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365 Cards in this Set

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Abciximab

Monoclonal antibody that inhibits the binding of platelet glycoprotein IIb/IIIa to fibrinogen




Used to prevent clotting after coronary angioplasty and in acute coronary syndrome




Eptifibatide

GPIIb/IIIa inhibitor

Tirofiban

GP IIb/IIIa inhibitor

Acetaminophen

Antipyretic analgesic




Very weak COX inhibitor w/ no inflammatory properties




Less GI distress than aspirin but dangerous in overdose - Hepatic necrosis




Antidote acetylcysteine

Acetazolamide

Carbonic anhydrase inhibiting diuretic acting in the PCT that produces a NaHCO3 diuresis leading bicarb depletion and metabolic acidosis




Self limited diuretic but persistent bicarb depleting action




Uses - glaucoma and mountain sickness




Toxicity - parastheisas, hepatic encephalopathy





Dorzolamide

Topical analog for glaucoma

Brinzolamide

Topical analog for glaucoma

Acetylcholine

Cholinomimetic prototype




NT in CNS, ENS, all ANS ganglia, parasympathetic synapses, sympathetic postganglionic fibers to sweat glands, and skeletal muscle end plate synapses

Acyclovir

DNA synthesis inhibitor in HSV/VZV




Requires activation by Thymidine kinase




Toxicity - behavioral effects and nephrotoxicity (Crystalluria) but minimal myelosuppression

Famciclovir, Penciclovir, valacyclovir

Similar MOA to Acyclovir with longer half lives

Adenosine

Antiarrhyhtmic (miscellaneous group)




Parenteral only




Hyperpolarizes AV nodal tissue, blocks conduction for 10-15 seconds




Used for nodal reentries




Toxicity - hypotension, flushing, chest pain



Albuterol

Prototypic rapid acting B2 agonist for acute asthma




Toxicity - tachycardia, arrhythmias, tremor

Metaproteronol and Terbutaline

B2 agonists

Formoterol and Salmeterol

Slow acting B2 agonists used for prophylaxis

Alendronate

Bisphosphonate




Chronic treatment with low doses increases bone mineral density and reduces fractures




High doses lower serum calcium




Uses - Osteoporosis and hypercalcemia in Paget's disease and malignancies




Toxicity - esophageal irritation (low doses), Renal dysfunction and osteonecrosis of jaw (high doses)

Etidronate, Pamidronate, Risedronate

Bisphosphate w/ similar action to Alendronate

Allopurinol

Irreversible inhibitor of xanthine oxidase reducing production of uric acid




Uses - gout and adjunct cancer chemotherapy




Inhibits metabolism of purine analogs (mercaptopurine and azathioprine)

Febuxostat

Irreversible inhibitor of xanthine oxidase

Alteplase (t-PA)

Thrombolytic human recombinant tissue plasminogen activator




Used to recanalize occluded blood vessels in acute MI, severe PE, stroke




Toxicity - bleeding

Reteplase and Tenecteplase

Thrombolytic human recombinant tissue plasminogen activator

Streptokinase

Bacterial protein w/ thrombolytic properties

Amiloride

K sparing diuretic blocking epithelial Na channels in collecting tubules




Toxicity - hyperkalemia

Amiodarone

Group 3 (and other groups) antiarrhythmic




Broad spectrum - blocks Na, K, and Ca channels and B receptors




High efficacy and very long half life (weeks to months)




Toxicity - deposits in tissues, skin coloration, hypo/hyperthryoidism, PULMONARY FIBROSIS, and optic neuritis

Amphetamine

Indirect-acting sympathomimetic displaces stored catecholamines in nerve endings




Marked CNS stimulant actions w/ high abuse liability




Uses - ADHD, short term weight loss, narcolepsy




Toxicity - psychosis, HTN, MI, seizures

Ephedrine pseudoephedrine, methylphenidate, tyramine

Indirect acting sympathomimetics that displace catecholamines

Amphotericin B

Antifungal Polyene that binds to ergosterol to disrupt fungal cell membrane permeability




Uses - systemic mycoses




Toxicity - chills and fever, hypotension, nephrotoxicity (dose limiting and less with liposomal forms)

Ampicillin

Penicillin w/ wider spectrum than Penicillin G susceptible to penicillinases unless used w/ sulbactam




Activity similar to Penicillin G plus E coli, H influenzae, P mirabilis, Shigella




Synergy w/ aminoglycosides versus Enterococcus and Listeria




Toxicity - penicillin allergy, GI effects, maculopapular skin rash

Amoxicillin

Greater oral bioavailability than Ampicillin and less GI effects




Used with Clavulanate, a penicllinase inhibitor

Anastrozole

Aromatase inhibitor - prototype inhibitor of the enzyme that converts testosterone to estradiol




Used in estrogen-dependent breast cancer

Letrozole

Aromatase inhibitor

Exemestane

Irreversible aromatase inhibitor

Aspirin

NSAID prototype - inhibits COX1/2 irreversibly




Antiplatelet agent, antipyretic, analgesic, and anti-inflammatory




Toxicity - GI ulcers, nephrotoxicity, rash, hypersensitivity leading to bronchoconstriction, saicyclism.

NSAIDS

ibuprofen, indomethacin, ketorolac, and naproxen

Atenolol

B1 selective blocker with low lipid solubility (less CNS effect)




Uses - HTN, angina




B1 selective blockers start with A-M except for Carteolol, caredilol, and labetalol




Toxicity - asthma, bradycardia, AV block, heart failure

Atropine

Muscarinic cholinoreceptor blocker prototype


- Lipid soluble - CNS effects




Antidote for cholinesterase poisoning




Toxicity - "Red as a beet, dry as a bone, blind as a bat, and mad as a hatter", urinary retention, mydriasis

Cyclopentolate and tropicamide

Antimuscarinics for opthamology




Toxicity - cycloplegia and mydriasis

Gylcopyrrolate

antimuscarinic w/ decreased CNS effects

Baclofen

GABA analog, spasmolytic




orally active




activates GABA-A receptors in spinal cord

Azithromycin

Macrolide antibiotic similar to erythromycin




Greater activity against H influenzae, chlamydiae, and strep




Long half life w/ renal elimination




Toxicity - GI distress but no inhibition of drug metabolism

Clarithromycin

Similar to Azithromycin except shorter half life




Inhibits drug metabolism

Benzotropine

Muscarinic cholinoreceptor blocker




Centrally acting anti-muscarinic prototype for Parkinsonism




Toxicity - excessive antimuscarinic effecs

Botlinum

Toxins produced by Clostridium botulinum


- enzymes that cleave synaptobrevin and block transmitter release from ACh vesicles




Injected to treat muscle spasm, wrinkles, and reduce excessive sweating




Toxicity - Paralysis

Bromocriptine

Ergot derivative prototype dopamine agonist that inhibits prolactin release



Uses - hyperprolactinemia and rarely used for Parkinsonism




Toxicity - CNS , dyskinesias, hypotension




Bupivacaine

Long acting amide local anesthetic prototype




Toxicity - greater cardiovascular toxicity than most local anesthetics

Buprenorphine

Long acting partial agonist of Mu receptors



Analgesic (not equivalent to Morphine)




Effective for detox and maintenance in opiod dependence


Nalbuphine

Mixed agonist/antagonist




activates kappa




weakly blocks Mu

Pentazocine

Mixe agonist/antagonist




Activates kappa




weak Mu antagonist or partial agonist

Bupropion

Antidepressant and used in smoking cessation




MOA uncertain but no direct actions on CNS amines




Toxicity - agitation, anxiety, aggravation of psychosis, and seizures (high doses)

Captopril

ACE inhbitor prototype




Uses - HTN, diabetic nephropathy and heart failure




Toxicity - hyperkalemia, retal renal damage, cough (sore throat)




