Calcium Channel Blockers
Calcium Channel Blockers
Calcium Channel Blockers
BROWSE TOPICS
Home
Abbrev
Website News
Calculators
Internal Medicine
Dilutions
Popular Links
Drugs
I.Dx.
Research/Reference
Medical
NEWs
Oncology
bepridil (Vascor):
clevidipine -Cleviprex :
diltiazem (Cardizem ):
felodipine (Plendil):
isradipine (Dynacirc):
nicardipine (cardene):
nifedipine (Procardia):
Nimodipine
nisoldipine (Sular):
verapamil (Isoptin )
--
Medical Links
Renal
General Links
RX List
Search
Career Center
MORE
Please see package insert for additional information and possible updates. The authors make no claims
of the accuracy of the information contained herein; and these suggested doses are not a substitute for clinical
judgment. Neither GlobalRPh Inc. nor any other party involved in the preparation of this program shall be liable
for any special, consequential, or exemplary damages resulting in whole or part from any user's use of or
reliance upon this material. PLEASE READ THE DISCLAIMER CAREFULLY BEFORE ACCESSING OR
USING THIS SITE. BY ACCESSING OR USING THIS SITE, YOU AGREE TO BE BOUND BY THE TERMS
AND CONDITIONS SET FORTH IN THE DISCLAIMER. [ Read the disclaimer | <<Back ]
amlodipine (Norvasc):
Adult (usual) Angina: 5-10 mg po qd.
Hypertension initial: 5 mg po qd; maintenance 5-10 mg po qd.
FDA labeled indications: Angina, stable or unstable; Hypertension. Small, fragile, or elderly individuals,
or patients with hepatic insufficiency may be started on 2.5 mg once daily and this dose may be used
when adding Norvasc to other antihypertensive therapy.
Titration: In general, titration should proceed over 7 to 14 days so that the physician can fully assess
the patient's response to each dose level.
[Supplied: 2.5, 5, 10mg tab]
Studies in Patients with Congestive Heart Failure:
Study: (PRAISE-2) randomized patients with NYHA class III
(80%) or IV (20%) heart failure without clinical symptoms or
objective evidence of underlying ischemic disease, on
stable doses of ACE inhibitor (99%), digitalis (99%) and
diuretics (99%), to placebo (n=827) or NORVASC (n=827)
and followed them for a mean of 33 months. There was no
statistically significant difference between NORVASC and
placebo in the primary endpoint of all cause mortality (95%
confidence limits from 8% reduction to 29% increase on
NORVASC). With NORVASC there were more reports of
pulmonary edema.
bepridil (Vascor):
Dosing: Adults: Oral: Initial: 200 mg/day, then adjust dose at 10-day intervals until optimal response is
achieved; usual dose: 300 mg/day; maximum daily dose: 400 mg
Dosage adjustment in renal impairment: Risk of toxic reactions is greater in patients with renal
impairment; dose selection should be cautious, usually starting at the low end of the dosage range
Elderly: Peak concentrations and half-life are markedly increased in the elderly (>74 years); dose
selection should be cautious, usually starting at the low end of the dosage range
Supplied
Tablet, as hydrochloride: 200 mg, 300 mg
clevidipine -Cleviprex
INDICATIONS AND USAGE
Cleviprex is a dihydropyridine calcium channel blocker indicated for the reduction of blood pressure
when oral therapy is not feasible or not desirable.
DRUG INTERACTIONS
At clinically relevant concentrations, clevidipine and its metabolites do not inhibit or induce any
CYP450 enzymes. The potential of clevidipine to interact with other drugs is low
USE IN SPECIFIC POPULATIONS
Pediatric use: Safety and effectiveness of Cleviprex in children under 18 years of age have not been
established.
