Name the Opioid Drugs that are Stong Analgesics (μ receptors agonists)

(10 of them)

Morphine

Codeine

Fentanyl

Heroin

Hydrocodone

Hydromorphone

Meperidine

Methadone

Oxycodone

Porpoxyphene

Name the Opioid Drugs that are Partial Agonists and mixed agonist/antagonist Analgesics

(4 of them)

Pentazocine

Buprenorhine

Butorphanol

Tramadol

Name the Opioid Drugs that are Opioid Antagonists

(3 of them)

Naloxone

Naltrexone

Methylnaltrexone

What are the two ways in which the body drives breathing?

How is this relavent to Opioid Poisoning?

1. CO2 receptors-when build up of the gas, tells body to breath MORE.

2. O2 Receptors- when build of of O2, tells the body to breath less.

**Opioids knock out the ability of CO2 receptors, that tell the body to breath more.  only have O2 receptors that only tell body to decrease respiration

Systemically administered morphine cause the release of ____________ and may aggrevate asthma and other obstructive pulmonary diseases.

What are possible side effects of Spinal Morphine Administration?

Antihistimine

can also cause irritation of the skin.  Benadryl, and other H-1 Histimine antagonists can alleviate this effect.  

Severe itching of trunk and face.  Treat with Naloxone.

What is the standard Therapeutic Dose of Morphine SC or IM?

1. CNS Depression (stuppor, coma)
2. Depressed Depth and rate of Respiration
3. Pin Point Pupils (although, if very close to death, pupils may in fact be dilated)

Morphine

Route of administration

Dose

Three Important Developments

Subcutaneously, IM or IV (Not as effective orally due to First Pass Metabolism

10mg SC, IM or 10-30mg P.O.

Infusion of autoinjector, Patient Controlled analgesia (pts. usually give less than needed), and Spinal Analgesia

Codeine

1. route of Administration
2. Dose
3. Uses

1. orally effective
2. 30-60mg P.O.  
3. for mild to moderate pain, and Antitussive

Hydromorphone

Roxicodone, Percodan, OxyContin

cross between morphine and codeine

Orally with acetaminophen

moderate to severe pain

OxyContin used for chronic pain (Sustained Release)

Hyrocodone

Lortab, Lorcet, Vicodin, Norco

Similar to Codeine and oxycodone

Used orally with acetaminophen for mild to moderate pain and antitussive

Most Widely Prescribed Opioid

Meperidine

1. Route of Administration
2. Potency as compared to morphine
3. Strength of effects on smooth muscle in comparison to morphine
4. used for... (type of pain)
5. duration of action

Demerol

1. Administered orally and parenterally
2. 1/10 potency of morphine
3. weaker effecs, so less constipation and urin retention
4. moderate to severe pain
5. 1-3 hours **Not appropriate for long term use due to toxic accumulation of Normeperidine Metabolite

Synthetic drug

Heroin

1. Potency compared to Morphine
2. Taken by...

Diactylmorphine

1. More potent, longer duration of action (4-6 hours), more euphoric
2. snorting, injection, smoking

Methadone

1. duration of action in acute care?
2. Duration of action in Chronic care?
3. Used for..

Dolophine

1. 4-6 hours
2. 12-24 hours
3. analgesic and in treatment of opioid addiction (less euphoric than heroine and morphine)

Propoxyphene 

Darvon

Withdrawn from market in 2010

Much less potent than morphine

Serious cardiac toxicity at high doses

Fentanyl 

1. Potency?
2. Administration?

(Sublimaze)

1. Very potent  μ agonist  (100X more potent than morphine
2. Administerd Parenterally to supplement Surgical Anaesthesia
3. Lozenge Preparation available for breakthrough treatment of pain
4.  Neuroleptic Analgesia=Innovar-Combo of fentanyl and droperidol to induce a state where diagnostic and small procedures can be performed without having to put patient under
5. Neuroleptic Anesthesia= innovar +NO

(Sufenta and Alfenta)

Similar to Fentanyl

Used IV as a supplement to Spinal anasthesia

Opioid Combination Preparations

1. what are the common combos?
2. Used for...

1. (codeine, hydrocodone, or oxycodone)+(aspirin, acetaminophen, or ibuprofen)
2. used at very high doses for treatment of severe pain

Pentazocine 

Butorphanol

Pentazocine

• agonist at kappa receptors, partial agonist at mu receptors (At high doses, becomes antagonist for mu receptors)
• Less effective than morphine for pain, and less sedation effects and less resp depression
• More CNS effects and hallucinations
• Less likely physical dependence
• can potentiate withdrawal syndrome
• Pentazocine+naloxone=Talwin Nx

Buprenorphine

(Ultram)

1. Mild-moderate pain
2. weak Mu agonist
3. inhibits synaptic reuptake of NE and Serotonin, like tricyclic antidepressants
4. good analgesia with only common opioid side effects
5. low abuse/addiction potential

Drug of choice for opiod poisoning (can reverse resp depressant effects of opioid)

1. Not effective orally, give Parenterally
2. Sometime in combination with oral narcotic analgesics to prevent abuse
3. SHORT action duration (1-2hrs)
4. can worsen withdrawal symptoms

(ReVia)

Opioid Antagonist

1. orally, lasts 24 hours
2. originally used in "immunizing" addicts (by inhibiting the high
3. Risk of Hepatotoxicity
4. Patient compliance is major problem
5. oppiod addicts must first be detoxified before using this
6. Effective in treatment of alcoholism

(Relistor)

Opioid Antagonist

1. Quaternary Salt-Treat opioid induced Constipation
2. Given Parenterally (Subcutaneous)
3. Treatment of Post-Operative Paralytic Ileus