Quiz 7 - Phar 605

norethindrone, ethinyl estradiol, and ferrous fumarate/iron

oral contraceptive

suppression of luteinizing hormone (LH) and follicle stimulation hormone (FSH) result in the inhibition of ovulation. Thickening of the cervical mucous (inhibiting sperm penetration) and alteration of the endometrium (which inhibits implantation) might also contribute to the effectiveness of oral contraceptives.

Tablets

norethindrone, ethinyl estradiol, and ferrous fumarate/iron

oral contraceptive

suppression of luteinizing hormone (LH) and follicle stimulation hormone (FSH) result in the inhibition of ovulation. Thickening of the cervical mucous (inhibiting sperm penetration) and alteration of the endometrium (which inhibits implantation) might also contribute to the effectiveness of oral contraceptives.

Tablets

norethindrone, ethinyl estradiol, and ferrous fumarate/iron

oral contraceptive

suppression of luteinizing hormone (LH) and follicle stimulation hormone (FSH) result in the inhibition of ovulation. Thickening of the cervical mucous (inhibitng sperm penetration) and alteration of the endometrium (which inhibits implantation) might also contribute to the effectiveness of oral contraceptives.

Tablets

benazepril hydrochloride

antihypertensive

thought to be due to its suppression of the renin-angiotensin-aldosterone system by competitively inhibiting the angiotensin-converting enzyme (ACE). ACE converts angiotensin I to angiotensin II, one of the most potent vasoconstrictors known. Inhibition of ACE decreases plasma angiotensin II which leads to decreased aldosterone secretion. The latter may cause an increase in serum potassium. The net result is a decrease in peripheral resistance.

Tablets

fentanyl (transdermal)

opioid analgesic

analgesia is produced centrally via action on the central opiate receptors. Fentanyl interacts predominantly with opioid u-receptor.

Transdermal systems (patches)

nitrofurantoin

antibacterial

may be due to an inhibition of acetyl-coenzyme A, interfering with the metabolism of carbohydrates in susceptible bacteria.

Capsules

nitrofurantoin

antibacterial

may be due to an inhibition of acetyl-coenzyme A, interfering with the metabolism of carbohydrates in susceptible bacteria.

Capsules

nitrofurantoin

antibacterial

may be due to an inhibition of acetyl-coenzyme A, interfering with the metabolism of carbohydrates in susceptible bacteria.

Suspension (25 mg/5 mL)

norethindrone acetate, ethinyl estradiol, and ferrous fumarate

oral contraceptives

Norethindrone is a progestogen and ethinyl estradiol is an estrogen. Absorption of both components from the GI tract is rapid with maximum plasma concentrations occurring 1 to 4 hours postdose. Norethindrone undergoes reduction and conjugation while ethinyl estradiol undergoes oxidation and conjugation. Oral contraceptives cuase 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.

Tablets (28 blister card)

norgestimate and ethinyl estradiol

oral contraceptive

suppression of luteinizing hormone (LH) and follicle stimulation hormone (FSH) result 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.

Tablets (Ortho Tri-Cyclen Lo)

digoxin

inotropic agent

digitalis glycosides inhibit membrane bound Na+/K+ ATPase resulting in an increased intracellular Na+ concentration and a slightly decreased intracellular K+ concentration. The increased intracellular Na+ leads to an influx of extracellular Ca2+. The net result is an increase in the force and velocity of systolic contractions, a slowing of the heart rate, and a decreased conduction velocity through the AV node.

• Tablets
• Elixir Pediatric

digoxin

inotropic agent

digitalis glycosides inhibit membrane bound Na+/K+ ATPase resulting in an increased intracellular Na+ concentration and a slightly decreased intracellular K+ concentration. The increased intracellular Na+ leads to an influx of extracellular Ca2+. The net result is an increase in the force and velocity of systolic contractions, a slowing of the heart rate, and a decreased conduction velocity through the AV node.

• Tablets
• Elixir Pediatric

fluticasone propionate (inhalation)

antiasthmatic

adrenocorticoids bind to certain receptor proteins found in the cytoplasm of sensitive cells to form a steroid-receptor complex. The 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 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 antiallergy and anti-inflammatory actions.

inhalation aerosol in a metered dose inhaler (MDI)

levetiracetam

anticonvulsant

precise MOA is unknown. It is a pyrolidine derivative and is chemically unrelated to existing antiepileptic drugs. In animal models, it protects against pilocarpine and kainic acid-induced secondary generalized activity from focal seizures. It also inhibits burst firing in the hippocampus without affecting normal neuronal excitability. This may prevent propagation of seizure activity.

• Tablet (IR, ER)
• Oral solution (IR)

terazosin hydrochloride

antihypertensive

decreases total peripheral resistance by competitively blocking alpha-1-adrenoreceptors. This action results in dilation of arterioles and veins which leads to decreased blood pressure. Diastolic pressure is affected more than systolic pressure. In the treatment of benign prostatic hyperplasia, terazosin relaxes smooth muscle in the bladder neck and prostate, resulting in improvements in urine flow rates.

Capsules

acyclovir

antiviral

synthetic acyclic purine nucleotide which in vitro inhibits Herpes simplex types 1 and 2, varicella-zoster, Epstein-Barr, and cytomegalovirus. In vitro, the inhibitory activity of acyclovir is highly selective for Herpes simplex virus. Acyclovir is preferentially taken up and converted to the active triphosphate form by HSV infected cells which then interferes with the HSV DNA polymerase and inhibits viral DNA replication. In vitro, as the acyclovir triphosphate is incorporated into the growing chains of DNA by viral and cellular DNA polymerase, the DNA chain is terminated.

