DRUG PROFILE OF PIROXICAM

PRESENTED TO:Dr. Samreen Faisal

PRESENTED BY:Ahad Nawaz

Pharm-D 4th Prof

Contents• Introduction• Product Description• Chemistry of Drug• Pharmacokinetics• Clinical Pharmacology• Dosage Schedule• Precautions• Side Effects• Administration Guidelines• Drug-drug Interactions• Drug Food Interactions• Therapeutic Drug Monitoring• Toxicology• References

Introduction

• Generic Name: Piroxicam

• Drug Category: Prescribed

• National Essential Drug List: Present

• WHO Essential Drug List: Present

Product Product DescriptionDescription

FeldeneFeldene• Generic: Piroxicam

• Dosage form: Tab/Cap/Gel/Inj

• Available strength:

10- 20mg/0.5%w/w& 20mg/ml• Manufactured By: Pfizer

OricamOricam• Generic: Piroxicam

• Dosage form: Tab & Cap

• Available strength:10-20mg• Manufactured By: Axis Pharma

Diodex• Generic: Piroxicam

• Dosage form: Tab/Cap & Gel

• Available strength: 20mg/ 0.5% w/w• Manufactured by: Pearl Pharma

CHEMISTRY OF DRUGCHEMISTRY OF DRUGChemical class: Enolic acid derivativeChemical Nature: AcidicMolecular formula/weight: C15H13N3O4S / 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

EliminationHalf Life

Metabolism Active Metabolite

Route of Excretion

50h50h Metabolise in the Metabolise in the liver. The major liver. The major metabolic metabolic transformation is transformation is CYP-mediatedCYP-mediatedhydroxylation 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

Pharmacological 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 Dosage ScheduleSchedule

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

StorageStorageKeep 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 InteractionsInteracting 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 synthesiswhich 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 Drug-Food InteractionsInteractions

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

ToxicologyToxic Dose Symptoms Treatment

60-80mg for 3 days

Lethargy, Drowsiness, Nausea, vomiting,Epigastric pain.Hypotension, Acute Renal failure, Respiratorydepression 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- 9th Edition Page 823

Goodman & Gillman's Manual of Pharmacology &

therapeutics-2008 Page-453

BNF 61st Edition Page-639

Clarke's Analysis of Drugs and Poisons 3rd Edition Page-521