Top Drugs - Mechanism of Action

Acetylcysteine (Acetadote, Mucomyst)

Hepatoprotective by restoring hepatic glutathione and enhancing the nontoxic sulfate conjugation of acetaminophen

Albuterol Sulfate (Proventil, Ventolin, Proair)

Short-acting B2 adrenergic agonist that relaxes bronchial smooth muscle

Alendronate (Fosamax)

Adheres to sites of bone resorption, inhibiting osteoclast activity. Normal bone is formed on top of alendronate, which is then incorporated into the bone matrix.

Allopurinol

Competitive inhibition of xanthine oxidase which prevents the conversion of hypoxanthine to xanthine to uric acid

Alprazolam

Binds to the GABA(A) receptor in the central nervous system and facilitates the action of GABA, an inhibitory neurotransmitter

Altplase

Initiates local fibrinolysis by binding to fibrin in the thrombus and converts entrapped plasminogen to plasmin

Amiodarone

Class III antiarrhythmic that lengthens the cardiac action potential by prolonging intranodal conduction and refractoriness of the AV node

Amitriptyline

Prevents reuptake of norepinephrine and serotonin at the presynaptic nerve terminal which increases activity at post synaptic terminals

Amlodipine

Dihydropyridine calcium channel blocker, inhibits calcium influx in vascular smooth muscle (more than cardiac muscle)

Amoxicillin

Inhibits bacterial wall synthesis via acylation transpeptidase enzyme

Amoxicillin/Clavulanate

Inhibits bacterial wall synthesis via acylation transpeptidase enzyme and inhibition of beta-lactamase

Amphetamine/Dextroamphetamine Salts

Releases norepinephrine and dopamine from storage sites causing stimulation on adrenergic receptors

Ampicillin/Sulbactam

Inhibits bacterial wall synthesis via acylation transpeptidase enzyme and inhibition of beta-lactamase

Anastrozole

Selective non-steroidal aromatase inhibitor which prevents the conversion of androstenedione to estrone and testosterone to estradiol. This decreases tumor mass or delays tumor progression

Apixaban

Selectively inhibitors Factor Xa which reduces thrombin formation

Arformoterol

Long-acting beta 2 adrenergic receptor agonist in the bronchial smooth muscle

Aripiprazole

Action may be combination of partial agonist activity at dopamine type 2 receptor and serotonin (5-HT1A and antagonism effects at 5-HT2 receptors)

Atenolol

Cardioselective beta 1 adrenergic blocker

Atomoxetine

May work by selective inhibition of the pre-synaptic norepinephrine transporter

Atorvastatin

Selective competitive inhibitor of HMG-CoA reductase

Azelastine

Histamine H1 receptor antagonist in peripheral tissues

Azithromycin

Suppresses protein synthesis by binding to the 50S ribosomal subunit

Baclofen

May work through hyperpolarization of afferent terminal resulting in inhibition of monosynaptic and polysynaptic reflexes

Benazepril

Angiotensin-converting enzyme inhibitor

Benztropine

Antagonist of muscarinic, cholinergic, and histaminergic receptors

Budesonide

Stimulates synthesis of anti-inflammatory proteins and enzymes

Budesonide/Formoterol

Stimulates synthesis of anti-inflammatory proteins and enzymes and long-acting beta 2 adrenergic receptor agonist

Bumetanide

inhibits reabsorption of sodium and chloride in the ascending loop of Henle

Bupropion

Blocks neuronal uptake of norepinephrine and dopamine in the central nervous system

Buspirone

May altar brain chemistry by increasing metabolism of norepinephrine, moderate presynaptic dopamine agonist, serotonin agonist

Carbamazepine

Na+ channel antagonist: delays recovery of inactive Na+ channels

Carbidopa/Levodopa

Levodopa is a precursor to dopamine, carbidopa is a DOPA-decarboxylase inhibitor and prevents the breakdown of levodopa before it crosses the blood brain barrier: combined, these increase the dopamine available to the central nervous system

