2Pharm II Flashcards
The Thyroid synthesizes ______ and ______ from ______
thyroxin (T4)
triiodothyronine (T3)
iodine
T/F
The control of secretion of T4 (thyroxin) and T3 (triiodothyronine) is determined by a negative feedback loop involving TRH (hypothalamus), TSH (anterior pituitary), and TH (thyroid)
True
Thyroid feedback loop: the hypothalamus secretes ______, the Anterior Pituitary secretes ______, and the Thyroid secretes _______
TRH
TSH
T4 and T3
Primary hypo/hyperthyroidism is a disease of the ______
Secondary hypo/hyperthyroidism is a disease of the ______
thyroid gland
hypothalamus or anterior pituitary
L-tyrosine is the precursor to ____ and _____
T4/T3 and epinephrine
Without iodine, there is a build up in the TH precursor, resulting in ______
goiter
What large glycoprotein integral to the synthesis of T4/T3 is NEVER secreted into the bloodstream?
Thyroglobulin
At the basement membrane, iodine is taken up by ______ epithelial cells
_____ precursors iodinate thyroglobulin
These are packaged into vesicles which are then fused with lysosomes and release the iodinated amino acids ____ and ____
Cuboidal
iodotyrosyl
T3, T4
What are the 2 synthetic thyroid preparations?
Which TH are they?
sodium levothyroxine (Synthroid, Levoxyl) T4
sodium liothyronin (Cytomel) T3
Why is sodium liothyronine (T3) less preferred than sodium levothyroxine (T4)?
Absorption more erratic
Synthroid is usually taken _____
It _____ the basal metabolic rate
in the morning/on an empty stomach
increases
T/F
Synthroid promotes gluconeogenesis, mobilizes glycogen stores, and stimulates protein synthesis
True
T/F
overuse of sodium levothyroxine (Synthroid) mimics hyperthyroidism and includes tachycardia, nervousness, increased appetite, and weight loss
True
Hyperthyroidism, aka _____ disease
Grave’s
The abuse of Synthroid is called _______ hyperthyroidism
Fictitious
What is the name of the Canadian drug used as palliative Tx of hyperthyroidism in preparation for radioactive iodine therapy?
Nickname?
Propylthiouracil
PTU
What are the side effects of propylthiouracil (iodination blocking drug for hyperthyroidism)?
Rash
Nausea
Agranulocytosis
What therapy is used in conjuction with propylthiouracil to prepare pts for surgery?
Saturated solution Potassium Iodide
*mechanism unclear
What drug is used in the palliative Tx of hyperthyroidism prior to thyroidectomy?
(Very expensive, inconvenient, serious adverse effects)
What oral side effects does it have?
Methimazole (Tapazole)
Tast alteration, salivary gland swelling
What is used to estimate the activity of the Thyroid Gland and irradiate/destroy it over a period of 3 months?
Radioactive Iodide I 131
What is easier from a Dental management perspective - hypo or hyperthyroidism?
Hypothyroid
In context of Dental considerations, Hypothyroid pts are more sensitive to what?
CNS depressants
*must lower dose of sedatives/opioids
Hyperthyroid pts have an Absolute contraindication to what?
Epinephrine
Hyperthyroid pts are less sensitive to what drug administered in Dental clinic?
CNS depressants
*may require higher dose.
**also may be mislabeled as “drug-seeking behaviors”
Type I Diabetes is an autoimmune disease that destroys ______ cells
Type II Diabetes occurs when ____ become blocked/insensitive
Beta (pancreatic)
insulin receptors
T/F
In Type I Diabetes the body destroys the beta cells, but the receptors are just fine.
True
_____% of diabetes is type I
____ is the only effective drug in treating Type 1 diabetes
10%
Insulin
*long ago was called Juvenile Diabetes
T/F
Insulin is a polypeptide, 5600 dalton mw, 2 chans connected by sulfide bridge
False
disulfide bridge
Older Insulin preparations came from cows/pigs, but this is no longer used because of ______ technology
recombinant
All insulins must be injected how?
SC
*although now we have a new inhalable form
In what 3 ways is insulin classified?
Onset
Peak
Duration
What are the 2 most popular insulins?
insulin Regular (HumuLIN R)
insulin Aspart (NovoLOG)
insulin Regular (HumuLIN R) is ____ acting
insulin Aspart (NovoLOG) is _____ acting
what are 3 additional categories of insulin?
short
rapid
intermediate, intermediate to long, long
(acting for all)
What is a long-acting insulin used for both type I and type II diabetes?
What are its oral complications?
insulin glargine (Lantus Solostar)
numb mouth
T/F
Some Type II diabetes interventions improve receptor function and control the insulin spike, but without lifestyle changes the pancreas will burn out.
