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amlodipine (Norvasc, Amlocard, Amvaz)
Tradename: Norvasc.
Indications:
- hypertension
- prinzmetal angina [5]
- angina pectoris & prophylaxis for angina pectoris [5]
Contraindications:
-> NOT for use in controlling ventricular response to atrial fibrillation
a) does NOT block AV nodal conduction
Dosage: start 2.5 to 5 mg PO QD, max 10 mg QD.
Tabs: 2.5, 5, 10 mg.
Pharmacokinetics:
-> metabolized in the liver by cyt P450 3A4
Adverse effects:
1) headache & edema are most common
2) GI: nausea, anorexia, constipation, dyspepsia
3) others: palpitations, flushing, dizziness
* less likely to cause orthostasis than diuretics []
Drug interactions:
1) fentanyl: severe hypotension may occur
2) any drug that inhibits cyt P450 3A4 may increase levels of amlodipine
3) any drug that induces cyt P450 3A4 may diminish levels of amlodipine
4) doses of simvastatin or lovastatin > 20 mg QD not recommended [6]
- no evidence of significant interaction with atorvastatin, rosuvastatin, pravastatin, fluvastatin, or pitavastatin [6]
Laboratory:
- amlodipine in hair
- amlodipine in body fluid
- amlodipine in blood
- amlodipine in serum/plasma
- amlodipine in urine
Mechanism of action:
1) inhibits L-type calcium channels
2) angiotensin II receptor type 2 & 4-stimulating antihypertensive
3) dilation of coronary arteries & arterioles
4) increased myocardial oxygen delivery
5) decreased systemic vascular resistance
6) increased cardiac output
7) does not alter AV nodal conduction
8) does not alter myocardial contractility
9) not a negative cardiac inotrope
10) no reflex tachycardia
Interactions
drug interactions
drug adverse effects (more general classes)
Related
African American Study of Kidney Disease & Hypertension (AASK)
ASCOT clinical trial
cytochrome P450 3A4 (cytochrome P450 C3, nifedipine oxidase, P450-PCN1, NF-25, CYP3A4)
VALUE trial
Specific
levamlodipine; S-amlodipine (Conjupri)
General
calcium channel blocker (CCB)
dihydropyridine
Properties
MISC-INFO: elimination route LIVER
pregnancy-category C
safety in lactation ?
Database Correlations
PUBCHEM correlations
References
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- Drug Information & Medication Formulary, Veterans Affairs,
Central California Health Care System, 1st ed., Ravnan et al
eds, 1998 - non formulary drug request
- Department of Veterans Affairs, VA National Formulary
- Medical Knowledge Self Assessment Program (MKSAP) 16, 18.
American College of Physicians, Philadelphia 2012, 2018.
- Deprecated Reference
- Wiggins BS, Saseen JJ, Page RL 2nd et al
Recommendations for Management of Clinically Significant
Drug-Drug Interactions With Statins and Select Agents Used
in Patients With Cardiovascular Disease. A Scientific
Statement From the American Heart Association.
Circulation. 2016;134:00-00
PMID: 27754879
http://circ.ahajournals.org/content/circulationaha/early/2016/10/17/CIR.0000000000000456.full.pdf
- Geriatric Review Syllabus, 10th edition (GRS10)
Harper GM, Lyons WL, Potter JF (eds)
American Geriatrics Society, 2019
Component-of
aliskiren/amlodipine (Tekamlo)
aliskiren/amlodipine/hydrochlorothiazide (Amturnide)
amlodipine/atorvastatin (Caduet)
amlodipine/benazepril (Lotrel)
amlodipine/celecoxib (Consensi)
amlodipine/hydrochlorothiazide/olmesartan (Tribenzor)
amlodipine/hydrochlorothiazide/valsartan
amlodipine/indapamide/telmisartan
amlodipine/olmesartan (Azor)
amlodipine/perindopril
amlodipine/telmisartan (Twynsta)
amlodipine/valsartan (Exforge)