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Pharmacology Ch 18
Terms in this set (94)
What is to be remembered about pain, generally?
Physiological & Psychological Experience, Usually associated with trauma or disease, Multidimensional, subjective experience, Perception of pain differs among individuals, Response to pain differs among cultures, Can be referred to as a protective mechanism
What are two concepts associated with the individual perception of pain?
Pain Tolerance, Pain Threshold
What are the characteristics of pain?
sensory dimension, affective dimension
What describes the sensory dimension of pain?
Location, Intensity, Quality
What describes the affective dimension of pain?
Stimulation of the limbic system produces this emotional response, How the pain influences a person's well-being
What factors influence the perception of pain?
What are the classification of types of pain?
Acute, Chronic, Nociceptor, Neuropathic, Intractable Pain
What is the time element of acute pain?
less than 6 months
Describe chronic pain
pain lasts for more than 6 months and interferes with daily life
What is noireceptor pain?
injury to tissues
What are the types of noirecptor pain?
What is neuropathic pain?
injury to nerves
What processes are involved with pain transmission?
Transduction,Transmission, Perception, Modulation
What stimulates nociceptors?
What kinds of fibers are in the spinal cord that receive pain impulses?
A-Delta Fibers, C Fibers
What spinal cord fibers for receiving pain impulses are myalinated?
What spinal cord fibers for receiving pain impulses are unmyalinated?
How does substance P fit into pain transmission process?
Controls if pain signals reach brain
What is the name for the interruption of pain transmission at the PNS level?
What is the name for the interruption of pain transmission at the CNS level?
What interrupts pain via neurotransmitters?
Serotonin, norepinephrine, GABA
What is important to remember about the pharmacotherapeutics of pain?
Used to correct the underlying cause, Used to decrease the pain response itself, It is preferable and easier to either prevent pain or treat low levels of pain vs. severe pain, Dose and type is individualized by need, Accepted standard plan is a step progression, Use of adjunct medications and nonpharmacological measures should be instituted
Why is it common practice to combine opioid and nonopioid analgesics?
they work synergistically to relieve pain and the dose of narcotic can be kept low to avoid dependence and/or adverse reactions
What are examples of combined nonopioid and opioid analgesics?
Vicodin (hydrocodone and acetaminophen), Percocet (oxycodone HCL and acetaminophen), Tylenol #3 (acetaminophen with codeine)
Where are opioid receptors found?
In the CNS, On nerves in the periphery, On cells in the GI tract
What are the types of opioid receptors?
mu, kappa, delta (affective) and nociceptin
What are the types of opioids?
agonist, antagonist, mixed
What are the prototypes for opioid agonists?
What is the standard measure for morphine or codeine for pain relief?
What is the prototype drug for antagonist opioids?
What is the prototype drug for mixed opioids?
What are the general ideas to remember about opioid agonists?
Drugs that react with the opioid receptors throughout the body, Causes strong analgesia
Effects, other than analgesia, are mediated by the types of opioid receptors affected, Classified as schedule II controlled substances
What does morphine sulfate do on the cellular level?
Reduces the release of presynaptic neurotransmitters, Produces hyperpolarization of postsynaptic neurons
What are the indications for opioid agonists?
Relief of severe acute or chronic pain, Preanesthetic medication, Antitussives, Relieve SOB d/t heart failure, Acute angina connected with MI
What are the contraindications for opioid agonists?
Diarrhea caused by Poisons, Respiratory Dysfunction, Gallbladder disease,
Acute or Severe Asthma, GI Obstruction
Significant Hepatic and Renal Impairment
What are the averse effects for opioid agonists?
Respiratory Depression, Orthostatic Hypotension, Neurological Effects, GU Effects
What are the drug-drug interactions important to opioid agonists?
What drug is used for an overdose of opioid agonist?
What needs to be remember about meperidine?
Synthetic compound, Metabolized to an active metabolite called normeperidine, Similar analgesic, respiratory depression, and physical dependency effects as morphine, Causes fewer constipating and antitussive effects when compared to morphine, Longer half-life
Less potent, generic name for Demerol, opioid agonist
What needs to be remembered about fentanyl
Synthetic compound, much more potent than morphine, Analgesic properties are equal to morphine, Produces fewer respiratory and emetic effects, opioid agonist
What forms does fentanyl come in?