True
It used to be that Type II diabetes was very rare before age ____
35
Why is there a lot of insulin in the blood of a Type 2 diabetic?
Target cells insensitive
What is the intervention for insensitive insulin target cells?
More insulin
*needed to get glc into cells
What is the outcome of Type 2 diabetes?
Hyperglycemia
T/F
Tx for Type 2 diabetes is Oral drugs, non-pharmacological intervention (weight, exercise, diet), and insulin
True
If a Type 2 diabetic is taking insulin, the pt is most likely poorly controlled
True
What are the 3 goals of drug therapy for Type2 diabetics?
***What is the risk for all of these interventions?
Increase insulin (w/ glc)
Suppress hepatic gluconeogenesis
Improve insulin sensitivity
***hypoglycemia
5 Drug classes to treat Type2 diabetes:
Sulfonylureas
Biguanides
Alpha-glucosidase inhibitors
Thiazolidinediones (TZD’s)
Incretins
What class of drugs promotes insulin release from pancreatic beta cells?
(type II intervention)
Sulfonylureas
The 2nd generation Sulfonylureas are more _____ but not more _____
potent
effective
What is a 1st generation Sulfonylurea?
*Tx Type II - promotes insulin release from beta cells
tolbutamide (Orinase)
*all end in “amide”
What is a 2nd generation Sulfonylurea?
glipizide (Glucotrol)
*all end in “ide”
What is the major distinction between 1st and 2nd generation Solfonylureas?
Potency
Sulfonylureas increase ______ mortality and are contraindicated in pts who are _______
Use caution in severe _____ disease
cardiovascular
allergic
hepatic
What is the main DDI to be concerned with when using Solfonylureas?
What does this drug do?
Aspirin
displaces sulfonylurea - resulting in hypoglycemia
Aspirin has 2 mechanisms to disrupt Sulfonylureas, what are they?
displace sulfonylurea - resulting in hypoglycemia
Inhibit prostaglandin E synth - PGE inhibits insulin secretion = too much secretion = hypoglycemia
What class of drugs is so well tolerated that it is regularly combined with other drugs?
What is the drug?
Biguanides
metformin (Glucophage)
metformin (Glucophage) has what 4 mechanisms?
Inhibit glc gut absorption
decrease hepatic glc production
increase insulin sensitivity at receptor
increase peripheral glc uptake/utilization
What drug is most effective at reducing glycemic level, creating fewer episodes of hypoglycemia, decreasing weight, reducing LDL, CV mortality, and Cancer?
metformin (Glucophage)
What occurs if there is renal impairment in pts taking metformin (Glucophage)
Who should not take this drug?
other side effect?
Lactic acidosis
Alcoholics (hepatic probs)
GI
acarbose (Precose) and miglitol (Glyset) are __________ enzyme inhibitors that normally degrade _____ in the gut
*this creates delay in blood glc concentrations after meal
Alpha-glucosidase
complex carbs
What class of drugs used to treat Type 2 diabets “resets” insulin receptors?
*improving target cell response/reducing insulin resistance
Thiazolidinediones
Name 2 Thiazolidinediones:
pioglitazone (Actos)
rosiglitazone (Avandia)
pioglitazone and rosiglitazone (thiazolidinediones) have been associated with more than 30 deaths due to _____, and there is an increased risk of _______
liver failure
heart failure
Thiazolidinediones like pioglitazone and rosiglitazone are contraindicates in what pts?
serious heart failure
they increase the risk
What class of drugs better regulates the release of insulin but are pro-inflammatory and may cause pancreatic cancer?
Incretins
Incretins mimic _______ to stimulate insulin release
hormones
What are 2 types of Incretin
GLP-1 (Glucagon Like Peptide -1) receptor agonists
DPP-4 (dipeptydyl peptidase-4) inhibitors
What is the normal blood sugar range?
What is fasting blood glc?
70-120 mg/dL
70-110 mg/dL
What is the gold standard in measuring blood glc (and monitoring diabetics)?
glycated hemoglobin (HbA1c)
What is the normal value for HbA1c?
What is the diabetic diagnosis?
What is the goal for diabetics?
less than 6%
above 6.5%
less than 7%
American College of Physicians 1st intervention for TypeII diabetes?
If fails, ________
If hyperglycemia persists, _______
lifestyle mods
metformin
more drugs
T/F
The endocrinologists algorithm suggests obesity management to lower glc and CV risk factor modification and glycemic controls
True
Natural estrogen is a steroid produced by the ovary, aka…
estradiol
Because estradiol is inactivated by the gut/liver, we must place a ______ group at C17 to make it orally active. This creates ______
ethinyl
ethinyl estradiol
Estrogen Replacement Drugs are of what 3 types?
