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Topical anesthesia - ANSWER The ability of an anesthetic to penetrate the axon membrane is determined by
- Molecular size
- Lipid solubility
- Degree of ionization at tissue ph
Lidocaine - ANSWER Injectable, gels Lido with epi to constrict blood flow and prolongs anesthesia and decrease risk of toxicity
Mu receptors - ANSWER Responses to activation of these receptors include: analgesia, respiratory depression, euphoria, sedation, and physical dependence Most important receptors for opioids because they act primarily by activating mu receptors
Kappa receptors - ANSWER Activation of these receptors can produce: analgesia and sedation Kappa activation my underly psychotomimetic effects seen with certain opioids
Delta receptors - ANSWER Generally opioids don't interact with these
Pure opioid agonists - ANSWER Activate mu and kappa receptors can produce analgesia, euphoria, sedation, respiratory depression, physical dependence, constipation, and other effects
Morphine - ANSWER Strong opioid agonist
Codeine - ANSWER Moderate to string opioid agonist
Agonist antagonist opioid - ANSWER Pentazocine, nalbuphine, butorphanol, buprenorphine When administered alone produces analgesia If admined with pure opioid agonist, can antagonize analgesia caused by the pure agonist
Pure opioid antagonists - ANSWER Naloxone (Narcan) our prototype Antagonist at mu and kappa receptors Do not produce analgesia or any of the other effects caused by opioid agonists Reversal of respiratory and cns depression caused by overdose with opioid agonist Not available in oral forms
Methyl naltrexone - ANSWER Used to treat opioid induced constipation Only work on mu receptors in the bowel
Naltrexone - ANSWER Used to treat opioid and alcohol abuse Prevents euphoria if the abuser takes opioid Doesn't prevent craving for opioid Candidates for treatment must be rendered opioid free before naltrexone is started
Morphine - ANSWER Source: poppy seed plant Therapeutic use: relief of pain Relieves pain without affecting other senses (like sight, touch, smell, and hearing) No loss of consciousness MOA: relieves pain by mimicking actions of endogenous opioid peptides, primarily at mu
Much weaker when compared to morphine for severe pain Can cause withdrawal in pts dependent on a pure opioid When given with pure agonist will decrease effectiveness of pure agonist
Tramadol (Ultram) - ANSWER MOA combo of opioid and non opioid mechanisms Used for moderate to severe pain Adverse effects and interactions are sedation, dizziness, headache, constipation, seizures Drug interactions are other cns depressants Abuse potential Immediate release and extended release available
COX-1 - ANSWER Present in nearly all tissues. It has protective effects on the gastric mucosa, maintains renal function, and enhances platelet aggregation
COX-2 - ANSWER Produced mainly at sites of injury where is mediates inflammation and sensitizes receptors to painful stimuli. Also present in the brain where it mediates fever and contributes to perception of pain. Present in the kidney to support renal function. Present in blood vessels to promote vasodilation, and colon where it can cause colon cancer.
