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Kinetics Exam1
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maryland-avocado-kilo-lamp-juliet-floor
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Published
02/06/2024
Dosing Regimen is {{c1::the manner in which a drug is taken}}.- How long- How often a day- How much- Doage form- Route of administration
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Pharmacokinetics (PK):- Covers the relationship between {{c1::drug input}} and the {{c1::concentration}} achieved with time.- {{c1::Drug input}}: {{c2…
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Pharmacodynamics (PD):- Covers the relationship between {{c1::concentration}} and both the {{c1::desired}} and {{c1::adverse effects}} produced with t…
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"What the body does to the drug" describes {{c1::Pharmacokinetics}}
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"What the drug does to the body" describes {{c1::Pharmacodynamics}}
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A Pharmacokinetics model graphs {{c1::Concentration}} vs {{c1::Time}}.A Pharmacodynamics model graphs {{c1::Effect}} vs {{c1::Log of Concentration}}.A…
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Concentration is defined as {{c1::Amount per Volume}}.
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02/06/2024
Localling acting: {{c1::Site of action is the same as site of administration}}. (Example: eye drops, nasal sprays, topical cream for skin diseases)Sys…
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Systemic exposure with time is obtained by measuring drug concentration either in {{c1::blood, plasma, or serum over time}}.
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What do each variable mean?
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Total AUC is a measure of {{c1::systemic exposure}}.
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ADME stands for
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Disposition is {{c1::all kinetic processes that occur to a drug subsequent to its systemic absorption = D + E}}
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Systemic absorption: process by which u{{c1::nchanged drug processed from the site of administration to site of measurement within the body, usually p…
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Intestinal absorption: {{c1::movement of drug across the intestinal epithelium}}.
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Routes of Administration:Intravascular: {{c1::IV and IA}}Extravascular: {{c1::SC, PO, IM, etc.}}
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Bioavailability is defined as: t{{c1::he rate and extent to which an active drug ingredient or therapeutic moiety is absorbed from a drug product and …
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F is {{c1::bioavailability (extent of absorption)}}Ka is {{c1::absorption rate constant (rate)}}
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What Route has F = 1 or 100%?- {{c1::Intravascular. IV or IA}}What route has F < 1 usually?- {{c1::Extravascular. PO, IM, SC, SL, etc}}
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EG is {{c1::gut extraction ratio}}EH is {{c1::hepatic extraction ratio}}
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02/06/2024
To calculate first-pass lost we use:{{c1::FG * FH }}.
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EH + FH = {{c1::1}}
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First-pass lost is NOT part of elimination since i{{c1::t occurs before the drug has entered the site of measurement.}}
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02/06/2024
How to calculate the Dose of a Drug with salt factor?
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CB is the concentration of drug in {{c1::(whole) blood}}C is the concentration of drug in {{c1::plasma}}.Drug concentration are usually assessed …
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What does Cb / C ratio tell us?
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Cb/C = 1 when {{c1::Cb=C}}Cb/C > 1 when {{c1::Cb>C}}Cb/C < 1 when {{c1::Cb<C}}
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02/06/2024
In class we assume in a regular 70kg person,Volume of blood is {{c1::5L}}Plasma volume is usually {{c1::3L}}This means that hematocrit is {{c1::0.4}} …
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Fraction unbound (fu):- measure of {{c1::how much drug is not being bound to plasma proteins}}.- ratio of unbound to total drug concentration in plasm…
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Fu,t = Cu/Ct is defined as the {{c1::concentration of drugs not bound to tissue}}.
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Amount of drug in plasma = {{c1::V(plasma) * C(plasma)}}
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Amount of drug in blood = {{c1::V(blood) * C(blood)}}
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Amount of drug in body (measured in blood) = {{c1::V(apparent volume of distribution in blood) * C(blood)}}
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Apparent blood volume of distribution (Vb) is the {{c1::proportionality constant between blood drug concentration and amount of drug in the body}}.A(b…
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Apparent plasma volume of distribution (V) is {{c1::the proportionally constant between plasma drug concentration and amount of drug in the body}}.A(b…
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In the equation relating V and fu; V = Vp + fu/fu,t * (Vt)How does volume of distribution relate with fu,t?
