Drug Quiz (2010)

Generic name: Esomeprazole

• Mechanism of Action:
• - Proton pump inhibitor suppresses gastric acid secretion by inhibition of the H⁺/K⁺-ATPase in the gastric parietal cell

• Indication:
• Oral:
• - Short-term (4-8 weeks) treatment of erosive esophagitis; maintaining symptom resolution and healing of erosive esophagitis;
• - treatment of symptomatic GERD (gastrointestinal esophageal reflux disease); as part of a multidrug regimen for Helicobacter pylori eradication in patients with duodenal ulcer disease;
• - prevention of gastric ulcers in patients at risk (age ≥60 years and/or history of gastric ulcer) associated with continuous NSAID therapy;
• - long-term treatment of pathological hypersecretory conditions including Zollinger-Ellison syndrome

• I.V.:
• - Short term (≤10 days) treatment of GERD (gastrointestinal esophageal reflux disease) when oral therapy is not possible or appropriate

Generic Name: Lansoprazole

• Mechanism of Action:
• - Decreases acid secretion in gastric parietal cells through inhibition of (H⁺, K⁺)-ATPase enzyme system, blocking the final step in gastric acid production

• Indication:
• - OTC (relief of frequent heartburn);
• - short-term treatment of active duodenal ulcers;
• - maintenance treatment of healed duodenal ulcers; as part of a multidrug regimen for H. pylori eradication to reduce the risk of duodenal ulcer recurrence;
• - short-term treatment of active benign gastric ulcer;
• - treatment of NSAID-associated gastric ulcer; to reduce the risk of NSAID-associated gastric ulcer in patients with a history of gastric ulcer who require an NSAID;
• - short-term treatment for all grades of erosive esophalgitis; to maintain healing of erosive esophagitis;
• - long-term treatment of pathological hypersecretory conditions, including Zollinger-Ellison syndrome

Generic Name: Pantoprazole

• Mechanism of Action:
• Suppresses gastric acid secretion by inhibiting the parietal cell H⁺/K⁺ ATP pump

• Indication:
• Oral:
• - treatment and maintenance of healing of erosive esophagitis associated with GERD;
• - reduction in relapse rates of daytime and nighttime heartburn symptoms in GERD;
• - hypersecretory disorders associated with Zollinger-Ellison syndrome or other neoplastic disorders

• I.V.:
• - Short-term treatment (7-10 days) of patients with gastroesophageal reflux disease (GERD) and a history of erosive esophagitis;
• - hypersecretory disorders associated with Zollinger-Ellison syndrome or other neoplastic disorders

Generic Name: Omeprazole and Sodium Bicarbonate

• Mechanism of Action:
• Proton pump inhibitor; suppresses gastric basal/stimulated acid secretion by inhibiting the parietal cell H⁺/K⁺ATP pump

• Indication:
• - short term treatment of active duodenal ulcer disease or active benign gastric ulcer;
• - treatment of heartburn and other symptoms associated with gastroesophageal reflux disease (GERD);
• - short-term treatment of endoscopically-diagnosed erosive esophagitis; maintenance healing of erosive esophagitis;
• - reduction of risk of upper gastrointestinal bleeding in critically¬-ill patients

Generic Name: Dexlansoprazole

• Mechanism of Action:
• Proton pump inhibitor; suppresses gastric basal/stimulated acid secretion by inhibiting the parietal cell H⁺/K⁺ ATP pump

• Indication:
• - short-term treatment of heartburn associated with nonerosive GERD;
• - short-term treatment of all grades of erosive esophagitis; to maintain healing of erosive esophagitis for up to 6 months

Generic Name: Escitalopram

• Mechanism of Action:
• Escitalopram is the S-enatiomer of the racemic derivative citalopram, which selectively inhibits the reuptake of serotonin with little or no effect on norepinephrine or dopamine reuptake. It has no or very low affinity for 5-HT_1-7, alpha- and beta-adrenergic, D_1-5, H_1-3, M_1-5 and benzodiazepine receptors. Escitalopram does not bind to or has low affinity for Na⁺, K⁺,Cl^- and Ca⁺⁺ ion channels

• Indication:
• - treatment of major depressive disorder;
• - generalized anxiety disorders (GAD)

Generic Name: Duloxetine

• Mechanism of Action:
• Duloxetine is a potent inhibitor of neuronal serotonin and norepinephrine reuptake and a weak inhibitor of dopamine reuptake. Duloxetine has no significant activity for muscarinic cholinergic, H₁-histaminergic, or alpha₂-adrenergic receptors. Duloxetine does not possess MAO-inhibitory activity

• Indication:
• - acute and maintenance treatment of major depressive disorder (MDD);
• - treatment of generalized anxiety disorder (GAD);
• - management of pain associated with diabetic neuropathy;
• - management of fibromyalgia

Generic Name: Venlafaxine and Desvenlafaxine (active metabolite)

Venlafaxine and its active metabolite, o-desmethylvenlafaxine (OVD), are potent inhibitors of neuronal serotonin and norepinephrine reuptake and weak inhibitors of dopamine reuptake. Venlafaxine and OVD have no significant activity for muscarinic cholinergic, H₁-histaminergic, or alpha₂-adrenergic receptors. Venlafaxine and OVD do not possess MAO-inhibitory activity.

• - treatment of major depressive disorder,
• - generalized anxiety disorder (GAD),
• - social anxiety disorder (social phobia),
• - panic disorder

Generic Name: Buproprion

• Mechanism of Action:
• Aminoketone antidepressant structurally different from all other marketed antidepressant; like other antidepressants the mechanism of bupropion's activity is not fully understood. Bupropion is a relatively weak inhibitor of the neuronal uptake of norepinephrine and dopamine, and does not inhibit monoamine oxidase or the reuptake of serotonin. Metabolite inhibits the reuptake of norepinephrine. The primary mechanism of action is thought to be dopaminergic and/or noradrenergic.

