Advanced Pharmacology Exam 1 Review
PAIN MEDICATIONS AND MANAGEMENT
Types of Pain
- Nociceptive
o Caused by damage to body tissue
o Secondary to noxious stimuli
- Neuropathic/Functional
o Pain that is disengaged from noxious stimuli or healing
o Described in terms of chronic pain
o Result of nerve damage (neuropathic) or abnormal operation of
the nervous system
o Ie postherpetic neuralgia, diabetic neuropathy, fibromyalgia,
irritable bowel syndrome, tension-type headache
Partial Agonist: A drug that can activate an opioid receptor to affect a submaximal
response.
Opioid Antagonist: A drug that blocks some or all opioid receptor subtypes.
Acetaminophen (Tylenol)
- Mechanism of Action: Believed to inhibit the synthesis of prostaglandins
in the CNS / block pain impulse.
- Dose: 325-650mg Q4h or 1000mg Q6h
o MAX: 4 Grams/ Day (If you have Liver impairment of alcoholism
can only have MAX 2 Grams/Day)
- Forms: PR/ PO/ Intravenous
- U.S. Box Warning: Acetaminophen may cause severe hepatoxicity,
potentially requiring liver transplant or resulting in death; hepatoxicity
is associated with excess acetaminophen use.
,Aspirin (Salicylates)
- Mechanism of Action: IRREVERSIBLY binds to COX-1 & COX-2 enzymes
- Properties: Analgesia, Anti-inflammatory, antipyretic,
Antiplatelet (irreversible)
o Prevents the synthesis of thromboxane A (vasoconstrictor &
induces of platelet aggregation)
- Adverse Effects:
o GI discomfort or bleeding
o Dizziness
o Reye’s Syndrome (Occurs in children w/ viral infections)
- AVOID USE WITH RECENT SURGERY
NSAIDs Adverse Effects:
- Cardio = Fluid retention, hypertension, edema
- GI = Irritation, ulcers, bleeding, and perforation
- Respiratory = Bronchospasm
- Skin = Rash, Renal = Insufficiency or Failure
- AVOID with other nephrotoxic drugs (Diuretics like
furosemide, hydrochlorothiazide, ACE inhibitors)
- BLACK BOX Warning
o Potential or serious adverse cardiovascular thrombotic
events including MI & Stroke
o Serious and potential GI bleeding and Ulceration
o Treatment of perioperative pain in the setting of CABG.
Ketorolac (Toradol)
- Available parenterally (IV or IM) and PO
- Indication: Short-term management of moderate to severe pain.
- Adverse Effects:
o Severe bleeding post-operatively
o Renal failure monitor: Bleeding, liver enzymes, serum creatinine
- LIMIT TO MAX 5 DAY THERAPY!
2
, Celecoxib (Celebrix):
- Advantages over nonselective COX inhibitors
o Decreased pain and inflammation with MINIMAL GI side effects
o No effect on platelet aggregation > Improved bleeding profile
- Disadvantages
o Renal dysfunction, “Sulfa Allergies”, Cardiovascular Events
o Vioxx – BAD for heart / COX-2 Selective
- So overall this medication causes LESS GI effects, but MORE likely
Cardiac effects may occur.
Classification of Opioid Agonists (IMPORTANT)
Phenanthrenes Phenylpiperidines Phenylheptanes
Morphine Meperidine Methadone
Hydromorphone Fentanyl
Levorphanol Sufentanil, Alfentanyl,
Oxymorphone Remifentanyl
Codeine
Hydrocodone
Oxycodone
- May Help in cases of a true allergy and PT needs medication switch!
Morphine (NOT FOR RENAL PT):
- Available PO, PR, IV, IM, Sub Q, Epidural, Intrathecal
- Dosing (Acute Pain)
o PO = 15-30mg Q4h PRN / IV = 2-4mg Q4h PRN
- Renally Eliminated
- 2 Active Metabolites
o 6-glucuronide: Active Analgesia
o 3-Glucuronide: Myoclonus, confusion, hallucinations
- Histamine Release (Hypotension, Pruritus) / Special for Morphine
Hydromorphone:
- Available PO, PR, IV, IM, SubQ, Epidural
- Dosing (Acute Pain)
o PO: 2-4mg q4-6h PRN
3
PAIN MEDICATIONS AND MANAGEMENT
Types of Pain
- Nociceptive
o Caused by damage to body tissue
o Secondary to noxious stimuli
- Neuropathic/Functional
o Pain that is disengaged from noxious stimuli or healing
o Described in terms of chronic pain
o Result of nerve damage (neuropathic) or abnormal operation of
the nervous system
o Ie postherpetic neuralgia, diabetic neuropathy, fibromyalgia,
irritable bowel syndrome, tension-type headache
Partial Agonist: A drug that can activate an opioid receptor to affect a submaximal
response.
