盐酸尼卡地平注射液说明书
盐酸尼卡地平注射液丨Meta分析证实...
妊娠高血压是妊娠期常见疾病综合征，发生于女性妊娠20周或之后，收缩压≥140mmHg和（或）舒张压≥90mmHg，是孕产妇死亡的主要原因，3%～10%伴有并发症。
妊娠高血压是严重威胁母儿健康和生命的孕期疾病，病情严重程度与母儿不良结局发生率正相关，因此早期预防和干预十分重要。
为预防心脑血管意外和胎盘早剥等严重母胎并发症，降低母儿围生期病死率，做好妊娠高血压的防治尤为重要。
药物是治疗妊娠高血压的重要手段。
尼卡地平目前，常用降压药物有肾上腺素能受体阻滞剂、钙离子通道阻滞剂及中枢性肾上腺素能神经阻滞剂等药物。
尼卡地平作为水溶性二氢吡啶类钙通道阻滞剂，广泛应用于妊娠期高血压疾病的治疗。
一项Meta分析系统评价尼卡地平单用或联用治疗妊娠期高血压的有效性及安全性。
尼卡地平组：采用尼卡地平单用治疗或尼卡地平联用其他降血压药物治疗对照组：采用其他降血压药物纳入标准：符合妊娠高血压诊断标准，即妊娠20周后首次出现高血压，收缩压≥140mmHg和（或）舒张压≥90mmHg。
研究共纳入符合研究文献10篇，共1760例患者。
分析结果纳入文献的Meta分析结果表明，尼卡地平单药治疗与对照组疗效相当，但尼卡地平联合用药治疗妊娠期高血压，收缩压降低幅度优于对照组。
治疗后收缩压变化Meta分析结果（experimental：尼卡地平组；control：对照组）同时，Meta分析结果表明，尼卡地平单用与联合用药治疗妊娠高血压，舒张压的降低幅度均优于对照组。
治疗后舒张压变化Meta分析结果（experimental：尼卡地平组；control：对照组）在不良反应发生情况方面，Meta分析结果表明，尼卡地平单用或联合用药治疗妊娠高血压，不良反应发生率与对照组无显著差异。
治疗后不良反应发生情况的Meta分析结果（experimental：尼卡地平组；control：对照组）综上所述，Meta分析结果显示，尼卡地平无论是单药治疗还是联合用药，降低妊娠期舒张压优于其他降压药，尤其是联合用药收缩压和舒张压均得到了更好控制。
尼卡地平FDA说明书
_________________________________________________________________________________________________ HIGHLIGHTS OF PRESCRIBING INFORMATION These highlights do not include all the information needed to use NICARDIPINE HYDROCHLORIDE safely and effectively. See full prescribing information for NICARDIPINE HYDROCHLORIDE. NICARDIPINE HYDROCHLORIDE injection, for intravenous use Initial U.S. Approval: 1988 ---------------------------RECENT MAJOR CHANGES ---------------------------Dosage and Administration (2.2) 04/2016 ---------------------------INDICATIONS AND USAGE----------------------------Nicardipine hydrochloride injection is a calcium channel blocker indicated for the short-term treatment of hypertension when oral therapy is not feasible. -----------------------DOSAGE AND ADMINISTRATION -----------------------∙ Individualize dosage based upon the severity of hypertension and response of the patient during dosing (2.1). ∙ Single dose vials must be diluted before use (2.2). ∙ When substituting for oral nicardipine therapy, use the intravenous ∙ rate by 2.5 mg/hr to a maximum of 15 mg/hr until desired blood pressure reduction is achieved. For a gradual blood pressure reduction the rate can be increased every 15 minutes, for a rapid reduction, every 5 minutes (2.4). ∙ If hypotension or tachycardia ensues, discontinue the infusion. After stabilized, patient can be restarted at low doses such as 3 to 5 mg/hr (2.5). ---------------------DOSAGE FORMS AND STRENGTHS----------------------∙ 25 mg/10 ml (2.5 mg/mL) single-dose vial (3) ∙ 20 mg in 200 ml (0.1 mg/mL) flexible container (3) ∙ 40 mg in 200 ml (0.2 mg/mL) flexible container (3) ------------------------------CONTRAINDICATIONS ------------------------------∙ Do not use in patients with advanced aortic stenosis (4.1). -----------------------WARNINGS AND PRECAUTIONS------------------------∙ To reduce the possibility of venous thrombosis, phlebitis, and vascular impairment, do not use small veins, such as those on the dorsum of the hand or wrist. Avoid intraarterial administration or extravasation (5.7). ∙ To minimize the risk of peripheral venous irritation, change the site of infusion of nicardipine every 12 hours (5.7). ∙ Nicardipine is not a beta-blocker and therefore gives no protection against the dangers of abrupt beta-blocker withdrawal. Withdraw beta-blockers gradually (5.8). ∙ Closely monitor response in patients with angina (5.3), congestive heart failure (5.4), impaired hepatic function (5.5), portal hypertension (5.5), and renal impairment (5.6) and pheochromocytoma (5.9). ------------------------------ADVERSE REACTIONS-------------------------------Most common adverse reactions are headache (13%), hypotension (5%), tachycardia (4%) and nausea/vomiting (4%). To report SUSPECTED ADVERSE REACTIONS, contact West-WardPharmaceuticals at 1-877-233-2001 or the FDA at 1-800-FDA-1088 or/medwatch .------------------------------DRUG INTERACTIONS-------------------------------∙ Cimetidine increases nicardipine plasma levels (7.3). ∙ Nicardipine may increase cyclosporine and tacrolimus plasma levels. Frequent monitoring of trough blood levels of cyclosporine and tacrolimus is recommended when co-administering nicardipine. (7.5, 7.6). -----------------------USE IN SPECIFIC POPULATIONS -----------------------∙ Pregnancy: Based on animal data, may cause fetal harm (8.1). ∙ Nursing Mothers: It is recommended that women who wish to breastfeed should not be given this drug (8.3). ∙ Safety and efficacy in patients under the age of 18 have not been established (8.4). Revised: 9/2016 FULL PRESCRIBING INFORMATION: CONTENTS* 1 INDICATIONS AND USAGE 1.1 Hypertension 2 DOSAGE AND ADMINISTRATION 2.1 General Information 2.2 Inspection and Preparation 2.3 Dosage as a Substitute for Oral Nicardipine Therapy 2.4 Dosage for Initiation of Therapy in