Endocrine Drugs Flashcards
What are the potential risks of estrogen therapy in women?
- Small increase in BP
- Increased risk of thromboembolism
- Cigarette smoking increases the risk of serious cardiovascular side effects, particularly in women smokers over the age of 35 years.
- N/V common
- Pregnancy Category X
What are common things to tell your patient about osteoporosis therapy when using bisphosphonates?
- Take with 8oz water to avoid esophageal injury and remain upright and take nothing by mouth for at least 30 minutes.
- Nausea and diarrhea are the most common side effects.
- Esophageal irritation, heartburn, and abdominal pain may also occur
- Because of dosage limitations and GI intolerance, two-thirds of the patients taking daily bisphosphonates and half of the patients taking weekly bisphosphonates discontinue therapy by the end of one year
- The bisphosphonates should not be prescribed for patients with esophageal problems, gastritis, or peptic ulcer disease.
What drugs can be used to relieve hot flashes?
Premarin is the only consistent satisfactory therapy to relieve hot flashes
What is Paroxetine [Brisdelle] used for?
- It is used to treat moderate-to-severe vasomotor symptoms associated with menopause.
- It does not cause weight gain or changes in libido
What are some emergency contraceptives for women who have unprotected sex?
- Preven
- Plan B
- Ulipristal Acetate (Ella)
How is Preven administered?
- Patients are given 2 tablets within 72 hours of unprotected intercourse at the initial visit and 2 tablets 12 hours later.
- May be effective for up to 5 days after intercourse
- If vomiting occurs within 2 hours, a repeat dose may be required
How is Plan B administered?
- Patients are given 2 tablets within 72 hours of unprotected intercourse at the initial visit and 2 tablets 12 hours later.
*
How does Plan B work?
- It acts by preventing ovulation and may prevent implantation of a fertilized egg. It will have no effect if a fertilized egg has already been implanted & will not terminate and existing pregnancy
- Importantly, if pregnancy does occur, having used levonorgestrel will not increase the risk of major congenital malformations, pregnancy complications, or any other pregnancy outcomes.
What are the s/x associated with Plan B?
Major Side Effects: heavier menstrual bleeding, nausea (can be reduced by taking an antiemetic 1 hr before dosing), abd pain, HA, dizziness
What type of contraceptive is Plan B & Ulipristal Acetate (Ella)?
progesterone receptor modulator.
How is Uliprist Acetate (Ella) administered?
- a single 30 mg dose is safe & effective for emergency contraception for up to 5 days following unprotected sex.
- It is effective even if taken 24-48 hours prior to ovulation.
What are some adverse effects of Ulipri Acetate (Ella)?
Most common adverse reaction (similar to levonorgestrel): HA, nausea, abd pain, dysmenorrhea, fatigue, dizziness.
What is the MOA of Ulipristal Acetate (Ella)?
- Acts as an agonist/antagonist at receptors for progestin.
- Like levonorgestrel, ulipristal acetate prevents conception primarily by suppressing ovulation.
What are the similarities and differences between levonorgestrel (Plan B) and Ulipristal Acetate (Ella)?
- Like levonorgestrel, ulipristal acetate prevents conception primarily by suppressing ovulation.
- Despite this similarity, ulipristal & levonorgestrel differ in 2 important ways:
- (1) ulipristal acetate remains highly effective when taken up to 5 days (120 hours) after intercourse, whereas levonorgestrel is most effective when taken within 3 days (72 hours) of intercourse;
What drugs are used in the management of preterm labor?
Of the various drugs with uterine relaxant effects (progesterone, NSAIDs, ethanol, magnesium sulfate & beta agonists), none are specific to the uterus other than hydroxyprogesterone,
What is Hydroxyprogesterone Caproate used for?
approved by the FDA to reduce the risk of preterm birth in females with singleton pregnancy.
How is Terbutaline used In the management of preterm labor?
- has been used to suppress premature labor although this is not an approved use.
