1

binds receptor to allow Na and K to diffuse down their gradient nicotine/Ach on nicotinic receptors

binds M2 (K channel and cAMP) in the heart bethanechol

binds M3 (IP3/DAG) to increase smooth muscle firing bethanechol

binds M2 to increase NO in the heart pilocarpine

binds M3 to increase glandular secretions pilocarpine

2

binds M1, M2, M3 as an antimuscarinic atropine

blocks cholinergic activity in the corpus striatum once dopaminergic inhibition has been lost benztropine

competitive muscarinic antagonist relaxes GI/GU smooth muscle and decreases secretions propantheline

reversibly binds acetylcholinesterase at the NMJ edrophonium

suicide inhibitor of cholinesterase that carbamylates the enzyme's active site neostigmine

3

organophosphate that binds to cholinesterase, phosphorylating it and making it resistant to

hydration parathion

analog of dopamine that stimulates b1, with a little b2 and a1 as well dobutamine

endogenous catecholamine that stimulates D1 at low doses to increase renal perfusion and diuresis dopamine

stimulates a1=a2>b1, with no b2 norepinephrine

taken up presynaptically and leads to the release of endogenous NE amphetamine

4

blocks reuptake, especially of NE cocaine

stimulates release of NE from sympathetic neurons, also acts directly ephedrine

a1 agonist increases intracellular calcium methoxamine

a1 agonist increases intracellular calcium phenylephrine

nonselective competitive antagonist of a-receptors phentolamine

5

irreversibly inhibits COX to block the production of PGG2 aspirin

blocks the conversion of arachidonic acid to prostaglandins ibuprofen

reversibly inhibits COX acetaminophen

binds tubulin to cause depolymerization colchicine

change activation of macs, inhibit lysosomal enzyme formation, decrease histamine release, suppress

PMN phagocytosis gold

6

a sulfapyridine linked to aspirin, acts only at the colon when bacteria break it apart sulfasalazine

converted to 6-mercaptopurine and inhibits IMP dehydrogenase -> death of lymphoid cells azathioprine

acts on T cells to inhibit transcription of IL-2 cyclosporine

leads to crosslinking of bases, abnormal base pairing, and DNA strand breakage alkylating agents

acts during S phase to inhibit DNA synthesis via incorporation of itself into the strand cytarabine

7

selectively inhibits DNA synthesis by inhibiting thymidylate synthase 5-FU

impairs synthesis of DNA and RNA, it is an analog of hypoxanthine and adenine mercaptopurine

leads to decreased synthesis of thymidylate, purines, and amino acids by preventing the recycling of folic

acid methotrexate

binds DNA, complexes with Fe, and forms free radicals to injure the DNA chain bleomycin

blocks DNA-dependent transcription by RNA polymerase and causes ss breaks dactinomycin

8

breaks DNA by free radical generation and topoisomerase II activation doxorubicin

binds topoisomerase II to induce ss breaks etoposide

competitive antagonist at estrogen receptor tamoxifen

binds tubulin to arrest cell at metaphase vinca alkaloids

competitvely inhibits H2 receptors cimetidine

9

weak bases that neutralize gastric HCl antacids

decrease hepatic secretion of cholesterol into bile, inhibits HMG-coA reductase, decreases reabsorption

of cholesterol by intestineursodiol (anti-gallstones)

facilitate GABA, increase Cl channel DURATION, hyperpolarize membrane barbiturates

potentiate GABA, increase Cl channel FREQUENCY of opening, hyperpolarize membrane benzodiazepines

selectively antagonist of serotonin 1A buspirone (anxiolytic)

10

acts as an anticonvulsant, induces glucuronyl transferase, it is a long acting barbiturate phenobarbital

blocks Na channels, inhibits uptake and release of NE carbamazepine

blocks Na channels, stabilizes membranes, decreases Ca influx, helps GABA phenytoin

enhances GABA accumulation valproic acid

increases threshold for firing of CNS neurons halothane

11

blocks Na channels on rapidly firing pain neurons procaine

competitively inhibits Ach at nicotinic receptors at motor end plates pancuronium

depolarizing NM blocker

succinylcholine

binds and activates GABA-b receptors in the CNS baclofen

decreases Ca release from SR dantrolene

12

decreases Ca entry and increases K conductance primarily at mu receptors morphine

acts on mu and delta receptors in the bowel diphenoxylate

acts on mu with extended duration of action methadone

pure mu antagonist naloxone

blocks D1 and D2 receptors chlorpromazine

13

high potency dopamine blocker haloperidol

inhibits recycling of neuronal membrane phosphoinositides used by alpha and muscarinic

receptors lithium

inhibit reuptake of NE and 5HT imipramine

SSRI (no antimuscarinic, antihistamine, a-blocker side effects) fluoxetine

inhibits MAO-B selectively selegiline

14

irreversibly inhibit MAO

phenelzine and isocarboxazid

selectively metabolizes serotonin MAO-A

selectively metabolizes dopamine MAO-B

two aspirin molecules linked by an azo bond, used in those with sulfa allergies for UC olsalazine