• Tablets
• Capsules
• Ointment
• Cream
• Suspension
• Powder for Injection

irbesartan

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. Irbesartan 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. Irbesartan does not inhibit ACE or bind to or block other hormone receptors or ion channels known to be important in cardiovascular regulation.

Tablets

budesonide (inhalation)

antiasthmatic

adrenocorticoids bind to certain receptor proteins found in the cytoplasm of sensitive cells to form a steroid-receptor complex. The 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 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 antiallergy and anti-inflammatory actions. Budesonide has strong glucocorticoid and weak mineralcorticoid activity.

• Suspension for Inhalation
• Metered Dose Inhaler (Flexhaler)

valacyclovir hydrochloride

antiviral

Valacyclovir is rapidly converted to acyclovir by first-pass intestinal and/or hepatic metabolism. Acyclovir is a synthetic acyclic purine nucleotide which in vitro inhibits Herpes simplex types 1 and 2, varicella-zoster, Epstein-Barr, and cytomegalovirus. In vitro, the inhibitory activity of acyclovir is highly selective for Herpes simplex virus (HSV). Acyclovir is preferentially taken up and converted to the active triphosphate form by HSV infected cells which then interferes with the HSV DNA polymerase and inhibits viral DNA replication. In vitro, as the acyclovir triphosphate is incorporated into the growing chains of DNA by viral and cellular DNA polymerase, the DNA chain is terminated.

Tablets

desvenlafaxine

antidepressant

Non-clinical studies have shown that desvenlafaxine is a potent inhibitor of neuronal serotonin and norepinephrine reuptake.

Tablets (Extended-release)

carbamazepine

anticonvulsant

appears to act by reducing polysynaptic responses and blocking the post-tetanic potentiation.

• Tablets (chewable, oral)
• Suspension

carbamazepine

anticonvulsant

appears to act by reducing polysynaptic responses and blocking the post-tetanic potentiation.

Tablets (Extended-Release)

carbamazepine

anticonvulsant

appears to act by reducing polysynaptic responses and blocking the post-tetanic potentiation.

Capsules (Extended-release)

carbamazepine

anticonvulsant

appears to act by reducing polysynaptic responses and blocking the post-tetanic potentiation.

Capsules (Extended-release)

levonorgestrel with ethinyl estradiol

oral contraceptive

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

Tablets, 28 day pack

levonorgestrel with ethinyl estradiol

oral contraceptive

suppression of luteinizing hormone (LH) and follicle stimulation hormone (FSH) result 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.

Tablets, 28 day pack

lithium carbonate

antipsychotic

exact MOA of lithium in the treatment of mania is unknown. Its mood-stabilizing effects may be due to an antagonism of the release of norepinephrine and dopamine from nerve terminals or from increasing the reuptake and inactivation of catecholamines. Lithium does not inhibit the release of serotonin. Another potential mechanism of action is through depletion of phosphatidylinositides in selected cells in the CNS. This may decrease the responsiveness of neurons to various neurotransmitters.

• Tablets (regular, sustained-release)
• Capsules
• Oral solution

lithium carbonate

antipsychotic

exact MOA of lithium in the treatment of mania is unknown. Its mood-stabilizing effects may be due to an antagonism of the release of norepinephrine and dopamine from nerve terminals or from increasing the reuptake and inactivation of catecholamines. Lithium does not inhibit the release of serotonin. Another potential mechanism of action is through depletion of phosphatidylinositides in selected cells in the CNS. This may decrease the responsiveness of neurons to various neurotransmitters.

• Tablets (regular, sustained-release)
• Capsules
• Oral solution

lithium carbonate

antipsychotic

exact MOA of lithium in the treatment of mania is unkown. Its mood-stabilizing effects may be due to an antagonism of the release of norepinephrine and dopamine from nerve terminals or from increasing the reuptake and inactivation of catecholamines. Lithium does not inhibit the release of serotonin. Another potential mechanism of action is through depletion of phosphatidylinositides in selected cells in the CNS. This may decrease the responsiveness of neurons to various neurotransmitters.

• Tablets (regular, sustained-release)
• Capsules
• Oral solution

etonogestrel and ethinyl estradiol (vaginal)

contraceptive

combination estrogen and progestin 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. Etonogrestrel is the progestin component of Nuvaring and is the primary active metabolite produced following oral administration of desogestrel.

vaginal ring

lovastatin

antihyperlipidemic

after oral ingestion, lovastatin is hydrolyzed to its beta-hydroxyacid form, becoming a specific inhibitor of HMG-CoA reductase. This enzyme is responsible for the conversion of HMG-CoA to mevalonate, an early rate limiting step in the synthesis of cholesterol. In therapeutic concentrations, HMG-CoA reductase is not completely blocked, allowing biologically necessary amounts of mevalonate to be produced. Mevacor reduces both normal and elevated LDL (low density lipoprotein) concentrations and VLDL (very low density lipoprotein) concentrations. It is not known whether Mevacor's therapeutic effect is due to an increased LDL catabolism, a decrease in VLDL (a precursor to LDL), or a direct decrease in LDL production. In addition to LDL reduction, Mevacor increases HDL (high density lipoprotein) concentrations. High LDL and low HDL levels have been shown to be risk factors in coronary heart disease.

Tablets