- Oral terbutaline should not be used for prevention or any treatment of preterm labor because it has not been shown to be effective & is potentially dangerous
How is Ethanol used to prevent preterm labor?
It exerts a direct effect on the uterine muscle and suppresses oxytocin release from the pituitary gland
How does magnesium sulfate prevent preterm labor?
- It is given IV, has long been used to prevent preterm labor although it lacks FDA approved indication.
- It inhibits myometrial contractility mediated by calcium.
What are some drug interactions associated with prednisone?
- Antacids (not food) interfere with absorption.
- Enzymeinducers (phenytoin & rifampin) decrease blood levels and shorten the half life.
- When combined with K-depleting diuretics, there is an increased risk of hypoglycemia.
- When combined when NSAIDs, there is an increase in risk of GI ulceration.
- There may also be a decrease in effectiveness of glucose lowering drugs and a decrease in antibody reactions to vaccinations when used in tandem with glucocorticoids.
What are the common adverse effects associated with long term use of prednisone?
- Acute adrenal insufficiency results from too rapid withdrawal after long term treatment (s/s: fever, myalgia, arthralgia, malasia).
- After long term use, pt may need protection from stress for 1-2 years following d/c of drug.
- Implications of prolonged treatment include pituitary-adrenal suppression, fluid & electrolyte imbalance, hyperglycemia, glycosuria, increased risk of infection, peptic ulcers, osteoporosis, myopathy, hypertension, behavioral issues, cataracts, growth arrest, Cushing symptoms (moon face, buffalo hump), HPA suppression.
What are the best steroids to use for cerebral edema with the least sodium retention?
- Dexamethasone had minimal mineralocorticoid activity and is frequently used
- Corticosteroids in large doses are of value in reduction or prevention of cerebral edema that accompanies intracranial tumors, but edema from closed head injury is not predictable responsive
What are some adverse effects of using testosterone replacement in athletes?
Use of androgens can cause a number of serious adverse reactions and, of particular concern, is hepatotoxicity. Because of misuse the androgens are DEA schedule III
What are some lifestyle changes that can affect insulin dosages?
- Insulin needs are increased by infection, stress, and obesity, the adolescent growth spurt, and pregnancy.
- Insulin needs are decreased by exercise and during the first trimester of pregnancy.
What are the neoplastic effects seen when using oral contraceptives?
- Breast cancer (uncertain): FDA advisory Committee concluded that the data do not provide sufficient evidence that long term pill use actually causes an increase in breast cancer. It may promote growth of existing cancer, especially in women with certain genes.
- Endometrial cancer (benefit): Data suggests the pill (progesterone) reduces the risk of endometrial cancer.
- Ovarian cancer (benefit): Data suggest that pill use reduces the risk of ovarian cancer.
- Pituitary adenoma (uncertain): Data suggest no association between pill use & pituitary prolactinomas.
- Malignant melanoma (uncertain): Studies have reported both increased risk and lower risk.
What are the cardiovascular effects & gynecology effects seen with oral contraceptives?
- Lipids (risk/benefit/uncertain): Estrogens increase HDL while progestins decrease HDL.
- Ovarian cysts (benefit/uncertain): monophasic pills appear to decrease risk while multiphasic pills do not reduce risk.
- Benign breast disease (benefit): Progestin lowers risk of fibroadenoma and fibrocystic breast disease.
- Menstrual symptoms (benefit): Less iron deficient anemia (due to lighter menstrual bleeding), less dysmenorrhea, less PMS.
- Pelvic inflammatory disease (benefit/uncertain): OCs appear to offer protection against gonococcal PID but increase the incidence of lower tract infections with Chlamydia.
What are the first line drugs for endometriosis?
Combination oral contraceptives are considered 1 st line drugs for the treatment of endometriosis. Studies show they reduce pain scores by 45-52% (compared with 14-17% with placebo). They are often used in combination with NSAIDs although one study showed NSAIDs were no more effective than a placebo.
