Nifelat 30 LA PR Overdose

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What happens if I overdose Nifelat 30 LA PR?

Contact 1-800-222-1222 (the American Association of Poison Control Centers), your local poison control center, or emergency room immediately. Symptoms may include coma; confusion; fainting; fast, slow, or irregular heartbeat; fever; hallucinations; hearing loss; loss of coordination; rapid breathing; ringing in the ears; seizures; severe or persistent dizziness; severe or persistent nausea or vomiting; shortness of breath; sluggishness; stomach pain; unusual sweating.

Proper storage of Nifelat 30 LA PR extended-release tablets:

Store Nifelat 30 LA PR extended-release tablets at room temperature, between 59 and 86 degrees F (15 and 30 degrees C). Store away from heat, moisture, and light. Do not store in the bathroom. Keep Nifelat 30 LA PR extended-release tablets out of the reach of children and away from pets.

Overdose of Nifelat 30 LA PR in details

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Experience with Nifelat 30 LA PR overdosage is limited. Generally, overdosage with Nifelat 30 LA PR leading to pronounced hypotension calls for active cardiovascular support, including monitoring of cardiovascular and respiratory function, elevation of extremities, judicious use of calcium infusion, pressor agents, and fluids. Clearance of Nifelat 30 LA PR would be expected to be prolonged in patients with impaired liver function. Since Nifelat 30 LA PR is highly protein-bound, dialysis is not likely to be of any benefit.

There has been one reported case of massive overdosage with Nifelat 30 LA PR Extended-Release Tablets. The main effects of ingestion of approximately 4800 mg of Nifelat 30 LA PR Extended-Release Tablets in a young man attempting suicide as a result of cocaine-induced depression was initial dizziness, palpitations, flushing, and nervousness. Within several hours of ingestion, nausea, vomiting, and generalized edema developed. No significant hypotension was apparent at presentation, 18 hours post-ingestion. Electrolyte abnormalities consisted of a mild, transient elevation of serum creatinine, and modest elevations of LDH and CPK, but normal SGOT. Vital signs remained stable, no electrocardiographic abnormalities were noted, and renal function returned to normal within 24 to 48 hours with routine supportive measures alone. No prolonged sequelae were observed.

The effect of a single 900 mg ingestion of Nifelat 30 LA PR capsules in a depressed anginal patient also on tricyclic antidepressants was loss of consciousness within 30 minutes of ingestion, and profound hypotension, which responded to calcium infusion, pressor agents, and fluid replacement. A variety of ECG abnormalities were seen in this patient with a history of bundle branch block, including sinus bradycardia and varying degrees of AV block. These dictated the prophylactic placement of a temporary ventricular pacemaker, but otherwise resolved spontaneously. Significant hyperglycemia was seen initially in this patient, but plasma glucose levels rapidly normalized without further treatment.

A young hypertensive patient with advanced renal failure ingested 280 mg of Nifelat 30 LA PR capsules at one time, with resulting marked hypotension responding to calcium infusion and fluids. No AV conduction abnormalities, arrhythmias, or pronounced changes in heart rate were noted, nor was there any further deterioration in renal function.

What should I avoid while taking Nifelat 30 LA PR?

Grapefruit and grapefruit juice may interact with Nifelat 30 LA PR and lead to potentially dangerous effects. Discuss the use of grapefruit products with your doctor. Do not increase or decrease the amount of grapefruit products in your diet without first talking to your doctor.

Avoid getting up too fast from a sitting or lying position, or you may feel dizzy. Get up slowly and steady yourself to prevent a fall.

Drinking alcohol can lower your blood pressure further and may increase certain side effects of Nifelat 30 LA PR.

