INTRODUCTION-
Phenylbutazone is a synthetic, pyrazolone derivative. It is a nonhormonal anti-inflammatory, antipyretic compound useful in the management of inflammatory conditions. The apparent analgesic effect is probably related mainly to the compound's anti-inflammatory properties and arise from its ability to reduce production of prostaglandin H and prostacyclin. Prostaglandins act on a variety of cells such as vascular smooth muscle cells causing constriction or dilation, on platelets causing aggregation or disaggregation and on spinal neurons causing pain. Prostacylcin causes vascular constriction platelet disaggregationPhenylbutazone, often referred to as "bute",[1] is a nonsteroidal anti-inflammatory drug (NSAID) for the short-term treatment of pain and fever in animals.
In the United States and United Kingdom, it is no longer approved for human use, as it can cause severe adverse effects such as suppression of white blood cell production and aplastic anemia
MECHANISM OF ACTION-
Phenylbutazone binds to and inactivates prostaglandin H synthase and prostacyclin synthase through peroxide (H2O2) mediated deactivation. The reduced production of prostaglandin leads to reduced inflammation of the surrounding tissues.
USES-
1-use in humans for the treatment of rheumatoid arthritis and gout
2-used to treat ankylosing spondylitis, but only when other therapies are unsuitable in UK
SIDE EFFECT-
1-gastrointestinal ulcers,
2-blood dyscrasia,
3- kidney damageoral lesions if given by mouth,
DRUG DRUG INTERACTION-
Phenylbutazone may affect blood levels and duration of action of phenytoin, valproic acid, sulfonamides, sulfonylurea antidiabetic agents, barbiturates, promethazine, rifampicin, chlorpheniramine, diphenhydramine, and penicillin G.
REFERENCE-
Tripathi K.D,"Essentials of medical pharmacology",7th edition,page no.192
Phenylbutazone is a synthetic, pyrazolone derivative. It is a nonhormonal anti-inflammatory, antipyretic compound useful in the management of inflammatory conditions. The apparent analgesic effect is probably related mainly to the compound's anti-inflammatory properties and arise from its ability to reduce production of prostaglandin H and prostacyclin. Prostaglandins act on a variety of cells such as vascular smooth muscle cells causing constriction or dilation, on platelets causing aggregation or disaggregation and on spinal neurons causing pain. Prostacylcin causes vascular constriction platelet disaggregationPhenylbutazone, often referred to as "bute",[1] is a nonsteroidal anti-inflammatory drug (NSAID) for the short-term treatment of pain and fever in animals.
In the United States and United Kingdom, it is no longer approved for human use, as it can cause severe adverse effects such as suppression of white blood cell production and aplastic anemia
MECHANISM OF ACTION-
Phenylbutazone binds to and inactivates prostaglandin H synthase and prostacyclin synthase through peroxide (H2O2) mediated deactivation. The reduced production of prostaglandin leads to reduced inflammation of the surrounding tissues.
USES-
1-use in humans for the treatment of rheumatoid arthritis and gout
2-used to treat ankylosing spondylitis, but only when other therapies are unsuitable in UK
SIDE EFFECT-
1-gastrointestinal ulcers,
2-blood dyscrasia,
3- kidney damageoral lesions if given by mouth,
DRUG DRUG INTERACTION-
Phenylbutazone may affect blood levels and duration of action of phenytoin, valproic acid, sulfonamides, sulfonylurea antidiabetic agents, barbiturates, promethazine, rifampicin, chlorpheniramine, diphenhydramine, and penicillin G.
REFERENCE-
Tripathi K.D,"Essentials of medical pharmacology",7th edition,page no.192
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