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While reducing the pain of rigidity and spasms, opiate analgesics, on rare occasions, may worsen them. Opioids work by binding to opioid receptors, which are found principally in the central and peripheral nervous system and the gastrointestinal tract. The receptors in these organ systems mediate both the beneficial effects and the side effects of opioids. The analgesic (painkiller) effects of opioids are due to decreased perception of pain, decreased reaction to pain, as well as increased pain tolerance. The side effects of opioids include sedation, respiratory depression, constipation, and a strong sense of euphoria.

Opioids can cause cough suppression, which can be both an indication for opioid administration or an unintended side effect. Opioid dependence can develop with ongoing administration, leading to a withdrawal syndrome with abrupt discontinuation.

New laws have been passed in the United States for stricter control of opioids designed to limit the manufacture, distribution, and prescription. Patients must sign a pain management contract. You may be referred to a pain management clinic if the general physician does not want to undertake the oversight of these drugs. The patient must submit to periodic drug testing, sometimes pill counting.

There are restrictions on submitting the scripts to pharmacies, the number of pills you can receive at one time, and the number of refills available before a return visit to the physician prescribing them for you. If you rely on these medications, it is crucial that you keep track of them and the refill schedule. Lost or misplaced drugs will not be replaced. If you do not have a valid prescription in place, you will not receive pills from the pharmacy to tide you over until your next appointment. You can read more about the rules here and see an example of a pain contract here.

1. Codeine

Codeine, or 3-methylmorphine (a naturally occurring methylated morphine), is an opiate used for its analgesic, antitussive, antidiarrheal, antihypertensive, anxiolytic, antidepressant, sedative and hypnotic properties. As with other opiate-based pain killers, chronic use of codeine can cause physical dependence. When physical dependence has developed, withdrawal symptoms may occur if a person suddenly stops the medication. Withdrawal symptoms include: drug craving, runny nose, yawning, sweating, insomnia, weakness, stomach cramps, nausea, vomiting, diarrhea, muscle spasms, chills, irritability, and pain. To minimize withdrawal symptoms, long-term users should gradually reduce their codeine medication under the supervision of a healthcare professional.

2. Demerol, Meperidine, Pethidine

Demerol is indicated for the treatment of moderate to severe pain, and is delivered as a hydrochloride salt in tablets, as a syrup, or by intramuscular, subcutaneous or intravenous injection. It has structural similarities to atropine and other tropane alkaloids and may have some of their effects and side effects. In addition to these opioidergic and anticholinergic effects, it has local anesthetic activity related to its interactions with sodium ion channels.

3. Fentanyl, Actiq, Durogesic, Fentora, Matrifen, Haldid, Onsolis, Instanyl, Abstral, Lazanda

Fentanyl is a potent, synthetic opioid analgesic with a rapid onset and short duration of action. It is a strong agonist at the μ-opioid receptors. Historically it has been used to treat breakthrough pain and is commonly used in pre-procedures as a pain reliever as well as an anesthetic in combination with a benzodiazepine. Fentanyl is approximately 80 to 100 times more potent than morphine and many times more potent than heroin.

4. Hydrocodone, Norco, Vicodin, Lortab, Vicodin

Hydrocodone is a semi-synthetic opioid derived from codeine used orally as a narcotic analgesic and antitussive (cough medicine), often in combination with acetaminophen or ibuprofen. Onset of action is about 10–30 minutes and duration is about 4–6 hours. Hydrocodone relieves pain by binding to opioid receptors in the CNS

5. Morphine (sold under hundreds of brand and generic names in different countries).

Morphine is an opioid analgesic drug and the main psychoactive chemical in opium. In clinical medicine, morphine is regarded as the gold standard of analgesics used to relieve intense pain. Like other opioids, such as oxycodone, hydromorphone, and diacetylmorphine (heroin), morphine acts directly on the central nervous system (CNS) to relieve pain.

Morphine has a high potential for addiction; tolerance and psychological dependence develop rapidly, although physiological dependence may take several months to develop. Tolerance to respiratory depression and euphoria develops more rapidly than tolerance to analgesia, and many chronic pain patients are therefore maintained on a stable dose for years. However, its effects can also reverse fairly rapidly, worsening pain through hyperalgesia.

6. Nucynta, tapentadol, Palexia, TAPAL

It is a centrally acting analgesic with a dual mode of action as an agonist of the μ-opioid receptor and as a norepinephrine reuptake inhibitor. Its analgesic properties come into effect within thirty-two minutes of oral administration. It is similar to tramadol in its dual mechanism of action. Unlike tramadol, it has only weak effects on the reuptake of serotonin, is a significantly more potent opioid and has no known active metabolites. Its general potency is somewhere between that of tramadol and morphine.

7. Oxycodone, Oxecta, OxyCONTIN, Oxyfast, Roxicodone, OxyIR, M-Oxy, Percolone, ETH-Oxydose, Endocodone, Roxicodone Intensol, Dazidox

Oxycodone is a semi-synthetic opioid synthesized from poppy-derived thebaine. It is a narcotic analgesic generally indicated for relief of moderate to severe pain. While the opioids induce acute pain relief, all of them have the potential for dependence, withdrawal, and the induction of pain sensitivity and hyperalgesia, thereby causing the symptom (pain) that they are being used to treat.

8. Propoxyphene, Darvon, Darvon-N/PP-Cap, Darvocet-N, Di-Gesic

Dextropropoxyphene is an analgesic in the opioid category used to treat mild pain, restless leg syndrome, and also has antitussive (cough suppressant) effects.  Its onset of analgesia (pain relief) is said to be 20-30 minutes and peak effects are seen about 1.5-2 hours after oral administration. In pure form, dextropropoxyphene is commonly used to ease the withdrawal symptoms in people addicted to opioids. Being very weak in comparison to commonly abused opioids, dextropropoxyphene can only act as a "partial" substitute. It does not have much effect on mental cravings; however, it can be effective in alleviating physical withdrawal effects, such as muscle cramps.

9. Tramadol, Ultram, Tramol

Tramadol has two different mechanisms. First, it binds to the μ-opioid receptor. Second, it inhibits the reuptake of serotonin and norepinephrine.

It is often combined with acetaminophen as this is known to improve the efficacy of tramadol in relieving pain. Tramadol is an atypical opioid because it is a serotonin-norepinephrine reuptake inhibitor of and, by itself, a fairly weak μ-opioid receptor agonist. Tramadol has inhibitory actions on the 5-HT2C receptor, which could be partially responsible for tramadol's reducing effect on depressive and obsessive-compulsive symptoms in patients with pain and co-morbid neurological illnesses. 5-HT2C blockade may also account for its lowering of the seizure threshold. Tramadol acts as an inhibitor of GABA-α receptors at high doses. When taken as an immediate-release oral formulation, the onset of pain relief usually occurs within about an hour.

Studies have shown that used together, baclofen increases the antinociception (inhibition of pain sensation) properties of Tramadol.

1. Cucuiet S, Dogaru G, Bild VN, Dogaru MT. Modulation of Tramadol antinocioception by Ketamine and Baclofen. Farmacia 2008; Vol LVI, 6, 675. Link to article.

2. Hama A, Sagen J. Combination Drug Therapy for Pain following Chronic Spinal Cord Injury. Pain Res Treat. 2012; 2012: 840486. Link to article.


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