Drugs Flashcards
Mechanism of Steroids
bind to cytoplasmic receptor found in all cells then enter the nucleus to affect transcription
- down-regulation of NF-kB
- induction of inhibitory-kB
- reduced phagocytic activity and migration of neutrophils
- apoptosis of lymphocytes
- NO is produced
- decreased prostaglandins
- IL-10 increased
Mechanism of IFX
Anti-tumor necrosis factor
- induces apoptosis of cells expressing membrane TNF
- blocks leukocyte migration
- complement fixation -binding of serum complement to an antigen-ab
Mechanism of 5-ASA
- Inhibition of adhesion of macrophages and neutrophils
- Inhibition of synthesis of prostaglandins (COX) and leukotrienes
- Impairment of white cell adhesion and functioning during acute inflammation
- free radical scavenging and antioxidant activity
Anti-secretory agents for slowing down diarrhea
- octreotide
- Anthicholinergics: scopolamine
- clonidine (alpha 2 adrenergic agonist)
- bismuth
- cholestyramine
Function of Loperamide and Lomotil
-mu opioid receptor agonist
Side effects of Octreotide
- hyperglycemia,
- increased gallstone formation in pts w/ acromegaly,
- decreased linear growth (suppression of growth hormone),
- abdominal bloating,
- hypothyroidism: suppresses TSH (but hypoT4 is rare),
- sinus bradycardia,
- headache.
What class of medication is Baclofen
- GABA agonist
- decrease number of TLESRs
- accelerates gastric emptying
Mechanism of Tacrolimus
- Macrolide antibiotic
- Binds to cytoplasmic receptors (FK binding protein 12)
- inhibits calcineurin:
1. enzyme required in T-cell receptor signalling and activation
2. inhibits cytokines IL-2
Mechanism of Cyclosporin
- inhibits calcineurin:
1. enzyme required in T-cell receptor signalling and activation
2. inhibits cytokines IL-2
-binds cyclophilin
Adverse effects of Tacrolimus and Cyclosporin
- Renal
- HTN
- Renal toxicity
- Electrolyte abnormalities: Hyperkalemia, hypomagnesemia
2.ID:
Opportunistic infections (PCP, Aspergillus)
-PTLD
-impaired wound healing
- Neurologic:
- Focal neurologic deficiets
- psychosis
- tremor
- seizures - Endocrine:
- Hyperlipidemia
- increased risk of DM - Cyclosporine Specific
- hypertrichosis
- gingival hyperplasia
- course facial features
- increased squamous-cell skin cancers - Tacrolimus specific
- alopecia
MMF mechanism of action
- hydrolyzed to the active immune suppressor MPA
- blocks de novo purine nucleotide synthesis by inhibiting type 2 IMPDH
- impairs B- and T- cell proliferation
- can be combined with Tac in ACR for:
- tapering steroids
- limites tac toxicity
Sirolimus (Rapamycin) MOA
- macrolide Abx that binds FK-binding protein
- acts via target of rapamycin (TOR)
- Inhibits G1 to S-phase cell division preventing proliferation
- inhibits B-cell proliferation and growth factor mediated proliferation of immune cells
- does not have nephrotoxicity
- advocated in pts who undergo LT for HCC
- Associated with hepatic artery thrombosis and poor wound healing
Domperidone
-D2, D3 antagonist
Metaclopramide
D2 antagonist
5HT4 agonist
5HT3 antagonists
Cisapride
5HT3 antagonist, 5HT4 agonist