DOSAGE AND ADMINISTRATION
For intravenous use: Cleviprex is intended for intravenous use. Titrate Cleviprex to achieve the
desired blood pressure reduction. Individualize dosage depending on the blood pressure response of
Advertisement
G H
M N
Q R
V W X
Z
MORE
Advertisement
G H
M N
Q R
V W X
Z
MORE
Dose
(mL/hour)
12
16
10
20
12
24
14
28
16
32
18
36
20
40
22
44
24
48
26
52
28
56
30
60
32
64
Advertisement
(at least 50% of peak response) of more than 12 hours following administration of the highest dose.
DynaCirc (isradipine) has been shown in controlled, double-blind clinical trials to be an effective
antihypertensive agent when used as monotherapy, or when added to therapy with thiazide-type
diuretics. During chronic administration, divided doses (b.i.d.) in the range of 5-20 mg daily have been
shown to be effective, with response at trough (prior to next dose) over 50% of the peak blood
pressure effect. The response is dose-related between 5-10 mg daily. DynaCirc (isradipine) is equally
effective in reducing supine, sitting, and standing blood pressure.
On chronic administration, increases in resting pulse rate averaged about 3-5 beats/min. These
increases were not dose-related.
Dosing: Hypertension:
Oral: Adults: 2.5 mg twice daily; antihypertensive response occurs in 2-3 hours; maximal response in
2-4 weeks; increase dose at 2- to 4-week intervals at 2.5-5 mg increments; usual dose range (JNC 7):
2.5-10 mg/day in 2 divided doses. Note: Most patients show no improvement with doses >10 mg/day
except adverse reaction rate increases; therefore, maximal dose in older adults should be 10 mg/day.
Supplied
Capsule (DynaCirc): 2.5 mg, 5 mg
Tablet, controlled release (DynaCirc CR): 5 mg, 10 mg
nicardipine (cardene):
Clinical Pharmacology- MECHANISM OF ACTION
Nicardipine inhibits the transmembrane influx of calcium ions into cardiac muscle and smooth muscle
without changing serum calcium concentrations. The contractile processes of cardiac muscle and
vascular smooth muscle are dependent upon the movement of extracellular calcium ions into these
cells through specific ion channels. The effects of nicardipine are more selective to vascular smooth
muscle than cardiac muscle. In animal models, nicardipine produced relaxation of coronary vascular
smooth muscle at drug levels which cause little or no negative inotropic effect
Dosage Adults:
Oral:
Immediate release: Initial: 20 mg 3 times/day; usual: 20-40 mg 3 times/day (allow 3 days between
dose increases).
Sustained release: Initial: 30 mg twice daily, titrate up to 60 mg twice daily.
Note: The total daily dose of immediate-release product may not automatically be equivalent to the
daily sustained-release dose; use caution in converting.
I.V. (dilute to 0.1 mg/mL):
Acute hypertension: Initial: 5 mg/hour increased by 2.5 mg/hour every 15 minutes to a maximum of
15 mg/hour; consider reduction to 3 mg/hour after response is achieved. Monitor and titrate to lowest
dose necessary to maintain stable blood pressure.
Substitution for oral therapy (approximate equivalents):
20 mg every 8 hours oral, equivalent to 0.5 mg/hour I.V. infusion
30 mg every 8 hours oral, equivalent to 1.2 mg/hour I.V. infusion
40 mg every 8 hours oral, equivalent to 2.2 mg/hour I.V. infusion
Dosing adjustment in renal impairment: Titrate dose beginning with 20 mg 3 times/day (immediate
release) or 30 mg twice daily (sustained release). Specific guidelines for adjustment of I.V. nicardipine
are not available, but careful monitoring/adjustment is warranted.
Dosing adjustment in hepatic impairment: Starting dose: 20 mg twice daily (immediate release) with
titration. Specific guidelines for adjustment of I.V. nicardipine are not available, but careful
monitoring/adjustment is warranted.
Supplied
Capsule (Cardene): 20 mg, 30 mg
Capsule, sustained release (Cardene SR): 30 mg, 45 mg, 60 mg
Injection, solution (Cardene IV): 2.5 mg/mL (10 mL)
nifedipine (Procardia):
WARNING
The use of sublingual short-acting nifedipine in
hypertensive emergencies and pseudoemergencies is
neither safe nor effective and SHOULD BE ABANDONED!
