Dihydropyridine calcium channel blockers are derivatives of 1,4-dihydropyridine that are used as L-type calcium channel blockers. [1] They are used in the treatment of hypertension. [2]
Compared with certain other L-type calcium channel blockers (for example those of the phenylalkylamine class such as verapamil) that have significant action at the heart, the dihydropyridine calcium channel blockers lower blood pressure mainly by relaxing the smooth muscle of the blood vessel walls. [3]
Dihydropyridine class L-type calcium channel blockers include, in alphabetical order (brand names vary in different countries):
Name | Image | Brand name | Citations |
Amlodipine | ![]() | Norvasc, Istin, Normodipine, Tenox, Cordi Cor | [4] |
Aranidipine | ![]() | Sapresta (サプレスタ) | [5] |
Azelnidipine | ![]() | CalBlock (カルブロック) | [6] |
Barnidipine | ![]() | Vasexten, Libradin, Cyress, HypoCa | [7] |
Benidipine | ![]() | Coniel | [8] |
Cilnidipine | ![]() | Atelec (アテレック), Cilacar, Cinalong, Siscard | [9] |
Clevidipine | ![]() | Cleviprex | [10] |
Cronidipine | ![]() | [11] | |
Darodipine | ![]() | [12] | |
Dexniguldipine | ![]() | [13] | |
Efonidipine | ![]() | Landel (ランデル) | [14] |
Elgodipine | ![]() | [15] | |
Elnadipine | ![]() | [16] | |
Felodipine | ![]() | Renedil, Plendil | [17] |
Flordipine | ![]() | [18] | |
Furnidipine | ![]() | [19] | |
Iganidipine | ![]() | [20] | |
Isradipine | ![]() | DynaCirc CR | [21] |
Lacidipine | ![]() | Lacipil, Motens, Sakure | |
Lemildipine | ![]() | ||
Lercanidipine | ![]() | Zanidip, Zanidip-Recordati | |
Levamlodipine | ![]() | EsCordi Cor | |
Levniguldipine | ![]() | ||
Manidipine | ![]() | Manyper, Caslot, Madipine | |
Nicardipine | ![]() | Cardene, Cardene SR | |
Nifedipine | ![]() | Adalat, Nifedical, Procardia, Corinfar, Cordaflex | |
Niguldipine | ![]() | ||
Niludipine | ![]() | ||
Nilvadipine | ![]() | Nivadil | |
Nimodipine | ![]() | Nimotop | |
Nisoldipine | ![]() | Sular, Baymycard, Syscor | |
Nitrendipine | ![]() | Baypress, Cardif, Nitrepin, Baylotensin | |
Olradipine | ![]() | ||
Oxodipine | ![]() | ||
Palonidipine | ![]() | ||
Pranidipine | ![]() | Acalas | |
Ryodipine | ![]() | ||
Sagandipine | ![]() | ||
Sornidipine | ![]() | ||
Teludipine | ![]() | ||
Tiamdipine | ![]() | ||
Trombodipine | ![]() | ||
Vatanidipine | ![]() | ||
The pharmaceutical drug finerenone is also a dihydrophyridine derivative, but does not act as a calcium channel blocker but as an antimineralocorticoid. [22]
An analgesic drug, also called simply an analgesic, antalgic, pain reliever, or painkiller, is any member of the group of drugs used for pain management. Analgesics are conceptually distinct from anesthetics, which temporarily reduce, and in some instances eliminate, sensation, although analgesia and anesthesia are neurophysiologically overlapping and thus various drugs have both analgesic and anesthetic effects.
Calcium channel blockers (CCB), calcium channel antagonists or calcium antagonists are a group of medications that disrupt the movement of calcium through calcium channels. Calcium channel blockers are used as antihypertensive drugs, i.e., as medications to decrease blood pressure in patients with hypertension. CCBs are particularly effective against large vessel stiffness, one of the common causes of elevated systolic blood pressure in elderly patients. Calcium channel blockers are also frequently used to alter heart rate, to prevent peripheral and cerebral vasospasm, and to reduce chest pain caused by angina pectoris.
Verapamil, sold under various trade names, is a calcium channel blocker medication used for the treatment of high blood pressure, angina, and supraventricular tachycardia. It may also be used for the prevention of migraines and cluster headaches. It is given by mouth or by injection into a vein.
Antihypertensives are a class of drugs that are used to treat hypertension. Antihypertensive therapy seeks to prevent the complications of high blood pressure, such as stroke, heart failure, kidney failure and myocardial infarction. Evidence suggests that reduction of the blood pressure by 5 mmHg can decrease the risk of stroke by 34% and of ischaemic heart disease by 21%, and can reduce the likelihood of dementia, heart failure, and mortality from cardiovascular disease. There are many classes of antihypertensives, which lower blood pressure by different means. Among the most important and most widely used medications are thiazide diuretics, calcium channel blockers, ACE inhibitors, angiotensin II receptor antagonists (ARBs), and beta blockers.
Amlodipine, sold under the brand name Norvasc among others, is a calcium channel blocker medication used to treat high blood pressure, coronary artery disease (CAD) and variant angina. It is taken orally.
