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426 Cards in this Set
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- 3rd side (hint)
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Km: Definition
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Km = Substrate at 0.5*Vmax
Km reflects the affinity of the enzyme for its substrate |
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Vmax indicates what?
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Vmax is directly proportional to the enzyme concentration.
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Relationship between Km and affinity
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-The lower the Km, the higher the affinity
-Smaller Km means enzyme is saturated earlier, which means that small amounts of substrate are picked up by the enzyme. |
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Reading an inverse curve: Y-intercept equals ?
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1/Vmax
The higher the Y-intercept the lower the Vmax |
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Reading an inverse curve: X-intercept equals ?
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(1/-Km)
The further to the right the x-intercept, the greater the Km |
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Reading an inverse curve: Slope equals ?
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Km/Vmax
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Reading an inverse curve: Effect of a competitive inhibitor
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X-intercept farther to the right, meaning Km is greater, because you need more substrate to get the same effect as the competitive inhibitor is hogging the enzyme.
The y-intercept is the same, meaning Vmax hasn't changed, because there isn't any more enzyme. The slope is greater, because Km has increased while Vmax has stayed the same. |
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Reading an inverse curve: Effect of a noncompetitive inhibitor
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The x-intercept is the same, meaning Km is the same, because the affinity for the enzyme hasn't changed, there's just less of it.
The y intercept has increased, meaning Vmax has decreased, because enzyme has been inactivated by the noncompetitive inhibitor The slope is greater, because Vmax has decreased while Km has stayed the same. |
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Competitive inhibitor: Resemble substrate
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Yes
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Competitive inhibitor: Overcome by increased substrate?
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Yes
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Competitive inhibitor: Binds active site?
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Yes
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Competitive inhibitor: Effect on Vmax
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Unchanged. The amount of enzyme has not changed.
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Competitive inhibitor: Effect on Km
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Increased. A lot more substrate needs to be available to seize the active sites.
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Noncompetitive inhibitor: Resemble substrate?
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No
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Noncompetitive inhibitor: Overcome by increased substrate?
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No
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Noncompetitive inhibitor: Binds active site?
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No
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Noncompetitive inhibitor: Effect on Vmax
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Decreased. Takes the enzyme out.
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Noncompetitive inhibitor: Effect on Km
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Unchanged. Does not change the affinity for the enzyme.
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Volume of distribution: Abbreviation
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Vd
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Vd: Stands for what?
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Volume of distribution
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Volume of distribution: definition
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Vd = (amount of drug in the body)/(plasma drug concentration)
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Volume of distribution: What alters it?
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Liver and kidney disease
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Where are drugs with a low Vd distributed?
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plasma
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Where are drugs with a medium Vd distributed?
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extracellular space
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Where are drugs with a high Vd distributed?
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tissues
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Clearance: definition
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=(rate of elimination of drug)/(plasma drug concentration)
=Vd x Ke where Ke=elimination constant |
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Half life: definition
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The time required to change the amount of drug in the body by 1/2 during elimination (or during a constant infusion).
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What percentage of steady state is a drug at after: 1 half life
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50%
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What percentage of steady state is a drug at after: 2 half lives
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75%
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What percentage of steady state is a drug at after: 3 half lives
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87.5%
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What percentage of steady state is a drug at after: 3.3 half lives
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90%
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What percentage of steady state is a drug at after: 4 half lives
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94%
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How many half lives does it take for a drug to reach the following percentage of steady state: 50%
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1 half life
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How many half lives does it take for a drug to reach the following percentage of steady state: 75%
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2 half lives
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How many half lives does it take for a drug to reach the following percentage of steady state: 87.5%
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3 half lives
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How many half lives does it take for a drug to reach the following percentage of steady state: 90%
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3.3 half lives
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How many half lives does it take for a drug to reach the following percentage of steady state: 94%
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4 half lives
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Cp stands for what?
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target plasma concentration
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What is the abbreviation for target plasma concentration?
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Cp
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In pharmacology, what is F an abbreviation for?
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Bioavailability
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What is the abbreviation in pharmacology for bioavailability?
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F
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Loading dose: Definition
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Loading dose = (Cp * Vd)/F (where Cp equals the target plasma concentration, Vd equals volume of distribution, and F equals bioavailability)
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Maintenance dose: Definition
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Maintenance dose = (Cp * CL)/F (where Cp is the target plasma concentration and CL is clearance and F is bioavailability)
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Zero-order elimination: definition
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Constant elimination over time regardless of drug.
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How does Cp vary with time during zero-order elimination?
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Cp decreases linearly with time.
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Zero-order elimination: Drug examples
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-Ethanol
-Phenytoin -Aspirin (at high concentrations) |
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First-order elimination: definition
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Rate of elimination is proportional to drug concentration
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Zero-order elimination vs First-order elimination: Comparison
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Zero-order: Constant amount of drug eliminated per unit time
1st-order: Constant fraction of drug eliminated per unit time |
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How does Cp vary with time during first-order elimination?
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Cp decreases exponentially with time.
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Urine: Which species get trapped in urine?
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Ionized species
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In what kind of environment is the following trapped?: Weak acids
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Basic environments
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In what kind of environment is the following trapped?: Weak bases
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Acidic environments
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In what kind of environment is the following digested?: Weak acids
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Acidic environments (below pKa)
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In what kind of environment is the following digested?: Weak bases
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Basic environments (above pKa)
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How do you treat an overdose of the following?: Weak acids
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Bicarbonate
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How do you treat an overdose of the following?: Weak bases
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Ammonium chloride
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Phase I metabolism: Processes
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Cytochrome P450
-reduction -oxidation -hydrolysis |
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Phase II metabolism: Processes
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Conjugation
-acetylation -glucuronidation -sulfation |
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Phase I metabolism: Metabolites
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-slightly polar
-water-soluble -often still active |
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Phase II metabolism: Metabolites
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-very polar
-renally excreted -inactive |
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What phase of metabolism do geriatric patients lose first?
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Phase I
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Effect on dose/effect curve of: competitive antagonist
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Shifts curve to the right, decreasing potency and increasing EC50.
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Effect on dose/effect curve of: noncompetitive antagonist
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Shifts curve downward, decreasing efficacy
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What is EC50?
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Dose causing 50% of maximal effect
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What is Kd?
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Concentration of drug required to bind 50% of receptor sites
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How many half lives does it take for a drug to reach the following percentage of steady state: 97%
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5 half lives
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What percentage of steady state is a drug at after: 5 half lives
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97%
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Effect on dose/effect curve: Spare receptors
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The drug binding and drug effect are independent of each other with effect to the left of binding.
