Pick the relation: C = C₀·e−kt, LD = Vd·C/(S·F), maintenance rate = CL·Css/(S·F), τ = ln(Cpeak/Ctrough)/k.
For kidney function, estimate CrCl with Cockcroft–Gault first, then scale the dose or the interval.
Check the result: levels fall by half every half-life, and steady state takes about five half-lives.
2Practice problems
1.PharmacologyMedium
A patient given haloperidol develops a sudden painful twisting of the neck and the eyes roll upward. Which drug is usually given?
ADantrolene by mouth to relax the twisted neck muscles
BA second dose of haloperidol
CNaloxone
DAn anticholinergic such as benzatropine (benztropine)
2.PharmacologyHard
A patient on warfarin is taught about diet. Which statement shows a need for further teaching?
A"I will keep the amount of green leafy vegetables I eat about the same each week."
B"I will stop eating all green vegetables from now on."
C"I will use a soft toothbrush and an electric razor."
D"I will tell my dentist that I take warfarin."
3.Dosage calculationsMedium
A patient weighs 18 kg and is prescribed 20 mg/kg as a single dose. Find the dose D in mg.
18 kg20 mg/kg
D = mg
4.Dosage calculationsHard
An infusion contains 50000 units of a drug in 1000 mL. The prescription is 1500 units per hour. At what rate R do you set the pump, in mL/h?
50000 units/1000 mL1500 units/h
R = mL/h
5.Clinical pharmacokineticsMedium
Practice exercise (made-up values, not clinical guidance). A 56 kg patient is to receive an aminophylline infusion (salt factor S = 0.8: 80% of aminophylline is theophylline). The theophylline clearance is 0.03 L/kg/h. What aminophylline infusion rate R in mg/h gives a steady-state theophylline level of 12 mg/L?
56 kgCL = 0.03 L/kg/hCss = 12 mg/LS = 0.8
R = mg/h
6.Clinical pharmacokineticsHard
Practice exercise (made-up values, not clinical guidance). A 64 kg patient has a phenytoin level of 8 mg/L; the target is 20 mg/L. The drug is given intravenously as phenytoin sodium (S = 0.92), and the volume of distribution is 0.7 L/kg. What extra loading dose LD raises the level to the target?
64 kgVd = 0.7 L/kgC = 8 → 20 mg/LS = 0.92
LD = mg
3Solutions
1.Pharmacology
Answer: D · An anticholinergic such as benzatropine (benztropine)
Why this is the answer
Acute dystonia is caused by dopamine blockade, which leaves acetylcholine activity relatively high. An IM or IV anticholinergic usually relieves it within minutes.
Answer
D · An anticholinergic such as benzatropine (benztropine)
2.Pharmacology
Answer: B · "I will stop eating all green vegetables from now on."
Why this is the answer
Patients on warfarin should keep their vitamin K intake consistent rather than avoid it. Sudden changes in green vegetable intake can make the INR unstable.
Answer
B · "I will stop eating all green vegetables from now on."
3.Dosage calculations
Answer: D = 360 mg
Dose calculation: the amount to give equals what is prescribed divided by what you have, times the quantity it comes in: amount = (desired dose/stock strength) × stock volume. Always keep the units the same (convert g to mg, mg to mcg first) and check that the answer is sensible.
Dose
20·18 = 360 mg
Answer
D = 360 mg
4.Dosage calculations
Answer: R = 30 mL/h
Dose calculation: the amount to give equals what is prescribed divided by what you have, times the quantity it comes in: amount = (desired dose/stock strength) × stock volume. Always keep the units the same (convert g to mg, mg to mcg first) and check that the answer is sensible.
Concentration
50000/1000 = 50 units/mL
Pump rate
R = 1500/50 = 30 mL/h
Answer
R = 30 mL/h
5.Clinical pharmacokinetics
Answer: R = 25.2 mg/h
Clearance and volume: at steady state the dosing rate equals the elimination rate, so the maintenance rate = CL × Css. A loading dose is LD = Vd × C/(S × F), with S the salt factor (fraction of active drug in the salt) and F the bioavailability (1 for IV). From two levels, k = ln(C₁/C₂)/Δt; for an IV bolus Vd = dose/C₀ and CL = k × Vd. The numbers are for practice only; at the bedside always follow local protocols and have high-risk doses double-checked.
Clearance
CL = 0.03·56 = 1.68 L/h
Infusion rate
R = CL·Css/S = 1.68·12/0.8 = 25.2 mg/h
Answer
R = 25.2 mg/h
6.Clinical pharmacokinetics
Answer: LD = 584.3 mg
Designing a regimen: with rapid IV doses the level falls from peak to trough during the interval, so τ = ln(Cpeak/Ctrough)/k and the dose that restores the peak is Vd × (Cpeak − Ctrough). The average steady-state level is Css,avg = S·F·dose/(CL·τ). An infusion rises as C = (R/CL)(1 − e−kt). For a drug cleared by the kidneys, the dose is scaled with the creatinine clearance. The numbers are for practice only; at the bedside always follow local protocols and have high-risk doses double-checked.
Volume of distribution
Vd = 0.7·64 = 44.8 L
Rise needed
20 − 8 = 12 mg/L
Loading dose
LD = 44.8·12/(0.92·1) = 584.3 mg
Answer
LD = 584.3 mg
In practice the dose is rounded to a convenient amount.