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26 Cards in this Set

  • Front
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Diphenylmethane Derivatives:
Drug Class
MOA
AEs
Stimulant laxative

MOA: promotes water accumuln and electrolytes in lumen; stimulates intestinal motility

Inc'd PGs and cAMP to inc secretion of water

AEs:
Damaging if overused-->hyponatremia/kalemia; CATHARTIC COLON (nerve damage--alter reflexes in defecation reflexes)
Bisacodyl:
Drug Class
MOA
AEs
Diphenylmethane Deriv; Stimulant laxative

MOA: promotes water accumuln and electrolytes in lumen; stimulates intestinal motility

Inc'd PGs and cAMP to inc secretion of water

AEs:
Damaging if overused-->hyponatremia/kalemia; CATHARTIC COLON (nerve damage--alter reflexes in defecation reflexes)
Antraquinone laxatives:
Drug Class
MOA
AEs
Stimulant laxative

MOA: promotes water accumuln and electrolytes in lumen; stimulates intestinal motility

Inc'd PGs and cAMP to inc secretion of water

AEs:
Damaging if overused-->hyponatremia/kalemia; CATHARTIC COLON (nerve damage--alter reflexes in defecation reflexes)
Octreotide:
Drug Class
Indication
MOA
SMS analogue
Use in secretory diarrhea

Dec'd release of Ach by acting on enkephalinergic receptors (enteric nerves)
5-ASA:
MOA
AEs
Inhibit PGE2 production

Dec Ab secretion, lymph fn (thus, dec'd nphil and mac chemotaxis)

Inc'd expression of heat shock proteins

AEs: rash, HA, fever, hepatitis (due to hypersens rxn, not sulfa rxn)
First-line therapy for Crohn's and UC.
5-ASA
Budesonide:
Drug Class
MOA
Corticosteroid

Interfere with NF-kappa beta and prevent production of proinflammatory cyotkines
Azothioprine:
Drug Class
MOA
Time of Onset
AEs
Immunomodulator--Thioguanine derivative

Metabolized to 6-thioguanine (active agent)-->incorporated into nucs and prevents lymphocyte prolifern

Also inhibit NKC and T cell fn

Takes 3-4 months for effect--NOT FOR FLARE-UPS

AEs:
Leukopenia
Infliximab:
Drug Class
MOA
AEs
Biological Response Modifier
MOA:
MAb xTNF-alpha

Used for severe CD/UC

AEs:
Opportunistic infections, esp Tb (need TNF-alpha to respond to infections)
Hypersens rxn to MAb
This biological exhibits LESS antigenicity than infliximab.
adalimumab
Natalizumab:
Drug Class
MOA
Indications
AEs
Biological Response Modifier

MOA:
Ab x alpha-4 integrin; blocks adhesion and leukocyte migration into gut (works all over body too)

mod to severe CD, UC

AEs: progressive multifocal leukoencephalopathy
Parietal cells:
Describe activation by:
Endocrine stimulation
Paracrine stimulation
Neural stimulation

Include differences in pumps activated.
Endocrine: gastrin release from G cells; works 2 ways:
1) Stimulates release of histamine from ECL cells
2) Stimulates CCK2 receptors on parietal cells to activate Ca2+ dependent proton pump

Paracrine: histamine released from ECL cells:
Acts at H2 receptors on parietal cells stimulating cAMP-dep activation of proton pump


Neural stimulation via vagus (ACh)-->2 ways:

1) Stimulates release of histamine from ECL cells
2) ACh (from enteric neurons) act directly on parietal cells stimulating M2/M3 receptors and activating Ca2+ dep activation of proton pump.
Prostaglandin effects on gastrin secretion.
1) binds PGE receptors on parietal cells-->inhibits cAMP-dep PW

2) Stimulates secretion of mucus and bicarb from epithelial cells
Cimetidine:
Drug class
AEs
H2 antag

AEs:
inhibits renal elimination of other basic drugs (procainamide)

inhibits cyp450, reducing metabolism of many drugs (phenytoin, theophylline, phenobarb, warfarin, TCA, CCBs)

GYNECOMASTIA, impotence, lactation (enhances secretion of PL)

note: cyp450 inhibition AND PL secretion (also binds androgen receptors) are unique to cimetidine and does not apply to other H2 antags
What drug is contraindicated with clopidogrel?

Why?
Omeprazole:
inhibits cyp450 enzyme that activates clopidogrel, thus reducing clopidogrel's inhibitory effect on platelet aggregation.
Omeprazole:
Drug Class
Proton Pump Inhibitor
RACEMIC MIXTRUE of R and S isomers (S = esomeprazole)
This antacid is contraindicated with tetracycline.
Al(OH)3; inhibits tetracycline's absorption
Sucralfate:
Drug Class
MOA
AEs
Sucralfate = Al(OH)3 + sulfated sucrose
Cytoprotective Agent

MOA: binds protein components of ulcer to form protective coating; this prevents degradative activity of pepsin and acid.

May also stimulate mucus and bicarb secretion, and may increase PG synthesis.

AE:
Constipation (contains Al(OH)3)

Dec'd bioavail of teatracycline, phenytoin, digoxin, cimetidine
Misoprostol:
Drug Class
MOA
Indications
AEs
Misoprostol = PGE2 analog

Cytoprotective agent

Acts as PGE2 analog and inhibits acid secretion; stimulates bicarb and mucus secretion

Indicated in pts who require NSAID tx

AEs:
Cramping and diarrhea due to inc'd GI secretion and motility

Contraction of uterine SM-->abortion
What are the effects of prokinetic agents?
Increase LES pressure, enhance esophageal peristalsis
Metoclopromide:
Drug Class
MOA
Prokinetic AND ANTIEMETIC

Enhanced release of ACh from nerves innervating GI tract smooth muscle

Also: 5HT4/ agonist (release ACh to enhance more ACh release), 5HT3 antag (suppress NANC), D2 antag--provides antiemetic effect (blocks D2 receptors in chemoreceptor trigger zone, solitary tract nucleus)
Cisapride:
Drug Class
MOA
AEs
Enhances release of ACh from nerves innervating SmoothM of GI tract

Also 5HT4 agonist, 5HT3 antag

FATAL ARRHYTHMIAS due to prolongation of QT interval.
Lesogaberan:
Drug Class
MOA
Effect
Motility altering agent

GABA-B agonist that inhibits signaling from vagal afferents in stomach and esophagus to reduce mechanosensitivity

Also inhibits vagal efferents

Effect: dec'd postprandial, tLESR, inc'd basal LES pressure

STILL IN CLINICAL TRIALS
Chlorpromazine:
Drug Class
MOA
AEs
Antiemetic

Muscarinic and histaminergic antagonist

ALSO ACTS AS NEUROLEPTIC

AEs: hypotn, sedation, tardive dyskinesia!
Haloperidol:
Drug Class
AEs
Antiemetic and neuroleptic

Sedation (less so than chlorpromazine); hypotn (less so than chlorpromazine)
Scopolamine:
Drug Class
Indications
AEs
Antimuscarinic

Motion sickness (not for emesis due to chemotx)

AE: dry mouth, sedation

Note: delivered transdermally