Nitrolingual Pump Spray Information
Nitrolingual pump spray (Nitroglycerinsublingual)
Nitrolingual pump spray (Nitroglycerinsublingual) Description
Nitroglycerin, an organic nitrate, is a vasodilator which has effects on both arteries and veins. The chemical name for nitroglycerin is 1,2,3-propanetriol trinitrate (CHNO). The compound has a molecular weight of 227.09. The chemical structure is:
Nitrolingual Pumpspray (nitroglycerin lingual spray 400 mcg) is a metered dose spray containing nitroglycerin. This product delivers nitroglycerin (400 mcg per spray, 60 or 200 metered sprays) in the form of spray droplets onto or under the tongue. Inactive ingredients: medium-chain triglycerides, dehydrated alcohol, medium-chain partial glycerides, peppermint oil.
Nitrolingual pump spray (Nitroglycerinsublingual) Clinical Pharmacology
The principal pharmacological action of nitroglycerin is relaxation of vascular smooth muscle, producing a vasodilator effect on both peripheral arteries and veins with more prominent effects on the latter. Dilation of the post-capillary vessels, including large veins, promotes peripheral pooling of blood and decreases venous return to the heart, thereby reducing left ventricular end-diastolic pressure (pre-load). Arteriolar relaxation reduces systemic vascular resistance and arterial pressure (after-load).
The mechanism by which nitroglycerin relieves angina pectoris is not fully understood. Myocardial oxygen consumption or demand (as measured by the pressure-rate product, tension-time index, and stroke-work index) is decreased by both the arterial and venous effects of nitroglycerin and presumably, a more favorable supply-demand ratio is achieved.
While the large epicardial coronary arteries are also dilated by nitroglycerin, the extent to which this action contributes to relief of exertional angina is unclear.
Nitroglycerin is rapidly metabolized , with a liver reductase enzyme having primary importance in the formation of glycerol nitrate metabolites and inorganic nitrate. Two active major metabolites, 1,2- and 1,3-dinitroglycerols, the products of hydrolysis, although less potent as vasodilators, have longer plasma half-lives than the parent compound. The dinitrates are further metabolized to mononitrates (considered biologically inactive with respect to cardiovascular effects) and ultimately glycerol and carbon dioxide.
Therapeutic doses of nitroglycerin may reduce systolic, diastolic and mean arterial blood pressure. Effective coronary perfusion pressure is usually maintained, but can be compromised if blood pressure falls excessively or increased heart rate decreases diastolic filling time.
Elevated central venous and pulmonary capillary wedge pressures, pulmonary vascular resistance and systemic vascular resistance are also reduced by nitroglycerin therapy. Heart rate is usually slightly increased, presumably a reflex response to the fall in blood pressure. Cardiac index may be increased, decreased, or unchanged. Patients with elevated left ventricular filling pressure and systemic vascular resistance values in conjunction with a depressed cardiac index are likely to experience an improvement in cardiac index. On the other hand, when filling pressures and cardiac index are normal, cardiac index may be slightly reduced.
In a pharmacokinetic study when a single 0.8 mg dose of Nitrolingual Pumpspray was administered to healthy volunteers (n = 24), the mean C and t were 1,041pg/mL ∙ min and 7.5 minutes, respectively. Additionally, in these subjects the mean area-under-the-curve (AUC) was 12,769 pg/mL ∙ min.
In a randomized, double-blind single-dose, 5-period cross-over study in 51 patients with exertional angina pectoris significant dose-related increases in exercise tolerance, time to onset of angina and ST-segment depression were seen following doses of 0.2, 0.4, 0.8 and 1.6 mg of nitroglycerin delivered by metered pumpspray as compared to placebo.
Additionally the drug was well tolerated as evidenced by a profile of generally mild to moderate adverse events.
Nitrolingual pump spray (Nitroglycerinsublingual) Indications And Usage
Nitrolingual Pumpspray is indicated for acute relief of an attack or prophylaxis of angina pectoris due to coronary artery disease.
