Diazoxide causing

Diazoxide is a potassium channel opener with a rapid antihypertensive action after intravenous administration. Diazoxide causes hyperglycaemia which may underlie side-effects such as nausea and vomiting, cardiac dysrhythmia and ketosis. Diazoxide was used occasionally in the management of hypertensive emergencies, but it is now largely abandoned for this indication. Diazoxide is an alternative for glucagons in patients with hypogycaemia. 

In contrast to the structurally related thiazide diuretics, diazoxide causes renal salt and water retention. However, because the drug is used for short periods only, this is rarely a problem. 

INSULIN VASODILATOR ANTIHYPERTENSIVES-DIAZOXIDE May t insulin requirement Diazoxide causes hyperglycaemia by inhibiting insulin release and probably by a catecholamine-induced extrahepatic effect. Used in the treatment of hypoglycaemia due to insulinomas Larger doses of insulin are often required, and there is a need to monitor blood sugar until adequate control of blood sugar is achieved... 

Because it stimulates the same potassium channel in the pancreatic islet cells as is blocked by sulphonylureas, diazoxide causes hyperglycaemia. This effect renders diazoxide unsuitable for chronic use in h5 ertension, but a useful drug to treat insulinoma. Long-term oral administration causes the same problem of hair growth seen with minoxidil (see below and alopecia ). 

Diazoxide causes hyperglycaemia by inhibiting insulin release and probably by a catecholamine-induced extrahepatic effect. Used in the treatment of hypoglycaemia due to insulinomas... 

Diazoxide Opens K4 channels and causes hyper polarization of smooth muscle. 

Diazoxide (II) has been known since the early 1960 s (9.) and must be considered as a well known lead. It bears a structural resemblance to the diuretic agent, chlorothiazide (XIX) but, unlike chlorothiazide, it is non-diuretic. Analogs have been prepared by scientists at Schering (10) and by a group in Italy (11). The Italian group reported that compound XX lowers blood pressure and heart rate intravenously in rats but causes... 

Diazoxide given i.v. causes prominent arteriolar dilation it can be employed in hypertensive crises. After its oral administration, insulin secretion is inhibited. Accordingly, diazoxide can be used in the management of insulin-secreting pancreatic tumors. Both effects are probably due to opening of (ATP-gated) K+ channels. 

Other vasodilators, such as diazoxide and minoxidil, cause dilation of blood vessels by activating potassium channels in vascular smooth muscle. An increase in potassium conductance results in hyperpolarization of the cell membrane, which will cause relaxation of vascular smooth muscle. 

Diazoxide (Hyperstat) is chemically similar to the thiazide diuretics. It is devoid of diuretic activity and causes Na and water retention. Diazoxide is a very potent vasodilator and is available only for intravenous... 

Diazoxide may cause hyperglycemia, especially in diabetics, so if the drug is used for several days, blood glucose levels should be measured. 

Diazoxide Opens channels and causes hyperpolarization of smooth muscle. 

From a clinical perspective, some of these PCO classes have attracted initial attention. Diazoxide and minoxidil have been evaluated as antihypertensive agents. These PCOs open K+ channels in the plasma membranes of vascular smooth muscle cells, causing vascular vasodilation, thereby lowering blood pressure. Cromakalim has been investigated as a smooth muscle bronchodilator for the treatment of human asthma. Nicorandil was launched in Japan in 1984 for the treatment of angina because of its perceived ability to promote vasodilation of coronary arteries. Developmental work on these and other PCOs is continuing for indications ranging from hypertension, asthma, urinary incontinence, psychosis, epilepsy, pain, and alopecia (hair loss). 

The peripheral receptors activated by noradrenaline fall into at least two classes, a-receptors and /3-receptors, which differ in their function and in their response to drugs. The a-receptors cause constriction of blood vessels and compounds used to block them include indoramin (216), prazosin (217) and phentolamine (218). Another imidazoline, tolazoline (2-benzyl-2-imidazoline), is a useful vasodilator but is unsuitable for the treatment of hypertension since it stimulates the heart. Other drugs described as peripheral vasodilators are diazoxide (219), which is related to the thiazide diuretics, hydralazine (220) which also depresses the CNS, hydracarbazine (221) and minoxidil (222). The /3-receptors control the action of adrenaline on the heart (among other effects) and the agents that block them are mostly nonheterocyclic aromatic compounds with aminoethanol or 3-amino-2-hydroxypropoxy side-chains. They have proved effective in the treatment of hypertension. One heterocyclic compound of this class, timolol (223), is in use. 

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