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    Question Answer

    Time it takes for amount of drug to fall to half of its value; thisis a constant in first order kinetics (majority of drugs)

    Half-life (T1/2)

    Relates the amount of drug in the body to the plasmaconcentration

    Volume of distribution (VD)

    Plasma concentration of a drug at a given time Cp

    The ratio of the rate of elimination of a drug to its plasma

    concentration Clearance (CL)The elimination of drug that occurs before it reaches thesystemic circulation

    First pass effect

    The fraction of administered dose of a drug that reachessystemic circulation

    Bioavailability (F)

    When the rate of drug input equals the rate of drug elimination Steady state

    This step of metabolism makes a drug more hydrophilic andhence augments elimination

    Phase I

    Different steps of Phase I Oxidation, reduction, hydrolysis

    Inducers of Cytochrome P450 (CYP450) Barbiturates, phenytoin, carbamazepine, andrifampin

    Inhibitors of CYP450Cimetidine, ketoconazole, erythromycin,isoniazid and grapefruit

    Products of Phase II conjugationGlucuronate, acetic acid, and glutathionesulfate

    Type of kinetics when a constant percentage of substrate ismetabolized per unit time

    First order kinetics

    Drug elimination with a constant amount metabolizedregardless of drug concentration

    Zero order kinetics

    Target plasma concentration times (volume of distributiondivided by bioavailability)

    Loading dose (Cp*(Vd/F))

    Concentration in the plasma times (clearance divided bybioavailability)

    Maintenance dose (Cp*(CL/F))

    Strength of interaction between drug and its receptor Affinity

    Selectivity of a drug for its receptor Specificity

    Amount of drug necessary to elicit a biologic effect; refers tothe drug's strength

    Potency

    Maximum response achieveable from a drug Efficacy

    Ability of a drug to produce 100% of the maximum responseregardless of the potency Full agonist

    Ability to produce less than 100% of the response Partial agonist

    Ability to bind reversibly to the same site as the drug andwithout activating the effector system

    Competitive antagonist

    Class of drugs with ability to decrease the maximal response toan agonist

    Noncompetitive antagonist

    A hormone whose mechanism of action (MOA) utilizesintracellular receptors

    Thyroid and steroid hormones

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    A hormone whose MOA utilizes transmembrane receptors Insulin

    Class of drugs whose MOA utilizes ligand gated ion channels Benzodiazepines and calcium channel blockers

    Median effective dose required for an effect in 50% of thepopulation

    ED50

    Median toxic dose required for a toxic effect in 50% of thepopulation

    TD50

    Dose which is lethal to 50% of the population LD50

    Window between therapeutic effect and toxic effect Therapeutic indexTerm for a high margin of safety High therapeutic index

    Term for a narrow margin of safety Low therapeutic index

    Antidote used for lead poisoning Dimercaprol, EDTA

    Antidote used for cyanide poisoning Nitrites

    Antidote used for anticholinergic poisoning Physostigmine

    Antidote used for organophosphate/anticholinesterasepoisoning

    Atropine, pralidoxime (2-PAM)

    Antidote used for iron salt toxicity Deferoxamine

    Antidote used for acetaminophen (APAP) toxicity N-acetylcysteine (Mucomyst)Antidote for arsenic, mercury, lead, and gold poisoning Dimercaprol

    Antidote used in poisonings: copper (Wilson's disease), lead,mercury, and arsenic

    Penicillamine

    Antidote used for heparin overdose Protamine

    Antidote used for warfarin toxicity Vitamin K and Fresh frozen plasma (FFP)

    Antidote for tissue plasminogen activator (t-PA), streptokinase Aminocaproic acid

    Antidote used for methanol and ethylene glycol Ethanol or fomepizole

    Antidote used for opioid toxicity Naloxone (IV), naltrexone (PO)

    Antidote used for benzodiazepine toxicity Flumazenil

    Antidote used for tricyclic antidepressants (TCA) Sodium bicarbonate

    Antidote used for carbon monoxide poisoning 100% O2 and hyperbaric O2

    Antidote used for digitalis toxicityDigibind (also need to d/c digoxin, normalizeK+, and lidocaine if pt. Is arrhythmic)

    Antidote used for beta agonist toxicity (eg. Metaproterenol) Esmolol

    Antidote for methotrexate toxicity Leucovorin

    Antidote for beta-blockers and hypoglycemia Glucagon

    Antidote useful for some drug induced Torsade de pointes Magnesium sulfateAntidote for hyperkalemia sodium polystyrene sulfonate (Kayexalate)

    Antidote for salicylate intoxication Alkalinize urine, dialysis

    Constant proportion of cell population killed rather than aconstant number

    Log-kill hypothesis

    Treatment with cancer chemotherapy at high doses every 3-4weeks, too toxic to be used continuously

    Pulse therapy

    Toxic effect of anticancer drug can be lessened by rescueagents

    Rescue therapy

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    Drug used concurrently with toxic anticancer agents to reducerenal precipitation of urates

    Allopurinol

    Pyrimidine analog that causes "Thymine-less death"" givenwith leucovorin rescue"

    5-flouracil (5-FU)

    Drug used in cancer therapy causes Cushing-like symptoms Prednisone

    Side effect of Mitomycin SEVERE myelosuppression

    MOA of cisplatin Alkylating agent

    Common toxicities of cisplatin Nephro and ototoxicityAnalog of hypoxanthine, needs HGPRTase for activation 6-mercaptopurine (6-MP)

    Interaction with this drug requires dose reduction of 6-MP Allopurinol

    May protect against doxorubicin toxicity by scavenging freeradicals

    Dexrazoxane

    Blows DNA (breaks DNA strands), limiting SE is pulmonaryfibrosis

    Bleomycin

    Bleomycin+vinblastine+etoposide+cisplatin produce almost a100% response when all agents are used for this neoplasm

    Testicular cancer

    ABVD regimen used for HD, but appears less likely to causesterility and secondary malignancies than MOPP Adriamycin (doxorubicin) +bleomycin,vinblastine +dacarbazine

    Regimen used for non-Hodgkin's lymphomaCHOP (cyclophosphamide, doxorubicin,vincristine, and prednisone) plus rituximab

    Regimen used for breast cancerCMF (cyclophosphamide, methotrexate, andfluorouracil) and tamoxifen if ER+

    Alkylating agent, vesicant that causes tissue damage withextravasation

    Mechlorethamine

    Anticancer drug also used in RA, produces acrolein in urinethat leads to hemorrhagic cystitis

    Cyclophosphamide

    Prevention of cyclophosphamide induced hemorrhagic cystitis Hydration and mercaptoethanesulfonate(MESNA)

    Microtubule inhibitor that causes peripheral neuropathy, footdrop (eg. ataxia), and "pins and needles"" sensation"

    Vincristine

    Interact with microtubules (but unlike vinca which preventdisassembly of tubules), it stabilizes tubulin and cells remainfrozen in metaphase

    Paclitaxel (taxol)

    Toxicities include nephrotoxicity and ototoxicity, leading to asevere interaction with aminoglycosides

    Cisplatin

    Agent similar to cisplatin, less nephrotoxic, but greater

    myelosuppressionCarboplatin

    Converts asparagine to aspartate and ammonia, denies cancercells of essential AA (asparagine)

    L-asparaginase

    Used for hairy cell leukemia; it stimulates NK cells Interferon alpha

    Anti-androgen used for prostate cancer Flutamide (Eulexin)

    Anti-estrogen used for estrogen receptor + breast cancer Tamoxifen

    Aromatase inhibitor used in breast cancer Letrozole, anastrozole

    Newer estrogen receptor antagonist used in advanced breastcancer

    Toremifene (Fareston)

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    Some cell cycle specific anti-cancer drugsBleomycin, vinca alkaloids, antimetabolites(eg., 5-FU, 6-MP, methotrexate, etoposide)

    Some cell cycle non-specific drugsAlkylating agents (eg., mechlorethamine,cyclophosphamide), antibiotics (doxorubicin,daunorubicin), cisplatin, nitrosourea

    Anti-emetics used in association with anti-cancer drugs thatare 5-HT3 (serotonin receptor subtype ) antagonists

    Odansetron, granisetron

    Nitrosoureas with high lipophilicity, used for brain tumors Carmustine (BCNU) and lomustine (CCNU)

    Produces disulfiram-like reaction with ethanol Procarbazine

    Somatostatin (SRIF) analog used for acromegaly, carcinoid,glucagonoma and other GH producing pituitary tumors

    Octreotide

    Somatotropin (GH) analog used in GH deficiency (dwarfism) Somatrem

    GHRH analog used as diagnostic agent Sermorelin

    GnRH agonist used for infertility or different types of CAdepending on pulsatile or steady usage respectively

    Leuprolide

    GnRH antagonist with more immediate effects, used forinfertility

    Ganirelix

    Dopamine (DA) agonist (for Parkinson's disease), used also forhyperprolactinemia

    Bromocriptine

    Hormone inhibiting prolactin release Dopamine

    ACTH analog used for diagnosis of patients with corticosteroidabnormality

    Cosyntropin

    Synthetic analog of ADH hormone used for diabetes insipidusand nocturnal enuresis

