ADME Flashcards by Ryan Lee

Range between Minimum Effective Conc. and Minimum Toxic Conc.

Therapeutic Window

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__ compounds can readily partition into fat tissue, becoming stored there

Lipid soluble

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__ drugs commonly bind to Albumin

Acidic

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__ drugs commonly bind to Globulins

Basic

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Absorption describes

Rate at which a drug leaves its site of admin, and extent to which that occurs

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Acidification of urine facilitates

Removal of Basic Drugs and Metabolites

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Active Transport: exhibits saturation?

Yes

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Alkalinization of urine facilitates

Removal of Acidic Drugs and Metabolites

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At steady state, acidic drugs will accumulate on more __ side of membrane

Basic

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At steady state, basic drugs will accumulate on more __ side of membrane

Acidic

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Cause of drug accumulation in tissues often arises from

Active transport or binding

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Concentration difference between Minimum Effect Conc. and Peak Plasma Concentration

Intensity of Oral Drug

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Conjugated byproducts of drugs previously metabolized by liver may undergo hydrolysis back to parent in intestines, and be reabsorbed to liver by portal circulation

Enterohepatic Cycling

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Diffusion Coefficient (D)

Inversely related to the size of the drug

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Driving force for drug movement across membrane is

Concentration gradient of non-ionized rug

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Drug binding to plamsa proteins is a ___ process

Saturable and Nonlinear

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Drug types good for Percutaneous

Lipid soluble

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Drugs are absorbed only when

Non-ionized

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Effect of Enterohepatic Cycling on elimination

Decreases elimination rate

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Facilitated Diffusion: exhibits saturation?

Yes

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Falling Phase

(Met + Exc) > Abs

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Fat soluble vitamins (ADEK) get in via

pinocytosis

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Fick’s Law

*-DAK (dC) / dX

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Formula for Vd

Amount of drug administered / Plasma drug concentration

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Fractional extent to which a given dose of a drug reaches either its site of action or a biological compartment from which the drug has free access to its site of action

Bioavailability

Glomerular Filtration Rate is a ___ process

Passive and Nonsaturable

How does gastric emptying affect absorption

Increasing gastric emptying increases absorption

How is GFR often measured clinically

Clearance of Creatinine

How many ATP necessary for CYP

none

If dissolution is slow relative to absorption, then we are concerned with

dissolution

If drug is filtered, but not secreted or reabsorbed, renal clearance will be

120 ml/min

If drug is net reabsorbed, renal clearance will be

less than 120 mL/min

If Phase 1 metabolites are sufficiently polar, they

may be excreted in urine

If renal clearance is < GFR)

Net reabsorption

If renal clearance is >120 mL/min (CLr > GFR)

Tubular secretion must be contributing

If renal clearance is 120 mL/min (CLr = GFR)

Drug is filtered, but not secreted or reabsorbed

If tubular secretion is contributing to elmination, renal clearance will be

greater than 120mL/min

Important consequence of Phase 1 metabolic reactions

Products are often highly reactive and potentially toxic

In non-uniform distribution pattern, the highest concentrations are often present in the

kidney, liver, and intestine

Increasing gastric emptying time will

increase drug absorption

Induction vs Inhibition

Induction increases metabolism of that and/or other drugs

Intensity of Oral Drug

Concentration difference between Minimum Effect Conc. and Peak Plasma Concentration

Ion trapping

Acidic drugs accumulate on more basic side of membrane and vice versa

Large and polar drugs need

carrier

Main conjugation reaction in body

Glucoronidation

Main way drugs get in

Passive Diffusion

Major catalyst of Phase 1 biotransformation

CYP450 family

Major determinant of fraction of drug bound to serum proteins at high conc.

Number of binding sites

Major determinant of fraction of drug bound to serum proteins at low conc.

Affinity of binding sites

Metabolism tends to convert

Active to less active and/or more polar and less lipophilic for excretion

Method of termination other than metabolism, excretion

Redistribution

Michaelis Menten eq.

V = Vmax(S) / (Km + [S])

Most acidic drugs will be __ in the stomach

Non-ionized --> Absorbed

Most drug metabolizing enzymes are found in

ER and Cytosol

Most phase 1 reactions take place in

Most phase 2 reactions take place in

Cytosol

MTC / MEC

Therapeutic Index

Only energy source for CYP

NADPH

Overall renal excretion is controlled by

what happens in tubules

Partition Coefficient (K)

Reflects the lipid solubility of the drug (oil:H2O)

pH Partition Theory

Drugs absorbed when non-ionized --> Higher lipid solubility

Phase 1 reactions usually convert

parent drug to inactive metabolite

Phase 2 reactions lead to

covalent addition of a functional group to parent compound, or to reactive product of phase 1 rxn

Rate at which a drug leaves its site of admin, and extent to which that occurs

Absorption

Reabsorption of weak electrolytes is ___ and therefore dependent on ___

Passive, pH ov urine

Renal capillaries have ___ permeability

greater --> more filtration

Resultant metabolite from phase 2 is usually

more water soluble and less lipid soluble --> less drug reabsorbed from kidney

Rising Phase

Abs > (Met + Exc)

Secretion of electrolytes in proximal tubule is

Active (requires transporter MDR2)

Size cut off for pinocytosis

>25 kD

Stomach traps __ drugs

basic

Substrates for P-Glycoprotein (MDR1)

Chemotherapeutic Agents

Therapeutic Index

MTC / MEC

Tissue binding usually arises thru

interactions with proteins and/or phospholipids

Total blood flow is greatest to

Brain, Kidneys, Liver, Muscle

Transporter in Proximal Tubule

MDR2

Type of drugs that would absorbed in stomach

Acid drugs (wouldn't be ionized)

Type of solution that absorbs quickly subQ

aqueous

Vd greater than 40 means

Concentrated in organ

Vd less than 4 means

Plasma

Vd of 40 means

Uniform

What body position decreases gastric emptying

Lying on left

What drugs decrease gastric emptying

Anticholinergics, Narcotics, Analgesics

What is excreted in Proximal tubule

Weak electrolytes

What is passively transferred in Distal Tubule

Lipid Soluble drugs

What size is considered low MW

100-200 Da

What type of meal decreases gastric emptying

Fatty

What type of molecules can be reabsorbed in distal tubules

Nonionized (lipid soluble) forms of weak acids/bases

Where does Glucoronidation occur

Liver

Which variable of Fick's law does ionization affect?