxicity w/ sodium nitrite & sodium thiosulfate

CN toxicity Hypotension HA

HTN crisis Acute heart failure or cardiogenic shock Controlled hypotension during pregnancy

Propafenone
Antiarrhythmic Class IC Na channel blocker Blocks Na channel in cardiac tissue conduction & prevent re-entry PR, QRS, & QT duration
SVT & life-threatening V arrhythmias
Proarrhythmic 1st 2 wks
Monitor ECG when starting Tx

GI disturbances digoxin levels

Quinidine
Antiarrhythmic Class IA Na channel blocker Blocks Na & K channels in cardiac tissue conduction QRS & QT duration
SVT & VT D-isomer = quinine, used to treat malaria pts
Cinchonism
Blurred vision Tinnitus Photophobia

levels w/
Amiodarone Cimetidine Diltiazem Verapamil Grapefruit juice

Sotalol
Antiarrhythmic Class III K channel blocker Blocks K channels in cardiac tissue
Prolongs repol. refractory period & QT interval

Torsades de pointes

Blocks adrenergic receptors

SVT & life-threatening arrhythmias

Spironolactone
K-sparring diuretic Aldosterone antagonist Blocks aldosterone receptors Na excretion K excretion
Primary hyperaldosteronism HTN hypokalemia Gynecomastia Impotence Hyperkalemia

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

Verapamil
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

Peripheral edema Constipation Gingival hyperplasia

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 5-HT1A receptors in dorsal raphe nucleus
firing serotonergic neurons Generalized anxiety disorder NO
Drug dependence Significant sedation Muscle relaxation Anticonvulsant effects

Dizziness Drowsiness Fatigue HA Excitement Nervousness Blurred vision Tachycardia N Rash Myalgia Sweating levels by
Erythromycin Itraconazole Grapefruit juice

Carbamazepine
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 Ataxia Drowsiness Blurred vision Agranulocytosis Aplastic anemia Thrombocytopenia Induces its own metabolism

Diazepam
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 Drowsiness Lethargy Physical/psychological dependence Tolerance

Disulfiram
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 Drowsiness

Ethosuximide
Anticonvulsant Succimide Binds T-type Ca channels in thalamic neurons Suppresses nerve transmissions to motor cortex
Generalized absence seizures
Petit mal epilepsy

Dizziness Drowsiness Gastric distress N

Flumazenil
Antidote Benzodiazepine receptor antagonist Blocks benzodiazepine receptors
Counteract adverse effects of benzodiazepines
Respiratory depression d/t IV OD

Seizures Dizziness Emotional lability

CI in status epilepticus

Gabapentin
Anticonvulsant GABA analogue GABA release from central neurons
Inhibits neuronal discharges from seizure foci Inhibits pain neurotransmission Partial seizures Chronic pain Migraine prophylaxis Ataxia Dizziness Drowsiness Nystagmus Tremor

Lamotrigine
Anticonvulsant Phenyltriazine Blocks voltagesensitive Na channels
Release of glutamate Prevents spread of seizure foci discharges Adjunct/monotherapy for partial seizures in adults Skin rash in 1st 8 wk of Tx
Can progress to Stevens-Johnson syn

Ataxia Dizziness Drowsiness Photosensitivity metabolism & ADR w/ valproate

Lorazepam
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
Dizziness Drowsiness Apnea & cardiac arrest w/ rapid IV admin Additive depression w/ alcohol & other depressants

Phenobarbital
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
Drowsiness Lethargy Delirium Hangover Physical & psychological dependence Induces CYP P450 metabolism of drugs

Phenytoin
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 Ataxia Diplopia Nystagmus Gingival hyperplasia

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

Valproate
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 Indigestion N, V Dizziness Sedation Hepatotoxicity

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

Acarbose
Antidiabetic -glucosidase inhibitor Inhibits intestinal enzyme that converts oligosaccharides & disaccharides to glucose digestion of starch & sucrose postprandial blood glucose & HbA1c
Type II DM

