Question Answer Time it takes for amount of drug to fall to half of its value; this Half-life (T1/2) is a constant

in first order kinetics (majority of drugs) Relates the amount of drug in the body to the plasma concentration Volume of distribution (VD) Cp Clearance (CL) First pass effect Bioavailability (F) Plasma concentration of a drug at a given time The ratio of the rate of elimination of a drug to its plasma concentration The elimination of drug that occurs before it reaches the systemic circulation The fraction of administered dose of a drug that reaches systemic circulation

When the rate of drug input equals the rate of drug elimination Steady state This step of metabolism makes a drug more hydrophilic and Phase I hence augments elimination Different steps of Phase I Inducers of Cytochrome P450 (CYP450) Inhibitors of CYP450 Products of Phase II conjugation Type of kinetics when a constant percentage of substrate is metabolized per unit time Drug elimination with a constant amount metabolized regardless of drug concentration Target plasma concentration times (volume of distribution divided by bioavailability) Concentration in the plasma times (clearance divided by bioavailability) Strength of interaction between drug and its receptor Selectivity of a drug for its receptor Amount of drug necessary to elicit a biologic effect; refers to the drug's strength Maximum response achieveable from a drug Ability of a drug to produce 100% of the maximum response regardless of the potency Ability to produce less than 100% of the response Ability to bind reversibly to the same site as the drug and without activating the effector system A hormone whose mechanism of action (MOA) utilizes intracellular receptors

Oxidation, reduction, hydrolysis

Barbiturates, phenytoin, carbamazepine, and rifampin Cimetidine, ketoconazole, erythromycin, isoniazid and grapefruit Glucuronate, acetic acid, and glutathione sulfate First order kinetics Zero order kinetics Loading dose (Cp*(Vd/F)) Maintenance dose (Cp*(CL/F)) Affinity Specificity Potency Efficacy Full agonist Partial agonist Competitive antagonist

Class of drugs with ability to decrease the maximal response to Noncompetitive antagonist an agonist Thyroid and steroid hormones

A hormone whose MOA utilizes transmembrane receptors Class of drugs whose MOA utilizes ligand gated ion channels Median effective dose required for an effect in 50% of the population Median toxic dose required for a toxic effect in 50% of the population Dose which is lethal to 50% of the population Window between therapeutic effect and toxic effect Term for a high margin of safety Term for a narrow margin of safety Antidote used for lead poisoning Antidote used for cyanide poisoning Antidote used for anticholinergic poisoning Antidote used for organophosphate/anticholinesterase poisoning

Insulin Benzodiazepines and calcium channel blockers ED50 TD50 LD50 Therapeutic index High therapeutic index Low therapeutic index Dimercaprol, EDTA Nitrites Physostigmine Atropine, pralidoxime (2-PAM) Deferoxamine N-acetylcysteine (Mucomyst) Dimercaprol Penicillamine Protamine Vitamin K and Fresh frozen plasma (FFP) Aminocaproic acid Ethanol or fomepizole Naloxone (IV), naltrexone (PO) Flumazenil Sodium bicarbonate 100% O2 and hyperbaric O2

Antidote used for iron salt toxicity Antidote used for acetaminophen (APAP) toxicity Antidote for arsenic, mercury, lead, and gold poisoning Antidote used in poisonings: copper (Wilson's disease), lead, mercury, and arsenic

Antidote used for heparin overdose Antidote used for warfarin toxicity Antidote for tissue plasminogen activator (t-PA), streptokinase Antidote used for methanol and ethylene glycol Antidote used for opioid toxicity Antidote used for benzodiazepine toxicity Antidote used for tricyclic antidepressants (TCA) Antidote used for carbon monoxide poisoning Antidote used for digitalis toxicity Antidote used for beta agonist toxicity (eg. Metaproterenol) Antidote for methotrexate toxicity Antidote for beta-blockers and hypoglycemia Antidote useful for some drug induced Torsade de pointes Antidote for hyperkalemia Antidote for salicylate intoxication Constant proportion of cell population killed rather than a constant number Toxic effect of anticancer drug can be lessened by rescue agents

Digibind (also need to d/c digoxin, normalize K+, and lidocaine if pt. Is arrhythmic) Esmolol Leucovorin Glucagon Magnesium sulfate sodium polystyrene sulfonate (Kayexalate) Alkalinize urine, dialysis Log-kill hypothesis Pulse therapy Rescue therapy

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

Drug used concurrently with toxic anticancer agents to reduce renal precipitation of urates Pyrimidine analog that causes "Thymine-less death"" given with leucovorin rescue" Drug used in cancer therapy causes Cushing-like symptoms Side effect of Mitomycin MOA of cisplatin Common toxicities of cisplatin Analog of hypoxanthine, needs HGPRTase for activation Interaction with this drug requires dose reduction of 6-MP May protect against doxorubicin toxicity by scavenging free radicals

Allopurinol 5-flouracil (5-FU) Prednisone SEVERE myelosuppression Alkylating agent Nephro and ototoxicity 6-mercaptopurine (6-MP) Allopurinol Dexrazoxane Bleomycin Testicular cancer Adriamycin (doxorubicin) +bleomycin, vinblastine +dacarbazine

Blows DNA (breaks DNA strands), limiting SE is pulmonary fibrosis ABVD regimen used for HD, but appears less likely to cause sterility and secondary malignancies than MOPP Regimen used for non-Hodgkin's lymphoma Regimen used for breast cancer Alkylating agent, vesicant that causes tissue damage with extravasation

Bleomycin+vinblastine+etoposide+cisplatin produce almost a 100% response when all agents are used for this neoplasm

CHOP (cyclophosphamide, doxorubicin, vincristine, and prednisone) plus rituximab

CMF (cyclophosphamide, methotrexate, and fluorouracil) and tamoxifen if ER+ Mechlorethamine Cyclophosphamide Hydration and mercaptoethanesulfonate (MESNA) Vincristine

Anticancer drug also used in RA, produces acrolein in urine that leads to hemorrhagic cystitis Prevention of cyclophosphamide induced hemorrhagic cystitis Microtubule inhibitor that causes peripheral neuropathy, foot drop (eg. ataxia), and "pins and needles"" sensation"

Interact with microtubules (but unlike vinca which prevent disassembly of tubules), it stabilizes tubulin and cells remain Paclitaxel (taxol) frozen in metaphase Toxicities include nephrotoxicity and ototoxicity, leading to a Cisplatin severe interaction with aminoglycosides Agent similar to cisplatin, less nephrotoxic, but greater myelosuppression Carboplatin L-asparaginase Interferon alpha Flutamide (Eulexin) Tamoxifen Letrozole, anastrozole Toremifene (Fareston) Converts asparagine to aspartate and ammonia, denies cancer cells of essential AA (asparagine) Used for hairy cell leukemia; it stimulates NK cells Anti-androgen used for prostate cancer Anti-estrogen used for estrogen receptor + breast cancer Aromatase inhibitor used in breast cancer Newer estrogen receptor antagonist used in advanced breast cancer

Some cell cycle specific anti-cancer drugs Some cell cycle non-specific drugs Anti-emetics used in association with anti-cancer drugs that are 5-HT3 (serotonin receptor subtype ) antagonists Nitrosoureas with high lipophilicity, used for brain tumors Produces disulfiram-like reaction with ethanol Somatostatin (SRIF) analog used for acromegaly, carcinoid, glucagonoma and other GH producing pituitary tumors

Bleomycin, vinca alkaloids, antimetabolites (eg., 5-FU, 6-MP, methotrexate, etoposide) Alkylating agents (eg., mechlorethamine, cyclophosphamide), antibiotics (doxorubicin, daunorubicin), cisplatin, nitrosourea Odansetron, granisetron Carmustine (BCNU) and lomustine (CCNU) Procarbazine Octreotide Somatrem Sermorelin Leuprolide Ganirelix

Somatotropin (GH) analog used in GH deficiency (dwarfism) GHRH analog used as diagnostic agent GnRH agonist used for infertility or different types of CA depending on pulsatile or steady usage respectively GnRH antagonist with more immediate effects, used for infertility

Dopamine (DA) agonist (for Parkinson's disease), used also for Bromocriptine hyperprolactinemia Hormone inhibiting prolactin release Dopamine ACTH analog used for diagnosis of patients with corticosteroid Cosyntropin abnormality SE of OCs Most widely used thyroid drugs such as Synthroid and Levoxyl contain T3 compound less widely used Anti-thyroid drugs

