Moxisylyte
Moxisylyte Uses, Dosage, Side Effects, Food Interaction and all others data.
Moxisylyte, denominated as thymoxamine in the UK, is a specific and orally active α1-adrenergic antagonist. According to the WHO, moxisylyte is approved since 1987 and in the same year, it acquired the denomination of orphan product by the FDA. This drug was developed by the Japanese company Fujirebio and also by the American company Iolab in the late 80s.
Administration of moxisylyte has shown to improve peripheral flow in occlusive arterial disease with little effect in blood pressure. There are reports of increases in cutaneous blood flow and skin temperature after local application of moxisylyte.
| Trade Name | Moxisylyte |
| Generic | Moxisylyte |
| Moxisylyte Other Names | Moxisylyte |
| Type | |
| Formula | C16H25NO3 |
| Weight | Average: 279.38 Monoisotopic: 279.183443669 |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
By the WHO, moxisylyte is indicated for the symptomatic management of sequelae of cerebral infarction or hemorrhage. The cerebral infarction is characterized by the blockage of the artery either by the formation of a thrombus or an embolus.
On the other hand, the FDA classified moxisylyte for the reversal of phenylephrine-induced mydriasis in patients who have narrow anterior angles and are at risk of developing an acute attack of angle-closure glaucoma. Closed-angle glaucoma is caused by the contact between the iris and the trabecular meshwork. This contact will damage the aqueous outflow by the meshwork thus, increasing eye pressure and producing the symptoms of glaucoma. Mydriasis is referred to the dilatation of the pupils and this standard body function is known to be a trigger factor for the development of acute closed-angle glaucoma.This risk is explained by the generation of a pupillary block, which is the contact between the pupillary margins and the lens, thus preventing flow from the aqueous humor to the anterior chamber and followed by an increased pressure gradient.
Moxisylyte is also approved in France as the first drug for the treatment of impotence.
How Moxisylyte works
Moxisylyte is vasodilator that works as a specific alpha-adrenergic blocking agent. Its action is known to be competitive against norepinephrine without beta-receptor blocking, anti-angiotensin or anti-serotonin activity.
Toxicity
Moxisylyte is very well accepted by the patients and it presents very few adverse effects. The side effects are usually related to a profound alpha blockade than to a toxic response.
Volume of Distribution
In preclinical trials, the volume of distribution presented for beagle dogs is in the range of 0.83-0.98 L/kg.
Elimination Route
Moxisylyte is rapidly absorbed after oral administration. Its pharmacokinetic profile is linear in the dose range from 10 to 30 mg for the values of Cmax and AUC. After intravenous administration, the maximal plasma concentration was of 352.8 ng/ml with an AUC of 152.6 mcg h/L. In preclinical trials, the bioavailability was always presented in approximately 10%.
Half Life
The half-life of moxisylyte was of 1-2 hours.
Clearance
In preclinical trials, the plasma clearance was of 7.17 ml min/kg for beagle dogs.
Elimination Route
The major elimination route of moxisylyte is via the kidneys. The complete elimination of all the metabolites by urine is of 75% when administered intravenously and 69% when administered orally. From the elimination profile, The specific ranges of the two major metabolites of moxisylyte in the urine are of 50% and 10% for desacetyl-thymoxamine and N-monodemethyl-desacetyl-thymoxamine respectively. The fecal elimination corresponded only to the 14% of the administered dose.
Innovators Monograph
You find simplified version here Moxisylyte