Serious adverse events (cerebrovascular ischemia,
syncope, heart block, stroke, sinus arrest, severe
hypotension, acute myocardial infarction, ECG changes,
and fetal distress) have been reported in relation to such
use.
CLINICAL PHARMACOLOGY
Nifedipine is a calcium ion influx inhibitor (slow-channel blocker or calcium ion antagonist) which
inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle.
The contractile processes of vascular smooth muscle and cardiac muscle are dependent upon the
movement of extracellular calcium ions into these cells through specific ion channels. Nifedipine
selectively inhibits calcium ion influx across the cell membrane of vascular smooth muscle and cardiac
muscle without altering serum calcium concentrations.
Mechanism of Action:
The mechanism by which nifedipine reduces arterial blood pressure involves peripheral arterial
vasodilatation and, consequently, a reduction in peripheral vascular resistance. The increased
peripheral vascular resistance that is an underlying cause of hypertension results from an increase in
active tension in the vascular smooth muscle. Studies have demonstrated that the increase in active
tension reflects an increase in cytosolic free calcium.
Nifedipine is a peripheral arterial vasodilator which acts directly on vascular smooth muscle. The
binding of nifedipine to voltage-dependent and possibly receptor-operated channels in vascular smooth
muscle results in an inhibition of calcium influx through these channels. Stores of intracellular calcium
in vascular smooth muscle are limited and thus dependent upon the influx of extracellular calcium for
contraction to occur. The reduction in calcium influx by nifedipine causes arterial vasodilation and
decreased peripheral vascular resistance which results in reduced arterial blood pressure.
Dosing: Oral:
Adolescents and Adults: ( Note: When switching from immediate release to sustained release
formulations, total daily dose will start the same)
Initial: 30 mg once daily as sustained release formulation, or if indicated, 10 mg 3 times/day as
capsules
Usual dose: 10-30 mg 3 times/day as capsules or 30-60 mg once daily as sustained release
Maximum dose: 120-180 mg/day
Increase sustained release at 7- to 14-day intervals
Dosing adjustment in hepatic impairment: Reduce oral dose by 50% to 60% in patients with
cirrhosis.
Supplied
Capsule, liquid-filled: 10 mg, 20 mg
Tablet, extended release: 30 mg, 60 mg, 90 mg
Adalat CC, Nifediac CC, Procardia XL: 30 mg, 60 mg, 90 mg
Afeditab, Nifedical XL: 30 mg, 60 mg
Nimodipine
Drug UPDATES: Nimodipine capsule
[Drug information / PDF]
Dosing: Click (+) next to Dosage and Administration section (drug info link)
Initial U.S. Approval: 2013
Mechanism of Action:
Nimodipine is a calcium channel blocker. The contractile processes of smooth muscle cells are
dependent upon calcium ions, which enter these cells during depolarization as slow ionic
transmembrane currents. Nimodipine inhibits calcium ion transfer into these cells and thus inhibits
contractions of vascular smooth muscle. In animal experiments, nimodipine had a greater effect on
cerebral arteries than on arteries elsewhere in the body perhaps because it is highly lipophilic, allowing
it to cross the blood-brain barrier; concentrations of nimodipine as high as 12.5 ng/mL have been
detected in the cerebrospinal fluid of nimodipine-treated subarachnoid hemorrhage (SAH) patients.
The precise mechanism of action of nimodipine in humans is unknown. Although the clinical studies
described below demonstrate a favorable effect of nimodipine on the severity of neurological deficits
caused by cerebral vasospasm following SAH, there is no arteriographic evidence that the drug either
prevents or relieves the spasm of these arteries. However, whether or not the arteriographic
methodology utilized was adequate to detect a clinically meaningful effect, if any, on vasospasm is
unknown.
INDICATIONS AND USAGE: Nimodipine is indicated for the improvement of neurological outcome by
reducing the incidence and severity of ischemic deficits in patients with subarachnoid hemorrhage from
ruptured intracranial berry aneurysms regardless of their post-ictus neurological condition (i.e., Hunt
and Hess Grades I-V).
