PENTAZOCINE HYDROCHLORIDE AND NALOXONE HYDROCHLORIDE

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Overview

What is PENTAZOCINE HYDROCHLORIDE AND NALOXONE HYDROCHLORIDE?

Pentazocine and Naloxone Tablets, USP contain pentazocine hydrochloride, USP, a partial opioid agonist, equivalent to 50 mg base and is a member of the benzazocine series (also known as the benzomorphan series), and naloxone hydrochloride, USP, an opioid antagonist equivalent to 0.5 mg base.

Pentazocine and Naloxone Tablets, USP are an analgesic for oral administration.

Chemically, pentazocine hydrochloride, USP is (2*,6*,11*)-1,2,3,4,5,6-Hexahydro-6,11-dimethyl-3-(3-methyl-2-butenyl)-2,6-methano-3-benzazocin-8-ol hydrochloride, a white, crystalline substance soluble in acidic aqueous solutions, and has the following structural formula:

Chemically, naloxone hydrochloride, USP is Morphinan-6-one,4,5-epoxy-3,14-dihydroxy-17-(2- propenyl)-, hydrochloride, (5α)-. It is a slightly off-white powder, and is soluble in water and dilute acids, and has the following structural formula:

Inactive Ingredients: colloidal silicon dioxide, dibasic calcium phosphate, D&C Yellow No. 10, magnesium stearate, microcrystalline cellulose, sodium lauryl sulfate and pregelatinized starch.

What does PENTAZOCINE HYDROCHLORIDE AND NALOXONE HYDROCHLORIDE look like?

What are the available doses of PENTAZOCINE HYDROCHLORIDE AND NALOXONE HYDROCHLORIDE?

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What should I talk to my health care provider before I take PENTAZOCINE HYDROCHLORIDE AND NALOXONE HYDROCHLORIDE?

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How should I use PENTAZOCINE HYDROCHLORIDE AND NALOXONE HYDROCHLORIDE?

Pentazocine and Naloxone Tablets are indicated for the management of pain severe enough to require an opioid analgesic and for which alternative treatments are inadequate.

Limitations of Use

Because of the risks of addiction, abuse, and misuse, with opioids, even at recommended doses, reserve Pentazocine and Naloxone Tablets for use in patients for whom alternative treatment options [e.g., non-opioid analgesics]

Important Dosage and Administration Instructions

Use the lowest effective dosage for the shortest duration consistent with individual patient treatment goals [see ]

Initiate the dosing regimen for each patient individually, taking into account the patient's severity of pain, patient response, prior analgesic treatment experience, and risk factors for addiction, abuse, and misuse [see ].

Monitor patients closely for respiratory depression, especially within the first 24 to 72 hours of initiating therapy and following dosage increases with Pentazocine and Naloxone Tablets and adjust the dosage accordingly [see ].

Initial Dosage

Use of Pentazocine and Naloxone Tablets as the First Opioid Analgesic

Initiate treatment with pentazocine hydrochloride and naloxone hydrochloride tablets, USP in a dosing range of 1 tablet every three to four hours. This may be increased to 2 tablets when needed. Total daily dosage should not exceed 12 tablets.

Conversion from Other Opioids to Pentazocine and Naloxone Tablets

There is inter-patient variability in the potency of opioid drugs and opioid formulations. Therefore, a conservative approach is advised when determining the total daily dosage of Pentazocine and Naloxone Tablets. It is safer to underestimate a patient's 24-hour Pentazocine and Naloxone Tablets dosage than to overestimate the 24-hour Pentazocine and Naloxone Tablets dosage and manage an adverse reaction due to overdose.

Titration and Maintenance of Therapy

Individually titrate Pentazocine and Naloxone Tablets to a dose that provides adequate analgesia and minimizes adverse reactions. Continually reevaluate patients receiving Pentazocine and Naloxone Tablets to assess the maintenance of pain control and the relative incidence of adverse reactions, as well as monitoring for the development of addiction, abuse, or misuse [see ]. Frequent communication is important among the prescriber, other members of the healthcare team, the patient, and the caregiver/family during periods of changing analgesic requirements, including initial titration.

If the level of pain increases after dosage stabilization, attempt to identify the source of increased pain before increasing the Pentazocine and Naloxone Tablets dosage. If unacceptable opioid- related adverse reactions are observed, consider reducing the dosage. Adjust the dosage to obtain an appropriate balance between management of pain and opioid-related adverse reactions.

