Top 161-180

oxcarbazepine

antiepileptic

may produce its antiseizure activity by blockade of voltage-sensitive sodium channels, resulting in stabilization of hyperexcited neural membranes, inhibition of repetitive neuronal firing, and diminution of propagation of synaptic impulses. Oxcarbazepine also increases potassium conductance and modulation of high-voltage activated calcium channels. After oral administration, oxcarbazepine is extensively metabolized to its pharmacologically active 10-monohydroxy metabolite (MHD).

• Tablets
• Oral suspension

levocetirizine dihydrochloride

antiallergy agent

active enantiomer of cetirizine. It produces its effects by antagonizing the H₁ (histimine) receptors in the periphery. It may also suppress histamine activity in the subcortical region of the CNS. In vitro binding studies revealed that levocetirizine has an affinity for the human H₁-receptor 2-fold higher than that of cetirizine (Ki = 3 nmol/L vs. 6 nmol/L, respectively). The clinical relevance of this finding is unknown.

• Tablets
• Oral solution

methylphenidate hydrochloride (ER)

CNS agent for ADHD

a central nervous system (CNS) stimulant. Its mechanism of action in Attention Deficit Hyperactivity Disorder (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. Concerta comprises an osmotically active trilayer core surrounded by a semipermeable membrane with an immediate-release drug overcoat.

Tablets (Extended-release)

buspirone hydrochloride

antianxiety agent

The exact mechanism of action of buspirone in vivo is not known. It may be due to a number of changes in brain chemistry including; (1) locus ceruleus, (2) acting as a moderate presynaptic dopamine agonist, and (3) acting as a serotonin agonist. Buspirone does not significanty affect benzodiazepine or GABA receptors. Therapeutic improvement is usually seen within 7 days but may take as long as 21 days.

Tablets

lisdexamfetamine dimesylate

CNS agent for ADHD

a prodrug of dextroamphetamine. Dextroamphetamine's mechanism of action in ADHD is unknown. In adults it causes CNS stimulation by a direct action on adrenergic receptors, releasing norepinephrine from storage sites.

Capsules

carbidopa with levodopa

antiparkinson agent

levodopa crosses the blood-brain barrier and is converted into dopamine in the basal ganglia. A large portion of levodopa is converted to dopamine in extracerebral tissue. Dopamine does not cross the blood-brain barrier. Carbidopa inhibits dopa-decarboxylase in extracerebral tissue, thereby increasing the levels of levodopa available to the central nervous system, and decreases the side effects (nausea) seen from high levels of peripheral dopamine.

Tablets

carbidopa with levodopa

antiparkinson agent

levodopa crosses the blood-brain barrier and is converted into dopamine in the basal ganglia. A large portion of levodopa is converted to dopamine in extracerebral tissue. Dopamine does not cross the blood-brain barrier. Carbidopa inhibits dopa-decarboxylase in extracerebral tissue, thereby increasing the levels of levodopa available to the central nervous system, and decreases the side effects (nausea) seen from high levels of peripheral dopamine.

Tablets

clindamycin hydrochloride (oral)

antibiotic

binds to the 50 S subunit of susceptible bacterial ribosomes and suppresses protein synthesis.

• Capsules
• Granules for oral solution

dipyridamole and aspirin

antiplatelet agent

Dipyridamole inhibits platelet aggregation in response to platelet activation factor (PAF), collagen and adenosine diphosphate (ADP). Its mechanism of action is due to an inhibition in the uptake of adenosine into platelets causing a stimulation of platelet adenylate cyclase and subsequent increase in platelet cyclic-3', 5'-adenosine monophosphate. Aspirin inhibits prostaglandin and thromboxane A2 synthesis by acetylating the enzyme cyclooxygenase. Thromboxane A2 induces platelet aggregation and causes vasoconstriction. Aspirin permanently inhibits the thromboxane A2 in platelets for the life of the platelet.