Nifelat 30 LA PR warnings

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Excessive Hypotension

Although, in most patients, the hypotensive effect of Nifelat 30 LA PR is modest and well tolerated, occasional patients have had excessive and poorly tolerated hypotension. These responses have usually occurred during initial titration or at the time of subsequent upward dosage adjustment. Although patients have rarely experienced excessive hypotension on Nifelat 30 LA PR alone, this may be more common in patients on concomitant beta blocker therapy. Although not approved for this purpose, Nifelat 30 LA PR and other immediate-release Nifelat 30 LA PR capsules have been used (orally and sublingually) for acute reduction of blood pressure. Several well-documented reports describe cases of profound hypotension, myocardial infarction, and death when immediate-release Nifelat 30 LA PR was used in this way. Nifelat 30 LA PR capsules should not be used for the acute reduction of blood pressure.

Severe hypotension and/or increased fluid volume requirements have been reported in patients receiving Nifelat 30 LA PR together with a beta-blocking agent who underwent coronary artery bypass surgery using high dose fentanyl anesthesia. The interaction with high dose fentanyl appears to be due to the combination of Nifelat 30 LA PR and a beta blocker, but the possibility that it may occur with Nifelat 30 LA PR alone, with low doses of fentanyl, in other surgical procedures, or with other narcotic analgesics cannot be ruled out. In Nifelat 30 LA PR treated patients where surgery using high dose fentanyl anesthesia is contemplated, the physician should be aware of these potential problems and, if the patient's condition permits, sufficient time (at least 36 hours) should be allowed for Nifelat 30 LA PR to be washed out of the body prior to surgery.

Increased Angina And/Or Myocardial Infarction

Rarely, patients, particularly those who have severe obstructive coronary artery disease, have developed well documented increased frequency, duration, and/or severity of angina or acute myocardial infarction on starting Nifelat 30 LA PR or at the time of dosage increase. The mechanism of this effect is not established.

Several well-controlled, randomized trials studied the use of immediate-release Nifelat 30 LA PR in patients who had just sustained myocardial infarctions. In none of these trials did immediate-release Nifelat 30 LA PR appear to provide any benefit. In some of the trials, patients who received immediate-release Nifelat 30 LA PR had significantly worse outcomes than patients who received placebo. Nifelat 30 LA PR capsules should not be administered within the first week or two after myocardial infarction, and they should also be avoided in the setting of acute coronary syndrome (when infarction may be imminent).

Use In Essential Hypertension

Nifelat 30 LA PR and other immediate-release Nifelat 30 LA PR capsules have also been used for the long-term control of essential hypertension, although Nifelat 30 LA PR capsules have not been approved for this purpose and no properly controlled studies have been conducted to define an appropriate dose or dose interval for such treatment. Nifelat 30 LA PR capsules should not be used for the control of essential hypertension.

Beta Blocker Withdrawal

Patients recently withdrawn from beta blockers may develop a withdrawal syndrome with increased angina, probably related to increased sensitivity to catecholamines. Initiation of Nifelat 30 LA PR treatment will not prevent this occurrence and might be expected to exacerbate it by provoking reflex catecholamine release. There have been occasional reports of increased angina in a setting of beta blocker withdrawal and Nifelat 30 LA PR initiation. It is important to taper beta blockers if possible, rather than stopping them abruptly before beginning Nifelat 30 LA PR.

Congestive Heart Failure

Rarely, patients, usually those receiving a beta blocker, have developed heart failure after beginning Nifelat 30 LA PR. Patients with tight aortic stenosis may be at greater risk for such an event, as the unloading effect of Nifelat 30 LA PR would be expected to be of less benefit to these patients, owing to their fixed impedance to flow across the aortic valve.

What should I discuss with my healthcare provider before taking Nifelat 30 LA PR?

Some medical conditions may interact with Nifelat 30 LA PR sustained-release tablets. Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:

Some MEDICINES MAY INTERACT with Nifelat 30 LA PR sustained-release tablets. Tell your health care provider if you are taking any other medicines, especially any of the following:

This may not be a complete list of all interactions that may occur. Ask your health care provider if Nifelat 30 LA PR sustained-release tablets may interact with other medicines that you take. Check with your health care provider before you start, stop, or change the dose of any medicine.