inhibits transcription of IL-2 with less nephrotoxicity than cyclosporine FK506

15

crosslink bases, abnormal base pairing, DNA strand breakage, but is not an alkylating agent cisplatin

antiemetic that acts by dopamine blockade metoclopramide

facilitates Ach release from myenteric plexus cisapride

benzodiazepine analog that antagonizes flumazenil

d-isomer of amethylated opioid used as antitussive dextromethorphan

16

used outpatient, pure antagonist at opioid mu receptors naltrexone

converted by dopa decarboxylase levodopa

inhibits dopa decarboxylase in the periphery carbidopa

binds cytosolic receptor and goes to nucleus to aid transcription of testosterone-responsive genes methyltestosterone

in premenopausal women, acts as a competitive inhibitor at estrogen receptors in the anterior

pituitary and hypothalamus clomiphene

17

bind a zinc finger DNA-binding protein estrogens, progestins

binds a receptor with tyrosine kinase activity insulin

nine amino acid peptide from the posterior pituitary oxytocin

causes release of vWF and factor VIII in the vascular endothelium vasopressin

inhibits things through a cAMP mechanism octreotide

18

thionamide that inhibits iodide organification, incorporation of iodine into tyrosine residues, and

conversion of T3 to T4 in the peripherypropylthiouracil

stimulates the release of insulin from beta cells and sensitizes peripheral tissues to insulin glyburide

actions at ATP-sensitive K channels mimics glucose and leucine glyburide

binds transpeptidases in dividing bacteria ampicillin

amino group allows it to pass into gram negatives ampicillin

19

monobactam that binds PBPs, inhibits peptidoglycan synthesis, only works in gram negatives aztreonam

beta lactam that binds transpeptidases and causes autolysis cephalosporins

binds and inactivates beta lactamases clavulanic acid

binds transpeptidases and inhibit bacterial cell wall synthesis imipenem

binds transpeptidases and has a bulky R group nafcillin

20

carboxyl R group allows penetration into gram-negative bacteria, acts by inhibiting

transpeptidase ticarcillin

enters bacteria by oxygen-dependent active transport aminoglycoside

interferes with formation of initiation complex, induces misreading of mRNA, causes breakup of

polysomes gentamicin

active transport pumps drug through the inner cytoplasmic membrane, prevents access of aminoacyl

tRNA to acceptor site on mRNA tetracycline

blocks peptidyl transferase at 50S chloramphenicol

21

inhibits micochondrial synthesis in bone marrow cells chloramphenicol

disrupts formation of 70S initiation complex and inhibits aminoacyl translocation step of peptide bond

synthesis clindamycin

inhibits translocation step of protein synthesis at 50S erythromycin

PABA analog, competitive antagonist of dihyropteroate synthetase sulfonamides

ultimately inhibits THF synthesis and impairs purine and thymidine synthesis sulfonamides

22

structurally similar to folic acid, inhibits DHFR trimethoprim

reductive bioactivation of nitro group by ferredoxin froms cytotoxic products metronidazole

forms covalent bonds with bacterial DNA in acidic urine nitrofurantoin

acts on gram negatives by distorting membrane lipid structure (it is a basic polypeptide containing fatty

acids) polymyxin

inhibits bacterial topoisomerase II quinolones

23

prevents polymerization of peptidoglycans vancomycin

guanosine analog that acts as a chain terminator and viral DNA polymerase inhibitor acyclovir

needs to be phosphorylated by viral thymidine kinase acyclovir

prevents assembly of influenza A2 virus amantadine

inhibits viral reverse transcriptase as dd ATP didanosine

24

inorganic phosphate that inhibits DNA polymerase, inhibits HIV reverse transcriptase foscarnet

guanine derivative inhibits DNA polymerase of CMV, prevents chain elongation ganciclovir

inhibits synthesis of guanine nucleotides by competitively inhibiting IMP dehydrogenase ribavirin

phosphorylated form inhibits 5 cap formation and inhibits viral RNA polymerase ribavirin

thymidine analog that gets into DNA and makes it break trifluridine

25

adenosine analong in which arabinose replaces ribose, inhibits viral DNA polymerase vidarabine

inhibits viral reverse transcriptase zidovudine (AZT)

binds membrane sterols and acts like a pore, high affinity for ergosterol amphotericin B

prevents conversion of lanesterol to ergosterol by inhibiting 14-a-methylase ketoconazole

converted by cytosine deaminase to 5-FU, which inhibits thymidylate synthase flucytosine

26

interacts with polymerized microtubules to disrupt mitotic spindle griseofulvin

binds tightly to keratin griseofulvin

topical conazole miconazole

binds ergosterol and disrupts membrane permeability and transport functions (topical) nystatin

analog of PABA that inhibits dihydropteroate synthase from synthesizing folate de novo dapsone

