Pharmacology Unit 3 Flashcards
omeprazole
proton pump inhibitor
esomeprazole
proton pump inhibitor
lansoprazole
proton pump inhibitor
cimetidine
H2 receptor antagonist; decrease gastric acid production; 4-5hr duration; high dose decrease testosterone binding and estrdiol hydroxylation causing galactorrhea in women and feminization in men
ranitidine
H2 receptor antagonist; decrease gastric acid production; 6-8 hr duration
famotidine
H2 receptor anatagonist; decrease gastric acid production; 10-12 hr duration
misoprostol
synthetic PGE1 analog; reduce 80-90% of basal or food-indiced acid production; short acting; prevention of NSAID-induced gastric ulcers; adverse: diarrhea, exacerbate IBD, contractions in pregnancy
sucralfate
barrier to protect epithelial cell layer; sucorse + AlOH3; stcks to duodenal ulcers; activated by acid, avoid antaacids or PPIs; Adverse: constipation, block drug absorption
aluminum hydroxide
antacid; slow acting, delays emptying and motility; Adverse: constipation, nausea, phosphate loss, binds tetracycline, rebound acid secretion
magnesium hydroxide
antacid; fast acting; stimulates gastric emptying and motility; avoid in renal disease, rebound acid secretion
Mg-trisilicate
antacid; adverse: avoid in renal disease, silica is absorbed and may cause renal stones, rebound acid secretion
calcium carbonate
antacid
pirenzepine
muscarinic antagonist; decrease gastric acid production; decrease vagal transmission to enteric nerve by blocking ganglionic transmission (M1), decr stimulation of parietal and ECL cells; reduce basal acid production 40-50%; rarely used for significant anticholinergic effects
bethanechol
cholinergic agonist; GI prokinetic agent; selective M2, M3 receptors to produce GI contraction;
Used to help urination post-surgical;
Adverse: cholinergic effects, disrupt natural reflex of oral contraction and anal relaxation
neostigmine methylsulfate
AChE inhibitor; GI prokinetic agent; eccentuate normal ACh release to incr GI motility; used in ileus
metoclopramide
Dopamine receptor antagonist; GI prokinetic agent, incr normal ACh release; incr lower esophageal sphincter tone, used in GERD; also antiemetic and laxative; adverse: antidopamine effects, parkinsonian symptoms, dystonias, tardive dyskenesia in chronic use
tegaserod
5-HT4 partial agonist; GI prokinetic agent; stimulate intrinsic sensory neurons (chemical/mechanical stimulation) increase motility in IBS and chronic constipation/bloating, mildly effective; adverse: fatal cardiac arrhythmia, restricted distribution by FDA; last line therapy
cisapride
5-HT4 partial agonist; GI prokinetic agent; also adenylate cyclase stimulant; used in GERD; adverse: fatal cardiac arrhythmia, restricted distribution by FDA; last line therapy
Erythromycin (macrolide abx)
motilin agonist (stimulate upper small bowel motility produced by EC cells); GI prokinetic agent; cause gastric dumping and emtpying in ileus, scleroderma, and pseudo-obstructions; acute use only
magnesium citrate
osmotic laxative; may stimulate motility through CCK receptors
magnesium hydroxide
osmotic laxative; may stimulate motility through CCK receptors; milk of magnesia
polyethyl glycol
osmotic laxative; alcohol
lactulose
osmotic laxative; used for constipation from opioid and vincristine use; bacterial fermentation can drop pH and trap NH4 in colon of patients with hepatic disease
mannitol
osmotic laxative; used for constipation from opioid and vincristine use
sorbitol
osmotic laxative; used for constipation from opioid and vincristine use
docusate
stool wetting/softener; surfactant that allows fatty substance and water in stool; do not increase frequency of defecation
