Advanced Pharm Exam 1 Flashcards
Aspirin- drug class?
NSAID: COX inhibitor (1st generation- inhibits COX-1 (stronger) & COX-2)
Aspirin- MOA?
Nonselective COX inhibitor, rapid binding/inhibition:
COX-1 inhibition leads to irreversible modification of platelets (last the life of platelet ~8days, until turnover), leading to decreased platelet aggregation and decreasing risk of stroke and MI.
COX-2 inhibition inhibits prostaglandin production, which decreases inflammation pathway including, decreasing pain and fever.
Aspirin induces ATLs, anti-inflammatory compounds.
Aspirin- adverse effects?
Gastro- GI distress, heartburn nausea, GI bleed, perforation, GI ulceration (with long-term use)
Renal- Renal impairment
Reyes Syndrome- in children: encephalopathy and fatty liver degeneration
Aspirin- indications
RA, OA (when other non-pharm routes and topical NSAIDs don’t work) - esp. when in multiple joints or hip joint
Aspirin- excretion?
Kidneys
What are the corticosteroid prototype drugs?
Prednisone, hydrocortisone, cortisone, methylprednisolone
Corticosteroids- indications?
RA, OA, asthma, Crohn’s disease, UC, IB
Used for inflammatory/immunologic disorders
Used as adjunctive for short term admin., during acute or exacerbation
Ibuprofen- indications?
RA and OA, pain relief, dysmenorrhea
Aspirin- max dose
3900mg PO
Ibuprofen- max dose?
3200mg/day PO over 3-4 doses
400mg every 4-6hours PRN
Ibuprofen- adverse effects?
Cardiovascular risk- thrombotic events, MI, stroke
GI risk- bleeding, ulceration, perforation (stomach/intestines)- GI risks higher for elderly
Corticosteroids- adverse effects
hypothalamic-pituitary-adrenal axis suppression: adrenal insufficiency
osteoporosis: from decreased osteoblasts decreasing bone formation and increased osteoclasts increasing bone resorption and decreased intestinal calcium leading to hypocalcemia leading to increased PTH leading to removal of calcium from the bone into blood
short term: hyperglycemia, BP changes, edema, GI bleed, poor wound healing, increased risk of infection, hypokalemia/hyperkalemia
Corticosteroids- MOA
Decrease prostaglandin & decrease leukotrienes -> decreased pro-inflammatory metabolites -> decreased inflammation
interrupted inflammatory process -> [decreased mediator synthesis -> decreased swelling, redness, pain, warmth AND decreased phagocytes -> decreased lysosomal enzymes -> decreased tissue injury -> decreased inflammation AND decreased lymphocyte proliferation -> decreased immune inflammatory response]
Ibuprofen- MOA?
Nonselective COX inhibition:
Cox-1 reversible inhibition (weaker than Aspirin) -> decreased platelet aggregation (not as long as Aspirin) -> decreases thrombotic events
Cox-2 inhibition -> decreases prostaglandin precursors -> decreased inflammatory response -> pain, fever, inflammation
Naproxen- drug class?
NSAID: 1st gen.- nonselective COX inhibitor
What are the NSAID prototype drugs?
Aspirin, Ibuprofen, Naproxen, Celecoxib, Indomethacin, Ketorolac
Indomethacin- drug class?
NSAID
Indomethacin- indications?
RA, OA, gout, closure of neonatal patent ductus arteriosus
Indomethacin- MOA?
COX inhibition -> decreased prostaglandin -> vasoconstriction (for patent ductus arteriosus) AND decreased inflammation AND decreased pain
Indomethacin- max dose?
150mg / day
Indomethacin- adverse effects?
Increased risk for CNS side effects: severe frontal headache, dizziness, vertigo, light-headed, confusion
Celecoxib- contraindications?
Patients with heart disease or recent CABG surgery
Celecoxib- drug class?
NSAID- 2nd gen. selective COX-2 inhibitor
Celecoxib- indications?
RA, OA, ankylosing spondylitis, migraine, pain, dysmenorrhea
Celecoxib- MOA?
