Hypertension, chronic:
Note: For patients who warrant combination therapy (BP >20/10 mm Hg above goal or suboptimal response to monotherapy), may use with another appropriate agent (eg, angiotensin-converting enzyme inhibitor, angiotensin II receptor blocker, or thiazide diuretic) (Ref).
Oral: Initial: 2.5 mg twice daily; evaluate response after ~2 to 4 weeks and titrate dose as needed up to 5 mg twice daily; if additional BP control is needed, consider combination therapy (Ref). Note: Most patients show no additional response with doses >10 mg/day and adverse reactions occur more frequently.
There are no dosage adjustments provided in the manufacturer's labeling; however, bioavailability is increased with mild renal impairment and decreased with severe renal impairment. Isradipine is not removed by hemodialysis; therefore, supplemental doses after hemodialysis are not necessary (Ref).
There are no dosage adjustments provided in the manufacturer's labeling; however, peak serum concentrations are increased by 32% and AUC is increased by 52%.
Refer to adult dosing.
(For additional information see "Isradipine: Pediatric drug information")
Hypertension: Limited data available: Infants, Children, and Adolescents: Immediate release: Oral: Initial: 0.05 to 0.1 mg/kg/dose 2 to 3 times daily; titrate upwards at 2- to 4-week intervals; maximum daily dose: 0.6 mg/kg/day not to exceed 10 mg/day (Ref). Based on retrospective observations, initial doses of 0.05 to 0.15 mg/kg/dose administered 3 to 4 times daily have been suggested in patients with secondary hypertension and acute severe hypertension; usual daily dose: 0.3 to 0.4 mg/kg/day in divided doses (eg, every 8 hours); reported range: 0.04 to 1.2 mg/kg/day (Ref). Note: Most adult patients show no improvement with doses >10 mg daily, and adverse reaction rate increases (Ref).
There are no dosage adjustments provided in manufacturer's labeling; however, bioavailability is increased with mild renal impairment; trend is reversed with further renal function deterioration. Other sources recommend that no initial dosage adjustment is required in pediatric and adult patients (Ref). Isradipine is not removed by hemodialysis; therefore, supplemental doses after hemodialysis are not necessary (Ref).
There are no dosage adjustments provided in manufacturer's labeling; however, adult pharmacokinetic data has shown peak serum concentrations are increased by 32% and bioavailability is increased by 52%; use with caution.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
>10%: Central nervous system: Headache (dose related 2% to 22%)
1% to 10%:
Cardiovascular: Edema (dose related 1% to 9%), flushing (dose related 1% to 5%), palpitations (dose related 1% to 5%), chest pain (3%), tachycardia (1% to 3%)
Central nervous system: Fatigue (dose related ≤9%), dizziness (2% to 8%)
Dermatologic: Skin rash (2%)
Gastrointestinal: Nausea (3% to 5%), abdominal distress (≤3%), diarrhea (≤3%), vomiting (≤1%)
Neuromuscular & skeletal: Weakness (≤1%)
Renal: Urinary frequency (1% to 3%)
Respiratory: Dyspnea (3%)
<1%, postmarketing, and/or case reports: Atrial fibrillation, cardiac failure, cerebrovascular accident, constipation, cough, decreased libido, depression, drowsiness, foot cramps, hyperhidrosis, hypotension, impotence, increased liver enzymes, insomnia, leg cramps, lethargy, leukopenia, myocardial infarction, nervousness, nocturia, numbness, paresthesia, pruritus, psoriasis (Song 2021), sore throat, syncope, transient ischemic attacks, urticaria, ventricular fibrillation, visual disturbance, xerostomia
Hypersensitivity to isradipine or any component of the formulation
Concerns related to adverse effects:
• Angina/MI: Increased angina and/or MI has occurred with initiation or dosage titration of dihydropyridine calcium channel blockers. Reflex tachycardia may occur resulting in angina and/or MI in patients with obstructive coronary disease, especially in the absence of concurrent beta-blockade.
