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Lecture notes study book The Book of Drugs of Mike Doughty - ISBN: 9780306820502 (CASE STUDIES ETC)
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1.Salbutamol
Tab/Cap
(aka
Albuterol)
Brand
-‐
Ventolin
Tab
2mg
Cat
-‐
P
only,
Preg
C
AI
-‐
Bronchodilator
in
reversible
AWO
(asthma,
COPD)
-‐
-‐
exercise-‐induced
bronchospasm
-‐
Manage
uncomplicated
premature
labor
in
last
trimester
MOA
-‐
Selective
B2
agonist,
relaxes
bronchial
SM
w
little
effect
of
HR
ADME
-‐
A:
Peak
effect:
2-‐3h,
Duration:
4-‐6h,
F:
~50%
PO
-‐
M:
Sig
1st
pass
by
liver
to
phenolic
sulphate
-‐
E:
1ly
urine
w
30%
unchanged
drug
t0.5:
3.7-‐5h
Dosing
-‐
Bronchospasm
-‐
Children:
2-‐6y:
0.1-‐0.2mg/kg/dose
TDS,
max
12mg/day;
6-‐12y:
2mg/dose
T/QDS,
max
24mg/day;
ER:
4mg
BD,
max
24mg/day
-‐
Adults:
2-‐4mg
T/QDS,
max
32mg/day;
ER:
8mg
BD,
max
32mg/day
-‐
Elderly:
2mg
T/QDS,
max
32mg/day,
w
water
1h
b4
or
2h
aft
meals
-‐
Premature
Labor:
Aft
IV
&
under
control,
may
continue
4mg
T/QDS
SE
-‐
CVS:
tachy,
palpi,
arrhythmia
-‐
CNS:
HA,
tremor,
nervous
-‐
GI:
NVD,
dry
mouth
-‐
Resp:
cough,
worsen
asthma
-‐
Rash,
allergic
rxn
-‐
Caution
in
DM/hyperthyroid/CVS
disorder
like
HTN
&
coro
insufficiency
-‐
corticosteroid,
diuretics/xanthine:
increases
hypoK
risk,
recommend
to
monitor
K
in
severe
asthma
w
combi
therapy
-‐
ER:
caution
in
pts
with
CV
disorders,
may
cause
paradoxical
bronchospasm
CI
-‐
Hypersen
to
salbuterol,
adrenergic
amines
-‐
Not
w
non-‐selective
BB
-‐
Extreme
caution
if
on
MAOI/TCA
PE
-‐
Common
AE:
tremors,
HA,
nervous,
palpi,
tachy
-‐
SOB/allerfic
rxn:
stop
med
&
see
doc
2.
Humulin
30/70
(vial,
penfilled
cartridge),
Mixtard
30
(vial,
novolet,
penfill)
Brand
-‐
70%
NPH,
30%
Reg
Insulin
(100U/ml)
Cat
-‐
P
only,
Preg
B
AI
-‐
T1DM
&
T2DM:
Monotherapy/
adjunct
to
other
oral
antidiabetic
MOA
-‐
Exogenous
insulin
-‐
Adipocytes:
incr
glc
uptake,
lipogenesis,
dec
lipolysis
-‐
Muscle:
incr
glc
uptake,
incr
glycogenesis,
incr
protein
synthesis
-‐
Liver:
dec
gluconeogenesis
&
glycogenolysis,
inc
glycogenesis
ADME
-‐
Onset:
30-‐60min
-‐
Peak:
4.4h
(1.5-‐16h)
-‐
Duration:
10-‐16h,
max
up
to
18-‐24h
Dosing
-‐
SQ
according
to
U
required,
30mins
b4
meal
-‐
Can
be
admin
BD
as
basal-‐bolus,
usually
2/3
in
morning,
1/3
in
evening,
for
any
one
injection,
dose
shouldn’t
>
50U
SE
-‐
Hypo:
hunger,
pallor,
fatigue,
perspire,
palpi,
tachy,
tremors,
blurred
vision,
confusion
-‐
Local
sen:
pruritus,
erythema,
swelling,
stinging,
warmth
at
injection
site
-‐
Rare
sys
sen
rxn:
generalized
urticaria,
wheezing,
dyspnea,
hypotension,
tachy
-‐
Wt
gain,
lipoastrophy,
lipohypertrophy
CI
-‐
Hypoglycemia
PE
-‐
S
&
s/x
of
hypo
&
management
(15,15,15)
-‐
Self-‐injection
tech:
site,
method,
proper
eq
(syring
size,
needle
gauge)
-‐
Prepare
insulin
dose,
check
type
and
exp,
inspect
vial
b4
withdrawal
&
withdrawing
dose
-‐
Store
at
2-‐8dc,
no
freeze,
corresponding
exp
-‐
Regular
f/u
on
A1c,
eye
exam,
lipid
panel,
neuropathy,
renal
fn
screen,
foot
exams
3.
