II. Mechanism
- Dihydropyridine Calcium Channel Blockers
- Nifedipine (Procardia) is prototype for class
III. Contraindications
- Avoid in Diabetes Mellitus (may increase Proteinuria)
IV. Drug Interactions
-
Clarithromycin
- Increases Calcium Channel Blocker levels via CYP3A4 inhibition especially with Dihydropyridines and over age 65 years
- Provokes Hypotension and Bradycardia
- Risk of Acute Kidney Injury (often requiring hospitalization)
- References
- Increases Calcium Channel Blocker levels via CYP3A4 inhibition especially with Dihydropyridines and over age 65 years
V. Preparations
- Nifedipine (Procardia)
- Amlodipine (Norvasc)
- Dosing
- 2.5-5mg PO qd (MAX 10mg qd)
- Advantages
- Does not exacerbate Left Ventricular Dysfunction
- Dosing
- Clevidipine
- Felodipine
-
Nicardipine
- Counters Cerebral Vessel spasm (e.g. early Subarachnoid Hemorrhage, CVA)
- Nimodipine
- Counters Cerebral Vessel spasm (e.g. early Subarachnoid Hemorrhage, CVA)
VI. Adverse Effects: Peripheral Edema (Norvasc)
- Occurs more commonly in women
- Occurs more commonly on Norvasc doses >5 mg
- Adding ACE Inhibitor to regimen decreases edema
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| amlodipine (on 5/17/2017 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| AMLODIPINE BESYLATE 10 MG TAB | Generic | $0.02 each |
| AMLODIPINE BESYLATE 2.5 MG TAB | Generic | $0.02 each |
| AMLODIPINE BESYLATE 5 MG TAB | Generic | $0.02 each |
| AMLODIPINE-ATORVAST 10-10 MG | Generic | $4.38 each |
| AMLODIPINE-ATORVAST 10-20 MG | Generic | $4.45 each |
| AMLODIPINE-ATORVAST 10-40 MG | Generic | $5.66 each |
| AMLODIPINE-ATORVAST 10-80 MG | Generic | $5.25 each |
| AMLODIPINE-ATORVAST 5-10 MG | Generic | $4.03 each |
| AMLODIPINE-ATORVAST 5-20 MG | Generic | $4.14 each |
| AMLODIPINE-ATORVAST 5-40 MG | Generic | $5.37 each |
| AMLODIPINE-BENAZEPRIL 10-20 MG | Generic | $0.23 each |
| AMLODIPINE-BENAZEPRIL 10-40 MG | Generic | $0.26 each |
| AMLODIPINE-BENAZEPRIL 2.5-10 | Generic | $0.39 each |
| AMLODIPINE-BENAZEPRIL 5-10 MG | Generic | $0.27 each |
| AMLODIPINE-BENAZEPRIL 5-20 MG | Generic | $0.20 each |
| AMLODIPINE-BENAZEPRIL 5-40 MG | Generic | $0.24 each |
| AMLODIPINE-OLMESARTAN 10-20 MG | Generic | $0.88 each |
| AMLODIPINE-OLMESARTAN 10-40 MG | Generic | $1.09 each |
| AMLODIPINE-OLMESARTAN 5-20 MG | Generic | $0.91 each |
| AMLODIPINE-OLMESARTAN 5-40 MG | Generic | $1.09 each |
| AMLODIPINE-VALSARTAN 10-160 MG | Generic | $0.61 each |
| AMLODIPINE-VALSARTAN 10-320 MG | Generic | $0.63 each |
| AMLODIPINE-VALSARTAN 5-160 MG | Generic | $0.40 each |
| AMLODIPINE-VALSARTAN 5-320 MG | Generic | $0.62 each |
| AMLODIPINE-VALSARTAN-HYDROCHLOROTHIAZIDE 10-160-12.5 MG TAB | Generic | $2.54 each |
| AMLODIPINE-VALSARTAN-HYDROCHLOROTHIAZIDE 10-160-25 MG TAB | Generic | $3.20 each |
| AMLODIPINE-VALSARTAN-HYDROCHLOROTHIAZIDE 10-320-25 MG TAB | Generic | $3.05 each |
| AMLODIPINE-VALSARTAN-HYDROCHLOROTHIAZIDE 5-160-12.5 MG TAB | Generic | $1.94 each |
| AMLODIPINE-VALSARTAN-HYDROCHLOROTHIAZIDE 5-160-25 MG TAB | Generic | $2.93 each |
| norvasc (on 6/1/2017 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| NORVASC 10 MG TABLET | Generic | $0.02 each |
| NORVASC 2.5 MG TABLET | Generic | $0.02 each |
| NORVASC 5 MG TABLET | Generic | $0.02 each |
Ontology: Dihydropyridines (C0012315)
| Definition (MSH) | Pyridine moieties which are partially saturated by the addition of two hydrogen atoms in any position. |
| Concepts | Organic Chemical (T109) , Pharmacologic Substance (T121) |
| MSH | D004095 |
| English | Dihydropyridines, Dihydropyridine, Dihydropyridines [Chemical/Ingredient], dihydropyridines, dihydropyridine |
| Swedish | Dihydropyridiner |
| Czech | dihydropyridiny |
| Finnish | Dihydropyridiinit |
| Russian | DIGIDROPIRIDINY, ДИГИДРОПИРИДИНЫ |
| Japanese | ジヒドロピリジン |
| Croatian | Not Translated[Dihydropyridines] |
| Polish | Dihydropirydyny pochodne |
| Portuguese | Di-Hidropiridinas |
| French | Dihydropyridines |
| German | Dihydropyridine |
| Italian | Diidropiridine |
| Spanish | Dihidropiridinas |
Ontology: Nimodipine (C0028094)
| Definition (NCI_NCI-GLOSS) | Belongs to a family of drugs called calcium channel blockers. It is being investigated for use with anticancer drugs to prevent or overcome drug resistance and improve response to chemotherapy. |
| Definition (NCI) | A dihydropyridine derivative and an analogue of the calcium channel blocker nifedipine, with antihypertensive activity. Nimodipine inhibits the transmembrane influx of calcium ions in response to depolarization in smooth muscle cells, thereby inhibiting vascular smooth muscle contraction and inducing vasodilatation. Nimodipine has a greater effect on cerebral arteries than on peripheral smooth muscle cells and myocardial cells, probably because this agent can cross the blood brain barrier due to its lipophilic nature. Furthermore, this agent also inhibits the drug efflux pump P-glycoprotein, which is overexpressed in some multi-drug resistant tumors, and may improve the efficacy of some antineoplastic agents. |
