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Facilitated passive diffusion occurs against a concentration gradient.
Facilitated passive diffusion occurs against a concentration gradient.
Increased first pass metabolism means that less drug has to be given orally.
Increased first pass metabolism means that less drug has to be given orally.
If pH > pKa, the larger proportion of the drug is in its unprotonated form.
If pH > pKa, the larger proportion of the drug is in its unprotonated form.
Volume of distribution (Vd) is used to calculate a loading dose.
Volume of distribution (Vd) is used to calculate a loading dose.
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If Vd is constant and the half-life of a drug is prolonged, the clearance of the drug is decreased.
If Vd is constant and the half-life of a drug is prolonged, the clearance of the drug is decreased.
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When metabolism is saturated, drug elimination follows zero-order kinetics.
When metabolism is saturated, drug elimination follows zero-order kinetics.
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In first-order kinetics, the elimination rate is proportional to the plasma drug concentration.
In first-order kinetics, the elimination rate is proportional to the plasma drug concentration.
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Increasing the rate of infusion changes the time required to achieve steady-state concentration.
Increasing the rate of infusion changes the time required to achieve steady-state concentration.
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Time to reach steady state depends on the dose of the drug.
Time to reach steady state depends on the dose of the drug.
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Area under the curve (AUC) gives a measure of the amount of drug absorbed.
Area under the curve (AUC) gives a measure of the amount of drug absorbed.
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In the second messenger system for the beta-2 adrenoceptor on bronchial smooth muscle, adrenaline increases the activity of cAMP.
In the second messenger system for the beta-2 adrenoceptor on bronchial smooth muscle, adrenaline increases the activity of cAMP.
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In the second messenger system for the beta-2 adrenoceptor on bronchial smooth muscle, inhibition of phosphodiesterase (PDE) decreases cAMP levels.
In the second messenger system for the beta-2 adrenoceptor on bronchial smooth muscle, inhibition of phosphodiesterase (PDE) decreases cAMP levels.
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In the second messenger system for the beta-2 adrenoceptor on bronchial smooth muscle, an increase in cAMP levels lowers intracellular calcium levels.
In the second messenger system for the beta-2 adrenoceptor on bronchial smooth muscle, an increase in cAMP levels lowers intracellular calcium levels.
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In the second messenger system for the beta-2 adrenoceptor on bronchial smooth muscle, caffeine increases cAMP levels in the cell.
In the second messenger system for the beta-2 adrenoceptor on bronchial smooth muscle, caffeine increases cAMP levels in the cell.
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In the second messenger system for the beta-2 adrenoceptor on bronchial smooth muscle, theophylline increases phosphorylation of myosin light chain kinase (MLCK).
In the second messenger system for the beta-2 adrenoceptor on bronchial smooth muscle, theophylline increases phosphorylation of myosin light chain kinase (MLCK).
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Dopamine increases the concentration of cAMP in myocardial muscle cells.
Dopamine increases the concentration of cAMP in myocardial muscle cells.
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Adrenaline increases the activity of phospholipase C in vascular smooth muscle.
Adrenaline increases the activity of phospholipase C in vascular smooth muscle.
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In vascular smooth muscle, an increase in inositol triphosphate causes smooth muscle relaxation.
In vascular smooth muscle, an increase in inositol triphosphate causes smooth muscle relaxation.
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Stimulation of alpha-1 adrenoceptors in vascular smooth muscle increases the concentration of diacylglycerol.
Stimulation of alpha-1 adrenoceptors in vascular smooth muscle increases the concentration of diacylglycerol.
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In skeletal blood vessels, stimulation of beta-2 adrenoceptors activates of myosin light chain kinase (MLCK).
In skeletal blood vessels, stimulation of beta-2 adrenoceptors activates of myosin light chain kinase (MLCK).
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Fluconazole has greater efficacy against Aspergillus infections than voriconazole.
Fluconazole has greater efficacy against Aspergillus infections than voriconazole.
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Posaconazole is used as a prophylaxis against invasive fungal infections.
Posaconazole is used as a prophylaxis against invasive fungal infections.
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Itraconazole inhibits cytochrome P450 enzymes.
Itraconazole inhibits cytochrome P450 enzymes.
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Voriconazole is preferred to amphotericin B in pregnant patients with invasive fungal infections.
