Endocrine Drugs Flashcards
1
Q
What are the potential risks of estrogen therapy in women?
A
- 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
2
Q
What are common things to tell your patient about osteoporosis therapy when using bisphosphonates?
A
- 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.
3
Q
What drugs can be used to relieve hot flashes?
A
Premarin is the only consistent satisfactory therapy to relieve hot flashes
4
Q
What is Paroxetine [Brisdelle] used for?
A
- It is used to treat moderate-to-severe vasomotor symptoms associated with menopause.
- It does not cause weight gain or changes in libido
5
Q
What are some emergency contraceptives for women who have unprotected sex?
A
- Preven
- Plan B
- Ulipristal Acetate (Ella)
6
Q
How is Preven administered?
A
- 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
7
Q
How is Plan B administered?
A
- Patients are given 2 tablets within 72 hours of unprotected intercourse at the initial visit and 2 tablets 12 hours later.
*
8
Q
How does Plan B work?
A
- 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.
9
Q
What are the s/x associated with Plan B?
A
Major Side Effects: heavier menstrual bleeding, nausea (can be reduced by taking an antiemetic 1 hr before dosing), abd pain, HA, dizziness
10
Q
What type of contraceptive is Plan B & Ulipristal Acetate (Ella)?
A
progesterone receptor modulator.
11
Q
How is Uliprist Acetate (Ella) administered?
A
- 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.
12
Q
What are some adverse effects of Ulipri Acetate (Ella)?
A
Most common adverse reaction (similar to levonorgestrel): HA, nausea, abd pain, dysmenorrhea, fatigue, dizziness.
13
Q
What is the MOA of Ulipristal Acetate (Ella)?
A
- Acts as an agonist/antagonist at receptors for progestin.
- Like levonorgestrel, ulipristal acetate prevents conception primarily by suppressing ovulation.
14
Q
What are the similarities and differences between levonorgestrel (Plan B) and Ulipristal Acetate (Ella)?
A
- 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;
15
Q
What drugs are used in the management of preterm labor?
A
Of the various drugs with uterine relaxant effects (progesterone, NSAIDs, ethanol, magnesium sulfate & beta agonists), none are specific to the uterus other than hydroxyprogesterone,
16
Q
What is Hydroxyprogesterone Caproate used for?
A
approved by the FDA to reduce the risk of preterm birth in females with singleton pregnancy.
17
Q
How is Terbutaline used In the management of preterm labor?
A
- 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
18
Q
How is Ethanol used to prevent preterm labor?
A
It exerts a direct effect on the uterine muscle and suppresses oxytocin release from the pituitary gland
19
Q
How does magnesium sulfate prevent preterm labor?
A
- 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.
20
Q
What are some drug interactions associated with prednisone?
A
- 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.
21
Q
What are the common adverse effects associated with long term use of prednisone?
A
- 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.
22
Q
What are the best steroids to use for cerebral edema with the least sodium retention?
A
- 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
23
Q
What are some adverse effects of using testosterone replacement in athletes?
A
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
24
Q
What are some lifestyle changes that can affect insulin dosages?
A
- 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.
25
What are the neoplastic effects seen when using oral contraceptives?
1. **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.
2. **Endometrial cancer (benefit):** Data suggests the pill (progesterone) **reduces the risk of endometrial cancer.**
3. **Ovarian cancer (benefit):** Data suggest that pill use reduces the risk of ovarian cancer.
4. **Pituitary adenoma (uncertain)**: Data suggest no association between pill use & pituitary prolactinomas.
5. **Malignant melanoma (uncertain):** Studies have reported both increased risk and lower risk.
26
What are the cardiovascular effects & gynecology effects seen with oral contraceptives?
1. **Lipids (risk/benefit/uncertain):** Estrogens increase HDL while progestins decrease HDL.
2. **Ovarian cysts (benefit/uncertain):** monophasic pills appear to decrease risk while multiphasic pills do not reduce risk.
3. **Benign breast disease (benefit):** Progestin lowers risk of fibroadenoma and fibrocystic breast disease.
4. **Menstrual symptoms (benefit):** Less iron deficient anemia (due to lighter menstrual bleeding), less dysmenorrhea, less PMS.
5. **Pelvic inflammatory disease (benefit/uncertain):** OCs appear to offer protection against gonococcal PID but increase the incidence of lower tract infections with Chlamydia.
27
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.
28
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
29
What are some patient instructions regarding taking Oral contraceptives?
1. **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.
2. 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.
