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week 13
week 13
138
Pharmacology
Graduate
05/02/2013

Additional Pharmacology Flashcards

 


 

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Term
Methadone Class / Category
Definition
Narcotic, analgesic, opiate agonist, antitussive, opiod
Term
Methadone MOA
Definition
Methadone is a mu-agonist; a synthetic opioid analgesic with multiple actions qualitatively similar to those of morphine, the most prominent of which involves the central nervous system and organs composed of smooth muscle. Methadone acts as an antagonist at the N-methyl-D-aspartate (NMDA) receptor. The contribution of NMDA receptor antagonism to methadone's efficacy is unknown.
Term
Methadone Uses
Definition
For the treatment of dry cough, drug withdrawal syndrome, opioid type drug dependence, and pain
Term
Methadone Serious ADR
Definition
respirtatory arrest, respiratory acidosis, respiratory depression, prolonged QT interval, edema, Torsades de pointes
Term
Methadone Common ADR
Definition
cardiac dysrrhymia, hypotension, diaphoresis, asthenia, dizziness, lightheadedness, sedation
Term
Methadone Pregnancy
Definition
Catetory C
Term
Methadone Uses
Definition
Methadone is used to treat chronic pain and to prevent symptoms of opioid withdrawal in opioid dependent patients. It is also rarely used as an antiperistaltic agent.
Term
Methadone Monitoring
Definition
Monitor for signs and symptoms of abuse and withdrawal depending upon the patient.
Term
morphine clinical uses
Definition
analgesia for severe pain; acute pulmonary edema: calms, slows respirations, & decreases pre- and after-load; post-MI: analgesic & sedative effects; anesthesia; pre-anesthetic med for sedative & analgesia; via direct application to spinal cord- provide regional analgesic effect while reducing resp. depression, N/V, & sedation from supraspinal actions when administered systemically
Term
morphine
Definition
Gold Standard of opioid analgesics; full opioid agonist with potent mu receptor and some kappa receptor effects
Term
morphine
Definition
exogenous opioid agonist that primarily directly activates the mu receptor, but may also evoke the release of endogenous opioids that additionally act on sigma & kappa receptors
Term
morphine kinetics
Definition
duration= 4-5 hrs; efficacy= high; need higher PO dose due to 1st pass; highly concentrated in brain, lungs, liver, kidney & spleen; conjugated to a compound w/ neuroexcitatory properties & an active metabolite w/ potent analgesic properties; accumulates in renal failure, large doses, & over long periods; excreted by kidneys
Term
morphine MOA
Definition
mu & kappa agonists decrease transmitter release from pre-synaptic terminals of nociceptive primary afferents AND mu agonsits also hyperpolarize second-order pain transmission neurons by opening K+ channels, thus inhibiting post-synaptic neurons
Term
morphine clinical effects
Definition
mu receptor activation leads to analgesia (both sensory & affective); sedation; respiratory inhibition; slowed GI transit; euphoria; modulation of excitatory hormone & neurotransmitter release. Kappa receptor activation leads to analgesia; psychomimetic effects; slowed GI transit.