Voriconazole is preferred to amphotericin B in pregnant patients with invasive fungal infections.
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Caspofungin is a fungal cell membrane synthesis inhibitor.
Caspofungin is a fungal cell membrane synthesis inhibitor.
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Tenofovir is associated with a higher incidence of lactic acidosis than stavudine.
Tenofovir is associated with a higher incidence of lactic acidosis than stavudine.
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The combination of emtricitabine and lamivudine is synergistic.
The combination of emtricitabine and lamivudine is synergistic.
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Darunavir is contraindicated in patients with a previous history of anaphylaxis due to a sulphur-containing drug.
Darunavir is contraindicated in patients with a previous history of anaphylaxis due to a sulphur-containing drug.
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Efavirenz is preferred over etravirine in patients with viral isolates with the K103N mutation.
Efavirenz is preferred over etravirine in patients with viral isolates with the K103N mutation.
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Atazanavir is preferred to lopinavir in patients with dyslipidemia.
Atazanavir is preferred to lopinavir in patients with dyslipidemia.
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Ganciclovir is preferred to valaciclovir in the treatment of CMV retinitis.
Ganciclovir is preferred to valaciclovir in the treatment of CMV retinitis.
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Oseltamivir is preferred to the annual influenza vaccine as prophylaxis against influenza.
Oseltamivir is preferred to the annual influenza vaccine as prophylaxis against influenza.
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Higher doses of aciclovir are required for genital herpes than herpes encephalitis.
Higher doses of aciclovir are required for genital herpes than herpes encephalitis.
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Ribavirin is ineffective against RSV (Respiratory Syncytial Virus).
Ribavirin is ineffective against RSV (Respiratory Syncytial Virus).
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Pegylated interferon is used in the treatment of chronic hepatitis B infections.
Pegylated interferon is used in the treatment of chronic hepatitis B infections.
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Flucloxacillin is β-lactamase sensitive.
Flucloxacillin is β-lactamase sensitive.
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Co-amoxiclav is used in the treatment of urinary tract infections.
Co-amoxiclav is used in the treatment of urinary tract infections.
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The half-life of penicillin G decreases with probenecid co-administration.
The half-life of penicillin G decreases with probenecid co-administration.
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Meropenem is used in the treatment of bacterial meningitis.
Meropenem is used in the treatment of bacterial meningitis.
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Cefepime is preferred to cefadroxil in the treatment of Pseudomonas aeruginosa infections.
Cefepime is preferred to cefadroxil in the treatment of Pseudomonas aeruginosa infections.
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Vancomycin is administered orally to treat respiratory tract infections.
Vancomycin is administered orally to treat respiratory tract infections.
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Cefotaxime crosses the blood-brain-barrier.
Cefotaxime crosses the blood-brain-barrier.
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In the treatment of urinary tract infections, metoclopramide increases the urinary levels of fosfomycin.
In the treatment of urinary tract infections, metoclopramide increases the urinary levels of fosfomycin.
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Cefamandole decreases alcohol metabolism.
Cefamandole decreases alcohol metabolism.
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High doses of penicillin G increase the risk of seizures.
High doses of penicillin G increase the risk of seizures.
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Fluoroquinolones are used to treat toxoplasmosis.
Fluoroquinolones are used to treat toxoplasmosis.
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Alkanization of the urine increases the risk of ciprofloxacin crystalluria.
Alkanization of the urine increases the risk of ciprofloxacin crystalluria.
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Moxifloxacin prolongs the QTc interval.
Moxifloxacin prolongs the QTc interval.
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Increase the risk of seizures in patients with epilepsy.
Increase the risk of seizures in patients with epilepsy.
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Are safe to use in growing children (<18 years of age).
Are safe to use in growing children (<18 years of age).
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Metronidazole is used in the treatment of acute necrotising ulcerative gingivitis.
Metronidazole is used in the treatment of acute necrotising ulcerative gingivitis.
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Metronidazole increases the risk of bleeding when co-administered with warfarin.
Metronidazole increases the risk of bleeding when co-administered with warfarin.
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Metronidazole is given as a single agent to eradicate Helicobacter pylori in peptic ulcer disease.
Metronidazole is given as a single agent to eradicate Helicobacter pylori in peptic ulcer disease.
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Metronidazole metabolism is increased when co-administered with cimetidine.