a Drug-Free Patient 2.5 Conditions Requiring Infusion Adjustment 2.6 Transfer to Oral Antihypertensive Agents 3 DOSAGE FORMS AND STRENGTHS 4 CONTRAINDICATIONS 4.1 Advanced Aortic Stenosis 5 WARNINGS AND PRECAUTIONS 5.1 Excessive Pharmacologic Effects 5.2 Rapid Decreases in Blood Pressure 5.3 Use in Patients with Angina 5.4 Use in Patients with Congestive Heart Failure 5.5 Use in Patients with Impaired Hepatic Function 5.6 Use in Patients with Impaired Renal Function 5.7 Intravenous Infusion Site 5.8 Beta-Blocker Withdrawal 5.9 Use in Patients with Pheochromocytoma 6 ADVERSE REACTIONS 6.1 Adverse Reactions Observed in Clinical Trials 7 DRUG INTERACTIONS 7.1 Antihypertensive Agents 7.2 Beta-Blockers 7.3 Cimetidine 7.4 Digoxin 7.5 Cyclosporine 7.6 Tacrolimus 7.7 In Vitro Interaction 8 USE IN SPECIFIC POPULATIONS 8.1 Pregnancy 8.3 Nursing Mothers 8.4 Pediatric Use 8.5 Geriatric Use 10 OVERDOSAGE 11 DESCRIPTION 12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action 12.2 Pharmacodynamics 12.3 Pharmacokinetics 13 NONCLINICAL TOXICOLOGY 13.1 Carcinogenesis, Mutagenesis, Impairment of Fertility 13.3 Reproductive and Developmental Toxicology 14 CLINICAL STUDIES 16 HOW SUPPLIED/STORAGE AND HANDLING 16.1 How Supplied 16.2 Storage and Handling *Sections or subsections omitted from the full prescribing information are not listed.FULL PRESCRIBING INFORMATION:1 INDICATIONS AND USAGE1.1 HypertensionNicardipine hydrochloride injection is indicated for the short-term treatment of hypertension when oral therapy is not feasible or desirable. For prolonged control of blood pressure, transfer patients to oral medication as soon as their clinical condition permits [see Dosage and Administration (2.6)].2 DOSAGE AND ADMINISTRATION2.1 General InformationIndividualize dosing based on the severity of hypertension and the response of the patient during dosing. Monitor blood pressure and heart rate both during and after the infusion to avoid tachycardia or too rapid or excessive reduction in either systolic or diastolic blood pressure.Administer Nicardipine Hydrochloride by slow continuous infusion by a central line or through a large peripheral vein. Change the infusion site every 12 hours if administered via peripheral vein [see Intravenous Infusion Site (5.7)].2.2 Inspection and PreparationParenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.Do not use the solution if particulate matter, precipitate, or crystallization is present, or if the container appears damaged.Single Dose VialsDilutionSingle dose vials must be diluted before infusion.Each vial (25 mg) must be diluted with 240 mL of compatible intravenous fluid (see below), resulting in 250 mL of solution at a concentration of 0.1 mg/mL.CompatabilityNicardipine hydrochloride injection has been found compatible and stable in polyvinyl chloride containers for 24 hours at controlled room temperature with:Dextrose (5%) Injection, USPDextrose (5%) and Sodium Chloride (0.45%) Injection, USPDextrose (5%) and Sodium Chloride (0.9%) Injection, USPDextrose (5%) with 40 mEq Potassium, USPSodium Chloride (0.45%) Injection, USPSodium Chloride (0.9%) Injection, USPNicardipine hydrochloride is not compatible with Sodium Bicarbonate (5%) Injection, USP or Lactated Ringer’s Injection, USP.Flexible ContainersDilution is not required for Nicardipine Hydrochloride in 0.9% Sodium Chloride Injection.Check the container for minute leaks prior to use by squeezing the bag firmly; ensure that the seal is intact. If leaks are found, discard solution as sterility may be impaired.Do not combine Nicardipine Hydrochloride in 0.9% Sodium Chloride Injection with any product in the same intravenous line or premixed container. Do not add supplementary medication to the bag. Protect from light until ready to use.Do not use plastic containers in series connections. Such use could result in air embolism due to residual air being drawn from the primary container before the administration of the fluid from the secondary container is complete.Preparation for administration1. Suspend container from eyelet support.2. Remove protector from outlet port at bottom of container.3. Attach administration set. Refer to complete directions accompanying set.2.3 Dosage as a Substitute for Oral Nicardipine TherapyThe intravenous infusion rate required to produce an average plasma concentration equivalent to a given oral dose at steady state is shown in the following table:Equivalent IntravenousOral Nicardipine DoseInfusion Rate20 mg q8h 0.5 mg/hr30 mg q8h 1.2 mg/hr40 mg q8h 2.2 mg/hr2.4 Dosage for Initiation of Therapy in a Drug-Free PatientThe time course of blood pressure decrease is dependent on the initial rate of infusion and the frequency of dosage adjustment. Nicardipine