Discontinuation of Pentazocine and Naloxone Tablets

When a patient who has been taking Pentazocine and Naloxone Tablets regularly and may be physically dependent no longer require therapy with Pentazocine and Naloxone Tablets, taper the dose gradually, by 25% to 50% every 2 to 4 days, while monitoring carefully for signs and symptoms of withdrawal. If the patient develops these signs or symptoms, raise the dose to the previous level and taper more slowly, either by increasing the interval between decreases, decreasing the amount of change in dose, or both. Do not abruptly discontinue Pentazocine and Naloxone Tablets in a physically-dependent patient [see ].

What interacts with PENTAZOCINE HYDROCHLORIDE AND NALOXONE HYDROCHLORIDE?

Pentazocine and Naloxone Tablets are contraindicated in patients with:

- Significant respiratory depression [see ]
- Acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment [see ]. Patients with known or suspected gastrointestinal obstruction, including paralytic ileus [see ]
- Patients with hypersensitivity to either pentazocine, naloxone, or any of the formulation excipients (e.g., anaphylaxis) [see ].

What are the warnings of PENTAZOCINE HYDROCHLORIDE AND NALOXONE HYDROCHLORIDE?

Addiction, Abuse, and Misuse

Pentazocine and Naloxone Tablets contain pentazocine, a Schedule IV controlled substance. As an opioid, Pentazocine and Naloxone Tablets expose users to the risks of addiction, abuse, and misuse [see ].

Although the risk of addiction in any individual is unknown, it can occur in patients appropriately prescribed Pentazocine and Naloxone Tablets. Addiction can occur at recommended dosages and if the drug is misused or abused.

Assess each patient's risk for opioid addiction, abuse, or misuse prior to prescribing Pentazocine and Naloxone Tablets, and monitor all patients receiving Pentazocine and Naloxone Tablets for the development of these behaviors and conditions. Risks are increased in patients with a personal or family history of substance abuse (including drug or alcohol abuse or addiction) or mental illness (e.g., major depression). The potential for these risks should not, however, prevent the proper management of pain in any given patient. Patients at increased risk may be prescribed opioids such as Pentazocine and Naloxone Tablets, but use in such patients necessitates intensive counseling about the risks and proper use of Pentazocine and Naloxone Tablets along with intensive monitoring for signs of addiction, abuse, and misuse.

Opioids are sought by drug abusers and people with addiction disorders and are subject to criminal diversion. Consider these risks when prescribing or dispensing Pentazocine and Naloxone Tablets. Strategies to reduce these risks include prescribing the drug in the smallest appropriate quantity and advising the patient on the proper disposal of unused drug [see ]. Contact local state professional licensing board or state controlled substances authority for information on how to prevent and detect abuse or diversion of this product.

Life-Threatening Respiratory Depression

Serious, life-threatening, or fatal respiratory depression has been reported with the use of opioids, even when used as recommended. Respiratory depression, if not immediately recognized and treated, may lead to respiratory arrest and death. Management of respiratory depression may include close observation, supportive measures, and use of opioid antagonists, depending on the patient's clinical status [see ]. Carbon dioxide (CO) retention from opioid-induced respiratory depression can exacerbate the sedating effects of opioids.

While serious, life-threatening, or fatal respiratory depression can occur at any time during the use of Pentazocine and Naloxone Tablets, the risk is greatest during the initiation of therapy or following a dosage increase. Monitor patients closely for respiratory depression, especially within the first 24 to 72 hours of initiating therapy with and following dosage increases of Pentazocine and Naloxone Tablets.

To reduce the risk of respiratory depression, proper dosing and titration of Pentazocine and Naloxone Tablets are essential [see ]. Overestimating the Pentazocine and Naloxone Tablets dosage when converting patients from another opioid product can result in a fatal overdose with the first dose.

Accidental ingestion of even one dose of Pentazocine and Naloxone Tablets, especially by children, can result in respiratory depression and death due to an overdose of pentazocine.

Neonatal Opioid Withdrawal Syndrome

Prolonged use of Pentazocine and Naloxone Tablets during pregnancy can result in withdrawal in the neonate. Neonatal opioid withdrawal syndrome, unlike opioid withdrawal syndrome in adults, may be life-threatening if not recognized and treated, and requires management according to protocols developed by neonatology experts. Observe newborns for signs of neonatal opioid withdrawal syndrome and manage accordingly. Advise pregnant women using opioids for a prolonged period of the risk of neonatal opioid withdrawal syndrome and ensure that appropriate treatment will be available [see ].

