Name of Drug Final

NAME OF DRUG
Generic Name:
glimepiride
Brand Name:
Solosa
Classification:
Antidiabetic Agents;
Sulfonylureas;
sulfonamides
Dosage:
Adults
Usual starting dose
is 1-2 mg PO OD with
breakfast or first
meal of the day;
usual maintenance
dose is 1-4 mg PO
OD, depending on
patient response and
glucose levels. Do
not exceed an
increase of
2mg/dose at 1-2
week intervals based
on glucose levels; do
not exceed total
daily dose of 8 mg.
Combination
with the
insulin
therapy: 8mg
PO OD with
first meal of
the day with
low-dose
INDICATIONS
CONTRADICTIO
NS
As an adjunct to
diet and exercise
to lower blood
glucose in
patients with
type 2 diabetes
mellitus whose
hypoglycemia
cannot be
controlled by diet
and exercise
alone.
Contradicted with
allergy to
sulfonylureas;
diabetes
complicated with
fever, severe
infections, severe
trauma, major
surgery, ketosis,
acidosis, coma
(insulin is
indicated in these
conditions); type
1 or juvenile
diabetes, serious
hepatic or renal
impairment,
uremia, thyroid or
endocrine
impairment,
glycosuria,
hyperglycemia
associated with
primary renal
disease; labor
and delivery if
glimepiride is
used during
pregnancy,
discontinue drug
at least 1 mo
before delivery;
lactation, safety
not established.
In combination
with metformin
or insulin to
better control
glucose as an
adjunct to diet
and exercise in
patients with
type 2 diabetes
mellitus.
Use cautiously
with pregnancy.
MECHANISM OF ACTIONS
SIDE EFFECTS
NURSING
RESPONSIBILITIES
Pharmacotherapeutic
Group: Blood glucoselowering drugs, excluding
insulins; sulfonamides, urea
derivatives.
CNS: Drowsiness,
asthenia,
nervousness, tremor,
insomnia, blurred
vision
Pharmacodynamics:
Glimepiride is an orally active
hypoglycemic substance
belonging to the sulfonylurea
group. It may be used in noninsulin dependent diabetes
mellitus.
Glimepiride acts mainly by
stimulating insulin release
from pancreatic -cells. As
with other sulfonylureas this
effect is based on an increase
of responsiveness of the
pancreatic -cells to the
physiological glucose
stimulus. In addition,
glimepiride seems to have
pronounced extra pancreatic
effects also postulated for
other sulfonylureas.
Sulfonylureas regulate insulin
secretion by closing the ATP
sensitive potassium channel
in the -cell membrane.
Closing the potassium
channel induces
depolarization of the -cell
and results by opening of
calcium channels in an
increased influx of calcium
into the cell. This leads to
insulin release through
exocytosis.
Glimepiride binds with a high
CV: Increased risk

of CV mortality
(possible)
Assessment of
Hx: Allergy to
sulfonylureas;
diabetes complicated
with fever, severe
infections, severe
trauma, major
surgery, ketosis,
acidosis, coma
(insulin is indicated
in these conditions);
type 1 or juvenile
diabetes, serious
hepatic or renal
impairment, uremia,
thyroid or endocrine
impairment,
glycosuria,
hyperglycemia
associated with
primary renal
disease; pregnancy
Endocrine:
Hypoglycemia,
SIADH
GI: Anorexia,
nausea, vomiting,
epigastric
discomfort,
heartburn, diarrhea
Hematologic:
Leukopenia,
thrombocytopenia,
anemia
Hypersensitivity:
Allergic skin
reactions, eczema,
pruritus, erythema,
urticaria,
photosensitivity,
fever, eosinophilia,
jaundice
Others: Diuresis,
tinnitus, fatigue,
weight gain,
hyponatremia
Physical: Skin color,