This means that EC50 is lower than Kd, so very little drug needs to bind to get 50% of the effect. |
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Effect on dose/effect curve: Partial agonist
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-Lower maximal efficacy
-Potency independent (amount of dose to get to maximum effect) |
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Therapeutic Index: Definition
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=(TD50)/(ED50)
where TD50 equals median toxic dose, and ED50 equals median effective dose. |
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Where are nicotinic receptors found?
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Preganglionic synapses before:
-Cardiac and smooth muscle (Parasympathetic and Sympathetic) -Gland cells (Parasympathetic and Sympathetic) -Nerve terminals (Parasympathetic and Sympathetic) -Renal vascular smooth muscle (Sympathetic) Neuromuscular junctions for skeletal muscle |
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What is the neurotransmitter at Nictoinic receptors?
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Acetylcholine
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What is the neurotransmitter at Muscarinic receptors?
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Acetylcholine
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Where are muscarinic receptors found?
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Parasympathetic end plates:
-Cardiac and smooth muscle -Gland cells -Nerve terminals Sympathetic end plate: -Sweat glands |
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Where are D1 receptors found?
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Sympathetic:
Renal vascular smooth muscle |
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What type of G-protein is associated with the following receptor type?: alpha-1
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Gq
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What type of G-protein is associated with the following receptor type?: alpha-2
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Gi
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What type of G-protein is associated with the following receptor type?: beta-1
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Gs
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What type of G-protein is associated with the following receptor type?: beta-2
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Gs
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What type of G-protein is associated with the following receptor type?: M1
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Gq
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What type of G-protein is associated with the following receptor type?: M2
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Gi
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What type of G-protein is associated with the following receptor type?: M3
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Gq
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What type of G-protein is associated with the following receptor type?: D1
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Gs
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What type of G-protein is associated with the following receptor type?: D2
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Gi
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What type of G-protein is associated with the following receptor type?: H1
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Gq
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What type of G-protein is associated with the following receptor type?: H2
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Gs
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What type of G-protein is associated with the following receptor type?: V1
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Gq
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What type of G-protein is associated with the following receptor type?: V2
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Gs
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What types of receptors are associated with the following G-proteins: q
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-alpha-1
-M1 -M3 -H1 -V1 |
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What types of receptors are associated with the following G-proteins: i
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-alpha-2
-M2 -D2 |
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What types of receptors are associated with the following G-proteins: s
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-beta-1
-beta-2 -D1 -H2 -V2 |
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What are the major functions of the following receptor type: alpha-1
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Increase vascular smooth muscle contraction
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What are the major functions of the following receptor type: alpha-2
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-Decrease sympathetic outflow
-Decrease insulin release |
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What are the major functions of the following receptor type: beta-1
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-Increase heart rate
-Increase contractility -Increase renin release -Increase lipolysis -Increase aqueous humor formation |
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What are the major functions of the following receptor type: beta-2
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-Vasodilation
-Bronchodilation -Increased glucagon release |
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What are the major functions of the following receptor type: M1
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CNS
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What are the major functions of the following receptor type: M2
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Decrease heart rate
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What are the major functions of the following receptor type: M3
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Increase exocrine gland secretions
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What are the major functions of the following receptor type: D1
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Relax renal vascular smooth muscle
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What are the major functions of the following receptor type: D2
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Modulate transmitter release (especially in brain)
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What are the major functions of the following receptor type: H1
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-Increase nasal/bronchial mucus production
-Contraction of bronchioles -Pruritus -Pain |
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What are the major functions of the following receptor type: H2
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Increased gastric acid secretion
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What are the major functions of the following receptor type: V1
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Increased vascular smooth muscle contraction
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What are the major functions of the following receptor type: V2
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-Increased water permeability and reabsorption in the collecting tubules of the kidney
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Gq protein pathway
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-Receptor stimulated
-Gq protein stimulates Phospholipase C -Phospholipase C catalyzes the conversion of Lipids to PIP2 -PIP2 splits into IP3 and DAG IP3 stimulates an increase in Calcium concentration DAG activates Protein Kinase C |
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Gs protein pathway
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-Receptor stimulated
-Gs protein stimulates Adenylylcyclase -Adenylylcyclase catalyzes conversion of ATP to cAMP -cAMP activates Protein Kinase A |
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Gi protein pathway
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-Receptor stimulated
-Gi protein inhibits Adenylylcyclase -Decreases conversion of ATP to cAMP -Decreased activation of Protein kinase A |
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Cholinergic pathway (presynaptic events to receptor)
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1. Choline transported into presynaptic bulb
2. Acetyl-Coa joints with Choline-ChAT to form acetylcholine, and the two are taken up by a vesicle. 3. The vesicle joins with the cell membrane and ACh is exocytosed 4. ACh is released into the synapse 5. Acetylcholine joints with the Cholinoceptor or is degraded by AChE into Choline + Acetate |
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Hemicholinum: Action and mechanism
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Inhibits cholinergic transmission
Mechanism: Inhibits transfer of choline into presynaptic bulb |
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Vesamicol: Action and mechanism
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Inhibits cholinergic transmission
Mechanism: Inhibits uptake of ACh into a vesicle in the presynaptic bulb |
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Ca2+: Action on presynaptic vesicles
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Stimulates exocytosis of neurotransmitters from presynaptic bulb
