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42 Cards in this Set

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STRONG ANALGESIC:

- Classification
- Prototype
- Type of pain relieved
- Site of action
- Tolerance / Dependence
Opioids

Morphine

All pains
(esp. chronic dull pain)

Central

Yes/Yes
Strong analgesics:

- mechanism of action?
- anti-inflammatory?
- antipyretic?
Stimulation of opioid receptors

No

No
WEAK ANALGESICS:

- Classification
- Prototype
- Type of pain relieved
- Site of action
- Tolerance / Dependence
NSAID

ASA

Musculoskeletal pain

Peripheral

No / No
Weak analgesics:

- mechanism of action?
- anti-inflammatory?
- antipyretic?
Inhibition of prostaglandin synthesis

Yes

Yes
List the opioids with full agonist activity. x6
Morphine

Hydromorphone

Diacetylmorphine [heroin]

Codeine

Hydrocodone

Oxycodone
MORPHINE:

- absorption
Well absorbed

25% bioavailability after 1st pass
MORPHINE distribution

- plasma bound
- blood brain barrier
33% bound

Small percentage cross BBB to interact with CNS
What happens if morphine administered spinally?
Rapid, profound analgesia

However, can spread rosterally and produce respiratory depression after subsided.
MORPHINE metabolism:

- major mechanism
Glucoronidation
MORPHINE excretion:

- excreted form?
- excreted how / how much?
Glucoronide conjugates

Urine: 90% first day
What does morphine do to the pain?
Elevates reaction
Alters perception of pain

NOT pain threshold
Difference between dextromethorphan and levorphanol.
d-isomer:

- does NOT act via opioid receptors
- no analgesia
- no addiction
- good antitussive

l-isomer:

- analgesic
- addictive
MORPHINE thermoregulation:

- low dosage
- high dosage
mild HYPOthermia

mild HYPERthermia
MORPHINE neuroendocrine effects:

- increases what x2
- decreases what x2
1. ADH (anti-diuretic)
2. Prolactin (disrupts menstrual cycle)

3. Gonadotropin releasing hormone
(decrease testosterone)
4. Corticotropin releasing hormone
(decrease cortisol)
Peripheral effects of Morphine on GI.
Decreases GI effect.
Leads to constipation
Peripheral effects of Morphine on Biliary tract.
Constricts sphincter of Oddi.
Leads to epigastric distress
Peripheral effects of Morphine on smooth muscles. x2
Urinary retention

Prolongs labor
Cardiovascular effects of morphine.
Vasodilation
(decrease peripheral resistance)

Leads to orthostatic hypotension
Immune effects of morphine.
Immunosuppressive
Skin effects of morphine.
Flushing due to vasodilation
Molecular effects of morphine on signal transduction systems.
Inhibits synaptic transmission
What are the therapeutic uses of morphine? x3
Pain management

Diarrhea

Dyspnea (acute pulmonary edema)
T/F - In clinical situations, tolerance and dependence of morphine is a problem.
False.

Thats right bitch. It is false.
Interaction of morphine with what drugs will lead to fatal overdose?
Barbiturates

EtOH

Neuroleptics
(CNS depressants)
Why would you be cautious with patients with the following problems:

- head injury
- decreased respiratory reserve
- reduced blood volume
- asthma
- biliary colic
Morphine increases intracranial pressure

Morphine is a respiratory depressant

Morphine causes hypotensive effects

Morphine suppresses cough reflex and respiration

Morphine constricts sphincter of Oddi, thus producing pancreatic pain.
What are the symptoms of morphine toxicity? x3
Coma

Decreased respiration

Pinpoint pupils
What is the treatment for morphine toxicity?

- procedures x3
- drugs
Establish airway
Ventilate
Detox

Narcotic antagonist (naloxone)
Narcotic substitution (methadone)
Clonidine (suppress withdrawal symptoms)
Hydromorphone:

- potency?
- absorption?
- when do you use?
2-4 times stronger than morphine

Greater bioavailability than morphine

Post-surgery
CA
Which opioid is found in cough syrups?
Hydrocodone

NOT oxycodone
List the phenylpiperidine derivatives. x2
Fentanyl

Meperidine
List the diphenylheptane derivatives. x3
Methadone

LAAM (l-alpha-acetylmethadol)

Propoxyphene
Fentanyl, Sufentanil, Remifentanil:

- potency? why?
- high dosage leads to what?
100-1000 times more potent than morphine.
Highly lipophilic

Muscular rigidity
Which drugs can precipitate withdrawal symptoms in opioid-dependent patients?
Opioid partial agonists

Opioid antagonists
List two opioid antagonists.
Naloxone

Naltrexone
What is naloxone used for? x2
Treatment of opioid OD

Diagnosis of opioid dependence
What is naltrexone used for?
Treatment of opioid addiction
List the opioid receptor types.
Kappa

Delta

Mu
Kappa receptors mediate what?
Dysphoria
Mu and Kappa mediate what?
Respiratory depression
Mu receptors mediate what?
Euphoria
Precursors:

- Beta-endorphins
- enkephalins
- dynorphins
POMC

Proenkephalin

Prodynorphins
What has recently been identified as a mu receptor agonist?
Endomorphins