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Pharmacology > Pharmacokinetics & Pharmodynamics > Flashcards

Pharmacokinetics & Pharmodynamics Flashcards

1
Q

In terms of the modified occupancy theory, an agonist is a drug that has both affinity and high intrinsic activity. ____ allows the agonist to bind to receptors, and______ allows the bound agonist to activate or turn on receptor function.

A

Affinity

Intrinsic activity

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2
Q

an antagonist is a drug with affinity for a receptor but with no ____ _____

A

intrinsic activity

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3
Q

Because antagonists act by preventing receptor activation, if there is no ____ present, administration of an antagonist will have no observable effect; the drug will bind to its receptors, but nothing will happen.

A

agonist

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4
Q

When the receptors of a cell are continually exposed to an agonist, the cell usually becomes less responsive. When this occurs, the cell is said to be desensitized or refractory or to have undergone __________

A

down-regulation

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5
Q

What does it mean if a drug has a high therapeutic index?

A

A high therapeutic index indicates that the effective dose of the drug is significantly lower than the toxic dose. In other words, there is a wide range of doses between the minimum effective dose and the dose at which toxicity occurs. This allows for a greater margin of error in dosing and reduces the risk of adverse effects.

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6
Q

What does it mean for a drug to be safe?

A

A safe drug is defined as one that cannot produce harmful effects—even if administered in very high doses and for a very long time.

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7
Q

Why is ease of administration important?

A

In addition to convenience, ease of administration has two other benefits: (1) It can enhance patient adherence, and (2) it can decrease risk

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8
Q

What does it mean for a drug to be selective?

A

A selective drug is defined as one that elicits only the response for which it is given. There is no such thing as a wholly selective drug because all drugs cause side effects

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9
Q

What does it mean if serum creatinine is elevated?

A

If creatinine level is HIGH, the kidney is not working well. It is unable to filter creatinine

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10
Q

What does it mean if creatinine clearance is low?

A

The kidney no so good

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11
Q

What does GFR stand for?

A

glomerular filtration rate: this is the number of mL/min the kidney can filter

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12
Q

What are signs the liver is not working well?

A

abdominal pain
loss of appetite
jaundice

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13
Q

What does LFT stand for in the context of liver function?

A

Liver Function Test

Liver function tests are a group of blood tests that are used to assess the functioning and health of the liver. These tests measure various enzymes, proteins, and substances in the blood that are indicative of liver function and any potential liver damage or disease

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14
Q

Rank the most common routes of administration from highest to lowest ease of absorption

A

IV

Inhalation

Intramuscular (IM)

Subcutaneous (SubQ)

Oral (PO)

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15
Q

The phenomenon in which drugs that are taken orally (PO) are metabolized by the liver before they reach systemic circulation.

When a drug is absorbed through the gastrointestinal tract, it travels to the liver via the portal vein. In the liver, enzymes can metabolize or inactivate a portion of the drug before it reaches the systemic circulation.

A

First Pass Effect

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16
Q

blood-brain barrier

A

The blood-brain barrier (BBB) is a highly selective and protective barrier that separates the circulating blood from the brain tissue. It is formed by specialized cells and structures that tightly regulate the passage of substances from the bloodstream into the brain and spinal cord.

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17
Q

This drug contains inactive or less active compounds that are designed to undergo specific biochemical transformations in the body to become the active drug

A

Prodrug

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18
Q

These transporters actively pump certain substances out of the brain

A

Efflux transporters - most important is P-glycoprotein (P-gp)

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19
Q

Which drugs can cross the blood-brain barrier?

A

-Lipid soluble (ex: benzos, opioids, anesthetics)
-Small (ex: caffeine)
-Prodrugs (ex: L-DOPA)
-Efflux transporter substrates (ex: rifampin)

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20
Q

why does the blood brain barrier make it difficult to treat meningitis?

A

The blood-brain barrier (BBB) poses a challenge in treating meningitis because it restricts the penetration of many medications into the central nervous system (CNS), including the brain and spinal cord. In meningitis, the infectious agents typically reside within the cerebrospinal fluid (CSF) or invade the meninges directly. As a result, medications need to cross the BBB to reach the site of infection and effectively combat the pathogens.

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21
Q

Many drugs have a tendency to bind to proteins, particularly ______, which is the most abundant protein in the blood.

A

albumin

22
Q

When a drug is highly protein-bound, it means that a significant portion of the drug molecules in the bloodstream are bound to proteins, leaving only a fraction of the drug molecules in their unbound or_____ form.

A

free

23
Q

What happens to free drug levels when another highly-protein bound drug is introduced?

