Diodex
•Generic: Piroxicam
•Dosage form: Tab/Cap & Gel
•Available strength: 20mg/ 0.5% w/w
•Manufactured by: Pearl Pharma
CHEMISTRY OF DRUGCHEMISTRY OF DRUG
Chemical class:
Enolic acid derivative
Chemical Nature:
Acidic
Molecular formula/weight:
C
15
H
13
N
3
O
4
S / 331.35
Physical Properties:
Off-white to yellow crystalline powder
Melting Point is198° to 200°c
Pharmacokinetics
AbsorptionAbsorption
Piroxicam is absorbed completely
after oral administration and
undergoes enterohepatic
circulation.
Peak concentrations in plasma
occur within 3-5hours
Distribution
•Bioavailability:Bioavailability:
65-90% 65-90%
•Protein Binding:Protein Binding:
99%99%
•Blood Brain Barrier:Blood Brain Barrier:
Not cross the BBBNot cross the BBB
•Secreted in Milk:Secreted in Milk:
YesYes
•Volume of Distribution:Volume of Distribution:
0.14L/kg0.14L/kg
Elimination
Half
Life
Metabolism Active
Metabolite
Route of
Excretion
50h50hMetabolise in the Metabolise in the
liver. The major liver. The major
metabolic metabolic
transformation is transformation is
CYP-mediatedCYP-mediated
hydroxylation to hydroxylation to
an inactive an inactive
metabolite and metabolite and
its glucuronide its glucuronide
conjugateconjugate..
YesYes Excreted Excreted
through through
Urine and Urine and
FecesFeces
Clinical Clinical
PharmacologyPharmacology
Pharmacologic
al Class
NSAIDs
Therapeutic
Class
Analgesic, Anti-inflammatory,
Antipyretic
MOA It inhibits cyclooxygenase and
blocked the synthesis of
prostaglandins.
Contra-
indications
Inflammatory bowel disease ,
Pregnancy, Hypersensitivity to
drug
FDA Pregnancy
Class
Pregnancy Category D
Dosage ScheduleDosage Schedule
Rheumatoid Arthritis
•Route of Administration:
Oral / ParenteralOral / Parenteral
•Recommended Dose:
20mg Once daily20mg Once daily
•Duration of Therapy:
7 to 12 Days7 to 12 Days
Osteoarthritis
•Route of Administration:
Oral / ParenteralOral / Parenteral
•Recommended Dose:
20mg Once daily20mg Once daily
•Duration of Therapy:
7 to 12 Days7 to 12 Days
Ankylosing Spondylitis
•Route of Administration:
Oral / ParenteralOral / Parenteral
•Recommended Dose:
20mg Once daily20mg Once daily
•Duration of Therapy:
7 to 12 Days7 to 12 Days
Juvenile Rheumatoid
Arthritis
•Route of Administration:
Oral / ParenteralOral / Parenteral
•Recommended Dose:
5-15mg5-15mg Once daily according Once daily according
to body weight of the childto body weight of the child
•Duration of Therapy:
5 to 8 Days5 to 8 Days
Side Effects
GI disturbances including
Discomfort, Nausea, Diarrhoea,
Heartburn, bleeding& Ulceration.
Rash, Dizziness, Tinnitus
Hepatic damage
Alveolitis, Pulmonary eosinophilia, Apnea
Dyspepsia, Increase bleeding time
StorageStorage
Keep medicine out of the reach of
children.
Store in a dry place,
Protect from sunlight and
moisture
Store below 30°C
PrecautionsPrecautions
•Piroxicam should be used with caution
in patients with coagulation defects &
•Patients on anticoagulant therapy.
•Discontinue drug if skin reaction
occurs.
Administration
Guidelines
•Give with milk, antacids, or food to
minimize GI upset.
Drug-Drug InteractionsDrug-Drug Interactions
Interacting
Drug
Mechanism Outcome
Methorexate
Piroxicam have been
competitively inhibit
methotrexate
accumulation in kidney
slices.
Eenhance the
toxicity of
methotrexate
Diuretics
(Thiazide &
Furosemide )
Also Inhibits the renal
prostaglandin synthesis
which is responsible for
netriuretic effect.
Reduce the
netriuretic effect of
diuretics
Warfarin
It also inhibit the
platelets aggregation .
Increase bleeding
time
ACE
inhibitors
Its have the maximum
protein binding then ace
inhibitors
Reduce the
antihypertensive
effect ace
inhibitors
Drug-Food InteractionsDrug-Food Interactions
Piroxicam have not shown any
food interaction.
Therapeutic Drug Monitoring
•NSAIDs have the wide therapeutic
index so due to this reason they don’t
require therapeutic drug monitoring
Toxicology
Toxic Dose Symptoms Treatment
60-80mg for 3
days
Lethargy,
Drowsiness,
Nausea,
vomiting,
Epigastric pain.
Hypotension,
Acute Renal
failure,
Respiratory
depression and
Coma may
occur
No specific
antidotes
Emesis or
activated
charcoal or
osmotic
cathartic may
be used to
overcome the
toxicity
REFERENCESREFERENCES
Basic & Clinical Pharmacology_
Bertram_G._Katzung- 9
th
Edition Page 823
Goodman & Gillman's Manual of
Pharmacology &
therapeutics-2008 Page-453
BNF 61
st
Edition Page-639
Clarke's Analysis of Drugs and Poisons 3
rd