about Nifedipine class, uses, side effects contraindications
Nifedipine
Short Description
Nifedipine is one of the most common medicines used to treat?heart conditions?and high blood pressure. It belongs to a family of medicines called calcium channel blockers.
Nifedipine is mainly used to treat??high blood pressure,??especially by long-acting tablets, and to treat??angina pectoris??, especially for the treatment of angina caused by coronary artery spasm and patients with heart failure. Nifedipine is also used as an ointment to treat anal fissures.
Category
Chemical class: Dihydropyridine derivative
Therapeutic class: Antianginal, antihypertensive
Pregnancy category: C
Indications
To manage angina
Adults. Initial: 10 mg t.i.d., increased over 1 to 2 wk as needed. Maintenance: 10 to 20 mg t.i.d. Maximum: 180 mg daily, 30 mg/dose.
Adults. Initial: 30 to 60 mg daily, increased or decreased over 7 to 14 days based on patient response. Maximum: 90 mg daily. To manage hypertension (ADALAT CC)
Adults. Initial: 30 mg daily. Maintenance: 30 to 60 mg daily, increased or decreased over 7 to 14 days based on patient response. Maximum: 90 mg daily. (ADALAT PA)
Adults. Initial: 10 to 20 mg b.i.d., increased every 3 wk based on patient response. Maintenance: 20 mg b.i.d. Maximum: 80 mg daily. (ADALAT XL)
Adults. Initial: 30 to 60 mg daily, increased or decreased over 7 to 14 days based on patient response. Maintenance: 60 to 90 mg daily. Maximum: 120 mg daily.
Adults. 30 to 60 mg daily, increased or decreased over 7 to 14 days based on patient response. Maximum: 120 mg daily.
DOSAGE ADJUSTMENT Dosage may be reduced for elderly patients and those with heart failure or impaired hepatic or renal function. Route Onset Peak Duration P.O. (caps) 20 min Unknown Unknown
Mechanism of Action
May slow movement of calcium into myocardial and vascular smooth-muscle cells by deforming calcium channels in cell membranes, inhibiting ion-controlled gating mechanisms, and disrupting calcium release from sarcoplasmic reticulum. Decreasing intracellular calcium level inhibits smooth-muscle cell contraction and dilates arteries, which decreases myocardial oxygen demand, peripheral resistance, blood pressure, and afterload.
Contraindications
Hypersensitivity to a calcium channel blocker, secondor third-degree AV block without artificial pacemaker, sick sinus syndrome
Interactions
anesthetics (hydrocarbon inhalation): Possibly hypotension antiviral , cimetidine, dalfopristin, diltiazem, erythromycin, fluconazole, itraconazole, ketoconazole, nefazodone, other antihypertensives, prazocin, quinupristin, timolol, valproic acid, verapamil: Increased risk of hypotension benazepril: Possibly increased heart rate and hypotensive effect
beta blockers: Increased risk of profound hypotension, heart failure, and worsening of angina calcium supplements: Possibly interference with action of nifedipine carbamazepine, NSAIDs, phenobarbitone, phenytoin, rifampin, rifapentine, St. John’s wort, sympathomimetics: Possibly decreased therapeutic effects of nifedipine digoxin: Transiently increased blood digoxin level, increased risk of digitalis toxicity disopyramide, flecainide: Increased risk of bradycardia, conduction defects, and heart failure doxazocin: Decreased doxazocin effectiveness; increased nifedipine effectiveness estrogens: Possibly increased fluid retention and decreased nifedipine effects lithium: Increased risk of neurotoxicity metformin: Increased metformin absorption and plasma level tacrolimus: Decreased tacrolimus metabolism grapefruit, grapefruit juice: Possibly increased bioavailability of nifedipine high-fat meals: Possibly delayed nifedipine absorption