Carvedilol

Non-selective beta- and alpha-1 adrenergic blocking activity

Cefazolin

Inhibits bacterial cell wall synthesis via acylation transpeptidase enzyme

Cefepime

Inhibits bacterial cell wall synthesis via acylation transpeptidase enzyme

Ceftriaxone

Inhibits cell wall synthesis via acylation transpeptidase enzyme

Celecoxib

Inhibits prostaglandin synthesis through selective inhibition of cyclooxygenase 2

Cephalexin

Inhibits cell wall synthesis via acylation transpeptidase enzyme

Chlorhexidine

Disrupts the plasma membrane of the bacterial cell

Chlorthalidone

Inhibits reabsorption of sodium and chloride at the cortical diluting segment of the ascending loop of Henle

Cholestyramine resin

binds with bile acids in the intestine, preventin reabsorption which is excreted in the feces

Ciprofloxacin

Prevents synthesis of bacterial DNA by interfering with the enzyme DNA gyrase

Cisatracurium

Competes with acetylcholine for cholinergic receptors inhibiting neuromuscular transmission

Citalopram

Blocks neuronal uptake of serotonin in the central nervous system

Clindamycin

Suppresses protein synthesis by binding to the 50S ribosomal subunit

Clobetasol Propionate

Binds to receptor proteins in the cytoplasm to form steroid-receptor complex. The complex enters the cell and alters mRNA transcription

Clonazepam

Binds to the GABA(A) receptor in the central nervous system and facilitates the action of GABA, an inhibitory neurotransmitter

Clonidine & Clonidine ER

Alpha 2 adrenergic receptor agonist resulting in reduced sympathetic outflow from the CNS

Clopidogrel

Inhibits platelet aggregation by irreversibly modifying platelet receptors

Clozapine

Antagonism of dopamine type 2 and 5-HT2A receptors, antagonist at adrenergic, cholinergic, histaminergic, and serotonergic receptors

Cyclobenzaprine

Acts in the brain stem to reduce tonic somatic motor activity

Dapaglifozin

Inhibits sodium-glucose co-transporter 2 (SGLT 2) which increases urinary glucose excretion

Desvenlafaxine

Blocks neuronal uptake of serotonin and norepinephrine in the central nervous system

Dexmedetomidine

Alpha 2 adrenergic receptor agonist

Dexmethylphenidate

May block reuptake of norepinephrine and dopamine in presynaptic neuron and increase the release of monoamines into extraneuronal space

Diazepam

Binds to the GABA(A) receptor in the central nervous system and facilitates the action of GABA, an inhibitory neurotransmitter

Diclofenac & Diclofenac (topical)

Inhibits prostaglandin synthesis through non-specific inhibition of cyclooxygenase

Dicyclomine

Inhibition of acetylcholine at postganglionic parasympathetic receptor sites in multiple tissues

Digoxin

Inhibits membrane bound Na+/K+ ATPase which increases intracellular Na+ concentration and a slightly decreased intracellular K+ concentration leading to increased extracellular Ca2+ influx increased force/velocity of heart

Diltiazem

Calcium channel blocker which inhibits calcium influx in vascular smooth muscle (more than in cardiac muscle)

Divalproex Sodium

MAY be related to voltage gated sodium channel blockade and increased brain levels of GABA

Dobutamine

Stimulates beta-2 and alpha-1 receptors to increase myocardial contractility and heart rate

Donepezil

Reversible acetylcholinesterase inhibitor working centrally to increase acetylcholine available at cholinergic synapses

Dopamine

Agonist at dopaminergic, alpha- and beta-adrenergic receptors; precursor for norepinephrine synthesis

Doxycycline

Prevents bacterial protein synthesis by competitively binding to the 30S ribosomal subunit

Dulaglutide

Human glucagon-like peptide-1 (GLP-1) receptor agonist and augments glucose dependent insulin secretion from the pancreas and slows gastric emptying

