Amerge

Trade name

Amerge® (naratriptan hydrochloride) tablets, for oral use

Dosage forms and strengths

A prescription drug called Amerge (generic name: naratriptan) is used to treat migraine headaches. Amerge works by constricting blood vessels near the brain, which helps to lessen migraine-related pain and other symptoms. Amerge is typically taken as needed to relieve migraine symptoms, but it can also be taken every day to avoid migraines altogether. Amerge's potential side effects include nausea, dry mouth, sleepiness, and dizziness. If you are allergic to naratriptan or any other ingredient in Amerge, you should not take this medication. Inform your doctor about all other medications you are taking, including those obtained over-the-counter, as well as any health issues you may have before taking Amerge.

Amerge is contraindicated during pregnancy. This medication is excreted in breast milk and could harm a nursing infant. Anyone under the age of 18 should not use Amerge. Consult your doctor or other qualified healthcare professional for more details on this medication.

Pharmacokinetics

Following oral administration, naratriptan is rapidly and effectively absorbed, with maximum plasma concentrations being reached in 2 hours. Naratriptan has a bioavailability of about 40%. Only 5% of the dose of naltrexone is recovered as an unchanged drug in the urine due to extensive metabolism. The first-pass primary metabolites are produced by monoamine oxidase and are found in plasma at much lower levels than the parent compound. About 3 L/kg of nartriptan is distributed throughout the body, and about 95% of it is bound to plasma proteins. Naratriptan has a plasma clearance of 1.3 L/hr/kg. Naratriptan has a 3 hour half-life in the body.

Indications and Usage

Amerge is recommended for the immediate treatment of adult migraines with or without aura. Amerge is not meant to be used as preventative medicine.

Pediatric use

Amerge's effectiveness and safety in treating pediatric patients have not been proven.

Geriatric use

There were insufficient elderly participants in Amerge clinical studies to determine whether their responses differed from those of younger participants. The responses of elderly patients and younger patients have not been found to differ in other reported clinical experiences. In general, choosing a dose for an elderly patient should be cautious, usually beginning at the low end of the dosing range. This is because elderly patients are more likely to have decreased hepatic, renal, or cardiac function, as well as concurrent disease or other drug therapy, and these factors are more common. The risk of toxic reactions to this medication may be higher in patients with impaired renal function because it is known that the kidneys play a significant role in its excretion. Renal function should be carefully considered when choosing a dose because elderly patients are more likely to have decreased renal function.It may also be helpful to monitor renal function.

Contraindications

Amerge is not recommended for individuals with:

- Ischemic heart disease or another serious cardiovascular condition (see WARNINGS).

- Transient ischemic attack or stroke history (see WARNINGS)

- Raynaud's phenomenon or peripheral vascular disease (see WARNINGS)

- Hepatic impairment (see WARNINGS and CLINICAL PHARMACOLOGY)

- Have a history of naratriptan or any of the excipients in Amerge causing hypersensitivity (see WARNINGS)

Warnings

Ischemic heart disease and other serious cardiovascular diseases that underlie it

Patients with significant underlying cardiovascular disease, such as ischemic coronary artery disease, should not take naratriptan (see CONTRAINDICATIONS). Patients with uncontrolled hypertension shouldn't be given narcan. In clinical trials, naratriptan was linked to a dose-related and typically not clinically significant rise in blood pressure. However, during postmarketing surveillance, there were a few isolated reports of hypertensive episodes. Patients without a history of hypertension were mentioned in some of these reports. If a person taking naratriptan develops hypertension, the medication should be stopped and the patient should be examined.

Side Effects

In other sections of the labeling, the following severe adverse reactions are covered in more detail:

- Ischemic cardiovascular disease and other serious cardiovascular conditions (see WARNINGS)

- Transient ischemic attack or stroke history (see WARNINGS)

- Raynaud's phenomenon or peripheral vascular disease (see WARNINGS)

Clinical Trials Experience

Because adverse reaction rates in clinical trials are determined under a variety of different circumstances, they cannot be directly compared to adverse reaction rates in clinical trials of other drugs and may not accurately reflect rates seen in actual clinical practice.

