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Pronunciation

amLODIPine: am-LOE-di-peen

diltiazem: dil-TYE-a-zem

felodipine: fe-LOE-di-peen

isradipine: is-RA-di-peen

niCARdipine: nye-KAR-di-peen

NIFEdipine: nye-FED-i-peen

niMODipine: nye-MOE-di-peen

nisoldipine: nye-SOLE-di-peen

verapamil: ver-AP-a-mil

Classifications

Therapeutic Classification: antianginals, antiarrhythmics, antihypertensives

Indications

REMS


Nimodipine

Action

  • Inhibits the transport of calcium into myocardial and vascular smooth muscle cells, resulting in inhibition of excitation-contraction coupling and subsequent contraction.
Diltiazem, verapamil
  • Decrease SA and AV conduction and prolong AV node refractory period in conduction tissue.
Therapeutic effects:
  • Systemic vasodilation resulting in decreased BP.
  • Coronary vasodilation resulting in decreased frequency and severity of attacks of angina.
Nimodipine
  • Prevention of vascular spasm after subarachnoid hemorrhage, resulting in decreased neurologic impairment.
Diltiazem, verapamil

Pharmacokinetics

Absorption: Amlodipine: Well absorbed after oral administration (64–90%); Diltiazem and verapamil: Well absorbed after oral administration but rapidly metabolized; Felodipine, isradipine, nicardipine, nimodipine, and nisoldipine: Well absorbed after oral administration but extensively metabolized, resulting in bioavailability; Nifedipine: Well absorbed after oral administration but rapidly metabolized, resulting in bioavailability (45–70%); bioavailability is (80%) with extended-release forms.

Distribution: Amlodipine, diltiazem, isradipine, nicardipine, verapamil: Well distributed to tissues; nimodipine: Crosses the blood-brain barrier.

Metabolism/Excretion: All agents are mostly metabolized by the liver; 10% excreted unchanged by kidneys.

Half-Life: Amlodipine: 30–50 hr; diltiazem: 3.5–9 hr; felodipine: 11–16 hr; isradipine: 8 hr; nicardipine: 2–4 hr; nifedipine: 2–5 hr; nimodipine: 1–2 hr; verapamil: 4.5–12 hr.

Time/Action Profile

( cardiovascular effects)

ROUTEONSETPEAKDURATION
Amlodipine POunknown6–924 hr
Diltiazem PO30 min2–3 hr6–8 hr
Diltiazem PO-CDunknown14 days24 hr
Diltiazem PO-XRunknown14 days24 hr
Diltiazem IV2–5 minunknownunknown
Felodipine PO1 hr2–4 hrup to 24 hr
Isradipine PO<2 hr2–3 hr12 hr
Nicardipine PO20 min1–2 hr8 hr
Nicardipine IVwithin min45 min50 hr
Nifedipine PO20 minunknown6–8 hr
Nifedipine PO-ERunknownunknown24 hr
Nimodipine POunknown1 hrunknown
Nisoldipineunknown6–12 hr24 hr
Verapamil PO1–2 hr30–90 min3–7 hr
Verapamil PO-ERunknown5–7 hr24 hr
Verapamil IV1–5 min3–5 min2 hr

Maximum antihypertensive effect with chronic therapy.

After discontinuation.

Single dose; effects from multiple doses may not be evident for 24–48 hr.

Antiarrhythmic effects; hemodynamic effects begin 3–5 min after injection and persist for 10–20 min.

Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

CV: peripheral edema (with amlodipine, felodipine, nifedipine), ARRHYTHMIAS, HF, bradycardia, chest pain, hypotension, palpitations, syncope, tachycardia

Derm: sweating, dermatitis, erythema multiforme, flushing (with nifedipine, nicardipine), photosensitivity, pruritus/urticaria, rash, STEVENS-JOHNSON SYNDROME (SJS)

EENT: blurred vision, disturbed equilibrium, epistaxis, tinnitus

Endo: gynecomastia, hyperglycemia

GI: liver enzymes, anorexia, constipation, diarrhea, dry mouth, dyspepsia, GI obstruction (with nifedipine), gingival hyperplasia, nausea, ulcer (with nifedipine), vomiting

GU: dysuria, nocturia, polyuria, sexual dysfunction, urinary frequency

Hemat: anemia, leukopenia, thrombocytopenia

Metab: weight gain

MS: joint stiffness, muscle cramps

Neuro: abnormal dreams, anxiety, confusion, dizziness, drowsiness, dysgeusia, headache(with nifedipine, isradipine, felodipine), nervousness, paresthesia, psychiatric disturbances, tremor, weakness

Resp: cough, dyspnea

Interactions

Drug-drug:

Drug-Natural Products:

Drug-Food:

Route/Dosage

Amlodipine

Hepatic Impairment

Diltiazem

Felodipine

Isradipine

Nicardipine

Nifedipine

Nimodipine

Nisoldipine

Verapamil

Availability

Amlodipine

(Generic available)

Diltiazem

(Generic available)

Felodipine

(Generic available)

Isradipine

(Generic available)

Nicardipine

(Generic available)

Nifedipine

(Generic available)

Nimodipine

(Generic available)

Nisoldipine

(Generic available)

Verapamil

(Generic available)

Assessment

Lab Test Considerations:

Implementation

Nifedipine

Nimodipine

IV Administration:

Diltiazem

Nicardipine

Verapamil

Patient/Family Teaching

Evaluation/Desired Outcomes

US Brand Names

amLODIPine: Katerzia, Norliqva, Norvasc,

diltiazem: Cardizem, Cardizem CD, Cardizem LA, Cartia XT, Taztia XT, Tiazac,

isradipine: DynaCirc,

niCARdipine: Cardene IV,

NIFEdipine: Adalat CC, Afeditab CR, Procardia, Procardia XL,

niMODipine: Nymalize,

nisoldipine: Sular,

verapamil: Calan, Calan SR, Verelan, Verelan PM

Canadian Brand Names

diltiazem: Tiazac XC,

felodipine: Plendil,

NIFEdipine: Adalat XL,

niMODipine: Nimotop