Risks from Concomitant Use with Benzodiazepines or Other CNS Depressants

Profound sedation, respiratory depression, coma, and death may result from the concomitant use of Pentazocine and Naloxone Tablets with benzodiazepines or other CNS depressants (e.g., non-benzodiazepine sedatives/hypnotics, anxiolytics, tranquilizers, muscle relaxants, general anesthetics, antipsychotics, other opioids, alcohol). Because of these risks, reserve concomitant prescribing of these drugs for use in patients for whom alternative treatment options are inadequate.

Observational studies have demonstrated that concomitant use of opioid analgesics and benzodiazepines increases the risk of drug-related mortality compared to use of opioid analgesics alone. Because of similar pharmacological properties, it is reasonable to expect similar risk with the concomitant use of other CNS depressant drugs with opioid analgesics .

If the decision is made to prescribe a benzodiazepine or other CNS depressant concomitantly with an opioid analgesic, prescribe the lowest effective dosages and minimum durations of concomitant use. In patients already receiving an opioid analgesic, prescribe a lower initial dose of the benzodiazepine or other CNS depressant than indicated in the absence of an opioid, and titrate based on clinical response. If an opioid analgesic is initiated in a patient already taking a benzodiazepine or other CNS depressant, prescribe a lower initial dose of the opioid analgesic, and titrate based on clinical response. Follow patients closely for signs and symptoms of respiratory depression and sedation.

Advise both patients and caregivers about the risks of respiratory depression and sedation when Pentazocine and Naloxone Tablets is used with benzodiazepines or other CNS depressants (including alcohol and illicit drugs). Advise patients not to drive or operate heavy machinery until the effects of concomitant use of the benzodiazepine or other CNS depressant have been determined. Screen patients for risk of substance use disorders, including opioid abuse and misuse, and warn them of the risk for overdose and death associated with the use of additional CNS depressants including alcohol and illicit drugs [see ].

Life-Threatening Respiratory Depression in Patients with Chronic Pulmonary Disease or in Elderly, Cachectic, or Debilitated Patients

The use of Pentazocine and Naloxone Tablets in patients with acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment is contraindicated.

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Monitor such patients closely, particularly when initiating and titrating Pentazocine and Naloxone Tablets and when Pentazocine and Naloxone Tablets are given concomitantly with other drugs that depress respiration [see ]Alternatively, consider the use of non-opioid analgesics in these patients.

Adrenal Insufficiency

Cases of adrenal insufficiency have been reported with opioid use, more often following greater than 1 month of use. Presentation of adrenal insufficiency may include non-specific symptoms and signs including nausea, vomiting, anorexia, fatigue, weakness, dizziness, and low blood pressure. If adrenal insufficiency is suspected, confirm the diagnosis with diagnostic testing as soon as possible. If adrenal insufficiency is diagnosed, treat with physiologic replacement doses of corticosteroids. Wean the patient off of the opioid to allow adrenal function to recover and continue corticosteroid treatment until adrenal function recovers. Other opioids may be tried as some cases reported use of a different opioid without recurrence of adrenal insufficiency. The information available does not identify any particular opioids as being more likely to be associated with adrenal insufficiency.

Severe Hypotension

Pentazocine and Naloxone Tablets may cause severe hypotension including orthostatic hypotension and syncope in ambulatory patients. There is increased risk in patients whose ability to maintain blood pressure has already been compromised by a reduced blood volume or concurrent administration of certain CNS depressant drugs (e.g., phenothiazines or general anesthetics) [see ]Monitor these patients for signs of hypotension after initiating or titrating the dosage of Pentazocine and Naloxone Tablets. In patients with circulatory shock, Pentazocine and Naloxone Tablets may cause vasodilation that can further reduce cardiac output and blood pressure. Avoid the use of Pentazocine and Naloxone Tablets in patients with circulatory shock.

Risks of Use in Patients with Increased Intracranial Pressure, Brain Tumors, Head Injury, or Impaired Consciousness

In patients who may be susceptible to the intracranial effects of CO2 retention (e.g., those with evidence of increased intracranial pressure or brain tumors), Pentazocine and Naloxone Tablets may reduce respiratory drive, and the resultant CO2 retention can further increase intracranial pressure. Monitor such patients for signs of sedation and respiratory depression, particularly when initiating therapy with Pentazocine and Naloxone Tablets.

Opioids may also obscure the clinical course in a patient with a head injury. Avoid the use of Pentazocine and Naloxone Tablets in patients with impaired consciousness or coma.

Risks of Use in Patients with Gastrointestinal Conditions

Pentazocine and Naloxone Tablets are contraindicated in patients with known or suspected gastrointestinal obstruction, including paralytic ileus.

The administration of Pentazocine and Naloxone Tablets or other opioids may obscure the diagnosis or clinical course in patients with acute abdominal conditions.