3. **Maximum effectiveness may not be reached for several days; additional contraceptive methods are recommended for the entire first cycle**.
4. **Missed pill:**
1. Additional contraceptive measures should be started immediately as soon as
2. the omission is discovered and continued for at least 7 days.
3. If one pill, take missed OC immediately and next OC at regular time.
4. Two pills in first week: take 2 OCs daily for next two days then resume regular schedule.
5. 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.
5. **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.
6. **Rescheduling menstrual cycle:** Continue active pills until special occasion is past.
7. Use alternate form of birth control during initial cycle, if missed doses, if severe diarrhea, or if antibiotic therapy.
8. **Stopping oral contraceptive:** There may be a delay in resumption of normal menstrual cycle; delay conception for 1-3 months after discontinuation of OCs
30
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
31
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).
32
What is the somogyi effect?
It is a rebound hyperglycemia that occurs after an early morning episode of insulin-induced hypoglycemia.
33
What drugs increase blood glucose levels?
* ACTH
* glucocorticoids
* thyroid hormones
* thiazides
* estrogens
* protease inhibitors
* epinephrine
* and glucagon.
34
What drugs decreases blood glucose levels?
* BBs
* ASA
* NSAIDs
* ETOH
* clofibrate
* ACE inhibitors
* and lithium
35
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
36
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
37
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
38
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.
39
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**
40
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
41
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.**
42
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**
43
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
44
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.
45
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.
46
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.
47
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
48
What are the drugs that increase risk of hypoglycemia d/t displacement of sulfonylureas (Glyburide) from serum proteins?
* Chloramphenicol, MAOI, salicylates, and sulfonamides.
49
What are drugs that can increase the risk of hyperglycemia with Glyburide?
* orticosteroids & thyroid, estrogens
50
What are some ABX that can cause hypoglycemia when taken with Glyburide?
* TMP/SMX, clarithromycin, levofloxacin, and fluconazole
51
What is type of drug is Glipizide and what is its MOA?
* Type: Oral hypoglycemic / Sulfonylurea
* MOA: Stimulates insulin release from the pancreatic beta cells; reduces glucose output from the liver; **insulin sensitivity is increased at peripheral target sites**
52
What type of drug is Repaglinide (Prandin) and what is its MOA?
* Type: Oral hypoglycemic
* MOA: oral hypoglycemic drugs, unrelated chemically to the sulfonylureas but are rapidly-acting insulin secretagogues that **lower blood glucose by stimulating the release of insulin from the pancreas** via the same mechanism as the sulfonylureas (block potassium channels and open calcium channels. Calcium influx increases insulin secretion.)
53
How is Repaglinide (Prandin) administered?
1. Dose of repaglinide is 0.5 to 4 mg PO **within 15 minutes of a meal (before or after).**
2. Blood levels of repaglinide may be altered by drugs affecting the CYP3A4 isoenzymes (metabolites are not active).
3. **Patients with moderate to severe impairment of liver function had higher and more prolonged serum concentrations of repaglinide.**
4. Repaglinide has a half-life of about 1 hr.
54
What are some adverse drug reactions associated with Repaglinide (Prandin)?
* **hypoglycemia - most common side effect**
* weight gain other adverse reactions: not different from placebo studies.
* (Pregnancy Category C)
55
What type of drug is Metformin [Glucophage] and what is its MOA?
* Oral antihyperglycemic
* MOA:
* It does NOT stimulate insulin release from the pancreas hence rarely causes hypoglycemia or weight gain (as is reported with sulfonylureas).
* Inhibits glucose production in liver **[prevents the release of glucose from the liver]**
* May increase sensitivity of insulin receptor sites in target tissues [fat & skeletal muscle]
* May decrease absorption from the gut; therefore, does not actively drive BG down, & poses little added risk of hypoglycemia when used alone [monotherapy]
* Lowers LDL and increases HDL. **Decreases glucose production by liver, increases tissue response to insulin. Decreases glucose production be the liver; increases tissue response to insulin.**
56
What are some adverse effects associated with Metformin [Glucophage]?
* **NVD [20%] main**. weight loss, unpleasant taste [3%] and lowered vitamin B12 levels [9%].
* GI distress (diarrhea, N/V, abdominal bloating) occurs in 20% of pts . b/c GI s/s during therapy initiation appear to be dose-related
* Because GI symptoms during therapy initiation appear to be dose-related, t**he suggestion is to start with 500 mg bid with morning and evening meal (this dose is unlikely to cause a clinically significant response) and increase dosage gradually (500 mg/week)**
57
For which type of patients is Metformin [Glucophage] administration **contraindicated?**
* renal dysfxn
* metabolic acidosis
* alcoholics - Caution against excessive alcohol intake since alcohol potentiates the effects of metformin on lactate metabolism.
