Carbamazepine Quiz

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What is the volume of distribution (V) of carbamazepine based on oral administered data?

1.4L/kg

What is the maintenance dose adjustment interval for carbamazepine?

Every 1-2 weeks

What is the half-life (t 1/2) of carbamazepine in adult patients receiving polytherapy?

$10$ hours

What is the therapeutic range for plasma concentration of carbamazepine?

<p>$4-8$ mg/L</p> Signup and view all the answers

What is the free fraction (α) of carbamazepine in plasma?

<p>$0.2-0.3$</p> Signup and view all the answers

What is the effective dose range for seizure disorders?

<p>15 to 25 mg/kg/day</p> Signup and view all the answers

Which enzyme is responsible for the metabolism of the drug?

<p>P450 isozyme CYP3A4</p> Signup and view all the answers

What is the ratio of carbamazepine-10,11-epoxide to carbamazepine in infants and preschool children compared to adults?

<p>Higher</p> Signup and view all the answers

What percentage of an oral dose of carbamazepine is excreted unchanged in urine?

<p>Less than 2%</p> Signup and view all the answers

What may affect the therapeutic range of the drug?

<p>$\alpha1$-acid glycoprotein concentration</p> Signup and view all the answers

In adult patients who have received the drug chronically, what is the average clearance value?

<p>$0.064$ L/kg/hr</p> Signup and view all the answers

What happens to clearance in patients who are taking other enzyme inducing antiepileptic drugs concurrently?

<p>Increased to $0.1$ L/kg/hr</p> Signup and view all the answers

What factor may require an increase in dose for reaching blood circulation in oral form?

<p>Bioavailability factor (F)</p> Signup and view all the answers

What occurs when a drug induces its own metabolism?

<p>Auto induction of its metabolic enzymes</p> Signup and view all the answers

What is the clearance value in children compared to adults?

<p>Higher ($0.11$ L/kg/hr)</p> Signup and view all the answers

How much of the drug is bound to plasma albumin and α1 –acid glycoprotein?

<p>70-80%</p> Signup and view all the answers

How much of the drug is excreted unchanged in urine?

<p>Less than 2%</p> Signup and view all the answers

What is the effective dose range for seizure disorders?

<p>15 to 25 mg/kg/day</p> Signup and view all the answers

Which enzyme is responsible for metabolizing the drug?

<p>P450 isozyme CYP3A4</p> Signup and view all the answers

In which age group is the formation of carbamazepine-10,11-epoxide higher compared to adults?

<p>Infants and preschool children</p> Signup and view all the answers

What percentage of the oral dose of carbamazepine is excreted unchanged in urine?

<p>Less than 2%</p> Signup and view all the answers

Which protein is the drug bound to in plasma?

<p>$\alpha1$-acid glycoprotein</p> Signup and view all the answers

What happens to clearance values when patients are taking other enzyme-inducing antiepileptic drugs concurrently?

<p>Clearance increased to $0.1L/kg/hr$.</p> Signup and view all the answers

What factor affects the bioavailability of the drug in oral form?

<p>Increase in clearance</p> Signup and view all the answers

What does alteration in serum protein concentration affect?

<p>Therapeutic range</p> Signup and view all the answers

What does alteration in serum protein concentration affect?

<p>Affects therapeutic range.</p> Signup and view all the answers

What is the volume of distribution (V) of carbamazepine?

<p>1.4L/kg</p> Signup and view all the answers

What is the reported steady-state half-life range for carbamazepine?

<p>$4-12$ hours</p> Signup and view all the answers

What is the half-life (t 1/2) of Carbamazepine in adult patients receiving monotherapy?

<p>$15$ hours</p> Signup and view all the answers

What is the therapeutic range of plasma concentration for Carbamazepine?

<p>$4-8$ mg/L</p> Signup and view all the answers

What is the free fraction of Carbamazepine in plasma?

<p>$0.2-0.3$</p> Signup and view all the answers

What effect does autoinduction commonly cause in steady-state carbamazepine levels?

<p>Increase in steady-state levels</p> Signup and view all the answers

When do clinicians prefer to take plasma samples for carbamazepine level monitoring?

<p>Early morning before the first dose is administered</p> Signup and view all the answers

What is the bioavailability factor (F) of controlled release products of carbamazepine in suspension?

<p>89%</p> Signup and view all the answers

What is the most sensible time for taking plasma samples to reflect trough concentration for carbamazepine level monitoring?

<p>Early morning before the first dose is administered</p> Signup and view all the answers

What are some examples of CYP 3A4 inducers that decrease plasma carbamazepine levels?

<p>Rifampicin, Theophylline</p> Signup and view all the answers

What are some adverse effects associated with Carbamazepine?

<p>Blurred vision, Ataxia, Nystagmus, Skin rashes</p> Signup and view all the answers

What is the bioavailability factor (F) of controlled release carbamazepine products compared to suspension?

<p>89%</p> Signup and view all the answers

What is the volume of distribution (V) of carbamazepine based on oral administered data?

<p>$1.4L/kg$</p> Signup and view all the answers

What is the maintenance dose adjustment interval for carbamazepine?

<p>$1$-week to $2$-week intervals</p> Signup and view all the answers

What are some examples of CYP 3A4 inducers that decrease plasma carbamazepine levels?

<p>Rifampicin, Theophylline, cisplatin, doxorubicin</p> Signup and view all the answers

What is the therapeutic range for plasma concentration for Carbamazepine?

<p>$4-8 mg/L$</p> Signup and view all the answers

What factor may require an increase in dose for reaching blood circulation in oral form?

<p>Bioavailability factor (F)</p> Signup and view all the answers

What is the most sensible time for taking plasma samples to reflect trough concentration for carbamazepine level monitoring?

