Pharm- Drug Elimination.txt

The sum of chemical reactions in which an endogenous or exogenous substrate is converted into a larger molecule or a smaller molecule.

Metabolism plays an important role in the ________ and ________ of drugs.

Kidneys provide a concentration gradient which favors...

The development of metabolic pathways renders lipid-soluble materials that would normally be resorbed back into the blood at the kidneys...

The primary site for drug metabolism.

The system of enzymes located on the smooth endoplasmic reticulum that is the primary site for drug metabolism and endogenous steroid metabolism.

A hyperbolic curve that provides estimates of maximal reaction velocity (Vmax) and the apparent Km.

What is phase I of drug metabolism?

Phase of drug metabolism that transforms the molecule to a more polar product which then may be excreted.

What are phase II reactions of drug metabolism?

The phase of drug metabolism in which the addition of a conjugate increased the polarity of the drug molecule and the size, making is much less likely to be resorbed at the kidney.

Phase ___ products sometimes retain biological activity, but Phase ___ products are rarely active.

The primary phase I reactions, _________ and __________, are carrier out by the __________, which requires... (3)

The phase II reactions are _______ in nature; they can be limited in their rate or capacity by... (2)

Metabolic transformation can result in... (3)

Acetominophenis a(n) ________ that is metabolized to a(n) ____________, which leads to ____________.

Benzo[a]pyrene is a(n) ___________ that is metabolized to a(n) ____________, which is ___________.

Two important properties of drug metabolism are...

When one drug stimulates or induces enzymes for its own metabolism and the metabolism of the other.

With enzyme induction, the dosage of the second drug will need ____________.

When one drug competitively or non-competitively inhibits the metabolism of another drug.

The u=inhibited drug may require that its dosage rate be __________ to __________.

With enzyme induction, when an active drug is metabolized to an inactive molecule, you need ________ drug.

With enzyme inhibition, when an active drug is metabolized to an inactive molecule, you need ________ drug.

With enzyme induction, when an inactive drug is metabolized to an active molecule, you need ________ drug.

With enzyme inhibition, when an inactive drug is metabolized to an active molecule, you need ________ drug.

The ________ is principally responsible for drug excretion.

Many polar drugs depend on excretion of the ________, __________ form of the drug as the main means of elimination.

There is significant _____________ in herbivores.

There is significant __________ in the lactating female.

The kidney functions ___________ to maintain body fluid composition and balance.

What are the steps of filtration in the kidney? (5)

The glomerular membrane acts as a filter, allowing _________ and _________ of the plasma to enter the nephron, while excluding ________ and ________.

Filtration through the glomerulus is driven by _____________.

The processes of _________ and ________ modify the tubular fluid in the tubule.

Active transport mechanisms occur primarily in the _________ of the kidney.

Most ________ solutes diffuse passively from higher concentration within the tubular fluid back to the blood via peritubular capillaries.

Drugs that are _____________ are not filtered at the glomerulus but are secreted by active transport.b

__________ accounts for the retention of many lipid-soluble substances, but substances that do not easily diffuse across membranes can be resorbed by _____________.

The rate of renal excretion of a substance is summarized by what 3 processes?

The volume of blood which would be required to contain the amount drug which is removed per unit of time; the rate of removal from thhe total body or from a specific organ.

Changes in ___________ or _____________ will affect a drug dosage schedule.

Two clearance mechanisms that are related to renal drug elimination.

A substance which is almost completely removed in one passage through the kidney can be used to measure ________.

As clearance increases, half-life _______.

As volume of distribution increases, half-life ________.

Inulin is only cleared by _________.

If clearance ratio is <1, _________ has taken place.

If clearance ratio = 1, then ___________.

If clearance ratio > 1, __________ has taken place.

Drugs that are weak acids or bases will ____________ from the ___________ to the __________.

If the concentration of drug exceeds the capacity of the transport system, then __________ occurs and the rate of _________ becomes limited.

If a drug is excreted by filtration but not secretion, then only ___________ is available for filtration and excretion. If a second drug competes with the first for protein binding so that more drug is _______________, the rate of excretion of the first drug will _________.

If a drug is protein bound and also actively secreted so that not only free drug but also bound drug become cleared as it passes through the kidney, if you cause less drug to be bound, excretion can be ________.

Diuretic drugs __________ drug excretion by.... (2)

Drugs which are extensively and rapidly removed by the liver following oral administration undergo ____________.

Drugs enter the bile by a ____________.

The proportion of drug in the bile compared to the urine increases as ____________ increases.

Dogs, rats, and chickens are classified as _______ excreters; cats and sheep are ___________ excreters; rabbits, guinea pigs, and primates are ________ excreters.

Unmetabolized drug secreted in the bile to the intestine ill undergo reabsorption according to its ______________; drug that are __________ at the pH of the intestine will not be reabsorbed; ___________ drugs will largely be reabsorbed back into circulation.

The major difference b/w renal and hepatic excretion is that...

Extraction ratio (E) > 0.7 refers to those drugs which are __________ (i.e most drugs undergoing ____________); E <0.3 refers to drugs with ___________.

Drugs with low extraction ratios are referred to as ____________ and depend on the _______________.

Drugs with low extraction ratios are cleared independently of _____________ but are sensitive to ____________ because clearance is limited to ____________.

Drugs with high extraction ratios are capable of ___________; they have _________-limited clearance and are not sensitive to ______________.

Drug elimination by milk, saliva, and perspiration are all primarily dependent on ____________ and _____________.

With systemic treatment for mastitis, ___________ tend to concentrate in the mammary gland more than ________.