Exam 3 Drugs

Question 1

Omega 3 fatty acids (fish oil/ linolenic)

Answer 1

improve the ratio of LDL-C to HDL-C
Reverse angiographic evidence of coronary atherosclerosis
Reduce mortality rate in patients with CHD
Lower triglyceride levels

Question 2

Epanova (omega 3 carboxylic acid)

Answer 2

Eicosapentaenoic acid and Docosoahexanenoic acid: poor substrates for the enzymes responsible for the synthesis of triglycerides in the liver

Question 3

Statins

Answer 3

Treats hypercholesterolemia
Active compound
Low bioavailability (extensive first pass metabolism)
Related to HMG-CoA and HMG-CoA reductase
HMG-CoA reductase is the rate limiting enzyme.
Statins reduce hepatic cholesterol biosynthesis and the amount of cholesterol available for incorporation into VLDL by inhibiting HMG-CoA reductase
Increases # of hepatic LDL receptors = Increases hepatic uptake of LDL-C
Decrease LDL-C levels
HDL-C levels are increased
Reduce serum triglycerides (don’t usually treat hyperglyceridemia)
Adverse effect: rhabdomyolysi, myopathy, myalgia

Question 4

Lovastatin

Answer 4

Inactive prodrug that must be converted to active metabolites in the liver
Block HMG-CoA reductase needed for cholesterol synthesis

Question 5

Simvastatin

Answer 5

Inactive prodrug that must be converted to active metabolites in the liver
Block HMG-CoA reductase needed for cholesterol synthesis

Question 6

Rosuvastatin

Answer 6

Greatest effect on triglyceride levels

Treats mixed hyperlipidemia

Question 7

Atorvastatin

Answer 7

Greatest effect on triglyceride levels

Treats mixed hyperlipidemia

Question 8

Cholestyramine

Answer 8

Bile acid binding resin (high molecular weight polymers)
Drug for hypercholesterolemia
Chloride ion that can be exchanged for bile acids in the gut
Not absorbed in the gut
Excreted in feces
Prevents the enteroheptic cycling of bile acids
Resins bind to bile acids = synthesizes replacement of bile acids from cholesterol
Liver increases # of LDL receptors = LDL-C reduced as more cholesterol is delivered to the liver
Can bind to digoxin, thyroxin, warfarin, etc

Question 9

Colestipol

Answer 9

Bile acid binding resin (high molecular weight polymers)
Drug for hypercholesterolemia
Chloride ion that can be exchanged for bile acids in the gut
Not absorbed in gut
Excreted in feces
Prevents the enteroheptic cycling of bile acids
Resins bind to bile acids = synthesizes replacement of bile acids from cholesterol
Liver increases # of LDL receptors = LDL-C reduced as more cholesterol is delivered to the liver
Can bind to digoxin, thyroxin, warfarin, etc.

Question 10

Colesevelam

Answer 10

Bile acid binding resin (high molecular weight polymers)
Drug for hypercholesterolemia
Chloride ion that can be exchanged for bile acids in the gut
Not absorbed in gut
Excreted in feces
Prevents the enteroheptic cycling of bile acids
Resins bind to bile acids = synthesizes replacement of bile acids from cholesterol
Liver increases # of LDL receptors = LDL-C reduced as more cholesterol is delivered to the liver

Question 11

Ezetimibe

Answer 11

Treats hyperlipidemia
Inhibits the absorption of dietary cholesterol
Absorbed in the intestines
Metabolized to the active metabolite ezetimibe- glucuronide
Active metabolite distributed by circulation of the small intestines
Localized in the bush border
Inhibits absorption of both biliary and dietary cholesterol
Half live 22 hrs
Can be used in a combination of other statins
MofA involves sterol transporter Niemann Pick C1 L1!!!!
Does not affect absorption of fat soluble nutrients (fat soluble vitamins, triglycerides, bile acid)
Interferes with the uptake of cholesterol and phytosterols
Reduces delivery of intestinal cholesterol to the liver

