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Questions and Answers
What is the effect of co-administering Trimethoprim with another antimicrobial?
What is the effect of co-administering Trimethoprim with another antimicrobial?
The combination results in a bactericidal effect and can improve the final outcome.
What is the primary action of Warfarin in the body?
What is the primary action of Warfarin in the body?
Warfarin prevents blood clotting by inhibiting platelet action.
How does the binding of molecules to plasma proteins affect their distribution in the body?
How does the binding of molecules to plasma proteins affect their distribution in the body?
Only the fraction of the drug that is unbound can pass from the bloodstream to tissues.
Why are lipophilic molecules more efficient at passing membranes?
Why are lipophilic molecules more efficient at passing membranes?
What characterizes Cefovecin as an antibiotic?
What characterizes Cefovecin as an antibiotic?
Explain the term Fu in the context of drug metabolism.
Explain the term Fu in the context of drug metabolism.
What role do xenobiotics play in relation to plasma protein binding?
What role do xenobiotics play in relation to plasma protein binding?
What is a potential misuse of Warfarin in veterinary medicine?
What is a potential misuse of Warfarin in veterinary medicine?
What is the significance of lipophilicity in drug absorption and distribution?
What is the significance of lipophilicity in drug absorption and distribution?
How does hydrophilicity affect the therapeutic use of drugs in systemic treatments?
How does hydrophilicity affect the therapeutic use of drugs in systemic treatments?
What are the two scenarios presented for hydrophilic drugs in treating pneumonia?
What are the two scenarios presented for hydrophilic drugs in treating pneumonia?
Explain the paracellular transport mechanism in drug passage.
Explain the paracellular transport mechanism in drug passage.
What role do active and passive transport mechanisms play in drug entry into cells?
What role do active and passive transport mechanisms play in drug entry into cells?
Why are unionized molecules more effective in passing through cell membranes?
Why are unionized molecules more effective in passing through cell membranes?
What is passive diffusion and what characteristics of a drug influence it?
What is passive diffusion and what characteristics of a drug influence it?
How do xenobiotic drugs utilize the same mechanisms as nutrients in drug absorption?
How do xenobiotic drugs utilize the same mechanisms as nutrients in drug absorption?
What effect does the blood-brain barrier (BBB) have on dogs with a specific genetic mutation when administered Loperamide?
What effect does the blood-brain barrier (BBB) have on dogs with a specific genetic mutation when administered Loperamide?
How is Minamata disease caused in newborn babies, and what is a significant factor in its development?
How is Minamata disease caused in newborn babies, and what is a significant factor in its development?
What happens to the BBB during meningitis, and what are the implications for drug treatment?
What happens to the BBB during meningitis, and what are the implications for drug treatment?
Which organs experience faster drug distribution due to high perfusion rates, and why is this significant?
Which organs experience faster drug distribution due to high perfusion rates, and why is this significant?
Describe the relationship between perfusion rate and drug distribution in tissues with low perfusion rates like teeth and ligaments.
Describe the relationship between perfusion rate and drug distribution in tissues with low perfusion rates like teeth and ligaments.
What role does age play in the permeability of the BBB, specifically in newborns?
What role does age play in the permeability of the BBB, specifically in newborns?
How does inflammation affect the permeability of the BBB?
How does inflammation affect the permeability of the BBB?
What is the significance of the blood-brain barrier compared to other bodily barriers like the mammary barrier?
What is the significance of the blood-brain barrier compared to other bodily barriers like the mammary barrier?
What is the primary mechanism that allows certain drugs to be redistributed in the body?
What is the primary mechanism that allows certain drugs to be redistributed in the body?
How does the redistribution of anti-parasitic drugs differ between animals and humans?
How does the redistribution of anti-parasitic drugs differ between animals and humans?
What role does perfusion play in drug distribution throughout the body?
What role does perfusion play in drug distribution throughout the body?
Explain the significance of ketamine's redistribution in patients following anesthesia.
Explain the significance of ketamine's redistribution in patients following anesthesia.
In the context of drug absorption, what does the term 'redistribution' specifically refer to?
In the context of drug absorption, what does the term 'redistribution' specifically refer to?
Why are spot-on formulations used for antiparasitic drugs in animals?
Why are spot-on formulations used for antiparasitic drugs in animals?
What defines a 'low-perfused organ' in relation to drug redistribution?
What defines a 'low-perfused organ' in relation to drug redistribution?
How does the concept of kinetic effect influence the design of veterinary drug treatments?
