Codeine Sulfate

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Overview

What is Codeine Sulfate?

Chemically, codeine is Morphinan-6-ol,7,8-didehydro-4,5-epoxy-3-methoxy-17-methyl-(5α,6α)-, sulfate (2:1) (salt), trihydrate. Its empirical formula is CHNO and its molecular weight is 299.36.

Its structure is as follows:

Each tablet contains 15, 30, or 60 mg of codeine sulfate and the following inactive ingredients: colloidal silicon dioxide, microcrystalline cellulose, pregelatinized starch, and stearic acid.

What does Codeine Sulfate look like?

What are the available doses of Codeine Sulfate?

Each 15 mg tablet for oral administration contains 15 mg of codeine sulfate. It is a white, biconvex tablet scored on one side, with strength-indicating number “15” debossed on the scored side and product identification number “54 613” debossed on the other side.

Each 30 mg tablet for oral administration contains 30 mg of codeine sulfate. It is a white, biconvex tablet scored on one side, with strength-indicating number “30” debossed on the scored side and product identification number “54 783” debossed on the other side.

Each 60 mg tablet for oral administration contains 60 mg of codeine sulfate. It is a white, biconvex tablet scored on one side, with strength-indicating number “60” debossed on the scored side and product identification number “54 412” debossed on the other side.

What should I talk to my health care provider before I take Codeine Sulfate?

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How should I use Codeine Sulfate?

Codeine sulfate is an opioid analgesic indicated for the relief of mild to moderately severe pain where the use of an opioid analgesic is appropriate.

Selection of patients for treatment with codeine sulfate should be governed by the same principles that apply to the use of similar opioid analgesics. Physicians should individualize treatment in every case, using non-opioid analgesics, opioids on an as needed basis and/or combination products, and chronic opioid therapy in a progressive plan of pain management.

As with any opioid drug product, adjust the dosing regimen for each patient individually, taking into account the patient’s prior analgesic treatment experience. In the selection of the initial dose of codeine sulfate, attention should be given to the following:

• the total daily dose, potency and specific characteristics of the opioid the patient has been taking previously;

• the reliability of the relative potency estimate used to calculate the equivalent codeine sulfate dose needed;

• the patient’s degree of opioid tolerance;

• the general condition and medical status of the patient;

• concurrent medications;

• the type and severity of the patient’s pain;

• risk factors for abuse, addiction or diversion, including a prior history of abuse, addiction or diversion.

The following dosing recommendations, therefore, can only be considered suggested approaches to what is actually a series of clinical decisions over time in the management of the pain of each individual patient.

Continual re-evaluation of the patient receiving codeine sulfate is important, with special attention to the maintenance of pain control and the relative incidence of side effects associated with therapy. During chronic therapy, especially for noncancer-related pain, the continued need for the use of opioid analgesics should be re-assessed as appropriate.

During periods of changing analgesic requirements, including initial titration, frequent contact is recommended between physician, other members of the healthcare team, the patient, and the caregiver/family.

The usual adult dosage for tablets is 15 mg to 60 mg repeated up to every four hours as needed for pain. The maximum 24 hour dose is 360 mg.

The initial dose should be titrated based upon the individual patient’s response to their initial dose of codeine. This dose can then be adjusted to an acceptable level of analgesia taking into account the improvement in pain intensity and the tolerability of the codeine by the patient.

It should be kept in mind, however, that tolerance to codeine sulfate can develop with continued use and that the incidence of untoward effects is dose-related. Adult doses of codeine higher than 60 mg fail to give commensurate relief of pain and are associated with an appreciably increased incidence of undesirable side effects.

When the patient no longer requires therapy with codeine sulfate, doses should be tapered gradually to prevent signs and symptoms of withdrawal in the physically dependent patient.

What interacts with Codeine Sulfate?

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What are the warnings of Codeine Sulfate?

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What are the precautions of Codeine Sulfate?

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What are the side effects of Codeine Sulfate?