Pentazocine and Naloxone Tablets may cause spasm of the sphincter of Oddi. Opioids may cause increases in serum amylase. Monitor patients with biliary tract disease, including acute pancreatitis, for worsening symptoms.

Withdrawal

The use of Pentazocine and Naloxone Tablets, a mixed agonist/antagonist opioid analgesic, in patients who are receiving a full opioid agonist analgesic may reduce the analgesic effect and/or precipitate withdrawal symptoms. Avoid concomitant use of Pentazocine and Naloxone Tablets with a full opioid agonist analgesic.

When discontinuing Pentazocine and Naloxone Tablets, gradually taper the dosage (see . Do not abruptly discontinue Pentazocine and Naloxone Tablets (see )

Acute CNS Manifestations

Patients receiving therapeutic doses of Pentazocine and Naloxone Tablets have experienced hallucinations (usually visual), disorientation, and confusion which have cleared spontaneously within a period of hours. The mechanism of this reaction is not known. Such patients should be very closely observed and vital signs checked. If the drug is reinstituted, it should be done with caution since these acute CNS manifestations may recur.

The amount of naloxone present in Pentazocine and Naloxone Tablets (0.5 mg per tablet) has no action when taken orally and will not interfere with the pharmacologic action of pentazocine. However, this amount of naloxone given by injection has profound antagonistic action to narcotic analgesics.

Severe, even lethal, consequences may result from misuse of tablets by injection either alone or in combination with other substances, such as pulmonary emboli, vascular occlusion, ulceration and abscesses, and withdrawal symptoms in narcotic dependent individuals.

Increased Risk of Seizures in Patients with Seizure Disorders

The pentazocine in Pentazocine and Naloxone Tablets may increase the frequency of seizures in patients with seizure disorders, and may increase the risk of seizures occurring in other clinical settings associated with seizures. Monitor patients with a history of seizure disorders for worsened seizure control during Pentazocine and Naloxone Tablets therapy.

Risks of Driving and Operating Machinery

Pentazocine and Naloxone Tablets may impair the mental or physical abilities needed to perform potentially hazardous activities such as driving a car or operating machinery. Warn patients not to drive or operate dangerous machinery unless they are tolerant to the effects of Pentazocine and Naloxone Tablets and know how they will react to the medication .

Infertility

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Chronic use of opioids may cause reduced fertility in females and males of reproductive potential. It is not known whether these effects on fertility are reversible [see ].

What are the precautions of PENTAZOCINE HYDROCHLORIDE AND NALOXONE HYDROCHLORIDE?

Porphyria

Particular caution should be exercised in administering pentazocine to patients with porphyria since it may provoke an acute attack in susceptible individuals.

Cardiovascular Disease

Pentazocine can elevate blood pressure, possibly through the release of endogenous catecholamines. Particular caution should be exercised in conditions where alterations in vascular resistance and blood pressure might be particularly undesirable, such as in the acute phase of myocardial infarction.

Pentazocine and Naloxone Tablets should be used with caution in patients with myocardial infarction who have nausea or vomiting.

Impaired Renal or Hepatic Function

Decreased metabolism of pentazocine by the liver in extensive liver disease may predispose to accentuation of side effects. Although laboratory tests have not indicated that pentazocine causes or increases renal or hepatic impairment, the drug should be administered with caution to patients with such impairment.

Biliary Surgery

Narcotic drug products are generally considered to elevate biliary tract pressure for varying periods following their administration. Some evidence suggests that pentazocine may differ from other marketed narcotics in this respect (i.e., it causes little or no elevation in biliary tract pressures). The clinical significance of these findings, however, is not yet known.

What are the side effects of PENTAZOCINE HYDROCHLORIDE AND NALOXONE HYDROCHLORIDE?

The following adverse reactions associated with the use of Pentazocine and Naloxone were identified in clinical studies or postmarketing reports. Because some of these reactions were reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.

Cardiovascular -

Respiratory -

Acute CNS Manifestations -

Other CNS Effects -

Autonomic -

Gastrointestinal -

Allergic -

Ophthalmic -

Hematologic -

Dependence and Withdrawal Symptoms -

Other -

: Cases of serotonin syndrome, a potentially life-threatening condition, have been reported during concomitant use of opioids with serotonergic drugs.
: Cases of adrenal insufficiency have been reported with opioid use, more often following greater than one month of use.
: Anaphylaxis has been reported with ingredients contained in Pentazocine and Naloxone Tablets.
: Cases of androgen deficiency have occurred with chronic use of opioids [see ].

