BILIRUBIN - keywords
O
metalloporphyrins block
competitively
COOH
N
N
[-]
80 % RBC
20 % shunt heme/ineffective
erythropoiesis
limit hemolysis
block heme
oxygenase
O
ivIg
ABO and Rh
asap
N
4Z-15Z
N
COOH
O2
COOH COOH
Fe++
NADPH
O2
Fe+++
CO
?
O
N
N
N
N
O
heme
biliverdin
bilirubin IXα
polar
polar
apolar
crosses placenta
crosses placenta
crosses placenta
heme oxygenase
biliverdin reductase
microsomes
cytoplasm
inducible
only mammals and sh
fi
HO 1: spleen, liver
HO 2: brain
limit hemolysis
block heme
oxygenase
OFRs
biliverdin
bilirubin
BVR
at Bf < 70 nmol/L B is recycled to neutralize
large amounts of OFRs
BVR main membrane antioxidant ?
(like glutathion in cytoplasm)
BVR expression in penumbra
role in Alzheimer’s
the jaundice of the cell PNAS Greenberg 2002
Bf
limit hemolysis
block heme
oxygenase
(at pH 7.4 with pK 8.0)
H+
H+
80 %
monitor Bf
H+
H+
H+
16 %
2%
H+
H+
max solubility 70 nMol/L at pH 7.4
> 70 < 1000 nMol/L oligomers and
metastable aggregates: self-aggreagation
ongoing from about TSB 85 µMol/L
fl
unsoluble macroprecipitates if Bf > 1000
nMol/L
reversible membrane
effects: altered lipid
polarity and uidity
irreversible
membrane
effects Bf > 70
nMol/L (4 µg/dL)
Bf underestimated at
higher [ ]
FFAs
allosteric interaction at FFA/A
molar ratio of 2-3
direct interaction at loose sites
>3
Balb
TPN, hypoglycaemia, heparin,
infection, hypothermia
loose binding
primary tight binding
several sites
equimolar would be 8.2 mg per
gram (B 10 mg/dL = 171 µmol/
L)
competitive displacement
by organic anions
drug interaction
(ceftriaxone 3.0,
furosemide 1.07,
cefotaxim 1.05,
rifampycin)
sick preterms (0.5) < sick
terms (0.7) < healthy terms
(0.9)
limit hemolysis
block heme
oxygenase
monitor Bf
maintain albumin level
avoid displacers
monitor FFAs
glutathion S transferase
(ligandin)
Disse space
Kuppfer cell
hepatocyte
transition to normal level in
about 10 days = second stage
of physiological icterus
prevents re ux into blood
sinusoid
endothelium
limit hemolysis
block heme
oxygenase
bile canaliculus
carrier mediated, facilitated
diffusion
passive diffusion at high
levels of Bf
maturation in brain does not
explain regional pattern of
kernicterus
monitor Bf
maintain albumin level
avoid displacers
monitor FFAs
increase uptake
enhance
glucuronidation
glucuroconjugation
day 3 diconjugates ~ 21 % of the conjugated
fraction COHb %/TCB%
adult levels achieved after a few weeks; low
levels contribute to early peak in physiological
jaundice; normal function at > 50 % levels
induction of endoplasmic reticulum mass by
phenobarbitone requires 2-5 days (plant
derivatives used in Asia); phenobarbitone may
alter brain bilirubin oxidation
fl
screen for G6PDH
UDPGT
- promotor: Gilbert’s
- gene: Crigler-Najjar I/II
- G6PDHdef (drugs, teas,
mothballs, favism)
enterohepatic
recirculation
Disse space
Kuppfer cell
hepatocyte
follows deconjugation
role of meconium
evacuation
sinusoid
endothelium
limit hemolysis
block heme
oxygenase
bile canaliculus
excretion into bile
mono- and diconjugates
photo-isomers
lumirubin
ß and γ isomers
saturable, rate limiting,
carrier mediated
calciumbinding
BF x 6 > 250 µmol/L
340 = alert
510 = never
monitor Bf
maintain albumin level
avoid displacers
breast feeding
monitor FFAs
jaundice ≠ breast
milk jaundice (ßglucuronidase)
increase uptake
enhance
glucuronidation
prevent recirculation
Causes/risk factors for increased plasma unconjugated bilirubin
Haemolysis
Traumatic birth associated with haemorrhage and tissue contusion
Neonatal polycythaemia
Sepsis
Hypoxia
Hypoglycaemia
Autosomal-inherited disorders
Crigler–Najjar types 1 and 2
Gilbert's disease
Galactosaemia
Fructose intolerance
Congenital hypothyroidism
Crigler–Najjar type 1
(UDPGT 1 exon)
Crigler–Najjar type 2
(UDPGT af nity for bili)
Gilbert's disease
(UDPGT promotor)
Unconjugated hyperbilirubinaemia 200–400 µmol/l, needs phototherapy, phenobarbitone=no effect
Unconjugated hyperbilirubinaemia 100–400 µmol/l, needs phototherapy, phenobarbitone effective
Unconjugated hyperbilirubinaemia 100–300 µmol/l is common and usually resolves after brief
exposure to phototherapy
Alagille's
Variable—includes paucity of bile ducts, pulmonary artery stenosis, triangular facies
(JAG1, notch signalling)
Alpha-1 antitrypsin de ciency Growth restriction in utero, severe cholestasis often with pale stools, 2% present with vitamin-K(protease inhibitor chro 14)