Intestinal bloating Flatulence oral bioavailability of metformin iron absorption

Alendronate
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

Absorption by Ca supplements, antacids, foods, beverages (except water)

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

Danazol
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

CI in pregnancy androgenic effects on female fetus Emotional lability Deepening voice Acne Hirsutism Amenorrhea breast size

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

Ergocalciferol
Vit. D Fat-soluble Activated in liver & kidneys to form calcitriol
Ca & phosphorus absorption from gut Vit. D deficiency
Rickets, osteomalacia

Hypercalcemia Hypercalciuria Cholestyramine inhibits vit. D absorption Induce vit. D metabolism

Phenytoin Barbiturates

Chronic renal failure Familial hypophosphatemia Hypocalcemia d/t hypoparathyroidism Postoperative & idiopathic tetany

Ethinyl estradiol & drospirenone

OCP Estrogen & progesterone Feedback inhibit GnRH
Estrogen
FSH secretion & maturation of dominant follicle

Drospirenone Antiandrogenic Blocks aldosterone

salt & water retention BP

Thromboembolism
risk w/ smoking

Progesterone
Inhibits midcycle LH surge & ovulation

Edema Efficacy w/
ABX Carbamazepine phenytoin

Contraception Regulate menstrual cycle Acne in women

Ethinyl estradiol & norethindrone

OCP Estrogen & progesterone Feedback inhibit GnRH
Estrogen
FSH secretion & maturation of dominant follicle

Norethidrone
Slightly androgenic Thromboembolism Edema Depression Gallbladder ds

Progesterone
Inhibits midcycle LH surge & ovulation

Contraception Regulate menstrual cycle Acne in women

Finasteride
Androgen synthesis inhibitor 5--reductase inhibitor Inhibits conversion testosterone dihydrotestosterone & androgenic stimulation of prostate & skin prostate size & promotes hair growth
BPH Male pattern baldness

CI pregnancy
Risk to male fetus Do NOT handle tablets

Impotence

Fludrocortisone
Corticosteroid Mineralocorticoid Activates aldosterone receptors in renal distal tubule
Na reabsorption K & H excretion Adrenal insufficiency
Addisons ds

Hypokalemia
by thiazide & loop diuretics

Congenital adrenogenital syn Tx idiopathic orthostatic hypotension w/ Na intake

Glyburide
Antidiabetic Sulfonylurea hypoglycemia Closes ATP-sensitive K channels preventing K efflux & depolarizing pancreas B cells
Influx Ca & relaxing insulin

Photosensitivity Hypoglycemia

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

Insulin
Antidiabetic Pancreatic hormone Replaces endogenous insulin
DM Rapid acting lispro Intermediate acting lente Long acting ultralente

Hypoglycemia -blockers mask signs of hypoglycemia & prolong recovery

Levothyroxine
Thyroid hormone Tetraiodothyronine Binds nuclear receptors & gene transcription
metabolic rate, protein synthesis, gluconeogenesis, cell growth & differentiation, & CNS development

Insomnia Irritability Tachycardia Wt loss Bile acid sequestrants absorption

Converted to T3 in tissues
Hypothyroidism

Medroxyprogesterone
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

Amenorrhea Breakthrough bleeding Dysmenorrhea

Metformin
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

N, V, D Abdominal bloating

Methimazole
Antithyroid Thiourea, thyroid hormone synthesis inhibitor Inhibits peroxidase & iodination & coupling of tyrosine residue of thyroglobulin thyroxine secretion
Hyperthyroidism Graves ds

Rash Agranulocytosis

Mifepristone
Abortificient Progesterone antagonist Partial agonist or antagonist progesterone receptors
Medical termination of pregnancy through 49d gestation Single dose + prostaglandin for 48hr stim. uterine contractions