• Indication:
• - treatment of major depressive disorder, including seasonal affective disorder (SAD);
• - adjunct in smoking cessation

Generic Name: Potassium Chloride

• Mechanism of Action:
• Potassium is the major cation of intracellular fluid and is essential for the conduction of nerve impulses in heart, brain, and skeletal muscle; contraction of cardiac, skeletal and smooth muscles; maintenance of normal renal function; acid-base balance, carbohydrate metabolism, and gastric secretion

• Indication:
• - treatment or prevention of hypokalemia (potassium deficiency)

Generic name: Sildenafil Citrate

• Mechanism of Action:
• Does not directly cause penile erections, but affects the response to sexual stimulation. The physiologic mechanism of erection of penis involves release of nitric oxide (NO) in the corpus cavernosum during sexual stimulation. NO activates the enzyme guanylate cyclase, which results in increased levels of cyclic guanosine monophosphate (cGMP), producing smooth muscle relaxation and inflow of blood to the corpus cavernosum. Sildenafil enhances the effect of nitric oxide(NO) by inhibiting phosphodiesterase type 5 (PDE-5), which is responsible for degradation of cGMP in the corpus cavernosum; when sexual stimulation causes local release of NO, inhibition of PDE-5 causes increased levels of cGMP in the corpus cavernosum, resulting in smooth muscle relaxation and inflow of blood to the corpus cavernosum; at recommended doses, it has no effect in the absence of sexual stimulation

• Indication:
• - treatment of erectile dysfunction (ED)

Generic Name: Tadalafil

• Mechanism of Action:
• Does not directly cause penile erections, but affects the response to sexual stimulation. The physiologic mechanism of erection of penis involves release of nitric oxide (NO) in the corpus cavernosum during sexual stimulation. NO activates the enzyme guanylate cyclase, which results in increased levels of cyclic guanosine monophosphate (cGMP), producing smooth muscle relaxation and inflow of blood to the corpus cavernosum. Tadalafil enhances the effect of nitric oxide (NO) by inhibiting phospodiesterase type 5 (PDE-5) which is responsible for degradation of cGMP in the corpus cavernosum; when sexual stimulation causes local release of NO, inhibition of PDE-5 causes increased levels of cGMP in the corpus cavernosum, resulting in smooth muscle relaxation and inflow of blood to the corpus cavernosum; at recommended doses it has no effect in the absence of sexual stimulation

• Indication:
• - treatment of erectile dysfunction (ED)

Generic Name: Vardenafil

• Mechanism of Action:
• Does not directly cause penile erections, but affects the response to sexual stimulation. The physiologic mechanism of erection of penis involves release of nitric oxide (NO) in the corpus cavernosum during sexual stimulation. NO activates the enzyme guanylate cyclase, which results in increased levels of cyclic guanosine monophosphate (cGMP), producing smooth muscle relaxation and inflow of blood to the corpus cavernosum. Vardenafil enhances the effect of nitric oxide (NO) by inhibiting phospodiesterase type 5 (PDE-5) which is responsible for degradation of cGMP in the corpus cavernosum; when sexual stimulation causes local release of NO, inhibition of PDE-5 causes increased levels of cGMP in the corpus cavernosum, resulting in smooth muscle relaxation and inflow of blood to the corpus cavernosum; at recommended doses it has no effect in the absence of sexual stimulation

• Indication:
• - treatment of erectile dysfunction

Generic Name: Budesonide

• Mechanism of Action:
• controls the rate of protein synthesis; depresses the migration of polymorphonuclear leukocytes, fibroblasts; reverse capillary permeability/lysosomal stabilization at the cellular level to prevent or control inflammation. Has potent glucocorticoid activity and weak mineralocorticoid activity

• Indications:
• - Management of symptoms of seasonal or perennial rhinitis

Generic Name: Mometasone Furoate

• Mechanism of Action:
• may depress the formation, release/activity of endogenous chemical mediators of inflammation (kinins, histamine, liposomal enzymes, prostaglandins); leukocytes/macrophages may have to be present for the initiation of responses mediated by the above substances; inhibits the margination/subsequent cell migration to the area of injury, and also reverses the dilation/increased vessel permeability in the area resulting in decreased access of cells to the sites of injury

• Indications:
• - treatment of nasal symptoms of seasonal/perennial allergic rhinitis;
• - prevention of nasal symptoms associated with seasonal allergic rhinitis;
• - treatment of nasal polyps in adults

Generic Name: Triamcinolone Acetonide

• Mechanism of Action:
• decreases inflammation by suppression of migratin of polymorphonuclear leukocytes/reversal of increased capillary permeability; suppresses the immune system by reducing activity/volume of the lymphatic system; suppresses adrenal function at high doses

• Indication:
• - management of seasonal/perennial allergic rhinitis

Generic Name: Modafinil

• Mechanism of Action:
• exact MOA unclear – increases high-frequency alpha waves while decreasing both delta/theta wave activity/these effects are consistent with generalized increases in mental alertness (may exert its stimulant effects by decreasing GABA-mediated neurotransmission)

• Indication:
• - improve wakefulness in patients with excessive daytime sleepiness associated with narcolepsy and shift work sleep disorder (SWSD);
• - adjunctive therapy for obstructive sleep apnea/hypopnea syndrome (OSAHS)

Generic Name: Lisdexamfetamine

• Mechanism of Action:
• a prodrug that’s converted to the active component dextroamphetamine that cause release of catecholamines (primarily dopamine/norepinephrine) from their storage sites in the presynaptic nerve terminals; less significant mechanism is it’s ability to block the reuptake of catecholamines by competitive inhibition

• Indication:
• - treatment of attention-deficit/hyperactivity disorder (ADHD)

Generic Name: Dextroamphetamine/Amphetamine

• Mechanism of Action:
• MOA is unknown. In adults it causes CNS stimulation by a direct action on adrenergic receptors, releasing norepinephrine from storage sites.