Other prils - benazepril, enalapril, lisinopril, quinapril

Carbamazepine

Antiseizure drug for tonic-clonic and partial seizures




Blocks Na channels in neuronal membrane




Drug of choice for trigeminal neuralgia




Back up drug in bipolar disorder




Toxicity - CNS depression, myelotoxic, induces liver drug metabolism enzymes, teratogenic

Carvedilol

Adrenoreceptor blocker




Racemic mixture


- 1 isomer is a non-selective B blocker


- other an alpha blocker




Uses - HTN, prolongs survival in HF




Toxicity - cardiovascular depression, asthma




Labetalol has similar MOA

Capsofungin

Antifungal echinocandin prototype




Inhibitor of B1-3 glucan synthesis (cell wall)




Used IV for disseminated Candida and Aspergillus infections




Toxicity - GI effects, flushing, and increases Cyclosporine levels

Cefazolin

First generation Cephalosporin prototype




Bactericidal Beta-Lactam inhibitor of cell wall synthesis




Activity against gram positive cocci, E coli, K pneumoniae




DOES NOT enter CNS




Toxicity - potential allergy, partial cross reactivity w/ penicillins



Ceftriaxone

Third gen cephalosporin




Active against many bacteria including pneumococci, gonococci (drug of choice), and gram negative rods




Enters CNS and is used in bacterial meningitis

Cefotaxime and Ceftazidime

Third gen cephalosporins

Celecoxib

Selective COX-2 inhibitors




Less GI toxicity than non-selective NSAIDs




Toxicity - nephrotoxic and increased risk of Myocardial thrombosis and stroke

Chloramphenicol

Broad spectrum antibiotic that inhibits protein synthesis (50S)




Uses - back up meningitis, anaerobic infections, Salmonella




Toxicity - reversible myelosuppression, aplastic anemia, GRAY BABY SYNDROME

Chloroquine

Antimalarial blood schizonticide used for treatment and prophylaxis in areas in which P falciparum is susceptible




Binds to HEMIN causing dysfunctional cell membranes




Resistance - Efflux via P-glycoprotein




Toxicity - GI distress and skin rash at low doses, peripheral neuropathy, skin lesions, auditory and visual impairment


- quinidine like toxicity at high doses

Chlropheniramine

Antihistamine first generation H1 blocker prototype




Toxicity - less sedation and ANS blocking action than diphenhydramine

Chlorpromazine

Phenothiazine antipsychotic drug prototype


- blocks Dopamine receptors in CNS




Toxicity - Atropine-like effects, EPS dysfunction, hyperprolactinemia, postural hypotension, sedation, seizures (overdose)

Fluphenazine and Trifluoperazine

Phenothiazine antipsychotics

Procholorperazine

Phenothiazine anti-emetic

Promethazine

Phenothiazine pre-operative sedation

Cholestyramine

Antihyperlipidemic




Bile acid binding resin prototype that sequesters bile acids in gut and diverts more cholesterol from the liver to bile acids instead of circulating lipoproteins




Uses - hypercholesterolemia




Toxicity - constipation, bloating, interferes w/ absorption of some drugs

Colestipol and Colesevelam

Similar to Cholestyramine




Bile acid binding resin prototype that sequesters bile acids in gut and diverts more cholesterol from the liver to bile acids instead of circulating lipoproteins

Cimetidine

H2 blocker prototype used in peptic disease




Toxicity - inhibits drug metabolism and anti-androgen effects (gynecomastia)

Ranitidine, Famotidine, Nizatidine

Less toxic H2 blockers

Ciprofloxacin

Second generation fluoroquinolone antibiotc


- Bactericidal inhibitor of topoisomerases




Active against E coli, H influenzae, Campylobacter, Enterobacter, Pseudomonas, Shigella




Toxicity - CNS dysfunction, GI distress, superinfection, collagen dysfunction (caution in children and pregnant women)




Inhibits metabolism of caffeine, theophylline, warfarin

Cisplatin

Anti-neoplastic




Platinum containing alkylating agent




Uses - solid tumors (testes, lung)




Toxicity - Neurotoxic and nephrotoxic

Carboplatin and oxaliplatin

Platinum containing alkylating agent

Clindamycin

Lincosamide antibiotic




BacterioSTATIC inhibitor of protein synthesis (50S)




Active against gram positive cocci, B fragilis




Toxicity - GI distress, pseudomembranous colitis

Clomiphene

Synthetic selective estrogen receptor modulator




Used in infertility to induce ovulation by blocking pituitary estrogen receptors




May result in multiple births



Clonidine

Alpha-2 agonist acts centrally to reduce SANS outflow that lowers BP




Uses - HTN and in drug dependency states




Toxicity - mild sedation in normal doses, rebound HTN if stopped suddenly

Clopidogrel

Antiplatelet agent




Irreversibly inhibits platelet ADP receptors and platelet aggregation




Uses - TIA and to prevent strokes and restenosis after placement of coronary stents




Toxicity - bleeding, neutropenia

Ticlopidine

Antiplatelet agent




Irreversibly inhibits platelet ADP receptors and platelet aggregation




Higher risk of neutropenia and thrombotic thrombocytopenia purpura

Cocaine

Indirect acting sympathomimetic that blocks amine reuptake into nerve endings




Local anesthetic ester type




Marked CNS stimulation, euphoria, high abuse and dependence liability




Toxicity - psychosis, HTN, cardiac arrhythmias, seizures

Colchicine

Microtubule assembly inhibitor that reduces macrophage mobility and phagocytosis




Uses - Chronic gout




Toxicity - GI, hepatic, renal damage

Cyclophosphamide

Antineoplastic, immunosuppressive




Cell cycle non-specific alkylating agent




Toxicity - alopecia, GI distress, hemorrhagic cystitis (mesna), and myelosuppression

Cyclosporine

Immunosuppressant




Immunophilin ligand inhibits T cell synthesis of cytokines




Toxicity - nephrotoxicity, HTN, peripheral neuropathy

Tacrolimus

Immunosuppressant




Immunophilin ligand inhibits T cell synthesis of cytokines




Toxicity - nephrotoxic, HTN, peripheral neuropathy

Sirolimus

Binds to same immunophilin as tacrolimus (FKBP12)




However, this complex inhibits mammalian target of Rapamycin (mTOR) kinase and T cell response to IL-2

Aldesleukin

IL-2 used in renal cancer

EPO

EPO-alpha used in anemias

Filgrastim

G-CSF used in neutropenia

Interferon-alpha

hepatitis B/C and cancer

Interferon-B

Multiple sclerosis

Interferon-gamma

Chronic granulomatous disease

Oprelvekin

IL-1 used in thrombocytopenia

Sargramostim

GM-CSF used in neutropenia

Dantrolene

Muscle relaxant




Blocks Calcium channel release from SR of skeletal muscle




Used in muscle spasm (cerebral palsy, MS, cord injury)




Emergency treatment of malignant hyperthermia

Desmopressin

ADH/Vasopressin analog more selective for V2 receptors




Uses - pituitary diabetes insipidus and mild hemophilia A or Von Willebrand disease

Vasopressin

Agonist at V1 and V2 receptors




Pituitary diabetes insipidus and bleeding esophageal varices

Conivaptan

Antagonist at V1a and V2 receptors




Uses - hyponatremia

Tolvaptan

Antagonist at V2 receptors



Uses - hyponatremia

Diazepam

Benzodiazepine prototype




Binds to BZ receptor on GABA-A receptor chloride ion channel complex




Facilitates the inhibitory actions of GABA by increasing the FREQUENCY of channel opening




Uses - anxiety, ethanol detox, muscle spasticity, status epilepticus




Toxicity - dependence, additive effects w/ other CNS depressants

Alprazolam, Lorazepam, Midazolam Triazolam

Benzodiazepines




Facilitate the inhibitory actions of GABA by increasing the frequency of chloride channel opening

