question

Levothyroxine/Synthroid class

answer

Thyroid hormone replacement (synthetic T4) dosed in mcg

question

Levothyroxine/Synthroid indication

answer

Hypothyroidism. Also TSH suppression in select cases of thyroid nodules and thyroid cancer

question

Levothyroxine/Synthroid MOA

answer

Replaces normal levels of T4 and T3 (T4 is converted into T3 in the periphery.)

question

Levothyroxine/Synthroid char.

answer

PO/ IV. Oral absorption ~70%. Once a day dosing. Slow onset of action. Half life of ~1 week. Takes 6-8 weeks to achieve steady state. Treatment is usually life long. Follow patient's clinical response and serum TSH. Hold or reduce dose if any complaints of angina. Begin at low dose and advance dosage slowly in patients over age 65 or in any patients with history of coronary artery disease.

question

Levothyroxine/Synthroid side effects

answer

Toxicity directly related to thyroxine level and manifests as palpitations, tachycardia, intolerance to heat, and anxiety. Long term elevation of serum T4 may accelerate cardiac disease and osteoporosis. In patients that have Addison's disease and hypothyroidism, thyroid replacement without first replacing cortisol can be fatal.

question

Thyroid USP/Armour class

answer

Thyroid hormone (T4 and T3 as well as T2 and T1) obtained from desiccated animal thyroid gland

question

Thyroid USP/Armour indication

answer

hypothyroidism

question

Thyroid USP/Armour MOA

answer

Replaces both T4 and T3

question

Thyroid USP/Armour char.

answer

PO. Generally standardized to iodine content. Initiate medication at low dose and increase dosage according to patient response. More cautious dosing in patients over age 65 or if history of cardiac disease

question

Thyroid USP/Armour side effects

answer

Similar to those of Thyroxine/ Synthroid. Follow patient's clinical response and serum TSH. Hold or reduce dose if any complaints of angina. Begin at low dose and advance dosage slowly in patients over age 65 or in any patients with history of coronary artery disease. In patients that have Addison's disease and hypothyroidism, thyroid replacement without first replacing cortisol can be fatal.

question

Liothyronine/Cytomel class

answer

Thyroid hormone replacement (synthetic T3) dosed in mcg

question

Liothyronine/Cytomel indication

answer

Patients with hypothyroidism that have demonstrated intolerance to T4 replacement therapy or no improvement on T4 replacement therapy. Myxedema coma. Also used for "Wilson's syndrome"

question

Liothyronine/Cytomel MOA

answer

Replaces T3

question

Liothyronine/Cytomel char.

answer

PO/IV. 100% oral absorption. Rapid onset of action. Half life of several hours

question

Liothyronine/Cytomel side effects

answer

Similar to T4. Higher peaks and troughs of T3 may increase risk of coronary artery disease and osteoporosis

question

Approximate equivalent doses of thyroid hormone preparations are as follows

answer

60 mg (1 grain) Thyroid USP (Armour) ~ = 100 mcg of T4 (Synthroid) ~ = 25 mcg of T3 (Cytomel)

question

Methimazole/Tapazole class

answer

Thionamide

question

Methimazole/Tapazole indication

answer

Hyperthyroidism (Grave's dis.) Can control hyperthyroidism until more definitive therapy (surgery or 131I therapy) is used. Patients may achieve a euthyroid state after treatment is discontinued. Treatment failure or recurrence of hyperthyroid state suggests that definitive treatment is necessary.

question

Methimazole/Tapazole MOA

answer

Inhibits transformation of inorganic iodine to organic iodine, therefore blocking the production of thyroxine. Also inhibits the coupling of iodotyrosine to form T3 and T4. Minimal effect of blocking the peripheral conversion of T4 to T3

question

Methimazole/Tapazole char.

answer

P.O. Once daily dosing. May take weeks to achieve therapeutic state, thus not used for thyroid storm. Concentrated in the thyroid. Does not affect thyroglobulin already stored in the thyroid gland

question

Methimazole/Tapazole side effects

answer

May cause hypothyroidism. Rash, edema, arthralgias may occur. Agranulocytosis is the most feared side effect. Drug is usually not given beyond a 6-12 month period. Not given during pregnancy as it can cross the placenta.

question

Propylthiouracil (PTU) class

answer

Thionamide

question

Propylthiouracil (PTU) indication

answer

Hyperthyroidism (Grave's disease) Can control hyperthyroidism until more definitive therapy (surgery or 131I therapy) is used. Patients may occasionally achieve a euthyroid state after treatment is discontinued

question

Propylthiouracil (PTU) MOA

answer

Inhibits transformation of inorganic iodine to organic iodine, blocking the production of thyroxine and inhibits the coupling of iodotyrosine to form T3 and T4. Notable effect of blocking the peripheral conversion of T4 to T3

question

Propylthiouracil (PTU) char.

answer

P.O. Once daily dosing. May take weeks to achieve therapeutic state, thus not used for thyroid storm. However, once a patient with thyroid storm who has been treated and stabilized, PTU is commonly used before definitive treatment by surgery or radioactive iodine ablation. Upon initiation of treatment, PTU affects the production of thyroid hormone but does not affect the T4 and thyroglobulin already stored in the thyroid gland.

question

Propylthiouracil (PTU) side effects

answer

May cause hypothyroidism. Rash, edema, arthralgias may occur. Agranulocytosis is the most feared side effect. Drug usually not given beyond a 6-12 month period. Category D but PTU is considered safer then Methimazole and is used in pregnancy when benefit outweighs potential risks.

question

Propanolol/Inderal class

answer

Non selective beta blocker

question

Propanolol/Inderal indication

answer

Blockade of adrenergic symptoms of hyperthyroidism (i.e. tachycardia, anxiety). Emergent treatment of thyroid storm.

question

Propanolol/Inderal MOA

answer

Beta-1 and Beta-2 receptor blockade

question

Propanolol/Inderal char.

answer

PO/IV

question

Propanolol/Inderal side effects

answer

Fatigue, sedation, impotency or depression may be noted

question

Iodine/S.S.K.I. class

answer

Elemental iodine

question

Iodine/S.S.K.I. indication

answer

Hyperthyroidism, thyroid storm

question

Iodine/S.S.K.I. MOA

answer

Large doses of iodine inhibit the release of thyroxine from the thyroid gland

question

Iodine/S.S.K.I. char.

answer

PO/IV. Usually given in the form of supersaturated potassium iodide (SSKI)

question

Iodine/S.S.K.I. side effects

answer

Rash, fever. Beneficial effects generally last no more then 2-3 weeks as thyroid gland appears to adapt and resumes secretion of thyroxine.