hydrochloride injection is administered by slow continuous infusion at a concentration of 0.1 mg/mL. With constant infusion, blood pressure begins to fall within minutes. It reaches about 50% of its ultimate decrease in about 45 minutes.When treating acute hypertensive episodes in patients with chronic hypertension, discontinuation of infusion is followed by a 50% offset of action in 30 minutes ± 7 minutes but plasma levels of drug and gradually decreasing antihypertensive effects exist for many hours.TitrationFor a gradual reduction in blood pressure, initiate therapy at a rate of 5 mg/hr. If desired blood pressure reduction is not achieved at this dose, increase the infusion rate by 2.5 mg/hr every 15 minutes up to a maximum of 15 mg/hr, until desired blood pressure reduction is achieved. For more rapid blood pressure reduction, titrate every 5 minutes.MaintenanceAdjust the rate of infusion as needed to maintain desired response.2.5 Conditions Requiring Infusion AdjustmentHypotension or Tachycardia: In case of hypotension or tachycardia, discontinue infusion. When blood pressure and heart rate stabilize, restart infusion at low doses such as 30 mL/hr to 50 mL/hr (3 mg/hr to 5 mg/hr) and titrate to maintain desired blood pressure.Infusion Site Changes: Change infusion site every 12 hours if administered via peripheral vein.Impaired Cardiac, Hepatic, or Renal Function: Monitor closely when titrating nicardipine hydrochloride injection in patients with congestive heart failure or impaired hepatic or renal function [see Warnings and Precautions (5.4, 5.5 and 5.6)].2.6 Transfer to Oral Antihypertensive AgentsIf treatment includes transfer to an oral antihypertensive agent other than nicardipine capsules, initiate oral therapy upon discontinuation of nicardipine hydrochloride injection.When switching to a TID regimen of nicardipine capsules, administer the first dose 1 hour prior to discontinuation of the infusion.3 DOSAGE FORMS AND STRENGTHSNicardipine hydrochloride is available in the following presentations:∙25 mg nicardipine hydrochloride in 10 mL injection (2.5 mg/mL) in a single dose vial∙20 mg nicardipine hydrochloride in 200 mL 0.9% sodium chloride injection (0.1 mg/mL) in a flexible container∙40 mg nicardipine hydrochloride in 200 mL 0.9% sodium chloride injection (0.2 mg/mL) in a flexible container4 CONTRAINDICATIONS4.1 Advanced Aortic StenosisDo not use nicardipine in patients with advanced aortic stenosis because of the afterload reduction effect of nicardipine. Reduction of diastolic pressure in these patients may worsen rather than improve myocardial oxygen balance.5 WARNINGS AND PRECAUTIONS5.1 Excessive Pharmacologic EffectsIn administrating nicardipine, close monitoring of blood pressure and heart rate is required. Nicardipine may occasionally produce symptomatic hypotension or tachycardia. Avoid systemic hypotension when administering the drug to patients who have sustained an acute cerebral infarction or hemorrhage.5.2 Rapid Decreases in Blood PressureNo clinical events have been reported suggestive of a too rapid decrease in blood pressure with nicardipine. However, as with any antihypertensive agent, blood pressure lowering should be accomplished over as long a time as is compatible with the patient’s clinical status.5.3 Use in Patients with AnginaIncreases in frequency, duration, or severity of angina have been seen in chronic oral therapy with nicardipine capsules. Induction or exacerbation of angina has been seen in less than 1% of coronary artery disease patients treated with nicardipine. The mechanism of this effect has not been established.5.4 Use in Patients with Congestive Heart FailureNicardipine reduced afterload without impairing myocardial contractility in preliminary hemodynamic studies of CHF patients. However, in vitro and in some patients, a negative inotropic effect has been observed. Therefore, monitor vital signs carefully when using nicardipine, particularly in combination with a beta-blocker, in patients with CHF or significant left ventricular dysfunction.5.5 Use in Patients with Impaired Hepatic FunctionSince nicardipine is metabolized in the liver, consider lower dosages and closely monitor response. Nicardipine administered intravenously increased hepatic venous pressure gradient by 4 mmHg in cirrhotic patients at high doses (5 mg/20 min) in one study. Use caution in patients with portal hypertension.5.6 Use in Patients with Impaired Renal FunctionWhen nicardipine was given to mild-to-moderate hypertensive patients with moderate renal impairment, a significantly lower systemic clearance and higher AUC was observed. These results are consistent with those seen after oral administration of nicardipine. Careful dose titration is