Mechanism of Action Flashcards by Boards August2013

Activates muscarinic receptors in ciliary muscle

Pilocarpine

How well did you know this?

Not at all

Perfectly

Used for the vasoocclusive crisis in sickle cell anemia with MOA of increasing HbF

Hydroxyurea

How well did you know this?

Not at all

Perfectly

Activates nicotinic receptors

Nicotine, Varenicline

How well did you know this?

Not at all

Perfectly

MOA: Betanechol

Activates muscarinic receptors

How well did you know this?

Not at all

Perfectly

Inhibits acetylcholinesterase and amplifies endogenousy released acetylcholine

Edrophonium, Neostigmine, Pyridostigmine, Physostigmine, Rivastigmine

How well did you know this?

Not at all

Perfectly

Competitively blocks all muscarinic receptors

Atropine, Homatropine, Cyclopentelate, Tropicamide

How well did you know this?

Not at all

Perfectly

Binds phosphorus of organophosphate and breaks organophosphate bond with cholinesterase

Pralidoxime

How well did you know this?

Not at all

Perfectly

Competitively blocks all muscarinic receptors restoring balance in the basal ganglia

Benztropine

How well did you know this?

Not at all

Perfectly

Blocks muscarinic receptors in brochial smooth muscle preventing vagal-stimulated bronchoconstriction

Ipatropium, Tiotropium

How well did you know this?

Not at all

Perfectly

Antagonizes histamine and serotonin

Scopolamine

How well did you know this?

Not at all

Perfectly

Competitively blocks nicotinic Ach receptors

Hexamethonium, Trimethaptan

How well did you know this?

Not at all

Perfectly

Activates alpha and beta receptors causing vasoconstriction, increased BP; increased HR, conduction and contractility; and bronchodilation

Epinephrine, Norepinephrine

How well did you know this?

Not at all

Perfectly

Activates alpha, beta, and dopamine-1 receptors causing vasoconstriction, increased BP; increased HR, conduction and contractility; and vasodilation in sphlanchnic and renal vessels

Dopamine

How well did you know this?

Not at all

Perfectly

Nonselectively activates beta adrenergic receptors

Isoproterenol

How well did you know this?

Not at all

Perfectly

Selectively activates alpha-1 adrenergic receptors

Phenylephrine, Pseudoephedrine

How well did you know this?

Not at all

Perfectly

Activates alpha-2 adrenergic receptors

Clonidine, Methyldopa, Apraclonidine

How well did you know this?

Not at all

Perfectly

Activates beta-1 adrenergic receptors

Dobutamine

How well did you know this?

Not at all

Perfectly

Activates beta-2 adrenergic receptors in bronchial smooth muscle causing bronchodilation

Albuterol, Salbutamol

Terbutaline, Ritodrine (uterine smooth muscles also)

How well did you know this?

Not at all

Perfectly

Irreversibly blocks alpha adrenergic receptors (alpha1>alpha2)

Phenoxybenzamine

Nonselective alpha blocker

How well did you know this?

Not at all

Perfectly

Reversibly blocks alpha adrenergic receptors (alpha1>alpha2)

Phenotolamine

Nonselective alpha blocker

How well did you know this?

Not at all

Perfectly

Selectively blocks alpha-1 adrenergic receptors

Prazosin, Doxazosin, Terzosin, Tamsulosin, Sildosin

Selective alpha-1 blockers

How well did you know this?

Not at all

Perfectly

Blocks beta-1 and beta-2 receptors. Blocks sympathetic effects on heart and BP reducing renin release

Propranolol, Pindolol, Timolol, Labetolol, Carvedilol, Nadolol
(Beta blockers)

How well did you know this?

Not at all

Perfectly

Selectively blocks beta-1 receptors. Blocks sympathetic effects on heart and BP

Atenolol, Betaxolol, Esmolol, Acebutolol, Metoprolol

Selective beta-1 blockers

How well did you know this?

Not at all

Perfectly

Drugs that causes decreased secretion of aqueous humor from the ciliary epithelium

Timolol (Beta blocker)
Mannitol (Osmotic diuretic)
Apraclonidine (Alpha-2 agonist)
Acetazolamide, Dorzolamide (Carbonic anhydrase inhibitors)

How well did you know this?

Not at all

Perfectly

Alters intracellular Ca++ metabolism relaxing arteriolar smooth muscle causing vasodilation.

Hydralazine

Opens K+ channels in vascular smooth muscle causing hyperpolarization, muscle relaxation and vasodilation

Minoxidil

Blocks voltage gated L-type calcium channels (cardiac > vascular)

Verapamil, Diltiazem | Non-dihydopyridine calcium channel blockers

Blocks voltage gated L-type calcium channels (vascular > cardiac)

Nifedipine, Felodipine, Amlodipine, Nicardipine, Nisoldipine, Israpidine

Drugs that cause ciliary muscle contraction, opening of trabecular meshwork, increased outflow

Pilocarpine, Physostigmine | Cholinomimetics

Its MOA causes increased outflow through canal of Schlemm

Latanoprost

Increased outflow via uveoscleral veins

Epinephrine

Relaxes venous and arteriolar smooth muscle

Nitroprusside

Causes arteriolar vasodilation of the afferent and efferent arterioles increasing renal blood flow

Fenoldopam

Inhibits ACE and formation of Angiotensin II decreasing aldosterone secretion.