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What should I look out for while using Codeine Sulfate?

Codeine sulfate is contraindicated in patients with known hypersensitivity to codeine or any components of the product. Persons known to be hypersensitive to certain other opioids may exhibit cross-sensitivity to codeine.

Codeine sulfate is contraindicated in patients with respiratory depression in the absence of resuscitative equipment.

Codeine sulfate is contraindicated in patients with acute or severe bronchial asthma or hypercarbia.

Codeine sulfate is contraindicated in any patient who has or is suspected of having paralytic ileus.

What might happen if I take too much Codeine Sulfate?

Acute overdose of codeine is characterized by respiratory depression (a decrease in respiratory rate and/or tidal volume, Cheyne-Stokes respiration, cyanosis), extreme somnolence progressing to stupor or coma, miosis (mydriasis may occur in terminal narcosis or severe hypoxia), skeletal muscle flaccidity, cold and clammy skin, and sometimes bradycardia and hypotension. In severe overdosage, apnea, circulatory collapse, cardiac arrest, and death may occur.

Codeine sulfate may cause 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 origin may produce similar findings). Marked mydriasis rather than miosis may be seen with hypoxia in overdose situations.

Primary attention should be given to the re-establishment of adequate respiratory exchange through provision of a patent airway and institution of assisted or controlled ventilation as necessary. Supportive measures (including oxygen and vasopressors) should be employed in the management of circulatory shock and pulmonary edema accompanying overdose as indicated. Cardiac arrest or arrhythmias may require cardiac massage or defibrillation. Induction of emesis is not recommended because of the potential for CNS depression and seizures. Activated charcoal is recommended if the patient is awake and able to protect his/her airway. In persons who are at risk for abrupt onset of seizures or mental status depression, activated charcoal should be administered by medical or paramedical personnel capable of airway management to prevent aspiration in the event of spontaneous emesis. Severe agitation or seizures should be treated with an intravenous benzodiazepine.

The opioid antagonist naloxone hydrochloride is a specific antidote against respiratory depression resulting from overdosage or unusual sensitivity to opiate agonists, including codeine. Therefore, an appropriate dose of naloxone hydrochloride (see prescribing information for naloxone hydrochloride) should be administered, preferably by the intravenous route, simultaneously with efforts at respiratory resuscitation. Since the duration of action of codeine may exceed that of the antagonist, the patient should be kept under continued surveillance and repeated doses of the antagonist should be administered as needed to maintain adequate respiration. A narcotic antagonist should not be administered in the absence of clinically significant respiratory or cardiovascular depression secondary to codeine sulfate overdose.

In an individual physically dependent on opioids, administration of the usual dose 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. Use of an opioid antagonist should be reserved for cases where such treatment is clearly needed. If it is necessary to treat serious respiratory depression in the physically dependent patient, administration of the antagonist should be initiated with care and titrated with smaller than usual doses.

How should I store and handle Codeine Sulfate?