| Definition (MSH) | A calcium channel blockader with preferential cerebrovascular activity. It has marked cerebrovascular dilating effects and lowers blood pressure. |
| Definition (CSP) | 1,4 dihydropyridine; centrally acting calcium channel blocker used in the treatment of a wide range of disorders, including drug withdrawal, AIDS motor/cognitive disorder, and post cardiac surgery recovery. |
| Definition (PDQ) | A dihydropyridine derivative and an analogue of the calcium channel blocker nifedipine, with antihypertensive activity. Nimodipine inhibits the transmembrane influx of calcium ions in response to depolarization in smooth muscle cells, thereby inhibiting vascular smooth muscle contraction and inducing vasodilatation. Nimodipine has a greater effect on cerebral arteries than on peripheral smooth muscle cells and myocardial cells, probably because this agent can cross the blood brain barrier due to its lipophilic nature. Furthermore, this agent also inhibits the drug efflux pump P-glycoprotein, which is overexpressed in some multi-drug resistant tumors, and may improve the efficacy of some antineoplastic agents. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=41210&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=41210&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C692" NCI Thesaurus) |
| Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| MSH | D009553 |
| SnomedCT | 387502003, 87285001 |
| English | Nimodipine, 3,5-Pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-, 2-methoxyethyl 1-methylethyl ester, NIMO, nimodipine, nimodipine (medication), NIMODIPINE, Nimodipine [Chemical/Ingredient], niMODipine, NiMODipine, Nimodipine (product), Nimodipine (substance) |
| Swedish | Nimodipin |
| Czech | nimodipin |
| Finnish | Nimodipiini |
| Russian | NIMODIPIN, НИМОДИПИН |
| Japanese | ニモジピン |
| Spanish | nimodipina, nimodipino, nimodipino (producto), nimodipino (sustancia), nimodipina (producto), nimodipina (sustancia), Nimodipino |
| Polish | Nimodypina |
| French | Nimodipine |
| German | Nimodipin |
| Italian | Nimodipina |
| Portuguese | Nimodipino |
Ontology: Amlodipine (C0051696)
| Definition (MSH) | A long-acting dihydropyridine calcium channel blocker. It is effective in the treatment of ANGINA PECTORIS and HYPERTENSION. |
| Definition (CHV) | a drug used to treat high blood pressure and chest pain (angina) |
| Definition (NCI) | A synthetic dihydropyridine and a calcium channel blocker with antihypertensive and antianginal properties. Amlodipine inhibits the influx of extracellular calcium ions into myocardial and peripheral vascular smooth muscle cells, thereby preventing vascular and myocardial contraction. This results in a dilatation of the main coronary and systemic arteries, decreased myocardial contractility, increased blood flow and oxygen delivery to the myocardial tissue, and decreased total peripheral resistance. This agent may also modulate multi-drug response (MDR) activity through inhibition of the p-glycoprotein efflux pump. |
| Definition (CSP) | long-acting dihydropyridine calcium channel blocker; it is effective in the treatment of angina pectoris and hypertension. |
| Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| MSH | D017311 |
| SnomedCT | 391763001, 108537001, 386864001 |
| LNC | LP28516-0, MTHU013162 |
| English | Amlodipine, 3,5-Pyridinedicarboxylic acid, 2-((2-aminoethoxy)methyl)-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-, 3-ethyl 5-methyl ester, AMLODIPINE, Amlodipine [Chemical/Ingredient], amLODIPine, Amlodipine - chemical, Amlodipine - chemical (substance), amlodipine, Amlodipine (product), Amlodipine (substance) |
| Swedish | Amlodipin |
| Czech | amlodipin |
| Finnish | Amlodipiini |
| Russian | AMLODIPIN, АМЛОДИПИН |
| Japanese | アムロジピン |
| Spanish | amlodipino, amlodipino (sustancia), amlodipina, amlodipino (producto), amlodipina (producto), amlodipina (sustancia), Amlodipino |
| Croatian | AMLODIPIN |
| Polish | Amlodypina |
| French | Amlodipine |
| German | Amlodipin |
| Italian | Amlodipina |
| Portuguese | Amlodipino |
Ontology: Norvasc (C0162712)
| Definition (CHV) | brand name of a hypertension drug |
| Definition (CHV) | brand name of a hypertension drug |
| Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| MSH | D017311 |
| English | istin, norvasc [brand name], norvasc, Istin, Mack Brand of Amlodipine Besilate, Pfizer Brand of Amlodipine Besilate, Amlor, Norvasc |