lesions; T;
orientation, reflexes,
peripheral sensation;
R, adventitious
sounds; liver
evaluation, bowel
sounds; urinalysis,
BUN, serum
creatinine, LFTs,
blood glucose, CBC
Interventions
WARNING. Transfer
to insulin therapy
during periods of
insulin
Transfer from
other
hypoglycemic
: No transition
period is
necessary.
Pediatric patients
Safety and efficacy
not established
Patients with renal
or hepatic
impairment; elderly,
debilitated,
malnourished
patients; patients
with adrenal or
pituitary
insufficiency
Usual starting dose
is 1 mg PO OD;
adjust dose carefully,
lower maintenance
doses may be
sufficient to control
blood sugar
Route: Oral
exchange rate to a -cell

membrane protein which is
associated with the ATP
sensitive potassium channel
but which is different from the
usual sulfonylurea binding
site.
The extra pancreatic effects
are for example an
improvement of the
sensitivity of the peripheral
tissue for insulin and a
decrease of the insulin uptake
by the liver. The uptake of
glucose from blood into
peripheral muscle and fat
tissues occurs via special
transport proteins, located in
the cells membrane. The
transport of glucose in these
tissues is the rate-limiting
step in the use of glucose.
Glimepiride increases very
rapidly the number of active
glucose transport molecules
in the plasma membranes of
muscle and fat cells, resulting
in stimulated glucose uptake.
Glimepiride increases the
activity of the glycosyl
phosphatidylinositol specific
phospholipase C which may
be correlated with the druginduced lipogenesis and
glycogenesis in isolated fat
and muscle cells.
Glimepiride inhibits the
glucose production in the liver
by increasing the intracellular
concentration of fructose 2,6
bisphosphate, which in its
turn inhibits the
gluconeogenesis.
high stress (eg,

infections, surgery,
and trauma).
Monitor
serum
glucose levels
frequently to
determine
effectiveness
of drug and
dosage being
used
Use IV
glucose if
severe
hypoglycemia
occur as a
result of
overdose
Arrange for
consultation
with dietitian
to establish
weight-loss
program and
dietary
control
Arrange for
thorough
diabetic
teaching
program,
including
disease,
dietary
control ,
exercise,
signs and
symptoms of
hypoglycemia
In healthy persons, the

minimum effective oral dose
is approximately 0.6-mg. The
effect of glimepiride is dose
dependent and reproducible.
The physiological response to
acute physical exercise,
reduction of insulin secretion,
is still present under
glimepiride.
There was no significant
difference in effect regardless
of whether the medicinal
product was given 30 min or
immediately before a meal. In
diabetic patients, good
metabolic control over 24 hrs
can be achieved with a single
daily dose.
Although the hydroxy
metabolite of glimepiride
caused a small but significant
decrease in serum glucose in
healthy persons, it accounts
for only a minor part of the
total drug effect. Improved
metabolic control for
concomitant glimepiride
therapy compared to
metformin alone in patients
not adequately controlled with
the maximum dose of
metformin has been shown in
1 study.
Data for combination therapy
with insulin are limited. In
patients not adequately
controlled with the maximum
dose of glimepiride,
concomitant insulin therapy
can be initiated. In 2 studies,
the combination achieved the
same improvement in
and
hyperglycemi
a, avoidance
of infection,
hygiene
Consider
adding
metformin to
drug regimen
if response is
not adequate;
monitor
patient
closely
Teaching points
Take this drug
OD with
breakfast or
the first main
meal of the
day
Do not
discontinue
this drug
without
consulting
your
healthcare
provider
Continue with
diet and
exercise
program for
diabetes
control
Monitor blood
for glucose as
prescribed
Do not use
this drug if
metabolic control as insulin

