Podcast
Questions and Answers
Which of the following medications is represented by the term 'وديكسا'?
Which of the following medications is represented by the term 'وديكسا'?
- Dexamethasone (correct)
- kni
- Omeprazole
- Ciprofloxacin
If a patient requires ciprofloxacin, which term would correctly identify the medication?
If a patient requires ciprofloxacin, which term would correctly identify the medication?
- Omeprazole
- أويم
- كني (correct)
- Dexamethasone
A pharmacist receives a prescription for 'أويم'. Which medication should they dispense?
A pharmacist receives a prescription for 'أويم'. Which medication should they dispense?
- kni
- Omeprazole (correct)
- Dexamethasone
- Ciprofloxacin
Which medication name is likely to be used to treat bacterial infections?
Which medication name is likely to be used to treat bacterial infections?
A doctor wants to prescribe a medication to reduce inflammation. Which of the following options should the doctor consider?
A doctor wants to prescribe a medication to reduce inflammation. Which of the following options should the doctor consider?
Which of the following best describes the interaction between phenytoin and cyclosporine A?
Which of the following best describes the interaction between phenytoin and cyclosporine A?
Erythromycin increases the risk of theophylline toxicity by which mechanism?
Erythromycin increases the risk of theophylline toxicity by which mechanism?
A patient taking theophylline develops arrhythmia after being prescribed erythromycin. Which of the following is the MOST likely cause?
A patient taking theophylline develops arrhythmia after being prescribed erythromycin. Which of the following is the MOST likely cause?
A patient on cyclosporine A begins taking phenytoin. What adjustments might be necessary to maintain therapeutic cyclosporine A levels?
A patient on cyclosporine A begins taking phenytoin. What adjustments might be necessary to maintain therapeutic cyclosporine A levels?
Which of the following drug-drug interactions could potentially lead to subtherapeutic medication levels?
Which of the following drug-drug interactions could potentially lead to subtherapeutic medication levels?
In a clinical setting, why is it essential to understand the specific mechanism of action for drugs like chloramphenicol and macrolides?
In a clinical setting, why is it essential to understand the specific mechanism of action for drugs like chloramphenicol and macrolides?
A patient is prescribed a medication that inhibits protein synthesis in bacteria. If the medication non-selectively binds to both prokaryotic and eukaryotic ribosomes, what is the most likely consequence?
A patient is prescribed a medication that inhibits protein synthesis in bacteria. If the medication non-selectively binds to both prokaryotic and eukaryotic ribosomes, what is the most likely consequence?
Which of the following statements best describes the primary difference in the mechanism of action between chloramphenicol and macrolides?
Which of the following statements best describes the primary difference in the mechanism of action between chloramphenicol and macrolides?
A new antibiotic is discovered that also targets the 50S ribosomal subunit. Initial studies show that it prevents the formation of the initiation complex. Which stage of protein synthesis is directly inhibited by this new antibiotic?
A new antibiotic is discovered that also targets the 50S ribosomal subunit. Initial studies show that it prevents the formation of the initiation complex. Which stage of protein synthesis is directly inhibited by this new antibiotic?
Suppose a bacterium develops resistance to both chloramphenicol and erythromycin (a macrolide). What is the most likely mechanism that could confer cross-resistance to these two drugs?
Suppose a bacterium develops resistance to both chloramphenicol and erythromycin (a macrolide). What is the most likely mechanism that could confer cross-resistance to these two drugs?
Which category of enzymes is primarily responsible for breaking down proteins into smaller peptides or amino acids?
Which category of enzymes is primarily responsible for breaking down proteins into smaller peptides or amino acids?
What class of enzymes is known for its broad substrate specificity and ability to hydrolyze a wide range of ester bonds?
What class of enzymes is known for its broad substrate specificity and ability to hydrolyze a wide range of ester bonds?
Which enzyme is responsible for the breakdown of acetylcholine, a neurotransmitter, in the nervous system?
Which enzyme is responsible for the breakdown of acetylcholine, a neurotransmitter, in the nervous system?
Which enzyme plays a primary role in the degradation of the peptide hormone insulin?