Synthetic analog of ADH hormone used for diabetes insipidus Desmopressin (DDAVP) and nocturnal enuresis L-thyroxine (T4) Cytomel

Increased thromboembolic events

Thioamide agents used in hyperthyroidism Thioamide less likely to cross placenta, inhibits peripheral conversion of T4 to T3 in high doses, and should be used with PTU extreme caution in pregnancy Inhibits thyroid hormone synthesis by blocking PTU (propylthiouracil) MOA iodination of the tyrosine residues of thyroglobulin Can be effective for short term therapy of thyroid storm, but after several weeks of therapy causes an exacerbation of Iodide salts hyperthyroidism Dose may need to be increased during pregnancy or with Ocs Thyroxine due to increased TBG in plasma Permanently cures thyrotoxicosis, patients will need thyroid replacement therapy thereafter. Contraindicated in pregnancy Radioactive iodine Ipodate Radio contrast media that inhibits the conversion of T4 to T3

Thioamides, iodides, radioactive iodine, and ipodate Methimazole and propylthiouracil (PTU)

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

Beta-blockers such as propranolol

Vitamins containing iron should NOT be taken simultaneously Iron deiodinates thyroxine with levothyroxine because Thyroxine dose may need to be increased in hypothyroid patient during pregnancy because 3 zones of adrenal cortex and their products Pneumonic for 3 zones of adrenal cortex Used for Addison's disease, Congenital Adrenal Hyperplasia (CAH), inflammation, allergies, and asthma (as a local inhalation) Short acting glucocorticoids Intermediate acting glucocorticoids Long acting glucocorticoids Mineralocorticoids Some side effects of corticosteroids Estogens increase maternal TBG Glomerulosa (mineralocorticoids), fasciculata (glucocorticoid=GC), and reticularis (adrenal androgens) GFR Glucocorticoids Cortisone and hydrocortisone (equivalent to cortisol)

Period of time of therapy after which GC therapy will need to 5-7 days be tapered Used for Cushing's syndrome (increased corticosteroid) Inhibits conversion of cholesterol to pregnenolone therefore inhibiting corticosteroid synthesis

Prednisone, methylprednisolone, prednisolone, and triamcinolone Betamethasone and dexamethasone Fludrocortisone and deoxycorticosterone Osteopenia, impaired wound healing, inc. risk of infection, inc. appetite, HTN, edema, PUD, euphoria, psychosis, stria, thinning of skin Dexamethasone suppression test Aminoglutethimide

Antifungal agent used for inhibition of all gonadal and adrenal Ketoconazole steroids Antiprogestin used as potent antagonist of GC receptor Diuretic used to antagonize aldosterone receptors Common SE of spironolactone Slightly increased risk of breast cancer, endometrial cancer, heart disease (questionable), has beneficial effects on bone loss Antiestrogen drugs used for fertility and breast cancer respectively

Mifepristone Spironolactone Gynecomastia and hyperkalemia Estrogen Clomiphene and tamoxifen Hot flashes Raloxifene Diethylstilbestrol (DES) Ethinyl estradiol and mestranol Mifepristone (RU-486)

Common SE of tamoxifen and raloxifene Selective estrogen receptor modulator (SERM) used for prevention of osteoporosis and prophylaxis in women with risk factors for breast cancer Non-steroidal estrogen agonist causes clear cell adenocarcinoma of the vagina in daughters of women who used it during pregnancy Estrogen mostly used in oral contraceptives (OC) Anti-progesterone used as abortifacient

Constant low dose of estrogen and increasing dose of progestin Combination oral contraceptives (OC) for 21 days (last 5 days are sugar pills or iron prep) Oral contraceptive available in a transdermal patch Converted to more active form DHT by 5 alpha-reductase 5 alpha-reductase inhibitor used for benign prostatic hyperplasia (BPH) and male pattern baldness Ortho-Evra Testosterone

Finasteride (Proscar and Propecia respectively) Nandrolone, oxymetholone, and oxandrolone Cyproterone acetate Leuprolide Glucagon Insulin Islets of Langerhans Somatostatin C-peptide Little C-peptide Normal C-peptide Lispro (Humalog), aspart, glulisine Regular (Humulin R) Ultralente (humulin U) Glargine (Lantus), detemir Hypoglycemia GLUT 2 GLUT 4 Acarbose, miglitol Act on intestine, delay digestion and absorption of glucose formed from digestion of starch and disacchrides

Anabolic steroid that has potential for abuse Anti-androgen used for hirsutism in females Drug is used with testosterone for male fertility What do alpha cells in the pancreas produce? What do beta cells in the pancreas produce? Where are beta cells found in the pancreas? What do delta cells in the pancreas produce? Product of proinsulin cleavage used to assess insulin abuse Exogenous insulin contains Endogenous insulin contains Very rapid acting insulin, having fastest onset and shortest duration of action Rapid acting, crystalline zinc insulin used to reverse acute hyperglycemia Long acting insulin Ultra long acting insulin, has over a day duration of action Major SE of insulin Important in synthesis of glucose to glycogen in the liver Important in muscle and adipose tissue for glucose transport across muscles and TG storage by lipoprotein lipase activation Examples of alpha-glucosidase inhibitors (AGI) MOA of AGI's SE of AGI's

Flatulence (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 Biguanide Drugs available in combination with metformin MOA of metformin Vascular effects of metformin Most important potential SE of metformin

Insulin secretagogue - closes ATP-sensitive K+ channel Metformin Glyburide, glipizide, and rosiglitazone Decreases hepatic glucose production and intestinal glucose absorption; increase insulin sensitivity Decreased micro and macro vascular disease Lactic acidosis

Incidence of hyoglycemia with metformin Meglitinide class of drugs MOA of repaglinide First generation sulfonylurea Second generation sulfonylurea MOA of both generations Common SE of sulfonylureas, repaglinide, and nateglinide Sulfonylurea NOT recommended for elderly because of very long half life Thiazolidinediones Reason troglitazone was withdrawn from market MOA of thiazolindinediones SE of Thiazolindinediones Hyperglycemic agent that increases cAMP and results in glycogenolysis, gluconeogenesis, reverses hypoglycemia, also used to reverse severe beta-blocker overdose and smooth muscle relaxation Available bisphosphonates MOA of Bisphosphonates Names of three bisphosphonates available IV Uses of bisphosphonates Major SE of bisphosphonates Bisphosphonates that cannot be used on continuous basis because it caused osteomalacia

Repaglinide

Insulin release from pancreas; faster and shorter acting than sulfonylurea Chlorpropamide, tolbutamide, tolazamide, etc. Glyburide, glipizide, glimepiride, etc.

Insulin release from pancreas by modifying K+ channels Hypoglycemia Chlorpropamide Pioglitazone, Rosiglitazone, Troglitazone (withdrawn/d from market) Hepatic toxicity

Stimulate PPAR-gamma receptor to regulate CHO and lipid metabolism Edema, mild anemia; interaction with drugs that undergo CytP450 3A4 metabolism Glucagon Alendronate, etidronate, risedronate, pamidronate, tiludronate, and zoledronic acid Inhibits osteoclast bone resorption Pamidronate, zoledronate, ibandronate Osteoporosis, Paget's disease, and osteolytic bone lesions, and hypercalcemia from malignancy Chemical esophagitis Etidronate Estrogen (HRT-Hormone replacement therapy) Raloxifene (SERM-selective estrogen receptor modulator) Calcitonin (salmon prep) Calcium Vitamin D St. Anthony's Fire Autocoids

Used for prevention of postmenopausal osteoporosis in women Increase bone density, also being tested for breast CA prophylaxis Used intranasally and decreases bone resorption Used especially in postmenopausal women, dosage should be 1500 mg Vitamin given with calcium to ensure proper absorption Disease caused by excess ergot alkaloids Endogenous substances commonly interpreted as histamine, serotonin, prostaglandins, and vasoactive peptides

Syndrome of hypersecretion of gastric acid and pepsin usually caused by gastrinoma; it is associated with severe peptic Zollinger-Ellison Syndrome ulceration and diarrhea