alone; however, a lower
average dose of insulin was
required in combination
therapy.
Special Populations: Pediatric
Population: An active
controlled clinical trial
(glimepiride up to 8 mg daily
or metformin up to 2,000 mg
daily) of 24 weeks duration
was performed in 285 children
(8-17 years) with type 2
diabetes.
Both glimepiride and
metformin exhibited a
significant decrease from
baseline in HbA1c [glimepiride
0.95 (se 0.41); metformin
1.39 (se 0.4)]. However,
glimepiride did not achieve
the criteria of non-inferiority
to metformin in mean change
from baseline of HbA1c. The
difference between
treatments was 0.44% in
favour of metformin. The
upper limit (1.05) of the 95%
confidence interval for the
difference was not below the
0.3% noninferiority margin.
Following glimepiride
treatment, there were no new
safety concerns noted in
children compared to adult
patients with type 2 diabetes
mellitus. No long-term
efficacy and safety data are
available in pediatric patients.
Pharmacokinetics: The
bioavailability of glimepiride
after oral administration is
you are
pregnant
Avoid alcohol
while taking
this drug
Report fever,
sore throat,
unusual
bleeding or
bruising, rash,
dark urine,
light colored
stools,
hypoglycemic
or
hyperglycemi
c reactions
complete. Food intake has no

relevant influence on
absorption, only absorption
rate is slightly diminished.
Maximum serum
concentrations (Cmax) are
reached approximately 2.5
hrs after oral intake (mean 0.3
mcg/mL during multiple
dosing of 4 mg daily) and
there is a linear relationship
between dose and both Cmax
and area under the
concentration-time curve
(AUC).
Glimepiride has a very low
volume of distribution
(approximately 8.8 L) which is
roughly equal to the albumin
distribution space, high
protein-binding (>99%) and a
low clearance (approximately
48 mL/min). In animals,
glimepiride is excreted in
milk. Glimepiride is
transferred to the placenta.
Passage of the blood brain
barrier is low.
Mean dominant serum half-life
(t), which is of relevance for
the serum concentrations
under multiple-dose
conditions, is about 5-8 hrs.
After high doses, slightly
longer t were noted.
After a single dose of
radiolabelled glimepiride, 58%
of the radioactivity was
recovered in the urine and
35% in the feces. No
unchanged substance was
detected in the urine. Two (2)
metabolites most probably
resulting from hepatic

metabolism (major enzyme is
CYP2C9) were identified both
in urine and feces: Hydroxy
and carboxy derivatives. After
oral administration of
glimepiride, the terminal t
of these metabolites were 3-6
and 5-6 hrs respectively.
Comparison of single and
multiple once-daily dosing
revealed no significant
differences in
pharmacokinetics and the
intraindividual variability was
very low. There was no
relevant accumulation.
Special Populations:
Pharmacokinetics were similar
in males and females, as well
as in young and elderly (>65
years) patients. In patients
with low creatinine clearance,
there was a tendency for
glimepiride clearance to
increase and for average
serum concentrations to
decrease, most probably
resulting from a more rapid
elimination because of lower
protein-binding. Renal
elimination of the 2
metabolites was impaired.
Overall, no additional risk of
accumulation is to be
assumed in such patients.
Pharmacokinetics in 5 nondiabetic patients after bile
duct surgery were similar to
those in healthy persons.
Pediatric Population: A fed
study investigating the
pharmacokinetics, safety and
tolerability of a glimepiride 1
mg single dose in 30 pediatric
patients (4 children 10-12
years and 26 children 12-17
years) with type 2 diabetes
showed mean AUC(0-last),
Cmax and t similar to that
previously observed in adults.
Toxicology: Preclinical Safety

Data: Preclinical effects
observed occurred at
exposures sufficiently in
excess of the maximum
human exposure as to
indicate little relevance to
clinical use or were due to the
pharmacodynamic action
(hypoglycemia) of the
compound. This finding is
based on conventional safety
pharmacology, repeated-dose
toxicity, genotoxicity,
carcinogenicity and
reproduction toxicity studies.
In the latter (covering
embryotoxicity, teratogenicity
and developmental toxicity),
adverse effects observed
were considered to be
secondary to the
hypoglycemic effects induced
by the compound in dams and
in offspring.
SOURCES:
o
o
Karch, Amy M., 2015. Lippincott Nursing Drug Guide. Wolters Kluwer.
http://www.mims.com/Philippines/drug/info/Solosa/Solosa?type=full

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NAME OF DRUG

CV: Increased risk

Physical: Skin color,

exchange rate to a -cell

high stress (eg,

In healthy persons, the

metabolic control as insulin

complete. Food intake has no

resulting from hepatic

Toxicology: Preclinical Safety

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