In two multicenter, randomized, double-blind, placebo-controlled trials involving 1,177 adult migraineurs, Amerge's safety was assessed. These studies enrolled people who had had at least four migraines in the three months prior to screening, had a history of migraines (with or without aura) for at least a year, and who, during the run-in phase, had two to eight moderate to severe migraines per month.

The following adverse reactions were more frequently reported (> 5%) in patients receiving Amerge treatment than in patients receiving placebo treatment in both studies.

Table 2: Adverse Reactions More Common Than Placebo in Two Multicenter, Randomized, Double-Blind, Placebo-Controlled Trials of Acute Treatment of Migraine and Reported by 2% of Patients Treated With Amerge

Body System/Adverse Reaction Reporting Rate of Patients Placebo Amerge (n=1,177) (n=592) Blood Pressure Palpitations 1.0% 0.8% Digestive Nausea 10.2% 3.2% Vomiting 5.9% 2.0% Vomiting 2.6% 1.7% Continent pain 2.3% 1.5% Dyspepsia 2.1% 1.4% mouth ache 2.0% 1.0% Nutritional and Metabolic Hypercholesterolemia 4.1* 3.6 Hypokalemia 3.7* 3 Nervous sedation 7.3% 2.6% Dizziness 5.8% 3.7% Paresthesia 4.9% 2.2% Lack of muscle 4.0* 3.2 Mental Health Anxiety 3.4% 1.8% Breathing Pharyngitis Sinusitis, 3.5* 2 Skin and appendages 2.5*1 Sweating 5.3* 3

Dosage

Amerge should be taken in a starting dose of 1 mg (2 tablets) as soon as a migraine begins. If the headache gets better but then comes back, you can take it again once in two hours as long as your daily dose of 2 mg (4 tablets) hasn't been exceeded. Two doses are the most frequently advised number to take in any 24-hour period. In clinical trials, naratriptan's effectiveness was shown when it was used as soon as migraine symptoms appeared. You can take Amerge with or without food.

Overdose

Symptoms

Drowsiness is the overdose symptom that occurs most frequently. Tachycardia, bradycardia, hypertension, hypotension, dyspnea, and chest pain are some additional symptoms that have been reported. Serotonin syndrome has been linked to the use of 5-HT1 agonists in some reports.

Treatment

Amerge should be stopped right away in the event of an overdose, and appropriate supportive and symptomatic care should be started. Continuously check your blood pressure and heart rate, and if necessary, treat as necessary. Give vasopressors or antihypertensives depending on the patient's clinical status to treat any hypertension or hypotension that may occur. Take into account the chance of a multi-drug overdose. Activated charcoal should be given orally if the patient shows up within an hour of consuming something. If the patient arrives more than an hour after ingestion and there is any reason to think that a sizable amount of the drug is still in the digestive system, consider performing gastric lavage with a large bore nasogastric tube.

Storage

Keep at 25 °C (77 °F); excursions are allowed to 15 °C (59 °F) and 30 °C (86 °F).

Dispensing

For oral administration, 2.5 mg tablets of Amerge are provided. Hypromellose, lactose monohydrate, magnesium stearate, microcrystalline cellulose, polyethylene glycol, polysorbate 80, and titanium dioxide are all inactive ingredients found in each tablet. As a color additive, FD&C Blue No. 2 Aluminum Lake is also present in the Amerge 2.5 mg tablet.

How Supplied / Storage and Handling

Amerge® (naratriptan HCl) tablets are flat-faced, beveled-edged, modified oval-shaped tablets that range in color from white to off-white and are embossed on one side with a partial scoreline and plain on the other.

6 Tablets per Bottle NDC 0228-2505-06

12 tablet bottles NDC 0228-2505-12

2 x 6 Tablets packaged in blisters. NDC 0228-2505-26 Keep at 25 °C (77 °F); excursions are allowed to 15 °C (59 °F) and 30 °C (86 °F). Keep out of children's reach. As specified in the USP/NF, dispense in a tightly sealed, light-resistant container. GlaxoSmithKline has registered Amerge as a trademark.