Lipid and GI Drugs - GI Exam 2 Flashcards

1
Q

The (drug class and examples), are HMG-CoA Reductase inhibitors.

A

The statins, Lovastatin and Atorvastatin, are HMG-CoA Reductase inhibitors.

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2
Q

Statins reduce ______ by inhibiting HMG-CoA Reductase. The have marked ____ and they are the best drug to reduce ___

A

Statins reduce endogenous cholesterol synthesis by inhibiting HMG-CoA Reductase. The have marked first-pass hepatic extraction and they are the best drug to reduce LDL

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3
Q

Statins reduce ___ & ___, increase ___ and ___. Can be used to treat _____ & _____. First line treatment after ____.

A

Statins reduce VLDL & LDL, increase LDL receptor expression and HDL. Can be used to treat hypercholesterolemia and mixed lipidemia. First line treatment after an MI

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4
Q

Side effects of statins include

  1. ???
  2. congnitive effects like confusion and memory loss
  3. ???
  4. myalgia/myositis. Check creatine kinase if symptomatic. D/c if rhabdo, myoglobinuria
A

Side effects of statins include

  1. diabetes
  2. congnitive effects like confusion and memory loss
  3. hepatitis due to increased hepatic enzymes
  4. myalgia/myositis. Check creatine kinase if symptomatic. D/c if rhabdo, myoglobinuria
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5
Q

Side effects of statins include

  1. diabetes
  2. ???
  3. hepatitis due to increased hepatic enzymes
  4. ???
A

Side effects of statins include

  1. diabetes
  2. congnitive effects like confusion and memory loss
  3. hepatitis due to increased hepatic enzymes
  4. myalgia/myositis. Check creatine kinase if symptomatic. D/c if rhabdo, myoglobinuria
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6
Q

Niacin MOA

  1. Reduces ___ synthesis in liver –> decreased ___
  2. Reduces ___ in adipose –> decreased ___ recylcling –> decreased ___ synthesis –> decreased ___
  3. Increases ___ activity –> increases ___ clearance
  4. Decreased ___ catabolism –> increased serum ___

**useful in mixed hyperlipidemia because of effects on VLDL, LDL, HDL**

A

Niacin MOA

  1. Reduces VLDL synthesis in liver –> decreased LDL
  2. Reduces lipolysis in adipose –> decreased FFA recylcling –> decreased VLDL synthesis –> decreased LDL
  3. Increases LPL activity –> increases VLDL clearance
  4. Decreased HDL catabolism –> increased serum HDL

**useful in mixed hyperlipidemia because of effects on VLDL, LDL, HDL**

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7
Q

____ has to be used in conjunction with other drugs for hypercholesterolemia/hypertriglyceridemia. If you give a dose high enough to be effective alone, it causes vasodilation, skin flushing, and pruritis mediated by prostaglandins. Aspirin helps with this side effect and flushing discontinues within a few days of treatment.

A

Niacin has to be used in conjunction with other drugs for hypercholesterolemia/hypertriglyceridemia. If you give a dose high enough to be effective alone, it causes vasodilation, skin flushing, and pruritis mediated by prostaglandins. Aspirin helps with this side effect and flushing discontinues within a few days of treatment.

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8
Q

Niacin has to be used in conjunction with other drugs for hypercholesterolemia/hypertriglyceridemia. If you give a dose high enough to be effective alone, it causes (3 SE) mediated by ______. (drug) helps with this side effect and (SE) discontinues within a few days of treatment.

A

Niacin has to be used in conjunction with other drugs for hypercholesterolemia/hypertriglyceridemia. If you give a dose high enough to be effective alone, it causes vasodilation, skin flushing, and pruritis mediated by prostaglandins. Aspirin helps with this side effect and flushing discontinues within a few days of treatment.

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9
Q

Niacin can cause _____. In diabetic patients, you might want to adjust ______ medications

A

Niacin can cause glucose intolerance. In diabetic patients, you might want to adjust glucose-lowering medications

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10
Q

____ can cause glucose intolerance. In diabetic patients, you might want to adjust glucose-lowering medications

A

Niacin can cause glucose intolerance. In diabetic patients, you might want to adjust glucose-lowering medications

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11
Q

Side effects of Niacin:

A. ??

B. ??

C. ??

D. ??

E. ??

Use with caution in patients with gout, diabetes, liver disease, and peptic ulcer dz

A

Side effects of Niacin:

A. flushing/pruritis

B. increased AST, ALT

C. glucose intolerance

D. hyperuricemia

E. gastric distress

Use with caution in patients with gout, diabetes, liver disease, and peptic ulcer dz

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12
Q

The drugs Gemfibrozil and Fenofibrate are _______. They decrease _________ and so are indicated in _______. Can also be used in _______ _______.

A

The drugs Gemfibrozil and Fenofibrate are fibric acid derivatives. They decreased triglycerides so are indicated in hypertriglyceridemia. Can also be used in mixed hyperlipidemia.

