Pharm Exam 3 Flashcards
(189 cards)
Cortisol
glucocorticoid, secreted in response to ACTH
interact with specific nuclear receptors to increase or decrease the expression of corticoresponsive genes
anti-inflammatory effects largely mediated by transrepression — main mechanism is repression of phospholipase A2; also COX2 & prevents proinflammatory cytokine expression & decreases number of immune cells
metabolic effects: upregulation of trangluconeogenesis enzymes
inactivated by 11βHSD2 (kidneys)
net metabolic effect is increased blood glucose levels
Cushings
A/E: impairs HPA axis, fluid/electrolyte abnormalities, HTN, hyperglycemia, increased risk for infx, osteoporosis/decreased bone density, myopathy, behavioral disturbances, cataracts, retarded growth, fat redistribution, striae
Betamethasone
long acting synthetic corticosteroid; anti-inflammatory effects 25x more potent than cortisol; long half life; no Na+ retention effects; 0.25 equivalent dose to cortisol
most commonly used topically for skin infections
Dexamethasone
longest acting synthetic corticosteroid; anti-inflammatory effects 25x more potent than cortisol; long half life; no Na+ retention effects; 0.25 equivalent dose to cortisol
used for acute adrenal crisis
Prednisone
intermediate strength corticosteroid (12-36 hr duration)
used for acute organ rejection, chronic adrenal insufficiency, rheumatic diseases, giant cell arteritis, systemic skin diseases (atopic dermatitis), IBD,
Triamcinolone
intermediate glucocorticoid
used for non-inflammatory joint disease (osteoarthritis), skin diseases (intralesional prep)
also used for asthma
Metyrapone
cortisol synthesis inhibitor
inhibits CYP 11B1
used to treat hypercortisolism, diagnostic tests of HPA axis
Ketoconazole
cortisol synthesis inhibitor
at high doses, inhibits CYP 17 (to synthesize cortisol & DHEA)
***most effective inhibitor to treat Cushings
anti-fungal at low doses
Aminoglutethimide
cortisol synthesis inhibitor
inhibits CYP 11A (initial & rate-limiting step)
used to treat Cushings
Aldosterone
endogenous mineralocorticoid
synthesized in response to K+ & angiotensin II
stimulates renal exchange between Na+/K+ or H+
acts on distal tubules & collecting ducts of kidney to increase reabsorption of Na+ (& thus water) & promote K+ excretion — results in fluid retention, increased BP
increase cardiac fibrosis
congenital adrenal hyperplasia commonly caused by CYP 21 mutation — decreases synthesis of aldosterone
Fludrocortisone
mineralocorticoid
mineralocorticoid agonist
use with corticosteroid in patients with CAH that also have salt wasting
Alfentanil
Opioid (class: Phenylpiperadine)
DOC for outpatient anesthesia — repeated doses do not accumulate, recovery is rapid
Codeine
opioid (class phenanthrene)
prodrug that gets metabolized to morphine by CYP 2D6; chemical modification improves 1st pass survivability
potency similar to morphine
oral analgesic & anti-tussive
Fentanyl
synthetic opioid (phenylpiperadine class)
80-100x greater potency compared to morphine
shorter duration
highly lipophilic, rapid distribution to other compartments
analgesic; improved cardiac stability; not anesthetic
fentanyl lollipop used for breakthrough pain
Hydrocodone
semi-synthetic opioid (class phenanthrene)
greater potency compared to morphine
Meperidine
Demerol
synthetic opioid (class phenylpiperadine)
1/10 morphine’s potency
25% bioavailable
used in labor & delivery
reduced likelihood of biliary spasm; does not cause miosis
toxicity: CNS excitation — seizure, tremor, convulsions — metabolite in patients with impaired renal function
Methadone
synthetic opioid (class phenylheptanone) -one of the highest risk
equipotent with morphine
high bioavailability
once daily dosage, PO
longer acting opioid
improved risk for heroin addicts
some NMDA receptor antagonist properties
Morphine
opioid (phenanthrene class)
central effects: analgesia, respiratory depression, anti-tussive (suppresses brainstem cough centers) miosis, tolerance, dependence
peripheral effects: analgesia, constipation, GI spasm; generally increases smooth muscle tone
degranulation of mast cells (which can cause pruritis, systemic hypotension)
active metabolites: excitotoxic, analgesic
main A/E: respiratory depression; also miosis, coma
more effective against continuous, dull pain
opioid for rescue drug for intractable migraine
Oxycodone
semi-synthetic opioid (class phenanthrene)
greater potency compared to morphine
Remifentanil
synthetic opioid (phenylpiperidine class)
Sufentanil
synthetic opioid (phenylpiperidine class)
Tapentadol
mixed opioid analgesic
moderate mu receptor agonist, NE reuptake inhibitor
metabolically stable congener of O-desmethyltramadol
Tramadol
mixed opioid analgesic — 5HT releaser, NE reuptake inhibitor, weak mu opioid receptor agonist
O-desmethyltramadol metabolite is a stronger mu agonist (CYP2D6 conversion)
toxicity: seziures (NOT respiratory depression)
Naloxone
mu opioid antagonist
shortest duration of action, not available orally because it gets destroyed in the liver before getting to bloodstream
use to treat opioid overdose; also alcoholism (by helping remove the positive reinforcement)
in healthy subjects does not alter pain threshold but increases hormone secretion
hyperalgesic in post surgery patients
attenuates/reduces analgesic effects
Naltrexone
opioid antagonist
longest duration of action
available orally
addict maintenance