alcohol use: Additive hypotensive effect
Side Efect
CNS: Anxiety, ataxia, confusion, dizziness, drowsiness, headache, nervousness (possibly extreme), nightmares, paresthesia, psychiatric disturbance, syncope, tremor, weakness
CV: Arrhythmias (bradycardia, tachycardia), chest pain, heart failure, hypotension, palpitations, peripheral edema
EENT: Altered taste, blurred vision, dry mouth, epistaxis, gingival hyperplasia, nasal congestion, pharyngitis, sinusitis, tinnitus
ENDO: Gynecomastia, hyperglycemia
GI: Anorexia, constipation, diarrhea, dyspepsia, elevated liver function test results, hepatitis, nausea, vomiting
GU: Dysuria, nocturia, polyuria, sexual dysfunction, urinary frequency
HEME: Anemia, leukopenia, positive Coombs’ test, thrombocytopenia
MS: Joint stiffness, muscle cramps
RESP: Chest congestion, cough, dyspnea, respiratory tract infection, wheezing
SKIN: Dermatitis, diaphoresis, erythema multiforme, flushing, photosensitivity, pruritus, rash, urticaria
Cautions
When starting and stopping nifedipine therapy, taper it, as prescribed, over 7 to 14 days. For closely monitored hospitalized patient with angina,dosage may be increased 10 mg every 4 to 6 hours to control chest pain. Because of drug’s negative inotropic effect on some patients, frequently monitor heart rate and rhythm and blood pressure in patients who take a beta blocker or have heart failure or significant left ventricular dysfunction. Monitor fluid intake and output and daily weight; fluid retention may lead to heart failure. Also assess for signs of heart failure, such as crackles, dyspnea, jugular vein distention, peripheral edema, and weight gain. PATIENT SAFTY
Instruct patient to swallow tablets whole, not to crush, chew, or break them. Inform her that their empty shells may appear in stool. Urge patient to take nifedipine exactly as prescribed, even when she’s feeling well. Advise her to notify prescriber if she misses two or more doses. Urge patient not to take drug within 1 hour of a high-fat meal or grapefruit. Urge her not to alter the amount of grapefruit in her diet without consulting prescriber.
WARNING Caution patient against stopping nifedipine abruptly because angina or dangerously high blood pressure could result. Teach patient to measure pulse rate and blood pressure, and advise her to call prescriber if they drop below accepted levels. Suggest keeping a log of weekly measurements and taking it to follow-up visits. Instruct patient to notify prescriber immediately about chest pain, difficulty breathing, ringing in ears, and swollen gums. Advise patient to avoid hazardous activities until drug’s CNS effects are known. Urge patient to avoid alcoholic beverages because they may worsen dizziness, drowsiness, and hypotension. Teach patient to minimize constipation by increasing her intake of fluids, if allowed, and dietary fiber. Emphasize the need to comply with prescribed lifestyle changes, such as alcohol moderation, low-fat or low-sodium diet, regular exercise, smoking cessation, stress reduction, and weight reduction. Stress the need for good oral hygiene and regular dental visits. Caution patient that hot tubs, saunas, and prolonged hot showers may cause dizziness and fainting. Advise patient to avoid prolonged sun exposure and to wear sunscreen outdoors.
