Buflomedil is a molecule that acts as a vasodilator, to increase the caliber of small blood vessels. It also facilitates blood circulation.
Mechanism of action
Peripheral and cerebral vasoactive action. Improves microcirculation in areas of vascular insufficiency of the extremities and increases cerebral blood flow in enf. cerebrovascular.
Description
The vascular activity of buflomedil is due to an a1- and a2-adrenergic effect and a direct action on the smooth muscular structures of the microcirculation. Due to its nonspecific adrenergic action, buflomedil locally antagonizes the effects of adrenaline, stress, and cold. Due to its action on microcirculation, buflomedil acts on the entry of calcium into perivascular myocytes, opening the precapillary sphincters and restoring musculocutaneous circulation. Microcinematographic studies in hamsters have shown that the administration of buflomedil by the intra-arterial, intravenous and intraduodenal routes increases femoral flow and skin and muscle flows with a decrease in peripheral resistance. In the man,red blood cells . Buflomedil has few hemodynamic effects without altering blood pressure , heart rate, left ventricular ejection pressure, or cardiac output. It exerts a peripheral and cerebral vasoactive action. It improves blood flow at the microcirculation level in areas of vascular insufficiency of the extremities and increases cerebral blood flow in patients with cerebrovascular disease . Its effectiveness in intermittent claudication is not proven in well-conducted clinical studies.
Pharmacokinetics
In laboratory animals, buflomedil is rapidly absorbed from the intestine, essentially remaining in plasma as free drug (50%). The plasma elimination half-life is short, about 2 hours. The speed of elimination and exchange between compartments does not depend on the route of administration. The volume of distribution is high, indicating that the drug experiences a large tissue distribution. Buflomedil is metabolized in the liver, mainly by isoenzyme 2D6 of cytochrome P450, and is subsequently eliminated in the urine., partly in the form of glucuronide conjugates and partly unmetabolized. However, in normal subjects, the simultaneous administration of a CYP2D6 inhibitor does not appear to have consequences, at least in terms of tolerance. In subjects with renal or hepatic impairment, inhibition of CYP2D6 could lead to a reduction in the clearance of buflomedil with a corresponding risk of an increased incidence of side effects, particularly at the neurological level.
Applications
Buflomedil is used to treat obstruction of the arteries of the lower limbs (obliterating arteriopathy of the lower limbs or AOMI) and Raynaud’s syndrome which results in numbness (sometimes pain) of the extremities due to blood vascularization disorders .
Properties
Buflomedil is a substance capable of causing a dilation of the vessels (vasodilation).
Indications and dosage
Vascular sclerosis, arteriosclerosis, arteritis, Raynaud’s syndrome and disease, erythrocyanosis, Buerger’s disease, ulcers and other trophic skin lesions in which there is poor circulation . Intermittent claudication, varied vasospastic diseases, including those associated with diabetes and other metabolic disorders, arteriopathies (phases II, III and IV) of known or idiopathic aetiology.
Parenteral administration
- Adults: The injectable dose (IM or slow IV) is 2 ampoules / day. In perfusion in glucose solution or isotonic saline solution: 2-8 ampoules. The dose should be reduced by half in case of kidney failure.
Oral administration
- Adults: the recommended dose is 300 to 600 mg / day divided into 2-3 doses.
Contraindications
Buflomedil is contraindicated in the immediate postpartum and in the presence of severe arterial bleeding. It is also absolutely contraindicated in patients with epilepsy.
Pregnancy and breastfeeding
The safety of its use during pregnancy and lactation has not been established. There is no clinical experience of its use in patients under 18 years of age. For tablets only: this specialty contains lactose. Cases of intolerance to this component have been described in children and adolescents. Although the amount is probably not enough to trigger symptoms of intolerance, should diarrhea appear, you should consult your doctor. In case of overdose, an increase in heart rate and decrease in blood pressure, seizures, coma and cardiac arrest may occur. If there is brain excitement, a benzodiazepine can be given .
Incompatibilities
No incompatibilities or interactions with other drugs have been described.
Adverse reactions
It is well tolerated. No significant changes in blood, kidney and liver function are observed after use. Side effects are rare and transient: headache, vertigo, nausea, gastrointestinal disturbances, itching, fainting, and flushing.