PCEU0302

Bio Pharmaceutics and Pharmacokinetics

Spring Semester 2023-2024

ALBENDAZOLE

Student name: Maather Khalil Alhadhrami

Student ID: NU180358
Student Emil: maather180358@nu.edu.om
Course instructor: Dr. Alka Ahuja

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 Assignment 1

Qustion1: Collect the details of Drug listed against your name and answer
the following:
a. What is Drug’s half -life and calculate its Ke?
 • Albendazole's half-life typically spans 8-12 hours, although
this duration can fluctuate based on factors like individual
characteristics and dosage. The elimination constant of
Albendazole is likewise influenced by variables such as age,
weight, and liver function. Nevertheless, on average,
Albendazole elimination half-life falls within the 8-12 hour
range. It's crucial to recognize that these figures may diverge
significantly depending on individual circumstances and other
considerations. Consequently, seeking guidance from a
healthcare provider is advisable for precise details regarding
Albendazole's half-life and elimination constant in specific
cases..
 To calculate the elimination constant of Albendazole, we need
the half-life of the drug. Since the half-life of Albendazole is 8
to 12 hours, we can take an average value of 10 hours. The
formula for elimination constant is:
Elimination constant = 0.693 / Half-life
Therefore, in this case,
Elimination constant = 0.693 / 10 hours
Elimination constant = 0.0693 hours^-1
So, the elimination constant of Albendazole is approximately
0.0693 hours^-1.

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b. After how many hours will the drug be 94 % eliminated?
 To calculate the time after which 94% of Albendazole will be
eliminated from the body, we can use the following formula:
t = (ln (C0/Ct) )/k
where t = time, C0 = initial concentration, Ct = concentration at
time t, and k = elimination constant.
Assuming that the initial concentration of Albendazole is 100%,
and the elimination constant is 0.0693 hours^-1, we can plug
these values into the formula and solve for t:
t = (ln (100/6) )/0.0693
t = 29.3 hours
Therefore, it takes approximately 29.3 hours for 94% of
Albendazole to be eliminated from the body..

c. Write names of 3 Pharmaceutical equivalents of your drug

formulations?
 Zentel (by GSK)
 Albenza (by Amedra Pharmaceuticals)
 Valbazen (by Zoetis)

d. What is the mechanism of absorption for your drug?

 Albendazole, an anti-parasitic medication, exhibits low water
solubility and limited bioavailability. Its absorption in the
gastrointestinal tract occurs through both passive diffusion and
active transport mechanisms. Upon ingestion, the liver rapidly
metabolizes Albendazole into its active form, Albendazole
sulfoxide, responsible for its therapeutic effects. Administration
alongside a fatty meal enhances its absorption by improving
solubility and intestinal permeability. Factors like pH, bile flow,
and concurrent medications also affect its absorption. Post-
absorption, Albendazole and its metabolites distribute widely
across various tissues, with a lengthy half-life of up to 9 hours.
Despite its complex absorption dynamics, Albendazole

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 generally demonstrates good tolerability and efficacy in treating
parasitic infections.

e. Which protein is it bound to?

 Albendazole undergoes significant metabolism in the liver,
producing its active metabolite, Albendazole sulfoxide, which
predominantly binds primary to plasma albumin. Albumin, a
liver-produced protein, facilitates the transportation of diverse
substances, including medications, throughout the body via the
bloodstream. In Albendazole's case, its binding to albumin
plays a crucial role in its distribution and removal from the
body. Given Albendazole sulfoxide's extended half-life, its
association with albumin can also impact the duration of the
drug's therapeutic efficacy.

f. Write one name of its Pharmaceutical alternative.

 One pharmaceutical alternative name for Albendazole is Zentel.

g. Does your drug follow linear or nonlinear Pharmacokinetics

 Albendazole displays non-linear pharmacokinetics, indicating
that its processing within the body is not directly proportional
to the dosage administered. Various factors, such as co-
administration with food and the dosage level, influence
Albendazole's absorption, distribution, metabolism, and
elimination. Albendazole metabolism appears to reach
saturation, causing its pharmacokinetics to vary. At lower
doses, the drug is cleared rapidly, but higher doses lead to
slower clearance due to saturation, resulting in a non-linear
correlation between dosage and Albendazole plasma
concentration. Consequently, administering higher doses of
Albendazole may lead to disproportionately elevated plasma
drug levels, posing a risk of toxicity to the patient.