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effect of Nifedipine in Pregnancy, Fetal Health
and Breast feeding
Pregnancy
. Hypertension during pregnancy: Hypertension remains a significant cause of maternal and fetal morbidity and death. Severe hypertension during Pregnancy
(BP >170/110mmHg) should be treated immediately to improve both maternal and fetal outcome. An uncontrolled reduction in BP may lead to coma, stroke, MI, acute renal failure, and death. Treatment of an acute hypertensive episode during Pregnancy
further complicates the process because an acute decrease in BP might adversely affect the fetus. Thus, the goal is not just to decrease BP, but to do so with minimal adverse effects while preserving organ function. Nifedipine is proven safe and effective. The antihypertensive effect of nifedipine does not correlate with the serum concentration. Given PO or SL, nifedipine (8-10mg ?1) has a longer duration of action and is more effective than either IV hydralazine (5- 10mg ?1) or IV labetolol (20mg ?1). In randomized trials, nifedipine retard was as effective as the rapidly acting formuation, though women given the retard form required a 2nd dose more frequently. One approach is to observe the patient 24h to learn the proper timing of nifedipine. This is based on the observation that hypertension is more pronounced at night in women with preeclampsia compared to chronic hypertension. Maternal cerebral blood flow is influenced by antihypertensive treatment. A reduction in middle cerebral artery flow velocities after nifedipine and methyldopa confirms that cerebral vasospasm occurs in preeclamptic women. In contrast to the middle cerebral artery, there is no change in uteroplacental Doppler-determined resistances in severe preeclamptic women treated with nifedipine. Preterm labor: No tocolytic agent actually stops preterm labor or alone improves perinatal outcome. Tocolysis changes perinatal outcome by allowing time for corticosteroid administration. When compared to placebo and any other tocolytic agent, calcium channel blockers and specifically nifedipine reduce the number of women giving birth within 48h or 7d of diagnosis. The doses used ranged widely from 30 to 240mg/d until contractions stop; 40mg PO q4-6h seem the typical starting dose. Like all other tocolytic agents, maintenance use offers no added benefit. The frequency of drug discontinuation for adverse effects is also dramatically reduced for nifedipine compared to all other tocolytic agents. In steady state, the mean nifedipine plasma concentration to achieve tocolysis is about the half of that measured after initial tocolysis. The use of nifedipine with magnesium sulfate is potentially dangerous; the combination is more frequently associated with severe hypotension, neuromuscular blockade, and cardiac depression. Similar to all other agents, maintenance therapy with oral nifedipine after the successful treatment of presumed preterm labor does not alter the timing of delivery. Several case reports note the occurrence of acute MI during the use of nifedipine for tocolysis. A short interval between cessation of b-mimetic therapy and the start of nifedipine may have had a role. Recently, a relationship 785 between oral erythromycin and sudden cardiac death was reported in patients also receiving strong inhibitors of CYP3A such as nitroimidazole antifungal agents, diltiazem, verapamil, and troleandomycin; each doubles, at least, the AUC for a CYP Breastfeeding
Nifedipine is excreted into human breast milk, achieving an M:P ratio approximating 0.3. It is unlikely the nursing newborn would ingest a clinically relevant amount.
the follwing drugs will increse Nifedipine by inhepiting cyp450