Term
morphine acute ADR
Definition
N/V; constipation; mental coudiness; euphoria; dysphoria (restlessness & tremor); respiratory center depression; miosis; disrupted sleep patterns; hyperthermia; urinary retention
Term
morphine chronic ADR
Definition
tolerance; cross tolerance across opioid class; physiologic dependence (w/ abstinence syndrome); & hyperalgesia (increased pain sensation)
Term
morphine toxicity
Definition
OD to coma w/ respiratory depression & hypotension to fatal results
Term
morphine abstinence syndrome
Definition
within 6-10 hrs after last dose; peak effects @ 36-48 hrs; induced by d/c opioid or administer antagonist such as naloxone; s/sx= rhinorrhea; lacrimation; yawning; anxiety & hostility; chills & gooseflesh; muscle aches; vomiting or diarrhea; hyperventialation; hyperthermia; mydriasis
Term
morphine DDI
Definition
additive CNS depression when combined w/ EtOH; sedative/hypnotics; anesthetics; antipsychotics; TCAs; or antihistamines. Increased risk coma and HTN when combined w/ MAOI. Avoid combo w/ weak partial agonist such as pentazocine which may decrease analgesic effect or induce withdrawal syndrome
Term
morphine contraindications
Definition
head injuries/ increased intracranial pressure (lethal); pregnancy (withdrawal symptoms in fetus early postpartum); impaired pulmonary function; impaired hepatic or renal function; hypothyroid or adrenal insufficiency (prolonged & exaggerated response to opioids)
Term
loperamide pharmacologic category
Definition
anti-diarrheal, opiod agonist
Term
loperamide MOA
Definition
acts directly on peripheral and intestinal muscles via the opiod receptor to inhibit peristalsis and increase transit time, decreases fluid/electrolyte loss, reduces fecal volume
Term
clinical advantages of of loperamide
Definition
no CNS penetration so no analgesic properties, euphoria, dependence, or addiction potential. No reported tolerance with long term use
Term
loperamide ADR
Definition
constipation, abdominal cramping, nausea
Term
loperamide uses
Definition
acute and chronic diarrhea (not to be used if bloody diarrhea or fever present)
Term
Patients with constipation secondary to loperamide should be treated with what?
Definition
stool softener and stimulant laxative
Term
Fentanyl Subclass
Definition
Strong opioid agonist- (Phenylpiperidine)
Term
Fentanyl MOA
Definition
Strong M-receptor agonist
Term
Fentanyl Effects
Definition
Analgesia, relief of anxiety, sedation, slowed gastrointestinal transit
Term
Fentanyl Clinical Application
Definition
Severe pain, adjunct in anesthesia
Term
Fentanyl Dosing in Elderly
Definition
Elderly twice as sensitive to fentanyl when compared to young patients. Take age, weight, physical status, underlying disease states, other drugs used, and the indication for fentanyl into consideration when choosing a dose
Term
Monitoring parameters for fentanyl
Definition
Effectiveness of pain relief, BP, CNS and respiratory status, Monitor for signs of withdrawal for 24 hrs after transdermal patch is removed. Discontinue slowly after prolonged use. Abuse of medication.
Term
How should fentanyl be disposed of?
Definition
In a secure garbage receptacle so that children/ pets/ other individuals do not have access to the medication, especially the patch. There is still a considerable amount of drug left in the patch after the 72 hr period for which it was used for. Adverse effects will occur by ingestion/ chewing the patch.
Term
Tramadol Class
Definition
Centrally acting opioid analgesic
Term
Tramadol MOA
Definition
Blocks serotonin reuptake and norepinephrine transport function, weak mu-receptor agonist
Term
Tramadol Toxicity
Definition
Seizures, serotonin syndrome especially with the coadministration with SSRIs.
Term
Tramadol Adverse Drug Reactions
Definition
Nausea and dizziness for first few days of administration, seizures, and serotonin syndrome
Term
Tramadol Clinical Uses
Definition
Adjunctive treatment with pure opioid agonist drugs for the treatment of neuropathic pain
Term
Ibuprofen Class
Definition
NSAID
Term
Ibuprofen Generic Names
Definition
Motrin, Advil (OTC), Nuprin (OTC)
Term
Ibuprofen Clinical Uses
Definition
Pain reliever, anti-inflammatory (depending on dosage)
Term
Ibuprofen Adverse Effects
Definition
GI irritant, nephrotoxicity
Term
Ibuprofen MOA
Definition
Non-selective COX inhibitor
Term
Ketorolac Pharmacodynamics
Definition
A nonsteroidal anti-inflammatory drug (NSAID) with the same analgesic, anti-inflammatory, and antipyretic actions as other NSAIDs but is primarily used in the treatment of moderately severe, acute pain (i.e., post-surgical). When given with an opioid, it may decrease the opioid requirement by 25-50%.
