Perhexilinum
Perhexilinum Uses, Dosage, Side Effects, Food Interaction and all others data.
Perhexilinum is a coronary vasodilator used especially for angina of effort. It may cause neuropathy and hepatitis.
Used in the treatment of unresponsive or refractory angina. Perhexilinum increases glucose metabolism at the expense of free-fatty-acid metabolism, enhancing oxygen efficiency during myocardial ischaemia. Perhexilinum also potentiates platelet responsiveness to nitric oxide both in patients with angina and patients with acute coronary syndrome. The predominant mechanism of this particular perhexiline effect is an increase in platelet cGMP responsiveness. Perhexilinum also may reduce the potential for nitric oxide clearance by neutrophil-derived oxygen. Perhexilinum relieves symptoms of angina, improves exercise tolerance, and increases the workload needed to induce ischaemia when used as monotherapy. The primary therapeutic roles for perhexiline are as short-term therapy (less than 3 months duration) in patients with severe ischaemia awaiting coronary revascularisation or long-term therapy in patients with ischaemic symptoms refractory to other therapeutic measures.
| Trade Name | Perhexilinum |
| Generic | Perhexiline |
| Perhexiline Other Names | Perhexilene, Perhexilina, Perhexiline, Perhexilinum |
| Type | |
| Formula | C19H35N |
| Weight | Average: 277.4879 Monoisotopic: 277.276950125 |
| Protein binding | Perhexiline and its metabolites are highly protein bound (>90%). |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
For the management of severe angina pectoris.
How Perhexilinum works
Perhexilinum binds to the mitochondrial enzyme carnitine palmitoyltransferase (CPT)-1 and CPT-2. It acts by shifting myocardial substrate utilisation from long chain fatty acids to carbohydrates through inhibition of CPT-1 and, to a lesser extent, CPT-2, resulting in increased glucose and lactate utilization. This results in increased ATP production for the same O2 consumption as before and consequently increases myocardial efficiency.
Toxicity
Oral LD50 rat: 2150 mg/kg; Oral LD50 Mouse: 2641 mg/kg. Short term adverse effects include nausea, transient dizziness, hypoglycaemia in diabetic patients, and torsade de pointes (rare).
Elimination Route
Well absorbed (>80%) from the gastrointestinal tract following oral administration.
Half Life
Variable and non-linear. Some reports show a half-life of 2-6 days, others indicate it could be as high as 30 days.
Innovators Monograph
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