Which enzyme plays a primary role in the degradation of the peptide hormone insulin?
A researcher is studying the metabolism of a novel peptide and identifies an enzyme that cleaves the peptide into smaller fragments. Based on the content, which type of enzyme is most likely involved in this process?
A researcher is studying the metabolism of a novel peptide and identifies an enzyme that cleaves the peptide into smaller fragments. Based on the content, which type of enzyme is most likely involved in this process?
Predict the impact of administering Rifampin together with Ketoconazole, considering their potential interaction through hepatic enzyme systems?
Predict the impact of administering Rifampin together with Ketoconazole, considering their potential interaction through hepatic enzyme systems?
A patient is prescribed Rifampin for tuberculosis. What advice should the healthcare provider give regarding potential interactions with other medications?
A patient is prescribed Rifampin for tuberculosis. What advice should the healthcare provider give regarding potential interactions with other medications?
A patient taking ketoconazole reports decreased drug effectiveness after starting rifampin. What is the most likely reason for this?
A patient taking ketoconazole reports decreased drug effectiveness after starting rifampin. What is the most likely reason for this?
If a patient requires both rifampin and ketoconazole, what strategy might a healthcare provider employ to mitigate potential drug interactions?
If a patient requires both rifampin and ketoconazole, what strategy might a healthcare provider employ to mitigate potential drug interactions?
How does Rifampin's mechanism of action contribute to its potential for drug interactions?
How does Rifampin's mechanism of action contribute to its potential for drug interactions?
Why is benzylpenicillin typically administered via injection rather than orally?
Why is benzylpenicillin typically administered via injection rather than orally?
Why is insulin typically administered via injection rather than orally?
Why is insulin typically administered via injection rather than orally?
What is the primary reason L-dopa is often administered with carbidopa?
What is the primary reason L-dopa is often administered with carbidopa?
What is the most likely consequence of administering benzylpenicillin orally?
What is the most likely consequence of administering benzylpenicillin orally?
A patient taking L-dopa experiences nausea and vomiting. How does the understanding of L-dopa metabolism inform the strategies to manage these side effects?
A patient taking L-dopa experiences nausea and vomiting. How does the understanding of L-dopa metabolism inform the strategies to manage these side effects?
Which term accurately defines the process of chemical alteration of drugs within the body?
Which term accurately defines the process of chemical alteration of drugs within the body?
In the context of pharmacology, what is the Arabic term 'التكسري' most accurately translated to?
In the context of pharmacology, what is the Arabic term 'التكسري' most accurately translated to?
If a drug's structure is altered within the body, which pharmacological process is directly responsible for this change?
If a drug's structure is altered within the body, which pharmacological process is directly responsible for this change?
Considering the breakdown of a drug into its metabolites, which process is fundamentally involved?
Considering the breakdown of a drug into its metabolites, which process is fundamentally involved?
Which concept is most closely associated with 'chemical alteration of drugs in the body'?
Which concept is most closely associated with 'chemical alteration of drugs in the body'?
Which conjugation reaction is MOST likely to affect the metabolism of steroid hormones?
Which conjugation reaction is MOST likely to affect the metabolism of steroid hormones?
A patient exhibits significantly altered drug response due to a genetic defect affecting acetylation. Which drug's metabolism would be MOST affected?
A patient exhibits significantly altered drug response due to a genetic defect affecting acetylation. Which drug's metabolism would be MOST affected?
A drug's half-life is significantly prolonged in patients with compromised hepatic function. Which conjugation reaction would MOST likely be impaired, leading to this prolonged half-life?
A drug's half-life is significantly prolonged in patients with compromised hepatic function. Which conjugation reaction would MOST likely be impaired, leading to this prolonged half-life?
If a patient has a genetic deficiency in catechol-O-methyltransferase (COMT), the metabolism of which substance would be MOST directly affected?
If a patient has a genetic deficiency in catechol-O-methyltransferase (COMT), the metabolism of which substance would be MOST directly affected?
A researcher is investigating a new drug that undergoes extensive sulfation. Which enzyme would be MOST crucial to study to understand the drug's metabolism?
