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Pharm 2 (AB) > Analgesics > Flashcards

Analgesics Flashcards

1
Q

The analgesic properties of the opiates are primarily mediated by what receptor?

A

Mu receptors

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2
Q

What are the drugs in the class of Opioid Analgesics?

A

Morphine sulfate - MS Contin
Fentanyl - Duragesic
Codeine - T#3, T#4
Tramadol/Ultram

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3
Q

Morphine/MS Contin
Class:
Indication:
MOA:

A

Morphine/MS Contin
Class: Opioid analgesic
Indication: Pain relief
MOA: Opiod agonist (high affinity for mu receptors; raises pain threshold and alters brain’s perception of pain

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4
Q

Morphine additional indications

A

MI: pain relief, decrease anxiety, peripheral vasodilator

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5
Q

Morphine
Char:
SE:

A

Morphine
Char: PO, PR, IM, IV
SE:
(1)respiratory depression (MC cause of death related to morphine use)
(2)Miosis (pin point pupils) due to enhanced parasympathetic stim
(3)Itching: histamine release
(4) N/V
(5) Constipation - decreased GI smooth muscle motility

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6
Q 
Fentanyl/ Duragesic
Class:
Indication:
MOA:
Char:
A

Fentanyl/ Duragesic
Class: Opioid analgesic
Ind: Pain relief, anesthesia
MOA: 80X the analgesic property of morphine
Char: IV, transdermal patch, buccal lozenge, sublingual spray, lollypop. Onset within minutes

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7
Q

Fentanyl/Duragesic

Duration of action

A

Fentanyl/Duragesic
Duration of Action:
Single IM dose duration 1-2 hours
Single IV dose 30 min - 1 hour

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8
Q

Fentanyl/Duragesic

SE

A

Fentanyl/Duragesic
SE:
(1) Respiratory depression: life threatening hypoventilation
(2) Beware of use with CYP 450 inhibitors
(3) N/V
(4) Constipation, paralytic ileus

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9
Q 
Codeine
Class:
Ind:
MOA:
Char:
A

Codeine
Class: Opioid analgesic
Ind: pain relief, antitussive
MOA: Opioid agonist (converted to morphine in the body but gm for gm is weaker than morphine)
Char: PO, IV, IM, SQ (lower abuse potential)

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10
Q

Codeine
Dosing:
DOA:
Pregnancy Cat:

A

Codeine
Dosing: PO (commonly w/syrup)
DOA: 4-6 hours
Pregnancy Cat: C

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11
Q

Codeine:

SE

A

Codeine:
SE: sedation, constipation, itching, potential for exaggerated response in certain individuals

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12
Q

What polymorphism was associated with ultra-rapid metabolism of codeine?

A

CYP2D6

Caused death in children following tonsillectomy and/or adenoidectomy

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13
Q

Tramadol/Ultram
Class:
Ind:
MOA:

A

Tramadol/Ultram
Class: centrally-acting analgesic
Ind: moderate to severe pain
MOA: agonist action at mu-opioid receptor and affects reuptake at noradrenergic and serotonergic systems

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14
Q

Tramadol/Ultram

Char:

A

Tramadol/Ultram
Char: does not have the common SE of respiratory depression in normal doses

May be effective against depression and anxiety

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15
Q

Heroin DEA drug designation

A

Category I : No accepted medical use

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16
Q

Difference between Methadone and Morphine?

A

Methadone: synthetic, orally effective, equal potency to morphine but less euphoria and longer DOA

17
Q 
Naloxone/Narcan
Class:
Ind:
MOA:
Char:
A

Naloxone/Narcan
Class: Opioid antagonist
Ind: opioid overdose (reverse coma and respiratory depression of opioid overdose)
MOA: Opioid antagonist binds with high affinity to opioid receptors but does not activate the receptor mediated response
Char: IV - rapidly displaces all receptor bound opioid molecules with onset of action w/in 30 seconds, half life 60-100 minutes, PO

18
Q

What other drug is Dextromethorphan related to?