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Q.2. Name three drugs which are transported by:-
a) Passive transport:
 Aspirin
 Alcohol(ethanol)
 Valproic acid
b) Pore transport:
 Levodopa
 Mannitol
 Foscarnet

Qustion.3 Name various enzymes in different parts of GIT? How do they

influence the release of drugs? Give examples of four drugs whose
absorption is influenced by them.

1. Salivary gland amylase

2. Stomach: pepsin
3. Pancreas: amylase, lipase, and proteases.
4. Small intestine: peptidases, sucrose, lactase, and maltase
The presence and activity of these enzymes can influence the
absorption of drugs by breaking them down into smaller molecules
that can be absorbed more easily. examples of drugs whose
absorption is influenced by enzymes in the GIT: Acetaminophen,
Warfarin, Penicillin, Lovastatin

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Qustion.4 Explain behavior of your drug in pediatric population in case it is
used in that age group

 Albendazole is not readily accessible in pediatric formulations, yet it

is frequently utilized off-label to address parasitic infections in
children. Its behavior in pediatric patients may deviate from that in
adults due to age-related variances in how the body metabolizes and
responds to drugs. In infants and young children, the liver's metabolic
capacity is not fully developed, potentially impacting Albendazole
clearance and increasing the risk of toxicity. Consequently, pediatric
Albendazole doses are typically lower than those for adults.
Moreover, Albendazole pharmacokinetics in children are influenced
by food intake, with high-fat meals notably enhancing its
effectiveness by improving its solubility. This dietary factor has been
observed to elevate the levels of Albendazole sulfoxide, the active
metabolite. Despite its generally good tolerance, Albendazole's safety
profile in the pediatric population, especially in infants under 6
months old, is not entirely established. Adverse effects such as liver
damage, reduced white blood cell count, and bone marrow
suppression may occur. Therefore, while Albendazole can effectively
treat parasitic infections in children, its usage necessitates careful
consideration of age-appropriate dosages and potential adverse
effects. Consulting a qualified healthcare professional before
administering Albendazole to children is essential.

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 Assignment 2

1. Calculate the daily and weekly dose of Elixir administered if digoxin

is administered as 600 µg tablets daily, F= 0.8 for tablets and F= O.8
for Elixir:
Digoxin each day= 600mg x 0.8= 480mg/day
Elixir daily dose= 480mg/day divided by 0.8 = 600mg/day
Elixir weekly dose= 600 x 7 = 4200mg/ week

2. Calculate administration rate of Aminophylline per day if it is infused

at a rate of 100 mg/hr.
100mg/hr= 1.67mg/min, 24 x 60= 1440min in a day
1.67mg/min x 1440min/day= 24048mg/day of Aminophylline

3. Calculate the maintenance dose of theophylline every 12 hours if

clearance is 6.8 L/hr and the rate of intravenous administration
produces a steady-state plasma theophylline concentration of 30
mg/L.
Maintenance dose= CL x Cssvre x T/ S x F
Maintenance dose = 30mg/L x 6.8L/hr x 12 divided by 1 x 1 = 2448mg/
12hrs

4. Calculate Lidocaine clearance if it is infused continuously at a rate of

5mg/min and if the concentration of lidocaine at steady state is 8mg/L.
Clearance= rate of drug administration/ Css
CL= 5mg/min x 60min/hr divided by 8mg/L
CL= 37.5L/hr

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References:
Albendazole (oral route) proper use (2024) Mayo Clinic. Mayo Foundation for Medical
Education and Research. Available at:
https://www.mayoclinic.org/drugssupplements/albendazole-oral-route/proper-use/drg-
20061505?
p=1#:~:text=Albendazole%20is%20used%20to%20treat%20infections%20caused
%20by%20worms.,only%20with%20your%20doctor's%20prescription
(2024) Albenza, (albendazole) dosing, indications, interactions, adverse effects, and
more. Available at: https://reference.medscape.com/drug/albenza-albendazole-342648
Albendazole oral: Uses, side effects, interactions, pictures, warnings & dosing (no date)
WebMD. WebMD. Available at: https://www.webmd.com/drugs/2/drug-
6261/albendazole-oral/details