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Nifedipine
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| Systematic (IUPAC) name | |
| dimethyl2,6-dimethyl-4-(2-nitrophenyl)- 1,4-dihydropyridine-3,5-dicarboxylate | |
| Identifiers | |
| CAS number | |
| ATC code | C08 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C17H18N2O6 |
| Mol. mass | 346. IUPAC Nomenclature is a system of naming Chemical compounds and of describing the science of Chemistry in general CAS registry numbers are unique numerical identifiers for Chemical compounds Polymers biological sequences mixtures and Alloys They are also referred to The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs It is controlled by the WHO Collaborating Centre for Drug A section of the Anatomical Therapeutic Chemical Classification System. PubChem is a Database of chemical Molecules The system is maintained by the National Center for Biotechnology Information (NCBI a component The DrugBank database available at the University of Alberta is a unique Bioinformatics and Cheminformatics resource that combines detailed drug (i A chemical formula is a way of expressing information about the Atoms that constitute a particular Chemical compound, and how the relationship between those atoms changes Carbon (kɑɹbən is a Chemical element with the symbol C and its Atomic number is 6 Hydrogen (ˈhaɪdrədʒən is the Chemical element with Atomic number 1 Nitrogen (ˈnaɪtɹəʤɪn is a Chemical element that has the symbol N and Atomic number 7 and Atomic weight 14 Oxygen (from the Greek roots ὀξύς (oxys (acid literally "sharp" from the taste of acids and -γενής (-genēs (producer literally begetteris the The molecular mass (abbreviated m of a substance, more commonly referred to as molecular weight and abbreviated as MW, is the Mass of one 335 g/mol |
| Physical data | |
| Melt. point | 173 °C (343 °F) |
| Pharmacokinetic data | |
| Bioavailability | 45-56% |
| Protein binding | 92-98% |
| Metabolism | Gastrointestinal, Hepatic |
| Half life | 2 hours |
| Excretion | Renal: >50%, Biliary: 5-15% |
| Therapeutic considerations | |
| Pregnancy cat. |
C: (USA) |
| Legal status | |
| Routes | Oral |
Nifedipine (brand name Adalat, Nifedical, and Procardia) is a dihydropyridine calcium channel blocker. The melting point of a solid is the temperature range at which it changes state from solid to Liquid. In Pharmacology, bioavailability is used to describe the fraction of an administered Dose of unchanged drug that reaches the Systemic circulation, one of A drug's efficiency may be affected by the degree to which it binds to the proteins within Blood plasma. Drug metabolism is the Metabolism of drugs, their Biochemical modification or degradation usually through specialized enzymatic systems The biological half-life of a substance is the time it takes for a substance (drug radioactive nuclide or other to lose half of its pharmacologic physiologic or radiologic activity Excretion is the process of eliminating waste products of Metabolism and other non-useful materials The pregnancy category of a pharmaceutical agent is an assessment of the risk of fetal injury due to the pharmaceutical if it is used as directed by the mother during The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction In Pharmacology and Toxicology, a route Dihydropyridine is a molecule based upon Pyridine, and the parent of a class of Molecules that have been semi- saturated with two Substituents Calcium channel blockers are a class of drugs and natural substances with effects on many excitable cells of the body like the muscle of the Heart, smooth muscles Its main uses are as an antianginal (especially in Prinzmetal's angina) and antihypertensive, although a large number of other uses have recently been found for this agent, such as Raynaud's phenomenon, premature labor, and painful spasms of the esophagus in cancer and tetanus patients. An antianginal is any drug used in the treatment of Angina pectoris, a symptom of ischaemic heart disease. Prinzmetal's angina, also known as variant angina or angina inversa, is a syndrome typically consisting of angina (cardiac chest pain at rest that occurs Antihypertensives are a class of drugs that are used in Medicine and Pharmacology to treat Hypertension (high blood pressure Raynaud's phenomenon (reɪˈnoʊz (rāy-NŌZ in Medicine, is a vasospastic disorder causing discoloration of the Fingers Toes and occasionally Premature birth (also known as preterm birth) is the Birth of a Baby before the standard period of Pregnancy is completed The esophagus or oesophagus (see American and British English spelling differences) sometimes known as the gullet, is an organ in Cancer (medical term Malignant Neoplasm) is a class of Diseases in which a group of cells display uncontrolled Tetanus is a medical condition that is characterized by a prolonged contraction of Skeletal muscle fibres It is also commonly used for the small subset of pulmonary hypertension patients whose symptoms respond to calcium channel blockers. In Medicine, pulmonary hypertension (PH is an increase in blood pressure in the Pulmonary artery, Pulmonary vein, or pulmonary capillaries together known Calcium channel blockers are a class of drugs and natural substances with effects on many excitable cells of the body like the muscle of the Heart, smooth muscles
