Pharm II - Test 3 Flashcards
Class: Levothyroxine (Synthroid)
Thyroid hormone replacement (synthetic T4)
Indication: Levothyroxine (Synthroid)
Hypothyroidism, TSH suppression in select cases of thyroid nodules and thyroid cancer
Side effects: Levothyroxine (Synthroid) and Thyroid USP (Armour) and Liothyronine (Cytomel)
Palpitations, tachycardia, intolerance to heat, anxiety
Long-term elevation of serum T4 may accelerate cardiac disease and osteoporosis
What is an important contraindication for patients with Addison’s disease and hypothyroidism take Synthroid or Armour thyroid?
Replacing thyroid hormone before replacing cortisol can be fatal.
Equivalent dosing: Armour vs. Synthroid vs. Cytomel
60 mg (1 grain) Armour = 100 mcg of T4 (Levothyroixine/Synthroid) = 25 mcg of T3 (Triiodothyronine/Cytomel)
Indication: Thyroid USP (Armour)
Hypothyroidism
MOA: Thyroid USP (Armour)
Replaces both T4 and T3
Thyroid USP (Armour) is standardized to ___
iodine content (0.2% iodine)
With what population should you use more cautious dosing of thyroid replacement?
Patients over 65 with a history of cardiac disease
Class: Liothyronine (Cytomel)
Thyroid hormone replacement (synthetic T3) dosed in mcg
Indication: Liothyronine (Cytomel)
Hypothyroidism with intolerance to T4 replacement therapy or no improvement on T4 replacement therapy
Myxedema coma
“Wilson’s syndrome”
Condition caused by excess administration of thyroid hormone
Thyroiditis factitia
Thyroid conditions can place patients at greater risk for ___(2).
Osteoporosis
Cardiac disease
What type of drugs are often used to block the signs and symptoms of hyperthyroidism?
Beta blockers
Class: Methimazole (Tapazole)
Thionamide
Indication: Methimazole (Tapazole)
Hyperthyroidism
MOA: Methimazole (Tapazole)
Inhibits transformation of inorganic iodine to organic iodine -> blocks production of thyroxine
Inhibits coupling of iodotyrosine to form T3/T4
Minimal effect blocking peripheral conversion of T4 to T3
Contraindications: Methimazole (Tapazole), Propylthiouracil (PTU)
Pregnancy - Propylthiouracil (PTU) is considered safer (category D)
Class: Propylthiouracil (PTU)
Thionamide
Indication: Propylthiouracil (PTU)
Hyperthyroidism
MOA: Propylthiouracil (PTU)
Inhibits transformation of inorganic iodine to organic iodine -> blocks production of thyroxine
Inhibits coupling of iodotyrosine to form T3/T4
Blocks peripheral conversion of T4 to T3
MOA: Methimazole (Tapazole) vs Propylthiouracil (PTU)
Propylthiouracil (PTU) has a greater effect on blocking peripheral conversion of T4 to T3
Indication: Iodine (SSKI)
Hyperthyroidism, thyroid storm
MOA: Iodine (SSKI)
Large doses of iodine inhibit release of thyroxine from thyroid gland
Beneficial effects of Iodine (SSKI) generally last no more than ___.
2-3 weeks
Indication: Radioactive iodine (131I)
Hyperthyroidism, Selected cases of thyroid cancer, thyroid nodules
Side effects: Radioactive iodine (131I)
Tenderness, swelling during initial week, N/V
transient BM depression and acute leukemia w/ extremely high doses
M - dec sperm, temp. infertility (~2 years)
Preparation for treatment with Radioactive iodine (131I)
Euthyroid state achieved by anti-thyroid drugs or SSKI
Contraindications: Radioactive iodine (131I)
Category X (delay 6-12 mos after tx)
SSx: Thyroid storm
High fever, irritability, delirium, V/D, dehydration, hypotension, vascular collapse
Coma, death
Which population is at risk for thyroid storm unless anti-thyroid medication has been administered?
