Endo/Repro - Pharmacology Flashcards
Leuprolide is a(n) _______ _______.
Leuprolide is a GnRH agonist.
What is leuprolide used to treat?
Endometriosis;
fibroids
Clomipheme is a(n) _______ _______.
Clomipheme is an estrogen receptor antagonist (at the level of the hypothalamus, thus inhibiting subsequent release of GnRH).
True/False.
Clomiphene and leoprolide have opposite effects on GnRH effects.
True.
Leoprolide is an agonist.
Clomiphene is an antagonist.
What medication inactivates progesterone receptors, thus being useful in termination of intrauterine pregnancies?
Mifepristone
What enzyme(s) does methimazole inhibit?
Thyroid peroxidase
What enzyme(s) does propylthiouracil inhibit?
Thyroid peroxidase;
5’-deiodinase
What is metformin’s mechanism of action?
Inhibiting mitochondrial mGDP and activating AMPK
What are the main side effects of metformin use?
Lactic acidosis;
GI effects
What is the major contraindication for metformin use?
Renal insufficiency
What is the main purpose of estrogen in OCPs?
What is the main purpose of progesterone in OCPs?
Inhibit ovulation;
stop the formation of endometrial carcinoma
Why are sulfonamides and ceftriaxone associated with kernicterus?
They displace bilirubin from albumin
Pregnancy causes a(n) ________ in blood volume and a(n) ________ in renal clearance.
Pregnancy causes an increase** in blood volume and a **decrease in renal clearance.
What antibiotic is known for its deleterious side effects involving teeth and bones?
Tetracyclines
What antibiotic is contraindicated in those under 18 because of its deleterious side effects involving tendon development?
Fluoroquinolones
Increasing age (and associated changes in renal and hepatic clearance) has what effect on drug half-lives and toxicity incidence?
Decreased renal and hepatic clearance lead to longer half-lives and increased toxicity incidence
What selective estrogen receptor modulator acts at the hypothalamus to inhibit GnRH release?
Clomiphene
What selective estrogen receptor modulator acts as an antagonist at the breast and an agonist at the uterus and bone?
Tamoxifen
What selective estrogen receptor modulator acts as an antagonist at the breast and uterus and an agonist at bone?
Raloxifene
What patients should never be given estrogens?
Pregnant women (remember DES and vaginal clear cell carcinoma in the fetus);
women with a history of thromboembolic events;
smokers
True/False.
Low-dose progestins can be used to inhibit ovulation with a near-100% efficiency.
False.
Low-dose progestins can be used to inhibit ovulation with a 60 - 80% efficiency (they also thicken the cervical mucus).
What is the main selective estrogen receptor modulator used in treating osteoporosis?
Raloxifene
What antiprogestin medication can be used in termination of an intrauterine pregnancy?
Mifepristone (RU 486)
Most birth control implants release what hormone(s)?
Progestins only
(medroxyprogesterone, etonogestrel, etc.)
What two progestins are found in high-dose birth control implants?
Medroxyprogesterone;
etonogestrel
Which progestin is often found in low-dose birth control implants (mini-pills)?
Norethindrone
Which has a longer duration of action and fewer side effects, methimazole or propylthiouracil?
Methimazole
How does potassium iodide exert an effect in cases of hyperthyroidism?
Inhibition of thyroid hormone release
In what situation is propylthiouracil absolutely indicated?
Thyroid storm
What medication can be used to alter circadian rhythyms in diabetics and ‘jump-start’ the BMR and insulin sensitivity?
Bromocriptine
Metformin acts primarily on which organ(s) of the body?
The liver
Women need _______ doses of Zolpidem (Ambien) than men.
Women need lower doses of Zolpidem (Ambien) than men.
Drugs that affect QT interval length tend to have greater effects in women. Why?
Premenopausal women have a longer average QT interval than men
A greater percentage of neonatal body fluids is extracellular fluid, meaning drugs like the antibiotic __________ need to be dosed differently.
A greater percentage of neonatal body fluids is extracellular fluid, meaning drugs like the antibiotic aminoglycosides need to be dosed differently.
Gray baby syndrome can occur in neonates treated with cloramphenicol because the _______ is still developing.
Gray baby syndrome can occur in neonates treated with cloramphenicol because the liver is still developing.
The side effects of antimuscarinics are especially pronounced in what patient population?
Geriatric
True/False.
As one gets older, creatinine clearance becomes less and less reliable in measuring renal clearance.
True.
Mifeprostone is useful in terminating pregnancy in the first ____ days of gestation.
Mifeprostone is useful in terminating pregnancy in the first 70 days of gestation.
Name some of the unwanted side effects of testosterone use.
Dyslipidemia;
aggression;
psychotic episodes;
liver damage;
priapism;
decreased sperm count
What are the two main categories of insulins (based on length of effect)?
Prandial (Regular + the short-actings);
basal (NPH + the long-actings)
Place these insulins in descending order by their length of duration of effect, from shortest to longest:
Aspart
Glargine
Regular (crystilline zinc)
Detemir
NPH
Lispro
Glulisine
Lispro < aspart < glulisine <<
regular (crystilline zinc) <<
NPH <<
detemir < glargine
Name three short-acting insulins.
Lispro,
aspart
glulisine
What are the two categories of diabetes medications known as secretogogues (because they increase insulin release)?