58
What are some patient teaching points regarding Metformin?
* Advise patients to take immediate release tablets twice daily with the morning and evening meals
* Advice to take extended release Metformin once daily with Evening meal
* **Inform patients about early signs of lactic acidosis-hyperventilation, myalgia, malaise, and unusual somnolence and instruct to seek medical attention if these symptoms develop.**
* Notify them that they can experience Nausea, Diarrhea and appetite reduction subside overtime if untolerable seek attention for alternative therapy.
* **Can reduce absorption of Vitamin B12 and Folic Acid**
* **Inform patients Alcohol increases the risk of Lactic Acidosis, should be avoided or consumed in moderation.**
59
What type of drug is Pioglitazone [Actos] and what is its MOA?
* Type: Glitazone
* MOA: Decrease insulin resistance and increase glucose uptake by muscle & adipose tissue. Also, decrease glucose production by the liver
60
How is Pioglitazone [Actos] administered?
* well absorbed and may be given once daily without regard to meals.
* Elimination half-life is 3 to 7 hr for both drugs
61
What are some adverse drug reactions associated with Pioglitazone [Actos]?
* **HF main adverse effect secondary to renal fluid retention**. UR/LR infxns, HA, sinusitis, myalgia and **fluid retention.**
* Most common adverse reactions to pioglitazone are upper respiratory tract infections [URI (13%)], HA (9%), sinusitis (6%) and myalgia (5%).
* **Pioglitazone should be avoided in patients with heart failure. ( Black Box Warning**
62
What type of drug is Acarbose [Precose] and what is its MOA?
* **Type:** Alpha-glucosidase inhibitor
* **MOA:** acarbose & miglitol reversibly bind to and block alpha-glucosidase at the brush borders of the small intestine and **minimize upper intestinal digest of carbs; prevents complex carbohydrates break down to monosaccharides.**
63
How is Acarbose [Precose] administered?
give Acarbose or miglitol 25 mg tid PO with the first bite of each meal
64
What are the adverse drug reactions associated with Acarbose [Precose]?
* **GI s/s [most common main]-** Abd pain (21%), diarrhea (33%), and flatulence (77%)
* (The delay in CHO absorption promotes increased fermentation of carbohydrates causing the GI effects.)
65
What is the MOA of Sitagliptin [Januvia]?
* increseases the availability of GLP-1 (T2diabetics have reduced levels of GLP-1); inhibits DPP-IV (which inactivates GLP-1) & increase the availability of GLP-1
* The gliptins “slow inactivation of the incretin hormone & reduce fasting and postprandial glucose concentrations in a glucose-dependent fashion.”
* **Because their effect is dependent on glucose , they do not cause hypoglycemia or weight gain.**
66
What are some adverse effects associated with Sitagliptin [Januvia]?
* Common adverse effects include nasopharyngitis, URIs,& HAs.
* Hypersensitivity reactions (angioedema, urticaria, skin exfoliation, bronchial hyperreactivity) have been reported.
* Hypoglycemia may occur when used with a sulfonylurea (reduce dose of sulfonylurea.
67
What type of drug is Canagliflozin [Invokana] and what is its MOA?
* **Type:** Sodium glucose co-transporter 2 inhibitor
* MOA: decrease glucose reabsorption and increase urinary glucose excretion and lowers BG levels. Sodium-glucose co-transporter 2 (SGLT2) is a membrane protein found mainly in the kidney . It transports filtered glucose from the proximal renal tubule into tubular epithelial cells.
## Footnote
**By inhibiting SGLT2 , canagliflozin and dapagliflozin**
**1. decrease glucose reabsorption,**
**2. increase urinary glucose excretion and**
**3. lowers blood glucose levels .**
68
What drugs can decrease serum concentrations of Canagliflozin [Invokana]?
* Rifampin,
* Phenobarbital,
* ritonavir, and
* phenytoin).
69
How is Canagliflozin [Invokana] administered?
Once daily before the first meal
70
What are the adverse effects associated with Canagliflozin [Invokana]?
* **Yeast infections**, volume depletion (r/t diuretic effect) and weight loss.
* Genital mycotic infections have occurred in both men and women **(increased sugar in the urine).**
* They also increase the risk of urinary tract infections.