A researcher is investigating a new drug that undergoes extensive sulfation. Which enzyme would be MOST crucial to study to understand the drug's metabolism?
A drug is metabolized into an active metabolite. How does this impact the original drug's effects?
A drug is metabolized into an active metabolite. How does this impact the original drug's effects?
If a drug's metabolism results in an inactive metabolite, what is the expected consequence?
If a drug's metabolism results in an inactive metabolite, what is the expected consequence?
Codeine is metabolized into morphine. What is the pharmacological significance of this conversion?
Codeine is metabolized into morphine. What is the pharmacological significance of this conversion?
A new drug is discovered that, upon metabolism, produces both an active and an inactive metabolite. What is the most complex consideration when determining appropriate dosing?
A new drug is discovered that, upon metabolism, produces both an active and an inactive metabolite. What is the most complex consideration when determining appropriate dosing?
A patient with impaired liver function is prescribed a prodrug that is metabolized into an active compound. How should the prescribing physician adjust the dosage?
A patient with impaired liver function is prescribed a prodrug that is metabolized into an active compound. How should the prescribing physician adjust the dosage?
Which of the following conditions warrants the use of Lincosamides ()لينكو?
Which of the following conditions warrants the use of Lincosamides ()لينكو?
How do smoking ( )بيدخنوand alcohol ( )ويسكروconsumption primarily impact the effectiveness of many medications?
How do smoking ( )بيدخنوand alcohol ( )ويسكروconsumption primarily impact the effectiveness of many medications?
What is a significant pharmacological consideration when administering Isoniazid ()أيزو?
What is a significant pharmacological consideration when administering Isoniazid ()أيزو?
Which of the following is the primary mechanism of action for Azole antifungals?
Which of the following is the primary mechanism of action for Azole antifungals?
A patient is prescribed both Isoniazid ()أيزو and Rifampin for the treatment of tuberculosis. What is the primary concern regarding this drug combination?
A patient is prescribed both Isoniazid ()أيزو and Rifampin for the treatment of tuberculosis. What is the primary concern regarding this drug combination?
A patient taking oral contraceptives is prescribed rifampin for tuberculosis. What is the most critical piece of information to convey regarding the interaction between these medications?
A patient taking oral contraceptives is prescribed rifampin for tuberculosis. What is the most critical piece of information to convey regarding the interaction between these medications?
Why is the interaction between rifampin and estrogen-containing oral contraceptives clinically significant?
Why is the interaction between rifampin and estrogen-containing oral contraceptives clinically significant?
A patient on oral contraceptives requires antibiotic treatment. Which antibiotic is LEAST likely to interact with their contraceptive, based on the information provided?
A patient on oral contraceptives requires antibiotic treatment. Which antibiotic is LEAST likely to interact with their contraceptive, based on the information provided?
A 28-year-old woman on oral contraceptives is diagnosed with latent tuberculosis and prescribed rifampin. Considering the drug interaction, which of the following management strategies would be the MOST appropriate?
A 28-year-old woman on oral contraceptives is diagnosed with latent tuberculosis and prescribed rifampin. Considering the drug interaction, which of the following management strategies would be the MOST appropriate?
A patient on combined oral contraceptives presents to the clinic with a new diagnosis of tuberculosis requiring rifampin. She expresses concern about contraceptive failure. Which course of action is MOST appropriate?
A patient on combined oral contraceptives presents to the clinic with a new diagnosis of tuberculosis requiring rifampin. She expresses concern about contraceptive failure. Which course of action is MOST appropriate?
In cases where a drug undergoes partial first-pass metabolism, how should the oral dosage be adjusted compared to the intravenous dosage to achieve a similar therapeutic effect?
In cases where a drug undergoes partial first-pass metabolism, how should the oral dosage be adjusted compared to the intravenous dosage to achieve a similar therapeutic effect?
How does proteolytic degradation affect the bioavailability of peptide drugs like insulin when administered orally, and what implications does this have for drug delivery?
