Oripavine

Uses

Drug makers use oripavine to make oxymorphone, the active ingredient in the prescription painkillers Opana, Numorphan, and Numorphone.

With a few extra steps, drug makers covert oripavine into a wide variety of other pain relievers, including oxycodone used in the name brand analgesics, OxyContin, Roxicodone, and others.

Drug makers also covert oripavine into buprenorphine, a drug doctors use to control withdrawal symptoms in drug-dependent patients.

General Drug Information

Drug manufacturers use a chain of chemical processes to extract oripavine from the opium poppy plant, Papaver somniferum, and turn it into safer therapeutic drugs. First, scientists break opium into its major alkaloids metabolites, codeine, morphine, and thebaine. Drug makers can produce codeine and morphine products ready for therapeutic use, or further refine their chemical structure and combine them with other medications to make them more effective or safer.

The metabolite thebaine is toxic and unsuitable for use but drug manufacturers can alter the chemical structure of thebaine to create oxycodone. Scientists can also break thebaine down into even smaller metabolites they can alter to make other medications.

Oripavine is the major metabolite of thebaine. In just a few steps, drug makers covert oripavine directly into oxymorphone. With a few more steps, scientists can covert oripavine back into thebaine, creating new avenues for synthesizing more potent pain relievers.

Oripavine is a strong pain reliever, with analgesia comparable to morphine. However, oripavine is extremely toxic and has relatively low therapeutic value.

Administration/Dosage

Pharmaceutical companies convert oripavine into a wide variety of semi-synthetic drugs that can be administered by mouth, intravenously or through a needle laying close to the spine.

Action

Scientists refer to the metabolites of opium, including oripavine, as opiates. Opiates relieve pain by binding to special opioid pain receptors in the nervous system. Medical professionals refer to any drug that binds to these receptors simply as an “opioid.”

Oripavine and opioids work directly with the central nervous system, or CNS, to change the way the brain perceives pain signals arriving from somewhere in the body. Opioids cause other neurological actions, with the most notable being sedation, relaxation and a euphoric feeling. These pleasant CNS effects make oripavine derivatives a target for recreational drug abusers.

Regular opioid use causes deeper neurological changes that alter how the consumer thinks, feels, and behaves. Left untreated, these alterations can interfere with the individual’s ability to work, take care of children or other responsibilities, and interact with others.

Opioids also work on smooth muscle groups in various locations in the body. Opioids stiffen these muscle groups to make them less effective, causing a variety of unwanted physical effects. For example, opioids cause constipation by acting on the smooth intestinal muscles responsible for propelling stool through the digestive tract. Opioids also affect the smooth muscles lining blood vessel walls in a way that increases blood pressure. The eyes, skin, and other organs contain smooth muscles affected by drugs created from oripavine.

With continuous use, some of the effects of opioids can become more permanent to cause long-lasting neurological and physical effects that can affect the consumer’s life in negative ways. Long-term substance abuse can result in illness, job loss and financial crisis leading to homelessness and crime, incarceration, overdose or death.

Warnings

Without further refinement, oripavine is toxic. In the laboratory, toxic doses of oripavine cause seizures followed by death in both rats and mice.

Oripavine can cause physical dependence resulting in uncomfortable withdrawal symptoms when the consumer stops using this drug. The potential for dependence on oripavine is greater than with thebaine but slightly less than with morphine.

The semi-synthetic drugs created from oripavine are extremely potent.

Precautions

Anyone can suffer an allergic reaction to any medication, including those made from oripavine. An allergic reaction is a serious medical emergency that requires immediate care. Symptoms of an allergic reaction include itching, rash, hives, difficulty breathing, a feeling of tightness in the chest, and swelling of the face, mouth, lips or tongue.

Oripavine products may cause the consumer to feel dizzy, drowsy, or impair his ability to make clear decisions. Other drugs, especially other opioids, or alcohol can enhance these effects. Consumers should avoid driving or operating other heavy machinery while taking oripavine products.

Contraindications

Drugs made from oripavine are not suitable for everyone. People with certain medical disorders should not use oripavine drugs. Drugs made from the oripavine derivative, oxymorphone, are not appropriate for patients with severe liver disease. Patients suffering an asthma attack should not use oxymorphone. This drug is not right for patients who have ever had the serious digestive problem, paralytic ileus.

Patients currently suffering from or have a history of certain illnesses should not use products made from the oxymorphone in oripavine, including respiratory conditions such as asthma, COPD, or sleep apnea. Those with liver or kidney disease, pancreatic disorders, underactive thyroid, significant curvature of the spine, brain tumors, epilepsy or another seizure disorder, or head injury should not use oxymorphone. This drug may not be appropriate for those with enlarge prostate, urinary problems, adrenal gland disorders such as Addison’s, a mental illness or previous problems with drugs or alcohol. Individuals with a history of opioid dependence or other substance abuse problems may not be able to use oripavine products.

Pregnancy, Labor and Delivery, Breastfeeding

The FDA classifies drugs made from oripavine and other opioids as Pregnancy Category C, meaning animal studies show these drugs have an adverse effect but there are no adequate studies to determine the risk in humans. In some cases, the benefits to the mother outweigh the potential risk to the fetus.

Drug Interactions

The oxymorphone derivative of oripavine may interact with other medications in unsafe or unexpected ways. Using oxymorphone with phenothiazines, especially chlorpromazine, can lower blood pressure. Doctors usually prescribe phenothiazines to treat various mental disorders. The popular class of anti-depressant and anti-hypertensive medications, MAO inhibitors, can interact with oxymorphone to cause fever, seizures, and coma.

