Pharmacokinetics

Beth Walton
Mind Map by , created over 5 years ago

Mind Map on Pharmacokinetics, created by Beth Walton on 05/25/2014.

49
1
0
Tags No tags specified
Beth Walton
Created by Beth Walton over 5 years ago
drug distribution
jjschneider
renal drug elimination
jjschneider
Antithrombotic Flashcards
Justice Mundy
Main Themes in Romeo and Juliet
Carlowl
GCSE Biology B2 (OCR)
Usman Rauf
Pharm I Exam 1
paigembrennan
Phamacodynamics and Pharmacokinetics
offersforalice
Pharmacokinetics-PHAR2102
jjschneider
Pharmacology: Exam 1
Beata Izmailov
Tablets
Jack Willach
Pharmacokinetics
1 Absorption
1.1 Transfer from site of admin to systemic circulation
1.2 Increase SA = Increased speed of A
1.3 Aq vehicle - Rapidly A
2 Elimination
2.1 Metabolism
2.1.1 Phase one
2.1.1.1 Oxidation
2.1.1.1.1 Hydroxylation
2.1.1.1.2 Epoxide
2.1.1.1.3 Dealkylation
2.1.1.1.4 Deamination
2.1.1.2 Reduction
2.1.1.3 Hydrolysis
2.1.2 Phase Two- conjugation
2.1.2.1 Sulphation
2.1.2.2 Glucuronidatiom
2.1.2.3 Amino Acid
2.1.2.4 Acetylation
2.1.2.5 Methylation
2.1.3 Phase three
2.1.3.1 Cytochrome P450
2.1.4 Kinetics

Annotations:

  • A. -->. A(m). --> Ae(m)     Km.         K(m)
2.2 Excretion
2.3 Irreversible removal of drug from the body
2.4 Clearance
2.4.1 Total CL=Hepatic CL + Renal CL+ other CL
2.4.2 CL=QxE
2.4.2.1 <90L/hr , (1.5L/min)
2.4.2.2 High E drug
2.4.2.2.1 CL=Q
2.4.2.3 Low E drug
2.4.2.3.1 CL=CLint x Fu
2.4.3 CL=Dose/AUC
2.4.4 CL=KV
2.4.4.1 T1/2=ln2V/CL
2.4.5 Independent of plasma conc, dependent on efficiency
2.4.5.1 First order kinetics
2.4.5.1.1 Rate=Vmax x C / Km + C
2.4.6 Vol of plasma/blood completely cleared of drug in a given time.
2.4.7 Greater CL -> smaller AUC, shorter t1/2, same V
2.4.8 Renal CL= GFR x Fu
2.4.8.1 125mL/min
2.5 Rate of E= CLxPlasma conc.
2.5.1 Extraction ratio= rate of E/ presenting conc.
2.5.1.1 Extraction Ratio= (Cart - Cven)/ Cart
2.6 Bioavailable fraction (F)
2.6.1 CL=FDose/AUC
2.6.1.1 AUC only changed by absorption not by rate
2.6.2 IV: 1
2.6.3 Fraction of unchanged drug that reaches systemic circulation
2.7 Major - liver M, biliary Ex ! Kidney, urinary M&Ex
2.8 Minor - lung M, breath Ex, breast milk, skin, alimentary tract
3 Distribution
3.1 Transfer from one compartment to another
3.2 V (L)
3.2.1 Vi, Vss
3.2.1.1 Vss=Vp + Vt x (Fu/Fut)
3.2.2 Vol of blood needed to account for the total amount of drug in the body
3.2.2.1 Amount=Volume x Conc
3.3 One compartment model
3.3.1 Instantaneous distribution
3.3.2 V is constant
3.3.3 K=E rate constant
3.3.4 Enter text here
3.3.5 1st order
3.3.5.1 Rate=Rate constant x amount
3.3.5.2 Rate of e= CL x Conc
3.4 Two compartment model
3.4.1 D equilibrium not instantaneous
3.4.1.1 V increases with time until D equilibrium reached
3.4.2 AUC=A/a + B/b
3.5 Central
3.6 Peripheral
3.7 CO=6L/min
3.8 Q= blood flow
3.8.1 Lungs = 10ml/min
3.8.2 Fat = 0.03ml/min
3.8.3 HBF~ 1.5L/min
3.8.4 Portal BF ~ 1.2L/min
3.8.5 Artery ~0.3L/min
3.8.6 Bile flow ~ 0.5mL/min
3.8.7 Increased by massage and excercise. A is the rate cntrolling step.
3.9 Multi compartment
4 Routes
4.1 Injections
4.1.1 Iv
4.1.2 Intra Arterial- targets specific organs
4.1.3 Spinal - drugs that don't cross the BBB. Not systemic. ABs, analgesics, antineoplastics
4.1.4 Intraperitoneal - high vascularity, large SA. Lipophilic absorbed quickly but variable. Some HFPM. Local targettng, A not complete
4.1.5 Intramuscular- High vascularity, variability between diff muscles. Deltoid 10.2 mcg/ml , GM 4.3, Vastus Leteralus 9.2
4.1.6 Avoid HFPM
4.1.7 Subcutaneous- Moderate vascularity, Q increased by heat + massage. Q is the ARL step. Limited fluid for dissolution. Local E activity; low. Mild pH
4.1.8 Intradermal - V. poor vascularity, small SA. Variable permeability. Local E activity: low. A increased by heat and hydration