Duloxetine

Blocks neuronal uptake of serotonin and norepinephrine in the central nervous system

Empaglifozin

Inhibits sodium-glucose co-transporter 2 (SGLT2) which increases urinary glucose excretion

Enoxaparin

Inhibits Factor Xa (and to a lesser extent IIa) which reduces thrombin formation

Ephedrine

Releases norepinephrine from tissue stores resulting in alpha- and beta-adrenergic stimulation

Epinephrine

Sympathomimetic catecholamine that acts on both alpha- and beta-adrenergic receptors causing vasoconstriction (alpha), cardiac stimulation (beta-1) and relaxation of bronchial smooth muscles (beta-2)

Epoprostenol

Directly stimulates vasodilation of all vascular beds. It activates intracellular adenylate cyclase which inhibits platelet aggregation. Also known as prostacyclin (PGI2)

Escitalopram

Blocks neuronal uptake of serotonin in the central nervous system

Esomeprazole

Inhibits H+/K+ ATPase enzyme system at the secretory surface of the gastric parietal cell

Estradiol

Replaces estrogen post menopause. Promotes growth and development of vagina, uterus, and fallopian tubes, and enlargement of the breast

Eszopiclone

MOA unknown, thought to bind or interact with GABA receptor complexes

Ezetimibe

Inhibits intestinal absorption of cholesterol and related phytosterols

Famotidine

Competitive inhibition of histamine at H2 receptors of the gastric parietal cells, which inhibits gastric acid secretion

Fenofibrate

Activates peroxisome proliferator activated receptor-a resulting in increased lipolysis and elimination of triglycerides

Fentanyl Transdermal Patch

Opioid receptor agonist

Finasteride

Competitively inhibits the enzyme 5-alpha-reductase, resulting in decreased metabolism of testosterone to DHT

Fluconazole

Inhibition of fungal ergosterol synthesis via inhibition of fungal C14 demethylase

Fluoxetine

Blocks neuronal uptake of serotonin in the central nervous system

Fluticasone furoate/Vilanterol

Stimulates synthesis of anti-inflammatory proteins and enzymes and long-acting beta 2 adrenergic receptor agonist

Fluticasone furoate/umeclidinium bromide/Vilanterol

Stimulates synthesis of anti-inflammatory proteins and enzymes, competitively inhibits action of M3 receptors in bronchial smooth muscle, and long-acting beta 2 adrenergic receptor agonist

Fluticasone propionate (inhalation and nasal)

Stimulates synthesis of anti-inflammatory proteins and enzymes

Fluticasone/Salmeterol

Stimulates synthesis of anti-inflammatory proteins and enzymes and long-acting beta 2 adrenergic receptor agonist

Folic acid

Vitamin that is required for the synthesis of thymidylate, purine nucleotides, and maintenance of normal erthropoiesis

Furosemide

Loop diuretic which inhibits reabsorption of sodium and chloride in the proximal and distal tubules and in the loop of Henle

Gabapentin

Ca2+ channel antagonist; binds with alpha 2 subunit of Ca2+ channel

Glimepiride

Stimulates insulin synthesis and release from beta cells in the pancreatic islets

Glipizide

Stimulates insulin synthesis and release from the beta cells in the pancreatic islets

Guanfacine ER

Alpha 2 adrenergic receptor agonist

Heparin

Inactivates thrombin and activated Factor Xa through an antithrombin dependent mechanism

Hydralazine

Alters cellular calcium metabolism in the vascular smooth muscle resulting in direct relaxation and decreased vascular resistance

Hydrochlorothiazide

Inhibits reabsorption of sodium and chloride at the distal renal tubule

Hydrocodone/acetaminophen

Opioid receptor agonist & inhibition of prostaglandin synthesis in the central nervous system

Hydrocortisone sodium succinate

Stimulates synthesis of anti-inflammatory proteins and enzymes

Hydromorphone

Opioid receptor agonist

Hydroxychloroquine

MOA not well understood