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GASTROINTESTINAL DRUGS - Coggle Diagram

- - - - first line ulcerative colitis
      - off label: crohn's disease
    - - sulfasalazine
        
        AE: sulfapyridine:
        
        derm
        
        pruritus
        
        rash
        
        GI
        
        ab pain
        
        loss appetite
        
        nausea
        
        vomitting
        
        folate toxicity reduce folic absorption
      - olsalazine and balsalazide
        
        AE: secretory diarrhea
    - - Azo compound
        
        20-30%
        
        decrease absorption in small intestine
        
        taken up by liver
        
        excreted unmetabolized in bile
        
        70 % distal GI tract: azo-bond cleaved by bacteria
      - absorbed from small intestine
      - does not reach distal small bowel or colon
    - - inhibits prostaglandin production
      - may inhbit NFkB activity
  - - - MOA
        
        : inhibition of dihydrofolate reductase
      - use: MAINTENANCE OF REMISSION
        
        crohn's disease
        
        ulcerative colitis
      - PK:
        
        renal elimination
        
        onset of action: weeks
      - AE
        
        :nauseated_face:
        
        leukopenia
        
        :forbidden:
        
        :forbidden: :pregnant_woman:
      - INTERACTION
        
        drug inhibit renal secretion of MTX
        
        salicylates
        
        NSAID
        
        PCN
        
        MONITOR
        
        CBCs
        
        liver function test
        
        q1-3 months
    - - use MAINTENANCE
        
        crohn's disease
        
        ulcerative colitis
      - AE
        
        myelosuppression
        
        N/V :nauseated_face:
        
        increase risk of lymphoma
        
        alopecia, rash :older_man:
        
        hepatoxicity
        
        pancreatitis
      - PK
        
        interaction: allopurinol
        
        xanthine oxidase inhibitor
        
        increase active 6-thioguanine
        
        severe leukopenia
        
        requires dose reduction of thiopurine derivative if pt on allpurinol
        
        monitor
        
        TMPT
        
        low level: bone marrow suppression
        
        high: less active drug
        
        CBC
        
        liver function
        
        onset of action: weeks
      - MOA
        
        incorporate fake base into DNA
        
        strand breakage
        
        inhibit inflammatory cell proliferation
      - proDRUG
        
        mercaptopurine (6-MP)
        
        azathioprine
  - - - natalizumab
        
        use
        
        maintenance of remission of crohn's disease
        
        AE
        
        progressive multifocal leukoencephalopathy
        
        reactivation of JC virus
        
        heptatotoxicity
        
        MOA: mab to integrins
        
        integrins
        
        adhesion molecule that allow WBC to extravasate to sites of inflammation
        
        antibodies against VLA-4
        
        reduce extravasation of lymphocyte
      - vedolizumab
        
        MOA
        
        mab to integrin alpha 4- beta 7
        
        reduced estravastration of lymphocytes into GI tract
        
        use: induction and maintenance o
        
        CD
        
        UC
        
        AE
        
        similar to natalizumab
        
        less leukoencephalopathy
    - - MOA
        
        prevent it from activating TNFR
        
        mab binds to soluble and membrane bound TNF
        
        TNF function
        
        one of the key proinflammatory cytokines in IBD
        
        produced by various immune cell
        
        biological activity mediated by binding to TNR receptor
        
        TNF bind to TNF R
        
        NFkB activation
        
        proinflammatory cytokines
        
        T cell activation
        
        proliferation
        
        apoptosis
      - use
        
        crohn's disease
        
        induce and maintain remission
        
        infliximab
        
        adalimumab
        
        certolizumab
        
        drug of choice for fistulizing crohn's disease
        
        ulcerative colitis
        
        induce and maintain remission
        
        infliximab
        
        adaliumab
        
        golimumab
      - AE
        
        TB infection
        
        must undergo TB test
        
        hypersensitivity
        
        malignancy: lymphoma
        
        infliximab: antibodies to antibodies attenuate or eliminate
        the clinical response
        