Digoxin

Cardiac glycoside prototype




Positive inotropic drug for HF




Half life - 40 hours




Inhibits Na/K ATPase




Toxicity - calcium overload arrhythmias, GI upset

Diphenhydramine

Antihistamine (1st gen) H1 blocker




Uses - Hay fever, motion sickness, dystonias




Toxicities - antimuscarinic, alpha blockade, strong sedative

Doxylamine

Antihistamine H1 blocker similar to Diphenhydramine

Dopamine

NT and agonist drug and dopamine receptors




Used in shock to increase renal blood flow (low dose) and cardiac output (moderate dose)

Doxorubicin

Antineoplastic




Anthracycline drug - cell cycle non-specific


- Intercalates between base pairs to disrupt DNA functions, inhibits topoisomerases, and forms cytotoxic free radicals




Toxicity - CARDIOMYOPATHY and myelosuppression




Danorubicin is similar

Dexrazoxane

Antidote for Doxorubicin cardiomyopathy

Doxycycline

Tetracycline antibiotic




Protein synthesis inhibitor (30S)




More effective than other tetracyclines against Chlamydia and in Lyme disease, and malaria prophylaxis




Unlike other tetracyclines, it is eliminated in the feces and has longer half life




Toxicity - GI upset and super infections, Fanconis syndrome, photosensitivity, and dental enamel dysplasia

Edrophonium

Cholinesterase inhibitor w/ short duration of action (15 minutes)




Used in diagnosis of Myasthenia gravis and to distinguish myasthenic from cholinergic crisis

Efavirenz

Non-nucleoside reverse transcriptase inhibitor (NNRTI)




Used in combo for HIV




Toxicity - skin rash, CNS effects, avoid in pregnancy

Delaviridine and Nevirapine

Non-nucleoside RTI's

Enfuviritide

Antiviral




HIV fusion inhibitor used in combo regimens




Toxicity - Injection site reactions and rare hypersensitivity

Enoxaparin



Low molecular weight Heparin




Used parenterally for anticoagulation




Primary effect is on factor Xa, less on thrombin




aPTT test is unreliable




Toxicity - bleeding

Dalteparin and Tinzaparin

LMW heparins

Entacapone

COMT inhibitor




Enhances levodopa access to CNS neurons, adjunctive in Parkinson's




Toxicity - exacerbates levodopa effects

Tolcapone

COMT inhibitor




Enhances levodopa access to CNS neurons, adjunctive in Parkinson's




Toxicity - Hepatotoxic

Ephedrine

Indirectly acting sympathomimetic




Like amphetamine but less CNS stimulation, more smooth muscle effects




In botanicals (Ma huang) and products for weight loss that are banned in the US




Toxicity - HTN, stroke

Epinephrine

Adrenoreceptor agonist prototype




Product of adrenal medulla and some CNS neurons




Affinity for all A/B receptors




Drug of choice in anaphylaxis, used as hemostatic and as adjunct to local anesthetics; cardiac stimulant, asthma




Toxicity - tachycardia, HTN, MI, PE, hemorrhage

Ergot Alkaloids

Ergonovine and Ergotamine




Prolonged vasoconstriction and uterine contraction




Used in migraine and obstetrics




Toxicity - vasospasm (including coronaries)

Erythromycin

Macrolide antibiotic - BacterioSTATIC inhibitor of protein synthesis (50S)




Activity includes gram-positive cocci and bacilli, M pneumoniae, Legionella pneumophila, C trachomatis




Toxicity - cholestatic jaundice (avoid estolate in pregnancy), inhibits liver drug metabolizing enzymes




Interactions with cisaparide, theophylline, and warfarin

Azithromycin and Clarithromycin

Macrolide antibiotics (50S) protein synthesis inhibitors

EPO

Hematopoietic growth factor




stimulates RBC production and releases from bone marrow




Used in anemia associated w/ renal failure and anemias secondary to cancer chemotherapy

Darbepoetin alfa

Longer half life version of EPO

Entanercept

DMARD - recombinant protein that binds TNF-alpha




Effective in RA and other chronic inflammatory diseases




Toxicity - Injection site reactions including erythema, itching, and swelling; possible increased rates of infection and malignancy

Infliximab and Adalimumab

recombinant protein that binds to TNF-a




Similar to Entanercept

Ethambutol

Antimycobacterial




Inhibitor of arabinogalactan synthesis, a cell wall component




Commonly used in standard anti-tubercular regimens




Toxicity - dose dependent ocular dysfunction, dizziness, headache, hyperuricemia

Ethanol

Sedative hypnotic




Acute actions include impaired judgement, ataxia, loss of consciousness, and cardiovascular/respiratory depression




Chronic use leads to dependence and dysfunction of multiple organ systems, fetal alcohol syndrome




Note - zero order elimination kinetics

Ethinyl estradiol

Synthetic estrogen - used in hormonal contraceptives




Mestranol has similar MOA

Ethosuximide

Anticonvulsant used in absence seizures




May block T type Ca channels in thalamic neurons




Toxicity - GI distress, SAFE in pregnancy

Ezetimibe

Antihyperlipidemic




Cholesterol lowering drug that inhibits GI transporter of dietary cholesterol and cholesterol secreted in bile




Uses - hypercholesterolemia, usually in combo with a statin




Toxicity - possible increased risk of hepatic damage when combined with statin

Fentanyl

Short acting potent opiod agonist used commonly in anesthesia and chronic pain management (transdermal)

Remifentanil and Sufentanil

Short acting potent opiod agonists used in anesthesia and chronic pain management

Finasteride

Anti-adrogen



steroid inhbitor of 5a-reductase activity that inhibits synthesis of DHT




Used in BPH and male pattern baldness




Dutasteride is similar


Flecainide

Group 1C antiarrhythmic prototype




Used in VENTICULAR tach and rapid atrial arrhythmias w/ Wolff Parkinson White syndrome




Toxicity - arrhythmogenic, CNS excitation

Fluconazole

Imidazole antifungal - inhibits ergosterol synthesis




CNS entry and renal elimination




Used in esophageal and vaginal candidiasis, coccidiomycosis, and in the prophylaxis and treatment of fungal meningitis




Toxicity - hepatic dysfunction, inhibits steroid synthesis and CYP450 dependent drug metabolism (less toxic of azoles)

Fludrocortisone

Synthetic corticosteroid




High mineralocorticoid and moderate glucocorticoid activity




Long duration of action




Used in Addison's disease

Flumazenil

Benzodiazepine receptor antagonist




Used to reverse CNS depressant effects of Benzos, zolpidem, eszopiclone, and zaleplon

Fluorouracil

Anti-neoplastic




Pyrimidine antimetabolite (cell cycle specific) that irreversibly inhibits thymidylate synthase resulting in dTMP deficiency and "thymine less" cell death




Used mainly for solid tumors




Toxicity - GI distress, myelosuppression, neurotoxicity

Fluoxetine

Antidepressant - SSRI prototype




Less ANS adverse effects and cardiotoxic potential than tricyclics




Toxicity - CNS stimulation, sexual dysfunction, seizures in overdose, serotonin syndrome

Citalopram

SSRI

Escitalopram

SSRI

Fluvoxamine

SSRI

Paroxetine

SSRI

Sertraline

SSRI




Zoloft

Flutamide

Anti-androgen




prototype androgen receptor anatagonist used in prostatic carcinoma

Bicalutamide and Nilutamide

androgen receptor antagonist

Furosemide

Loop diuretic prototype




Blocks Na/K/2Cl transporter in TAL




High efficacy, used in acute PE, refractory edematous states, hypercalcemia, and HTN




Toxicity - OTOTOXIC, K wasting, hypovolemia, increased serum uric acid

Bumetanide and Torsemide

Blocks Na/K/2Cl transporter in TAL




High efficacy, used in acute PE, refractory edematous states, hypercalcemia, and HTN




Toxicity - OTOTOXIC, K wasting, hypovolemia, increased serum uric acid




Differ from Furosemide via half lives

Ethacrynic acid

Blocks Na/K/2Cl transporter in TAL




Similar to Furosemide but causes less hyperuricemia and may even reduce uric acid levels