Contents |
Dosing
Nifedipine rapidly lowers blood pressure, and patients are commonly warned they may feel dizzy or faint after taking the first few doses. Tachycardia (fast heart rate) may occur as a reaction. These problems are much less frequent in the sustained-release preparations of nifedipine (such as Adalat OROS). A more novel release system is GITS (Gastro-Intestinal Therapeutic System), which - according to Bayer - provides 24-hour continuous release through an osmotic push system. Recent trials with GITS include INSIGHT (for blood pressure)[1] and ACTION (for angina). [2]
Extended release formulations of nifedipine should be taken on an empty stomach, and patients are warned not to consume anything containing grapefruit or grapefruit juice, as they raise blood nifedipine levels. The grapefruit is a subtropical Citrus Tree grown for its Fruit which was originally named the "forbidden fruit " of Barbados There are several possible mechanisms, including the lowering of CYP3A4 activity. Cytochrome P450 3A4 (abbreviated CYP3A4) ( a member of the Cytochrome P450 mixed-function oxidase system is one of the most important enzymes involved in the metabolism [3]
It is also used to block pre-term contractions in pregnant women.
Uses
Approved uses
The approved uses for nifedipine are the long-term treatment of hypertension (high blood pressure) and angina pectoris. Hypertension, also referred to as high blood pressure, HTN or HPN, is a medical condition in which the Blood pressure is chronically elevated Angina pectoris, commonly known as angina, is severe Chest pain due to Ischemia (a lack of blood and hence Oxygen supply of the heart In hypertension, recent clinical guidelines generally favour diuretics and ACE inhibitors, although calcium channel antagonists are still favoured as primary treatment for older black patients. A diuretic is any Drug that elevates the rate of urination ( Diuresis) ACE inhibitors, or inhibitors of '''A'''ngiotensin-'''C'''onverting '''E'''nzyme, are a group of Pharmaceuticals that are used primarily in treatment of Hypertension [4]
Sublingual nifedipine has previously been used in hypertensive emergencies. A hypertensive emergency is severe Hypertension (high blood pressure with acute impairment of an Organ system (especially the Central nervous system This was found to be dangerous, and has been abandoned. [5][6]
Off-label uses
Nifedipine has been used frequently as a tocolytic (agent that delays premature labor). Tocolytics are medications used to suppress Premature labor (from the Greek tokos, Childbirth, and lytic, capable of dissolving A Cochrane review has concluded that it is comparable with magnesium sulfate and beta-agonists (such as ritodrine) with fewer side-effects. Ritodrine hydrochloride (trade name Yutopar) is a Tocolytic Drug, used to stop Premature labor. [7] Its role vis à vis atosiban is not established. Atosiban ( Tractocile or Antocin, RWJ 22164 is an inhibitor of the hormones Oxytocin and Vasopressin.
Raynaud's phenomenon is often treated with nifedipine. Raynaud's phenomenon (reɪˈnoʊz (rāy-NŌZ in Medicine, is a vasospastic disorder causing discoloration of the Fingers Toes and occasionally A 2005 meta-analysis showed modest benefits (33% decrease in attack severity, 2. 8-5 reduction in absolute number of attacks per week); it does conclude that most included studies used low doses of nifedipine. [8]
Topical nifedipine has been shown to be as effective as topical nitrates for anal fissures. In Medicine, a topical Medication is applied to body surfaces such as the Skin or Mucous membranes for example the Vagina An anal fissure is an unnatural crack or tear in the Anus skin [9]
Nifedipine is also used in high-altitude medicine to treat high altitude pulmonary edema. High altitude pulmonary edema (HAPE is a life-threatening form of non-cardiogenic Pulmonary edema that occurs in otherwise healthy Mountaineers at altitudes above [10]
History
Nifedipine (initially BAY a1040) was developed by the German pharmaceutical company Bayer, with most initial studies being performed in the early 1970s. Germany, officially the Federal Republic of Germany ( ˈbʊndəsʁepuˌbliːk ˈdɔʏtʃlant is a Country in Central Europe. For other uses see Bayer (disambiguation or Beyer or Buyer. Bayer AG (German ˈbaɪə () is a German [11]
The use of nifedipine and related calcium channel antagonists was reduced much in response to 1995 trials that mortality was increased in patients with coronary artery disease who took nifedipine. Coronary artery disease (CAD (or atherosclerotic Heart disease) is the end result of the accumulation of atheromatous plaques within the walls [12] This study was a meta-analysis, and demonstrated harm mainly in short-acting forms of nifedipine (that could cause large fluctations in blood pressure) and at high doses of 80 mg a day and more. [13]
References
- ^ Brown MJ, Palmer CR, Castaigne A, et al (2000). "Morbidity and mortality in patients randomised to double-blind treatment with a long-acting calcium-channel blocker or diuretic in the International Nifedipine GITS study: Intervention as a Goal in Hypertension Treatment (INSIGHT)". Lancet 356 (9227): 366-72. doi:. A digital object identifier ( DOI) is a permanent identifier given to an Electronic document. PMID 10972368.
