ADME - Sheet1 Flashcards

1
Q

What is absorption in pharmacokinetics?

A

The movement of a drug from the site of administration into the blood.

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2
Q

What determines drug action during absorption?

A

The rate and amount of absorption.

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3
Q

What happens with a higher absorption rate?

A

Faster onset of drug effects.

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4
Q

What happens when a drug is absorbed quickly and well?

A

It produces effects quickly and elicits a better response.

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5
Q

What factors affect absorption?

A

Rate of dissolution, surface area (e.g., villi), blood flow, lipid solubility, and pH partitioning.

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6
Q

What are the routes of administration under absorption?

A

Enteral (via GI tract), parenteral (by injection), and other routes.

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7
Q

What does “enteral” refer to?

A

Administration via the GI tract, including oral (PO), NG tubes, and gastrostomy tubes.

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8
Q

What forms of medication are administered enterally?

A

Tablets/capsules, enteric-coated, sustained/extended-release, sublingual, and liquids/solutions.

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9
Q

What does “parenteral” refer to?

A

Administration by injection, such as IV, IM, and subcutaneous routes.

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10
Q

What are some other routes of drug administration?

A

Topical, transdermal, inhaled, suppository (rectal or vaginal), and direct injection (e.g., heart, joints, nerves, CNS).

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11
Q

What is distribution in pharmacokinetics?

A

The movement of drugs through the body after absorption.

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12
Q

What are the three factors determining drug distribution?

A
  1. Blood flow to tissues, 2. Exiting the vascular system, 3. Entering cells.
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13
Q

What is metabolism in pharmacokinetics?

A

The process of altering the structure and function of drugs, nutrients, vitamins, and minerals.

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14
Q

Where does most drug metabolism occur?

A

In the liver.

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15
Q

What is the role of hepatic microsomal enzymes?

A

They metabolize drugs, with cytochrome P450 (CYP) being the primary enzyme group.

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16
Q

How does the CYP system help eliminate drugs?

A

By making them water-soluble so they can be excreted by the kidneys and urine.

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17
Q

What are the three roles of drugs in the CYP system?

A
  1. Substrates (rely on CYP for metabolism), 2. Enzyme inhibitors (block CYP activity), 3. Enzyme inducers (accelerate metabolism).
18
Q

What happens when a drug acts as a CYP enzyme inhibitor?

A

It can lead to toxic drug levels by preventing metabolism of substrate drugs.

19
Q

What happens when a drug acts as a CYP enzyme inducer?

A

It accelerates metabolism, decreasing drug levels and potentially reducing effectiveness.

20
Q

What is the first-pass effect?

A

When an oral drug is metabolized to an inactive form in the liver before reaching target cells.

21
Q

Why is nitroglycerin given sublingually?

A

To avoid the first-pass effect in the liver.

22
Q

What are special considerations in drug metabolism?

A

Age, induction of drug-metabolizing enzymes, first-pass effect, nutrition status, competition among drugs, and enterohepatic recirculation.

23
Q

What is enterohepatic recirculation?

A

The recycling of drugs and metabolites between the liver and intestines, prolonging their presence in the body.

24
Q

What is excretion in pharmacokinetics?

A

The process of removing drugs and their metabolites from the body.

25
Q

What is the primary organ responsible for excretion?

A

The kidneys (renal excretion).

26
Q

How does urine pH affect drug excretion?

A

It influences the reabsorption and elimination of drugs.

27
Q

Why is dose reduction necessary in renal impairment?

A

Impaired kidneys cannot excrete drugs effectively, leading to accumulation and toxicity.

28
Q

What are other excretion routes besides the kidneys?

A

Breast milk, bile/feces, lungs, sweat, and saliva.

29
Q

What are plasma drug levels?

A

They indicate the amount of drug in the blood and determine therapeutic effectiveness.

30
Q

What is the minimum effective concentration (MEC)?

A

The lowest plasma drug level required to produce a therapeutic effect.

31
Q

What is the toxic concentration?

A

The plasma drug level at which harmful effects occur.

32
Q

What is the therapeutic range?

A

The range between the MEC and the toxic concentration, where the drug is effective and safe.

33
Q

What is plasma half-life (t1/2)?

A

The time it takes for the amount of drug in the body to decrease by 50%.

34
Q

How does half-life affect dosing frequency?

A

Drugs with a longer half-life require less frequent dosing.

35
Q

How many half-lives does it take for a drug to be almost completely excreted?

A

Approximately four half-lives.

36
Q

What is a loading dose?

A

A higher initial dose of a drug to quickly reach the therapeutic range.

37
Q

What is a maintenance dose?

A

A dose used to maintain the drug level within the therapeutic range.

38
Q

What happens to drug levels with repeated dosing?

A

The drug accumulates over time, reaching a plateau after about four half-lives.

39
Q

How long does it take to reach a plateau with repeated dosing?

A

Four half-lives of the drug.

40
Q

What does Phase 3 of the dose-response relationship indicate?

A

Toxicity due to excessively high doses.