        rare severe hepatic reactions
        
        acute infusion reaction
        
        fever
        
        HA
        
        dizziness
        
        urticaria
        
        hypotension
        
        SOB
        
        muscle spasm
        
        chest discomfort
      - drugs
        
        infliximab
        
        chimeric mouse-human
        
        IgG1 monoclonal antibody
        
        IV
        
        t 1/2 = 8-10 d
        
        human IgG1 monoclonal antibody
        
        adalimumab
        
        SQ
        
        t1/2 = 10-20d
        
        golimumab
        
        IV, SQ
        
        t 1/2 = 14d
        
        certolizumab pegol
        
        humanized Fab fragment linked to two PEG molecules
        
        IV
        
        t 1/2 = 14 d
  - - - inhibition of PLA2
        
        decrease synethesis of
        
        prostaglandin
        
        leukotrienes
      - decrease gene transcription
        
        NOS
        
        COX 2
        
        NFkB
        
        decrease inflammatory
        
        cytokines
        
        chemokinines
    - - ulcerative colitis
      - crohn's disease
    - - oral
      - controlled release
      - enemas
      - suppositories
    - - prednisone
      - budesonide
      - hydrocortisone
    - - osteoporosis
        
        decrease osteoblast
        
        increase osteoclast
      - moon face
        
        fatty acid deposition
      - sus infection
        
        immunosupression
      - hyperglycemia
        
        more broken down protein
        
        thin extremities
        
        thin skin
        
        purple strae
        
        bruises and petechiae
      - Na and fluid retention
        
        aldosterone effect
  - - - diarrhea
      - ab pain
      - bleeding
      - anemia
      - weight loss
      - sub types
        
        CROHN'S DISEASE
        
        granulomatous inflammation of entire wall (transmural)
        
        regional lymph node
        
        complication
        
        abcesses
        
        fistulas
        
        stenosis
        
        colon cancer
        
        ULCERATIVE COLITIS
        
        neutrophil dominated inflammation of mucosa/ submucosa
        
        complication
        
        bleeding
        
        toxic megacolon
        
        colon cancer
- - - - MOA
        
        D2 RECEPTOR ANTAGONIST
        
        stimulate antral and small intestinal contractions
        
        increase lower esophageal shincter tone
        
        5 HT4 AGONIST
        
        5 HT3 ANTAGONIST
      - use
        
        impaired gastric emptying
        
        post-surgery
        
        diabetic gastroparesis
        
        prevention of vomitting
        
        GERD sx relief
        
        antiemetic
        
        GERD
      - AE
        
        CNS :cry: :sleeping:
        
        depression
        
        schizophrenia
        
        extrapyramidal effects "extra
        
        parkinson
        
        tremor
        
        rigidity
        
        tardive dyskinesia
        
        "spicy food
        
        lips smacking
        
        tongue moving
        
        long terms used
        
        prolactin :arrow_up:
        
        galactorrhea
        
        gynecomastia
        
        impotence
        
        menstrual disorder
    - - MOA
        
        5-HT4 AGONIST
        
        secretory function
        
        produced by EC cell in response to chemical and mechanical stimulation
        
        triggers peristaltic reflex
        
        NORMAL MOTOR
        
        weak 5 HT3 antagonist
      - use
        
        gastroparesis
        
        GERD
      - AE
        
        TORSADE DE POINTES
        
        (blocked K channel)
        
        prolonged QT interval
        
        cardiac arrhtymias :revolving_hearts:
        
        make sure ECG before prescribing
        
        available via restricted investigational drug protocol
      - INTERACTION
        
        CYP3A4 metabolism
    - - MOTILIDES
        
        motilin
        
        peptide hormone
        
        GI M cell and EC cell
        
        contractile agent of upper GI tract
      - use: diabetic gastroparesis
      - AE
        
        downregulation of motilin receptor = tolerance
        
        antibiotic AE
  - - - BULK FORMING AGENTS
        
        absorb water into colon
        
        form bulky, emollient gel
        
        increase peristalsis
        
        1-3 days softening feces
        
        drugs
        
        methylcellulose
        
        calcium polycarbophil
        
        psyllium
        
        important: DRINK LOTS OF WATER
      - OSMOTIC AGENTS
        
        nonabsorbable osmotic agents
        
        increase secretion of water
        
        softening stool
        
        promote defecation
        
        drugs
        
        saline laxative: MOM
        
        AE: hypermagnesia = avoid in renal disease
        
        nondigestble sugar and alcohol
        
        LACTULOSE
        
        MOA
        
        colonic bacteria metabolize forming
        
        2 more items...
        
        increase motility and secretion
        
        use
        
        IBS
        
        hepatic encephalopathy
        
        2 more items...
        
        AE
        
        ab pain
        
        flatulence :wind_blowing_face:
        
        diarrhea :toilet:
        
        sorbitol
        
        PEG: clean out b4 procedure
      - SOFT WETTING AGENTS
        
        DOCUSATE SALTS
        
        24-72H
        
        Anionic surfactants
        
        lower surface tension
        
        more mixing aqueous and fatty substances
        
        stool softening
        
        1 more item...
        