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Botulinum: Action and mechanism
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Inhibits cholinergic transmission
Mechanism: Inhibits exocytosis of neurotransmitters from presynaptic bulb |
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Noradrenergic pathway (presynaptic events to receptor)
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1. Tyrosine is transferred into the presynaptic bulb
2. Tyrosine is converted into DOPA 3. DOPA is converted to Dopamine 4. Dopamine is converted to Norepinephrine and transferred into a vesicle 5. Norepinephrine is exocytosed from the presynaptic terminal 6. 3 possibilities happen a. Norepinephrine binds to a beta adrenoreceptor. b. Norepinephrine is reuptaken by the releasing neuron c. Norepinephrine binds to an alpha-2 receptor on the releasing neuron d. It diffuses away/is metabolized. |
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Metyrosine: Action and mechanism
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Action: Inhibits noradrenergic transmission
Mechanism: Inhibits step where tyrosine is converted into DOPA |
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Reserpine: Action and mechanism
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Action: Inhibits noradrenergic transmission
Mechanism: Prevents sequestration of norepinephrine into vesicles |
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Guanethidine: Action and mechanism
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Action: Inhibits noradrenergic transmission
Mechanism: Inhibits exocytosis of Norepinephrine from presynaptic bulb |
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Amphetamine: Action and mechanism
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Action: Stimulates noradrenergic transmission
Mechanism: Stimulates exocytosis of norepinephrine from presynaptic bulb |
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Tricyclic antidepressant: Mechanism
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Decreases reuptake of norepinephrine from synaptic cleft into releasing neuron
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Cocaine: Mechanism
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Decreases reuptake of norepinephrine from synaptic cleft into releasing neuron
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Angiotensin II: Effect on noradrenergic pre-synaptic neurons
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Enhances release of NE
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Cholinomimetics: Direct agonists
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Bethanechol, Carbachol, Pilocarpine, Methacholine
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Cholinomimetics: Indirect agonists
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Neostigmine (AChE inhibitor), Pyridostigmine, Edrophonium, Physostigmine, Echothiophate
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Use of: Bethanechol
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Postoperative and neurogenic ileus and urinary retention
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Use of: Carbachol
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-Glaucoma
-pupillary contraction -release of intraocular pressure |
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Use of: Pilocarpine
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Potent stimulator of:
-Sweat -Tears -Saliva |
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Use of: Methacholine
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Challenge test for diagnosis of asthma
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Use of: Neostigmine
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AChE inhibitor
-Postoperative/neurogenic ileus/urinary retetnion -Myasthenia Gravis -Reversal of neuromuscular junction blockade (postoperative) -No CNS penetration |
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Use of: Pyridostigmine
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-Myasthenia Gravis (increases strength)
-does penetrate CNS |
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Use of: Edrophonium
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Diagnosis of myasthenia gravis (extremely short acting)
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Use of: Physostigmine
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-Glaucoma (crosses blood-brain barrier into CNS)
-Atropine overdose |
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Use of: Ecthiophate
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-Glaucoma
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Mechanism of indirect cholinomimetics
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Increase endogenous ACh
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Synonym for indirect cholinomimetics
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Anticholinesterases
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Synonym for anticholinesterases
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indirect cholinomimetics
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Bethanechol: mechanism
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-Activates bowel and bladder smooth muscle
-Resistant to AChE |
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Carbachol: mechanism
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-Contracts ciliary muscle of eye (open angle)
-Contracts Pupillary sphincter (narrow angle) -Resistant to AChE |
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Methacholine: mechanism
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Stimulates muscarinic receptors in airway when inhaled
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Symptoms of cholinesterase inhibitor poisoning
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DUMBBELS SAC
-Diarrhea -Urination -Miosis -Bronchospasm -Bradycardia -Excitation of skeletal muscle and CNS -Lacrimation -Sweating -Salivation -Abdominal Cramping |
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Antidote to cholinesterase inhibitor poisoning
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-Atropine (muscarinic antagonist) +
-Pralidoxime (chemical antagonist used to regenerate active cholinesterase) |
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Cholinesterase inhibitors
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-Parathion
-Other organophosphates |
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Cholinoreceptor blockers
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-Atropine (homatropine, tropicamide)
-Benztropine -Scopolamine -Ipratropium -Methscoplamine (oxybutin, glycopyrrolate) |
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Cholinoreceptor blockers used to produce: mydriasis and cycloplegia
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Atropine, homatropine, tropicamide
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Cholinoreceptor blockers used for: Parkinson's disease
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Benztropine
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Cholinoreceptor blockers used for: Motion sickness
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Scopolamine
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Cholinoreceptor blockers used for: Obstructive pulmonary disease
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Ipratropium
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Cholinoreceptor blockers used for: Genitourinary problems
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-Methscopolamine
-Oxybutin -Glycopyrrolate |
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Application of: Atropine
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Produce mydriasis and cycloplegia
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Application of: Homatropine
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Produce mydriasis and cycloplegia
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Application of: Tropicamide
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Produce mydriasis and cycloplegia
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Application of: Benztropine
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Parkinson's Disease
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Application of: Scopolamine
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Motion sickness
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Application of: Ipratropium
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Obstructive pulmonary diseases
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Application of: Methscopolamine
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-Reduce urgency in mild cystitis
-Reduce bladder spasms |
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Application of: Oxybutin
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-Reduce urgency in mild cystitis
-Reduce bladder spasms |
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Application of: Glycopyrrolate
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-Reduce urgency in mild cystitis
-Reduce bladder spasms |
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Glaucoma drugs: Categories
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-alpha-agonists
-beta-blockers -diuretics -cholinomimetics -prostaglandins |
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Glaucoma drugs - alpha agonists:
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Epinephrine
Brimonidine |
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Which glaucoma drug should not be used in closed-angle glaucoma?