Oxymorphone can combine with barbiturate anesthetics, the ulcer medication cimetidine, or narcolepsy medication, sodium oxybate, to cause severe drowsiness, coma, confusion, or slowed or difficult breathing. COPD medication and other anti-spasmodic drugs can cause constipation or trouble urinating when taken with oxymorphone. Some pain medications reduce the effectiveness of oxymorphone and increase the risk for withdrawal symptoms.

Side effects

Oxymorphone created from oripavine can cause unpleasant or unwanted side effects. Serious side effects include confusion, fainting, fever, severe or persistent headache, vomiting or unusual swelling. Consumers should seek emergency assistance upon experiencing trouble breathing, a fast, slow or irregular heartbeat, mood chances, hallucinations, or problems urinating after taking products created from oripavine derivatives. Less serious side effects include anxiety, constipation, dizziness or drowsiness, dry mouth, gas, headache, lightheadedness, nausea and vomiting, or perspiring.

Overdose

Prescription painkiller overdose kill nearly 15,000 people every year in the United States; many of these products contain oripavine derivatives, including oxymorphone and oxycodone. The number of overdose deaths is increasing in the U.S.: in 2008, there were three times as many deaths from prescription drug overdose as there had been in 1999.

Emergency room visits for problems involving oxycodone more than doubled in just four years, rising from an estimated 41,700 visits in 2004 to more than 105,000 in 2008.

The use of super-potent oripavine derivatives is at least partially responsible for these deaths and emergency department visites. Oripavine products may be thousands of times stronger than morphine, and are much more toxic than morphine or codeine from the host opium poppy plant.

Suspected victims of overdose should go directly to the nearest emergency room or contact the poison control center at 1-800-222-1222 at the first sign of symptoms.

Symptoms of the overdose may vary subtly between the different oripavine derivative products. Oxymorphone overdose symptoms include:

  • Bluish Skin
  • Chest Pain
  • Cold, Clammy Skin
  • Coma
  • Difficult or Slow Breathing
  • Limp Muscles
  • Numbness of an Arm or Leg
  • Pinpoint Pupils
  • Severe Drowsiness
  • Severe Dizziness
  • Slow or Irregular Heartbeat

Symptoms of oxycodone overdose can include:

  • Change in Consciousness
  • Chest Pain or Discomfort
  • Constricted, Pinpoint or Small Pupils
  • Decreased Awareness or Responsiveness
  • Extreme Drowsiness
  • Loss of Consciousness
  • No Muscle Tone or Movement
  • Severe Sleepiness
  • Slow or Irregular Heartbeat

Abuse

The United States DEA classified oripavine as schedule II narcotic in 2007. This classification means oripavine products pose a relatively high risk for abuse.

Both the oxycodone and the oxymorphone made from oripavine are associated with a high rate of abuse. According to the DEA, oxycodone became “the most frequently encountered pharmaceutical drug by law enforcement” in 2009.

Withdrawal

Anyone who uses oripavine products for therapeutic or recreational reasons regularly for more than a few weeks can become physically dependent on these products. The human body adapts to the presence of even toxic substances, including oripavine products. In time, the body begins to rely on a certain level of these opioids to feel normal - it becomes opioid-dependent. When opioid levels drop drastically, the opioid-dependent body struggles to recover from the toxic effects of oripavine, a process doctors refer to as detoxification. The opioid-dependent person experiences oripavine detoxification through unpleasant physical and psychological withdrawal symptoms.

These withdrawal symptoms tend to appear in two phases, with the first wave beginning a few hours after the last dose of oripavine opioids. Initially, the patient will suffer muscle aches, watery eyes and runny nose, insomnia. He might feel agitated and anxious, and seem to sweat or yawn excessively. Later he might develop stomach cramps, diarrhea, nausea and vomiting, loss of appetite, dilated pupils, and cold, clammy skin.

Withdrawal symptoms last five or more days. The most severe symptoms tend to appear on or about the fourth day. Unless interrupted, symptoms fade as the patient completes the detoxification process and achieves an opioid-free state. The individual may reduce the severity of symptoms with non-opioid drugs, such as Imodium for diarrhea and vitamins for muscle aches. He could stop withdrawal symptoms completely by relapsing to oripavine drug, but this would halt the detoxification process and return him to an opioid-dependent state.

Detoxification

According to statistics cited by the Institute of Addiction Medicine, almost 2 million Americans are dependent on derivatives of oripavine and other opioids. Each of these individuals must undergo some form of detoxification to reach an opioid-free state. Oripavine detoxification can occur at home without professional help, at home with the assistance of an outpatient program, at a hospital, or at a dedicated inpatient detoxification center.

Rapid detox is the safest, most efficient approach to detoxification from oripavine products. During rapid detox, anesthesiologists sedate and anesthetized patients before administering the standard detoxification and anti-withdrawal drugs. Rapid detox patients doze in a comfortable “twilight sleep,” unaware of uncomfortable and demoralizing withdrawal symptoms.

Storage

Storage needs will vary according to the individual oripavine product. Some products need refrigeration while others are stable at room temperature. Most oripavine products should be protected from heat, light, and excess humidity.

Consumers should keep all oripavine products out of the reach of children, and away from adults who may use opioids intentionally or accidently. It is illegal to give oripavine derivatives to another individual, even if both people suffer from similar symptoms.

Facts

  • Oripavine