Sulfonylureas;
glinides
Lispro is insulin with a _________ and proline transposed.
Aspart is insulin with an _________ substituted for proline.
Glulisine is insulin with an _________ substituted for lysine.
NPH is insulin plus _________.
Lispro is insulin with a lysine and proline transposed.
Aspart is insulin with an aspartate substituted for proline.
Glulisine is insulin with an asparagine substituted for lysine.
NPH is insulin plus protamine.
_________ is a twice-daily basal insulin.
NPH is a twice-daily basal insulin.
True/False.
The effect of rapid-acting insulins typically last a few hours.
The effect of NPH typically lasts about 12 hours.
The effect of long-acting insulins lasts about 24 hours.
True.
Name an example ultra-long acting insulin (> 40 hours).
Degludec
Name two hazards of insulin use.
Hypoglycemia;
also some risk of immunologic effects
If morning fasting plasma glucose rates are high, increase the ________ (prandial/basal) insulin dose.
If morning fasting plasma glucose rates are high, increase the basal insulin dose.
What is the risk of only relying on NPH for glucose control?
Nighttime hyperglycemia
Which secretogogue category has weight gain and hypoglycemia as side effects?
Sulfonylureas
Which of the two secretogogue categories less risk of side effects such as hypoglycemia?
Glinides
Which diabetes medications act by inhibiting KATP channels (causing membrane depolarization and calcium influx) and causing increased insulin secretion?
(1) Glinides
(2) Sulfonylureas
Are secretogogues used in type I DM, type II DM, or both?
Type II only
Which allows for more fine-tuning of insulin release, sulfonylureas or glinides?
Glinides
(shorter duration of action = shorter duration of insulin spike = less risk of weight fain and hypoglycemia)
Metformin should not be prescribed if eGFR is ______.
Metformin should not be prescribed if eGFR is < 30.
Which diabetic medication shows some benefit in patients with CHF?
Which diabetic medication category is especially contraindicated in patients with CHF?
Metformin;
thiazolidinediones (glitazones)
True/False.
Metformin is associated with weight gain.
False.
What is the end effect of metformin on liver function?
Decreased gluconeogenesis
Glitazones (thiazolidinediones) are insulin _________ that act via PPAR-gamma.
Glitazones (thiazolidinediones) are insulin sensitizers that act via PPAR-gamma.
Thiazolidinediones (glitazones) are associated with weight _______ and fluid _______.
Thiazolidinediones (glitazones) are associated with weight gain and fluid retention.
PPAR-gamma activation increases _________ expression.
PPAR-gamma activation increases GLUT4 expression.
Which two diabetes medication classes are incretin modifiers?
GLP1 agonists;
DPP4 antagonists
Pramlintide is a(n) ________ analog.
Pramlintide is an amylin analog.
True/False.
Acarbose and miglitol are SGLT-2 inhibitors.
False.
Acarbose and miglitol are glucosidase inhibitors.
True/False.
Insulin leves spike much more in response to oral glucose than to IV glucose.
True.
(The incretin effect)
Name two incretins found in the body.
Glucose-like peptide 1 (GLP1);
glucose-dependent insulinotropic peptide (GIP)
GLP-1 _________ insulin secretion.
GIP _________ insulin secretion.
GLP-1 increases insulin secretion (as well as blocking glucagon release).
GIP increases insulin secretion.
What is the relationship between GLP-1 and DPP-4?
DPP-4 degrades GLP-1
(so one can either give resistant GLP-1 analogs or DPP-4 inhibitors to boost the incretin effect)
Which diabetes medications can lead to appetite suppression and weight loss?
GLP-1 analogs (e.g. exanetide);
amylin analogs (e.g. pramlintide)
(Note: SGLT-2 inhibitors can also cause weight loss.)
Pramlintide is used to directly decrease ________ levels, thus indirectly decreasing ________ levels.
Pramlintide is used to directly decrease glucagon levels, thus indirectly decreasing serum glucose levels.
Besides suppressing appetite, GLP-1 analogs and pramlintide both slow what process?
Gastric emptying
Which diabetic medication class has some associated risk for development of pancreatitis and/or C cell tumors?
GLP-1 analogs
SGLT-2 inhibitors cause an increase in what?
Renal glucose excretion
Where are the effects of SGLT-2 inhibitors mainly exerted in a diabetic patient?
The PCT
SGLT-2 inhibitors are associated with what side effects?
Hypoglycemia;
UTIs
Which diabetes medication class also reduces blood pressure?
SGLT-2 inhibitors
Name the four major first steps in T2DM management (not necessarily concurrent).
- Weight loss
- Metformin
- Insulin
- Sulfonylureas
True/False.
Insulin is associated with weight gain.
True.
If a patient is allergic to penicillin, how are they treated for syphilis?
Tetracyclines
If a pregnant patient is allergic to penicillin, how are they treated for syphilis?
Penicillin desensitization with subsequent administration of penicillin G
How is isolated chlamydia treated?
How is isolated gonorrhea treated?
Azithromycin + doxycycline;
ceftriaxone
A patient presents with a vaginal discharge and you suspect either chlamydial or gonorrheal infection.
What do you do?
Ceftriaxone + azithromycin
(two shots, one setting)
A hypertensive diabetic might be well-served by what diabetic medication?
SLGT-2 inhibitors