Patients undergoing surgery for hyperthyroidism
Tx: Thyroid storm
Beta blockade + IV Iodine
Dx: DM
Confirmed fasting blood glucose level of >/= 126 mg/dl
Non-fasting blood glucose of >/= 200 mg/dl in pt presenting w/ sxs or exam findings consistent with DM
Concordance for development in identical twins: Type I vs II diabetes
Type I: 50%
Type II: 90-100%
What antibody testing should be considered in all non-obese adults who present with sxs of type II diabetes (type 1.5)?
Islet cell, insulin, and glutamic acid decarboxylase antibodies
MOA: Metformin vs. Sulfonylureas/Meglitinides vs. Alpha-glucosidase inhibitors vs. Thiazolidinediones (Glitazones) vs. DPP-4 inhibitors
Metformin = inhibits hepatogluconeogenesis, dec insulin resistance
Sulfonylureas/Meglitinides = inc secretion of insulin (secretagogues)
Alpha-glucosidase inhibitors = delay absorption of glucose by intestines
Thiazolidinediones (Glitazones) = dec insulin resistance (via PPAR-gamma)
DPP-4 inhibitors = promote release of insulin from pancreas after eating a meal (via GLP-1)
Class: Metformin (Glucophage)
Biguanides
MOA: Metformin (Glucophage)
Dec hepatic glucose production, inc insulin sensitivity in skeletal muscle
Pregnancy and Metformin (Glucophage)
Category B
Side effects: Metformin (Glucophage)
Abdominal cramping, N, metallic taste, inc risk for B12 deficiency
Lactic acidosis (rare)
Contraindications: Metformin (Glucophage)
Do not use in pts w/ impaired renal fxn (serum creatinine >1.5 mg/dl in M or >1.4 in F)
MOA: Sulfonylureas
Interaction w/ ATP-sensitive K channel in the beta cell membrane -> inc. insulin production from intact beta cells (secretagogues)
What is the MC side effect of sulfonylureas?
Weight gain
In general, sulfonylureas become ineffective within ___.
5-10 years
Contraindications: Sulfonylureas
Patients w/ sulfa allergy
2nd-generation sulfonylureas (3)
Glipizide (Glucotrol)
Glyburide (Micronase, Diabeta)
Glimepiride (Amaryl)
MOA: Meglitinides
Interaction w/ ATP-sensitive K channel in the beta cell membrane -> Inc. insulin release from beta cells (secretagogues)
Meglitinides (2)
Nateglinide (Starlix)
Repaglinide (Prandin)
Which meglitinide has been shown to be equally effective to the sulfonylureas?
Repaglinide (Prandin)
Side effects: Sulfonylureas, Meglitinides
Hypoglycemia, weight gain
Contraindication: Meglitinides
Do not combine with sulfonylurea drugs due to increased risk for hypoglycemia
MOA: Thiazolidinediones / Glitazone
Affect gene expression of PPAR gamma -> dec. peripheral insulin resistance, dec. hepatic glucose production
What is the only glitazone approved for concurrent use with insulin?
Pioglitazone (ACTOS)
TZDs/Glitazones (2)
Rosiglitazone (Avandia)
Pioglitazone (ACTOS)
Side effects: TZDs/Glitazones
Increased risk of CHF, MI(?), bone fractures, weight gain, ALT elevation
Alpha-glucosidase inhibitors (2)
Acarbose (Precose)
Miglitol (Glyset)
MOA: Alpha-glucosidase inhibitors
Inhibit alpha-glucosidase -> delays absorption of glucose and other monosaccharides
Alpha-glucosidase inhibitors can increase the risk for hypoglycemia when combined with ___.