question

Radioactive iodine (131I) class

answer

Radioactive isotope

question

Radioactive iodine (131I) indication

answer

Thyroid gland ablation in cases of Grave's disease, thyroid nodules and in some cases of thyroid cancer

question

Radioactive iodine (131I) MOA

answer

Radioactive emission of beta particles results in destruction of thyroid tissue.

question

Radioactive iodine (131I) char.

answer

Oral route. Generally takes weeks for destruction of thyroid gland tissue to be complete.

question

Radioactive iodine (131I) side effects

answer

May cause tenderness and swelling during initial week of therapy. Nausea, vomiting may occur. No evidence of increased risk for malignancy of the thyroid gland or other head and neck structures has been noted. Prior to treatment, patients generally need to be rendered euthyroid by anti-thyroid drugs and/or doses of supersaturated potassium iodide (SSKI). Strictly contraindicated in pregnancy -Category X. I-131 given during pregnancy can irreversibly damage the fetal thyroid tissue. When given to a nursing mother, radioactive iodine can reach a baby through the breast milk. Pregnancy should be delayed until at least six to 12 months after I-131 treatment, since the treatment exposes the ovaries to radiation. Extremely high doses may result in bone marrow depression which is usually transient. Acute leukemia has been reported. Most patients who have undergone radioactive iodine treatment for Grave's disease will result in hypothyroid state requiring life long administration of thyroid hormone replacement. Men who receive RAI treatment for thyroid cancer may have decreased sperm counts and temporary infertility for periods of roughly two years. A physician may discuss sperm banking with a male patient who is expected to need several doses of RAI for thyroid cancer.

question

The present criteria for the diagnosis of diabetes mellitus include

answer

A confirmed fasting blood glucose level of >126 mg/dL. Non-fasting blood glucose of >200 mg/dL in a patient presenting with symptoms or exam findings consistent with diabetes. A positive oral glucose tolerance test resulting in a blood glucose of >200mg/ dL at 2 to 3 hours after a bolus of glucose

question

Metformin/Glucophage class

answer

the single member of the biguanide class that is currently approved for use in the U.S.

question

Metformin/Glucophage indication

answer

Type 2 diabetes

question

Metformin/Glucophage MOA

answer

Metformin decreases hepatic glucose production and to a lesser extent, enhances insulin sensitivity in skeletal muscle. Metformin used alone generally does not cause hypoglycemia.

question

Metformin/Glucophage char.

answer

Metformin has a similar efficacy to the sulfonylureas (for ex. Glipizide/Glucotrol and Glyburide/Micronase) in terms of reducing a patient's fasting serum glucose, non-fasting serum glucose and A1c levels Generic Metformin comes in 500, 850 and 1000 mg tabs and is generally dosed twice a day. A usual daily dose is 1500 to 2000 mg at a cost of ~$55.00/ month. The generic form of extended release Metformin comes in 500 and 750 mg doses and is generally dosed once a day at 1500 to 2000 mg at a cost of ~$60.00 per month. Brand name substitutions such as Glucophage or Fortamet generally raises the monthly cost to $100 or more.

question

Metformin/Glucophage side effects

answer

Unlike the sulfonylureas, Metformin can cause a patient to experience a modest reduction of weight (between 4 to 7 lbs.) rather than weight gain. The most commonly noted complaint by patients taking Metformin is abdominal cramping and nausea. These effects may be notably reduced by using the slow or extended release forms of the drug. Metallic taste is another common side effect. Patients taking Metformin have an increased risk for the development of B 12 deficiency and supplementation with a B complex should be standard practice. The most serious side effect of Metformin is the development of lactic acidosis which is rare but can prove fatal. The risk for lactic acidosis is markedly diminished by not using the drug in patients with impaired renal function. Metformin should not be started or if started, should be stopped in patients with renal insufficiency (As a guideline: a serum creatinine >1.5 mg/dL in males and a serum creatinine >1.4 dL in females.)

question

Sulfonylureas MOA

answer

Sulfonylureas stimulate intact beta cells of the pancreas to release more insulin. Increased insulin release occurs as a result of the interaction of a sulfonylurea with the ATP-sensitive potassium channels in the beta cell membrane. By partially blocking potassium channels, the time the beta cell spends in the calcium release stage of cell signaling is increased which initiates more insulin release from the affected beta cell.

question

Chlorpropamide (Diabinese) and Tolbutamide (Orinase) class

answer

the only 1st generation sulfonylureas still available in the US today but they are seldom used

question

Glipizide (Glucotrol), Glyburide (Micronase, Diabeta) and Glimepiride* (Amaryl) class

answer

2nd generation sulfonylurea drugs (Glimepiride is sometimes listed as a 3rd generation)

question

Sulfonylurea side effects

answer

The adverse effect of most concern with the use of a sulfonylurea is hypoglycemia, particularly in patients with impaired renal or hepatic function. Weight gain may be the most commonly noted side effect of the sulfonylureas. As a general rule, all of the agents in the sulfonylurea class generally become ineffective in achieving glucose control after 5 to 10 years of use All drugs from this class are to be avoided in patients with a known sulfa allergy.

question

Choosing a sulfonylurea

answer

The literature suggests that Gyburide (Micronase) appears to have a greater incidence of hypoglycemic events than either Glimepiride (Amaryl) or Glipizide (Glucotrol). All of the sulfonylureas are available as generic drugs and range in cost from $4 (generic Glucotrol) to ~$20.00 (generic Glyburide) per month. The brand name versions of these drugs range in monthly cost from $30.00 (Diabeta) to ~$50.00 (Micronase).

question

Sulfonylureas char.

answer

The dosing schedule for all of these agents is usually one dose in the morning.

question

Meglitinides MOA

answer

The Meglitinides are a drug class that stimulate the beta cells to release insulin Nateglinide (Starlix) and Repaglinide (Prandin), although structurally different from the sulfonylureas, also bind to ATP-sensitive potassium channels on beta cells and thereby increase insulin release.

question

Nateglinide (Starlix) and Repaglinide (Prandin) class

answer

meglitinides These drugs are chemically unrelated to the sulfonylureas and thus they are also referred to as the non-sulfonylurea secretagogues

question

Meglitinides char.

answer

Nateglinide appears to be less effective than Repaglinide, which has proven to be equally effective to the Sulfonylureas in improving blood glucose control and lowering A1c levels. Both Repaglinide and Nateglinide are rapidly absorbed from the GI tract causing the plasma levels of insulin to peak within 30 to 60 mins. and thereafter are rapidly cleared These drugs are to be taken 3 to 4 times a day, before each meal and if a meal is missed, the drug should not be taken. There are no generic options available and the cost of using one of these drugs normally runs from $150.00 to $300.00 per month.