A

Dextromethorphan is the dextro-isomer of CODEINE.

19
Q

What happens to an individual who not addicted to an opiate analgesic if they take Naloxone?

A

Nothing

20
Q

What do NSAIDs inhibit synthesis of?

A

Prostaglandins including thromboxanes and prostacyclins

21
Q

What precursor are prostaglandins synthesized from?

A

Arachadonic Acid via the cyclooxygenase pathway?

22
Q

What do prostaglandins do in the body?

A

Promote inflammation, pain and fever

Support clotting function of platelets

Protect the lining of the stomach

23
Q

What enzymes produce prostaglandins?

A

Cox-1 and Cox-2

Cox-1: production related to platelets and protecting the stomach

24
Q

Aspirin
Class:
MOA:
Ind:

A

Aspirin
Class: NSAID
MOA: Irreversible inhibition of COX 1 and 2 enzymes. Diminishes pain and sensitivity to pain by blocking prostaglandin E2 (PGE2)
Ind: Inflammation, pain, fever

25
Q

Aspirin SE

A

GI irritation and PUD
N/V
Increased risk of bleeding
Renal insufficiency

26
Q

Aspirin use is associated with increased risk for what syndrome?

A

Reye’s syndrome

27
Q

What are the signs of salicylsim?

A

Dizziness, tinnitus, hyperventilation, mental status changes and potential for coma/death.

28
Q

What is treatment for salicylism?

A

IV hydration, alkalization of urine and dialysis if renal insufficiency occurs.

29
Q

What is a major difference between Aspirin and Ibuprophen?

A

Ibuprophen is REVERSIBLE while Aspirin IRREVERSIBLY blocks COX-1 and COX-2 enzymes

30
Q 
Celecoxib/Celebrex
IND:
MOA:
Char:
SE:
A

Celecoxib/Celebrex
IND: ADENOMATOUS POLYPS, inflammation, pain
MOA: Reversible selective COX-2 inhibition
Char: Less GI bleeding, no inhibition of platelet agg
SE: possible CVD

31
Q

Acetaminophen/Tylenol
IND:
MOA:
Char:

A

Acetaminophen/Tylenol
IND: Pain, fever
MOA: Peripheral blockade of prostaglandin synthesis in hypothalamus
Char: PO, PR, Metab by liver, no risk of GI bleed, no risk for Reye’s syndrome

32
Q

Acetaminophen/Tylenol

Overdose/SE

A

Overdoes (>7 gm/24 hour) or with alcohol.

Hepatic necrosis leading to liver failure, coma, death

33
Q

What is the maximum safe dose of Acetaminophen in an adult w/o underlying liver disease

Pregnancy category

A

4 grms/24 hours

Pregnancy category: B

34
Q

What toxic metabolite is acetaminophen metabolized to in the liver via P450?

A

N-acetyl-p=benzoquinone-imine (NAPQI)

35
Q

What is NAPQI conjugated with under normal conditions?

A

Glutathione

36
Q

With excess NAPQI what happens?

A

NAPQI binds to vital proteins and the lipid bilayer of hepatocytes resulting in hepatocellular death and liver necrosis.

37
Q

What are the stages of acetaminophen toxicity?

A

Stage 1: 12-24 hrs - N/V

Stage 2: 24-48 hrs- rising AST/ALT and bilirubin

Stage 3: 72-96 hours - peak hepatotoxicity (AST may be > 20,000)

Stage 4: > 96 hrs - recovery, need for liver transplant or death

38
Q

What is the antidote to acetaminophen toxicity?

A

Syrup of ipecac to produce emesis

N-acetylcysteine (NAC) - should be administered as early as possible

39
Q

How is acetylcysteine used?

A 
Mucolytic (mucomyst)
Acetaminophen overdose (Acetadote)

Augments glutathione reserves and binds toxic metabolites to protect hepatocytes from NAPQI toxicity.

Pharm 2 (AB) (8 decks)

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