Gabapentin

Anticonvulsant




structural analog of GABA that facilitates its inhibitory actions in the CNS




Used for Partial seizures, for neuropathic pain, and in bipolar disorders




Toxicity - sedation, movement disorders

Ganciclovir

Antiviral




Effective against herpesviruses (CMV) and HSV




CMV Tx requires bioactivation via viral phosphotransferase




Toxicity - myelosuppression, nephrotoxicty, and neurotoxicity

Gemfibrozil

Antihyperlipidemic




Fibrate prototype used for hypertriglyceridemia


- Lowers serum VLDL and triglycerides and increases HDL by activating peroxisome proliferator activated receptor-alpha nuclear receptors




Toxicity - GI distress, cholelithiasis, increased risk of myopathy when combined w/ statins or niacin

Gentamicin

Aminoglycoside prototype




Bacterial inhibitor of protein synthesis (30S)




Active against many aerobic gram negative bacteria




Narrow therapeutic window, dose reduction required in real impairment




Toxicity - NEPHROTOXIC, renal dysfunction, ototoxic




Once daily dosing is effective (post-antibiotic effect) and less toxic

Amikacin and Tobramycin

Aminoglycoside inhibitor of protein synthesis 30S

Glipizide

Oral Antidiabetic - second generation




Potent sulfonylurea secretagogue, Blocks K+ channels in pancreatic B cells causing DEpolarization and release of insulin




Toxicity - hypoglycemia, weight gain

Glyburide, Chlorpropamide, and Tolbutamide

Antidiabetic sulfonylurea



Blocks K+ channels in pancreatic B cells causing depolarization and release of insulin

Short acting sulfonylurea secretagogue

Repaglinide and Nateglinide




Blocks K+ channels in pancreatic B cells causing depolarization and release of insulin

Glucagon

Hormone from pancreatic A cells




Increases blood glucose via increased cAMP




Used in severe hypoglycemia




Antidote - B blocker overdose

Haloperidol

Antipsychotic Butyrophenone




Blocks brain dopamine D2 receptors




Toxicity - marked EPS dysfunction, hyperprolactinemia, fewer ANS side effects than phenothiazines

Halothane

General anesthetic prototype - inhaled halogenated hydrocarbon




Toxicity - cardiovascular and respiratory depression and relaxation of skeletal and smooth muscle




Use is declining because of sensitization of heart to catecholamines and rare occurrence of hepatitis

Isoflurane and Sevoflurane

Inhaled halogenated hydrocarbon

Heparin

Anticoagulant - Large polymeric molecule w/ activity against thrombin and factor X




Rapid onset, parenteral admin




Toxicity - bleeding

Heparin overdose

Protamine

LMW heparins Enoxaparin and Fondaparinux

more selective for Factor X

Hexamethonium

Prototypic ganglion blocker, no longer used




Causes marked blockade of PANS/SANS, hypostension




Trimethaphan and Mecamylamine are alternatives but also rarely used

Hydralazine

Antihypertensive - arteriolar vasodilator, orally active




Uses - severe HTN and HF




Toxicity - tachycardia, salt and water retention, lupus like syndrome

Minoxidil

Arteriolar dilator w/ more powerful anti-hypertensive properties




Also used in male pattern baldness




Uses - severe HTN and HF




Toxicity - tachycardia, salt and water retention

Hydrochlorothiazide

Thiazide diuretic prototype



Acts in DCT to block Na/Cl transporter




Uses - HTN, HF, nephrolithiasis




Toxicity - hypersensitivity reactions, increased serum lipids, uric acid, glucose, K wasting



Hydroxychloroquine

DMARD immunosuppresant used for RA




Toxicity - rash, GI distress, ocular toxicity, myopathy, neuropathy

Methotrexate

DMARD

Sulfasalazine

DMARD

Gold salts

DMARD

Penicillamine

DMARD

Ibuprofen

NSAID - non-selective COX inhibitor w/ analgesic, anti-pyretic, and anti-inflammatory actions similar to aspirin




No low dose anti-platelet effect

Imipenem

Prototype carbapenem antibiotic




Active against many aerobic and anaerobic bacteria including penicilliinase producing organisms (bactericidal inhibitor of cell wall synthesis)




Used w/ cilastatin (inhibits metabolism by renal dehydropeptidases




Toxicity - allergy (partial cross reactivity w/ penicillins), seizures

Meropenem and Ertapenem

Carbapenem antibiotic, bactericidal inhibitor of cell wall synthesis




DO NOT require cilasatin and are less likely to cause seizures

Imipramine

TCA - blocks reuptake of NE and 5-HT




Toxicity - atropine like, postural hypotension, sedation, cardiac arrhythmias, in overdose, additive effects w/ other CNS depressants

Amitriptyline

TCA - blocks reuptake of NE and 5-HT

Clomipramine

TCA - blocks reuptake of NE and 5-HT

Doxepin

TCA - blocks reuptake of NE and 5-HT

Indinavir

HIV protease inhibitor used as a component of combo regimens in AIDS




Toxicity - anemia, nephrolithiasis, metabolic disorders, inhibits P450 drug metabolism

Amprenavir

HIV protease inhibitors


- major P450 inhibitor

Nelfinavir

HIV protease inhibitor


- major P450 inhibitor

Ritonavir

HIV protease inhibitor


- major P450 inhibitor

Saquinavir

HIV protease inhibitor

Indomethacin

NSAID - highly potent




Usually reserved for acute inflammation (acute gout), neonatal PDA




Toxicity - GI and renal damage

Interferon alpha

Cytokine




Treatment for Hep B/C and some malignancies




Toxicity - flu like syndrome, myelosuppression, and neurotoxicity

Ipratropium

Antimuscarinic agent




aerosol for asthma and COPD, bronchodilator




Not as efficacious as B2 agonists but less toxic in COPD




Toxicity - dry mouth

Tiotropium

Antimuscarinic agent




aerosol for asthma and COPD w/ longer duration of action




Not as efficacious as B2 agonists but less toxic in COPD




Toxicity - dry mouth

Isoniazid

Antimycobacterial




Primary drug in combo regimens for TB, used as sole agent in latent infection




Metabolic clearance via N-acetyltransferases




Toxicity - hepatotoxicity, peripheral neuropathy (reversed by pyridoxine), hemolysis in G-6PD deficiency

Isoproterenol

Beta1/Beta2 agonist catecholamine prototype




Bronchodilator and cardiac stimulant




Always causes tachycardia because both direct and reflex actions increase HR




Toxicity - arrhythmias, tremor, angina

Ivermectin

Antihelminthic




Drug of choice for onchocerciasis and threadworm infections




Intensifies GABA mediated neurotransmission in nematodes but no access to CNS in humans




Toxicity - onchocerciasis causes headache, fever, hypotension and joint pain

Ketoconazole

Antifungal azole prototype - active systemically




Inhibits the synthesis of ergosterol




Uses - C ablican, dermatophytosis and non-life threatening systemic mycoses. Sometimes used to suppress adrenocorticoid or gonadal hormone synthesis




Toxicity - hepatic dysfunction, inhibits steroid synthesis, and CYP-450 drug dependent metabolism