Captopril, Enalapril, Benazepril, Fosinopril, Lisinopril, Quinapril, Ramipril, Trandolapril

Blocks angiotension AT1 receptors in vascular smooth muscle and adrenal cortex decreasing aldosterone secretion.

Losartan, Candesartan, Valsartan, Irbesartan, Eprosartan, Telmisartan

Inhibits renin preventing conversion of angiotensinogen to angiotensin I

Aliskiren

Releases NO, increase cGMP and relaxes smooth muscle especially vascular

``` Amyl nitrite (ultra short acting) Nitroglycerin, Isosorbide dinitrate, Isosorbide mononitrate (short acting) ```

Inhibits Na/K-ATPase increasing intracellular Ca increasing cardiac contractility

Digoxin

Use- and state-dependent block of I-Na channels; some block of I-K channels. Slowed conduction velocityand pacemaker activity, prolonged AP duration and refractory period

Procainamide, Disopyramide, Quinidine | Class IA antiarrhythmic

Highly selective use- and state-dependent I-Na block; minimal effect on normal tissue, no effect on I-K

Lidocaine, Mexiletine, Tocainide, Phenytoin | Class IB antiarrhythmic

Selective use- and state-dependent I-Na block; slowed conduction velocity and pacemaker activity

Flecainide, Propafenone, Encainide, Moricizine | Class IC antiarrhythmic

Selective I-K block; prolonged AP and QT duration

Dofetilide | Class III antiarrhythmic

I-K block and beta-adrenoceptor block

Sotalol | Class III antiarrhythmic

Strong I-K block produces marked prolongation of AP and refractory period. Group 1 activity slows conduction velocity; groups 2 and 4 activity confer additional antiarrhythmic activity

Amiodarone, Dronedarone | Class III antiarrhythmic

Increase in diastolic I-K of AV node that causes marked hyperpolarization and conduction block; reduced I-Ca

Adenosine

Inhibits carbonic anhydrase

Acetazolamide, Dorzolamide, Brinzolamide, Dichlorphenamide, Methazolamide (Carbonic anhydrase inhibitor)

Inhibit Na/K/2Cl transporter in thick ascending limb of LOH

Furosemide, Bumetanide, Toresamide, Ethacrynic acid | Loop diuretics

Inhibit Na/Cl transporter in DCT

Hydrochlorthiazide, Chlorthalidone, Indapamide, Metozalone | Thiazide diuretic

Steroid inhibitors of cytoplasmic aldosterone receptor in cortical CD reducing K excretion

Spironolactone, Eplerone | Aldosterone antagonist

Inhibitor of ENaC epithelial sodium channels in cortical CD, reducing Na reabsorption and K excretion

Amiloride, Triamterene | Na blocker, K sparing

Osmotically retains water in tubule by reducing reabsorption in PT, descending limb of LOH and CD

Mannitol, Glycerin, Isosorbide, Urea | Osmotic diuretic

Agonists at V1 and V2 receptos. Activate insertion of aquaporin water channels in CT

Desmopressin | Antidiuretic hormone

Antagonist at V1a, V2 receptors

Conivaptan, Tolvaptan, Lixivaptan, Demeclocycline, Lithium | ADH antagonist

Inhibits HMG-CoA reductase in the cholesterol biosynthesis

Simvastatin, Atorvastatin, Rosuvastatin, Fluvastatin, Pravastatin, Lovastatin, Pitavastatin

Binds bile acids preventing their reabsorption and increasing cholesterol utilization for replacement

Cholestyramine, Colesevelam, Colestipol | Bile acid-binding resin

Selective inhibitor of the NPC1L1 transporter, decreasing intestinal absorption of cholesterol and other phytosterols

Ezetimibe

Cholesterol analog, taking place of dietary and biliary cholesterol, decreasing intestinal absorption of cholesterol and other phytosterol

Sitosterol

Decreases VLDL synthesis and LDL cholesterol concentrations. Increases HDL concentration.

Niacin

Activates PPAR-alpha and increases expression of LPL and apolipoproteins. Lowers triglycerides. Increases HDL.

Gemfibrozil

Competitive pharmacologic block of peripheral and CNS H1 receptors plus alpha- and M-receptor block. Anti-motion sickness effect.

Diphenhydramine, Chlorpheniramine, Cyclizine, Meclizine, Promethazine

Competitive pharmacologic block of peripheral H1 receptors. No autonomic or anti-motion sickness effects.

Cetirizine, Loratadine, Fexofenadine, Desloratadine, Terfenadine, Astemizole

Competitive pharmacologic block of H2 receptors. Reduction of gastric acid secretion.

Cimetidine, Ranitidine, Famotidine, Nizatidine

5-HT1D agonist causing vasoconstriction. Modulates neurotransmitter release.

Sumatriptan, Almotriptan, Eletriptan, Frovatriptan, Naratriptan, Rizatriptan, Zolmitriptan

5-HT3 receptor antagonist

Ondansetron, Granisetron, Dolasetron, Palonosetron, Alosetron