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Distribution is the process of {{c1::reversible transfer of a drug to and from the site of measurement and the peripheral tissue}}.Elimintation is the…
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Metabolism: {{c1::known as biotransformation, is the conversion of one chemical species into another. (Drug to Metabolite)}}Excretion: {{c1::irreversi…
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Fe + Fm + Fother = 1What do each variable represent?
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Fe (fraction excreted)- Unitless or %- Definition: {{c1::fraction of drug systemically available that is excreted unchanged in urine}}- Measure of how…
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Fm (fraction metabolized):- unitless or %- Defination: {{c1::Fraction of drug systemically available that is converted to a metabolite.}}- Measure of …
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02/06/2024
Extraction ratio (E): Calculated by using (C - Cout)/COR{{c1::E = CLb,organ / Qorgan}}
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02/06/2024
Blood clearance (CLb):- CLb is a measure of the {{c1::body's ability to eliminated the drug}}.- CLb represents the {{c1::theoretical}} volume of blood…
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02/06/2024
Hepatic blood clearance (CLb,h)Blood flow in liver is:Qh = {{c1::81 L/h or 1350 mL/min}}EH= {{c1::CLb,h / Qh}}
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Renal blood clearance (CLb,r)Qr = {{c1::66L/h or 1100 mL/min}}Er = {{c1::CLb,r / Qr}}
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Total blood clearance (CLb) is calculated using:{{c1::CLb,r + CLb,h + CLb,other = CLb}}
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Plasma clearance (CL):- measure of the {{c1::body's ability to eliminate the drug}}.- Represents the {{c1::theoretical volume of plasma}} which is cle…
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02/06/2024
How does ROE relate with Cb/C (how does it relate with plasma and blood in an equation)
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Low Extraction ratio (E) = {{c1::0 to < 0.3}} means F = {{c1::>0.7 to 1}}Intermediate E = {{c1::0.3 to 0.7}} means F = {{c1::>0.3 to 0.7}}Hig…
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02/06/2024
How does elimination rate constant (k) relate with ROE?
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02/06/2024
k = CL/V shows a {{c1::dependency relationship}}. Same goes with C= A/V
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Elimination half-Life (t1/2):- period of time {{c1::required for the amount or concentration of a drug to decrease by half}}.- dependent variable of {…
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List of PK parameters (constant variable not depend on drug concentration) (9 total)
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List of some PK observations (9 total) (changed with drug dosage strength)
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Extravasation: {{c1::tissue uptake from blood}}
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Distribution is rate-limited by: {{c1::perfusion}} or {{c1::permability}}
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The variable Kp,b is calculated by {{c1::Ct/Ca}}
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Distribution rate constant (kt) is defined as {{c1::(rate of leaving)/(Amount of drug in tissue).}}
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Factors that affect kt
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Distrubtion half-life is calculated by
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Tissue concentration (Ct) can be calculated by
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02/06/2024
In a distibution, the time to reach 97% of the max Ct,ss is ....?
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02/06/2024
The normal pH for a human body is
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What species is favored when:1. pKa > pH?2. pKa < pH?
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02/06/2024
Rank the membrane permeability:1. Blood capillaries2. Nasal, lungs, GI3. Blood-brain barrier
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02/06/2024
What is the relationship between V and Kp?
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What are the 3 major plasma proteins? What gets saturated fastest?
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In plasma proteins,Acidic drugs then to bind to {{c1::albumin}}.Basic drugs then to bind to {{c1::AAG}}.It is the {{c1::free or unbound}} drug that ge…
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02/06/2024
Factors that affect fraction unbound:1. {{c1::Ka = binding equilibrium constant between drugs and plasma protein}}2. {{c1::fu,p = fraction of the tota…
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02/06/2024
First generation antihistamines (diphenhydramine) have {{c1::sedative}} effects while second generation (fexofenadine) {{c1::do not}}.This is because …
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02/06/2024
Impact on GFJ (grape fruit juice) on fexofenadine
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02/06/2024
Transporter:Uptake rate = {{c1::Puptake * SA * Cu}}Efflux rate = {{c1::Pefflux * SA * Cu,t}}At steady-state; net movement = {{c1::0}}
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