Proglicem
Proglicem - General Information
A benzothiadiazine derivative that is a peripheral vasodilator used for hypertensive emergencies. It lacks diuretic effect, apparently because it lacks a sulfonamide group. [PubChem]
Pharmacology of Proglicem
Proglicem is a potassium channel activator, which causes local relaxation in smooth muscle by increasing membrane permeability to potassium ions. This switches off voltage-gated calcium ion channels which inhibits the generation of an action potential.
Proglicem for patients
Proglicem Interactions
Proglicem Contraindications
Contraindicated in ischemic heart disease as the reflex sympathetic response to diazoxide can provoke angina, electrocardiographic evidence of ischemia, and cardiac failure in patients with ischemic heart disease. Also in hyperglycemia as it can complicate diazoxide use, particularly in persons with renal insufficiency.
Additional information about Proglicem
Proglicem Indication: Used parentally to treat hypertensive emergencies. Also used to treat hypoglycemia secondary to insulinoma.
Mechanism Of Action: As a diuretic, diazoxide inhibits active chloride reabsorption at the early distal tubule via the Na-Cl cotransporter, resulting in an increase in the excretion of sodium, chloride, and water. Thiazides like diazoxide also inhibit sodium ion transport across the renal tubular epithelium through binding to the thiazide sensitive sodium-chloride transporter. This results in an increase in potassium excretion via the sodium-potassium exchange mechanism. The antihypertensive mechanism of diazoxide is less well understood although it may be mediated through its action on carbonic anhydrases in the smooth muscle or through its action on the large-conductance calcium-activated potassium (KCa) channel, also found in the smooth muscle. As a antihypoglycemic, diazoxide inhibits insulin release from the pancreas, probably by opening potassium channels in the beta cell membrane.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Diazoxide
Synonyms: Not Available
Drug Category: Antihypertensive Agents; Diuretics, Thiazide; Vasodilator Agents
Drug Type: Small Molecule; Approved
Other Brand Names containing Diazoxide: Dizoxide; Eudemine; Hyperstat; Hypertonalum; Mutabase; Proglicem; Proglycem;
Absorption: Readily absorbed following oral administration.
Toxicity (Overdose): Oral LD50 in rat and mouse: 980 mg/kg and 444 mg/kg, respectively.
Protein Binding: Very high (more than 90%) to serum proteins.
Biotransformation: Hepatic.
Half Life: 28 ±8.3 hours in normal adults.
Dosage Forms of Proglicem: Capsule Oral
Chemical IUPAC Name: 7-chloro-3-methyl-4H-benzo[e][1,2,4]thiadiazine 1,1-dioxide
Chemical Formula: C8H7ClN2O2S
Diazoxide on Wikipedia: https://en.wikipedia.org/wiki/Diazoxide
Organisms Affected: Humans and other mammals
