B mn Ha Dc i hc Y

Dc TPHCM

Bupropion +
Naltrexone

GS. TS. L Anh Khoa

PGS. TS. Nguyn Hu
Qun

Bupropion

1-(3-Chlorophenyl)-2-[(2-methyl-2-propanyl)amino]-1-propanone
Naltrexone

(4R,4aS,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy2,4,5,6,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2e]isoquinoline-7-one

C ch tc
ng

https://qph.is.quoracdn.
net/main-qimg8726e1305a48c21e6c3
e2584566057c5?
convert_to_webp=true

- Polypeptide tin thn cha 241 aminoacid

- c phn tch to ra nhiu peptide hormone
- -MSH sn xut bi t bo thn kinh trong nhn arcuate c vai tr quan trng trong s
iu chnh s thm n v hnh vi tnh dc
- -endorphin l peptide opioid ni sinh

C ch tc
ng

http://w
ww.horm
ones.gr/i
mages/2
015%20
DOI/Chri
stou/Chri
stou_1.jp
g

C ch tc
ng
BUPROPION

c ch ti hp thu
dopamine v
noradrenaline. Cc
catecholamine ny
kch thch POMC trong
nhn arcuate ca
hypothalamus. POMC
l tin thn ca -MSH
v -endorphin.
-MSH tc ng ln
cc th th
melanocortin-4
gim lng thc n,
trong khi -endorphin
gi c ch feedback
c ch POMC nn lm
gim hiu ng ny
hn ch tc dng ca
Bupropion khi dng
n tr

C ch tc
ng
NALTREXONE

i khng endorphin ti th th
-opioid, ngn cn
c ch feedback
tng POMC

C ch tc
ng

Tng hp

Oxymorphone

m-Chloropropiophenone

Naltrexone

Bupropion hydrochloride

Kim nghim

altrexone Hydrochloride
CHARACTERS
Appearance
White or almost white powder, very
hygroscopic.
Solubility
Freely soluble in water, slightly soluble in
ethanol (96 per cent), practically insoluble in
methylene chloride.
IDENTIFICATION
A. Infrared absorption spectrophotometry
(2.2.24).
B. It gives reaction (a) of chlorides (2.3.1).

Kim nghim

altrexone Hydrochloride
TESTS
Solution S
Dissolve 0.40 g in carbon dioxide-free water R
and dilute to 20.0 mL with the same solvent.
Acidity and alkalinity
To 10 mL of solution S, add 0.05 mL of methyl
red solution R. Not more than 0.2 mL of 0.02
M sodium hydroxide or 0.02 M hydrochloric
acid is required to change the colour of the
indicator.
Specific optical rotation (2.2.7)
Related substances
Liquid chromatography (2.2.29)
Ethanol (2.4.24, System A)

Kim nghim

altrexone Hydrochloride

ASSAY
Dissolve 0.200 g in 60 mL of ethanol
(96 per cent) R, add 1.0 mL of 0.1 M
hydrochloric acid . Carry out a
potentiometric titration (2.2.20),
using 0.1 M sodium hydroxide. The
curve shows 3 points of inflexion.
Read the volume added between the
first 2 points of inflexion.
1 mL of 0.1 M sodium hydroxide is
equivalent to 37.79 mg of
C20H24ClNO4.
STORAGE
In an airtight container. Protected
from light.

Kim nghim

altrexone Hydrochloride
IMPURITIES
Specified impuritiesA, B, C, D, E, F, G, H, I, J.

A. R = CHO: 17-formyl-4,5a-epoxy-3,14-dihydroxymorphinan-6-one,
B. R = H: 4,5a-epoxy-3,14-dihydroxymorphinan-6-one (noroxymorphone),
C. R = CH2-CH2-CH=CH2: 17-but-3-enyl-4,5a-epoxy-3,14dihydroxymorphinan-6- one,

Dc ng hc
There is a potential
for drug-drug
interactions,
particularly with
those agents that are
metabolized by the
cytochrome CYP2B6
(cyclophosphamide,
propofol, tamoxifen,
valproic acid, etc.).

Bupropion is extensively
metabolized in humans to 3
active metabolites:
hydroxybupropion (hepatic
metabolism via CYP2B6),
threohydrobupropion and
erythrohydrobupropion
(nonCYP metabolism

Dc ng hc
Naltrexone
-Hp thu: sinh kh dng ng ung 5-40%
-Chuyn ha: cht chuyn ha 6--naltrexol
-Bi tit: ch yu qua thn
- half-life for naltrexone and 6--naltrexol is 4 hours and 13 hours

Tc dng ph
Bupropion:Mt ng au u, ng kinh (0,4%), tng huyt p
Naltrexone: bun nn

Vin phng thch ko di: 8 mg naltrexone v 90 mg bupropion

FDA chp thun naltrexone / kt hp bupropion bn trn th trng di tn Contrave
iu tr bnh bo ph trong thng Chn nm 2014
Tun 1: 1 vin mi ngy mt ln vo mi bui sng.
Tun 2: 1 vin mi bui sng v bui ti.
Tun 3: 2 vin mi bui sng v 1 vo bui ti.
Tun 4 tr i: 2 vin mi bui sng v bui ti.