Abdominal pain Diarrhea N, V Uterine bleeding Cramping

Octreotide
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

Arrhythmias Hyperglycemia Hypoglycemia Constipation Diarrhea Flatulence N

Oxytocin
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

Excessive & painful uterine contractions

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 appearance
Moon facies Buffalo hump

susceptibility to infection

Raloxifene
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

Hot flashes Cholestyramine inhibits absorption

Repaglinide
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

Hypoglycemia

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

Testosterone
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 androgen-deficient men Delayed puberty in males

Edema Acne Gynecomastia Impotence Oligospermia Priapism

Gastrointestinal

Bisacodyl Calcium carbonate Dicyclomine Docusate Lactulose Loperamide Mesalamine Metoclopramide

Misoprostol Omeprazole Ondansetron Promethazine Ranitidine Sucralfate Tegaserod

Bisacodyl
Stimulant laxative Inhibits GI fluid reabsorption & stimulates peristalsis
Bowel evacuation prior colonoscopy or surgery Acute constipation Cramping N Fluid & electrolyte depletion
Hypokalemia

Calcium carbonate
Antacid, Ca supplement Ca salt Neutralizes gastric acid Provides Ca supplementation
Dyspepsia Hypocalcemia Prevention of osteoporosis Admin 1-1.5hr after meals & @ bedtime Constipation absorption of drugs
Tetracyclines Fluoroquinolones Phenytoin Iron salts

Dicyclomine
Antispasmodic Muscarinic receptor antagonist Blocks PNS stim. intrinsic nervous system & GI tone & motility
Directly relaxes GI smooth m. IBS cramping & pain Constipation Dyspepsia Dry mouth Urinary retention Blurred vision Decreased sweating

Docusate
Stool softener, laxative Surface-active agent Facilitates hydration of fecal material & softens feces
Constipation Fecal impaction rectal enema

Lactulose
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

Cramping Abdominal distention Flatulence

Loperamide
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

Constipation Drowsiness Additive effects

Kava Chamomile Valerian

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 sulfapyridine mesalamine &

Metoclopramide
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 CI in Parkinsons ds & seizure disorders Drowsiness EPS rxns restlessness

Misoprostol
Cytoprotective Synthetic PGE1 analogue gastric mucosal secretion & secretion of bicarbonate & mucus
Prevent gastric mucosal injury from NSAIDs Abortificient in combo w/ mifepristone CI in pregnancy Abdominal pain D Miscarriage

Omeprazole
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 Abdominal pain Inhibits metabolism
Diazepam Cyclosporine Phenytoin

Ondansetron
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 HA Constipation D

Promethazine
Antiemetic, antihistamine, sedative H1 receptor antagonist, phenothiazine Blocks H1 & M1 receptors Inhibits stim. chemoreceptor trigger zone & vomiting center
N, V Preoperative sedation Allergic rxns Neuroleptic malignant syn Sedation Confusion Disorientation

Ranitidine
Antiulcer H2 receptor antagonist Blocks H2 receptors in gastric parietal cells
gastric acid secretion Peptic ulcer ds GE reflux Dyspepsia

Sucralfate
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 Constipation absorption
Fat soluble vitamins fluoroquinolones

Tegaserod
GI motility agent Partial agonist @ 5-HT4 receptors Activates 5-HT4 receptors on sensory neurons in enteric nervous system
Release neurotransmitters & peristalsis IBS in women w/ constipation Diarrhea Ischemic colitis

Hematologic

Abciximab Alteplase Aspirin Atorvastatin Bivalirudin Cholestyramine Cilostazol Clopidogrel Cyclosporine Enoxaparin

Epoetin Eptifibatide Ezetimibe Filgrastim Folic acid Gemfibrozil Heparin Niacin Sirolimus Warfarin

Abciximab
Antithrombotic Monoclonal Ab Inactivates platelet gp llb/llla receptors
Prevents platelet aggregation Prevent thrombosis during coronary angioplasty & stent placement Bleeding Thrombocytopenia

