Phenylbutazone

Phenylbutazone is a congener of aminopyrine and antipyrine, having analgesic, antipyretic, antinflammatory and mild uricosuric properties; rapidly gained favour after its introduction in 1949 for the treatment of inflammatory joint disordes. Phenylbutazone is used in the treatment of gout, ankylosing spondylitis But it has a large number of serious adverse effects.


Adult Dose
Dose: 100 mg
Single Dose: 100 (100)
Frequency: 8 hourly
Route: PO
Instructions: Maintenance, As Required
Neonatal
Dose:
Single Dose:
Frequency:
Route:
Instructions: Not recommended in this age group
Paedriatic
Dose:
Single Dose:
Frequency:
Route:
Instructions: Not recommended in this age group
Characteristics
. It is of Synthetic origin and belongs to Pyrazolidine. It belongs to Cyclo-oxygenase inhibitor pharmacological group on the basis of mechanism of action and also classified in Analgesics and Anti-inflammatory Agents pharmacological group.The Molecular Weight of Phenylbutazone is 308.40. 5.34% solution of the drug is isotonic and Its pKa is 4.5.
Contraindications
Phenylbutazone is contraindicated in conditions like Peptic ulcer,Blood dyscrasias,Congestive heart failure,Hepatitis.
Effects
The severe or irreversible adverse effects of Phenylbutazone, which give rise to further complications include Hepatitis, Exfoliative dermatitis, Peptic ulceration, Goitre, Chromosomal damage, Gastric erosions.Phenylbutazone produces potentially life-threatening effects which include Pulmonary edema, Blood dyscrasias, Bleeding, Cardiac failure, Peptic ulceration, Perforation. which are responsible for the discontinuation of Phenylbutazone therapy.The signs and symptoms that are produced after the acute overdosage of Phenylbutazone include Death, Acidosis, Acute renal failure, Encephalitis, Neurological syndrome, Acute hepatitis.The symptomatic adverse reactions produced by Phenylbutazone are more or less tolerable and if they become severe, they can be treated symptomatically, these include Rashes, Stomatitis, Hematuria, Rectal bleeding, Salivary gland swelling, Increased intracranial pressure.
Indications
Phenylbutazone is primarily indicated in conditions like Acute gout, Advanced prostate cancer, Agitation and restlessness in the elderly, Ankylosing spondylitis, Nausea and vomiting (palliative care), Pain, Schizophrenia and other psychoses, and can also be given in adjunctive therapy as an alternative drug of choice in Bone pain, Gout, Osteoarthritis, Psoriatic arthritis, Reiters disease, Rheumatic fever, Rheumatoid arthritis, Thrombophlebitis.
Interactions
Phenylbutazone is known to interact with other drugs, the details of drug interactions is as follows:DrugDetailsSeverityOnsetManagementAlcoholAluminium Hydroxide and OxideAspirinCoadministration exacerbate the serious gastrointestinal toxicity. Aspirin at higher doses also decreases the plasma concentration of phenylbutazoneModerateCoadministration should be avoided due to increased risk of toxicity. Patient should take medication with food and should report the sign and symptoms of GI ulceration and bleeding to physician immediately.ChlorambucilChloroquineChlorpropamidePhenylbutazone inhibit the metabolism and renal clearence of chlorpropamide and displace it from plasma protein binding site thus potentiate the hypoglycaemic effect.ModerateMonitor blood sugar regularly. Closely monitor for increased hypoglycemic effect. Reduce the dose of chlorpropamide if necessary.CholestyramineClozapineBoth agents acts additively thus enhances the risk and severity of hematologic toxicityMajorThis combination should be avaoided due to increased risk of agranulocytosis and bone marrow suppression.Colestipol (HCl)EthinyloestradiolEtodolacFenbufenFenoprofenFloctafenineFlurbiprofenFosphenytoinGestodeneGlibornurideGliclazideGliquidoneGlymidineLiothyronine (Na)Magnesium Oxides and HydroxidesMeloxicamMethotrexateMethylphenidate (HCl)MetyrosineTheoretical potential for PHENYLBUTAZONE reducing the HYPOTENSIVE effect of METIROSINEModerateOxaprozinPerindoprilTheoretical potential for PHENYLBUTAZONE reducing the HYPOTENSIVE effect of Perindopril Erbumine. ModeratePhenobarbitonePhenytoin (Na)Phenytoin (Na)SulfapyridinePhenylbutazone has also been reported to potentiate the effects of sulfonamides.SulphamethizolePhenylbutazone may displace sulfonamides from plasma protein binding sites, increasing sulfonamide concentrations.TenoxicamThyroxine (Na)TolbutamideTolbutamideWarfarin (Na) These interactions are sometimes beneficial and sometimes may pose threats to life. Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Interfrence
Thyroid Function Test
Risks
Drug should not be given to Pregnant Mothers, Geriatrics, and Neonates.If prescribing authority justifies the benefits of the drug against the possible damages he/she should reevaluate them and consult the reference material and previous studies.
Storage
Tab Store Below 25°C. Protect from Moisture.
Warnings
Phenylbutazone should be used with caution in patients with incipient cardiac failure, blood dyscrasias, pancreatitis, kidney or liver diseases, gastrointestinal (GI) inflammation.patients should observe caution while driving or performing other tasks requiring alertness, because it may cause drowsiness.
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