Nifelat 30 LA PR precautions

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General

Hypotension

Because Nifelat 30 LA PR decreases peripheral vascular resistance, careful monitoring of blood pressure during the initial administration and titration of Nifelat 30 LA PR is suggested. Close observation is especially recommended for patients already taking medications that are known to lower blood pressure.

Peripheral Edema

Mild to moderate peripheral edema occurs in a dose-dependent manner with Nifelat 30 LA PR. The placebo subtracted rate is approximately 8% at 30 mg, 12% at 60 mg and 19% at 90 mg daily. This edema is a localized phenomenon, thought to be associated with vasodilation of dependent arterioles and small blood vessels and not due to left ventricular dysfunction or generalized fluid retention. With patients whose hypertension is complicated by congestive heart failure, care should be taken to differentiate this peripheral edema from the effects of increasing left ventricular dysfunction.

Use in Cirrhotic Patients

Clearance of Nifelat 30 LA PR is reduced and systemic exposure increased in patients with cirrhosis. It is unknown how systemic exposure may be altered in patients with moderate or severe liver impairment. Careful monitoring and dose reduction may be necessary; consider initiating therapy with the lowest dose available.

Information for Patients

Nifelat 30 LA PR is an extended release tablet and should be swallowed whole and taken on an empty stomach. It should not be administered with food. Do not chew, divide or crush tablets.

Laboratory Tests

Rare, usually transient, but occasionally significant elevations of enzymes such as alkaline phosphatase, CPK, LDH, SGOT, and SGPT have been noted. The relationship to Nifelat 30 LA PR therapy is uncertain in most cases, but probable in some. These laboratory abnormalities have rarely been associated with clinical symptoms; however, cholestasis with or without jaundice has been reported. A small increase (<5%) in mean alkaline phosphatase was noted in patients treated with Nifelat 30 LA PR. This was an isolated finding and it rarely resulted in values which fell outside the normal range. Rare instances of allergic hepatitis have been reported with Nifelat 30 LA PR treatment. In controlled studies, Nifelat 30 LA PR did not adversely affect serum uric acid, glucose, cholesterol or potassium.

Nifelat 30 LA PR, like other calcium channel blockers, decreases platelet aggregation in vitro. Limited clinical studies have demonstrated a moderate but statistically significant decrease in platelet aggregation and increase in bleeding time in some Nifelat 30 LA PR patients. This is thought to be a function of inhibition of calcium transport across the platelet membrane. No clinical significance for these findings has been demonstrated.

Positive direct Coombs’ test with or without hemolytic anemia has been reported but a causal relationship between Nifelat 30 LA PR administration and positivity of this laboratory test, including hemolysis, could not be determined.

Although Nifelat 30 LA PR has been used safely in patients with renal dysfunction and has been reported to exert a beneficial effect in certain cases, rare reversible elevations in BUN and serum creatinine have been reported in patients with pre-existing chronic renal insufficiency. The relationship to Nifelat 30 LA PR therapy is uncertain in most cases but probable in some.

Drug Interactions

Nifelat 30 LA PR is mainly eliminated by metabolism and is a substrate of CYP3A. Inhibitors and inducers of CYP3A can impact the exposure to Nifelat 30 LA PR and consequently its desirable and undesirable effects. In vitro and in vivo data indicate that Nifelat 30 LA PR can inhibit the metabolism of drugs that are substrates of CYP3A, thereby increasing the exposure to other drugs. Nifelat 30 LA PR is a vasodilator, and co-administration of other drugs affecting blood pressure may result in pharmacodynamic interactions.

CYP3A inhibitors

CYP3A inhibitors such as ketoconazole, fluconazole, itraconazole, clarithromycin, erythromycin (Azithromycin, although structurally related to the class of macrolide antibiotic is void of clinically relevant CYP3A4 inhibition), grapefruit, nefazodone, fluoxetine, saquinavir, indinavir, nelfinavir, and ritonavir may result in increased exposure to Nifelat 30 LA PR when co-administered. Careful monitoring and dose adjustment may be necessary; consider initiating Nifelat 30 LA PR at the lowest dose available if given concomitantly with these medications.

