Antihyperlipidemia/anxiolytic Flashcards
What is the mechanism of statins? what is its side effect?
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)
What are bile acid sequestrants? What are their side effects?
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
What is the mechanism of niacin? what are its side effects?
Inhibit VLDL synthesis—>decrease VLDL/LDL and increase HDL
Rashes (prostaglandin mediated)—>use aspirin to prevent it/hyperglycemia
What is the mechanism of fibrates? side effects?
Gemfibrozil/fenofibrate
Bind to PPAR—>increase LPL synthesis—>decrease VLDL/LDL/TG and increase HDL
Gallstone
Which anti lipid drug can be used against hyperTGs?
Fibrates
What is ezetimibe and how do we use it?
Inhibit enterocyte absorption of cholesterol—>decrease LDL
Use with statin
What is orlistat?
Used for weight loss
Inhibit the intestinal breakdown of TG—>cause steatorrhea and malabsorption of ADEK vitamin
What is the dose affect on the CNS from benzo and barb?
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
What neurotransmitter/drugs bind to GABAa complex?
GABA–>bind to alpha subunit
Benzo—>bind to gamma subunit
Barb—>bind to beta subunit
Alcohol binds somewhere
What ion channel is GABAa?
Stimulation—>chloride influx—>inhibitory
What is the mechanism of benzo?
Benzo potentiate GABA—->bind to GABAa—>increase frequency of Cl- channel opening
Will benzo has any affect without GABA presence?
No, it needs its best friend GABA
What receptors do benzo act via and what are the effects?
BZ1—>sedation
BZ2—>anti anxiety/cognitive impairment
What is the role of flumazenil and how does it work?
Treats benzo overdose—>bind to BZ1 and BZ2 receptors
Mechanism of barb?
Increase duration of Cl- channel opening
Which one has GABA mimetic activity, benzo or barb?
Barb at high dose—>cause coma and death
What are the short and long acting benzo and what are they used for?
Short—>midazolam—>IV anesthesia
Long—>Lorazepam—>anti anxiety/muscle relaxation/withdraw
What is benzo’s affect on sleeping stages?
Increase stage 2/decrease stage 3 and REM
What are the 3 benzo that are not metabolized in the liver and what are they used for?
Outside The Liver
Oxazepam/temazepam/lorazepam
Used for elderly or pt with liver dysfunction
What are the barbs? and which one is the classic CYP450 inducer?
Phenobarbitol/Thiopental
Penobarbitol is the classic inducer
What is barb contraindicated in?
Pt with porphyrias (it induces production of porphyrins)
Chronic use of benzo/barb/alcohol can lead to?
Cross tolerance
What are the withdraw signs of benzo/barb/alcohol?
Benzo (stimulatory)—>Insomnia/anxiety/seizures
Barb and alcohol—>delirium (delirium tremen for alcohol)/life threatening for barb
How to treat alcohol withdraw?
Lorazepam
What are the drug interaction of benzo/barb/alcohol that we should be cautious about?
Addictive affect combine with other CNS depressant (e.g. opioid, anesthetics) can cause life-threatening respiratory depression
What are the 3 BZ1 agonist drugs? what is the antidote for overdose of these drugs?
ZZZ (sleep)
Zolpidem/zaleplon/eszopiclone
less effect on sleep stages
Flumazenil
What is the mechanism of buspirone and what is it used for?
For anti anxiety without sedation
5-HT1a partial agonist
Takes 1-2 weeks to work
In general how do we treat acute and chronic anxiety?
Acute—>GABA—>use benzo
Chronic—>5HT—>use SSRI or buspirone
How do we treat sleep disorders?
Use melatonin—>Ramelteon
Use GABA agonist—>benzo and ZZZ drugs