question

Meglitinides side effects

answer

Repaglinide and Nateglinide each cause hypoglycemia and weight gain similar to that seen with the Sulfonylureas. Both of these drugs are approved by the FDA for combined use with Metformin or with a drug from the Glitazone class but avoidance of combined use with a drug from the Sulfonylurea class is suggested due to the increased risk for hypoglycemia.

question

Thiazolidinediones/Glitazones MOA

answer

The TZDs or Glitazones improve insulin sensitivity in skeletal muscle cells, fat cells and liver cells and also decreases hepatic glucose production.

question

Rosiglitazone (Avandia) and Pioglitazone (ACTOS) class

answer

Thiazolidinediones/Glitazones

question

Thiazolidinediones/Glitazones char.

answer

Avandia and Actos are usually dosed once per day. The Glitazones may take 6 to 14 weeks to achieve their maximum effects. Avandia and ACTOS are FDA approved for use as monotherapy or in combination with Metformin or a Sulfonylurea. Only ACTOS is currently approved for concurrent use with insulin

question

Thiazolidinediones/Glitazones side effects

answer

The cardiovascular safety of the TZDs particularly Avandia, is controversial. Both Avandia and Actos increase the risk of congestive heart failure. A meta-analysis found an increased risk of myocardial infarction with Avandia but a more recent randomized prospective study specifically found no evidence of increased risk for myocardial infarction in patients taking Avandia. Liver functions tests should be performed being initiating treatment with a Glitazone, rechecked at 1 month and repeated again in 3 months to assess for any rise in ALT. Both Avandia and Actos have been associated with reduced bone density and an increased incidence of bone fractures. Weight gain from 5 to 10 pounds and much greater has been reported for each of these agents.

question

Alpha-glucosidase inhibitors MOA

answer

These agents inhibit the alpha-glucosidase enzymes that line the brush border of the small intestine, interfering with hydrolysis of carbohydrates and delaying absorption of glucose and other monosaccharides

question

Acarbose (Precose) and Miglitol (Glyset) class

answer

Alpha-glucosidase inhibitors

question

Alpha-glucosidase inhibitors char.

answer

In order to lower postprandial glucose levels, Acarbose or Miglitol must be taken with each meal

question

Alpha-glucosidase inhibitors side effects

answer

Given alone, either Acarbose or Miglitol will not cause hypoglycemia, but when given with either a Sulfonylurea or with insulin, these drugs can increase the risk for hypoglycemia. Unabsorbed carbohydrates can cause abdominal pain, diarrhea and flatulence due to both osmotic effects and bacterial fermentation. Acarbose in high doses has been associated rarely with moderate transaminase elevations and although considered to be a rare event fatal hepatic failure has been reported with Acarbose. In the event of hypoglycemia, oral treatment of patients taking these drugs must be with glucose rather than sucrose because alpha-glucosidase inhibitors interfere with the breakdown of sucrose. Acarbose and Miglitol are contraindicated in patients with chronic intestinal diseases, inflammatory bowel disease, colonic ulceration or any degree of intestinal obstruction.

question

Sitagliptin/Januvia MOA

answer

Sitagliptin works to competitively inhibit the enzyme dipeptidyl peptidase 4 (DPP-4). This enzyme breaks down the incretins GLP-1 and GIP, gastrointestinal hormones that are released in response to a meal. By preventing GLP-1 and GIP inactivation, GLP-1 and GIP are able to potentiate the secretion of insulin and suppress the release of glucagon by the pancreas. GLP-1 and GIP preservation drives blood glucose levels towards normal. As the blood glucose level approaches normal, the amounts of insulin released and the amounts glucagon suppressed diminish thus tending to prevent an overshoot of normal serum glucose levels and the subsequent hypoglycemia which can occur with other oral hypoglycemic agents.

question

Sitagliptin/Januvia char.

answer

Sitagliptin has been approved for use in the treatment of type 2 diabetes as monotherapy or in combination with Metformin, a Sulfonylurea or a TZD, but not with insulin. Efficacy trials of Sitagliptin, alone or in combination with Metformin, a Sulfonylurea or a Glitazone, have shown consistent reductions in A1c concentrations Januvia comes in 25, 50 and 100 mg tabs and the typical adult dose is generally 100 mg taken once per day. No generic versions of Januvia exist and a typical monthly cost to the patient ranges between $200.00 and $400.00.

question

Pramlintide/Symlin class

answer

Pramlintide is a synthetic form of the hormone amylin, which is produced along with insulin by the beta cells.

question

Pramlintide/Symlin indication

answer

Symlin is a drug that may be used by both type 1 diabetics and type 2 diabetics who use insulin and are still unable to reach their goal levels of HgbA1c

question

Pramlintide/Symlin MOA

answer

Symlin allows patients to use less insulin while lowering average blood sugar levels and also acts to substantially reduce the rise in blood sugar that usually occurs in diabetics immediately after meals

question

Pramlintide/Symlin char.

answer

Because of differences in the chemistry of Pramlintide and insulin, the two cannot be combined in the same vial or syringe and must be injected separately Pramlintide injections administered at meal times have been shown to improve A1c levels without causing increased hypoglycemia or causing weight gain. Pramlintide appears to actually promote modest weight loss.

question

Pramlintide/Symlin side effects

answer

The primary side effect of Pramlintide is nausea, which tends to improve over time and as the patient determines his or her optimal dose.

question

Exenatide/Byetta class

answer

Exenatide is the first in a new class of drugs referred to as incretin mimetics that have been developed for type 2 diabetes. It is a synthetic version of exendin-4, a naturally occurring hormone that was first isolated from the saliva of the Gila monster

question

Exenatide/Byetta indication

answer

type 2 diabetes

question

Exenatide/Byetta MOA

answer

Exenatide acts to lower blood glucose levels primarily by increasing insulin secretion.

question

Exenatide/Byetta char.

answer

injectable

question

Exenatide/Byetta side effects

answer

Because Exenatide only has this effect in the presence of elevated blood glucose levels, it does not increase the risk of hypoglycemia on its own, although hypoglycemia can occur if taken in conjunction with another hypoglycemic agent such as a sulfonylurea

question

Insulin indication

answer

Insulin replacement is required for the survival of all type 1 diabetics. Insulin is also used in the treatment of type 2 diabetes when diet, exercise and the use of oral hypoglycemic agents have failed to restore adequate glucose control

question

Insulin MOA

answer

Insulin stimulates glucose movement into cells, especially skeletal muscle and fat tissue which are not capable of allowing passive diffusion of glucose into myocytes and lipocytes and also activates the liver enzyme, hexokinase, which phosphorylates glucose, trapping it within the cell. Insulin activates transcription of at least 100 genes with the resultant action of increased "fuel" storage, increased cell growth and increased cell differentiation. Insulin is an anabolic hormone that promotes energy storage. Insulin promotes glycogen production and inhibits glycogenolysis. Insulin promotes fatty acid synthesis. Insulin promotes triglyceride storage. Insulin inhibits hepatic ketogenesis and hepatic gluconeogenesis.