• Indication:
• - Attention-deficit /hyperactivity disorder (ADHD); narcolepsy

Generic Name: Dexmethylphenidate

• Mechanism of Action:
• Dexmethylphenidate HCl, the d-enatinomer of racenic methylphenidate, is a CNS stimulant. It's MOA for ADHD is not known. It is thought to block the reuptake of norepinephrine and dopamine into the presynaptic neuron and increase the release of these monoamines into the extraneuronal space

• Indication:
• - treatment of attention-deficit/hyperactivity disorder (ADHD)

Generic Name: Atomoxetine

• Mechanism of Action:
• Selectively inhibits the reuptake of norepinephrine with little or no activity at the other neuronal reuptake pumps or receptor sites

• Indication:
• - treatment of attention deficit/hyperactivity disorder (ADHD)

Generic Name: Methylphenidate, Methylphenidate HCl

• Mechanism of Action:
• mild CNS stimulant; blocks the reuptake of norepinephrine/dopamine into presynaptic neurons; appears to stimulate the cerebral cortex/subcortical structures similar to amphetamines

• Indication:
• - treatment of attention-deficit/hyperactivity disorder (ADHD);
• - symptomatic management of narcolepsy

Generic Name: Latanoprost

• Mechanism of Action:
• a prostanoid selective FP receptor agonist that reduces the intraocular pressure (IOP) by increasing the outflow of aqueous humor via increased uveoscleral outflow. Chemically latanoprost is a prostaglandin F-2-alpha analogue. It is absorbed through the cornea where it is hydrolyzed to the active acid form.

• Indication:
• - reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension

Generic Name: Bimatoprost

• Mechanism of Action:
• a synthetic analog of prostaglandin which mimics the effects of naturally occurring prostamides. It acts on the trabecular meshwork and uveoscleral routes and lncreases outflow of aqueous humor thereby lowering intraocular pressure (IOP). Bimatoprost acts locally without systemic action. After absorption, metabolism occurs rapidly via oxidation, N-deethylation and glucuronidation.

• Indication:
• - reduction of intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension;
• - hypotrichlosis treatment of the eyelashes

Generic Names: Brimonidine Tartrate

• Mechanism of Action:
• a relatively selective alpha-2-adrenergic agonist which lowers elevated intraocular pressure. It's MOA is due to a reduction of aqueous humor production and increasing uveoscleral outflow. Elevated IOP increases patient's risk of optic nerve damage and field loss.

• Indication:
• - Lowering of intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension

Generic Name: Travoprost

• Mechanism of Action:
• a synthetic prostaglandin F analogue which selectively stimulates FP prostanoid receptor agonist. The primary MOA to reduce intraocular pressure is thought to be through increased uveoscleral outflow. Travoprost acts locally without significant systemic action.

• Indication:
• - reduction of elevated intraocular pressure in patients with open-angled glaucoma or ocular hypertension who are intolerant of the other IOP-lowering medications or insufficiently responsive (failed to achieve target IOP determined after multiple measurements over time) to another IOP-lowering medication

Generic Name: Olopatadine HCl

• Mechanism of Action:
• an inhibitor of the release of histamine from mast cells and a relatively selective histamine H-1 antagonist that inhibits the type immediate hypersensitivity reaction including inhibition of histamine induced effects on human conjunctival epithelial cells. Systemic absorption following topical use is very low.

• Indication:
• - treatment of the signs/symptoms of allergic conjunctivitis

Generic Name: Brimonidine Tartrate and Timolol Maleate

• Mechanism of Action:
• a selective alpha-2 adrenergic receptor agonist with a nonselective beta-adrenergic receptor inhibitor that has a dual mechanism of action by reducing aqueous humor production and increasing non-pressure dependent uveoscelerol outflow

• Indication:
• - reduction of intraocular pressure (IOP) in patients with glaucoma or ocular hypertension

Generic Name: Moxifloxacin HCl

• Mechanism of Action:
• a fluoroquinolone antibiotic with antibacterial activity against Gram-positive and Gram-negative bacteria, Its MOA is due to the inhibition of the enzymes topoisomerase II (DNA gyrase) and topoisomerase IV. DNA gyrase is an essential enzyme that is involved in the replication, transcription and repair of bacterial DNA. Topoisomerase IV is an enzyme known to play a key role in the partitioning of the chromosomal DNA during bacterial cell division.

• Indication:
• - Treatment of bacterial conjunctivitis caused by susceptible organisms

Generic Name: Gatifloxacin

• Mechanism of Action:
• a DNA gyrase (topoisomerase II) inhibitor and also inhibits topoisomerase IV. (DNA gyrase aka topoisomerase II is an essential bacterial enzyme that maintains the superhelical structure of DNA – required for DNA replication/transcription, DNA repair, recombination, and transposition); inhibition is bactericidal

• Indication:
• - treatment of bacterial conjunctivitis

Generic Name: Loteprednol Etabonate Opthalmic Suspension

• Mechanism of Action:
• an ocular corticosteroid thought to act by the induction of phospholipase A2 inhibitory proteins, collectively called lipocortins. (It is postulated that these proteins control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2.)

• Indication:
• - inflammatory conditions (treatment of steroid-responsive inflammatory conditions of the palpebral/bulbar conjunctiva, cornea, and anterior segment of the globe such as allergic conjunctivitis, acne rosacea, superficial punctate keratitis, herpes zoster keratitis, iritis, cyclitis, selected infective conjunctivitis, when the inherent hazard of steroid use is accepted to obtain an advisable diminution in edema and inflammation)
• - treatment of postoperative inflammation following ocular surgery

Generic Name: Cyclosporine ophthalmic emulsion

• Mechanism of Action:
• When used systemically, cyclosporine is a potent immunosuppressive agent. Its exact MOA is unknown. Cyclosporine is thought to act as a partial immunomodulator in patients whose tear production is supressed from ocular inflammation due to keratoconjuctivitis sicca. Cyclosporine ophthalmic emulsion is not absorbed systemically in any measurable amount.

• Indication:
• - Increases tear production when suppressed tear production is presumed to be due to keratoconjunctivities sicca-associated ocular inflammation (in patients not already using topical anti-inflammatory drugs or punctual plugs)

Generic Name: Moxifloxacin, Systemic

• Mechanism of Action:
• a DNA gyrase inhibitor (topoisomerase II) and also inhibits topoisomerase IV. DNA gyrase (topoisomerase II) is an essential bacterial enzyme that maintains the superhelical structure of DNA. DNA gyrase is required for DNA replication and transcription, DNA repair, recombination, and transposition; inhibition is bactericidal.