• Hypotension/syncope: Symptomatic hypotension with or without syncope can rarely occur; blood pressure must be lowered at a rate appropriate for the patient's clinical condition.
• Peripheral edema: A common side effect is peripheral edema (dose-dependent); may begin within 2 to 3 weeks of starting therapy.
Disease-related concerns:
• Aortic stenosis: Use with extreme caution in patients with severe aortic stenosis; may reduce coronary perfusion resulting in ischemia.
• Heart failure (HF): The AHA/ACC/HFSA heart failure guidelines recommend to avoid use in patients with heart failure due to lack of benefit and/or worse outcomes with calcium channel blockers in general (AHA/ACC/HFSA [Heidenreich 2022]).
• Hepatic impairment: Use with caution in patients with hepatic impairment; may require lower starting dose.
• Hypertrophic cardiomyopathy (HCM) with outflow tract obstruction: Use with caution in patients with HCM and outflow tract obstruction since reduction in afterload may worsen symptoms associated with this condition.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule, Oral:
Generic: 2.5 mg, 5 mg
Yes
Capsules (Isradipine Oral)
2.5 mg (per each): $1.90 - $12.20
5 mg (per each): $2.78 - $12.34
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Oral: May be administered without regard to meals.
Oral: May be administered without regard to meals.
Hypertension, chronic: Management of hypertension.
Dynacirc [multiple international markets] may be confused with Dynacin brand name for clindamycin, systemic [Philippines]
Substrate of CYP3A4 (major); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.
Alfuzosin: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Amifostine: Blood Pressure Lowering Agents may enhance the hypotensive effect of Amifostine. Management: When used at chemotherapy doses, hold blood pressure lowering medications for 24 hours before amifostine administration. If blood pressure lowering therapy cannot be held, do not administer amifostine. Use caution with radiotherapy doses of amifostine. Risk D: Consider therapy modification
Amphetamines: May diminish the antihypertensive effect of Antihypertensive Agents. Risk C: Monitor therapy
Antipsychotic Agents (Second Generation [Atypical]): Blood Pressure Lowering Agents may enhance the hypotensive effect of Antipsychotic Agents (Second Generation [Atypical]). Risk C: Monitor therapy
Arginine: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Atosiban: Calcium Channel Blockers may enhance the adverse/toxic effect of Atosiban. Specifically, there may be an increased risk for pulmonary edema and/or dyspnea. Risk C: Monitor therapy
Barbiturates: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Benperidol: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Brigatinib: May diminish the antihypertensive effect of Antihypertensive Agents. Brigatinib may enhance the bradycardic effect of Antihypertensive Agents. Risk C: Monitor therapy
Brimonidine (Topical): May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Bromperidol: May diminish the hypotensive effect of Blood Pressure Lowering Agents. Blood Pressure Lowering Agents may enhance the hypotensive effect of Bromperidol. Risk X: Avoid combination
Calcium Salts: May diminish the therapeutic effect of Calcium Channel Blockers. Risk C: Monitor therapy
Cimetidine: May increase the serum concentration of Calcium Channel Blockers. Risk C: Monitor therapy
Clopidogrel: Calcium Channel Blockers may diminish the therapeutic effect of Clopidogrel. Risk C: Monitor therapy
CycloSPORINE (Systemic): Calcium Channel Blockers (Dihydropyridine) may increase the serum concentration of CycloSPORINE (Systemic). CycloSPORINE (Systemic) may increase the serum concentration of Calcium Channel Blockers (Dihydropyridine). Risk C: Monitor therapy
CYP3A4 Inducers (Moderate): May decrease the serum concentration of Isradipine. Risk C: Monitor therapy
CYP3A4 Inducers (Strong): May decrease the serum concentration of Isradipine. Risk C: Monitor therapy
CYP3A4 Inhibitors (Moderate): May increase the serum concentration of Isradipine. Risk C: Monitor therapy
CYP3A4 Inhibitors (Strong): May increase the serum concentration of Isradipine. Risk C: Monitor therapy
Dantrolene: May enhance the hyperkalemic effect of Calcium Channel Blockers. Dantrolene may enhance the negative inotropic effect of Calcium Channel Blockers. Risk X: Avoid combination
