Endo/Repro - Pharmacology Flashcards

1
Q

Leuprolide is a(n) _______ _______.

A

Leuprolide is a GnRH agonist.

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2
Q

What is leuprolide used to treat?

A

Endometriosis;

fibroids

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3
Q

Clomipheme is a(n) _______ _______.

A

Clomipheme is an estrogen receptor antagonist (at the level of the hypothalamus, thus inhibiting subsequent release of GnRH).

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4
Q

True/False.

Clomiphene and leoprolide have opposite effects on GnRH effects.

A

True.

Leoprolide is an agonist.

Clomiphene is an antagonist.

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5
Q

What medication inactivates progesterone receptors, thus being useful in termination of intrauterine pregnancies?

A

Mifepristone

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6
Q

What enzyme(s) does methimazole inhibit?

A

Thyroid peroxidase

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7
Q

What enzyme(s) does propylthiouracil inhibit?

A

Thyroid peroxidase;

5’-deiodinase

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8
Q

What is metformin’s mechanism of action?

A

Inhibiting mitochondrial mGDP and activating AMPK

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9
Q

What are the main side effects of metformin use?

A

Lactic acidosis;

GI effects

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10
Q

What is the major contraindication for metformin use?

A

Renal insufficiency

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11
Q

What is the main purpose of estrogen in OCPs?

What is the main purpose of progesterone in OCPs?

A

Inhibit ovulation;

stop the formation of endometrial carcinoma

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12
Q

Why are sulfonamides and ceftriaxone associated with kernicterus?

A

They displace bilirubin from albumin

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13
Q

Pregnancy causes a(n) ________ in blood volume and a(n) ________ in renal clearance.

A

Pregnancy causes an increase** in blood volume and a **decrease in renal clearance.

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14
Q

What antibiotic is known for its deleterious side effects involving teeth and bones?

A

Tetracyclines

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15
Q

What antibiotic is contraindicated in those under 18 because of its deleterious side effects involving tendon development?

A

Fluoroquinolones

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16
Q

Increasing age (and associated changes in renal and hepatic clearance) has what effect on drug half-lives and toxicity incidence?

A

Decreased renal and hepatic clearance lead to longer half-lives and increased toxicity incidence

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17
Q

What selective estrogen receptor modulator acts at the hypothalamus to inhibit GnRH release?

A

Clomiphene

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18
Q

What selective estrogen receptor modulator acts as an antagonist at the breast and an agonist at the uterus and bone?

A

Tamoxifen

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19
Q

What selective estrogen receptor modulator acts as an antagonist at the breast and uterus and an agonist at bone?

A

Raloxifene

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20
Q

What patients should never be given estrogens?

A

Pregnant women (remember DES and vaginal clear cell carcinoma in the fetus);

women with a history of thromboembolic events;

smokers

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21
Q

True/False.

Low-dose progestins can be used to inhibit ovulation with a near-100% efficiency.

A

False.

Low-dose progestins can be used to inhibit ovulation with a 60 - 80% efficiency (they also thicken the cervical mucus).

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22
Q

What is the main selective estrogen receptor modulator used in treating osteoporosis?

A

Raloxifene

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23
Q

What antiprogestin medication can be used in termination of an intrauterine pregnancy?

A

Mifepristone (RU 486)

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24
Q

Most birth control implants release what hormone(s)?

A

Progestins only

(medroxyprogesterone, etonogestrel, etc.)

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25
Q

What two progestins are found in high-dose birth control implants?

A

Medroxyprogesterone;

etonogestrel

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26
Q

Which progestin is often found in low-dose birth control implants (mini-pills)?

A

Norethindrone

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27
Q

Which has a longer duration of action and fewer side effects, methimazole or propylthiouracil?

A

Methimazole

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28
Q

How does potassium iodide exert an effect in cases of hyperthyroidism?

A

Inhibition of thyroid hormone release

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29
Q

In what situation is propylthiouracil absolutely indicated?

A

Thyroid storm

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30
Q

What medication can be used to alter circadian rhythyms in diabetics and ‘jump-start’ the BMR and insulin sensitivity?

A

Bromocriptine

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31
Q

Metformin acts primarily on which organ(s) of the body?

A

The liver

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32
Q

Women need _______ doses of Zolpidem (Ambien) than men.

A

Women need lower doses of Zolpidem (Ambien) than men.

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33
Q

Drugs that affect QT interval length tend to have greater effects in women. Why?

A

Premenopausal women have a longer average QT interval than men

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34
Q

A greater percentage of neonatal body fluids is extracellular fluid, meaning drugs like the antibiotic __________ need to be dosed differently.

A

A greater percentage of neonatal body fluids is extracellular fluid, meaning drugs like the antibiotic aminoglycosides need to be dosed differently.

35
Q

Gray baby syndrome can occur in neonates treated with cloramphenicol because the _______ is still developing.

A

Gray baby syndrome can occur in neonates treated with cloramphenicol because the liver is still developing.

36
Q

The side effects of antimuscarinics are especially pronounced in what patient population?

A

Geriatric

37
Q

True/False.

As one gets older, creatinine clearance becomes less and less reliable in measuring renal clearance.

A

True.

38
Q

Mifeprostone is useful in terminating pregnancy in the first ____ days of gestation.

A

Mifeprostone is useful in terminating pregnancy in the first 70 days of gestation.

39
Q

Name some of the unwanted side effects of testosterone use.

A

Dyslipidemia;

aggression;

psychotic episodes;

liver damage;

priapism;

decreased sperm count

40
Q

What are the two main categories of insulins (based on length of effect)?

A

Prandial (Regular + the short-actings);

basal (NPH + the long-actings)

41
Q

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

A

Lispro < aspart < glulisine <<

regular (crystilline zinc) <<

NPH <<

detemir < glargine

42
Q

Name three short-acting insulins.

