Endo/Repro - Pharmacology Flashcards by Jason Worley

Leuprolide is a(n) _______ _______.

Leuprolide is a GnRH agonist.

How well did you know this?

Not at all

Perfectly

What is leuprolide used to treat?

Endometriosis;

fibroids

How well did you know this?

Not at all

Perfectly

Clomipheme is a(n) _______ _______.

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

How well did you know this?

Not at all

Perfectly

True/False.

Clomiphene and leoprolide have opposite effects on GnRH effects.

True.

Leoprolide is an agonist.

Clomiphene is an antagonist.

How well did you know this?

Not at all

Perfectly

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

Mifepristone

How well did you know this?

Not at all

Perfectly

What enzyme(s) does methimazole inhibit?

Thyroid peroxidase

How well did you know this?

Not at all

Perfectly

What enzyme(s) does propylthiouracil inhibit?

Thyroid peroxidase;

5’-deiodinase

How well did you know this?

Not at all

Perfectly

What is metformin’s mechanism of action?

Inhibiting mitochondrial mGDP and activating AMPK

How well did you know this?

Not at all

Perfectly

What are the main side effects of metformin use?

Lactic acidosis;

GI effects

How well did you know this?

Not at all

Perfectly

What is the major contraindication for metformin use?

Renal insufficiency

How well did you know this?

Not at all

Perfectly

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

How well did you know this?

Not at all

Perfectly

Why are sulfonamides and ceftriaxone associated with kernicterus?

They displace bilirubin from albumin

How well did you know this?

Not at all

Perfectly

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.

How well did you know this?

Not at all

Perfectly

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

Tetracyclines

How well did you know this?

Not at all

Perfectly

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

Fluoroquinolones

How well did you know this?

Not at all

Perfectly

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

How well did you know this?

Not at all

Perfectly

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

Clomiphene

How well did you know this?

Not at all

Perfectly

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

Tamoxifen

How well did you know this?

Not at all

Perfectly

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

Raloxifene

How well did you know this?

Not at all

Perfectly

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

How well did you know this?

Not at all

Perfectly

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).

How well did you know this?

Not at all

Perfectly

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

Raloxifene

How well did you know this?

Not at all

Perfectly

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

Mifepristone (RU 486)

How well did you know this?

Not at all

Perfectly

Most birth control implants release what hormone(s)?

Progestins only

(medroxyprogesterone, etonogestrel, etc.)

How well did you know this?

Not at all

Perfectly

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 K_ATP 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).

1. Weight loss 2. Metformin 3. Insulin 4. 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