Capsules

darifenacin hydrobromide

urinary bladder modifier

competitive muscarinic receptor antagonist with a high affinity for the M₃ receptor. Blockage of this receptor results in an increase in bladder capacity by decreasing the frequency of unstable detrusor contractions and increasing the volume threshold for unstable contractions.

Tablets (extended-release)

methylprednisolone

anti-inflammatory

adrenocorticoids bind to certain receptor proteins found in the cytoplasm of sensitive cells to form a steroid-receptor complex. This steroid-receptor complex enters the nucleus of the cell where it reacts with chromatin, or DNA. The steroid (or possibly the receptor) then uses stored information to stimulate or inhibit the transcription of m-RNA. The stimulation of m-RNA results in the synthesis of specific proteins and ultimately specific enzymes that carry out its antiallergy and anti-inflammatory actions.

• Tablets
• Dosepak
• Injection (Solu-Medrol)
• Injection (Depo-Medrol)

baclofen

muscle relaxant

Baclofen is an analog of gamma-aminobutyric acid (GABA). It most likely works at the spinal cord level, reducing both the flexor and extensor spasms. Its mechanism of action may be due to a hyperpolarization of afferent terminals resulting in inhibition of monosynaptic and polysynaptic reflexes.

• Tablets
• Injection

nystatin (topical)

antifungal antibiotic

an antimycotic polyene antibiotic obtained from Streptomyces noursei. Its mechanism of action is by binding to sterols in the cell membrane of susceptible Candida species and changing the permeability of the cell membrane. Nystatin is both fungicidal and fungistatic against many fungi. Nystatin is not absorbed from intact skin or mucous membranes.

• Topical powder
• Topical cream
• Topical ointment

sumatriptan succinate

antimigrainous agent

a selective agonist for a vascular 5-hydroxytryptamine 1 receptor subtype with no significant affinity or pharmacological activity at other receptors including 5-HT2, 5-HT3, alpha1, alpha2, beta-adrenergic receptors. 5-HT1 receptor subtypes are present on cranial arteries in both dog and primate, on the human basilar artery, and in the vasculature of the isolated dura mater of humans. In these tissues, sumatriptan activates this receptor to cause vasoconstriction, an action in humans correlating with relief to migraine.

• Tablets
• Injection, sumatriptan (base) as the succinate salt
• Nasal spray

phenytoin sodium (extended)

antiepileptic

increases the extrusion of sodium ions from neurons and cardiac myocytes. This produces a stabilization of the excitable membrane to repetitive stimuli. The primary site of action appears to be the motor cortex.

Capsules (extended-release)

promethazine hydrochloride

antiemetic

competitively inhibits histamine at the H₁ receptor site causing a spasmolytic and decongestant effect. Antihistimines will prevent, but not reverse, histamine-mediated reactions.

• Tablets
• Syrup, Phenergan Plain
• Suppositories
• Injection

prednisolone sodium phosphate

anti-inflammatory

Prednisolone is a synthetic adrenocorticoid with predominantly glucocorticoid properties. Its pharmacological effects include promotion of gluconeogenesis; increased deposition of glycogen in the liver; inhibition of the utilization of glucose; anti-insulin activity; increased catabolism of protein; increased lipolysis; stimulation of fat synthesis and storage; increased glomerular filtration rate with an increase in urinary excretion rate; increased calcium excretion; depressed production of eosinophils and lymphocytes; stimulation of erythropoiesis and production of polymorphonuclear leukocytes; and inhibition of inflammtory response.

• Tablets (regular, orally disintegrating)
• Solution

prednisolone sodium phosphate

anti-inflammatory

Prednisolone is a synthetic adrenocorticoid with predominantly glucocorticoid properties. Its pharmacological effects include promotion of gluconeogenesis; increased deposition of glycogen in the liver; inhibition of the utilization of glucose; anti-insulin activity; increased catabolism of protein; increased lipolysis; stimulation of fat synthesis and storage; increased glomerular filtration rate with an increase in urinary excretion rate; increased calcium excretion; depressed production of eosinophils and lymphocytes; stimulation of erythropoiesis and production of polymorphonuclear leukocytes; and inhibition of inflammatory response.