Metronidazole metabolism is increased when co-administered with cimetidine.
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Metronidazole decreases the plasma concentration of lithium.
Metronidazole decreases the plasma concentration of lithium.
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Long-term use of co-trimoxazole increases the risk of folic acid deficiency.
Long-term use of co-trimoxazole increases the risk of folic acid deficiency.
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Co-trimoxazole increases digoxin plasma levels when used concurrently.
Co-trimoxazole increases digoxin plasma levels when used concurrently.
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Co-trimoxazole increases the conversion of vitamin K into the active form in the intestine.
Co-trimoxazole increases the conversion of vitamin K into the active form in the intestine.
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Co-trimoxazole is contraindicated in G6PD deficiency.
Co-trimoxazole is contraindicated in G6PD deficiency.
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Co-trimoxazole is safe to use during the last month of pregnancy.
Co-trimoxazole is safe to use during the last month of pregnancy.
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Silver sulfadiazine is used orally to treat burn wounds.
Silver sulfadiazine is used orally to treat burn wounds.
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Trimethoprim is excreted in the urine.
Trimethoprim is excreted in the urine.
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Sulfamethoxazole inhibits dihydrofolate reductase.
Sulfamethoxazole inhibits dihydrofolate reductase.
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Sulfacetamide is used topically for the treatment of conjunctivitis.
Sulfacetamide is used topically for the treatment of conjunctivitis.
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The concurrent use of sulfamethoxazole and glibenclamide increases the risk of hypoglycemia.
The concurrent use of sulfamethoxazole and glibenclamide increases the risk of hypoglycemia.
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Nitrofurantoin absorption is decreased by food.
Nitrofurantoin absorption is decreased by food.
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Nitrofurantoin is used in the treatment of bacterial meningitis.
Nitrofurantoin is used in the treatment of bacterial meningitis.
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Nitrofurantoin inhibits folic acid synthesis.
Nitrofurantoin inhibits folic acid synthesis.
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Nitrofurantoin is contraindicated after 38 weeks of gestation.
Nitrofurantoin is contraindicated after 38 weeks of gestation.
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Long-term use of nitrofurantoin increases the risk of lung fibrosis.
Long-term use of nitrofurantoin increases the risk of lung fibrosis.
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Gentamicin is used to treat Staphylococcus aureus infections.
Gentamicin is used to treat Staphylococcus aureus infections.
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Streptomycin is ototoxic.
Streptomycin is ototoxic.
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Aminoglycosides are safe to use in patients with myasthenia gravis.
Aminoglycosides are safe to use in patients with myasthenia gravis.
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Aminoglycosides are used to treat Pseudomonas aeruginosa infections.
Aminoglycosides are used to treat Pseudomonas aeruginosa infections.
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The elimination half-life of gentamicin is decreased in patients with renal impairment.
The elimination half-life of gentamicin is decreased in patients with renal impairment.
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Telithromycin increases the risk of bleeding when given concurrently with warfarin.
Telithromycin increases the risk of bleeding when given concurrently with warfarin.
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Tigecycline is safe to use in young children (<12 years of age).
Tigecycline is safe to use in young children (<12 years of age).
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Quinupristin-dalfopristin inhibits DNA gyrase.
Quinupristin-dalfopristin inhibits DNA gyrase.
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Linezolid is used in the treatment of MRSA.
Linezolid is used in the treatment of MRSA.
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Fusidic acid is used to treat osteomyelitis.
Fusidic acid is used to treat osteomyelitis.
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Azithromycin has a shorter half-life than erythromycin.
Azithromycin has a shorter half-life than erythromycin.
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Tetracycline is used to treat tick bite fever (Rickettsia).
Tetracycline is used to treat tick bite fever (Rickettsia).
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Clindamycin is used in the treatment of pseudomembranous colitis.
Clindamycin is used in the treatment of pseudomembranous colitis.
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In the treatment of neonatal bacterial meningitis, chloramphenicol is preferred to ceftriaxone.
In the treatment of neonatal bacterial meningitis, chloramphenicol is preferred to ceftriaxone.
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Daptomycin depolarizes the bacterial cell membrane.
Daptomycin depolarizes the bacterial cell membrane.