Mixed partial agonist effects at 5HT2 and alpha-adrenoceptors causing marked smooth muscle contraction but blocks alpha-agonist vasoconstriction (vasoselective)

Ergotamine, Dihydroergotamine, Methysergide

Mixed partial agonist effects at 5HT2 and alpha-adrenoceptors causing marked smooth muscle contraction but blocks alpha-agonist vasoconstriction (uteroselective)

Ergonovine, Methyergonovine

Prostaglandin activating EP receptors causing increased HCO3 and mucus secretion in stomach.

Misoprostol, Gemeprost

Activates EP receptors causing vascular smooth muscle and relaxation

Alprostadil

Prostaglandin E2 analog that in low concentrations contract and high concentrations relax uterine and cervical smooth muscle

Dinoprostine, Sulprostone

Activates FP receptors

Carboprost, Bimaprost, Travoprost, Unoprostone

Activates IP receptors causing vasodilation and reducing platelet aggregation

Epoprostenol, Beraprost, Iloprost, Trepostinil

Anti-asthma drug that inhibits phosphodiesterase antagonizing adeonosine receptors causing bronchodilation

Theophylline, Aminophylline, Pentoxyfylline | Methylxanthines

Anti-asthma drug that prevents Ca influx and stabilizes mast cells, preventing degranulation and release of histamine, leukotrienes and other mediators

Cromolyn, Nedodromil, Lodoxamide | Mast cell stabilizer

Anti-asthma drug that inhibits phospholipase A2 reducing expression of cyclooxygenase

Fluticasone, Beclomethasone, Budesonide, Ciclesonide, Flunisolide, Momethasone, Triamcinoline (Corticosteroid)

Anti-asthma drug that inhibits 5-lipooxygenase reducing synthesis of leukotrienes preventing airway inflammation and bronchoconstriction

Zileuton | Leukotriene synthesis inhibitor

Anti-asthma drug that blocks cysteinyl leukotriene-1 receptor for leukotrienes C4, D4, E4 preventing airway inflammation and bronchoconstriction

Montelukast, Zafirlukast, Pranlukast

Anti-asthma that binds IgE antibodies on mast cells reducing reaction to inhaled

Omalizumab

Cofactor required for essential enzymatic reactions that form tetrahydrofolate, convert homocysteine to methione and metabolize methymalonyl-CoA

Cyanocobalamin, Hydroxycobalamin

Precursor of an essential donor of methyl groups used for synthesis of amino acids, purines, and deoxynucleotide

Folic acid, Folacin, Folinic acid

Agonist of erythropoeitin receptors expressed by red cell progenitors

Epoetin alfa, Darbepoetin alfa, Methoxy polyethylene, Glycolepoetin beta

Binds receptors on myeloid progenitors and stimulates cell maturation and proliferation; accelerates neutrophil recovery and reduces incidence of infection

Filgrastim, Sargramostim, Pegfilgrastim

Recombinant form of an endogenous cytokine, activating IL-11 receptors

Oprelvekin

Nonselective, irreversible COX 1&2 inhibitor reducing platelet production of thromboxane A2, a potent stimulator of platelet aggregation

Aspirin

Inhibits platelet aggregation by interfering with GPIIb/IIIa binding to fibrinogen and other ligands What disease does it resemble?

Abciximab, Eptifibatide, Tirofiban (Glycoprotein IIb-IIIa inhibitors) Glanzmann's Thrombasthenia

Irreversibly inhibits binding of ADP to platelet receptors reducing platelet aggregation

Clopidogrel, Ticlopidine, Prasugrel

Inhibits phosphodiesterase III and increase cAMP in platelets and blood vessels inhibiting platelet aggregation and causes vasodilation

Dipyridamole, Cilostazol

Activates antithrombin III by inactivating thrombin or factor IIa, factor IXa & factor Xa by forming stable complexes with them

Heparin

Binds and potentiates effect of antithrombin III on factor Xa more selective

Enoxaparin, Daltaparin, Tinzaparin, Danaparoid, Fondaparinux

Binds to thrombin's active site and inhibits its enzymatic action

Lepuridin, Desidurin, Bivalirudin, Argatroban

Inhibits vitamin K epoxide reductase responsible for gamma-carboxylation of the vitamin K-dependent clotting factors

Warfarin, Dicumarol

Chemical antagonist of heparin

Protamine sulfate

Tissue plasminogen activator analog converting plasminogen to plasmin which degrades the fibrin and fibrinogen causing thrombolysis

Alteplase, Anistreplase, Reteplase, Streptokinase, Tenecteplase, Urokinase

Competitively inhibits plasminogen activation

Aminocaproic acid, Tranexamic acid

Increases supply of reduced vitamin K which is required for synthesis of functional vitamin K-dependent clotting and anticlotting factors