• Tablets (regular, orally disintegrating)
• Solution

drospirenone and ethinyl estradiol (24)

oral contraceptive

oral contraceptives cause suppression of luteinizing hormone (LH) and follicle stimulation hormone (FSH) resulting in the inhibition of ovulation. Thickening of the cervical mucous (inhibiting sperm penetration) and alteration of the endometrium (which inhibits implantation) may also contribute to their effectiveness. The progestin drospirenone is a spironolactone analogue with antimineralcorticoid activity including the retention of potassium.

Tablets (28 day blister packs)

bumetanide

diuretic

inhibits reabsorption of sodium and chloride in the ascending limb of the loop of Henle. It also exerts a diuretic action in the proximal tubule, but not noticeably in the distal tubule.

• Tablets
• Injection

mirtazapine

antidepressant

mechanism of action may be due to its action as an antagonist of central presynaptic alpha-2 adrenergic inhibitory autoreceptors and heteroreceptors, an action that is postulated to result in an increase in central noradrenergic and serotonergic activity. Mirtazapine is also a potent antagonist of serotonin 5HT2 and 5HT3 receptors. It also a potent inhibitor of histamine H1 receptors and a moderate inhibitor of adrenergic alpha-1 and muscarinic receptors.

Tablets (regular, orally disintegrating)

gemfibrozil

antihyperlipidemic

decreases serum triglycerides and VLDL-cholesterol and increases HDL-cholesterol. Reduction of triglycerides is due to an inhibition of peripheral lipolysis and reduction of hepatic extraction of free fatty acids. Reduction of VLDL-cholesterol is due to an inhibition of the synthesis of VLDL carrier apolipoprotein B. It is not known how gemfibrozil increases HDL-cholesterol.

Tablets

hydroxychloroquine sulfate

antimalarial

The exact mechanism of action of hydroxychloroquine in the treatment of malaria is unknown. It may raise the pH of certain components in sensitive parasites and interfere with lysosomal degradation of hemoglobin. It does not affect the exoerthrocytic tissue stages and therefore is not indicated for prophylaxis. It has a very large volume of distribution which adds to its long half-life of 3 days. Its mechanism of action in the treatment of discoid and systemic lupus erythematosus and rheumatoid arthritis is unknown.

Tablets

olopatadine hydrochloride (ophthalmic)

ophthalmic anti-allergy

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

Ophthalmic drops: 0.1% olopatadine HCl

olopatadine hydrochloride (ophthalmic)

ophthalmic anti-allergy

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

Ophthalmic drops: 0.2% olopatadine HCl

budesonide and formoterol fumarate dihydrate (inhalation)

antiasthmatic

Budesonide in a potent anti-inflammatory corticosteroid which shows inhibitory activities against multiple cell types (eg, mast cells, eosinophils, neutrophils, macrophages, and lymphocytes) and mediators (eg, histamine, eicosanoids, leukotrienes, and cytokines). Formoterol is a long-acting selective beta-2-adrenergic agonist which acts locally in the lung as a bronchodilator. Formoterol, through stimulation of adenyl cyclase, relaxes smooth muscle and inhibits the release of mast cell mediators such as histamine and leukotrienes.

Metered Dose Inhaler (MDI)

norethindrone and ethinyl estradiol

oral contraceptive

cause suppression of luteinizing hormone (LH) and follicle stimulation hormone (FSH) resulting in the inhibition of ovulation. Thickening of the cervical mucous (inhibiting sperm penetration) and alteration of the endometrium (which inhibits implantation) may also contribute to their effectiveness.