Dapoxetine: May enhance the orthostatic hypotensive effect of Calcium Channel Blockers. Risk C: Monitor therapy
Dexmethylphenidate: May diminish the therapeutic effect of Antihypertensive Agents. Risk C: Monitor therapy
Diazoxide: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
DULoxetine: Blood Pressure Lowering Agents may enhance the hypotensive effect of DULoxetine. Risk C: Monitor therapy
Flunarizine: May enhance the therapeutic effect of Antihypertensive Agents. Risk C: Monitor therapy
Fosphenytoin-Phenytoin: Isradipine may increase the serum concentration of Fosphenytoin-Phenytoin. Fosphenytoin-Phenytoin may decrease the serum concentration of Isradipine. Risk C: Monitor therapy
Herbal Products with Blood Pressure Increasing Effects: May diminish the antihypertensive effect of Antihypertensive Agents. Risk C: Monitor therapy
Herbal Products with Blood Pressure Lowering Effects: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Hypotension-Associated Agents: Blood Pressure Lowering Agents may enhance the hypotensive effect of Hypotension-Associated Agents. Risk C: Monitor therapy
Iloperidone: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Indoramin: May enhance the hypotensive effect of Antihypertensive Agents. Risk C: Monitor therapy
Inhalational Anesthetics: May enhance the hypotensive effect of Calcium Channel Blockers. Risk C: Monitor therapy
Isocarboxazid: May enhance the antihypertensive effect of Antihypertensive Agents. Risk X: Avoid combination
Levodopa-Foslevodopa: Blood Pressure Lowering Agents may enhance the hypotensive effect of Levodopa-Foslevodopa. Risk C: Monitor therapy
Loop Diuretics: May enhance the hypotensive effect of Antihypertensive Agents. Risk C: Monitor therapy
Lormetazepam: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Magnesium Sulfate: May enhance the adverse/toxic effect of Calcium Channel Blockers (Dihydropyridine). Specifically, the risk of hypotension or muscle weakness may be increased. Risk C: Monitor therapy
Melatonin: May diminish the antihypertensive effect of Calcium Channel Blockers (Dihydropyridine). Risk C: Monitor therapy
Methylphenidate: May diminish the antihypertensive effect of Antihypertensive Agents. Risk C: Monitor therapy
Molsidomine: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Naftopidil: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Neuromuscular-Blocking Agents (Nondepolarizing): Calcium Channel Blockers may enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents (Nondepolarizing). Risk C: Monitor therapy
Nicergoline: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Nicorandil: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Nitroprusside: Blood Pressure Lowering Agents may enhance the hypotensive effect of Nitroprusside. Risk C: Monitor therapy
Obinutuzumab: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Management: Consider temporarily withholding blood pressure lowering medications beginning 12 hours prior to obinutuzumab infusion and continuing until 1 hour after the end of the infusion. Risk D: Consider therapy modification
Pentoxifylline: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Pholcodine: Blood Pressure Lowering Agents may enhance the hypotensive effect of Pholcodine. Risk C: Monitor therapy
Phosphodiesterase 5 Inhibitors: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Prazosin: Antihypertensive Agents may enhance the hypotensive effect of Prazosin. Risk C: Monitor therapy
Prostacyclin Analogues: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Quinagolide: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Silodosin: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Sincalide: Drugs that Affect Gallbladder Function may diminish the therapeutic effect of Sincalide. Management: Consider discontinuing drugs that may affect gallbladder motility prior to the use of sincalide to stimulate gallbladder contraction. Risk D: Consider therapy modification
Tacrolimus (Systemic): Calcium Channel Blockers (Dihydropyridine) may increase the serum concentration of Tacrolimus (Systemic). Risk C: Monitor therapy
Terazosin: Antihypertensive Agents may enhance the hypotensive effect of Terazosin. Risk C: Monitor therapy
Urapidil: Antihypertensive Agents may enhance the hypotensive effect of Urapidil. Risk C: Monitor therapy
Administration with food delays absorption, but does not affect availability. Management: Administer without regard to meals.