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13
Q

Fibric Acid Derivatives MOA

  • Promote (enzyme) –> decrease ____ –> ___ to tissues
  • Decrease ____ synthesis
  • variable effects on ___, maybe increases ___
A

Fibric Acid Derivatives MOA

  • Promote LPL –> decrease VLDL –> FFA to tissues
  • Decrease VLDL synthesis
  • variable effects on LDL, maybe increases HDL
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14
Q

Side Effect of Fibric Acid Derivatives:

Myalgias, risk increases with coadministration of statin

???

blood cell deficiency

???

increased AST, ALT

???

contraindiacted in hepatic and renal dysfunction

A

Side Effect of Fibric Acid Derivatives:

Myalgias, risk increases with coadministration of statin

Allergice rxn

blood cell deficiency

hypokalemia

increased AST, ALT

moderate risk of gallstones

contraindiacted in hepatic and renal dysfunction

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15
Q

Side Effect of Fibric Acid Derivatives:

???

Allergice rxn

???

hypokalemia

???

moderate risk of gallstones

???

A

Side Effect of Fibric Acid Derivatives:

Myalgias, risk increases with coadministration of statin

Allergice rxn

blood cell deficiency

hypokalemia

increased AST, ALT

moderate risk of gallstones

contraindiacted in hepatic and renal dysfunction

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16
Q

Cholestipol and Cholestyramine are (drug class). They are only moderately effective for _____.

A

Cholestipol and Cholestyramine are bile acid binding agents. They are only moderately effective for hypercholesterolemia.

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17
Q

bile acid binding agents MOA

bind bile acid –> bile acid can’t recycle –> liver makes new bile acid with cholesterol –> liver increases _____ to make more cholesterol –> less LDL in blood

A

bile acid binding agents MOA

bind bile acid –> bile acid can’t recycle –> liver makes new bile acid with cholesterol –> liver increases LDL receptor to make more cholesterol –> less LDL in blood

18
Q

bile acid binding agents may increase _____.

A

bile acid binding agents may increase triglycerides.

Maybe because increase LDL takeup in liver?? recycled to VLDL?

19
Q

side effects of bile acid binding drugs:

  • ??
  • unpalatable taste
  • ??
  • interfere with digoxin, HCTZ, and warfarin
A

side effects of bile acid binding drugs:

  • annoying GI effects (nausea, bloating, constipation)
  • unpalatable taste
  • interefere with fat soluble vitamin absorption
  • interfere with digoxin, HCTZ, and warfarin
20
Q

side effects of bile acid binding drugs:

annoying GI effects (nausea, bloating, constipation)

??

interefere with fat soluble vitamin absorption

??

A

side effects of bile acid binding drugs:

annoying GI effects (nausea, bloating, constipation)

unpalatable taste

interefere with fat soluble vitamin absorption

interfere with digoxin, HCTZ, and warfarin

21
Q

Bile acid binding drugs are used in patients who _____ or as an add-on. They have __ _____ _____ effects.

A

Bile acid binding drugs are used in patients who can’t tolerate other drugs or as an add-on. They have no systemic adverse effects.

22
Q

Ezetimibe inhibits intestinal absorption of ____ and _____. The body responds by upregulating the _____ enhancing ___ plasma clearance. It has a low incidence of toxicity.

A

Ezetimibe inhibits intestinal absorption of phytosterols and cholesterol (endogenous and exogenous). The body responds by upregulating the LDL receptor enhancing LDL plasma clearance. It has a low incidence of toxicity.

It increases cholesterol production, but the drug just keeps binding it. ta-da!

23
Q

If your patient’s LDL doesn’t come down with one drug, try multidrug therapy. Specifically, (3 drugs).

Statins + (drug class) are more effective together than statins + (drug).

A

If your patient’s LDL doesn’t come down with one drug, try multidrug therapy. Specifically, a statin, a bile acid binding resin, and niacin.

Statins + bile acid binding resin are more effective together than statins + niacin.

24
Q

Similar MOAs

____ = HMG-CoA Reductase inhibitor

____ and ____: upregulate LPL

_____ and _____: bind stuff in gut lumen to make liver take up more LDL for cholesterol synthesis

A

Similar MOAs

statins = HMG-CoA Reductase inhibitor

fibric acid derivatives and niacin: upregulate LPL

bile acid binding resins and ezetimibe: bind stuff in gut lumen to make liver take up more LDL for cholesterol synthesis

25
Q

_____ combines a statin to reduce cholesterol synthesis and Ezetimibe to reduce cholesterol absorption ergo serum LDL. The drug has not been shown to be any more effective at reducing heart attack risk than a statin alone

A

Vytorin combines a statin to reduce cholesterol synthesis and Ezetimibe to reduce cholesterol absorption ergo serum LDL. The drug has not been shown to be any more effective at reducing heart attack risk than a statin alone

26
Q

___ is made of omega 3-fatty acids. It reduces synthesis of triglycerides in the liver. It can increase LDL in some patients, so check that lab. Most common side effects are flu sx, infections, upset stomach, change in the sene of taste.