Nitrolingual pump spray (Nitroglycerinsublingual) Contraindications
Allergic reactions to organic nitrates are rare. Nitroglycerin is contraindicated in patients who are allergic to it. Nitrolingual Pumpspray is contraindicated in patients taking certain drugs for erectile dysfunction (phosphodiesterase inhibitors), as their concomitant use can cause severe hypotension. The time course and dose-dependency of this interaction are not known.
Nitrolingual pump spray (Nitroglycerinsublingual) Warnings
Amplification of the vasodilatory effects of Nitrolingual Pumpspray by certain drugs (phosphodiesterase inhibitors) used to treat erectile dysfunction can result in severe hypotension. The time course and dose dependence of this interaction have not been studied. Appropriate supportive care has not been studied, but it seems reasonable to treat this as a nitrate overdose, with elevation of the extremities and with central volume expansion. The use of any form of nitroglycerin during the early days of acute myocardial infarction requires particular attention to hemodynamic monitoring and clinical status.
Nitrolingual pump spray (Nitroglycerinsublingual)
Nitrolingual pump spray (Nitroglycerinsublingual) Adverse Reactions
Adverse reactions to oral nitroglycerin dosage forms, particularly headache and hypotension, are generally dose-related. In clinical trials at various doses of nitroglycerin, the following adverse effects have been observed:
Headache, which may be severe and persistent, is the most commonly reported side effect of nitroglycerin with an incidence on the order of about 50% in some studies. Cutaneous vasodilation with flushing may occur. Transient episodes of dizziness and weakness, as well as other signs of cerebral ischemia associated with postural hypotension, may occasionally develop. Occasionally, an individual may exhibit marked sensitivity to the hypotensive effects of nitrates and severe responses (nausea, vomiting, weakness, restlessness, pallor, perspiration and collapse) may occur even with therapeutic doses. Drug rash and/or exfoliative dermatitis have been reported in patients receiving nitrate therapy. Nausea and vomiting appear to be uncommon.
Nitrolingual Pumpspray given to 51 chronic stable angina patients in single doses of 0.4, 0.8 and 1.6 mg as part of a double-blind, 5-period single-dose cross-over study exhibited an adverse event profile that was generally mild to moderate. Adverse events occurring at a frequency greater than 2% included: headache, dizziness, and paresthesia. Less frequently reported events in this trial included (≤2%): dyspnea, pharyngitis, rhinitis, vasodilation, peripheral edema, asthenia, and abdominal pain.
Nitrolingual pump spray (Nitroglycerinsublingual) Dosage And Administration
At the onset of an attack, one or two metered sprays should be administered onto or under the tongue. No more than three metered sprays are recommended within a 15-minute period. Nitrolingual Pumpspray may be used prophylactically five to ten minutes prior to engaging in activities which might precipitate an acute attack.
Each metered spray of Nitrolingual Pumpspray delivers 48 mg of solution containing 400 mcg of nitroglycerin after an initial priming of 5 sprays. It will remain adequately primed for 6 weeks. If the product is not used within 6 weeks it can be adequately reprimed with 1 spray. Longer storage periods without use may require up to 5 repriming sprays. There are 60 or 200 metered sprays per bottle. The total number of available doses is dependent, however, on the number of sprays per use (1 or 2 sprays), and the frequency of repriming.
The transparent container can be used for continuous monitoring of the consumption. Once fluid falls below the level of the center tube, sprays will not be adequate and the container should be replaced. As with all other sprays, there is a residual volume of fluid at the bottom of the bottle which cannot be used.
During application the patient should rest, ideally in the sitting position. The container should be held vertically with the valve head uppermost and the spray orifice as close to the mouth as possible. The dose should preferably be sprayed onto the tongue by pressing the button firmly and the mouth should be closed immediately after each dose. THE SPRAY SHOULD NOT BE INHALED. The medication should not be expectorated or the mouth rinsed for 5 to 10 minutes following administration. Patients should be instructed to familiarize themselves with the position of the spray orifice, which can be identified by the finger rest on top of the valve, in order to facilitate orientation for administration at night.