Medications considered acceptable for the treatment of chronic hypertension during pregnancy may generally be continued in patients trying to conceive. Isradipine is generally not considered a preferred agent for use during pregnancy (ACC/AHA [Whelton 2018]; ACOG 2019; NICE 2019); however, use may be considered (ESC [Cífková 2020]).
Isradipine crosses the human placenta. In a study of 16 women, umbilical cord concentrations were variable but less than maternal serum (Lunell 1993).
Chronic maternal hypertension is associated with adverse events in the fetus/infant. Chronic maternal hypertension may increase the risk of birth defects, low birth weight, premature delivery, stillbirth, and neonatal death. Actual fetal/neonatal risks may be related to the duration and severity of maternal hypertension. Untreated chronic hypertension may also increase the risks of adverse maternal outcomes, including gestational diabetes, preeclampsia, delivery complications, stroke, and myocardial infarction (ACOG 2019).
Due to pregnancy-induced physiologic changes, some pharmacokinetic properties of oral isradipine may be altered (Christensen 1994).
Patients with preexisting hypertension may continue their medication during pregnancy unless contraindications exist (ESC [Regitz-Zagrosek 2018]). When treatment of hypertension is initiated during pregnancy, agents other than isradipine may be preferred (ACOG 2019; ESC [Regitz-Zagrosek 2018]; SOGC [Magee 2022]); however, use of isradipine may be considered (ESC [Cífková 2020]).
It is not known if isradipine is present in breast milk.
Due to the potential for serious adverse reactions in the breastfeeding infant, the manufacturer recommends a decision be made whether to discontinue breastfeeding or to discontinue the drug, considering the importance of treatment to the mother. Use of a calcium channel blocker other than isradipine may be preferred in lactating patients (ESC [Cífková 2020]).
Blood pressure; heart rate.
Inhibits calcium ion from entering the “slow channels” or select voltage-sensitive areas of vascular smooth muscle and myocardium during depolarization, producing relaxation of vascular smooth muscle, resulting in coronary vasodilation and reduced blood pressure; increases myocardial oxygen delivery in patients with vasospastic angina
Onset of action: 2 to 3 hours; Note: Full hypotensive effect may not occur for 2 to 4 weeks
Duration: >12 hours
Absorption: 90% to 95%, but large first-pass effect
Distribution: Vd: 3 L/kg
Protein binding: 95%
Metabolism: Extensive first-pass effect; hepatically metabolized via cytochrome P450 isoenzyme CYP3A4; major metabolic pathways include oxidation and ester cleavage; six inactive metabolites have been identified
Bioavailability: 15% to 24%
Mild renal impairment (CrCl 30 to 80 mL/minute): Increased by 45%; as renal function continues to decline, this increase in AUC is reversed to a reduction in AUC as seen with severe renal impairment.
Severe renal impairment (CrCl <10 mL/minute); concurrent hemodialysis: Decreased by 20% to 50%
Hepatic impairment: Increased by 52%
Half-life elimination: Alpha half-life: 1.5 to 2 hours; Terminal half-life: 8 hours
Time to peak, serum: 1 to 1.5 hours
Excretion: Urine (60% to 65% as metabolites); feces (25% to 30%)
Hepatic function impairment: The Cmax increases by 32%
Older adult: The AUC and Cmax increases.
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