1/35-28 day pack

norethindrone and ethinyl estradiol

oral contraceptive

cause suppression of luteinizing hormone (LH) and follicle stimulation hormone (FSH) resulting in the inhibition of ovulation. Thickening of the cervical mucous (inhibiting sperm penetration) and alteration of the endometrium (which inhibits implantation) may also contribute to their effectiveness.

1/35-28 day pack

norethindrone and ethinyl estradiol

oral contraceptive

cause suppression of luteinizing hormone (LH) and follicle stimulation hormone (FSH) resulting in the inhibition of ovulation. Thickening of the cervical mucous (inhibiting sperm penetration) and alteration of the endometrium (which inhibits implantation) may also contribute to their effectiveness.

1/35-28 day pack

testosterone gel (topical)

hormone

Endrogenous androgens, including testosterone and dihydrotestosterone (DHT) are the major sex hormones in males and are involved in development of the male sex characteristics. Testosterone and DHT binds to certain receptor proteins found in the cytoplasm of sensitive cells and forms an hormone-receptor complex. This hormone-receptor complex enters the nucleus of the cell where it reacts with chromatin, or DNA. The hormone, or possibly the receptor, then uses stored information to stimulate, or in some cases inhibit, the transcription of m-RNA. The stimulation of m-RNA results in the synthesis of specific proteins and ultimately specific enzymes that carry out its actions. Topically applied testosterone gel provides continuous absorption of testosterone for 24 hours.

• Topical 1% gel pump
• Topical 1% gel foil packets
• Topical 1.62% gel

testosterone gel (topical)

hormone

Endrogenous androgens, including testosterone and dihydrotestosterone (DHT) are the major sex hormones in males and are involved in development of the male sex characteristics. Testosterone and DHT binds to certain receptor proteins found in the cytoplasm of sensitive cells and forms an hormone-receptor complex. This hormone-receptor complex enters the nucleus of the cell where it reacts with chromatin, or DNA. The hormone, or possibly the receptor, then uses stored information to stimulate, or in some cases inhibit, the transcription of m-RNA. The stimulation of m-RNA results in the synthesis of specific proteins and ultimately specific enzymes that carry out its actions. Topically applied testosterone gel provides continuous absorption of testosterone for 24 hours.

Topical 2% gel

testosterone gel (topical)

hormone

Endrogenous androgens, including testosterone and dihydrotestosterone (DHT) are the major sex hormones in males and are involved in development of the male sex characteristics. Testosterone and DHT binds to certain receptor proteins found in the cytoplasm of sensitive cells and forms an hormone-receptor complex. This hormone-receptor complex enters the nucleus of the cell where it reacts with chromatin, or DNA. The hormone, or possibly the receptor, then uses stored information to stimulate, or in some cases inhibit, the transcription of m-RNA. The stimulation of m-RNA results in the synthesis of specific proteins and ultimately specific enzymes that carry out its actions. Topically applied testosterone gel provides continuous absorption of testosterone for 24 hours.

gel

clozapine

antipsychotic

classified as an "atypical" antipsychotic drug because its profile of binding to dopamine receptors and its effects on various dopamine mediated behaviors differ from those exhibited by more typical antipsychotic drugs. In particular, although clozapine does interfere with the binding of dopamine at both D-1 and D-2 receptors, it does not induce catalepsy nor inhibit apomorphine-induced stereotypy. This may explain its relative freedom from extrapyramidal side effects. Clozapine also acts as an antagonist at adrenergic, cholinergic, histaminergic and serotonergic receptors.

Tablets

varenicline tartrate

smoking cessation aid

partial agonist at nicotinic receptors in the brain. Its mechanism of action appears to be due to selective binding to the alpha-4-beta-2 neuronal nicotinic acetylcholine receptors. Varenicline has mild agonist activity at these receptors although at a much less degree than that of nicotine. By occupying these receptor sites, varenicline prevents stimulation by nicotine of the central nervous mesolimbic dopamine system. This is the system believed to be responsible for the positive reward effect experienced through smoking. Varenicline also has mild affinity to serotonin 5-HT3 receptors.

