Académique Documents
Professionnel Documents
Culture Documents
GENERIC
NAME AND
BRAND
NAME
CLASSIFICATIO
N
MECHANISM OF ACTION
ADVERSE EFFECT
Tramadol
(Ultram,
Ultram ER,
Rybix ODT,
ConZip)
Analgesics
(Opioid) /
Supportive
Care Therapy
Tramadol HCl is a
cyclohexanol derivative
with central analgesic
and antitussive
activities. Tramadol
(and its active M1
metabolite) acts as an
opiate agonist,
apparently by selective
activity at the mcreceptor. In addition to
opiate agonist activity,
tramadol inhibits
reuptake of certain
monoamine
(norepinephrine,
serotonin) which
appears to contribute to
its analgesic effect.
Unlike morphine,
tramadol has no
respiratory depressant
effect over a wide range
of analgesic doses. It
also does not affect
gastrointestinal motility.
Its effects on the
cardiovascular system
are relatively slight.
Nausea, vomiting,
diarrhea,
constipation.
Tiredness,
drowsiness,
dizziness,
headache,
confusion,
hallucinations. Skin
rashes, tachycardia,
orthostatic
hypotension,
bradycardia,
flushing, allergic
reactions.
GI ulceration,
bleeding &
perforation, post-op
bleeding, acute
renal failure, liver
failure,
anaphylactic &
anaphylactoid
reactions.
Ketorolac
(Toradol)
Nonsteroidal
Antiinflammatory
Drugs
(NSAIDs)
Meperidine
(Pethidine,
Demerol)
FENTANYL
(Sublimaze
)
Synthetic
opioids, Opioid
Analgesics
Agitation, angina,
bradycardia, cariac
arrest, coma.
Constipation,
dizziness, dry
mouth
Analgesics
(Opioid)
Oral
Breakthrough cancer
pain
Adult: For patients who
are already receiving and
tolerant to opioid
treatment: As a loz:
Initially, 200 mcg over 15
minutes for an episode of
breakthrough pain; may
repeat once after 15
minutes if needed. Titrate
subsequent doses based
on response up to 1.6 mg
per dose. Once the
effective dose has been
identified, no more than 4
unit doses should be
taken daily.
Elderly: and debilitated
patients: Dose reduction
may be needed.
Intravenous
Adjunct to general
anaesthesia
Adult: For patients with
spontaneous respiration:
Initially, 50-200 mcg
followed by supplements
of 50 mcg. To be injected
over 3-5 minutes.
Possible increased risk of
resp depression following
doses >200 mcg. For
patients with assisted
ventilation: Initially, 3003,500 mcg (up to 50
mcg/kg) followed by
supplements of 100-200
mcg depending on the
patient's response. To be
injected over 3-5
minutes.
Child: For patients with
spontaneous respiration:
>2 yr: 3-5 mcg/kg IV,
supplements of 1 mcg/kg
Fentanyl is a potent
opioid analgesic that
increases pain
threshold, alters pain
reception and inhibits
ascending pain
pathways by binding to
stereospecific receptors
within the CNS.
Onset: Rapid.
Duration: Short.
Distribution: Rapidly
into tissues; appears in
the CSF, crosses the
placenta and small
amounts enter the
breast milk. Proteinbinding: 80%
Metabolism: Hepatic
via N-dealkylation and
hydroxylation.
Excretion: Urine (as
metabolites and
unchanged drug); 4 hrs
(elimination half-life).
Nausea, vomiting;
bradycardia,
oedema, CNS
depression,
confusion,
dizziness,drowsines
s, headache,
sedation, transient
hypotension,
peripheral
vasodilation;
increased
intracranial
pressure. High IV
dose may cause
chest wall rigidity.
Transdermal: Rash,
erythema and
itching.
Potentially
Fatal: Respiratory
depression, trunk
rigidity,
laryngospasm,
bronchoconstriction
.
before induction
of anaesthesia.