question

Insulin char.

answer

Insulin can be given SQ, IM, and IV but cannot be utilized as an oral agent. (That is, until technology is capable of creating a delivery system that would allow oral insulin to survive proteolytic breakdown.) Insulin preparations are divided into four major categories depending upon onset of action and duration of action following SQ injection: Rapid acting Short acting Intermediate acting Long acting Combinations of above

question

Insulin side effects

answer

Insulin absorption from an injection site can vary dramatically depending upon blood flow and degree of fibrosis in sites that may be frequently used. Weight gain is a common side effect after beginning insulin treatment. Hypoglycemia as a result of insulin administration is perhaps the most feared potential complication as seizures, coma and death can result. Hypokalemia can also occur after insulin administration because potassium entry into the cell from the serum is stimulated. Injection sites may become fibrotic. Injection sites may also exhibit muscle or fat atrophy.

question

Lispro/Aspart and Humulog/Novalog class

answer

rapid acting insulin

question

Lispro/Aspart and Humulog/Novalog onset in hours

answer

≤0.25

question

Lispro/Aspart and Humulog/Novalog peak in hours

answer

0.5 - 1.5

question

Lispro/Aspart and Humulog/Novalog duration in hours

answer

3-5

question

Regular (Humulin R) class

answer

short acting insulin

question

Regular (Humulin R) onset in hours

answer

0.5-1

question

Regular (Humulin R) peak in hours

answer

2-4

question

Regular (Humulin R) duration in hours

answer

4-12

question

NPH (Humulin N) class

answer

intermediate acting insulin

question

NPH (Humulin N) onset in hours

answer

1-3

question

NPH (Humulin N) peak in hours

answer

6 - 10

question

NPH (Humulin N) duration in hours

answer

10-18

question

Glargine (Lantus) class

answer

long acting insulin

question

Glargine (Lantus) onset in hours

answer

4-6

question

Glargine (Lantus) peak in hours

answer

"flat"

question

Glargine (Lantus) duration in hours

answer

24

question

Insulin dosing

answer

One common insulin regimen is a combination of NPH and Regular insulin before breakfast and before dinner. Another commonly utilized insulin regimen is Regular insulin before meals with NPH or Ultralente in the afternoon. Lispro is utilized for its rapid onset of effects and is dosed ~15 minutes before each meal. Lantus insulin is utilized for its prolonged period of action which allows for improved coverage during sleeping hours.

question

Glucagon indication

answer

Glucagon is a potent hyperglycemic agent that is indicated for the treatment of severe hypoglycemia.

question

Glucagon MOA

answer

The mechanism of action of exogenous glucagon is stimulation of glucagon receptor sites with increased glucose levels obtained by breakdown of hepatic glycogen stores.

question

Glucagon char.

answer

Glucagon preparations are formulated from recombinant human DNA and can be administered IM, IV or SQ in 1 mg doses

question

Calcium supplementation recommended dosage

answer

The standard recommended amount of daily calcium intake for individuals less then 50 years of age is 1000 mg per day and the recommended dose for individuals over the age of 50 is 1,200 - 1,500 mg of calcium/ day. Breast-feeding women should have 2,000 mg of calcium supplementation per day

question

Calcium obtained from ___________ has been shown to have detectable levels of lead present as a contaminant.

answer

oyster shell source or dolomite (animal bone sources)

question

Current adult guidelines for vitamin D supplementation recommend the following:

answer

600 IU (15 mcg) for individuals from age 1 - 70 and 800 IU (20 mcg) for those individuals over 70 years of age. Data does exist to suggest that these recommendations should be at least double the above figures and that perhaps 2000 IU is a more appropriate daily dose.

question

Calcitriol (Rocaltrol)

answer

a prescription-form of vitamin D that can increase bone mass and decrease the rate of spinal fractures

question

Calcitriol (Rocaltrol) side effects

answer

calcitriol increases the risk for elevated serum calcium levels and patients on this medication require frequent monitoring

question

Magnesium dose

answer

An average dose of magnesium is 300 mg to 1000 mg a day

question

Strontium/Strontium ranelate dose

answer

Based on current evidence strontium ranelate can be taken at a dose of 500 mg to 1 gram daily to prevent osteoporosis and at a higher dose of 2 grams daily to treat existing osteoporosis

question

Strontium/Strontium ranelate side effects

answer

When taken in recommended doses, strontium supplements appear to be safe and usually free of side effects other than mild gastrointestinal upset and possible diarrhea. Attention to dosing of strontium is important as excessive intake (>2 gms per day) may actually weaken bone by replacing too much of the bone's calcium with strontium.

question

Alendronate/Fosamax class

answer

Bisphosphonates

question

Alendronate/Fosamax indication

answer

Prevention and treatment of osteoporosis, Paget's disease

question

Alendronate/Fosamax MOA

answer

Inhibition of osteoclast activity

question

Alendronate/Fosamax char.

answer

PO. Once daily. Instructions for taking Alendronate are noted under side effects.

question

Alendronate/Fosamax side effects

answer

GI - especially stomach ache, heartburn, nausea and possible erosive esophagitis. It is generally recommended that bisphosphonates be taken on an empty stomach in the morning with 6 to 8 ounces of water (not juice or carbonated or mineral water). The patient should remain upright and not eat for 30 minutes after each dose. Osteonecrosis of the jaw (rare) has been reported. Atypical femur fractures (sub-trochanteric and shaft). Myalgias.

question

Raloxifene/Evista class

answer

SERM

question

Raloxifene/Evista indication

answer

Increases bone mass and reduces the risk of vertebral fracture. Raloxifene has been shown to significantly reduce the incidence of breast cancer.

question

Raloxifene/Evista MOA

answer

Binding to select estrogen receptor sites. This drug developed to maintain beneficial estrogenic activity on bone and lipids and "anti-estrogenic" activity on endometrial and breast tissue

question

Raloxifene/Evista char.

answer

PO. Once per day.

question

Raloxifene/Evista side effects

answer

Hot flashes, arthralgias, myalgias, edema, pruritis, small but definite increased risk for development of deep venous thrombosis (DVT). Evista is contraindicated in pregnant and lactating women and women with active or past history of venous thromboembolic events, including DVT, PE and retinal vein thrombosis

question

Calcitonin/Miacalcin class

answer

Synthetic hormone to ↑serum Ca2

question

Calcitonin/Miacalcin indication

answer

Treatment of osteoporosis

question

Calcitonin/Miacalcin MOA

answer

Inhibits osteoclastic activity

question

Calcitonin/Miacalcin char.

