Podcast
Questions and Answers
Which of the following routes of administration can bypass the blood-brain barrier?
Which of the following routes of administration can bypass the blood-brain barrier?
What is a significant disadvantage of using certain drug delivery methods?
What is a significant disadvantage of using certain drug delivery methods?
What is the route that delivers drugs directly into the spinal subarachnoid space?
What is the route that delivers drugs directly into the spinal subarachnoid space?
What is the rate limiting barrier in passive percutaneous absorption of drugs through the skin?
What is the rate limiting barrier in passive percutaneous absorption of drugs through the skin?
Signup and view all the answers
Which drug administration route is particularly useful when intravenous access is not possible?
Which drug administration route is particularly useful when intravenous access is not possible?
Signup and view all the answers
Which of the following routes is primarily used for local effects through mucous membranes?
Which of the following routes is primarily used for local effects through mucous membranes?
Signup and view all the answers
What factor enhances systemic absorption of drugs through the skin?
What factor enhances systemic absorption of drugs through the skin?
Signup and view all the answers
Which of the following statements about transdermal drug delivery is correct?
Which of the following statements about transdermal drug delivery is correct?
Signup and view all the answers
What should be avoided when administering drugs during menstruation?
What should be avoided when administering drugs during menstruation?
Signup and view all the answers
Which of the following drugs is known for causing significant fetal malformation when administered during pregnancy?
Which of the following drugs is known for causing significant fetal malformation when administered during pregnancy?
Signup and view all the answers
Why is it important to adjust drug doses for children?
Why is it important to adjust drug doses for children?
Signup and view all the answers
How does age affect drug metabolism and dosing?
How does age affect drug metabolism and dosing?
Signup and view all the answers
What factor contributes to racial variations in drug metabolism?
What factor contributes to racial variations in drug metabolism?
Signup and view all the answers
What is the impact of liver disease on drug administration?
What is the impact of liver disease on drug administration?
Signup and view all the answers
What constitutes a drug interaction?
What constitutes a drug interaction?
Signup and view all the answers
What must be done in cases of kidney failure regarding drug dosage?
What must be done in cases of kidney failure regarding drug dosage?
Signup and view all the answers
Which CYP isoform is responsible for metabolizing caffeine?
Which CYP isoform is responsible for metabolizing caffeine?
Signup and view all the answers
What is one factor that can affect the biotransformation capabilities of P450 enzymes?
What is one factor that can affect the biotransformation capabilities of P450 enzymes?
Signup and view all the answers
Which drug is recognized as an inhibitor of CYP2D6?
Which drug is recognized as an inhibitor of CYP2D6?
Signup and view all the answers
What effect does grapefruit juice have on CYP3A4/5?
What effect does grapefruit juice have on CYP3A4/5?
Signup and view all the answers
Which CYP isoform is primarily responsible for metabolizing warfarin?
Which CYP isoform is primarily responsible for metabolizing warfarin?
Signup and view all the answers
Why do children and the elderly typically have limited abilities of biotransformation?
Why do children and the elderly typically have limited abilities of biotransformation?
Signup and view all the answers
Which of the following drug interactions can lead to increased toxicity due to CYP inhibition?
Which of the following drug interactions can lead to increased toxicity due to CYP inhibition?
Signup and view all the answers
Which CYP isoform metabolizes omeprazole?
Which CYP isoform metabolizes omeprazole?
Signup and view all the answers
What does the α-phase in a Cp vs time plot represent?
What does the α-phase in a Cp vs time plot represent?
Signup and view all the answers
What is the purpose of a loading dose?
What is the purpose of a loading dose?
Signup and view all the answers
In a multiple dosing regimen, what happens to the drug concentration over time?
In a multiple dosing regimen, what happens to the drug concentration over time?
Signup and view all the answers
How is the maintenance dose defined in pharmacology?
How is the maintenance dose defined in pharmacology?
Signup and view all the answers
What are common drug receptors that interact with medications?
What are common drug receptors that interact with medications?
Signup and view all the answers
What is the effect of repeating intravenous bolus injections on drug concentration?
What is the effect of repeating intravenous bolus injections on drug concentration?
Signup and view all the answers
Which of the following statements is false regarding pharmacodynamics?
Which of the following statements is false regarding pharmacodynamics?
Signup and view all the answers
What is typically achieved with multiple dose administration?
What is typically achieved with multiple dose administration?
Signup and view all the answers
What is enterohepatic recycling?
What is enterohepatic recycling?
Signup and view all the answers
Which of the following substances are conserved through enterohepatic recycling?
Which of the following substances are conserved through enterohepatic recycling?
Signup and view all the answers
How does enterohepatic recycling affect the half-life of drugs?
How does enterohepatic recycling affect the half-life of drugs?
Signup and view all the answers
What is the primary route of excretion for unabsorbed orally ingested drugs?
What is the primary route of excretion for unabsorbed orally ingested drugs?
Signup and view all the answers
Why is the excretion of drugs in breast milk a concern?
Why is the excretion of drugs in breast milk a concern?
Signup and view all the answers
Which of the following statements is true about the bioavailability (F) of IV administered drugs?
Which of the following statements is true about the bioavailability (F) of IV administered drugs?
Signup and view all the answers
What type of drugs tends to accumulate in breast milk due to its acidity?
What type of drugs tends to accumulate in breast milk due to its acidity?
Signup and view all the answers
Which route of excretion is least common for drug elimination?
Which route of excretion is least common for drug elimination?
Signup and view all the answers
Study Notes
Drug Administration Routes
-
Intravenous (IV) Route:
- Drug is directly injected into the vein.
- Fastest route of drug administration.
- 100% bioavailability.
- Not suitable for drugs with large particle sizes (> 20 μm) or very small ones (< 5 μm).
