Metligine
Metligine Uses, Dosage, Side Effects, Food Interaction and all others data.
An ethanolamine derivative that is an adrenergic alpha agonist. It is used as a vasoconstrictor agent in the treatment of hypotension.
Metligine is a prodrug, i.e., the therapeutic effect of orally administered midodrine is due to the major metabolite desglymidodrine formed by deglycination of midodrine. Administration of midodrine results in a rise in standing, sitting, and supine systolic and diastolic blood pressure in patients with orthostatic hypotension of various etiologies. Standing systolic blood pressure is elevated by approximately 15 to 30 mmHg at 1 hour after a 10-mg dose of midodrine, with some effect persisting for 2 to 3 hours. Metligine has no clinically significant effect on standing or supine pulse rates in patients with autonomic failure.
| Trade Name | Metligine |
| Availability | Prescription only |
| Generic | Midodrine |
| Midodrine Other Names | Midodrin, Midodrina, Midodrine, Midodrinum |
| Related Drugs | phenylephrine, norepinephrine, ephedrine, Levophed, droxidopa, ProAmatine |
| Type | |
| Formula | C12H18N2O4 |
| Weight | Average: 254.2823 Monoisotopic: 254.126657074 |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | Japan |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Metligine is an alpha-adrenergic antagonist used to treat orthostatic hypotension.
For the treatment of symptomatic orthostatic hypotension (OH).
Metligine is also used to associated treatment for these conditions: Symptomatic Orthostatic Hypotension
How Metligine works
Metligine undergoes metabolism to form its pharmacologically active metabolite, desglymidodrine. Desglymidodrine acts as an agonist at the alpha1-adrenergic receptors expressed in the arteriolar and venous vasculature. Activation of alpha1-adrenergic receptor signaling pathways lead to an increase in the vascular tone and elevation of blood pressure. Desglymidodrine is reported to have negligible effect on the cardiac beta-adrenergic receptors.
Toxicity
Symptoms of overdose could include hypertension, piloerection (goosebumps), a sensation of coldness and urinary retention. The single doses that would be associated with symptoms of overdosage or would be potentially life- threatening are unknown. The oral LD50 is approximately 30 to 50 mg/kg in rats, 675 mg/kg in mice, and 125 to 160 mg/kg in dogs. Desglymidodrine is dialyzable.
Food Interaction
- Take with or without food. The absorption is unaffected by food.
Metligine Hypertension interaction
[Major] Metligine can cause marked elevation of supine blood pressure (BP>200 mmHg systolic) and should not be used in patients with persistent and excessive supine hypertension.
Systolic elevations of this degree are most likely to be observed in patients with relatively elevated pre-treatment systolic blood pressures (mean 170 mmHg).
There is no experience in patients with initial supine systolic pressure above 180 mmHg, as those patients were excluded from the clinical trials.
Use of midodrine in such patients is not recommended.
Additionally, care should be taken when using this agent in orthostatic hypotensive patients who are also diabetic.
Supine and sitting hypertension should be evaluated at the beginning of therapy, and blood pressure (supine, sitting, and orthostatic) should be monitored regularly.
Metligine Drug Interaction
Unknown: diphenhydramine, diphenhydramine, apixaban, apixaban, polyethylene glycol 3350, polyethylene glycol 3350, levothyroxine, levothyroxine, acetaminophen, acetaminophen, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol, ondansetron, ondansetron, cetirizine, cetirizine
Metligine Disease Interaction
Major: hypertension/diabetes, hypertensive effects, renal dysfunctionModerate: hepatic dysfunction
Elimination Route
Rapidly absorbed following oral administration. The peak plasma concentrations of the prodrug, desglymidodrine, is reached about half an hour following drug administration. The metabolites reach their peak plasma concentrations at about 1 to 2 hours following drug administration. The absolute bioavailability of midodrine (measured as desglymidodrine) is 93% and is not affected by food. As desglymidodrine displays poor diffusibility across the blood-brain barrier, it is expected to have minimal effects on the central nervous system.
Half Life
The metabolites display a half-life of about 3 to 4 hours.
Clearance
- Renal cl=385 mL/minute
Innovators Monograph
You find simplified version here Metligine