Term
Ketorolac MOA:
Definition
Nonselective Cyclooxygenase (COX) inhibitor. Inhibits prostaglandin synthesis.
Term
Ketorolac Toxicities/ADR’s
Definition
Similar to other NSAIDs: gastric irritation (peptic ulcers and GI bleeding), cardiovascular (thrombosis/MI, heart failure, fluid retention/edema), liver dysfunction, renal failure in patients with decreased renal function, and bronchospasm in patients with asthma.
Inhibits platelet aggregation, and can cause hypersensitivity reactions/anaphylaxis.
Term
Ketorolac Pharmacokinetics
Definition
T1/2 is 4-10 hours with 58% of delivered dose excreted unchanged in urine
Term
Ketorolac Special Considerations
Definition
Dose adjustments required for patients less than 50 kg, over 65 years of age, and patients with reduced renal function. Contraindicated with breastfeeding and is Pregnancy Category C.
Not to be used longer than 5 days, NOT indicated for minor or chronic pain.
Term
Dextromethorphan class/category
Definition
Antitussive, Opioid analgesic
Term
Dextromethorphan effects
Definition
Reduces cough reflex
Term
Dextromethorphan MOA
Definition
Poorly understood but strong and partial u agonists are also effective antitussives
Term
Dextromethorphan clinical applications
Definition
Acute debilitating cough
Term
Dextromethorphan Pharmacokinetics
Definition
30-60 minute duration. Toxicity: minimal when taken as directed
Term
Dextromethorphan considerations
Definition
- Use with caution in patients taking monoamine oxidase inhibitors

- Use in childeren less than 6 years of age has been banned by the FDA, due to the increasing reports of death in young children taking this in formulations of over-the-counter "cold/cough" medications.
Term
Dextromethorphan benefit
Definition
Is free of addictive properties and produces less constipation than codeine
Term
Colchicine
Definition
Antigout
Term
Colchicine (MOA)
Definition
Prevents uric acid deposition by interfering with assembly of inflamasome complex , decreases leukocyte motility, and lactic acid production.
Term
Colchicine (ADR)
Definition
Alopecia, rash, diarrhea, vomitting
Term
Colchicine (Contraindications)
Definition
life threatening reaction in hepatic or renal impairment using CP3A4 inhibitors or p-glycoproteins
Term
Ketorolac/Toradol
(MOA)
Definition
NSAID- Nonselective COX Inhibitor: diminshes prostaglandins which decreases inflammation

*Significant Analgesic Action*
Term
Ketorolac/Toradol
(Clinical Uses)
Definition
Uses:
**SIGNIFICANT ANALGESIC ACTION**
-post surgical pain (in place of morphine)
-pain
-Inflammation
-allergic conjuncitivitis
Term
Ketolorac/Toradol
(ADR)
Definition
ADR:
Same as all NSAIDS-
Hematologic- anemia, bleeding
CNS- confusion, drowsiness
CV- HTN, Na/H20 retention
Pulm-bronchospasm
GI-ulcerations
RENAL COMPLICATIONS!

****VERY HARD ON KIDNEYS*****
*Do NOT use for > 5 days
*Do not use in Elderly
Term
dextromethorphan (Clinical Uses)
Definition
cough, antitussive, ex: robitussin
Term
dextromethorphan (MOA)
Definition
opioid derivative; stereoisomer of a methylated derivative of levorphanol
Term
dextromethorphan (ADR)
Definition
mild side effects: Dizziness, Somnolence, Fatigue;Use with caution in patients who are also taking MAOIs, can not be used in patients younger than 6 years old
Term
Allopurinol MOA/Uses
Definition
Reduces total uric acid by inihibiting xanthine oxidase
First line treatment for tx of chronic gout in period between attacks
antiprotozoal agent to prevent massive uricosuira
Term
Allopurinol ADR
Definition
GI intolerance (N/V/D)
peripheral neuritis
necrotizing vasculitis
bone marrow suppresion
hepatic toxicity
Term
Allopurinol nursing considerations
Definition
Colchicine or an NSAID should be given during the first several weeks of therapy to prevent gouty arthritis episodes
Reduce dose with given with chemotherapetuic purine
Term
Tramadol MOA/Uses
Definition
A weak mu angonist with primary MOA on inhibition of serotonin reuptake. Also bloxks norepinephire transport function. Its clinical use is for the treatment of moderate pain and used additionally to pure opoid agonist to treat neuropathy.