What should I look out for while using PENTAZOCINE HYDROCHLORIDE AND NALOXONE HYDROCHLORIDE?

Pentazocine and Naloxone Tablets are contraindicated in patients with:

What might happen if I take too much PENTAZOCINE HYDROCHLORIDE AND NALOXONE HYDROCHLORIDE?

Clinical Presentation

Acute overdose with Pentazocine and Naloxone Tablets can be manifested by respiratory depression, somnolence progressing to stupor or coma, skeletal muscle flaccidity, cold and clammy skin, constricted pupils, and, in some cases, pulmonary edema, bradycardia, hypotension, partial or complete airway obstruction, atypical snoring, and death. Marked mydriasis rather than miosis may be seen with hypoxia in overdose situations.

For pentazocine alone in single doses above 60 mg there have been reports of the occurrence of nalorphine-like psychotomimetic effects such as anxiety, nightmares, strange thoughts, and hallucinations. Somnolence, marked respiratory depression associated with hypertension and tachycardia have also resulted as have seizures, hypotension, dizziness, nausea, vomiting, lethargy, and paresthesias. The respiratory depression is antagonized by naloxone (see ). Circulatory failure and deepening coma may occur in more severe cases, particularly in patients who have also ingested other CNS depressants such as alcohol, sedative/hypnotics, or antihistamines."

Treatment of Overdose

In case of overdose, priorities are the reestablishment of a patent and protected airway and institution of assisted or controlled ventilation, if needed. Employ other supportive measures (including oxygen and vasopressors) in the management of circulatory shock and pulmonary edema as indicated. Cardiac arrest or arrhythmias will require advanced life-support techniques.

The opioid antagonist, naloxone or nalmefene, are specific antidotes to respiratory depression resulting from opioid overdose. For clinically significant respiratory or circulatory depression secondary to pentazocine overdose, administer an opioid antagonist. As pentazocine is a mixed opioid agonist/antagonist, larger doses of naloxone or nalmefene may be needed to reverse the effects of an overdose.

Opioid antagonists should not be administered in the absence of clinically significant respiratory or circulatory depression secondary to pentazocine overdose.

In an individual physically dependent on opioids, administration of the recommended usual dosage of the antagonist will precipitate an acute withdrawal syndrome. The severity of the withdrawal symptoms experienced will depend on the degree of physical dependence and the dose of the antagonist administered. If a decision is made to treat serious respiratory depression in the physically dependent patient, administration of the antagonist should be begun with care and by titration with smaller than usual doses of the antagonist.

How should I store and handle PENTAZOCINE HYDROCHLORIDE AND NALOXONE HYDROCHLORIDE?

Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.] Protect from moisture.Dispense in a tight, light-resistant container as defined in the USP. FOR YOUR PROTECTION:DEA Order Form Required.To request medical information or to report Suspected Adverse Reactions, contact Alvogen Customer Service at 1-866-770-3024 or FDA at 1-800-FDA-1088 or Made in USAStore at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.] Protect from moisture.Dispense in a tight, light-resistant container as defined in the USP. FOR YOUR PROTECTION:DEA Order Form Required.To request medical information or to report Suspected Adverse Reactions, contact Alvogen Customer Service at 1-866-770-3024 or FDA at 1-800-FDA-1088 or Made in USAStore at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.] Protect from moisture.Dispense in a tight, light-resistant container as defined in the USP. FOR YOUR PROTECTION:DEA Order Form Required.To request medical information or to report Suspected Adverse Reactions, contact Alvogen Customer Service at 1-866-770-3024 or FDA at 1-800-FDA-1088 or Made in USAStore at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.] Protect from moisture.Dispense in a tight, light-resistant container as defined in the USP. FOR YOUR PROTECTION:DEA Order Form Required.To request medical information or to report Suspected Adverse Reactions, contact Alvogen Customer Service at 1-866-770-3024 or FDA at 1-800-FDA-1088 or Made in USAStore at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.] Protect from moisture.Dispense in a tight, light-resistant container as defined in the USP. FOR YOUR PROTECTION:DEA Order Form Required.To request medical information or to report Suspected Adverse Reactions, contact Alvogen Customer Service at 1-866-770-3024 or FDA at 1-800-FDA-1088 or Made in USAStore at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.] Protect from moisture.Dispense in a tight, light-resistant container as defined in the USP. FOR YOUR PROTECTION:DEA Order Form Required.To request medical information or to report Suspected Adverse Reactions, contact Alvogen Customer Service at 1-866-770-3024 or FDA at 1-800-FDA-1088 or Made in USAPentazocine and Naloxone Tablets USP are light yellow, capsule shaped tablets debossed "NL" on left side and "680" on the right side of the bisect and plain on the other side, supplied in bottles of 100 and 500.Bottles of 100 (NDC 43386-680-01).Bottles of 500 (NDC 43386-680-05).Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature]. Dispense in a tight, light-resistant container as defined in the USP. Manufactured by:Novel Laboratories, Inc.Somerset, NJ 08873Manufactured for:Lupin Pharmaceuticals, Inc.Baltimore, MD 21202PI6800000205Rev. 12/2016Pentazocine and Naloxone Tablets USP are light yellow, capsule shaped tablets debossed "NL" on left side and "680" on the right side of the bisect and plain on the other side, supplied in bottles of 100 and 500.Bottles of 100 (NDC 43386-680-01).Bottles of 500 (NDC 43386-680-05).Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature]. Dispense in a tight, light-resistant container as defined in the USP. Manufactured by:Novel Laboratories, Inc.Somerset, NJ 08873Manufactured for:Lupin Pharmaceuticals, Inc.Baltimore, MD 21202PI6800000205Rev. 12/2016Pentazocine and Naloxone Tablets USP are light yellow, capsule shaped tablets debossed "NL" on left side and "680" on the right side of the bisect and plain on the other side, supplied in bottles of 100 and 500.Bottles of 100 (NDC 43386-680-01).Bottles of 500 (NDC 43386-680-05).Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature]. Dispense in a tight, light-resistant container as defined in the USP. Manufactured by:Novel Laboratories, Inc.Somerset, NJ 08873Manufactured for:Lupin Pharmaceuticals, Inc.Baltimore, MD 21202PI6800000205Rev. 12/2016Pentazocine and Naloxone Tablets USP are light yellow, capsule shaped tablets debossed "NL" on left side and "680" on the right side of the bisect and plain on the other side, supplied in bottles of 100 and 500.Bottles of 100 (NDC 43386-680-01).Bottles of 500 (NDC 43386-680-05).Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature]. Dispense in a tight, light-resistant container as defined in the USP. Manufactured by:Novel Laboratories, Inc.Somerset, NJ 08873Manufactured for:Lupin Pharmaceuticals, Inc.Baltimore, MD 21202PI6800000205Rev. 12/2016Pentazocine and Naloxone Tablets USP are light yellow, capsule shaped tablets debossed "NL" on left side and "680" on the right side of the bisect and plain on the other side, supplied in bottles of 100 and 500.Bottles of 100 (NDC 43386-680-01).Bottles of 500 (NDC 43386-680-05).Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature]. Dispense in a tight, light-resistant container as defined in the USP. Manufactured by:Novel Laboratories, Inc.Somerset, NJ 08873Manufactured for:Lupin Pharmaceuticals, Inc.Baltimore, MD 21202PI6800000205Rev. 12/2016Pentazocine and Naloxone Tablets USP are light yellow, capsule shaped tablets debossed "NL" on left side and "680" on the right side of the bisect and plain on the other side, supplied in bottles of 100 and 500.Bottles of 100 (NDC 43386-680-01).Bottles of 500 (NDC 43386-680-05).Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature]. Dispense in a tight, light-resistant container as defined in the USP. Manufactured by:Novel Laboratories, Inc.Somerset, NJ 08873Manufactured for:Lupin Pharmaceuticals, Inc.Baltimore, MD 21202PI6800000205Rev. 12/2016Pentazocine and Naloxone Tablets USP are light yellow, capsule shaped tablets debossed "NL" on left side and "680" on the right side of the bisect and plain on the other side, supplied in bottles of 100 and 500.Bottles of 100 (NDC 43386-680-01).Bottles of 500 (NDC 43386-680-05).Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature]. Dispense in a tight, light-resistant container as defined in the USP. Manufactured by:Novel Laboratories, Inc.Somerset, NJ 08873Manufactured for:Lupin Pharmaceuticals, Inc.Baltimore, MD 21202PI6800000205Rev. 12/2016Pentazocine and Naloxone Tablets USP are light yellow, capsule shaped tablets debossed "NL" on left side and "680" on the right side of the bisect and plain on the other side, supplied in bottles of 100 and 500.Bottles of 100 (NDC 43386-680-01).Bottles of 500 (NDC 43386-680-05).Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature]. Dispense in a tight, light-resistant container as defined in the USP. Manufactured by:Novel Laboratories, Inc.Somerset, NJ 08873Manufactured for:Lupin Pharmaceuticals, Inc.Baltimore, MD 21202PI6800000205Rev. 12/2016Pentazocine and Naloxone Tablets USP are light yellow, capsule shaped tablets debossed "NL" on left side and "680" on the right side of the bisect and plain on the other side, supplied in bottles of 100 and 500.Bottles of 100 (NDC 43386-680-01).Bottles of 500 (NDC 43386-680-05).Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature]. Dispense in a tight, light-resistant container as defined in the USP. Manufactured by:Novel Laboratories, Inc.Somerset, NJ 08873Manufactured for:Lupin Pharmaceuticals, Inc.Baltimore, MD 21202PI6800000205Rev. 12/2016Pentazocine and Naloxone Tablets USP are light yellow, capsule shaped tablets debossed "NL" on left side and "680" on the right side of the bisect and plain on the other side, supplied in bottles of 100 and 500.Bottles of 100 (NDC 43386-680-01).Bottles of 500 (NDC 43386-680-05).Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature]. Dispense in a tight, light-resistant container as defined in the USP. Manufactured by:Novel Laboratories, Inc.Somerset, NJ 08873Manufactured for:Lupin Pharmaceuticals, Inc.Baltimore, MD 21202PI6800000205Rev. 12/2016Pentazocine and Naloxone Tablets USP are light yellow, capsule shaped tablets debossed "NL" on left side and "680" on the right side of the bisect and plain on the other side, supplied in bottles of 100 and 500.Bottles of 100 (NDC 43386-680-01).Bottles of 500 (NDC 43386-680-05).Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature]. Dispense in a tight, light-resistant container as defined in the USP. Manufactured by:Novel Laboratories, Inc.Somerset, NJ 08873Manufactured for:Lupin Pharmaceuticals, Inc.Baltimore, MD 21202PI6800000205Rev. 12/2016Pentazocine and Naloxone Tablets USP are light yellow, capsule shaped tablets debossed "NL" on left side and "680" on the right side of the bisect and plain on the other side, supplied in bottles of 100 and 500.Bottles of 100 (NDC 43386-680-01).Bottles of 500 (NDC 43386-680-05).Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature]. Dispense in a tight, light-resistant container as defined in the USP. Manufactured by:Novel Laboratories, Inc.Somerset, NJ 08873Manufactured for:Lupin Pharmaceuticals, Inc.Baltimore, MD 21202PI6800000205Rev. 12/2016Pentazocine and Naloxone Tablets USP are light yellow, capsule shaped tablets debossed "NL" on left side and "680" on the right side of the bisect and plain on the other side, supplied in bottles of 100 and 500.Bottles of 100 (NDC 43386-680-01).Bottles of 500 (NDC 43386-680-05).Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature]. Dispense in a tight, light-resistant container as defined in the USP. Manufactured by:Novel Laboratories, Inc.Somerset, NJ 08873Manufactured for:Lupin Pharmaceuticals, Inc.Baltimore, MD 21202PI6800000205Rev. 12/2016

