SUMMARY Betamethasone is a systemic

corticosteroid used to relieve

inflammation in various conditions,
including but not limited to allergic
states, dermatologic disorders,
gastrointestinal diseases, and
hematological disorders
BACKGROUND Betamethasone is a long-
acting corticosteroid with
immunosuppressive and
antiinflammatory
properties.11 It can be used
topically to manage
inflammatory skin conditions
such as eczema, and
parenterally to manage
several disease states
including autoimmune
disorders.11 Betamethasone
has potent glucocorticoid
activity and negligible
mineralocorticoid activity.11

STRUKTUR KIMIA

Formula
C22H29FO5

PHARMACOLOGY
As a member of the corticosteroid
INDICATION family, betamethasone is indicated
for the treatment of several
inflammatory conditions. As topical
monotherapy, betamethasone is
indicated to relieve pruritic and
 inflammatory symptoms of
corticosteroid-responsive-
dermatoses.12,14,15 Betamethasone can
be used topically in combination with
a vitamin D analog such as
calcipotriene to treat plaque
psoriasis.16 The corticosteroid is also
available as an injectable suspension
and can be used to manage a range
of inflammatory conditions including
endocrine disorders, gastrointestinal
disorders, and rheumatic disorders
among other conditions.
CONTRAINDICATION
Toxicity Chronic high doses of
glucocorticoids can lead to
the development of
cataracts, glaucoma,
hypertension, water
retention, hyperlipidemia,
peptic ulcer, pancreatitis,
myopathy, osteoporosis,
mood changes, psychosis,
dermal atrophy, allergy,
acne, hypertrichosis,
immune suppression,
decreased resistance to
infection, moon face,
hyperglycemia,
hypocalcemia,
hypophosphatemia,
metabolic acidosis, growth
suppression, and secondary
adrenal
insufficiency.6 Overdose
may be treated by adjusting
the dose or stopping the
corticosteroid as well as
initiating symptomatic and
supportive treatment.6
Pharmacodynamics Corticosteroids bind to the
glucocorticoid receptor
inhibiting pro-inflammatory
signals, while promoting
anti-inflammatory
signals.1 Corticosteroids
have a wide therapeutic
window as patients may
require doses that are
multiples of what the body
naturally
produces.1 Patients who
require long-term treatment
with a corticosteroid should
be counselled regarding the
risk of hypothalamic-
pituitary-adrenal axis
suppression and increased
susceptibility to infections.1

Pharmacokinetics
Mechanism of action Glucocorticoids inhibit
neutrophil apoptosis and
demargination, and inhibit
NF-Kappa B and other
TARGET ACTIONS ORGANISM
agonist
inflammatory transcription
AGlucocorticoid Humans
factors.1 They also inhibit
receptor
phospholipase A2, leading to
decreased formation of
arachidonic acid
derivatives.1 In addition,
glucocorticoids promote
anti-inflammatory genes like
interleukin-10.1

Corticosteroids like
betamethasone can act through
nongenomic and genomic
pathways.3 The genomic pathway
is slower and occurs when
 glucocorticoids activate
glucocorticoid receptors and
initiate downstream effects that
promote transcription of anti-
inflammatory genes including
phosphoenolpyruvate
carboxykinase (PEPCK), IL-1-
receptor antagonist, and tyrosine
amino transferase (TAT).3 On the
other hand, the nongenomic
pathway is able to elicit a quicker
response by modulating T-cell,
platelet and monocyte activity
through the use of existing
membrane-bound receptors and
second messengers.3
ABSORPTION The absorption and potency of
any topical corticosteroid
including betamethasone depends
on the vehicle in which the
steroid is delivered. For example,
betamethasone dipropionate
0.05% ointment is classified as a
highly potent topical steroid,
while betamethasone
dipropionate 0.05% cream or
lotion is considered to be
moderately potent.4
There are several structural
modifications that can determine
the potency of a topical
corticosteroid. For example,
corticosteroids containing a
halogen at specific carbons, or
that contain esters are more
potent due to enhanced
lipophilicity.5 As such, there is a
marked difference between
topical products containing
betamethasone dipropionate vs.
 betamethasone valerate.
Betamethasone dipropionate
contains 2 esters which enhances
its potency, while betamethasone
valerate has only one ester and is
less potent.5
It should be noted that the use of
occlusive dressings with topical
steroids significantly increases
the absorption, increasing the risk
for adverse effects.14

Volume of distribution In a study that included

Indian women of
reproductive age, the
volume of distribution
following a single
intramuscular dose of
betamethasone phosphate
was 94,584±23,539 mL(s).9

Protein binding Betamethasone valerate

binds to serum albumin and
corticosteroid-binding
globulin

Metabolism The metabolism of

betamethasone yields 6
metabolites.10 The metabolic
processes include 6β
hydroxylation, 11β-hydroxyl
oxidation, and reduction of
the C-20 carbonyl group
followed by removal of the
side chain.10

Route of elimination Corticosteroids are

eliminated predominantly in
the urine.2