How does proteolytic degradation affect the bioavailability of peptide drugs like insulin when administered orally, and what implications does this have for drug delivery?
A novel peptide-based therapeutic is developed, showing promise in initial trials. However, oral administration results in negligible plasma concentrations. What is the MOST probable reason for this?
A novel peptide-based therapeutic is developed, showing promise in initial trials. However, oral administration results in negligible plasma concentrations. What is the MOST probable reason for this?
A patient is switched from intravenous propranolol to oral propranolol. Given that propranolol undergoes significant first-pass metabolism, what adjustment to the dosage should be expected to maintain a similar therapeutic effect?
A patient is switched from intravenous propranolol to oral propranolol. Given that propranolol undergoes significant first-pass metabolism, what adjustment to the dosage should be expected to maintain a similar therapeutic effect?
A research team is formulating a new oral drug. To optimize its bioavailability, they need to consider the impact of first-pass metabolism. Which strategy would be MOST effective in minimizing the first-pass effect?
A research team is formulating a new oral drug. To optimize its bioavailability, they need to consider the impact of first-pass metabolism. Which strategy would be MOST effective in minimizing the first-pass effect?
Flashcards
Warfarin Accumulation Consequence
Warfarin Accumulation Consequence
Warfarin buildup can lead to increased risk of bleeding.
Phenytoin & Cyclosporine A Interaction
Phenytoin & Cyclosporine A Interaction
Phenytoin speeds up cyclosporine A metabolism, reducing its effectiveness and potentially causing graft rejection.
Erythromycin & Theophylline Interaction
Erythromycin & Theophylline Interaction
Erythromycin inhibits the metabolism of theophylline, potentially leading to theophylline toxicity and arrhythmias.
Drug Metabolism
Drug Metabolism
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Arrhythmia
Arrhythmia
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Dexamethasone
Dexamethasone
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Ciprofloxacin
Ciprofloxacin
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Omeprazole
Omeprazole
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Medications ending in 'sone'
Medications ending in 'sone'
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Medications ending in 'prazole'
Medications ending in 'prazole'
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Rifampin
Rifampin
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Ketoconazole
Ketoconazole
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Chloramphenicol
Chloramphenicol
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Macrolides
Macrolides
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Erythromycin
Erythromycin
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Macrolides Mechanism
Macrolides Mechanism
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Macrolides use
Macrolides use
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Nonspecific Esterases
Nonspecific Esterases
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Acetylcholine Metabolism
Acetylcholine Metabolism
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Peptidases
Peptidases
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Insulin Metabolism
Insulin Metabolism
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Insulinase
Insulinase
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Benzylpenicillin Stability
Benzylpenicillin Stability
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Oral Insulin Ineffectiveness
Oral Insulin Ineffectiveness
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L-dopa Metabolism in Gut
L-dopa Metabolism in Gut
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Gastric Acid Drug Degradation
Gastric Acid Drug Degradation
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Enzymatic Hormone Degradation
Enzymatic Hormone Degradation
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Drug Metabolism Definition
Drug Metabolism Definition
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Metabolism: Chemical Alteration
Metabolism: Chemical Alteration
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Drug Metabolism: Process
Drug Metabolism: Process
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What happens in drug metabolism?
What happens in drug metabolism?
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Lincosamides
Lincosamides
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Isoniazid
Isoniazid
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Azoles
Azoles
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Smoking & Alcohol
Smoking & Alcohol
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Termination of Drug Effect
Termination of Drug Effect
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Inactive Metabolite
Inactive Metabolite
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Active Metabolite
Active Metabolite
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Prolongation of Drug Effect
Prolongation of Drug Effect
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Codeine to Morphine
Codeine to Morphine
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Methylation
Methylation
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COMT (Catechol-O-Methyltransferase)
COMT (Catechol-O-Methyltransferase)
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Acetylation
Acetylation
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Sulfation
Sulfation
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Sulfotransferases
Sulfotransferases
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Antibiotics & Estrogen Pill Interaction
Antibiotics & Estrogen Pill Interaction
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Enzyme Induction
Enzyme Induction
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Rifampin & Estrogen Interaction
Rifampin & Estrogen Interaction
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Rifabutin
Rifabutin
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Drug Interaction Consequence
Drug Interaction Consequence
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Proteolytic Insulin Degradation
Proteolytic Insulin Degradation
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First-Pass Effect
First-Pass Effect
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Dose Adjustment for First-Pass
Dose Adjustment for First-Pass
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Propranolol First-Pass Example
Propranolol First-Pass Example
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Bioavailability
Bioavailability
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Study Notes
- Metabolism, or biotransformation, refers to the process of chemical alteration of drugs in the body.