Elderly: and debilitated
patients: Dose reduction
may be needed.
Incompatibility: Thiope
ntal sodium and
methohexital sodium.
NALBUPHINE
(Nubaine)
Adult 0.15-0.2
mg/kg body wt.
Childn 0.1-0.2
mg/kg up to a total
single dose of 10
mg SC, IM or IV.
May be repeated 36 hrly as needed.
* Relief of
moderate to severe
pain. Pre-op
analgesia, as a
supplement to
balanced anesth,
surgical anesth, for
obstet analgesia
during labor &
relief of pain
following MI. Postop somatic &
visceral pain.
HYDROMORPHON
E (Dilaudid,
Dilaudid-HP,
Exalgo)
Analgesi
cs
(Opioid)
Oral
Analgesia
Adult: Opioid naive
patients: 2-4 mg every 4-6
hr. Higher doses may be
required in patients
previously exposed to
opioids. Usual dose range:
2-8 mg every 3-4 hr.
Hepatic
impairment: Dose
adjustments may be
needed.
Oral
Cough suppressant
Adult: 1 mg every 3-4 hr.
a phenanthrene
derivative opioid
analgesic with
mixed opioid
agonist and
antagonist activity.
inhibits the
ascending pain
pathways,
altering the
perception of
and response
to pain by
binding to
opiate
receptors in
the CNS.
produces
generalised
CNS
depression.
Hydromorphone is a
semisynthetic
phenanthrenederivative opiate
agonist. It is a strong
analgesic used to
manage moderate to
severe pain. It also
has an antitussive
activity which is
useful in the control
of persistent and nonproductive cough.
Onset: 15-30
minutes.
Duration: 4-5 hr.
Sedation, dizziness,
vertigo, miosis,
headache; nausea,
vomiting, dry
mouth; itching,
burning, urticaria.
Respiratory
depression,
dyspnoea, asthma;
speech difficulty,
urinary urgency,
blurred vision,
flushing, warmth;
clamminess.
Potentially Fatal:
Anaphylactic or
anaphylactoid and
other serious
hypersensitivity
reactions e.g.
shock, respiratory
distress,
respiratory arrest,
bradycardia,
cardiac arrest,
hypotension,
laryngeal oedema.
GI disturbances.
Difficulty with
micturition, ureteric
or biliary spasm,
antimuscarinic
effects, CV effects,
hypothermia,
hallucinations,
dysphoria, mood
changes,
dependence, miosis,
decreased libido or
potency,
hypersensitivity
reactions.
Respiratory
MORPHINE (MS
Contin, Avinza,
Depodur,
Duramorph,
Infumorph,Astram
orph, Kadian)
Analgesics
(Opioid)
Oral
Pain relief
Adult: Initially, 5-20 mg
every 4 hr (or equivalent
for modified release
formulations). Start with
low dose and adjust
according to response.
Elderly: Dosage may
need to be reduced.
Renal
impairment: Dosage
may need to be reduced.
Hepatic
impairment: Dosage
may need to be reduced.
Oral
Intractable cough asso
ciated with lung cancer
Adult: Initially, 5 mg oral
solution given every 4 hr.
Adjust according to
response.
Intravenous
Pain associated with
myocardial infarction
Adult: 10 mg at a rate of
Absorption: Oral
admin: Rapidly but
incompletely
absorbed from the GI
tract. Plasma levels
peak within 30-60
minutes. Oral
bioavailability: About
50&; undergoes
extensive 1st pass
metabolism.
Distribution: Protein
binding: 8-19%.
Widely distributed in
the tissues and
crosses the placenta.
Metabolism: Extensi
vely metabolised by
glucuronidation
hepatically.
Excretion: Plasma
elimination half-life:
About 2.5 hr after oral
or IV doses. Excreted
in the urine mainly as
conjugated
hydromorphone,
dihydromorphine,
dihydroisomorphine.