Inhibition of COX-1 - ANSWER Benefits : protection against MI and stroke Adverse effects: gastric ulceration, bleeding, renal impairment
Inhibition of Cox 2 - ANSWER Benefits: suppression of inflammation, alleviation of pain, reduction of fever, protection against colorectal cancer Adverse effects: gastric ulceration, bleeding, renal impairment, increase risk of mi and stroke
First generation anti inflammatories - ANSWER Inhibit cox 1 and Cox 2
Anti inflammatory: asa and nsaids Non anti inflammatory: acetaminophen
First generation nsaids - ANSWER Inhibit COX-1 and COX- Used to treat inflammatory disorders (rheumatoid arthritis, osteoarthritis, bursitis) Alleviate mild to moderate pain Suppress fever Relieve dysmenorrhea Suppress inflammation but pose risk of serious harm ( gastric ulceration, bleeding, renal impairment) Decrease risk for heart disease
2nd generation cox inhibitors - ANSWER Only inhibit Cox 2, so suppress inflammation and causing fewer adverse effects In reality they appear less safe that the first generation Increase risk for mi and stroke Celecoxib is only one left on the market
Celebrex - ANSWER As effective as traditional nsaid, lower gi risk, can impair renal function, can cause hypertension and edema, increased risk for mi and stroke Last choice drug due to cardiovascular risk Uses: osteoarthritis, RA, acute pain, dysmenorrhea, familial adenomatous, polyposis
Celebrex side effects - ANSWER -Most common side effects are dyspepsia and abdominal pain
-Increases risk of MI events due to vasoconstriction
-Renal impairment
Non-Aspirin First Generation NSAIDs - ANSWER these are aspirin like drugs but have fewer GI, renal and hemorrhagic effects
they inhibit COX 1 and 2, but inhibition is reversible
- do NOT protect against MI and stroke
ex. (Ibuprofen and naproxen, ketorolac)
Advil - ANSWER Indications are fever, pain and arthritis Generally well tolerated Low incidence of adverse effects Gi bleed possible
Acetaminophen - ANSWER Use: analgesia, antipyretic Not anti inflammatory or anti rheumatic Moa inhibits prostaglandin synthesis in cns Few ae Drug interactions: alcohol, warfarin by risk of bleeding, and can blunt immune response after vaccines
Stevens-Johnson Syndrome - ANSWER Acute generalized exanthematous pustulosis and toxic epidermal necrolysis Hepatotoxic-> s/sx n and v, d, sweats, abdominal pain Treatment of overdose with aceytlcysteine aka mucomyst Worst case is liver failure coma and death
Glucocorticoids- ANSWER Stop inflammatory process through many mechanisms
Uses: RA, SLE, IBD, ASTHMA, allergic conditions, derm disorders, misc inflammatory disorders Have metabolic effects long list Want to avoid adrenal suppression Happens bc pituitary loses ability to to make acth and without acth adrenal glands atrophy and lose ability to make cortisol and other glucocorticoids Should taper med if on drug for longer than seven days
ra - ANSWER Goal of tx is to decrease inflammation and pain while maintaining fcn and preventing deformity
RA tx - ANSWER First line is methotrexate aka dmards this to prevent joint deformity and nsaid for inflammation All txs can cause, sepsis, Lymphoma, and tb
Mehtotrexate - ANSWER Can cause damage to bone marrow liver and lungs
RA biologic response modifiers - ANSWER Non tnf: Abatacept,Anakinra, tocilizumab Anti tnf: influximab, adalimumab, etancercept, certolizumab, golimumab
Oral JAK inhibitors - ANSWER Can tx ra Tofacitinib
Gout - ANSWER NSAIDS UNLESS -> Add allopurinol for patients with two or more attacks per year or tophaceus gout that has joint damage that is visible on radiography Tx to be considered if Uric acid levels are nine or above
Xanthin oxidase inhibitors (XOIs), - ANSWER allopurinol (first line Aloprim, Lopurin, Zyloprim) or febuxostat (Uloric)
Ok: oral or nasal sq Ae don't give to heart pt, teratogenic
Newest : lasmiditan Scheduled bc causes drowsiness Rimigepant does not cause drowsiness
preventive migraine therapy - ANSWER Should be prescribed if patient needs to use abortive therapy too frequently Beta blockers doses may need to be titration up: propranolol and metoprolol Anti epileptic : depakote, topi ram ate ( also causes wt loss) Tca: amitryptiline low dose at bedtime Calcium channel blocker: verapamil less evidence Botox muscles of scalp neck and upper back Ace inhibitor less evidence Riboflavin, coenzyme 10 Feverfew Butterbur liver damage and cancer Menstrual migraine- ANSWER Tx: naratriptan, frovatriptan, zolmitriptan Plus estrogen gel or patch And naproxen
Treximet - ANSWER sumatriptan/naproxen for migraine
Ergotamine - ANSWER Causes profound vasoconstriction; second line for stopping ongoing headache when pt doesn't respond to triptan Can cause nausea and vomiting Teratogenic
Calcitonin gene-related peptide (CGRP) - ANSWER Ubrogepant To treat acute migraine Interact with azole, macrolide, grapefruit juice and floxins
Cgrp antagonists for migraine prevention - ANSWER New Moa bind and antagonize fcn of cgrp receptors Erenumab sq once a month Galcanezumab Fremanezumab Eptinezumab All injections Se are muscle cramping and constipation $