What are the Adverse effects of combination oral contraceptives?
- headaches/migraines, heavy/irregular vaginal bleeding, nausea/vomiting acne, dysmenorrhea, weight gain, mood changes, anxiety/panic attacks, and breast pain. All OCs increase the risk of venous thromboembolism.
- Most serious is the risk of thromboembolic disorders. Hypertension and abnormal uterine bleeding may occur but the risk is low
What are some patient instructions regarding taking Oral contraceptives?
- Starting pills for first time: Take pill at same time each day, starting either on first day of bleeding, or on the first Sunday after period begins, or on the 5th day after period begins.
- With 28-day pack, begin new pack immediately after using last pill in previous pack. With 21-day pack, stop taking pills for 1 week then start new pack. Progestin only: take one pill every day and do not skip days between packs; take at same time each day.
- Maximum effectiveness may not be reached for several days; additional contraceptive methods are recommended for the entire first cycle.
-
Missed pill:
- Additional contraceptive measures should be started immediately as soon as
- the omission is discovered and continued for at least 7 days.
- If one pill, take missed OC immediately and next OC at regular time.
- Two pills in first week: take 2 OCs daily for next two days then resume regular schedule.
- 2 pills in 3rd week or 3 pills anytime: take 1 OC daily until last day and then begin new OC cycle that same day.
- Missed period: If one missed period and no missed pills, there is an extremely low risk of pregnancy but if one or more pills were missed or there are 2 missed periods, stop taking pills, use an alternate form of birth control, and perform pregnancy test.
- Rescheduling menstrual cycle: Continue active pills until special occasion is past.
- Use alternate form of birth control during initial cycle, if missed doses, if severe diarrhea, or if antibiotic therapy.
- Stopping oral contraceptive: There may be a delay in resumption of normal menstrual cycle; delay conception for 1-3 months after discontinuation of OCs
What is the MOA of insulin?
Facilitates the transport of glucose across cell membranes and enhances phosphorylation
of glucose w/in cells. The result is a lowering of blood glucose as it enters muscle and fat cells
What are the AE associated with insulin?
- hypoglycemia (main symptom) . initial symptoms of hypoglycemia reflect the compensatory effects of increased epinephrine secretion (diaphoresis, tachycardia, hypertension, weakness, hunger).
- CNS symptoms of hypoglycemia reflect the dependence of the brain on glucose.
- HA, blurred vision, mental confusion, incoherent speech, coma, and convulsions.
- For Severe hypoglycemia, treat w/50% glucose solution or glucagon IV.
- Allergic reactions [erythematous indurated area at the site of insulin injection] &
- Lipodystrophy [fat at the sites of insulin injection; minimized by rotating sites].
- Insulin resistance is when there is > than 200 u of insulin used daily. associated w/trauma (s/s or infection).
What is the somogyi effect?
It is a rebound hyperglycemia that occurs after an early morning episode of insulin-induced hypoglycemia.
What drugs increase blood glucose levels?
- ACTH
- glucocorticoids
- thyroid hormones
- thiazides
- estrogens
- protease inhibitors
- epinephrine
- and glucagon.
What drugs decreases blood glucose levels?
- BBs
- ASA
- NSAIDs
- ETOH
- clofibrate
- ACE inhibitors
- and lithium
What type of insulin is Insulin Lispro (Humalog) & what is its onset of action ?
- Short duration; rapid acting insulin
- Onset 15-30 min of SQ injection, peak 30-120 min and DOA 3-4 hrs
What type of insulin is Insulin Aspart (Novolog) & what is its onset of action ?
- short duration; rapid acting
- Onset 10-20 min of SQ injection, duration of action 3-5 hrs. DOC in pump
What type of insulin is Regular insulin & what is its onset of action?
