Aponal

Aponal is a dibenzoxepin-derivative tricyclic antidepressant (TCA). TCAs are structurally similar to phenothiazines. They contain a tricyclic ring system with an alkyl amine substituent on the central ring. In non-depressed individuals, Aponal does not affect mood or arousal, but may cause sedation. In depressed individuals, Aponal exerts a positive effect on mood. TCAs are potent inhibitors of serotonin and norepinephrine reuptake. Tertiary amine TCAs, such as Aponal and amitriptyline, are more potent inhibitors of serotonin reuptake than secondary amine TCAs, such as nortriptyline and desipramine. TCAs also down-regulate cerebral cortical β-adrenergic receptors and sensitize post-synaptic serotonergic receptors with chronic use. The antidepressant effects of TCAs are thought to be due to an overall increase in serotonergic neurotransmission. TCAs also block histamine H1 receptors, α1-adrenergic receptors and muscarinic receptors, which accounts for their sedative, hypotensive and anticholinergic effects (e.g. blurred vision, dry mouth, constipation, urinary retention), respectively. Aponal has less sedative and anticholinergic effects than amitriptyline. See toxicity section below for a complete listing of side effects. Aponal may be used to treat depression and insomnia. Unlabeled indications include chronic and neuropathic pain, and anxiety. Aponal may also be used as a second line agent to treat idiopathic urticaria.

Aponal Capsules, USP are recommended for the treatment of:

The target symptoms of psychoneurosis that respond particularly well to Aponal capsules include anxiety, tension, depression, somatic symptoms and concerns, sleep disturbances, guilt, lack of energy, fear, apprehension and worry.

Clinical experience has shown that Aponal capsules are safe and well tolerated even in the elderly patient. Owing to lack of clinical experience in the pediatric population, Aponal capsules are not recommended for use in children under 12 years of age.

This medication guide provides information about the use of Aponal (Sinequan or other generic names) to treat depression or anxiety. Aponal is another brand of Aponal that is not covered in this medication guide.

Aponal is a tricyclic antidepressant. Aponal affects chemicals in the brain that may become unbalanced.

Aponal (Sinequan or other generic name) is used to treat symptoms of depression and/or anxiety associated with alcoholism, psychiatric conditions, or manic-depressive conditions.

Aponal may also be used for purposes not listed in this medication guide.

The dose of Aponal (Aponal tablets) should be individualized.

Dosing in Adults

The recommended dose of Aponal (Aponal tablets) for adults is 6 mg once daily. A 3 mg once daily dose may be appropriate for some patients, if clinically indicated.

Dosing in the Elderly

The recommended starting dose of Aponal (Aponal tablets) in elderly patients ( ≥ 65 years old) is 3 mg once daily. The daily dose can be increased to 6 mg, if clinically indicated.

Administration

Aponal (Aponal tablets) should be taken within 30 minutes of bedtime.

To minimize the potential for next day effects, Aponal (Aponal tablets) should not be taken within 3 hours of a meal.

The total Aponal (Aponal tablets) dose should not exceed 6 mg per day.

How supplied

Dosage Forms And Strengths

Aponal (Aponal tablets) is an immediate-release, oval-shaped, tablet for oral administration available in strengths of 3 mg and 6 mg. The tablets are blue (3 mg) or green (6 mg) and are debossed with 3 or 6, respectively, on one side and SP on the other. Aponal (Aponal tablets) tablets are not scored.

Aponal (Aponal tablets) 3 mg tablets are oval shaped, blue, identified with debossed markings of “3” on one side and “SP” on the other, and are supplied as:

NDC 42847-103-30..................Bottle of 30

NDC 42847-103-10..................Bottle of 100

NDC 42847-103-50..................Bottle of 500

NDC 42847-103-03..................Blister trade pack of 30

Aponal (Aponal tablets) 6 mg tablets are oval shaped, green, identified with debossed markings of “6” on one side and “SP” on the other, and are supplied as:

NDC 42847-106-30..................Bottle of 30

NDC 42847-106-10..................Bottle of 100

NDC 42847-106-50..................Bottle of 500

NDC 42847-106-03..................Blister trade pack of 30

Storage and Handling

Store at controlled room temperature 20° - 25°C (68° - 77°F), protected from light.

Manufactured for: Somaxon Pharmaceuticals, Inc. San Diego, CA 92130 USA.

See also:
What is the most important information I should know about Aponal?

Hypersensitivity

Aponal (Aponal tablets) is contraindicated in individuals who have shown hypersensitivity to Aponal HCl, any of its inactive ingredients, or other dibenoxepines.

Co-administration with Monoamine Oxidase Inhibitors (MAOIs)

Serious side effects and even death have been reported following the concomitant use of certain drugs with MAO inhibitors. Do not administer Aponal (Aponal tablets) if patient is currently on MAOIs or has used MAOIs within the past two weeks. The exact length of time may vary depending on the particular MAOI dosage and duration of treatment.

Glaucoma and Urinary Retention

Aponal (Aponal tablets) is contraindicated in individuals with untreated narrow angle glaucoma or severe urinary retention.

Use Aponal capsules as directed by your doctor. Check the label on the medicine for exact dosing instructions.