Drug that causes contraction of the uterus Distribution of histamine receptors H1, H2, and H3 Prototype antagonist of H1 and H2 receptors 1st generation antihistamine that is highly sedating 1st generation antihistamine that is least sedating 2nd generation antihistamines Generation of antihistamine that has the most CNS effects

Oxytocin

Smooth muscle; stomach, heart, and mast cells; nerve endings, CNS respectively Diphenhydramine and cimetridine, respectively Diphendydramine Chlorpheniramine or cyclizine Fexofenadine, loratadine, and cetirizine First generation due to being more lipidsoluble Use in IgE mediated allergic reaction

Major indication for H1 receptor antagonist Antihistamine that can be used for anxiety and insomnia and is hydroxyzine (Atarax) not addictive H1 antagonist used in motion sickness Most common side effect of 1st generation antihistamines Lethal arrhythmias resulting from concurrent therapy with azole fungals (metabolized by CYP 3A4) and these antihistamines which inhibit the 3A4 iso-enzyme. Clinical use for H2 blockers Receptors for serotonin (5HT-1) are located 5HT-1d agonist used for migraine headaches Triptan available in parenteral and nasal formulation H1 blocker that is also a serotonin antagonist Agents for reduction of postpartum bleeding Agents used in treatment of carcinoid tumor 5HT-3 antagonist used in chemotherapeutic induced emesis 5HT-3 antagonist that has been associated with QRS and QTc prolongation and should not be used in patients with heart disease DOC to treat chemo-induced nausea and vomiting Drug used in ergot alkaloids overdose, ischemia and gangrene Reason ergot alkaloids are contraindicated in pregnancy SE of ergot alkaloids Ergot alkaloid used as an illicit drug Dopamine agonist used in hyperprolactinemia Peptide causing increased capillary permeability and edema Mediator of tissue pain, edema, inactivated by ACE, and may be a contributing factor to the development of angioedema Drug causing depletion of substance P (vasodilator)

Dimenhydrinate, meclizine, and other 1st generation Sedation Terfenadine and astemizole (have been removed from the market) Cimetidine Acid reflux disease, duodenal ulcer and peptic ulcer disease

H2 blocker that causes the most interactions with other drugs

Mostly in the brain, and they mediate synaptic inhibition via increased K+ conductance Sumatriptan, naratriptan, and rizatriptan Sumatriptan Cyproheptadine Oxytocin, ergonovine and ergotamine Ketanserin cyproheptadine, and phenoxybenzamine

Ondansetron, granisetron, dolasetron and alosetron Dolasetron Odansetron Nitroprusside Uterine contractions Hallucinations resembling psychosis LSD Bromocriptine Bradykinin and histamine Bradykinin Capsaicin

Prostaglandins that cause abortions Difference between COX 1 and COX 2 Drug that selectively inhibits COX 2 Inhibitor of lipoxygenase Major SE of zileuton

Prostaglandin E1 (misoprostol) PGE2, and PGF2alpha

Inhibitor of leukotrienes (LTD4) receptors and used in asthma Used in pediatrics to maintain patency of ductus arteriosis Approved for use in severe pulmonary HTN Prostaglandin used in the treatment of impotence Irreversible, nonselective COX inhibitor Class of drugs that reversibly inhibit COX Primary endogenous substrate for Nitric Oxidase Synthase MOA and effect of nitric oxide Long acting beta 2 agonist used in asthma Muscarinic antagonist used in asthma MOA of cromolyn Methylxanthine derivative used as a remedy for intermittent claudication MOA of corticosteroids MOA of quinolones MOA of penicillin SE of long term (>5 days) corticosteroid therapy and remedy

COX 1 is found throughoutthe body and COX 2 is onlyin inflammatory tissue Celecoxib and rofecoxib Zileuton Liver toxicity Zafirlukast and montelukast PGE1 PGI2 (epoprostenol) Alprostadil Aspirin NSAIDS Arginine

Stimulates cGMP which leads to vascular smooth muscle relaxation Salmeterol Ipratropium Mast cell stabilizer Pentoxifylline inhibit phospholipase A2 Adrenal suppression and weaning slowly, respectively Inhibit DNA gyrase Block cell wall synthesis by inhibiting peptidoglycan cross-linkage Vancomycin Blocks peptidoglycan synthesis Point mutation Rifampin

Drug used for MRSA Vancomycin MOA Type of resistance found with vancomycin Meningitis prophylaxis in exposed patients Technique used to diagnose perianal itching, and the drug used Scotch tape technique and mebendazole to treat it Two toxicities of aminoglycosides DOC for Legionnaires' disease MOA of sulfonamides Penicillins active against penicillinase secreting bacteria Cheap wide spectrum antibiotic DOC for otitis media Class of antibiotics that have 10% cross sensitivity with penicillins PCN active against pseudomonas Antibiotic causing red-man syndrome, and prevention nephro and ototoxicity Erythromycin Inhibit dihydropteroate synthase Methicillin, nafcillin, and dicloxacillin Amoxicillin Cephalosporins Carbenicillin, piperacillin and ticarcillin Vancomycin, infusion at a slow rate and

Drug causes teeth discoloration MOA of tetracycline Drug that causes gray baby syndrome and aplastic anemia Drug notorious for causing pseudomembranous colitis DOC for tx of pseudomembranous colitis

antihistamines Tetracycline

Treatment of resistant pseudomembranous colitis Anemia caused by trimethoprim Reason fluoroquinolones are contraindicated in children and pregnancy DOC for giardia, bacterial vaginosis, pseudomembranous colitis, and trichomonas Treatment for TB patients (think RIPE)

Decreases protein synthesis by inhibiting 30S ribosome Chloramphenicol Clindamycin Metronidazole ORAL vancomycin Megaloblastic anemia Cartilage damage Metronidazole Rifampin, Isoniazid, Pyrazinamide, and Ethambutol Disulfiram-like reaction Red urine discoloration Bind ergosterol in fungal cell membrane Administration of Vit. B6 (pyridoxine) Nephrotoxicity Gynecomastia Topical mupirocin (Bactroban) Amantadine Ribavirin Ganciclovir Neutro, leuko and thrombocytopenia Nevirapine, amprenavir Delavirdine, efavirenz, and ribavirin

Metronidazole SE if given with alcohol Common side effect of Rifampin MOA of nystatin Neurotoxicity with isoniazid (INH) prevented by Toxicity of amphotericin SE seen only in men with administration of ketoconazole Topical DOC in impetigo DOC for influenza A DOC for RSV DOC for CMV retinitis SE for ganciclovir Anti-viral agents associated with Stephen Johnson syndrome HIV antiviral class known to have severe drug interactions by Protease inhibitors causing inhibition of metabolism Antivirals that are teratogens Antivirals associated with neutropenia HIV med used to reduce transmission during birth Drug used for African sleeping sickness Drug used in Chagas disease Cephalosporins able to cross the BBB Cephalosporins NOT able to cross the BBB Drug used for N. gonorrhea in females Cephalosporin causes kernicterus in neonates SE of INH Aminoglycoside that is least ototoxic

Ganciclovir, zidovudine, saquinavir, and interferon AZT (zidovudine) Suramin Nifurtimox

Cefuroxime (2nd) generation, Ceftazidime, Ceftriaxone Cefixime (3rd) generation Ceftriaxone Ceftriaxone or cefuroxime Peripheral neuritis and hepatitis Streptomycin

Drug used in exoerythrocytic cycle of malaria Oral antibiotic of choice for moderate inflammatory acne Drug of choice for leprosy DOC for herpes and its MOA Anti-microbials that cause hemolysis in G6PD-deficient patients MOA of erythromycin

Primaquine Minocycline

Dapsone, rifampin and clofazimine combination

Acyclovir; incorporated into viral DNA and chain termination Sulfonamides Inhibition of protein synthesis at the 50s subunit of ribosome sulfamethoxazole/ trimethoprim Aztreonam Seizures Didanosine Sedation

Anti-biotic frequently used for chronic UTI prophylaxis Lactam that can be used in PCN allergic patients SE of imipenem Anti-viral with a dose limiting toxicity of pancreatitis Common side effect of hypnotic agents Occurs when sedative hypnotics are used chronically or at high Tolerance doses The most common type of drug interaction of sedative hypnotics with other depressant medications Benzodiazepines used to promote sleep Benzodiazepine used for anxiety Non-benzodiazepine used as an anxiolytic Non-benzodiazepine used for sleep Major effect of benzodiazepines on sleep at high doses Neurologic SE of benzodiazepines Reason benzos are used cautiously in pregnancy Main route of metabolism for benzodiazepines Benzodiazepine that undergo extrahepatic conjugation (which are useful in older or hepatically impaired) MOA for benzodiazepines Antidote to benzodiazepine overdose (antagonist that reverses the CNS effects)