A

Increases free drug levels –>
-Enhanced Pharmacological Effects
-Increased Potential for Drug Interaction
-Altered Drug Clearance

24
Q

Refers to the study of how the body processes a drug, including its absorption, distribution, metabolism, and excretion

A

Pharmacokinetics

25
Q

Refers to the movement of a drug from its site of administration into the bloodstream

A

Absorption

26
Q

What does a CYP450 enzyme inducer do?

A

It “revs up” or “induces” the liver, and therefore levels of other drugs the patient is taking when the inducer is started will decrease

27
Q

What does a CYP450 enzyme inhibitor do?

A

It “slows down” or “inhibits” the liver from metabolizing, and therefore levels of other drugs the patient is taking when the inhibitor is started will increase

28
Q

In a general way, understand the differences between the different routes of absorption. Compare PO, transdermal

A

ADD

29
Q

How many half-lives does it take for a drug to reach a plateau? (Where the rate of drug elimination equals the rate of drug administration)

A

It takes 4 half-lives for a drug to reach a plateau

30
Q

The time required for the concentration of a drug to reduce by half

A

half-life

31
Q

The range of drug concentrations in the body that is considered effective and safe for achieving the desired therapeutic effect

A

Therapeutic range

32
Q

The occurrence of adverse or harmful effects when drug concentrations exceed the therapeutic range

A

Toxicity

33
Q

What type of monitoring is often done for drugs with small therapeutic windows?

A

Drugs with small therapeutic windows often require close monitoring of drug levels in the blood to ensure they are within the desired range. Additionally, monitoring for signs and symptoms of toxicity and assessing relevant laboratory parameters may be necessary.

34
Q

The initial higher dose of a medication given at the beginning of treatment to rapidly achieve the desired drug concentration in the body.

A

Loading Dose

35
Q

Would a change in the pH of the stomach would affect the absorption of aspirin (an acidic drug)?

A

Aspirin is an acidic drug, and changes in stomach pH can affect its absorption. Lowering stomach pH (increasing acidity) can enhance the absorption of acidic drugs like aspirin.

36
Q

Consider how altering the pH of the urine (making the urine more basic) might hasten excretion of aspirin in overdose.

A

Altering the pH of urine to be more basic (alkaline) can increase the excretion of acidic drugs like aspirin (this is helpful for overdose)

37
Q

A specialized macromolecule located on or within a cell that binds to specific substances, such as drugs, hormones, or neurotransmitters. Binding to these substances triggers specific cellular responses.

A

Receptor

38
Q

Subtle differences in receptors make selectivity possible. Why are selective drugs desirable?

A

Selective drugs are desirable because they target specific receptors in the body, leading to more specific therapeutic effects while minimizing unwanted side effects. Selectivity allows for the modulation of specific physiological processes without interfering with others.

39
Q

A drug that binds to a receptor and activates it, resulting in a biological response. It mimics the action of endogenous substances and produces a similar effect

A

Agonist

40
Q

A drug that binds to a receptor but does not activate it. Instead, it blocks the receptor from being activated by agonists or endogenous ligands, thereby inhibiting their effects

A

Antagonist

41
Q

A ____ agonist is a drug that binds to a receptor and activates it, but with less intensity or efficacy compared to a full agonist. They can produce a partial response, even in the presence of a full agonist.

A

partial

42
Q

A ___ _____ medication is a medication that needs to be administered within a specific time frame (usually 30 minutes) to achieve its desired therapeutic effect or prevent harm. It must be given promptly as prescribed to ensure optimal patient outcomes.

A

time critical

43
Q

How do most drugs pass the cell membrane?

A

Direct penetration

44
Q

A phenomenon where ionizable drugs distribute differentially across biological membranes based on the pH gradient. It occurs when a drug exists in different ionized and non-ionized forms, leading to accumulation in compartments with pH conditions favoring its ionization.

A

Ion trapping / pH partitioning

45
Q

All the following are factors that can affect _______

Lipid solubility
Rate of dissolution (how fast a pill dissolves)
Surface area
Blood flow
pH partitioning

A

absorption

46
Q

PO medication that is covered with material that dissolves in the intestines, not stomach

A

enteric-coated preparation

47
Q

a drug that is released steadily over the day

A

sustained-release preparation

48
Q

An important family of enzymes that metabolize drugs

A

The P450 system

49
Q

What are the therapeutic consequences of drug metabolism?

A

-Accelerated renal drug excretion
-Drug inactivation OR activation (prodrugs)
-Increased therapeutic action
-Increased or decreased toxicity

50
Q

What are the 3 steps of renal drug excretion?

A

1) Glomerular filtration
2) Passive tubular reabsorption
3) Active tubular secretion

51
Q

What molecules can go through glomerular filtration?

A

-Small molecules can pass
-Proteins and protein-bound cannot

Pharmacology (21 decks)

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