Opioid Antagonist: A drug that blocks some or all opioid receptor subtypes.
Acetaminophen (Tylenol)
- Mechanism of Action: Believed to inhibit the synthesis of prostaglandins
in the CNS / block pain impulse.
- Dose: 325-650mg Q4h or 1000mg Q6h
o MAX: 4 Grams/ Day (If you have Liver impairment of alcoholism
can only have MAX 2 Grams/Day)
- Forms: PR/ PO/ Intravenous
- U.S. Box Warning: Acetaminophen may cause severe hepatoxicity,
potentially requiring liver transplant or resulting in death; hepatoxicity
is associated with excess acetaminophen use.
,Aspirin (Salicylates)
- Mechanism of Action: IRREVERSIBLY binds to COX-1 & COX-2 enzymes
- Properties: Analgesia, Anti-inflammatory, antipyretic,
Antiplatelet (irreversible)
o Prevents the synthesis of thromboxane A (vasoconstrictor &
induces of platelet aggregation)
- Adverse Effects:
o GI discomfort or bleeding
o Dizziness
o Reye’s Syndrome (Occurs in children w/ viral infections)
- AVOID USE WITH RECENT SURGERY
NSAIDs Adverse Effects:
- Cardio = Fluid retention, hypertension, edema
- GI = Irritation, ulcers, bleeding, and perforation
- Respiratory = Bronchospasm
- Skin = Rash, Renal = Insufficiency or Failure
- AVOID with other nephrotoxic drugs (Diuretics like
furosemide, hydrochlorothiazide, ACE inhibitors)
- BLACK BOX Warning
o Potential or serious adverse cardiovascular thrombotic
events including MI & Stroke
o Serious and potential GI bleeding and Ulceration
o Treatment of perioperative pain in the setting of CABG.
Ketorolac (Toradol)
- Available parenterally (IV or IM) and PO
- Indication: Short-term management of moderate to severe pain.
- Adverse Effects:
o Severe bleeding post-operatively
o Renal failure monitor: Bleeding, liver enzymes, serum creatinine
- LIMIT TO MAX 5 DAY THERAPY!
2
, Celecoxib (Celebrix):
- Advantages over nonselective COX inhibitors
o Decreased pain and inflammation with MINIMAL GI side effects
o No effect on platelet aggregation > Improved bleeding profile
- Disadvantages
o Renal dysfunction, “Sulfa Allergies”, Cardiovascular Events
o Vioxx – BAD for heart / COX-2 Selective
- So overall this medication causes LESS GI effects, but MORE likely
Cardiac effects may occur.
Classification of Opioid Agonists (IMPORTANT)
Phenanthrenes Phenylpiperidines Phenylheptanes
Morphine Meperidine Methadone
Hydromorphone Fentanyl
Levorphanol Sufentanil, Alfentanyl,
Oxymorphone Remifentanyl
Codeine
Hydrocodone
Oxycodone
- May Help in cases of a true allergy and PT needs medication switch!
Morphine (NOT FOR RENAL PT):
- Available PO, PR, IV, IM, Sub Q, Epidural, Intrathecal
- Dosing (Acute Pain)
o PO = 15-30mg Q4h PRN / IV = 2-4mg Q4h PRN
- Renally Eliminated
- 2 Active Metabolites
o 6-glucuronide: Active Analgesia
o 3-Glucuronide: Myoclonus, confusion, hallucinations
- Histamine Release (Hypotension, Pruritus) / Special for Morphine
Hydromorphone:
- Available PO, PR, IV, IM, SubQ, Epidural
- Dosing (Acute Pain)
o PO: 2-4mg q4-6h PRN
3