<p>just before the next dose</p> Signup and view all the answers

What happens to clearance values when patients are taking other enzyme-inducing antiepileptic drugs concurrently?

<p>Clearance increases</p> Signup and view all the answers

What factor may affect the therapeutic range of the drug?

<p>$V_d$ value</p> Signup and view all the answers

What is the free fraction (α) of carbamazepine in plasma?

<p>0.2 - 0.3</p> Signup and view all the answers

What is the bioavailability of carbamazepine when administered orally?

<p>0.8</p> Signup and view all the answers

What is the average clearance value of carbamazepine in adults?

<p>$0.064 L/kg/hr$</p> Signup and view all the answers

What is the reported steady-state half-life range for carbamazepine in children on monotherapy?

<p>$4-12$ hours</p> Signup and view all the answers

What factor affects the bioavailability of carbamazepine in oral form?

<p>Food intake</p> Signup and view all the answers

What is the most sensible time for taking plasma samples to reflect trough concentration for carbamazepine level monitoring?

<p>Before the next dose</p> Signup and view all the answers

What enzyme is responsible for metabolizing carbamazepine?

<p>CYP 3A4</p> Signup and view all the answers

Which drug is mentioned as a chemically similar alternative to carbamazepine with an improved safety profile?

<p>Oxcarbazepine</p> Signup and view all the answers

What is the bioavailability of carbamazepine when administered orally?

<p>0.8</p> Signup and view all the answers

What is the volume of distribution (V) of carbamazepine?

<p>1.4 L/kg</p> Signup and view all the answers

What is the average clearance value of carbamazepine in adults?

<p>$0.064 L/kg/hr$</p> Signup and view all the answers

What is the reported steady-state half-life range for carbamazepine in children on monotherapy?

<p>$4-12$ hours</p> Signup and view all the answers

What are the limitations of carbamazepine therapy?

<p>Autoinduction, drug interactions, toxicities, and teratogenicity.</p> Signup and view all the answers

What factor affects the therapeutic range of carbamazepine?

<p>Autoinduction</p> Signup and view all the answers

What happens to clearance values when patients are taking other enzyme-inducing antiepileptic drugs concurrently?

<p>Clearance values increase</p> Signup and view all the answers

What protein is carbamazepine primarily bound to in plasma?

<p>Albumin and α1- acid glycoprotein</p> Signup and view all the answers

Which drug is mentioned as a chemically similar alternative to carbamazepine with an improved safety profile?

<p>Oxcarbazepine</p> Signup and view all the answers

When should plasma sampling be done for monitoring carbamazepine levels?

<p>Within the first few weeks of therapy, preferably in the early morning or before the next dose.</p> Signup and view all the answers

Study Notes

Carbamazepine Pharmacokinetics and Clinical Considerations

  • Therapeutic plasma concentration for carbamazepine: 4-12 mg/L; toxicity symptoms at >9 mg/L; preferred range of 4-8 mg/L.
  • Carbamazepine drug interactions: CYP 3A4 inhibitors increase plasma levels; inducers decrease levels.
  • Adverse drug reactions include CNS effects, skin rashes, and hematological side effects.
  • Bioavailability of carbamazepine: approximately 0.8 when administered orally; slower absorption and variable bioavailability.
  • Volume of distribution: approximately 1.4L/kg, primarily bound to albumin and α1- acid glycoprotein.
  • Clearance: exclusively metabolic, with less than 2% excretion unchanged in urine; average value approximately 0.064 L/kg/hr in adults.
  • Autoinduction of metabolism by carbamazepine leads to changes in steady-state levels and cross-induction of other anticonvulsants.
  • Children metabolize carbamazepine more rapidly than adults, with reported steady-state half-lives of 4-12 hours in children and 15 hours in adults on monotherapy.
  • Timing of plasma sampling: within the first few weeks of therapy, preferably in the early morning or before the next dose.
  • Limitations of carbamazepine therapy include autoinduction, drug interactions, toxicities, and teratogenicity.
  • Oxcarbazepine is a chemically similar alternative to carbamazepine with an improved safety profile.
  • Clinical case scenarios provide examples for calculating daily doses and adjusting regimens based on plasma levels.

Carbamazepine Pharmacokinetics and Clinical Considerations

  • Therapeutic plasma concentration for carbamazepine: 4-12 mg/L; toxicity symptoms at >9 mg/L; preferred range of 4-8 mg/L.
  • Carbamazepine drug interactions: CYP 3A4 inhibitors increase plasma levels; inducers decrease levels.
  • Adverse drug reactions include CNS effects, skin rashes, and hematological side effects.
  • Bioavailability of carbamazepine: approximately 0.8 when administered orally; slower absorption and variable bioavailability.
  • Volume of distribution: approximately 1.4L/kg, primarily bound to albumin and α1- acid glycoprotein.
  • Clearance: exclusively metabolic, with less than 2% excretion unchanged in urine; average value approximately 0.064 L/kg/hr in adults.
  • Autoinduction of metabolism by carbamazepine leads to changes in steady-state levels and cross-induction of other anticonvulsants.
  • Children metabolize carbamazepine more rapidly than adults, with reported steady-state half-lives of 4-12 hours in children and 15 hours in adults on monotherapy.
  • Timing of plasma sampling: within the first few weeks of therapy, preferably in the early morning or before the next dose.
  • Limitations of carbamazepine therapy include autoinduction, drug interactions, toxicities, and teratogenicity.
  • Oxcarbazepine is a chemically similar alternative to carbamazepine with an improved safety profile.
  • Clinical case scenarios provide examples for calculating daily doses and adjusting regimens based on plasma levels.

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