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Pharmacology - Final - Part 2

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davidwurbel7's version from 2016-08-14 17:37

Immunopharmacology

Question Answer
Inhibit MHC expression. Block cytokine gene expression. Inhibit proliferation of T lymphocytes. Either used alone or in combination with other drugs. Limitation: Long term complicationsCorticosteroid
They commonly are combined with other immunosuppressive agents to prevent and treat transplant rejection. High dose pulses of intravenous. Used to reverse acute transplant rejection and acute exacerbations of selected autoimmune disordersCorticosteroid
Adverse effects include Growth retardation in children, Osteomalacia, Increased risk of infection, Poor wound healing, Cataracts, Hyperglycemia and HypertensionCorticosteroids
Binds to cyclophilin. The complex inhibits calcineurin which decreased IL-2, IL-3 and IFN productionCyclosporin
Binds to FK-binding protein (FKBP). The complex inhibits calcineurin which decreased IL-2, IL-3 and IFN productionTacrolimus
Used in Kidney, liver, heart, and other organ transplantation, Rheumatoid arthritis and PsoriasisCyclosporin and Tacrolimus
Usually is combined with other agents, especially glucocorticoids and azathioprineCyclosporin
Adverse effects include nephrotoxicityCyclosporin and Tacrolimus
This drug interaction increases the concentration of cyclosporin and tacrolimus due to a decrease in metabolismCYP Inhibitors
This drug interaction decreases the concentration of cyclosporin and tacrolimus due to an increase in metabolismCYP Inducers
Inhibits T-lymphocyte activation and proliferation decreasing production of IL-2. It binds to and inhibits a protein kinase, designated mammalian target of rapamycin (mTOR)Sirolimus (Rapamycin)
Adverse effects include dose-dependent increase in serum cholesterol and triglycerides, Anemia, Leukopenia and ThrombocytopeniaSirolimus (Rapamycin)
The mechanism of action inhibits inosine monophosphate dehydrogenase-enzyme in denovo purine synthesisMycophenolate Mofetil
This drug is used transplant rejection- is typically used in combination with glucocorticoids and a calcineurin inhibitorMycophenolate Mofetil
The mechanism of action inhibits enzyme required for ribonucleotide synthesis. Used as a secondary drug for rheumatoid arthritisLeflunomide
This drug spontaneously converts to 6-mercaptopurine which inhibits purine metabolismAzathioprine
This drug is an anti-TNF-a monoclonal antibody. Currently used for Rheumatoid arthritis and Crohn's diseaseInfliximab
The mechanism of action binds to the CD3. Antibody treatment induces rapid internalization of the T-cell receptor. This prevents subsequent antigen recognitionMuromonab
Can only used for acute rejection and is combined with corticosteroidsMuromonab
Blocks IL-2 receptors. Used organ transplant rejection reactionDaclizumab
TNF-Alpha antagonist. Used Rheumatoid arthritis, crohn’s diseaseInfliximab
Antagonist at gpIIb/IIIa receptor. Use: as antiplateletAciximab
Bind to CD20 antigen on B lymphocytes. Use: Non Hodgkins lymphomaRituximab
Bind to HER2 protein. Use: Carcinoma breastTraztuzumab
Use- respiratory syncytial virus (RSV) infectionPalivizumab
Human IgG against Rh(D) antigen. Use: administer to a Rh–ve mother with Rh+ve foetus. Anti-D is given within 72 hrs of delivery/abortion -- Prevent of haemolytic disease in subsequent pregnancyAnti-D Immunoglobulin
Available only under a restricted distribution program. The mechanism of action is inhibits TNF-alpha, reduces phagocytosis. Use: Erythema nodosum leprosum (ENL) and in multiple myelomaThalidomide
Recombinant interleukin-2. Used in renal cell carcinoma, malignant melanomaAldesleukin
Used in hairy cell leukemia, CML, kaposi’s sarcoma and hepatitis BInterferon Alpha-2a
Used in multiple sclerosisInterferon Beta-1b
Used in chronic granulomatous diseaseInterferon Gamma-1b
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Drugs of Abuse
(Insert all)

Review

Pharmacokinetics / Pharmacodynamics
pH
Equations
Protein Binding
Drug Metabolism - Phase I and Phase II
Drug Metabolism - CYP Inducers and CYP Inhibitors
Dose response curves - Potency and EC
Dose response curves - Receptor binding for agonist and antagonist
Dose response curves - Therapeutic Index

 

ANS
Reserpine
Release and Reuptake
G-proteins and secondary messengers
Gq - alpha 1, M1, M3
Gs - beta
Gi - alpha 2, M2
Receptor effect on various organ system
Drug toxicities
Dose depend effects - Dopamine
low dose - D1
moderate dose - beta1
high dose - alpha1
post operative iliac paralytersis - Bethenocol
cholinergic drugs - glaucoma
Increase drainage - Pilocrapine, physostigmine, Latanoprost
Decrease secretion - Timolol, Apraclonidine Acetazolamide
Emergency glaucoma - Mannitol
Contraindicated in glaucoma - Antimuscarinic drugs
Asthma drugs - all
Benztropine - Parkinson extrapyramidal symptoms
Sympathetic drugs - effects on receptors - Epi, Norepi, Dobbitamine, Isoproterenol, Fenoldopam, Amphetamine, Cocaine, Ephedrine
Blood pressure, heart rate, peripheral resistance graphs
Alpha 2 drugs - methyldopa, clonidine
Alpha blockade - Epinephrine with alpha blockers

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