• Indication:
• - treatment of mild-to-moderate community-acquired pneumonia, including multidrug-resistant ‘Streptococcus pneumoniae (MDRSP);
• - acute bacterial exacerbation of chronic bronchitis;
• - acute bacterial sinusitis;
• - complicated/uncomplicated skin/skin structure infections;
• - complicated intra-abominal infections

Generic Name: Fexofenadine and Pseudoephedrine

• Mechanism of Action:
• Fexofenadine, a metabolite of terfenadine, antagonizes H₁ (histamine) receptors in peripheral tissues. Fexofenadine does not penetrate the BBB. Pseudoephedrine stimulates alpha-1-adrenergic receptor in smooth muscle causing vasoconstriction.

• Indication:
• - relief of symptoms associated with seasonal allergic rhinitis in adults and children ≥12 years of age

Generic Name: Levocetirizine

• Mechanism of action:
• the active enantiomer of cetirizine; it produces its effects by antagonizing the H₁ receptors in the periphery. It may also suppress histamine activity in the subcortical region of the CNS.

• Indication:
• - relief of symptoms of perennial/seasonal allergic rhinitis;
• - treatment of skin manifestation (uncomplicated) of chronic idiopathic urticarial

Generic Name: Azelastine, Nasal

• Mechanism of Action:
• a histamine H₁-receptor antagonist that blocks histamine release in peripheral tissues. Azelastine is metabolized by cytochrome P450 enzyme system to an active metabolite, desmethylazelastine

• Indication:
• - treatment of the symptoms of seasonal allergic rhinitis such as rhinorrhea, sneezing, and nasal pruritus;
• - treatment of the symptoms of vasomotor rhinitis

Generic Name: Fluticasone Furoate, Nasal

• Mechanism of Action:
• a synthetic trifluorinated corticosteroid with potent anti-inflammatory activity. Fluticasone reduces the accumulation of surface basophillic cells resulting in a localized anti-inflammatory effect.
• The precise mechanism of action on rhinitis symptoms is not known.

• Indication:
• - management of seasonal and perennial allergic rhinitis

Generic Name: Desloratadine

• Mechanism of Action:
• a long-acting tricyclic histamine antagonist with selective H₁ receptor histamine antagonist activity that offers clinically proven benefits for the management of AR and CIU.

• Indication:
• - relief of nasal and non-nasal symptoms of seasonal allergic rhinitis (SAR) and perennial allergic rhinitis (PAR);
• - treatment of chronic idiopathic urticarial (CIU)

Generic Name: Eletriptan

• Mechanism of Action:
• selective agonist for serotonin (5-HT1B and 5-HT1D receptors) in cranial arteries; causes vasoconstriction and reduces sterile inflammation associated with antidromic neuronal transmission correlating with relief of migraine

• Indication:
• - acute treatment of migraine, with or without aura

Generic Name: Rizatriptan

• Mechanism of Action:
• selective agonist for serotonin (5-HT1B and 5-HT1D receptors) in cranial arteries; causes vasoconstriction and reduces sterile inflammation associated with antidromic neuronal transmission correlating with relief of migraine

• Indication:
• - acute treatment of migraine with or without aura (seeing an orb of light in field of vision)

Generic Name: Atorvastatin

• MOA:
• - Inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase (rate limiting enzyme in cholesterol synthesis → a compensatory increase in the expression of LDL receptors on hepatocyte membranes/a stimulation of LDL catabolism

• Indication:
• - Treatment of dyslipidemias or primary/secondary prevention of cardiovascular disease

Generic Name: Rosuvastatin

• MOA:
• - Inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase

• Indication:
• - used with dietary therapy for hyperlipidemias to reduce elevations in total cholesterol (TC), LDL-C, apolipoprotein B, nonHDL-C, and triglycerides (TG) in patients with primary hypercholesterolemia;
• - treatment of primary dysbetalipoproteinemia; treatment of homozygous familial hypercholesterolemia (FM);
• - to slow progression of atherosclerosis as an adjunct to diet to lower TC and LDL-C

Generic Name: Fenofibrate

• Indication:
• - Adjunct to dietary therapy for the treatment of adults with elevations of serum triglyceride levels (types IV/V hyperlipidemia);
• - adjunct to dietary therapy for the reduction of LDL-C, TC, TG/apolipoprotein B (apo B) in adult patients with primary hypercholesterolemia or mixed dyslipidemia (Frederickson types IIa/IIb)

• MOA:
• - Fenofibric acid, an agonist for the nuclear transcription factor PPAR-alpha (peroxisome proliferator-activated receptor-alpha) downregulates an inhibitor of lipoprotein lipase (apoprotein C-III) and upregulates the synthesis of apolipoprotein A-I, fatty acid transport protein/lipoprotein lipase resulting in an increase in VDL catabolism, fatty acid oxidation/elimination of triglyceride-rich particles;
• - as a result of a decrase in VLDL levels, total plasma triglycerides are reduced by 30 – 60%; modest increase in HDL occurs in some hypertriglyceridemic patients

Generic Name: Ezetimibe/Simvastatin

• Indication:
• - Used in combination with dietary modification for the treatment of primary hypercholesterolemia/homozygous familial hypercholesterolemia

• MOA:
• - Ezetimibe inhibits absorption of cholesterol at the brush border of the small intestine via the sterol transporter NPC1L1 (Niemann-Pick C1-Like1) → decreased delivery of cholesterol to the liver, reduction of hepatic cholesterol stores/an increased clearance of cholesterol from the blood;
• - decreases total cholesterol, LDL-C, ApoB/TG while increasing HDL¬¬-cholesterol (HDL¬-C)
• - Simvastatin is a methylated derivative of lovastatin that acts by competitively inhibiting 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, the enzyme that catalyzes the rate-limiting step in cholesterol biosynthesis

Generic Name: Ezetimibe

• Indication:
• - Use in combination with dietary therapy for the treatment of primary hypercholesterolemia;
• - homozygous sitosterolemia; homozygous familial hypercholesterolemia;
• - mixed hyperlipidemia