    Desmopressin (DDAVP)

    SE of OCs Increased thromboembolic events

    Most widely used thyroid drugs such as Synthroid andLevoxyl contain

    L-thyroxine (T4)

    T3 compound less widely used Cytomel

    Anti-thyroid drugsThioamides, iodides, radioactive iodine, andipodate

    Thioamide agents used in hyperthyroidism Methimazole and propylthiouracil (PTU)

    Thioamide less likely to cross placenta, inhibits peripheralconversion of T4 to T3 in high doses, and should be used withextreme caution in pregnancy

    PTU

    PTU (propylthiouracil) MOAInhibits thyroid hormone synthesis by blockingiodination of the tyrosine residues of

    thyroglobulinCan be effective for short term therapy of thyroid storm, butafter several weeks of therapy causes an exacerbation ofhyperthyroidism

    Iodide salts

    Dose may need to be increased during pregnancy or with Ocsdue to increased TBG in plasma

    Thyroxine

    Permanently cures thyrotoxicosis, patients will need thyroidreplacement therapy thereafter. Contraindicated in pregnancy

    Radioactive iodine

    Radio contrast media that inhibits the conversion of T4 to T3 Ipodate

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    Block cardiac adverse effects of thyrotoxicosis such astachycardia, inhibits the conversion of T4 to T3

    Beta-blockers such as propranolol

    Vitamins containing iron should NOT be taken simultaneouslywith levothyroxine because

    Iron deiodinates thyroxine

    Thyroxine dose may need to be increased in hypothyroidpatient during pregnancy because

    Estogens increase maternal TBG

    3 zones of adrenal cortex and their productsGlomerulosa (mineralocorticoids), fasciculata(glucocorticoid=GC), and reticularis (adrenal

    androgens)Pneumonic for 3 zones of adrenal cortex GFR

    Used for Addison's disease, Congenital Adrenal Hyperplasia(CAH), inflammation, allergies, and asthma (as a localinhalation)

    Glucocorticoids

    Short acting glucocorticoidsCortisone and hydrocortisone (equivalent tocortisol)

    Intermediate acting glucocorticoidsPrednisone, methylprednisolone, prednisolone,and triamcinolone

    Long acting glucocorticoids Betamethasone and dexamethasoneMineralocorticoids Fludrocortisone and deoxycorticosterone

    Some side effects of corticosteroidsOsteopenia, impaired wound healing, inc. riskof infection, inc. appetite, HTN, edema, PUD,euphoria, psychosis, stria, thinning of skin

    Period of time of therapy after which GC therapy will need tobe tapered

    5-7 days

    Used for Cushing's syndrome (increased corticosteroid) Dexamethasone suppression test

    Inhibits conversion of cholesterol to pregnenolone thereforeinhibiting corticosteroid synthesis

    Aminoglutethimide

    Antifungal agent used for inhibition of all gonadal and adrenalsteroids

    Ketoconazole

    Antiprogestin used as potent antagonist of GC receptor Mifepristone

    Diuretic used to antagonize aldosterone receptors Spironolactone

    Common SE of spironolactone Gynecomastia and hyperkalemia

    Slightly increased risk of breast cancer, endometrial cancer,heart disease (questionable), has beneficial effects on bone loss

    Estrogen

    Antiestrogen drugs used for fertility and breast cancerrespectively

    Clomiphene and tamoxifen

    Common SE of tamoxifen and raloxifene Hot flashesSelective estrogen receptor modulator (SERM) used forprevention of osteoporosis and prophylaxis in women with riskfactors for breast cancer

    Raloxifene

    Non-steroidal estrogen agonist causes clear celladenocarcinoma of the vagina in daughters of women whoused it during pregnancy

    Diethylstilbestrol (DES)

    Estrogen mostly used in oral contraceptives (OC) Ethinyl estradiol and mestranol

    Anti-progesterone used as abortifacient Mifepristone (RU-486)

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    Constant low dose of estrogen and increasing dose of progestinfor 21 days (last 5 days are sugar pills or iron prep)

    Combination oral contraceptives (OC)

    Oral contraceptive available in a transdermal patch Ortho-Evra

    Converted to more active form DHT by 5 alpha-reductase Testosterone

    5 alpha-reductase inhibitor used for benign prostatichyperplasia (BPH) and male pattern baldness

    Finasteride (Proscar and Propecia respectively)

    Anabolic steroid that has potential for abuse Nandrolone, oxymetholone, and oxandrolone

    Anti-androgen used for hirsutism in females Cyproterone acetateDrug is used with testosterone for male fertility Leuprolide

    What do alpha cells in the pancreas produce? Glucagon

    What do beta cells in the pancreas produce? Insulin

    Where are beta cells found in the pancreas? Islets of Langerhans

    What do delta cells in the pancreas produce? Somatostatin

    Product of proinsulin cleavage used to assess insulin abuse C-peptide

    Exogenous insulin contains Little C-peptide

    Endogenous insulin contains Normal C-peptide

    Very rapid acting insulin, having fastest onset and shortestduration of action

    Lispro (Humalog), aspart, glulisine

    Rapid acting, crystalline zinc insulin used to reverse acutehyperglycemia

    Regular (Humulin R)

    Long acting insulin Ultralente (humulin U)

    Ultra long acting insulin, has over a day duration of action Glargine (Lantus), detemir

    Major SE of insulin Hypoglycemia

    Important in synthesis of glucose to glycogen in the liver GLUT 2

    Important in muscle and adipose tissue for glucose transport

    across muscles and TG storage by lipoprotein lipase activation GLUT 4Examples of alpha-glucosidase inhibitors (AGI) Acarbose, miglitol

    MOA of AGI'sAct on intestine, delay digestion andabsorption of glucose formed from digestion ofstarch and disacchrides

    SE of AGI'sFlatulence (do not use beano to tx), diarrhea,abdominal cramps

    Alpha-glucosidase inhibitor associated with elevation of LFT's Acarbose

    Amino acid derivative, active as an insulin secretagogue Nateglinide

    MOA of nateglinide Insulin secretagogue - closes ATP-sensitiveK+ channel

    Biguanide Metformin

    Drugs available in combination with metformin Glyburide, glipizide, and rosiglitazone

    MOA of metforminDecreases hepatic glucose production andintestinal glucose absorption; increase insulinsensitivity

    Vascular effects of metformin Decreased micro and macro vascular disease

    Most important potential SE of metformin Lactic acidosis

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    Incidence of hyoglycemia with metformin

    Meglitinide class of drugs Repaglinide

    MOA of repaglinideInsulin release from pancreas; faster andshorter acting than sulfonylurea

    First generation sulfonylurea Chlorpropamide, tolbutamide, tolazamide, etc.

    Second generation sulfonylurea Glyburide, glipizide, glimepiride, etc.

    MOA of both generationsInsulin release from pancreas by modifying K+

    channelsCommon SE of sulfonylureas, repaglinide, and nateglinide Hypoglycemia

    Sulfonylurea NOT recommended for elderly because of verylong half life

    Chlorpropamide

    ThiazolidinedionesPioglitazone, Rosiglitazone, Troglitazone(withdrawn/d from market)

    Reason troglitazone was withdrawn from market Hepatic toxicity

    MOA of thiazolindinedionesStimulate PPAR-gamma receptor to regulateCHO and lipid metabolism

    SE of Thiazolindinediones Edema, mild anemia; interaction with drugsthat undergo CytP450 3A4 metabolism

    Hyperglycemic agent that increases cAMP and results inglycogenolysis, gluconeogenesis, reverses hypoglycemia, alsoused to reverse severe beta-blocker overdose and smoothmuscle relaxation

    Glucagon

    Available bisphosphonatesAlendronate, etidronate, risedronate,pamidronate, tiludronate, and zoledronic acid

    MOA of Bisphosphonates Inhibits osteoclast bone resorption

    Names of three bisphosphonates available IV Pamidronate, zoledronate, ibandronate

    Uses of bisphosphonates Osteoporosis, Paget's disease, and osteolyticbone lesions, and hypercalcemia frommalignancy

    Major SE of bisphosphonates Chemical esophagitis

    Bisphosphonates that cannot be used on continuous basisbecause it caused osteomalacia

    Etidronate

    Used for prevention of postmenopausal osteoporosis in women Estrogen (HRT-Hormone replacement therapy)

    Increase bone density, also being tested for breast CAprophylaxis

    Raloxifene (SERM-selective estrogen receptormodulator)

    Used intranasally and decreases bone resorption Calcitonin (salmon prep)

    Used especially in postmenopausal women, dosage should be1500 mg

    Calcium

    Vitamin given with calcium to ensure proper absorption Vitamin D

    Disease caused by excess ergot alkaloids St. Anthony's Fire

    Endogenous substances commonly interpreted as histamine,serotonin, prostaglandins, and vasoactive peptides

    Autocoids

    Syndrome of hypersecretion of gastric acid and pepsin usuallycaused by gastrinoma; it is associated with severe pepticulceration and diarrhea

    Zollinger-Ellison Syndrome

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    Drug that causes contraction of the uterus Oxytocin

    Distribution of histamine receptors H1, H2, and H3Smooth muscle; stomach, heart, and mast cellsnerve endings, CNS respectively

    Prototype antagonist of H1 and H2 receptors Diphenhydramine and cimetridine, respectively

    1st generation antihistamine that is highly sedating Diphendydramine

    1st generation antihistamine that is least sedating Chlorpheniramine or cyclizine

    2nd generation antihistamines Fexofenadine, loratadine, and cetirizine

    Generation of antihistamine that has the most CNS effects First generation due to being more lipid-soluble

    Major indication for H1 receptor antagonist Use in IgE mediated allergic reaction

    Antihistamine that can be used for anxiety and insomnia and isnot addictive

    hydroxyzine (Atarax)

    H1 antagonist used in motion sicknessDimenhydrinate, meclizine, and other 1stgeneration

    Most common side effect of 1st generation antihistamines Sedation

    Lethal arrhythmias resulting from concurrent therapy withazole fungals (metabolized by CYP 3A4) and theseantihistamines which inhibit the 3A4 iso-enzyme.