        MINERAL OIL
        
        oral drug
        
        soften tool
        
        AE
        
        decrease fat-soluble absorption
        
        aspiration if severe lipid pneumonitis
        
        take while upright, not lying down
    - - BISACODYL
        
        prodrug: require hydrolysis in bowel
        
        induce bowel movement
        
        PO: 6-12h
        
        suppository: 30-60min
        
        AE
        
        ab pain
      - ANTHRAQUINONE LAXATIVE
        
        drugs
        
        cascara
        
        senna
        
        aloe
        
        prodrug: activated by gut flora
        
        induce bowel movement
        
        6-12h
        
        AE
        
        melanotic pigmentation of colon
        
        melanosis coli (harmless)
      - CASTOR OIL
        
        prodrug: hydrolysis in gut into
        
        gycerol
        
        ricinoleic acid (active agent)
        
        laxative effect 1-3h
        
        AE
        
        unpleasant taste
        
        ab pain
    - - LUBIPROSTONE :
        
        use
        
        chronic constipation
        
        IBS-C (constipation)
        
        24h onset
        
        AE
        
        nausea :nauseated_face: b/c trigger GI motility
        
        diarrhea
        
        HA
        
        : pregnancy :forbidden: :pregnant_woman:
        
        MOA: PROSTAGLANDIN ANALOG
        
        stimulate EP4 RECEPTOR, Gs
        on GI epithelial cells
        
        increase Cl- activity
        
        increase fluid and electrolyte secretion
        
        increase motility
      - LINACLOTIDE, PLECANATIDE
        
        :forbidden: :baby: :children_crossing:
        
        MOA
        
        stimulate receptor coupled to Gc-C receptor
        on GI epithelial cell
        
        increase Cl- channel activity
        
        increase fluid and electrolyte secretion
        
        increase motility
        
        AE:
        
        diarrhea :toilet:
        
        ab pain
  - - - LOPERAMIDE
        
        use
        
        travel diarrhea
        
        acute/ chronic diarrhea
        
        AE
        
        ab pain
        
        constipation :poop:
      - DIPHENOXYLATE ->DEFENOXIN/ atropine
        
        AE
        
        CNS
        
        depression :frowning_face:
        
        HA
        
        dizziness :dizzy:
        
        anticholinergic
        
        dry mouth
        
        blurred vision
        
        urinary retention
        
        constipation :poop:
      - MOA
        
        decrease peristaltic contraction
        
        increase segmental contraction
        
        increase transit time
        
        increase anal sphincter tone
        
        anti-secretory activity against cholera toxin/ E.coli toxin
    - - MOA
        
        bind bile salts + bacteria
        
        decrease unbound bile acid
        
        decrease fluid/electrolyte secretion
      - use
        
        diarrhea caused by excess fecal bile
        
        resection of distal ileum
        
        crohn's disease
      - cholestyramine, colestipol, colesevalam
        
        AE
        
        constipation :poop:
        
        bloating 😮‍💨
    - - MOA
        
        direct antimicrobial effects
        
        binds enterotoxin
      - use
        
        peptic ulcer (H.pylori)
        
        acute diarrhea
        
        travelers diarrhea
      - AE
        
        black tongue
        
        black stool
        
        :forbidden: :children_crossing: Reye's syndome
    - - MOA
        
        master inhibitor found in hypothalamus
        
        cholecystokinin
        
        vasoactive intestinal peptide
        
        5-HT
        
        gastrin
        
        decrease intestinal fluid secretion, pancreatic secretion
        
        decrease GI motility
      - somatostatin short half life 3 min
      - octreotide
        
        PK 1.5h
        
        AE
        
        short-term: :nauseated_face:, pain at injection site
        
        longterm use: gallstrone / hypo + hyperglycemia
  - - - block M3 on Gi smooth muscle
        
        decrease contractions
        
        antispasmodic
    - - ab pain
    - - antimuscarinic
- - - - H2 RECEPTOR ANTAGONIST (tidine)
        
        cimetidine AE
        
        gatactorrhea
        
        gynecomastia/ impotence
        
        INCREASE PROLACTIN
        
        other -tidine AE
        
        increase risk of infection
        
        develop tolerance
      - PPI (prazole)
        