advised when treating patients with more than mild renal impairment.5.7 Intravenous Infusion SiteTo reduce the possibility of venous thrombosis, phlebitis, local irritation, swelling, extravasation, and the rare occurrence of vascular impairment, administer drug through large peripheral veins or central veins rather than arteries or small peripheral veins, such as those on the dorsum of the hand or wrist. To minimize the risk of peripheral venous irritation, consider changing the site of the drug infusion every 12 hours.5.8 Beta-Blocker WithdrawalNicardipine is not a beta-blocker and therefore gives no protection against the dangers of abrupt beta-blocker withdrawal. Withdraw beta-blockers gradually.5.9 Use in Patients with PheochromocytomaOnly limited clinical experience exists in use of nicardipine for patients with hypertension from pheochromocytoma.6 ADVERSE REACTIONS6.1 Adverse Reactions Observed in Clinical TrialsBecause clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.Two hundred forty-four patients participated in two multicenter, double-blind, placebo-controlled trials of nicardipine. Adverse experiences were generally not serious and most were expected consequences of vasodilation. Adverse reactions occasionally required dosage adjustment. Therapy was discontinued in approximately 12% of patients, mainly due to hypotension, headache, and tachycardia. Adverse reactions that occurred more often on nicardipine than on placebo by at least 2% were headache (13%) and nausea/vomiting (4%).The following adverse reactions have been reported in clinical trials or in the literature during the use of intravenously administered nicardipine.Body as a Whole: fever, neck painCardiovascular: angina pectoris, atrioventricular block, ST segment depression, inverted T wave, deep-vein thrombophlebitisDigestive: dyspepsiaHemic and Lymphatic: thrombocytopeniaMetabolic and Nutritional: hypophosphatemia, peripheral edemaNervous: confusion, hypertoniaRespiratory: respiratory disorderSpecial Senses: conjunctivitis, ear disorder, tinnitusUrogenital: urinary frequencySinus node dysfunction and myocardial infarction, which may be due to disease progression, have been seen in patients on chronic therapy with orally administered nicardipine.7 DRUG INTERACTIONS7.1 Antihypertensive AgentsSince nicardipine hydrochloride injection may be administered to patients already being treated with other medications, including other antihypertensive agents, careful monitoring of these patients is necessary to detect and to treat promptly any undesired effects from concomitant administration.7.2 Beta-BlockersIn most patients, nicardipine hydrochloride injection can safely be used concomitantly with beta-blockers. However, monitor response carefully when combining nicardipine hydrochloride injection with a beta-blocker in the treatment of congestive heart failure patients [see Warnings and Precautions (5.4)].7.3 CimetidineCimetidine has been shown to increase nicardipine plasma concentrations with oral nicardipine administration. Carefully monitor patients receiving the two drugs concomitantly. Data with other histamine-2 antagonists are not available.7.4 DigoxinStudies have shown that oral nicardipine usually does not alter digoxin plasma concentrations.7.5 CyclosporineConcomitant administration of oral or intravenous nicardipine and cyclosporine results in elevated plasma cyclosporine levels through nicardipine inhibition of hepatic microsomal enzymes, including CYP3A4. Monitor closely plasma concentrations of cyclosporine during nicardipine hydrochloride injection administration, and adjust the dose of cyclosporine accordingly.7.6 TacrolimusConcomitant administration of intravenous nicardipine and tacrolimus may result in elevated plasma tacrolimus levels through nicardipine inhibition of hepatic microsomal enzymes, including CYP3A4. Closely monitor plasma concentrations of tacrolimus during nicardipine administration, and adjust the dose of tacrolimus accordingly.7.7 In Vitro InteractionThe plasma protein binding of nicardipine was not altered when therapeutic concentrations of furosemide, propranolol, dipyridamole, warfarin, quinidine, or naproxen were added to human plasma in vitro.8 USE IN SPECIFIC POPULATIONS8.1 PregnancyPregnancy Category C.There are no adequate and well-controlled studies of nicardipine use in pregnant women. There are limited human data in pregnant women with pre-eclampsia and preterm labor. In animal reproduction and developmental toxicity studies, evidence of fetal harm was observed. Therefore use nicardipine during pregnancy only if the potential benefit justifies the potential risk to the fetus.In reproduction studies conducted in rats and rabbits, increased