Antihyperlipidemia/anxiolytic Flashcards

1
Q

What is the mechanism of statins? what is its side effect?

A

Inhibit HMG-CoA reductase—>decrease liver cholesterol—>increase LDL receptor expression on liver cells—>take in LDL from plasma—>decrease serum LDL level
Myalgia—>rhadomyolysis (combine with gemfibrozil—>increase risk)

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2
Q

What are bile acid sequestrants? What are their side effects?

A

Cholestyramine/colestipol
Bind to bile salt—>prevent reabsorption (recycling)—>increase new bile salt production—>pull LDL out of the blood
They increase serum TGs/malabsorption of ADEK vitamins

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3
Q

What is the mechanism of niacin? what are its side effects?

A

Inhibit VLDL synthesis—>decrease VLDL/LDL and increase HDL

Rashes (prostaglandin mediated)—>use aspirin to prevent it/hyperglycemia

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4
Q

What is the mechanism of fibrates? side effects?

A

Gemfibrozil/fenofibrate
Bind to PPAR—>increase LPL synthesis—>decrease VLDL/LDL/TG and increase HDL
Gallstone

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5
Q

Which anti lipid drug can be used against hyperTGs?

A

Fibrates

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6
Q

What is ezetimibe and how do we use it?

A

Inhibit enterocyte absorption of cholesterol—>decrease LDL

Use with statin

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7
Q

What is orlistat?

A

Used for weight loss

Inhibit the intestinal breakdown of TG—>cause steatorrhea and malabsorption of ADEK vitamin

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8
Q

What is the dose affect on the CNS from benzo and barb?

A

Low dose—>both cause sedation/anti anxiety—>a little higher dose—>hypnosis (sleeping)—>higher dose—>anesthesia—>higher dose—>medullary depression—>benzo affect flats out—>higher dose—>barb causes coma or death

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9
Q

What neurotransmitter/drugs bind to GABAa complex?

A

GABA–>bind to alpha subunit
Benzo—>bind to gamma subunit
Barb—>bind to beta subunit
Alcohol binds somewhere

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10
Q

What ion channel is GABAa?

A

Stimulation—>chloride influx—>inhibitory

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11
Q

What is the mechanism of benzo?

A

Benzo potentiate GABA—->bind to GABAa—>increase frequency of Cl- channel opening

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12
Q

Will benzo has any affect without GABA presence?

A

No, it needs its best friend GABA

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13
Q

What receptors do benzo act via and what are the effects?

A

BZ1—>sedation

BZ2—>anti anxiety/cognitive impairment

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14
Q

What is the role of flumazenil and how does it work?

A

Treats benzo overdose—>bind to BZ1 and BZ2 receptors

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15
Q

Mechanism of barb?

A

Increase duration of Cl- channel opening

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16
Q

Which one has GABA mimetic activity, benzo or barb?

A

Barb at high dose—>cause coma and death

17
Q

What are the short and long acting benzo and what are they used for?

A

Short—>midazolam—>IV anesthesia

Long—>Lorazepam—>anti anxiety/muscle relaxation/withdraw

18
Q

What is benzo’s affect on sleeping stages?

A

Increase stage 2/decrease stage 3 and REM

19
Q

What are the 3 benzo that are not metabolized in the liver and what are they used for?

A

Outside The Liver
Oxazepam/temazepam/lorazepam
Used for elderly or pt with liver dysfunction

20
Q

What are the barbs? and which one is the classic CYP450 inducer?

A

Phenobarbitol/Thiopental

Penobarbitol is the classic inducer

21
Q

What is barb contraindicated in?

A

Pt with porphyrias (it induces production of porphyrins)

22
Q

Chronic use of benzo/barb/alcohol can lead to?

A

Cross tolerance

23
Q

What are the withdraw signs of benzo/barb/alcohol?

A

Benzo (stimulatory)—>Insomnia/anxiety/seizures

Barb and alcohol—>delirium (delirium tremen for alcohol)/life threatening for barb

24
Q

How to treat alcohol withdraw?

A

Lorazepam

25
Q

What are the drug interaction of benzo/barb/alcohol that we should be cautious about?

A

Addictive affect combine with other CNS depressant (e.g. opioid, anesthetics) can cause life-threatening respiratory depression

26
Q

What are the 3 BZ1 agonist drugs? what is the antidote for overdose of these drugs?

A

ZZZ (sleep)
Zolpidem/zaleplon/eszopiclone
less effect on sleep stages
Flumazenil

27
Q

What is the mechanism of buspirone and what is it used for?

A

For anti anxiety without sedation
5-HT1a partial agonist
Takes 1-2 weeks to work

28
Q

In general how do we treat acute and chronic anxiety?

A

Acute—>GABA—>use benzo

Chronic—>5HT—>use SSRI or buspirone

29
Q

How do we treat sleep disorders?

A

Use melatonin—>Ramelteon

Use GABA agonist—>benzo and ZZZ drugs