        AE
        
        decrease vit B12
        
        hypocalcemia
        
        hypomagnesia
        
        increase risk of infection
        
        enteric
        
        respiratory
        
        CYP interactions
      - ANTACIDS
        
        DRUG
        
        Mg hydroxide
        
        AE: diarrhea
        
        Al hydroxide
        
        AE: constipation
        
        NaHCO3, CaCO3
        
        AE
        
        belching
        
        gastric distension
        
        use
        
        instant relief
        
        postprandial dosing
      - metoclopramide
        
        uncommon
        
        last line if accomapny by gastroparesis
    - - increase bed of bed 6 inches
      - weight loss
      - avoid
        
        fatty food
        
        chocolate
        
        carbonated beverages
        
        alcohol
        
        citrus juices
        
        large meals
        
        tobacco
        
        post-prandial recumbency
  - - - pyrosis
      - reguritation
      - dysphagia
    - - chest pain
      - cought
      - asthma
      - recurrent sore throat
      - dental enamel loss
- - - - PROSTAGLANDIN ANALOGS (misoprostol)
        
        AE
        
        :forbidden: :pregnant_woman: increase uterine contraction
        
        diarrhea :toilet:
        
        MOA
        
        stimulate EP3 receptors on parietal cells + surface mucous cell
        
        decrease cAMP
        
        decrease H+
        
        stimulate EP3 receptor surface mucous cell
        
        increase mucous secretion
        
        increase HCO3
        
        use: NSAID induced ulcer
      - BISMUTH SUBSALICYLATE
        
        MOA
        
        direct antimicrobial effects
        
        binds enterotoxin
        
        coat ulcer
        
        use
        
        peptic ulcer (H.pylori)
        
        acute diarrhea
        
        travelers diarrhea
        
        AE
        
        black tongue
        
        black stool
        
        :forbidden: :children_crossing: Reye's syndome
      - SUCRALFATE
        
        use: peptic ulcer
        
        minimal AE
        
        MOA: forms viscous paste that adheres to ulcers
      - PPI + antibiotics
      - H2 receptor antagonist
    - - discontinue NSAIDs
      - diet change similar to GERD
      - smoking cessation
  - - - H. pylori
      - NSAIDs
- - - - chronic EtOH
      - hepatitis B and C
      - drug toxicity I.e acetaminophen
    - - hepatocyte death
      - increase collagen deposistion from Stellate cells
    - - increase portal vein pressure
        
        portal vein HTN
    - - decrease urea cycle
        
        increase NH3
      - decrease gluconeogenesis
      - decrease clotting factor
  - - - jaundice
      - dark urine
    - - gynecommastia, ED, testicular atrophy
  - - - increase post-portal vein resistance from liver fibrosis
      - splanchnic vasodilation
      - esophageal varices = acute hemorrhage
      - treatment:
        
        propranolol
        
        MOA
        
        nonselective beta blocker
        
        beta 2
        
        decrease splanchnic vasodilation
        
        1 more item...
        
        octreotide
        
        MOA
        
        somatostatin receptor agonist (Gi)
        
        decrease release of vasodilator
        
        decrease splanchnic vasodilation
        
        1 more item...
        
        also treat hormone secreting tumor syndromes
        
        AE
        
        ab pain
        
        diarrhea :toilet:
        
        NV
        
        gallstone - decrease gallbladder contraction
        
        vasopressin
        
        MOA
        
        activate V1 receptor (Gq)
        
        splanchnic vasoconstriction (upstream of portal vein)
        
        decrease portal pressure
        
        1 more item...
        
        rarely used
        
        AE
        
        HTN
        
        hyponatremia (stimulate V2 in kidney = water retention
    - - edema in peritoneal cavity from
        
        increase cap pressure in GI capillaries
        
        hyperaldosterone
        
        decrease osmotic
      - treatment: spironolactone
        
        MOA
        
        block mineralcorticoid receptor
        
        decrease renal sodium retention
        
        block androgen receptor
        
        AE
        
        hyperkalemia
        increase K retention
        
        gynecomastia, sexual dysfunction
    - - treatment
        
        LACTULOSE
        
        MOA
        
        colonic bacteria metabolize forming
        
        formic acid
        
        acetic acid
        
        increase motility and secretion
        
        use
        
        IBS
        
        hepatic encephalopathy
        
        acidify gastric content
        
        convert NH3 to NH4+
        
        NH3 not go to brain
        
        AE
        
        ab pain
        
        flatulence :wind_blowing_face:
        
        diarrhea :toilet:
        
        rifaximin
        
        MOA
        
        nonabsorbable antibiotic
        
        kill GI bacteria that metabolize urea to NH3
        
        AE
        
        ab pain
        
        nausea