• MOA:
• - inhibits absorption of cholesterol at the brush border of the small intestine via the sterol transporter NPC1L1 (Niemann-Pick C1-Like1) → decreased delivery of cholesterol to the liver, reduction of hepatic cholesterol stores/an increased clearance of cholesterol from the blood;
• - decreases total cholesterol, LDL-C, ApoB/TG while increasing HDL¬¬-cholesterol (HDL¬-C)

Generic Name: Niacin

• Indication:
• - adjunctive treatment of dyslipidemias to lower the risk of recurrent MI/or slow progression of coronary artery disease, including combination therapy with other anti-dyslipidemic agents when additional triglyceride-lowering or HDL-increasing effects are desired; treatment of hypertriglyceridemia in patients at risk of pancreatitis;
• - treatment of peripheral vascular disease/circulatory disorders;
• - treatment of pellagra; dietary supplement

• MOA:
• - component of two coenzymes which is necessary for tissue respiration, lipid metabolism/glycogenolysis;
• - inhibits the synthesis of very low density lipoproteins (VLDL)/low density lipoproteins (LDL);
• - may also increase the rate of chylomicron triglyceride removal from plasma

Generic Name: Fenofibric acid

• Indication:
• - Adjunct to dietary therapy for the treatment of severely elevated serum TG levels;
• - adjunct to dietary therapy for the reduction of LDL-C, total cholesterol, TG, and apoB/to increase HDL-C in patients with primary hypercholesterolemia or mixed dyslipidemia;
• - also indicated as adjunct to dietary therapy concomitantly with a statin to reduce TG levels/increase HDL-C levels in patients with mixed dyslipidemia/coronary heart disease (CHD) or at risk for CHD

• MOA:
• - activates PPARa → increases lipolysis/eliminatioin of TG-rich particles from plasma by activating lipoprotein lipase/reducing production of Apo CIII → decrease in TG producing an alteration in the size/composition of LDL from small, dense, particles to large buoyant particles, which have a greater affinity for cholesterol receptors/are catabolized rapidly. PPARa activation also induces an increase in the synthesis of HDL-C/Apo AI/AII

Generic Brand: Colesevelam

• Indication:
• - Management of elevated LDL in primary hypercholesterolemia when used alone or in combination with an HMG-CoA reductase inhibitor, improve control of type 2 diabetes mellitus in conjunction with insulin or oral antidiabetic agents

• MOA:
• - Binds to bile acids in the intestine which reduces the amount of bile acids that are returned to the liver via enterohepatic circulation → results in upregulation of the hepatic enzyme, cholesterol 7-α-hydroxylase, which increases conversions of cholesterol to bile acids. As more bile acids are formed, the demand for cholesterol by the liver cell increases → in the dual effect of increased transcription/activity of the cholesterol biosynthetic enzyme hydroxymethyl-alutaryl-coenzyme A (HMG-CoA) reductase → increase clearance of LDL-C from the blood with decreased serum LDL-C

Generic Name: Clopidogrel

• Indication:
• - reduces rate of atherothrombotic events (myocardial infarction, stroke, vascular deaths) in patients with recent MI or stroke, or established peripheral arterial disease;
• - reduces rate of atherothrombotic events in patients with unstable angina or non-ST-segment elevation acute coronary syndromes (unstable angina/non-ST-segment elevation MI) managed medically or thru percutaneous coronary intervention (PCI) (with or without stent) or CABG; reduces rate of death/atherothrombotic events in patients with ST-segment elevation MI managed medically

• MOA:
• - requires in vivo biotransformation to an active thiol metabolite which irreversibly blocks the P2Y12 component of ADP receptors on the platelet surface, which prevents activation of the GPIIb/IIIa receptor complex, thereby reducing platelet aggregation. Platelets blocked by clopidogrel are affected for the remainder of their lifespan (-7-10 days)

Generic Name: Warfarin

• Indication:
• - Prophylaxis/treatment of thromboembolic disorders (eg. Venous, pulmonary)/embolic complications arising from atrial fibrillation or cardiac valve replacement;
• - adjunct to reduce risk of systemic embolism (recurrent MI, stroke) after myocardial infarction

• MOA:
• - competitively inhibits the subunit 1 of the multi-unit VKOR complex, thus depleting functional vitamin K reserves/hence reduces synthesis of active clotting factors

Generic Name: Aspirin/Dipyridamole

• Indication:
• Reduction in the risk of stroke in patients who have had transient ischemia of the brain or ischemic stroke due to thrombosis

• MOA:
• inhibits both adenosine deaminase/phosphodiesterase, preventing the degradation of cAMP (an inhibitor of platelet function) → elevation in cAMP blocks the release of aracidonic acid from membrane phospholipids/reduces thromboxane A2 activity; also directly stimulates the release of prostacyclin which induces adenylate cyclase activity thereby raising the intraplatelet concentration of cAMP/further inhibiting platelet aggregation

Generic Name: Enoxaparin

• Indication:
• - Acute coronary syndromes (unstable angina, non-ST-elevation/ST-elevation myocardial infarction);
• - DVT prophylaxis;
• - acute DVT treatment (inpatient/outpatient)

• MOA:
• - acts as an anticoagulant by enhancing the inhibition rate of clotting proteases by antithrombin III impairing normal hemostasis/inhibition of factor Xa;
• - derived from porcine heparin that undergoes benzylation followed by alkaline depolymerization

• Generic Name: Pioglitazone
• Indication:
• Type 2 DM monotherapy; adjunct to diet/exercise, to improve glycemic control; also Type 2 DM combination therapy with sulfonylurea, metformin, or insulin; when diet, exercise/a single agent alone does not result in adequate glycemic control
• MOA:
• a Thiazolidinedione antidiabetic agent that lowers blood glucose by improving target cell response to insulin, without increasing pancreatic insulin secretion → MOA is dependent on the presence of insulin for activity; is a potent/selective agonist for PPARgamma which influences the production of a number of gene products involved in glucose/lipid metabolism

Generic Name: Insulin Glargine

• Indication:
• - Treatment of type 1 diabetes mellitus/type 2 diabetes mellitus to improve glycemic control