sensitive coagulopathy
Bile acid synthesis disorders
hydroxy-steroid dehydrogenase Normal GGT, low serum bile acids, no pruritis
oxosteroid reductase
Severe jaundice and coagulopathy
25diOHcholanic cleavage
Normal GGT, elevated ALP and cholesterol, pruritis
Cystic brosis
Jaundice, hepatomegaly, meconium ileus, inspissated bile syndrome, pale stools
Dubin–Johnson syndrome
Conjugated bilirubin (30–400 µmol/l), transaminases normal, centri-lobule pigment granules on liver biopsy
PFIC type 1 Byler's disease
(MDR1)
PFIC type 2
(bile salt export pump)
PFIC type 3
(MDR3)
Normal GGT, normal cholesterol, variable jaundice, pruritis (diarrhoea±pancreatitis)
Normal GGT, no intestinal symptoms, giant cell hepatitis common
Elevated GGT, troublesome pruritis
Accumulation of very long-chain fatty acids (C27), large fontanelle, high forehead, profound hypotonia
fi
Zellweger's
(bile acid side chain)
fi
Conjugated hyperbilirubinaemia, but no accumulation of bile acids in the liver and normal liver function tests
fi
Rotor syndrome
H+
toxicity=
[Bf] x exposure time
H+
limit hemolysis
block heme
oxygenase
monitor Bf
maintain albumin level
avoid displacers
monitor FFAs
brain capillary
astrocyte
decreased glu reuptake
inhibited PKC activity
endothelium
neuron
mitochondrion
ependyma
prevent recirculation
limited para- and
transcellular diffusion
transmembrane passage
not restricted
contact time: CBFlow
(CO2), congestion and
duration of jaundice
increase uptake
enhance
glucuronidation
prevent capillary
injury
reduce contacttime
open BBB
local hemolysis
apoptosis
necrosis at higher []
regional selectivity (motor and auditory)
enhanced by hypoxia
neurones 1.5 more sensitive than astroglia
limit hemolysis
block heme
oxygenase
monitor Bf
maintain albumin level
avoid displacers
monitor FFAs
ursodeoxycholic acid
inhibitor of apoptosis
proteins
increase uptake
enhance
glucuronidation
prevent recirculation
acidosis
more BH2 aggregation
higher CBF
injury to BBB
effect on alb binding ?
prevent capillary
injury
reduce contacttime
prevent apoptosis
treat acidosis
BBB
bidirectional, facilitated diffusion
R
A
TP
OA
MD
MR
P
MRP
P
maintain albumin level
avoid displacers
monitor FFAs
increase uptake
enhance
glucuronidation
low CSF protein &
similar ratio B/A
prevent recirculation
MDR
steep [] gradient
B-CSF
- ef ux of lipophilic substances
- inhibitors of MDR may
contribute to KI: ceftriaxone,
verapamil, rifampicin
fl
monitor Bf
MR
OATPA
MRP
OATPA
ABC transporter (ATP hydrolysis)
unidirectional towards blood
fi
bili induces
MRP1,
promotes
traf cking from
Golgi to plasma
membrane
MRP
OATPA
limit hemolysis
block heme
oxygenase
MDR
ABC transporter (ATP hydrolysis)
unidirectional either to CSF or to blood
upregulated by astrocytes at BBB
prevent capillary
injury
reduce contacttime
prevent apoptosis
treat acidosis
enhance extrusion
limit hemolysis
block heme
oxygenase
monitor Bf
maintain albumin level
avoid displacers
monitor FFAs
4Z,15Z
bilirubin conjugation
bilirubin oxidation
increase uptake
enhance
glucuronidation
prevent recirculation
prevent capillary
injury
reduce contacttime
prevent apoptosis
treat acidosis
enhance extrusion
limit hemolysis
block heme
oxygenase
≥ 30 Mw/cm2/nm
monitor Bf
surface area
maintain albumin level
avoid displacers
monitor FFAs
around 460 nm
increase uptake
enhance
glucuronidation
4Z,15Z
4Z,15E
fi
lumi
con gurational isomers
- immediate
- T1/2 > 12 hours
- reversible in bile and gut
lumirubins
- slower generation
- intensity-dependent
- T1/2 short (few hours)
- irreversible
prevent recirculation
prevent capillary
injury
reduce contacttime
prevent apoptosis
treat acidosis
enhance extrusion
effective photoR/
limit hemolysis
block heme
oxygenase
monitor Bf
maintain albumin level
avoid displacers
monitor FFAs
increase uptake
enhance
glucuronidation
prevent recirculation
prevent capillary
injury
reduce contacttime
prevent apoptosis
treat acidosis
enhance extrusion
effective photoR/
limit hemolysis
block heme
oxygenase
monitor Bf
to prevent kernicterus is much more than
just following phototherapy schemes
to understand all options, all
molecular steps in the bilirubin
metabolism have to be understood
maintain albumin level
avoid displacers
monitor FFAs
increase uptake
enhance
glucuronidation
prevent recirculation
prevent capillary
injury
reduce contacttime
prevent apoptosis
treat acidosis
enhance extrusion
effective photoR/