Test 1 Flashcards
All drugs in the opiate category act by binding to specific opioid receptors in order to produce effects that mimic the actions of endogenous neurotransmitters, referred to as
the opiopeptins
The opiopeptins include peptides such as
endorphins and enkephalins
The analgesic properties of the opiates are primarily mediated by
mu receptors…mu 1 most commonly for pain
enkephalins interact more selectively with what receptors
delta receptors in the periphery
receptor possibly responsible for hallucinations and dysphoria often associated with opiate use
sigma receptor
class of Morphine/ MS Contin
opioid analgesic
ind. of Morphine/ MS Contin
pain relief
MOA of Morphine/ MS Contin
Potent opioid agonist. High affinity for μreceptors. Morphine relieves pain both by raising the pain threshold at the brain stem, thalamic and spinal cord level as well as by altering the brain’s perception of pain. Patients treated with morphine may still be aware of the presence of pain but perception of the actual sensation of pain is blocked.
Morphine/ MS Contin can also be used for what condition
acute myocardial infarction. It can potentially provide pain relief, decrease anxiety and also acts as a peripheral vasodilator.
side effects of Morphine/ MS Contin
Morphine causes respiratory depression by reducing the sensitivity of respiratory center neurons to carbon dioxide. Respiratory depression is the most common cause of death related to morphine. Miosis (pin point pupils) is due to enhanced parasympathetic stimulation to the occulomotor nerve. Itching is a common side effect due to the fact that the opiate drugs can stimulate histamine release.
Morphine often causes nausea and vomiting due to stimulation of the chemoreceptor trigger (nausea center) in the brain. Constipation due to reduced G.I. smooth muscle motility. PARALYTIC ILEUS is possible. Morphine crosses the placenta, thus potentially creating physical dependence in infants exposed to the drug.
class of Fentanyl/ Duragesic
opioid analgesic
indication of Fentanyl/ Duragesic
pain relief, anesthesia
MOA of Fentanyl/ Duragesic
similar to morphine with 80x the analgesic property of morphine. Used for anesthesia and for intractable pain
Drug often used as a transdermal patch or lollypop form
Fentanyl/ Duragesic
side effects of Fentanyl/ Duragesic
Respiratory depression with life threatening hypoventilation can occur. Patients using concomitant CYP 450 inhibitors may result in fatal blood levels of Fentanyl. Nausea/ vomiting. Constipation is a commonly occurring side effect and paralytic ileus can occur. Highly addictive.
class of Codeine
opioid analgesic
indication of Codeine
pain relief, antitussive
MOA of Codeine
Opioid agonist, is converted to morphine in the body but mg per mg, codeine is much weaker analgesic then morphine.
Can you cut a Fentanyl/Duragesic patch?
No, it will mess up the timed release of the patch.
Should you place a heating pad on a Fentanyl/Duragesic patch?
No, it will increase the dose
side effets of Codeine
Sedation, constipation, itching and increased potential for exaggerated response in certain individuals at risk due to genetic variability . The FDA has issued a Drug Safety Communication after reviewing reports of children who developed serious adverse effects, including death, after receiving codeine in the usual dosage range for pain relief following tonsillectomy and/or adenoidectomy for obstructive sleep apnea syndrome.
Which is better at controlling cough: Codeine, Morphine, or Fentanyl?
Codeine
Respiratory depression, a common side-effect of most opioids, is not clinically significant in normal doses of
Tramadol/ Ultram
Drug used in the controlled withdrawal of heroin and morphine in addicted patients
Methadone…Dependence can develop but the withdrawal syndrome is much milder then with heroin or morphine.
class of Naloxone/ Narcan
opioid antagonist
indication of Naloxone/ Narcan
Opioid overdose. Naloxone/ Narcan is used to reverse the coma and respiratory depression of opioid overdose.
MOA of Naloxone/ Narcan
Opioid antagonists bind with high affinity to opioid receptors but do not activate the receptor mediated response
isomer of codeine.
Dextromethorphan…effective antitussive and is commonly used in OTC cough meds. Generally has little to no analgesic, sedative or GI effects.
Pain relief agents you would not be expected to effect the GI
agents with DM aka dextromethorphan
The nonsteroidal anti-inflammatory drugs (NSAIDs) act by inhibiting the synthesis of
prostaglandins
Prostaglandins, thromboxanes and prostacyclins are all synthesized from the precursor fatty acid, arachadonic acid, via the
cyclooxygenase pathway
COX 1 and 2 inhibitors
aspirin and other salicylates, ibuprofen (motrin, advil), acetaminophen (tylenol)
isolated COX 2 inhibitor
Celecoxib (celebrex)
class of Aspirin/ Acetylsalicylic acid (ASA)
NSAID
indication of Aspirin/ Acetylsalicylic acid (ASA)
inflammation, pain, fever
MOA of Aspirin/ Acetylsalicylic acid (ASA)
Irreversible inhibition of COX-1 and COX-2 enzymes. Anti-inflammatory and analgesic effect largely due to blockade of prostaglandin synthesis at target tissues. Anti-pyretic effect due to blockade of prostaglandin synthesis at thermoregulatory centers in the hypothalamus.
Prostaglandin E2 (PGE2) is thought to sensitize nerve endings to the actions of bradykinins, histamines and other inflammatory mediators. Thus, aspirin serves to diminish pain by decreasing tissue sensitivity to the sensation of pain.
Drug that irreversibly inhibits COX-1 and COX-2 enzymes
Aspirin/ Acetylsalicylic acid (ASA)
side effects of Aspirin/ Acetylsalicylic acid (ASA)
Many potential side effects. Primarily G.I. irritation and peptic ulcer disease, nausea, and vomiting. Increased risk of bleeding. Renal insufficiency. Increased risk of Reye’s syndrome.