amiodarone ; aprepitant ; atomoxetine ; boceprevir ; ceritinib ; chloramphenicol ; cimetidine ; ciprofloxacin ; clarithromycin ; crizotinib ; delaviridine ; diethyl-dithiocarbamate ; diltiazem ; entrectinib ; erythromycin ; esomeprazole ; fluconazole ; fluvoxamine ; gestodene ; grapefruit juice ; idelalisib ; imatinib ; indinavir ; itraconazole ; ivacaftor ; ketoconazole ; lesinurad ; letermovir ; mibefradil ; mifepristone ; nefazodone ; nelfinavir ; netupitant/palonosetron ; norfloxacin ; norfluoxetine ; omeprazole ; pantoprazole ; perampanel ; quercetin ; regorafenib ; ribociclib ; ritonavir ; rucaparib ; saquinavir ; simeprevir ; starfruit ; telaprevir ; telithromycin ; ticagrelor ; tucatinib ; verapamil ; voriconazole ;
the follwing drugs will decrease Nifedipine by inhancing cyp450
barbiturates ; brigatinib ; carbamazepine ; clobazam ; dabrafenib ; efavirenz ; elagolix ; enzalutamide ; eslicarbazepine ; glucocorticoids ; letermovir ; lorlatinib ; modafinil ; nevirapine ; oxcarbazepine ; perampanel ; phenobarbital ; phenytoin ; pioglitazone ; rifabutin ; rifampin ; St. John's Wort ; telotristat ; troglitazone ; vemurafenib ;
trad drugs based on Nifedipine
| Gen name | Trade name | Catagory name |
| nifedipine | Adalat | Calcium channel blocking agents |
| nifedipine | Adalat CC | Calcium channel blocking agents |
| nifedipine | Afeditab CR | Calcium channel blocking agents |
| nifedipine | Nifediac CC | Calcium channel blocking agents |
| nifedipine | Nifedical XL | Calcium channel blocking agents |
| nifedipine | Procardia | Calcium channel blocking agents |
| nifedipine | Procardia XL | Calcium channel blocking agents |
| Nifedipine | ADALAT 30MG LA TAB | |
| Nifedipine | ADALAT 60MG LA TAB | |
| Nifedipine | ADALAT RETARD 20MG TABS | |
| Nifedipine | Angilat 10 Tablets | |
| Nifedipine | Angilat 20 Tablets | |
| Nifedipine | EPILAT 10MG CAPS | |
| Nifedipine | NIF-TEN CAPS | |
| Nifedipine | NOVO-NIFEDIN 10MG CAPS. | |
other drugs from same cataogory
| Gen name | trade name | catogry |
| amlodipine | Norvasc | Calcium channel blocking agents |
| diltiazem | Cartia XT | Calcium channel blocking agents |
| diltiazem | Cardizem | Calcium channel blocking agents |
| verapamil | Calan SR | Calcium channel blocking agents |
| diltiazem | Cardizem CD | Calcium channel blocking agents |
| nifedipine | Adalat | Calcium channel blocking agents |
| nifedipine | Procardia | Calcium channel blocking agents |
| nifedipine | Nifedical XL | Calcium channel blocking agents |
| verapamil | Calan | Calcium channel blocking agents |
| verapamil | Verelan PM | Calcium channel blocking agents |
| diltiazem | Tiazac | Calcium channel blocking agents |
| nifedipine | Procardia XL | Calcium channel blocking agents |
| verapamil | Isoptin SR | Calcium channel blocking agents |
| diltiazem | Dilt-XR | Calcium channel blocking agents |
| verapamil | Verelan | Calcium channel blocking agents |
| nisoldipine | Sular | Calcium channel blocking agents |
| felodipine | Plendil | Calcium channel blocking agents |
| nimodipine | Nimotop | Calcium channel blocking agents |
| diltiazem | Cardizem LA | Calcium channel blocking agents |
| nifedipine | Adalat CC | Calcium channel blocking agents |
| diltiazem | Taztia XT | Calcium channel blocking agents |
| nifedipine | Nifediac CC | Calcium channel blocking agents |
| isradipine | DynaCirc CR | Calcium channel blocking agents |
| diltiazem | Dilacor XR | Calcium channel blocking agents |
| verapamil 1 review | Covera-HS | Calcium channel blocking agents |
| nimodipine | Nymalize | Calcium channel blocking agents |
| diltiazem | Matzim LA | Calcium channel blocking agents |
| isradipine | Dynacirc | Calcium channel blocking agents |
| diltiazem | Diltia XT | Calcium channel blocking agents |
| levamlodipine | Conjupri | Calcium channel blocking agents |
| nicardipine | Cardene SR | Calcium channel blocking agents |
| nicardipine | Cardene IV | Calcium channel blocking agents |
| nifedipine | Afeditab CR | Calcium channel blocking agents |
| diltiazem | Tiadylt ER | Calcium channel blocking agents |
| amlodipine | Norliqva | Calcium channel blocking agents |
| amlodipine | Katerzia | Calcium channel blocking agents |
| diltiazem | Diltzac | Calcium channel blocking agents |
| clevidipine | Cleviprex | Calcium channel blocking agents |
| nicardipine | Cardene | Calcium channel blocking agents |