Talacen

• Compumed Pharmaceuticals, Inc.

• PD-Rx Pharmaceuticals, Inc.

• Pharma Pac (A Service Of H.J. Harkins Co., Inc.)

• Quality Care Pharmaceuticals

• Sanofi-Aventis U.S. LLC

• Sanofi-Synthelabo Inc.

CIV

Talacen is a combination of pentazocine hydrochloride, USP, equivalent to 25 mg base and acetaminophen, USP, 650 mg.

Pentazocine is a member of the benzazocine series (also known as the benzomorphan series). Chemically, pentazocine is (2R*, 6R*, 11R*)1,2,3,4,5,6-hexahydro-6,11-dimethyl-3-(3-methyl-2-butenyl)-2,6-methano-3-benzazocin-8-ol, a white, crystalline substance soluble in acidic aqueous solutions, and has the following structural formula:

Chemically, acetaminophen is Acetamide, N-(4-hydroxyphenyl)-, and has the following structural formula:

Pentazocine is an analgesic and acetaminophen is an analgesic and antipyretic.

Inactive Ingredients: Colloidal Silicon Dioxide, FD&C Blue #1, Gelatin, Microcrystalline Cellulose, Potassium Sorbate, Pregelatinized Starch, Sodium Lauryl Sulfate, Sodium Metabisulfite, Sodium Starch Glycolate, Stearic Acid.

Talacen is an analgesic possessing antipyretic actions.

Pentazocine is an analgesic with agonist/antagonist action which when administered orally is approximately equivalent on a mg for mg basis in analgesic effect to codeine.

Acetaminophen is an analgesic and antipyretic.

Onset of significant analgesia with pentazocine usually occurs between 15 and 30 minutes after oral administration, and duration of action is usually three hours or longer. Onset and duration of action and the degree of pain relief are related both to dose and the severity of pretreatment pain. Pentazocine weakly antagonizes the analgesic effects of morphine, meperidine, and phenazocine; in addition, it produces incomplete reversal of cardiovascular, respiratory, and behavioral depression induced by morphine and meperidine. Pentazocine has about 1/50 the antagonistic activity of nalorphine. It also has sedative activity.

Pentazocine is well absorbed from the gastrointestinal tract. Plasma levels closely correspond to the onset, duration, and intensity of analgesia. The time to mean peak concentration in 24 normal volunteers was 1.7 hours (range 0.5 to 4 hours) after oral administration and the mean plasma elimination half-life was 3.6 hours (range 1.5 to 10 hours).

The action of pentazocine is terminated for the most part by biotransformation in the liver with some free pentazocine excreted in the urine. The products of the oxidation of the terminal methyl groups and glucuronide conjugates are excreted by the kidney. Elimination of approximately 60% of the total dose occurs within 24 hours. Pentazocine passes the placental barrier.

Onset of significant analgesic and antipyretic activity of acetaminophen when administered orally occurs within 30 minutes and is maximal at approximately 2 1/2 hours. The pharmacological mode of action of acetaminophen is unknown at this time.

Acetaminophen is rapidly and almost completely absorbed from the gastrointestinal tract. In 24 normal volunteers the time to mean peak plasma concentration was 1 hour (range 0.25 to 3 hours) after oral administration and the mean plasma elimination half-life was 2.8 hours (range 2 to 4 hours).

The effect of pentazocine on acetaminophen plasma protein binding or vice versa has not been established. For acetaminophen there is little or no plasma protein binding at normal therapeutic doses. When toxic doses of acetaminophen are ingested and drug plasma levels exceed 90 mcg/mL, plasma binding may vary from 8% to 43%.

Acetaminophen is conjugated in the liver with glucuronic acid and to a lesser extent with sulfuric acid. Approximately 80% of acetaminophen is excreted in the urine after conjugation and about 3% is excreted unchanged. The drug is also conjugated to a lesser extent with cysteine and additionally metabolized by hydroxylation.

If Talacen is taken every 4 hours over an extended period of time, accumulation of pentazocine and to a lesser extent, acetaminophen, may occur.