Alteplase
Thrombolytic Plasminogen activator Converts plasminogen plasmin
Degrades fibrin & fibrinogen AMI Acute ischemic stroke Occluded central venous access devices Streptokinase & urokinase for pulmonary embolism Reperfusion arrhythmia Contraindications
Internal bleeding Recent CNS surgery or trauma

Atorvastatin
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 Myalgia Myositis Rhabdomyolysis Hepatitis GI distress Effects w/
Grapefruit juice Azole antifungals cyclosporine

Bivalirudin
Anticoagulant Hirudin analogue Inhibits thrombin
Prevents blood coagulation Thrombosis in unstable angina AMI Stent insertion Used in pts w/ heparininduced thrombocytopenia

Bleeding

Cholestyramine
Cholesterol-lowering agent Bile-acid binding resin Binds intestinal bile acids
Prevents reabsorption cholesterol utilization
LDL levels

Constipation Abdominal discomfort

Hypercholesterolemia Diarrhea d/t excess bile acids

Cilostazol
Antiplatelet Platelet aggregation inhibitor Inhibits phosphodiesterase III & cAMP in platelet & blood vessels
Inhibit platelet aggregation Causes vasodilation Intermittent claudication
Improves blood flow & walking distance

HA Effects w/ CYP3A4 inhibitors

Azole antifungals Erythromycin Grapefruit juice

Additive effects w/ aspirin

Clopidogrel
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 Hypersensitivity reaction

Cyclosprine
Immunosuppressant IL2 expression inhibitor Bind immunophilins
Complex binds calcineurin inhibits transcription of IL2 gene Prevent rejection of renal, cardiac or hepatic allografts Severe RA & psoriasis HTN Nephrotoxic Gingival hyperplasia Hirsutism Tremor Induce metabolism
Rifampin Barbiturates Carbamazepine

Inhibits metabolism
Grapefruit juice

Enoxaparin
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

Thrombocytopenia

Effects reversed w/ protamine sulfate NO monitoring w/ PTT

Epoetin
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

HTN

Used as performance-enhancing drug by athletes

Eptifibatide
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

Bleeding

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

Filgrastim
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 Bone pain

Folic acid
Vitamin, hematologic agent Metabolic cofactor for DNA synthesis Activated folate transfer one-carbon units to purine & pyrimidine precursors
Megaloblastic anemia Fetal neural tube defects Coronary artery ds Pregnant woman have requirements Absorption by
Phenytoin Cholestyramine

Folate reductase inhibited by MTX

Gemfibrozil
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 GI distress Myositis Statins risk rhabdomyolisys

Heparin
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 Thrombocytopenia

Niacin
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 Flushing Pruritis GI distress, peptic ulcer Hyperglycemia Hepatotoxicity Statins risk rhabdomyolysis

Sirolimus
Immunosuppressant T-lymphocyte inhibitor Inhibits regulatory kinase in cytokinedriven T-cell prolif.
Combo w/ corticosteroid & cyclosporine Prevent
Rejection renal allograph Coronary stent restenosis

Leukopenia Thrombocytopenia Hyperlipidemia Rash blood levels

Cyclosporine Azole antifungals Erythromycin Grapefruit juice Cimetidine

Warfarin
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 Fetal malformations Abnormal bone development

Musculoskeletal

Acetaminophen Allopurinol Celecoxib Cyclobenaprine Etanercept Ibuprofen

Indomethacin Infliximab Ketorolac Probenecid & colchicine

Acetaminophen
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 OD cause fatal hepatic failure hepatotoxicity w/ alcohol renal toxicity w/ salicylates & NSAIDs

Allopurinol
Antigout Xanthine oxidase inhibitor Inhibits xanthine oxidase & catabolism of purines xanthine & uric acid
uric acid levels Prevent hyperuricemia & gout Rash Inhibits metabolism
Mercaptopurine

Celecoxib
NSAID COX-2 inhibitor Inhibits COX-2 & synthesis of PG causing pain, fever, & inflammation
OA RA Inflammatory jt ds GI bleeding risk stroke & MI