Store at controlled room temperature 20° to 25°C (68° to 77°F) [see USP] .Codeine SulfateNDC 54868-2541-0: Bottles of 10 TabletsNDC 54868-2541-1: Bottles of 30 TabletsNDC 54868-2541-2: Bottles of 60 Tablets StorageStore at Controlled Room Temperature, 15º to 30ºC (59º to 86ºF). Protect from moisture and light. Dispense in well-closed container as defined in the USP/NF.All opioids are liable to diversion and misuse both by the general public and healthcare workers and should be handled accordingly.Codeine SulfateNDC 54868-2541-0: Bottles of 10 TabletsNDC 54868-2541-1: Bottles of 30 TabletsNDC 54868-2541-2: Bottles of 60 Tablets StorageStore at Controlled Room Temperature, 15º to 30ºC (59º to 86ºF). Protect from moisture and light. Dispense in well-closed container as defined in the USP/NF.All opioids are liable to diversion and misuse both by the general public and healthcare workers and should be handled accordingly.Codeine SulfateNDC 54868-2541-0: Bottles of 10 TabletsNDC 54868-2541-1: Bottles of 30 TabletsNDC 54868-2541-2: Bottles of 60 Tablets StorageStore at Controlled Room Temperature, 15º to 30ºC (59º to 86ºF). Protect from moisture and light. Dispense in well-closed container as defined in the USP/NF.All opioids are liable to diversion and misuse both by the general public and healthcare workers and should be handled accordingly.Codeine SulfateNDC 54868-2541-0: Bottles of 10 TabletsNDC 54868-2541-1: Bottles of 30 TabletsNDC 54868-2541-2: Bottles of 60 Tablets StorageStore at Controlled Room Temperature, 15º to 30ºC (59º to 86ºF). Protect from moisture and light. Dispense in well-closed container as defined in the USP/NF.All opioids are liable to diversion and misuse both by the general public and healthcare workers and should be handled accordingly.Codeine SulfateNDC 54868-2541-0: Bottles of 10 TabletsNDC 54868-2541-1: Bottles of 30 TabletsNDC 54868-2541-2: Bottles of 60 Tablets StorageStore at Controlled Room Temperature, 15º to 30ºC (59º to 86ºF). Protect from moisture and light. Dispense in well-closed container as defined in the USP/NF.All opioids are liable to diversion and misuse both by the general public and healthcare workers and should be handled accordingly.Codeine SulfateNDC 54868-2541-0: Bottles of 10 TabletsNDC 54868-2541-1: Bottles of 30 TabletsNDC 54868-2541-2: Bottles of 60 Tablets StorageStore at Controlled Room Temperature, 15º to 30ºC (59º to 86ºF). Protect from moisture and light. Dispense in well-closed container as defined in the USP/NF.All opioids are liable to diversion and misuse both by the general public and healthcare workers and should be handled accordingly.Codeine SulfateNDC 54868-2541-0: Bottles of 10 TabletsNDC 54868-2541-1: Bottles of 30 TabletsNDC 54868-2541-2: Bottles of 60 Tablets StorageStore at Controlled Room Temperature, 15º to 30ºC (59º to 86ºF). Protect from moisture and light. Dispense in well-closed container as defined in the USP/NF.All opioids are liable to diversion and misuse both by the general public and healthcare workers and should be handled accordingly.Codeine SulfateNDC 54868-2541-0: Bottles of 10 TabletsNDC 54868-2541-1: Bottles of 30 TabletsNDC 54868-2541-2: Bottles of 60 Tablets StorageStore at Controlled Room Temperature, 15º to 30ºC (59º to 86ºF). Protect from moisture and light. Dispense in well-closed container as defined in the USP/NF.All opioids are liable to diversion and misuse both by the general public and healthcare workers and should be handled accordingly.Codeine SulfateNDC 54868-2541-0: Bottles of 10 TabletsNDC 54868-2541-1: Bottles of 30 TabletsNDC 54868-2541-2: Bottles of 60 Tablets StorageStore at Controlled Room Temperature, 15º to 30ºC (59º to 86ºF). Protect from moisture and light. Dispense in well-closed container as defined in the USP/NF.All opioids are liable to diversion and misuse both by the general public and healthcare workers and should be handled accordingly.

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Clinical Information

Chemical Structure

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Clinical Pharmacology

Codeine sulfate is an opioid analgesic, related to morphine, but with less potent analgesic properties. Codeine is selective for the mu receptor, but with a much weaker affinity than morphine. The analgesic properties of codeine have been speculated to come from its conversion to morphine, although the exact mechanism of analgesic action remains unknown.

The principal therapeutic action of codeine sulfate is analgesia. Although the precise mechanism of the analgesic action is unknown, specific CNS opiate receptors and endogenous compounds with morphine-like activity have been identified throughout the brain and spinal cord and are likely to play a role in the expression and perception of analgesic effects. Some other CNS effects of codeine include anxiolysis, euphoria, and feelings of relaxation. Codeine sulfate causes respiratory depression, in part by a direct effect on the brainstem respiratory centers. Codeine sulfate and other related opioids depress the cough reflex by direct effect on the cough center in the medulla. Codeine sulfate may also cause miosis.