``` Vitamin K1 (Phytonadione) Vitamin K2 (Menaquinone) Vitamin K3 (Menadione) ```

Selective COX2 inhibitor, inhibiting prostaglandin synthesis

Celecoxib, Etroricoxib, Parecoxib, Rofecoxib, Valdecoxib

Inhibits AICAR transformylase and thymidylate synthetase with secondary effects on polymorphonuclear chemotaxis

Methotrexate

Binds to TNF-alpha preventing it from TNF-alpha receptor

Infliximab, Adalimumab, Etanercept

Forms 6-Thioguanine, suppressing inosinic acid synthesis, B-cell and T-cell function, immunoglobulin production and interleukin-2 secretion

Azathioprine

Suppression of T-lymphocyte responses to mitogens decreasing leukocyte chemotaxis, stabilization of lysosomal enzymes, inhibition of DNA and RNA synthesis, trapping of free radicals

Chloroquine, Hydroxychloroquine

Forms phosphoramide mustard which cross-links DNA to prevent cell replication suppresses T-cell and B-cell activation

Cyclophospamide

Inhibits interleukin-1 and interleukin-2 receptor production and secondarily inhibits macrophage T-cell interaction and T-cell rsponsiveness

Cyclosporine

Its active product inhibits inosine monophosphate dehydrogenase and inhibits T-cell lymphocyte proliferation

Mycophenolate mofetil

Active metabolite inhibits the release of inflammatory cytokines

Sulfasalazine

Antigout drug that inhibits microtuble assembly, decreasing macrophage migration and synthesis

Colchicine

Competes with uric acid for reabsorption in the proximal tubules increasing uric acid excretion

Probenecid

Active metabolite, alloxanthine irreversibly inhibits xanthine oxidase and lowers production of uric acid

Allopurinol

Nonpurine reversible inhibitor of xanthine oxidase more selective than allopurinol lowering production of uric acid

Febuxostat

Bind to GABA-A receptor subunits to increasing frequency of Cl channel opening hyperpolarizing membrane

Benzodiazepenes Midazolam, Brotizolam, Triazolam, Oxazepam, Etizolam (short-acting) Lorazepam, Alprazolam, Estazolam, Clonazepam,Lormetrazepam, Nitrazepam, Temazepam (intermediate-acting) Diazepam, Chlorazepate, Chlordiazepoxide, Flurazepam, Quezepam, Flunitrazepam (long-acting)

Antagonist at benzodiazepene sites on GABA-A receptor

Flumazenil

Bind to GABA-A receptor sites by increasing duration of Cl channel opening

Barbiturates Thiopental, Methohexital, Thiamylal (ultrashort) Pentobarbital, Secobarbital, Amobarbital, Butalbital, Butabarbital, Talbultal, Aprobarbital (short and intermediate) Phenobarbital, Mephobarbital, Primidone (long)

Bind selectively to a subgroup of GABA-A receptors, acting like benzodiazepenes to enhance membrane hyperpolarization

Zolpidem, Zaleplon, Eszopiclone

Anxiolytic that partial antagonist at 5-HT1 receptors and possibly D2 receptors

Buspirone

Anti-seizure drug that blocks voltage gated channels

Phenytoin, Fosyphenytoin, Mephenytoin, Ethotoin

Anti-seizure drug that blocks voltage gated channels and decrease glutamate release

Carbamazepine

Anticonvulsant that blocks high frequency firing of neurons modifies amino acid metabolism

Valproic acid

Anticonvulsant that decreases Ca++ currents in thalamus

Ethosuximide

Anticonvulsant that blocks Ca++ channels inhibiting neuronal discharge from seizure foci

Gabapentin, Pregabalin

Anticonvulsant that blocks Na and Ca channels decreasing glutamate

Lamotrigine

Anticonvulsant that selectively binds synaptic vesicular protein SV2A modifyng synaptic release of glutamate and GABA

Levetiracetam

Anticonvulsant with multiple actions on synaptic function via actions on phosphorylation

Topiramate

Facilitates GABA-mediated inhibition blocking brain NMDA and ACh-N receptors

Inhalational anesthetics

Intravenous anesthetic that blocks excitation by glutamate at NMDA receptors

Ketamine

Intravenous anesthetic that modulates GABAa receptors containing beta-3 subunits

Etomidate

Intravenous anesthetic that potentiates GABA-A receptors and blocks Na channels

Propofol

Blockade of Na channels slows then prevents axon potential propagation

Ester local anesthetics (1i) - Procaine, Benzocaine, Butamben, Cocaine, Tetracaine Amide local anesthtics (2is) - Lidocaine, Prilocaine, Bupivacaine, Ropivacaine

