Tukarkan separuh hayat kepada pemalar kadar: k = 0.693/t½.
Tukarkan nilai bagi setiap kg kepada jumlah: Vd (L) = L/kg × berat, CL (L/h) = L/kg/h × berat.
Pilih hubungan: C = C₀·e−kt, LD = Vd·C/(S·F), kadar penyelenggaraan = CL·Css/(S·F), τ = ln(Cpuncak/Cpalung)/k.
Untuk fungsi buah pinggang, anggarkan CrCl dengan Cockcroft–Gault dahulu, kemudian skalakan dos atau sela.
Semak keputusan: paras jatuh separuh setiap separuh hayat, dan keadaan mantap mengambil masa kira-kira lima separuh hayat.
2Soalan latihan
1.FarmakologiSederhana
A man taking tamsulosin is planning cataract surgery. What should the nurse advise?
AThe drug has no link with eye surgery
BStop the drug for one day and no further action is needed
CTake a double dose on the day of surgery
DTell the eye surgeon, as it can cause floppy iris syndrome
2.FarmakologiSukar
A woman with chronic hypertension who takes lisinopril is now pregnant. What is the key concern?
ALisinopril has no known fetal effects and should be continued
BAll antihypertensives must be stopped in pregnancy
CACE inhibitors harm fetal kidneys, so a safer drug is used
DLisinopril works better in pregnancy, so the dose should be increased
3.Pengiraan dosSederhana
Berapa miligram ubat m terdapat dalam 50 mL larutan 10% (b/i)?
10% w/v50 mL
m = mg
4.Pengiraan dosSukar
Anda perlu menyediakan 250 mL larutan 0.5% (w/v) daripada larutan stok 20% (w/v). Berapa banyak air W yang mesti ditambah pada stok?
C₁ = 20%C₂ = 0.5%V₂ = 250 mL
W = mL
5.Farmakokinetik klinikalSederhana
Latihan (nilai rekaan, bukan panduan klinikal). Seorang pesakit menerima bolus IV 130 mg gentamicin. Paras yang diekstrapolasi ke belakang kepada masa sifar ialah 8 mg/L dan separuh hayatnya ialah 3 h. Cari klirens CL dalam L/h.
D = 130 mgC₀ = 8 mg/Lt½ = 3 h
CL = L/h
6.Farmakokinetik klinikalSukar
Latihan (nilai rekaan, bukan panduan klinikal). Seorang pesakit menerima vankomisin IV setiap 12 h; klirens vankomisin ialah 4.5 L/h. Apakah dos D dalam mg yang memberikan purata paras keadaan mantap 20 mg/L?
CL = 4.5 L/hτ = 12 hS = 1F = 1Css,avg = 20 mg/L
D = mg
3Larutan
1.Farmakologi
Jawapan: D · Tell the eye surgeon, as it can cause floppy iris syndrome
Mengapa ini jawapannya
Tamsulosin can cause intraoperative floppy iris syndrome, which complicates cataract surgery. The surgeon needs to know so that the technique can be adapted.
Jawapan
D · Tell the eye surgeon, as it can cause floppy iris syndrome
2.Farmakologi
Jawapan: C · ACE inhibitors harm fetal kidneys, so a safer drug is used
Mengapa ini jawapannya
ACE inhibitors and ARBs cause fetal kidney damage, oligohydramnios and other problems, especially later in pregnancy. Drugs such as labetalol, nifedipine or methyldopa are used instead.
Jawapan
C · ACE inhibitors harm fetal kidneys, so a safer drug is used
3.Pengiraan dos
Jawapan: m = 5000 mg
Solution strengths: a percentage strength is grams per 100 mL, so 1% = 1 g/100 mL = 10 mg/mL. A ratio strength 1:1000 means 1 g in 1000 mL = 1 mg/mL; 1:10 000 is 0.1 mg/mL. For a dilution the amount of drug stays the same: C₁·V₁ = C₂·V₂.
Kepekatan
10% = 10 g/100 mL = 100 mg/mL
Jisim ubat
m = 100·50 = 5000 mg
Jawapan
m = 5000 mg
4.Pengiraan dos
Jawapan: W = 243.8 mL
Solution strengths: a percentage strength is grams per 100 mL, so 1% = 1 g/100 mL = 10 mg/mL. A ratio strength 1:1000 means 1 g in 1000 mL = 1 mg/mL; 1:10 000 is 0.1 mg/mL. For a dilution the amount of drug stays the same: C₁·V₁ = C₂·V₂.
Isi padu stok
V₁ = 0.5·250/20 = 6.25 mL
Air untuk ditambah
W = 250 − 6.25 = 243.8 mL
Jawapan
W = 243.8 mL
5.Farmakokinetik klinikal
Jawapan: CL = 3.755 L/h
Klirens dan isi padu: pada keadaan mantap kadar pendosan sama dengan kadar penyingkiran, jadi kadar penyelenggaraan = CL × Css. Dos pemuat ialah LD = Vd × C/(S × F), dengan S faktor garam (pecahan ubat aktif dalam garam) dan F bioketersediaan (1 untuk IV). Daripada dua paras, k = ln(C₁/C₂)/Δt; untuk bolus IV Vd = dos/C₀ dan CL = k × Vd. Nombor hanya untuk latihan; di sisi katil sentiasa ikut protokol tempatan dan minta dos berisiko tinggi disemak dua kali.
Isi padu taburan
Vd = 130/8 = 16.25 L
Pemalar kadar
k = 0.693/3 = 0.231 h⁻¹
Klirens
CL = 0.231·16.25 = 3.755 L/h
Jawapan
CL = 3.755 L/h
6.Farmakokinetik klinikal
Jawapan: D = 1080 mg
Merangka regimen: dengan dos IV pantas, paras jatuh dari puncak ke palung semasa sela, jadi τ = ln(Cpuncak/Cpalung)/k dan dos yang memulihkan puncak ialah Vd × (Cpuncak − Cpalung). Purata paras keadaan mantap ialah Css,avg = S·F·dos/(CL·τ). Infusi meningkat sebagai C = (R/CL)(1 − e−kt). Untuk ubat yang dibersihkan oleh buah pinggang, dos dilaraskan mengikut klirens kreatinina. Nombor hanya untuk latihan; di sisi katil sentiasa ikut protokol tempatan dan minta dos berisiko tinggi disemak dua kali.
Dos
D = Css,avg·CL·τ/(S·F) = 20·4.5·12/(1·1) = 1080 mg