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Match the antibiotic correctly to its mechanism of action
Match the antibiotic correctly to its mechanism of action
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The antibiotic is matched with its side effect
The antibiotic is matched with its side effect
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Study Notes
Basic Pharmacokinetics
- Facilitated passive diffusion occurs against a concentration gradient.
- Increased first-pass metabolism results in less drug needing oral administration.
- A higher pH than pKa value indicates a larger proportion of the drug is in its unprotonated form.
- Volume of distribution (Vd) calculation determines loading dose.
- Constant Vd and prolonged drug half-life lead to decreased drug clearance.
Pharmacokinetics
- Drug elimination follows zero-order kinetics when metabolism is saturated.
- First-order kinetics: elimination rate is proportional to the plasma drug concentration.
- Infusion rate changes the time to steady-state drug concentration.
- Area under the curve (AUC) represents the total amount of absorbed drug.
- Time to reach steady-state depends on the drug dose.
Second Messenger System for Beta-2 Adrenoceptor on Bronchial Smooth Muscle
- Adrenaline increases cAMP activity.
- Inhibition of phosphodiesterase (PDE) decreases cAMP levels.
- Increased cAMP lowers intracellular calcium levels.
- Caffeine increases cAMP levels.
- Theophylline increases myosin light chain kinase (MLCK) phosphorylation.
Signal Transduction and Drug Action
- Dopamine increases cAMP concentration in myocardial muscle.
- Adrenaline increases phospholipase C activity in vascular smooth muscle.
- Inositol triphosphate increases smooth muscle relaxation.
- Alpha-1-adrenoceptor stimulation increases diacylglycerol concentration.
- Beta-2-adrenoceptor stimulation activates myosin light chain kinase (MLCK).
Antifungals
- Fluconazole is more effective against Aspergillus than voriconazole.
- Posaconazole is used as a prophylaxis against invasive fungal infections.
- Itraconazole inhibits cytochrome P450 enzymes.
- Voriconazole is preferred to amphotericin B in pregnant patients with invasive fungal infections.
- Caspofungin is a fungal cell membrane synthesis inhibitor.
Antiretrovirals
- Tenofovir is associated with a higher incidence of lactic acidosis than stavudine.
- Efavirenz is preferred to etravirine in patients with K103N viral isolates.
- Atazanavir is favored over lopinavir for patients with dyslipidemia.
- Combination of emtricitabine and lamivudine is synergistic.
- Darunavir is contraindicated for patients with a previous history of sulphur-containing drug anaphylaxis.
Antivirals
- Ganciclovir is preferred to valaciclovir for CMV retinitis
- Oseltamivir is preferred to annual flu vaccine prophylaxis for influenza.
- Higher doses of acyclovir are needed for herpes encephalitis than for genital herpes.
- Ribavirin is ineffective against RSV (Respiratory Syncytial Virus).
- Pegylated interferon treats chronic hepatitis B.
Beta-Lactam Antibiotics
- Flucloxacillin is beta-lactamase sensitive.
- Co-amoxiclav treats urinary tract infections.
- Penicillin G half-life decreases with probenecid.
- Meropenem treats bacterial meningitis.
- Cefepime is preferred to cefadroxil for Pseudomonas aeruginosa infections.
Cell Wall Synthesis Inhibitors
- Vancomycin oral administration is for treating respiratory tract infections.
- Cefotaxime crosses the blood-brain barrier.
- Metoclopramide increases urinary fosfomycin levels.
- Cefamandole metabolism decreases alcohol.
- High penicillin G doses increase seizure risk.
Fluoroquinolones
- Urine alkalization increases ciprofloxacin crystalluria risk.
- Moxifloxacin prolongs QTc interval.
- Fluoroquinolones are to treat toxoplasmosis.
- Fluoroquinolones can increase seizure risk in patients with epilepsy.
- Fluoroquinolones are safe in growing children under 18.
Metronidazole
- Used in acute necrotizing ulcerative gingivitis.
- Increases bleeding risk with warfarin co-administration.
- Eradicates Helicobacter pylori in peptic ulcer disease.
- Metabolism increases with cimetidine co-administration.
- Decreases lithium plasma concentrations.
Co-trimoxazole
- Long-term use increases folic acid deficiency risk.
- Increases digoxin plasma levels when combined.
- Converted vitamin K into active form in intestines.
- Contraindicated in G6PD deficiency.