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Epinephrine
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Epinephrine: Mechanisms and side effects
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-M:
--Increased outflow of aqueous humor -E: --Mydriasis --Stinging --Do not use in closed angle glaucoma |
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Brimonidine: Mechanisms and side effects
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M: Decreased aqueous humor synthesis
E: No pupillary or vision changes |
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Glaucoma drugs - beta blockers:
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Timolol
Betaxolol Carteolol |
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Glaucoma drugs - beta blockers: Mechanism and side effects
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M: Decreased aqueous humor secretion
E: No pupillary or vision changes |
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Glaucoma drugs - diuretics: Drugs
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Acetazolamide
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Glaucoma drugs - diuretics: mechanisms and side effects
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M: Decreased aqueous humor secretion due to decreased bicarbonate (via inhibition of carbonic anhydrase)
E: No pupillary or vision changes |
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Glaucoma drugs - Cholinomimetics: Drugs
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Direct: Pilocarpine, Carbechol
Indirect: Physostigmine, Ecthiopate |
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Glaucoma drugs - Cholinomimetics: Mechanism and Side effects
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M:
-Increase outflow of aqueous humor -Contract ciliary muscle and open trabecular meshwork -Use pilocarpine in emergencies -Very effective at opening canal of Schlemm E: -Miosis -Cyclospasm |
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Glaucoma drugs - Prostaglandins: Drugs
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Latanoprost (PGF-2alpha)
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Glaucoma drugs - Prostaglandins: Mechanism and Effects
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M: Increase outflow of aqueous humor
E: Darkens color of iris (browning) |
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Atropine: General effects mnemonic
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Blocks BUMBLED ASS
B: Bradycardia U: Urination M: Miosis B: Bronchospasm L: Lacrimation E: Excitation of skeletal muscle and CNS D: Diarrhea A: Abdominal cramping S: Sweating S: Salivation |
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Atropine: Side effects
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-Hot as a hare (Increased body temperature; hyperthermia in infants)
-Dry as a bone (Dry mouth and dry skin; Urinary retention in men with prostatic hypertrophy; Constipation) -Red as a beet (Flushed skin) -Blind as a bat (Cycloplegia, Acute angle-closure glaucoma in elderly) -Mad as a hatter (disorientation) |
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Atropine: Mechanism
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Muscarinic antagonist
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Atropine: Effects on organ system: Eye
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-Increased pupil dilation
-Cycloplegia |
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Atropine: Effects on organ system: Airway
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-Decreased secretions
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Atropine: Effects on organ system: Stomach
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-Decreased acid secretion
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Atropine: Effects on organ system: Gut
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-Decreased motility
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Atropine: Effects on organ system: Bladder
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-Decreased urgency in cystitis
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Hexamethonium: Mechanism
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Nicotinic ACh receptor antagonist: Ganglionic blocker
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Hexamethonium: Clinical use
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Prevents vagal reflex responses to changes in blood pressure (eg prevents reflex bradycardia caused by NE)
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Sympathomimetics: Catecholamines: List
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-Epinephrine
-Norepinephrine -Isoproterenol -Dopamine -Dobutamine |
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Sympathomimetics: Non-catecholamines: List
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-Amphetamine
-Ephedrine -Phenylephrine -Albuterol -terbutaline -Cocaine -Clonidine -Alpha-methyldopa |
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Catecholamines: Epinephrine: Mechanism/selectivity
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-alpha-1
-alpha-2 -beta-1 (low doses beta-1 selective) -beta-2 |
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Catecholamines: Epinephrine: Applications
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-Anaphylaxis
-Glaucoma (open angle) -Asthma -Hypotension |
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Catecholamines: Norepinephrine: Mechanism/selectivity
|
More selective
-alpha-1 -alpha-2 Less selective -beta-1 |
|
|
|
Catecholamines: Norepinephrine: Applications
|
Hypotension (but decreased renal perfusion)
|
|
|
|
Catecholamines: Isoproterenol: Mechanism/selectivity
|
beta-1 = beta-2
|
|
|
|
Catecholamines: Isoproterenol: Applications
|
AV block (rare)
|
|
|
|
Catecholamines: Dopamine: Mechanism/selectivity
|
In decreasing order:
-D1=D2 -beta -alpha |
|
|
|
Catecholamines: Dopamine: Applications
|
-Shock (Increased renal perfusion)
-Heart failure |
|
|
|
Catecholamines: Dobutamine: Mechanism/selectivity
|
In decreasing order:
-Beta-1 -Beta-2 |
|
|
|
Catecholamines: Dobutamine: Applications
|
-Shock
-Heart failure cardiac stress testing |
|
|
|
Catecholamines: Amphetamine: Mechanism/selectivity
|
-Indirect general agonist
-Releases stored catecholamines |
|
|
|
Non-catecholamine sympathomimetics: Amphetamine: Applications
|
-Narcolepsy
-Obesity -ADD |
|
|
|
Non-catecholamine sympathomimetics: Ephedrine: Mechanism/selectivity
|
-Indirect general agonist
-releases stored catecholamines |
|
|
|
Non-catecholamine sympathomimetics: Ephedrine: Applications
|
-Nasal decongestion
-Urinary incontinence -Hypotension |
|
|
|
Non-catecholamine sympathomimetics: Phenyephrine: Mechanism/selectivity
|
alpha-1 more than alpha-2
|
|
|
|
Non-catecholamine sympathomimetics: Phenyephrine: Applications
|
-Pupil dilator
-Vasoconstriction -Nasal decongestion |
|
|
|
Non-catecholamine sympathomimetics: Albuterol: Mechanism/selectivity
|
Beta-2 > Beta-1
|
|
|
|
Non-catecholamine sympathomimetics: Albuterol: Applications
|
Asthma
|
|
|
|
Non-catecholamine sympathomimetics: Terbutaline: Mechanism/selectivity
|
Beta-2 > Beta-1
|
|
|
|
Non-catecholamine sympathomimetics: Terbutaline: Applications
|
Asthma
|
|
|
|
Non-catecholamine sympathomimetics: Cocaine: Mechanism/selectivity
|
-Indirect general agonist
-Uptake inhibitor |
|
|
|
Non-catecholamine sympathomimetics: Cocaine: Applications
|
-Vasoconstriction
-Local anesthesia |
|
|
|
Non-catecholamine sympathomimetics: Clonidine: Mechanism/selectivity
|
-Centrally acting alpha-2 agonist
-Decreases central adrenergic outflow |
|
|
|
Non-catecholamine sympathomimetics: alpha-methyldopa: Mechanism/selectivity
|
-Centrally acting alpha-2 agonist
-Decreases central adrenergic outflow |
|
|
|
Non-catecholamine sympathomimetics: Clonidine: Applications
|
Hypertension (especially with renal disease, as there is no decrease in blood flow)
|
|
|
|
Non-catecholamine sympathomimetics: alpha-methyldopa: Applications
|
Hypertension (especially with renal disease, as there is no decrease in blood flow)
|
|
|
|
Sympathomimetics selective for: alpha-1
|
-Phenylephrine (alpha-1 more than alpha-2)
-Norepinephrine (alpha-1 and alpha-2 more than beta-1) |
|
|
|
Sympathomimetics selective for: alpha-2
|
-Clonidine
-alpha-methyldopa -Norepinephrine (alpha-1 and alpha-2 more than beta-1) -Phenylephrine (alpha-1 more than alpha-2) -Norepinephrine (alpha-1 and alpha-2 more than beta-1) |
|
|
|
Sympathomimetics selective for: beta-1
|
-Dobutamine (beta-1 more than beta-2)
-Isoproterenol (beta-1 = beta-2) -Epinephrine (at low doses) -Albuterol, terbutaline (beta-2 more than beta-1) |
|
|
|
Sympathomimetics selective for: beta-2
|
-Albuterol, terbutaline (beta-2 more than beta-1)
-Isoproterenol (beta-1 = beta-2) -Dobutamine (beta-1 more than beta-2) |
|
|
|
Sympathomimetics selective for: None (general agonists)
|
-Amphetamine
-Ephedrine -Cocaine -Epinephrine (alpha and beta) |
|
|
|
Effect on blood pressure: Norepinephrine
|
Increases from 100 to 150
Mechanism: 1. Stimulates alpha more than beta 2. Systolic blood pressure goes up along with but more than diastolic blood pressure 3. Mean blood pressure rises |
|
|
|
Effect on blood pressure: Epinephrine
|
Mean pressure stays at 100, with wide pulse-pressure (100)
Mechanism: 1. Nonselectively stimulates both alpha and beta receptors 2. Alpha receptors: Systolic blood pressure goes up AND beta receptors: Diastolic blood pressure goes down 3. Mean blood pressure stays the same 4. Pulse pressure is wide |
|
|
|
Effect on blood pressure: Isoproterenol
|
Mean blood pressure goes down to 50, but pulse-pressure becomes wider (~75).
