Term
| What does an increased V(d) imply? |
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Definition
that the drug will stay in the body longer.
V(d) = drug in body / drug in blood |
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Term
The Liver has two important drug metabolizing systems: 1)Cytochrome P450 2) UDP-Glucurinyl Transferase |
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Definition
—1)Cytochrome P450 — —2) UDP-Glucurinyl Transferase — — —1)_ Fe – Heme monooxygenase enzyme assoc with NADPH -- - req NADPH and Oxygen — —CYP’s also involved in endogenous metabolism )STEROIDS) — —------------------------------------- —2) forms glucuronic acid conj. |
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Term
***What drug competes for Penicillin's Transport mechanism in the kidney, thereby retaining it in the body? |
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Definition
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Term
In order to treat a drug overdose, we can alter Urine PH: 1) Acidify Urine 2) Alkalinize urine |
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Definition
1) Enhances excretion of BASIC DRUGS 2) Enhances excretion of ACIDIC DRUGS |
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Term
Biotransformation of a drug most generally leads to: |
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Definition
| A decrease in the duration of drug in body |
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Term
An Acidic Drug (pka 3.4) is going to be more: (Ionized/NonIonized) At pH 8.9? |
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Definition
ionized *** BASIC DRUGS WILL IONIZE TOWADS ACID ACID DRUGS WILL IONIZE TOWARDS BASIC*** |
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Term
| A basic drug will be more inonized or nonionized at PH 9.9? |
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Definition
more nonionized *** BASIC DRUGS WILL IONIZE TOWADS ACID ACID DRUGS WILL IONIZE TOWARDS BASIC*** |
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Term
| what is the relationship between pka and ionized:nonionized ratio? |
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Definition
at pH = PKA, the ration is 1:1 for every unit of pH away from PKA, the ration increases 10 fold acid drugs ionize at basic cond basic drugs ionize at acid cond |
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Term
| Acidic drugs tend to conc. on which side of the conc. gradient over a memb? |
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Definition
Acid --> HIGH PH - BASIC Basic --> Low PH - ACIDIC |
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Term
| What is required to get a net transfer of drug across a memb barrier by passive diffusion? |
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Definition
a higher conc of NONIONIZED drug on one side of memb
the MORE LIPOPHILIC, the FASTER it diffuses |
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Term
A first order elimination process follows a ________ elimination A ZERO order elimination follows a _______ elimination ---This occurs WHEN? |
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Definition
1) Logarithmic elimination 2) LINEAR -- OVERDOSE SITUATION -- when the tp system is SATURATED |
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Term
Clearance (ml/min) formula: 2) What is the glomerular filtration rate? 3) hepatic? |
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Definition
D / AUC D=Tissue distribution AUC = Area under curve 2) 125 ml/min 3)1500 ml/min ***If a drug is expelled by kidney, and the clearance exceeds 125 ml/min, it is beacuse of SECRETION |
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Term
| ***It takes ___ half-lives to reach the steady state*** |
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Definition
4 The same is true any time the dose is altered ALL DRUGS |
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Term
Difference between
Clearance
Half-Life
Volume of Distribution |
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Definition
CLEARANCE - measures TOTAL EFFICIENCY by which the body removes a drug
Half- Life expresses the rate by which a drug is removed from body
Vol of Dist -- How much drug is in tissue vs blood |
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Term
| _____ is the sole determinant of the time it takes to reach steady state in blood conc. |
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Definition
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Term
| ____ can help reach therapeutic range, but not steady state conc faster |
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Definition
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Term
| Loading dose can help reach ------, but not ------ faster |
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Definition
therapeutic range
teady state conc |
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Term
| Blood conc at _______ are governed by DOSE, dose interal, halflife, bioavailability, and vol of distribution |
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Definition
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Term
The RATE OF CLEARANCE in:
Renal eliminated drugs are governed by ____
Hepatically eliminated drugs _____ |
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Definition
1) Completely by kidney func.
2) MAINLY by activity of metabolizing enzymes |
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Term
| _____ = Due to allelic variation at a single gene |
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Definition
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Term
| due to variations at 2 or more genes |
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Definition
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Term
| frequently occurring monogenic variants occurring at a frequency >1% |
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Definition
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Term
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Definition
single nucleotide polymorphism
over 2 million in human genome
(mutation at a single gene) |
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Term
Codeine is useless as a painkiller in 10% of the pop B/c _________.
The anticancer drug 6-MERCAPTOPURINE (AZATHIOPRINE) is toxic in a small fraction of the pop bc ____ |
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Definition
rapid metabolism through CYP2D6
MONOGENIC INHERITANCE OF THIOPURINE METHYLETRANSFERASE (TMPT) |
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Term
| The breast cancer drug _____ is only effective in cancer cells that overexpress HER2 gene |
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Definition
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Term
| The right drug -- for cancer is influenced by enzyme ___ |
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Definition
TPMT -- Thiopurine methyltransferase
Low TPMT = increased thiopurine toxicity and increased risk for secondary cancer
HIGH = decreased theraputic effect |
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Term
| the most perscribed drug in the world, that treates cardiovascular dz is: |
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Definition
STATINS -- HMG CoA Reductase Inhibitors
Reduces "bad" cholesterol in bloodstream. |
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Term
| __2___ = gene affectin Warfarin |
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Definition
VKORC1
Warfarin exerts its pharm affect by inhibiting VKORC1, which is the vit K cycle enzyme controlling the regeneration of of reduced vit K -- essential for clott form.
VKORC1 mutation can cause Warfarin RESISTANCE
CYP2C9 gene mutation = SENSITIVITY |
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Term
| why do redheads need more anesthetic? |
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Definition
red hair assoc with melanocortin 1 receptor that encodes melanocyte stim hormone involved in MELANOGENESIS
MC1R gene involved with complex neuromodulatory regulation within the CNS |
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