A

Lovaza is made of omega 3-fatty acids. It reduces synthesis of triglycerides in the liver. It can increase LDL in some patients, so check that lab. Most common side effects are flu sx, infections, upset stomach, change in the sene of taste.

27
Q

Lovaza is made of ____. It reduces synthesis of _____ in the liver. It can increase ___ in some patients, so check that lab. Most common side effects are (4 things).

A

Lovaza is made of omega 3-fatty acids. It reduces synthesis of triglycerides in the liver. It can increase LDL in some patients, so check that lab. Most common side effects are flu sx, infections, upset stomach, change in the sene of taste.

28
Q

_____ inhibits PSCK9 thus increasing LDL receptor levels. There are few side effects, but they may include injection site reaction, nasopharyngitis, flu sx

A

Alirocumab inhibits PSCK9 thus increasing LDL receptor levels. There are few side effects, but they may include injection site reaction, nasopharyngitis, flu sx

29
Q

Alirocumab inhibits _____ thus increasing LDL receptor levels. There are few side effects, but they may include (3 things)

A

Alirocumab inhibits PSCK9 thus increasing LDL receptor levels. There are few side effects, but they may include injection site reaction, nasopharyngitis, flu sx

30
Q

Drugs used to treat peptic ulcer and GERD

  1. Proton Pump Inhibitors
  2. Histamine H2 receptor antagonists
  3. Antacids
  4. ?????
  5. Antibiotics (for eradicating H. pylori)
A

Drugs used to treat peptic ulcer and GERD

  1. Proton Pump Inhibitors
  2. Histamine H2 receptor antagonists
  3. Antacids
  4. Mucosal protective agents
  5. Antibiotics (for eradicating H. pylori)
31
Q

_______ and _______ are Dopamine D2 receptor antagonists

A

Metoclopramide and Domperidone are Dopamine D2 receptor antagonists

32
Q

Metoclopramide and Domperidone are (class)

A

Metoclopramide and Domperidone are Dopamine D2 receptor antagonists

33
Q

Metoclopramide…

  • causes the release of _____ in myenteric plexus
  • enhances tone and motility in the ____ GI tract
  • stimulates gastric motility (prokinetic) without increasing ____
A

Metoclopramide…

  • causes the release of acetylcholine from cholinergi neurons in myenteric plexus
  • enhances tone and motility in the upper GI tract
  • stimulates gastric motility (prokinetic) without increasing acid secretion
34
Q

Metaclopramide crosses the _____, so it has ___ effects. For this reason, it can be use as an _____ in patients receiving chemotherapy. However, it is contraindicated in patients with a _____ disorder or with _____. It can also cause _____ effects (think _____)

A

Metaclopramide crosses the blood brain barrier. It has CNS effects. For this reason, it can be use as an antiemetic in patients receiving chemotherapy. However, it is contraindicated in patients with a seizure disorder or with mechanical obstruction of the GI tract. It can also cause extrapyramidal effects (think Parkinsonism)

35
Q

Metoclopramide can be used to treat (4 upper GI issues).

A

Metoclopramide can be used to treat GERD, gastroparesis, reflux esophagitis, and intractable hiccups.

36
Q

Unlike Metoclopramide, _____ does not cross the blood brain barrier and so does not have extrapyramidal effects

A

Unlike Metoclopramide, Domperidone does not cross the blood brain barrier and so does not have extrapyramidal effects

37
Q

Errythromycin acts on the _______ to increase gastric motility. It can be used to treat ___or in patients with upper GI bleed ____.

A

Errythromycin acts on the motilin receptor to increase gastric motility. It can be used to treat gastroparesis or in patients with upper GI bleed prior to endoscopy.

38
Q

_______ acts on the motilin receptor to increase gastric motility. It can be used to treat gastroparesis or in patients with upper GI bleed prior to endoscopy.

A

Erythromycin acts on the motilin receptor to increase gastric motility. It can be used to treat gastroparesis or in patients with upper GI bleed prior to endoscopy.

39
Q

Bethanecol

  • stimulates ______ to increase gastric motility and tone.
  • also used as a drug for _____
  • increases _____ pressure and evokes _____contractions
  • side effects include ????? - the parasympathetic nervous system’s greatest hits.
A

Bethanecol

  • stimulates parasympathetic nervous system to increase gastric motility and tone.
  • also used as a drug for urinary retention (muscarinic receptor agonist).
  • increases lower esophageal sphincter pressure and evokes fundoantral contractions
  • side effects include dizziness, nausea, diarrhea, sweating, urinary urgency, salivation, and lacrimation - the parasympathetic nervous system’s greatest hits.
40
Q

Gastroparesis is treated with 3 different drug families

  1. ???
  2. ???
  3. ???
A

Gastroparesis is treated with 3 different drug families

  1. prokinetics
  2. PPI/H2receptor antagonists to alleviate sx from acid production
  3. anti-emetics