Fluconazole, Itraconazole, Voriconazole

Inhibit synthesis of ergosterol




Wider spectrum and less inhibitory effects on hepatic cytochromes P450

Ketorolac

NSAID




Mainly used as a systemic analgesic




Only NSAID available in parenteral form

Lamivudine

Nucleoside reverse transcriptase inhibitor also known as 3TC




Least toxic NRTI




Uses - Chronic Hep B and HIV

Lamotrogine

Anti-epileptic drug for absence and partial seizures



Also used in bipolar disorder




Toxicity - rash, possibly life threatening in pediatric patients


Latanoprost

Prostaglandin F2a analog used topically in closed angle glaucoma




Bimatoprost and Travoprost

Lepirudin

Anti-thrombotic




Recombinant form of a medical leech protein that directly inhibits thrombin




Rapid onset, parenteral admin




Used in heparin induced




Toxicity - bleeding, monitor with aPTT

Bivalirudin

Recombinant form of medical leech protein that directly inhibits thrombin




Used for PCI

Argatroban

Small molecule anti-thrombotic used parenterally for PCI

Dabigatran

Oral thrombin inhibitor

Leuprolide

GnRH analog




Continuous therapy used to suppress gonadotropin and gonadal hormone synthesis, especially in concert w/ gonadotropins for ovulation induction and in advanced prostate cancer

Goserelin and Nafarelin

GnRH analog



Continuous therapy used to suppress gonadotropin and gonadal hormone synthesis, especially in concert w/ gonadotropins for ovulation induction and in advanced prostate cancer

Levodopa

Dopamine precursor




Used in parkinsonism, usually in combination w/ carbidopa (peripheral inhibitor of dopamine metabolism)




Toxicity - dyskinesias, hypotension, on-off phenomenon, behavioral changes

Levofloxacin

Fluoroquinolone - Bactericidal inhibitor of topoisomerases




Respiratory fluoroquinolones including gemifloxacin and moxifloxacin w/ greater activity than ciproflaxin against pneumococci




Toxicity - CNS dysfunction, GI distress, superinfection, collagen dysfunction

Levonorgestrel

Progestin


- combined oral contraceptives


- progestin only contraceptives


- levonorgestrel IUD


- subcutaneous implants


- Plan B

Lidocaine

Amide local anesthetic, medium duration amide prototype, Parenteral only




Highly selective use dependent group 1B anti-arrhyhtmic




Used for nerve block and acute post MI ischemic ventricular arrhythmias




Toxicity - CNS excitation

Mexiletine

Amide local anesthetic




Highly selective use dependent group 1B anti-arrhythmic




Used for nerve block and acute post MI ischemic ventricular arrhythmias




Toxicity - CNS excitation




Longer duration and orally active

Lithium

Antimanic prototype




Primary drug in mania and bipolar affective disorders




Blocks recycling of phosphatidylinositol second messenger system




Toxicty - tremor, diabetes insipidus, goiter, siezures in overdose

Loratadine

Second generation H1 anti-histamine




used in hay fever




Toxicity - much less sedation than first generation antihistamines, no ANS effects

Desloratadine

Second gen H1 anti-histamine

Cetirizine

Second gen H1 anti-histamine

Fexofenadine

Second gen H1 anti-histamine

Losartan

Angiotensin AT1 receptor blocker




Uses - HTN




Effects and toxicity similar to ACE inhibitors but less cough

Candesartan

Angiotensin AT1 receptor blocker

Eprosartan

Angiotensin AT1 receptor blocker

Irbesartan

Angiotensin AT1 receptor blocker

Olmesartan

Angiotensin AT1 receptor blocker

Telmisartan

Angiotensin AT1 receptor blocker

Valsartan

Angiotensin AT1 receptor blocker

Lovastatin

Antihyperlipidemic




HMG-CoA reductase inhibitor prototype used for hypercholesteremia




Acts in liver to reduce synthesis of cholesterol and indirectly increase LDL receptor synthesis




Toxicity - hepatotoxicity, muscle damage, teratogen

Atorvastatin

HMG-CoA reductase inhibitor

Fluvastatin

HMG-CoA reductase inhibitor

Pravastatin

HMG-CoA reductase inhibitor

Rosuvastatin

HMG-CoA reductase inhibitor

Simvastatin

HMG-CoA reductase inhibitor

Malathion

Organophosphate insecticide cholinesterase inhibitor




Prodrug converted to malaoxon




Less toxic in mammals and birds because metabolized to inactive products

Parathion

Organophosphate insecticide cholinesterase inhibitor




Prodrug converted to paraoxon

Nerve gases

Sarin and soman gases




Organophosphate insecticide cholinesterase inhibitors

Mannitol

Osmotic diuretic




Used short term for reduction of intracranial pressure to promote excretion of renal toxins in hemolysis, rhabdomyolysis




Toxicity - Initial expansion of ECF volume w/ resulting hyponatremia, headache, nausea




With excessive use, dehydration and hypernatremia

Mebendazole

Anti-helminithic




Common nematode infections




Inhibits microtubule synthesis and glucose uptake in nematodes




Toxicity - GI distress, caution in pregnancy

Albendazole

widely used anti-helminthic for nematode infections

Thiabendazole

More toxic anti-helminthic for nematode infections

Medroxyprogesterone

Progestin




Used in combo with an estrogen for treatment of menopausal symptoms and used as a long acting injection (Depo-Provera) for contraception

Mefloquine

Anti-malarial - unkown MOA




Used for prophylaxis against and treatment of choloroquine resistant malaria




Toxicity - GI distress, dizziness, seizures in ovrdose, arrhythmias

Meperidine

Opiod analgesic - synthetic, orally bioavailable equivalent to morphine




Strong agonist at Mu receptors, blocks muscarinic receptors, serotonergic activity




Toxicity - normeperidine accumulation may cause seizures, serotonin syndrome w/ SSRIs

Metformin

Oral anti-diabetic - prototype Biguanide




Inhibits hepatic and renal gluconeogenesis, minimal hypoglycemia or weight gain




Toxicity - GI distress, lactic acidosis possible but rare

Methadone

Opiod analgesic




Synthtic mu agonist, equivalent to morphine in efficacy but orally bioavailable w/ a longer half life




Used as analgesic, to suppress withdrawl symptoms, and in maintenance programs




Toxicity - constipation, emesis, sedation, respiratory depression, miosis, and urinary retention

Methotrexate

Anti-neoplastic, DMARD, immunosuppressant


Cell cycle specific drug that inhibits dihydrofolate reductase




Major dose reduction required in renal impairment




Toxicity - Gi distress, myelosuppression, and crystalluria




Leucovorin rescue used to reduce toxicity




Leucovorin

Rescue used to reduce methotrexate toxicity

Methimazole

Anti-thyroid drug




Inhibits tyrosine iodination and coupling reactions, orally active




Toxicity - rash, agranulocytosis

Propylthiouracil

Anti-thyroid drug




Inhibits tyrosine iodination and coupling reactions




Toxicity - rash and agranulocytosis

Methyldopa

Anti-hypertensive




Prodrug of methylnorepinephrine - CNS alpha-2 agonist




Reduces SANS outflow from vasomotor center


- similar activity to clonidine




Toxicity - positive Combs test, sedation, hemolysis

Metoclopramide

Prokinetic agent




Dopamine D2 receptor agonist used to stimulate upper GI motility in patients w/ gastroparesis and used as an anti-emetic




Toxicity - restlessness, insomnia, agitation, extrapyramidal effects, elevated prolactin

Metronidazole/Tinidazole

Antiprotozoal antibiotic




Drug of choice in extraluminal amebiasis and trichomoniasis




Effective against bacterial anaerobes (B fragilis) and in antibiotic induced colitis (C diff)




Toxicity - peripheral neuropathy, GI distress, ethanol intolerance, mutagenic potential

Mifepristone

Progestin and glucocorticoid receptor antagonist




Used in prostagandin analogs for medical abortion in early pregnancy

Misoprostol

Prostaglandin E1 derivative




Orally active prostaglandin used to prevent GI ulcers caused by NSAIDs




Also used w/ Mifepristone as abortion drug




Toxicity - minimal

Motelukast

Leukotriene receptor blocker (LTD4) used for prophylaxis in asthma




Orally active, once daily admin

Zafirulkast

Leukotrience receptor blocker (LTD4) used for asthma

Morphine

Opiod analgesic prototype - strong Mu agonist


- poor bioavailability




Toxicity - constipation, emesis, sedation, respiratory depression, miosis, and urinary retention




