Clinical problems associated with the opiates

• Respiratory depression: not really, you’d have to use massive oral doses to get this
• Sedation
• Interactions with CNS depressant drugs: act as synergists
• Constipation: very real with codeine, any dose lasting 2-4 days will have a change in bowel habits
• Nausea, vomiting: rare
• Endocrine disturbances
• Tolerance to analgesic effect
• Physical dependence
• Abuse potential

Addiction is a primary, chronic, neurobiologic disease, with genetic, psychosocial, and environmental factors influencing its development and manifestations. It is characterized by behaviors that include one or more of the following: impaired control over drug use, compulsive use, continued use despite harm, and craving.

Physical dependence is a state of adaptation that is manifested by a drug class specific withdrawal syndrome that can be produced by abrupt cessation, rapid dose reduction, decreasing blood level of the drug, and/or administration of an antagonists.

The 5 C’s which define addiction: Chronic, impaired Control over drug use, Compulsive use, Continued use despite harm, Craving

Tolerance is a state of adaptation in which exposure to a drug induces changes that result in a diminution of one or more of the drug’s effects over time. You must escalate the drug in order to get the same therapeutic effect.

Opiate Antagonists include Naloxone (Narcan), which must be given by injection. It binds to opiate receptors and can reverse opiate side effects. This can be an antidote to opiate overdose. Naltrexone (Revia) is given once a day orally, and blocks physical dependence to morphine, heroin and other opiates. However, there is severe liver damage with prolonged use.


Tramadol (Ultram) is a central acting analgesic, its not an opiate or an NSAID. It is indicated for moderate to severe pain. For adults only. Interacts with MAO inhibitors. It was the #1 used drug in Europe for a while and since its not an opiate, you don’t need a DEA narcotic prescribing license number.


We can see that when a pt is given Tramadol for pain in combination with Flurbiprofen, there is very good analgesia.


You need to know the components of Tylenol I, II, III, Percocet, Darvocet, Vicodin, Vicoprofen, Ultracet. Ultracet is brand new, and combines tramadol (centrally acting, non-opioid) with acetaminophen (peripherally acting). So you’ve got a lot of choices regarding pain management.


Percocet exists with varying oxycodone concentrations (7.5mg and 10 mg). You can see by the “C” with “II” in it that Percocet is a controlled substance II, which means that you need a triplicate prescription form. Oxycodone has a greater addiction liability, so that’s why Percocet is classified as a schedule II drug.

Usually the contraindications have to do with hypersensitivity to the components. YOU MUST NOT GIVE DEMEROL IF THE PT IS TAKING MAO INHIBITORS, YOU WILL KILL THE PATIENT. It is a lethal drug interaction.


It will be a very rare condition when you will want to prescribe hydrocodone alone. It requires a triplicate prescription form, and no refills are allowed. Hydrocodone alone is an addictive substance, it can produce very rapid tolerance and dependence. If you see hydrocodone in a fixed combination with another drug like acetaminophen, the dose is low enough that it usually means it will be a schedule III. If you look at schedule III drugs, you are allowed refills but the pt must be reevaluated every six months. That’s important for a physician treating chronic pain with opiates, for our case we’re always dealing with short-term pain of about five days.

Category: Pharmacology Notes