Cyclobenzaprine
Skeletal m. relaxant Tricyclic central-acting m. relaxant Acts on brainstem & spinal cord to reduce tonic somatic m. activity via & motor neurons
Acute muscle spasm Dizziness Drowsiness Dry mouth AVOID MAOI

Etanercept
Antirheumatic agent, antitumor necrosis factor Antitumor necrosis factor p57 combined w/ Fc of IgG Binds TNF- & jt inflammation & pain Slows progression of RA
RA URI HA Ab response to live virus vaccines

Ibuprofen
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

GI bleeding N, V Dyspepsia Allergic rxns Hepatitis & renal failure

risk colon, breast, lung, & prostate cancers

Indomethacin
NSAID Nonselective COX inhibitor Inhibits COX-1 & COX-2
Inflammatory disorders
Gouty arthritis OA RA Ankylosing spondylitis

GI bleeding N, V Dyspepsia Allergic rxns Dizziness Drowsiness HA

PDA in premature neonates

Infliximab
Ds modifying antirheumatic Monoclonal Ab to TNF Inactivates TNF- & jt inflammation, pain, & destruction Sx of Crohns ds
RA Crohns ds Fatigue N, V URI

Ketorolac
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

Aspirin-allergy Allergic rxn in pt w/ asthma Nasal polyps

Probenecid & Colchicine

Antigout Uricosuric probenicid Anti-inflammatory colchicine Probenecid
Inhibits renal reabsorption of uric acid & uric acid secretion

Probenecid
Inhibits renal tubular secretion of Penicillins
Used to penicillin serum levels

Colchicine
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

Baclofen
Antispasticity GABA-B receptor agonist neuronal cAMP & Ca influx
K influx motor neuron excitability & inhibits spinal reflexes Spasticity
MS Spinal cord injury ALS

Drowsiness Dizziness Fatigue Weakness Additive effects

Alcohol Kava Valerian Chamomile

Benztropine
Anti-Parkinson Central anticholinergic Blocks cholinergic receptors & restores neurotransmitter balance in basal ganglia
Parkinsons ds Drug-induced EPS tremor > bradykinesia & rigidity Blurred vision Dry eyes Constipation Dry mouth Urinary retention

Donepezil
Anti-Alzheimer Cholinesterase inhibitor Inhibits cholinesterase in CNS
Ach neurotransmission Slows decline in cognitive function Alzheimers ds Does NOT prevent ds progression N, D HA

Entacapone
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 Rhabdomyolysis Neuroleptic malignant syndrome

Interferon-beta-1b
Anti-multiple sclerosis Interferon Binds cell surface receptors producing immuno-suppressive effects
relapse & slows physical disability in MS Relapsing-remitting MS SubQ daily HA Weakness GI distress Sweating Neutropenia Myalgia Chills Fever

Levodopa-carbidopa
Anti-Parkinson Dopamine precursor, decarboxylase inhibitor Levodopa
Converted to D in CNS
Augments neurotransmission in basal ganglia

Dyskinesia involuntary movements N, V Hallucinations arrhythmia w/ halothane

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

Pergolide
Anti-Parkinson Dopamine receptor agonist Activates D receptors in basal ganglia
Parkinsons ds in conjunction w/ levodopa/carbidopa Dyskinesia Hallucination Orthostatic hypotension Constipation

Selegiline
Anti-Parkinson Type B MAOI
Converted to active form by MAO Irreversibly inhibits D degradation by MAO
response to levodopa/carbidopa Tx Parkinsons ds w/ levodopa/carbidopa Slows progression of Parkinsons ds
AVOID Meperidine & opioids
Fatal rxn Excitation Rigidity HTN coma Serotonin syn Asystole HTN Syncope Rigidity seizures

