Immunosuppressives, Autonomics Flashcards Preview

Renal Pharm > Immunosuppressives, Autonomics > Flashcards

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

Autonomic Pharmocology: what are the effects of M3, alpha1, beta1, and beta2 receptors?

-Muscarinic M3 receptor: contracts detrusor muscle of bladder, relaxes trigone and sphincter
-beta2-relaxes bladder smooth muscle
-alpha1-contracts bladder base, urethral sphincter, prostate
-beta1-increases renin release