HOW SUPPLIED: Nimodipine capsules 30 mg are clear yellow solution filled in oblong opaque light
yellow softgel capsules, imprinted 135 in black ink. The capsules are available as follows:
NDC 57664-135-64 Unit Dose Blisters of 30 (6 x 5)
NDC 57664-135-65 Unit Dose Blisters of 100 (4 x 25)
Storage: The capsules should be stored in manufacturer's original foil package at 20 to 25C (68 to
77F) [see USP Controlled Room Temperature].
Capsules should be protected from light and freezing.
----------------Drug UPDATES: NYMALIZE (nimodipine) oral solution Initial U.S. Approval: 1988
[Drug information / PDF]
Dosing: Click (+) next to Dosage and Administration section (drug info link)
Initial U.S. Approval: 2013
INDICATIONS AND USAGE: NYMALIZE is a dihydropyridine calcium channel blocker indicated for
the improvement of neurological outcome by reducing the incidence and severity of ischemic deficits in
adult patients with subarachnoid hemorrhage (SAH) from ruptured intracranial berry aneurysms
regardless of their post-ictus neurological condition (i.e., Hunt and Hess Grades I-V).
DOSAGE AND ADMINISTRATION
2.1 Administration Instructions
Administer only enterally (e.g., oral, nasogastric tube, or gastric tube route). Do not administer
intravenously or by other parenteral routes. For all routes of administration, begin NYMALIZE within 96
hours of the onset of SAH. Administer one hour before a meal or two hours after a meal for all routes
of administration [see Clinical Pharmacology (12.3)].
2.2 Administration by Oral Route
The recommended oral dosage is 20 mL (60 mg) every 4 hours for 21 consecutive days.
2.3 Administration Via Nasogastric or Gastric Tube
Using the supplied oral syringe labeled "ORAL USE ONLY", administer 20 mL (60 mg) every 4 hours
into a nasogastric or gastric tube for 21 consecutive days. For each dose, refill the syringe with 20 mL
of 0.9% saline solution and then flush any remaining contents from nasogastric or gastric tube into the
stomach.
2.4 Dosage Adjustments in Patients with Cirrhosis
In patients with cirrhosis, reduce the dosage to 10 mL (30 mg) every 4 hours [see Warnings and
Precautions (5.2), Clinical Pharmacology (12.3)].
HOW SUPPLIED:Oral Solution: 60 mg per 20 mL (3 mg/mL), pale yellow solution
nisoldipine (Sular):
CLINICAL PHARMACOLOGY
Mechanism of Action
Nisoldipine is a member of the dihydropyridine class of calcium channel antagonists (calcium ion
antagonists or slow channel blockers) that inhibit the transmembrane influx of calcium into vascular
smooth muscle and cardiac muscle. It reversibly competes with other dihydropyridines for binding to
the calcium channel. Because the contractile process of vascular smooth muscle is dependent upon
the movement of extracellular calcium into the muscle through specific ion channels, inhibition of the
calcium channel results in dilation of the arterioles. In vitro studies show that the effects of nisoldipine
on contractile processes are selective, with greater potency on vascular smooth muscle than on
cardiac muscle. Although, like other dihydropyridine calcium channel blockers, nisoldipine has negative
inotropic effects in vitro, studies conducted in intact anesthetized animals have shown that the
vasodilating effect occurs as doses lower than those that affect cardiac contractility.
The effect of nisoldipine on blood pressure is principally a consequence of a dose-related decrease of
peripheral vascular resistance. While nisoldipine, like other dihydropyridines, exhibits a mild diuretic
effect, most of the antihypertensive activity is attributed to its effect on peripheral vascular resistance.
Adults: Oral: Initial: 20 mg once daily, then increase by 10 mg/week (or longer intervals) to attain
adequate control of blood pressure; usual dose range (JNC 7): 10-40 mg once daily; doses >60 mg
once daily are not recommended. A starting dose not exceeding 10 mg/day is recommended for the
elderly and those with hepatic impairment.