Mechanism: 1. Stimulates beta more than alpha. 2. Diastolic drops along with but more than systolic blood pressure 3. Mean blood pressure drops with wide pulse pressure |
|
|
|
Effect on heart rate: Norepinephrine
|
1. Mean pressure goes up
2. Goes down to 50 (reflex bradycardia) |
|
|
|
Effect on heart rate: Epinephrine
|
1. Beta-1 receptors are stimulated
2. Increases to 100 |
|
|
|
Effect on heart rate: Isoproterenol
|
1. Beta-1 receptors are stimulated more than alpha receptors
2. Increases to ~125 |
|
|
|
Sympathomimetic of choice for: Anaphylaxis
|
Epinephrine
|
|
|
|
Sympathomimetic of choice for: Open-angle glaucoma
|
Epinephrine
|
|
|
|
Sympathomimetic of choice for: Asthma
|
-Albuterol
-Terbutaline -Epinephrine |
|
|
|
Sympathomimetic of choice for: Hypotension
|
-Epinephrine
-Norepinephrine (though with decreased renal perfusion) -Ephedrine |
|
|
|
Sympathomimetic of choice for: AV block
|
Isoproterenol
|
|
|
|
Sympathomimetic of choice for: Shock
|
-Dopamine (increased renal perfusion)
-Dobutamine |
|
|
|
Sympathomimetic of choice for: Heart failure
|
Dopamine
|
|
|
|
Sympathomimetic of choice for: Heart failure cardiac stress testing
|
Dobutamine
|
|
|
|
Sympathomimetic of choice for: Narcolepsy
|
Amphetamine
|
|
|
|
Sympathomimetic of choice for: Obesity
|
Amphetamine
|
|
|
|
Sympathomimetic of choice for: Attention defecit disorder
|
Amphetamine
|
|
|
|
Sympathomimetic of choice for: Nasal decongestion
|
-Ephedrine
-Phenylephrine |
|
|
|
Sympathomimetic of choice for: Urinary incontinence
|
Ephedrine
|
|
|
|
Sympathomimetic of choice for: Dilation of pupils
|
Phenylephrine
|
|
|
|
Sympathomimetic of choice for: desired vasoconstriction
|
-Phenylephrine
-Cocaine |
|
|
|
Sympathomimetic of choice for: Local anesthesia
|
Cocaine
|
|
|
|
Sympathomimetic of choice for: Treatment of hypertension
|
Clonidine and alpha-methyldopa (especially for those with renal disease, no decrease in blood flow to kidney)
|
|
|
|
alpha-blockers: drug list
|
Non-selective
-Irreversible: Phenoxybenzamine -Reversible: Phentolamine alpha-1 selective -Prazosin -Terazosin -Doxazosin alpha-2 selective -Mirtazapine |
|
|
|
Phenoxybenzamine: Mechanism
|
irreversible nonselective alpha-blocker
|
|
|
|
Phentolamine: Mechanism
|
reversible nonselective alpha-blocker
|
|
|
|
Prazosin: Mechanism
|
alpha-1 blocker
|
|
|
|
Terazosin: Mechanism
|
alpha-1 blocker
|
|
|
|
Doxazosin: Mechanism
|
alpha-1 blocker
|
|
|
|
Mirtazapine: Mechanism
|
alpha-2 blocker
|
|
|
|
Nonselective alpha blockers: Application
|
Pheochromocytoma
|
|
|
|
alpha-2 blockers: Application
|
Depression
|
|
|
|
alpha-1 blockers: Application
|
-Hypertension
-Urinary retention in BPH |
|
|
|
Nonselective alpha blockers: Toxicity
|
-Orthostatic hypotension
-Reflex tachycardia |
|
|
|
alpha-2 blockers: Toxicity
|
-Sedation
-Increase in serum cholesterol -Increase in appetite |
|
|
|
alpha-1 blockers: Toxicity
|
-1st-dose orthostatic hypotension
-dizziness -headache |
|
|
|
Which class of alpha blockers should you use for: Pheochromocytoma
|
Nonselective alpha blockers
|
|
|
|
Which class of alpha blockers should you use for: Hypertension
|
alpha-1 blockers
|
|
|
|
Which class of alpha blockers should you use for: Urinary retention in bph
|
alpha-1 blockers
|
|
|
|
Which class of alpha blockers should you use for: Depression
|
alpha-2 blockers (Mirtazapine)
|
|
|
|
beta-blockers: mechanism in control of: hypertension
|
-decreased cardiac output
-decreased renin secretion |
|
|
|
beta-blockers: mechanism in control of: angina pectoris
|
1. decreased heart rate and contractility
2. result: decreased O2 consumption |
|
|
|
beta-blockers: mechanism in control of: MI
|
decrease in mortality (no mechanism given)
|
|
|
|
beta-blockers: mechanism in control of: supraventricular tachycardia
|
decreased AV conduction velocity
|
|
|
|
beta-blockers: mechanism in control of: congestive heart failure
|
slows progression (no mechanism given)
|
|
|
|
beta-blockers: mechanism in control of: glaucoma
|
decreased secretion of aqueous humor
|
|
|
|
which beta-blockers are used in control of: supraventricular tachycardia
|
-Propranolol
-Esmolol |
|
|
|
which beta-blockers are used in control of: glaucoma
|
Timolol
|
|
|
|
beta-blockers: toxicity: non-CV, non-CNS
|
-Impotence
-Asthma exacerbation |
|
|
|
beta-blockers: toxicity: Cardiovascular
|
-bradycardia
-AV block -congestive heart failure |
|
|
|
beta-blockers: toxicity: CNS
|
-sedation
-sleep alterations |
|
|
|
Non-selective beta blockers
|
-Propranol
-Timolol -Nadolol -Pindolol (partial agonist) -Labetalol (partial agonist) |
|
|
|
beta-1-selective beta-blockers
|
A BEAM of beta-1 blockers
-Acebutolol (partial agonist) -Betaxolol -Esmolol (short acting) -Atenolol -Metoprolol |
|
|
|
Antidote for: Acetaminophen
|
N-acetylcysteine
|
|
|
|
Antidote for: Salicylates
|
1. Alkalinize urine
2. Dialysis |
|
|
|
Antidote for: Anticholinesterases
|
-Atropine
-Pralidoxime |
|
|
|
Antidote for: Organophosphates
|
-Atropine
-Pralidoxime |
|
|
|
Antidote for: Anti-muscarinic anti-cholinergic agents
|
Physostigmine salicylate
|
|
|
|
Antidote for: beta-blockers
|
Glucagon
|
|
|
|
Antidote for: Digitalis
|
1. Stop digitalis
2. Normalize potassium 3. Lidocaine 4. anti-digitalis Fab fragments 5. Magnesium |
|
|
|
Antidote for: Iron
|
Deferoxamine
|
|
|
|
Antidote for: Lead
|
1st line: CaEDTA & Dimercaprol
2nd line?: Penicillamine Kids: Succimer |
First Aid lists Penicillamine in the antidotes section, but not in the section below, hence the ?