27

inhibits incorporation of mycolic acid into mycobacterial cell wall ethambutol

inhibits biosynthesis of mycolic acids isoniazid

inhibits DNA-dependent RNA polymerase of mycobacteria by interacting with beta subunit rifampin

suppresses RNA chain initiation rifampin

kills plasmodium in RBCs chloroquine

28

metabolized to quinolone-quinone intermediates that are oxidants primaquine

uncouples oxidative phosphorylation and activates

ATPasesniclosamide

increases membrane permeability to Ca praziquantel

inhibits microtubule synthesis mebendazole

neuromuscular blockade at nicotinic receptors pyrantel pamoate

29

inhibits glucose metabolism in nonreplicating PCP pentamidine

forms chemically active radicals nifurtimox

inhibits parasitic enzymes involved in energy metabolism suramin

arsenical that binds sulfhydryl groups to inactivate a wide variety of enzymes melarsoprol

inhibits glycolysis or nucleic acid metabolism sodium stibogluconate

30

D2 agonist, D1 antagonist bromocriptine

act at alpha, dopamine, and serotonin receptors ergot alkaloids

competes for a weak acid carrier transporter in the proximal tubule probenecid

inhibits platelet release, platelet adhesion, and prostaglandin synthesis sulfinpyrazone

inhibits xanthine oxidase, leading to less uric acid production allopurinol

31

irreversibly inactivates aldehyde dehydrogenase, leads to accumulation of acetaldehyde disulfiram

reacts rapidly with trivalent iron of cytochrome oxidase in mitochondria cyanide

uncouples oxidative phosphorylation by substituting for phosphates in ATP arsenic

inhibits delta-ALA dehydratase and ferrochelatase lead

competitve antagonist of glycine strychnine

32

blocks proliferation of activated T cells prednisone

reversible competitive inhibitor of H1 receptors diphenhydramine

stimulates beta receptors to increase cAMP isoproterenol

activates b2 receptor to stimulate adenylate cyclase albuterol

parenteral b2 bronchodilator terbutaline

33

increases cAMP to relax smooth muscle methylxanthines

M3 antagonist, inhaled ipratropium

decreased accumulation of Ca in mast cells cromolyn sodium

enhances responsiveness of b2 receptors, inhibits phospholipase A2 beclomethasone

activates presynaptic a2 receptors when given orally clonidine

34

activates postsynaptic a2 receptors when given IV clonidine

converted to methyl-NE in the brain, binds presynaptic a2 receptors methyldopa

competes for nicotinic receptor on postganglionic neurons hexamethonium

taken up by NE reuptake mechanism, binds vesicles, inhibits release of NE guanethidine

decreases slope of phase 4 in pacemaker cells propranolol

35

decreases renin release by blocking b1 in the JGA propranolol

increases refractory period at AV node propranolol

activates guanylate cyclase and increases permeability to K hydralazine

decreases phase 4 slope and decreases rise of phase 0 slope verapamil

dihydropyridine that blocks L-type Ca channels nifedipine

36

combines with RBCs to release NO in both arteries and veins nitroprusside

inhibits carbonic anhydrase to reduce renal reabsorption of bicarbonate ions acetazolamide

inhibits Na/K/2Cl transporter in the TAL furosemide

inhibits Na/Cl transporter in the DCT, increases Ca reabsorption HCTZ

inhibits hepatic secretion of VLDL, leading to lower LDL production niacin

37

increases LDL receptors in addition to sequestering cholesterol in the intestines colestipol

increases LPL activity, decreases hepatic synth and secretion of VLDL gemfibrozil

inhibits Na/K ATPase, leads to high intracellular Na and therefore high intracellular Ca -> positive

inotropy digitalis

Na channel blockade in the heart, a 1A antiarrhythmic, anticholinergic quinidine

class III antiarrhythmic, K channel blockade, Na channel blockade, beta blocker, Ca channel blocker,

vasodilator, negative inotrope amiodarone

38

sodium channel blockade

class I antiarrhythmic

beta blockade class II antiarrhythmic

K channel blockadeclass III

antiarrhythmic

Ca channel blockade class IV antiarrhythmic

class 1B antiarrhythmic lidocaine

39

class 1C antiarrhythmic flecainide

decreases aqueous humor formation by nonselective beta blockade timolol

acts via purinergic receptors, G protein mediated decrease in cAMP and increased outward K current adenosine

bipyridine that blocks phosphodiesterase, leading to increased cAMP and increaed Ca influx: increased

cardiac contractility and vasodilation amrinone

hyperpolarizes arterial smooth muscle, inhibits insulin secretion diazoxide

40

inhibits epoxide reductase in the liver warfarin

activates ATIII by exposing binding site heparin

interferes with platelet 2b/3a binding of fibrinogen ticlopidine

inhibits platelet granule release, adherence to subendothelial cells, synth of prostaglandins sulfinpyrazone

lysine analog that prevents plasmin from binding fibrin aminocaproic acid

41

exposes an active site on plasminogen streptokinase

competitive antagonist of aldosterone in the DCT spironolactone