Nitrolingual pump spray (Nitroglycerinsublingual) How Supplied
Each box of Nitrolingual Pumpspray contains one glass bottle coated with red transparent plastic which assists in containing the glass and medication should the bottle be shattered. Each bottle contains 4.9 g or 12 g (Net Content) of nitroglycerin lingual spray which will deliver 60 or 200 metered sprays containing 400 mcg of nitroglycerin per spray after priming.
Nitrolingual Pumpspray is available as:
Nitrolingual pump spray (Nitroglycerinsublingual)
Nitrolingual pump spray (Nitroglycerinsublingual) Information For The Patient
Before using your Nitrolingual Pumpspray (nitroglycerin lingual spray) 400 mcg per spray, 60 or 200 metered sprays, read carefully the following directions for use.
Nitrolingual Pumpspray is a metered dose spray which delivers 48 mg of solution containing 400 mcg of nitroglycerin with each spray. Nitroglycerin is absorbed from the tongue and surrounding mucosa producing a prompt therapeutic effect. It is best to use Nitrolingual Pumpspray in a sitting position.
During an anginal attack, one or two sprays should be administered into your mouth, preferably onto or under the tongue. Do not inhale spray. The medication should not be expectorated or the mouth rinsed for 5 to 10 minutes following administration. A spray may be repeated approximately every 3-5 minutes as needed. No more than three metered sprays are recommended within a 15-minute period. If chest pain persists, prompt medical attention is recommended. Nitrolingual Pumpspray may be used 5 to 10 minutes prior to engaging in activities which might provoke an acute attack.
There are approximately 60 or 200 metered sprays of nitroglycerin per Nitrolingual Pumpspray bottle. However, the number of times the medication may be used is dependent on the number of sprays per use (1 or 2 sprays), and frequency of repriming. Each metered spray of Nitrolingual Pumpspray delivers 400 mcg of nitroglycerin after an initial priming of 5 sprays. The container will remain adequately primed for 6 weeks. If the medication is not used within 6 weeks, it can be adequately reprimed with 1 spray. Longer storage periods without use may require up to 5 repriming sprays.
Your physician has determined that this product is likely to help your personal health.
If you have any questions about alternatives, consult with your physician.
Do not share or give your medication to others, particularly those who may appear to be having chest discomfort similar to yours. Nitrolingual Pumpspray should be used during an episode of chest pain or may be used 5 to 10 minutes prior to engaging in activities which might provoke an acute attack.
Nitrolingual Pumpspray is available in a clear glass bottle with a red plastic coating on the exterior. This plastic coating is designed to contain the glass and medication should the bottle be shattered.
The transparent container can be used for continuous monitoring of the consumption. Once fluid falls below the level of the center tube, sprays will not be adequate and the container should be replaced. As with all other sprays, there is a residual volume of fluid at the bottom of the bottle which cannot be used. Nitrolingual Pumpspray contains 20% alcohol. Do not forcefully open or burn container. Do not spray toward flames.
Store at 25 °C (77 °F); excursions permitted to 15-30 °C (59-86 °F) [see USP Controlled Room Temperature].
The following trademarks are either registered trademarks or trademarks of Pohl-Boskamp in the United States and/or other countries: Pohl-Boskamp word mark; Pohl-Boskamp logo; Nitrolingual word mark; Peppermint flavor of nitroglycerin; Peppermint scent of nitroglycerin; Nitrolingual Pumpspray shapes, Nitrolingual Pumpspray colors, and the sound of Nitrolingual Pumpspray.
Rev. 09/10
Nitrolingual pump spray (Nitroglycerinsublingual) Principal Display Panel - Metered Spray Carton Label
(nitroglycerin lingual spray)
400 mcg per spray 60 Metered Sprays 4.9 g NET CONTENTS
NDC 24338-300-65