Site of Metabolism
- Liver: Primary site of drug metabolism.
- Other organs involved: kidney, lungs, and the gastrointestinal tract.
Effect of Enzymes on Drugs
- Active Drug converted to Inactive Metabolite: Most common outcome, leads to termination of the drug effect.
- Active Drug converted to Active Metabolite: Leads to prolongation of the drug effect; for example, codeine converts to morphine.
- Inactive Drug (Pro-Drug) converted to Active Metabolite: L-dopa is converted to dopamine, and enalapril becomes enalaprilat.
- Non-Toxic Drug converted to Toxic Metabolite: This occurs when paracetamol is converted to N-acetyl benzo-quinone.
- Metabolism aims to convert lipid-soluble drugs to water-soluble metabolites.
- This conversion facilitates drug excretion in body water, including urine, bile, milk, and sweat.
- It also decreases tissue penetration and potential re-absorption due to the increased water solubility.
Biochemical Reactions in Drug Metabolism
- Phase 1 Reactions: Oxidation, reduction, and hydrolysis.
- Phase 2 Reactions: Conjugation.
- Drugs converted into water-soluble compounds via Phase 1 reactions may not need to undergo Phase 2 metabolism.
Phase 1 Reactions - Oxidation
- Oxidation: The addition of O2, or the removal of H+ from the drug.
Microsomal Oxidation:
- Utilizes oxidizing enzymes located in the microsomes of many organs, especially the liver.
- Microsomes are sub-cellular membranous vesicles found in the smooth endoplasmic reticulum of cells.
- Cytochrome P450 enzyme (Cp450 or CYP450) is the primary enzyme in the microsomal enzyme system.
- CP450 family consists of numerous iso-enzymes, formed of hemoproteins, that catalyze oxidation-reduction reactions, acting as mixed function oxidases.
Microsomal Liver Enzyme Inducers and Inhibitors
- Microsomal Enzyme Induction:
- Increases the rate of metabolism for some drugs, resulting in decreased serum levels and therapeutic failure.
- For acetaminophen, induced metabolism can lead to increased levels of toxic metabolites.
- An increased dose may be required for a drug affected by metabolism.
- Examples of inducers: Rifampicin (can accelerate the metabolism of contraceptive pills, and may cause failure of contraception) and Phenytoin (accelerates metabolism of cyclosporine A, potentially causing graft rejection).
Microsomal Enzyme Inhibition:
- Decreases the rate of metabolism for some drugs, leading to increased serum levels and toxicity.
- An opposite or decreased dose of the drug may be required.
- Examples of inhibitors: Ciprofloxacin (inhibits warfarin metabolism, leading to accumulation and bleeding) and Erythromycin (inhibits theophylline metabolism, resulting in theophylline toxicity and arrhythmia).
Examples of Enzyme Inducers
- Oxcarbazepine
- Carbamazepine
- Dexamethasone
- Omeprazole
- Phenytoin
- Phenobarbitone
- Smoking & alcohol
- Rifampin
- St. John's Wort
Examples of Enzyme Inhibitors
- Cimetidine
- Allopurinol
- Quinolones (ciprofloxacin)
- Chloramphenicol
- Macrolides (erythro & clarithro)
- Lincosamides
- Isoniazide
- Azoles (ketoconazole)
- Interferon
- Ritonavir
- Grapefruit juice
Non-Microsomal Oxidation
- Done By: Soluble enzymes in cytoplasm or mitochondria.
- Xanthine Oxidase: Converts xanthine into uric acid.
