Major Opiates: Prescription and Illegal

Question 1

what is the most abused opiate?

Answer 1

• nonmedical prescription pills are the most abused opiate and is the leading cause of accidental death in the US (taken over car accidents)

Question 2

Morphine and codeine?

Answer 2

• opium is smoked
• morphine and codeine were isolated from opium and became available in liquid form for oral consumption (available in powder form and pill form)
• they can be snorted or mixed with a liquid and injected
• opiates are an effective cough suppressant - codeine was sold as an OCT cough suppressant – this led to the abuse of cough medicines (now only available with doctor prescription)

Question 3

Heroin

Answer 3

• not a naturally occurring opiate
• synthesized by C.R. Adler Wright in 1874 by adding 2 acetyl groups to the morphine molecule
• more lipid soluble and less ionized than morphine and gains access to the CNS more readily
• it was introduced in the form of Bayer Heroin in 1898 as a nonaddictive analgesic good for coughs and chest pains

Question 4

Fentanyl

Answer 4

• a synthetic opioid that’s 100x more potent than morphine
• its typically used to treat patients with severe pain
• can be administered through a transdermal patch (Duragesic) lollipops for children (Actiq), lozenges or injection (Sublimaze)
• often associated with overdoses by recreational users who are not aware that they have been given it or how much they have been given

Question 5

Derivatives of fentanyl

Answer 5

• more potent than fentanyl and can be added to any street drug
• most of these derivatives are coming from China
• involved in overdose cases

Question 6

Oxycodone

Answer 6

• combined with aspirin = Percodan
• combined with acetaminophen = Percocet in a time-release known as oxytocin
• synthesized from thebaine in opium
• oxytocin users would crush the pills up to destroy the time-release but know manufacturers have made it almost impossible to crush

Question 7

hydrocodone

Answer 7

• combined with acetaminophen = Vicodin or Norco with the difference being the dose of acetaminophen
• lower doses = Norco due to potential liver toxicity
• high abuse levels

Question 8

oxycodone and hydrocodone

Answer 8

• structurally they are very similar - the difference comes down to one extra oxygen atom on Oxycodone
• oxycodone is semi-synthetic and is synthesized from thebaine and will only relieve pain, not cough
• hydrocodone is also semi-synthetic but derived from codeine (more potent than codeine and has cough suppressant effects)
• oxycodone is a stronger pain reliever than hydrocodone and is for managing severe pain whereas hydrocodone is for mild to moderate pain

Question 9

oxymorphone (Opana)

Answer 9

• extended-release formulation - high abuse potential and has been reported to overtake oxycontin as the most abused prescription opiate

Question 10

hydromorphone (Dilaudid)

Answer 10

• morphine derivative

- widely abused

Question 11

Tramadol (Ultran)

Answer 11

• less potent than morphine
• tramadol not only activate opiate receptors but it also increases the brain levels of serotonin and norepinephrine (antidepressant effects)
• pain-relieving effects and also cause side effects and withdrawal symptoms normally not seen with other narcotics
• it also makes it difficult for the usual opiate antagonist to actually work so it makes it harder to treat people who OD on this drug

Question 12

what is the opitae antagonist? (2)

Answer 12

• Naloxone (Narcan): used to reverse opiate ODs (onset in minutes anf effective duration of about 30mins)
• Naltrexone (ReVia or Trexan): given orally and has a longer duration of action