Flashcards in Immunosuppressives, Autonomics Deck (16):
1
Cyclosporine/Tacrolimus
-inhibits calcineurin phosphatase activity
-Dec. dephosphorylation of NFAT
-T-cell selective
-renal toxicity
-hyperglycemia with tacrolimus
2
Sirolimus/Everolimus
-same family as tacrolimus/cyclosporine
-blocks T cell response to cytokines & inhibits a kinase involved in cell-cycle progression
-hyperlipidemia as adverse effect
-Everolimus-closely related to sirolimus; shorter half-life, quicker time to achieve steady-state concentration
3
Azathioprine/6-Mercaptopurine
-Dec. purine biosynthesis
-fraudulent nucleotide
-allopurinol interaction
4
Mycophenolate Mofetil
-inhibits inosine monophosphate dehydrogenase & dec. de novo purine biosynthesis
-T and B cell sensitive due to lack of salvage pathway
-related drug: mizoribine
5
Cyclophosphamide
-alkylates DNA
-effects on rapidly proliferating cells
6
Methotrexate
-inhibition of DHFR
7
Antithymocyte Globulin
-Mixture of cytotoxic antibodies to various CD molecules
-Adverse effects: fever, chills, hypotension
8
Muromonab CD3
-Antibody that blocks binding of APC to T-cell: Blocks T-cell function & Decreases T-cell number
-Initial stimulation of cytokine release syndrome
9
Daclizumab, Basiliximab
-Monoclonal antibodies against IL-2 receptor, Blocks IL-2 mediated T-cell activation
-Potential anaphylactic reactions
10
Cholinergic activating agents - - bethanechol, neostigmine
-stimulate bladder emptying
-treatment of urinary retention problems post surgery
-only used with no obstructive problems
11
Anti-cholinergics - - tolterodine, oxybutynin, darifenacin, solifenacin, fesoterodine
-relaxes bladder, slows voiding
-treatment of bladder spasms post surgery or due to inflammation & treatment of urinary incontinence
12
Alpha-1 agonists - - ephedrine, pseudoephedrine
Used for the Tx of urinary incontinence
13
Alpha-1 antagonists - - prazosin, terazosin, doxazosin, tamsulosin
-treatment of symptoms of urinary obstruction (BPH)
-tamsulosin greater potency in inhibiting contraction in prostate smooth muscle vs. vascular smooth muscle
14
Propanolol
-Nonselective Beta blocker-Competitive block of β receptors, local anesthetic effect
-Beta2-involved in relaxing the detrusor muscle, therefore, beto blockade should increase contractility of detrusor.
-Beta1-involved in the release of renin, therefore, beta blockade should dec. GFR and cause dec. urine production.
-Uses-Angina, arrhythmias (treatment and prophylaxis), hypertension, thyrotoxicosis, tremor, stage fright, migraine
-Oral and IV Duration: 4–6 h. Ready entry into CNS
-Tox-Excessive β blockade: bronchospasm (can be fatal in asthmatics), atrioventricular block, heart failure, CNS sedation, lethargy, sleep disturbances
15
Metoprolol, atenolol
-Competitive block of β1 receptors
-Uses-Hypertension, angina, arrhythmias
-Oral, Duration: 6–9 h
-Tox-Like propranolol with somewhat less danger of bronchospasm
-Metoprolol-like atenolol, oral, shown to reduce mortality in heart failure
16