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Clinical Information

Chemical Structure

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Clinical Pharmacology

Mechanism of Action

Pentazocine is a mixed agonist-antagonist at opioid receptors. Pentazocine is a partial agonist at the mu opioid receptor and an agonist at the kappa opioid receptor.

Naloxone is an opioid antagonist.

Pharmacodynamics

Effects on the Central Nervous System

Pentazocine produces respiratory depression by direct action on brain stem respiratory centers. The respiratory depression involves a reduction in the responsiveness of the brain stem respiratory centers to both increases in carbon dioxide tension and electrical stimulation.

Pentazocine causes miosis, even in total darkness. Pinpoint pupils are a sign of opioid overdose but are not pathognomonic (e.g., pontine lesions of hemorrhagic or ischemic origins may produce similar findings). Marked mydriasis rather than miosis may be seen due to hypoxia in overdose situations.

Effects on the Gastrointestinal Tract and Other Smooth Muscle

Pentazocine causes a reduction in motility associated with an increase in smooth muscle tone in the antrum of the stomach and duodenum. Digestion of food in the small intestine is delayed and propulsive contractions are decreased. Propulsive peristaltic waves in the colon are decreased, while tone may be increased to the point of spasm, resulting in constipation. Other opioid- induced effects may include a reduction in biliary and pancreatic secretions, spasm of sphincter of Oddi, and transient elevations in serum amylase.

Effects on the Cardiovascular System

Pentazocine produces peripheral vasodilation which may result in orthostatic hypotension or syncope. Manifestations of histamine release and/or peripheral vasodilation may include pruritus, flushing, red eyes, sweating, and/or orthostatic hypotension.