Supplied
Tablet, extended release: 10 mg, 20 mg, 30 mg, 40 mg
verapamil (Isoptin )
Adult (usual):
Angina: (extended-release) initial: 180 mg po qd at bedtime. Titrate up to 480 mg at bedtimemaximum 540 mg at bedtime. (immediate release) initial: 80 mg po tid - may titrate at daily or weekly
intervals to 360 mg daily.
Arrhythmias, supraventricular: (immediate-release) initial: 240-320 mg po daily in 3-4 divided doses.
Non-digitalized patients may require up to 480 mg daily in 3-4 divided doses. Arrhythmias,
supraventricular: 5-10 mg IV (0.075-0.15 mg/kg) IV bolus over 2 min. May give additional 10 mg after
30 minutes if no response.
Hypertension: (extended-release) initial, 180 mg tablet po qd at bedtime OR 200 mg capsule po qd at
bedtime. Maintenance: titrate up to 480 mg TAB qd at hs or 400 mg capsule po qd at hs.
Hypertension: (immediate-release) initial- 80 mg po tid. May titrate at daily or weekly intervals to 360480 mg daily. Hypertension: (sustained-release) initial: 240 mg orally once daily in the morning.
Maintenance (based on response): titrate up to 240 mg bid (tablet) or 480 mg (capsule) once a day in
the morning.
Migraine headache, prophylaxis: 80 mg po 3-4 times daily.
[Supplied:
Immediate release tablet: 40, 80, 120mg.
Sustained release tablets (SR): 120, 180, 240 mg.
Sustained released capsules (Verelan): 120,180,240,360mg.
Covera HS (extended release tab): 180,240mg.
Verelan PM (ER cap): 100,200,300mg. ]
----------------------------------Dosing (Adults):
Angina: Oral: Initial: 80-120 mg twice daily (elderly or small stature: 40 mg twice
daily); range: 240-480 mg/day in 3-4 divided doses
Hypertension: Oral:
Immediate release: 80 mg 3 times/day; usual dose range (JNC 7): 80-320 mg/day in 2 divided doses.
Sustained release: 240 mg/day; usual dose range (JNC 7): 120-360 mg/day in 1-2 divided doses; 120
mg/day in the elderly or small patients (no evidence of additional benefit in doses >360 mg/day).
Extended release:
Covera-HS: Usual dose range (JNC 7): 120-360 mg once daily (once-daily dosing is recommended
at bedtime)
Verelan PM: Usual dose range: 200-400 mg once daily at bedtime
Arrhythmia (SVT): I.V.: 2.5-5 mg (over 2 minutes); second dose of 5-10 mg (~0.15 mg/kg) may be
given 15-30 minutes after the initial dose if patient tolerates, but does not respond to initial dose;
maximum total dose: 20 mg
Disclaimer
Listed dosages are for - Adult patients ONLY. PLEASE READ THE DISCLAIMER CAREFULLY
BEFORE ACCESSING OR USING THIS SITE. BY ACCESSING OR USING THIS SITE, YOU AGREE
TO BE BOUND BY THE TERMS AND CONDITIONS SET FORTH IN THE DISCLAIMER. GlobalRPH
does not directly or indirectly practice medicine or provide medical services and therefore assumes no
liability whatsoever of any kind for the information and data accessed through the Service or for any
diagnosis or treatment made in reliance thereon.
This document Copyright 1993-2016 David McAuley, Pharm.D. , All Rights Reserved. Do Not Copy, Distribute
or otherwise Disseminate without express permission. This page was last updated: 09/23/2016 11:27:16
This document Copyright 1993-2016 David McAuley, Pharm.D. , All Rights Reserved. Do Not Copy, Distribute
or otherwise Disseminate without express permission. This page was last updated: 08/28/2016 21:13:15
This site complies with the HONcode standard for trustworthy health information: verify here.
Disclaimer