- Monoamine oxidase (MAO): Oxidizes catecholamines and serotonin.
Reduction Reaction
- Less common compared to oxidation.
- Types:
- Microsomal: Nitroreductase (chloramphenicol).
- Non-microsomal: Carbonyl reductase (naloxone).
Hydrolysis Reactions
- Mainly non-microsomal, occurring in plasma, tissues, & body fluids.
- Involves Non-specific esterases, such as Cholinesterase, involved in acetylcholine metabolism.
- Also involves Peptidases: Insulin metabolism by insulinase.
- If a drug is initially water-soluble, it does not need to undergo metabolism and is excreted unchanged.
Phase 2 Reactions (Conjugation) Definition
- Involves the coupling of a drug or its metabolite to an endogenous substrate, usually glucuronic acid, to form a water-soluble conjugate that can be easily excreted in urine or bile
Types of Endogenous Substrates and Conjugation Reactions
- Glucuronide Conjugation (Microsomal)
- Most common conjugation reaction.
- Involves the conjugation of activated glucuronic acid to drugs or metabolites.
- Glucuronide conjugates are inactive and rapidly excreted in urine or bile.
- Glucuronide conjugates secreted in bile are hydrolyzed by intestinal bacteria, which can free the drug to be reabsorbed (enterohepatic circulation), increasing the duration of drug action e.g. estrogen pills.
- Other Conjugation Reactions (Non-Microsomal)
- Glutathione conjugation: Uses glutathione (for acetaminophen, ethacrynic acid).
- Glycine conjugation: Uses glycine (for salicylic acid).
- Methylation: Uses a methyl group (COMT for noradrenaline).
- Acetylation: Uses acetic acid (for isoniazid, salicylic acid).
- Sulfation: Uses sulfotransferase (for steroid hormones).
Breakthrough Pregnancy
- Contraceptive pills contain estrogen, which undergoes metabolism through glucuronide conjugation before excretion via bile conjugate.
- Intestinal bacteria can hydrolyze the estrogen conjugate in the gut, freeing estrogen for reabsorption, lengthening its duration of action.
- Antibiotics can disrupt this process by killing the intestinal bacteria
- Estrogen from contraceptive pills may lose its prolonged action, thus increasing the chances of pregnancy.
- The drug interaction between antibiotics and estrogen pills is debatable and only proven for rifampin.
First-Pass Metabolism (Pre-Systemic Elimination) Definition
- Occurs when drugs are metabolized at the site of administration before reaching systemic circulation.
First-Pass Metabolism (Pre-Systemic Elimination) Examples
- Oral Route:
- Gut First-Pass Metabolism: Gastric acidity destroys benzyl penicillin, digestive enzymes, and hormones such as insulin degrade COMT found in intestinal mucosa metabolize L-dopa.
- Hepatic First-Pass Metabolism: drugs degraded by the liver include Morphine & H2-blockers, Beta Blockers, Nitrates
- Lung Absorption: Some metabolism can occur following inhalation.
- SC After Topical Skin Application: Insulin can be degraded by proteolytic enzymes.
How to Avoid First-Pass Metabolism
- Increase drug dose if the first-pass effect is partial: For example, 5mg Propranolol IV is equivalent to 100mg orally administered.
- Utilize other drug routes if the first pass effect is comprehensive: These options are Sublingual, inhalation, or intravenous.
- In cases of acute angina, sublingual nitroglycerin is preferred over oral
Factors Affecting Drug Metabolism
- Genetic Factors: Acetylation status (fast or slow metabolizers).
- Malnutrition: Decreased availability of vitamins & amino acids (needed for metabolism).
- Age (Extremes): Metabolism may be decreased in the elderly and in children aged < 6 months.
- Liver Disease & Liver Cell Failure (LCF): Impaired hepatic enzyme function and decreased amino acid availability.
- Hepatic Enzyme Inducers or Inhibitors:
- Reduced drug metabolism leads to decreased clearance and longer t1/2 , requiring a decrease drug dose.
- Increased drug metabolism leads to increased clearance and shorter t1/2, increasing the needed drug dose.
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