Competitive antagonists at skeletal muscle nicotinic acetylcholine receptors

Tubocurarine, Mivacurium, Atracurium, Vecuronium, Rocuronium, Pancuronium

Agonist at ACh-N receptors causing initial twitch then persistent depolarization

Succinylcholine

Inhibits peripheral metabolism of Levodopa via dopa decarboxylase

Carbidopa

Antiparkinsonism drug that partially antagonizes dopamine D2 receptors in brain

Bromocriptine, Pergolide

Antiparkinsonism drug that partially agonizes dopamine D3 receptors in brain

Pramipexole, Ropinirole

Antiparkinsonism drug that partially agonizes dopamine D3 receptors and antagonizes at 5-HT and alpha-adrenoceptors

Apomorphine

Selective inhibitors of MAO type B leading to decreased degradation of dopamine and increasing response to levodopa/carbidopa

Selegiline, Rasagiline

Antiparkinsonism drug that block L-dopa metabolism by inhibiting catechol-O-methytransferase in periphery or CNS prolonging response to levodopa

Entacapone, Tolcapone

Antiparkinsonism drug that potentiates dopaminergic function by influencing the synthesis, release or reuptake of dopamine antagonizing the effects of adenosine at adenosine A2 receptors

Amantadine

Antiparkinsonism drug that decreases the excitatory actions of cholinergic neurons on cells in the striatum by blocking muscarinic receptors

Benztropine, Biperiden, Trihexyphenidyl, Orphenadrine

Block of D2 receptors >> 5-HT2 receptors

Typical antipsychotics | Chlorpromazine, Thioridazine, Haloperidol, Droperidol

Block of 5-HT2 receptors >> D2 receptors

Atypical antipsychotics | Clozapine, Olanzapine, Quetiapine, Risperidone, Ziprasidone, Aripriprazole

Mood stabilizer that decreases cAMP inhibiting inosotol-1-phosphatase causing depleting of inositol and inositol triphosphate

Lithium

Blocks NE and 5-HT transporters

Imipramine, Clomipramine, Desipramine, Amitryptyline, Nortryptiline (Tricyclic antidepressant)

Inhibits neuronal reuptake of serotonin

Fluoxetine, Parozetine, Citalopram, Escitalopram, Sertraline, Fluvoxamine (Selective serotonin reuptake inhibitor)

Inhibits neuronal reuptake of serotonin and norepinephrine

Venlafaxine, Duloxetine, Desvenlafaxine | Serotonin-norepinephrine reuptake inhibitor

Blocks 5-HT2 receptors

Trazadone, Nefazodone | serotonin antagonist

Strong norepinephrine reuptake inhibitor and weak serotonin reuptake inhibitor; blocks dopamine D2 receptors

Amoxapine

Increases amine release from nerve endings by antagonism of presynaptic alpha-2 adrenoceptors; blocks serotonin 5-HT2 receptors

Mirtazipine

Inhibits neuronal reuptake of dopamine and norepinephrine increasing their activities

Bupropion

Inhibits MAO types A and B increasing CNS levels of NE and serotonin

Phenelzine, Tranylcypromine, Selegeline

Strong agonist at mu receptors

Morphine, Fentanyl, Sufentanil, Alfentanil, Remifentanil, Ohmefentanyl, Methadone

Strong agonist at mu and kappa receptors

Meperidine, Hydroxycodone, Oxycodone

Decreases sensitivity of cough receptors depressing the medullary cough center through sigma receptor stimulation

Dextrometorpham, Codeine

Weak agonist at mu receptors

Propoxyphene, Levopropoxyphene, Dextropropo, Tramadol, Tapentadol

Strong agonist at kappa receptors, weak antagonist activity at mu receptors

Nalbuphine, Buprenorphine, Butorphanol, Pentazocine

Competitively blocks mu, delta and kappa receptors

Naloxone, Naltrexone, Nalmefene

Increases release of IGF-1 in the liver and cartilage

Somatropin

Suppression secretion of GH, IGF-1, serotonin and GI peptides

Octreotide, Lanreotide

Activates FSH receptos mimicking effects of endogenous FSH

Follitropin alfa, Menotropins, Urofollitropin, Follitropin beta

Activates LH receptos mimicking effects of endogenous LH

Choriogonadotropin alfa, Human chorionic gonadotropin, Lutropin

Increased LH and FSH secretion with intermittent administration and reduced LH and FSH secretion with prolonged continuous administration

Leuprolide, Gonadorelin, Goserelin, Histrelin, Nafarelin, Triptorelin

Blocks GnRH receptors reducing production of LH and FSH

Ganirelix, Cetrorelix, Abarelix, Degarelix

Inhibits thyroid peroxidase reactions; blocks iodine organification; inhibits peripheral conversion of T4 into T3

Propylthiouracil

Inhibits thyroid peroxidase reactions; blocks iodine organification

Methimazole

Emits beta rays causing destruction of thyroid parenchyma

Radioactive iodine

Inhibits iodine organification and hormone release reducing size and vascularity of thyroid gland

Potassium iodide | Lugol's solution

Activates glucocorticoid receptors, leading to altered gene transcription suppressing inflammation