    Terfenadine and astemizole (have been

    removed from the market)

    H2 blocker that causes the most interactions with other drugs Cimetidine

    Clinical use for H2 blockersAcid reflux disease, duodenal ulcer and pepticulcer disease

    Receptors for serotonin (5HT-1) are locatedMostly in the brain, and they mediate synapticinhibition via increased K+ conductance

    5HT-1d agonist used for migraine headaches Sumatriptan, naratriptan, and rizatriptan

    Triptan available in parenteral and nasal formulation Sumatriptan

    H1 blocker that is also a serotonin antagonist Cyproheptadine

    Agents for reduction of postpartum bleeding Oxytocin, ergonovine and ergotamine

    Agents used in treatment of carcinoid tumorKetanserin cyproheptadine, andphenoxybenzamine

    5HT-3 antagonist used in chemotherapeutic induced emesisOndansetron, granisetron, dolasetron andalosetron

    5HT-3 antagonist that has been associated with QRS and QTcprolongation and should not be used in patients with heartdisease

    Dolasetron

    DOC to treat chemo-induced nausea and vomiting Odansetron

    Drug used in ergot alkaloids overdose, ischemia and gangrene NitroprussideReason ergot alkaloids are contraindicated in pregnancy Uterine contractions

    SE of ergot alkaloids Hallucinations resembling psychosis

    Ergot alkaloid used as an illicit drug LSD

    Dopamine agonist used in hyperprolactinemia Bromocriptine

    Peptide causing increased capillary permeability and edema Bradykinin and histamine

    Mediator of tissue pain, edema, inactivated by ACE, and maybe a contributing factor to the development of angioedema

    Bradykinin

    Drug causing depletion of substance P (vasodilator) Capsaicin

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    Prostaglandins that cause abortionsProstaglandin E1 (misoprostol) PGE2, andPGF2alpha

    Difference between COX 1 and COX 2COX 1 is found throughoutthe body and COX2 is onlyin inflammatory tissue

    Drug that selectively inhibits COX 2 Celecoxib and rofecoxib

    Inhibitor of lipoxygenase Zileuton

    Major SE of zileuton Liver toxicity

    Inhibitor of leukotrienes (LTD4) receptors and used in asthma Zafirlukast and montelukastUsed in pediatrics to maintain patency of ductus arteriosis PGE1

    Approved for use in severe pulmonary HTN PGI2 (epoprostenol)

    Prostaglandin used in the treatment of impotence Alprostadil

    Irreversible, nonselective COX inhibitor Aspirin

    Class of drugs that reversibly inhibit COX NSAIDS

    Primary endogenous substrate for Nitric Oxidase Synthase Arginine

    MOA and effect of nitric oxideStimulates cGMP which leads to vascularsmooth muscle relaxation

    Long acting beta 2 agonist used in asthma Salmeterol

    Muscarinic antagonist used in asthma Ipratropium

    MOA of cromolyn Mast cell stabilizer

    Methylxanthine derivative used as a remedy for intermittentclaudication

    Pentoxifylline

    MOA of corticosteroids inhibit phospholipase A2

    SE of long term (>5 days) corticosteroid therapy and remedyAdrenal suppression and weaning slowly,respectively

    MOA of quinolones Inhibit DNA gyrase

    MOA of penicillin Block cell wall synthesis by inhibitingpeptidoglycan cross-linkage

    Drug used for MRSA Vancomycin

    Vancomycin MOA Blocks peptidoglycan synthesis

    Type of resistance found with vancomycin Point mutation

    Meningitis prophylaxis in exposed patients Rifampin

    Technique used to diagnose perianal itching, and the drug usedto treat it

    Scotch tape technique and mebendazole

    Two toxicities of aminoglycosides nephro and ototoxicity

    DOC for Legionnaires' disease Erythromycin

    MOA of sulfonamides Inhibit dihydropteroate synthase

    Penicillins active against penicillinase secreting bacteria Methicillin, nafcillin, and dicloxacillin

    Cheap wide spectrum antibiotic DOC for otitis media Amoxicillin

    Class of antibiotics that have 10% cross sensitivity withpenicillins

    Cephalosporins

    PCN active against pseudomonas Carbenicillin, piperacillin and ticarcillin

    Antibiotic causing red-man syndrome, and preventionVancomycin, infusion at a slow rate and

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    antihistamines

    Drug causes teeth discoloration Tetracycline

    MOA of tetracyclineDecreases protein synthesis by inhibiting 30Sribosome

    Drug that causes gray baby syndrome and aplastic anemia Chloramphenicol

    Drug notorious for causing pseudomembranous colitis Clindamycin

    DOC for tx of pseudomembranous colitis Metronidazole

    Treatment of resistant pseudomembranous colitis ORAL vancomycinAnemia caused by trimethoprim Megaloblastic anemia

    Reason fluoroquinolones are contraindicated in children andpregnancy

    Cartilage damage

    DOC for giardia, bacterial vaginosis, pseudomembranouscolitis, and trichomonas

    Metronidazole

    Treatment for TB patients (think RIPE)Rifampin, Isoniazid, Pyrazinamide, andEthambutol

    Metronidazole SE if given with alcohol Disulfiram-like reaction

    Common side effect of Rifampin Red urine discolorationMOA of nystatin Bind ergosterol in fungal cell membrane

    Neurotoxicity with isoniazid (INH) prevented by Administration of Vit. B6 (pyridoxine)

    Toxicity of amphotericin Nephrotoxicity

    SE seen only in men with administration of ketoconazole Gynecomastia

    Topical DOC in impetigo Topical mupirocin (Bactroban)

    DOC for influenza A Amantadine

    DOC for RSV Ribavirin

    DOC for CMV retinitis Ganciclovir

    SE for ganciclovir Neutro, leuko and thrombocytopenia

    Anti-viral agents associated with Stephen Johnson syndrome Nevirapine, amprenavir

    HIV antiviral class known to have severe drug interactions bycausing inhibition of metabolism

    Protease inhibitors

    Antivirals that are teratogens Delavirdine, efavirenz, and ribavirin

    Antivirals associated with neutropeniaGanciclovir, zidovudine, saquinavir, andinterferon

    HIV med used to reduce transmission during birth AZT (zidovudine)

    Drug used for African sleeping sickness Suramin

    Drug used in Chagas disease Nifurtimox

    Cephalosporins able to cross the BBBCefuroxime (2nd) generation, Ceftazidime,Ceftriaxone

    Cephalosporins NOT able to cross the BBB Cefixime (3rd) generation

    Drug used for N. gonorrhea in females Ceftriaxone

    Cephalosporin causes kernicterus in neonates Ceftriaxone or cefuroxime

    SE of INH Peripheral neuritis and hepatitis

    Aminoglycoside that is least ototoxic Streptomycin

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    Drug used in exoerythrocytic cycle of malaria Primaquine

    Oral antibiotic of choice for moderate inflammatory acne Minocycline

    Drug of choice for leprosyDapsone, rifampin and clofaziminecombination

    DOC for herpes and its MOAAcyclovir; incorporated into viral DNA andchain termination

    Anti-microbials that cause hemolysis in G6PD-deficientpatients

    Sulfonamides

    MOA of erythromycinInhibition of protein synthesis at the 50ssubunit of ribosome

    Anti-biotic frequently used for chronic UTI prophylaxis sulfamethoxazole/ trimethoprim

    Lactam that can be used in PCN allergic patients Aztreonam

    SE of imipenem Seizures

    Anti-viral with a dose limiting toxicity of pancreatitis Didanosine

    Common side effect of hypnotic agents Sedation

    Occurs when sedative hypnotics are used chronically or at highdoses

    Tolerance

    The most common type of drug interaction of sedativehypnotics with other depressant medications

