Test 3 Flashcards
1
Q
class of Levothyroxine/ Synthroid
A
Thyroid hormone replacement (synthetic T4) dosed in mcg.
2
Q
ind. of Levothyroxine/ Synthroid
A
Hypothyroidism. Also TSH suppression in select cases of thyroid nodules and thyroid cancer.
3
Q
MOA of Levothyroxine/ Synthroid
A
Replaces normal levels of T4 and T3 (T4 is converted into T3 in the periphery.)
4
Q
side effects of Levothyroxine/ Synthroid
A
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.
5
Q
drug where long term elevation of serum T4 may accelerate cardiac disease and osteoporosis.
A
Levothyroxine/ Synthroid
6
Q
Normal ratio of T4:T3
A
4:1
7
Q
thyroid med always dosed in micrograms (mcg)
A
Levothyroxine/ Synthroid
8
Q
In patients that have Addison’s disease and hypothyroidism, what treatment can lead to death.
A
Thyroid replacement without first replacing cortisol can be fatal.
9
Q
class of Thyroid USP/ Armour
A
Thyroid hormone (T4 and T3 as well as T2 and T1) obtained from desiccated animal thyroid gland
10
Q
ind. of Thyroid USP/ Armour
A
hypothyroidism
11
Q
MOA of Thyroid USP/ Armour
A
Replaces both T4 and T3
12
Q
side effects of Thyroid USP/ Armour
A
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.
13
Q
60 mg dose of Thyroid USP/ Armour is equal to how many grains
A
1 grain
14
Q
60 mg dose of Thyroid USP/ Armour is equal to how many mcg of Synthroid
A
100 mcg Synthroid
15
Q
drug that is standardized to iodine content
A
Thyroid USP/ Armour
16
Q
class of Liothyronine/ Cytomel
A
Thyroid hormone replacement (synthetic T3) dosed in mcg.
17
Q
ind. of Liothyronine/ Cytomel
A
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”.
18
Q
MOA of Liothyronine/ Cytomel
A
Replaces T3
19
Q
side effects of Liothyronine/ Cytomel
A
Similar to T4. Higher peaks and troughs of T3 may increase risk of coronary artery disease and osteoporosis.
20
Q
60 mg Thyroid USP (Armour) ~ = how many mcg of T3
A
25 mcg of T3 (Cytomel)
21
Q
25 mcg of T3 (Cytomel) is equal to how many mcg of T4 (Synthroid)
A
100 mcg of T4 (Synthroid)
22
Q
class of Methimazole/ Tapazole
A
Thionamide
23
Q
ind. of Methimazole/ Tapazole
A
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.
24
Q
MOA of Methimazole/ Tapazole
A
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
25
side effects of Methimazole/ Tapazole
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.
26
Most feared side effects of Methimazole/ Tapazole
agranulocytosis
27
drug with minimal effect of blocking the peripheral conversion of T4 to T3
Methimazole/ Tapazole
28
class of Propylthiouracil (PTU)
thionamide
29
ind. of Propylthiouracil (PTU)
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.
30
MOA of Propylthiouracil (PTU)
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.
31
side effects of Propylthiouracil (PTU)
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.
32
drug with notable effect of blocking the peripheral conversion of T4 to T3.
Propylthiouracil (PTU)
33
class of Propranolol/ Inderal
Non selective beta blocker
34
ind. of Propranolol/ Inderal
Blockade of adrenergic symptoms of hyperthyroidism (i.e. tachycardia, anxiety). Emergent treatment of thyroid storm.
35
MOA of Propranolol/ Inderal
Beta-1 and Beta-2 receptor blockade
36
side effects of Propranolol/ Inderal
Fatigue, sedation, impotency or depression may be noted.
37
class of Iodine/ S.S.K.I.
elemental iodine
38
ind. of Iodine/ S.S.K.I.
hyperthyroidism, thyroid storm
39
MOA of Iodine/ S.S.K.I.
large doses of iodine inhibit the release of thyroxine from the thyroid gland.
40
side effects of Iodine/ S.S.K.I.
Rash, fever. Beneficial effects generally last no more then 2-3 weeks as thyroid gland appears to adapt and resumes secretion of thyroxine.
41
class of Radioactive iodine (131I)
Radioactive isotope
42
ind. of Radioactive iodine (131I)
Thyroid gland ablation in cases of Grave’s disease, thyroid nodules and in some cases of thyroid cancer.