Sulfonylureas
Contraindications: Alpha-glucosidase inhibitors
Pts w/ chronic intestinal dz, IBD, colonic ulceration, intestinal obstruction
Pregnancy: Alpha-glucosidase inhibitors
Category B
MOA: Sitagliptin (Januvia)
Dipeptidyl peptidase 4 (DPP-4) inhibitor -> prevent breakdown of GLP-1 and GIP -> potentiate secretion of insulin, suppress glucagon release -> normalize blood glucose
Side effects: Sitagliptin (Januvia)
Hypoglycemia
Inc. risk of acute/chronic pancreatitis
Indication: Pramlintide (Symlin)
Type 1 or 2 diabetes pts who are not achieving their A1c goal levels
First drug for type I since 1920s
Contraindication: Pramlintide (Symlin)
Cannot be combined with insulin
Side effect: Pramlintide (Symlin)
NAUSEA, modest weight loss
No hypoglycemia or weight gain
Rapid-acting insulin
Lispro (Aspart)
Humulog (Novalog)
Short-acting insulin
Regular Insulin (Humulin R)
Intermediate-acting insulin
NPH (Humulin N)
Long-acting insulin
Glargine (Lantus)
Insulin type for sleeping hours
Glargine (Lantus)
Insulin type before meals
Lispro (Aspart)
Side effects: Insulin
Weight gain, hypoglycemia (seizures, coma, death), hypokalemia, fibrotic/atrophic injection sites
Indication: Glucagon
Severe hypoglycemia
MOA: Glucagon
Stimulation of glucagon receptor sites -> increased glucose levels from hepatic breakdown
When prescribing Metformin to a pre-diabetic/diabetic women of child-bearing age who have been unable to become pregnant, be conscious that ___.
Prescription of OCs may be needed to prevent pregnancy
A person with a Dexa scan T-score of -1 has __ the risk of a normal 40 year old. -2? -3?
- 1 has 2x the risk
- 2 has 4x the risk
- 3 has 8x the risk
T -1 or higher = ___
Normal
T -2.5 to -1 = ___
Osteopenia
T below -2.5 = ___
Osteoporosis
T below -2.5 plus bone fragility = ___
Severe osteoporosis
Risk factors: Osteoporosis
F, Small/thin body stature, increased age, Caucasian/Asian, FHx, diet low in Ca/Vit D, Low E(F), Low T(M), inactive lifestyle, smoking, excess EtOH, glucocorticoids, anticonvulsants
Side effects: Calcitriol (Rocaltrol)
Inc. serum calcium levels
Indication: Calcitonin (Mialcin)
Treatment of osteoporosis
Indication: Raloxifene (Evista)
Treatment and prevention of osteoporosis
Reduce risk of breast cancer
Class: Raloxifene (Evista)
Selective estrogen receptor modulator (SERM)
MOA: Bisphosphanates
Inhibit osteoclast activity - inc. bone mass
Indication: Bisphosphanates
Treatment and/or Prevention of osteoporosis
Side effect: Alendronate (Fosamax)
Heartburn, N, ESOPHAGITIS, OSTEONECROSIS OF THE JAW, ATYPICAL FEMUR FRACTURES, myalgia
Class: Alendronate (Fosamax)
Bisphosphanate
Indication: Alendronate (Fosamax)
Prevention and Treatment of osteoporosis
MOA: Alendronate (Fosamax)
Inhibition of osteoclast activity
MOA: Raloxifene (Evista)
Binding to select estrogen receptor sites
Contraindications: Raloxifene (Evista)
Pregnancy, lactating women, women with active/hx of DVT/PE/renal vein thrombosis
Class: Calcitonin (Miacalcin)
Synthetic hormone from parathyroid gland
MOA: Calcitonin (Miacalcin)
Inhibition of osteoclast activity
Class: Teriparatide (Forteo)
Synthetic PTH analogue
Indication: Teriparatide (Forteo)
Treatment of osteoporosis
MOA: Teriparatide (Forteo)
Activates bone turnover, stimulates new bone formation in spine/hip
Teriparatide (Forteo) can be used for how long?
Up to 2 years
When estrogen is taken alone, it can increase a woman’s risk of ___.
endometrial cancer
What is usually combined with estrogen in HRT to mitigate the risk for cancer?
progestin hormone
What is Prempro?
HRT (mix of estrogen and progestin)
Prempro has been linked to increased risk for ___.