Injection , Transdermal patch , Transmucosal, buccal
What is a trade name for injection injected fentanyl?
What is a trade name for fentanyl given via transdermal patch?
What is significant about Duragesic?
Usually used for persistent moderate-severe chronic pain, Contains several black box warnings, Iontophoretic system (IONSYS)-patient controlled analgesic, is a trade name for transdermal fenatnyl
What are transmucosal and buccal form of fentanyl used for?
breakthrough pain in cancer patients
What are the functions of narcotic agonist-antagonist?
Relief of moderate to severe pain, Adjuncts to general anesthesia, Relief of pain during labor and delivery
What needs to be remembered about narcotic agonist-antagonists generally?
Agonist for the kappa receptors, Weak antagonist at the mu receptors, Same analgesic effect as morphine sulfate, Can cause withdrawal symptoms in those dependent on opioids
What are "T's" and "Blues"?
Common form of abused mixed opioids, Talwin NX was produced to decrease this abuse, Pulmonary disease results from blocking the pulmonary arteries and arterioles
What are the contraindications for narcotic agonist-antagonists?
Chronic Obstructive Pulmonary Disease (COPD), Coronary artery disease (CAD)
What are the averse effects for narcotic agonist-antagonists?
Dizziness, Sedation, Headache, Circulatory depression and tachycardia, Disturbed dreams and hallucinations, Soft tissue nodules, cutaneous depression, ulceration with sloughing and pruritis
What are the drug/drug interactions for narcotic agonist-antagonists
Barbiturate general anesthetics
What are narcotic antagonists?
Drugs that bind strongly to opioid receptors, but do not activate the receptors
What needs to be remembered about narcotic antagonists generally?
Useful in blocking unwanted adverse effects from narcotics, Duration of narcotic agonist may be longer than the action of the antagonist
Used to diagnose cause of overdose, Intense effects are seen in people who are dependent on narcotics
What are the treatments for opioid addiction?
Switch from IV and inhalation forms to oral form
methadone (Dolophine), Does not cure but avoids withdrawal symptoms, Treatment may continue for many months and years
Called Methadone Maintenance, Newer treatment: buprenorphine (Subutex)-Sublingual (SL) route, A combination drug (Suboxone) is used later in the maintenance of opioid addiction
What are the two types of migraines?
Which type of migraine has an aura?
What is the underlying cause for migraine?
What is the prototype drug for Triptans?
What needs to be remembered about Triptans?
Not associated with all of the vascular and GI effects of the ergot derivatives, Bind to selective serotonin receptor sites (5-HT1) to cause vasoconstriction of intracranial vessels, Indicated for the treatment of acute migraine, Available in various forms (PO, SQ, Intranasal)
What are the contraindications for Triptans?
Recent MI, History of Angina Pectoris, History of HTN, Renal or Hepatic Dysfunction
What are the drug/drug interactions for Triptans?
MAO Inhibitor & SSRIs
What is the prototype for ergot derivatives?
How is ergotamine administered?
What is cafergot?
combines ergotamine with caffeine to increase its absorption from the GI tract, oral form
What is dihydroergotamine (Migranal)?
the IM, IV or nasal spray form. Provides rapid relief from migraine
What do ergot derivatives do with regard to systemic averse drug reactions?
Blocks alpha-adrenergic, dopaminergic and serotonin receptor sites in the brain
What are the contraindications for ergot derivatives?
Cardiac Disease, HTN or PVD, Diabetes Mellitus
Impaired Hepatic and Renal Function, Pregnancy (Category X)
What are the averse effects of ergot derivatives?
Central Nervous System, Cardiovascular,
What is the name for a syndrome associated with ergot derivatives?
What are the migraine prophylaxis drugs?
Anticonvulsants, Beta-Adrenergic Antagonists
propranolol is the most commonly used, Calcium Channel Blockers, Tricyclic Antidepressants
onabotulinumtoxin A (Botox)
How does botox prevent migraine?
