Dihydrocodeine, Acetaminophen, Caffeine

Drug Class: Dihydrocodeine, Acetaminophen And Caffeine > Dihydrocodeine > Ethers Of Morphine > Semi Synthetic Opioid > Opioids > Opioid Agonist > Analgesic.

Uses

Consumers use combination drugs containing dihydrocodeine bitartrate, acetaminophen and caffeine to relieve moderate to moderately severe pain.

Other, off label uses for this medicine

Ingredients in this drug suppress a nagging cough, bring down body temperature and reduce swelling. This medication may be appropriate for conditions causing not only pain but also cough, fever and inflammation.

General Drug Information

Drug makers combine dihydrocodeine bitartrate, acetaminophen and caffeine in a convenient tablet form. Most preparations contain 32 mg of dihydrocodeine, 712.8 mg of acetaminophen and 60 mg of caffeine. These combination drugs may contain other inactive ingredients.

Dihydrocodeine is an opioid pain reliever, sometimes called a narcotic analgesic. Acetaminophen is a non-narcotic pain reliever. Caffeine is a stimulant that counteracts the sleepiness that narcotics sometimes cause.

Administration/Dosage

Dihydrocodeine bitartrate, acetaminophen and caffeine combination tablets, sometimes called polydrugs, are for oral use. Consumers can take dihydrocodeine bitartrate, acetaminophen and caffeine tablets with or without food; taking this polydrug with food may reduce stomach upset.

The usual adult dosage is one dihydrocodeine bitartrate, acetaminophen and caffeine tablet every four hours as needed to control pain. Physicians will adjust dosage according to the severity of pain and the patient’s response to treatment for that pain. Consumers should not use more than one tablet per dose and should not exceed five doses in any 24-hour period.

Dihydrocodeine bitartrate, acetaminophen and caffeine products are not appropriate for children. Older patients may have a stronger reaction to this polydrug and require smaller doses.

Action

The body absorbs dihydrocodeine bitartrate, acetaminophen and caffeine through the digestive tract. The liver metabolizes dihydrocodeine and acetaminophen, breaking these ingredients down into smaller components easily eliminated from the body through urine.

Dihydrocodeine acts in a variety of ways in the body. Dihydrocodeine relieves pain by depressing the central nervous system, or CNS, to dull the brain’s perception of pain. This opioid also causes CNS effects like sedation, relaxation and a pleasant sense of euphoria.

Opioids suppress the cough reflex in the brain and depress respiratory centers in the brain to cause slow, shallow and irregular breathing patterns. Dihydrocodeine also increases the tone of smooth muscles, like those in the intestines and bladder, to make these muscles stiff and less functional. Dihydrocodeine can also cause vasodilation, widening blood vessels enough to lower blood pressure.

Acetaminophen works to relieve pain differently than dihydrocodeine. Acetaminophen blocks the production of prostaglandins, a substance that sends pain messages to the brain and causes inflammation.

Opioids tend to cause drowsiness significant enough to keep consumers from an active lifestyle. Caffeine blocks the production of adenosine, a chemical that causes sleepiness in the brain.

At the beginning of opioid therapy, doctors say a patient is “opioid-naïve,” or sensitive to the effects of opioids. With continued use at therapeutic doses, the consumer becomes tolerant to the effects of dihydrocodeine. Someone who is opioid-tolerant requires stronger doses of dihydrocodeine more frequently to achieve the same analgesic effects.

Warnings

Respiratory Depression

The slow, shallow and irregular breathing patterns caused by dihydrocodeine may result in respiratory depression, a dangerous and sometimes fatal breathing condition. Respiratory depression prevents the lungs from adequately exchanging spent carbon dioxide for fresh oxygen, causing oxygen starvation and toxic carbon dioxide levels.

Respiratory depression occurs more frequently in elderly or debilitated patients, especially after opioid-naïve consumers take large doses or when the patient takes this combination drug with another medication that depresses breathing.

Patients with the serious breathing problem COPD or the heart condition known as cor pulmonale should exercise caution when using this polydrug, as should consumers with diminished lung capacity, low oxygen levels, high carbon dioxide levels or pre-existing respiratory depression. Physicians should consider a non-opioid analgesic for these patients, or prescribe the lowest possible dose and monitor their conditions closely.

Head Injury and Intracranial Pressure

Respiratory depression associated with dihydrocodeine can cause high carbon dioxide levels and increase the intracranial fluid pressure inside the patient’s skull; head injuries, brain tumors or pre-existing high intracranial pressure can markedly exaggerate these effects.