    Additive CNS depression

    Benzodiazepines used to promote sleep Temazpam, trizolam, flurazepam

    Benzodiazepine used for anxiety Alprazolam

    Non-benzodiazepine used as an anxiolytic Buspirone

    Non-benzodiazepine used for sleep Zolpidem

    Major effect of benzodiazepines on sleep at high doses REM is decreased

    Neurologic SE of benzodiazepines Anterograde amnesia

    Reason benzos are used cautiously in pregnancy Ability to cross the placentaMain route of metabolism for benzodiazepines Hepatic

    Benzodiazepine that undergo extrahepatic conjugation (whichare useful in older or hepatically impaired)

    Lorazepam, oxazepam, and temazepam

    MOA for benzodiazepinesincrease the FREQUENCY of GABA-mediated chloride ion channel opening

    Antidote to benzodiazepine overdose (antagonist that reversesthe CNS effects)

    Flumazenil

    Benzodiazepine with useful relaxant effects in skeletal musclespasticity of central origin

    Diazepam

    Benzodiazepine that has efficacy against absence seizures andin anxiety states, such as agoraphobia

    Clonazepam

    Benzodiazepines that are the most effective in the treatment ofpanic disorder

    Alprazolam and Clonazepam

    Benzodiazepine that is used for anesthesia Midazolam

    DOC for status epilepticus Diazepam

    Longer acting benzodiazepines used in the management ofwithdrawal states of alcohol and other drugs

    Chlordiazepoxide and Diazepam

    Agents having active metabolites, long half lives, and a high Diazepam, Flurazepam, chlordiazepoxide, and

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    incidence of adverse effects clorazepate

    Barbiturates

    Barbiturates may precipitate this hematologic condition Acute intermittent porphyria

    Barbiturates decrease the effectiveness of many other drugs viathis pharmacokinetics property

    Liver enzyme INDUCTION

    Barbiturates MOAIncrease the DURATION of GABA-mediatedchloride ion channels

    Barbiturate used for the induction of anesthesia ThiopentalSite of action for zaleplon and zolpidem

    Benzodiazepine receptor BZ1 (although do nothave a benzodiazepine ring structure)

    Good hypnotic activity with less CNS SE than mostbenzodiazepines

    Zolpidem, zaleplon

    Agent that is a partial agonist for the 5-HT1A receptor Buspirone

    Drug of choice for generalized anxiety disorder, NOT effectivein acute anxiety

    Buspirone

    Agent that is metabolized to acetaldehyde by alcoholdehydrogenase and microsomal ethanol-oxidizing system

    (MEOS)

    Ethanol

    Agent with zero-order kinetics Ethanol

    Rate limiting step of alcohol metabolism Aldehyde dehydrogenase

    System that increases in activity with chronic ethanol exposureand may contribute to tolerance

    MEOS

    Enzyme that metabolizes acetaldehyde to acetate Aldehyde dehydrogenase

    Agents that inhibit acetaldehyde dehydrogenaseDisulfiram, metronidazole, certainsulfonylureas and cephalosporins

    Agent that inhibits alcohol dyhydrogenase and its clinical use

    FOMEPIZOLE used to prevent formation

    of toxic metabolites from methanol andethylene glycol ingestion

    Agent used in the treatment of alcoholism, if alcohol isconsumed concurrently, acetaldehyde builds up and results innausea, headache, flushing, and hypotension

    Disulfiram

    The most common neurologic abnormality in chronicalcoholics

    Peripheral neuropathy (also excessive alcoholuse is associated with HTN, anemia, and MI)

    Agent that is teratogen and causes a fetal syndrome Ethanol

    Agent that is the antidote for methanol overdose Ethanol, fomepizole

    Drug that inhibits alcohol dehydrogenase and is used in

    ethylene glycol exposure FomepizoleMost frequent route of metabolism Hepatic enzymes

    Mechanisms of action for Phenytoin, Carbamazepine,Lamotrigine

    Sodium channel blockade

    MOA for benzodiazepines and barbiturates GABA-related targets

    MOA for Ethosuximide Calcium channels

    MOA for Valproic acid at high dosesAffect calcium, potassium, and sodiumchannels

    Drugs of choice for generalized tonic-clonic and partial

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    seizuresValproic acid and Phenytoin

    DOC for febrile seizures Phenobarbital

    Drugs of choice for absence seizures Ethosuximide and valproic acid

    Drug of choice for myoclonic seizures Valproic acid

    Drugs of choice for status epilepticusIV diazepam for short term (acute) treatment;phenytoin for prolonged therapy

    Drugs that can be used for infantile spasms Corticosteroids

    Anti-seizure drugs used also for bipolar affective disorder(BAD)

    Valproic acid, carbamazepine, phenytoin andgabapentin

    Anti-seizure drugs used also for Trigeminal neuralgia Carbamazepine

    Anti-seizure drugs used also for pain of neuropathic orgin Gabapentin

    Anti-seizure agent that exhibits non-linear metabolism, highlyprotein bound, causes fetal hydantoin syndrome, and stimulateshepatic metabolism

    Phenytoin

    SE of phenytoinGingival hyperplasia, nystagmus, diplopia andataxia

    Anti-seizure agent that induces formation of liver drug-metabolism enzymes, is teratogen and can cause craniofacialanomalies and spina bifida

    Carbamazepine

    Agent that inhibits hepatic metabolism, is hepatotoxic andteratogen that can cause neural tube defects andgastrointestinal distress

    Valproic acid

    Laboratory value required to be monitored for patients onvalproic acid

    Serum ammonia and LFT's

    SE for Lamotrigine Stevens-Johnson syndrome

    SE for Felbamate Aplastic anemia and acute hepatic failure

    Anti-seizure medication also used in the prevention ofmigraines

    Valproic acid

    Carbamazepine may cause Agranulocytosis

    Anti-seizure drugs used as alternative drugs for moodstabilization

    Carbamazepine, gabapentin, lamotrigine, andvalproic acid

    MOA of general anestheticsMost are thought to act at GABA-A receptor -chloride channel

    Inhaled anesthetic with a low blood/gas partition coefficient Nitrous oxide

    Inversely related to potency of anestheticsMinimum alveolar anesthetic concentration

    (MAC)Inhaled anesthetics metabolized by liver enzymes which has amajor role in the toxicity of these agents

    Halothane and methoxyflurane

    Most inhaled anesthetics SE Decrease arterial blood pressure

    Inhaled anesthetics are myocardial depressants Enflurane and halothane

    Inhaled anesthetic causes peripheral vasodilation Isoflurane

    Inhaled anesthetic that may sensitize the myocardium toarrhythmogenic effects of catecholamines and has producedhepatitis

    Halothane

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    Inhaled anesthetic, less likely to lower blood pressure thanother agents, and has the smallest effect on respiration

    Nitrous oxide

    Fluoride released by metabolism of this inhaled anesthetic maycause renal insufficiency

    Methoxyflurane

    Prolonged exposure to this inhaled anesthetic may lead tomegaloblastic anemia

    Nitrous oxide

    Pungent inhaled anesthetic which leads to high incidence ofcoughing and vasospasm

    Desflurane

    DOC for malignant hyperthermia that may be caused by use ofhalogenated anesthetics

    Dantrolene

    IV barbiturate used as a pre-op anesthetic Thiopental

    Benzodiazepine used adjunctively in anesthesia Midazolam

    Benzodiazepine receptor antagonist, it accelerates recoveryfrom benzodiazepine overdose

    Flumazenil

    This produces "dissociative anesthesia"", is a cardiovascularstimulant which may increases intracranial pressure, andhallucinations occur during recovery"

    Ketamine

    Opioid associated with respiratory depression, but is used inhigh risk patients who may not survive full general anesthetia Fentanyl

    State of analgesia and amnesia produced when fentanyl is usedwith droperidol and nitrous oxide

    Neuroleptanesthesia

    Produces both rapid anesthesia and recovery, has antiemeticactivity and commonly used for outpatient surgery, may causemarked hypotension

    Propofol

    MOA of local anesthetics (LA's) Block voltage-dependent sodium channels

    This may enhance activity of local anesthetics Hyperkalemia

    This may antagonize activity of local anesthetics Hypercalcemia

    Almost all local anesthetics have this property and sometimesrequire the administration of vasoconstrictors (ex. Epinephrine)to prolong activity

    Vasodilation

    Local anesthetic with vasoconstrictive property, favored forhead, neck, and pharyngeal surgery

    Cocaine

    Longer acting local anesthetics which are less dependent onvasoconstrictors

    Tetracaine and bupivacaine

    These LA's have surface activity Cocaine and benzocaine

    Most important toxic effects of most local anesthetics CNS toxicity

    Commonly abused LA which has cardiovascular toxicityincluding severe hypertension with cerebral hemorrhage,cardiac arrhythmias, and myocardial infarction

    Cocaine

    LA causing methemoglobinemia Prilocaine

    Structurally related to acetylcholine, used to produce muscleparalysis in order to facilitate surgery or artifical ventilation.Full doses lead to respiratory paralysis and require ventilation

    Neuromuscular blocking drugs

    These drugs strongly potentiate and prolong effect ofneuromuscular blockade (NMB)

