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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, they are relatively vascular selective in their mechanism of action in lowering blood pressure. [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, analgaesic, pain reliever, or painkiller, is any member of the group of drugs used to achieve relief from pain. 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.
Amlodipine, sold under the brand name Norvasc among others, is a calcium channel blocker medication used to treat high blood pressure and coronary artery disease. It is taken by mouth.
Diltiazem, sold under the brand name Cardizem among others, is a 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. 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.
Vanoxerine is a piperazine derivative which is a potent and selective dopamine reuptake inhibitor (DRI). Vanoxerine binds to the target site on the dopamine transporter (DAT) ~ 50 times more strongly than cocaine, but simultaneously inhibits the release of dopamine. This combined effect only slightly elevates dopamine levels, giving vanoxerine only mild stimulant effects. Vanoxerine has also been observed to be a potent blocker of the IKr (hERG) channel. Vanoxerine also binds with nanomolar affinity to the serotonin transporter.
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.
Nitrendipine is a dihydropyridine calcium channel blocker. It is used in the treatment of primary (essential) hypertension to decrease blood pressure and can reduce the cardiotoxicity of cocaine.
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.
An adrenergic antagonist is a drug that inhibits the function of adrenergic receptors. There are five adrenergic receptors, which are divided into two groups. The first group of receptors are the beta (β) adrenergic receptors. There are β1, β2, and β3 receptors. The second group contains the alpha (α) adrenoreceptors. There are only α1 and α2 receptors. Adrenergic receptors are located near the heart, kidneys, lungs, and gastrointestinal tract. There are also α-adreno receptors that are located on vascular smooth muscle.
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 "Efonta" & 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.
Forasartan, otherwise known as the compound SC-52458, is a nonpeptide angiotensin II receptor antagonist (ARB, AT1 receptor blocker).
LY-215,840 is an ergoline derivative drug developed by Eli Lilly, which acts as a potent and selective antagonist at the serotonin 5-HT2 and 5-HT7 receptors. It has anti-hypertensive and muscle relaxant effects in animal studies.
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.
Alison Marion Gurney is professor of Pharmacology at the University of Manchester. She previously held the W.C. Bowman Chair of Pharmacology at the University of Strathclyde, where she was the first female appointed to a science professorship and the first female Professor of Pharmacology in Scotland. She is known for her research into the pharmacology and physiological roles of ion channels, especially in the pulmonary circulation.