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20 Cards in this Set

  • Front
  • Back

Absorption

-passage of intact drug from administration site into systemic circulation

Distribution

-Reversible movement of drug between systemic circulation and the tissues

Metabolism

-Irreversible enzymatic alteration of the drug

Excretion

-Irreversible passage of the drug/metabolite out of the body

Absorption Rate Constant (Ka)

-primary PK parameter


-dependent on:


blood flow,gastric emptying, GIT motility

Oral Bioavailability (F)

-primary PK parameter


-dependent on:


gastric emptying, acid secretion,enzyme activity, GIT motility

Hepatic Clearance (Cl H)

-primary PK parameter


-dependent on:


hepatic blood flow, binding in blood, intrinsic clearance

Renal Clearance (Cl R)

-primary PK paramter


-dependent on:


renal blood blow, fraction unbound drug, active secretion/reabsorption

Volume of distribution (Vd)

-primary PK parameter


-dependent on:


fraction unbound, tissue binding, body composition size

Elimination of half-life

-secondary PK parameter


-dependent on primary PK paramters --> Vd and Cl S

Elimination rate constant

-secondary PK parameter


-dependent on Vd and Cls

Fraction excreted unchanged

-secondary PK parameter


-dependent on Cl R and Cl S`

Oral Dosing



Advantages:


convenience of administration


cheap


avoidance of high toxic concentrations




Disadvantages:


inefficient (erratic bioavailability)


first pass effect

Buccal/Sublingual

Advantages:


by-pass the liver --> first-pass effect


rapid absorption


drug stability




Disadvantages:


small concentrations


inconvenient/discomfort

Rectal

Advantages:


by-pass the liver


avoid GIT side effects




Disadvantages:


erratic absorption


patient compliance

Parenteral Route - Intravenous



Advantages:


rapid onset


total dose




Disadvantages:


hard to find vein


trained personnel


high Cp --> toxicity possibility

Parenteral Route - subcutaneous

Advantages:


self-administered


slow but complete absorption




Disadvantages:


can be painful


smaller doses

Parenteral Route - intramuscular

Advantages:


rapid absorption


a depot effect possible




Disadvantages:


erratic absorption


trained personnel

Noyes-Whitney Equation

dC/dt = (D/h) (S) (Cs -C)




dC/dt - rate of dissolution


D - diffusion coefficient, affected by temp


h - width of diffusion layer, affected by agitation


s - surface area of the drug, affected by particle size (smaller size --> incr. SA)


Cs - drug conc in diffusion layer


C - conc in bulk solution

What are factors that affect the pH of the drug environment?

-dosage form ingredients


-salt form of drug


-region of GIT


-disease


-co-administered drugs