Term
Tramadol ADR
Definition
Reduces seizure threshold, therefore contraindicated in those with seizure disorders.
Because it blocks serotonin reuptake, can increase risk for serotonin syndrome should not be used in those taking SSRI's for depression.
Nausea and Vomiting can occur once initally started, but should subside after a few days. It has no effect on respiratory system and is only partially antagonized by naloxone in case of OD.
Term
Febuxostat (MOA)
Definition
A potent and selective xanthine oxidase inhibitor which decreases serum uric acid, without affecting other enzymes in the purine orpyrimidine metabolic pathway.
Term
Febuxostat (Clinical Use)
Definition
Treatment of chronic hyperuricemia in gout patients.
Term
Febuxostat (ADR)
Definition
Liver function abnormalities, rash, diarrhea, headache,and nausea.
Term
Fentanyl (MOA)
Definition
Strong Mu receptor agonist. Follows MOA of all opioids: closing calcium channels, opening potassium channels which all work to stop neurotransmission of a pain signal.
Term
Fentanyl (clinical uses)
Definition
Severe Pain, adjunctive anesthesia, used often in sedation/analgesia protocols for mechanical ventilation
Term
Fentanyl ADR
Definition
Follows similar rules as will all opioids: CNS depression, slowed GI motility, itcing/flushing skin, miosis, hypotension, euphoria and subsequent addition properties
Term
Celecoxib MOA
Definition
COX 2 selective inhibitor resulting in analgesic, antipyretic, and antiinflammatory effects.
Term
Celecoxib ADR
Definition
Renal toxicity, cardiovascular thrombotic events, rashes, can interact with Warfarin; monitor carefully. Has about 1/2 the GI side effects of NSAIDS (much better tolerated)
Term
Celecoxib Rx considerations
Definition
CO-2 selective inhibitors have no effect on platelet aggregation; as such patients that need cardioprotective effects (usually found in a traditional NSAID) may need a low dose aspirin supplemented
Term
Celecoxib dosing
Definition
Recommended 100-200 mg PO BID. Has T1/2 of 11 hours
Term
Ibuprofen
Definition
Analgesic and antipyretic at low doses, anti-inflammatory at doses of ≥2400mg/day, effective in closing patent ductus arteriosus in preterm infants | Inhibits prostaglandin synthesis | ADRs similar to other NSAIDs | Black Box: ↑Cardiac and GI risk
Term
Ketorolac MOA
Definition
has typical NSAID anti-inflammatory properties by inhibiting prostoglandin biosynthesis
Term
Ketorolac Clinical Uses
Definition
not usuallly used as anti-inflammatory medication but as a systemic analgesic mostly after surgical procedures; it successfully reduces morphine doses in many cases, sometimes by 25-50%
Term
Ketorolac Adverse Effects
Definition
renal toxicity is common with chronic use, other ADRs include: rashes, headaches, abdominal discomfort, stomach ulcers (rarely), abnormal liver function
Term
Loperamide MOA
Definition
phenylpiperidine derivative used to control diarrhea. However, due to the action on peripheral u-opiod receptors and lack of effect on CNS receptors it has gotten renewed interest in the treatment of neurpathic pain.
Term
Loperamide Clinical Uses
Definition
anti-diarrheal, neuropathic pain
Term
Loperamide ADR
Definition
mild cramping, but little or no CNS toxicity. constipation.