43
MOA of Radioactive iodine (131I)
Radioactive emission of beta particles results in destruction of thyroid tissue.
44
side effects of Radioactive iodine (131I)
As previously noted. 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.
45
Radioiodine should never be used in a patient who is
Radioiodine should never be used in a patient who is pregnant. 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.
Category X
46
signs of a thyroid storm
high fever, irritability, delirium, vomiting, diarrhea, dehydration, hypotension and vascular collapse
Coma and death may occur.
47
Treatment for thyroid storm
beta blockade as well as I.V. iodine to “stun” the thyroid gland’s ability to utilize iodine to synthesize thyroid hormone
48
level of fasting blood glucose to be DM
>126
49
class of Metformin
biguanides
50
MOA of Metformin
decreases hepatic glucose production and to a lesser extent, enhances insulin sensitivity in skeletal muscles
51
drug that may cause weight loss
Metformin
52
common side effects of Metformin (know this)
Most common are abdominal cramping and nausea. Others include metallic taste and increased risk for development of B12 deficiency.
53
Most serious side effect of Metformin
lactic acidosis which is rare but can prove fatal. Risk is diminished by not using drug in patients with impaired renal function.
54
MOA of sulfonylureas
stimulate intact beta cells of the pancreas to release more insulin
55
1st generation Sulfonylureas
Chlorpropamide (Diabinese) and Tolbutamide (Orinase)
56
2nd generation Sulfonylureas
Glipizide (Glucotrol), Glyburide (Micronase, Diabeta), Glimerpiride (Amaryl)
57
most common adverse effects of sulfonylurea
hypoglycemia, particularly in patients with impaired renal or hepatic function. Weight gain as well.
58
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
59
sulfonylurea drug that appears to have a greater incidence of hypoglycemic events
Glyburide (Micronase)
60
MOA of Meglitinides
stimulate the beta cells to release insulin
61
Meglitinide drugs
Nateglinide (Starlix) and Repaglinide (Prandin).
62
side effects of Meglitinides
hypoglycemia and weight gain similar to Sulfonylureas
63
MOA of Thiazolidinediones/ Glitazones
The TZDs aka Glitazones improve insulin sensitivity in skeletal muscle cells, fat cells and liver cells and also decreases hepatic glucose production.
64
drug associated with CHF side effect
The cardiovascular safety of the TZDs particularly Avandia, is controversial.
Both Avandia and Actos increase the risk of congestive heart failure.
65
what tests should be performed with use of Glitazones
LFTs
66
Side effects of glitazones
reduced bone density, weight gain
67
Alpha-glucosidase inhibitors
Two alpha glucosidase inhibitors are available in the US, Acarbose (Precose) and Miglitol (Glyset).
68
What drugs classes do not cause blood glucose levels to fall below 60
Ubiquinides and alpha glucosidase inhibitors
69
MOA of Alpha-glucosidase inhibitors
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.
70
side effects of Alpha-glucosidase inhibitors
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.
71
In the event of hypoglycemia, oral treatment of patients taking Alpha-glucosidase inhibitor drugs must be
dosed with glucose rather than sucrose because alpha-glucosidase inhibitors interfere with the breakdown of sucrose
72
MOA of Sitagliptin/ Januvia
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.
73
Key side effect of Sitagliptin/ Januvia
pancretitis
74
Two relatively new injectable drugs have recently been approved by the FDA for the treatment of type 1 and type 2 diabetes
Pramlintide/Symlin and Exenatide
75
Drug that is a synthetic form of the hormone amylin, which is produced along with insulin by the beta cells.
Pramlintide/Symlin
76
Drug that is a synthetic version of exendin-4, a naturally occurring hormone that was first isolated from the saliva of the Gila monster.
Exenatide
77
MOA of Pramlintide/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.
78
class of Exenatide/ Byetta
incretin mimetics
79
MOA of Exenatide/ Byetta
acts to lower blood glucose levels primarily by increasing insulin secretion
80
Way that insulin cannot be taken
PO
81
Rapid acting insulin onset and duration
```
Rapid acting insulins:
Humolog/ Lispro, Novolog/ Aspart
Onset: ≤0.25h
Peak: 0.5-1.5h
Duration 3-5h
```
82
short acting insulin onset and duration
```
Short acting insulins:
Regular/ Humulin R
Onset: 0.5-1h
Peak: 2-4h
Duration: 5-8h
```
83
intermediate acting insulin onset and duration
```
Intermediate acting insulin:
NPH/ Humulin N:
Onset: 1-3h
Peak: 7-9h
Duration: 12-18h
```
84
long acting insulin onset and duration
```
Long acting insulins
Glargine / Lantus
Onset: 1h
Peak: “flat”
Duration: 18-24h
```
85
Rapid acting insulin
Lispro/Aspart (Humulog/Novalog)
86
Short acting insulin
Regular (Humulin R)
87
Intermediate acting insulin
NPH (Humulin N)
88
Long acting insulin
Glargine (Lantus)
89
Common side effect and most feared side effect
Weight gain is common. Hypoglycemia is most feared.
| Hypokalemia can also occur.
