Adverse Reaction:
Hypotension, nausea, vomiting, dry mouth, stomach pain.
Somnolence, dizziness, confusion, anxiety, euphoria.
Floating feeling, nervousness, parathesia,
abnormal dreams, agitation. Sweating.
Pharmacology/ Pharmacokinetics:
Ref- Drug Facts And Comparisons(2010)
Pharmacology:
Butrophanol is a potent analgesic with both narcotic agonist and antagonist effects. The exact mechanism of action is inknown. Narcotic anatgonist analgesics may exert analgesic effect via the CNS mechanism.
Pharmacokinetics:
Butrophanol is extensively metabolised in the liver,the major metabolite being hydroxybutorphanl.
The elimination half-life of hydroxybutorphanol may be greater than the parent compound.
Elimination occurs in urine(about 80%) and feces( about 15%).
Mean pharmacokinetics Parameters of Butorphanol IV
in Younger and Elderly Subjects
Parameters Younger Elderly
AUC (inf) 7.24 (1.57) 8.71(2.02)
ng*h/mL (4.4 to 9.77) 4.76 to 13.03)
Half-life(h) 4.56 (1.67) 5.61(1.36)
(2.06 to 8.7) 3.25 to 8.79
Volume of 487(155) 552(124)
distribution(L) (305 to 901) (305 to 737)
Total body 99 (23) 82(21)
clearance (L/h) (70 to 154) (52 to 143)
Younger subjects (n=24) are from 20 to 40 years
Elderly subjects (n=24) are greater than 65 years of age
AUC area under the curve after 1mg dose
BUTORPHENOL INTRANASAL-
Mean pharmacokinetic Parameters of Butorphenol
in Younger and Elderly subjects
Parameters IV Nasal
Younger Elderly Younger Elderly
t max(h) - - 0.62(0.32) 1.03(0.74)
(0.15 to 1.5) (0.25 to 3)
Cmax - - 1.04 (0.4) 0.9 (0.57)
(0.35 to1.97) 0.1 to 2.68)
AUC (inf) 7.24 (1.57) 8.71(2.02) 4.93(1.24) 5.24 (2.27)
(ng*h/mL) (4.4 to 9.77) 4.76 to13.03) (2.16 to 7.27) (0.3 to 10.34)
Half-life(h) 4.56 (1.67) 5.61(1.36) 4.74 (1.57) 6.56 (1.51)
(2.06 to 8.7) (3.25 to 8.79) (2.89 to 8.79) (3.75 to 9.17)
Absolute - - 69(16) 61(25)
bioavail (44 to 113) (3 to 121)
ability (%)
Volume of 487(155) 552 - -
distribution (305 to 901) (305 to 737)
(L)
Total body 99(23) 82(21) - -
clearance (70 to 154) (52 to 143)
(L/h)
Younger subjects (n=24) are from 20 to 40 years old
Elderly subjects (n-24) are greater than 65 years of age
Peak plasma concentration normalized to 1mg dose
Area under te plasma concentration curve after 1mg dose
( range obsrved values)