Digoxin Phenytoin Cyclosporin Tacrolimu Sirolimus Lithium CBZ VA Phenobarb

e s
Biphasic Distribution Distributio Distribution
phase: Large n phase: phase does
8-12h 6h not relate
to efficacy
and safety
Plasma 25% 90% Significant Extensive Extensive Bound to High
protein albumin
binding and alpha Saturation at
acid > 50 mcg/mL
glycoprotei
n
T1/2 36h 22h 7h 8-12h 62h Elimination 35h Short acting Long acting
phase: 18- => divided => once
24h Chronic doses daily
t1/2 = 11-
27h 4-17h 5 days

Vd 7 L/kg (use 0.65 L/kg 4-5 L/kg 1 L/kg 12 L/kg 0.7 L/kg 0.8-3 L/kg 0.1-0.5 L/kg 0.7 L/kg
IBW unless
ABW < IBW) (1L/kg in 0.9 L/kg in
neonates neonates
If CrCl<30 and
Vd = (226 + children <1
(298*CrCl / yr)
29.1 + CrCl)
* wt/70) Obese:
0.65*(IBW
+1.3 (TBW-
IBW)
 Onset PO: 1-2h
IV: 5-30 min
Peak PO: 2-8h
IV: 1-4h
F Tablet: 70% 1 30% 25% Solution:14 1 if IR 0.8 IR: 1 1
Elixir: 80% (<1 in % 0.75 if SR ER: 0.9
Liquid certain Food Tablets:18 Food S = 0.9 for
capsule: cases) decreases % Rapid increases Rapid IM & IV
95% absorptio absorption absorption absorption
Absorption: n High fat
non linear meal Tmax = Absorption
increases 15-45 min : zero
absorption if solution order
1-3h if IR
4-12h if SR
Dose LD: 1-1.5mg LD: 2.5 – 5 0.1 mg/kg LD: 6-15mg Start: 600- 10-15 5-10 Adults:
PO divided Adults: 10- mg/kg BID BID MD: 2-5mg 900 mg/kg/day mg/kg/day 1-3
LD = (AFib) 15 mg/kg daily mg/day in in 2 or 3 Titrated 250- mg/kg/day
Css*Vd/F (max 2-3 divided divided 500 mg q 3
MD: infusion doses doses days Peds: 2-5
MD = 0.25mg/day 50mg/min) mg/kg/day
(Css*Cltotal* Peds: 15-20 MD: 900- Max Max
τ)/SF CrCl < 20: mg/kg (max 1800mg/da 1200mg 60mg/kg/da
LD = 0.5mg infusion 1-3 y per day y At bedtime
PO mg/kg/min) (1200mg if
MD = elderly) IV LD = 25 Start ¼ 1st
0.125mg/da MD: mg/kg week then
y Adults: 4-7 300mg = titrate ¼
mg/kg/day 8.12mEq over 3
Peds: 4-10 weeks
mg/kg/day 5mL =
 8mEq LD divided
DD = Vm*Css into 3 doses
/ Km+ Css 1/3 q8h
Vm = 7
mg/kg/day Give ½ dose
Km = 4mg/L when
administere
d with VA
Therapeutic CHF: 10-20 100 – 250 5-15 5-15 ng/mL [] co-relate 4-12 50-100 15-40
range 0.5-1 mcg/L mcg/mL ng/mL ng/mL with mcg/mL mcg/mL mcg/mL
(0.8) efficacy
AFib: If hypoalbu- and safety
0.8-2 mcg/L minemia:
(1.2) Corrected 0.6-1.2
level = mEq/L
measured /
(0.2*albumi
n + 0.1)

If CrCl < 15
Corrected
level =
measured /
(0.1*albumi
n + 0.1)
Monitoring Trough IV: >2h Trough (SS: SS: 3-4 SS: 20-25 Full SS: 3-5 Trough: q1-2 2 weeks to
1-4h before after 1-2 day) days days response days weeks for 2 reach SS
dose infusion after 1-2 months then
IM: >4h weeks Trough q1- q3-6 months
after 2 weeks
injection SS: 3-5 for 2-3
 PO: within days months
3-4 days Monitor then q4-6
Then q6 qweek for months
months 1 month
then q6-12
months
Metabolism Kidney CYP 2C9/19 Gut CYP Gut CYP Gut CYP Renal 99% in the Minimal in Renal
& (75%) 3A4 3A4 3A4 liver urine (40%) &
Elimination Renal < 5% metabolism metabolis metabolism Hepatic
Hepatic + m Induces its Metabolized (60%)
Biliary (25%) Pgp efflux Pgp efflux own by liver
Pgp efflux metabolis enzymes
Enterohepa m (2-5
tic days  2-4 Toxic
circulation weeks) metabolite
occurs =>
hepatotoxici
ty
Cl 1.303*CrCl + 5-10 0.04-0.08 140-220 0.25*CrCl 0.06 L/kg/h
Clnr mL/kg/min L/kg/h mL/kg/h

Clnr = = 0.3-0.6 = 0.14-0.22

40mL/min (if L/kg/h L/kg/h
no HF, or
mild sx)
20mL/min (if
HF stage
3/4)
Dosage PO Chewable IR: 150, IR: 100, Capsules: Oral
forms tablets 300, 200mg 125, 250mg Rectal
& strengths IV (given 600mg IM
 over 5-10 Suspension CR: 100, Tablets: 125,
min) SR: 300, 200, 250, 500mg Tablets (15,
Capsules 450mg 400mg 30, 60,
Not IM ER: 500mg 100mg)
(erratic and IV Oral syrup SR: 200,
painful) 300mg Injection: IV & IM (30,
IM (fos- 500mg/5mL 60, 65,
phenytoin) PO PO solution: 130mg/mL)
1.5mg suspension 250mg/5mL
fosphen = : PO elixir
1mg phen 100mg/5m (15mg/5mL
L &
100, 200, 20mg/5mL)
300mg No IV
Pregnancy Excreted Pregnancy Teratogenic Crosses
& into category D placenta
Breastfeedi breastmilk Compatible and is
ng Excreted in with excreted in
D/C in 1st breastmilk breastfeedin breastmilk
trimester g
of  CI
pregnancy
Comments Anticholi-
nergic
activity