benzhydrocodone/acetaminophen

Action and Spectrum

Actions and Spectrum 

benzhydrocodone: 

Action: benzhydrocodone is classified as an opioid analgesic, which implies its mechanism of action involves targeting the central nervous system to alleviate pain. It attaches to opioid receptors located in the brain and spinal cord, resulting in a diminished perception of pain. 

Spectrum: benzhydrocodone provides pain relief across a spectrum of conditions, including moderate to severe pain. It is commonly used for acute, postoperative, and chronic pain management when other non-opioid options have been insufficient. 

acetaminophen: 

Action: acetaminophen is classified as a non-opioid analgesic and antipyretic. Although its precise mode of action is not completely elucidated, it is thought to function by inhibiting specific enzymes in the brain responsible for generating prostaglandins. Prostaglandins are compounds that contribute to the sensation of pain and the occurrence of fever. 

Spectrum: acetaminophen demonstrates effectiveness in alleviating mild to moderate pain, including headaches, toothaches, muscle aches, and menstrual cramps. Additionally, it aids in reducing fever. 

Drug Interaction

Adverse Reaction

Frequency defined  

>10% 

Pruritus (11.5%) 

Somnolence (18.5%) 

Nausea (21.5%) 

Constipation (12%) 

Vomiting (13%) 

1-10% 

Headache (6%)  

Dizziness (7.5%)  

1-5% 

Respiratory, thoracic and mediastinal disorders: Dyspnea 

Nervous system disorders: Presyncope, tremor 

Vascular disorders: Hot flush, hypotension 

Gastrointestinal disorder: Abdominal distension, abdominal pain, flatulence 

General disorders and administration site conditions: Asthenia 

<1% 

Psychiatric disorders: Agitation, euphoric mood, nightmare 

Eye disorders: Eye pruritus 

Gastrointestinal disorders: Diarrhea, gastroesophageal reflux disease, hematemesis 

Nervous system disorders: Hypoesthesia, syncope 

Infections and infestations: Rhinitis 

Black Box Warning

Black Box Warning:  

Life-threatening respiratory depression, neonatal opioid withdrawal syndrome, 

Hepatotoxicity  

Contraindication / Caution

Contraindication/Caution:  

Hypersensitivity or allergy: If you have a known hypersensitivity or allergy to benzhydrocodone, acetaminophen, or any other ingredients in the medication, you should avoid using it. 

Respiratory depression: benzhydrocodone is an opioid, and opioids can suppress breathing. If you have severe respiratory insufficiency, chronic obstructive pulmonary disease (COPD), severe bronchial asthma, or any condition that impairs your ability to breathe, the use of benzhydrocodone/acetaminophen may worsen your condition. 

Paralytic ileus: This medication should not be used in individuals with paralytic ileus, a condition characterized by the inability of the intestines to contract and move food and fluids through the digestive system. 

Severe liver impairment: The drug contains acetaminophen, which the liver processes If you have severe liver impairment or active liver disease. 

Alcohol and other CNS depressants: The drug can enhance the sedative effects of alcohol and other central nervous system (CNS) depressants, such as benzodiazepines or certain antidepressants. Combining these substances can increase the risk of respiratory depression, excessive sedation, and other adverse effects.  

Monoamine oxidase inhibitors (MAOIs): MAOIs are a type of antidepressant medication. Concurrent use of this drug with MAOIs or within 14 days of discontinuing MAOIs is contraindicated due to the risk of serotonin syndrome. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: N/A 

Lactation: Excreted into human milk is known 

Pregnancy Categories:         

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

Category B: There were a lack of studies on pregnant women and no evidence of risk to the fetus in animal experiments.   

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.   

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology:  

The combination of benzhydrocodone and acetaminophen in a single formulation provides synergistic analgesic effects. While benzhydrocodone primarily acts as an opioid analgesic, acetaminophen contributes to pain relief through its non-opioid mechanisms. 

Pharmacodynamics:  

benzhydrocodone is a prodrug of hydrocodone, which means it is converted into hydrocodone in the body. It exerts its pharmacological effects by binding to mu-opioid receptors in the central nervous system, resulting in pain relief and a decrease in the perception of pain. The activation of mu-opioid receptors also leads to other effects, such as sedation, respiratory depression, and a sense of euphoria. 

acetaminophen, also known as paracetamol, is a non-opioid analgesic and antipyretic medication. It is believed that the drug operates by impeding the synthesis of prostaglandins within the central nervous system. acetaminophen accomplishes this by inhibiting specific enzymes (COX-1 and COX-2), thereby diminishing the production of prostaglandins. These substances play a role in generating pain signals and regulating body temperature. Consequently, acetaminophen aids in alleviating pain and reducing fever.   

Pharmacokinetics: 

Absorption 

Both these drugs are orally administered drugs, meaning they are typically taken by mouth. After oral ingestion, they are absorbed from the gastrointestinal tract into the bloodstream. The rate and extent of absorption may vary depending on factors such as formulation, dosage form, and individual patient characteristics. 

Distribution 

The medications are distributed across the body by means of the circulatory system. They possess the ability to traverse the blood-brain barrier, enabling them to produce their pain-relieving effects within the central nervous system. 

Metabolism 

The drug undergo different metabolic pathways. 

benzhydrocodone: It undergoes extensive metabolism primarily in the liver. The main metabolic pathway involves enzymatic conversion of benzhydrocodone to hydrocodone, its active metabolite. This conversion is primarily mediated by the cytochrome P450 enzyme CYP3A4. 

acetaminophen: It undergoes hepatic metabolism through several enzymatic pathways. The major pathway involves conjugation with glucuronic acid or sulfate to form inactive metabolites, which are then eliminated in the urine. 

Excretion and elimination 

Elimination of both benzhydrocodone and acetaminophen primarily occurs via the kidneys. 

benzhydrocodone: Following the conversion of hydrocodone through metabolism, the drug and its metabolites are primarily expelled from the body through urine excretion. A minor fraction may also be eliminated via fecal excretion. 

acetaminophen: It is primarily eliminated in the urine as inactive metabolites. A small portion is excreted unchanged, and a minor fraction is eliminated in the feces. 

Adminstartion

Administration:  

Dosage: The dosage of the drug will depend on several factors such as the severity of the pain, your medical condition, and your response to the medication. It is typically available in tablet form, with different strengths of this drug.  

It’s important to swallow the tablets whole and not crush, chew, or dissolve them unless instructed otherwise.  

Timing: Follow the prescribed dosing schedule and avoid taking more than the recommended amount. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: benzhydrocodone/acetaminophen 

Why do we use benzhydrocodone/acetaminophen?  

Pain relief: The drug is prescribed to relieve moderate to severe pain, such as postoperative pain, injuries, dental procedures, or chronic pain conditions. 

Analgesia after surgery: It may be used for pain control after surgical procedures, providing short-term relief during the recovery period. 

Chronic pain management: The drug may be prescribed for chronic pain conditions, such as osteoarthritis, rheumatoid arthritis, or fibromyalgia, where non-opioid analgesics alone are insufficient to manage the pain.