Ausdipine Dosage

• Dosage of Ausdipine in details
• Ausdipine interactions
• Ausdipine reviews

Dosage of Ausdipine in details

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Suspension,

Oral, as benzoate:

Katerzia: 1 mg/mL (150 mL) [contains polysorbate 80, sodium benzoate]

Tablet,

Oral:

Norvasc: 10 mg

Generic: 10 mg

Tablet,

Oral, as besylate:

Norvasc: 2.5 mg, 5 mg

Generic: 2.5 mg, 5 mg

Dosing: Adult

Angina:

Chronic stable angina (alternative agent):

Note: A beta-blocker is the preferred initial therapy; if there are ongoing symptoms on beta-blocker therapy, a long acting dihydropyridine calcium channel blocker (eg, Ausdipine) may be added; Ausdipine may also be used as an alternative therapy if there are contraindications or unacceptable adverse effects with beta-blockade (ACC/AHA [Fihn 2012]).

Oral:

5 to 10 mg once daily.

Vasospastic angina:

Note: May use alone or in combination with nitrates (ACC/AHA [Fihn 2012]).

Oral:

5 to 10 mg once daily.

Hypertension:

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 [ACE] inhibitor, angiotensin II receptor blocker [ARB], or thiazide diuretic) (ACC/AHA [Whelton 2018]). For combination therapy, some experts recommend Ausdipine plus either an ACE inhibitor or ARB (Jamerson 2008; Mann 2019).

Oral:

Initial: 2.5 to 5 mg once daily; titrate every 1 to 2 weeks as needed based on patient response; maximum: 10 mg/day (ACC/AHA [Whelton 2018]; Jamerson 2008); antihypertensive effect attenuates with higher doses and adverse effects may become more prominent (Mann 2019).

Raynaud phenomenon (off-label use):

Oral:

5 mg once daily; if needed, increase dose gradually based on patient response and tolerability, usually once every 4 weeks, but not more frequently than once every 7 to 10 days; monitor blood pressure closely with each dose increase; maximum dose: 20 mg/day (ESVM [Belch 2017]; Wigley 2020).

Dosing: Geriatric

Dosing should start at the lower end of dosing range and be titrated to response due to possible increased incidence of hepatic, renal, or cardiac impairment. Elderly patients also show decreased clearance of Ausdipine.

Chronic stable angina (alternative agent); vasospastic angina:

Oral: Initial: 5 mg once daily.

Hypertension:

Oral: Initial: 2.5 mg once daily.

Dosing: Pediatric

Hypertension:

Oral:

Children 1 to 5 years: Limited data available: Note: A population pharmacokinetic study found that children <6 years of age had weight-adjusted clearance and V of Ausdipine that were significantly greater than children ≥6 years of age. This may suggest the need for higher mg/kg/day doses in younger children (<6 years of age); however, the study included only a small number of younger children (n=11) (Flynn 2006). One retrospective pediatric study (n=55) that included only eight patients 1-6 years of age used initial doses of 0.05-0.1 mg/kg/day; doses were titrated upwards as needed; mean required dose was significantly higher in patients 1-6 years of age (0.3 ± 0.16 mg/kg/day) compared to older children (6 to 12 years: 0.16 ± 0.12 mg/kg/day; 12 to 20 years: 0.14 ± 0.1 mg/kg/day) (Flynn 2000a).

Children and Adolescents 6 to 17 years: 2.5 to 5 mg once daily; doses >5 mg daily have not been fully studied. In a randomized, placebo-controlled trial of Ausdipine in children (n=268; mean age: 12.1 years; range: 6 to 16 years), a significant reduction in systolic blood pressure (compared to placebo) was observed in both the 2.5 mg once daily and the 5 mg once daily Ausdipine groups. The authors recommend an initial dose of 0.06 mg/kg/day with a maximum dose of 0.34 mg/kg/day (not to exceed 10 mg/day) (Flynn 2004).

What other drugs will affect Ausdipine?

Tell your doctor about all your current medicines and any you start or stop using, especially:

• nitroglycerin;

• simvastatin (Zocor, Simcor, Vytorin); or

• any other heart or blood pressure medications.

This list is not complete. Other drugs may interact with Ausdipine, including prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed in this medication guide.

Ausdipine interactions

Ausdipine has been safely administered with thiazide diuretics, alpha blockers, beta-blockers, ACE inhibitors, long-acting nitrates, sublingual nitroglycerine, non-steroidal anti-inflammatory drugs, antibiotics, and oral hypoglycemic drugs.

In vitro data from studies with human plasma indicate that Ausdipine has no effect on protein binding of the drugs tested (digoxin, phenytoin, warfarin, or indomethacin).

Simvastatin: Co-administration of multiple doses of 10 mg Ausdipine with 80 mg simvastatin resulted in a 77% increase in exposure to simvastatin compared to simvastatin alone. Limit the dose of simvastatin in patients on Ausdipine to 20 mg daily.