Dihydrocodeine causes pinpoint pupils and changes in consciousness levels in a way that mimics the signs of a head injury. As a result, opioids can obscure the presence and healing process of head injuries.

Healthcare providers should administer dihydrocodeine polydrugs with care to patients with head injuries or increase intracranial pressure.

Hypotensive Effect

The vasodilation caused by dihydrocodeine reduces blood pressure, causing hypotension in patients who already have trouble maintaining adequate blood pressure either because they have lost a lot of blood or because they have taken a drug that lowers blood pressure. Healthcare providers should administer dihydrocodeine with care to patients in shock, as vasodilation can further reduce blood pressure and worsen the patient’s condition.

Dihydrocodeine may cause orthostatic hypotension, or blood pressure that drops drastically when the person stands up quickly.

Drug Dependence

Anyone who uses dihydrocodeine regularly for more than a few weeks may become opioid-dependent and suffer withdrawal symptoms when he discontinues this medication. Physicians should exercise care when prescribing dihydrocodeine bitartrate, acetaminophen and caffeine products, especially to patients with a history of substance abuse.

Precautions

Dihydrocodeine bitartrate, acetaminophen and caffeine can make the consumer feel dizzy or drowsy, or impair her mental and physical performance. The consumer should not drive a motor vehicle or operate heavy machinery until she knows how this combination drug affects her.

Prescribing physicians should use caution when deciding if an opioid analgesic is right for the patient and adjust dosage according to the patient’s needs and response to treatment. Elderly or debilitated individuals should use dihydrocodeine bitartrate, acetaminophen and caffeine with caution, as should anyone with Addison’s disease, asthma, COPD, acute alcoholism or delirium tremens, sometimes referred to as DTs. Patients with diminished lung capacity due to emphysema, severe obesity, cor pulmonale or curvature of the spine should use this combination product cautiously.

Healthcare providers should exercise caution when administering this product to comatose patients, those suffering pre-existing CNS depression or increased intracranial pressure, and to those with the severe mental disorder, toxic psychosis. Patients with head injury, hypotension and some types of thyroid, prostate and urinary problems should exercise caution when using dihydrocodeine bitartrate, acetaminophen and caffeine preparations.

Dihydrocodeine can obscure the presence or healing process in patients with acute abdominal conditions. Dihydrocodeine can cause or worsen seizures in some circumstances.

Most consumers tolerate acetaminophen well but patients suffering from severe liver or kidney disease should exercise caution when taking this analgesic. Malnourished patients and those with a history of chronic alcohol abuse should exercise care when using acetaminophen as these consumers may be more susceptible to liver damage.

High doses of caffeine may stimulate the central nervous and cardiovascular systems and irritate the gastrointestinal tract.

Contraindications

Dihydrocodeine bitartrate, acetaminophen and caffeine combination drugs may not be appropriate for everyone. Individuals with hypersensitivity to dihydrocodeine, codeine, acetaminophen, caffeine or any inactive ingredients in this combination drug should not use this product.

Dihydrocodeine is not appropriate in any situation where opioids are contraindicated, including in patients suffering from respiratory depression in unmonitored settings or in locations without resuscitative equipment. Patients with asthma, high carbon dioxide levels or the serious type of bowel obstruction known as paralytic ileus should not use dihydrocodeine.

Special Risk Consumers

Medical researchers have not yet established the effectiveness or safety of using dihydrocodeine bitartrate, acetaminophen and caffeine in children. Elderly patients should use this combination drug with caution.

Since the liver metabolizes dihydrocodeine bitartrate, acetaminophen and caffeine, physicians should monitor the condition of consumers who suffer from liver problems. Acetaminophen use may cause hepatotoxicity, which is liver damage associated with drug use.

Physicians should decrease the dosage of dihydrocodeine bitartrate, acetaminophen and caffeine preparations for patients suffering from kidney problems and monitor these patients closely.

Dihydrocodeine acts on the smooth muscles in the biliary tract, which includes the pancreas, gall bladder, liver and the ducts connecting these organs. Dihydrocodeine may cause spasms in the sphincter controlling the flow of pancreatic juices and bile into the small intestine. Patients with biliary tract disease including pancreatitis should use dihydrocodeine products with caution.

