Mytensa

Losartan Potassium, Amlodipine Besilate.

Each film-coated tablet contains: Losartan potassium 50 mg, Amlodipine (as Besilate) 5 mg.

Pharmacological classification: Vasodilators, hypotensive medicines.
Pharmacology: Pharmacodynamics: Losartan: Losartan and its principal active metabolite block the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor found in many tissues (e.g., vascular smooth muscle, adrenal gland). Both Losartan and its principal active metabolite do not exhibit any partial agonist activity at the AT1 receptor and have much greater affinity (about 1000-fold) for the AT1 receptor than theAT2 receptor.
Amlodipine: Amlodipine inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle. Experimental data suggest that Amlodipine binds to both dihydropyridine and nondihydropyridine binding sites. The contractile processes of cardiac muscle and vascular smooth muscle are dependent upon the movement of extracellular calcium ions into these cells through specific ion channels. Amlodipine inhibits calcium ion influx across cell membranes selectively, with a greater effect on vascular smooth muscle cells than on cardiac muscle cells. Amlodipine is a peripheral arterial vasodilator that acts directly on vascular smooth muscle to cause a reduction in peripheral vascular resistance and reduction in blood pressure.
Pharmacokinetics: Absorption: Amlodipine: Plasma levels peak 6-12 hrs after oral administration; absolute bioavailability is estimated to be 64-90%.
Losartan: Well absorbed; undergoes substantial 1st pass metabolism by CYP450 enzymes; systemic bioavailability is about 33%; about 14% of an oral dose is converted to active metabolites.
Distribution: Amlodipine: 93% bound to plasma proteins.
Losartan and its active metabolites: Highly bound to plasma proteins, mainly albumin.
Metabolism: Amlodipine: About 90% converted to inactive metabolites hepatically.
Losartan: Metabolized to an active carboxylic acid metabolite E-3174 (EXP-3174), which has greater pharmacological activity than losartan; some inactive metabolites are also formed.
Excretion: Amlodipine: 10% of parent compound and 60% of the metabolites are removed in the urine; elimination from the plasma is biphasic with terminal half-life of about 30-50 hrs.
Losartan and its active metabolites: Biliary excretion; terminal half-life: About 2 hrs (Losartan) and 6-9 hrs (metabolites).

Losartan potassium/Amlodipine besilate (Mytensa) is indicated for the treatment of hypertension, angina pectoris and mild to moderate hypertension, alone or in combination with other antihypertensives.

The usual starting and maintenance dose is one tablet once daily for most patients. The dose may be increased to 2 tablets once daily. A lower dose should be considered for patients with a history of hepatic impairment. Or as prescribed by the physician.

Hypotension, tachycardia and bradycardia could occur from parasympathetic (vagal) stimulation. Neither Losartan potassium/Amlodipine besilate (Mytensa) nor the active metabolite can be removed by haemodialysis.
Gastric lavage may be of benefit. Intravenous calcium gluconate may be of benefit reversing the effects of calcium channel blockade.

Losartan potassium/Amlodipine besilate (Mytensa) during pregnancy and lactation is contraindicated. Safety and efficacy has not been established in children. Hypersensitivity to any of the ingredients and dihydropyridines.

Losartan potassium/Amlodipine besilate (Mytensa) is contraindicated in pregnancy and should be used with care, at all, during breastfeeding. Losartan potassium/Amlodipine besilate (Mytensa) should be used with caution in patients with bilateral renal artery stenosis or stenosis of an artery to single kidney, aortic valve stenosis, and hypertrophic obstructive cardiomyopathy. Symptomatic hypotension may occur after initiation of Losartan potassium/Amlodipine besilate (Mytensa). Reduced doses must be considered in patients with hepatic impairment.
Use in Renal Failure: Severe renal impairment, may however, require a dosage reduction. Amlodipine is not dialyzable.
Use in lmpaired Hepatic Function: Losartan potassium/Amlodipine besilate (Mytensa) should be administered at lower doses in these patients.
Use in Heart Failure: Losartan potassium/Amlodipine besilate (Mytensa) may increase in patients with heart failure.
Porphyria: Safety has not been established.
Use in Children: Safety and efficacy has not been established.
Use in the Elderly: Elderly patients should start Losartan potassium/Amlodipine besilate (Mytensa) therapy at a lower dose.

Use in pregnancy: Drugs that act directly on the RAAS can cause fetal and neonatal morbidity and death when administered to pregnant women. When pregnancy is detected, this combination of Losartan and Amlodipine should be discontinued as soon as possible. Oligohydramnios has also been reported, presumably reporting from decreased fetal renal function.
Use in lactation: It is not known whether Losartan or Amlodipine is excreted in human milk. In the absence of this information, it is recommended that nursing may be discontinued while the combination is administered.

Most Common: Edema, dizziness, flushing, and palpitation.
Common: Fatigue, nausea, abdominal pain, somnolence.
Other Adverse Effects: Cardiovascular: Arrhythmia (including ventricular tachycardia and atrial fibrillation), bradycardia, chest pain, peripheral ischemia, syncope, tachycardia, vasculitis.
Central and Peripheral Nervous System: Hypoesthesia, peripheral neuropathy, paresthesia, tremor, vertigo.
Gastrointestinal: Anorexia, constipation, dysphagia, diarrhea, flatulence, pancreatitis, vomiting, gingival hyperplasia.
General: Allergic reaction, asthenia, back pain, hot flushes, malaise, pain, rigors, weight decrease.
Musculoskeletal System: Arthralgia, arthritis, muscle cramps, myalgia.
Psychiatric: Sexual dysfunction (male and female), insomnia, nervousness, depression, abnormal dreams, anxiety, depersonalization.
Respiratory System: Dyspnea, epistaxis.
Skin and Appendages: Angioedema, erythema multiforme, pruritus, rash, rash erythematous, rash maculopapular.
Special Senses: Abnormal vision, conjunctivitis, diplopia, eye pain, tinnitus.
Urinary System: Micturition frequency, micturition disorder, nocturia.
Autonomic Nervous System: Dry mouth, sweating increased.
Metabolic Nutritional: Hyperglycemia, thirst.
Hematopoietic: Leukopenia, purpura, thrombocytopenia.

Non-steroidal anti-inflammatory drugs (NSAIDs) may antagonize the antihypertensive effect. Concurrent use with sympathomimetics may reduce the antihypertensive effect. Potassium-sparing diuretics may lead to elevation of serum potassium. Concurrent administration of sublingual nitroglycerin, long-acting nitrates, beta-blockers or other antianginal agents with Amlodipine may produce additive antihypertensive and anti-anginal effects.

Store at temperatures not exceeding 30°C.

Angiotensin II Antagonists / Calcium Antagonists

C09DB06 - losartan and amlodipine ; Belongs to the class of angiotensin II receptor blockers (ARBs) and calcium channel blockers. Used in the treatment of cardiovascular disease.

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