- Safe during the last month of pregnancy.
Folic Acid Synthesis Inhibitors
- Silver sulfadiazine used orally for burn wound treatment.
- Trimethoprim excreted in urine.
- Sulfamethoxazole inhibits dihydrofolate reductase.
- Sulfamethoxazole combined with glibenclamide increases hypoglycemia risk.
- Sulfacetamide used topically for conjunctivitis.
Nitrofurantoin
- Absorption reduced by food.
- Treats bacterial meningitis.
- Inhibits folic acid synthesis.
- Contraindicated after the 38th gestational week.
- Long-term use increases risk of lung fibrosis.
Aminoglycosides
- Gentamicin treats Staphylococcus aureus infections.
- Streptomycin is ototoxic.
- Safe to use in patients with myasthenia gravis.
- Treats Pseudomonas aeruginosa infections.
- Elimination half-life decreases with renal impairment.
Antibiotics (Various)
- Telithromycin increases bleeding risk with warfarin.
- Tigecycline is safe in young children.
- Quinupristin-dalfopristin inhibits DNA gyrase.
- Linezolid treats MRSA.
- Fusidic acid treats osteomyelitis.
Drugs used for bacterial infections
- Azithromycin has shorter half-life than erythromycin.
- Tetracycline treats tick bite fever (Rickettsia).
- Clindamycin treats pseudomembranous colitis.
- Chloramphenicol is preferred to ceftriaxone in neonatal bacterial meningitis.
- Daptomycin depolarizes the bacterial cell membrane.
Matching Antibiotics to Mechanism of Action
- Metronidazole: Forms reactive intermediates, interact with bacterial DNA.
- Clindamycin: Inhibits protein translocation.
- Doxycycline: Inhibits protein synthesis on bacterial 30S ribosomes.
- Vancomycin: Inhibits bacterial cell wall synthesis.
- Fosfomycin: Inhibits codon anticodon interactions.
Antibiotics and Side Effects
- Telithromycin: Hepatotoxicity.
- Imipenem: Seizures.
- Erythromycin: Constipation.
- Vancomycin: Red Man Syndrome.
- Minocycline: Skin discoloration.
Malaria Prophylaxis
- Mefloquine is a blood schizonticide.
- Doxycycline is safe during third trimester of pregnancy.
- In other malaria prophylaxis cases: Mefloquine is preferred to atovaquone-proguanil in certain patients; proguanil inhibits folic acid synthesis, and mefloquine is teratogenic.
Treatment of malaria
- Quinine is contraindicated in cerebral malaria.
- Primaquine is contraindicated in pregnancy.
- Artemether inhibits the erythrocytic phase of the malaria life cycle in humans.
- lumefantrine has longer duration of action compared to Artemether
- Doxycycline antagonizes the effect of quinine.
Treatment of Helminth Infections
- Mebendazole treats Strongyloides stercoralis.
- Albendazole is safe during first trimester of pregnancy.
- Praziquantel effectively treats schistosomiasis.
- Praziquantel causes paralysis of helminth.
- Niclosamide prevents polymerization of cytoplasmic microtubules in susceptible helminths.
Treatment of Protozoal and Ectoparasitic Infections
- Metronidazole is contraindicated during pregnancy's first trimester.
- Tinidazole has shorter duration of action than Metronidazole.
- Chloroquine is preferred to metronidazole for luminal amoeba infections.
- Co-trimoxazole treats pneumocystosis.
- Lindane is readily absorbed through the skin.
Rifampicin
- Increases digoxin clearance.
- Induces verapamil metabolism.
- Effective prophylaxis against meningococcal carriage.
- Increases warfarin anticoagulant effect.
- Effective against multidrug-resistant strains of Mycobacterium tuberculosis.
Ethionamide
- Inhibits cytochrome P450 enzymes.
- Does not penetrate the blood-brain barrier.
- Causes pyridoxine-sensitive peripheral neuropathy.
- Precipitates seizures in susceptible individuals.
-
95% excreted unchanged in the urine.
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Description
This quiz covers essential concepts in pharmacokinetics, including drug absorption, distribution, metabolism, and elimination. Additionally, it explores the second messenger system for beta-2 adrenoceptors affecting bronchial smooth muscle. Test your understanding of these critical pharmacological principles.