Tolerance may be marked, high potential for psychological and physiologic dependence




Additive effects w/ other CNS depressants

Nafcillin

Penicillinase-resistant penicillin


- narrow spectrum used for suspected or known staph infections (not active against MRSA)




Toxicity - penicillin allergy

Methicillin

Penicillinase resistant penicillin


- resistance in MRSA


- prototype

Oxacillin

Penicillinase resistant penicillin for staph infections

Claxacillin

Penicillinase resistant penicillin for staph infections

Dicloxacillin

Penicillinase resistant penicillin for staph infections

Naloxone

Opiod Mu receptor antagonist




Used to reverse CNS depressant effects of Opiod analgesics (overdose or when used in anesthesia)

Naltrexone

Orally active, related to Naloxone




Used in ethanol dependency states

Neostigmine

Cholinesterase inhibitor - prototype synthetic quarternary nitrogen carbamate w/ little CNS effects




Toxicity - excess cholinomimetic effects

Pyridostigmine

Cholinesterase inhibitor - prototype synthetic quarternary nitrogen carbamate w/ little CNS effects



Toxicity - excess cholinomimetic effects




Longer duration than Neostigmine

Physostigmine

Lipid soluble plant alkaloid




Cholinesterase inhibitor




Toxicity - excess cholinomimetic effects





Echothiophate

Rarely used organophosphate cholinesterase inhibitor for topical opthalmic use

Niacin

Anti-hyperlipidemic




Inhibits VLDL synthesis and release of fatty acids from adipose tissue




Lowers LDL cholesterol and triglycerides and raises HDL cholesterol




Toxicity - flushing, pruritus, liver dysfunction, increased risk of myopathy when combined with statins

Nifedipine

Dihydropyridine calcium channel blocker


prototype used in angina and HTN




Less cardio-depressant than verapamil and diltiazem




Toxicity - constipation, headache, tachycardia, arrhythmias

Amlodipine, Felodipine, Nicardipine

Dihydropyridine calcium channel blocker prototype used in angina and HTN

Nitric Oxide

Endogenous vasodilator released from vascular endothelium, NT




Mediates vasodilating effect of ACh, histamine, and hydralazine




Active metabolite of nitroprusside and of nitrates used in angina




Used as a pulmonary dilator in neonatal hypoxia, pulmonary HTN




Toxicity - excessive vasodilation and hypotension

Nitrogylcerin

Antianginal vasodilator prototype




Releases NO in veins, less in arteries, and causes smooth muscle relaxation




Standard of therapy in angina (atherosclerotic and variant)




Toxicity - tachycardia, hypotension, headache

Isosorbide dinitrate, isosorbide mononitrate

Oral nitrates




Releases NO in veins, less in arteries, and causes smooth muscle relaxation

Norepinephrine

Adrenoceptor agonist prototype, NT



Acts at all alpha adrenoceptors and B1 adrenoceptors used as a vasoconstrictor




Causes reflex bradycardia




Toxicity - ischemia, arrhythmias, HTN


Olanzapine

Atypical anti-psychotic




High affinity antagonist at 5-HT2a receptors w/ minimal extrapyramidal side effects




Improves both positive and negative symptoms of schizophrenia

Quetiapine

Atypical anti-psychotic - short half life




High affinity antagonist at 5-HT2a receptors w/ minimal extrapyramidal side effects




Improves both positive and negative symptoms of schizophrenia

Risperidone

Atypical anti-psychotic - less EPS effects




High affinity antagonist at 5-HT2a receptors w/ minimal extrapyramidal side effects




Improves both positive and negative symptoms of schizophrenia

Sertindole

Atypical anti-psychotic - QT prolongation




High affinity antagonist at 5-HT2a receptors w/ minimal extrapyramidal side effects




Improves both positive and negative symptoms of schizophrenia

Clozapine

Atypical anti-psychotic - agranulocytosis




High affinity antagonist at 5-HT2a receptors w/ minimal extrapyramidal side effects




Improves both positive and negative symptoms of schizophrenia

Omeprazole

Proton pump inhibitor prototype


- Irreversible blocker of H/K ATPase proton pump in parietal cells of stomach




Used in GI ulcers, Zollinger-Ellison syndrome, GERD

Esomeprazole

Proton pump inhibitor prototype


- Irreversible blocker of H/K ATPase proton pump in parietal cells of stomach




Used in GI ulcers, Zollinger-Ellison syndrome, GERD

Dexlansoprazole

Proton pump inhibitor prototype


- Irreversible blocker of H/K ATPase proton pump in parietal cells of stomach




Used in GI ulcers, Zollinger-Ellison syndrome, GERD

Lansoprazole

Proton pump inhibitor prototype


- Irreversible blocker of H/K ATPase proton pump in parietal cells of stomach




Used in GI ulcers, Zollinger-Ellison syndrome, GERD

Pantoprazole

Proton pump inhibitor prototype

- Irreversible blocker of H/K ATPase proton pump in parietal cells of stomach




Used in GI ulcers, Zollinger-Ellison syndrome, GERD



Rabeprazole

Proton pump inhibitor prototype


- Irreversible blocker of H/K ATPase proton pump in parietal cells of stomach




Used in GI ulcers, Zollinger-Ellison syndrome, GERD

Ondanestron

5-HT3 receptor blocker prototype




Important anti-emetic for cancer chemotherapy, used post-operatively to reduce vomiting




Toxicity - extrapyramidal effects

Dolasetron

5-HT3 receptor blocker prototype



Important anti-emetic for cancer chemotherapy, used post-operatively to reduce vomiting




Toxicity - extrapyramidal effects

Granisetron

5-HT3 receptor blocker prototype




Important anti-emetic for cancer chemotherapy, used post-operatively to reduce vomiting




Toxicity - extrapyramidal effects

Palonosetron

5-HT3 receptor blocker prototype




Important anti-emetic for cancer chemotherapy, used post-operatively to reduce vomiting




Toxicity - extrapyramidal effects

Oseltamivir

Antiviral




Neuraminidase inhibitor blocking release of mature virions of Flu A and B and decreasing their infectivity




Prophylactic and shortens duration of flu symptoms

Zanamivir

Antiviral



Neuraminidase inhibitor blocking release of mature virions of Flu A and B and decreasing their infectivity




Prophylactic and shortens duration of flu symptoms

Oxybutynin

Muscarinic cholinoceptor blocker




Relieves bladder spasm and incontinence

Tolterodine

Muscarininc cholinoceptor blocker




Relieves bladder spasm and incontinence




Weak but more selective for M3 receptors

Paclitaxel

Antineoplastic plant alkaloid




Cell cycle (M phase) specific agent




Inhibits mitotic spindle disassembly




Toxicity - hematotoxicity, peripheral neuropathy, hypersensativity reactions

Docetaxel

Antineoplastic plant alkaloid




Cellc cycle (M phase specific agent




Inhibits mitotic spindle disassembly




Toxicity - hematotoxicity, peripheral neuropathy, hypersensativity reactions

Penicillinamine

Chelator, Immunomodulator




Treatment of copper poisoning and Wilson's disease




Formerly used in RA

Penicillin G

Penicillin prototype - penicillinase suscpeptible




Active against strep, gram positive bacilli, gram negative cocci, spirochetes, and enterococci (if used w/ aminoglycoside)




Toxicity - penicillin allergy

Phenelzine

Irreversible nonselective MOA inhibitor




Backup drug for atypical depression




Toxicity - Malignant HTN w/ indirect acting sympathomimetics and tyramine, serotonin syndrome w/ serotonergic drugs

Phenobarbital

Long acting barbiturate used as a sedative and for tonic-clonic seizures




Facilitates GABA mediated neuronal inhibition increasing DURATION of chloride channel opening and may block excitatory NT's




Partial renal clearance that can be increased by urinary ALKALINIZATION




Chronic use leads to induction of liver drug metabolizing enzymes and ALA synthase