Pregnancy, Labor and Delivery, Breastfeeding

The FDA classifies dihydrocodeine bitartrate, acetaminophen and caffeine products as Pregnancy Category C, meaning scientists do not yet know if using this product during pregnancy can harm the unborn baby or if this combination drug affects the reproductive capabilities in males and females. A pregnant woman should use dihydrocodeine bitartrate, acetaminophen and caffeine combination products if the benefits clearly outweigh the possible risks, especially during the first three months of pregnancy.

Using dihydrocodeine bitartrate, acetaminophen and caffeine during and immediately before labor and delivery may cause the newborn to suffer respiratory depression.

Small amounts of dihydrocodeine bitartrate, acetaminophen and caffeine pass into human milk and onto a nursing baby but scientists have not yet established how these drugs affect a nursing infant. Because of the potential harm to nursing babies, mothers should decide between breastfeeding and taking this combination product.

Drug Interactions

Dihydrocodeine bitartrate, acetaminophen and caffeine combination products can interact with other medications in unintended or unsafe ways.

Dihydrocodeine

Dihydrocodeine may interact with other CNS depressants to enhance the way both drugs depress the central nervous system. Examples of CNS depressants include other opioids, sedatives or tranquilizers, muscle relaxants, general anesthetics, anti-vomiting drugs, anti-psychotic medications and alcohol. When a patient needs both dihydrocodeine and another CNS depressant, the physician should reduce the dose of one or both medications.

Many people take monoamine oxidase inhibitors, or MAOIs, to control high blood pressure or depression. Dihydrocodeine can interact with MAOIs to excite the central nervous system and increase blood pressure.

Some medications can interfere with the way dihydrocodeine works, reducing its ability to relieve pain and causing withdrawal symptoms in opioid-dependent consumers. Examples of drugs that do this are pentazocine, nalbuphine, butorphanol and buprenorphine.

Acetaminophen

Chronic and excessive alcohol use can increase the risk for hepatotoxicity associated with acetaminophen. This hepatotoxic risk is also higher for patients taking certain anti-seizure medications or isoniazid, a medication to treat tuberculosis.

Taking large doses of acetaminophen for a long time enhances the way some blood thinners work, increasing the risk for dangerous bleeding problems. Taking acetaminophen along with phenothiazines, used to treat some mental disorders, may cause severely low body temperatures.

Caffeine

Caffeine enhances the way some cardiac drugs strengthen heart muscle contractions to cause a pounding heartbeat. Disulfiram, commonly used to treat chronic alcoholism, can affect the rate at which the body eliminates caffeine. Caffeine can increase the rate at which the body breaks down other drugs, including phenobarbital and aspirin.

Side effects

All drugs, including preparations containing dihydrocodeine bitartrate, acetaminophen and caffeine, can cause adverse reactions in some consumers. Dihydrocodeine, acetaminophen and caffeine produce different, specific side effects.

Dihydrocodeine

The most commonly reported side effects associated with dihydrocodeine are lightheadedness, dizziness, drowsiness, headache and sedation. Consumers have also frequently reported sweating, constipation, itching, skin reactions, nausea and vomiting. Except for constipation, these side effects disappear as the consumer develops tolerance to dihydrocodeine.

Other dihydrocodeine side effects include respiratory depression, orthostatic hypotension, suppression of a necessary cough, confusion, diarrhea and pinpoint pupils. Consumers have experienced abdominal pain, dry mouth, upset stomach, loss of appetite, spasm of the biliary tract and trouble urinating.

Someone can suffer anaphylaxis, which is a serious form of an allergic reaction, or a hypersensitivity reaction to dihydrocodeine. Dihydrocodeine may cause rarely hallucination, vivid dreams, and some serious types of kidney problems.

Acetaminophen

Therapeutic doses of acetaminophen rarely cause side effects for most consumers. The most serious adverse reaction is liver damage associated with acetaminophen overdose. Acetaminophen use may cause low platelet counts leading to bleeding problems or other blood disorders. Rarely, a consumer may suffer a hypersensitivity reaction and experience hives or other skin reactions, swelling of the throat or under the skin and anaphylaxis after taking acetaminophen.

Caffeine

Caffeine may cause the consumer to feel anxious, excited, irritable, lightheaded, restless or tense. Other side effects include headaches, insomnia, shakiness, fast of irregular heartbeat, stomachache, nausea and vomiting, diarrhea, frequent urination, hives, ringing in the ears and visual disturbances.

Overdose

It is possible to overdose on the dihydrocodeine bitartrate, acetaminophen or caffeine components of this polydrug - all of these overdoses pose serious health risks.

