Swellstop

Drug Category: Steroid anti-inflammatory + non-steroidal anti-inflammatory

Dosage form: Sterile injectable Solution

Composition: Each ml of drug contains 180 mg phenylbutazone plus 0.35 mg dexamethasone it is in the form of sodium phosphate salt.

Mechanism of action: Phenylbutazone block the first step of prostaglandin synthesis by binding to and inhibition cyclooxygenase. Phenylbutazone is a Nonsteriodal anti-inflammatmy drug (NSAID) Phenylbutazone and other NSAID have no direct effect on pain perception, rather, they reduce hypersensitiv­ity to pain by reducing the inflammatmy response inflamed tissue.

Dexamethasone is a flouro-methyl derivative of prednisolone which exhibits potent gluconeogenic, anti-inflammatory and anti-shock properties. Steroid hormones are known to exist in plasma, bound partly to albumin but mainly to a transport protein (in the case of cortisol, a- globulin called transcortin). This complex releases the steroid at appropriate cells which the steroid then enters. Inside the cell, the steroid reacts with a specific receptor protein which then undergoes a confonnational change. Within the nucleus the complex, its binding sites now exposed, become attached to a chromatin protein and DNA. In this position the synthesis of proteins is influenced by an action which increases the transcription of mRNA, perhaps due to a de-repressing action of the complex on the appropriate part of the genome, e.g. leading in the liver to the synthesis of enzymes involved in gluconeogen­esis and glycogenesis

Pharmacokinetics:

Phenylbutazone is readily absorbed following intravenous administration. Phenylbutazone is estimated to be 99% bound to plasma albumen. Phenylbutazone is metabolized by the liver, with less than 2% of the drug being excreted as parent compound in the urine in some species.

Its major metabolites are oxyphenylbutazone, which is less active than phenylbutazone, and inactive 0 hydroxyphenylb­utazone. Dexamethasone is readily absorbed when given parenteral then its bonds to specific proteins of plasma ( a- globulin) namely transcortin which is reversible bounding. The half-life is 3-4.5 hours. Dexamethasone is rapidly metabolized in liver to inactive metabolites. This is excreted by kidneys.

Indications:

Phenylbutazone is a synthetic non-steroidal anti- inflammatmy drug

(NASID) used as an antipyretic, anti-inflammatmy, and analgesic. It is indicated for use in the treatment of muscular and articular inflammations including arthritis of the hock, stifle and hip, generalized arthritis, Laminitis in horses, Cattle and dogs.

It is also used to treat hypersensitivity reactions, shock and stress, etc.

Dosage and Administration Routs:

Horse :20 ml daily intravenously slowly or once every two days depending on the severity of the disease.

Dog: 1ml per 15 kg bodyweight daily by slow intravenous or intramuscular

Recommended tips:

Intravenous injection should be done slowly. Avoid aspiration of blood into the syringe during intravenous injection.

Intramuscular injection should be performed deep into the muscle. The drug should be injected under aseptic conditions.

Contra Indication:

Phenylbutazone is contraindicated in animals with cardiac, renal, or hepatic insufficiency.

Corticosteroids should not be used in bacterial, viral, or parasitic infections unless concurrent anti-infective agents are used. Clinical signs may abate with their use, but with their sole use the underlying disease remains active. Corticosteroids give to animal in the last trimester of pregnancy can induce premature parturition and predispose to retained placenta and and provide patient inflammation. Dexametha¬sone may delay wound healing.

Adverse and Common Side Effects:

High, continued doses of dexamethasone can cause suppression of adrenocortical function. Use of dexamethasone in horses under certain conditions has been associated with the occurrence of laminitis, possibly due to increased vascular reactivity to biogenic amines.

If phenylbutazone administered at a dose greater than the suggested recommendation, especially if a high dose is maintained for more than a few days. Signs of toxicity include anorexia, depression, oral and gastrointestinal ulcers, protein losing enteropathy, and death from shock. Neutropenia and severe depletion of bone marrow neutrophils also occur.

Drug Interactions:

Corticosteroid actions are potentiated by erythromycin, possibly by interference, with metabolism of the corticosteroids.

Phenylbutazone is highly bound to plasma proteins and can displace other drugs that bind to plasma proteins, such as other anti - inflammatmy drugs, sulfonamides, or anticoagulants such as warfarin, leading to increased phannacologi­cal effect or toxicity of the displaced drug.

Pharmaceutical precautions:

Store below 30°C, protected from light. Do not freeze.

Packaging: 20 ml, 50 ml and l00 ml glass vial.