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

1

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

2

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

3

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

4

suppress PMN phagocytosis gold 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. decrease histamine release. inhibit lysosomal enzyme formation.

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. and DNA strand breakage alkylating agents acts during S phase to inhibit DNA synthesis via incorporation of itself into the strand cytarabine 6 . abnormal base pairing.

complexes with Fe.selectively inhibits DNA synthesis by inhibiting thymidylate synthase 5-FU impairs synthesis of DNA and RNA. and amino acids by preventing the recycling of folic acid methotrexate binds DNA. and forms free radicals to injure the DNA chain bleomycin blocks DNA-dependent transcription by RNA polymerase and causes ss breaks dactinomycin 7 . purines. it is an analog of hypoxanthine and adenine mercaptopurine leads to decreased synthesis of thymidylate.

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 8 .

increase Cl channel DURATION. hyperpolarize membrane barbiturates potentiate GABA. hyperpolarize membrane benzodiazepines selectively antagonist of serotonin 1A buspirone (anxiolytic) 9 . inhibits HMG-coA reductase. decreases reabsorption of cholesterol by intestine ursodiol (anti-gallstones) facilitate GABA. increase Cl channel FREQUENCY of opening.weak bases that neutralize gastric HCl antacids decrease hepatic secretion of cholesterol into bile.

induces glucuronyl transferase. stabilizes membranes. helps GABA phenytoin enhances GABA accumulation valproic acid increases threshold for firing of CNS neurons halothane 10 . it is a long acting barbiturate phenobarbital blocks Na channels. decreases Ca influx. inhibits uptake and release of NE carbamazepine blocks Na channels.acts as an anticonvulsant.

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 .

used in those with sulfa allergies for UC olsalazine inhibits transcription of IL-2 with less nephrotoxicity than cyclosporine FK506 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.

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 .crosslink bases. abnormal base pairing. DNA strand breakage.

acts as a competitive inhibitor at estrogen receptors in the anterior pituitary and hypothalamus clomiphene 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.

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. 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 . incorporation of iodine into tyrosine residues.

inhibits peptidoglycan synthesis.monobactam that binds PBPs. 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 .

acts by inhibiting transpeptidase ticarcillin enters bacteria by oxygen-dependent active transport aminoglycoside interferes with formation of initiation complex. prevents access of aminoacyl tRNA to acceptor site on mRNA tetracycline blocks peptidyl transferase at 50S chloramphenicol 20 . causes breakup of polysomes gentamicin active transport pumps drug through the inner cytoplasmic membrane.carboxyl R group allows penetration into gram-negative bacteria. induces misreading of mRNA.

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 .

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 .structurally similar to folic acid.

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 .

which inhibits thymidylate synthase flucytosine 25 . 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.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.

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 .

leading to less uric acid production allopurinol 30 . D1 antagonist bromocriptine act at alpha.D2 agonist. and prostaglandin synthesis sulfinpyrazone inhibits xanthine oxidase. platelet adhesion. dopamine. and serotonin receptors ergot alkaloids competes for a weak acid carrier transporter in the proximal tubule probenecid inhibits platelet release.

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 .

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 .increases cAMP to relax smooth muscle methylxanthines M3 antagonist.

binds presynaptic a2 receptors methyldopa competes for nicotinic receptor on postganglionic neurons hexamethonium taken up by NE reuptake mechanism. inhibits release of NE guanethidine decreases slope of phase 4 in pacemaker cells propranolol 34 . binds vesicles.activates postsynaptic a2 receptors when given IV clonidine converted to methyl-NE in the brain.

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 .

increases Ca reabsorption HCTZ inhibits hepatic secretion of VLDL. leading to lower LDL production niacin 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.

K channel blockade. leads to high intracellular Na and therefore high intracellular Ca -> positive inotropy digitalis Na channel blockade in the heart. vasodilator. Ca channel blocker. anticholinergic quinidine class III antiarrhythmic.increases LDL receptors in addition to sequestering cholesterol in the intestines colestipol increases LPL activity. a 1A antiarrhythmic. beta blocker. decreases hepatic synth and secretion of VLDL gemfibrozil inhibits Na/K ATPase. negative inotrope amiodarone 37 . Na channel blockade.

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. inhibits insulin secretion diazoxide 39 . 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 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 .

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