Question 12

Anesthesia

Answer 12

loss of all sensation

Question 13

Analgesia

Answer 13

loss of pain sensation

Question 14

Epinephrine in anesthetics

Answer 14

Produces vasoconstriction
Slows rate of absorption
Not used to anesthetize tissues with end arteries (fingers, toes, etc)

Question 15

Ester type anesthetics

Answer 15

Procaine
Benzocaine
Cocaine
Metabolized in the plasma by butyrylcholinesterases to PABA derivatives
Cause hypersensitivity more than do amide type

Question 16

Amide type anesthetics

Answer 16

Lidocaine
Bupivacaine
Prilocaine
Undergo metabolism by hepatic P450 enzymes to yield polar metabolites
Excreted in urine

Question 17

Mechanism of action for anesthetics

Answer 17

Cause a reversible inhibition of action potential conduction by binding to the SODIUM CHANNEL/ decreases the nerve membrane permeability to sodium
Nonpolar/ lipophilic form passes through the neuronal membrane switches to the polar/hydrophilic form in the cytoplasm of the neuron
Cationic form bind to cytoplasmic side of the sodium channel protein = prolongs INACTIVATION state of the sodium channel (action potential can’t propagate along neuronal fiber/ sensory input lost)
Nonionized to ionized form
Open sodium channel

Question 18

Use dependent blockade

Answer 18

Selective inhibition of nerve fibers

Question 19

Size dependent blockade

Answer 19

Small diameter fibers are blocked more easily

Ex: unmyelinated C and lightly myelinated Aō pain fibers

Question 20

Anesthetics

Answer 20

Cause hypotension, cardiac depression, vasodilators, block vasoconstriction
Antiarrhythmic activity
Allergic reactions are common!
Ester type anesthetics = Hypersensitivity reactions bc metabolized to PABA

Question 21

Chloroprocaine

Answer 21

Amide type anesthesics
Not associated with allergic rxn
Longer duration of action

Question 22

Lidocaine

Answer 22

Amide type anesthesics
Not associated with allergic rxn
Longer duration of action
Infiltration anesthesia
Injected directly into subcutaneous tissue under the skin
For dermal procedures/ minor surgical procedures

Question 23

Procaine

Answer 23

Topical anesthesia
Used to treat pruritus (itching)
Can relieve pain caused by oral teething, nasal, laryngeal, or rectal disorders or surgery
Ester type anesthetics

Question 24

Benzocaine

Answer 24

Topical anesthesia
Used to treat pruritus (itching)
Can relieve pain caused by oral teething, nasal, laryngeal, or rectal disorders or surgery
Ester type anesthetics

Question 25

Articaine

Answer 25

Infiltration anesthesia
Injected directly into subcutaneous tissue under the skin
For dermal procedures/ minor surgical procedures
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Question 26

Ropivacaine

Answer 26

Nerve block and field block anesthesia (regional anesthesia)

Goal: block conductivity of sensory nerves from that area

Question 27

Bupivacaine

Answer 27

Spinal intrathecal anesthesia
Epidural anesthesia (can cause cardiac depression/ neurotoxicity in labor mothers)
Used to block somatosensory and motor fibers during procedures (lower limb/ pelvic structure)
Injected into the subarachnoid/ intrathecal space

Question 28

Levobupivacaine

Answer 28

Spinal intrathecal anesthesia
Used to block somatosensory and motor fibers during procedures (lower limb/ pelvic structure)
Injected into the subarachnoid/ intrathecal space
Used as epidural anesthesia for labor

Question 29

Diethyl ether

Answer 29

General anesthetics
Limb amputations
Slow rate of induction
Highly flammable

Question 30

Chloroform

Answer 30

General anesthetics

Question 31

Minimal alveolar concentration (MAC)

Answer 31

the potency of inhalational anesthetics

Inspired concentration of the anesthetic required to produce anesthesia