Selective COX-2 inhibition -> decreased COX-2 -> increased vasoconstriction AND decreased prostaglandin precursors -> decreased prostaglandin synthesis -> decreased pain and inflammation
Celecoxib- dosing?
200mg
Celecoxib- adverse effects?
serious cardiovascular risk: increased risk of MI and stroke
GI risk
renal impairment
Diclofenac- drug class?
NSAID- 1st gen. nonselective COX inhibitor
Diclofenac- indications?
RA, OA, pain, dysmenorrhea
Diclofenac- MOA?
first phase: COX-1 and -2 inhibition -> decreased plasma levels -> COX-2 inhibition (only) {later phase}
Diclofenac- dosing?
Max: 200mg/day
Diclofenac- adverse effects?
Cardiovascular risk, GI risk
Diclofenac- routes?
Oral, topical (patch, spray, cream)
Ketorolac- drug class?
NSAID
Ketorolac- indications?
OA, RA
short term management of acute pain (5days or less)
Strong analgesic: rapid onset, short duration
Medium anti-inflammatory drug
Ketorolac- MOA?
COX inhibition -> decreased pain, inflammation
Ketorolac- dosing?
Max: 120mg/day for max 5 days
Ketorolac- adverse effects?
GI risk, renal damage, bleeding, hypersensitivity
Ketorolac- routes?
Oral, IV, IM, intranasally
Naproxen- indications?
Gout, RA, OA, abnormal uterine bleeding, pain, fever
Naproxen- MOA?
Nonselective COX inhibitor -> decrease prostaglandin precursors -> decrease inflammatory pathway -> decreased pain, fever, inflammation
Naproxen- dosing?
Max: 1.5g / day
Naproxen- adverse effects?
GI risk, renal impairment, nausea, dizziness, tinnitus
Acetaminophen- drug class?
Non-NSAID analgesic/antipyretic
(not anti-inflammatory)
Acetaminophen- indication?
Pain, fever
Acetaminophen- MOA?
CNS COX inhibition -> decreased prostaglandin synthesis in CNS -> decreased fever and pain
Acetaminophen- dosing?
4,000mg / 24hours
Acetaminophen- adverse effects?
Toxicity, liver damage: 72-96hours post ingestion, severe hepatomegaly (AST > 10,000IU/L), plasma bilirubin > 4.0mg/dL
RA- tests?
ESR/CRP: elevated
RA- S/Sx
Morning stiffness (doesn’t resolve with movement), symmetric inflammation/pain
OA- S/Sx
Joint pain, stiffness, swelling/tenderness, grating/clicking with movement, decreased ROM
RA vs. OA
RA: morning stiffness, symmetrical swelling/pain, caused by autoimmune
OA: asymmetrical swelling/pain, grating/clicking sound w/ movement, caused by injuries/overuse
CD vs. UC
CD: inflammation throughout GI (mouth to anus), patches of damage reaching outer lining, NOT bloody diarrhea
UC: inflammation in colon & rectum, damage maintained in inner lining, bloody diarrhea
Glucocorticoids- MOA for osteoporosis?
Increased osteoclasts, decreased osteoblasts, increased calcium excretion, decreased calcium absorption
Glucocorticoids- bone loss time frame?
After initiating steroid therapy: increased bone loss within the first 3-6months
After 6 months of therapy: continued, slowed bone loss
Increased fracture risk with 3months of Prednisone, more than 5mg / day
Osteoclasts
Bone “carving”, resorption (2-3weeks)
Activated by: osteoblasts, PTH, thyroid hormone, Vitamin D3, thyroid hormone, glucocorticoids
Osteoblasts
Bone “building”, formation
Regulated by: PTH, Vitamin D, insulin growth factor
Inhibited by: glucocorticoids
Recommended Calcium intake for adults?
1000-1200mg elemental calcium
500mg/ dose, divided throughout the day
What is required for calcium absorption?
Vitamin D
Vitamin D deficiency can cause what in adults and what in children?