Morphine is a
phenanthrene
derivative which acts
mainly on the CNS
and smooth muscles.
It binds to opiate
receptors in the CNS
altering pain
perception and
response. Analgesia,
euphoria and
dependence are
thought to be due to
its action at the mu1 receptors while
respiratory
depression and
inhibition of
intestinal
movements are due
to action at the mu-2
receptors. Spinal
analgesia is
mediated by
morphine agonist
action at the K
receptor. Cough is
depression and
hypotension may
occur with larger
doses.
Convulsions;
nausea, vomiting,
dry mouth,
constipation; urinary
retention; headache,
vertigo; palpitations;
hypothermia;
pruritus, urticaria;
tachycardia,
bradycardia; blurred
vision; miosis;
dependency;
drowsiness;
lightheadedness;
dizziness; sweating;
dysphoria; euphoria.
Potentially
Fatal: Respiratory
depression;
circulatory failure;
hypotension;
deepening coma;
anaphylactic
reactions.
2 mg/minute followed by
a further dose of 5-10 mg
if necessary.
Elderly: 5 mg at a rate of
2 mg/min followed by a
further dose of 2.5-5 mg if
necessary.
Renal
impairment: Dosage
may need to be reduced.
Hepatic
impairment: Dosage
may need to be reduced.
Intravenous
Acute pulmonary
oedema
Adult: 5-10 mg via slow
inj at a rate of 2
mg/minute.
Elderly: Dosage may
need to be reduced.
Renal
impairment: Dosage
may need to be reduced.
Hepatic
impairment: Dosage
may need to be reduced.
Parenteral
Acute pain
Adult: IM or SC admin::
10 mg every 4 hr (or more
frequently during
titration); adjust according
to response. IV admin:
Initially, 2.5 mg every 4 hr
(or more frequently during
titration), adjust according
to response
Child: By IM or SC inj: <1
mth: 150 mcg/kg 6 hrly;
1-12 mth: 200 mcg/kg 6
hrly; 1-5 yr: 2.5-5 mg 4
hrly; 5-12 yr: 5-10 mg 4
hrly. Repeat doses should
only be given when
necessary. Adjust
according to response.
Elderly: Dosage may
need to be reduced.
Renal
impairment: Dosage
may need to be reduced.
Hepatic
impairment: Dosage
may need to be reduced.
Intraspinal
Moderate to severe
suppressed by direct
action on cough
centre.
Onset: 1 hr (oral);
5-10 minutes (IV);
20-60 minutes
(rectal); 50-90
minutes (SC); 30-60
minutes (IM).
Duration: 4 hr.
Absorption: Variabl
y absorbed from the
GI tract (oral);
readily absorbed into
blood (IM/SC).
Distribution: Kidne
ys, liver, lungs,
spleen, brain and
muscles (low
concentrations);
crosses the bloodbrain barrier and
placenta; enters
breast milk. Proteinbinding: 20-35%.
Metabolism: Hepati
c and gut by
glucuronidation;
extensive first-pass
metabolism.
Excretion: Faeces,
urine (as metabolites
and unchanged
drug) Elimination
half-life of around 2
hr but varies
between individuals.
pain
Adult: Initially, 5 mg
epidural inj; after 1 hr,
additional doses of 1-2 mg
may be given if pain relief
is unsatisfactory up to a
total dose of 10 mg/24 hr.
Alternatively, 2-4 mg/24
hr continuous infusion,
increased by further 1-2
mg increments if
necessary.
Elderly: Dosage may
need to be reduced.
Renal
impairment: Dosage
may need to be reduced.
Hepatic
impairment: Dosage
may need to be reduced.
Intrathecal
Moderate to severe
pain
Adult: 0.2-1 mg, to be
injected on a single
occasion.
Parenteral
Premedication in
surgery
Adult: IM/SC inj: Up to 10
mg 60-90 minutes before
operation.
Child: IM inj: 150 mcg/kg
before operation.