MI, stroke, DVT/PE, breast cancer
Indication: Denosumab (Prolia)
Osteoporosis (tx), bone metastases, RA, MM, giant cell tumor
MOA: Denosumab (Prolia)
inhibits RANKL -> RANK not activated on pre-osteoclasts -> osteoclasts not formed
Route: Denosumab (Prolia)
SQ, every 6 mos
Indication: Estrogen in postmenopausal women
Symptoms of menopause (hot flashes, night sweats, tissue atrophy (vulva, vagina, urethra), insomnia, osteoporosis)
BiEst is a combination of ___
estriol, estradiol (80:20)
TriEst is a combination of ___
estriol, estradiol, estrone (80:10:10)
Bio-identical estrogen has been shown to decease risk of ___ compared to synthetic estrogen.
blood clots
Indications: Conjugated estrogens (Premarin)
Prevention/Tx of osteoporosis, post-menopausal sxs (hot flashes, vaginal dryness, itching)
Premarin is a combination of ___
conjugated estrogens (estrone, equillin)
MOA: Conjugated estrogens (Premarin)
Alters gene transcription
___ should be added to estrogen HRT in ____.
Progesterone
Women who have NOT undergone a hysterectomy
Side effects: Conjugated estrogens (Premarin)
vaginal bleeding, breast tenderness/pain, inc. risk of DVT, inc. risk of atherosclerosis and CAD, inc. risk of uterine and breast CA, inc. breast size,
Contraindications: Conjugated estrogens (Premarin)
Hx of DVT, breast CA, ovarian CA, uterine CA
Category X
Class: Medroxyprogesterone (Provera)
Synthetic progresterone
Indications: Medroxyprogesterone (Provera)
Contraceptive, HRT, DUB, endometriosis
MOA: Medroxyprogesterone (Provera)
Alters gene transcription
Contraindications: Medroxyprogesterone (Provera)
Hx of DVT, breast CA, ovarian CA, uterine CA
Category X
Class: Pramlintide (Symlin)
Amylin agonist analogs
MOA: Pramlintide (Symlin)
Slows gastric emptying, suppresses glucagon production and release
Class: Exenatide (Byetta)
Incretin (GLP-1) mimetics
MOA: Exenatide (Byetta)
Enhance glucose-dependent insulin secretion, suppress glucagon secretion, slow gastric emptying
MOA: Estrogen vs. Progestin in OCs
Estrogen suppresses ovulation
Progestin prevents implantation in the endometrium via inhibition of gonadotropin secretion
Dosages of E vs. P in OCs
Constant dose of E over 21 days
Increasing, triphasic dose of P over 21 days
OCs may lower the risk for what type of cancer?
Colorectal, Ovarian, Endometrial
What is a “mini-pill”?
Progestin-only OC
Drugs that can reduce the efficacy of OCs when used concurrently?
Penicillin, Amoxil, Tetracycline, Cephalosporins, Sulfa drugs, seizure drugs, St. John’s wort
The use of OCs for 5 years or more dec. risk of ovarian cancer later in life by __.
50%
The use of OCs for 10 years or more dec. risk of ovarian cancer and endometrial cancer later in life by __.
80%
Class: Drospirenone (Yaz, Yasmin)
Anti-androgenic synthetic progestin
Depo-Provera is a injectable contraceptive given ___
4 times per year
Class: Depo-Provera
Progestin-only injectable contraceptive
MOA: Depo-Provera
Dec. GnRH release -> Dec FSH and LH - inhibition of follicular development and ovulation
Depo-Provera has been shown to reduce the risk of endometrial cancer by up to ___.
80%
Side effects: Depo-Provera
Menstrual irregularities, abd. discomfort, weight changes, HA, hair loss, fatigue, depression, nervousness, DELAYED RETURN OF FERTILITY
BONE LOSS, INC RISK FOR OSTEOPOROSIS
How long does it take for fertility to return after discontinuation with Depo-Provera?
9-10 months
What does the black box warning for Depo-Provera say?
Do not use for > 2 years dt concerns over bone loss
Class: Implanon
Implantable progestin contraceptive
Implanon is inserted (location) and must be removed within ___.
Inner arm
3 years
Class: Ortho Evra
Transdermal patch contraceptive
Contraindications: Nuva ring
Risk of blood clots
MOA: Paragard
Impairs mobility of sperm
Irritates endometrial lining -> inhibits implantation
MOA: Mirena, Liletta, Skyla
Release of long-acting synthetic progestin (Levonorgestrel) -> diminish frequency of ovulation and changes in cervical mucosa -> dec. implantation
Ingredients: Plan B, Next Choice
Progestin-only (Levonorgestrel)
Class: Ulipristal acetate (Ella)
Selective progesterone receptor modulator (SPRM)
Indication: Ulipristal acetate (Ella)
Emergency contraception
MOA: Ulipristal acetate (Ella)
Delay/inhibition of ovulation and inhibition of follicle rupture
Which form has been shown to be more effective as a morning after pill: combination or progestin-only?