Inhibits neuromuscular transmission by blocking the release of acetylcholine from specific muscles , Migraines subside up to 3 months
morphine (Astramorph PF, Duramorph, others) therapeutic class
morphine (Astramorph PF, Duramorph, others) pharmo class
Opioid receptor agonist
morphine (Astramorph PF, Duramorph, others) actions
-binds with both mu and kappa receptor sites to produce profound analgesia
-causes euphoria, constriction of pupils, and stimulation of cardiac muscle
morphine (Astramorph PF, Duramorph, others) uses
-symptomatic relief of serious acute and chronic pain after nonnarcotic analgesics have failed
-as preanesthetic medication
-to relieve shortness of breath associated with heart failure and pulmonary edema
-acute chest pain connected with MI
morphine (Astramorph PF, Duramorph, others) adverse effects
-may cause dysphoria (restlessness, depression, and anxiety), hallucinations, nausea, constipation, dizziness, and an itching sensation
-overdose may result in severe respiratory depression and cardiac arrest
morphine (Astramorph PF, Duramorph, others) Black Box Warning
-when administered as an epidural drug, due to the risk of adverse effects, patients must be observed in a fully equipped and staffed environment for at least 24 hours.
-administered as extended-release tablets, it has an abuse liability similar to other opioid analgesics
-alcohol should be avoided
-failure to follow warnings could result in fatal respiratory depression
morphine (Astramorph PF, Duramorph, others) contraindications
-may intensify or mask the pain of gallbladder disease, due to biliary tract spasms
-should be avoided in cases of acute or severe asthma, GI obstruction, and severe hepatic or renal impairment
naloxone (Narcan) therapeutic class
drug for treatment of acute opioid overdose and misuse
naloxone (Narcan) pharmo class
opioid receptor antagonist
naloxone (Narcan) actions
-pure opioid antagonist, blocking both mu and kappa receptors
naloxone (Narcan) uses
-for complete or partial reversal of opioid effects in emergency situations when acute opioid overdose is suspected
-occasionally, given as adjunctive therapy to reverse hypotension caused by septic shock
naloxone (Narcan) adverse effects
-reversal of the effects of opioids may result in rapid loss of analgesia, increased blood pressure, tremors, hyperventilation, nausea and vomiting, and drowsiness
naloxone (Narcan) contraindications
-should not be used for respiratory depression caused by nonopioid medications
aspirin (acetylsalicylic acid, ASA) therapeutic class
-nonsteroidal anti-inflammatory drug (NSAID)
aspirin (acetylsalicylic acid, ASA) pharmo class
-cyclooxygenase (COX) inhibitor
aspirin (acetylsalicylic acid, ASA) actions
-inhibits prostaglandin synthesis involved in the processes of pain and inflammation and produces mild to moderate relief of fever
-limited effects on peripheral blood vessels, causing vasodilation and sweating
-significant anticoagulant activity, and this property is responsible for its ability to reduce the risk of mortality following MI, and to reduce the incidence of strokes
aspirin (acetylsalicylic acid, ASA) adverse effects
-at high doses, may cause gastric discomfort and bleeding because of its antiplatelet effects
-enteric-coated tablets and buffered preparations are available for patients who experience GI side effects.
aspirin (acetylsalicylic acid, ASA) contraindications
-because of increased bleeding time, it should not be given to patients receiving therapy such as warfarin, heparin, and plicamycin
sumatriptan (Imitrex) therapeutic class
sumatriptan (Imitrex) pharmo class
-5-HT (serotonin) receptor drug
-vasoconstrictor of intracranial arteries
sumatriptan (Imitrex) actions
-triptans act by causing vasoconstriction of cranial arteries; this vasoconstriction is moderately selective and does not usually affect overall blood pressure
sumatriptan (Imitrex) adverse effects
-some dizziness, drowsiness, or a warming sensation may be experienced after taking but not severe enough to warrant discontinuation of therapy
sumatriptan (Imitrex) contraindications
-because of its vasoconstricting action, the drug should be used cautiously, if at all, in patients with recent myocardial infarction, or with a history of angina pectoris, hypertension, or diabetes
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