Short Acting Opiate Pain Medications

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There are essentially three categories of opiate pain medications.  These categories are based on pharmacological similarities that allow similar medications to be used in similar situations.

 Short acting opiates

These are drugs that get into the body quickly, have an effect quickly and are metabolized quickly.  The quick onset of action makes them ideal for acute pain situations.  However, the quickness of their actions makes them more likely to cause euphoria and therefore, cause addictive behaviors.  Another problem is that they wear off quickly.  This causes the patients to have increased pain shortly before their next dose is due.  In fact, some patients seem to become irritable or have other symptoms as well. This suggests that there may be some withdrawal at the end of each dosing interval.

Many patients attempt to treat their pain chronically with these medicines.  They get into the habit of taking the medication on a time schedule: “it’s bedtime, time for my pill”,  “I’ll take the pill with breakfast and lunch and dinner”  “I’m going to work, its time for my pill”.  Whenever the clock is figuring into a decision to take the pill, trouble is beginning.  The patient is trying to maintain a therapeutic level of medication with scheduled doses.  It is very difficult to do this.  The patients are left with pain (and perhaps withdrawal) waxing and waning all day.  This results in a lot more pain experienced than with other regimens.  In fact, some patients have less pain without any medications than they do on an inefficient pain regimen.  This can only be determined after a detox is performed. 

The following are the more common medications used:

Tramadol- (Ultram, Ultracet) is a  medication that mildly stimulates the opiate pain receptors.  There is a small but definite risk of addictive behavior, especially in persons who have had prior issues with opiates.  The only advantage is it is not legally controlled (I wonder who was paid off in the FDA for this to happen) so that most doctors give it out easily.  It is safe and effective for most people, but probably not for the people who are visiting this site.

Codeine- (Tylenol #3 and #4) also a good cough medication.  It gets metabolized to morphine but levels of morphine never get too high.  This limits effectiveness.  There is a tendency for it to cause a lot of sedation and nausea considering how much pain relief is obtained

Propoxyphene- (Darvon, Darvocet) actually, this is slight longer acting than most of the short acting drugs.  It also tends to be a weaker agent.  It was recently taken off the market secondary to the concern for heart disease.

Hydrocodone-
(Vicodan, Lorcet, Lortab, Vicoprofen, Norco) this is a stronger medication than the first three.  It is great for cough.  There is a tendency for it to cause some sedation and nausea.  It is easy to prescribe and is the most widely abused prescription opiate. 

Oxycodone (Percocet, Roxicodone, Tylox, OxyIR, Endocet) this is a stronger medication than hydrocodone for most, but not all, patients.  It tends to have fewer problems with the stomach.

Morphine (MSIR, Roxanol, Duramorph) this is the original opiate drug, purified from the poppy plant, and the standard by which all other drugs are measured.  It causes nausea and sedation to a greater extent than the others.

Meperidine (Demerol) a synthetic medication, it is used widely in the hospitals because it is injectible and effective. It may be safer to use in patients with certain types of stomach problems.  An active metabolite, normeperidine, can accumulate with chronic use and causes seizures and other problems.

Hydromorphone- (Dilaudid) is a potent and well-tolerated agent. It is probably the most addictive opiate; even heroin users would rather use it than heroin. 

Levorphanol- (Levo-dromoran) slightly longer acting.  It is not widely used outside the hospital setting.   I rarely see patients using or abusing this.

Fentanyl- (Actiq) only recently available, it is the most potent of all opiates.  It is available in a lollipop form.

Oxymorphone- (Numorphan) this is rarely use outside of health settings although it has a suppository form which can be useful.

The following drugs are not pure stimulators of the pain receptors but have more complicated actions.  They are felt to carry less risk of addiction:

Pentazocine (Talwin, Talacen)-is not widely used.  Talwin was reported to be both a partial agonist and a blocker at the mu receptor(see pharmacology article).  It was felt that it would pose less of a risk of addiction.  There was some abuse.  I have no experience with it and it is very infrequently used.  It can precipitate withdrawal in patients who have been using high doses of other opiate medication.

Butorphanol (Stadol)  Like Talwin it is a partial agonist and a blocker at the mu receptor; it can precipitate withdrawal in patients who have been on high doses of other opiates.  It also stimulates kappa opioid receptors which potentially result in some degree of psychological unease.  It was thought this latter effect would reduce its' abuse potential. 

It is available as a nasal spray.  I have seen abuse of this even though it was thought the drug was less likely to be abused. It is still a short acting agent with periods of relative euphoria and than withdrawal.  Its half life is 4 hrs vs Suboxone whose half life is 36 hours.  It may be less addictive than oxycodone or hydrocodone, but it is still not safe.

Nalbuphin- (Nubain) this is used for pain in health care settings but I have rarely seen it prescribed as an outpatient medication.  It is also a partial agonist and a blocker.

Nucynta- This is a new opioid medication.  It stimulates norepinephrine receptors an addition to opiod receptors.  This presumably  allows more pain relief for a given amount of opiod receptor stimulation,  This means the same effect can be achieved with fewer side effects and addiction potential.  

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