answer

Nasal spray, IV. Not approved for the prevention of osteoporosis.

question

Calcitonin/Miacalcin side effects

answer

Nose bleeds and sinusitis noted with nasal spray. Both nasal spray and IV routes may cause headache, dizziness, edema, anorexia, diarrhea and skin rashes

question

Teriparatide/Forteo class

answer

Synthetic PTH analogue

question

Teriparatide/Forteo indication

answer

Approved for postmenopausal women and men with osteoporosis who are at high risk for having a fracture. Shown to reduce the risk of vertebral and non-vertebral fractures in postmenopausal women. In men, Teriparatide reduces the risk of vertebral fractures but the effect on nonvertebral fractures is still being investigated.

question

Teriparatide/Forteo MOA

answer

Activates bone turnover with osteoblasts being activated to a much greater extant than osteoclasts. Stimulates new bone formation in both spine and hip

question

Teriparatide/Forteo char.

answer

SQ. Once per day. Teriparatide is approved for use for up to 24 months.

question

Teriparatide/Forteo side effects

answer

The most commonly reported side effects are nausea, leg cramps and dizziness.

question

Estrogen/HRT indication

answer

Estrogen/hormone replacement therapy (ET/HRT) has been shown to reduce bone loss, increase bone density in both the spine and hip, and reduce the risk of hip and spine fractures in postmenopausal women When used solely for the prevention of postmenopausal osteoporosis, any ET/HRT regimen should only be considered for women at significant risk of osteoporosis and non-estrogen medications should be carefully considered as treatment options

question

Estrogen/HRT MOA

answer

In menopause estrogen deficiency induces cancellous as well as cortical bone loss. Highly increased bone resorption in cancellous bone leads to general bone loss and destruction of local architecture because of penetrative resorption and microfractures. In cortical bone the first response of estrogen withdrawal is enhanced endocortical resorption. Later, also intracortical porosity increases. These lead to decreased bone mass, disturbed architecture and reduced bone strength. At cellular level in bone, estrogen inhibits differentiation of osteoclasts thus decreasing their number and reducing the amount of active remodeling units.

question

Estrogen/HRT char.

answer

ET/HRT is approved for the prevention of postmenopausal osteoporosis and is most commonly administered in the form of a pill or skin patch. When estrogen is taken alone (i.e. Premarin), it can increase a woman's risk of developing endometrial cancer Before the specific dangers of conjugated equine estrogens were well understood and perhaps more importantly, accepted by the conventional medical community, the standard dose of conjugated equine estrogens (i.e. Premarin) was 0.625 mg/d. In a study by the NIH, esterified estrogens were not proven to pose the same risks to health as conjugated equine estrogens.

question

Estrogen/HRT side effects

answer

To potentially eliminate the increased risk for development of endometrial cancer for those women taking estrogen who have not had a hysterectomy, the hormone progestin is usually given in combination with estrogen (i.e. Prempro). Well documented side effects of ET/HRT include vaginal bleeding, breast tenderness, venous blood clots and increased risk for gallbladder disease. The Women's Health Initiative (WHI), a large government-funded research study, demonstrated that hormone replacement therapy with Prempro was associated with a modest but definite increase in the risk of breast cancer, stroke and MI. The WHI also demonstrated that Premarin use is associated with an increase in the risk of stroke.

question

Denosumab/Prolia class

answer

Denosumab is a human monoclonal antibody

question

Denosumab/Prolia indication

answer

Denosumab is a human monoclonal antibody that was approved by the FDA at the end of 2010 for the treatment of osteoporosis, bone metastases, rheumatoid arthritis, multiple myeloma and giant cell tumor of bone. At present, Prolia is approved for use in the treatment of osteoporosis but is not yet approved for use in the prevention of osteoporosis.

question

Denosumab/Prolia MOA

answer

Denosumab targets RANKL (the RANK ligand), a protein that acts as the primary signal to promote bone removal.

question

Denosumab/Prolia char.

answer

The drug is administered as a SQ injection, once every 6 months

question

Denosumab/Prolia side effects

answer

Similar to the adverse affect profile of other alpha-TNF agents, Prolia is known to increase susceptibility to infection

question

Statin class drugs

answer

Some studies have reported a lower risk of hip and other fractures in people who take statins drugs, such as Lovastatin (Mevacor) and Simvastatin (Zocor). To date, few clinical trials have been published, and more work is needed to confirm the possible beneficial effects that statins may have on bone density seen in these early studies.

question

Phytoestrogens

answer

Also called "dietary estrogens ", phyto-estrogens are a diverse group of naturally occurring nonsteroidal plant compounds that, because of their structural similarity with estradiol (17-β-estradiol), have the ability to bind at estrogen receptor sites. Once bound at estrogen sites, phyto-estrogenic compounds may cause estrogenic or/and anti-estrogenic effects. Phytoestrogens have the potential benefit of activating estrogen receptor sites on bone so as to enhancing bone remodeling while providing less risk of stimulating estrogen receptor sites on tissues such as breast, cervix and prostate.

question

Ipriflavone

answer

Ipriflavone, a synthetic isoflavone, has shown some promise in its ability to conserve bone in postmenopausal women. However, a three-year study of more than 400 postmenopausal women recently concluded that ipriflavone did not prevent bone loss. Further studies of phytoestrogens and isoflavones are ongoing.

question

The WHI-CEE trial arm

answer

Major results of this study were that, compared with placebo, women receiving estrogen alone experienced: No difference in risk MI An increased risk of stroke An increased risk of blood clots An uncertain effect on breast cancer risk No difference in risk for colorectal cancer A reduced risk of fracture

question

WHI-E+P trial arm

answer

This trial found that, compared with placebo, women receiving estrogen plus progestin had: Increased risk of myocardial infarction Increased risk of stroke Increased risk of DVT and PE Increased risk of breast cancer Decreased risk of colorectal cancer Fewer fractures The trial arm was ended early in 2002 when the researchers found that the subjects with estrogen plus progestin had a greater incidence of coronary heart disease, breast cancer, stroke, and pulmonary embolism than the subjects receiving placebo.

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BiEst

answer

BiEst is a combination of two estrogens: estriol and estradiol. It is most commonly formulated in an 80: 20 ratio of estriol to estradiol.

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TriEst

answer

TriEst is a combination of three estrogens: estriol, estradiol and estrone. It is most commonly found in a ratio of 80: 10: 10, estriol, estradiol and estrone.

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Conjugated estrogens/Premarin class

answer

Premarin, so named because it is obtained from the urine of pregnant mares is a preparation of conjugated estrogens - estrone and equillin.

question

Conjugated estrogens/Premarin indication

answer

Indications: Prevention and treatment of osteoporosis and of post-menopausal symptoms such as hot flashes, vaginal dryness and itching.