Tablets

insulin detemir (Levemir)

antidiabetic

insulin is the primary hormone responsible for carrying out proper glucose utilization in metaboic processes. In adipose and muscle tissue, insulin activates specific enzymes, promotes the transport of monosaccharides (including glucose) across cell membranes and facilitates the transformation of intracellular amino acids into proteins. Insulin detemir is a recombinant human insulin analog that is long-acting (up to 24 hours). Insulin detemir differs from human insulin in that the amino acid threonine at position B30 has been omitted, and a C14 fatty acid chain has been attached to the amino acid B29. Insulin detemir produces a prolonged action after injection due to a strong self-association of drug molecules and albumin binding.

Solution for injection

phenazopyridine hydrochloride

urinary tract analgesic

excreted in the urine where it exerts a topical analgesic effect on the urinary tract mucosa. Clinical effects include relief of pain, burning, urgency and frequency. Phenazopydridine's exact mechanism of action is unknown.

Tablets

sildenafil citrate

Agent for erectile dysfunction

The physiology of the erection of the penis involves the release of nitric oxide in the corpus cavernosum following sexual stimulation. Nitric oxide then activates the enzyme guanylate cyclase which increases cGMP resulting in smooth muscle relaxation in the corpus cavernosum and allowing inflow of blood. Sildenafil citrate inhibits phosphodiesterase type 5 (PDE5) which is responsible for degradation of cGMP in the corpus cavernosum. The increased levels of cGMP allows inflow of blood and resulting erection. Sildenafil citrate has no effect in the absence of sexual stimulation.

Tablets

sitagliptin phosphate

antidiabetic

inhibits the dipeptidyl peptidase-4 (DDP-4) enzyme. DDP-4 is responsible for deactivating the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). These hormones are released by the intestine in response to food and are credited with increasing insulin synthesis and release from pancreatice beta cells. GLP-1 also decreases hepatic glucose production by lowering glucagon secretion from pancreatic alpha cells. By inhibiting DDP-4, sitagliptin increases insulin and decreases glucagon in response to elevated blood glucose. Inhibition of DDP-4 by sitagliptin lasts for 24 hours.

Tablets

progesterone (oral)

hormone replacement

Progestins increase the synthesis of RNA by interacting with chromatin (DNA), causing the transformation of proliferative endometrium into secretory endometrium in women with adequate endogenous estrogen.

Capsules

atomoxetine hydrochloride

CNS agent for ADHD

The exact mechanism of action of atomoxetine in the treatment of ADHD is unknown. It may be related to a selective inhibition of the pre-synaptic norepinephrine transporter. After oral absorption, atomoxetine undergoes oxidative metabolism through the CYP2D6 pathway.

Capsules

chlorhexidine gluconate

antiplaque rinse

an effective antimicrobial against both gram-positive and gram-negative bacteria and does not seem to result in significant bacterial resistance. Its activity is caused by a disruption of the plasma membrane of the bacterial cell. Peridex is poorly absorbed from the gastrointestinal tract. After rinsing, 30% of the active ingredient chlorhexidine gluconate is retained in the oral cavity. The retained drug is slowly released into the oral fluids.

Oral rinse

chlorhexidine gluconate

antiplaque rinse

an effective antimicrobial against both gram-positive and gram-negative bacteria and does not seem to result in significant bacterial resistance. Its activity is caused by disruption of the plasma membrane of the bacterial cell. After rinsing, 30% of the active ingredient chlorhexidine gluconate is retained in the oral cavity. The retained drug is slowly released into the oral fluids.

Oral rinse

diclofenac sodium (topical)

nonsteroidal anti-inflammatory

The exact mechanism of action of diclofenac is unknown. It may be due to decreased prostaglandins, thromboxanes, and prostacyclin formation through an inhibition of cyclooxygenase (COX), an early component of the arachidonic acid cascade. Systemic exposure after topical application is much less than after oral administration.