Additive CNS depression Temazpam, trizolam, flurazepam Alprazolam Buspirone Zolpidem REM is decreased Anterograde amnesia Ability to cross the placenta Hepatic Lorazepam, oxazepam, and temazepam increase the FREQUENCY of GABAmediated chloride ion channel opening Flumazenil

Benzodiazepine with useful relaxant effects in skeletal muscle Diazepam spasticity of central origin

Benzodiazepine that has efficacy against absence seizures and Clonazepam in anxiety states, such as agoraphobia Benzodiazepine that is used for anesthesia DOC for status epilepticus Longer acting benzodiazepines used in the management of withdrawal states of alcohol and other drugs Agents having active metabolites, long half lives, and a high Midazolam Diazepam

Benzodiazepines that are the most effective in the treatment of Alprazolam and Clonazepam panic disorder

Chlordiazepoxide and Diazepam Diazepam, Flurazepam, chlordiazepoxide, and

incidence of adverse effects clorazepate Barbiturates Barbiturates may precipitate this hematologic condition Acute intermittent porphyria Barbiturates decrease the effectiveness of many other drugs via Liver enzyme INDUCTION this pharmacokinetics property Barbiturates MOA Barbiturate used for the induction of anesthesia Site of action for zaleplon and zolpidem Good hypnotic activity with less CNS SE than most benzodiazepines

Increase the DURATION of GABA-mediated chloride ion channels Thiopental

Benzodiazepine receptor BZ1 (although do not have a benzodiazepine ring structure) Zolpidem, zaleplon

Agent that is a partial agonist for the 5-HT1A receptor Buspirone Drug of choice for generalized anxiety disorder, NOT effective Buspirone in acute anxiety Agent that is metabolized to acetaldehyde by alcohol dehydrogenase and microsomal ethanol-oxidizing system (MEOS) Agent with zero-order kinetics Rate limiting step of alcohol metabolism System that increases in activity with chronic ethanol exposure and may contribute to tolerance Enzyme that metabolizes acetaldehyde to acetate Agents that inhibit acetaldehyde dehydrogenase Agent that inhibits alcohol dyhydrogenase and its clinical use Agent used in the treatment of alcoholism, if alcohol is consumed concurrently, acetaldehyde builds up and results in nausea, headache, flushing, and hypotension The most common neurologic abnormality in chronic alcoholics Agent that is teratogen and causes a fetal syndrome Agent that is the antidote for methanol overdose Drug that inhibits alcohol dehydrogenase and is used in ethylene glycol exposure Most frequent route of metabolism Mechanisms of action for Phenytoin, Carbamazepine, Lamotrigine MOA for benzodiazepines and barbiturates MOA for Ethosuximide MOA for Valproic acid at high doses Drugs of choice for generalized tonic-clonic and partial Ethanol Ethanol Aldehyde dehydrogenase MEOS Aldehyde dehydrogenase Disulfiram, metronidazole, certain sulfonylureas and cephalosporins FOMEPIZOLE used to prevent formation of toxic metabolites from methanol and ethylene glycol ingestion Disulfiram Peripheral neuropathy (also excessive alcohol use is associated with HTN, anemia, and MI) Ethanol Ethanol, fomepizole Fomepizole Hepatic enzymes Sodium channel blockade GABA-related targets Calcium channels

Affect calcium, potassium, and sodium channels

seizures DOC for febrile seizures Drugs of choice for absence seizures Drug of choice for myoclonic seizures Drugs of choice for status epilepticus Drugs that can be used for infantile spasms Anti-seizure drugs used also for bipolar affective disorder (BAD) Anti-seizure drugs used also for Trigeminal neuralgia Anti-seizure drugs used also for pain of neuropathic orgin Anti-seizure agent that exhibits non-linear metabolism, highly protein bound, causes fetal hydantoin syndrome, and stimulates hepatic metabolism SE of phenytoin Anti-seizure agent that induces formation of liver drugmetabolism enzymes, is teratogen and can cause craniofacial anomalies and spina bifida Agent that inhibits hepatic metabolism, is hepatotoxic and teratogen that can cause neural tube defects and gastrointestinal distress Laboratory value required to be monitored for patients on valproic acid SE for Lamotrigine SE for Felbamate Anti-seizure medication also used in the prevention of migraines Carbamazepine may cause Anti-seizure drugs used as alternative drugs for mood stabilization MOA of general anesthetics Inhaled anesthetic with a low blood/gas partition coefficient Inversely related to potency of anesthetics

Valproic acid and Phenytoin Phenobarbital Ethosuximide and valproic acid Valproic acid

IV diazepam for short term (acute) treatment; phenytoin for prolonged therapy Corticosteroids Valproic acid, carbamazepine, phenytoin and gabapentin Carbamazepine Gabapentin Phenytoin Gingival hyperplasia, nystagmus, diplopia and ataxia Carbamazepine Valproic acid Serum ammonia and LFT's Stevens-Johnson syndrome Valproic acid Agranulocytosis Carbamazepine, gabapentin, lamotrigine, and valproic acid Aplastic anemia and acute hepatic failure

Most are thought to act at GABA-A receptor chloride channel Nitrous oxide Minimum alveolar anesthetic concentration (MAC) Decrease arterial blood pressure Enflurane and halothane Isoflurane Halothane

Inhaled anesthetics metabolized by liver enzymes which has a Halothane and methoxyflurane major role in the toxicity of these agents Most inhaled anesthetics SE Inhaled anesthetics are myocardial depressants Inhaled anesthetic causes peripheral vasodilation Inhaled anesthetic that may sensitize the myocardium to arrhythmogenic effects of catecholamines and has produced hepatitis

Inhaled anesthetic, less likely to lower blood pressure than other agents, and has the smallest effect on respiration Prolonged exposure to this inhaled anesthetic may lead to megaloblastic anemia

Nitrous oxide

Fluoride released by metabolism of this inhaled anesthetic may Methoxyflurane cause renal insufficiency Nitrous oxide Desflurane Pungent inhaled anesthetic which leads to high incidence of coughing and vasospasm IV barbiturate used as a pre-op anesthetic Benzodiazepine used adjunctively in anesthesia Benzodiazepine receptor antagonist, it accelerates recovery from benzodiazepine overdose

DOC for malignant hyperthermia that may be caused by use of Dantrolene halogenated anesthetics

Thiopental Midazolam Flumazenil Ketamine Fentanyl

This produces "dissociative anesthesia"", is a cardiovascular stimulant which may increases intracranial pressure, and hallucinations occur during recovery" Opioid associated with respiratory depression, but is used in high risk patients who may not survive full general anesthetia

State of analgesia and amnesia produced when fentanyl is used Neuroleptanesthesia with droperidol and nitrous oxide Produces both rapid anesthesia and recovery, has antiemetic activity and commonly used for outpatient surgery, may cause marked hypotension MOA of local anesthetics (LA's) This may enhance activity of local anesthetics This may antagonize activity of local anesthetics Almost all local anesthetics have this property and sometimes require the administration of vasoconstrictors (ex. Epinephrine) to prolong activity Local anesthetic with vasoconstrictive property, favored for head, neck, and pharyngeal surgery Longer acting local anesthetics which are less dependent on vasoconstrictors These LA's have surface activity Most important toxic effects of most local anesthetics Commonly abused LA which has cardiovascular toxicity including severe hypertension with cerebral hemorrhage, cardiac arrhythmias, and myocardial infarction LA causing methemoglobinemia Structurally related to acetylcholine, used to produce muscle paralysis in order to facilitate surgery or artifical ventilation. Full doses lead to respiratory paralysis and require ventilation These drugs strongly potentiate and prolong effect of neuromuscular blockade (NMB) These prevent the action of Ach at the skeletal muscle endplate Propofol Block voltage-dependent sodium channels Hyperkalemia Hypercalcemia Vasodilation Cocaine Tetracaine and bupivacaine Cocaine and benzocaine CNS toxicity Cocaine Prilocaine Neuromuscular blocking drugs Inhaled anesthetics, especially isoflurane, aminoglycosides, and antiarrhythmic

to produce a "surmountable blockade,"" effect is reversed by Nondepolarizing type antagonists cholinesterase inhibitors (ex. neostigmine or pyridostigmine)" Agent with long duration of action and is most likely to cause Tubocurarine histamine release Non-depolarizing skeletal muscle antagonist that has short duration Mivacurium Pancuronium Atracurium Succinylcholine Cholinesterase inhibitors Spasmolytic drugs Diazepam Baclofen Tizanidine Dantrolene Cyclobenzaprine Drug induced Parkinsonism L-dopa Skeletal muscle agent that can block muscarinic receptors Skeletal muscle agent that undergoes Hofmann elimination (breaks down spontaneously)