90
Treatment for severe hypoglycemia
Glucagon is a potent hyperglycemic agent that is indicated for the treatment of severe hypoglycemia.
Glucose is always given first though.
91
what is required for survival of all type 1 diabetics
insulin replacement
92
while there is no consensus, studies show that this type of calcium may be best absorbed
calcium citrate
93
what type of calcium has lead in it?
calcium obtained from oyster shell source
94
recommended daily calcium for people less than 50
1000 mg/day
95
recommended daily calcium for people over 50
1200-1500 mg/day
96
recommended daily calcium for breast feeding women
2000 mg/day
97
vit D recommendation for people age 1-70
600 IU (15 mcg)
98
vit D recommendation for people age 70+
800 IU (20 mcg)
99
prescription form of vit D
Calcitriol (Rocaltrol)
100
average daily dose of magnesium
300-1000 mg
101
dose of strontium to prevent osteoporosis
500 mg to 1 gram daily
102
dose of strontium to treat osteoporosis
2 grams/day
103
what happens if you take >2 grams/day strontium
may actually weaken bone by replacing too much calcium with strontium
104
drug approved by FDA for both prevention and treatment of postmenopausal osteoporosis
Bisphosphonates such as Alendronate
105
drug approved for prevention and treatment of osteoporosis
Raloxifene (Evista) is a selective estrogen receptor modulator which has been approved for both the prevention and treatment of osteoporosis.
106
drug approved for treatment of osteoporosis but not for prevention
Calcitonin (Mialcin) has been approved for the treatment of osteoporosis but is not yet approved for osteoporosis prevention.
107
Drug approved for the treatment of the disease in postmenopausal women and in men who are at high risk for fracture
Teriparatide, a synthetic PTH analogue is approved for the treatment of the disease in postmenopausal women and in men who are at high risk for fracture.
108
Drug approved for prevention of postmenopausal osteoporosis
Estrogen/hormone replacement therapy (ET/HRT)
109
What is Denosumab?
Denosumab is a human monoclonal antibody that was approved by the FDA at the end of 2010 for the treatment of osteoporosis.
110
requirement for people taking bisphosphonates
they have to be able to stand for a period of time
111
class of Alendronate/ Fosamax
Bisphosphonates
112
ind. of Alendronate/ Fosamax
Prevention and treatment of osteoporosis
113
MOA of Alendronate/ Fosamax
Inhibition of osteoclast activity
114
side effects of Alendronate/ Fosamax
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.
115
key side effects of Alendronate/ Fosamax
Esophagitis. Osteonecrosis of the jaw. Atypical femur fractures.
116
class of Raloxifene/ Evista
SERM (selective estrogen-receptor modulators)
117
ind. of Raloxifene/ Evista
Increases bone mass and reduces the risk of vertebral fracture. Raloxifene has been shown to significantly reduce the incidence of breast cancer.
118
MOA of Raloxifene/ Evista
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
119
side effects of Raloxifene/ Evista
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
120
class of Calcitonin/ Miacalcin
Synthetic hormone to ↑serum Ca2
121
ind. of Calcitonin/ Miacalcin
treatment of osteoporosis
122
MOA of Calcitonin/ Miacalcin
Inhibits osteoclastic activity
123
side effects of Calcitonin/ Miacalcin
Nose bleeds and sinusitis noted with nasal spray. Both nasal spray and IV routes may cause headache, dizziness, edema, anorexia, diarrhea and skin rashes.
124
drug for osteoporosis that is available in a nasal spray
Calcitonin/ Miacalcin
125
class of Teriparatide/ Forteo
Synthetic PTH analogue that has been altered to have opposite effect of native PTH model.
126
ind. of Teriparatide/ Forteo
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.