• Aponal capsules comes with an extra patient information sheet called a Medication Guide. Read it carefully. Read it again each time you get Aponal capsules refilled.
• Take Aponal capsules by mouth with or without food.
• Taking Aponal capsules at bedtime may help reduce side effects (eg, daytime drowsiness). Discuss this possibility with your doctor.
• If you miss a dose of Aponal capsules, take it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not take 2 doses at once. If you take 1 dose daily at bedtime, do not take the missed dose the next morning.

Ask your health care provider any questions you may have about how to use Aponal capsules.

This medication is used to treat mental/mood problems such as depression and anxiety. It may help improve mood and feelings of well-being, relieve anxiety and tension, help you sleep better, and increase your energy level. This medication belongs to a class of medications called tricyclic antidepressants. It works by affecting the balance of certain natural chemicals (neurotransmitters) in the brain.

How to use Aponal

Read the Medication Guide provided by your pharmacist before you start taking Aponal and each time you get a refill. If you have any questions, consult your doctor or pharmacist.

Take this medication by mouth, usually 1 to 3 times daily or as directed by your doctor. If you take it only once a day, take it at bedtime to reduce daytime sleepiness. The dosage is based on your medical condition and response to treatment.

To reduce your risk of side effects (such as drowsiness, dry mouth, dizziness), your doctor may direct you to start this medication at a low dose and gradually increase your dose. Follow your doctor's instructions carefully.

Take this medication regularly in order to get the most benefit from it. To help you remember, take it at the same time(s) each day. Do not increase your dose or use this drug more often or for longer than prescribed. Your condition will not improve any faster, and your risk of side effects will increase.

It is important to continue taking this medication even if you feel well. Do not stop taking this medication without consulting your doctor. Some conditions may become worse when this drug is suddenly stopped. Also, you may experience symptoms such as mood swings, headache, and tiredness. To prevent these symptoms while you are stopping treatment with this drug, your doctor may reduce your dose gradually. Consult your doctor or pharmacist for more details. Report any new or worsening symptoms right away.

This medication may not work right away. You may see some benefit within a week. However, it may take up to 3 weeks before you feel the full effect.

Tell your doctor if your condition persists or worsens (such as your feelings of sadness get worse, or you have thoughts of suicide).

See also:
What other drugs will affect Aponal?

Cytochrome P450 Isozymes

Aponal (Aponal tablets) is primarily metabolized by hepatic cytochrome P450 isozymes CYP2C19 and CYP2D6, and to a lesser extent, by CYP1A2 and CYP2C9. Inhibitors of these isozymes may increase the exposure of Aponal. Aponal (Aponal tablets) is not an inhibitor of any CYP isozymes at therapeutically relevant concentrations. The ability of Aponal (Aponal tablets) to induce CYP isozymes is not known.

Cimetidine

Aponal (Aponal tablets) exposure is doubled with concomitant administration of cimetidine, a nonspecific inhibitor of CYP isozymes. A maximum dose of 3 mg is recommended in adults and elderly when cimetidine is co-administered with Aponal

Alcohol

When taken with Aponal (Aponal tablets), the sedative effects of alcohol may be potentiated.

CNS Depressants and Sedating Antihistamines

When taken with Aponal (Aponal tablets), the sedative effects of sedating antihistamines and CNS depressants may be potentiated.

Tolazamide

A case of severe hypoglycemia has been reported in a type II diabetic patient maintained on tolazamide (1 g/day) 11 days after the addition of oral Aponal (75 mg/day).

Drug Abuse And Dependence

Controlled Substance

Aponal is not a controlled substance.

Abuse

Aponal is not associated with abuse potential in animals or in humans. Physicians should carefully evaluate patients for history of drug abuse and follow such patients closely, observing them for signs of misuse or abuse of Aponal (e.g., incrementation of dose, drug-seeking behavior).

Dependence

In a brief assessment of adverse events observed during discontinuation of Aponal following chronic administration, no symptoms indicative of a withdrawal syndrome were observed. Thus, Aponal does not appear to produce physical dependence.

See also:
What are the possible side effects of Aponal?

Controlled Clinical Trials

Systemic Adverse Effects: In controlled clinical trials of patients treated with Aponal (Aponal) Cream, the most common systemic adverse event reported was drowsiness. Drowsiness occurred in 71 of 330 (22%) of patients treated with Aponal (Aponal) Cream compared to 7 of 334 (2%) of patients treated with vehicle cream. Drowsiness resulted in the premature discontinuation of the drug in approximately 5% of patients treated with Aponal (Aponal) Cream in controlled clinical trials.

Local Site Adverse Effects: In controlled clinical trials of patients treated with Aponal (Aponal) Cream, the most common local site adverse event reported was burning and/or stinging at the site of application. These occurred in 76 of 330 (23%) of patients treated with Aponal (Aponal) Cream compared to 54 of 334 (16%) of patients treated with vehicle cream. Most of these reactions were categorized as "mild"; however, approximately 25% of patients who reported burning and/or stinging reported the reaction as "severe". Four patients treated with Aponal (Aponal) Cream withdrew from the study because of the burning and/or stinging.

The table below presents the adverse events reported at an incidence of ≥ 1 % in either Aponal (Aponal) or vehicle cream treatment groups during the trials:

Adverse events occurring in 0.5% to < 1.0% of Aponal (Aponal) Cream treated patients in the controlled clinical trials included: nervousness/anxiety, tongue numbness, fever, and nausea.

Post Marketing Experience

Twenty-six cases of allergic contact dermatitis have been reported in patients using Aponal (Aponal) Cream, twenty of which were documented by positive patch test to Aponal 5% cream.