• MOA:
• - a recombinant human insulin analog that’s long-acting (up to 24 hours duration of action), parenteral blood-glucose lowering agent;
• - Produced via recombinant DNA technology utilizing a non-pathogenic lab strain of E. coli as the production organism.
• - Primary activity of insulin is regulation of glucose metabolism. Insulin/its analog lower blood glucose levels by stimulating peripheral glucose uptake, especially by skeletal muscle/fat and by inhibiting hepatic glucose production.
• - Insulin inhibits lipolysis in the adipocyte, inhibits proteolysis/enhances protein synthesis

Generic Name: Sitagliptin

• Indication:
• - Management of type 2 DM as an adjunct to diet/exercise as monotherapy or in combination therapy with other antidiabetic agents

• MOA:
• - inhibits dipeptidyl peptidase IV enzyme resulting in prolonged active incretin levels (incretin hormones/glucose-dependent insulinotropic polypeptide regulate glucose homeostasis by increasing insulin synthesis/release from pancreatic beta cells/decreasing glucagon secretion from pancreatic alpha cells

Generic Name: Insulin Aspart

• Indication:
• - Treatment of type 1 DM/type 2 DM to improve glycemic control

• MOA:
• - Main function is the regulation of glucose metabolism;
• - binds to the insulin receptors on muscle/fat cells and lower blood glucose by facilitating the cellular uptake of glucose/simultaneously inhibiting the output of glucose from the liver

Generic Name: Insulin Lispro

• Indication:
• - Treatment of type 1 DM/type 2 DM to improve glycemic control

• MOA:
• - Main function is the regulation of glucose metabolism;
• - binds to the insulin receptors on muscle/fat cells and lower blood glucose by facilitating the cellular uptake of glucose/simultaneously inhibiting the output of glucose from the liver

Generic Name: Insulin Glargine

• Indication:
• - Treatment of type 1 diabetes mellitus/type 2 diabetes mellitus to improve glycemic control

• MOA:
• - a recombinant human insulin analog that’s long-acting (up to 24 hours duration of action), parenteral blood-glucose lowering agent; Produced via recombinant DNA technology utilizing a non-pathogenic lab strain of E. coli as the production organism. Primary activity of insulin is regulation of glucose metabolism. Insulin/its analog lower blood glucose levels by stimulating peripheral glucose uptake, especially by skeletal muscle/fat and by inhibiting hepatic glucose production. Insulin inhibits lipolysis in the adipocyte, inhibits proteolysis/enhances protein synthesis

Generic Name: Glipizide XL

• Indication:
• - Management of type 2 DM

• MOA:
• - stimulates insulin release from the pancreatic beta cells; reduces glucose output from the liver; insulin sensitivity is increased at peripheral target sites

Generic Name: Rosiglitazone

• Indication:
• - Type 2 DM monotherapy: improve glycemic control as an adjunct to diet and exercise

• MOA:
• - a Thiazolidinedione antidiabetic agent that lowers blood glucose by improving target cell response to insulin, without increasing pancreatic insulin secretion → MOA dependent on the presence of insulin for activity (an agonist for PPARgamma receptors)

Generic Name: Exenatide

• Indication:
• - Tx of type 2 DM to improve glycemic control

• MOA:
• - an analog of the hormone incretin which increases glucose-dependent insulin secretion, decreases inappropriate glucagon secretion, increases B-cel growth/replication, slows gastric emptying/decreases food intake → decreases in hemoglobin A_1c by approximately 0.5% to 1%

Generic Name: Sitagliptin/Metformin

• Indication:
• - management of type 2 DM in patients not adequately controlled on metformin or sitagliptin monotherapy/as an adjunct to diet and exercise

• MOA:
• - Combines two antihyperglycemic agents with complementary MOA to improve glycemic control in patients with type 2 diabetes.
• - Sitagliptin is an orally active, potent/highly selective DPP-4 (dipeptidyl peptidase 4) inhibitor (DPP-4 acts as an incretin enhancers) thus increasing levels of GLP-1 (glucagon-like peptide-1)/GIP (glucose-dependent insulinotropic polypeptide) which increase insulin synthesis/release from pancreatic β-cells GLP-1 also lowers glucagon secretion from pancreatic α-cells, leading to reduced hepatic glucose production.
• - Metformin is an antiyperglycemic agent that improves glucose tolerance in patients with type 2 diabetes, lowering both basal/postprandial plasma glucose.
• - Decreases hepatic glucose production, decreases intestinal absorption of glucose/improves insulin sensitivity by increases peripheral glucose uptake/utilization.
• - Insulin secretion remains unchanged while fasting insulin levels/day-long plasma insulin response may actually decrease

Generic Name: Insulin Detemir

• Indication:
• - TX of type 1 DM/type 2 DM to improve glycemic control

• MOA:
• - Primary activity is the regulation of glucose metabolism thru its specific action via binding to insulin receptors → lowers blood glucose by facilitating cellular uptake of glucose into skeletal muscle/fat and by inhibiting the output of glucose from the liver

Generic Name: Isophane Insulin Suspension

• Indication:
• - TX of type 1 DM/type 2 DM to improve glycemic control

• MOA:
• - a crystalline suspension of human insulin with protamine/zinc providing an intermediate-acting insulin with a slower onset of action/a duration of activity up to 24 hours than that of regular insulin

Generic Name: Pioglitazone/Metformin

• Indication:
• - Management of type 2 DM

• MOA:
• - contains 2 anti-diabetic drugs Pioglitazone/metformin;
• - Pioglitazone a Thiazolidinedione antidiabetic agent that lowers blood glucose by improving target cell response to insulin, without increasing pancreatic insulin secretion → MOA is dependent on the presence of insulin for activity; is a potent/selective agonist for PPARgamma which influences the production of a number of gene products involved in glucose/lipid metabolism
• - Metformin is an antiyperglycemic agent that improves glucose tolerance in patients with type 2 diabetes, lowering both basal/postprandial plasma glucose.
• - Decreases hepatic glucose production, decreases intestinal absorption of glucose/improves insulin sensitivity by increases peripheral glucose uptake/utilization.
• - Insulin secretion remains unchanged while fasting insulin levels/day-long plasma insulin response may actually decrease

