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

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

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

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

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

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

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

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

weak bases that neutralize gastric HCl

antacids

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

ursodiol (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)

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

10

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

11

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

12

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

13

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

14

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

15

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

16

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

17

thionamide that inhibits iodide organification, incorporation of iodine into tyrosine residues, and conversion of T3 to T4 in the periphery

propylthiouracil

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

18

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

19

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

20

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

21

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

22

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

23

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

24

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

25

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

26

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

27

metabolized to quinolone-quinone intermediates that are oxidants

primaquine

uncouples oxidative phosphorylation and activates ATPases

niclosamide

increases membrane permeability to Ca

praziquantel

inhibits microtubule synthesis

mebendazole

neuromuscular blockade at nicotinic receptors

pyrantel pamoate

28

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

29

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

30

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

31

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

32

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

33

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

34

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

35

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

36

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

37

sodium channel blockade

class I antiarrhythmic

beta blockade

class II antiarrhythmic

K channel blockade

class III antiarrhythmic

Ca channel blockade

class IV antiarrhythmic

class 1B antiarrhythmic

lidocaine

38

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

39

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

40

exposes an active site on plasminogen

streptokinase

competitive antagonist of aldosterone in the DCT

spironolactone

41