Term
Colchicine
Definition
Mostly used for Gout and Familiar Mediterranean Fever. MOA = It is an alkaloid extracted from plants in the lily family with action not fully established, the belief is that interfers with the activation of interleukin-1beta in neutrophils & monocytes. There is also inhibition of microtubule assembly in various cells (leukocytes), that binds to and interferes with polymerization of microtubule subunit tubulin. In gout, Colchicine interrupts the monosodium urate crystal deposition in joint tissues to help prevent inflammation in the joints or a gout attack.
Term
Colchicine - Pharm
Definition
Absorption - 45% bioavailbility, no effect on food, Distribution - Protein binding, Albumin 39%, Metabolism - partial Hepatic, Excretion - Renal 40-60%, extensive fecal, not dialyzable.
Term
Colchicine - Adverse Effects
Definition
Diarrhea, Nausea/Vomiting, myelosuppression, colchicine toxicity, neutropenia, acute renal failure, thrombocytopenia, CHF. HMG-CoA inhibitors, Fibrates, Gemfibrozil, and Digoxin can increase adverse effects and monitor pt for myopathy & Rhabdomylosis; CYP3A4 inhibitors can increase colchicine concentrations causing toxicity & should be monitored.
Term
Celecoxib Clinical Uses
Definition
• Ankylosing spondylitis
• Juvenile rheumatoid arthritis
• Osteoarthritis
• Pain, acute
• Primary dysmenorrhea
• Rheumatoid arthritis
Term
Celecoxib MOA
Definition
It’s thought that Celecoxib inhibits the cyclooxygenase-2isoform which suppresses the production of prostaglandin E2 at the inflammation site. Celecoxib is a COX-2 selective inhibitor that has analgesic, antipyretic, and anti-inflammatory effects similar to non-selective NSAIDS but does not have the GI effects and do not effect platelet aggregation.
Term
Celecoxib ADR
Definition
May cause rashes. Associated with a higher incidence of renal toxicity than non-selective NSAIDS, and cardiovascular thrombotic events.
Term
Fentanyl
Definition
Strong opiod agonist; most widely used synthetic opioid
Term
Fentanyl MOA
Definition
Strong mu-receptor agonist with variable affinity for delta and kappa receptors
Term
Fentanyl effects
Definition
Analgesia, decreased anxiety, sedation, decreased GI transit
Term
Fentanyl Clinical Uses
Definition
Severe pain, use with anesthesia
Term
Fentanyl Pharmacokinetics
Definition
First-pass effect; rapid distribution with high concentrations in tissues; excreted by kidneys; short half-life. Available in buccal, transdermal, intravenous forms.
Term
Fentanyl Adverse Effects
Definition
Restlessness, tremors, hyperactivity, respiratory depression, nausea, vomiting, increased ICP, constipation, urinary retention, itching
Term
Fentanyl Special Considerations
Definition
Fentanyl patch may take 6-12 hours for analgesic effects as the drug first has to enter the tissue. The analgesic effect will last 6-12 hours after the patch is removed.
Term
Dextromethorphan MOA
Definition
Poorly understood. It is a dextrorotatory stereoisomer of a methylated derivative of levorphanol. It may be a N-methly-D-aspartate receptor antagonist.
Term
Dextromethorphan Clinical Uses
Definition
At lower doses=Cough suppressant; At higher doses=CNS effects similar to opioids; At higher doses euphoria, dysphoria, hallucinations, or hyperactive behavior can occur; OTC
Term
Dextromethorphan Considerations
Definition
Acute overdose may result in N/V, dizziness, ataxia, drowsiness, lethargy, slurred speech, nystagmus, mydriasis, euphoria, tachycardia, hypertension, urinary retention, stupor, hallucinations, hysteria, hallunciations, hysteria, agitation, or coma. Available OTC. Found to enhance the analgesic action of morphine and other mu receptors. Banned for use in children under 6 years old.