* Canagliflozin, empagliflozin and dapagliflozin can have a **diuretic effect and cause volume depletion , especially in elderly patients with renal dysfunction.**
* **They may cause weight loss and has a low risk of hypoglycemia** (40% in study patients; 30% in placebo patients with canagliflozin)
71
What are some warnings associated with Canagliflozin [Invokana]?
* increased risk of fractures with canagliflozin
* **The FDA has warned that use of SGLT2 inhibitors may lead to ketoacidosis in type 2 diabetic patients**
72
What do studies suggest regarding diabetes control?
* Studies suggest that the extended-release formulation appears to be more effective than twice-daily immediate-release formulation in lowering HbA1c and equally effective in reducing body weight.
* There are no specific guidelines for selecting oral agents, but recent long-term randomized studies suggest that metformin should be the preferred agent for initial therapy. However, other studies also point out problems with this drug because of the misuse of metformin in patients for whom it is contraindicated.
* The package insert states mixing pramlintide in the same syringe with insulin should not be done but clinical studies found no clinically significant difference in effect when mixed. The half-life of the drug is about 48 minutes.
73
How should a patient be taught to prepare subQ injections?
1. Before loading the syringe, disperse insulin suspensions (i.e NPH insulin preparations) by rolling the vial between the palms. Vigorous agitation cause frothing and must be avoided. If granules or clumps remain after mixing discard the vial.
2. Except for NPH insulin, all preparations are formulated as clear, colorless solutions, and hence can be administered without resuspension. If a preparation becomes cloudy or discolored, or if a precipitate develops, discard the vial.
3. Before loading the syringe, swab the bottle cap with alcohol
4. Eliminate air bubbles from the syringe and needle after loading
5. Cleanse the skin (with alcohol or soap and water) before injection.
74
What should be taught to patients regarding subQ injection sites?
1. Usual sites of injection are the abdomen, upper arm, and thigh. To minimize variability in responses, make all injections in just one of these areas. Injections in the abdomen provide the most consistent insulin levels and effects
2. Rotate the injection site within the general area employed (e.g. abdomen)
3. Allow about 1 inch between sites. If possible, use each site just once a month
75
What should patients be taught regarding insulin storage?
1. Store unopened vials of insulin in the refrigerator but do not freeze. When stored under these conditions, insulin can be used up to the expiration date on the vial.
2. The vial in current use can be stored at room temperature for up to 1 month but must be **kept out of direct sunlight and extreme heat.** Discard partially filled vials after several weeks if left unused.
3. Mixtures of insulin prepared in vials may be stored for 1 **month at room temperature, and for 3 months under refrigeration.**
4. Mixtures of insulin in prefilled syringes (plastic or glass) should be stored in a refrigerator, where they will be stable for at least 1 week, and perhaps 2 weeks. Store the syringe vertically (needle pointing up) to avoid clogging the needle. Gently agitate the syringe before administration to resuspend the insulin.
76
What is the DOC for hypothyroidism?
Levothyroxine (#1) [Synthroid] Levothyroxine (sometimes simply called thyroxine although there is a dextrothyroxine) is the preferred and most frequently administered drug for hypothyroidism, generally given orally.
77
What are the s/x associated with Levothyroxine [Synthroid]?
* Side effects are rare unless the dose is too high, in which case the symptoms are similar to hyperthyroidism **(weight loss, nervousness, irritability, sweating, diarrhea, tremors, and tachycardia).**
* The elderly with cardiovascular diseases may be especially at risk for side effects.
* Long-term therapy has been associated with decreased bone density in pre- and postmenopausal women. Angina pectoris and atrial fibrillation have been reported, particularly in elderly patients
78
What are some drug interactions associated with Levothyroxine [Synthroid]?
* Cholestyramine, orlistat and antacids may interfere with the oral absorption of thyroxine.
* Glucocorticoids may decrease TSH secretion. Lithium decreases thyroid hormone secretion while amiodarone may either increase or decrease thyroid hormone secretion.
* Enzyme inducers may increase hepatic metabolism of thyroxine.
* Thyroxine increases the anticoagulant effect of warfarin by increasing the catabolism of hepatic clotting factors.
79
What is the MOA of propylthiouracil and methimazole [Tapazole] and what type of drugs are they?
