Exam 3 Drugs Flashcards
Omega 3 fatty acids (fish oil/ linolenic)
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
Epanova (omega 3 carboxylic acid)
Eicosapentaenoic acid and Docosoahexanenoic acid: poor substrates for the enzymes responsible for the synthesis of triglycerides in the liver
Statins
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
Lovastatin
Inactive prodrug that must be converted to active metabolites in the liver
Block HMG-CoA reductase needed for cholesterol synthesis
Simvastatin
Inactive prodrug that must be converted to active metabolites in the liver
Block HMG-CoA reductase needed for cholesterol synthesis
Rosuvastatin
Greatest effect on triglyceride levels
Treats mixed hyperlipidemia
Atorvastatin
Greatest effect on triglyceride levels
Treats mixed hyperlipidemia
Cholestyramine
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
Colestipol
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.
Colesevelam
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
Ezetimibe
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
Anesthesia
loss of all sensation
Analgesia
loss of pain sensation
Epinephrine in anesthetics
Produces vasoconstriction
Slows rate of absorption
Not used to anesthetize tissues with end arteries (fingers, toes, etc)
Ester type anesthetics
Procaine
Benzocaine
Cocaine
Metabolized in the plasma by butyrylcholinesterases to PABA derivatives
Cause hypersensitivity more than do amide type
Amide type anesthetics
Lidocaine Bupivacaine Prilocaine Undergo metabolism by hepatic P450 enzymes to yield polar metabolites Excreted in urine
Mechanism of action for anesthetics
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
Use dependent blockade
Selective inhibition of nerve fibers
Size dependent blockade
Small diameter fibers are blocked more easily
Ex: unmyelinated C and lightly myelinated Aō pain fibers
Anesthetics
Cause hypotension, cardiac depression, vasodilators, block vasoconstriction
Antiarrhythmic activity
Allergic reactions are common!
Ester type anesthetics = Hypersensitivity reactions bc metabolized to PABA
Chloroprocaine
Amide type anesthesics
Not associated with allergic rxn
Longer duration of action
Lidocaine
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
Procaine
Topical anesthesia
Used to treat pruritus (itching)
Can relieve pain caused by oral teething, nasal, laryngeal, or rectal disorders or surgery
Ester type anesthetics
Benzocaine
Topical anesthesia
Used to treat pruritus (itching)
Can relieve pain caused by oral teething, nasal, laryngeal, or rectal disorders or surgery
Ester type anesthetics
Articaine
Infiltration anesthesia
Injected directly into subcutaneous tissue under the skin
For dermal procedures/ minor surgical procedures
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Ropivacaine
Nerve block and field block anesthesia (regional anesthesia)
Goal: block conductivity of sensory nerves from that area
Bupivacaine
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
Levobupivacaine
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
Diethyl ether
General anesthetics
Limb amputations
Slow rate of induction
Highly flammable
Chloroform
General anesthetics
Minimal alveolar concentration (MAC)
the potency of inhalational anesthetics
Inspired concentration of the anesthetic required to produce anesthesia