Generic Name: Isophane Insulin/Regular Insulin

• Indication:
• - Tx of type 1 DM/type 2 DM to improve glycemic control

• MOA:
• - stimulates peripheral glucose uptake;
• - inhibits hepatic glucose production;
• - inhibits lipolysis/proteolysis;
• - regulating glucose metabolism

Generic Name: Insulin Aspart Protamine/Insulin Aspart

• Indication:
• - Tx of type 1 DM/type 2 DM to improve glycemic control

• MOA:
• - regulates glucose metabolism → binds to insulin receptors on muscle/fat cells → lower blood glucose by facilitating the cellular uptake of glucose, while simultaneously inhibiting the output of glucose from the liver

Generic Name: Isophane Insulin/Regular Insulin

• Indication:
• - Tx of type 1 DM/type 2 DM to improve glycemic control

• MOA:
• - stimulates peripheral glucose uptake;
• - inhibits hepatic glucose production;
• - inhibits lipolysis/proteolysis;
• - regulating glucose metabolism

Generic Name: Rosiglitazone/Metformin

• Indication:
• - management of type 2 DM as an adjunct to diet/exercise in patients where dual rosiglitazaone/metformin therapy is appropriate

• MOA:
• - combines 2 antidiabetic agents with different mechanisms of action to improve glycemic control in patients with type 2 DM;
• - Rosiglitazone is a member of the thiazolidinedione class, and metformin is a member of the biguanide class.
• - Thiazolidinediones are insulin sensitizing agents that act primarily by enhancing peripheral glucose utilization, whereas biguanides act primarily by decreasing endogenous hepatic glucose production.
• - Rosiglitazone, a member of the thiazolidinedione class of antidiabetic agents, improves glycemic control by improving insulin sensitivity while reducing circulating insulin levels.

Generic Name: Insulin Regular

• Indication:
• - TX of type 1 DM/type 2 DM to improve glycemic control

• MOA:
• - acts via specific membrane-bound receptors on target tissues to regulate metabolism of carbohydrate, protein/fats

Generic Name: Insulin Lispro protamine/Insulin Lispro

• Indication:
• - TX of type 1 DM/type 2 DM to improve glycemic control

• MOA:
• - Primary activity is to regulate glucose metabolism;
• - [75% insulin lispro protamine suspension and 25% insulin lispro injection, (rDNA origin)] is a mixture of insulin lispro solution, a rapid-acting blood glucose-lowering agent and insulin lispro protamine suspension, an intermediate-acting blood glucose-lowering agent - binds to the insulin receptors on muscle/fat cells and lower blood glucose by facilitating the cellular uptake of glucose/simultaneously inhibiting the output of glucose from the liver

Generic Name: Repaglinide

• Indication:
• - Management of type 2 DM as an adjunct to diet and exercise;
• - may be used in combination with metformin or thiazolidinediones

• MOA:
• - Nonsulfonylurea hypoglycemic agent which blocks ATP-dependent potassium channels, depolarizing the membrane/facilitating calcium entry thru calcium channels. Increased intracellular calcium stimulates insulin release from the pancreatic beta cells

Generic Name: Valsartan

• Indication:
• - alone or in combination with other antihypertensive agents in the treatment of essential hypertension;
• - reduction of cardiovascular mortality in patients with left ventricular dysfunction postmyocardial infarction;
• - treatment of heart failure

• MOA:
• - produces direct antagonism of the angiotension II (AT2) receptors → displaces AT2 from AT1 receptor/produces its blood pressure-lowering effects by antagonizing AT1-induced vasoconstriction, aldosterone release, catecholamine release, arginine vasopressin release, water intake/hypertrophic responses → more efficient blockade of the cardiovascular effects of AT2/fewer side effects than ACE inhibitors

Generic Name: Valsartan/Hydrochlorothiazide

• Indication:
• - Tx of hypertension

• MOA:
• - blocks the vasoconstrictor/aldosterone-secreting effects of AT2 by selectively blocking the binding of AT2 to AT1 receptor in many tissues

Generic Name: Losartan

• Indication:
• - TX of HTN;
• - tx of diabetic nepropathy in patients with type 2 DM/a history of HTN;
• - stroke risk reduction in patients with HTN/left ventricular hypertrophy (LVH)

• MOA:
• - a selective/competitive, nonpeptide AT2 receptor antagonist that blocks the vasoconstrictor/aldosterone-secreting effects of AT2
• - interacts reversibly at the AT1/AT2 receptors of many tissues/has slow dissociation kinetics;
• - also increases urinary flow rate/in addition to being natriuretic/kaliuretic, increases excretion of chloride, magnesium, uric acid, calcium/phosphate

Generic Name: Olmesartan

• Indication:
• - TX of HTN with or without concurrent use of other antihypertensive agents

• MOA:
• - a selective/competitive, nonpeptide AT2 receptor antagonist that blocks the vasoconstrictor/aldosterone-secreting effects of AT2
• - interacts reversibly at the AT1/AT2 receptors of many tissues/has slow dissociation kinetics;
• - also increases urinary flow rate/in addition to being natriuretic/kaliuretic, increases excretion of chloride, magnesium, uric acid, calcium/phosphate

Generic Name: Olmesartan/hydrochlorothiazide

• Indication:
• - Tx of HTN (not recommended for initial treatment)

• MOA:
• - blocks the vasoconstrictor effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor in vascular smooth muscle.
• - Hydrochlorothiazide is a thiazide diuretic - indirectly, the diuretic action of hydrochlorothiazide reduces plasma volume, with consequent increases in plasma renin activity, increases in aldosterone secretion, increases in urinary potassium loss, and decreases in serum potassium.