127
MOA of Teriparatide/ Forteo
Activates bone turnover with osteoblasts being activated to a much greater extant than osteoclasts. Stimulates new bone formation in both spine and hip.
128
side effects of Teriparatide/ Forteo
The most commonly reported side effects are nausea, leg cramps and dizziness.
129
what is given alongside Estrogen/HRT in order to potentially eliminate the increased risk for development of endometrial cancer
progestin
130
MOA of Denosumab/ Prolia
Denosumab targets RANKL (the RANK ligand), a protein that acts as the primary signal to promote bone removal.
131
drug class that randomly may lower risk of hip and other fractures
statin drugs
132
most potent form of endogenous estrogen in women
estradiol...other major estrogen have 1/10 the potency
133
if given orally, what limitation do naturally occurring estrogens have
first pass clearance by liver
134
risks of exogenous hormone replacement
increased risk of stroke, blood clots, ovarian cancer, endometrial cancer, and breast cacner
135
what is premarin?
conjugated estrogen...from urine of pregnant mares
136
ind. of premarin
Prevention and treatment of osteoporosis and of post-menopausal symptoms such as hot flashes, vaginal dryness and itching.
137
MOA Conjugated estrogens/ Premarin
alters gene transcription
138
side effects of Conjugated estrogens/ Premarin
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.
139
Premarin contraindications
Pregnancy, prior history of DVT, breast/ovarian/uterine cancer
140
two most common uses of progestins
prevent endometrial hyperplasia and for hormonal contraception
141
class of Medroxyprogesterone/Provera
Medroxyprogesterone acetate is a synthetic variant of progesterone.
142
ind. of Medroxyprogesterone/Provera
Contraceptive, hormone replacement therapy, dysfunctional uterine bleeding and treatment of endometriosis.
143
MOA of Medroxyprogesterone/Provera
Alters gene transcription.
144
side effects of Medroxyprogesterone/Provera
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.
145
side effects of oral contraceptives
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.
146
The use of oral contraceptives for five years or more appears to decreases the risk of
ovarian cancer in later life by 50%
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.
147
Combined oral contraceptive use 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.
148
Several studies have shown that women who take contraceptive pills containing this drug 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.
Drospirenone
149
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.
150
side effects of Medroxyprogesterone acetate/ Depo-Provera I.M.
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.
Depo-Provera has been shown to increase bone loss and increase the risk for the development of osteoporosis.
151
why does Medroxyprogesterone acetate/ Depo-Provera I.M. have a black box warning
Due to concerns over bone loss, a black box warning was added to the package insert for Depo-Provera in 2004 stating the FDA recommendation that the drug not be used for longer than 2 years, unless there is no viable alternative method of contraception.
152
MOA of Medroxyprogesterone acetate/ Depo-Provera I.M.
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.
153
progestin implant
Implanon
154
transdermal patch for contraception
Ortho Evra
155
the transdermal patch contains higher levels of
estrogen compared to most oral hormonal pills
156
what reduces the efficacy of NuvaRing
accidentally expelled of left outside vagina for more than three hours
157
most commonly reported adverse events with NuvaRing
vaginitis, headache, leucorrhea, nausea, weight gain
158
Beyond the risks associated with combined oral contraceptives, NuvaRing is contraindicated for a risk of ____ that is specific to 3rd generation class of contraceptives.
blood clots
159
IUD containing copper
ParaGard
160
Three hormone containing IUDs
Mirena, Liletta, Skyla...each contains progestin and levonorgestrel in differing concentrations
161
The non-copper IUD utilize what
long-acting synthetic progestin, levonorgestrel
162
Mirena and Liletta have how much levonorgestral at initial placement and are marketed for having release rates of?
52 mg levonorgestral and release rate of 20 mcg/day
163
Skyla has how much levonorgestral at initial placement and is marketed for having release rates of?
13.5 mg levonorgestral and release rate of 14 mcg/day
164
class of Ulipristal acetate/Ella
Selective Progesterone Receptor Modulator (SPRM)
165
what does Ulipristal acetate/Ella do and when is it given
Ulipristal acetate prevents pregnancy by delaying or inhibiting ovulation and inhibiting follicle rupture.
It is to be given within 120 hrs (5 days) after unprotected intercourse or contraceptive failure.
166
Progestin-only emergency contraceptive is available as a contraceptive product under many names worldwide, including
Plan B and Next Choice...more effective than combo drugs
167
what is Mifepristone/ Mifeprex
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.
168
MOA of Mifepristone/ Mifeprex
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.