    Inhaled anesthetics, especially isoflurane,aminoglycosides, and antiarrhythmic

    These prevent the action of Ach at the skeletal muscle endplate

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    to produce a "surmountable blockade,"" effect is reversed bycholinesterase inhibitors (ex. neostigmine or pyridostigmine)"

    Nondepolarizing type antagonists

    Agent with long duration of action and is most likely to causehistamine release

    Tubocurarine

    Non-depolarizing skeletal muscle antagonist that has shortduration

    Mivacurium

    Skeletal muscle agent that can block muscarinic receptors Pancuronium

    Skeletal muscle agent that undergoes Hofmann elimination(breaks down spontaneously) Atracurium

    One depolarizing blocker that causes continuous depolarizationand results in muscle relaxation and paralysis, causes musclepain postoperatively and myoglobinuria may occur

    Succinylcholine

    During Phase I these agents worsen muscle paralysis bysuccinylcholine, but during phase II they reverse the blockadeproduced by succinylcholine

    Cholinesterase inhibitors

    Agents acting in the CNS or in the skeletal muscle, used toreduce abnormally elevated tone caused by neurologic ormuscle end plate disease

    Spasmolytic drugs

    Facilitates GABA presynaptic inhibition Diazepam

    GABA agonist in the spinal cord Baclofen

    Similar to clonidine and may cause hypotension Tizanidine

    DOC for malignant hyperthermia by acting on thesacroplasmic reticulum or skeletal muscle

    Dantrolene

    Agent used for acute muscle spasm Cyclobenzaprine

    Irreversible condition resulting from the use of antipsychotics,reserpine at high doses, and MPTP (by-product of illicitmeperidine analog)

    Drug induced Parkinsonism

    Agent used in drug therapy of Parkinson's instead ofDopamine which has low bioavailability and does not cross theBBB

    L-dopa

    This is combined with L-dopa, inhibits DOPA decarboxylase(active only peripherally) which allows lower effective dosesof L-dopa and allows for fewer SE's (GI distress, posturalhypotension, and dyskinesias)

    Carbidopa

    Clinical response that may fluctuate in tx of Parkinson's dx "On-off-phenomenon"" "

    Anti-Parkinson's drug which increases intraocular pressure andis contraindicated in closed angle glaucoma

    Levodopa

    Ergot alkaloid that is a partial agonist at D2 receptors in thebrain, used for patients who are refractory or cannot toleratelevodopa, causes erythromelalgia

    Bromocriptine

    Non ergot agents used as first-line therapy in the initialmanagement of Parkinson's

    Pramipexole and ropinirole

    Enhances dopaminergic neurotransmission SE's include CNSexcitation, acute toxic psychosis and livedo reticularis

    Amantadine

    Inhibitor of MAO type B which metabolizes dopamine, usedadjunct to levodopa or as sole agent in newly diagnosedpatients

    Selegiline

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    Inhibitors of catechol-O-methyltransferase (COMT), used asadjuncts in Parkinson's dx and cause acute hepatic failure(monitor LFT's)

    Entacapone and Tolcapone

    Agent decreases the excitatory actions of cholinergic neurons.May improve tremor and rigidity but have LITTLE effect onbradykinesia. Atropine-like side effects

    Benztropine

    Agent effective in physiologic and essential tremor Propranolol

    Agents used in Huntington's DiseaseTetrabenazine (amine depleting drug),Haloperidol (antipsychotic)

    Agents used in Tourette's dx Haloperidol or pimozide

    Chelating agent used in Wilson's disease Penicillamine

    Extrapyramidal dysfunction is more common with theseagents, which block this subtype of dopamine receptor

    Older antipsychotic agents, D2 receptors

    MOA of neuroleptics Dopamine blockade

    Side effects occuring in antipsychotics that block dopamineHyperprolactinemia, menorrhea, galactorrhea,confusion, mood changes, decreased sexualinterest, and weight gain

    Antipsychotics that reduce positive symptoms only Older antipsychoticsNewer atypical antipsychotics that also improve some of thenegative symptoms and help acute agitation

    Olanzapine, aripiprazole, and sertindole

    Antipsychotic used in the treatment of psychiatric symptoms inpatients with dementia

    Risperidone

    Atypical antipsychotic causing high prolactin levels Risperidone

    Newer atypical antipsychotic used for bipolar disorder, knownto cause weight gain, and adversely affect diabetes

    Olanzapine

    Agent more frequently associated with extrapyramidal sideeffects that can be treated with benzodiazepine,diphenhydramine or muscarinic blocker

    Haloperidol

    Drug used in neuroleptic malignant syndrome Dantrolene

    Agents may exacerbate tardive dyskinesias (may beirreversible and there is no treatment)

    Muscarinic blockers

    Antipsychotic having the strongest autonomic effects Thioridazine

    Antipsychotic having the weakest autonomic effects Haloperidol

    Only phenothiazine not exerting antiemetic effects, can causevisual impairment due to retinal deposits, and high doses havebeen associated with ventricular arrhythmias

    Thioridazine

    Agent having no effect on D2 receptors, blocks D4, reservedfor resistant schizophrenia, and can cause fatal agranulocytosis

    Clozapine

    Anti-psychotic not shown to cause tardive dyskinesia Clozapine

    Anti-psychotics available in depot preparation Fluphenazine and haloperidol

    Reduced seizure thresholdLow-potency typical antipsychotics andclozapine

    Orthostatic hypotension and QT prolongation Low potency phenothiazines and ziprasidone

    Increased risk of developing cataracts Quetiapine

    Major route of elimination for Lithium Kidneys

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    Patients being treated with lithium, who are dehydrated, ortaking diuretics concurrently, could develop

    Lithium toxicity

    Drug increases the renal clearance hence decreases levels oflithium

    Theophylline

    Lithium is associated with this congenital defectCardiac anomalies and is contraindicated inpregnancy or lactation

    DOC for bipolar affective disorder Lithium

    Concern using lithium Low therapeutic indexSE of lithium

    Tremor, sedation, ataxia, aphasia, thyroidenlargement, and reversible diabetes insipidus

    Example of three antidepressants that are indicated forobsessive compulsive disorder

    Clomipramine, fluoxetine and fluvoxamine

    Neurotransmitters affected by the action of antidepressants Norepinephrine and serotonin

    Usual time needed for full effect of antidepressant therapy 2 to 3 weeks

    Population group especially sensitive to side effects ofantidepressants

    Elderly patients

    All antidepressants have roughly the same efficacy in treatingdepression, agents are chosen based on these criterion Side-effect profile and prior pt response

    Well-tolerated and are first- line antidepressants SSRI's, bupropion, and venlafaxine

    Most useful in patients with significant anxiety, phobicfeatures, hypochondriasis, and resistant depression

    Monamine oxidase inhibitors

    Condition will result from in combination of MAOI withtyramine containing foods (ex. wine, cheese, and pickledmeats)

    Hypertensive crisis

    MAOI should not be administered with SSRI's or potent TCA'sdue to development of this condition

    Serotonin syndrome

    Sedation is a common side effect of these drugs, they lowerseizure threshold, uses include BAD, acute panic attacks,phobias, enuresis, and chronic pain and their overdose can bedeadly

    Tricyclic antidepressants (TCA)

    Three C's associated with TCA toxicityComa, Convulsions, Cardiac problems(arrhythmias and wide QRS)

    Agents having higher sedation and antimuscarinic effects thanother TCA's

    Tertiary amines

    TCA used in chronic pain, a hypnotic, and has markedantimuscarinic effects

    Amitriptyline

    TCA used in chronic pain, enuresis, and ADD ImipramineTCA with greatest sedation of this group, and markedantimuscarinic effects, used for sleep

    Doxepin

    TCA used in obsessive compulsive disorder (OCD), mostsignificant of TCA's for risk of seizure, weight gain, andneuropsychiatric signs and symptoms

    Clomipramine

    Secondary amines that have less sedation and more excitationeffect

    Nortriptyline, Desipramine

    Side effects seen with tricyclic antidepressantsMuscarinic blockade (dry mouth, constipation)weak alpha-1 block (orthostatic hypotension);

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    weak hisamine block (sedation)

    Antidepressant associated with neuroleptic malignantsyndrome

    Amoxapine

    Antidepressant associated with seizures and cardiotoxicity Maprotiline

    Antidepressant having stimulant effects similar to SSRI's andcan increase blood pressure

    Venlafaxine

    Antidepressant inhibiting norepinephrine, serotonin, anddopamine reuptake

    Venlafaxine

    Antidepressant also used for sleep that causes priapism Trazodone

    Antidepressant which is inhibitor of CYP450 enzymes andmay be associated with hepatic failure

    Nefazodone

    Heterocyclic antidepressants least likely to affect sexualperformance, used for management of nicotine withdrawal,SE's include dizziness, dry mouth, aggravation of psychosis,and seizures

    Bupropion

    Antidepressant with MOA as alpha 2 antagonist, has effects onboth 5-HT and NE, blocks histamine receptors, and is sedating

    Mirtazapine

    SE of mirtazapine Liver toxicity, increased serum cholesterolExcept for these agents all SSRI have significant inhibition ofCytP450 enzymes