Generic Name: Losartan/hydrochlorothiazide

• Indication:
• - Tx of HTN;
• - stroke risk reduction in patients with HTN/left ventricular hypertrophy (LVH)

• MOA:
• - block the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor found in many tissues, (e. g., vascular smooth muscle, adrenal gland).
• - Hydrochlorothiazide is a thiazide diuretic. Thiazides affect the renal tubular mechanisms of electrolyte reabsorption, directly increasing excretion of sodium and chloride in approximately equivalent amounts. Indirectly, the diuretic action of hydrochlorothiazide reduces plasma volume, with consequent increases in plasma renin activity, increases in aldosterone secretion, increases in urinary potassium loss, and decreases in serum potassium.

Generic Name: Metoprolol Succinate

• Indication:
• - Tx of angina pectoris,
• - HTN,
• - to reduce mortality/hospitalization in patients with heart failure already receiving ACE inhibitors, diuretics/or digoxin

• MOA:
• - selective inhibitor of beta1-adrenergic receptors;
• - competitively blocks beta1-receptors, with little or no effect on beta2-receptors at doses ,<100 mg;
• - does not exhibit any membrane stabilizing or intrinsic sympathomimetic activity

Generic Name: Irbesartan

• Indication:
• - Tx of HTN alone or in combination with other antihypertensives;
• - tx of diabetic nephropathy in patients with type 2 DM/HTN

• MOA:
• - an angiotensin receptor antagonist which binds to the AT1 angiotension II receptor thereby blocking the vasoconstriction/aldosterone secreting effects of angiotension II

Generic Name: Irbesartan/hydrochlorothiazide

• Indication:
• - Combination therapy for the management of HTN; may be used as initial therapy in patients likely to need multiple drugs to achieve blood pressure goals

• MOA:
• - Irbesartan is a specific competitive antagonist of AT1 receptors with a much greater affinity (more than 8500-fold) for the AT1 receptor than for the AT2 receptor, and no agonist activity - blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively binding to the AT1 angiotensin II receptor.
• - Hydrochlorothiazide is a thiazide diuretic. Thiazides affect the renal tubular mechanisms of electrolyte reabsorption, directly increasing excretion of sodium and chloride in approximately equivalent amounts. Indirectly, the diuretic action of hydrochlorothiazide reduces plasma volume, with consequent increases in plasma renin activity, increases in aldosterone secretion, increases in urinary potassium loss, and decreases in serum potassium.

Generic Name: Amlodipine/Benazepril

• Indication:
• - Tx of HTN

• MOA:
• - amlodipine is a dihydropyridine calcium antagonist (calcium ion antagonist or slow channel blocker) that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle - produces vasodilation resulting in a reduction of supine and standing blood pressures. These decreases in blood pressure are not accompanied by a significant change in heart rate or plasma catecholamine levels with chronic dosing
• - Benazepril inhibits ACE inhibition of ACE results in decreased plasma angiotensin II, which leads to decreased vasopressor activity and to decreased aldosterone secretion.

Generic Name: Telmisartan

• Indication:
• - Tx of HTN (may be used alone or in combination with other antihypertensive agents); cardiovascular risk reduction in patients ≥ years of age unable to take ACE inhibitors/who are at high risk of major cardiovascular events (eg stoke, MI, death)

• MOA:
• - a nonpeptide AT1 angiotensin II receptor antagonist
• - binding prevents angiotensin II from binding to the receptor tereby blocking the vasoconstriction/aldosterone secreting effects of angiotensin II

Generic Name: Telmisartan/Hydrochlorothiazide

• Indication:
• - TX of HTN; combination product should not be used for initial therapy

• MOA:
• - Telmisartan blocks the vasoconstrictor and aldosterone secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor in many tissues, such as vascular smooth muscle and the adrenal gland. Its action is therefore independent of the pathways for angiotensin II synthesis.
• - Hydrochlorothiazide is a thiazide diuretic. Thiazides affect the renal tubular mechanisms of electrolyte reabsorption, directly increasing excretion of sodium and chloride in approximately equivalent amounts. Indirectly, the diuretic action of hydrochlorothiazide reduces plasma volume, with consequent increases in plasma renin activity, increases in aldosterone secretion, increases in urinary potassium loss, and decreases in serum potassium.

Generic Name: Amlopidine besylate/Valsartan

• Indication:
• - Tx of HTN

• MOA:
• - Amlopidine is a peripheral arterial vasodilator that acts directly on vascular smooth muscle to cause a reduction in peripheral vascular resistance and reduction in blood pressure.
• - Valsartan blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor in many tissues, such as vascular smooth muscle and the adrenal gland.

Generic Name: Candesartan

• Indication:
• - alone or in combination with other antihypertensive agents in treating essential HTN;
• - tx of heart failure

• MOA:
• - an angiotensin receptor antagonist;
• - binds to the AT1 angiotensin II receptor preventing angiotensin II from binding to the receptor thereby blocking the vasoconstriction and aldosterone secreting effects of angiotensin II

Generic Name: Amlopidine/Olmesartan)

• Indication:
• - Tx of HTN, including initial tx in patients who will require multiple antiypertensives for adequate control

• MOA:
• -is a combination of two antihypertensive drugs: a dihydropyridine calcium antagonist (calcium ion antagonist or slow-channel blocker), amlodipine besylate, and an angiotensin II receptor blocker, olmesartan medoxomil. The amlodipine component of Azor inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle, and the olmesartan medoxomil component of Azor blocks the vasoconstrictor effects of angiotensin II.

Generic Name: Aliskiren

• Indication:
• - Tx of HTN, alone or in combination with other antihypertensive agents

• MOA:
• - a direct renin inhibitor → blockade of the conversion of angiotensinogen to angiotensin I → decrease in the formation of angiotensin II

Generic Name: Clonidine

• Indication:
• -Management of mild-to-moderate HTN; either used alone or in combination with other antihypertensives

• MOA:
• -Stimulates alpha2-adrenocetors in the brain stem, thus activating an inhibitory neuron, resulting in reduced sympathetic outflow from the CNS, producing a decrease in peripheral resistance, renal vascular resistance, heart rate, and blood pressure

Generic Name: Nebivolol

• Indication:
• -Tx of HTN, alone or in combination with other agents

• MOA:
• -selectively antagonizes beta-1 adrenergic receptors → renin activity suppression; vasodilation; and decreased heart rate, myocardial contractility, and peripheral vascular resistance