bisacodyl
irritant laxative; used orally or rectally; overdose leads to catharsis; stimulate motility; dont chew to avoid gastric irritation (target is small intestine)
castor oil
irritant laxative; smooth muscle stimulant; ricinoleic acid speeds motility in small bowel; 4ml for laxative effect-16ml for catharsis
methylcellulose
bulk laxative
polycarbophil
bulk laxative
psyllium
bulk laxative
bismuth subsalicylate (pepto-bismol)
antidiarrheal; salicylate released in stomach and absorbed sytemically
diphenoxylate difenoxin
antidiarrheal; opioid piperidine derivatives; can have CNS effects; packaged with atropine to discourage abuse
loperamide
antidiarrheal; opioid poorly absorbed mu agonist; stops bowel motility; 50x morphine potency; doesnt enter CNS
octreotide
antidiarrheal; somatostatin derivative; parenteral block secretory diarrhea of hormone secreting tumors; inhibit gastrin and serotonin; Uses: post-surgical dumping, diarrhea assoc chemotherpay, pncreatitis; adverse: nausea, vomiting, bloating, injection site pain, gall stones with long term use
chlorpromazine
antiemetic; phenothiazine dopamine receptor antagonist; target D2 in CTZ and H1; uses: nausea, emesis, morning sickness (H1); adverse: parkinsonian symptoms, dysphoria
cyclizine
antiemetic; Antihistamine (h1); also has anticholinergic effects used in abdominal cancer; used in morning sickness, postop emesis; acts in STN and vestibular apparatus
diphenhydramine (Benadryl)
antiemetic; antiemetic; Antihistamine (h1); used in morning sickness, postop emesis; acts in STN and vestibular apparatus;
dimenhydrinate (Dramamine)
antiemetic; salt of dephenhydramine and chlorotheophylinate (stimulant to stop sedation)
dolasetron
antiemetic; 5-HT3 antagonist (CTZ, STN, and small intestine); oral and parenteral; 8 hr half-life
hydroxyzine
antiemetic; Antihistamine (h1); used in morning sickness, postop emesis; acts in STN and vestibular apparatus
granisetron
antiemetic; 5-HT3 antagonist (CTZ, STN, and small intestine); oral and parenteral; 10 hr half-life
metochlopramide
antiemetic; dopamine antagonist; prevents emesis and promotes defecation (prokinetic effect); preferred in chemotherpay induced nausea
ondansetron
antiemetic; 5-HT3 antagonist (CTZ, STN, and small intestine); oral and parenteral; 4 hr half-life
palonosetron
antiemetic; 5-HT3 antagonist (CTZ, STN, and small intestine) (highest affinity in class); parenteral only; 40 hr half-life
prochlorperazine
antiemetic; phenothiazine dopamine receptor antagonist; target D2 in CTZ and H1; uses: nausea, emesis, morning sickness (H1); adverse: parkinsonian symptoms, dysphoria
promethazine
antiemetic; Antihistamine (h1); used in morning sickness, postop emesis; acts in STN and vestibular apparatus
scopolamine
antiemetic; muscarinic (ACh) antagonist; parenteral or transdermal patch; acts on M receptor in vestibular apparatus; minimal CTZ effect (not effective with chemo-induced nausea; uses: short and long term motion sickness, post op emesis; adverse: xerostomia, blurred vision, may cause uncontrolled behavior when used with anxiety or pain
apomorphine
emetic agent; acts on CTZ; subQ; superseded by acrtivated charcoal
ipecac
emetic agent; acts on CTZ; superseded by activated charcoal; oral use shrotly after ingestion of drug or toxin
6-mercaptopurine
IBD thiopurine therpay; converted to 6-thiioguanine, inhibits DNA synthesis; immunosupressive; maintain remission of IBD and help fistulas in Crohns; adverse: pancreatitis, marrow supression, fever, rash, arthralgia, n/v
adalimumab