Toxicity - psychological and physiologic dependence, additive effects w/ other CNS depressants

Phenoxybenzamine

Alpha blocker prototype (non-selective)


- irreversible action




Used in pheochromocytoma




Toxicity - excessive hypotension

Phentolamine

Alpha blocker (non-selective) w/ irreversible competitive action




Used in pheochromocytoma




Toxicity - excessive hypotension

Phenytoin

Anticonvulsant


- Used for tonic-clonic and partial seizures




Blocks Na channels in neuronal membranes




Serum levels variable because of first pass metabolism and non-linear elimination kinetics




Toxicity - sedation, diplopia, gingival hyperplasia, hirsutism, teratogenic potential (fetal hydantoin sydrome)




Interactions via effects on plasma protein binding or induction of hepatic metabolism

Pilocarpine

Muscarinic receptor partial agonist prototype


- tertiary amine alkaloid




May cause paradoxic HTN by activating muscarinic excitatory post-synaptic neurons in post-ganglionic sympathtic neurons




Used in Sjorgrens syndrome, xerostomia, glaucoma




Toxicity - muscarinic excess





Piperacillin

Extended spectrum penicillin active against selected gram negative bacteria


- Pseudomonas aeruginosa (syngeristic w/ aminoglycosides)




Susceptible to penicillinases unless used w/ Tazobactam




Toxicity - penicllin allergy

Pralidoxime

Acetylcholinesterase regenerator




Antidote w/ atropine for organophosphate poisoning




Chemical antagonist w/ very high affinity for phosphorus in organophosphates




Toxicity - neuromuscular weakness

Pramipexole

Dopamine D3 receptor agonist in CNS


- Often a first line drug in Parkinsonism




Toxicity - postural hypotension, dyskinesias




Less toxicity than ergot bromocriptine

Ropinirole

Dopamine D3 receptor agonist in CNS




Toxicity - postural hypotension, dyskinesias




Less toxicity than ergot bromocriptine

Praziquantel

Antihelminthic for Trematode (fluke) and cestode (tapeworm)




Increases membrane permeability to Ca2+ causing muscle contraction followed by paralysis




Toxicity - headache, dizziness, GI distress, fever, potential abortion drug

Prazosin

Alpha-1 selective blocker prototype




Used in HTN and BPH




Toxicity - first dose orthostatic hypotension but less reflex tachycardia than non-selective alpha blockers

Terazosin

Alpha-1 selective blocker prototype



Used in HTN and BPH




Toxicity - first dose orthostatic hypotension but less reflex tachycardia than non-selective alpha blockers

Doxazosin

Alpha-1 selective blocker prototype




Used in HTN and BPH




Toxicity - first dose orthostatic hypotension but less reflex tachycardia than non-selective alpha blockers

Tamulosin

Alpha 1 selective blocker




Used in BPH

Prednisone

Glucocorticoid prototype

- potent, short acting


- less mineralocorticoid activity than cortisol but more than dexamethasone, bethamethasone, triamcinolone



Probenecid

Uricosuric - inhibitor of renal weak acid secretion and reabsorption in PCT




Prolongs half-life of some antimicrobial drugs, accelerates clearance of uric acid




Used in gout

Sulfinpyrazole

Uricosuric - inhibitor of renal weak acid secretion and reabsorption in PCT




Prolongs half life of come antimicrobial drugs, accelerates clearance of uric acid




Used in gout

Procainamide

Group 1A antiarrhytmic drug prototype




Short half life metabolized by N-acetyltransferase




Toxicity - may cause a Lupus like syndrome and torsades de pointes arrhythmias, Cardiodepressant

Quinidine

Group 1A antiarrhytmic drug



Short half life metabolized by N-acetyltransferase




Toxicity - may cause a Lupus like syndrome and torsades de pointes arrhythmia

Propanolol

Non-selective B blocker prototype




Local anesthetic action but no partial agonist effect




Used in HTN, angina, arrhythmias (group 2), migraine, hyperthryoidism, and tremor




Toxicity - asthma, AV block, HF

Prostacyclin

PGI2 - endogenous prostaglandin vasodilator and inhibitor of platelet aggregation

Epoprostenol

PGI2 analog - used in pulmonary HTN

Pyrimethamine

Antiprotozaol - antifolate that inhibits DHF reductase and synergistic, via sequential blockade, w/ sulfadiazine against T gondii




Folinic acid is needed to offset hematologic toxicity

Quinine

Antimalarial - Blood schizonticide w/ no effect on liver stages




Interferes with nucleic acid metabolism in plasmodium




Toxicity - Cinchonism

Ramelteon

Hypnotic agonist at brain melatonin receptors, not a controlled substance




Toxicity - fatigue, increased prolactin, and decreased testosterone

Reserpine

Antihypertensive




Selective inhibitor of vesicle catecholamine H antiporter (VMAT)




Obsolete use in HTN, causes depletion of catecholamines and 5-HT from their stores




Toxicity - severe depression, suicide, ulcers, diarrhea

Rifampin

Antimicrobial inhibitor of DNA dependent RNA polymerase used in TB drug regimens and meningococcal carrier state



Toxicity - hepatic dysfunction, induction of liver drug metabolizing enzymes (drug interactions), flu like syndromes with intermittent dosing


Rifabutin

Antimicrobial inhibitor of DNA dependent RNA polymerase used in TB drug regimens and meningococcal carrier state




Less toxicity and drug interactions than Rifampin

Ritonavir

Antiviral HIV protease inhibitor


- used at low dose as a component combination regimens in AIDS to inhibit metabolism of other drugs (Indinavir)




Toxicity - implicated in many drug interactions when used as a sole protease inhibitor

Rosiglitazone

Oral antidiabetic - thiazolidinedione stimulator of peroxisome proliferator activator receptors (PPAR) and enhances target tissue sensitivity to insulin




Less hypoglycemia and weight gain than secretagogues antidiabetics




Toxicity - fluid retention, heart failure, fractures in women

Pioglitazone

Oral antidiabetic - thiazolidinedione stimulator of peroxisome proliferator activator receptors (PPAR) and enhances target tissue sensitivity to insulin



Less hypoglycemia and weight gain than secretagogues antidiabetics




Toxicity - fluid retention, heart failure, fractures in women

Rivaroxaban

Oral factor X inhibitor



Prevention of DVT, PE, post surgery, and stroke in A fib.




Fixed doses, no routine monitoring




Side effect - bleeding w/ no specific reversal agent




Selegiline

MAO-B inhibitor - selective inhibitor of enzyme that metabolizes dopamine (no tyramine interactions at normal dosage)




Used in Parkinson's




Toxicities - GI distress, CNS stimulation, dyskinesias, serotonin syndrome if used w/ SSRIs

Rasagiline

MAO-B inhibitor - selective inhibitor of enzyme that metabolizes dopamine (no tyramine interactions at normal dosage)



Used in Parkinson's (more common than Selegiline)




Toxicities - GI distress, CNS stimulation, dyskinesias, serotonin syndrome if used w/ SSRIs

Sildenafil

Inhibits Phosphodiestrase (PDE-5) preventing breakdown of cyclic guanosine monophosphate, which promotes vasodilation and smooth muscle relaxation




Used for ED and Pulmonary HTN




Toxicity - severe hypotension when combined with nitrates, impaired blue-green vision

Tadalfil

Inhibits Phosphodiestrase (PDE-5) preventing breakdown of cyclic guanosine monophosphate, which promotes vasodilation and smooth muscle relaxation




Used for ED and Pulmonary HTN




Toxicity - severe hypotension when combined with nitrates, impaired blue-green vision

Vardenafil

Inhibits Phosphodiestrase (PDE-5) preventing breakdown of cyclic guanosine monophosphate, which promotes vasodilation and smooth muscle relaxation




Used for ED and Pulmonary HTN




Toxicity - severe hypotension when combined with nitrates, impaired blue-green vision