Gastric, biliary and pancreatic secretions may be decreased by codeine. Codeine also causes a reduction in motility and is associated with an increase in 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 is increased to the point of spasm. The end result may be constipation. Codeine can cause a marked increase in biliary tract pressure as a result of the spasm of the sphincter of Oddi. Codeine may also cause spasms of the sphincter of the urinary bladder.

Codeine produces peripheral vasodilation which may result in orthostatic hypotension and fainting. Release of histamine can occur, which may play a role in opioid-induced hypotension. Manifestations of histamine release and/or peripheral vasodilation may include pruritus, flushing, red eyes, and sweating.

Opioid agonists such as codeine sulfate have been shown to have a variety of effects on the secretion of hormones. Opioids inhibit the secretion of ACTH, cortisol, and luteinizing hormone (LH) in humans. They also stimulate prolactin, growth hormone (GH) secretion, and pancreatic secretion of insulin and glucagons in humans and other species, rats and dogs. Thyroid stimulating hormone (TSH) has been shown to be both inhibited and stimulated by opioids.

Codeine has been shown to have a variety of effects on components of the immune system in and animal models. The clinical significance of these findings is unknown.

Codeine concentrations do not correlate with brain concentration or relief of pain.

The minimum effective concentration varies widely and is influenced by a variety of factors, including the extent of previous opioid use, age and general medical condition. Effective doses in tolerant patients may be significantly higher than in opioid-naïve patients.

Codeine is absorbed from the gastrointestinal tract with maximum plasma concentration occurring 60 minutes post administration.

When 60 mg codeine sulfate was administered 30 minutes after ingesting a high fat/high calorie meal, there was no significant change in the rate and extent of absorption of codeine.

Administration of 15 mg codeine sulfate every four hours for 5 days resulted in steady-state concentrations of codeine, morphine, morphine-3-glucuronide (M3G) and morphine-6-glucuronide (M6G) within 48 hours.

Codeine has been reported to have an apparent volume of distribution of approximately 3-6 L/kg, indicating extensive distribution of the drug into tissues. Codeine has low plasma protein binding with about 7-25% of codeine bound to plasma proteins.

About 70-80% of the administered dose of codeine is metabolized by conjugation with glucuronic acid to codeine-6-glucuronide (C6G) and via -demethylation to morphine (about 5-10%) and -demethylation to norcodeine (about 10%) respectively. UDP-glucuronosyltransferase (UGT) 2B7 and 2B4 are the major enzymes mediating glucurodination of codeine to C6G. Cytochrome P450 2D6 is the major enzyme responsible for conversion of codeine to morphine and P450 3A4 is the major enzyme mediating conversion of codeine to norcodeine. Morphine and norcodeine are further metabolized by conjugation with glucuronic acid. The glucuronide metabolites of morphine are morphine-3-glucuronide (M3G) and morphine-6-glucuronide (M6G). Morphine and M6G are known to have analgesic activity in humans. The analgesic activity of C6G in humans is unknown. Norcodeine and M3G are generally not considered to possess analgesic properties.

Approximately 90% of the total dose of codeine is excreted through the kidneys, of which approximately 10% is unchanged codeine. Plasma half-lives of codeine and its metabolites have been reported to be approximately 3 hours.

Non-Clinical Toxicology

Codeine sulfate is contraindicated in patients with known hypersensitivity to codeine or any components of the product. Persons known to be hypersensitive to certain other opioids may exhibit cross-sensitivity to codeine.

Codeine sulfate is contraindicated in patients with respiratory depression in the absence of resuscitative equipment.

Codeine sulfate is contraindicated in patients with acute or severe bronchial asthma or hypercarbia.