- ^ Poole-Wilson PA, Kirwan BA, Vokó Z, de Brouwer S, van Dalen FJ, Lubsen J (2006). "Safety of nifedipine GITS in stable angina: the ACTION trial". Cardiovas Drugs Ther 20 (1): 45-54. doi:. A digital object identifier ( DOI) is a permanent identifier given to an Electronic document. PMID 16552473.
- ^ Odou P, Ferrari N, Barthélémy C, et al (2005). "Grapefruit juice-nifedipine interaction: possible involvement of several mechanisms". Journal Clinical Pharm Ther 30 (2): 153-8. doi:. A digital object identifier ( DOI) is a permanent identifier given to an Electronic document. PMID 15811168.
- ^ Hypertension: management of hypertension in adults in primary care. Clinical guideline CG34. National Institute for Health and Clinical Excellence (NICE), June 2006. Fulltext index. ISBN 1-86016-285-1.
- ^ Grossman E, Messerli FH, Grodzicki T, Kowey P (1996). "Should a moratorium be placed on sublingual nifedipine capsules given for hypertensive emergencies and pseudoemergencies?". JAMA 276 (16): 1328-31. doi:. A digital object identifier ( DOI) is a permanent identifier given to an Electronic document. PMID 8861992.
- ^ Varon J, Marik PE (2003). "Clinical review: the management of hypertensive crises". Critical care (London, England) 7 (5): 374-84. doi:. A digital object identifier ( DOI) is a permanent identifier given to an Electronic document. PMID 12974970.
- ^ King JF, Flenady VJ, Papatsonis DN, Dekker GA, Carbonne B (2003). "Calcium channel blockers for inhibiting preterm labour". Cochrane database of systematic reviews (Online) (1): CD002255. doi:. A digital object identifier ( DOI) is a permanent identifier given to an Electronic document. PMID 12535434.
- ^ Thompson AE, Pope JE (2005). "Calcium channel blockers for primary Raynaud's phenomenon: a meta-analysis". Rheumatology (Oxford, England) 44 (2): 145-50. doi:. A digital object identifier ( DOI) is a permanent identifier given to an Electronic document. PMID 15546967.
- ^ Ezri T, Susmallian S (2003). "Topical nifedipine vs. topical glyceryl trinitrate for treatment of chronic anal fissure". Dis. Colon Rectum 46 (6): 805-8. doi:. A digital object identifier ( DOI) is a permanent identifier given to an Electronic document. PMID 12794583.
- ^ Ali, Mir Omar and Qazi, Samia (2007-09-19). Year 2007 ( MMVII) was a Common year starting on Monday of the Gregorian calendar in the 21st century. Events 335 - Dalmatius is raised to the rank of Caesar by his uncle Constantine I. Pulmonary Edema, High-Altitude. eMedicine. Retrieved on 2007-11-25. Year 2007 ( MMVII) was a Common year starting on Monday of the Gregorian calendar in the 21st century. Events 1034 - Máel Coluim mac Cináeda, King of Scots dies Donnchad, the
- ^ Vater W, Kroneberg G, Hoffmeister F, et al (1972). "[Pharmacology of 4-(2'-nitrophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid dimethyl ester (Nifedipine, BAY a 1040)]" (in German). Arzneimittel-Forschung 22 (1): 1-14. PMID 4622472.
- ^ Furberg CD, Psaty BM, Meyer JV (1995). "Nifedipine. Dose-related increase in mortality in patients with coronary heart disease". Circulation 92 (5): 1326-31. PMID 7648682.
- ^ Opie LH, Messerli FH (1995). "Nifedipine and mortality. Grave defects in the dossier". Circulation 92 (5): 1068-73. PMID 7648646.
External links
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