Sotalol

Group 3 antiarrhythmic prototype




Blocks I-K channels and B receptors




Used for atrial and ventricular arrhythmias




Toxicity - Torsades de pointes

Ibutilide

Group 3 antiarrhythmic prototype



Blocks I-K channels and B receptors




Used for atrial and ventricular arrhythmias




Toxicity - Torsades de pointes

Dofetilide

Group 3 antiarrhythmic prototype




Blocks I-K channels and B receptors




Used for atrial and ventricular arrhythmias




Toxicity - Torsades de pointes

Spironolactone

Aldosterone receptor antagonist




K sparing diuretic action in the collecting tubules




Used in aldosteronism, HTN, and female hirsutism (androgen receptor blocking action)




Toxicity - hyperkalemia, gynecomestia

Eplerenone

More selective aldosterone antagonist




Used in HTN and Heart failure

Streptogramins

Antibiotics - Synercid is the combination of quinupristin and dalfopristin




Bactericidal inhibitors of protein synthesis




IV use for drug resistant gram positive cocci including MRSA, VRE, and pneumococci




Toxicity - Infusion related pain, arthralgia, myalgia





Linezolid

Inhibitor of protein synthesis used for drug resistant gram positive cocci, including PRSP strains

Succinylcholine

Depolarizing neuromuscular relaxant prototype




Short duration (5 minutes) if patient has normal plasma cholinesterase




No antidote




Implicated in malignant hyperthermia

Sulfasalazine

5-Aminosalicyclate (5-ASA) anti inflammatory drug




Used for IBS and RA




Toxicity - rash, GI distrubances, leukopenia

Mesalamine

5-Aminosalicyclate (5-ASA) anti inflammatory drug




Used for IBS




Toxicity - rash, GI distrubances, leukopenia

Balsalazide

5-Aminosalicyclate (5-ASA) anti inflammatory drug




Used for IBS




Toxicity - rash, GI distrubances, leukopenia

Olsalazine

5-Aminosalicyclate (5-ASA) anti inflammatory drug




Used for IBS




Toxicity - rash, GI distrubances, leukopenia

Sumatriptan

5-HT1D receptor agonist used to abort migraine attacks




Toxicity - coronary vasospasm, chest pain, or pressure




Six other triptans are currently available

Tamoxifen

Selective estrogen receptor modulator (SERM)


- blocks estrogen receptors in breast tissue and activates endometrial receptors




Used in estrogen positive receptor positive cancers, possibly prophylaxis in high risk patients





Toremifene

Selective estrogen receptor modulator (SERM)

- blocks estrogen receptors in breast tissue and activates endometrial receptors




Used in estrogen positive receptor positive cancers, possibly prophylaxis in high risk patients

Raloxifene

Selective estrogen receptor modulator (SERM)

- blocks estrogen receptors in breast tissue and activates endometrial receptors




Approved for Osteoporosis, activates bone estrogen receptors but is an antagonist of breast and endometrial receptors

Terbinafine

Antifungal




Fungicidal inhibitor of squalene epoxidase




Most effective agent in onychomycosis with oral and topical forms




Toxicity - GI upset, headache, rash



Tetracycline

BacterioSTATIC inhibitor of protein synthesis (30S)




Broad spectrum but many resistant organisms


- Mycoplasmal, chlamydial, rickettsial infections, chronic bronchitis, acne, cholera, a back up drug for syphilis




Toxicity - GI upset and superinfections, Fanconi's syndrome, photosensitivity dental enamel dysplasia




Doxycline and Tigecycline (IV) are used for multidrug resistant nosocomial pathogens

Theophylline

Methylxanthine derivative found in tea



Used in asthma




Bronchodilator and mild CNS stimulant




Caffeine and theobromine are similar



Trimethoprim-Sulfamethoxazole (TMP-SMX)

Antimicrobial drug combination causes synergistic sequential blockade of folic acid synthesis




Active against many gram negative bacteria


- Aeromonas, Enterobacter, H influenze, K pneumoniae, Moraxella, Salmonella, Serratia, and Shigella




Toxicity - mainly due to sulfonamides and includes hypersensitivity, myelotoxity, kernicterus, and drug interactions caused by competition for plasma protein binding

Tubocurarine

Nondepolarizing neuromuscular blocking agent prototype


- competitive nicotinic blocker




Analogs


- Pancuronium, Atracurium, Vecuronium




Toxicity - respiratory paralysis




Releases histamine and may cause hypotension therefore rarely used

Tubocurarine antidote

Cholinesterase inhibitor - neostigmine

Tyramine

Indirect acting sympathomimetic prototype




Releases or displaces NE from stores in nere endings




Presence in certain foods may cause potentially lethal HTN responses in patients taking MAO-I's

Valproic Acid

Anticonvulsant used in absence, clonic-tonic, and myoclonic seizure states




Also used for bipolar disorder




Toxicity - GI distress, hepatic necrosis, teratogenic (spina bifida), inhibits drug metabolism

Vancomycin

Glycopeptide bactericidal antibiotic




Inhibits synthesis of cell wall precursor molecules




A drug of choice for MRSA and effective in antibiotic induced colitis




Dose reduction required in renal impairment or hemodialysis




Toxicity - OTOTOXIC, hypersensitivity, renal dysfunction

Verapamil

Calcium channel blocker prototype


- Blocks L type channels


- Cardiac depressant and vasodilator




Uses - HTN, angina, arrhythmias (group 4)




Toxicity - AV block, HF, constipation

Diltiazem

Calcium channel blocker prototype

- Blocks L type channels


- Cardiac depressant and vasodilator




Uses - HTN, angina, arrhythmias (group 4)




Toxicity - AV block, HF, constipation, more cardiodepressant than verapamil

Vincristine

Antineoplastic cell cycle (M specific) plant alkaloid




Inhibits mitotic spindle formation




Toxicity - peripheral neuropathy

Vinblastine

Antineiplastic cell cycle (M specific) plant alkaloid




Inhibits mitotic spindle formation




Toxicity - myelosuppression

Warfarin

Oral anticoagulant prototype


- causes synthesis of non-functional vitamin K dependent clotting factors (II, VII, IX, XI)




Toxicity - bleeding, teratogenic

Warfarin Antidote

Vitamin K, fresh plasma

Zidovudine

Antiviral




Prototype NRTI used in combinations for HIV infections in prophylaxis for needlesticks and vertical transmission




Toxicity - severe myelosuppression

Abacavir

Antiviral



NRTI used in combinations for HIV infections in prophylaxis for needlesticks and vertical transmission




Toxicity - severe myelosuppression

Didanosine (ddI)

Antiviral



NRTI used in combinations for HIV infections in prophylaxis for needlesticks and vertical transmission




Toxicity - severe myelosuppression

Lamivudine (3TC)

Antiviral



NRTI used in combinations for HIV infections in prophylaxis for needlesticks and vertical transmission




Toxicity - severe myelosuppression

Stavudine (d4T)

Antiviral



NRTI used in combinations for HIV infections in prophylaxis for needlesticks and vertical transmission




Toxicity - severe myelosuppression

Zalcitabine (ddC)

Antiviral



NRTI used in combinations for HIV infections in prophylaxis for needlesticks and vertical transmission




Toxicity - severe myelosuppression

Zolpidem

Non-benzodiazepine hypnotic acts via the BZ1 receptor subtype




Reversed by Flumazenil




Less amnesia and mucsle relaxation and lower dependence liability that benzodiazepines

Zaleplon

Non-benzodiazepine hypnotic acts via the BZ1 receptor subtype



Reversed by Flumazenil




Less amnesia and mucsle relaxation and lower dependence liability that benzodiazepines

Eszoplicone

Non-benzodiazepine hypnotic acts via the BZ1 receptor subtype
Reversed by Flumazenil
Less amnesia and mucsle relaxation and lower dependence liability that benzodiazepines