A

Lispro,

aspart

glulisine

43
Q

What are the two categories of diabetes medications known as secretogogues (because they increase insulin release)?

A

Sulfonylureas;

glinides

44
Q

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 _________.

A

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.

45
Q

_________ is a twice-daily basal insulin.

A

NPH is a twice-daily basal insulin.

46
Q

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.

A

True.

47
Q

Name an example ultra-long acting insulin (> 40 hours).

A

Degludec

48
Q

Name two hazards of insulin use.

A

Hypoglycemia;

also some risk of immunologic effects

49
Q

If morning fasting plasma glucose rates are high, increase the ________ (prandial/basal) insulin dose.

A

If morning fasting plasma glucose rates are high, increase the basal insulin dose.

50
Q

What is the risk of only relying on NPH for glucose control?

A

Nighttime hyperglycemia

51
Q

Which secretogogue category has weight gain and hypoglycemia as side effects?

A

Sulfonylureas

52
Q

Which of the two secretogogue categories less risk of side effects such as hypoglycemia?

A

Glinides

53
Q

Which diabetes medications act by inhibiting KATP channels (causing membrane depolarization and calcium influx) and causing increased insulin secretion?

A

(1) Glinides
(2) Sulfonylureas

54
Q

Are secretogogues used in type I DM, type II DM, or both?

A

Type II only

55
Q

Which allows for more fine-tuning of insulin release, sulfonylureas or glinides?

A

Glinides

(shorter duration of action = shorter duration of insulin spike = less risk of weight fain and hypoglycemia)

56
Q

Metformin should not be prescribed if eGFR is ______.

A

Metformin should not be prescribed if eGFR is < 30.

57
Q

Which diabetic medication shows some benefit in patients with CHF?

Which diabetic medication category is especially contraindicated in patients with CHF?

A

Metformin;

thiazolidinediones (glitazones)

58
Q

True/False.

Metformin is associated with weight gain.

A

False.

59
Q

What is the end effect of metformin on liver function?

A

Decreased gluconeogenesis

60
Q

Glitazones (thiazolidinediones) are insulin _________ that act via PPAR-gamma.

A

Glitazones (thiazolidinediones) are insulin sensitizers that act via PPAR-gamma.

61
Q

Thiazolidinediones (glitazones) are associated with weight _______ and fluid _______.

A

Thiazolidinediones (glitazones) are associated with weight gain and fluid retention.

62
Q

PPAR-gamma activation increases _________ expression.

A

PPAR-gamma activation increases GLUT4 expression.

63
Q

Which two diabetes medication classes are incretin modifiers?

A

GLP1 agonists;

DPP4 antagonists

64
Q

Pramlintide is a(n) ________ analog.

A

Pramlintide is an amylin analog.

65
Q

True/False.

Acarbose and miglitol are SGLT-2 inhibitors.

A

False.

Acarbose and miglitol are glucosidase inhibitors.

66
Q

True/False.

Insulin leves spike much more in response to oral glucose than to IV glucose.

A

True.

(The incretin effect)

67
Q

Name two incretins found in the body.

A

Glucose-like peptide 1 (GLP1);

glucose-dependent insulinotropic peptide (GIP)

68
Q

GLP-1 _________ insulin secretion.

GIP _________ insulin secretion.

A

GLP-1 increases insulin secretion (as well as blocking glucagon release).

GIP increases insulin secretion.

69
Q

What is the relationship between GLP-1 and DPP-4?

A

DPP-4 degrades GLP-1

(so one can either give resistant GLP-1 analogs or DPP-4 inhibitors to boost the incretin effect)

70
Q

Which diabetes medications can lead to appetite suppression and weight loss?

A

GLP-1 analogs (e.g. exanetide);

amylin analogs (e.g. pramlintide)

(Note: SGLT-2 inhibitors can also cause weight loss.)

71
Q

Pramlintide is used to directly decrease ________ levels, thus indirectly decreasing ________ levels.

A

Pramlintide is used to directly decrease glucagon levels, thus indirectly decreasing serum glucose levels.

72
Q

Besides suppressing appetite, GLP-1 analogs and pramlintide both slow what process?

A

Gastric emptying

73
Q

Which diabetic medication class has some associated risk for development of pancreatitis and/or C cell tumors?

A

GLP-1 analogs

74
Q

SGLT-2 inhibitors cause an increase in what?

A

Renal glucose excretion

75
Q

Where are the effects of SGLT-2 inhibitors mainly exerted in a diabetic patient?

A

The PCT

76
Q

SGLT-2 inhibitors are associated with what side effects?

A

Hypoglycemia;

UTIs

77
Q

Which diabetes medication class also reduces blood pressure?

A

SGLT-2 inhibitors

78
Q

Name the four major first steps in T2DM management (not necessarily concurrent).

A
  1. Weight loss
  2. Metformin
  3. Insulin
  4. Sulfonylureas
79
Q

True/False.

Insulin is associated with weight gain.

A

True.

80
Q

If a patient is allergic to penicillin, how are they treated for syphilis?

A

Tetracyclines

81
Q

If a pregnant patient is allergic to penicillin, how are they treated for syphilis?

A

Penicillin desensitization with subsequent administration of penicillin G

82
Q

How is isolated chlamydia treated?

How is isolated gonorrhea treated?

A

Azithromycin + doxycycline;

ceftriaxone

83
Q

A patient presents with a vaginal discharge and you suspect either chlamydial or gonorrheal infection.

What do you do?

A

Ceftriaxone + azithromycin

(two shots, one setting)

84
Q

A hypertensive diabetic might be well-served by what diabetic medication?

A

SLGT-2 inhibitors