|
|
|
Antidote for: Arsenic
|
-Dimercaprol (BAL)
-Succimer -Penicillamine |
|
|
|
Antidote for: Gold
|
-Dimercaprol (BAL)
-Succimer -Penicillamine |
|
|
|
Antidote for: Mercury
|
-Dimercaprol (BAL)
-Succimer |
|
|
|
Antidote for: Copper
|
Penicillamine
|
|
|
|
Antidote for: Cyanide
|
-Nitrite
-Hydroxocobalamin -Thiosulfate |
|
|
|
Antidote for: Methemoglobin
|
Methylene blue
|
|
|
|
Antidote for: Carbon Monoxide
|
-100% Oxygen
-Hyperbaric Oxygen |
|
|
|
Antidote for: Methanol
|
-Ethanol
-Dialysis -Fomepizole |
|
|
|
Antidote for: Ethylene glycol (antifreeze)
|
-Ethanol
-Dialysis -Fomepizole |
|
|
|
Antidote for: Opioids
|
Naloxone/naltrexone
|
|
|
|
Antidote for: Benzodiazepines
|
Flumazenil
|
|
|
|
Antidote for: Tricyclics
|
NaHCO3 (nonspecific)
|
|
|
|
Antidote for: Heparin
|
Protamine
|
|
|
|
Antidote for: Warfarin
|
-Vitamin K
-Fresh frozen plasma |
|
|
|
Antidote for: tPA
|
Aminocaproic acid
|
|
|
|
Antidote for: streptokinase
|
Aminocaproic acid
|
|
|
|
For what drug(s) is the following an antidote?: N-acetylcysteine
|
Acetaminophen
|
|
|
|
For what drug(s) is the following an antidote?:
1. Alkalinize urine 2. Dialysis |
Salicylates
|
|
|
|
For what drug(s) is the following an antidote?: Atropine
|
-Anticholinesterases
-Organophosphates |
|
|
|
For what drug(s) is the following an antidote?: Pralidoxime
|
-Anticholinesterases
-Organophosphates |
|
|
|
For what drug(s) is the following an antidote?: Physostigmine salicylate
|
Antimuscarinic, anticholinergic agents
|
|
|
|
For what drug(s) is the following an antidote?: Glucagon
|
beta-blockers
|
|
|
|
For what drug(s) is the following an antidote?: Deferoxamine
|
Iron
|
|
|
|
For what drug(s) is the following an antidote?: CaEDTA
|
Lead
|
|
|
|
For what drug(s) is the following an antidote?: Dimercaprol
|
Dimercaprol is GLAMorous
-Gold -Lead -Arsenic -Mercury |
|
|
|
For what drug(s) is the following an antidote?: Succimer
|
-Lead
-Arsenic -Mercury -Gold |
|
|
|
For what drug(s) is the following an antidote?: Penicillamine
|
-Lead
-Copper -Arsenic -Gold |
|
|
|
For what drug(s) is the following an antidote?: Nitrite
|
Cyanide
|
|
|
|
For what drug(s) is the following an antidote?: Hydroxocobalamin
|
Cyanide
|
|
|
|
For what drug(s) is the following an antidote?: Thiosulfate
|
Cyanide
|
|
|
|
For what drug(s) is the following an antidote?: Methylene blue
|
Methemoglobin
|
|
|
|
For what drug(s) is the following an antidote?: Oxygen
|
Carbon monoxide (Oxygen should be 100% or hyperbaric)
|
|
|
|
For what drug(s) is the following an antidote?: Ethanol
|
-Methanol
-Ethylene glycol (antifreeze) |
|
|
|
For what drug(s) is the following an antidote?: Dialysis
|
-Methanol
-Ethylene glycol (antifreeze) -Salicylates |
|
|
|
For what drug(s) is the following an antidote?: Fomepizole
|
-Methanol
-Ethylene glycol (antifreeze) |
|
|
|
For what drug(s) is the following an antidote?: Naloxone/Naltrexone
|
Opioids
|
|
|
|
For what drug(s) is the following an antidote?: Flumazenil
|
Benzodiazepines
|
|
|
|
For what drug(s) is the following an antidote?: NaHCO3
|
Tricyclic Antidepressants
|
|
|
|
For what drug(s) is the following an antidote?: Protamine
|
Heparin
|
|
|
|
For what drug(s) is the following an antidote?: Vitamin K
|
Warfarin
|
|
|
|
For what drug(s) is the following an antidote?: Fresh, frozen plasma
|
Warfarin
|
|
|
|
For what drug(s) is the following an antidote?: Aminocaproic acid
|
-tPA
-streptokinase |
|
|
|
Lead poisoning: Signs and symptoms
|
LLEEAADD
-Lead Lines on: --gingivae --epiphyses of long bones on x-ray -Encephalopathy -Erythrocyte basophilic stippling -Abdominal colic -sideroblastic Anemia -wrist Drop -foot Drop |
|
|
|
Lead poisoning: 1st line treatment for adults
|
Both:
-Dimercaprol -EDTA |
|
|
|
Lead poisoning: 1st line treatment for children
|
Succimer
(It "sucks" to be a kid who eats lead) |
|
|
|
Causal agent for the following reaction: Atropine-like side effects
|
Tricyclic Antidepressants
|
|
|
|
Causal agent for the following reaction: Cardiac toxicity
|
-Doxorubicin (Adriamycin)
-Daunorubicin |
|
|
|
Causal agent for the following reaction: Coronary vasospasm
|
Cocaine
|
|
|
|
Causal agent for the following reaction: Cutaneous flushing
|
-Niacin
-Ca2+-channel blockers -Adenosine -Vancomycin |
|
|
|
Causal agent for the following reaction: Torsades des pointes
|
-Class III antiarrhythmics (sotalol)
-Class IA antiarrhytmics (quinidine) -Cisapride |
|
|
|
Causal agent for the following reaction: Agranulocytosis
|
-Clozapine
-Carbamazepine -Colchicine |
|
|
|
Causal agent for the following reaction: Aplastic anemia
|
-Chloramphenicol
-Benzene -NSAIDs |
|
|
|
Causal agent for the following reaction: Gray baby syndrome
|
Chloramphenicol
|
|
|
|
Causal agent for the following reaction: Hemolysis in G6PD-deficient patients
|
G6PD IS PAIN
-Isoniazid -Sulfonamides -Primaquine -Aspirin -Ibuprofen -Nitrofurantoin |
|
|
|
