Mechanism of action:
Diazoxide causes activation of the ATPase sensitive potassium channels resulting in the hyperpolarization of the vascular smooth muscles leading to the relaxation of the arterioles (smooth muscles) leading to reduced systemic vascular resistance resulting in diminished blood pressure.
Actions:
It causes a promoted cardiac rate and cardiac output along with a fall in both of the systolic and diastolic pressure due to its vasodepressive action. This vasodepression is most importantly due to arteriolar dilatation, however venous dilatation is also effective in causing vasodepression.
It also causes relaxation of the other smooth muscles.
It also blocks the release of insulin from pancreatic β-cells. It can cause salt and water retention resulting in weight gain.
Therapeutic uses:
1. It is used in hypertensive crisis (IV).
2. It is used in hypoglycemia due to hyperinsulinemia (Oral).
Pharmacokinetics:
Most of the drug gets bind with protein. Its plasma half life is about 25-60 hours. The drug is eliminated by renal tubular secretion and biotransformation.
Adverse effect:
It may cause Angina, edema, serious hypotension which may lead to stroke and myocardial infarction or Hyperglycemia.
Contraindications:
It is contraindicated in patients of
1. Diabetes mellitus
2. Congestive heart failure
Dosage:
In the beginning 75-100 mg; but if necessary dose may increase up to 150 mg every 5 minute until blood pressure comes to normal.
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