Tolbutamide
Brand
-‐
Generic
by
DHA,
Tab
500mg
Cat
-‐
POM,
Preg
C
(FDA,
TGA)
AI
-‐
Adjunct
to
diet
for
T2DM
st
MOA
-‐
Short-‐acting
1
gen
SU:
Binds
to
SU
receptor
on
functuinal
beta
cells,
-‐
K-‐ATP
pump,
+
insulin
synthesis
&
release
-‐
+
Initial
rapid
peak
release
but
no
prolonged
basal
release
ADME
-‐
A:
Food
no
effect
on
absorption
(admin
0.5h
b4
meal
to
control
postprandial)
-‐
D:
80-‐99%
bound,
Vd
6-‐10L
-‐
M:
extensively
metab
cyp2C9
(oxidized)
in
liv
to
2
inactive
metab
-‐
E:
extensively
excreted
in
urine
as
metab
(75-‐80%
w/i
24h)
st
-‐
DDI:
Incr
hypo
risk
w
other
antidiabetic
like
incretin
therapies.
Alter
BG
(hypo)
w
FQ.
Disulfiram-‐like
rxn
w
EtOH,
esp
1
gen
Dosing
-‐
15-‐30
min
b4
meal
-‐
Initial:
1-‐2g/day
single
dose
in
morn
or
divided,
Maintain:
0.25-‐3g/day
-‐
Dosing
adjustment
for
hepatic
impairment,
recommended
in
renal
impairment
SE
-‐
Hypo:
esp
in
elderly,
renal/hepatic
insufficient,
pts
on
other
anti-‐diabetic
&
alcohol
, -‐
NVDC,
Wt
gain
-‐
Bld
dyscrasias:
leukopenia,
thrombocytopenia
(rare)
-‐
Skin
hypersen
rxn
(subside
w
use),
prutitus,
erythema
-‐
Rare
hepatic
dysfn
&
jaundice
-‐
Avoid
during
P/L,
severe
H/R
insufficient,
acute
porphyria
CI
-‐
Ketoacidosis
-‐
SU
hypersen
-‐
Monotherapy
for
T1DM
PE
-‐
Used
w
proper
diet
&
exercise
to
control
high
BG
in
T2
DM
-‐
BG
control
–
kidney
damage,
blindness,
loss
of
limbs.
Dec
risk
of
heart
atk,
stroke
-‐
SE:
VD,
wt
gain
(may)
-‐
Stop
&
see
doc:
easy
bleeding/bruising,
sx
of
infection
(sore
throat,
fever),
severe
skin
rxn/rash/hives,
dark
colored
urine/light
colored
stool,
yellow
skin/eyes
-‐
Hypo
esp
if
on
other
antidiabetic,
after
heavy
exercise,
skip
meal
(cold
sweat,
blurred
vision,
dizzy,
drowsy,
palpi,
faint,
hunger).
Eat
glc
tab
or
simple
sug
(tab
sug,
honey,
candy)
-‐
Interacts
w
med.
Tell
doc
-‐
Avoid
alcohol
4.
Metformin
Tab
Brand
-‐
Diabetmin
FCT
(850),
Diabetmin
T
(500),
Diaformin
FCT
(500),
Glucophage
1000
FCT,
Glucophage
FCT
(500/850),
Glucophage
XR
ERT
(500/750),
Glycomet
T
(500/850),
Glyformin
FCT
(500),
Metforal
850
CT,
Beacons
T
(250/500),
Camden
T
(500),
DHA
T
(250/500),
Sunward
FCT
(250/500),
Synco
T
(500),
Teva
FCT
(850),
SP-‐Glucomet
FCT
(500)
Cat
-‐
POM,
Preg
B
AI
-‐
T2DM
as
monotherapy
when
X
be
managed
w
diet
&
exercise
alone
st
-‐
1
choice
in
overweight
pts
-‐
May
be
used
w
SU
or
insulin
to
improve
glycemic
control
MOA
-‐
Dec
hepatic
glc
production,
dec
intestinal
glc
absorption,
improves
insulin
sen
(inc
peripheral
glc
uptake
&
use)
-‐
Unlike
SU:
x
incr
insulin
secretion,
x
hypo
at
therapeutic
doses
exp
in
special
situations,
x
weight
gain
ADME
-‐
A:
Onset
w/I
days,
max
up
to
2
wks,
F:
PO
regular
release
50-‐60%,
time
to
peak:
immediate
2-‐3h,
ER
7h
(4-‐8h)
-‐
D:
Vd
654+-‐358L,
partitions
into
RBC,
negligible
protein
binding
-‐
M:
not
by
liver
-‐
E:
urine
(90%
unchanged,
active
secretion),
t0.5
plasma:
4-‐9h
Dosing
-‐
Allow
1-‐2wk
b4
dose
titration.