Gel: 1% diclofenac sodium

estradiol (oral)

hormone/estrogen

17 beta-estradiol is the major estrogenic hormone secreted by the human. Estradiol binds to certain receptor proteins found in the cytoplasm of sensitive cells and forms an estrogen-receptor complex. This estrogen-receptor complex enters the nucleus of the cell where it reacts with chromatin, or DNA. THe estrogen, or possibly the receptor, then uses stored information to stimulate, or in some cases inhibit, the transcription of m-RNA. The stimulation of m-RNA results in the synthesis of specific proteins and ultimately specific enzymes that carry out its actions. Estrogens cause growth and development of the vagina, uterus, and fallopian tubes, enlargement of the breasts, and other tangible and intangible attributes of femininity.

Tablets

raloxifene hydrochloride

osteoporosis agent

a selective estrogen receptor modulator. Decreases in estrogen levels after menopause lead to bone resorption and bone loss. Raloxifene decreases bone resorption by producing an estrogen-like effect on bone. It also possesses estrogen-like activity on lipid metabolism (decrease in total and LDL cholesterol levels). Raloxifene is an estrogen antagonist in uterine and breast tissue.

Tablets

insulin (Humulin)

antidiabetic

Insulin is the primary hormone responsible for carrying out proper glucose utilization in metabolic processes. In adipose and muscle tissue, insulin activates specific enzymes, promotes the transport of monosaccharides (including glucose) across cell membranes and facilitates the transformation of intracellular amino acids into proteins. Insulin also decreases the formation of triglycerides. Humulin insulins are semisynthetic formulations of human insulin.

• NPH (N): Isophane insulin suspension, 100 units/mL
• Regular (R): Insulin, 100 units/mL and 500 units/mL
• 70/30: 70% isophane/30% insuli, 100 units/mL

hyoscyamine sulfate

GI antispasmodic

inhibits the muscarinic action of acetylcholine on smooth muscle. Blockage does not occur at the autonomic ganglia. Hyoscyamine relaxes bladder smooth muscle which decreases urgency, frequency, urinary leakage, and dysuria. It also inhibits gastric, pharyngeal, tracheal, and bronchial secretions.

• Tablets (regular, sublingual)
• Elixir
• Drops

hyoscyamine sulfate

GI antispasmodic

inhibits the muscarinic action of acetylcholine on smooth muscle. Blockage does not occur at the autonomic ganglia. Hyoscyamine relaxes bladder smooth muscle which decreases urgency, frequency, urinary leakage, and dysuria. It also inhibits gastric, pharyngeal, tracheal, and bronchial secretions.

Tablets (extended-release)

hyoscyamine sulfate

GI antispasmodic

inhibits the muscarinic action of acetylcholine on smooth muscle. Blockage does not occur at the autonomic ganglia. Hyoscyamine relaxes smooth muscle which decreases urgency, frequency, urinary leakage, and dysuria. It also inhibits gastric, pharyngeal, tracheal, and bronchial secretions.

• Tablets (regular, sublingual)
• Elixir
• Drops

hyoscyamine sulfate

GI antispasmodic

inhibits the muscarinic action of acetylcholine on smooth muscle. Blockage does not occur at the autonomic ganglia. Hyoscyamine relaxes smooth muscle which decreases urgency, frequency, urinary leakage, and dyuria. It also inhibits gastric, pharyngeal, tracheal, and bronchial secretions.

• Tablets (regular, sublingual)
• Elixir
• Drops

telmisartan

antihypertensive

Angiotensin II is a potent vasoconstrictor, the primary vasoactive hormone of the renin-angiotensin system and an important component in the pathophysiology of hypertension. It also stimulates aldosterone secretion by the adrenal cortex. Telmisartan blocks 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. Telmisartan does not inhibit ACE or bind to or block other hormone receptors or ion channels known to be important in cardiovascular regulation.

Tablets (individually sealed in blister packs)