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45 Cards in this Set
- Front
- Back
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What is the formula for
CLint Explian the components |
Vmax / km
Vmax: is increase w making more enzymes km: is a dissociation constant, change affinity of active site, change configuration by increasing Km |
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CL hepatic formula is
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LBF* E
Vmax / (km+C) if km >> C , cancel C |
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Css, avg, po formula is
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(F*d/tau)/ CL
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What will cause changes in Css?
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a) disease state
b)fb bcoz of malnutrition c)drug interaction (induction, inhibition) |
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C free = ?
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C tot* fb
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ffp =?
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= 1-E
= LBF / (LBF+Clint*fb) slove for E and get 2nd eq. |
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What is webstern law of clearance?
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E = CLint*fb / (LBF + Clint*fb)
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What is E related to?
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ffb, CLint, LBF
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For M M theory
what is clearance? Explain the graph of dose vs Cl |
CL = F*D / (AUC)
related to Ke = CL / V neagtive line: slope is -km, y axis intersect is Vmax |
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For IV, what is Css?
What is Co for IV? |
Css = ko / CL
Co = C e -(ke*t) |
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H2O soluble drug eliminated by
Lipid soluble drug eliminated by |
H2O: kidneys
Lipid: liver |
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What r criterias for Low E drugs?
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a) 100 % CLh
b) LBF >> CLint*F c) Not dependent on LBF |
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ko / (Clint*fb)
(fabs*ffp*D/tau) / (Clint*fb) |
For low E drugs
CL hep~CLint*fb APPROXIMATION |
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ko / LBF ( (or CL h))
(ffb*fabs*D/tau) / LBF (or CL h) |
For High E drugs
CL hep~LBF ROUTE/flow DEPENDENT APPROXIMATION |
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Equations forCss in IV & po, avg
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Css, iv = ko / CL tot
Css, avg, po = (fabs*ffp*D/tau) / {LBF*Clint*fb / (LBF+Clint*fb)) |
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T or F
For high and low E drugs, LBF is needed. Explain why Inhibition is major in High E drugs, not so much induction by po |
T: LBF is not needed. Do not show in either eq. for Css, avg, PO only
True, induction is almost not possible, too much destroyed by ffp |
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With HIGH E, 100% CL hep, PO, Css =?
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Css = (fabs*D/tau) / CLhep (LBF)
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With LOW E, 100% CL hep, PO, Css =?
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Css = (fabs*D/tau) / (CLint*fb)
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What is considered high or low E?
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low 0 to 0.3
high 0.7 to 1 |
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T or F
HF results in low blood flow output which decreases blood flow to eliminating organ. |
T
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T or F
a)Clearance is not always additive b) negative clearance denotes Cl filtered c)Tubular secretion is passive and no need for carriers d) all drugs r filtered to some extent e) Bound drug is filtered |
a) F, always
b) F, Reabsorption c) F, active d) T e)F, only unbound |
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Renal mechanism is composed of what renal process?
What is a good indication of kidneys pwerformance? |
Secreted & filtered
Creatine cl, cleared by kidney primarily and not protein bound |
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Factors that affect efficiency of CL Reab in kidneys
Explain E=1, E>1, E<1 in kidneys |
Lipid
ionization (pH, pKa) urine flow filtration, filtration & secretion, Filtration & reabsorption |
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if u want to change Cl sec & Cl reab, what should u do?
most accurate renal fnc test... most convenient ,, ,, ... |
Cl sec:change carrier sites
Cl reab: change the flow or pH ou urine accurate: inulin(sugar) conve: creatinine |
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T or F
E=1 means Secr is balanced by Reabs what is E used for? |
T, 1% of the time
used for manipulation to alter Css(extent t1/2 of drug) & predict drug interaction |
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HIGH E with low LBF is ,,,,,,,
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NEVER simplified, wRONG WAY
Po must show constant [], while IV shows route dependence for [] |
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Formula for 24 hr urine collection
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(Ucr * Vur) / (Scr * T)
very accurate |
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What r the rules for Cockroft and Gault?
What is the formula for it? |
Adults only
Not for Obese: ABW/IBW<1.3 Stable Serum Creatine > 65 y/o patients, adjust to 0.8 memorize formu. |
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Which CrCl formula is for Obese patients?
What is the formula? |
Salazar and Corcoran
memorize formu. |
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Explain the advantage and disadvantage of MDRD
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Good for finding kidney disease
Not good for patients on drug, false result, Over estimate CrCL |
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a)What is considered normal GFR
b)Modest low c) moderate low d)substantial low |
a) 120ml/min
b)50-60 ml/min c) 25-30 d)< 15 decr dose, or incr interval or both: always adjust to not destroy the acid-base or electrolytes balances |
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What is the difference between Intact nephron hypothesis & in vivo models
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nephron: all segments r affected EQUALLY
In vivo: GFR and tubular declines in a nonparallel manner |
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Drug metabolism with renal failure is associated with what?
which drugs r most susceptible? |
smoking, etOH, age, currnet drug intake, inhibition of P450's becoz of pH changes
b) high E |
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Effect of renal disease on Vd
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1) increase mostly Vd (can't pee), may also decrease
2) decr. protein binding hypoalbuminemia, pH imbalance, prob in binding sites, affinity changes 3) alterded tissue binding (fb/ft) |
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What aspect of ADME does renal disease affect?
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all and affect other organs(liver)
A(bioavaliablity) D(Vd, protein binding) M (liver because of pH imbalanced) E (renal elimination) AUC, Cmax, Tmax, CL, Vd, F, fb |
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Normal gestation is...
gastric acid in premature infant is... neonates reach normal level at... |
36-40 wk
more acidic than full term infants 2 y/o |
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acid labile r...
example of acid labile drugs r... how do u adjust it in pediatric... What about weak acid? |
destroyed in acid environment
Penicillin, amoxicillin increase dose in premature since higher acid level But decrease dose in full term W.A. absorbs more in acidic env. so less is needed |
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intestinal motility in pediatric is...
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decreased, so they absorb easily, need less dose,
food increase motility, so may need more |
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GastroIntestinal enzymes r not developed fully, expect...
exception is |
higher F, less drug needed
Digoxin, need flora to become to active form |
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biliary fnc matures months after birth, expect...
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drug with high lipid solubility not readily absorb, low bile acid
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gastric emptying in neonates is responsible for drug...
Absorption depend on ... |
delaying, more time to reach Cmax
age and physical development |
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What model of administration shoud be avoided in neonates? Why
What is a neonate TBW? ECW is a clue for... |
IM, they r bags of H2O, no muscle tone, no friction in the area/ contractility
Rectal admin., they poop it out but F may increase Transdermal absor is higher, may be dangerous lowest amount on face and groin area 92% aminoglycosides, important becoz they have 50% ECW |
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What is the driving force for Vd?
Neonates increase or decrease in: H2O Fat Proteins endogenous |
free drug
increase, dec., dec., inc. |
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Septriaxon, Sulfa & phenytoin...
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r highly protein bound and use bilirubin to move in pediatric, Dangerous causes jaundice & Brain damage
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High water solubility= ex.
high lipid solubility= ex. |
= larger Vd in infants, higher dose, ex. gentamicin
= small Vd in infants, ex. bezodiazepines |