Strong CYP3A inducers

Strong CYP3A inducers, such as rifampin, rifabutin, phenobarbital, phenytoin, carbamazepine, and St. John’s Wort reduce the bioavailability and efficacy of Nifelat 30 LA PR; therefore Nifelat 30 LA PR should not be used in combination with strong CYP3A inducers such as rifampin.

Cardiovascular Drugs

Antiarrhythmics

Quinidine: Quinidine is a substrate of CYP3A and has been shown to inhibit CYP3A in vitro. Co-administration of multiple doses of quinidine sulfate, 200 mg t.i.d., and Nifelat 30 LA PR, 20 mg t.i.d., increased Cmax and AUC of Nifelat 30 LA PR in healthy volunteers by factors of 2.30 and 1.37, respectively. The heart rate in the initial interval after drug administration was increased by up to 17.9 beats/minute. The exposure to quinidine was not importantly changed in the presence of Nifelat 30 LA PR. Monitoring of heart rate and adjustment of the Nifelat 30 LA PR dose, if necessary, are recommended when quinidine is added to a treatment with Nifelat 30 LA PR.

Flecainide: There has been too little experience with the co-administration of Tambocor with Nifelat 30 LA PR to recommend concomitant use.

Calcium Channel Blockers

Diltiazem: Pre-treatment of healthy volunteers with 30 mg or 90 mg t.i.d. diltiazem p.o. increased the AUC of Nifelat 30 LA PR after a single dose of 20 mg Nifelat 30 LA PR by factors of 2.2 and 3.1, respectively. The corresponding Cmax values of Nifelat 30 LA PR increased by factors of 2.0 and 1.7, respectively. Caution should be exercised when co-administering diltiazem and Nifelat 30 LA PR and a reduction of the dose of Nifelat 30 LA PR should be considered.

Verapamil: Verapamil, a CYP3A inhibitor, can inhibit the metabolism of Nifelat 30 LA PR and increase the exposure to Nifelat 30 LA PR during concomitant therapy. Blood pressure should be monitored and reduction of the dose of Nifelat 30 LA PR considered.

ACE Inhibitors

Benazepril: In healthy volunteers receiving single dose of 20 mg Nifelat 30 LA PR ER and benazepril 10 mg, the plasma concentrations of benazeprilat and Nifelat 30 LA PR in the presence and absence of each other were not statistically significantly different. A hypotensive effect was only seen after co-administration of the two drugs. The tachycardic effect of Nifelat 30 LA PR was attenuated in the presence of benazepril.

Angiotensin-II Blockers

Irbesartan: In vitro studies show significant inhibition of the formation of oxidized irbesartan metabolites by Nifelat 30 LA PR. However, in clinical studies, concomitant Nifelat 30 LA PR had no effect on irbesartan pharmacokinetics.

Candesartan: No significant drug interaction has been reported in studies with candesartan cilexitil given together with Nifelat 30 LA PR. Because candesartan is not significantly metabolized by the cytochrome P450 system and at therapeutic concentrations has no effect on cytochrome P450 enzymes, interactions with drugs that inhibit or are metabolized by those enzymes would not be expected.

Beta-blockers

Nifelat 30 LA PR was well tolerated when administered in combination with beta-blockers in 187 hypertensive patients in a placebo-controlled clinical trial. However, there have been occasional literature reports suggesting that the combination Nifelat 30 LA PR and beta-adrenergic blocking drugs may increase the likelihood of congestive heart failure, severe hypotension or exacerbation of angina in patients with cardiovascular disease. Clinical monitoring is recommended and a dose adjustment of Nifelat 30 LA PR should be considered.

Timolol: Hypotension is more likely to occur if dihydropryridine calcium antagonists such as Nifelat 30 LA PR are co-administered with timolol.