Codeine sulfate is contraindicated in any patient who has or is suspected of having paralytic ileus.

Drug Interactions:

Respiratory depression is the primary risk of codeine sulfate. Respiratory depression occurs more frequently in elderly or debilitated patients and in those suffering from conditions accompanied by hypoxia, hypercapnia, or upper airway obstruction, in whom even moderate therapeutic doses may significantly decrease pulmonary ventilation. Codeine produces dose-related respiratory depression.

Caution should be exercised when codeine sulfate is used postoperatively, in patients with pulmonary disease or shortness of breath, or whenever ventilatory function is depressed. Opioid related respiratory depression occurs more frequently in elderly or debilitated patients and in those suffering from conditions accompanied by hypoxia, hypercapnia, or upper airway obstruction, in whom even moderate therapeutic doses may significantly decrease pulmonary ventilation. Opioids, including codeine sulfate, should be used with extreme caution in patients with chronic obstructive pulmonary disease or cor pulmonale and in patients having a substantially decreased respiratory reserve (e.g., severe kyphoscoliosis), hypoxia, hypercapnia, or pre-existing respiratory depression. In such patients, even usual therapeutic doses of codeine sulfate may increase airway resistance and decrease respiratory drive to the point of apnea. Alternative non-opioid analgesics should be considered, and codeine sulfate should be employed only under careful medical supervision at the lowest effective dose in such patients. [see 10 OVERDOSAGE]

Codeine sulfate is an opioid agonist of the morphine-type and a Schedule II controlled substance. Such drugs are sought by drug abusers and people with addiction disorders. Diversion of Schedule II products is an act subject to criminal penalty.

Codeine can be abused in a manner similar to other opioid agonists, legal or illicit. This should be considered when prescribing or dispensing codeine sulfate in situations where the physician or pharmacist is concerned about an increased risk of misuse, abuse, or diversion.

Misuse and abuse of codeine sulfate poses a significant risk to the abuser that could result in overdose and death. Codeine may be abused by crushing, chewing, snorting or injecting the product. [see 9 DRUG ABUSE AND DEPENDENCE]

Concerns about abuse and addiction should not prevent the proper management of pain. Healthcare professionals should contact their State Professional Licensing Board or State Controlled Substances Authority for information on how to prevent and detect abuse or diversion of this product.

Codeine sulfate may be expected to have additive effects when used in conjunction with alcohol, other opioids, or illicit drugs that cause central nervous system depression, because respiratory depression, hypotension, profound sedation, coma or death may result.

Respiratory depressant effects of opioids and their capacity to elevate cerebrospinal fluid pressure resulting from vasodilation following CO retention may be markedly exaggerated in the presence of head injury, other intracranial lesions or a pre-existing increase in intracranial pressure. Furthermore, opioids including codeine sulfate, produce adverse reactions which may obscure the clinical course of patients with head injuries.

Codeine sulfate may cause severe hypotension in an individual whose ability to maintain blood pressure has already been compromised by a depleted blood volume or concurrent administration of drugs such as phenothiazines or general anesthetics. Codeine sulfate may produce orthostatic hypotension and syncope in ambulatory patients.

Codeine sulfate should be administered with caution to patients in circulatory shock, as vasodilation produced by the drug may further reduce cardiac output and blood pressure.

Codeine sulfate should not be administered to patients with gastrointestinal obstruction, especially paralytic ileus because codeine sulfate diminishes propulsive peristaltic waves in the gastrointestinal tract and may prolong the obstruction.

Chronic use of opioids, including codeine sulfate, may result in obstructive bowel disease especially in patients with underlying intestinal motility disorder. Codeine sulfate may cause or aggravate constipation.

Administration of codeine sulfate may obscure the diagnosis or clinical course of patients with acute abdominal conditions.

Codeine sulfate should be used in caution in patients with biliary tract disease, including acute pancreatitis, as codeine sulfate may cause spasm of the sphincter of Oddi and diminish biliary and pancreatic secretions.

