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Basic -Chap. 2 3 4 5

Pharmacology, what you need to know for each drug class

An____ is a compound that binds to a receptor and produces the biological response. AGONIST
Specialized target macromolecule that binds a drug and medicates its pharmacological action. Drug receptor
Enzymes, nucleic acids, or specialized membrane-bound proteins Receptors
More closely related to plasma concentration than dose-response curves. Concentration-response curves
Full agonist The effect reaches 100% of the maximum possible.
Partial agonist Produces the biological response but cannot product 100% of the biological response even at very high doses.
__________ is the maximal response a drug can produce. Efficacy
____________ is a measure of the dose that is required to produce a response. Potency
For example, drug A produces complete eradication of PVCs at a dose of 10 mg. Drug B produces complete eradication of PVCs at a dose of 20 mg. Both drugs have the same _______, but Drug A is _________ than Drug B. Same efficacy (complete eradication of PVCs), A is more potent than B. It takes less of Drug A to produce the same effect.
Drug C reduces PVCs by 60% and takes a dose of 50 mg to achieve the effect. Therefore, drug C has less _______ and less ______ in the reduction of PVCs compared to Drugs A and B. efficacy and potency
ED50 (effective dose) Potency is often expressed as the dose of a drug required to achieve 50% of the desired therapeutic effect.
___________ is a measure of drug safety. A drug with a higher ___________ is safer than one with a lower _____________. Therapeutic index, therapeutic index, therapeutic index (7)
____________ is the ultimate toxicity. Death (7
The ___________ ___________ is the range of plasma concentrations of a drug that will elicit the desired response in a population of patients. therapeutic window (7)
____________ block or reverse the effect of agonists. They have no effect of their own. Antagonists
Binding of an ________ to a ________ does not produce a biological effect. antagonist, receptor (7)
The _________ can block the effect of an _________ or it can reverse the effect of an _________. antagonist, agonist, agonist (7)
An example of an antagonist is ___________, an _________ antagonist. naloxone, opiod (7)
No effect of its own. Naloxone (7)
Mechanism of action of B-blockers. antagonist which blocks or reverses the effect of endogenously produced compounds, such as epinephrine or norepinephrine. (8)
The __________ are competitive, they compete for the same site on the receptor as the agonist. If the _______ wins, a reponse is produced. If the ________ wins, no reponse is produced. antagonists, agonist, antagonist (8)
Increase the _________ of ______, increase odds that ________ will win the receptor spot and produce the effect. concentration, agonist, agonist molecule (8)
Reduces the maximal response that an agonist can produce. Noncompetitive antagonist (8)
________ _______ have opposite effects from those full agonists. They are not the same as antagonists, which block the effect of both agonists and inverse agonists. Inverse agonists (9)
______ increase the relative amount of time the channel is in open state compared to basal rate and _____ ____ decrease. Agonists, inverse agonists (9)
Leads to sedation. GABAa receptor channel complex, agonists increase the amount of chloride that moves into neuron and will hyperpolarize it. (9)
Leads to increase in excitability and can cause seizures. An inverse agonist will decrease the amount of chloride that moves into the neuron, which will result in a depolarization compared to the resting state. (9)
Inverse agonists bind to receptor and tip equilibrium toward the _________ state, agonists toward the ________ state inactive, active (9)
Bind to the receptor and have no effect on the basal state. Antagonists (9)
Liver is a metabolic machine, can inactivate drugs on their way to GI tract to body. This is called ____________ ____________ ________. first-pass effect (11)
Great chemical plant in the body. Liver (11)
Almost all require that the drug cross a _______ ________ to reach its site of action. biological membrane (11)
Drugs cross membranes by _______ _______ or _____ _______. passive diffusion, active transport (11)
Passive diffusion requires a _________ _______ across the membrane. Vast majority of drugs gain access to their site of action by this methods. concentration gradient (11)
_____________ _________ can penetrate the cell membrane through aqueous channels. Water-soluble drugs (11)
Just move through the membrane. More commonly lipid-soluble drugs (11)
A drug tends to pass through membranes if it is _________. Uncharged (11)
Uncharged drugs are more ______ ________ than charged drugs. Many drugs are _______ or ______. lipid soluble, weak acids, weak bases (11)
For a weak acid, when pH is less than pK, the _______ form (nonionized) ________. When pH greater than pK, the ______________ (ionized) form predominates. protonated, predominates,unprotonated (12)
Happy to give up a hydrogen ion and become charged. Weak acids are hydrogen ion donors. (13)
When you put HCL into water it immediately turns into ______ and _______. H+ and CL-, use this example to remember weak acids donate a hydrogen ion and become charged. (12)
If we _____________ the pH by adding more ____, we will move the equilibrium for the weak acid more to the left, which is the ________ (__________) form. decrease, H+, nonionized, uncharged (12)
If we __________ H+, making pH _______, we drive the equilibrium toward the _______. This increases the concentration of the _______ form of the ______ ______. take away (or decrease), higher, right,ionized, weak acid (12)
When the pH is _______ than the pK for the ______, the charged form of the acid predominates. higher, acid (12)
For a weak base, pH less than pK _________ _____ ______ ________. ionized form (protonated) predominates (12)
When pH is greater than pK, the _______ _____ form _______. unprotonated (nonionized), predominates (2)
Weak bases are ________ of weak acids. Weak base is a hydrogen ion acceptor. If a loose hydrogen ion seeks to join it, the base may accept it. If it accepts the hydrogen ion, then it becomes _______. opposite, charged (12)
In the stomach (pH 2.0) ____ ______ are uncharged and will be absorbed into the blood-stream, whereases _____ _______ are charged and will remain in the GI tract. weak acids, weak bases (13)