Central Alpha1-Blockers

Doxazosin: Healthy volunteers participating in a multiple dose doxazosin-Nifelat 30 LA PR interaction study received 2 mg doxazosin q.d. alone or combined with 20 mg Nifelat 30 LA PR ER b.i.d. Co-administration of Nifelat 30 LA PR resulted in a decrease in AUC and Cmax of doxazosin to 83% and 86% of the values in the absence of Nifelat 30 LA PR, respectively. In the presence of doxazosin, AUC and Cmax of Nifelat 30 LA PR were increased by factors of 1.13 and 1.23, respectively. Compared to Nifelat 30 LA PR monotherapy, blood pressure was lower in the presence of doxazosin. Blood pressure should be monitored when doxazosin is co-administered with Nifelat 30 LA PR, and dose reduction of Nifelat 30 LA PR considered.

Digitalis

Digoxin: The simultaneous administration of Nifelat 30 LA PR and digoxin may lead to reduced clearance resulting in an increase in plasma concentrations of digoxin. Since there have been isolated reports of patients with elevated digoxin levels, and there is a possible interaction between digoxin and Nifelat 30 LA PR, it is recommended that digoxin levels be monitored when initiating, adjusting and discontinuing Nifelat 30 LA PR to avoid possible over- or under- digitalization.

Antithrombotics

Coumarins: There have been rare reports of increased prothrombin time in patients taking coumarin anticoagulants to whom Nifelat 30 LA PR was administered. However the relationship to Nifelat 30 LA PR therapy is uncertain.

Platelet Aggregation Inhibitors

Clopidogrel: No clinically significant pharmacodynamic interactions were observed when clopidrogrel was co-administered with Nifelat 30 LA PR.

Tirofiban: Co-administration of Nifelat 30 LA PR did not alter the exposure to tirofiban importantly.

Other

Diuretics, PDE5 inhibitors, alpha-methyldopa: Nifelat 30 LA PR may increase the blood pressure lowering effect of these concomitantly administered agents.

Non-Cardiovascular Drugs

Antifungal Drugs

Ketoconazole, itraconazole and fluconazole are CYP3A inhibitors and can inhibit the metabolism of Nifelat 30 LA PR and increase the exposure to Nifelat 30 LA PR during concomitant therapy. Blood pressure should be monitored and a dose reduction of Nifelat 30 LA PR considered.

Antisecretory Drugs

Omeprazole: In healthy volunteers receiving a single dose of 10 mg Nifelat 30 LA PR, AUC and Cmax of Nifelat 30 LA PR after pretreatment with omeprazole 20 mg q.d. for 8 days were 1.26 and 0.87 times those after pre-treatment with placebo. Pretreatment with or co-administration of omeprazole did not impact the effect of Nifelat 30 LA PR on blood pressure or heart rate. The impact of omeprazole on Nifelat 30 LA PR is not likely to be of clinical relevance.

Pantoprazole: In healthy volunteers the exposure to neither drug was changed significantly in the presence of the other drug.

Ranitidine: Five studies in healthy volunteers investigated the impact of multiple ranitidine doses on the single or multiple dose pharmacokinetics of Nifelat 30 LA PR. Two studies investigated the impact of co-administered ranitidine on blood pressure in hypertensive subjects on Nifelat 30 LA PR. Co-administration of ranitidine did not have relevant effects on the exposure to Nifelat 30 LA PR that affected the blood pressure or heart rate in normotensive or hypertensive subjects.