SSRI

Tricyclics

Other Drugs

Alprostadil Bosentan Epoprostenol

Latanoprost Mesna Succimer

Alprostadil
Vasodilator Prostaglandin E1 Activates PG EP receptors
Vascular smooth m. relaxation & vasodilation Maintain PDA in neonates awaiting surgery
IV infusion

IV infusion
Apnea Hypotension Arrhythmia

Local products
Prolonged/painful erection lightheadedness

Male erectile dysfunction

Local injection or pellets

Bosentan
Vasodilator Endothelin-1 receptor antagonist Blocks endothelin A & B receptors pulmonary vascular resistance & dyspnea Improves walking distance
Pulmonary arterial HTN CI in pregnancy
Causes birth defects

serum aminotransferase levels

Epoprostenol
Vasodilator Naturally occurring prostacyclin (PGI2) Activated prostaglandin IP receptors
Vascular smooth m. relaxation Flushing Hypotension Tachycardia Diarrhea N, V

pulmonary blood flow & reduces dyspnea

Pulmonary arterial HTN

Latanoprost
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 Alters color of iris causing permanent eye color change by amount of melanin in melanocytes

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

Amitriptyline
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
Lethargy Sedation Blurred vision Constipation Urinary retention appetite & wt gain OD wide QRS complex VT Altered effects by drugs that inhibit/induce CYP450
Carbamazepine Quinidine Rifampin

Amphetamine
CNS stimulant Sympathomimetic amine neuronal release of norepinephrine
ADHD
attention span motor restlessness

Tachycardia HTN Anorexia Irritability Insomnia Tremor Growth inhibition Drug dependence HTN crisis w/ MAOI

Narcolepsy
mental alertness drowsiness & fatigue

Atomoxetine
ADHD agent Selective NE reuptake inhibitor Inhibits neuronal reuptake of NE in CNS
ADHD in children/adults levels & effect in slow metabolizers CYP2D6 appetite Insomnia Levels & effects altered by drugs that inhibit/induce CYP2D6

Bupropion
Antidepressant Neuronal reuptake inhibitor Inhibits neuronal reuptake of DA > 5-HT & NE
Depression Smoking cessation Delayed onset for antidepressant effects Agitation HA Dry mouth N Tremor Impaired motor & cognitive skills MAOI adverse effects Seizure risks w/ phenothiazines

Desipramine
Antidepressant Tricyclic Blocks neuronal reuptake NE > 5-HT Blocks muscarinic & adrenergic receptors
Depression Chronic pain Delayed onset for antidepressant effects AVOID
MAOI SSRI

Lethargy Sedation Blurred vision Constipation Urinary retention appetite & wt gain OD wide QRS complex VT

Fluoxetine
Antidepressant SSRI Inhibits neuronal reuptake of serotonin
Depression OCD Bulimia nervosa Anorexia nervosa Fibromyalgia Panic attacks Phobias Prementsrual dysmorphic disorder Active metabolite 5-7d half-life AVOID MAOI Anxiety Drowsiness Insomnia Nervousness Sexual dysfunction Sweating Tremor levels metabolized by CYP2D6

Haloperidol
Typical antipsychotic Butyrophenone Blocks D2 receptors in mesolimbic area, chemoreceptor trigger zone, solitary tract, & basal ganglia Blocks muscarinic & adrenergic receptors
Psychotic disorders
Schizophrenia

Neuroleptic malignant syn

Fever Respiratory distress Tachycardia Seizures Severe m. stiffness Altered BP

Extrapyramidal rxns Tardive dyskinesia Blurred vision Constipation Dry mouth Urinary retention Hypotension

Tourettes syn

Lithium
Mood stabilizer, antimanic Inorganic cation noradrenergic neurotransmission or effects b/c of cAMP Inhibition of inositol-1phosphatase
Depletion of inositol & IP3
Polyuria Impaired memory Acne Tremor ECG changes GI distress Hypothyroidism Leukocytosis NM toxicity w/ haloperidol toxicity
Diuretics NSAIDS Fluoxetine