Adults: osteomalacia
children: Rickets
Deficiency: Serum vitamin D <30mg/mL
PTH Pathway- start with Caclium
decreased calcium -> increased PTH -> increased calcium reabsorption -> decreased calcium in bones -> increased calcium in blood
Calcium carbonate (CaCO3)- environmental requirements?
Acidic environment for absorption- must be taken with meals
Calcium carbonate- adverse effects?
Constipation, hypocalcemia, nausea
Calcium carbonate- indications?
GERD (reduces acid in stomach)
Osteoporosis (maintains calcium levels in the blood)
Calcium carbonate- max dose?
2000mg / day
Alendronate- drug class?
Bisphosphonate: Antiresorptive agent
Alendronate- MOA?
Antiresorptive- inhibits osteoclast activity -> decreases bone loss
Bisphosphonates- contraindications?
Hypocalcemia (d/t inhibited osteoclasts -> decreased calcium released into blood)
Inability to sit up right
Caution with renal impairment (DONT USE if CrCl <35mL/min)
Bisphosphonates- adverse effects?
Dyspepsia, dysphagia, heartburn, nausea, vomiting, hypocalcemia
(bisphosphonates bind to mucosal lining of esophagus -> decrease protection -> irritation of esophagus -> dysphagia, heartburn, nausea, vomiting)
Bisphosphonates- dosing?
Must be taken separate from calcium, iron, magnesium and antiacids by at least 2 hours
Bisphosphonates- treatment duration?
3-5years (pts with low fracture risk)
Bisphosphonate- MOA?
Antiresorptive: osteoclast inhibition -> decreased calcium resorption -> decreased calcium leaving bone -> decreased bone loss
Alendronate- dosing?
Prevention: 5mg PO / day
Treatment: 10mg PO / day
Ibandronate- drug class?
Bisphosphonate- antiresorptive
Ibandronate- MOA?
Osteoclast inhibition
Ibandronate- routes?
PO, IV (if pt cant sit upright/esophagitis)
Ibandronate- dosing?
Oral: 150mg / monthly (must stay upright at least 30min)
IV: 3mg / 3months (slow admin.)
Alendronate- indication?
Osteoporosis
Ibandronate- indication?
Osteoporosis (for post-menopausal women)
Raloxifene- drug class?
Selective estrogen receptor modulator (SERM)
Raloxifene- MOA?
SERM: Estrogen agonist/antagonist -> decreased bone resorption
Raloxifene- dosing?
60mg / day (prevention & treatment)
Separate from levothyroxine
Discontinue 72hours before prolonged immobilization (surgery)
Raloxifene- contraindications?
History of VTE, pregnancy
Increases risk of venous thromboembolism (VTE)
Raloxifene- adverse effects?
Hot flashes, peripheral edema, arthralgia, leg cramps/muscle spasms/flu symptoms
Menopausal symptoms
What form can Vitamin D supplementation be in to help with bone building?
Vitamin D3 and Vitamin D2
Raloxifene- indication?
Osteoporosis- treatment and prevention (postmenopausal women)
What drugs can treat osteoperosis?
Raloxifene, Ibandronate, Alendronate, Calcium Carbonate
What are the two parts in asthma treatment?
Bronchodilation (symptom relief)
Inhaled corticosteroid (control of inflammation)
What is the primary treatment of COPD?
Bronchodilators
GOLD COPD Guidlines
Group A (low exacerbations/assessment score): only bronchodilator
Group : (low exacerbations and assessment score): bronchodilator and LAMA/LABA
Groups E (high exacerbations): bronchodilator and LABA/LAMA
Which of these gets shaken before use?: MDI or DPI
MDI (metered dose inhaler)- use a propellant spray
Which of these does NOT get shaken before use?: MDI or DPI
DPI (dry powder inhaler)
What drug is a short acting beta2 agonist? (SABA)
Albuterol
What is a short acting beta2 agonist (SABA)?
Short term relief- rescue inhaler
What is a long acting beta2 agonist (LABA)?
Long term maintenance, not used alone for asthma
Salmeterol
Albuterol- dose?
MDI/DPI 1-2 inhalations / 4-6hours
Nebulizer
Albuterol- cautions?