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Conjugated estrogens/Premarin MOA

answer

Conjugated estrogens undergo less first pass hepatic metabolism Alters gene transcription.

question

Conjugated estrogens/Premarin char.

answer

Oral and topical creams. Progesterone should be added to estrogen HRT in any women who has not undergone a hysterectomy.

question

Conjugated estrogens/Premarin side effects

answer

Vaginal bleeding, breast tenderness, increased risk of DVT, increased risk of atherosclerosis and coronary artery disease, increased risk for uterine and breast cancer. Side effects that may occur with Premarin include breast pain, increased breast size, palpitations, fever, hives, hoarseness, joint pain, stiffness or swelling, rash, redness of skin, shortness of breath, wheezing, edema and weight gain. Premarin is contraindicated if prior history of DVT or a history of breast, ovarian or uterine cancer is noted. Risks vs. benefits of use must be considered in every patient in whom hormone replacement therapy is being considered. Conjugated estrogens are in the FDA pregnancy category X.

question

Medroxyprogesterone/Provera class

answer

Medroxyprogesterone acetate is a synthetic variant of progesterone.

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Medroxyprogesterone/Provera indication

answer

Contraceptive, hormone replacement therapy, dysfunctional uterine bleeding and treatment of endometriosis

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Medroxyprogesterone/Provera MOA

answer

Alters gene transcription

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Medroxyprogesterone/Provera char.

answer

PO. Depo-form is I.M. The progestin component of HRT is added to prevent the development of endometrial hyperplasia and endometrial cancer

question

Medroxyprogesterone/Provera side effects

answer

Acne, weight gain, edema, breast tenderness, increased facial hair, insomnia, anxiety, weight loss or gain. Increases the ratio of LDL to HDL cholesterol and increases risk for DVT, Contraindicated if prior history of DVT or history of breast, ovarian or uterine cancer. Can cause birth defects if taken by pregnant women.

question

Combination Oral Contraceptive Pill (COCP) class

answer

a birth control method that includes a combination of an estrogen and a progestin.

question

Combination Oral Contraceptive Pill (COCP) indication

answer

When taken every day as directed, female fertility is inhibited. Taking oral contraceptives also appears to reduce the risk of colorectal cancer, and improves conditions such as pelvic inflammatory disease, dysmenorrhea, premenstrual syndrome and acne*. Additionally, birth control pills may reduce symptoms of endometriosis and polycystic ovary syndrome, and decrease anemia The use of oral contraceptives for five years or more appears to decreases the risk of ovarian cancer in later life by 50%. Combined oral contraceptive use also appears to reduce the risk of ovarian cancer by 40% and the risk of endometrial cancer by 50% compared to non-users. The risk reduction increases with duration of use, with an 80% reduction in risk for both ovarian and endometrial cancer with use for more than 10 years

question

Combination Oral Contraceptive Pill (COCP) MOA

answer

The estrogen component suppresses ovulation while the progestin prevents implantation in the endometrium and helps to make the cervical mucus impenetrable to sperm.

question

Combination Oral Contraceptive Pill (COCP) char.

answer

Combined oral contraceptive pills should be taken at approximately the same time each day. Most brands of combined pills are packaged in one of two different packet sizes, with days marked off for a 28 day cycle. For the 28-pill packet, 21 pills are taken, followed by week of placebo or sugar pills

question

Combination Oral Contraceptive Pill (COCP) side effects

answer

A woman on the pill will usually have a withdrawal bleed sometime during the placebo week, and is still protected from pregnancy during this week. There are also birth control pills (Yaz 28 and Loestrin 24) that have 24 days of active hormone pills, followed by 4 days of placebo. If one or more tablets are forgotten for more than 12 hours, contraceptive protection will be reduced. Multiple potential side effects including increased risk for cardiovascular disease, DVT, hypertension and stroke (especially in women who smoke or who are over 35 years of age. Other side effects include acne, depression, headache, edema, nausea and breast fullness.

question

Mini pill class

answer

A progestin only pill (the so called "mini-pill") is also available wherein a consistent dose of progestin with no estrogenic agent is delivered for 21 days

question

Mini pill indication

answer

This form of contraception is indicated if patient cannot tolerate an estrogenic agent or estrogen is contraindicated.

question

Mini pill side effects

answer

The mini-pill is not as effective as the combination pill and generally causes irregular menses more frequently than does the combination pill

question

Drospirenone class

answer

Drospirenone is a synthetic progestin that has been marketed under the names Yaz and Yasmin.

question

Drospirenone MOA

answer

Drospirenone differs from other synthetic progestins in that its pharmacological profile in preclinical studies shows it to be closer to the natural progesterone. It has anti-mineralocorticoid properties, counteracts the estrogen-stimulated activity of the renin-angiotensin-aldosterone system, and is not androgenic

question

Drospirenone side effects

answer

Several studies have shown that women who take contraceptive pills containing Drospirenone have a 6- to 7-risk of developing thromboembolism compared to women who do not take any contraceptive pill, and twice the risk of women who take a contraceptive pill containing Levonorgestrel.

question

Medroxyprogesterone acetate/ Depo-Provera I.M. class

answer

Depo-Provera contraceptive injection is the brand name for a 150 mg aqueous suspension of medroxyprogesterone acetate for intramuscular injection, either in the upper arm or upper outer gluteal area

question

Medroxyprogesterone acetate/ Depo-Provera I.M. indication

answer

A woman is protected from pregnancy immediately after receiving each injection Depo-Provera has been shown to reduce the risk of endometrial cancer by up to 80%. This reduced risk is thought to be due to both the direct anti-proliferative effect of a progestogen on the endometrium as well as the protective effects of reduction of estrogen levels by suppression of ovarian follicular development

question

Medroxyprogesterone acetate/ Depo-Provera I.M. MOA

answer

Depo-Provera and other high dose forms of progestin only contraceptives inhibit follicular development and prevent ovulation as their primary mechanism of action. High dose progestogens decrease the gonadotropin-releasing hormone (GnRH) release by the hypothalamus, which decreases the release of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) by the anterior pituitary

question

Medroxyprogesterone acetate/ Depo-Provera I.M. char.

answer

The shot is required 4 times a year to maintain the drug's high effectiveness

question

Medroxyprogesterone acetate/ Depo-Provera I.M. side effects

answer

Side effects include possible menstrual irregularities (bleeding or amenorrhea or alterations between the two), abdominal discomfort, weight changes, headache, hair loss, fatigue, depression and nervousness. Delayed return of fertility. The average return to fertility is 9 to 10 months after the last injection. Bone loss and increased risk for the development of osteoporosis is a major concern. In 2004, a black box warning was added to the package insert including the FDA recommendation that Depo-Provera not be used for longer than 2 years, unless there is no viable alternative method of contraception, due to concerns over bone loss.