* **Type:** anti-thyroid drugs
* **MOA:** They inhibit the formation of thyroid hormone by interfering with the incorporation of iodine into tyrosine residues of thyroglobulin and suppress synthesis of thyroid
hormones. They do not destroy existing thyroid hormones; hence require several weeks before producing an euthyroid state. Some authorities suggest that methimazole (10-20 mg/d) is preferred to propylthiouracil because of a lower risk of liver injury, is safer and dosing is more convenient.
80
How is propylthiouracil administered?
Administered orally and rapidly concentrate in the thyroid gland. They are used to return the patient to an euthyroid state. Therapeutic effect may require several weeks because of stores of thyroid hormones. After several years they may be discontinued because 30-40% of patients remain euthyroid after withdrawal of the drug
81
Propylthiouracil is considered the DOC in which instances?
* Propylthiouracil is considered the drug of choice in pregnancy and during breast feeding (PTU apparently causes less congenital disorders and is found in insignificant amounts in milk.).
* In life-threatening thyroid storm, propylthiouracil may be preferred because it inhibits conversion of T4 to T3 (methimazole does not).
82
What are the s/x associated with Propylthiouracil administration?
* Side effects are a skin rash (3%), hepatic injury, and leukopenia.
* Patients should be advised to report sore throat and fever
* **Propylthiouracil is the 3 rd leading cause of liver transplants due to drug toxicity** (acetaminophen and isoniazid are the first two)
* **Agranulocytosis is the most feared side effect of antithyroid drug therapy**. It occurs in about 0.3% of patients, the incidence is the same with both drugs (other references suggest agranulocytosis is more common with PTU), and **almost always occurs within the first 3 months of therapy**
83
How is iodide used to treat hyperthyroidism?
Iodides inhibit release of thyroid hormone by a negative feedback effect on the hypothalamus or anterior pituitary. Their effect is short lived but they are effective in the acute management of hyperthyroidism. Iodides (potassium iodide saturated solution [KISS]) also are used to protect the thyroid from radioactive iodine fallout after a nuclear acciden
84
How is radioactive iodide used to treat hyperthyroidism?
* Radioactive Iodine ( 131 I) is rapidly and efficiently trapped by the thyroid gland. Emission of beta rays destroys thyroid cells with little or no damage to surrounding tissue. After a single dose, 40%-70% of patients will be euthyroid in 6-8 weeks. In most patients,
* hypothyroidism will occur and long-term T4 replacement will be necessary
85
How is propranolol used to treat hyperthyroidism?
* Beta-blockers without sympathomimetic activity (eg. propranolol, metoprolol, atenolol) **may be used in conjunction with antithyroid drugs to control the cardiac events in thyroid storm.**
* They do not affect thyroid hormone synthesis; rather, they act by d**ecreasing the symptoms of adrenergic stimulation, particularly the life-threatening tachycardia.**
* Propranolol is the drug most commonly mentioned in the literature. The beta blockers should be tapered and discontinued as soon as the patient is euthyroid and asymptomatic.
86
How is hyper or hypothyroidism diagnosed?
Measurement of a serum thyroid-stimulating hormone (TSH) level is adequate for the diagnosis of hypothyroidism and hyperthyroidism (target range 0.5-2.5 microunits/mL) although some references suggest actual thyroid function depends on the level of free T4
87
What are the two types of hypothyroidism?
1. Primary (failure of the thyroid gland)
2. Secondary (failure of TRH or TSH release)
88
What causes hypothyroidism and what are some symptoms seen?
* Lack of dietary iodine, inflammation, and certain drugs may also cause hypothyroidism.
* Full-blown hypothyroid syndrome in adults is called myxedema **(cold intolerance, weight gain, constipation, lethargy, thick dry skin, and puffy appearance)**
89
What are the treatment options for Diabetes Insipidus?
* Hyposecretion of vasopressin results in diabetes insipidus; it characterized by excretion of large amounts of dilute urine.
* Neurogenic diabetes insipidus is caused by tumors or trauma in the hypothalamus or pituitary and is treated by replacement therapy with **vasopressin or desmopressin.**
90
What are the uses for Vasopressin?
* **It is indicated (IM injection):**
* For prevention and treatment of postoperative abdominal distention
* In abdominal roentgenography to dispel interfering gas shadows
* Diabetes insipidus
* **Unlabeled uses include administrated IV:**
* Bleeding esophageal varices
* In place of epinephrine in the treatment of Vfib/pulseless vTach cardiac arrest (given IV; extravasation causes severe tissue injury).
Because it can only be given by injection and has a duration of action of 2-8 hours, its usefulness in the treatment of diabetes insipidus is limited.