One depolarizing blocker that causes continuous depolarization and results in muscle relaxation and paralysis, causes muscle pain postoperatively and myoglobinuria may occur During Phase I these agents worsen muscle paralysis by succinylcholine, but during phase II they reverse the blockade produced by succinylcholine Agents acting in the CNS or in the skeletal muscle, used to reduce abnormally elevated tone caused by neurologic or muscle end plate disease Facilitates GABA presynaptic inhibition GABA agonist in the spinal cord Similar to clonidine and may cause hypotension DOC for malignant hyperthermia by acting on the sacroplasmic reticulum or skeletal muscle

Agent used for acute muscle spasm Irreversible condition resulting from the use of antipsychotics, reserpine at high doses, and MPTP (by-product of illicit meperidine analog) Agent used in drug therapy of Parkinson's instead of Dopamine which has low bioavailability and does not cross the BBB This is combined with L-dopa, inhibits DOPA decarboxylase (active only peripherally) which allows lower effective doses of L-dopa and allows for fewer SE's (GI distress, postural hypotension, 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 and Levodopa is contraindicated in closed angle glaucoma Ergot alkaloid that is a partial agonist at D2 receptors in the brain, used for patients who are refractory or cannot tolerate levodopa, causes erythromelalgia Non ergot agents used as first-line therapy in the initial management of Parkinson's Bromocriptine Pramipexole and ropinirole Amantadine Selegiline

Enhances dopaminergic neurotransmission SE's include CNS excitation, acute toxic psychosis and livedo reticularis Inhibitor of MAO type B which metabolizes dopamine, used adjunct to levodopa or as sole agent in newly diagnosed patients

Inhibitors of catechol-O-methyltransferase (COMT), used as adjuncts in Parkinson's dx and cause acute hepatic failure Entacapone and Tolcapone (monitor LFT's) Agent decreases the excitatory actions of cholinergic neurons. May improve tremor and rigidity but have LITTLE effect on Benztropine bradykinesia. Atropine-like side effects Agent effective in physiologic and essential tremor Propranolol Agents used in Huntington's Disease Agents used in Tourette's dx Chelating agent used in Wilson's disease Extrapyramidal dysfunction is more common with these agents, which block this subtype of dopamine receptor MOA of neuroleptics Side effects occuring in antipsychotics that block dopamine Antipsychotics that reduce positive symptoms only Newer atypical antipsychotics that also improve some of the negative symptoms and help acute agitation

Tetrabenazine (amine depleting drug), Haloperidol (antipsychotic) Haloperidol or pimozide Penicillamine Older antipsychotic agents, D2 receptors Dopamine blockade Hyperprolactinemia, menorrhea, galactorrhea, confusion, mood changes, decreased sexual interest, and weight gain Older antipsychotics Olanzapine, aripiprazole, and sertindole

Antipsychotic used in the treatment of psychiatric symptoms in Risperidone patients with dementia Atypical antipsychotic causing high prolactin levels Risperidone Newer atypical antipsychotic used for bipolar disorder, known Olanzapine to cause weight gain, and adversely affect diabetes Agent more frequently associated with extrapyramidal side effects that can be treated with benzodiazepine, diphenhydramine or muscarinic blocker Drug used in neuroleptic malignant syndrome Agents may exacerbate tardive dyskinesias (may be irreversible and there is no treatment) Haloperidol Dantrolene Muscarinic blockers Thioridazine Haloperidol Thioridazine Clozapine Clozapine Fluphenazine and haloperidol

Antipsychotic having the strongest autonomic effects Antipsychotic having the weakest autonomic effects Only phenothiazine not exerting antiemetic effects, can cause visual impairment due to retinal deposits, and high doses have been associated with ventricular arrhythmias Agent having no effect on D2 receptors, blocks D4, reserved for resistant schizophrenia, and can cause fatal agranulocytosis Anti-psychotic not shown to cause tardive dyskinesia Anti-psychotics available in depot preparation Reduced seizure threshold Orthostatic hypotension and QT prolongation Increased risk of developing cataracts Major route of elimination for Lithium

Low-potency typical antipsychotics and clozapine Low potency phenothiazines and ziprasidone Quetiapine Kidneys

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

Lithium toxicity Theophylline Cardiac anomalies and is contraindicated in pregnancy or lactation Lithium Low therapeutic index

Drug increases the renal clearance hence decreases levels of lithium Lithium is associated with this congenital defect DOC for bipolar affective disorder Concern using lithium SE of lithium Example of three antidepressants that are indicated for obsessive compulsive disorder

Tremor, sedation, ataxia, aphasia, thyroid enlargement, and reversible diabetes insipidus Clomipramine, fluoxetine and fluvoxamine Norepinephrine and serotonin 2 to 3 weeks Elderly patients Side-effect profile and prior pt response SSRI's, bupropion, and venlafaxine Monamine oxidase inhibitors

Neurotransmitters affected by the action of antidepressants Usual time needed for full effect of antidepressant therapy Population group especially sensitive to side effects of antidepressants Well-tolerated and are first-line antidepressants Most useful in patients with significant anxiety, phobic features, hypochondriasis, and resistant depression

All antidepressants have roughly the same efficacy in treating depression, agents are chosen based on these criterion

Condition will result from in combination of MAOI with tyramine containing foods (ex. wine, cheese, and pickled Hypertensive crisis meats) MAOI should not be administered with SSRI's or potent TCA's Serotonin syndrome due to development of this condition Sedation is a common side effect of these drugs, they lower seizure threshold, uses include BAD, acute panic attacks, phobias, enuresis, and chronic pain and their overdose can be deadly Three C's associated with TCA toxicity Tricyclic antidepressants (TCA) Coma, Convulsions, Cardiac problems (arrhythmias and wide QRS)

Agents having higher sedation and antimuscarinic effects than Tertiary amines other TCA's TCA used in chronic pain, a hypnotic, and has marked antimuscarinic effects TCA used in chronic pain, enuresis, and ADD TCA with greatest sedation of this group, and marked antimuscarinic effects, used for sleep Amitriptyline Imipramine Doxepin Clomipramine

TCA used in obsessive compulsive disorder (OCD), most significant of TCA's for risk of seizure, weight gain, and neuropsychiatric signs and symptoms Secondary amines that have less sedation and more excitation effect Side effects seen with tricyclic antidepressants

Nortriptyline, Desipramine Muscarinic blockade (dry mouth, constipation); weak alpha-1 block (orthostatic hypotension);

Antidepressant associated with neuroleptic malignant syndrome

weak hisamine block (sedation) Amoxapine Maprotiline Venlafaxine Venlafaxine Trazodone Nefazodone Bupropion

Antidepressant associated with seizures and cardiotoxicity Antidepressant having stimulant effects similar to SSRI's and can increase blood pressure Antidepressant inhibiting norepinephrine, serotonin, and dopamine reuptake Antidepressant also used for sleep that causes priapism Antidepressant which is inhibitor of CYP450 enzymes and may be associated with hepatic failure

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

Antidepressant with MOA as alpha 2 antagonist, has effects on Mirtazapine both 5-HT and NE, blocks histamine receptors, and is sedating SE of mirtazapine Except for these agents all SSRI have significant inhibition of CytP450 enzymes

Liver toxicity, increased serum cholesterol 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 for Fluoxetine maintenance, not acute tx SSRI indicated for premenstrual dysphoric disorder Some of SSRIs' therapeutic effects beside depression SSRI less likely to cause a withdrawal syndrome Inhibit synaptic activity of primary afferents and spinal cord pain transmission neurons Activation of these receptors open K+ ion channels to cause membrane hyperpolarization