CVD, glaucoma, hyperthyroidism, seizures, diabetes
Albuterol- adverse effects?
Nervousness, tremor, tachycardia, palpitations, cough, hyperglycemia, decreased potassium
Albuterol- drug class?
Short acting beta2 agonist (SABA)
Salmeterol- drug class?
Long acting beta2 agonist (LABA)
Salmeterol- dosing?
DPI 1 inhalation BID (2x / day)
Maintenance inhaler only
Salmeterol- adverse effects?
Nervousness, tremor, tachycardia, palpitations, cough, hyperglycemia, decreased potassium
Salmeterol- cautions?
Only use in pts receiving inhaled corticosteroids
Maintenance inhaler only
Can oral corticosteroids be used long-term?
NO, significant adverse effects:
mood swings, hypertension, etc
What drugs are inhaled corticosteroids?
Fluticasone and budesonide
Inhaled corticosteroids (ICS)- adverse effects?
Fluticasone and budesonide-
Prolonged high doses -> adrenal suppression
Dysphonia, oral candidiasis (thrush)
What drug do you need to rinse and spit after use?
ICS- fluticasone and budesonide
ICS (fluticasone and budesonide)- MOA?
Activates anti-inflammatory gene expression -> suppresses airway inflammation -> controls underlying inflammation in asthma
ICS (fluticasone and budesonide)- indication?
Asthma (long-term)
What drugs are muscarinic antagonists?
Ipratropium and tiotropium
Which drug is a short acting muscarinic antagonist (SAMA)?
Ipratropium
Which drug is a long acting muscarinic antagonist (LAMA)?
Tiotropium
Ipratropium- drug class?
Anticholinergic bronchodilator- short acting muscarinic antagonist (SAMA)
Tiotropium- drug class?
Anticholinergic bronchodilator- long acting muscarinic antagonist (LAMA)
Anticholinergic bronchodilators: muscarinic antagonists- MOA?
inhibition of airway vagal tone -> blocks bronchoconstriction effects -> bronchodilation -> relieves COPD symptoms of obstruction
Ipratropium- indication?
COPD, asthma
Tiotropium- indication?
COPD
Ipratropium- dosing?
MDI 2inhalations / 4 times daily
Ipratropium- adverse effects?
dry mouth, URTI, cough, bitter taste
Tiotropium- dosing?
MDI 2 inhalations / day
Tiotropium- indications?
COPD maintenance treatment
Tiotropium- adverse effects?
dry mouth, urinary retention, cough, hoarseness
What drugs are oral corticosteroids?
Prednisone, methylprednisolone
What is a prednisone steroid burst?
40-60mg prednisone daily for 3-10 days (or more if no change), taper down (gradual reduction to determine lowest dose to keep pt symptom free)
Long term effects of oral corticosteroids (prednisone and methylprednisolone?
adrenal suppression, osteoporosis, hyperglycemia, immunosuppression
Short term effects of oral corticosteroids (prednisone and methylprednisolone)?
Hyperglycemia, insomnia, irritation, upset stomach
What is a methylprednisolone steroid burst?
Asthma exacerbation (no response from SABA): 40-60mg / day for 5-7 days, or resolution of symptoms
COPD exacerbation: 40-60mg/ day for 5-14 days (use IV if pt cant PO)
Prednisone- indications?
COPD, asthma, IBD, OA, RA
Methylprednisolone- indications?
COPD, asthma, UC, CD, OA, RA
Montelukast- drug class?
Leukotriene receptor antagonist (reduces airway inflammation and constriction)
Montelukast- indication?
Asthma
Montelukast- dosing?
10mg / day in the evening
Montelukast- warnings?
Neuropsychiatric events (mood changes, suicidal thoughts/actions)- to be monitored
Montelukast- adverse effects?
headache, abdominal pain, increased liver function tests
What drugs are antihistamines?
Azelastine, Cetirizine, Fexofenadine, Levocetirizine, Loratadine
Which antihistamines is most sedating but faster onset?