    Citalopram and its metabolite escitalopram

    Side effects frequently seen with SSRIs CNS stimulation; GI upset

    Antidepressants with no effect on BP, no sedation SSRIs

    SSRI with long T1/2 and can be administered once weekly formaintenance, not acute tx

    Fluoxetine

    SSRI indicated for premenstrual dysphoric disorder Fluoxetine (Sarafem)

    Some of SSRIs' therapeutic effects beside depression

    Panic attacks, social phobias, bulimia nervosa,

    and PMDD (premenstrual dysphoric disorder),OCD

    SSRI less likely to cause a withdrawal syndrome Fluoxetine

    Inhibit synaptic activity of primary afferents and spinal cordpain transmission neurons

    Ascending pathways

    Activation of these receptors close Ca2+ ion channels to inhibitneurotransmitter release

    Presynaptic mu, delta, and kappa receptors

    Activation of these receptors open K+ ion channels to causemembrane hyperpolarization

    Postsynaptic Mu receptors

    Tolerance to all effects of opioid agonists can develop except Miosis and constipation

    All opioids except this agent (which has a muscarinic blockingaction) cause pupillary constriction

    Meperidine

    SE of these drugs include dependence, withdrawal syndrome,sedation, euphoria, respiratory depression nausea andvomiting, constipation, biliary spasm, increased ureteral andbladder tone, and reduction in uterine tone

    Opioid Analgesics

    Strong opioid agonistsMorphine, methadone, meperidine, andfentanyl

    Opioids used in anesthesia Morphine and fentanyl

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    Opioid used in the management of withdrawal states Methadone

    Opioid available trans-dermally Fentanyl

    Opioid that can be given PO, by epidural, and IV, which helpsto relieve the dyspnea of pulmonary edema

    Morphine

    Use of this opioid with MAOI can lead to hyperpyrexic coma,and with SSRI's can lead to serotonin syndrome

    Meperidine

    Moderate opioid agonists Codeine, hydrocodone, and oxycodone

    Weak opioid agonist, poor analgesic, its overdose can causesevere toxicity including respiratory depression, circulatorycollapse, pulmonary edema, and seizures

    Propoxyphene

    Partial opioid agonist, considered a strong analgesic, has along duration of action and is resistant to naloxone reversal

    Buprenorphine

    Opioid antagonist that is given IV and had short DOA Naloxone

    Opioid antagonist that is given orally in alcohol dependencyprograms

    Naltrexone

    These agents are used as antitussive Dextromethorphan, Codeine

    These agents are used as antidiarrheal Diphenoxylate, Loperamide

    Inhalant anesthetics NO, chloroform, and diethyl ether

    Toxic to the liver, kidney, lungs, bone marrow, peripheralnerves, and cause brain damage in animals, sudden death hasoccurred following inhalation

    Fluorocarbons and Industrial solvents

    Cause dizziness, tachycardia, hypotension, and flushing Organic nitrites

    Causes acne, premature closure of epiphyses, masculinizationin females, hepatic dysfunction, MI, and increases in libidoand aggression

    Steroids

    Readily detected markers that may assist in diagnosis of the

    cause of a drug overdose include

    Changes in heart rate, blood pressure,

    respiration, body temperature, sweating, bowelsigns, and pupillary responses

    Most commonly abused in health care professionalsHeroin, morphine, oxycodone, meperidine andfentanyl

    This route is associated with rapid tolerance and psychologicdependence

    IV administration

    Leads to respiratory depression progressing to coma and death Overdose of opioids

    Lacrimation, rhinorrhea, yawning, sweating, weakness,gooseflesh, nausea, and vomiting, tremor, muscle jerks, andhyperpnea are signs of this syndrome

    Abstinence syndrome

    Treatment for opioid addiction Methadone, followed by slow dose reductionThis agent may cause more severe, rapid and intensesymptoms to a recovering addict

    Naloxone

    Sedative-Hypnotics actionReduce inhibition, suppress anxiety, andproduce relaxation

    Additive effects when Sedative-Hypnotics used in combinationwith these agents

    CNS depressants

    Common mechanism by which overdose result in deathDepression of medullary and cardiovascularcenters

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    "Date rape drug" Flunitrazepam (rohypnol)

    The most important sign of withdrawal syndrome Excessive CNS stimulation (seizures)

    Treatment of withdrawal syndrome involvesLong-acting sedative-hypnotic or a gradualreduction of dose, clonidine or propranolol

    These agents are CNS depressants Ethanol, Barbiturates, and Benzodiazepines

    Withdrawal from this drug causes lethargy, irritability, andheadache

    Caffeine

    W/D from this drug causes anxiety and mental discomfort Nicotine

    Treatments available for nicotine addictionPatches, gum, nasal spray, psychotherapy, andbupropion

    Chronic high dose abuse of nicotine leads toPsychotic state, overdose causes agitation,restlessness, tachycardia, hyperthermia,hyperreflexia, and seizures

    Tolerance is marked and abstinence syndrome occurs Amphetamines

    Amphetamine agents Dextroamphetamines and methamphetamine

    These agents are congeners of Amphetamine DOM, STP, MDA, and MDMA "ecstasy"" "

    Overdoses of this agent with powerful vasoconstrictive actionmay result in fatalities from arrhythmias, seizures, respiratorydepression, or severe HTN (MI and stroke)

    Cocaine "super-speed"""

    Most dangerous of the currently popular hallucinogenic drugs,OD leads to nystagmus, marked hypertension, and seizures,presence of both horizontal and vertical nystagmus ispathognomonic

    PCP

    Removal of PCP may be aidedUrinary acidification and activated charcoal orcontinual nasogastric suction

    THC is active ingredient, SE's include impairment ofjudgment, and reflexes, decreases in blood pressure and

    psychomotor performance occur

    Marijuana

    This agent has greater affinity for muscarinic receptors andused for postoperative and neurogenic ileus and urinaryretention

    Bethanechol

    Only direct acting agent that is very lipid soluble and used inglaucoma

    Pilocarpine

    This agent used to treat dry mouth in Sjgren's syndrome Cevimeline

    Indirect-Acting ACh Agonist, alcohol, short DOA and used indiagnosis of myasthenia gravis

    Edrophonium

    Carbamate with intermediate action, used for+A1170postoperative and neurogenic ileus and urinary retention Neostigmine

    Treatment of atropine overdose and glaucoma (because lipidsoluable). Enters the CNS rapidly and has a stimulant effect,which may lead to convulsions

    Physostigmine

    Treatment of myasthenia gravis Pyridostigmine

    Antiglaucoma organophosphate Echothiophate

    Associated with an increased incidence of cataracts in patientstreated for glaucoma

    Long acting cholinesterase inhibitors

    Scabicide organophosphate Malathion

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    Organophosphate anthelmintic agent with long DOA Metrifonate

    Toxicity of organophosphate:

    DUMBELSS (diarrhea, urination, miosis,bronchoconstriction, excitation of skeletalmuscle and CNS, lacrimation, salivation, andsweating)

    The most frequent cause of acute deaths in cholinesteraseinhibitor toxicity

    Respiratory failure

    The most toxic organophosphate Parathion

    Treatment of choice for organophosphate overdose Atropine

    This agent regenerates active cholinesterase and is a chemicalantagonist used to treat organophosphate exposure

    Pralidoxime

    Prototypical drug is atropine Nonselective Muscarinic Antagonists

    Treat manifestations of Parkinson's disease and EPS Benztropine, trihexyphenidyl

    Treatment of motion sickness Scopolamine, meclizine

    Produce mydriasis and cycloplegia Atropine, homatropine,C1208 tropicamide

    Bronchodilation in asthma and COPD Ipratropium

    Reduce transient hyper GI motility Dicyclomine, methscopolamineCystitis, postoperative bladder spasms, or incontinence Oxybutynin, dicyclomine

    Toxicity of anticholinergicsblock SLUD (salivation, lacrimation, urination,defecation

    Another pneumonic for anticholinergic toxicity"dry as a bone, red as a beet, mad as a hatter,hot as a hare, blind as a bat"

    Atropine fever is the most dangerous effect and can be lethalin this population group

    Infants

    Contraindications to use of atropineInfants, closed angle glaucoma, prostatichypertrophy

    Limiting adverse effect of ganglion blockade that patientsusually are unable to tolerate

    Severe hypertension

    Reversal of blockade by neuromuscular blockers Cholinesterase inhibitors

    Tubocurarine is the prototype, pancuronium, atracurium,vecuronium are newer short acting agent, produce competitiveblock at end plate nicotinic receptor, causing flaccid paralysis

    Nondepolarizing Neuromuscular Blockers

    Only member of depolarizing neuromuscular blocker, causesfasciculation during induction and muscle pain after use; hasshort duration of action

    Succinylcholine

    Chemical antagonists that bind to the inhibitor of ACh Estraceand displace the enzyme (if aging has not occurred) Cholinesterase regenerators, pralidoxime

    Used to treat patients exposed to insecticides such as parathion Pralidoxime, atropine

    Pneumonic for beta receptors You have 1 heart (Beta 1) and 2 lungs (Beta 2)