embryolethality occurred when nicardipine was administered intravenously at doses equivalent to human intravenous doses of 1.6 (rats) and 0.32 mg/kg/day (rabbits).Increased embryolethality was also observed when nicardipine was administered orally to pregnant rabbits at a dose equivalent to a human oral dose of about 48 mg/kg/day (a dose 24 times the maximum recommended human oral dose and one associated with marked maternal body weight gain suppression). At a lower oral dose, equivalent to a human dose of about 32 mg/kg/day (16 times the maximum recommended human oral dose), in a different strain of rabbit, there were no adverse effects on the fetus, though there was increased maternal mortality. There was no evidence of embyolethality or teratogenicity when pregnant rats were administered nicardipine orally at a dose equivalent to a human oral dose ofabout 16 mg/kg/day (8 times the MRHD); however, dystocia, reduced birth weight, reduced neonatal survival and reduced neonatal weight gain were reported [see Nonclinical Toxicology (13.3)].8.3 Nursing MothersNicardipine is minimally excreted into human milk. Among 18 infants exposed to nicardipine through breast milk in the postpartum period, calculated daily infant dose was less than 0.3 mcg and there were no adverse events observed. It is recommended that women who wish to breastfeed should not be given this drug.In a study of 11 women who received oral nicardipine 4 days to 14 days postpartum, 4 women received immediate-release nicardipine 40 to 80 mg daily, 6 women received sustained-release nicardipine 100 mg to 150 mg daily, and one woman received intravenous nicardipine 120 mg daily. The peak milk concentration was 7.3 mcg/L (range 1.9 to 18.8), and the mean milk concentration was 4.4 mcg/L (range 1.3 to 13.8).Infants received an average of 0.073% of the weight-adjusted maternal oral dose and 0.14% of the weight-adjusted maternal intravenous dose.In another study of seven women who received intravenous nicardipine for an average of 1.9 days in the immediate postpartum period as therapy for pre-eclampsia, 34 milk samples were obtained at unspecified times and nicardipine was undetectable (less than 5 mcg/L) in 82% of the samples. Four women who received 1 to 6.5 mg/hour of nicardipine had 6 milk samples with detectable nicardipine levels (range 5.1 to 18.5 mcg/L). The highest concentration of 18.5 mcg/L was found in a woman who received 5.5 mg/hour of nicardipine. The estimated maximum dose in a breastfed infant was less than 0.3 mcg daily or 0.015% to 0.004% of the therapeutic dose in a 1 kg infant.8.4 Pediatric UseSafety and efficacy in patients under the age of 18 have not been established.8.5 Geriatric UseThe steady-state pharmacokinetics of nicardipine are similar in elderly hypertensive patients (greater than 65 years) and young healthy adults.Clinical studies of nicardipine did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects.Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal or cardiac function, and concomitant disease of other drug therapy.10 OVERDOSAGESeveral overdosages with orally administered nicardipine have been reported. One adult patient allegedly ingested 600 mg of nicardipine immediate release capsules, and another patient, 2160 mg of the sustained release formulation of nicardipine. Symptoms included marked hypotension, bradycardia, palpitations, flushing, drowsiness, confusion and slurred speech. All symptoms resolved without sequelae. Anoverdosage occurred in a one-year-old child who ingested half of the powder in a 30 mg nicardipine standard capsule. The child remained asymptomatic.Based on results obtained in laboratory animals, lethal overdose may cause systemic hypotension, bradycardia (following initial tachycardia) and progressive atrioventricular conduction block. Reversible hepatic function abnormalities and sporadic focal hepatic necrosis were noted in some animal species receiving very large doses of nicardipine.For treatment of overdosage, standard measures including monitoring of cardiac and respiratory functions should be implemented. The patient should be positioned to avoid cerebral anoxia. Frequent blood pressure determinations are essential. Vasopressors are clinically indicated for patients exhibiting profound hypotension. Intravenous calcium gluconate may help reverse the effects of calcium entry blockade.11 DESCRIPTIONNicardipine hydrochloride is a calcium ion influx inhibitor (slow channel blocker or calcium channel blocker). Nicardipine hydrochloride for intravenous administration contains 2.5 mg/mL of nicardipine hydrochloride. Nicardipine hydrochloride is a dihydropyridine derivative with IUPAC (International Union of Pure and Applied Chemistry) chemical name (±)-2-(benzyl-methyl amino) ethyl methyl 1,4dihydro-2, 6-dimethyl-4-(m-nitrophenyl)-3,5-pyridinedicarboxylate monohydrochloride and has the following structure:Nicardipine hydrochloride is a yellow to pale yellow, odorless, crystalline powder that has a melting point range of 165-170◦ C. It is soluble in methanol, sparingly soluble in ethanol, slightly soluble in ace tone, chloroform and water. It has a molecular weight of 515.99.Nicardipine hydrochloride injection is available as a sterile, non-pyrogenic, clear, yellow solution in 10 mL vials for intravenous infusion after dilution. Each mL contains 2.5 mg nicardipine hydrochloride, 0.305 mg benzoic acid, USP and 7.5 mg sodium chloride, USP, in Water for Injection, USP. Sodium hydroxide, NF, may have been added to adjust pH to 3.5.Nicardipine Hydrochloride in 0.9% Sodium Chloride Injection is available as a single-use, ready-to-use, iso-osmotic, clear, yellow solution for intravenous administration in a 200 mL flexible container. Each mL contains 0.1 mg or 0.2 mg nicardipine hydrochloride in 9 mg Sodium Chloride, USP. Hydrochloric acid may have been added to adjust pH.12 CLINICAL PHARMACOLOGY12.1 Mechanism of ActionNicardipine 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 vascul a r 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.12.2 PharmacodynamicsHemodynamicsNicardipine produces significant decreases in systemic vascular resistance. In a study of intra-arterially administered nicardipine, the degree of vasodilation and the resultant decrease in blood pressure were more prominent in hypertensive patients than in normotensive volunteers. Administration of nicardipine to normotensive volunteers at dosages of 0.25 to 3 mg/hr for eight hours produced changes of less than 5 mmHg in systolic blood pressure and less than 3 mmHg in diastolic blood pressure.An increase in heart rate is a normal response to vasodilation and decrease in blood pressure; in some patients these increases in heart rate may be pronounced. In placebo-controlled trials, the mean increases in heart rate were 7 ± 1 bpm in postoperative patients and 8 ± 1 bpm in patients with severe hypertension at the end of the maintenance period.Hemodynamic studies following intravenous dosing in patients with coronary artery disease and normal or moderately abnormal left ventricular function have shown significant increases in ejection fraction and cardiac output with no significant change, or a small decrease, in left ventricular end-diastolic pressure (LVEDP). There is evidence that nicardipine increases blood flow. Coronary dilatation induced by nicardipine improves perfusion and aerobic metabolism in areas with chronic ischemia, resulting in reduced lactate production and augmented oxygen consumption. In patients with coronary artery disease, nicardipine, administered after beta-blockade, significantly improved systolic and diastolic left ventricular function.In congestive heart failure patients with impaired left ventricular function, nicardipine increased cardiac output both at rest and during exercise. Decreases in left ventricular end-diastolic pressure were also observed. However, in some patients with severe left ventricular dysfunction, it may have a negative inotropic effect and could lead to worsened failure.“Coronary steal” has not been observed during treatment with nicardipine (Coronary steal is the detrimental redistribution of coronary blood flow in patients with coronary artery disease from underperfused areas toward better perfused areas.) Nicardipine has been shown to improve systolic shortening in both normal and hypokinetic segments of myocardial muscle. Radionuclide angiography has confirmed that wall motion remained improved during increased oxygen demand. (Occasional patients have developed increased angina upon receiving nicardipine capsules. Whether this represents coronary steal in these patients, or is the result of increased heart rate and decreased diastolic pressure, is not clear.)In patients with coronary artery disease, nicardipine improves left ventricular diastolic distensibility during the early filling phase, probably due to a faster rate of myocardial relaxation in previously underperfused areas. There is little or no effect on normal myocardium, suggesting the improvement is mainly by indirect mechanisms such as afterload reduction and reduced ischemia. Nicardipine has no。
尼卡地平说明书用法用量
尼卡地平说明书用法用量
尼卡地平是一种治疗高血压和心绞痛的药物，下面介绍它的用法和用量。
尼卡地平通常以口服片剂的形式服用。
用法方面，首先需要遵循医生的指示和
药物说明书上的建议。
一般情况下，尼卡地平建议在饭前或饭后服用，可以选择与餐食一起服用或单独服用。
最重要的是每天服用药物的时间保持一致，这有助于维持药物的疗效。
用量方面，应根据医生的建议和个人情况来确定。
一般来说，起始剂量为每天
一次服用30毫克。
根据个体的响应和需要，医生可能会适当调整剂量。
一些病人
可能需要较高的剂量，最高不超过每天240毫克。
然而，请务必不要自行改变剂量，尽量按医生的指示进行。
对于老年人和肝功能受损的患者，起始剂量可能需要调整，因为药物的代谢和
