Composition:Each tablet contains Amlodipine 5 mg.Chemistry:(R,S) 3-ethyl-5- methyl -2 -(2 - aminoethoxymethyl )- 4 - ( 2 - chlorophenyl )-1,4 - dihydro - 6-methyl-3,5 -pyridinedicarboxylate benzenesulphonate.C20H25CIN2O5 . C6H6O3S M.W = 567.1 (PDR 2002)Mechanism of action:Vazodipine is dihydropyridine calcium antagonist (calcium ion antagonist or slow channel blocker) that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle. Vazodipine inhibits calcium ion influx across cell membranes selectively, with a greater effect on vascular smooth muscle cells than on cardiac muscle cells. Negative inotropic effects can be detected invitro but such effects have not been seen in intact animals at therapeutic doses. Vazodipine is a peripheral arterial vasodilator that acts directly on vascular smooth muscle to cause a reduction in blood pressure. (PDR 2002)Pharmacokinetics:Absorption: Slowly and almost completely absorbed from the gastrointestinal tract, absorption not affected by food. Bioavailability is approximately 60 to 65%. (USP DI 2002)Volume of distribution:21 L per kg. (USP DI 2002)Protein binding:Very high (95 to 98%) (USP DI 2002)Biotransformation:Undergoes for minimal presystemic metabolism. Vazodipine undergoes slow but extensive hepatic metabolism, producing metabolites lacking significant pharmacological activity. (USP DI 2002)Half life:Elimination - Mean, 35 hours in healthy volunteers, may be prolonged to a mean of 48 hours in hypertensive patients, 65 hours in the elderly, and 60 hours in patients with hepatic function impairment. Not affected by renal function impairment. (USP DI 2002)Time to peak concentration:Single dose - 6 to 9 hours. (USP DI 2002)Duration of action:24 hours. (USP DI 2002)Elimination:Renal - 59 to 62 % (about % 5 as unchanged Amlodipine).Biliary/ fecal - 20 to 25 %.In dialysis - Vazodipine is not removed by hemodialysis. (USP DI 2002)Indications:1- Hypertension: Vazodipine is indicated for the treatment of hypertension. It may be used alone or in combination with other antihypertensive agents. (PDR 2002)2- Chronic stable angina: Vazodipine is indicated for the treatment of chronic stable angina. It may be used alone or in combination with other antianginal agents. (PDR 2002)3- Vasospastic angina (Prinzmetal's or variant angina): Vazodipine is indicated for the treatment of confirmed or suspected vasospastic angina. It may be used as monotherapy or in combination with other antianginal agents. (PDR 2002)Contraindications:Vazodipine is contraindicated in patients with known sensitivity to it. (PDR 2002)Warnings:Increased angina and/ or myocardial infarction:Rarely, patients, particularly those with severe obstructive coronary artery disease,have developed documented increased frequnecy, duration and / or severity of angina or acute myocardial infarction on starting calcium channel blocker therapy or at the time of dosage increase. The mechanism of this effect has not been elucidated. (PDR 2002)Pregnancy:Pregnancy category CVazodipine has been shown to prolong both the gestation period and the duration of labor in rats. There are no adequate and well - controlled studies in pregnant women.Vazodipine should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. (PDR 2002)Nursing mothers:It is not known whether Vazodipine is excreted in human milk. In the absence of this information, it is recommended that nursing be discontinued while Vazodipine is administered. (PDR 2002)Pediatric use:Safety and effectiveness of Vazodipine in children have not been established. (PDR 2002)Precautions:Except under special circumstances, this medication should not be used when the following medical problem exists:-Severe hypotension (Vazodipine may aggravate this condition).Risk- benefit should be considered when the following medical problems exist:-Aortic stenosis (increased risk of heart failure because of fixed impedance to flow across aortic valve).-Congestive heart failure (Vazodipine should be used with caution in patients with congestive heart failure because of the slight risk for negative inotropic effect).-Hepatic function impairment (clearance of Vazodipine may be reduced since it undergoes extensive hepatic metabolism, elimination half life may be prolonged to 60 hours).-Sensitivity to Amlodipine.-Risk of gingival hyperplasia. (USP DI 2002)Drug interactions:The following drug interactions have been selected on the basis of their potential clinical significance, not necessarily inclusive:• Anesthetics, hydrocarbon inhalation ( concurrent use with Vazodipine may produce additive hypotension, although calcium channel blocking agents may be useful to prevent supraventricular tachycardias, hypertension, or coronary spasm during surgery, caution is recommended during use).• Anti - inflammatory drugs, nonsteroidal (NSAIDs), especially indomethacin (may reduce the antihypertensive effects of Vazodipine by inhibiting renal prostaglandin synthesis and causing sodium and fluid retention).• Beta-adrenergic blocking agents (although reports of adverse effects resulting from concurrent use of Vazodipine with the beta - adrenergic blocking agents are lacking, caution is recommended given the similarity of Vazodipine to nifedipine, concurrent use of nifedipine with the beta - adrenergic blocking agents, although usually well- tolerated, may produce excessive hypotension and, in rare cases, may increase the possibility of congestive heart failure.• Estrogens (estrogen - induced fluid retention may tend to increase blood pressure, the patient should be carefully monitored to confirm that the desired effect is being obtained. - Highly protein - bound medications, such as:• Anticonvulsants, hydantoin.• Anticoagulants, coumarin- and indandione - derivatives.• Anti - inflammatory drugs, nonsteroidal.Quinine, salicylates, sulfinpyrazone.(caution is advised when these medications are used concurrently with Vazodipine since Vazodipine is highly protein bound changes in serum concentrations of the free unbound medications may occur).• Hypotension-producing medications: (antihypertensive effects may be potentiated when Vazodipine is used concurrently with hypotension - producing medications, when any of these medications are used concurrently, dosage adjustments may be neccessary.• Lithium (concurrent use with Vazodipine potentially may result in neurotoxicity in the form of nausea, vomiting, diarrhea, ataxia, tremors, and tinnitus, caution is recommended).• Sympathomimetics (concurrent use may reduce antihypertensive effects of Vazodipine, the patient should be carefully monitored to confirm that the desired effect is being obtained). (USP DI 2002)Adverse effects:The following adverse effects have been selected on the basis of their potential clinical significance- not necessarily inclusive:Those indicating need for medical attention:Incidence more frequent: Edema peripheral (swelling of ankles and feet).Incidence less frequent: Dizziness, palpitation.Incidence rare: Angina (chest pain), bradycardia, hypotension, jaundice, orthostatic hypotension.Those indicating need for medical attention only if they continue or are bothersome:Incidence more frequent: Abdominal pain, flushing, headache, somnolence.Incidence less frequent: Fatigue, nausea. (USP DI 2002)Dosage and administration:Usual adult dose:Chronic stable angina, vasospastic angina or hypertension:Oral, 5 to 10 mg once a day.Note: An initial antihypertensive dose of 2.5 mg is recommended for small, fragile, or elderly patients, patients with hepatic function impairment, or when adding Vazodipine to other antihypertensive therapy. An initial antianginal dose of 5 mg is recommended for the elderly and for patients with hepatic function impairment .Usual pediatric dose:Safety and efficacy have not been established. (USP DI 2002)Storage:Store at controlled room temperature between 15 and 30°C in a tight,light-resistant container. (USP DI 2002)How supplied:Vazodipine, 5 mg, is available as white barrel- shaped scored tablet in 3 blisters each contains 10 tablets in a box.
Use logical operators AND, OR, NOT (In Upper case) for Advance Search.
Ex : Niro AND Tehran , Iran OR Investment