question

Ortho Evra class

answer

transdermal contraceptive

question

Ortho Evra MOA

answer

The middle layer contains Norelgestromin and ethinyl estradiol. The inner layer is an adhesive and the outer is a protective cover.

question

Ortho Evra char.

answer

The first patch should be applied within the first 5 days of the menstrual cycle and a new patch should be applied every week for 3 weeks, followed by 1 patch-free week

question

Implanon class

answer

Implantable contraceptive

question

Implanon MOA

answer

Progestin implant

question

Implanon char.

answer

Implanon is placed sub-dermally, generally in the inner arm. The implant can be removed at any time, but it must be removed at the end of 3 years.

question

NuvaRing class

answer

NuvaRing is the trade name for a combined hormonal contraceptive ring made of flexible plastic that releases a low dose of a progestin and estrogen over three weeks

question

NuvaRing MOA

answer

combined hormonal contraceptive ring made of flexible plastic that releases a low dose of a progestin and estrogen over three weeks

question

NuvaRing char.

answer

The currently approved regimen specifies insertion of the ring into the vagina for a three-week period, then removal of the ring for one week, during which the user will experience a menstrual period.

question

NuvaRing side effects

answer

Contraceptive efficacy is reduced if the ring is removed, accidentally expelled, or left outside of the vagina for more than three hours. If left outside of the vagina for more than three hours, the device is to be rinsed and reinserted immediately. If this occurs, the manufacturer recommends that a backup method of contraception be used until the ring has been used continuously for a subsequent seven days The most commonly reported adverse events vaginitis, headache, leucorrhea nausea and weight gain Beyond the risks associated with combined oral contraceptives, NuvaRing is contraindicated for a risk of blood clots that is specific to 3rd generation class of contraceptives. NuvaRing contains the hormone etonogestrel, the active metabolite of the pro-drug desogestrel.

question

Paragard class

answer

copper intrauterine contraceptive

question

Paragard MOA

answer

Copper IUDs work by impairing the mobility of sperm. Additionally, the presence of a foreign body within the uterus irritates the endometrial lining and the subsequent inflammation makes it difficult for an embryo to implant.

question

Paragard char.

answer

Once in place, the Paragard IUD is approved for birth control for up to 10 years.

question

Mirena class

answer

IUD with Levonorgestrel

question

Mirena MOA

answer

The Mirena IUD utilizes a long-acting synthetic progestogen which is released into the uterine cavity to diminish the frequency of ovulation and changes the consistency of cervical mucus in addition to making implantation less likely by virtue of the inflammatory response to an indwelling foreign body.

question

Mirena char.

answer

Once in place, the Mirena IUD is approved for birth control for up to 5 year

question

The "morning after" pill class

answer

Emergency contraceptive pill

question

The "morning after" pill MOA

answer

The progestin-only method uses the progestin, Levonorgestrel, in a dose of 1.5 mg, either as two 750 μg doses 12 hours apart, or more recently as a single dose. Act both to prevent ovulation or fertilization and possibly post-fertilization implantation of a blastocyst

question

The "morning after" pill char.

answer

Progestin-only emergency contraceptive is available as a contraceptive product under many names worldwide, including: Plan B and Next Choice. The phrase "morning-after pill" is a bit of a misnomer; as emergency contraceptive pills are effective when used shortly before intercourse, and are licensed for use up to 72 hours after sexual intercourse. The WHO says they can be used for up to 5 days after unprotected intercourse

question

The "morning after" pill additional information

answer

The combined method uses large doses of both estrogen and progestin, taken as two doses at a 12-hour interval. This method is now believed to be less effective and less well-tolerated than the progestin-only method. It is possible to obtain the same dosage of hormones, and therefore the same effect, by taking several regular combined oral contraceptive pills. For example, 4 Ovral pills, 2 taken q 12 hrs x 2 doses.

question

Ulipristal acetate/Ella class

answer

Ulipristal acetate (trade name Ella) is a selective progesterone receptor modulator (SPRM) used for emergency contraception.

question

Ulipristal acetate/Ella indication

answer

It has shown to prevent about 60% of expected pregnancies, which is comparable to the emergency contraception with plan B/ Levonorgestrel.

question

Ulipristal acetate/Ella MOA

answer

It prevents pregnancy by delaying or inhibiting ovulation and inhibiting follicle rupture.

question

Ulipristal acetate/Ella char.

answer

It is to be given within 120 hours (5 days) after unprotected intercourse or contraceptive failure.

question

Mifepristone/Mifeprex class

answer

synthetic steroid compound

question

Mifepristone/Mifeprex indication

answer

Mifepristone is a synthetic steroid compound used as an abortifacient in the first two months of pregnancy, and in smaller doses as an emergency contraceptive.

question

Mifepristone/Mifeprex MOA

answer

Mifepristone acts a progestin antagonist with partial agonist activity. MOA is blockade of progesterone receptors (which when stimulated, normally sustain the endometrium) as well as causing a decline in human chorionic gonadotropin levels which in turn causes decreased production of progesterone by the corpus luteum.

question

Mifepristone/Mifeprex char.

answer

Administration of Mifepristone during the 1st trimester of pregnancy results in abortion in ~85% of cases. Mifepristone is often used in conjunction with Misoprostol (Cytotec), a prostaglandin E1 analog.

question

Mifepristone/Mifeprex side effects

answer

In clinical trials, nearly all women using Mifepristone experienced abdominal pain, uterine cramping, and vaginal bleeding or spotting for an average of 9-16 days. Up to 8% of women experienced some type of bleeding for 30 days or more. Other less common side effects included nausea, vomiting, diarrhea, dizziness, fatigue, and fever. Excessive uterine bleeding or incomplete termination of a pregnancy require emergent medical intervention. Mifepristone use is contraindicated in the presence of an intrauterine device (IUD), in cases of ectopic pregnancy, in patients with known hemorrhagic disorders or on anticoagulant therapy and patients on long term prednisone therapy

question

Clomiphene/Clomid class

answer

Estrogen receptor agonist

question

Clomiphene/Clomid indication

answer

Infertility, amenorrhea

question

Clomiphene/Clomid MOA

answer

Binding to estrogen receptor sites in the brain interferes with the normal negative feedback of estrogen on gonadotropin releasing hormone (GnRH), which results in the increased secretion of GnRH. This causes an increased release of LH and FSH and stimulation of ovulation.

question

Clomiphene/Clomid char.

answer

PO. Careful administration with assessment for potential side effects.

