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6 Extravascular routes of drug administration

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122 Basic Pharmacokinetics<br />

Table 6.2 Lincomycin, an antibiotic used when patient is allergic to penicillin or when penicillin is inappropriate<br />

Route <strong>of</strong> <strong>administration</strong> Fraction absorbed Mean peak serum concentration (µg mL −1 ) Peak time (h)<br />

Oral a 0.30 2.6 2 to 4<br />

Intramuscular Not available 9.5 0.5<br />

Intravenous 1.00 19.0 0.0<br />

a Not commercially available in the USA.<br />

Table 6.3 Haloperidol (Haldol), a <strong>drug</strong> used for psychotic disorder management<br />

Route <strong>of</strong> <strong>administration</strong> Percentage absorbed Peak time (h) Half life (h [range])<br />

Oral 60 2 to 6 24 (12–38)<br />

Intramuscular 75 0.33 21 (13–36)<br />

Intravenous 100 Immediate 14 (10–19)<br />

Table 6.4 Ranitidine HCl (Zantac)<br />

Route and dose Fraction absorbed Mean peak levels (ng mL −1 ) Peak time (h)<br />

Oral (150 mg) 0.5–0.6 440–545 1–3<br />

Intramuscular or intravenous (50 mg) 0.9–1.0 576 0.25<br />

KaFX0 Ioral =<br />

V (Ka – K )<br />

C p (ng mL –1 )<br />

I IV = (C p ) 0 = X 0 /V = highest concentration value<br />

Oral route<br />

Time (h)<br />

IV route<br />

Slope = –K<br />

2.303<br />

Figure 6.20 Administration <strong>of</strong> a <strong>drug</strong> by intravascular (IV) and extravascular (oral) <strong>routes</strong> (one-compartment model). Even for<br />

<strong>administration</strong> <strong>of</strong> the same dose, the value <strong>of</strong> plasma concentration (Cp) at time zero [(Cp)0] for the intravenous bolus may be<br />

higher than the intercept for the extravascular dose. This will be determined by the relative magnitudes <strong>of</strong> the elimination rate<br />

constant (K ) and the absorption rate constant (Ka) and by the size <strong>of</strong> fraction absorbed (F) for the extravascular dosage form. X0,<br />

oral dose <strong>of</strong> <strong>drug</strong>; X0, IV bolus dose <strong>of</strong> <strong>drug</strong>.<br />

t 1/2 =<br />

Sample chapter for Basic Pharmacokinetics 2nd edition<br />

0.693<br />

K

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