Lower
starting
dose
&
gradual
inc
to
minimize
GI
s/x
-‐
Immediate
release
-‐
10-‐16yo:
initial
500mg
BD
w
meal,
daily
dosage
made
in
increments
of
500mg
wkly
given
in
divided
dose,
max
2000mg/day
-‐
>16:
initial
500mg
BD
w
meal
(incr
by
1
tab/day
wkly)
or
850mg
OD
w
meal
(incr
by
1
tab/day
EOW),
doses
up
to
2000mg/day
given
BD,
>2000mg
given
TDS,
max
2550mg/day
-‐
Extended
release
(Glucophage
XR
RR
Tab):
>16:
initial
500mg
OD
w
meal,
incr
by
5000mg
wkly,
max
2000mg
OD
-‐
Renal
impairment:
CI
if
sCr
>
1.5mg/dL
(m),
>1.4mg/dL
(f)
and
in
pts
with
abnormal
Cl,
avoid
in
pts
with
CrCl
<
60-‐70ml/min
-‐
Hepatic
impairment:
Avoid,
liver
disease
is
RF
for
developing
lactic
acidosis
-‐
Dosing
in
geriatric
pts:
X
use
in
pts
>
80yo
unless
normal
renal
fns.
Initial
&
maintenance
dose
should
be
conservative
due
to
potential
for
dec
renal
fn,
X
use
max
dose
SE
-‐
GI:
NVD,
flatulence,
indigestion,
ab
discomfort
-‐
NMS:
weakness
-‐
CVS:
flushing,
palpi
-‐
CNS:
HA,
chills,
dizzy,
light-‐headed
-‐
Rash,
Dec
Vit
V12
lvl
Cautions:
not
recommended
during
P/L
(cat
B),
lactic
acidosis
is
rare
but
severe
CI
-‐
Hypersen
-‐
Renal
disease
(sCr
>
1.5
in
m
or
>
1.4
in
f)
-‐
Abnormal
CrCl
(shock,
AMI,
septicemia)
-‐
CHF
requiring
pharm
Tx
-‐
Acute/chronic
metabolic
acidosis,
including
DKA
(incr
LA
risk)
-‐
IV
iodinated
contrast
media
in
radiologic
studies
(should
d/c
metformin
for
48h):
possible
acute
alteration
of
renal
fn
incr
LA
risk
PE
-‐
Take
w
food
to
dec
GI
upset
-‐
Swallow
ERT
whole,
x
crush,
break
or
chew
-‐
Take
at
the
same
time
each
day.
X
use
more
med
or
use
it
more
often
than
your
doc
tells
you
yo
-‐
Miss
dose:
use
it
ASAP.
If
almost
time
for
next
dose,
wait
and
skip
missed
dose.
Do
not
double.
-‐
Avoid/limit
alcohol
(incr
LA,
may
cause
hypo)
-‐
May
experience
NVD
(take
w
meals
or
eat
small
frequent
meals
may),
flatulence,
muscle
weakeness,
HA,
drowsy,
dizzy
(caution
on
driving/handling
machinery)
-‐
d/c
and
see
doc
if
exp
SOB,
slow/irregular
heartbeat,
muscle
pain,
persistent
nv
and
ab
pain.
(signs
of
LA)
5.
Glipizide
Tab
Brand
-‐
Glucotrol
XL
5mg
&
10mg
(ER),
Minidiab
5mg,
Melizide
5mg
Cat
-‐
POM,
Preg
C
(FDA,
TGA)
AI
-‐
Manage
T2DM
nd
MOA
-‐
2
gen
SU:
+
insulin
release
from
beta
cells,
dec
hepatic
glc
production,
incr
insulin
sensitivity
at
peripheral
targets
ADME
-‐
A:
rapid
&
complete
absorption,
delayed
w
food
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