Phenoxybenzamin (marketed under the trade name Dibenzyline) is an alpha-adrenergic antagonist with long duration of action. It is indicated in the treatment of pheochromocytoma, to control episodes of hypertension and sweating. If tachycardia is excessive, it may be necessary to use a beta-blocking agent concomitantly. Phenoxybenzamine produces its therapeutic actions by blocking alpha receptors, leading to a muscle relaxation and a widening of the blood vessels. This widening of the blood vessels results in a lowering of blood pressure. Phenoxybenzamine hydrochloride can produce and maintain “chemical sympathectomy” by oral administration. It increases blood flow to the skin, mucosa and abdominal viscera, and lowers both supine and erect blood pressures. It has no effect on the parasympathetic system. Twenty to percent of orally administered phenoxybenzamine appears to be absorbed in the active form. The half-life of orally administered phenoxybenzamine hydrochloride is not known; however, the half-life of intravenously administered drug is approximately 24 hours. Demonstrable effects with intravenous administration persist for at least 3 to 4 days, and the effects of daily administration are cumulative for nearly a week. The following adverse reactions have been observed, but there are insufficient data to support an estimate of their frequency: Postural hypotension, tachycardia, inhibition of ejaculation, nasal congestion, and miosis. These so-called “side effects” are actually evidence of adrenergic blockade and vary according to the degree of blockade. Miscellaneous: Gastrointestinal irritation, drowsiness, fatigue.

Cyclandelate is a vasodilator developed for the treatment of cardiovascular diseases. The drug was used in many countries for such diseases as intermittent claudication, arteriosclerosis obliterans, thrombophlebitis, nocturnal leg cramps, local frostbite, Raynaud's phenomenon. In the USA it was also approved for intermittent claudication and cognitive dysfunction in Alzheimer's disease under the name Cyclospasmol. Cyclandelate exerts its effect by blocking calcium channels and inhibiting smooth muscles contration. Cyclandelate was withdrawn from the market in the USA for lack of effectiveness.

AZAPETINE, a benzazepine derivative, is an alpha-1 adrenoceptor antagonist. It is a potent arterial vasodilator in the treatment of peripheral vascular diseases.

Fasudil is a potent Rho kinase inhibitor, which was developed by Asahi Kasei. The drug is used in Asia for the prevention of cerebral vasospasm in patients with subarachnoid hemorrhage.

Bencyclane, a cycloheptane, is a vasodilator, antiplasmodic and a platelet aggregation inhibitor found to be effective in a variety of peripheral circulation disorders. Bencyclane has various other potentially useful pharmacological effects such as smooth muscle relaxation. Under the trade name Halidor it is used in several European countries to treat the symptoms of atherosclerosis, occlusive arterial disease. Its mechanism may involve block of calcium channels. However as was shown in vitro it does not act by a direct influence on the Ca2+ pumps of vascular smooth muscle cells. In in vitro biochemical assays related to smooth muscle excitation-contraction coupling, binding to beta 1-, beta 2-, and alpha-adrenergic receptors, inhibition of phosphodiesterase activity, and antagonism of calcium accumulation bencyclane bound to alpha- and beta-receptors. Bencyclane appeared to be a promising anti-sickling agent that can be used orally in sickle cell anaemia (SCD).

Naftidrofuryl (INN), also known as nafronyl or as the oxalate salt naftidrofuryl oxalate or nafronyl oxalate, is a vasodilator used in the management of peripheral and cerebral vascular disorders. The drug act as a selective antagonist of 5-HT2 receptors. Naftidrofuryl is marketed under a variety of trade names, including Artocoron, Azunaftil, Di-Actane, Dusodril, Enelbin, Frilix, Gevatran, Iridus, Iridux, Luctor, Nafti, Naftoling, Naftodril, Nafoxal, Praxilene, Sodipryl retard, and Vascuprax. Praxilene belongs to a group of medicines known as ‘metabolic activators’. These are used to treat different types of blood circulation problems. Praxilene allows the body to make better use of the oxygen in your blood. Praxilene is used to treat the following symptoms: cramp-like pains; cramps in legs at night; severe pain in r legs when people are resting (rest pain); pale or blue fingers or toes which get worse when it is cold; numbness, tingling or burning feelings in the fingers or toes (Raynaud’s syndrome or acrocyanosis); open sores on the legs or feet (trophic ulcers); poor circulation caused by diabetes (diabetic arteriopathy).

Ifenprodil (marketed under the brands Vadilex; Dilvax; Creocral; Cerocral) is a selective NMDA receptor (glutamate) antagonist. Additionally, ifenprodil inhibits GIRK channels, and interacts with alpha1 adrenergic, serotonin, and sigma receptors. Ifenprodil acts as a vasodilator. Ifenprodil is a medicine available in a number of countries worldwide, but not in US.

Cetiedil is effective potassium channel blocker used as a peripheral vasodilator to treat patients with painful crises in sickle cell anemia and pain in the extremities caused by an arterial disease. Known pharmacological properties of the drug include vascular smooth muscle relaxation, inhibition of phosphodiesterase with the consequent increase in circulating cyclic AMP concentration, blockade of the effect of bradykinin and serotonin, analgesia, inhibition of platelet aggregation and the decrease of plasma and blood viscosity and plasma fibrinogen level. The antisickling effect of cetiedil is explained mainly in the light of the changes it induces in the activities of membrane-bound ATPases and the permeability properties of the erythrocyte membrane to cations and anions.

Butalamine hydrochloride under the brand name Adrevil forte is an effective drug for the treatment of patients suffering from blood flow disorders of the lower extremities.

Cinepazide or cinepazide maleate (Kelinao or Anjieli in China) is a vasodilator used in China for the treatment of cardiovascular and cerebrovascular diseases, and peripheral vascular diseases. As a calcium channel blocker, cinepazide can stop calcium from entering vascular smooth muscle cells and relax smooth muscles of cerebral vessels, coronary arteries and peripheral vessels so as to relieve vasospasm, reduce vascular resistance, improve flexibility of red blood cells, increase blood circulation in cerebral vessels and improve microcirculation and brain metabolism. Cinepazide could also increase the number of cAMP by inhibiting cAMP phosphodiesterase and reduce oxygen consumption. In April 2002, cinepazide of Beijing Hwellso Pharmaceutical Co., Ltd was approved to enter the market with two dosage forms of oral formulation and injection under the trade name of Kelinao. Currently, Kelinao is the only domestic brand for the treatment of cardiovascular diseases. And in 2009, cinepazide was included in the national medicare drug list. Cinepazide maleate, after wide application, has gained the recognition of Chinese doctors and patients for the treatment of cerebral arteriosclerosis, transient ischemic attack, cerebral thrombosis, cerebral embolism, cerebral hemorrhage sequel and post-traumatic brain syndrome. Besides, due to its efficacy in cardiovascular diseases and peripheral vascular diseases, cinepazide maleate has become a leading product in cerebrovascular drug market.