Hydrocortisone Desonide (low potency) Fluticasone, Mometasone (medium potency) Desoximethasone, Clobetasol (high potency)

Strong agonist of mineralocorticoid receptors and moderate activation of glucocorticoid receptors

Fludrocortison, Deoxycorticosterone

Inhibits desmolase blocking conversion of cholesterol to pregnenolone reducing synthesis of all hormonally active steroids

Aminogluthethimide

Inhibits cholesterol side-chain cleavage, cytochrome P450 enzymes blocking ergosterol synthesis

Ketoconazole, Fluconazole, Itraconazole

Inhibits cholesterol side-chain cleavage, cytochrome P450 enzymes blocking ergosterol synthesis

Ketoconazole, Fluconazole, Itraconazole | Clotrimazole

Estrogen antagonistic actions in breast tissue and CNS. Estrogen agonist effects in uterus, liver, and bone.

Tamoxifen, Toremifene

Estrogen antagonistic actions in breast tissue, uterus and CNS. Estrogen agonist effects in liver, and bone.

Raloxifene

Partial agonist of estrogen receptors in pituitary; reduces negative feedback by estradiol; increases FH and LSH output

Clomiphene

Estrogen synthesis inhibitor

Anastrazole, Letrozole, Exemestane

Partial agonist of progestin and androgen receptors

Danazol

Pharmacologic antagonist of glucocorticoid and progesterone receptors

Mifeprestone

Competitive antagonist at androgen receptor

Flutamide, Bicalmutamide, Nilutamide

Inhibits 5alpha-reductase enzyme that converts testosterone to dihydrotestosterone

Finasteride, Dutasteride

Increases insulin secretion from panceratic beta cells by closing ATP-sensitive K+ channels

Insulin secretagogues Chlorpropamide, Tolbutamide, Tolazamide (1st gen) Glipizide, Glimepiride, Glyburide, Glibenclamide, Gliclazide (2nd gen) Repaglinide, Nateglinide, Mitiglinide

Activates AMP-stimulated protein kinase leading to inhibition of hepatic and renal gluconeogenesis

Metformin

Regulates gene expression by binding to PPAR-gamma

Pioglitazone, Rosiglitazone, Troglitazone

Inhibits intestinal alpha-glucosidase

Acarbose

Activates amylin receptors suppressing glucagon release; delays gastric emptying; stimulates CNS to reduce appetite

Pramlintide

Activates GLP-1 receptors augmenting stimulated insulin release from pancreatic B cells; inhibits glucagon secretion; produces satiety

Exanatide | Incretin modulator

Inhibts dipeptidyl peptidase-4 that degrades GLP-1 and other incretins

Sitagliptin, Linagliptin

Inhibits GI and pancreatic lipases reducing absoprtion of fats

Orlistat

Antiobesity drug that inhibits NE and serotonin reuptake in the CNS

Sibutramine

Antiobesity drug that selectively blocks cannabinoid receptors

Rimonabant

Acts through PTH receptors to produce a net increase in bone formation

Teriparatide

Suppresses the activity of osteoclasts inhibiting bone resorption

Alendronate, Etidronate, Ibandronate, Pamidronate, Risedronate, Tiludronate, Zoledronic acid

Binds to dietary phosphate and prevents its absorption

Sevelamer

Binds to proteins inhibiting transpeptidation in bacterial cell walls

Penicillins

Inhibits inactivation of penicillins by bacterial beta-lactamase

Clavulanic acid, Sulbactam, Tazobactam

Inhibits cell wall synthesis by binding to the D-ala-D-ala terminus of nascent polypeptidoglycan

Vancomycin, Teicoplanin

Interferes with a late stage in cell wall synthesis in gram positive organisms

Bacitracin

Blocks incorporation of D-ala into the pentapeptide side chain of the peptidoglycan