Fluoxetine (Sarafem) Panic attacks, social phobias, bulimia nervosa, and PMDD (premenstrual dysphoric disorder), OCD Fluoxetine Ascending pathways

Activation of these receptors close Ca2+ ion channels to inhibit Presynaptic mu, delta, and kappa receptors neurotransmitter release 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 blocking Meperidine action) cause pupillary constriction SE of these drugs include dependence, withdrawal syndrome, sedation, euphoria, respiratory depression nausea and vomiting, constipation, biliary spasm, increased ureteral and bladder tone, and reduction in uterine tone Strong opioid agonists Opioids used in anesthesia Opioid Analgesics Morphine, methadone, meperidine, and fentanyl Morphine and fentanyl

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 helps Morphine to relieve the dyspnea of pulmonary edema Moderate opioid agonists Weak opioid agonist, poor analgesic, its overdose can cause severe toxicity including respiratory depression, circulatory collapse, pulmonary edema, and seizures Partial opioid agonist, considered a strong analgesic, has a long duration of action and is resistant to naloxone reversal

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

Codeine, hydrocodone, and oxycodone Propoxyphene Buprenorphine Naloxone Naltrexone Dextromethorphan, Codeine Diphenoxylate, Loperamide NO, chloroform, and diethyl ether Fluorocarbons and Industrial solvents Organic nitrites Steroids Changes in heart rate, blood pressure, respiration, body temperature, sweating, bowel signs, and pupillary responses Heroin, morphine, oxycodone, meperidine and fentanyl IV administration Overdose of opioids Abstinence syndrome Methadone, followed by slow dose reduction Naloxone Reduce inhibition, suppress anxiety, and produce relaxation Depression of medullary and cardiovascular centers

Opioid antagonist that is given IV and had short DOA Opioid antagonist that is given orally in alcohol dependency programs

These agents are used as antitussive These agents are used as antidiarrheal Inhalant anesthetics Toxic to the liver, kidney, lungs, bone marrow, peripheral nerves, and cause brain damage in animals, sudden death has occurred following inhalation Cause dizziness, tachycardia, hypotension, and flushing Causes acne, premature closure of epiphyses, masculinization in females, hepatic dysfunction, MI, and increases in libido and aggression Readily detected markers that may assist in diagnosis of the cause of a drug overdose include Most commonly abused in health care professionals This route is associated with rapid tolerance and psychologic dependence

Leads to respiratory depression progressing to coma and death Lacrimation, rhinorrhea, yawning, sweating, weakness, gooseflesh, nausea, and vomiting, tremor, muscle jerks, and hyperpnea are signs of this syndrome Treatment for opioid addiction This agent may cause more severe, rapid and intense symptoms to a recovering addict Sedative-Hypnotics action

Additive effects when Sedative-Hypnotics used in combination CNS depressants with these agents Common mechanism by which overdose result in death

"Date rape drug" The most important sign of withdrawal syndrome Treatment of withdrawal syndrome involves These agents are CNS depressants Withdrawal from this drug causes lethargy, irritability, and headache W/D from this drug causes anxiety and mental discomfort Treatments available for nicotine addiction Chronic high dose abuse of nicotine leads to

Flunitrazepam (rohypnol) Excessive CNS stimulation (seizures)

Long-acting sedative-hypnotic or a gradual reduction of dose, clonidine or propranolol Ethanol, Barbiturates, and Benzodiazepines Caffeine Nicotine Patches, gum, nasal spray, psychotherapy, and bupropion Psychotic state, overdose causes agitation, restlessness, tachycardia, hyperthermia, hyperreflexia, and seizures Amphetamines Dextroamphetamines and methamphetamine DOM, STP, MDA, and MDMA "ecstasy"" "

Tolerance is marked and abstinence syndrome occurs Amphetamine agents These agents are congeners of Amphetamine Overdoses of this agent with powerful vasoconstrictive action may result in fatalities from arrhythmias, seizures, respiratory Cocaine "super-speed""" depression, or severe HTN (MI and stroke) Most dangerous of the currently popular hallucinogenic drugs, OD leads to nystagmus, marked hypertension, and seizures, PCP presence of both horizontal and vertical nystagmus is pathognomonic Removal of PCP may be aided THC is active ingredient, SE's include impairment of judgment, and reflexes, decreases in blood pressure and psychomotor performance occur This agent has greater affinity for muscarinic receptors and used for postoperative and neurogenic ileus and urinary retention Only direct acting agent that is very lipid soluble and used in glaucoma

Urinary acidification and activated charcoal or continual nasogastric suction Marijuana Bethanechol Pilocarpine

This agent used to treat dry mouth in Sjgren's syndrome Cevimeline Indirect-Acting ACh Agonist, alcohol, short DOA and used in Edrophonium diagnosis of myasthenia gravis Carbamate with intermediate action, used for+A1170 postoperative and neurogenic ileus and urinary retention Neostigmine Physostigmine Pyridostigmine Echothiophate Long acting cholinesterase inhibitors Malathion Treatment of atropine overdose and glaucoma (because lipid soluable). Enters the CNS rapidly and has a stimulant effect, which may lead to convulsions Treatment of myasthenia gravis Antiglaucoma organophosphate Associated with an increased incidence of cataracts in patients treated for glaucoma Scabicide organophosphate

Organophosphate anthelmintic agent with long DOA Toxicity of organophosphate: The most frequent cause of acute deaths in cholinesterase inhibitor toxicity

Metrifonate

DUMBELSS (diarrhea, urination, miosis, bronchoconstriction, excitation of skeletal muscle and CNS, lacrimation, salivation, and sweating) Respiratory failure Parathion Atropine Pralidoxime Nonselective Muscarinic Antagonists Benztropine, trihexyphenidyl Scopolamine, meclizine Atropine, homatropine,C1208 tropicamide Ipratropium Dicyclomine, methscopolamine Oxybutynin, dicyclomine

The most toxic organophosphate Treatment of choice for organophosphate overdose This agent regenerates active cholinesterase and is a chemical antagonist used to treat organophosphate exposure Prototypical drug is atropine Treat manifestations of Parkinson's disease and EPS Treatment of motion sickness Produce mydriasis and cycloplegia

Bronchodilation in asthma and COPD Reduce transient hyper GI motility Cystitis, postoperative bladder spasms, or incontinence Toxicity of anticholinergics Another pneumonic for anticholinergic toxicity Atropine fever is the most dangerous effect and can be lethal in this population group Contraindications to use of atropine Limiting adverse effect of ganglion blockade that patients usually are unable to tolerate

block SLUD (salivation, lacrimation, urination, defecation "dry as a bone, red as a beet, mad as a hatter, hot as a hare, blind as a bat" Infants Infants, closed angle glaucoma, prostatic hypertrophy Severe hypertension Cholinesterase inhibitors Nondepolarizing Neuromuscular Blockers Succinylcholine Cholinesterase regenerators, pralidoxime Pralidoxime, atropine You have 1 heart (Beta 1) and 2 lungs (Beta 2) Epinephrine Amphetamines Phenylephrine

Reversal of blockade by neuromuscular blockers Tubocurarine is the prototype, pancuronium, atracurium, vecuronium are newer short acting agent, produce competitive block at end plate nicotinic receptor, causing flaccid paralysis Only member of depolarizing neuromuscular blocker, causes fasciculation during induction and muscle pain after use; has short duration of action Chemical antagonists that bind to the inhibitor of ACh Estrace and displace the enzyme (if aging has not occurred)

Used to treat patients exposed to insecticides such as parathion Pneumonic for beta receptors This is the drug of choice for anaphylactic shock Phenylisopropylamines that are used legitimately and abused for narcolepsy, attention deficit disorder, and weight reduction Alpha agonist used to produce mydriasis and reduce conjunctival itching and congestion caused by irritation or allergy, it does not cause cycloplegia

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

Reduce aqueous secretion

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

Longer acting Beta 2 agonist is recommended for prophylaxis Salmeterol of asthma 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 help maintain perfusion Shock due to septicemia or myocardial infarction is made worse by Epinephrine is often mixed with a local anesthetic to Chronic orthostatic hypotension can be treated with Beta 2 agonist used to suppress premature labor, but cardiac stimulatory effects may be hazardous to mother and fetus Mast cells to reduce release of hisamine and inflammatory mediators