Diltiazem, sold under the brand name Cardizem among others, is a nondihydropyridine calcium channel blocker medication used to treat high blood pressure, angina, and certain heart arrhythmias. It may also be used in hyperthyroidism if beta blockers cannot be used. It is taken by mouth or injection into a vein. When given by injection, effects typically begin within a few minutes and last a few hours.
Betaxolol is a selective beta1 receptor blocker used in the treatment of hypertension and angina. It is also a adrenergic blocker with no partial agonist action and minimal membrane stabilizing activity. Being selective for beta1 receptors, it typically has fewer systemic side effects than non-selective beta-blockers, for example, not causing bronchospasm as timolol may. Betaxolol also shows greater affinity for beta1 receptors than metoprolol. In addition to its effect on the heart, betaxolol reduces the pressure within the eye. This effect is thought to be caused by reducing the production of the liquid within the eye. The precise mechanism of this effect is not known. The reduction in intraocular pressure reduces the risk of damage to the optic nerve and loss of vision in patients with elevated intraocular pressure due to glaucoma.
Nebivolol is a beta blocker used to treat high blood pressure and heart failure. As with other β-blockers, it is generally a less preferred treatment for high blood pressure. It may be used by itself or with other blood pressure medication. It is taken by mouth.
1,4-Dihydropyridine (DHP) is an organic compound with the formula CH2(CH=CH)2NH. The parent compound is uncommon, but derivatives of 1,4-dihydropyridine are important commercially and biologically. The pervasive cofactors NADH and NADPH are derivatives of 1,4-dihydropyridine. 1,4-Dihydropyridine-based drugs are L-type calcium channel blockers, used in the treatment of hypertension. 1,2-Dihydropyridines are also known.
Lercanidipine is an antihypertensive drug. It belongs to the dihydropyridine class of calcium channel blockers, which work by relaxing and opening the blood vessels allowing the blood to circulate more freely around the body. This lowers the blood pressure and allows the heart to work more efficiently.
Flunarizine, sold under the brand name Sibelium among others, is a drug classified as a calcium antagonist which is used for various indications. It is not available by prescription in the United States or Japan. The drug was discovered at Janssen Pharmaceutica (R14950) in 1968.
The L-type calcium channel is part of the high-voltage activated family of voltage-dependent calcium channel. "L" stands for long-lasting referring to the length of activation. This channel has four isoforms: Cav1.1, Cav1.2, Cav1.3, and Cav1.4.
Gingival enlargement is an increase in the size of the gingiva (gums). It is a common feature of gingival disease. Gingival enlargement can be caused by a number of factors, including inflammatory conditions and the side effects of certain medications. The treatment is based on the cause. A closely related term is epulis, denoting a localized tumor on the gingiva.
Manidipine is a calcium channel blocker that is used clinically as an antihypertensive.
Efonidipine (INN) is a dihydropyridine calcium channel blocker marketed by Shionogi & Co. of Japan. It was launched in 1995, under the brand name Landel (ランデル). The drug blocks both T-type and L-type calcium channels. Drug Controller General of India (DCGI) has approved the use of efonidipine in India. It is launched under the brand name "Efnocar".
Alpha-blockers, also known as α-blockers or α-adrenoreceptor antagonists, are a class of pharmacological agents that act as antagonists on α-adrenergic receptors (α-adrenoceptors).
Anipamil is a calcium channel blocker, specifically of the phenylalkylamine type. This type is separate from its more common cousin Dihydropyridine. Anipamil is an analog of the more common drug verapamil, which is the most common type of phenylalkylamine style calcium channel blocker. Anipamil has been shown to be a more effective antiarrhythmic medication than verapamil because it does not cause hypertension as seen in verapamil. It is able to do this by bonding to the myocardium tighter than verapamil.
AH-1058 is a lipophilic antiarrhythmic calcium channel blocker synthesized by the Pharmaceutical Research Laboratories of Ajinomoto Co., Inc in Kawasaki, Japan. It is derived from cyproheptadine, a compound with known antiserotonic, antihistaminic and calcium channel blocking properties. The IUPAC name of AH-1058 is: 4-(5H-dibenzo[a,d]cyclohepten-5-ylidene)-1-[E-3-(3-methoxy-2-nitro) phenyl-2-propenyl]piperidine hydrochloride.
Lomerizine (INN) is a diphenylpiperazine class L-type and T-type calcium channel blocker. This drug is currently used clinically for the treatment of migraines, while also being used experimentally for the treatment of glaucoma and optic nerve injury.
The Hantzsch pyridine synthesis or Hantzsch dihydropyridine synthesis is a multi-component organic reaction between an aldehyde such as formaldehyde, 2 equivalents of a β-keto ester such as ethyl acetoacetate and a nitrogen donor such as ammonium acetate or ammonia. The initial reaction product is a dihydropyridine which can be oxidized in a subsequent step to a pyridine. The driving force for this second reaction step is aromatization. This reaction was reported in 1881 by Arthur Rudolf Hantzsch.