91
What are the s/x associated with Vasopressin?
* Facial pallor, nausea, belching, abdominal cramps and bronchial constriction (because it affects v1 & v2 receptors)
* **It may cause severe vasoconstriction if extravasation occurs.**
* It must be used cautiously in patients with vascular disease and in the presence of epilepsy, migraine, asthma, or heart failure.
* It is used as an alternative to epinephrine (to increase blood pressure) for the treatment of shock-refractory V. fib. It is given 40 U IV as a single dose, followed by amiodarone or procainamide. **Vasopressin may be more a more effective vasopresor agent than epinephrine for promoting return of spontaneous circulation in cardiac arrest.**
92
What is Ergonovine (Ergotrate) used for & how is it administered?
* These agents are used as **postpartum oxytocics**, causing prolonged and intense contractions of the uteruss.
* The drugs may be used orally or IM (IV is not recommended).
* Onset of action is about 5 min after IM injection and persists for about 3 h.
93
What are the s/x and contraindications for using Ergonovine (Ergotrate)?
* At usual doses may cause uterine cramping as well as nausea, vomiting, and diarrhea.
* Are vasoconstrictors but at usual doses they do not cause significant increases in blood pressure in most subjects. However, IV use or use in patients with potential cardiovascular risk, increases in blood pressure may be associated with eclampsia, CVA, or limb ischemia.
* **Accidental overdoses or extended use of the drugs may cause ergotism, characterized by NVD, hypertensive reactions, limb ischemia, and seizures.**
94
What is the MOA of prednisone?
* They suppress inflammation by stabilizing mast cells, preventing the release of various chemicals (e.g., histamine, serotonin, leukotrienes) that cause inflammation and edema. They also prevent infiltration and activity of inflammatory cells (neutrophils & eosinophils).
* **They potentiate the effect of beta-agonists and prevent down-regulation of beta-receptors**
95
How is prednisone used in the treatment of asthma?
* Corticosteroids may be useful in long-term treatment and suppression of asthma that fails to respond to other antiasthmatic preparations. Because of side effects of long-term use, the goal is to gradually decrease the dose and ultimately discontinue the corticosteroid.
* Aerosol therapy with glucocorticoids is less likely to suppress the hypothalamic-pituitary-adrenal axis than systemic use. (Most glucocorticoids used by inhalation for asthma are rapidly metabolized and have relatively little systemic action.)
* **Inhaled anti-inflammatory agents are considered drugs of choice in persistent asthma.**
96
What are the drug interactions with Cholestyramine?
It decreases bioavailability of Mycophenolate Mofetil by 40%, **may interfere with the oral absorption of thyroxine.**
97
When and why is leucovorin used for?
Levoleucovorin (active isomer of leucovorin) was approved by FDA for rescue therapy of patients receiving high doses of methotrexate, beginning as soon as possible after a methotrexate overdose.
98
What is Tamoxifen (Novaldex) used for?
* Tamoxifen ( Novaldex) is considered the gold standard for endocrine treatment of breast cancer.
* This drug is approved for **treating established disease and primary prevention** in women at high risk.
99
What is the MOA of Tamoxifen (Novaldex)?
* It is a prodrug that undergoes hepatic conversion to active metabolites. These metabolites then block ERs (estrogen receptors) on breast cancer cells, and thereby prevent receptor activation by estradiol, the principal endogenous estrogen.
* Estrogen acts on tumor cells to stimulate growth and proliferation.Hence, in the absence of estradiol influence , the rate of tumor cell proliferation declines. Tumor regresses in size as the rate of cell death outpaces new cell production.
* **For treatment is to be effective, target cells must be estrogen receptor positive.**
100
What are common s/x of antineoplastic drugs?
* Neutropenia, thrombocytopenia, anemia, digestive tract injury, stomatitis, diarrhea, N&V,
* Other important toxicity: Alopecia, reproductive toxicity, hyperuricemia, local injury from extravasation, Unique toxicities pertaining to individual medications, Cacinogenesis
101
What are some characteristics of malignant (neoplastic) cells that makes chemotherapy possible?
1. **Persistent Proliferation** - Cancer cells undergo unrestrained growth & division.
* This capacity for persistent proliferation is the most distinguishing property of malignant cells.
* Malignant cells are unresponsive to the feedback mechanism that regulate cellular proliferation in healthy tissue.
2. **Invasive Growth -** Malignant cells are free of the constraints that inhibit invasive growth. As a result, cells of a solid tumor can penetrate adjacent tissues, thereby allowing the cancer to spread.