Progestin-only
Class: Mifepristone (Mifeprex)
Synthetic steroid abortifacient
MOA: Mifepristone (Mifeprex)
Progesterone receptor antagonist w/ partial agonist activity, dec. human chorionic gonadotropin levels -> dec. progesterone production by corpus luteum
Contraindications: Mifepristone (Mifeprex)
Presence of IUD, ectopic pregnancy, known hemorrhagic d/o, on anticoagulant therapy, on long-term prednisone therapy
Class: Clomiphene (Clomid)
Estrogen receptor agonist
Indications: Clomiphene (Clomid)
Infertility, amenorrhea
MOA: Clomiphene (Clomid)
Binds to E receptor sites in brain -> interferes w/ normal negative feedback of E on GnRH -> inc secretion of GnRH -> inc release of LH and FSH -> ovulation
Side effects: Clomiphene (Clomid)
Vaginal dryness, vaginal bleeding, breast tenderness, anxiety, hot flashes
MULTIPLE BIRTHS
Contraindications: Clomiphene (Clomid)
Prior hx of LV dz, breast cancer, or uterine cancer
How long can Paragard be used?
10 years
Dosage of Levonorgesetrel: Mirena vs. Liletta vs. Skyla
Mirena = 52 mg (20 mcg/d)
Liletta = 52 mg (20 mcg/d)
Skyla = 13.5 mg (14 mcg/d)
How long can Mirena/Liletta be used?
5 years
How long can Skyla be used?
3 years
Indications: Exogenous T
Anemia, severe osteoporosis, hormone therapy for transsexual men
Side effects: Testosterone (M)
Acne, baldness, gynecomastia, priapism, inc. risk of prostatic hyperplasia and PrCa, worsening of sleep apnea, dec. sperm count/infertility, fluid retention/edema
Side effects: Testosterone (F)
Virilization (excess body/facial hair), acne, deepening of voice, clitoral enlargement, menstrual irregularities
Effect on Labs: Testosterone
Inc. LDL, dec. HDL, Inc. RBC
MOA: Testosterone
Alters gene transcription
MC indication of anti-androgen treatment?
Prostate cancer
Normal growth of prostate tissue is regulated by ___(2).
T, DHT
Class: Leuprolide (Lupron)
Anti-androgenic hormone, anti-estrogenic hormone
Indications: Leuprolide (Lupron)
Prostate cancer, precocious puberty, endometriosis, uterine fibroids, IVF
MOA: Leuprolide (Lupron)
GnRH agonist -> downregulation of FSH and LH -> dec. T/E
Indication: Finasteride (Proscar)
BPH, male-pattern baldness, PrCa
MOA: Finasteride (Proscar)
Limits conversion of T to DHT via inhibition of type II 5-alpha reductase
Side effects: Finasteride (Proscar)
Dec. libido, ED, impotency, depression, breast swelling, breast tenderness
Class: Sildenafil citrate (Viagra)
PDE5 inhibitor
Indications: Sildenafil citrate (Viagra)
ED, pulmonary HTN
MOA: Sildenafil citrate (Viagra)
Inhibition of PDE5 enzyme that degrades cGMP in the SM cells lining the blood vessels of the penis -> blood remains in penis -> erection maintained
Contraindications: Sildenafil citrate (Viagra)
Concurrent use w/ NO donors, organic nitrites/nitrates (nitroglycerin)
CV risk factors (recent stroke, heart attack)
Severe impairment of LV or KD fxn
Hypotension
Hereditary degenerative retinal d/o
Side effects: Sildenafil citrate (Viagra)
HA, flushing, nasal congestion, dyspepsia, impaired vision, cyanopsia
Acute angle closure glaucoma, ventricular arrhythmias, severe hypotension, MI, stroke, priapism
Contraindications: T replacement therapy
PrCa, BrCa, erythrocytosis, unstable CHF, severe untreated sleep apnea
Testosterone -> ? -> Estrogen
Aromatase