Cimetidine: Five studies in healthy volunteers investigated the impact of multiple cimetidine doses on the single or multiple dose pharmacokinetics of Nifelat 30 LA PR. Two studies investigated the impact of co-administered cimetidine on blood pressure in hypertensive subjects on Nifelat 30 LA PR. In normotensive subjects receiving single doses of 10 mg or multiple doses of up to 20 mg Nifelat 30 LA PR t.i.d. alone or together with cimetidine up to 1000 mg/day, the AUC values of Nifelat 30 LA PR in the presence of cimetidine were between 1.52 and 2.01 times those in the absence of cimetidine. The Cmax values of Nifelat 30 LA PR in the presence of cimetidine were increased by factors ranging between 1.60 and 2.02. The increase in exposure to Nifelat 30 LA PR by cimetidine was accompanied by relevant changes in blood pressure or heart rate in normotensive subjects. Hypertensive subjects receiving 10 mg q.d. Nifelat 30 LA PR alone or in combination with cimetidine 1000 mg q.d. also experienced relevant changes in blood pressure when cimetidine was added to Nifelat 30 LA PR. The interaction between cimetidine and Nifelat 30 LA PR is of clinical relevance and blood pressure should be monitored and a reduction of the dose of Nifelat 30 LA PR considered.

Cisapride: Simultaneous administration of cisapride and Nifelat 30 LA PR may lead to increased plasma concentrations of Nifelat 30 LA PR.

Antibacterial Drugs

Quinupristin/Dalfopristin: In vitro drug interaction studies have demonstrated that quinupristin/dalfopristin significantly inhibits the CYP3A metabolism of Nifelat 30 LA PR. Concomitant administration of quinupristin/dalfopristin and Nifelat 30 LA PR (repeated oral dose) in healthy volunteers increased AUC and Cmax for Nifelat 30 LA PR by factors of 1.44 and 1.18, respectively, compared to Nifelat 30 LA PR monotherapy. Upon co-administration of quinupristin/dalfopristin with Nifelat 30 LA PR, blood pressure should be monitored and a reduction of the dose of Nifelat 30 LA PR considered.

Erythromycin: Erythromycin, a CYP3A inhibitor, can inhibit the metabolism of Nifelat 30 LA PR and increase the exposure to Nifelat 30 LA PR during concomitant therapy. Blood pressure should be monitored and reduction of the dose of Nifelat 30 LA PR considered.

Antitubercular Drugs

Rifampin: Strong CYP3A inducers, such as rifampin, rifapentin, and rifabutin reduce the bioavailability of Nifelat 30 LA PR which may reduce the efficacy of Nifelat 30 LA PR; therefore Nifelat 30 LA PR should not be used in combination with strong CYP3A inducers such as rifampin. The impact of multiple oral doses of 600 mg rifampin on the pharmacokinetics of Nifelat 30 LA PR after a single oral dose of 20 mg Nifelat 30 LA PR capsule was evaluated in a clinical study. Twelve healthy male volunteers received a single oral dose of 20 mg Nifelat 30 LA PR capsule on study Day 1. Starting on study Day 2, the subjects received 600 mg rifampin once daily for 14 days. On study Day 15, a second single oral dose of 20 mg Nifelat 30 LA PR capsule was administered together with the last dose of rifampin. Compared to study Day 1, 14 days pretreatment with rifampin reduced Cmaxand AUC of concomitantly administered Nifelat 30 LA PR on average by 95% and 97%, respectively.

Antiviral Drugs

Amprenavir, atanazavir, delavirine, fosamprinavir, indinavir, nelfinavir and ritonavir, as CYP3A inhibitors, can inhibit the metabolism of Nifelat 30 LA PR and increase the exposure to Nifelat 30 LA PR. Caution is warranted and clinical monitoring of patients recommended.

CNS Drugs

Nefazodone, a CYP3A inhibitor, can inhibit the metabolism of Nifelat 30 LA PR and increase the exposure to Nifelat 30 LA PR during concomitant therapy. Blood pressure should be monitored and a reduction of the dose of Nifelat 30 LA PR considered.

Fluoxetine, a CYP3A inhibitor, can inhibit the metabolism of Nifelat 30 LA PR and increase the exposure to Nifelat 30 LA PR during concomitant therapy. Blood pressure should be monitored and a reduction of the dose of Nifelat 30 LA PR considered.

Valproic acid may increase the exposure to Nifelat 30 LA PR during concomitant therapy. Blood pressure should be monitored and a dose reduction of Nifelat 30 LA PR considered.