Causal agent for the following reaction: Thrombotic complications
|
oral contraceptive pills
|
|
|
|
Causal agent for the following reaction: Cough
|
ACE inhibitors (not ARBs)
|
|
|
|
Causal agent for the following reaction: Pulmonary fibrosis
|
-Bleomycin
-Amiodarone -Busulfan |
|
|
|
Causal agent for the following reaction: Acute cholestatic hepatitis
|
Macrolides
|
|
|
|
Causal agent for the following reaction: Focal to massive hepatic necrosis
|
-Halothane
-Valproic acid -Acetaminophen -Amanita phalloides |
|
|
|
Causal agent for the following reaction: Hepatitis
|
INH
|
|
|
|
Causal agent for the following reaction: Pseudomembranous colitis
|
-Clindamycin
-Ampicillin |
|
|
|
Causal agent for the following reaction: Adrenocortical insufficiency
|
Glucocorticoid withdrawal (HPA suppression)
|
|
|
|
Causal agent for the following reaction: Gynecomastia
|
Some Drugs Create Extra-Awesome Knockers
-Spironolactone -Digitalis -Cimetidine -estrogens -Alcohol (chronic use) -Ketoconazole |
|
|
|
Causal agent for the following reaction: Hot flashes
|
Tamoxifen
|
|
|
|
Causal agent for the following reaction: Gingival hyperplasia
|
Phenytoin
|
|
|
|
Causal agent for the following reaction: Osteoporosis
|
-Corticosteroids
-Heparin |
|
|
|
Causal agent for the following reaction: Photosensitivity
|
SAT for a photo
-Sulfonamides -Amiodarone -Tetracycline |
|
|
|
Causal agent for the following reaction: SLE-like syndrome
|
(It's not HIPP to have lupus)
-Hydralazine -INH -Procainamide -Phenytoin |
|
|
|
Causal agent for the following reaction: Tendonitis, tendon rupture, and cartilage damage
|
Fluoroquinolones (kids)
|
|
|
|
Causal agent for the following reaction: Fanconi's syndrome
|
Expired tetracycline
|
|
|
|
Causal agent for the following reaction: Interstitial nephritis
|
Methicillin
|
|
|
|
Causal agent for the following reaction: Hemorrhagic cystitis
|
-Cyclophosphamide
-Ifosfamide |
|
|
|
Causal agent for the following reaction: Cinchonism
|
-Quinidine
-Quinine |
|
|
|
Causal agent for the following reaction: Diabetes insipidus
|
-Lithium
-Demeclocycline |
|
|
|
Causal agent for the following reaction: Seizures
|
-Bupropion
-Imipenem/cilastatin |
|
|
|
Causal agent for the following reaction: Tardive dyskinesia
|
Antipsychotics
|
|
|
|
Causal agent for the following reaction: Disulfiram-like reaction
|
-Metronidazole
-Certain cephalosporins -Procarbazine -Sulfonylureas |
|
|
|
Causal agent for the following reaction: Nephrotoxicity/neurotoxicity
|
Polymyxins
|
|
|
|
Causal agent for the following reaction: Nephrotoxicity/ototoxicity
|
-Aminoglycosides
-Loop diuretics -Cisplatin |
|
|
|
P-450 Inducers
|
Queen Barb takes Phen-phen and Strictly Refuses Greasy Carbs
-Quinidine (CYP3A4) -Barbiturates -Phenytoin -St. John's Wort -Rifampin -Griseofulvin -Carbamazepine |
|
|
|
P-450 Inhibitors
|
Inhibitors Quickly Stop Cyber-Kids from Eating Grapefruit
-Isoniazid -Quinidine (CYP2D6) -Sulfonamides -Cimetidine -Ketoconazole -Erythromycin -Grapefruit juice |
|
|
|
P-450 inducer or inhibitor: Quinidine
|
Inhibitor: CYP2D6 (more prominent)
Inducer: CYP3A4 |
|
|
|
P-450 inducer or inhibitor: Barbiturates
|
Inducer
|
|
|
|
P-450 inducer or inhibitor: Phenytoin
|
Inducer
|
|
|
|
P-450 inducer or inhibitor: Rifampin
|
Inducer
|
|
|
|
P-450 inducer or inhibitor: Griseofulvin
|
Inducer
|
|
|
|
P-450 inducer or inhibitor: Carbamazepine
|
Inducer
|
|
|
|
P-450 inducer or inhibitor: St. John's wort
|
Inducer
|
|
|
|
P-450 inducer or inhibitor: Isoniazid
|
Inhibitor
|
|
|
|
P-450 inducer or inhibitor: Sulfonamides
|
Inhibitor
|
|
|
|
P-450 inducer or inhibitor: Cimetidine
|
Inhibitor
|
|
|
|
P-450 inducer or inhibitor: Ketoconazole
|
Inhibitor
|
|
|
|
P-450 inducer or inhibitor: Erythromycin
|
Inhibitor
|
|
|
|
P-450 inducer or inhibitor: Grapefruit juice
|
Inhibitor
|
|
|
|
Active metabolite of ethylene glycol
|
Oxalic acid
|
|
|
|
Active metabolite of methanol
|
-Formaldehyde
-Formic acid |
|
|
|
Active metabolite of ethanol
|
Acetaldehyde
|
|
|
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Pathway and toxicities of metabolism of: ethylene glycol
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1. Ethylene glycol is converted by alcohol dehydrogenase to
2. Oxalic acid causes: -Acidosis -Nephrotoxicity |
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Pathway and toxicities of metabolism of: methanol
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1. Methanol is converted by alcohol dehydrogenase to
2. Formaldehyde and formic acid which cause: -Severe Acidosis -Retinal damage |
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Pathway and toxicities of metabolism of: ethanol
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1. Ethanol is converted by alcohol dehydrogenase to
2. Acetaldehyde which causes: -Nausea -Vomiting -Headache -Hypotension |
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What enzyme is inhibited by disulfiram?