How does the concept of kinetic effect influence the design of veterinary drug treatments?
What role does biotransformation play in the elimination of hormones in the body?
What role does biotransformation play in the elimination of hormones in the body?
How do biotransformations relate to environmental pollutants and xenobiotics?
How do biotransformations relate to environmental pollutants and xenobiotics?
Explain the significance of transforming lipophilic substances into hydrophilic compounds.
Explain the significance of transforming lipophilic substances into hydrophilic compounds.
What percentage of drugs are expected to lose efficacy after biotransformation?
What percentage of drugs are expected to lose efficacy after biotransformation?
What characteristics differentiate endogenous compounds from xenobiotics?
What characteristics differentiate endogenous compounds from xenobiotics?
Why is it important for the liver's capacity for biotransformation to evolve in humans?
Why is it important for the liver's capacity for biotransformation to evolve in humans?
Describe how biotransformation affects the bioactivity of drugs.
Describe how biotransformation affects the bioactivity of drugs.
In what way can drugs sometimes exploit toxic effects despite undergoing biotransformation?
In what way can drugs sometimes exploit toxic effects despite undergoing biotransformation?
What is aflatoxin B1 and how is it formed?
What is aflatoxin B1 and how is it formed?
Explain the biotransformation of aflatoxin B1 in the liver.
Explain the biotransformation of aflatoxin B1 in the liver.
What are the potential health consequences of DNA modification by aflatoxin B1 epoxide?
What are the potential health consequences of DNA modification by aflatoxin B1 epoxide?
Define 'teratogenic' and 'mutagenic' effects as they relate to aflatoxin B1.
Define 'teratogenic' and 'mutagenic' effects as they relate to aflatoxin B1.
Why is aflatoxin B1 monitored in food and feed?
Why is aflatoxin B1 monitored in food and feed?
What role does benzopyrene play in relation to cancer?
What role does benzopyrene play in relation to cancer?
Describe the oxidation process of amylofloxacin to ciprofloxacin.
Describe the oxidation process of amylofloxacin to ciprofloxacin.
What does the chromatographic graph peak signify in the context of ciprofloxacin?
What does the chromatographic graph peak signify in the context of ciprofloxacin?
Flashcards
Hydrophilicity
Hydrophilicity
The ability of a molecule to dissolve in water or an aqueous solution.
Lipophilicity
Lipophilicity
The ability of a molecule to dissolve in fats or lipids.
Paracellular Transport
Paracellular Transport
The movement of molecules through the gaps between cells.
Active Transport
Active Transport
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Passive Diffusion
Passive Diffusion
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Unionized Molecule
Unionized Molecule
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Xenobiotics
Xenobiotics
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Drug Absorption and Distribution
Drug Absorption and Distribution
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Free drug fraction (Fu)
Free drug fraction (Fu)
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Rational for plasma protein binding
Rational for plasma protein binding
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Half-life
Half-life
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Plasma protein binding
Plasma protein binding
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Trimethoprim and Sulfonamide combination
Trimethoprim and Sulfonamide combination
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Warfarin (Coumadin)
Warfarin (Coumadin)
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Cefovecin
Cefovecin
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Low Plasma Protein Binding Drugs
Low Plasma Protein Binding Drugs
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Biotransformation
Biotransformation
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Lipophilic
Lipophilic
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Hydrophilic
Hydrophilic
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Lipophilic to Hydrophilic Conversion
Lipophilic to Hydrophilic Conversion
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Excretion
Excretion
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Bioactivity
Bioactivity
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Termination of Bioactivity
Termination of Bioactivity
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Drug Distribution
Drug Distribution
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Drug Redistribution
Drug Redistribution
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Liposoluble Drugs
Liposoluble Drugs
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Highly Perfused Organs
Highly Perfused Organs
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Less Perfused Organs
Less Perfused Organs
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Ketamine (Dissociative Anesthetic)
Ketamine (Dissociative Anesthetic)
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Spot-on Formulations
Spot-on Formulations
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Drug Metabolism
Drug Metabolism
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What is the blood-brain barrier (BBB)?
What is the blood-brain barrier (BBB)?
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What happens when the BBB is less effective?
What happens when the BBB is less effective?
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How does the BBB differ in newborns?
How does the BBB differ in newborns?
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What happens to the BBB during inflammation?
What happens to the BBB during inflammation?
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What influences drug distribution in the body?
What influences drug distribution in the body?
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How does blood flow affect drug distribution?
How does blood flow affect drug distribution?