    This is the drug of choice for anaphylactic shock Epinephrine

    Phenylisopropylamines that are used legitimately and abusedfor narcolepsy, attention deficit disorder, and weight reduction

    Amphetamines

    Alpha agonist used to produce mydriasis and reduceconjunctival itching and congestion caused by irritation orallergy, it does not cause cycloplegia

    Phenylephrine

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    Newer alpha 2 agonist (apraclonidine and brimonidine) treatglaucoma by acting to

    Reduce aqueous secretion

    Short acting Beta 2 agonists that is drug of choice in treatmentof acute asthma but not recommended for prophylaxis

    Albuterol

    Longer acting Beta 2 agonist is recommended for prophylaxisof asthma

    Salmeterol

    These agents increase cardiac output and may be beneficial intreatment of acute heart failure and some types of shock

    Beta1 agonists

    These agents decrease blood flow or increase blood pressure,are local decongestants, and used in therapy of spinal shock(temporary maintenance of blood pressure which may helpmaintain perfusion

    Alpha1 agonists

    Shock due to septicemia or myocardial infarction is madeworse by

    Increasing afterload and tissue perfusiondeclines

    Epinephrine is often mixed with a local anesthetic to Reduce the loss from area of injection

    Chronic orthostatic hypotension can be treated with Midodrine

    Beta 2 agonist used to suppress premature labor, but cardiac

    stimulatory effects may be hazardous to mother and fetus

    Terbutaline

    Sympathetic agent which stimulates heart rate and can dilatevessels in skeletal muscle at low doses

    Epinephrine

    Mast cells to reduce release of hisamine and inflammatorymediators

    Epinephrine

    Agent used in shock because it dilates coronary arteries andincreases renal blood flow

    Dopamine

    Agent which stimulates cardiac contractile force more than ratewith little effect on total peripheral resistance

    Dobutamine

    Long acting sympathomimetic, sometimes used to improve

    urinary continence in children and elderly with enuresis EphedrineAlpha 1 agonist toxicity Hypertension

    Beta 1 agonist toxicity Sinus tachycardia and serious arrhythmias

    Beta 2 agonist toxicity Skeletal muscle tremor, tachycardia

    The selective agents loose their selectivity at high doses

    Nonselective alpha-blocking drug, long acting and irreversible,and used to treat pheochromocytoma. Blocks 5-HT, sooccasionaly used for carcinoid tumor. Blocks H1 and used inmastocytosis

    Phenoxybenzamine

    Nonselective alpha-blocking drug, short acting and reversible,used for rebound HTN from rapid clonidine withdrawal, andRaynaud's phenomena

    Phentolamine

    Selective Alpha 1 blocker used for hypertension, BPH, maycause first dose orthostatic hypotension

    Prazosin, terazosin, doxazosin

    Selective Alpha-1A blocker, used for BPH, but with littleeffect on HTN

    Tamsulosin

    Selective Alpha 2 blocker used for impotence (controversialeffectiveness)

    Yohimbine

    SelectiveB1 Receptor blockers that may be useful in treating

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    patients even though they have asthmaAcebutolol, atenolol, esmolol, metoprolol

    Combined alpha and beta blocking agents that may haveapplication in treatment of CHF

    Labetalol and carvedilol

    Beta blockers partial agonist activity (intrinsicsympathomimetic activity) cause some bronchodilation andmay have an advantage in treating patients with asthma

    Pindolol and acebutolol

    This beta blocker lacks local anesthetic activity (a property

    which decreases protective reflexes and increases the risk ofcorneal ulceration) and used in treating glaucoma Timolol

    This parenteral beta blocker is a short acting (minutes) Esmolol

    This beta blocker is the longest acting Nadolol

    These beta blockers are less lipid soluble Acebutolol and atenolol

    This beta blocker is highly lipid soluble and may account forside effects such as nightmares

    Propranolol

    Clinical uses of these agents include treatment of HTN, angina,arrhythmias, chronic CHF, and selected post MI patients

    Beta blockers

    Toxicity of these agents include bradycardia, AV blockade,exacerbation of acute CHF; signs of hypoglycemia may bemasked (tachycardia, tremor, and anxiety)

    Beta blockers

    Cholinomimetics that increase outflow, open trabecularmeshwork, and cause ciliary muscle contraction

    Pilocarpine, carbachol, physostigmine

    Nonselective alpha agonists that increases outflow, probablyvia the uveoscleral veins

    Epinephrine, dipivefrin

    Selective alpha agonists that decreases aqueous secretion Apraclonidine, brimonidine

    These Beta blockers decrease aqueous secretion Timolol (nonselective), betaxolol (selective)

    This diuretic decreases aqueous secretion due to lack of

    HCO3- ion. Causes drowsiness and paresthesias, alkalinizationof the urine may precipitate calcium salts, hypokalemia,acidosis

    Acetazolamide

    This agent cause increased aqueous outflow Prostaglandin PGF2a

    Inhibit angiotensin-converting enzyme (ACE) ACE inhibitors

    Captopril and enalapril (-OPRIL ending) are ACE inhibitors

    SE of ACE inhibitors Dry cough, hyperkalemia

    ACE inhibitors are contraindicated in pregnancy and with K+

    Losartan and valsartan block Angiotensin receptor

    Angiotensin receptor blockers do NOT cause Dry coughAgents that block L-type calcium channel Calcium channel blockers

    CCB contraindicated in CHF Verapamil

    CCB with predominate effect on arteriole dilation Nifedipine

    SE of CCB Constipation, edema, and headache

    Agents that reduce heart rate, contractility, and O2 demand Beta-blockers

    B-blockers that are more cardioselective Beta-1 selective blockers

    Cardioselective Beta 1-blockers Atenolol, acebutolol, and metoprolol

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    Beta-blockers should be used cautiously inAsthma (bronchospastic effects), diabetes(block signs of hypoglycemia) and peripheralvascular disease

    Non-selective Beta-blocker also used for migraine prophylaxis Propranolol

    SE of beta blockersBradycardia, SEXUAL DYSFUNCTION,decrease in HDL, and increase in Triglycerols(TG)

    Alpha 1selective blockers

    Prazosin, terazosin and doxazosin (-AZOSIN

    ending)Non-selective Alpha1blockers use to treat pheochromocytoma Phenoxybenzamine

    For rebound HTN from rapid clonidine withdrawal Phentolamine

    A1a-selective blocker with no effects on HTN used for BPH Tamsulosin (Flomax)

    SE of alpha blockersOrthostatic hypotension (especially with firstdose) and reflex tachycardia

    Presynaptic Alpha 2 agonist used in HTN, and acts centrally Clonidine, and methyldopa

    SE of methyldopa Positive Coomb's test, depression

    Methyldopa is contraindicated in Geriatrics due to its CNS (depression) effects

    SE of clonidine Rebound HTN, sedation, dry mouth

    Direct vasodilator of arteriolar smooth muscle Hydralazine

    SE of hydralazine Lupus-like syndrome

    Arterial vasodilator that works by opening K+ channels Minoxidil

    SE of minoxidil Hypertrichosis

    IV Drug used Hypertensive Crisis Nitroprusside

    Nitroprusside vasodilates Arteries and veins

    Toxicity caused by nitroprusside and treatmentCyanide toxicity treated with sodium

    thiosulfateCarbonic anhydrase inhibitor Acetazolamide

    Diuretic used for mountain sickness and glaucoma Acetazolamide

    SE of acetazolamide

    Paresthesias, alkalization of the urine (whichmay ppt. Ca salts), hypokalemia, acidosis, andencephalopathy in patients with hepaticimpairment

    MOA of loop diuretics inhibits Na+/K+/2Cl- cotransport

    Site of action of loop diuretics Thick ascending limb

    SE of loop (furosemide) diuretics Hyperuricemia, hypokalemia and ototoxicity

    Aminoglycosides used with loop diuretics potentiate adverseeffect

    Ototoxicity

    Loops lose and thiazide diuretics retain Calcium

    MOA of thiazide diuretics Inhibit Na+/Cl- cotransport

    Site of action of thiazide diuretics Work at early distal convoluted tubule

    Class of drugs that may cause cross-sensitivity with thiazidediuretics

    Sulfonamides

    SE of thiazide (HCTZ) diureticsHyperuricemia, hypokalemia andhyperglycemia

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    Potassium sparing diuretics inhibit Na+/K+ exchange

    Diuretic used to treat primary aldosteronism Spironolactone

    SE of spironolactone Gynecomastia hyperkalemia, and impotence

    Osmotic diuretic used to treat increased intracranial pressure Mannitol

    ADH agonist used for pituitary diabetes insipidus Desmopressin (DDAVP)

    Used for SIADH Demeclocycline

    SE of demeclocyclineBone marrow and teeth discoloration forchildren under 8 years of age

    MOA of class I A (eg. Procainamide), class IB (eg.Lidocaine), and class IC (eg. Flecainide) antiarrhythmics