Conjugated equine estrogens
Esterified estrogens
Estradiol preps
Conjugated equine estrogen:
This treats the ______ symptoms of menopause
It also might prevent _______
Premarin
vasomotor
bone loss (osteoporosis)
4 common side effects of Premarin:
Peripheral edema
Breast tenderness
Bloating
Headache
A serious side effect of Premarin if you have an intact uterus:
May also increase _____ cancer
Increased risk for endometrial (uterine) cancer)
breast
What are 2 Esterified Estrogens?
How are they different from Premarin (conjugated estrogen)?
Estratab
Menest
1/2 dose - 0.3mg daily
T/F Esterified Estrogens (Estratab, Menest) have the same effects as Premarin (conjugated estrogen)
True
Estrogen + progesterone =
adding progesterone does what?
Prempro
reduces risk of endometrial cancer
What is Prempro used for?
This is a combo of what 2 drugs?
menopause/osteoporosis
Premarin, Provera
*estrogen, medroxyprogesterone
In a large study (2800 w/ heart disease), women on HRT (estrogen) saw ____ go down and ______ go up with and no reduction is ______
cholesterol
blood clots
heart disease
Estrogen in combo with progestin may increase the risk of _________
*this outweighs long term use to prevent ________
stroke
osteoporosis
The PremPro study at the NIH was cancelled b/c it increased the risk of what 4 thing?
Heart disease
Stroke
Pulmonary embolism
Invasive breast cancer
What 2 benefits of PremPro aren’t enough to outweigh the risks of hear disease, stroke, pulmonary embolism, and breast cancer?
Reduced fractures
Reduced colorectal cancer
HRT (estrogen) is used on a ______ term basis to treat menopause, usually less than ____ years
short
5
Progesterone is a _____ produced by the _______.
It induces the secretory _______, affects uterine mobility, and cervical ______
steroid
corpus luteum
endometrium
mucous
Progesterone prevents the buildup of the ______
endometrial lining
Aside from contraception, Progesterone can be used to treat _______ and _______
endometriosis
menstrual disorders
Oral progesterone must be modified to be taken orally - what are 2 of them?
norethindrone (contraceptives)
medroxyprogesterone (Provera)
medroxyprogesterone (Provera) is used to treat what 3 things?
Abnormal uterine bleeding
secondary amenorrhea
endometrial cancer
Testosterone is a steroid that must be _____ before taken orally
methylated
Testosterone 4 Tx’s:
Delayed male puberty
Hypogonadism
Inoperable female breast cancer
Libido loss postmenopausal women
T/F
Male “menopause” beginning in 4th or 5th decades may be treated with testosterone, synthetic androgens, or estrogens
True
T/F - testosterone levels
250-800 mg/dl for men
15-40 ng/dl for women
0-20 ng/dl for postmenopausal women
True
Testosterone naturally diminished by 1% every year after ____, and common conditions observed are obesity, type 2 diabetes, _____, and ______
35
pain
depression
*these are just aging
Conditions that negatively impact T level are Metabolic syndrome, oteoporosis, COPD, Coronary heart disease, inflammatory conditions, cardiac, renal, and liver failure, and pituitary tumor
True
What syndrome entails both symptoms and biochemical evidence of T deficiency?
Hypogonadism
Testosterone is linked to the ______ of the male population and is a biomarker for occult diseases like atherosclerosis, _____, and early death
general health
cancer
Testosterone decreases fat, increases muscle, improves libido - and what 3 blood/diabetic/heart disease factors?
insulin resistance
Ha1C
lipid profiles
T/F
Exogenous testosterone can impair endogenous T, cause probs with fertility, increase the size of the prostate, and increase risk for blood clots
True
T can be administered many ways - including buccal which causes edema, irritation, and _____
dysgeusia
taste perversion
T/F
There is evidence that supports testosterone use for women
False
*no benefits as HRT
When can T be used for women?
postmenopausal hypoactive sexual desire
There are no FDA approved uses for Testosterone with women in the US, but in Europe there was a _____ that was withdrawn from the market in 2012 due to breast cancer concerns
patch
What can be given for moderate to severe vasomotor symptoms associated with menopause (when not improved by estrogens alone)
Estrogen + methyltestosterone
What has more anabolic effects and no androgenic effects?
Anabolic steroids
Anabolic steroids can increase muscle mass by ____%
30
Oral contraceptives contain both _____ and _______
Estrogen
Progestin
*99% effective
Oral contraceptives are usually taken days ____ through ____ of the menstrual cycle, the other 7 days a _____ is taken
5
25
placebo
Most contraceptive preparations are ______, but some are ________ (in case of Plan B, etc)
sequential
single entity
The morning after pill (Plan B) is _______ alone
Estrogen
What is used for rape/incest cases?
DES - diethyl stilbestrol
RU-486 is a progesterone ______ called mifepristone (Mifeprex) for the medical termination of pregnancy
antagonist