Elderly: Lower dose may
be required.
Renal
impairment: Dosage
may need to be reduced.
Hepatic
impairment: Dosage
may need to be reduced.
Intravenous
Unstable angina not
responsive to antiischaemic therapy
Adult: 2-5 mg repeated
every 5-30 minutes as
needed for symptom
relief.
Parenteral
Analgesia during
labour
Adult: 10 mg by IM or SC
inj.
Rectal
Chronic pain
Nonsteroid
al AntiInflammat
ory Drugs
(NSAIDs) /
Ophthalmi
c
Decongest
ants,
Anesthetic
s, AntiInflammat
ories
Diclofenac has
potent antiinflammatory,
analgesic and
antipyretic actions. It
inhibits the enzyme,
cyclooxygenase,
thus resulting in
reduced synthesis of
prostaglandin
precursors.
Absorption: Rapidly
absorbed (oral
solution, rectal
suppository, IM);
more slowly (entericcoated tab).
Distribution: Penet
rates synovial fluid;
enters breast milk
(small amounts).
Protein-binding:
>99%.
Metabolism: Exten
sively hepatic;
converted to
metabolites.
Excretion: About
60% excreted in
urine as glucuronide
and sulfate
conjugates; 35% in
bile; 1-2 hr
(elimination halflife).
GI disturbances;
headache, dizziness,
rash; GI bleeding,
peptic ulceration;
abnormalities of
kidney function. Pain
and tissue damage
at Inj site (IM); local
irritation (rectal);
transient burning
and stinging
(ophthalmic).
Potentially
Fatal: StevensJohnson syndrome,
exfoliative
dermatitis, toxic
epidermal
necrolysis.
up to 4 times/day.Pain
and discomfort after
radial keratectomy As
0.1% soln: As Na: Instill 1
drop before surgery
followed by 1 drop
immediately after surgery,
then 1 drop 4 times/day
up to 2
days. Inflammation
after argon laser
trabeculoplasty As 0.1%
soln: As Na: Instill 1 drop
4 times/day during the 2
hr before procedure
followed by 1 drop 4
times/day up to 7 days
after
procedure. Inflammation
and discomfort after
strabismus surgery As
0.1% soln: As Na: Instill 1
drop 4 times/day for the
1st wk, 3 times/day for
2nd wk, twice daily for 3rd
wk and as needed for 4th
wk. Pain after
accidental traumaAs
0.1% soln: As Na: Instill 1
drop 4 times/day up to 2
days. Topical Local relief
of pain and
inflammation As 1% gel:
As Na: Apply 3-4
times/day. Osteoarthritis
As 1.6% soln: As Na:
Apply 4 times/day. Actinic
keratosis As 3% gel: As
Na: Apply twice daily for
60-90 days.
Click to view diclofenac
Dosage by Indications
ACETYLSALICYLIC
ACID (ASPIRIN)
NSAIDS
Adult: PO Prophylaxis
of MI 75-325
mg/day. Stent
implantation 325 mg 2
hr pre-op, then 160-325
mg/day. Pain and fever
325-650 mg 4-6 hrly. Max:
4 g/day. Pain and
inflammation
associated w/
musculoskeletal and
joint disorders Initial:
2.4-3.6 g/day.
Maintenance: 3.6-5.4
Aspirin is an
analgesic, antiinflammatory and
antipyretic. It inhibits
cyclooxygenase,
which is responsible
for the synthesis of
prostaglandin and
thromboxane. It also
inhibits platelet
aggregation.
Duration: 4-6 hr.
Absorption: Rapidly
absorbed from the GI
GI disturbances;
prolonged bleeding
time, rhinitis,
urticaria and
epigastric
discomfort;
angioedema,
salicylism, tinnitus;
bronchospasm.