3. **Formation of Metastases -** Metastases are secondary tumors that appear at sites distant from the primary tumor. Metastases result from the unique ability of malignant cells to break away from their site of origin, migrate to other parts of the body (via the lymphatic & circulatory systems), & then reimplant to form a new tumor.
4. **Immortality -** Cancer cells can undergo endless divisions. The underlying cause is telomerase, an enzyme that is active in most cancers, & expressed only rarely in normal cells. Telomerase permits repeated divisions by preserving telomeres - the DNA-protein “caps” found on the end of each chromosome. In cancer cells, telomerase continually adds back lost pieces of the telomere, & thereby preserves or extends telomere length. As a result, cancer cells can divide indefinitely
102
What are some s/x associated with Cyclophosphamide?
* Damage to hair follicles leading to alopecia is common, “Highly” emetogenic (\>90%), thrombocytopenia less common. **N&V occur regardless of route of administration.**
* **Sterile hemorrhagic cystitis** occurs in 7-40% of patients (force fluids and void often). May be severe or even fatal.
103
What is the MOA of Cetuximab and Gefitinib?
* Drugs that inhibit EGFR, **suppress cell proliferation and promote apoptosis** (programmed cell death).
* Cetuximab, erlotinib and gefitinib are drugs that either block the receptor or **inhibit TK directly, which in turn blocks the Epidermal growth factor receptor from activating**
* Cetuximab (Erbitux) is a monoclonal antibody that competitively binds with high affinity to the EGFR. It is being studied for use in colorectal cancer as well as other solid tumors.
* Gefitinib, erlotinib and lapatinib are tyrosine kinase inhibitors also targeting EGFR and HER2.
104
What are the two type of flu vaccine available & what reactions are associated with each type?
1. **Inactivated influenza vaccine:** adverse effects are uncommon, except for soreness in the IM site. People who have not been vaccinated previously may experience fever, myalgia and malaise for 1-2 days. Flu vaccine may carry a small risk of Guillain-Barre syndrome.
2. **Live, attenuated influenza vaccine:** some adverse effects include mild transient effects. Runny nose, nasal congestion, cough, headache, vomiting, muscle aches and fever.
105
What are some precatuions / contraindications for receiving the flu vaccine?
People with acute febrile illness should defer vaccination until symptoms abate. **Special considerations are indicated for people with hypersensitivity to egg**s because the vaccines are produced from viruses grown in eggs and may contain trace amounts of egg proteins.
106
Who should be vaccinated with the flu shot?
It is recommended for 6 months and older, especially for those at high risk of flu complications such as: children younger than 2, children 18 years and younger receiving long term aspirin therapy, pregnant women, people 65+, people who are morbidly obese, those who live in nursing homes, american indians/alaska natives, people who are immunosuppressed and people with certain chronic medical conditions such as spinal cord injuries, asthma, anemia, diabetes, heart, kidney, or lung disease, neurologic disorders such as epilepsy and cerebral palsy that can lead to breathing or swallowing problems. \* **these people at high risk should only receive the inactivated influenza vaccine.**
107
Who should not be vaccinated with the flu shot?
People who have SEVERE allergic reaction (angioedema, respiratory distress) to chicken eggs, people who have had a severe reaction of influenza vaccination in the past, people who have experiences GBS.
108
What are the common pediatric immunizations & their immunization schedules from birth to the 1st year of life?
* Birth- HepB
* 2 months- HepB, Dtap, Hib, IPV, PCV, RV
* 4 months- Dtap, Hib, IPV, PCV, RV
* 6 months- HepB, Dtap, Hib, IPV, PCV, RV, Influenza
* 12 months- HIB PCV, Varicella, MMR, HepA
109
What are the common pediatric immunizations & their immunization schedules from 15months - 12 years?
* 15-18 months- Dtap
* 18 months- HepA
* 4-6 years- Dtap, IPV, MMR, Varicella
* 11-12 years- Tdap, MCV4, HPV
110
What is Famciclovir used for?
Famciclovir is a prodrug used to treat acute herpes zoster(Shingles) and genital herpes infection. In patient with herpes zoster, the drug can decrease the time to full crusting from 7 days down to 5 days. In patient with genital herpes simplex infection, famciclovir is active against the first episode and recurrent episodes
111
What are the s/x associated with Cyclosporine?