question

Clomiphene/Clomid side effects

answer

vaginal dryness, vaginal bleeding, breast tenderness, anxiety, hot flashes. Potentially contraindicated if prior history of liver disease, breast cancer or uterine cancer. Multiple births is a known potential risk when using this drug.

question

Testosterone class

answer

Androgenic hormone

question

Testosterone indication

answer

Testosterone replacement for both androgenic and/or anabolic effects Exogenous administration of testosterone is used in males with inadequate testosterone production (hypogonadism). Testosterone is also used in conjunction with other hormones to promote skeletal growth in prepubertal boys with pituitary dwarfism. Post-pubertal hypogonadism is manifested primarily by infertility, abnormalities of sexual function (erectile dysfunction and decreased libido), alterations in behavior (irritability, depression), loss of muscle mass and tone, increased rate of osteoporosis and possible loss of secondary sexual characteristics (decrease in axillary and pubic hair). Bone marrow stimulation and anemia Severe osteoporosis Hormone therapy for transsexual men Unapproved use - androgenic steroids are used to increase lean body mass, muscle strength and aggressiveness in athletes and body builders. "Anti-aging"

question

Testosterone MOA

answer

Alters gene transcription

question

Testosterone char.

answer

IM (as testosterone cypionate), patch, gel, SL lozenges. Not used in oral form because of inactivation by first-pass metabolism. Dosed daily for patches or gel or one dose every 1-2 weeks for injection

question

Testosterone side effects

answer

In males, excess androgens can cause acne, baldness, gynecomastia, priapism, increased risk of prostatic hyperplasia and prostatic cancer*, exacerbation of sleep apnea and result in reduced sperm count and infertility (due to negative feedback). In females, excess androgens can result in virilization such as excess body and facial hair, acne, deepening of voice, clitoral enlargement and menstrual irregularities In children, excess androgens can cause abnormal rate of sexual maturation and can result in diminished height due to premature closing of growth plates. The unauthorized use high dose anabolic steroids by athletes has been documented to result in different liver abnormalities, gynecomastia and breast cysts, cystic acne, premature epiphyseal plate closure and increased aggression ("roid rage") Additional adverse effects include abnormal lipid levels. Androgens increase serum LDL and lower serum HDL, therefore increasing the risk of atherosclerosis and coronary artery disease. Androgens can also cause fluid retention and edema. Increased red blood cell mass may cause increased blood viscosity and sludging of blood and increase the risk for ischemia.

question

Leuprolide/Lupron class

answer

Anti-androgenic hormone and anti-estrogenic hormone.

question

Leuprolide/Lupron indication

answer

Prostatic cancer, precocious puberty, endometriosis and uterine fibroids, as well as being part of some protocols of I.V.F.

question

Leuprolide/Lupron MOA

answer

Synthetic analog of gonadotropin releasing hormone (GnRH). Leuprolide interrupts production of both testosterone and estrogen.

question

Leuprolide/Lupron char.

answer

SQ, IM. Different preparations have different half lives.

question

Leuprolide/Lupron side effects

answer

Decreased libido, impotence nausea, vomiting, hot flashes, night sweats, arthralgias, myalgias, osteoporosis.

question

Finasteride/Proscar class

answer

Anti-androgen

question

Finasteride/Proscar indication

answer

Benign prostatic hyperplasia. In lower doses it is used to treat male-pattern baldness. In higher doses it is used to treat prostate cancer.

question

Finasteride/Proscar MOA

answer

Limits conversion of testosterone to dihydrotestosterone (DHT) by inhibiting type II 5-alpha reductase

question

Finasteride/Proscar char.

answer

P.O. Once daily dosing. Intended for use by men only. No blood donation is allowed while a patient is taking Proscar. Side effects: Women who are or may potentially be pregnant must not use Proscar and should be instructed not to handle crushed or broken tablets because of the risk of birth defects.

question

Finasteride/Proscar side effects

answer

Decreased libido, erectile dysfunction, impotency, depression, breast swelling and breast tenderness

question

Alpha blockers used for BPH include...

answer

Doxazosin (Cardura), Terazosin (Hytrin), Tamsulosin (Flomax and Urimax), and Silodosin (Urief) All five are equally effective but have slightly different side effect profiles

question

Alpha blocker side effects

answer

Common side effects of alpha blockers include weakness, orthostatic hypotension and nasal congestion.

question

Phosphodiesterase type 5 inhibitors MOA

answer

Phosphodiesterase type 5 inhibitors block the degradative action of the enzyme, phosphodiesterase type 5 on cyclic GMP in the smooth muscle cells lining the blood vessels supplying the corpus cavernosum of the penis. This causes blood to remain in the corpus cavernosum and thereby an erection is maintained.

question

Phosphodiesterase type 5 inhibitors indication

answer

Because PDE5 is also present in the arterial wall smooth muscle within the lungs, PDE5 inhibitors such as Sildenafil have also been utilized for the treatment of pulmonary hypertension, a disease in which blood vessels in the lungs become abnormally narrow.

question

Sildenafil citrate/Viagra class

answer

PDE5 inhibitor

question

Sildenafil citrate/Viagra indication

answer

E.D., pulmonary hypertension

question

Sildenafil citrate/Viagra MOA

answer

Sildenafil is a potent and selective inhibitor of cGMP specific phosphodiesterase type 5 (PDE5), which is responsible for the degradation of cGMP stores in the corpus cavernosum. When this occurs in the smooth muscle cells lining the blood vessels supplying the corpus cavernosum of the penis, blood remains in the cavernosum and thereby an erection is maintained. Sildenafil does not generally cause an erection without sexual stimulation because there is lack of activation of the nitric oxide/cGMP system.

question

Sildenafil citrate/Viagra char.

answer

Sildenafil is available in 25 mg, 50 mg and 100 mg tablets. The dose of Sildenafil for erectile dysfunction is 25 mg to 100 mg, to be taken between 30 minutes and 4 hours prior to sexual intercourse. Patients are instructed to take no more than one tablet per day.

question

Sildenafil citrate/Viagra side effects

answer

The most common adverse effects of Sildenafil include headache, flushing, dyspepsia and nasal congestion. Impaired vision, including photophobia and blurred vision, is also commonly reported. Some Sildenafil users have complained of seeing everything in the visual field as being tinted blue (cyanopsia). Rare but serious adverse effects include increased intraocular pressure and acute angle closure glaucoma, ventricular arrhythmias, severe hypotension, myocardial infarction and stroke, as well as priapism.

question

Sildenafil citrate/Viagra contraindications

answer

Not to be used by patients on nitric oxide donors, organic nitrites and nitrates, such as nitroglycerin and Isosorbide dinitrate. In men for whom sexual intercourse is inadvisable due to cardiovascular risk factors such as recent stroke or heart attack Severe impairment of liver or renal function Hypotension Hereditary degenerative retinal disorders

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