Salicylism involves dizziness, tinnitus, hyperventilation, mental status changes and potential for coma and death.
Treatment for salicylism involves I.V. hydration, alkalinization of urine and dialysis if renal insufficiency occurs.
class of Ibuprofen/ Motrin, Advil
NSAID
ind. of Ibuprofen/ Motrin, Advil
inflammation, pain, fever
MOA of Ibuprofen/ Motrin, Advil
Reversible inhibition of COX-1 and COX-2 enzymes. Anti-inflammatory and analgesic effect largely due to blockade of prostaglandin synthesis at target tissues.
class of Celecoxib/ Celebrex
NSAID
ind. of Celecoxib/ Celebrex
inflammation, pain, treatment of adenomatous polyps
MOA of Celecoxib/ Celebrex
reversible, selective COX-2 inhibition
side effects of Celecoxib/ Celebrex
presently unclear if a definite increased risk for cardiovascular disease exists with Celecoxib/ Celebrex
drug with reversible, selective COX-2 inhibition
Celecoxib/ Celebrex
2004, Merck & Co., Inc. announced a voluntary withdrawal of ___ from the U.S. and worldwide market due to safety concerns of an increased risk of cardiovascular events (including heart attack and stroke) in patients on
Rofecoxib/ Vioxx
class of Acetaminophen/ Tylenol
NSAID
indication of Acetaminophen/ Tylenol
pain, fever
MOA of Acetaminophen/ Tylenol
Not fully understood. Weak peripheral blockade of prostaglandin synthesis with stronger blockade of prostaglandin synthesis in hypothalamus
side effects of Acetaminophen/Tylenol
overdose (>7 gm/ 24 hrs) or when acetaminophen is taken with alcohol can lead to severe hepatic necrosis leading to liver failure, coma and death.
Never mix Acetaminophen/Tylenol with
alcohol
maximum safe dose of Acetaminophen/Tylenol in the absence of alcohol use or underlying liver disease
4 grams/24 hours
Acetaminophen is oxidatively metabolized in the liver via the mixed function P450 system to a toxic metabolite
N-acetyl-p-benzoquinone-imine (NAPQI).
antidote for acetaminophen/tylenol
N-acetylcystein (NAC)
Serotonin 1 (5 HT-1) receptors appear to elicit
vascoconstriction
Serotonin 2 (5 HT-2) receptors appear to elicit
vasodilation
class of Propranolol/ Inderal
non-selective beta blocker
indication of Propranolol/ Inderal
HTN, angina, AMI, panic attacks and migraine headaches
what class of meds is best for prodromal phase of headaches
Triptans
whats classes of meds are used for actual headache phase
analgesics, anti-emetics
MOA of Propranolol/ Inderal
blocks adrenergic stimulation which serves to decrease heart rate and myocardial oxygen demand and also decreases renin release
side effects of Propranolol/ Inderal
Bronchoconstriction, hypotension, bradycardia, fatigue, impotence. Abrupt discontinuation may cause rebound hypertension and tachycardia with subsequent increase in myocardial oxygen demand. Abrupt discontinuation increases the risk of arrythmias, stroke, angina and M.I.
class of Amitriptyline/ Elavil
tricyclic antidepressant (TCA)
ind. of Amitriptyline/ Elavil
migraine/tension headache, chronic pain, bipolar disorder and depression
MOA of Amitriptyline/ Elavil
CNS modulation of both serotonin and norepinephrine
side effects of Amitriptyline/ Elavil
Dizziness and marked drowsiness. Anticholinergic effects such as dry mouth, constipation, urinary hesitancy and blurred vision. Do not use with monoamine oxidase (MAO) inhibitors. The full benefits of Amitriptyline may take days to several weeks to be observed whereas side effects are usually noted within first several days.
Topiramate/ Topamax class
anticonvulsant
ind. of Topiramate/ Topamax
anticonvulsant approved for use in treating epilepsy and prophylaxis of migraine headaches. Off-label use for bipolar disorder.
MOA of Topiramate/ Topamax
Block voltage-dependent sodium channels in the CNS, augmenting the activity of the neurotransmitter gamma-amino butyrate (GABA) at some subtypes of the GABA-A receptor. MOA as a migraine medication is not fully known.
side effects of Topiramate/ Topamax
fatigue, dizziness, vision, changes, acute angle glaucoma, nausea, constipation
class of Methysergide/ Sansert
Ergot derivative - serotonin 2 receptor antagonist
ind. of Methysergide/ Sansert
prophylaxis of migraine and cluster headache
MOA of Methysergide/ Sansert
MOA not fully known, yet it appears to be a serotonin 2 receptor antagonist which results in vasoconstrictor effect
caution w/ use of Methysergide/ Sansert
Should never be used beyond ~6 months without a drug free interval. Dosage must be tapered to avoid rebound. Do not use within 24 hrs of a triptan because of increased risk of vasoconstrictive spasm.
Side effects of Methysergide/ Sansert
Multiple potential side effects make methysergide a less attractive choice then newer treatment options. These side effects include but are not limited to hypertension, thrombophlebitis, nausea and vomiting. Pulmonary fibrosis and retroperitoneal fibrosis are severe and potentially life threatening occurrences.
Heart valve thickening has also been reported. Contraindicated in pregnancy (Category X) and in patients with peripheral vascular disease. Because of potential severe side effects.
Methysergide is usually reserved for cases refractive to other medications and treatment modalities.
Life threatening Side effects of Methysergide/ Sansert
Pulmonary fibrosis and retroperitoneal fibrosis are severe and potentially life threatening occurrences.
class of Sumatriptan/ Imitrex
serotonin agonist
ind. of Sumatriptan/ Imitrex
migraine and cluster headache