Damage to hair follicles leading to alopecia is common, “Highly” emetogenic (\>90%), thrombocytopenia less common. N&V occur regardless of route of administration. Sterile hemorrhagic cystitis occurs in 7-40% of patients (force fluids and void often). May be severe or even fatal.
112
What type of drug is Azathioprine and what are some s/x associated with it?
* Immunosuppressive drug/ anti-regection drug
* S/X:
* Myelosuppression is the most significant adverse event, Leukopenia is the most common SE.
* **Hematological toxicity (leukopenia, thrombocytopenia) is the primary concern with use of azathioprine**.
* Infection is a predictable complication of any form of immunosuppressive therapy.
* **Nausea, vomiting, & diarrhea are common.** Hair loss, hepatotoxicity, and induction of neoplasms are also reported.
* **Azathioprine is contraindicated during pregnancy.**
113
What happens when Azathioprine is administered with allopurinol?
* Azathioprine is converted in the body to mercaptopurine, **which combines with nucleotides interfering with the synthesis of RNA and DNA.**
* Mercaptopurine is metabolized by xanthine oxidase; **hence concomitant administration of allopurinol (a xanthine oxidase inhibitor) requires a 65-75% reduction in dosage of azathioprine.**
114
What are the indications for receiving the Pneumonia 23 vaccine?
It is recommended for adults at increased risk of pneumococcal disease. It may be used in children over 2 years of age with chronic illnesses specifically associated with increased risk of pneumonia
115
How do vaccines work physiologically?
* Vaccines (whole bacteria or viruses that are killed or attenuated) and toxoids (denatured bacterial secretions i.e., toxins) stimulate active immunity and have greatly reduced the incidence and severity of many infectious diseases
* Administration of vaccines provokes an immune response identical to that which occurs during natural bacterial or viral infections. Development of immunity requires the presence of an immune system that is capable of an adequate response. (Immunosuppressants may diminish the immunological response to vaccines.
* Administration of a vaccine causes the recipient’s immune system to manufacture antibodies directed against the microbe from which the vaccine was made
116
When and to whom should live vaccines not be administered?
* should not be given to patients infected with HIV or who are otherwise immunosuppressed (including those taking corticosteroids or antineoplastic agents) or living with someone who is immunosuppressed.
* Likewise, **these vaccines should not be given during pregnancy**
117
What is the Tetanus Td or Tdap administration schedule?
* For persons aged 65 years or older who have close contact with an infant younger than 12 months should get vaccinated with the Tdap vaccine regardless of the interval since the last Td-containing vaccine.
* For adults, a one-time dose of Tdap is recommended then boosters with Td very 10 years.
118
What is Raloxifene [Evista] used for?
* It is a SERM [Selective Estrogen Receptor Modifier] drug that is an **agonist at estrogen receptors in bone but antagonist at estrogen receptors in the breast and endometrium.**
* It is given PO 60 mg once a day for the prevention and treatment of osteoporosis and to protect against estrogen receptor (ER) positive breast cancer.
119
What are some s/x and warnings associated with Raloxifene [Evista]?
* Like estrogens, it **increases the risk of deep vein thrombosis and pulmonary embolism (black box warning)**
* Unlike estrogens, it does not reduce hot flushes.
* **Most common side effects include hot flashes, leg cramps, weight gain and nausea.**
* Pregnancy Category X.
120
What type of drug is Clomiphene and what is its MOA?
* Nonsteroidal drug with a structure similar to synthetic estrogens.
* **It stimulates gonadotropin secretion by binding to estrogen receptors in the hypothalamus and anterior pituitary.** This diminishes the number of receptors available to the suppressant action of endogenous estrogen, signaling the hypothalamus to increase output of gonadotropin releasing factor and pituitary gonadotropin.
121
What is Clomiphene used for?
* It is used to promote follicular maturation and ovulation in selected infertile women. nonhormonal product similar to hCG which blocks estrogen receptors in the hypothalamus & pituitary and promotes pituitary release of FSH and LH.
* It is given orally (100 mg/day for 5 days) to treat infertility in women who have normal ovarian and pituitary function but lack the normal hypothalamic stimulus
122
What are the s/x associated with Clomiphene?
hot flashes, nausea, & abdominal discomfort
123
What are some common drug interactions with Rifampin?
* Cyclosporine clearance is accelerated by rifampin which leads to rejection of transplanted organs
* Rifampin can cause decreased levels of tacrolimus
* Decreases the level of offectiveness of oral contraceptives
* Can decrease serum concentrations of linagliptin
* Can decrease concentrations of Canagliflozin
