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Pharmacology > Opiod Analgesics (The Patient Satisfaction Score Drugs) > Flashcards

Opiod Analgesics (The Patient Satisfaction Score Drugs) Flashcards

1
Q

High efficiency Agonists

A 
Morphine
Hydromorphone
Oxymorphone
Methadone
Fentanyl
Meperidine
Heroin
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2
Q

Low-medium agonists

A

Codeine, oxycodone

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3
Q

Mixed agonist / antagonists and others

A

Buprenorphine, Tramadol

Pentazocine

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4
Q

Non - analgesic opiods

A

Dextromethorphan

Loperamide

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5
Q

Mu opiod receptors

A

Major receptor for drugs - analgesia, respiratory depression, euphoria, addiction

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6
Q

Kappa opiod receptors

A

Analgesia, sedation, dysphoria

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7
Q

DM receptor

A

Antitussive effects

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8
Q

Opiod analgesia

A

Increased threshold and tolerance, pain over perception. Better results for slow and nociceptive, rather than neuropathic pain.

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9
Q

Mechanism of opiod constipation

A

Mu opiod receptors on enteric nerves - decrease in propulsion, peristalsis, and secretion.

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10
Q

Common adverse effects

A

Constipation, nausea, vomiting, sedation, miosis, pruitis.

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11
Q

Triad of overdose

A

Coma

Respiratory Depression

Pinpoint pupils

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12
Q

If you have a high tolerance, should you get more opioids to get the same anesthetic effect?

A

NO! Therapeutic index is unchanged.

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13
Q

Contraindications

A 
Head Injury
pregnancy
Impaired pulmonary, hepatic, renal function
Hypothyroid
Substance abuse history
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14
Q

Drug Interactions

A

MAOI’s - life threatening serotonin syndrome

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15
Q

Hydromorphone (“That drug that starts with ‘D’”)

A

More potent than morphine. Less histamine release - less pruitis, less hypotension/ bronchoconstriction. Better in renal disease because its metabolite is renally excreted.

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16
Q

Oxymorphone

A

More potent than morphine. Less histamine release - less pruitis, less hypotension/ bronchoconstriction. Better in renal disease because its metabolite is renally excreted.

17
Q

Fentanyl

A

More lipophilic than morphine - 75-100x more potent. Admin via lollipop, lozenge, tablet, nasal spray. Short acting. Used in IV anasthesia

18
Q

Methadone

A

Used to treat heroin addiction. Well absorbed PO. Long T 1/2.

LONG QT - Arrythmias

19
Q

Meperidine (Demerol)

A

Less potent, short t 1/2. Metabolism is demethylation via CYP3A4 to toxic NORMEPERIDINE. This can lead to fatal neurotoxicity. Avoid in renal impairment / MAOI use.

20
Q

Heroin

A

No therapeutic use, but has led to some good music.

21
Q

Low-Medium efficiency opiod antagonists problems.

A

Combined with asprin or acetominophen - risk of liver toxicity. Often abused

22
Q

Codeine

A

Prodrug - converted to morphine via demethylation via CYP2D6. metabolism is polymorphic - different effects on different patients. Also a good antitussive.

23
Q

Oxycodone (percocet)

A

Highest efficiency - metabolized to oxymorphone by CYP2D6. Slow release version - oxycontin - crush it up to disable slow release and have a good time

24
Q

Hydrocodone

A

Metabolized to hydromorphone via CYP2D6. Good antitussive. Less pruritis than codeine. Very popular

25
Q

Mixed agonist-antagonist mechanism (general)

A

Agonists at kappa receptors - analgesic, dysphoria, hallucinations.

Antagonist at mu receptors - less respiratory depression, less euphoria

26
Q

Pentazocine

A

mixed agonist-antagonist - not recommended parentral due to necrosis and sepsis.

27
Q

Buprenorphine

A

mixed agonist-antagonist - sublingual due to 1st pass. Used to treat opiod dependence by antagonizing mu receptors.

28
Q

Tramadol

A

Mixed opiod and NE reuptake inhibitor.

29
Q

Tramadol risks

A

Seizures, avoid with MAOI’s - serotonin syndrome

30
Q

Antitussive opiod

A

Dextromethorphan - active at DM receptor only.

31
Q

Antidiarrheals

A

Loperamide

32
Q

Loperamide

A

Immodium - reduces diarrhea by antagonizing gastric plexus. little BBB penetration.

33
Q

Opiod Antagonist

A

Naxolone - Narcan - Competitive antagonist at ALL opiod receptors - used in overdose.

Pharmacology (11 decks)

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