-
Intramuscular (IM) Route:
- Drug is injected directly into the muscle.
- Slower absorption than IV route due to blood flow in muscles.
- Suitable for depot preparations, providing sustained drug release.
-
Subcutaneous (SC) Route:
- Drug is injected into the subcutaneous tissue.
- Absorption rate depends on blood flow and drug solubility.
- Useful for slow and sustained drug release.
-
Intra-arterial Route:
- Used for localized effect in a particular tissue or organ.
- Requires expertise and careful administration.
- No first-pass effect.
-
Intra-thecal Route:
- Drug is injected directly into the spinal subarachnoid space.
- Bypasses blood-brain barrier and blood-cerebrospinal fluid (CSF) barrier.
-
Intraventricular Route:
- Drug is injected into the ventricles of the brain.
- Used for example in the treatment of brain tumors or CNS infections.
-
Intraosseous Route:
- Drug is injected into the bone marrow.
- Useful for unconscious patients where IV access is difficult.
-
Topical Administration:
- Drugs are applied to mucous membranes or skin.
- Primarily for local effects.
- Absorption through mucous membranes occurs readily.
-
Skin:
- Commonly used for local effects.
- The main route for drug penetration is through the epidermal layer.
- Stratum corneum is the rate-limiting barrier for passive percutaneous absorption.
-
Transdermal Drug Delivery:
- Not all drugs penetrate intact skin.
- Systemic absorption occurs more readily through abraded, burned, or denuded skin.
- Absorption can be enhanced by suspending the drug in an oily vehicle and rubbing it into the skin.
Biotransformation (Drug Metabolism)
-
Major P450 Enzymes:
- P450 enzymes are responsible for drug metabolism in the liver.
- Major enzymes include CYP1A2, CYP2A6, CYP2B6, CYP2C, CYP2D6, CYP2E1, and CYP3A.
-
Examples of Drugs Metabolized by CYP Isoforms:
- CYP1A2: Caffeine, Theophylline
- CYP2C9: Warfarin, Phenytoin
- CYP2C19: Omeprazole, Diazepam
- CYP2D6: Antidepressants, Quinidine
- CYP3A4/5: Antiretrovirals, Calcium Channel Blockers
-
Factors Affecting Biotransformation:
- Age: Children and elderly may have limited ability to metabolize drugs.
- Sex: Variation in CYP450 enzyme levels between males and females.
- Genetic Factors: Affect enzyme levels in the body.
- Drug Interactions: Enzyme induction or inhibition.
- Diet: Malnutrition can reduce the ability to synthesize CYP450.
Drug Interactions
-
Enzyme Inhibition:
- Drugs can inhibit CYP450 enzyme activity, causing increased levels of the drug and its metabolites.
- Example: Cimetidine inhibits CYP450, which can increase levels of digitoxin and lead to toxicity.
-
Examples of Inhibition Reactions:
- CYP2C9: Fluoxetine (Prozac)
- CYP2D6: Quinidine, Paroxetine
- CYP3A4/5: Ketoconazole, Itraconazole, Ritonavir, Grapefruit Juice
- CYP2E1: Disulfiram
- CYP1A2: Amiodarone
Excretion
-
Enterohepatic Circulation:
- Drug is secreted into bile, passes to the small intestine, and is reabsorbed back into the bloodstream.
- This recycling process can prolong drug half-life.
-
Other Routes of Excretion:
- Feces: Un-absorbed drugs or metabolites excreted in bile.
- Breast Milk: Excretion of drugs in breast milk can affect nursing infants.
- Lungs: Gases and volatile substances are excreted via the lungs.
- Sweat, Saliva, Tears: Small amounts of drugs are excreted into these fluids.
Pharmacokinetics
-
Bioavailability (F):
- Fraction of the administered drug that reaches the systemic circulation as intact drug.
- IV administration has 100% bioavailability.
-
Drug Concentration-Time Profiles:
-
Single Dose Administration:
- Two-phase decline in plasma concentration:
- Alpha (α) phase: Represents drug redistribution.
- Beta (β) phase: Represents drug elimination.
- Two-phase decline in plasma concentration:
-
Multiple Dosing:
- Accumulation of drug in plasma to reach a steady-state concentration.
-
Single Dose Administration:
-
Loading Dose:
- An initial larger dose is administered to quickly reach the target concentration in plasma.
-
Maintenance Dose:
- Smaller doses are given to maintain the steady-state concentration in the body.
Pharmacodynamics
-
Receptors:
- Drug targets that drugs interact with to produce their effects.
- Common targets include ion channels, enzymes, and carrier molecules.
Factors Affecting Drug Action
-
Sex Differences:
- Normal physiological variations between males and females.
-
Pregnancy:
- Many drugs can cross the placenta and cause fetal malformations (teratogenesis).
-
Breastfeeding:
- Many drugs are excreted in breast milk and can harm nursing infants.
-
Body Weight:
- Dosage is often adjusted according to body weight.
-
Age:
- Pharmacokinetic changes with age affect drug absorption, metabolism, distribution, and elimination.
-
Race:
- Racial variations in enzyme levels and activity.
-
Genetic Variations:
- Genetic variations in drug metabolizing enzymes and transporter proteins.
-
Liver and Kidney Disease:
- Liver disease affects drug metabolism, and kidney failure reduces drug excretion.
Studying That Suits You
Use AI to generate personalized quizzes and flashcards to suit your learning preferences.
Related Documents
Description
Test your knowledge on various drug administration routes including intravenous, intramuscular, subcutaneous, intra-arterial, and intra-thecal methods. Understand their characteristics, absorption rates, and specific applications in medical practice. This quiz will help reinforce your understanding of pharmacology principles.