Potentially
Fatal: Gastric
erosion, ulceration
and bleeding;
severe, occasionally
MELOXICAM
(BERAMEX)
CELECOXIB
(Celebrex)
NSAIDS
g/day.
fatal exacerbation of
airway obstruction in
asthma; Reye's
syndrome (children
<12 yr).
Hepatotoxicity; CNS
depression which
may lead to coma;
CV collapse and resp
failure; paroxysmal
bronchospasm and
dyspnoea.
Meloxicam inhibits
prostaglandin
synthesis by
reducing
cyclooxygenase
enzyme activity. This
results in decreased
production of
prostaglandin
precursors.
Absorption: Well
absorbed from the GI
tract (oral).
Distribution: Protei
n-binding: 99%.
Metabolism: Exten
sively hepatic via
oxidation pathway.
Excretion: Via urine
and faeces (as
inactive
metabolites); 20 hr
(elimination halflife).
Dyspepsia,
headache, nausea,
diarrhoea, upper
respiratory tract
infection, abdominal
pain, dizziness,
oedema, flatulence,
influenza-like
symptoms, back
pain, muscle
spasms,
musculoskeletal
pain, rash, anaemia.
GI perforation,
ulceration and/or
bleeding. In children:
Abdominal pain,
vomiting, diarrhoea,
headache, pyrexia.
Potentially
Fatal: Stevens
Johnson syndrome,
thrombocytopenia,
interstitial nephritis
and idiosyncratic
liver abnormality.
Adult: PO Osteoarthritis
200 mg 1-2 times/day.
Abdominal pain,
diarrhea, nausea,
Nonsteroid
al AntiInflammat
ory Drugs
(NSAIDs)
Parenteral
Postoperative pain
Adult: 40 mg slow IM or
IV inj, then 20 or 40 mg
every 6-12 hr as required.
Max dose: 80 mg/day.
Child: <18 yr: Not
recommended.
Elderly: <50 kg: 20 mg
slow IV or IM inj, repeat to
a max of 40 mg/day.
Hepatic
impairment: Mild
impairment (Child-Pugh
score 5-6): No dosage
adjustment. Moderate
impairment (Child-Pugh
score 7-9): Half the usual
dose, repeat to a max of
40 mg/day. Severe
impairment (Child-Pugh
score >9): Not
recommended.
Reconstitution: Reconsti
tute with sodium chloride
0.9%, glucose 5%, or
sodium chloride 0.45%
with glucose 5%.
activity. It inhibits
the conversion of
arachidonic acid to
prostaglandins while
having no effect on
the formation of
prostaglandins that
mediate the normal
homeostasis in the
GI tract, kidneys and
platelets catalysed
by COX-1.
oedema, dizziness,
headache, insomnia,
upper respiratory
tract infections;
rash.
Potentially Fatal:
Serious skin
reactions such as
exfoliative
dermatitis, StevensJohnson syndrome,
and toxic epidermal
necrolysis.
Parecoxib is the
prodrug of
valdecoxib. It has a
very high selectivity
for inhibiting cyclooxygenase-2 (COX-2)
mediated
prostaglandin
synthesis to reduce
mediators of pain
and inflammation.
The selective
inhibition of COX-2 is
coupled with
reduced GI toxicity,
but associated
increased risk for
thrombotic events
and renal
impairment have
been noted.
Distribution: Plasm
a protein binding:
approx 98%.
Metabolism: Hydrol
ysed in the liver to
its active metabolite,
valdecoxib, and
propionic acid;
plasma half-life: 22
min.
Excretion: Via
urine; approx 70% of
a dose appearing as
inactive metabolites,
<5% of a dose
appears as
unchanged
valdecoxib in the
urine. Trace amounts
of unchanged drug
in faeces.
Rash, ulcerations or
any other signs of
an allergic reaction;
GI disturbances and
bleeding;
hypotension;
hypertension; back
pain; oedema;
numbness; agitation
or sleeping
difficulties; anaemia;
sore throat or
difficulty breathing;
pruritus; decreased
urine output;
jaundice, abnormal
liver function; low
platelet count; skin
swelling, blistering
or peeling; kidney
failure; heart failure,
heart attack,
bradycardia,
arrhythmia.