Grapefruit Juice: Co-administration of 240 mL grapefruit juice with a single oral dose of 10 mg Ausdipine in 20 healthy volunteers had no significant effect on the pharmacokinetics of Ausdipine. The study did not allow examination of the effect of genetic polymorphism in CYP3A4, the primary enzyme responsible for metabolism of Ausdipine; therefore, administration of Ausdipine with grapefruit or grapefruit juice is not recommended as bioavailability may be increased in some patients, resulting in increased blood pressure lowering effects.

CYP3A4 Inhibitors: Co-administration of a 180 mg daily dose of diltiazem with 5 mg Ausdipine in elderly hypertensive patients (69 to 87 years of age) resulted in a 57% increase in Ausdipine systemic exposure. Co-administration of erythromycin in healthy volunteers (18 to 43 years of age) did not significantly change Ausdipine systemic exposure (22% increase in area under the concentration versus time curve [AUC]). Although the clinical relevance of these findings is uncertain, pharmacokinetic variations may be more pronounced in the elderly.

Strong inhibitors of CYP3A4 (e.g., ketoconazole, itraconazole, ritonavir) may increase the plasma concentrations of Ausdipine to a greater extent than diltiazem. Ausdipine should be used with caution when administered with CYP3A4 inhibitors.

Clarithromycin: Clarithromycin is an inhibitor of CYP3A4. There is an increased risk of hypotension in patients receiving clarithromycin with Ausdipine. Close observation of patients is recommended when Ausdipine is co-administered with clarithromycin.

CYP3A4 Inducers: There is no data available regarding the effect of CYP3A4 inducers on Ausdipine. Concomitant use of CYP3A4 inducers (e.g., rifampicin, hypericum perforatum) may decrease the plasma concentrations of Ausdipine. Ausdipine should be used with caution when administered with CYP3A4 inducers.

In the following studies, there were no significant changes in the pharmacokinetics of either Ausdipine or another drug within the study, when co-administered.

Special Studies: Effect of Other Agents on Ausdipine: Cimetidine: Co-administration of Ausdipine with cimetidine did not alter the pharmacokinetics of Ausdipine.

Aluminum/Magnesium (Antacid): Co-administration of aluminum/magnesium (antacid) with a single dose of Ausdipine had no significant effect on the pharmacokinetics of Ausdipine.

Sildenafil: A single 100 mg dose of sildenafil in subjects with essential hypertension had no effect on the pharmacokinetic parameters of Ausdipine. When Ausdipine and sildenafil were used in combination, each agent independently exerted its own blood pressure lowering effect.

Special Studies: Effect of Ausdipine on Other Agents: Atorvastatin: Co-administration of multiple 10 mg doses of Ausdipine with 80 mg atorvastatin resulted in no significant change in the steady-state pharmacokinetic parameters of atorvastatin.

Digoxin: Co-administration of Ausdipine with digoxin did not change serum digoxin levels or digoxin renal clearance in healthy volunteers.

Ethanol (Alcohol): Single and multiple 10 mg doses of Ausdipine had no significant effect on the pharmacokinetics of ethanol.

Warfarin: Co-administration of Ausdipine with warfarin did not change the warfarin prothrombin response time.

Cyclosporin: No drug interaction studies have been conducted with cyclosporin and Ausdipine in healthy volunteers or other populations, with the exception of renal transplant patients. Various studies in renal transplant patients report that co-administration of Ausdipine with cyclosporin affects the trough concentrations of cyclosporin, from no change up to an average increase of 40%. Consideration should be given for monitoring cyclosporin levels in renal transplant patients on Ausdipine.

Tacrolimus: There is a risk of increased tacrolimus blood levels when co-administered with Ausdipine. In order to avoid toxicity of tacrolimus, administration of Ausdipine in a patient treated with tacrolimus requires monitoring of tacrolimus blood levels and dose adjustment of tacrolimus when appropriate.

Drug/Laboratory Test Interactions: None known.

References

1. MeSH. "Antihypertensive Agents". https://www.ncbi.nlm.nih.gov/mesh/68... (accessed September 17, 2018).
2. European Chemicals Agency - ECHA. "3,5-Pyridinedicarboxylic acid, 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-, 3-ethyl 5-methyl ester: The information provided here is aggregated from the "Notified classification and labelling" from ECHA's C&L Inventory. ". https://echa.europa.eu/information-o... (accessed September 17, 2018).
3. PubMed Health. "Norvasc: This section provide the link out information of drugs collectetd in PubMed Health. ". http://www.ncbi.nlm.nih.gov/pubmedhe... (accessed September 17, 2018).

Reviews

The results of a survey conducted on ndrugs.com for Ausdipine are given in detail below. The results of the survey conducted are based on the impressions and views of the website users and consumers taking Ausdipine. We implore you to kindly base your medical condition or therapeutic choices on the result or test conducted by a physician or licensed medical practitioners.

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Information checked by Dr. Sachin Kumar, MD Pharmacology