Cycloserine

Bacterial protein synthesis inhibitors

``` buy AT 30, CELLS at 50 A = Aminoglycosides T = Tetracyclines C = Chloramphenicol E = Erythromycin L = Lincosamides L = Linezolid S = Streptogranins ```

Bacterial protein synthesis inhibitor that binds to 30s ribosomal subunit by blocking formation of the initiation complex, causing misreading of the code on the mRNA template and inhibiting translocation

Aminoglycosides | Gentamicin, Amikacin, Streptomycin, Neomycin, Spectinomycin

Binds to 30s subunit by inhibiting binding of tRNA to A side

Tetracycline, Doxycycline, Minocycline, Tigecycline, Demeclocycline

Binds to 50s subunit by inhibiting transpeptidation

Chloramphenicol

Binds to 50s subunit by inhibiting translocation

Macrolides and Lincosamides Macrolide - Erythromycin, Azithromycin, Clarithromycin, Telithromycin Lincosamide - Clindamycin, Lincomycin

Inhibits dihydropteroate synthase

Silver sulfadiazine, Mafenide acetate, Sulfamethoxazole

Sequential blockade of dihydropteroate synthase and dihydrofolate reductase

Co-trimoxazole (Sulfamethoxazole-Trimethprim)

Inhibits DNA replication by binding to DNA gyrase and topoisomerase IV

Fluoroquinolones Ciprofloxacin, Ofloxacin, Norfloxacin (2nd gen) Levofloxacin, Sparfloxacin, Grepafloxacin (3rd gen) Moxifloxacin, Trovafloxacin, Gemifloxacin, Gatifloxacin (4th gen) Nadilixic acid, Cinaxacin, Rosoxacin (1st gen - obsolete)

Reactive reduction by ferredoxin forming free radicals that disrupt electron transport chain

Metronidazole, Tinidazole

Forms multiple ractive intermediates when acted upon by bacterial nitrofuran reductase

Nitrofurantoin

Antimycobacterial that inhibits mycolic acid synthesis

Isoniazid

Antimycobacterial that inhibits DNA-dependent RNA polymerase

Rifampicin, Rifabutin, Rifapentine

Antimycobacterial that inhibits arabinosyl transferases involved in the synthesis of arabinogalactan in mycobacterial cell wall

Ethambutol

Antimycobacterial that inhibits folic acid synthesis

Dapsone

Antimycobacterial that binds to guanine in bacterial DNA

Clofazimine

Antifungal that binds to ergosterol in fungal cell membranes forming artificial pores

Amphotericin B | Nystatin

Accumulated by fungal cells by the action of permease and converted by cytosine deaminase to 5-FU which inhibits thimidylate synthase

Flucytosine

Inhibits beta-glucan sythase decreasing fungal cell wall synthesis

Caspofungin, Anidulafungin, Micafungin

Antifungal that interferes with microtubule function inhibiting synthesis and polymerization of nucleic acids

Griseofulvin

Interferes with ergosterol synthesis by inhibiting fungal squalene oxidase

Terbinafene

Activated by viral thymidine kinase to forms that inhibit viral DNA polymerase

Acyclovir, Valacyclovir, Penciclovir, Famciclovir, Docosanol

Inhibits viral DNA polymerase causing chain termination

Ganciclovir, Valganciclovir | Cifodovir

Inhibits viral RNA polymerase, DNA polymerase and HIV reverse transcriptase and binds to pyrophosphate binding site

Foscarnet

Inhibit HIV reverse transcriptase after phosphorylation by cellular enzymes

Zidovudine, Abacavir, Didonasine, Emtricitabine, Lamivudine, Stavudine, Tenofovir, Zalcitabine (Nucleoside reverse transcriptase inhibitors)

Inhibit HIV reverse transcriptase but no phosphorylation

Delavirdine, Efavirenz, Etravirine, Nevirapine (Non-nucleoside reverse transcriptase inhibitors)

Inhibit viral protein processing

Indinavir, Amprenavir, Atazanavir, Darunavir, Indinavir, Lopinavir, Nelfinavir, Ritonavir, Saquinavir, Tipranavir (Protease inhibitor)

Binds to gp41 subunit of viral envelope glycoprotein preventing fusion of viral and cellular membranes

Enfuvirtide | Fusion inhibitor

Blocks viral attachment via transmembrane chemokine receptor CCR5

Maraviroc

Inhibit early step replication and prevent uncoating by binding to M2 proton channels

Amantadine, Rimantadine

Inhibits neuramidase decreasing releasing of progeny virus

Oseltamivir, Zanamivir

Degrades viral RNA via activation of host cell RNAase

Interferon-alpha

Inhibits HBV DNA polymerase

Lamivudine, Adefovir dipivoxil, Entacavir, Telbivudine, Tenofovir

Inhibits GTP formation, prevents capping of viral mRNA and blocks RNA-dependent RNA polymerase

Ribavirin

Antimalarial drug that prevents polymerization of heme into hemozoin

Chloroquine, Hydroxychloroquine

Antimalarial drug that complexes with DNA to prevent strand separation, blocks DNA replication and transcription

Quinine, Quinidine

Antimalarial drug that forms electron-transfering redox compounds that act as cellular oxidants; tissue schizonticide

Primaquine

Antimalarial drug that disrupts mitochondrial electron transport and inhibits folate synthesis

Atovaquone-Proguanil

Antimalarial drug with sequential blockade of folic acid synthesis

Sulfadoxone-Pyrimethamine

Antimalarial drug that impairs progeny of malarial apicoplast genes resulting in abnormal cell division

Doxycycline

Antimalarial drug that forms free radicals in malarial food vacuole

Artemisin, Artesunate, Artemether, Dihydroartemisinin

Antiprotozoal drug that inhibits protein synthesis and blocks ribosomal movement along messenger RNA