Term
Methadone MOA
Definition
Strong u-receptor agonists, its racmic mixture of D- and L-methadone isomers can also block both NMDA receptors and monoaminergic reuptake transporters
Term
Methadone Effects
Definition
Analgesia-Relieves difficult to treat pain (neuropathic and cancer pain)
Relief of anxiety
Sedation
Slowed GI transit
Term
Methadone Clinical Applications
Definition
Severe Pain
Widely used in the treatment of opioid abuse-detox treatment for morphine and heroin abuse
Term
MethadoneADR
Definition
Respiratory depression
constipation
Prolonged QT-based cardiac arrhythmias-rare
Term
Ibuprofen MOA
Definition
nonselective COX inhibitor that inhibits prostaglandin synthesis, resulting in analgesic and antipyretic effects
Term
Ibuprofen Clinical Uses
Definition
anti-inflammatory, analgesic, antipyretic, primary dysmenorrhea, Rheumatoid arthritis; effective in closing patent ductus arteriosus in preterm infants
Term
Ibuprofen ADR
Definition
headache, tinnitus, dizziness, fluid retention, hypertension, edema, abdominal pain, dysplasia, nausea, vomiting, GI ulcers or bleeding, abnormal LFTs, asthma, rash, renal insufficiency, renal failure, hyperkalemia, proteinuria
Term
Tramadol MOA
Definition
Blocks serotonin reuptake and inhibits norepinephrine transporter function. This helps reduce chronic neuropathic pain.
Term
Tramadol Uses
Definition
Treatment of moderate pain. It is an opioid agonist so it is often used with opioid medication in chronic pain management
Term
Tramadol Pharm.
Definition
Hepatically metabolised. Half-life of 4-6 hours.
Term
Tramadol ADR
Definition
Seizures, it is contraindicated in patients with epilepsy. Risk of serotonin syndrome (especially if taking SSRI antidepressant). Also dizziness and nausea.
Term
Morphine MOA
Definition
opioid, full agonist at the mu-opioid receptor, the major analgesic opioid receptor
Term
Morphine Pharmacodynamics
Definition
CNS-dependence, withdrawal, tolerance, cough suppression, miosis, Nausea & vommiting;GI=>constipation, heart=>peripheral vasodialtion=hypotension;Misc=>flushing diaphoresis, itching
Term
Morphine clinical uses
Definition
analgesia, acute pulmonary edema, cough, diarrhea, shivering, applications in anesthesia
Term
Morphine pharmakokinetics
Definition
PO dose may need to be much higher because of the 1st pass effect to become therapeutic
Term
Morphine A/E
Definition
tolerance, dependence, addiction,
Term
Morphine Contraindications
Definition
use with a weak partial agoist, pts with head injury, use during pregnancy, impaired pulmonary function, imparied liver and kidney function, pts with endocrine diseases such as Addison's and hypothyroidism (myxedema)
Term
KETOROLAC
Definition
NSAID that inhibits cyclooxygenase and thereby prostaglandins. Most often given intravenously or intramuscularly for pain control in post-operative patients. ADR include headache, fluid retention, hypertension, edema, nausea, vomiting, abdominal pain, gastrointestinal ulcers/bleeding, and renal injury (only use for 5 days).
Term
Ibuprofen
Definition
A type of nonsteroidal anti-inflammatory drug (NSAID) that exhibits analgesic and antipyretic activities by inhibiting prostaglandin synthesis.
Term
Ibuprofen contraindications
Definition
In individuals with nasal polyps, angioedema, and bronchospastic reactivity to aspirin.
Term
Adverse effects of ibuprofen
Definition
Aseptic meningitis and fluid retention. Interaction with anticoagulants is uncommon. When given with aspirin, may block the platelet inhibition induced by aspirin. Others (similar of all NSAIDS): headache, hypertension, abdominal pain, rare thrombocytopenia, abnormal LFTs, asthma, rashes, renal insufficiency.
Term
Celecoxib
Definition
selective COX-2 inhibitor, sulfonamide. Selectively bind to and block COX-2 enzyme which in turn inhibits PG synthesis at the site of inflammation with exception to cardiac. Metabolized by CYP2C9.