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Acetaldehyde dehydrogenase
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What inhibits acetaldehyde dehydrogenase?
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Disulfiram
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Clinical uses/toxicities for: Echinacea
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Use: Common cold
Toxicities: -GI distress -dizziness -headache |
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Clinical uses/toxicities for: Ephedra
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Uses: As for ephedrine
Toxicities: -CNS and cardiovascular stimulation At high doses: -Arrhythmias -Stroke -Seizure |
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Clinical uses/toxicities for: Feverfew
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Use: Migraine
Toxicities: -GI distress -Mouth ulcers -Antiplatelet actions |
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Clinical uses/toxicities for: Ginkgo
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Use: Intermittent claudication
Toxicities: -GI distress -anxiety -insomnia -headache -antiplatelet actions |
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Clinical uses/toxicities for: Kava
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Use: Chronic anxiety
Toxicities: -GI distress -sedation -ataxia -hepatotoxicity -phototoxicity -dermatotoxicity |
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Clinical uses/toxicities for: Milk thistle
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Use: Viral hepatitis
Toxicities: Loose stools |
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Clinical uses/toxicities for: Saw palmetto
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Use: Benign prostatic hyperplasia
Toxicities: -GI distress -Decreased libido -Hypertension |
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Clinical uses/toxicities for: St. John's wort
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Use: Mild to moderate depression
Toxicities: -GI distress and phototoxicity -serotonin syndrome with SSRIs -induces P-450 system |
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Clinical uses/toxicities for: DHEA
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Uses: Symptomatic improvement in females with SLE or AIDS
Toxicities: -Androgenization (premenopausal women) -Estrogenic effects (post menopausal) -Feminization (young men) |
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Clinical uses/toxicities for: Melatonin
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Use:
-Jet lag -Insomnia Toxicities: -Sedation -Suppresses midcycle LH -Hypoprolactinemia |
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Category for drug names ending with: -afil
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Erectile dysfunction (eg Sildenafil)
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Category for drug names ending with: -ane
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Inhalational general anesthetic (eg Halothane)
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Category for drug names ending with: -azepam
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Benzodiazepine (eg Diazepam)
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Category for drug names ending with: -azine
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Phenothiazine (neuroleptic, antiemetic) (eg Chlorpromazine)
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Category for drug names ending with: -azole
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Antifungal (eg Ketoconazole)
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Category for drug names ending with: -barbital
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Barbiturate (eg Phenobarbital)
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Category for drug names ending with: -caine
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Local anesthetic (eg Lidocaine)
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Category for drug names ending with: -cillin
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Penicillin (eg Methicillin)
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Category for drug names ending with: -cycline
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Antibiotic, protein synthesis inhibitor (Tetracycline)
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Category for drug names ending with: -ipramine
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Tricyclic Antidepressant (eg Imipramine)
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Category for drug names ending with: -navir
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Protease inhibitor (eg Saquinavir)
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Category for drug names ending with: -olol
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beta-blocker (eg Propranolol)
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Category for drug names ending with: -operidol
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Butyrophone (neuroleptic) (eg Haloperidol)
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Category for drug names ending with: -oxin
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Cardiac glycoside (inotropic agent) (eg Digoxin)
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Category for drug names ending with: -phylline
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Methylxanthine (eg Theophylline)
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Category for drug names ending with: -pril
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ACE inhibitor (eg Captopril)
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Category for drug names ending with: -terol
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beta-2 agonist (eg Albuterol)
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Category for drug names ending with: -tidine
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H2 antagonist (eg Cimetidine)
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Category for drug names ending with: -triptyline
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Tricyclic antidepressant (eg Amitryptyline)
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Category for drug names ending with: -tropin
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Pituitary hormone (eg Somatotropin)
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Category for drug names ending with: -zosin
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alpha-1 antagonist (eg Prazosin)
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Common ending for drug names in the following category: Erectile dysfunction
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-afil (eg Slidenafil)
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Common ending for drug names in the following category: Inhalational general anesthetic
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-ane (eg Halothane)
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Common ending for drug names in the following category: Benzodiazepine
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-azepam (eg Diazepam)
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Common ending for drug names in the following category: Phenothiazine (neuroleptic, antiemetic)
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-azine (eg Chlorpromazine)
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Common ending for drug names in the following category: Antifungal
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-azole (eg Ketoconazole)
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Common ending for drug names in the following category: Barbiturate
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-barbital (eg Phenobarbital)
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Common ending for drug names in the following category: Local anesthetic
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-caine (eg Lidocaine)
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Common ending for drug names in the following category: Penicillin
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-cillin (eg Methicillin)
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Common ending for drug names in the following category: Bacterial protein synthesis inhibitor
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-cycline (eg Tetracycline)
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Common ending for drug names in the following category: Tricyclic antidepressant
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-ipramine (Imipramine)
-triptyline (Amitriptyline) |
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Common ending for drug names in the following category: Protease inhibitor
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-navir (Saquinavir) (Mnemonic: Navir tease a pro)
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Common ending for drug names in the following category: beta-antagonist
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-olol (Propranolol)
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Common ending for drug names in the following category: butyrophenone (neuroleptic)
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-operidol (Haloperidol)
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Common ending for drug names in the following category: Cardiac glycoside
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-oxin (Digoxin)
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Common ending for drug names in the following category: Methylxanthine
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-phylline (eg Theophylline)
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Common ending for drug names in the following category: ACE inhibitor
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-pril (Captopril)
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Common ending for drug names in the following category: beta-2 agonist
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-terol (eg Albuterol)
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Common ending for drug names in the following category: H2 antagonist
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-tidine (eg Cimetidine)
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Common ending for drug names in the following category: Pituitary hormone
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-tropin (eg Somatotropin)
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Common ending for drug names in the following category: alpha-1 antagonist
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-zosin (eg Prazosin)
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