Products & Portfolio (5)
FROVATRIPTAN SUCCINATE
frovatriptan succinate
Post-LOE
ORAL · TABLET
5-HT 1B/1D receptors. The therapeutic activity of frovatriptan succinate is thought to be due to the agonist effects at the 5-HT 1B/1D receptors on intracranial blood vessels (including the arterio-venous anastomoses) and sensory nerves of the trigeminal system which result in cranial vessel constriction and inhibition of pro-inflammatory neuropeptide release.
migraine attackscluster headache ( )migraine
2022
30
METOLAZONE
metolazone
Post-LOE
ORAL · TABLET
CLINICAL PHARMACOLOGY Metolazone is a quinazoline diuretic, with properties generally similar to the thiazide diuretics. The actions of metolazone result from interference with the renal tubular mechanism of electrolyte reabsorption. Metolazone acts primarily to inhibit sodium reabsorption at the cortical diluting site and to a lesser extent in the proximal convoluted tubule. Sodium and chloride ions are excreted in approximately equivalent amounts. The increased delivery of sodium to the distal tubular exchange site results in increased potassium excretion. Metolazone does not inhibit carbonic anhydrase. A proximal action of metolazone has been shown in humans by increased excretion of phosphate and magnesium ions and by a markedly increased fractional excretion of sodium in patients with severely compromised glomerular filtration. This action has been demonstrated in animals by micropuncture studies. When metolazone tablets, are given, diuresis and saluresis usually begin within one hour and may persist for 24 hours or more. For most patients, the duration of effect can be varied by adjusting the daily dose. High doses may prolong the effect. A single daily dose is recommended. When a desired therapeutic effect has been obtained, it may be possible to reduce dosage to a lower maintenance level. The diuretic potency of metolazone tablets, at maximum therapeutic dosage is approximately equal to thiazide diuretics. However, unlike thiazides, metolazone tablets, may produce diuresis in patients with glomerular filtration rates below 20 mL/min. Metolazone tablets, and furosemide administered concurrently have produced marked diuresis in some patients where edema or ascites was refractory to treatment with maximum recommended doses of these or other diuretics administered alone. The mechanism of this interaction is unknown (see and , ). Maximum blood levels of metolazone are found approximately eight hours after dosing. A small fraction of metolazone is metabolized. Most of the drug is excreted in the unconverted form in the urine.
saltwater retention including: • edema accompanying congestive heart failurehypertension+5 more
2022
30
METOPROLOL TARTRATE
metoprolol tartrate
Post-LOE
ORAL · TABLET
1 -selective (cardioselective) adrenergic receptor blocking agent. This preferential effect is not absolute, however, and at higher plasma concentrations, metoprolol also inhibits beta 2 -adrenoreceptors, chiefly located in the bronchial and vascular musculature. Metoprolol has no intrinsic sympathomimetic activity, and membrane-stabilizing activity is detectable only at plasma concentrations much greater than required for beta-blockade. Animal and human experiments indicate that metoprolol slows the sinus rate and decreases AV nodal conduction. The relative beta 1 -selectivity of metoprolol has been confirmed by the following: (1) In normal subjects, metoprolol is unable to reverse the beta 2 -mediated vasodilating effects of epinephrine. This contrasts with the effect of nonselective beta-blockers, which completely reverse the vasodilating effects of epinephrine. (2) In asthmatic patients, metoprolol reduces FEV 1 and FVC significantly less than a nonselective beta-blocker, propranolol, at equivalent beta 1 -receptor blocking doses. Hypertension: The mechanism of the antihypertensive effects of beta-blocking agents has not been elucidated. However, several possible mechanisms have been proposed: (1) competitive antagonism of catecholamines at peripheral (especially cardiac) adrenergic neuron sites, leading to decreased cardiac output; (2) a central effect leading to reduced sympathetic outflow to the periphery; and (3) suppression of renin activity. Angina Pectoris: By blocking catecholamine-induced increases in heart rate, in velocity and extent of myocardial contraction, and in blood pressure, metoprolol reduces the oxygen requirements of the heart at any given level of effort, thus making it useful in the long-term management of angina pectoris. Heart Failure: The precise mechanism for the beneficial effects of beta-blockers in heart failure has not been elucidated.
hypertension in adult patientsto lower blood pressurethe long-term treatment of angina pectoris+6 more
1995
30
RISPERIDONE
risperidone
Post-LOE
ORAL · TABLET
2008
30
ROSUVASTATIN CALCIUM
rosuvastatin calcium
Post-LOE
ORAL · TABLET
2016
30
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Interview Prep Quick Facts
Founded: 2024
Portfolio: 5 approved products
Top TAs: Cardiovascular, Neurology, Psychiatry
Portfolio Health
Post-LOE5 (100%)
5 total products
Therapeutic Area Focus
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