DƯỢC LÍ Goodman & Gilman's The Pharmacological Basis of Therapeutics 12th, 2010

Table 17–4
Structures, Trade Names, and Major Pharmacological Properties of Selected Barbiturates
R 3 O
N C
(or S )* O C 2 3 5C
N C
H O
R 5a
R 5b
SECTION II
NEUROPHARMACOLOGY
COMPOUND DOSAGE t 1/2
(TRADE NAMES) R 3
R 5a
R 5b
FORMS b ( hours) THERAPEUTIC USES COMMENTS
Amobarbital —H —C 2
H 5
—CH 2
CH 2
CH(CH 3
) 2
IM, IV 10-40 Insomnia, pre-op Only Na + salt
(AMYTAL) sedation, emergency administered
management of parenterally
seizures
Butabarbital —H —C 2
H 5
—CH(CH 3
)CH 2
CH 3
Oral 35-50 Insomnia, pre-op Redistribution shortens
(BUTISOL, sedation duration of action of
others)
single dose to 8 hours
Mephobarbital —CH 3
—C 2
H 5
Oral 10-70 Seizure disorders, Second-line
(MEBARAL) daytime sedation anticonvulsant
Methohexital —CH 3
—CH 2
CH:CH 2
—CH(CH 3
)CæCCH 2
CH 3
IV 3-5 c Induction and Only Na + salt
(BREVITAL) maintenance available; single
of anesthesia
dose provides
5-7 min of
anesthesia c
Pentobarbital —H —C 2
H 5
—CH(CH 3
)CH 2
CH 2
CH 3
Oral, IM, 15-50 Insomnia, pre-op Only Na + salt
(NEMBUTAL) IV, rectal sedation, emergency administered
management of seizures parenterally
Phenobarbital —H —C 2
H 5
Oral, IM, IV 80-120 Seizure disorders, First-line anti-
(LUMINAL, status epilepticus, convulsant; only
others) daytime sedation Na + salt
administered
parenterally
Secobarbital —H —CH 2
CH:CH 2
—CH(CH 3
)CH 2
CH 2
CH 3
Oral 15-40 Insomnia, preoperative Only Na + salt
(SECONAL) sedation available
Thiopental —H —C 2
H 5
—CH(CH 3
)CH 2
CH 2
CH 3
IV 8-10 c Induction/maintenance Only Na + salt
(PENTOTHAL) of anesthesia, pre-op available; single
sedation, emergency dose provides
management of seizures brief of anesthesia c
a
O except in thiopental, where it is replaced by S. b IM, intramuscular injection; IV, intravenous administration. c Value represents terminal t 1/2
due to metabolism by the liver; redistribution following
parenteral administration produces effects lasting only a few minutes