In the intestine (pH 8.0), which will be better absorbed, a weak acid (pK 6.8) or a weak base (pK 7.1)? a weak base (13)
If we alkalinize the urine to a pH of 7.8, will a lower or higher percentage of a weak acid (pK 7.1) be ionized, compared with when the urine pH was 7.2)? Higher, because more weak acid will be ionized the more the pH exceeds the pK. (13)
The amount of drug that is absorbed after administration by route X compared with the amount of drug that is absorbed after IV administration. X is any route of drug administration other than IV. Bioavailability (13)
Indicates rate which drug is cleared from the body. Clearance (14)
Clearance is defined as the volume of plasma from which all drug is removed in a given time. Thus, the units for clearance are given in _____ per ____ ____. volume, unit time (14)
Total body clearance Sum of clearances from various organs involved in drug metabolism and elimination. (15)
Is the mathematical description of the rate and extent of uptake, distribution, and elimination of drugs in the body. Pharmacokinetics (16)
Vd Volume of distribution is a calculation of the apparent volume in which a drug is dissolved. (16)
Vd = _____________ Volume of distribution = Dose(mg)/plasma concentration (mg/ml) (16).
Drug is lipid soluble and stored in _____. fat (16)
Most drugs disappear from plasma by processs that are concentration-dependent, which results in __________. first-order kinetics. With first-order elimination, a constant percentage of the drug is lost per unit time. An elimination rate constant can be described. (17)
ke The elimination rate constant (units are 1/time) (17)
Half-life Period of time required for the concentration of a drug to decrease by one half. (17)
t 1/2 = 0.693/ke The half-life is constant and related to ke for drugs that have first-order kinetics. (18)
Clearance of drug is _________ from the elimination rate. different (18)
Clearance Volume of fluid cleared of a drug per unit time. (18)
Rate of removal of drug in weight per unit time. Elimination rate (19)
Drugs with first-order kinetics, clearance and elimination rate are_______, related (19)
Zero-order kinetics Drugs that saturate routes of elimination disappear from plasma in a non-concentration-dependent. (19)
Involves specific enzymes which is one of the most important factors that contribute to a drug having zero-order kinetics. Metabolism in the liver. (19)
Many drugs show zero-order kinetics at ______, or _____ concentrations. high, toxic (19)
For drugs with zero-order kinetics, a constant amount of drug is lost per unit time. The _____ _______ is ____ constant for zero-order reactions, but depends on the ___________. half-life, not, concentration (19)
The ______ the concentration, the _______ the t 1/2. higher, longer (19)
Nonlinear or dose-dependent kinetics Zero-order kinetics is also known as... (19)
Refers to drugs that are first-order at lower doses and switch to zero-order at higher doses (often in the therapeutic range). Dose-dependent, zero-order, and nonlinear (20)
________ refers to the fact that drugs with zero-order kinetics do not show a linear relationship between drug dose and plasma concentration. Nonlinear (20)
When multiple dosing, or a continuous infusion, a drug will accumulate until the amount __________ per unit time is equal to the amount __________ per unit time. The plasma concentration at this point is called the ______ ____ ______ (Css). administrated, eliminated, steady-state concentration (20)
Elimination rate is proportional to the _____ ______ of the drug, so the concentration ______ so does the _________ rate. plasma concentration, rises, elimination (20)
Steady State The infusion rate and the elimination rate are equal. (20)
Css = ___________ Css = Infusion rate (mg/min)/Clearance (ml/min) = mg/ml (20)
Direct relationship between Css and the infusion rate (assuming clearance is constant). If we double the infusion rate, the Css _______. doubles (21)
Repeated dosing is associated with ______ and ________ plasma concentrations. peak, trough (21)
The time need to reach steady state depends ONLY on the _____ _____ of the drug. Ninety percent of steady state is reached in 3.3 half-lives. half-life (21)
3.3 half-lives equals _________. 90% of percentage of steady state achieved (22).
4 half-lives equals ________. 94% of percentage of steady state achieved (22).
5 half-lives equals ________. 97% of percentage of steady state achieved (22).
What is used if the half-life of a drug is long such as approx. 6 days for digitoxin to achieve a steady state (about 4 times the half-life)? This would take over 3 weeks. Loading dose (22)
Loading dose Single dose of a drug used to raise the plasma concentration to a therapeutic level more quickly than would occur through repeated smaller doses. (22)
Major site for drug metabolism. Liver (24)
Goal of metabolism is to produce ______ that are ______, or _______ and can be eliminated by the kidney. metabolites, polar, charged (24)
Frequently involve the P-450 system. Phase I (24)
Reactions are conjugations, mostly with glucuronide. Phase II (24)
Reactions convert lipophilic molecules into more polar molescules by introducing or unmasking a polar functional group such as -OH or -BG2. Most of these reactions utilize the microsomal P-450 enzymes. Phase I (24)
Plays a role in the metabolism of about 50% of the drugs. CYP3A4 (24)
Induces CYP3A4 which can increase metabolism of estrogen, thus reducing the effectiveness of birth control pills. Rifampin (24)
Conjugation reactions. Phase II (24)
Glomerular filtration, proximal tubular section, and distal tubular reabsorption. Renal elimination involves 3 physiological processes. (25)
Free drug flows out of body. Size of molecule is the only limiting factor. Glomerular tubular secretion (25)
Drugs are actively secreted into. Proximal tubular section (25)
Uncharged drugs, may diffuse out of the kidney and escape elimination. Distal tubular reabsorption.
Needs to be charged. For a drug to be excreted so that it is trapped in the urine and can't cross the membrane to sneak back into the body. (25)
When pH is _______ than pK, the unprotonated forms (A- and B) predominate. higher (25)
When pH is _______ than the pK, the protonated forms (HA and BH+) predominate. less (25)
Created by: mareed3



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