Effects on the Endocrine System

Opioids inhibit the secretion of adrenocorticotropic hormone (ACTH), cortisol, and luteinizing hormone (LH) in humans see ]. They also stimulate prolactin, growth hormone (GH) secretion, and pancreatic secretion of insulin and glucagon.

Chronic use of opioids may influence the hypothalamic-pituitary-gonadal axis, leading to androgen deficiency that may manifest as low libido, impotence, erectile dysfunction, amenorrhea, or infertility. The causal role of opioids in the clinical syndrome of hypogonadism is unknown because the various medical, physical, lifestyle, and psychological stressors that may influence gonadal hormone levels have not been adequately controlled for in studies conducted to date [see ].

Effects on the Immune System

Opioids have been shown to have a variety of effects on components of the immune system. The clinical significance of these findings is unknown. Overall, the effects of opioids appear to be modestly immunosuppressive.

Concentration–Efficacy Relationships

The minimum effective analgesic concentration will vary widely among patients, especially among patients who have been previously treated with potent agonist opioids. The minimum effective analgesic concentration of pentazocine for any individual patient may increase over time due to an increase in pain, the development of a new pain syndrome, and/or the development of analgesic tolerance [see ].

Concentration–Adverse Reaction Relationships

There is a relationship between increasing pentazocine plasma concentration and increasing frequency of dose-related opioid adverse reactions such as nausea, vomiting, CNS effects, and respiratory depression. In opioid-tolerant patients, the situation may be altered by the development of tolerance to opioid-related adverse reactions [see ].

Opioid Antagonist Effects

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.

Naloxone when administered orally at 0.5 mg has no pharmacologic activity. Naloxone hydrochloride administered parenterally at the same dose is an antagonist to pentazocine and a pure antagonist to narcotic analgesics.

Pentazocine and Naloxone Tablets are a potent analgesic when administered orally. However, the presence of naloxone in Pentazocine and Naloxone Tablets is intended to prevent the effect of pentazocine if the product is misused by injection.

Studies in animals indicate that the presence of naloxone does not affect pentazocine analgesia when the combination is given orally. If the combination is given by injection the action of pentazocine is neutralized.

Pharmacokinetics

Onset of significant analgesia usually occurs between 15 and 30 minutes after oral administration, and duration of action is usually three hours or longer.

Pentazocine is well absorbed from the gastrointestinal tract. Concentrations in plasma coincide closely with 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).

Pentazocine is metabolized in the liver and excreted primarily 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 into the fetal circulation.

Non-Clinical Toxicology

Pentazocine and Naloxone Tablets are contraindicated in patients with:

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See and

for interaction with CNS drugs and alcohol. Methocarbamol may inhibit the effect of pyridostigmine bromide. Therefore, methocarbamol should be used with caution in patients with myasthenia gravis receiving anticholinesterase agents.

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Particular caution should be exercised in administering pentazocine to patients with porphyria since it may provoke an acute attack in susceptible individuals.

The following adverse reactions associated with the use of Pentazocine and Naloxone were identified in clinical studies or postmarketing reports. Because some of these reactions were reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.

Cardiovascular -

Respiratory -

Acute CNS Manifestations -

Other CNS Effects -

Autonomic -

Gastrointestinal -

Allergic -

Ophthalmic -

Hematologic -

Dependence and Withdrawal Symptoms -

Other -

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Reference

This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"

While we update our database periodically, we cannot guarantee it is always updated to the latest version.

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Clonazepam Description Each single-scored tablet, for oral administration, contains 0.5 mg, 1 mg, or 2 mg Clonazepam, USP, a benzodiazepine. Each tablet also contains corn starch, lactose monohydrate, magnesium stearate, microcrystalline cellulose, and povidone. Clonazepam tablets USP 0.5 mg contain Yellow D&C No. 10 Aluminum Lake. Clonazepam tablets USP 1 mg contain Yellow D&C No. 10 Aluminum Lake, as well as FD&C Blue No. 1 Aluminum Lake. Chemically, Clonazepam, USP is 5-(o-chlorophenyl)-1,3-dihydro-7-nitro-2H-1,4-benzodiazepin-2-one. It is a light yellow crystalline powder. It has the following structural formula: C15H10ClN3O3 M.W. 315.72

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Interactions

A total of 440 drugs (1549 brand and generic names) are known to interact with Imbruvica (ibrutinib). 228 major drug interactions (854 brand and generic names) 210 moderate drug interactions (691 brand and generic names) 2 minor drug interactions (4 brand and generic names) Show all medications in the database that may interact with Imbruvica (ibrutinib).

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