Cetirizine and levocetirizine
Which antihistamines are less sedating?
Fexofenadine and loratadine
What drugs are used for GERD?
Calcium carbonate, famotidine, pantoprazole
What drugs are used for PUD?
Bismuth subsalicylate, metronidazole, tetracyclines
What drugs are used for Ulcerative Colitis (UC) / Crohn’s Disease (CD)?
Azathioprine, ustekinumab, vedolizumab
What drugs are used for IBS- constipation?
Polyethylene glycol, methylcellulose, linaclotide, lubiprostone
What drugs are used for IBS- diahrrea?
Loperamide, dicyclomine
Calcium carbonate- adverse effects?
constipation, bloating, belching
Famotidine- drug class?
Histamine-2 receptor antagonist
Famotidine- indication?
GERD
Famotidine- MOA?
Binds to H-2 receptor -> antagonizes effects of histamine on partial cells -> decreased acid secretion
Famotidine- onset?
within 60minutes
Famotidine- duration?
4-10hours
Famotidine- adverse effects?
Tolerance if taken on a schedule (take PRN)
Famotidine- warnings?
Delirium, vitamin B12 deficiency w/ prolonged use >2years
QT prolongation w/ renal dysfunction
Pantoprazole- drug class?
Proton Pump Inhibitor (PPI)
Pantoprazole- indication?
GERD, PUD, H. pylori infections
Pantoprazole- MOA?
Binds (irreversibly) to gastric H+, K+-ATPase in parietal cells -> inhibit acid secretion
Pantoprazole- onset?
1-3hours
Pantoprazole- duration?
> 24hours
Pantoprazole- therapeutic/symptom relief?
1-4days (not for immediate relief, can be paired with calcium carbonate)
Pantoprazole- warnings?
C. diff, osteoporosis (long-term use, >1year), Vitamin B12 deficiency(prolonged use >2years)
Rebound acid secretion- if stopped abruptly, must taper down over 4-6weeks
Pantoprazole- adverse effects?
headache, ab pain, nausea, diarrhea
Pantoprazole- dosing?
Take 30-60minutes before meals to maximize effects
Tetracycline- indication?
PUD, triple therapy
Tetracycline- adverse effects?
Photosensitivity, tooth discoloration (children)
Bismuth- indication?
PUD, combination therapy, GERD
Bismuth- adverse effects?
dark stools, dark “hairy” tongue
Metronidazole- indication?
PUD, combination therapy
Metronidazole- adverse effects?
N/V/D, ab pain, metallic taste
Avoid alcohol
What is Inflammatory Bowel Disease (IBD)?
Ulcerative colitis, Crohn’s disease
Vedolizumab- indication?
CD, UC
Vedolizumab- MOA?
Binds to alpha4beta7 integrin -> blocks interaction with mucosal addressin cell adhesion molecule 1 -> inhibits migration of memory T-lymphocytes across endothelium into inflamed GI parenchymal tissue
Vedolizumab- dosing?
300mg at 0week, 2weeks, then every 8weeks
d/c if no results after 14weeks
Ustekinumab- indications?
CD, UC
Ustekinumab- MOA?
Interferes w/ cytokines, IL12, IL13 -> inhibits T-cell activation -> inhibits inflammatory response
Ustekinumab- dosing?
First: 260-520mg IV single dose
Maintenance: 90mg SW Q8weeks, 8weeks after first dose
Duloxetine- Drug class? indications? MOA?
Selective serotonin reuptake inhibitor (SNRI- used for depression)
Osteoarthritis
Increases serotonin and norepinephrine in brain -> decreased pain signals
Methotrexate- indications? MOA?
OA, RA
Promotes release of adenosine -> anti-inflammatory
Adalimumab- drug class? Indication? MOA?
Biologics
Autoimmune disease (RA), CD, UC
Blocks tumor necrosis factor (TNF-a) from binding to receptor -> prevents activation of inflammatory pathways / producing cytokines
Infliximab- drug class? Indications? MOA?
Biologics
CD, UC, RA
Binds to TNF-a -> inflammatory response is blocked -> reduces inflammation