排泄能力可能会受到影响。
在这种情况下，应该咨询医生或药剂师获得准确的用法和用量建议。
尼卡地平的用法和用量是根据个体情况和病情来确定的，因此每个人的用法和
用量可能会有所不同。
请务必遵循医生的指示并按照药物说明书上的建议使用，如果有任何疑问或不适，应及时咨询医生。
同时，不要自行更改用法和用量，以免对个体健康造成不良影响。
盐酸尼卡地平doc
【盐酸尼卡地平】结构式：日文名：塩酸ニカルジピン英文名：Nicardipine Hydrochloride解离常数(25℃)：pKa = 7.2（针对叔胺基、采用滴定法测定）在各pH值溶出介质中的溶解度pH1.2：1.0mg/ml pH4.0：8.8mg/ml (37℃)：pH6.8：0.014mg/ml 水：8.4mg/ml在各溶出介质中的稳定性：水：未测定；在各pH值溶出介质中：未测定。
光：水溶液在荧光灯下（365nm），60分钟降解12.8%。
备注：滤膜对本品吸附严重，建议溶出液取出后、勿过滤、采用离心法测定。
《四条标准溶出曲线》溶出度试验条件：桨板法/50转、溶出介质中不添加表面活性剂。
< 1g:100mg规格散剂>< 10mg规格片剂> < 20mg规格片剂>《质量标准》●1g:100mg规格散剂取本品，混匀，精密量取适量（相当于盐酸尼卡地平20mg），照溶出度测定法（桨板法），以0.05mol/L醋酸/醋酸钠缓冲液(pH4.0)900ml为溶剂，转速为每分钟50转，依法操作，经15分钟时，取溶液适量滤过，弃去至少10ml初滤液，精密量取续滤液4ml，置10ml 量瓶中，加0.05mol/L醋酸/醋酸钠缓冲液(pH4.0)稀释至刻度，摇匀，作为供试品溶液。
另精密称取经105℃干燥2小时的对照品适量，加甲醇溶解稀释制成每1ml中含0.18mg的溶液，精密量取适量，加溶出介质稀释制成每1ml中含9μg的溶液，作为对照品溶液。
取上述两种溶液照紫外-可见分光光度法，分别在240nm波长处测定吸光度，计算溶出量，限度应为标示量的85%。
●10mg规格和20mg规格片剂取本品，照溶出度测定法（桨板法），以0.05mol/L醋酸/醋酸钠缓冲液(pH4.0)900ml为溶剂，转速为每分钟50转，依法操作，经（10mg:45分钟；20mg:90分钟）时，取溶液适量滤过，弃去至少10ml初滤液，取续滤液作为供试品溶液（20mg规格再稀释1倍）。
盐酸尼卡地平 熔点
盐酸尼卡地平熔点盐酸尼卡地平（Nifedipine Hydrochloride）是一种常用的钙通道阻滞剂，广泛应用于临床治疗高血压、心绞痛等心血管疾病。
它是一种白色结晶性粉末，能溶解于水和醇类溶剂。
其熔点是指在常压下，物质从固体状态转变为液体状态所需的温度。
盐酸尼卡地平的熔点为131-133℃。
盐酸尼卡地平是通过抑制细胞内钙离子的内流，从而降低血管平滑肌的张力，扩张冠状动脉和外周血管，增加心肌供血，降低心肌耗氧量，从而起到降压和缓解心绞痛的作用。
盐酸尼卡地平还具有选择性作用，主要作用于冠状动脉，而对其他血管影响较小，因此对心血管系统的影响较为特异。
在临床应用中，盐酸尼卡地平常用于治疗高血压。
高血压是一种常见的慢性疾病，长期不受控制会增加心脏负荷，导致心脏肥厚、心力衰竭等并发症。
盐酸尼卡地平通过扩张血管，降低外周阻力，从而降低血压。
此外，由于其对冠状动脉的扩张作用，盐酸尼卡地平还可用于缓解心绞痛。
心绞痛是由于冠状动脉狭窄或阻塞引起的心肌缺血所致的胸痛，盐酸尼卡地平能够通过扩张冠状动脉，增加心肌血供，缓解心绞痛的发作。
盐酸尼卡地平的用法用量为口服给药，一般每次剂量为10-20毫克，每日2-3次。
为了减少胃肠道反应，盐酸尼卡地平常采用缓释制剂，使药物缓慢释放。
此外，由于盐酸尼卡地平的血压降低作用较快，刚开始使用时可能会出现头晕、头痛等不良反应，需要逐渐调整剂量以减少不良反应的发生。
尽管盐酸尼卡地平在临床应用中效果显著，但仍需注意一些潜在的安全问题。
首先，由于盐酸尼卡地平的扩血管作用，可能导致血压过低，特别是在起始治疗或剂量调整过程中。
其次，长期使用盐酸尼卡地平可能导致心脏反射性加快和血管反射性收缩，增加心脏负荷和心肌耗氧量，应密切监测心率和血压的变化。
此外，盐酸尼卡地平在妊娠期和哺乳期慎用，因为其对胎儿和婴儿的安全性尚不明确。
盐酸尼卡地平是一种常用的钙通道阻滞剂，通过扩张血管，降低血压和缓解心绞痛。
其熔点为131-133℃。
钙通道阻滞药CCB分类、作用及注意事项
钙通道阻滞药目录钙通道阻滞药 (1)二氢吡啶类 (2)硝苯地平Nifedipine (2)尼群地平Nitrendipine (3)尼莫地平 (3)氨氯地平Amlodipine (4)左旋氨氯地平levamlodipine (5)非洛地平Felodipine (6)拉西地平Lacidipine (7)尼卡地平Nicardipine (7)乐卡地平Lercanidipine (9)巴尼地平Barnidipine (9)贝尼地平Benidipine (10)非二氢吡啶类 (11)维拉帕米Verapamil (11)地尔硫卓Diltiazem (13)二氢吡啶类硝苯地平Nifedipine【适应证】用于高血压，冠心病，心绞痛。
【注意事项】(1)严重肝功能不全时减小剂量。
(2)老年人用药应从小剂量开始。
(3)严重主动脉瓣狭窄慎用。
(4)终止服药应缓慢减量。
(5)影响驾车和操作机械的能力。
(6)不得与利福平合用。
【禁忌证】对硝苯地平过敏者，心源性休克，儿童、孕妇和哺乳期妇女。
【不良反应】常见面部潮红、头晕、头痛、恶心、下肢肿胀、低血压、心动过速。
较少见呼吸困难。
罕见胸痛、昏厥、胆石症、过敏性肝炎。
【用法和用量】口服：(1)片剂、胶囊剂、胶丸：初始剂量一次10mg，一日3次，维持剂量一次10～20mg，一日3次；冠脉痉挛者可一次20～30mg，一日3～4次，单次最大剂量30mg，一日最大剂量120mg。
(2)缓释片剂、缓释胶囊剂：一次10～20mg，一日2次，单次最大剂量40mg，一日最大剂量120mg。
(3)控释片剂：一次30mg，一日1次。
缓控释制剂与规格不可掰开或嚼服。
静脉滴注：遮光，一次2.5～5mg，加入5%葡萄糖注射液250ml稀释后在4～8小时内缓慢滴入，最大剂量一日15～30mg，可重复使用3天，以后改为口服制剂。
【制剂与规格】硝苯地平片：(1)5mg；(2)10mg。
硝苯地平缓释片：(1)10mg；(2)20mg。
盐酸尼卡地平注射液
盐酸尼卡地平注射液【药品名称】通用名称：盐酸尼卡地平注射液英文名称：Nicardipine Hydrochloride Injection【成份】盐酸尼卡地平。
化学名为：2,6二甲基-4-（3硝基苯基）-1,4二氢吡啶-3,5二羧酸-3-[(N-苄基-N-甲氨基)]-乙酯-5-甲酯盐酸盐。
其结构式为：分子式：C28H20N3O6,HCl分子量：515.99【适应症】手术时异常高血压的急救处置；高血压性急症。
【用法用量】1．手术时异常高血压的急救处置；本品用生理盐水或5%葡萄糖注射液稀释后，以盐酸尼卡地平计，0.01～0.02%（1ml中的含量为0.1～0.2mg）的溶液进行静脉滴注。
这时，以1分钟2～10μg/kg（体重）的滴注速度开始给予，将血压降到目的值后，边监测血压边调节滴注速度。
如有必要迅速降低血压时，则将本品以盐酸尼卡地平计，10～30μg/kg（体重）的剂量进行静脉给予。
2．高血压性紧急症本品用生理或5%葡萄糖注射稀释后，以盐酸尼卡地平计，0.01～0.02%（1ml中的含量为0.1～0.2mg）的溶液进行静脉滴注。
这时，以1分钟0.5～6μg/kg（体重）的滴注速度速度给予。
从1分钟0.5μg/kg（体重）开始，将血压降到目的值后，边监测血压边调节滴注速度。
【不良反应】1．循环系统有时会出现心动过速、心慌、面赤、全身不适感、心电图变化。
2．肝脏有时会出现肝功能障碍（GOT、GPT等的上升）。
3．肾脏有时BUN、肌酐会上升。
4．消化系统有时回出现恶心。
5．其他有时会出现血氧过少、头痛、体温上升、尿量减少、血液总胆固醇下降。
【禁忌】1．颅内出血的，估计尚未完全止血的病人。
2．脑中风的急性期颅内压增高病人。
3．对盐酸尼卡地平有过敏史者。
【注意事项】1．本品作用因人而异，因此应充分监测血压、心搏率等情形下慎重用药。
2．因本品给予过多引起明显低血压时，应中止给予。
此外，如想迅速恢复血压，应投与升压制（正肾上腺素）。
盐酸尼卡地平缓释胶囊(佩尔)的说明书
盐酸尼卡地平缓释胶囊(佩尔)的说明书老年人的健康是每个子女都很关心的，尤其是患有心脑血管这种会威胁到性命的老年人，很多子女都在为如何治愈这种疾病和烦恼。
盐酸尼卡地平缓释胶囊(佩尔)是目前治疗心脑血管疾病效果非常好的一种药物，作为子女的可以给家里老年人了解一下。
【药品名称】通用名称：盐酸尼卡地平缓释胶囊商品名称：盐酸尼卡地平缓释胶囊(佩尔)拼音全码：YanSuanNiKaDiPingHuanShiJiaoNang(PeiEr)【适应症/功能主治】原发性高血压。
同时适用于心绞痛，缺血性及出血性脑血管意外后遗症等。
【规格型号】40mg*30s【用法用量】成人：口服，每日二次，每次一粒（40mg）。
【不良反应】1 常见者有足踝部水肿、头晕、头痛、面部潮红等。
2 有时出现GOT、GPT、γ-GTP升高，偶有胆红素升高。
3 较少见者心悸、乏力、心动过速。
4 有时出现便秘腹痛、偶有食欲不振、腹泻、恶心、呕吐。
5 其它：偶有LDH、胆固醇、尿素氮、肌酐升高，偶见粒细胞减少。
【禁忌】1 对本品有过敏应者。
2 颅内出血尚未完全止血的患者。
3 脑中风性期颅内压增高的患者。
4 重度主动脉瓣狭窄。
【注意事项】1 有肝、肾功能障碍的患者，低血压、心力衰竭，青光眼，孕妇，哺乳期妇女，儿童慎用本品。
肝功能不全者宜从低剂量开始。
2 性脑梗死和脑缺血患者，应慎用，以防发生低血压。
3 本药时需观察血压，心率。
4 停用本品时应逐渐减少剂量，并密切观察病情。
【有效期】36 月【批准文号】国药准字H20030233【生产企业】安斯泰来制药(中国)有限公司【化学名】:2,6-二甲基-4-(3-硝基苯基)-1，4-二氢吡啶-3，5-二羧酸，3-［β-（N-苄基-N-甲氨基）］乙酯-5-甲酯盐酸盐。
【英文名】Nicardipine Hydrochloride Sust【商品名】佩尔【通用名】盐酸尼卡地平缓释胶囊【规格】40mg【剂型】胶囊剂【药理作用】本品为钙离子拮抗剂，通过抑制钙离子流入血管平滑肌细胞内而发挥血管扩张作用，从而使血压下降。
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盐酸尼卡地平注射液
盐酸尼卡地平注射液使用说明书
•【药品名称】
通用名称：盐酸尼卡地平注射液
英文名称：Nicadipine Hydrochloride Injection
•【成份】盐酸尼卡地平
•【性状】本品为淡黄色的澄明液体。
•【适应症】
手术时异常高血压的急救处置；高血压性急症。
•【用法用量】1．手术时异常高血压的急救处置；本品用生理盐水或5%葡萄糖注射液稀释后，以盐酸尼卡地平计，0.01～0.02%（1ml中的含量为0.1～0.