Term
celecoxib
Definition
ADRs- rash, renal toxicity, interacts with warfarin, some COX2 inhibiotrs have been removed from sale because of cardiovascular thrombotic events, monitor for these sx.
Term
celecoxib
Definition
Anti-inflammatory, antipyretic, analgesic. About half of the GI disturbances of other NSAIDs.
Term
Colchicine
Definition
Class: Uricosuric Agent (is not an analgesic)
Use: Gout, Familial Mediterranean Fever, Behcet’s Syndrome
MOA: Colchicine inhibits microtubule polymerization by binding to tubulin, one of the main constituents of microtubules
Pregnancy Category C
S/E: GI-D/N/V, abd pain. Pharyngolaryngeal pain (2-3%), HA, fatigue
ADR: Cell injury-renal, circulatory, hepatic, CNS. Myelosuppression. Neurological-sensory motor neuropath. Derm-alopecia, pupura, maculopapular rash. Hematological-thrombocytopenia, leukopenia, granulocytopenia, pancytopenia, aplastic anemia. Hepatobiliary- elevated AST/ALT. Musculoskeletal-myotonia, weakness, myopathy, rhabdomyolysis, elevated CPK. Reproductive-azoospermia, oligospermia.
Term
Allopurinol MOA
Definition
Decreases uric acid concentrations in both serum and urine by inhibiting uric acid formation through inhibition of the action of xanthine oxidase. Allopurinol metabolizes to oxypurinol.
Term
Allopurinol Uses
Definition
Primary and secondary gout, cancer (where treatment increases uric acid levels), calcium renal calculus, hyperuricemia from tumor lysis syndrome
Term
Allopurinol Clinical Teaching
Definition
Skin rash, decreased alertness, drowsiness, diarrhea, nausea, liver toxicity (wt. loss anorexia, pruritus), benefit seen in 2 to 6 weeks, maintain hydration if taken for kidney stone
Term
Allopurinol ADR
Definition
Minimal, Only 1% or less of the following: Rash, liver toxicity, kidney failure, agranulocytosis
Term
Tramadol
Definition
A weak centrally acting opiod agonist used for mild to
moderate pain. Also inhibits the update of norepinephrine and serotonin, and
decreases the threshold for seizures. Does not produce the respiratory effects
as seen with opiods. ADR are CNS related and include: drowsiness, dizziness,
HA, fatigue, restlessness. N/V, constipation, dry mouth, and diaphoresis.
Tramadol has a low potential for dependence.
Term
Fentanyl
Definition
Potent synthetic opioid analgesic with a
rapid onset and short duration of action. It is a strong agonist at the
μ-opioid receptors. Fentanyl is approximately 100 times more potent than
morphine.
Term
Fentanyl MOA
Definition
Fentanyl provides some of the effects typical of other
opioids through its agonism of the opioid receptors. Its strong potency in
relation to that of morphine is largely due to its high lipophilicity,( easily
penetration to the CNS). Fentanyl binds μ-opioid G-protein-coupled receptors,
which inhibit pain neurotransmitter release by decreasing intracellular Ca2+
levels.
Term
Fentanyl
ADR
Definition
Fentanyl's major side effects include; diarrhea, nausea, constipation, dry mouth,
somnolence, confusion, asthenia (weakness), and sweating and. Less frequent
side effects are: abdominal pain, headache, fatigue, anorexia and weight loss,
dizziness, nervousness, hallucinations, anxiety, depression, flu-like symptoms,
dyspepsia (indigestion), dyspnea (shortness of breath), hypoventilation, apnea,
and urinary retention. Fentanyl has been assigned to pregnancy category C by
the FDA.
Term
Dextromethorphan
Definition
An opioid derivative used in antitussive preparations. Exact MOA unknown, but does enhance enalgesic effects of opioid agonists. No addictive properties, but abuse of powdered form can lead to serious effects, including death. Use is banned in children under 6 due to reports of death.
Term
Febuxostat
Definition
Non-purine Xanthine oxidase inhibitor used in the treatment of hyperuricemia.
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