Trimetazidine is a medicine, which is used for the treatment of angina pectoris. The drug mechanism of action is explained by its ability to selectively inhibit long-chain 3-ketoacyl coenzyme A thiolase, an enzyme responsible for mitochondrial beta-oxidation of long chain fatty acids. Trimetazidine also increases pyruvate dehydrogenase activity, binds to the mitochondrial membrane, directly inhibits cardiac fibrosis and improves mechanical resistance of the sarcolemma.

Lidoflazine is a vasodilator used for the treatment of angina pectoris. Lidoflazine is a high-affinity blocker of the HERG K(+)channel.

Methylchromone (3-methylchromone) is the first synthetic chromone to be used clinically. It has both antispasmodic and coronary vasodilator actions. It was recommended for the treatment of angina pectoris but it doesn’t produce any remarkable improvements and its clinical use has been discontinued. Osteomalacia case caused by the ingestion of 3-methylchromone was reported. 3-methylchromone was used in ureteral lithiasis and gravels. 3-methylchromone stated to have better vitamin K activity.

Oxyfedrine, an amino ketone derivative and partial agonist at beta receptors, has been shown to have potent antianginal properties and to increase coronary blood flow in normal and ischemic myocardial regions.

Salvianolic acid B is a bioactive molecule isolated from Radix Salviae Miltiorrhizae. The compound shows high antioxidant and free radical scavenging activities. It is a major component of the commercial Fufang Danshen products (Compound Danshen Dripping Pill, the Danshen Pian, and the Danshen Injection, ICP), used for the treatment of angina pectoris, and other heart diseases.

Bepridil (trade name Vascor) is an amine calcium channel blocker used to treat angina. Bepridil is a calcium channel blocker that has well characterized anti-anginal properties and known but poorly characterized type 1 anti-arrhythmic and anti-hypertensive properties. It is not related chemically to other calcium channel blockers such as diltiazem hydrochloride, nifedipine and verapamil hydrochloride. Bepridil has inhibitory effects on both the slow calcium (L-type) and fast sodium inward currents in myocardial and vascular smooth muscle, interferes with calcium binding to calmodulin, and blocks both voltage and receptor operated calcium channels. Bepridil inhibits the transmembrane influx of calcium ions into cardiac and vascular smooth muscle. This has been demonstrated in isolated myocardial and vascular smooth muscle preparations in which both the slope of the calcium dose response curve and the maximum calcium-induced inotropic response were significantly reduced by bepridil. In cardiac myocytes in vitro, bepridil was shown to be tightly bound to actin. Bepridil regularly reduces heart rate and arterial pressure at rest and at a given level of exercise by dilating peripheral arterioles and reducing total peripheral resistance (afterload) against which the heart works. Bepridil is no longer sold in the United States, but it is still marketed in other countries. Bepridil has antihypertensive and selective anti-arrhythmia activities and acts as a calmodulin antagonist. Although, it contains one chiral center, it is generally administered as a racemates. The drug bepridil is a racemic mixture of two enantiomers for the 2R as CID 16048570 and 2S as CID 445143. (R)-isomer of bepridil is more active than (-S)- isomer, in certain cases. In the retrogradely perfused, paced rat heart the higher activity was found for the ( )-enantiomer, which was 4.27 times more potent in increasing coronary flow than the (-)-isomer. The two enantiomers of bepridil showed a lower activity on maximum systolic left ventricular pressure (MSLVP) than on coronary flow, and a similar 3-4 fold stereoselectivity with both parameters.

Celiprolol is beta blocker, used to treat high blood pressure. Celiprolol is a selective β1 receptor antagonist, β2 receptor partial agonist. Celiprolol is not approved by the FDA, but is available worldwide under brand names Cardem, Selectol, Celipres, Celipro, Celol, Cordiax, Dilanorm. It is used to treat mild to moderate hypertension and angina prectoris. In 2010 celiprolol has demonstrated positive results in the prevention of vascular complications of Ehlers-Danlos syndrome. Celiprolol has fewer CNS-related side effects than other beta blockers presumably because of limited penetration through blood-brain barrier because of its solubility.

Benidipine is an orally triple L-, T-, and N-type calcium channel blocker for the treatment of hypertension and angina pectoris synthesized and developed by Kyowa Hakko Kogyo Co., Ltd. Benidipine, approved in Japan in November 1991, has become one of the three best selling CCBs and is highly useful as a potent, long-lasting antihypertensive and antianginal agent.

Perhexiline, 2-(2,2-dicyclohexylethyl)piperidine, is an anti-anginal drug. Perhexiline reduces fatty acid metabolism through the inhibition of carnitine palmitoyltransferase, the enzyme responsible for mitochondrial uptake of long-chain fatty acids. Perhexiline is used for reducing the frequency of moderate to severe attacks of angina pectoris due to coronary artery disease in patients who have not responded to other conventional therapy or in whom such therapy may be contraindicated. Heart Metabolics Limited is developing perhexiline for the treatment of hypertrophic cardiomyopathy

Visnadine is a natural product extracted from the seeds and aerial parts of Ammi visnaga (Umbelliferae), plant widely used in Egyptian medicine since the Pharaohs times as antispastic and for the treatment of angina pectoris and other cardiovascular diseases. It has been used since a long time in western medicine for the treatment of various cardiac diseases and peripheral vasculopathies. Visnadine seems to act by inhibiting the contractile responses mediated by Ca2+ entry through L-type Ca2+ channels.Topical use of Visnadine may increase regional vascularization afecting turgidity and sensorial threshold of the area of application. A formulation for vulvar application (ReFeel® spray, IDI Integratori Dietetici Italiani S.r.l., Italy) has been developed and it contains Visnadine at high concentration (1%) with an elevate purity index (minimum 95%). Visnadine spray displayed positive effects on sexual function in women with and without FSD and it was well tolerated. Topical Visnadine may not only be part of multimodal strategies to manage clinically relevant sexual symptoms but also simply to help women to enhance their subjective impaired perception of sexual response.