IBD immune modulator; human anti-TNF-a ab; may be less effective than infliximab; parenteral; for crohns and UC; adverse: incr infecctions (URIs), lack of repsonse to Tb
alosetron
IBS tx focues on motility; 5-HT3 antagoinst; decr bowel motility; used for diarrhea predominant in IBS; adverse: constipation -> ischemic colitis; dangerous
azathioprine
IBD thiopurine; converted to 6-mercaptopurine -> 6-thioguanine -> inhibit DNA synthesis
budesonide
IBD glucocorticoid; oral; 200X more portent than hydrocortisone but not well absorbed from bowel -topical tx for bowel; adverse: typical ssteroid effects, well tolerated (only 10% bioavailable and most removed by first pass)
infliximab
IBD immune modulator; anti-TNF-a “humanized” ab; interferes with inflammatory process; parenteral; for crohns and UC; adverse: incr infecctions (URIs), lack of repsonse to Tb
mesalamine
IBD 5-ASA therapy; pH senstive capsule released in ileum, delayed releasse capsule releases in jejunum; uses: IBD flar-ups, maintenance of remission of UC; adverse: interstitial nephritis, headache, dyspepsia, rash
olsalazine
IBD 5-ASA therapy; prodrug converted in in colon to mesalamine; uses: IBD flar-ups, maintenance of remission of UC; adverse: diarrhea, headache, dyspepsia, rash; better tolerated than sulfsalazine
prednisone
IBD glucocorticoid; oral use for acurte exacerbation and severe disease; target infalmmation and immune response; adverse: typical steroid effect (immunosupression, endocrine disruption, steroid psychoses)
sulfasalazine
IBD 5-ASA therapy; prodrug converted in in colon to mesalamine; uses: IBD flar-ups, maintenance of remission of UC; adverse: due to sulfa group - headache, nausea, fatigue, allergic rxn, contraindicated in pregnancy
heparin sulfate
anticoagulant; measured effect by PTT; binds anti-thrombin III and inactivation IXa, Xa, and IIa; administered as initial bolus followed by continuous infusion; Adverse: bleeding, heparin-induced thrombocytopenia (less with LMW); antagonized by protamine sulfate; FFP does not correct heparin effect
warfarin
anticoagulant; antagonizes vit K dependant gamma-carboxylation of procoagulants II, VII, IX, X and proteins C and S; blocks regeneration of reduced K; Monitored by INR (PT); antagonized by menadione (vit K); given oral; interacts with basically ALL drugs; adverse: bleeding (exaggerated by NSAID use), clotting with initial therpay withut heparin; teratogenic (not for pregnancy), cause skin necrosis (high dose); FFP can correct warfarin effect
dalteparin
LMW heparin
enoxaparin
LMW heparin
fondaparinux
ultra-LMW heparin
argatroban
direct thrombin inhibitor; IV; short acting; hepatically cleared; indication when heparin is needed and there is hx of heparin-induced thrombocytopenia
bivalirudin
direct thrombin inhibitor; IV; synthetic hirudin
dabigatran etexilate
direct thrombin inhibitor; oral; no antogonist!
t-PA
thrombolytic; activated plasminogen -> plasim -> fibrin degredation
streptokinase
thrombolytic; from B-hemolytic strep; forms complex with plasminogen -> activation; adverse: anaphylaxis and fever; must be given at arge dose to overcome neutralizing abs
urokinase
thrombolytic; isolated from human cells (no neutralizing abs); activates plasminogen; rapidly metabolized (10-15 min half-life)0
abciximab
anti-platelet; Anti-c7E3 ab; binds glycoprotine IIb/IIIa receptor and inhibits fibrinogen bindings platelets and platelet aggreagation
aspirin
anti-platelet; irreversilby inhibits COX for life of platelet -> thromboxane A2 production -> decr platelet aggregation, vasoconstriction; half-life 4hr but effect can last days
clopidogrel
anti-platelet; oral;adverse: thrombotic thrombocytopenia purpura