Hydrocodone
Hydrocodone is a synthetic opioid derivative of codeine.14 It is commonly used in combination with acetaminophen to control moderate to severe pain. Historically, hydrocodone has been used as a cough suppressant although this has largely been replaced by dextromethorphan in current cough and cold formulations. Hydrocodone's more potent metabolite, hydromorphone has also found wide use as an analgesic and is frequently used in cases of severe pain.
Mechanism of effect
Hydrocodone binds to the mu opioid receptor (MOR) with the highest affinity followed by the delta opioid receptors (DOR).13 Hydrocodone's agonist effect at the MOR is considered to contribute the most to its analgesic effect
Pharmacodynamic
Hydrocodone inhibits pain signaling in both the spinal cord and brain 12. Its actions in the brain also produce euphoria, respiratory depression, and sedation
Pharmacokinetics
The liquid formulations of hydrocodone have a Tmax of 0.83-1.33 h.
Hydrocodone is 36% bound to plasma proteins
Hydrocodone undergoes oxidative O-demethylation to form hydromorphone, a more potent active metabolite
The half-life of elimination reported for hydrocodone is 7-9 h.
Drug indications
AntitussiveDosage
The following dosing recommendations can only be considered suggested approaches to what is actually a series of clinical decisions over time; each patient should be managed individually.
Drug contraindications
Contraindications. Contraindications to hydrocodone/acetaminophen include patients who have severe respiratory depression, acute or significant bronchial asthma, gastrointestinal obstruction, and anaphylactic reactions due to components of the formula
Side effects
- stomach pain
- dry mouth
- tiredness
- headache
- back pain
- muscle tightening
- difficult, frequent, or painful urination
- ringing in the ears
- difficulty falling asleep or staying asleep
- foot, leg, or ankle swelling
- uncontrollable shaking of a part of the body
Some side effects can be serious. If you experience any of these symptoms or those listed in the IMPORTANT WARNING or SPECIAL PRECAUTIONS sections, call your doctor immediately or get emergency medical treatment:
- chest pain
- agitation, hallucinations (seeing things or hearing voices that do not exist), fever, sweating, confusion, fast heartbeat, shivering, severe muscle stiffness or twitching, loss of coordination, nausea, vomiting, or diarrhea
- nausea, vomiting, loss of appetite, weakness, or dizziness
- inability to get or keep an erection
- irregular menstruation
- decreased sexual desire
- swelling of your eyes, face, lips, tongue, or throat
- hoarseness
- changes in heartbeat
- hives
- itching
- difficulty swallowing or breathing
Interactions
Cefalexin , Succinylcholine , Methocarbamol , Midazolam , Chlorpheniramine , fentanyl , Rifabutin , Rifapentine , Darunavir , Sodium Oxybate , Tapentadol , rasagiline , codeine , ritonavir , Pindolol , Alprazolam , Diazepam , Diphenhydramin , Zolpidem , Cetirizine , Zaleplon , Promazine , Triazolam , Methohexital , Chloral hydrate , Chlorzoxazone , Orphenadrine , Mibefradil , Doxylamine , Molindone , cobicistat , Delavirdine , Letermovir , Alvimopan , Paliperidone , Paraldehyde , Butorphanol , Butabarbital , Acetaminophen and benzhydrocodone , Pimavanserin , Tasimelteon , Ramelteon , Secobarbital , Apalutamide , Tolcapone , Estazolam , Oxymorphone , Ethchlorvynol , Aminoglutethimide (Oral) , nalbuphine , voxelotor , dexmedetomidineAlerts
You should not use hydrocodone if you are allergic to it, or if you have:
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severe asthma or breathing problems; or
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a blockage in your stomach or intestines.
To make sure hydrocodone is safe for you, tell your doctor if you have ever had:
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breathing problems, sleep apnea;
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a head injury, brain tumor, or seizures;
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drug or alcohol addiction, or mental illness;
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urination problems;
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liver or kidney disease;
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problems with your gallbladder, pancreas, or thyroid; or
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a heart rhythm disorder called long QT syndrome.
Pregnancy level
XIf you use opioid medicine while you are pregnant, your baby could become dependent on the drug. This can cause life-threatening withdrawal symptoms in the baby after it is born. Babies born dependent on opioids may need medical treatment for several weeks.
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