As with other opioids, codeine sulfate should be used with caution in elderly or debilitated patients and those with severe impairment of hepatic or renal function, hypothyrodism, Addison’s disease, prostatic hypertrophy or urethral stricture. [see 8 USE IN SPECIFIC POPULATIONS] The usual precautions should be observed and the possibility of respiratory depression should be kept in mind.

Caution should be exercised in the administration of codeine sulfate to patients with CNS depression, acute alcoholism, and delirium tremens.

All opioids may aggravate convulsions in patients with convulsive disorders, and all opioids may induce or aggravate seizures in some clinical settings.

Some individuals may be ultra-rapid metabolizers due to a specific CYP2D6*2x2 genotype. These individuals convert codeine into its active metabolite, morphine, more rapidly and completely than other people. This rapid conversion results in higher than expected serum morphine levels. Even at labeled dosage regimens, individuals who are ultra-rapid metabolizers may experience overdose symptoms such as extreme sleepiness, confusion, or shallow breathing.

The prevalence of this CYP2D6 phenotype varies widely and has been estimated at 0.5 to 1% in Chinese and Japanese, 0.5 to 1% in Hispanics, 1 to 10% in Caucasians, 3% in African Americans, and 16 to 28% in North Africans, Ethiopians, and Arabs. Data are not available for other ethnic groups.

When physicians prescribe codeine-containing drugs, they should choose the lowest effective dose for the shortest period of time and inform their patients about these risks and the signs of morphine overdose. [see 8 USE IN SPECIFIC POPULATIONS]

Patients should be cautioned that codeine sulfate could impair the mental and/or physical abilities needed to perform potentially hazardous activities such as driving a car or operating machinery.

Patients should also be cautioned about the potential combined effects of codeine sulfate with other CNS depressants, including opioids, phenothiazines, sedative/hypnotics, and alcohol. [see 7 DRUG INTERACTIONS]

Serious adverse reactions associated with codeine are respiratory depression and, to a lesser degree, circulatory depression, respiratory arrest, shock, and cardiac arrest.

The most frequently observed adverse reactions with codeine administration include drowsiness, lightheadedness, dizziness, sedation, shortness of breath, nausea, vomiting, sweating, and constipation.

Other adverse reactions include allergic reactions, euphoria, dysphoria, abdominal pain, and pruritis.

Other less frequently observed adverse reactions expected from opioid analgesics, including codeine sulfate, include:

Cardiovascular system:

Digestive System:

Nervous system:

Skin and Appendages:

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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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Codeine Sulfate

Overview

What is Codeine Sulfate?

What does Codeine Sulfate look like?

What are the available doses of Codeine Sulfate?

What should I talk to my health care provider before I take Codeine Sulfate?

How should I use Codeine Sulfate?

What interacts with Codeine Sulfate?

What are the warnings of Codeine Sulfate?

What are the precautions of Codeine Sulfate?

What are the side effects of Codeine Sulfate?

What should I look out for while using Codeine Sulfate?

What might happen if I take too much Codeine Sulfate?

How should I store and handle Codeine Sulfate?

Clinical Information

Chemical Structure

Clinical Pharmacology

Non-Clinical Toxicology

Reference

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

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Codeine Sulfate

Overview

What is Codeine Sulfate?

What does Codeine Sulfate look like?

What are the available doses of Codeine Sulfate?

What should I talk to my health care provider before I take Codeine Sulfate?

How should I use Codeine Sulfate?

What interacts with Codeine Sulfate?

What are the warnings of Codeine Sulfate?

What are the precautions of Codeine Sulfate?

What are the side effects of Codeine Sulfate?

What should I look out for while using Codeine Sulfate?

What might happen if I take too much Codeine Sulfate?

How should I store and handle Codeine Sulfate?

Clinical Information

Chemical Structure

Clinical Pharmacology

Non-Clinical Toxicology

Reference

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

Review

Rate this treatment and share your opinion

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Reason for Taking This Treatment

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