What are the 6 drug classes used for tx of IBD?
- aminosalicylates
- corticosteroids
- Abx
- immunosuppressive
- IV cyclosporine
- Immune modifies
Aminosalicylates:
- 2 MC medications
- uses
- Routes of Adminitration
2MC medications: Sulfasalazine and Mesalamine
Use: 1st line
-induce and maintain remission in UC & Crohns
Routes of Administration: -PO
- Enema
- Suppository
Sulfasalazine:
- pregnancy category?
- unique characteristic
- CI
- frequency of administration
Pregnancy ca. B
Unique: converted to mesalamine in the proximal colon
Frequency: tablets administered 4x daily
CI in sulfa allergy
Mesalamine:
- pregnancy category
- routes of administration
- unique features
Pregnancy: B
Routes:
- PO tablet/capsule
- enema
- rectal suppositores
Unique: poorly absorbed through the GI tract so works primarily like a topical agents with limited systemic SE and drug interactions.
aminosalicylates:
- moa
- CI
- dosing
MOA:
- unknown
- blocks prostaglandin production, perhaps interfers with production of inflamm cytokines, may inhibit NK cells, lymphocytes, and mfs.
CI :
- aspirin or salicylate allergy
- G6PD
- hx of sulfa allergy
Dosing:
- must be used at max dose for max therapeutic effect
- varies from once daily to 4x/day
Sulfasalazine:
- SE
- WHat labs must you monitor?
- Worst side effect profile of all aminosalicylates
- n/v
- photosensitivity
- oligospermia
- skin discoloration
- decreased folate levels (Must take folic acid supplement)
- Severe: SJS, hepatitis, bone marrow suppression.
Labs:
- CBC
- LFT
- renal
Mesalamine
- SE
- what labs must be monitored?
HA, malaise, abd pain, diarrhea
Labs:
- renal function
- CBC
- LFT
Corticosteroids
- when do you use these?
- short and long term SE
- medication names
Used for acute exacerbations, NOT used for maintaining remission
SE:
Short -psychosis, elevated blood sugar, HTN, upset stomach, insomnia
Long:osteoporosis, obesity (buffalo hump), cataracts, suppression of pituitary adrenal axis, hirsutism
Meds:
-Prednisone or Prednisolone: IV = hydrocortisone and methylprednisolone.
-Budesonide (poor bioavailability , good b/c stays in the gut.
Topical:
-cortenema, cortifoam, anusol-HC suppositories
Abx:
- what medications?
- use
Ciprofloxacin
Metronidazole
take at least 1mo to induce sx improvement
Use:
used when pt doesnt respond to 5-ASA (mesalamine) after 3-4wks or if pt is intolerant to 5-ASA
(add on or 2nd line therapy)
Immune Moddifiers
- what are the medication names?
- clinical use
- time to sx reduction
- MOA
Meds:
- azathioprine*
- 6-mercaptiopurine*
- methotrexate
- infliximab
- cyclosporine
Use:
induction and maintenance of remission
-allows reduction of steroid therapy
Time to sx reduction: 17wks
MOA:
-inhibition of purine neucleotide metabolism and DNA synthesis and repair, resulting in inhibition of cell division and proliferation.
(*decrease proliferation of immune cells leading to lower autoimmune activity)
Azathioprine and 6-mercaptopurine
- SE
- CI
SE:
- n/v/d
- fever, rash
- pancreatitis
- bone marrow suppression*
- hepatic toxicity
- arthralgias, malaise
- drug toxicity with concurrent use of allopurinol
CI:
- CI in pregnancy or active liver dz
- decrease dose for CrCl less than 50
Whenever using immune suppression drugs what 3 organs are we most concerned with?
Kidneys, Liver, BM
Methotrexate
- use
- routes of administration
- MOA
- Pregnancy category
- SE
use: induction and maintenance
Routes: PO, SQ, IM
MOA:
- inhibits metabolism of folic acid
- interferes with inflamm actions
- may stimulate apoptosis and death of activated T lymphos.
- *Make sure on folic acid supplements**
Pregnancy cat X
SE:
- alopecia
- muscositis
- BM suppression
- megaloblastic anemia
- cirrhosis and liver fibrosis
- penumonitis
- folic acid deficiency
- rash
- nause and diarrhea
Cyclosporine
- use
- time to sx relief
- routes of admin
- SE
Use: used for acute tx of severe, steroid refractory exacerbations
Sx relief in 2-3days
Routes of admin: IV
SE: nephrotoxicity, hypomagnesemia, HTN
anti- TNF inhibitors
- use
- medications
- MOA
- SE
- BBW
Uses: severe dz, when not responding to steroids.
must get TB test prior to use of this drug
Meds:
- infliximab (Remicade)
- Adalimumab (Humira)
- Certolizumab Pegol (Cimzia)
MOA: monoclonal abys dial down the immune system
SE:
- fever chills, pruritis, urticaria, chest pain, hemodynamic instability = infusion rxns
- delayed infusion rxns: myalgia, athralgia, rash, urticaria, facial, hand, and lip edema
BBW:
-reactivation of latent TB!!!!!!!!!!!!!!!!!!!!!!!!!!!!!!!!!!!
Overview of medical therapy: describe the stepwise Rx order of IBD medications
5-ASA… if no response give Abx….if no response… oral steroids… if no response… immunosuppressive drugs.
*skip ABX step if treating UC.
5-ASA …complete response = maintenance.
T/F, use of combo oral and rectal 5-ASA have better efficacy than either agent alone?
True.
IBS
-therapy is based on what?
Symptomology, ie. constipation or diarrhea.
Tx constipation
Tx Pain
Tx Diarrhea
Constipation: Increase fluids and fiber TCA or SSRI Peppermint oil osmotic laxatives lubiprostone
Pain:
- antispasmodics (anticholinergics)
- TCAs
- SSRI
- Peppermint oil
Diarrhea;
- fiber
- loperamide
- cholestyramine
- TCA
- lotronex
- SSRI
Antispasmodics:
- medications
- MOA
- SE
- CI
- which med is 1st line?
- dosage
Meds:
Anticholinergics: Hyoscyamine (levbid), dicyclomine (bentyl)
MOA:
- block action of Ach at muscarinic cholinergic receptors.
- reduce contraction of bowel**
SE:
anticholinergic
CI:
- peptic ulcer
- arrhythmia
- CHF
- Glaucoma
1st line is Bentyl
Dosage: PRN
Anti-constipation agents:
-meds
MedS: Miralax/polyethylene glycol (osmotic)
Lubiprostone, linaclotide
Chloride Channel Activator: LUBIPROSTONE
- MOA
- use
- SE
MOA: locally acting calcium channel activator that increases intestinal fluid secretion.
uSe; approved for women with CONSTIPATION predominant IBS
SE:
- n/d
- abd pain
- abd distention
Chloride Channel Activator: Linaclotide (Linzess)
- MOA
- Admin route
MOA: binds to GC-C receptor on intestinal epithelium and increases intestinal fluid.
route: once daily in Am after eating
Psychotrophic Agents used in IBS?
TCAS:
- amitryptyline
- desipramine
- imipramine
SSRI:
- escitalopram (lexapro)
- citalopram (celexa)
- sertraline (Zoloft)
- paroxetine (Paxil)
- fluoxetine (Prozac)