Emetine, Dehydroemetine

Antiprotozoal drug that inhibits protein synthesis and binds to 16s ribosomal subunit

Paromomycin

Antiprotozoal drug that reduces ferredoxin forming free radicals that disrupt electron transport chain

Nitazoxanide

Antiprotozoal drug that is suicide inhibitor of ornithine decarboxylase

Eflornithine

Antiprotozoal drug that is a organic arsenical and inhibits enzyme sulfahydryl groups in trypanosomes

Melarsoprol

Antiprotozoal drug that inhibits trypanothione reductase

Nifurtimox

Antihelminthic drug that inhibits microtubule synthesis and glucose uptake in nematodes

Mebendazole

Antihelminthic drug that inhibits microtubule synthesis that is ovicidal and larvicidal

Albendazole

Antihelminthic drug that intensifies GABA-mediated neurotransmission in nematodes

Ivermectin

Antihelminthic drug that stimulates nicotinic receptors at NMJ of nematodes causing depolarization-induced paralysis

Pyrantel pamoate

Antihelminthic drug that inhibits microtubule synthesis and glucose reuptake in nematodes; inhibits fumarate reductase

Thiabendazole

Antihelminthic drug that increases membrane permeability to calcium causing muscle paralysis, vacuolization and death

Praziquantel

Antihelminthic drug that uncouples oxidative phosphorylation or activates ATPases

Niclosamide

Alkalyting agents that form DNA cross-links resulting in inhibition of DNA synthesis and function

Cyclophosphamide, Chlorambucil, Cisplatin, Carboplatin, Oxaliptin, Bisulfan

Alkalyting agent that forms hydrogen peroxide which generates free radicals that cause DNA strand scission

Procarbazine, Dacarbazine

Antimetabolite chemotherapeutic drugs that inhibit de novo purine nucleotide synthesis

6-Mercaptopurine, 6-Thioguanine, Fludarabine, Cladribine

Antimetabolite chemotherapeutic drug that inhibits thymidilate synthesis causing thymineless death

5-Flurouracil

Antimetabolite chemotherapeutic drugs that inhibit DNA synthesis and repair; inhibit ribonucleotide reductase with reduced formation of dNTPs

Cytarabine, Gemcitabine

Chemotherapeutic drug that prevents microtubule assembly causing cell arrest at metaphase

Vincristine, Vinblastine

Chemotherapeutic drug that inhibits DNA topoisomerase II (DNA gyrase) and inhibits mitochondrial electron transport

Etoposide, Teniposide

Chemotherapeutic drug that inhibits DNA topoisomerase I (DNA swivelase)

Topotecan, Irinotecan

Chemotherapeutic drug that interferes with mitotic spindle and prevents microtubule disassembly into tubulin monomers

Paclitaxel, Docetaxel

Antitumor antibiotic that intercalates between base pairs, inhibits topoisomerase II and generates free radicals

Doxorubicin, Daunorubicin, Idarubicin, Epirubicin, Mitoxantrone

Antitumor antibiotic that generates free radical which cause DNA strand breaks and intercalates with DNA

Bleomycin

Antitumor antibiotic that binds to double-stranded DNA and inhibits DNA-dependent RNA synthesis

Actinomycin D

Anticancer drug that inhibits tyrosine kinase activity of the protein product of bcl-abl oncogene in CML and c-kit tyrosine kinase in GIST

Imatinib, Dasatinib, Nilotinib

Anticancer drug that acts against breast cancer cells that over-express the HER-2/neu receptor for epidermal growth factor (EGF)

Trastuzumab

Anticancer drug that inhibits binding of VEGF to VEGFR leading to inhibition of VEGF signaling; inhibits tumor vascular permeability but enhances tumor blood flow and drug delivery

Bevacizumab

Anticancer drug that binds to a surface protein in NHL cells inducing complement-mediated lysis, direct cytotoxicity and induction of apoptosis

Rituximab

Anticancer drug that depletes serum asparagine

Asparaginase

Anticancer drug that allows DNA transcription and differentiation of immature leukemic promyelocytes into mature granulocytes

All-trans retinoic acid

Neutralize stomach acid by reacting with protons in the lumen of the gut

Magnesium-aluminum hydroxide

Irreversible blockade of H/K/ATPase in active gastric parietal cells causing long-lastng reduction of meal-stimulated and nocturnal acid secretion

Omeprazole, Lansoprazole, Rabeprazole, Pantoprazole, Esomeprazole

Binds to injured tissue and forms a protective covering over ulcer beds accelerating healing of peptic ulcers and reduces recurrence rate

Sucralfate

Forms a protective coating on ulcerated tissue; stimulates mucosal protective mechanisms, direct antimicrobial effects and sequestration of enterotoxins

Bismuth salicylate

Soften stool material permitting water and lipids to penetrate

Docusate, Glycerine, Mineral oil

Indigestible, hydrophillic colloids that absorb water forming a bulky, emollient gel that distends the colon and promotes peristalsis

Psyllium, Methylcellulose, Polycarbophil

Soluble but nonabsorbable compounds that result in increased stool liquidity due to an obligate increase in fecal fluid

Lactulose, Magnesium oxide, Sorbitol, Magnesium citrate, Sodium phosphate, Polyethylene glycol

Chemo drugs that bind and inhibit EGF receptors

Transtuzumab (breast) Cetuximab (colon) Bevaxizumab (head and neck)