Potentially
Fatal: Anaphylaxis,
Steven-Johnson
syndrome, toxic
epidermal
necrolysis.
Elimination half-life:
8 hr.
KETOPROFEN
(Nexcede)
Nonsteroid
al AntiInflammat
ory Drugs
(NSAIDs)
Oral
Rheumatic disorders
Adult: 100-200 mg/day in
2-4 divided doses. As
modified-release
formulation: Administer
dose once daily. Max: 300
mg daily in divided doses.
Elderly: >75 yr: Reduce
initial dose.
Renal impairment: Max
dose: Mild impairment:
150 mg daily; severe
impairment: 100 mg daily.
Hepatic
impairment: Max dose:
100 mg daily if serum
albumin <3.5 g/dL.
Oral
Pain and inflammation
Adult: 25-50 mg every 68 hr. Max: 300 mg daily in
divided doses.
Elderly: >75 yr: Reduce
initial dose.
Renal impairment: Max
dose: Mild impairment:
150 mg daily; severe
impairment: 100 mg daily.
Hepatic
impairment: Max dose:
100 mg daily if serum
albumin <3.5 g/dL.
Intramuscular
Pain and inflammation
associated with
musculoskeletal and
joint disorders
Adult: 50-100 mg by
deep inj into the gluteal
muscle every 4 hr. Max:
200 mg in 24 hr for up to
3 days.
Intramuscular
Pain following
orthopaedic surgery
Adult: 50-100 mg by
deep inj into the gluteal
muscle every 4 hr. Max:
200 mg in 24 hr for up to
3 days.
Topical/Cutaneous
Local pain relief
Adult: Apply 2.5% gel
Ketoprofen exhibits
anti-inflammatory,
analgesic and
antipyretic activities.
It potently inhibits
the enzyme
cyclooxygenase
resulting in
prostaglandin
synthesis inhibition.
It also prevents
formation of
thromboxane A2 by
platelet aggregation.
Absorption: Readily
absorbed from the GI
tract (oral); reduced
absorption with food.
Peak plasma
concentrations after
0.5-2 hr. Well
absorbed (IM,
rectal); minimal
(topical).
Distribution: Synov
ial fluid (substantial
concentrations).
Protein-binding:
99%.
Metabolism: Hepati
c via conjugation
with glucuronic acid.
Excretion: Urine (as
glucuronide
conjugates); 1.5-4 hr
(elimination halflife).
Acute interstitial
nephritis, reversible
decline in renal
function; GI
symptoms e.g.
discomfort, nausea,
diarrhoea; pain and
tissue damage at inj
site (IM).
Potentially
Fatal: Rarely,
idiosyncrasy,
anaphylaxis; very
rarely GI
haemorrhage.
NSAIDS
1 tab 2x a day
Naproxen sodium is
a nonsteroidal antiinflammatory drug
(NSAID) that exhibits
anti-inflammatory,
analgesic and
antipyretic activity
by inhibiting
cyclooxygenase
(COX)-1 and COX-2
isoenzymes resulting
in inhibition of
prostaglandin
synthesis.
Most frequently
reported adverse
events (frequency 110%) associated
with naproxen and
other NSAIDs
include heartburn,
abdominal pain,
nausea,
constipation,
diarrhea, dyspepsia,
stomatitis,
flatulence, gross
bleeding/perforation,
GI ulcers
(gastric/duodenal),
vomiting, headache,
dizziness,
drowsiness,
lightheadedness,
vertigo, pruritus
(itching), skin
eruptions,
ecchymoses,
sweating, purpura,
tinnitus, visual and
hearing
disturbances,
edema, palpitations,
dyspnea, thirst,
abnormal renal
function, anemia,
elevated liver
enzymes, increased
bleeding time and
rashes.