    Sodium channel blockers

    SE of procainamide Lupus-like syndrome

    Limiting side effect of Quinidine Prolongs QT interval

    Other side effects of QuinidineThrombocytopenic purpura, andCINCHONISM

    Major drug interaction with Quinidine Increases concentration of Digoxin

    DOC for management of acute ventricular arrhythmias Amiodarone

    DOC for digoxin induced arrhythmias Phenytoin

    Class of anti-arrhythmics that has a pro-arrhythmic effect(CAST trial), therefore are used as last line agents

    Class IC (flecainide, propafenone, moricizine)

    Class II antiarrhythmics are B-blockers

    Antiarrhythmic that exhibits Class II and III properties Sotalol

    Side effect of sotalol prolongs QT and PR interval

    Used intravenously for acute arrhythmias during surgery Esmolol

    Anti-arrhythmics that decrease mortality B-blockers

    MOA of class III antiarrhythmics Potassium channel blockers

    Class III antiarrhythmic that exhibits properties of all 4 classes Amiodarone

    Specific pharmacokinetic characteristic of amiodarone Prolonged half-life, up to six weeks

    Antiarrhythmic effective in most types of arrhythmia Amiodarone

    SE of AmiodaroneCardiac dysfunction, photosensitivity, skin(blue smurf syndrome), Pulmonary fibrosis,thyroid and corneal deposits

    MOA of class IV antiarrhythmics Calcium channel blockers

    Life threatening cardiac event that prolong QT leads to Torsades de pointes

    Agent to treat torsades de pointes Magnesium sulfate

    Drug used supraventricular arrhythmias Digoxin

    DOC for paroxysmal supraventricular tachycardia (PSVT) Adenosine

    Adenosine's MOAActivattion on an inward K+ current andinhibition of Ca++ current resulting in markedhyperpolarization

    Anti-arrhythmic with 15 second duration of action Adenosine

    MOA of sildenafil (Viagra)Inhibits phosphodiesterase-5, enhancing effectsof nitric oxide-activated increases in cGMP

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    Drugs used in the management of angina Aspirin, Nitrates, CCB, and Beta blockers

    Aspirin reduces mortality in unstable angina by Platelet aggregation inhibition

    MOA of nitratesRelax vascular smooth muscle, at low dosesdilate veins and at high doses dilate arterioles

    Nitrate used for acute anginal attacks Nitroglycerin sublingual tablets

    Nitrate used to prevent further attacks Oral and transdermal forms of nitroglycerin

    Nitrate free intervals are needed due to Tolerance

    SE of nitratesPostural hypotension, reflex tachycardia, hotflashes, and throbbing headache due tomeningeal artery dilation

    CCB are DOC for Prinzmetal's angina

    Beta blockers are used for which type of anginal attack Classic

    MOA of Cardiac glycosides (eg. digoxin)Indirectly increase intracellular calcium andcardiac contractility by inhibiting Na+/K+ATPase

    Digoxin is used in Atrial fibrillation and CHF

    Digoxin toxicity can be precipitated by Hypokalemia

    Antidote for digoxin toxicity Digibind

    Phosphodiesterase inhibitors that increase mortality and havebeen found to have NO beneficial effects

    Amrinone and milrinone

    SE of amrinone Thrombocytopenia

    Beta 1 agonists used in acute CHF Dobutamine and dopamine

    Diuretics work in CHF by Reducing preload

    Beta blockers work in CHF byReducing progression of heart failure (neveruse in acute heart failure)

    Peptide drug used to treat CHF Nesiritide (BNP)MOA of nesiritide

    Increasing sodium excretion and decreasesarterial and venous tone

    SE of nesiritide Excessive hypotension and kidney failure

    Agent used in CHF that is a selective alpha and nonselectivebeta blocker

    Carvedilol

    Agent used in acutely decompensated CHF resemblingnatriuretic peptide

    Nesiritide (Natrecor)

    Vitamin K dependent anticoagulant Warfarin (PT)

    Warfarin is contraindicated in Pregnancy

    Anticoagulant of choice in pregnancy Heparin

    Heparin (PTT) increases activity of Antithrombin 3

    Route of administration of warfarin Oral

    Routes of administration of heparin IV and IM (only LMW)

    SE of both warfarin and heparin Bleeding

    SE of heparin Heparin induced thrombocytopenia (HIT)

    Alternative anticoagulant used if HIT develops Lepirudin

    Antidote to reverse actions of warfarin Vitamin K or fresh frozen plasma

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    Antidote to reverse actions of heparin Protamine sulfate

    MOA of aspirin Irreversibly blocking cyclooxygenase

    Agent used to treat MI and to reduce incidence of subsequentMI

    Aspirin, metoprolol

    SE of Aspirin GI bleeding

    Antiplatelet drug reserved for patients allergic to aspirin Ticlopidine

    SE for ticlopidine Neutropenia and agranulocytosis

    Effective in preventing TIA's Clopidogrel and ticlopidinePrevents thrombosis in patients with artificial heart valve Dipyridamole

    Block glycoprotein IIb/IIIa involved in platelet cross-linking Abciximab, tirofiban and eptifibatide

    MOA of thrombolyticsDegradation of fibrin clots and areadministered IV

    Thrombolytics are used for Pulmonary embolism and DVT

    Thrombolytic that can cause allergic reaction Streptokinase

    Thrombolytic used for acute MI and ischemic (nonhemorrhagic) CVA

    Tissue plasmin activator

    SE of tPA Cerebral hemorrhageAntidote for thrombolytics Aminocaproic acid

    Agent to treat hypochromic microcytic anemias Ferrous sulfate

    Chelating agent used in acute iron toxicity Deferoxamine

    Agent for pernicious anemia Cyanocobalamin (Vit B12)

    Agent used for neurological deficits in megaloblastic anemia Vitamin B12

    Agent used for megaloblastic anemia (but does NOT reverseneurologic symptoms) and decrease neural tube defects duringpregnancy

    Folic acid

    Agent used for anemias associated with renal failure Erythropoietin

    Agent used neutropenia especially after chemotherapyG-CSF (filgrastim) and GM-CSF(sargramostim)

    Treatment of patients with prior episodes of thrombocytopeniaafter a cycle of cancer chemotherapy

    Interleukin 11 (oprelvekin)

    Drugs decrease intestinal absorption of cholesterol Bile acid-binding resins

    Cholestyramine and colestipol are Bile acid-binding resins

    Major nutritional side effect of bile acid-binding resinsImpair absorption of fat soluble vitaminabsorption (A,D,E,K)

    MOA of lovastatin (STATIN) inhibits HMG COA reductaseHMG CoA reductase inhibitors are contraindicated in Pregnancy

    MOA of drug or foods (grapefruit juice) that increase statineffect

    Inhibit Cytochrome P450 3A4

    SE of HMG COA reductase inhibitors Rhabdomyolysis and Hepatotoxicity

    Monitoring parameter to obtain before initiation of STATINS LFT's

    Decreases liver triglycerol synthesis Niacin

    SE of niacin Cutaneous flush

    Cutaneous flush and be reduced by pretreatment with Aspirin

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    Fibrates (gemfibrozil) increase activity of Lipoprotein lipase

    Most common SE of fibrates Nausea

    Fibrates are contraindicated in Pregnancy

    Concurrent use of fibrates and statins increases risk of Rhabdomyolysis

    New class of drugs that works by inhibiting absorption ofintestinal cholesterol and can be given concurrently with theStatins

    Ezetimibe (Zetia)

    MOA of NSAIDS inhibit prostaglandin synthesis by inhibitingcyclo-oxygenase (cox)

    Difference between aspirin and other NSAIDS Aspirin irreversibly inhibits cyclooxygenase

    Four main actions of NSAIDSAnti-inflammatory, analgesia, antipyretic andantiplatelet activity

    Agent used for closure of patent ductus arteriosus Indomethacin

    Aspirin is contraindicated in children with viral infection Potential for development of Reye's syndrome

    SE of salicylates Tinnitus, GI bleeding

    NSAID also available as an ophthalmic preparation Diclofenac, ketoralac

    NSAID available orally, IM and ophthalmically KetoralacNSAID that is used for acute condition, such as pre-opanesthesia and has limited duration (

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    NSAID used in gout Indomethacin

    NSAID contraindicated in gout Aspirin

    MOA of colchicine (used in acute gout) Selective inhibitor of microtubule assembly

    SE of colchicine Kidney and liver toxicity, diarrhea

    Agent used to treat chronic gout by increasing uric acidsecretion and excretion

    Probenecid and sulfinpyrazone

    Allopurinol treats chronic gout by decreasing uric acid

    production by inhibitingXanthine oxidase

    Rapid acting insulins that do not self-aggregate lispro insulin, aspart insulin, glulisine insulin

    Peakless ling acting insulin Insulin glargine

    DOC for paroxysmal supraventricular tachycardia; has highefficacy and short duration of action

    Adenosine

    Insulin bound to neutral protamine NPH (NP = neutral protamine)

    Insulin that self-aggregates into hexamers insulin glargine

    Side effect of quinidine characterised by tinnitus, headache,deafness, and (occasionally) anaphylactoid shock

    Cinchonism

    This antibiotic can be used to treat Paget's disease of bone aswell as hypercalcemia plicamycin