Phenytoin, Phenobarbital, and Carbamazepine: Nifelat 30 LA PR is metabolized by CYP3A. Co-administration of Nifelat 30 LA PR 10 mg capsule and 60 mg Nifelat 30 LA PR coat-core tablet with phenytoin, an inducer of CYP3A, lowered the AUC and Cmax of Nifelat 30 LA PR by approximately 70%. Phenobarbital and carbamazepine are also inducers of CYP3A. Alternative antihypertensive therapy should be considered in patients taking phenytoin, phenobarbital, and carbamazepine.

Antiemetic Drugs

Dolasetron: In patients taking dolasetron by the oral or intravenous route and Nifelat 30 LA PR, no effect was shown on the clearance of hydrodolasetron.

Immunosuppressive Drugs

Tacrolimus: Tacrolimus has been shown to be metabolized via the CYP3A system. Nifelat 30 LA PR has been shown to inhibit the metabolism of tacrolimus in vitro. Transplant patients on tacrolimus and Nifelat 30 LA PR required from 26% to 38% smaller doses than patients not receiving Nifelat 30 LA PR. Nifelat 30 LA PR can increase the exposure to tacrolimus. When Nifelat 30 LA PR is co-administered with tacrolimus the blood concentrations of tacrolimus should be monitored and a reduction of the dose of tacrolimus considered.

Sirolimus: A single 60 mg dose of Nifelat 30 LA PR and a single 10 mg dose of sirolimus oral solution were administered to 24 healthy volunteers. Clinically significant pharmacokinetic drug interactions were not observed.

Glucose Lowering Drugs

Pioglitazone: Co-administration of pioglitazone for 7 days with 30 mg Nifelat 30 LA PR ER administered orally q.d. for 4 days to male and female volunteers resulted in least square mean (90% CI) values for unchanged Nifelat 30 LA PR of 0.83 (0.73-0.95) for Cmax and 0.88 (0.80-0.96) for AUC relative to Nifelat 30 LA PR monotherapy. In view of the high variability of Nifelat 30 LA PR pharmacokinetics, the clinical significance of this finding is unknown.

Rosiglitazone: Co-administration of rosiglitazone (4 mg b.i.d.) was shown to have no clinically relevant effect on the pharmacokinetics of Nifelat 30 LA PR.

Metformin: A single dose metformin-Nifelat 30 LA PR interaction study in normal healthy volunteers demonstrated that co-administration of Nifelat 30 LA PR increased plasma metformin Cmax and AUC by 20% and 9%, respectively, and increased the amount of metformin excreted in urine. Tmax and half-life were unaffected. Nifelat 30 LA PR appears to enhance the absorption of metformin.

Miglitol: No effect of miglitol was observed on the pharmacokinetics and pharmacodynamics of Nifelat 30 LA PR.

Repaglinide: Co-administration of 10 mg Nifelat 30 LA PR with a single dose of 2 mg repaglinide (after 4 days Nifelat 30 LA PR 10 mg t.i.d. and repaglinide 2 mg t.i.d.) resulted in unchanged AUC and Cmax values for both drugs.

Acarbose: Nifelat 30 LA PR tends to produce hyperglycemia and may lead to loss of glucose control. If Nifelat 30 LA PR is co-administered with acarbose, blood glucose levels should be monitored carefully and a dose adjustment of Nifelat 30 LA PR considered.

Drugs Interfering with Food Absorption

Orlistat: In 17 normal-weight subjects receiving orlistat 120 mg t.i.d. for 6 days, orlistat did not alter the bioavailability of 60 mg Nifelat 30 LA PR (extended release tablets).