These agents increase cardiac output and may be beneficial in Beta1 agonists treatment of acute heart failure and some types of shock Alpha1 agonists Increasing afterload and tissue perfusion declines Reduce the loss from area of injection Midodrine Terbutaline Epinephrine Epinephrine Dopamine

Sympathetic agent which stimulates heart rate and can dilate vessels in skeletal muscle at low doses Agent used in shock because it dilates coronary arteries and increases renal blood flow Long acting sympathomimetic, sometimes used to improve urinary continence in children and elderly with enuresis

Agent which stimulates cardiac contractile force more than rate Dobutamine with little effect on total peripheral resistance Ephedrine Hypertension Sinus tachycardia and serious arrhythmias Skeletal muscle tremor, tachycardia high doses Phenoxybenzamine Alpha 1 agonist toxicity Beta 1 agonist toxicity Beta 2 agonist toxicity The selective agents loose their selectivity at Nonselective alpha-blocking drug, long acting and irreversible, and used to treat pheochromocytoma. Blocks 5-HT, so occasionaly used for carcinoid tumor. Blocks H1 and used in mastocytosis

Nonselective alpha-blocking drug, short acting and reversible, used for rebound HTN from rapid clonidine withdrawal, and Phentolamine Raynaud's phenomena Selective Alpha 1 blocker used for hypertension, BPH, may Prazosin, terazosin, doxazosin cause first dose orthostatic hypotension Selective Alpha-1A blocker, used for BPH, but with little effect on HTN Tamsulosin Yohimbine Selective Alpha 2 blocker used for impotence (controversial effectiveness) SelectiveB1 Receptor blockers that may be useful in treating

patients even though they have asthma Combined alpha and beta blocking agents that may have application in treatment of CHF

Acebutolol, atenolol, esmolol, metoprolol Labetalol and carvedilol Pindolol and acebutolol Timolol Esmolol Nadolol Acebutolol and atenolol Propranolol

Beta blockers partial agonist activity (intrinsic sympathomimetic activity) cause some bronchodilation and may have an advantage in treating patients with asthma This beta blocker lacks local anesthetic activity (a property which decreases protective reflexes and increases the risk of corneal ulceration) and used in treating glaucoma This parenteral beta blocker is a short acting (minutes) This beta blocker is the longest acting These beta blockers are less lipid soluble This beta blocker is highly lipid soluble and may account for side effects such as nightmares Toxicity of these agents include bradycardia, AV blockade, exacerbation of acute CHF; signs of hypoglycemia may be masked (tachycardia, tremor, and anxiety) Cholinomimetics that increase outflow, open trabecular meshwork, and cause ciliary muscle contraction

Clinical uses of these agents include treatment of HTN, angina, Beta blockers arrhythmias, chronic CHF, and selected post MI patients Beta blockers Pilocarpine, carbachol, physostigmine Epinephrine, dipivefrin

Nonselective alpha agonists that increases outflow, probably via the uveoscleral veins

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, alkalinization Acetazolamide of the urine may precipitate calcium salts, hypokalemia, acidosis This agent cause increased aqueous outflow Inhibit angiotensin-converting enzyme (ACE) Captopril and enalapril (-OPRIL ending) are SE of ACE inhibitors ACE inhibitors are contraindicated in Losartan and valsartan block Angiotensin receptor blockers do NOT cause Agents that block L-type calcium channel CCB contraindicated in CHF CCB with predominate effect on arteriole dilation SE of CCB Agents that reduce heart rate, contractility, and O2 demand B-blockers that are more cardioselective Cardioselective Beta 1-blockers Prostaglandin PGF2a ACE inhibitors ACE inhibitors Dry cough, hyperkalemia pregnancy and with K+ Angiotensin receptor Dry cough Calcium channel blockers Verapamil Nifedipine Constipation, edema, and headache Beta-blockers Beta-1 selective blockers Atenolol, acebutolol, and metoprolol

Asthma (bronchospastic effects), diabetes (block signs of hypoglycemia) and peripheral vascular disease Non-selective Beta-blocker also used for migraine prophylaxis Propranolol Bradycardia, SEXUAL DYSFUNCTION, SE of beta blockers decrease in HDL, and increase in Triglycerols (TG) Beta-blockers should be used cautiously in 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) Alpha 1selective blockers SE of alpha blockers Presynaptic Alpha 2 agonist used in HTN, and acts centrally SE of methyldopa Methyldopa is contraindicated in SE of clonidine Direct vasodilator of arteriolar smooth muscle SE of hydralazine Arterial vasodilator that works by opening K+ channels SE of minoxidil IV Drug used Hypertensive Crisis Nitroprusside vasodilates Toxicity caused by nitroprusside and treatment Carbonic anhydrase inhibitor Diuretic used for mountain sickness and glaucoma SE of acetazolamide MOA of loop diuretics Site of action of loop diuretics SE of loop (furosemide) diuretics Aminoglycosides used with loop diuretics potentiate adverse effect Loops lose and thiazide diuretics retain MOA of thiazide diuretics Site of action of thiazide diuretics Class of drugs that may cause cross-sensitivity with thiazide diuretics SE of thiazide (HCTZ) diuretics

Orthostatic hypotension (especially with first dose) and reflex tachycardia Clonidine, and methyldopa Positive Coomb's test, depression Geriatrics due to its CNS (depression) effects Rebound HTN, sedation, dry mouth Hydralazine Lupus-like syndrome Minoxidil Hypertrichosis Nitroprusside Arteries and veins Cyanide toxicity treated with sodium thiosulfate Acetazolamide Acetazolamide

Paresthesias, alkalization of the urine (which may ppt. Ca salts), hypokalemia, acidosis, and encephalopathy in patients with hepatic impairment inhibits Na+/K+/2Cl- cotransport Thick ascending limb Hyperuricemia, hypokalemia and ototoxicity Ototoxicity Calcium Inhibit Na+/Cl- cotransport Work at early distal convoluted tubule Sulfonamides Hyperuricemia, hypokalemia and hyperglycemia

Potassium sparing diuretics inhibit Diuretic used to treat primary aldosteronism SE of spironolactone Osmotic diuretic used to treat increased intracranial pressure ADH agonist used for pituitary diabetes insipidus Used for SIADH SE of demeclocycline MOA of class I A (eg. Procainamide), class IB (eg. Lidocaine), and class IC (eg. Flecainide) antiarrhythmics SE of procainamide Limiting side effect of Quinidine Other side effects of Quinidine Major drug interaction with Quinidine DOC for management of acute ventricular arrhythmias DOC for digoxin induced arrhythmias Class of anti-arrhythmics that has a pro-arrhythmic effect (CAST trial), therefore are used as last line agents

Na+/K+ exchange Spironolactone Gynecomastia hyperkalemia, and impotence Mannitol Desmopressin (DDAVP) Demeclocycline Bone marrow and teeth discoloration for children under 8 years of age Sodium channel blockers Lupus-like syndrome Prolongs QT interval

Thrombocytopenic purpura, and CINCHONISM Increases concentration of Digoxin Amiodarone Phenytoin Class IC (flecainide, propafenone, moricizine) B-blockers Sotalol prolongs QT and PR interval Esmolol B-blockers Potassium channel blockers Amiodarone Prolonged half-life, up to six weeks Amiodarone Cardiac dysfunction, photosensitivity, skin (blue smurf syndrome), Pulmonary fibrosis, thyroid and corneal deposits Calcium channel blockers Torsades de pointes Magnesium sulfate Digoxin Adenosine Activattion on an inward K+ current and inhibition of Ca++ current resulting in marked hyperpolarization Adenosine

Class II antiarrhythmics are Antiarrhythmic that exhibits Class II and III properties Side effect of sotalol Used intravenously for acute arrhythmias during surgery Anti-arrhythmics that decrease mortality MOA of class III antiarrhythmics Class III antiarrhythmic that exhibits properties of all 4 classes Specific pharmacokinetic characteristic of amiodarone Antiarrhythmic effective in most types of arrhythmia SE of Amiodarone MOA of class IV antiarrhythmics Life threatening cardiac event that prolong QT leads to Agent to treat torsades de pointes Drug used supraventricular arrhythmias DOC for paroxysmal supraventricular tachycardia (PSVT) Adenosine's MOA Anti-arrhythmic with 15 second duration of action MOA of sildenafil (Viagra)