- short duration; slower acting
- DOC for abrupt onset of hyperglycemia or DKA
- Four approved routes: SQ injection, SQ infusion, IM injection (rarely), & oral inhalation
- Onset 30-60 min, peak 1-5 hrs and DOA 6-10 hrs. given IV or SC a.c
What type of insulin is NPH insulin (Humulin N & Novolin N) & what is its onset of action?
- It is an intermediate acting insulin
- onset 1-2 hrs, peak 4-12 hrs and DOA 18-24 hrs.
How is NPH insulin administered?
- Because onset is delayed, NPH insulin cannot be administered at mealtime to control postprandial hyperglycemia.
- Rather the drug is injected twice or three times daily to provide glycemic control between meals and during the night.
- It is only administered via SUBQ injection
What type of insulin is Insulin Glargine (lantus) & what is its onset of action?
- Long duration slow acting insulin
- Onset: 6-1-2hrs
- Peak: None
- Duration: 18-24hrs
- SQ injection forms micro precipitates that slowly dissolve, &
release insulin in small amounts over extended time
- don’t give IV and don’t dilute or mix w/any other insulin or solution
- Has a lower incidence of nocturnal hypoglycemia than NPH insulin
How is Insulin Glargine [Lantus] administered?
- Once daily and preferably at the same time every day.
- The drug should NOT be mixed with other insulins, and should NEVER be given IV.
What type of insulin is Detemir (levemir) & what is its onset of action?
- Slow onset & long duration
- At low doses(0.2u/kg) , DOA 12 hrs
- at higher doses(0.4u/kg) , DOA 20-24 hrs. b/c of slow onset/prolonged DOA used to provide basal glycemic control.
- Peaks in 12-24 hrs and DOA 12-24 hrs. Not given a.c. meals to control pp hyperglycemia
What type of drug is Exenatide (Byetta) and what is its MOA?
- Exenatide is a Glucagon Like P-1 agonist
- peptide hormones stimulate release of insulin from the pancreatic beta cells, lowers serum glucagon concentrations, slows gastric emptying and promotes satiety
Why is Exenatide (Byetta) used and what are some adverse effects associated with this drug?
- Used for glycemic control in pts w/DMII not controlled by oral agents
- Nausea is common and may be severe. Vomiting/diarrhea, hypoglycemia [w/sulfonylureas (reduce the dose of the sulfonylurea)]. Hypoglycemia did not occur when the drug was added to metformin alone.
- It is Pregnancy Category C –> it slows fetal growth and produces skeletal and other abnormalities.
What type of drug is Liraglutide (Victoza) and what are some precautions associated with this drug?
- GLP-1 receptor agonist
- It is not recommended for first-line therapy.
- Major adverse effect is nausea
- Hypoglycemia is a concern in patients taking liraglutide concurrently with insulin
- secretagogues, such as a sulfonylurea.
What is Glyburide used for and what is its MOA?
- available in combination w/metformin and is indicated as either 1st or 2nd line tx for T2DM
-
MOA:
- By binding to the plasma membrane of functional beta-cells, sulfonylureas cause a
decrease in potassium permeability and membrane depolarization which, leads to an increase in intracellular calcium ions & exocytosis of insulin-containing secretory granules.
* Stimulates pancreatic cells to secrete insulin; actively drive BG down by increasing insulin release from beta cells of pancreas; may also increase tissue response to insulin.
What are the adverse effects associated with Glyburide?
- Hypoglycemia with coma may occur but most likely with the long acting drugs, [in the elderly or in pts w/hepatic or renal dysfunction.]
- GI upset, sulfonylureas they may be taken with food except for glipizide, which should be taken 30 minutes before meals to increase effectiveness
- weight gain
- Not recommended for use in pregenancy
What are the drugs that increase risk of hypoglycemia d/t displacement of sulfonylureas (Glyburide) from serum proteins?
- Chloramphenicol, MAOI, salicylates, and sulfonamides.
What are drugs that can increase the risk of hyperglycemia with Glyburide?
- orticosteroids & thyroid, estrogens