Dietary Supplements

Grapefruit Juice: In healthy volunteers, a single dose co-administration of 250 mL double strength grapefruit juice with 10 mg Nifelat 30 LA PR increased AUC and Cmax by factors of 1.35 and 1.13, respectively. Ingestion of repeated doses of grapefruit juice (5 x 200 mL in 12 hours) after administration of 20 mg Nifelat 30 LA PR ER increased AUC and Cmax of Nifelat 30 LA PR by a factor of 2. Grapefruit juice should be avoided by patients on Nifelat 30 LA PR. The intake of grapefruit juice should be stopped at least 3 days prior to initiating patients on Nifelat 30 LA PR.

Herbals

St. John’s Wort: St. John’s Wort is an inducer of CYP3A and may decrease exposure to Nifelat 30 LA PR. Alternative antihypertensive therapy should be considered in patients in whom St. John’s Wort therapy is necessary.

CYP2D6 Probe Drug

Debrisoquine: In healthy volunteers, pretreatment with Nifelat 30 LA PR 20 mg t.i.d. for 5 days did not change the metabolic ratio of hydroxydebrisoquine to debrisoquine measured in urine after a single dose of 10 mg debrisoquine. Thus, it is improbable that Nifelat 30 LA PR inhibits in vivo the metabolism of other drugs that are substrates of CYP2D6.

Carcinogenesis, Mutagenesis, Impairment of Fertility

Nifelat 30 LA PR was administered orally to rats for two years and was not shown to be carcinogenic. When given to rats prior to mating, Nifelat 30 LA PR caused reduced fertility at a dose approximately 30 times the maximum recommended human dose. There is a literature report of reversible reduction in the ability of human sperm obtained from a limited number of infertile men taking recommended doses of Nifelat 30 LA PR to bind to and fertilize an ovum in vitro. In vivo mutagenicity studies were negative.

Pregnancy

Pregnancy Category C.

In rodents, rabbits and monkeys, Nifelat 30 LA PR has been shown to have a variety of embryotoxic, placentotoxic, teratogenic and fetotoxic effects, including stunted fetuses (rats, mice and rabbits), digital anomalies (rats and rabbits), rib deformities (mice), cleft palate (mice), small placentas and underdeveloped chorionic villi (monkeys), embryonic and fetal deaths (rats, mice and rabbits), prolonged pregnancy (rats; not evaluated in other species), and decreased neonatal survival (rats; not evaluated in other species). On a mg/kg or mg/m2 basis, some of the doses associated with these various effects are higher than the maximum recommended human dose and some are lower, but all are within an order of magnitude of it.

The digital anomalies seen in Nifelat 30 LA PR-exposed rabbit pups are strikingly similar to those seen in pups exposed to phenytoin, and these are in turn similar to the phalangeal deformities that are the most common malformation seen in human children with in utero exposure to phenytoin.

From the clinical evidence available, a specific prenatal risk has not been identified. However, an increase in perinatal asphyxia, caesarean delivery, prematurity and intrauterine growth retardation have been reported.

Careful monitoring of blood pressure must be exercised in pregnant women, when administering Nifelat 30 LA PR in combination with IV magnesium sulfate due to the possibility of an excessive fall in blood pressure which could harm the mother and fetus.

There are no adequate and well-controlled studies in pregnant women.

Nursing Mothers

Nifelat 30 LA PR is excreted in human milk. Nursing mothers are advised not to breastfeed their babies when taking the drug.

Pediatric Use

The safety and effectiveness of Nifelat 30 LA PR in pediatric patients have not been established.

Geriatric Use

Although small pharmacokinetic studies have identified an increased half-life and increased Cmax and AUC, clinical studies of Nifelat 30 LA PR 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 of concomitant disease or other drug therapy.

Patients with Galactose Intolerance

Since this medicinal product contains lactose, patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.

What happens if I miss a dose of Nifelat 30 LA PR?

Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.



References

  1. DailyMed. "NIFEDIPINE: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
  2. DrugBank. "nifedipine". http://www.drugbank.ca/drugs/DB01115 (accessed September 17, 2018).
  3. MeSH. "Vasodilator Agents". https://www.ncbi.nlm.nih.gov/mesh/68... (accessed September 17, 2018).

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