Inhibits phosphodiesterase-5, enhancing effects of nitric oxide-activated increases in cGMP

Drugs used in the management of angina Aspirin reduces mortality in unstable angina by MOA of nitrates Nitrate used for acute anginal attacks Nitrate used to prevent further attacks Nitrate free intervals are needed due to SE of nitrates CCB are DOC for Beta blockers are used for which type of anginal attack MOA of Cardiac glycosides (eg. digoxin) Digoxin is used in Digoxin toxicity can be precipitated by Antidote for digoxin toxicity Phosphodiesterase inhibitors that increase mortality and have been found to have NO beneficial effects SE of amrinone Beta 1 agonists used in acute CHF Diuretics work in CHF by Beta blockers work in CHF by Peptide drug used to treat CHF MOA of nesiritide SE of nesiritide Agent used in CHF that is a selective alpha and nonselective beta blocker Agent used in acutely decompensated CHF resembling natriuretic peptide Vitamin K dependent anticoagulant Warfarin is contraindicated in Anticoagulant of choice in pregnancy Heparin (PTT) increases activity of Route of administration of warfarin Routes of administration of heparin SE of both warfarin and heparin SE of heparin Alternative anticoagulant used if HIT develops Antidote to reverse actions of warfarin

Aspirin, Nitrates, CCB, and Beta blockers Platelet aggregation inhibition

Relax vascular smooth muscle, at low doses dilate veins and at high doses dilate arterioles Nitroglycerin sublingual tablets Oral and transdermal forms of nitroglycerin Tolerance Postural hypotension, reflex tachycardia, hot flashes, and throbbing headache due to meningeal artery dilation Prinzmetal's angina Classic Indirectly increase intracellular calcium and cardiac contractility by inhibiting Na+/K+ ATPase Atrial fibrillation and CHF Hypokalemia Digibind Amrinone and milrinone Thrombocytopenia Dobutamine and dopamine Reducing preload Nesiritide (BNP)

Reducing progression of heart failure (never use in acute heart failure) Increasing sodium excretion and decreases arterial and venous tone Excessive hypotension and kidney failure Carvedilol Nesiritide (Natrecor) Warfarin (PT) Pregnancy Heparin Antithrombin 3 Oral IV and IM (only LMW) Bleeding Heparin induced thrombocytopenia (HIT) Lepirudin Vitamin K or fresh frozen plasma

Antidote to reverse actions of heparin MOA of aspirin Agent used to treat MI and to reduce incidence of subsequent MI SE of Aspirin Antiplatelet drug reserved for patients allergic to aspirin SE for ticlopidine Effective in preventing TIA's Prevents thrombosis in patients with artificial heart valve Block glycoprotein IIb/IIIa involved in platelet cross-linking MOA of thrombolytics Thrombolytics are used for Thrombolytic that can cause allergic reaction Thrombolytic used for acute MI and ischemic (non hemorrhagic) CVA

Protamine sulfate Irreversibly blocking cyclooxygenase Aspirin, metoprolol GI bleeding Ticlopidine Neutropenia and agranulocytosis Clopidogrel and ticlopidine Dipyridamole Abciximab, tirofiban and eptifibatide Degradation of fibrin clots and are administered IV Pulmonary embolism and DVT Streptokinase Tissue plasmin activator Cerebral hemorrhage Aminocaproic acid Ferrous sulfate Deferoxamine Cyanocobalamin (Vit B12) Vitamin B12 Folic acid Erythropoietin G-CSF (filgrastim) and GM-CSF (sargramostim) Bile acid-binding resins Bile acid-binding resins

SE of tPA Antidote for thrombolytics Agent to treat hypochromic microcytic anemias Chelating agent used in acute iron toxicity Agent for pernicious anemia Agent used for neurological deficits in megaloblastic anemia Agent used for megaloblastic anemia (but does NOT reverse neurologic symptoms) and decrease neural tube defects during pregnancy Agent used for anemias associated with renal failure Agent used neutropenia especially after chemotherapy

Treatment of patients with prior episodes of thrombocytopenia Interleukin 11 (oprelvekin) after a cycle of cancer chemotherapy Drugs decrease intestinal absorption of cholesterol Cholestyramine and colestipol are

Major nutritional side effect of bile acid-binding resins MOA of lovastatin (STATIN) HMG CoA reductase inhibitors are contraindicated in MOA of drug or foods (grapefruit juice) that increase statin effect

Impair absorption of fat soluble vitamin absorption (A,D,E,K) inhibits HMG COA reductase Pregnancy Inhibit Cytochrome P450 3A4 Rhabdomyolysis and Hepatotoxicity LFT's Niacin Cutaneous flush Aspirin

SE of HMG COA reductase inhibitors Monitoring parameter to obtain before initiation of STATINS Decreases liver triglycerol synthesis SE of niacin Cutaneous flush and be reduced by pretreatment with

Fibrates (gemfibrozil) increase activity of Most common SE of fibrates Fibrates are contraindicated in Concurrent use of fibrates and statins increases risk of New class of drugs that works by inhibiting absorption of intestinal cholesterol and can be given concurrently with the Statins MOA of NSAIDS Difference between aspirin and other NSAIDS Four main actions of NSAIDS Agent used for closure of patent ductus arteriosus Aspirin is contraindicated in children with viral infection SE of salicylates NSAID also available as an ophthalmic preparation NSAID available orally, IM and ophthalmically NSAID that is used for acute condition, such as pre-op anesthesia and has limited duration (<5 days) of use due to nephrotoxicity Newer NSAID that selectively inhibits COX-2 COX 2 inhibitors may have reduced risk of COX 2 inhibitors should be used cautiously in pts with Acetaminophen only has SE of acetaminophen Antidote for acetaminophen toxicity DMARDs are slow acting drugs for Initial DMARD of choice for patients with RA Drug ofter used in combination with TNF - alpha inhitors for RA Causes bone marrow suppression SE of penicillamine Interferes with activity of T-lymphocytes Anti-malarial drug used in rheumatoid arthritis (RA) SE of hydroxychloroquine MOA of Leflunomide (newer agent) Proteins that prevent action of tumor necrosis factor alpha (TNF-alpha) Anti-rheumatic agent also used for ulcerative colitis Anti-rheumatic agent also used for Chron's disease

Lipoprotein lipase Nausea Pregnancy Rhabdomyolysis Ezetimibe (Zetia) inhibit prostaglandin synthesis by inhibiting cyclo-oxygenase (cox) Aspirin irreversibly inhibits cyclooxygenase

Anti-inflammatory, analgesia, antipyretic and antiplatelet activity Indomethacin Potential for development of Reye's syndrome Tinnitus, GI bleeding Diclofenac, ketoralac Ketoralac Ketoralac Celecoxib Gastric ulcers and GI Bleeding Pre-existing cardiac or renal disease Antipyretic and analgesic activity Hepatotoxicity N-acetylcysteine Rheumatic disease Methotrexate Methotrexate Methotrexate Aplastic anemia and renal toxicity Hydroxychloroquine Hydroxychloroquine Retinal destruction and dermatitis

Inhibiting dihydroorotate dehydrogenase which leads to decreased pyrimidine synthesis, decreased T cell proliferation and decreased antibody production by B cells Adalimumab, infliximab and etanercept Sulfasalazine Infliximab

NSAID used in gout NSAID contraindicated in gout MOA of colchicine (used in acute gout) SE of colchicine Agent used to treat chronic gout by increasing uric acid secretion and excretion Allopurinol treats chronic gout by decreasing uric acid production by inhibiting Rapid acting insulins that do not self-aggregate Peakless ling acting insulin DOC for paroxysmal supraventricular tachycardia; has high efficacy and short duration of action

Indomethacin Aspirin Selective inhibitor of microtubule assembly Kidney and liver toxicity, diarrhea Probenecid and sulfinpyrazone Xanthine oxidase lispro insulin, aspart insulin, glulisine insulin Insulin glargine Adenosine NPH (NP = neutral protamine) insulin glargine Cinchonism plicamycin

Insulin bound to neutral protamine Insulin that self-aggregates into hexamers Side effect of quinidine characterised by tinnitus, headache, deafness, and (occasionally) anaphylactoid shock

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