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
Antidepressant Tetracyclic Inhibits presynaptic 2 autoreceptors & heteroreceptors
NE & 5-HT release Depression Appetite stimulation AVOID MAOI
HTN, seizure, death

appetite & wt gain Constipation Dry mouth Drowsiness

Olanzapine
Atypical antipsychotic Thienobenzodiazepine Blocks D2 & 5-HT2 receptors in CNS Blocks H1, muscarinic, & adrenergic receptors
Schizophrenia Manic episodes of biploar Anorexia nervosa Oral tablets contain aspartame
Avoid in phenylketonuria

Agitation Dizziness Restlessness Sedation Amblyopia Orthostatic hypotension Tachycardia Constipation Dry mouth Wt gain Tremor

Phenelzine
Antidepressant MAOI Inhibits MAO & CNS levels of NE & 5-HT
Neurotic & atypical depression Avoid
Fluoxetine Tyramine

Dizziness Insomnia Restlessness Blurred vision Orthostatic hypotension Diarrhea Potentially fatal
SSRI Tricyclics

HTN crisis
Tyramine Amphetamines Methyldopa Levodopa

Risperidone
Atypical antipsychotic Benzisoxazole Blocks 5-HT2 > D2 receptors in CNS Blocks H1 & -adrenergic receptors
Schizophrenia Psychotic disorders Monitor pt for neuroleptic malignant syn Aggressive behavior Extrapyramidal rxns Sleep disturbances Insomnia Sedation Constipation or diarrhea Wt gain

Thioridazine
Typical antipsychotic Phenothiazine Blocks D2 receptors in mesolimbic area, chemoreceptor trigger zone, solitary tract, & basal ganglia Blocks muscarinic receptors
Psychotic disorders Schizophrenia Extrapyramidal rxns Tardive dyskinesia Photosensitivity Potential for V arrhythmias & sudden death Retinal pigmentation w/ high doses
melanosis

Venlafaxine
Antidepressant Phenethylamine Inhibits neuronal reuptake 5-HT & NE
Depression Generalized anxiety disorder AVOID MAOI Sexual dysfunction GI distress Dizziness Insomnia Nervousness

Respiratory

Albuterol Cromolyn Diphenhydramine Fluticasone Ipratropium Loratadine

Montelukast Omalizumab Salmeterol Theophylline Zileuton

Albuterol
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

Muscle tremor Nervousness Restlessness Tachycardia HTN crisis w/ MAOI

Chronic bronchitis & emphysema

Reversible airway obstruction

Cromolyn
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 Nasal & throat irritation

Diphenhydramine
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 Drowsiness Blurred vision Dry mouth Urinary retention Anorexia

Fluticasone
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

Nasal & throat irritation Oral candidiasis

Ipratropium
Bronchodilator Muscarinic receptor antagonist Blocks muscarinic receptors in bronchial smooth m. & nasal mucosa Prevents vagal-stimulated bronchoconstriction
COPD Rhinitis Asthma Inhalation admin

Cough Nasal dryness & irritation

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 leukotriene1 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

Omalizumab
Antiasthmatic IgE antagonist Blocks IgE
Severe asthma in combo w/ corticosteroid therapy SubQ every 2-4 wks Allergic rxns
anaphylaxis

Salmeterol
Bronchodilator 2 agonist cAMP Relaxes bronchial smooth m. Inhibits late phase allergeninduced bronchoconstriction
Asthma
Prevent nocturnal attacks Exercise-induced asthma NOT acute bronchospasm

Tachycardia Nervousness HA

Inhalation admin

Theophylline
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

N, V Anxiety Insomnia Tachycardia

Zileuton
Antiasthmatic Leukotriene synthesis inhibitor Inhibits 5-lipoxygenase & leukotriene synthesis
Prevents airway inflammation & bronchoconstriction Long-term asthma control

Flu-like syn HA Drowsiness Dyspepsia serum aminotransferase levels & hepatitis Inhibits CYP450 & 3A4
theophylline & warfarin levels