Each year, overdose from prescription analgesics like dihydrocodeine claim the lives of nearly 15,000 Americans. Symptoms of dihydrocodeine overdose include respiratory depression, pinpoint pupils and loss of consciousness. The victim may suffer seizures and collapse of the circulatory system; death may occur.

Large doses of the non-prescription pain reliever, acetaminophen, poses a significant health threat as well. Acetaminophen is the leading cause of acute liver failure in the United States. Acetaminophen overdose is one of the most common poisonings worldwide, with about 60,000 cases annually in the United States.

The most serious effect of acetaminophen overdose is potentially fatal liver disease known as hepatic necrosis, or death of liver cells. Laboratory tests and physician examination may not reveal signs of hepatotoxicity for 48 to 72 hours after the toxic dose of acetaminophen. Early symptoms of a hepatotoxic dose include excessive sweating, general malaise, nausea and vomiting.

Acetaminophen overdose can also cause death of kidney cells, coma and clotting disorders that can lead to bleeding problems.

Consuming large amounts of caffeine can cause acute caffeine poisoning, producing symptoms such as restlessness, trouble sleeping, shakiness, delirium, seizures and fast or irregular heartbeat.

Treatment for Overdose

Overdose of dihydrocodeine bitartrate, acetaminophen and caffeine combination drugs requires immediate medical assistance. Emergency department personnel will give a conscious patient ipecac to induce vomiting then introduce activated charcoal into the stomach to absorb excess medication along with a drug to encourage bowel movements. The patient may require stomach pumping; some patients need hemodialysis to remove these drugs.

Nurses start intravenous fluids to counteract hypotension. Physicians may order vitamin K if the patient shows signs of clotting disorders. The patient showing signs of respiratory depression may receive drugs to lower dihydrocodeine levels, but this may cause withdrawal symptoms in opioid-dependent patients; these withdrawal symptoms can complicate overdose treatment.

Healthcare providers will establish an airway or place the patient on mechanical ventilation to help him breathe.

Emergency department physicians will order the antidote to acetaminophen overdose, acetylcysteine, if fewer than 24 hours have elapsed since the victim consumed the toxic dose of acetaminophen. Physicians will monitor liver injury through laboratory tests.

Medical researchers have not developed a specific antidote for caffeine poisoning but aluminum hydroxide soothes the associated stomach irritation while diazepam or barbiturates treat any resulting seizures.

Abuse

Many individuals abuse dihydrocodeine preparations because of the pleasant euphoria opioids produce. The DEA classifies polydrugs containing dihydrocodeine bitartrate, acetaminophen and caffeine as class III drugs, meaning they pose the same relative potential for abuse as Tylenol with codeine or the body building drugs, anabolic steroids.

To reduce this risk, a consumer must have a legal prescription to purchase dihydrocodeine bitartrate, acetaminophen and caffeine products.

Withdrawal

Long-term dihydrocodeine use, whether for recreational or therapeutic purposes, increases the chance the consumer will grow dependent on opioids and suffer withdrawal symptoms when he stops using this product. Withdrawal symptoms begin a few hours after the last dose of dihydrocodeine and continue for five or more days.

Someone going through dihydrocodeine withdrawal feels irritable, restless and anxious; he will suffer insomnia, excessive sweating and irregular heartbeat.

Caffeine can be habit-forming, especially with prolonged use at high doses, and cause withdrawal symptoms when the individual stops using caffeine abruptly. Caffeine withdrawal symptoms include headaches, irritation, anxiety, nervousness and dizziness.

Detox

While tapering works for most opioid-dependent people, severe and prolonged withdrawal symptoms prevent many from quitting dihydrocodeine bitartrate, acetaminophen and caffeine preparations at the appropriate time. Many local healthcare institutions now offer detoxification services to help people overcome these symptoms. Detoxification typically involves drugs to lower dihydrocodeine levels along with medications to relieve withdrawal symptoms.

Many informed consumers now choose rapid detox to overcome withdrawal symptoms. Rapid detox includes sedatives and anesthesia along with the standard detoxification and anti-withdrawal drugs, allowing the patient to doze in a comfortable “twilight sleep” during the detoxification process.

Storage

Consumers and caregivers should store preparations containing dihydrocodeine bitartrate, acetaminophen and caffeine at temperatures ranging from 59 to 86 degrees Fahrenheit. Protect this polydrug from moisture.