Talacen should not be administered to patients who are hypersensitive to either pentazocine or acetaminophen.

Clinical experience with Talacen has been insufficient to define all possible adverse reactions with this combination. However, reactions reported after oral administration of pentazocine hydrochloride in 50 mg dosage include gastrointestinal: nausea, vomiting, infrequently constipation; and rarely abdominal distress, anorexia, diarrhea. CNS effects: dizziness, lightheadedness, hallucinations, sedation, euphoria, headache, confusion, disorientation; infrequently weakness, disturbed dreams, insomnia, syncope, visual blurring and focusing difficulty, depression; and rarely tremor, irritability, excitement, tinnitus. Autonomic: sweating; infrequently flushing; and rarely chills. Allergic: infrequently rash; and rarely urticaria, edema of the face. Cardiovascular: infrequently decrease in blood pressure, tachycardia. Hematologic: rarely depression of white blood cells (especially granulocytes), which is usually reversible, moderate transient eosinophilia. Other: rarely respiratory depression, urinary retention, paresthesia, serious skin reactions, including erythema multiforme, Stevens-Johnson Syndrome, toxic epidermal necrolysis, and in one instance, an apparent anaphylactic reaction has been reported.

Numerous clinical studies have shown that acetaminophen, when taken in recommended doses, is relatively free of adverse effects in most age groups, even in the presence of a variety of disease states.

A few cases of hypersensitivity to acetaminophen have been reported, as manifested by skin rashes, thrombocytopenic purpura, rarely hemolytic anemia and agranulocytosis.

Occasional individuals respond to ordinary doses with nausea and vomiting and diarrhea.

Adult

The usual adult dose is 1 caplet every 4 hours as needed for pain relief, up to a maximum of 6 caplets per day.

The usual duration of therapy is dependent upon the condition being treated but in any case should be reviewed regularly by the physician. The effect of meals on the rate and extent of bioavailability of both pentazocine and acetaminophen has not been documented.

Talacen is available for oral administration as a pale blue, scored caplet embossed with "Winthrop" on one side and "T37" on the other side.

Bottles of 100 (NDC 0024-1937-04).

Store at 25° C (77° F); excursions permitted between 15° – 30° C (59° – 86° F).

Revised August 2008

Manufactured for:
sanofi-aventis U.S. LLC
Bridgewater, NJ 08807

©2008 sanofi-aventis U.S. LLC

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
• Signs of liver problems like dark urine, feeling tired, not hungry, upset stomach or stomach pain, light-colored stools, throwing up, or yellow skin or eyes.
• Very bad dizziness or passing out.
• Trouble breathing, slow breathing, or shallow breathing.
• Feeling confused.
• Very upset stomach or throwing up.
• Very hard stools (constipation).
• Feeling very tired or weak.
• A fast heartbeat.
• Fever or chills.
• Sore throat.
• Hallucinations (seeing or hearing things that are not there).
• Mood changes.
• Seizures.
• Very bad headache.
• Shakiness.
• Not able to sleep.
• Trouble passing urine.
• Change in eyesight.
• A very bad skin reaction (Stevens-Johnson syndrome/toxic epidermal necrolysis) may happen. It can cause very bad health problems that may not go away, and sometimes death. Get medical help right away if you have signs like red, swollen, blistered, or peeling skin (with or without fever); red or irritated eyes; or sores in your mouth, throat, nose, or eyes.
• A very bad and sometimes deadly health problem called serotonin syndrome may happen if you take this drug with drugs for depression, migraines, or certain other drugs. Call your doctor right away if you have agitation; change in balance; confusion; hallucinations; fever; fast or abnormal heartbeat; flushing; muscle twitching or stiffness; seizures; shivering or shaking; sweating a lot; very bad diarrhea, upset stomach, or throwing up; or very bad headache.
• Taking an opioid drug like this drug may lead to a rare but very bad adrenal gland problem. Call your doctor right away if you have very bad dizziness or passing out, very bad upset stomach or throwing up, or if you feel less hungry, very tired, or very weak.