169
Risk with Mifepristone/ Mifeprex
Administration of Mifepristone during the 1st trimester of pregnancy results in abortion in ~85% of cases.
170
Mifepristone is often used in conjunction with
Misoprostol (Cytotec), a prostaglandin E1 analog.
171
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.
172
A characteristic that distinguishes selective estrogen receptor modulators from pure receptor agonists and antagonists is that
their action is different in various tissues, thereby granting the possibility of selectively inhibiting or stimulating estrogen-like action in various tissues.
173
class of Clomiphene/ Clomid
Selective estrogen receptor modulator
174
ind. of Clomiphene/ Clomid
infertility, amenorrhea
175
MOA of Clomiphene/ Clomid
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.
176
side effects of Clomiphene/ Clomid
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.
177
The mechanism of action of testosterone and all biologic and synthetic analogues of testosterone is
the alteration of gene transcription.
178
interesting thing testosterone increases
RBC production
179
ratio of androgenic to anabolic activity in exogenous testosterone preparations
1:1
180
Older testosterone preparations which were formulated to be taken orally were found to increase the risk of
liver disease such as hepatitis and hepatic carcinoma.
181
adverse effects of androgens in males
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).
182
adverse effects of androgens in females
In females, excess androgens can result in virilization such as excess body and facial hair, acne, deepening of voice, clitoral enlargement and menstrual irregularities.
183
adverse effects of androgens in children
In children, excess androgens can cause abnormal rate of sexual maturation and can result in diminished height due to premature closing of growth plates.
184
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”).
185
Effect of androgens on cholesterol
Androgens increase serum LDL and lower serum HDL, therefore increasing the risk of atherosclerosis and coronary artery disease.
They are cause fluid retention and edema
186
class of Testosterone
androgenic hormone
187
ind. of Testosterone
Testosterone replacement for both androgenic and/or anabolic effects. See prior slides
188
MOA of Testosterone
alters gene transcription
189
The approved use of anabolic steroids include
refractory anemia, severe osteoporosis and severe wasting conditions such as AIDS and cancer.
190
Anti-androgen treatment is most often utilized for the treatment of
advanced prostatic cancer.
191
class of Leuprolide/ Lupron
Anti-androgenic hormone and anti-estrogenic hormone.
192
ind. of
| Leuprolide/ Lupron
Prostatic cancer, precocious puberty, endometriosis and uterine fibroids, as well as being part of some protocols of I.V.F.
193
MOA of Leuprolide/ Lupron
Synthetic analog of gonadotropin releasing hormone (GnRH). Leuprolide interrupts production of both testosterone and estrogen.
194
side effects of
| Leuprolide/ Lupron
Decreased libido, impotence nausea, vomiting, hot flashes, night sweats, arthralgias, myalgias, osteoporosis.
195
class of Finasteride/ Proscar
Anti-androgen
196
ind. of Finasteride/ Proscar
Benign prostatic hyperplasia. In lower doses it is used to treat male-pattern baldness. In higher doses it is used to treat prostate cancer.
197
MOA of Finasteride/ Proscar
Limits conversion of testosterone to dihydrotestosterone (DHT) by inhibiting type II 5-alpha reductase.
198
side effects of Finasteride/ Proscar
Decreased libido, erectile dysfunction, impotency, depression, breast swelling and breast tenderness.
No blood donation is allowed while a patient is taking Proscar.
199
drug where women who are or may potentially be pregnant must not use and should be instructed not to handle crushed or broken tablets because of the risk of birth defects.
Finasteride/ Proscar
200
The two main medications for management of BPH are
5α-reductase inhibitors and the alpha blockers.
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Example of an alpha blocker
Tamsulosin (Flomax and Urimax)
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Common side effects of alpha blockers include
weakness, orthostatic HYPOTENSION and nasal congestion.
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class of Sildenafil citrate/ Viagra
PDE5 inhibitor
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ind. of Sildenafil citrate/ Viagra
ED, pulmonary hypertension
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MOA of Sildenafil citrate/ Viagra
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.
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Drug used for pulmonary hypertension
Sildenafil citrate/ Viagra
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when to take Sildenafil citrate/ Viagra
taken between 30 minutes and 4 hours prior to sexual intercourse.
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Contraindications to Sildenafil citrate/ Viagra
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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adverse effects of Sildenafil citrate/ Viagra
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).
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Rare but serious adverse effects of Sildenafil citrate/ Viagra
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.