2mg）的溶液进行静脉滴注。
这时，以1分钟2～10μg/kg（体重）的滴注速
度开始给予，将血压降到目的值后，边监测血压边调节滴注速度。
如有必要
迅速降低血压时，则将本品以盐酸尼卡地平计，10～30μg/kg（体重）的剂
量进行静脉给予。
2．高血压性紧急症本品用生理或5%葡萄糖注射稀释后，
以盐酸尼卡地平计，0.01～0.02%（1ml中的含量为0.1～0.2mg）的溶液进行•【不良反应】1．循环系统有时会出现心动过速、心慌、面赤、全身不适感、心电图变化。
2．肝脏有时会出现肝功能障碍（GOT、GPT等的上升）。
3．肾
脏有时BUN、肌酐会上升。
4．消化系统有时回出现恶心。
5．其他有时会出
现血氧过少、头痛、体温上升、尿量减少、血液总胆固醇下降。
•【禁忌】1．颅内出血的，估计尚未完全止血的病人。
2．脑中风的急性期颅内压增高病人。
3．对盐酸尼卡地平有过敏史者。
•【注意事项】1．本品作用因人而异，因此应充分监测血压、心搏率等情形下慎重用药。
2．因本品给予过多引起明显低血压时，应中止给予。
此外，
如想迅速恢复血压，应投与升压制（正肾上腺素）。
3．对高血压性急症，经投与本品，血压达到目标后，仍然继续进行降压治疗，且有可能时应改为口服。
4．高血压急症在停止使用本品后血压有时会重新上升，因此应逐渐减量，停药后仍应细心观察血压。
此外，改为口服时，也应注意血压再次上升。
5．长期使用本品若注射部位出现疼痛或发红时，应改变注射部位。
6．有肝、肾功能障碍的患者或主动脉瓣狭窄症进展的患者慎用。
7．孕妇必须在认真权衡利弊后慎用。
哺乳期妇女避免使用，如需应用本品，应停止哺乳。
8．老年人用药时，应从低剂量开始（如0.5μg/kg/分），仔细观察病情，慎重给予。
本品对小儿的安全性尚未确立。
9．与下列药物合用时应慎重：（1）降血压药（会加剧降血压药的效果）；（2）β-阻滞剂（充血性心力衰竭患者有时会呈阴性变力作用）；（3）西米地丁会使本品的血药浓度上升；（4）地高辛（会使地高辛的血药浓度升高）；（5）芬太尼麻醉（与β-阻滞剂合用时，有时会出现低血压）（6）环胞素（会使环胞素的血药浓度上升）；（7）苯妥英钠（会使苯妥英钠的血药浓度上升，引起神经性中毒症状）；（8）硝苯呋海因（有报告指出，使用其他钙拮抗剂的动物实验中，观察到心室纤维性颤动）；（9）硝酸甘油（有报告指出，出现过房室性传导阻滞）；（10）本品对光不稳定，使用时应避免阳光直射。
•【孕妇及哺乳期妇女用药】孕妇必须在认真权衡利弊后慎用。
哺乳期妇女避免使用，如需应用本品，应停止哺乳。
•【儿童用药】本品对小儿的安全性尚未确立。
•【老年用药】老年人用药时，应从低剂量开始（如0.5μg/kg/分），仔细观察病情，慎重给予。
•【药物相互作用】（1）降血压药（会加剧降血压药的效果）；（2）β-阻滞剂（充血性心力衰竭患者有时会呈阴性变力作用）；（3）西米地丁会使本品的血药浓度上升；（4）地高辛（会使地高辛的血药浓度升高）；（5）芬太尼麻醉（与β-阻滞剂合用时，有时会出现低血压）（6）环胞素（会使
环胞素的血药浓度上升）；（7）苯妥英钠（会使苯妥英钠的血药浓度上升，引起神经性中毒症状）；（8）硝苯呋海因（有报告指出，使用其他钙拮抗
剂的动物实验中，观察到心室纤维性颤动）；（9）硝酸甘油（有报告指出，出现过房室性传导阻滞）；
•【药理毒理】本品抑制心肌与血管平滑肌的跨膜钙离子内流而不改变血钙浓度，其作用在血管平滑肌胜于在心肌，故其血管选择性较强。
动物实验中本
品选择性扩张冠状血管平滑肌，此作用产生时的血药浓度不产生负性肌力作
用(心肌)，对心律及心收缩力的影响极小。
在人体，本品降低周围血管阻力，此作用在高血压患者大于正常血压者，降压时会有反射性心率加快。
本品使
心脏射血分数及心排血量增多，而左室舒张末压改变不多。
能降低心肌耗氧
量及总外周阻力，也可增加冠脉侧枝循环，使冠状血流增加。
本品为二氢吡
啶类钙拮抗剂，可阻滞钙离子流入血管平滑肌细胞内，从而扩张血管，使血
压下降。
•【药代动力学】据资料报道，健康男性成年人，按0.01～0.02mg/kg盐酸尼卡地平静脉给予后，消除半衰期为50～63分钟。
尿内主要代谢物为M-11结合
物。
本品的血浆蛋白结合率约90%左右。
【注意】
药物说明书里面有三种标识，一般要注意一下：
1.第一种就是禁用，就是绝对禁止使用。
2.第二种就是慎用，就是药物可以使用，但是要密切关注患者口服药以后的情况，一旦有不良反应发生，需要马上停止使用。
3.第三种就是忌用，就是说明药物在此类人群中有明确的不良反应，应该是由医生根据病情给出用药建议。
如果一定需要这种药物，就可以联合其他的能减轻不良反应的药物一起服用。
大家以后在服用药物的时候，多留意说明书，留意注意事项，避免不良反应的发生。
本文到此结束，谢谢大家!。