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How does perfusion rate impact drug distribution and re-distribution?
How does perfusion rate impact drug distribution and re-distribution?
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How does drug distribution impact its effects?
How does drug distribution impact its effects?
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What is Aflatoxin B1?
What is Aflatoxin B1?
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How does the liver try to detoxify Aflatoxin B1?
How does the liver try to detoxify Aflatoxin B1?
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How does Aflatoxin B1 cause cancer?
How does Aflatoxin B1 cause cancer?
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How does benzopyrene in cigarette smoke cause cancer?
How does benzopyrene in cigarette smoke cause cancer?
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Can all biotransformations detoxify compounds?
Can all biotransformations detoxify compounds?
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How does ciprofloxacin undergo biotransformation?
How does ciprofloxacin undergo biotransformation?
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Do all organisms react the same way to toxins?
Do all organisms react the same way to toxins?
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How is Aflatoxin B1 controlled?
How is Aflatoxin B1 controlled?
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Study Notes
Pharmacokinetics
- Pharmacokinetics is the study of how drugs move through the body.
- It encompasses administration, distribution, metabolism, and elimination (ADME).
- Pharmacodynamics is the study of how drugs affect the body.
- It focuses on the mechanisms of drug action, such as binding to receptors or altering blood osmolarity.
Drug Administration Routes
- Drugs can be administered orally, parentally (IV, IM, SC, etc), or topically.
- Formulation is tailored to the route; a pill is not suitable for injection.
Absorption
- Absorption is the movement of a drug from the site of administration to the bloodstream.
- Factors like drug solubility, ionization (pH), and other components of the formulation affect absorption.
- The absorption rate impacts the time it takes for a drug to have an effect.
Distribution
- Distribution is the movement of a drug from the bloodstream to various tissues and organs.
- Drug binding to plasma proteins influences the distribution; only free drug can access tissues.
- Tissues and organs with higher blood flow receive higher drug concentrations.
Metabolism
- Biotransformation, mainly in the liver, is the conversion of a drug to another form or to metabolites.
- This process often makes the drug more water-soluble for excretion.
- This conversion can sometimes be to a less-active or more toxic form.
- The process can occur in other organs and tissues, not just the liver.
Elimination
- Elimination is the removal of a drug from the body.
- Excretion. Excretion primarily occurs via the kidneys (urine), but also from the liver (bile), and through sweat, feces, etc.
- Renal function is vital in drug elimination, kidney failure can slow or stop drug removal, leading to toxicity
Factors Affecting Drug Absorption
- Lipophilicity/hydrophilicity: lipophilic drugs cross membranes easily.
- Ionization: the ionized form is more polar and less lipid-soluble.
- pH: the environment affects drug ionization and thus its passage through membranes.
Factors Affecting Drug Distribution
- Blood flow to tissues.
- Plasma protein binding (only free drug can enter tissues).
- Drug-tissue interactions.
Factors Affecting Drug Metabolism
- Enzyme induction/inhibition (e.g., by drugs or environmental factors).
- Genetic polymorphisms.
- Age.
- Gender.
- Disease.
- Diet
Factors Affecting Kidney Function
- Renal disease, which can affect both glomerular filtration and tubular secretion.
Drug Transport
- Solute carriers (SLCs) and ATP-binding cassette (ABC) transporters are membrane proteins that play a role in drug absorption, distribution, and excretion.
- These transporters can be affected by drug-drug interactions
Bioavailability
- Bioavailability is the fraction of the administered drug that enters the systemic circulation and is available to bind to receptors.
- It's often expressed by the area under the concentration-time curve (AUC).
- Important when assessing different routes of administration (IV, IM, oral).
Routes of Administration
- Oral
- Intravenous
- Intramuscular
- Subcutaneous
- Topical
- Others (inhalation, intra-articular etc)
Other important concepts:
- Henderson-Hasselbalch equation. This equation reveals the relationship between the pH of the environment and the ionization.
- First-pass metabolism. This is the metabolism of the drug by the liver after absorption from the gastrointestinal tract, resulting in a lower bioavailability.
- Hepato-enterohepatic recirculation. This process can potentially prolong the presence of drugs in the body, especially the water-soluble drug metabolites and also the parent drug.
- Phase I and Phase II reactions of metabolism.
- Cytochromes p450. These enzymes play a key role in the biotransformation of drugs.
- Clinical relevance. These are important considerations for drug dosages and patient health. (e.g., species-selective differences, drug and drug interactions)
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