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Questions and Answers
Which factor does NOT affect drug absorption?
Which factor does NOT affect drug absorption?
- Drug dose
- Molecular weight
- Color of the tablet (correct)
- Local effect of drug
What route of administration is mentioned for drug absorption?
What route of administration is mentioned for drug absorption?
- Intramuscular
- Sublingual (correct)
- Inhalation
- Topical
How does blood flow affect absorption?
How does blood flow affect absorption?
- Enhances absorption at the site (correct)
- Decreases surface area
- Reduces drug dose
- Increases contact time
Which dosage form is identified as having an effect on absorption?
Which dosage form is identified as having an effect on absorption?
What does a greater surface area generally do to drug absorption?
What does a greater surface area generally do to drug absorption?
Which of the following factors is NOT drug-related?
Which of the following factors is NOT drug-related?
What is a characteristic of sustained-release tablets?
What is a characteristic of sustained-release tablets?
Which aspect is important for ensuring absorption occurs effectively?
Which aspect is important for ensuring absorption occurs effectively?
What is the major site of drug metabolism in the body?
What is the major site of drug metabolism in the body?
Which of the following phases of metabolism involves the conversion of lipophilic molecules into more polar molecules?
Which of the following phases of metabolism involves the conversion of lipophilic molecules into more polar molecules?
What type of drug is a prodrug?
What type of drug is a prodrug?
What is the effect of lipophilic drugs in terms of solubility and accumulation?
What is the effect of lipophilic drugs in terms of solubility and accumulation?
What type of reactions are involved in Phase I metabolism?
What type of reactions are involved in Phase I metabolism?
Which of the following is not a characteristic of the Blood Brain Barrier?
Which of the following is not a characteristic of the Blood Brain Barrier?
What is a common drawback of chronic use of drugs that accumulate in body tissues?
What is a common drawback of chronic use of drugs that accumulate in body tissues?
Which of the following is not a typical metabolite from Phase I reactions?
Which of the following is not a typical metabolite from Phase I reactions?
What is the outcome of Phase II metabolism?
What is the outcome of Phase II metabolism?
Which of the following terms describes the biotransformation of a drug for easier elimination?
Which of the following terms describes the biotransformation of a drug for easier elimination?
What is the primary function of microsomal enzymes in drug metabolism?
What is the primary function of microsomal enzymes in drug metabolism?
Which phase of drug metabolism involves glucuronide conjugation?
Which phase of drug metabolism involves glucuronide conjugation?
Where are non-microsomal enzymes primarily found?
Where are non-microsomal enzymes primarily found?
What is the primary aim of drug metabolism?
What is the primary aim of drug metabolism?
What type of reaction is primarily associated with phase I drug metabolism?
What type of reaction is primarily associated with phase I drug metabolism?
What is the primary role of drug-metabolizing enzymes?
What is the primary role of drug-metabolizing enzymes?
What type of metabolism involves metabolizing a constant ratio of the drug over time?
What type of metabolism involves metabolizing a constant ratio of the drug over time?
What is a characteristic of phase I metabolic reactions?
What is a characteristic of phase I metabolic reactions?
Which statement correctly describes zero order metabolism?
Which statement correctly describes zero order metabolism?
Which type of enzymes are responsible for most phase II reactions except glucuronide acid conjugation?
Which type of enzymes are responsible for most phase II reactions except glucuronide acid conjugation?
What is meant by 'first pass metabolism'?
What is meant by 'first pass metabolism'?
What classification do enzymes like CYP450 belong to?
What classification do enzymes like CYP450 belong to?
What does half-life refer to in drug metabolism?
What does half-life refer to in drug metabolism?
What is the overall significance of increasing the water solubility of drugs during metabolism?
What is the overall significance of increasing the water solubility of drugs during metabolism?
What factor increases the absorption of a drug at the absorption site?
What factor increases the absorption of a drug at the absorption site?
How does lipid solubility affect drug absorption?
How does lipid solubility affect drug absorption?
What happens to acidic drugs in a basic environment?
What happens to acidic drugs in a basic environment?
What role does available surface area play in drug absorption?
What role does available surface area play in drug absorption?
Which of the following statements about drug ionization is correct?
Which of the following statements about drug ionization is correct?
What effect does diarrhea have on absorption?
What effect does diarrhea have on absorption?
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Study Notes
Absorption
- Key factors in drug absorption include blood flow to sites, contact time, and molecular weight.
- Lipid solubility is crucial, as it combines drug lipophilicity and ionization, influenced by pH.
- Acidic drugs become charged in basic environments, while basic drugs become charged in acidic settings.
- Sustained-release formulations, dosage forms, and route of administration affect absorption efficiency.
- Increased available surface area (e.g., intestines) enhances absorption, particularly with altered conditions like diarrhea.
Distribution
- Drugs can redistribute to adipose tissue, potentially leading to prolonged effects and toxicity.
- The Blood-Brain Barrier restricts access to the brain, allowing only uncharged, lipid-soluble drugs to penetrate.
Metabolism
- Metabolism refers to the transformation of drugs for easier elimination, primarily occurring in the liver.
- Biotransformation can convert drugs from active to inactive forms or vice versa (prodrugs).
- Phase I reactions modify lipophilic molecules to form more polar molecules through oxidation, reduction, or hydrolysis.
- Phase II reactions involve conjugation where endogenous groups are added to functional groups, enhancing water solubility.
Drug-Metabolizing Enzymes
- Microsomal enzymes (e.g., CYP450) are critical for Phase I reactions and some Phase II reactions, located in the endoplasmic reticulum of hepatocytes.
- Non-microsomal enzymes cater to Phase II reactions other than glucuronidation and are located in various cellular compartments.
Kinetics of Metabolism
- First-order metabolism indicates a constant ratio of drug elimination per time, characterized by a half-life.
- Zero-order metabolism signifies a constant amount of drug eliminated per time, which may occur at high drug concentrations.
First Pass Metabolism
- First-pass metabolism occurs when drugs metabolized in the liver reduce bioavailability prior to systemic circulation.
- The extent of first-pass metabolism affects the efficacy and dosing of orally administered drugs.
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